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。

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。

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.

公开(公告)号：US3941785A

公开(公告)日：1976-03-02

申请号：US427558

申请日：1973-12-26

申请人： Robert William Clarke ,  David Hartley ,  Alexander William Oxford

发明人： Robert William Clarke ,  David Hartley ,  Alexander William Oxford

IPC分类号： A61K31/53 ,  C07D253/075 ,  C07D487/04 ,  C07D253/08

CPC分类号： C07D253/075 ,  A61K31/53 ,  C07D487/04 ,  Y10S514/826 ,  Y10S514/869 ,  Y10S514/87

摘要： Compounds of the general formula: ##SPC1##In which:R.sub.1 and R.sub.2 which may be the same or different, represent a hydrogen atom or an alkyl group which may optionally be substituted by an aryl group, or represents an alkanoyl, aroyl or alkanesulphonyl group;R.sub.3 represents a hydrogen atom, or an alkyl group which may optionally be substituted by an aryl group, or represents an alkenyl, aryl or alkylthio group;R.sub.4 represents a hydrogen atom or an alkyl group; andR.sub.5 represents a hydrogen atom or an aryl or alkyl group, which alkyl group may optionally be substituted by a cycloalkyl group;And physiologically acceptable salts and derivatives thereof and addition products formed by nucleophilic addition.These compounds act as spasmolytics and phosphodiasterase inhibitors and have cardiotonic and diuretic properties. They are also of use in the treatment of skin disorders and gout.

摘要翻译： 通式的化合物：