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    Imidazolyl-cyclic acetals
    2.
    发明授权
    Imidazolyl-cyclic acetals 有权
    咪唑基 - 环状缩醛

    公开(公告)号：US06602877B1

    公开(公告)日：2003-08-05

    申请号：US09456360

    申请日：1999-12-08

    申请人： Paul L. Bamborough ,  Alan J. Collis ,  Frank Halley ,  Richard A. Lewis ,  David J. Lythgoe ,  Jeffrey M. McKenna ,  Iain M. McLay ,  Barry Porter ,  Andrew J. Ratcliffe ,  Paul A. Wallace

    发明人： Paul L. Bamborough ,  Alan J. Collis ,  Frank Halley ,  Richard A. Lewis ,  David J. Lythgoe ,  Jeffrey M. McKenna ,  Iain M. McLay ,  Barry Porter ,  Andrew J. Ratcliffe ,  Paul A. Wallace

    IPC分类号： C07D23354

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/04 ,  C07D403/04 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D491/10 ,  C07D493/10

    摘要： Compounds of formula (I) are described in which R1 is optionally substituted heteroaryl; R2 is optionally substituted aryl or optionally substituted heteroaryl; R3 is a group —L1—R7 or —L2—R8 [where L1 is an optionally substituted alkylene linkage; R7 is hydrogen, aryl, cyano, cycloalkyl, heteroaryl, heterocycloalkyl, nitro, —S(O)nR9, —NHSO2R9, —C(═Z)OR10, —C(═Z)R10, —OR10, —N(R11)—C(═Z)R9, —NY1Y2, —SO2NY1Y2, —C(═Z)—NY1Y2, —N(R11)—C(═Z)—NY1Y2, —N(OR10)—C(═Z)—NY1Y2, —N(OR10)—C(═Z)R10, —C(═NOR10)R10, —C(═Z)NR10OR12, —N(R11)—C(═NR13)—NY1Y2 or —N(R11)—C(═Z)OR11; L2 is a direct bond or a straight- or branched-carbon chain comprising from 2 to about 6 carbon atoms and contains a double or triple carbon-carbon bond; and R8 is hydrogen, aryl, cycloalkenyl, cycloalkyl, heteroaryl or heterocycloalkyl]; R4 is a group —L3—R14 [where L3 is a direct bond or an optionally substituted alkylene linkage and R14 is hydrogen, alkyl, azido, hydroxy, alkoxy, aryl, arylalkyloxy, aryloxy, carboxy (or an acid bioisostere), cycloalkyloxy, heteroaryl, heteroarylalkyloxy, heteroaryloxy, heterocycloalkyl, heterocycloalkyloxy, nitro, —NY4Y5, —N(R10)—C(═Z)—R15; —N(R10)—C(═Z)—L4—R16, —NH—C(═Z)—NH—R15, —NH—C(═Z)—NH—L4—R16, —N(R10)—SO2—R15, —N(R10)—SO2—L4—R16, —S(O)nR9, —C(═Z)—NY4Y5 or —C(═Z)—OR9]; R5 is hydrogen, alkyl or hydroxyalkyl; or R4 and R5, when attached to the same carbon atom, may form with the said carbon atom a cycloalkyl, cycloalkenyl or heterocycloalkyl ring or a group C═CH2; R6 is hydrogen or alkyl; and m is zero or an integer 1 or 2; and N-oxides thereof, and their prodrugs; and pharmaceutically acceptable salts and solvates (e.g. hydrates) of compounds of formula (I) and N-oxides thereof, and their prodrugs. The compounds are TNF inhibitors and are useful as pharmaceuticals.

    摘要翻译： 描述式（I）的化合物，其中R 1是任选取代的杂芳基; R2是任选取代的芳基或任选取代的杂芳基; R3是基团-L1-R7或-L2-R8 [其中L1是任选取代的亚烷基键; R 7是氢，芳基，氰基，环烷基，杂芳基，杂环烷基，硝基，-S（O）n R 9，-NHSO 2 R 9，-C（= Z）OR 10，-C（= Z）R 10，-OR 10，-N（R 11） -C（= Z）R9，-NY1Y2，-SO2NY1Y2，-C（= Z）-NY1Y2，-N（R11）-C（= Z）-NY1Y2，-N（OR10）-C（= Z）-NY1Y2 ，-N（OR 10）-C（= Z）R 10，-C（= NOR 10）R 10，-C（= Z）NR 10 OR 12，-N（R 11）-C（= NR 13）-NY 1 Y 2或-N（R 11） C（= Z）OR 11; L2是直接键或包含2至约6个碳原子并含有双或三碳 - 碳键的直链或支链碳链; 和R8是氢，芳基，环烯基，环烷基，杂芳基或杂环烷基]; R4是基团-L3-R14 [其中L3是直接键或任选取代的亚烷基键，R 14是氢，烷基，叠氮基，羟基，烷氧基，芳基，芳基烷氧基，芳氧基，羧基（或酸式生物电子等排体） 杂芳基烷氧基，杂芳氧基，杂环烷基，杂环烷氧基，硝基，-NY 4 Y 5，-N（R 10）-C（= Z）-R 15; -N（R10）-C（= Z）-L4-R

    1-pyrazolo[4,3-c]isoquinoline derivatives, preparation thereof and therapeutic use thereof
    5.
    发明授权
    1-pyrazolo[4,3-c]isoquinoline derivatives, preparation thereof and therapeutic use thereof 有权
    1-吡唑并[4,3-c]异喹啉衍生物，其制备及其治疗用途

    公开(公告)号：US08461175B2

    公开(公告)日：2013-06-11

    申请号：US13265981

    申请日：2010-04-22

    申请人： Georges Delettre ,  Stéphanie Deprets ,  Frank Halley ,  Laurent Schio ,  Fabienne Thompson

    发明人： Georges Delettre ,  Stéphanie Deprets ,  Frank Halley ,  Laurent Schio ,  Fabienne Thompson

    IPC分类号： C07D471/04 ,  A61K31/4745 ,  A61P35/00

    CPC分类号： C07D471/04

    摘要： The invention relates to a compound of formula (I), where: R1 is a phenyl group optionally substituted by one or more halogen atoms; R2 is: a hydrogen atom or a halogen atom or a cyano group; a —C(═O)Y group where Y is a hydrogen atom, or a —NH2 or —OR3 group; a —C(═S)NH2 group; a —C(═NH)NH—OH group; a —CH2OH or —CH2F group; a —CH═N—OH group; a —CH═CH2 or —C═C—R3 group; a H or H R1 group being a hydrogen or (C1-C4)alkyl group; R3 is a hydrogen atom or (C1-C4)alkyl group; and R4 is a —NH2, (C1-C4)alkyl, (C1-C4)fluoroalkyl or (C3-C7)cycloalkyl group.

    摘要翻译： 本发明涉及式（I）化合物，其中：R 1是任选被一个或多个卤素原子取代的苯基; R2是：氢原子或卤素原子或氰基; Y为氢原子的-C（= O）Y基团，或-NH2或-OR3基团; -C（= S）NH 2基团; -C（= NH）NH-OH基团; -CH 2 OH或-CH 2 F基团; -CH = N-OH基团; -CH = CH 2或-C = C-R 3基团; H或H R 1基团为氢或（C 1 -C 4）烷基; R3是氢原子或（C1-C4）烷基; 并且R 4是-NH 2，（C 1 -C 4）烷基，（C 1 -C 4）氟烷基或（C 3 -C 7）环烷基。