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1. 发明申请

US20100041695A1 Thieno[2,3-b]pyridines as Potassium Channel Inhibitors 有权
标题翻译：噻吩并[2,3-b]吡啶作为钾通道抑制剂
公开(公告)号：US20100041695A1
公开(公告)日：2010-02-18
申请号：US12543151
申请日：2009-08-18
申请人： John FORD , Nicholas John PALMER , John Frederick ATHERALL , David John MADGE , Derek JOHN
发明人： John FORD , Nicholas John PALMER , John Frederick ATHERALL , David John MADGE , Derek JOHN
IPC分类号： A61K31/4436 , A61P9/06 , A61P19/02 , A61P29/00 , A61P1/00 , A61P3/10
CPC分类号： C07D495/04 , C07D333/36 , C07D333/38 , C07D409/12
摘要： The invention provides compounds of the formula: wherein R1 is aryl, heteroaryl, cycloalkyl or alkyl; R2 is H, alkyl, nitro, CO2R7, CONR5R6 or halo; R3 and R4 are H, NR5R6, NC(O)R7, halo, trifluoromethyl, alkyl, CONR5R6, CO2R7, nitrile or alkoxy; R5 and R6 may be the same or different and may be H, alkyl, aryl, heteroaryl or cycloalkyl; or R5 and R6 may together form a saturated, unsaturated or partially saturated 4 to 7 member ring, wherein said ring may optionally comprise one or more further heteroatoms selected from N, O or S; R7 is H or alkyl; A is H, halo, or a group of formula X-L-Y; X is O, S or NR8; R8 is H or alkyl; L is (CH2)n, where n is 0, 1, 2, 3 or 4; and Y is aryl, a heterocyclic group, alkyl, alkenyl or cycloalkyl; the products of mono- and di-oxidation of sulphur and/or mono-oxidation of nitrogen moieties in compounds of formula I; or a pharmaceutically acceptable salt thereof. These compounds find use as inhibitors of potassium ion channels and thus are useful in the treatment of various conditions including arrhythmia and type-2 diabetes mellitus.
摘要翻译：本发明提供下式的化合物：其中R1是芳基，杂芳基，环烷基或烷基; R2是H，烷基，硝基，CO 2 R 7，CONR 5 R 6或卤素; R3和R4是H，NR5R6，NC（O）R7，卤素，三氟甲基，烷基，CONR5R6，CO2R7，腈或烷氧基; R5和R6可以相同或不同，可以是H，烷基，芳基，杂芳基或环烷基; 或R 5和R 6可以一起形成饱和的，不饱和的或部分饱和的4至7元环，其中所述环可任选地包含一个或多个选自N，O或S的其它杂原子; R7是H或烷基; A是H，卤素或式X-L-Y基团; X是O，S或NR8; R8是H或烷基; L是（CH 2）n，其中n是0,1,2,3或4; Y为芳基，杂环基，烷基，链烯基或环烷基; 式I化合物中硫的单和二氧化和/或氮部分的单氧化的产物; 或其药学上可接受的盐。这些化合物可用作钾离子通道的抑制剂，因此可用于治疗各种病症，包括心律失常和2型糖尿病。

2. 发明申请

US20130217664A1 NOVEL COMPOUNDS USEFUL FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES 审中-公开
标题翻译：用于治疗衰老和炎症疾病的新型化合物
公开(公告)号：US20130217664A1
公开(公告)日：2013-08-22
申请号：US13762155
申请日：2013-02-07
申请人： Christel Jeanne Marie MENET , Benoit Antoine SCHMITT , Raphael Jean Joel GENEY , Kevin James DOYLE , Joanne PEACH , Nicholas John PALMER , Graham Peter JONES , David HARDY , James Edward Stewart DUFFY
发明人： Christel Jeanne Marie MENET , Benoit Antoine SCHMITT , Raphael Jean Joel GENEY , Kevin James DOYLE , Joanne PEACH , Nicholas John PALMER , Graham Peter JONES , David HARDY , James Edward Stewart DUFFY
IPC分类号： C07D471/04 , A61K31/506 , A61K31/496 , A61K31/541 , A61K31/4545 , A61K31/5377 , A61K31/497 , A61K45/06 , A61K31/444 , A61K31/437 , C07D491/107
CPC分类号： C07D471/04 , A61K31/437 , A61K31/444 , A61K31/4545 , A61K31/496 , A61K31/497 , A61K31/506 , A61K31/5377 , A61K31/541 , A61K45/06 , C07D403/12 , C07D491/107
摘要： Novel imidazolopyridines according to Formula I, able to inhibit JAK are disclosed, these compounds may be prepared as a pharmaceutical composition, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, allergic or inflammatory conditions, autoimmune diseases, proliferative diseases, transplantation rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 or interferons. Wherein R1, L1, R3, R4, Cy, L2 and R5 are as defined herein.
摘要翻译：公开了能够抑制JAK的式I的新型咪唑并吡啶，这些化合物可以制备成药物组合物，并且可以用于预防和治疗包括人在内的哺乳动物中的各种病症，包括通过非限制性的方式例如过敏或炎症状况，自身免疫性疾病，增殖性疾病，移植排斥反应，涉及软骨周转损害的疾病，先天性软骨畸形和/或与IL6或干扰素分泌过多相关的疾病。其中R1，L1，R3，R4，Cy，L2和R5如本文所定义。

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