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1. 发明申请

WO2008033857A3 SUBSTITUTED AMIDES, METHOD OF MAKING, AND METHOD OF USE THEREOF 审中-公开
标题翻译：取代的氨基，制备方法及其使用方法
公开(公告)号：WO2008033857A3
公开(公告)日：2008-06-05
申请号：PCT/US2007078185
申请日：2007-09-11
申请人： CGI PHARMACEUTICALS INC , BLOMGREN PETER A , LEE TONY , MITCHELL SCOTT A , XU JIANJUN , SCHMITT AARON C
发明人： BLOMGREN PETER A , LEE TONY , MITCHELL SCOTT A , XU JIANJUN , SCHMITT AARON C
IPC分类号： C07D401/12 , C07D413/12 , C07D417/12
CPC分类号： C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/12 , C07D417/12 , C07D417/14 , C07D513/04
摘要： At least one chemical entity chosen from compounds of Formula 1 and pharmaceutically acceptable salts, solvates, chelates, non-covalent complexes, prodrugs, and mixtures thereof is described herein. Pharmaceutical compositions comprising at least one chemical entity of the invention, 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：本文描述了至少一种选自式1化合物的化学实体及其可药用盐，溶剂合物，螯合物，非共价复合物，前药及其混合物。描述了包含本发明的至少一个化学实体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。

2. 发明申请

WO2009039397A3 SUBSTITUTED AMIDES, METHODS OF MAKING, USE THEREOF FOR THE TREATMENT OF DISEASES SUCH AS CANCER 审中-公开
标题翻译：替代药物，制备方法，用于治疗疾病等癌症
公开(公告)号：WO2009039397A3
公开(公告)日：2009-05-22
申请号：PCT/US2008077054
申请日：2008-09-19
申请人： CGI PHARMACEUTICALS INC , BLOMGREN PETER A , CURRIE KEVIN S , LEE SEUNG H , MITCHELL SCOTT A , XU JIANJUN , SCHMITT AARON C , ZHAO ZHONGDONG , ZHICHKIN PAVEL E , STAFFORD DOUGLAS G , KROPF JEFFREY E
发明人： BLOMGREN PETER A , CURRIE KEVIN S , LEE SEUNG H , MITCHELL SCOTT A , XU JIANJUN , SCHMITT AARON C , ZHAO ZHONGDONG , ZHICHKIN PAVEL E , STAFFORD DOUGLAS G , KROPF JEFFREY E
IPC分类号： C07D241/08 , A61K31/497 , A61P35/00 , C07D409/12
CPC分类号： C07D409/12 , C07D241/08
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。

3. 发明申请

WO2010068810A3 CERTAIN SUBSTITUTED AMIDES, METHOD OF MAKING, AND METHOD OF USE THEREOF 审中-公开
标题翻译：某些替代的制剂，制备方法及其使用方法
公开(公告)号：WO2010068810A3
公开(公告)日：2011-02-10
申请号：PCT/US2009067575
申请日：2009-12-10
申请人： CGI PHARMACEUTICALS INC , BLOMGREN PETER A , CURRIE KEVIN S , GENENTECH INC , MITCHELL SCOTT A , BRITTELLI DAVID R , SCHMITT AARON C , BARBOSA JR ANTONIO J
发明人： BLOMGREN PETER A , CURRIE KEVIN S , MITCHELL SCOTT A , BRITTELLI DAVID R , SCHMITT AARON C , BARBOSA JR ANTONIO J
IPC分类号： C07D487/04 , A61K31/53 , A61P19/08 , A61P29/00 , A61P35/00 , A61P35/02 , A61P37/08
CPC分类号： C07D487/04
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。

4. 发明申请

WO2008033858A3 KINASE INHIBITORS, AND METHODS OF USING AND IDENTIFYING KINASE INHIBITORS 审中-公开
标题翻译：激酶抑制剂和使用和鉴定激酶抑制剂的方法
公开(公告)号：WO2008033858A3
公开(公告)日：2008-10-16
申请号：PCT/US2007078186
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 , G01N33/68
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的磷酸化抑制BTK活性的方法，提供了通过抑制BTK的Y551的磷酸化，结合BTK的化学实体和抑制复合物来抑制BTK活性来治疗患者的方法。

5. 发明申请

WO2006099075A3 CERTAIN SUBSTITUTED AMIDES, METHOD OF MAKING, AND METHOD OF USE THEREOF 审中-公开
标题翻译：某些替代的制剂，制备方法及其使用方法
公开(公告)号：WO2006099075A3
公开(公告)日：2007-04-26
申请号：PCT/US2006008472
申请日：2006-03-09
申请人： CGI PHARMACEUTICALS INC , BRITTELLI DAVID R , CURRIE KEVIN S , DARROW JAMES W , KROPF JEFFREY E , LEE SEUNG H , GALLION STEVEN L , MITCHELL SCOTT A , PIPPIN DOUGLAS A I , BLOMGREN PETER A , STAFFORD DOUGLAS GREGORY
发明人： BRITTELLI DAVID R , CURRIE KEVIN S , DARROW JAMES W , KROPF JEFFREY E , LEE SEUNG H , GALLION STEVEN L , MITCHELL SCOTT A , PIPPIN DOUGLAS A I , BLOMGREN PETER A , STAFFORD DOUGLAS GREGORY
IPC分类号： C07D213/74 , A61K31/4412 , A61K31/4427 , A61K31/4965 , A61K31/497 , A61K31/4985 , C07D241/20 , C07D241/24 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D487/04
CPC分类号： C07D213/74 , C07D241/20 , C07D241/24 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D487/04
摘要： At least one chemical entity chosen from compounds of Formula (2) and pharmaceutically acceptable salts, solvates, chelates, non-covalent complexes, prodrugs, and mixtures thereof is described herein. Pharmaceutical compositions comprising at least one chemical entity of the invention, 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：本文描述了至少一种选自式（2）的化合物的化学实体及其药学上可接受的盐，溶剂合物，螯合物，非共价复合物，前药及其混合物。描述了包含本发明的至少一种化学实体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细胞活性的抑制作用的疾病的患者的方法。描述了确定样品中Btk的存在的方法。

6. 发明申请

WO2007024294A3 CERTAIN SUBSTITUTED UREAS, AS MODULATORS OF KINASE ACTIVITY 审中-公开
标题翻译：某些替代的UREAS，作为激酶的调节剂
公开(公告)号：WO2007024294A3
公开(公告)日：2007-05-31
申请号：PCT/US2006016916
申请日：2006-05-02
申请人： CGI PHARMACEUTICALS INC , MITCHELL SCOTT A , DANCA MIHAELA DIANA , BLOMGREN PETER , BRITTELLI DAVID , ZHICHKIN PAVEL , VOSS MATTHEW E
发明人： MITCHELL SCOTT A , DANCA MIHAELA DIANA , BLOMGREN PETER , BRITTELLI DAVID , ZHICHKIN PAVEL , VOSS MATTHEW E
IPC分类号： C07D401/06 , A61K31/437 , A61P35/00 , C07D471/04
CPC分类号： C07D471/04 , C07D401/06
摘要： Certain chemical entities chosen from compounds of Formula (1) and pharmaceutically acceptable salts, solvates, chelates, non-covalent complexes, and prodrugs thereof, are provided herein. Pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicles chosen from carriers, adjuvants, and excipients, are also provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to angiogenic kinase modulation, which comprise 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, including breast neoplasia, endometrial cancer, colon cancer, and neck squamous cell carcinoma. Methods of treatment include administering at least one chemical entity as a single active agent or administering such at least one chemical entity 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 at least one chemical entity 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：在本文中提供了选自式（1）的化合物的某些化学实体及其药学上可接受的盐，溶剂合物，螯合物，非共价复合物和前药。还提供了包含至少一种化学实体和一种或多种选自载体，佐剂和赋形剂的药学上可接受的载体的药物组合物。公开了治疗患有对血管生成激酶调节反应的某些疾病和病症的患者的方法，其包括向这些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，包括乳腺肿瘤，子宫内膜癌，结肠癌和颈部鳞状细胞癌。治疗方法包括给予至少一种化学实体作为单一活性剂或者与一种或多种其它治疗剂组合施用这样的至少一种化学实体。一种用于确定样品中存在或不存在血管生成激酶的方法，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至少一种化学实体接触确定样品中存在或不存在血管生成激酶。

7. 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。

8. 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。

9. 发明申请

WO2005047290A3 IMIDAZO[1,2-A] PYRAZIN-8-YLAMINES AS KINASE INHIBITORS 审中-公开
标题翻译：咪唑并[1,2-A]吡嗪-8-胺作为激酶抑制剂
公开(公告)号：WO2005047290A3
公开(公告)日：2005-08-11
申请号：PCT/US2004037433
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： A61K31/498 , C07D487/04 , A61K31/519 , A61P37/02
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。

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