Abstract: The invention concerns a method and an equipment for the simulated distillation, by means of gas chromatography, of petroleum products, capable of characterizing also high boiling products, exceeding C55, over 600 C TBP. A chromatograph is used with a capillary column having a length less than or equal to 10 m, containing an immobilized non polar polydimethylsilicon gum stationary phase with a film thickness less than or equal to 0.2 .mu.m. The sample is introduced through a non vaporizing direct cold on-column injection and the eluted sample is detected by means of a FID detector. The column oven is operated in temperature programming conditions up to temperatures exceeding 400 (up to 430-450 C.).
Type:
Grant
Filed:
December 19, 1985
Date of Patent:
July 12, 1988
Assignee:
Carlo Erba Strumentazione S.p.A.
Inventors:
Sorin Trestianu, Fausto Munari, Carlo Saravalle
Abstract: The invention discloses 4-substituted androstendione derivatives of the following formula (I) ##STR1## wherein R is amino or substituted amino or azido,one of R.sub.1 and R.sub.2 is hydrogen and the other is hydrogen, alkyl, alkenyl or alkynyl, and(x) and (y) are each, independently, a single bond or a double bond.The compounds of formula (I) are useful aromatase inhibitors.
Type:
Grant
Filed:
February 10, 1986
Date of Patent:
July 12, 1988
Assignee:
Farmitalia Carlo Erba, S.p.A.
Inventors:
Franco Faustini, Roberto D'Alessio, Vittoria Villa, Enrico di Salle, Paolo Lombardi
Abstract: Anthracycline glycosides of the general formula (A'): ##STR1## wherein R.sub.1 represents a hydrogen atom, a hydroxy group or a methoxy group; one of R.sub.2 and R.sub.3 represents a hydroxy group and the other of R.sub.2 and R.sub.3 represents a nitro group; and R.sub.4 represents a hydrogen atom or a hydroxy group; and their pharmaceutically acceptable salts; have anti-tumor activity.
Type:
Grant
Filed:
September 26, 1986
Date of Patent:
June 7, 1988
Assignee:
Farmitalia Carlo Erba S.p.A.
Inventors:
Francesco Angelucci, Mauro Gigli, Sergio Penco, Fernando Giuliani
Abstract: Ergoline derivatives of the formula I ##STR1## wherein R.sub.1 =H,CH.sub.3 ; R.sub.2 =H, halogen, CH.sub.3, CN, C.sub.1 -C.sub.4 alkylthio or phenylthio; R.sub.3 =C.sub.1 -C.sub.4 hydrocarbon; R.sub.4 =H, OCH.sub.3 ; R.sub.5 =H and R.sub.6 =--CH.dbd.CH--CONHR.sub.7 or R.sub.5 and R.sub.6 =.dbd.CH--CONHR.sub.7 ; R.sub.7 =2-thiazolyl, 3-pyridazinyl, 1,3,4-thiadiazol-2-yl or 4-pyrimidinyl group optionally substituted, and pharmaceutically acceptable salts thereof, display activity on the Central Nervous System and are useful as antiprolactinic agents. Their preparation and pharmaceutical compositions containing them are also described.
Abstract: A method is disclosed for purifying non-homogeneous systems, known as liposomic suspensions, from non-entrapped drugs wherein said suspensions are treated with liquid or solid polymers of synthetic and organic nature having chemical functionality, which are used as ion-exchangers. The liquid or solid polymers are based on styrene, divinylbenzene, acrylic acid, methacrylic acid, and the like, normally known as ion-exchange resins, and may include carboxylic, phosphonic or sulphonic functions of different matrices. The ion-exchange resins may also include salified quaternary ammonium, primary, secondary and tertiary amminic or phosphinic functions or other functions with different matrices, including phenolformaldehyde, styrene-divinylbenzene, acrylates, methacrylates, hydrocarbons and condensation-resins.
Type:
Grant
Filed:
October 22, 1986
Date of Patent:
May 24, 1988
Assignee:
Farmitalia Carlo Erba S.p.A.
Inventors:
Luigi Moro, Guido Neri, Alessandro Rigamonti
Abstract: Distamycin A derivatives of formula ##STR1## wherein R is (a)--NHR.sub.3, wherein R.sub.3 is(a')--CON(NO)R.sub.4, in which R.sub.4 is C.sub.1 -C.sub.4 alkyl either unsubstituted or substituted by halogen; or(b') --CO(CH.sub.2).sub.m --R.sub.5, in which R.sub.5 is halogen, oxiranyl, methyloxiranyl, aziridinyl, a group ##STR2## or a group ##STR3## and m is zero or an integer of 1 to 4; or (b) ##STR4## wherein either R.sub.6 and R.sub.7 are the same and are each oxiranemethyl, aziridinemethyl, or C.sub.2 -C.sub.4 alkyl 2-substituted by halogen or by a group --OSO.sub.2 R.sub.8, wherein R.sub.8 is C.sub.1 -C.sub.4 alkyl or phenyl, or one of R.sub.6 and R.sub.7 is hydrogen and the other is as defined above; andeach group R.sub.1 is, independently, hydrogen or C.sub.1 -C.sub.4 alkyl, and the pharmaceutically acceptable salts thereof.The compounds are useful as antiviral or antitumor agents.
Abstract: The invention relates to a method and device for direct non-vaporizing on column-injection of samples containing high boiling point and/or medium volatile compounds, in gas chromatographic analysis on capillary column. For reasons of economy, the oven containing the column is maintained at a temperature very mcuh higher than the boiling point of the solvent, while the initial part of the column (at least 10 cm) is cooled during the injection. The quantity of sample and solvent injected is related to the length of the cooled section of the column.
Type:
Grant
Filed:
January 8, 1986
Date of Patent:
March 29, 1988
Assignee:
Carlo Erba Strumentazione S.p.A.
Inventors:
Sorin Trestianu, Fausto Munari, Giovanni Ostan, Carlo Saravalle
Abstract: The present invention relates to new 4-aza-17.beta.-substituted 5.alpha.-androstan-3-ones, to a process for their preparation, to pharmacological compostions containing them, and to the use of said compounds as inhibitors of androgen action by means of testosterone 5-reductase inhibition.
Type:
Grant
Filed:
February 3, 1986
Date of Patent:
March 22, 1988
Assignees:
Farmitalia Carlo Erba, S.p.A., Consiglio Nazionale Delle Ricerche
Inventors:
Gianfranco Cainelli, Giorgio Martelli, Mauro Panunzio, Giuseppe Spunta, Giuliano Nannini, Enrico di Salle
Abstract: Antibacterial compounds of formula (I) ##STR1## wherein, R.sub.1 ' is alkyl or hydroxyalkyl;R.sub.2 is hydrogen or a carboxy protecting group; andY' is a group-S-heterocyclic or pyridyl, which group may be substituted, and pharmaceutically or veterinarily acceptable salts thereof and pharmaceutical compositions containing the same.
Type:
Grant
Filed:
December 11, 1985
Date of Patent:
March 8, 1988
Assignee:
Farmitalia Carlo Erba S.p.A.
Inventors:
Marco Alpegiani, Angelo Bedeschi, Maurizio Foglio, Giovanni Francheschi, Ettore Perrone
Abstract: The invention relates to ergoline derivatives having the general formula (I): ##STR1## where R=H, CH.sub.3 ; R.sub.1 =H, halogen, CH.sub.3, phenylthio, C.sub.1 -C.sub.4 alkylthio; R.sub.2 =H, CH.sub.3 O, and R.sub.3 =H or R.sub.2 +R.sub.3 =chemical bond; R.sub.4 =C.sub.1 -C.sub.4 hydrocarbon; R.sub.5, R.sub.6, R.sub.8, R.sub.9 independently=H, C.sub.1 -C.sub.4 alkyl, or R.sub.5, R.sub.8 independently=H, C.sub.1 -C.sub.4 alkyl and R.sub.6 +R.sub.9 =CH.sub.2 CH.sub.2, CH.sub.2 CH.sub.2 CH.sub.2 ; R.sub.7 =H, C.sub.1 -C.sub.4 alkyl, phenyl, NR'R"; R',R" independently=H, C.sub.1 -C.sub.4 alkyl, acyl or NR'R"=heterocyclic ring; W=0, H.sub.2 ; n=0, 1, 2, and their pharmaceutically acceptable salts, these compounds exhibiting antihypertensive activity making them useful anxiolytic and antipsychotic agents. A process for their preparation and pharmaceutical compositions containing them are also described.
Abstract: A process for preparing compounds of the formula I ##STR1## wherein either (i) each of R.sub.1 and R.sub.2 independently represents H or an organic group, or (ii) NR.sub.1 R.sub.2 is a heterocyclic ring or (iii) R.sub.2 is H and R.sub.1 is ##STR2## wherein each of R.sub.6 and R.sub.7 independently represents H or an organic group, m is 1 or 2, n is 0-3, X is O, S, NH, NR.sub.8, CHNO.sub.2 or CHSO.sub.2 R.sub.4 wherein R.sub.8 and R.sub.4 are organic groups and R.sub.3 represents an organic group is characterized by the following reaction sequence: ##STR3## There are also provided new compounds of the formula I wherein n is 0 and m is 2 and pharmaceutical compositions containing them. These compounds and their pharmaceutically acceptable acid addition salts are active as anti-ulcer agents.
Type:
Grant
Filed:
March 17, 1986
Date of Patent:
December 29, 1987
Assignee:
Farmitalia Carlo Erba S.p.A.
Inventors:
Ugo Scarponi, Anna M. Lazzarini, Daniela Toti, Roberto de Castiglione
Abstract: There are provided compounds of formula ##STR1## wherein R is hydrogen atom or C.sub.1 -C.sub.3 alkyl group optionally substituted from halogen atom or hydroxy group optionally protected, and Q.sup.(+) represents a group ##STR2## wherein R.sub.1, R.sub.2 and R.sub.3 are each either: (i) optionally substituted alkyl, aralkyl or aryl radical or(ii) R.sub.1 is as defined above under (i) and R.sub.2, R.sub.3, taken together, represent an optionally substituted or fused heterocyclic radical or(iii) R.sub.1, R.sub.2, R.sub.3, taken together, represent an optionally substituted azonia-bicyclo or tricyclo radical or(iv) R.sub.1, R.sub.2, R.sub.3, taken together, represent an optionally substituted fused pyridinium radical or(v) R.sub.1, R.sub.2, R.sub.3, taken together, represent an optionally substituted pyrazimium, pyrazolium or pyridazinium radical, and the pharmaceutically or veterinarily acceptable salts thereof.A method of preparation is also provided.The compounds show high antibacterial activity.
Type:
Grant
Filed:
June 24, 1985
Date of Patent:
December 15, 1987
Assignee:
Farmitalia Carlo Erba S.p.A.
Inventors:
Ettore Perrone, Marco Alpegiani, Franco Zarini, Costantino D. Bruna, Giovanni Franceschi
Abstract: A new process is described for the preparation of (5R)-penem derivatives of the general formula I: ##STR1## wherein R.sub.1 represents a hydrogen atom or an organic group; R.sub.2 represents a hydrogen atom or a carboxy protecting group and Y represents a hydrogen or halogen atom or an organic group. A 2-thiacephem derivative of the general formula II: ##STR2## wherein R.sub.1, R.sub.2 and Y have the meanings/given above is oxidized by means of organic peracids to the corresponding sulphone of the general formula III: ##STR3## which is subsequently submitted to a desulphurative ring contraction by extrusion of SO.sub.2 to give exclusively the desired (5R)-penem derivatives of the general formula I.
Type:
Grant
Filed:
January 24, 1986
Date of Patent:
December 15, 1987
Assignee:
Farmitalia Carlo Erba S.p.A.
Inventors:
Marco Alpegiani, Angelo Bedeschi, Maurizio Foglio, Giovanni Franceschi, Ettore Perrone
Abstract: Compounds of formula I: ##STR1## wherein R.sub.1 represents a hydrogen atom or a methyl group; R.sub.2 represents a hydrogen or halogen atom or a methyl, cyano, C.sub.1 -C.sub.4 alkylthio or phenylthio group; R.sub.7 and R.sub.8 represent hydrogen atoms and R.sub.3 represents a hydrogen atom or a methoxy group, or R.sub.7 represents a hydrogen atom and R.sub.3 and R.sub.8 taken together represent a bond, or R.sub.3 represents a hydrogen atom or a methoxy group and R.sub.7 and R.sub.8 taken together represent a bond; R.sub.4 represents a hydrocarbon group having from 1 to 4 carbon atoms; R.sub.5 represents a hydrogen atom or a hydrocarbon group having from 1 to 4 carbon atoms or a phenyl group; X represents an oxygen or sulphur atom or an imino group, R.sub.9 represents a hydrogen atom and B represents a cyano, a C.sub.2 -C.sub.5 alkoxycarbonyl or carbamoyl group, or R.sub.
Type:
Grant
Filed:
April 26, 1984
Date of Patent:
September 1, 1987
Assignee:
Farmitalia Carlo Erba
Inventors:
Luigi Bernardi, Laura Chiodini, Sergio Mantegani, Daniela Ruggieri, Aldemio Temperilli, Patricia Salvati
Abstract: Anthracycline glycosides of general formula (I) ##STR1## wherein R is hydrogen or hydroxy, and pharmaceutically acceptable salts thereof, are anti-tumor agents.
Type:
Grant
Filed:
March 24, 1986
Date of Patent:
August 4, 1987
Assignee:
Farmitalia Carlo Erba S.p.A.
Inventors:
Alberto Bargiotti, Michele Caruso, Antonino Suarato, Sergio Penco, Fernando Giuliani
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:
October 16, 1985
Date of Patent:
June 23, 1987
Assignee:
Farmitalia Carlo Erba, S.p.A.
Inventors:
Gaetano Gatti, Diego Oldani, Carlo Confalonieri, Luciano Gambini
Abstract: Ergoline derivatives of formula: ##STR1## wherein n=0,1,2; R.sub.1 =H, CH.sub.3 ; R.sub.2 =H, CH.sub.3, halogen; R.sub.3 =H, OCH.sub.3 ; R.sub.4 =hydrocarbon group and R.sub.5 is a residue of general formula II, III, IV, V, VI, VII: ##STR2## wherein R.sub.6 =H, Cl, OCH.sub.3, NR.sub.11 R.sub.12, wherein R.sub.11 and R.sub.12 =H, lower alkyl; phenyl or are bonded together to form a heterocyclic ring, R.sub.7, R.sub.8 and R.sub.9 and R.sub.10 =H or C.sub.1 -C.sub.3 alkyl, with the proviso that if R.sub.5 is of formula II and R.sub.2 =R.sub.7 =R.sub.8 =H, then R.sub.4 is not methyl or n is not 0.Pharmaceutically acceptable acid addition salts are also provided. A method for their preparation is also provided.The compounds have anti-depressive, anti-hypertensive and antiprolactin activity.
Abstract: Anthracycline glycosides of the general formula (A): ##STR1## wherein X is hydrogen or hydroxy and R is hydrogen or a methyl or a hydroxymethyl group; and their pharmaceutically acceptable salts; are useful as antitumor agents.
Type:
Grant
Filed:
March 17, 1986
Date of Patent:
June 9, 1987
Assignee:
Farmitalia Carlo ERBA S.p.A.
Inventors:
Alberto Bargiotti, Pierangelo Zini, Sergio Penco, Fernando Giuliani
Abstract: 2H-Benzofuran-3-one derivatives, process for their preparation and pharmaceutical compositions containing them. The compounds and compositions are useful in the treatment of allergies.
Type:
Grant
Filed:
July 19, 1979
Date of Patent:
June 2, 1987
Assignee:
Farmitalia Carlo Erba, S.p.A.
Inventors:
Gianfederico Doria, Ciriaco Romeo, Maria L. Corno
Abstract: The present invention relates to the preparation of sterile and stable freeze-dried forms of Cisplatinum containing from 10 to 50 mg of active ingredient, which can be obtained on an industrial scale and which have particular characteristics of facility and rapidity of dissolution which permit them to be used in a more advantageous and rational manner in antitumor chemotherapy, as compared with the freeze-dried forms of Cisplatinum presently on the market.These particular characteristics are achieved as the result of employing special ingredients in respect of formulation (concentration of the solution to be freeze-dried, introduction of alcohols, adjustment of the pH of the solution to an appropriate value), and as the result of using a manufacturing technique having as its final stage the freeze-drying of Cisplatinum in a water-alcoholic medium.
Type:
Grant
Filed:
May 28, 1985
Date of Patent:
June 2, 1987
Assignee:
Farmitalia Carlo Erba S.p.A.
Inventors:
Gaetano Battelli, Diego Oldani, Alessandro Rigamonti