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47 条记录 (耗时 0.044 秒)

    Pyrrolidinyl and pyrrolinyl ethylamine compounds as kappa agonists
    4.
    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：US06310061B2

    公开(公告)日：2001-10-30

    申请号：US09770515

    申请日：2001-01-26

    申请人： Fumitaka Ito ,  Hiroshi Kondo

    发明人： Fumitaka Ito ,  Hiroshi Kondo

    IPC分类号： A61K31445

    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, piperidine or morpholine ring. 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，哌啶或吗啉环。 这些化合物可用作κ激动剂。

    Pyrrolidinyl and pyrrolinyl ethylamine compounds as kappa agonists
    5.
    发明授权
    Pyrrolidinyl and pyrrolinyl ethylamine compounds as kappa agonists 失效

    公开(公告)号：US06307061B2

    公开(公告)日：2001-10-23

    申请号：US09771029

    申请日：2001-01-26

    申请人： Fumitaka Ito ,  Hiroshi Kondo

    发明人： Fumitaka Ito ,  Hiroshi Kondo

    IPC分类号： C07D20704

    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.

    Pyrrolidinyl and pyrrolinyl ethylamine compounds as kappa agonists
    6.
    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：US06201007B1

    公开(公告)日：2001-03-13

    申请号：US09254805

    申请日：1999-03-12

    申请人： Fumitaka Ito ,  Hiroshi Kondo

    发明人： Fumitaka Ito ,  Hiroshi Kondo

    IPC分类号： A61K31402

    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, 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，虚线代表任选的双键，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 hydroxamic acid compounds and their production process
    7.
    发明授权
    Pyrrolidinyl hydroxamic acid compounds and their production process 失效
    吡咯烷基异羟肟酸化合物及其制备方法

    公开(公告)号：US5952369A

    公开(公告)日：1999-09-14

    申请号：US913823

    申请日：1997-09-26

    申请人： Fumitaka Ito

    发明人： Fumitaka Ito

    IPC分类号： C07D295/12 ,  A61K31/40 ,  A61K31/4025 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/4433 ,  A61P1/00 ,  A61P7/00 ,  A61P7/10 ,  A61P23/00 ,  A61P25/00 ,  A61P25/04 ,  A61P25/28 ,  A61P29/00 ,  A61P43/00 ,  C07D20060101 ,  C07D207/12 ,  C07D213/54 ,  C07D295/13 ,  C07D307/79 ,  C07D401/06 ,  C07D401/12 ,  C07D405/06 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  A61K31/41

    CPC分类号： C07D213/54 ,  C07D207/12 ,  C07D295/13 ,  C07D307/79 ,  C07D405/12 ,  C07D409/12 ,  Y02P20/55

    摘要： A compound of formula (I) ##STR1## and its pharmaceutically acceptable salt, wherein A is hydrogen or OY, wherein Y is a hydroxy protecting group; Ar is phenyl optionally substituted with one or more substituents selected from halo, hydroxy, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, CF.sub.3, C.sub.1 -C.sub.4 alkoxy-C.sub.1 -C.sub.4 alkyloxy and carboxy-C.sub.1 -C.sub.4 alkyloxy;X is phenyl, naphthyl, biphenyl, indanyl, benzofuranyl, benzothiophenyl, 1-tetralone-6-yl,C.sub.1 -C.sub.4 alkylenedioxy, pyridyl, furyl and thienyl these groups optionally being substituted with up to three substituents selected from halo, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, hydroxy, NO.sub.2, CF.sub.3 and SO.sub.2 CH.sub.3 ; andR is hydrogen, C.sub.1 -C.sub.4 alkyl or a hydroxy protecting group. These compounds and pharmaceutical compositions containing them are useful as analgesic, anti-inflammatory, diuretic, anesthetic or neuroprotective agents, or an agent for stroke or treatment of functional bowel diseases such as abdominal pain, for the treatment of a mammalian subject, especially a human subject. Further, the present invention provides processes for producing the hydroxamic compounds of formula (I) and their intermediate compounds of the formula. ##STR2##

    摘要翻译： PCT No.PCT / JP96 / 00820 Sec。 371日期：1997年9月26日 102（e）1997年9月26日PCT PCT 1996年3月28日PCT公布。 WO96 / 30339 PCT公开号 日期：1996年10月3日一种式（I）化合物及其药学上可接受的盐，其中A为氢或OY，其中Y为羟基保护基; Ar是任选被一个或多个选自卤素，羟基，C 1 -C 4烷基，C 1 -C 4烷氧基，CF 3，C 1 -C 4烷氧基-C 1 -C 4烷氧基和羧基-C 1 -C 4烷氧基的取代基取代的苯基; X是苯基，萘基，联苯基，茚满基，苯并呋喃基，苯并噻吩基，1-四氢萘酮-6-基，C 1 -C 4亚烷基二氧基，吡啶基，呋喃基和噻吩基，这些基团任选被至多三个选自卤素，C 1 -C 4烷基， C 1 -C 4烷氧基，羟基，NO 2，CF 3和SO 2 CH 3; 和R是氢，C 1 -C 4烷基或羟基保护基。 这些化合物和含有它们的药物组合物可用作止痛剂，抗炎剂，利尿剂，麻醉剂或神经保护剂，或用于中风或治疗功能性肠病如腹痛的药剂，用于治疗哺乳动物受试者，特别是人 学科。 此外，本发明提供了制备式（I）的异羟肟酸化合物及其下式的中间体化合物的方法。

    2-benzimidazolylamine compounds as ORL-1-receptor agonists
    10.
    发明授权
    2-benzimidazolylamine compounds as ORL-1-receptor agonists 失效
    2-苯并咪唑胺化合物作为ORL-1受体激动剂

    公开(公告)号：US06340681B1

    公开(公告)日：2002-01-22

    申请号：US09606921

    申请日：2000-06-29

    申请人： Fumitaka Ito

    发明人： Fumitaka Ito

    IPC分类号： C07D40104

    CPC分类号： C07D401/04

    摘要： A compound of the formula: or a pharmaceutically acceptable salt thereof, wherein R1 and R2 are independently selected from hydrogen, halo, hydroxy, (C1-C4)alkyl, halo (C1-C4)alkyl and the like; R3 and R4 are independently selected from hydrogen, halo(C1-C10)alkyl, optionally substituted (C1-C6)alkyl and the like, or R3 and R4, together with the nitrogen atom to which they are attached, form an optionally substituted fully saturated, partially saturated or fully unsaturated heterocyclic ring; and R5 is (C4-C11)cycloalkyl and the like, has ORL1-receptor agonist activity, and are useful as analgesics or the like in mammalian subjects.

    摘要翻译： 下式化合物或其药学上可接受的盐，其中R 1和R 2独立地选自氢，卤素，羟基，（C 1 -C 4）烷基，卤代（C 1 -C 4）烷基等; R 3和R 4独立地选自氢，卤素（C 1 -C 10）烷基，任选取代的（C 1 -C 6）烷基等，或者R 3和R 4与它们所连接的氮原子一起形成任选取代的 饱和的，部分饱和的或完全不饱和的杂环; R5为（C4-C11）环烷基等具有ORL1-受体激动剂活性，在哺乳动物受试者中可用作止痛药等。