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公开(公告)号：US08198446B2
公开(公告)日：2012-06-12
申请号：US12601150
申请日：2008-05-20
IPC分类号： C07D489/08
CPC分类号： A61K9/1688 , A61K9/2018 , A61K31/485 , C07D489/08
摘要： Crystalline particles of N-(17-cyclopropylmethyl-4,5α-epoxy-3,14-dihydroxy-morphinan-6β-yl)-phthalimide or a pharmaceutically acceptable salt thereof are disclosed. The crystalline particles have a particle diameter distribution in which a particle diameter (D50) at the point where cumulative frequency of volume distribution cumulatively calculated from particles having a smaller diameter reaches 50% is within a range of 1 to 30 μm, and a particle diameter (D90) at the point where cumulative frequency of volume distribution cumulatively calculated from particles having a smaller diameter reaches 90% is not more than 90 μm, which crystalline particles have a degree of crystallinity of not less than 80%. By the crystalline particles, bioavailability of the active substance may be increased while ensuring storage stability of the compound.
摘要翻译： 公开了N-（17-环丙基甲基-4,5α-环氧-3,14-二羟基 - 吗啡喃-6'-基） - 邻苯二甲酰亚胺或其药学上可接受的盐的结晶颗粒。 结晶粒子具有粒径分布，其中由具有小直径的颗粒累积计算的体积分布的累积频率达到50％的点处的粒径（D50）在1至30μm的范围内，并且粒径 （D90）在由具有较小直径的颗粒累积计算的体积分布的累积频率达到90％的点处不超过90μm，该结晶颗粒的结晶度不小于80％。 通过结晶颗粒，可以提高活性物质的生物利用度，同时确保化合物的储存稳定性。
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公开(公告)号：US20100160634A1
公开(公告)日：2010-06-24
申请号：US12601150
申请日：2008-05-20
IPC分类号： C07D489/08
CPC分类号： A61K9/1688 , A61K9/2018 , A61K31/485 , C07D489/08
摘要： Crystalline particles of N-(17-cyclopropylmethyl-4,5α-epoxy-3,14-dihydroxy-morphinan-6β-yl)-phthalimide or a pharmaceutically acceptable salt thereof are disclosed. The crystalline particles have a particle diameter distribution in which a particle diameter (D50) at the point where cumulative frequency of volume distribution cumulatively calculated from particles having a smaller diameter reaches 50% is within a range of 1 to 30 μm, and a particle diameter (D90) at the point where cumulative frequency of volume distribution cumulatively calculated from particles having a smaller diameter reaches 90% is not more than 90 μm, which crystalline particles have a degree of crystallinity of not less than 80%. By the crystalline particles, bioavailability of the active substance may be increased while ensuring storage stability of the compound.
摘要翻译： 公开了N-（17-环丙基甲基-4,5α-环氧-3,14-二羟基 - 吗啡喃-6'-基） - 邻苯二甲酰亚胺或其药学上可接受的盐的结晶颗粒。 结晶粒子具有粒径分布，其中由具有小直径的颗粒累积计算的体积分布的累积频率达到50％的点处的粒径（D50）在1至30μm的范围内，并且粒径 （D90）在由具有较小直径的颗粒累积计算的体积分布的累积频率达到90％的点处不超过90μm，该结晶颗粒的结晶度不小于80％。 通过结晶颗粒，可以提高活性物质的生物利用度，同时确保化合物的储存稳定性。
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公开(公告)号：US08470845B2
公开(公告)日：2013-06-25
申请号：US11667136
申请日：2005-11-04
申请人： Naoki Izumimoto , Kuniaki Kawamura , Toshikazu Komagata , Tadatoshi Hashimoto , Hiroshi Nagabukuro
发明人： Naoki Izumimoto , Kuniaki Kawamura , Toshikazu Komagata , Tadatoshi Hashimoto , Hiroshi Nagabukuro
IPC分类号： A61K31/44 , C07D221/22
CPC分类号： C07D489/08 , A61K31/485
摘要： An analgesic which may be applied to wide variety of pain from various causes is disclosed. The analgesic comprises as an effective ingredient a specific morphinan derivative having a nitrogen containing heterocyclic group, such as compound 1:
摘要翻译： 公开了可以应用于各种原因的多种疼痛的止痛剂。 止痛剂包含具有含氮杂环基的具体吗啡喃衍生物作为有效成分，例如化合物1：
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公开(公告)号：US20070299100A1
公开(公告)日：2007-12-27
申请号：US11667136
申请日：2005-11-04
申请人： Naoki Izumimoto , Kuniaki Kawamura , Toshikazu Komagata , Tadatoshi Hashimoto , Hiroshi Nagabukuro
发明人： Naoki Izumimoto , Kuniaki Kawamura , Toshikazu Komagata , Tadatoshi Hashimoto , Hiroshi Nagabukuro
IPC分类号： A61K31/44 , A61P29/00 , C07D221/28
CPC分类号： C07D489/08 , A61K31/485
摘要： An analgesic which may be applied to wide variety of pain from various causes is disclosed. The analgesic comprises as an effective ingredient a specific morphinan derivative having a nitrogen containing heterocyclic group, such as compound 1:
摘要翻译： 公开了可以应用于各种原因的多种疼痛的止痛剂。 止痛剂包含具有含氮杂环基的具体吗啡喃衍生物作为有效成分，例如化合物1：
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5.发明申请公开(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。
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公开(公告)号：US07718664B2
公开(公告)日：2010-05-18
申请号：US11547441
申请日：2005-03-30
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。
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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。
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8.发明授权公开(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。
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