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1. 再颁专利

USRE31512E 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：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.

2. 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。

3. 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。

4. 发明授权

US3997533A Process for the preparation of 7-acylamino-desacetoxycephalosporanic derivatives 失效
标题翻译：制备7-酰氨基 - 去乙酸基头孢烷衍生物的方法
公开(公告)号：US3997533A
公开(公告)日：1976-12-14
申请号：US442810
申请日：1974-02-14
申请人： Hans-Joachim Kabbe , Uwe Petersen
发明人： Hans-Joachim Kabbe , Uwe Petersen
IPC分类号： A61K31/545 , B01J27/00 , C07B61/00 , C07D20060101 , C07D205/00 , C07D279/00 , C07D401/04 , C07D499/04 , C07D501/10 , C07D501/22 , C07D501/28 , C07D501/30 , C07D501/34
CPC分类号： C07D499/00
摘要： 7-Acylaminodesacetoxycephalosporanic acid derivatives are produced by heating a penicillin ester S-oxide to a temperature between 60.degree. C and 150.degree. C in the presence of a heavy metal salt.
摘要翻译：通过在重金属盐的存在下将青霉素酯S-氧化物加热至60℃至150℃的温度来制备7-酰基乙酰氧基头孢烷酸衍生物。

5. 发明授权

US3936447A 7-Acylamino-desacetoxy-cephalosporanic acid esters and their production 失效
标题翻译： 7-酰氨基 - 脱乙酸基 - 头孢菌酸酯及其制备
公开(公告)号：US3936447A
公开(公告)日：1976-02-03
申请号：US454921
申请日：1974-03-26
申请人： Uwe Petersen , Hans-Joachim Kabbe , Siegfried Petersen
发明人： Uwe Petersen , Hans-Joachim Kabbe , Siegfried Petersen
IPC分类号： B01J31/00 , C07B61/00 , C07D499/00 , C07D501/10 , C07D501/22 , C07D501/18
CPC分类号： C07D499/00
摘要： 7-Acylamino-desacetoxy-cephalosporanic acid esters are produced by heating a sulfoxide of 6-acylaminopenicillanic acid ester at a temperature of from about 60.degree.C to about 150.degree.C in the presence of a phenol catalyst. The 7-acylamino-desacetoxy-cephalosporanic acid esters produced are known per se and are useful as intermediates for the preparation of desacetoxy-cephalosporin derivatives which exhibit antibacterial activity.
摘要翻译： 7-酰基氨基 - 脱乙酸基 - 头孢烷酸酯是通过在苯酚催化剂存在下，在约60℃至约150℃的温度下加热6-酰基氨基青霉烷酸酯的亚砜来制备的。所生产的7-酰基氨基 - 脱乙酸基 - 头孢菌酸酯本身是已知的，可用作制备具有抗菌活性的脱乙酸基 - 头孢菌素衍生物的中间体。

6. 发明授权

US5409932A Piperazine-substituted pyrroloanthracenes 失效
标题翻译：哌嗪取代的吡咯并蒽
公开(公告)号：US5409932A
公开(公告)日：1995-04-25
申请号：US164499
申请日：1993-12-09
申请人： Eckhard Schwenner , Gaetan Ladouceur , Hans-Joachim Kabbe , Thomas M. Aune
发明人： Eckhard Schwenner , Gaetan Ladouceur , Hans-Joachim Kabbe , Thomas M. Aune
IPC分类号： C07D209/58 , A61K31/495 , C07D403/00
CPC分类号： C07D209/58 , Y10S514/825
摘要： The piperazine-substituted pyrroloanthracenes are prepared by reacting either furanoanthracenes with piperazinalkylamines or reacting unsubstituted pyrroloanthracenes first with dihalogenoalkyl compounds and then with appropriately substituted piperazines or by reacting furan derivatives first with piperazinalkylamines and then condensing with anthracenes. The new compounds can be employed as active ingredients in medicaments, in particular in immunomodulators.
摘要翻译：哌嗪取代的吡咯并苯是通过使呋喃那嗪与哌嗪烷基胺反应或首先使未取代的吡咯并苯与二卤代烷基化合物反应，然后与适当取代的哌嗪反应或首先使呋喃衍生物与哌嗪烷基胺反应，然后与蒽缩合而制备的。新化合物可用作药物中的活性成分，特别是在免疫调节剂中。

7. 发明授权

US4285965A Combating pests with 2-carboxymethyl-3-carboxy-chromones and esters 失效
标题翻译：防治害虫与2-羧甲基-3-羧基 - 色酮和酯类
公开(公告)号：US4285965A
公开(公告)日：1981-08-25
申请号：US104223
申请日：1979-12-17
申请人： Hans-Joachim Kabbe , Paul-Ernst Frohberger , Peter Roessler
发明人： Hans-Joachim Kabbe , Paul-Ernst Frohberger , Peter Roessler
IPC分类号： A01N43/14 , C07D311/24 , A61K31/35
CPC分类号： C07D311/24
摘要： 2-Carboxymethyl-3-carboxy-chromones and esters of the formula ##STR1## in which R, R.sup.1 and R.sup.2 each independently is hydrogen, an optionally substituted alkyl, alkenyl, cycloalkyl, cycloalkenyl, aralkyl or aryl group, halogen, hydroxyl, cyano or an optionally substituted alkoxy, aryloxy, aralkoxy, alkoxy-carbonyl or dialkylamino group, orR and R.sup.1, together with two carbon atoms of the benzene ring system, form a carbocyclic or heterocyclic 5-membered or 6-membered ring, andR.sup.3 is hydrogen, optionally substituted alkyl, alkenyl, cycloalkyl, cycloalkenyl or aralkyl,are characterized by fungicidal and arthropodicidal activities. The novel compounds are produced by reacting an o-hydroxyacetophenone of the formula ##STR2## with a glyoxylic acid derivative of the formulaOCH--COOZin whichZ is a cation,in the presence of a basic compound, followed by acidification to form the dicarboxylic acid and, optionally, the ester.
摘要翻译： 2-羧甲基-3-羧基 - 色酮和式“IMAGE”的酯，其中R，R 1和R 2各自独立地为氢，任选取代的烷基，烯基，环烷基，环烯基，芳烷基或芳基，卤素，羟基，氰基或任选取代的烷氧基，芳氧基，芳烷氧基，烷氧基 - 羰基或二烷基氨基，或R和R 1与苯环体系的两个碳原子一起形成碳环或杂环的5元或6元环，并且R 3为氢，任选取代的烷基，烯基，环烷基，环烯基或芳烷基，其特征在于杀真菌和节肢动物杀虫活性。通过在碱性化合物的存在下，使式“IMAGE”的邻羟基苯乙酮与其中Z为阳离子的式OCH-COOZ的乙醛酸衍生物反应，然后酸化形成二羧酸酸和任选的酯。

8. 发明授权

US4261988A Chromanone derivatives 失效
标题翻译：色酮衍生物
公开(公告)号：US4261988A
公开(公告)日：1981-04-14
申请号：US20119
申请日：1979-03-13
申请人： Arno Widdig , Hans-Joachim Kabbe , Martin Scheer , Rudiger Sitt
发明人： Arno Widdig , Hans-Joachim Kabbe , Martin Scheer , Rudiger Sitt
IPC分类号： A61K31/35 , A61K31/352 , A61P19/06 , C07D311/22 , C07D311/24 , C07D311/32 , C07D311/92 , C07D311/96 , C07D405/04 , C07D491/10 , C07D491/107
CPC分类号： C07D491/10 , C07D311/22 , C07D311/24 , C07D311/32 , C07D311/92 , C07D311/96
摘要： Compounds useful in the treatment of cholesterolaemia are of the general formula ##STR1## or salts thereof in which R.sup.1 and R.sup.2 independently denote radicals including hydrogen, alkyl, aryl and heterocyclic radical or together complete a carbocyclic or heterocylic ring, R.sup.3 denotes a radical ##STR2## in which R.sup.9, R.sup.10 and R.sup.11 include hydrogen, cyano, nitro, alkyl and aryl or, in pairs, complete carbocyclic rings, X denotes cyano, nitro or substituted carbonyl, sulphonyl or phosphonyl group, R.sup.4 is hydrogen or a radical defined for R.sup.1 or R.sup.3, and R.sup.5, R.sup.6, R.sup.7 and R.sup.8 include hydrogen, nitro, cyano, carboxyl, alkyl and aryl or, in pairs, complete carbocyclic rings, with the proviso that R.sup.1 and R.sup.9 are not both phenyl if X denotes CO--C.sub.6 H.sub.6. The compounds exhibit considerably higher hypocholesterolaemic activity than the known clofibrate and in addition exhibit a pronounced nutritive effect, e.g., in a medicated fodder or premix.
摘要翻译：用于治疗胆固醇血症的化合物具有通式（I）或其盐，其中R 1和R 2独立地表示包括氢，烷基，芳基和杂环基团的基团，或者一起完成碳环或杂环，R3表示其中R9，R10和R11包括氢，氰基，硝基，烷基和芳基，或成对地成为完全碳环，X表示氰基，硝基或取代的羰基，磺酰基或膦酰基，R4是氢或基团对于R 1或R 3而言，R 5，R 6，R 7和R 8包括氢，硝基，氰基，羧基，烷基和芳基，或成对地成为完全碳环，条件是如果X表示CO，则R 1和R 9不是苯基 -C6H6。化合物显示比已知的氯贝特明显更高的降血胆固醇血症活性，并且还显示出明显的营养作用，例如在药物饲料或预混物中。

9. 发明授权

US4111933A Protection of functional groups during reaction and their subsequent restoration 失效
标题翻译：反应过程中功能组的保护及其后续的恢复
公开(公告)号：US4111933A
公开(公告)日：1978-09-05
申请号：US792080
申请日：1977-04-28
申请人： Heiner Eckert , Ivar Ugi , Hans-Joachim Kabbe
发明人： Heiner Eckert , Ivar Ugi , Hans-Joachim Kabbe
IPC分类号： C07B31/00 , C07B51/00 , C07C27/00 , C07C29/00 , C07C45/63 , C07C47/14 , C07C51/00 , C07C67/00 , C07C68/02 , C07C209/00 , C07C209/62 , C07D333/24 , C07D499/04 , C07D501/02 , C07D501/04 , C08K5/00
CPC分类号： C07C45/63 , C07C47/14 , C07C68/02 , C08K5/005
摘要： In the process for preparing an organic compound of the formulaA' -- Xin whichX is an amino group, a hydroxyl group or a carboxyl group, andA' is the remainder of the molecule, from an organic compound of the formulaA -- Xin whichA is the remainder of the molecule which can undergo reaction to form A', by converting A -- X into a compound of the formulaA -- Z -- COORin whichZ is --NH--, --O-- or a direct C--C bond, andR is a radical of the formula ##STR1## IN WHICH Y is a direct C--C single bond, the --CH.dbd.CH-- group or an arylene group,R.sup.1 to R.sup.4 each independently is hydrogen, halogen or an alkyl, aryl, aralkyl, alkoxycarbonyl, alkylaminocarbonyl, arylaminocarbonyl or cycloalkylaminocarbonyl radical, orR.sup.1 + r.sup.2 and R.sup.3 + R.sup.4 each independently completes a 5- or 6-membered carbocyclic ring, orR.sup.1 and R.sup.3 conjointly with the grouping --C--Y--C-- forms a carbocyclic ring with 5 or 6 carbon atoms, and Hal is halogen,Thereby to protect X, then converting A -- Z -- COOR into a compound of the formulaA' -- Z -- COORand then treating the compound A' -- Z -- COOR to restore the group X, the improvement which comprises effecting the treatment of the compound A' -- Z -- COOR with an alkali metal compound of a complex of monovalent cobalt. The process is applicable particularly to aminocarboxylic acids including intermediates from various stages of the synthesis of penicillins and cephalosporins.

10. 发明授权

US4377518A Azo dyestuffs derived from polycyclo-hetercyclic coupler components 失效
标题翻译：衍生自多环异环成色剂的偶氮染料
公开(公告)号：US4377518A
公开(公告)日：1983-03-22
申请号：US183872
申请日：1980-09-03
申请人： Dieter vor der Bruck , Hans-Joachim Kabbe
发明人： Dieter vor der Bruck , Hans-Joachim Kabbe
IPC分类号： C07D491/04 , C07D491/14 , C07D493/04 , C09B29/01 , C09B29/36 , C09B62/085 , D21H21/28
CPC分类号： C07D491/04 , C07D491/14 , C07D493/04 , C09B29/0003 , C09B29/0022 , C09B29/3686 , C09B62/085 , D21H21/28
摘要： Dyestuffs of the formulaD--N.dbd.N--A Iin whichD represents the radical of a diazo component andA represents the radical of a coupling component of the formulae ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 designate hydrogen or non-ionic radicals,R designates hydrogen or an optionally substituted alkyl, cycloalkyl, aryl, aralkyl or heterocyclic radical,X designates OH or ##STR2## T designates the remaining members of a fused-on ring and Y and Z designate hydrogen, optionally substituted alkyl or optionally substituted aryl, processes for their preparation and process for pigmenting organic material using the dyestuffs of the formula I.
摘要翻译：式DN = NA I的染料，其中D表示重氮组分的基团，A表示式的耦合组分的基团，其中R 1，R 2和R 3表示氢或非离子性基团，R表示氢或任选取代的烷基，环烷基，芳基，芳烷基或杂环基，X表示OH或Y表示稠合环的其余成员，Y和Z表示氢，任选取代的烷基或任选地取代的芳基，其制备方法和使用式I的染料着色有机材料的方法。

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