ЛЕКАРСТВЕННЫЙ ПРЕПАРАТ И ПИЩЕВОЙ ПРОДУКТ ИЛИ НАПИТОК ДЛЯ УЛУЧШЕНИЯ ГИПЕРГЛИКЕМИЧЕСКОГО СОСТОЯНИЯ

FIELD: medicine; pharmacology. SUBSTANCE: invention refers to medicinal agent applied for improved hyperglycemia containing 9,19-cyclolanostan-3-ol and/or 24-methylene-9,19-cyclolanostan-3-ol or extract made by extraction with organic solvent or hot water of plant selected from group Liliaceae, Gramineae and Solanaceae, or its part, food substance or beverage, application of 9,19-cyclolanostan-3-ol and/or 24-methylene-9,19-cyclolanostan-3-ol for production of medicinal agent for improved hyperglycemia and method of improved hyperglycemia including introduction of 9,19-cyclolanostan-3-ol and/or 24-methylene-9,19-cyclolanostan-3-ol or composition containing given compound (compounds). EFFECT: agent has improved efficiency. 13 cl, 4 tbl, 3 ex ÐÎÑÑÈÉÑÊÀß ÔÅÄÅÐÀÖÈß RU (19) (11) 2 327 463 (13) C2 (51) ÌÏÊ A61K 31/575 (2006.01) A61K 36/886 (2006.01) A61P 3/10 (2006.01) ÔÅÄÅÐÀËÜÍÀß ÑËÓÆÁÀ ÏÎ ÈÍÒÅËËÅÊÒÓÀËÜÍÎÉ ÑÎÁÑÒÂÅÍÍÎÑÒÈ, ÏÀÒÅÍÒÀÌ È ÒÎÂÀÐÍÛÌ ÇÍÀÊÀÌ (12) ÎÏÈÑÀÍÈÅ ÈÇÎÁÐÅÒÅÍÈß Ê ÏÀÒÅÍÒÓ (21), (22) Çà âêà: 2006116567/15, 30.03.2005 (24) Äàòà íà÷àëà îòñ÷åòà ñðîêà äåéñòâè ïàòåíòà: 30.03.2005 (30) Êîíâåíöèîííûé ïðèîðèòåò: 29.09.2004 JP 2004-283549 (43) Äàòà ïóáëèêàöèè çà âêè: 10.12.2007 R U (72) Àâòîð(û): ÕÈÃÓÒÈ Ðèóóèòè (JP), ÈÍÀÃÀÊÈ Ìàñàíîðè (JP), ÕÀßÑÀÂÀ Õèðîòîñè (JP), ßÌÀÄÀ Ìóíåî (JP), ÒÀÍÀÊÀ Ìèþêè (JP), ÌÈÑÀÂÀ Ýðèêî (JP), ÂÀÊÈÌÎÒÎ Íîðèêî (JP), ÈÒÎÓ Éîóñóêå (JP) (45) Îïóáëèêîâàíî: 27.06.2008 Áþë. ¹ 18 (85) Äàòà ïåðåâîäà çà âêè PCT íà íàöèîíàëüíóþ ôàçó: 15.05.2006 2 3 2 7 4 6 3 R U (87) Ïóáëèêàöè PCT: WO 2006/035525 (06.04.2006) C 2 C 2 (86) Çà âêà PCT: JP 2005/006021 (30.03.2005) Àäðåñ äë ïåðåïèñêè: 129010, Ìîñêâà, óë. Á.Ñïàññêà , 25, ñòð.3, ÎÎÎ "Þðèäè÷åñêà ôèðìà Ãîðîäèññêèé è Ïàðòíåðû", ïàò.ïîâ. Å.Å.Íàçèíîé, ðåã. ¹ 517 (54) ËÅÊÀÐÑÒÂÅÍÍÛÉ ÏÐÅÏÀÐÀÒ È ÏÈÙÅÂÎÉ ÏÐÎÄÓÊÒ ÈËÈ ÍÀÏÈÒÎÊ ÄËß ÓËÓ×ØÅÍÈß ÃÈÏÅÐÃËÈÊÅÌÈ×ÅÑÊÎÃÎ ÑÎÑÒÎßÍÈß (57) Ðåôåðàò: Èçîáðåòåíèå îòíîñèòñ ê îáëàñòè ôàðìàêîëîãèè è ìåäèöèíû è êàñàåòñ ñðåäñòâà äë óëó÷øåíè ãèïåðãëèêåìè÷åñêîãî ñîñòî íè , ñîäåðæàùåãî 9,19 ...

14,17-C2-МОСТИКОВЫЕ СТЕРОИДЫ И ФАРМАЦЕВТИЧЕСКИЙ ПРЕПАРАТ

Изобретение относится к 14,17-C2-мостиковым стероидам формулы I, где R3 - O, R6 - H, α или β-(С1-С4)-алкил, причем тогда R6′ и R7 вместе образуют дополнительную связь; R7 - α- или β-(С1-С4)-алкил, причем тогда R6 и R6′- оба Н, или R9 и R10 каждый Н или вместе образуют связь, R11 и R12 каждый Н или вместе образуют связь, R13 - СН3 или С2H5; R15 - H или С1-С3-алкил; R16 и R16′ независимо Н, (С1-С3)-алкил или С1-С4-алкенил или вместе образуют (С1-С3)-алкилиден; R15 и R16 вместе образуют цикл где n = 1, а Х - О и R16 - Н, - H, (С1-С3)-алкил, - H, (С1-С3)-алкил, и каждый Н или вместе образуют связь, R21 - H или (С1-С3)-алкил, R21′ - H, (С1-С3)-алкил или ОН; за исключением 14,17-этано-19-норпрегн-4-ен-3,20-диона. Соединения проявляют очень высокую гестагенную активность, а также оказывают воздействие на другие стероидные рецепторы, что используется в фармацевтических препаратах. 2 с. и 9 з.п.ф-лы. (I) ...

СТЕРОИДНЫЕ СОЕДИНЕНИЯ, СПОСОБ СЕЛЕКТИВНОЙ МОДИФИКАЦИИ, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ

Изобретение относится к стероидным соединениям формулы 1, где --- - необязательные двойные связи, R6- Н, =СН2, -СН3 или –СН2-СН3; R7 - Н, С1-4-алкил, С2-5-алкенил или С2-5-алкинил; R11 - Н, С1-4 -алкил, С2-4-алкенил, С2-4-алкинил, С1-4-алкилиден; Е - пяти-семичленное кольцо, образованное вместе с 16 и 17 атомами углерода, находящееся в α, цис-положении по отношению к стероидной структуре, возможно содержащее до двух двойных связей. Соединения могут применятся в терапии и в способах селективной модификации активности эстрогеновых рецепторов. 3 н. и 9 з.п. ф-лы, 1 табл.

Способ получения 3-ацетата-28-сукцината бетулинола

Изобретение относится к химико-фармацевтической промышленности и касается получения 3-ацетата-28-сукцината бетулинола – биологически активного вещества, проявляющего гепатопротекторную, антигрибковую и антидрожжевую активность. 3-Ацетат-28-сукцинат бетулинола формулы, приведенной ниже, получают сплавлением 3-ацетата бетулинола с янтарной кислотой при соотношении реагентов 1,0:1,5 при температуре 190-200 °C в течение 3-4 минут. Технический результат изобретения – упрощение процесса получения 3-ацетата-28-сукцината бетулинола, повышение его экономической эффективности за счёт резкого сокращения продолжительности процесса и исключения использования дорогих и токсичных реагентов. 2 пр.

СОДЕРЖАЩИЙ ТРИТЕРПЕН АГЕНТ ОБРАЗОВАНИЯ ОЛЕОГЕЛЯ, СОДЕРЖАЩИЙ ТРИТЕРПЕН ОЛЕОГЕЛЬ И СПОСОБ ПОЛУЧЕНИЯ СОДЕРЖАЩЕГО ТРИТЕРПЕН ОЛЕОГЕЛЯ

... 1. Применение по меньшей мере одного высокодисперсного тритерпена со средним размером частиц менее 50 мкм в олеогеле в качестве агента образования олеогеля. 2. Применение по п.1, где средний размер частиц этого по меньшей мере одного тритерпена составляет менее 10 мкм. 3. Применение по одному из предыдущих пунктов, где доля вторичных агломератов в этом по меньшей мере одном тритерпене составляет менее 20 вес.%. 4. Применение по п.3, где этот по меньшей мере один тритерпен имеет однородное распределение частиц по размерам. 5. Применение по п.1, где удельная поверхность этого по меньшей мере одного тритерпена составляет от 1 до 500 м2/г. 6. Применение по п.5, где удельная поверхность этого по меньшей мере одного тритерпена составляет от 10 до 100 м2/г. 7. Применение по п.6, где удельная поверхность этого по меньшей мере одного тритерпена составляет от 20 до 50 м2/г. 8. Применение по п.1, где доля этого по меньшей мере одного высокодисперсного тритерпена составляет более 80 вес.%. 9. Применение ...

АГЕНТ ДЛЯ СНИЖЕНИЯ ИНСУЛИНОРЕЗИСТЕНТНОСТИ

1. Агент для снижения инсулинорезистентности, содержащий соединение, представленное следующей общей формулой (1), в качестве активного ингредиента: ! ! (в формуле R1 представляет алкильную группу или алкенильную группу, содержащую 1 или 2 двойные связи, или замещенную алкильную или алкенильную группу, содержащую 1 или 2 гидроксильные группы и/или карбонильные группы, которая имеет прямую или разветвленную цепь, содержащую от 6 до 8 атомов углерода, R2 и R3, каждый независимо, представляет атом водорода или метильную группу, а R4 образует С=О с атомом углерода в составе кольца или является группой, представленной одной из следующих формул) ! ! . ! 2. Агент для снижения инсулинорезистентности по п.1, где вышеупомянутый R1 представлен любой из следующих формул, вышеупомянутые R2 и R3, оба, являются метильными группами, а вышеупомянутый R4 является гидроксильной группой ! -СН2-СН2-СН2-СН(СН3)2 ! -СН2-СН2-СНRа-С(СН3)2Rb ! (где Rа является любым из атома водорода, гидроксильной или метильной групп, а Rb является атомом водорода или гидроксильной группой) ! -СН2-СН2-СН(СН2СН3)-СН(СН3)2 ! -СН2-СН2-СНRс-С(СН3)=СН2 ! (где Rс является любым из атома водорода, гидроксильной или метильной групп) ! -СН2-СН2-С(=О)-С(СН3)=СН2 ! -СН2-СН2-С(=СН2)-СН(СН3)2 ! -СН2-СН2-СН=С(СН3)2 ! -СН2-СН=С(СН3)-СН(СН3)2 ! -СН2-СН2-С(=СНСН3)-СН(СН3)2. ! 3. Агент для снижения инсулинорезистентности по п.2, где вышеупомянутое соединение является 9,19-циклоланостан-3-олом или 24-метилен-9,19-циклоланостан-3-олом. ! 4. Агент для снижения инсулинорезистентности по любому из пп.1-3, который содержит, по меньшей мере, 0,001 мас.% вышеупомянутого соединения. ! 5. Агент для снижения инсулинорезистентности, который содержит экстракт растения орган� РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) 2008 112 884 (13) A (51) МПК A61K 31/704 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ, ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ (12) ЗАЯВКА НА ИЗОБРЕТЕНИЕ (21), (22) Заявка: 2008112884/04, 22.09.2006 (71) Заявитель(и): МОРИНАГА ...

30-(4-Гидроксиметилбензилиден)-20-оксо-29-нор-бетулин - средство тритерпеновой природы, обладающее гипогликемической активностью

Изобретение относится к химико-фармацевтической промышленности, конкретно к соединению 30-(4-гидроксиметилбензилиден)-20-оксо-29-нор-бетулин формулы (1). Изобретение обеспечивает соединение (1), обладающее гипогликемической активностью и низкой токсичностью, которое может быть использовано в доклиническом изучении в качестве потенциального препарата, снижающего уровень глюкозы в крови при гипергликемических состояниях, вызванных пониженной толерантностью к глюкозе и сахарным диабетом. 2 н.п. ф-лы, 1 табл., 3 пр.

DERMATOLOGISCHE ZUBEREITUNGEN

DERMATOLOGISCHE ZUBEREITUNGEN

GAMMA-LACTONDERIVATE UND VERFAHREN ZU DEREN HERSTELLUNG

GESTAGEN WIRKSAME 19,11-ÜBERBRÜCKTE 4-ESTRENE

16,17-CARBOCYCLISCH KONDENSIERTE STEROID-VERBINDUNGEN MIT SELEKTIVER ÖSTROGENISCHER WIRKSAMKEIT

1ALPHA,2ALPHA-METHYLEN-4-CHLOR- DELTA HOCH 4 -BZW. DELTA HOCH 4,6- 7-METHYL-VERBINDUNGEN DER PREGNANREIHE, VERFAHREN ZU IHRER HERSTELLUNG SOWIE DIESE ENTHALTENDE ARZNEIMITTEL

Verfahren zur Herstellung von 3-oxygenierten 7alpha, 10alpha-Cyclo-B-Homo-19-nor-steroiden

Improvements in or relating to 1-substituted-5,10-methylene-19-nor-3-keto-and 3-substituted-5,10-seco-5,19-cyclo-í¸-steroids

Novel steroids of the formula (wherein X is CN, C1- 8 alkyl, C2- 8 alkenyl or C2- 8 alkynyl; R is C1- 8 alkyl, C2- 8 alkenyl or C2- 8 alkynyl; R1 is H or acyl; R2 is H, C1- 8 alkyl, C2- 8 alkenyl or C2- 8 alkynyl; R3 is H, OH or O-acyl; R4 is H or a - or b -CH3; and Y is H, keto or b -OH) are prepared from the corresponding 5,10-methylene-19-nor-D 1-steroids, in which 17-side chains are protected by ketal formation, and Grignard reagents, the mixture formed being separated by chromatography. On treatment of the 1a -substituted products with a mineral acid in a lower aliphatic alcohol there are produced the corresponding 1a -substituted-D 4-3-keto-steroids. If a 17-keto-starting material is used in the Grignard process a 17a -substituted-17b -ol is obtained. If an alkali metal cyanide replaces the Grignard reagent in the first-described process the 1a -cyano-5, 10-methylene ...

VITAMIN D3

Pentacyclic Steroid Intermediates and Method of Preparing the same

... 1,151,209. Steroids. WARNER-LAMBERT PHARMACEUTICAL CO. 22 Aug., 1966 [23, Aug.,. 1965], No.37534/66. Heading C2U. The invention comprises compounds having the formulµ wherein R is H or CH 3 , R1 is. H, F or CH 3 , Y is H 2 , H(#-OH), or =O, Z is H or halogen, T is H 2 , H(#-CH 3 ),H(-CH 3 ), (H,#-F), (H,,F), (H,-Cl), (H,#-Cl), or =CH 2 , R3 is H or C 1-9 acyl and the C 17 carbon atom has the structure where E represents one of the groups in which n is 1 or 2 and W is CH 3 or C 2 H 5 ,. or in the first of the above formula the C 17 carbon atom has the structure where X and X1 which can be the same or different, are selected from H, OH or O Acyl containing up to 9 atoms and B is H or a saturated or unsaturated hydrocarbon radical containing up to 3 carbon, atoms, with the proviso that T is H 2 when B is other than H, and a method for the-preparation of compounds of the formula wherein R, R, T, Y, Z, and the C 17 carbon atom are as defined above for the first formula ...

5ª‰, 19-cycloandrostanes

... (wherein R is hydrogen, HZ, HZCO or PhZ, and R1 and R11 are hydroxy, HZCOO or ketonic oxygen; Z being C1- 7 alkylene and Ph being phenyl) are prepared by treating steroids of the formula (wherein R has the above values except hydrogen, and R11 is tolyl, Ph or HZ) with water or an acid HZCOOH and, if desired, reducing the 17-ones so formed to 17b -ols which may then be esterified and/or oxidizing the 6-ols so formed to 6-ones and/or hydrolysing the 3-esters to 3-ols. The 3-benzyloxy compounds may be hydrogenolysed to 3-ols; and 6-ones may be reduced to 6-ols which may be acylated. Esters may be hydrolysed to the free ols. Steroids of the second general formula above are prepared from the 19-ols and sulphonyl chlorides.

Process for producing i-brassicasterol

Disclosed herein is a process for producing i-brassicasterol, comprising charging a mixture of i-sterols derived from a mixture of sterols including brassicasterol into a column packed with a filler obtained by chemically binding alkyl group(s) of 15 to 24 carbon atoms to silica, and subjecting said mixture of i-sterols to reversed-phase partition column-chromatography while using (i) an alcohol of one to three carbon atoms or a mixture therof, or (ii) a mixed solvent comprising more than 50% by volume of said alcohol(s) and a solvent other than said alcohol(s) as an eluent, thereby isolating and purifying i-brassicasterol.

Derivatives of 6ª‡-methyl-17ª‡-hydroxyprogesterone and method of preparing them

The invention comprises steroids of the general formula wherein Y represents hydrogen or an alkoxy group, and X represents hydrogen or the group of the formula wherein n is 0 or 1, and the preparation thereof by reacting the corresponding 3-keto steroid with 1,2-ethanedithiol or 1,3-propane-dithiol to form steroids of the first formula above wherein X is the group of the second formula above and, if desired esterifying the product in the case where Y is hydrogen and, when required, reducing these steroids to form steroids of the first general formula above wherein X represents hydrogen and, if desired esterifying the product as above. A suitable reagent for carrying out the reduction is Raney nickel. Therapeutic compositions having anti-ovulating properties contain as the active ingredients steroids of the first general formula above. The compositions may be in the form of pills, tablets, capsules, syrups or elixirs for oral administration, or in ...

Steroid intermediates in the synthesis of-hydroxyvitamin D2

This invention relates to hydroxylated derivatives of vitamin D2, to processes for preparing such compounds, to intermediates utilized in such processes and to certain isotopically labelled vitamin D2 compounds. The vitamin D2 derivatives would find application in the treatment of or prophylaxsis for various disease states characterized by calcium and phosphorous imbalances and as a substitute for vitamin D3 and its metabolites in their various applications.

6,6-ethylene-19-nortestosterones

... 1,129,382. 6,6-Ethylene-steroids. SMITH KLINE & FRENCH LABORATORIES. 13 Sept., 1966 [17 Sept., 1965], No. 40953/66. Heading C2U. The invention comprises compounds of formula wherein R is hydrogen, cyclopenten-1-yl, cyclohexen-1-yl, 11-ethoxy-cyclopentyl, 11-ethoxycyclohexyl, 21-tetrahydropyranyl or C 2-10 acyl, and R 1 is hydrogen, methyl, ethyl, vinyl, ethynyl, chloroethynyl, bromoethynyl, 1-propynyl or 3,3,3-trifluoro-1-propynyl, and their preparation by reaction of a 17#-acetoxy-6 unsubstituted analogue with trimethyl orthoformate to give the 3-methoxy-3,5-diene, condensing this with #-acetoxyethyl-mercuric acetate to give the 3-methoxy-6-(#-acetoxy)-ethyl-3, 5 diene, hydrolysing to the 3-methoxy-17#- hydroxy.6.(#-hydrozyethyl)-3,5 diene, and cyclizing, followed if desired by (a) total or partial hydrogenation of a 17-ethynyl compound, or (b) 17-etherification or esterification. The compounds of the invention have anabolic and androgenic acitivity and may be used in pharmaceutical ...

YPSILON-LACTONE DERIVATIVES

Steroid esters

The invention comprises steroids of the formula (wherein R is alkyl of 1 to 7 carbon atoms, phenyl or nitrophenyl) and their preparation by esterification of the corresponding 6-ols with a reactive derivative of the appropriate acid in the presence of an excess of pyridine at a temperature between 10 DEG and 100 DEG C. 6a - Hydroxy - 17 - ethylenedioxy - 3a ,5a - cycloandrostane is prepared by reduction of the corresponding 6-one.

VITAMIN D3 DERIVATIVES

Improvements in or relating to 5,10-seco-5,19-cyclo-steroids

Novel compounds of the formulae being tautomeric mixtures of the D 1(10)2,4 5,10-seco - 5,19 - cyclo - steroids and the D 1,3 - 5, 10-methylene - 19 - nor - steroids (wherein R is OR4 or NR5R6 in which R4 is C1- 8 alkyl or cycloalkyl, or acyl, R5 is C1- 8 alkyl, aryl or aralkyl, and R6 is hydrogen, C1- 8 alkyl, C6- 8 aryl or C6- 8 aralkyl, or NR5R6 is a saturated heterocycle; X is H, C1- 8 alkyl, C2- 8 alkenyl or C2- 8 alkynyl; Y is hydroxy or acyloxy, or X and Y together are keto; R2 is H, hydroxy or acyloxy; R3 is H, methyl or a -OH, or R2 and R3 together are 16a ,17a -methylenedioxy which may be substituted by R7 and R8, R7 being C1- 8 alkyl and R8 being C1- 8 alkyl, aryl or aralkyl; R9 is H or acyl; X1 is H or halogen; and Y1 is H or b -OH or keto, with X1 being H when Y1 is H; the acyl groups containing up to 12 carbon atoms and being optionally substituted) and, ...

New 19-Nor-Pregnene derivatives.

The invention relates to compounds of formula (i), in which r1, r2, r3, r4, r5, r6, n and x as defined in the specification, and to pharmaceutical compositions containing them. These compounds are excellent progestogens which are devoid of residua androgenic activity.

New 9-nor pregn ne de ivati es

MEASURING INSTRUMENT FOR THE RECORDING OF THE NUMBER OF IRREGULARITIES AND/OR ERRORS OF A PRODUCT

PROCEDURES FOR the PRODUCTION OF 24,25-DIHYDROXY CHOLESTERINDERIVATEN

PROCEDURE FOR the PRODUCTION OF NEW ONE 4-ANDROSTEN-3-ONEN

18-METHYL-19-NOR-ANDROST-4-EN-17,17-SPIROETHER (18-METHYL-19-NOR-20SPIROX-4-EN-3-ONE), AS WELL AS THESE CONTAINING PHARMACEUTICAL PREPARATIONS

IMPROVED PROCEDURE FOR THE PRODUCTION OF BETULINSÄURE

MEDICINE TO WACHSTUMSINHIBIERUNG OF TUMORS

TRITERPENHALTIGER OLEOGELBILDNER, TRITERPENHALTIGES OLEOGEL AND PROCEDURE FOR THE PRODUCTION OF A TRITERPENHALTIGEN OLEOGELS

MESSEINRICHTUNG ZUR AUFZEICHNUNG DER ZAHL VON UNREGELMAESSIGKEITEN BZW. FEHLERN EINES PRODUKTES

PROCEDURE FOR the PRODUCTION OF NEW ONE 4-ANDROSTEN-3-ONEN

PROCEDURE FOR the PRODUCTION OF NEW ONE 15ALPHA, 16ALPHA-METHYLEN-4-OSTREN-17BETA-OLEN

TURN OUT FOR RECORDING HAUFIGKEIT FROM EVENTS

PROCEDURES FOR the PRODUCTION OF 24,25-DIHYDROXY CHOLESTERINDERIVATEN

PROCEDURE FOR THE PRODUCTION OF CHOLESTENDERIVATEN AND NEW INTERMEDIATE PRODUCTS IN THEIR PRODUCTION.

Procedure for the production of new Steroiden

Procedure for the production of new Steroiden

Procedure for the production of new Steroide

Procedure for the production of new 18-Methyl-9β, 10α-steroiden of the Androstanreihe

Procedure for the production of new 1α, 2α, 6ß, 7ß, - Dimethylensteroide

Procedure for the production of new 18-Methyl-9β, 10α-steroiden of the Androstanreihe

Procedure for the production again 4-Chlor-1,2α-methylen-Δ<4,6>-pregnadien-17α-ol-3,20-dion and its new 17-Estern

PROCEDURE FOR the PRODUCTION OF 3-KETO-7ALPHAALKOXYCARBONYLDELTA4,5-STEROIDEN AS WELL AS INTERMEDIATE PRODUCTS

17-hydroxy-19-nor-21-carboxylic acid-steroid gamma-lactone derivative, use thereof, and medicament containing the derivative

Compounds useful for treating neurodegenerative disorders

2,19-METHYLENEOXY AND 2,19-METHYLENETHIO BRIDGED STEROIDS AS AROMATASE AND 19-HYDROXYLASE INHIBITORS

Antitumor agents

17-OXO-STEROIDS

Linkers

CHOLESTADIENE DERIVATIVES, A PROCESS FOR THE PREPARATION THEREOF, AND THE USE THEREOF AS PHARMACEUTICALS ACTING TO INHIBIT HMG-COA REDUCTASE

NOVEL TRITERPENE DERIVATIVES, PREPARATION THEREOF AND USE THEREOF

14-HYDROXY-3-DESOXYCARDENOLIDES

ISOTOPICALLY LABELED VITAMIN D DERIVATIVES AND PROCESSES FOR PREPARING SAME

This invention relates to isotopically labeled vitamin D compounds, including radiolabeled vitamin D compounds of high specific activity, methods for their preparation, and novel intermediates in their synthesis. The radiolabeled vitamin D compounds are characterized by high specific activity (up to 160 Ci/mmol) with the process providing a facile and convenient method for synthesizing such compounds.

PROCESS FOR PRODUCING 15A, 16A-UMETHYLENE-D*SU4 UOEST REN-17B-UOLS

4-ANDROSTEN-3-ONE AND PROCESS FOR ITS PRODUCTION

ISOTOPICALLY LABELED VITAMIN D DERIVATIVES AND PROCESSES FOR PREPARING SAME

25-ALKYLCHOLESTEROL DERIVATIVES

18-METHYL-19-NOR-ANDROST-4-EN-17,17-SPIROETHER (18-METHYL-19-NOR-20-SPIROX-4-EN-3-ONE) AND PHARMACEUTICAL PREPARATIONS COMPRISING THE SAME

The invention relates to novel 18-methyl-19-nor-androst-4-en-17,17- spiro ether of general formula (I), where Z = O, two H, =NOR or =NNHSO2R, R = H, o r straight or branched chain C1-4 or C3-4alkyl, R4 = H, halogen, or CF3 and R6 and/or R7 are .alpha.- or ß-positioned and R6 and R7 independently = H or straight or branched chain C1-4 or C3-4alkyl or a straight or branched chai n C2-4 or C3-4alkylene or a saturated C3-5 cycloalkyl, or together form a me thylene group or a double bond. The novel compounds have gestagenic and anti mineralcorticoid action.

PREPARATION OF PHARMACEUTICAL SALTS OF 3-O-(3',3'-DIMETHLSUCCINYL) BETULINIC ACID

BETULIN DERIVED COMPOUNDS AS ANTI-FEEDANTS FOR PLANT PESTS

The invention relates to compounds derived from betulin, and to the use t hereof in plant pest control, particularly as antifeedants for butterfly lar vae, beetles and snails. Further, the invention relates to novel betulin der ivatives and methods for the production thereof either directly from betulin , or via intermediates derived therefrom.

EXTENDED TRITERPENE DERIVATIVES

The present invention concerns novel pharmaceutically active triterpene d erivatives, pharmaceutical compositions containing the same, their use as me dicaments, and the use of the compounds for the manufacture of specific medi caments. The present invention also concerns a method of treatment involving administration of the compounds. Specifically, the compounds are derivative s of betulinic acid having substitutions at one or more of the C-3, C2-8 and C-19 positions as further described herein. The novel compounds are useful as antiretroviral agents. In particular, the novel compounds are useful for the treatment of Human Immunodeficiency Virus (HIV).

2,19-METHYLENEOXY AND 2,19-METHYLENETHIO BRIDGED STEROIDS AS AROMATASE AND 19-HYDROXYLASE INHIBITORS

The present invention is directed to a group of compounds which are 2,19-methyleneoxy or 2,19-methylenethio bridged steroids, and related steroidal compounds of the formula OR which are useful as aromatase and 19-hydroxylase inhibitors.

19-NOR STEROIDS PHENOXYALKYLSULFONAMIDE OR PHENOXYALKYLSULFONYLUREA CHAIN ON 11 BETA POSITION, PROCESS AND INTERMEDIATES FOR THEIR PREPARATION, APPLICATION AS MEDICAMENTS AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

L'invention a pour objet les composés de formule (I) : (I) dans laquelle, R17 et R'17 sont tels que soit R17 et R'17 forment ensemble une cétone soit R17 représente un radical hydroxyle, ou un radical acyloxy et R'17 représente un atome d'hydrogène, un radical alkyle, alcényle ou alcynyle, R3 représente un atome d'hydrogène, un radical alkyle ou un radical acyle, R1 et R2 identiques ou différents, représentent un atome d'hydrogène, un radical alkyle, éventuellement substitué, un radical acyle, un radical aryle ou aralkyle, éventuellement substitué, un radical alkyle, aralkyle ou aryle carbamoyle éventuellement substitué, ou forment avec l'atome d'azote auquel ils sont liés un hétérocycle saturé pouvant renfermer un second hétéroatome choisi parmi N, O et S et être substitué, ou forment un radical dialkylaminométhylène, n est égal au plus à 18, et les sels d'addition de ceux-ci, leur préparation, leur application comme médicaments, les compositions les renfermant et les nouveaux intermédiaires ...

PROCESSES FOR PREPARATION OF 9,11-EPOXY STEROIDS AND INTERMEDIATES USEFUL THEREIN

Multiple novel reaction schemes, novel process steps and novel intermediates are provided for the synthesis of epoxymexrenone and other compounds of Formula I (see formula I) wherein: -A-A- represents the group -CHR4-CHR5- or -CR4=CR5- R3, R4 and R5 are independently selected from the group consisting of hydrogen, halo, hydroxy, lower alkyl, lower alkoxy, hydroxyalkyl, alkoxyalkyl, hydroxycarbonyl, cyano, aryloxy; R1 represents an alpha-oriented lower alkoxycarbonyl or hydroxyalkyl radical; -B-B- represents the group -CHR6-CHR7- or an alpha- or beta- oriented group: (see formula III) where R6 and R7 are independently selected from the group consisting of hydrogen, halo, lower alkoxy, acyl, hydroxyalkyl, alkoxyalkyl, hydroxycarbonyl, alkyl, alkoxycarbonyl, acyloxyalkyl, cyano and aryloxy; and R8 and R9 are independently selected from the group consisting of hydrogen, hydroxy, halo, lower alkoxy, acyl, hydroxyalkyl, alkoxyalkyl, hydroxycarbonyl, alkyl, alkoxycarbonyl, acyloxyalkyl, cyano ...

PROCESSES FOR PREPARATION OF 9,11-EPOXY STEROIDS AND INTERMEDIATES USEFUL THEREIN

Multiple novel reaction schemes, novel process steps and novel intermediates are provided for the synthesis of epoxymexrenone and other compounds of formula (I) wherein: -A-A- represents the group -CHR4-CHR5- or -CR4=CR5-, R3, R4 and R5 are independently selected from the group consisting of hydrogen, halo, hydroxy, lower alkyl, lower alkoxy, hydroxyalkyl, alkoxyalkyl, hydroxycarbonyl, cyano, aryloxy; R1 represents an alpha-oriented lower alkoxycarbonyl or hydroxyalkyl radical; -B-B- represents the group -CHR6-CHR7-or an alpha- or beta-oriented group (III), where R6 and R7 are independently selected from the group consisting of hydrogen, halo, lower alkoxy, acyl, hydroxyalkyl, alkoxyalkyl, hydroxycarbonyl, alkyl, alkoxycarbonyl, acyloxyalkyl, cyano and aryloxy; and R8 and R9 are independently selected from the group consisting of hydrogen, hydroxy, halo, lower alkoxy, acyl, hydroxyalkyl, alkoxyalkyl, hydroxycarbonyl, alkyl, alkoxycarbonyl, acyloxyalkyl, cyano and aryloxy, or R8 and R9 together ...

Verfahren zur Herstellung neuer Steroide der Pregnanreihe

Verfahren zur Herstellung neuer Steroide der Pregnanreihe

Verfahren zur Herstellung neuer Steroide der Pregnanreihe

Verfahren zur Herstellung neuer Steroide der Pregnanreihe

Ovulation inhibiting pregnenes

Ovulation inhibiting pregnenes Cpds. are 4-chloro-17-hydroxy or acyloxy-1 alpha, 2 alpha:6 alpha, 7 alpha-dimethylene-4-pregnene-3,20 -diones.

Verfahren zur Herstellung eines 22-Aryl-bisnor-5,7,9-cholatrien-22-on-Additionsproduktes.

Verfahren zur Herstellung von 3-Keto-1,4,17(20)-pregnatrien-21-carbonsäuren oder deren Estern

Verfahren zur Herstellung eines Additionsproduktes eines 3-Acyloxy-5,7,9-pregnatrien-20-ons.

Verfahren zur Herstellung eines 22-Acyloxy-bisnor-5,7,9,20-cholatetraen-Additionsproduktes.

Verfahren zur Herstellung eines Additionsproduktes von Bisnor-5,7,9-cholatrien-22-al-3-on.

Verfahren zur Herstellung eines Maleinsäure-Additionsproduktes.

Verfahren zur Herstellung neuer Steroidverbindungen

Verfahren zur Herstellung neuer Cyclosteroide

Verfahren zur Herstellung von 16,17-Methylen-20-ketosteroiden

Verfahren zur Herstellung von 16,17-Methylen-20-ketosteroiden

Verfahren zur Herstellung von 1,2-Methylen- 4,6-3-ketosteroiden

Procédé de préparation de nouveaux stéroïdes

Verfahren zur Herstellung neuer Pregnenderivate

Procédé de préparation de 6-aminostéroïdes

Verfahren zur Herstellung neuer 1,2a-Methylen- 6-17a-hydroxy-progesterone

Verfahren zur Herstellung von 17B-oxy-17a-alkinyl-Steroiden

Procédé de préparation de nouveaux dérivés des stéroïdes

Procédé de préparation de nouveaux dérivés des stéroïdes

Verfahren zur Herstellung neuer Cyclosteroide

Verfahren zur Herstellung von 11a-Hydroxy-11,19-cyclo-steroiden

Verfahren zur Herstellung neuer B-Homo-steroiden

Procédé de préparation des esters de 6-hydroxy-17-éthylène-dioxy-3a,5a-cycloandrostane

Verfahren zur Herstellung neuer 1,2B-Methylensteroide

Process for the preparation of drospirenone

A process is described for the preparation of drospirenone, a synthetic steroid with progestogenic, antimineralocorticoid and antiandrogenic activity, useful for preparing pharmaceutical compositions with contraceptive action; comprising the oxidation of 17α-(3-hydroxypropyl)-6β,7β,15β,16β-dimethylene-5β-androstane-3β,5,17β-triol.

Preparation method of drospirenone

The present invention discloses the preparation method of drospirenone. 3β,5-dyhydroxy-6β,7β,15β,16β-dimethylene-5β-androstane-17,20-epoxy is taken as the raw material. It is subject to oxidization of the hydroxyl at the 3 rd position, ketalization of 3-ketone group, condensation reaction and deesterification to obtain carboxylic acid lactone, sulfonation of the hydroxyl at the 5 th position, and deketalization and desulphonation in the reaction system of glacial acetic acid and sodium acetate to produce the 3-keto-4-alkenyl compound, thus obtaining drospirenone. The preparation method of the invention has high intensification, reaction specificity, less by-products and high yield of products in each step, thus overcoming the disadvantages of low yield and unstable quality.

Derivatives of 3-O-(3',3'-dimethylsuccinyl)-betulinic acid

The present invention relates to compounds of the following formula (I): 2. The compound according to claim 1 , characterized in that R represents a (C-C)alkyl group substituted with one or more claim 1 , preferably one or two claim 1 , groups chosen from COOH and NHR.3. The compound according to or claim 1 , characterized in that R represents a group —(CHR)—(CHR)—X claim 1 , in which:n represents 0 or 1,{'sup': '1', 'X represent a group COOH or NHR, and'}{'sup': 2', '3', '1, 'sub': 1', '8', '1', '4, 'Rand Rrepresent, independently of each other, a hydrogen atom or a (C-C)alkyl group, preferably a (C-C)alkyl group, optionally substituted with a group COOH or NHR,'}{'sup': 2', '3, 'preferably at least Ror Rrepresenting a hydrogen atom.'}4. The compound according to any of to claim 1 , characterized in that Rrepresents a hydrogen atom or a —C(O)O-Alk group claim 1 , in particular a hydrogen atom or a tert-butyloxycarbonyl group.6. A compound according to any of to as a medicine.7. A compound according to any of to for use in the treatment of an infection with a retrovirus such as HIV claim 1 , and in particular HIV-1.8. A pharmaceutical composition comprising at least one compound according to any of to and at least one pharmaceutically acceptable vehicle. The present invention relates to derivatives of 3-O-(3′,3′-dimethylsuccinyl)-betulinic acid, a method for preparing them and their use in the treatment of an infection with a retrovirus such as HIV.Most of the anti-HIV-1 drug inhibitors target the enzymatic activities catalyzed by the reverse transcriptase (RT), the integrase (IN) or the protease (PR) and have caused the emergence of multidrug-resistant HIV-1 strains. Thus, the scientific community has been involved in the discovery of new targets to fight AIDS and in the development of new molecules directed against these targets. The assembly of the HIV-1 Gag precursor (Pr55Gag) and the maturation steps of the virus replication represent attractive targets for the ...

VEGF Production Promoter

Provided are a VEGF production promoter, a hair quality improver, and an external preparation for skin, each of which has a VEGF production promoting activity and can be used as a pharmaceutical agent, a cosmetic, a food, or a material therefor. The VEGF production promoter, the hair quality improver, and the external preparation for skin each comprises, as an active ingredient, a cycloartane-type glycoside represented by the following general formula (1) (where R represents a xylose residue or an arabinose residue, and the ring D moiety represents any one of the following moieties a to f (where R 1 represents a hydrogen atom or a methyl group, R 2 represents a hydrogen atom or an acetyl group, R 3 represents a hydrogen atom or a hydroxyl, group, R 4 represents a hydrogen atom or a hydroxyl group, and Ac represents an acetyl group)).

Process for Production of Triterpene Alcohol

A process for producing triterpene alcohol, comprising sequentially conducting the following steps (A) to (C): 1. A process for producing triterpene alcohol , comprising sequentially conducting the following steps (A) to (C):(A) subjecting γ-oryzanol to alkaline hydrolysis;(B) mixing the alkaline hydrolysate with a low polarity organic solvent, and extracting triterpene alcohol to obtain a triterpene alcohol-containing low polarity organic solvent; and(C) adding water to the triterpene alcohol-containing low polarity organic solvent thus obtained, removing the low polarity organic solvent, and then melting triterpene alcohol in hot water, followed by cooling.2. The process for producing triterpene alcohol according to claim 1 , wherein the low polarity organic solvent is hexane.3. The process for producing triterpene alcohol according to claim 1 , wherein the amount of water added to the triterpene alcohol-containing low polarity organic solvent is 5 to 100 times by weight of the initial amount of γ-oryzanol.4. The process for producing triterpene alcohol according to claim 1 , wherein the amount of water added to the triterpene alcohol-containing low polarity organic solvent is 5 to 20 times by weight of the initial amount of γ-oryzanol.5. The process for producing triterpene alcohol according to claim 1 , wherein the amount of water added to the triterpene alcohol-containing low polarity organic solvent is 8 to 15 times by weight of the initial amount of γ-oryzanol.6. The process for producing triterpene alcohol according to claim 1 , wherein the temperature of the hot water for melting triterpene alcohol is from 85 to 100° C.7. The process for producing triterpene alcohol according to claim 1 , wherein the temperature of the hot water for melting triterpene alcohol is from 90 to 100° C.8. The process for producing triterpene alcohol according to claim 1 , comprising conducting adsorption treatment for exposing the triterpene alcohol-containing low polarity ...

Substituted 16,17-annellated steroid compounds for use in womens health

The present invention relates to substituted steroid compounds having the formula Wherein R 1 is H or halogen; R 2 is H, (1C-4C)alkyl, (1C-4C)acyl, glucuronyl or sulfamoyl; R 3 is H or halogen; R 4 is H, (1C-4C)alkyl, (2C-4C)alkenyl or (2C-4C)alkynyl; R 5 is methyl or ethyl; R 6 is H or methyl; R 7 is H or methyl; R 8 is H or acyl for use in the treatment and prevention of endometriosis, for contraception, for hormonal therapy in perimenopausal and post-menopausal women, for the treatment of osteoporosis and for the treatment uterine fibroids and other menstrual-related disorders, such as dysfunctional uterine bleeding.

METHODS FOR INHIBITING MUSCLE ATROPHY

In one aspect, the invention relates methods for inhibiting or preventing muscle atrophy or increasing muscle mass by providing to a subject in need thereof an effective amount of ursolic acid, a derivative thereof, or an analog of the ursane scaffold. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention. 2. The method of claim 1 , wherein the mammal has been diagnosed with a need for treatment of muscle atrophy prior to the administering step.3. The method of claim 1 , wherein the compound is not ursolic acid claim 1 , boswellic acid claim 1 , corosolic acid claim 1 , betulinic acid claim 1 , or UA0713.4. The method of claim 1 , wherein the compound is ursolic acid claim 1 , boswellic acid claim 1 , corosolic acid claim 1 , betulinic acid claim 1 , or UA0713.5. The method of claim 1 , wherein the compound is ursolic acid.6. The method of claim 1 , wherein the compound is not administered as a foodstuff.7. The method of claim 1 , wherein administration increases muscle mass and/or muscular strength in the animal.17. The method of claim 16 , wherein AA is a phenylalanine residue claim 16 ,19. A pharmaceutical composition comprising at least one compound as defined in .20. A pharmaceutical composition comprising at least one compound as defined in . This application claims the benefit of U.S. Applications No. 61/346,813, filed on May 20, 2010, and No. 61/445,488, filed on Feb. 22, 2011, which are hereby incorporated by reference in entirety.This invention was made with government support under grant VA Career Development Award-2 to Christopher M. Adams, and support from a VA Research Enhancement Award Program to Steven D. Kunkel. The United States government has certain rights in the invention.Skeletal muscle atrophy is characteristic of starvation and a common effect of aging. It is also a nearly universal consequence of severe human illnesses, including cancer, ...

C-3 CYCLOALKENYL TRITERPENOIDS WITH HIV MATURATION INHIBITORY ACTIVITY

Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, C-3 cycloalkenyl triterpenoids that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formulas I, II, III and IV: 2. The compound as claimed in claim 1 , wherein said compound has the Formula I.3. The compound as claimed in claim 1 , wherein said compound has the Formula II.4. The compound as claimed in claim 1 , wherein said compound has the Formula III.5. The compound as claimed in claim 2 , wherein Ris isopropenyl.6. The compound as claimed in claim 5 , wherein X is selected from the group of Ccycloalkenyl claim 5 , Cspirocycloalkyl claim 5 , and Cspirocycloalkenyl.7. The compound as claimed in claim 6 , wherein Y is —COOR.8. The compound as claimed in claim 7 , wherein Y is —COOH.9. The compound as claimed in claim 6 , wherein A is —H.12. A pharmaceutical composition which comprises an antiviral effective amount of one or more of the compounds as claimed in claim 1 , together with one or more pharmaceutically acceptable carriers claim 1 , excipients or diluents.13. A pharmaceutical composition which comprises an antiviral effective amount of one or more of the compounds as claimed in claim 10 , together with one or more pharmaceutically acceptable carriers claim 10 , excipients or diluents.14. pharmaceutical composition which comprises an antiviral effective amount of one or more of the compounds as claimed in claim 11 , together with one or more pharmaceutically acceptable carriers claim 11 , excipients or diluents.15. The pharmaceutical composition of claim 12 , useful for treating infection by HIV claim 12 , which additionally comprises an antiviral effective amount of an AIDS treatment agent selected from the group consisting of: (a) an AIDS antiviral agent; (b) an anti-infective agent; (c) an immunomodulator; and (d) another HIV entry inhibitor.16. A method for ...

(11beta, 17alpha)-11-(4-(2-11C-ACETYL)PHENYL)-17,23-EPOXY-19,24-DINORCHOLA-4,9,20-TRIEN-3-ONE

The present invention relates to (11β,17α)-11-(4-(2-C-acetyl)phenyl)-17,23-epoxy-19,24-dinorchola-4,9,20-trien-3-one, an C-labelled ORG 33628; a process for the preparation thereof, intermediates used in this process and the use of this compound as a PET tracer for the detection of breast cancer. 1. (canceled)48-. (canceled)9. The process according to wherein the acid treatment is combined with the previous reaction step.10. The process according to wherein in step b the base is a Grignard reagent.11. The process according to wherein the Grignard reagent is isopropylmagnesium bromide.12. The process according to wherein the [C]methyllithium is prepared by reacting [C]methyl halide with (C3-6)alkyl-lithium.13. A method of diagnosing or monitoring breast cancer or a breast cancer state in mammals comprising the steps of:a. administering an effective amount of the compound according to Formula 1 to a subject;b. imaging said mammal, performing a PET scan on the subject to generate PET scan images and diagnosing or monitoring said breast cancer or breast cancer state.1415-. (canceled) The present invention relates to (11β,17α)-11-(4-(2-C-acetyl)phenyl)-17,23-epoxy-19,24-dinorchola-4,9,20-trien-3-one, an C-labelled ORG 33628; a process for the preparation thereof, intermediates used in this process and the use of this compound as a PET tracer for the detection of breast cancer.Breast cancer is a common cause of death among women and, although less common, also in men. Breast cancer is a well known example of a hormone dependent cancer in which steroid hormone receptors play a key role in tumor proliferation and disease progression. Steroid hormone receptors, more specifically estrogen receptors and progesterone receptors, are often expressed in breast tumor tissue.ORG 33628 is a highly selective progesterone receptor modulator (PRM) with a predominant anti-progestagenic profile. Two main indications for the use of PRMs are the treatment of breast cancer and fertility ...

Triterpene-containing oleogel-forming agent, triterpene-containing oleogel and method for producing a triterpene-containing oleogel

The invention relates to an oleogel-forming agent which comprises at least one highly dispersed triterpene. The invention also relates to an oleogel which comprises a nonpolar liquid in an amount ranging from 80% by weight to 99% by weight based on the total weight of the oleogel and an oleogel-forming agent comprising a highly dispersed triterpene in an amount ranging from 1% by weight to 20% by weight based on the total weight of the oleogel. The invention also relates to a method for producing an oleogel.

Process for the Preparation of Drospirenone

A process is described wherein, by employing 17α-(3-hydroxypropyl) -63,7β3;15β,16β-dimethylene-5β-androstane-3β,5,17β-triol (II) as starting product, in a single stage reaction there is obtained drospirenone, (I), whereby the reaction is achieved using gaseous oxygen as the stoichiometric oxidant in the presence of a catalytic system containing (i) TEMPO or a derivative thereof (ii) a ferric salt (Fe3+) and (iii) NaCl. The product drospirenone is a known synthetic steroid with progestogenic, antimineralocorticoid and antiandrogenic action, that is useful for preparing pharmaceutical compositions with contraceptive action. 2. The process according to claim 1 , wherein the oxygen is employed in the form of pure oxygen claim 1 , air or mixtures of inert gas and oxygen.3. The process according to claim 1 , wherein the derivative of 2 claim 1 ,2 claim 1 ,6 claim 1 ,6-tetramethylpiperidine-1-oxyl radical is selected from the group consisting of 4-hydroxy-2 claim 1 ,2 claim 1 ,6 claim 1 ,6-tetramethylpiperidine-1-oxyl radical claim 1 , 4-methoxy-2 claim 1 ,2 claim 1 ,6 claim 1 ,6-tetramethylpiperidine-1-oxyl radical claim 1 , 4-(benzoyloxy)-2 claim 1 ,2 claim 1 ,6 claim 1 ,6-tetramethylpiperidine-1-oxyl radical claim 1 , 4-acetamido-2 claim 1 ,2 claim 1 ,6 claim 1 ,6-tetramethylpiperidine-1-oxyl radical and 4-amino-2 claim 1 ,2 claim 1 ,6 claim 1 ,6-tetramethylpiperidine-1-oxyl radical.4. The process according to claim 1 , wherein said acid is selected from the group consisting of acetic acid claim 1 , anhydrous or hydrated oxalic acid claim 1 , citric acid claim 1 , anhydrous or hydrated para toluene sulphonic acid claim 1 , formic acid claim 1 , sulphuric acid claim 1 , perchloric acid claim 1 , hydrochloric acid claim 1 , phosphoric acid claim 1 , nitric acid claim 1 , hydrobromic acid claim 1 , fumaric acid claim 1 , maleic acid claim 1 , xinafoic acid claim 1 , benzoic acid and substitution derivatives thereof on the aromatic ring claim 1 , or alkali metal and ...

ANXIOLYTIC MARCGRAVIACEAE COMPOSITIONS CONTAINING BETULINIC ACID, BETULINIC ACID DERIVATIVES, AND METHODS

Pharmaceutical compositions for preventing or treating anxiety, comprising betulinic acid or derivatives thereof are provided. Methods for preventing or treating anxiety with betulinic acid or derivatives thereof are also provided. The invention further provides betulinic-acid containing preparations of plants of the family Marcgraviaceae having anxiolytic activity and methods for making such extracts and using them to prevent or treat anxiety in a subject. 1. A betulinic acid-containing composition obtained from of a plant of the family Marcgraviaceae.2. The composition of claim 1 , wherein the composition is an extract of Marcgraviaceae claim 1 , prepared by a method comprising:(a) contacting a Marcgraviaceae plant, or part thereof, with a first solvent in which betulinic acid is soluble, to form a betulinic acid-containing extract; and(b) recovering the betulinic acid-containing extract from the first solvent, thereby preparing a betulinic acid-containing composition.3. The composition of claim 2 , wherein (b) further comprises:(a) filtering the betulinic acid-containing extract from (a); and(b) evaporating the first solvent.4. The composition of claim 2 , wherein (b) further comprises:(a) filtering the betulinic acid-containing extract from (a),(b) evaporating the solvent,(c) extracting by stirring with a second solvent; and(d) evaporating the second solvent.5. The composition of claim 1 , comprising at least about 0.1% to 90% by weight betulinic acid.6. The composition of claim 1 , comprising at least about 0.5% by weight betulinic acid.7. The composition of claim 1 , comprising at least about 1% by weight betulinic acid.8. The composition of claim 1 , comprising at least about 5% by weight betulinic acid.9Marcgraviastrum, Norantea, Ruyschia, Sarcopera, Marcgravia, Pseudosarcopera, SouroubeaSchwartzia.. The composition of claim 1 , wherein the plant is of a genus selected from the group consisting of claim 1 , or10Souroubea. The composition of claim 1 , wherein ...

Process for the preparation of 17-(3-hydroxypropyl)-17-hydroxysteroids

The present invention relates to a process for the preparation of 17α-(3-hydroxypropyl)-17β-hydroxysteroids of the formula I starting from 17-ketosteroids of the formula III via the intermediates of the formula V wherein the radicals R 3 , R 5 , R 6 , R 7 , R 10 , R 13 , R 15 , R 16 , R 40 , R 41 and R 42 have the meaning indicated in the description.

STEROID DERIVATIVE REGULATORS, METHOD FOR PREPARING THE SAME, AND USES THEREOF

Steroid derivative regulators, a method for preparing the same, and uses thereof are described. Specifically, a compound as shown in formula (I), a preparation method therefor, a pharmaceutical composition containing the compound, and uses thereof as a regulator of GABA A receptor for treating depression, convulsion, Parkinson's disease, and nervous system diseases are described, wherein the substituents of the formula (I) are as defined in the description. 16. The compound of formula (I) claim 5 , the stereoisomer thereof claim 5 , or the pharmaceutically acceptable salt thereof according to claim 5 , wherein Rselected from the group consisting of hydrogen atom claim 5 , cyano claim 5 , halogen claim 5 , nitro claim 5 , Calkyl claim 5 , Calkynyl claim 5 , Calkoxy claim 5 , Chaloalkyl claim 5 , Ccycloalkyl claim 5 , Chydroxyalkyl claim 5 , 5 to 10 membered heterocyclyl claim 5 , 5 to 10 membered heteroaryl claim 5 , —(CH) claim 5 ,10R claim 5 , —(CH)SR claim 5 , —(CH)C(O)R claim 5 , —(CH)C(O)NRR claim 5 , —(CH)C(O)ORand —(CH)S(O)R claim 5 , wherein the Calkyl claim 5 , Calkoxy claim 5 , Chaloalkyl claim 5 , Ccycloalkyl claim 5 , Chydroxyalkyl claim 5 , wherein the 5 to 10 membered heterocyclyl and 5 to 10 membered heteroaryl are each optionally substituted by one or more substituents selected from the group consisting of hydrogen atom claim 5 , Calkyl claim 5 , halogen claim 5 , cyano claim 5 , hydroxy claim 5 , Ccycloalkyl claim 5 , Chydroxyalkyl claim 5 , 5 to 10 membered heterocyclyl and 5 to 10 membered heteroaryl;{'sub': 23', '24', '1-6, 'Rand Rare each independently selected from the group consisting of hydrogen atom, Calkyl and 3 to 8 membered heterocyclyl.'}17. The compound of formula (I) claim 5 , the stereoisomer thereof claim 5 , or the pharmaceutically acceptable salt thereof according to claim 5 ,wherein:{'sub': 2', '2', '2', '2', '2, 'Z is selected from the group consisting of —CH—, —CHNH—, —CHO—, —CH—, —NH— and —NHSO—;'}{'sub': 3a', '1-6', '1-6', '1-6 ...

Methods and compounds for modulating the secretion or expression of adhesion proteins or angiopoietins of cells

This invention provides methods, processes, compounds and compositions for modulating the gene expression or secretion of adhesion proteins, angiopoietins or their receptors to cure diseases, for anti-angiogenesis and for treating parasites, wherein the adhesion proteins or receptors comprise fibronectin, integrins family, myosin, vitronectin, collagen, laminin, glycosylation cell surface proteins, polyglycans, cadherin, heparin, tenascin, CD 54, CAM, elastin and FAK; wherein the angiopoietins comprise angiopoietin 1, angiopoietin 2, angiopoietin 3, angiopoietin 4, angiopoietin 5, angiopoietin 6, angiopoietin 7, angiopoietin-like 1, angiopoietin-like 2, angiopoietin-like 3, angiopoietin-like 4, angiopoietin-like 5, angiopoietin-like 6, and angiopoietin-like 7; wherein the cancers comprise breast cancer, leukocyte cancer, liver cancer, ovarian cancer, bladder cancer, prostate cancer, skin cancer, bone cancer, brain cancer, leukemia cancer, lung cancer, colon cancer, CNS cancer, melanoma cancer, renal cancer, cervical cancer, esophageal cancer, testicular cancer, spleenic cancer, kidney cancer, lymphatic cancer, pancreas cancer, stomach cancer and thyroid cancer.

C-3 AND C-17 MODIFIED TRITERPENOIDS AS HIV-1 INHIBITORS

Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, betulinic acid derivatives that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formula I: 3. The compound of claim 2 , wherein Ris isopropenyl.4. The compound of claim 3 , wherein Y is —COOR.5. The compound of claim 4 , wherein Ris H.6. The compound of claim 1 , wherein Ris —Calkyl-Q.7. The compound of claim 6 , wherein Qis —NRR.9. The compound of claim 8 , wherein Rand Rare each selected from the group of —H and —Calkyl.10. The compound of claim 1 , wherein Qis —CN.14. A composition which comprises an HIV ameliorating amount of one or more compounds as claimed in claim 1 , together with one or more pharmaceutically acceptable carriers claim 1 , excipients claim 1 , and/or diluents.15. A composition which comprises an HIV ameliorating amount of one or more compounds as claimed in claim 11 , together with one or more pharmaceutically acceptable carriers claim 11 , excipients claim 11 , and/or diluents.16. A composition which comprises an HIV ameliorating amount of one or more compounds as claimed in claim 12 , together with one or more pharmaceutically acceptable carriers claim 12 , excipients claim 12 , and/or diluents.17. A composition which comprises an HIV ameliorating amount of one or more compounds as claimed in claim 13 , together with one or more pharmaceutically acceptable carriers claim 13 , excipients claim 13 , and/or diluents.18. A method for treating a mammal infected with the HIV virus comprising administering to said mammal an HIV ameliorating amount of a compound as claimed in claim 1 , together with one or more pharmaceutically acceptable carriers claim 1 , excipients claim 1 , and/or diluents.19. A method for treating a mammal infected with the HIV virus comprising administering to said mammal an HIV ameliorating amount of a compound as claimed in claim 12 ...

PROCESS FOR THE PREPARATION OF DROSPIRENONE

A process is disclosed wherein, using either 17a-(3-hydroxypropyl)-6p,7p;15p,16p-dimethylene-5p-androstane-3p,5,17p-triol (II) or 3β,5̂iÎκ̂-6β,7β;15β,16β-dimethylene-5β,17α-pregnane-21,17-carbolactone (III) as starting material, through a single-step reaction it is obtained drospirenone (I), a synthetic steroid with progestogenic, antimineralocorticoid and antiandrogenic activity, useful for preparing pharmaceutical compositions with contraceptive action. 2. The process according to claim 1 , wherein oxygen is used in form of pure oxygen claim 1 , air claim 1 , or mixtures of an inert gas and oxygen at a pressure between 1 and 10 bar.3. The process according to claim 1 , wherein said palladium compound is selected from acetate (Pd(CHO)) claim 1 , acetylacetonate (Pd(CHO)) claim 1 , trifluoroacetate (Pd(COF)) claim 1 , hexafluoroacetylacetonate (Pd(CHOF)) claim 1 , propionate (Pd(CHO)) claim 1 , chloride (PdCl) claim 1 , bromide (PdBr) claim 1 , iodide (PdI) claim 1 , cyanide (Pd(CN)) claim 1 , nitrate (Pd(NO)) claim 1 , sulfide (PdS) claim 1 , oxide (PdO) and hydroxide (Pd(OH)).4. The process according to claim 1 , wherein said palladium compound is used in amounts by weight ranging from 1% to 100% with respect to compound (II) or compound (III).5. The process according to claim 1 , wherein said organic base is selected from pyridine and its alkyl derivatives claim 1 , triethylamine claim 1 , aniline claim 1 , pyrrolidine claim 1 , DBU (1 claim 1 ,8-Diazabicyclo[5.4.0]undec-7-ene) claim 1 , DBN (1 claim 1 ,5-Diazabicyclo[4.3.0]non-5-ene) claim 1 , and cyclic compounds containing two or more nitrogen atoms claim 1 , both aromatic and non-aromatic.6. The process according to claim 1 , wherein said organic base is used in amount by weight equal to or greater than 0.5 times the amount of palladium compound used.7. The process according to claim 6 , wherein the amount by weight of organic base is between 0.5 and 25 times as much as the amount of palladium compound used. ...

EPOXY-(METH)ACRYLATE MONOMERS AND POLYMERS AND METHODS OF MAKING AND USING THE SAME

The present invention relates to the unexpected discovery of novel monomer compounds capable of crosslinking interpenetrating polymer networks (IPNs). In certain embodiments, the monomer compounds of the invention each comprise at least one methacrylate functionality capable of forming polymeric bonds with other methacrylate and vinyl functionalities, and at least one epoxide functionality capable of forming polymeric bonds with epoxide functionalities, amine functionalities, and/or reactive oxygen species. 2. The compound of claim 1 , wherein m is 1 and n is 1.3. A composition comprising at least one monomer of .4. The composition of claim 3 , further comprising at least one polymerization initiator.5. The composition of claim 4 , wherein the polymerization initiator is at least one selected from the group consisting of photoinitiators claim 4 , thermal initiators claim 4 , and redox initiators claim 4 , with and/or without an accelerator.6. The composition of claim 3 , further comprising at least one additional compound comprising at least one selected from the group consisting of an epoxide functionality claim 3 , a methacrylate functionality claim 3 , a vinyl functionality claim 3 , an acrylate functionality claim 3 , an allylic functionality claim 3 , a cyclic carbonate functionality claim 3 , a thiol functionality claim 3 , an amine functionality claim 3 , an aniline functionality claim 3 , an anhydride functionality claim 3 , a carboxylic acid functionality claim 3 , and an unsaturated polyester.7. The composition of claim 6 , wherein the at least one additional compound is selected from the group consisting of bisphenol A diglycidyl ether claim 6 , bisphenol F diglycidyl ether claim 6 , bisguaiacol diglycidyl ether claim 6 , novolac epoxies claim 6 , glycidyl ethers of hydrogenated bisphenols and epoxides claim 6 , di(cyclohexane epoxidemethyl)ether claim 6 , epoxy cyclohexyl methyl-epoxy cyclohexane carboxylate claim 6 , 4 claim 6 ,4′- ...

NOVEL BETULINIC ACID DERIVATIVES AS HIV INHIBITORS

The invention relates to novel betulinic acid derivatives and related compounds, and pharmaceutical compositions useful for therapeutic treatment of viral diseases and particularly HIV mediated diseases. 3. A compound selected from the group consisting of:(1R,3aS,5aR,5bR,7aR,9S,11aR,11bR,13aR,13bR)-9-((1S,3R)-3-(carboxymethyl)-2,2-dimethylcyclopropanecarbonyloxy)-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysene-3a-carboxylic acid,2-((1R,3S)-2,2-dimethyl-3-(((1R,3aS,5aR,5bR,7aR,9S,11aR,11bR,13aR,13bR)-5a,5b,8,8,11a-pentamethyl-3a-(piperidine-1-carbonyl)-1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yloxy)carbonyl)cyclopropyl)acetic acid,2,2-dimethyl-4-oxo-4-((1R,3aS,5aR,5bR,7aR,9S,11aR,11bR,13aR,13bR)-5a,5b,8,8,11a-pentamethyl-1-(1-methylcyclopropyl)-3a-(piperidine-1-carbonyl)icosahydro-1H cyclopenta[a]chrysen-9-yloxy)butanoic acid,4-((1R,3aS,5aR,5bR,7aR,9S,11aR,11bR,13aR,13bR)-3a-(2,2-dimethyl-3-(piperidine-1-carbonyl)cyclobutylcarbamoyl)-5a,5b,8,8,11a-pentamethyl-1-(1-methylcycloprop yl)icosahydro-1H-cyclopenta[a]chrysen-9-yloxy)-2,2-dimethyl-4-oxobutanoicacid,2-((1R,3S)-2,2-dimethyl-3-(((1R,3aS,5aR,5bR,7aR,9S,11aR,11bR,13aR,13bR)-5a,5b,8,8,11a-pentamethyl-3a-(5-phenyl-1,3,4-oxadiazol-2-yl)-1-(prop-1-en-2-yl)icosa hydro-1H-cyclopenta[a]chrysen-9-yloxy)carbonyl)cyclopropyl)acetic acid,2-((1R,3S)-2,2-dimethyl-3-(((1R,3aS,5aR,5bR,7aR,9S,11aR,11bR,13aR,13bR)-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-yl)-3a-(5-(pyridin-3-yl)-1,3,4-oxadiazol-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yloxy)carbonyl)cyclopropyl)aceticacid,4-((1R,3aS,5aR,5bR,7aR,9S,11aR,11bR,13aR,13bR)-3a-(4-(1-methylethyl-2,2,2,1′,1′,1′-D6)piperazine-1-carbonyl)-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yloxy)-2,2-dimethyl-4-oxobutanoic acid,4-((1R,3aS,5aR,5bR,7aR,9S,11aR,11bR,13aR,13bR)-3a-((1R,3S)-3-(4-(1-methylethyl-2,2,2,1′,1′,1′-D6)piperazine-1-carbonyl)-2,2-dimethylcyclobutylcarbamoyl)-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en ...

DERIVATIVES OF BETULIN

The present invention relates to compounds characterized by having a structure according to the following formula I: 2. The compound of claim 1 , wherein Land Lare both [C(RR′)].3. The compound of claim 1 , wherein Land Lare both —CH—.4. The compound of claim 1 , wherein each instance of q is independently 1 claim 1 , 2 claim 1 , or 3.5. The compound of claim 1 , wherein q is 1.6. The compound of claim 1 , wherein W is O.7. The compound of claim 1 , wherein W is a bond.8. The compound of claim 1 , wherein when W is a bond claim 1 , then Ris —H.9. The compound of claim 1 , wherein when W is O claim 1 , then Ris —H.10. The compound of claim 1 , wherein Qin the A group is absent and in the A group is —CH— and the Q in the Formula I structure is —C(═O)—.11. The compound of claim 1 , wherein Ris —H.12. The compound of claim 1 , wherein Ris —(CH)NRR.13. The compound of claim 1 , wherein Ris (dimethylamino)ethyl.14. The compound of claim 1 , wherein each instance of r is independently 0 claim 1 , 1 claim 1 , 2 claim 1 , or 3.15. The compound of claim 1 , wherein r is 2.17. The compound of claim 1 , wherein X is a monocyclic (C-C)aryl.18. The compound of claim 1 , wherein X is phenyl.19. The compound of claim 1 , wherein Ris —H.20. The compound of claim 1 , wherein each instance of m is independently 0 or 1.21. The compound of claim 1 , wherein m is 0.22. The compound of claim 1 , wherein m is 1.23. The compound of claim 1 , wherein n is 1.24. The compound of claim 1 , wherein Rand R′ are both —H.25. The compound of claim 1 , wherein Rand Rare both (C-C)alkyl.26. The compound of claim 1 , wherein Ris methyl.27. The compound of claim 1 , wherein Ris methyl.28. The compound of claim 1 , wherein Rand Rare both methyl.29. The compound of claim 1 , wherein Ris halo.30. The compound of claim 1 , wherein Ris selected from chloro claim 1 , bromo claim 1 , or fluoro.31. The compound of claim 1 , wherein Ris chloro.32. The compound of claim 1 , wherein Ris absent.33. The compound of ...

METHODS FOR INHIBITING MUSCLE ATROPHY

In one aspect, the invention relates methods for inhibiting or preventing muscle atrophy or increasing muscle mass by providing to a subject in need thereof an effective amount of ursolic acid, a derivative thereof, or an analog of the ursane scaffold. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention. 2. The method of claim 1 , wherein the ursolic acid or pharmaceutically acceptable salt claim 1 , hydrate claim 1 , or solvate thereof is administered to the animal in an amount of greater than or equal to 100 mg per day.3. The method of claim 1 , wherein the animal is a mammal.4. The method of claim 1 , wherein the animal is a human.5. The method of claim 1 , wherein the animal is selected from the group consisting of a dog claim 1 , cat claim 1 , pig claim 1 , cow claim 1 , horse claim 1 , goat claim 1 , bison claim 1 , sheep claim 1 , chicken claim 1 , turkey claim 1 , duck claim 1 , goose claim 1 , and domesticated fish.6. The method of claim 1 , wherein the ursolic acid is present as a pharmaceutically acceptable salt selected from salts derived from aluminum claim 1 , ammonium claim 1 , calcium claim 1 , copper (-ic and -ous) claim 1 , ferric claim 1 , ferrous claim 1 , lithium claim 1 , magnesium claim 1 , manganese claim 1 , potassium claim 1 , sodium claim 1 , or zinc; salts of primary claim 1 , secondary claim 1 , and tertiary amines; and salts derived from arginine claim 1 , betaine claim 1 , caffeine claim 1 , choline claim 1 , N claim 1 ,N′-dibenzylethylenediamine claim 1 , diethylamine claim 1 , 2-diethylaminoethanol claim 1 , 2-dimethylaminoethanol claim 1 , ethanolamine claim 1 , ethylenediamine claim 1 , N-ethylmorpholinc claim 1 , N-ethylpiperidine claim 1 , glucamine claim 1 , glucosamine claim 1 , histidine claim 1 , hydrabamine claim 1 , isopropylamine claim 1 , lysine claim 1 , methylglucamine claim 1 , morpholine claim 1 , piperazine claim 1 , ...

PHARMACEUTICALLY ACCEPTABLE SALTS OF NOVEL BETULINIC ACID DERIVATIVES

The present invention relates to certain novel salts of Betulinic acid derivatives, to process for preparing such compounds, to use the compounds in treating diseases or disorders mediated by HIV infection, to methods for their therapeutic use and to pharmaceutical compositions containing them. 2. A salt of a compound selected from the group consisting of:Arginine salt of 4-((1R,3aS,5aR,5bR,9S,1aR)-3a-((1R,3S)-2,2-dimethyl-3-(piperidine-1-carbonyl)cyclobutylcarbamoyl)-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yloxy)-2,2-dimethyl-4-oxobutanoic acid (Compound 1),Amino guanidine salt of 4-((1R,3aS,5aR,5bR,9S,11aR)-3a-((1R,3S)-2,2-dimethyl-3-(piperidine-1-carbonyl)cyclobutylcarbamoyl)-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yloxy)-2,2-dimethyl-4-oxobutanoic acid (Compound 2),Calcium salt of 4-((1R,3aS,5aR,5bR,9S,11aR)-3a-((1R,3S)-2,2-dimethyl-3-(piperidine-1-carbonyl)cyclobutylcarbamoyl)-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yloxy)-2,2-dimethyl-4-oxobutanoic acid (Compound 3),Choline salt of 4-((1R,3aS,5aR,5bR,9S,11aR)-3a-((1R,3S)-2,2-dimethyl-3-(piperidine-1-carbonyl)cyclobutylcarbamoyl)-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yloxy)-2,2-dimethyl-4-oxobutanoic acid (Compound 4),Dicyclohexylamine salt of 4-((1R,3aS,5aR,5bR,9S,11aR)-3a-((1R,3S)-2,2-dimethyl-3-(piperidine-1-carbonyl)cyclobutylcarbamoyl)-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yloxy)-2,2-dimethyl-4-oxobutanoic acid (Compound 5),Diethanolamine salt of 4-((1R,3aS,5aR,5bR,9S,11aR)-3a-((1R,3S)-2,2-dimethyl-3-(piperidine-1-carbonyl)cyclobutylcarbamoyl)-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yloxy)-2,2-dimethyl-4-oxobutanoic acid (Compound 6),2,6-dimethyl piperazine salt of 4-((1R,3aS,5aR,5bR,9S,1aR)-3a-((1R,3S)-2,2-dimethyl-3-(piperidine-1-carbonyl)cyclobutylcarbamoyl ...

C-3 alkyl and alkenyl modified betulinic acid derivatives

Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, alkyl and alkenyl C-3 modified betulinic acid derivatives that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formulas I, II, III and IV: a compound of Formula I a compound of Formula II a compound of Formula III and a compound of Formula IV These compounds are useful for the treatment of HIV and AIDS.

PENTACYCLIC TRITERPENE COMPOUNDS AND USES THEREOF

Disclosed herein is a PEGylated bis pentacyclic triterpene, compositions comprising the PEGylated bis pentacyclic triterpene, methods of preparing the PEGylated bis pentacyclic triterpene, and a method of treating or preventing a fungal disease in a plant using the compounds and compositions disclosed herein. The PEGylated bis pentacyclic triterpene has the formula A-P-B, wherein A is a first pentacyclic triterpene; B is a second pentacyclic triterpene; and P is a polyethylene glycol (PEG) molecule. 1. A PEGylated bis pentacyclic triterpene having the formula:{'br': None, 'A-P-B,'}wherein,A is a first pentacyclic triterpene;B is a second pentacyclic triterpene; andP is a polyethylene glycol (PEG) molecule, for use in preventing or treating a fungal disease in a plant.2. The PEGylated bis pentacyclic triterpene of claim 1 , wherein the first and second pentacyclic triterpenes are each independently betulin claim 1 , betulinic acid claim 1 , lupeol claim 1 , or an analogue or derivative thereof.3. The PEGylated bis pentacyclic triterpene of claim 1 , wherein the first and second pentacyclic triterpenes are each betulin.4. The PEGylated bis pentacyclic triterpene of claim 1 , wherein the PEG molecule has a molecular weight of about 1500 Da to about 8 claim 1 ,000 Da.5. The PEGylated bis pentacyclic triterpene of claim 4 , wherein the PEG molecule has a molecular weight of about 3 claim 4 ,000 Da.6. The PEGylated bis pentacyclic triterpene of claim 1 , wherein the PEG molecule is α claim 1 ,ω biscarboxymethyl PEG.7. The PEGylated bis pentacyclic triterpene of claim 3 , wherein the PEG molecule is covalently bound via a first ester linkage to C3 or C28 of the first pentacyclic triterpene and via a second ester linkage to C3 or C28 of the second pentacyclic triterpene.8. The PEGylated bis pentacyclic triterpene of claim 1 , wherein the fungal disease is blight.9Phytophthora infestans, Phytophthora infestansBotrytis cinerea.. The PEGylated bis pentacyclic triterpene of ...

NEUROACTIVE STEROIDS AND COMPOSITIONS AND METHODS THEREOF

The invention provides novel neuroactive steroids and pharmaceutical compositions thereof, as well as methods of their preparation and use, in therapy of various diseases and conditions, for example, various neurological or brain diseases. 2. The compound of claim 1 , wherein at least one of Rand Ris a halogen.3. (canceled)4. The compound of claim 2 , wherein the halogen is F.5. The compound of claim 1 , wherein each of Rand Ris H6. The compound of claim 1 , wherein Ris CH.7. The compound of claim 1 , wherein Ris H.8. The compound of claim 1 , wherein Ris an unsubstituted C-Calkyl.9. The compound of claim 8 , wherein Ris an unsubstituted methyl.10. The compound of claim 8 , wherein Ris a substituted C-Calkyl.11. The compound of claim 10 , wherein Ris a substituted methyl which is substituted with a heterocyclic or heterobicyclic group.12. (canceled)14. The compound of claim 13 , wherein X is CH.15. The compound of claim 13 , wherein X is N.16. The compound of claim 13 , wherein each of X claim 13 , X claim 13 , Xand Xis CH.17. The compound of claim 13 , wherein Ris CN claim 13 , F claim 13 , is C═O(NH claim 13 , O(CHCHO)CHor CHO(CHCHO)CH.1821-. (canceled)24. A pharmaceutical composition comprising a compound according to claim 1 , effective to treat or reduce one or more diseases or disorders claim 1 , in a mammal claim 1 , including a human claim 1 , and a pharmaceutically acceptable excipient claim 1 , carrier claim 1 , or diluent.2531-. (canceled)32. A unit dosage form comprising a pharmaceutical composition of .33. (canceled)3548-. (canceled) This application claims the benefit of priority to U.S. Provisional Application No. 62/944,006, filed Dec. 5, 2019, the entire content of which is incorporated herein by reference for all purposes.The invention generally relates to pharmaceuticals and therapeutic methods. More particularly, the invention provides novel neuroactive steroids and pharmaceutical compositions thereof, as well as methods of their preparation and ...

METHOD FOR THE SEPARATION OF THE ISOPRENIC CONSTITUENTS OF GUAYULE

Method for the separation of at least one isoprenic constituent from the resin of a plant of guayule and/or of the guayule type comprising the steps of: a) providing a defatted resin of guayule and/or of the guayule type; b) subjecting the defatted resin to partitioning of the liquid-liquid type with solvents that are immiscible in each other thus obtaining an apolar extract containing the isoprenic constituents guayulin A, guayulin B and argentatin B; and a polar extract containing the isoprene constituents argentatin A, argentatin C and argentatin D; and c) separating at least one isoprenic constituent from said polar extract and/or from the apolar extract thus obtained, wherein step c) comprises a step in which the polar extract is subjected to partitioning of the liquid-liquid type with solvents immiscible in each other and/or a step in which the apolar extract is subjected to partitioning of the solid-liquid type. 1. A method for separating at least one isoprenic constituent from a resin of a guayule and/or of the guayule type plant , the method comprising:a) forming a defatted resin of a guayule, a guayule-type plant, or both;b) liquid-liquid partitioning the defatted resin with solvents that are immiscible in each other to obtain: an apolar extract comprising the isoprenic constituents guayulin A, guayulin B and argentatin B; and a polar extract comprising the isoprenic constituents argentatin A, argentatin C and argentatin D; andc) separating at least one isoprenic constituent from the polar extract, the apolar extract, or both 'liquid-liquid partitioning the polar extract with solvents that are immiscible in each other,', 'wherein the separating c) comprisessolid-liquid partitioning the apolar extract,or a combination thereof.2. The method according to claim 1 , wherein the at least one isoprenic constituent is selected from the group consisting of guayulin A claim 1 , guayulin B claim 1 , argentatin A claim 1 , argentatin B claim 1 , argentatin C claim 1 , ...

CYCLOPENTANOPERHYDROPHENANTHRENE FRAMEWORK COMPOUNDS AND PREPARATION METHOD THEREFOR

The present invention pertains to the field of pharmaceutical chemistry, and relates to compounds having cyclopentanoperhydrophenanthrene skeletons and preparation methods therefore. The compounds have some physiological activity, and are useful as synthons/intermediates for further synthesizing some compounds having specific structures. These compounds and salts thereof are useful as lead compounds for synthesizing pharmaceuticals, pesticides and new materials. From this, further screen and preparation by chemical, biological and medical means offer new compounds that are more valuable and have important applications, achieving the object of inventing and creating new drugs. The present invention relates to compounds having cyclopentanoperhydrophenanthrene skeletons and preparation methods therefore. The compounds may have some physiological activity, and are useful as synthons/intermediates for further synthesizing some compounds having specific structures.Cyclopentanoperhydrophenanthrene compounds exist widely in plants and animals, and play an important role in their life processes. Biologically active cyclopentanoperhydrophenanthrene compounds have long been a hot research area, and nowadays these compounds still play an important role in community, offering great social and economic benefits.In pharmaceutical chemistry, natural endogenous compounds from plants and animals are studied in order to find physiologically active and effective ingredients as well as lead compounds for synthesizing pharmaceuticals, pesticides and new materials. From this, further screen and preparation by chemical, biological and medical means offer new compounds that are more valuable and have important applications, achieving the object of inventing and creating new drugs. In order to enrich compound libraries, reveal biological relations of compounds, and provide new skeletons and new lead compounds for the screen of active compounds, we synthesized compounds having ...

18-METHYL-6,7-METHYLENE-3-OXO-17-PREGN-4-ENE-21,17B-CARBOLACTONES, PHARMACEUTICAL PREPARATIONS COMPRISING SAID COMPOUNDS AND USE THEREOF IN THE TREATMENT OF ENDOMETRIOSIS

The present invention relates to 18-methyl-6,7-methylene-17-pregn-4-ene-21,17β-carbolactones of general formula I 2. Compound according to claim 1 , namely 18-methyl-6β claim 1 ,7β-methylene-3-oxo-17-pregn-4-ene-21 claim 1 ,17β-carbolactone.3. 18-Methyl-6 claim 1 ,7-methylene-3-oxo-17-pregn-4-ene-21 claim 1 ,17β-carbolactone for use in the treatment of endometriosis.4. 18-Methyl-6β claim 1 ,7β-methylene-3-oxo-17-pregn-4-ene-21 claim 1 ,17β-carbolactone for use in the treatment of endometriosis.5. Pharmaceutical preparations containing at least one compound according to and at least one pharmaceutically harmless carrier.6. Pharmaceutical preparations according to further comprising at least one other active pharmaceutical ingredient selected from the group of selective oestrogen receptor modulators (SERMs) claim 5 , oestrogen receptor (ER) antagonists claim 5 , aromatase inhibitors claim 5 , 17β-HSD1 inhibitors claim 5 , steroid sulphatase (STS) inhibitors claim 5 , GnRH agonists and antagonists claim 5 , kisspeptin receptor (KISSR) antagonists claim 5 , selective androgen receptor modulators (SARMs) claim 5 , 5α-reductase inhibitors claim 5 , selective progesterone receptor modulators (SPRMs) claim 5 , gestagens claim 5 , antigestagens claim 5 , oral contraceptives claim 5 , inhibitors of mitogen activated protein (MAP) kinases and inhibitors of MAP kinase kinases (Mkk3/6 claim 5 , Mek1/2 claim 5 , Erk1/2) claim 5 , inhibitors of protein kinases B (PKBα/β/γ; Akt1/2/3) claim 5 , inhibitors of phosphoinositide-3-kinases (PI3K) claim 5 , inhibitors of cyclin-dependent kinase (CDK1/2) claim 5 , inhibitors of the hypoxia-induced signalling pathway (HIF1alpha inhibitors claim 5 , activators of prolylhydroxylases) claim 5 , histone deacetylase (HDAC) inhibitors claim 5 , prostaglandin F receptor (FP) (PTGFR) antagonists or non-steroidal anti-inflammatory drugs (NSAIDs) in a pharmaceutically harmless carrier.7. Pharmaceutical preparations according to containing a compound ...

METHOD FOR PRODUCING 30-HALOGENATED BETULINIC ACID

The invention discloses a method for producing 30-halogenated betulinic acid. Betulin is used as a raw material and selectively oxidized and halogenated to generate 30-betulinic acid, and the selected oxidation and halogenation agent has high selectivity and does not affect C-3 hydroxyl or carbon-carbon double bonds. Oxidation and halogenation are completed in one step, so the process route is short, the treatment method is simple, and the product is purified easily. 1. A method for producing 30-halogenated betulinic acid , wherein betulinol is selectively oxidized and halogenated to give a crude 30-halogenated betulinic acid , and then the crude 30-halogenated betulinic acid is purified to obtain 30-halogenated betulinic acid product.2. The method for producing 30-halogenated betulinic acid according to claim 1 , wherein the 30-halogenated betulinic acid is selected from 30-chloro-betulinic acid and 30-bromo-betulinic acid.3. A method for producing 30-halogenated betulinic acid claim 1 , wherein betulinol is used as starting material claim 1 , comprising the following steps in turn:(1) Oxidation and halogenation of betulinol to prepare a crude 30-halogenated betulinic acid: the betulinol being dissolved in an organic solvent and added with 2,2,6,6-tetramethyl-1-piperidone, sodium bicarbonate and an oxidizing and halogenating agent, stirred at 40˜60° C. for 3˜5 hours, then terminating the reaction by adding ethanol, filtering, and the filtrate being acidified with hydrochloric acid to pH of 3.5 to 4.5, concentrated under reduced pressure to precipitate out, and then the resulting precipitate being filtered and washed with distilled water and naturally dried to give a crude 30-halogenated betulinic acid; and(2) Purification of the crude 30-halogenated betulinic acid to obtain 30-halogenated betulinic acid product: the crude 30-halogenated betulinic acid being purified by recrystallization to obtain 30-halogenated betulinic acid product.4. The method for producing 30- ...

Method for producing microparticles from pressurized and heated starting material solution

The present invention addresses the problem of providing a method for efficiently producing uniform microparticles of curcumin and/or γ-oryzanol at a higher yield. The target microparticles are produced by dissolving a starting material in a solvent to give a starting material solution and then subjecting the starting material solution to crystallization by a poor solvent method to thereby deposit the starting material. To prepare the starting material solution, curcumin and/or γ-oryzanol are used as the starting material(s) and ethanol is used as the solvent. The starting material(s) and the solvent are stirred in a pressurized state at a temperature of 78.3-130° C. inclusive to give the starting material solution. Then, the starting material solution thus obtained is subjected to crystallization by the poor solvent method and thus the target microparticles are produced.

ENRICHMENT OF TRITERPINE ESTERS

A new process for enriching triterpene esters comprising: providing a mixture comprising a non-distilled vegetable oil and/or a non-distilled vegetable fat, further comprising triterpene esters, performing a mild transesterification with a lower alcohol, removing lower alcohol esters by deodorization, physical refining, evaporation or distillation, and recovering the remaining fraction rich in triterpene esters. Triterpene esters enriched with the method as well as uses of the same are also provided. One advantage is that it is a more economically viable way of achieving higher concentration of triterpene esters. There is both the chance to fully keep the natural distribution of triterpene esters but in the other end also to replace the natural level of cinnamic and acetic acids-triterpene esters with a high level of long fatty acid triterpene-esters. 1. A process for enriching triterpene esters comprising:providing a mixture comprising at least one non-distilled vegetable oil or non-distilled vegetable fat, wherein the mixture further comprises at least one triterpene ester,performing a mild transesterification with at least one lower alcohol at a temperature equal to or lower than the boiling point of the mixture, to obtain lower alcohol esters,removing the lower alcohol esters by at least one procedure chosen from deodorization, physical refining, evaporation and distillation, andrecovering the remaining fraction rich in triterpene esters.2. The process according to claim 1 , wherein the mixture comprises at least one vegetable oil chosen from rice bran oil claim 1 , shea butter claim 1 , shea butter oil claim 1 , avocado oil claim 1 , olive oil claim 1 , soy bean oil claim 1 , rape seed oil claim 1 , mango butter claim 1 , argon oil claim 1 , palm oil claim 1 , red palm oil claim 1 , coconut oil claim 1 , palm kernel oil claim 1 , safflower oil claim 1 , cocoa butter claim 1 , almond oil claim 1 , sun flower oil claim 1 , peach kernel oil claim 1 , evening ...

NATURAL PRODUCT ANALOGS INCLUDING AN ANTI-INFLAMMATORY CYANOENONE PHARMACORE AND METHODS OF USE

This invention provides novel compounds comprising the following anti-inflammatory pharmacore: 2. The compound of claim 1 , wherein Rand Rare each independently hydrogen claim 1 , alkylor substituted alkyl.36-. (canceled)8. The compound of claim 7 , wherein Rand Rare each independently hydrogen claim 7 , alkylor substituted alkyl.915-. (canceled)16. The compound of claim 7 , wherein X is —CN.1718-. (canceled)20173-. (canceled)174. A method of making a compound of claim 1 , comprising:(a) obtaining an organic compound having two to eight five and/or six-membered rings, provided that the organic compounds is not argentatin, betulinic acid, lanostane, oleanic acid, boswellic acid, glycyrrhetinic acid, ursolic acid, or tricyclic-bis-enone;{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, '(b) reacting the organic compound in a series of one of more steps to obtain a compound according to .'}175. The method of claim 174 , wherein the compound's induction of Nrf2 activity is at least ten times higher than the organic compound's induction of Nrf2 activity.176. The method of claim 174 , wherein the compound's inhibition of NF-κB activity is at least ten times higher than the organic compound's inhibition of NF-κB activity.177. The method of claim 174 , wherein the compound's inhibition of IFNγ induced NO activity is at least ten times higher than the organic compound's inhibition of IFNγ induced NO activity. The present application is a continuation application of U.S. patent application Ser. No. 14/950,557, filed Nov. 24, 2015, now U.S. Pat. No. 9,796,668, which is a divisional application of U.S. patent application Ser. No. 13/552,530, filed Jul. 18, 2012, now U.S. Pat. No. 9,233,998, which is a continuation application of U.S. patent application Ser. No. 12/426,889, filed Apr. 20, 2009, now U.S. Pat. No. 8,258,329, which claims the benefit of priority to U.S. Provisional Application No. 61/046,363, filed Apr. 18, 2008, the entire contents of each of which are ...

AMPHIPHILIC COMPOUNDS WITH NEUROPROTECTIVE PROPERTIES

Amphiphilic compounds with tetradecahydrophenanthrene skeleton and their enantiomers, exhibiting neuroprotective effects, their use in methods of treatment of neuropsychiatric disorders associated with an imbalance in glutamatergic neurotransmitter system, such as ischemic damage of CNS, neurodegenerative changes and disorders of CNS, affective disorders, depression, post-traumatic stress disorder and diseases related to stress, anxiety, schizophrenia and psychotic disorders, pain, addiction, multiple sclerosis, epilepsy, glioma, and a pharmaceutical composition containing compound. 2. The amphiphilic compound of general formula I according to claim 1 , selected from:pyridinium (2R,4aS,4bS,8aR,10aR)-4a-methyltetradecahydrophenanthren-2-yl 2-sulfate (8), pyridinium (2R,4aS,4bS,7 S,8S,8 aS,10aR)-7-(methoxymethyl)-4a,7,8-trimethyltetradecahydrophenanthren-2-yl 2-sulfate (18),4-(((2R,4aS,4bS,7S,8aS,10aR)-7 -(methoxymethyl)-4a,7,8-trimethyltetradecahydrophenanthren-2-yl)oxy)-4-oxobutanoic acid (19),pyridinium (2R,4aS,7S, 8S,10aR)-7-(methoxycarbonyl)-4a,7 ,8-trimethyltetradecahydrophenanthren-2-yl 2-sulfate (22),4-(((2R,4aS,4bS,7R,8aS,10aR)-4a,7-dimethyltetradecahydrophenanthren-2-yl)oxy)-4-oxobutanoic acid (34),pyridinium (2R,4aS,4bS,7R,8aS,10aR)-4a,7-dimethyltetradecahydrophenanthren-2-yl 2-sulfate (35), methyl (2S,4aS,4bS,7R,8aR,10aS)-2,4b-dimethyl-7-(sulfooxy)tetradecahydrophenanthren-2-carboxylate (40),pyridinium (3R,5R,8S,9S,10S,13S,14S)-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-3-yl 3-sulfate (49),2-(((3R,5R,8S,9S,10S,13S,14S)-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)oxy)-2-oxoethanoic acid (50),2-(((3R,5R,8S,9S,10S,13S,14S)-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)oxy)-2-oxopropanoic acid (51),2-(((3R,5R,10S,13S,14S)-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)amino)-2-oxoacetic acid (59),((3R,5R,8S,9S,10S,13S,14S)-10,13-dimethylhexadecahydro-1H-cyclopenta[a]fenanthren-3-yl)amino)-3- ...

PROCESS FOR THE PREPARATION OF DROSPIRENONE

It is described of a process for the preparation of drospirenone, the compound of formula 1 shown below, a synthetic steroid with progestogenic, antimineralocorticoid and antiandrogenic activity, useful for preparing pharmaceutical compositions having contraceptive action, starting from 17α-(3-hydroxypropyl)-6β,7β;15β,16β-dimethylene-5β-androstane-3β,5,17β-trioI. 1. Process for the preparation of drospirenone comprising the following steps:a) oxidation of the compound 17α-(3-hydroxypropyl)-6β,7β;15β,16β-dimethylene-5β-androstane-3β,5,17β-triol with an oxidizing agent in the presence of a catalytic amount of 2,2,6,6-tetramethylpiperidine-1-oxyl radical or a derivative thereof;b) removal of the solvent from the reaction mixture by distillation, obtaining a raw oily product containing 6β,7β;15β,16β-dimethylene-5β-hydroxy-3-oxo-17α-androstane-21,17-carbolactone;c) addition to said raw oily product of a mixture of water and an organic base and heating of the resulting mixture at a temperature comprised between 45 and 90° C., to form drospirenone.2. The process according to claim 1 , wherein steps a) claim 1 , b) and c) take place in a single reaction container claim 1 , with no isolation and purification of intermediate compounds.3. The process according to claim 1 , wherein the oxidizing agent is selected from the group consisting of hypohalides of alkali and alkaline-earth metals claim 1 , iodine claim 1 , oxygen in the presence of CuCI claim 1 , potassium peroxymonosulfate (KHSO) claim 1 , and 1 claim 1 ,3 claim 1 ,5-trichloro-2 claim 1 ,4 claim 1 ,6-triazinetrione.4. The process according to claim 3 , wherein said oxidizing agent is selected from the group consisting of calcium hypochlorite and sodium hypochlorite.5. The process according to claim 4 , wherein the oxidizing agent is employed in an amount claim 4 , measured in equivalents claim 4 , at least equal to 3 times the number of moles of 17α-(3-hydroxypropyl)-6β claim 4 ,7β;15β claim 4 ,16β-dimethylene-5β- ...

COMPOUNDS AND COMPOSITIONS FOR TREATING HIV WITH DERIVATIVES OF BETULIN

The present invention relates to compounds characterized by having a structure according to the following Formula I: 1128-. (canceled)134. The method according to claim 133 , wherein the administering is performed separately.135. The method according to claim 133 , wherein the administering is performed simultaneously.137. The method according to claim 136 , wherein the administering is performed separately.138. The method according to claim 136 , wherein the administering is performed simultaneously.140. The method according to claim 139 , wherein the administering is performed separately.141. The method according to claim 139 , wherein the administering is performed simultaneously.143. The method according to claim 142 , wherein the administering is performed separately.144. The method according to claim 142 , wherein the administering is performed simultaneously. This is a Continuation application of U.S. application Ser. No. 14/461,731 filed 18 Aug. 2014, now abandoned, which is a Continuation application of U.S. patent application Ser. No. 13/714,627, now granted U.S. Pat. No. 9,102,685, which claims priority to US Provisonal Application No. 61/576,448 filed 16 Dec. 2011, which is hereby incorporated by reference in its entirety.The present invention relates to compounds, pharmaceutical compositions, and methods of use thereof for (i) inhibiting HIV replication in a subject infected with HIV, or (ii) treating a subject infected with HIV, by administering such compounds.Human immunodeficiency virus type 1 (HIV-1) leads to the contraction of acquired immune deficiency disease (AIDS). The number of cases of HIV continues to rise, and currently over twenty-five million individuals worldwide suffer from the virus. Presently, long-term suppression of viral replication with antiretroviral drugs is the only option for treating HIV-1 infection. Indeed, the U.S. Food and Drug Administration has approved twenty-five drugs over six different inhibitor classes, which have ...

C-3 AND C-17 MODIFIED TRITERPENOIDS AS HIV-1 INHIBITORS

Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, betulinic acid derivatives that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formula I: 1. The compoundor a pharmaceutically acceptable salt thereof. The present invention relates to novel compounds useful against HIV and, more particularly, to compounds derived from betulinic acid and other compounds which are useful as HIV maturation inhibitors, and to pharmaceutical compositions containing same, as well as to methods for their preparation.HIV-1 (human immunodeficiency virus-1) infection remains a major medical problem, with an estimated 45-50 million people infected worldwide at the end of 2010. The number of cases of HIV and AIDS (acquired immunodeficiency syndrome) has risen rapidly. In 2005, approximately 5.0 million new infections were reported, and 3.1 million people died from AIDS. Currently available drugs for the treatment of HIV include nucleoside reverse transcriptase (RT) inhibitors or approved single pill combinations: zidovudine (or AZT or RETROVIR®), didanosine (or VIDEX®), stavudine (or ZERIT®), lamivudine (or 3TC or EPIVIR®), zalcitabine (or DDC or HMD®), abacavir succinate (or ZIAGEN®), tenofovir disoproxil fumarate salt (or VIREAD®), emtricitabine (or FTC-EMTRIVA®), COMBIVIR® (contains −3TC plus AZT), TRIZIVIR® (contains abacavir, lamivudine, and zidovudine), EPZICOM® (contains abacavir and lamivudine), TRUVADA® (contains VIREAD® and EMTRIVA®); non-nucleoside reverse transcriptase inhibitors: nevirapine (or VIRAMUNE®), delavirdine (or RESCRIPTOR®) and efavirenz (or SUSTIVA®), ATRIPLA® (TRUVADA®+SUSTIVA®), and etravirine, and peptidomimetic protease inhibitors or approved formulations: saquinavir, indinavir, ritonavir, nelfinavir, amprenavir, lopinavir, KALETRA® (lopinavir and Ritonavir), darunavir, atazanavir (REYATAZ®) and tipranavir (APTIVUS®) and ...

Derivatives of Betulin

The present invention relates to compounds characterized by having a structure according to the following Formula I: , or a pharmaceutically acceptable salt thereof. Compounds of the present invention are useful for the treatment or prevention of HIV.

Compositions and Methods For Increasing Telomerase Activity

The present invention relates to methods and compositions for increasing telomerase activity in cells. Such compositions include pharmaceutical formulations. The methods and compositions are useful for treating diseases subject to treatment by an increase in telomerase activity in cells or tissue of a patient. They are also useful for enhancing replicative capacity of cells in culture, as in ex vivo cell therapy and for enhancing proliferation of stem and progenitor cells. 7. The compound of claim 1 , wherein at least one of Xor Xis —OC(O)CH(NH)CH(CH)CHCH.8. The compound of claim 1 , wherein both Xand Xare —OC(O)CH(NH)CH(CH)CHCH.10. The compound of claim 1 , wherein Xis a —OC(O)CH(NH)CH(CH)and Xand Xare OH.11. The compound of claim 1 , wherein Xis a —OC(O)CH(NH)CH(CH)CHCHand Xand Xare —OH.12. The compound of claim 1 , wherein Xis a —OC(O)CH(NH)CH(CH)and Xand Xare OH.13. The compound of claim 1 , wherein Xis a —OC(O)CH(NH)CH(CH)CHCHand Xand Xare OH.15. The compound of wherein the pharmaceutically acceptable salt is hydrochloride salt.16. A compound selected from the group consisting of:2-(L)-amino-3-methyl-butyric acid 6α, 16β-dihydroxy-17-[5-(1-hydroxy-1-methyl-ethyl)-2-methyl-tetrahydro-furan-2-yl]-4,4,13,14-tetramethyl-tetradecahydro-cyclopropa[9,10]cyclopenta[a]phenanthren-30-yl ester;2-(L)-amino-3-methyl-butyric acid 6α-(2-amino-3-methyl-butyryloxy)-16β-hydroxy-17-[5-(1-hydroxy-1-methyl-ethyl)-2-methyl-tetrahydro-furan-2-yl]-4,4,13,14-tetramethyl-tetradecahydro-cyclopropa[9,10]cyclopenta[a]phenanthren-3β-yl ester;2-(L)-tert-butoxycarbonylamino-3-methyl-butyric acid 3b-acetoxy-16b-hydroxy-17-[5-(1-hydroxy-1-methyl-ethyl)-2-methyl-tetrahydro-furan-2-yl]-4,4,13,14-tetramethyl-tetradecahydro-cyclopropa[9,10]cyclopenta[a]phenanthren-6a-yl ester;2-(L),3-dimethyl-pentanoic acid 6α,16β-di hydroxy-17-[5-(1-hydroxy-1-methyl-ethyl)-2-methyl-tetrahydro-furan-2-yl]-4,4,13,14-tetramethyl-tetradecahydro-cyclopropa[9,10]cyclopenta[a]phenanthren-3β-yl ester,2-(L)-Amino-3-methyl- ...

TOMATIDINE, ANALOGS THEREOF, COMPOSITIONS COMPRISING SAME, AND USES FOR SAME

In one aspect, the invention relates to methods for promoting muscle hypertrophy or decreasing adiposity by providing to an animal in need thereof an effective amount of a compound. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention. 3. The method according to claim 2 , wherein Ris H and Ris H.6. The method according to claim 1 , wherein said composition comprises not less than 0.14% by weight of said compound or pharmaceutically acceptable salt thereof.7. The method according to claim 1 , wherein said composition comprises not less than 0.28% by weight of said compound or pharmaceutically acceptable salt thereof.8. The method according to claim 2 , wherein the compound or pharmaceutically acceptable salt thereof is present in an amount greater than 5 mg.9. The method according to claim 1 , wherein the composition is a solution claim 1 , dispersion claim 1 , suspension or emulsion.10. The method according to claim 1 , wherein said composition is a nutraceutical claim 1 , animal chow claim 1 , medicinal food claim 1 , energy bar claim 1 , energy drink claim 1 , sports drink claim 1 , protein bar claim 1 , tea claim 1 , coffee claim 1 , milk claim 1 , milk product claim 1 , cereal claim 1 , oatmeal claim 1 , infant formula claim 1 , or supplement.11. The method according to claim 10 , wherein the compound is α-tomatine.12. The method according to claim 10 , comprising administering the composition orally claim 10 , and wherein the composition comprises a preservative.13. The method according to claim 12 , wherein the composition is animal chow.14. The method according to claim 13 , wherein the animal chow additionally comprises at least one further additive selected from the group consisting of flavoring agents claim 13 , coloring agents claim 13 , and binders.16. The method according to claim 15 , comprising administering the composition so as to provide to the ...

C-3 novel triterpenone with c-28 urea derivatives as hiv inhibitors

The present invention relates to C-3 novel triterpenone with C-28 urea derivatives of formula (I); or pharmaceutically acceptable salts, pharmaceutically acceptable solvates, pharmaceutically acceptable hydrates, tautomers, stereoisomers, prodrugs, compositions or combination thereof, wherein R 1 , R 2 , R 3 , W, J and X are as defined herein. The present invention also relates to pharmaceutical compositions comprising compounds of formula (I) useful for the treatment of viral diseases and particularly HIV mediated diseases.

COMPOSITIONS AND METHODS FOR INCREASING TELOMERASE ACTIVITY

The present invention relates to methods and compositions for increasing telomerase activity in cells. Such compositions include pharmaceutical formulations. The methods and compositions are useful for treating diseases subject to treatment by an increase in telomerase activity in cells or tissue of a patient. They are also useful for enhancing replicative capacity of cells in culture, as in ex vivo cell therapy and for enhancing proliferation of stem and progenitor cells. 7. The compound of claim 1 , wherein at least one of Xor Xis —OC(O)CH(NH)CH(CH)CHCH.8. The compound of claim 1 , wherein both Xand Xare —OC(O)CH(NH)CH(CH)CHCH.10. The compound of claim 1 , wherein Xis a —OC(O)CH(NH)CH(CH)and Xand Xare OH.11. The compound of claim 1 , wherein Xis a —OC(O)CH(NH)CH(CH)CHCHand Xand Xare —OH.12. The compound of claim 1 , wherein Xis a —OC(O)CH(NH)CH(CH)and Xand Xare OH.13. The compound of claim 1 , wherein Xis a —OC(O)CH(NH)CH(CH)CHCHand Xand Xare OH.15. The compound of wherein the pharmaceutically acceptable salt is hydrochloride salt.16. A compound selected from the group consisting of:2-(L)-amino-3-methyl-butyric acid 6α,16β-dihydroxy-17-[5-(1-hydroxy-1-methyl-ethyl)-2-methyl-tetrahydro-furan-2-yl]-4,4,13,14-tetramethyl-tetradecahydro-cyclopropa[9,10]cyclopenta[a]phenanthren-3β-yl ester;2-(L)-amino-3-methyl-butyric acid 6α-(2-amino-3-methyl-butyryloxy)-16β-hydroxy-17-[5-(1-hydroxy-1-methyl-ethyl)-2-methyl-tetrahydro-furan-2-yl]-4,4,13,14-tetramethyl-tetradecahydro-cyclopropa[9,10]cyclopenta[a]phenanthren-3β-yl ester;2-(L)-tert-butoxycarbonylamino-3-methyl-butyric acid 3b-acetoxy-16b-hydroxy-17-[5-(1-hydroxy-1-methyl-ethyl)-2-methyl-tetrahydro-furan-2-yl]-4,4,13,14-tetramethyl-tetradecahydro-cyclopropa[9,10]cyclopenta[a]phenanthren-6a-yl ester;2-(L),3-dimethyl-pentanoic acid 6α,16β-di hydroxy-17-[5-(1-hydroxy-1-methyl-ethyl)-2-methyl-tetrahydro-furan-2-yl]-4,4,13,14-tetramethyl-tetradecahydro-cyclopropa[9,10]cyclopenta[a]phenanthren-3β-yl ester,2-(L)-Amino-3-methyl- ...

Contraceptive Use of Triterpenoids

Disclosed are systemic and intravaginal non-hormonal contraceptives comprising a spermicidal triterpenoid. The contraceptive may be in the form of a foam, cream or gel, or in unit form of a pill, vaginal contraceptive film (VCF), suppository, sponge, transdermal or hypodermal patches or a slow release intravaginal device or intrauterine device such as a drug-impregnated silicone elastomer vaginal ring or polymeric IUD. 1. A pharmaceutical composition comprising a spermicidal plant triterpenoid formulated and configured as an intravaginal or systemic contraceptive.2. The composition of formulated and configured in form of a vaginal contraceptive foam claim 1 , cream or gel claim 1 , and the triterpenoid is in a predetermined claim 1 , unit or multi-unit dosage effective for contraception.3. The composition of formulated and configured in unit form of a vaginal contraceptive film (VCF) claim 1 , suppository claim 1 , sponge claim 1 , slow release intravaginal devices or intrauterine devices such as drug-impregnated silicone elastomer vaginal rings or polymeric IUDs claim 1 , and the triterpenoid is in a predetermined claim 1 , unit dosage effective for contraception.4. The composition of formulated and configured in form of a systemic contraceptive that is a pill claim 1 , transdermal or hypodermal patch claim 1 , and the triterpenoid is in a predetermined claim 1 , unit or multi-unit dosage effective for contraception.5. The composition of claim 1 , wherein the triterpenoid inhibits human tubular fluid claim 1 , progesterone (P4)- or pregnenolone sulfate (PregS)-induced activation of the principal human sperm calcium channel claim 1 , CatSper claim 1 , such as indicated by calcium imaging or recording of inward monovalent currents (I) through the channel with electrophysiology or calcium imaging.6. The composition of claim 1 , wherein the triterpenoid inhibits P4- or PregS-induced human sperm hyperactivation claim 1 , sperm motility or fertilization.7. The ...

NOVEL BETULINIC ACID PROLINE DERIVATIVES AS HIV INHIBITORS

The invention relates to novel betulinic acid derivatives and related compounds, and pharmaceutical compositions useful for the therapeutic treatment of viral diseases and particularly HIV mediated diseases. 2. The compound of claim 1 , wherein W is —C(O)—.3. The compound of claim 1 , wherein when R claim 1 , R claim 1 , or both are substituted amino acid claim 1 , the amino acid is substituted by substituted or unsubstituted alkyl claim 1 , phosphoric acid claim 1 , or phosphorus prodrugs.5. The compound of claim 4 , wherein W is —C(O)—.7. The compound of claim 6 , wherein W is —C(O)—.8. A compound selected from the group consisting of2,2-dimethyl-4-oxo-4-((1R,3aS,5aR,5bR,7aR,9S,11aR,11bR,13aR,13bR)-5a,5b,8,8,11a-pentamethyl-3a-((R)-2-(3-phenyl-1,2,4-oxadiazol-5-yl)pyrrolidine-1-carbonyl)-1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yloxy)butanoic acid,3,3-dimethyl-5-oxo-5-((1R,3aS,5aR,5bR,7aR,9S,11aR,11bR,13aR,13bR)-5a,5b,8,8,11a-pentamethyl-3a-((R)-2-(3-phenyl-1,2,4-oxadiazol-5-yl)pyrrolidine-1-carbonyl)-1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yloxy)pentanoic acid,2,2-dimethyl-4-oxo-4-((1R,3aS,5aR,5bR,7aR,9S,11aR,11bR,13aR,13bR)-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-yl)-3a-((R)-2-(3-(pyridin-3-yl)-1,2,4-oxadiazol-5-yl)pyrrolidine-1-carbonyl)icosahydro-1H-cyclopenta[a]chrysen-9-yloxy)butanoic acid,3,3-dimethyl-5-oxo-5-((1R,3aS,5aR,5bR,7aR,9S,11aR,11bR,13aR,13bR)-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-yl)-3a-((R)-2-(3-(pyridin-3-yl)-1,2,4-oxadiazol-5-yl)pyrrolidine-1-carbonyl)icosahydro-1H-cyclopenta[a]chrysen-9-yloxy)pentanoic acid,2,2-dimethyl-4-oxo-4-((1R,3aS,5aR,5bR,7aR,9S,11aR,11bR,13aR,13bR)-5a,5b,8,8,11a-pentamethyl-1-(1-methylcyclopropyl)-3a-((R)-2-(3-phenyl-1,2,4-oxadiazol-5-yl)pyrrolidine-1-carbonyl)icosahydro-1H-cyclopenta[a]chrysen-9-yloxy)butanoic acid,3,3-dimethyl-5-oxo-5-((1R,3aS,5aR,5bR,7aR,9S,11aR,11bR,13aR,13bR)-5a,5b,8,8,11a-pentamethyl-1-(1-methylcyclopropyl)-3a-((R)-2-(3-phenyl-1,2,4-oxadiazol-5-yl)pyrrolidine-1- ...

DERIVATIVES OF BETULIN

The present invention relates to compounds characterized by having a structure according to the following Formula I: 2. The compound of claim 1 , wherein Land Lare both [C(RR)].3. The compound of claim 1 , wherein Land Lare both —CH—.4. The compound of claim 1 , wherein each instance of q is independently 1 claim 1 , 2 claim 1 , or 3.5. The compound of claim 1 , wherein q is 1.6. The compound of claim 1 , wherein W is O.7. The compound of claim 1 , wherein W is a bond.8. The compound of claim 1 , wherein when W is a bond claim 1 , then Ris —H.9. The compound of claim 1 , wherein when W is O claim 1 , then Ris —H.10. The compound of claim 1 , wherein Qin the A group is absent and Q claim 1 , in the A group is —CH— and the Q in the Formula I structure is C(═O)11. The compound of claim 1 , wherein Ris —H.12. The compound of claim 1 , wherein Ris —(CH)NRR.13. The compound of claim 1 , wherein Ris (dimethylamino)ethyl.14. The compound of claim 1 , wherein each instance of r is independently 0 claim 1 , 1 claim 1 , 2 claim 1 , or 3.15. The compound of claim 1 , wherein r is 2.17. The compound of claim 1 , wherein X is a monocyclic (C-C)aryl.18. The compound of claim 1 , wherein X is phenyl.19. The compound of claim 1 , wherein Ris —H.20. The compound of claim 1 , wherein each instance of m is independently 0 or 1.21. The compound of claim 1 , wherein m is 0.22. The compound of claim 1 , wherein m is 1.23. The compound of claim 1 , wherein n is 1.24. The compound of claim 1 , wherein Rand R are both —H.25. The compound of claim 1 , wherein Rand Rare both (C-C)alkyl.26. The compound of claim 1 , wherein Ris methyl.27. The compound of claim 1 , wherein Ris methyl.28. The compound of claim 1 , wherein Rand Rare both methyl.29. The compound of claim 1 , wherein Ris halo.30. The compound of claim 1 , wherein Ris selected from chloro claim 1 , bromo claim 1 , or fluoro.31. The compound of claim 1 , wherein Ris chloro.32. The compound of claim claim 1 , wherein Ris absent.33. The ...

N-acetyl amino acid ESTER derivatives of Betulin and preparation method thereof

The present invention disclosed N-acetyl amino acid ester derivatives of betulin and the preparation method thereof, the method comprising the steps that in the presence of an alkaline substance, a catalyst and a racemization-inhibitor, the carboxyl group of N-acetyl amino acid is activated by a coupling agent; and then the activated N-acetyl amino acid is reacted with betulin via esterification reaction to obtain the N-acetyl amino acid ester derivative of betulin. The present invention provided a simple synthesis method to synthesize the N-acetyl amino acid ester derivatives of betulin by using betulin as a precursor compound and modifying the molecular structure of betulin. Such structural modification of betulin significantly enhances the anti-tumor activity of the betulin derivatives and therefore has important values. 2. A method for preparing the N-acetyl amino acid ester derivative of betulin of claim 1 , comprising the steps that in the presence of an alkaline substance claim 1 , a catalyst and a racemization-inhibitor claim 1 , the carboxyl group of N-acetyl amino acid is activated by a coupling agent; and then the activated N-acetyl amino acid is reacted with betulin via esterification reaction to obtain the N-acetyl amino acid ester derivative of betulin.3. The method for preparing the N-acetyl amino acid ester derivative of betulin according to claim 2 , further comprising the steps that a N-acetyl amino acid claim 2 , an alkaline substance claim 2 , a catalyst and a racemization-inhibitor are added into an organic solvent claim 2 , and an coupling agent is added after adequate stirring claim 2 , to react for 0.5 to 4 hours at 20˜50° C. under nitrogen; and then claim 2 , betulin is added to react for 8 to 24 hours at 20˜50° C. claim 2 , thereby to obtain the N-acetyl amino acid ester derivative of betulin.4. The method for preparing the N-acetyl amino acid ester derivative of betulin according to claim 2 , further comprising the purification step of the ...

C-3 AND C-17 MODIFIED TRITERPENOIDS AS HIV-1 INHIBITORS

Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, betulinic acid derivatives that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formula I: 2. A pharmaceutical composition comprising a compound or salt of .3. A method for treating a mammal infected with the HIV virus comprising administering to said mammal a composition of . The present invention relates to novel compounds useful against HIV and, more particularly, to compounds derived from betulinic acid and other compounds which are useful as HIV maturation inhibitors, and to pharmaceutical compositions containing same, as well as to methods for their preparation.HIV-1 (human immunodeficiency virus-1) infection remains a major medical problem, with an estimated 45-50 million people infected worldwide at the end of 2010. The number of cases of HIV and AIDS (acquired immunodeficiency syndrome) has risen rapidly. In 2005, approximately 5.0 million new infections were reported, and 3.1 million people died from AIDS. Currently available drugs for the treatment of HIV include nucleoside reverse transcriptase (RT) inhibitors or approved single pill combinations: zidovudine (or AZT or RETROVIR®), didanosine (or VIDEX®), stavudine (or ZERIT®), lamivudine (or 3TC or EPIVIR®), zalcitabine (or DDC or HIVID®), abacavir succinate (or ZIAGEN®), tenofovir disoproxil fumarate salt (or VIREAD®), emtricitabine (or FTC-EMTRIVA®), COMBIVIR® (contains-3TC plus AZT), TRIZIVIR® (contains abacavir, lamivudine, and zidovudine), EPZICOM® (contains abacavir and lamivudine), TRUVADA® (contains VIREAD® and EMTRIVA®); non-nucleoside reverse transcriptase inhibitors: nevirapine (or VIRAMUNE®), delavirdine (or RESCRIPTOR®) and efavirenz (or SUSTIVA®), ATRIPLA® (TRUVADA®+SUSTIVA®), and etravirine, and peptidomimetic protease inhibitors or approved formulations: saquinavir, indinavir, ritonavir, ...

MOLECULAR HOST FRAMEWORKS AND METHODS OF MAKING AND USING SAME

Crystalline molecular framework:small molecule compounds. The molecular framework is formed from guanidinium cations and organosulfonate anions and the guanidinium cations and organosulfonate anions are associated via one or more hydrogen bond. The small molecule(s) is/are encapsulated by the molecular framework. Methods for making crystalline molecular framework:small molecule compounds may include combining guanidinium cations, organosulfonate anions, and small molecules in a single step. The crystalline molecular framework:small molecule compounds can be used to determine the structure of the small molecule(s). 1. A crystalline molecular framework:small molecule compound comprising a molecular framework and one or more small molecules , wherein the molecular framework comprises a plurality of guanidinium cations and a plurality of organosulfonate anions , wherein the guanidinium cations and organosulfonate anions are associated via one or more hydrogen bond and the small molecule(s) is/are encapsulated by the molecular framework.2. The compound of claim 1 , wherein the plurality of organosulfonate anions is chosen from organomonosulfonate anions and organopolysulfonate anions.3. The compound of claim 2 , wherein the organopolysulfonates anions are chosen from organodisulfonates anions claim 2 , organotrisulfonates anions claim 2 , organotetrasulfonates anions claim 2 , and organopentasulfonate anions.4. The compound of claim 1 , wherein the compound is a single crystal.5. The compound of claim 1 , wherein the compound comprises one or more crystalline domain having at least one dimension of 100 nm to 200 μm.6. The compound of claim 1 , wherein each small molecule is a hydrocarbon.7. The compound of claim 1 , wherein the molecular framework does not comprise a metal and/or the small molecule does not comprise a metal atom or metal ion.8. The compound of claim 1 , wherein at least one small molecule or all of the small molecules has/have one or more stereocenters.9 ...

Triterpene-containing oleogel, triterpene-containing oleogel and process for the preparation of a triterpenhaltigen oleogel

Die vorliegende Erfindung betrifft einen Oleogelbildner, der wenigstens ein hochdisperses Triterpen aufweist. Die Erfindung betrifft außerdem ein Oleogel, das eine unpolare Flüssigkeit mit einem Anteil zwischen 80 Gew.-% und 99 Gew.-%, bezogen auf das Gesamtgewicht des Gels, und einen ein hochdisperses Triterpen aufweisenden Oleogelbildner mit einem Anteil zwischen 1 Gew.-% und 20 Gew.-%, bezogen auf das Gesamtgewicht des Gels, aufweist. Die Erfindung betrifft außerdem ein Verfahren zur Herstellung eines Oleogels. The present invention relates to an oleogel former comprising at least one highly dispersed triterpene. The invention further relates to an oleogel which comprises a nonpolar liquid in a proportion of between 80% and 99% by weight, based on the total weight of the gel, and a oleogel former containing a highly dispersed triterpene, in an amount of between 1% by weight. and 20% by weight, based on the total weight of the gel. The invention also relates to a process for the preparation of an oleogel.

3-Beta,7-beta,15-alpha-trihydroxy-5-androsten-17-one, its 3,15-dipivalate, and its preparation

A process for the preparation of 3β,7β,15α-trihydroxy-5- androsten-17-one and the 3,15-dipivalate thereof comprises epimerizing 3p,7a,15a-trihydroxy-5-androsten-17-one in the presence of a ketone with or without a solvent, with dilute mineral acid and subsequent treatment with an organic base, and optionally subsequently esterifying the 3p- and 15a-positions of the resultant 3β,7β,15α-triol with a reactive derivative of pivalic acid.

Process for the preparation of Drospirenone

A process for the preparation of Drospirenone (I) according to the following scheme wherein the substituent R is defined in the description. The process improves the product yield and purity by reducing the formation of undesired side-products and is particularly convenient for industrial-scale manufacturing.

Process for the preparation of 17-alpha-acyloxy-6-chloro-1-alpha,2-alpha-methylene-4,6-pregnadiene-3-20-diones

16ALFA, 17BETA-METILEN-ESTRA-4,9-DIEN-3-ONAS REPLACED IN 11BETA.

EL INVENTO SE REFIERE A UNA NUEVA 11(BETA) 16 (ALFA), 17(ALFA) FORMULA (I), TRATA DE UN PROCEDIMIENTO PARA LA PRODUCCION DEL COMPUESTO DE FORMULA (I); RESEÑA LA ACTIVIDAD ANTIESTAGENA DEL COMPUESTO DE FORMULA (I) Y DESCRIBE LA APLICACION DEL COMPUESTO DE FORMULA (I) PARA LA PRODUCCION DEL MEDICAMENTO. SIENDO: R1 METILO O ETILO; R (AL CUADRADO) HIDROGENO O ALQUIL, ALCOXIMETILO, ALCANOILO, ALCOXICARBONILO CON C1 A 6, O Z-METOXIETILO, Z-HIDROXIETILO, 2 ILO CON UN RESTO ALQUILO DE C1 A 4; R3 VINILO, ALQUILO DE C1 A 6 O UN RESTO FENILO PARA SUSTITUIDO CON -OCH3-, -SCH3-, -N(CH3)2-, -NHCH3, -CN O UN GRUPO ALQUILO DE C1 A 4 Y X OXIGENO, UN GRUPO METOXIAMINO N-OCH3, UN HIDROXIMINO N-OH O UN TIOCETAL CICLICO CON C2 A 3 EN EL ANILLO. THE INVENTION REFERS TO A NEW 11 (BETA) 16 (ALPHA), 17 (ALPHA) FORMULA (I), IT IS A PROCEDURE FOR THE PRODUCTION OF THE FORMULA COMPOUND (I); REVIEWS THE ANTI-STAGE ACTIVITY OF THE FORMULA (I) COMPOUND AND DESCRIBES THE APPLICATION OF THE FORMULA (I) COMPOUND FOR THE PRODUCTION OF THE MEDICINAL PRODUCT. BEING: R1 METHYL OR ETHYL; R (SQUARE) HYDROGEN OR ALKYL, ALCOXYMETHYL, ALCANOYL, ALCOXYCARBONYL WITH C1 TO 6, OR Z-METHOXYTHYL, Z-HYDROXYTHYL, 2 ILO WITH A REST OF ALKYL FROM C1 TO 4; R3 VINYL, RENT FROM C1 TO 6 OR A FENYL REST FOR SUBSTITUTED WITH -OCH3-, -SCH3-, -N (CH3) 2-, -NHCH3, -CN OR A RENT GROUP FROM C1 TO 4 AND X OXYGEN, A METOXYAMINE GROUP N-OCH3, A N-OH HYDROXIMINE OR A CYCLIC THIOCETAL WITH C2 TO 3 IN THE RING.

Новые производные бетулина, получение указанных соединений и их применение

1. Соединение формулы Iили его фармацевтически приемлемая соль или пролекарство, в которойRозначает С-Салканоил, карбоксиалканоил, карбоксиалкеноил, алкоксикарбонилалканоил, алкенилоксикарбонилалканоил, цианоалканоил, гидроксиалканоил, аминокарбонилалканоил, гидроксиаминокарбонилалканоил, моноалкиламинокарбонилалканоил, диалкиламинокарбонилалканоил, гетероарилалканоил, гетероциклилалканоил, гетероциклилкарбонилалканоил, гетероариламинокарбонилалканоил, гетероциклиламинокарбонилалканоил, цианоаминокарбонилалканоил, алкилсульфониламинокарбонилалканоил, арилсульфониламинокарбонилалканоил, сульфоаминокарбонилалканоил, фосфоноаминокарбонилалканоил, фосфоно, сульфо, фосфоноалканоил, сульфоалканоил, алкилсульфонилалканоил или алкилфосфоноалканоил;Rозначает формил, карбоксиалкенил, гетероциклил, гетероарил, -CHSR, -CHSOR, -CHSOR,,,,,,или;Rозначает водород, гидроксил, изопропенил, изопропил, 1'-гидроксиизопропил, 1'-галогенизопропил, 1'-тиоизопропил, 1'-трифторметилизопропил, 2'-гидроксиизопропил, 2'-галогенизопропил, 2'-тиоизопропил, 2'-трифторметилизопропил, 1'-гидроксиэтил, 1'-(алкокси)этил, 1'-(алкоксиалкокси)этил, 1'-(арилалкокси)этил, 1'-(арилкарбонилокси)этил, ацетил, 1'-(гидроксил)-1'-(гидроксиалкил)этил, (2'-оксо)тетрагидрооксазолил, 1',2'-эпоксиизопропил, 2'-галогенизопропенил, 2'-гидроксиизопропенил, 2'-аминоизопропенил, 2'-тиоизопропенил, 3'-галогенизопропенил, 3'-гидроксиизопропенил, 3'-аминоизопропенил, 3'-тиоизопропенил, 1'-алкоксиэтил, 1'-гидроксииминоэтил, 1'-алкоксиимино или;где Y означает -SRили -NRR;Rозначает водород или гидрокси;Rи Rнезависимо означают водород, алкил, алканоил, арилалкил, гетероарилалкил, арилсульфо ÐÎÑÑÈÉÑÊÀß ÔÅÄÅÐÀÖÈß (19) RU (11) 2007 121 729 (13) A (51) ÌÏÊ C07J 3/00 (2006.01) ÔÅÄÅÐÀËÜÍÀß ÑËÓÆÁÀ ÏÎ ÈÍÒÅËËÅÊÒÓÀËÜÍÎÉ ÑÎÁÑÒÂÅÍÍÎÑÒÈ, ÏÀÒÅÍÒÀÌ È ÒÎÂÀÐÍÛÌ ÇÍÀÊÀÌ (12) ÇÀßÂÊÀ ÍÀ ÈÇÎÁÐÅÒÅÍÈÅ (21), (22) Çà âêà: 2007121729/04, 14. ...

신규한 수용성 베툴린 유도체, 이의 제조방법 및 이를 포함하는 주름 개선용 화장료 조성물

본 발명은 신규한 수용성 베툴린 유도체, 이의 제조방법 및 이를 포함하는 주름 개선용 화장료 조성물에 관한 것이다. 본 발명에 따른 수용성 베툴린 유도체는 화학적 안정성 및 용해도가 증가하여, 피부에 자극 없이 콜라겐 합성을 증가시켜 피부재생 및 주름 감소, 피부탄력 증대, 엘라스틴 분해 억제 등 피부노화 억제에 유용하게 사용될 수 있다. 베툴린, 폴리에틸렌글리콜, 유도체, 콜라겐, 주름

Patent JPH0212479B2

制备Drospirenon(6β,7β;15β,16β－二亚甲基－3－氧代－17α孕甾－4－烯－21,17－羰内酯,DRSP)的方法以及该方法的中间产物7α－(3－羟基－1－丙基)－6β,7β;15β,16β－二亚甲基－5β－雄甾烷－3β,5,17β－三醇(ZK92836)和6β,7β,15β,16β－二亚甲基－5β－羟基－3－氧代－17α－雄甾烷－21,17羰内酯

本发明涉及制备Drospirenon(6β,7β;15β,16β－二亚甲基－3－氧代－17α－孕甾－4－烯－21,17－羰内酯,DRSP)的方法以及该方法的中间产物7α－(3－羟基－1－丙基)－6β,7β;15β,16β－二亚甲基－5β－雄甾烷－3β,5,17β－三醇(ZK92836)和6β,7β；15β,16β－二亚甲基－5β－羟基－3－氧代－17α－雄甾烷－21,17－羰内酯(ZK90965)。

TIGOGENIN β-CELLOBIOSIDES

FIELD: organic chemistry. SUBSTANCE: product: tigogenin 6-b-cellobiosides of the general formula (I) (image), where R R 4 CO where R 4 -C 1 -C 4 -alkyl; R 1 and R 2 are separately taken R 1 -R 4 CO where R 4 as indicated above; R 2 a group of the formula (II) (image) or R 1 and R 2 together mean a residue of the formula (III) (image) where R 4 as indicated above. R and R 1 are preferably acetyl, and R 4 methyl. EFFECT: improved method of synthesis. 8$ ЭСУОбОсС ПЧ Го КУЗЗАМ АСЕМСУ ГОК РАТЕМТ$ АМО ТКАОЕМАКК$ (19) 13) ВИ” 2042 688 ' (БТ) ть С° С 074 21000 СЛ 12) АВЗТКАСТ ОЕ 1МУЕМТОМ (21), (22) АррИсаНоп: 4830049/04, 12.06.1990 (30) Рпогйу: 13.06.1989 Ц$ 365588 (46) Рае ог рибИсаНоп: 27.08.1995 (71) АррИсапе: Р\атег К. (0$) (72) пуетог. — Ргейпк Отвоп УгБап[у$] (73) Ргорпеюг: Рарег пк. (05) (54) ПСОСЕММ В-СЕТЕОВОЗЮЕ$ (57) АБзГасЕ: НЕЕО: огдапс спетгу. ЗОВЗТАМСЕ: ргоЧис: Чдодепт 6-6-сейорюзаез о Ше депега! Гогтуа (Г) (таде), мпеге В В.СО мпеге К4-С41-Сла-аку; К ап9 КВ ае зерагаеу 1акеп К1-К4СО \мПпеге К аз паса ароуе; К2 а агоир о Ше югт\а (|1) (таде) ог К. апа В> юдейег теап а гез4ие о! {Ле Гогтша (!!!) (таде) мпеге Кл аз паса ароуе. К апя К.А аге ргаегаыу асеу|, апа К. тешу|. ЕРЕЕСТ: тргоуеа теоа ог зутПез. ОВ 2042688 С1 КО 8$ ЭСУОбОсС ПЧ ГЭ Изобретение относится к новым и благоприятным способам синтеза тигогенин В-целлобиозида и некоторым НОВЫМ промежуточным соединениям, используемым в этих способах. Тигогенин В -целлобиозид представляет собой известное соединение, имеющее пригодной при лечении (гипер) холестеринемии и атеросклероза [1 и 2] Каждый патент раскрывает различный синтез этого соединения из В -целлобиозоктаацетата; первый посредством гептаацетата гликолилбромида, который сопрягают с тигогенином в присутствии карбоната серебра последующим гидролизом; а второ посредством катализируемого четыреххлористым оловом сопряжения октаацетата с тигогенином в метиленхлориде, вновь с последующим гидролизом. В работе Малиноу и др. взаимодействие целлобиозоктаацетата с ...

Process for producing steroid (16 alpha 17 beta)cyclohexane- or naphthalene-21-carboxylic acids or their esters

Steroids having the formula <IMAGE> wherein X is hydrogen or halogen; Y is hydrogen, methyl or fluorine; R4 is chlorine, fluorine or hydroxy and R5 is hydrogen or R4 and R5 together are = O; R2 and R3 are the same or different and are hydrogen, alkyl or aryl or taken together with the double bond to which they are attached form a benzene ring; R6 and R7 are the same or different and are hydrogen, alkyl, alkoxy, formyl, <IMAGE> phenyl or cyano and in addition hydroxy, halogen carboalkoxy and alkylcarbonyl when R2 and R3 are separate with the proviso that when R6 and R7 are different, one of R6 and R7 is hydrogen; R8 is hydrogen or CHR9R10 wherein R9 and R10 are the same or different and are hydrogen or alkyl may be used as intermediates in preparing compounds having antiinflammatory activity. The invention extends to acetals of the 21-aldehydes.

STEROIDSULFAMATE, METHOD FOR THE PRODUCTION THEREOF AND THE APPLICATION THEREOF

Method for treating deodorizer distillate

この発明は種々の油類を脱臭する処理の間に得られた留出物を処理するための方法に関する。さらに特定的には、この発明は種々の油類の脱臭から得られた留出物から脂肪酸類、トコフェロール類及びステロール類を回収するための方法に関する。

The method for preparing steroid derivatives

制备甾族化合物的方法，该甾族化合物用作合成 植物生长调节剂、芸苔属甾族化合物的中间体，它用 通式(4)(式中R 1 为 ，其中R 2 为甲基或乙基，★表明R 1 在甾核上的位置)或通式 (5)(式中R 1 的定义如上)表示。

Triterpenoid compounds with apoptosis-inducing activity on cells

본 발명은 세포사멸 유도작용을 갖는 트리테르펜 화합물에 관한 것으로, 더욱 상세하게는 세포사멸(apoptosis) 유도작용을 가짐으로써 세포들의 이상 증가와 활성화에 관련된 면역계 질환이나 뇌질환 등을 포함하는 다양한 난치성, 만성질환의 예방, 치료 및 치료보조제로서 사용할 수 있는 트리테르펜 화합물과 헐떡이풀로부터 세 가지 트리테르펜 화합물을 분리하는 방법에 관한 것이다. The present invention relates to a triterpene compound having an apoptosis inducing action, and more particularly, having apoptosis inducing action, various intractable properties including an immune system disease or a brain disease related to abnormal increase and activation of cells, The present invention relates to a triterpene compound that can be used as a prophylactic, therapeutic and therapeutic aid for chronic diseases and to separating three triterpene compounds from a pancreas.

Method of obtaining depo-steroid esters

Methods for inhibiting muscle atrophy

在一方面，本发明涉及通过将有效量的熊果酸、其衍生物，或乌苏烷骨架的类似物提供给需要其的受试者来抑制或预防肌萎缩或增加肌肉质量的方法。本摘要意在作为扫描工具以便在具体领域中进行搜索，而无意限制本发明。

Processes for preparation of 9,11-epoxy steroids and intermediates useful therein

다중 신규 반응식, 신규 공정 단계 및 신규 중간체가 에폭시멕스레논 및 화학식 I Multiple novel reaction schemes, new process steps and new intermediates may be used for (화학식 I) Formula I (식에서, -A-A-는 -CHR 4 -CHR 5 - 또는 -CR 4 =CR 5 - 기를 나타내고, (Wherein -AA- represents a -CHR 4 -CHR 5 -or -CR 4 = CR 5 -group, R 3 , R 4 및 R 5 는 독립적으로 수소, 할로, 히드록시, 저급 알킬, 저급 알콕시, 히드록시알킬, 알콕시알킬, 히드록시 카르보닐, 시아노 및 아릴옥시 기로 이루어진 군으로부터 선택되고; R 3 , R 4 and R 5 are independently selected from the group consisting of hydrogen, halo, hydroxy, lower alkyl, lower alkoxy, hydroxyalkyl, alkoxyalkyl, hydroxy carbonyl, cyano and aryloxy groups; R 1 은 알파-배향의 저급 알콕시카르보닐 또는 히드록시알킬 라디칼을 나타내고; R 1 represents an alpha-oriented lower alkoxycarbonyl or hydroxyalkyl radical; -B-B- 는 -CHR 6 -CHR 7 - 기 또는 알파- 또는 베타- 배향의 기 -BB- is a -CHR 6 -CHR 7 -group or an alpha- or beta-oriented group (화학식 III) Formula III (식에서, R 6 및 R 7 은 독립적으로 수소, 할로, 저급 알콕시, 아실, 히드록시알킬, 알콕시알킬, 히드록시카르보닐, 알킬, 알콕시카르보닐, 아실옥시알킬, 시아노 및 아릴옥시로부터 선택된다)를 나타내고; Wherein R 6 and R 7 are independently selected from hydrogen, halo, lower alkoxy, acyl, hydroxyalkyl, alkoxyalkyl, hydroxycarbonyl, alkyl, alkoxycarbonyl, acyloxyalkyl, cyano and aryloxy ); R 8 및 R 9 는 독립적으로 수소, 히드록시, 할로, 저급 알콕시, 아실, 히드록시알킬, 알콕시알킬, 히드록시카르보닐, 알킬, 알콕시카르보닐, 아실옥시알킬, 시아노 및 아릴옥시 기로 이루어진 군으로부터 선택되거나, 또는 R 8 및 R 9 는 함께 카르보고리형 또는 헤테로고리형 고리 구조를 구성하거나, 또는 R 6 또는 R 7 과 함께 5-원 고리형 D 고리에 융합된 카르보고리형 또는 헤테로고리형 고리 구조를 구성한다)의 다른 화합물의 합성을 위해 제공된다. R 8 and R 9 are independently a group consisting of hydrogen, hydroxy, halo, lower alkoxy, acyl, hydroxyalkyl, alkoxyalkyl, hydroxycarbonyl, alkyl, alkoxycarbonyl, acyloxyalkyl, cyano and aryloxy groups Or R 8 and R 9 together form a carbocyclic or heterocyclic ring structure, or together with R 6 or R 7 , a carbocyclic or heterocyclic type fused to a 5-membered cyclic D ring Constituting a ring structure).

Method of producing betulin

FIELD: technological processes. SUBSTANCE: invention relates to a method of producing betulin from birch bark for use in medicine and perfumery, involving UHF extraction of birch bark with propylene glycol at ratio of extractant : bark of 30:1, power of 300 W, duration of 10 minutes, followed by crystallization. EFFECT: method provides higher efficiency of the process of producing betulin via reduction of technological operations, shorter duration of extraction of the end product, avoiding use of highly flammable alcohols. 1 cl, 2 tbl РОССИЙСКАЯ ФЕДЕРАЦИЯ ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) (19) RU (11) (13) 2 710 374 C1 (51) МПК A61K 41/00 (2006.01) A61K 36/185 (2006.01) A61K 129/00 (2006.01) C07J 53/00 (2006.01) C07J 63/00 (2006.01) B01D 11/02 (2006.01) B01D 9/02 (2006.01) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ (52) СПК A61K 41/00 (2019.08); A61K 36/185 (2019.08); A61K 2236/00 (2019.08); C07J 53/00 (2019.08); C07J 63/00 (2019.08); B01D 11/02 (2019.08); B01D 9/02 (2019.08) (21)(22) Заявка: 2019116770, 30.05.2019 30.05.2019 Дата регистрации: 26.12.2019 (45) Опубликовано: 26.12.2019 Бюл. № 36 2 7 1 0 3 7 4 R U (54) Способ получения бетулина (57) Реферат: Изобретение относится к способу получения бетулина из березовой коры для использования в медицине и парфюмерии, включающему СВЧ экстракцию коры березы пропиленгликолем при соотношении экстрагент:кора 30:1, мощностью 300 Вт, продолжительностью 10 мин, с последующей кристаллизацией. Способ Стр.: 1 (56) Список документов, цитированных в отчете о поиске: SU 382657 A1, 23.05.1973. RU 2501805 C1, 20.12.2013. RU 2439093 C1, 10.01.2012. RU 2523545 C1, 20.07.2014. КОПТЕЛОВА Е.Н. и др. Извлечение экстрактивных веществ и бетулина из бересты при воздействии СВЧполя//Химия растительного сырья. - 2013. - N 4. - С.159-164. обеспечивает повышение эффективности процесса получения бетулина за счет сокращения технологических операций, снижения продолжительности выделения целевого продукта, исключения использования ...

New 19-norsteroids containing phenoxyalkylsulfoneamide or phenoxyalkylsulfonylcarbamide chain at position 11-beta, method and intermediate compounds of their synthesis, and pharmaceutical composition containing thereof

Изобретение относится к новым 19-норстероидам, к способу их получения, к фармацевтической композиции на их основе и к промежуточным соединениям синтеза.

N'-{n-[3-oxo-lupan-28-oyl]-9-aminononanoyl}-3-amino-3-phenylpropionic acid and its salts as antiviral and immunostimulating agents

FIELD: organic chemistry of natural compounds. SUBSTANCE: invention relates to novel compounds, namely, to N'-{N-[3-oxo-lupan-28-oyl]-9-aminononanoyl}-3-amino-3-phenylpropionic acid and its salts of the formula (I) given in the invention description. This compound shows antiviral activity, in particular, anti-HIV activity, and immunostimulating activity. Compounds of the formula (I) are nontoxic and can be obtained from betulin isolated from birch bark as available raw with the high yield. EFFECT: valuable medicinal properties of compound. 4 tbl, 9 ex ÐÎÑÑÈÉÑÊÀß ÔÅÄÅÐÀÖÈß RU (19) (11) 2 317 996 (13) C1 (51) ÌÏÊ C07K C07J C07J A61K A61P A61P ÔÅÄÅÐÀËÜÍÀß ÑËÓÆÁÀ ÏÎ ÈÍÒÅËËÅÊÒÓÀËÜÍÎÉ ÑÎÁÑÒÂÅÍÍÎÑÒÈ, ÏÀÒÅÍÒÀÌ È ÒÎÂÀÐÍÛÌ ÇÍÀÊÀÌ (12) 5/062 63/00 53/00 38/05 31/18 37/04 (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) ÎÏÈÑÀÍÈÅ ÈÇÎÁÐÅÒÅÍÈß Ê ÏÀÒÅÍÒÓ (21), (22) Çà âêà: 2006138356/04, 30.10.2006 (24) Äàòà íà÷àëà îòñ÷åòà ñðîêà äåéñòâè ïàòåíòà: 30.10.2006 (45) Îïóáëèêîâàíî: 27.02.2008 Áþë. ¹ 6 (73) Ïàòåíòîîáëàäàòåëü(è): Èíñòèòóò íåôòåõèìèè è êàòàëèçà ÐÀÍ (RU) (54) N'-{N-[3-ÎÊÑÎ-ËÓÏÀÍ-28-ÎÈË]-9-ÀÌÈÍÎÍÎÍÀÍÎÈË}-3-ÀÌÈÍÎ-3-ÔÅÍÈË-ÏÐÎÏÈÎÍÎÂÀß îáëàäàþùèì ïðîòèâîâèðóñíîé (àíòè-ÂÈ×) è èììóíîñòèìóëèðóþùåé àêòèâíîñòüþ. Ñîåäèíåíè ôîðìóëû I íåòîêñè÷íû, ïîëó÷àþòñ ñ âûñîêèì âûõîäîì èç äîñòóïíîãî ñûðü - áåòóëèíà, âûäåë åìîãî èç áåðåçîâîé êîðû. 4 òàáë. R U 2 3 1 7 9 9 6 C 1 C 1 ÊÈÑËÎÒÀ È ÅÅ ÑÎËÈ ÊÀÊ ÏÐÎÒÈÂÎÂÈÐÓÑÍÛÅ È ÈÌÌÓÍÎÑÒÈÌÓËÈÐÓÞÙÈÅ ÀÃÅÍÒÛ (57) Ðåôåðàò: Èçîáðåòåíèå îòíîñèòñ ê íîâûì õèìè÷åñêèì ñîåäèíåíè ì, êîíêðåòíî ê N'-{N-[3-îêñî-ëóïàí-28îèë]-9-àìèíîíîíàíîèë}-3-àìèíî-3-ôåíèëïðîïèîíîâîé êèñëîòå è åå ñîë ì, ôîðìóëà I, Ñòðàíèöà: 1 RU 2 3 1 7 9 9 6 Àäðåñ äë ïåðåïèñêè: 450075, ã.Óôà, ïð-êò Îêò áð , 141, ÈÍÊ ÐÀÍ, ïàòåíòíà ãðóïïà R U (56) Ñïèñîê äîêóìåíòîâ, öèòèðîâàííûõ â îò÷åòå î ïîèñêå: RU 2211843 C1, 10.09.2003. US 5468888 A, 21.11.1995. US 6369109 B1, 09.04.2002. (72) Àâòîð(û): Äæåìèëåâ Óñåèí Ìåìåòîâè÷ (RU), Òîëñòèêîâ Ãåíðèõ Àëåêñàíäðîâè÷ (RU), Ïîêðîâñêèé Àíäðåé Ãåîðãèåâè÷ (RU), ...

Derivatives of estra-1,3,5(10)-triene, method of their synthesis, pharmaceutical composition

FIELD: organic chemistry, pharmacy. SUBSTANCE: invention describes new estra-1,3,5(10)- -triene sulfamates of the general formula (I) where R means the group R 1 R 2 N where R 1 and R 2 means independently hydrogen atom or C 1 -C 5 -alkyl group or in common with nitrogen atom form polymethyleneimino-group containing 4-6 carbon atoms or morpholino-group; R 3 means hydrogen atom or C 1 -C 5 -alkyl group; R 4 means hydrogen atom, hydroxyl group, esterified hydroxyl group, halogenalkyl group containing 1-5 carbon atoms or alkoxy-group contaning 1-5 carbon atoms; R 5 and R 6 each means hydrogen atom or in common means methylene group; R 7 , R 8 and R 9 mean independently each of other hydrogen atom or hydroxyl group and ring B can has one or two double bonds, or R 8 means alkynyl residue containing up to 5 carbon atoms, or R 8 and R 9 in common can mean oxygen atom in the case when at least one of residues R 3 , R 4 , R 5 , R 6 or R 7 is not hydrogen atom. Compounds can be used for the hormonal contraception and substituent therapy of climacteric hormone (HRT) and for treatment of patients with gynecological and andrological illnesses. Compounds show low estrogenicite effect on the liver. Invention describes also methods of synthesis of compounds and pharmaceutical compositions preparing. EFFECT: improved method of synthesis and preparing, enhanced hormonal effectiveness. 4 cl, 1 tbl, 26 ex сззе* гс пы Го РОССИЙСКОЕ АГЕНТСТВО ПО ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ (19) ВИ “” 2 139 885 ' (51) МПК 13) Сл С 07 + 1/00, 31/00, А 61 К 31/565 12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ РОССИЙСКОЙ ФЕДЕРАЦИИ (21), (22) Заявка: 97104003/04, 03.07.1995 (24) Дата начала действия патента: 03.07.1995 (30) Приоритет: 09.08.1994 ОЕ Р 4429397.6 (46) Дата публикации: 20.10.1999 (56) Ссылки: 4. Меа. Свет. - (1994), 37, 219-221. /. Епаосппо|. - 1988, 118. Тринус Ф.П. Фармакотерапевтический справочник.-Киев: 1989, с. 265-267. (86) Заявка РСТ: ОЕ 95/00877 (03.07.95) (87) Публикация РСТ: М/О 96/05216 (22.02.96) ...

Pharmaceutical compositions containing derivatives of estra-1,3,5(10)-triene

Изобретение относится к медицине. Фармацевтические композиции, содержащие в качестве активных ингредиентов производные эстра-1,3,5(10)-триена, несущие в их С3-положении группу общей формулы R-SO 2 -O-, где R обозначает группу R 1 R 2 N, в которой R 1 и R 2 не зависят друг от друга и обозначают атом водорода, С 1 -С 5 алкильный радикал или вместе с атомом азота обозначают полиметилениминогруппу, содержащую 4-6 атомов углерода, или морфолиногруппу, предназначены для гормональной контрацепции и для гормонзаместительной терапии (HRT). Они проявляют низкую эстрогенность в отношении печени. 2 з.п. ф-лы, 10 табл. (19) (13) ВИ `” 2 179 442” С2 5 МК’ д 61 К 31/56, А 61 Р 5/00, 5/18, 5/24, 35/00 Стб Ас ПЧ с» РОССИЙСКОЕ АГЕНТСТВО ПО ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ (12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ РОССИЙСКОЙ ФЕДЕРАЦИИ (21), (22) Заявка: 97104120/14, 03.07.1995 (24) Дата начала действия патента: 03.07.1995 (30) Приоритет: 09.08.1994 ОЕ Р 4429398.4 (43) Дата публикации заявки: 20.04.1999 (46) Дата публикации: 20.02.2002 (56) Ссылки: 1. ЕК 2133484 АЛ, 01.02.1972. 2. 20 114806 А, 20.08.1975. 3. ОЕ 207447 А, 29.02.1984. 4. ЗСН\УАКХ $. еа!. Зего!а$. 15: ЗуНопуюху АепуаНуе$ оГ езгодеп$', РБагтале, 30, № 1: 1975, р. 17-21. 5. $9 1789216 АЛ, 23.01.1993. (85) Дата перевода заявки РСТ на национальную фазу: 09.03.1997 (86) Заявка РСТ: ОЕ 95/00879 (03.07.1995) (87) Публикация РСТ: М/О 96/05217 (22.02.1996) (98) Адрес для переписки: 101000, Москва, пер. Малый Златоустинский 10, кв.15, "ЕВРОМАРКПАТ", Веселицкой И.А. (71) Заявитель: ИЕНАФАРМ ГМБХ УНД КО. КГ (ОЕ) (72) Изобретатель: ЭЛЬГЕР Вальтер (0Е), ШВАРЦ Зигфрид (ОЕ), ЗИМАН Ханс-Иоахим (ОЕ), РЕДДЕРСЕН Гудрун (ОЕ), ШНАЙДЕР Биргитт (ОЕ) (73) Патентообладатель: ИЕНАФАРМ ГМБХ УНД КО. КГ (ОЕ) (74) Патентный поверенный: Веселицкая Ирина Александровна (54) ФАРМАЦЕВТИЧЕСКИЕ КОМПОЗИЦИИ, СОДЕРЖАЩИЕ ПРОИЗВОДНЫЕ ЭСТРА-1,3,5(10)-ГРИЕНА (57) Изобретение относится к медицине. Фармацевтические композиции, содержащие в качестве активных ингредиентов ...

New stigmasterol derivatives or pharmaceutically acceptable salts thereof, process for the preparation thereof and composition comprising the same for inhibiting obesity or for preventing and treating hyperlipidemia

본 발명은 신규한 스티그마스테롤 유도체 또는 이의 약학적으로 허용가능한 염, 이의 제조방법, 및 이를 포함하는 비만 억제 또는 고지혈증 예방 및 치료용 조성물에 관한 것이다. 본 발명에 따른 스티그마스테롤 유도체는 혈액 내에서 중성지방, 총 콜레스테롤 및 LDL-콜레스테롤의 함량을 낮추고, HDL-콜레스테롤의 함량을 증가시키며, 체중증가를 억제하는 효과가 우수하다. 따라서, 본 발명에 따른 스티그마스테롤 유도체는 비만 억제 또는 고지혈증 예방 및 치료에 유용한 의약품 및 건강식품으로 사용될 수 있다. The present invention relates to a novel stigmasterol derivative or a pharmaceutically acceptable salt thereof, a preparation method thereof, and a composition for preventing and treating obesity or preventing hyperlipidemia comprising the same. The stigmasterol derivative according to the present invention is excellent in the effect of lowering the content of triglycerides, total cholesterol and LDL-cholesterol in the blood, increasing the content of HDL-cholesterol, and inhibiting weight gain. Therefore, the stigmasterol derivatives according to the present invention can be used as medicines and health foods useful for inhibiting obesity or preventing and treating hyperlipidemia.

Application of triterpenes and dimer compounds thereof in preparation of drugs for treating diseases mediated by protein tyrosine phosphatase 1B

本申请公开一种三萜及其二聚体类化合物在制备治疗蛋白酪氨酸磷酸酶1B所介导疾病药物中的用途，本申请保护性地采集少许华东黄杉植物样品(其枝叶，易再生)，分离出7种三萜及其二聚体类化合物，然后对上述分离得到的三萜及其二聚体类化合物进行了蛋白酪氨酸磷酸酶1B(PTP1B)抑制活性实验，实验结果表明这类化合物均具有显著的抑制活性，可用于制成预防、延缓或治疗由PTP1B介导的疾病，特别是II型糖尿病和肥胖症的药物或是作为该类药物的先导化合物。

DERIVATIVE 17β-CYANO-18A-HOMO-19-NOR-ANDROST-4-ENA, ITS APPLICATION AND MEDICINES CONTAINING A DERIVATIVE

1. Производное 17β-циано-18а-гомо-19-нор-андрост-4-ена, имеющее общую химическую формулу 1 ! ! где Z выбран из группы, включающей О, два атома водорода, NOR и NNHSO2R, в котором R представляет собой водород или С1-С4-алкил, ! R4 представляет собой водород или галоген, ! кроме того каждый: ! R6a, R6b вместе образуют метилен или 1,2-этандиил или R6a представляет собой водород и R6b выбран из группы, включающей водород, метил и гидроксиметилен и ! R7 выбран из группы, включающей водород, C1-C4-алкил, C2-С3-алкенил и циклопропил, ! или: ! R6a представляет собой водород и R6b и R7 также образуют метилен или упускаются с образованием двойной связи между С6 и С7, ! R9, R10 представляют собой водород или упускаются с образованием двойной связи между С9 и С10, ! R15, R16 представляют собой водород или вместе образуют метилен, ! R17 выбран из группы, включающей водород, С1-С4-алкил и аллил, ! по крайней мере один из заместителей R4, R6a, R6b, R7, R15, R16, R17 не являются водородом или R6b и R7 упускаются с образованием двойной связи между С6 и С7 или упускаются с образованием двойной связи между С1 и С2, ! и его сольваты, гидраты, стереоизомеры, диастереомеры, энантиомеры и соли. ! 2. Производное 17β-циано-18а-гомо-19-нор-андрост-4-ена по п.1, отличающееся тем, что R15 и R16 вместе образуют метилен. ! 3. Производное 17β-циано-18а-гомо-19-нор-андрост-4-ена по п.1, отличающееся тем, что Z выбран из группы, включающей О, NOH и NNHSO2H. ! 4. Производное 17β-циано-18а-гомо-19-нор-андрост-4-ена по п.1, отличающееся тем, что Z представляет собой О. ! 5. Производное 17β-циано-18а-гомо-19-нор-андрост-4-ена по п.1, отличающееся тем, что R4 представляет собой водород или хлор. ! 6. Производное 17β-циано-18а-гомо-19-нор-андрост-4-ена по п.1, отличающееся тем, чт� РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) 2010 100 334 (13) A (51) МПК C07J 41/00 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ, ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ (12) ЗАЯВКА НА ИЗОБРЕТЕНИЕ (21)(22) Заявка: 2010100334/04, 04. ...

Immunomodulatory and antiviral agent based on (2-((coumarin-7-yl)oxy)ethyl) 3-hydroxy-20(29)-lupen-28-oate

FIELD: medicine. SUBSTANCE: invention refers to medicine and chemical-pharmaceutical industry and concerns a new immunomodulatory and antiviral agent based on a hybrid molecule of triterpenoid-coumarin derivatives, namely (2-((coumarin-7-yl)oxy)ethyl) 3-hydroxy 20(29)-lupen-28-oate. EFFECT: declared compound has immunomodulatory properties, having an effect on activation of the humoral response, and expressed antiviral activity against influenza virus A/California/07/09 (H1N1)pdm09 in Balb/c mice in therapeutic and prophylactic mode of application in doses of 10 mg/kg, can be used in medical practice in treating and preventing viral infections. 1 cl, 6 dwg, 2 tbl, 3 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2 686 743 C1 (51) МПК C07J 53/00 (2006.01) A61K 31/56 (2006.01) A61P 37/02 (2006.01) A61P 31/12 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ (52) СПК C07J 53/00 (2019.02); A61K 31/56 (2019.02); A61P 37/02 (2019.02); A61P 31/12 (2019.02) (21) (22) Заявка: 2018138717, 01.11.2018 (24) Дата начала отсчета срока действия патента: 01.11.2018 30.04.2019 (45) Опубликовано: 30.04.2019 Бюл. № 13 (73) Патентообладатель(и): ОБЩЕСТВО С ОГРАНИЧЕННОЙ ОТВЕТСТВЕННОСТЬЮ "СИР" (RU) Адрес для переписки: 198328, Санкт-Петербург, ул. Маршала Захарова, 14, корп. 2, кв. 338, Абышев Азад Зияд оглы (56) Список документов, цитированных в отчете о поиске: Colman PM. "A novel approach to C 1 2 6 8 6 7 4 3 R U (54) ИММУНОМОДУЛИРУЮЩЕЕ И ПРОТИВОВИРУСНОЕ СРЕДСТВО НА ОСНОВЕ (2((КУМАРИН-7-ИЛ)ОКСИ)ЭТИЛ) 3-ГИДРОКСИ-20(29)-ЛУПЕН-28-ОАТА (57) Реферат: Изобретение относится к медицине и химикоответа, и выраженной противовирусной фармацевтической промышленности и касается активностью в отношении вируса гриппа A/ нового иммуномодулирующего и California/07/09 (H1N1)pdm09 у мышей Balb/c при противовирусного средства на основе гибридной лечебно-профилактическом режиме применения молекулы производных тритерпеноида-кумарина, в дозах 10 мг/кг, может найти ...

Method of producing 3-acetate-28 phthalate of betulinol

FIELD: pharmaceutics. SUBSTANCE: invention relates to chemical-pharmaceutical industry and relates to a method of producing 3-acetate-28-phthalate betulinol – a biologically active substance exhibiting hepatoprotective, antifungal and anti-cystic activity. In the method described, 3-acetate-28-phthalate of betulinol is obtained by fusion of 3-acetate of betulinol with phthalic acid at ratio of reagents of 1.0:1.5 at temperature of 180–200 °C for 2–3 minutes. EFFECT: simple process of producing betulinol 3-acetate-28-phthalate, high economic efficiency thereof by cutting the duration of the process and avoiding the use of expensive and toxic reagents. 1 cl, 2 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2 729 621 C1 (51) МПК C07J 53/00 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ (52) СПК C07J 53/00 (2020.02) (21)(22) Заявка: 2020110500, 11.03.2020 (24) Дата начала отсчета срока действия патента: Дата регистрации: 11.08.2020 (45) Опубликовано: 11.08.2020 Бюл. № 23 2 7 2 9 6 2 1 R U (56) Список документов, цитированных в отчете о поиске: RU 2614149 C1 (Федеральное государственное бюджетное учреждение науки Институт химии и химической технологии Сибирского отделения Российской академии наук (ИХХТ СО РАН), 23.03.2017. Флехтер О.Б., Синтез эфиров тритерпеноидов группы лупана и их гепатопротекторная активность. Биоорганическая химия, 2000, т. 26(3), 215-223. (54) СПОСОБ ПОЛУЧЕНИЯ 3-АЦЕТАТА-28 ФТАЛАТА БЕТУЛИНОЛА (57) Реферат: Изобретение относится к химикосоотношении реагентов 1,0:1,5 при температуре фармацевтической промышленности и относится 180-200°С в течение 2-3 минут. Технический к способу получения 3-ацетата-28-фталата результат - упрощение процесса получения 3бетулинола - биологически активного вещества, ацетата-28-фталата бетулинола, повышение его проявляющего гепатопротекторную, экономической эффективности за счет резкого антигрибковую и антидрожжевую активность. В сокращения продолжительности процесса и ...

The method of obtaining derivatives pregnana

18-METHYL-19-NORANDROST-4-EN-17, 17-SPIROESTER (18-METHYL-19-NOR-20-SPIROX-4-EN-3-OH) AND PHARMACEUTICALS THAT CONTAIN

1. 18-Метил-15β,16β-метилен-19-нор-20-спирокс-4-ен-3-оны общей формулы I ! ! в которой Z представляет собой атом кислорода, два атома водорода, группу =NOR или =NNHSO2R, где R представляет собой атом водорода или прямоцепочечную или разветвленную алкильную группу, содержащую от 1 до 4 или от 3 до 4 атомов углерода, ! R4 представляет собой атом водорода, атом галогена или трифторметильную группу, ! R6 и/или R7 могут иметь α или β конфигурацию, и R6 и R7 независимо друг от друга представляют собой атом водорода или прямоцепочечную или разветвленную алкильную группу, содержащую от 1 до 4 или от 3 до 4 атомов углерода, или прямоцепочечную или разветвленную алкенильную группу, содержащую от 2 до 4 или от 3 до 4 атомов углерода, или насыщенную циклоалкильную группу, содержащую от 3 до 5 атомов углерода, или вместе представляют собой метиленовую группу или двойную связь. ! 2. 18-Метил-15β,16β-метилен-19-нор-20-спирокс-4-ен-3-оны общей формулы I, отличающиеся тем, что Z представляет собой атом кислорода. ! 3. 18-Метил-15β,16β-метилен-19-нор-20-спирокс-4-ен-3-оны общей формулы I, отличающиеся тем, что R4 представляет собой атом водорода, метильную группу или атом хлора. ! 4. 18-Метил-15β,16β-метилен-19-нор-20-спирокс-4-ен-3-оны общей формулы I, отличающиеся тем, что R6 и R7 вместе представляют собой 5α,6α- или 5β,6β-метиленовую группу или дополнительную связь. ! 5. 18-Метил-15β,16β-метилен-19-нор-20-спирокс-4-ен-3-оны общей формулы I, отличающиеся тем, что R7 представляет собой α-или β- метил-, этил-, пропил- или этенильную группу или α- или β- циклопропильный остаток. ! 6. Соединения по п.1, в частности ! 18-метил-15β,16β-метилен-19-нор-20-спирокса-4,6-диен-3-он ! 18-метил-15β,16β-метилен-19-нор-20-спирокс-4-ен-3-он ! 18-метил-6β,7β,15β РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) 2009 102 772 (13) A (51) МПК C07J 53/00 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ, ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ (12) ЗАЯВКА НА ИЗОБРЕТЕНИЕ (21), (22) Заявка: 2009102772/04, 29.06.2007 (71) ...

19,11-crosslinked 4-estrene having gestagen action

Method of producing betulin

FIELD: technological processes. SUBSTANCE: invention relates to a method of producing betulin, including extraction with ethyl alcohol prepared raw materials at elevated temperature and pressure, with a temperature of 90–150 ºC, pressure – not less than 10 atm, consumption of ethyl alcohol is 5–25 kg/kg of raw materials, extraction time is 20 minutes – 4 hours. EFFECT: new method of producing betulin, which allows to separate betulin from birchbark with a high yield and purity, which does not produce toxic or difficult to dispose waste and by-products. 1 cl, 1 tbl РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2 668 976 C1 (51) МПК C07J 53/00 (2006.01) C07J 63/00 (2006.01) C07J 75/00 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ (52) СПК C07J 53/00 (2006.01); C07J 63/008 (2006.01); C07J 75/00 (2006.01) (21)(22) Заявка: 2017142786, 07.12.2017 (24) Дата начала отсчета срока действия патента: Дата регистрации: 05.10.2018 (45) Опубликовано: 05.10.2018 Бюл. № 28 Адрес для переписки: 163002, г. Архангельск, наб. Северной Двины, 17, Северный (Арктический) федеральный университет имени М.В. Ломоносова (73) Патентообладатель(и): Федеральное государственное автономное образовательное учреждение высшего образования "Северный (Арктический) федеральный университет имени М.В. Ломоносова" (RU) (56) Список документов, цитированных в отчете о поиске: RU 2172178 C1, 20.08.2001. RU 2 6 6 8 9 7 6 R U (54) Способ получения бетулина (57) Реферат: Изобретение относится к способу получения бетулина, включающему экстракцию этиловым спиртом подготовленного сырья при повышенных температуре и давлении, при этом температура составляет 90–150ºС, давление - не менее 10 атм, расход этилового спирта составляет 5-25 кг/кг сырья, продолжительность экстракции Стр.: 1 C 1 C 1 2131882 C1, 20.06.1999. RU 2340624 C1, 10.12.2008. RU 2623220 C1, 23.06.2017. 2 6 6 8 9 7 6 Приоритет(ы): (22) Дата подачи заявки: 07.12.2017 R U 07.12.2017 (72) Автор(ы): Ивахнов Артем ...

enrichment of triterpene esters

트리테르펜 에스테르의 새로운 농축 방법이 제공되며, 상기 방법은 다음의 단계들을 포함한다: a) 증류되지 않은 식물성 오일 및/또는 증류되지 않은 식물성 지방을 포함하는 혼합물을 제공하는 단계로서, 상기 혼합물은 트리테르펜 에스테르를 더 포함하는, 단계; b) 저급 알코올을 사용하여 온화한 에스테르교환 반응을 수행하는 단계; 및 c) 탈취(deodorisation), 물리적 정제(physical refining), 증발(evaporation) 또는 증류(distillation)에 의하여 저급 알코올 에스테르를 제거하고, 트리테르펜 에스테르가 풍부한 잔류 분획을 회수하는 단계. 상기 방법으로 농축된 트리테르펜 에스테르 및 이의 용도 또한 제공된다. 하나의 이점은, 본 발명의 방법이 TTP 에스테르들의 더욱 높은 농도를 달성하기 위한, 더욱 경제적으로 실행가능한 방법이라는 것이다. TTP 에스테르들의 자연 그대로의 분포를 충실하게 유지할 수 있는 가능성, 그러면서도 한편으로는 또한, 천연 상태 농도의 신남산 및 아세트산의 TTP 에스테르들을 고농도의 긴 사슬 지방산의 TTP 에스테르들로 대체할 수 있는 가능성, 둘 다가 제공된다. A novel process for the concentration of triterpene esters is provided, said process comprising the steps of: a) providing a mixture comprising undistilled vegetable oil and/or undistilled vegetable fat, said mixture comprising the steps of: further comprising a terpene ester; b) carrying out a mild transesterification reaction using a lower alcohol; and c) removing the lower alcohol esters by deodorisation, physical refining, evaporation or distillation and recovering the residual fraction rich in triterpene esters. Also provided are triterpene esters concentrated by the above method and uses thereof. One advantage is that the process of the present invention is a more economically viable method for achieving higher concentrations of TTP esters. The possibility of faithfully maintaining the pristine distribution of TTP esters, but also the possibility of replacing the TTP esters of cinnamic acid and acetic acid in natural concentrations with TTP esters of long-chain fatty acids in high concentrations; everything is provided

11β-substituted 16α, 17α-methylene-estradi-4,9-dien-3-one

Triterpene-containing oleogel-forming agent, triterpene-containing oleogel and method for producing triterpene-containing oleogel

FIELD: medicine. ^ SUBSTANCE: invention refers to medicine and chemical-pharmaceutical industry, particularly to an oleogel-forming agent which contains at least one highly dispersed triterpene. The invention also refers to an oleogel which comprises a nonpolar liquid - oil in an amount ranging from 80 wt % to 99 wt % of total weight of the gel and an oleogel-forming agent containing a highly dispersed triterpene in an amount ranging from 1 wt % to 20 wt % of total weight of the gel. ^ EFFECT: invention also refers to a method for producing an oleogel. ^ 52 cl, 1 dwg, 2 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) 2 430 717 (13) C2 (51) МПК A61K 9/06 (2006.01) A61K 9/10 (2006.01) A61K 31/01 (2006.01) A61K 47/06 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ, ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ (12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ (21)(22) Заявка: 2007102084/15, 21.06.2005 (24) Дата начала отсчета срока действия патента: 21.06.2005 (73) Патентообладатель(и): БИРКЕН ГМБХ (DE) R U Приоритет(ы): (30) Конвенционный приоритет: 22.06.2004 DE 102004030044.5 (72) Автор(ы): ШЕФФЛЕР Армин (DE) (43) Дата публикации заявки: 27.07.2008 Бюл. № 21 2 4 3 0 7 1 7 (45) Опубликовано: 10.10.2011 Бюл. № 28 2 4 3 0 7 1 7 R U (85) Дата начала рассмотрения заявки PCT на национальной фазе: 22.01.2007 C 2 C 2 (56) Список документов, цитированных в отчете о поиске: "Development and Evaluation of Antiinflammatory Oleogels of Bosewellia serrata (GUGUL) and Curcuma longa (TURMERIC)" Shrikhande B.K. et al., Indian Drugs 38 (12) December 2001, p 613-616. ЕР 1410790 A1, 21.04.2004. US 2003/0087789 A1, 08.05.2003. (86) Заявка PCT: EP 2005/006710 (21.06.2005) (87) Публикация заявки РСТ: WO 2005/123037 (29.12.2005) Адрес для переписки: 129090, Москва, ул. Б.Спасская, 25, стр.3, ООО "Юридическая фирма Городисский и Партнеры", пат.пов. Е.Е.Назиной (54) СОДЕРЖАЩИЙ ТРИТЕРПЕН АГЕНТ ОБРАЗОВАНИЯ ОЛЕОГЕЛЯ, СОДЕРЖАЩИЙ ТРИТЕРПЕН ОЛЕОГЕЛЬ, И СПОСОБ ПОЛУЧЕНИЯ СОДЕРЖАЩЕГО ТРИТЕРПЕН ОЛЕОГЕЛЯ (57) Реферат: Изобретение ...

Method of obtaining 11 b-fluoroandrestene

Method of preparing 6-beta-7-beta-15,16-dimethylene-1,4-androstadien-3-ones

Cationic cholesteryl derivatives containing cyclic polar groups

The present invention discloses compounds which are cationic cholesteryl derivatives having a nitrogen-containing ring structure as their polar head group. These compounds are useful for delivering biologically active substances to cells and for transfecting nucleic acids into cells.

New compound separated from fruit of japanese styrax, separating method for new compound, antifungal material containing thereof

본 발명은 때죽나무 열매로부터 분리하여 하기 구조식(1)의 신규한 화합물, 이 화합물의 분리방법 및 동 화합물을 포함하는 항진균제에 관한 것이다. The present invention relates to a novel compound of the following structural formula (1), a method for isolating the compound, and an antifungal agent comprising the same compound, isolated from the deadwood fruit. 구조식(1) Structural Formula (1) 상기 구조식(1)에서 R 1 , R 2 , R 3 , R 4 는 각각 다음과 같다. In the formula (1), R 1 , R 2 , R 3 , R 4 are as follows. , , , , 본 발명은 때죽나무 열매로부터 항진균 활성을 가지는 신규한 화합물을 규명하고, 이러한 항진균 활성을 가지는 신규한 화합물을 포함하는 항진균제의 제공을 목적으로 한다.  An object of the present invention is to identify a novel compound having antifungal activity from the deadwood fruit and to provide an antifungal agent comprising the novel compound having such antifungal activity.

Method of obtaining betulin

FIELD: chemistry. SUBSTANCE: method of obtaining betulin from birch bark comprising a preliminary activation of birch bark and betulin extraction of 86% ethanol solution, wherein the activation is carried out by ultrasonic treatment with intensity in the range of 10-15 W/cm 2 at a frequency of not less than 20-22 kHz at a temperature of 40°C for a period of 5-25 min and subsequent extraction is intensified by the ultrasonic impact reduced to 5 W/cm 2 of the fluctuation intensity at a temperature not less than 40°C for a time determined by the initial particle size of the birch bark. EFFECT: reducing the duration of the betulin obtaining process. 1 dwg, 1 tbl, 2 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2 640 587 C1 (51) МПК C07J 53/00 (2006.01) C07J 63/00 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ (52) СПК C07J 53/00 (2006.01); C07J 63/008 (2006.01) (21)(22) Заявка: 2017104346, 09.02.2017 (24) Дата начала отсчета срока действия патента: Дата регистрации: 10.01.2018 (45) Опубликовано: 10.01.2018 Бюл. № 1 Адрес для переписки: 659305, Алтайский край, г. Бийск, ул. Героя Советского Союза Трофимова, д. 27, ФГБОУ ВО "Алтайский государственный технический университет им. И.И.Ползунова, Бийский технологический институт (филиал) (56) Список документов, цитированных в отчете о поиске: RU 2264411 C1, 20.11.2005. RU C 1 2501805 C1, 20.12.2013. RU 2595332C1, 27.08.2016. RU 2131882 C1, 20.06.1999. (54) Способ получения бетулина (57) Реферат: Изобретение относится к способу получения бетулина из бересты березы, включающему предварительную активацию бересты и экстракцию бетулина 86%-ным раствором этилового спирта, при этом активацию осуществляют при помощи ультразвукового воздействия с интенсивностью в диапазоне 10-15 R U Вт/см2 на частоте не менее 20-22 кГц при температуре 40°C в течение 5-25 мин, а Стр.: 1 последующую экстракцию интенсифицируют ультразвуковым воздействием с уменьшенной до 5 Вт/см2 интенсивностью колебаний ...

Novel compounds derived from leaves of Actinidia arguta and Anti-inflammatory use thereof

본 발명은 다래나무 잎으로부터 유래된 신규 화합물 및 이의 항염증 용도에 관한 것으로, 보다 구체적으로는 다래나무 잎으로부터 분리 정제된 트리테르펜계 신규 화합물; 상기 화합물을 유효성분으로 포함하는 항염증 또는/및 미백용 조성물에 관한 것이다. 본 발명에 따른 화학식 1로 표시되는 화합물은 다래나무 잎으로부터 분리 정제된 트리테르펜계 신규 화합물에 해당한다. 이러한 신규 화합물은 NF-κB 활성을 효과적으로 억제시키며 멜라닌 생성을 저해하는 활성을 갖는바, 이를 유효성분으로 포함하는 조성물은 항염증 또는/및 미백을 위한 식품, 의약품 및 화장료 소재로 유용하게 사용될 수 있다. The present invention relates to a novel compound derived from a oleander leaf and its anti-inflammatory use, more specifically, a triterpene-based novel compound separated and purified from an oleander leaf; It relates to a composition for anti-inflammatory or / and whitening comprising the compound as an active ingredient. The compound represented by Chemical Formula 1 according to the present invention corresponds to a triterpene-based new compound separated and purified from a dead tree leaf. Since these new compounds effectively inhibit NF-κB activity and have an activity of inhibiting melanin production, a composition comprising them as an active ingredient can be usefully used as food, pharmaceutical and cosmetic materials for anti-inflammatory or/and whitening. .

Process for preparing steroidal (16, 17 - b) cyclohexene and naphthaleno - 21 - carboxylic acid and esters

Title compds. I≮X = H, halogen; Y = H, F, Me; R = COOH; R4 = Cl, F, OH; R5 = H, R2,R3 = H, alkyl, aryl; R6,R7 = H, alkyl, alkoxy, formyl, phenyl, cyano; R8 = H, or CH-C9C10(R9,R10 = H, alkyl)≉, useful as local antiinflammatory, were prepared by oxidizing 21-hydroxysteroid I (R = CH2OH). Thus, a mixt. of 9-fluoro-11β,21-dihydroxy pregna-1,4-dieno≮15α,17-d≉ cyclohexen-3,20-dione 1.2 g, methanol 150ml and CuNO3 300mg was stirred for 1 hr at room temp. to give 9-fluoro-11β-hydroxy-3,20-dioxopregna-1,4-dieno-≮16α,17-d≉ cyclohexene-21-oic acid methyl ester.

7-carboxylic < / RTI > 9,11-epoxy steroids and the general methods for the epoxidation of intermediates and olefinic double bonds useful in the present invention

(화학식 I) (화학식 III) 여러 신규한 반응식, 신규한 공정단계 및 신규한 중간체가 에폭시멕스레논 및 화학식 I의 다른 화합물의 합성에 제공되고, -A-A-는 기 -CHR 4 -CHR 5 - 또는 -CR 4 =CR 5 -를 나타내고, R 3 , R 4 및 R 5 는 수소, 할로, 히드록시, 저급알킬, 저급알콕시, 히드록시알킬, 알콕시알킬, 히드록시카르보닐, 시아노, 아릴옥시로 이루어지는 군에서 독립적으로 선택되고, R 1 은 α-배향 저급 알콕시카르보닐 또는 히드록시카르보닐 라디칼을 나타내고, -B-B-는 기 -CHR 6 -CHR 7 - 또는 화학식 III의 α- 또는 β-배향기를 나타내고, R 6 및 R 7 은 수소, 할로, 저급알콕시, 아실, 히드록시알킬, 알콕시알킬, 히드록시카르보닐, 알킬, 알콕시카르보닐, 아실옥시알킬, 시아노, 아릴옥시로 이루어지는 군에서 독립적으로 선택되고, R 8 및 R 9 는 수소, 할로, 저급알콕시, 아실, 히드록시알킬, 알콕시알킬, 히드록시카르보닐, 알킬, 알콕시카르보닐, 아실옥시알킬, 시아노, 아릴옥시로 이루어지는 군에서 독립적으로 선택되고, 또는 R 8 및 R 9 는 함께 탄소환 또는 헤테로고리환 구조를 이루고, 또는 R 8 또는 R 9 는 R 6 또는 R 7 과 함께 5환 D고리로 축합된 탄소환 또는 헤테로고리환 구조를 이룬다.

17-HYDROXY-3-OXO-17α-PREGN-4-EN-7α, 21-DICORBOXYLATE EPOXY DERIVATIVES AND THEIR APPLICATION

ÐÎÑÑÈÉÑÊÀß ÔÅÄÅÐÀÖÈß RU (19) (11) 2005 121 439 (13) A (51) ÌÏÊ C07J 71/00 (2006.01) ÔÅÄÅÐÀËÜÍÀß ÑËÓÆÁÀ ÏÎ ÈÍÒÅËËÅÊÒÓÀËÜÍÎÉ ÑÎÁÑÒÂÅÍÍÎÑÒÈ, ÏÀÒÅÍÒÀÌ È ÒÎÂÀÐÍÛÌ ÇÍÀÊÀÌ (12) ÇÀßÂÊÀ ÍÀ ÈÇÎÁÐÅÒÅÍÈÅ (21), (22) Çà âêà: 2005121439/04, 07.07.2005 (71) Çà âèòåëü(è): ÄÆÈ. ÄÈ. ÑÈÐË ÝÍÄ ÊÎ. (US) (30) Êîíâåíöèîííûé ïðèîðèòåò: 11.12.1996 US 60/033,315 11.06.1997 US 60/049,388 (62) Íîìåð è äàòà ïîäà÷è ïåðâîíà÷àëüíîé çà âêè, èç êîòîðîé äàííà çà âêà âûäåëåíà: 99114851 12.07.1999 A 2 0 0 5 1 2 1 4 3 9 (57) Ôîðìóëà èçîáðåòåíè 1. 4,5:9,11-Äèýïîêñèä 17-ãèäðîêñè-3-îêñî-17α-ïðåãí-4-åí-7α,21äèêàðáîêñèëàòà γ-ëàêòîíà ôîðìóëû 2. Ïðèìåíåíèå ñîåäèíåíè ïî ï.1 â êà÷åñòâå ïðîìåæóòî÷íîãî ïðîäóêòà â ñèíòåçå ñòåðîèäíûõ ñîåäèíåíèé. 3. Ïðèìåíåíèå ñîåäèíåíè ïî ï.1 â êà÷åñòâå õðîìàòîãðàôè÷åñêîãî ìàðêåðà. 4. 11α,12α-Ýïîêñè-17-ãèäðîêñè-3-îêñî-17α-ïðåãí-4-åí-7α,21-äèêàðáîêñèëàòà γ-ëàêòîí ôîðìóëû Ñòðàíèöà: 1 RU A R U (54) ÝÏÎÊÑÈÄÍÛÅ ÏÐÎÈÇÂÎÄÍÛÅ α-ËÀÊÒÎÍÀ 17-ÃÈÄÐÎÊÑÈ-3-ÎÊÑÎ-17α-ÏÐÅÃÍ-4-ÅÍ-7α, 21-ÄÈÊÎÐÁÎÊÑÈËÀÒÀ È ÈÕ ÏÐÈÌÅÍÅÍÈÅ 2 0 0 5 1 2 1 4 3 9 Àäðåñ äë ïåðåïèñêè: 129010, Ìîñêâà, óë. Á.Ñïàññêà , 25, ñòð.3, ÎÎÎ "Þðèäè÷åñêà ôèðìà Ãîðîäèññêèé è Ïàðòíåðû", ïàò.ïîâ. Ã.Á. Åãîðîâîé R U (43) Äàòà ïóáëèêàöèè çà âêè: 20.01.2007 Áþë. ¹ 2 (72) Àâòîð(û): Íà Äæîí Ñ. (US), ËÈÓ ×èí (US), ÀÍÄÅÐÑÎÍ Äåííèñ Ê. (US), ËÎÑÎÍ Äæîí Ï. (US), ÂÅ×ÎÐÅÊ Äæîçåô (US), ÊÓÍÄÀ Ñàñòðè À. (US), ËÅÒÅÍÄÐÅ Ëåî Äæ. (US), ÏÎÇÇÎ Ìàðê Äæ. (US), ÑÈÍà Þýí-Ëóíã Ë. (US), ÂÀÍà Ïèíã Ò. (US), ÉÎÍÀÍ Ýäâàðä Ý. (US), ÂÅÉÅÐ Ðè÷àðä Ì. (US), ÊÎÂÀÐ Òîìàñ Ð. (US), ÁÀÅÑ Õóëèî À. (US), ÝÐÁ Áåðíõàðä (US) 5. Ïðèìåíåíèå ñîåäèíåíè ïî ï.4 â êà÷åñòâå ïðîìåæóòî÷íîãî ïðîäóêòà â ñèíòåçå ñòåðîèäíûõ ñîåäèíåíèé. 6. Ïðèìåíåíèå ñîåäèíåíè ïî ï.4 â êà÷åñòâå õðîìàòîãðàôè÷åñêîãî ìàðêåðà. R U R U A 2 0 0 5 1 2 1 4 3 9 A 2 0 0 5 1 2 1 4 3 9 Ñòðàíèöà: 2

Benzopyran-containing compounds and method for their use

Certain benzopyran antiestrogens are disclosed for treating estrogen sensitive diseases such as breast cancer. Prodrug forms provide ease of manufacturing, good shelf life, and bioavailability, and preferred stereoisomers are shown to be more effective than racemic mixtures.

11β-SUBSTITUTED 19-NORSTEROIDS, METHOD OF THEIR SYNTHESIS, COMPOUNDS, PHARMACEUTICAL COMPOSITION

Описываются новые 11β-замещенные 19-норстероиды общей формулы (I), в которой n = 5 или 6; R 1 и R 2 , одинаковые или различные -атом водорода, линейный или разветвленный алкильный радикал С 1 -С 8 , возможно замещенным галогеном, или R 1 -карбамоильный радикал, монозамещенный линейным или разветвленным алкильным радикалом С 1 -С 8 или фенильным радикалом, возможно замещенным атомом галогена, а R 2 - атом водорода, или R 1 и R 2 вместе с атомом азота, с которым они связаны, образуют циклический карбамид формулы (II), в которой n = 2 или 3, или R 1 и R 2 образуют диалкил-С 1 -С 4 -аминометиленовый радикал. Соединения формулы (I) обладают глюкокортикоидной или антиглюкокортикоидной, прогестомиметической или антипрогестомиметической, андрогенной или антиандрогенной, эстрогенной или антиэстрогенной активностью и могут входить в состав фармацевтических композиций. 4 с. и 6 з.п. ф-лы, 1 табл. ССУОбОТЬсС ПЧ Го РОССИЙСКОЕ АГЕНТСТВО ПО ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ (19) ВИ” 2140 423 ' 13) СЛ ОМК С 07 4 41/00, 31/00, Абл К 31/58 12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ РОССИЙСКОЙ ФЕДЕРАЦИИ (21), (22) Заявка: 94022277/04, 16.06.1994 (24) Дата начала действия патента: 16.06.1994 (30) Приоритет: 17.06.1993 ЕК 9307310 (46) Дата публикации: 21.10.1999 (56) Ссылки: ЕР 0347370, 1989. ЕР 0116974, 1984. ЕР 0369881, 1990. ЕР 0375347, 1989. /.Зегоа. Вюспет. - (1979) 1: 637-648. Тринус Ф.П. Фармако-терапевтический справочник. - Киев: Здоровья, 1989, с.265. (98) Адрес для переписки: 103735, Москва, ул.Ильинка 5/2, Союзпатент (71) Заявитель: Руссель-Юклаф (ЕК) (72) Изобретатель: Франсуа Никке (ЕК), Жан-Жорж Тетш (ЕК), Патрик Ван де Вельд (ЕК) (73) Патентообладатель: Руссель-Юклаф (ЕК) С1 (54) 11В-ЗАМЕЩЕННЫЕ 19-НОРСТЕРОИДЫ, СПОСОБ ИХ ПОЛУЧЕНИЯ, СОЕДИНЕНИЯ, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ (57) Реферат: Описываются новые 11 В-замещенные 19-норстероиды общей формулы (1), в которой п = 5 или 6; В. и К>, одинаковые или различные -атом водорода, линейный или разветвленный алкильный радикал С.\-Сё, возможно ...

19,11-bridged over 4-estrenes, method of their synthesis, pharmaceutical composition, intermediate compounds

FIELD: organic chemistry, pharmacy. SUBSTANCE: invention describes the novel 19,11-bridged over 4-estrenes of the general formula (I) where each R 6a and R 6b means hydrogen atom or in common mean methylene group; R 7 means hydrogen atom; or R 6a means hydrogen atom or fluorine, chlorine, bromine or iodine atom or saturated at α- or β-position alkyl residue with direct or branched chain with amount of C-atoms up to 4; R 6b and R 7 each means hydrogen atom or in common mean additional bond; or R 14 , R 15 , R 16 each means hydrogen atom; R 14 means hydrogen atom at α--position; R 15 and R 16 in common mean additional bond or methylene bridge at β-position; or R 16 in common with R 17α mean methylene bridge at α-position and R 17β means the group -C-R 22 ; or R 16 means hydrogen atom and R 14 and R 15 in common mean additional bond; R 11 , R 11′ and R 19 each means hydrogen atom; or R 11 means hydrogen atom at α-position; and R 11 and R 19 in common mean additional bond; or R 19 means hydrogen atom and R 11 and R 11′ in common mean additional bond; R 17β /R 17α mean -alkyl or -C-R 22 -False or R 17β /R 17α in common mean the formula (II) where x = 1; U = 0; R 21 means hydrogen atom; R 23 means C 1 -C 4 -alkyl group; R 22 means C 1 -C 3 -alkyl group' A means hydrogen atom, cyano-group or -OR 25 and R 25 means hydrogen atom; B means hydrogen atom, C 1 -C 4 -alkyl group, C 2 - or C 3 -alkyl group; D means hydrogen atom or hydroxy-group; E and G each means hydrogen atom or C 1 -C 3 -alkyl; N = 0, 1, 2, 3 or 4; m = 0, 1 or 2; p = 0 or 1; k = 0, 1, 2 or 3; R 16 means hydrogen atom or methyl-group. New compounds show strong gestagenic activity and used for drugs preparing. Invention describes also method of their synthesis, pharmaceutical composition and intermediate compounds. EFFECT: new compounds indicated above, improved method of synthesis and pharmaceutical composition preparing, valuable pharmacological properties. 13 cl, 2 tbl, 1 dwg, 46 ex УЕЗД 9Ес ПЧ сэ ...

Method of preparing spirolactones

Novel androgens

公开的本发明涉及新颖类固醇的出人意料的发现，该类固醇的特征在于14β，15β-环丙烷环和17α羟甲基。发现根据本发明的这些类固醇通常具有雄激素活性。它们可用于制备雄性避孕药剂，以及用于制备治疗雄激素不足的药物。

Method for separation of isoprenic constituents of guayule

Предложен способ выделения по меньшей мере одного изопренового компонента из смолы гваюлы и/или гваюлоподобного растения, включающий стадии: a) обеспечения обезжиренной смолы из гваюлы и/или гваюлоподобного растения; b) воздействия на указанную обезжиренную смолу путем разделения на фракции жидкость-жидкостного типа с растворителями, которые не смешиваются друг с другом, с получением таким образом неполярного экстракта, содержащего изопреновые компоненты гваюлин А, гваюлин В и аргентатин В: и полярного экстракта, содержащего изопреновые компоненты аргентатин А, аргентатин С и аргентатин D: с) выделения по меньшей мере одного изопренового компонента из указанного полярного экстракта и/или из указанного неполярного экстракта, полученного таким образом, в котором стадия с) включает стадию, на которой указанный полярный экстракт подвергают разделению на фракции жидкость-жидкостного типа с растворителями, не смешиваемыми друг с другом, и/или стадию, на которой указанный неполярный экстракт подвергают разделению на фракции жидкость-твердофазного типа. Технический результат - возможность обеспечения более практичного, недорогостоящего, легко приспосабливаемого масштабируемого и обеспечивающего высокий выход способа в отношении разделения изопропеновых компонентов из смолы растения гваюлы, в частности гваюлина А, гваюлина В, аргентатина А, аргентатина В, аргентатина С и/или аргентатина D. 19 з.п. ф-лы, 12 пр., 1 табл., 4 ил. РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2 704 821 C2 (51) МПК C07J 53/00 (2006.01) C07C 67/56 (2006.01) C07C 67/58 (2006.01) C07C 69/618 (2006.01) C07C 69/92 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ (52) СПК C07J 53/00 (2019.05); C07C 67/56 (2019.05); C07C 67/58 (2019.05); C07C 69/618 (2019.05); C07C 69/92 (2019.05) (21)(22) Заявка: 2018105348, 29.07.2016 29.07.2016 Дата регистрации: 31.10.2019 31.07.2015 IT 102015000040937 (43) Дата публикации заявки: 29.08.2019 Бюл. № 25 (45) Опубликовано: 31.10 ...

Method for isolating guapula isoprene components

РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2018 105 348 A (51) МПК C07J 53/00 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ЗАЯВКА НА ИЗОБРЕТЕНИЕ (21)(22) Заявка: 2018105348, 29.07.2016 (71) Заявитель(и): ВЕРСАЛИС С.П.А. (IT) Приоритет(ы): (30) Конвенционный приоритет: 31.07.2015 IT 102015000040937 (85) Дата начала рассмотрения заявки PCT на национальной фазе: 28.02.2018 R U (43) Дата публикации заявки: 29.08.2019 Бюл. № 25 (72) Автор(ы): КУЭРЧИ Сесилия (IT), ДЕЛЬ ПРЕТЕ Данило (IT), КАЛЬДАРАРО Мария (IT), ДЖИРОТТИ Джанни (IT) (86) Заявка PCT: (87) Публикация заявки PCT: WO 2017/021852 (09.02.2017) R U (54) Способ выделения изопреновых компонентов гваюлы (57) Формула изобретения 1. Способ выделения по меньшей мере одного изопренового компонента из смолы гваюлы и/или гваюлоподобного растения, включающий стадии: a) обеспечения обезжиренной смолы из гваюлы и/или гваюлоподобного растения; b) воздействия на указанную обезжиренную смолу путем разделения на фракции жидкость-жидкостного типа с растворителями, которые не смешиваются друг с другом, с получением таким образом неполярного экстракта, содержащего изопреновые компоненты гваюлин А, гваюлин В и аргентатин В; и полярного экстракта, содержащего изопреновые компоненты аргентатин А, аргентатин С и аргентатин D; и c) выделения по меньшей мере одного изопренового компонента из указанного полярного экстракта и/или из указанного неполярного экстракта, полученного таким образом, в котором стадия с) включает стадию, на которой указанный полярный экстракт подвергают разделению на фракции жидкость-жидкостного типа с растворителями, не смешиваемыми друг с другом, и/или стадию, на которой указанный неполярный экстракт подвергают разделению на фракции жидкость-твердофазного типа. 2. Способ по п. 1, в котором указанный по меньшей мере один изопреновый компонент выбирают из группы, которая включает гваюлин А, гваюлин В, аргентатин А, аргентатин В, аргентатин С, аргентатин D и их смеси. 3. Способ по п. 1 или 2, в ...