Patents by Inventor Vesperto Torelli
Vesperto Torelli has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).
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Patent number: 5043332Abstract: Novel 19-nor-steroids of the formula ##STR1## wherein R.sub.1 is an organic group of 1 to 18 carbon atoms optionally containing at least one heteroatom with the atom immediately adjacent the 11-carbon atom being carbon, R.sub.2 is a hydrocarbon of 1 to 8 carbon atoms, X is the remainder of a pentagonal or hexagonal ring optionally substituted and optionally containing one unsaturated--bond, the A and B rings are selected from the group consisting of ##STR2## R' and R" are individually selected from the group consisting of hydrogen, --CN and alkyl of 1 to 4 carbon atoms, R.sub.x is selected from the group consisting of hydrogen and OR.sub.e, R.sub.e is selected from the group consisting of hydrogen, optionally substituted alkyl of 1 to 6 carbon atoms and acyl, R.sub.a may be in the E or Z positions as indicated by the wavy line and is selected from the group consisting of ##STR3## and acyloxy, R'.sub.a and R".sub.Type: GrantFiled: October 13, 1989Date of Patent: August 27, 1991Assignee: Roussel UclafInventors: Jean-Georges Teutsch, Vesperto Torelli, Roger Deraedt, Daniel Philibert, Germain Costerousse
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Patent number: 4978657Abstract: Novel 19-nor-steroids of the formula ##STR1## wherein R.sub.1 is an organic group of 1 to 18 carbon atoms optionally containing at leat one heteroatom with the atom immediately adjacent the 11-carbon atom being carbon, R.sub.2 is a hydrocarbon of 1 to 8 carbon atoms, X is the remainder of a pentagonal or hexagonal ring optionally substituted and optionally containing one unsaturated bond, the A and B rings are selected from the group consisting of ##STR2## R' and R" are individually selected from the group consisting of hydrogen, --CN and alkyl of 1 to 4 carbon atoms, R.sub.x is selected from the group consisting of hydrogen and OR.sub.e, R.sub.e is selected from the group consisting of hydrogen, optionally substituted alkyl of 1 to 6 carbon atoms and acyl, R.sub.a may be in the E or Z positions as indicated by the wavy line and is selected from the group consisting of ##STR3## and acyloxy, R.sub.a ' and R.sub.Type: GrantFiled: December 17, 1985Date of Patent: December 18, 1990Assignee: Roussel UclafInventors: Jean-Georges Teutsch, Vesperto Torelli, Roger Deraedt, Daniel Philibert, Germain Costerousse
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Patent number: 4753932Abstract: A novel steroid of the formula ##STR1## wherein X is methylene and R is an optionally substituted carbocyclic aryl or heterocyclic aryl or optionally substituted vinyl or ethynyl or X is a simple bond or --S-- and R is optionally substituted carbocyclic aryl or heterocyclic aryl, R.sub.2 is methyl or ethyl, R.sub.3 is selected from the group consisting of optionally substituted alkyl of 1 to 8 carbon atoms and optionally substituted alkenyl and alkynyl of 2 to 8 carbon atoms, R.sub.4 is selected from the group consisting of hydrogen and acyl, ##STR2## is selected from the group consisting of ##STR3## R.sub.6 is selected from the group consisting of hydrogen and methyl, the wavy line indicates .alpha. or .beta.- and the dotted line in 1(2) indicates the optional presence of a second carbon-carbon bond and novel process and intermediates therefore having anti-glucocorticoid activity.Type: GrantFiled: January 14, 1986Date of Patent: June 28, 1988Assignee: Roussel UclafInventors: Jean-Georges Teutsch, Germain Costerousse, Vesperto Torelli, Daniel Philibert
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Patent number: 4701449Abstract: Novel 10-substituted steroids of the formula ##STR1## wherein R is selected from the group consisting of hydrogen, alkyl and substituted alkyl of 1 to 8 carbon atoms, alkenyl, substituted alkenyl, alkynyl and substituted alkynyl of 2 to 8 carbon atoms, aryl and substituted aryl, aralkyl and substituted aralkyl, protected hydroxy, optionally esterified carboxy, --NH.sub.2, protected amino, mono and di-alkyl amino of 1 to 4 alkyl carbon atoms, halogen and trialkylsilyl, R.sub.2 is methyl or ethyl, R.sub.6 and R.sub.7 together with the carbon atoms to which they are attached form cyclopropyl or R.sub.6 is hydrogen and R.sub.7 is R.sub.1, R.sub.1 is selected from the group consisting of hydrogen, alkyl and substituted alkyl of 1 to 6 carbon atoms, acetylthio and alkenyl, substituted alkenyl, alkynyl and substituted alkynyl of 2 to 6 carbon atoms, X is optionally acylated or etherified hydroxyl and Y is selected from the group consisting of hydrogen, R.sub.4, --CH.sub.2 --CH.sub.2 COOM and --CH.sub.2 --CH.sub.Type: GrantFiled: August 23, 1985Date of Patent: October 20, 1987Assignee: Roussel UclafInventors: Vesperto Torelli, Lucien Nedelec, Martine Moguilewski, Anne-Marie Moura
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Patent number: 4634695Abstract: Novel 19-nor steroids and 19-nor-D-homo-steroids of the formula ##STR1## wherein R.sub.1 is an organic radical of 1 to 18 carbon atoms containing at least one atom selected from the group consisting of nitrogen, phosphorous and silicon with the atom immediately adjacent to the 11-carbon atom being carbon, R.sub.2 is a hydrocarbon of 1 to 8 carbon atoms, X is selected from the group consisting of a pentagonal ring and a hexagonal ring optionally substituted and optionally containing a double bond, B and C together form a double bond or an epoxy group, the C.dbd.A group at position 3 is selected from the group consisting of C.dbd.O, ketal, which may be open or closed ##STR2## are selected from the group consisting of alkyl of 1 to 8 carbon atoms and aralkyl of 7 to 15 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts having anti-glucocorticoid activity and a process for their preparation.Type: GrantFiled: January 22, 1985Date of Patent: January 6, 1987Assignee: Roussel UclafInventors: Vesperto Torelli, Jean G. Teutsch, Daniel Philibert
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Patent number: 4634696Abstract: Novel 19-nor-steroids of the formula ##STR1## wherein R.sub.1 is an organic group of 1 to 18 carbon atoms optionally containing at least one heteroatom with the atom immediately adjacent the 11-carbon atom being carbon, R.sub.2 is a hydrocarbon of 1 to 8 carbon atoms, X is the remainder of a pentagonal or hexagonal ring optionally substituted and optionally containing one unsaturated--bond, the A and B rings are selected from the group consisting of ##STR2## R' and R" are individually selected from the group consisting of hydrogen, --CN and alkyl of 1 to 4 carbon atoms with at least one being other than hydrogen, R.sub.x is selected from the group consisting of hydrogen and OR.sub.e, R.sub.e is selected from the group consisting of hydrogen, optionally substituted alkyl of 1 to 6 carbon atoms and acyl, R.sub.a may be in the E or Z positions as indicated by the wavy line and is selected from the group consisting of ##STR3## and acyloxy, R.sub.a ' and R.sub.Type: GrantFiled: July 30, 1985Date of Patent: January 6, 1987Assignee: Roussel UclafInventors: Jean-Georges Teutsch, Vesperto Torelli, Roger Deraedt, Daniel Philibert
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Patent number: 4565656Abstract: A novel process for the preparation of 17.beta.-hydroxyacetyl-17.alpha.-ol-steroids of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of hydrogen, alkyl of 1 to 4 carbon atoms optionally substituted with halogen or an oxygen or nitrogen function and alkenyl and alkynyl of 2 to 4 carbon atoms, R.sub.2 is alkyl of 1 to 4 carbon atoms and the A,B,C and D rings may contain one or more double bonds and are optionally substituted with at least one member of the group consisting of hydroxy, keto, halogen, alkyl and alkoxy of 1 to 4 carbon atoms and alkenyl and alkynyl of 2 to 4 carbon atoms which compounds are generally known of the cortisonic type with known properties.Type: GrantFiled: January 27, 1982Date of Patent: January 21, 1986Assignee: Roussel UclafInventors: Lucien Nedelec, Vesperto Torelli, Michel Hardy
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Patent number: 4547493Abstract: Novel 19-nor-steroids of the formula ##STR1## wherein R.sub.1 is an organic group of 1 to 18 carbon atoms optionally containing at least one heteroatom with the atom immediately adjacent the 11-carbon atom being carbon, R.sub.2 is a hydrocarbon of 1 to 8 carbon atoms, X is the remainder of a pentagonal or hexagonal ring optionally substituted and optionally containing one unsaturated bond, the A and B rings are selected from the group consisting of ##STR2## R' and R" are individually selected from the group consisting of hydrogen, --CN and alkyl of 1 to 4 carbon atoms with at least one being other than hydrogen, R.sub.x is selected from the group consisting of hydrogen and OR.sub.e R.sub.e is selected from the group consisting of hydrogen, optionally substituted alkyl of 1 to 6 carbon atoms and acyl, R.sub.a may be in the E or Z positions as indicated by the wavy line and is selected from the group consisting of ##STR3## and acyloxy, R.sub.a ' and R.sub.Type: GrantFiled: June 6, 1983Date of Patent: October 15, 1985Assignee: Roussel UclafInventors: Jean-Georges Teutsch, Vesperto Torelli, Roger Deraedt, Daniel Philibert
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Patent number: 4464302Abstract: Novel 17-[(hydroxymethyl)formamido methylene]-steroids of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of hydrogen, alkyl of 1 to 4 carbon atoms optionally substituted with halogen or an oxygen or nitrogen function and alkenyl and alkynyl of 2 to 4 carbon atoms, R.sub.2 is alkyl of 1 to 4 carbon atoms and the A,B,C and D rings may contain one or more double bonds and are optionally substituted with at least one member of the group consisting of hydroxy, keto, halogen, alkyl and alkoxy of 1 to 4 carbon atoms and alkenyl and alkynyl of 2 to 4 carbon atoms and a process for their preparation which are intermediates for the preparation of the corresponding 17-hydroxyacetyl steroids.Type: GrantFiled: July 28, 1980Date of Patent: August 7, 1984Assignee: Roussel UclafInventors: Lucien Nedelec, Vesperto Torelli
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Patent number: 4444767Abstract: A compound selected from the group consisting of: 3-amino-.DELTA..sup.5 -pregnenes of the formula I: ##STR1## wherein X is selected from the group of ##STR2## the wavy lines indicate that the group may be in the .alpha.-or .beta.-position, R.sub.1 is selected from the group consisting of hydrogen and hydroxyalkyl or 2 to 5 carbon atoms, R.sub.2 is selected from the group consisting of hydrogen, hydroxyalkyl of 2 to 5 carbon atoms, acyl of an aliphatic carboxylic acid of 3 to 8 carbon atoms, alkoxycarbonyl of 2 to 8 carbon atoms, acyl of an .alpha.-amino-carboxylic acid or from a peptide of 2 to 3 amino acids of which amines may be either unsubstituted or mono-or disubstituted with alkyl of 1 to 5 carbon atoms with the proviso that R.sub.1 and R.sub.2 are not both hydrogen and that if the 3-amino group is in the .beta.-position, (i) when X is ##STR3## R.sub.1 and R.sub.2 are not both hydroxyethyl or (ii) when X is ##STR4## and R.sub.1 is hydrogen, R.sub.Type: GrantFiled: October 25, 1982Date of Patent: April 24, 1984Assignee: Roussel UclafInventors: Vesperto Torelli, Josette Benzoni, Roger Deraedt
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Patent number: 4424218Abstract: A 3-amino-steroid of the formula ##STR1## wherein W is selected from the group consisting of hydrogen and --OH and taken together with X is ethylidene, X is selected from the group consisting of ethyl, ##STR2## the wavy line indicates the substituent has the .alpha.- and .beta.-position, R.sub.1 is selected from the group consisting of hydrogen and --CH.sub.3, R.sub.2 is selected from the group consisting of hydrogen, alkyl of 1 to 5 carbon atoms and hydroxyalkyl of 2 to 5 carbon atoms, R.sub.3 is selected from the group consisting of hydrogen, alkyl of 1 to 5 carbon atoms, hydroxyalkyl of 2 to 5 carbon atoms, acyl of organic acid of 2 to 8 carbon atoms, alkoxycarbonyl of 2 to 8 carbon atoms, acyl of an .alpha.-amino-carboxylic acid and a peptide of 2 to 3 .alpha.-amino-carboxylic acids and their non-toxic, pharmaceutically acceptable acid addition acids with the proviso that R.sub.2 and R.sub.3 are not both hydrogen and (i) when R.sub.1 is methyl, W and R.sub.2 are hydrogen and X is ##STR3## in the case R.Type: GrantFiled: August 14, 1981Date of Patent: January 3, 1984Assignee: Roussel UclafInventors: Roger Deraedt, Vesperto Torelli, Jean Vacher, Josette Benzoni
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Patent number: 4396614Abstract: Novel steroids of the formula ##STR1## wherein R is selected from the group consisting of R.sub.1 and R.sub.2, R.sub.1 is selected from the group consisting of alkyl of 1 to 8 carbon atoms and alkenyl and alkynyl of 2 to 8 carbon atoms R.sub.2 is --(CH.sub.2).sub.n --R.sub.3, n is an integer from 1 to 8 and R.sub.3 is selected from the group consisting of free or protected --OH, free or protected --NH.sub.2, monoalkyl and dialkylamino with 1 to 6 carbon atoms, a free, esterified or salified --COOH and halogen X and Y together form ##STR2## or X is OH and Y is --CH.sub.2 --CH.sub.2 --COOM, M is selected from the group consisting of hydrogen, an alkali metal and --NH.sub.4, Ra is selected from the group consisting of hydrogen and methyl, the dotted line in the I(2)-position indicates the optional presence of a double bond and the wavy line indicates that R may be in the .alpha.- or .beta.-position, with the proviso that R is not R.sub.1 or R.sub.2 when n is 1 and R.sub.Type: GrantFiled: December 21, 1981Date of Patent: August 2, 1983Assignee: Roussel UclafInventors: Lucien Nedelec, Vesperto Torelli, Daniel Philibert
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Patent number: 4395408Abstract: Novel 3-amino-steroids of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of hydrogen and methyl, W is selected from the group consisting of hydrogen and --OH and taken together with x forms ethylidene, X is selected from the group consisting of ethyl, ##STR2## and taken together with W forms ethylidene and the wavy lines signify that the substituents are in the .alpha. or .beta.-position with the proviso that when R.sub.1 is methyl and X is ethyl, ##STR3## W is --OH and their non-toxic, pharmaceutically acceptable acid addition salts and their preparation and intermediates therefore capable of stimulating immunitary activity.Type: GrantFiled: August 14, 1981Date of Patent: July 26, 1983Assignee: Roussel UclafInventors: Vesperto Torelli, Roger Deraedt, Lucien Nedelec
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Patent number: 4376734Abstract: A novel process for the preparation of 3-amino-steroids of the formula ##STR1## wherein X is selected from the group consisting of ##STR2## and the wavy lines indicate that the substituents may be in the .alpha.- or .beta.-position and their non-toxic, pharmaceutically acceptable acid addition salts in good yields and novel intermediates.Type: GrantFiled: November 10, 1981Date of Patent: March 15, 1983Assignee: Roussel UclafInventors: Vesperto Torelli, Lucien Nedelec
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Patent number: 4263290Abstract: Novel 19-nor-steroids of the formula ##STR1## wherein R.sub.1 and R.sub.2 taken together form a cycloalkyl of 3 to 8 carbon atoms or are individually selected from the group consisting of hydrogen, alkyl of 1 to 4 carbon atoms and alkenyl and alkynyl of 2 to 6 carbon atoms with the proviso that both cannot be hydrogen, R.sub.3 is alkyl of 2 to 4 carbon atoms, R.sub.4 ' is selected from the group consisting of hydrogen, hydroxyl, acyloxy of an organic carboxylic acid of 1 to 18 carbon atoms and ##STR2## and M is selected from the group consisting of hydrogen and alkali metal, having antagonistic properties to aldosterone and increasing sodium-water diuresis with conservation of organic potassium and a novel process and novel intermediates for their preparation.Type: GrantFiled: November 30, 1979Date of Patent: April 21, 1981Assignee: Roussel UclafInventors: Lucien Nedelec, Vesperto Torelli, Robert Fournex
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Patent number: 4258039Abstract: Novel 7-alkyl-.DELTA..sup.4 -17.alpha.-pregnene-3-ones of the formula ##STR1## wherein R is selected from the group consisting of saturated and unsaturated alkyl of 2 to 8 carbon atoms, cycloalkyl alkyl of 4 to 8 carbon atoms and arylalkyl of 7 to 12 carbon atoms and X and Y form the group ##STR2## or X is OH and Y is ##STR3## and M is selected from the group consisting of hydrogen, alkali metal and NH.sub.4 and the wavy line indicates the .alpha.- or .beta.-position or mixtures thereof having aldosterone antagonistic activity and increased hydrosodium diuresis with organic potassium conservation while devoid of secondary hormonal effects and their preparation.Type: GrantFiled: February 29, 1980Date of Patent: March 24, 1981Assignee: Roussel UclafInventors: Lucien Nedelec, Vesperto Torelli, Robert Fournex, Colette Tournemine
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Patent number: 4203981Abstract: Novel steroids of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of hydrogen and acyl of an organic carboxylic acid of 1 to 18 carbon atoms, R.sub.2 is selected from the group consisting of optionally substituted aryl of 6 to 12 carbon atoms and optionally substituted heterocyclic selected from the group consisting of furyl, thienyl, pyridyl and pyrimidyl, the optional substituents being selected from the group consisting of hydroxy, alkyl and alkoxy of 1 to 4 carbon atoms, halogens and --CF.sub.3, the dotted line in the A ring indicates an optional .DELTA..sup.1(2) - double bond and A may be oxo and B is hydrogen or A is .DELTA.--OH and B is hydrogen or halogen or A and B form a .DELTA..sup.9(10) - double bond having very good anti-inflammatory activity and their preparation and novel intermediates.Type: GrantFiled: January 3, 1979Date of Patent: May 20, 1980Assignee: Roussel UclafInventors: Andre Pierdet, Vesperto Torelli, Roger Deraedt
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Patent number: 4154730Abstract: Novel 17-spirosultines of steroids and the corresponding .gamma.-hydroxy acids of the formula ##STR1## wherein R.sub.1 is alkyl of 1 to 4 carbon atoms, A is hydrogen and B is hydrogen or hydroxyl of .beta.configuration or A and B together form a double bond, X and Y together form the group ##STR2## or X is --OH and Y is ##STR3## and M is selected from the group consisting of hydrogen, --NH.sub.4 and an alkali metal having a remarkable progestomimetic and antialdosteronic activity and a novel process for their preparation and novel intermediates.Type: GrantFiled: October 20, 1977Date of Patent: May 15, 1979Assignee: Roussel UclafInventors: Vesperto Torelli, Daniel Philibert
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Patent number: 4136179Abstract: 2,2-DIMETHYL-19-NOR-STEROIDS OF THE FORMULA ##STR1## wherein R.sub.1 is selected from the group consisting of hydrogen, ##STR2## and R.sub.2 is selected from the group consisting of hydrogen and hydrocarbon of 1 to 17 carbon atoms and the dotted lines indicate the optional presence of a double bond in 9(10) and 11(12) positions having antialdosteronic activity and an increased sodium diuresis with conservation of organic potassium and their preparation and novel intermediates.Type: GrantFiled: September 7, 1977Date of Patent: January 23, 1979Assignee: Roussel UclafInventors: Lucien Nedelec, Vesperto Torelli, Robert Fournex
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Patent number: 4093720Abstract: Novel 17-spirosultines and their corresponding .gamma.-hydroxy acids of the formula ##STR1## wherein A is hydrogen and B is alkyl of 1 to 4 carbon atoms in the .alpha.- or .beta.-position or A and B form a methylene group in the 6.alpha., 7.alpha.- or 6.beta., 7.beta.-position and X and Y form a group of the formula ##STR2## or X is OH and Y is ##STR3## and M is selected from the group consisting of hydrogen, --NH.sub.4 and an alkali metal cation having antialdosterone activity and their preparation and novel intermediates therefore.Type: GrantFiled: March 14, 1977Date of Patent: June 6, 1978Assignee: Roussel UclafInventors: Genevieve Rousseau, Vesperto Torelli