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213 条记录 (耗时 0.04 秒)

    Pyrrolidinyl and pyrrolinyl ethylamine compounds as kappa agonists
    5.
    发明授权
    Pyrrolidinyl and pyrrolinyl ethylamine compounds as kappa agonists 失效
    吡咯烷基和吡咯啉基乙胺化合物作为κ激动剂

    公开(公告)号：US06313302B2

    公开(公告)日：2001-11-06

    申请号：US09770513

    申请日：2001-01-26

    申请人： Fumitaka Ito ,  Hiroshi Kondo

    发明人： Fumitaka Ito ,  Hiroshi Kondo

    IPC分类号： C07C23724

    CPC分类号： C07D213/82 ,  C07D207/10 ,  C07D207/12 ,  C07D207/20 ,  C07D207/24 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  Y02P20/55

    摘要： A compound of the following formula: and the salts thereof, wherein A is hydrogen, halo, or hydroxy; the broken line represents an optional double bond with proviso that if the broken line is a double bond, then A is absent; Ar1 is optionally substituted phenyl; Ar2 is aryl or heteroaryl selected from phenyl, napththyl, or pyridyl, the aryl or heteroaryl being optionally substituted; R1 is hydrogen, hydroxy, or C1-C4 alkyl; and R2 and R3 are independently selected from optionally substituted C1-C7 alkyl, C3-C6 cycloalkyl, C2-C6 alkenyl, C2-C6 alkynyl, or R2 and R3, together with the nitrogen atom to which they are attached, form an optionally substituted pyrrolidine. These compounds are useful as kappa agonists.

    摘要翻译： 下式的化合物及其盐，其中A是氢，卤素或羟基; 虚线表示任选的双键，条件是如果虚线是双键，则A不存在; Ar1是任选取代的苯基; Ar2是选自苯基，萘乙基或吡啶基的芳基或杂芳基，芳基或杂芳基任选被取代; R1是氢，羟基或C1-C4烷基; 并且R 2和R 3独立地选自任选取代的C 1 -C 7烷基，C 3 -C 6环烷基，C 2 -C 6烯基，C 2 -C 6炔基或R 2和R 3与它们所连接的氮原子一起形成任选取代的 吡咯烷。 这些化合物可用作κ激动剂。

    Pyrrolidinyl and pyrrolinyl ethylamine compounds as kappa agonists
    6.
    发明授权
    Pyrrolidinyl and pyrrolinyl ethylamine compounds as kappa agonists 失效

    公开(公告)号：US06294569B2

    公开(公告)日：2001-09-25

    申请号：US09770514

    申请日：2001-01-26

    申请人： Fumitaka Ito ,  Hiroshi Kondo

    发明人： Fumitaka Ito ,  Hiroshi Kondo

    IPC分类号： A61K314025

    CPC分类号： C07D213/82 ,  C07D207/10 ,  C07D207/12 ,  C07D207/20 ,  C07D207/24 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  Y02P20/55

    摘要： A compound of the following formula: and the salts thereof, wherein A is hydrogen, halo, hydroxy, or the like; the broken line represents an optional double bond with proviso that if the broken line is a double bond, then A is absent; Ar1 is optionally substituted phenyl or the like; Ar2 is aryl or heteroaryl selected from phenyl, napththyl, pyridyl, and the like, the aryl or heteroaryl being optionally substituted; R1 is hydrogen, hydroxy, C1-C4 alkyl, or the like; and R2 and R3 are independently selected from optionally substituted C1-C7 alkyl, C3-C6 cycloalkyl, C2-C6 alkenyl, C2-C6 alkynyl, and the like or R2 and R3, together with the nitrogen atom to which they are attached, form an optionally substituted pyrrolidine, piperidine or morpholine ring. These compounds are useful as kappa agonists.

    2-substituted-1-piperidyl benzimidazole compounds as ORL1-receptor agonists
    7.
    发明授权
    2-substituted-1-piperidyl benzimidazole compounds as ORL1-receptor agonists 失效
    2-取代-1-哌啶基苯并咪唑化合物作为ORL1-受体激动剂

    公开(公告)号：US06172067B2

    公开(公告)日：2001-01-09

    申请号：US09369208

    申请日：1999-08-05

    申请人： Fumitaka Ito ,  Hirohide Noguchi ,  Hiroshi Kondo

    发明人： Fumitaka Ito ,  Hirohide Noguchi ,  Hiroshi Kondo

    IPC分类号： A61K31454

    CPC分类号： C07D401/04 ,  C07D211/58 ,  C07D401/14

    摘要： A compound of the formula: or a pharmaceutically acceptable salt thereof, wherein R is unsubstituted, mono-, di- or tri-substituted (C3-C11)cycloalkyl or (C3-C11)cycloalkenyl or the like, A is unsubstituted (C1-C7)alkyl or (C2-C5 )alkenyl, or unsubstituted, mono-, di- or tri-substituted aryl, or aromatic-heterocyclic or the like, Y is hydrogen, halo, amino or mercapto, or unsubstituted, mono-, di- or tri- substituted (C1-C10)alkyl-M—, (C3-C7)cycloalkyl-M—, (C2-C6)alkenyl-M—, (C1-C4)alkyl-NH-((C1-C4)alkyl)-M—, di(C1-C4)alkyl-N-((C1-C4)alkyl)-M—, aryl-M—, aromatic or non-aromatic heterocyclic-M—, aryl-(C1-C5)alkyl-M— or aromatic non-aromatic heterocyclic-(C1-C5)alkyl-M—, wherein M is a covalent bond O, S, NH or the like, or the like; Z1, Z2, Z3 and Z4 are hydrogen or the like, has ORL1-receptor agonist activity, and are useful as analgesics or the like in mammalian subjects.

    摘要翻译： 一种下式的化合物或其药学上可接受的盐，其中R是未取代的一价，二或三取代的（C 3 -C 11）环烷基或（C 3 -C 11）环烯基等，A是未取代的（C1- C7）烷基或（C2-C5）烯基或未取代的单，二或三取代的芳基或芳族杂环等，Y是氢，卤素，氨基或巯基，或未取代的单，二 - （C 1 -C 6）烷基-M-，（C 3 -C 7）环烷基M - ，（C 2 -C 6）烯基-M-，（C 1 -C 4）烷基-NH-（（C 1 -C 4） 烷基）-M-，二（C 1 -C 4）烷基-N - （（C 1 -C 4）烷基）-M-，芳基M-，芳族或非芳族杂环M-，芳基 - （C 1 -C 5） 烷基-M-或芳族非芳族杂环 - （C1-C5）烷基-M-，其中M是共价键O，S，NH等; Z1，Z2，Z3和Z4为氢等具有ORL1-受体激动剂活性，并且可用作哺乳动物受试者中的止痛剂等。

    Pyrrolidinyl and pyrrolinyl ethylamine compounds as kappa agonists
    10.
    发明授权
    Pyrrolidinyl and pyrrolinyl ethylamine compounds as kappa agonists 失效
    吡咯烷基和吡咯啉基乙胺化合物作为κ激动剂

    公开(公告)号：US06303602B1

    公开(公告)日：2001-10-16

    申请号：US09770512

    申请日：2001-01-26

    申请人： Fumitaka Ito ,  Hiroshi Kondo

    发明人： Fumitaka Ito ,  Hiroshi Kondo

    IPC分类号： A61K31401

    CPC分类号： C07D213/82 ,  C07D207/10 ,  C07D207/12 ,  C07D207/20 ,  C07D207/24 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  Y02P20/55

    摘要： A compound of the following formula: or a salt thereof, wherein A is hydrogen, halo, hydroxy; the broken line represents an optional double bond with proviso that if the broken line is a double bond, then A is absent; Ar1 is optionally substituted phenyl; Ar2 is aryl or heteroaryl selected from phenyl, napththyl, furanyl or thienyl, the aryl or heteroaryl being optionally substituted; R1 is hydrogen, hydroxy, or C1-C4 alkyl; and R2 and R3 are independently selected from optionally substituted C1-C7 alkyl, C3-C6 cycloalkyl, C2-C6 alkenyl, C2-C6 alkynyl, or R2 and R3, together with the nitrogen atom to which they are attached, form an optionally substituted pyrrolidine, piperidine or morpholine ring. These compounds are useful as kappa agonists.

    摘要翻译： 下式的化合物或其盐，其中A是氢，卤素，羟基; 虚线表示任选的双键，条件是如果虚线是双键，则A不存在; Ar1是任选取代的苯基; Ar 2是选自苯基，萘乙基，呋喃基或噻吩基的芳基或杂芳基，芳基或杂芳基任选被取代; R1是氢，羟基或C1-C4烷基; 并且R 2和R 3独立地选自任选取代的C 1 -C 7烷基，C 3 -C 6环烷基，C 2 -C 6烯基，C 2 -C 6炔基或R 2和R 3与它们所连接的氮原子一起形成任选取代的 吡咯烷，哌啶或吗啉环。 这些化合物可用作κ激动剂。