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21. 发明授权

US09012462B2 Phosphorous derivatives as kinase inhibitors 有权
标题翻译：磷酸衍生物作为激酶抑制剂
公开(公告)号：US09012462B2
公开(公告)日：2015-04-21
申请号：US12736910
申请日：2009-05-21
申请人： Yihan Wang , Wei-Sheng Huang , Shuangying Liu , William C. Shakespeare , R. Mathew Thomas , Jiwei Qi , Feng Li , Xiaotian Zhu , Anna Kohlman , David C. Dalgarno , Jan Antoinette C. Romero , Dong Zou
发明人： Yihan Wang , Wei-Sheng Huang , Shuangying Liu , William C. Shakespeare , R. Mathew Thomas , Jiwei Qi , Feng Li , Xiaotian Zhu , Anna Kohlman , David C. Dalgarno , Jan Antoinette C. Romero , Dong Zou
IPC分类号： A61K31/506 , C07F9/30 , C07D239/48 , C07F9/6509 , C07F9/6512 , C07F9/6521 , C07F9/6558 , C07F9/6561 , C07F9/6568 , C07F9/6571
CPC分类号： C07F9/6533 , C07D239/48 , C07F9/58 , C07F9/650905 , C07F9/6512 , C07F9/6521 , C07F9/65218 , C07F9/65583 , C07F9/65586 , C07F9/6561 , C07F9/65616 , C07F9/65685 , C07F9/657172 , C07F9/65846
摘要： The invention features 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：本发明的特征在于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。

22. 发明授权

US08586566B2 Unsaturated heterocyclic derivatives 有权
标题翻译：不饱和杂环衍生物
公开(公告)号：US08586566B2
公开(公告)日：2013-11-19
申请号：US13311106
申请日：2011-12-05
申请人： Yihan Wang , Wei-Sheng Huang , Rajeswari Sundaramoorthi , Xiaotian Zhu , R. Mathew Thomas , William C. Shakespeare , David C. Dalgarno , Tomi K. Sawyer
发明人： Yihan Wang , Wei-Sheng Huang , Rajeswari Sundaramoorthi , Xiaotian Zhu , R. Mathew Thomas , William C. Shakespeare , David C. Dalgarno , Tomi K. Sawyer
IPC分类号： A61K31/675 , A61K31/52 , A61P35/00 , C07F9/6561 , C07D473/32
CPC分类号： C07F9/65616
摘要： This invention relates to specific compounds and their pharmaceutically acceptable salts of the general formula: wherein Q is —CR═CR′— and Ring A is an aryl, heteroaryl or heterocyclic ring or ring system. This invention also relates to pharmaceutical compositions comprising such specific compounds or their pharmaceutically acceptable salts and a pharmaceutically acceptable carrier or adjuvant.
摘要翻译：本发明涉及以下通式的具体化合物及其药学上可接受的盐：其中Q是-CR = CR'-，环A是芳基，杂芳基或杂环或环系。本发明还涉及包含这些特定化合物或其药学上可接受的盐和药学上可接受的载体或佐剂的药物组合物。

23. 发明授权

US08476434B2 Protein kinase modulators and method of use 有权
标题翻译：蛋白激酶调节剂及其使用方法
公开(公告)号：US08476434B2
公开(公告)日：2013-07-02
申请号：US12952156
申请日：2010-11-22
申请人： Stephanie D. Geuns-Meyer , Brian L. Hodous , Stuart C. Chaffee , Paul Tempest , Ning Xi , Phillip R. Olivieri , Joseph L. Kim , Steven Bellon , Xiaotian Zhu , Yuan Cheng , Brian K. Albrecht , Vinod F. Patel , Victor J. Cee , Karina Romero , Hanh Nho Nguyen , Holly L. Deak , Rebecca E. Johnson
发明人： Stephanie D. Geuns-Meyer , Brian L. Hodous , Stuart C. Chaffee , Paul Tempest , Ning Xi , Phillip R. Olivieri , Joseph L. Kim , Steven Bellon , Xiaotian Zhu , Yuan Cheng , Brian K. Albrecht , Vinod F. Patel , Victor J. Cee , Karina Romero , Hanh Nho Nguyen , Holly L. Deak , Rebecca E. Johnson
IPC分类号： C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , A61K31/4427 , A61K31/506 , A61K31/54 , A61P19/02 , A61P35/00
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, H1-5 and R1-4 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 proliferative 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，H1-5和R1-4在本文中定义，以及能够调节各种蛋白激酶受体酶的合成中间体，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，化合物能够调节激酶，从而影响血管发生过程并治疗血管生成相关疾病和其它增殖性疾病，包括癌症和炎症。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。

24. 发明授权

US08470851B2 Substituted acetylenic imidazo[1,2-A]pyridine compounds as kinase inhibitors 有权
标题翻译：取代的炔属咪唑并[1,2-A]吡啶化合物作为激酶抑制剂
公开(公告)号：US08470851B2
公开(公告)日：2013-06-25
申请号：US13357745
申请日：2012-01-25
申请人： Dong Zou , Wei-Sheng Huang , R. Mathew Thomas , Jan Antoinette C. Romero , Jiwei Qi , Yihan Wang , Xiaotian Zhu , William C. Shakespeare , Rajeswari Sundaramoorthi , Chester A. Metcalf, III , David C. Dalgarno , Tomi K. Sawyer
发明人： Dong Zou , Wei-Sheng Huang , R. Mathew Thomas , Jan Antoinette C. Romero , Jiwei Qi , Yihan Wang , Xiaotian Zhu , William C. Shakespeare , Rajeswari Sundaramoorthi , Chester A. Metcalf, III , David C. Dalgarno , Tomi K. Sawyer
IPC分类号： A61K31/44
CPC分类号： C07D471/04 , C07D473/34 , C07D487/04
摘要： This invention relates to compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.
摘要翻译：本发明涉及以下通式的化合物：其中可变基团如本文所定义，及其制备和用途。

25. 发明申请

US20120178716A1 Unsaturated Heterocyclic Derivatives 有权
标题翻译：不饱和杂环衍生物
公开(公告)号：US20120178716A1
公开(公告)日：2012-07-12
申请号：US13311106
申请日：2011-12-05
申请人： Yihan Wang , Wei-Sheng Huang , Rajeswari Sundaramoorthi , Xiaotian Zhu , R. Mathew Thomas , William C. Shakespeare , David C. Dalgarno , Tomi K. Sawyer
发明人： Yihan Wang , Wei-Sheng Huang , Rajeswari Sundaramoorthi , Xiaotian Zhu , R. Mathew Thomas , William C. Shakespeare , David C. Dalgarno , Tomi K. Sawyer
IPC分类号： A61K31/675 , A61P35/00 , C07F9/6561 , A61K31/52 , C07D473/32
CPC分类号： C07F9/65616
摘要： This invention relates to compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.
摘要翻译：本发明涉及以下通式的化合物：其中可变基团如本文所定义，以及其制备和用途。

26. 发明授权

US08071609B2 Unsaturated heterocyclic derivatives 有权
标题翻译：不饱和杂环衍生物
公开(公告)号：US08071609B2
公开(公告)日：2011-12-06
申请号：US11990299
申请日：2006-08-11
申请人： Yihan Wang , Wei-Sheng Huang , Rajeswari Sundaramoorthi , Xiaotian Zhu , R. Mathew Thomas , William C. Shakespeare , David C. Dalgarno , Tomi K. Sawyer
发明人： Yihan Wang , Wei-Sheng Huang , Rajeswari Sundaramoorthi , Xiaotian Zhu , R. Mathew Thomas , William C. Shakespeare , David C. Dalgarno , Tomi K. Sawyer
IPC分类号： C07D473/16 , C07D473/34 , A61K31/52 , C07F9/6561 , C07D473/40 , A61P35/00
CPC分类号： C07F9/65616
摘要： This invention relates to compounds of the general formula: in which Q is an ethynyl or ethenyl moiety; Ring A is an aryl, heteroaryl or heterocyclic ring or ring system; and the remaining variable groups are as defined herein, and to their preparation and use.
摘要翻译：本发明涉及下列通式的化合物：其中Q是乙炔基或乙烯基部分; 环A是芳基，杂芳基或杂环或环系; 并且其余的可变基团如本文所定义，以及其制备和使用。

27. 发明申请

US20110294806A1 AZAINDOLE DERIVATIVES AS KINASE INHIBITORS 有权
标题翻译：亚胺衍生物作为激酶抑制剂
公开(公告)号：US20110294806A1
公开(公告)日：2011-12-01
申请号：US12998873
申请日：2009-12-11
申请人： Jiwei Qi , Yihan Wang , Feng Li , William C. Shakespeare , Anna Kohlmann , David C. Dalgarno , Xiaotian Zhu
发明人： Jiwei Qi , Yihan Wang , Feng Li , William C. Shakespeare , Anna Kohlmann , David C. Dalgarno , Xiaotian Zhu
IPC分类号： A61K31/437 , A61P35/00 , A61K31/506 , C07D471/04 , A61K31/5377
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。

28. 发明申请

US20060009453A1 Protein kinase modulators and method of use 有权
标题翻译：蛋白激酶调节剂及其使用方法
公开(公告)号：US20060009453A1
公开(公告)日：2006-01-12
申请号：US11126000
申请日：2005-05-09
申请人： Stephanie Geuns-Meyer , Brian Hodous , Stuart Chaffee , Paul Tempest , Philip Olivieri , Rebecca Johnson , Brian Albrecht , Vinod Patel , Victor Cee , Joseph Kim , Steven Bellon , Xiaotian Zhu , Yuan Cheng , Ning Xi , Karina Romero , Hanh Nguyen , Holly Deak
发明人： Stephanie Geuns-Meyer , Brian Hodous , Stuart Chaffee , Paul Tempest , Philip Olivieri , Rebecca Johnson , Brian Albrecht , Vinod Patel , Victor Cee , Joseph Kim , Steven Bellon , Xiaotian Zhu , Yuan Cheng , Ning Xi , Karina Romero , Hanh Nguyen , Holly Deak
IPC分类号： A61K31/53 , A61K31/506 , C07D43/14
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, H1-5 and R1-4 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，和合成中间体，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。

29. 发明申请

US20050209221A1 Substituted heterocyclic compounds and methods of use 失效
标题翻译：取代的杂环化合物及其使用方法
公开(公告)号：US20050209221A1
公开(公告)日：2005-09-22
申请号：US10875896
申请日：2004-06-23
申请人： Joseph Nunes , Xiaotian Zhu , Patricia Amouzegh , Chiara Ghiron , David Johnston , Eoin Power
发明人： Joseph Nunes , Xiaotian Zhu , Patricia Amouzegh , Chiara Ghiron , David Johnston , Eoin Power
IPC分类号： C07D213/82 , C07D239/46 , C07D239/48 , C07D417/02 , A61K31/4439 , A61K31/496 , A61K31/513 , A61K31/5377 , A61K31/541 , C07D413/02 , C07D43/02
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，斑秃，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括给予治疗有效量的上述化合物。

30. 发明授权

US06589758B1 Crystal of a kinase-ligand complex and methods of use 失效
标题翻译：激酶 - 配体复合物的晶体和使用方法
公开(公告)号：US06589758B1
公开(公告)日：2003-07-08
申请号：US09862154
申请日：2001-05-21
申请人： Xiaotian Zhu
发明人： Xiaotian Zhu
IPC分类号： C12Q148
CPC分类号： C12N9/1205 , C07K2299/00 , C12Q1/485
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 structural 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被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i）疾病的治疗或调节的治疗剂; 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。

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