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1. 发明授权

US06284769B1 Nonpeptide kappa opioid receptor antagonists 失效
标题翻译：非肽κ阿片受体拮抗剂
公开(公告)号：US06284769B1
公开(公告)日：2001-09-04
申请号：US09454670
申请日：1999-12-03
申请人： William Dunn , Ludwig Bauer , Hemendra N. Bhargava
发明人： William Dunn , Ludwig Bauer , Hemendra N. Bhargava
IPC分类号： A61K31485
CPC分类号： C07D489/08
摘要： The compounds of structural formulae (I) and (II) and use of the compounds and salts and hydrates thereof, as therapeutic agents, is disclosed. A compound of formula (I) or (II) is an agonist for the &mgr; and &dgr; opioid receptors, an antagonist for the &kgr; opioid receptor, and has high affinity at all three receptors. A compound of formula (I) or (II) has utility in a variety of therapeutic and research areas where &kgr; opioid receptor antagonism is beneficial, including the treatment of opiate addiction or pain, or in a method of stimulating an immune system of a human.
摘要翻译：公开了结构式（I）和（II）的化合物及其化合物及其盐和水合物作为治疗剂的用途。式（I）或（II）的化合物是mu和δ阿片样受体的激动剂，它是κ阿片受体的拮抗剂，并且在所有三种受体上具有高亲和力。式（I）或（II）的化合物可用于各种治疗和研究领域，其中κ阿片受体拮抗作用是有益的，包括治疗阿片成瘾或疼痛，或在刺激人的免疫系统的方法中。

2. 发明授权

US06670370B1 Dextromethorphan tannate 失效
标题翻译：丹宁酸右美沙芬
公开(公告)号：US06670370B1
公开(公告)日：2003-12-30
申请号：US10281725
申请日：2002-10-28
申请人： Vilas M. Chopdekar , James R. Schleck , Hemant S. Desai
发明人： Vilas M. Chopdekar , James R. Schleck , Hemant S. Desai
IPC分类号： A61K31485
CPC分类号： A61K31/4402 , C07D213/38 , Y10S514/85 , Y10S514/855
摘要： The invention pertains to a composition comprising dextromethorphan tannate and to a method for preparing dextromethorphan tannate by reacting dextromethorphan at a temperature of about 80 to about 180° C. with tannic acid either neat or as an aqueous slurry containing about 5 to about 30 wt. % water. The dextromethorphan tannate has extended release properties and is useful in pharmaceutical compositions as an antitussive for human beings.
摘要翻译：本发明涉及包含右美沙芬丹宁酸盐的组合物和通过使右美沙芬在约80至约180℃的温度下反应制备右美沙芬来制备右美沙芬的方法，所述丹宁酸是纯的或含有约5至约30wt。％水。右美沙芬丹宁酸盐具有延长的释放性能，并且可用作药物组合物作为人类镇咳药。

3. 发明授权

US06589960B2 Hydromorphone and hydrocodone compositions and methods for their synthesis 有权
标题翻译：氢吗啡酮和氢可酮组合物及其合成方法
公开(公告)号：US06589960B2
公开(公告)日：2003-07-08
申请号：US10256996
申请日：2002-09-27
申请人： William H. Harclerode , Robert Gault , Mark D. Sandison
发明人： William H. Harclerode , Robert Gault , Mark D. Sandison
IPC分类号： A61K31485
CPC分类号： C07D489/02 , A61K31/485
摘要： A method for the preparation of a ketone from a narcotic alkaloid having an allyl alcohol moiety is disclosed. The method includes mixing the narcotic alkaloid with an acid in the presence of a catalyst wherein the method is carried out in the substantial absence of hydrogen gas. The method is useful for preparing hydromorphone and hydrocodone compositions having novel impurity profiles. Compositions comprising hydromorphone and hydrocodone are also disclosed.
摘要翻译：公开了从具有烯丙醇部分的麻醉生物碱制备酮的方法。该方法包括在催化剂存在下将麻醉生物碱与酸混合，其中该方法基本上不存在氢气。该方法可用于制备具有新杂质分布的氢吗啡酮和氢可酮组合物。还公开了包含氢吗啡酮和氢可酮的组合物。

4. 发明授权

US06387917B1 Salts of opioid analgesics, particularly morphine, and methods of using same 有权
标题翻译：阿片类镇痛药，特别是吗啡的盐及其使用方法
公开(公告)号：US06387917B1
公开(公告)日：2002-05-14
申请号：US09692088
申请日：2000-10-19
申请人： Lisbeth Illum , Peter Watts , Ian Lafferty , Alan Smith
发明人： Lisbeth Illum , Peter Watts , Ian Lafferty , Alan Smith
IPC分类号： A61K31485
CPC分类号： C07D489/04
摘要： The methane sulphonate salt of morphine and compositions thereof have medicinal uses, particularly in the treatment of pain. Compositions comprising a methane sulphonate salt of an opioid analgesic also have medicinal uses, adapted for nasal delivery.
摘要翻译：吗啡的甲磺酸盐及其组合物具有药用，特别是用于治疗疼痛。包含阿片类镇痛剂的甲磺酸盐的组合物也具有适于鼻腔输送的药用。

5. 发明授权

US06784186B1 Therapeutic compounds 失效
标题翻译：治疗化合物
公开(公告)号：US06784186B1
公开(公告)日：2004-08-31
申请号：US09582059
申请日：2000-11-20
申请人： Roy W. Jackson , Kamani R. Subasinghe , Alan L. A. Boura
发明人： Roy W. Jackson , Kamani R. Subasinghe , Alan L. A. Boura
IPC分类号： A61K31485
CPC分类号： C07D489/12 , A61K47/54 , C07D489/02
摘要： This invention relates to novel structural analogues and derivatives of compounds with general analgesic or related pharmacological activity. In particular the invention relates to derivatives of opioid compounds, particularly morphine and related compounds, in which an opioid compound is linked via the nitrogen at position 17 to a spacer group, which in turn is linked to a charged group, or a pharmaceutically acceptable salt thereof. In particularly preferred embodiments the opioid compound is morphine, codeine, or buprenorphine.
摘要翻译：本发明涉及具有一般止痛剂或相关药理活性的新型结构类似物和化合物衍生物。特别地，本发明涉及阿片样物质的衍生物，特别是吗啡和相关化合物，其中阿片样物质通过17位的氮连接到间隔基基团上，间隔基团又连接于带电荷的基团或药学上可接受的盐其中。在特别优选的实施方案中，阿片样物质是吗啡，可待因或丁丙诺啡。

6. 发明授权

US06713488B2 Neutral antagonists and use thereof in treating drug abuse 失效
标题翻译：中性拮抗剂及其在治疗药物滥用中的用途
公开(公告)号：US06713488B2
公开(公告)日：2004-03-30
申请号：US10173337
申请日：2002-06-14
申请人： Wolfgang Sadée , Danxin Wang
发明人： Wolfgang Sadée , Danxin Wang
IPC分类号： A61K31485
CPC分类号： A61K31/485
摘要： The invention relates to the use of naltrexone and naloxone analogs, which are neutral antagonists at the &mgr; opioid receptor, for the treatment of drug dependency in a drug-dependent individual. Surprisingly, it has been found that administration of a therapeutically effect amount of the naloxone or naltrexone analogs described herein for the treatment of a drug dependency, can result in reduction of undesirable side effects resulting from current treatments using naloxone and naltrexone. For example, the treatment described herein can result in a reduction in the withdrawal symptoms and aversion encountered in the use of naloxone and naltrexone in the treatment of drug dependency. In addition, the naltrexone and naloxone analogs of the invention can be used for the treatment of pain in an individual in need thereof by modulating opoid pain treatment using neutral antagonists, for example, reversing respiratory depression withough causing other adverse effects. In addition, during chronic use of opioid drugs for pain therapy, neutral antagonists can be used to diminish constipation peripherally without effecting the central analgesic effects.
摘要翻译：本发明涉及在阿片样物质受体中作为中性拮抗剂的纳曲酮和纳洛酮类似物用于治疗依赖于药物的个体的药物依赖性。令人惊奇的是，已经发现，治疗有效量的本文所述的纳洛酮或纳曲酮类似物的给药用于治疗药物依赖性可导致由使用纳洛酮和纳曲酮的当前治疗引起的不希望的副作用的减少。例如，本文所述的治疗可导致使用纳洛酮和纳曲酮治疗药物依赖性时所引起的戒断症状和厌恶的减少。此外，本发明的纳曲酮和纳洛酮类似物可以用于通过使用中性拮抗剂调节类固醇疼痛治疗来治疗有需要的个体的疼痛，例如逆转呼吸抑制而不引起其他副作用。此外，在慢性使用阿片类药物进行疼痛治疗时，中性拮抗剂可用于周边地减少便秘而不影响中枢镇痛作用。

7. 发明授权

US06440987B1 Antipruritic 有权
标题翻译：止痒药
公开(公告)号：US06440987B1
公开(公告)日：2002-08-27
申请号：US09970978
申请日：2001-10-04
申请人： Hiroshi Nagase , Takashi Endoh , Toshiaki Tanaka , Kuniaki Kawamura
发明人： Hiroshi Nagase , Takashi Endoh , Toshiaki Tanaka , Kuniaki Kawamura
IPC分类号： A61K31485
CPC分类号： A61K31/541 , A61K31/40 , A61K31/4025 , A61K31/435 , A61K31/485 , A61K31/5377 , C07D489/00 , C07D489/08
摘要： This invention provides an antipuritic comprising an opiate &kgr; receptor agonist as an effective component, a new morphian quaternary ammonium salt derivative and a new morphian-N-oxide derivative which are useful in treating puritus complicated with some diseases.
摘要翻译：本发明提供了含有鸦片类κ受体激动剂作为有效成分的抗炎药，可用于治疗与某些疾病并发的荨麻疹的新的吗啉季铵盐衍生物和新的吗啉-N-氧化物衍生物。

8. 发明授权

US06703398B2 Orally administered analgesic compositions containing nalbuphine 失效
标题翻译：口服镇痛组合物含有纳布啡
公开(公告)号：US06703398B2
公开(公告)日：2004-03-09
申请号：US09991948
申请日：2001-11-26
申请人： Oliver Yoa-Pu Hu , Cheng-Huei Hsiong
发明人： Oliver Yoa-Pu Hu , Cheng-Huei Hsiong
IPC分类号： A61K31485
CPC分类号： A61K31/485
摘要： The present invention provides orally administered pharmaceutical compositions which contains an effective amount of free base or pharmaceutcially acceptable salts of nalbuphine and/or nalbuphine ester, an oily substance, and a solubility-assisting agent. The oily substance is preferably sesame oil. The solubility-assisting agent is preferably benzyl benzoate. The pharmaceutical composition is useful as an analgesic. The compositions achieves a much higher bioavailability rate and yields much longer lasting effects on nalbuphine than other nalbuphine products currently in the market.
摘要翻译：本发明提供口服给药的药物组合物，其含有有效量的游离碱或药物可接受的纳布啡和/或纳布丁酯的盐，油性物质和溶解性辅助剂。油状物优选为芝麻油。溶解性助剂优选苯甲酸苄酯。药物组合物可用作止痛剂。与目前市场上其他纳布啡组合物相比，组合物达到高得多的生物利用度并且对纳布啡组产生更长时间的持久作用。

9. 发明授权

US06608075B2 Use of methylnaltrexone and related compounds 有权
标题翻译：使用甲基纳曲酮及其相关化合物
公开(公告)号：US06608075B2
公开(公告)日：2003-08-19
申请号：US09862169
申请日：2001-05-21
申请人： Joseph F. Foss , Michael F. Roizen , Jonathan Moss , Chun-Su Yuan , William Drell
发明人： Joseph F. Foss , Michael F. Roizen , Jonathan Moss , Chun-Su Yuan , William Drell
IPC分类号： A61K31485
CPC分类号： A61K31/485
摘要： A method for preventing or treating opioid induced changes in gastrointestinal motility. The method comprises administering methylnaltrexone or another quaternary derivative of noroxymorphone to a patient prior to the administration of an opioid or after the onset of side effects induced by the administration of an opioid, wherein the methylnaltrexone or quaternary derivative is administered orally in an enterically coated form.
摘要翻译：一种预防或治疗阿片样物质诱导胃肠蠕动变化的方法。所述方法包括在施用阿片样物质之前或在施用阿片样物质引起的副作用开始之后向患者施用甲氧基纳曲酮或其他季戊四醇衍生物，其中所述甲基纳曲酮或季衍生物以肠溶包衣形式口服给药。

10. 发明授权

US06316461B1 Antipruritic 有权
标题翻译：止痒药
公开(公告)号：US06316461B1
公开(公告)日：2001-11-13
申请号：US09615540
申请日：2000-07-13
申请人： Hiroshi Nagase , Jun Utsumi , Takashi Endoh , Toshiaki Tanaka , Junzo Kamei , Kuniaki Kawamura
发明人： Hiroshi Nagase , Jun Utsumi , Takashi Endoh , Toshiaki Tanaka , Junzo Kamei , Kuniaki Kawamura
IPC分类号： A61K31485
CPC分类号： A61K31/541 , A61K31/40 , A61K31/4025 , A61K31/435 , A61K31/485 , A61K31/5377 , C07D489/00 , C07D489/08
摘要： This invention provides an antipruritc comprising an opiate &kgr; receptor agonist as an effective component, a new morphinan quaternary ammonium salt derivative and a new morphinan-N-oxide derivative which are useful in treating pruritus complicated with some diseases.
摘要翻译：本发明提供了含有鸦片类κ受体激动剂作为有效成分的止痒剂，新的吗啡喃季铵盐衍生物和新的吗啡喃-N-氧化物衍生物，其可用于治疗与某些疾病并发的瘙痒。

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