Remedies or preventives for urinary frequency or urinary incontinence and morphinan derivatives having nitrogen-containing heterocyclic group
    1.
    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

    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。

    Remedies or preventives for urinary frequency or urinary incontinence and morphinan derivatives having nitrogen-containing heterocyclic group
    2.
    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

    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。

    Anti-itching agent
    5.
    发明授权
    Anti-itching agent 有权
    抗痒剂

    公开(公告)号:US07718664B2

    公开(公告)日:2010-05-18

    申请号:US11547441

    申请日:2005-03-30

    IPC分类号: A01N43/42 A61K31/44

    CPC分类号: C07D489/08 A61K31/485

    摘要: A method of inhibiting or reducing occurrence or intensity of pruritus including administering to a patient an effective amount of one or more of the morphinan derivative having a nitrogen-containing cyclic group of the Formula (Ia): wherein R1 is cyclopropylmethyl; R2 and R3 are independently hydrogen, hydroxy, C1-C5 alkoxy, C3-C7 alkenyloxy, C7-C13 aralkyloxy or C1-C5 alkanoyloxy; and the Formula (Ia) includes (+), (−) and (±) isomers or the pharmaceutically acceptable acid addition salt thereof.

    摘要翻译: 一种抑制或减少瘙痒的发生或强度的方法,包括向患者施用有效量的一种或多种具有式(Ia)的含氮环状基团的吗啡喃衍生物:其中R1是环丙基甲基; R2和R3独立地是氢,羟基,C1-C5烷氧基,C3-C7链烯氧基,C7-C13芳烷氧基或C1-C5烷酰氧基; 式(Ia)包括(+),( - )和(±)异构体或其药学上可接受的酸加成盐。

    Anti-Itching Agent
    6.
    发明申请
    Anti-Itching Agent 有权
    抗痒剂

    公开(公告)号:US20080275074A1

    公开(公告)日:2008-11-06

    申请号:US11547441

    申请日:2005-03-30

    IPC分类号: A61K31/485 A61P17/00

    CPC分类号: C07D489/08 A61K31/485

    摘要: A novel antipruritic useful for the treatment of pruritus accompanying various diseases is disclosed. The antipruritic comprises a specific morphinan derivative having a nitrogen-containing cyclic group or the pharmaceutically acceptable acid addition salt thereof such as N-(17-cyclopropylmethyl-4,5α-epoxy-3,14-dihydroxy-morphinan-6β-yl)-phthalimide hydrochloric acid salt or N-(17-cyclopropylmethyl-4,5α-epoxy-3,14-dihydroxy-morphinan-6β-yl)-3,4,5,6-tetrahydrophthalimide tartaric acid salt.

    摘要翻译: 公开了一种用于治疗伴随各种疾病的瘙痒的新型止痒剂。 止痒剂包含具有含氮环状基团的具体吗啡喃衍生物或其药学上可接受的酸加成盐,例如N-(17-环丙基甲基-4,5α-环氧-3,14-二羟基 - 吗啡喃-6β-基) - 邻苯二甲酰亚胺盐酸盐或N-(17-环丙基甲基-4,5α-环氧-3,14-二羟基 - 吗啡喃-6β-基)-3,4,5,6-四氢邻苯二甲酰亚胺酒石酸盐。

    Antitussive agent
    7.
    发明授权
    Antitussive agent 有权
    镇咳药

    公开(公告)号:US08106065B2

    公开(公告)日:2012-01-31

    申请号:US12158100

    申请日:2006-12-15

    CPC分类号: C07D489/08 A61K31/485

    摘要: An antitussive, which can be used for therapy or prophylaxis of coughing, is disclosed. The antitussive comprises as an effective ingredient a morphinan derivative having a nitrogen-containing cyclic substituent or a pharmaceutically acceptable acid addition salt thereof, having a specific structure, such as the compound below [N-(17-cyclopeopylmethyl-4,5α-epoxy-3,14-dihydroxy-morphinan-6β-yl)-3,4,5,6-tetrahydrophthalimide]. The antitussive has an excellent therapeutic or prophylactic effect against coughing and the side effects thereof are small.

    摘要翻译: 公开了可用于治疗或预防咳嗽的镇咳药。 止咳剂作为有效成分包含具有特定结构的含氮环状取代基的吗啡喃衍生物或其药学上可接受的酸加成盐,例如[N-(17-环戊基甲基-4,5α-环氧 - 3,14-二羟基 - 吗啡喃-6'-基)-3,4,5,6-四氢邻苯二甲酰亚胺]。 止咳剂对咳嗽具有优异的治疗或预防作用,其副作用小。

    Antitussive Agent
    8.
    发明申请
    Antitussive Agent 有权
    镇咳药

    公开(公告)号:US20090176818A1

    公开(公告)日:2009-07-09

    申请号:US12158100

    申请日:2006-12-15

    CPC分类号: C07D489/08 A61K31/485

    摘要: An antitussive, which can be used for therapy or prophylaxis of coughing, is disclosed. The antitussive comprises as an effective ingredient a morphinan derivative having a nitrogen-containing cyclic substituent or a pharmaceutically acceptable acid addition salt thereof, having a specific structure, such as the compound below [N-(17-cyclopeopylmethyl-4,5α-epoxy-3,14-dihydroxy-morphinan-6β-yl)-3,4,5,6-tetrahydrophthalimide]. The antitussive has an excellent therapeutic or prophylactic effect against coughing and the side effects thereof are small.

    摘要翻译: 公开了可用于治疗或预防咳嗽的镇咳药。 镇咳药包含具有特定结构的含氮环状取代基的吗啡喃衍生物或其药学上可接受的酸加成盐,例如[N-(17-环戊基甲基-4,4α-环氧 - 3,14-二羟基 - 吗啡喃-6β-基)-3,4,5,6-四氢邻苯二甲酰亚胺]。 止咳剂对咳嗽具有优异的治疗或预防作用,其副作用小。