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1. 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。

2. 发明申请

WO2016057924A1 PYRROLIDINE AMIDE COMPOUNDS AS HISTONE DEMETHYLASE INHIBITORS 审中-公开
标题翻译：吡咯烷酰胺化合物作为HISTONE DEMETHYLASE抑制剂
公开(公告)号：WO2016057924A1
公开(公告)日：2016-04-14
申请号：PCT/US2015/054949
申请日：2015-10-09
申请人： GENENTECH, INC. , CONSTELLATION PHARMACEUTICALS, INC. , LAI, Kwong Wah
发明人： LAI, Kwong Wah , LIANG, Jun , ZHANG, Birong , LABADIE, Sharada , ORTWINE, Daniel , DRAGOVICH, Peter , KIEFER, James , GEHLING, Victor, S. , HARMANGE, Jean-Christophe
IPC分类号： C07D401/14 , C07D405/14 , C07D403/06 , C07D403/14 , A61K31/4178 , A61K31/4155 , A61P35/00
CPC分类号： A61K31/41 , A61K31/4025 , C07D207/04 , C07D237/04 , C07D401/14 , C07D403/06 , C07D403/14 , C07D405/14
摘要： The present invention relates to compounds of formula (I) useful as inhibitors of one or more histone demethylses, such as KDM5. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and the compounds for use in methods for the treatment of various disorders. Formula (I): or a salt thereof, wherein: A is selected from the group consisting of:
摘要翻译：本发明涉及可用作一种或多种组蛋白脱甲基酶抑制剂的式（I）化合物，例如KDM5。本发明还提供包含本发明化合物和用于治疗各种疾病的方法的化合物的药学上可接受的组合物。式（I）：或其盐，其中：A选自：

3. 发明申请

WO2015035062A1 ANTIPROLIFERATIVE COMPOUNDS 审中-公开
标题翻译：抗生素化合物
公开(公告)号：WO2015035062A1
公开(公告)日：2015-03-12
申请号：PCT/US2014/054114
申请日：2014-09-04
申请人： GENENTECH, INC. , CONSTELLATION PHARMACEUTICALS, INC.
发明人： ALBRECHT, Brian, K. , BELLON, Steven, F. , GEHLING, Victor, S. , HARMANGE, Jean-Christophe , LEBLANC, Yves , LIANG, Jun , MAGNUSON, Steven , TSUI, Vickie , ZHANG, Birong
IPC分类号： A61K31/519 , A61P35/00
CPC分类号： C07D487/04 , A61K31/519 , A61K45/06 , A61N5/10
摘要： The present invention relates to compounds formula (I) and to salts thereof, wherein R 1 -R 4 and A have any of the values defined in the specification, and compositions and uses thereof. The compounds are useful as inhibitors of histone demethylases, such as KDM5. Also included are pharmaceutically acceptable compositions comprising the 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）化合物及其盐，其中R 1 -R 4和A具有说明书中定义的任何值，以及其组成和用途。该化合物可用作组蛋白脱甲基酶的抑制剂，例如KDM5。还包括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。

4. 发明申请

WO2014139326A1 PYRAZOLO COMPOUNDS AND USES THEREOF 审中-公开
标题翻译：吡咯化合物及其用途
公开(公告)号：WO2014139326A1
公开(公告)日：2014-09-18
申请号：PCT/CN2014/000262
申请日：2014-03-13
申请人： GENENTECH, INC. , CONSTELLATION PHARMACEUTICALS, INC. , ALBRECHT, Brian K. , BELLON, Steven F. , GEHLING, Victor S. , HARMANGE, Jean-Christophe , LAI, Tommy , LIANG, Jun , DRAGOVICH, Peter , ORTWINE, Dan , LABADIE, Sharada , ZHANG, Birong , KIEFER, Jim
发明人： ALBRECHT, Brian K. , BELLON, Steven F. , GEHLING, Victor S. , HARMANGE, Jean-Christophe , LAI, Tommy , LIANG, Jun , DRAGOVICH, Peter , ORTWINE, Dan , LABADIE, Sharada , ZHANG, Birong , KIEFER, Jim
IPC分类号： C07D487/04 , A61K31/519 , A61P35/04
CPC分类号： C07D487/04 , A61K31/337 , A61K31/437 , A61K31/517 , A61K31/519 , A61K31/5377 , A61K45/06 , C07D487/14 , C07D498/04 , C12N9/99
摘要： Provided are compounds useful as inhibitors of one or more histone demethylses, such as KDM5. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using the present composition in the treatment of various disorders.
摘要翻译：提供了可用作一种或多种组蛋白去甲基化酶抑制剂的化合物，例如KDM5。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本发明组合物治疗各种疾病的方法。

5. 发明申请

WO2015135094A1 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：WO2015135094A1
公开(公告)日：2015-09-17
申请号：PCT/CN2014/000261
申请日：2014-03-13
申请人： GENENTECH, INC. , CONSTELLATION PHARMACEUTICALS, INC. , ALBRECHT, Brian K. , GEHLING, Victor S. , HARMANGE, Jean-Christophe , LAI, Tommy , LIANG, Jun , DRAGOVICH, Peter , ORTWINE, Dan , LABADIE, Sharada , ZHANG, Birong , KIEFER, Jim
发明人： ALBRECHT, Brian K. , GEHLING, Victor S. , HARMANGE, Jean-Christophe , LAI, Tommy , LIANG, Jun , DRAGOVICH, Peter , ORTWINE, Dan , LABADIE, Sharada , ZHANG, Birong , KIEFER, Jim
IPC分类号： C07D487/04 , A61P35/00 , A61K31/4162
CPC分类号： C07D487/04 , A61K31/337 , A61K31/519 , A61K45/06 , A61K2300/00
摘要： The present invention relates to compounds useful as inhibitors of one or more histone demethylses, such as KDM5. 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：本发明涉及可用作一种或多种组蛋白去甲基化酶抑制剂的化合物，例如KDM5。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。

6. 发明申请

WO2014144850A1 METHODS OF TREATING CANCER AND PREVENTING CANCER DRUG RESISTANCE 审中-公开
标题翻译：治疗癌症和预防癌症药物耐药性的方法
公开(公告)号：WO2014144850A1
公开(公告)日：2014-09-18
申请号：PCT/US2014/029432
申请日：2014-03-14
申请人： GENENTECH, INC. , CONSTELLATION PHARMACEUTICALS, INC. , ARORA, Shilpi , COSTA, Michael, Robert , LAU, Ted , TROJER, Patrick
发明人： ARORA, Shilpi , COSTA, Michael, Robert , LAU, Ted , TROJER, Patrick , ALBRECHT, Brian, K. , BUKER, Shane , CLASSON, Marie , GEHLING, Victor, S. , HARMANGE, Jean-christophe , JACKSON, Erica, L. , LIANG, Jun , PHILLIPS, Heidi , SANDY, Peter , SETTLEMAN, Jeffrey , STEPHAN, Jean-philippe
IPC分类号： A61K39/395 , A61K31/4353 , A61K31/337 , A61K45/06 , A61K33/24 , A61K31/517 , A61K31/437 , A61K31/7088 , A61P31/00
CPC分类号： A61K31/519 , A61K31/337 , A61K31/437 , A61K31/517 , A61K31/555 , A61K31/713 , A61K33/24 , A61K45/06 , C12N15/113 , C12N2310/14 , C12N2310/531 , A61K2300/00
摘要： Provided herein are methods of treating and/or preventing cancer drug resistance using antagonists of KDM5.
摘要翻译：本文提供使用KDM5拮抗剂治疗和/或预防癌症耐药性的方法。

7. 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。

9. 发明公开

EP3242875A1 4,5-DIHYDROIMIDAZOLE DERIVATIVES AND THEIR USE AS HISTONE DEMETHYLASE (KDM2B) INHIBITORS 有权
标题翻译： 4,5-二氢咪唑衍生物及其作为组蛋白激酶二甲基化酶（KDM2B）抑制剂的用途
公开(公告)号：EP3242875A1
公开(公告)日：2017-11-15
申请号：EP16702999.0
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 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.

10. 发明公开

EP3041474A1 ANTIPROLIFERATIVE COMPOUNDS 有权
标题翻译：抗增殖CONNECTIONS
公开(公告)号：EP3041474A1
公开(公告)日：2016-07-13
申请号：EP14766355.3
申请日：2014-09-04
申请人： Genentech, Inc. , Constellation Pharmaceuticals, Inc.
发明人： ALBRECHT, Brian, K. , BELLON, Steven, F. , GEHLING, Victor, S. , HARMANGE, Jean-Christophe , LEBLANC, Yves , LIANG, Jun , MAGNUSON, Steven, R. , TSUI, Vickie, Hsiao-Wei , ZHANG, Birong
IPC分类号： A61K31/519 , A61P35/00
摘要： The present invention relates to compounds formula (I): and to salts thereof, wherein R1-R4 and A have any of the values defined in the specification, and compositions and uses thereof. The compounds are useful as inhibitors of histone demethylases, such as KDM5. Also included are pharmaceutically acceptable compositions comprising the compounds of the present invention and methods of using said compositions in the treatment of various disorders.

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