Compounds Useful in Therapy
    8.
    发明申请
    Compounds Useful in Therapy 审中-公开
    化合物可用于治疗

    公开(公告)号:US20080234252A1

    公开(公告)日:2008-09-25

    申请号:US11914688

    申请日:2006-05-08

    摘要: Compounds of formula (I), or a pharmaceutically acceptable salt, solvate, ester or amide thereof, wherein R1 represents [CH2]n—R2. R2 represents H, C1-6 alkyloxy or Het; n represents a number selected from 0 to 6; Het represents an unsaturated heterocycle of 5 or 6 atoms containing one or more heteroatoms selected from O, N, and S; R3 represents halo; Ring A represents a 4 to 7 membered, saturated, partially saturated, or unsaturated heterocycle containing one or more heteroatoms selected from O, N, and S; Ring B represents a saturated, partially saturated, or unsaturated heterocycle of from 3 to 8 atoms containing one or more heteroatoms selected from O, N, and S, or Ring B represents a saturated or unsaturated carbocyclic ring of from 3 to 8 atoms; Ring B is optionally fused to an aryl ring and is optionally substituted with one or more groups independently selected from R4; Ring A and Ring B share at least one atom; R4 represents oxo, [CH2]m—R5 or CH—R6R7; R5 represents H, OH, C1-6 alkyloxy, COOH, or CONR8R9; m represents a number selected from 0 or 1; and R6, R7, R8 and R9 independently represent H or C1-6 alkyl; are useful for treating a disorder for which a V1a antagonist is indicated, in particular, dysmenorrhoea.

    摘要翻译: 式(I)化合物或其药学上可接受的盐,溶剂合物,酯或酰胺,其中R 1表示[CH 2 N] -R <2> 。 R 2表示H,C 1-6烷氧基或Het; n表示选自0〜6的数; Het表示含有一个或多个选自O,N和S的杂原子的5或6个原子的不饱和杂环; R 3表示卤素; 环A表示含有一个或多个选自O,N和S的杂原子的4至7元饱和的,部分饱和的或不饱和的杂环; 环B表示含有一个或多个选自O,N和S的杂原子的3至8个原子的饱和,部分饱和或不饱和杂环,或环B表示3至8个原子的饱和或不饱和碳环; 环B任选地与芳环稠合并且任选地被一个或多个独立地选自R 4的基团取代; 环A和环B共享至少一个原子; R 4表示氧代,[CH 2 CH 2] m -R 5或CH-R 6, 7&lt; 7&gt;; R 5表示H,OH,C 1-6烷氧基,COOH或CONR 8 R 9; m表示选自0或1的数字; 且R 6,R 7,R 8和R 9独立地表示H或C 1〜 6烷基; 可用于治疗指示V1a拮抗剂的疾病,特别是痛经。

    1H-pyrazoles useful in therapy
    9.
    发明授权
    1H-pyrazoles useful in therapy 失效
    用于治疗的1H-吡唑

    公开(公告)号:US07425569B2

    公开(公告)日:2008-09-16

    申请号:US11870451

    申请日:2007-10-11

    IPC分类号: A61K31/44

    CPC分类号: C07D231/18 C07D401/12

    摘要: Compounds of formula (I), or a pharmaceutically acceptable derivative thereof, wherein R1 and R3 independently represent H, C1-6alkyl, C3-8cycloalkyl, or halogen; R2 represents C1-6alkyl, CF3 or aryl; a represents 1 or 2; R4, R5, R7 and R8 independently represent H, C1-6alkyl, C1-6alkyloxy, CN or halogen, or R4 and R5, or R7 and R8, together with the ring to which they are attached form an aryl or heterocyclic fused ring system; X represents C or N; Y represents CH2 or O; R6 represents H, CN or halo provided that, when X represents N, R6 is absent. The compounds are 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.

    摘要翻译: 式(I)化合物或其药学上可接受的衍生物,其中R 1和R 3独立代表H,C 1-6烷基 C 3-8环烷基或卤素; R 2表示C 1-6烷基,CF 3或芳基; a代表1或2; R 4,R 5,R 7和R 8独立地表示H,C 1-6 C 1-6烷基,C 1-6烷氧基,CN或卤素,或R 4和R 5或R 7 和它们所连接的环连接形成芳基或杂环稠环体系; X表示C或N; Y表示CH 2或O; R 6表示H,CN或卤素,条件是当X表示N时,R 6不存在。 这些化合物可用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。

    1H-pyrazoles useful in therapy
    10.
    发明授权
    1H-pyrazoles useful in therapy 失效
    用于治疗的1H-吡唑

    公开(公告)号:US07309712B2

    公开(公告)日:2007-12-18

    申请号:US11592574

    申请日:2006-11-03

    CPC分类号: C07D231/18 C07D401/12

    摘要: Compounds of formula (I), or a pharmaceutically acceptable derivative thereof, wherein R1 and R3 independently represent H, C1-6alkyl, C3-8cycloalkyl, or halogen; R2 represents C1-6alkyl, CF3 or aryl; a represents 1 or 2; R4, R5, R7 and R8 independently represent H, C1-6alkyl, C1-6alkyloxy, CN or halogen, or R4 and R5, or R7 and R8, together with the ring to which they are attached form an aryl or heterocyclic fused ring system; X represents C or N; Y represents CH2 or O; R6 represents H, CN or halo provided that, when X represents N, R6 is absent. The compounds are 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.

    摘要翻译: 式(I)化合物或其药学上可接受的衍生物,其中R 1和R 3独立代表H,C 1-6烷基 C 3-8环烷基或卤素; R 2表示C 1-6烷基,CF 3或芳基; a代表1或2; R 4,R 5,R 7和R 8独立地表示H,C 1-6 C 1-6烷基,C 1-6烷氧基,CN或卤素,或R 4和R 5或R 7 和它们所连接的环连接形成芳基或杂环稠环体系; X表示C或N; Y表示CH 2或O; R 6表示H,CN或卤素,条件是当X表示N时,R 6不存在。 这些化合物可用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。