НОВЫЕ ФАКТОРЫ РОСТА ФИБРОБЛАСТОВ

Изобретение относится к медицине и касается применения полипептида FGF-9 или его биологически активного фрагмента для получения лекарственного средства для лечения рассеянного склероза. Полипептид может быть на 94-95% идентичен последовательности, простирающейся от аминокислоты 1 до аминокислоты 208 человеческого FGF-9, представленной на фиг.3 (SEQ ID NO: 5). Изобретение обеспечивает стимуляцию миелинизации, пролиферации и выживания нейронов, олигодендроцитов, улучшенную регенерацию нервов. 5 з.п. ф-лы, 9 ил., 2 табл.

СОЕДИНЕНИЯ 7-ФЕНИЛПИРАЗОЛОПИРИДИНА

Изобретение относится к производным 7-фенилпиразолопиридина формулы (I) где R1, R5, R6, R40, R41 и R42 представляют собой различные углеводородные заместители или функциональные группы, его солям или гидратам, в особенности к солям N-циклопропилметил-N-7-[2,6-диметокси-4-(метоксиметил)фенил]-2-этилпиразоло[1,5-а]пиридин-3-ил-N-тетрагидро-2Н-4-пиранилметиламина. Соединение формулы (I), в особенности соли N-циклопропилметил-N-7-[2, 6-диметокси-4-(метоксиметил)фенил]-2-этилпиразоло[1,5-а]пиридин-3-ил-N-тетрагидро-2Н-4-пиранилметиламина, проявляют активность в качестве антагонистов рецептора кортикотропин-высвобождающего фактора и могут найти применение в медицине для лечения ряда заболеваний нервной системы и желудочно-кишечного тракта. Технический результат - получение ряда новых биологически активных веществ. 8 н. и 13 з. п. ф-лы. 5 табл.

ПРИМЕНЕНИЕ АГЕНТА, ОБЛАДАЮЩЕГО МОДИФИЦИРУЮЩИМИ СВОЙСТВАМИ В ОТНОШЕНИИ ГОРМОНОВ НАДПОЧЕЧНИКОВ

Настоящая группа изобретений относится к медицине, а именно к терапии и эндокринологии, и касается применения агента, обладающего модифицирующими свойствами в отношении гормонов надпочечников. Для этого вводят эффективное количество соединения формулы I или его фармацевтически приемлемой соли. При этом для соединения формулы I n равно 1; R представляет собой водород, R, Rи Rнезависимо представляют собой водород, галоген или цианогруппу при условии, что не более чем один из R, Rи Rобозначает водород, и Rи Rпредставляют собой водород.Это обеспечивает эффективное лечение заболеваний и расстройств, характеризующихся повышенными уровнями гормонов стресса. 4 н. и 20 з.п. ф-лы, 2 ил., 2 табл., 8 пр.

АНТАГОНИСТЫ КОРТИКОТРОПИН-РИЛИЗИНГ ФАКТОРА

Изобретение относится к новым соединениям общих формул I, II, III или их фармацевтически приемлемым солям, в которых пунктирными линиями обозначены необязательные двойные связи; A - -CR7 или N; В - -NR1R2, -CR1R2R11, -C(= CR2R12 )R1, -NHCHR1R2, -ОСHR1R2, -SCHR1R2, -CHR2OR12, -CHR2SR12, -C(S)R2 или -C(O)R2, N-этил-2,2,2-трифторацетамид; G - кислород, сера, NH, NH3, водород, метокси, этокси, трифторметокси, метил, этил, тиометокси, NH2, NHCH3 , N(СН3 )2 или трифторметил; Y-N; Z - NH, О, S, -N(C1-C2 алкил) или -C(R13R14), где R13 и R14 независимо друг от друга представляют собой водород, трифторметил или метил, либо один из элементов R13 и R14 является цианогруппой, а другой - водородом или метилом; R1 - C1 -С6 алкил, который может быть необязательно замещен одним или двумя заместителями R8, независимо друг от друга выбираемыми из группы, включающей гидрокси, фтор, хлор, бром, йод, CF3, C1-C4 алкокси, -O-CO-(C1-C4 алкил), где (C1-C4) алкильные части вышеуказанных групп R1 могут необязательно ...

ПРОИЗВОДНОЕ ПЕПТИДА, СПОСОБ ЛЕЧЕНИЯ РАКА У ПАЦИЕНТА

Производное пептида, содержащее остаток соматостатина, или бомбезина, или их производного, фрагмента или аналога, и заместитель формулы I, II или III (значения радикалов см. в п.1 формулы изобретения) имеет более высокую и продленную биологическую активность по сравнению с немодифицированным соматостатином. 2 с. и 15 з.п. ф-лы, 4 табл., 1 ил.

КОМПОЗИЦИЯ С ЗАМЕДЛЕННЫМ ВЫСВОБОЖДЕНИЕМ ДЛЯ ПЕРОРАЛЬНОГО ВВЕДЕНИЯ ЛЕКАРСТВЕННЫХ СРЕДСТВ

... 1. Композиция с замедленным высвобождением для перорального введения лекарственного средства, содержащая лекарственное вещество, носитель для замедленного высвобождения лекарственного вещества и ускорителя гидратации геля, в которой весовое отношение лекарственного вещества, носителя для длительного высвобождения лекарственного вещества и ускорителя гидратации геля находится в интервале 1:3˜30:0,1˜15; носитель является смесью альгината натрия и ксантановой камеди, имеющей весовое отношение 1:0,1˜10; и ускоритель гидратации геля является смесью гидроксипропилметилцеллюлозы и альгината пропиленгликоля, имеющей весовое отношение 1:0,05˜20. 2. Композиция по п.1, в которой носитель дополнительно содержит камедь рожкового дерева в качестве основы (носителя) для замедленного высвобождения лекарственного вещества. 3. Композиция по п.2, в которой весовое отношение альгината натрия, ксантановой камеди и камеди рожкового дерева находится в интервале 1:0,2˜10:0,1˜5. 4. Композиция по п.1, в которой ...

Способ получения производных стероидов

Изобретение касается производных стероидов, в частности соединений общей формулы R2 В R где R, - -С -Сф-алкилдигидроиндолип, пиридинил, фенил, замещенный -алкиламиногруппой или киламино-С -С4-алкильной группой (в которых азот может быть окислен), пирролидинилом, ди-С ,-С4.-алкиламино- -С -С -алкилтио-, ди-С -С -алкиламино-С -С ,-алкилокси- или триметилси- лильной группой; R- з ОН, CHjO, этинил, карбонил, -C-NOH; Н; С2-С4.-алкенил, С -С -алкади- ен, С -С -алкинил (может быть замещен „галогеном, , (CEj)Sit низшим ал- кенилом); В и С образуют двойную связь или эпоксидную группу, которые обладают фармакологически ценными свойствами. Цель изобретения - создание новых веществ с нехарактерной для данного класса активностью. Синтез ведут из соответствующего кеталя (А - кетальная группа, которая может быть циклической или нециклической), который дегидратируют катионообменной сульфосмолой или НС1. Полз енный продукт при необходимости обрабатывают гидроксиламином или, если R, - ди-. -С,-С4-алкиламино-С ...

Способ получения стероидных спирооксазолидинов или их стереоизомеров

Способ получения кортикоидов

STEROIDSPIROOXAZOLIDINONDERIVATE, VERFAHREN ZU DEREN HERSTELLUNG UND DIESE ENTHALTENDE ARZNEIMITTEL

Delayed and sustained drug release

6,7 ALPHA-DIFLUOROMETHYLENANDROSTA-1,4-DIEN-3-ONE DERIVATIVES AND PROCESS FOR THEIR PREPARATION

Chemical compounds

16a-hydroxy-17a-amino pregnanes their synthesis and their conversion to pregnano[

A process for preparing 16 alpha -hydroxy-17 alpha -aminopregnane derivatives through the opening of the corresponding 16 alpha , 17 alpha -epoxides with amines. The use of the thus obtained compounds as intermediates in the synthesis of pharmacologically active pregnano-?17 alpha ,16 alpha -d!oxazolines is also claimed.

New 11B, 18-epoxy steroids having anti-aldosterone activity

Compounds of the formula: wherein X is a hydrogen atom or a halogen atom, Y<1> is a hydrogen atom, an acetylthio group, a carboxy or esterified carboxy group, a lower alkyl group or a halogen atom, Y<2> is a hydrogen atom or a halogen atom Z<1> is a hydroxy group and Z<2> is a group of the formula -CH2CH2COOM (in which M is potassium or sodium); or Z<1> and Z<2> when taken together with the adjacent carbon atom to which they are attached represent a gamma -lactone ring of the formula: and the dotted lines between 1- and 2-positions and between the 6- and 7-positions represent double bonds which can optionally be present. Activity: antialdosterone, with reduced side-effects.

CHEMICAL COMPOUNDS

Hydrocortisone derivative

... 17 alpha -butyryloxy-11 beta -hydroxy-21-propionyloxy-4-pregnen-3,20-dione, i.e., hydrocortisone 17-butyrate 21-propionate of the present invention is prepared by acylating hydrocortisone 17-butyrate with propionic acid anhydride or halide. The compound of the present invention has excellent anti-inflammatory effect, percutaneous absorption and less side effect.

DERIVATIVES OF 9-FLUOROPREDNISOLONE

The active compounds correspond to the general formula I in which R1 denotes an alkanoyl group or cycloalkanoyl group having 1 to 8 carbon atoms or a benzoyl group and X represents a fluorine atome, a chlorine atom or an alkanoyloxy group having 3 to 8 carbon atoms. The novel 9-fluoroprednisolone derivatives can be obtained by opening corresponding 9,11 beta -epoxy compounds with hydrogen fluoride or halogenating or esterifying corresponding 9-fluoro derivatives in the 21-position or cleaving a corresponding 17 alpha -cycloalkanecarbonyloxy compound with a trimethylsilyl halide or triphenylmethyl halide. Medicaments which contain at least one of the abovementioned compounds as an active component can be used for the treatment of inflammations.

COMPOUNDS OF THE PREGNANE SERIES WITH AN OXYGEN FUNCTION IN THE 19-POSITION PHARMACEUTICAL PREPARATIONS CONTAINING SUCH COMPOUNDS

CORTICOIDS

New forms and salts of a dihydropyrrolo[1,2C]imidazolyl aldosterone synthase or aromatase inhibitor

Substituted pyrido- or pyrimido- containing 6,6- or 6,7- bicyclic derivatives.

This invention relates to compounds of the formula R5/Wherein:A is nitrogen or CR7 B is NR'R2, -CR'R2R10, -C(=CR2Rn)Rl, -NHCR:R2R10, -OCR'R'R13, -SCR'R^10, -CR'R^NHR1, -CR2RiaORl, -CR;RIOSRS or -COR2, and is single bonded to D; or 3 is CR'R2, and is double bonded to D and D is carbon; D and G are nitrogen; E and K are carbon; Z is NK, oxygen,, sulphur, -IMCd-G, alkyl) or CR13R" Wherein R13 and Ru are independently selected from Hydrogen and methyl with the exception that one R13 and R1J may optionally be cyano; With proviso that in the six or seven numbered rings cf Structures in formula I there can not be two double Bands adjacent to each other; R3 and R3 are as defined in the general descriotion.

Substituted pyrido- or pyrimido- containing 6,6- or 6,77-bicyclic derivatives

New forms and salts of a dihydropyrrolo[1,2C]imidazolyl aldosterone synthase or aromatase inhibitor

New forms and salts of a dihydropyrrolo[1,2C]imidazolyl aldosterone synthase or aromatase inhibitor

Substituted pyrido- or pyrimido- containing 6,6-or6,7-bicyclic derivatives

Heterocyclic derivatives their process of production and pharmaceutical composition the container

New steroids comprising a cycle spirannic in position 17, their method and intermediaries of preparation, their application like drugs and the compositions pharmaceutical containing them.

Compos. pharmac. constituted as active ingredient, by the 9a, 11B-dichloro 16a-methyl 21-oxycarbonyldicyclohexyl méthyloxy pregna-1,4-diene 3,20-dione and by a excip. pharmac. inert suited has to allow the action of the product in the rectum or the colonist.

Substituted pyrido- or pyrimido- containing 6,6- or 6,77-bicyclic derivatives

HETEROCYCLIC DERIVATIVES

HETEROCYCLIC DERIVATIVES

PHARMACEUTICAL PREPARATION WITH RETARDED RELEASE FOR ORAL ACTIVE SUBSTANCE ADMINISTRATION

PROCEDURE FOR THE PRODUCTION OF NEW THIOETIANSAEUREDERIVATEN

PROCEDURE FOR THE PRODUCTION OF NEW STEROID SPIRO OXAZOLIDINON DERIVATIVES AND YOUR STEREOISOMERS

VERFAHREN ZUR HERSTELLUNG NEUER KORTIKOIDE

TRICYCLI STEROIDHORMONKERNREZEPTOR MODULATORS

GLYCYRRHETINSÄUREDERIVATE AND YOUR USE FOR the PRODUCTION of a MEDICINE FOR the INHIBITION of the 11BETA-HYDROXYSTEROID DEHYDROGENASE

INJECT-CASH FOAM AND NEW ONE PHARMACEUTICAL APPLICATIONS FOR IT

VERFAHREN ZUR HERSTELLUNG VON NEUEN 9-FLUORPREDNISOLON-DERIVATEN

BV8-NUKLEINSÄUREN AND POLYPEPTIDE WITH MITOGENER ACTIVITY

PROCEDURE FOR the PRODUCTION of NEW 3-KETO-DELTA 4,9,19-NORSTEROID-DERIVATE

USE OF THE L-DEPRENYLS FOR THE DELAY OF THE AGECAUSED DESTRUCTION OF THE MEMORY WITH DOGS

ETHYL DIAMINE DERIVATIVES AND YOUR USE AS OREXINREZEPTORANTAGONISTEN

6,6-ETHYLEN-15,16-METHYLEN-3-OXO-17ALPHA-PREGN EN-21,17-CARBOLACTONE, PROCEDURE FOR THEIR PRODUCTION AND THIS CONTAINING PHARMACEUTICAL PRAPARATE.

3-BETA, 7-BETA, 15-ALPHA-TRIHYDROXY-5-ANDROSTEN-1 - ONE, YOUR 3,15-TRIMETHYLESSIGSAEURE-ESTER AND YOUR PRODUCTION.

15,16-METHYLEN-17-ALPHA-PREGNA-4,6-DIEN-21CARBONS|URESALZE, THESE CONTAINING PHARMACEUTICAL PREPARATIONS AS WELL AS PROCEDURES TOO THEIR PRODUCTION.

PROCEDURE FOR THE PRODUCTION OF NEW ONE, DIURETISCH EFFECTIVE STEROID SPIRO OXAZOLIDINON DERIVATIVES EN AND OF MEDICINE MEANS PREPARED FROM THESE CONNECTIONS

PROCEDURE FOR the PRODUCTION OF INTERMEDIATE PRODUCTS FOR 11-beta, 16-ALPHA, 17-ALPHA, 21TETRAHYDROXYPREGNA-3-20-DIONE 16-ALPHA, 17-ALPHAACETAL AND THEIR 21-ESTER.

IN THE THERAPEUTIK APPLICABLE COMPOSITION WITH AGGREGATION-RESTRAINING EFFECT ON BLOOD PANELS.

DRUG FOR ORAL ADMINISTRATION, CONSISTING ON THE ONE HAND OF 9-ALPHA, 11-BETA-DICHLOR-16-ALPHAMETHYL-21-OXYCARBONYLDICYCLOHEXYL-METHYLOXYPREGNA-1,4-DIENE-3,20-DIONE AS ACTIVE SUBSTANCE AND ON THE OTHER HAND FROM an INERT PHARMACEUTICAL ONE EXIPIENS, THE EFFECTIVENESS OF THE PRODUCT IN REKTUM OR IN THE KOLON UNFOLDING LOADS ITSELF, AS WELL AS THE USE OF THIS ACTIVE SUBSTANCE TO

PROGESTERON DERIVATIVES, PROCEDURES FOR YOUR PRODUCTION AND PHARMACEUTICAL COMPOSITIONS.

7-ALKYL-STEROIDDERIVATE, PROCEDURE FOR YOUR PRODUCTION, YOUR USE IN DRUGS AND PHARMACEUTICAL COMPOSITIONS, IT CONTAINING.

14BETA-H, 14 - AND 15-EN-11BETA-ARYL-4-ESTRENE

PROCEDURE FOR THE TREATMENT OF INFLAMMATION-CAUSED CONDITIONS OF THE EYES

TRICYCLIC CRF RECEPTOR ANTAGONIST

GALENI KORTIKOIDFORMEN FOR BY AND SUBLINGUALE ADMINISTRATION AND YOUR MANUFACTURING PROCESS.

USE FROM BICYCLI IMIDAZOL CONNECTIONS TO THE TREATMENT OF HYPERALDOSTERONISMUS.

PRESERVATIVE FOR RESTAURANTS PHARMACEUTICAL PREPARATIONS CONTAINING A FATTY ACID/CAMINO ACID ABSTENTION SOAP

TWO-CHAMBER CARTOUCHE FOR VERNEBLER

LIVER-SPECIFIC BILE ACID DERIVATIVES OF THE ANTIGLUKOKORTICOIDS RU486

ACYLIERTE INSULIN-SIMILAR

TNF RECEPTOR AND STEROIDHORMON DHEA IN A COMBINATION THERAPY

AMINOTHIAZOLE DERIVATIVES, YOUR PRODUCTION AND IT ABSTENTION PHARMACEUTICAL COMPOSITIONS

PHENYLSULFONYL-1,3-DIHYDRO-2H-INDOL-2-ON OF DERIVATIVES, THEIR PRODUCTION AND THEIR THERAPEUTIC USE

3-BETA-HYDROXYLIERTE NATURAL ONE STEROIDDERIVATE ABSTENTION DRUG COMPOSITIONS AND THEIR USE

INCLUSION COMPLEXES OF DEHYDROEPIANDROSTERON AND CORRESPONDING PHARMACEUTICAL COMPOSITIONS

DNA encoding a human melanin concentrating hormone receptor (MCH1) and uses thereof

Crystal form of bromodomain protein inhibitor drug, preparation method and use thereof

Provided are a crystal form of a bromodomain protein inhibitor 2-[4-(2-hydroxyethoxy)-3,5-dimethylphenyl]-5,7-dimethoxyquinazolin-4(3H)-one represented by Formula I, a preparation method and a use thereof. The present invention belongs to the field of medicine. The crystal forms are crystal form CS2, crystal form CS8, crystal form CS13, crystal form CS20, crystal form CS1, crystal form CS7, crystal form CS9, crystal form CS11, and crystal form CS4, and can be used to prepare drugs for treating cardiovascular, cholesterol, or lipid-related disorders.

HALOGENATED DERIVATIVES OF 16 ALPHA-METHYL PREGNAME

AMINO ACID DERIVATIVES (AND ABNORMAL PEPTIDES) AS HUMAN PLASMA RENIN INHIBITORS

METHOD OF TREATMENT USING 17 BETA-CYCLOPROPYLAMINOANDROSTENE DERIVATIVES

3 KETO DELTA4,9,19-NOR STEROID DERIVATIVES

Human 3 relaxin

Abstract 5 Human H3 preprorelaxin, human H3 prorelaxin, human H3 relaxin, human relaxin analogues having a modified A chain and/or a modified B chain are described. Also described are nucleic acid sequences encoded human H3 preprorelaxin, human H3 prorelaxin, human H3 relaxin, human relaxin analogues. Also described are methods for the treatment of conditions responsive to administration of H3 relaxin or analogues thereof.

Etomidate analogues that do not inhibit adrenocortical steroid synthesis

The invention is directed to compounds according to formula (I): where R ...

Etomidate analogues that do not inhibit adrenocortical steroid synthesis

The invention is directed to compounds according to formula (I): where R is LC(O)OT or LC(O)OLC(O)OT; R is a substituted or unsubstituted C-Calkyl, C-C alkenyl, or C-C alkynyl, or R; n is an integer from 0 to 5; each R is independently halogen or R; Rand R are independently H, halogen, CN or CF; Land L are each independently a bond, a substituted or unsubstituted C-C alkylene, C-C alkenylene, or C-C alkynylene; and T is H, a substituted or unsubstituted C-C alkyl, C-C alkenyl, or C-C alkynyl, nitrophenol, or cyclopropyl. The invention is also directed to a pharmaceutical composition comprising a compound according to formula (I) and a pharmaceutically acceptable carrier, and to methods for providing anesthesia in mammals by administering such a pharmaceutical composition.

AMINO ACID DERIVATIVES

Pharmaceutical formulation

Transdermal pharmaceutical delivery composition

7ALPHA-ACYLTHIO-1ALPHA,2ALPHA-METHYLENE-3-OXO-17ALPHA-PREG- 4ENE--21,17-CARBOLACTONES

7-ALKYLATED STEROID DERIVATIVES

Insulin-like growth factor (IGF) I mutant variants

SUBSTITUTED STEROID-SPIRO-OXAZOLIDINONE DERIVATIVES

Corticotropin releasing factor antagonists

D-HOMOSTEROIDS AND PHARMACEUTICAL COMPOSITIONS

Genes associated with diseases of the kidney

DIOL-CONTAINING RENIN INHIBITORS

Liver specific bile acid derivatives of the glucocorticoid antagonist ru486

Electrospun pharmaceutical compositions

AMINO ACID DERIVATIVES

7ALPHA-ACYLTHIO-1ALPHA,2ALPHA-METHYLENE-3-OXO-17ALPHA-PREG- 4ENE--21,17-CARBOLACTONES

THIO ETIANIC ACID DERIVATIVES

Conjugates of dna interacting groups with steroid hormones for use as nucleic acid transfection agents

Lipid metabolism transcription factor

COMPOSITIONS FOR REDUCING SYMPATHOMIMETIC-INDUCED SIDE EFFECTS BY SERENOA REPENS EXTRACT

Provided are compositions including Serenoa repens and extracts thereof, in combination with a sympathomimetic agent, which may be used to control a variety of physical conditions, including obesity, appetite suppression, decongestion, asthma and energy stimulation.Serenoa repens, or extracts thereof, when added to dosage forms of pharmacologic agents with sympathomimetic activity, or when administered in combination with sympathomimetic agents, decreases side effects. Thus, debilitating side effects associated with use of pharmacologic agents that stimulate adrenergic receptors and display sympathomimetic effects can be reduced.

LIPID METABOLISM TRANSCRIPTION FACTOR

The invention provides a mammalian nucleic acid sequence and fragments thereof. It also provides for the use of these nucleic acid sequences in a model system for the characterization, diagnosis, evaluation, treatment, or prevention of conditions, diseases and disorders associated with expression of the mammalian nucleic acid sequence. The invention additionally provides expression vectors and host cells for the production of the protein encoded by the mammalian nucleic acid sequence.

DOMINANT NEGATIVE PROTEINS AND METHODS THEREOF

The invention relates to novel proteins with TNFSF antagonist activity and nucleic acids encoding these proteins. The invention further relates to the use of the novel proteins in the treatment of TNFSF-related disorders.

GLUCOCORTICOID-SELECTIVE AGENTS

Compounds having Formula (I) are useful for modulating the glucocorticoid receptor in a mammal. Also disclosed are pharmaceutical compositions comprising compounds of Formula (1) and methods of treating immune, autoimmune, inflammatory, adrenal imbalance, cognitive and behavioral diseases in a mammal.

PROCESS FOR THE PREPARATION OF 10-SUBSTITUTED STEROIDS

L'invention a pour objet un procédé de préparation des produits (I): (I) où X est -CH2- et R est un aryle éventuellement substitué, ou vinyle ou éthynyle éventuellement substitué; ou X est un soufre ou une liaison et R est un aryle éventuellement substitué; R2 est méthyle ou éthyle; R3 est alkyle, alkényle ou alkynyle (1-8C) éventuellement substitué; R4 est H ou acyle; ; et le trait pointillé indique la présence éventuelle d'une liaison. L'invention concerne également les produits (I) gui possèdent une remarquable activité anti-glucocorticoîde et, pour certains, glucocorticoîde. L'invention concerne en outre une composition pharmaceutique renfermant au moins un des produits (I) avec un excipient pharmaceutiquement acceptable.

METHOD OF PRODUCING ANTI-ADRENAL ACTIVITY AND COMPOSITIONS THEREFOR

Use of tyrosine kinase inhibitors for treatment of cushing's disease and hypercortisolism

The invention relates to methods and kits for the treatment of, prevention of, and lowering the chances of developing Cushing's Disease and/or hypercortisolism by the administration of a tyrosine kinase inhibitor, such as gefitinib.

Differential diagnosis of ectopic cushing's syndrome

Improved methods and systems for diagnosing and for treating Cushing's syndrome and Cushing's Disease are provided herein, including methods and systems for concurrently treating Cushing's syndrome and differentially diagnosing Cushing's Disease from Ectopic Cushing's Syndrome in a patient with an established diagnosis of ACTH-dependent Cushing's syndrome. Treatment methods can use glucocorticoid receptor antagonists (GRAs), which differentially affect the ratio of cortisol to ACTH levels in patients having Cushing's Disease versus patients having Ectopic Cushing's Syndrome. Methods for concurrently treating and differentially diagnosing Cushing's Disease from Ectopic Cushing's Syndrome include obtaining baseline cortisol and ACTH levels of a patient, treating the patient with a GRA according to a protocol that would typically substantially elevate cortisol levels, obtaining post-treatment cortisol and ACTH levels of the patient, determining a differential relationship between baseline cortisol and ACTH levels and post-treatment cortisol and ACTH levels and providing a positive diagnosis based on the differential relationship.

Treatment and differential diagnosis of cushing's disease and ectopic cushing's syndrome

Improved methods and systems for diagnosing and for treating Cushing's syndrome and Cushing's Disease are provided herein, including methods and systems for concurrently treating Cushing's syndrome and differentially diagnosing Cushing's Disease from Ectopic Cushing's Syndrome in a patient with an established diagnosis of ACTH-dependent Cushing's syndrome. Treatment methods can use glucocorticoid receptor antagonists (GRAs), which differentially affect the ratio of cortisol to ACTH levels in patients having Cushing's Disease versus patients having Ectopic Cushing's Syndrome. Methods for concurrently treating and differentially diagnosing Cushing's Disease from Ectopic Cushing's Syndrome include obtaining baseline cortisol and ACTH levels of a patient, treating the patient with a GRA according to a protocol that would typically substantially elevate cortisol levels, obtaining post-treatment cortisol and ACTH levels of the patient, determining a differential relationship between baseline cortisol and ACTH levels and post-treatment cortisol and ACTH levels and providing a positive diagnosis based on the differential relationship.

Compounds for improved viral transduction

The present invention provides methods and compositions for improving efficacy of viral transduction of cells. More particularly, the present invention provides methods and materials useful for safely and reliably improving the efficiency of methods and materials useful for safely and reliably improving the efficiency of methods for transducing cells, such as human hematopoietic stem cells (HSC), with viruses and/or viral vectors. The compositions and methods are useful for therapeutic indications amenable to treatment with hematopoietic stem cell gene therapies.

Methods of treating congenital adrenal hyperplasia

Patients with congenital adrenal hyperplasia (CAH) need adequate care and treatment in order to lead normal lives. Hence, there is a need for new methods of treating CAH. This disclosure provides new compounds, salts, compositions and uses thereof in the treatment of CAH.

CORTICOTROPIN RELEASING FACTOR RECEPTOR ANTAGONISTS

The present invention provides novel pharmaceutical compositions comprising -(4-Chloro-2-(morpholin-4-yl)thiazol-5-yl)-7-(1-ethylpropyl)-2,5-dimethylpyrazolo(1,5-a)pyrimidine and methods of using the same for the treatment of Congenital adrenal hyperplasia (CAH). 2. The method of claim 1 , wherein Compound 1 or a pharmaceutically acceptable salt thereof is administered at a dose between about 50 mg/day and about 1600 mg/day.3. The method of claim 1 , wherein Compound 1 or a pharmaceutically acceptable salt thereof is administered at a dose between about 100 mg/day and about 600 mg/day.4. The method of claim 1 , wherein Compound 1 or a pharmaceutically acceptable salt thereof is administered at a dose of about 200 mg/day.5. The method of claim 1 , wherein Compound 1 or a pharmaceutically acceptable salt thereof is in the form of microparticles.6. The method of claim 5 , wherein the average size of the microparticles is between about 1 μm and about 20 μm.7. The method of claim 1 , wherein Compound 1 or a pharmaceutically acceptable salt thereof is in the form of a pharmaceutical composition.8. The method of claim 7 , wherein the pharmaceutical composition is in the form of a capsule or a tablet.9. The method of claim 1 , wherein CAH is classic CAH.10. The method of claim 1 , wherein CAH is non-classic CAH.11. The method of claim 1 , wherein the 17-OHP level in a human is reduced by at least 15% from baseline.12. The method of claim 1 , wherein the 17-OHP level in a human is reduced by at least 20% from baseline.13. The method of claim 1 , wherein the 17-OHP level in a human is reduced by at least 25% from baseline.14. The method of claim 1 , wherein the 17-OHP level in a human is reduced by at least 10% from baseline and is maintained at a reduced level post 24 hours.15. The method of claim 1 , wherein the 17-OHP level in a human is reduced by at least 10% from baseline and is maintained at a reduced level post 4 weeks.16. The method of claim 1 , wherein the 17-OHP ...

Treatment of congenital adrenal hyperplasia

CRF1 receptor antagonists have the potential to directly inhibit ACTH release in patients with CAH and thereby allow normalization of androgen production while using lower, more physiologic doses of hydrocortisone, and thus reducing treatment-associated side effects.

CORTICOTROPIN RELEASING FACTOR RECEPTOR ANTAGONISTS

The present invention provides novel pharmaceutical compositions comprising -(4-Chloro-2-(morpholin-4-yl)thiazol-5-yl)-7-(1-ethylpropyl)-2,5-dimethylpyrazolo(1,5-a)pyrimidine and methods of using the same for the treatment of Congenital adrenal hyperplasia (CAH). 2. The method of claim 1 , wherein Compound 1 claim 1 , or a pharmaceutically acceptable salt or solvate thereof claim 1 , is administered at a dose between about 50 mg/day and about 1200 mg/day.3. The method of or claim 1 , wherein Compound 1 claim 1 , or a pharmaceutically acceptable salt or solvate thereof claim 1 , is administered at a dose between about 50 mg/day and about 1000 mg/day.4. The method of any one of to claim 1 , wherein Compound 1 claim 1 , or a pharmaceutically acceptable salt or solvate thereof claim 1 , is administered at a dose between about 50 mg/day and about 800 mg/day.5. The method of any one of to claim 1 , wherein Compound 1 claim 1 , or a pharmaceutically acceptable salt or solvate thereof claim 1 , is administered at a dose between about 100 mg/day and about 600 mg/day.6. The method of any one of to claim 1 , wherein Compound 1 claim 1 , or a pharmaceutically acceptable salt or solvate thereof claim 1 , is administered at a dose between about 200 mg/day and 400 mg/day.7. The method of any one of to claim 1 , wherein Compound 1 claim 1 , or a pharmaceutically acceptable salt or solvate thereof claim 1 , is administered at a dose of about 200 mg/day.8. The method of any one of to claim 1 , wherein Compound 1 claim 1 , or a pharmaceutically acceptable salt or solvate thereof claim 1 , is in the form of microparticles.9. The method of claim 8 , wherein the average size of the microparticles is between about 1 μm and about 20 μm.10. The method of or claim 8 , wherein the average size of the microparticles is between about 5 μm and about 15 μm.11. The method of any one of to claim 8 , wherein the average size of the microparticles is less than about 10 μm.12. The method of any one of ...

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.

Антагонисты рецептора cfr1 для лечения врожденной гиперплазии коры надпочечников

РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2020 112 197 A (51) МПК A61K 31/427 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ЗАЯВКА НА ИЗОБРЕТЕНИЕ (21)(22) Заявка: 2020112197, 21.01.2015 (71) Заявитель(и): НЬЮРОКРАЙН БАЙОСАЙЕНСИЗ, ИНК. (US) Приоритет(ы): (30) Конвенционный приоритет: (72) Автор(ы): ГРИГОРИАДИС, Димитри, Э. (US) R U (54) АНТАГОНИСТЫ РЕЦЕПТОРА CFR1 ДЛЯ ЛЕЧЕНИЯ ВРОЖДЕННОЙ ГИПЕРПЛАЗИИ КОРЫ НАДПОЧЕЧНИКОВ (57) Формула изобретения 1. Применение антагониста рецептора CRF1, выбранного из группы, состоящей из 2,5-диметил-3-[2-метил-4-(метилокси)фенил]-N-[(1S)-1-(3-метил-1,2,4-оксадиазол-5-ил) пропил]пиразоло[1,5-a]пиримидин-7-амина (NBI-77860) и 4-(2-хлор-4-метокси-5метилфенил)-N-[(1S)-2-циклопропил-1-(3-фтор-4-метилфенил)этил]-5-метил-N-(2-пропин1-ил)-2-тиазоламина (SSR-125543), или их фармацевтически приемлемых солей, для лечения врожденной гиперплазии коры надпочечников. 2. Применение по п.1, где антагонистом рецептора CRF1 является NBI-77860 или его фармацевтически приемлемая соль. 3. Способ по п.1, где антагонистом рецептора CRF1 является SSR-125543 или его фармацевтически приемлемая соль. 4. Применение антагониста рецептора CRF1, выбранного из группы, состоящей из 2,5-диметил-3-[2-метил-4-(метилокси)фенил]-N-[(1S)-1-(3-метил-1,2,4-оксадиазол-5-ил) пропил]пиразоло[1,5-a]пиримидин-7-амина (NBI-77860) и 4-(2-хлор-4-метокси-5метилфенил)-N-[(1S)-2-циклопропил-1-(3-фтор-4-метилфенил)этил]-5-метил-N-(2-пропин1-ил)-2-тиазоламина (SSR-125543), или их фармацевтически приемлемых солей, для снижения уровней 17-гидроксипрогестерона (17-OHP) и АКТГ у субъекта с врожденной гиперплазией коры надпочечников (ВГКН). 5. Применение по п.4, где антагонистом рецептора CRF1 является NBI-77860 или его фармацевтически приемлемая соль. Стр.: 1 A 2 0 2 0 1 1 2 1 9 7 A Адрес для переписки: 129090, Москва, ул. Б.Спасская, 25, строение 3, ООО "Юридическая фирма Городисский и Партнеры" 2 0 2 0 1 1 2 1 9 7 (43) Дата публикации заявки: 21.05.2020 Бюл. № 15 R U 21.01. ...

Антагонисты рецептора cfr1 для лечения врожденной гиперплазии коры надпочечников

РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2016 133 972 A (51) МПК A61K 31/427 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ЗАЯВКА НА ИЗОБРЕТЕНИЕ (21)(22) Заявка: 2016133972, 21.01.2015 (71) Заявитель(и): НЬЮРОКРАЙН БАЙОСАЙЕНСИЗ, ИНК. (US) Приоритет(ы): (30) Конвенционный приоритет: 21.01.2014 US 61/929,941; 17.04.2014 US 61/981,033; 27.10.2014 US 62/069,155 (72) Автор(ы): ГРИГОРИАДИС Димитри Э. (US) R U (43) Дата публикации заявки: 05.03.2018 Бюл. № 07 (85) Дата начала рассмотрения заявки PCT на национальной фазе: 22.08.2016 US 2015/012315 (21.01.2015) (87) Публикация заявки PCT: R U Адрес для переписки: 129090, Москва, ул. Б.Спасская, 25, строение 3, ООО "Юридическая фирма Городисский и Партнеры" (54) АНТАГОНИСТЫ РЕЦЕПТОРА CFR1 ДЛЯ ЛЕЧЕНИЯ ВРОЖДЕННОЙ ГИПЕРПЛАЗИИ КОРЫ НАДПОЧЕЧНИКОВ (57) Формула изобретения 1. Способ лечения врожденной гиперплазии коры надпочечников (ВГКН) посредством введения нуждающемуся в этом субъекту антагониста рецептора CRF1 с периодом полудиссоциации свыше 30 минут. 2. Способ по п.1, где период полудиссоциации антагониста рецептора CRF1 составляет свыше 40 минут. 3. Способ по п.1, где период полудиссоциации антагониста рецептора CRF1 составляет свыше 50 минут. 4. Способ по п.1, где антагонист рецептора CRF1 является Соединением I (NBI-77860; 2,5-диметил-3-[2-метил-4-(метилокси)фенил]-N-[(1S)-1-(3-метил-1,2,4-оксадиазол-5-ил) пропил]пиразоло[1,5-a]пиримидин-7-амином). 5. Способ по п.1, где антагонист рецептора CRF1 является NBI-30775, NBI-34041, SSR-126374, SSR-125543, анталармином (N-бутил-N-этил-2,5,6-триметил-7-(2,4,6триметилфенил)пирроло[3,2-e]пиримидин-4-амином) или DMP904. 6. Способ по любому из пп.1-5, где антагонист рецептора CRF1 вводят перед сном. Стр.: 1 A 2 0 1 6 1 3 3 9 7 2 A WO 2015/112642 (30.07.2015) 2 0 1 6 1 3 3 9 7 2 (86) Заявка PCT: A 2 0 1 6 1 3 3 9 7 2 A R U 2 0 1 6 1 3 3 9 7 2 Стр.: 2 R U 7. Способ по любому из пп.1-5, где антагонист рецептора CRF1 вводят во время или перед расчетным временем ...

Composition comprising hydrocortisone

FIELD: medicine; pharmaceuticals. SUBSTANCE: group of inventions refers to the chemical-pharmaceutical industry and is a pharmaceutical composition for oral administration for the treatment of adrenal insufficiency, comprising a carrier in the form of microparticles; drug layer comprising an effective amount of hydrocortisone and a binding agent; insulating polymer layer containing at least 14% w/w. hydroxypropylmethylcellulose and 1-2% w/w. magnesium stearate, contacting said layer of the drug, wherein said insulating polymer layer separates the drug layer and the taste-masking polymer layer containing at least 0.14% w/w. hydroxypropylmethylcellulose and at least 0.58% w/w. ethylcellulose contacting said insulating layer. Invention also provides a method of treatment for monitoring adrenal insufficiency in children, including administering an effective amount of the composition. EFFECT: hydrocortisone in the proposed composition is released immediately, after a small delay phase. 18 cl, 3 dwg, 6 tbl, 3 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2 664 678 C2 (51) МПК A61K 9/50 (2006.01) A61K 31/573 (2006.01) A61K 47/00 (2006.01) A61P 5/38 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ (52) СПК A61K 9/50 (2018.05); A61K 31/573 (2018.05); A61K 47/00 (2018.05); A61P 5/38 (2018.05) (21)(22) Заявка: 2015150303, 12.05.2014 (24) Дата начала отсчета срока действия патента: Дата регистрации: 21.08.2018 17.05.2013 GB 1308933.9 (43) Дата публикации заявки: 22.06.2017 Бюл. № 18 2008187586 A1, 07.08.2008. RU 2385156 C2, 27.03.2010. С.И. Ожегов, Н.Ю. Шведова. Толковый словарь Ожегова. - 1949-1992. RU 2290940 С2, 10.01.2007. Raymond C Rowe, Paul J Sheskey, Marian E Quinn, Handbook of Pharmaceutical Excipients, No 6, 2009, p. 917, 20.06.1998. (45) Опубликовано: 21.08.2018 Бюл. № 24 (85) Дата начала рассмотрения заявки PCT на национальной фазе: 17.12.2015 (86) Заявка PCT: GB 2014/051442 (12.05.2014) C 2 C 2 (56) Список документов, ...

Patent JPH0212479B2

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`7ВУ’” 2015150303” АЗ Дата публикации: 26.03.2018 Форма № 18 ИЗ,ПМ-2011 Федеральная служба по интеллектуальной собственности Федеральное государственное бюджетное учреждение «Федеральный институт промышленной собственности» ж 9 (ФИПС) ОТЧЕТ О ПОИСКЕ 1. . ИДЕНТИФИКАЦИЯ ЗАЯВКИ Регистрационный номер Дата подачи 2015150303/15(077480) 12.05.2014 РСТ/6В2014/051442 12.05.2014 Приоритет установлен по дате: [ ] подачи заявки [ ] поступления дополнительных материалов от к ранее поданной заявке № [ ] приоритета по первоначальной заявке № из которой данная заявка выделена [ ] подачи первоначальной заявки № из которой данная заявка выделена [ ] подачи ранее поданной заявки № [Х] подачи первой(ых) заявки(ок) в государстве-участнике Парижской конвенции (31) Номер первой(ых) заявки(ок) (32) Дата подачи первой(ых) заявки(ок) (33) Код страны 1. 1308933.9 17.05.2013 ОВ Название изобретения (полезной модели): [Х] - как заявлено; [ ] - уточненное (см. Примечания) Композиция, содержащая гидрокортизон Заявитель: ДАЙЭРНАЛ ЛИМИТЕД, СВ 2. ЕДИНСТВО ИЗОБРЕТЕНИЯ [Х] соблюдено [ ] не соблюдено. Пояснения: см. Примечания 3. ФОРМУЛА ИЗОБРЕТЕНИЯ: [Х] приняты во внимание все пункты см. п см. Примечания [ ] приняты во внимание следующие пункты: [ ] принята во внимание измененная формула изобретения (см. Примечания) 4. КЛАССИФИКАЦИЯ ОБЪЕКТА ИЗОБРЕТЕНИЯ (ПОЛЕЗНОЙ МОДЕЛИ) (Указываются индексы МПК и индикатор текущей версии) Аб/1К 9/50 (2006.01) Аб/1К 31/573 (2006.01) Аб1К 47/00 (2006.01) Аб1Р 5/38 (2006.01) 5. ОБЛАСТЬ ПОИСКА 5.1 Проверенный минимум документации РСТ (указывается индексами МПК) Аб1К 9/00, 9/50, Аб1К 31/00, 31/573, Аб1К 47/00, Аб1Р 5/00, 5/38 5.2 Другая проверенная документация в той мере, в какой она включена в поисковые подборки: 5.3 Электронные базы данных, использованные при поиске (название базы, и если, возможно, поисковые термины): Свет ШОр/а$, Езрасепе боозе, РАТЕМТСОРЕ, Раеагсв, РаБСвет, РиБМеа, КОРТО, ОРТО, БД ВИНИТИ 6. ДОКУМЕНТЫ, ОТНОСЯЩИЕСЯ К ПРЕДМЕТУ ПОИСКА Кате- Наименование ...

Cfr1 receptor antagonists for treating congenital adrenal hyperplasia

FIELD: medicine; therapy; endocrinology. SUBSTANCE: present group of inventions concerns treating congenital hyperplasia of adrenal glands. That is ensured by administering an effective amount of CRF 1 receptor antagonist with a half-dissociation period of more than 50 minutes, specifically compound of 2,5-dimethyl-3-[2-methyl-4-(methyloxy)phenyl-]N-[(1S)-1-(3-methyl-1,2,4-oxadiazol-5-yl)propyl]pyrazolo-[1,5-a]pyrimidin-7-amine (NBI-77860) or 4-(2-chloro-4-methoxy-5-methylphenyl)- N -[(1 S )-2-cyclopropyl-1-(3-fluoro-4-methylphenyl)ethyl]-5-methyl- N -(2-propyn-1-yl)-2-thiazolamine (SSR-125543). EFFECT: this allows correcting the levels of hormones included in the "hypothalamic-pituitary axis", in particular 17-hydroxyprogesterone and ACTH, and thus providing normalization of androgen formation with using lower, more physiological doses of hydrocortisone, thereby reducing treatment-related side effects. 6 cl, 6 dwg, 2 tbl, 6 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2 718 918 C2 (51) МПК A61K 31/427 (2006.01) A61P 5/38 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ (52) СПК A61K 31/427 (2020.01); A61P 5/38 (2020.01) (21)(22) Заявка: 2016133972, 21.01.2015 (24) Дата начала отсчета срока действия патента: (73) Патентообладатель(и): НЬЮРОКРАЙН БАЙОСАЙЕНСИЗ, ИНК. (US) Дата регистрации: 15.04.2020 21.01.2014 US 61/929,941; 17.04.2014 US 61/981,033; 27.10.2014 US 62/069,155 (43) Дата публикации заявки: 05.03.2018 Бюл. № 7 (45) Опубликовано: 15.04.2020 Бюл. № 11 (56) Список документов, цитированных в отчете о поиске: US 2010222339 A1 02.09.2010. Tellew J.E. et al. "Discovery of NBI-77860/GSK561679, a potent corticotrophin-releasing factor (CRF1)receptor antagonist with imoroved pharmacokinetic properties". Bioorganic& Medicinal Chemistry Letters 20(2010)7259-7264. М.Ф.ЛОГАЧЕВА и др. "Врожденная гиперплазия надпочечников: современные проблемы терминологии и (см. прод.) C 2 C 2 (85) Дата начала рассмотрения заявки ...

Genes associated with diseases of the kidney

The invention provides novel kidney disease-associated genes and polypeptides encoded by those genes. The invention also provides expression vectors, host cells, and antibodies. The invention also provides methods for diagnosing, treating or preventing diseases of the kidney.

Aminothiazole derivative, method for producing the same, and pharmaceutical composition containing the same

Production of novel steroid derivatives

Methods for treating inflammation-mediated conditions of the eye

Methods for treating inflammation-mediated conditions of the eye are described, comprising: implanting into the vitreous of the eye of an individual a bioerodible implant comprising a steroidal anti-inflammatory agent and a bioerodible polymer, wherein the implant delivers the agent to the vitreous in an amount sufficient to reach a concentration equivalent to at least about 0.05 mug/ml dexamethasone within about 48 hours and maintains a concentration equivalent to at least about 0.03 mug/ml dexamethasone for at least about three weeks.

Fluorine-containing vitamin d derivative

(57)【要約】本公報は電子出願前の出願データであるた め要約のデータは記録されません。

Process for preparing derivatives of thioethyanic acid

Thio etianic acid derivatives of the formula wherein X' is hydrogen, fluoro, or chloro; X 2 is hydrogen, fluoro, chloro or bromo; X 3 is =C=O Cl may also be =C when X 2 is chloro; H R is alkyl of 1 to 6 carbon atoms, or phenyl or benzyl optionally substituted with a substituent on the phenyl ring which is alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon _ atoms or halo; R 1 is hydrogen or alkanoyl of 2 to 6 carbon atoms when R 2 is hydrogen, a-methyl or β-methyl or OR 1 and R 2 together are 16a, 17a-isopropylidenedioxy; and the solid and broken lines between C-1 and C-2 represent a double or single bond; are useful an anti-inflammatory steroids. They can be prepared by reacting the corresponding 17β-carboxylic acid or a reactive derivative thereof with an alkali metal salt of RSH.

Method of producing derivatives of 2,2-dialkyl-18,19-dinopregn-4-en-3,20-dion

Patent RU2016133972A3

`”ВУ“” 2016133972” АЗ Дата публикации: 26.09.2018 Форма № 18 ИЗ,ПМ-2011 Федеральная служба по интеллектуальной собственности Федеральное государственное бюджетное учреждение «Федеральный институт промышленной собственности» ж 9 (ФИПС) ОТЧЕТ О ПОИСКЕ 1. . ИДЕНТИФИКАЦИЯ ЗАЯВКИ Регистрационный номер Дата подачи 2016133972/15(052/775) 21.01.2015 РСТ/О$2015/012315 21.01.2015 Приоритет установлен по дате: [ ] подачи заявки [ ] поступления дополнительных материалов от к ранее поданной заявке № [ ] приоритета по первоначальной заявке № из которой данная заявка выделена [ ] подачи первоначальной заявки № из которой данная заявка выделена [ ] подачи ранее поданной заявки № [Х] подачи первой(ых) заявки(ок) в государстве-участнике Парижской конвенции (31) Номер первой(ых) заявки(ок) (32) Дата подачи первой(ых) заявки(ок) (33) Код страны 1. 61/929,941 21.01.2014 05 2. 61/981,033 17.04.2014 05 3. 62/069,155 27.10.2014 05 Название изобретения (полезной модели): [Х] - как заявлено; [ ] - уточненное (см. Примечания) АНТАГОНИСТЫ РЕЦЕПТОРА СЕК1 ДЛЯ ЛЕЧЕНИЯ ВРОЖДЕННОЙ ГИПЕРПЛАЗИИ КОРЫ НАДПОЧЕЧНИКОВ Заявитель: НЬЮРОКРАИН БАЙОСАИЙЕНСИЗ, ИНК.., 0$ 2. ЕДИНСТВО ИЗОБРЕТЕНИЯ [Х] соблюдено [ ] не соблюдено. Пояснения: см. Примечания 3. ФОРМУЛА ИЗОБРЕТЕНИЯ: [Х] приняты во внимание все пункты (см. Примечания) [ ] приняты во внимание следующие пункты: [ ] принята во внимание измененная формула изобретения (см. Примечания) 4. КЛАССИФИКАЦИЯ ОБЪЕКТА ИЗОБРЕТЕНИЯ (ПОЛЕЗНОЙ МОДЕЛИ) (Указываются индексы МПК и индикатор текущей версии) Аб/1К 31/427 (2006.01) Аб1Р 5/38 (2006.01) 5. ОБЛАСТЬ ПОИСКА 5.1 Проверенный минимум документации РСТ (указывается индексами МПК) Аб1К 31/427 АБР 5/38 5.2 Другая проверенная документация в той мере, в какой она включена в поисковые подборки: 5.3 Электронные базы данных, использованные при поиске (название базы, и если, возможно, поисковые термины): ЕАРАТБ, Езрасепе, Соозе, Раеагсв, РиБСВет, РиБМеча, КОРТО, БД "Российская медицина", БД ВИНИТИ, РМЖ 6. ДОКУМЕНТЫ, ОТНОСЯЩИЕСЯ ...

Method of preparing derivatives of steroidspiroxyzolidinone

Diuretic pharmaceutically active steroid-spiro-oxazolidinone compounds of the formula (I), <IMAGE> (I) wherein R1 is hydrogen or methyl, R2 is C1-4 alkyl, R3 is hydrogen, C1-4 alkyl or C2-4 alkenyl, Z1 and Z2 each are hydrogen or together form a second valence bond, or Z1 is hydrogen and Z2 is R4-S-, Z3 and Z4 each are hydrogen or together form a second valence bond, or Z3 is hydrogen and Z4 is R4-S-, with at least one of the pairs Z1-Z2 and Z3-Z4 representing hydrogen and an R4-S- group, and R4 is hydrogen or alkyl, alkenyl, aralkyl or acyl with up to 7 carbon atoms, provided that when Z1 and Z2 together form a valence bond, or Z1 represents a hydrogen atom and Z2 and R4-S- group then R1 is methyl.

Method of preparing pregnane derivatives

19-Oxygenated steroid compounds of the pregnane series of the formula I <IMAGE> (I) in which R1 represents a hydrogen atom, and R2 represents an alpha -oriented lower alkanoylthio group, or R1 and R2 together represent a carbon-carbon bond or an alpha -or beta -oriented methylene radical, R3 represents a free hydroxymethyl group or a hydroxymethyl group etherified by a lower alkyl or esterified by a lower alkanoyl; or represents a formyl group, a carboxyl group or a lower alkoxycarbonyl group, and R4 represents a hydrogen atom or the acyl radical Ac of a carboxylic acid, and corresponding 1,2-dehydro derivatives have valuable aldosterone-antagonizing properties with a minimum effect on sexual functions. As the compounds reduce the excessive sodium retention and potassium excretion induced by aldosterone, they are especially useful as the active ingredient in pharmaceutical preparations for alleviating diseases involving hyperaldosteronismus in man and other warm-blooded animals.

Method of preparing spirolactones

Aqueous suspensions of ciclesonide for nebulisation

本发明涉及通过使用湿热灭菌制备环索奈德的无菌水混悬液的方法。本发明进一步涉及药物组合物，特别涉及在预防和/或治疗呼吸系统疾病中通过雾化给药的环索奈德无菌水混悬液。

Hydrocortisone Composition

РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2015 150 303 A (51) МПК A61K 9/50 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ЗАЯВКА НА ИЗОБРЕТЕНИЕ (21)(22) Заявка: 2015150303, 12.05.2014 (71) Заявитель(и): ДАЙЭРНАЛ ЛИМИТЕД (GB) Приоритет(ы): (30) Конвенционный приоритет: 17.05.2013 GB 1308933.9 (85) Дата начала рассмотрения заявки PCT на национальной фазе: 17.12.2015 R U (43) Дата публикации заявки: 22.06.2017 Бюл. № 18 (72) Автор(ы): ХЬЮТАН Хип (GB), РОСС Ричард (GB), УИТАКЕР Мартин (GB), ПЁЛЛИНГЕР Норберт (DE), ГРАФЕ Аннетте (DE) (86) Заявка PCT: (87) Публикация заявки PCT: WO 2014/184525 (20.11.2014) R U (54) Композиция, содержащая гидрокортизон (57) Формула изобретения 1. Фармацевтическая композиция для перорального введения, которая содержит носитель в виде микрочастиц, содержащий эффективное количество гидрокортизона и связывающий агент, и соприкасающийся с указанным носителем в виде микрочастиц изолирующий полимерный слой, который отделяет носитель в виде микрочастиц и маскирующий вкус полимерный слой. 2. Композиция по п. 1, где указанное эффективное количество гидрокортизона составляет от примерно 0,25 мг масс./масс. до 30 мг масс./масс. гидрокортизона на стандартную дозу. 3. Композиция по п. 2, где указанное эффективное количество составляет примерно 0,25 мг масс./масс., 0,5 мг масс./масс., 1,0 мг масс./масс., 2,0 мг масс./масс., 5,0 мг масс./ масс., 10 мг масс./масс., 20 мг масс./масс., или 30 мг масс./масс., на стандартную дозу. 4. Композиция по п. 1, где указанный носитель содержит частицы микрокристаллической целлюлозы, диаметр которых составляет от 350 до 500 мкм. 5. Композиция по п. 4, где диаметр указанных частиц выбран из группы, состоящей из 350 мкм, 375 мкм, 400 мкм, 425 мкм, 450 мкм, 475 мкм или 500 мкм. 6. Композиция по п. 1, где связывающий агент составляет от 0,60 до 0,70% масс./масс. композиции. 7. Композиция по п. 6, где связывающий агент составляет примерно 0,66% масс./масс. композиции. 8. Композиция по п. 1, где ...

COMPOUNDS FOR ASSOCIATIVE SYNTHESIS OF SULFUR OR NON-SULFUR AMINO ACIDS WITH D-4 PREGNENE 3,20-DIONE DERIVATIVES OR WITH D-1,4 PREGNADIENE 3,20-DIONE DERIVATIVES WITH GLUCOCORTICOID AND ANTI-INFLAMMATORY PROPERTIES, METHODS OBTAINED, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM. PHARMACOLOGICAL PROPERTIES AND APPLICATIONS

Spirolactone producing method

New spirolactones of the formula <IMAGE> (I) wherein <IMAGE> +tr <IMAGE> R is a lower alkyl of up to 5 carbon atoms, and <IMAGE> +tr <IMAGE>

14β-H-, 14- and 15-ene-11β-aryl-4-estrene

Spirocyclic piperidine melanocortin subtype-2 receptor (MC2R) antagonists and uses thereof

【解決手段】本明細書にはメラノコルチンサブタイプ－２受容体（ＭＣ２Ｒ）モジュレーターである化合物、上記化合物を作る方法、上記化合物を含む医薬組成物と製剤、およびＭＣ２Ｒ活性の調節から利益を得ることになる疾病、疾患、または障害の処置において上記化合物を使用する方法が記載されている。【選択図】なし

Two chamber cartridge for atomizers

Die vorliegende Erfindung betrifft eine Vorrichtung bestehend aus einer Verschlußkappe und einem Behälter in Form einer Zweikammer-Kartusche, in der ein Wirkstoff und ein Lösungsmittel bis zur Verwendung der Vorrichtung in einem Vernebler getrennt gelagert werden können, sowie ein Wirkstoffkonzentrat, in der der Wirkstoff zum Zweck der Lagerung als Lösung oder Suspension vorliegt.

Two-chamber cartridge for atomizers

The present invention relates to a device consisting of a closing cap (3) and a container (2) in the form of a two-chamber cartridge in which an active substance and a solvent can be stored separately untill the device is used in an atomizer. A chamber (17), containing a concentrate of an active substance is formed in cap (3), in which the active substance used for storing is present as a solution or suspension.

Two-chamber cartridge for vaporizers

Eldeki bulus, bir kapak ile iki hazneli kartustan meydana gelen bir tertibati konu almakta olup, bu tertibat içerisinde bir etken madde ve bir çözücü madde, tertibat kullanilana kadar bir vaporizatör içerisinde birbirinden ayri yerlerde muhafaza edilebilmekte ve bu bulus ayni zamanda içindeki etken maddenin, muhafaza amaçli olarak çözelti veya süspansiyon halinde bulundugu bir etken madde konsantresini de ele almaktadir. The present invention is based on a device consisting of a lid and a two-chamber cartridge, in which an active substance and a solvent can be stored separately in a vaporizer until the device is used, and the present invention is also intended for storage purposes. It also deals with an active substance concentrate in which it is in solution or suspension.

The CRF for the treatment of adrenal,congenital hyperplasia1receptor antagonist

CRF 1 受体拮抗剂可能直接抑制患有CAH的患者的ACTH释放，从而在使用多个较低生理剂量的氢化可的松时，使雄激素的产生正常化，并且因此减少治疗相关的副作用。

Two-chamber cartridge for nebulizer

Patente de Invenção: <B>"CARTUCHO DE DUAS CâMARAS PARA NEBULIZADOR"<D>. A presente invenção refere-se a um aparelho que compreende uma tampa de fechamento e um recipiente na forma de um cartucho de duas câmaras no qual um ingrediente ativo e um solvente podem ser armazenados em separado até que o aparelho seja usado em um nebulizador, assim como um concentrado de substância ativa, no qual a substância ativa está presente como uma solução ou suspensão para fins de armazenagem.

Manufacture of 16alpha-hydroxy-17alpha- aminopregnane derivatives

2-(3-pyridinyl)-1h-benzimidazole derivative compound and medicine containing same

Provided is a compound represented by general formula (1) or a salt thereof as well as a medicine containing the compound or the salt. (In the formula, R 1 represents a hydrogen atom or CO 2 R a ; R 2 represents a hydrogen atom, a halogen atom, or CO 2 R a ; R 3 represents a hydrogen atom or a C1-10 hydroxyalkyl group; R 4 represents a hydrogen atom, a hydroxy group, or a C1-10 alkoxy group; R 5 represents a C1-5 chain alkyl group in which the hydrogen atoms are optionally substituted with halogen atoms, a C3-5 cyclic alkyl group in which the hydrogen atoms are optionally substituted with halogen atoms, a C1-5 hydroxyalkyl group, or an o-, p-, or m-halobenzyl group; A represents CH or a nitrogen atom; X 1 and X 3 independently represent hydrogen atoms or halogen atoms; X 2 represents a hydrogen atom, a halogen atom, or a nitrile group; at least one of X 1 , X 2 , and X 3 represents a halogen atom; and R a independently represents a C1-10 alkyl group.)

PROCESS FOR PREPARING STEROIDIC COMPOUNDS OXYGENATED IN 19

La présente invention concerne la préparation de stéroïdes. Il s'agit d'un procédé de préparation de composés stéroïdiques oxygènes en 19 de la série des prégnanes de formule :

Method of producing 9-chloroprednisolone derivatives

Derivatives of 9-chloroprednisolone of the formula <IMAGE> in which R1 is alkanoyl with 1 to 8 carbon atoms or benzoyl, and X is fluorine, chlorine, hydroxyl, alkanoyloxy with 1 to 8 carbon atoms or benzoyloxy, are prepared. These compounds are obtained by adding HOCl onto the corresponding DELTA <9,11>-prednisolones. The compounds can be used for the treatment of inflammations.

METHODS FOR THE PREPARATION OF 16A-HYDROXY-17A-AMINOPREGNANE DERIVATIVES, USEFUL FOR THE SYNTHESIS OF OXAZOLINES, AND SUBSTANCES OBTAINED THEREFROM

PROCEDE POUR LA PREPARATION DE DERIVES DE 16A-HYDROXY-17A-AMINOPREGNANE PAR OUVERTURE DES 16A, 17A-EPOXYDES CORRESPONDANTS AVEC LES AMINES; LES COMPOSES AINSI OBTENUS SONT INTERESSANTS A UTILISER COMME PRODUITS INTERMEDIAIRES EN VUE DE LA SYNTHESE DE PREGNANO17A, 16A-D OXAZOLINES PHARMACOLOGIQUEMENT ACTIVES. PROCESS FOR THE PREPARATION OF 16A-HYDROXY-17A-AMINOPREGNANE DERIVATIVES BY OPENING THE 16A, 17A-EPOXIDES CORRESPONDING WITH THE AMINES; THE COMPOUNDS SO OBTAINED ARE INTERESTING TO USE AS INTERMEDIATE PRODUCTS FOR THE SYNTHESIS OF PREGNANO17A, 16A-D PHARMACOLOGICALLY ACTIVE OXAZOLINES.

Delayed and sustained drug release

The invention relates to the controlled release of preparations of therapeutic agents, for example a steroid; formulations comprising said preparations; and the use of said formulations to treat diseases such as those diseases which would benefit from steroid treatment.

NEW PRODUCTS DERIVED FROM THE STRUCTURE 3-CETO 4,9 19-NOR STEROIDS, THEIR PREPARATION PROCESS AND THEIR APPLICATION AS MEDICAMENTS

Patent FR2408623B1

Patent FR2366313B1

STEROIDIC SPIROLACTONS AND MEDICINAL PRODUCTS CONTAINING IT

Spirolactones stéroïdiques. Elles répondent à la formule : Steroidal spirolactones. They respond to the formula:

COMPOUNDS OF THE PREGNANES SERIES WITH AN OXYGEN FUNCTION IN POSITION 19, PROCESS OF PREPARATION AND PHARMACEUTICAL PREPARATIONS WHICH CONTAIN THESE COMPOUNDS

L'invention concerne des médicaments nouveaux. Il s'agit, à titre de médicament nouveau, d'un composé de formule I : The invention relates to novel drugs. It is, as a new drug, a compound of formula I:

Patent FR2494699B1

Branched alkylamino thiazole derivatives, processes for their preparation and pharmaceutical compositions containing them.

Pharmaceutical formulations containing relacorilant, a heteroaryl-ketone fused azadecalin compound

Disclosed herein are novel formulations containing relacorilant ((R)-(1-(4-fluorophenyl)-6-((1-methyl-1H-pyrazol-4-yl)sulfonyl)-4,4a,5,6,7,8-hexahydro-1H-pyrazolo[3,4-g]isoquinolin-4a-yl)(4-(trifluoromethyl)pyridin-2-yl)methanone) that are suitable for administration, including oral administration, to patients suffering from disorders amenable to treatment by glucocorticoid receptor modulators (GRMs). Single unit dosage forms comprise softgel capsules containing these formulations. Such softgel capsules may contain, e.g., relacorilant formulations containing 25 milligrams (mg), 50 mg, 100 mg, 200 mg, 300 mg, 400 mg, 500 mg, or other amounts of relacorilant. These novel formulations and single unit dosage forms may be used to treat diseases and disorders including Cushing's syndrome, Cushing's Disease, and other disorders.

NOVEL 11B SUBSTITUTED STEROID DERIVATIVES, THEIR PREPARATION PROCESS AND THEIR APPLICATION AS MEDICAMENTS

NOVEL 11B SUBSTITUTED STEROID DERIVATIVES, THEIR PREPARATION PROCESS AND THEIR APPLICATION AS MEDICAMENTS

LA PRESENTE DEMANDE DE PREMIER CERTIFICAT D'ADDITION A POUR OBJET D'ILLUSTRER PAR DE NOUVEAUX EXEMPLES LA FORMULE I DU BREVET PRINCIPAL. LA PRESENTE DEMANDE CONCERNE NOTAMMENT LA 11B-4-(DIMETHYLAMINO) PHENYL17B-HYDROXY 17A-(3-HYDROXY PROP-1-YNYL) ESTRA 4,9-DIEN 3-ONE. THIS APPLICATION FOR FIRST CERTIFICATE OF ADDITION IS INTENDED TO ILLUSTRATE WITH FORMER EXAMPLES FORM I OF THE MAIN PATENT. THIS APPLICATION RELATES IN PARTICULAR TO 11B-4- (DIMETHYLAMINO) PHENYL17B-HYDROXY 17A- (3-HYDROXY PROP-1-YNYL) ESTRA 4.9-DIEN 3-ONE.

Production of steroidal pylols

AMINOTHIAZOLE DERIVATIVES, PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME

The invention concerns compounds of formula (I) in which R1, R2, R3, R4, R5 and R6 are such as defined in claim 1. The compounds have a strong affinity for CRF receptors.

Patent FR2481279B1

Method of solidification using anti-solvent

FIELD: chemistry. SUBSTANCE: according to novel method liquid medium, containing at least one dissolved organic or inorganic compound, which is subject to solidification, is forced through membrane into one or several anti-solvents, or one or few anti-solvents are forced through membrane into liquid medium, which contains at least one organic or inorganic compound. Membrane is located in membrane module, has pores with size to 3mcm, membrane form is selected from pipe, fibre or spiral winding. Method is realised as continuous process. Method ensures obtaining solid particles, which include organic or inorganic compound, which are non - agglomerated. Method can be used for large volumes and allows controlling particle size. EFFECT: obtaining possibility of application for large volumes and ensuring control of particle size. 15 cl, 2 dwg, 2 tbl, 5 ex ÐÎÑÑÈÉÑÊÀß ÔÅÄÅÐÀÖÈß RU (19) (11) 2 339 364 (13) C2 (51) ÌÏÊ A61K A61K B01D B01J 9/14 (2006.01) 9/16 (2006.01) 9/02 (2006.01) 2/06 (2006.01) ÔÅÄÅÐÀËÜÍÀß ÑËÓÆÁÀ ÏÎ ÈÍÒÅËËÅÊÒÓÀËÜÍÎÉ ÑÎÁÑÒÂÅÍÍÎÑÒÈ, ÏÀÒÅÍÒÀÌ È ÒÎÂÀÐÍÛÌ ÇÍÀÊÀÌ (12) ÎÏÈÑÀÍÈÅ ÈÇÎÁÐÅÒÅÍÈß Ê ÏÀÒÅÍÒÓ (21), (22) Çà âêà: 2005136983/15, 28.04.2004 (24) Äàòà íà÷àëà îòñ÷åòà ñðîêà äåéñòâè ïàòåíòà: 28.04.2004 (30) Êîíâåíöèîííûé ïðèîðèòåò: 29.04.2003 US 60/466,761 (43) Äàòà ïóáëèêàöèè çà âêè: 20.03.2006 (73) Ïàòåíòîîáëàäàòåëü(è): Í.Â.ÎÐÃÀÍÎÍ, NL (NL) (45) Îïóáëèêîâàíî: 27.11.2008 Áþë. ¹ 33 2 3 3 9 3 6 4 (56) Ñïèñîê äîêóìåíòîâ, öèòèðîâàííûõ â îò÷åòå î ïîèñêå: US 6221398 Â1, 24.04.2001. WO 03/032951 À1, 24.04.2003. RU 2026670 Ñ1, 20.01.1995. RU 2136665 Ñ1, 10.09.1999. (85) Äàòà ïåðåâîäà çà âêè PCT íà íàöèîíàëüíóþ ôàçó: 29.11.2005 2 3 3 9 3 6 4 R U (87) Ïóáëèêàöè PCT: WO 2004/096405 (11.11.2004) C 2 C 2 (86) Çà âêà PCT: EP 2004/004506 (28.04.2004) Àäðåñ äë ïåðåïèñêè: 129090, Ìîñêâà, óë. Á.Ñïàññêà , 25, ñòð.3, ÎÎÎ "Þðèäè÷åñêà ôèðìà Ãîðîäèññêèé è Ïàðòíåðû", ïàò.ïîâ. Å.Å.Íàçèíîé, ðåã. ¹ 517 (54) ÑÏÎÑÎÁ ÇÀÒÂÅÐÄÅÂÀÍÈß Ñ ÏÐÈÌÅÍÅÍÈÅÌ ÀÍÒÈÐÀÑÒÂÎÐÈÒÅËß (57) Ðåôåðàò: Ñîãëàñíî íîâîìó ...

PHARMACEUTICAL COMPOSITION CONSTITUTED ON THE ONE HAND, AS ACTIVE INGREDIENT, BY 9A, 11B-DICHLORO 16A-METHYL 21-OXYCARBONYLDICYCLOHEXYL METHYLOXY PREGNA-1,4-DIENE 3,20-DIONE AND ON THE OTHER HAND, BY A PHARM EXCIPIENT INERTE CAPABLE OF ALLOWING THE ACTION OF THE PRODUCT IN THE RECTUM OR THE COLON

PHARMACEUTICAL SOLUTION OF HYDROCORTISONE FOR INJECTION DEVICE

Branched alkylamino derivatives of thiazole, processes for their preparation and pharmaceutical compositions containing them

L'invention a pour objet, les dérivés de formule I: (CF DESSIN DANS BOPI) dans laquelle, R1 représente un radical phényle ou naphtyle (éventuellement substitués), R2 représente un atome d'hydrogène, d'halogène, un radical alkyle, hydroxyméthyle ou formyle, R3 représente un radical alkyle, cycloalkyle, alcényle, cycloalkyl alkyle, ou phényle, R4 représente un atome d'hydrogène, un radical alkyle, cycloalkyle, ou cycloalkyl alkyle, R5 représente un radical alkyle, cycloalkyle, cycloalkyl alkyle, alcényle ou un radical de formule B: (CF DESSIN DANS BOPI) (p = 0, 1, 2, ou 3), R6 représente un radical phényle, pyridyle, imidazolyle, pyrrolyle, thiènyle, furyle éventuellement substitués, ou un radical cycloalkyle, m, n, identiques ou différents représentent chacun 0 ou 1, leurs stéréoisomères et leurs sels d'addition. Médicaments. The subject of the invention is the derivatives of formula I: (CF DRAWING IN BOPI) in which, R1 represents a phenyl or naphthyl radical (optionally substituted), R2 represents a hydrogen or halogen atom, an alkyl radical, hydroxymethyl or formyl, R3 represents an alkyl, cycloalkyl, alkenyl, cycloalkyl alkyl or phenyl radical, R4 represents a hydrogen atom, an alkyl, cycloalkyl or cycloalkyl alkyl radical, R5 represents an alkyl, cycloalkyl, cycloalkyl alkyl, alkenyl radical or a radical of formula B: (CF DRAWING IN BOPI) (p = 0, 1, 2, or 3), R6 represents a phenyl, pyridyl, imidazolyl, pyrrolyl, thienyl, furyl, optionally substituted, or a cycloalkyl radical, m , n, identical or different each represent 0 or 1, their stereoisomers and their addition salts. Medicines.

Patent FR2374037B1

6,6-ETHYLENE-15,16-METHYLENE-3-OXO-17.alpha.-PREGN-4-ENE- 21,17-CARBOLACTONES, PROCESSES FOR THE PRODUCTION THEREOF AND PHARMACEUTICAL PREPARATIONS CONTAINING THEM

Abstract 6,6-ethylene-15,16-methylene-3-oxo-17.alpha.-pregn-4-ene-21,17.alpha.-carbolactones of general Formula I (I) wherein is a CC-single of CC-double bond, R1 is a hydrogen atom or a methyl group, R2 is a methyl or ethyl group, and is or

Application of Bexarotene in preparation of anti-pituitary adrenocorticotropic hormone adenoma medicine

本发明公开了蓓萨罗丁在制备抗垂体促肾上腺皮质激素腺瘤药物制备中的应用，垂体促肾上腺皮质激素腺瘤使病人长期过度分泌促肾上腺皮质激素(ACTH)，刺激肾上腺分泌大量皮质醇，导致病人出现向心性肥胖、骨质疏松、肌肉萎缩、性功能障碍、高血压、失眠等症状，属罕见病。本发明发现，蓓萨罗丁能显著抑制肿瘤生长，并抑制ACTH分泌和其前体POMC的表达。蓓萨罗丁可用于制备抗垂体促肾上腺皮质激素腺瘤药物，减少不良反应，为疾病的治疗和预防提供一种安全、有效、经济的解决办法。

BENZENESULFONAMIDE DERIVATIVES, THEIR PREPARATION AND THERAPEUTIC USE THEREOF

Dérivés de benzènesulfonamide de formule générale (I): (CF DESSIN DANS BOPI) dans laquelle: R1 représente un atome d'hydrogène ou d'halogène, tel que chlore ou fluor, ou un groupe C1-4 alkyle ou C1-4 alcoxy, linéaire ou ramifié, et R2 , R3 et R4 représentent, indépendamment les uns des autres, des atomes d'hydrogène ou des groupes C1-4 alkyle linéaire, ramifié ou cyclique. Application en thérapeutique.

CORTICOSTEROIDS AND MEDICINAL PRODUCTS CONTAINING THEM

Nouveaux corticostéroïdes. Ils répondent à la formule New corticosteroids. They answer the formula

Patent FR2421912B1

PREDNISOLONE 9-CHLORO DERIVATIVES AND MEDICINAL PRODUCTS CONTAINING IT

Dérivés de la chloro-9 prednisolone. Ils répondent à la formule : Derivatives of 9-chloro prednisolone. They answer the formula:

11B-SUBSTITUTED STEROIDS ESPECIALLY USEFUL IN THE TREATMENT OF HORMONO-DEPENDENT TUMORS AND METHOD FOR THE PRODUCTION THEREOF

NOVEL GALENIC FORMS OF CORTICOIDS FOR PER- AND SUBLINGUAL ADMINISTRATION AND THEIR PREPARATION PROCESS

Liposomes containing steroid esters

ABSTRACT Pharmaceutical composition for administration primarily to the respiratory tract when treating and controlling anti-inflammatory conditions comprising liposomes in combination with a compound of the formula I wherein Q is and R1 is a saturated or unsaturated, straight or branched alkyl group with 11-l9 carbon atoms and R is H, -COCH3, -COC2H5, -CO(CH2)2CH3 or -CO(CH2)3CH3. The invention also refers to the compounds of the formula I per se processes for preparation of these compounds and to a method for the treatment of inflammatory conditions.

PHARMACEUTICAL SOLUTION OF HYDROCORTISONE FOR INJECTION DEVICE

L'invention concerne une solution pharmaceutique d'hydrocortisone qui comprend au moins : - de l'hydrocortisone ou un sel pharmaceutiquement acceptable de celle-ci ; - de la rongalite ; - de l'EDTA disodique ; - un solvant. L'invention a aussi pour objet son utilisation dans le traitement de l'insuffisance surrénalienne aigüe et de l'asthme. L'invention concerne également un dispositif d'injection rempli de cette solution pharmaceutique. The invention relates to a pharmaceutical hydrocortisone solution which comprises at least: - hydrocortisone or a pharmaceutically acceptable salt thereof; - rongalite; disodium EDTA; a solvent. The invention also relates to its use in the treatment of acute adrenal insufficiency and asthma. The invention also relates to an injection device filled with this pharmaceutical solution.

11 beta -Substituted steroids useful especially in the treatment of hormone-dependent tumours and process for producing them

The 11 beta -substituted steroids according to the invention are 3-oxo or 3-methylene-4(5),9(10)-estradienes of general formula I: Applications: Pharmaceutical compositions in human and veterinary medicine especially as antiprogesterone and antiglucocorticoid agents and in the treatment of hormone-dependent tumours.

Patent FR2510584A1

UN COMPOSE, QUI PRESENTE UNE ACTIVITE ANTI-ALDOSTERONE AMELIOREE, A LA FORMULE: (CF DESSIN DANS BOPI) OU X EST UN ATOME D'HYDROGENE OU UN ATOME D'HALOGENE, Y EST UN GROUPE ACETYLTHIO, UN GROUPE CARBOXY OU CARBOXY ESTERIFIE, UN GROUPE ALKYLE INFERIEUR OU UN ATOME D'HALOGENE, Y EST UN ATOME D'HYDROGENE OU UN ATOME D'HALOGENE, Z EST UN GROUPE HYDROXY ET Z EST UN GROUPE DE FORMULE: -CHCHCOOM (OU M EST LE POTASSIUM OU LE SODIUM), OU, QUAND Z ET Z SONT PRIS AVEC L'ATOME DE CARBONE ADJACENT AUQUEL ILS SONT FIXES, ILS REPRESENTENT UN NOYAU DE G-LACTOME AYANT LA FORMULE: (CF DESSIN DANS BOPI) ET LES LIGNES EN POINTILLE ENTRE LES POSITIONS 1 ET 2 ET ENTRE LES POSITIONS 6 ET 7 REPRESENTENT DES DOUBLES LIAISONS QUI PEUVENT ETRE PRESENTES DE MANIERE FACULTATIVE. A COMPOUND, WHICH SHOWS AN IMPROVED ANTI-ALDOSTERONE ACTIVITY, WITH THE FORMULA: (CF DRAWING IN BOPI) OR X IS A HYDROGEN ATOM OR A HALOGEN ATOM, Y IS AN ACETYLTHIO GROUP, AN ESTERIFIED CARBOXY OR CARBOXY GROUP, A LOWER ALKYL GROUP OR A HALOGEN ATOM, Y IS A HYDROGEN ATOM OR A HALOGEN ATOM, Z IS A HYDROXY GROUP AND Z IS A GROUP OF THE FORMULA: -CHCHCOOM (OR M IS POTASSIUM OR SODIUM) , OR, WHEN Z AND Z ARE TAKEN WITH THE ADJACENT CARBON ATOM TO WHICH THEY ARE ATTACHED, THEY REPRESENT A G-LACTOME CORE WITH THE FORMULA: (CF DRAWING IN BOPI) AND THE DOT LINES BETWEEN POSITIONS 1 AND 2 AND BETWEEN POSITIONS 6 AND 7 REPRESENT DOUBLE LINKS WHICH CAN BE PRESENTED ON AN OPTIONAL WAY.

STEROID COMPOUNDS OXYGENATED IN 19

LA PRESENTE INVENTION CONCERNE DES COMPOSES CHIMIQUES NOUVEAUX. IL S'AGIT DE COMPOSES STEROIDIQUES OXYGENES EN 19 DE LA SERIE DES PREGNANES DE FORMULE IA: (CF DESSIN DANS BOPI) OU R REPRESENTE UN ATOME D'HYDROGENE ET R UN GROUPE ALCANOYLE INFERIEUR-THIO ORIENTE EN A, OU R ET R REPRESENTENT ENSEMBLE UNE LIAISON CARBONE-CARBONE OU UN RADICAL METHYLENE ORIENTE EN A OU B, R UN GROUPE HYDROXYMETHYLE LIBRE OU ETHERIFIE PAR UN ALCOYLE INFERIEUR OU ESTERIFIE PAR UN ALCANOYLE INFERIEUR, UN GROUPE CARBOXYLE OU UN GROUPE ALCOXY INFERIEUR-CARBONYLE, ET R REPRESENTE UN ATOME D'HYDROGENE OU LE RADICAL ACYLE D'UN ACIDE CARBOXYLIQUE AC, AINSIQUE LES DERIVES 1,2-DEHYDRO DE CES CORPS ET LES SELS DE TOUS LES COMPOSES CORRESPONDANTS AYANT UN GROUPE CARBOXYLE LIBRE. CES COMPOSES SONT UTILES COMME MEDICAMENTS.

STEROIDS OF THE TYPE (16, 17-A) CYCLOPENTANOPREGNENES AND THEIR THERAPEUTIC USES, IN PARTICULAR AS ANTI-INFLAMMATORY AGENTS

LES STEROIDES REPONDANT A LA FORMULE: (CF DESSIN DANS BOPI) ET LEURS DERIVES 1,2 DESHYDROGENES DANS THE STEROIDS RESPONDING TO THE FORMULA: (CF DRAWING IN BOPI) AND THEIR DERIVATIVES 1,2 DEHYDROGENES IN

Melanocortin derivatives for specific binding of melanocortin receptor 3, 4 or 5

The invention provides novel peptides derived from the group of hormones including ACTH. These so-called melanocortins can target different receptors which often have different localizations on several tissues. The presently invented peptides are useful for targeting receptors in the nervous system in an agonistic manner. Pharmaceutical compositions and uses are also disclosed.

STEROID-BASED COMPOSITIONS

Patent FR2285137B1

LIPOSOMER INNEHAOLLANDE STEROIDA ESTRAR.

20-spiroxanes and analogues with open ring e, process for their preparation and pharmaceutical compositions

Compounds for improved viral transduction

본 발명은 세포의 바이러스 형질도입의 효율을 개선시키는 방법 및 조성물을 제공한다. 보다 특히, 본 발명은, 바이러스 및/또는 바이러스 벡터를 사용하여, 인간 조혈 줄기 세포(HSC) 등의 세포를 형질도입하는 방법의 효율을 안전하고 신뢰성 있게 개선시키는데 유용한 방법 및 물질을 제공한다. 당해 조성물 및 방법은 조혈 줄기 세포 유전자 치료를 사용한 치료에 적합한 치료학적 징후에 유용하다. The present invention provides methods and compositions for improving the efficiency of viral transduction of cells. More particularly, the present invention provides methods and materials useful for safely and reliably improving the efficiency of methods of transducing cells such as human hematopoietic stem cells (HSC) using viruses and / or viral vectors. The compositions and methods are useful for therapeutic indications suitable for treatment with hematopoietic stem cell gene therapy.

Analogous process for the preparation of sultins of 17-hydroxy-3-oxo-17alpha-pregn-4-ene-21-sulfinic acids.

Methods for treating inflammation-mediated conditions of the eye

Methods for treating inflammation-mediated conditions of the eye are described, comprising: implanting into the vitreous of the eye of an individual a bioerodible implant comprising a steroidal anti-inflammatory agent and a bioerodible polymer, wherein the implant delivers the agent to the vitreous in an amount sufficient to reach a concentration equivalent to at least about 0.05 µg/ml dexamethasone within about 48 hours and maintains a concentration equivalent to at least about 0.03 µg/ml dexamethasone for at least about three weeks.

11 beta -substituted DELTA -steroids

11 beta -Substituted steroids of formula (I> <IMAGE> wherein R1 and R2 are both hydrogen or, taken together, form the group oxo or =CH2; R3 is an alkyl, alkenyl or alkynyl substituent at C-6 or C-7; R5 is alkyl; R6 is hydroxy and R7 is hydrogen, alkyl, alkenyl or alkynyl, or R6 and R7, taken together, form =CH2; R4 is, e. g., an alkyl, cycloalkyl, phenyl or heterocyclic group, each optionally substituted by a substituent chosen from (i) unsubstituted or substituted amino or heterocyclic amino, (ii) a silyl group, (iii) a hydroxy, alkoxy or aminoalkoxy group and (iv) halogen or haloalkyl, and pharmaceutically or veterinarily acceptable salts thereof. The compounds of formula (I) exhibit anti-progesterone and antiglucocorticoid activity and are useful in treatment of hormone-dependent tumors.

Antisolvent solidification process

The present invention relates to a antisolvent solidification process wherein a liquid medium comprising at least one organic or inorganic compound which is to be solidified is forced through a membrane into one or more antisolvents, or wherein one or more antisolvents are forced through a membrane into a liquid medium comprising at least one organic or inorganic compound which is to be solidified, yielding a composition comprising solid particles comprising said organic and/or inorganic compound(s).

6,6-ethylene-15,16-methylene-3-oxo-17-alpha-pregn-4-ene 21-17 carbolactone, process for their preparation and pharmaceutical compositions containing them

Method of producing 11beta-substituted steroids or their pharmaceutically or veterinarily acceptable salts

Изобретение касаетс  замещенных стероидов , в частности, получени  соединений общей формулы @ , где R 1 -C 1 -C 3 - алкил The invention relates to substituted steroids, in particular, the preparation of compounds of the general formula @, where R 1 -C 1 -C 3 is alkyl R 2 -A-Z R 2 -AZ A-фенилен A-phenylene Z-NR 5 R 6 Z-NR 5 R 6 R 5 и R 6 -C 1 -C 3 -алкил R 5 and R 6 -C 1 -C 3 -alkyl R 3 -OH R 3 -OH R 4 -C 2 -C 5 -алкинил или их фармацевтически или ветеринарно приемлемых солей, обладающих противоглюкокортикоидной активностью. Цель - создание более активных и малотоксичных веществ указанного класса. Синтез ведут дегидратацией и декетализацией соединени  общей формулы @ где R 1 -R 4 - см.выше R 4 -C 2 -C 5 -quinil or their pharmaceutically or veterinary acceptable salts with anti-glucocorticoid activity. The goal is to create more active and low-toxic substances of the specified class. Synthesis is carried out by dehydration and deketalization of the compound of the general formula @ where R 1 -R 4 is above [R 1 +R 11 ] - защищенна  оксогруппа в виде циклического кетал . В случае необходимости выделенный продукт превращают в нужную соль. Новые вещества малотоксичны и более активны, чем картексолон. 1 табл. [R 1 + R 11 ] is a protected oxo group in the form of a cyclic ketal. If necessary, the selected product is converted to the desired salt. New substances are less toxic and more active than cartexolone. 1 tab.

Composition for reducing or preventing adverse effect of steroid therapy

연골 및 상처회복의 분야와 관련하여, 스테로이드의 일부 부작용을 인슐린-유사 생장인자 I(IGF-I)으로 경감시키거나 억제시키는 방법 및 이를 위한 조성물이 기술된다. Regarding the field of cartilage and wound healing, methods and compositions for reducing or inhibiting some side effects of steroids with insulin-like growth factor I (IGF-I) are described.

Glycyrrhetinic acid derivatives, progesterone and progesterone derivatives and their use for the manufacture of a medicament to inhibit 11beta-hydroxysteroid dehydrogenase activity

The present invention provides use of a compound in the manufacture of a medicament to inhibit 11β-HSD activity, wherein the compound is selected from glycyrrhetinic acid derivatives, progesterone and progesterone derivatives.

Steroid compounds

Amino acid derivatives

Abstract New aminoacid derivatives of the formula I X-Z-NR2-CHR3-CR4-(CHR5)n-CO-E-NR6-(CHR7)s-D wherein X, Z, R2, R3, R4, R5, E, R6, R7, D, n and s have the meaning indicated in Patent Claim 1, and salts thereof inhibit the activity of human plasma renin.

Crf1 receptor antagonists for the treatment of congenital adrenal hyperplasia

ABSTRACT CRF1 receptor antagonists have the potential to directly inhibit ACTH release in patients with CAH and thereby allow normalization of androgen production while using lower, more physiologic doses of hydrocortisone, and thus reducing treatment-associated side effects. Date Recue/Date Received 2022-04-19

Corticoid derivatives and process for production thereof

Novel corticoid 17α-alkoxycarbonyl carboxylate derivatives are disclosed. These derivatives have strong topical anti-inflammatory activity and extremely weak systemic adverse reactions and are useful for the treatment of acute and chronic eczema, eczema seborrhoicorum, contact dermatitis, atopic dermatitis, asthma, etc.

Steroids;preparation and pharmaceutical compositions

Transdermal pharmaceutical delivery composition

A pharmaceutically delivery system is described comprising a pharmaceutically active agent and acidified nitrite as an agent to produce local production of nitric oxide at the skin surface. The dosage form may be in any pharmaceutically acceptable carrier means and comprises an acidifying agent adapted to reduce the pH at the environment. In one embodiment, a barrier consisting of a membrane allows diffusions of the anaesthetic and nitrite ions while preventing direct contact of the skin and acidifying agent.

Mousse composition

Use of bicyclic imidazole compounds for the treatment of hyperaldosteronism

The invention relates to specific bicyclic imidazole compounds such as 5-(p-cyanophenyl)-5,6,7,8-tetrahydroimidazo[1,5-a]pyridine, or pharmaceutically acceptable non-toxic salts thereof, for the treatment of hyperaldosteronism, and to a method of treating hyperaldosteronism using such compounds, as well as to the use of said compounds for the preparation of pharmaceutical compositions for the treatment of hyperaldosteronism.

Two chamber cartridge for atomizers

The invention relates to an apparatus comprising a closure-cap and a container in the form of a two-chamber cartridge in which an active ingredient and a solvent can be stored separately until the apparatus is used in a nebuliser, as well as an active substance concentrate in which the active substance is present as a solution or suspension for storage purposes.

D-homo-(16-ene)-11β-aryl-4-estrenes, process for their production as well as their use as pharmaceutical agents

New D-homo-(16-ene)-11β-aryl-4-estrenes of general formula I ##STR1## as well as their pharmaceutically compatible addition salts with acids are described in which X stands for an oxygen atom, the hydroxyimino grouping >N˜OH or two hydrogen atoms, R 1 stands for a hydrogen atom or a methyl group, R 2 stands for an hydroxy group, a C 1 -C 10 alkoxy or C 1 -C 10 acyloxy group, R 11 stands for a fluorine, chlorine or bromine atom, and then R 12 and R 13 together mean an additional bond or R 11 stands for a straight-chain or branched-chain C 1 -C 4 -alkyl radical or a hydrogen atom, and then R 12 and R 13 each mean a hydrogen atom or together mean an additional bond, and R 3 and R 4 have the usual meanings indicated in the description for competitive progesterone antagonists. The invention further relates to a process for the production of new compounds, pharmaceutical preparations containing these compounds, their use for the production of pharmaceutical agents as well as the new intermediate products necessary for the process. The new compounds have a strong affinity to the gestagen receptor and show strong antigestagen as well as antiglucocorticoid, antimineral corticoid and antiandrogenic properties.

NOVEL 19-NOR STEROIDS SUBSTITUTED IN 11B AND POSSIBLY IN 2, PROCESS FOR THE PREPARATION THEREOF AND THEIR APPLICATION AS A MEDICINAL PRODUCT

L'INVENTION A POUR OBJET LES PRODUITS DE FORMULE I: (CF DESSIN DANS BOPI) DANS LAQUELLE: R RADICAL ORGANIQUE C COMPORTANT EVENTUELLEMENT UN HETEROATOME; R RADICAL HYDROCARBONE C; X CYCLE PENTAGONAL OU HEXAGONAL. LES CYCLES A ET B REPRESENTENT LES GROUPEMENTS: (CF DESSIN DANS BOPI) R ET R H, CN OU ALKYLE C; RA -N; RA ET RA ALK C SOIT RA ET RA FORMENT UN HETEROCYCLE; OU RA ACYLOXY. LEUR PROCEDE DE PREPARATION ET LEUR APPLICATION COMME MEDICAMENTS. THE SUBJECT OF THE INVENTION IS THE PRODUCTS OF FORMULA I: (CF DRAWING IN BOPI) IN WHICH: R ORGANIC RADICAL C POSSIBLY CONTAINING A HETEROATOM; R RADICAL HYDROCARBON C; X PENTAGONAL OR HEXAGONAL CYCLE. CYCLES A AND B REPRESENT THE GROUPINGS: (CF DRAWING IN BOPI) R AND R H, CN OR ALKYL C; RA -N; RA AND RA ALK C EITHER RA AND RA FORM A HETEROCYCLE; OR RA ACYLOXY. THEIR PREPARATION PROCESS AND THEIR APPLICATION AS MEDICINAL PRODUCTS.