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公开(公告)号：US20090018150A1
公开(公告)日：2009-01-15
申请号：US10564010
申请日：2004-07-23
申请人： Richard Anthony Borman , Robert Alexander Coleman , Kenneth Lyle Clark , Alexander William Oxford , George Hynd , Janet Ann Archer , Amanda Aley , Neil Victor Harris
发明人： Richard Anthony Borman , Robert Alexander Coleman , Kenneth Lyle Clark , Alexander William Oxford , George Hynd , Janet Ann Archer , Amanda Aley , Neil Victor Harris
IPC分类号： A61K31/505 , C07D239/42 , C07D233/88 , A61K31/4168 , A61K31/421 , C07D263/48 , C07D249/14 , A61K31/4196 , A61P1/00
CPC分类号： C04B35/632 , A61K31/4168 , A61K31/4178 , A61K31/421 , A61K31/4439 , A61K31/505 , A61K31/506 , C07D233/88 , C07D239/47 , C07D239/48 , C07D249/14 , C07D263/48 , C07D401/12 , C07D409/04 , C07D413/10 , C07D417/12
摘要： Compounds of formulae: (I), (II), (IIIa), (IIIb), (IVa) and (IVb): or a pharmaceutically acceptable salt thereof, for use as pharmaceuticals, in particular for the treatment of a condition alleviated by antagonism of a 5-HT2B receptor.
摘要翻译： 用于药物的式（I），（II），（IIIa），（IIIb），（IVa）和（IVb）化合物或其药学上可接受的盐，特别是用于治疗由 拮抗5-HT2B受体。
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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：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：US07326732B2
公开(公告)日：2008-02-05
申请号：US11055724
申请日：2005-02-11
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： C07C233/65 , C07D257/04 , A61K31/41 , A61K31/164
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： A compound of formula (I): or a salt, solvate and chemically protected form thereof, wherein: R5 is an optionally substituted C5-20 aryl or C4-20 alkyl group; A is selected from the group consisting of: 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; R3 is selected from H, F, Cl and optionally substituted C1-4 alkyl, C1-4 alkoxy, C5-7 aryl and C5-7 aryl-C1-4 alkyl groups; R4 is selected from H, F, Cl and optionally substituted C1-4 alkyl, C1-4 alkoxy, C5-7 aryl and C5-7 aryl-C1-4 alkyl groups; R6 is selected from H, F, Cl and optionally substituted C1-4 alkyl, C1-4 alkoxy, C5-7 aryl and C5-7 aryl-C1-4 alkyl groups; D is selected from: B is selected from the group consisting of: where RN′ is selected from H and C1-4 alkyl; where one of RP3 and RP4 is —Cm alkylene-R2 and the other of RP3 and RP4 is H, m and n can be 0 or 1, and m+n=1 or 2; and additionally when RP3 is —Cm alkylene-R2, m can also be 2 or 3, and m+n=1, 2, 3 or 4, and when R2 is tetrazol-5-yl, m+n may be 0; or where one of RP3 and RP4 is —O—CH2—R2, and the other of RP3 and RP4 is H, n is 0; RN is H or optionally substituted C1-4 alkyl; R2 is either: —CO2H (carboxy); —CONH2; —CH2—OH; or tetrazol-5-yl.
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公开(公告)号：US20100130556A1
公开(公告)日：2010-05-27
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： A61K31/443 , C07C249/00 , A61K31/195 , C07C229/40 , C07D307/02 , A61K31/341 , C07D405/12 , C07D263/56 , A61K31/423
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: formulae (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: formulae (i) (ii) (iii) (iv) (v) (vii) (viii) (ix) B is selected from the group consisting of: formulae (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：US07662839B2
公开(公告)日：2010-02-16
申请号：US11950613
申请日：2007-12-05
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： A61K31/44 , C07D401/02
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： A compound of formula (I): or a salt, or chemically protected form thereof, wherein: R5 is an optionally substituted phenyl; A is wherein Q is N; R3 is selected from H, F, Cl and optionally substituted C1-4 alkyl, C1-4 alkoxy, C5-7 aryl, and C5-7 aryl-C1-4 alkyl groups; R4 is selected from H, F, Cl and optionally substituted C1-4 alkyl, C1-4 alkoxy, C5-7 aryl, and C5-7 aryl-C1-4 alkyl groups; R6 is selected from H, F, Cl, and optionally substituted C1-4 alkyl, C1-4 alkoxy, C5-7 aryl, and C5-7 aryl-C1-4 alkyl groups; D is selected from: B is selected from the group consisting of: Where RN′ is selected from H and C1-4 alkyl; where one of RP3 and RP4 is —Cm-alkylene-R2 and the other of RP3 and RP4 is H, m and n can be 0 or 1, and m+n=1 or 2; and additionally, when RP3 is —Cm-alkylene-R2, m can also be 2 or 3, and m+n=1, 2, 3 or 4, and when R2 is tetrazol-5-yl, m+n may be 0; or where one of RP3 and RP4 is —O—CH2—R2, and the other of RP3 and RP4 is H, n is 0; RN is H or optionally substituted C1-4 alkyl; R2 is either: (i) —CO2H; (ii) —CONH2; (iii) —CH2—OH; or (iv) tetrazol-5-yl.
摘要翻译： 式（I）化合物或其盐或其化学保护形式，其中：R 5为任选取代的苯基; A是其中Q是N; R 3选自H，F，Cl和任选取代的C 1-4烷基，C 1-4烷氧基，C 5-7芳基和C 5-7芳基-C 1-4烷基; R4选自H，F，Cl和任选取代的C 1-4烷基，C 1-4烷氧基，C 5-7芳基和C 5-7芳基-C 1-4烷基; R 6选自H，F，Cl和任选取代的C 1-4烷基，C 1-4烷氧基，C 5-7芳基和C 5-7芳基-C 1-4烷基; D选自：B选自：其中RN'选自H和C 1-4烷基; 其中RP3和RP4中的一个是-C m - 亚烷基-R2，RP3和RP4中的另一个是H，m和n可以是0或1，m + n = 1或2; 另外当RP3为-C1亚烷基-R2时，m也可以是2或3，m + n = 1,2,3或4，当R 2为四唑-5-基时，m + n可以为0 ; 或RP3和RP4之一为-O-CH2-R2，RP3和RP4中的另一个为H，n为0; RN为H或任选取代的C 1-4烷基; 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：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：US20080119526A1
公开(公告)日：2008-05-22
申请号：US11950613
申请日：2007-12-05
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： A61K31/4418 , C07D307/66 , A61K31/341 , A61P27/06 , A61P19/08 , A61P37/00 , A61P43/00 , C07D213/78
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： A compound of formula (I): or a salt, solvate and chemically protected form thereof, wherein: R5 is an optionally substituted C5-20 aryl or C4-20 alkyl group; A is selected from the group consisting of: 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; R3 is selected from H, F, Cl and optionally substituted C1-4 alkyl, C1-4 alkoxy, C5-7 aryl and C5-7 aryl-C1-4 alkyl groups; R4 is selected from H, F, Cl and optionally substituted C1-4 alkyl, C1-4 alkoxy, C5-7 aryl and C5-7 aryl-C1-4 alkyl groups; R6 is selected from H, F, Cl and optionally substituted C1-4 alkyl, C1-4 alkoxy, C5-7 aryl and C5-7 aryl-C1-4 alkyl groups; D is selected from: B is selected from the group consisting of: where RN′ is selected from H and C1-4 alkyl; where one of RP3 and RP4 is —Cm alkylene-R2 and the other of RP3 and RP4 is H, m and n can be 0 or 1, and m+n=1 or 2; and additionally when RP3 is —Cm alkylene-R2, m can also be 2 or 3, and m+n=1, 2, 3 or 4, and when R2 is tetrazol-5-yl, m+n may be 0; or where one of RP3 and RP4 is —O—CH2—R2, and the other of RP3 and RP4 is H, n is 0; RN is H or optionally substituted C1-4 alkyl; R2 is either: —CO2H (carboxy); —CONH2; —CH2—OH; or tetrazol-5-yl.
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