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1. 发明申请

WO2007059157A1 BISAMIDE INHIBITORS OF HEDGEHOG SIGNALING 审中-公开
标题翻译：双嘧达莫抑制剂信号传导信号
公开(公告)号：WO2007059157A1
公开(公告)日：2007-05-24
申请号：PCT/US2006/044240
申请日：2006-11-14
申请人： GENENTECH, INC. , CURIS, INC. , GOLDSMITH, Richard, A. , SUTHERLIN, Daniel, P. , ROBARGE, Kirk, D. , OLIVERO, Alan, G.
发明人： GOLDSMITH, Richard, A. , SUTHERLIN, Daniel, P. , ROBARGE, Kirk, D. , OLIVERO, Alan, G.
IPC分类号： C07D213/82 , C07D239/28 , C07D277/56 , C07D401/12 , C07D417/12 , C07D231/14 , A61K31/167 , A61K31/496 , A61K31/444 , A61K31/44 , A61K31/4545 , A61K31/4164 , A61K31/4196 , A61K31/4453 , A61K31/5375
CPC分类号： A61K31/167 , A61K31/381 , A61K31/4164 , A61K31/4196 , A61K31/426 , A61K31/433 , A61K31/44 , A61K31/444 , A61K31/4453 , A61K31/4545 , A61K31/496 , A61K31/505 , A61K31/5375 , A61K31/538 , C07D213/82 , C07D231/14 , C07D233/06 , C07D239/28 , C07D249/08 , C07D265/36 , C07D277/56 , C07D285/06 , C07D295/155 , C07D307/68 , C07D333/38 , C07D401/04 , C07D401/12 , C07D401/14 , C07D417/12
摘要： The invention provides inhibitors of hedgehog signaling that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula (I), wherein ring A, ring B, R 1 , R 2 , R 3 , R 4 , R 5 , m and n are as defined herein.
摘要翻译：本发明提供了可用作治疗恶性肿瘤的治疗剂的刺猬蛋白信号传导抑制剂，其中化合物具有通式（I），其中环A，环B，R 1，R 2 R 3，R 3，R 5，m和n如本文所定义。

2. 发明申请

WO2009042607A1 THIAZOLOPYRIMIDINE P13K INHIBITOR COMPOUNDS AND METHODS OF USE 审中-公开
标题翻译：噻唑吡啶P13K抑制剂化合物及其使用方法
公开(公告)号：WO2009042607A1
公开(公告)日：2009-04-02
申请号：PCT/US2008/077394
申请日：2008-09-23
申请人： GENENTECH, INC. , F. HOFFMANN - LA ROCHE AG , CASTANEDO, Georgette, M. , GUNZNER, Janet, L. , MALESKY, Kimberly , MATHIEU, Simon , OLIVERO, Alan, G. , SUTHERLIN, Daniel, P. , WANG, Shumei , ZHU, Bing-yan , CHUCKOWREE, Irina , FOLKES, Adrian , OXENFORD, Sally , WAN, Nan Chi
发明人： CASTANEDO, Georgette, M. , GUNZNER, Janet, L. , MALESKY, Kimberly , MATHIEU, Simon , OLIVERO, Alan, G. , SUTHERLIN, Daniel, P. , WANG, Shumei , ZHU, Bing-yan , CHUCKOWREE, Irina , FOLKES, Adrian , OXENFORD, Sally , WAN, Nan Chi
IPC分类号： C07D513/04 , A61K31/519 , A61P35/00
CPC分类号： C07D513/04
摘要： Compounds of Formulas (Ia and Ib), and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula Ia and Ib 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（Ia和Ib）的化合物，并且包括立体异构体，几何异构体，互变异构体，溶剂合物，代谢物和药学上可接受的盐可用于抑制脂质激酶（包括PI3K）和用于治疗由脂质激酶介导的癌症等疾病。公开了将式Ia和Ib化合物用于体外，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。

3. 发明申请

WO2009123971A1 BENZOPYRAN AND BENZOXEPIN PI3K INHIBITOR COMPOUNDS AND METHODS OF USE 审中-公开
标题翻译：苯并吡喃和苯唑西林PI3K抑制剂化合物及其使用方法
公开(公告)号：WO2009123971A1
公开(公告)日：2009-10-08
申请号：PCT/US2009/038795
申请日：2009-03-30
申请人： GENENTECH, INC. , F. HOFFMANN- LA ROCHE AG , DO, Steven , GOLDSMITH, Richard , HEFFRON, Tim , KOLESNIKOV, Aleksandr , STABEN, Steven , OLIVERO, Alan, G. , SIU, Michael , SUTHERLIN, Daniel, P. , ZHU, Bing-yan , GOLDSMITH, Paul , BAYLISS, Tracy , FOLKES, Adrian , PEGG, Neil
发明人： DO, Steven , GOLDSMITH, Richard , HEFFRON, Tim , KOLESNIKOV, Aleksandr , STABEN, Steven , OLIVERO, Alan, G. , SIU, Michael , SUTHERLIN, Daniel, P. , ZHU, Bing-yan , GOLDSMITH, Paul , BAYLISS, Tracy , FOLKES, Adrian , PEGG, Neil
IPC分类号： C07D495/04 , C07D513/04 , A61K31/38 , A61K31/429 , A61P35/00
CPC分类号： C07F5/02 , A61K31/381 , A61K31/4155 , A61K31/4196 , A61K31/4245 , A61K31/427 , A61K31/429 , A61K31/4365 , A61K31/4436 , A61K31/496 , A61K31/53 , C07D495/04 , C07D495/14 , C07D513/14
摘要： Benzopyran and benzoxepin compounds of Formulas I and II, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formulas I and II 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和II的苯并吡喃和苯并辛菌素化合物，包括立体异构体，几何异构体，互变异构体，溶剂合物，代谢物和药学上可接受的盐，可用于抑制脂质激酶，包括p110α和PI3K的其他同种型，并用于治疗疾病如癌症由脂质激酶介导。公开了使用式I和II的化合物在体外，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。

4. 发明申请

WO2017108723A2 PYRAZOLO[1,5a]PYRIMIDINE DERIVATIVES AS IRAK4 MODULATORS 审中-公开
标题翻译：作为IRAK4调节剂的吡唑并[1,5a]嘧啶衍生物
公开(公告)号：WO2017108723A2
公开(公告)日：2017-06-29
申请号：PCT/EP2016/081810
申请日：2016-12-19
申请人： F. HOFFMANN-LA ROCHE AG , GENENTECH, INC.
发明人： BRYAN, Marian, C. , GOBBI, Alberto , KIEFER, James, Richard, Jr. , KOLESNIKOV, Aleksandr , OLIVERO, Alan, G. , DROBNICK, Joy , LIANG, Jun , RAJAPAKSA, Naomi
IPC分类号： C07D487/04
CPC分类号： C07D487/04 , C07D519/00
摘要： Compounds of Formula (0), Formula (I), and Formula (II) and methods of use as Interleukin-1 Receptor Associated Kinase (IRAK4) inhibitors are described herein.
摘要翻译：式（0），式（I）和式（II）的化合物以及作为白细胞介素-1受体相关激酶（IRAK4）抑制剂的方法在本文中描述。

5. 发明公开

EP1144373A2 SERINE PROTEASE INHIBITORS 有权
标题翻译：丝氨酸蛋白酶抑制剂
公开(公告)号：EP1144373A2
公开(公告)日：2001-10-17
申请号：EP00911572.6
申请日：2000-01-11
申请人： Genentech, Inc.
发明人： ALIAGAS-MARTIN, Ignacio , ARTIS, Dean, R. , DINA, Michael, S. , FLYGARE, John, A. , GOLDSMITH, Richard, A. , MUNROE, Regina, A. , OLIVERO, Alan, G. , PASTOR, Richard , RAWSON, Thomas, E. , ROBARGE, Kirk, D. , SUTHERLIN, Daniel, P. , WEESE, Kenneth, J. , ZHOU, Aihe , ZHU, Yan
IPC分类号： C07C317/00
CPC分类号： C07C257/18 , C07C311/05 , C07C311/08 , C07C311/13 , C07C311/18 , C07C311/29 , C07C311/51
摘要： Compounds having structure (A) are useful to inhibit serine protease enzymes, such as TF/factor VIIa, factor Xa, thrombin and kallikrein. These compounds may be used in methods of preventing and/or treating clotting disorders.

6. 发明公开

EP1144373A3 SERINE PROTEASE INHIBITORS 有权
标题翻译：丝氨酸蛋白酶抑制剂
公开(公告)号：EP1144373A3
公开(公告)日：2002-01-02
申请号：EP00911572.6
申请日：2000-01-11
申请人： Genentech, Inc.
发明人： ALIAGAS-MARTIN, Ignacio , ARTIS, Dean, R. , DINA, Michael, S. , FLYGARE, John, A. , GOLDSMITH, Richard, A. , MUNROE, Regina, A. , OLIVERO, Alan, G. , PASTOR, Richard , RAWSON, Thomas, E. , ROBARGE, Kirk, D. , SUTHERLIN, Daniel, P. , WEESE, Kenneth, J. , ZHOU, Aihe , ZHU, Yan
IPC分类号： C07C311/51
CPC分类号： C07C257/18 , C07C311/05 , C07C311/08 , C07C311/13 , C07C311/18 , C07C311/29 , C07C311/51

7. 发明公开

EP0975608A2 HALO-ALKOXYCARBONYL PRODRUGS 失效
标题翻译：卤代烷氧基前药
公开(公告)号：EP0975608A2
公开(公告)日：2000-02-02
申请号：EP98913417.6
申请日：1998-04-08
申请人： Genentech, Inc.
发明人： BLACKBURN, Brent , OLIVERO, Alan, G. , ROBARGE, Kirk
IPC分类号： C07D243/24 , A61K31/55
CPC分类号： C07D243/14
摘要： Halo-alkoxycarbonyl derivatives of formula (I) are provided as prodrug moieties for pharmaceutical agents containing a basic or polar nitrogen containing fucntionality. The prodrugs are provided as pharmaceutical compositions as well as in methods of treatment. A compound of said formula wherein [(H)0-2(X)1-3] is selected from the group consisting of X3, HX2, and H2X and X2 is a halogen selected from the group consisting of F, Cl, Br, I or a combination thereof; R?2 and R3¿ are the same or different and are selected from the group consisting of H, C¿1?-C4alkyl, C1-C4alkoxy, cyano, halo(F, Cl, Br, I) C1-C4alkyl and aryl, AG-Q is a biologically active pharmaceutical agent wherein Q is a basic N-containing functionality selected from the group consisting of an amino, amidino, aminoalkyleneamino, iminoalkyleneamino, and guanidino group.
摘要翻译：式（I）的卤代 - 烷氧基羰基衍生物作为含有碱性或极性含氮官能团的药剂的前药部分提供。前药作为药物组合物以及治疗方法提供。上式的化合物，其中[（H）0-2（X）1-3]选自X3，HX2和H2X，X2是选自F，Cl，Br，我或其组合; R 2和R 3'相同或不同，选自H，C 1 -C 4烷基，C 1 -C 4烷氧基，氰基，卤代（F，Cl，Br，I）C 1 -C 4烷基和芳基， AG-Q是生物活性药剂，其中Q是选自氨基，脒基，氨基亚烷基氨基，亚氨基亚烷基氨基和胍基的基本的含N官能团。

8. 发明授权

EP2207781B1 THIAZOLOPYRIMIDINE P13K INHIBITOR COMPOUNDS AND METHODS OF USE 有权
标题翻译：噻唑并嘧啶P13K抑制剂化合物及其使用方法
公开(公告)号：EP2207781B1
公开(公告)日：2012-11-28
申请号：EP08832932.1
申请日：2008-09-23
申请人： Genentech, Inc. , F. Hoffmann-La Roche AG
发明人： CASTANEDO, Georgette, M. , GUNZNER, Janet, L. , MALESKY, Kimberly , MATHIEU, Simon , OLIVERO, Alan, G. , SUTHERLIN, Daniel, P. , WANG, Shumei , ZHU, Bing-yan , CHUCKOWREE, Irina , FOLKES, Adrian , OXENFORD, Sally , WAN, Nan Chi
IPC分类号： C07D513/04 , A61K31/519 , A61P35/00
CPC分类号： C07D513/04

9. 发明公开

EP2207781A1 THIAZOLOPYRIMIDINE P13K INHIBITOR COMPOUNDS AND METHODS OF USE 有权
标题翻译：噻唑并嘧啶P13K抑制剂化合物及其使用方法
公开(公告)号：EP2207781A1
公开(公告)日：2010-07-21
申请号：EP08832932.1
申请日：2008-09-23
申请人： Genentech, Inc. , F. Hoffmann-La Roche AG
发明人： CASTANEDO, Georgette, M. , GUNZNER, Janet, L. , MALESKY, Kimberly , MATHIEU, Simon , OLIVERO, Alan, G. , SUTHERLIN, Daniel, P. , WANG, Shumei , ZHU, Bing-yan , CHUCKOWREE, Irina , FOLKES, Adrian , OXENFORD, Sally , WAN, Nan Chi
IPC分类号： C07D513/04 , A61K31/519 , A61P35/00
CPC分类号： C07D513/04
摘要： Compounds of Formulas (Ia and Ib), and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula Ia and Ib 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（Ia和Ib）化合物，包括其立体异构体，几何异构体，互变异构体，溶剂化物，代谢物和药学上可接受的盐可用于抑制包括PI3K在内的脂质激酶，以及用于治疗诸如由脂质激酶介导的癌症等疾病。公开了使用式Ia和Ib化合物体外，原位和体内诊断，预防或治疗哺乳动物细胞中的此类病症或相关病理学病症的方法。

10. 发明授权

EP0975608B1 HALO-ALKOXYCARBONYL PRODRUGS 失效
标题翻译：卤代烷氧基前药
公开(公告)号：EP0975608B1
公开(公告)日：2005-06-15
申请号：EP98913417.6
申请日：1998-04-08
申请人： Genentech, Inc.
发明人： BLACKBURN, Brent , OLIVERO, Alan, G. , ROBARGE, Kirk
IPC分类号： C07D243/24 , A61K31/55
CPC分类号： C07D243/14

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