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16 条记录 (耗时 0.022 秒)

    Benzthiazole-3 oxides useful for the treatment of proliferative disorders
    1.
    发明申请
    Benzthiazole-3 oxides useful for the treatment of proliferative disorders 审中-公开

    公开(公告)号：US20060040997A1

    公开(公告)日：2006-02-23

    申请号：US11192893

    申请日：2005-07-28

    申请人： Campbell McInnes ,  Christopher Meades ,  Mokdad Mezna ,  Peter Fischer

    发明人： Campbell McInnes ,  Christopher Meades ,  Mokdad Mezna ,  Peter Fischer

    IPC分类号： A61K31/428

    CPC分类号： C07D277/68 ,  A61K31/428 ,  Y02A50/411

    摘要： The present invention relates to the use of a compound of formula I, or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, and R4 are each independently H, NO2, CF3, SCF3, CN, halo, OH, OR6, NH2, NHR6, NR6R7, N+R6R7R8, COOH, COOR6, CONH2, CONHR6, CONR6R7, COH, COR6, SR6, SOR6, SO2R6, SO2OH, SO2OR6, SO2NH2, SO2NHR6, SO2NR6R7, alkyl, cycloalkyl, cycloheteroalkyl, aryl, or heteroaryl, with the proviso that at least one of R1, R2, R3, and R4 is other than H; or R1 and R2, R2 and R3, or R3 and R4, may together form part of a fused or unfused saturated or unsaturated ring system, optionally containing up to two heteroatoms selected from N, O, and S; R5 is OH, OR9, CN, CONH2, CONHNH2, CONHOH, CONHR9, CONR9R10, NH2, NHR9, or NR9R10; each R6, R7 and R8 is independently hydrocarbyl, or two of R6, R7 and R8 together form part of a saturated or unsaturated ring system, optionally containing up to two heteroatoms selected from N, O, and S; each R9 and R10 is independently hydrocarbyl, or R9 and R10 together form part of a saturated or unsaturated ring system, optionally containing up to two heteroatoms selected from N, O, and S; in the preparation of a medicament for treating a proliferative disorder.

    Pyridinylamino-pyrimidine derivatives as protein kinase inhibitors
    7.
    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
    8.
    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.

    Therapeutic applications of 2-substituted 4-heteroarylpyrimidines
    10.
    发明申请
    Therapeutic applications of 2-substituted 4-heteroarylpyrimidines 审中-公开

    公开(公告)号：US20050282843A1

    公开(公告)日：2005-12-22

    申请号：US11140136

    申请日：2005-05-26

    申请人： Shudong Wang ,  Christopher Meades ,  Gavin Wood ,  Kenneth Duncan ,  Daniella Zheleva ,  Peter Fischer

    发明人： Shudong Wang ,  Christopher Meades ,  Gavin Wood ,  Kenneth Duncan ,  Daniella Zheleva ,  Peter Fischer

    IPC分类号： A61K31/506 ,  A61P5/48 ,  A61P9/00 ,  A61P17/14 ,  A61P25/00

    CPC分类号： A61K31/506

    摘要： The present invention relates to the use of a compound of formula I, or a pharmaceutically acceptable salt thereof, wherein (A) one of X and Y is S, and the other is N; or one of X and Y is NH or N—R5, and the other is C—R6; “a” is a single bond; “b”, “c”, “d”, “e” and “f” are single or double bonds so as to form a heteroaryl ring; R1 is is R7 with the proviso that R1 is other than H or Me; or (B) one of X and Y is S, and the other is NH or N—R5; “a” and “d” are each double bonds; “b”, “c”, “e” and “f” are each single bonds; R1 is oxo; and R2, R3, R4, R5, and R6 are each independently H or R7; R7 is a group (CH2)n—R8, wherein n is 0, 1, 2, 3 or 4 and wherein R8 is selected from alkyl, aryl, heteroaryl, heterocycloalkyl, F, Cl, Br, I, CF3, NO2, CN, OH, O-alkyl, O-aryl, O-heteroaryl, O-heterocycloalkyl, CO-alkyl, CO-aryl, CO-heteroaryl, CO-heterocycloalkyl, COO-alkyl, NH2, NH-alkyl, NH-aryl, N(alkyl)2, NH-heteroaryl, NH-heterocycloalkyl, COOH, CONH2, CONH-alkyl, CON(alkyl)2, CONH-aryl, CONH-heteroaryl, CONH-heterocycloalkyl, SO3H, SO2-alkyl, SO2-aryl, SO2-heteroaryl, SO2-heterocycloalkyl, SO2NH2, SO2NH-alkyl, SO2N(alkyl)2, SO2NH-aryl, SO2NH-heteroaryl, or SO2NH-heterocycloalkyl, wherein said alkyl, aryl, heteroaryl, and heterocycloalkyl groups are optionally substituted with one or more groups selected from halogeno, NO2, OH, O-methyl, NH2, COOH, CONH2 and CF3; in the preparation of a medicament for treating diabetes. The compounds of the invention also have applications in the treatment of CNS disorders, alopecia, cardiovascular disorders and stroke.