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1. 发明申请

WO2008024724A1 AZA-BENZOTHIOPHENYL COMPOUNDS AND METHODS OF USE 审中-公开
标题翻译： AZA-BENZOTHOPHENYL化合物及其使用方法
公开(公告)号：WO2008024724A1
公开(公告)日：2008-02-28
申请号：PCT/US2007/076340
申请日：2007-08-20
申请人： GENENTECH, INC. , PRICE, Stephen , WILLIAMS, Karen , SAVY, Pascal Pierre , DYKE, Hazel Joan , MONTANA, John Gary , STANLEY, Mark S. , BAO, Liang
发明人： PRICE, Stephen , WILLIAMS, Karen , SAVY, Pascal Pierre , DYKE, Hazel Joan , MONTANA, John Gary , STANLEY, Mark S. , BAO, Liang
IPC分类号： C07D495/04 , A61K31/4743 , A61P35/00 , A61P29/00
CPC分类号： C07D495/04
摘要： The invention relates to azabenzothiophenyl compounds of Formula (I) with anti-cancer and/or anti-inflammatory activity and more specifically to azabenzothiophenyl compounds which inhibit MEK kinase activity. The invention provides compositions and methods useful for inhibiting abnormal cell growth or treating a hyperproliferative disorder, or treating an inflammatory disease in a mammal. The invention also relates to methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.
摘要翻译：本发明涉及具有抗癌和/或抗炎活性的式（I）的氮杂苯并噻吩基化合物，更具体地涉及抑制MEK激酶活性的氮杂苯并噻吩基化合物。本发明提供了可用于抑制异常细胞生长或治疗过度增殖性疾病或治疗哺乳动物炎性疾病的组合物和方法。本发明还涉及将化合物用于体外，原位和体内诊断或治疗哺乳动物细胞或相关病理状况的方法。

2. 发明申请

WO2008067481A1 AZA-INDOLYL COMPOUNDS AND METHODS OF USE 审中-公开
标题翻译： AZA-INDOLYL化合物及其使用方法
公开(公告)号：WO2008067481A1
公开(公告)日：2008-06-05
申请号：PCT/US2007/085962
申请日：2007-11-29
申请人： GENENTECH, INC. , GOODACRE, Simon Charles , WILLIAMS, Karen , PRICE, Stephen , DYKE, Hazel Joan , MONTANA, John Gary , STANLEY, Mark S. , BAO, Liang , LEE, Wendy
发明人： GOODACRE, Simon Charles , WILLIAMS, Karen , PRICE, Stephen , DYKE, Hazel Joan , MONTANA, John Gary , STANLEY, Mark S. , BAO, Liang , LEE, Wendy
IPC分类号： C07D471/04 , C07D487/04 , A61K31/407 , A61P29/00 , A61P35/00
CPC分类号： C07D471/04 , C07D487/04
摘要： The invention relates to azaindolyl compounds of Formula I with anti-cancer and/or anti-inflammatory activity and more specifically to azaindolyl compounds which inhibit MEK kinase activity. The invention provides compositions and methods useful for inhibiting abnormal cell growth or treating a hyperproliferative disorder, or treating an inflammatory disease in a mammal. The invention also relates to methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.
摘要翻译：本发明涉及具有抗癌和/或抗炎活性的具有式I的唑烷基化合物，更具体地涉及抑制MEK激酶活性的唑烷基化合物。本发明提供了可用于抑制异常细胞生长或治疗过度增殖性疾病或治疗哺乳动物炎性疾病的组合物和方法。本发明还涉及将化合物用于体外，原位和体内诊断或治疗哺乳动物细胞或相关病理状况的方法。

3. 发明申请

WO2008024725A1 AZA-BENZOFURANYL COMPOUNDS AND METHODS OF USE 审中-公开
标题翻译： AZA-BENZOFURANYL化合物及其使用方法
公开(公告)号：WO2008024725A1
公开(公告)日：2008-02-28
申请号：PCT/US2007/076344
申请日：2007-08-20
申请人： GENENTECH, INC. , PRICE, Stephen , WILLIAMS, Karen , SAVY, Pierre Pascal , DYKE, Hazel Joan , MONTANA, John Gary , STANLEY, Mark S. , BAO, Liang
发明人： PRICE, Stephen , WILLIAMS, Karen , SAVY, Pierre Pascal , DYKE, Hazel Joan , MONTANA, John Gary , STANLEY, Mark S. , BAO, Liang
IPC分类号： C07D491/048 , A61K31/4355 , A61K31/5025 , A61K31/519 , A61P35/00 , A61P29/00
CPC分类号： C07D491/048
摘要： The invention relates to azabenzofuranyl compounds of Formula (I) with anti-cancer and/or anti-inflammatory activity and more specifically to azabenzofuranyl compounds which inhibit MEK kinase activity. The invention provides compositions and methods useful for inhibiting abnormal cell growth or treating a hyperproliferative disorder, or treating an inflammatory disease in a mammal. The invention also relates to methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.
摘要翻译：本发明涉及具有抗癌和/或抗炎活性的式（I）的氮杂苯并呋喃基化合物，更具体地涉及抑制MEK激酶活性的氮杂苯并呋喃基化合物。本发明提供了可用于抑制异常细胞生长或治疗过度增殖性疾病或治疗哺乳动物炎性疾病的组合物和方法。本发明还涉及将化合物用于体外，原位和体内诊断或治疗哺乳动物细胞或相关病理状况的方法。

4. 发明申请

WO2008157179A3 N-SUBSTITUTED AZAINDOLES AND METHODS OF USE 审中-公开
公开(公告)号：WO2008157179A3
公开(公告)日：2008-12-24
申请号：PCT/US2008/066570
申请日：2008-06-11
申请人： GENENTECH, INC. , DYKE, Hazel Joan , PRICE, Stephen , WILLIAMS, Karen
发明人： DYKE, Hazel Joan , PRICE, Stephen , WILLIAMS, Karen
IPC分类号： C07D471/04 , A61K31/437 , A61P35/00 , A61P37/00
摘要： The invention relates to N-substituted azaindolyl compounds of Formula I with anti-cancer and/or anti-inflammatory activity and more specifically to N-substituted azaindolyl compounds which inhibit MEK kinase activity. The invention provides compositions and methods useful for inhibiting abnormal cell growth or treating a hyperproliferative disorder, or treating an inflammatory disease in a mammal. The invention also relates to methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.

5. 发明申请

WO2010003025A1 BICYCLIC HETEROCYCLES AS MEK KINASE INHIBITORS 审中-公开
标题翻译：双相异构体作为MEK激酶抑制剂
公开(公告)号：WO2010003025A1
公开(公告)日：2010-01-07
申请号：PCT/US2009/049453
申请日：2009-07-01
申请人： GENENTECH, INC. , HEALD, Robert, Andrew , JACKSON, Philip , LYSSIKATOS, Joseph , PRICE, Stephen , SAVY, Pascal, Pierre
发明人： HEALD, Robert, Andrew , JACKSON, Philip , LYSSIKATOS, Joseph , PRICE, Stephen , SAVY, Pascal, Pierre
IPC分类号： C07D231/56 , C07D275/04 , C07D403/12 , C07D405/12 , C07D471/04 , A61K31/437 , A61P35/00
CPC分类号： C07D231/56 , C07D275/04 , C07D403/12 , C07D405/12 , C07D471/04
摘要： The invention relates to bicyclic heterocycles of formulae I and II with anti-cancer and/or anti-inflammatory activity and more specifically with MEK kinase inhibitory activity. The invention provides compositions and methods useful for inhibiting abnormal cell growth, treating a hyperproliferative disorder, or treating an inflammatory disease in a mammal. The invention also relates to methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.
摘要翻译：本发明涉及式I和II的双环杂环，其具有抗癌和/或抗炎活性，更具体地涉及MEK激酶抑制活性。本发明提供了可用于抑制异常细胞生长，治疗过度增殖性疾病或治疗哺乳动物炎性疾病的组合物和方法。本发明还涉及将化合物用于体外，原位和体内诊断或治疗哺乳动物细胞或相关病理状况的方法。

6. 发明申请

WO2010138589A1 BICYCLIC PYRIMIDINE PI3K INHIBITOR COMPOUNDS SELECTIVE FOR P110 DELTA, AND METHODS OF USE 审中-公开
标题翻译： PI10K PI3K抑制剂PI3K抑制剂化合物的选择性及其使用方法
公开(公告)号：WO2010138589A1
公开(公告)日：2010-12-02
申请号：PCT/US2010/036199
申请日：2010-05-26
申请人： GENENTECH, INC. , F. HOFFMANN-LA ROCHE AG , CASTANEDO, Georgette , CHAN, Bryan , GOLDSTEIN, David Michael , KONDRU, Rama K. , LUCAS, Matthew C. , PALMER, Wylie Solang , PRICE, Stephen , SAFINA, Brian , SAVY, Pascal Pierre Alexandre , SEWARD, Eileen Mary , SUTHERLIN, Daniel P. , SWEENEY, Zachary Kevin
发明人： CASTANEDO, Georgette , CHAN, Bryan , GOLDSTEIN, David Michael , KONDRU, Rama K. , LUCAS, Matthew C. , PALMER, Wylie Solang , PRICE, Stephen , SAFINA, Brian , SAVY, Pascal Pierre Alexandre , SEWARD, Eileen Mary , SUTHERLIN, Daniel P. , SWEENEY, Zachary Kevin
IPC分类号： C07D487/04 , C07D491/04 , C07D513/04 , A61K31/519 , A61P35/00 , A61P9/00 , A61P29/00 , A61P25/00
CPC分类号： C07D513/04 , C07D487/04 , C07D491/04 , C07D495/04
摘要： Formula (I) ((Ia) and (Ib)) compounds wherein (i) X 1 is N and X 2 is S, (ii) X 1 is CR 7 and X 2 is S, (iii) X 1 is N and X 2 is NR 2 , or (iv) X 1 is CR 7 and X 2 is O, including stereoisomers, tautomers, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting the delta isoform of PI3K, and for treating disorders mediated by lipid kinases such as inflammation, immunological, and cancer. Methods of using compounds of Formula (I) for in vitro, in situ , and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
摘要翻译：式（I）（（Ia）和（Ib））化合物，其中（i）X1是N，X2是S，（ii）X1是CR7，X2是S，（iii）X1是N，X2是NR2，或 iv）X1是CR7，X2是O，包括立体异构体，互变异构体，代谢物和药学上可接受的盐，可用于抑制PI3K的δ同种型，以及用于治疗由脂质激酶如炎症，免疫学和癌症介导的病症。公开了使用式（I）化合物在体外，原位和体内诊断，预防或治疗哺乳动物细胞或相关病理状况中的这种病症的方法。

7. 发明申请

WO2009085980A1 8-ANILIN0IMIDAZ0PYRIDINES AND THEIR USE AS ANTI-CANCER AND/OR ANTI-INFLAMMATORY AGENTS 审中-公开
标题翻译： 8-ANILIN0IMIDAZ0PYRIDINES及其作为抗癌剂和/或抗炎剂的用途
公开(公告)号：WO2009085980A1
公开(公告)日：2009-07-09
申请号：PCT/US2008/087476
申请日：2008-12-18
申请人： GENENTECH, INC. , PRICE, Stephen , HEALD, Robert , SAVY, Pascal Pierre Alexandre
发明人： PRICE, Stephen , HEALD, Robert , SAVY, Pascal Pierre Alexandre
IPC分类号： C07D471/04 , C07D487/04 , A61K31/437 , A61P35/00
CPC分类号： C07D471/04 , C07D487/04
摘要： The invention relates to imidazopyridines of formula I with anti -cancer and/or anti- inflammatory activity and more specifically to imidazopyridines which inhibit MEK kinase activity. The invention provides compositions and methods useful for inhibiting abnormal cell growth or treating a hyperprolif erative disorder, or treating an inflammatory disease in a mammal. The invention also relates to methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions. (Formula I)
摘要翻译：本发明涉及式I的咪唑并吡啶与抗癌和/或抗炎活性，更具体地涉及抑制MEK激酶活性的咪唑并吡啶类。本发明提供了可用于抑制异常细胞生长或治疗过度增生性病症或治疗哺乳动物炎性疾病的组合物和方法。本发明还涉及将化合物用于体外，原位和体内诊断或治疗哺乳动物细胞或相关病理状况的方法。（式I）

8. 发明申请

WO2005040167A1 NOVEL DIAZASPIROALKANES AND THEIR USE FOR TREATMENT OF CCR8 MEDIATED DISEASES 审中-公开
标题翻译：新西兰双倍体药物及其用于治疗CCR8介导性疾病的用途
公开(公告)号：WO2005040167A1
公开(公告)日：2005-05-06
申请号：PCT/SE2004/001522
申请日：2004-10-21
申请人： ASTRAZENECA AB , BLADH, Håkan , CONNOLLY, Stephen , DYKE, Hazel Joan , LISIUS, Annea , PRICE, Stephen , SHAMOVSKY, Igor , VAN DEN HEUVEL, Marco
发明人： BLADH, Håkan , CONNOLLY, Stephen , DYKE, Hazel Joan , LISIUS, Annea , PRICE, Stephen , SHAMOVSKY, Igor , VAN DEN HEUVEL, Marco
IPC分类号： C07D471/10
CPC分类号： C07D471/10
摘要： The invention provides compounds of general formula. wherein A, B, W, X, Y, Z, D, E, R1 and n are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
摘要翻译：本发明提供了通式的化合物。其中A，B，W，X，Y，Z，D，E，R 1和n如说明书中所定义，其制备方法，含有它们的药物组合物及其在治疗中的用途。

9. 发明申请

WO2007115410A1 COMPOSITIONS AND METHODS FOR MODULATING GATED ION CHANNELS 审中-公开
标题翻译：用于调制离子通道的组合物和方法
公开(公告)号：WO2007115410A1
公开(公告)日：2007-10-18
申请号：PCT/CA2007/000596
申请日：2007-04-10
申请人： PAINCEPTOR PHARMA CORPORATION , VOHRA, Rahul , GAN, Zhonghong , WEI, Chang-Qing , PRICE, Stephen , DYKE, Hazel, Joan , DECHAUX, Elsa, Amandine
发明人： VOHRA, Rahul , GAN, Zhonghong , WEI, Chang-Qing , PRICE, Stephen , DYKE, Hazel, Joan , DECHAUX, Elsa, Amandine
IPC分类号： C07D217/04 , A61K31/472 , A61K31/4725 , A61K31/497 , A61K31/501 , C07D401/04 , C07D401/14 , C07D413/04
CPC分类号： C07D471/04 , C07D209/40
摘要： The present invention relates to compounds of the Formula (I),(II), (III), (IV) or (V) useful to modulate the activity of gated ion channels. The invention further relates to methods wherein said compounds are used to modulate gated ion channels comprised of at least one subunit which is a member of the DEG/ENaC, P2X or TRPV gene superfamilies. The activity of the gated ion channels which are modulated by compounds I-V are associated with pain, inflammatory disorders or neurological disorders.
摘要翻译：本发明涉及可用于调节门控离子通道活性的式（I），（II），（III），（IV）或（V）化合物。本发明还涉及其中所述化合物用于调节由至少一个亚基组成的门控离子通道的方法，该亚基是DEG / ENaC，P2X或TRPV基因超家族的成员。由化合物I-V调节的门控离子通道的活性与疼痛，炎症性疾病或神经障碍有关。

10. 发明申请

WO2005014588A1 SUBSTITUTED THIENYL-HYDROXAMIC ACIDS HAVING HISTONE DEACETYLASE ACTIVITY 审中-公开
标题翻译：具有HISTONE脱乙酰酶活性的取代的三羟基酸
公开(公告)号：WO2005014588A1
公开(公告)日：2005-02-17
申请号：PCT/GB2004/000353
申请日：2004-01-29
申请人： ARGENTA DISCOVERY LIMITED , DYKE, Hazel, Joan , PRICE, Stephen , VAN DEN HEUVEL, Marco , SUTTON, Jonathan, Mark , MACKENZIE, Robert, Edward , HEALD, Robert, Andrew
发明人： DYKE, Hazel, Joan , PRICE, Stephen , VAN DEN HEUVEL, Marco , SUTTON, Jonathan, Mark , MACKENZIE, Robert, Edward , HEALD, Robert, Andrew
IPC分类号： C07D409/04
CPC分类号： C07D409/04 , C07D409/14
摘要： A compound of formula (I): in which A represents optionally substituted monocyclic heteroaryl or phenyl B represents optionally substituted heteroaryl, aryl, aryl-fused-heterocycloalkyl, heteroaryl-fused-cycloalkyl, heteroaryl-fused-heterocycloalkyl or aryl-fused-cycloalkyl X and Y, which may be the same or different, each independently represent -0-, -NR 1 -, CO-, -S0 2 -, -SO-, -S-, -NR 1 CO-, -NR 1 S0 2 -, -CONR 1 -, -SO 2 NR 1 -, -NR 1 CONR 1 or X may be a direct bond when Y represents -NR 1 -, -NR 1 CO-, -NR 1 SO 2 -, -CONR 1 -, - SO 2 NR 1 - or -NR 1 CONR I - provided that R 1 represents alkyl substituted by -OR 2 , -NR 3 R 4 , - NR 4 COR 5 , -NR 4 SO 2 R 5 , -CONR 3 R 4 or -S0 2 NR 3 R 4 R 1 represents H, alkyl, arylalkyl, heteroarylalkyl, heterocycloalkylalkyl, cycloalkylalkyl, or alkyl substituted by -OR 2 , -NR 3 R 4 , -NR 4 COR 5 , -NR 4 S0 2 R 5 , -CONR 3 R 4 or -S0 2 NR 3 R 4 R 2 represents H, alkyl, arylalkyl, heteroarylalkyl, heterocycloalkylalkyl, cycloalkylalkyl, aryl, heteroaryl, heterocycloalkyl or cycloalkyl R 3 represents H or alkyl R 4 represents H, alkyl, arylalkyl, heteroarylalkyl, heterocycloalkylalkyl, cycloalkylalkyl, aryl, heteroaryl, heterocycloalkyl or cycloalkyl or NR 3 R 4 represents a cyclic amine R 5 represents alkyl, aryl, heteroaryl, cycloalkyl, heterocycloalkyl, arylalkyl, heteroarylalkyl, cycloalkylalkyl, heterocycloalkylalkyl n represents 0-3 m represents 1-3 p represents 0-3 and corresponding N -oxides, pharmaceutically acceptable salts, solvates and prodrugs thereof; and use to treat a disease in which inhibition of histone deacetylase can prevent, inhibit or ameliorate the pathology and/or symptomatology of the disease.
摘要翻译：式（I）化合物：其中A表示任选取代的单环杂芳基或苯基B表示任选取代的杂芳基，芳基，芳基稠合 - 杂环烷基，杂芳基 - 稠合环烷基，杂芳基 - 稠合 - 杂环烷基或芳基稠合 - 环烷基X 和Y可以相同或不同，各自独立地表示-O - ， - NR - ， - CO - ， - SO2-，-SO - ， - S - ， - NR 1 CO - ， - NR 当Y表示-NR 1 - ，-NR 1时，SO 2 - ， - CONR 1 - ， - SO 2 NR 1 - ， - NR 1 CONR 1或X可以是直接键 CO - ， - NR 1 SO 2 - ， - CONR 1 - ， - SO 2 NR 1 - 或-NR 1 CONR - 条件是R 1表示被-OR 2取代的烷基， -NR 3 R 4，-NR 4 COR 5，-NR 4 SO 2 R 5，-CONR 3 R 4或-SO 2 NR 3 R 4， R 1表示H，烷基，芳基烷基，杂芳基烷基，杂环烷基烷基，环烷基烷基或被-OR 2取代的烷基，-NR 3 R 4，-NR 4 COR 5， 4 SO 2 R 5，-CONR 3 R 4或-SO 2 NR 3 R 4表示H，烷基，芳基烷基，杂芳基烷基，杂环烷基烷基，环烷基烷基，芳基，杂芳基 1，杂环烷基或环烷基R 3表示H或烷基R 4表示H，烷基，芳基烷基，杂芳基烷基，杂环烷基烷基，环烷基烷基，芳基，杂芳基，杂环烷基或环烷基或NR 3 R 4表示环状胺 R 5表示烷基，芳基，杂芳基，环烷基，杂环烷基，芳基烷基，杂芳基烷基，环烷基烷基，杂环烷基烷基n表示0-3m表示1-3p表示0-3及相应的N-氧化物，药学上可接受的盐，溶剂合物和前药物; 并且用于治疗组蛋白脱乙酰酶的抑制可以预防，抑制或改善疾病的病理学和/或症状学的疾病。

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