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    Remedies or preventives for urinary frequency or urinary incontinence and morphinan derivatives having nitrogen-containing heterocyclic group
    1.
    发明申请
    Remedies or preventives for urinary frequency or urinary incontinence and morphinan derivatives having nitrogen-containing heterocyclic group 有权
    尿频或尿失禁的补救措施或预防措施以及含有氮杂环基的吗啡喃衍生物

    公开(公告)号：US20060040970A1

    公开(公告)日：2006-02-23

    申请号：US10530664

    申请日：2003-10-08

    申请人： Naoki Izumimoto ,  Koji Kawai ,  Kuniaki Kawamura ,  Morihiro Fujimura ,  Toshikazu Komagata

    发明人： Naoki Izumimoto ,  Koji Kawai ,  Kuniaki Kawamura ,  Morihiro Fujimura ,  Toshikazu Komagata

    IPC分类号： A61K31/473

    CPC分类号： C07D489/08

    摘要： The invention provides a morphinan derivative of the Formula (I): (wherein R1 is methyl, cyclopropylmethyl or the like; R2 and R3 are hydroxy, methoxy, acetoxy or the like; both Y and Z are valence bonds, —C(═O)— or the like; X is C2-C5 carbon chain (one of the carbon atoms may be substituted by oxygen, sulfur or nitrogen) constituting a part of the ring structure, or the like; (R4)k is substituted or non-substituted benzene fused ring, carbonyl group or the like; R9 is hydrogen or the like; R10 and R11 are bound to represent —O—, or the like, and R6 is hydrogen or the like) or a pharmaceutically acceptable acid addition salt thereof. The invention also provides a therapeutic or prophylactic agent for urinary frequency or urinary incontinence, comprising as an effective ingredient the morphinan derivative or the pharmaceutically acceptable acid addition salt thereof; a method for therapy or prophylaxis of the diseases.

    摘要翻译： 本发明提供式（I）的吗啡喃衍生物：其中R 1是甲基，环丙基甲基等; R 2和R 3 O >是羟基，甲氧基，乙酰氧基等; Y和Z都是价键，-C（-O） - 等; X是C 2 -C 5 构成环结构的一部分的碳链（其中一个碳原子可以被氧，硫或氮取代）等;（R 4） 是取代或未取代的苯稠环，羰基等; R 9是氢等; R 10和R 11， 必须代表-O-等，R 6是氢等）或其药学上可接受的酸加成盐。 本发明还提供了用于尿频或尿失禁的治疗或预防剂，其包含吗啡喃衍生物或其药学上可接受的酸加成盐作为有效成分; 一种治疗或预​​防疾病的方法。

    Remedies or preventives for urinary frequency or urinary incontinence and morphinan derivatives having nitrogen-containing heterocyclic group
    2.
    发明授权
    Remedies or preventives for urinary frequency or urinary incontinence and morphinan derivatives having nitrogen-containing heterocyclic group 有权
    尿频或尿失禁的补救措施或预防措施以及含有氮杂环基的吗啡喃衍生物

    公开(公告)号：US07320984B2

    公开(公告)日：2008-01-22

    申请号：US10530664

    申请日：2003-10-08

    申请人： Naoki Izumimoto ,  Koji Kawai ,  Kuniaki Kawamura ,  Morihiro Fujimura ,  Toshikazu Komagata

    发明人： Naoki Izumimoto ,  Koji Kawai ,  Kuniaki Kawamura ,  Morihiro Fujimura ,  Toshikazu Komagata

    IPC分类号： A61K31/485 ,  C07D489/00

    CPC分类号： C07D489/08

    摘要： The invention provides a morphinan derivative of the Formula (I): wherein R1 is methyl, cyclopropylmethyl or the like; R2 and R3 are hydroxy, methoxy, acetoxy or the like; both Y and Z are valence bonds, —C(═O)— or the like; X is C2-C5 carbon chain (one of the carbon atoms may be substituted by oxygen, sulfur or nitrogen) constituting a part of the ring structure, or the like; (R4)k is substituted or non-substituted benzene fused ring, carbonyl group or the like; R9 is hydrogen or the like; R10 and R11 are bound to represent —O—, or the like, and R6 is hydrogen or the like or a pharmaceutically acceptable acid addition salt thereof. The invention also provides a therapeutic or prophylactic agent for urinary frequency or urinary incontinence, comprising as an effective ingredient the morphinan derivative or the pharmaceutically acceptable acid addition salt thereof; a method for therapy or prophylaxis of the diseases.

    摘要翻译： 本发明提供式（I）的吗啡喃衍生物：其中R 1是甲基，环丙基甲基等; R 2和R 3是羟基，甲氧基，乙酰氧基等; Y和Z都是价键，-C（-O） - 等; X是C 2 -C 5 -C 5碳链（其中一个碳原子可以被氧，硫或氮取代）构成环结构的一部分等 ; （R 4）k是取代或未取代的苯稠环，羰基等; R 9是氢等; R 10和R 11结合表示-O-等，R 6是氢等或其药学上可接受的 其酸加成盐。 本发明还提供了用于尿频或尿失禁的治疗或预防剂，其包含吗啡喃衍生物或其药学上可接受的酸加成盐作为有效成分; 一种治疗或预​​防疾病的方法。

    Morphinan derivatives and pharmaceutical use thereof
    7.
    发明授权
    Morphinan derivatives and pharmaceutical use thereof 失效
    吗啡衍生物及其药物用途

    公开(公告)号：US06177438B1

    公开(公告)日：2001-01-23

    申请号：US08754750

    申请日：1996-11-21

    申请人： Hiroshi Nagase ,  Jun Hayakawa ,  Kuniaki Kawamura ,  Koji Kawai ,  Takashi Endoh

    发明人： Hiroshi Nagase ,  Jun Hayakawa ,  Kuniaki Kawamura ,  Koji Kawai ,  Takashi Endoh

    IPC分类号： C07D49108

    CPC分类号： C07D489/08 ,  C07D489/00

    摘要： A morphinan derivative or its pharmaceutically acceptable acid addition salt represented with, for example, and an analgesic, diuretic, antitussive and brain cell protector having its derivative or its salt as the active ingredient are described. The compound of the present invention possesses strong analgesic activity, diuretic action and antitussive action as a highly selective &kgr;-opioid agonist, allowing it to be used as a useful analgesic, diuretic and antitussive. On the other hand, the compound of the present invention also possesses remarkable cerebro-neuroprotective activity, thus allowing it be used as a useful cerebro-neuroprotective agents.

    摘要翻译： 描述了以其衍生物或其盐作为活性成分代表的吗啡喃衍生物或其药学上可接受的酸加成盐和镇痛药，利尿剂，镇咳药和脑细胞保护剂。本发明化合物具有强的止痛活性 ，利尿作用和镇咳作用作为高度选择性的κ-阿片样物质激动剂，使其可用作有用的止痛剂，利尿剂和镇咳药。 另一方面，本发明的化合物也具有显着的脑血管保护作用，因此可用作有用的脑血管保护剂。

    Remedies for sepsis
    9.
    发明授权
    Remedies for sepsis 失效
    败血症的治疗方法

    公开(公告)号：US07652025B2

    公开(公告)日：2010-01-26

    申请号：US10477062

    申请日：2002-05-08

    申请人： Tomohiko Suzuki ,  Hideaki Inada ,  Yoshitaka Yoshizawa ,  Kuniaki Kawamura ,  Toshiaki Tanaka

    发明人： Tomohiko Suzuki ,  Hideaki Inada ,  Yoshitaka Yoshizawa ,  Kuniaki Kawamura ,  Toshiaki Tanaka

    IPC分类号： A01N43/42 ,  A61K31/44

    CPC分类号： A61K31/40 ,  A61K31/485 ,  A61K38/00 ,  C07D489/08 ,  C07K5/1016

    摘要： A therapeutic agent for sepsis and various symptoms accompanying sepsis (such as septic shock, disseminated intravascular coagulation syndrome, adult respiratory distress syndrome and multiple organ dysfunction) is disclosed. The therapeutic agent for sepsis according to the present invention comprises as an effective ingredient an opioid κ receptor agonist compound such as (−)-17-(cyclopropylmethyl)-3,14β-dihydroxy-4,5α-epoxy-6β[N-methyl-trans-3-(3-furyl)acrylamide] oxide derivative. The opioid κ receptor agonist compound may be administered as it is or in the form of a pharmaceutical composition prepared by mixing the compound with a known pharmaceutically acceptable acid, carrier or vehicle orally or parenterally.

    摘要翻译： 公开了脓毒症和伴随脓毒症的各种症状的治疗剂（例如脓毒性休克，弥散性血管内凝血综合征，成人呼吸窘迫综合征和多器官功能障碍）。 根据本发明的败血症治疗剂包括作为有效成分的阿片样物质κ受体激动剂化合物，例如（ - ） - 17-（环丙基甲基）-3,14β-二羟基-4,5α-环氧-6β-[N-甲基 （3-呋喃基）丙烯酰胺]氧化物衍生物。 阿片样物质κ受体激动剂化合物可以原样或以通过将化合物与已知的药学上可接受的酸，载体或载体口服或胃肠外混合制备的药物组合物的形式进行给药。