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29 条记录 (耗时 0.047 秒)

    PHARMACEUTICAL COMPOUNDS
    5.
    发明公开
    PHARMACEUTICAL COMPOUNDS 审中-公开
    药物化合物

    公开(公告)号：EP2013206A1

    公开(公告)日：2009-01-14

    申请号：EP07732554.6

    申请日：2007-04-25

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

    发明人： SAXTY, Gordon ,  VERDONK, Marinus, Leendert ,  CALDWELL, John ,  COLLINS, Ian ,  CHEUNG, Kwai-Ming ,  DA FONSECA MCHARDY, Tatiana, Faria

    IPC分类号： C07D471/04 ,  C07D495/04 ,  C07D498/04 ,  A61K31/506 ,  A61P35/00

    CPC分类号： C07D471/04 ,  C07D495/04

    摘要： Compounds of the formula (I), and salts, solvates, tautomers and N-oxide thereof; wherein TG is selected from groups (1) and (2): wherein the asterisk (*) represents the point of attachment of the group E to the group X; Rla is an optionally substituted aryl or heteroaryl group; Rlb is hydrogen or a group Rla; X is an optionally substituted bicyclic heterocyclic group having 8 to 12 ring members of which up to 5 are heteroatoms selected from O, N and S; and A, E, R2, R3, R4, Q1 and Q2 are as defined in the claims; provided that when E is aryl or heteroaryl, then Q2 is other than a bond; and further provided that the moiety (a) is other than a group (BG1) or (BG2); wherein (BGl) and (BG2) are each optionally substituted; T is N or CRZ; J1-J2 is selected from N=C(RZ), (RZ)C=N, (RZ)N-C(O), (RZ)2C-C(O), N=N and (RZ)C=C(R6); J4 -J3 is a group N=C(RZ) or a group (RZ)N-CO; and RZ is hydrogen or a substituent. The compounds of the formula (I) have PKA and PKB kinase inhibiting activity and are useful in the treatment of cancers.

    摘要翻译： 式（I）化合物及其盐，溶剂化物，互变异构体和N-氧化物; 其中TG选自组（1）和（2）：其中星号（*）表示基团E与基团X的连接点; R 1a是任选取代的芳基或杂芳基; R 1b是氢或基团R 1a; X是任选取代的具有8至12个环成员的双环杂环基团，其中至多5个是选自O，N和S的杂原子; 和A，E，R2，R3，R4，Q1和Q2如权利要求中所定义; 条件是当E是芳基或杂芳基时，则Q2不是键; 并进一步提供部分（a）不是基团（BG1）或（BG2）; 其中（BG1）和（BG2）各自任选被取代; T是N或CRZ; （RZ）C = N，（RZ）NC（O），（RZ）2C-C（O），N = N和（RZ）C = C（R 6） ）; J4-J3是基团N = C（RZ）或基团（RZ）N-CO; 并且RZ是氢或取代基。 式（I）化合物具有PKA和PKB激酶抑制活性并可用于治疗癌症。

    PHARMACEUTICAL COMPOUNDS
    6.
    发明公开
    PHARMACEUTICAL COMPOUNDS 审中-公开
    药物化合物

    公开(公告)号：EP1902032A1

    公开(公告)日：2008-03-26

    申请号：EP06755582.1

    申请日：2006-06-21

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

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

    IPC分类号： C07D231/12 ,  C07D401/10 ,  C07D403/10 ,  C07D403/12 ,  C07D401/04 ,  C07D413/10 ,  A61K31/415 ,  A61K31/4155 ,  A61P35/00 ,  A61P9/00 ,  A61P3/00 ,  A61P29/00

    CPC分类号： C07D401/14 ,  C07D231/12 ,  C07D401/04 ,  C07D401/10 ,  C07D403/10 ,  C07D403/12 ,  C07D413/10

    摘要： The invention provides compounds of the formula (I) having ROCK kinase and/or protein kinase p70S6K inhibiting activity: wherein A is a saturated hydrocarbon linker group containing from 1 to 7 carbon atoms, the 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, 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 A may optionally bear one or more substituents selected from oxo, fluorine and hydroxy, provided that the hydroxy group when present is not located at a carbon atom α with respect to the NR2R3 group and provided that the oxo group when present is located at a carbon atom α with respect to the NR2R3 group; E is a monocyclic or bicyclic carbocyclic or heterocyclic group; R1 is an aryl or heteroaryl group; and R2, R3, R4 and R5 are as defined in the claims.

    摘要翻译： 本发明提供了具有ROCK激酶和/或蛋白激酶p70S6K抑制活性的式（I）化合物：其中A是含有1至7个碳原子的饱和烃连接基团，连接基团具有5个原子的最大链长 在R1和NR2R3之间以及在E和NR2R3之间延伸的4个原子的最大链长，其中接头基团中的一个碳原子可以任选地被氧或氮原子替代; 并且其中连接基团A的碳原子可以任选地带有一个或多个选自氧代，氟和羟基的取代基，条件是存在的羟基相对于NR 2 R 3基团不位于碳原子α处，并且条件是 当存在时，氧代基团相对于NR 2 R 3基团位于碳原子α处; E是单环或双环碳环或杂环基团; R1是芳基或杂芳基; R2，R3，R4和R5如权利要求中所定义。

    PURINE AND DEAZAPURINE DERIVATIVES AS PHARMACEUTICAL COMPOUNDS
    7.
    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.