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1. 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。

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

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。

4. 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。

5. 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。

6. 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。

7. 发明专利

JP2013028628A 1,3-diaryl substituted ureas as modulators of kinase activity 审中-公开
标题翻译：作为激酶活性调节剂的1,3-DIARYL替代尿素
公开(公告)号：JP2013028628A
公开(公告)日：2013-02-07
申请号：JP2012208429
申请日：2012-09-21
申请人： Cgi Pharmaceuticals Inc , シージーアイファーマシューティカルズ,インコーポレーテッド
发明人： MITCHELL SCOTT A , DANCA MIHAELA DIANA , BLOMGREN PETER A , DESIMONE ROBERT W , PIPPIN DOUGLAS A I , BRITTELLI DAVID R
IPC分类号： C07D401/06 , A61K31/4439 , A61K31/497 , A61K31/506 , A61K31/5377 , A61P3/10 , A61P7/04 , A61P9/10 , A61P9/14 , A61P15/00 , A61P15/08 , A61P15/12 , A61P17/06 , A61P19/02 , A61P25/16 , A61P25/28 , A61P27/02 , A61P29/00 , A61P31/04 , A61P35/00 , A61P35/02 , A61P37/06 , A61P43/00 , C07D401/14 , C07D405/14 , C07D417/14
CPC分类号： C07D401/14 , C07D401/06
摘要： PROBLEM TO BE SOLVED: To provide an effective substance for treating disease or disorder responsive to angiogenesis kinase activity modulation, for example, cancers such as breast neoplasia, endometrial cancer, colon cancer, and neck squamous cell carcinoma.SOLUTION: This invention relates to compounds of Formula 1 and pharmaceutically acceptable salts, solvates, crystal forms, chelates, non-covalent complexes, prodrugs, and mixtures thereof.
摘要翻译：要解决的问题：提供用于治疗对血管生成激酶活性调节有响应的疾病或病症的有效物质，例如癌症如乳腺肿瘤，子宫内膜癌，结肠癌和颈鳞状细胞癌。本发明涉及式1的化合物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。版权所有（C）2013，JPO＆INPIT

8. 发明专利

CA2661654C CERTAIN SUBSTITUTED AMIDES, METHOD OF MAKING, AND METHOD OF USE THEREOF 未知
公开(公告)号：CA2661654C
公开(公告)日：2016-10-11
申请号：CA2661654
申请日：2007-09-11
申请人： CGI PHARMACEUTICALS INC
发明人： BLOMGREN PETER A , CURRIE KEVIN S , KROPF JEFFREY E , LEE SEUNG H , DARROW JAMES W , MITCHELL SCOTT A , XU JIANJUN , SCHMITT AARON C
IPC分类号： C07D409/14 , A61K31/444 , A61P29/00 , C07D401/12
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.

9. 发明专利

CA2601628C CERTAIN SUBSTITUTED AMIDES, METHOD OF MAKING, AND METHOD OF USE THEREOF 未知
公开(公告)号：CA2601628C
公开(公告)日：2014-05-13
申请号：CA2601628
申请日：2006-03-09
申请人： CGI PHARMACEUTICALS INC
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
摘要： B-cell development, activiation, signaling and survival are all regulated in part by Bruton's Tyrosine Kinase (Btk). B-cells and Btk have a role in allergic disorders, autoimmune diesase, inflammatory disease, apoptosis and cancer. Inhibition of Btk by at least one chemical entity chosen from compounds of Formula 3 (see formula 3) and pharmaceutically acceptable salts, solvates, chelates, non-covalent complexes, prodrugs, and mixtures, can be useful in the treatment of diesases that involve Btk. 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 also described. Further, methods of treating patients suffering from certain diseases responsive to inhibition of Btk activity and/or B-cell activity and methods for determining the presence of Btk in a sample are provided.

10. 发明专利

ES2363269T3 AMIDAS SUSTITUIDAS, PROCEDIMIENTO DE PREPARACION Y PROCEDIMIENTO DE UTLIZACION DE LAS MISMAS. 未知
公开(公告)号：ES2363269T3
公开(公告)日：2011-07-28
申请号：ES07842267
申请日：2007-09-11
申请人： CGI PHARMACEUTICALS INC
发明人： BLOMGREN PETER A , LEE SEUNG H , MITCHELL SCOTT A , XU JIANJUN , SCHMITT AARON C
IPC分类号： C07D401/12
摘要： Compuesto seleccionado de entre compuestos de la fórmula 1: (fórmula 1) y profármacos, complejos no covalentes, quelatos, solvatos, sales farmacéuticamente aceptables, y mezclas de los mismos, en la que R se selecciona de entre arilo opcionalmente sustituido y heteroarilo opcionalmente sustituido; R4 se selecciona de entre hidrógeno, alquilo C1-C4 opcionalmente sustituido, alcoxilo C1-C4 opcionalmente sustituido, halógeno e hidroxilo; R21 y R22 se seleccionan independientemente de entre hidrógeno y alquilo C1-C4 opcionalmente sustituido; R16 se selecciona de entre hidrógeno, ciano, cicloalquilo opcionalmente sustituido y alquilo C1-C4 opcionalmente sustituido; A se selecciona de entre heteroarilo de 5 miembros opcionalmente sustituido, piridazinilo opcionalmente sustituido; pirimidinilo opcionalmente sustituido; y pirazinilo opcionalmente sustituido; L se selecciona de entre alquileno C0-C4 opcionalmente sustituido, -O-alquileno C0-C4 opcionalmente sustituido, -(alquileno C0-C4)(SO)-, -(alquileno C0-C4)(SO2)-; y -(alquileno C0-C4)(C=O)-; y G se selecciona de entre hidrógeno, halógeno, hidroxilo, alcoxilo, nitro, alquilo opcionalmente sustituido, amino opcionalmente sustituido, carbamimidoílo opcionalmente sustituido, heterocicloalquilo opcionalmente sustituido, cicloalquilo opcionalmente sustituido, arilo opcionalmente sustituido y heteroarilo opcionalmente sustituido. en el que los profármacos son acetato, formiato, y benzoato y derivados de grupos funcionales (tales como grupos amina o alcohol) en los compuestos de fórmula 1; en el que quelato indica una entidad química formada por la coordinación de un compuesto a un ion metálico en dos o más puntos; en el que complejo no covalente indica una entidad química formada por la interacción de un compuesto y otra molécula en el que no se forma un enlace covalente entre el compuesto y la molécula.

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