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    PURINE AND DEAZAPURINE DERIVATIVES AS PHARMACEUTICAL COMPOUNDS
    1.
    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.

    PURINE AND DEAZAPURINE DERIVATIVES AS PHARMACEUTICAL COMPOUNDS
    5.
    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.

    PHARMACEUTICAL COMPOUNDS
    10.
    发明公开
    PHARMACEUTICAL COMPOUNDS 审中-公开
    药物化合物

    公开(公告)号：EP2016077A2

    公开(公告)日：2009-01-21

    申请号：EP07732548.8

    申请日：2007-04-25

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

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

    IPC分类号： C07D471/04 ,  C07D473/00 ,  C07D473/34 ,  C07D487/04 ,  A61K31/407 ,  A61K31/4188

    CPC分类号： C07D473/34 ,  C07D471/04 ,  C07D473/00 ,  C07D487/04

    摘要： The invention provides a compound having 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); A is an optionally substituted saturated C1-7 hydrocarbon linker group having a maximum chain length of 5 atoms extending between R1 and NR2R3 and a maximum chain length of 4 atoms extending between E and NR2R3, one of the carbon atoms in the linker group being optionally replaced by oxygen or nitrogen; E is a monocyclic or bicyclic carbocyclic or heterocyclic group or an acyclic group X-G wherein X is CH2, O, S or NH and G is a C1-4 alkylene chain wherein one of the carbon atoms is optionally replaced by O, S or NH; R1 is hydrogen or an aryl or heteroaryl group; R2 and R3 are each hydrogen, optionally substituted C1-4 hydrocarbyl or optionally substituted C1-4 acyl; or NR2R3 forms an imidazole group or a saturated monocyclic heterocyclic group having 4-7 ring members; or NR2R3 and A together form a saturated monocyclic heterocyclic group having 4-7 ring members which is optionally substituted by C1-4 alkyl; or NR2R3 and the adjacent carbon atom of linker group A together form a cyano group; or R1, A and NR2R3 together form a cyano group; and R4, R5, R6, R7 and R8 are each independently selected from hydrogen and various substituents 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.

    摘要翻译： 本发明提供了具有式（I）的化合物：或其盐，溶剂化物，互变异构体或N-氧化物，其中T是N或CR 5; （R6），（R7）C = N，（R8）N-C（O），（R8）2C-C（O），N = N或（R7）C = C（R6）。 A是任选取代的饱和C1-7烃连接基团，其具有在R1和NR2R3之间延伸的5个原子的最大链长和在E和NR2R3之间延伸的4个原子的最大链长，连接基团中的一个碳原子任选地 被氧或氮取代; E为单环或双环碳环或杂环基团或无环基团X-G，其中X为CH2，O，S或NH，G为C1-4亚烷基链，其中一个碳原子任选被O，S或NH替代; R1是氢或芳基或杂芳基; R2和R3各自为氢，任选取代的C1-4烃基或任选取代的C1-4酰基; 或NR 2 R 3形成咪唑基或具有4-7个环成员的饱和单环杂环基; 或NR 2 R 3和A一起形成具有4-7个环成员的饱和单环杂环基，其任选被C 1-4烷基取代; 或NR 2 R 3和接头基团A的相邻碳原子一起形成氰基; 或R1，A和NR2R3一起形成氰基; 和R4，R5，R6，R7和R8各自独立地选自氢和权利要求中定义的各种取代基，其中所述化合物用于：（a）治疗或预防疾病或病症，其中调节 指出了ROCK激酶或蛋白激酶p70S6K的抑制作用; 和/或（b）治疗其中指示ROCK激酶或蛋白激酶p70S6K的调节（例如抑制）的受试者或患者群体。