公开(公告)号：WO2010042649A3

公开(公告)日：2010-11-18

申请号：PCT/US2009059888

申请日：2009-10-07

Applicant: AMGEN INC ,  TASKER ANDREW ,  FALSEY JAMES RICHARD ,  RZASA ROBERT M ,  HERBERICH BRADLEY J ,  ZHANG DAWEI

Inventor： TASKER ANDREW ,  FALSEY JAMES RICHARD ,  RZASA ROBERT M ,  HERBERICH BRADLEY J ,  ZHANG DAWEI

IPC: C07D237/30 ,  A61K31/498 ,  A61P29/00 ,  C07D237/32 ,  C07D237/34

CPC classification number: C07D401/12 ,  C07D237/30 ,  C07D237/32 ,  C07D237/34 ,  C07D401/04 ,  C07D403/04 ,  C07D413/04

Abstract: The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation and related conditions. The compounds have a general Formula I wherein A4, L, R1, R2, R3, R5 and m are as defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, uses of such compounds and compositions for treatment of p38 map kinase mediated diseases including rheumatoid arthritis, psoriasis, chronic obstructive pulmonary disease, ankylosing spondylitis, pain and other inflammatory disorders, as well as intermediates and processes useful for the preparation of compounds of Formula I.

Abstract translation: 本发明包括一类新的可用于预防和治疗蛋白激酶介导的疾病，包括炎症和相关病症的化合物。 该化合物具有通式I，其中A4，L，R1，R2，R3，R5和m如本文所定义。 本发明还包括药物组合物，其包含一种或多种式I化合物，这些化合物和组合物用于治疗p38地图激酶介导的疾病，包括类风湿性关节炎，牛皮癣，慢性阻塞性肺病，强直性脊柱炎，疼痛和其它炎症性疾病的用途，如 以及可用于制备式I化合物的中间体和方法。

公开(公告)号：WO2008011109A2

公开(公告)日：2008-01-24

申请号：PCT/US2007/016382

申请日：2007-07-17

Applicant: AMGEN INC. ,  HU, Essa ,  HUMAN, Jason, Brooks ,  KUNZ, Roxanne ,  TASKER, Andrew ,  WHITE, Ryan

Inventor： HU, Essa ,  HUMAN, Jason, Brooks ,  KUNZ, Roxanne ,  TASKER, Andrew ,  WHITE, Ryan

IPC: C07D401/04 ,  C07D471/04 ,  A61P35/00 ,  A61K31/517 ,  A61K31/4709

CPC classification number: C07D471/04 ,  C07D401/04

Abstract: The present invention comprises a new class of compounds capable of modulating the c-kit receptor and, accordingly, useful for treatment of c-kit mediated diseases, including various inflammatory, fibrotic and/or mast cell mediated diseases such as mastocytosis. The compounds have a general Formula: (I); wherein A0-3 and R1-6 are defined herein. The invention further comprises pharmaceutical compositions, methods for treatment of c-kit mediated diseases, and intermediates and processes useful for the preparation of compounds of the invention.

Abstract translation: 本发明包括能够调节c-kit受体的新一类化合物，因此可用于治疗c-kit介导的疾病，包括各种炎性，纤维化和/或肥大细胞介导的疾病如肥大细胞增多症。 该化合物具有通式：（I）; 其中A0-3和R1-6在本文中定义。 本发明还包括药物组合物，用于治疗c-kit介导的疾病的方法，以及可用于制备本发明化合物的中间体和方法。

公开(公告)号：WO2007124181A3

公开(公告)日：2007-11-01

申请号：PCT/US2007/010093

申请日：2007-04-23

Applicant: AMGEN INC. ,  HONG, Fang-Tsao ,  FALSEY, James R. ,  RZASA, Robert M. ,  TADESSE, Seifu ,  TASKER, Andrew

Inventor： HONG, Fang-Tsao ,  FALSEY, James R. ,  RZASA, Robert M. ,  TADESSE, Seifu ,  TASKER, Andrew

IPC: C07D495/04 ,  A61K31/519 ,  A61P29/00

Abstract: The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation and related conditions. The compounds have a general Formula (I), wherein A 1 , A 2 , B, R 2 and R 3 are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula (I), uses of such compounds and compositions for treatment of kinase mediated diseases including rheumatoid arthritis, psoriasis and other inflammation disorders, as well as intermediates and processes useful for the preparation of compounds of Formula (I).

公开(公告)号：WO2007084391A2

公开(公告)日：2007-07-26

申请号：PCT/US2007000871

申请日：2007-01-11

Applicant: AMGEN INC ,  ZENG QINGPING ,  ALLEN JOHN G ,  BOURBEAU MATTHEW P ,  DOMINGUEZ CELIA ,  FOTSCH CHRISTOPHER H ,  HAN NIANHE ,  HONG FANG-TSAO ,  HUANG XIN ,  LEE MATTHEW R ,  LI AIWEN ,  LIU QINGYIAN ,  RIDER JAMES T ,  TADESSE SEIFU ,  TASKER ANDREW S ,  VISWANADHAN VELLARKAD N ,  WANG XIANGHONG ,  WEILER KURT E ,  WOHLHIETER GEORGE E ,  YAO GUOMIN ,  YUAN CHESTER CHENGUANG

Inventor： ZENG QINGPING ,  ALLEN JOHN G ,  BOURBEAU MATTHEW P ,  DOMINGUEZ CELIA ,  FOTSCH CHRISTOPHER H ,  HAN NIANHE ,  HONG FANG-TSAO ,  HUANG XIN ,  LEE MATTHEW R ,  LI AIWEN ,  LIU QINGYIAN ,  RIDER JAMES T ,  TADESSE SEIFU ,  TASKER ANDREW S ,  VISWANADHAN VELLARKAD N ,  WANG XIANGHONG ,  WEILER KURT E ,  WOHLHIETER GEORGE E ,  YAO GUOMIN ,  YUAN CHESTER CHENGUANG

IPC: C07D417/04 ,  C07D277/42 ,  C07D277/54 ,  C07D417/14 ,  C07D471/04 ,  C07D495/04 ,  C07D513/04

CPC classification number: C07D417/04 ,  C07D417/14 ,  C07D471/04 ,  C07D495/04 ,  C07D513/04

Abstract: The invention relates to thiazole compounds of Formula (I) and Formula (II) and compositions thereof useful for treating diseases mediated by protein kinase B (PKB) where the variables have the definitions provided herein. The invention also relates to the therapeutic use of such thiazole compounds and compositions thereof in treating disease states associated with abnormal cell growth, cancer, inflammation, and metabolic disorders.

Abstract translation: 本发明涉及式（I）和式（II）的噻唑化合物及其组合物，其用于治疗由蛋白激酶B（PKB）介导的疾病，其中变量具有本文提供的定义。 本发明还涉及这种噻唑化合物及其组合物在治疗与异常细胞生长，癌症，炎症和代谢紊乱相关的疾病状态中的治疗用途。

公开(公告)号：WO2006060318A3

公开(公告)日：2006-06-08

申请号：PCT/US2005/042935

申请日：2005-11-29

Applicant: AMGEN INC. ,  KIM, Tae-seong ,  BELLON, Steven ,  BOOKER, Shon ,  D'ANGELO, Noel ,  DOMINGUEZ, Celia ,  FELLOWS, Ingrid ,  LEE, Matthew ,  LIU, Longbin ,  RAINBEAU, Elizabeth ,  SIEGMUND, Aaron, C. ,  TASKER, Andrew ,  XI, Ning ,  CHENG, Yuan

Inventor： KIM, Tae-seong ,  BELLON, Steven ,  BOOKER, Shon ,  D'ANGELO, Noel ,  DOMINGUEZ, Celia ,  FELLOWS, Ingrid ,  LEE, Matthew ,  LIU, Longbin ,  RAINBEAU, Elizabeth ,  SIEGMUND, Aaron, C. ,  TASKER, Andrew ,  XI, Ning ,  CHENG, Yuan

IPC: A61K31/4709 ,  C07D401/12 ,  C07D401/14 ,  A61P35/00

Abstract: Selected compounds of Formula (I) are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases such as cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes. R - X - W - A - Y - R Formula (I) wherein R is X is O, S, NR2 or CR3R4 W is an substituted or unsubstituted aryl or substituted or unsubstituted 5- or 6- membered heteroaryl.

公开(公告)号：WO2010042646A1

公开(公告)日：2010-04-15

申请号：PCT/US2009/059883

申请日：2009-10-07

Applicant: AMGEN INC. ,  TASKER, Andrew ,  PETTUS, Liping H. ,  WURZ, Ryan

Inventor： TASKER, Andrew ,  PETTUS, Liping H. ,  WURZ, Ryan

IPC: C07D471/04 ,  A61K31/5025 ,  A61P29/00

CPC classification number: C07D471/04

Abstract: The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation and related conditions. The compounds have a general Formula (I) wherein A 1 , A 2 , A 3 , A 4 , L, R 1 , R 2 , R 3 , R 5 and m are as defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, uses of such compounds and compositions for treatment of p38 map kinase mediated diseases including rheumatoid arthritis, psoriasis, chronic obstructive pulmonary disease, ankylosing spondylitis, pain and other inflammatory disorders, as well as intermediates and processes useful for the preparation of compounds of Formula (I).

Abstract translation: 本发明包括一类新的可用于预防和治疗蛋白激酶介导的疾病，包括炎症和相关病症的化合物。 化合物具有通式（I），其中A1，A2，A3，A4，L，R1，R2，R3，R5和m如本文所定义。 本发明还包括药物组合物，其包含一种或多种式I化合物，这些化合物和组合物用于治疗p38地图激酶介导的疾病，包括类风湿性关节炎，牛皮癣，慢性阻塞性肺病，强直性脊柱炎，疼痛和其它炎症性疾病的用途，如 以及可用于制备式（I）化合物的中间体和方法。

公开(公告)号：WO2009038784A1

公开(公告)日：2009-03-26

申请号：PCT/US2008/010931

申请日：2008-09-19

Applicant: AMGEN INC. ,  PETTUS, Liping H. ,  SHAM, Kelvin K., C. ,  TASKER, Andrew ,  XU, Shimin

Inventor： PETTUS, Liping H. ,  SHAM, Kelvin K., C. ,  TASKER, Andrew ,  XU, Shimin

IPC: C07D249/18 ,  C07D403/12 ,  C07D405/04 ,  A61K31/4192 ,  A61P29/00

CPC classification number: C07D249/18 ,  C07D401/04 ,  C07D403/04 ,  C07D403/12 ,  C07D409/04 ,  C07D413/04 ,  C07D413/12 ,  C07D413/14 ,  C07D417/06 ,  C07D417/12 ,  C07D471/04

Abstract: The present invention comprises a new class of compounds useful for modulating the activity of p38 MAP kinase. The compounds have a general Formula (I) wherein A 1 , A 2 , A 3 , A 4 , A 5 , A 6 , R 1 and R 5 are defined herein. The invention further provides pharmaceutical compositions including one or more compounds of Formula (I), use of such compounds and compositions for treatment of p38 MAP kinase mediated diseases including rheumatoid arthritis, psoriasis and other inflammatory disorders, as well as intermediates and processes useful for the preparation of compounds of Formula (I).

Abstract translation: 本发明包括一类可用于调节p38 MAP激酶活性的化合物。 化合物具有通式（I），其中A1，A2，A3，A4，A5，A6，R1和R5如本文所定义。 本发明进一步提供包含一种或多种式（I）化合物的药物组合物，这些化合物和组合物用于治疗p38 MAP激酶介导的疾病（包括类风湿性关节炎，牛皮癣和其它炎症性疾病）的用途，以及可用于 式（I）化合物的制备。

公开(公告)号：WO2009006548A3

公开(公告)日：2009-03-19

申请号：PCT/US2008069085

申请日：2008-07-02

Applicant: NONO INC ,  ARBOR VITA CORP ,  TASKER ANDREW ,  DOUCETTE TRACY ,  TYMIANSKI MICHAEL ,  MENDOZA KENNETH ,  BELMARES MICHAEL P ,  GARMAN DAVID ,  LU PETER S

Inventor： TASKER ANDREW ,  DOUCETTE TRACY ,  TYMIANSKI MICHAEL ,  MENDOZA KENNETH ,  BELMARES MICHAEL P ,  GARMAN DAVID ,  LU PETER S

IPC: A61K38/04 ,  C12P21/04

CPC classification number: A61K38/1787 ,  A61K38/07

Abstract: The invention provides methods of treating or effecting prophylaxis of a patient having or at risk of developing symptoms of anxiety in which an effective regime of an agent that inhibits specific binding of PSD95 to an NMDA receptor is administered to a patient.

Abstract translation: 本发明提供了治疗或有效预防患有焦虑症状或具有发展焦虑症状风险的患者的方法，其中向患者施用抑制PSD95与NMDA受体的特异性结合的药剂的有效方案。

公开(公告)号：WO2008137176A1

公开(公告)日：2008-11-13

申请号：PCT/US2008/005865

申请日：2008-05-06

Applicant: AMGEN INC. ,  PETTUS, Liping H. ,  TASKER, Andrew ,  XU, Shimin ,  WURZ, Ryan

Inventor： PETTUS, Liping H. ,  TASKER, Andrew ,  XU, Shimin ,  WURZ, Ryan

IPC: C07D471/04 ,  A61K31/437

CPC classification number: C07D471/04

Abstract: The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation and related conditions. The compounds have a general Formula (I) wherein A 1 , A 2 , A 3 , A 4 , B, R 1 , R 2 , R 3 , R 4 and R 5 are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, uses of such compounds and compositions for treatment of P38 map kinase mediated diseases including rheumatoid arthritis, psoriasis, chronic obstructive pulmonary disease, pain and other inflammatory disorders, as well as intermediates and processes useful for the preparation of compounds of Formula I.

Abstract translation: 本发明包括一类新的可用于预防和治疗蛋白激酶介导的疾病，包括炎症和相关病症的化合物。 化合物具有通式（I），其中A 1，A 2，A 3，A 4， B，R 1，R 2，R 3，R 4和R 5 O >在本文中定义。 本发明还包括药物组合物，其包含一种或多种式I化合物，用于治疗P38地图激酶介导的疾病（包括类风湿性关节炎，牛皮癣，慢性阻塞性肺病，疼痛和其它炎症性疾病）的这些化合物和组合物的用途以及中间体 和可用于制备式I化合物的方法。

公开(公告)号：WO2008045393A2

公开(公告)日：2008-04-17

申请号：PCT/US2007/021505

申请日：2007-10-05

Applicant: AMGEN INC. ,  ZHANG, Dawei ,  TASKER, Andrew ,  SHAM, Kelvin, K.C. ,  CHAKRABARTI, Partha, Pratim ,  FALSEY, Richard, James ,  HERBERICH, Bradley, J. ,  PETTUS, Liping, H. ,  RZASA, Robert, M.

Inventor： ZHANG, Dawei ,  TASKER, Andrew ,  SHAM, Kelvin, K.C. ,  CHAKRABARTI, Partha, Pratim ,  FALSEY, Richard, James ,  HERBERICH, Bradley, J. ,  PETTUS, Liping, H. ,  RZASA, Robert, M.

CPC classification number: C07D471/04

Abstract: The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation and related conditions. The compounds have general Formula (I), wherein A, B, R 1 , R 2 , R 3 and R 4 are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula (I), uses of such compounds and compositions for treatment of P38 map kinase mediated diseases including rheumatoid arthritis, psoriasis and other inflammation disorders, as well as intermediates and processes useful for the preparation of compounds of Formula (I).

Abstract translation: 本发明包括一类新的可用于预防和治疗蛋白激酶介导的疾病，包括炎症和相关病症的化合物。 化合物具有通式（I），其中A，B，R 1，R 2，R 3和R 4， / SUP>。 本发明还包括包含一种或多种式（I）化合物的药物组合物，这些化合物和组合物用于治疗P38地图激酶介导的疾病（包括类风湿性关节炎，牛皮癣和其他炎症疾病）的用途，以及可用于 式（I）化合物的制备。