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1. 发明授权

US08716287B2 Pharmaceutical compounds 有权
标题翻译：药物化合物
公开(公告)号：US08716287B2
公开(公告)日：2014-05-06
申请号：US13697743
申请日：2011-05-12
申请人： Robert George Boyle , David Winter Walker , Richard Justin Boyce
发明人： Robert George Boyle , David Winter Walker , Richard Justin Boyce
IPC分类号： A61K31/535 , C07D241/00
CPC分类号： C07D241/26 , A61K31/4965 , A61K31/497 , A61K31/5377 , A61N5/10 , C07D241/20 , C07D403/12 , C07D405/12 , C07D413/12
摘要： A compound of the formula (I):
摘要翻译：式（I）的化合物：

2. 发明申请

US20130065900A1 PHARMACEUTICAL COMPOUNDS 有权
标题翻译：药物化合物
公开(公告)号：US20130065900A1
公开(公告)日：2013-03-14
申请号：US13697743
申请日：2011-05-12
申请人： Robert George Boyle , David Winter Walker , Richard Justin Boyce
发明人： Robert George Boyle , David Winter Walker , Richard Justin Boyce
IPC分类号： A61K31/5377 , C07D241/26 , C07D405/12 , C07D403/12 , A61K31/4965 , A61N5/10 , C07D413/12 , C07D413/02 , A61K31/497 , C07D403/02
CPC分类号： C07D241/26 , A61K31/4965 , A61K31/497 , A61K31/5377 , A61N5/10 , C07D241/20 , C07D403/12 , C07D405/12 , C07D413/12
摘要： The invention provides a compound of the formula (1): or a salt, N-oxide or tautomer thereof; wherein R1 is cyano or C1-4 alkyl; R2 is hydrogen or C1-4 alkyl; R3 is hydrogen or C1-4 alkyl; R4 and R5 are the same or different and each is selected from hydrogen, saturated C1-4 hydrocarbyl and saturated C1-4 hydrocarbyloxy; R6 and R7 are the same or different and each is selected from hydrogen, halogen, CN, C1-4 alkyl and C1-4 alkoxy wherein the C1-4 alkyl and C1-4 alkoxy are each optionally substituted with hydroxy, C1-2 alkoxy or by one or more flourine atoms; R8 is hydrogen or C1-4 alkyl; Q is an alkylene chain of 1 to 4 carbon atoms in length between the moiety Ar and the nitrogen atom N, wherein one or more of the 1 to 4 carbon atoms of the alkylene chain may optionally be substituted with one or two C1-4 alkyl groups, or wherein one carbon atom of the 1 to 4 carbon atoms of the alkylene chain may optionally be substituted with a group —CH2CH2— which together with the said one carbon atom forms a cyclopropyl group; m is 1, 2, 3 or 4; n is 0 or 1; and Ar is a monocyclic or bicyclic aryl or heteroaryl group of 5 to 10 ring members containing 0, 1, 2, 3 or 4 heteroatom ring members selected from O, N and S, the aryl or heteroaryl group being optionally substituted with one to four substituents R13 as defined in the claims.The compounds are inhibitors of Chk-1 kinase and are active against cancers.
摘要翻译：本发明提供式（1）化合物或其盐，N-氧化物或其互变异构体; 其中R1是氰基或C1-4烷基; R2是氢或C1-4烷基; R3是氢或C1-4烷基; R4和R5相同或不同，各自选自氢，饱和C 1-4烃基和饱和C 1-4烃氧基; R 6和R 7相同或不同，各自选自氢，卤素，CN，C 1-4烷基和C 1-4烷氧基，其中C 1-4烷基和C 1-4烷氧基各自任选被羟基，C 1-2烷氧基或通过一个或多个荧光原子; R8是氢或C1-4烷基; Q是部分Ar和氮原子N之间的长度为1至4个碳原子的亚烷基链，其中亚烷基链的1至4个碳原子中的一个或多个可以任选被一个或两个C 1-4烷基取代基团，或其中亚烷基链的1至4个碳原子的一个碳原子可以任选被基团-CH 2 CH 2取代，所述基团与所述一个碳原子一起形成环丙基; m为1,2,3或4; n为0或1; 并且Ar是具有0至1个，2个，3个或4个选自O，N和S的杂原子环成员的5至10个环成员的单环或双环芳基或杂芳基，芳基或杂芳基任选被一至四个取代基R 13如权利要求中所定义。这些化合物是Chk-1激酶的抑制剂并且对癌症有活性。

3. 发明申请

US20100063065A1 THIOPHENE DERIVATIVES AS PPAR AGONISTS I 审中-公开
标题翻译：噻吗衍生物作为PPAR激动剂I
公开(公告)号：US20100063065A1
公开(公告)日：2010-03-11
申请号：US12088333
申请日：2006-09-28
申请人： Andrew Ayscough , David Rodyney Owen , Paul Meo , David James Pearson , Yvonne Walker , Richard Justin Boyce , Fabio Zuccotto
发明人： Andrew Ayscough , David Rodyney Owen , Paul Meo , David James Pearson , Yvonne Walker , Richard Justin Boyce , Fabio Zuccotto
IPC分类号： A61K31/381 , C07D333/36 , C07D409/10 , A61K31/506 , A61K31/4436 , A61P3/10 , A61P3/04 , A61P17/02 , A61P29/00 , A61P25/00
CPC分类号： C07D333/36
摘要： The invention discloses compounds of formula (I); wherein: R is a carboxylic acid or a derivative thereof; R1 is alkyl, alkenyl, alkynyl, cycloalkyl, alkoxy, alkylthio, halo or trihalomethyl; R2 is aryl, heteroaryl, arylalkyl or heteroarylalkyl; R3 is H or F; and L is a linking group comprising a chain of from 2 to 8 atoms linking R and the carbonyl group (A); and pharmaceutically acceptable derivatives thereof, useful for treating disorders mediated by peroxisome-proliferator-activated receptor (PPAR) subtype δ (PPARδ). The compounds of the invention are therefore useful in the treatment of metabolic syndrome, obesity, type-II diabetes, dyslipidemia, wound healing, inflammation, neurodegenerative disorders and multiple sclerosis.
摘要翻译：本发明公开了式（I）的化合物; 其中：R是羧酸或其衍生物; R1是烷基，烯基，炔基，环烷基，烷氧基，烷硫基，卤代或三卤代甲基; R2是芳基，杂芳基，芳基烷基或杂芳基烷基; R3为H或F; L是包含连接R和羰基（A）的2至8个原子的链的连接基团; 和其药学上可接受的衍生物，其可用于治疗由过氧化物酶体增殖物激活受体（PPAR）亚型δ（PPARδ）介导的病症。因此，本发明的化合物可用于治疗代谢综合征，肥胖症，II型糖尿病，血脂异常，伤口愈合，炎症，神经变性疾病和多发性硬化。

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