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    Arylamine substituted bicyclic heteroaromatic compounds as p38 kinase inhibitors
    4.
    发明授权
    Arylamine substituted bicyclic heteroaromatic compounds as p38 kinase inhibitors 失效
    芳胺取代的双环杂芳族化合物作为p38激酶抑制剂

    公开(公告)号：US07423047B2

    公开(公告)日：2008-09-09

    申请号：US10518725

    申请日：2003-06-20

    申请人： Daniel Christopher Brookings ,  Jeremy Martin Davis ,  Barry John Langham

    发明人： Daniel Christopher Brookings ,  Jeremy Martin Davis ,  Barry John Langham

    IPC分类号： A61K31/4365

    CPC分类号： C07D495/04

    摘要： Bicyclic heteroaromatic derivatives of formula (1) are described: F (1) where: the dashed line joining A and C(Ra) is present and represents a bond and A is a —N═ atom or a —C(Rb)═ group, or the dashed line is absent and A is a —N(Rb)—, or —C(Rb)(Rc)— group; X is an —O—, —S— or substituted nitrogen atom or a —S(O)—, —S(O2)— or —NH-group; Y is a nitrogen or substituted carbon atom or a —CH═ group; n is zero or the integer 1; Alk1 is an optionally substituted aliphatic or heteroaliphatic chain L1 is a covalent bond or a linker atom or group; Cy1 is a hydrogen atom or an optionally substituted cycloaliphatic, polycycloaliphatic, heterocycloaliphatic, polyheterocycloaliphatic, aromatic or heteroaromatic group; Ar is an optionally substituted aromatic or heteroaromatic group; and the remaining substituents are defined in the specification. The compounds are potent and selective inhibitors of p38 kinase and are of use in the prophylaxis and treatment of immune or inflammatory disorders.

    摘要翻译： 描述了式（1）的双环杂芳族衍生物：F（1）其中：连接A和C（R a）的虚线表示键，A是-N-原子或 或者虚线不存在，A是-N（R b） - 或-C（R b） （R c）） - 基团; X是-O-，-S-或取代的氮原子或-S（O） - ， - S（O）2 - 或-NH-基团; Y是氮或取代的碳原子或-CH-基团; n为零或整数1; Alk 1是任选取代的脂族或杂脂族链L 1是共价键或连接原子或基团; Cy 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; Ar是任选取代的芳族或杂芳族基团; 并且其余的取代基在说明书中定义。 这些化合物是p38激酶的有效和选择性抑制剂，可用于预防和治疗免疫或炎症性疾病。

    Pyridine and pyrimidine derivatives
    8.
    发明授权
    Pyridine and pyrimidine derivatives 失效
    吡啶和嘧啶衍生物

    公开(公告)号：US07323464B2

    公开(公告)日：2008-01-29

    申请号：US10495885

    申请日：2002-11-20

    申请人： Jeremy Martin Davis ,  Barry John Langham ,  Manisha Naik ,  Daniel Christopher Brookings ,  Rachel Jane Cubbon ,  Richard Jeremy Franklin

    发明人： Jeremy Martin Davis ,  Barry John Langham ,  Manisha Naik ,  Daniel Christopher Brookings ,  Rachel Jane Cubbon ,  Richard Jeremy Franklin

    IPC分类号： C07D403/04 ,  A61K31/506

    CPC分类号： C07D401/04 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/04 ,  C07D413/14

    摘要： Compounds of formula (1) are described in which Ra and Rb is each independently a hydrogen atom or a group Rc, or Ra and Rb together form an oxo (═O) or thio (═S) group; X is a N atom or an optionally substituted CH group: Y is a —O— or —S— atom or —SO— or —SO2— group or an optionally substituted —CH2— or —NH— group with the proviso that when Ra and Rb together form an oxo (═O) or thio (═S) group Y is an optionally substituted —CH2— or —NH-group; L1 is a covalent bond or a linker atom or group; p is zero or the integer 1; Alk1 is an optionally substituted C1-10aliphatic or C1-10heteroaliphatic chain; n is zero the integer 1, 2 or 3 with the proviso that when n is zero Y is an optionally substituted —CH2— group; Ar is an optionally substituted C6-12aromatic or C1-9heteroaromatic group; m is zero or the integer 1, 2 or 3; q is zero or the integer 1 or 2; R1, Rc and Rd are hydrogen atoms or the substituents described in the patent specification; and the salts, solvates, hydrates and N-oxides thereof. The compounds are potent and selective inhibitors of p38 kinase and are useful in the treatment of immune or inflammatory disorders.

    摘要翻译： 描述式（1）的化合物，其中R a和R b各自独立地为氢原子或基团R c，或R （-O）或硫代（-S）基团一起形成一个或多个， X是N原子或任选取代的CH基团：Y是-O-或-S-原子或-SO-或-SO 2 - 基团或任选取代的-CH 2 或-NH-基团，条件是当R a a和R b一起形成氧代（-O）或硫代（-S）基团Y 是任选取代的-CH 2 - 或-NH-基团; L 1是共价键或连接子原子或基团; p为零或整数1; Alk 1是任选取代的C 1-10 1-10脂族或C 1-10 1-10杂脂肪族链; n为整数1,2或3，条件是当n为零时，Y为任选取代的-CH 2 - 基团; Ar是任选取代的C 6-12芳族或C 1-19杂芳族基团; m为零或整数1,2或3; q为零或整数1或2; R 1，R 2和R d是氢原子或专利说明书中所述的取代基; 及其盐，溶剂合物，水合物和N-氧化物。 这些化合物是p38激酶的有效和选择性抑制剂，可用于治疗免疫或炎症性疾病。

    Bicyclic oxopyridine and oxopyrimidine derivatives
    9.
    发明授权
    Bicyclic oxopyridine and oxopyrimidine derivatives 失效
    双环氧基吡啶和氧代嘧啶衍生物

    公开(公告)号：US07176215B2

    公开(公告)日：2007-02-13

    申请号：US10492466

    申请日：2002-10-16

    申请人： Jeremy Martin Davis ,  Daniel Christopher Brookings ,  Barry John Langham

    发明人： Jeremy Martin Davis ,  Daniel Christopher Brookings ,  Barry John Langham

    IPC分类号： A01N43/42 ,  A61K31/44 ,  C07D471/02 ,  C07D491/02 ,  C07D498/02

    CPC分类号： C07D471/04 ,  C07D495/04

    摘要： Compounds of formulae (1a) and (1b) are described: in which the dashed line represents an optional bond; A is a —N═ atom or a —N(Rb)—, —C(Rb)═ or —C(Rb)(RC)— group; Ra, Rb and Rc is each independently a hydrogen atom or an optionally substituted C1-6alkyl group; X is an —O— or —S— atom or —NH— group or substituted N atom; each Y is independently a N atom or CH group or substituted C atom; n is zero or the integer 1; Alk1 is an optionally substituted aliphatic or heteroaliphatic chain L1 is a covalent bond or a linker atom or group; Cy1 is a hydrogen atom or an optionally substituted cycloaliphatic, polycycloaliphatic, heterocycloaliphatic, polyheterocycloaliphatic, aromatic or heteroaromatic group; Ar is an optionally substituted aromatic or heteroaromatic group; and the salts, solvates, hydrates and N-oxides thereof; The compounds are potent inhibitors of p38 kinase and are use in the prophylaxis or treatment of p38 kinase mediated diseases or disorders, such as rheumatoid arthritis

    摘要翻译： 描述式（1a）和（1b）的化合物：其中虚线表示任选的键; A是-N-原子或-N（R b） - ， - C（R b） - 或-C（R b） >）（R 0 C） - 基团; R a，R b和R c各自独立地为氢原子或任选取代的C 1-6烷基， 烷基; X是-O-或-S-原子或-NH-基团或取代的N原子; 每个Y独立地是N原子或CH基团或取代的C原子; n为零或整数1; Alk 1是任选取代的脂族或杂脂族链L 1是共价键或连接原子或基团; Cy 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; Ar是任选取代的芳族或杂芳族基团; 及其盐，溶剂合物，水合物及其N-氧化物; 这些化合物是p38激酶的有效抑制剂，并且用于预防或治疗p38激酶介导的疾病或病症，例如类风湿性关节炎