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1. 发明专利

JP2013060458A Substituted benzimidazole as kinase inhibitor 审中-公开
标题翻译：取代苄嘧菌胺作为激酶抑制剂
公开(公告)号：JP2013060458A
公开(公告)日：2013-04-04
申请号：JP2012264553
申请日：2012-12-03
申请人： Novartis Ag , ノバルティスアーゲー
发明人： AIKAWA MINA E , AMIRI PAYMAN , DOVE JEFFREY H , LEVINE BARRY HASKELL , MCBRIDE CHRISTOPHER , PICK TERESA E , POON DANIEL J , RAMURTHY SAVITHRI , RENHOWE PAUL A , SHAFER CYNTHIA , STUART DARRIN , SUBRAMANIAN SHARADHA
IPC分类号： C07D401/14 , A61K31/4439 , A61K31/496 , A61P35/00 , A61P35/02 , A61P43/00 , C07D405/14
CPC分类号： C07D401/14 , Y02P20/55
摘要： PROBLEM TO BE SOLVED: To provide: new substituted benzimidazole compounds, their tautomers, stereoisomers, polymorphs, esters, metabolites, and prodrugs; the pharmaceutically acceptable salts of the compounds, tautomers, stereoisomers, polymorphs, esters, metabolites, and prodrugs; compositions of any of the embodiments together with pharmaceutically acceptable carriers; and uses of any of the embodiments, either alone or in combination with at least one additional therapeutic agent, in the prophylaxis or treatment of cancer.SOLUTION: The new substituted benzimidazole compounds of formula (I), compositions, and methods of inhibition of kinase activity associated with carcinogenicity 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 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：待解决的问题：提供：新取代的苯并咪唑化合物，其互变异构体，立体异构体，多晶型物，酯，代谢物和前药; 化合物，互变异构体，立体异构体，多晶型物，酯，代谢物和前药的药学上可接受的盐; 任何实施方案的组合物和药学上可接受的载体; 以及任何实施方案的单独使用或与至少一种其它治疗剂组合用于预防或治疗癌症中的用途。提供了式（I）的新取代的苯并咪唑化合物，组合物和抑制与人或动物受试者中致癌性相关的激酶活性的方法。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。化合物和组合物可以单独使用或与用于治疗丝氨酸/苏氨酸激酶或受体酪氨酸激酶介导的病症例如癌症的至少一种另外的药物组合使用。版权所有（C）2013，JPO＆INPIT

2. 发明专利

PL1926722T3 Podstawione benzimidazole jako inhibitory kinaz 未知
公开(公告)号：PL1926722T3
公开(公告)日：2012-02-29
申请号：PL06824870
申请日：2006-08-30
申请人： NOVARTIS AG
发明人： AIKAWA MINA E , AMIRI PAYMAN , DOVE JEFFREY H , LEVINE BARRY HASKELL , MCBRIDE CHRISTOPHER , PICK TERESA E , POON DANIEL J , RAMURTHY SAVITHRI , RENHOWE PAUL A , SHAFER CYNTHIA , STUART DARRIN , SUBRAMANIAN SHARADHA
IPC分类号： C07D401/14 , A61K31/435 , A61P35/00

3. 发明专利

SI1926722T1 Substituirani benzimidazoli kot kinazni inhibitorji 未知
公开(公告)号：SI1926722T1
公开(公告)日：2012-01-31
申请号：SI200631203
申请日：2006-08-30
申请人： NOVARTIS AG
发明人： AIKAWA MINA E , AMIRI PAYMAN , DOVE JEFFREY H , LEVINE BARRY HASKELL , MCBRIDE CHRISTOPHER , PICK TERESA E , POON DANIEL J , RAMURTHY SAVITHRI , RENHOWE PAUL A , SHAFER CYNTHIA , STUART DARRIN , SUBRAMANIAN SHARADHA
IPC分类号： C07D401/00 , A61K31/435 , A61P35/00

4. 发明专利

DK1926722T3 Substituerede benzimidazoler som kinaseinhibitorer 未知
公开(公告)号：DK1926722T3
公开(公告)日：2011-12-19
申请号：DK06824870
申请日：2006-08-30
申请人： NOVARTIS AG
发明人： AIKAWA MINA E , AMIRI PAYMAN , DOVE JEFFREY H , LEVINE BARRY HASKELL , MCBRIDE CHRISTOPHER , PICK TERESA E , POON DANIEL J , RAMURTHY SAVITHRI , RENHOWE PAUL A , SHAFER CYNTHIA , STUART DARRIN , SUBRAMANIAN SHARADHA
IPC分类号： C07D401/14 , A61K31/435 , A61P35/00

5. 发明专利

AT526325T 未知
公开(公告)号：AT526325T
公开(公告)日：2011-10-15
申请号：AT06824870
申请日：2006-08-30
申请人： NOVARTIS AG
发明人： AIKAWA MINA E , AMIRI PAYMAN , DOVE JEFFREY H , LEVINE BARRY HASKELL , MCBRIDE CHRISTOPHER , PICK TERESA E , POON DANIEL J , RAMURTHY SAVITHRI , RENHOWE PAUL A , SHAFER CYNTHIA , STUART DARRIN , SUBRAMANIAN SHARADHA
IPC分类号： C07D401/14 , A61K31/435 , A61P35/00
摘要： New substituted benzimidazole 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.

6. 发明专利

CU20080027A7 BENCIMIDAZOLES SUSTITUIDOS COMO INHIBIDORES DE CINASA 未知
公开(公告)号：CU20080027A7
公开(公告)日：2010-12-08
申请号：CU20080027
申请日：2008-02-25
申请人： NOVARTIS AG
发明人： SUBRAMANIAN SHARADHA , STUART DARRIN , SHAFER CYNTHIA , RENHOWE PAUL A , RAMURTHY SAVITHRI , POON DANIEL J , PICK TERESA E , MCBRIDE CHRISTOPHER , LEVINE BARRY HASKELL , DOVE JEFFREY H , AMIRI PAYMAN , AIKAWA MINA E
IPC分类号： A61K31/435 , C07D401/14
摘要： Se proporcionan nuevos compuestos de bencimidazol sustituidos de la fórmula (I), composiciones, y métodos para la inhibición de la actividad de cinasa asociada con tumorigénesis en un sujeto humano o animal. En ciertas modalidades, los compuestos y las composiciones son efectivos para inhibir la actividad de cuando menos una cinasa de serina/treonina o una cinasa de tirosina receptora. Los nuevos compuestos y composiciones se pueden utilizar solos o bien en combinación con cuando menos un agente adicional para el tratamiento de un trastorno mediado por cinasa de serina/treonina o por cinasa de tirosina receptora, tal como cáncer.

7. 发明专利

SMAP200800022A Benzimidazoli sostituiti come inibitori delle chinasi 未知
公开(公告)号：SMAP200800022A
公开(公告)日：2008-04-02
申请号：SM200800022
申请日：2006-08-30
申请人： NOVARTIS AG
发明人： AIKAWA MINA E , AMIRI PAYMAN , DOVE JEFFREY H , LEVINE BARRY HASKELL , MCBRIDE CHRISTOPHER , PICK TERESA E , POON DANIEL J , RAMURTHY SAVITHRI , RENHOWE PAUL A , SHAFER CYNTHIA , STUART DARRIN , SUBRAMANIAN SHARADHA

8. 发明专利

ES2374451T3 BENCIMIDAZOLES SUSTITUIDOS COMO INHIBIDORES DE QUINASA. 未知
公开(公告)号：ES2374451T3
公开(公告)日：2012-02-16
申请号：ES06824870
申请日：2006-08-30
申请人： NOVARTIS AG
发明人： AIKAWA MINA E , AMIRI PAYMAN , DOVE JEFFREY H , LEVINE BARRY HASKELL , MCBRIDE CHRISTOPHER , PICK TERESA E , POON DANIEL J , RAMURTHY SAVITHRI , RENHOWE PAUL A , SHAFER CYNTHIA , STUART DARRIN , SUBRAMANIAN SHARADHA
IPC分类号： C07D401/14 , A61K31/435 , A61P35/00
摘要： Un compuesto de fórmula (I): en donde, cada R1 se selecciona independientemente de entre hidroxi, halo, alquilo C1 - 6, alcoxi C1 - 6, (alquil C1 - 6)sulfanilo, (alquil C1 - 6)sulfonilo, cicloalquilo, heterocicloalquilo, fenilo, y heteroarilo; R2 es alquilo C1 - 6 o halo(alquilo C1 - 6); cada R3 se selecciona independientemente de entre halo, alquilo C1 - 6, y alcoxi C1 - 6; cada R4 se selecciona independientemente de entre hidroxi, alquilo C1 - 6, alcoxi C1 - 6, halo, heterocicloalquilcarbonilo, carboxilo, (alcoxi C1 - 6)carbonilo, aminocarbonilo, alquilaminocarbonilo C1 - 6, carbonitrilo, cicloalquilo, heterocicloalquilo, fenilo, y heteroarilo; en donde R1, R2, R3, y R4 pueden ser opcionalmente sustituidos con uno o más sustituyentes independientemente seleccionados de entre hidroxi, halo, alquilo C1 - 6, halo(alquilo C1 - 6), alcoxi C1 - 6, y halo(alcoxi C1 - 6); a es 1, 2, 3, 4, o 5; b es 0, 1, 2, o 3; y c es 1 o 2; o un tautómero, estereoisómero, polimorfo, o éster del mismo o una sal farmacéuticamente aceptable del compuesto, tautómero, estereoisómero, polimorfo o éster.

9. 发明专利

BRPI0615309A2 未知
公开(公告)号：BRPI0615309A2
公开(公告)日：2011-05-17
申请号：BRPI0615309
申请日：2006-08-30
申请人： NOVARTIS AG
发明人： AIKAWA MINA E , AMIRI PAYMAN , DOVE JEFFREY H , LEVINE BARRY HASKELL , PICK TERESA E , POON DANIEL J , RAMURTHY SAVITHRI , RENHOWE PAUL A , SHAFER CYNTHIA , STUART DARRIN , SUBRAMANIAN SHARADHA , MCBRIDE CHRISTOPHER
IPC分类号： C07D401/14 , A61K31/435 , A61P35/00
摘要： New substituted benzimidazole 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.

10. 发明专利

SMP200800059B Chinazoline per l'inibizione di pdk1 未知
公开(公告)号：SMP200800059B
公开(公告)日：2009-09-07
申请号：SM200800059
申请日：2007-04-05
申请人： NOVARTIS AG
发明人： AIKAWA MINA E , AMIRI PAYMAN , RAMURTHY SAVITHRI , SUBRAMANIAN SHARADHA , WANG X MICHEAL , ZHOU YASHEEN , LIN XIAODONG , RICO ALICE , NG SIMON , PFISTER KEITH , JAIN RAMA , MURRAY JEREMY M , BASHAM STEVEN E , WARNE ROBERT L , SHU WEI , JANSEN JOHANNA M

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