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：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：WO2006004658A3

公开(公告)日：2006-01-12

申请号：PCT/US2005/022727

申请日：2005-06-29

Applicant: AMGEN INC. ,  BUCHANAN, John L. ,  BUCKNER, William H. ,  BURKITT, Simon A. ,  DIMAURO, Erin F. ,  FARTHING, Christopher N. ,  FRENKEL, Alexander David ,  HARRISON, Martin J. ,  KAYSER, Frank ,  LIU, Jinqian ,  LIVELY, Sarah E. ,  MARSHALL, Teresa L. ,  MCGOWAN, David C. ,  SHARMA, Rajiv ,  SHUTTLEWORTH, Stephen Joseph ,  ZHU, Xiaotian

Inventor： BUCHANAN, John L. ,  BUCKNER, William H. ,  BURKITT, Simon A. ,  DIMAURO, Erin F. ,  FARTHING, Christopher N. ,  FRENKEL, Alexander David ,  HARRISON, Martin J. ,  KAYSER, Frank ,  LIU, Jinqian ,  LIVELY, Sarah E. ,  MARSHALL, Teresa L. ,  MCGOWAN, David C. ,  SHARMA, Rajiv ,  SHUTTLEWORTH, Stephen Joseph ,  ZHU, Xiaotian

IPC: C07D498/04 ,  A61K31/519

Abstract: The present invention relates to furanopyrimidine compounds having the general Formula (I) and stereoisomers, tautomers, solvates, pharmaceutically acceptable salts and derivatives, and prodrugs thereof. The invention also includes pharmaceutical compositions comprising a compound of Formula (I), methods of treating various diseases and conditions in a mammal, including inflammation, inhibition of T cell activation, proliferation, arthritis, organ transplant, ischemic or reperfusion injury, myocardial infarction, stroke, multiple sclerosis, inflammatory bowel disease, Crohn's disease, lupus, hypersensitivity, type 1 diabetes, psoriasis, dermatitis, Hashimoto's thyroiditis, Sjogren's syndrome, autoimmune hyperthyroidism, Addison's disease, autoimmune diseases, glomerulonephritis, allergic diseases, asthma, hayfever, eczema, cancer, colon carcinoma and thymoma, comprising administering to the mammal a therapeutically effective amount of a compound of Formula (I). The invention also relates to methods of manufacturing medicaments, which comprise one or more compounds of Formula (I).

公开(公告)号：WO2006004658A2

公开(公告)日：2006-01-12

申请号：PCT/US2005022727

申请日：2005-06-29

Applicant: AMGEN INC ,  BUCHANAN JOHN L ,  BUCKNER WILLIAM H ,  BURKITT SIMON A ,  DIMAURO ERIN F ,  FARTHING CHRISTOPHER N ,  FRENKEL ALEXANDER DAVID ,  HARRISON MARTIN J ,  KAYSER FRANK ,  LIU JINQIAN ,  LIVELY SARAH E ,  MARSHALL TERESA L ,  MCGOWAN DAVID C ,  SHARMA RAJIV ,  SHUTTLEWORTH STEPHEN JOSEPH ,  ZHU XIAOTIAN

Inventor： BUCHANAN JOHN L ,  BUCKNER WILLIAM H ,  BURKITT SIMON A ,  DIMAURO ERIN F ,  FARTHING CHRISTOPHER N ,  FRENKEL ALEXANDER DAVID ,  HARRISON MARTIN J ,  KAYSER FRANK ,  LIU JINQIAN ,  LIVELY SARAH E ,  MARSHALL TERESA L ,  MCGOWAN DAVID C ,  SHARMA RAJIV ,  SHUTTLEWORTH STEPHEN JOSEPH ,  ZHU XIAOTIAN

IPC: C07D498/00

CPC classification number: C07D491/04 ,  C07D495/04

Abstract: The present invention relates to furanopyrimidine compounds having the general Formula (I) and stereoisomers, tautomers, solvates, pharmaceutically acceptable salts and derivatives, and prodrugs thereof. The invention also includes pharmaceutical compositions comprising a compound of Formula (I), methods of treating various diseases and conditions in a mammal, including inflammation, inhibition of T cell activation, proliferation, arthritis, organ transplant, ischemic or reperfusion injury, myocardial infarction, stroke, multiple sclerosis, inflammatory bowel disease, Crohn's disease, lupus, hypersensitivity, type 1 diabetes, psoriasis, dermatitis, Hashimoto's thyroiditis, Sjogren's syndrome, autoimmune hyperthyroidism, Addison's disease, autoimmune diseases, glomerulonephritis, allergic diseases, asthma, hayfever, eczema, cancer, colon carcinoma and thymoma, comprising administering to the mammal a therapeutically effective amount of a compound of Formula (I). The invention also relates to methods of manufacturing medicaments, which comprise one or more compounds of Formula (I).

Abstract translation: 本发明涉及具有通式（I）的呋喃并嘧啶化合物及其立体异构体，互变异构体，溶剂化物，药学上可接受的盐和衍生物以及前药。 本发明还包括包含式（I）化合物的药物组合物，治疗哺乳动物各种疾病和病症的方法，包括炎症，抑制T细胞活化，增殖，关节炎，器官移植，局部缺血或再灌注损伤，心肌梗塞， 中风，多发性硬化症，炎性肠病，克罗恩病，狼疮，超敏反应，1型糖尿病，牛皮癣，皮炎，桥本氏甲状腺炎，干燥综合征，自身免疫性甲状腺机能亢进症，艾迪生病，自身免疫性疾病，肾小球肾炎，过敏性疾病， 癌症，结肠癌和胸腺瘤，所述方法包括给所述哺乳动物施用治疗有效量的式（I）化合物。 本发明还涉及制造包含一种或多种式（I）化合物的药物的方法。