公开(公告)号：WO2006036664A1

公开(公告)日：2006-04-06

申请号：PCT/US2005/033659

申请日：2005-09-19

Applicant: AMGEN INC. ,  ASKEW, JR, Ben, C. ,  AYA, Toshihiro ,  BISWAS, Kaustav ,  CAI, Guolin ,  CHEN, Jian, J. ,  FOTSCH, Christopher, H. ,  HAN, Nianhe ,  HUMAN, Jason, Brooks ,  LI, Aiwen ,  LIU, Qingyian ,  PETERKIN, Tanya ,  QIAN, Wenyuan ,  RIAHI, Babak ,  YUAN, Chester, Chenguang ,  ZHU, Jiawang

Inventor： ASKEW, JR, Ben, C. ,  AYA, Toshihiro ,  BISWAS, Kaustav ,  CAI, Guolin ,  CHEN, Jian, J. ,  FOTSCH, Christopher, H. ,  HAN, Nianhe ,  HUMAN, Jason, Brooks ,  LI, Aiwen ,  LIU, Qingyian ,  PETERKIN, Tanya ,  QIAN, Wenyuan ,  RIAHI, Babak ,  YUAN, Chester, Chenguang ,  ZHU, Jiawang

IPC: C07C311/19 ,  C07D207/48 ,  C07D211/08 ,  A61K31/18 ,  A61K31/40 ,  A61K31/445

CPC classification number: C07D207/26 ,  C07C311/19 ,  C07C311/29 ,  C07C2601/02 ,  C07C2601/08 ,  C07C2602/10 ,  C07D211/38 ,  C07D215/36 ,  C07D233/24 ,  C07D243/08 ,  C07D275/06 ,  C07D281/02 ,  C07D291/08 ,  C07D295/135 ,  C07D311/68

Abstract: This invention is in the field of pharmaceutical agents and specifically relates to compounds, compositions, uses and methods for treating inflammation-related disorders, including pain.

Abstract translation: 本发明涉及药剂领域，具体涉及用于治疗炎症相关疾病（包括疼痛）的化合物，组合物，用途和方法。

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：WO2007061661A2

公开(公告)日：2007-05-31

申请号：PCT/US2006043951

申请日：2006-11-13

Applicant: AMGEN INC ,  BIOVITRUM AB ,  HENRIKSSON MARTIN ,  HOMAN EVERT ,  JOHANSSON LARS ,  VALLGARDA JERK ,  WILLIAMS MEREDITH ,  BERCOT ERIC A ,  FOTSCH CHRISTOPHER H ,  LI AIWEN ,  CAI GUOLIN ,  HUNGATE RANDALL W ,  YUAN CHESTER CHENGUANG ,  TEGLEY CHRISTOPHER ,  ST JEAN DAVID J JR ,  HAN NIANHE ,  HUANG QI ,  LIU QINGYIAN ,  BARTBEGER MICHAEL D ,  MONIZ GEORGE A ,  FRIZZLE MATTHEW J ,  MARSHALL TERESA L

Inventor： HENRIKSSON MARTIN ,  HOMAN EVERT ,  JOHANSSON LARS ,  VALLGARDA JERK ,  WILLIAMS MEREDITH ,  BERCOT ERIC A ,  FOTSCH CHRISTOPHER H ,  LI AIWEN ,  CAI GUOLIN ,  HUNGATE RANDALL W ,  YUAN CHESTER CHENGUANG ,  TEGLEY CHRISTOPHER ,  ST JEAN DAVID J JR ,  HAN NIANHE ,  HUANG QI ,  LIU QINGYIAN ,  BARTBEGER MICHAEL D ,  MONIZ GEORGE A ,  FRIZZLE MATTHEW J ,  MARSHALL TERESA L

IPC: C07D277/54 ,  A61K31/426 ,  A61K31/427 ,  C07D277/60 ,  C07D417/04 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14

CPC classification number: C07D277/54 ,  C07D277/60 ,  C07D417/04 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14

Abstract: The present invention relates to thiazolinones and also to pharmaceutical compositions comprising the compounds, as well as methods of use of the compounds for treatment of disorders associated with human 11-ß-hydroxysteroid dehydrogenase type 1 enzyme and for the preparation of a medicament which acts on the human 11- ß-hydroxysteroid dehydrogenase type 1 enzyme.

Abstract translation: 本发明涉及噻唑啉酮以及包含该化合物的药物组合物，以及该化合物用于治疗与人类11-羟基类固醇脱氢酶1型酶有关的病症的用途的方法以及用于制备作用于 人类11-羟基类固醇脱氢酶1型酶。

公开(公告)号：WO2013090683A1

公开(公告)日：2013-06-20

申请号：PCT/US2012/069688

申请日：2012-12-14

Applicant: GLAXOSMITHKLINE LLC ,  HAN, Nianhe ,  JOHNS, Brian Alvin ,  TANG, Jun

Inventor： HAN, Nianhe ,  JOHNS, Brian Alvin ,  TANG, Jun

IPC: C07C69/753

CPC classification number: C07D239/30 ,  C07C69/34 ,  C07C235/78 ,  C07C2603/52 ,  C07D213/61 ,  C07J63/008

Abstract: The present invention relates to a compound characterized by Formula (I); or a pharmaceutically acceptable salt thereof, wherein X, Y, and Z are as described herein. Compounds of the present invention are useful for the treatment of HIV.

Abstract translation: 本发明涉及式（I）表示的化合物： 或其药学上可接受的盐，其中X，Y和Z如本文所述。 本发明的化合物可用于治疗HIV。

公开(公告)号：WO2013020245A1

公开(公告)日：2013-02-14

申请号：PCT/CN2011/001302

申请日：2011-08-08

Applicant: GLAXOSMITHKLINE LLC ,  GAO, Daxin ,  HAN, Nianhe ,  JOHNS, Brian ,  JIN, Zhimin ,  NING, Fangxian ,  TANG, Jun ,  WU, Yongyong ,  YANG, Heping

Inventor： GAO, Daxin ,  HAN, Nianhe ,  JOHNS, Brian ,  JIN, Zhimin ,  NING, Fangxian ,  TANG, Jun ,  WU, Yongyong ,  YANG, Heping

IPC: C07J53/00 ,  A61K31/56 ,  A61P31/18

CPC classification number: C07J63/008

Abstract: Disclosed are a compound characterized by the following formula I or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising said compound or a pharmaceutically acceptable salt thereof, wherein R3, L, and A are as described in the application. Said compounds are useful for the treatment of HIV.

Abstract translation: 公开了以下式I表示的化合物或其药学上可接受的盐，以及包含所述化合物或其药学上可接受的盐的药物组合物，其中R3，L和A如申请中所述。 所述化合物可用于治疗HIV。

公开(公告)号：WO2007084391A3

公开(公告)日：2007-07-26

申请号：PCT/US2007/000871

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 ,  C07D417/14 ,  C07D513/04 ,  C07D471/04 ,  C07D277/54 ,  C07D495/04 ,  C07D277/42 ,  A61K31/427 ,  A61P35/00

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.

公开(公告)号：WO2005116002A3

公开(公告)日：2005-12-08

申请号：PCT/US2005/018081

申请日：2005-05-24

Applicant: AMGEN INC. ,  BIOVITRUM AB ,  HENRIKSSON, Martin ,  HOMAN, Evert ,  JOHANSSON, Lars ,  VALLGARDA, Jerk ,  WILLIAMS, Meredith ,  BERCOT, Eric ,  FOTSCH, Christopher, H. ,  LI, Aiwen ,  CAI, Guolin ,  HUNGATE, Randall, W. ,  YUAN, Chester, Chenguang ,  TEGLEY, Chirstopher ,  ST. JEAN, David ,  HAN, Nianhe ,  HUANG, Qi ,  LIU, Qingyian ,  BARTBERGER, Michael, D. ,  MONIZ, George, A. ,  FRIZZLE, Matthew, J.

Inventor： HENRIKSSON, Martin ,  HOMAN, Evert ,  JOHANSSON, Lars ,  VALLGARDA, Jerk ,  WILLIAMS, Meredith ,  BERCOT, Eric ,  FOTSCH, Christopher, H. ,  LI, Aiwen ,  CAI, Guolin ,  HUNGATE, Randall, W. ,  YUAN, Chester, Chenguang ,  TEGLEY, Chirstopher ,  ST. JEAN, David ,  HAN, Nianhe ,  HUANG, Qi ,  LIU, Qingyian ,  BARTBERGER, Michael, D. ,  MONIZ, George, A. ,  FRIZZLE, Matthew, J.

IPC: C07D277/54 ,  C07D263/48 ,  A61K31/42 ,  A61K31/426 ,  A61P3/04 ,  A61P3/00 ,  A61P3/06 ,  A61P3/10 ,  A61P19/10 ,  A61P31/12 ,  A61P29/00 ,  A61P25/28 ,  A61P25/24

Abstract: The present invention relates to compounds with the formula (I), (II), (III) or (IV): (I) (II), (III), or (IV), wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , X and Z are as defined herein, and also to pharmaceutical compositions comprising the compounds, as well as methods of use of the compounds for treatment of disorders associated with human 11-β-hydroxysteroid dehydrogenase type 1 enzyme and for the preparation of a medicament which acts on the human 11-β-hydroxysteroid dehydrogenase type 1 enzyme.

公开(公告)号：WO03049702A2

公开(公告)日：2003-06-19

申请号：PCT/US0239589

申请日：2002-12-10

Applicant: AMGEN INC ,  BO YUNXIN Y ,  CHAKRABARTI PARTHA P ,  CHEN NING ,  DOHERTY ELIZABETH M ,  FOTSCH CHRISTOPHER H ,  HAN NIANHE ,  KELLY MICHAEL G ,  LIU QINGYIAN ,  NORMAN MARK HENRY ,  OGNYANOV VASSIL I ,  WANG XIANGHONG ,  ZHU JIAWANG

Inventor： BO YUNXIN Y ,  CHAKRABARTI PARTHA P ,  CHEN NING ,  DOHERTY ELIZABETH M ,  FOTSCH CHRISTOPHER H ,  HAN NIANHE ,  KELLY MICHAEL G ,  LIU QINGYIAN ,  NORMAN MARK HENRY ,  WANG XIANGHONG ,  ZHU JIAWANG ,  OGNYANOV VASSIL I

IPC: C07D249/18 ,  A61K31/17 ,  A61K31/18 ,  A61K31/343 ,  A61K31/357 ,  A61K31/36 ,  A61K31/37 ,  A61K31/381 ,  A61K31/4025 ,  A61K31/404 ,  A61K31/41 ,  A61K31/415 ,  A61K31/4184 ,  A61K31/4192 ,  A61K31/423 ,  A61K31/428 ,  A61K31/44 ,  A61K31/4402 ,  A61K31/4406 ,  A61K31/443 ,  A61K31/444 ,  A61K31/453 ,  A61K31/47 ,  A61K31/4704 ,  A61K31/4709 ,  A61K31/472 ,  A61K31/496 ,  A61K31/4965 ,  A61K31/498 ,  A61K31/505 ,  A61K31/517 ,  A61K31/5375 ,  A61K31/538 ,  A61P1/00 ,  A61P1/04 ,  A61P1/12 ,  A61P3/10 ,  A61P9/00 ,  A61P11/00 ,  A61P11/02 ,  A61P11/06 ,  A61P13/00 ,  A61P13/10 ,  A61P17/00 ,  A61P17/02 ,  A61P17/04 ,  A61P17/06 ,  A61P17/14 ,  A61P19/02 ,  A61P25/00 ,  A61P25/06 ,  A61P27/02 ,  A61P29/00 ,  A61P31/12 ,  A61P37/08 ,  A61P43/00 ,  C07C233/11 ,  C07C233/15 ,  C07C233/33 ,  C07C233/44 ,  C07C311/13 ,  C07C311/16 ,  C07C317/40 ,  C07C323/35 ,  C07D209/08 ,  C07D209/12 ,  C07D209/42 ,  C07D209/48 ,  C07D213/26 ,  C07D213/64 ,  C07D213/643 ,  C07D213/74 ,  C07D213/75 ,  C07D215/22 ,  C07D215/227 ,  C07D215/32 ,  C07D215/38 ,  C07D215/40 ,  C07D215/42 ,  C07D217/04 ,  C07D231/40 ,  C07D231/56 ,  C07D233/38 ,  C07D235/08 ,  C07D235/26 ,  C07D237/20 ,  C07D239/42 ,  C07D239/88 ,  C07D239/90 ,  C07D241/20 ,  C07D241/42 ,  C07D263/56 ,  C07D265/36 ,  C07D277/62 ,  C07D277/82 ,  C07D307/79 ,  C07D311/16 ,  C07D319/18 ,  C07D319/20 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D407/12 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  A61K

CPC classification number: C07D471/04 ,  C07D209/08 ,  C07D209/12 ,  C07D209/42 ,  C07D209/48 ,  C07D213/26 ,  C07D213/643 ,  C07D213/74 ,  C07D213/75 ,  C07D215/227 ,  C07D215/38 ,  C07D217/04 ,  C07D231/40 ,  C07D231/56 ,  C07D233/38 ,  C07D237/20 ,  C07D239/42 ,  C07D239/90 ,  C07D241/42 ,  C07D263/56 ,  C07D265/36 ,  C07D277/62 ,  C07D277/82 ,  C07D307/79 ,  C07D319/20 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D407/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14

Abstract: Compounds having the general structure (formule 1) and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed−vascular and non−vascular syndromes, tension headache, , general inflammation arthritis, rheumatic diseases, osteorthritis, inflammatory bowel disorders, inflammatory eye disorders,inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neuropathy pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentiation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritis, vitiligo, general gastrointestinal disorders, gastric ulceration, duodenal ulcers, diarrhea, gastric lesions induced by necrotising agents, hair growth, vasomotor or allergic rhinitis, bronchial disorders or bladder disorders.

Abstract translation: 具有一般结构的化合物（配方1）和含有它们的组合物，用于治疗急性，炎性和神经性疼痛，牙痛，一般头痛，偏头痛，丛集性头痛，混合血管和非血管性综合征，紧张性头痛，一般 炎症性关节炎，风湿性疾病，骨关节炎，炎症性肠病，炎症性眼病，炎症性或不稳定性膀胱病，牛皮癣，皮肤炎症成分炎症，慢性炎性病症，炎性疼痛及相关的痛觉过敏和异常性疼痛，神经病痛及相关的痛觉过敏和异常性疼痛， 糖尿病性神经病疼痛，灼痛，交感神经保持疼痛，交感综合征，哮喘，上皮组织损伤或功能障碍，单纯疱疹，呼吸道内脏运动紊乱，泌尿生殖道，胃肠或血管区域，伤口，烧伤，过敏性皮肤反应，瘙痒症，白癜风， 一般胃肠素 胃溃疡，十二指肠溃疡，腹泻，坏死因子诱导的胃损伤，毛发生长，血管舒缩或过敏性鼻炎，支气管疾病或膀胱疾病。

公开(公告)号：WO2013091144A1

公开(公告)日：2013-06-27

申请号：PCT/CN2011/002159

申请日：2011-12-21

Applicant: GLAXOSMITHKLINE LLC ,  HAN, Nianhe ,  JOHNS, Brian, A. ,  TANG, Jun

Inventor： HAN, Nianhe ,  JOHNS, Brian, A. ,  TANG, Jun

IPC: C07J63/00 ,  C07J53/00 ,  A61K31/575 ,  A61K31/58 ,  A61K45/00 ,  A61P31/18

CPC classification number: C07J63/008

Abstract: The present invention relates to a compound characterized by the following Formula I or a pharmaceutically acceptable salt thereof, wherein X, Y, and Z are as described herein. Compounds of the present invention are useful for the treatment of HIV.

Abstract translation: 本发明涉及以下式I表征的化合物或其药学上可接受的盐，其中X，Y和Z如本文所述。 本发明的化合物可用于治疗HIV。

公开(公告)号：WO2011100308A1

公开(公告)日：2011-08-18

申请号：PCT/US2011/024174

申请日：2011-02-09

Applicant: GLAXOSMITHKLINE LLC ,  GAO, Daxin ,  HAN, Nianhe ,  JIN, Zhimin ,  NING, Fangxian ,  TANG, Jun ,  WU, Yongyong ,  YANG, Heping

Inventor： GAO, Daxin ,  HAN, Nianhe ,  JIN, Zhimin ,  NING, Fangxian ,  TANG, Jun ,  WU, Yongyong ,  YANG, Heping

IPC: A01N45/00 ,  A61K31/50 ,  A61K31/56

CPC classification number: A61K31/50 ,  A61K31/56 ,  C07C225/14 ,  C07C233/76 ,  C07C235/78 ,  C07C275/30 ,  C07C311/04 ,  C07C2601/02 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2603/52 ,  C07D205/04 ,  C07D213/40 ,  C07D231/12 ,  C07D295/185 ,  C07D295/26 ,  C07D333/20

Abstract: The present invention relates to a compound characterized by Formula I or a pharmaceutically acceptable salt thereof, wherein R 1 , R 2 , R 3 , X, and Y are as described herein. Compounds of the present invention are useful for the treatment of HIV-1.

Abstract translation: 本发明涉及式I化合物或其药学上可接受的盐，其中R1，R2，R3，X和Y如本文所述。 本发明的化合物可用于治疗HIV-1。