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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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2.发明授权Substituted O-acylglycosylamides, pharmaceutical compositions and method of use 失效取代的O-酰基糖基酰胺，药物组合物和使用方法
公开(公告)号：US4574122A
公开(公告)日：1986-03-04
申请号：US675690
申请日：1984-11-28
申请人： Bernd-Wieland Kruger , Oswald Lockhoff , Peter Stadler , Karl G. Metzger , Hans-Georg Opitz , Klaus G. Stunkel , Hans-Joachim Zeiler
发明人： Bernd-Wieland Kruger , Oswald Lockhoff , Peter Stadler , Karl G. Metzger , Hans-Georg Opitz , Klaus G. Stunkel , Hans-Joachim Zeiler
CPC分类号： C07H15/04 , Y10S514/885
摘要： Compounds of the formula ##STR1## in which X is hydrogen or the radical --CH.sub.2 OR.sup.5,three of R.sup.2, R.sup.3, R.sup.4 and R.sup.5 each independently is hydrogen or ##STR2## and the fourth is ##STR3## Z each independently is oxygen, sulphur, NH or CH.sub.2, and R.sup.1, R.sup.6 and R.sup.7 each independently is an optionally substituted hydrocarbon radical having up to 50 carbon atoms,stimulate the immune system's response and antibody production.
摘要翻译： 其中X是氢或基团-CH 2 OR 5，R 3，R 4，R 5和R 5中的三个各自独立地是氢或者“IMAGE”，而第四个是Z，Z各自独立地是氧，硫， NH或CH 2，并且R 1，R 6和R 7各自独立地为具有至多50个碳原子的任选取代的烃基，刺激免疫系统的应答和抗体产生。
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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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4.发明授权Substituted O-sulphonyl-glycosylamides, processes for their preparation and their use as medicaments 失效取代的O-磺酰基 - 糖基酰胺，其制备方法及其作为药物的用途
公开(公告)号：US4699899A
公开(公告)日：1987-10-13
申请号：US832482
申请日：1986-02-21
申请人： Bernd-Wieland Kruger , Yutaka Hayauchi , Oswald Lockhoff , Peter Stadler , Karl G. Metzger , Klaus G. Stunkel , Hans-Joachim Zeiler
发明人： Bernd-Wieland Kruger , Yutaka Hayauchi , Oswald Lockhoff , Peter Stadler , Karl G. Metzger , Klaus G. Stunkel , Hans-Joachim Zeiler
IPC分类号： C07H13/00 , A61K31/70 , A61K31/7024 , A61K31/7028 , A61P31/00 , A61P37/04 , C07H1/00 , C07H13/12 , C07H15/04 , C07H15/12
CPC分类号： C07H13/12 , C07H15/04 , Y10S514/885
摘要： Novel compounds of the formula ##STR1## in which X is hydrogen or --CH.sub.2 --OR.sup.5,Z represents OR.sup.4, NH.sub.2 or ##STR2## R.sup.2, R.sup.3, R.sup.4 and R.sup.5 each independently is hydrogen or ##STR3## at least one of R.sup.2, R.sup.3, R.sup.4 and R.sup.5 being ##STR4## Y and W each independently is oxygen, sulphur, NH or CH.sub.2, and R.sup.1, R.sup.6, R.sup.7 and R.sup.8 each independently is an optionally substituted hydrocarbon radical with up to 50 C atoms,stimulate the immune system.
摘要翻译： 式中，X为氢或-CH 2 OR 5的新颖化合物，Z为OR 4，NH 2或R 2，R 3，R 4和R 5各自独立地为氢或R 2，R 3， ，R 4和R 5是Y，W各自独立地是氧，硫，NH或CH 2，R 1，R 6，R 7和R 8各自独立地是具有至多50个C原子的任选取代的烃基，刺激免疫系统。
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5.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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6.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：US4438260A
公开(公告)日：1984-03-20
申请号：US334401
申请日：1981-12-24
IPC分类号： A23K20/195 , A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/7036 , A61P31/04 , C07D317/20 , C07D317/24 , C07D317/28 , C07D317/32 , C07D319/06 , C07D321/06 , C07H15/236 , C07H15/22
CPC分类号： C07D319/06 , C07D317/20 , C07D317/24 , C07D317/28 , C07D317/32 , C07D321/06 , C07H15/236
摘要： The invention relates to sisomicin derivatives of formula (I) and methods for their preparation. Also included in the invention are compositions containing said sisomicin derivatives and the use of said derivatives and compositions for the treatment of bacterial infections.
摘要翻译： 本发明涉及式（I）的西索米星衍生物及其制备方法。 本发明还包括含有所述西索米星衍生物的组合物和所述衍生物和组合物用于治疗细菌感染的用途。
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公开(公告)号：US4659603A
公开(公告)日：1987-04-21
申请号：US735494
申请日：1985-05-17
IPC分类号： A61K31/47 , A61K31/495 , A61P37/04 , C07D215/56 , A61K39/00
CPC分类号： C07D215/56 , A61K31/495 , Y10S514/885
摘要： 1-Cyclopropylquinolone-3-carboxylic acids of the formula ##STR1## in which R.sup.1 is hydrogen, methyl, ethyl or .beta.-hydroxyethyl, andR.sup.2 is hydrogen, chlorine or fluorineor salts thereof stimulate the immune system, especially in conjunction with an antigen.
摘要翻译： 其中R 1是氢，甲基，乙基或β-羟基乙基，R 2是氢，氯或氟或其盐的1-环丙基喹诺酮-3-羧酸，其中R 1是氢，甲基，乙基或β-羟乙基，其刺激免疫系统，特别是与抗原 。
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9.再颁专利Pseudotrissaccharides, a process for their production and their use as medicaments 失效伪三糖，其生产过程及其作为药物的用途
公开(公告)号：USRE31512E
公开(公告)日：1984-01-31
申请号：US260853
申请日：1981-05-06
申请人： Peter Stadler , Karl G. Metzger , Eckart Voss , Uwe Petersen , Hans-Joachim Zeiler , Hans-Joachim Kabbe
发明人： Peter Stadler , Karl G. Metzger , Eckart Voss , Uwe Petersen , Hans-Joachim Zeiler , Hans-Joachim Kabbe
IPC分类号： A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/7036 , A61P31/04 , C07D317/72 , C07H15/236
CPC分类号： C07D317/72 , C07H15/236
摘要： Pseudotrisaccharides of the sisomycin type are provided which are effective an antibacterial agents, particularly against gram-negative microorganisms. The invention also includes methods for the manufacture of the pseudotrisaccharides, compositions containing said pseudotrisaccharides and methods for the treatment of warm-blooded animals using said compounds and compositions.
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10.发明授权
公开(公告)号：US4335114A
公开(公告)日：1982-06-15
申请号：US161527
申请日：1980-06-20
IPC分类号： A23K20/195 , A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/7036 , A61P31/04 , C07H15/236 , A61K31/71 , C07H15/22
CPC分类号： C07H15/236
摘要： The invention relates to sisomicin derivatives defined below in Formula (I) and a process for the preparation of said derivatives. Also included in the invention are compositions containing said derivatives and methods for using said derivatives and compositions. ##STR1##
摘要翻译： 本发明涉及式（I）中定义的西索米星衍生物及其制备方法。 本发明还包括含有所述衍生物的组合物和使用所述衍生物和组合物的方法。 （一）
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