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47 条记录 (耗时 0.038 秒)

    Pyrrolidinyl and pyrrolinyl ethylamine compounds as kappa agonists
    21.
    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
    22.
    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
    23.
    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。

    Pyrrolidinyl and pyrrolinyl ethylamine compounds as kappa agonists
    24.
    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
    25.
    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。

    Headstock of a polishing machine
    29.
    发明授权
    Headstock of a polishing machine 失效
    抛光机头架

    公开(公告)号：US6027401A

    公开(公告)日：2000-02-22

    申请号：US955701

    申请日：1997-10-23

    申请人： Hideo Saito ,  Fumitaka Ito

    发明人： Hideo Saito ,  Fumitaka Ito

    IPC分类号： B24B37/30 ,  B24B41/04 ,  B24B7/22

    CPC分类号： B24B37/30 ,  B24B41/042

    摘要： The present invention provides a headstock of a polishing machine, having a simple structure and capable of tracing a pad surface. The headstock of the present invention is formed of a spindle, a holder plate, a spherical bearing, and a plate spring. The holder plate is connected to a lower end portion of the spindle via the spherical bearing and the plate spring. A workpiece is attached to the lower surface of the holder plate. The spherical bearing has a center of tilting movement on a rotation axis of the spindle. The holder plate has a balance plate. The center of gravity of the holder plate including the balance plate coincides with the center of tilting movement of the spherical bearing. The plate spring has an axisymmetric shape. More specifically, the plate spring has an opening portion at the center and a plurality of arm portions extending to the outer periphery in the diameter direction. The plate spring is connected to the lower end of the spindle by use of first fitting holes which are formed along the inner periphery, and the plate spring is also attached to the holder plate by use of second fitting holes which are formed in the distal end of the plate spring. The first and second fitting holes are respectively located on small- and large-diameter circles which are concentrically arranged around the rotation axis of the spindle.

    摘要翻译： 本发明提供一种抛光机的头架，其具有简单的结构并且能够跟踪垫表面。 本发明的主轴箱由主轴，保持板，球面轴承和板簧构成。 保持板通过球面轴承和板簧连接到主轴的下端部分。 工件附接到保持板的下表面。 球面轴承在主轴的旋转轴线上具有倾斜运动的中心。 支架板具有平衡板。 包括平衡板的保持板的重心与球面轴承的倾斜运动的中心重合。 板簧具有轴对称形状。 更具体地，板簧在中心具有开口部分，并且在直径方向上延伸到外周的多个臂部分。 板簧通过使用沿着内周形成的第一嵌合孔连接到主轴的下端，并且板簧也通过使用形成在远端的第二装配孔附接到保持板 的板簧。 第一和第二装配孔分别位于围绕主轴的旋转轴线同心布置的小直径和大直径的圆周上。

    Morphinan hydroxamic acid compounds
    30.
    发明授权
    Morphinan hydroxamic acid compounds 失效
    吗啡异羟肟酸化合物

    公开(公告)号：US5834478A

    公开(公告)日：1998-11-10

    申请号：US928953

    申请日：1997-09-12

    申请人： Fumitaka Ito

    发明人： Fumitaka Ito

    IPC分类号： C07D489/00 ,  A61K31/485 ,  A61P1/00 ,  A61P7/10 ,  A61P23/02 ,  A61P25/00 ,  A61P25/02 ,  A61P25/04 ,  A61P29/00 ,  A61P43/00 ,  C07D489/08 ,  C07D489/02

    CPC分类号： C07D489/08 ,  Y02P20/55

    摘要： This invention provides a compound of the following formula: ##STR1## and the pharmaceutically acceptable salts thereof, wherein R is hydrogen, C.sub.1 -C.sub.5 alkyl or an O-protecting group; B is a dircet bond, C.sub.1 -C.sub.5 alkylene or C.sub.2 -C.sub.5 alkenylene; R.sup.1 is C.sub.1 -C.sub.5 alkyl, C.sub.2 -C.sub.5 alkenyl or C.sub.3 -C.sub.7 cycloalkyl-C.sub.1 -C.sub.3 alkyl; R.sup.2 is hydroxy or C.sub.1 -C.sub.5 alkoxy; R.sup.3 is hydrogen, hydroxy or C.sub.1 -C.sub.5 alkoxy; and R.sup.4 is hydrogen, phenyl or heteroaryl selected from furyl, thienyl and pyrrolyl, the phenyl and heteroaryl being optionally substituted by one to five substitutents selected from halo, hydroxy, C.sub.1 -C.sub.3 allyl, C.sub.1 -C.sub.3 alkoxy and C.sub.2 -C.sub.5 alkenyl. These compounds and pharmaceutical compositions containing such compounds are useful as analgesic, antiinflammatory, 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.

    摘要翻译： 本发明提供了下式的化合物：其中R是氢，C 1 -C 5烷基或O-保护基; B是Dircet键，C1-C5亚烷基或C2-C5亚烯基; R 1是C 1 -C 5烷基，C 2 -C 5烯基或C 3 -C 7环烷基-C 1 -C 3烷基; R2是羟基或C1-C5烷氧基; R3是氢，羟基或C1-C5烷氧基; R4是氢，选自呋喃基，噻吩基和吡咯基的苯基或杂芳基，苯基和杂芳基任选被1至5个选自卤素，羟基，C 1 -C 3烯丙基，C 1 -C 3烷氧基和C 2 -C 5烯基的取代基取代。 含有这些化合物的这些化合物和药物组合物可用作止痛剂，抗炎药，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，特别是人类受试者 。