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22 条记录 (耗时 0.04 秒)

    Pyridine and pyrimidine derivatives
    5.
    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
    6.
    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

    5-cyano-2-aminopyrimidine derivatives
    7.
    发明授权
    5-cyano-2-aminopyrimidine derivatives 失效
    5-氰基-2-氨基嘧啶衍生物

    公开(公告)号：US06579983B1

    公开(公告)日：2003-06-17

    申请号：US09596952

    申请日：2000-06-16

    申请人： Mark James Batchelor ,  David Festus Charles Moffat ,  Jeremy Martin Davis ,  Martin Clive Hutchings

    发明人： Mark James Batchelor ,  David Festus Charles Moffat ,  Jeremy Martin Davis ,  Martin Clive Hutchings

    IPC分类号： C07D23942

    CPC分类号： C07D239/42 ,  C07D401/04 ,  C07D403/12 ,  C07D409/04

    摘要： Pyrimidines of formula (1) are described wherein Ar is an optionally substituted aromatic or heteroaromatic group; R1 is a hydrogen atom or a straight or branched chain alkyl group; R2 is a —X1—R3 group where X1 is a direct bond or a linker atom or group, and R3 is an optionally substituted aliphatic, cycloaliphatic, heteroaliphatic, heterocycloaliphatic, aromatic or heteroaromatic group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are selective KDR Kinase and/or FGFr Kinase inhibitors and are of use in the prophylaxis and treatment of disease states assoicated with angiogenesis.

    摘要翻译： 描述式（1）的嘧啶，其中Ar是任选取代的芳族或杂芳族基团; R 1是氢原子或直链或支链烷基; R 2是-X 1 -R 3基团，其中X 1是直接键或连接原子或 基团，和R 3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;及其盐，溶剂合物，水合物和N-氧化物。化合物是选择性KDR激酶和/或FGFr激酶抑制剂， 与血管生成有关的疾病状态的预防和治疗。

    4,5-disubstituted-2-aminopyrimidines
    8.
    发明授权
    4,5-disubstituted-2-aminopyrimidines 失效
    4,5-二取代-2-氨基嘧啶

    公开(公告)号：US06600037B1

    公开(公告)日：2003-07-29

    申请号：US09692368

    申请日：2000-10-19

    申请人： Jeremy Martin Davis ,  David Festus Charles Moffat

    发明人： Jeremy Martin Davis ,  David Festus Charles Moffat

    IPC分类号： C07D23942

    CPC分类号： C07D239/42 ,  A61K31/505 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/12 ,  C07D403/12

    摘要： Pyrimidines of formla (1) are described: wherein R1 is a —XR6 group; R2 and R3 which may be the same or different is each a hydrogen or halogen atom or a group selected from an optionally substituted aliphatic, cycloaliphatic, heteroaliphatic, heterocycloaliphatic, —OH, —OR10 [where R10 is an optionally substituted aliphatic, cycloaliphatic, heteroaliphatic, heterocycloaliphatic, aromatic or heteroaromatic group] —SH, —NO2, —CN, —SR10, —COR10, S(O)R10, —SO2R8, —SO2N(R8)(R9), —CO2R8, —CON(R8)(R9), —CSN(R8)(R9), —NH2 or substituted amino group; R4 is a X1R11 group where X1 is a covalent bond or a —C(R12)(R13)— [where each of R12 and R13 is a hydrogen or halogen atom or a hydroxyl, alkyl or haloalkyl group] or —C(O)— group and R11 is an optionally substituted phenyl, thienyl, thiazolyl or indolyl group; R5 is a halogen atom or an alkynyl group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are selective KDR kinase and/or FGFr kinase inhibitors and are of use in the prophylaxis and treatment of disease states associated with angiogenesis.

    摘要翻译： 描述了formla（1）的嘧啶：其中R1是-XR6基团; R2和R3可以相同或不同，各自为氢或卤素原子或选自任选取代的脂族，脂环族，杂脂族，杂环脂族， OH，-OR 10 [其中R 10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] -SH，-NO 2，-CN，-SR 10，-COR 10，S（O）R 10，-SO 2 R 8，-SO 2 N （R8）（R9），-CO2R8，-CON（R8）（R9），-CSN（R8）（R9），-NH2或取代氨基; R4是X1R11基团，其中X1是共价键或-C （R 12）（R 13） - [其中R 12和R 13各自为氢或卤素原子或羟基，烷基或卤代烷基]或-C（O） - 基，R 11为任选取代的苯基，噻吩基，噻唑基或吲哚基 基团; R5是卤素原子或炔基;以及它们的盐，溶剂合物，水合物和N-氧化物。化合物是选择性KDR激酶和/或FGFr激酶抑制剂，并且可用于植物 治疗与血管生成相关的疾病状态。

    Substituted 2-anilinopyrimidines useful as protein kinase inhibitors
    9.
    发明授权
    Substituted 2-anilinopyrimidines useful as protein kinase inhibitors 失效
    用作蛋白激酶抑制剂的取代的2-苯胺基嘧啶

    公开(公告)号：US5958935A

    公开(公告)日：1999-09-28

    申请号：US753041

    申请日：1996-11-19

    申请人： Peter David Davis ,  David Festus Charles Moffat ,  Jeremy Martin Davis ,  Martin Clive Hutchings

    发明人： Peter David Davis ,  David Festus Charles Moffat ,  Jeremy Martin Davis ,  Martin Clive Hutchings

    IPC分类号： C07D239/42 ,  C07D239/48 ,  C07D401/04 ,  C07D417/04 ,  A61K31/505 ,  C07D239/28

    CPC分类号： C07D401/04 ,  C07D239/42 ,  C07D239/48 ,  C07D417/04

    摘要： 2-Anilinopyrimidines, processes for their preparation, pharmaceutical compositions containing them, their use in medicine. In a preferred embodiment, the compounds have the general formula (1): ##STR1## wherein R.sup.1 is preferably methoxy; R.sup.2 and R.sup.3 are preferably methyl; R.sup.4 is preferably a hydrogen atom; R.sup.5 is a hydrogen atom or an optionally substituted straight or branched chain alkyl, alkenyl or alkynyl group; R.sup.6 is a hydrogen or halogen atom or an amino (--NH.sub.2), substituted amino, nitro, carboxyl (--CO.sub.2 H), esterified carboxyl or --X.sup.1 R.sup.6a where X.sup.1 is a direct bond or a linker atom or group and R.sup.6a is an optionally substituted straight or branched chain alkyl, alkenyl or alkynyl group; X is a direct bond or a linker atom or group; and R.sup.7 is an optionally substituted aliphatic, cycloaliphatic, heteroaliphatic, heterocycloaliphatic, aromatic or heteroaromatic group. Compounds of the invention are selective protein kinase inhibitors, particularly the kinases p56.sup.lck, p59.sup.fyn, ZAP-70 and protein kinase C and are of use in the prophylaxis and treatment of immune diseases, hyperproliferative disorders and other diseases in which inappropriate protein kinase action is believed to have a role.

    摘要翻译： 2-苯胺基嘧啶，其制备方法，含有它们的药物组合物，它们在药物中的用途。 在优选的实施方案中，化合物具有通式（1）：其中R 1优选为甲氧基; R2和R3优选为甲基; R4优选为氢原子; R5是氢原子或任选取代的直链或支链烷基，烯基或炔基; R6是氢或卤原子或氨基（-NH2），取代的氨基，硝基，羧基（-CO2H），酯化的羧基或-X1R6a，其中X1是直接键或连接原子或基团，R 6a是任选取代的直链 或支链烷基，烯基或炔基; X是直接键或连接原子或基团; 并且R 7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。 本发明的化合物是选择性蛋白激酶抑制剂，特别是激酶p56lck，p59fyn，ZAP-70和蛋白激酶C，并且可用于预防和治疗免疫疾病，过度增殖性疾病和其中认为不适当的蛋白激酶作用的其它疾病 有一个角色。