公开(公告)号：US20080194574A1

公开(公告)日：2008-08-14

申请号：US10596508

申请日：2004-12-16

申请人： Jan Eike Eikhoff ,  Mark Richard Ashton ,  Stephen Martin Courtney ,  Christopher John Yarnold ,  Maurizio Varrone ,  Pui Leng Loke ,  Thomas Herget ,  Wilfried Schwab ,  Doris Hafenbradl

发明人： Jan Eike Eikhoff ,  Mark Richard Ashton ,  Stephen Martin Courtney ,  Christopher John Yarnold ,  Maurizio Varrone ,  Pui Leng Loke ,  Thomas Herget ,  Wilfried Schwab ,  Doris Hafenbradl

IPC分类号： A61K31/4985 ,  C07D487/04 ,  C07D241/10 ,  A61K31/4965 ,  A61P31/00 ,  A61P37/00 ,  A61P25/16 ,  A61P25/28

CPC分类号： C07D401/04 ,  C07D241/20 ,  C07D403/12 ,  C07D405/06 ,  C07D405/12 ,  C07D409/12 ,  C07D409/14

摘要： The present invention relates to pyrazine derivatives according to the general formula (I) and pharmaceutically acceptable salts thereof and their use as pharmaceutical compounds as well as the use of these compounds for the preparation of a pharmaceutical composition for the prophylaxis and/or treatment of infectious diseases, including opportunistic diseases, prion diseases, immunological diseases, autoimmune diseases, bipolar and clinical disorders, cardiovascular diseases, cell proliferative diseases, diabetes, inflammation, transplant rejections, erectile dysfunction, neurodegenerative diseases, stroke and especially for the treatment of herpesviral induced infections, including opportunistic infections as well as infections and diseases caused by human cytomegalovirus (HCMV).

摘要翻译： 本发明涉及根据通式（I）的吡嗪衍生物及其药学上可接受的盐及其作为药物化合物的用途，以及这些化合物在制备用于预防和/或治疗感染性疾病的药物组合物中的用途 疾病，包括机会性疾病，朊病毒疾病，免疫疾病，自身免疫性疾病，双相和临床病症，心血管疾病，细胞增殖性疾病，糖尿病，炎症，移植排斥，勃起功能障碍，神经变性疾病，中风，特别是治疗疱疹病毒诱导的感染 ，包括机会性感染以及由巨细胞病毒（HCMV）引起的感染和疾病。

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。

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。

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：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：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。

公开(公告)号：US20090023788A1

公开(公告)日：2009-01-22

申请号：US12232444

申请日：2008-09-17

申请人： David Middlemiss ,  Mark Richard Ashton ,  Edward Andrew Boyd ,  Frederick Arthur Brookfield ,  Eric Roy Pettipher ,  Michael George Hunter ,  Mark Whittaker ,  Chris Palmer

发明人： David Middlemiss ,  Mark Richard Ashton ,  Edward Andrew Boyd ,  Frederick Arthur Brookfield ,  Eric Roy Pettipher ,  Michael George Hunter ,  Mark Whittaker ,  Chris Palmer

IPC分类号： A61K31/428 ,  A61K31/404 ,  A61P11/00 ,  A61P37/08 ,  A61P19/02

CPC分类号： C07D209/12 ,  A61K31/404 ,  A61K31/426 ,  A61K31/428 ,  A61K31/4709 ,  A61K31/498 ,  C07D209/08 ,  C07D209/10 ,  C07D401/06 ,  C07D403/06 ,  C07D417/06

摘要： The present invention provides indole derivatives that antagonize prostaglandin D2, and that can be used to treat inflammatory diseases mediated by prostaglandin D2.

摘要翻译： 本发明提供了拮抗前列腺素D2的吲哚衍生物，其可用于治疗由前列腺素D2介导的炎性疾病。

公开(公告)号：US20090018138A1

公开(公告)日：2009-01-15

申请号：US12232446

申请日：2008-09-17

申请人： David Middlemiss ,  Mark Richard Ashton ,  Edward Andrew boyd ,  Frederick Arthur Brookfield ,  Michael George Hunter ,  Mark Whittaker ,  Chris Palmer ,  Eric R. Pettipher

发明人： David Middlemiss ,  Mark Richard Ashton ,  Edward Andrew boyd ,  Frederick Arthur Brookfield ,  Michael George Hunter ,  Mark Whittaker ,  Chris Palmer ,  Eric R. Pettipher

IPC分类号： A61K31/404 ,  A61P11/00 ,  A61P17/00 ,  A61K31/498 ,  A61K31/427 ,  A61K31/426 ,  A61K31/4709 ,  A61P29/00

CPC分类号： C07D209/12 ,  A61K31/404 ,  A61K31/426 ,  A61K31/428 ,  A61K31/4709 ,  A61K31/498 ,  C07D209/08 ,  C07D209/10 ,  C07D401/06 ,  C07D403/06 ,  C07D417/06

摘要： The present invention provides indole derivatives that antagonize prostaglandin D2, and that can be used to treat inflammatory diseases mediated by prostaglandin D2.

公开(公告)号：US09174987B2

公开(公告)日：2015-11-03

申请号：US13234793

申请日：2011-09-16

申请人： David John Hughes ,  Paul Anthony Worthington ,  Charles Adam Russell ,  Eric Daniel Clarke ,  James Edward Peace ,  Mark Richard Ashton ,  Thomas Stephen Coulter ,  Richard Spurring Roberts ,  Louis-Pierre Molleyres ,  Fredrik Cederbaum ,  Jerome Cassayre ,  Peter Maienfisch

发明人： David John Hughes ,  Paul Anthony Worthington ,  Charles Adam Russell ,  Eric Daniel Clarke ,  James Edward Peace ,  Mark Richard Ashton ,  Thomas Stephen Coulter ,  Richard Spurring Roberts ,  Louis-Pierre Molleyres ,  Fredrik Cederbaum ,  Jerome Cassayre ,  Peter Maienfisch

IPC分类号： A01N43/90 ,  A01N47/38 ,  C07D471/10 ,  A01P5/00 ,  A01P7/02 ,  A01P7/04 ,  A01P9/00 ,  A01N47/34 ,  C07D211/70 ,  C07D211/76 ,  C07D491/10

CPC分类号： A01N43/90 ,  A01N47/34 ,  A01N47/38 ,  C07B2200/11 ,  C07D211/70 ,  C07D211/76 ,  C07D471/10 ,  C07D491/10

摘要： Insecticidal, acaricidal, nematicidal or molluscicidal compounds of formula (I) wherein Y is a single bond, C═O, C═S or S(O)q where q is 0, 1 or 2; and R1, R2, R3, R4, R8, R9 are R10 are as defined in the claims or salts or N-oxides thereof, processes for preparing them and compositions containing them.

摘要翻译： 其中Y是单键，C = O，C = S或S（O）q，其中q是0,1或2的式（I）的杀虫，杀螨，杀线虫或杀软体动物化合物; 且R 1，R 2，R 3，R 4，R 8，R 9为R 10如权利要求中所定义或其盐或N-氧化物，制备方法和含有它们的组合物。

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.