公开(公告)号：WO2008137060A1

公开(公告)日：2008-11-13

申请号：PCT/US2008/005664

申请日：2008-04-29

Applicant: AMGEN INC. ,  ALLEN, Jennifer R. ,  BURLI, Roland ,  FROHN, Michael J. ,  HUNGATE, Randall W. ,  NEIRA, Susana C. ,  REED, Anthony B.

Inventor： ALLEN, Jennifer R. ,  BURLI, Roland ,  FROHN, Michael J. ,  HUNGATE, Randall W. ,  NEIRA, Susana C. ,  REED, Anthony B.

IPC: A61K31/4365 ,  A61K31/437 ,  A61P7/06 ,  A61P9/10 ,  A61P9/12 ,  A61P3/10 ,  A61P17/02 ,  A61P29/00 ,  A61P35/00 ,  A61P43/00 ,  C07D495/04 ,  C07D513/04

CPC classification number: A61K31/4365 ,  A61K31/437 ,  C07D495/04 ,  C07D513/04

Abstract: Compounds of Formula I are useful inhibitors of HIF prolyl hydroxylases. Compounds of Formula I have the following structure:(I) where the definitions of the variables are provided herein.

Abstract translation: 式I化合物是HIF脯氨酰羟化酶的有用抑制剂。 式I化合物具有以下结构：（I）其中本文提供变量的定义。

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：WO2004052286A3

公开(公告)日：2004-08-12

申请号：PCT/US0338716

申请日：2003-12-05

Applicant: MERCK & CO INC ,  FRALEY MARK E ,  HAMBAUGH SCOTT R ,  RUBINO ROBERT S ,  HUNGATE RANDALL W

Inventor： FRALEY MARK E ,  HAMBAUGH SCOTT R ,  RUBINO ROBERT S ,  HUNGATE RANDALL W

IPC: A61K45/06 ,  A61P3/08 ,  A61P19/00 ,  A61P35/00 ,  C07D487/04 ,  A61K31/519 ,  A61K31/535 ,  C07D413/14

CPC classification number: C07D487/04 ,  A61K45/06

Abstract: The present invention relates to compounds which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angiogenesis, cancer, tumor growth, atherosclerosis, age related macular degeneration, diabetic retinopathy, macular edema, retinal ischemia, inflammatory diseases, and the like in mammals.

Abstract translation: 本发明涉及抑制，调节和/或调节酪氨酸激酶信号转导的化合物，含有这些化合物的组合物，以及使用它们治疗酪氨酸激酶依赖性疾病和病症如血管生成，癌症，肿瘤生长，动脉粥样硬化 ，年龄相关性黄斑变性，糖尿病性视网膜病，黄斑水肿，视网膜缺血，炎性疾病等。

公开(公告)号：WO0129025A3

公开(公告)日：2001-11-01

申请号：PCT/US0028625

申请日：2000-10-16

Applicant: MERCK & CO INC ,  ARRINGTON KENNETH L ,  BILODEAU MARK T ,  FRALEY MARK E ,  HARTMAN GEORGE D ,  HOFFMAN WILLIAM F ,  HUNGATE RANDALL W ,  KIM YUNTAE

Inventor： ARRINGTON KENNETH L ,  BILODEAU MARK T ,  FRALEY MARK E ,  HARTMAN GEORGE D ,  HOFFMAN WILLIAM F ,  HUNGATE RANDALL W ,  KIM YUNTAE

IPC: C07D401/04 ,  A61K31/4709 ,  A61K31/495 ,  A61K31/496 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/551 ,  A61K45/00 ,  A61K45/06 ,  A61N5/10 ,  A61P9/10 ,  A61P17/02 ,  A61P17/06 ,  A61P19/02 ,  A61P19/08 ,  A61P27/02 ,  A61P29/00 ,  A61P35/00 ,  A61P43/00 ,  C07D401/00 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14

CPC classification number: C07D413/14 ,  A61K31/495 ,  A61K45/06 ,  C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D417/14 ,  A61K2300/00

Abstract: The present invention relates to compounds which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angiogenesis, cancer, tumor growth, atherosclerosis, age related macular degeneration, diabetic retinopathy, inflammatory diseases, and the like in mammals.

公开(公告)号：WO1997040833A1

公开(公告)日：1997-11-06

申请号：PCT/US1997007131

申请日：1997-04-29

Applicant: MERCK & CO., INC. ,  COBURN, Craig, A. ,  FRALEY, Mark, E. ,  HOLLOWAY, M., Katharine ,  HUNGATE, Randall, W. ,  PRENDERGAST, Kristine

Inventor： MERCK & CO., INC.

IPC: A61K31/445

CPC classification number: C07D221/22 ,  C07D405/10 ,  C07D417/06

Abstract: Compounds such as formula (A) or pharmaceutically acceptable salts thereof are HIV protease inhibitors. These compounds are useful in the prevention or treatment of infection by HIV and in the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.

Abstract translation: 式（A）或其药学上可接受的盐的化合物是HIV蛋白酶抑制剂。 这些化合物可用于预防或治疗HIV的感染和治疗AIDS，无论是作为化合物，药学上可接受的盐，药物组合物成分，无论是否与其他抗病毒剂，免疫调节剂，抗生素或疫苗结合使用。 还描述了治疗艾滋病的方法和预防或治疗HIV感染的方法。

公开(公告)号：WO2007061661A3

公开(公告)日：2008-12-11

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 ,  A61K31/428 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  A61P9/12 ,  A61P19/10 ,  A61P25/24 ,  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：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：WO2005116002B1

公开(公告)日：2006-08-24

申请号：PCT/US2005018081

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 ,  A61K31/42 ,  A61K31/426 ,  A61P3/00 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  A61P19/10 ,  A61P25/24 ,  A61P25/28 ,  A61P29/00 ,  A61P31/12 ,  C07D20060101 ,  C07D263/48 ,  C07D277/42 ,  C07D277/60 ,  C07D413/14 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14 ,  C07D513/10 ,  C07F7/18

CPC classification number: C07D417/06 ,  C07D263/34 ,  C07D263/48 ,  C07D275/03 ,  C07D277/42 ,  C07D277/54 ,  C07D277/60 ,  C07D413/14 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07D513/10 ,  C07F7/1856

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-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: （I），（II），（III）或（IV）的化合物：其中R 1， R 2，R 3，R 4，R 5，R 6，R 6，R 5，R 8，R 8，R 8， R 7，X和Z如本文所定义，并且还涉及包含所述化合物的药物组合物，以及所述化合物用于治疗与人11-β-羟基类固醇相关的病症的方法 脱氢酶1型酶和用于制备作用于人类11-β-羟基类固醇脱氢酶1型酶的药物的用途。

公开(公告)号：WO0128993A3

公开(公告)日：2001-09-13

申请号：PCT/US0028641

申请日：2000-10-16

Applicant: MERCK & CO INC ,  FRALEY MARK E ,  HAMBAUGH SCOTT R ,  HUNGATE RANDALL W

Inventor： FRALEY MARK E ,  HAMBAUGH SCOTT R ,  HUNGATE RANDALL W

IPC: A61K31/337 ,  A61K31/437 ,  A61K31/4375 ,  A61K31/4465 ,  A61K31/4704 ,  A61K31/497 ,  A61K39/395 ,  A61K45/00 ,  A61P9/00 ,  A61P9/10 ,  A61P17/00 ,  A61P17/06 ,  A61P27/00 ,  A61P29/00 ,  A61P35/00 ,  A61P43/00 ,  C07D401/04 ,  C07D401/14 ,  C07D471/04 ,  C07D495/04 ,  A61K31/496 ,  A61K31/4355 ,  A61K31/4365 ,  A61K31/551 ,  C07D403/04 ,  C07D487/04 ,  C07D491/048 ,  C07D507/00

CPC classification number: C07D401/04 ,  C07D401/14

Abstract: The present invention relates to compounds which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angiogenesis, cancer, tumor growth, atherosclerosis, age related macular degeneration, diabetic retinopathy, inflammatory diseases, and the like in mammals.

Abstract translation: 本发明涉及抑制，调节和/或调节酪氨酸激酶信号转导的化合物，含有这些化合物的组合物，以及使用它们治疗酪氨酸激酶依赖性疾病和病症如血管生成，癌症，肿瘤生长，动脉粥样硬化 ，年龄相关性黄斑变性，糖尿病性视网膜病，炎性疾病等。

公开(公告)号：WO2007070359A2

公开(公告)日：2007-06-21

申请号：PCT/US2006/046785

申请日：2006-12-08

Applicant: AMGEN INC. ,  ALLEN, Jennifer R. ,  TEGLEY, Christopher M. ,  BISWAS, Kaustav ,  BURLI, Roland ,  MULLER, Kristine M. ,  FROHN, Michael J. ,  GOLDEN, Jennifer E. ,  MERCEDE, Stephanie J. ,  NEIRA, Susana C. ,  PETERKIN, Tanya A. N. ,  HUNGATE, Randall W. ,  KURZEJA, Robert ,  YU, Violeta ,  DAO, Jennifer

Inventor： ALLEN, Jennifer R. ,  TEGLEY, Christopher M. ,  BISWAS, Kaustav ,  BURLI, Roland ,  MULLER, Kristine M. ,  FROHN, Michael J. ,  GOLDEN, Jennifer E. ,  MERCEDE, Stephanie J. ,  NEIRA, Susana C. ,  PETERKIN, Tanya A. N. ,  HUNGATE, Randall W. ,  KURZEJA, Robert ,  YU, Violeta ,  DAO, Jennifer

CPC classification number: C07D215/22 ,  C07D215/56 ,  C07D401/04 ,  C07D405/04 ,  C07D409/04 ,  C07D413/04 ,  C07D417/04 ,  G01N33/542

Abstract: This invention relates to new quinolone based compounds that exhibit prolyl hydroxylase inhibitory activity. This invention also relates to methods of increasing HIF levels or activity in a subject or treating a condition associated with HIF levels or activity in a subject by administering to the subject at least one quinolone based compound. This invention further involves assays for the detection of a hydroxyproline residue in a HIF molecule.

Abstract translation: 本发明涉及显示脯氨酰羟化酶抑制活性的新型喹诺酮类化合物。 本发明还涉及通过向受试者施用至少一种基于喹诺酮的化合物来增加受试者中HIF水平或活性或治疗与受试者中HIF水平或活性相关的病症的方法。 本发明还涉及用于检测HIF分子中的羟脯氨酸残基的测定法。