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    • 9. 发明申请
    • PYRAZOLE DERIVATIVES AS PROGESTERONE RECEPTOR ANTAGONISTS
    • 作为孕激素受体拮抗剂的吡唑衍生物
    • WO2006111856A1
    • 2006-10-26
    • PCT/IB2006/001096
    • 2006-04-10
    • PFIZER LIMITEDBRADLEY, Paul, AnthonyDACK, Kevin, NeilMARSH, Ian, Roger
    • BRADLEY, Paul, AnthonyDACK, Kevin, NeilMARSH, Ian, Roger
    • C07D231/18C07D403/06C07D417/06A61K31/415A61P15/00
    • C07D231/28C07D231/18C07D401/04C07D401/06C07D403/04C07D403/06C07D413/06C07D417/06
    • Compounds of formula (I), or pharmaceutically acceptable derivatives thereof, wherein: R 1 represents H, C 1-6 alkyl, C 1-6 alkyloxy, C 3-8 cycloalkyl, or halo; R 2 represents H, C 1-6 alkyl (optionally substituted by R 3 ), phenyl (optionally substituted by CN), or Het; R 3 represents OH, CN, Het, -R 4 - C 1-6 alkyl, or CONR 5 R 6 ; R 4 represents ―CO 2 -, or ―O-; R 5 and R 6 independently represent H, C 1-6 alkyl (optionally substituted by OR 7 ) or C 3-8 cycloalkyl; R 7 represents H or C 1-6 alkyl; Het represents a five or six membered aromatic heterocyclic group containing (i) from one to four nitrogen heteroatom(s) or (ii) one or two nitrogen heteroatom(s) and one oxygen or one sulphur heteroatom or (iii) one or two oxygen or sulphur heteroatom (s), said heterocyclic group being optionally substituted by one or more groups selected from CN and C 1-6 alkyl; R 8 represents C 1-6 alkyl, C 1-6 alkyloxy, C 3-8 cycloalkyl, or halo; R 9 and R 10 independently represent H, C 1-6 alkyl, C 1-6 alkyloxy, CN, CF 3 or halo; may be useful for treating endometriosis, uterine fibroids (leiomyomata), menorrhagia, adenomyosis, primary and secondary dysmenorrhoea (including symptoms of dyspareunia, dyschexia and chronic pelvic pain), or chronic pelvic pain syndrome.
    • 式(I)化合物或其药学上可接受的衍生物,其中:R 1表示H,C 1-6烷基,C 1-6 烷氧基,C 3-8环烷基或卤素; R 2表示H,C 1-6烷基(任选被R 3 O 3取代),苯基(任选被CN取代)或Het; R 3表示OH,CN,Het,-R 4,C 1-6烷基或CONR 5 [R 6 ; R 4表示2 CO 2 - 或αO-; R 5和R 6独立地表示H,C 1-6烷基(任选被OR 7取代)或 ç 3-8 环烷基; R 7表示H或C 1-6烷基; Het表示含有(i)1-4个氮杂原子或(ii)一个或两个氮杂原子和一个氧或一个硫杂原子的五元或六元芳族杂环基,或(iii)一个或两个氧 或硫杂原子,所述杂环基团任选被一个或多个选自CN和C 1-6烷基的基团取代; R 8表示C 1-6烷基,C 1-6烷氧基,C 3-8环烷基,或 光环; R 9和R 10独立地代表H,C 1-6烷基,C 1-6烷氧基,CN CF 3或卤素; 可能有助于治疗子宫内膜异位症,子宫肌瘤(平滑肌瘤),月经过多,子宫腺肌症,原发性和继发性痛经(包括性交疼痛,dyschexia和慢性盆腔疼痛症状)或慢性盆腔疼痛综合征。