发明申请
- 专利标题: AZACYCLIC COMPOUNDS AS INHIBITORS OF SENSORY NEURONE SPECIFIC SODIUM CHANNELS
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申请号: US11993557申请日: 2006-07-07
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公开(公告)号: US20100204224A1公开(公告)日: 2010-08-12
- 发明人: Richard Hamlyn , Glyn Addison , Christopher Geoffrey Earnshaw , Harry Finch , Mike Huckstep , Rosemary Lynch , Sarah Mellor
- 申请人: Richard Hamlyn , Glyn Addison , Christopher Geoffrey Earnshaw , Harry Finch , Mike Huckstep , Rosemary Lynch , Sarah Mellor
- 申请人地址: GB Winnersh
- 专利权人: VERNALIS R & D LIMITED
- 当前专利权人: VERNALIS R & D LIMITED
- 当前专利权人地址: GB Winnersh
- 优先权: GB0514018.1 20050707
- 国际申请: PCT/GB2006/002539 WO 20060707
- 主分类号: A61K31/5377
- IPC分类号: A61K31/5377 ; C07D471/08 ; A61K31/4995 ; C07D487/10 ; A61K31/407 ; C07D487/04 ; A61P13/10 ; A61P25/00
摘要:
Compounds of the formula (I), and pharmaceutically acceptable salts thereof, are found to be antagonists of SNS sodium channels. They are therefore useful as analgesic and neuroprotective agents; wherein (1) represents (A), (B) or (C); R1 represents: (a) -L-A or L′-A′ wherein L represents a bond or a C1-C6 alkyl, C2-C6 alkenyl or C2-C6 alkynyl moiety, A represents a phenyl, 5- to 10-membered heteroaryl, C3-C6 carbocyclyl or 5- to 10 membered heterocyclyl group, L′ represents a C1-C6 alkyl, C2-C6 alkenyl or C2-C6 alkynyl moiety, and A′ represents -Het-A or —X-A wherein Het represents —O—, —S— or NR′, and X represents —CO—, —SO—, SO2—, —CO—O—, CO—S, CONR′, —O—CO—, —S—CO— or NR′—CO—, wherein R′ represents hydrogen or C1-C6 alkyl; (b) -L-A-A′ or -L-A-L-A wherein A′ is as defined above, each A is the same or different and is as defined above and each L is the same or different and is as defined above; (c) -A-Z-A wherein Z is -Het-L′, —X-L′, -L′-Het- or L′-X, wherein Het, L′ and X are as defined above and each A is the same or different and is as defined above; (d) -A-Het-Y or -A-X—Y wherein is [L′-Het]n-L′, [L′-Het]n-L′, -[L′-Het]n-A, -L′-B-L′, -L′-B-A or -A-L-A wherein n is from 1 to 4 and B is —X—, —NR′—CO—NR′, —O—CO—NR′— or —NR′—CO—O, and wherein X and L are as defined above, each A is the same or different and is as defined above, each L′ is the same or different and is as defined above, each R′ is the same or different and is as defined above and each Het is the same or different and is as defined above; or (e) -L-CR(A)(A′) or L-CR(A)(L-A) wherein R is hydrogen or C1-C4 alkyl, A′ is as defined above, each L is the same or different and is as defined above and each A is the same or different and is as defined above; R2 represents -L-A-, L′-A′, -L-A-A′ or L-A-L-A wherein L′ and A′ are as defined above, each L is the same or different and is as defined above and each A is the same or different and is as defined above J represents —NR3—, —O— or a direct bond wherein R3 represent s hydrogen C1-C6 alkyl, C2-C6 alkenyl or C2-C6 alkynyl; p is an integer from 1 to 3; q is 1 or 2; and one of E and E′ is —CH2— and the other is a direct bond.
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