公开(公告)号：WO0170695A8

公开(公告)日：2001-11-29

申请号：PCT/US0109256

申请日：2001-03-22

Applicant: VERTEX PHARMA ,  SALITURO FRANCESCO ,  BEMIS GUY ,  EVINDAR GHOTAS

Inventor： SALITURO FRANCESCO ,  BEMIS GUY ,  EVINDAR GHOTAS

IPC: C07D487/04 ,  A61K31/4418 ,  A61K31/519 ,  A61P1/04 ,  A61P1/16 ,  A61P1/18 ,  A61P3/10 ,  A61P5/14 ,  A61P7/00 ,  A61P7/02 ,  A61P7/04 ,  A61P7/06 ,  A61P7/10 ,  A61P9/00 ,  A61P9/04 ,  A61P9/10 ,  A61P11/00 ,  A61P11/06 ,  A61P13/12 ,  A61P17/00 ,  A61P17/06 ,  A61P19/02 ,  A61P19/08 ,  A61P19/10 ,  A61P21/04 ,  A61P25/00 ,  A61P25/04 ,  A61P25/16 ,  A61P25/28 ,  A61P29/00 ,  A61P29/02 ,  A61P31/04 ,  A61P31/12 ,  A61P35/00 ,  A61P35/02 ,  A61P37/00 ,  A61P37/02 ,  A61P37/06 ,  A61P37/08 ,  A61P43/00 ,  C07D213/75 ,  C07D489/04 ,  A61K31/4402 ,  A61K31/5025

CPC classification number: C07D213/75 ,  C07D489/04

Abstract: The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli, having the formula (III), or tautomers thereof or pharmaceutically acceptable salts thereof, wherein: each of Q1 and Q2 are independently selected from 5-6 membered aromatic carbocyclic or heterocyclic ring systems, or 8-10 membered bicyclic ring systems comprising aromatic carbocyclic rings, aromatic heterocyclic rings or a combination of an aromatic carbocyclic ring and an aromatic heterocyclic ring. 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.

Abstract translation: 本发明涉及p38的抑制剂，哺乳动物蛋白激酶涉及细胞增殖，细胞死亡和对细胞外刺激的反应，具有式（III）或其互变异构体或其药学上可接受的盐，其中：Q1和Q2各自独立地 选自5-6元芳族碳环或杂环系统，或包含芳族碳环，芳族杂环或芳族碳环和芳族杂环的组合的8-10元双环体系。 本发明还涉及生产这些抑制剂的方法。 本发明还提供包含本发明抑制剂的药物组合物和利用这些组合物治疗和预防各种疾病的方法。

公开(公告)号：WO2008024196A1

公开(公告)日：2008-02-28

申请号：PCT/US2007/017542

申请日：2007-08-07

Applicant: PRAECIS PHARMACEUTICALS INCORPORATED ,  EVINDAR, Ghotas ,  DENG, Hongfeng

Inventor： EVINDAR, Ghotas ,  DENG, Hongfeng

IPC: C07C237/04 ,  A61K31/197 ,  A61P37/00

CPC classification number: C07C237/04

Abstract: The invention provides compounds formula (I), their preparation, and their use as pharmaceutically active immunosuppressive agents for the treatment of autoimmune disorders, organ transplant rejection, disorders associated with an activated immune system, as well as other disorders modulated by lymphopenia or S1P receptors.

Abstract translation: 本发明提供化合物式（I），其制备方法及其作为药物活性免疫抑制剂用于治疗自身免疫性疾病，器官移植排斥，与活化的免疫系统相关的病症以及由淋巴细胞减少或S1P受体调节的其它障碍的用途 。

公开(公告)号：WO2008016692A2

公开(公告)日：2008-02-07

申请号：PCT/US2007/017282

申请日：2007-08-01

Applicant: PRAECIS PHARMACEUTICALS INCORPORATED ,  EVINDAR, Ghotas ,  DENG, Hongfeng ,  BERNIER, Sylvie ,  YAO, Gang ,  COFFIN, Aaron ,  YANG, Hongfang

Inventor： EVINDAR, Ghotas ,  DENG, Hongfeng ,  BERNIER, Sylvie ,  YAO, Gang ,  COFFIN, Aaron ,  YANG, Hongfang

IPC: C07D213/38 ,  C07D239/26 ,  C07D261/08 ,  C07D271/10 ,  C07D277/28 ,  C07D285/12 ,  C07D417/12 ,  C07F9/6539 ,  A61K31/425 ,  A61K31/433 ,  A61K31/44 ,  A61K31/505 ,  A61P37/00

CPC classification number: C07D277/28 ,  C07D213/38 ,  C07D261/08 ,  C07D271/10 ,  C07D285/12 ,  C07D417/12 ,  C07F9/582 ,  C07F9/65033 ,  C07F9/65122 ,  C07F9/653 ,  C07F9/65312 ,  C07F9/65318 ,  C07F9/6539 ,  C07F9/65395

Abstract: The invention provides compounds formula I, their preparation, and their use as pharmaceutically active immunosuppressive agents for the treatment of autoimmune disorders, organ transplant rejection, disorders associated with an activated immune system, as well as other disorders modulated by lymphopenia or SlP receptors.

公开(公告)号：WO2007092190A2

公开(公告)日：2007-08-16

申请号：PCT/US2007/002353

申请日：2007-01-30

Applicant: PRAECIS PHARMACEUTICALS, INC. ,  DENG, Hongfeng ,  EVINDAR, Ghotas ,  KAVARANA, Malcolm, J. ,  MORGAN, Barry ,  SAHA, Ashis, K. ,  SATZ, Alexander, L.

Inventor： DENG, Hongfeng ,  EVINDAR, Ghotas ,  KAVARANA, Malcolm, J. ,  MORGAN, Barry ,  SAHA, Ashis, K. ,  SATZ, Alexander, L.

IPC: A61K31/16 ,  A61K31/33 ,  C07C235/00 ,  C07D231/12 ,  C07D233/64 ,  C07D239/26 ,  C07D249/06 ,  C07D261/08 ,  C07D263/32 ,  C07D271/10 ,  C07D277/28 ,  C07D285/12 ,  C07D307/42 ,  C07D317/58 ,  C07D317/64 ,  C07D471/04 ,  C07F9/00 ,  A61P37/02

CPC classification number: C07F9/65062 ,  C07B2200/07 ,  C07C237/04 ,  C07C237/42 ,  C07C255/60 ,  C07C271/22 ,  C07C317/40 ,  C07C323/41 ,  C07C2601/14 ,  C07D207/12 ,  C07D209/88 ,  C07D213/30 ,  C07D231/12 ,  C07D233/54 ,  C07D233/64 ,  C07D239/26 ,  C07D249/06 ,  C07D261/08 ,  C07D263/32 ,  C07D271/10 ,  C07D277/28 ,  C07D285/12 ,  C07D307/42 ,  C07D317/58 ,  C07D317/64 ,  C07D333/16 ,  C07D417/10 ,  C07D471/04 ,  C07F9/091 ,  C07F9/65033 ,  C07F9/65037 ,  C07F9/65122 ,  C07F9/65181 ,  C07F9/65182 ,  C07F9/653 ,  C07F9/65312 ,  C07F9/6539 ,  C07F9/65395 ,  C07F9/65517 ,  C07F9/6561

Abstract: The present invention relates to compounds which modulate the activity of the SlPl receptor, the use of these compounds for treating conditions associated with signaling through the SlPl receptor, and pharmaceutical compositions comprising these compounds.

Abstract translation: 本发明涉及调节S1P1受体活性的化合物，这些化合物用于治疗与通过S1P1受体的信号传导相关的病症的用途，以及包含这些化合物的药物组合物。

公开(公告)号：WO2008097819A3

公开(公告)日：2008-11-13

申请号：PCT/US2008052735

申请日：2008-02-01

Applicant: SMITHKLINE BEECHAM CORP ,  COFFIN AARON ,  EVINDAR GHOTAS ,  YAO GANG

Inventor： COFFIN AARON ,  EVINDAR GHOTAS ,  YAO GANG

IPC: C07D207/12 ,  C07D207/16

CPC classification number: A61K31/403 ,  C07D207/12 ,  C07D207/16 ,  C07F9/5532 ,  C07F9/568 ,  C07F9/5722 ,  C07F9/592 ,  C07F9/65583

Abstract: The invention provides compounds formula I, their preparation, and their use as pharmaceutically active immunosuppressive agents for the treatment of autoimmune disorders, organ transplant rejection, disorders associated with an activated immune system, as well as other disorders modulated by lymphopenia or SlP receptors.

Abstract translation: 本发明提供了式I化合物，其制备方法及其作为药物活性免疫抑制剂用于治疗自身免疫病症，器官移植排斥反应，与激活的免疫系统相关的病症以及由淋巴细胞减少症或S1P受体调节的其他病症的用途。

公开(公告)号：WO2008091967A1

公开(公告)日：2008-07-31

申请号：PCT/US2008/051832

申请日：2008-01-24

Applicant: SMITHKLINE BEECHAM CORPORATION ,  DENG, Hongfeng ,  EVINDAR, Ghotas ,  YAO, Gang

Inventor： DENG, Hongfeng ,  EVINDAR, Ghotas ,  YAO, Gang

IPC: A61K31/12 ,  C07C233/07

CPC classification number: C07D417/10 ,  C07F9/65318 ,  C07F9/65583

Abstract: The invention provides compounds Formula (I), their preparation, and their use as pharmaceutically active immunosuppressive agents for the treatment of autoimmune disorders, organ transplant rejection, disorders associated with an activated immune system, as well as other disorders modulated by lymphopenia or SlP receptors.

Abstract translation: 本发明提供化合物式（I），其制备及其作为药物活性免疫抑制剂用于治疗自身免疫性疾病，器官移植排斥，与活化的免疫系统相关的病症以及由淋巴细胞减少或S1P受体调节的其它障碍的用途 。

公开(公告)号：WO2008016692A3

公开(公告)日：2008-03-20

申请号：PCT/US2007017282

申请日：2007-08-01

Applicant: PRAECIS PHARM INC ,  EVINDAR GHOTAS ,  DENG HONGFENG ,  BERNIER SYLVIE ,  YAO GANG ,  COFFIN AARON ,  YANG HONGFANG

Inventor： EVINDAR GHOTAS ,  DENG HONGFENG ,  BERNIER SYLVIE ,  YAO GANG ,  COFFIN AARON ,  YANG HONGFANG

IPC: C07D213/38 ,  A61K31/425 ,  A61K31/433 ,  A61K31/44 ,  A61K31/505 ,  A61P37/00 ,  C07D261/08 ,  C07D271/10 ,  C07D277/28 ,  C07D285/12 ,  C07D417/12 ,  C07F9/6539

CPC classification number: C07D277/28 ,  C07D213/38 ,  C07D261/08 ,  C07D271/10 ,  C07D285/12 ,  C07D417/12 ,  C07F9/582 ,  C07F9/65033 ,  C07F9/65122 ,  C07F9/653 ,  C07F9/65312 ,  C07F9/65318 ,  C07F9/6539 ,  C07F9/65395

Abstract: The invention provides compounds formula I, their preparation, and their use as pharmaceutically active immunosuppressive agents for the treatment of autoimmune disorders, organ transplant rejection, disorders associated with an activated immune system, as well as other disorders modulated by lymphopenia or SlP receptors.

Abstract translation: 本发明提供式I化合物及其制备方法及其作为药物活性免疫抑制剂用于治疗自身免疫疾病，器官移植排斥，与活化的免疫系统相关的病症以及由淋巴细胞减少或S1P受体调节的其它病症的用途。

公开(公告)号：WO2008016674A1

公开(公告)日：2008-02-07

申请号：PCT/US2007/017243

申请日：2007-08-01

Applicant: PRAECIS PHARMACEUTICALS INCORPORATED ,  DENG, Hongfeng ,  EVINDAR, Ghotas ,  BERNIER, Sylvie ,  YAO, Gang ,  COFFIN, Aaron ,  YANG, Hongfang ,  ACHARYA, Raksha, A.

Inventor： DENG, Hongfeng ,  EVINDAR, Ghotas ,  BERNIER, Sylvie ,  YAO, Gang ,  COFFIN, Aaron ,  YANG, Hongfang ,  ACHARYA, Raksha, A.

IPC: C07D277/28 ,  C07D285/12 ,  C07F9/09 ,  A61K31/426 ,  A61K31/433 ,  A61K31/661 ,  A61P25/28

CPC classification number: C07D285/12 ,  C07D277/28 ,  C07F9/6539 ,  C07F9/65395

Abstract: The invention provides compounds of formula I and formula II, their preparation, a their use as pharmaceutically active immunosuppressive agents for the treatment of autoimmune disorders, organ transplant rejection, disorders associated with an activated immune system, as well as other disorders modulated by lymphopenia or SlP receptors.

Abstract translation: 本发明提供式I和式II化合物及其制备，它们作为药物活性免疫抑制剂用于治疗自身免疫性疾病，器官移植排斥，与活化的免疫系统相关的病症，以及由淋巴细胞减少或其它调节的其它疾病 S1P受体。

公开(公告)号：WO2008097819A2

公开(公告)日：2008-08-14

申请号：PCT/US2008/052735

申请日：2008-02-01

Applicant: SMITHKLINE BEECHAM CORPORATION ,  COFFIN, Aaron ,  EVINDAR, Ghotas ,  YAO, Gang

Inventor： COFFIN, Aaron ,  EVINDAR, Ghotas ,  YAO, Gang

IPC: A61K31/403

CPC classification number: A61K31/403 ,  C07D207/12 ,  C07D207/16 ,  C07F9/5532 ,  C07F9/568 ,  C07F9/5722 ,  C07F9/592 ,  C07F9/65583

Abstract: The invention provides compounds formula I, their preparation, and their use as pharmaceutically active immunosuppressive agents for the treatment of autoimmune disorders, organ transplant rejection, disorders associated with an activated immune system, as well as other disorders modulated by lymphopenia or SlP receptors.

Abstract translation: 本发明提供了式I化合物，其制备以及它们作为药物活性免疫抑制剂用于治疗自身免疫病症，器官移植排斥，与激活的免疫系统相关的病症以及其他病症的用途 受淋巴细胞减少或S1P受体调节。

公开(公告)号：WO2008019090A3

公开(公告)日：2008-03-20

申请号：PCT/US2007017384

申请日：2007-08-02

Applicant: PRAECIS PHARM INC ,  EVINDAR GHOTAS ,  DENG HONGFENG

Inventor： EVINDAR GHOTAS ,  DENG HONGFENG

IPC: C07D233/64 ,  A61K31/167 ,  A61K31/426 ,  A61K31/433 ,  A61K31/661 ,  A61P25/28 ,  C07C237/20 ,  C07D241/04 ,  C07D241/08 ,  C07D277/28 ,  C07D285/12 ,  C07F9/09

CPC classification number: C07D277/28 ,  C07B2200/07 ,  C07C323/41 ,  C07D233/64 ,  C07D241/04 ,  C07D241/08 ,  C07D285/12 ,  C07F9/091 ,  C07F9/65062 ,  C07F9/650964 ,  C07F9/6539 ,  C07F9/65395

Abstract: The invention provides compounds formulae I-III, their preparation, and their use as pharmaceutically active immunosuppressive agents for the treatment of autoimmune disorders, organ transplant rejection, disorders associated with an activated immune system, as well as other disorders modulated by lymphopenia or SlP receptors.

Abstract translation: 本发明提供化合物式I-III，它们的制备及其作为药物活性免疫抑制剂用于治疗自身免疫性疾病，器官移植排斥，与活化的免疫系统相关的病症以及由淋巴细胞减少或S1P受体调节的其它病症的用途 。