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公开(公告)号:NO20051207A
公开(公告)日:2005-05-18
申请号:NO20051207
申请日:2005-03-08
Applicant: VERTEX PHARMA
Inventor: GREEN JEREMY , HALE MICHAEL , MALTAIS FRANCOIS , LEDFORD BRIAN E , COCHDRAN JOHN , NANTHAJUMAR SUGANTHINI
IPC: C07D239/00 , A61P19/00 , A61P25/00 , A61P29/00 , A61P35/00 , A61P37/00 , C07D213/74 , C07D239/42 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , A61K31/44
CPC classification number: C07D213/74 , C07D239/42 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12
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公开(公告)号:NZ517694A
公开(公告)日:2005-03-24
申请号:NZ51769400
申请日:2000-08-11
Applicant: VERTEX PHARMA
Inventor: GREEN JEREMY , BEMIS GUY , GRILLOT ANNE-LAURE , LEDEBOER MARK , SALITURO FRANCIS , HARRINGTON EDMUND , GAO HUAI , AKER CHRISTOPHER , CAO JINGRONG , HALE MICHAEL
IPC: A61K31/341 , A61K31/4155 , A61K31/4192 , A61K31/42 , A61K31/4439 , A61K31/4545 , A61K31/506 , A61K31/5377 , A61P1/04 , A61P1/16 , A61P1/18 , A61P3/10 , A61P7/02 , A61P7/04 , A61P7/06 , A61P9/00 , A61P9/10 , A61P11/02 , A61P11/06 , A61P13/12 , A61P17/00 , A61P17/06 , A61P19/02 , A61P19/08 , A61P19/10 , A61P21/02 , A61P21/04 , A61P25/00 , A61P25/14 , A61P25/16 , A61P25/28 , A61P29/00 , A61P31/00 , A61P35/00 , A61P35/02 , A61P37/00 , A61P37/02 , A61P37/06 , A61P37/08 , A61P43/00 , C07D413/04 , C07D413/14 , C07D401/04 , C07D405/04 , C07D403/04
Abstract: Disclosed herein are compounds of formula (I), wherein R1 is H, CONH2, T(n)-R, or T(n)-Ar2; G is R or Ar1; R is an aliphatic or substituted aliphatic group; n may be zero or one; and Ar1, Ar2, XYZ, and Q are as described in the specification. These compounds are inhibitors of protein kinase, particularly inhibitors of JNK, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. Also disclosed are methods for producing these inhibitors, and pharmaceutical compositions comprising these inhibitors and methods of utilizing those compositions in the treatment and prevention of various disorders.
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公开(公告)号:ZA200305799B
公开(公告)日:2004-07-28
申请号:ZA200305799
申请日:2003-07-28
Applicant: VERTEX PHARMA
Inventor: CAO JINGRONG , GREEN JEREMY , MALTAIS FRANCOIS , STRAUB JUDY , TANG QING , ARONOV ALEX , HALE MICHAEL
IPC: A61K20060101 , A61P20060101 , C07D20060101 , C07D , A61K , A61P
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公开(公告)号:ZA200301696B
公开(公告)日:2004-04-28
申请号:ZA200301696
申请日:2001-09-14
Applicant: VERTEX PHARMA
Inventor: HALE MICHAEL , JANETKA JAMES , MALTAIS FRANCOIS , CAO JINGRONG , MASHAL ROBERT
IPC: A61K31/42 , A61K31/433 , A61K31/4439 , A61K31/454 , A61K31/4725 , A61K31/496 , A61K31/5377 , A61K31/551 , A61K45/00 , A61P1/00 , A61P1/02 , A61P1/16 , A61P1/18 , A61P3/10 , A61P5/00 , A61P7/02 , A61P9/00 , A61P9/04 , A61P9/08 , A61P9/10 , A61P11/00 , A61P11/06 , A61P13/08 , A61P13/10 , A61P13/12 , A61P15/00 , A61P17/00 , A61P17/06 , A61P19/00 , A61P19/02 , A61P19/04 , A61P25/00 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/20 , A61P25/28 , A61P29/00 , A61P31/00 , A61P31/12 , A61P35/00 , A61P35/02 , A61P37/02 , A61P37/08 , A61P43/00 , C07D413/04 , C07D413/14 , C07D417/14 , C07D , A61K , A61P
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公开(公告)号:YU39800A
公开(公告)日:2004-03-12
申请号:YU39800
申请日:1998-03-09
Applicant: VERTEX PHARMA
Inventor: TUNG ROGER , HALE MICHAEL , BAKER CHRISTOPHER , FURFINE ERIC STEVEN , KALDOR ISTVAN , KAZMIERSKI MIECZYSLAW , SPALTENSTEIN ANDREW
IPC: A61K31/18 , A61K31/215 , A61K31/265 , A61K31/27 , A61K31/34 , A61K31/341 , A61K31/4025 , A61K31/496 , A61K31/66 , A61K31/661 , A61K31/664 , A61K31/7048 , A61K45/00 , A61P31/12 , A61P31/18 , A61P43/00 , C07C311/15 , C07C311/18 , C07C311/37 , C07D277/30 , C07D307/20 , C07D405/12 , C07D407/12 , C07D417/12 , C07F9/655 , C07F9/6584 , C07H15/04 , C07H15/26
Abstract: Ovaj pronalazak se odnosi na pro-lekove jedne klase sulfonamida koji su inhibitori aspartil proteaze. U jednoj realizaciji, ovaj pronalazak se odnosi na novu klasu pro-lekova inhibitora HIV aspartil proteaze koja se karakterišu pogodnom rastvorljivošću u vodi, visokom bioprihvatljivošću i lakim in vivo obrazovanjem aktivne komponente. Pronalazak se takodje odnosi na farmaceutske kompozicije koje sadrže ove pro-lekove. Pro-lekovi i farmaceutske kompozicije prema ovom pronalasku su izuzetno dobro pogodni za smanjenje tabletnog opterećenja ("pill burden") i povećanje saglasnosti pacijenta. Ovaj pronalazak se takodje odnosi na postupke za tretiranje sisara sa ovim prolekovima i farmaceutskim kompozicijama.
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公开(公告)号:BR0207114A
公开(公告)日:2004-02-25
申请号:BR0207114
申请日:2002-02-08
Applicant: VERTEX PHARMA
Inventor: CAO JINGRONG , GREEN JEREMY , HALE MICHAEL , MALTAIS FRANCOIS , STRAUB JUDY , TANG QING , ARONOV ALEX
IPC: A61K31/506 , A61K31/517 , A61K31/5377 , A61K31/551 , A61P1/16 , A61P3/10 , A61P5/00 , A61P7/02 , A61P9/08 , A61P9/10 , A61P17/06 , A61P19/00 , A61P25/00 , A61P25/28 , A61P29/00 , A61P31/04 , A61P31/12 , A61P35/00 , A61P37/06 , A61P37/08 , A61P43/00 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D413/14
Abstract: Described herein are compounds that are useful as protein kinase inhibitors having the formula: wherein Z 1 and Z 2 are each independently nitrogen or CH and Ring A, T m R 1 , QR 2 , U n R 3 , and Sp are as described in the specification. The compounds are especially useful as inhibitors of ERK2 and for treating diseases in mammals that are alleviated by a protein kinase inhibitor, particularly diseases such as cancer, inflammatory disorders, restenosis, diabetes, and cardiovascular disease.
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87.
公开(公告)号:HU0302991A2
公开(公告)日:2003-12-29
申请号:HU0302991
申请日:2001-09-14
Applicant: VERTEX PHARMA
Inventor: CAO JINGRONG , HALE MICHAEL , JANETKA JAMES , MALTAIS FRANCOIS , MASHAL ROBERT
IPC: A61K31/42 , A61K31/433 , A61K31/4439 , A61K31/454 , A61K31/4725 , A61K31/496 , A61K31/5377 , A61K31/551 , A61K45/00 , A61P1/00 , A61P1/02 , A61P1/16 , A61P1/18 , A61P3/10 , A61P5/00 , A61P7/02 , A61P9/00 , A61P9/04 , A61P9/08 , A61P9/10 , A61P11/00 , A61P11/06 , A61P13/08 , A61P13/10 , A61P13/12 , A61P15/00 , A61P17/00 , A61P17/06 , A61P19/00 , A61P19/02 , A61P19/04 , A61P25/00 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/20 , A61P25/28 , A61P29/00 , A61P31/00 , A61P31/12 , A61P35/00 , A61P35/02 , A61P37/02 , A61P37/08 , A61P43/00 , C07D413/04 , C07D413/14 , C07D417/14
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公开(公告)号:NO20033491L
公开(公告)日:2003-10-08
申请号:NO20033491
申请日:2003-08-06
Applicant: VERTEX PHARMA
Inventor: CAO JINGRONG , GREEN JEREMY , HALE MICHAEL , MALTAIS FRANCOIS , STRAUB JUDY , TANG QING , ARONOV ALEX
IPC: A61K31/506 , A61K31/517 , A61K31/5377 , A61K31/551 , A61P1/16 , A61P3/10 , A61P5/00 , A61P7/02 , A61P9/08 , A61P9/10 , A61P17/06 , A61P19/00 , A61P25/00 , A61P25/28 , A61P29/00 , A61P31/04 , A61P31/12 , A61P35/00 , A61P37/06 , A61P37/08 , A61P43/00 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D413/14
Abstract: Described herein are compounds that are useful as protein kinase inhibitors having the formula: wherein Z 1 and Z 2 are each independently nitrogen or CH and Ring A, T m R 1 , QR 2 , U n R 3 , and Sp are as described in the specification. The compounds are especially useful as inhibitors of ERK2 and for treating diseases in mammals that are alleviated by a protein kinase inhibitor, particularly diseases such as cancer, inflammatory disorders, restenosis, diabetes, and cardiovascular disease.
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公开(公告)号:BR0013551A
公开(公告)日:2003-06-17
申请号:BR0013551
申请日:2000-08-11
Applicant: VERTEX PHARMA
Inventor: GREEN JEREMY , BEMIS GUY , GRILLOT ANNE-LAURE , LEDERBOER MARK , SALITURO FRANCISCO , HARRINGTON EDMUNDO , GAO HUAI , BAKER CHRISTOPHER , CAO JINGRONG , HALE MICHAEL
IPC: A61K31/341 , A61K31/4155 , A61K31/4192 , A61K31/42 , A61K31/4439 , A61K31/4545 , A61K31/506 , A61K31/5377 , A61P1/04 , A61P1/16 , A61P1/18 , A61P3/10 , A61P7/02 , A61P7/04 , A61P7/06 , A61P9/00 , A61P9/10 , A61P11/02 , A61P11/06 , A61P13/12 , A61P17/00 , A61P17/06 , A61P19/02 , A61P19/08 , A61P19/10 , A61P21/02 , A61P21/04 , A61P25/00 , A61P25/14 , A61P25/16 , A61P25/28 , A61P29/00 , A61P31/00 , A61P35/00 , A61P35/02 , A61P37/00 , A61P37/02 , A61P37/06 , A61P37/08 , A61P43/00 , C07D413/04 , C07D413/14 , C07D401/04 , C07D405/04 , C07D403/04
Abstract: The present invention provides compounds of formula I: where R 1 is H, CONH 2 , T( n )-R, or T( n )-Ar 2 , n may be zero or one, and G, XYZ, and Q are as described below. These compounds are inhibitors of protein kinase, particularly inhibitors of JNK, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.
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公开(公告)号:CA2437767A1
公开(公告)日:2002-08-22
申请号:CA2437767
申请日:2002-02-08
Applicant: VERTEX PHARMA
Inventor: STRAUB JUDY , ARONOV ALEX , TANG QING , CAO JINGRONG , MALTAIS FRANCOIS , HALE MICHAEL , GREEN JEREMY
IPC: A61K31/506 , A61K31/517 , A61K31/5377 , A61K31/551 , A61P1/16 , A61P3/10 , A61P5/00 , A61P7/02 , A61P9/08 , A61P9/10 , A61P17/06 , A61P19/00 , A61P25/00 , A61P25/28 , A61P29/00 , A61P31/04 , A61P31/12 , A61P35/00 , A61P37/06 , A61P37/08 , A61P43/00 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D413/14
Abstract: Described herein are compounds that are useful as protein kinase inhibitors having the formula (I) wherein Z1 and Z2 are each independently nitrogen or CH and Ring A, TmR1, QR2, UnR3, and Sp are as described in the specification. The compounds are especially useful as inhibitors of ERK2 and for treating diseases in mammals that are alleviated by a protein kinase inhibitor, particularly diseases such as cancer, inflammatory disorders, restenosis, diabetes, and cardiovascular disease.
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