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1. 发明申请

WO2006004658A2 FURANOPYRIMIDINES 审中-公开
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
申请人： 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
发明人： 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分类号： C07D498/00
CPC分类号： C07D491/04 , C07D495/04
摘要： 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).
摘要翻译：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。

2. 发明申请

WO2005113494A3 NITROGENATED HETEROCYCLIC DERIVATIVES AS PROTEIN KINASE MODULATORS AND USE FOR THE TREATMENT OF ANGIOGENESIS AND CANCER 审中-公开
标题翻译：作为蛋白激酶调节剂的氮杂异构体衍生物和用于治疗血液发生和癌症的用途
公开(公告)号：WO2005113494A3
公开(公告)日：2006-03-16
申请号：PCT/US2005016346
申请日：2005-05-09
申请人： AMGEN INC , GEUNS-MEYER STEPHANIE D , HODOUS BRIAN L , CHAFFEE STUART C , TEMPEST PAUL A , OLIVIERI PHILIP R , JOHNSON REBECCA E , ALBRECHT BRIAN K , PATEL VINOD F , CEE VICTOR J , KIM JOSEPH L , BELLON STEVEN , ZHU XIAOTIAN , CHENG YUAN , XI NING , ROMERO KARINA , NGUYEN HANH NHO , DEAK HOLLY L
发明人： GEUNS-MEYER STEPHANIE D , HODOUS BRIAN L , CHAFFEE STUART C , TEMPEST PAUL A , OLIVIERI PHILIP R , JOHNSON REBECCA E , ALBRECHT BRIAN K , PATEL VINOD F , CEE VICTOR J , KIM JOSEPH L , BELLON STEVEN , ZHU XIAOTIAN , CHENG YUAN , XI NING , ROMERO KARINA , NGUYEN HANH NHO , DEAK HOLLY L
IPC分类号： C07D401/04 , A61K31/4427 , A61K31/4439 , A61K31/497 , A61K31/506 , A61K31/53 , C07D213/73 , C07D401/14 , C07D405/14 , C07D407/14 , C07D409/14 , C07D413/14 , C07D471/04
CPC分类号： C07D213/73 , C07D239/42 , C07D401/04 , C07D401/14 , C07D405/14 , C07D407/14 , C07D409/14 , C07D413/14 , C07D471/04
摘要： The present invention relates to chemical compounds having a general formula (I) wherein A, B, D, E, G, H
摘要翻译：本发明涉及具有通式（I）的化合物，其中A，B，D，E，G，H

3. 发明申请

WO0070030A9 CRYSTAL OF A LYMPHOCYTE KINASE-LIGAND COMPLEX AND METHODS OF USE 审中-公开
标题翻译： LYMPHOCYTE KINASE-LIGAND复合物的晶体和使用方法
公开(公告)号：WO0070030A9
公开(公告)日：2002-08-29
申请号：PCT/US0013881
申请日：2000-05-19
申请人： AMGEN INC , ZHU XIAOTIAN
发明人： ZHU XIAOTIAN
IPC分类号： C12N9/12 , C12Q1/42
CPC分类号： C12N9/1205 , Y02A90/26
摘要： The invention relates to the three-dimensional structure of a crystal of a kinase enzyme complexed with a ligand. The three-dimensional structure of a protein kinase-ligand complex is disclosed. The invention also relates to methods of preparing such crystals. Kinase-ligand crystal structures wherein the ligand is an inhibitor molecule are useful for providing structure information that may be integrated into drug screening and drug design processes. Thus, the invention also relates to methods of using the crystal structure of kinase enzyme-ligand complexes for identifying, designing, selecting, or testing inhibitors of kinase enzymes, such inhibitors being useful as therapeutics for the treatment or modulation of (i) diseases; (ii) disease symptoms; or (iii) the effect of other physiological events mediated by kinases; having one or more kinase enzymes involved in their pathology.
摘要翻译：本发明涉及与配体络合的激酶的晶体的三维结构。公开了蛋白激酶 - 配体复合物的三维结构。本发明还涉及制备这种晶体的方法。其中配体是抑制剂分子的激酶配体晶体结构可用于提供可以整合到药物筛选和药物设计过程中的结构信息。因此，本发明还涉及使用激酶 - 配体配合物的晶体结构鉴定，设计，选择或测试激酶的抑制剂的方法，所述抑制剂可用作治疗或调节（i）疾病的治疗剂; （ii）疾病症状; 或（iii）由激酶介导的其他生理事件的作用; 具有参与其病理学的一种或多种激酶。

4. 发明申请

WO2007133560A9 ACETYLENIC HETEROARYL COMPOUNDS 审中-公开
标题翻译：乙炔基杂原子化合物
公开(公告)号：WO2007133560A9
公开(公告)日：2008-11-13
申请号：PCT/US2007011134
申请日：2007-05-08
申请人： ARIAD PHARMA INC , WANG YIHAN , ZHU XIAOTIAN , SUNDARAMOORTHI RAJESWARI , HUANG WEI-SHENG , ZOU DONG , THOMAS R MATHEW , QI JIWEI , ROMERO JAN ANTOINETTE C , DALGARNO DAVID C , SHAKESPEARE WILLIAM C , SAWYER TOMI K , METCALF CHESTER A
发明人： WANG YIHAN , ZHU XIAOTIAN , SUNDARAMOORTHI RAJESWARI , HUANG WEI-SHENG , ZOU DONG , THOMAS R MATHEW , QI JIWEI , ROMERO JAN ANTOINETTE C , DALGARNO DAVID C , SHAKESPEARE WILLIAM C , SAWYER TOMI K , METCALF CHESTER A
IPC分类号： A61K31/53 , A61K31/4745 , A61K31/496 , A61K31/498 , A61K31/503 , A61K31/519 , C07D487/04
CPC分类号： C07D213/56 , C07D213/73 , C07D213/75 , C07D213/78 , C07D217/14 , C07D217/22 , C07D237/20 , C07D237/28 , C07D239/26 , C07D241/12 , C07D241/20 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/06 , C07D413/12 , C07D417/12 , C07D471/04
摘要： This invention relates to compounds of the general formula (I):in which the variable groups are as defined herein, and to their preparation and use.
摘要翻译：本发明涉及通式（I）的化合物：其中可变基团如本文所定义，及其制备和用途。

5. 发明申请

WO2007133562A2 MONOCYCLIC HETEROARYL COMPOUNDS 审中-公开
标题翻译：单环异构化合物
公开(公告)号：WO2007133562A2
公开(公告)日：2007-11-22
申请号：PCT/US2007011136
申请日：2007-05-08
申请人： ARIAD PHARMA INC , SHAKESPEARE WILLIAM C , HUANG WEI-SHENG , DALGARNO DAVID C , ZHU XIAOTIAN , THOMAS R MATHEW , WANG YIHAN , QI JIWEI , SUNDARAMOORTHI RAJESWARI , ZOU DONG , METCALF CHESTER A , SAWYER TOMI K , ROMERO JAN ANTIONETTE C
发明人： SHAKESPEARE WILLIAM C , HUANG WEI-SHENG , DALGARNO DAVID C , ZHU XIAOTIAN , THOMAS R MATHEW , WANG YIHAN , QI JIWEI , SUNDARAMOORTHI RAJESWARI , ZOU DONG , METCALF CHESTER A , SAWYER TOMI K , ROMERO JAN ANTIONETTE C
IPC分类号： E06B3/12
CPC分类号： C07D231/12 , C07D233/64 , C07D233/90 , C07D277/40 , C07D403/12 , C07D403/14 , C07D417/12 , C07D417/14
摘要： This invention relates to compounds of the general formula(I) in which the variable groups are as defined herein, and to their preparation and use.
摘要翻译：本发明涉及其中可变基团如本文所定义的通式（I）的化合物及其制备和用途。

6. 发明申请

WO2007133560A2 ACETYLENIC HETEROARYL COMPOUNDS 审中-公开
标题翻译：乙烯异构体化合物
公开(公告)号：WO2007133560A2
公开(公告)日：2007-11-22
申请号：PCT/US2007011134
申请日：2007-05-08
申请人： ARIAD PHARMA INC , WANG YIHAN , ZHU XIAOTIAN , SUNDARAMOORTHI RAJESWARI , HUANG WEI-SHENG , ZOU DONG , THOMAS R MATHEW , QL JIWEI , ROMERO JAN ANTIONETTE C , DALGARNO DAVID C , SHAKESPEARE WILLIAM C , SAWYER TOMI K , METCALF CHESTER A
发明人： WANG YIHAN , ZHU XIAOTIAN , SUNDARAMOORTHI RAJESWARI , HUANG WEI-SHENG , ZOU DONG , THOMAS R MATHEW , QL JIWEI , ROMERO JAN ANTIONETTE C , DALGARNO DAVID C , SHAKESPEARE WILLIAM C , SAWYER TOMI K , METCALF CHESTER A
IPC分类号： E06C7/16
CPC分类号： C07D213/56 , C07D213/73 , C07D213/75 , C07D213/78 , C07D217/14 , C07D217/22 , C07D237/20 , C07D237/28 , C07D239/26 , C07D241/12 , C07D241/20 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/06 , C07D413/12 , C07D417/12 , C07D471/04
摘要： This invention relates to compounds of the general formula (I):in which the variable groups are as defined herein, and to their preparation and use.
摘要翻译：本发明涉及通式（I）的化合物：其中可变基团如本文所定义，及其制备和用途。

7. 发明申请

WO2010068292A8 AZAINDOLE DERIVATIVES AS KINASE INHIBITORS 审中-公开
标题翻译：亚胺衍生物作为激酶抑制剂
公开(公告)号：WO2010068292A8
公开(公告)日：2011-06-30
申请号：PCT/US2009006520
申请日：2009-12-11
申请人： ARIAD PHARMA INC , QI JIWEI , WANG YIHAN , LI FENG , SHAKESPEARE WILLIAM C , KOHLMANN ANNA , DALGARNO DAVID C , ZHU XIAOTIAN
发明人： QI JIWEI , WANG YIHAN , LI FENG , SHAKESPEARE WILLIAM C , KOHLMANN ANNA , DALGARNO DAVID C , ZHU XIAOTIAN
IPC分类号： A01N43/42 , A61K31/44
CPC分类号： A61K31/44 , C07D471/04
摘要： This invention relates to compounds of the general formula (I) in which the variable groups are as defined herein, and to their preparation and use.
摘要翻译：本发明涉及其中可变基团如本文所定义的通式（I）的化合物及其制备和用途。

8. 发明申请

WO2007075869A2 BICYCLIC HETEROARYL COMPOUNDS 审中-公开
标题翻译：双环杂芳基化合物
公开(公告)号：WO2007075869A2
公开(公告)日：2007-07-05
申请号：PCT/US2006048758
申请日：2006-12-22
申请人： ARIAD PHARMA INC , ZOU DONG , HUANG WEI-SHENG , THOMAS R MATHEW , ROMERO JAN ANTIONETTE C , QI JIWEI , WANG YIHAN , ZHU XIAOTIAN , SHAKESPEARE WILLIAM C , SUNDARAMOORTHI RAJESWARI , METCALF CHESTER A III , DALGARNO DAVID C , SAWYER TOMI K
发明人： ZOU DONG , HUANG WEI-SHENG , THOMAS R MATHEW , ROMERO JAN ANTIONETTE C , QI JIWEI , WANG YIHAN , ZHU XIAOTIAN , SHAKESPEARE WILLIAM C , SUNDARAMOORTHI RAJESWARI , METCALF CHESTER A III , DALGARNO DAVID C , SAWYER TOMI K
IPC分类号： A61K31/53 , A61K31/519
CPC分类号： C07D471/04 , C07D473/34 , C07D487/04
摘要： This invention relates to compounds of the general formula (I) in which the variable groups are as defined herein, and to their preparation and use.
摘要翻译：本发明涉及其中可变基团如本文所定义的通式（I）的化合物，及其制备和用途。

9. 发明申请

WO03018022A8 2-AMINO-4-HETEROARYLAMINOPYRIMIDINE DERIVATIVES FOR USE IN THE TREATMENT OF CANCER 审中-公开
标题翻译：用于治疗癌症的2-氨基-4-杂芳基氨基嘧啶衍生物
公开(公告)号：WO03018022A8
公开(公告)日：2003-10-02
申请号：PCT/US0226926
申请日：2002-08-22
申请人： AMGEN INC
发明人： BUCHANAN JOHN L , CHAFFEE STUART , HARMANGE JEAN-CHRISTOPHE , NOVAK PERRY M , ZHU XIAOTIAN
IPC分类号： A61K31/506 , A61K31/5377 , A61P35/00 , A61P43/00 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
CPC分类号： C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
摘要： Compounds of Formula (I) are claimed, wherein R is a heteroaryl ring containing at least one oxygen of sulfur heteroatom and R is as defined in the claims. These compounds are useful in the treatment of cancer.
摘要翻译：要求保护式（I）的化合物，其中R 1是含有至少一个硫杂原子氧的杂芳基环，并且R 2如权利要求中所定义。这些化合物可用于治疗癌症。

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