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11. 发明授权

US06953798B1 β-alanine derivates 失效
标题翻译： β-丙氨酸衍生物
公开(公告)号：US06953798B1
公开(公告)日：2005-10-11
申请号：US09450999
申请日：1999-11-29
申请人： John Robert Porter , John Clifford Head , Graham John Warrellow , Sarah Catherine Archibald
发明人： John Robert Porter , John Clifford Head , Graham John Warrellow , Sarah Catherine Archibald
IPC分类号： A61K31/197 , A61K31/40 , A61K31/4406 , A61K31/455 , A61K31/497 , A61K31/506 , A61K31/53 , A61P1/00 , A61P3/10 , A61P7/04 , A61P11/06 , A61P17/06 , A61P29/00 , A61P37/02 , A61P37/06 , C07C233/80 , C07C233/83 , C07D207/16 , C07D207/48 , C07D213/56 , C07D213/81 , C07D213/82 , C07D401/12 , C07D405/12 , C07D413/12 , C07D417/12 , C07D417/14 , C07D403/12 , A61K31/444 , A61P19/10
CPC分类号： C07D213/81 , C07C233/80 , C07C2601/14 , C07D207/16 , C07D213/56 , C07D213/82 , C07D401/12 , C07D405/12 , C07D413/12 , C07D417/12 , C07D417/14
摘要： Alkanoic acid derivatives of formula (1) are described: Ar1(Alka)rL1Ar2CH(R1)C(Ra)(Ra′)R (1) Ar1 is an optionally substituted aromatic or heteroarotic group; L1 is a covalent bond or a linker atom or group; Ar2 is an optionally substituted phenylene or nitrogen-containing six-membered heteroarylene group; R is a carboxylic acid (—CO2H) or a derivative thereof; and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the binding of α4 integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders.
摘要翻译：描述式（1）的烷酸衍生物：<？in-line-formula description =“In-line formula”end =“lead”？> Ar <1> 其中，R 1，R 2，R 2，R 1，R 2，（R））（R i）（R 1）R（1）<βin-line-formula description =“In-line formula”end =“tail”？> Ar < 是任选取代的芳族或杂芳族基团; L 1是共价键或连接原子或基团; Ar 2是任选取代的亚苯基或含氮六元杂亚芳基; R是羧酸（-CO 2 H）或其衍生物; 及其盐，溶剂合物，水合物和N-氧化物。该化合物能够抑制α4整联蛋白与其配体的结合，并且可用于预防和治疗免疫或炎症性疾病。

12. 发明授权

US06555562B1 Phenylalanine derivatives 失效
标题翻译：苯丙氨酸衍生物
公开(公告)号：US06555562B1
公开(公告)日：2003-04-29
申请号：US09258522
申请日：1999-02-26
申请人： Sarah Catherine Archibald , John Clifford Head , Graham John Warrellow , John Robert Porter
发明人： Sarah Catherine Archibald , John Clifford Head , Graham John Warrellow , John Robert Porter
IPC分类号： A61K3144
CPC分类号： C07D213/81 , C07C233/87 , C07C235/60 , C07C237/30 , C07C323/62 , C07D213/61
摘要： Phenylalanine derivatives of formula (1) are described: wherein R is a carboxylic acid or a derivative thereof; L1 is a linker atom or group; Ar is an optionally substituted aromatic group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the binding of alpha4 integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders.
摘要翻译：描述了式（1）的苯丙氨酸衍生物：其中R是羧酸或其衍生物; L1是连接原子或基团; Ar是任选取代的芳族基团;及其盐，溶剂合物，水合物和N-氧化物。化合物能够抑制α4整联蛋白与其配体的结合，并且可用于预防和治疗免疫或炎性疾病。

13. 发明授权

US06329362B1 Cinnamic acid derivatives 失效
标题翻译：肉桂酸衍生物
公开(公告)号：US06329362B1
公开(公告)日：2001-12-11
申请号：US09270408
申请日：1999-03-16
申请人： Sarah Catherine Archibald , John Clifford Head , Graham John Warrellow , John Robert Porter
发明人： Sarah Catherine Archibald , John Clifford Head , Graham John Warrellow , John Robert Porter
IPC分类号： A61K3103
CPC分类号： C07D213/82 , A61K38/00 , C07C233/81 , C07K5/06139 , C07K5/06191 , Y10S514/826 , Y10S514/858 , Y10S514/863 , Y10S514/866 , Y10S514/885 , Y10S514/886 , Y10S514/887
摘要： Compounds of formula (1) are described: wherein L1 is a covalent bond or a linker atom or group; R is a carboxylic acid (—CO2H) or a derivative threof; R6 and R7 which may be the same or different is each an atom or group —L2(Alk2)tL3R12 in which L2, L3, Alk2 and t are as previously defined and R12 is a hydrogen or halogen atom or an —OR9, —NR9R10, —NO2, —CN, —CO2R9, —CONR9R10, —COR9, —N(R9)COR10, —N(R9)CSR10, —SO2N(R9)(R10), —N(R9)SO2R9, —N(R9)CON(R10)(R11), —N(R9)CSN(R10)(R11), —N(R9)SO2N(R10)(R11), or an optionally substituted aliphatic, heteroaliphatic, cycloaliphatic, heterocycloaliphatic, aromatic or heteroaromatic group provided that R6 and R7 are not both hydrogen atoms and when R7 is a hydrogen atom then R4 and R5 is each a hydrogen or halogen atom or an alkyl, alkoxy or nitro group; and the salts, solvates, hydrates and N-oxides thereof, for use in modulating cell adhesion. The compounds are able to inhibit the binding of alpha 4 integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders.
摘要翻译：描述了式（1）的化合物：其中L 1是共价键或连接原子或基团; R是羧酸（-CO 2 H）或衍生物; R 6和R 7可以相同或不同，各自为原子或基团-L2（Alk2）tL3R12，其中L2，L3，Alk2和t如前定义，R12是氢或卤素原子或-OR9，-NR9R10，-NO2，-CN，-CO2R9，-CONR9R10，-COR9 ，-N（R9）COR10，-N（R9）CSR10，-SO2N（R9）（R10），-N（R9）SO2R9，-N（R9）CON（R10）（R11）（R 10）（R 11），-N（R 9）SO 2 N（R 10）（R 11）或任选取代的脂族，杂脂族，脂环族，杂脂族，芳族或杂芳族基团，条件是R 6和R 7不是氢原子，氢原子然后R4和R5各自为氢或卤素原子或烷基，烷氧基或硝基; 和其盐，溶剂合物，水合物和N-氧化物，用于调节细胞粘附。化合物能够抑制α4整联蛋白与其配体的结合，并且可用于预防和治疗免疫或炎症性疾病。

14. 发明授权

US06369229B1 Pyridylalanine derivatives 失效
标题翻译：吡啶丙氨酸衍生物
公开(公告)号：US06369229B1
公开(公告)日：2002-04-09
申请号：US09538918
申请日：2000-03-30
申请人： John Clifford Head , Graham John Warrellow , John Robert Porter , Sarah Catherine Archibald
发明人： John Clifford Head , Graham John Warrellow , John Robert Porter , Sarah Catherine Archibald
IPC分类号： A61K31506
CPC分类号： C07D213/82 , C07D207/16 , C07D401/12
摘要： Aromatic amines of formula (1) are described: wherein Az is an optionally substituted monocyclic six-membered nitrogen-containing aromatic group; L1 is a linker atom or group; R is a carboxylic acid or a derivative thereof; and R5 is a group —L2(CH2)tR6 in which L2 is a —N(R7)CO— or —N(R7)CS-group. The compounds are able to inhibit the binding of &agr;4 integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders.
摘要翻译：描述了式（1）的芳族胺：其中Az是任选取代的单环六元含氮芳族基团; L1是连接原子或基团; R是羧酸或其衍生物; R5是基团 - L2（CH2）tR6，其中L2是-N（R7）CO-或-N（R7）CS-基。这些化合物能够抑制α4整联蛋白与其配体的结合，并且可用于预防和治疗免疫或炎性疾病。

15. 发明授权

US06274577B1 Benzodiazepines 失效
标题翻译：苯二氮卓类
公开(公告)号：US06274577B1
公开(公告)日：2001-08-14
申请号：US09408258
申请日：1999-09-29
申请人： Julien Alistair Brown , Graham John Warrellow , John Robert Porter , Sarah Catherine Archibald , John Clifford Head
发明人： Julien Alistair Brown , Graham John Warrellow , John Robert Porter , Sarah Catherine Archibald , John Clifford Head
IPC分类号： A61K31551
CPC分类号： C07D401/14
摘要： Benzodiazapine derivatives of formula (1) are described: wherein Ar1 is an aromatic or heteroaromatic group; L1 is a linker atom or group; Ar2 is an optionally substituted aromatic or heteroaromatic group; R5 is a carboxylic acid (—CO2H) or a derivative thereof; The compounds are able to inhibit the binding of alpha 4 integrins to their ligands and are of use in the prophylaxis and treatment of immune in inflammatory disorders.
摘要翻译：描述式（1）的苯并二氮杂衍生物：其中Ar1是芳族或杂芳族基团; L1是连接原子或基团; Ar2是任选取代的芳族或杂芳族基团; R 5是羧酸（-CO 2 H）或其衍生物; 这些化合物能够抑制α4整联蛋白与其配体的结合，并且可用于预防和治疗炎症性疾病中的免疫。

16. 发明授权

US6110945A Aromatic amine derivatives 失效
标题翻译：芳香族胺衍生物
公开(公告)号：US6110945A
公开(公告)日：2000-08-29
申请号：US323966
申请日：1999-06-02
申请人： John Clifford Head , Graham John Warrellow , John Robert Porter , Sarah Catherine Archibald
发明人： John Clifford Head , Graham John Warrellow , John Robert Porter , Sarah Catherine Archibald
IPC分类号： C07D213/65 , A61K31/4427 , A61K31/4439 , A61K31/444 , A61P29/00 , A61P43/00 , C07D207/16 , C07D213/75 , C07D213/82 , C07D401/12 , A61K31/44 , A61K31/54 , C07D213/36 , C07D401/02 , C07D417/02
CPC分类号： C07D213/82 , C07D207/16 , C07D401/12
摘要： Aromatic amines of formula (1) are described: ##STR1## wherein Az is an optionally substituted monocyclic six-membered nitrogen-containing aromatic group;L.sup.1 is a linker atom or group;R is a carboxylic acid or a derivative thereof;and R.sup.5 is a group --L.sup.2 (CH.sub.2).sub.t R.sup.6 in which L.sup.2 is a --N(R.sup.7)CO-- or --N(R.sup.7)CS-- group.The compounds are able to inhibit the binding of .alpha..sub.4 integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders.
摘要翻译：描述式（1）的芳族胺：其中Az是任选取代的单环六元含氮芳族基团; L1是连接原子或基团; R是羧酸或其衍生物; 并且R 5是其中L 2是-N（R 7）CO-或-N（R 7）CS-基团的基团-L 2（CH 2）t R 6。这些化合物能够抑制α4整联蛋白与其配体的结合，并且可用于预防和治疗免疫或炎症性疾病。

17. 发明授权

US06534513B1 Phenylalkanoic acid derivatives 失效
标题翻译：苯基链烷酸衍生物
公开(公告)号：US06534513B1
公开(公告)日：2003-03-18
申请号：US09408243
申请日：1999-09-29
申请人： John Robert Porter , Graham John Warrellow , Sarah Catherine Archibald , John Clifford Head
发明人： John Robert Porter , Graham John Warrellow , Sarah Catherine Archibald , John Clifford Head
IPC分类号： A61K41435
CPC分类号： C07D213/81 , C07C235/38 , C07C237/22
摘要： Phenylalkanoic acid derivatives of formula (1) are described: wherein Ar1 is an aromatic or heteroaromatic group; L1 is a covalent bond or a linker atom or group; A is an optionally substituted aliphatic, heteroaliphatic, cycloaliphatic, polycycloaliphatic, heterocycloaliphatic, polyheterocycloaliphatic, aromatic or heteroaromatic group; R is a carboxylic acid (—CO2H) or a derivative thereof; and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the binding of alpha 4 integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders.
摘要翻译：描述了式（1）的苯基链烷酸衍生物：其中Ar1是芳族或杂芳族基团; L1是共价键或连接原子或基团; A是任选取代的脂族，杂脂族，脂环族，多环脂族，杂脂族，多杂环脂族，芳族或杂芳基; R是羧酸（-CO 2 H）或其衍生物;及其盐，溶剂合物，水合物和N-氧化物。这些化合物能够抑制α4整联蛋白与其配体的结合，并且可用于预防和治疗免疫或炎症性疾病。

18. 发明授权

US06465471B1 Cinnamic acid derivatives 失效
标题翻译：肉桂酸衍生物
公开(公告)号：US06465471B1
公开(公告)日：2002-10-15
申请号：US09346235
申请日：1999-07-01
申请人： Graham John Warrellow , John Clifford Head , John Robert Porter , Sarah Catherine Archibald
发明人： Graham John Warrellow , John Clifford Head , John Robert Porter , Sarah Catherine Archibald
IPC分类号： A61K314406
CPC分类号： C07D213/81 , C07D213/82 , C07D401/12
摘要： Compounds of formula (1) are described: in which Het is a heteroaromatic group, Alk1 is an optionally substituted aliphatic or heteroaliphatic chain and R is a carboxylic acid or a derivative thereof. The compounds are able to inhibit the binding of &agr;4 integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders.
摘要翻译：描述了式（1）的化合物：其中Het是杂芳族基团，Alk1是任选取代的脂族或杂脂族链，R是羧酸或其衍生物。该化合物能够抑制α4整联蛋白与其配体的结合，并且可用于预防和治疗免疫或炎症性疾病。

19. 发明授权

US06329372B1 Phenylalanine derivatives 失效
标题翻译：苯丙氨酸衍生物
公开(公告)号：US06329372B1
公开(公告)日：2001-12-11
申请号：US09237060
申请日：1999-01-26
申请人： John Clifford Head , Sarah Catherine Archibald , Graham John Warrellow , John Robert Porter
发明人： John Clifford Head , Sarah Catherine Archibald , Graham John Warrellow , John Robert Porter
IPC分类号： A01N4364
CPC分类号： C07D207/416 , C07D209/42 , C07D213/81 , C07D213/82 , C07D215/50 , C07D231/14 , C07D241/24 , C07D277/56 , C07D401/12 , C07D409/12
摘要： Phenylalanine derivatives of formula (1) are described: wherein R is a carboxylic acid or a derivative thereof; L1 is a linker atom or group; Het is an optionally substituted heteroaromatic group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the binding of alpha4 integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders.
摘要翻译：描述了式（1）的苯丙氨酸衍生物：其中R是羧酸或其衍生物; L1是连接原子或基团; Het是任选取代的杂芳族基团;及其盐，溶剂合物，水合物和N-氧化物。化合物能够抑制α4整联蛋白与其配体的结合，并且可用于预防和治疗免疫或炎性疾病。

20. 发明授权

US06911451B1 Phenylalanine derivatives 失效
标题翻译：苯丙氨酸衍生物
公开(公告)号：US06911451B1
公开(公告)日：2005-06-28
申请号：US09326020
申请日：1999-06-04
申请人： John Robert Porter , John Clifford Head , Graham John Warrellow , Sarah Catherine Archibald
发明人： John Robert Porter , John Clifford Head , Graham John Warrellow , Sarah Catherine Archibald
IPC分类号： C07D213/81 , A61K31/198 , A61K31/4409 , A61K31/455 , A61P29/00 , A61P43/00 , C07C233/81 , C07C233/87 , C07C311/13 , C07C311/19 , C07D213/82 , A61K31/435 , A61K31/44 , A61K31/445 , C07D211/72 , C07D211/78
CPC分类号： C07D213/82 , C07C233/81 , C07C311/13 , C07C2601/08 , C07C2603/74
摘要： Phenylalanine derivatives of formula (1) are described: wherein L1 is a linker atom or group; X1 is a group selected from —N(R3)CO—, —N(R3)SO2—, —N(R3)C(O)O— or —N(R3)CON(R3a)—; and R is a carboxylic acid or a derivative thereof. The compounds are able to inhibit the binding of a 4 integrins to their ligands and are of use in the prophylaxis and treatment of diseases or disorders involving inflammation.
摘要翻译：描述了式（1）的苯丙氨酸衍生物：其中L 1是连接原子或基团; X 1是选自-N（R 3）CO - ， - N（R 3 SO）SO 2的基团， -N（R 3）C（O）O-或-N（R 3）CON（R 3a） - ; 并且R是羧酸或其衍生物。这些化合物能够抑制4种整联蛋白与其配体的结合，并且可用于预防和治疗涉及炎症的疾病或病症。

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