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公开(公告)号：WO2012004217A1
公开(公告)日：2012-01-12
申请号：PCT/EP2011/061198
申请日：2011-07-04
申请人： NOVARTIS AG , BURGER, Matthew , DING, Yu , HAN, Wooseok , LINDVALL, Mika , NISHIGUCHI, Gisele A. , RICO, Alice , SMITH, Aaron , TANNER, Huw , WAN, Lifeng
发明人： BURGER, Matthew , DING, Yu , HAN, Wooseok , LINDVALL, Mika , NISHIGUCHI, Gisele A. , RICO, Alice , SMITH, Aaron , TANNER, Huw , WAN, Lifeng
IPC分类号： C07D407/04 , C07D407/14 , C07D417/14 , C07D491/04 , A61K31/444
CPC分类号： C07D417/14 , A61K31/444 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/541 , A61K45/06 , C07D405/14 , C07D407/04 , C07D407/14 , C07D491/04 , A61K2300/00
摘要： The present invention provides a compound of Formula (I): and pharmaceutically acceptable salts thereof, as further described herein. Also provided are formulations comprising compounds of formula I, and a method to use such compounds for treating a disease or condition mediated by Provirus Integration of Maloney Maloney Kinase (PIM Kinase), GSK3, PKC, KDR, PDGFRa, FGFR3, FLT3, or cABL.
摘要翻译： 本发明提供如本文进一步描述的式（I）化合物及其药学上可接受的盐。 还提供了包含式I化合物的制剂和使用这些化合物治疗由Maloney Maloney激酶（PIM激酶），GSK3，PKC，KDR，PDGFRa，FGFR3，FLT3或cABL的Provirus整合介导的疾病或病症的方法 。
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公开(公告)号：WO2016038582A1
公开(公告)日：2016-03-17
申请号：PCT/IB2015/056989
申请日：2015-09-11
申请人： NOVARTIS AG , AVERSA, Robert John , BURGER, Matthew T. , DILLON, Michael Patrick , DINEEN JR., Thomas A. , LOU, Yan , NISHIGUCHI, Gisele A , RAMURTHY, Savithri , RICO, Alice C. , RAUNIYAR, Vivek , SENDZIK, Martin , SUBRAMANIAN, Sharadha , SETTI, Lina Quattrocchio , TAFT, Benjamin R. , TANNER, Huw Rowland , WAN, Lifeng
发明人： AVERSA, Robert John , BURGER, Matthew T. , DILLON, Michael Patrick , DINEEN JR., Thomas A. , LOU, Yan , NISHIGUCHI, Gisele A , RAMURTHY, Savithri , RICO, Alice C. , RAUNIYAR, Vivek , SENDZIK, Martin , SUBRAMANIAN, Sharadha , SETTI, Lina Quattrocchio , TAFT, Benjamin R. , TANNER, Huw Rowland , WAN, Lifeng
IPC分类号： C07D405/14 , C07D405/12 , C07D305/06 , A61K31/501 , A61P35/00
CPC分类号： C07D405/14 , A61P35/00 , C07D305/06 , C07D405/12 , C07D413/14
摘要： The present invention provides compounds of Formula (I) and (II) as described herein, and salts thereof, and therapeutic uses of these compounds for treatment of disorders associated with Raf kinase activity. The invention further provides pharmaceutical compositions comprising these compounds, and compositions comprising these compounds and a therapeutic co-agent.
摘要翻译： 本发明提供了本文所述的式（I）和（II）化合物及其盐，以及这些化合物治疗与Raf激酶活性相关的疾病的治疗用途。 本发明还提供包含这些化合物的药物组合物，以及包含这些化合物和治疗性助剂的组合物。
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公开(公告)号：WO2014151616A1
公开(公告)日：2014-09-25
申请号：PCT/US2014/026107
申请日：2014-03-13
申请人： NOVARTIS AG , AVERSA, Robert , BARSANTI, Paul A. , BURGER, Matthew , DILLON, Michael Patrick , DIPESA, Alan , HU, Cheng , LOU, Yan , NISHIGUCHI, Gisele , PAN, Yue , POLYAKOV, Valery , RAMURTHY, Savithri , RICO, Alice , SETTI, Lina , SMITH, Aaron , SUBRAMANIAN, Sharadha , TAFT, Benjamin , TANNER, Huw , WAN, Lifeng , YUSUFF, Naeem
发明人： AVERSA, Robert , BARSANTI, Paul A. , BURGER, Matthew , DILLON, Michael Patrick , DIPESA, Alan , HU, Cheng , LOU, Yan , NISHIGUCHI, Gisele , PAN, Yue , POLYAKOV, Valery , RAMURTHY, Savithri , RICO, Alice , SETTI, Lina , SMITH, Aaron , SUBRAMANIAN, Sharadha , TAFT, Benjamin , TANNER, Huw , WAN, Lifeng , YUSUFF, Naeem
IPC分类号： C07D403/12 , C07D401/14 , C07D405/14 , C07D413/14 , C07D213/74 , C07D213/75 , C07D233/88 , C07D401/04 , C07D401/12 , C07D403/04 , C07D237/20 , C07D405/04 , C07D405/12 , C07D239/42 , C07D241/20
CPC分类号： A61K31/5377 , A61K31/444 , A61K31/501 , A61K31/5375 , A61K31/541 , A61K45/06 , C07B59/002 , C07B2200/05 , C07D213/74 , C07D213/75 , C07D213/81 , C07D213/82 , C07D213/84 , C07D233/88 , C07D237/20 , C07D237/22 , C07D237/24 , C07D239/42 , C07D239/47 , C07D239/48 , C07D241/20 , C07D263/58 , C07D277/42 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D405/04 , C07D405/12 , C07D405/14 , C07D409/14 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/12 , C07D471/04 , C07D487/04 , C07D491/04 , C07D491/048 , C07D491/08 , C07D491/107 , C07D493/04 , C07D493/10 , C07D495/04 , C07D498/08 , C07D513/04
摘要： The present invention provides compounds of Formula (I) as described herein, and salts thereof, and therapeutic uses of these compounds for treatment of disorders associated with Raf kinase activity. The invention further provides pharmaceutical compositions comprising these compounds, and compositions comprising these compounds and a therapeutic co-agent.
摘要翻译： 本发明提供了本文所述的式（I）化合物及其盐，以及这些化合物治疗与Raf激酶活性相关的疾病的治疗用途。 本发明还提供包含这些化合物的药物组合物，以及包含这些化合物和治疗性助剂的组合物。
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公开(公告)号：WO2014099880A1
公开(公告)日：2014-06-26
申请号：PCT/US2013/075613
申请日：2013-12-17
IPC分类号： C07D487/04 , A61K31/495 , A61P35/00
CPC分类号： C07D487/04 , A61K31/5025 , A61K45/06
摘要： The present invention provides a compound of formula (I) as described herein, and pharmaceutically acceptable salts, enantiomers, rotamers, tautomers, or racemates thereof. Also provided are methods of treating a disease or condition mediated by PIM kinase using the compounds of Formula (I), and pharmaceutical compositions comprising such compounds.
摘要翻译： 本发明提供本文所述的式（I）化合物及其药学上可接受的盐，对映异构体，旋转异构体，互变异构体或外消旋物。 还提供了使用式（I）的化合物治疗由PIM激酶介导的疾病或病症的方法和包含这些化合物的药物组合物。
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公开(公告)号：WO2009109576A1
公开(公告)日：2009-09-11
申请号：PCT/EP2009/052506
申请日：2009-03-03
申请人： NOVARTIS AG , BURGER, Matthew , LAN, Jiong , LINDVALL, Mika , NISHIGUCHI, Gisele , TETALMAN, Michelle
IPC分类号： C07D417/12 , C07D417/14 , A61K31/4439 , A61P35/00
CPC分类号： C07D417/12 , C07D417/14
摘要： The present invention relates to new compounds of Formulas (I) and (II), their tautomers, stereoisomers and polymorphs, and pharmaceutically acceptable salts, esters, metabolites or prodrugs thereof, compositions of the new compounds together with pharmaceutically acceptable carriers, and uses of the new compounds, either alone or in combination with at least one additional therapeutic agent, in the inhibition of Pirn kinase activity and/or the prophylaxis or treatment of cancer.
摘要翻译： 本发明涉及式（I）和（II）的新化合物，其互变异构体，立体异构体和多晶型物及其药学上可接受的盐，酯，代谢物或前药，新化合物与药学上可接受的载体的组合物，以及 新化合物单独或与至少一种另外的治疗剂联合用于抑制皮激素活性和/或预防或治疗癌症。
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公开(公告)号：WO2014033631A1
公开(公告)日：2014-03-06
申请号：PCT/IB2013/058034
申请日：2013-08-27
申请人： NOVARTIS AG , BURGER, Matthew , NISHIGUCHI, Gisele , RICO, Alice , SIMMONS, Robert Lowell , TAMEZ, JR., Victoriano , TANNER, Huw , WAN, Lifeng
发明人： BURGER, Matthew , NISHIGUCHI, Gisele , RICO, Alice , SIMMONS, Robert Lowell , TAMEZ, JR., Victoriano , TANNER, Huw , WAN, Lifeng
IPC分类号： C07D405/14 , C07D401/12 , C07D417/12 , A61K31/4427 , A61P35/00
CPC分类号： C07D401/12 , C07D405/14 , C07D417/12
摘要： The present invention provides a compound of formula (I): as described herein, and pharmaceutically acceptable salts, enantiomers, rotamers, tautomers, or racemates thereof. Also provided are methods of treating a disease or condition mediated by PIM kinase using the compounds of Formula (I), and pharmaceutical compositions comprising such compounds.
摘要翻译： 本发明提供式（I）化合物：如本文所述，及其药学上可接受的盐，对映异构体，旋转异构体，互变异构体或外消旋体。 还提供了使用式（I）的化合物治疗由PIM激酶介导的疾病或病症的方法和包含这些化合物的药物组合物。
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公开(公告)号：WO2012120415A1
公开(公告)日：2012-09-13
申请号：PCT/IB2012/050981
申请日：2012-03-01
申请人： NOVARTIS AG , BURGER, Matthew , DING, Yu , HAN, Wooseok , NISHIGUCHI, Gisele , RICO, Alice , SIMMONS, Robert Lowell , SMITH, Aaron R. , TAMEZ, JR., Victoriano , TANNER, Huw , WAN, Lifeng
发明人： BURGER, Matthew , DING, Yu , HAN, Wooseok , NISHIGUCHI, Gisele , RICO, Alice , SIMMONS, Robert Lowell , SMITH, Aaron R. , TAMEZ, JR., Victoriano , TANNER, Huw , WAN, Lifeng
IPC分类号： C07D213/81 , C07D401/14 , C07D405/14 , C07D417/12 , C07D417/14 , A61K31/444 , A61P35/00
CPC分类号： A61K31/4439 , A61K31/444 , A61K31/4745 , A61K31/497 , A61K31/506 , A61K31/513 , A61K31/519 , A61K31/5377 , A61K31/664 , A61K31/704 , A61K31/7068 , A61K33/24 , A61K39/395 , A61K45/06 , C07D213/81 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/12 , C07D417/14 , A61K2300/00
摘要： The present invention provides a compound of formula (I) as further described herein, and pharmaceutically acceptable salts, enantiomers, rotamers, tautomers, or racemates thereof. Also provided are methods of treating a disease or condition mediated by PIM kinase using the compounds of Formula I, and pharmaceutical compositions comprising such compounds.
摘要翻译： 本发明提供了本文进一步描述的式（I）化合物及其药学上可接受的盐，对映异构体，旋转异构体，互变异构体或其外消旋体。 还提供了使用式I化合物治疗PIM激酶介导的疾病或病症的方法和包含这些化合物的药物组合物。
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公开(公告)号：WO2008106692B1
公开(公告)日：2008-10-30
申请号：PCT/US2008055724
申请日：2008-03-03
申请人： NOVARTIS VACCINES & DIAGNOSTIC , BURGER MATTHEW , LINDVALL MIKA , HAN WOOSEOK , LAN JIONG , NISHIGUCHI GISELE , SHAFER CYNTHIA , BELLAMACINA CORNELIA , HUH KAY , ATALLAH GORDANA , MCBRIDE CHRISTOPHER , ANTONIOS-MCCREA WILLIAM JR , ZAVOROTINSKAYA TATIANA , WALTER ANNETTE , GARCIA PABLO
发明人： BURGER MATTHEW , LINDVALL MIKA , HAN WOOSEOK , LAN JIONG , NISHIGUCHI GISELE , SHAFER CYNTHIA , BELLAMACINA CORNELIA , HUH KAY , ATALLAH GORDANA , MCBRIDE CHRISTOPHER , ANTONIOS-MCCREA WILLIAM JR , ZAVOROTINSKAYA TATIANA , WALTER ANNETTE , GARCIA PABLO
IPC分类号： C07D213/78 , A61K31/44 , A61P35/00 , C07D239/28 , C07D401/12
CPC分类号： C07D401/12 , C07D213/78 , C07D239/28
摘要： New compounds, compositions and methods of inhibition of kinase activity associated with tumorigenesis in a human or animal subject are provided. In certain embodiments, the compounds and compositions are effective to inhibit the activity of at least one serine/threonine kinase or receptor tyrosine kinase. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a serine/threonine kinase- or receptor tyrosine kinase- mediated disorder, such as cancer.
摘要翻译： 提供了在人或动物受试者中抑制与肿瘤发生相关的激酶活性的新化合物，组合物和方法。 在某些实施方案中，化合物和组合物有效地抑制至少一种丝氨酸/苏氨酸激酶或受体酪氨酸激酶的活性。 新化合物和组合物可以单独使用或与至少一种另外的药物组合使用，用于治疗丝氨酸/苏氨酸激酶或受体酪氨酸激酶介导的病症，例如癌症。
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公开(公告)号：WO2016038583A1
公开(公告)日：2016-03-17
申请号：PCT/IB2015/056990
申请日：2015-09-11
申请人： NOVARTIS AG , BARSANTI, Paul Andrew , BURGER, Matthew T. , LOU, Yan , NISHIGUCHI, Gisele A. , POLYAKOV, Valery Rostislavovich , RAMURTHY, Savithri , SUBRAMANIAN, Sharadha , TAFT, Benjamin R. , TANNER, Huw Rowland , WAN, Lifeng
发明人： BARSANTI, Paul Andrew , BURGER, Matthew T. , LOU, Yan , NISHIGUCHI, Gisele A. , POLYAKOV, Valery Rostislavovich , RAMURTHY, Savithri , SUBRAMANIAN, Sharadha , TAFT, Benjamin R. , TANNER, Huw Rowland , WAN, Lifeng
IPC分类号： C07D401/14 , C07D413/14 , C07D213/74 , C07D401/04 , C07D401/10 , C07D407/14 , C07D411/14 , C07D413/12 , A61K31/4439 , A61K31/444 , A61K31/44 , A61K31/5377 , A61P35/00
CPC分类号： C07D498/08 , A61K31/4418 , A61K31/444 , A61K31/496 , A61K31/501 , A61K31/5377 , A61K31/541 , C07D213/74 , C07D213/85 , C07D401/04 , C07D401/10 , C07D401/14 , C07D405/12 , C07D405/14 , C07D407/14 , C07D411/14 , C07D413/12 , C07D413/14 , C07D451/02
摘要： The present invention provides compounds of Formula (I) and (II) as described herein, and salts thereof, and therapeutic uses of these compounds for treatment of disorders associated with Raf kinase activity. The invention further provides pharmaceutical compositions comprising these compounds, and compositions comprising these compounds and a therapeutic co-agent.
摘要翻译： 本发明提供了本文所述的式（I）和（II）化合物及其盐，以及这些化合物治疗与Raf激酶活性相关的疾病的治疗用途。 本发明还提供包含这些化合物的药物组合物，以及包含这些化合物和治疗性助剂的组合物。
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公开(公告)号：WO2014033630A1
公开(公告)日：2014-03-06
申请号：PCT/IB2013/058033
申请日：2013-08-27
申请人： NOVARTIS AG , BURGER, Matthew , DING, Yu , HAN, Wooseok , NISHIGUCHI, Gisele , RICO, Alice , SIMMONS, Robert Lowell , TANNER, Huw , WAN, Lifeng
发明人： BURGER, Matthew , DING, Yu , HAN, Wooseok , NISHIGUCHI, Gisele , RICO, Alice , SIMMONS, Robert Lowell , TANNER, Huw , WAN, Lifeng
IPC分类号： C07D417/12 , A61K31/427 , C07D417/14 , A61P35/00
CPC分类号： C07D417/14 , A61K31/427 , C07D417/12
摘要： The present invention provides a compound of formula (I), as described herein, and pharmaceutically acceptable salts, enantiomers, rotamers, tautomers, or racemates thereof. Also provided are methods of treating a disease or condition mediated by PIM kinase using the compounds of Formula I, and pharmaceutical compositions comprising such compounds.
摘要翻译： 本发明提供如本文所述的式（I）化合物及其药学上可接受的盐，对映异构体，旋转异构体，互变异构体或外消旋体。 还提供了使用式I化合物治疗PIM激酶介导的疾病或病症的方法和包含这些化合物的药物组合物。
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