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公开(公告)号:US07528157B2
公开(公告)日:2009-05-05
申请号:US11615024
申请日:2006-12-22
申请人: Alexander W. Oxford , Richard J. Davis , Robert A. Coleman , Kenneth L. Clark , David E. Clark , Neil V. Harris , Garry Fenton , George Hynd , Keith A. J. Stuttle , Jonathan M. Sutton , Christopher G. Newton
发明人: Alexander W. Oxford , Richard J. Davis , Robert A. Coleman , Kenneth L. Clark , David E. Clark , Neil V. Harris , Garry Fenton , George Hynd , Keith A. J. Stuttle , Jonathan M. Sutton , Christopher G. Newton
IPC分类号: C07D307/68 , C07D405/10 , A61K31/34 , A61K31/443
CPC分类号: C07D307/54 , A61K31/34 , A61K31/341 , A61K31/4155 , A61K31/443 , C07D307/64 , C07D307/68 , C07D405/12 , C07D407/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D417/14
摘要: Compounds of formula (I): wherein: R2 is H or an optionally substituted C1-4 alkyl group; Y is either —(CH2)n—X—, where n is 1 or 2 and X is O, S, S(═O), S(═O)2, or NRN1, where RN1 is selected from H or optionally substituted C1-4 alkyl, or Y is —C(═O)NRN2—, where RN2 is selected from H, and optionally substituted C1-7 alkyl or C5-20 aryl; R3 is an optionally substituted C6 aryl group linked to a further optionally substituted C6 aryl group, wherein if both C6 aryl groups are benzene rings, there may be an oxygen bridge between the two rings, bound adjacent the link on both rings; A is a single bond or a C1-3 alkylene group; and R5 is either: (i) carboxy; (ii) a group of formula (II): (iii) a group of formula (III): wherein R is optionally substituted C1-7 alkyl, C5-20 aryl or NRN3RN4, where RN3 and RN4 are independently selected from optionally substituted C1-4 alkyl; (iv) tetrazol-5-yl.
摘要翻译: 式(I)化合物:其中:R2是H或任选取代的C 1-4烷基; Y是 - (CH 2)n X-,其中n是1或2,X是O,S,S(-O),S(-O)2或NRN1,其中RN1选自H或任选取代的C1- 4烷基或Y是-C(-O)NRN 2 - ,其中RN 2选自H,和任选取代的C 1-7烷基或C 5-20芳基; R3是与另外任意取代的C 6芳基连接的任意取代的C6芳基,其中如果两个C 6芳基都是苯环,则两个环之间可能有一个氧桥,与两个环上的连接相邻; A是单键或C1-3亚烷基; 并且R 5是:(i)羧基; (ii)式(II)的基团:(iii)式(III)的基团:其中R是任选取代的C 1-7烷基,C 5-20芳基或NRN 3 R N 4,其中RN 3和RN 4独立地选自任选取代的C 1 -4-烷基; (ⅳ)四唑-5-基。
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公开(公告)号:US07417068B2
公开(公告)日:2008-08-26
申请号:US10964831
申请日:2004-10-15
申请人: David Edward Clark , Neil Victor Harris , Garry Fenton , George Hynd , Keith Alfred James Stuttle , Jonathan Mark Sutton , Alexander William Oxford , Richard Jon Davis , Robert Alexander Coleman , Kenneth Lyle Clark
发明人: David Edward Clark , Neil Victor Harris , Garry Fenton , George Hynd , Keith Alfred James Stuttle , Jonathan Mark Sutton , Alexander William Oxford , Richard Jon Davis , Robert Alexander Coleman , Kenneth Lyle Clark
IPC分类号: A61K31/341 , C07D307/34
CPC分类号: C07D307/68
摘要: A compound of formula (I): or a salt, solvate and chemically protected form thereof, wherein one of R2 and R5 is: (i) H or an optionally substituted C1-4 alkyl group; or (ii)an optionally substituted C5-7 aryl; and the other of R2 and R5 is the other group; m and n can be 0 or 1, and m+n=1 or 2 RN is H or optionally substituted C1-4 alkyl R3 is either: (i) carboxy; (ii) a group of formula (II): (iii) a group of formula (III): wherein R is optionally substituted C1-7 alkyl, C5-20 aryl, or NRN3RN4, where RN3 and RN4 are independently selected from optionally substituted C1-4 alkyl; or (iv) tetrazol-5-yl.
摘要翻译: 式(I)化合物或其盐,溶剂合物和化学保护形式,其中R 2和R 5中的一个为:(i)H或任选地 取代的C 1-4烷基; 或(ii)任选取代的C 5-7芳基; R 2和R 5中的另一个是另一个基团; m和n可以是0或1,m + n = 1或2 R N是H或任选取代的C 1-4烷基R 3, SUP>是:(i)羧基; (ii)式(II)的基团:(iii)式(III)的基团:其中R是任选取代的C 1-7烷基,C 5〜20 其中R 3,N 3和R 4各自独立地选自任选取代的C 1 -C 6芳基或NR N 3 N, 1-4个C 1-4烷基; 或(iv)四唑-5-基。
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公开(公告)号:US20080039502A1
公开(公告)日:2008-02-14
申请号:US11889570
申请日:2007-08-14
申请人: Alexander Oxford , Richard Davis , Robert Coleman , Kenneth Clark , David Clark , Neil Harris , Garry Fenton , George Hynd , Keith Stuttle , Jonathan Sutton , Christopher Newton
发明人: Alexander Oxford , Richard Davis , Robert Coleman , Kenneth Clark , David Clark , Neil Harris , Garry Fenton , George Hynd , Keith Stuttle , Jonathan Sutton , Christopher Newton
IPC分类号: A61K31/34 , A61K31/341 , A61K31/4155 , A61K31/443 , A61P25/06 , C07D231/12 , C07D231/18 , C07D307/68 , C07D307/77 , C07D405/12 , C07D413/12
CPC分类号: C07D307/54 , A61K31/34 , A61K31/341 , A61K31/4155 , A61K31/443 , C07D307/64 , C07D307/68 , C07D405/12 , C07D407/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D417/14
摘要: Compounds of formula (I): wherein: R2 is H or an optionally substituted C1-4 alkyl group; Y is either —(CH2)n—X—, where n is 1 or 2 and X is O, S, S(═O), S(═O)2, or NRN1, where RN1 is selected from H or optionally substituted C1-4 alkyl, or Y is —C(═O)NRN2—, where RN2 is selected from H, and optionally substituted C1-7 alkyl or C5-20 aryl; R3 is an optionally substituted C6 aryl group linked to a further optionally substituted C6 aryl group, wherein if both C6 aryl groups are benzene rings, there may be an oxygen bridge between the two rings, bound adjacent the link on both rings; A is a single bond or a C1-3 alkylene group; and R5 is either: (i) carboxy; (ii) a group of formula (II): (iii) a group of formula (III): wherein R is optionally substituted C1-7 alkyl, C5-20 aryl or NRN3RN4, where RN3 and RN4 are independently selected from optionally substituted C1-4 alkyl; (iv) tetrazol-5-yl.
摘要翻译: 式(I)的化合物:其中:R 2是H或任选取代的C 1-4烷基; Y是 - (CH 2)n -X-,其中n是1或2,X是O,S,S(-O),S(-O )N 2,或NR 11,其中R 0,1选自H或任选取代的C 1-4烷基 ,或Y是-C(-O)NR N2 - ,其中R N2选自H和任选取代的C 1-7 - 烷基或C 5-20-20芳基; R 3是与另外任选取代的C 6 -C 6芳基连接的任选取代的C 6-14芳基,其中如果两个C 6 芳基是苯环,两个环之间可能有一个氧桥,与两个环上的连接相邻; A是单键或C 1-3-3亚烷基; 和R 5是:(i)羧基; (ii)式(II)的基团:(iii)式(III)的基团:其中R是任选取代的C 1-7烷基,C 5〜20 其中R“N 3”和“R”N 4“独立地选自任选取代的C 1 -C 6烷基, 烷基; (ⅳ)四唑-5-基。
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公开(公告)号:US07196089B2
公开(公告)日:2007-03-27
申请号:US10766030
申请日:2004-01-29
申请人: Alexander W. Oxford , Richard J. Davis , Robert A. Coleman , Kenneth L. Clark , David E. Clark , Neil V. Harris , Garry Fenton , George Hynd , Keith A. J. Stuttle , Jonathan M. Sutton , Christopher G. Newton
发明人: Alexander W. Oxford , Richard J. Davis , Robert A. Coleman , Kenneth L. Clark , David E. Clark , Neil V. Harris , Garry Fenton , George Hynd , Keith A. J. Stuttle , Jonathan M. Sutton , Christopher G. Newton
IPC分类号: A61K31/341 , A61K31/443 , A61K31/506 , C07D239/34 , C07D405/10 , C07D307/91 , C07D307/68
CPC分类号: C07D307/54 , A61K31/34 , A61K31/341 , A61K31/4155 , A61K31/443 , C07D307/64 , C07D307/68 , C07D405/12 , C07D407/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D417/14
摘要: Compounds of formula (I): wherein: R2 is H or an optionally substituted C1-4 alkyl group; Y is either —(CH2)n—X—, where n is 1 or 2 and X is O, S, S(═O), S(═O)2, or NRN1, where RN1 is selected from H or optionally substituted C1-4 alkyl, or Y is —C(═O)NRN2—, where RN2 is selected from H, and optionally substituted C1-7 alkyl or C5-20 aryl; R3 is an optionally substituted C6 aryl group linked to a further optionally substituted C6 aryl group, wherein if both C6 aryl groups are benzene rings, there may be an oxygen bridge between the two rings, bound adjacent the link on both rings; A is a single bond or a C1-3 alkylene group; and R5 is either: (i) carboxy; (ii) a group of formula (II): or (iii) a group of formula (III): wherein R is optionally substituted C1-7 alkyl, C5-20 aryl or NRN3RN4, where RN3 and RN4 are independently selected from optionally substituted C1-4 alkyl; (iv) tetrazol-5-yl.
摘要翻译: 式(I)的化合物:
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公开(公告)号:US08080567B2
公开(公告)日:2011-12-20
申请号:US12063421
申请日:2006-08-09
申请人: Alexander William Oxford , Richard Jon Davis , Robert Alexander Coleman , Kenneth Lyle Clark , David Edward Clark , Shirley Ann Brunton , Neil Victor Harris , Garry Fenton , George Hynd , Keith Alfred James Stuttle , Jonathan Mark Sutton , Mark Richard Ashton , Edward Andrew Boyd
发明人: Alexander William Oxford , Richard Jon Davis , Robert Alexander Coleman , Kenneth Lyle Clark , David Edward Clark , Shirley Ann Brunton , Neil Victor Harris , Garry Fenton , George Hynd , Keith Alfred James Stuttle , Jonathan Mark Sutton , Mark Richard Ashton , Edward Andrew Boyd
IPC分类号: A61K31/44 , A61K31/42 , A61K31/195
CPC分类号: C07C233/81 , C07C257/18 , C07D213/70 , C07D263/57 , C07D307/42 , C07D307/54 , C07D307/68 , C07D307/91 , C07D405/12
摘要: A compound of formula (III): or a salt, solvate and chemically protected form thereof, wherein: R5 is an optionally substituted C5-20 aryl or C4-20alkyl group; L′ is a single bond, —O— or —C(═O)—; A is selected from the group consisting of: formula (i) (ii) (iii) wherein X and Y are selected from the group consisting of: O and CR3; S and CR3; NH and CR3; NH and N; O and N; S and N; N and S; and N and O, and where the dotted lines indicate a double bond in the appropriate location, and where Q is either N or CH; D is selected from: formula (i) (ii) (iii) (iv) (v) (vii) (viii) (ix) B is selected from the group consisting of: formula (A) (B) where RP6 is selected from fluoro and chloro; and R2 is either: (i) —CO2H; (ii) —CONH2; (iii) —CH2—OH; or (iv) tetrazol-5-yl.
摘要翻译: 式(III)化合物或其盐,溶剂化物和化学保护形式,其中:R 5为任选取代的C 5-20芳基或C 4-20烷基; L'是单键,-O-或-C(= O) - ; A选自:式(i)(ii)(iii)其中X和Y选自:O和CR 3; S和CR3; NH和CR3; NH和N; O和N; S和N; N和S; 和N和O,并且其中虚线表示适当位置的双键,并且其中Q为N或CH; D选自:式(i)(ii)(iii)(iv)(v)(vii)(viii)(ix)B选自:其中选择RP6的式(A)(B) 来自氟和氯; 并且R2是:(i)-CO 2 H; (ii)-CONH 2; (ⅲ)-CH 2 -OH; 或(iv)四唑-5-基。
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公开(公告)号:US07803841B2
公开(公告)日:2010-09-28
申请号:US12346516
申请日:2008-12-30
申请人: Alexander William Oxford , Richard Jon Davis , Robert Alexander Coleman , Kenneth Lyle Clark , David Edward Clark , Neil Victor Harris , Garry Fenton , George Hynd , Keith Alfred James Stuttle , Jonathan Mark Sutton , Mark Richard Ashton , Edward Andrew Boyd , Shirley Ann Brunton
发明人: Alexander William Oxford , Richard Jon Davis , Robert Alexander Coleman , Kenneth Lyle Clark , David Edward Clark , Neil Victor Harris , Garry Fenton , George Hynd , Keith Alfred James Stuttle , Jonathan Mark Sutton , Mark Richard Ashton , Edward Andrew Boyd , Shirley Ann Brunton
IPC分类号: A61K31/166 , C07C233/65
CPC分类号: C07D213/81 , C07C233/75 , C07C233/81 , C07C235/84 , C07D233/90 , C07D257/04 , C07D277/24 , C07D277/26 , C07D277/56 , C07D307/46 , C07D307/68 , C07D307/91 , C07D333/38 , C07D401/12 , C07D405/04 , C07D405/12 , C07D409/12
摘要: The disclosure provides EP2 receptor agonist compounds and methods for using the compounds for treating conditions which can be alleviated by agonism of an EP2 receptor.
摘要翻译: 本公开提供EP2受体激动剂化合物和使用该化合物治疗可通过EP2受体激动作用缓解的病症的方法。
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公开(公告)号:US20090298899A1
公开(公告)日:2009-12-03
申请号:US12346516
申请日:2008-12-30
申请人: Alexander William Oxford , Richard Jon Davis , Robert Alexander Coleman , Kenneth Lyle Clark , David Edward Clark , Neil Victor Harris , Garry Fenton , George Hynd , Keith Alfred James Stuttle , Jonathan Mark Sutton , Mark Richard Ashton , Edward Andrew Boyd , Shirley Ann Brunton
发明人: Alexander William Oxford , Richard Jon Davis , Robert Alexander Coleman , Kenneth Lyle Clark , David Edward Clark , Neil Victor Harris , Garry Fenton , George Hynd , Keith Alfred James Stuttle , Jonathan Mark Sutton , Mark Richard Ashton , Edward Andrew Boyd , Shirley Ann Brunton
IPC分类号: A61K31/395 , C07D307/68 , C07D257/04 , A61P27/06 , A61K31/34
CPC分类号: C07D213/81 , C07C233/75 , C07C233/81 , C07C235/84 , C07D233/90 , C07D257/04 , C07D277/24 , C07D277/26 , C07D277/56 , C07D307/46 , C07D307/68 , C07D307/91 , C07D333/38 , C07D401/12 , C07D405/04 , C07D405/12 , C07D409/12
摘要: The disclosure provides EP2 receptor agonist compounds and methods for using the compounds for treating conditions which can be alleviated by agonism of an EP2 receptor.
摘要翻译: 本公开提供EP2受体激动剂化合物和使用该化合物治疗可通过EP2受体激动作用缓解的病症的方法。
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公开(公告)号:US07429607B2
公开(公告)日:2008-09-30
申请号:US10364672
申请日:2003-02-12
申请人: Alexander William Oxford , Richard Anthony Borman , Robert Alexander Coleman , Kenneth Lyle Clark , George Hynd , Janet Ann Archer , Amanda Aley , Neil Victor Harris
发明人: Alexander William Oxford , Richard Anthony Borman , Robert Alexander Coleman , Kenneth Lyle Clark , George Hynd , Janet Ann Archer , Amanda Aley , Neil Victor Harris
IPC分类号: A61K31/42 , A61K31/445 , A61K31/55 , C07D263/00 , C07D413/00 , C07D419/00 , C07D403/00
CPC分类号: C07D413/04 , C07D263/48
摘要: The present invention relates to compounds of formula I: wherein one of R1 and R4 is selected from the group consisting of H, and optionally substituted C1-6 alkyl, C3-7 cycloalkyl, C3-7 cycloalkyl-C1-4 alkyl, and phenyl-C1-4 alkyl; and the other of R1 and R4 is an optionally substituted C9-14 aryl group; R2 and R3 are either: (i) independently selected from H, R, R′, SO2R, C(═O)R, (CH2)nNR5R6, where n is from 1 to 4 and R5 and R6 are independently selected from H and R, where R is optionally substituted C1-4 alkyl, and R′ is optionally substituted phenyl-C1-4 alkyl, or (ii) together with the nitrogen atom to which they are attached, form an optionally substituted C5-7 heterocyclic group; and their use as pharmaceuticals, in particular for treating conditions alleviated by the antagonism of a 5-HT2B receptor.
摘要翻译: 本发明涉及式I化合物:其中R 1和R 4中的一个选自H和任选取代的C 1〜 C 6 -C 12烷基,C 3-7环烷基,C 3-7环烷基-C 1-4烷基和苯基-C 1-4个C 1-4烷基; R 1和R 4中的另一个是任选取代的C 9-14芳基; R 2和R 3是:(i)独立地选自H,R,R',SO 2 R,C(-O )R,(CH 2)2 NR 6,其中n为1至4,R H和R 6独立地选自H和R,其中R是任选取代的C 1-4烷基,R'任选被取代 苯基-C 1-4烷基,或(ii)与它们所连接的氮原子一起形成任选取代的C 5-7杂环基; 以及它们作为药物的用途,特别是用于治疗由5-HT 2B受体拮抗而缓解的病症。
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公开(公告)号:US20100331410A1
公开(公告)日:2010-12-30
申请号:US12865321
申请日:2009-02-05
申请人: Robert Coleman , David Middlemiss
发明人: Robert Coleman , David Middlemiss
IPC分类号: A61K31/24 , A61K31/167 , A61P27/02 , A61P27/06 , C07C229/00 , C07C235/24
CPC分类号: C07D207/16 , C07C233/75 , C07C233/87 , C07C235/20
摘要: A compound of formula: for treating ocular hypertension.
摘要翻译: 用于治疗高眼压症的化合物。
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公开(公告)号:US20100261760A1
公开(公告)日:2010-10-14
申请号:US12820752
申请日:2010-06-22
申请人: Alexander William Oxford , Richard John Davis , Robert Alexander Coleman , Kenneth Lyle Clark , David Edward Clark , Neil Victor Harris , Garry Fenton , George Hynd , Keith Alfred James Stuttle , Jonathan Mark Sutton , Mark Richard Ashton , Edward Andrew Boyd , Shirley Ann Brunton
发明人: Alexander William Oxford , Richard John Davis , Robert Alexander Coleman , Kenneth Lyle Clark , David Edward Clark , Neil Victor Harris , Garry Fenton , George Hynd , Keith Alfred James Stuttle , Jonathan Mark Sutton , Mark Richard Ashton , Edward Andrew Boyd , Shirley Ann Brunton
IPC分类号: A61K31/4439 , A61K31/4418 , A61K31/381 , A61K31/36 , A61K31/341 , C07D401/12 , C07D213/81 , C07D333/38 , C07D407/10 , C07D307/54 , A61P13/12 , A61P15/00 , A61P27/06 , A61P19/10 , A61P11/06 , A61P37/00
CPC分类号: C07D213/81 , C07C233/75 , C07C233/81 , C07C235/84 , C07D233/90 , C07D257/04 , C07D277/24 , C07D277/26 , C07D277/56 , C07D307/46 , C07D307/68 , C07D307/91 , C07D333/38 , C07D401/12 , C07D405/04 , C07D405/12 , C07D409/12
摘要: The disclosure provides EP2 receptor agonist compounds and methods for using the compounds for treating conditions which can be alleviated by agonism of an EP2 receptor.
摘要翻译: 本公开提供EP2受体激动剂化合物和使用该化合物治疗可通过EP2受体激动作用缓解的病症的方法。
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