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    3-(Carbonyl) 1h-indazole compounds as cyclin dependent kinases (cdk) inhibitors
    1.
    发明申请
    3-(Carbonyl) 1h-indazole compounds as cyclin dependent kinases (cdk) inhibitors 审中-公开
    3-（羰基）1h-吲唑化合物作为细胞周期蛋白依赖性激酶（cdk）抑制剂

    公开(公告)号：US20060135516A1

    公开(公告)日：2006-06-22

    申请号：US10524760

    申请日：2003-08-08

    申请人： Valerio Berdini ,  Maria Carr ,  Gordon Saxty ,  Alison Woolford ,  Paul Wyatt

    发明人： Valerio Berdini ,  Maria Carr ,  Gordon Saxty ,  Alison Woolford ,  Paul Wyatt

    IPC分类号： A61K31/5377 ,  A61K31/496 ,  A61K31/454 ,  A61K31/4439 ,  A61K31/43 ,  C07D498/02

    CPC分类号： C07D513/04

    摘要： The invention provides a compound of the formula (I): wherein E is O, S, or NH; G is selected from hydrogen; carbocyclic and heterocyclic groups having from 3 to 12 ring members; and acyclic C1-8 hydrocarbyl groups optionally substituted; provided that E—G is not OH or SH and further provided that E—G does not contain the group O—O; two adjacent moieties selected from R3, R4, R5 and R6, together with the carbon atoms to which they are attached, form a fused heterocyclic group having from 5 to 7 ring members and 1, 2 or 3 ring heteroatoms selected from N, O and S; and the other two moieties selected from R3, R4, R5 and R6 are the same or different and are each as defined in the description. The Invention also provides compounds of the formula (I) for use as inhibitors of cyclin dependent kinases and for use in the treatment of disease states and conditions mediated by cyclin dependent kinases.

    摘要翻译： 本发明提供式（I）的化合物：其中E是O，S或NH; G选自氢; 具有3至12个环成员的碳环和杂环基; 和任选取代的非环状C 1-8烃基; 条件是E-G不是OH或SH，并且进一步规定E-G不含O-O基团; 选自R 3，R 4，R 5和R 6的两个相邻部分与碳原子一起 形成具有5至7个环成员和1,2或3个选自N，O和S的环杂原子的稠合杂环基; 并且选自R 3，R 4，R 5和R 6的另外两个部分是相同或 不同的并且各自如说明书中所定义。 本发明还提供用作细胞周期蛋白依赖性激酶抑制剂的式（I）化合物，并用于治疗由细胞周期蛋白依赖性激酶介导的疾病状态和状况。

    3,4-Disubstituted Pyrazoles as Cyclin Dependent Kinases (Cdk) or Aurora Kinase or Glycogen Synthase 3 (Gsk-3) Inhibitors
    4.
    发明申请
    3,4-Disubstituted Pyrazoles as Cyclin Dependent Kinases (Cdk) or Aurora Kinase or Glycogen Synthase 3 (Gsk-3) Inhibitors 审中-公开
    作为细胞周期蛋白依赖性激酶（Cdk）或极光激酶或糖原合酶3（Gsk-3）抑制剂的3,4-二取代吡唑类

    公开(公告)号：US20080004270A1

    公开(公告)日：2008-01-03

    申请号：US11571713

    申请日：2005-07-05

    申请人： Adrian Gill ,  Maria Carr ,  Michael O'Brien ,  Paul Wyatt ,  Valerio Berdini

    发明人： Adrian Gill ,  Maria Carr ,  Michael O'Brien ,  Paul Wyatt ,  Valerio Berdini

    IPC分类号： A61K31/5377 ,  A61K31/4188 ,  A61P25/28 ,  A61P35/00 ,  C07D235/02 ,  C07D471/02 ,  C07D265/34 ,  A61P37/00 ,  A61P31/12 ,  A61K31/47

    CPC分类号： C07D471/04 ,  C07D487/04 ,  C07D495/04

    摘要： The invention provides compounds of the formula (I); or salts or solvates or N-oxides thereof; wherein: Rq is selected from groups (a), (b) and (c); the asterisk denoting the point of attachment to the pyrazole ring; X is N or CR5; X″ is NR4; O, S or S(O); A is a bond or —(CH2)m—(B)n—; B is C═O, NRg(C═O) or O(C═O) wherein Rg is hydrogen or C1-4 hydrocarbyl optionally substituted by hydroxy or C1-4 alkoxy; m is 0, 1 or 2; n is 0 or 1; R0 is hydrogen or, together with NRg when present, forms a group —(CH2)p— wherein p is 2 to 4; and R1 to R6b are as defined in the description. Compounds of the formula (I) have activity as inhibitors of CDK, aurora and GSK-3 kinases are useful in treating or preventing diseases such as cancers that are mediated by the said kinases.

    摘要翻译： 本发明提供式（I）化合物; 或其盐或溶剂合物或N-氧化物; 其中：R q选自（a），（b）和（c）组; 星号表示与吡唑环的连接点; X是N或CR 5; X“是NR 4; O，S或S（O）; A是键或 - （CH 2）m - （B）n - B为CO，NR（CO）或O（CO），其中R为氢或任选被羟基取代的C 1-4烷基烃基 或C 1-4烷氧基; m为0,1或2; n为0或1; 当存在时，R 0是氢或与NR a一起形成基团 - （CH 2 CH 2）n - - 其中p为2至4; 和R 1至R 6b如说明书中所定义。 式（I）化合物具有作为CDK抑制剂的活性，极光和GSK-3激酶可用于治疗或预防诸如由所述激酶介导的癌症的疾病。

    5 Amino-2-carbonylthiophene derivatives for use as p38 map kinase inhibitors in the treatment of inflammatory diseases
    6.
    发明申请
    5 Amino-2-carbonylthiophene derivatives for use as p38 map kinase inhibitors in the treatment of inflammatory diseases 审中-公开

    公开(公告)号：US20070082898A1

    公开(公告)日：2007-04-12

    申请号：US10553361

    申请日：2004-04-13

    申请人： Adrian Gill ,  Steven Woodhead ,  Maria Carr

    发明人： Adrian Gill ,  Steven Woodhead ,  Maria Carr

    IPC分类号： A61K31/538 ,  A61K31/522 ,  A61K31/52 ,  A61K31/517 ,  A61K31/496 ,  A61K31/4745 ,  A61K31/4709 ,  A61K31/4178 ,  A61K31/416 ,  C07D417/02 ,  C07D413/02 ,  C07D409/02

    CPC分类号： C07D409/12 ,  C07D333/38 ,  C07D409/14 ,  C07D417/12 ,  C07D417/14

    摘要： The invention provides the use of a compound for the manufacture of a medicament for the prophylaxis or treatment of a disease state or condition mediated by a p38 MAP kinase; the compound being defined by formula (I): wherein: R1 and R2 are the same or different and each is selected from hydrogen, C1-4 hydrocarbyl, halogen and cyano; X is selected from C═O, C═S, C(═O)NH, C(═S)NH, C(═O)O, C(═O)S, C(═S)O and C(═S)S; R3 is selected from aryl and hetcroaryl groups each having from 5 to 12 ring members, the aryl and heteroaryl groups each being unsubstituted or substituted by one or more substituent groups R7 selected from halogen, hydroxy, trifluoromethyl, cyano, nitro, carboxy, amino, carbocyclic and heterocyclic groups having from 3 to 12 ring members; a group Ra—Rb wherein Ra is a bond, 0, CO, X1C(X2), C(X2)X1, X1C(X2)X1, S, SO, SO2, NRc, SO2NRc or NRcSO2; and Rb is selected from hydrogen, carbocyclic and heterocyclic groups having from 3 to 7 ring members, and a C1-8 hydrocarbyl group optionally substituted by one or more substituents selected from hydroxy, oxo, halogen, cyano, nitro, amino, mono- or di-C1-4 hydrocarbylamino, carbocyclic and heterocyclic groups having from 3 to 12 ring members and wherein one or more carbon atoms of the C1-8 hydrocarbyl group may optionally be replaced by O, S, SO, SO2, NRc, X1C(X2), C(X2)X1 or X1C(X2)X1; X1 is O, S or NRc and X2 is ═O, ═S or ═NRc; Rc is hydrogen or C1-4 hydrocarbyl; R4 is a group YR5 or a group R6; Y is is NH, O or S; R5 is selected from (a) carbocyclic and heterocyclic groups having from 3 to 12 ring members; and (b) C1-8 hydrocarbyl groups optionally substituted by one or more substituents selected from hydroxy, oxo, halogen, cyano, amino, mono- or di- C1-4 hydrocarbylamino, and carbocyclic and heterocyclic groups having from 3 to 12 ring members, wherein one or more carbon atoms of the C1-8 hydrocarbyl group may optionally be replaced by O, S, SO, SO2, NRc, X1C(X2), C(X2)X1 or X1C(X2)X1, provided that when Y is O, a carbon atom adjacent to the group Y is not replaced by O; and R6 is a heterocyclic group having from 4 to 12 ring members and containing at least one ring nitrogen atom through which R6 is linked to the adjacent carbonyl group; wherein the carbocyclic and heterocyclic groups of substituents R5 and R6 are each unsubstituted or substituted by one or more substituent groups R7 as hereinbefore defined. Also provided are novel compounds, pharmaceutical compositions containing the compounds and methods for their preparation.

    5-Morpholinylmethylthiophenyl Pharmaceutical Compounds As P38 MAP Kinase Modulators
    8.
    发明申请
    5-Morpholinylmethylthiophenyl Pharmaceutical Compounds As P38 MAP Kinase Modulators 审中-公开
    5-吗啉基甲硫基苯基药物化合物为P38

    公开(公告)号：US20070208015A1

    公开(公告)日：2007-09-06

    申请号：US10599931

    申请日：2005-04-13

    申请人： Adrian Gill ,  Maria Carr ,  John Lyons ,  Neil Thompson ,  David Rees

    发明人： Adrian Gill ,  Maria Carr ,  John Lyons ,  Neil Thompson ,  David Rees

    IPC分类号： A61K31/5377 ,  C07D413/14

    CPC分类号： C07D333/36 ,  C07D409/12 ,  C07D417/12

    摘要： The invention provides compounds of the formula (I) or a salt, solvate or N-oxide thereof, wherein: R1 and R2 are the same or different and each is selected from hydrogen, saturated C1-3 hydrocarbyl, halogen and cyano; X is selected from C═O, C═S, C(═O)NH, C(═S)NH, C(═O)O, C(═O)S, C(═S)O and C(═S)S; R3 is selected from aryl and heteroaryl groups each having from 5 to 12 ring members and being unsubstituted or substituted by one or more substituent groups R10 as defined in the claims; R4 and R5 are the same or different and are selected from hydrogen and methyl; or one of R4 and R5 is selected from hydroxymethyl and ethyl and the other is hydrogen; and R6 and R7 are the same or different and are selected from hydrogen and methyl. The compounds of the formula (I) hayed activity as p38 MAP kinase and Taf kinase inhibitors.

    摘要翻译： 本发明提供式（I）化合物或其盐，溶剂合物或N-氧化物，其中：R 1和R 2相同或不同，各自为 选自氢，饱和C 1-3烃基，卤素和氰基; X选自C-O，C-S，C（-O）NH，C（-S）NH，C（-O）O，C（-O）S，C（-S）O和C（-S） R 3选自具有5至12个环成员的芳基和杂芳基，并且未被取代或被权利要求中所定义的一个或多个取代基R 10取代; R 4和R 5相同或不同，并且选自氢和甲基; 或者R 4和R 5中的一个选自羟甲基和乙基，另一个是氢; 和R 6和R 7相同或不同，并且选自氢和甲基。 式（I）化合物具有作为p38 MAP激酶和Taf激酶抑制剂的活性。