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1. 发明授权

US06713514B1 PPAR-&ggr; agonists as agents for the treatment of type II diabetes 失效
标题翻译： PPAR-γ激动剂作为治疗II型糖尿病的药物
公开(公告)号：US06713514B1
公开(公告)日：2004-03-30
申请号：US09552477
申请日：2000-04-18
申请人： Hartmuth C. Kolb , Gerard McGeehan , Zhi-Cai Shi , Laxma Reddy Kolla , Cullen Cavallaro
发明人： Hartmuth C. Kolb , Gerard McGeehan , Zhi-Cai Shi , Laxma Reddy Kolla , Cullen Cavallaro
IPC分类号： A61K31195
CPC分类号： C07C323/42 , C07C237/30 , C07C237/38 , C07C2601/08 , C07C2601/14
摘要： N-(substituted)carbamoylaryl- and heteroaryl substituted aminopropanoic and butanoic acid compounds which are highly selective agonists for the PPAR-&ggr; receptor or prodrugs of agonists for the PPAR-&ggr; receptor, and are useful in the treatment of Type II diabetes (NIDDM). Specifically disclosed are compounds of the formula: or the pharmaceutically acceptable non-toxic salts thereof wherein: Z is aryl or heteroaryl; n and m are 0, 1 or 2; A is a carboxylic acid or ester; or A is where D, F and G are hydrogen, (un)substituted amino, (un)substituted alkoxy, methylene or an (un)substituted sulfide; R4 is oxo, hydrogen, hydroxy, lower alkyl, lower alkoxy, cycloalkyl, keto, acyl, or sulfonyl; Y is hydrogen, (un)substituted amino, (un)substituted alkoxy, methylene, an (un)substituted sulfide, (un)substituted sulfonyl or an (un)substituted sulfoxide; and R5, R6 and R8 are hydrogen, lower alkyl, lower alkoxy, cycloalkyl, keto, acyl, or sulfonyl; or R5 and R6 together form a ring.
摘要翻译：作为PPAR-γ受体的高选择性激动剂或PPAR-γ受体激动剂前药的N-（取代的）氨基甲酰基芳基和杂芳基取代的氨基丙酸和丁酸化合物，可用于治疗II型糖尿病（NIDDM）。具体公开的是下式的化合物或其药学上可接受的无毒盐，其中：Z是芳基或杂芳基; n和m是0,1或2; A是羧酸或酯; 或A是其中D，F和G是氢，（未）取代的氨基，（未）取代的烷氧基，亚甲基或（取代的）取代的硫醚; R 4是氧代，氢，羟基，低级烷基，低级烷氧基，环烷基，酮基，酰基，或磺酰基; Y是氢，（未）取代的氨基，（未）取代的烷氧基，亚甲基，（未）取代的硫醚，（未）取代的磺酰基或（取代的）取代的亚砜; R 5，R 6和R 8是氢，低级烷基，低级烷氧基，环烷基，酮基，酰基或磺酰基; 或R 5和R 6一起形成环。

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