公开(公告)号：WO2008057282A1

公开(公告)日：2008-05-15

申请号：PCT/US2007/022714

申请日：2007-10-25

Applicant: AMGEN INC. ,  HARRINGTON, Paul, E. ,  FOTSCH, Christopher, H. ,  TASKER, Andrew

Inventor： FOTSCH, Christopher, H. ,  TASKER, Andrew

IPC: A61P1/12 ,  A61P3/14 ,  A61P5/20 ,  C07D207/06 ,  C07D207/09 ,  C07D207/48 ,  C07D211/22 ,  C07D211/62 ,  C07D213/30 ,  C07D213/38 ,  C07D213/81 ,  C07D213/82 ,  C07D231/14 ,  C07D233/60 ,  C07D235/06 ,  C07D237/14

CPC classification number: C07D261/18 ,  C07C211/29 ,  C07C217/58 ,  C07C233/43 ,  C07C233/44 ,  C07C233/80 ,  C07C271/28 ,  C07C311/37 ,  C07C317/32 ,  C07C323/32 ,  C07C2601/08 ,  C07C2601/16 ,  C07D207/06 ,  C07D207/09 ,  C07D207/48 ,  C07D211/22 ,  C07D211/62 ,  C07D213/30 ,  C07D213/38 ,  C07D213/81 ,  C07D213/82 ,  C07D231/14 ,  C07D233/60 ,  C07D235/06 ,  C07D237/14 ,  C07D239/42 ,  C07D249/08 ,  C07D261/08 ,  C07D263/24 ,  C07D263/34 ,  C07D271/06 ,  C07D285/06 ,  C07D295/088 ,  C07D295/185 ,  C07D295/205 ,  C07D295/26 ,  C07D307/68 ,  C07D317/58 ,  C07D333/38 ,  C07D333/40 ,  C07D409/04 ,  C07D413/12 ,  C07D417/04

Abstract: The present invention relates generally to compounds represented in Formula I, pharmaceutical compositions comprising them and methods of treating of diseases or disorders related to the function of the calcium sensing receptor. The invention also relates to processes for making such compounds and to intermediates useful in these processes.

Abstract translation: 本发明一般涉及式I表示的化合物，包含它们的药物组合物以及治疗与钙敏感受体功能有关的疾病或病症的方法。 本发明还涉及制备这些化合物和在这些方法中有用的中间体的方法。

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：WO2008011453A2

公开(公告)日：2008-01-24

申请号：PCT/US2007/073767

申请日：2007-07-18

Applicant: AMGEN INC. ,  BIOVITRUM AB ,  FOTSCH, Christopher, H. ,  BARTBERGER, Michael, D. ,  HARALDSSON, Martin ,  ST. JEAN, David ,  JOHANSSON, Lars ,  NILSSON, Marianne ,  SUTIN, Lori

Inventor： FOTSCH, Christopher, H. ,  BARTBERGER, Michael, D. ,  HARALDSSON, Martin ,  ST. JEAN, David ,  JOHANSSON, Lars ,  NILSSON, Marianne ,  SUTIN, Lori

CPC classification number: C07D403/06 ,  C07D413/06 ,  C07D413/12

Abstract: Compounds of formula I and IV are described and have therapeutic utility, particularly in the treatment of diabetes, obesity and related conditions and disorders:formula I and IV wherein the variables A-B, R, 1, r R> 2, m, and Q are described herein.

Abstract translation: 描述了式I和IV的化合物，具有治疗效用，特别是治疗糖尿病，肥胖症和相关病症和病症：式I和IV，其中变量AB，R，1，r R> 2，m和Q为 在此描述。

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：WO2004092116A1

公开(公告)日：2004-10-28

申请号：PCT/US2004/011105

申请日：2004-04-12

Applicant: AMGEN, INC. ,  ARRAY BIOPHARMA, INC. ,  GRONEBERG, Robert, D. ,  ASKEW, Ben ,  D'AMICO, Derin ,  ZHAN, James ,  TORO, Andras ,  SUZUKI, Hideo ,  MARESKA, David, A. ,  HAN, Nianh ,  FOTSCH, Christopher, H. ,  LIU, Qinglan ,  RIAHI, Babak ,  YANG, Kevin ,  LI, Aiwan ,  YUAN, Chester ,  BISWAS, Kaustav ,  HARRIED, Scott ,  NGUYEN, Tom ,  QIAN, Wenyuan ,  CHEN, Jian, J. ,  NOMAK, Rana

Inventor： GRONEBERG, Robert, D. ,  ASKEW, Ben ,  D'AMICO, Derin ,  ZHAN, James ,  TORO, Andras ,  SUZUKI, Hideo ,  MARESKA, David, A. ,  HAN, Nianh ,  FOTSCH, Christopher, H. ,  LIU, Qinglan ,  RIAHI, Babak ,  YANG, Kevin ,  LI, Aiwan ,  YUAN, Chester ,  BISWAS, Kaustav ,  HARRIED, Scott ,  NGUYEN, Tom ,  QIAN, Wenyuan ,  CHEN, Jian, J. ,  NOMAK, Rana

IPC: C07C311/18

CPC classification number: C07C311/19 ,  C07C311/13 ,  C07C311/29 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2602/08 ,  C07C2602/10 ,  C07D205/04 ,  C07D207/12 ,  C07D207/16 ,  C07D207/20 ,  C07D209/14 ,  C07D209/16 ,  C07D209/40 ,  C07D209/52 ,  C07D211/38 ,  C07D211/44 ,  C07D211/46 ,  C07D211/60 ,  C07D211/70 ,  C07D213/42 ,  C07D213/56 ,  C07D213/64 ,  C07D215/38 ,  C07D215/40 ,  C07D215/42 ,  C07D217/22 ,  C07D233/54 ,  C07D239/74 ,  C07D271/08 ,  C07D277/64 ,  C07D279/02 ,  C07D285/14 ,  C07D295/125 ,  C07D295/13 ,  C07D295/135 ,  C07D307/14 ,  C07D307/28 ,  C07D307/79 ,  C07D307/81 ,  C07D311/68 ,  C07D317/58 ,  C07D333/20 ,  C07D333/24 ,  C07D333/58 ,  C07D333/62 ,  C07D405/04 ,  C07D405/06 ,  C07D405/12 ,  C07D407/06 ,  C07D407/12 ,  C07D409/06 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D487/08

Abstract: Selected compounds are effective for treatment of pain and diseases, such as inflammation mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving pain, inflammation, and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

Abstract translation: 所选化合物对于治疗疼痛和疾病如炎症介导的疾病是有效的。 本发明包括新的化合物，类似物，前药和药学上可接受的衍生物，用于预防和治疗疾病和其它疾病或涉及疼痛，炎症等的病症的药物组合物和方法。 本发明还涉及制备这些化合物的方法以及在这些方法中有用的中间体。

公开(公告)号：WO2004035549A1

公开(公告)日：2004-04-29

申请号：PCT/US2003/032823

申请日：2003-10-16

Applicant: AMGEN INC. ,  BALAN, Chenera ,  BO, Yunxin ,  DOMINGUEZ, Celia ,  FOTSCH, Christopher, H. ,  GORE, Vijay, K. ,  MA, Vu Van ,  NORMAN, Mark, H. ,  OGNYANOV, Vassil, I. ,  QIAN, Yi-xin ,  WANG, Xianghong ,  XI, Ning ,  XU, Shimin

Inventor： BALAN, Chenera ,  BO, Yunxin ,  DOMINGUEZ, Celia ,  FOTSCH, Christopher, H. ,  GORE, Vijay, K. ,  MA, Vu Van ,  NORMAN, Mark, H. ,  OGNYANOV, Vassil, I. ,  QIAN, Yi-xin ,  WANG, Xianghong ,  XI, Ning ,  XU, Shimin

IPC: C07D235/30

CPC classification number: C07D401/04 ,  C07D235/30 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04

Abstract: Compounds of formula (I) are useful in the treatment of vanilloid-receptor-meditated diseases, such as inflammatory or neuropathic pain and diseases involving sensory nerve function such as asthma, rheumatoid arthritis, osteoarthritis, inflammatory bowel disorders, urinary incontinence, migraine and psoriasis.

Abstract translation: 式（I）化合物可用于治疗香草素受体冥想疾病，例如炎性或神经性疼痛以及涉及感觉神经功能的疾病如哮喘，类风湿性关节炎，骨关节炎，炎性肠病，尿失禁，偏头痛和牛皮癣 。

公开(公告)号：WO2009051718A3

公开(公告)日：2009-06-11

申请号：PCT/US2008011755

申请日：2008-10-15

Applicant: AMGEN INC ,  COULTER THOMAS S ,  FOTSCH CHRISTOPHER H ,  GHIRON CHIARA ,  HARRINGTON PAUL E ,  KELLY MICHAEL G ,  MILLER PHILIP ,  RISHTON GILBERT M ,  ST JEAN DAVID J JR ,  SEMIN DAVID J

Inventor： COULTER THOMAS S ,  FOTSCH CHRISTOPHER H ,  GHIRON CHIARA ,  HARRINGTON PAUL E ,  KELLY MICHAEL G ,  MILLER PHILIP ,  RISHTON GILBERT M ,  ST JEAN DAVID J JR ,  SEMIN DAVID J

IPC: C07D207/48 ,  A61K31/40 ,  A61K31/415 ,  A61K31/4164 ,  A61P7/00 ,  C07D207/335 ,  C07D231/12 ,  C07D231/16 ,  C07D231/22 ,  C07D233/64 ,  C07D261/08 ,  C07D271/06 ,  C07D277/28 ,  C07D401/04

CPC classification number: C07D233/64 ,  C07D207/335 ,  C07D207/48 ,  C07D231/12 ,  C07D231/16 ,  C07D231/22 ,  C07D261/08 ,  C07D271/06 ,  C07D277/28 ,  C07D401/04

Abstract: The present invention relates generally to novel calcimimetic compounds and pharmaceutical compositions comprising them. The invention also relates to methods of treating of diseases or disorders related to the function of the calcium sensing receptor using the compounds represented in Formula I.

Abstract translation: 本发明一般涉及新型拟钙剂化合物和包含它们的药物组合物。 本发明还涉及使用式I代表的化合物治疗与钙敏感受体功能有关的疾病或病症的方法。

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.