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1. 发明申请

WO2010002779A3 NAPHTHYRIDININONES AS AURORA KINASE INHIBITORS 审中-公开
标题翻译：萘啶类化合物作为AURORA激酶抑制剂
公开(公告)号：WO2010002779A3
公开(公告)日：2011-03-03
申请号：PCT/US2009049035
申请日：2009-06-29
申请人： MERCK PATENT GMBH , XIAO YUFANG , CHEN XIAOLING , KARRA SRINIVASA R , HUCK BAYARD R , SUTTON AMANDA E , GOUTOPOULOS ANDREAS
发明人： XIAO YUFANG , CHEN XIAOLING , KARRA SRINIVASA R , HUCK BAYARD R , SUTTON AMANDA E , GOUTOPOULOS ANDREAS
IPC分类号： C07D471/04 , A61K31/436 , A61P35/00
CPC分类号： C07D471/04 , A61K31/436 , A61K45/06 , A61K2300/00
摘要： Naphthyridinone derivative compounds that inhibit Aurora kinase enzymes are disclosed along with pharmaceutical compositions comprising these compounds and methods for synthesizing the same. Such compounds have utility in the treatment of proliferative diseases resulting from unregulated and/or disturbed Aurora kinases such as cancers, psoriasis, viral and bacterial infections, inflammatory and autoimmune diseases.
摘要翻译：公开了抑制极光激酶的萘吡啶酮衍生物化合物以及包含这些化合物的药物组合物及其合成方法。这些化合物可用于治疗由不规则和/或扰乱的极光激酶如癌症，牛皮癣，病毒和细菌感染，炎性和自身免疫性疾病引起的增殖性疾病。

2. 发明专利

SG11202100818RA TLR7/8 ANTAGONISTS AND USES THEREOF 未知
公开(公告)号：SG11202100818RA
公开(公告)日：2021-02-25
申请号：SG11202100818R
申请日：2019-07-29
申请人： MERCK PATENT GMBH
发明人： SHERER BRIAN , LAN RUOXI , BRUGGER NADIA , CHEN XIAOLING , TOURE MOMAR , CLEARY ESTHER , DESELM LIZBETH CELESTE , WANG YANPING
IPC分类号： C07D401/04 , A61K31/519 , A61P35/00 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D471/04 , C07D471/10 , C07D495/10
摘要： Compounds of Formula (I) and pharmaceutically acceptable compositions thereof are useful as TLR7/8 antagonists.

3. 发明专利

CA3127475A1 PYRIMIDINONE DERIVATIVES AS SHP2 ANTAGONISTS 未知
公开(公告)号：CA3127475A1
公开(公告)日：2020-10-15
申请号：CA3127475
申请日：2020-04-08
申请人： MERCK PATENT GMBH
发明人： JORAND-LEBRUN CATHERINE , BOIVIN ROCH , JOHNSON THERESA , WANG YANPING , XIAO YUFANG , CHEN XIAOLING , LINDE NINA , MUSCH DOREEN , KUMAR DEEPAK
IPC分类号： A61K31/506 , A61P35/00 , C07D239/22 , C07D401/04 , C07D403/04 , C07D491/107
摘要： The invention relates to pyrimidinone derivatives of the general Formula (II), or a pharmaceutically acceptable salt thereof, the use of the compounds of the present invention for the treatment of hyperproliferative diseases and disorders in mammals, especially humans, and pharmaceutical compositions containing such compound.

4. 发明专利

CA2844704C AMINOPYRIMIDINE DERIVATIVES FOR USE AS MODULATORS OF KINASE ACTIVITY 未知
公开(公告)号：CA2844704C
公开(公告)日：2020-04-28
申请号：CA2844704
申请日：2012-09-12
申请人： MERCK PATENT GMBH
发明人： LAN RUOXI , HUCK BAYARD R , CHEN XIAOLING , DESELM LIZBETH CELESTE , XIAO YUFANG , QIU HUI , NEAGU CONSTANTIN , MOCHALKIN IGOR , JOHNSON THERESA L
IPC分类号： C07D239/48 , A61K31/506 , A61P35/00 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D405/14 , C07D413/04 , C07D413/14 , C07D417/14
摘要： The invention provides novel heterocyclic amine compounds accord¬ ing to Formula (I) and their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.

5. 发明专利

ES2746756T3 Derivados de 6-[4-(1H-imidazol-2-il)piperidin-1-il]pirimidin-4-amina como moduladores de la actividad cinasa 未知
公开(公告)号：ES2746756T3
公开(公告)日：2020-03-06
申请号：ES14715758
申请日：2014-03-10
申请人： MERCK PATENT GMBH
发明人： LAN RUOXI , CHEN XIAOLING , XIAO YUFANG , HUCK BAYARD R , GOUTOPOULOS ANDREAS
IPC分类号： C07D401/14 , A61K31/506 , A61P35/00
摘要： Compuesto seleccionado del grupo que consiste en: 4-amino-6-{3,4-cis-4-[1-(2-azetidin-1-il-etil)-4-(4-fluoro-3-trifluorometil-fenil)-1H-imidazol-2-il]-3-fluoropiperidin-1-il}- pirimidin-5-carbonitrilo (racémico) ("1"); 4-amino-6-{3,4-cis-4-[1-(2-azetidin-1-il-etil)-4-(4-fluoro-3-trifluorometil-fenil)-1H-imidazol-2-il]-3-fluoropiperidin-1-il}- pirimidin-5-carboxamida (racémica) ("2"); 4-amino-6-[(3R,4S)-4-[1-[2-(azetidin-1-il)etil]-4-[4-fluoro-3-(trifluorometil)fenil]imidazol-2-il]-3-fluoro-1- piperidil]pirimidin-5-carboxamida (quiral) ("3"); 4-amino-6-[(3S,4R)-4-[1-[2-(azetidin-1-il)etil]-4-[4-fluoro-3-(trifluorometil)fenil]imidazol-2-il]-3-fluoro-1- piperidil]pirimidin-5-carboxamida (quiral) ("4"); 4-amino-6-{3,4-cis-4-[1-(2-azetidin-1-il-etil)-4-(4-fluoro-3-trifluorometil-fenil)-1H-imidazol-2-il]-3-metil-piperidin-1-il}- pirimidin-5-carbonitrilo (racémico) ("5"); 4-amino-6-{3,4-cis-4-[1-(2-azetidin-1-il-etil)-4-(4-fluoro-3-trifluorometil-fenil)-1H-imidazol-2-il]-3-metil-piperidin-1-il}- pirimidin-5-carboxamida (racémica) ("6"); 4-amino-6-{3,4-trans-4-[1-(2-azetidin-1-il-etil)-4-(4-fluoro-3-trifluorometil-fenil)-1H-imidazol-2-il]-3-fluoro-piperidin-1-il}- pirimidin-5-carbonitrilo (racémico) ("7"); 4-amino-6-{3,4-trans-4-[1-(2-azetidin-1-il-etil)-4-(4-fluoro-3-trifluorometil-fenil)-1H-imidazol-2-il]-3-fluoro-piperidin-1-il}- pirimidin-5-carboxamida (racémica) ("8"); 4-amino-6-{3,4-cis-4-[1-(2-dimetilaminoetil)-4-(4-fluoro-3-metil-fenil)imidazol-2-il]-3-fluoro-1-piperidil]}-pirimidin-5- carbonitrilo (racémico) ("9"); 6-{3,4-cis-4-[1-(2-azetidin-1-il-etil)-4-(4-fluoro-3-trifluorometil-fenil)-1H-imidazol-2-il]-3-fluoro-piperidin-1-il}-5-cloropirimidin- 4-ilamina (racémica) ("10"); 6-{3,4-trans-4-[1-(2-azetidin-1-il-etil)-4-(4-fluoro-3-trifluorometil-fenil)-1H-imidazol-2-il]-3-fluoro-piperidin-1-il}-5-cloropirimidin- 4-ilamina (racémica) ("11"); 5-cloro-6-{3,4-cis--4-[1-(2-dimetilamino-etil)-4-(4-fluoro-3-metil-fenil)-1H-imidazol-2-il]-3-fluoro-piperidin-1-il}-pirimidin- 4-ilamina (racémica) ("12"); 6-{3,4-cis-4-[1-(2-azetidin-1-il-etil)-4-(4-fluoro-3-trifluorometil-fenil)-1H-imidazol-2-il]-3-fluoro-piperidin-1-il}-5-etilpirimidin- 4-ilamina (racémica) ("13"); 4-amino-6-{3,4-cis-4-[1-(2-dimetilamino-etil)-4-(4-fluoro-3-trifluorometil-fenil)-1H-imidazol-2-il]-3-fluoro-piperidin-1-il}- pirimidin-5-carbonitrilo (racémico) ("14"); 4-amino-6-{3,4-cis-4-[1-(2-dimetilamino-etil)-4-(4-fluoro-3-trifluorometil-fenil)-1H-imidazol-2-il]-3-fluoro-piperidin-1-il}- pirimidin-5-carbonitrilo (racémico) ("15"); 6-{3,4-cis-4-[1-(2-azetidin-1-il-etil)-4-(4-fluoro-3-trifluorometil-fenil)-1H-imidazol-2-il]-3-fluoro-piperidin-1-il}-5-etoxipirimidin- 4-ilamina (racémica) ("16"), o sales farmacéuticamente aceptables, solvatos o solvatos de sales del mismo.

6. 发明专利

IL272016D0 Pyrrolidine derivatives and their use as tlr7/8 antagonists 未知
公开(公告)号：IL272016D0
公开(公告)日：2020-02-27
申请号：IL27201620
申请日：2020-01-13
申请人： BRUGGER NADIA , MERCK PATENT GMBH , LAN RUOXI , CHEN XIAOLING , SHERER BRIAN A
发明人： BRUGGER NADIA , LAN RUOXI , CHEN XIAOLING , SHERER BRIAN A
IPC分类号： A61P20060101
摘要： Compounds of Formula I and pharmaceutically acceptable compositions thereof, useful as TLR7/8 antagonists, are described herein.

7. 发明专利

NZ706418A Azaquinazoline carboxamide derivatives 未知
公开(公告)号：NZ706418A
公开(公告)日：2019-09-27
申请号：NZ70641813
申请日：2013-11-27
申请人： MERCK PATENT GMBH
发明人： JOHNSON THERESA L , HUCK BAYARD R , LAN RUOXI , POTNICK JUSTIN , DESELM LIZBETH CELESTE , CRONIN MARK W , CHEN XIAOLING , BOIVIN ROCH , GOUTOPOULOS ANDREAS , NEAGU CONSTANTIN
IPC分类号： C07D403/12 , A61K31/519 , A61K31/53 , A61P35/00 , C07D253/08 , C07D401/12 , C07D471/04
摘要： Novel azaquinazoline carboxamide derivatives of formula (I) wherein each W1, W2, W3, W4 is independently N or CH, wherein at least one of W1, W2, W3 or W4 is N and R1, R2, R3 and m are as defined herein, are p70S6K inhibitor, and can be employed, inter alia, for the treatment of hyperproliferative disorders.

8. 发明专利

CA2844830C NOVEL IMIDAZOLE AMINES AS MODULATORS OF KINASE ACTIVITY 未知
公开(公告)号：CA2844830C
公开(公告)日：2019-09-10
申请号：CA2844830
申请日：2012-09-12
申请人： MERCK PATENT GMBH
发明人： HUCK BAYARD R , CHEN XIAOLING , XIAO YUFANG , LAN RUOXI , DESELM LIZBETH CELESTE , QIU HUI , NEAGU CONSTANTIN , BANKSTON DONALD , JONES CHRISTOPHER CHARLES VICTOR
IPC分类号： C07D401/14 , A61K31/506
摘要： The invention provides novel imidazole amine compounds according to Formula (I) and Formula (II) their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.

9. 发明专利

AU2017239625B2 Novel heterocyclic carboxamides as modulators of kinase activity 未知
公开(公告)号：AU2017239625B2
公开(公告)日：2019-07-11
申请号：AU2017239625
申请日：2017-10-06
申请人： MERCK PATENT GMBH
发明人： HUCK BAYARD R , CHEN XIAOLING , XIAO YUFANG , LAN RUOXI , DE SELM LIZBETH CELESTE , NEAGU CONSTANTIN , POTNICK JUSTIN , KARRA SRINIVASA R , JOHNSON THERESA L
IPC分类号： C07D215/48 , A61K31/4709 , A61K31/517 , A61P35/00 , C07D239/74 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12
摘要： V I Il:U1 U6 VPC Abstract The invention provides novel heterocyclic carboxamide compounds compounds according to Formula (1) their manufacture and use for the treatment of hyperproliferative 5 diseases, such as cancer.

10. 发明专利

SG10201900954SA Heterocycles as Modulators of Kinase Activity 未知
公开(公告)号：SG10201900954SA
公开(公告)日：2019-02-27
申请号：SG10201900954S
申请日：2014-03-10
申请人： MERCK PATENT GMBH
发明人： LAN RUOXI , CHEN XIAOLING , XIAO YUFANG , HUCK BAYARD R , GOUTOPOULOS ANDREAS
摘要： Heterocycles as Modulators of Kinase Activity The invention provides novel heterocyclic amines according to Formula (I) their manufacture and use for the treatment of hyperproliferative diseases, such as cancer. (I)

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