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    PYRROLOPYRIMIDINES AND USED AS KINASE INHIBITORS
    2.
    发明申请
    PYRROLOPYRIMIDINES AND USED AS KINASE INHIBITORS 审中-公开
    吡咯并嘧啶并用作激酶抑制剂

    公开(公告)号：US20120088753A1

    公开(公告)日：2012-04-12

    申请号：US13254355

    申请日：2010-03-04

    申请人： Edward Giles Mciver ,  Joanne HOUGH ,  Joanne Hough

    发明人： Edward Giles Mciver ,  Joanne HOUGH ,  Joanne Hough

    IPC分类号： A61K31/551 ,  A61K31/5377 ,  A61K31/496 ,  A61K31/519 ,  C07D487/04 ,  A61P29/00 ,  A61P35/00 ,  A61P19/02 ,  A61P17/06 ,  A61P9/00 ,  A61P9/10 ,  C12Q1/48 ,  A61P25/28

    CPC分类号： C07D487/04

    摘要： The invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or ester thereof, wherein: R1 is —NR7(CO)R11; R2 is aryl, heteroaryl, fused aryl-C3-6-heterocycloalkyl or fused heteroaryl-C3-6-heterocycloalkyl, each of which is optionally substituted; each R7 is selected from hydrogen, C1-6-alkyl and C3-7-cycloalkyl, wherein said C1-6-alkyl is optionally substituted by one or more halogens; each R11 is independently selected from C1-6-alkyl, C3-7-cycloalkyl, C1-6alkyl-C3-7-cycloalkyl, Ĉ-heterocycloalkyl, aryl and heteroaryl, each of which may be optionally substituted. Further aspects of the invention relate to pharmaceutical compositions comprising the same, and methods for treating or preventing a disorder selected from cancer, septic shock, Primary open Angle Glaucoma (POAG), hyperplasia, rheumatoid arthritis, psoriasis, artherosclerosis, retinopathy, osteoarthritis, endometriosis, chronic inflammation and Alzheimer's disease. Another aspect of the invention relates to the use of a compound as described above in the preparation of a medicament for the prevention or treatment of a disorder caused by, associated with or accompanied by any abnormal kinase activity, wherein the kinase is selected from TBK1, ERK8, CDK2, MARK3, YES1, VEG-FR, IKKepsilon and combinations thereof.

    摘要翻译： 本发明涉及式（I）化合物或其药学上可接受的盐或酯，其中：R 1是-NR 7（CO）R 11; R 2是芳基，杂芳基，稠合的芳基-C 3-6 - 杂环烷基或稠合的杂芳基-C 3-6 - 杂环烷基，其各自任选被取代; 每个R 7选自氢，C 1-6 - 烷基和C 3-7 - 环烷基，其中所述C 1-6 - 烷基任选被一个或多个卤素取代; 每个R 11独立地选自C 1-6 - 烷基，C 3-7 - 环烷基，C 1-6烷基-C 3-7 - 环烷基，杂环烷基，芳基和杂芳基，其各自可以任选地被取代。 本发明的其它方面涉及包含其的药物组合物，以及用于治疗或预防选自癌症，败血性休克，原发性开角型青光眼（POAG），增生，类风湿性关节炎，牛皮癣，动脉粥样硬化，视网膜病，骨关节炎，子宫内膜异位症 ，慢性炎症和阿尔茨海默病。 本发明的另一方面涉及如上所述的化合物在制备用于预防或治疗由任何异常激酶活性引起或伴随任何异常激酶活性引起的病症的药物中的用途，其中所述激酶选自TBK1， ERK8，CDK2，MARK3，YES1，VEG-FR，IKKepsilon及其组合。

    COMPOUNDS
    5.
    发明申请
    COMPOUNDS 审中-公开

    公开(公告)号：US20100317646A1

    公开(公告)日：2010-12-16

    申请号：US12727754

    申请日：2010-03-19

    申请人： Edward Giles Mciver ,  Ela Smiljanic ,  Denise Jamilla Harding ,  Joanne Hough

    发明人： Edward Giles Mciver ,  Ela Smiljanic ,  Denise Jamilla Harding ,  Joanne Hough

    IPC分类号： A61K31/437 ,  C07D471/04 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/4725 ,  A61K31/497 ,  A61K31/538 ,  A61K31/498 ,  A61K31/506 ,  A61P25/28 ,  A61P35/00 ,  A61P25/16

    CPC分类号： C07D471/04

    摘要： A compound of formula I, or a pharmaceutically acceptable salt or ester thereof, wherein R1 is selected from: aryl; heteroaryl; —NHR3; fused aryl-C4-7-heterocycloalkyl; —CONR4R5; —NHCOR6; —C3-7-cycloalkyl; —O—C3-7-cycloalkyl; —NR3R6; and optionally substituted —C1-6 alkyl; wherein said aryl, heteroaryl, fused aryl-C4-7-heterocycloalkyl and C4-7-heterocycloalkyl are each optionally substituted; R2 is selected from hydrogen, aryl, C1-6-alkyl, C2-6-alkenyl, C3-7-cycloalkyl, heteroaryl, C4-7 heterocycloalkyl and halogen, wherein said C1-6-alkyl, C2-6-alkenyl, aryl, heteroaryl and C4-7-heterocycloalkyl are each optionally substituted; R3 is selected from aryl, heteroaryl, C4-7-heterocycloalkyl, C3-7-cycloalkyl, fused aryl-C4-7-heterocycloalkyl and C1-6-alkyl, each of which is optionally substituted; R4 and R5 are each independently hydrogen, or optionally substituted C3-7-cycloalkyl, aryl, heteroaryl, C1-6-alkyl or C3-6-heterocycloalkyl; or R4 and R5 together with the N to which they are attached form a C3-6-heterocycloalkyl ring; each R6 is independently selected from C1-6-alkyl, C3-7 cycloalkyl, C4-7-heterocycloalkyl, aryl and heteroaryl, each of which is optionally substituted each R7 is selected from hydrogen, optionally substituted C1-6-alkyl and C3-7-cycloalkyl; each of R8 and R9 is independently hydrogen or optionally substituted C1-6-alkyl; or R8 and R9 together with the N to which they are attached form a C4-6-heterocycloalkyl; each R10 is selected from C3-7-cycloalkyl and optionally substituted C1-6-alkyl; each R11 is independently selected from C1-6-alkyl, C3-7-cycloalkyl, C1-6 alkyl-C3-7-cycloalkyl, C4-7-heterocycloalkyl, aryl and heteroaryl, each of which is optionally substituted; A is selected from halogen, —NR4SO2R5, —CN, —OR6, —NR4R5, —NR7R11, hydroxyl, —CF3, —CONR4R5, —NR4COR5, —NR7(CO)NR4R5, —NO2, —CO2H, —CO2R6, —SO2R6, —SO2NR4R5, —NR4COR5, —NR4COOR5, C1-6-alkyl and —COR6. Further aspects relate to pharmaceutical compositions, therapeutic uses and process for preparing compounds of formula I.

    PYRAZOLOPYRIDINES AS INHIBITORS OF THE KINASE LRRK2
    6.
    发明申请
    PYRAZOLOPYRIDINES AS INHIBITORS OF THE KINASE LRRK2 审中-公开

    公开(公告)号：US20130267513A1

    公开(公告)日：2013-10-10

    申请号：US13697878

    申请日：2011-05-16

    申请人： Brayn Chan ,  Anthony Estrada ,  Zachary Sweeney ,  Edward Giles Mciver ,  Stephen Lewis

    发明人： Brayn Chan ,  Anthony Estrada ,  Zachary Sweeney ,  Edward Giles Mciver ,  Stephen Lewis

    IPC分类号： A61K31/437 ,  A61K31/5377 ,  A61K31/506 ,  C07D471/04

    CPC分类号： A61K31/437 ,  A61K31/506 ,  A61K31/5377 ,  C07D401/04 ,  C07D471/04

    摘要： A compound of formula Ia or formula Ib, or a pharmaceutically acceptable salt or ester thereof, wherein R1 is selected from: aryl; heteroaryl; —NHR3; fused aryl-C4-7-heterocycloalkyl; —CONR4R5; —NHCOR6; —C3-7-cycloalkyl; -0-C3-7-cycloalkyl; —NR3R6; and optionally substituted —C1-6 alkyl; wherein said aryl, heteroaryl, fused aryl-C4-7-heterocycloalkyl and C4-7-heterocycloalkyl are each optionally substituted; Q is CN, halogen, or is selected from C1-6-alkyl, C3-7-cycloalkyl, heterocycloalkyl, aryl and heteroaryl, each of which is optionally substituted with one or more substituents A; R2 is selected from hydrogen, aryl, C1-6-alkyl, C2-6-alkenyl, C3-7-cycloalkyl, heteroaryl, C4-7-heterocycloalkyl and halogen, wherein said C1-6-alkyl, Cz-B-alkenyl, aryl, heteroaryl and C4-7-heterocycloalkyl are each optionally substituted; R3 is selected from aryl, heteroaryl, C4-7-heterocycloalkyl, C3-7-cycloalkyl, fused aryl-C-heterocycloalkyl and C1-6-alkyl, each of which is optionally substituted; R4 and R5 are each independently hydrogen, or optionally substituted C3-7-cycloalkyl, aryl, heteroaryl, C1-6-alkyl or C3-6-heterocycloalkyl; or R4 and R5 together with the N to which they are attached form a C3-6-heterocycloalkyl ring; each R6 is independently selected from C1-6-alkyl, C3-7-cycloalkyl, C-heterocycloalkyl, aryl and heteroaryl, each of which is optionally substituted; each R7 is selected from hydrogen, optionally substituted C1-6-alkyl and C3-7-cycloalkyl; each of R8 and R9 is independently hydrogen or optionally substituted C1-6-alkyl; or R8 and R9 together with the N to which they are attached form a C4-6-heterocycloalkyl; each R10 is selected from C3-7-cycloalkyl and optionally substituted C1-6-alkyl; each R11 is independently selected from C1-6-alkyl, C3-7-cycloalkyl, C1-6-alkyl-C3-7-cycloalkyl, C4-7-heterocycloalkyl, aryl and heteroaryl, each of which is optionally substituted; A is selected from halogen, —NR4S02R5, —CN, —OR6, —NR4R5, —NR7R11, hydroxyl, —CF3, —CONR4R5, —NR4COR5, —NR7(CO)NR4R5, —N02, —C02H, —C02R6, —S02R6, —S02NR4R5, —NR4COR5, —NR4COOR5, 6-alkyl and —COR6. Further aspects relate to pharmaceutical compositions, therapeutic uses and process for preparing compounds of formulae Ia and Ib.

    Amino-heterocycles as VR-1 antagonists for treating pain
    7.
    发明授权
    Amino-heterocycles as VR-1 antagonists for treating pain 失效

    公开(公告)号：US07442701B2

    公开(公告)日：2008-10-28

    申请号：US10534584

    申请日：2003-11-14

    申请人： Peter Blurton ,  Frank Burkamp ,  Stephen Robert Fletcher ,  Gregory John Hollingworth ,  A. Brian Jones ,  Edward Giles McIver ,  Christopher Richard Moyes ,  Lauren Rogers

    发明人： Peter Blurton ,  Frank Burkamp ,  Stephen Robert Fletcher ,  Gregory John Hollingworth ,  A. Brian Jones ,  Edward Giles McIver ,  Christopher Richard Moyes ,  Lauren Rogers

    IPC分类号： A61K31/44 ,  A61K31/497 ,  C07D403/02

    CPC分类号： C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  C07D471/04

    摘要： The present invention provides a compound of formula (I): wherein V represents NR5, O, S, SO or S(O)2; W and X each independently represent CH or N; Y represents N, CH or C—Ar2, with the proviso that at least one, but no more than two, of W, X and Y are N; Z represents CH or C—Ar2, with the proviso that when Y is N or CH then Z is C—Ar2, and with the further proviso that when Y is C—Ar2 then Z is CH; Ar1 represents a fused 9 or 10 membered heterobicyclic ring system containing one, two, three or four heteroatoms selected from nitrogen, oxygen and sulfur, wherein at least one of the rings in said ring system is aromatic; Ar2 represents an aromatic ring selected from phenyl, pyridyl, pyrimidinyl and pyridazinyl which is optionally fused and substituted; R1 represents halogen, hydroxy, oxo, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, haloC1-6alkyl, hydroxyC1-6alkyl, C1-6alkoxy, haloC1-6alkoxy, hydroxyC1-6alkoxy, C3-7cycloalkyl, C3-7cycloalkoxy, C3-5cycloalkylC1-4alkyl, cyano, nitro, SR6, SOR6, SO2R6, COR6, NR3COR6, CONR3R4, NR3SO2R6, SO2NR3R4, —(CH2)mcarboxy, esterified —(CH2)mcarboxy or —(CH2)mNR3R4; R2 represents hydrogen, halogen, hydroxy, C1-6alkyl, haloC1-6alkyl, C3-7cycloalkyl, C1-6alkoxy, haloC1-6alkoxy, unsubstituted phenyl or phenyl substituted with one or two groups selected from halogen, C1-6alkyl, haloC1-6alkyl, C3-7cycloalkyl, C1-6alkoxy or haloC1-6alkoxy; R3 and R4 are each independently hydrogen, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C3-7cycloalkyl or fluoroC1-6alkyl; or R3 and R4 and the nitrogen atom to which they are attached together form a heteroaliphatic ring of 4 to 7 ring atoms, optionally substituted by one or two groups selected from hydroxy or C1-4alkoxy, which ring may optionally contain as one of the said ring atoms an oxygen or a sulfur atom, S(O), S(O)2, or NR5; R5 represents hydrogen, C1-4alkyl, hydroxyC1-4alkyl or C1-4alkoxyC1-4alkyl; R6 represents hydrogen, C1-6alkyl, fluoroC1-6alkyl, C3-7cycloalkyl, unsubstituted phenyl, or phenyl substituted with one or two groups selected from halogen, C1-6alkyl, haloC1-6alkyl, C3-7cycloalkyl, C1-6alkoxy or haloC1-6alkoxy; m is either zero or an integer from 1 to 4; n is either zero or an integer from 1 to 3; or a pharmaceutically acceptable salt, N-oxide or a prodrug thereof; a pharmaceutical composition comprising it; its use in methods of treatment; use of it for the manufacture of a medicament for treating VR-1 related conditions such as those in which pain and/or inflammation predominate; and methods of treatment using it.

    Compound
    10.
    发明申请
    Compound 审中-公开
    复合

    公开(公告)号：US20100056524A1

    公开(公告)日：2010-03-04

    申请号：US12384477

    申请日：2009-04-02

    申请人： Edward Giles Mciver ,  Justin Stephen Bryans ,  Ela Smiljanic ,  Stephen John Lewis ,  Joanne Hough ,  Thomas Drake

    发明人： Edward Giles Mciver ,  Justin Stephen Bryans ,  Ela Smiljanic ,  Stephen John Lewis ,  Joanne Hough ,  Thomas Drake

    IPC分类号： A61K31/5377 ,  C07D239/02 ,  C07D403/12 ,  C07D413/12 ,  A61K31/505 ,  A61K31/506

    CPC分类号： C07D239/48 ,  C07D401/12 ,  C07D403/12 ,  C07D407/12 ,  C07D407/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D471/04

    摘要： A first aspect of the invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or ester thereof, wherein: R1 is C3-8-cycloalkyl; X is O, NR7 or C3-6-heterocycloalkyl; R2 is aryl, heteroaryl, fused or unfused aryl-C3-6-heterocycloalkyl or fused or unfused heteroaryl-C3-6-heterocycloalkyl, each of which is optionally substituted by one or more substitutents selected from aryl, heteroaryl, C1-6-alkyl, C3-7-cycloalkyl and a group A, wherein said C1-6-alkyl group is optionally substituted by one or more substituents selected from aryl, heteroaryl, R10 and a group A, said heteroaryl group is optionally substituted by one or more R10 groups; and wherein said C3-6-heterocycloalkyl group optionally contains one or more groups selected from oxygen, sulfur, nitrogen and CO; R3 is C1-6-alkyl optionally substituted by one or more substituents selected from aryl, heteroaryl, —NR4R5, —OR6, —NR7(CO)R6, —NR7(CO)NR4R5, —NR7SO2R6, —NR7COOR7, —CONR4R5, C3-6-heterocycloalkyl and wherein R4-7 and A are as defined in the claims.Further aspects relate to the use of said compounds in the treatment of various therapeutic disorders, and more particularly as inhibitors of one or more kinases.

    摘要翻译： 本发明的第一方面涉及式（I）化合物或其药学上可接受的盐或酯，其中：R 1为C 3-8 - 环烷基; X是O，NR 7或C 3-6 - 杂环烷基; R 2是芳基，杂芳基，稠合或未稠合的芳基-C 3-6 - 杂环烷基或稠合或未稠合的杂芳基-C 3-6 - 杂环烷基，其各自任选被一个或多个选自芳基，杂芳基，C 1-6 - 烷基 C 3-7 - 环烷基和基团A，其中所述C 1-6 - 烷基任选被一个或多个选自芳基，杂芳基，R 10和A基团的取代基取代，所述杂芳基任选地被一个或多个R 10 团体 并且其中所述C 3-6杂环烷基任选地含有一个或多个选自氧，硫，氮和CO的基团; R 3是任选被一个或多个选自芳基，杂芳基，-NR 4 R 5，-OR 6，-NR 7（CO）R 6，-NR 7（CO）NR 4 R 5，-NR 7 SO 2 R 6，-NR 7 COOR 7，-CONR 4 R 5，C 3 -6-杂环烷基，其中R 4-7和A如权利要求中所定义。 其它方面涉及所述化合物在治疗各种治疗性疾病中的用途，更具体地涉及一种或多种激酶的抑制剂。