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1. 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。

2. 发明申请

WO2009039397A2 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：WO2009039397A2
公开(公告)日：2009-03-26
申请号：PCT/US2008/077054
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. , KROFT, 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. , KROFT, Jeffrey E.
IPC分类号： C07D241/08 , C07D409/12 , A61K31/497 , A61P35/00
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

WO2008033854A1 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：WO2008033854A1
公开(公告)日：2008-03-20
申请号：PCT/US2007/078181
申请日：2007-09-11
申请人： CGI PHARMACEUTICALS, INC. , BLOMGREN, Peter A. , CURRIE, Kevin S. , KROPF, Jeffrey E. , LEE, Tony , DARROW, James W. , MITCHELL, Scott A. , XU, Jianjun , SCHMITT, Aaron C.
发明人： BLOMGREN, Peter A. , CURRIE, Kevin S. , KROPF, Jeffrey E. , LEE, Tony , DARROW, James W. , MITCHELL, Scott A. , XU, Jianjun , SCHMITT, Aaron C.
IPC分类号： C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , A61K31/444 , A61P29/00
CPC分类号： C07D213/64 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14
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：至少一种选自式（1）的化合物和其药学上可接受的盐，solvat

4. 发明申请

WO2008033834A1 PYRIMIDINES DERIVATIVES AND THEIR USE AS KINASE INHIBITORS 审中-公开
标题翻译：吡啶衍生物及其作为激酶抑制剂的用途
公开(公告)号：WO2008033834A1
公开(公告)日：2008-03-20
申请号：PCT/US2007/078154
申请日：2007-09-11
申请人： CGI PHARMACEUTICALS, INC. , CURRIE, Kevin S. , LEE, Tony , DARROW, James W. , BLOMGREN, Peter A.
发明人： CURRIE, Kevin S. , LEE, Tony , DARROW, James W. , BLOMGREN, Peter A.
IPC分类号： C07D239/42 , C07D401/12 , C07D403/12 , C07D409/12 , C07D409/14 , A61K31/505 , A61K31/506 , A61P35/00
CPC分类号： C07D239/42 , C07D401/12 , C07D403/12 , C07D409/12 , C07D409/14
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 Formula 1, 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。描述了包含至少一种式1的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。

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

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。

7. 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

8. 发明申请

WO2010068810A2 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：WO2010068810A2
公开(公告)日：2010-06-17
申请号：PCT/US2009/067575
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 , A61P35/00 , A61P35/02 , A61P19/08 , A61P29/00 , 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。

9. 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。

10. 发明申请

WO2006076592A1 1,3 SUBSTITUTED DIARYL UREAS AS MODULATORS OF KINASE ACTIVITY 审中-公开
标题翻译： 1,3作为激素的调节剂的替代性尿崩症
公开(公告)号：WO2006076592A1
公开(公告)日：2006-07-20
申请号：PCT/US2006/001271
申请日：2006-01-13
申请人： CGI PHARMACEUTICALS, INC. , MITCHELL, Scott A. , DANCA, Mihaela Diana , BLOMGREN, Peter A. , DESIMONE, Robert W. , PIPPIN, Douglas A. I.
发明人： MITCHELL, Scott A. , DANCA, Mihaela Diana , BLOMGREN, Peter A. , DESIMONE, Robert W. , PIPPIN, Douglas A. I.
IPC分类号： C07D401/04 , A61K31/4164 , A61P35/00
CPC分类号： C07D401/04 , C07D401/06
摘要： Certain chemical entities chosen from compounds of Formula 1 and pharmaceutically acceptable salts, solvates, crystal forms, chelates, non-covalent complexes, prodrugs, and mixtures thereof , are provided herein. Pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle chosen from carriers, adjuvants, and excipients, are also provided herein. Use in 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. 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
摘要翻译：本文提供了选自式1化合物的某些化学实体及其药学上可接受的盐，溶剂合物，结晶形式，螯合物，非共价复合物，前药及其混合物。本文还提供了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，其选自载体，佐剂和赋形剂。用于治疗患有对血管生成激酶调节有反应的某些疾病和病症的患者，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的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。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

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