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1. 发明申请

WO2010068257A1 IMIDAZOPYRAZINE SYK INHIBITORS 审中-公开
标题翻译：咪唑吡嗪SYK抑制剂
公开(公告)号：WO2010068257A1
公开(公告)日：2010-06-17
申请号：PCT/US2009/006445
申请日：2009-12-07
申请人： CGI PHARMACEUTICALS, INC. , MITCHELL, Scott A. , CURRIE, Kevin S. , BLOMGREN, Peter A. , KROPF, Jeffrey E. , LEE, Seung H. , XU, Jianjun , STAFFORD, Douglas G. , HARDING, James P. , BARBOSA, Jr., Antonio J. , ZHAO, Zhongdong
发明人： MITCHELL, Scott A. , CURRIE, Kevin S. , BLOMGREN, Peter A. , KROPF, Jeffrey E. , LEE, Seung H. , XU, Jianjun , STAFFORD, Douglas G. , HARDING, James P. , BARBOSA, Jr., Antonio J. , ZHAO, Zhongdong
IPC分类号： A01N43/60 , A61K31/495
CPC分类号： C07D487/04 , A61K31/495 , C07D471/04 , C07D491/107 , C07D498/04 , C07D519/00 , C12Q1/485 , G01N33/573 , G01N2333/91205
摘要： Certain imidazopyrazines and pharmaceutical compositions thereof are provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are provided. Also provided are methods for determining the presence or absence of Syk kinase in a sample.
摘要翻译：本文提供了某些咪唑并嗪及其药物组合物。治疗患有某些对抑制Syk活性有作用的疾病和病症的患者的方法，其包括给予这些患者一定量的至少一种有效减少疾病或病症体征或症状的化学实体。还提供了用于确定样品中Syk激酶的存在或不存在的方法。

2. 发明申请

WO2009102468A1 6-ARYL-IMIDAZ0[L, 2-A] PYRAZINE DERIVATIVES, METHOD OF MAKING, AND METHOD OF USE THEREOF 审中-公开
标题翻译： 6-ARYL-IMIDAZO [L，2-A]吡嗪衍生物，制备方法及其使用方法
公开(公告)号：WO2009102468A1
公开(公告)日：2009-08-20
申请号：PCT/US2009/000919
申请日：2009-02-12
申请人： CGI PHARMACEUTICALS, INC. , MITCHELL, Scott A. , CURRIE, Kevin S. , BLOMGREN, Peter A. , ARMISTEAD, David M. , RAKER, Joseph
发明人： MITCHELL, Scott A. , CURRIE, Kevin S. , BLOMGREN, Peter A. , ARMISTEAD, David M. , RAKER, Joseph
IPC分类号： C07D487/04 , A61K31/4985 , A61P37/00
CPC分类号： C07D487/04
摘要： Certain chemical entities chosen from compounds represented by Formula I and pharmaceutically acceptable salts and mixtures thereof, are provided herein. Pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include cancer (e.g., B -cell lymphoma and leukemia), autoimmune diseases, inflammatory diseases, acute inflammatory reactions, and allergic disorders. Methods of treatment include administering at least one chemical entity as a single active agent or administering at least one chemical entity in combination with one or more other therapeutic agents. Also provided are methods for determining the presence or absence of Syk kinase in a sample. Formula I
摘要翻译：在本文中提供了选自由式I表示的化合物的某些化学实体及其药学上可接受的盐及其混合物。包含至少一种化学实体和一种或多种药学上可接受的载体的药物组合物。公开了治疗患有对抑制Syk活性有反应的某些疾病和病症的患者的方法，所述方法包括向所述患者施用一定量的至少一种有效减少疾病或病症体征或症状的化学实体。这些疾病包括癌症（例如，B细胞淋巴瘤和白血病），自身免疫疾病，炎性疾病，急性炎症反应和过敏性疾病。治疗方法包括给予至少一种化学实体作为单一活性剂或与一种或多种其它治疗剂组合施用至少一种化学实体。还提供了用于确定样品中Syk激酶的存在或不存在的方法。一级方程式

3. 发明申请

WO2005019220A9 SUBSTITUTED IMIDAZO[1,2-A]PYRAZINES AS MODULATORS OF KINASE ACTIVITY 审中-公开
标题翻译：取代的咪唑并[1,2-a]吡嗪类化合物作为激酶活性的调节剂
公开(公告)号：WO2005019220A9
公开(公告)日：2005-06-02
申请号：PCT/US2004025884
申请日：2004-08-11
申请人： CELLULAR GENOMICS INC , MITCHELL SCOTT A , DESIMONE ROBERT W , DARROW JAMES W , PIPPIN DOUGLAS A , DANCA M DIANA
发明人： MITCHELL SCOTT A , DESIMONE ROBERT W , DARROW JAMES W , PIPPIN DOUGLAS A , DANCA M DIANA
IPC分类号： A61K31/498 , A61P35/00 , C07D487/04 , A61K31/4985
CPC分类号： C07D487/04
摘要： Certain substituted imidazo[1,2-a]pyrazines and the pharmaceutically-acceptable salts thereof, are provided herein. Pharmaceutical compositions containing one or more compound of Formula I, or a pharmaceutically acceptable salt of such compounds, and one or more pharmaceutically acceptable carriers, excipients, or diluents, are also provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to EphB4 kinase modulation, which comprise administering to such patients an amount of a compound of Formula I effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include cancer, including breast neoplasia, endometrial cancer, colon cancer, and neck squamous cell carcinoma. Thus methods of treatment include administering a sufficient amount of a compound of the invention to decrease the symptoms or slow the progression of these diseases or disorders. Methods of treatment include administering a compound of Formula I as a single active agent or administering a compound of Formula I in combination with one or more other therapeutic agents. A method for determining the presence or absence of an angiogenic kinase in a sample comprising contacting the sample with a compound of Formula I under conditions that permit detection of activity of the angiogenic kinase, detecting a level of the activity of the angiogenic kinase, and therefrom determining the presence or absence of the angiogenic kinase in the sample.
摘要翻译：本文提供了某些取代的咪唑并[1,2-a]吡嗪及其药学上可接受的盐。本文还提供了含有一种或多种式I化合物或这些化合物的药学上可接受的盐以及一种或多种药学上可接受的载体，赋形剂或稀释剂的药物组合物。公开了治疗患有对EphB4激酶调节有响应的某些疾病和病症的患者的方法，其包括向所述患者施用有效减少疾病或病症的体征或症状的量的式I化合物。这些疾病包括癌症，包括乳腺瘤，子宫内膜癌，结肠癌和颈部鳞状细胞癌。因此治疗方法包括给予足够量的本发明化合物以减轻这些疾病或病症的症状或减缓其进展。治疗方法包括施用式I化合物作为单一活性剂或将式I化合物与一种或多种其他治疗剂组合施用。用于确定样品中血管生成激酶的存在或不存在的方法，包括在允许检测血管生成激酶活性，检测血管生成激酶活性水平的条件下使样品与式I化合物接触，并由此确定样品中血管生成激酶的存在或不存在。

4. 发明申请

WO2005047290A2 CERTAIN IMIDAZO[1,2-a]PYRAZIN-8-YLAMINES, METHOD OF MAKING, AND METHOD OF USE THEREOF 审中-公开
标题翻译：某些咪唑并[1,2-a]吡嗪-8-胺，其制备方法及其使用方法
公开(公告)号：WO2005047290A2
公开(公告)日：2005-05-26
申请号：PCT/US2004/037433
申请日：2004-11-10
申请人： CELLULAR GENOMICS INC. , CURRIE, Kevin, S. , DESIMONE, Robert, W. , PIPPIN, Douglas, A. , DARROW, James, W. , MITCHELL, Scott, A.
发明人： CURRIE, Kevin, S. , DESIMONE, Robert, W. , PIPPIN, Douglas, A. , DARROW, James, W. , MITCHELL, Scott, A.
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： At least one chemical entity chosen from compounds of Formula (1) and pharmaceutically acceptable pharmaceutically acceptable salts, hydrates, solvates, crystal forms, diastereomers, and prodrugs thereof. Methods of treating or preventing disorders in which aberrant kinase activity is implicated, pharmaceutical compositions, and methods for detecting the presence kinases in cells or biological preparations and for identifying kinases of therapeutic interest.
摘要翻译：至少一种选自式（1）化合物的化学实体及其药学上可接受的药学上可接受的盐，水合物，溶剂化物，晶体形式，非对映异构体和前药。治疗或预防涉及异常激酶活性的病症的方法，药物组合物和用于检测细胞或生物制剂中存在的激酶以及鉴定治疗感兴趣的激酶的方法。

5. 发明申请

WO2005019220A3 SUBSTITUTED IMIDAZO[1,2-A]PYRAZINES AS MODULATORS OF KINASE ACTIVITY 审中-公开
公开(公告)号：WO2005019220A3
公开(公告)日：2005-03-03
申请号：PCT/US2004/025884
申请日：2004-08-11
申请人： CELLULAR GENOMICS INC. , MITCHELL, Scott, A. , DESIMONE, Robert, W. , DARROW, James, W. , PIPPIN, Douglas, A. , DANCA, M. Diana
发明人： MITCHELL, Scott, A. , DESIMONE, Robert, W. , DARROW, James, W. , PIPPIN, Douglas, A. , DANCA, M. Diana
IPC分类号： C07D487/04
摘要： Certain substituted imidazo[1,2-a]pyrazines and the pharmaceutically-acceptable salts thereof, are provided herein. Pharmaceutical compositions containing one or more compound of Formula I, or a pharmaceutically acceptable salt of such compounds, and one or more pharmaceutically acceptable carriers, excipients, or diluents, are also provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to EphB4 kinase modulation, which comprise administering to such patients an amount of a compound of Formula I effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include cancer, including breast neoplasia, endometrial cancer, colon cancer, and neck squamous cell carcinoma. Thus methods of treatment include administering a sufficient amount of a compound of the invention to decrease the symptoms or slow the progression of these diseases or disorders. Methods of treatment include administering a compound of Formula I as a single active agent or administering a compound of Formula I in combination with one or more other therapeutic agents. A method for determining the presence or absence of an angiogenic kinase in a sample comprising contacting the sample with a compound of Formula I under conditions that permit detection of activity of the angiogenic kinase, detecting a level of the activity of the angiogenic kinase, and therefrom determining the presence or absence of the angiogenic kinase in the sample.

6. 发明申请

WO2011140488A1 PYRIDONE AND AZA-PYRIDONE COMPOUNDS AND METHODS OF USE 审中-公开
标题翻译：吡咯烷酮和AZA-吡咯烷酮化合物及其使用方法
公开(公告)号：WO2011140488A1
公开(公告)日：2011-11-10
申请号：PCT/US2011/035596
申请日：2011-05-06
申请人： GILEAD CONNECTICUT, INC. , GENENTECH, INC. , BARBOSA, Antonio, J., M. , BLOMGREN, Peter, A. , CURRIE, Kevin, S. , KRISHNAMOORTHY, Ravi , KROPF, Jeffrey, E. , LEE, Seung H. , MITCHELL, Scott A. , ORTWINE, Daniel , SCHMITT, Aaron, C. , WANG, Xiaojing , XU, Jianjun , YOUNG, Wendy , ZHANG, Honglu , ZHAO, Zhongdong , ZHICHKIN, Pavel E.
发明人： BARBOSA, Antonio, J., M. , BLOMGREN, Peter, A. , CURRIE, Kevin, S. , KRISHNAMOORTHY, Ravi , KROPF, Jeffrey, E. , LEE, Seung H. , MITCHELL, Scott A. , ORTWINE, Daniel , SCHMITT, Aaron, C. , WANG, Xiaojing , XU, Jianjun , YOUNG, Wendy , ZHANG, Honglu , ZHAO, Zhongdong , ZHICHKIN, Pavel E.
IPC分类号： C07D487/04 , C07D495/04 , C07D498/04 , A61K31/498 , A61P35/00
CPC分类号： C07D519/00 , A61K31/497 , A61K31/4985 , A61K31/501 , A61K31/5025 , A61K31/506 , A61K31/5377 , A61K31/5383 , A61K31/5386 , A61K31/551 , A61K45/06 , C07C69/65 , C07D209/52 , C07D471/14 , C07D487/04 , C07D495/04 , C07D498/04 , C07F5/04
摘要： Pyridone and aza-pyridone compounds of Formula I are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
摘要翻译：提供式I的吡啶酮和氮杂 - 吡啶酮化合物，包括其可用于抑制Btk激酶的立体异构体，互变异构体和其药学上可接受的盐，以及用于治疗免疫疾病如由Btk激酶介导的炎症。公开了使用式I化合物进行体外，原位和体内诊断以及哺乳动物细胞或相关病理条件中的这些疾病的治疗的方法。

7. 发明申请

WO2010068806A1 AMIDE DERIVATIVES AS BTK INHIBITORS IN THE TREATMENT OF ALLERGIC, AUTOIMMUNE AND INFLAMMATORY DISORDERS AS WELL AS CANCER 审中-公开
标题翻译：作为BTK抑制剂的AMID衍生物治疗过敏，自发性和炎症性疾病如癌症
公开(公告)号：WO2010068806A1
公开(公告)日：2010-06-17
申请号：PCT/US2009/067569
申请日：2009-12-10
申请人： CGI PHARMACEUTICALS, INC. , GENENTECH, INC. , BLOMGREN, Peter A. , CURRIE, Kevin S. , MITCHELL, Scott A. , BRITTELLI, David R.
发明人： BLOMGREN, Peter A. , CURRIE, Kevin S. , MITCHELL, Scott A. , BRITTELLI, David R.
IPC分类号： C07D401/14 , C07D403/14 , C07D409/14 , C07D471/04 , C07D487/04 , C07D491/04 , A61P35/00 , A61P37/00 , A61K31/4412 , A61K31/4188 , A61K31/53
CPC分类号： C07D401/14 , C07D409/14 , C07D471/04 , C07D487/04 , C07D498/04 , C07D519/00
摘要： Compounds of Formula I that inhibit Btk are described herein. Pharmaceutical compositions comprising at least one compound of Formula I, together with at least one pharmaceutically acceptable vehicle chosen from carriers, adjuvants, and excipients, are described. Methods of treating patients suffering from certain diseases responsive to inhibition of Btk activity and/ or B-cell activity are described. Methods for determining the presence of Btk in a sample are described.
摘要翻译：本文描述了抑制Btk的式I化合物。描述了包含至少一种式I化合物的药物组合物以及选自载体，佐剂和赋形剂的至少一种药学上可接受的载体。描述了治疗患有某些对Btk活性和/或B细胞活性的抑制作出反应的某些疾病的患者的方法。描述了确定样品中Btk的存在的方法。

8. 发明申请

WO2010068258A1 IMIDAZOPYRAZINE SYK INHIBITORS 审中-公开
标题翻译：咪唑并吡嗪SYK抑制剂
公开(公告)号：WO2010068258A1
公开(公告)日：2010-06-17
申请号：PCT/US2009/006446
申请日：2009-12-07
申请人： CGI PHARMACEUTICALS, INC. , MITCHELL, Scott A. , CURRIE, Kevin S. , BLOMGREN, Peter A. , KROPF, Jeffrey E. , LEE, Seung H. , XU, Jianjun , STAFFORD, Douglas G.
发明人： MITCHELL, Scott A. , CURRIE, Kevin S. , BLOMGREN, Peter A. , KROPF, Jeffrey E. , LEE, Seung H. , XU, Jianjun , STAFFORD, Douglas G.
IPC分类号： A61K31/535
CPC分类号： C07D519/00 , A61K9/0053 , C07D471/04 , C07D487/04 , G01N2333/9121
摘要： Certain imidazopyrazines and pharmaceutical compositions thereof are provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are provided. Also provided are methods for determining the presence or absence of Syk kinase in a sample.
摘要翻译：本文提供了某些咪唑并吡嗪及其药物组合物。提供了治疗患有抑制Syk活性的某些疾病和病症的患者的方法，该方法包括给予这些患者一定量的至少一种有效减少疾病或病症的体征或症状的化学实体。还提供了确定样品中Syk激酶存在或不存在的方法。

9. 发明申请

WO2008033858A2 KINASE INHIBITORS, AND METHODS OF USING AND IDENTIFYING KINASE INHIBITORS 审中-公开
标题翻译：激酶抑制剂，以及使用和鉴定激酶抑制剂的方法
公开(公告)号：WO2008033858A2
公开(公告)日：2008-03-20
申请号：PCT/US2007/078186
申请日：2007-09-11
申请人： CGI PHARMACEUTICALS, INC. , WHITNEY, James A. , DI PAOLO, Julie , VALLECA, Mark A. , BRITELLI, David R. , CURRIE, Kevin S. , DARROW, James W. , KROPF, Jeffrey E. , LEE, Tony , GALLION, Steven L. , MITCHELL, Scott A. , PIPPEN, Douglas A.I. , BLOMGREN, Peter A. , STAFFORD, Douglas Gregory
发明人： WHITNEY, James A. , DI PAOLO, Julie , VALLECA, Mark A. , BRITELLI, David R. , CURRIE, Kevin S. , DARROW, James W. , KROPF, Jeffrey E. , LEE, Tony , GALLION, Steven L. , MITCHELL, Scott A. , PIPPEN, Douglas A.I. , BLOMGREN, Peter A. , STAFFORD, Douglas Gregory
IPC分类号： A61K31/00 , A61K31/44 , A61K31/4965 , A61K31/497 , A61K31/4985 , A61K31/5377 , A61P43/00
CPC分类号： A61K31/00 , A61K31/44 , A61K31/4965 , A61K31/497 , A61K31/4985 , A61K31/5377 , C12Q1/485 , G01N2500/04
摘要： Methods of inhibiting BTK activity by inhibiting phosphorylation of Y551 of BTK, methods of treating patients by inhibiting BTK activity by inhibiting phosphorylation of Y551 of BTK, chemical entities that bind to BTK and inhibited complexes are provided.
摘要翻译：通过抑制BTK的Y551的磷酸化来抑制BTK活性的方法，通过抑制BTK的Y551的磷酸化来抑制BTK活性来治疗患者的方法，结合BTK和抑制的复合物的化学实体。 / p>

10. 发明申请

WO2005019220A2 SUBSTITUTED IMIDAZO[1,2-A]PYRAZINES AS MODULATORS OF KINASE ACTIVITY 审中-公开
标题翻译：取代的咪唑并[1,2-A]吡啶作为激酶活性的调节剂
公开(公告)号：WO2005019220A2
公开(公告)日：2005-03-03
申请号：PCT/US2004025884
申请日：2004-08-11
申请人： CELLULAR GENOMICS INC , MITCHELL SCOTT A , DESIMONE ROBERT W , DARROW JAMES W , PIPPIN DOUGLAS A , DANCA M DIANA
发明人： MITCHELL SCOTT A , DESIMONE ROBERT W , DARROW JAMES W , PIPPIN DOUGLAS A , DANCA M DIANA
IPC分类号： A61K31/498 , A61P35/00 , C07D487/04 , A61K31/4985
CPC分类号： C07D487/04
摘要： Certain substituted imidazo[1,2-a]pyrazines and the pharmaceutically-acceptable salts thereof, are provided herein. Pharmaceutical compositions containing one or more compound of Formula I, or a pharmaceutically acceptable salt of such compounds, and one or more pharmaceutically acceptable carriers, excipients, or diluents, are also provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to EphB4 kinase modulation, which comprise administering to such patients an amount of a compound of Formula I effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include cancer, including breast neoplasia, endometrial cancer, colon cancer, and neck squamous cell carcinoma. Thus methods of treatment include administering a sufficient amount of a compound of the invention to decrease the symptoms or slow the progression of these diseases or disorders. Methods of treatment include administering a compound of Formula I as a single active agent or administering a compound of Formula I in combination with one or more other therapeutic agents. A method for determining the presence or absence of an angiogenic kinase in a sample comprising contacting the sample with a compound of Formula I under conditions that permit detection of activity of the angiogenic kinase, detecting a level of the activity of the angiogenic kinase, and therefrom determining the presence or absence of the angiogenic kinase in the sample.
摘要翻译：本文提供了某些取代的咪唑并[1,2-a]吡嗪及其药学上可接受的盐。本文还提供了含有一种或多种式I化合物或这些化合物的药学上可接受的盐以及一种或多种药学上可接受的载体，赋形剂或稀释剂的药物组合物。公开了治疗患有某些对EphB4激酶调节作用的疾病和病症的患者的方法，其包括给予这样的患者一定量的有效降低疾病或病症体征或症状的式I化合物。这些疾病包括癌症，包括乳腺肿瘤，子宫内膜癌，结肠癌和颈部鳞状细胞癌。因此，治疗方法包括施用足量的本发明化合物以减少症状或减缓这些疾病或病症的进展。治疗方法包括给予式I化合物作为单一活性剂或将一种式I化合物与一种或多种其它治疗剂联合给药。一种用于确定样品中血管生成激酶存在或不存在的方法，包括在允许检测血管生成激酶活性，检测血管生成激酶活性水平的条件下将样品与式I化合物接触确定样品中存在或不存在血管生成激酶。

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