公开(公告)号：EP3224258A1

公开(公告)日：2017-10-04

申请号：EP15816578.7

申请日：2015-11-25

申请人： Genentech, Inc. ,  Constellation Pharmaceuticals, Inc.

发明人： ROMERO, F. Anthony ,  MAGNUSON, Steven ,  PASTOR, Richard ,  TSUI, Vickie Hsiao-Wei ,  MURRAY, Jeremy ,  CRAWFORD, Terry ,  ALBRECHT, Brian, K. ,  COTE, Alexandre ,  TAYLOR, Alexander, M. ,  LAI, Kwong Wah ,  CHEN, Kevin, X. ,  BRONNER, Sarah ,  ADLER, Marc ,  EGEN, Jackson ,  LIAO, Jiangpeng ,  WANG, Fei ,  CYR, Patrick ,  ZHU, Bing-Yan ,  KAUDER, Steven

IPC分类号： C07D471/04 ,  A61K31/437 ,  A61P35/00 ,  A61P29/00 ,  A61P37/00

CPC分类号： A61K31/437 ,  A61K31/4375 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/498 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/5415 ,  A61K31/55 ,  A61K45/06 ,  C07D471/04 ,  C07D519/00

摘要： The present invention relates to compounds of formula (I) or formula (II): and to salts thereof, wherein R1-R4 of formula (I) and R1-R3 of formula (II) have any of the values defined herein, and compositions and uses thereof. The compounds are useful as inhibitors of CBP and/or EP300. Also included are pharmaceutical compositions comprising a compound of formula (I) of formula (II) or a pharmaceutically acceptable salt thereof, and methods of using such compounds and salts in the treatment of various CBP and/or EP300-mediated disorders.

摘要翻译： 本发明涉及式（I）或式（II）的化合物及其盐，其中式（I）的R 1 -R 4和式（II）的R 1 -R 3具有本文所定义的任何值， 及其用途。 该化合物可用作CBP和/或EP300的抑制剂。 还包括药物组合物，其包含式（II）的式（I）化合物或其药学上可接受的盐，以及使用该化合物和盐治疗各种CBP和/或EP300介导的病症的方法。

公开(公告)号：EP3632915A1

公开(公告)日：2020-04-08

申请号：EP19191423.3

申请日：2015-11-25

申请人： GENENTECH, INC. ,  Constellation Pharmaceuticals, Inc.

发明人： ROMERO, F. Anthony ,  MAGNUSON, Steven ,  PASTOR, Richard ,  TSUI, Vickie Hsiao-Wei ,  MURRAY, Jeremy ,  CRAWFORD, Terry ,  ALBRECHT, Brian, K. ,  COTE, Alexandre ,  TAYLOR, Alexander, M. ,  LAI, Kwong Wah ,  CHEN, Kevin, X. ,  BRONNER, Sarah ,  ADLER, Marc ,  EGEN, Jackson ,  LIAO, Jiangpeng ,  WANG, Fei ,  CYR, Patrick ,  ZHU, Bing-Yan ,  KAUDER, Steven

IPC分类号： C07D471/04 ,  A61K31/437 ,  A61P35/00 ,  A61P29/00 ,  A61P37/00

摘要： The present invention relates to compounds of formula (I) or formula (II):

and to salts thereof, wherein R 1 -R 4 of formula (I) and R 1 -R 3 of formula (II) have any of the values defined herein, and compositions and uses thereof. The compounds are useful as inhibitors of CBP and/or EP300. Also included are pharmaceutical compositions comprising a compound of formula (I) of formula (II) or a pharmaceutically acceptable salt thereof, and methods of using such compounds and salts in the treatment of various CBP and/or EP300-mediated disorders.

公开(公告)号：EP3224258B1

公开(公告)日：2019-08-14

申请号：EP15816578.7

申请日：2015-11-25

申请人： Genentech, Inc. ,  Constellation Pharmaceuticals, Inc.

发明人： ROMERO, F. Anthony ,  MAGNUSON, Steven ,  PASTOR, Richard ,  TSUI, Vickie Hsiao-Wei ,  MURRAY, Jeremy ,  CRAWFORD, Terry ,  ALBRECHT, Brian, K. ,  COTE, Alexandre ,  TAYLOR, Alexander, M. ,  LAI, Kwong Wah ,  CHEN, Kevin, X. ,  BRONNER, Sarah ,  ADLER, Marc ,  EGEN, Jackson ,  LIAO, Jiangpeng ,  WANG, Fei ,  CYR, Patrick ,  ZHU, Bing-Yan ,  KAUDER, Steven

IPC分类号： C07D471/04 ,  A61K31/437 ,  A61P35/00 ,  A61P29/00 ,  A61P37/00

公开(公告)号：EP2356117A1

公开(公告)日：2011-08-17

申请号：EP09761108.1

申请日：2009-11-19

申请人： Genentech, Inc. ,  F. Hoffmann-La Roche AG

发明人： DOTSON, Jennafer ,  HEFFRON, Tim ,  OLIVERO, Alan G. ,  SUTHERLIN, Daniel P. ,  STABEN, Steven ,  WANG, Shumei ,  ZHU, Bing-Yan ,  CHUCKOWREE, Irina S. ,  FOLKES, Adrian J. ,  WAN, Nan Chi

IPC分类号： C07D471/04 ,  A61K31/437 ,  A61P35/00

CPC分类号： C07D471/04

摘要： Compounds of Formula (I), 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 or inflammation mediated by lipid kinases. 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.

公开(公告)号：EP2348860A1

公开(公告)日：2011-08-03

申请号：EP09824234.0

申请日：2009-11-02

申请人： Genentech, Inc.

发明人： BLANEY, Jeffrey ,  GIBBONS, Paul A. ,  HANAN, Emily ,  LYSSIKATOS, Joseph P. ,  MAGNUSON, Steven R. ,  PASTOR, Richard ,  RAWSON, Thomas E. ,  ZHOU, Aihe ,  ZHU, Bing-Yan

IPC分类号： A01N43/90 ,  A61K31/519

CPC分类号： C07D487/04

摘要： The invention provides JAK kinase inhibitors of Formula Ia, enantiomers, diasteriomers or pharmaceutically acceptable salts thereof, wherein R1, R2, R7 and Z are defined herein, a pharmaceutical composition that includes a compound of Formula Ia and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of a JAK kinase activity in a patient. Ia

公开(公告)号：EP2114950A2

公开(公告)日：2009-11-11

申请号：EP07865255.9

申请日：2007-12-05

申请人： Genentech, Inc. ,  F.HOFFMANN-LA ROCHE AG

发明人： CASTANEDO, Georgette ,  DOTSON, Jennafer ,  GOLDSMITH, Richard ,  GUNZNER, Janet ,  HEFFRON, Tim ,  MATHIEU, Simon ,  OLIVERO, Alan ,  STABEN, Steven ,  SUTHERLIN, Daniel P. ,  TSUI, Vickie ,  WANG, Shumei ,  ZHU, Bing-Yan ,  BAYLISS, Tracy ,  CHUCKOWREE, Irina ,  FOLKES, Adrian ,  WAN, Nan Chi

IPC分类号： C07D491/048 ,  C07D495/04 ,  A61K31/519 ,  A61P35/00

CPC分类号： C07D491/048 ,  C07D495/04

摘要： Compounds of Formulas Ia-d where X is S or O, mor is a morpholine group, and R3 is a monocyclic heteroaryl group, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for modulating the activity of lipid kinases including PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula Ia-d for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed. Formula (Ic) and (Id).

公开(公告)号：EP2046799A1

公开(公告)日：2009-04-15

申请号：EP07776052.8

申请日：2007-04-24

申请人： Genentech, Inc. ,  F.HOFFMANN-LA ROCHE AG

发明人： CASTANEDO, Georgette ,  GOLDSMITH, Richard ,  GUNZNER, Janet ,  HEFFRON, Tim ,  MALESKY, Kimberly ,  MATHIEU, Simon ,  OLIVERO, Alan ,  SUTHERLIN, Daniel, P. ,  TSUI, Vickie ,  WANG, Shumei ,  WEISMANN, Christian ,  ZHU, Bing-Yan ,  DOTSON, Jennafer ,  FOLKES, Adrian ,  SHUTTLEWORTH, Stephen ,  OXENFORD, Sally ,  HANCOX, Tim ,  BAYLISS, Tracy

IPC分类号： C07D491/04 ,  C07D495/04 ,  C07D519/00 ,  A61K31/519 ,  A61P35/00

CPC分类号： C07D491/04 ,  C07D495/04

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，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。 公开了使用式Ia和Ib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。

公开(公告)号：EP2041139A2

公开(公告)日：2009-04-01

申请号：EP07755937.5

申请日：2007-04-24

申请人： F.HOFFMANN-LA ROCHE AG ,  Genentech, Inc.

发明人： FOLKES, Adrian ,  SHUTTLEWORTH, Stephen ,  CHUCKOWREE, Irina ,  OXENFORD, Sally ,  WAN, Nan Chi ,  CASTANEDO, Georgette ,  GUNZNER, Janet ,  HEFFRON, Tim ,  MATHIEU, Simon ,  OLIVERO, Alan ,  SUTHERLIN, Daniel, P. ,  ZHU, Bing-Yan ,  GOLDSMITH, Richard

IPC分类号： C07D491/04

CPC分类号： A61K31/5377 ,  A61K31/551 ,  A61K45/06 ,  C07D491/04 ,  C07D491/048 ,  C07D495/04

摘要： Compounds of Formulae la and Ib, and 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 la 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化合物及其立体异构体，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。

公开(公告)号：EP1919920A2

公开(公告)日：2008-05-14

申请号：EP06813425.3

申请日：2006-08-14

申请人： Genentech, Inc. ,  F.HOFFMANN-LA ROCHE AG

发明人： RAWSON, Thomas, E. ,  SAFINA, Brian ,  DOTSON, Jennafer ,  ALIAGAS-MARTIN, Ignacio ,  HALLADAY, Jason ,  LIANG, Jun ,  RUETH, Matthias ,  ZHU, Bing-Yan ,  BROOKFIELD, Frederick ,  PRIME, Michael ,  ZHANG, Birong ,  LI, Jun, M. ,  Zhou, Aihe.

IPC分类号： C07D487/04 ,  C07D491/04 ,  A61K31/4155 ,  A61P35/00

CPC分类号： C07D487/04 ,  C07D491/04

摘要： The invention provides novel kinase inhibitors that are useful as therapeutic agents for example in the treatment malignancies where the compounds have the general formula: (I) wherein A, X, Y, Z, Ra, Rb, Rc, R1 , R2, R3 and m are defined herein.

公开(公告)号：EP4436957A1

公开(公告)日：2024-10-02

申请号：EP22839958.0

申请日：2022-11-21

申请人： Genentech, Inc.

发明人： ZBIEG, Jason Robert ,  SMITH, Russell Tyler ,  BEROZA, Paul Powell ,  VERMA, Vishal ,  ZHU, Bing-Yan ,  BEVERIDGE, Ramsay ,  BARTON, Lisa Marie ,  CHAN, Bryan Ka Ip ,  COLWELL, Curtis ,  BOUAYAD-GERVAIS, Samir ,  DEY, Anwesha ,  EVANGELISTA, Marie Anne

IPC分类号： C07D231/56 ,  C07D471/04 ,  A61P35/00 ,  A61K31/437 ,  A61K31/416

CPC分类号： C07D231/56 ,  C07D471/04 ,  A61P35/00