发明名称 Tetrazole compounds as calcium channel blockers
摘要 The present invention relates to novel tetrazole compounds of Formula (I) wherein A is (II) or (III); to processes for their preparation; to pharmaceutical compositions containing the compounds; and to the use of the compounds in therapy to treat diseases for which blocking the Cav2.2 calcium channels is beneficial.; wherein A is ;
申请公布号 US9115132(B2) 申请公布日期 2015.08.25
申请号 US201113808243 申请日期 2011.07.08
申请人 Convergence Pharmaceuticals Limited 发明人 Beswick Paul;Gleave Robert James;Hachisu Shuji;Vile Sadie;Bertheleme Nicholas;Ward Simon E.
分类号 A61K31/41;C07D401/14;C07D403/06;C07D413/06;C07D417/06;C07D471/04;C07D471/10;C07D487/04;C07D487/08;C07D491/08;C07D513/04;C07D257/04;C07D257/06 主分类号 A61K31/41
代理机构 Foley & Lardner LLP 代理人 Foley & Lardner LLP
主权项 1. A compound of formula (I), or a salt thereof: wherein A is R1 is hydrogen, methyl or chloro; R2 is hydrogen, trifluoromethyl, trifluoromethoxy, chloro or cyano; R3 is hydrogen, cyano, trifluoromethyl, trifluoromethoxy, difluoromethoxy, chloro, bromo, —S—CH3, —SO2—C1-3alkyl or —SF5; R4 is hydrogen, trifluoromethyl, trifluoromethoxy, chloro or cyano; R5 is hydrogen, methyl or chloro; wherein at least one of R1, R2, R3, R4 or R5 is a group other than hydrogen; X is —CH2—, —CH2—CH2— or —CH(CH3)—; wherein when R1 is methyl, R5 is hydrogen or chloro, and when R5 is methyl, R1 is hydrogen or chloro; wherein when R2 is chloro, R4 is hydrogen, trifluoromethyl, trifluoromethoxy or cyano, and when R4 is chloro, R2 is hydrogen, trifluoromethyl, trifluoromethoxy or cyano; R6 is hydrogen and R7 is C1-5 alkyl or C3-6cycloalkyl; or R6 and R7 together with the nitrogen atom to which they are attached form a saturated ring system B, where B is selected from a) a 4 to 7 membered monocyclic heterocyclic ring, b) a 5 to 10 membered fused bicyclic ring system; c) a bridged 4 to 7 membered monocyclic heterocyclic ring system; and d) a 7 to 11 membered spiro ring system; which ring system B is unsubstituted or substituted with 1 to 3 substituents independently selected from halogen, oxo, C1-3 alkyl, cyano, —SO2—C1-3 alkyl, C1-3 haloalkyl and —CO—C1-3alkyl; with the proviso that the compound is not 4-({1-[3-(trifluoromethyl)phenyl]-1H-tetrazol-5-yl}methyl)morpholine hydrochloride, 4-({1-[3-(trifluoromethyl)phenyl]-1H-tetrazol-5-yl}methyl)morpholine, 4-{[1-(3,4-dichlorophenyl)-1H-tetrazol-5-yl]methyl}morpholine, 1-{[1-(4-chlorophenyl)-1H-tetrazol-5-yl]methyl}-4-(methylsulfonyl)piperazine, 1-{[1-(4-chlorophenyl)-1H-tetrazol-5-yl]methyl}-4-(propylsulfonyl)piperazine; 1-{[1-(3,4-dichlorophenyl)-1H-tetrazol-5-yl]methyl}piperidine; 4-{[1-(4-chlorophenyl)-1H-tetrazol-5-yl]methyl}morpholine; 1-{[1-(4-chlorophenyl)-1H-tetrazol-5-yl]methyl}-4-methylpiperidine; 1-{[1-(4-chlorophenyl)-1H-tetrazol-5-yl]methyl}piperidine; 1-{[1-(4-chlorophenyl)-1H-tetrazol-5-yl]methyl}-4-(ethylsulfonyl)piperazine; 1-{[1-(4-chlorophenyl)-1H-tetrazol-5-yl]methyl}-2-methylpiperidine; 1-{[1-(4-chlorophenyl)-1H-tetrazol-5-yl]methyl}piperazine; 1-(4-chlorophenyl)-5-(1-pyrrolidinylmethyl)-1H-tetrazole; 1-{[1-(4-chlorophenyl)-1H-tetrazol-5-yl]methyl}-4-methylpiperazine or 1-{[1-(4-chlorophenyl)-1H-tetrazol-5-yl]methyl}hexahydro-1H-azepine.
地址 London GB