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公开(公告)号:US20080188478A1
公开(公告)日:2008-08-07
申请号:US11912592
申请日:2006-04-18
申请人: Justin Stephen Bryans , Mark Edward Bunnage , Patrick Stephen Johnson , Helen Janet Mason , Lee Richard Roberts , Thomas Ryckmans , Alan Stobie , Toby James Underwood
发明人: Justin Stephen Bryans , Mark Edward Bunnage , Patrick Stephen Johnson , Helen Janet Mason , Lee Richard Roberts , Thomas Ryckmans , Alan Stobie , Toby James Underwood
IPC分类号: A61K31/454 , C07D401/04 , C07D471/04 , A61K31/5025 , A61P25/00 , A61K31/437 , C07D487/04
CPC分类号: C07D471/04 , C07D401/14 , C07D413/14 , C07D417/14 , C07D487/04 , C07D513/04
摘要: Compounds of formula (I), or pharmaceutically acceptable derivatives thereof, wherein: R1 represents a group selected from H, CF3, and C1-6 alkyl (optionally substituted by C1-6 alkyloxy or triazolyl); R2 represents halo; Ring A represents a 5- or 6-membered heterocyclic ring containing at least one N atom (the ring being optionally bridged with two or more carbon atoms); R3 represents a 5- or 6-membered heterocyclic ring containing at least one atom selected from N, O or S, the heterocyclic ring being optionally substituted by one or more groups selected from C1-6 alkyl oxo or NH2, the heterocyclic ring being further optionally fused to a 5- or 6-membered aryl or heterocyclic ring containing at least one atom selected from N, O or S, the fused aryl or heterocyclic ring being substituted by one or more halo atoms; are useful for treating a disorder for which a V1a antagonist is indicated, in particular, dysmenorrhea.
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表示选自H,CF 3 N和C 1-6的基团, (任选被C 1-6烷氧基或三唑基取代); R 2表示卤素; 环A表示含有至少一个N原子(该环任选地与两个或多个碳原子桥连)的5-或6-元杂环; R 3表示含有至少一个选自N,O或S的原子的5元或6元杂环,杂环任选被一个或多个选自C 1〜 -6个烷基氧基或NH 2,杂环进一步任选地与含有至少一个选自N,O或S的原子的5-或6-元芳基或杂环稠合 稠合的芳基或杂环被一个或多个卤素原子取代; 可用于治疗指示V1a拮抗剂的疾病,特别是痛经。
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公开(公告)号:US07442795B2
公开(公告)日:2008-10-28
申请号:US11416498
申请日:2006-05-01
IPC分类号: C07D401/14 , C07D413/14
CPC分类号: C07D401/04 , C07D413/14 , C07D487/04 , C07D513/04
摘要: A compound of formula (I), or a pharmaceutically acceptable derivative, wherein A, B, V, W, X, Y, and Z are as defined herein; pharmaceutical compositions thereof; and uses thereof.
摘要翻译: 式(I)化合物或其药学上可接受的衍生物,其中A,B,V,W,X,Y和Z如本文所定义; 其药物组合物; 及其用途。
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公开(公告)号:US07119088B2
公开(公告)日:2006-10-10
申请号:US10782285
申请日:2004-02-18
IPC分类号: A61K31/5517 , C07D487/14 , C07D498/14 , C07D513/14
CPC分类号: C07D401/04 , C07D413/14 , C07D487/04 , C07D513/04
摘要: A compound of formula (I), or a pharmaceutically acceptable derivative thereof, wherein A, B, V, W, X, Y, and Z are as defined herein; pharmaceutical compositions thereof; and uses thereof.
摘要翻译: 式(I)化合物或其药学上可接受的衍生物,其中A,B,V,W,X,Y和Z如本文所定义; 其药物组合物; 及其用途。
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公开(公告)号:US07745630B2
公开(公告)日:2010-06-29
申请号:US11009768
申请日:2004-12-10
IPC分类号: A61K31/454 , C07D401/04 , C07D401/14
CPC分类号: C07D401/04 , C07D249/08 , C07D249/14 , C07D401/14 , C07D403/04 , C07D405/14 , C07D413/04 , C07D413/14 , C07D471/04
摘要: Compounds of formula (I), or pharmaceutically acceptable derivatives thereof, wherein: Z, O, A, V, Y and Y′ are as defined herein; are useful for treating dysmenorreah.
摘要翻译: 式(I)化合物或其药学上可接受的衍生物,其中:Z,O,A,V,Y和Y'如本文所定义; 对治疗dysmenorreah有用。
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公开(公告)号:US07084145B2
公开(公告)日:2006-08-01
申请号:US10693327
申请日:2003-10-24
申请人: Robert Duncan Armour , Andrew Douglas Baxter , Justin Stephen Bryans , Kevin Neil Dack , Patrick Stephen Johnson , Russell Andrew Lewthwaite , Julie Newman , David James Rawson , Thomas Ryckmans
发明人: Robert Duncan Armour , Andrew Douglas Baxter , Justin Stephen Bryans , Kevin Neil Dack , Patrick Stephen Johnson , Russell Andrew Lewthwaite , Julie Newman , David James Rawson , Thomas Ryckmans
IPC分类号: A61K31/4965 , C07D403/00
CPC分类号: C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D413/04 , C07D413/06 , C07D413/14
摘要: The invention provides compounds of formula (I), the pharmaceutically acceptable salts and solvates thereof, wherein A, B, R1, R2, and R7 are as defined herein; pharmaceutical compositions thereof; combinations thereof; and uses thereof as vasopressin V1A antagonists.
摘要翻译: 本发明提供式(I)化合物,其药学上可接受的盐和溶剂化物,其中A,B,R 1,R 2和R 7, / SUP>如本文所定义; 其药物组合物; 其组合; 并且其用作血管加压素V 1A拮抗剂。
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公开(公告)号:US08093400B2
公开(公告)日:2012-01-10
申请号:US12777522
申请日:2010-05-11
IPC分类号: C07D249/12 , C07D249/08 , C07D249/04 , A61K31/4196 , A61K31/4192
CPC分类号: C07D401/04 , C07D249/08 , C07D249/14 , C07D401/14 , C07D403/04 , C07D405/14 , C07D413/04 , C07D413/14 , C07D471/04
摘要: The present invention provides compounds of formula (I), or pharmaceutically acceptable derivatives thereof wherein the variables Z, Q, Ring A, V, X, Y and Y′ are as defined herein, and pharmaceutical compositions comprising these compounds. The compounds of formula (I) and pharmaceutical compositions comprising them are useful for treating a disorder for which a V1a antagonist is indicated, in particular, dysmenorrhoea.
摘要翻译: 本发明提供式(I)化合物或其药学上可接受的衍生物,其中变量Z,Q,环A,V,X,Y和Y'如本文所定义,以及包含这些化合物的药物组合物。 式(I)化合物和包含它们的药物组合物可用于治疗指示V1a拮抗剂,特别是痛经的病症。
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公开(公告)号:US20100317652A1
公开(公告)日:2010-12-16
申请号:US12777522
申请日:2010-05-11
IPC分类号: A61K31/454 , C07D413/14 , C07D401/14 , C07D403/04 , C07D413/04 , A61K31/5377 , A61K31/506 , A61K31/4545 , A61K31/551 , A61K31/496 , A61P9/10 , A61P9/00 , A61P9/12 , A61P9/04 , A61P29/00 , A61P15/00 , A61P15/06
CPC分类号: C07D401/04 , C07D249/08 , C07D249/14 , C07D401/14 , C07D403/04 , C07D405/14 , C07D413/04 , C07D413/14 , C07D471/04
摘要: The present invention provides compounds of formula (I), or pharmaceutically acceptable derivatives thereof wherein the variables Z, Q, Ring A, V, X, Y and Y′ are as defined herein, and pharmaceutical compositions comprising these compounds. The compounds of formula (I) and pharmaceutical compositions comprising them are useful for treating a disorder for which a V1a antagonist is indicated, in particular, dysmenorrhoea.
摘要翻译: 本发明提供式(I)化合物或其药学上可接受的衍生物,其中变量Z,Q,环A,V,X,Y和Y'如本文所定义,以及包含这些化合物的药物组合物。 式(I)化合物和包含它们的药物组合物可用于治疗指示V1a拮抗剂,特别是痛经的病症。
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公开(公告)号:US20080234252A1
公开(公告)日:2008-09-25
申请号:US11914688
申请日:2006-05-08
IPC分类号: A61K31/55 , C07D249/08 , A61K31/4196 , C07D471/02 , C07D487/02 , A61P15/00 , A61K31/519 , A61K31/437 , C07D221/20 , C07D223/16
CPC分类号: C07D471/04 , C07D401/04 , C07D403/04 , C07D403/14 , C07D471/10 , C07D487/04 , C07D491/10 , C07D498/04
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> SUP>。 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。
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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。
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公开(公告)号:US07309712B2
公开(公告)日:2007-12-18
申请号:US11592574
申请日:2006-11-03
IPC分类号: A61K31/44 , C07D401/00 , C07D231/10
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。
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