Patents Assigned to ERBA S.R.L.
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Patent number: 5218130Abstract: 4-substituted anthracyclinones of formula (I) ##STR1## wherein R represents a hydrogen atom or a straight or branched alkyl, alkenyl or alkynyl group having from 1 to 10 carbon atoms, are intermediates in the preparation of antitumor anthracycline glycosides of formula (IX): ##STR2## wherein R is as defined above and R.sub.1 is a hydrogen atom or a hydroxy group, and pharmaceutically acceptable salts thereof.Type: GrantFiled: January 25, 1991Date of Patent: June 8, 1993Assignee: Farmitalia Carlo Erba S r lInventors: Walter Cabri, Silvia De Bernardinis, Franco Francalanci, Sergio Penco
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Patent number: 5212166Abstract: The present invention concerns steroidic 5.alpha.-reductase inhibitors having the following formula (I) ##STR1## wherein Y is oxygen or sulphur;R is a group;a) --OR.sub.4, wherein R.sub.4 is hydrogen or a C.sub.1 -C.sub.6 alkyl group;b) ##STR2## wherein each of R.sub.5 and R.sub.6, independently, is hydrogen or a C.sub.1 -C.sub.6 alkyl group;c) ##STR3## wherein R.sub.7 is hydrogen or a C.sub.1 -C.sub.6 alkyl group and W is a group:(i) ##STR4## wherein R.sub.8 is a C.sub.1 -C.sub.6 alkyl group, a C.sub.5 -C.sub.6 cycloalky group, a C.sub.6 -C.sub.6 cycloalkylalkyl group, a phenyl group or a benzyl group; or(ii) ##STR5## wherein R.sub.9 is a C.sub.1 -C.sub.6 alkyl group or a C.sub.5 -C.sub.6 cycloalkyl group; or(iii) ##STR6## wherein R.sub.5 and R.sub.6 are as defined above; d) ##STR7## wherein each of R.sub.10 and R.sub.11 is, independently, hydrogen or a C.sub.1 -C.sub.Type: GrantFiled: May 21, 1992Date of Patent: May 18, 1993Assignee: Farmitalia Carlo Erba S.r.l.Inventors: Achille Panzeri, Marcella Nesi, Enrico Di Salle
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Patent number: 5210194Abstract: Ergoline derivatives of the formula I: ##STR1## wherein R represents hydrogen or C.sub.1 -C.sub.4 alkyl; R.sub.1 represents hydrogen, chlorine, bromine or methyl; either R.sub.2 and R.sub.3 both represent hydrogen or together represent a chemical bond; R.sub.4 represents a C.sub.1 -C.sub.4 hydrocarbon group; each of R.sub.5, R.sub.6, R.sub.8 and R.sub.9 independently represents hydrogen or C.sub.1 -C.sub.4 alkyl; R.sub.7 represents hydrogen, C.sub.1 -C.sub.4 alkyl, phenyl or C.sub.3 -C.sub.7 cycloalkyl and n is 0, 1 or 2; are prepared by reaction between compounds of the formulae II and III: ##STR2## and subsequent cyclization of the resultant compounds. The compounds of the formula I are known useful anxiolytic, antipsychotic and anti-parkinson agents.Type: GrantFiled: September 25, 1991Date of Patent: May 11, 1993Assignee: Farmitalia Carlo Erba S.r.l. An Italian Body CorporateInventors: Sergio Mantegani, Gabriella Traquandi, Tiziano Bandiera, Enzo Brambilla
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Patent number: 5206258Abstract: Heteroaryl-3-oxo-propanenitrile derivatives of formula (I) ##STR1## wherein X represents an oxygen atom or a --CH(R.sub.4)--, --O--CH(R.sub.4)--,--S(O).sub.n --, --S(O).sub.n --CH(R.sub.4)--, --CH(R.sub.4)--O--, --CH(R.sub.4)--S(O).sub.n -- or --CH(R.sub.4)--CH.sub.2 -- group wherein n is 0, 1 or 2; R.sub.1 represents C.sub.1 --C.sub.6 alkyl, pyridyl or unsubstituted or substituted phenyl; R.sub.2, R.sub.3 and R.sub.4 are as herein defined; and Q is hydrogen, carboxy, C.sub.2 -C.sub.7 - alkoxycarbonyl or a --CON(R.sub.a)R.sub.b group, R.sub.a and R.sub.b being as defined herein; and their pharmaceutically acceptable salts are useful in stimulating myelopoiesis in bone marrow suppressed mammals.Type: GrantFiled: March 12, 1991Date of Patent: April 27, 1993Assignee: Farmitalia Carlo Erba S.r.l.Inventors: Gianfederico Doria, Anna M. Isetta, Rinaldo Ferreccio, Mario Ferrari, Maria C. Fornasiero, Domenico Trizio
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Patent number: 5204364Abstract: The present invention relates to new N-imidazolyl and N-imidazolylmethyl derivatives of bicyclic compounds having the general formula (I) ##STR1## Wherein A is a .gtoreq.CR.sub.3 or >CHR.sub.3 group, in which R.sub.3 is hydrogen or C.sub.1 -C.sub.6 alkyl, or a >C.dbd.CR.sub.4 R.sub.5 group, in which each of R.sub.4 and R.sub.5 independently is hydrogen or C.sub.1 -C.sub.5 alkyl;Z is --CH.sub.2 --, --O-- or --S--;n is zero or 1;each of R and R.sub.1 is independently hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.2 is --COCH.sub.2 OH, --CH.sub.2 OR', --COOR', --CONR'R" or --CH.dbd.CH--COOR', in which each of R' and R" independently is hydrogen or C.sub.1 -C.sub.6 alkyl, and the pharmaceutically acceptable salts thereof; and wherein:a) when n is zero, then Z is --CH.sub.2 -- or --O--; whereas when n is one, then Z is --CH.sub.2 --, --O-- or --S--;b) when A is .gtoreq.CR.sub.3 or >CHR.sub.3 in which R.sub.3 is hydrogen, then n is one; andc) when, at the same time, A is >CHR.sub.3 in which R.sub.Type: GrantFiled: June 27, 1990Date of Patent: April 20, 1993Assignee: Farmitalia Carlo Erba, S.r.l.Inventors: Germano Carganico, Paolo Cozzi, Antonio Pillan, Patricia Salvati, Corrado Ferti
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Patent number: 5202325Abstract: Compounds of the formula I ##STR1## wherein n is 1 or 2, R.sub.1 represents a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group, R.sub.2 represents a hydrogen atom and R.sub.3 represents a hydrogen atom or a hydroxy group or R.sub.2 and R.sub.3 together represent a chemical bond, R.sub.4 represents a hydrogen atom, or a phenyl or C.sub.1 -C.sub.4 alkyl group, R.sub.5 represents a C.sub.1 -C.sub.4 alkyl group or an alkyl group and R.sub.6 represents a hydrogen or halogen atom, and the pharmaceutically acceptable salt thereof, are useful for the manufacture of a pharmaceutical composition useful in the treatment of emesis.Type: GrantFiled: July 12, 1990Date of Patent: April 13, 1993Assignee: Farmitalia Carlo Erba S r l.Inventors: Alessandro Rossi, Metilde Buonamici, Lorenzo Pegrassi, Enzo Brambilla
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Patent number: 5200403Abstract: Compounds of the formula I ##STR1## wherein R' is a free or esterified carboxy group or a carboxylate anion and R.sup.2 is an organic group have beta-lactamase inhibition activity. A process for the preparation of the same and pharmaceutical compositions containing these compounds are provided.Type: GrantFiled: July 23, 1991Date of Patent: April 6, 1993Assignee: Farmitalia Carlo Erba S.r.l.Inventors: Marco Alpegiani, Stephen Hanessian, Giuseppe Meinardi, Ettore Perrone
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Patent number: 5180758Abstract: 4-substituted anthracyclinones of general formula (I): ##STR1## wherein R represents a hydrogen atom or a COOR.sub.1 group in which R.sub.1 may be a hydrogen atom or an optionally substituted C.sub.1 -C.sub.10 alkyl group, which are intermediates in the preparation of antitumor anthracycline glycosides, are prepared by:(i)(a) reacting a 4-demethyl-4-sulfonyl-7-deoxy-13-dioxolanyl daunomycinone of formula (V): ##STR2## wherein R' represents an alkyl group having from 1 to 10 carbon atoms optionally substituted by one or more halogen atoms or an aryl group optionally substituted by halogen, alkyl, alkoxy or nitro, in a reducing environment with a catalytic amount of a compound of formula (VIII):ML.sub.n L'.sub.Type: GrantFiled: August 26, 1991Date of Patent: January 19, 1993Assignee: Farmitalia Carlo Erba S.r.l.Inventors: Walter Cabri, Ilaria Candiani, Silvia De Bernardinis, Franco Francalanci
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Patent number: 5178838Abstract: A chemical reagent vial has an elongated shape from the end portions of which extend two lugs, one of which is closed by a frangible membrane which can be broken by a projection of a funnel element which can be screw engaged on a set lug. The other lug having an outer surface at least a portion of which is conical and on which tightly abuts a conical surface of a hollow sleeve which, moreover, tightly engages with a thread of the lug thereon the sleeve is threaded, through the lug at least an outlet hole being formed, which is arranged between the two sealing regions of the sleeve on the lug.Type: GrantFiled: July 19, 1991Date of Patent: January 12, 1993Assignee: Farmitalia Carlo Erba S. R. L.Inventors: Nello Sala, Gilberto Passerini, Mario Buelli, Davide Conti, Rosario D. Lorenzo, Ivo Secondini, Simona Bravi
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Patent number: 5166152Abstract: Compounds having the general formula (I) ##STR1## wherein X represents an oxygen atom or a --S(O).sub.n --group, wherein n is zero, 1 or 2;R represents C.sub.1 -C.sub.6 alkyl, pyridyl or substituted or unsubstituted phenyl;R.sub.2, R.sub.3 and R.sub.4 are as defined herein; and Q represents hydrogen, carboxy, C.sub.2 -C.sub.7 alkoxycarbonyl or a --CON(R.sub.a)'R.sub.b group wherein R.sub.a and R.sub.b are as defined herein; and their pharmaceutically acceptable salts have immunomodulating activity and are useful in particular as immunostimulating agents, in the treatment of neoplastic diseases and acute and chronic infections of both bacterial and viral origin in mammals.Type: GrantFiled: December 20, 1990Date of Patent: November 24, 1992Assignee: Farmitalia Carlo Erba S.r.l.Inventors: Gianfederico Doria, Anna M. Isetta, Mario Ferrari, Domenico Trizio
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Patent number: 5130472Abstract: The present invention relates to a new process for the preparation of Erbstatin and Erbstatin analogs, which can be represented by the following formula (I) ##STR1## wherein R is hydrogen, a lower alkyl or a lower alkanoyl group;n is an integer of 1 to 3;A is --CH.dbd.CH-- or --CH.sub.2 --CH.sub.2 --;R.sub.1 is hydrogen or a lower alkyl group, andR.sub.2 is a hydrogen or halogen atom.Type: GrantFiled: November 2, 1990Date of Patent: July 14, 1992Assignee: Farmitalia Carlo Erba S.r.l.Inventors: Franco Buzzetti, Angelo Crugnola, Paolo Lombardi
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Patent number: 5126333Abstract: A pharmaceutical composition comprising a drug and a dehydrated cyclodextrin having improved dissolution properties, and the process for the preparation thereof.Type: GrantFiled: August 2, 1990Date of Patent: June 30, 1992Assignee: Farmitalia Carlo Erba S.R.L.Inventors: Alessandro Martini, Clara Torricelli, Carlo Confalonieri, Roberto De Ponti
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Patent number: 5124318Abstract: A sealed glass container containing therein a stable, injectable, sterile, pyrogen-free doxorubicin anti-tumor composition in a solution which consists essentially of a physiologically acceptable salt of doxorubicin dissolved in a physiologically acceptable solvent therefor, wherein said solution has not been reconstructed from a lyophilizate, and wherein said solution has a pH of from 2.5-3.5 and a concentration of said doxorubicin of from 0.1 to 100 mg/ml.Type: GrantFiled: January 25, 1990Date of Patent: June 23, 1992Assignee: Farmitalia Carlo Erba S.r.l.Inventors: Gaetano Gatti, Diego Oldani, Giuseppe Bottoni, Carlo Confalonieri, Luciano Gambini, Roberto De Ponti
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Patent number: 5122537Abstract: The invention relates to new arylvinylamide derivatives of formula ##STR1## wherein Y is a bicyclic ring system chosen from (A), (B), (C), (D), and (E); ##STR2## in which m is zero, 1 or 2; R is hydrogen, a C.sub.1 -C.sub.6 alkyl or C.sub.1 -C.sub.6 alkanoyl group;R.sub.1 is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.2 is hydrogen, halogen, cyano or C.sub.1 -C.sub.6 alkyl; andn is an integer of 1 to 3; and wherein each of the substituents --CH.dbd.CHNHCOR.sub.1, OR and R.sub.2 may be independently on either of the aryl and heteroaryl moieties of the bicyclic ring system (A), (C), (D) and (E); whereas only the benzene ring may be substituted in the bicyclic ring system (B),which are useful as tyrosine kinase inhibitors.Type: GrantFiled: November 2, 1990Date of Patent: June 16, 1992Assignee: Farmitalia Carlo Erba S.r.l.Inventors: Franco Buzzetti, Angelo Crugnola
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Patent number: 5103029Abstract: 4-Demethoxy-daunomycinone I: ##STR1## the known aglycone of 4-demethoxy-daunorubicin, is prepared by protecting the 13-keto group of 4-demethyldaunomycinone, sulfonylating the 4-hydroxy group, reacting the sulfonylated compound, in an appropriate reducing environment, with a catalytic amount of a transition metal complex, preferably palladium or nickel with 1,3 diphenylphosphinopropane or 1,1'-bis (diphenylphosphino) ferrocene, and eliminating the 13-dioxolanyl group by treatment with trifluoroacetic acid.Type: GrantFiled: April 6, 1989Date of Patent: April 7, 1992Assignee: Farmitalia Carlo Erba S.r.l.Inventors: Walter Cabri, Silvia de Bernardinis, Franco Francalanci, Sergio Penco
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Patent number: 5091372Abstract: Stable, rapidly soluble, lyophilized injectable preparations comprising an anthracycline glycoside, or a pharmaceutically acceptable salt thereof, as the active drug substance, and use of said preparations in the treatment of tumors.Type: GrantFiled: September 26, 1990Date of Patent: February 25, 1992Assignee: Farmitalia Carlo Erba S.r.l.Inventors: Gaetano Gatti, Diego Oldani, Carlo Confalonieri, Luciano Gambini
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Patent number: 5091373Abstract: Stable, rapidly soluble, lyophilized injectable preparations comprising an anthracycline glycoside, or a pharmaceutically acceptable salt thereof, as the active drug substance, and use of said preparations in the treatment of tumors.Type: GrantFiled: September 28, 1990Date of Patent: February 25, 1992Assignee: Farmitalia Carlo Erba S.r.l.Inventors: Gaetano Gatti, Diego Oldani, Carlo Confalonieri, Luciano Gambini
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Patent number: 5089489Abstract: 6-substituted penem esters of formula (I): ##STR1## wherein R.sub.1 is halogen or a C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, phenyl, phenoxy, benzyl or sulphonyloxy group; R.sub.2 is a C.sub.1 -C.sub.4 alkyl, benzyl diphenylmethyl ##STR2## group where A is C.sub.1 -C.sub.4 alkyl, benzyl, p-nitrobenzyl or p-methoxybenzyl; and R.sub.3 is an organic radical, are elastase inhibitors and thereby useful antiinflammatory and antidegenerative agents.Type: GrantFiled: April 5, 1990Date of Patent: February 18, 1992Assignee: Farmitalia Carlo Erba S.r.l.Inventors: Marco Alpegiani, Ettore Perrone, Piergiuseppe Orezzi, Paolo Carminati, Giuseppe Cassinelli
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Patent number: 5084454Abstract: The present invention relates to compounds having the following formula (I) ##STR1## wherein X represents --O-- or --S--;each of R and R.sub.1, independently, is hydrogen, halogen, hydroxy, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, amino, nitro or trihalo-C.sub.1 -C.sub.6 alkyl;each of R.sub.2 and R.sub.3, independently, is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl or phenyl-C.sub.1 -C.sub.6 alkyl; or R.sub.2 and R.sub.3, taken together with the nitrogen atom to which they are linked, form an unsubstituted or substituted, 6-membered, saturated, heteromonocyclic ring optionally containing a further heteroatom chosen from oxygen, sulphur and nitrogen;each of R.sub.4 and R.sub.5, independently, is hydrogen, halogen, nitro, amino or trihalo-C.sub.1 -C.sub.6 alkyl; and the pharmaceutically acceptable salts thereof. The compounds of the invention are useful in therapy as major tranquilizers e.g., in the management of psychotic disorders.Type: GrantFiled: October 11, 1989Date of Patent: January 28, 1992Assignee: Farmitalia Carlo Erba S.r.l.Inventors: Mario Varasi, Piero Melloni, Maria A. Cervini, Alberto Bonsignori, Roberto Commisso
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Patent number: 5077286Abstract: Compounds of formulae Ia and Ib ##STR1## wherein A is hydrogen atom or an organic residue, R.sup.1 is halogen atom, or an organic group, R.sup.2 is hydrogen or halogen atom, C.sub.1 -C.sub.4 alkyl or alkoxy group, R.sup.3 is hydrogen atom, C.sub.1 -C.sub.4 alkyl or alkoxy group, benzyl or a methylene group and R.sub.4 is an organic residue are disclosed. Compounds (Ia) and (Ib) are endowed with elastase inhibitory activity. A two-step process for their preparation starting from the corresponding 4-carboxy cephem or 3-carboxy penam is also provided.Type: GrantFiled: April 10, 1989Date of Patent: December 31, 1991Assignee: Farmitalia Carlo Erba S.r.l.Inventors: Pierluigi Bissolino, Marco Alpegiani, Ettore Perrone, Piergiuseppe Orezzi, Giuseppe Cassinelli, Giovanni Franceschi