公开(公告)号：WO2012177893A2

公开(公告)日：2012-12-27

申请号：PCT/US2012/043566

申请日：2012-06-21

Applicant: AMGEN INC. ,  BISWAS, Kaustav ,  BROWN, James ,  CHEN, Jian, J. ,  GORE, Vijay, Keshav ,  HARRIED, Scott ,  HORNE, Daniel, B. ,  KALLER, Matthew, R. ,  LIU, Qingyian ,  MA, Vu, Van ,  MONENSCHEIN, Holger ,  NGUYEN, Thomas, T. ,  YUAN, Chester, Chenguang ,  ZHONG, Wenge ,  ST. JEAN, David, J., Jr.

Inventor： BISWAS, Kaustav ,  BROWN, James ,  CHEN, Jian, J. ,  GORE, Vijay, Keshav ,  HARRIED, Scott ,  HORNE, Daniel, B. ,  KALLER, Matthew, R. ,  LIU, Qingyian ,  MA, Vu, Van ,  MONENSCHEIN, Holger ,  NGUYEN, Thomas, T. ,  YUAN, Chester, Chenguang ,  ZHONG, Wenge ,  ST. JEAN, David, J., Jr.

IPC: C07D213/40

CPC classification number: C07D213/82 ,  C07D213/40 ,  C07D213/61 ,  C07D213/81 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04

Abstract: Compounds of Formula (I) are useful as antagonists of TRPM8. Such compounds are useful in treating a number of TRPM8 mediated disorders and conditions and may be used to prepare medicaments and pharmaceutical compositions useful for treating such disorders and conditions. Examples of such disorders include, but are not limited to, migraines and neuropathic pain. Compounds of Formula (I) have a structure where the definitions of the variables are provided herein.

Abstract translation: 式（I）的化合物可用作TRPM8的拮抗剂。 这些化合物可用于治疗多种TRPM8介导的病症和病症，并且可用于制备用于治疗这种病症和病症的药物和药物组合物。 这些疾病的实例包括但不限于偏头痛和神经性疼痛。 式（I）的化合物具有这里提供变量的定义的结构。

公开(公告)号：WO2012138776A1

公开(公告)日：2012-10-11

申请号：PCT/US2012/032192

申请日：2012-04-04

Applicant: AMGEN INC. ,  BARTBERGER, Michael, D. ,  CROGHAN, Michael, D. ,  FOTSCH, Christopher, H. ,  NORMAN, Mark, H. ,  PENNINGTON, Lewis, D. ,  REICHELT, Andreas ,  ST. JEAN, David, J., Jr. ,  TEGLEY, Christopher, M.

Inventor： BARTBERGER, Michael, D. ,  CROGHAN, Michael, D. ,  FOTSCH, Christopher, H. ,  NORMAN, Mark, H. ,  PENNINGTON, Lewis, D. ,  REICHELT, Andreas ,  ST. JEAN, David, J., Jr. ,  TEGLEY, Christopher, M.

IPC: C07D321/10 ,  C07D333/58 ,  C07D407/12 ,  C07D407/14 ,  C07D409/04 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D495/04 ,  C07D513/04 ,  A61K31/357 ,  A61K31/381 ,  A61K31/422

CPC classification number: A61K31/506 ,  A61K31/155 ,  A61K31/357 ,  A61K31/381 ,  A61K31/422 ,  A61K31/427 ,  A61K31/429 ,  A61K31/4365 ,  A61K31/443 ,  A61K31/4436 ,  A61K31/4709 ,  A61K45/06 ,  C07D321/10 ,  C07D333/58 ,  C07D405/14 ,  C07D407/12 ,  C07D407/14 ,  C07D409/04 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D495/04 ,  C07D513/04 ,  A61K2300/00

Abstract: The present invention relates to compounds of formula I or II, or pharmaceutically acceptable salts thereof, that interact with glucokinase regulatory protein. In addition, the present invention relates to methods of treating type 2 diabetes, and other diseases and/or conditions where glucokinase regulatory protein is involved using the compounds, or pharmaceutically acceptable salts thereof, and pharmaceutical compositions that contain the compounds, or pharmaceutically acceptable salts thereof.

Abstract translation: 本发明涉及与葡萄糖激酶调节蛋白相互作用的式I或II化合物或其药学上可接受的盐。 此外，本发明还涉及治疗2型糖尿病的方法，以及使用该化合物或其药学上可接受的盐涉及葡萄糖激酶调节蛋白的其它疾病和/或病症，以及含有该化合物或其药学上可接受的盐的药物组合物 它们。

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：EP2723717A2

公开(公告)日：2014-04-30

申请号：EP12730134.9

申请日：2012-06-21

Applicant: Amgen Inc.

Inventor： BISWAS, Kaustav ,  BROWN, James ,  CHEN, Jian, J. ,  GORE, Vijay, Keshav ,  HARRIED, Scott ,  HORNE, Daniel, B. ,  KALLER, Matthew, R. ,  LIU, Qingyian ,  MA, Vu, Van ,  MONENSCHEIN, Holger ,  NGUYEN, Thomas, T. ,  YUAN, Chester, Chenguang ,  ZHONG, Wenge ,  ST. JEAN, David, J., Jr.

IPC: C07D213/40 ,  C07D213/61 ,  C07D213/81 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04 ,  A61K31/45 ,  A61P29/00

CPC classification number: C07D213/82 ,  C07D213/40 ,  C07D213/61 ,  C07D213/81 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04

Abstract: Compounds of Formula (I) are useful as antagonists of TRPM8. Such compounds are useful in treating a number of TRPM8 mediated disorders and conditions and may be used to prepare medicaments and pharmaceutical compositions useful for treating such disorders and conditions. Examples of such disorders include, but are not limited to, migraines and neuropathic pain. Compounds of Formula (I) have a structure where the definitions of the variables are provided herein.

公开(公告)号：EP2694491A1

公开(公告)日：2014-02-12

申请号：EP12713839.4

申请日：2012-04-04

Applicant: Amgen Inc.

Inventor： BARTBERGER, Michael, D. ,  CROGHAN, Michael, D. ,  FOTSCH, Christopher, H. ,  NORMAN, Mark, H. ,  PENNINGTON, Lewis, D. ,  REICHELT, Andreas ,  ST. JEAN, David, J., Jr. ,  TEGLEY, Christopher, M.

IPC: C07D321/10 ,  C07D333/58 ,  C07D407/12 ,  C07D407/14 ,  C07D409/04 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D495/04 ,  C07D513/04 ,  A61K31/357 ,  A61K31/381 ,  A61K31/422

CPC classification number: A61K31/506 ,  A61K31/155 ,  A61K31/357 ,  A61K31/381 ,  A61K31/422 ,  A61K31/427 ,  A61K31/429 ,  A61K31/4365 ,  A61K31/443 ,  A61K31/4436 ,  A61K31/4709 ,  A61K45/06 ,  C07D321/10 ,  C07D333/58 ,  C07D405/14 ,  C07D407/12 ,  C07D407/14 ,  C07D409/04 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D495/04 ,  C07D513/04 ,  A61K2300/00

Abstract: The present invention relates to compounds of formula I or II, or pharmaceutically acceptable salts thereof, that interact with glucokinase regulatory protein. In addition, the present invention relates to methods of treating type 2 diabetes, and other diseases and/or conditions where glucokinase regulatory protein is involved using the compounds, or pharmaceutically acceptable salts thereof, and pharmaceutical compositions that contain the compounds, or pharmaceutically acceptable salts thereof.

公开(公告)号：EP1951696A2

公开(公告)日：2008-08-06

申请号：EP06844335.7

申请日：2006-11-13

Applicant: Amgen Inc. ,  BIOVITRUM AB

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

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-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.