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公开(公告)号：US20170114083A1
公开(公告)日：2017-04-27
申请号：US15397787
申请日：2017-01-04
Applicant: Matthew T. BURGER , Savithri RAMURTHY , Benjamin R. TAFT
Inventor： Matthew T. BURGER , Savithri RAMURTHY , Benjamin R. TAFT
IPC: C07F9/6558 , A61K31/675
CPC classification number: C07F9/65583 , A61K31/675 , C07D213/74 , C07D403/12 , C07D413/04 , C07D413/14
Abstract: The present invention provides a compound of Formula I: wherein X, Y, Z, R1 and R2 are 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.
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公开(公告)号：US20160038504A1
公开(公告)日：2016-02-11
申请号：US14774431
申请日：2014-03-13
Applicant: Robert AVERSA , Paul A. BARSANTI , Matthew BURGER , Michael Patrick DILLON , Alan DIPESA , Cheng HU , Yan LOU , Gisele NISHIGUCHI , Yue PAN , Valery POLYAKOV , Savithri RAMURTHY , Alice RICO , Lina SETTI , Aaron SMITH , Sharadha SUBRAMANIAN , Benjamin TAFT , Huw TANNER , Lifeng WAN , Naeem YUSUFF
Inventor： Robert John AVERSA , Paul Andrew BARSANTI , Matthew T. BURGER , Michael Patrick DILLON , Alan DIPESA , Cheng HU , Yan LOU , Gisele A. NISHIGUCHI , Yue PAN , Valery Rostislavovich POLYAKOV , Savithri RAMURTHY , Alice C. RICO , Lina Quattrocchio SETTI , Aaron SMITH , Sharadha SUBRAMANIAN , Benjamin R. TAFT , Huw Roland TANNER , Lifeng WAN , Naeem YUSUFF
IPC: A61K31/5377 , C07D401/12 , C07D413/04 , C07D413/14 , C07D239/48 , A61K31/541 , C07D401/04 , C07D413/12 , C07D417/12 , C07D239/47 , C07D491/107 , C07D403/04 , C07D498/08 , A61K31/5375 , C07D237/20 , C07D213/74 , C07D405/14 , C07D405/04 , C07D241/20 , C07D405/12 , C07D237/22 , C07D213/84 , C07D213/82 , C07D487/04 , C07D471/04 , C07D495/04 , C07D491/048 , C07D513/04 , C07D409/14 , C07D213/81 , C07D263/58 , C07D239/42
CPC classification number: 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
Abstract: 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.
Abstract translation: 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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3.发明授权Substituted benz-azoles and methods of their use as inhibitors of RAF kinase 失效取代的苯并唑及其作为RAF激酶抑制剂的方法公开(公告)号：US08614330B2
公开(公告)日：2013-12-24
申请号：US12723483
申请日：2010-03-12
Applicant: Payman Amiri , Wendy Fantl , Teresa Hansen , Barry Haskell Levine , Christopher McBride , Daniel J. Poon , Savithri Ramurthy , Paul A. Renhowe , Cynthia M. Shafer , Sharadha Subramanian , Leonard Sung
Inventor： Payman Amiri , Wendy Fantl , Teresa Hansen , Barry Haskell Levine , Christopher McBride , Daniel J. Poon , Savithri Ramurthy , Paul A. Renhowe , Cynthia M. Shafer , Sharadha Subramanian , Leonard Sung
IPC: A61K31/4439 , C07D417/12
CPC classification number: C07D401/14 , C07D401/12 , C07D405/12 , C07D405/14 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/12 , C07D417/14 , C07D453/02
Abstract: New substituted benz-azole compounds, compositions and methods of inhibition of Raf kinase activity in a human or animal subject are provided. The new compounds compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.
Abstract translation: 提供了新的取代的苯并唑化合物，抑制人或动物受试者中Raf激酶活性的组合物和方法。 新化合物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Raf激酶介导的病症，例如癌症。
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公开(公告)号：US08592459B2
公开(公告)日：2013-11-26
申请号：US12759578
申请日：2010-04-13
Applicant: Mina E. Aikawa , Payman Amiri , Jeffrey H. Dove , Barry Haskell Levine , Christopher McBride , Teresa E. Pick , Daniel J. Poon , Savithri Ramurthy , Paul A. Renhowe , Cynthia Shafer , Darrin Stuart , Sharadha Subramanian
Inventor： Mina E. Aikawa , Payman Amiri , Jeffrey H. Dove , Barry Haskell Levine , Christopher McBride , Teresa E. Pick , Daniel J. Poon , Savithri Ramurthy , Paul A. Renhowe , Cynthia Shafer , Darrin Stuart , Sharadha Subramanian
IPC: A61K31/4439 , C07D401/12
CPC classification number: C07D401/14 , Y02P20/55
Abstract: 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.
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5.发明申请SUBSTITUTED BENZAZOLES AND METHODS OF THEIR USE AS INHIBITORS OF RAF KINASE 审中-公开替代苯扎唑及其作为RAF激酶抑制剂的方法公开(公告)号：US20130224195A1
公开(公告)日：2013-08-29
申请号：US13856225
申请日：2013-04-03
Applicant: Abran Costales , Teresa Hansen , Barry H. Levine , Christopher McBride , Daniel J. Poon , Savithri Ramurthy , Paul A. Renhowe , Cynthia M. Shafer , Sharadha Subramanian , Joelle Verhagen
Inventor： Abran Costales , Teresa Hansen , Barry H. Levine , Christopher McBride , Daniel J. Poon , Savithri Ramurthy , Paul A. Renhowe , Cynthia M. Shafer , Sharadha Subramanian , Joelle Verhagen
IPC: C07D401/12 , C07D405/12 , C07D401/14 , A61K31/4545 , A61K31/5377 , A61K45/06 , A61K31/444 , C07D417/12 , C07D417/14 , C07D413/14 , A61K31/551 , A61K31/4439 , A61K31/496
CPC classification number: C07D401/12 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/496 , A61K31/5377 , A61K31/551 , A61K45/06 , C04B35/632 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/12 , C07D417/14
Abstract: New substituted benzazole compounds, compositions and methods of inhibition of Raf kinase activity in a human or animal subject are provided. The new compounds compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.
Abstract translation: 提供了新的取代的苯唑化合物，抑制人或动物受试者中的Raf激酶活性的组合物和方法。 新化合物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Raf激酶介导的病症，例如癌症。
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Patent Agency Ranking
公开(公告)号：US07732465B2
公开(公告)日：2010-06-08
申请号：US12315779
申请日：2008-12-05
Applicant: Mina E. Aikawa , Payman Amiri , Jeffrey H. Dove , Barry Haskell Levine , Christopher McBride , Teresa E. Pick , Daniel J. Poon , Savithri Ramurthy , Paul A. Renhowe , Cynthia Shafer , Darrin Stuart , Sharadha Subramanian
Inventor： Mina E. Aikawa , Payman Amiri , Jeffrey H. Dove , Barry Haskell Levine , Christopher McBride , Teresa E. Pick , Daniel J. Poon , Savithri Ramurthy , Paul A. Renhowe , Cynthia Shafer , Darrin Stuart , Sharadha Subramanian
IPC: A61K31/4439
CPC classification number: C07D401/14 , Y02P20/55
Abstract: 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.
Abstract translation: 提供了新的取代的苯并咪唑化合物，组合物和抑制与人或动物受试者的肿瘤发生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。 新化合物和组合物可以单独使用或与至少一种另外的药剂组合使用，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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7.发明授权6-O-substituted benzoxazole and benzothiazole compounds and methods of inhibiting CSF-1R signaling 有权6-O-取代的苯并恶唑和苯并噻唑化合物以及抑制CSF-1R信号传导的方法公开(公告)号：US07553854B2
公开(公告)日：2009-06-30
申请号：US11737069
申请日：2007-04-18
Applicant: James C Sutton , Marion Wiesmann , Weibo Wang , Mika Lindvall , Jiong Lan , Savithri Ramurthy , Anu Sharma , Elizabeth J. Mieuli , Liana M. Klivansky , William Lenahan , Susan Kaufman , Hong Yang , Simon C. Ng , Keith Pfister , Allan S. Wagman , Victoria Sung , Martin Sendzik
Inventor： James C Sutton , Marion Wiesmann , Weibo Wang , Mika Lindvall , Jiong Lan , Savithri Ramurthy , Anu Sharma , Elizabeth J. Mieuli , Liana M. Klivansky , William Lenahan , Susan Kaufman , Hong Yang , Simon C. Ng , Keith Pfister , Allan S. Wagman , Victoria Sung , Martin Sendzik
IPC: C07D215/00 , A61K31/44
CPC classification number: C07D413/12 , C07D417/12
Abstract: Benzoxazole and benzothiazole compounds and the stereoisomers, tautomers, solvates, oxides, esters, and prodrugs thereof and pharmaceutically acceptable salts thereof are disclosed. Compositions of the compounds, either alone or in combination with at least one additional therapeutic agent, with a pharmaceutically acceptable carrier, and uses of the compounds, either alone or in combination with at least one additional therapeutic agent are also disclosed. The embodiments are useful for inhibiting cellular proliferation, inhibiting the growth and/or metathesis of tumors, treating or preventing cancer, treating or preventing degenerating bone diseases such as rheumatoid arthritis, and/or inhibiting molecules such as CSF-1R.
Abstract translation: 公开了苯并恶唑和苯并噻唑化合物及其立体异构体，互变异构体，溶剂合物，氧化物，酯和前药及其药学上可接受的盐。 还公开了单独或与至少一种另外的治疗剂组合的化合物与药学上可接受的载体的组合，以及化合物单独或与至少一种另外的治疗剂组合的用途。 这些实施方案可用于抑制细胞增殖，抑制肿瘤的生长和/或复分解，治疗或预防癌症，治疗或预防退行性骨疾病如类风湿性关节炎和/或抑制分子如CSF-1R。
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8.发明授权Substituted benzazoles and methods of their use as inhibitors of Raf kinase 失效取代的苯并唑及其作为Raf激酶抑制剂的方法公开(公告)号：US07423150B2
公开(公告)日：2008-09-09
申请号：US10967089
申请日：2004-10-15
Applicant: Abran Costales , Teresa Hansen , Barry H. Levine , Christopher McBride , Daniel J. Poon , Savithri Ramurthy , Paul A. Renhowe , Cynthia M. Shafer , Sharadha Subramanian , Joelle Verhagen
Inventor： Abran Costales , Teresa Hansen , Barry H. Levine , Christopher McBride , Daniel J. Poon , Savithri Ramurthy , Paul A. Renhowe , Cynthia M. Shafer , Sharadha Subramanian , Joelle Verhagen
IPC: C07D401/00 , C07D233/00 , C07D233/02
CPC classification number: C07D401/12 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/496 , A61K31/5377 , A61K31/551 , A61K45/06 , C04B35/632 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/12 , C07D417/14
Abstract: New substituted benzazole compounds, compositions and methods of inhibition of Raf kinase activity in a human or animal subject are provided. The new compounds compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.
Abstract translation: 提供了新的取代的苯唑化合物，抑制人或动物受试者中的Raf激酶活性的组合物和方法。 新化合物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Raf激酶介导的病症，例如癌症。
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公开(公告)号：US07384942B2
公开(公告)日：2008-06-10
申请号：US11202013
申请日：2005-08-10
Applicant: John M. Nuss , Savithri Ramurthy
Inventor： John M. Nuss , Savithri Ramurthy
IPC: C07D241/00
CPC classification number: C07D401/12 , A61K31/427 , A61K31/4965 , A61K31/497 , A61K38/28 , C07D241/20 , A61K2300/00
Abstract: New bicyclic based compounds, compositions and methods of inhibiting the activity of glycogen synthase kinase (GSK3) in vitro and of treatment of GSK3 mediated disorders in vivo are provided. The methods, compounds and compositions of the invention may be employed alone, or in combination with other pharmacologically active agents in the treatment of disorders mediated by GSK3 activity, such as in the treatment of diabetes, Alzheimer's disease and other neurodegenerative disorders, obesity, atherosclerotic cardiovascular disease, essential hypertension, polycystic ovary syndrome, syndrome X, ischemia, traumatic brain injury, bipolar disorder, immunodeficiency or cancer.
Abstract translation: 提供了新的双环类化合物，体外抑制糖原合成酶激酶（GSK3）活性和体内GSK3介导的病症治疗的组合物和方法。 本发明的方法，化合物和组合物可以单独使用或与其它药理活性剂组合用于治疗由GSK3活性介导的病症，例如治疗糖尿病，阿尔茨海默病和其他神经变性疾病，肥胖症，动脉粥样硬化 心血管疾病，原发性高血压，多囊卵巢综合征，X综合征，缺血，创伤性脑损伤，双相情感障碍，免疫缺陷或癌症。
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公开(公告)号：US09809610B2
公开(公告)日：2017-11-07
申请号：US15397787
申请日：2017-01-04
Applicant: Matthew T. Burger , Savithri Ramurthy , Benjamin R. Taft
Inventor： Matthew T. Burger , Savithri Ramurthy , Benjamin R. Taft
IPC: C07D403/12 , C07D213/74 , C07D413/04 , C07D413/14 , A61K31/675 , C07F9/6558
CPC classification number: C07F9/65583 , A61K31/675 , C07D213/74 , C07D403/12 , C07D413/04 , C07D413/14
Abstract: The present invention provides a compound of Formula I: wherein X, Y, Z, R1 and R2 are 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.
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