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：US07569602B2

公开(公告)日：2009-08-04

申请号：US10576095

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之一为：（ⅰ）H或任选取代的C 1-4烷基; 或（ii）任选取代的C 5-7芳基; R2和R5中的另一个为另一组; m和n可以是0或1，并且m + n = 1或2个RN是H或任选取代的C 1-4烷基R 3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; 或（iv）四唑-5-基。

公开(公告)号：US20090192138A1

公开(公告)日：2009-07-30

申请号：US12158872

申请日：2006-12-20

申请人： Daniel Kaspar Baeschlin ,  David Edward Clark ,  Stephen John Dunsdon ,  Garry Fenton ,  Amanda Fillmore ,  Neil Victor Harris ,  Christopher Higgs ,  Christopher Antony Hurley ,  Sussie Lerche Krintel ,  Robert Edward Mackenzie ,  Nils Ostermann ,  Finton Sirockin ,  Jonathan Mark Sutton

发明人： Daniel Kaspar Baeschlin ,  David Edward Clark ,  Stephen John Dunsdon ,  Garry Fenton ,  Amanda Fillmore ,  Neil Victor Harris ,  Christopher Higgs ,  Christopher Antony Hurley ,  Sussie Lerche Krintel ,  Robert Edward Mackenzie ,  Nils Ostermann ,  Finton Sirockin ,  Jonathan Mark Sutton

IPC分类号： A61K31/397 ,  C07D487/02 ,  A61K31/496 ,  A61K31/519 ,  C07D243/08 ,  A61K31/551 ,  C07D413/14 ,  A61K31/5377 ,  C07D403/14 ,  A61K31/501 ,  A61P3/00 ,  A61P9/00 ,  A61P25/00 ,  A61P1/00 ,  A61P35/00

CPC分类号： C07D487/04

摘要： The invention provides novel deazaxanthine and deazahypoxanthine compounds. The compounds may be useful in the therapy of diseases and conditions in which dipeptidylpeptidase-IV (DPP-IV) is implicated.

摘要翻译： 本发明提供新颖的脱甲黄嘌呤和脱邻二黄嘌呤化合物。 该化合物可用于治疗涉及二肽基肽酶-IV（DPP-IV）的疾病和病症。

公开(公告)号：US20080306117A1

公开(公告)日：2008-12-11

申请号：US12186308

申请日：2008-08-05

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： A61K31/443 ,  C07D307/34 ,  A61K31/341 ,  C07D261/06 ,  A61P29/00 ,  A61K31/422 ,  C07D405/02

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之一为：（ⅰ）H或任选取代的C 1-4烷基; 或（ii）任选取代的C 5-7芳基; R2和R5中的另一个为另一组; m和n可以是0或1，并且m + n = 1或2个RN是H或任选取代的C 1-4烷基R 3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; 或（iv）四唑-5-基。

公开(公告)号：US07211586B2

公开(公告)日：2007-05-01

申请号：US10715662

申请日：2003-11-18

申请人： Garry Fenton ,  Neil Victor Harris

发明人： Garry Fenton ,  Neil Victor Harris

IPC分类号： A61K31/4709 ,  A61K31/47 ,  C07D217/12

CPC分类号： C07D413/06 ,  C07D217/06 ,  C07D217/16 ,  C07D413/14

摘要： The invention is directed to physiologically active compounds of formula (I): wherein: R1 represents optionally substituted aryl, optionally substituted heteroaryl, R3NH—Ar1—L2— or R3—NH—C(═O)—NH—Ar2—L2—; R3 represents aryl or heteroaryl; Ar1 represents a saturated, partially saturated or fully unsaturated 8- to 10-membered bicyclic ring system containing at least one heteroatom selected from O, S or N; Ar2 represents aryldiyl or heteroaryldiyl; L1 represents a linkage, such as an alkylene linkage; L2 represents an alkylene chain linkage; R2 represents hydrogen, halogen, C1-4alkyl or C1-4alkoxy; and Y is carboxy or an acid bioisostere; but excluding compounds where an oxygen, nitrogen or sulfur atom is attached directly to a carbon carbon multiple bond of an alkenylene or alkynylene residue; and the corresponding N-oxides and ester prodrugs thereof, and the pharmaceutically acceptable salts and solvates of such compounds, and the N-oxides and ester prodrugs thereof. Such compounds have valuable pharmaceutical properties, in particular the ability to regulate the interaction of VCAM-1 and fibronectin with the integrin VLA-4 (α4β1).

摘要翻译： 本发明涉及式（I）的生理活性化合物：其中：R 1表示任选取代的芳基，任选取代的杂芳基，R 3 NH-Ar 1 - 或 - R 3 -NH-C（ - ） - -NH-Ar 2 -L 2 - ; R 3表示芳基或杂芳基; Ar 1表示含有至少一个选自O，S或N的杂原子的饱和的，部分饱和的或完全不饱和的8至10元双环体系; Ar 2代表芳基二基或杂芳基二基; L 1表示连接，例如亚烷基键; L 2代表亚烷基链键; R 2表示氢，卤素，C 1-4烷基或C 1-4烷氧基; Y为羧基或酸式生物电子等排体; 但不包括其中氧，氮或硫原子直接连接到亚烯基或亚炔基残基的碳碳多重键上的化合物; 和其相应的N-氧化物和酯前体药物，以及这些化合物的药学上可接受的盐和溶剂化物，及其N-氧化物和酯前体药物。 这些化合物具有有价值的药物性质，特别是调节VCAM-1和纤连蛋白与整联蛋白VLA-4（α4β1）的相互作用的能力。

公开(公告)号：US07166616B2

公开(公告)日：2007-01-23

申请号：US10427598

申请日：2003-05-01

申请人： Neil Victor Harris ,  Garry Fenton

发明人： Neil Victor Harris ,  Garry Fenton

IPC分类号： C07D263/58 ,  C07D261/02 ,  A61K31/423 ,  A61K31/445

CPC分类号： C07D263/58 ,  A61K31/423 ,  C07C275/42 ,  C07C2601/08 ,  C07C2602/08 ,  C07D413/12

摘要： The invention is directed to physiologically active compounds of general formula (I): wherein: represents (i) a saturated 3 to 6 membered carbocycle, optionally substituted by one or more alkyl groups, (ii) indanyl or (iii) a saturated 4 to 6 membered heterocyclic ring; R1 represents R3Z1-Het- or R4N(R5)—C(═O)—NH—Ar1—; L1 represents an —R6—R7— linkage; R2 represents hydrogen, halogen, lower alkyl or lower alkoxy; L2 represents an alkylene linkage; Y is carboxy or an acid bioisostere; and their corresponding N-oxides or prodrugs, and pharmaceutically acceptable salts and solvates of such compounds and their corresponding N-oxides or prodrugs. Such compounds have valuable pharmaceutical properties, in particular the ability to regulate the interaction of VCAM-1 and fibronectin with the integrin VLA-4 (α4β1).

摘要翻译： 本发明涉及通式（I）的生理活性化合物：其中：（i）饱和的3至6元碳环，任选被一个或多个烷基取代，（ii）茚满基或（iii）饱和的4至 6元杂环; R 1表示R 3 Z 1或H 4 - 或R 4 N（R 5） （O）-NH-Ar 1 - ; L 1表示-R 6-6R 7 - 键; R 2表示氢，卤素，低级烷基或低级烷氧基; L 2表示亚烷基键; Y是羧基或酸生物电子等排体; 及其相应的N-氧化物或前体药物，以及这些化合物的药学上可接受的盐和溶剂合物及其相应的N-氧化物或前体药物。 这些化合物具有有价值的药物性质，特别是调节VCAM-1和纤连蛋白与整联蛋白VLA-4（α4β1）的相互作用的能力。