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1. 发明申请

WO2013178591A1 AMINOQUINAZOLINE AND PYRIDOPYRIMIDINE DERIVATIVES 审中-公开
标题翻译：氨基喹啉和吡咯并吡啶衍生物
公开(公告)号：WO2013178591A1
公开(公告)日：2013-12-05
申请号：PCT/EP2013/060884
申请日：2013-05-27
申请人： F. HOFFMANN-LA ROCHE AG , GENENTECH, INC.
发明人： CHEN, Huifen , CRAWFORD, Terry , HARRIS, Seth F. , MAGNUSON, Steven , NDUBAKU, Chudi , WANG, Lan
IPC分类号： C07D403/12 , C07D401/04 , C07D401/06 , C07D403/06 , C07D405/12 , C07D239/94 , C07D239/95 , C07D413/12 , C07D471/04 , A61P35/00 , A61K31/517 , A61K31/519
CPC分类号： A61K31/519 , A61K31/5377 , A61K31/551 , A61K31/553 , C07D239/94 , C07D239/95 , C07D401/04 , C07D401/06 , C07D403/06 , C07D403/12 , C07D405/12 , C07D413/12 , C07D471/04
摘要： The invention provides novel compounds having the general formula (I): wherein A, R 1 R 2 and R 3 are as defined herein, compositions including the compounds and methods of using the compounds.
摘要翻译：本发明提供具有通式（I）的新化合物：其中A，R 1 R2和R 3如本文所定义，包括该化合物的组合物和使用该化合物的方法。

2. 发明申请

WO2012035039A1 AZABENZOTHIAZOLE COMPOUNDS, COMPOSITIONS AND METHODS OF USE 审中-公开
标题翻译： AZABENZOTHIAZOLE化合物，组合物和使用方法
公开(公告)号：WO2012035039A1
公开(公告)日：2012-03-22
申请号：PCT/EP2011/065892
申请日：2011-09-14
申请人： F. HOFFMANN-LA ROCHE AG , BLENCH, Toby , ELLWOOD, Charles , GOODACRE, Simon , LAI, Yingjie , LIANG, Jun , MACLEOD, Calum , MAGNUSON, Steven , TSUI, Vickie , WILLIAMS, Karen , ZHANG, Birong
发明人： BLENCH, Toby , ELLWOOD, Charles , GOODACRE, Simon , LAI, Yingjie , LIANG, Jun , MACLEOD, Calum , MAGNUSON, Steven , TSUI, Vickie , WILLIAMS, Karen , ZHANG, Birong
IPC分类号： A61K31/429 , C07D513/00 , A61P29/00
CPC分类号： A61K31/5377 , A61K31/437 , A61K31/501 , A61K31/506 , A61K31/519 , C07D513/04
摘要： Provided are compounds of Formula I, stereoisomers, tautomers, solvates, prodrugs and pharmaceutically acceptable salts thereof, wherein A, X, R 1 , R 2 , R 4 and R 5 are defined herein, a pharmaceutical composition that includes a compound of Formula I and a pharmaceutically acceptable carrier, adjuvant or vehicle, methods of using the compound or composition in therapy, and methods of 5 manufacturing a compound of Formula I.
摘要翻译：提供式I化合物，立体异构体，互变异构体，溶剂合物，前药和药学上可接受的盐，其中A，X，R 1，R 2，R 4和R 5在本文中定义，药物组合物包括式I化合物和药学上可接受的载体，佐剂或载体，在治疗中使用化合物或组合物的方法，以及制备式I化合物的方法。

3. 发明申请

WO2012066061A1 PYRAZOLOPYRIDINES AND PYRAZOLOPYRIDINES AND THEIR USE AS TYK2 INHIBITORS 审中-公开
标题翻译：吡唑并吡啶和吡唑并吡啶及其作为TY2抑制剂的用途
公开(公告)号：WO2012066061A1
公开(公告)日：2012-05-24
申请号：PCT/EP2011/070313
申请日：2011-11-17
申请人： F. HOFFMANN-LA ROCHE AG , BLENCH, Toby , GOODACRE, Simon , LAI, Yingjie , LIANG, Yun , MACLEOD, Calum , MAGNUSON, Steven , TSUI, Vickie , WILLIAMS, Karen , ZHANG, Birong
发明人： BLENCH, Toby , GOODACRE, Simon , LAI, Yingjie , LIANG, Yun , MACLEOD, Calum , MAGNUSON, Steven , TSUI, Vickie , WILLIAMS, Karen , ZHANG, Birong
IPC分类号： C07D471/04 , C07D487/04 , A61K31/37 , A61K31/519 , A61P11/02 , A61P11/06 , A61P17/06 , A61P19/02
CPC分类号： C07D471/04 , C07D487/04
摘要： The invention provides compounds of Formula (I), stereoisomers or pharmaceutically acceptable salts thereof, wherein A, X, R 1 , R 2 , R 4 and R 5 are defined herein, a pharmaceutical composition that includes a compound of Formula (I) and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of using the compound or composition in therapy, as TYK2 Kinase inhibitors.
摘要翻译：本发明提供式（I）的化合物，其立体异构体或其药学上可接受的盐，其中A，X，R 1，R 2，R 4和R 5在本文中定义;药物组合物，其包含式（I）的化合物和药学上可接受的载体，佐剂或载体，以及在治疗中使用该化合物或组合物的方法，作为TYK2激酶抑制剂。

4. 发明申请

WO2016112251A1 4,5-DIHYDROIMIDAZOLE DERIVATIVES AND THEIR USE AS HISTONE DEMETHYLASE (KDM2B) INHIBITORS 审中-公开
标题翻译： 4,5-DIHYDROIMIDAZOLE衍生物及其用作HISTONE DEMETHYLASE（KDM2B）抑制剂
公开(公告)号：WO2016112251A1
公开(公告)日：2016-07-14
申请号：PCT/US2016/012588
申请日：2016-01-08
申请人： GENENTECH, INC. , CONSTELLATION PHARMACEUTICALS, INC.
发明人： ALBRECHT, Brian, K. , COTE, Alexandre , GEHLING, Victor , HSIAO-WEI TSUI, Vickie , KIEFER, James, Richard, Jr. , LIANG, Jun , MAGNUSON, Steven , NASVESCHUK, Christopher, G. , ROMERO, F. Anthony , TAYLOR, Alexander, M.
IPC分类号： C07D403/12 , C07D233/44 , C07D401/04 , C07D235/02 , C07D401/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D487/08 , A61K31/454 , A61K31/496 , A61K31/4995 , A61P35/00
CPC分类号： C07D233/44 , C07D235/02 , C07D401/04 , C07D401/12 , C07D403/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D487/08
摘要： The present invention relates to compounds of formula (I), (formula I) wherein: X is C(=0) or S(0) 2 ; R 1 is selected from the group consisting of N-linked piperazinyl, relinked piperidine, and N-linked diazabicyclo[3.2.1]octane, wherein R 1 is optionally substituted with one or more groups; R 2 and R 3 are each independently selected from H, C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, and C 3-8 cycloalkyl, wherein any C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, and C 3-8 cycloalkyl is optionally substituted with one or more groups; or R 2 and R 3 taken together with the carbon to which they are attached form a 3-, 4-, 5-, or 6-membered carbocyclic ring that is optionally substituted with one or more groups; R 4 and R 5 are each independently selected from H, C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, and C 3-8 cycloalkyl, wherein any C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, and C 3-8 cycloalkyl is optionally substituted with one or more groups; or R 4 and R 5 taken together with the carbon to which they are attached form a 3-, 4-, 5-, or 6-membered carbocyclic ring that is optionally substituted with one or more groups; and R 6 is a 5-10 membered heteroaryl, 5-10 membered heterocycle, or a 6-10 membered aryl, which 5-10 membered heteroaryl, 5-10 membered heterocycle, and 6-10 membered aryl is optionally substituted with one or more groups; useful as inhibitors of one or more histone demethylses, such as KDM2b. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using said compositions in the treatment of various disorders.
摘要翻译：本发明涉及式（I），（式I）的化合物，其中：X为C（= O）或S（O）2; R1选自N-连接的哌嗪基，再连接的哌啶和N-连接的二氮杂双环[3.2.1]辛烷，其中R 1任选被一个或多个基团取代; R 2和R 3各自独立地选自H，C 1-6烷基，C 2-6烯基，C 2-6炔基和C 3-8环烷基，其中任何C 1-6烷基，C 2-6烯基，C 2-6炔基和C 3-8环烷基任选被一个或更多组; 或者R 2和R 3与它们所连接的碳一起形成任选被一个或多个基团取代的3-，4-，5-或6-元碳环; R 4和R 5各自独立地选自H，C 1-6烷基，C 2-6烯基，C 2-6炔基和C 3-8环烷基，其中任何C 1-6烷基，C 2-6烯基，C 2-6炔基和C 3-8环烷基任选被一个或更多组; 或R 4和R 5与它们所连接的碳一起形成任选被一个或多个基团取代的3-，4-，5-或6-元碳环; 并且R 6是5-10元杂芳基，5-10元杂环或6-10元芳基，其中5-10元杂芳基，5-10元杂环和6-10元芳基任选被一个或多个组; 可用作一种或多种组蛋白去甲基酶的抑制剂，例如KDM2b。本发明还提供包含本发明化合物的药学上可接受的组合物和使用所述组合物治疗各种疾病的方法。

5. 发明申请

WO2017205538A1 PYRAZOLOPYRIDINE DERIVATIVES FOR THE TREATMENT OF CANCER 审中-公开
标题翻译：吡唑并吡啶衍生物用于治疗癌症
公开(公告)号：WO2017205538A1
公开(公告)日：2017-11-30
申请号：PCT/US2017/034326
申请日：2017-05-24
申请人： GENENTECH, INC. , CONSTELLATION PHARMACEUTICALS, INC.
发明人： CYR, Patrick , BRONNER, Sarah , ROMERO, F. Anthony , MAGNUSON, Steven , TSUI, Vickie Hsiao-Wei , MURRAY, Jeremy M. , WAI, John , LAI, Kwong Wah , WANG, Fei , CHEN, Kevin X.
IPC分类号： C07D471/04 , C07D519/00 , A61K31/437 , A61P35/00
摘要： The present invention relates to a compound formula (I): and to salts thereof, wherein R 1 , R 2 X, and Y 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) 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 such as cancer, inflammatory disorders and autoimmune diseases.
摘要翻译：本发明涉及式（I）化合物及其盐，其中R 1，R 2 X和Y具有式本文定义的任何值，以及其组成和用途。该化合物可用作CBP和/或EP300的抑制剂。还包括包含式（I）化合物或其药学上可接受的盐的药物组合物，以及使用该化合物和盐治疗各种CBP和/或EP300介导的疾病如癌症，炎性疾病和自身免疫疾病的方法

6. 发明申请

WO2016036873A1 THERAPEUTIC COMPOUNDS AND USES THEREOF 审中-公开
标题翻译：治疗化合物及其用途
公开(公告)号：WO2016036873A1
公开(公告)日：2016-03-10
申请号：PCT/US2015/048174
申请日：2015-09-02
申请人： GENENTECH, INC. , CONSTELLATION PHARMACEUTICALS, INC.
发明人： ALBRECHT, Brian, K. , COTE, Alexandre , CRAWFORD, Terry , DUPLESSIS, Martin , GOOD, Andrew, Charles , LEBLANC, Yves , MAGNUSON, Steven , NASVESCHUK, Christopher, G. , PASTOR, Richard , ROMERO, F. Anthony , TAYLOR, Alexander, M.
IPC分类号： C07D403/12 , C07D401/04 , C07D401/12 , C07D403/04 , C07D249/12 , A61K31/4196 , A61P35/00
CPC分类号： C07D403/12 , A61K31/53 , A61K45/06 , C07D249/12 , C07D253/075 , C07D401/04 , C07D401/12 , C07D403/04
摘要： The present invention relates to compounds of formula (1): The present invention relates to methods for treating PCAF mediated disorders using a compound of formula (I) or a pharmaceutically acceptable salt thereof: Formula (1) wherein R 1 , R 3 -R 6 , X, and each R e have any of the values defined in the specification. Also included are novel compounds of formula (I) and salts thereof, as well as pharmaceutical compositions comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明涉及式（I）化合物：本发明涉及使用式（I）化合物或其药学上可接受的盐治疗PCAF介导的病症的方法：式（1）其中R1，R3-R6，X ，并且每个Re具有说明书中定义的任何值。还包括式（I）的新化合物及其盐，以及包含式（I）化合物或其药学上可接受的盐的药物组合物。

7. 发明申请

WO2015054642A9 USE OF CBP/EP300 BROMODOMAIN INHIBITORS FOR CANCER IMMUNOTHERAPY 审中-公开
公开(公告)号：WO2015054642A9
公开(公告)日：2015-04-16
申请号：PCT/US2014/060147
申请日：2014-10-10
申请人： GENENTECH, INC. , CONSTELLATION PHARMACEUTICALS, INC.
发明人： ALBRECHT, Brian, K. , AUDIA, James, Edmund , BELLON, Steven , COCHRAN, Andrea , COTE, Alexandre , CRAWFORD, Terry , FAUBER, Benjamin , GHOSH, Srimoyee , HARMANGE, Jean-Christophe , HATZIVASSILIOU, Georgia , JAYARAM, Hariharan , KIM, Jeong , LORA, Jose, M. , MAGNUSON, Steven , MELLMAN, Ira , ROMERO, F., Anthony , TAYLOR, Alexander, M. , TSUI, Vickie
IPC分类号： A61K38/00 , A61P17/00
摘要： The present invention relates to use of CBP/EP300 bromodomain inhibitors for the treatment of cancer.

8. 发明申请

WO2016123391A1 THERAPEUTIC COMPOUNDS AND USES THEREOF 审中-公开
标题翻译：治疗化合物及其用途
公开(公告)号：WO2016123391A1
公开(公告)日：2016-08-04
申请号：PCT/US2016/015450
申请日：2016-01-28
申请人： GENENTECH, INC. , CONSTELLATION PHARMACEUTICALS, INC.
发明人： ADLER, Marc , BURDICK, Daniel, J. , CRAWFORD, Terry , DUPLESSIS, Martin , MAGNUSON, Steven , NASVESCHUK, Christopher, G. , ROMERO, F. Anthony , TANG, Yong , TSUI, Vickie Hsiao-Wei , WANG, Shumei
IPC分类号： C07D471/04 , A61K31/437 , A61P35/00
CPC分类号： C07D471/04 , A61K31/437 , A61K31/444 , A61K31/4545 , A61K31/506 , A61K31/5377 , A61K45/06 , C07D519/00
摘要： The present invention relates to compounds of formula (I): and to salts thereof, wherein R 1 -R 6 have any of the values defined in the specification, and compositions and uses thereof. The compounds are useful as inhibitors of TAF1. Also included are pharmaceutical compositions comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof, and methods of using such compounds and salts in the treatment of various TAF1-mediated disorders.
摘要翻译：本发明涉及式（I）化合物及其盐，其中R 1 -R 6具有说明书中定义的任何值，以及其组成和用途。该化合物可用作TAF1的抑制剂。还包括包含式（I）化合物或其药学上可接受的盐的药物组合物，以及在治疗各种TAF1介导的病症中使用这些化合物和盐的方法。

9. 发明申请

WO2016086200A9 4,5,6,7-TETRAHYDRO-1 H-PYRAZOLO[4,3-C]PYRIDIN-3-AMINE COMPOUNDS AS CBP AND/OR EP300 INHIBITORS 审中-公开
标题翻译：作为CBP和/或EP300抑制剂的4,5,6,7-四氢-1H-吡唑并[4,3-C]吡啶-3-胺化合物
公开(公告)号：WO2016086200A9
公开(公告)日：2016-06-02
申请号：PCT/US2015/062794
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.
摘要翻译：本发明涉及式（I）或式（II）的化合物及其盐，其中R 1 -R 4，（I）和式（II）的R 1 -R 3具有本文所定义的任何值，及其组合物和用途。该化合物可用作CBP和/或EP300的抑制剂。还包括包含式（II）的式（I）化合物或其药学上可接受的盐的药物组合物，以及在治疗各种CBP和/或EP300介导的病症中使用此类化合物和盐的方法。

10. 发明申请

WO2014144721A2 TREATING TH2-MEDIATED DISEASES BY INHIBITION OF BROMODOMAINS 审中-公开
标题翻译：通过抑制BROMODOMAINS治疗TH2介导的疾病
公开(公告)号：WO2014144721A2
公开(公告)日：2014-09-18
申请号：PCT/US2014/029252
申请日：2014-03-14
申请人： GENENTECH, INC. , CONSTELLATION PHARMACEUTICALS, INC.
发明人： ALBRECHT, Brian K. , COTE, Alexandre , CRAWFORD, Terry , FAUBER, Benjamin , HUANG, Hon-Ren , LORA, Jose M. , MAGNUSON, Steven , NASVESCHUK, Christopher G. , SALMERON, Andres , SIMS III, Robert J. , TAYLOR, Alexander M.
IPC分类号： C12N15/11
CPC分类号： C12N15/113 , A61K31/437 , A61K31/444 , A61K31/496 , A61K31/713 , C07K14/4702 , C12N2310/14 , C12N2320/30 , G01N33/505 , G01N2333/52 , G01N2500/04 , G01N2500/10 , Y02A50/422
摘要： The invention provides methods for treating Th2 cytokine-mediated diseases by inhibiting bromodomain function.
摘要翻译：本发明提供了通过抑制溴结构域功能来治疗Th2细胞因子介导的疾病的方法。

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