Patents Assigned to Sigma-Tau Industrie Farmaceutiche
  • Patent number: 5599806
    Abstract: The invention describes hydrazino and hydroxyamino-14.beta.-hydroxyandrostane derivatives having general formula (I): ##STR1## wherein the symbol means .alpha. or .beta. configuration and A, B, R.sup.1, R.sup.2, R.sup.3, and R.sup.4 have the meanings given in the description and their use in the treatment of cardiovascular disorders such as heart failure and hypertension.
    Type: Grant
    Filed: May 18, 1995
    Date of Patent: February 4, 1997
    Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.
    Inventors: Alberto Cerri, Giuseppe Bianchi, Patrizia Ferrari, Elena Folpini, Piero Melloni
  • Patent number: 5596110
    Abstract: An improvement in a process for producing 3.beta.,14.beta.-dihydroxyethianaldehyde is disclosed wherein the oxidation of the lactone ring of digitoxigenin-3-acetate is conducted with an alkaline periodate in the presence of a catalytic amount of ruthenium tetroxide obtained in situ by reacting RuO.sub.2 hydrate or RuCl.sub.3 with the alkaline periodate.
    Type: Grant
    Filed: March 16, 1995
    Date of Patent: January 21, 1997
    Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.
    Inventors: Mauro Gobbini, Marco Torri
  • Patent number: 5593982
    Abstract: Cyclopentanperhydrophenantren-17.beta.-(3-furyl)-3-derivatives and pharmaceutical compositions containing same for the treatment of cardiovascular disorders such as heart failure and hypertension, are disclosed.
    Type: Grant
    Filed: May 9, 1995
    Date of Patent: January 14, 1997
    Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.
    Inventors: Luisa Quadri, Luigi Bernardi, Patrizia Ferrari, Mauro Gobbini, Piero Melloni, Loredana Valentino
  • Patent number: 5591777
    Abstract: The use of 6,7-substituted-2-aminotetralines (e.g. 2-amino-6-fluoro-7-methoxytetraline) is disclosed for preparing pharmaceutical compositions useful for the treatment of septic shock and having antiinflammatory and antipyretic activities.
    Type: Grant
    Filed: February 27, 1996
    Date of Patent: January 7, 1997
    Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.
    Inventors: Piero Foresta, Vito Ruggiero
  • Patent number: 5591734
    Abstract: The present invention relates to a group of 17-(3-furyl)- and (4-pyridazinyl) 5.beta.,14.beta.-androstane derivatives, active on the cardiovascular system, to processes for their preparation and to pharmaceutical compositions containing same for the treatment of cardiovascular disorders such as heart failure and hypertension.
    Type: Grant
    Filed: August 16, 1993
    Date of Patent: January 7, 1997
    Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.
    Inventors: Luisa Quadri, Luigi Bernardi, Giuseppe Bianchi, Patrizia Ferrari, Piero Melloni, Loredana Valentino
  • Patent number: 5583127
    Abstract: Disclosed are 17-iminomethylalkenyl and 17-iminoalkyl-14.beta.-hydroxy-5.beta.-androstane derivatives of the formula (I): ##STR1## wherein the symbol means .alpha. or .beta. configuration or a Z or E configuration; A represents (CH.sub.2).sub.m or --(CH.dbd.CH).sub.n --; m represents an integer number from 1 to 6; n represents an integer number from 1 to 3; R.sup.2 represents hydrogen or hydroxy; R.sup.1 represents hydrogen, C.sub.2 -C.sub.4 alkyl unsubstituted or substituted by NR.sup.4 R.sup.5 wherein R.sup.4 and R.sup.5, which may be the same or different, represent hydrogen, C.sub.1 -C.sub.4 alkyl or R.sup.4 and R.sup.5 may form, when taken together with the nitrogen atom, a five- or six- membered heterocyclic ring optionally containing one or more heteroatoms selected from oxygen and nitrogen; R.sup.3 represents NHC(.dbd.X)NR.sup.6 R.sup.7 or OR.sup.8 wherein R.sup.6 and R.sup.7, which may be the same or different, represent hydrogen, methyl, or C.sub.2 -C.sub.4 alkyl unsubstituted or substituted by NR.
    Type: Grant
    Filed: December 23, 1994
    Date of Patent: December 10, 1996
    Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.
    Inventors: Alberto Cerri, Giuseppe Bianchi, Patrizia Ferrari, Elena Folpini, Piero Melloni
  • Patent number: 5567697
    Abstract: Present invention relates to a group of 17-(4-pyridazinyl)-5.beta.,14.beta.-androstane derivates active on the cardiovascular system and to pharmaceutical compositions containing same.
    Type: Grant
    Filed: June 2, 1995
    Date of Patent: October 22, 1996
    Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.
    Inventors: Luisa Quadri, Luigi Bernardi, Giuseppe Bianchi, Patrizia Ferrari, Piero Melloni, Loredana Valentino
  • Patent number: 5567694
    Abstract: 17-aryl and heterocyclyl-5.beta.,14.beta.-androstane compounds having the formula (I) ##STR1## wherein R is an aryl ring or a saturated or unsaturated heterocyclic ring are active on the cardiovascular system and are useful in treating cardiovascular disorders.
    Type: Grant
    Filed: September 29, 1993
    Date of Patent: October 22, 1996
    Assignee: SIGMA-TAU Industrie Farmaceutiche Riunite S.p.A.
    Inventors: Nicoletta Almirante, Luigi Bernardi, Alberto Cerri, Piero Melloni, Gloria Padoani, Luisa Quadri
  • Patent number: 5556846
    Abstract: 17-Heterocyclyl-5.alpha.-14.beta.-androstane, androstene and androstadiene of formula (I): ##STR1## wherein: Y is oxygen or guanidinoimino, when a double bond exists at position 3;Y is hydroxy, OR.sup.2 or SR.sup.2, when a single bond exists at position 3;R is a saturated or unsaturated mono- or biheterocyclic ring, containing one or more heteroatoms selected from the group consisting of oxygen, sulfur, and nitrogen, unsubstituted or substituted by one or more of halogen, hydroxymethyl, alkoxy, amino, alkylamino, dialkylamino, cyano, nitro, sulfonamido, C.sub.1 -C.sub.6 lower alkyl or COR.sup.3 ; andR.sup.1 is hydrogen, methyl, ethyl or n-propyl substituted by OH or NR.sup.4 R.sup.5.
    Type: Grant
    Filed: September 29, 1993
    Date of Patent: September 17, 1996
    Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.
    Inventors: Piero Melloni, Luigi Bernardi, Mara Ferrandi, Marco Frigerio, Marina Mauro, Luisa Quadri
  • Patent number: 5547986
    Abstract: The L-carnitine ester with gamma-hydroxybutyric acid and its pharmacologically acceptable salts of formula (I) ##STR1## wherein X.sup.- is the anion of a pharmacologically acceptable salt, e.g. chloride, bromide, orotate, acid aspartate, acid citrate, acid phosphate, acid fumarate, lactate, acid maleate, acid oxalate, acid sulfate and glucosephosphate are active in inhibiting neuronal degeneration (as it occurs in Alzheimer's senile dementia and Parkinson's disease) and in the treatment of coma.
    Type: Grant
    Filed: March 29, 1995
    Date of Patent: August 20, 1996
    Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.
    Inventors: Maria O. Tinti, Domenico Misiti, Claudio Cavazza
  • Patent number: 5543556
    Abstract: The esters of acyl L-carnitines with gamma-hydroxybutyric acid in the form of pharmacologically acceptable salts of formula (I) ##STR1## wherein X.sup.- is the anion of a pharmacologically acceptable salt, e.g. chloride, bromide, orotate, acid aspartate, acid citrate, acid phosphate, acid fumarate, lactate, acid maleate, acid oxalate, acid sulfate and glucosephosphate or in the form of inner salts of formula (I') ##STR2## wherein R is a straight or branched acyl group having from 2 to 5 carbon atoms, such as e.g. acetyl, propionyl, n-butyryl, isobutyryl and isovaleryl, are active in inhibiting neuronal degeneration (as it occurs in Alzheimer's senile dementia and Parkinson's disease) and in the treatment of coma.
    Type: Grant
    Filed: October 4, 1994
    Date of Patent: August 6, 1996
    Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.
    Inventors: Maria O. Tinti, Domenico Misiti, Claudio Cavazza, Nazareno Scafetta
  • Patent number: 5538960
    Abstract: The present invention relates to new 17-hydrazonomethyl- and 17-hydrazono-14.beta.-hydroxy-5.beta.-androstane derivatives active on the cardiovascular system, to a process for their preparation and to pharmaceutical compositions containing same for the treatment of cardiovascular disorders, such as heart failure and hypertension.
    Type: Grant
    Filed: August 16, 1993
    Date of Patent: July 23, 1996
    Assignee: SIGMA-TAU Industrie Farmaceutiche Riunite S.p.A.
    Inventors: Alberto Cerri, Luigi Bernardi, Giuseppe Bianchi, Patrizia Ferrari, Elena Folpini, Piero Melloni
  • Patent number: 5534549
    Abstract: The esters of acyl L-carnitines with gamma-hydroxybutyric acid in the form of pharmacologically acceptable salts of formula (I) ##STR1## wherein X.sup.- is the anion of a pharmacologically acceptable salt, e.g. chloride, bromide, orotate, acid aspartate, acid citrate, acid phosphate, acid fumarate, lactate, acid maleate, acid oxalate, acid sulfate and glucosephosphate or in the form of inner salts of formula (I') ##STR2## wherein R is a straight or branched acyl group having from 2 to 5 carbon atoms, such as e.g. acetyl, propionyl, n,butyryl, isobutyryl and isovaleryl, are active in inhibiting neuronal degeneration (as it occurs in Alzheimer's senile dementia and Parkinson's disease) and in the treatment of coma.
    Type: Grant
    Filed: February 28, 1995
    Date of Patent: July 9, 1996
    Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.
    Inventors: Maria O. Tinti, Domenico Misiti, Claudio Cavazza, Nazareno Scafetta
  • Patent number: 5532410
    Abstract: L-(-)-carnitine is prepared from D-(+)-carnitinamide by (a) reacting D-(+)-carnitinamide in an acid medium with a straight or branched chain aliphatic alcohol thereby forming D-(+)-carnitine ester, (b) acylating the D-(+)-carnitine ester with an anhydride R.sub.2 O, thereby forming an acylated ester intermediate, (c) acid hydrolyzing the ester group of the acyl carnitine ester thereby obtaining acyl D-(+)-carnitine, (d) lactonizing the acyl D-(+)-carnitine to a lactone of L-(-)-carnitine, and (e) reacting the lactone with base thereby forming L-(-)-carnitine.
    Type: Grant
    Filed: April 4, 1994
    Date of Patent: July 2, 1996
    Assignee: Sigma-Tau Industrie Farmaceutiche Ruinite S.p.A.
    Inventors: Fabio Giannessi, Nazareno Scafetta, Ida Bernabei, Maria O. Tinti, Francesco De Angelis
  • Patent number: 5532409
    Abstract: A process for producing aminocarnitine is described, wherein methanesulfonylcarnitine is converted to a lactone which is reacted with an azide to give azidocarnitine. The catalytic hydrogenation of azidocarnitine gives aminocarnitine.
    Type: Grant
    Filed: September 30, 1994
    Date of Patent: July 2, 1996
    Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.
    Inventors: Fabio Giannessi, Roberto Castagnani, Francesco De Angelis, Maria O. Tinti, Domenico Misiti
  • Patent number: 5525627
    Abstract: Esters of acyl L-carnitines of general formula (I) ##STR1## wherein R is a straight or branched acyl group having 2 to 16 carbon atoms, in particular isobutyryl and isovaleryl;n is an integer comprised between 7 and 15, particularly 10; and,X- is the anion of a pharmacologically acceptable acid are endowed with potent antimycotic activity particularly against yeast like fungi, such as Candida albicans, the aetiologic agent of candidiasis and against filamentous fungi, such as Aspergillus fumigatus, the aetiologic agent of aspergillosis. Orally or parenterally administrable or topically applicable pharmaceutical compositions comprise an ester of formula (I) as active ingredient.
    Type: Grant
    Filed: March 24, 1995
    Date of Patent: June 11, 1996
    Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.
    Inventors: Mose Santaniello, Maria O. Tinti, Domenico Misiti, Piero Foresta
  • Patent number: 5519056
    Abstract: Esters of acyl L-carnitines of general formula (I) ##STR1## wherein R is a straight or branched acyl group having 2 to 16 carbon atoms, in particular isobutyryl and isovaleryl;n is an integer comprised between 7 and 15, particularly 10; and,X.sup.- is the anion of a pharmacologically acceptable acid are endowed with potent antimycotic activity particularly against yeast like fungi, such as Candida albicans, the aetiologic agent of candidiasis and against filamentous fungi, such as Aspergillus fumigatus, the aetiologic agent of aspergillosis.Orally or parenterally administrable or topically applicable pharmaceutical compositions comprise an ester of formula (I) as active ingredient.
    Type: Grant
    Filed: May 26, 1994
    Date of Patent: May 21, 1996
    Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.
    Inventors: Mose Santaniello, Maria O. Tinti, Domenico Misiti, Piero Foresta
  • Patent number: 5510538
    Abstract: A process for the selective oxidation of a primary or secondary alcohol to an aldehyde or ketone and for the oxidation of a 1,2-diol to an .alpha.-ketol or .alpha.-diketone, which comprises contacting the alcohol or 1,2-diol with o-iodoxybenzoic acid. This process is suited for selective oxidation of alcohols containing easily oxidizable groups, such as amino or thioether groups and easily oxidizable heterocycles.
    Type: Grant
    Filed: December 16, 1994
    Date of Patent: April 23, 1996
    Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.
    Inventors: Marco Frigerio, Simona Sputore, Marco Santagostino
  • Patent number: 5498633
    Abstract: Esters of acyl L-carnitines of general formula (I) ##STR1## wherein R is a straight or branched acyl group having 2 to 16 carbon atoms, in particular isobutyryl and isovaleryl;n is an integer comprised between 7 and 15, particularly 10; and,X- is the anion of a pharmacologically acceptable acid are endowed with potent antibacterial activity. Pharmaceutical compositions comprising an ester of formula (I) can be utilized in human therapy and in the veterinary field.
    Type: Grant
    Filed: March 22, 1995
    Date of Patent: March 12, 1996
    Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.
    Inventors: Mose Santaniello, Maria O. Tinti, Domenico Misiti, Piero Foresta
  • Patent number: 5498632
    Abstract: Esters of acyl L-carnitines of general formula (I) ##STR1## wherein R is a straight or branched acyl group having 2 to 16 carbon atoms, in particular isobutyryl and isovaleryl;n is an integer comprised between 7 and 15, particularly 10; and,X- is the anion of a pharmacologically acceptable acid are endowed with potent antibacterial activity.Pharmaceutical compositions comprising an ester of formula (I) can be utilized in human therapy and in the veterinary field.
    Type: Grant
    Filed: May 26, 1994
    Date of Patent: March 12, 1996
    Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.
    Inventors: Mose Santaniello, Marie O. Tinti, Domenico Misiti, Piero Foresta