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30 条记录 (耗时 0.063 秒)

    Squaric acid derivates
    7.
    发明授权
    Squaric acid derivates 失效
    方酸衍生物

    公开(公告)号：US06455539B2

    公开(公告)日：2002-09-24

    申请号：US09742038

    申请日：2000-12-21

    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： C07C22914

    CPC分类号： C07D471/04 ,  C07C229/34 ,  C07C229/36 ,  C07C2601/04

    摘要： Squaric acid derivatives of formula (1) are described: wherein R1 is a group Ar1Ar2Alk- in which Ar1 is an optionally substituted aromatic or heteroaromatic group; Ar2 is an optionally substituted phenylene or nitrogen-containing six-membered heteroarylene group; and Alk is a chain —CH2—CH(R)—, —CH═C(R)—, in which R is a carboxylic acid (—CO2H) or a derivative or biostere thereof; R2 is a hydrogen atom or a C1-6 alkyl 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, heteropolycycloaliphatic, 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 or inflammatory disorders, or disorders involving the inappropriate growth or migration of cells.

    摘要翻译： 描述式（1）的方酸衍生物：其中R1是Ar1Ar2Alk-基团，其中Ar1是任选取代的芳族或杂芳族基团; Ar2是任选取代的亚苯基或含氮六元杂亚芳基; 并且Alk是链-CH 2 -CH（R） - ， - CH = C（R） - ，其中R是羧酸（-CO 2 H）或其衍生物或生物固体; R 2是氢原子或C1- 6烷基; L1是共价键或连接原子或基团; n为零或整数1; Alk1为任选取代的脂族链; R3为氢原子或任选取代的杂脂肪族，脂环族，杂环脂族，多环脂族，杂多环脂族 ，芳族或杂芳族基团：及其盐，溶剂合物，水合物和N-氧化物。化合物能够抑制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或涉及 细胞不适当的生长或迁移。

    Cinnamic acid derivatives
    8.
    发明授权
    Cinnamic acid derivatives 失效
    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。

    2,7-naphthyridine derivatives
    10.
    发明授权
    2,7-naphthyridine derivatives 失效
    2,7-萘啶衍生物

    公开(公告)号：US06545013B2

    公开(公告)日：2003-04-08

    申请号：US09867016

    申请日：2001-05-29

    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： A61K31435

    CPC分类号： C07D471/04 ,  Y10S977/904

    摘要： 2,7-Naphthyridine containing squaric acids of formula (1) are described: wherein Ar1 is an optionally substituted 2,7-naphthridin-1-yl group; L2 is a covalent bond or a linker atom or group; Ar2 is an optionally substituted aromatic or heteroaromatic chain; Alk is a chain —CH2CH(R)—, —CH═C(R)—,  in which R is a carboxylic acid (—CO2H) or a derivative or biostere thereof; R1 is a hydrogen atom or a C1-6alkyl group; L1 is a covalent bond or a linker atom or group; Alk1 is an optionally substituted aliphatic chain; n is zero or the integer 1; R2 is a hydrogen atom or an optionally substituted heteroaliphatic, cycloaliphatic, heterocycloaliphatic, polycycloalphatic, heteropoly-cycloaliphatic, 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 immuno or inflammatory disorders or disorders involving the inappropriate growth or migration of cells.

    摘要翻译： 描述了含有式（1）的方酸的2,7-萘啶：其中Ar1是任选取代的2,7-萘啶-1-基; L2是共价键或连接原子或基团; Ar 2是任选取代的芳族 或杂芳族链; Alk是其中R是羧酸（-CO 2 H）或其衍生物或生物试剂的链; R 1是氢原子或C 1-6烷基; L 1是共价键或连接原子或基团; Alk1是任选取代的脂族链; n是0或整数1; R2是氢原子或任选取代的杂脂族，脂环族，杂脂族，多环芳族，杂多环脂族，芳族或杂芳族基团;以及盐，溶剂合物，水合物和 化合物能够抑制整联蛋白与其配体的结合，并且可用于预防和治疗涉及细胞不适当生长或迁移的免疫或炎性疾病或病症。