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1.发明授权N-acylated 1-alkylamino-1-deoxy-ketose derivatives, a process for their preparation and their use 失效N-酰化的1-烷基氨基-1-脱氧酮酮衍生物，其制备方法及其应用
公开(公告)号：US4631272A
公开(公告)日：1986-12-23
申请号：US699712
申请日：1985-02-08
申请人： Oswald Lockhoff , Bernd-Wieland Kruger , Peter Stadler , Karl G. Metzger , Hein-Peter Kroll , Klaus Schaller , Hans-Joachim Zeiler
发明人： Oswald Lockhoff , Bernd-Wieland Kruger , Peter Stadler , Karl G. Metzger , Hein-Peter Kroll , Klaus Schaller , Hans-Joachim Zeiler
IPC分类号： C07H13/02 , A61K31/70 , A61K31/7024 , A61P31/04 , C07H7/02 , C07H13/04 , C07H13/06 , C07H13/12 , C07H15/12 , C07H5/06
摘要： Compounds of the formula ##STR1## in which R.sup.1 represents hydrogen or an optionally substituted, straight-chain or branched alkyl or mono- or poly-unsaturated alkenyl radical with in each case up to 30 C atoms,X represents CH.sub.2, O, S or NR,whereinR denotes hydrogen or an alkyl group with up to 20 C atoms, andR.sup.2 represents hydrogen or an optionally substituted, straight-chain or branched, saturated or mono- or poly-unsaturated hydrocarbon radical with up to 30 C atoms,or pharmaceutically acceptable salts thereof, stimulate the immune system and help fight infection.
摘要翻译： 其中R 1表示氢或任选取代的直链或支链烷基或单或多不饱和烯基，其中在每种情况下最多达30个C原子，X代表CH2 ，O，S或NR，其中R表示氢或具有至多20个C原子的烷基，R 2表示氢或任选取代的直链或支链，饱和或单或多不饱和烃基，其直到 30 C原子或其药学上可接受的盐刺激免疫系统并帮助抵抗感染。
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公开(公告)号：US4737488A
公开(公告)日：1988-04-12
申请号：US676160
申请日：1984-11-29
申请人： Oswald Lockhoff , Bernd-Wieland Kruger , Peter Stadler , Karl G. Metzger , Hans-Georg Opitz , Klaus Schaller , Klaus G. Stunkel , Hans-Joachim Zeiler
发明人： Oswald Lockhoff , Bernd-Wieland Kruger , Peter Stadler , Karl G. Metzger , Hans-Georg Opitz , Klaus Schaller , Klaus G. Stunkel , Hans-Joachim Zeiler
摘要： Compounds of the formula ##STR1## wherein R.sup.1 is hydrogen, an optionally substituted aromatic hydrocarbon radical, an aralkyl radical or an optionally substituted aliphatic hydrocarbon radical having up to 45 C atoms,R.sup.2 is an optionally substituted aromatic hydrocarbon radical, an aralkyl radical or an optionally substituted aliphatic hydrocarbon radical having 5-50 C atoms,X is O, S, NH or NR, R being an alkyl radical having up to 20 C atoms, andZ is a glycosyl radical bonded via the anomeric carbon atom,or pharmaceutically acceptable salts thereof stimulate the immune system.
摘要翻译： 其中R 1是氢，任选取代的芳族烃基，芳烷基或具有至多45个C原子的任选取代的脂族烃基的式的化合物，R 2是任选取代的芳族烃基，芳烷基或 任选取代的具有5-50个碳原子的脂族烃基，X是O，S，NH或NR，R是具有至多20个C原子的烷基，Z是通过端基异碳键键合的糖基，或药学上可接受的 其盐刺激免疫系统。
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3.发明授权Novel pharmaceutically active N-(2-aminoacylamido-2-deoxy-hexosyl)-amides, -carbamates and -ureas 失效新型药物活性N-（2-氨基酰氨基-2-脱氧己糖基） - 酰胺， - 氨基甲酸酯和脲
公开(公告)号：US4855283A
公开(公告)日：1989-08-08
申请号：US874983
申请日：1986-06-16
申请人： Oswald Lockhoff , Yutaka Hayauchi , Peter Stadler , Klaus G. Stunkel , Gert Streissle , Arnold Paessens , Volker Klimetzek , Hans-Joachim Zeiler , Karl G. Metzger , Hein-Peter Kroll , Helmut Brunner , Klaus Schaller
发明人： Oswald Lockhoff , Yutaka Hayauchi , Peter Stadler , Klaus G. Stunkel , Gert Streissle , Arnold Paessens , Volker Klimetzek , Hans-Joachim Zeiler , Karl G. Metzger , Hein-Peter Kroll , Helmut Brunner , Klaus Schaller
IPC分类号： A61K31/70 , A61K31/7024 , A61K31/7028 , A61K39/39 , A61P1/16 , A61P11/00 , A61P27/16 , A61P29/00 , A61P31/04 , A61P31/12 , A61P37/00 , C07H13/04 , C07H13/06 , C07H13/12 , C07H15/04 , C07H15/12
CPC分类号： C07H13/04 , A61K39/39 , C07H13/12 , A61K2039/55511
摘要： Compounds of the formula ##STR1## in which R.sup.1 denotes hydrogen or a saturated or singly or multiply unsaturated alkyl radical having up to 50 carbon atoms,X represents --CH.sub.2 --, --O-- or --NH--,R.sup.2 denotes hydrogen or a saturated or singly or multiply unsaturated alkyl radical having up to 50 carbon atoms,R.sup.3, R.sup.4 and R.sup.5, independently of one another, denotes hydrogen or acyl--CO--R.sup.6, R.sup.6 being an alkyl radical having up to 10 carbon atoms,R.sup.7 denotes hydrogen, C.sub.1 -C.sub.7 -alkyl-, hydroxymethyl, 1-hydroxyethyl, mercaptomethyl, 2-(methylthio)-ethyl, 3-aminopropyl, 3-ureidopropyl, 3-guanidyl-propyl, 4-aminobutyl, carboxymethyl, carbamylmethyl, 2-carboxyethyl, 2-carbamoylethyl, benzyl, 4-hydroxybenzyl, 3-indolylmethyl or 4-imidazolylmethyl, andR.sup.8 represents hydrogen or methyl, andR.sup.9 represents hydrogen, acetyl, benzoyl, trichloroacetyl, trifluoroacetyl, methoxycarbonyl, t-butyloxycarbonyl or benzyloxycarbonyl andR.sup.7 and R.sup.8 together can denote --CH.sub.2 --CH.sub.2 --CH.sub.2, and pharmaceutically acceptable salts thereof stimulate the immune system and can be used in conjuction with antibiotics and vaccines. New intermediates are also shown.
摘要翻译： 其中R 1表示氢或具有至多50个碳原子的饱和或单或多不饱和烷基的式“IMAGE”的化合物，X表示-CH 2 - ， - O-或-NH-，R 2表示氢或饱和或 具有多达50个碳原子的单或多不饱和烷基，R 3，R 4和R 5彼此独立地表示氢或酰基-CO-R 6，R 6是具有至多10个碳原子的烷基，R 7表示氢，C 1 C 1-7 - 烷基 - ，羟甲基，1-羟乙基，巯基甲基，2-（甲硫基） - 乙基，3-氨丙基，3-脲基丙基，3-氨基丙基 - 丙基，4-氨基丁基，羧甲基，氨基甲酰甲基，2-羧乙基， 乙酰基，苯甲酰基，三氯乙酰基，三氟乙酰基，甲氧基羰基，叔丁氧基羰基或苄氧基羰基，R7和R8一起可以表示（C 1 -C 6）烷基，苄基，4-羟基苄基，3-吲哚基甲基或4-咪唑基甲基，R 8表示氢或甲基， -CH 2 -CH 2 -CH 2，及其药学上可接受的盐 模拟免疫系统，并可与抗生素和疫苗结合使用。 还显示了新的中间体。
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公开(公告)号：US4716152A
公开(公告)日：1987-12-29
申请号：US675808
申请日：1984-11-28
申请人： Bernd-Wieland Kruger , Oswald Lockhoff , Karl G. Metzger , Hans-Georg Opitz , Klaus Schaller , Klaus G. Stunkel , Hans-Joachim Zeiler
发明人： Bernd-Wieland Kruger , Oswald Lockhoff , Karl G. Metzger , Hans-Georg Opitz , Klaus Schaller , Klaus G. Stunkel , Hans-Joachim Zeiler
IPC分类号： A61K31/70 , A61K31/7028 , A61P37/00 , C07H15/04 , C07H15/10
CPC分类号： C07H15/04
摘要： Compounds of the formula ##STR1## in which X is hydrogen or the radical CH.sub.2 OR.sup.5,R.sup.2, R.sup.3, R.sup.4 and R.sup.5 each independently is hydrogen or the radical ##STR2## Y is oxygen, sulphur, NH or CH.sub.2, and R.sup.1 and R.sup.6 each independently is an optionally substituted hydrocarbon radical having up to 50 carbon atoms, with the proviso that at least one of the radicals R.sup.1 and/or R.sup.6 contains between 9 to 50 carbon atoms,some of which are known, stimulate the immune system's response and antibody production.
摘要翻译： 其中X为氢或基团CH 2 OR 5，R 2，R 3，R 4和R 5各自独立地为氢或基团Y为氧，硫，NH或CH 2的式“IMAGE”的化合物，R 1和R 6各自独立地为 是具有至多50个碳原子的任选取代的烃基，条件是基团R 1和/或R 6中的至少一个含有9至50个碳原子，其中一些是已知的，刺激免疫系统的应答和抗体产生 。
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5.发明授权N-glycosylated carboxamide derivatives and their use for influencing the body's inherent defences 失效N-糖基化的甲酰胺衍生物及其用于影响身体内在防御的用途
公开(公告)号：US4683222A
公开(公告)日：1987-07-28
申请号：US725060
申请日：1985-04-19
IPC分类号： A61K31/70 , A61K31/7008 , A61K31/7024 , A61K31/7028 , A61P37/04 , C07H5/06 , C07H13/04 , C07H13/06 , C07H15/12
摘要： The invention relates to N-glycosylated carboxamide derivatives of Formula I which are useful for influencing the body's inherent defenses, e.g. for increasing immune system antibodies. Also included in the invention are compositions containing said N-glycosylated carboxamide derivative of Formula I as active ingredients and methods for the use of said compounds and compositions.
摘要翻译： 本发明涉及式I的N-糖基化的甲酰胺衍生物，其可用于影响身体的固有防御，例如， 用于增加免疫系统抗体。 本发明还包括含有式I的N-糖基化羧酰胺衍生物作为活性成分的组合物和使用所述化合物和组合物的方法。
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公开(公告)号：US5684023A
公开(公告)日：1997-11-04
申请号：US503116
申请日：1995-07-17
申请人： Bernd Riedl , Dieter Habich , Andreas Stolle , Hanno Wild , Rainer Endermann , Klaus Dieter Bremm , Hein-Peter Kroll , Harald Labischinski , Klaus Schaller , Hans-Otto Werling
发明人： Bernd Riedl , Dieter Habich , Andreas Stolle , Hanno Wild , Rainer Endermann , Klaus Dieter Bremm , Hein-Peter Kroll , Harald Labischinski , Klaus Schaller , Hans-Otto Werling
IPC分类号： C07D333/52 , A61K31/42 , A61P31/04 , C07D307/81 , C07D333/70 , C07D413/04 , C07D413/14
CPC分类号： C07D413/04 , C07D413/14
摘要： The present invention relates to benzofuranyl- and benzothienyloxazolidinones, processes for their preparation and their use as medicaments, in particular as antibacterial medicaments.
摘要翻译： 本发明涉及苯并呋喃基 - 和苯并噻吩并恶唑烷酮，其制备方法及其用作药物，特别是抗菌药物。
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公开(公告)号：US5627181A
公开(公告)日：1997-05-06
申请号：US503369
申请日：1995-07-17
申请人： Bernd Riedl , Dieter H abich , Andreas Stolle , Hanno Wild , Rainer Endermann , Klaus D. Bremm , Hein-Peter Kroll , Harald Labischinski , Klaus Schaller , Hans-Otto Werling
发明人： Bernd Riedl , Dieter H abich , Andreas Stolle , Hanno Wild , Rainer Endermann , Klaus D. Bremm , Hein-Peter Kroll , Harald Labischinski , Klaus Schaller , Hans-Otto Werling
IPC分类号： C07D237/20 , A61K31/44 , A61K31/4418 , A61K31/47 , A61K31/495 , A61K31/50 , A61P31/04 , C07D213/72 , C07D215/38 , C07D215/48 , C07D239/42 , C07D241/44 , C07D413/04 , C07D413/14 , C07D417/14 , C07D471/04 , A61K31/535
CPC分类号： C07D413/04 , C07D413/14 , C07D417/14
摘要： The invention relates to 6-membered nitrogen-containing heteroaryloxazolidinones, processes for their preparation and their use as medicaments, in particular as antibacterial medicaments.
摘要翻译： 本发明涉及6元含氮杂芳基恶唑烷酮，其制备方法及其作为药物的用途，特别是抗菌药物。
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公开(公告)号：US5843967A
公开(公告)日：1998-12-01
申请号：US749581
申请日：1996-11-15
申请人： Bernd Riedl , Dieter Habich , Andreas Stolle , Hanno Wild , Rainer Endermann , Klaus Dieter Bremm , Hein-Peter Kroll , Harald Labischinski , Klaus Schaller , Hans-Otto Werling
发明人： Bernd Riedl , Dieter Habich , Andreas Stolle , Hanno Wild , Rainer Endermann , Klaus Dieter Bremm , Hein-Peter Kroll , Harald Labischinski , Klaus Schaller , Hans-Otto Werling
IPC分类号： C07D237/20 , A61K31/44 , A61K31/4418 , A61K31/47 , A61K31/495 , A61K31/50 , A61P31/04 , C07D213/72 , C07D215/38 , C07D215/48 , C07D239/42 , C07D241/44 , C07D413/04 , C07D413/14 , C07D417/14 , C07D471/04 , C07D401/04
CPC分类号： C07D413/04 , C07D413/14 , C07D417/14
摘要： The invention relates to 6-membered nitrogen-containing heteroaryloxazolidinones, processes for their preparation and their use as medicaments, in particular as antibacterial medicaments.
摘要翻译： 本发明涉及6元含氮杂芳基恶唑烷酮，其制备方法及其作为药物的用途，特别是抗菌药物。
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公开(公告)号：US5698574A
公开(公告)日：1997-12-16
申请号：US503183
申请日：1995-07-17
申请人： Bernd Riedl , Dieter Habich , Andreas Stolle , Hanno Wild , Rainer Endermann , Klaus Dieter Bremm , Hein-Peter Kroll , Harald Labischinski , Klaus Schaller , Hans-Otto Werling
发明人： Bernd Riedl , Dieter Habich , Andreas Stolle , Hanno Wild , Rainer Endermann , Klaus Dieter Bremm , Hein-Peter Kroll , Harald Labischinski , Klaus Schaller , Hans-Otto Werling
IPC分类号： C07D333/38 , A61K31/42 , A61K31/421 , A61K31/4245 , A61K31/425 , A61K31/426 , A61K31/44 , A61K31/655 , A61P31/04 , C07D263/32 , C07D263/48 , C07D277/20 , C07D277/44 , C07D333/66 , C07D413/04 , C07D413/08 , C07D413/14 , C07D417/04 , C07D417/14 , C07D413/00
CPC分类号： C07D413/04 , C07D263/48 , C07D413/08 , C07D413/14 , C07D417/04
摘要： The present invention relates to 5-membered heteroaryl-oxazolidinones, to processes for their preparation and to their use as medicaments, in particular as antibacterial medicaments.
摘要翻译： 本发明涉及5元杂芳基 - 恶唑烷酮，其制备方法和用作药物，特别是抗菌药物。
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公开(公告)号：US6069160A
公开(公告)日：2000-05-30
申请号：US631516
申请日：1996-04-12
申请人： Andreas Stolle , Dieter Habich , Stephan Bartel , Bernd Riedl , Martin Ruppelt , Hanno Wild , Rainer Endermann , Klaus-Dieter Bremm , Hein-Peter Kroll , Harald Labischinski , Klaus Schaller , Hans-Otto Werling
发明人： Andreas Stolle , Dieter Habich , Stephan Bartel , Bernd Riedl , Martin Ruppelt , Hanno Wild , Rainer Endermann , Klaus-Dieter Bremm , Hein-Peter Kroll , Harald Labischinski , Klaus Schaller , Hans-Otto Werling
IPC分类号： A61K31/40 , A61K31/42 , A61K31/423 , A61K31/425 , A61K31/44 , A61K31/445 , A61K31/655 , A61K31/66 , A61P31/04 , C07D263/58 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/14 , C07D419/04 , C07F9/6558 , C07F9/6584 , A61K31/428 , C07D263/54 , C07D277/62
CPC分类号： C07D263/58 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/14 , C07D419/04 , C07F9/6558 , C07F9/65842
摘要： The invention relates to heteroatom-containing benzocyclopentaneoxazolidinones, to processes for their preparation and their use as medicaments, especially as antibacterial medicaments.
摘要翻译： 本发明涉及含杂原子的苯并环戊恶唑烷酮，其制备方法及其作为药物的用途，特别是作为抗菌药物。
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