公开(公告)号：US20080280873A1

公开(公告)日：2008-11-13

申请号：US10594367

申请日：2005-03-25

申请人： Jun Liang ,  Prasun K. Chakravarty ,  Deborah E. Pan ,  William H. Parsons ,  Pengcheng P. Shao ,  Feng Yee ,  Bishan Zhou

发明人： Jun Liang ,  Prasun K. Chakravarty ,  Deborah E. Pan ,  William H. Parsons ,  Pengcheng P. Shao ,  Feng Yee ,  Bishan Zhou

IPC分类号： A61K31/4965 ,  C07D241/24

CPC分类号： C07D241/24 ,  B05B1/02 ,  B05B1/14 ,  B05B1/34 ,  B65D83/20 ,  C07D241/18 ,  C07D403/06 ,  C07D405/04 ,  C07D413/06

摘要： Biaryl substituted pyrazinone compounds represented by Formula I, or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, sodium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, urinary incontinence, itchiness, allergic dermatitis, epilepsy, irritable bowel syndrome, depression, anxiety, multiple sclerosis, and bipolar disorder, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds. A method of administering local anesthesia comprises administering an effective amount of a compound of the instant invention, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier.

摘要翻译： 由式I表示的二芳基取代的吡嗪酮化合物或其药学上可接受的盐。 药物组合物包含单独的或与一种或多种其它治疗活性化合物组合的有效量的本发明化合物和药学上可接受的载体。 治疗与钠通道活性相关或由其引起的疾病的方法，包括例如急性疼痛，慢性疼痛，内脏痛，炎性疼痛，神经性疼痛，尿失禁，瘙痒，过敏性皮炎，癫痫，肠易激综合征，抑郁症 ，焦虑，多发性硬化和双相性精神障碍，包括单独或与一种或多种其它治疗活性化合物组合施用有效量的本发明化合物。 施用局部麻醉的方法包括单独施用有效量的本发明化合物或与一种或多种其它治疗活性化合物和药学上可接受的载体组合施用。

公开(公告)号：US10442819B2

公开(公告)日：2019-10-15

申请号：US15532549

申请日：2015-12-01

申请人： Christian Fischer ,  Stephane L. Bogen ,  Matthew L. Childers ,  Francesc Xavier Fradera Llinas ,  J. Michael Ellis ,  Sara Esposite ,  Qingmei Hong ,  Chunhui Huang ,  Alexander J. Kim ,  John W. Lampe ,  Michelle R. Machacek ,  Daniel R. McMasters ,  Ryan D. Otte ,  Dann L. Parker, Jr. ,  Michael Reutershan ,  Nunzio Sciammetta ,  Pengcheng P. Shao ,  David L. Sloman ,  Feroze Ujjainwalla ,  Catherine White ,  Zhicai Wu ,  Yang Yu ,  Kake Zhao ,  Craig Gibeau ,  Tesfaye Biftu ,  Purakkattle Biju ,  Lei Chen ,  Joshua Close ,  Peter H. Fuller ,  Xianhai Huang ,  Min K. Park ,  Valdimir Simov ,  David J. Witter ,  Hongjun Zhang

发明人： Christian Fischer ,  Stephane L. Bogen ,  Matthew L. Childers ,  Francesc Xavier Fradera Llinas ,  J. Michael Ellis ,  Sara Esposite ,  Qingmei Hong ,  Chunhui Huang ,  Alexander J. Kim ,  John W. Lampe ,  Michelle R. Machacek ,  Daniel R. McMasters ,  Ryan D. Otte ,  Dann L. Parker, Jr. ,  Michael Reutershan ,  Nunzio Sciammetta ,  Pengcheng P. Shao ,  David L. Sloman ,  Feroze Ujjainwalla ,  Catherine White ,  Zhicai Wu ,  Yang Yu ,  Kake Zhao ,  Craig Gibeau ,  Tesfaye Biftu ,  Purakkattle Biju ,  Lei Chen ,  Joshua Close ,  Peter H. Fuller ,  Xianhai Huang ,  Min K. Park ,  Valdimir Simov ,  David J. Witter ,  Hongjun Zhang

IPC分类号： A61K31/351 ,  A61K31/4353 ,  A61K31/5355 ,  A61K31/551 ,  C07D471/04 ,  C07D471/14 ,  C07D498/08 ,  C07D471/08 ,  C07D498/04 ,  C07D498/10 ,  A01N43/00

摘要： The present invention is directed to tricyclic compounds of formula (I) which are inhibitors of one or more mutant IDH enzymes: (I). The present invention is also directed to uses of the tricyclic compounds described herein in the potential treatment or prevention of cancers in which one or more mutant IDH enzymes are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such cancers.