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1. 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。

2. 发明申请

WO2016055028A1 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：WO2016055028A1
公开(公告)日：2016-04-14
申请号：PCT/CN2015/091614
申请日：2015-10-10
申请人： GENENTECH, INC. , CONSTELLATION PHARMACEUTICALS, INC. , ROMERO, F. Anthony , MAGNUSON, Steven R. , PASTOR, Richard , TSUI, Vickie Hsiao-Wei , MURRAY, Jeremy , CRAWFORD, Terry , BURDICK, Daniel J. , ALBRECHT, Brian K. , COTE, Alexandre , TAYLOR, Alexander M. , NASVESCHUK, Christopher G. , LEBLANC, Yves , HEWITT, Michael Charles , LAI, Kwong Wah , CHEN, Kevin
发明人： ROMERO, F. Anthony , MAGNUSON, Steven R. , PASTOR, Richard , TSUI, Vickie Hsiao-Wei , MURRAY, Jeremy , CRAWFORD, Terry , BURDICK, Daniel J. , ALBRECHT, Brian K. , COTE, Alexandre , TAYLOR, Alexander M. , NASVESCHUK, Christopher G. , LEBLANC, Yves , HEWITT, Michael Charles , LAI, Kwong Wah , CHEN, Kevin
IPC分类号： C07D223/16 , C07D243/12 , C07D267/14 , C07D281/10 , A61K31/551 , A61K31/553 , A61K31/554 , A61P29/00 , A61P37/00 , A61P35/00
CPC分类号： A61K31/55 , A61K31/337 , A61K31/5513 , A61K45/06 , C07D223/16 , C07D243/12 , C07D243/24 , C07D267/14 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/14 , C07D405/04 , C07D405/12 , C07D413/04 , C07D413/10 , C07D471/04 , C07D495/04 , A61K2300/00
摘要： The present invention relates to compounds of formula (I): and to salts thereof, wherein A has any of the values defined in the specification, 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.
摘要翻译：本发明涉及式（I）的化合物及其盐，其中A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，以及在治疗各种CBP和/或EP300介导的病症中使用这些化合物和盐的方法。

3. 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。

4. 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.

5. 发明申请

WO2016123387A1 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：WO2016123387A1
公开(公告)日：2016-08-04
申请号：PCT/US2016/015440
申请日：2016-01-28
申请人： GENENTECH, INC. , CONSTELLATION PHARMACEUTICALS, INC.
发明人： ALBRECHT, Brian, K. , AUDIA, James, Edmund , COTE, Alexandre , DUPLESSIS, Martin , GEHLING, Victor, S. , GOOD, Andrew, Charles , HARMANGE, Jean-Christophe , LEBLANC, Yves , NASVESCHUK, Christopher, G. , TAYLOR, Alexander, M. , VASWANI, Rishi, G.
IPC分类号： C07D231/12 , C07D401/12 , C07C211/42 , C07D405/12 , C07D211/78 , C07D213/38 , A61K31/00 , A61P35/00
CPC分类号： C07C211/42 , A61K31/135 , A61K31/166 , A61K31/196 , A61K31/277 , A61K31/337 , A61K31/351 , A61K31/397 , A61K31/40 , A61K31/415 , A61K31/4155 , A61K31/437 , A61K31/4406 , A61K31/445 , A61K31/4545 , A61K31/4747 , A61K31/495 , A61K31/517 , A61K45/06 , C07C217/74 , C07C229/50 , C07C237/48 , C07C255/58 , C07C317/36 , C07C2601/02 , C07C2601/04 , C07C2603/94 , C07D205/04 , C07D205/12 , C07D207/06 , C07D211/26 , C07D211/46 , C07D211/78 , C07D213/38 , C07D215/08 , C07D231/12 , C07D295/185 , C07D305/08 , C07D309/04 , C07D401/12 , C07D405/12
摘要： Provided herein are compounds of formula I: and salts thereof and compositions and uses thereof. The compounds are useful as inhibitors of LSD1. 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 LSD1-mediated disorders.
摘要翻译：本文提供式I化合物及其盐及其组合物和用途。该化合物可用作LSD1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LSD1介导的病症中使用这些化合物和盐的方法。

6. 发明申请

WO2016077380A1 SUBSTITUTED PYRROLOPYRIDINES AS INHIBITORS OF BROMODOMAIN 审中-公开
标题翻译：取代的吡咯烷酮作为BROMODOMAIN的抑制剂
公开(公告)号：WO2016077380A1
公开(公告)日：2016-05-19
申请号：PCT/US2015/060007
申请日：2015-11-10
申请人： GENENTECH, INC. , CONSTELLATION PHARMACEUTICALS, INC.
发明人： ALBRECHT, Brian, K. , BELLON, Steven, F. , BURDICK, Daniel, J. , COTE, Alexandre , CRAWFORD, Terry , DAKIN, Les, A. , HEWITT, Michael, Charles , HSIAO-WEI TSUI, Vickie , LEBLANC, Yves , MAGNUSON, Steven, R. , NASVESCHUK, Christopher, G. , ROMERO, F. Anthony , TANG, Yong , TAYLOR, Alexander, M. , WANG, Shumei
IPC分类号： C07D471/04 , A61K31/407 , A61P35/00 , A61P37/00 , C07D519/00
CPC分类号： C07D471/04 , A61K31/437 , A61K31/4545 , A61K31/496 , A61K31/4985 , A61K45/06 , C07D519/00
摘要： The present invention relates to compounds of formula (I) and to salts thereof, wherein R 1 , R 2 , and Q have any of the values defined in the specification, and compositions and uses thereof. The compounds are useful as inhibitors of bromodomains. 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 bromodomain-mediated disorders.
摘要翻译：本发明涉及式（I）化合物及其盐，其中R 1，R 2和Q具有说明书中定义的任何值及其组成和用途。该化合物可用作溴结构域的抑制剂。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，以及在治疗各种溴结构域介导的病症中使用这些化合物和盐的方法。

7. 发明申请

WO2016077375A1 BROMODOMAIN INHIBITORS AND USES THEREOF 审中-公开
标题翻译： BROMODOMAIN抑制剂及其用途
公开(公告)号：WO2016077375A1
公开(公告)日：2016-05-19
申请号：PCT/US2015/059997
申请日：2015-11-10
申请人： GENENTECH, INC. , CONSTELLATION PHARMACEUTICALS, INC.
发明人： ALBRECHT, Brian, K. , BELLON, Steven, F. , BURDICK, Daniel, J. , COTE, Alexandre , CRAWFORD, Terry , DAKIN, Les, A. , HSIAO-WEI TSUI, Vickie , HEWITT, Michael, Charles , LEBLANC, Yves , MAGNUSON, Steven, R. , NASVESCHUK, Christopher, G. , ROMERO, F., Anthony , TANG, Yong , TAYLOR, Alexander, M. , WANG, Shumei
IPC分类号： C07D471/04 , C07D519/00
CPC分类号： A61K31/40 , C07D471/04 , C07D519/00
摘要： The present invention relates to compounds of formula (I): [INSERT FORMULA (1)] and to salts thereof, wherein R 1 , R 2 , R c , and R d have any of the values defined in the specification, and compositions and uses thereof. The compounds are useful as inhibitors of bromodomains. 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 bromodomain-mediated disorders.
摘要翻译：本发明涉及式（I）化合物：[嵌段式（1）]及其盐，其中R 1，R 2，R c和R d具有本说明书中定义的任何值及其组成和用途。该化合物可用作溴结构域的抑制剂。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，以及在治疗各种溴结构域介导的病症中使用这些化合物和盐的方法。

8. 发明申请

WO2016036954A1 PHTHALAZINE DERIVATIVES OF FORMULA (I) AS PCAF AND GCN5 INHIBITORS FOR USE IN THE TREATMENT OF CANCER 审中-公开
标题翻译：公式（I）作为PCFA和GCN5抑制剂用于治疗癌症的苯乙胺衍生物
公开(公告)号：WO2016036954A1
公开(公告)日：2016-03-10
申请号：PCT/US2015/048354
申请日：2015-09-03
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 , C07D401/12 , C07D237/32 , C07D471/04 , C07D487/04 , A61K31/502 , A61K31/5025 , A61P35/00 , A61P31/18 , A61P11/06 , A61P19/10 , A61P33/00
CPC分类号： C07D487/04 , A61K31/502 , A61K31/5025 , A61K31/5377 , A61K31/55 , C07D237/32 , C07D237/34 , C07D401/12 , C07D403/12 , C07D405/12 , C07D471/04
摘要： The present invention relates to methods for treating PCAF and GCN5 mediated disorders using a compound of formula (I) or a pharmaceutically acceptable salt thereof: wherein ring A, R 1, R 3 , R 4 , R 5 , 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：本发明涉及使用式（I）化合物或其药学上可接受的盐治疗PCAF和GCN5介导的病症的方法：其中环A，R 1，R 3，R 4，R 5和每个Re具有以下定义的任何值规格。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。

9. 发明申请

WO2016112298A1 PYRIDAZINONE DERIVATIVES AND THEIR USE IN THE TREATMENT OF CANCER 审中-公开
标题翻译：吡咯烷酮衍生物及其在治疗癌症中的用途
公开(公告)号：WO2016112298A1
公开(公告)日：2016-07-14
申请号：PCT/US2016/012659
申请日：2016-01-08
申请人： GENENTECH, INC. , CONSTELLATION PHARMACEUTICALS, INC.
发明人： ALBRECHT, Brian, K. , BURDICK, Daniel, J. , COTE, Alexandre , DUPLESSIS, Martin , NASVESCHUK, Christopher, G. , TAYLOR, Alexander, M.
IPC分类号： C07D403/12 , C07D401/14 , C07D405/14 , C07D413/14 , C07D401/12 , C07D405/12 , A61K31/501 , A61P35/00
CPC分类号： C07D401/12 , A61K31/501 , A61K31/55 , A61K45/06 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D413/14 , C07D451/04
摘要： The invention relates to compounds of formula (I) and salts thereof: wherein R 1 -R 3 have any of the values defined in the specification. The compounds and salts are useful for treating PCAF mediated disorders and/or GCN5 mediated disorders. The invention also provides pharmaceutical compositions comprising a compound of formula (I), or a pharmaceutically acceptable salt thereof, as well as and methods of using said compounds, salts, or compositions in the treatment of various disorders.
摘要翻译：本发明涉及式（I）化合物及其盐：其中R1-R3具有说明书中定义的任何值。化合物和盐可用于治疗PCAF介导的病症和/或GCN5介导的病症。本发明还提供包含式（I）化合物或其药学上可接受的盐的药物组合物，以及使用所述化合物，盐或组合物治疗各种疾病的方法。

10. 发明申请

WO2016112284A1 (PIPERIDIN-3-YL)(NAPHTHALEN-2-YL)METHANONE DERIVATIVES AND RELATED COMPOUNDS AS INHIBITORS OF THE HISTONE DEMETHYLASE KDM2B FOR THE TREATMENT OF CANCER 审中-公开
标题翻译：（PIPERIDIN-3-YL）（萘-2-炔）甲酮衍生物及其相关化合物作为用于治疗癌症的组蛋白脱乙酰酶KDM2B的抑制剂
公开(公告)号：WO2016112284A1
公开(公告)日：2016-07-14
申请号：PCT/US2016/012638
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. , PASTOR, Richard , ROMERO, F. Anthony , TAYLOR, Alexander, M. , ZHANG, Birong
IPC分类号： C07D401/06 , C07D405/06 , C07D409/06 , C07D413/06 , C07D241/04 , C07D211/30 , A61K31/44 , A61K31/444 , A61K31/4439 , A61K31/4433 , A61K31/4436 , A61K31/495 , A61P35/00 , A61P35/02 , A61P31/04
CPC分类号： C07D401/06 , C07D211/30 , C07D241/04 , C07D405/06 , C07D409/06 , C07D413/06
摘要： The present invention relates to (piperidin-3-yl)(naphthalen-2-yl) methanone derivatives and related compounds 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 discloses methods of using said compositions in the treatment of cancer, such as lung cancer, leukemia or lymphoma.
摘要翻译：本发明涉及（哌啶-3-基）（萘-2-基）甲酮衍生物和相关化合物作为一种或多种组蛋白脱甲基酶如KDM2b的抑制剂。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，并公开了使用所述组合物治疗癌症（例如肺癌，白血病或淋巴瘤）的方法。

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