Hemmer der retroviralen Protease

PROCEDURE AND INTERMEDIATE FOR THE PRODUCTION OF RETROVIRALEN PROTEASEHEMMERN

INHIBITORS THAT RETROVIRALEN PROTEASE

PRODUCTION of a SUBSTITUTED ONE 2,5-DIAMINO-3 HYDROXYHEXAN

INTERMEDIATE PRODUCTS FOR THE PRODUCTION OF RETROVIRALER PROTEASEHEMMENDEN CONNECTIONS

1,4-Bis-amino-2-hydroxy-butane derivatives

replaced 1,4-Diammino-2-idrossibutani

Composti di partenza by la preparazione there inibitorii depression proteasi retrovirali.

MARKER FOR USE IN THE COMBINATORIAL CHEMICAL SYNTHESIS

HEMMER THAT RETROVIRALEN PROTEASE

INTERMEDIATE PRODUCTS FOR the PRODUCTION of a SUBSTITUTED ONE 2,5-DIAMINO-3-HYDROXYHEXAN.

PROCEDURE FOR THE PRODUCTION OF SUBSTITUTED CYCLOBUTANES.

Retroviral protease inhibiting compounds

PROCESS FOR THE PREPARATION OF A SUBSTITUTED 2,5-DIAMINO-3-HYDROXYHEXANE

Intermediates and processes are disclosed which are useful for the preparation of a substantially pure compound of formula (3), wherein R6 and R7 are each hydrogen or R6 and R7 are independently selected from (i), wherein Ra and Rb are independently selected from hydrogen, loweralkyl and phenyl and Rc, Rd and Re are independently selected from hydrogen, loweralkyl, trifluoromethyl, alkoxy, halo and phenyl; and (ii) wherein the naphthyl ring is unsubstituted or substituted with one, two or three substituents independently selected from loweralkyl, trifluoromethyl, alkoxy and halo; or R6 is as defined above and R7 is R7aOC (O)-wherein R7a is loweralkyl or benzyl; or R6 and R7 taken together with the nitrogen atom to which they are bonded are (a) or (b), wherein Rf, Rg, Rh and Ri are independently selected from hydrogen, loweralkyl, alkoxy, halogen and trifluoromethyl and R8 is hydrogen or -C(O)R" wherein R" is loweralkyl, alkoxy, benzyloxy or phenyl wherein the phenyl ring is unsubstituted ...

RETROVIRAL PROTEASE INHIBITING COMPOUNDS

A retroviral protease inhibiting compound of formula (A) is disclosed ...

Inhibitors of interleukin 5 gene expression

CARBOCYCLIC NUCLEOSIDE ANALOGS

CARBOCYCLIC NUCLEOSIDE ANALOGS ABSTRACT OF THE DISCLOSURE A compound of the formula: wherein A is a purin-9-yl group, a heterocyclic isostere of a purin-9-yl group, a pyrimidin-1-yl group or a heterocyclic isostere of a pyrimidin-1-yl group; E is hydrogen, -CH2OH or -OH; and G and D are independently selected from hydrogen, C1 to C10 alkyl, OH, -CH2OH, -CH2OR20 wherein R20 i8 C1 to C6 alkyl, -CH20C(O)R21 wherein R21 is C1 to C10 alkyl, -CH20C(O)CH(R22)(NHR23) wherein R22 is tha side chain of any of the naturally occuring amino acids and R23 is hydrogen or -C(O)CH(R24)(NH2) wherein R24 is the side chain of any of the naturally occuring amino acids, -CH2SH, -CH2C1, -CH2F, -CH2Br, -CH2I, -C(O)H, -CH2CN, -CH2N3, -CH2NR1R2, -CO)2R1, -CH2OH2OH, -CH2CH2OR20 R20 is as defined above, -CH2CH20C(O)R21 wherein R21 is as defined above, -CH2CH20C(O)CH(R22)(NHR23) wherein R22 and R23 are as defined above, -CH2CH2PO3H2, -CH2OPO3H2, -OCH2PO3H2 and -CH2CO2R3 wherein R1 and R2 are independently selected from hydrogen and C1 to 10 alkyl and R3 is hydrogen, C1 to C10 alkyl, carboxyalkyl or aminoalkyl; or a pharmaceutically acceptable salt thereof. (11-1088P)

RETROVIRAL PROTEASE INHIBITING COMPOUNDS

A retroviral protease inhibiting compound of formula (A) is disclosed -(see formula I)

INHIBITOREN DER RETROVIRALEN PROTEASE.

Cyclobut-3-ene-1,2,-dione inhibitors of polo-like kinases

Compounds of formula (I) where X1, C1, and D1 are defined herein, are inhibitors of polo-like kinases. The compounds of formula (I) are useful for treatment of diseases of cellular proliferation, such as, for example, cancer.

Retroviral protease inhibiting compounds

Retroviral Protease Inhibitor (2S,3S,5S)-5-(N-(N-Methyl-N-((2-Isopropyl-4-Thiazo lyl)Methyl)Amino)(Arbonyl)Valinyl)-Amino)-2-(N-((5-Thiazoly l)Methoxycarbonyl)Amino)-1,6-Diphenyl-3-Hydroxyhexane

ATTACHED TAGS FOR USE IN COMBINATORIAL CHEMISTRY SYNTHESIS

The present invention relates to a process of coding and identifying individual members of a chemical combinatorial library synthesized on a plurality of solid supports which undergo mix and split synthesis. The process provides for tagging the solid supports with a coding identifier that is attached to the solid support and which can be decoded by infrared or Raman spectroscopy when directly attached to the support.

CODING COMBINATORIAL LIBRARIES WITH FLUORINE TAGS

The present invention relates to coding combinatorial chemical libraries synthesized on a plurality of solid supports by attaching "tags" that comprise fluorine containing compounds in combinations and/or ratios. The tags can be decoded while attached to the solid support by fluorine nuclear magnetic resonance spectroscopy to follow the reaction history of individual beads, and to determine the particular member of the library that is attached on the bead.

Verfahren zur Herstellung substituierter Cyclobutane.

PROCESS FOR PREPARING SUBSTITUTED CYCLOBUTANES

PROCESS FOR PREPARING SUBSTITUTED CYCLOBUTANES ABSTRACT OF THE DISCLOSURE The present invention relates to a process for the preparation of substituted cyclobutanes and their use as intermediates for the preparation of anti-viral nucleoside analogs.

PROCESS FOR THE PREPARATION OF A SUBSTITUTED 2,5-DIAMINO-3-HYDROXYHEXANE

Intermediates and processes are disclosed which are useful for the preparati on of a substantially pure compound of formula (3), wherein R6 and R7 are each hydrogen or R6 and R7 are independently selected from (i), wherein Ra and Rb are independently selected from hydrogen, loweralkyl and phenyl and Rc, Rd a nd Re are independently selected from hydrogen, loweralkyl, trifluoromethyl, alkoxy, halo and phenyl; and (ii) wherein the naphthyl ring is unsubstituted or substituted with one, two or three substituents independently selected fr om loweralkyl, trifluoromethyl, alkoxy and halo; or R6 is as defined above and R7 is R7aOC (O)-wherein R7a is loweralkyl or benzyl; or R6 and R7 taken togethe r with the nitrogen atom to which they are bonded are (a) or (b), wherein Rf, Rg, Rh and Ri are independently selected from hydrogen, loweralkyl, alkoxy, halogen and trifluoromethyl and R8 is hydrogen or -C(O)R" wherein R" is loweralkyl, alkoxy, benzyloxy or phenyl wherein the phenyl ring is unsubstituted or substituted with one, two or three substituents independent ly selected from loweralkyl, trifluoromethyl, alkoxy and halo; or an acid addition salt thereof.

Heterocyclic kinase inhibitors

Compounds having the formula are useful for inhibiting protein kinases. Also disclosed are methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.

Retroviral protease inhibiting compounds

INHIBITOREN DER RETROVIRALEN PROTEASE

Retriviral protease inhibiting compounds

Verfahren zur Herstellung substituierter Cyclobutane.

Heterocyclic Kinase Inhibitors

Compounds having the formula are useful for inhibiting protein kinases. Also disclosed are methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.

Retroviral protease inhibiting compounds

Zwischenprodukte zur Herstellung retroviraler proteasehemmenden Verbindungen

Heterocyclic kinase inhibitors

Compounds having the formula, are useful for inhibiting protein kinases. Also disclosed are methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.

Macrocyclic kinase inhibitors

Compounds having the formula are useful for inhibiting protein kinases. Also disclosed are methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.

PROCESSES AND INTERMEDIATES FOR MANUFACTURING RETROVIRAL PROTEASE INHIBITING COMPOUNDS

INHIBITOREN DER RETROVIRALEN PROTEASE

Herstellung einer substituierten 2,5-Diamino-3-hydroxyhexan

Zwischenprodukte zur Herstellung retroviraler proteasehemmenden Verbindungen

Hemmer der retroviralen Protease

Verfahren und Intermediate zur Herstellung von retroviralen Proteasehemmern

Inhibiting composites of protease retroviral

METHOD FOR PRODUCING SUBSTITUTED 2,5-DIAMINO-3-HYDROXYHEXANE

PROBLEM TO BE SOLVED: To provide a substituted 2,5-diamino-3-hydroxyhexane useful for producing HIV protease inhibitors, and to provide a method for producing the compound. SOLUTION: The substituted 2,5-diamino-3-hydroxyhexane useful for producing HIV protease inhibitors is represented by general formula I. COPYRIGHT: (C)2006,JPO&NCIPI ...

Macrocyclic kinase inhibitors

Compounds having the formula are useful for inhibiting protein kinases. Also disclosed are methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.

Coding combinatorial libraries with fluorine tags

The present invention relates to coding combinatorial chemical libraries synthesized on a plurality of solid supports by attaching "tags" that comprise fluorine containing compounds in combinations and/or ratios. The tags can be decoded while attached to the solid support by fluorine nuclear magnetic resonance spectroscopy to follow the reaction history of individual beads, and to determine the particular member of the library that is attached on the bead.

Macrocyclic kinase inhibitors

Compounds having the formula are useful for inhibiting protein kinases. Also disclosed are methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.

Retroviral protease inhibiting compounds

A retroviral protease inhibiting compound of the formula:is disclosed.

COMPOUND INHIBITING RETROVIRUS PROTEASE

PROBLEM TO BE SOLVED: To obtain the subject new compound having a specific molecular structure, exhibiting an action on the inhibition of a retrovirus protease, and useful for the therapy of retrovirus infection, especially human immunodeficiency virus(HIV) infection causing AIDS, etc. SOLUTION: A new compound of formula I [R1 is a mono-substituted (iso) thiazolyl, a mono-substituted (iso)oxazolyl; (n) is 1-3; R2, R6 are each H, a lower alkyl; R3 is a lower alkyl; R4, R4a are each a (substituted)phenyl, a (substituted) thiazolyl; R7 is a (substituted) (iso)thiazolyl, a (substituted) (iso)oxazolyl; X is H and Y is OH, or X is OH and Y is H, etc.; Z is absent, O, S, CH2, etc.,]. The compound of formula I is useful for the therapy of retrovirus infection, etc. The compound is obtained by reacting an amino group-containing compound of formula II with an N-substitute amino acid of formula III or its active ester derivative. COPYRIGHT: (C)1997,JPO ...

CARBOCYCLIC NUCLEOSIDE ANALOGUE

NEW MATERIAL: A compd. represented by formula I [wherein A is a purin-9-yl or a group represented by formula II (J and L are each H, OH, halogen, alkoxy, SH, N3 or the like; and M is H, alkyl, halogen or the like) or pyrimidin-1-yl or a group represented by formula III (V is O or S; Q is OH, alkoxy, SH, thioalkoxy or the like; and T is H, alkyl halogen, CN or the like); or the like; E is H, CH2OH is OH; G and D are each E, alkyl or CH2OH20 (R20 ia alkyl)] or its salt. EXAMPLE: 9-2',3'-bis (hydroxymethyl) cyclobutyl)guanine. USE: Useful for treating a viral disease, hepatitis and a tumor. PROCESS: For example, 2-amino-6-chloropurine is reacted with a compd. represented by formula IV (wherein X is a leaving group; and R28 and R27 are alkyl or aryl) to obtain a product which is, in turn, reduce to obtain a bis-hydroxymethyl deriv. and this deriv. is hydrolyzed to obtain the designated compd. COPYRIGHT: (C)1991,JPO ...

Fused tri and tetra-cyclic pyrazole kinase inhibitors

Compounds having the formula (I) are useful for inhibiting protein kinases. Also disclosed are methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.

INHIBITORS OF POLO-LIKE KINASES

Compounds that inhibit Plk1, compositions containing the compounds and methods of treating diseases using the compounds are disclosed.

Attached tags for use in combinatorial chemistry synthesis

The present invention relates to a process of coding and identifying individual members of a chemical combinatorial library synthesized on a plurality of solid supports which undergo mix and split synthesis. The process provides for tagging the solid supports with a coding identifier that is attached to the solid support and which can be decoded by infrared or raman spectroscopy when directly attached to the support.

PRODUCTION OF SUBSTITUTED CYCLOBUTANE

PURPOSE: To obtain the subject compound as substantially pure enantiomer by allowing diester of fumaric acid to react with ketene dithioacetal in the presence of Lewis acid catalyst, and to react with several processes. CONSTITUTION: The substantially pure enantiomer being trans form of compound of formula II (R1 is H, hydroxyl protecting group) is obtained by allowing diester, dithio ester or diamide of fumaric acid which ester, thioester or amide group is derived from alcohol, thioalcohol or amine to be pure in enantiomer (the ester, thioester, amide can be obtained with symmetric selectivity with 2+2 cyclic addition reaction) to react with the compound of formula I in the presence of Lewis acid catalyst, to convert the obtained product into diol, or if necessary, to protect hydroxyl group and hydrolyze dithioketal into ketone. In formula I, Ra, Rb are each alkyl, cycloalkyl, optionally substituted phenyl, optionally substituted benzyl. COPYRIGHT: (C)1992,JPO ...

Attached tags for use in combinatorial chemistry synthesis

The present invention relates to a process of coding and identifying individual members of a chemical combinatorial library synthesized on a plurality of solid supports which undergo mix and split synthesis. The process provides for tagging the solid supports with a coding identifier that is attached to the solid support and which can be decoded by infrared or raman spectroscopy when directly attached to the support.

Processo para a preparacao de um 2,5-diamino-3-hidroxi-hexano substituido

Preparation of a substituted 2,5-diamino-3-hydroxyhexane

Inhibitors of interleukin 5 gene expression

A method of inhibiting interleukin 5 gene expression in a mammal comprising administering to a mammal in need of such treatment a pharmaceutically effective amount of one or more compounds selected from formula (I) and/or from formula (II).

Retroviral protease inhibiting compounds.

Retroviral protease inhibiting compounds

A retroviral protease inhibiting compound of the formula: ##STR1## is disclosed.

Process for the preparation of a substituted 2.5-diamino-3-hydroxyhexane

Intermediates and processes are disclosed which are useful for the preparation of a substantially pure compound of the formula: ##STR1## wherein R 6 and R 7 are each hydrogen or R 6 and R 7 are independently selected from ##STR2## wherein R a and R b are independently selected from hydrogen, loweralkyl and phenyl and R c , R d and R e are independently selected from hydrogen, loweralkyl, trifluoromethyl, alkoxy, halo and phenyl; and ##STR3## wherein the naphthyl ring is unsubstituted or substituted with one, two or three substitutents independently selected from loweralkyl, trifluoromethyl, alkoxy and halo; or R 6 is as defined above and R 7 is R 7a OC(O)-- wherein R 7a is loweralkyl or benzyl; or R 6 and R 7 taken together with the nitrogen atom to which they are bonded are ##STR4## wherein R f , R g , R h and R i are independently selected from hydrogen, loweralkyl, alkoxy, halogen and trifluoromethyl and R 8 is hydrogen or --C(O)R" wherein R" is loweralkyl, alkoxy, benzyloxy or phenyl wherein the phenyl ring is unsubstituted or substituted with one, two or three substituents independently selected from loweralkyl, trifluoromethyl, alkoxy and halo; or an acid addition salt thereof.

Process for the preparation of a disubstituted 2,5-diamino-3-hydroxyhexane

Intermediates and processes are disclosed which are useful for the preparation of a substantially pure compound of the formula: ##STR1## wherein R 6 and R 7 are each hydrogen or R 6 and R 7 are independently selected from ##STR2## wherein R a and R b are independently selected from hydrogen, loweralkyl and phenyl and R c , R d and R e are independently selected from hydrogen, loweralkyl, trifluoromethyl, alkoxy, halo and phenyl; and ##STR3## wherein the naphthyl ring is unsubstituted or substituted with one, two or three substitutents independently selected from loweralkyl, trifluoromethyl, alkoxy and halo; or R 6 is as defined above and R 7 is R 7a OC(O)-- wherein R 7a is loweralkyl or benzyl; or R 6 and R 7 taken together with the nitrogen atom to which they are bonded are ##STR4## wherein R f , R g , R h and R i are independently selected from hydrogen, loweralkyl, alkoxy, halogen and trifluoromethyl and R 8 is hydrogen or --C(O)R" wherein R" is loweralkyl, alkoxy, benzyloxy or phenyl wherein the phenyl ring is unsubstituted or substituted with one, two or three substituents independently selected from loweralkyl, trifluoromethyl, alkoxy and halo; or an acid addition salt thereof.

UNITED MARKERS INTENDED FOR USE IN COMBINATORY CHEMICAL SYNTHESIS.

LA PRESENTE INVENCION SE REFIERE A UN PROCESO PARA LA CODIFICACION E IDENTIFICACION DE LOS MIEMBROS INDIVIDUALES DE UNA LIBRERIA QUIMICA COMBINATORIA SINTETIZADA EN UNA PLURALIDAD DE SOPORTES SOLIDOS QUE SOPORTAN UNA SINTESIS POR MEZCLA Y SEPARACION. EL PROCESO CONSISTE EN MARCAR LOS SOPORTES SOLIDOS CON UN IDENTIFICADOR DE CODIFICACION QUE SE ACOPLA AL SOPORTE SOLIDO Y QUE SE PUEDE DECODIFICAR A TRAVES DE UNA ESPECTROSCOPIA POR RAYOS INFRARROJOS O RAMAN CUANDO ESTAN DIRECTAMENTE ACOPLADOS AL SOPORTE. THE PRESENT INVENTION REFERS TO A PROCESS FOR THE CODING AND IDENTIFICATION OF INDIVIDUAL MEMBERS OF A COMBINATORY CHEMICAL LIBRARY SYNTHESIZED IN A PLURALITY OF SOLID SUPPORTS THAT SUPPORT A SYNTHESIS BY MIXING AND SEPARATION. THE PROCESS CONSISTS OF MARKING THE SOLID SUPPORTS WITH A CODING IDENTIFIER THAT COUPLES THE SOLID SUPPORT AND CAN BE DECODED THROUGH A SPECTROSCOPY BY INFRARED RAYS OR RAMAN WHEN THEY ARE DIRECTLY COUPLED TO THE SUPPORT.

Retroviral protease inhibiting compounds.

Intermediates for retroviral protease inhibiting compounds

Borooxazine compounds of the formula <see formula> are used as intermediates in processes to compounds of the formula <see formula>

Process for preparation of intermediates of carbocyclic nucleoside analogs

A compound of the formula: ##STR1## wherein A is a purin-9-yl group, a heterocyclic isostere of a purin-9-yl group, a pyrimidin-1-yl group or a heterocyclic isostere of a pyrimidin-1-yl group; E is hydrogen, --CH 2 OH or --OH; and G and D are independently selected from hydrogen, C 1 to C 10 alkyl, --OH, --CH 2 OH, --CH 2 OR 20 wherein R 20 is C 1 to C 6 alkyl, --CH 2 OC(O)R 21 wherein R 21 is C 1 to C 10 alkyl, --CH 2 OC(O)CH(R 22 )(NHR 23 ) wherein R 22 is the side chain of any of the naturally occuring amino acids and R 23 is hydrogen or --C(O)CH(R 24 )(NH 2 ) wherein R 24 is the side chain of any of the naturally occuring amino acids, --CH 1 SH, --Ch 2 Cl, --Ch 2 F, --CH 2 Br, --CH 2 I, --C(O)H, --CH 2 CN, --CH 2 N 3 , --CH 2 NR 1 R 2 , --CO 2 R 1 , --CH 2 CH 2 OH, --CH 2 CH 2 OR 20 wherein R 20 is as defined above, --CH 2 CH 2 OC(O)R 21 wherein R 21 is as defined above, --CH 2 CH 2 OC(O)CH(R 22 )(NHR 23 ) wherein R 22 and R 23 are as defined above, --CH 2 CH 2 PO 3 H 2 , --Ch 2 OPO 3 H 2 , --OCH 2 PO 3 H 2 and --CH 2 CO 2 R 3 wherein R 1 and R 2 are independently selected from hydrogen and C 1 to C 10 alkyl and R 3 is hydrogen, C 1 to C 10 alkyl, carboxyalkyl or aminoalkyl; or a pharmaceutically acceptable salt thereof.

Coding combinatorial libraries with fluorine tags

The present invention relates to coding combinatorial chemical libraries synthesized on a plurality of solid supports by attaching 'tags' that comprise fluorine containing compounds in combinations and/or ratios. The tags can be decoded while attached to the solid support by fluorine nuclear magnetic resonance spectroscopy to follow the reaction history of individual beads, and to determine the particular member of the library that is attached on the bead.

Intermediates for the preparation of compounds that inhibit retroviral protease

A retroviral protease inhibiting compound of formula (A) is disclosed for use in combination with other active pharmaceutical agents for treating a human infected by HIV. Intermediates and processes useful in the manufacture of compounds of formula (A) are also disclosed. <CHEM>

Attached tags for use in combinatorial chemistry synthesis

The present invention relates to a process of coding and identifying individual members of a chemical combinatorial library synthesized on a plurality of solid supports which undergo mix and split synthesis. The process provides for tagging the solid supports with a coding identifier that is attached to the solid support and which can be decoded by infrared or Raman spectroscopy when directly attached to the support.

Intermediates for retroviral protease inhibiting compounds

Intermediates and their process of preparation are provided, the intermediates being useful in the preparation of a retroviral protease inhibiting compound of formula (A)

Verfahren und intermediate zur herstellung von retroviralen proteasehemmern

Macrocyclic kinase inhibitors

Compounds having the formula (I) are useful for inhibiting protein kinases. Also disclosed are methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds

Verfahren zur herstellung substituierter cyclobutane.

Marker zur verwendung in der kombinatorischen chemischen synthese

Macrocyclic kinase inhibitors

Compounds having the formula (I) are useful for inhibiting protein kinases. Also disclosed are methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds

Herstellung einer substituierten 2,5-diamino-3- hydroxyhexan

Zwischenprodukte für die herstellung einer substituierten 2,5-diamino-3-hydroxyhexan.

Zwischenprodukte zur herstellung retroviraler proteasehemmenden verbindungen

Hemmer der retroviralen protease

Coding combinatorial libraries with fluorine tags

The present invention relates to coding combinatorial chemical libraries synthesized on a plurality of solid supports by attaching 'tags' that comprise fluorine containing compounds in combinations and/or ratios. The tags can be decoded while attached to the solid support by fluorine nuclear magnetic resonance spectroscopy to follow the reaction history of individual beads, and to determine the particular member of the library that is attached on the bead.