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    Squaric acid derivates
    2.
    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。

    Squaric acid derivatives
    3.
    发明授权
    Squaric acid derivatives 失效
    方酸衍生物

    公开(公告)号：US06740654B2

    公开(公告)日：2004-05-25

    申请号：US09899488

    申请日：2001-07-05

    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： C07D23514

    CPC分类号： C07D495/04 ,  C07D235/30

    摘要： Squaric acid derivatives of formula (1) are described: wherein Het is an optionally substituted bicyclic fused ring heteroaromatic group; L2 is a covalent bond or an atom or group —O—, —S—, —C(O)—, —C(S)—, —S(O)—, —S(O)2, —N(R8)— or —C(R8)(R8a)—; Ar2 is an optionally substituted aromatic or heteroaromatic group; Alk is a chain  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, heteropolycycloaliphatic, aromatic or heteroaromatic group other than a 2,6-naphthyridin-1-yl, isoquinolin-1-yl, 2,7-naphthyridin-1-yl or quinazolin-4-yl 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Het是任选取代的双环稠环杂芳族基团; L 2是共价键或-O - ， - S - ， - C（O） - ， -C（S） - ， - S（O） - ， - S（O）2，-N（R 8） - 或-C（R 8）（R 8a） - ; Ar 2 >是任选取代的芳族或杂芳族基团; Alk是一种链霉素，其中R是羧酸（-CO 2 H）或其衍生物或生物试剂; 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; Alk 1是任选取代的脂族链; n是0或整数1; R 2是氢原子或任选取代的杂脂肪族，脂环族，杂脂族，多环烷基， 除2,6-二氮杂萘-1-基，异喹啉-1-基，2,7-萘啶-1-基或喹唑啉-4-基之外的杂多环脂族，芳族或杂芳族基;以及盐，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生长或迁移的病症。

    3-Substituted isoquinolin-1-yl derivatives
    4.
    发明授权
    3-Substituted isoquinolin-1-yl derivatives 失效
    3-取代的异喹啉-1-基衍生物

    公开(公告)号：US06403608B1

    公开(公告)日：2002-06-11

    申请号：US09867060

    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： C07D21708

    CPC分类号： C07D401/12 ,  C07D217/22 ,  C07D217/24 ,  C07D417/12 ,  C07D487/08

    摘要： 3-Substituted isoquinoline containing squaric acids of formula (1) are described: wherein Ar1 is a 3-substituted isoquinolin-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 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, 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 disordes 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3-取代的异喹啉：其中Ar1是3-取代的异喹啉-1-基; L2是共价键或连接原子或基团; Ar2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霉素; 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为零或整数1; R 2为氢原子或任选取代的杂脂族，脂环族，杂环脂族，多环芳族，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。 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症性紊乱或紊乱。

    2,7-naphthyridine derivatives
    7.
    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。

    Propanoic acid derivatives
    8.
    发明授权
    Propanoic acid derivatives 失效
    丙酸衍生物

    公开(公告)号：US06319922B1

    公开(公告)日：2001-11-20

    申请号：US09448840

    申请日：1999-11-23

    申请人： Rikki Peter Alexander ,  Barry John Langham ,  James Thomas Reuberson ,  Emma Louise Trown ,  Graham John Warrellow

    发明人： Rikki Peter Alexander ,  Barry John Langham ,  James Thomas Reuberson ,  Emma Louise Trown ,  Graham John Warrellow

    IPC分类号： A61K3153

    CPC分类号： C07D239/26 ,  C07D231/12 ,  C07D233/56 ,  C07D239/34 ,  C07D239/42 ,  C07D249/08 ,  C07D401/12 ,  C07D403/12 ,  C07D405/14

    摘要： Propanoic acid derivatives of formula (1) are described: Ar—X1—Ar1—Z—R  (1) in which Ar is a nitrogen base containing group; X1 is linker atom or group; Ar1 is an optionally substituted 5- or 6-membered nitrogen-containing aromatic or non-aromatic monocycle; Z is a group —CH(R13)CH2— [in which R13 is an optionally substituted aliphatic, cycloaliphatic, heteroaliphatic, heterocycloaliphatic, aromatic or heteroaromatic group], —C(R12a)(R13)—CH(R12b)— [in which R12a and R12b together with the carbon atoms to which they are attached form a C3-7cycloalkyl group] or C(R13)═CH—; R is a carboxylic acid (—CO2H) or a derivative or biostere thereof; and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the binding of &agr;V 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）的丙酸衍生物：其中Ar是含氮基团; X1是连接原子或基团; Ar1​​是任选取代的含有5或6元的含氮芳族或非芳族单环; Z是 基团-CH（R 13）CH 2 - [其中R 13是任选取代的脂族，脂环族，杂脂族，杂脂族，芳族或杂芳族基团]，-C（R12a）（R13）-CH（R12b） - [其中R12a和 R12b与它们所连接的碳原子一起形成C 3-7环烷基]或C（R 13）= CH-; R是羧酸（-CO 2 H）或其衍生物或生物试剂; 及其盐，溶剂合物，水合物和N-氧化物。 该化合物能够抑制αV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。