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公开(公告)号：US5633231A
公开(公告)日：1997-05-27
申请号：US301506
申请日：1994-09-07
申请人： Dieter Habich , Thomas J. Schulze , Jurgen Reefschlager , Jutta Hansen , Rainer Neumann , Gert Streissle , Arnold Paessens
发明人： Dieter Habich , Thomas J. Schulze , Jurgen Reefschlager , Jutta Hansen , Rainer Neumann , Gert Streissle , Arnold Paessens
IPC分类号： A61K38/00 , A61P31/12 , C07D209/42 , C07D213/30 , C07D213/56 , C07D213/70 , C07D215/14 , C07D215/48 , C07D241/24 , C07D241/46 , C07D249/06 , C07K1/113 , C07K5/068 , C07K5/072 , C07K5/09 , C07K5/097 , C07D241/04 , C07D211/06
CPC分类号： C07D213/30 , C07D209/42 , C07D213/56 , C07D213/70 , C07D215/14 , C07D215/48 , C07D241/24 , C07D241/46 , C07D249/06 , C07K5/06095 , C07K5/0821 , A61K38/00
摘要： The present invention relates to valine-containing, substituted pseudopeptides of the general formula (I) ##STR1## in which the substituents have the meaning given in the description, to processes for their preparation, and to their use as anti-viral agents, in particular against cytomegaloviruses.
摘要翻译： 本发明涉及含缬氨酸的通式（I）的取代假肽，其中取代基具有本说明书中给出的含义，其制备方法及其作为抗病毒剂的用途 药剂，特别是抗巨细胞病毒。
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公开(公告)号：US5646121A
公开(公告)日：1997-07-08
申请号：US302064
申请日：1994-09-07
申请人： Dieter Habich , Thomas-J. Schulze , Jurgen Reefschlager , Jutta Hansen , Rainer Neumann , Gert Streissle , Arnold Paessens
发明人： Dieter Habich , Thomas-J. Schulze , Jurgen Reefschlager , Jutta Hansen , Rainer Neumann , Gert Streissle , Arnold Paessens
IPC分类号： C07D249/06 , A61K38/00 , A61P31/12 , C07C237/22 , C07C271/10 , C07C275/28 , C07C279/02 , C07C279/14 , C07C311/64 , C07C317/44 , C07D213/24 , C07D213/81 , C07D215/48 , C07D311/70 , C07D333/70 , C07K1/02 , C07K1/10 , C07K1/113 , C07K1/12 , C07K5/068 , C07K5/072 , C07K5/087 , C07K5/09 , C07K5/093 , C07K5/097 , C07D241/04 , A61K31/16 , A61K31/165 , C07D211/06
CPC分类号： C07K5/0817 , C07C311/64 , C07K5/06095 , A61K38/00
摘要： The present invention relates to novel pseudopeptides with antiviral activity of the general formula (I) ##STR1## in which the substituents have the meaning given in the description, to a process for their preparation, and to their use as antiviral agents, especially against cytomegaloviruses.
摘要翻译： 本发明涉及具有通式（I）（I）的抗病毒活性的新型伪肽，其中取代基具有本说明书中给出的含义，其制备方法及其作为抗病毒剂的用途， 特别是针对巨细胞病毒。
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公开(公告)号：US5492896A
公开(公告)日：1996-02-20
申请号：US196939
申请日：1994-02-15
申请人： Dieter Habich , Michael Matzke , Klaus Frobel , Thomas Henkel , Hartwig Muller , Karl-Heinz Weber , Jurgen Reefschlager , Gert Streissle , Jutta Hansen , Rainer Neumann , Arnold Paessens
发明人： Dieter Habich , Michael Matzke , Klaus Frobel , Thomas Henkel , Hartwig Muller , Karl-Heinz Weber , Jurgen Reefschlager , Gert Streissle , Jutta Hansen , Rainer Neumann , Arnold Paessens
IPC分类号： A61K38/00 , A61P31/12 , C07K1/02 , C07K1/113 , C07K5/02 , C07K5/06 , C07K5/072 , C07K5/08 , C07K5/09 , C07K14/81 , C07K5/00 , C07K7/00 , C07K17/00
CPC分类号： C07K5/0817 , C07K5/0217 , C07K5/06095 , A61K38/00
摘要： The invention relates to new pseudopeptides having an antiviral action, oft he general formula (I) ##STR1## with the meanings given in the description for the substituents, to a process for their preparation and to their use as antiviral agents, in particular against cytomegaloviruses.
摘要翻译： 本发明涉及具有抗病毒作用的新的假肽，其通式（I）为取代基，其制备方法及其作为抗病毒剂，特别是针对巨细胞病毒的用途。
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公开(公告)号：US5430151A
公开(公告)日：1995-07-04
申请号：US920216
申请日：1992-07-24
申请人： Dieter Habich , Wolfgang Roben , Jutta Hansen , Arnold Paessens
发明人： Dieter Habich , Wolfgang Roben , Jutta Hansen , Arnold Paessens
IPC分类号： A61K31/16 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/435 , A61K31/4427 , A61K31/445 , A61K31/47 , A61K31/535 , A61K31/5375 , A61K31/66 , A61K38/00 , A61P31/12 , A61P31/18 , C07C237/22 , C07C271/22 , C07C317/44 , C07D207/08 , C07D209/42 , C07D211/18 , C07D215/12 , C07D217/14 , C07D295/16 , C07D295/18 , C07D401/12 , C07F9/40 , C07F9/572 , C07F9/59 , C07F9/62 , C07K5/06 , C07K5/08 , C07K5/083 , C07D211/06 , C07D207/04
CPC分类号： C07D207/08 , C07C317/44 , C07D211/18 , C07D217/14 , C07K5/06191 , C07K5/081 , C07K5/0827 , A61K38/00
摘要： The present invention relates to new trifluoromethyl-containing pseudopeptides of the general formula (I) ##STR1## in which W, A, B, D, E, R.sub.1, R.sub.2 and R.sub.3 have the meaning as outlined of their making and use as pharmaceuticals.
摘要翻译： 本发明涉及通式（I）的新的含三氟甲基的伪肽，其中W，A，B，D，E，R 1，R 2和R 3具有其制备和使用概述的含义 作为药物。
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5.发明授权Dithiolanylglycine-containing HIV protease inhibitors of the hydroxyethylene isostere type 失效含二硫醇基甘氨酸的HIV蛋白酶抑制剂是羟基乙烯异构体型
公开(公告)号：US5424426A
公开(公告)日：1995-06-13
申请号：US59488
申请日：1993-05-10
申请人： Dieter Habich , Wolfgang Bender , Jutta Hansen , Arnold Paessens
发明人： Dieter Habich , Wolfgang Bender , Jutta Hansen , Arnold Paessens
IPC分类号： A61K31/44 , A61K31/385 , A61K31/4433 , A61K31/445 , A61K31/47 , A61K38/00 , A61K38/55 , A61P31/12 , A61P31/18 , C07D215/48 , C07D339/06 , C07D409/12 , C07D409/14 , C07K5/02 , C07K5/03
CPC分类号： C07D409/12 , C07D409/14 , C07K5/0207 , A61K38/00
摘要： The invention relates to dithiolanylglycine-containing HIV protease inhibitors of the hydroxyethylene isostere type of the general formula (I) ##STR1## processes for their preparation and their use as retroviral agents.
摘要翻译： 本发明涉及通式（I）的羟基亚乙基异构体类型的二硫醇基甘氨酸的HIV蛋白酶抑制剂，其制备及其用作逆转录病毒剂。
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6.发明授权Use of substituted chromans, some of which are known, as medicaments, new active compounds and processes for their preparation 失效取代的苯并二氢吡喃酮（其中一些已知的）用作药物，新的活性化合物及其制备方法
公开(公告)号：US5492918A
公开(公告)日：1996-02-20
申请号：US251986
申请日：1994-06-01
申请人： Hanno Wild , Wolfgang Bender , Dieter Habich , Hans-Georg Heine , Siegfried Raddatz , Wolfgang Roben , Jutta Hansen , Arnold Paessens
发明人： Hanno Wild , Wolfgang Bender , Dieter Habich , Hans-Georg Heine , Siegfried Raddatz , Wolfgang Roben , Jutta Hansen , Arnold Paessens
IPC分类号： A61K31/443 , A61K31/445 , A61P31/12 , C07D405/06 , C07D405/14
CPC分类号： C07D405/06 , C07D405/14
摘要： The present invention relates to the use of substituted chromans of the general formula (I) ##STR1## in which the substituents have the meaning indicated in the description, for the production of medicaments, in particular as HIV protease-inhibiting agents, new active compounds and processes for their preparation.
摘要翻译： 本发明涉及通式（I）的取代苯并二氢吡喃的用途，其中取代基具有说明书中指出的含义，用于生产药物，特别是作为HIV蛋白酶抑制剂，新的活性化合物 及其制备方法。
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7.发明授权Phosphonopyrrolidine- and piperidine-containing pseudopeptides of the statin type, a process for their preparation and their use as medicaments against retroviruses 失效苯妥英类和苯哌啶类药物的类型，其制备方法及其作为抗逆转录病毒药物使用的方法
公开(公告)号：US5147865A
公开(公告)日：1992-09-15
申请号：US746272
申请日：1991-08-15
申请人： Dieter Habich , Jutta Hansen , Arnold Paessens
发明人： Dieter Habich , Jutta Hansen , Arnold Paessens
IPC分类号： A61K31/675 , A61K38/00 , A61P31/12 , A61P31/18 , C07F9/572 , C07F9/59 , C07K5/02 , C07K5/06 , C07K5/08
CPC分类号： C07K5/0205 , C07F9/5726 , A61K38/00
摘要： The invention relates to new phosphonopyrrolidine- and piperidine-containing pseudopeptides, to a process for their preparation and to their use as medicaments, in particular as antiviral agents in human and veterinary medicine.
摘要翻译： 本发明涉及新的膦酰基吡咯烷和哌啶的伪肽，涉及其制备方法和用作药物，特别是作为人和兽医学中的抗病毒剂。
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8.发明授权Phosphonate-containing pseudopeptides of the hydroxyethylamine and norstatin type 失效含有膦酸盐的假多肽的羟乙胺和类维生素D类
公开(公告)号：US5364931A
公开(公告)日：1994-11-15
申请号：US746271
申请日：1991-08-15
申请人： Dieter Habich , Jutta Hansen , Arnold Paessens
发明人： Dieter Habich , Jutta Hansen , Arnold Paessens
IPC分类号： A61K31/675 , A61K38/00 , A61P31/12 , A61P31/18 , C07C317/44 , C07D303/36 , C07D331/02 , C07F9/572 , C07F9/6558 , C07K5/06 , C07K5/08 , C07F9/58 , C07F9/60
CPC分类号： C07K5/06191 , C07C317/44 , C07D303/36 , C07D331/02 , C07F9/5726 , C07K5/0827 , A61K38/00
摘要： The invention relates to phosphonate-containing pseudopeptides of the hydroxyethylamine and norstatin type, to new oxirane- and thiirane-containing pseudopeptides as intermediates, to processes for their preparation and to their use as retroviral agents.
摘要翻译： 本发明涉及羟乙基胺和去饱和抑制素类型的含膦酸盐的假肽，新的环氧乙烷和含硫脲的假肽作为中间体，其制备方法及其作为逆转录病毒剂的用途。
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公开(公告)号：US5162538A
公开(公告)日：1992-11-10
申请号：US624173
申请日：1990-12-07
IPC分类号： A61K31/44 , A61K31/4402 , A61K31/4418 , A61P31/12 , C07D213/40
CPC分类号： C07D213/40
摘要： Antiviral new peptides of the formula ##STR1## in which R.sup.3 denotes straight-chain or branched alkyl having up to 8 carbon atoms ordenotes aryl having 6 to 10 carbon atoms or tolyl, andR.sup.4 denotes straight-chain or branched alkyl having up to 8 carbon atoms,and physiologically acceptable salts thereof.
摘要翻译： 式“IMAGE”的抗病毒新肽，其中R3表示具有至多8个碳原子的直链或支链烷基或表示具有6至10个碳原子的芳基或甲苯基，R4表示直链或支链烷基， 碳原子及其生理上可接受的盐。
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10.发明授权Peptides retroviral protease inhibitors comprising 2-amino-2-methylpropionic acid 失效包含2-氨基-2-甲基丙酸的肽类复性蛋白酶抑制剂
公开(公告)号：US5145951A
公开(公告)日：1992-09-08
申请号：US639627
申请日：1991-01-10
IPC分类号： A61K38/00 , A61P31/12 , C07C233/30 , C07C237/22 , C07C271/22 , C07K5/02 , C07K5/06 , C07K5/08 , C07K5/10 , C07K7/02 , C07K14/81
CPC分类号： C07K5/0227 , C07C271/22 , C07K5/0207 , C07K7/02 , A61K38/00 , C07C2101/14 , Y02P20/55
摘要： Antiviral peptides of the formula ##STR1## in which W is an amino protecting group,A,B,D,E and L each independently is a direct bond, or a radical of the formula ##STR2## R.sup.1 and R.sup.2 each independently is cycloakyl or optionally substituted alkyl or alkenyl,Y is --NHR.sup.10, andR.sup.10 is cycloalkyl or optionally substituted alkyl, and their physiologically acceptable salts.The formula includes a 2-amino-2-methylpropionic acid (AiB) residue, which may optionally be protected, as the N-terminal .alpha.-amino acid. The peptides are expected to be useful as medicaments, in particular as antiviral agents in human and veterinary medicine. The peptides are shown to inhibit aspartyl proteases including human immunodeficiency virus (HIV) protease, to have anti-HIV activity and to inhibit the proliferation of HIV in HIV-I infected human lymphocytes. The peptides are expected to be useful in treating patients having HIV related disorders such as ARC and AIDS.
摘要翻译： 其中W是氨基保护基团，A，B，D，E和L的式“IMAGE”的抗病毒肽各自独立地是直接键合，或下式的基团R 1和R 2各自独立地 是环烷基或任选取代的烷基或烯基，Y是-NHR 10，R 10是环烷基或任选取代的烷基，以及它们的生理上可接受的盐。 该式包括可任选被保护的2-氨基-2-甲基丙酸（AiB）残基作为N-末端α-氨基酸。 预期肽可用作药物，特别是作为人和兽医学中的抗病毒剂。 显示该肽抑制包括人免疫缺陷病毒（HIV）蛋白酶在内的天冬氨酰蛋白酶具有抗HIV活性并抑制HIV-1感染的人淋巴细胞中的HIV增殖。 这些肽预期可用于治疗患有HIV相关疾病如ARC和AIDS的患者。
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