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    THIOPHENE AMIDE COMPOUNDS FOR USE IN THE TREATMENT OR PROPHYLAXIS OF CANCERS
    52.
    发明申请
    THIOPHENE AMIDE COMPOUNDS FOR USE IN THE TREATMENT OR PROPHYLAXIS OF CANCERS 审中-公开
    用于治疗或预防癌症的硫胺酰胺化合物

    公开(公告)号：WO2006040569A8

    公开(公告)日：2007-04-26

    申请号：PCT/GB2005003957

    申请日：2005-10-14

    Applicant: ASTEX THERAPEUTICS LTD ,  GILL ADRIAN LIAM ,  LYONS JOHN FRANCIS ,  THOMPSON NEIL THOMAS

    Inventor： GILL ADRIAN LIAM ,  LYONS JOHN FRANCIS ,  THOMPSON NEIL THOMAS

    IPC: A61K31/5386 ,  A61K31/4155 ,  A61K31/4439 ,  A61K31/496 ,  A61K31/5377 ,  A61P35/00

    CPC classification number: A61K31/4155 ,  A61K31/4439 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/5386

    Abstract: The invention provides the use of a compound for the manufacture of a medicament for the prophylaxis or treatment of a cancer or a para-neoplastic effect associated with a cancer, the para-neoplastic effect being other than cachexia, and the compound being a compound of the formula (I), or a salt, solvate or N-oxide thereof, wherein: R 1 and R 2 are the same or different and each is selected from hydrogen, C 1-4 hydrocarbyl, halogen and cyano; X is selected from C=O, C=S, C(=O)NH, C(=S)NH, C(=O)O, C(=O)S, C(=S)O and C(=S)S; R 3 is an aryl or heteroaryl group of 5 to 12 ring members optionally substituted by one or more substituent groups R 7 wherein R 7 is as defined in the claims; R 4 is a group YR 5 or a group R 6 ; Y is NH, O or S; R 5 is selected from (a) optionally substituted carbocyclic and heterocyclic groups having from 3 to 12 ring members; and (b) optionally substituted C 1-8 hydrocarbyl 20 groups; and R 6 is an optionally substituted heterocyclic group having from 4 to 12 ring members and containing at least one ring nitrogen atom through which R 6 is linked to the adjacent carbonyl group.

    Abstract translation: 本发明提供化合物在制备用于预防或治疗与癌症相关的癌症或副肿瘤作用的药物中的用途，所述副肿瘤作用不是恶病质，所述化合物是化合物 式（I）或其盐，溶剂化物或N-氧化物，其中：R 1和R 2相同或不同，各自选自氢， C 1-4烃基，卤素和氰基; X选自C = O，C = S，C（= O）NH，C（= S）NH，C（= O）O，C（= O）S，C（= S）O和C（= S）S; R 3是任选被一个或多个取代基R 7取代的5至12个环成员的芳基或杂芳基，其中R 7为 在权利要求中限定; R 4是基团YR 5或基团R 6; Y是NH，O或S; R 5选自（a）具有3-12个环成员的任选取代的碳环和杂环基; 和（b）任选取代的C 1-8烃基20基团; 并且R 6是具有4-12个环成员并且含有至少一个环氮原子的任选取代的杂环基，R 6通过该环氮原子与相邻的羰基连接。

    COMBINATIONS
    55.
    发明申请
    COMBINATIONS 审中-公开
    组合

    公开(公告)号：WO2015144804A1

    公开(公告)日：2015-10-01

    申请号：PCT/EP2015/056512

    申请日：2015-03-26

    Applicant: ASTEX THERAPEUTICS LTD

    Inventor： JOVCHEVA, Eleonora ,  PERERA, Timothy Pietro Suren

    IPC: A61K31/498 ,  A61K31/4985 ,  A61K31/5025 ,  A61P35/00

    CPC classification number: A61K31/4985 ,  A61K31/498 ,  A61K31/5025 ,  A61K45/06 ,  A61K2300/00

    Abstract: The invention relates to a combination of a first compound selected from N-(3,5-dimethoxyphenyl)-N'-(1-methylethyl)-N-[3-(1-methyl-1H-pyrazol-4-yl)quinoxalin-6-yl]ethane-1,2-diamine or a pharmaceutically acceptable salt thereof or a solvate thereof, and N-(2-fluoro-3,5-dimethoxyphenyl)-N-(1H-imidazol-2-ylmethyl)-3-(1-methyl-1H-pyrazol-4-yl)pyrido[2,3-b]pyrazin-6-amine or a pharmaceutically acceptable salt thereof or a solvate thereof; and a second compound which is a cMet inhibitor. The combination is for use in the treatment of a proliferative disorder, in particular for use in the treatment of cancer. The FGFR inhibitor (N-(3,5-dimethoxyphenyl)-N'-(1-methylethyl)-N-[3-(1-methyl-1H-pyrazol-4-yl)quinoxalin-6-yl]ethane-1,2-diamine or a pharmaceutically acceptable salt thereof or a solvate thereof, and N-(2-fluoro-3,5-dimethoxyphenyl)-N-(1H-imidazol-2-ylmethyl)-3-(1-methyl-1H-pyrazol-4-yl)pyrido[2,3-b]pyrazin-6-amine or a pharmaceutically acceptable salt thereof or a solvate thereof) and the cMet inhibitor can be administered simultaneously, separately or sequentially. The invention further relates to a pharmaceutical composition comprising a pharmaceutically acceptable carrier and a combination according to the invention.

    Abstract translation: 本发明涉及选自N-（3,5-二甲氧基苯基）-N' - （1-甲基乙基）-N- [3-（1-甲基-1H-吡唑-4-基）喹喔啉 -6-基]乙烷-1,2-二胺或其药学上可接受的盐或其溶剂化物，和N-（2-氟-3,5-二甲氧基苯基）-N-（1H-咪唑-2-基甲基） 3-（1-甲基-1H-吡唑-4-基）吡啶并[2,3-b]吡嗪-6-胺或其药学上可接受的盐或其溶剂合物; 和作为cMet抑制剂的第二化合物。 该组合用于治疗增殖性疾病，特别是用于治疗癌症。 FGFR抑制剂（N-（3,5-二甲氧基苯基）-N' - （1-甲基乙基）-N- [3-（1-甲基-1H-吡唑-4-基）喹喔啉-6-基]乙烷-1 ，2-二胺或其药学上可接受的盐或其溶剂合物，和N-（2-氟-3,5-二甲氧基苯基）-N-（1H-咪唑-2-基甲基）-3-（1-甲基-1H- - 吡唑-4-基）吡啶并[2,3-b]吡嗪-6-胺或其药学上可接受的盐或其溶剂化物），cMet抑制剂可以同时，分开或依次施用。 本发明还涉及包含药学上可接受的载体和根据本发明的组合的药物组合物。

    PURINE AND DEAZAPURINE DERIVATIVES AS PHARMACEUTICAL COMPOUNDS
    59.
    发明申请
    PURINE AND DEAZAPURINE DERIVATIVES AS PHARMACEUTICAL COMPOUNDS 审中-公开
    作为药物化合物的嘌呤和多巴林衍生物

    公开(公告)号：WO2007125321A3

    公开(公告)日：2007-12-27

    申请号：PCT/GB2007001518

    申请日：2007-04-25

    Applicant: ASTEX THERAPEUTICS LTD ,  CANCER RES INST ROYAL ,  CANCER REC TECH LTD ,  DAVIES THOMAS GLANMOR ,  GARRETT MICHELLE DAWN ,  BOYLE ROBERT GEORGE ,  COLLINS IAN

    Inventor： DAVIES THOMAS GLANMOR ,  GARRETT MICHELLE DAWN ,  BOYLE ROBERT GEORGE ,  COLLINS IAN

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

    CPC classification number: C07D471/04 ,  C07D473/34 ,  C07D487/04

    Abstract: 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 a 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.

    Abstract translation: 本发明提供式（I）化合物或其盐，溶剂化物，互变异构体或N-氧化物，其中T为N或CR 5; J 1是N = C（R 6），（R 7）C = N， （R 8）NC（O），（R 8）2 CC（O），N = N或（R 7） ）C = C（R 6 ）; E是5或6个环成员的单环碳环或杂环基，杂环基含有至多3个选自O，N和S的杂原子; Q 1是一个键或饱和的C 1-3烃连接基团，连接基团中的一个碳原子任选地被氧或氮原子代替， 或相邻的一对碳原子可以被CONR Q或Q Q取代，其中R q是氢或甲基，或R 0 q是与R 1连接的C 1-4亚烷基链或Q 1的碳原子以形成环状的 部分; 并且其中连接基团Q 1的碳原子可以任选地具有一个或多个选自氟和羟基的取代基; Q 2是含有1至3个碳原子的键或饱和烃连接基团，其中连接基团中的一个碳原子可以任选被氧或氮原子取代; 并且其中所述连接基团的碳原子可以任选地具有一个或多个选自氟和羟基的取代基，条件是当存在的羟基不相对于G基团位于碳原子a时; 并且条件是当E是芳基或杂芳基时，则Q 2不是键; G是氢，NR 2 R 3，OH或SH，条件是当E是芳基或杂芳基且Q 2是键时，则G 是氢; R 1是氢或芳基或杂芳基，条件是当R 1是氢并且G是NR 2 R 3 ，则Q 2是一个键; 和R 2，R 3，R 4，R 6和R 8， 如权利要求中所定义，其中所述化合物用于：（a）治疗或预防其中指示调节（例如抑制）ROCK激酶或蛋白激酶P70S6K的疾病或病症; 和/或（b）治疗其中指示调节（例如抑制）ROCK激酶或蛋白激酶P70S6K的受试者或患者群体。

    PHARMACEUTICAL COMPOUNDS
    60.
    发明申请
    PHARMACEUTICAL COMPOUNDS 审中-公开
    药物化合物

    公开(公告)号：WO2007125315A3

    公开(公告)日：2007-12-27

    申请号：PCT/GB2007001510

    申请日：2007-04-25

    Applicant: ASTEX THERAPEUTICS LTD ,  CANCER RES INST ROYAL ,  CANCER REC TECH LTD ,  DAVIES THOMAS GLANMOR ,  GARRETT MICHELLE DAWN ,  BOYLE ROBERT GEORGE ,  COLLINS IAN

    Inventor： DAVIES THOMAS GLANMOR ,  GARRETT MICHELLE DAWN ,  BOYLE ROBERT GEORGE ,  COLLINS IAN

    IPC: C07D471/04 ,  A61K31/407 ,  A61K31/4188 ,  A61P9/00 ,  A61P35/00 ,  A61P37/00 ,  C07D473/00 ,  C07D473/34 ,  C07D487/04

    CPC classification number: C07D473/34 ,  C07D471/04 ,  C07D473/00 ,  C07D487/04

    Abstract: The invention provides a compound having 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 ); A is an optionally substituted saturated C 1-7 hydrocarbon linker group having a maximum chain length of 5 atoms extending between R 1 and NR 2 R 3 and a maximum chain length of 4 atoms extending between E and NR 2 R 3 , 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 CH 2 , O, S or NH and G is a C 1-4 alkylene chain wherein one of the carbon atoms is optionally replaced by O, S or NH; R 1 is hydrogen or an aryl or heteroaryl group; R 2 and R 3 are each hydrogen, optionally substituted C 1-4 hydrocarbyl or optionally substituted C 1-4 acyl; or NR 2 R 3 forms an imidazole group or a saturated monocyclic heterocyclic group having 4-7 ring members; or NR 2 R 3 and A together form a saturated monocyclic heterocyclic group having 4-7 ring members which is optionally substituted by C 1-4 alkyl; or NR 2 R 3 and the adjacent carbon atom of linker group A together form a cyano group; or R 1 , A and NR 2 R 3 together form a cyano group; and R 4 , R 5 , R 6 , R 7 and R 8 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.

    Abstract translation: 本发明提供具有式（I）的化合物或其盐，溶剂合物，互变异构体或N-氧化物，其中T是N或CR 5; J 1是N = C（R 6），（R 7）C = N， （R 8）NC（O），（R 8）2 CC（O），N = N或（R 7） ）C = C（R 6 ）; A是在R 1和R 2之间延伸的最大链长为5个原子的任选取代的饱和C 1 -C 7烃连接基团 连接基团中的一个碳原子是任选的，并且在E和NR 2 R 3之间延伸的最大链长为4个原子 用氧或氮代替; E是单环或双环碳环或杂环基或非环基XG，其中X是CH 2，O，S或NH，G是C 1-4亚烷基链 其中一个碳原子任选被O，S或NH取代; R 1是氢或芳基或杂芳基; R 2和R 3各自为氢，任选取代的C 1-4 - 烃基或任选取代的C 1-4 - >酰基; 或NR 2 R 3形成具有4-7个环成员的咪唑基或饱和单环杂环基; 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， 烷基; 或NR 2 R 3和连接基团A的相邻碳原子一起形成氰基; 或R 1，A和NR 2 R 3一起形成氰基; 和R 4，R 5，R 6，R 7和R 8， 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）治疗或预防其中调节（例如抑制）ROCK激酶或蛋白激酶p70S6K的疾病或病症 被指示 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。

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