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9 条记录 (耗时 0.033 秒)

    Pyridinylamino-pyrimidine derivatives as protein kinase inhibitors
    1.
    发明申请
    Pyridinylamino-pyrimidine derivatives as protein kinase inhibitors 审中-公开

    公开(公告)号：US20060241297A1

    公开(公告)日：2006-10-26

    申请号：US11339059

    申请日：2006-01-25

    申请人： Shudong Wang ,  Christopher Meades ,  Darren Gibson ,  Peter Fischer

    发明人： Shudong Wang ,  Christopher Meades ,  Darren Gibson ,  Peter Fischer

    IPC分类号： C07D417/14

    CPC分类号： C07D417/14

    摘要： The present invention relates to compounds of formula I, or pharmaceutically acceptable salts thereof, wherein: (A) “a” is a single bond and “b” is a double bond; R1 and R2 are each independently as defined below; R10 is absent; or (B) “a” is a double bond and “b” is a single bond; R1 is oxygen; R2 is as defined below; and R10 is H or alkyl; X is S, O, NH, or NR7; Y is N or CR8; one of Z1, Z2, and Z3 is N or N+Ra and the remainder are each independently CR7; R1, R2, R5 and R6 are each independently R7; R3 and R4 are each independently R8; each R7 is independently H, halogen, NRbRc, ORd or a hydrocarbyl group optionally substituted by one or more R9 groups; each R8 is independently H or (CH2)nR9, where n is 0 or 1; each R9 is independently selected from H, halogen, NO2, CN, Re, NHCORf, CF3, CORg, NRhRi, CONRjRk, SO2NRlRm, SO2Rn, ORp, OCH2CH2ORq, morpholine, piperidine and piperazine; and Ra-q are each independently H or alkyl, wherein said alkyl group is optionally substituted by one or more R9 groups; where the compound is other than [4-(2,4-dimethyl-thiazol-5-yl)-pyrimidin-2-yl]-pyridin-2-yl-amine and 4-[4-fluorophenyl)-1-(1-methyl-4-piperidinyl)-1H-imidazol-5-yl]-N-4-pyridinyl-2-pyrimidinamine. Further aspects of the invention relate to the use of compounds of formula I in the treatment of proliferative disorders, viral disorders, CNS disorders, strokes, alopecia and/or diabetes.

    Pyrimidin-4-YL-3, 4-thione compounds and their use in therapy
    2.
    发明申请
    Pyrimidin-4-YL-3, 4-thione compounds and their use in therapy 有权

    公开(公告)号：US20070021452A1

    公开(公告)日：2007-01-25

    申请号：US11408463

    申请日：2006-04-21

    申请人： Shudong Wang ,  Gavin Wood ,  Kenneth Duncan ,  Christopher Meades ,  Darren Gibson ,  Janice McLachlan ,  Alex Perry ,  David Blake ,  Daniella Zheleva ,  Peter Fischer

    发明人： Shudong Wang ,  Gavin Wood ,  Kenneth Duncan ,  Christopher Meades ,  Darren Gibson ,  Janice McLachlan ,  Alex Perry ,  David Blake ,  Daniella Zheleva ,  Peter Fischer

    IPC分类号： A61K31/506 ,  C07D417/04

    CPC分类号： C07D417/04 ,  C07D417/14

    摘要： The present invention relates to compounds of formula I, or pharmaceutically acceptable salts thereof, wherein R1 and R5 are each independently H, C(ORj′) or a hydrocarbyl group optionally substituted by one or more R6 groups; R2, R3, and R4 are each independently H, alkyl or alkenyl, each of which may be optionally substituted with one or more R7 groups; R6 and R7 are each independently halogen, NO2, CN, (CH2)mORa, O(CH2)nORb, (CH2)pNRcRd, CF3, COORe, CONRfRg, CORh, SO3H, SO2Ri, SO2NRjRk, (CH2)qNRa′CORg′, Rf′, (CH2)rNRb′SO2Rh′, SO2NRd′Ri′, SO2NRe′(CH2)sORc′, heterocycloalkyl or heteroaryl, wherein said heterocycloalkyl and heteroaryl may be optionally substituted by one or more substituents selected from aralkyl, sulfonyl, Rm and CORn; Rg′, Rh′, Ri′ and Rj′ are each independently selected from alkyl, aryl, aralkyl and heteroaryl, each of which may be optionally substituted with one or more substituents selected from halogen, OH, NO2, NH2 CF3 and COOH; m, p, q and r are each independently 0, 1, 2 or 3; n and s are each independently 1, 2, or 3; and Ra-n and Ra′-f′ are each independently H or alkyl. Further aspects of the invention relate to pharmaceutical compositions comprising such compounds, and their use in the preparation of a medicament for treating one or more of the following: a proliferative disorder, a viral disorder, a CNS disorder, a stroke, alopecia and diabetes.

    Pyrimidin-4-yl-3, 4-thione compounds and their use in therapy
    4.
    发明授权
    Pyrimidin-4-yl-3, 4-thione compounds and their use in therapy 有权
    嘧啶-4-基-3,4-硫酮化合物及其在治疗中的应用

    公开(公告)号：US07902361B2

    公开(公告)日：2011-03-08

    申请号：US11408463

    申请日：2006-04-21

    申请人： Shudong Wang ,  Gavin Wood ,  Kenneth Duncan ,  Christopher Meades ,  Darren Gibson ,  Janice McLachlan ,  Alex Perry ,  David Blake ,  Daniella I. Zheleva ,  Peter Martin Fischer

    发明人： Shudong Wang ,  Gavin Wood ,  Kenneth Duncan ,  Christopher Meades ,  Darren Gibson ,  Janice McLachlan ,  Alex Perry ,  David Blake ,  Daniella I. Zheleva ,  Peter Martin Fischer

    IPC分类号： C07D403/04 ,  C07D403/14 ,  C07D417/04 ,  C07D417/14 ,  A61K31/506 ,  A61P3/10 ,  A61P19/02 ,  A61P35/02

    CPC分类号： C07D417/04 ,  C07D417/14

    摘要： The present invention relates to compounds of formula I, or pharmaceutically acceptable salts thereof, wherein R1 and R5 are each independently H, C(ORj′) or a hydrocarbyl group optionally substituted by one or more R6 groups; R2, R3, and R4 are each independently H, alkyl or alkenyl, each of which may be optionally substituted with one or more R7 groups; R6 and R7 are each independently halogen, NO2, CN, (CH2)mORa, O(CH2)nORb, (CH2)pNRcRd, CF3, COORe, CONRfRg, CORh, SO3H, SO2Ri, SO2NRjRk, (CH2)qNRa′CORg′, Rf′, (CH2)rNRb′SO2Rh′, SO2NRd′Ri′, SO2NRe′(CH2)sORc′, heterocycloalkyl or heteroaryl, wherein said heterocycloalkyl and heteroaryl may be optionally substituted by one or more substituents selected from aralkyl, sulfonyl, Rm and CORn; Rg′, Rh′, Ri′ and Rj′ are each independently selected from alkyl, aryl, aralkyl and heteroaryl, each of which may be optionally substituted with one or more substituents selected from halogen, OH, NO2, NH2 CF3 and COOH; m, p, q and r are each independently 0, 1, 2 or 3; n and s are each independently 1, 2, or 3; and Ra-n and Ra′-f′ are each independently H or alkyl. Further aspects of the invention relate to pharmaceutical compositions comprising such compounds, and their use in the preparation of a medicament for treating one or more of the following: a proliferative disorder, a viral disorder, a CNS disorder, a stroke, alopecia and diabetes.

    摘要翻译： 本发明涉及式I化合物或其药学上可接受的盐，其中R 1和R 5各自独立地为H，C（OR j'）或任选被一个或多个R 6基团取代的烃基; R 2，R 3和R 4各自独立地为H，烷基或烯基，其各自可以任选被一个或多个R 7基团取代; R6和R7各自独立地为卤素，NO2，CN，（CH2）mORa，O（CH2）nORb，（CH2）pNRcRd，CF3，COORe，CONRfRg，CORh，SO3H，SO2Ri，SO2NRjRk，（CH2）qNRa'CORg' Rf'，（CH2）rNRb'SO2Rh'，SO2NRd'Ri'，SO2NRe'（CH2）sORc'，杂环烷基或杂芳基，其中所述杂环烷基和杂芳基可以任选地被一个或多个选自芳烷基，磺酰基，R m和 玉米; R''，R''，R''和R“'各自独立地选自烷基，芳基，芳烷基和杂芳基，它们各自可以被一个或多个选自卤素，OH，NO 2，NH 2 CF 3和COOH的取代基取代; m，p，q和r各自独立地为0,1,2或3; n和s各自独立地为1,2或3; 和Ra-n和Ra'-f'各自独立地为H或烷基。 本发明的其它方面涉及包含这些化合物的药物组合物及其在制备用于治疗以下一种或多种的药物中的用途：增殖性病症，病毒病症，CNS病症，中风，脱发和糖尿病。

    2-Aminophenyl-4-phenylpyrimidines as kinase inhibitors
    6.
    发明申请
    2-Aminophenyl-4-phenylpyrimidines as kinase inhibitors 审中-公开

    公开(公告)号：US20070021419A1

    公开(公告)日：2007-01-25

    申请号：US11339058

    申请日：2006-01-25

    申请人： Shudong Wang ,  Janice McLachlan ,  Darren Gibson ,  Ashley Causton ,  Nicholas Turner ,  Peter Fischer

    发明人： Shudong Wang ,  Janice McLachlan ,  Darren Gibson ,  Ashley Causton ,  Nicholas Turner ,  Peter Fischer

    IPC分类号： A61K31/5377 ,  A61K31/506 ,  C07D413/14 ,  C07D403/14

    CPC分类号： C04B35/632 ,  C07D239/42 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D403/10

    摘要： The present invention relates to compounds of formula I, or pharmaceutically acceptable salt thereof, wherein: Z is CR10 or N; one of R1 and R2 is selected from (CH2)mR11, (CH2)mR12, (CH2)mNR12R13, (CH2)mOR12, (CH2)mNR13CO(CH2)nR11, (CH2)mNR13COR12, (CH2)mCONR13(CH2)nR11, (CH2)mCONR12R13, (CH2)mCO(CH2)nR11 and (CH2)mCOR12; where m is 0, 1, 2, 3 or 4 and n is 1, 2, 3 or 4; the other of R1 and R2 is H or R11; R3 and R5 are both H; R4 is H or R11; R6is H or (CH2)pR11, where p is 0 or 1; R7, R9 and R10 are each independently H or R11; R8 is selected from H, halogen, NO2, CN, OR13, NR13R14, NHCOR13, CF3, COR13, R13, CONR13R15, SO2NR13R14, SO2R13, NR13SO2R14, OCH2CH2OH, OCH2CH2OMe, morpholine, piperidine, and piperazine; each R11 is independently halogen, NO2, CN, (CH2)qOR13(CH2)rNR13R14, NHCOR13, CF3, COR13, R13, CONR13R14, SO2NR13R14, SO2R13, OR12, NR13SO2R14, OCH2CH2OH, OCH2CH2OMe, NR13SO2R12, (CH2)sNR12R13, morpholine, piperidine or piperazine, where q, r and s are each independently 0, 1, 2, 3 or 4; each R12 is independently a hydrocarbyl group optionally containing one or more heteroatoms and optionally substituted with one or more R11 groups; each R13 and each R14 is independently H or an alkyl group; and R15 is an alkyl group; providing that when Z is CR10 and R9 is H, at least one of R7, R8 and R10 is other than OMe; and Z is CR10 and R7-9 are all H, R10 is other than OCF2CHF2.

    Compounds
    8.
    发明申请
    Compounds 审中-公开
    化合物

    公开(公告)号：US20080318954A1

    公开(公告)日：2008-12-25

    申请号：US10588372

    申请日：2005-02-07

    申请人： Kenneth Duncan ,  Darren Gibson ,  Shudong Wang ,  Daniella I. Zheleva ,  Peter Martin Fischer

    发明人： Kenneth Duncan ,  Darren Gibson ,  Shudong Wang ,  Daniella I. Zheleva ,  Peter Martin Fischer

    IPC分类号： A61K31/505 ,  A61P19/08 ,  C07D401/02 ,  A61K31/5355 ,  A61K31/444 ,  C07D413/02 ,  C07D417/04

    CPC分类号： C07D417/04 ,  C07D417/14

    摘要： The present invention relates to compounds of formula (I), or a pharmaceutically acceptable salts thereof, wherein: Z1: 1 is N or CH; Z2 and Z3 are each independently N or CR7; R1, R2, R3, R4, R5, R6, and R7 are each independently H, R8, or R9; each R8 is independently a hydrocarbyl group; and each R9 is independently halo, NO2, alkoxy, CN, CF3, S03H, SO2NR10R11, S02R12, NR13R14(CH2)aCOOR15, (CH2)bCONR16R17, (CH2)cCOR18 or (CH2)dOH; a, b, c and d are each independently 0, 1 2 3 or 4; R10-18 are each independently H or alkyl; provided that when R1 and R2 are both H, Z1 is CH; or Z2 is N; or Z1 is CH and Z2 is N; and wherein the compound is other than 4-(4,5-dimethylthiazol-2-yl)-N-(3,4,5trimethoxyphenyl)-2-pyrimidineamine or 4-(5-(2-hydroxyethyl)-4-methylthiazol-2-yl)N-(3,4,5-trimethoxyphenyl)-2-pyrimidineamine. Further aspects relate to the use of compounds of formula (I) in the preparation of a medicament for treating one or more disorders selected from a proliferative disorder, a viral disorder, a CNS disorder, diabetes, stroke or alopecia.

    摘要翻译： 本发明涉及式（I）化合物或其药学上可接受的盐，其中：Z1：1是N或CH; Z2和Z3各自独立地为N或CR7; R 1，R 2，R 3，R 4，R 5，R 6和R 7各自独立地为H，R 8或R 9; 每个R 8独立地是烃基; 并且每个R 9独立地为卤素，NO 2，烷氧基，CN，CF 3，SO 3 H，SO 2 NR 10 R 11，SO 2 R 12，NR 13 R 14（CH 2）a COOR 15，（CH 2）b CONR 16 R 17，（CH 2）c COR 18或（CH 2） a，b，c和d各自独立地为0，1 2 3或4; R 10-18各自独立地为H或烷基; 条件是当R1和R2都是H时，Z1是CH; 或Z2为N; 或Z 1为CH，Z 2为N; 并且其中所述化合物不是4-（4,5-二甲基噻唑-2-基）-N-（3,4,5-三甲氧基苯基）-2-嘧啶胺或4-（5-（2-羟乙基）-4-甲基噻唑-2-基） 吡啶-2-基）N-（3,4,5-三甲氧基苯基）-2-嘧啶胺。 其它方面涉及式（I）化合物在制备用于治疗选自增殖性病症，病毒病症，CNS病症，糖尿病，中风或脱发的一种或多种病症的药物中的用途。