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71. 发明授权

US06348465B1 Fructosamine oxidase: antagonists and inhibitors 有权
标题翻译：果糖胺氧化酶：拮抗剂和抑制剂
公开(公告)号：US06348465B1
公开(公告)日：2002-02-19
申请号：US09671967
申请日：2000-09-27
申请人： John Richard Baker
发明人： John Richard Baker
IPC分类号： A61K31495
CPC分类号： A61K31/132 , A61K31/15
摘要： The present invention relates to methods of treating an individual with diabetes mellitus by administering to said individual an effective amount of copper chelators, hydrazine compounds, and/or substrate analogues. The invention also relates to methods of treating an individual with diabetes mellitus by lessening frictosamine odixase activity in said individual. Provided within is disclosure pertaining to treatment, pharmaceutical compositions, dosage ranges, and uses of frictosaminc oxidase enzyme inhibitors to lessen fructosamine oxidase activity.
摘要翻译：本发明涉及通过向所述个体施用有效量的铜螯合剂，肼化合物和/或底物类似物来治疗患有糖尿病的个体的方法。本发明还涉及通过减少所述个体中的氟沙胺奥曲肽酶活性来治疗患有糖尿病的个体的方法。提供关于治疗，药物组合物，剂量范围以及氟虫胺氧化酶抑制剂用于降低果糖胺氧化酶活性的公开内容。

72. 发明授权

US06346533B1 Intraconazole exhibiting an improved solubility, a method of preparing the same and a pharmaceutical composition for oral administration comprising the same 失效
标题翻译：表现出改善的溶解度的内给唑唑，其制备方法和包含其的口服给药药物组合物
公开(公告)号：US06346533B1
公开(公告)日：2002-02-12
申请号：US09445886
申请日：1999-12-14
申请人： Bong-Jin Cha , Jun-Gyo Oh , Su-Eon Kim
发明人： Bong-Jin Cha , Jun-Gyo Oh , Su-Eon Kim
IPC分类号： A61K31495
CPC分类号： C07D405/14 , Y10S514/951
摘要： The particle diameter of itraconazole, insoluble drug, is reduced and crystallinity thereof is changed from crystalline into amorphous, increasing water solubility and a dissolution rate thereof. The improved itraconazole is applied to an oral adminstration drug.
摘要翻译：伊曲康唑，不溶性药物的粒径降低，其结晶度从结晶变为无定形，增加水溶性及其溶解速率。改善的伊曲康唑应用于口服药物。

73. 发明授权

US06344456B1 Piperazinone derivatives and their uses 失效
标题翻译：哌嗪酮衍生物及其用途
公开(公告)号：US06344456B1
公开(公告)日：2002-02-05
申请号：US09743411
申请日：2001-01-10
申请人： Christophe Yue , Marguerite Henry , Thierry Giboulot , Brigitte Lesur
发明人： Christophe Yue , Marguerite Henry , Thierry Giboulot , Brigitte Lesur
IPC分类号： A61K31495
CPC分类号： C07D401/12 , C07D241/08 , C07D405/12 , Y02P20/55
摘要： The invention concerns compounds of formula (I) wherein R1, R2, R3, R4 and R5 are as defined herein. Said compounds are useful in therapy as antithrombotic agents.
摘要翻译：本发明涉及式（I）的化合物，其中R 1，R 2，R 3，R 4和R 5如本文所定义。所述化合物可用于治疗抗血栓形成剂。

74. 发明授权

US06342514B1 Compositions and methods for treating bone deficit conditions 失效
公开(公告)号：US06342514B1
公开(公告)日：2002-01-29
申请号：US08808741
申请日：1997-02-28
申请人： Charles Petrie , Mark W. Orme , Nand Baindur , Kirk G. Robbins , Maria Kontoyianni , Gregory R. Mundy
发明人： Charles Petrie , Mark W. Orme , Nand Baindur , Kirk G. Robbins , Maria Kontoyianni , Gregory R. Mundy
IPC分类号： A61K31495
CPC分类号： A61K31/655 , A61K31/196 , A61K31/4184 , A61K31/428 , A61K31/444 , A61K31/47 , A61K31/4709 , A61K31/498 , A61K31/517 , A61K31/53
摘要： Compounds containing two aromatic systems covalently linked through a linker containing one or more atoms, or “linker” defined as including a covalent bond per se so as to space the aromatic systems at a distance 1.5-15 Å, are effective in treating conditions associated with bone deficits. The compounds can be administered to vertebrate subjects alone or in combination with additional agents that promote bone growth or that inhibit bone resorption. They can be screened for activity prior to administration by assessing their ability to effect the transcription of a reporter gene coupled to a promoter associated with a bone morphogenetic protein and/or their ability to stimulate calvarial growth in model animal systems.

75. 发明授权

US06335331B1 Pseudopolymorphic forms of 2-[2-[4-[Bis (4-fluorophenyl) methyl]-1-piperazinyl]ethoxy]acetic acid dihydrochloride 有权
公开(公告)号：US06335331B1
公开(公告)日：2002-01-01
申请号：US09800665
申请日：2001-03-08
申请人： Monique Berwaer , Guy Bodson , Michel Deleers , Charles Dogimont , Domenico Fanara , Jacques Timmermans
发明人： Monique Berwaer , Guy Bodson , Michel Deleers , Charles Dogimont , Domenico Fanara , Jacques Timmermans
IPC分类号： A61K31495
摘要： The present invention relates to new pseudopolymorphic forms of 2-[2-[4-[bis (4-fluorophenyl)methyl]-1-piperazinyl]ethoxy]acetic acid dihydrochloride, namely, anhydrous 2-[2-[4-[bis(4-fluorophenyl)methyl]-1-piperazinyl]ethoxy]acetic acid dihydrochloride and 2-[2-[4-[bis(4-fluorophenyl)methyl]-1-piperazinyl]ethoxy]acetic acid dihydrochloride monohydrate. It also relates to processes for the preparation of these pseudopolymorphic forms and to pharmaceutical compositions containing them.

76. 发明授权

US06319927B1 Method of using levocetirizine and pharmaceutical compositions containing the same for inducing sleep 失效
标题翻译：使用左西替利嗪的方法和含有它的诱导睡眠的药物组合物
公开(公告)号：US06319927B1
公开(公告)日：2001-11-20
申请号：US09858678
申请日：2001-05-16
申请人： Peter Martin
发明人： Peter Martin
IPC分类号： A61K31495
CPC分类号： A61K9/0043 , A61K31/495
摘要： Disclosed is a method of inducing sleep in a human suffering from a sleeping disorder comprising administering to the human a therapeutically effective amount of cetirizine hydrochloride once daily. Also disclosed is pharmaceutical compositions concerning the same.
摘要翻译：公开了在患有睡眠障碍的人中诱导睡眠的方法，其包括每天向人施用治疗有效量的盐酸西替利嗪。还公开了涉及其的药物组合物。

77. 发明授权

US06303607B1 Method for administering a sustained release ranolanolazine formulation 有权
标题翻译：施用持续释放雷诺拉嗪制剂的方法
公开(公告)号：US06303607B1
公开(公告)日：2001-10-16
申请号：US09321522
申请日：1999-05-27
申请人： Andrew A. Wolff , Fiona Baker , John Richard Langridge
发明人： Andrew A. Wolff , Fiona Baker , John Richard Langridge
IPC分类号： A61K31495
CPC分类号： A61K9/2846 , A61K9/2027 , A61K9/205 , A61K9/2054 , A61K9/2077 , A61K9/2866 , A61K31/495 , A61K31/496 , Y10S514/964
摘要： A sustained release ranolazine formulation contains an intimate mixture of ranolazine and a partially neutralized pH-dependent binder to form a film that is mostly insoluble in aqueous media below pH 4.5 and soluble in aqueous media above pH 4.5. The formulation is suitable for twice daily administration of ranolazine and is useful for controlling the rate of dissolution of ranolazine, and to maintain human plasma ranolazine levels at between 550 and 7500 ng base/mL.
摘要翻译：持续释放的雷诺拉嗪制剂含有雷诺嗪和部分中和的pH依赖性粘合剂的紧密混合物，以形成大部分不溶于低于pH4.5的水性介质中并可溶于高于pH 4.5的水性介质中的膜。该制剂适用于每日两次给予雷诺嗪，并且可用于控制雷诺嗪的溶出速率，并维持人血浆雷诺嗪水平在550至7500ng / mL之间。

78. 发明授权

US06300332B1 Methods for reducing respiratory depression and attendant side effects of mu opioid compounds 失效
标题翻译：减少呼吸抑制和阿片样物质副作用的方法
公开(公告)号：US06300332B1
公开(公告)日：2001-10-09
申请号：US09352308
申请日：1999-07-12
申请人： Kwen-Jen Chang , Robert W. McNutt, Jr. , Hugh O. Pettit , Michael J. Bishop
发明人： Kwen-Jen Chang , Robert W. McNutt, Jr. , Hugh O. Pettit , Michael J. Bishop
IPC分类号： A61K31495
CPC分类号： A61K31/495 , A61K31/00 , A61K31/40 , A61K31/445 , A61K31/485 , A61K31/496 , A61K31/55 , A61K45/06 , C07D295/096 , C07D295/155 , A61K2300/00
摘要： A method of reducing, treating or preventing drug-mediated respiratory depression, muscle rigidity, or nausea/vomiting in an animal, incident to the administration to said animal of a mixed delta/mu opioid agonist or a respiratory depression-mediating drug, comprising administering to the animal receiving said drug an effective amount of a delta receptor agonist compound.
摘要翻译：一种减少，治疗或预防动物中药物介导的呼吸抑制，肌肉僵硬或恶心/呕吐的方法，该方法是向所述动物施用混合的δ/μ阿片样物质激动剂或呼吸抑制介导药物，包括施用给予接受所述药物的动物有效量的δ受体激动剂化合物。

79. 发明授权

US06291462B1 Oral medicinal preparations with reproducible release of the active ingredient gatifloxacin or its pharmaceutically suitable salts or hydrates 失效
标题翻译：具有可重复释放活性成分加替沙星或其药学上合适的盐或水合物的口服药物制剂
公开(公告)号：US06291462B1
公开(公告)日：2001-09-18
申请号：US09700055
申请日：2001-02-16
申请人： Johannes Bartholomaeus , Juergen Betzing
发明人： Johannes Bartholomaeus , Juergen Betzing
IPC分类号： A61K31495
CPC分类号： A61K9/2054 , A61K31/4709
摘要： Solid medicinal forms having a multiphase structure for oral administration, containing gatifloxacin or pharmaceutically acceptable salts or hydrates thereof and auxiliary substances selected from the group of fillers, binders, lubricants, disintegration aids and mixtures thereof, in which the inner phase contains the active ingredient gatifloxacin or pharmaceutically acceptable salts or hydrates thereof and auxiliary substances from the group of binders, fillers, disintegration aids and mixtures thereof, and at least one outer phase necessarily contains at least one disintegration aid and further auxiliary substances from the group of at least one lubricant, optionally fillers and/or optionally binders, and a process for the preparation of such solid medicinal forms.
摘要翻译：包含加替沙星或其药学上可接受的盐或水合物的多相结构的固体药物形式和选自填充剂，粘合剂，润滑剂，崩解助剂及其混合物的辅助物质，其中内相含有活性成分加替沙星或其药学上可接受的盐或水合物和来自粘合剂组，填料，崩解助剂及其混合物的辅助物质，并且至少一个外相必须含有至少一种崩解助剂和来自至少一种润滑剂组的其它辅助物质，任选的填料和/或任选的粘合剂，以及制备这种固体药物形式的方法。

80. 发明授权

US06291461B1 Stephacidin antitumor antibiotics 有权
标题翻译：杀草素抗肿瘤药
公开(公告)号：US06291461B1
公开(公告)日：2001-09-18
申请号：US09391131
申请日：1999-09-07
申请人： Jingfang Qian Cutrone , Kimberly D. Krampitz , Yue-Zhong Shu , Li-Ping Chang , Susan E. Lowe
发明人： Jingfang Qian Cutrone , Kimberly D. Krampitz , Yue-Zhong Shu , Li-Ping Chang , Susan E. Lowe
IPC分类号： A61K31495
CPC分类号： C07D471/18 , C07D519/00
摘要： The novel antitumor antibiotics designated stephacidin A and stephacidin B are produced by fermentation of Aspergillus ochraceus ATCC-74432. The antibiotics inhibit the growth of mammalian tumors, including particularly prostate carcinoma.
摘要翻译：命名为杀青霉素A和间歇杀菌素B的新型抗肿瘤抗生素通过发酵赭曲霉ATCC-74432产生。抗生素抑制哺乳动物肿瘤的生长，特别是前列腺癌。

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