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1. 发明授权

US4035362A Methods for preparing cephalosporins 失效
标题翻译：头孢菌素的制备方法
公开(公告)号：US4035362A
公开(公告)日：1977-07-12
申请号：US672527
申请日：1976-03-31
申请人： Paolo Masi , Maurizio Foglio , Giovanni Franceschi , Antonino Suarato , Gianfranco Cainelli , Federico Arcamone
发明人： Paolo Masi , Maurizio Foglio , Giovanni Franceschi , Antonino Suarato , Gianfranco Cainelli , Federico Arcamone
IPC分类号： C07D205/08 , C07D205/095 , C07D501/08 , C07D501/10 , C07D501/20
CPC分类号： C07D501/08 , C07D205/095
摘要： A process for preparing cephalosporins of the structure: ##STR1## where R is any of hydrogen, C.sub.1 to C.sub.4 alkyl, t-butoxy, benzyloxy, cyano-methyl, thienyl-methyl, furyl-methyl, naphthyl-methyl, phenyl-methyl, phenoxy-methyl, phenoxy-isopropyl, pyridyl-4-thiomethyl and tetrazolyl-1-methyl;R.sub.1 is any of hydroxyl, C.sub.1 to C.sub.4 alkoxy, benzyloxy, p-methoxy- (or nitro-) benzyloxy, benzhydryloxy, triphenylmethoxy, phenacyloxy, p-halophenacyloxy and trichloroethoxy;Z is any of hydrogen, hydroxyl, --O--CO--C.sub.1 -C.sub.4 alkyl, --O--C.sub.1 -C.sub.4 alkyl, --Br, --I, --Cl, --N.sub.3, --NH.sub.2, --O--CO--CH.sub.3, --O--CO--NH.sub.2 and an -S-mononuclear nitrogen heterocyclic ring,By reacting compounds of the structure: ##STR2## IN WHICH R, R.sub.1, and Z are as above defined; R.sub.2 and R.sub.3 are the same or different and represent a C.sub.1 to C.sub.4 alkyl, a mononuclear aryl ring, --CN, a mononuclear heterocyclic ring or the radicals --COR.sub.4, COOR.sub.4, --PO(OR.sub.4).sub.2, --CO--NHR.sub.4 or R.sub.2 and R.sub.3 together may represent: ##STR3## where T represents >CH.sub.2, -N--R.sub.4 ; and R.sub.4 is lower alkyl, a mononuclear aryl ring or a mononuclear heterocyclic ring,Alone or as mixtures with each other in a suitable solvent at a temperature between -100 and +120.degree. C with a strong base to give compounds of formula I that are a mixture of .DELTA..sub.2 and .DELTA..sub.3 cephem-derivatives from which the .DELTA..sub.3 cephem derivatives can be obtained.
摘要翻译：一种制备结构式头孢菌素的方法：其中R是氢，C1-C4烷基，叔丁氧基，苄氧基，氰基 - 甲基，噻吩基 - 甲基，呋喃基 - 甲基，萘基 - 甲基，苯基 - 甲基，苯氧基甲基，苯氧基 - 异丙基，吡啶基-4-硫代甲基和四唑基-1-甲基; R1是羟基，C1〜C4烷氧基，苄氧基，对甲氧基 - （或硝基）苄氧基，二苯甲氧基，三苯基甲氧基，苯甲酰氧基，对卤代苯氧基和三氯乙氧基中的任一个。 Z是氢，羟基，-O-CO-C 1 -C 4烷基，-O-C 1 -C 4烷基，-Br，-I，-Cl，-N 3，-NH 2，-O-CO-CH 3，-O -CO-NH 2和-S-单核氮杂环，通过反应结构的化合物：其中R，R 1和Z如上所定义;其中R，R 1和Z如上所定义; R2和R3相同或不同，表示C1至C4烷基，单核芳基环，-CN，单核杂环或基团-COR4，COOR4，-PO（OR4）2，-CO-NHR4或R2和 R3一起可以表示：其中T表示> CH 2，-N-R 4; 并且R 4为低级烷基，单核芳基环或单核杂环，单独或混合于适宜溶剂中的温度为-100℃和+120℃之间的强碱，得到式I化合物可以获得DELTA 2和DELTA 3头孢烯衍生物的混合物，其中可以获得DELTA 3头孢烯衍生物。

2. 发明授权

US5721360A Process for the preparation of a thiazoline-azetidinone 失效
标题翻译：制备噻唑啉 - 氮杂环丁酮的方法
公开(公告)号：US5721360A
公开(公告)日：1998-02-24
申请号：US656979
申请日：1996-06-06
申请人： Gianfranco Cainelli , Achille Umani Ronchi , Michele Contento , Mauro Panunzio , Sergio Sandri , Marco Da Col , Leone Dall'Asta
发明人： Gianfranco Cainelli , Achille Umani Ronchi , Michele Contento , Mauro Panunzio , Sergio Sandri , Marco Da Col , Leone Dall'Asta
IPC分类号： C07D205/085 , C07D513/04 , C07D205/12
CPC分类号： C07D513/04
摘要： The present invention refers to process for the preparation of a tiazoline-azetidinone of formula I ##STR1## which comprises N-protecting in position 1 of (3S,4S)-3-phenylace tamido-4-acetoxy-azetidin-2-one, converting the product thus obtained into the corresponding thioamide and subsequently ciclyzing and deprotecting.
摘要翻译：本发明涉及制备（3S，4S）-3-苯基三氨基-4-乙酰氧基 - 氮杂环丁烷-2-酮的式Ⅰ的噻唑烷 - 氮杂环丁酮的方法，将所得产物转化为相应的硫代酰胺随后凝结和脱保护。

3. 发明授权

US5532353A Process for the preparation of halogenated .beta.-lactam compounds 失效
标题翻译：卤代β-内酰胺化合物的制备方法
公开(公告)号：US5532353A
公开(公告)日：1996-07-02
申请号：US58714
申请日：1993-05-10
申请人： Marco Da Col , Leone Dall'Asta , Irene Resta , Gianfranco Cainelli , Michele Contento , Mauro Panunzio , Achille Umani Ronchi
发明人： Marco Da Col , Leone Dall'Asta , Irene Resta , Gianfranco Cainelli , Michele Contento , Mauro Panunzio , Achille Umani Ronchi
IPC分类号： C07D501/00 , C07D501/59 , C07D501/02
CPC分类号： C07D501/00
摘要： There is described the preparation of halogenated .beta.-lactam derivatives by introduction of a chlorine atom in the 3-position of the cephem nucleus starting from a 3-sulfonyloxycephem. Such starting materials are reacted with a chlorine ions donor in a basic medium.
摘要翻译：描述了由3-磺酰氧基头孢烯引入头孢烯核的3-位上的氯原子制备卤代β-内酰胺衍生物。这样的原料与碱性介质中的氯离子供体反应。

4. 发明授权

US06369218B1 Isomerisation of 6&bgr;-fluorosteroids into the corresponding 6&agr;-fluoro derivatives 失效
标题翻译： 6β-氟甾类异构化成相应的6α-氟衍生物
公开(公告)号：US06369218B1
公开(公告)日：2002-04-09
申请号：US09858407
申请日：2001-05-16
申请人： Gianfranco Cainelli , Achille Umani-Ronchi , Michele Contento , Sergio Sandri , Marco Da Col
发明人： Gianfranco Cainelli , Achille Umani-Ronchi , Michele Contento , Sergio Sandri , Marco Da Col
IPC分类号： C07J500
CPC分类号： C07J5/00 , C07J71/00
摘要： Described herein is the isomerisation process of 6&bgr;-fluorosteroids into the corresponding pharmacologically active 6&agr;-fluoro derivatives, comprising the reaction of 6&bgr;-fluorosteroids, or 6&agr;/6&bgr; isomeric mixtures, with an organic base containing a diazoimino group in a suitable organic solvent.
摘要翻译：本文描述了6β-荧光素类化合物进入相应的药理学活性6α-氟衍生物的异构化过程，其包括6β-荧光素类或6α/6β异构体混合物与合适的有机溶剂中含有重氮基亚氨基的有机碱的反应。

5. 发明授权

US4732897A Steroidic 5.alpha.-reductase inhibitors 失效
标题翻译：类固醇5α-还原酶抑制剂
公开(公告)号：US4732897A
公开(公告)日：1988-03-22
申请号：US825348
申请日：1986-02-03
申请人： Gianfranco Cainelli , Giorgio Martelli , Mauro Panunzio , Giuseppe Spunta , Giuliano Nannini , Enrico di Salle
发明人： Gianfranco Cainelli , Giorgio Martelli , Mauro Panunzio , Giuseppe Spunta , Giuliano Nannini , Enrico di Salle
IPC分类号： C07C231/00 , A61K31/47 , A61K31/48 , C07C67/00 , C07C69/716 , C07C235/72 , C07C235/74 , C07C235/82 , C07J41/00 , C07J73/00 , A61K31/58
CPC分类号： C07J41/0061 , C07J73/005 , C07C2103/16
摘要： The present invention relates to new 4-aza-17.beta.-substituted 5.alpha.-androstan-3-ones, to a process for their preparation, to pharmacological compostions containing them, and to the use of said compounds as inhibitors of androgen action by means of testosterone 5-reductase inhibition.
摘要翻译：本发明涉及新的4-氮杂-17β-取代的5α-雄甾烷-3-酮，其制备方法，含有它们的药物组合物，以及所述化合物作为雄激素作用的抑制剂的用途的睾酮5-还原酶抑制。

6. 发明申请

US20060116359A1 17.Beta-(alpha-hydroxy)-esters of androstanes as intermediates for the preparation of 17.beta-fluorinated-androstane esters 审中-公开
标题翻译： 17.作为制备17.β-氟化 - 雄甾烷酯的中间体的雄甾烷的β-（α-羟基） - 酯
公开(公告)号：US20060116359A1
公开(公告)日：2006-06-01
申请号：US10538083
申请日：2003-12-18
申请人： Gianfranco Cainelli , Achille Umani Ronchi , Sergio Sandri , Michele Contento , Giuseppe Fortunato , Marco Da Col , Maria Boriani , Stefano Da Col
发明人： Gianfranco Cainelli , Achille Umani Ronchi , Sergio Sandri , Michele Contento , Giuseppe Fortunato , Marco Da Col , Maria Boriani , Stefano Da Col
IPC分类号： A61K31/573 , C07J3/00
CPC分类号： C07J31/006 , C07J71/0015 , C07J71/0031
摘要： Process for the preparation of polyhalogenated steroids, in particular of androstanic fluoro derivatives corticosteroids by means of the formation of new androstanic S-hydroxy alkyl or aralkyl-17-carbothioate intermediates.
摘要翻译：通过形成新的雄激素S-羟基烷基或芳烷基-17-硫代磷酸酯中间体，制备多卤代类固醇，特别是曲霉氟衍生物皮质类固醇的方法。

7. 发明申请

US20050192437A1 Process for the preparation of 6alpha-fluoro steroids by isomerisation of 6beta-fluorosteroids 审中-公开
标题翻译：通过6β-荧光素类异构化制备6α-氟类固醇的方法
公开(公告)号：US20050192437A1
公开(公告)日：2005-09-01
申请号：US10508668
申请日：2003-03-31
申请人： Gianfranco Cainelli , Achille Umani-Ronchi , Sergio Sandri , Michele Contento , Marco Da Col , Maria Boriani , Stefano Da Col
发明人： Gianfranco Cainelli , Achille Umani-Ronchi , Sergio Sandri , Michele Contento , Marco Da Col , Maria Boriani , Stefano Da Col
IPC分类号： C07J75/00 , C07B55/00 , C07J3/00 , C07J31/00 , C07J71/00
CPC分类号： C07J71/0031 , C07J3/005 , C07J31/006
摘要： The process for the preparation of 6α-fluoro steroids, comprising the reaction of the corresponding 6β-fluoro steroids, or of 6α/6β isomeric mixtures with an organic base having a diazo iminic group, in a suitably selected organic solvent, is described.
摘要翻译：描述了制备6α-氟类固醇的方法，其包括相应的6β-氟类固醇或6α/6β异构体混合物与具有重氮亚胺基团的有机碱在适当选择的有机溶剂中的反应。

8. 发明授权

US5639744A Bile acids derivatives useful in the therapy of the biliary calculosis from cholesterol and of the pathologies caused by cholestasis 失效
标题翻译：胆汁酸衍生物可用于治疗由胆固醇引起的胆汁淤积症和胆汁淤积引起的病理学
公开(公告)号：US5639744A
公开(公告)日：1997-06-17
申请号：US416155
申请日：1995-04-04
申请人： Egidio Marchi , Maria Rita Milani , Silvano Piani , Aldo Roda , Gianfranco Cainelli
发明人： Egidio Marchi , Maria Rita Milani , Silvano Piani , Aldo Roda , Gianfranco Cainelli
IPC分类号： C07J43/00 , A61K31/58
CPC分类号： C07J43/003
摘要： An amide of formula ##STR1## and its pharmacologically acceptable organic or inorganic salt shows a metabolic stability, both enteric and hepatic, greater than that of the corresponding bile acids conjugated with glycine or taurine physiologically present in the enterohepatic circulation. The pharmacological activity of the compounds of formula I or their pharmacologically acceptable organic or inorganic salt makes the use effective for the therapy of biliary calculosis from cholesterol and in every pathology caused by cholestasis like chronic hepatitis from cholestasis, primitive biliary cirrhosis and juvenile hepatopathy associated with cystic fibrosis.
摘要翻译：式Ⅰ的酰胺及其药理学上可接受的有机或无机盐显示出与肠肝循环中生理上存在的甘氨酸或牛磺酸结合的相应胆汁酸的代谢稳定性，包括肠和肝的代谢稳定性。式I化合物或其药理学上可接受的有机或无机盐的药理活性使其有效用于治疗胆固醇和胆汁淤积引起的每一种胆汁淤积症，如胆汁淤积症，慢性肝炎，原始胆汁性肝硬化和与青少年肝病有关的少年肝病囊性纤维化。

9. 发明授权

US4435575A Process for preparing carboxylated organic compounds 失效
标题翻译：制备羧基有机化合物的方法
公开(公告)号：US4435575A
公开(公告)日：1984-03-06
申请号：US279090
申请日：1981-06-30
申请人： Gianfranco Cainelli , Marco Foa' , Achille U. Ronchi , Andrea Gardano
发明人： Gianfranco Cainelli , Marco Foa' , Achille U. Ronchi , Andrea Gardano
IPC分类号： C07C69/614 , B01J31/00 , B01J31/20 , C07B31/00 , C07B41/08 , C07B41/10 , C07B41/12 , C07B61/00 , C07C51/00 , C07C51/10 , C07C57/32 , C07C67/00 , C07C67/36 , C07C69/38 , C07D307/54
CPC分类号： C07C51/10 , C07D307/54
摘要： A process is herein described for preparing carboxylated organic compounds (acids, esters, alkaline salts) of formula ##STR1## wherein R is a hydrocarbyl group having up to 11 carbon atoms (an aliphatic, alicyclic, aryl- or heteroarylalkyl group), also substituted, in its turn, by groups inert under the reaction conditions (alkyl, aryl, etheric, thioetheric, halogen, nitrile, ester, amide, ketonic groups), and R' is a hydrogen atom or an alkyl C.sub.1 -C.sub.8 group, by reaction of carbon monoxide with the corresponding hydrocarbyl halides, having the halogen bound to a non-tertiary carbon atom, in the presence of catalysts which are salts of cobalt hydrocarbonyl, or precursors thereof, in a hydro-alcoholic or alcoholic solvent and in the presence of bases.The process is characterized in that the catalytic system composed by the salt of cobalt hydrocarbonyl is supported on an anion exchange resin. The process permits to operate also continuously, in any case allowing an easy recovery, recycle and regeneration of the catalysts.The products obtained, i.e. carboxylic acids, esters and alkaline salts thereof, are utilized as intermediates for organic syntheses particularly for fine chemistry (phytopharmaceuticals, pharmaceuticals, etc.).
摘要翻译：本文描述了制备式（IMAGE）的羧化有机化合物（酸，酯，碱性盐）的方法，其中R是具有至多11个碳原子的烃基（脂族，脂环族，芳基或杂芳基烷基），也被取代（烷基，芳基，醚基，硫醚，卤素，腈，酯，酰胺，酮基）为惰性的基团，R'为氢原子或C1-C8烷基，通过反应的一氧化碳与相应的烃基卤化物，其卤素与非叔碳原子结合，在催化剂存在下，在氢醇或醇溶剂中存在钴烃基或其前体的催化剂存在下，基地该方法的特征在于将由烃基烃基组成的催化体系负载在阴离子交换树脂上。该方法允许连续操作，在任何情况下允许催化剂的容易回收，再循环和再生。获得的产物，即羧酸，其酯和碱金属盐被用作有机合成的中间体，特别用于精细化学（植物药物，药物等）。

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