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    PURINE AND DEAZAPURINE DERIVATIVES AS PHARMACEUTICAL COMPOUNDS
    4.
    发明公开
    PURINE AND DEAZAPURINE DERIVATIVES AS PHARMACEUTICAL COMPOUNDS 审中-公开
    嘌呤和脱氮衍生物作为药物化合物

    公开(公告)号：EP2043655A2

    公开(公告)日：2009-04-08

    申请号：EP07732555.3

    申请日：2007-04-25

    申请人： Astex Therapeutics Limited ,  The Institute of Cancer Research: Royal Cancer Hospital ,  Cancer Research Technology Limited

    发明人： DAVIES, Thomas, Glanmor ,  GARRETT, Michelle, Dawn ,  BOYLE, Robert, George ,  COLLINS, Ian

    IPC分类号： A61K31/52 ,  A61K31/522 ,  A61K31/4523 ,  A61K31/519 ,  A61P29/00 ,  A61P35/00 ,  A61P25/00 ,  A61P37/00 ,  C07D471/04 ,  C07D473/34 ,  C07D487/04

    CPC分类号： C07D471/04 ,  C07D473/34 ,  C07D487/04

    摘要： The invention provides a compound of the formula (I) or salts, solvates, tautomers or N-oxides thereof, wherein T is N or CR5; J1-J2 is N═C(R6), (R7)C═N, (R8)N—C(O), (R8)2C—C(O), N═N or (R7)C═C(R6); E is a monocyclic carbocyclic or heterocyclic group of 5 or 6 ring members, the heterocyclic group containing up to 3 heteroatoms selected from O, N and S; Q1 is a bond or a saturated C1-3 hydrocarbon linker group, one of the carbon atoms in the linker group being optionally be replaced by an oxygen or nitrogen atom, or an adjacent pair of carbon atoms may be replaced by CONRq or NRqCO where Rq is hydrogen or methyl, or Rq is a C1-4alkylene chain linked to R1 or a carbon atom of Q1 to form a cyclic moiety; and wherein the carbon atoms of the linker group Q1 may optionally bear one or more substituents selected from fluorine and hydroxy; Q2 is a bond or a saturated hydrocarbon linker group containing from 1 to 3 carbon atoms, wherein one of the carbon atoms in the linker group may optionally be replaced by an oxygen or nitrogen atom; and wherein the carbon atoms of the linker group may optionally bear one or more substituents selected from fluorine and hydroxy, provided that the hydroxy group when present is not located at a carbon atom α with respect to the G group; and provided that when E is aryl or heteroaryl, then Q2 is other than a bond; G is hydrogen, NR2R3, OH or SH provided that when E is aryl or heteroaryl and Q2 is a bond, then G is hydrogen; R1 is hydrogen or an aryl or heteroaryl group, with the proviso that when R1 is hydrogen and G is NR2R3, then Q2 is a bond; and R2, R3R4, R6 and R8 are as defined in the claims, wherein the compound is for use in: (a) the treatment or prophylaxis of a disease or condition in which the modulation (e.g. inhibition) of ROCK kinase or protein kinase P70S6K is indicated; and/or (b) the treatment of a subject or patient population in which the modulation (e.g. inhibition) of ROCK kinase or protein kinase P70S6K is indicated.

    PURINE AND DEAZAPURINE DERIVATIVES AS PHARMACEUTICAL COMPOUNDS
    5.
    发明公开
    PURINE AND DEAZAPURINE DERIVATIVES AS PHARMACEUTICAL COMPOUNDS 审中-公开

    公开(公告)号：EP3421471A1

    公开(公告)日：2019-01-02

    申请号：EP18182786.6

    申请日：2007-04-25

    申请人： Astex Therapeutics Limited ,  The Institute of Cancer Research: Royal Cancer Hospital ,  Cancer Research Technology Limited

    发明人： DAVIES, Thomas, Glanmor ,  BOYLE, Robert, George ,  COLLINS, Ian

    IPC分类号： C07D471/04 ,  C07D473/34 ,  C07D487/04 ,  A61K31/4523 ,  A61K31/519 ,  A61K31/52 ,  A61K31/522 ,  A61P35/00

    摘要： The invention provides a compound of the formula (I):

    or salts, solvates, tautomers or N-oxides thereof, wherein T is N or CR 5 ; J 1 -J 2 is N=C(R 6 ), (R 7 )C=N, (R 8 )N-C(O), (R 8 ) 2 C-C(O), N=N or (R 7 )C=C(R 6 ); E is a monocyclic carbocyclic or heterocyclic group of 5 or 6 ring members, the heterocyclic group containing up to 3 heteroatoms selected from O, N and S; Q 1 is a bond or a saturated C 1-3 hydrocarbon linker group, one of the carbon atoms in the linker group being optionally be replaced by an oxygen or nitrogen atom, or an adjacent pair of carbon atoms may be replaced by CONR q or NR q CO where R q is hydrogen or methyl, or R q is a C 1-4 alkylene chain linked to R 1 or a carbon atom of Q 1 to form a cyclic moiety; and wherein the carbon atoms of the linker group Q 1 may optionally bear one or more substituents selected from fluorine and hydroxy; Q 2 is a bond or a saturated hydrocarbon linker group containing from 1 to 3 carbon atoms, wherein one of the carbon atoms in the linker group may optionally be replaced by an oxygen or nitrogen atom; and wherein the carbon atoms of the linker group may optionally bear one or more substituents selected from fluorine and hydroxy, provided that the hydroxy group when present is not located at a carbon atom α with respect to the G group; and provided that when E is aryl or heteroaryl, then Q 2 is other than a bond; G is hydrogen, NR 2 R 3 , OH or SH provided that when E is aryl or heteroaryl and Q 2 is a bond, then G is hydrogen;
    R 1 is hydrogen or an aryl or heteroaryl group, with the proviso that when R 1 is hydrogen and G is NR 2 R 3 , then Q 2 is a bond; and R 2 , R 3 , R 4 , R 6 and R 8 are as defined in the claims, wherein the compound is for use in: (a) the treatment or prophylaxis of a disease or condition in which the modulation (e.g. inhibition) of ROCK kinase or protein kinase P70S6K is indicated; and/or (b) the treatment of a subject or patient population in which the modulation (e.g. inhibition) of ROCK kinase or protein kinase P70S6K is indicated.