Patents Assigned to Gruppo Lepetit S.p.A.
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Patent number: 4211709Abstract: Pharmacologically-active aminopyrrole derivatives of the formula ##STR1## wherein: R is selected from hydrogen, (C.sub.1-4)alkyl, benzyl and chlorobenzyl;R.sub.1 is selected from hydrogen, (C.sub.1-4)alkyl, phenyl and phenyl substituted by a radical selected from methyl, ethyl, methoxy, ethoxy, benzyloxy, fluoro, chloro and bromo;R.sub.2 and R.sub.3 individually represent hydrogen or (C.sub.1-4)alkyl or, taken together, represent an isopropylidene, a benzylidene or a chlorobenzylidene radical;R.sub.4 is selected from (C.sub.2-4)alkanoyl; carbo(C.sub.1-3)alkoxy; benzoyl, benzoyl substituted by a radical selected from chloro, methoxy or ethoxy; carbamoyl, methylcarbamoyl and phenyl carbamoyl;R.sub.5 is selected from hydrogen, (C.sub.1-4)alkyl, carbo(C.sub.1-3)alkoxy, carbomethoxymethyl, carbethoxymethyl, trifluoromethyl and carbamoyl, with the proviso that when R is hydrogen, R.sub.1 and R.sub.5 are methyl and R.sub.4 is carbethoxy, and R.sub.2 and R.sub.Type: GrantFiled: November 13, 1978Date of Patent: July 8, 1980Assignee: Gruppo Lepetit S.p.A.Inventors: Giorgio Tarzia, Gianbattista Panzone
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Patent number: 4201865Abstract: Novel prostaglandin analogues of the following general formula ##STR1## wherein R is an alkyl group from 1 to 4 carbon atoms, e.g. methyl, ethyl, propyl, isopropyl, butyl, isobutyl or tert-buytyl, R.sub.1 is hydrogen, R.sub.2 is hydroxyor R.sub.1 and R.sub.2 taken together represent a group oxo, R.sub.3 is hydrogen or methyl. The new compounds have antisecretory utility.Type: GrantFiled: February 10, 1978Date of Patent: May 6, 1980Assignee: Gruppo Lepetit S.p.A.Inventors: Umberto Guzzi, Romeo Ciabatti
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Patent number: 4198502Abstract: Pharmacologically-active aminopyrrole derivatives of the formula ##STR1## wherein: R is selected from hydrogen, (C.sub.1-4)alkyl, benzyl and chlorobenzyl;R.sub.1 is selected from hydrogen, (C.sub.1-4)alkyl, phenyl and phenyl substituted by a radical selected from methyl, ethyl, methoxy, ethoxy, benzyloxy, fluoro, chloro and bromo;R.sub.2 and R.sub.3 taken together, represent a benzylidene or a chlorobenzylidene radical;R.sub.4 is selected from (C.sub.2-4)alkanoyl; benzoyl, and benzoyl substituted by a radical selected from chloro, methoxy or ethoxy;R.sub.5 is selected from hydrogen, (C.sub.1-4)alkyl, or trifluoromethyl anda salt thereof with a pharmaceutically-acceptable acid.The compounds have anti-inflammatory and CNS-depressant utility. They are also useful as analgesics and antipyretics and display a very low degree of anti-ulcerogenic activity.Type: GrantFiled: November 13, 1978Date of Patent: April 15, 1980Assignee: Gruppo Lepetit S.p.A.Inventors: Giorgio Tarzia, Gianbattista Panzone
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Patent number: 4189606Abstract: Prostaglandin derivatives wherein the atom at the position 13 of the lower side-chain is replaced by nitrogen. The new compounds have abortifacient activity.Type: GrantFiled: March 22, 1979Date of Patent: February 19, 1980Assignee: Gruppo Lepetit S.p.A.Inventors: Duccio Favara, Umberto Guzzi
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Patent number: 4188321Abstract: The invention is concerned with a new class of rifamycins, namely, the 25-desacetylrifamycins, and with a process for their preparation. The new compounds display antibacterial activity quite similar to that shown by the parent 25-acetylrifamycins, and are characterized by a higher solubility and a lower toxicity than the parent substances.Type: GrantFiled: October 30, 1967Date of Patent: February 12, 1980Assignee: Gruppo Lepetit S.p.A.Inventors: Nicola Maggi, Piero Sensi
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Patent number: 4182903Abstract: Prostaglandin derivatives wherein the atom at the position 13 of the lower side-chain is replaced by nitrogen.The new compounds have abortifacient activity.Type: GrantFiled: February 2, 1977Date of Patent: January 8, 1980Assignee: Gruppo Lepetit S.p.A.Inventors: Duccio Favara, Umberto Guzzi
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Patent number: 4169834Abstract: A process for preparing 4-deoxy-thiazolo[5,4-c]rifamycin SV derivatives of the following general formula ##STR1## wherein R represents hydrogen or a straight or branched alkyl chain containing from 1 to 10 carbon atoms, R.sub.1 is selected from hydrogen and acetyl.Compounds of formula I above, wherein R is a straight or branched alkyl chain containing from 1 to 10 carbon atoms, R.sub.1 is selected from hydrogen and acetyl. These compounds possess antimicrobial utility.Type: GrantFiled: March 22, 1978Date of Patent: October 2, 1979Assignee: Gruppo Lepetit S.p.A.Inventor: Renato Cricchio
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Patent number: 4144234Abstract: A method for preparing thiazolorifamycin derivatives from rifamycin S and a cysteine ester to produce an intermediate product which is cyclized to thiazolorifamycin and the novel products formed therefrom.Type: GrantFiled: May 12, 1977Date of Patent: March 13, 1979Assignee: Gruppo Lepetit S.p.A.Inventor: Renato Cricchio
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Patent number: 4143055Abstract: New 2,4,6-trisubstituted-2,3-dihydro-benzofuran derivatives of the following general formula ##STR1## wherein R is selected from hydrogen or methyl; one of R.sub.1 and R.sub.2 represents hydroxy, (C.sub.1-4)alkoxy or (C.sub.2-4)alkanoyloxy, and the other one is selected from cyano, carboxy, carbo(C.sub.1-4)alkoxy, carbamoyl and a --NR.sub.3 R.sub.4 group, wherein R.sub.3 and R.sub.4 independently represent hydrogen (C.sub.1-4)alkyl, (C.sub.2-4)alkanoyl, carbo(C.sub.1-4)alkoxy, carbobenzyloxy, carbamoyl, mono- and di-(C.sub.1-4)alkylamino-(C.sub.1-4)alkyl, benzenesulfonyl, toluenesulfonyl, (C.sub.1-4)alkylsulfonyl or phenacylsulfonyl; and salts therewith of pharmaceutically acceptable acids. The compounds have antinflammatory, analgesic and antipyretic utility.Type: GrantFiled: March 27, 1978Date of Patent: March 6, 1979Assignee: Gruppo Lepetit S.p.A.Inventor: Emilio Occelli
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Patent number: 4140696Abstract: Pharmacologically-active aminopyrrole derivatives of the formula ##STR1## wherein: R is selected from hydrogen, (C.sub.1-4)alkyl, benzyl and chlorobenzyl;R.sub.1 is selected from hydrogen, (C.sub.1-4)alkyl, phenyl and phenyl substituted by a radical selected from methyl, ethyl, methoxy, ethoxy, benzyloxy, fluoro, chloro and bromo;R.sub.2 and R.sub.3 individually represent hydrogen or (C.sub.1-4)alkyl or, taken together, represent an isopropylidene, a benzylidene or a chlorobenzylidene radical;R.sub.4 is selected from (C.sub.2-4)alkanoyl; carbo(C.sub.1-3)alkoxy; benzoyl, benzoyl substituted by a radical selected from chloro, methoxy or ethoxy; carbamoyl, methylcarbamoyl and phenyl carbamoyl;R.sub.5 is selected from hydrogen, (C.sub.1-4)alkyl, carbo(C.sub.1-3)alkoxy, carbomethoxymethyl, carbethoxymethyl, trifluoromethyl and carbamoyl, with the proviso that when R is hydrogen, R.sub.1 and R.sub.5 are methyl and R.sub.4 is carbethoxy, R.sub.2 and R.sub.Type: GrantFiled: December 15, 1976Date of Patent: February 20, 1979Assignee: Gruppo Lepetit S.p.A.Inventors: Giorgio Tarzia, Gianbattista Panzone
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Patent number: 4129562Abstract: Novel 4-desoxy-thiazolo[5,4-c]rifamycin SV derivatives having antibacterial activity and a method of preparing same by the reaction of rifamycin S with a cysteine derivative followed by the oxidation of the resulting product.Type: GrantFiled: May 12, 1977Date of Patent: December 12, 1978Assignee: Gruppo Lepetit S.p.A.Inventor: Renato Cricchio
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Patent number: 4119635Abstract: New 1-alkyl-3,5-disubstituted-1,2,4-triazole derivatives of following formula I ##STR1## wherein R may represent phenyl; phenyl substituted by a radical selected from (C.sub.1-4)alkyl, e.g. methyl, ethyl, propyl, isopropyl, butyl, sec.-butyl, isobutyl or tert.-butyl, (C.sub.1-4)alkoxy, e.g. methoxy, ethoxy, propoxy, butoxy, isobutyloxy or tert.-butoxy, fluoro, chloro, bromo, nitro, amino, cyano, carbamoyl, carboxy, hydroxymethyl, methylenedioxy and trifluoromethyl; dichlorophenyl; dimethoxyphenyl; 3,4,5-trimethoxyphenyl;R.sub.1 may represent phenyl, phenyl substituted by a radical selected from (C.sub.1-4)alkyl as above defined, (C.sub.1-4)alkoxy as above defined; fluoro, chloro, bromo, hydroxymethyl, (C.sub.2-4)aliphatic acyloxymethyl, e.g. acetoxymethyl, propionyloxymethyl or butyryloxymethyl, carbamoyloxymethyl, bromomethyl and dimethylaminomethyl; dimethylphenyl; dimethoxyphenyl; phenyl contemporaneously substituted by o-hydroxymethyl and chloro;R.sub.2 represents a (C.sub.Type: GrantFiled: September 3, 1976Date of Patent: October 10, 1978Assignee: Gruppo Lepetit S.p.A.Inventors: Amedeo Omodei-Sale, Giorgio Pifferi, Pietro Consonni, Alberto Diena, Bonaccorso Rosselli del Turco
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Patent number: 4113731Abstract: Fused isoquinoline derivatives of the general formula ##STR1## wherein: A is a divalent radical selected from the groups ##STR2## wherein R.sub.3 and R.sub.4 each independently represents hydrogen, alkyl,, alkenyl, cycloalkyl, aryl, aralkyl, aralkenyl, cycloalkyl-alkyl or, taken together with the adjacent double bond, represent a cycloalkene containing from 5 to 8 carbon atoms or an aromatic nucleus;R.sub.5 represents hydrogen, hydroxyl, alkyl, alkenyl, cycloalkyl, aryl, aralkyl, aralkenyl or cycloalkyl-alkyl;Y is .dbd.O, .dbd.S or .dbd.NH;X is --O--, --S-- or --NR.sub.6 -- wherein R.sub.6 represents hydrogen, alkyl, cycloalkyl, aryl, aralkyl or cycloalkyl-alkyl;R.sub.1 and R.sub.2 each independently represents hydrogen, alkyl, phenyl, cycloalkyl, alkoxy, alkenyloxy, methylenedioxy, cycloalkoxy, halo or di-alkylamino or, taken together with the adjacent carbon atoms of the benzene ring, form a cycloalkenyl group containing 5 or 6 carbon atoms or an aromatic nucleus fused on the benzene ring.Type: GrantFiled: August 9, 1976Date of Patent: September 12, 1978Assignee: Gruppo Lepetit S.p.A.Inventors: Giorgio Winters, Nunzio DiMola
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Patent number: 4113953Abstract: 2-Nitroimidazole derivatives of the following formula: ##STR1## wherein R is benzoyl, phenylcarbamoyl or the group ##STR2## wherein R.sub.1 is C.sub.1-4 alkyl, ##STR3## in which R.sub.2 is hydrogen, halo, cyano, amino, C.sub.1-2 alkyl, or C.sub.1-3 alkoxy and X is oxygen or sulfur. These compounds have antimicrobial and amoebicidal utilities.Type: GrantFiled: January 17, 1977Date of Patent: September 12, 1978Assignee: Gruppo Lepetit S.p.A.Inventors: Bruno Cavalleri, Giancarlo Volpe
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Patent number: 4075341Abstract: A new process for preparing s-triazolo[5,1-a]-isoquinoline derivatives of the formula ##STR1## wherein A represents the group --CH.sub.2 --CH.sub.2 -- or --CH.dbd.CH--; R is selected from hydrogen, amino, lower alkylamino, di-lower alkylamino, acylamino, diacylamino, ureido, thioureido, carbethoxythioureido, benzoylthioureido, sulfhydryl, lower alkyl, trifluoromethyl, phenyl, substituted phenyl, pyridyl, methylpyridyl and dimethylpyridyl; and R.sub.1 and R.sub.2 each independently represents hydrogen or lower alkoxy; by condensation of a 2-amino-3,4-dihydro-1(2H)-isoquinolinone with an imidolyl, cyanamide, cyanic or thiocyanic derivative.New compounds of the formula I wherein A represents the group --CH.sub.2 --CH.sub.2 -- or --CH.dbd.CH--, R has the same meaning as above with the exclusion of hydrogen, methyl, phenyl, and trifluoromethyl, R.sub.1 and R.sub.2 have the same meaning as above, with the proviso that when A represents the group --CH.dbd.CH--, R cannot be tolyl or pyridyl.Type: GrantFiled: November 28, 1975Date of Patent: February 21, 1978Assignee: Gruppo Lepetit S.p.A.Inventors: Amedeo Omodei-Sale, Pietro Consonni, Leonard Lerner
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Patent number: 4075342Abstract: Novel tricyclic compounds containing two ring notrogen atoms and represented by the following formula I ##STR1## wherein: A is one of the groups --CH.sub.2 --; --CH.dbd.CH--; and --CH.sub.2 --CH.sub.2 --;R is hydrogen, lower alkyl, lower alkoxy, lower alkenyloxy, lower alkynyloxy, cyclo(C.sub.3-6 alkyl)oxy, hydroxy, benzyloxy, halo, sulfamoyl, cyano, trifluoromethyl or nitro; R.sub.1 is hydrogen, lower alkoxy or halo; or R and R.sub.1 taken together are methylenedioxy; the sequence ##STR2## is one of the following moieties: ##STR3## WHEREIN R.sub.2 is hydrogen or lower alkyl; R.sub.3 is hydrogen or lower alkyl; R.sub.4 is hydrogen, methyl, carboxy, carbo(lower alkoxy), carbamyl, mono- or di-(lower alkyl) carbamyl or hydroxymethyl; provided that when the sequence ##STR4## is one of the moieties a) and b) wherein R.sub.2 is hydrogen or lower alkyl, A is not --CH.dbd.CH--; when the sequence ##STR5## is one of the moieties (a) and (b) wherein R.sub.2 is hydrogen, A is not --CH.sub.Type: GrantFiled: November 6, 1975Date of Patent: February 21, 1978Assignee: Gruppo Lepetit, S.p.A.Inventors: Amedeo Omodie Sale, Emilio Toia, Giulio Galliani, Leonard J. Lerner
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Patent number: 4075241Abstract: The compounds 2-Aryl-3-amino-1-butanol derivatives of the formula ##STR1## wherein R represents hydrogen or acyl; R.sup.1 and R.sup.2 each independently represents hydrogen, phenyl lower alkyl, or lower alkoxy substituted phenyl lower alkyl, or both R.sup.1 and R.sup.2 are lower alkyl; and their pharmaceutically acceptable acid salts.The compounds are crystalline solids or liquids which, having two asymmetry centers, can be obtained in their stereoisomeric forms as racemic mixtures or in their optically active forms. The compounds have cardiovascular activity as coronary dilators.The compounds can be prepared by reacting an .alpha.-arylcrotonate with ammonia or with an amine followed by hydrogenation of the carbalkoxy group to give the corresponding butanol. The butanols are acylated in usual ways to give the compounds of formula (I) wherein R represents an acyl group.Type: GrantFiled: May 8, 1972Date of Patent: February 21, 1978Assignee: Gruppo Lepetit S.p.A.Inventors: Elvio Bellasio, Franco Cristiani
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Patent number: 4072689Abstract: Pharmacologically active 2,4,5-trisubstituted oxazoles of the general formula ##STR1## wherein A is cyclohexyl, thienyl or a group of the formula ##STR2## in which R represents one to three substituents each independently selected from the group consisting of hydrogen, lower alkyl, halo, halo-lower alkyl, lower alkoxy, nitro, cyano, amino, carbamoyl, acetamino or carboxy; one of the R.sub.1 and R.sub.2 groups is a lower alkyl group and the other is an amido group, ##STR3## wherein R.sub.3 is selected from the group consisting of hydrogen, lower alkyl, lower alkenyl, cycloalkyl, phenyl, substituted phenyl, phenyl-lower alkyl, hydroxy-lower alkyl, lower acyloxy-lower alkyl, hydroxy, amino, lower alkylideneamino, cycloalkylideneamino, benzylideneamino and R.sub.4 is selected from hydrogen, lower alkyl, lower alkenyl, cycloalkyl, phenyl, substituted phenyl, phenyl-lower alkyl, hydroxy-lower alkyl, lower acyloxy-lower alkyl, or R.sub.3 and R.sub.Type: GrantFiled: December 17, 1975Date of Patent: February 7, 1978Assignee: Gruppo Lepetit S.p.A.Inventor: Giorgio Tarzia
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Patent number: 4042683Abstract: This invention is directed to rifamycin compounds which are produced by fermentation of Nocardia mediterranea ATCC 31064, ATCC 31065 or ATCC 31066 in an aqueous nutrient medium under aerobic conditions. These rifamycins are referred to as rifamycin P, rifamycin Q, rifamycin R and rifamycin U.Type: GrantFiled: August 4, 1975Date of Patent: August 16, 1977Assignee: Gruppo Lepetit S.p.A.Inventors: Richard J. White, Giancarlo Lancini, Piero Antonini
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Patent number: 4041168Abstract: The compound 5-[(1-hydroxy-1-methyl)ethyl]-1-methyl-2-nitroimidazole is valuable in combatting Trichomonas vaginalis infections in mammals.Type: GrantFiled: December 29, 1975Date of Patent: August 9, 1977Assignee: Gruppo Lepetit S.p.A.Inventors: Alessandro Assandri, Giancarlo Lancini, Giancarlo Volpe, Bruno Cavalleri