Patents Assigned to Pierrel S.p.A.
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Patent number: 4894460Abstract: Basic esters of 1,4-dihydropyridine-3,5-dicarboxylic acid of formula (I) ##STR1## are described, in which R.sup.1 is a linear or branched alkyl radical containing 1-5 carbon atoms which is unsubstituted or substituted by an alkoxy group; R.sup.2 is phenyl or a nitro phenyl radical; R.sup.3 is phenyl, phenyl substituted by one to three radicals selected from (C.sub.1-4)alkyl, (C.sub.1-4)alkoxy, fluoro, chloro, bromo, nitro, cyano, COOR in which R is alkyl of 1 to 4, trifluo carbon atoms, romethyl, hydroxy, amino, mono- or di-alkylamino, mono- or di-acylamino, mercapto, S(O).sub.n -alkyl with n=0, 1 or 2, (C.sub.1-5)acyl, carbamoyl, ureido or R.sup.Type: GrantFiled: December 19, 1983Date of Patent: January 16, 1990Assignee: Pierrel S.p.A.Inventors: Silvia Z. Tricerri, Cesare Casagrande, Franco de Marchi, Massimo Nicola
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Patent number: 4588712Abstract: (8S)-8-fluoroerythromycin derivatives of formula ##STR1## wherein R is an optionally substituted alkyl, alkenyl or phenyl groupR' is hydrogen or methyl andR" is hydrogen or hydroxy,may be prepared by fluorination of the corresponding 8,9-anhydroerythromycin 6,9-hemiketals with perchloryl fluoride in the presence of a compound ROH in strictly anhydrous conditions.The new compounds as well as their pharmaceutically acceptable esters, salts and salt-esters may be employed as the active ingredients of pharmaceutical compositions for antibacterial use suitable for oral administration.Type: GrantFiled: February 28, 1985Date of Patent: May 13, 1986Assignee: Pierrel S.p.A.Inventor: Luciano Toscano
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Patent number: 4579861Abstract: Compounds having general formula I ##STR1## wherein R.sub.1 is hydrogen, lower alkyl, lower alkoxy, alkyl enoxy, halogen, cyano, carboxyamido or ureido group optionally separated from the phenyl ring by a methylene or ethylene bridge;R.sub.2 is hydrogen, halogen, lower alkyl or alkoxy;R.sub.3 is hydrogen, halogen, lower alkyl, lower alkoxy or R.sub.2 and R.sub.3, taken together, are a methylendioxy group;R.sub.4 is hydrogen or lower alkyl,endowed with remarkable cardioselective .beta.-adrenolytic properties, are described.The process for their preparation and pharmaceutical compositions containing them are also described.Type: GrantFiled: January 6, 1984Date of Patent: April 1, 1986Assignee: Pierrel S.p.A.Inventors: Cesare Casagrande, Massimo Nicola
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Patent number: 4560662Abstract: The fermentation of a substrate selected among erythronolide B, erythronolide A and erythronolide A oxime with a novel mutant, Streptomyces antibioticus ATCC 31771, obtained from an industrial stock for the production of oleandomycin, said novel mutant being incapable of producing the same oleandomycin, permits novel macrolide antibiotics to be produced, having not only an activity range like that of erythromycin, but characterized by a greater stability in acidic environment, whereby for the administration of the antibiotic it is no longer necessary to have recourse to esters and/or salts highly toxic for the organism.Type: GrantFiled: November 3, 1983Date of Patent: December 24, 1985Assignee: Pierrel S.p.A.Inventors: Leonardo M. Cappelletti, Roberto Spagnoli, Luciano Toscano
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Patent number: 4540662Abstract: From the fermentation carried, out with mutants blocked in the synthesis respectively of erythromycin and of oleandomycin, namely Streptomyces erythreus ATCC 31772 and Streptomyces antibioticus ATCC 31771, using as the substrate a derivative of erythronolide A, namely (8S)-B-fluoroerythronolide A, a derivative of erythronolide B, namely (8S)-B-fluoroerythronolide B, or a derivative of 3-O-mycarosyl-erythronolide B, namely 3-O-mycarosyl-(8S)-fluoroerythronolide B, the corresponding (8S)-8-fluoro derivatives of the erythromycins A,B, C and D, as well as 3-O-oleandrosyl-5-desosaminyl-(8S)-8-fluoroerythronolide A and 3-O-oleandrosyl-5-O-desosaminyl-(8S)-8-fluoroerythronolide B, all belonging to the class of the marcolide antibiotics are obtained.Type: GrantFiled: January 16, 1984Date of Patent: September 10, 1985Assignee: Pierrel S.p.A.Inventors: Luciano Toscano, Leonard M. Cappelletti
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Patent number: 4526985Abstract: A process for the preparation of the anhydride of N-formyl-L-aspartic acid by reacting L-aspartic acid with nearly stoichiometric amounts of formic acid and acetic anhydride, under controlled conditions of temperature, reaction and addition times. The product is a known intermediate in the synthesis of .alpha.-L-aspartyl-L-phenylalanine methyl ester, a known sweetening agent.Type: GrantFiled: July 18, 1983Date of Patent: July 2, 1985Assignee: Pierrel S.p.A.Inventors: Vincenzo Giobbio, Giorgio Ornato, Livio Buracchi, Alberto Mangia
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Patent number: 4508719Abstract: Compounds of formula I: ##STR1## are described in which R.sup.1 is a linear or branched alkyl radical containing between 1 and 5 carbon atoms, the alkyl radical being unsubstituted or substituted by an alkoxy group; R.sup.2 is an unsubstituted phenyl of phenyl substituted by a nitro group; R.sup.3 is hydrogen or a linear or branched alkyl residue containing between 1 and 4 carbon atoms, the alkyl radical being unsubstituted or substituted by at least one alkoxy or fluorine atom or both alkoxy and fluorine atoms; R.sup.4 is hydrogen or a linear or branched alkyl containing between 1 and 4 carbon atoms, the alkyl radical being unsubstituted or substituted by alkoxy, carbalkoxy, dialkylamino, 1-aryl or 1-heteroarylpiperazinyl, aryl or a monocyclic 5 or 6 membered heterocycle in which at least one of the heteroatoms is N,O,S such as 1-piperidinyl, 4-morpholinyl or R.sub.4 is alkenyl or cyclo(C.sub.3 -C.sub.Type: GrantFiled: May 26, 1983Date of Patent: April 2, 1985Assignee: Pierrel S.p.A.Inventors: Silvia Z. Tricerri, Cesare Casagrande, Franco De Marchi, Massimo Nicola
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Patent number: 4439426Abstract: From the fermentation carried, out with mutants blocked in the synthesis respectively of erythromycin and of oleandomycin, namely Streptomyces erythreus ATCC 31772 and Streptomyces antibioticus ATCC 31771, using as the substrate a derivative of erythronolide A, namely (8S)-8-fluoroerythronolide A, a derivative of erythronolide B, namely (8S)-8-fluoroerythronolide B, or a derivative of 3-O-mycarosyl-erythronolide B, namely 3-O-mycarosyl-(8S)-fluoroerythronolide B, the corresponding (8S)-8-fluoro derivatives of the erythromycins A, B, C and D, as well as 3-O-oleandrosyl-5-desosaminyl-(8S)-8-fluoroerythronolide A and 3-O-oleandrosyl-5-O-desosaminyl-(8S)-8-fluoroerythronolide B, all belonging to the class of the macrolide antibiotics are obtained.Type: GrantFiled: January 8, 1982Date of Patent: March 27, 1984Assignee: Pierrel S.p.A.Inventors: Luciano Toscano, Leonardo M. Cappelletti
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Patent number: 4434097Abstract: A process for the removal of the formyl group in N-formylated peptides or their esters is described. The N-formyl compound is reacted with hydrazine or a substituted hydrazine of formula I: ##STR1## at a pH between 1 and 3.5, keeping the pH constant during the reaction. The process is particularly useful for the preparation of aspartam.Type: GrantFiled: April 26, 1982Date of Patent: February 28, 1984Assignee: Pierrel S.p.A.Inventors: Vincenzo Giobbio, Giorgio Ornato, Livio Buracchi, Alberto Mangia
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Patent number: 4429115Abstract: The fermentation of a substrate selected among erythronolide B, erythronolide A and erythronolide A oxime with a novel mutant, Streptomyces antibioticus ATCC 31771, obtained from an industrial stock for the production of oleandomycin, said novel mutant being incapable of producing the same oleandomycin, permits novel macrolide antibiotics to be produced, having not only an activity range like that of erythromycin, but characterized by a greater stability in acidic environment, whereby for the administration of antibiotic it is no longer necessary to have recourse to esters and/or salts highly toxic for the organism.Type: GrantFiled: January 8, 1982Date of Patent: January 31, 1984Assignee: Pierrel S.p.A.Inventors: Leonardo M. Cappelletti, Roberto Spagnoli, Luciano Toscano
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Patent number: 4390533Abstract: The present invention relates to 2-chloro-6.beta.-fluoro-pregna-1,4-diene-3,20-diones having good anti-inflammatory activity, to processes for their preparation and pharmaceutical compositions thereof.Type: GrantFiled: February 23, 1981Date of Patent: June 28, 1983Assignee: Pierrel, S.p.A.Inventors: Mario Riva, Luciano Toscano
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Patent number: 4347247Abstract: A pharmacological preparation for use in animal husbandry, consists essentially of sodium bicarbonate and an active ingredient which is either 2-methyl-3 (.beta.-hydroxyethylcarbamoyl) quinoxaline-1,4-di-N-oxide or N.sub.1, N.sub.4 -dioxo-quinoxaline-2-methyleneimino-N-methylurethane. The sodium bicarbonate imparts fireproofness to what would otherwise be a highly flammable preparation.Type: GrantFiled: May 1, 1980Date of Patent: August 31, 1982Assignee: Pierrel S.p.A.Inventors: Vincenzo Giobbio, Livio Buracchi
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Patent number: 4299962Abstract: 2-Sulphanilamido-3-methoxypyrazine is produced in high purity and good yield, by reacting 2,3-dichloropyrazine with sulphanilamide in the presence of potassium carbonate, an aprotic solvent such as dimethylformamide and a second solvent such as toluene which is inert toward the reagents and is adapted to remove the water of reaction.Type: GrantFiled: January 22, 1980Date of Patent: November 10, 1981Assignee: Pierrel S.p.A.Inventors: Vincenzo Giobbio, Giorgio Ornato, Livio Buracchi
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Patent number: 4275061Abstract: The present invention relates to 2-chloro-6.beta.-fluoropregna-1,4-diene-3,20-diones having good anti-inflammatory activity, to processes for their preparation and pharmaceutical compositions thereof.Type: GrantFiled: March 27, 1979Date of Patent: June 23, 1981Assignee: Pierrel S.p.A.Inventors: Mario Riva, Luciano Toscano
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Patent number: 4272446Abstract: Novel steroids are described together with processes of making them and pharmaceutical compositions containing them. The steroids have pharmaceutical activity, especially antiinflammatory activity. They are all 2-Bromo-6.beta.-fluoro-pregna-1,4-diene-3,20-diones.Type: GrantFiled: January 12, 1979Date of Patent: June 9, 1981Assignee: Pierrel S.p.A.Inventors: Mario Riva, Luciano Toscano
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Patent number: 4226862Abstract: Novel steroids are described together with processes of making them and pharmaceutical compositions containing them. The steroids have pharmaceutical activity, especially anti-inflammatory activity. They are all 2-Bromo-6.beta.-fluoro-pregna-1,4-diene-3,20-diones.Type: GrantFiled: February 26, 1975Date of Patent: October 7, 1980Assignee: Pierrel S.p.A.Inventors: Mario Riva, Gaetano Palladino, Lucian Toscano
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Patent number: 4181740Abstract: The present invention provides 1-(p-azidobenzoyl)-5-methoxy-2-methyl-3-indolylacetic acid and its pharmaceutically acceptable salts and esters and processes of preparation.Type: GrantFiled: May 13, 1977Date of Patent: January 1, 1980Assignee: Pierrel S.p.A.Inventors: Silvia Tricerri Zumin, Alberto Bianchetti
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Patent number: 4073903Abstract: The present invention relates to a novel therapeutically active derivative of 7-aminocephalosporanic acid which is 7- 1-(1H-4-nitroimidazolyl)acetyl!amino-3- 5-(1H-1-methyltetrazolyl)thio!m ethyl-3-cephem-4-carboxylic acid.Type: GrantFiled: September 27, 1976Date of Patent: February 14, 1978Assignee: Pierrel S.p.A.Inventors: Silvia Zumin Tricerri, Lino Chiarani
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Patent number: 4013679Abstract: This invention relates to compounds of the formula: ##STR1## wherein R.sub.1 and R.sub.2 may be the same or different and include hydrogen, methyl, and benzyl, their method of preparation, and pharmaceutical compositions containing these compounds.Type: GrantFiled: June 30, 1975Date of Patent: March 22, 1977Assignee: Pierrel S.p.A.Inventors: Mario Riva, Luciano Toscano, Giampiero Grisanti, Alberto Bianchetti