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1. 发明申请

WO2007024680A1 PYRAZOLOPYRIDINE AND PYRAZOLOPYRIMIDINE COMPOUNDS USEFUL AS KINASE ENZYMES MODULATORS 审中-公开
标题翻译：用作激酶酶调节剂的吡唑并吡啶和吡唑并嘧啶化合物有用
公开(公告)号：WO2007024680A1
公开(公告)日：2007-03-01
申请号：PCT/US2006/032314
申请日：2006-08-18
申请人： AMGEN INC. , BUCHANAN, John L. , BUCKNER, William H. , CARDOZO, Mario G. , DIMAURO, Erin F. , FU, Jiasheng , HAO, Xiaolin , JIAO, XianYun , KAYSER, Frank , KOPECKY, David J. , MASSE, Craig E. , TOMLINSON, Susan A. , WHITE, Ryan , ZHU, Xiaotian
发明人： BUCHANAN, John L. , BUCKNER, William H. , CARDOZO, Mario G. , DIMAURO, Erin F. , FU, Jiasheng , HAO, Xiaolin , JIAO, XianYun , KAYSER, Frank , KOPECKY, David J. , MASSE, Craig E. , TOMLINSON, Susan A. , WHITE, Ryan , ZHU, Xiaotian
IPC分类号： C07D487/04 , C07D231/56 , C07D403/06 , C07D405/06 , C07D401/14 , A61K31/519 , A61K31/416 , A61P19/00 , A61P17/00 , A61P35/00
CPC分类号： C07D403/06 , C07D231/56 , C07D401/14 , C07D405/06 , C07D487/04
摘要： The present invention relates to compounds of Formula (I) or a stereomer, a tautomer, a solvate, a pharmaceutically acceptable salt, or a prodrug thereof, pharmaceutical formulations containing the compounds, methods of treatments using the compounds, for example, protein tyrosine kinase-associated disorders such as immunologic and oncologic disorders and methods of preparing medicaments comprising the compounds.
摘要翻译：本发明涉及式（I）的化合物或立体异构体，互变异构体，溶剂化物，药学上可接受的盐或其前药，含有该化合物的药物制剂，使用该化合物的治疗方法，例如蛋白酪氨酸激酶 - 相关疾病如免疫学和肿瘤学疾病以及制备包含该化合物的药物的方法。

2. 发明申请

WO2006004658A3 FURANOPYRIMIDINES 审中-公开
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
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： C07D498/04 , A61K31/519
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).

3. 发明申请

WO2005113494A2 PROTEIN KINASE MODULATORS AND METHOD OF USE 审中-公开
标题翻译：蛋白激酶调节剂及其使用方法
公开(公告)号：WO2005113494A2
公开(公告)日：2005-12-01
申请号：PCT/US2005/016346
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： C07D1/04
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 1-5 and R 1-4 are defined herein, and synthetic intermediates, which are capable of modulating various protein kinase receptor enzymes and, thereby, influencing various disease states and conditions related to the activities of these kinases. For example, the compounds are capable of modulating kinase enzymes thereby influencing the process of angiogenesis and treating angiogenesis-related diseases and other poliferative disorders, including cancer and inflammation. The invention also includes pharmaceutical compositions, including the compounds, and methods of treating disease states related to the activity of protein kinases.
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 1-5和R 1-4如本文所定义，以及合成中间体，其能够调节各种蛋白激酶受体酶，从而影响与这些激酶的活性相关的各种疾病状态和状况。例如，这些化合物能够调节激酶，从而影响血管生成过程并治疗血管生成相关疾病和其它包括癌症和炎症的复发性疾病。本发明还包括药物组合物，包括该化合物，以及治疗与蛋白激酶活性有关的疾病状态的方法。

4. 发明申请

WO2005021551A1 SUBSTITUTED HETEROCYCLIC COMPOUNDS AND METHODS OF USE 审中-公开
标题翻译：取代的杂环化合物及其使用方法
公开(公告)号：WO2005021551A1
公开(公告)日：2005-03-10
申请号：PCT/US2004/029246
申请日：2004-08-23
申请人： AMGEN INC. , NUNES, Joseph J. , ZHU, Xiaotian , ERMANN, Monika , GHIRON, Chiara , JOHNSTON, David N. , SALUSTE, Carl-Gustaf Pierre
发明人： NUNES, Joseph J. , ZHU, Xiaotian , ERMANN, Monika , GHIRON, Chiara , JOHNSTON, David N. , SALUSTE, Carl-Gustaf Pierre
IPC分类号： C07D487/14
CPC分类号： C07D487/14
摘要： The present invention relates to tetracyclic pyrimidines or pyridines or pharmaceutically-acceptable salts or derivatives thereof. Also included are methods of use of the tetracyclic pyrimidines or pyridines including use related to treating inflammation, inhibiting T cell activation and proliferation, arthritis, organ transplant, ischemic or reperfusion injury, myocardial infarction, stroke, multiple sclerosis, inflammatory bowel disease and many other related disorders in a subject, the methods comprising administering a therapeutically-effective amount a compound as described above to the subject.
摘要翻译：本发明涉及四环嘧啶或吡啶或其药学上可接受的盐或衍生物。还包括使用四环嘧啶或吡啶的方法，包括与治疗炎症有关的用途，抑制T细胞活化和增殖，关节炎，器官移植，缺血或再灌注损伤，心肌梗死，中风，多发性硬化，炎性肠病等许多方法所述方法包括向受试者施用治疗有效量的如上所述的化合物。

5. 发明申请

WO2005009443A1 2-AMINO-4-HYDROXY-5-PYRIMIDINECARBOXAMIDE DERIVATIVES AND RELATED COMPOUNDS AS INHIBITORS OF T CELL ACTIVATION FOR THE TREATMENT OF INFLAMMATORY DISEASES 审中-公开
标题翻译： 2-氨基-4-羟基-5-嘧啶甲酰胺衍生物及相关化合物作为T细胞活化的抑制剂治疗炎症性疾病
公开(公告)号：WO2005009443A1
公开(公告)日：2005-02-03
申请号：PCT/US2004/020243
申请日：2004-06-24
申请人： AMGEN INC. , NUNES, Joseph J. , ZHU, Xiaotian , AMOUZEGH, Patricia , GHIRON, Chiara , JOHNSTON, David N. , POWER, Eoin, Christopher
发明人： NUNES, Joseph J. , ZHU, Xiaotian , AMOUZEGH, Patricia , GHIRON, Chiara , JOHNSTON, David N. , POWER, Eoin, Christopher
IPC分类号： A61K31/506
CPC分类号： C07D213/82 , C07D239/47 , C07D239/48
摘要： The present invention relates to pyrimidine or pyridine carboxamides or pharmaceutically-acceptable salts thereof. Also included is a method of treatment of inflammation, inhibition of T cell activation and proliferation, arthritis, rheumatoid arthritis, psoriatic arthritis, osteoarthritis, organ transplant, acute transplant or heterograft or homograft rejection, transplantation tolerance induction, ischemic or reperfusion injury, myocardial infarction, stroke, multiple sclerosis, inflammatory bowel disease, including ulcerative colitis, Crohn's disease, lupus, contact hypersensitivity, delayed-type hypersensitivity, and gluten-sensitive enteropathy, type 1 diabetes, psoriasis, contact dermatitis, Hashimoto's thyroiditis, Sjogren's syndrome, autoimmune hyperthyroidism, Addison's disease, autoimmune polyglandular disease, autoimmune alopecia, pernicious anemia, vitiligo, autoimmune hypopituatarism, Guillain-Barre syndrome, glomerulonephritis, serum sickness, uticaria, allergic diseases, asthma, hayfever, allergic rhinitis, scleracielma, mycosis fungoides, dermatomyositis, alopecia areata, chronic actinic dermatitis, eczema, Behcet's disease, Pustulosis palmoplanteris, Pyoderma gangrenum, Sezary's syndrome, atopic dermatitis, systemic schlerosis, morphea, atopic dermatitis, colon carcinoma or thymoma in a mammal comprising administering a therapeutically-effective amount a compound as described above.
摘要翻译：本发明涉及嘧啶或吡啶甲酰胺或其药学上可接受的盐。还包括治疗炎症，抑制T细胞活化和增殖，关节炎，类风湿性关节炎，银屑病关节炎，骨关节炎，器官移植，急性移植或异种移植或同种移植物排斥，移植耐受性诱导，缺血或再灌注损伤，心肌梗死的方法，中风，多发性硬化，炎症性肠病，包括溃疡性结肠炎，克罗恩病，狼疮，接触性超敏反应，迟发型超敏反应和麸质敏感性肠病，1型糖尿病，牛皮癣，接触性皮炎，桥本氏甲状腺炎，干燥综合征，自身免疫性甲状腺功能亢进，艾迪生病，自身免疫性多腺病，自身免疫性脱发，恶性贫血，白癜风，自身免疫性低位症，吉兰巴利综合征，肾小球性肾炎，血清病，荨麻疹，过敏性疾病，哮喘，高粱，过敏性鼻炎，巩膜瘤，蕈样真菌病，皮肌炎，秃头症，慢性交感包括给予治疗有效量的如上所述的化合物，包括给予治疗有效量的上述化合物，其中，所述治疗有效量的治疗有效量的药物组合物包含给药治疗有效量的化合物。

6. 发明申请

WO2000070030A1 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：WO2000070030A1
公开(公告)日：2000-11-23
申请号：PCT/US2000/013881
申请日：2000-05-19
申请人： AMGEN INC. , ZHU, Xiaotian
发明人： ZHU, Xiaotian
IPC分类号： C12N9/12
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。

8. 发明公开

EP2841062A1 METHODS AND COMPOSITIONS FOR RAF KINASE MEDIATED DISEASES 审中-公开
标题翻译： RAF激酶介导的疾病的方法和组合物
公开(公告)号：EP2841062A1
公开(公告)日：2015-03-04
申请号：EP13782134.4
申请日：2013-03-12
申请人： ARIAD PHARMACEUTICALS, INC. , Gozgit, Joseph M. , Rivera, Victor M. , Shakespeare, William C. , Zhu, Xiaotian , Dalgarno, David C.
发明人： GOZGIT, Joseph, M. , RIVERA, Victor, M. , SHAKESPEARE, William, C. , ZHU, Xiaotian , DALGARNO, David, C.
IPC分类号： A61K31/165
CPC分类号： C07D487/04 , A61K31/437 , A61K31/496 , A61K31/4985 , A61K31/5025 , A61K31/5377 , C07D471/04 , C07D473/34
摘要： The invention discloses methods and compositions for treating or preventing RAF kinase mediated diseases or conditions by administering a compound of Formula 1: or a pharmaceutically acceptable salt, solvate or hydrate thereof, wherein the variables are defined as herein.
摘要翻译：本发明公开了通过施用式1的化合物或其药学上可接受的盐，溶剂化物或水合物来治疗或预防RAF激酶介导的疾病或病症的方法和组合物，其中变量如本文所定义。

9. 发明公开

EP2844642A1 COMPOUNDS FOR INHIBITING CELL PROLIFERATION IN EGFR-DRIVEN CANCERS 有权转让
标题翻译：一种抑制细胞增殖的EGFR介导的肿瘤
公开(公告)号：EP2844642A1
公开(公告)日：2015-03-11
申请号：EP13788352.6
申请日：2013-03-15
申请人： ARIAD PHARMACEUTICALS, INC. , Zhu, Xiaotian , Wang, Yihan , Shakespeare, William C. , Huang, Wei-Sheng , Dalgarno, David C.
发明人： ZHU, Xiaotian , WANG, Yihan , SHAKESPEARE, William, C. , HUANG, Wei-Sheng , DALGARNO, David, C.
IPC分类号： C07D239/48
摘要： The invention features compounds, pharmaceutical compositions and methods for treating patients who have an EGFR-driven cancer of Formula (I), wherein the variables are as defined herein.

10. 发明申请

WO2015195228A1 HETEROARYL COMPOUNDS FOR KINASE INHIBITION 审中-公开
标题翻译：用于激酶抑制的异氟醚化合物
公开(公告)号：WO2015195228A1
公开(公告)日：2015-12-23
申请号：PCT/US2015/030576
申请日：2015-05-13
申请人： ARIAD PHARMACEUTICALS, INC. , HUANG, Wei-sheng , GONG, Yongjin , LI, Feng , BENCIVENGA, Nicholas, E. , DALGARNO, David, C. , KOHLMANN, Anna , SHAKESPEARE, William, C. , THOMAS, Ranny, M. , ZHU, Xiaotian , WEST, Angela, V. , YOUNGSAYE, Willmen , ZHANG, Yun , ZHOU, Tianjun
发明人： HUANG, Wei-sheng , GONG, Yongjin , LI, Feng , BENCIVENGA, Nicholas, E. , DALGARNO, David, C. , KOHLMANN, Anna , SHAKESPEARE, William, C. , THOMAS, Ranny, M. , ZHU, Xiaotian , WEST, Angela, V. , YOUNGSAYE, Willmen , ZHANG, Yun , ZHOU, Tianjun
IPC分类号： C07D403/14 , C07D473/16
CPC分类号： C07D471/04 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/12 , C07D405/14 , C07F9/65583
摘要： Compounds and pharmaceutical compositions that modulate kinase activity, including mutant EGFR and mutant HER2 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including mutant EGFRand mutant HER2 activity, are described herein.
摘要翻译：本文描述了调节激酶活性的化合物和药物组合物，包括突变型EGFR和突变型HER2激酶活性，以及化合物，药物组合物和治疗与激酶活性相关的疾病和病症（包括突变型EGFR和突变型HER2活性）的方法。

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