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1. 发明授权

US4148996A 3,7-Disubstituted cephalosporins 失效
标题翻译： 3,7-二取代头孢菌素
公开(公告)号：US4148996A
公开(公告)日：1979-04-10
申请号：US797606
申请日：1977-05-16
申请人： Giorgio Palamidessi , Franco Zarini , Giovanni Franceschi , Giovanna Schioppacassi , Federico Arcamone
发明人： Giorgio Palamidessi , Franco Zarini , Giovanni Franceschi , Giovanna Schioppacassi , Federico Arcamone
IPC分类号： C07D501/04 , A61K31/545 , A61K31/546 , A61P31/04 , C07D501/24 , C07D501/36
CPC分类号： C07D501/36 , A61K31/545
摘要： 7-Acylamino-3-pyrazinylthiomethyl-3-cephem-4-carboxylic acids are disclosed having the general formula: ##STR1## wherein R is an alkyl having from 1 to 5 carbon atoms or ##STR2## wherein Y = Y.sup.1 = HY = y.sup.1 = clY = cl, Y.sup.1 = FY = h,y .sup.1 = cl andIn which n is an integer from 1 to 4, X is O or S, and R.sub.2 is thienyl, phenyl, 1,4-cyclohexadienyl, phenoxy, pyrazinyl and substituted phenyl, thienyl, pyrazinyl and phenoxy, the substituent being selected from the group consisting of hydroxy, chlorine, bromine, and alkyl and alkoxy having from 1 to 4 carbon atoms;R.sub.3 is alkali metal such as sodium or potassium, hydrogen, alkyl having from 1 to 4 carbon atoms, benzyl, trichloroethyl, methoxybenzyl, benzhydryl, pivaloyloxymethyl, and an alkaline earth metal; R.sup.1 may be a pyrazinyl of the general formulae: ##STR3## in which R.sup.4, R.sup.5, R.sup.6 are equal or different and are selected from the group consisting of F, Cl, Br, hydrogen, alkyl, phenyl, cyano, thiocyano, carboxyl, carboxyalkyl, carboxamido, thiocarboxamido, hydroxy, alkoxy, thiol, alkylthio, amino, alkylamino, phenylamino. By the terms alkyl, an alkyl having from 1 to 4 carbon atoms is intended. Processes for making them are also disclosed.The new cephalosporin derivatives of formula (I) exhibit a broad spectrum antibacterial activity and are useful as therapeutic agents in the treatment of infectious diseases caused by gram-negative and gram-positive bacteria.
摘要翻译：公开了具有以下通式的7-酰基氨基-3-吡嗪基硫甲基-3-头孢烯-4-羧酸：其中R是具有1至5个碳原子的烷基或者具有1或5个碳原子的烷基其中Y = Y1 = HY = Y1 = C1 Y = C1，Y1 = FY = H，Y1 = C1和IN，其中N为1至4的整数，X为O或S，R2为噻吩基，苯基，1,4-环己二烯基，苯氧基，吡嗪基和取代的苯基，噻吩基，吡嗪基和苯氧基，所述取代基选自羟基，氯，溴以及具有1至4个碳原子的烷基和烷氧基; R3是碱金属如钠或钾，氢，具有1至4个碳原子的烷基，苄基，三氯乙基，甲氧基苄基，二苯甲基，新戊酰氧基甲基和碱土金属; R 1可以是以下通式的吡嗪基：其中R 4，R 5，R 6相同或不同，并且选自F，Cl，Br，氢，烷基，苯基，氰基，硫氰基，羧基，羧基烷基，甲酰氨基，硫代甲酰胺基，羟基，烷氧基，硫醇，烷硫基，氨基，烷基氨基，苯基氨基。术语烷基是指具有1至4个碳原子的烷基。还披露了制作它们的过程。

2. 发明授权

US4206211A Cephalosporins 失效
标题翻译：头孢菌素
公开(公告)号：US4206211A
公开(公告)日：1980-06-03
申请号：US885126
申请日：1978-03-10
申请人： Giorgio Palamidessi , Maurizio Foglio , Franco Zarini , Giovanni Franceschi , Aurora Sanfilippo , Federico Arcamone
发明人： Giorgio Palamidessi , Maurizio Foglio , Franco Zarini , Giovanni Franceschi , Aurora Sanfilippo , Federico Arcamone
IPC分类号： C07D501/04 , A61K31/425 , A61K31/545 , A61K31/546 , A61P31/04 , C07D20060101 , C07D501/00 , C07D501/16 , C07D501/18 , C07D501/24 , C07D501/28 , C07D501/36 , C07D501/57 , C07D501/60 , C07F7/02 , C07F7/08
CPC分类号： C07D501/57
摘要： 7.beta.-acylamino-7.alpha.-methoxy-3-pyrazinylthiomethyl-cephalosporins and their intermediates having high resistance toward .beta.-lactamase enzymes, as well as good antibacterial activity and processes for preparation thereof.
摘要翻译： 7β-酰基氨基-7α-甲氧基-3-吡嗪基硫甲基头孢菌素及其对β-内酰胺酶具有高抗性的中间体，以及良好的抗菌活性及其制备方法。

3. 发明授权

US4155911A Process for the production of substituted 4-thia-2,6-diaza[3.2.0]-2-heptene-7-one 失效
标题翻译：制备取代的4-硫杂-2,6-二氮杂{8 3.2.0 {9,2-庚烯-7-酮
公开(公告)号：US4155911A
公开(公告)日：1979-05-22
申请号：US820895
申请日：1977-08-01
申请人： Maurizio Foglio , Antonino Suarato , Paolo Masi , Giovanni Franceschi , Giorgio Palamidessi , Luigi Bernardi
发明人： Maurizio Foglio , Antonino Suarato , Paolo Masi , Giovanni Franceschi , Giorgio Palamidessi , Luigi Bernardi
IPC分类号： C07D205/08 , C07D513/04
CPC分类号： C07D513/04 , C07D205/08
摘要： A new process is disclosed for the preparation of compounds of structure: ##STR1## and are as defined herein characterized in that a compound of structure ##STR2## where R and R.sup.1 have the meanings given herein, is reacted in a suitable solvent with a haloamide in the presence of a metal oxide or a haloamide in the presence of a free radical initiator under the influence of light or heat or alternatively with a halogen in the presence of a metal oxide, to give a compound of structure: ##STR3## where R and R.sup.1 have the meanings given herein, Hal is a halogen atom; THE INTERMEDIATE COMPOUND (III) in a suitable solvent is then reacted with an appropriate nucleophilic reagent to obtain the compound IV where Z replaces Hal, where Z is defined herein;The compound (IV) is then subjected to an allylic halogenation in a suitable solvent by reacting it with a haloamide either under the influence of light alone or by heating it in the presence of a free radical initiator, to give a compound of structure: ##STR4## where R, R.sup.1 and Hal and Z have the above meanings; THE INTERMEDIATE COMPOUND (V) is then reacted with a reducing agent to give finally the desired compound (I).
摘要翻译：公开了用于制备结构式（I）的化合物的新方法，其定义如下，其特征在于其中R和R 1具有本文给出的含义的结构式（II）的化合物在在金属氧化物或卤代酰胺的存在下，在自由基引发剂的存在下，在光或热的作用下，或者在卤素存在下，在金属氧化物的存在下，与卤代酰胺合适的溶剂，得到结构化合物（III）其中R和R1具有本文给出的含义，Hal是卤素原子; 然后将合适的溶剂中的中间体化合物（III）与合适的亲核试剂反应，得到Z代替Hal的化合物IV，其中Z在本文中定义; 然后使化合物（IV）在合适的溶剂中通过与单独的光的影响下的卤代酰胺反应或通过在自由基引发剂的存在下加热使其与卤代酰胺反应，得到结构式（V）其中R，R1，Hal和Z具有上述含义; 然后将中间体化合物（V）与还原剂反应，最终得到所需化合物（I）。

4. 发明授权

US4141899A 4,5,6,7-Tetrahydroimidazo-[4,5-c]-pyridine derivatives 失效
标题翻译： 4,5,6,7-四氢咪唑并 - {8 4,5-c {9-吡啶衍生物
公开(公告)号：US4141899A
公开(公告)日：1979-02-27
申请号：US838844
申请日：1977-10-03
申请人： Giuliana Arcari , Luigi Bernardi , Giovanni Falconi , Fulvio Luini , Giorgio Palamidessi , Ugo Scarponi
发明人： Giuliana Arcari , Luigi Bernardi , Giovanni Falconi , Fulvio Luini , Giorgio Palamidessi , Ugo Scarponi
IPC分类号： C07D471/04
CPC分类号： Y10S514/926 , Y10S514/927
摘要： New 4,5,6,7-tetrahydroimidazo-[4,5-c]-pyridine derivatives are disclosed, and more particularly derivatives of Formula I ##STR1## where R.sub.1 is hydrogen or an alkyl having from 1 to 4 carbon atoms;R.sub.2 is hydrogen, an alkyl having from 1 to 4 carbon atoms, a cycloalkyl having from 3 to 6 carbon atoms, phenyl or a heterocycle;R.sub.3 is hydrogen, a saturated or unsaturated straight or branched alkyl having from 1 to 6 carbon atoms, a cycloalkyl having from 3 to 6 carbon atoms, benzoyl or phenyl; andX is O, S or NR.sub.4 where R.sub.4 is hydrogen, an alkyl having from 1 to 4 carbon atoms, cyano, amino, nitro or acylamino;Or pharmaceutically acceptable acid addition salts thereof. Also disclosed is a process of preparing these compounds which comprises condensing an appropriate 4,5,6,7-tetrahydroimidazo-[4,5-c]-pyridine with an appropriate alkyl isocyanate, alkyl isothiocyanate or substituted S-methyl thiourea, preferably in a solvent such as ethanol, acetonitrile or dioxane, usually under reflux for from 4 to 12 hours. The products can be isolated by crystallization as free bases or as salts of pharmaceutically acceptable acids. The new compounds have proved to be well tolerated and to inhibit both the number of experimental ulcers and the gastric secretion in experimental animals. Thus, they should prove useful in the therapy of gastric and duodenal ulcers in man.
摘要翻译：公开了新的4,5,6,7-四氢咪唑并[4,5-c] - 吡啶衍生物，更具体地，其中R 1是氢或具有1至4个碳原子的烷基的式I的衍生物; R 2是氢，具有1至4个碳原子的烷基，具有3至6个碳原子的环烷基，苯基或杂环; R3是氢，具有1至6个碳原子的饱和或不饱和直链或支链烷基，具有3至6个碳原子的环烷基，苯甲酰基或苯基; 且X为O，S或NR 4，其中R 4为氢，具有1至4个碳原子的烷基，氰基，氨基，硝基或酰氨基; 或其药学上可接受的酸添加剂。还公开了制备这些化合物的方法，其包括将合适的4,5,6,7-四氢咪唑并[4,5-c] - 吡啶与适当的烷基异氰酸酯，异硫氰酸烷基酯或取代的S-甲基硫脲缩合，优选在溶剂如乙醇，乙腈或二恶烷，通常在回流下4至12小时。可以通过结晶作为游离碱或药学上可接受的酸的盐分离产物。这些新化合物已被证明是良好的耐受性，并且在实验动物中抑制实验性溃疡的数量和胃分泌。因此，它们应该证明在治疗人和十二指肠溃疡方面是有用的。

5. 发明授权

US4077970A Methyl-.alpha.[3'acetoxy-1'isopropenyl]-3 substituted 1.alpha.,5x-4-thia 2,6 diaza[3,2,0]2-heptene-6 acetate 7-one 失效
标题翻译：甲基 - {60 {8 3 {40乙酰氧基-1 {40异丙烯基{9,3取代的1 {60,5x-4-硫杂-2,6-二氮杂{8 3,2,0 {9 2-庚烯-6-乙酸酯7- 一
公开(公告)号：US4077970A
公开(公告)日：1978-03-07
申请号：US603605
申请日：1975-08-11
申请人： Maurizio Foglio , Antonino Suarato , Paolo Masi , Giovanni Franceschi , Giorgio Palamidessi , Luigi Bernardi
发明人： Maurizio Foglio , Antonino Suarato , Paolo Masi , Giovanni Franceschi , Giorgio Palamidessi , Luigi Bernardi
IPC分类号： C07D205/08 , C07D513/04 , C07D513/08
CPC分类号： C07D513/04 , C07D205/08
摘要： A process is disclosed for the preparation of a compound of the formula ##STR1## where R and R.sup.1 are defined herein below, wherein a compound of the structure; ##STR2## is reacted in a suitable solvent with a haloamide in the presence of a metal oxide or a haloamide in the presence of a free radical initiator under the influence of light or heat or alternatively with a halogen in the presence of a metal oxide, to give a compound of the structure; ##STR3## which compound, in a suitable solvent is reacted with a suitable nucleophilic reagent to obtain the compound; ##STR4## which compound is then subjected to allylic halogenation to give a compound of the structure; ##STR5## which is then reacted with a reducing agent to yield I.
摘要翻译：公开了用于制备下式化合物的方法，其中R和R 1如下文所定义，其中该结构的化合物; 在自由基引发剂的存在下，在光或热的作用下，或者在卤素存在下，在金属氧化物或卤代酰胺的存在下，在合适的溶剂中与卤代酰胺反应。，得到结构的化合物; 该化合物在合适的溶剂中与合适的亲核试剂反应得到化合物; 然后将该化合物进行烯丙基卤化，得到结构的化合物; 然后将其与还原剂反应以产生I.

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