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1. 发明专利

JP2014098022A Compounds and compositions as protein kinase inhibitors 有权
标题翻译：作为蛋白激酶抑制剂的化合物和组合物
公开(公告)号：JP2014098022A
公开(公告)日：2014-05-29
申请号：JP2014021339
申请日：2014-02-06
申请人： Irm Llc , アイアールエム・リミテッド・ライアビリティ・カンパニーIrm,Llc , Novartis Ag , ノバルティスアーゲー
发明人： HUANG SHENLIN , JIN XIANMING , LIU ZUOSHENG , POON DANIEL , TELLEW JOHN E , WAN YONGQIN , WANG XING , XIE YONGPING
IPC分类号： C07D401/14 , A61K31/506 , A61K45/00 , A61K47/02 , A61K47/04 , A61K47/06 , A61K47/10 , A61K47/12 , A61K47/14 , A61K47/20 , A61K47/26 , A61K47/32 , A61K47/34 , A61K47/36 , A61K47/38 , A61K47/44 , A61P35/00 , A61P43/00 , C07D403/04 , C07D405/14
CPC分类号： C07D403/04 , A61K9/0053 , A61K31/4184 , A61K31/506 , A61K45/06 , C07D401/14 , C07D405/14 , A61K2300/00
摘要： PROBLEM TO BE SOLVED: To provide compounds for treating or preventing diseases or disorders associated with kinase activity, particularly diseases or disorders that involve abnormal activation of B-Raf.SOLUTION: The compounds are compounds of the formula Ia, tautomers thereof, or the like. [In the formula, Y is selected from N and CR6; R2, R3, R5 and R6 are independently hydrogen, halo, cyano, a C1-4 alkyl, an alkoxy, or the like; R4 is selected from -R9 and -NR10R11; R9 is a C1-6 alkyl, a C3-8 cycloalkyl, a C3-8 heterocycloalkyl, an aryl, a heteroaryl, or the like; R10 and R11 are independently selected from hydrogen and R9; and R7 is hydrogen, a C1-4 alkyl, a C3-5 cycloalkyl, or the like.]
摘要翻译：要解决的问题：提供用于治疗或预防与激酶活性相关的疾病或病症的化合物，特别是涉及B-Raf异常活化的疾病或病症。溶剂化合物是式Ia化合物，其互变异构体等。 [式中，Y选自N和CR 6; R2，R3，R5和R6独立地是氢，卤素，氰基，C1-4烷基，烷氧基等; R4选自-R9和-NR10R11; R 9是C 1-6烷基，C 3-8环烷基，C 3-8杂环烷基，芳基，杂芳基等; R 10和R 11独立地选自氢和R 9; 和R7是氢，C1-4烷基，C3-5环烷基等。]

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

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。

4. 发明专利

ME03546B JEDINJENJA IZOKSAZOL HIDROKSAMSKE KISELINE KАО INHIBIТORI LPXC 未知
公开(公告)号：ME03546B
公开(公告)日：2020-07-20
申请号：MEP2019305
申请日：2015-12-15
申请人： NOVARTIS AG
发明人： FU JIPING , JIN XIANMING , KARUR SUBRAMANIAN , LAPOINTE GUILLAUME , MADERA ANN MARIE , SWEENEY ZACHARY KEVIN
IPC分类号： A61K31/42 , C07D261/08 , C07D413/06 , C07D413/12

5. 发明专利

AU2017219216B2 Tetracyclic pyridone compounds as antivirals 未知
公开(公告)号：AU2017219216B2
公开(公告)日：2019-12-19
申请号：AU2017219216
申请日：2017-02-16
申请人： NOVARTIS AG
发明人： FU JIPING , JIN XIANMING , LEE PATRICK , LU PEICHAO , YOUNG JOSEPH MICHAEL
IPC分类号： C07D217/08 , A61K31/4745 , A61P31/12 , C07D491/14
摘要： The invention provides compounds of Formula (I) as described herein, along with pharmaceutically acceptable salts, pharmaceutical compositions containing such compounds, and methods to use these compounds, salts and compositions for treating viral infections, particularly infections caused by hepatitis B virus, and reducing the occurrence of serious conditions associated with HBV.

6. 发明专利

DK3233843T3 Isoxazol-hydraxamsyreforbindelser som LPXC-hæmmere 未知
公开(公告)号：DK3233843T3
公开(公告)日：2019-11-18
申请号：DK15816893
申请日：2015-12-15
申请人： NOVARTIS AG
发明人： FU JIPING , JIN XIANMING , KARUR SUBRAMANIAN , LAPOINTE GUILLAUME , MADERA ANN MARIE , SWEENEY ZACHARY KEVIN
IPC分类号： C07D413/06 , A61K31/42 , C07D261/08 , C07D413/12

7. 发明专利

AU2015365455B2 Isoxazole hydroxamic acid compounds as LpxC inhibitors 未知
公开(公告)号：AU2015365455B2
公开(公告)日：2019-01-17
申请号：AU2015365455
申请日：2015-12-15
申请人： NOVARTIS AG
发明人： FU JIPING , JIN XIANMING , KARUR SUBRAMANIAN , LAPOINTE GUILLAUME , MADERA ANN MARIE , SWEENEY ZACHARY KEVIN
IPC分类号： C07D413/06 , A61K31/42 , C07D261/08 , C07D413/12
摘要： This invention pertains generally to compounds of Formula I as described herein and compositions containing such compounds, as well as methods of using such compounds to treat bacterial infections. In certain aspects, the invention provides methods and compositions comprising these compounds for treating infections caused by Gram-negative bacteria.

8. 发明专利

ES2687393T3 Derivados del ácido hidroxámico de isoxazolina como inhibidores de LpxC 未知
公开(公告)号：ES2687393T3
公开(公告)日：2018-10-25
申请号：ES15721435
申请日：2015-04-22
申请人： NOVARTIS AG
发明人： FU JIPING , KARUR SUBRAMANIAN , LEE PATRICK , SWEENEY ZACHARY KEVIN , JIN XIANMING , LAPOINTE GUILLAUME
IPC分类号： C07D413/04 , A61K31/42 , A61P31/04 , C07D261/04 , C07D413/10
摘要： Un compueto de formula (I):**Fórmula** o una sal farmacéuticamente aceptable del mismo, en donde: Z es N o CR1, donde R1 se selecciona de H, halo, C1-4 alquilo y C1-4 haloalquilo; R2 y R3 se seleccionan independientemente de C1-4 alquilo y C1-4haloalquilo, R4 es H o C1-4 alquilo; X se selecciona de H, halo, C1-4 alquilo, C1-4 haloalquilo, y CN; L se selecciona de -C≡C-, -CR5>=CR6-, -O-, -S-, y un enlace directo entre A y el anillo que contiene Z; R5 y R6 se seleccionan independientemente de H, halo, C1-4 alquilo, y C1-4 haloalquilo; y A es halo, CN, o un grupo opcionalmente sustituido seleccionado de C1-4 alquilo, C3-6 cicloalquilo, fenilo, C2-6 alquenilo, C2-6 alquinilo, heteroarilo de 5-6 miembros que contiene hasta cuatro heteroátomos seleccionados de N, O y S como miembros de anillo, y heterociclilo de 4 a 6 miembros que contiene hasta dos heteroátomos seleccionados de N, O y S como miembros de anillo, en donde los C1-4 alquilo, C3-6 cicloalquilo, fenilo, C2-6 alquenilo, C2-6alquinilo, heteroarilo de 5-6 miembros que contiene hasta cuatro heteroátomos seleccionados de N, O y S como miembros de anillo, y heterociclilo de 4 a 6 miembros que contiene hasta dos heteroátomos seleccionados de N, O y S como miembros de anillo están cada uno opcionalmente sustituidos con hasta tres grupos seleccionados de halo, hidroxi, CN, R10, -(CH2)0-2OR10, -SR10, -S (O)R10,-SO2R10, -S (O) (NH)R10, y -(CH2)0-2N (R10)2; donde cada R10 es independientemente H o C1-4 alquilo opcionalmente sustituido con uno o dos grupos seleccionados de amino, hidroxi, C1-4 alcoxi, y CN; y -N (R10)2 puede representar un anillo heterocíclico de 5-6 miembros que contiene opcionalmente un heteroátomo adicional seleccionado de N, O y S como un miembro de anillo, y opcionalmente sustituido con uno o dos grupos seleccionados de oxo, halo, hidroxi, C1-4 alquilo, C1-4 alcoxi, y amino.

9. 发明专利

TN2017000207A1 ISOXAZOLE HYDROXAMIC ACID COMPOUNDS AS LPXC INHIBITORS 未知
公开(公告)号：TN2017000207A1
公开(公告)日：2018-10-19
申请号：TN2017000207
申请日：2015-12-15
申请人： NOVARTIS AG
发明人： FU JIPING , JIN XIANMING , KARUR SUBRAMANIAN , LAPOINTE GUILLAUME , MADERA ANN MARIE , SWEENEY ZACHARY KEVIN
IPC分类号： A61K31/42 , C07D261/08 , C07D413/06 , C07D413/12
摘要： This invention pertains generally to compounds of Formula I as described herein and compositions containing such compounds, as well as methods of using such compounds to treat bacterial infections. In certain aspects, the invention provides methods and compositions comprising these compounds for treating infections caused by Gram-negative bacteria.

10. 发明专利

CU20170084A7 COMPUESTOS DE ISOXAZOL DE ÁCIDO HIDROXÁMICO COMO INHIBIDORES DE LpxC 未知
公开(公告)号：CU20170084A7
公开(公告)日：2017-11-07
申请号：CU20170084
申请日：2015-12-15
申请人： NOVARTIS AG
发明人： FU JIPING , JIN XIANMING , KARUR SUBRAMANIAN , LAPOINTE GUILLAUME , MADERA ANN MARIE , SWEENEY ZACHARY KEVIN
IPC分类号： A61K31/42 , C07D261/08 , C07D413/06 , C07D413/12
摘要： Esta invención se refiere en general a compuestos de Fórmula I tal como se describen en el presente documento y composiciones que contienen dichos compuestos, así como métodos de uso de dichos compuestos para tratar infecciones bacterianas. En ciertos aspectos, Ia invención proporciona métodos y composiciones que comprenden estos compuestos para el tratamiento de infecciones causadas por bacterias Gram negativas. ESPACIO PARA FÓRMULA

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