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    Compounds useful in therapy
    2.
    发明申请
    Compounds useful in therapy 失效
    化合物可用于治疗

    公开(公告)号：US20070105909A1

    公开(公告)日：2007-05-10

    申请号：US11592574

    申请日：2006-11-03

    申请人： Paul Bradley ,  Kevin Dack ,  Patrick Johnson ,  Sarah Skerratt

    发明人： Paul Bradley ,  Kevin Dack ,  Patrick Johnson ,  Sarah Skerratt

    IPC分类号： A61K31/4439 ,  A61K31/4152 ,  C07D403/02 ,  C07D231/12

    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。

    Compounds useful in therapy
    3.
    发明申请
    Compounds useful in therapy 失效
    化合物可用于治疗

    公开(公告)号：US20060241125A1

    公开(公告)日：2006-10-26

    申请号：US11408286

    申请日：2006-04-18

    申请人： Paul Bradley ,  Kevin Dack ,  Ian Marsh

    发明人： Paul Bradley ,  Kevin Dack ,  Ian Marsh

    IPC分类号： A61K31/506 ,  A61K31/4152 ,  C07D403/02

    CPC分类号： C07D231/28 ,  C07D231/18 ,  C07D401/04 ,  C07D401/06 ,  C07D403/04 ,  C07D403/06 ,  C07D413/06 ,  C07D417/06

    摘要： Compounds of formula (I), or pharmaceutically acceptable derivatives thereof, wherein: R1 represents H, C1-6-alkyl, C1-6alkyloxy, C3-8cycloalkyl, or halo; R2 represents H, C1-6alkyl (optionally substituted by R3), phenyl (optionally substituted by CN), or Het; R3 represents OH, CN, Het, —R4—C1-6alkyl, or CONR5R6; R4 represents —CO2—, or —O—; R5 and R6 independently represent H, C1-6alkyl (optionally substituted by OR7) or C3-8cycloalkyl; R7 represents H or C1-6alkyl; 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 C1-6 alkyl; R8 represents C1-6alkyl, C1-6alkyloxy, C3-8cycloalkyl, or halo; R9 and R10 independently represent H, C1-6alkyl, C1-6alkyloxy, CN, CF3 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.

    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表示H，C 1-6烷基，C 1-6烷基， 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-CO 2 - 或-O-; R 5和R 6独立地表示H，C 1-6烷基（任选被OR 7取代）或 C 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。

    1H-Pyrazoles Useful In Therapy
    7.
    发明申请
    1H-Pyrazoles Useful In Therapy 失效
    1H-吡唑有用的治疗

    公开(公告)号：US20080085919A1

    公开(公告)日：2008-04-10

    申请号：US11870451

    申请日：2007-10-11

    申请人： Paul Bradley ,  Kevin Dack ,  Patrick Johnson ,  Sarah Skerratt

    发明人： Paul Bradley ,  Kevin Dack ,  Patrick Johnson ,  Sarah Skerratt

    IPC分类号： A61K31/415 ,  A61K31/4152 ,  A61K31/4709 ,  A61P43/00 ,  A61P7/00

    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。

    Novel pharmaceuticals
    9.
    发明申请
    Novel pharmaceuticals 失效
    新药

    公开(公告)号：US20050075392A1

    公开(公告)日：2005-04-07

    申请号：US10739425

    申请日：2003-12-18

    申请人： Kevin Dack ,  Robert Maguire

    发明人： Kevin Dack ,  Robert Maguire

    IPC分类号： C07D213/30 ,  C07D295/185 ,  A61K31/215

    CPC分类号： C07D213/30 ,  C07D295/185

    摘要： The invention relates to NEP inhibitors for treating cardiovascular disorders. Preferred NEP inhibitors are compounds of formula (I) wherein R1 is C1-C6alkyl, C1-C6alkoxyC1-C3alkyl or C1-C6alkoxyC1-C6alkoxyC1-C3alkyl; R2 is hydrogen or C1-C6alkyl; L is a three atom linkage selected from —CH2—X—CH2— and —CH2—CH2—X— where the right hand side of the linkage is attached to R3 and where X is oxygen, sulfur or methylene; R3 is phenyl or aromatic heterocyclyl, either of which may be independently substituted by one or more groups selected from: C1-C6alkyl, halo, haloC1-C6alkyl, C1-C6alkoxy, haloC1-C6alkoxy, C1-C6alkylthio, haloC1-C6alkylthio and nitrile; and R4 and R5 are either both hydrogen, or one of R4 and R5 is hydrogen and the other is a biolabile ester-forming group that in the body of a patient is replaced by hydrogen.

    摘要翻译： 本发明涉及用于治疗心血管疾病的NEP抑制剂。 优选的NEP抑制剂是式（I）的化合物，其中R 1是C 1 -C 6烷基，C 1 -C 6烷氧基C 1 -C 3烷基或C 1 -C 6烷氧基C 1 -C 6烷氧基C 1 -C 3烷基; R 2是氢或C 1 -C 6烷基; L是选自-CH 2 -X-CH 2 - 和-CH 2 -CH 2 -X-的三原子键，其中键的右手侧连接到R 3，其中X是氧，硫或亚甲基; R 3是苯基或芳族杂环基，其中任一个可以独立地被一个或多个选自以下的基团取代：C 1 -C 6烷基，卤素，卤代C 1 -C 6烷基，C 1 -C 6烷氧基，卤代C 1 -C 6烷氧基，C 1 -C 6烷硫基，卤代C 1 -C 6烷硫基 和腈; R 4和R 5都是氢，R 4和R 5中的一个是氢，另一个是生物不稳定酯形成基团，在患者体内被氢替代 。