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61. 发明授权

US4990661A Process for the preparation of benzoic acid derivatives 失效
标题翻译：苯甲酸衍生物的制备方法
公开(公告)号：US4990661A
公开(公告)日：1991-02-05
申请号：US330396
申请日：1989-03-29
申请人： Uwe Petersen , Michael Schriewer , Ernst Kysela , Klaus Grohe
发明人： Uwe Petersen , Michael Schriewer , Ernst Kysela , Klaus Grohe
IPC分类号： C07C63/72 , C07C51/363 , C07C51/60 , C07C63/00 , C07C63/70 , C07C67/00 , C07C227/00 , C07C229/60
CPC分类号： C07C51/363 , C07C51/60
摘要： A process for the preparation of a compound of the formula ##STR1## in which X.sup.1 and X.sup.2 each independently is chlorine or fluorine, andY is chlorine, bromine, fluorine or iodine, comprising subjecting a compound of the formula ##STR2## to a Sandmeyer or Balz-Schiemann reaction thereby to produce a carboxylic acid of the formula ##STR3## and converting the carboxylic acid (Ia) into an acyl chloride of the formula ##STR4## The compound (II) is new. The products are known intermediates for anti-bacterials.

62. 发明授权

US4956465A Quinolone- and 1,8-naphthyridin-4-one-carboxylic acids which are C-bonded in the 7-position 失效
标题翻译：在7-位C键合的喹诺酮和1,8-萘啶-4-酮羧酸
公开(公告)号：US4956465A
公开(公告)日：1990-09-11
申请号：US252631
申请日：1988-10-03
申请人： Michael Schriewer , Klaus Grohe , Uwe Petersen
发明人： Michael Schriewer , Klaus Grohe , Uwe Petersen
IPC分类号： C07D215/56 , C07D471/04
CPC分类号： C07D471/04 , C07D215/56
摘要： As novel intermediates for antibacterials, the quinolone- and 1,8-naphthyridine-4-one-carboxylic acids which are C-bonded in the 7-position of the formula ##STR1## in which Y represents a carboxyl group, a nitrile group, an ester group --COOR.sup.3, or an acid amide group --CONR.sup.4 R.sup.5, where R.sup.3 stands for C.sub.1 -C.sub.4 -alkyl,X.sup.2 stands for hydrogen, nitro, alkyl having 1 to 3 carbon atoms and halogen, in particularR.sup.1 can be alkyl having 1-4 carbon atoms, vinyl, halogenoalkyl, hydroxyalkyl, cycloalkyl having 1-6 carbon atoms or optionally substituted phenyl,R.sup.2 stands for hydrogen, alkyl having 1-3 carbon atoms which is optionally substituted by halogen, alkoxy having 1-2 carbon atoms or nitro, phenyl and for a radical ##STR2## and Z.sup.1 and Z.sup.2 can each be hydrogen or various organic radicals or together form a ring,and salts and esters thereof.
摘要翻译：作为抗细菌剂的新型中间体，在其中Y表示羧基的式“I”的7-位上与C键合的喹诺酮和1,8-二氮杂萘-4-酮羧酸，腈基，酯基-COOR3或酰胺基-CONR4R5，其中R3代表C1-C4-烷基，X2代表氢，硝基，具有1至3个碳原子的烷基和卤素，特别是R1可以是具有1个 -4个碳原子，乙烯基，卤代烷基，羟基烷基，具有1-6个碳原子的环烷基或任选取代的苯基，R 2代表氢，具有1-3个碳原子的烷基，其任选被卤素，具有1-2个碳原子的烷氧基或硝基，苯基和基团，并且Z 1和Z 2各自可以是氢或各种有机基团或一起形成环，以及它们的盐和酯。

63. 发明授权

US4851160A Process for the preparation of benzoic acid derivatives 失效
标题翻译：苯甲酸衍生物的制备方法
公开(公告)号：US4851160A
公开(公告)日：1989-07-25
申请号：US90888
申请日：1987-08-28
申请人： Uwe Petersen , Michael Schriewer , Ernst Kysela , Klaus Grohe
发明人： Uwe Petersen , Michael Schriewer , Ernst Kysela , Klaus Grohe
IPC分类号： C07C63/72 , C07C51/363 , C07C51/60 , C07C63/00 , C07C63/70 , C07C67/00 , C07C227/00 , C07C229/60
CPC分类号： C07C51/363 , C07C51/60
摘要： A process for the preparation of a compound of the formula ##STR1## in which X.sup.1 and X.sup.2 each independently is chlorine or fluorine, andY is chlorine, bromine, fluorine or iodine, comprising subjecting a compound of the formula ##STR2## to a Sandmeyer or Balz-Schiemann reaction thereby to produce a carboxylic acid of the formula ##STR3## and converting the carboxylic acid (Ia) into an acyl chloride of the formula ##STR4## The compound (II) is new. The products are known intermediates for anti-bacterials.
摘要翻译：一种制备式（I）的化合物的方法，其中X1和X2各自独立地为氯或氟，Y为氯，溴，氟或碘，其包括使式（VI）化合物（II）转化为Sandmeyer或Balz-Schiemann反应，从而产生下式的羧酸（Ia），并将羧酸（Ia）转化成式（Ⅰb）的酰氯化合物（ II）是新的。该产品是已知的抗细菌中间体。

64. 发明授权

US4235888A Pseudotrissaccharides, a process for their production and their use as medicaments 失效
标题翻译：伪三糖，其生产过程及其作为药物的用途
公开(公告)号：US4235888A
公开(公告)日：1980-11-25
申请号：US52871
申请日：1979-06-28
申请人： Peter Stadler , Karl-Georg Metzger , Eckart Voss , Uwe Petersen , Hans-Joachim Zeiler , Hans-Joachim Kabbe
发明人： Peter Stadler , Karl-Georg 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 , C07H17/08
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.
摘要翻译：提供了具有抗菌剂，特别是抗革兰氏阴性微生物的抗生素，具有抗生素的类型。本发明还包括制备假三糖的方法，含有所述假三糖的组合物和使用所述化合物和组合物治疗温血动物的方法。

65. 发明授权

US4224315A Pseudotrisaccharides and their medicinal use 失效
标题翻译：伪三糖及其药用
公开(公告)号：US4224315A
公开(公告)日：1980-09-23
申请号：US931708
申请日：1978-08-07
申请人： Peter Stadler , Karl G. Metzger , Uwe Petersen , Eckart Voss
发明人： Peter Stadler , Karl G. Metzger , Uwe Petersen , Eckart Voss
IPC分类号： A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/7036 , A61P31/04 , C07H15/234 , C07H15/236 , A61K31/71 , C07H15/22
CPC分类号： C07H15/234
摘要： The invention includes, as novel compounds, aminoglycoside antibiotics of the 4,6-di-O-(aminoglycosyl)-1,3-diaminocyclitols which are 3-N"-substituted. Also included in the invention are compositions containing said novel compounds and methods for the use of said compounds and compositions.
摘要翻译：本发明包括作为3-N“取代的4,6-二-O-（氨基糖基）-1,3-二氨基二醇的氨基糖苷类抗生素作为新化合物。本发明还包括含有所述新化合物的组合物和使用所述化合物和组合物的方法。

66. 发明授权

US4234572A 1-N-4,6-di-O-(Aminoglycosyl)-1,3-diamino-cyclitol derivatives, processes for their preparation and their use 失效
标题翻译： 1-N-4,6-di-O-（氨基糖基）-1,3-二氨基 - 环烷醇衍生物，其制备及其用途
公开(公告)号：US4234572A
公开(公告)日：1980-11-18
申请号：US960205
申请日：1978-11-13
申请人： Uwe Petersen , Eckart Voss , Karl G. Metzger , Peter Stadler
发明人： Uwe Petersen , Eckart Voss , Karl G. Metzger , Peter Stadler
IPC分类号： C07H15/23 , A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/7036 , A61P31/04 , C07D207/48 , C07D211/46 , C07D333/48 , C07H13/12 , C07H15/234 , C07H15/236 , A61K31/71 , C07H15/22
CPC分类号： C07D333/48 , C07D207/48 , C07D211/46 , C07H13/12 , C07H15/234
摘要： The invention relates to 1-N-4,6-di-O-(aminoglycosyl)-1,3-diamino-cyclitol derivatives useful as antimicrobial agents. Also included in the invention are methods for preparing said derivatives, the provision of pharmaceutical compositions containing said derivatives and methods for the use of said derivatives and compositions.
摘要翻译：本发明涉及可用作抗微生物剂的1-N-4,6-di-O-（氨基糖基）-1,3-二氨基 - 环状醇衍生物。本发明还包括制备所述衍生物的方法，提供含有所述衍生物的药物组合物和使用所述衍生物和组合物的方法。

67. 发明授权

US4190722A 4,6-Di-O-(aminoglycosyl)-1,3-diaminocyclitols, process for their production and their use 失效
标题翻译： 4,6-二-O-（氨基糖基）-1,3-二氨基二醇，其制备及其用途
公开(公告)号：US4190722A
公开(公告)日：1980-02-26
申请号：US913135
申请日：1978-06-06
申请人： Eckart Voss , Peter Stadler , Uwe Petersen , Hans-Joachim Kabbe , Karl G. Metzger
发明人： Eckart Voss , Peter Stadler , Uwe Petersen , Hans-Joachim Kabbe , Karl G. Metzger
IPC分类号： C07H15/234 , 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 includes selectively acylated or sulphenylated 4,6-O-(aminoglycosyl)-1,3-diaminocyclitols (and methods for their preparation). Also included in the invention are 1-N-acylated-derivatives, such as 1-N-formyl-sisomicin, useful because of the anti-bacterial effects (and methods for their procurement). The invention includes, furthermore, methods for the procurement of said 1-N-acylated or sulphenylated derivatives, compositions containing them and methods for their use.
摘要翻译：本发明包括选择性酰化或磺基化的4,6-O-（氨基糖基）-1,3-二氨基二醇（及其制备方法）。本发明还包括1-N-酰化衍生物，例如1-N-甲酰基西索米星，因为其具有抗菌作用（及其采购方法）。此外，本发明还包括采购所述1-N-酰化或磺化衍生物的方法，含有它们的组合物及其使用方法。

68. 发明授权

US08034817B2 Treatment of bacterial diseases of the respiratory organs 有权
标题翻译：治疗呼吸器官细菌性疾病
公开(公告)号：US08034817B2
公开(公告)日：2011-10-11
申请号：US10775888
申请日：2004-02-10
申请人： Rainer Endermann , Harald Labischinski , Christoph Ladel , Uwe Petersen , Ben Newton
发明人： Rainer Endermann , Harald Labischinski , Christoph Ladel , Uwe Petersen , Ben Newton
IPC分类号： A61K31/497 , A61K9/14 , A61K9/00 , A61K9/12
CPC分类号： A61K9/0075 , A61K31/496
摘要： The invention relates to inhalable quinolonecarboxylic acid derivative compositions for local control of diseases of the respiratory organs, in particular of lung diseases.
摘要翻译：本发明涉及用于局部控制呼吸器官疾病，特别是肺部疾病的吸入性喹诺酮羧酸衍生物组合物。

69. 发明申请

US20120010215A1 Treatment of bacterial diseases of the respiratory organs 审中-公开
标题翻译：治疗呼吸器官细菌性疾病
公开(公告)号：US20120010215A1
公开(公告)日：2012-01-12
申请号：US13192893
申请日：2011-07-28
申请人： Rainer Endermann , Harald Labischinski , Christoph Ladel , Uwe Petersen , Ben Newton
发明人： Rainer Endermann , Harald Labischinski , Christoph Ladel , Uwe Petersen , Ben Newton
IPC分类号： A61K31/496 , A61P11/08 , A61P11/00 , A61P31/04
CPC分类号： A61K9/0075 , A61K31/496
摘要： The invention relates to inhalable quinolonecarboxylic acid derivative compositions for local control of diseases of the respiratory organs, in particular of lung diseases.
摘要翻译：本发明涉及用于局部控制呼吸器官疾病，特别是肺部疾病的吸入性喹诺酮羧酸衍生物组合物。

70. 发明授权

US5659038A 5-vinyl-and 5-ethinyl-quinolone- and -naphthyridone-carboxylic acids 失效
标题翻译： 5-乙烯基和5-乙炔基 - 喹诺酮 - 和 - 萘啶酮 - 羧酸
公开(公告)号：US5659038A
公开(公告)日：1997-08-19
申请号：US642662
申请日：1996-05-03
申请人： Thomas Himmler , Uwe Petersen , Klaus-Dieter Bremm , Rainer Endermann , Michael Stegemann , Heinz-Georg Wetzstein
发明人： Thomas Himmler , Uwe Petersen , Klaus-Dieter Bremm , Rainer Endermann , Michael Stegemann , Heinz-Georg Wetzstein
IPC分类号： C07D401/10 , A01N43/40 , A01N43/90 , A23K1/16 , A23L3/3526 , A23L3/3544 , A61K31/47 , A61P31/04 , C07D215/56 , C07D401/04 , C07D471/04 , C07D487/04 , C07D487/08 , C07D487/14 , C07D487/18 , C07D491/04 , C07D491/048
CPC分类号： C07D215/56 , A23K20/116 , A23L3/3526 , A23L3/3544 , C07D401/04 , C07D471/04 , C07D487/04 , C07D487/08 , C07D487/14 , C07D491/04
摘要： The invention relates to new 5-vinyl- and 5-ethinylquinolone- and -naphthyridonecarboxylic acids, to processes for their preparation, and to antibacterial compositions and feed additives containing them.
摘要翻译：本发明涉及新的5-乙烯基和5-乙炔基喹诺酮和 - 萘啶酮羧酸，其制备方法以及含有它们的抗菌组合物和饲料添加剂。

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