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公开(公告)号：US5733907A
公开(公告)日：1998-03-31
申请号：US622945
申请日：1996-03-27
IPC分类号： C07D401/06 , A61K31/495 , A61P31/12 , A61P37/04 , C07D213/38 , A61K31/535 , C07D413/14
CPC分类号： C07D213/38
摘要： Prodrugs of the HIV protease inhibitor L-735,524 are useful in the inhibition of HIV protease, the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating ADS and methods of preventing or treating infection by HIV are also described.
摘要翻译： HIV蛋白酶抑制剂L-735,524的前药可用于抑制HIV蛋白酶，预防或治疗HIV感染和治疗艾滋病，作为化合物，药学上可接受的盐，药物组合物成分，无论是否与 其他抗病毒药，免疫调节剂，抗生素或疫苗。 还描述了治疗ADS的方法和预防或治疗HIV感染的方法。
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公开(公告)号：US5961483A
公开(公告)日：1999-10-05
申请号：US878493
申请日：1997-06-18
IPC分类号： A61K9/00 , A61K9/70 , A61K31/42 , A61K31/4439 , A61K31/4545 , A61N1/30
CPC分类号： A61K31/4545 , A61K31/42 , A61K31/4439 , A61K9/0009
摘要： This invention relates to novel methods and devices for iontophoretically administering therapeutic doses of cell adhesion receptor antagonists in a controlled manner through the skin. Such antagonist compounds include but are not limited to antagonists of the IIb/IIIa and .alpha..sub.v .beta..sub.3 integrins and related cell surface adhesive protein receptors. The present invention includes iontophoretic delivery devices comprising cell adhesion receptor antagonists. Such methods and devices are useful, alone or in combination with other therapeutic agents, for the treatment of thromboembolic disorders, angiogenic disorders, inflammation, bone degradation, cancer metastasis, diabetic retinopathy, restenosis, macular degeneration, and other conditions mediated by cell adhesion and/or cell migration and/or angiogenesis.
摘要翻译： 本发明涉及以受控方式通过皮肤离子电渗施用治疗剂量的细胞粘附受体拮抗剂的新方法和装置。 这种拮抗剂化合物包括但不限于IIb / IIIa和αvβ3整联蛋白和相关细胞表面粘附蛋白受体的拮抗剂。 本发明包括包含细胞粘附受体拮抗剂的离子电渗疗法递送装置。 这些方法和装置单独或与其它治疗剂组合用于治疗血栓栓塞障碍，血管生成障碍，炎症，骨退化，癌转移，糖尿病性视网膜病变，再狭窄，黄斑变性和由细胞粘附介导的其它病症， /或细胞迁移和/或血管发生。
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公开(公告)号：US4910314A
公开(公告)日：1990-03-20
申请号：US301843
申请日：1989-01-26
申请人： Pierre M. R. de Montigny , Larry A. Sternson , Arnold J. Repta , John F. Stabaugh , Takeru Higuchi, deceased , by Martin B. Dickinson, Jr., co-executor , by Kenji W. Higuchi, co-executor
发明人： Pierre M. R. de Montigny , Larry A. Sternson , Arnold J. Repta , John F. Stabaugh , Takeru Higuchi, deceased , by Martin B. Dickinson, Jr., co-executor , by Kenji W. Higuchi, co-executor
CPC分类号： G01N33/52 , G01N33/6809
摘要： There is provided a fluorescent adduct which is amenable to detection by fluorometric and electrochemical techniques. The adduct is of the formula: ##STR1## wherein X is a radical derived from a primary amine of the formula X--NH.sub.2 and where R.sub.1 --R.sub.6 are selected from various organic or inorganic substituents.
摘要翻译： 提供荧光加合物，其可以通过荧光和电化学技术进行检测。 加合物具有下式：其中X是衍生自式X-NH 2伯胺的基团，其中R 1 -R 6选自各种有机或无机取代基。
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公开(公告)号：US06185453B2
公开(公告)日：2001-02-06
申请号：US08877829
申请日：1997-06-18
申请人： Munir A. Hussain , Arnold J. Repta
发明人： Munir A. Hussain , Arnold J. Repta
IPC分类号： A61N130
CPC分类号： A61K31/4545 , A61K9/0009 , A61K31/42 , A61K31/4439 , A61N1/0428 , A61N1/0436 , A61N1/0448
摘要： This invention relates to novel methods and devices for iontophoretically administering therapeutic doses of integrin receptor antagonists in a controlled manner through the skin. Such integrin receptor antagonists include but are not limited to antagonists of the IIb/IIIa and &agr;v&bgr;3 integrins and related cell surface adhesive protein receptors. The present invention includes iontophoretic delivery devices comprising integrin inhibitors. Such methods and devices are useful, alone or in combination with other therapeutic agents, for the treatment of thromboembolic disorders, angiogenic disorders, inflammation, bone degradation, cancer metastasis, diabetic retinopathy, restenosis, macular degeneration, and other conditions mediated by cell adhesion and/or cell migration and/or angiogenesis.
摘要翻译： 本发明涉及以受控方式通过皮肤离子电渗治疗施用治疗剂量的整联蛋白受体拮抗剂的新方法和装置。 这样的整联蛋白受体拮抗剂包括但不限于IIb / IIIa和alphavbeta3整联蛋白和相关的细胞表面粘附蛋白受体的拮抗剂。 本发明包括包含整联蛋白抑制剂的离子电渗疗法递送装置。 这些方法和装置单独或与其它治疗剂组合用于治疗血栓栓塞障碍，血管生成障碍，炎症，骨退化，癌转移，糖尿病性视网膜病变，再狭窄，黄斑变性和由细胞粘附介导的其它病症， /或细胞迁移和/或血管生成。
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公开(公告)号：US06649187B2
公开(公告)日：2003-11-18
申请号：US10074385
申请日：2002-02-12
申请人： Munir A. Hussain , Arnold J. Repta
发明人： Munir A. Hussain , Arnold J. Repta
IPC分类号： A61K924
CPC分类号： A61K31/496 , A61K9/0004 , A61K9/2031
摘要： The invention provides a method and device for administering an amine drug, such as [S-(R,S)]-2-[4-[[(4-methyl)piperazin-1-yl]carbonyl]phenoxy]-3,3-diethyl-N-[1-(3,4-methylenedioxyphenyl)butyl]-4-oxo-1-azetidinecarboxamide), in a sustained release dosage form. The invention includes a pharmaceutical composition and dosage form containing a polyalkylamine polymer and an amine drug. The polyalkylamine polymer is a hydrogel that forms hydrated particles when exposed to an aqueous environment. When mixed with the amine drug in the core of a coated tablet, the polyalkylamine polymer controls the release of the amine drug into an aqueous environment of use. The hydrated particles of the polymer together with the amine drug are released from the tablet core through plural apertures in the surrounding coat.
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公开(公告)号：US4684630A
公开(公告)日：1987-08-04
申请号：US720035
申请日：1985-04-04
申请人： Arnold J. Repta , Parviz Mojaverian
发明人： Arnold J. Repta , Parviz Mojaverian
CPC分类号： A61K31/70 , A61K47/18 , A61K47/20 , A61K9/0019 , Y10S514/936
摘要： A method of parenterally delivering aqueously unstable drugs that includes the aqueous dilution of a stable, anhydrous organic solution having the drug dissolved therein. The resulting organic-aqueous solution is physiologically suitable for parenteral delivery into a warm-blooded mammal and contains the drug in an effective dosage concentration per unit volume.
摘要翻译： 肠胃外输送不稳定药物的方法，其包括溶解有药物的稳定的无水有机溶液的水稀释液。 所得的有机 - 水溶液在生理学上适合于肠胃外输送到温血哺乳动物中并且含有每单位体积有效剂量浓度的药物。
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公开(公告)号：US3943137A
公开(公告)日：1976-03-09
申请号：US377401
申请日：1973-07-09
IPC分类号： C07D491/04 , C07D491/052
CPC分类号： C07D491/052
摘要： Acronycine derivatives having the structural formula: ##SPC1##Wherein R is acyl and A is an anion of a suitably strong acid, stabilized formulations thereof and pharmaceutical compositions comprised of same exhibit broad spectrum antitumor activity, and are especially suited for intravenous administration.
摘要翻译： 具有以下结构式的顺铂衍生物：
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公开(公告)号：US06214834B1
公开(公告)日：2001-04-10
申请号：US09049305
申请日：1998-03-27
IPC分类号： C07D23156
CPC分类号： C07D401/12 , C07D403/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D471/04
摘要： This invention relates to novel heterocycles which are useful as antagonists of the &agr;v&bgr;3 integrin and related cell surface adhesive protein receptors, to pharmaceutical compositions containing such compounds, to iontophoretic delivery of such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of cell adhesion, the treatment of angiogenic disorders, inflammation, bone degradation, cancer metastasis, diabetic retinopathy, thrombosis, restenosis, macular degeneration, and other conditions mediated by cell adhesion and/or cell migration and/or angiogenesis.
摘要翻译： 本发明涉及可用作αphavbeta3整联蛋白和相关细胞表面粘附蛋白受体的拮抗剂的新型杂环，含有这些化合物的药物组合物，这些化合物的离子电渗疗法，以及单独或与 用于抑制细胞粘附，血管生成障碍的治疗，炎症，骨退化，癌症转移，糖尿病性视网膜病变，血栓形成，再狭窄，黄斑变性和由细胞粘附和/或细胞迁移介导的其它病症和/或 血管生成。
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公开(公告)号：US5376383A
公开(公告)日：1994-12-27
申请号：US13111
申请日：1993-02-01
IPC分类号： A61K9/00 , A61K9/20 , A61K31/00 , A61K31/215 , A61K31/22 , A61K31/365 , A61K9/24
CPC分类号： A61K31/22 , A61K31/00 , A61K31/215 , A61K31/365 , A61K9/0004 , A61K9/2054
摘要： The instant invention is directed to a method for enhancing the lowering of plasma cholesterol level in a subject in need thereof which comprises the time-controlled administration of a nontoxic therapeutically effective amount of an HMG-CoA reductase inhibitor to said subject which surprisingly affords an equivalent or improved reduction of plasma cholesterol levels while significantly reducing the amount of HMG-CoA reductase inhibitor circulating in the bloodstream of the subject as compared to the same parameters when the oral administration of a conventional rapid release dosage form is utilized.
摘要翻译： 本发明涉及用于增强有需要的受试者中血浆胆固醇水平降低的方法，其包括将无毒治疗有效量的HMG-CoA还原酶抑制剂时间控制施用于所述受试者，令人惊讶地提供相当于 或者当使用常规的快速释放剂型的口服给药时，与相同的参数相比，血浆胆固醇水平的改善降低，同时显着减少在受试者的血液中循环的HMG-CoA还原酶抑制剂的量。
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公开(公告)号：US4997658A
公开(公告)日：1991-03-05
申请号：US274173
申请日：1988-11-21
IPC分类号： A61K9/00 , A61K9/28 , A61K31/00 , A61K31/215 , A61K31/365 , A61K45/00 , A61K45/08 , A61M37/00 , A61P3/06 , A61P9/10 , A61P43/00
CPC分类号： A61K9/0004 , A61K31/00 , A61K31/215 , A61K31/365
摘要： The instant invention is directed to a method for enhancing the lowering of plasma cholesterol level in a subject in need thereof which comprises the time-controlled administration of a nontoxic therapeutically effective amount of an HMG-CoA reductase inhibitor to said subject which surprisingly affords an equivalent or improved reduction of plasma cholesterol levels while significantly reducing the amount of HMG-CoA reductase inhibitor circulating in the bloodstream of the subject as compared to the same parameters when the oral administration of a conventional rapid release dosage form is utilized.
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