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Heterobicyclo-substituted compounds- [1,2,4] triazolo [1,5-c] quinazolin-5-amine suitable for the treatment or prevention of central nervous system disorders
专利权人:
MERCK SHARP & DOHME CORP.
发明人:
ALI, Amjad,LO, Michael Man-Chu,LIM, Yeon-Hee,STAMFORD, Andrew,KUANG, Rongze,TEMPEST, Paul,YU, Younong,HUANG, Xianhai,HENDERSON, Timothy,KIM, Jae-Hun,BOYCE, Christopher,TING, Pauline,ZHENG, Junying,MET
申请号:
ES13866588
公开号:
ES2667477T3
申请日:
2013.12.20
申请国别(地区):
ES
年份:
2018
代理人:
摘要:
compound of Formula GI: *** Formula ** or a pharmaceutically acceptable salt thereof, in which: W is nitrogen or carbon; m is 1, 2, 3 or 4; n is an integer from 0 to 4, where the sum of n + m is at least 2 to 4, and where, when W is N, m is at least 2; Gd1 to Gd4 are independently hydrogen or a C1-6 alkyl; p is 1 or 2; X, Y and Z together with W and the carbon to which X and W are linked form an aromatic or heteroaromatic moiety of 5 to 6 members, and are independently: (a) - (RG1) C>; =, in which RG1 is : (i) hydrogen; (ii) C1-8 alkyl, optionally substituted with one or more halogen atoms; (iii) -C (O) -C 1-8 alkyl; (iv) -CN; (v) -S-C1-8 alkyl; (vi) -O-C1-6 alkyl; (vii) - (CH2) q1- (C>; = O) q2-N (R2) 2, where R2 25 is independently each time hydrogen appears, C1-6 alkyl or heteroaryl, and where q1 is 0 or 1 and q2 is 0 or 1; (viii) -C (O) O-C1-8 alkyl; (ix) halogen; (x) a mono or polycyclic heterocyclic moiety comprising up to 10 carbon atoms and one or more heteroatoms selected from N, S or O, optionally substituted with one or more C1-6 alkyl, morpholino, phenyl (optionally substituted with halogen), heteroaryl or halogen; (xi) aryl, which is optionally substituted with one or more substituents that are: (1) halogen; or (2) C1-6 alkyl which is optionally substituted with one or more halogen atoms; (xii) -NH-C (O) -R3, wherein R3 is C1-6 alkyl or heteroaryl; or (xiii) heteroaryl, which is optionally substituted with C1-6 alkyl (which is optionally substituted with one or more halogen atoms) or amino; or (b)>; NRG2, in which RG2 is: (i) hydrogen; (ii) C1-8 alkyl; or (iii) an aromatic moiety of up to 10 carbon atoms; (c) -N>; =; (d) -O-; or (e) -S-; and RG3 is a remainder of the structure: ** Formula ** in which: t is 0, 1 or 2; RG5 and RG6 are independently each time they appear: (a) H; (b) C1-10 alkyl, optionally substituted with one or more fluorine atoms; or (c) RG5 and RG6 taken together form a carbonyl moiety (C>; = O), with the proviso that if t>
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