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1. 发明申请

US20100261760A1 EP2 Receptor Agonists 审中-公开
标题翻译： EP2受体激动剂
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。

2. 发明申请

US20090221604A1 Thiazole Compounds and Their Use as PGD2 Antagonists 审中-公开
标题翻译：噻唑化合物及其用作PGD2拮抗剂
公开(公告)号：US20090221604A1
公开(公告)日：2009-09-03
申请号：US12065756
申请日：2006-09-08
申请人： Neil Victor Harris , George Hynd , Sophie Gardan
发明人： Neil Victor Harris , George Hynd , Sophie Gardan
IPC分类号： A61K31/496 , C07D417/04 , A61P35/00 , A61P17/00 , A61P11/06
CPC分类号： C07D277/42 , C07D277/56 , C07D417/04
摘要： A compound for use as a PGD2 antagonist is of structural formula [1] in which: A represents a fully saturated or partially unsaturated monocyclic 5-7 membered ring containing one or two nitrogen atoms; B represents a direct bond, an optionally substituted methylene group, an optionally substituted nitrogen atom, oxygen, or S(O)n, where n=0, 1, or 2; L represents a direct bond, or an optionally substituted alkylene or alkenylene group; R1 represents an optionally substituted aryl or heteroaryl group, or an optionally substituted aryl-fused-heterocycloalkyl, heteroaryl-fused-cycloalkyl, heteroaryl-fused-heterocycloalkyl or aryl-fused-cycloalkyl group; R2 represents an optionally substituted aryl or heteroaryl group, or an optionally substituted aryl-fused-heterocycloalkyl, heteroaryl-fused-cycloalkyl, heteroaryl-fused-heterocycloalkyl or aryl-fused-cycloalkyl group; X represents a carboxylic acid, tetrazole, 3-hydroxyisoxazole, hydroxamic acid, phosphinate, phosphonate, phosphonamide, sulfonic acid or a group of formula C(═O)NHSO2Y or SO2NHC(═O)Y; and Y represents an optionally substituted aryl or heteroaryl group or an optionally substituted alkyl or cycloalkyl group; or a N-oxide, pharmaceutically acceptable salt, solvate or prodrug thereof.
摘要翻译：用作PGD 2拮抗剂的化合物是结构式[1]，其中：A表示含有一个或两个氮原子的完全饱和或部分不饱和的单环5-7元环; B表示直接键，任选取代的亚甲基，任选取代的氮原子，氧或S（O）n，其中n = 0,1或2; L表示直接键或任选取代的亚烷基或亚烯基; R 1表示任选取代的芳基或杂芳基，或任选取代的芳基稠合 - 杂环烷基，杂芳基 - 稠合 - 环烷基，杂芳基 - 稠合 - 杂环烷基或芳基 - 稠合环烷基; R 2表示任选取代的芳基或杂芳基，或任选取代的芳基稠合 - 杂环烷基，杂芳基 - 稠合 - 环烷基，杂芳基 - 稠合 - 杂环烷基或芳基 - 稠合环烷基; X表示羧酸，四唑，3-羟基异恶唑，异羟肟酸，次膦酸盐，膦酸盐，膦酰胺，磺酸或式C（-O）NHSO 2 Y或SO 2 NHC（-O）Y的基团; 并且Y表示任选取代的芳基或杂芳基或任选取代的烷基或环烷基; 或其N-氧化物，药学上可接受的盐，溶剂合物或前药。

3. 发明授权

US07569602B2 Furan derivatives as EP4 receptor antagonists 失效
标题翻译：呋喃衍生物作为EP4受体拮抗剂
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。

4. 发明申请

US20090192138A1 COMPOUNDS 审中-公开
标题翻译：化合物
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。

5. 发明申请

US20080306117A1 EP4 RECEPTOR ANTAGONISTS 审中-公开
标题翻译： EP4受体拮抗剂
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。

6. 发明授权

US07211586B2 Substituted tetrahydroisoquinolines 失效
标题翻译：取代的四氢异喹啉
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。

7. 发明授权

US07166616B2 Substituted alkanoic acids 失效
标题翻译：取代的链烷酸
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。

8. 发明授权

US06706738B2 Substituted bicyclic heteroaryl compounds and their use as integrin antagonists 有权
标题翻译：取代的双环杂芳基化合物及其作为整联蛋白拮抗剂的用途
公开(公告)号：US06706738B2
公开(公告)日：2004-03-16
申请号：US09975721
申请日：2001-10-11
申请人： David Edward Clark , Paul Robert Eastwood , Neil Victor Harris , Clive McCarthy , Andrew David Morley , Stephen Dennis Pickett
发明人： David Edward Clark , Paul Robert Eastwood , Neil Victor Harris , Clive McCarthy , Andrew David Morley , Stephen Dennis Pickett
IPC分类号： A61K31443
CPC分类号： C07D401/12 , C07D401/14 , C07D413/12 , C07D413/14
摘要： The invention is directed to physiologically active compounds of general formula (I): R1Z1—Het—L1—Ar1—L2—Y (I) wherein Het is an optionally substituted, saturated, partially saturated or fully unsaturated 8 to 10 membered bicyclic ring containing at least one heteroatom selected from O, S or N; R1 is optionally substituted aryl, heteroaryl, alkyl, alkenyl, alkynyl, cycloalkyl or heterocycloalkyl; Z1 represents a direct bond, an alkylene chain, NR4, O or S(O)n; L1 is an a —R5—R6— linkage where R5 is alkylene, alkenylene or alkynylene and R6 is a direct bond, cycloalkylene, heterocycloalkylene, arylene, heteroaryldiyl, —C(═Z3)—NR4—, —NR4—C(═Z3)—, —Z3—, —C(═O)—, —C(═NOR4)—, —NR4—, —NR4—C(═Z3)—NR4—, —SO2—NR4—, —NR4—SO2—, —O—C(═O)—, —C(═O)—O—, —NR4—C(═O)—O— or —O—C(═O)—NR4—; L2 is a direct bond; an optionally substituted alkylene, alkenylene, alkynylene, cycloalkenylene, cycloalkylene, heteroaryldiyl, heterocycloalkylene or arylene linkage; a —[C(═O)—N(R9)—C(R4)(R10)]p— linkage; a —Z4—R11— linkage; a —C(═O)—CH2—C(═O)— linkage; a —R11—Z4—R11— linkage; or a —L3—L4—L5— linkage; and Y is carboxy or an acid bioisostere; and the corresponding N-oxides, and their prodrugs; and pharmaceutically acceptable salts and solvates (e.g. hydrates) of such compounds and their N-oxides and 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 (&agr;4&bgr;1).
摘要翻译：本发明涉及通式（I）的生理活性化合物：其中Het是任选取代的，饱和的，部分饱和的或完全不饱和的8至10元双环，其含有至少一个选自O，S或N的杂原子; R 1是任选取代的芳基，杂芳基，烷基，烯基，炔基，环烷基或杂环烷基; Z 1表示直接键，亚烷基链，NR 4，O或S（O）n; L 1是-R 5 -R 6 - 键，其中R 5是亚烷基，亚烯基或亚炔基，R 6是直接键，亚环烷基，亚杂环亚烷基，亚芳基，杂芳基二基，-C （= Z 3）-NR 4 - ， - NR 4 -C（= Z 3） - ， - Z 3 - ， - C（= O） - ， - -NR 4 - ， - NR 4 -C（= Z 3）-NR 4 - ， - SO 2 -NR 4 - ， - NR 4 -SO 2 - ， - OC（= O） - ， - C（= O）-O-，-NR 4 -C（= O）-O-或-OC（= O）-NR 4 - L 2是直接键; 亚烯基，亚炔基，亚环烯基，亚环烷基，杂芳基二基，杂环亚烷基或亚芳基键; a - [C（= O）-N（R 9）-C（R 4）（R 10）] p - 键; a -Z 4 -R 11 - 键; -C（= O）-CH 2 -C（= O） - 键; -R 11 -Z 4 -R 11 - 键; 或-L 3 -L 4 -L 5 - 键; Y为羧基或酸式生物电子等排体; 和相应的N-氧化物及其前药; 和这些化合物的药学上可接受的盐和溶剂合物（例如水合物）及其N-氧化物和前药。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。

9. 发明授权

US06562851B2 Substituted bicyclic compounds 有权
标题翻译：取代的双环化合物
公开(公告)号：US06562851B2
公开(公告)日：2003-05-13
申请号：US10002041
申请日：2001-11-02
申请人： David Edward Clark , Paul Robert Eastwood , Neil Victor Harris , Clive McCarthy , Andrew David Morley , Stephen Dennis Pickett
发明人： David Edward Clark , Paul Robert Eastwood , Neil Victor Harris , Clive McCarthy , Andrew David Morley , Stephen Dennis Pickett
IPC分类号： A61K31423
CPC分类号： C07D263/58 , C07D235/30 , C07D413/12 , C07D413/14
摘要： The invention is directed to physiologically active compounds of general formula (I): wherein Het is an optionally substituted, saturated, partially saturated or fully unsaturated 8 to 10 membered bicyclic ring system containing at least one heteroatom selected from O, S or N; R1 is optionally substituted aryl, heteroaryl, alkyl, alkenyl, alkynyl, cycloalkyl or heterocycloalkyl; R2 is hydrogen, halogen, lower alkyl or lower alkoxy; Z1 is NR5; L1 is a —R6—R7— linkage (where R6 is alkylene, alkenylene or alkynylene and R7 is a direct bond, cycloalkylene, heterocycloalkylene, aryldiyl, heteroaryldiyl, —C(═Z3)—NR5—, —NR5—C(═Z3)—, —Z3—, —C(═O)—, —C(═NOR5)—, —NR5—, —NR5—C(═Z3)—NR5—, —SO2—NR5—, —NR5—SO2—, —O—C(═O)—, —C(═O)—O—, —NR5—C(═O)—O— or —O—C(═O)—NR5—); L2 is an alkylene chain substituted by hydroxy, oxo, —OR4, —O—C(═O)—R4, —N(R8)—C(═O)—R9, —N(R8)—C(═O)—OR9, —N(R8)—SO2—R9, or —NY3Y4; and Y is carboxy or an acid bioisostere; and the corresponding N-oxides, and their prodrugs; and pharmaceutically acceptable salts and solvates of such compounds and their N-oxides and 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 (&agr;4&bgr;1).
摘要翻译：本发明涉及通式（I）的生理活性化合物：其中Het是含有至少一个选自O，S或N的杂原子的任选取代的，饱和的，部分饱和的或完全不饱和的8至10元双环体系; R 1是任选取代的芳基，杂芳基，烷基，烯基，炔基，环烷基或杂环烷基; R2是氢，卤素，低级烷基或低级烷氧基; Z1是NR5; L1是-R6-R7-键（其中R6是亚烷基，亚烯基或亚炔基，R7是直接键，亚环烷基，亚杂烷基亚烷基，芳基二基，杂芳基二基，-C（= Z3）-NR5-，-NR5-C（= Z3 ） - ， - Z3 - ， - （= O） - ， - （= NOR5） - ， - NR5-，-NR5-C（= Z3）-NR5-，-SO2-NR5-，-NR5-SO2- ，-OC（= O） - ， - C（= O）-O-，-NR 5 -C（= O）-O-或-OC（= O）-NR 5 - ）; L2是被羟基，氧代，-OR4，-OC（= O）-R4，-N（R8）-C（= O）-R9，-N（R8）-C（= O）-OR9取代的亚烷基链，-N（R 8）-SO 2 -R 9或-NY 3 Y 4; Y为羧基或酸式生物电子等排体; 和相应的N-氧化物及其前药; 和这些化合物及其N-氧化物和前药的药学上可接受的盐和溶剂化物。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。

10. 发明授权

US06352977B1 Substituted &bgr;-alanines 有权
标题翻译：取代的β-丙氨酸
公开(公告)号：US06352977B1
公开(公告)日：2002-03-05
申请号：US09589825
申请日：2000-06-08
申请人： Peter Charles Astles , Neil Victor Harris , Andrew David Morley
发明人： Peter Charles Astles , Neil Victor Harris , Andrew David Morley
IPC分类号： C07C27542
CPC分类号： C07D207/27 , C07C275/42
摘要： The invention is directed to physiologically active compounds of general formula (I): wherein R1 is hydrogen, halogen, lower alkyl or lower alkoxy; X1, X2 and X6 independently represent N or CR2; and one of X3, X4 and X5 represents CR3 and the others independently represents N or CR2 where R2 is hydrogen, halogen, lower alkyl or lower alkoxy; and R3 represents a group —L1—(CH2)n—C(═O)—N(R4)—CH2—CH2—Y; and their prodrugs, and pharmaceutically acceptable salts and solvates of such compounds and their 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 (&agr;4&bgr;1).
摘要翻译：本发明涉及通式（I）的生理活性化合物：其中R 1是氢，卤素，低级烷基或低级烷氧基; X1，X2和X6独立地表示N或CR2; X 3，X 4和X 5中的一个表示CR 3，其余的独立地表示N或CR 2，其中R 2为氢，卤素，低级烷基或低级烷氧基; 并且R 3表示基团-L 1 - （CH 2）n -C（= O）-N（R 4）-CH 2 -CH 2 -Y; 及其前药，以及这些化合物及其前药的药学上可接受的盐和溶剂合物。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。

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