发明名称 Azetidine compounds, compositions and methods of use
摘要 Provided are compounds of Formula I, R1-L1-A-L2-R2  (I), and stereoisomers, tautomers and pharmaceutically acceptable salts thereof, wherein A, L1, L2, R1 and R2 are defined herein. The present invention also provides a pharmaceutical composition and methods of using such compounds. The compounds are useful for therapy and/or prophylaxis in a patient, and in particular to inhibitors of Soluble Epoxide Hydrolase (sEH).
申请公布号 US8809552(B2) 申请公布日期 2014.08.19
申请号 US201213661072 申请日期 2012.10.26
申请人 Hoffmann-La Roche Inc. 发明人 Ceccarelli Simona M.;Guerot Carine;Knust Henner
分类号 C07D205/04;A61K31/397;C07D487/04;C07D487/10 主分类号 C07D205/04
代理机构 代理人
主权项 1. A compound of Formula (I): R1-L1-A-L2-R2  (I)wherein: A is wherein X is NH or CH2; Y is N or CH; L1 is selected from the group consisting of a bond, —(CH2)1-3—, —NH—(CH2)0-3—C(O)—, —(CH2)0-3—C(O)—, —(CH2)0-3—SO2— and —(CH2)0-3—NR3—C(O)—; L2 is selected from the group consisting of a bond, —(CH2)1-3—, —(CH2)0-3—C(O)—NH—,—NH—(CH2)0-3—C(O)—NH—,—(CH2)0-3—C(O)—, —(CH2)0-3—SO2— and —(CH2)0-3—NR3—C(O)—; R1 is selected from the group consisting of phenyl, 5- or 6-membered heteroaryl, adamantyl and —(CH2)1-3-phenyl, wherein said phenyl, heteroaryl or adamantyl is unsubstituted or substituted by one to three R5 groups; R2 is selected from the group consisting of phenyl, 5- or 6-membered heteroaryl and —(CH2)1-3-phenyl, wherein said phenyl or heteroaryl is unsubstituted or substituted by one to three R5 groups; R3 is hydrogen or lower alkyl; R4 is hydrogen or lower alkyl; and R5 is selected from the group consisting of halogen, lower alkyl, lower haloalkyl, lower haloalkoxy, and —C(O)OR4, or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof, with the proviso that said compound is not (4-bromophenyl)[6-[(4-methylphenyl)sulfonyl]-1,6-diazaspiro[3,3]hept-1-yl]methanone, 6-[(4-methylphenyl)sulfonyl]-1-(phenylmethyl)-1,6-diazaspiro[3,3]heptane, 2,6-bis[(4-methylphenyl)sulfonyl]-2,6-diazaspiro[3,3]heptane or 2-phenyl-6-(phenylmethyl)-2,6-diazaspiro[3,3]heptane, and the further provisos that when L2 is —C(O)—NH—, L1 is not —CH2—; when L2 is —CH2—, L1 is not a bond; when L2 is —SO2—, L1 is not —CH2—; and L1 and L2 are different.
地址 Nutley NJ US