Patents Assigned to Farmitalia Carlo Erba
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Patent number: 5420296Abstract: The invention relates to ureido derivatives of substituted pyrroles of formula ##STR1## wherein each of m and n, being the same, is an integer of 1 to 3; W is oxygen of sulphur;each of the B groups, which are the same, isa) a saturated or unsaturated, carbocyclic or condensed carbocyclic ring substituted by one or more acid groups;b) a saturated or unsaturated, heteromonocyclic or heterobicyclic ring, containing one or more heteroatoms chosen from nitrogen, oxygen and sulphur, substituted by one or more acid groups;c) a pyranyl or furanyl sugar residue substituted by one or more acid groups; ord) a --CH.sub.2 (CHA).sub.r CH.sub.2 A group, wherein each A group, being the same or different, is an acid group and r is 0, 1 or 2; and the pharmaceutically acceptable salts thereof, which are useful as angiogenesis inhibitors.Type: GrantFiled: May 25, 1993Date of Patent: May 30, 1995Assignee: Farmitalia Carlo Erba S r lInventors: Nicola Mongelli, Giovanni Biasoli, Alfredo Paio, Maria Grandi, Marina Ciomei
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Patent number: 5418238Abstract: A compound of formula (I): ##STR1## wherein R is a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group;A is a single bond or a straight or branched C.sub.1 -C.sub.6 alkylene chain;R.sub.1 is a hydrogen atom or a C.sub.1 -C.sub.6 alkyl group;R.sub.2 is a C.sub.1 -C.sub.6 alkyl group, a C.sub.5 -C.sub.7 cycloalkyl or a C.sub.6 -C.sub.10 cycloalkylalkyl group, aryl or a C.sub.7 -C.sub.10 arylalkyl group, or a C.sub.6 -C.sub.10 heterocyclylalkyl group;R.sub.3 is hydrogen, a C.sub.1 -C.sub.4 alkyl group or an aryl or a C.sub.7 -C.sub.10 arylalkyl group;Z is a C.sub.1 -C.sub.6 alkyl group, an --OR.sub.5 group wherein R.sub.5 is a C.sub.1 -C.sub.6 alkyl group, ##STR2## group wherein each of R.sub.6 and R.sub.7 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.5 -C.sub.7 cycloalkyl, phenyl or R.sub.6 and R.sub.7 taken together with the nitrogen to which they are linked form a pentatomic or hexatomic saturated heteromonocyclic ring; and the symbol represents a single or a double bond, is a testosterone 68 5.alpha.Type: GrantFiled: July 29, 1993Date of Patent: May 23, 1995Assignee: Farmitalia Carlo Erba S.R.L.Inventors: Achille Panzeri, Marcella Nesi, Enrico di Salle
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Patent number: 5416208Abstract: Antibacterial penems of formula (I), where R represents a hydrogen atom or a hydroxy protecting group, are prepared by reacting a .beta.-lactam of formula (II) with an oxalyl halide in an inert solvent in the presence of an organic or inorganic base or an acid scavenger to produce a compound of formula (III), wherein X is a halogen atom, treating the resultant compound of formula (III) with a 1,3-dioxolen-2-one of formula (IV), wherein Y is a hydroxy group, in the presence of molecular sieves or an organic or inorganic base to produce a compound of formula (V), and cyclizing the compound of formula (V) in the presence of a trialkylphosphite to provide the penems of formula (I).Type: GrantFiled: February 22, 1994Date of Patent: May 16, 1995Assignee: Farmitalia Carlo Erba S r lInventors: Ettore Perrone, Marco Alpegiani, Franco Zarini, Giuseppe Mazzini, Giovanni Franceschi
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Patent number: 5412081Abstract: Anthracycline glycosides having the general formula 1 and 2: ##STR1## wherein R.sub.1 is selected from the group consisting of hydrogen, fluorine, hydroxy or amino; R.sub.2 and R.sub.3 represent hydroxy or one of R.sub.2 and R.sub.3 is a hydrogen atom, a nitro or an amino group and the other of R.sub.2 and R.sub.3 is a HYDROXY group, exhibit activity against LoVo and LoVo/Dx in vitro.Type: GrantFiled: January 6, 1993Date of Patent: May 2, 1995Assignee: Farmitalia Carlo Erba S.R.L.Inventors: Francesco Angelucci, Alberto Bargiotti, Daniela Faiardi, Stefania Stefanelli, Antonino Suarato
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Patent number: 5409949Abstract: The invention provides new methylen-indole derivatives of formula (I) ##STR1## wherein R is a group ##STR2## in which R.sub.4 is hydrogen, hydroxy, C.sub.1 -C.sub.6 alkoxy, C.sub.2 -C.sub.6 alkanoyloxy, carboxy, nitro or NHR.sub.7, wherein R.sub.7 is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.5 is hydrogen, C.sub.1 -C.sub.6 alkyl or halogen; andR.sub.6 is hydrogen or C.sub.1 -C.sub.6 alkyl;n is zero, 1 or 2;R.sub.1 is hydrogen, C.sub.1 -C.sub.6 alkyl or C.sub.2 -C.sub.6 alkanoyl;R.sub.2 is hydrogen, C.sub.1 -C.sub.6 alkyl, halogen, cyano, carboxyl, nitro or --NHR.sub.7 in which R.sub.7 is as defined above;R.sub.3 is hydrogen, C.sub.1 -C.sub.6 alkyl or C.sub.2 -C.sub.6 alkanoyl; and the pharmaceutically acceptable salts thereof; and wherein, when, at the same time, R.sub.2 is hydrogen, C.sub.1 -C.sub.6 alkyl, halogen or cyano and R.sub.3 is hydrogen, R.sub.1 and n being as defined above, then at least one of R.sub.4, R.sub.5 and R.sub.6 is other than hydrogen, which are useful as tyrosine kinase inhibitors.Type: GrantFiled: March 12, 1993Date of Patent: April 25, 1995Assignee: Farmitalia Carlo Erba S.r.l.Inventors: Franco Buzzetti, Antonio Longo, Maristella Colombo
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Patent number: 5407939Abstract: Compounds of formula (I) ##STR1## wherein: the symbol represents a single or a double bond;B is a bond or a straight or branched C.sub.1 -C.sub.6 alkylene chain;R is hydrogen or C.sub.1 -C.sub.4 alkyl;R.sub.1 is hydrogen, C.sub.1 -C.sub.6 alkyl or benzyl;R.sub.2 isa) hydrogen, fluorine, C.sub.1 -C.sub.6 alkyl, C.sub.5 -C.sub.7 cycloalkyl or C.sub.6 -C.sub.9 cycloalkylalkyl; orb) aryl or C.sub.7 -C.sub.10 arylalkyl;R.sub.3 isa) hydrogen, fluorine or C.sub.1 -C.sub.4 alkyl; orb) aryl or C.sub.7 -C.sub.10 arylalkyl;R.sub.4 is hydrogen, fluorine, or is absent when Y is a double bond;R.sub.5 is hydrogen, fluorine or C.sub.1 -C.sub.6 alkyl; and when Y is a single bond, A is hydrogen, fluorine or ##STR2## wherein each of R.sub.6, R.sub.7 and R.sub.8 independently is hydrogen, fluorine or C.sub.1 -C.sub.6 alkyl; and when Y is a double bond, A is a ##STR3## wherein each of R.sub.6 and R.sub.7 is independently hydrogen, fluorine or C.sub.1 -C.sub.6 alkyl; with the proviso that at least one of the groups R, R.sub.1, R.Type: GrantFiled: July 29, 1993Date of Patent: April 18, 1995Assignee: Farmitalia Carlo Erba S.R.L.Inventors: Achille Panzeri, Marcella Nesi, Enrico Di Salle
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Patent number: 5401750Abstract: Derivatives of 1-phenyl-3-azabicycloalkylimidazolidin-2-ones are provided of general formula (I) ##STR1## in which inter alia R.sub.3 represents a group ##STR2## wherein n is an integer of 1 or 2 and R.sub.8 is hydrogen, C.sub.1 -C.sub.6 alkyl unsubstituted or substituted by phenyl, C.sub.2 -C.sub.4 alkenyl, C.sub.2 -C.sub.4 alkynyl, formyl or C.sub.2 -C.sub.6 alkanoyl; and the pharmaceutically acceptable salts thereof, which are useful in the treatment of CNS disorders, gut motility disorders, emesis and migraine, as cognition activators, anti-drug addition agents and analgesic.Type: GrantFiled: June 14, 1993Date of Patent: March 28, 1995Assignee: Farmitalia Carlo Erba S.r.l.Inventors: Mario Varasi, Franco Heidempergher, Nicola Carfagna, Ruggero Fariello
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Patent number: 5399679Abstract: There is provided a process for preparing a compound of formula (I) ##STR1## wherein R is H or a hydroxy protecting group, R.sub.2 is an organic residue and R.sub.3 is H or a nitrogen protecting group, which process comprises reacting together a compound of formula (II) ##STR2## wherein R.sub.1 is a C.sub.1 -C.sub.4 alkyl or a phenyl group, R and R.sub.3 are as defined above, a compound of formula (III) ##STR3## wherein R.sub.2 is as defined above and X is a cation or a silicon-containing residue, and a salt of a group IIa, IIb or transition element. The compounds of formula (I) are intermediates in the synthesis of penem antibiotics.Type: GrantFiled: April 30, 1993Date of Patent: March 21, 1995Assignee: Farmitalia Carlo Erba S.r.l.Inventors: Walter Cabri, Ilaria Candiani, Franco Zarini, Angelo Bedeschi
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Patent number: 5397787Abstract: The present invention relates to the compounds of formula (I) ##STR1## wherein one of the groups X.sup.1 to X.sup.4 is N and the others are CH; the rest of the variables are as defined in the specification.Type: GrantFiled: December 22, 1993Date of Patent: March 14, 1995Assignee: Farmitalia Carlo Erba S.R.L.Inventors: Franco Buzzetti, Angelo Crugnola, Dario Ballinari, Felicita Greco
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Patent number: 5391735Abstract: The present invention relates to a new process for the preparation of 3-substituted derivatives of 1-amino-2-hydroxy-propane in the form of single diastereoisomers, to certain of these diastereoisomers, and to compounds which are intermediates in the new process of the invention.Type: GrantFiled: April 12, 1994Date of Patent: February 21, 1995Assignee: Farmitalia Carlo Erba S.p.A.Inventors: Piero Melloni, Arturo D. Torre, Ettore Lazzari, Giuseppe Mazzini
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Patent number: 5391577Abstract: N-phenylalkyl substituted .alpha.-amino carboxamide derivatives of formula (I) ##STR1## wherein R is C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.8 cycloalkyl, furyl, thienyl, pyridyl or unsubstituted or substituted phenyl; A is a --(CH.sub.2).sub.m -- or --(CH.sub.2).sub.p --X--(CH.sub.2).sub.q -- group wherein X is --O--, --S-- or --NR.sub.4 --; R.sub.1, R.sub.2, R.sub.3, R'.sub.3, R.sub.4, n, m, p and q are as herein defined; and each of R.sub.5 and R.sub.6 is independently hydrogen or C.sub.1 -C.sub.6 alkyl, and the pharmaceutically acceptable salts thereof, are active on the central nervous system and can be used as anti-epileptic, anti-Parkinson, neuroprotective, antidepressant, antispastic and/or hypnotic agents in mammals.Type: GrantFiled: May 25, 1993Date of Patent: February 21, 1995Assignee: Farmitalia Carlo Erba S r lInventors: Philippe Dostert, Paolo Pevarello, Franco Heidempergher, Mario Varasi, Alberto Bonsignori, Romeo Roncucci
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Patent number: 5387578Abstract: Conjugate of general formula 1:[A--O--W-Z].sub.a -T 1wherein the moity A--O--is the residue of drug of formula A--O--H in which --O--H is a primary or secondary hydroxyl group; a is an integer of from 1 to 30; W is a group of general formula 2: ##STR1## wherein b is an integer of from 1 to 4, B represents a C.sub.1 -C.sub.3 alkylene group and R.sub.1 and R.sub.2 each independently represent hydrogen, halogen, alkyl, phenyl or substituted phenyl; Z is a spacer group and T is a carrier moiety.Type: GrantFiled: April 3, 1992Date of Patent: February 7, 1995Assignee: Farmitalia Carlo Erba S.r.l.Inventors: Francesco Angelucci, Laura Bersani, Michele Caruso, Marina Ripamonti, Daniela Ruggieri, Antonino Suarato
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Patent number: 5382669Abstract: The invention provides a process for the preparation of ergoline derivatives of the formula I ##STR1## the process comprising reacting an ergoline amide of the formula II with an isocyanate of formula III ##STR2## in presence of a metal catalyst and of a phosphorus compound. The compounds of the formula I are useful antiprolactinic and antiparkinson agents.Type: GrantFiled: March 9, 1993Date of Patent: January 17, 1995Assignee: Farmitalia Carlo Erba S.r.l.Inventors: Ilaria Candiani, Walter Cabri, Angelo Bedeschi, Franco Zarini
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Patent number: 5374626Abstract: The present invention relates to the use as antivirals of compounds of formula: ##STR1## wherein B is a purinic or pyrimidinic heterocycle; X is oxygen or sulphur; R.sup.1 is a hydroxyl group or a hydrogen atom; R.sup.2 is a linear, branched or cyclic, alkyl group of up to twenty carbon atoms; R.sup.3 is as specified for R.sup.2 above or a hydrogen atom, a cation or a polyhydroxy group.Type: GrantFiled: March 12, 1993Date of Patent: December 20, 1994Assignee: Farmitalia Carlo ERBAInventors: Carlo Battistini, Giovanni Franceschi, Domenico Ungheri, Maria A. Verini, Sergio Vioglio
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Patent number: 5374652Abstract: Aryl- and heteroarylethenylene derivatives of formula ##STR1## wherein Y is a mono- or bicyclic ring system chosen from (A), (B), (C), (D), (E), (F) and (G) ##STR2## R is a group of formula R.sub.1 is hydrogen, C.sub.1 -C.sub.6 alkyl or C.sub.2 -C.sub.6 alkanoyl; R.sub.2 is hydrogen, halogen, cyano or C.sub.1 -C.sub.6 alkyl;n is zero or an integer of 1 to 3: n is zero or an integer of 1 to 3 when Y is a ring system (A); it is zero, 1 or 2 when Y is a ring system (B), (E), (F) or (G); or it is zero or 1 when Y is a ring system (C) or (D); and the pharmaceutically acceptable salts thereof; and wherein each of the substituents R, OR.sub.1 and R.sub.2 may be independently on either of the aryl or heteroaryl moieties of the bicyclic ring system (A), (E), (F) and (G), whereas only the benzene moiety may be substituted in the bicyclic ring system (B), are useful as tyrosine kinase activity inhibitors.Type: GrantFiled: September 27, 1993Date of Patent: December 20, 1994Assignee: Farmitalia Carlo Erba S r lInventors: Franco Buzzetti, Antonio Longo, Maristella Colombo
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Patent number: 5364854Abstract: Derivatives of 2,3,3a,4-tetrahydro-2-azabicyclo alkyl-1H-imidazo[5,1,-c][1,4]benzoxazin-1-one are provided of general formula (I) ##STR1## in which inter alia R.sub.3 represents ##STR2## wherein n is an integer of 1 or 2 and R.sub.8 is hydrogen, C.sub.1 -C.sub.6 alkyl unsubstituted or substituted by phenyl, C.sub.2 -C.sub.4 alkenyl, C.sub.2 -C.sub.4 alkynyl, formyl or C.sub.2 -C.sub.6 alkanoyl; and the pharmaceutically acceptable salts thereof, which are useful in the treatment of CNS disorders, gut motility disorders, emesis and migraine, as cognition activators, anti-drug addiction agents and analgesic.Type: GrantFiled: June 3, 1993Date of Patent: November 15, 1994Assignee: Farmitalia Carlo Erba S.r.l.Inventors: Mario Varasi, Franco Heidempergher, Claudio Arrigoni, Carla Caccia
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Patent number: 5364781Abstract: The ability to convert carminomycin to daunorubicin can be conferred on a host by transforming the host with a recombinant vector comprising a DNA having the configuration of restriction sites shown in FIGS. 2, 3 & 4 and nucleotide sequence shown in FIG. 3 of the accompanying drawings or a restriction fragment derived therefrom containing a gene coding for carminomycin 4-O-methyltransferase.Type: GrantFiled: October 9, 1992Date of Patent: November 15, 1994Assignee: Farmitalia Carlo ERBA S.r.lInventors: Charles R. Hutchinson, Krishna M. Madduri, Francesca Torti, Anna L. Colombo
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Patent number: 5364768Abstract: An in vitro process for preparing 6((1R)-hydroxyethyl) penem acids by hydrolyzing the carboxylic ester derivative thereof using an enzyme capable of selectively hydrolyzing the ester group at the 3-position of the carboxylic acid ester using an esterase, acylase or lipase enzyme, wherein the enzymatic hydrolysis is effected at a pH in the range of from 5 to 8 and at a temperature in the range of 20.degree. C. to 40.degree. C.Type: GrantFiled: September 4, 1992Date of Patent: November 15, 1994Assignee: Farmitalia Carlo Erba S.r.l.Inventors: Maria Altamura, Franco Francalanci, Marcello Marchi
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Patent number: 5362831Abstract: A polymer conjugate consisting essentially of: from 90 to 99.9 mol % of units represented by the formula ##STR1## from 0.1 to 5 mol % of units represented by the formula ##STR2## wherein one of R.sub.1 and R.sub.2 is a copolymer residue of the formula ##STR3## and the other one is hydrogen atom; from 0 to 9.9 mol % of units represented by the formula ##STR4## wherein R is a phenyl or t-butoxy group, R.sub.3 is H or an acetyl group, A and A.sub.1 which may be the same or different, represent a chemical single bond, an amino acid residue or peptide spacer selected from .beta. Ala, Gly, Phe-Gly, Phe-Phe-, Leu-Gly, Val-Ala, Phe-Ala, Leu-Phe, Leu-Ala, Phe-Leu-Gly, Phe-Phe-Leu, Leu-Leu-Gly, Phe-Tyr-Ala, Phe-Gly-Phe, Phe-Phe-Gly, Phe-Leu-Gly-Phe, Gly-Phe-Leu-Gly-Phe,-.beta.Ala, Phe-Gly-.beta.Ala, Phe-Phe-.beta.Ala, Leu-Gly-.beta.Ala, Val-Ala-.beta.Ala, Phe-Ala-.beta.Ala, Leu-Phe-.beta.Ala, Leu-Gly-.beta.Ala, Phe-Leu-Gly-.beta.Ala, Phe-Phe-Leu .beta.Ala, Leu-Leu-Gly-.beta.Ala, Phe-Tyr-Ala-.beta.Ala, Phe-Gly-Phe-.Type: GrantFiled: June 16, 1993Date of Patent: November 8, 1994Assignee: Farmitalia Carlo Erba S.r.l.Inventors: Nicola Mongelli, Francesco Angelucci, Enrico Pesenti, Antonino Suarato, Giovanni Biasoli
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Patent number: 5362729Abstract: Compounds which are useful in anti-tumors therapy having the formula (I) ##STR1## wherein Het imidazole, A represents a direct linkage at the phenyl 4-position: R is hydrogen; one of R.sub.3 and R.sub.4 is C.sub.1 -C.sub.3 alkyl unsubstituted or omega substituted by C.sub.1 -C.sub.3 alkoxy, and the other, independently, is:a) C.sub.1 -C.sub.3 alkyl unsubstituted or omega substituted by C.sub.1 -C.sub.3 alkoxy; orb) --(CH.sub.2).sub.m --O--(CH.sub.2).sub.n --NR.sub.a R.sub.b wherein each of m and n, which may be the same or different is an integer of 1 to 3, each of R.sub.a and R.sub.b, which may be the same or different, is hydrogen or C.sub.1 -C.sub.3 alkyl; R.sub.5 is hydrogen or C.sub.1 -C.sub.6 alkyl unsubstituted or substituted by a morpholino;each of R.sub.1 and R.sub.2 is independently a group --OR' wherein R' is C.sub.1 -C.sub.6 alkyl; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: September 1, 1992Date of Patent: November 8, 1994Assignee: Farmitalia Carlo ERBA S.r.l.Inventors: Paolo Cozzi, Maria Menichincheri, Laura Capolongo, Nicola Mongelli