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1. 发明授权

US06034055A Glycosyl-amides of 2-aminoacylamino-2-deoxy-sugars 失效
标题翻译： 2-氨基酰氨基-2-脱氧糖的糖基酰胺
公开(公告)号：US06034055A
公开(公告)日：2000-03-07
申请号：US255642
申请日：1999-02-22
申请人： Oswald Lockhoff , Burkhard Mielke , Helmut Brunner , Klaus Schaller
发明人： Oswald Lockhoff , Burkhard Mielke , Helmut Brunner , Klaus Schaller
IPC分类号： C07H13/06 , A61K38/00 , A61P37/00 , A61P37/04 , C07H15/12 , C07K5/06 , C07K5/08 , C07K5/10 , C07K9/00 , A61K38/16 , A01N43/04
CPC分类号： C07H15/12 , C07K9/005 , A61K38/00 , Y10S514/885
摘要： The present invention relates to (2-aminoacylamino-2-deoxy-glycosyl)-amides, which are substituted on the nitrogen atom of the amino acid, 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 in medicaments.
摘要翻译：本发明涉及在通式（I）的氨基酸的氮原子上取代的（2-氨基酰基氨基-2-脱氧糖基） - 酰胺，其中取代基具有在说明书中给出的含义，其制备过程及其在药物中的应用。

2. 发明授权

US5905071A Glycosylamides of 2-aminoacylamino-2-deoxy sugars 失效
标题翻译： 2-氨基酰氨基-2-脱氧糖的糖基酰胺
公开(公告)号：US5905071A
公开(公告)日：1999-05-18
申请号：US605031
申请日：1996-06-25
申请人： Oswald Lockhoff , Burkhard Mielke , Helmut Brunner , Klaus Schaller
发明人： Oswald Lockhoff , Burkhard Mielke , Helmut Brunner , Klaus Schaller
IPC分类号： C07H13/06 , A61K38/00 , A61P37/00 , A61P37/04 , C07H15/12 , C07K5/06 , C07K5/08 , C07K5/10 , C07K9/00 , A61K31/70 , A01N43/04 , C07H15/00
CPC分类号： C07H15/12 , C07K9/005 , A61K38/00 , Y10S514/885
摘要： The present invention relates to (2-aminoacylamino-2-deoxy-glycosyl)-amides, which are substituted on the nitrogen atom of the amino acid, 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 in medicaments.
摘要翻译： PCT No.PCT / EP94 / 02736 Sec。 371日期1996年6月25日第 102（e）1996年6月25日PCT PCT 1994年8月17日PCT公布。出版物WO95 / 06654 日期：1995年3月9日本发明涉及在通式（I）的氨基酸的氮原子上被取代的（2-氨基酰基氨基-2-脱氧 - 糖基） - 酰胺，其中取代基具有在描述中给出了它们的制备过程及其在药物中的用途。

3. 发明授权

US4855283A Novel pharmaceutically active N-(2-aminoacylamido-2-deoxy-hexosyl)-amides, -carbamates and -ureas 失效
标题翻译：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。

4. 发明授权

US4737488A Immune system-stimulating N-glycosylated ureas and carbamates 失效
标题翻译：免疫系统刺激N-糖基化尿素和氨基甲酸酯
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
IPC分类号： C07H15/00 , C07H13/12 , C07H15/04 , A61K31/70 , C07H5/06
CPC分类号： C07H13/12 , C07H15/04
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。

5. 发明授权

US4716152A Pharmaceutical use of substituted O-acylglycosides 失效
标题翻译：取代的O-酰基糖苷类药物用途
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。

6. 发明授权

US4631272A N-acylated 1-alkylamino-1-deoxy-ketose derivatives, a process for their preparation and their use 失效
标题翻译： 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
CPC分类号： C07H13/04 , C07H13/06 , C07H13/12 , C07H15/12 , C07H7/02
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。

7. 发明授权

US4683222A N-glycosylated carboxamide derivatives and their use for influencing the body's inherent defences 失效
标题翻译： 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
申请人： Peter Stadler , Oswald Lockhoff , Hans-Georg Opitz , Klaus Schaller
发明人： Peter Stadler , Oswald Lockhoff , Hans-Georg Opitz , Klaus Schaller
IPC分类号： A61K31/70 , A61K31/7008 , A61K31/7024 , A61K31/7028 , A61P37/04 , C07H5/06 , C07H13/04 , C07H13/06 , C07H15/12
CPC分类号： 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。

8. 发明授权

US4891425A N-glycosylamide derivatives, processes for their preparation and their use as medicaments 失效
标题翻译： N-糖酰胺衍生物，其制备方法及其作为药物的用途
公开(公告)号：US4891425A
公开(公告)日：1990-01-02
申请号：US7703
申请日：1987-01-28
申请人： Oswald Lockhoff , Yutaka Hayauchi , Peter Stadler , Helmut Brunner
发明人： Oswald Lockhoff , Yutaka Hayauchi , Peter Stadler , Helmut Brunner
IPC分类号： A01N57/16 , A61K31/70 , A61K31/7028 , A61P31/04 , A61P37/00 , C07H13/04 , C07H15/04 , C07H15/12 , C07H15/18
CPC分类号： C07H13/04 , C07H15/04
摘要： A N-glycosylamide derivative of the formula (I) ##STR1## in which R.sup.1 denotes hydrogen or a saturated or mono- or polyunsaturated alkyl radical with one to 50 carbon atoms,R.sup.2 denotes hydrogen or a saturated or mono- or polyunsaturated alkyl radical with one to 50 carbon atoms,R.sup.3 denotes hydrogen or an acyl radical with up to 20 carbon atoms,R.sup.4 denotes hydrogen or an alkyl radical with up to 4 carbon atoms andR.sup.5 and R.sup.6 independently of one another denote hydrogen or an acyl radical with up to 10 carbon atoms or a saturated or an unsaturated alkyl radical or an aralkyl radical with up to 10 carbon atoms, orR.sup.5 l and R.sup.6 together denote a grouping ##STR2## wherein R.sup.7 and R.sup.8 independently of one another denote hydrogen or lower alkyl with up to 5 carbon atoms or an unsubstituted or substituted aryl radical with up to 10 C atoms in the aromatic part. The N-glycosylamide derivatives exhibiting a broad defense-increasing action in the body.
摘要翻译：式（I）的N-糖酰胺衍生物其中R 1表示氢或具有1至50个碳原子的饱和或单或多不饱和烷基，R 2表示氢或饱和或单或多不饱和的具有1至50个碳原子的烷基，R 3表示氢或至多20个碳原子的酰基，R 4表示氢或具有至多4个碳原子的烷基，R 5和R 6彼此独立地表示氢或酰基具有至多10个碳原子或饱和或不饱和的烷基或具有至多10个碳原子的芳烷基，或者R 5和R 6一起表示分组，其中R 7和R 8彼此独立地表示氢或低级烷基具有多至5个碳原子的芳族部分或未被取代的或取代的芳基，其中芳族部分中具有至多10个C原子。 N-糖酰胺衍生物在体内表现出广泛的防御增加作用。

9. 发明授权

US5070190A Substituted N-glycosylamides, process for their preparation, and their use as medicaments 失效
标题翻译：取代的N-甲酰胺，其制备方法及其作为药物的用途
公开(公告)号：US5070190A
公开(公告)日：1991-12-03
申请号：US336497
申请日：1989-04-12
申请人： Oswald Lockhoff , John Goossens , Helmut Brunner , Michael Sperzel , Klaus G. Stunkel
发明人： Oswald Lockhoff , John Goossens , Helmut Brunner , Michael Sperzel , Klaus G. Stunkel
IPC分类号： A61K31/70 , A61K31/7028 , A61P37/04 , C07H15/12
CPC分类号： C07H15/12 , Y10S514/885
摘要： The invention relates to new N-glycosylamides of the general formula I ##STR1## in which R.sup.1 denotes a saturated alkyl radical or a singly, doubly or triply unsaturated alkenyl radical having up to 50 carbon atoms,R.sup.2 denotes a saturated alkyl radical or a singly, doubly or triply unsaturated alkenyl radical having up to 50 carbon atoms,A represents --CO-- or represents a group ##STR2## in which R.sup.3 represents hydrogen, C.sub.1 -C.sub.7 alkyl, hydroxymethyl, 1-hydroxyethyl, mercaptomethyl, 2-methylthioethyl, 3-aminopropyl, 2-ureidopropyl, 3-guanidylpropyl, 4-aminobutyl, carboxymethyl, carbamoylmethyl, 2-carboxyethyl, 2-carbamoylethyl, benzyl, 4-hydroxybenzyl, 3-indolylmethyl or 4-imidazolylmethyl, andn represents 0 to 10,and which are substituted in the sugar residue with an amino acid residue, as well as process for their preparation and their use as medicaments.
摘要翻译：本发明涉及通式Ⅰ“IMAGE”的新的N-糖基酰胺，其中R 1表示饱和的烷基或具有至多50个碳原子的单，双或三不饱和烯基，R2表示饱和的烷基或单，具有至多50个碳原子的双或三重不饱和烯基，A表示-CO-或代表其中R3表示氢，C1-C7烷基，羟甲基，1-羟乙基，巯基甲基，2-甲硫基乙基，氨基丙基，2-脲基丙基，3-胍基丙基，4-氨基丁基，羧甲基，氨基甲酰基甲基，2-羧基乙基，2-氨基甲酰基乙基，苄基，4-羟基苄基，3-吲哚基甲基或4-咪唑基甲基，n表示0〜10，在糖残基中用氨基酸残基取代，以及其制备方法及其作为药物的用途。

10. 发明授权

US4699899A Substituted O-sulphonyl-glycosylamides, processes for their preparation and their use as medicaments 失效
标题翻译：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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