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15 条记录 (耗时 0.056 秒)

    Substituted 4-phenyl-4-(1H-imidazol-2-yl)-piperidine derivatives and their use as selective non-peptide delta opioid agonists
    6.
    发明授权
    Substituted 4-phenyl-4-(1H-imidazol-2-yl)-piperidine derivatives and their use as selective non-peptide delta opioid agonists 有权
    取代的4-苯基-4-（1H-咪唑-2-基） - 哌啶衍生物及其作为选择性非肽δ阿片激动剂的用途

    公开(公告)号：US07282508B2

    公开(公告)日：2007-10-16

    申请号：US10491379

    申请日：2002-10-10

    申请人： Frans Eduard Janssens ,  Joseph Elisabeth Leenaerts ,  Francisco Javier Fernández-Gadea ,  Antonio Gómez-Sánchez ,  Theo Frans Meert

    发明人： Frans Eduard Janssens ,  Joseph Elisabeth Leenaerts ,  Francisco Javier Fernández-Gadea ,  Antonio Gómez-Sánchez ,  Theo Frans Meert

    IPC分类号： A61K31/445 ,  C07D401/00

    CPC分类号： C07D401/04 ,  C07D401/14 ,  C07D413/14 ,  C07D417/14

    摘要： The present invention relates to novel 4-phenyl-4-[1H-imidazol-2-yl]-piperidine derivatives according to Formula (I) the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the tautomeric forms thereof and the N-oxide forms thereof. In particular are claimed compounds according to Formula (I) in which A═B is C═O or SO2, X is a covalent bond, R1 is alkyloxy, alkyloxyalkyl, Ar or NR9R10, wherein R9 and R10 each independently are hydrogen or Ar; or A═B and R1 together form a benzoxazolyl radical; p is zero, R3 is benzyl optionally substituted with hydroxy, alkyl or alkyloxycarbonyl and R4 and R5 each are hydrogen. The invention also relates to processes for the preparation of the compounds according to the invention and their use in medicine, in particular as selective non-peptide δ-opioid agonists for use in the treatment of various pain conditions.

    摘要翻译： 本发明涉及式（I）的新的4-苯基-4- [1H-咪唑-2-基] - 哌啶衍生物，其药学上可接受的酸或碱加成盐，其立体化学异构形式，其互变异构体 及其N-氧化物形式。 特别是根据式（I）的化合物，其中AB是CO或SO 2，X是共价键，R 1是烷氧基，烷氧基烷基，Ar或NR 其中R 9和R 10各自独立地是氢或Ar;其中R 9和R 10各自独立地是氢或Ar; 或A-B和R 1一起形成苯并恶唑基; p为0，R 3为任选被羟基，烷基或烷氧基羰基取代的苄基，R 4和R 5各自为氢。 本发明还涉及根据本发明的化合物的制备方法及其在医学中的用途，特别是用于治疗各种疼痛病症的选择性非肽δ-阿片样物质激动剂。

    Substituted 4-phenyl-4-[1H-imidazol-2-yl]-piperidine derivatives for reducing ischaemic damage
    7.
    发明授权
    Substituted 4-phenyl-4-[1H-imidazol-2-yl]-piperidine derivatives for reducing ischaemic damage 有权
    取代的4-苯基-4- [1H-咪唑-2-基] - 哌啶衍生物，用于减少缺血性损伤

    公开(公告)号：US07390822B2

    公开(公告)日：2008-06-24

    申请号：US10492778

    申请日：2002-10-10

    申请人： Frans Eduard Janssens ,  Joseph Elisabeth Leenaerts ,  Francisco Javier Fernández-Gadea ,  Paul Joannes Ludovicus Herijgers ,  Theo Frans Meert ,  Antonio Gómez-Sánchez ,  Willem Flameng ,  Marcel J. M. Borgers

    发明人： Frans Eduard Janssens ,  Joseph Elisabeth Leenaerts ,  Francisco Javier Fernández-Gadea ,  Paul Joannes Ludovicus Herijgers ,  Theo Frans Meert ,  Antonio Gómez-Sánchez ,  Willem Flameng ,  Marcel J. M. Borgers

    IPC分类号： A61K31/445 ,  A61K31/454

    CPC分类号： A61K31/454

    摘要： The present invention relates to an agent for reducing ischaemic damage to an organ, in particular to a heart and a brain, pharmaceutical compositions comprising said agent and the use of said agent for the treatment of ischaemic diseases to the heart and the brain. The agent comprises a substituted 4-phenyl-4-[1H-imidazol-2-yl]-piperidine derivative according to Formula (I) the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the tautomeric forms thereof, the N-oxide forms thereof and the prodrugs thereof. In particular are claimed the compounds according to Formula (I) in which A=B is C═O or SO2, X is a covalent bond, R1 is alkyloxy, alkyloxyalkyl, Ar or NR9R10, wherein R9 and R10 each independently are hydrogen or Ar; or A=B and R1 together form a benzoxazolyl radical; p is zero, R3 is benzyl optionally substituted with hydroxy, alkyl or alkyloxycarbonyl and R4 and R5 each are hydrogen. The use of said agents has important clinical ramifications with regard to the reduction of ischaemic damage to an organ in a mammal, in particular to a heart and/or a brain, the prevention of coronary artery diseases in a mammal by inducing a cardioprotective effect and the treatment and prevention of stroke.

    摘要翻译： 本发明涉及用于减轻对器官特别是心脏和脑的缺血性损伤的药剂，包含所述药物的药物组合物和所述药物用于治疗心脏和脑部的缺血性疾病的用途。 该试剂包含根据式（I）的取代的4-苯基-4- [1H-咪唑-2-基] - 哌啶衍生物，其药学上可接受的酸或碱加成盐，其立体化学异构形式，其互变异构形式， 其N-氧化物形式及其前药。 特别要求保护的是根据式（I）的化合物，其中A = B是CO或SO 2，X是共价键，R 1是烷氧基，烷氧基烷基， Ar或NR 9 R 10，其中R 9和R 10各自独立地为氢或Ar; 或A = B和R 1一起形成苯并恶唑基; p为0，R 3为任选被羟基，烷基或烷氧基羰基取代的苄基，R 4和R 5各自为氢。 所述试剂的使用对于减少对哺乳动物，特别是心脏和/或脑的器官的缺血损伤，通过诱导心脏保护作用来预防哺乳动物的冠状动脉疾病，具有重要的临床后果，以及 治疗和预防中风。

    Method of using substituted tetracyclic tetrahydrofuran derivatives
    9.
    发明授权
    Method of using substituted tetracyclic tetrahydrofuran derivatives 有权
    使用取代四环四氢呋喃衍生物的方法

    公开(公告)号：US06194405B1

    公开(公告)日：2001-02-27

    申请号：US09533625

    申请日：2000-03-22

    申请人： Pilar Gil-Lopetegui ,  Francisco Javier Fernández-Gadea ,  Theo Frans Meert

    发明人： Pilar Gil-Lopetegui ,  Francisco Javier Fernández-Gadea ,  Theo Frans Meert

    IPC分类号： A01N4346

    CPC分类号： C07D493/04 ,  C07D307/93

    摘要： This invention concerns the compounds of formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts and the stereoisomeric forms thereof, wherein n is zero to 6; p and q are zero to 4; r is zero to 5; R1 and R2 each independently are hydrogen; optionally substituted C1-6alkyl; C1-6alkylcarbonyl; halomethylcarbonyl; or R1 and R2 taken together with the nitrogen atom to which they are attached may form a morpholinyl ring or an optionally substituted heterocycle; each R3 and R4 independently are halo, cyano, hydroxy, halomethyl, halomethoxy, carboxyl, nitro, amino, mono- or di(C1-6alkyl)amino, C1-6alkylcarbonylamino, aminosulfonyl, mono- or di(C1-6alkyl)aminosulfonyl, C1-6alkyl, C1-6alkyloxy, C1-6alkylcarbonyl, C1-6alkyloxycarbonyl; each R5 independently is C1-6alkyl, cyano or halomethyl; X is CR6R7, NR8, O, S, S(═O) or S(═O)2; aryl is optionally substituted phenyl; provided that the compound is other than (±)-3,3a,8,12b-tetrahydro-N-methyl-2H-dibenzo[3,4:6,7]-cyclohepta[1,2-b]-furan-2-methanamine oxalic acid. The compounds of formula (I) may be used as therapeutic agents in the treatment or the prevention of CNS disorders, cardiovascular disorders or gastrointestinal disorders.

    摘要翻译： 本发明涉及式（I）化合物，N-氧化物形式，其药学上可接受的加成盐和立体异构形式，其中n为0-6; p和q为零至4; r为0〜5; R1和R2各自独立地为氢; 任选取代的C 1-6烷基; C 1-6烷基羰基; 卤代甲基羰基; 或者R 1和R 2与它们所连接的氮原子一起可以形成吗啉基环或任选取代的杂环; 每个R 3和R 4独立地是卤素，氰基，羟基，卤代甲基，卤代甲氧基，羧基，硝基，氨基，单或二（C 1-6烷基）氨基，C 1-6烷基羰基氨基，氨基磺酰基，一或二（C 1-6烷基）氨基磺酰基， C 1-6烷基，C 1-6烷氧基，C 1-6烷基羰基，C 1-6烷氧基羰基; 每个R 5独立地是C 1-6烷基，氰基或卤代甲基; X是CR 6 R 7，NR 8，O，S，S（= O）或S（= O）2; 芳基是任选取代的苯基; 条件是该化合物不是（±）-3,3a，8,12b-四氢-N-甲基-2H-二苯并[3,4：6,7] - 环庚并[1,2-b] - 呋喃-2-基 - 草胺草酸。 式（I）化合物可用作治疗或预防CNS障碍，心血管疾病或胃肠道疾病的治疗剂。