公开(公告)号：WO2002066470A1

公开(公告)日：2002-08-29

申请号：PCT/US2002/000743

申请日：2002-01-11

Applicant: AMGEN INC.

Inventor： CHEN, Guoqing ,  ADAMS, Jeffrey ,  BEMIS, Jean ,  BOOKER, Shon ,  CAI, Guolin ,  CROGHAN, Michael ,  DIPIETRO, Lucian ,  DOMINGUEZ, Celia ,  ELBAUM, Daniel ,  GERMAIN, Julie ,  GEUNS-MEYER, Stephanie ,  HANDLEY, Michael ,  HUANG, Qi ,  KIM, Joseph, L. ,  KIM, Tae-Seong ,  KISELYOV, Alexander ,  OUYANG, Xiaohu ,  PATEL, Vinod, F. ,  SMITH, Leon, M. ,  STEC, Markian ,  TASKER, Andrew ,  XI, Ning ,  XU, Shimin ,  YUAN, Chester, Chenguang

IPC: C07D409/12

CPC classification number: C07D213/82 ,  A61K31/443 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/538 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/00 ,  C07D409/04 ,  C07D409/12 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04

Abstract: Selected heterocyclic compounds are effective for prophylaxis and treatment of diseases, such as angiogenesis 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, cancer 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: 所选择的杂环化合物对于预防和治疗诸如血管生成介导的疾病等疾病是有效的。 本发明包括新型化合物，类似物，前药及其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癌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：WO2007061661A4

公开(公告)日：2007-05-31

申请号：PCT/US2006/043951

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 ,  C07D277/60 ,  C07D417/04 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14 ,  A61K31/426 ,  A61K31/427 ,  A61K31/428 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  A61P19/10 ,  A61P25/24 ,  A61P9/12

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-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：WO2006019975A1

公开(公告)日：2006-02-23

申请号：PCT/US2005/025090

申请日：2005-07-15

Applicant: AMGEN INC.

Inventor： ASKEW, JR., Benny C. ,  AYA, Toshihiro ,  BISWAS, Kaustav ,  CAI, Guolin ,  CHEN, Jian Jeffrey ,  HAN, Nianhe ,  LIU, Qingyian ,  NGUYEN, Thomas ,  NISHIMURA, Nobuko ,  NOMAK, Rana ,  PETERKIN, Tanya ,  QIAN, Wenyuan ,  YANG, Kevin ,  YUAN, Chester Chenguang ,  ZHU, Jiawang ,  D'AMICO, Derin C. ,  HUMAN, Jason Brooks ,  HUANG, QI

IPC: C07D241/08

CPC classification number: C07D221/10 ,  C07D221/08 ,  C07D239/74 ,  C07D241/08 ,  C07D243/08 ,  C07D249/08 ,  C07D295/135 ,  C07D311/96 ,  C07D335/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D417/12 ,  C07D491/04

Abstract: Selected compounds are effective for treatment of pain and diseases, such as inflammation mediated diseases. The invention encompasses novel compounds of formula (I) 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。 本发明包括式（I）的新型化合物及其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，炎症等的疾病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：WO2003044021A3

公开(公告)日：2003-05-30

申请号：PCT/US2002/036699

申请日：2002-11-16

Applicant: AMGEN INC. ,  CAI, Guolin ,  CHAU, Jennifer, N. ,  DOMINGUEZ, Celia ,  RISHTON, Gilbert, M. ,  LU, Yuelie

Inventor： CAI, Guolin ,  CHAU, Jennifer, N. ,  DOMINGUEZ, Celia ,  RISHTON, Gilbert, M. ,  LU, Yuelie

IPC: C07D487/04

Abstract: Selected novel substituted indolizine-like compounds are effective for treatment of diseases, such as TNF-α, IL-1β, IL-6 and/or IL-8 mediated diseases, and other maladies, such as cancer, pain and diabetes. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for treatment of diseases and other maladies or conditions involving inflammation, cancer, pain, diabetes and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

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：WO2006044355A1

公开(公告)日：2006-04-27

申请号：PCT/US2005/036489

申请日：2005-10-11

Applicant: AMGEN INC. ,  AYA, Toshihiro ,  CAI, Guolin ,  CHEN, Jian, J. ,  D'AMICO, Derin, C. ,  NGUYEN, Thomas ,  QIAN, Wenyuan

Inventor： AYA, Toshihiro ,  CAI, Guolin ,  CHEN, Jian, J. ,  D'AMICO, Derin, C. ,  NGUYEN, Thomas ,  QIAN, Wenyuan

IPC: C07D403/06 ,  A61K31/497 ,  A61K31/4192 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D471/04

CPC classification number: C07D401/14 ,  C07D403/06 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D471/04

Abstract: Compounds of Formula (I): 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: 式（I）的化合物：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：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：WO2003044021A2

公开(公告)日：2003-05-30

申请号：PCT/US2002/036699

申请日：2002-11-16

Applicant: AMGEN INC. ,  CAI, Guolin ,  CHAU, Jennifer, N. ,  DOMINGUEZ, Celia ,  RISHTON, Gilbert, M. ,  LU, Yuelie

Inventor： CAI, Guolin ,  CHAU, Jennifer, N. ,  DOMINGUEZ, Celia ,  RISHTON, Gilbert, M. ,  LU, Yuelie

IPC: C07D487/04

CPC classification number: C07D401/04 ,  C07D471/04 ,  C07D487/04

Abstract: Selected novel substituted indolizine-like compounds are effective for treatment of diseases, such as TNF-α, IL-1β, IL-6 and/or IL-8 mediated diseases, and other maladies, such as cancer, pain and diabetes. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for treatment of diseases and other maladies or conditions involving inflammation, cancer, pain, diabetes 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: 所选择的新型取代的中氮茚样化合物对于治疗疾病如TNF-α，IL-1β，IL-6和/或IL-8介导的疾病以及其他疾病，例如 癌症，疼痛和糖尿病。 本发明包括新化合物，类似物，前药和药学上可接受的盐，用于治疗涉及炎症，癌症，疼痛，糖尿病等的疾病和其它疾病或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用于这些方法的中间体。