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    • 3. 发明申请
    • 2,3,4-SUBSTITUTED CYCLOPENTANONES AS THERAPEUTIC AGENTS
    • 作为治疗药物的2,3,4-替代环孢素
    • WO2006055481A1
    • 2006-05-26
    • PCT/US2005/041171
    • 2005-11-14
    • ALLERGAN , INC.DONDE, YarivBURK, Robert, M.GARST, Michael, E.NGUYEN, Jeremiah, H.
    • DONDE, YarivBURK, Robert, M.GARST, Michael, E.NGUYEN, Jeremiah, H.
    • C07C405/00C07D333/60C07D333/62A61P27/06A61K31/5575
    • C07D333/62C07C405/0025C07D333/56
    • Disclosed herein are compounds comprising Formula (I) or a pharmaceutically acceptable salt or a prodrug thereof, wherein a dashed line represents the presence or absence of a bond; Y is a carboxylic acid, sulfonic acid, or phosphonic acid functional group; or an amide or ester thereof comprising from 0 to 12 carbon atoms; or Y is hydroxymethyl or an ether thereof comprising from 0 to 12 carbon atoms; or Y is a tetrazolyl functional group; A is -(CH 2 ) 6 -, cis -CH 2 -CH=CH-(CH 2 ) 3 -, or -CH2-C =- C-(CH 2 ) 3 - wherein 1 or 2 carbons may be substituted with S or O; B is hydrogen, C 1-6 hydrocarbyl, CN, CO2H , or -(CH 2 ) m X(CH 2 ) p H, wherein m is at least 1 and the sum of m and p is from 1 to 5; X is S or O; J is H, CH 3 , or CF 3 D is a covalent bond, CH 2 . O, or S; and E is an aromatic heterobicyclic ring system which may have substituents comprising up to 6 non-hydrogen atoms each. Methods, compositions, and medicaments related thereto are also disclosed.
    • 本文公开了包含式(I)或其药学上可接受的盐或其前药的化合物,其中虚线表示键的存在或不存在; Y是羧酸,磺酸或膦酸官能团; 或其包含0至12个碳原子的酰胺或酯; 或Y是含有0至12个碳原子的羟甲基或其醚; 或Y为四唑基官能团; A是 - (CH 2 CH 2)6 - ,顺式-CH 2 -CH = CH-(CH 2 CH 2) )3 - 或-CH 2 -C = -C(CH 2)3 - ,其中1或2个碳可被S 或O; B是氢,C 1-6烃基,CN,CO 2 H,或 - (CH 2 CH 2)m X (CH 2)n H,其中m为至少1,m和p之和为1至5; X为S或O; J是H,CH 3,或CF 3 D是共价键,CH 2。 O或S; 并且E是芳族杂双环系统,其可以具有各自含有多达6个非氢原子的取代基。 还公开了与其相关的方法,组合物和药物。