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11. 发明授权

US06518283B1 Squaric acid derivatives 失效
标题翻译：方酸衍生物
公开(公告)号：US06518283B1
公开(公告)日：2003-02-11
申请号：US09579317
申请日：2000-05-25
申请人： Barry John Langham , Rikki Peter Alexander , John Clifford Head , Janeen Marsha Linsley , John Robert Porter , Sarah Catherine Archibald , Graham John Warrellow
发明人： Barry John Langham , Rikki Peter Alexander , John Clifford Head , Janeen Marsha Linsley , John Robert Porter , Sarah Catherine Archibald , Graham John Warrellow
IPC分类号： A61K31445
CPC分类号： C07D213/79 , C07B2200/07 , C07C229/34 , C07C229/36 , C07C233/55 , C07C233/81 , C07C235/16 , C07C235/56 , C07C235/64 , C07C235/84 , C07C237/40 , C07C255/57 , C07C271/22 , C07C271/28 , C07C271/58 , C07C2601/04 , C07C2603/18 , C07D213/81 , C07D215/42 , C07D217/22 , C07D239/34 , C07D239/42 , C07D241/42 , C07D241/44 , C07D295/135 , C07D333/70 , C07D471/04 , C40B40/00
摘要： Squaric acid Derivatives of formula (1) are described: wherein R1 is an integrin binding group; R2 is a hydrogen atom or a C1-6alkyl group; L1 is a covalent bond or a linker atom or group; n is zero or the integer 1; Alk1 is an optionally substituted aliphatic chain; R3 is a hydrogen atom or an optionally substituted heteroaliphatic, cycloaliphatic, heterocycloaliphatic, polycycloaliphatic, polyheterocycloaliphatic, aromatic or heteroaromatic group: and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the binding of integrins to their ligands and are of use in the prophylaxis and treatment of immune of inflammatory disorders, or disorders involving the inappropriate growth or migration of cells.
摘要翻译：式（1）的方酸描述：其中R1是整联蛋白结合基团; R2是氢原子或C1-6烷基; L1是共价键或连接原子或基团; n是0或整数1; Alk1是任选取代的脂族链; R3是氢原子或任选取代的杂脂族，脂环族，杂脂族，多环脂族，多杂环脂族，芳族或杂芳族基团：及其盐，溶剂合物，水合物和N-氧化物。抑制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或涉及细胞不适当生长或迁移的疾病的免疫。

12. 发明授权

US06677339B2 Phenylalanine derivatives 失效
标题翻译：苯丙氨酸衍生物
公开(公告)号：US06677339B2
公开(公告)日：2004-01-13
申请号：US09927874
申请日：2001-08-10
申请人： John Clifford Head , John Robert Porter , Graham John Warrellow , Sarah Catherine Archibald , Brian Woodside Hutchinson
发明人： John Clifford Head , John Robert Porter , Graham John Warrellow , Sarah Catherine Archibald , Brian Woodside Hutchinson
IPC分类号： C07D21302
CPC分类号： C07D213/81 , C07D213/89 , C07D251/30 , C07D251/46 , C07D401/12 , C07D409/12 , C07D413/12
摘要： Phenylalanine derivatives of formula (1) are described: in which: Ar1 is an aromatic or heteroaromatic group; L1 is a linker atom or group; R is a carboxylic acid or a derivative thereof; Ar2 is an optionally substituted aromatic or heteroaromatic group; and the salts, solvates, hydrates and N-oxides 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）的苯丙氨酸衍生物：其中：Ar 1是芳族或杂芳族基团; L 1是连接原子或基团; R是羧酸或其衍生物; Ar 2是任选取代的芳族或杂芳族基团;以及其盐，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

US06362204B1 Phenylalanine derivatives 失效
标题翻译：苯丙氨酸衍生物
公开(公告)号：US06362204B1
公开(公告)日：2002-03-26
申请号：US09317081
申请日：1999-05-20
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： A61K314439
CPC分类号： C07D213/82 , A61K38/00 , C07K5/06139
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; 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 &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; R5是其中L2是-N（R7）CO的基团-L2（CH2）tR6 - 或-N（R7）CS-基团。化合物能够抑制结合α4整联蛋白与其配体，并且可用于预防和治疗免疫或炎症性疾病。

14. 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。

15. 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。

16. 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。

17. 发明授权

US6093696A Tyrosine derivatives 失效
标题翻译：酪氨酸衍生物
公开(公告)号：US6093696A
公开(公告)日：2000-07-25
申请号：US86421
申请日：1998-05-29
申请人： John Clifford Head , Sarah Catherine Archibald , Graham John Warrellow
发明人： John Clifford Head , Sarah Catherine Archibald , Graham John Warrellow
IPC分类号： A61K38/00 , A61P1/00 , A61P11/06 , A61P17/00 , A61P17/06 , A61P19/02 , A61P29/00 , A61P43/00 , C07D277/06 , C07K5/02 , C07K5/06 , C07K5/078 , A61K31/425 , A61K38/05
CPC分类号： C07K5/06139 , C07D277/06 , C07K5/0202 , C07K5/0205 , C07K5/021 , C07K5/06191 , A61K38/00
摘要： Tyrosine derivatives of formula (1) are described: ##STR1## in which R is (1) a group R.sup.1 X.sup.1 -- where R.sup.1 is an optionally substituted alkyl or aromatic group, and X.sup.1 is a covalent bond or a --(CH.sub.2).sub.n -- [where n is an integer 1 or 2], --C(O)--, --CH.sub.2 C(O)--, --NHC(O)--, --CH.sub.2 NHC(O)--, or --SO.sub.2 -- group, or (2) a group (Hal.sup.1).sub.3 CSO.sub.2 --, where Hal.sup.1 is a fluorine or chlorine atom;R.sup.2 and R.sup.3, which may be the same or different, is each a hydrogen or halogen atom or an alkyl, alkoxy, hydroxyl or nitro group;Alk is an alkylene chain;m is zero or an integer 1;R.sup.4 is a hydrogen atom or a methyl group;R.sup.5 is a group --(CH.sub.2).sub.p CO.sub.2 R.sup.8 where p is zero or an integer 1 and R.sup.8 is a hydrogen atom or an alkyl group;R.sup.6 is a hydrogen atom or an alkyl group;Y is a sulphur atom or a --S(O).sub.q -- group where q is an integer 1 or 2;X.sup.2 is a --C(O)--, --C(O)O--, --CONH-- or --S(O).sub.2 -- group;R.sup.7 is an optionally substituted alkyl group or an aryl or aralkyl group;and the salts, solvates and hydrates thereof.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：描述了式（1）的酪氨酸衍生物：其中R是（1）R1X1基团，其中R1是任选取代的烷基或芳族基团，并且X 1是共价键或 - （CH 2）n - [其中n是整数1或2]，-C（O） - ， - CH 2 C（O） - ， - NHC（O） - ， - CH 2 NHC（O） - 或-SO 2 - 基，或（2） 3CSO2-，其中Hal1是氟或氯原子; R 2和R 3可以相同或不同，各自为氢或卤素原子或烷基，烷氧基，羟基或硝基; Alk是亚烷基链; m为零或整数1; R4是氢原子或甲基; R5是 - （CH2）pCO2R8基团，其中p为0或整数1，R8为氢原子或烷基; R6是氢原子或烷基; Y是硫原子或-S（O）q-基，其中q是整数1或2; X2是-C（O） - ， - C（O）O-，-CONH-或-S（O）2 - 基团; R7是任选取代的烷基或芳基或芳烷基; 及其盐，溶剂化物和水合物。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

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。

19. 发明授权

US06521626B1 Thiocarboxamide derivatives 失效
标题翻译：硫代羧酰胺衍生物
公开(公告)号：US06521626B1
公开(公告)日：2003-02-18
申请号：US09274918
申请日：1999-03-23
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： A61K31426
CPC分类号： C07D277/06 , Y10S977/904
摘要： Compounds of formula (1): wherein R1 is a hydrogen atom or an optionally substituted cycloaliphatic, polycycloaliphatic, heterocycloaliphatic, polyheterocycloaliphatic, aromatic or heteroaromatic group; Alk1 is an optionally substituted aliphatic or heteroaliphatic chain; L1 is a linker atom or group; r and s is each zero or an integer 1; R2 and R3, which may be the same or different, is each a hydrogen or halogen atom or a straight or branched alkyl, haloalkyl, alkoxy, haloalkoxy, hydroxyl or nitro group; Alk2 is a straight or branched alkylene chain; m is zero or an integer 1; R4 is a hydrogen atom or a methyl group; R5 is a hydrogen atom or a straight or branched alkyl group; R6 is a group —(CH2)tR7 in which t is zero or the integer 1 and R7 is an optionally substituted polycycloaliphatic, heterocycloaliphatic, polyheterocycloaliphatic, aromatic or heteroaromatic group; R is a carboxylic acid (—CO2H) or a derivative thereof; and the salts, solvates and hydrates thereof are described. 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：式（1）的化合物：其中R 1是氢原子或任选取代的脂环族，多环脂族，杂脂环族，多杂环脂族，芳族或杂芳族基团; Alk1是任选取代的脂族或杂脂族链; L1是连接原子或基团; r和s 每个为零或整数1; R 2和R 3可以相同或不同，各自为氢或卤素原子或直链或支链烷基，卤代烷基，烷氧基，卤代烷氧基，羟基或硝基; Alk2为直链或支链烷基，支链亚烷基链; m为0或整数1; R4为氢原子或甲基; R5为氢原子或直链或支链烷基; R6为 - （CH2）tR7，其中t为0或整数1和R7是任选取代的多环脂族，杂脂环族，多杂环脂族，芳族或杂芳族基团; R是羧酸（-CO 2 H）或其衍生物;其盐，溶剂化物和水合物被描述。化合物 s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。

20. 发明授权

US06348463B1 Phenylalanine derivatives 失效
标题翻译：苯丙氨酸衍生物
公开(公告)号：US06348463B1
公开(公告)日：2002-02-19
申请号：US09406560
申请日：1999-09-27
申请人： John Clifford Head , John Robert Porter , Graham John Warrellow , Sarah Catherine Archibald , Brian Woodside Hutchinson
发明人： John Clifford Head , John Robert Porter , Graham John Warrellow , Sarah Catherine Archibald , Brian Woodside Hutchinson
IPC分类号： C07D23924
CPC分类号： C07D213/81 , C07D213/89 , C07D251/30 , C07D251/46 , C07D401/12 , C07D409/12 , C07D413/12
摘要： Phenylalanine derivatives of formula (1) are described: in which: Ar1 is an aromatic or heteroaromatic group; L1 is a linker atom or group; R is a carboxylic acid or a derivative thereof; Ar2 is an optionally substituted aromatic or heteroaromatic group; and the salts, solvates, hydrates and N-oxides 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）的苯丙氨酸衍生物：其中：Ar1是芳族或杂芳族基团; L1是连接原子或基团; R是羧酸或其衍生物; Ar2是任选取代的芳族或杂芳族基团;和其盐，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症性疾病。

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