发明名称 P2X7 MODULATORS
摘要 The present invention is directed to compounds of Formulas (I, IIa and IIb):;;The invention also relates to pharmaceutical compositions comprising compounds of Formulas (I, IIa and IIb). Methods of making and using the compounds of Formulas (I, IIa and IIb) are also within the scope of the invention.
申请公布号 US2014275015(A1) 申请公布日期 2014.09.18
申请号 US201414212669 申请日期 2014.03.14
申请人 Janssen Pharmaceutica NV 发明人 Alcazar Vaca Manuel Jesus;Andres Gil Jose Ignacio;Chrovian Christa C.;Coate Heather R.;De Angelis Meri;Dvorak Curt A.;Gelin Christine F.;Letavic Michael A.;Savall Brad M.;Soyode-Johnson Akinola;Stenne Brice M.;Swanson Devin M.
分类号 C07D471/04 主分类号 C07D471/04
代理机构 代理人
主权项 1. A compound of Formula I: wherein: R1 is (a) phenyl, optionally substituted with zero to four groups selected from the group consisting of: halo, C1-C4alkyl, alkoxy, perhaloalkyl and perhaloalkoxy; or(b) heteroaryl, selected from the group consisting of: wherein Rk is selected from the group consisting of: H, halo, C1-C3alkyl and alkoxy;Rj is selected from the group consisting of: H, C1-C3alkyl optionally substituted with halo, OH and alkoxy; andn is an integer from 0-3;X is N or CR2;R2 is H, perhaloalkyl or C1-C3 lower alkyl; R3 is H, perhaloalkyl, C1-C4 alkyl, alkalkoxy, CH2Ri, —C(O)Re or phenyl; wherein phenyl is optionally substituted with zero to two groups selected from the group consisting of: halo, C1-C3alkyl, alkoxy, perhaloalkyl and perhaloalkoxy; Ri is OH, OC1-C3 alkyl, NC3H6, N(C1-C3alkyl)2 or halo;Re is OH, OC1-C3 alkyl, N(C1-C3alkyl)2, or NC3H6;R4 and R5 are H or C1-C3 alkyl; and R8 is phenyl or pyridyl; optionally substituted with zero to four Rm substituents wherein Rm is selected from the group consisting of: halo, C1-C3alkyl, alkoxy, perhaloalkyl and perhaloalkoxy; or R8 is selected from the group consisting of:  and pharmaceutically acceptable salts of compounds of Formula (I).
地址 Beerse BE