发明名称 BICYCLIC AZA COMPOUNDS AS MUSCARINIC M1 RECEPTOR AGONISTS
摘要 This invention relates to compounds (Formula (1)) 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 where R1-R5, X1, X2 and p are as defined herein.;
申请公布号 US2015232443(A1) 申请公布日期 2015.08.20
申请号 US201314428927 申请日期 2013.09.18
申请人 Heptares Therapeutics Limited 发明人 Brown Giles Albert;Cansfield Julie Elaine;Congreve Miles Stuart;Pickworth Mark;Tehan Benjamin Gerald
分类号 C07D401/04 主分类号 C07D401/04
代理机构 代理人
主权项 1. A compound of the formula (1): or a salt thereof, wherein: p is 0, 1 or 2; X1 and X2 are saturated hydrocarbon groups which together contain a total of five to nine carbon atoms and which link together such that the moiety: forms a bicyclic ring system; R1 is a C1-10 non-aromatic hydrocarbon group which is optionally substituted with one to six fluorine atoms and wherein one or two, but not all, carbon atoms of the hydrocarbon group may optionally be replaced by a heteroatom selected from O, N and S and oxidised forms thereof; R2 is hydrogen or a C1-10 non-aromatic hydrocarbon group; or R1 and R2 together with the nitrogen atom to which they are attached form a non-aromatic heterocyclic ring 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 substitutents selected from C1-2 alkyl; fluorine; and cyano; R3 is selected from hydrogen; halogen; cyano; hydroxy; C1-3 alkoxy; and a C1-5 non-aromatic hydrocarbon group which is optionally substituted with one to six fluorine atoms and wherein one or two, but not all, carbon atoms of the hydrocarbon group may optionally be replaced by a heteroatom selected from O, N and S; R4 is a C1-6 non-aromatic hydrocarbon group which is optionally substituted with one to six fluorine atoms and wherein one or two, but not all, carbon atoms of the hydrocarbon group may optionally be replaced by a heteroatom selected from O, N and S and oxidised forms thereof; and R5 is fluorine.
地址 Welwyn Garden City GB