Patents Assigned to Dobfar S.p.A.
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Patent number: 4590185Abstract: There are provided 3-azinomethyl rifamycins of the formula I: ##STR1## wherein R represents hydrogen or acetyl;R.sub.1 represents hydrogen or lower alkyl;R.sub.2 represents an alkyl group having from 2 to 4 carbon atoms substituted by a dialkoxy group each having from 1 to 3 carbon atoms;R.sub.3 represents an alkyl group having from 1 to 4 carbon atoms;R.sub.2 and R.sub.3 may form with the amino nitrogen atom a 4- to 8-membered heterocyclic ring, having a maximum of two hetero atoms, substituted by hydroxy-, alkoxy-, dialkoxy- or alkylenedioxy groups each having from 1 to 4 carbon atoms, arylalkoxyimino groups having from 7 to 9 carbon atoms, acyloxy groups having from 1 to 4 carbon atoms;R.sub.1 and R.sub.2 may form with the amino nitrogen atom and the carbon atom a 5 to 7-membered heterocyclic ring optionally substituted by alkyl or alkoxy group having from 1 to 4 carbon atoms.The compounds display antibacteria activity against Gram-positive and Gram-negative bacteria and Mycobacteria.Type: GrantFiled: April 1, 1985Date of Patent: May 20, 1986Assignee: DOBFAR S.p.A.Inventors: Leonardo Marsili, Marco Falciani, Renato Broggi
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Patent number: 4393205Abstract: Cephapirine esters having the formula ##STR1## wherein R is selected from the group consisting of ##STR2## Such esters and salts thereof, having antibiotic activity, are prepared by reacting 7-ACA with bromophtalide or chloromethylpivalate in the presence of an alkylamine, at a temperature in the range of 0.degree.-70.degree. C. The reaction compound is reacted with chlorohydrate chloride of 4-piridylthioacetic acid. A salt of the compound of formula (I) is isolated from the reaction mixture, after washing with acidic water and addition of a pharmaceutically acceptable acid, by treatment with a suitable solvent.Type: GrantFiled: March 5, 1981Date of Patent: July 12, 1983Assignee: Dobfar S.p.A.Inventors: Marco Falciani, Renato Broggi
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Patent number: 4388460Abstract: Cephalosporine desacetoxy esters having the formula ##STR1## wherein R is selected from the group consisting of ##STR2## and R.sub.1 is selected from the group consisting of ##STR3## Such esters and salts thereof having antibiotic activity are prepared by reacting 7-ADCA with bromophthalide or chloromethyl pivalate in the presence of an alkylamine at a temperature in the range of 0.degree.-70.degree. C. The reaction product is reacted with chloride chlorohydrate of D(-)dihydrophenylglycine or D(-)p-hydroxy phenylgycine.A salt of the compound of formula (I) is isolated from the reaction mixture, which after washing with acidic water and addition of a pharmaceutically acceptable acid is obtained by treatment with suitable solvent.Type: GrantFiled: March 4, 1981Date of Patent: June 14, 1983Assignee: Dobfar S.p.A.Inventors: Marco Falciani, Renato Broggi
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Patent number: 4380630Abstract: N-carboxy cefadroxil disodium salt having formula ##STR1## Said salt is endowed with antibiotic activity and can be administered parenterally.Type: GrantFiled: March 4, 1981Date of Patent: April 19, 1983Assignee: Dobfar S.p.A.Inventors: Marco Falciani, Renato Broggi
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Patent number: 4354023Abstract: Salts of cefadroxil with an amino acid selected from the group consisting of L-lysine, L-arginine and acetylcysteine. Said salts are obtained by reacting an aqueous suspension of cefadroxil with an aqueous solution of an amino acid or its derivative, selected from the group consisting of L-lysine, L-arginine and acetylcysteine. To isolate the salt, the aqueous solution is submitted to lyophilization.Type: GrantFiled: March 4, 1981Date of Patent: October 12, 1982Assignee: Dobfar S.p.A.Inventors: Marco Falciani, Renato Broggi
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Patent number: 4310460Abstract: Process for the production of 6-D-.alpha.-amino-p-hydroxyphenylacetamido penicillanic acid which is a potent antibiotic also known generically as amoxicillin. According to the process there is reacted a boron derivative of 6-APA with an acylating agent derived from the D(-)-p-hydroxyphenylglycine, in dimethylformamide or in dimethylsulfoxide in admixture with methylene chloride or chloroform, hydrolyzing and then removing the enaminic group.Type: GrantFiled: March 24, 1980Date of Patent: January 12, 1982Assignee: Dobfar S.p.A.Inventors: Marco Falciani, Renato Broggi
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Patent number: 4299955Abstract: Process for preparing cephalexine monohydrate and cephadroxyl monohydrate, according to which a reaction is carried out of a mixed anhydride prepared from a Dane salt of phenylglycine or p-hydroxyphenyl-glycine with a chloroformiate, with an aqueous solution of 7-ADCA in a solvent selected from the group comprising dimethyl sulphoxide, dimethylacetamide, formamide, dimethylformamide and dioxane.Type: GrantFiled: March 24, 1980Date of Patent: November 10, 1981Assignee: Dobfar S.p.A.Inventors: Marco Falciani, Renato Broggi
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Patent number: 4139702Abstract: A process for preparing cephalosporines in which a cephalosporanic derivative is treated with a polar solvent, then with an organic base to give a mixture which is cooled at a temperature lower than -25.degree. C. A cyclic derivative of boron is added to the mixture and the temperature is increased to about 0.degree. C. An intermediate compound is formed which by treatment first with an acylating agent and then with a mixture of water and alcohol provides a solution containing cephalosporines.Type: GrantFiled: December 12, 1977Date of Patent: February 13, 1979Assignee: DOBFAR S.p.A.Inventors: Renato Broggi, Marco Falciani
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Patent number: 4127571Abstract: A process for preparing penicillins, in which 6APA is treated with a polar solvent, then with an organic base to give a mixture which is cooled at a temperature lower than -25.degree. C. A cyclic derivative of boron is added to the mixture and the temperature is increased to about 0.degree. C.An intermediate compound is formed which by treatment first with an acylating agent and then with a mixture of water and alcohol provides a solution containing the penicillin.Type: GrantFiled: December 12, 1977Date of Patent: November 28, 1978Assignee: Dobfar S.p.A.Inventors: Renato Broggi, Marco Falciani