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1. 发明申请

WO2009143246A3 ARYLSULFONAMIDE COMPOUNDS, COMPOSITIONS AND METHODS OF USE 审中-公开
标题翻译：芳香酰胺化合物，组合物和使用方法
公开(公告)号：WO2009143246A3
公开(公告)日：2010-04-29
申请号：PCT/US2009044680
申请日：2009-05-20
申请人： GENENTECH INC , INST MEDICAL W & E HALL , BAELL JONATHAN , LESSENE GUILLAUME LAURENT , SLEEBS BRAD EDMUND , FAIRBROTHER WAYNE , FLYGARE WAYNE , KOEHLER MICHAEL
发明人： BAELL JONATHAN , LESSENE GUILLAUME LAURENT , SLEEBS BRAD EDMUND , FAIRBROTHER WAYNE , FLYGARE WAYNE , KOEHLER MICHAEL
IPC分类号： C07D215/38 , A61K31/517 , A61P35/02
CPC分类号： C07D215/38
摘要： Disclosed are compounds which inhibit the activity of anti-apoptotic protein family members, compositions containing the compounds and uses of the compounds for preparing medicaments for treating diseases during which occurs expression one or more than one of an anti apoptotic protein family member.
摘要翻译：公开了抑制抗凋亡蛋白家族成员的活性的化合物，含有该化合物的组合物和该化合物用于制备治疗疾病的药物的用途，其中发生表达一种或多种抗凋亡蛋白家族成员。

2. 发明申请

WO2008061208A3 ARYLSULFONAMIDE COMPOUNDS 审中-公开
标题翻译：芳香酰胺化合物
公开(公告)号：WO2008061208A3
公开(公告)日：2008-07-03
申请号：PCT/US2007084873
申请日：2007-11-15
申请人： GENENTECH INC , INST MEDICAL W & E HALL , BAELL JONATHAN BAYLDON , LESSENE GUILLAUME LAURENT , SLEEBS BRAD EDMUND , FAIRBROTHER WAYNE J , FLYGARE JOHN A , KOEHLER MICHAEL F T
发明人： BAELL JONATHAN BAYLDON , LESSENE GUILLAUME LAURENT , SLEEBS BRAD EDMUND , FAIRBROTHER WAYNE J , FLYGARE JOHN A , KOEHLER MICHAEL F T
IPC分类号： C07D239/94 , A61K31/517 , A61P43/00
CPC分类号： C07D239/94
摘要： The invention relates generally to small molecules that mimic the biological activity of certain peptides and proteins, to compositions containing them and to their use. In particular, the invention relates to compounds of the general formula (I) that mimic the biological activity of BH3-only proteins and are capable of binding to and neutralising prosurvival Bcl-2 proteins: wherein A 1 , A 2 , B 1, B 2 , B 3 , X, Z, R 1 , R 2 , R 3 and t are as described herein. The invention also relates to processes of preparing the benzenesulfonamide compounds that mimic portions of peptides and proteins, and to the use of such compounds in the regulation of cell death and the treatment and/or prophylaxis of diseases or conditions associated with the deregulation of cell death.
摘要翻译：本发明一般涉及模拟某些肽和蛋白质的生物学活性的小分子，含有它们的组合物及其用途。特别地，本发明涉及模拟仅含BH3蛋白的生物学活性的通式（I）的化合物，并且能够结合并中和前病毒Bcl-2蛋白：其中A 1， B 1，B 2，B 3，X 3，Z 1，R 2， R 2，R 3和R 3如本文所述。本发明还涉及制备模仿肽和蛋白质的一部分的苯磺酰胺化合物的方法，以及这些化合物在调节细胞死亡中的用途以及治疗和/或预防与细胞死亡调节相关的疾病或病症。

3. 发明申请

WO2010080478A1 COMPOUNDS AND METHODS OF USE 审中-公开
标题翻译：化合物和使用方法
公开(公告)号：WO2010080478A1
公开(公告)日：2010-07-15
申请号：PCT/US2009/068400
申请日：2009-12-17
申请人： GENENTECH, INC. , THE WALTER AND ELIZA HALL INSTITUTE OF MEDICAL RESEARCH , ABBOTT LABORATORIES , BAELL, Jonathon, Bayldon , BUI, Chinh, Thien , COLMAN, Peter , DUDLEY, Danette, A. , FAIRBROTHER, Wayne, J. , FLYGARE, John, A. , LASSENE, Guillaume, Laurent , NDUBAKU, Chudi , NIKOLAKOPOULOS, George , RYE, Carl, Steven , SLEEBS, Brad, Edmund , SMITH, Brian, John , WATSON, Keith, Geoffrey , ELMORE, Steven, W. , PETROS, Andrew, M. , SOUERS, Andrew, J.
发明人： BAELL, Jonathon, Bayldon , BUI, Chinh, Thien , COLMAN, Peter , DUDLEY, Danette, A. , FAIRBROTHER, Wayne, J. , FLYGARE, John, A. , LASSENE, Guillaume, Laurent , NDUBAKU, Chudi , NIKOLAKOPOULOS, George , RYE, Carl, Steven , SLEEBS, Brad, Edmund , SMITH, Brian, John , WATSON, Keith, Geoffrey , ELMORE, Steven, W. , PETROS, Andrew, M. , SOUERS, Andrew, J.
IPC分类号： A61K31/535
CPC分类号： C07D417/14 , C07D417/12 , C07D487/04
摘要： In one aspect, the present invention provides for a compound of Formula (I) in which, the variables X 1 , X 2a , X 2b , X 2c , R 1 , B, L, E, A and the subscript n are as defined herein. In another aspect, the present invention provides for pharmaceutical compositions comprising compounds of Formula (I) as well as methods for using compounds of Formula (I) for the treatment of diseases and conditions (e.g., cancer, thrombocythemia, etc) characterized by the expression or over-expression of Bcl-2 anti-apoptotic proteins, e.g., of anti-apoptotic Bcl-x L proteins.
摘要翻译：一方面，本发明提供式（I）的化合物，其中变量X1，X2a，X2b，X2c，R1，B，L，E，A和下标n如本文所定义。在另一方面，本发明提供包含式（I）化合物的药物组合物以及使用式（I）化合物治疗由表达特征的疾病和病症（例如癌症，血小板增多症等）的方法或过度表达Bcl-2抗凋亡蛋白，例如抗凋亡Bcl-xL蛋白。

4. 发明申请

WO2009143246A2 ARYLSULFONAMIDE COMPOUNDS, COMPOSITIONS AND METHODS OF USE 审中-公开
标题翻译：芳香酰胺化合物，组合物和使用方法
公开(公告)号：WO2009143246A2
公开(公告)日：2009-11-26
申请号：PCT/US2009/044680
申请日：2009-05-20
申请人： GENENTECH, INC. , THE WALTER AND ELIZA HALL INSTITUTE OF MEDICAL RESEARCH , BAELL, Jonathan , LESSENE, Guillaume, Laurent , SLEEBS, Brad, Edmund , FAIRBROTHER, Wayne , FLYGARE, Wayne , KOEHLER, Michael
发明人： BAELL, Jonathan , LESSENE, Guillaume, Laurent , SLEEBS, Brad, Edmund , FAIRBROTHER, Wayne , FLYGARE, Wayne , KOEHLER, Michael
IPC分类号： C07D215/38
CPC分类号： C07D215/38
摘要： Disclosed are compounds which inhibit the activity of anti-apoptotic protein family members, compositions containing the compounds and uses of the compounds for preparing medicaments for treating diseases during which occurs expression one or more than one of an anti apoptotic protein family member.
摘要翻译：公开了抑制抗凋亡蛋白家族成员的活性的化合物，含有该化合物的组合物和该化合物用于制备用于治疗疾病的药物的用途，其中发生表达一种或多种抗凋亡蛋白家族成员。

5. 发明申请

WO2008061208A2 ARYLSULFONAMIDE COMPOUNDS 审中-公开
标题翻译：芳基磺酰胺化合物
公开(公告)号：WO2008061208A2
公开(公告)日：2008-05-22
申请号：PCT/US2007/084873
申请日：2007-11-15
申请人： GENENTECH, INC. , WALTER AND ELIZA HALL INSTITUTE OF MEDICAL RESEARCH , BAELL, Jonathan Bayldon , LESSENE, Guillaume Laurent , SLEEBS, Brad Edmund , FAIRBROTHER, Wayne J. , FLYGARE, John A. , KOEHLER, Michael F. T.
发明人： BAELL, Jonathan Bayldon , LESSENE, Guillaume Laurent , SLEEBS, Brad Edmund , FAIRBROTHER, Wayne J. , FLYGARE, John A. , KOEHLER, Michael F. T.
IPC分类号： C07D239/94 , A61K31/517 , A61P43/00
CPC分类号： C07D239/94
摘要： The invention relates generally to small molecules that mimic the biological activity of certain peptides and proteins, to compositions containing them and to their use. In particular, the invention relates to compounds of the general formula (I) that mimic the biological activity of BH3-only proteins and are capable of binding to and neutralising prosurvival Bcl-2 proteins: wherein A 1 , A 2 , B 1, B 2 , B 3 , X, Z, R 1 , R 2 , R 3 and t are as described herein. The invention also relates to processes of preparing the benzenesulfonamide compounds that mimic portions of peptides and proteins, and to the use of such compounds in the regulation of cell death and the treatment and/or prophylaxis of diseases or conditions associated with the deregulation of cell death.
摘要翻译：本发明一般涉及模拟某些肽和蛋白质的生物活性的小分子，含有它们的组合物及其用途。具体而言，本发明涉及模拟仅BH3蛋白的生物学活性并能够结合并中和促存活Bcl-2蛋白的通式（I）的化合物：其中A 1， A 2，B 1，B 2，B 3，X，Z，R 1，B 1，B 2，B 3， R 2，R 3和t如本文所述。本发明还涉及制备模拟肽和蛋白质部分的苯磺酰胺化合物的方法，并涉及这些化合物在调节细胞死亡以及治疗和/或预防与细胞死亡失调相关的疾病或病症中的用途

6. 发明申请

WO2012131297A1 PYRIDO [3',2' :4,5] THIENO [3, 2-D] PYRIMIDIN- 4 - YLAMINE DERIVATIVES AND THEIR THERAPEUTICAL USE 审中-公开
标题翻译：吡咯并[3'，2'：4,5]噻吩并[3,2-D]嘧啶-4-基氨基衍生物及其治疗用途
公开(公告)号：WO2012131297A1
公开(公告)日：2012-10-04
申请号：PCT/GB2012/000280
申请日：2012-03-27
申请人： BAELL, Jonathan Bayldon , STREET, Ian Philip , SLEEBS, Brad Edmund
发明人： BAELL, Jonathan Bayldon , STREET, Ian Philip , SLEEBS, Brad Edmund
IPC分类号： C07D495/04 , A61K31/519 , A61P25/00 , A61P35/00 , A61P29/00 , A61P3/00
CPC分类号： C07D495/04
摘要： The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain fused triaryl amine compounds of the following formula (for convenience, collectively referred to herein as "FTA compounds"), which, inter alia , inhibit LIM kinase (LIMK) activity. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit LIMK activity, and in the treatment of diseases and conditions that are mediated by LIMK, that are ameliorated by the inhibition of LIMK activity, etc., including proliferative conditions such as cancer (e.g., breast cancer, prostate cancer, melanoma, glioma, etc.), as well as vasodilation (including, e.g., hypertension, angina, cerebral vasospasm, and ischemia following subarachnoid hemorrhage), neurodegenerative disorders, atherosclerosis, fibrosis, and inflammatory diseases (including, e.g., Crohn's disease and chronic obstructive pulmonary disease (COPD)), and glaucoma (also known as ocular hypertension).
摘要翻译：本发明一般涉及治疗化合物领域，更具体地涉及以下式的某些稠合三芳基胺化合物（为了方便起见，本文统称为“FTA化合物”），其特别地抑制LIM激酶（LIMK ）活动。本发明还涉及包含这些化合物的药物组合物，以及这些化合物和组合物在体外和体内的用途，以抑制LIMK活性，以及治疗由LIMK介导的疾病和病症，其被改善通过抑制LIMK活性等，包括增殖条件如癌症（例如乳腺癌，前列腺癌，黑素瘤，神经胶质瘤等），以及血管舒张（包括例如高血压，心绞痛，脑血管痉挛和蛛网膜下腔出血后的缺血），神经变性疾病，动脉粥样硬化，纤维化和炎性疾病（包括例如克罗恩病和慢性阻塞性肺病（COPD））和青光眼（也称为高眼压症）。

7. 发明申请

WO2010080503A1 HETEROCYCLIC COMPOUNDS AND METHODS OF USE 审中-公开
标题翻译：杂环化合物和使用方法
公开(公告)号：WO2010080503A1
公开(公告)日：2010-07-15
申请号：PCT/US2009/068496
申请日：2009-12-17
申请人： GENENTECH, INC. , THE WALTER AND ELIZA HALL INSTITUTE OF MEDICAL RESEARCH , ABBOTT LABORATORIES , BAELL, Jonathon, Bayldon , BUI, Chinh, Thien , COLMAN, Peter , CZABOTAR, Peter , DUDLEY, Danette, A. , FAIRBROTHER, Wayne, J. , FLYGARE, John, A. , LASSENE, Guillaume, Laurent , NDUBAKU, Chudi , NIKOLAKOPOULOS, George , SLEEBS, Brad, Edmund , SMITH, Brian, John , WATSON, Keith, Geoffrey , ELMORE, Steven, W. , HASVOLD, Lisa, A. , PETROS, Andrew, M. , SOUERS, Andrew, J. , TAO, Zhi-Fu , WANG, Le , WANG, Xilu , DESHAYES, Kurt
发明人： BAELL, Jonathon, Bayldon , BUI, Chinh, Thien , COLMAN, Peter , CZABOTAR, Peter , DUDLEY, Danette, A. , FAIRBROTHER, Wayne, J. , FLYGARE, John, A. , LASSENE, Guillaume, Laurent , NDUBAKU, Chudi , NIKOLAKOPOULOS, George , SLEEBS, Brad, Edmund , SMITH, Brian, John , WATSON, Keith, Geoffrey , ELMORE, Steven, W. , HASVOLD, Lisa, A. , PETROS, Andrew, M. , SOUERS, Andrew, J. , TAO, Zhi-Fu , WANG, Le , WANG, Xilu , DESHAYES, Kurt
IPC分类号： A01N43/00
CPC分类号： C07D417/14 , C07D471/06 , C07D473/00 , C07D487/04 , C07D495/04 , C07D513/04 , C07D513/06
摘要： In one aspect, the present invention provides for a compound of Formula I; in which the variable X 1a , X 1b , X 1c , X 1d , Q, A, R 1 , B, L, E, and the subscripts m and n have the meanings as described herein. In another aspect, the present invention provides for pharmaceutical compositions comprising compounds of Formula I as well as methods for using compounds of Formula I for the treatment of diseases and conditions (e.g., cancer, thrombocythemia, etc) characterized by the expression or over-expression of Bcl-2 anti-apoptotic proteins, e.g., of anti-apoptotic Bcl-x L proteins.
摘要翻译：一方面，本发明提供式I的化合物; 其中变量X1a，X1b，X1c，X1d，Q，A，R1，B，L，E和下标m和n具有如本文所述的含义。另一方面，本发明提供包含式I化合物的药物组合物以及使用式I化合物治疗以表达或过表达为特征的疾病和病症（例如癌症，血小板增多症等）的方法的Bcl-2抗凋亡蛋白，例如抗凋亡Bcl-xL蛋白。

8. 发明申请

WO2009039553A1 BENZOTHIAZOLE COMPOUNDS 审中-公开
标题翻译：苯并噻唑化合物
公开(公告)号：WO2009039553A1
公开(公告)日：2009-04-02
申请号：PCT/AU2007/001442
申请日：2007-09-27
申请人： THE WALTER AND ELIZA HALL INSTITUTE OF MEDICAL RESEARCH , WATSON, Keith Geoffrey , LESSENE, Guillaume Laurent , BAELL, Jonathan Bayldon , HUANG, David Ching Siang , STREET, Ian Philip , ADAMS, Jerry McKee , COLMAN, Peter Malcolm , SLEEBS, Brad Edmund , SMITH, Brian John , CZABOTAR, Peter Edward
发明人： WATSON, Keith Geoffrey , LESSENE, Guillaume Laurent , BAELL, Jonathan Bayldon , HUANG, David Ching Siang , STREET, Ian Philip , ADAMS, Jerry McKee , COLMAN, Peter Malcolm , SLEEBS, Brad Edmund , SMITH, Brian John , CZABOTAR, Peter Edward
IPC分类号： C07D277/82 , C07D417/12 , C07D417/14 , A61P19/02 , A61P35/02 , A61K31/428 , A61P29/00 , A61P37/06
CPC分类号： C07D417/12 , C07D277/82 , C07D417/14
摘要： The present invention relates to benzothiazole compounds that mimic the activity of BH3 only proteins and are capable of binding to and neutralizing pro survival Bcl 2 proteins. The invention also relates to the use of such compounds in the regulation of cell death or cell survival and the treatment and/or prophylaxis of diseases or conditions associated with the deregulation of cell death or cell survival.
摘要翻译：本发明涉及苯并噻唑化合物，其类似于仅BH3蛋白的活性并且能够结合和中和生存的Bcl 2蛋白。本发明还涉及这些化合物在调节细胞死亡或细胞存活以及治疗和/或预防与细胞死亡或细胞存活失调相关的疾病或病症中的用途。

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