公开(公告)号：AT410439T

公开(公告)日：2008-10-15

申请号：AT99912662

申请日：1999-03-19

Applicant: VERTEX PHARMA

Inventor： WANNAMAKER MARION ,  BEMIS GUY ,  CHARIFSON PAUL ,  LAUFFER DAVID ,  MULLICAN MICHAEL ,  MURCKO MARK ,  WILSON KEITH ,  JANETKA JAMES ,  DAVIES ROBERT ,  GRILLOT ANNE-LAURE ,  SHI ZHAN ,  FORSTER CORNELIA

IPC: C07D207/273 ,  C07K5/023 ,  A61K31/47 ,  A61K38/00 ,  A61K38/03 ,  A61K38/04 ,  A61P5/48 ,  A61P7/00 ,  A61P9/00 ,  A61P17/00 ,  A61P19/00 ,  A61P19/08 ,  A61P19/10 ,  A61P25/00 ,  A61P29/00 ,  A61P31/04 ,  A61P35/00 ,  A61P37/00 ,  A61P37/06 ,  A61P43/00 ,  C07D401/12 ,  C07K5/02

Abstract: The present invention relates to novel classes of compounds which are caspase inhibitors, in particular interleukin-1² converting enzyme ("ICE") inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting caspase activity and consequently, may be advantageously used as agents against interleukin-1- ("IL-1"), apoptosis-, interferon-³ inducing factor-(IGIF), or interferon-³-("IFN-³") mediated diseases, including inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, and degenerative diseases. This invention also relates to methods for inhibiting caspase activity and decreasing IGIF production and IFN-³ production and methods for treating interieukin-1, apoptosis-, and interferon-³ mediated diseases using the compounds and compositions of this invention. This invention also relates to methods of preparing the compounds of this invention.

公开(公告)号：CA2663528A1

公开(公告)日：2008-03-27

申请号：CA2663528

申请日：2007-09-18

Applicant: VERTEX PHARMA

Inventor： TANNER KIRK ,  NANTHAKUMAR SUGANTHINI ,  COME JON ,  ARONOV ALEXANDER ,  MCGINTY KIRA ,  LI PAN ,  COURT JOHN ,  DEININGER DAVID ,  STAMOS DEAN ,  LAUFFER DAVID

IPC: C07D497/04 ,  A61K31/433 ,  A61P35/00 ,  C07D513/04

Abstract: The present invention provides compounds useful as inhibitors of c-Met ty rosine kinase. The invention also provides pharmaceutically acceptable compo sitions comprising the compounds of the invention and methods of using the c ompositions in the treatment of various proliferative disorders.

公开(公告)号：AU2007297754A1

公开(公告)日：2008-03-27

申请号：AU2007297754

申请日：2007-09-18

Applicant: VERTEX PHARMA

Inventor： MCGINTY KIRA ,  NANTHAKUMAR SUGANTHINI ,  COURT JOHN ,  STAMOS DEAN ,  TANNER KIRK ,  LI PAN ,  ARONOV ALEXANDER ,  COME JON ,  LAUFFER DAVID ,  DEININGER DAVID

IPC: C07D497/04 ,  A61K31/433 ,  A61P35/00 ,  C07D513/04

Abstract: The present invention provides compounds useful as inhibitors of c-Met tyrosine kinase. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various proliferative disorders.

公开(公告)号：CA2623032A1

公开(公告)日：2007-04-12

申请号：CA2623032

申请日：2006-09-28

Applicant: VERTEX PHARMA

Inventor： FARMER LUC ,  WANG JIAN ,  WANG TIANSHENG ,  BETHIEL RANDY ,  WANNAMAKER MARION ,  SALITURO FRANCESCO ,  MARTINEZ-BOTELLA GABRIEL ,  DUFFY JOHN ,  ARONOV ALEXANDER ,  PIERCE ALBERT ,  LAUFFER DAVID

IPC: C07D487/04 ,  A61K31/495 ,  A61P29/00 ,  C07D519/00

Abstract: The present invention relates to compounds useful as inhibitors of protein kinases, particularly of JAK family kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorder.

公开(公告)号：AU2006297351A1

公开(公告)日：2007-04-12

申请号：AU2006297351

申请日：2006-09-28

Applicant: VERTEX PHARMA

Inventor： WANNAMAKER MARION ,  BETHIEL RANDY ,  FARMER LUC ,  SALITURO FRANCESCO ,  LAUFFER DAVID ,  WANG JIAN ,  DUFFY JOHN ,  ARONOV ALEXANDER ,  MARTINEZ-BOTELLA GABRIEL ,  PIERCE ALBERT ,  WANG TIANSHENG

IPC: C07D487/04 ,  A61K31/495 ,  A61P29/00 ,  C07D519/00

Abstract: The present invention relates to compounds useful as inhibitors of protein kinases, particularly of JAK family kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorder.

公开(公告)号：BG108927A

公开(公告)日：2006-06-30

申请号：BG10892798

申请日：1998-07-13

Applicant: VERTEX PHARMA

Inventor： BATCHELOR MARK ,  BEBBINGTON DAVID ,  BEMIS GUY ,  FRIDMAN WOLF ,  GILLESPIE ROGER ,  GOLEC JULIAN ,  GU YONG ,  LAUFFER DAVID ,  LIVINGSTON DAVID ,  MATHARU SAROOP ,  MULLICAN MICHAEL ,  MURCKO MARK ,  MURDOCH ROBERT ,  NYCE PHILIP ,  ROBIDOUX ANDREA ,  SU MICHAEL ,  WANNAMAKER M ,  WILSON KEITH ,  ZELLE ROBERT

IPC: C07D243/12 ,  C07K5/02 ,  A61K31/55 ,  A61K31/551 ,  A61K31/553 ,  A61K31/675 ,  A61K38/00 ,  A61K38/04 ,  A61K38/05 ,  A61K38/06 ,  A61K38/07 ,  A61K38/55 ,  A61P13/12 ,  A61P19/08 ,  A61P19/10 ,  A61P25/00 ,  A61P25/28 ,  A61P29/00 ,  A61P31/00 ,  A61P31/04 ,  A61P35/00 ,  A61P37/00 ,  A61P37/06 ,  A61P43/00 ,  C07D243/10 ,  C07D243/14 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D473/00 ,  C07D487/04 ,  C07D491/048 ,  C07D495/04 ,  C07D498/04 ,  C07D513/04 ,  C07D519/00 ,  C07F9/645 ,  C07F9/6561 ,  C07K5/00 ,  C07K5/023 ,  C07K5/06 ,  C07K5/078 ,  C07K5/097

Abstract: The invention relates to a new class of compounds which are inhibitors of interleukin-1'beta' converting enzyme (ICE), to a method for the preparation thereof and to pharmaceutical compositions containing these compounds. They are suitable for inhibiting ICE activity and can be used for the treatment of diseases and materialized by interleukin-1 ("IL-1"), apoptosis, the factor inducing interferon gamma ("IGIF") and interferon ("INF-gamma"), including inflammatory diseases, autoimmune diseases, destructive bone disorder, proliferative, infectious and degenerative diseases.

公开(公告)号：PE04512002A1

公开(公告)日：2002-06-06

申请号：PE0009312001

申请日：2001-09-14

Applicant: VERTEX PHARMA

Inventor： DAVIES ROBERT ,  BEBBINGTON DAVID ,  KNEGTEL RONALD ,  WANNAMAKER MARION ,  LI PAN ,  FORSTER CORNELIA J ,  LAUFFER DAVID ,  PIERCE ALBERT ,  KAY DAVID

IPC: C07D403/12 ,  A61K31/415 ,  A61K31/4155 ,  A61K31/437 ,  A61K31/4427 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/501 ,  A61K31/5025 ,  A61K31/506 ,  A61K31/517 ,  A61K31/519 ,  A61K31/52 ,  A61K31/53 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/55 ,  A61K45/00 ,  A61P1/16 ,  A61P3/08 ,  A61P3/10 ,  A61P3/14 ,  A61P5/00 ,  A61P9/00 ,  A61P9/10 ,  A61P11/06 ,  A61P17/06 ,  A61P19/00 ,  A61P19/02 ,  A61P19/10 ,  A61P25/18 ,  A61P25/28 ,  A61P29/00 ,  A61P31/12 ,  A61P35/00 ,  A61P35/02 ,  A61P37/02 ,  A61P37/06 ,  A61P37/08 ,  A61P43/00 ,  C07D239/26 ,  C07D239/36 ,  C07D239/70 ,  C07D239/88 ,  C07D401/12 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D407/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D473/16 ,  C07D475/10 ,  C07D487/04 ,  C07D491/04 ,  C07D491/044 ,  C07D491/048 ,  C07D491/052 ,  C07D491/107 ,  C07D491/113 ,  C07D491/20 ,  C07D493/04 ,  C07D495/04 ,  C07D498/04 ,  C07D513/04 ,  C07D521/00

CPC classification number: C07D401/14 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/12 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D407/14 ,  C07D409/14 ,  C07D417/14 ,  C07D471/04 ,  C07D473/16 ,  C07D487/04 ,  C07D491/04 ,  C07D493/04 ,  C07D495/04 ,  C07D513/04

Abstract: SE REFIERE A COMPUESTOS DE PIRAZOL DE FORMULA I DONDE EL ANILO C ES FENILO, PIRIDINILO, PIRIMIDINILO, PIRIDAZINILO, PIRAZINILO, 1,2,4-TRIAZINILO SUSTITUIDO EN LA POSICION ORTO POR HALO, CN, NO2, T-V-R6, FENILO, HETEROARILO, HETEROCICLO, UN GRUPO ALIFATICO C1-C6; EN LA POSICION DIFERENTE DE ORTO ES SUSTITUIDO POR R5; R1 Y R2 SON R, R-W-R6, ANILLO DE 5-8 MIEMBROS SUSTITUIDO CON HALO, OXO, CN, NO2R7, VR6; Rx Y Ry SON T-R3, ANILLO FUSIONADO SUSTITUIDO CON T-R3, OXO, R4; T ES ENLACE, ALQUILIDENO, C1-C4; R3 ES R, HALO, OR, COR, N(R4)2, CON(R7)2, ENTRE OTROS; R ES H, ARILO C6-C10, HETEROARILO C5-C10, HETEROCICLO 5-10 MIEMBROS; R4 ES R7, CON(R7)2, SO2R7; R7 ES H, GRUPO ALIFATICO, DOS R7 FORMAN HETEROARILO, HETEROCICLO; R5 ES R, HALO, OR, NR4COR, COCOR, ENTRE OTROS; V ES O, S, SO, SO2, NR6SO2, SO2NR6, CONR6, ENTRE OTROS; R6 ES H, GRUPO ALIFATICO C1-C4, DOS R6 FORMAN HETEROARILO, HETEROCICLO; W ES C(R6)2O, C(R6)2S, CO2, CONR6. TAMBIEN SE REFIERE A COMPUESTOS DE FORMULA A, B, ENTRE OTROS; R10 ES F, Br, HALOALQUILO C1-C6, NITRO, 1-PIRROLO; R1 ES Cl, F, CF3, CN, NO2; LOS COMPUESTOS SON INHIBIDORES DE LA ACTIVIDAD DE CINASAS GLICOGENO SINTASA GSK-3; SERINA TREONINA AURORA-2, AUMENTAN LA SINTESIS DE GLICOGENO, DISMINUYEN NIVEL SANGUINEO DE GLUCOSA, INHIBEN LA PRODUCCION DE PROTEINA TAU HIPERFOSFORILADA, INHIBEN LA FOSFORILACION DE ß-CATEINA Y PUEDEN SER UTILES PARA EL TRATAMIENTO DE DIABETES, ALZHEIMER, ESQUIZOFRENIA, CANCER

公开(公告)号：PE10812001A1

公开(公告)日：2001-10-22

申请号：PE0001442001

申请日：2001-02-09

Applicant: VERTEX PHARMA

Inventor： LAUFFER DAVID ,  TOMLINSON RONALD CHARLES ,  MULLICAN MICHAEL

IPC: A61K31/40 ,  A61K31/4025 ,  A61K31/427 ,  A61K31/4523 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/4995 ,  A61K31/506 ,  A61K38/22 ,  A61K38/27 ,  A61P19/04 ,  A61P21/00 ,  A61P21/04 ,  A61P25/00 ,  A61P25/02 ,  A61P25/04 ,  A61P25/14 ,  A61P25/16 ,  A61P25/28 ,  A61P29/00 ,  C07D20060101 ,  C07D205/04 ,  C07D207/16 ,  C07D209/52 ,  C07D211/26 ,  C07D211/60 ,  C07D211/62 ,  C07D211/78 ,  C07D277/06 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D417/06 ,  C07D417/12 ,  C07D487/08

CPC classification number: C07D401/04 ,  C07D205/04 ,  C07D207/16 ,  C07D211/60 ,  C07D211/62 ,  C07D277/06 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D487/08

Abstract: SE REFIERE A DERIVADOS DE PIPERAZINA Y PIPERIDINA DE FORMULA I DONDE Q ES UN SISTEMA DE ANILLO MONOCICLICO, BICICLICO, TRICICLICO DONDE CADA ANILLO TIENE DE 3-7 ATOMOS SELECCIONADOS DE C, N, O, S; AL MENOS UN ANILLO TIENE UN ATOMO DE NITROGENO CON R1; DE 1-5 ATOMOS DE H EN Q CON HALO, OH, =O, =N-OR1, ALQUILO C1-C6, ENTRE OTROS; Q NO ES UN INDOL O UNA PORCION PIROGLUTAMICA DONDE R1 ES ALQUILO C1-C6, Ar-ALQUILO C1-C6, CICLOALQUILO -(ALQUILO C1-C6), ALQUENILO C2-C6, ENTRE OTROS; Ar ES FENILO, 1-NAFTILO, INDENILO, AZULENILO, ENTRE OTROS; X ES C(R2)2, N, N(R2), S, S(O), SO2; Y ES UN ENLACE, -O-, ALQUILO C1-C6, ALQUENILO C2-C6, ALQUINILO; p ES 0-2; A Y B SON H, Ar ; R2 ES H, ALQUILO C1-C6, ALQUENILO C2-C6, ALQUINILO. SE REFIERE TAMBIEN A UNA COMPOSICION FARMACEUTICA. SON COMPUESTOS PREFERIDOS 1-[4-(1,1-DIFENILMETIL)-PIPERAZIN-1-IL]-1-((S)-1-ETILPIPERIDIN-2-IL)-METANONA,1-[4-(1,1-DIFENILMETIL)-PIPERAZIN-1-IL]-1-(RS)-1-ETILPIPERIDIN-2-IL)-METANONA LOS COMPUESTOS DE PIPERAZINA Y PIPERIDINA DE FORMULA I SON UTILES PARA PREVENIR O TRATAR EL DANO NEURONAL ASOCIADO A ENFERMEDADES NEUROLOGICAS, ALZHEIMER, PARKINSON, PARALISIS

公开(公告)号：AU4146401A

公开(公告)日：2001-08-20

申请号：AU4146401

申请日：2001-02-09

Applicant: VERTEX PHARMA

Inventor： TOMLINSON RONALD ,  LAUFFER DAVID ,  MULLICAN MICHAEL

IPC: A61K31/40 ,  A61K31/4025 ,  A61K31/427 ,  A61K31/4523 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/4995 ,  A61K31/506 ,  A61K38/22 ,  A61K38/27 ,  A61P19/04 ,  A61P21/00 ,  A61P21/04 ,  A61P25/00 ,  A61P25/02 ,  A61P25/04 ,  A61P25/14 ,  A61P25/16 ,  A61P25/28 ,  A61P29/00 ,  C07D20060101 ,  C07D205/04 ,  C07D207/16 ,  C07D209/52 ,  C07D211/26 ,  C07D211/60 ,  C07D211/62 ,  C07D211/78 ,  C07D277/06 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D417/06 ,  C07D417/12 ,  C07D487/08

Abstract: The present invention relates to piperazine and piperidine derivatives, which are especially useful for treating or preventing neuronal damage, particularly damage associated with neurological diseases. These compounds are also useful for stimulating nerve growth. The invention also provides compositions comprising the compounds of the present invention and methods of utilizing those compositions for treating or preventing neuronal damage or for stimulating nerve growth.

公开(公告)号：AU6075400A

公开(公告)日：2001-01-22

申请号：AU6075400

申请日：2000-07-06

Applicant: VERTEX PHARMA

Inventor： LAUFFER DAVID ,  LEDFORD BRIAN ,  MULLICAN MICHAEL

IPC: A61K31/4409 ,  A61K31/444 ,  A61K38/22 ,  A61P9/10 ,  A61P21/04 ,  A61P25/00 ,  A61P25/02 ,  A61P25/14 ,  A61P25/16 ,  A61P25/28 ,  A61P27/02 ,  C07D213/40 ,  A61K31/4465

Abstract: The present invention relates N-substituted glycine derivatives for treating or preventing neuronal damage associated with neurological diseases. The invention also provides compositions comprising the compounds of the present invention and methods of utilizing those compositions for treating or preventing neuronal damage.