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Geminal substituted quinuclidine amide compounds as nicotinic alpha-7 acetylcholine receptor agonists
专利权人:
Axovant Sciences GmbH
发明人:
ACHARYA, Raksha,BURNETT, Duane A.,BURSAVICH, Matthew Gregory,COOK, Andrew Simon,HARRISON, Bryce Alden,KOENIG, Gerhard,MCRINER, Andrew J.
申请号:
ES15870786
公开号:
ES2764660T3
申请日:
2015.12.14
申请国别(地区):
ES
年份:
2020
代理人:
摘要:
A geminal substituted quinuclidine amide compound represented by formula (I): ** (See formula) ** wherein the moiety C (R1) (R2) forms a carbocycle (3-4 membered), where R1 and R2 taken together represent a C2-C3 alkyl di-radical; wherein the C2-C3 alkyl di-radical can be substituted with up to 4 radical substituents comprising: -D, -F, -Cl, -Br, -I, -CN, CH3, CH2CH3, = O, -OR3 or -OCF3; R3 independently represents -H; a branched or unbranched C1-C4 alkyl radical; C3-C4 cycloalkyl radical; wherein the C1-C4 alkyl radical and the C3-C4 cycloalkyl radical can be substituted with up to 4 radical substituents comprising: -D, -F, -Cl, -Br, -I, -CN, = O, -OH , -O-C1-C4 alkyl or -OCF3; and W represents a residue represented by the MI, M-II, M-III, M-IV, MV or M-VI ring system: ** (See formula) ** where: Z1, Z2, Z3, Z4 and Z5 independently represent N or CR4; provided that no more than two of Z1, Z2, Z3, Z4 and Z5 are N; R4 independently represents -H; -D; -F; -Cl; -Br; -I; -CN; -NO2; -OR5; -N (R5) (R6); -SO2 (CH2) mR5; - (CO) (CH2) mR5; - (CO) N (R5) (R6); -OCF3; a C1-C6 alkyl radical; a C1-C6 haloalkyl radical; a C3-C6 cycloalkyl radical; a heterocycloalkyl radical (3-6 membered); an aryl radical; or a heteroaryl radical; or when adjacent members of Z1, Z2, Z3, Z4 and Z5 are (CR4) (CR4), (CR4) (CR4) can form a ring such that the adjacent R4 substituents taken together represent a heteroalkyl di-radical (from 3 -6-membered) with at least one ring atom of the di-heteroalkyl radical (3-6 membered) selected from the group consisting of oxygen, nitrogen, and sulfur, provided that when the at least one ring atom is nitrogen, the nitrogen is substituted with -H, a branched or unbranched C1-C4 alkyl radical, a C3-C4 cycloalkyl radical, - (CO) -branched or unbranched C1-C4 alkyl, or - (SO2) -C1 alkyl -C4 branched or unbranched, wherein the C1-C4 alkyl radical and the C3-C4 cycloalkyl radical can be substituted with up to 4 radical substituents comprising: -D, halogen, = O, -OH, -O
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