发明名称 Muscarinic M1 receptor agonists
摘要 This invention relates to compounds that are agonists of the muscarinic M1 receptor and which are useful in the treatment of muscarinic M1 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds provided are of formula I, where n is 1 or 2; p is 0, 1 or 2; q is 0, 1 or 2; and R1-R6 are as defined herein.;
申请公布号 US9573929(B2) 申请公布日期 2017.02.21
申请号 US201514941328 申请日期 2015.11.13
申请人 Heptares Therapeutics Limited 发明人 Congreve Miles Stuart;Brown Giles Albert;Cansfield Julie Elaine;Tehan Benjamin Gerald
分类号 A61K31/55;C07D401/04;C07D211/06;C07D401/14 主分类号 A61K31/55
代理机构 McCarter & English, LLP 代理人 McCarter & English, LLP ;Davis Steven G.;Bai Mei
主权项 1. A compound of the formula: or a salt thereof, wherein: R1 is selected from 2-methylpropyl, tert-butyl, 2-methylbutyl, 2,2-dimethylpropyl, 2-methylbut-2-yl, cyclobutylmethyl, cyclopropylmethyl, cyclopentylmethyl, isopropyl, 1-methylcyclohexyl, 1-methylcyclopentylmethyl, 2-cyclopropylpropyl, 1-methylcyclobutyl, cyclopentyl, 2,3-dimethylbutan-2-yl, 1-ethylcyclobutylmethyl, 1-methylcyclopentyl, 2-cyclopropylpropan-2-yl, cyclobutyl, 1-methylcyclobutylmethyl, 1-(trifluoromethyl)cyclobutyl, 1-ethylcyclobutyl, (2H3)methyl(2H6)propyl and 2-methylpentan-2-yl; R2 is selected from hydrogen, methyl, ethyl and isopropyl; or R1 and R2 together with the nitrogen atom to which they are attached form a non-aromatic heterocyclic group of four to nine ring members, wherein the heterocyclic ring may optionally contain a second heteroatom selected from O, N and S and oxidised forms thereof; and wherein the heterocyclic ring may optionally be substituted with one to six more substitutents selected from C1-2 alkyl; fluorine; and cyano; R3 is selected from hydrogen; fluorine; cyano; methoxy and methyl; and R4 is selected from methyl, ethyl, ethynyl and 1-propynyl.
地址 Welwyn Garden City, Hertfordshire GB