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1. 发明申请

WO2012101065A3 PYRIMIDINE BIARYL AMINE COMPOUNDS AND THEIR USE AS CDK9 INHIBITORS 审中-公开
标题翻译：吡嗪二胺化合物及其作为CDK9抑制剂使用
公开(公告)号：WO2012101065A3
公开(公告)日：2013-01-10
申请号：PCT/EP2012050909
申请日：2012-01-20
申请人： NOVARTIS AG , ANTONIOS-MCCREA WILLIAM R , BARSANTI PAUL A , HU CHENG , JIN XIANMING , LIN XIAODONG , MARTIN ERIC J , PAN YUE , PFISTER KEITH B , RENHOWE PAUL A , SENDZIK MARTIN , SUTTON JAMES , WAN LIFENG
发明人： ANTONIOS-MCCREA WILLIAM R , BARSANTI PAUL A , HU CHENG , JIN XIANMING , LIN XIAODONG , MARTIN ERIC J , PAN YUE , PFISTER KEITH B , RENHOWE PAUL A , SENDZIK MARTIN , SUTTON JAMES , WAN LIFENG
IPC分类号： C07D401/04 , A61K31/444 , A61K31/506 , A61P35/00 , C07D401/14 , C07D403/04 , C07D405/14 , C07D409/14 , C07D413/14
CPC分类号： C07D401/04 , C07D401/14 , C07D403/04 , C07D405/14 , C07D409/14 , C07D413/14
摘要： The present invention provides a pyrimidine compound of formula (I): wherein one of X and Y but not both is N, and pharmaceutically acceptable salts, enantiomers, stereoisomers, rotamers, tautomers, diastereomers, deuterated versions, or racemates thereof. These compounds inhibit the activity of CDK9 and are thus useful as pharmaceuticals. Also provided are methods of treating a disease or condition mediated by CDK9 using the compounds of Formula I and isomers thereof, and pharmaceutical compositions comprising such compounds.
摘要翻译：本发明提供式（I）的嘧啶化合物：其中X和Y之一，但不是二者均为N，以及其药学上可接受的盐，对映异构体，立体异构体，旋转异构体，互变异构体，非对映异构体，氘化形式或其外消旋体。这些化合物抑制CDK9的活性，因此可用作药物。还提供了使用式I化合物及其异构体治疗由CDK9介导的疾病或病症的方法，以及包含这些化合物的药物组合物。

2. 发明申请

WO2011026911A8 BIPYRIDINES USEFUL FOR THE TREATMENT OF PROLIFERATIVE DISEASES 审中-公开
标题翻译：联吡啶类用于治疗增殖性疾病
公开(公告)号：WO2011026911A8
公开(公告)日：2011-04-21
申请号：PCT/EP2010062893
申请日：2010-09-02
申请人： NOVARTIS AG , BARSANTI PAUL A , HU CHENG , JIN XIANMING , NG SIMON C , PFISTER KEITH B , SENDZIK MARTIN , SUTTON JAMES
发明人： BARSANTI PAUL A , HU CHENG , JIN XIANMING , NG SIMON C , PFISTER KEITH B , SENDZIK MARTIN , SUTTON JAMES
IPC分类号： C07D401/04 , A61K31/444 , A61P35/00 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14
CPC分类号： C07D401/14 , C07D401/04 , C07D405/14 , C07D409/14 , C07D413/14
摘要： The present invention provides compounds of Formula (I): and pharmaceutically acceptable salts thereof. Also provided is a method of using a compound of Formula I for treating a disease or condition mediated by a CDK inhibitor.
摘要翻译：本发明提供了式（I）的化合物：及其药学上可接受的盐。还提供了使用式I化合物治疗由CDK抑制剂介导的疾病或病症的方法。

3. 发明申请

WO2004018419B1 BENZIMIDAZOLE QUINOLINONES AND USES THEREOF 审中-公开
标题翻译：苯并咪唑喹啉酮及其用途
公开(公告)号：WO2004018419B1
公开(公告)日：2004-07-29
申请号：PCT/US0325990
申请日：2003-08-19
申请人： CHIRON CORP , BARSANTI PAUL A , BUSSIERE DIRKSEN , HARRISON STEPHEN D , HEISE CARLA C , JANSEN JOHANNA M , JAZAN ELISA , MACHAJEWSKI TIMOTHY D , MCBRIDE CHRISTOPHER , MCCREA WILLIAM R , NG SIMON , NI ZHI-JIE , PECCHI SABINA , PFISTER KEITH , RAMURTHY SAVITHRI , RENHOWE PAUL A , SHAFER CYNTHIA M , SILVER JOEL B , WAGMAN ALLAN , WIESMANN MARION , WAYMAN KELLY
发明人： BARSANTI PAUL A , BUSSIERE DIRKSEN , HARRISON STEPHEN D , HEISE CARLA C , JANSEN JOHANNA M , JAZAN ELISA , MACHAJEWSKI TIMOTHY D , MCBRIDE CHRISTOPHER , MCCREA WILLIAM R , NG SIMON , NI ZHI-JIE , PECCHI SABINA , PFISTER KEITH , RAMURTHY SAVITHRI , RENHOWE PAUL A , SHAFER CYNTHIA M , SILVER JOEL B , WAGMAN ALLAN , WIESMANN MARION , WAYMAN KELLY
IPC分类号： A61K31/4375 , A61K31/4709 , A61K31/496 , A61K31/52 , A61P35/00 , C07D401/04 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D453/02 , C07D453/06 , C07D471/04 , A61K31/435
CPC分类号： C07D401/04 , A61K31/4375 , A61K31/4709 , A61K31/496 , A61K31/52 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D453/02 , C07D453/06 , C07D471/04
摘要： Methods of inhibiting various enzymes and treating various conditions are provided that include administering to a subject a compound of Structure I or IB, a pharmaceutically acceptable salt thereof, a tautomer thereof, or a pharmaceutically acceptable salt of the tautomer. Compounds having the Structure I and IB have the following structures and have the variables described herein. Such compounds may be used to prepare medicaments for use in inhibiting various enzymes and for use in treating conditions mediated by such enzymes.
摘要翻译：提供了抑制各种酶和治疗各种病症的方法，其包括向受试者施用结构I或IB的化合物，其药学上可接受的盐，其互变异构体或互变异构体的药学上可接受的盐。具有结构I和IB的化合物具有以下结构并具有本文所述的变量。这些化合物可用于制备用于抑制各种酶的药物，并用于治疗由这些酶介导的病症。

4. 发明申请

WO2004018419A3 BENZIMIDAZOLE QUINOLINONES AND USES THEREOF 审中-公开
标题翻译：苯并咪唑喹诺酮及其用途
公开(公告)号：WO2004018419A3
公开(公告)日：2004-06-03
申请号：PCT/US0325990
申请日：2003-08-19
申请人： CHIRON CORP , BARSANTI PAUL A , BUSSIERE DIRKSEN , HARRISON STEPHEN D , HEISE CARLA C , JANSEN JOHANNA M , JAZAN ELISA , MACHAJEWSKI TIMOTHY D , MCBRIDE CHRISTOPHER , MCCREA WILLIAM R , NG SIMON , NI ZHI-JIE , PECCHI SABINA , PFISTER KEITH , RAMURTHY SAVITHRI , RENHOWE PAUL A , SHAFER CYNTHIA M , SILVER JOEL B , WAGMAN ALLAN , WIESMANN MARION , WAYMAN KELLY
发明人： BARSANTI PAUL A , BUSSIERE DIRKSEN , HARRISON STEPHEN D , HEISE CARLA C , JANSEN JOHANNA M , JAZAN ELISA , MACHAJEWSKI TIMOTHY D , MCBRIDE CHRISTOPHER , MCCREA WILLIAM R , NG SIMON , NI ZHI-JIE , PECCHI SABINA , PFISTER KEITH , RAMURTHY SAVITHRI , RENHOWE PAUL A , SHAFER CYNTHIA M , SILVER JOEL B , WAGMAN ALLAN , WIESMANN MARION , WAYMAN KELLY
IPC分类号： A61K31/4375 , A61K31/4709 , A61K31/496 , A61K31/52 , A61P35/00 , C07D401/04 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D453/02 , C07D453/06 , C07D471/04 , A61K31/435
CPC分类号： C07D401/04 , A61K31/4375 , A61K31/4709 , A61K31/496 , A61K31/52 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D453/02 , C07D453/06 , C07D471/04
摘要： Methods of inhibiting various enzymes and treating various conditions are provided that include administering to a subject a compound of Structure I or IB, a pharmaceutically acceptable salt thereof, a tautomer thereof, or a pharmaceutically acceptable salt of the tautomer. Compounds having the Structure I and IB have the following structures and have the variables described herein. Such compounds may be used to prepare medicaments for use in inhibiting various enzymes and for use in treating conditions mediated by such enzymes.
摘要翻译：提供了抑制各种酶和治疗各种病症的方法，其包括向受试者施用结构I或1B的化合物，其药学上可接受的盐，其互变异构体或互变异构体的药学上可接受的盐。具有结构I和IB的化合物具有以下结构并且具有本文所述的变量。此类化合物可用于制备用于抑制各种酶的药物和用于治疗由这些酶介导的病症的药物。

5. 发明申请

WO2008086122A3 IMIDAZOLE DERIVATIVES AS KINESIN SPINDLE PROTEIN INHIBITORS (EG-5) 审中-公开
标题翻译：作为KINESIN主轴蛋白抑制剂的咪唑衍生物（EG-5）
公开(公告)号：WO2008086122A3
公开(公告)日：2008-10-16
申请号：PCT/US2008050149
申请日：2008-01-03
申请人： NOVARTIS AG , BOYCE RUSTUM , MARTIN ERIC , WANG WEIBO , YANG HONG , BARSANTI PAUL A
发明人： BOYCE RUSTUM , MARTIN ERIC , WANG WEIBO , YANG HONG , BARSANTI PAUL A
IPC分类号： C07D403/06 , A61K31/422 , A61P35/00 , C07D413/06
CPC分类号： C07D403/06 , C07D413/06
摘要： The present invention relates to new substituted imidazole compounds have the following Formula (I) and to the pharmaceutically acceptable salts, esters, or prodrugs thereof, to compositions of the compounds together with pharmaceutically acceptable carriers, and to uses of the compounds: (I).
摘要翻译：本发明涉及具有下式（I）的新的取代的咪唑化合物及其药学上可接受的盐，酯或前药与化合物与药学上可接受的载体的组合物，以及该化合物的用途：（I）。

6. 发明申请

WO2011128388A3 OXAZOLE AND THIAZOLE COMPOUNDS AS KSP INHIBITORS 审中-公开
标题翻译：氯化唑和噻唑化合物作为KSP抑制剂
公开(公告)号：WO2011128388A3
公开(公告)日：2013-03-14
申请号：PCT/EP2011055855
申请日：2011-04-13
申请人： NOVARTIS AG , BARSANTI PAUL A , DING YU , HAN WOOSEOK
发明人： BARSANTI PAUL A , DING YU , HAN WOOSEOK
IPC分类号： C07D263/32 , A61K31/421 , A61K31/422 , A61K31/426 , A61K31/427 , A61P35/00 , C07D277/28 , C07D413/12 , C07D417/12 , C07D417/14
CPC分类号： A61K31/427 , A61K31/422 , A61K31/426 , A61K31/437 , A61K45/06 , C07D263/32 , C07D277/28 , C07D413/12 , C07D417/12 , C07D417/14 , C07D471/04
摘要： Disclosed are substituted oxazole and thiazole compounds of Formula (I) or a pharmaceutically acceptable salt thereof: wherein: R1 is selecled from the group consisting of alkyl, branched alkyl, and substituted alkyl; R2 is selected from the group consisting of hydrogen, alkyl, and substituted alkyl; R3 is selected from the group consisting of -L1-A1 wherein L1 is selected from the group consisting of -C(O)-, -C(S)-, -S(O)- and -S(O)2- and A1 is selected from the group consisting, of alkyl, substituted alkyl, alkoxy, substituted alkoxy, aryl, substituted aryl, heteroaryl, substituted heteroaryl, cycloalkyl, substituted- cycloalkyl, heterocycloalkyl, substituted heterocycloalkyl;, and NR8R9; R4 is selected from the group consisting of hydrogen, alkyl substituted alkyl, alkenyl, substituted alkenyl, alkynyl, and substituted alkynyl, and optionally substituted pyrrolidinyl; or R3 and R4 together with the nitrogen atom bound thereto join to form a five to seven member heterocycloalkyl or substituted heterocycloalkyl group where optionally one carbon ring atom is selected from the group consisting of O, S, or NR11; X is Q or S; R6 is selected from the group consisting of cycloalkyl, heterocycloalkyl, aryl, and heteroaryl, all of which may be optionally substituted with -(R10)m where R10 is as defined herein, m is 1, 2, 3, or 4, and each R10 may be the same or different when m is 2, 3, or 4; R7 is -L2-A2 wherein L2 is C1-C5 aJkylene and A2 is selected from the group consisting of aryl, substituted aryl, heteroaryl, substituted heteroaryl, cycloalkyl, substituted cycloalkyl, heterocycloalkyl, and substituted heterocycloalkyl, The compounds of Formula (I) are useful for treating KSP mediated diseases, including cancer.
摘要翻译：公开了式（I）的取代的恶唑和噻唑化合物或其药学上可接受的盐：其中：R1由烷基，支链烷基和取代的烷基取代; R2选自氢，烷基和取代的烷基; R3选自-L1-A1，其中L1选自-C（O） - ， - C（S） - ， - S（O） - 和-S（O）2 - ，和 A 1选自烷基，取代的烷基，烷氧基，取代的烷氧基，芳基，取代的芳基，杂芳基，取代的杂芳基，环烷基，取代的 - 环烷基，杂环烷基，取代的杂环烷基和NR8R9。 R4选自氢，烷基取代的烷基，烯基，取代的烯基，炔基和取代的炔基，以及任选取代的吡咯烷基; 或者R 3和R 4与其结合的氮原子一起形成五至七元杂环烷基或取代的杂环烷基，其中任选一个碳环原子选自O，S或NR 11; X为Q或S; R 6选自环烷基，杂环烷基，芳基和杂芳基，其全部可以任选被 - （R 10）m取代，其中R 10如本文所定义，m为1,2,3或4，且各自为当m为2,3或4时，R10可以相同或不同; R7是-L2-A2，其中L2是C1-C5亚氨基，A2选自芳基，取代的芳基，杂芳基，取代的杂芳基，环烷基，取代的环烷基，杂环烷基和取代的杂环烷基。式（I）可用于治疗KSP介导的疾病，包括癌症。

7. 发明专利

MA29885B1 2-AMINO-7,8-DIHYDRO-6H-PYRIDO [4,3-D] PYRIMIDINE -5-ONES 未知
公开(公告)号：MA29885B1
公开(公告)日：2008-10-03
申请号：MA30873
申请日：2008-04-24
申请人： COSTALES ABRAN , RICO ALICE , BRAMMEIER NATHAN , PICK TERESA , RENHOWE PAUL A
发明人： MACHAJEWSKI TIMOTHY D , SHAFER CYNTHIA M , MCBRIDE CHRISTOPHER , ANTONIOS-MCCREA WILLIAM , DOUGHAN BRANDON M , LEVINE BARRY H , XIA YI , MCKENNA MAUREEN , WANG MICHAEL X , MENDENHALL KRIS , ZHOU YASHEEN , GONG BAOQING , GU DAN , DOLAN JOHN , TULINSKY JOHN , BRINNER KRISTIN , GAO ZHENHAI , POON DANIEL , BARSANTI PAUL A , LIN XIAODONG , COSTALES ABRAN , RICO ALICE , BRAMMEIER NATHAN , PICK TERESA , RENHOWE PAUL A
IPC分类号： C07D471/04 , A61K31/519 , A61P35/00 , C07D211/86
摘要： L'INVENTION CONCERNE DES COMPOSÉS DE 2-AMINO-7,8-DIHYDRO-6H-PYRIDO[4,3-D]PYRIMIDINE-5-ONE, LEURS STÉRÉOISOMÈRES, DES TAUTOMÈRES, DES SELS PHARMACEUTIQUEMENT ACCEPTABLES ET DES PROMÉDICAMENTS DE CEUX-CI ; DES COMPOSITIONS QUI COMPRENNENT UN SUPPORT PHARMACEUTIQUEMENT ACCEPTABLE ET UN OU PLUSIEURS DES COMPOSÉS DE 2-AMINO-7,8-DIHYDRO-6H-PYRIDO[4,3-D]PYRIMIDINE-5-ONE, SOIT SEULS, SOIT EN COMBINAISON AVEC UN OU PLUSIEURS AGENTS THÉRAPEUTIQUES SUPPLÉMENTAIRES. L'INVENTION PRÉSENTE AUSSI DES PROCÉDÉS UTILISANT LES COMPOSÉS DE 2-AMINO-7,8-DIHYDRO-6H-PYRIDO[4,3-D]PYRIMIDINE-5-ONE, SOIT SEULS, SOIT EN COMBINAISON AVEC UN OU PLUSIEURS AGENTS THÉRAPEUTIQUES SUPPLÉMENTAIRES, DANS LA PROPHYLAXIE OU LE TRAITEMENT DE MALADIES À PROLIFÉRATION CELLULAIRE, VIRALES, AUTOIMMUNES, CARDIOVASCULAIRES ET DU SYSTÈME NERVEUX CENTRAL.

8. 发明专利

JP2012158611A 2-AMINO-7,8-DIHYDRO-6H-PYRIDO[4,3-d] PYRIMIDIN-5-ONE 审中-公开
标题翻译： 2-氨基-7,8-二氢-6H-吡啶并[4,3-d]嘧啶-5-酮
公开(公告)号：JP2012158611A
公开(公告)日：2012-08-23
申请号：JP2012119613
申请日：2012-05-25
申请人： Novartis Ag , ノバルティスアーゲー
发明人： MACHAJEWSKI TIMOTHY D , SHAFER CYNTHIA M , MCBRIDE CHRISTOPHER , ANTONIOS-MCCREA WILLIAM , DOUGHAN BRANDON M , LEVINE BARRY H , XIA YI , MCKENNA MAUREEN , WANG X MICHAEL , MENDENHALL KRIS , ZHOU YASHEEN , GONG BAOQING , GU DAN , DOLAN JOHN , TULINSKY JOHN , BRINNER KRISTIN , GAO ZHENHAI , POON DANIEL , BARSANTI PAUL A , LIN XIAODONG , COSTALES ABRAN , RICO ALICE , BRAMMEIER NATHAN , PICK TERESA , RENHOWE PAUL A
IPC分类号： C07D471/04 , A61K31/282 , A61K31/337 , A61K31/404 , A61K31/4375 , A61K31/44 , A61K31/4745 , A61K31/506 , A61K31/513 , A61K31/519 , A61K31/5377 , A61K31/675 , A61K31/704 , A61K31/7068 , A61K33/24 , A61K39/395 , A61P35/00 , C07D211/86
CPC分类号： C07D211/86 , C07D471/04
摘要： PROBLEM TO BE SOLVED: To provide 2-amino-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one compounds, their tautomers, stereoisomers, pharmaceutically acceptable salts, and prodrugs thereof.SOLUTION: There are disclosed 2-amino-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one compounds, their stereoisomers, tautomers, pharmaceutically acceptable salts, and prodrugs thereof; compositions that include a pharmaceutically acceptable carrier and one or more of the 2-amino-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one compounds, either alone or in combination with at least one additional therapeutic agent. There are disclosed methods of using the 2-amino-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one compounds, either alone or in combination with at least one additional therapeutic agent, in the prophylaxis or treatment of cellular proliferative, viral, autoimmune, cardiovascular, and central nevous system diseases.
摘要翻译：待解决的问题：提供2-氨基-7,8-二氢-6H-吡啶并[4,3-d]嘧啶-5-酮化合物，其互变异构体，立体异构体，其药学上可接受的盐和前药。解决方案：公开了2-氨基-7,8-二氢-6H-吡啶并[4,3-d]嘧啶-5-酮化合物，其立体异构体，互变异构体，其药学上可接受的盐和前药; 包括药学上可接受的载体和一种或多种2-氨基-7,8-二氢-6H-吡啶并[4,3-d]嘧啶-5-酮化合物的组合物，单独或与至少一种额外的治疗剂。公开了在预防中单独使用2-氨基-7,8-二氢-6H-吡啶并[4,3-d]嘧啶-5-酮化合物或与至少一种另外的治疗剂组合使用的方法或治疗细胞增殖，病毒，自身免疫，心血管和中枢神经系统疾病。版权所有（C）2012，JPO＆INPIT

9. 发明专利

NO342258B1 2-amino-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-oner, fremgangsmåte for fremstilling derav og farmasøytiske preparater inneholdende slike 未知
公开(公告)号：NO342258B1
公开(公告)日：2018-04-30
申请号：NO20082069
申请日：2008-04-30
申请人： NOVARTIS AG
发明人： POON DANIEL J , PICK TERESA E , MCBRIDE CHRISTOPHER , RENHOWE PAUL A , MACHAJEWSKI TIMOTHY D , SHAFER CYNTHIA M , ANTONIOS-MCCREA WILLIAM , DOUGHAN BRANDON M , LEVINE BARRY H , XIA YI , MCKENNA MAUREEN , WANG X MICHAEL , MENDENHALL KRIS , ZHOU YASHEEN , GONG BAOQING , GU DAN , DOLAN JOHN , TULINSKY JOHN , BRINNER KRISTIN , GAO ZHENHAI , BARSANTI PAUL A , LIN XIAODONG , COSTALES ABRAN , RICO ALICE , BRAMMEIER NATHAN
IPC分类号： C07D471/04 , A61K31/519 , A61P35/00 , C07D211/86
摘要： Det beskrives 2-arnino-7,8-dihydro-6H-pyrido[4,3-d]pyrirnidin-5-on forbindelser, deres stereoisomerer, tautomerer, farmasøytisk akseptable salter og prodrugs derav; preparater som inkluderer en farmasøytisk akseptabel bærer og en eller flere av 2-amino-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-on forbindelsene, enten alene eller i kombinasjon med minst et ytterligere terapeutisk middel. Det beskrives videre metoder for anvendelse av 2-amino-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-on forbindelser, enten alene eller i kombinasjon med minst et ytterligere terapeutisk middel, for profylakse eller behandling av cellulære proliferative, virale, autoimmune, kardiovaskulære og sentralnervesystem sykdommer.

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