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公开(公告)号：US06306891B1
公开(公告)日：2001-10-23
申请号：US09323519
申请日：1999-06-01
申请人： Harold G. Selnick , Melissa Egbertson , Daria Jean Hazuda , James P. Guare, Jr. , John S. Wai , Steven D. Young , David L. Clark , Julio C. Medina
发明人： Harold G. Selnick , Melissa Egbertson , Daria Jean Hazuda , James P. Guare, Jr. , John S. Wai , Steven D. Young , David L. Clark , Julio C. Medina
IPC分类号： A61K3140
CPC分类号： A61K45/06 , A61K31/40 , A61K31/445 , A61K2300/00
摘要： Nitrogen-containing heteroaryl dioxo-butyric acid derivatives are described as inhibitors of HIV integrase and inhibitors of HIV replication. These compounds are useful in 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 AIDS and methods of preventing or treating infection by HIV are also described.
摘要翻译： 含氮杂芳基二氧代丁酸衍生物被描述为HIV整合酶的抑制剂和HIV复制抑制剂。 这些化合物可用于预防或治疗HIV的感染和治疗AIDS，无论是化合物，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，抗生素或疫苗结合使用。 还描述了治疗艾滋病的方法和预防或治疗HIV感染的方法。
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公开(公告)号：US06380249B1
公开(公告)日：2002-04-30
申请号：US09323417
申请日：1999-06-01
申请人： Steven D. Young , Melissa Egbertson , Linda S. Payne , John S. Wai , Thorsten E. Fisher , James P. Guare, Jr. , Mark W. Embrey , Lekhanh Tran , Linghang Zhuang , Joseph P. Vacca , H. Marie Langford , Jeffrey Melamed , Juan C. Jaen , David L. Clark , Julio C. Medina
发明人： Steven D. Young , Melissa Egbertson , Linda S. Payne , John S. Wai , Thorsten E. Fisher , James P. Guare, Jr. , Mark W. Embrey , Lekhanh Tran , Linghang Zhuang , Joseph P. Vacca , H. Marie Langford , Jeffrey Melamed , Juan C. Jaen , David L. Clark , Julio C. Medina
IPC分类号： A61K31215
CPC分类号： C07D213/64 , C07C59/84 , C07C59/86 , C07C59/88 , C07C59/90 , C07C69/738 , C07C217/60 , C07C229/34 , C07C229/42 , C07C233/63 , C07C235/60 , C07C255/41 , C07C271/16 , C07C271/28 , C07C323/62 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2602/08 , C07C2602/10 , C07D209/12 , C07D241/12 , C07D253/08 , C07D263/58 , C07D295/088 , C07D295/155 , C07D295/192 , C07D333/22
摘要： Certain six-membered aromatic and heteroaromatic-dioxobutyric acid derivatives are described as inhibitors of HIV integrase and inhibitors of HIV replication. These compounds are useful in 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 AIDS and methods of preventing or treating infection by HIV are also described.
摘要翻译： 某些六元芳族和杂芳族二氧代丁酸衍生物被描述为HIV整合酶的抑制剂和HIV复制的抑制剂。 这些化合物可用于预防或治疗HIV的感染和治疗AIDS，无论是化合物，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，抗生素或疫苗结合使用。 还描述了治疗艾滋病的方法和预防或治疗HIV感染的方法。
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公开(公告)号：US4686226A
公开(公告)日：1987-08-11
申请号：US771927
申请日：1985-09-03
IPC分类号： A61K31/435 , A61P1/00 , A61P3/04 , A61P3/08 , A61P7/02 , A61P9/12 , A61P25/02 , A61P25/24 , A61P25/26 , C07D455/06 , C07D471/14 , C07D491/14 , C07D491/147 , C07D495/14 , A61K31/38
CPC分类号： C07D471/14 , C07D455/06 , C07D491/14 , C07D495/14
摘要： Substituted hexahydro arylquinolizines and pharmaceutically acceptable salts thereof are selective .alpha..sub.2 -adrenergic receptor antagonists and thereby useful as antidepressants, antihypertensives, ocular antihypertensives, antidiabetics, antiobesity and platelet aggregation inhibitors and modifiers of gastrointestinal motility.
摘要翻译： 取代的六氢芳基喹啉及其药学上可接受的盐是选择性α2-肾上腺素能受体拮抗剂，从而可用作抗抑郁药，抗高血压药，眼用抗高血压药，抗糖尿病药，抗肥胖药和血小板聚集抑制剂和胃肠运动性调节剂。
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4.发明授权Anti-depressant spiro hexahydro arylquinolizine derivatives, composition, and method of use therefor 失效抗抑郁螺旋六氢芳基喹啉衍生物，组合物及其用途
公开(公告)号：US4710504A
公开(公告)日：1987-12-01
申请号：US848262
申请日：1986-04-04
申请人： John J. Baldwin , Joel R. Huff , Joseph P. Vacca , Steven D. Young , Jane deSolms , James P. Guare, Jr.
发明人： John J. Baldwin , Joel R. Huff , Joseph P. Vacca , Steven D. Young , Jane deSolms , James P. Guare, Jr.
IPC分类号： C07D471/20 , C07D491/22 , C07D495/22 , C07D498/22 , C07D513/22 , A61K31/415 , A61K31/305 , C07D455/00
CPC分类号： C07D471/20 , C07D491/22 , C07D495/22 , C07D498/22 , C07D513/22
摘要： Substituted hexahydro arylquinolizines and pharmaceutically acceptable salts thereof are selective .alpha..sub.2 -adrenergic receptor antagonists and thereby useful as antidepressants, antihypertensives, ocular antihypertensives, antidiabetics, platelet aggregation inhibitors, antiobesity agents, and modifiers of gastrointestinal motility.
摘要翻译： 取代的六氢芳基喹啉及其药学上可接受的盐是选择性α2-肾上腺素能受体拮抗剂，因此可用作抗抑郁药，抗高血压药，眼用抗高血压药，抗糖尿病药，血小板聚集抑制剂，抗肥胖剂和消化道运动性改良剂。
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5.发明申请Novel Lipid Nanoparticles and Novel Components for Delivery of Nucleic Acids 审中-公开新型脂质纳米颗粒和用于递送核酸的新型组分公开(公告)号：US20110224447A1
公开(公告)日：2011-09-15
申请号：US13059491
申请日：2009-08-11
申请人： Keith A. Bowman , James P. Guare, JR. , George D. Hartman , Rubina G. Parmar , Chandra Vargeese , Weimin Wang , Ye Zhang
发明人： Keith A. Bowman , James P. Guare, JR. , George D. Hartman , Rubina G. Parmar , Chandra Vargeese , Weimin Wang , Ye Zhang
IPC分类号： C07J9/00 , A61K31/713 , A61P1/16
CPC分类号： A61K9/5123 , A61K9/1272 , A61K9/1277 , A61K9/5192 , A61K47/28 , C07C217/42
摘要： The instant invention provides for novel lipid nanoparticles and novel lipid nanoparticle components (specifically cationic lipids) that are useful for the delivery of nucleic acids, specifically siRNA, for therapeutic purposes.
摘要翻译： 本发明提供新颖的脂质纳米颗粒和新颖的脂质纳米颗粒组分（特别是阳离子脂质），其可用于递送核酸，特别是用于治疗目的的siRNA。
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公开(公告)号：US5968938A
公开(公告)日：1999-10-19
申请号：US86107
申请日：1998-05-29
IPC分类号： C07D211/46 , C07D211/96 , C07D213/74 , C07D235/06 , C07D239/42 , C07D241/20 , C07D295/185 , A61K31/495 , C07D401/12 , C07D403/12
CPC分类号： C07D213/74 , C07D211/46 , C07D211/96 , C07D235/06 , C07D239/42 , C07D241/20 , C07D295/185
摘要： This invention relates to certain novel piperazine compounds and derivatives thereof, their synthesis, and their use as oxytocin receptor antagonists. One application of these compounds is in the treatment of preterm labor in mammals, especially humans. The ability of the compounds to relax uterine contractions in mammals also makes them useful for treating dysmenorrhea and stopping labor prior to cesarean delivery.
摘要翻译： 本发明涉及某些新的哌嗪化合物及其衍生物，其合成及其作为催产素受体拮抗剂的用途。 这些化合物的一种应用是在哺乳动物，特别是人类中治疗早产。 化合物放松哺乳动物子宫收缩的能力也使它们可用于治疗痛经并在剖宫产分娩前停止劳动。
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7.发明授权
公开(公告)号：US5939414A
公开(公告)日：1999-08-17
申请号：US959264
申请日：1997-10-28
申请人： Ian M. Bell , Daria Jean Hazuda , James P. Guare, Jr. , Peter M. Munson , Wayne J. Thompson , Joseph P. Vacca
发明人： Ian M. Bell , Daria Jean Hazuda , James P. Guare, Jr. , Peter M. Munson , Wayne J. Thompson , Joseph P. Vacca
IPC分类号： A61K31/5513 , C07D243/20 , C07D403/12 , A61K31/55 , C07D243/14
CPC分类号： C07D403/12 , A61K31/5513 , C07D243/20
摘要： Compounds having a benzodiazepine hydrazide core are described. These compounds are useful in the inhibition of HIV integrase, 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 AIDS and methods of preventing or treating infection by HIV are also described.
摘要翻译： 描述了具有苯并二氮杂肼核心的化合物。 这些化合物可用作抑制HIV整合酶，预防或治疗HIV感染和治疗AIDS，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，抗生素或其他抗生素组合使用 疫苗。 还描述了治疗艾滋病的方法和预防或治疗HIV感染的方法。
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公开(公告)号：US4824849A
公开(公告)日：1989-04-25
申请号：US90641
申请日：1987-08-28
申请人： John J. Baldwin , Joel R. Huff , Joseph P. Vacca , Steven D. Young , Jane deSolms , James P. Guare, Jr.
发明人： John J. Baldwin , Joel R. Huff , Joseph P. Vacca , Steven D. Young , Jane deSolms , James P. Guare, Jr.
IPC分类号： C07D471/20 , C07D471/22 , C07D491/22 , C07D495/22 , C07D498/22 , C07D513/22 , A61K31/415 , A61K31/305 , C07D455/00
CPC分类号： C07D471/20 , C07D471/22 , C07D491/22 , C07D495/22 , C07D498/22 , C07D513/22
摘要： Substituted hexahydro arylquinolizines and pharmaceutically acceptable salts thereof are selective .alpha..sub.2 -adrenergic receptor antagonists and thereby useful as antidepressants, antihypertensives, ocular antihypertensives, antidiabetics, platelet aggregation inhibitors, antiobesity agents, and modifiers of gastrointestinal motility.
摘要翻译： 取代的六氢芳基喹啉及其药学上可接受的盐是选择性α2-肾上腺素能受体拮抗剂，因此可用作抗抑郁药，抗高血压药，眼用抗高血压药，抗糖尿病药，血小板聚集抑制剂，抗肥胖剂和消化道运动性改良剂。
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