Abstract: A process for the preparation of 4-aminoandrostenediones of formula (I) ##STR1## and pharmaceutically acceptable salts thereof, wherein one of R.sub.1 and R.sub.2 is hydrogen and the other is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl or C.sub.2 -C.sub.6 alkynyl, and the symbol indicates that each of (x) and (y), independently, is a single bond or a double bond, comprising reacting a compound of formula (II) ##STR2## wherein E is a halogen atom and R.sub.1, R.sub.2, (x) and (y) each are as defined as above with ammonia.
Type:
Grant
Filed:
May 10, 1988
Date of Patent:
September 12, 1989
Assignee:
Farmitalia Carlo Erba S.r.l.
Inventors:
Antonio Longo, Fabrizio Orzi, Paolo Lombardi, Maristella Colombo
Abstract: Compounds of formula ##STR1## wherein R is hydrogen atom or C.sub.1 -C.sub.4 alkyl group optionally substituted from halogen atom or hydroxy group optionally protected, A is a Z, Z--O--C--O-- or Z--C)-- residue, wherein Z is phenylene, naphthylene, heterocyclediyl, C.sub.1 -C.sub.7 alkylene, C.sub.2 -C.sub.4 alkenylene, alkynylene, ##STR2## C.sub.3 -C.sub.8 cycloalkylene, aralkylene radical optionally substituted, and O.sup.(+) represents a group +NR.sub.1 R.sub.2 R.sub.3, wherein R.sub.1, R.sub.2 and R.sub.3 are each either:(i) a optionally substituted alkyl, aralkyl or aryl radical or(ii) R.sub.1 is as defined above under (i) and R.sub.2 and R.sub.3, taken together, represent an optionally substituted or fused heterocyclic radical, or(iii) R.sub.1, R.sub.2 and R.sub.3, taken together, represent an optionally substituted azonia-bicyclo or tricyclo radical, or(iv) R.sub.1, R.sub.2 and R.sub.
Type:
Grant
Filed:
April 8, 1986
Date of Patent:
September 5, 1989
Assignee:
Farmitalia Carlo Erba
Inventors:
Ettore Perrone, Marco Alpegiani, Angelo Bedeschi, Franco Zarini, Giovanni Franceschi, Costantino D. Bruna
Abstract: This invention concerns a method and a device to perform the adjustment of the cooling temperature of a trap for samples in an apparatus of gas chromatographic analysis. The method according to the invention is characterized in that the cooling fluid flow fed to the trap is adjusted by varying the vacuum caused by a suction device downstream the trap, which is capable of sucking the cooling fluid from a vessel upstream the trap itself.The device according to the invention is characterized in that it comprises a suction means placed downstream the trap and connected by means of a first duct to an end of the trap itself, the other end of the trap being connected, by a second duct, to a vessel containing the refrigerating fluid.
Type:
Grant
Filed:
July 31, 1987
Date of Patent:
September 5, 1989
Assignee:
Carlo Erba Strumentazione S.p.A.
Inventors:
Fausto Munari, Giovanni Ostan, Bruno Tosi
Abstract: Disclosed is a process for purifying an impure anthracyclinone glycoside by selective adsorption of a slightly acidic aqueous solution of an impure glycoside on at least one resin and subsequent de-absorption of the purified glycoside by elution with acidic water or a mixture of water and a polar solvent.
Type:
Grant
Filed:
February 2, 1987
Date of Patent:
August 29, 1989
Assignee:
Farmitalia Carlo Erba S.p.A.
Inventors:
Ernesto Oppico, Carlo Varesio, Onorino G. Rosa
Abstract: Pharmaceutical compounds of the formula ##STR1## wherein R is H or CH.sub.3, R.sub.1 is H or OCH.sub.3, R.sub.2 is a C.sub.1 -C.sub.4 hydrocarbon group and X is an organic group. Also disclosed is a process for the preparation of these compounds. The compounds have dopamine agonist or antagonist activity.
Type:
Grant
Filed:
March 31, 1987
Date of Patent:
August 29, 1989
Assignee:
Farmitalia Carlo Erba, S.p.A
Inventors:
Luigi Bernardi, Laura Chiodini, Aldemio Temperilli
Abstract: An ergoline derivative of the formula I: ##STR1## wherein R.sub.1 represents hydrogen or a methyl group; R.sub.2 represents hydrogen or a halogen atom, a methyl, cyano or phenyl group or an alkylthio group having from 1 to about 4 carbon atoms; R.sub.3 represents a hydrocarbon group having from 1 to about 4 carbon atoms; R.sub.4 represents hydrogen, a phenyl group or a hydrocarbon group having from 1 to about 4 carbon atoms; wherein either (a) R.sub.6 and R.sub.7 represent a valence bond or hydrogen atoms and R.sub.8 represents a hydrogen atom or a methoxy group, or (b) R.sub.6 represents a hydrogen atom and R.sub.7 and R.sub.8 taken together represent a valence bond; W represents an oxygen atom or an imino group; A represents a group of the formula CHR.sub.5, CH.dbd.CR.sub.5 or CH.sub.2 CHR.sub.5 wherein R.sub.
Abstract: The invention relates to compounds having the general formula (I) ##STR1## and the pharmaceutically acceptable salts thereof, which possess immunomodulating activity and are useful e.g. in the treatment of neoplastic diseases and acute and chronic infections of both bacterial and viral origin in mammals.
Type:
Grant
Filed:
January 15, 1988
Date of Patent:
August 1, 1989
Assignee:
Farmitalia Carlo Erba S.r.l.
Inventors:
Gianfederico Doria, Anna M. Isetta, Mario Ferrari, Domenico Trizio
Abstract: The invention relates to cycloalkyl substituted 4-aminophenyl halo derivatives of formula (I) ##STR1## wherein n is an integer of 1 to 5;A is >C.dbd.O or --CH.sub.2 -- and B is, independently, --O--, --NH-- or --CH.sub.2 --; andeither R is halogen and R.sub.1 is unsubstituted C.sub.1 -C.sub.4 alkyl; or R is hydrogen and R.sub.1 is C.sub.1 -C.sub.4 alkyl substituted by 1 to 4 halogen atoms,including the pharmaceutically acceptable salts thereof. The compounds of the invention show aromatase inhibiting activity and can find use, for example, in the treatment of estrogen-dependent tumors and of prostatic hyperplasia.
Type:
Grant
Filed:
January 11, 1988
Date of Patent:
July 11, 1989
Assignee:
Farmitalia Carlo Erba S.r.l.
Inventors:
Angelo Crugnola, Enrico di Salle, Paolo Lombardi
Abstract: Compounds of the formula I ##STR1## wherein R.sub.1 represents a hydrogen atom or a methyl group, either R.sub.2 and R.sub.3 represent hydrogen atoms or together represent a chemical bond, R.sub.4 represents a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group, R.sub.5 represents a C.sub.1 -C.sub.4 alkyl group or an allyl group and R.sub.6 represents a hydrogen or halogen atom, and pharmaceutically acceptable salts thereof, are disclosed as being useful for the treatment of extrapyramidal syndromes such as Parkinson's disease.
Type:
Grant
Filed:
November 18, 1988
Date of Patent:
July 11, 1989
Assignee:
Farmitalia Carlo Erba
Inventors:
Metilde Buonamici, Lorenzo Pegrassi, Alessandro Rossi, Sergio Mantegani
Abstract: t-Alkyl ergoline derivatives of formula I are produced ##STR1## wherein (R.sub.1 =H, OCH.sub.3 and R.sub.2 =H) or (R.sub.1 +R.sub.2 =a ring bond and R.sub.3 =H, optionally substituted nicotinoyl or 1-oxo-2-cyclopenten-3-yl); and their pharmaceutically acceptable salts.A process for the preparation of these derivatives from lysergol and a t-alkyl alcohol is also described, as are pharmaceutical compositions containing them.
Type:
Grant
Filed:
June 23, 1987
Date of Patent:
June 27, 1989
Assignee:
Farmitalia Carlo Erba S.p.A.
Inventors:
Aldemio Temperilli, Enzo Brambilla, Mauro Gobbini, Maria A. Cervini
Abstract: 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:
Grant
Filed:
August 6, 1986
Date of Patent:
June 20, 1989
Assignee:
Farmitalia Carlo Erba s.r.l.
Inventors:
Gaetano Gatti, Diego Oldani, Carlo Confalonieri, Luciano Gambini
Abstract: Ergoline derivatives of the formula I ##STR1## wherein R.sub.1 represents a hydrogen atom or a methyl group; R.sub.2 represents a hydrogen atom or a methoxy group;R.sub.3 represents a hydrocarbon group having from 1 to 4 carbon atoms;X represents a nitrogen atom and Y represents an oxygen atom, a ##STR2## group wherein R.sub.4 represents a hydrogen atom, a C.sub.1 -C.sub.4 alkyl or a phenyl group, R.sub.5 represents a hydrogen atom, a C.sub.1 -C.sub.4 alkyl, a phenyl, an amino or di(C.sub.1 -C.sub.4 alkyl)amino group and the nitrogen atom of the group ##STR3## is not joined to the nitrogen atom represented by X, or Y represents a nitrogen atom and X represents an oxygen atom or a ##STR4## group wherein R.sub.4 is as above defined; and the pharmaceutically acceptable salt thereof; are useful for treatment of Parkinsonism and dyskinetic symptoms.
Abstract: New anthracycline glycosides having formula: ##STR1## wherein R.sup.1 is hydrogen or hydroxy and either R.sup.2 or R.sup.3 is hydrogen with the other amino-methyl are described. The new compounds and their pharmaceutically acceptable addition salts are useful as antitumour agents.
Type:
Grant
Filed:
September 28, 1987
Date of Patent:
June 13, 1989
Assignee:
Farmitalia Carlo Erba S.p.A.
Inventors:
Alberto Bargiotti, Teresa Bordoni, Pierangelo Zini, Sergio Penco
Abstract: Compounds of the following formula I ##STR1## wherein X represents a sulphur or an oxygen atom,R is hydrogen or a C.sub.1 -C.sub.4 alkyl group either unsubstituted or substituted by one or more substituents chosen from a free or protected hydroxy group and halogen atom;A is a Z, Z--O--CO-- or --Z--CO-- residue, whereinZ represents(a) an optionally substituted phenylene or naphthylene group,(b) an optionally substituted heterocyclediyl radical wherein the hetero ring is mono or bicyclic, saturated or unsaturated containing at least one heteroatom selected from the group of oxygen, sulphur and nitrogen;(c) an optionally substituted linear or branched C.sub.1 -C.sub.7 alkylene radical;(d) a C.sub.2 -C.sub.4 alkenylene or alkynylene group or a group of formula ##STR2## (e) an optionally substituted C.sub.3 -C.sub.8 cycloalkylene ring; (f) an aralkylene radical of the formula ##STR3## wherein n is 1, 2 or 3; andQ.sup.(+) represents a +NR.sub.1 R.sub.2 R.sub.3 group, wherein(i) R.sub.1, R.sub.2, R.sub.
Type:
Grant
Filed:
April 8, 1986
Date of Patent:
June 6, 1989
Assignee:
Farmitalia Carlo Erba
Inventors:
Ettore Perrone, Marco Alpegiani, Angelo Bedeschi, Franco Zarini, Giovanni Franceschi, Costantino D. Bruna
Abstract: A process and an apparatus for performing analyses in liquid chromatography, by ways of a pump capable of drawing a fluid and injecting it at high pressure, through at least a control valve, into a separation column.To obtain maximum precision as required by the analysis, before each analysis or each group of analyses, or with respect to each fluid used, a pump stroke is performed with the pump delivery side shut off in order to record and store the characteristics of compressibility of the fluid. These characteristics are kept into consideration in the subsequent operative stages to obtain an exactly constant delivery of the feed pump to the separation column.
Abstract: The invention relates to compounds having the general formula (I) ##STR1## wherein n is zero, 1 or 2;each of R.sub.1 and R.sub.2 is independently:(a) hydrogen, halogen, trifluoromethyl or C.sub.1 -C.sub.6 alkyl;(b) hydroxy, C.sub.1 -C.sub.6 alkoxy or C.sub.3 -C.sub.4 alkenyloxy;(c) nitro, amino, formylamino or C.sub.2 -C.sub.8 alkanoylamino;R.sub.3 represents hydrogen or C.sub.1 -C.sub.8 alkyl;R.sub.4 is:(a') C.sub.1 -C.sub.20 alkyl, unsubstituted or substituted by ##STR2## wherein each of R.sub.a and R.sub.b is independently phenyl or C.sub.1 -C.sub.6 alkyl, or R.sub.a and R.sub.b, taken together with the nitrogen atom to which they are linked, form a N-pyrrolidinyl, N-piperazinyl, hexahydroazepin-1-yl, thiomorpholino, morpholino or piperidino ring, wherein said heterocyclic rings may be unsubstituted or substituted by C.sub.1 -C.sub.6 alkyl or phenyl;(b') C.sub.5 -C.sub.
Type:
Grant
Filed:
January 26, 1988
Date of Patent:
May 2, 1989
Assignee:
Farmitalia Carlo Erba s.r.l.
Inventors:
Gianfederico Doria, Anna M. Isetta, Mario Ferrari, Domenico Trizio
Abstract: The invention relates to new 6- or 7-methylenandrosta-1,4-diene-3,17-diones of the following formula ##STR1## wherein R is hydrogen or fluorine; R.sub.1 is hydrogen or C.sub.1 -C.sub.6 alkyl; R.sub.2 is hydrogen or halogen; one of R.sub.3 and R.sub.4 is .dbd.CH.sub.2 and the other is hydrogen or C.sub.1 -C.sub.4 alkyl, and when R.sub.3 is .dbd.CH.sub.2, at least one of R and R.sub.4 is other than hydrogen; and the symbol ##STR2## represents a double bond and the symbol ##STR3## represents a single bond when R.sub.3 is .dbd.CH.sub.2 or the symbol ##STR4## represents a single bond and the symbol ##STR5## represents a double bond when R.sub.4 is .dbd.CH.sub.2, which are useful in therapy, in particular as anti-cancer agents.
Type:
Grant
Filed:
July 7, 1987
Date of Patent:
April 25, 1989
Assignee:
Farmitalia Carlo Erba S.r.l.
Inventors:
Franco Buzzetti, Natale Barbugian, Paolo Lombardi, Enrico di Salle
Abstract: The invention relates to 4-substituted 6-alkylidenandrostene-3,17-dione derivatives of the following formula ##STR1## wherein each of R.sub.1, R.sub.2 and R.sub.3 is, independently, hydrogen or C.sub.1 -C.sub.6 alkyl; R.sub.4 is hydrogen of fluorine; (x) represents a single or double bond; and R is, especially, a hydroxy or mercapto or amino group or a functional derivative thereof. The compounds of the invention show aromatase inhibitory activity and may be useful, for instance, in the treatment of hormone-dependent tumors and of prostatic hyperplasia.
Type:
Grant
Filed:
August 18, 1987
Date of Patent:
April 18, 1989
Assignee:
Farmitalia Carlo Erba S.R.L.
Inventors:
Maristella Colombo, Franco Buzzetti, Enrico di Salle, Paolo Lombardi
Abstract: The invention relates to compounds having the general formula (I) ##STR1## and the pharmaceutically acceptable salts thereof, which possess immunomodulating activity and are useful e.g. in the treatment of neoplastic diseases and acute and chronic infections of both bacterial and viral origin in mammals.
Type:
Grant
Filed:
December 31, 1987
Date of Patent:
March 28, 1989
Assignee:
Farmitalia Carlo Erba s.r.l
Inventors:
Gianfederico Doria, Anna M. Isetta, Mario Ferrari, Domenico Trizio
Abstract: The invention relates to new aromatase inhibitor agents having the general formula (I) ##STR1## wherein R.sub.1 is hydrogen or a group=CHR.sub.3 wherein R.sub.3 is hydrogen or C.sub.1 -C.sub.6 alkyl; the symbol indicates the presence of a single or double bond in such a way that, when R.sub.1 is hydrogen, (a) is single bond and (b) is either single or double bond, while, when R.sub.1 is a group.dbd.CHR.sub.3 as defined above, (a) is double bond and (b) is single bond; R.sub.2 is hydrogen or fluorine; and R is(1) a group --OR.sub.4 wherein R.sub.4 is(a) hydrogen;(b) C.sub.1 -C.sub.6 alkyl;(c) a phenyl or benzyl group, each unsubstituted or ring-substituted by one or more substituents chosen from C.sub.1 -C.sub.4 alkyl, halogen, trifluoromethyl, nitro, amino, hydroxy and C.sub.1 -C.sub.4 alkoxy;(d) a group--COR.sub.5 wherein R.sub.5 is(i) a C.sub.1 -C.sub.22 saturated or C.sub.2 -C.sub.22 unsaturated aliphatic hydrocarbon radical;(ii) a C.sub.4 -C.sub.
Type:
Grant
Filed:
August 18, 1987
Date of Patent:
March 7, 1989
Assignee:
Farmitalia Carlo Erba S. R. L.
Inventors:
Franco Buzzetti, Enrico di Salle, Paolo Lombardi