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    • 6. 发明申请
    • Calcium channel blockers
    • 钙通道阻滞剂
    • US20070185105A1
    • 2007-08-09
    • US11601005
    • 2006-11-16
    • Terrance SnutchGerald Zamponi
    • Terrance SnutchGerald Zamponi
    • A61K31/5375A61K31/495A61K31/445
    • C07D295/185A61K31/4468A61K31/451A61K31/4515A61K31/454A61K31/4545A61K31/495A61K31/496A61K31/498A61K31/506A61K31/5375A61K31/538A61K31/5415C07D211/14C07D211/16C07D211/46C07D211/58C07D213/38C07D277/74C07D277/82C07D295/03C07D317/60C07D401/04C07D401/14
    • Compounds of the formula wherein m is 0, 1 or 2; wherein when m is 0, Z is O, when m is 1, Z is N, and when m is 2, Z is C; Y is H, OH, NH2, or an organic moiety of 1-20 C, optionally additionally containing 1-8 heteroatoms selected from the group consisting of N, P, O, S and halo; each 11 1 and 12 is independently 0-5; 13 is O or 1; each of R1, R2 and R3 is independently alkyl (1-6 C), aryl (6-10 C) or arylalkyl (7-16 C) optionally containing 1-4 heteroatoms selected from the group consisting of halo, N, P, O, and S or each of R1 and R2 may independently be halo, COOR, CONR2, CF3, CN or NO2, wherein R is H or lower alkyl (1-4 C) or alkyl (1-6 C); n is 0 or 1; X is a linker; with the proviso that Y is not a tropolone, a coumarin, or an antioxidant containing an aromatic group and with the further proviso that if 13 is 0, and either 11 and 12 is 0 or 1 and if R1 and/or R2 represent F in the para position, Z cannot be C or N; and are useful to treat pain. Libraries of these compounds can also be used to identify antagonists for other targets.
    • 下式的化合物其中m为0,1或2; 其中当m为0时,Z为O,当m为1时,Z为N,当m为2时,Z为C; Y是H,OH,NH 2或1-20C的有机部分,任选地另外含有1-8个选自N,P,O,S和卤素的杂原子; 每个1&lt; 1&gt; 1和1&lt; 2&gt;独立地为0-5; 1 3是O或1; R 1,R 2和R 3各自独立地为烷基(1-6C),芳基(6-10C)或芳基烷基 (7-16C)任选地含有1-4个选自卤素,N,P,O和S的杂原子或者R 1和R 2各自的1-4个杂原子, 可以独立地为卤素,COOR,CONR 2,CF 3,CN或NO 2,其中R为H或低级烷基(1-4 C)或(1-6C)烷基; n为0或1; X是一个连接子; 条件是Y不是托普洛尔,香豆素或含有芳族基团的抗氧化剂,进一步的条件是,如果1 <3>和0 <1> 和1 是0或1,如果R 1和/或R 2在对位表示F,则Z不能为C或N ; 并且可用于治疗疼痛。 这些化合物的文库也可用于鉴定其他靶标的拮抗剂。