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1. 发明授权

US08093400B2 Compounds useful in therapy 失效
标题翻译：化合物可用于治疗
公开(公告)号：US08093400B2
公开(公告)日：2012-01-10
申请号：US12777522
申请日：2010-05-11
申请人： Justin Stephen Bryans , Patrick Stephen Johnson , Lee Richard Roberts , Thomas Ryckmans
发明人： Justin Stephen Bryans , Patrick Stephen Johnson , Lee Richard Roberts , Thomas Ryckmans
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。

2. 发明授权

US07425569B2 1H-pyrazoles useful in therapy 失效
标题翻译：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
申请人： Paul Anthony Bradley , Kevin Neil Dack , Patrick Stephen Johnson , Sarah Elizabeth Skerratt
发明人： Paul Anthony Bradley , Kevin Neil Dack , Patrick Stephen Johnson , Sarah Elizabeth Skerratt
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。

3. 发明授权

US07309712B2 1H-pyrazoles useful in therapy 失效
标题翻译：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
申请人： Paul Anthony Bradley , Kevin Neil Dack , Patrick Stephen Johnson , Sarah Elizabeth Skerratt
发明人： Paul Anthony Bradley , Kevin Neil Dack , Patrick Stephen Johnson , Sarah Elizabeth Skerratt
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。

4. 发明授权

US07442795B2 Triazole compounds useful in therapy 失效
标题翻译：用于治疗的三唑化合物
公开(公告)号：US07442795B2
公开(公告)日：2008-10-28
申请号：US11416498
申请日：2006-05-01
申请人： Justin Stephen Bryans , Patrick Stephen Johnson , Thomas Ryckmans , Alan Stobie
发明人： Justin Stephen Bryans , Patrick Stephen Johnson , Thomas Ryckmans , Alan Stobie
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。

5. 发明授权

US08916593B2 Alkoxy-substituted 2-aminopyridines as ALK inhibitors 有权
标题翻译：烷氧基取代的2-氨基吡啶作为ALK抑制剂
公开(公告)号：US08916593B2
公开(公告)日：2014-12-23
申请号：US13695770
申请日：2011-05-04
申请人： Mark Edward Bunnage , Andrew Simon Cook , Jingrong Jean Cui , Kevin Nell Dack , Judith Gail Deal , Danlin Gu , Mingying He , Patrick Stephen Johnson , Ted William Johnson , Phuong Thi Quy Le , Cynthia Louise Palmer , Hong Shen
发明人： Mark Edward Bunnage , Andrew Simon Cook , Jingrong Jean Cui , Kevin Nell Dack , Judith Gail Deal , Danlin Gu , Mingying He , Patrick Stephen Johnson , Ted William Johnson , Phuong Thi Quy Le , Cynthia Louise Palmer , Hong Shen
IPC分类号： A61K31/4427 , C07D213/73 , C07D498/04 , C07D413/14 , C07D403/14 , C07D409/14 , C07F9/53 , C07D471/04 , C07D403/04 , C07D417/04 , C07D403/12 , C07F9/6558 , C07F5/02 , C07D413/04 , C07D417/14 , C07D241/20 , C07D401/14 , C07D401/12 , C07D451/02 , C07D401/04 , C07F7/18
CPC分类号： C07D213/73 , C07D241/20 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/14 , C07D451/02 , C07D471/04 , C07D498/04 , C07F5/025 , C07F7/1804 , C07F9/5325 , C07F9/65583
摘要： The invention relates to compounds of Formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in numerous diseases in which ALK protein is involved or in which inhibition of ALK activity may induce benefit, especially for the treatment of cancer mediated by a mutated EML4-ALK fusion protein.
摘要翻译：本发明涉及式（1）的化合物以及制备用于制备含有这些衍生物的组合物和用途的中间体的方法。根据本发明的化合物可用于其中涉及ALK蛋白的许多疾病或其中ALK活性的抑制可诱导益处的疾病，特别是用于治疗由突变的EML4-ALK融合蛋白介导的癌症的治疗。

6. 发明申请

US20130196952A1 HETEROCYCLIC DERIVATIVES FOR THE TREATMENT OF DISEASES 有权
标题翻译：用于治疗疾病的杂环衍生物
公开(公告)号：US20130196952A1
公开(公告)日：2013-08-01
申请号：US13695770
申请日：2011-05-04
申请人： Mark Edward Bunnage , Andrew Simon Cook , Jingrong Jean Cui , Kevin Nell Dack , Judith Gail Deal , Danlin Gu , Mingying He , Patrick Stephen Johnson , Ted William Johnson , Phuong Thi Quy Le , Cynthia Louise Palmer , Hong Shen
发明人： Mark Edward Bunnage , Andrew Simon Cook , Jingrong Jean Cui , Kevin Nell Dack , Judith Gail Deal , Danlin Gu , Mingying He , Patrick Stephen Johnson , Ted William Johnson , Phuong Thi Quy Le , Cynthia Louise Palmer , Hong Shen
IPC分类号： C07D213/73 , C07D417/04 , C07D401/14 , C07D417/14 , C07D413/04 , C07D403/14 , C07D403/04 , C07D413/14 , C07D241/20 , C07D403/12 , C07D471/04 , C07D498/04 , C07D401/12 , C07D409/14 , C07F9/6558 , C07D451/02 , C07D401/04
CPC分类号： C07D213/73 , C07D241/20 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/14 , C07D451/02 , C07D471/04 , C07D498/04 , C07F5/025 , C07F7/1804 , C07F9/5325 , C07F9/65583
摘要： The invention relates to compounds of Formula (1) and to processes for the preparation of intermediates used in the preparation of compositions containing and the uses of such derivatives. The compounds according to the present invention are useful in numerous diseases in which ALK protein is involved or in which inhibition of ALK activity may induce benefit, especially for the treatment of cancer mediated by a mutated EML4-ALK fusion protein.
摘要翻译：本发明涉及式（1）的化合物以及制备用于制备含有此类衍生物的组合物的中间体的方法。根据本发明的化合物可用于其中涉及ALK蛋白的许多疾病或其中ALK活性的抑制可诱导益处的疾病，特别是用于治疗由突变的EML4-ALK融合蛋白介导的癌症的治疗。

7. 发明申请

US20100317652A1 Compounds Useful In Therapy 失效
标题翻译：化合物可用于治疗
公开(公告)号：US20100317652A1
公开(公告)日：2010-12-16
申请号：US12777522
申请日：2010-05-11
申请人： Justin Stephen Bryans , Patrick Stephen Johnson , Lee Richard Roberts , Thomas Ryckmans
发明人： Justin Stephen Bryans , Patrick Stephen Johnson , Lee Richard Roberts , Thomas Ryckmans
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。

8. 发明申请

US20080234252A1 Compounds Useful in Therapy 审中-公开
标题翻译：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
申请人： Justin Stephen Bryans , Patrick Stephen Johnson , Lee Richard Roberts , Thomas Ryckmans
发明人： Justin Stephen Bryans , Patrick Stephen Johnson , Lee Richard Roberts , Thomas Ryckmans
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> 。 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。

9. 发明授权

US07119088B2 Triazole compounds useful in therapy 失效
标题翻译：三唑化合物可用于治疗
公开(公告)号：US07119088B2
公开(公告)日：2006-10-10
申请号：US10782285
申请日：2004-02-18
申请人： Justin Stephen Bryans , Patrick Stephen Johnson , Thomas Ryckmans , Alan Stobie
发明人： Justin Stephen Bryans , Patrick Stephen Johnson , Thomas Ryckmans , Alan Stobie
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。

10. 发明申请

US20080188478A1 Compounds Useful In Therapy 审中-公开
标题翻译：化合物可用于治疗
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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