Patents Assigned to Roussel-UCLAF
  • Patent number: 5554604
    Abstract: A method of controlling male fertility in warm-blooded male animals comprising administering to male warm-blooded animals an amount of a compound selected from the group consisting of a compound of the formula ##STR1## wherein R.sub.1 and R.sub.2 are individually selected from the group consisting of alkyl of 1 to 8 carbon atoms and benzyl or taken together with the nitrogen form a saturated 5 to 6 ring heterocycle optionally containing a second nitrogen or oxygen in the ring, R.sub.3 is .alpha.- or .beta.- methyl, n is an integer from 2 to 10, R.sub.4 and R.sub.5 together are .dbd.0 or R.sub.4 is selected from the group consisting of hydrogen, --OH and acyloxy of an organic carboxylic acid of up to 12 carbon atoms and R.sub.5 is selected from the group consisting of hydrogen, --OH, acyloxy of an organic carboxylic acid of up to 12 carbon atoms and alkyl, alkenyl and alkynyl of up to 8 carbon atoms, R.sub.6 and R.sub.7 together are .dbd.
    Type: Grant
    Filed: March 8, 1995
    Date of Patent: September 10, 1996
    Assignee: Roussel Uclaf
    Inventors: Armelle Bonfils, Daniel Philibert
  • Patent number: 5547869
    Abstract: Recombinant plasmids capable of replicating themselves in Escherichia coli containing a complete or partial sequence of the double or single strand DNA or a Densovirus causing a densovirosis in a sensitive insect, a process for obtaining said plasmids and a method of combatting ravager insects.
    Type: Grant
    Filed: February 14, 1994
    Date of Patent: August 20, 1996
    Assignee: Roussel Uclaf
    Inventors: Bruno Dumas, Monica Gervais, Max Bergoin, Mireille Jourdan, Francoise X. Jousset
  • Patent number: 5543400
    Abstract: A compound selected from the group consisting of a compound of the formula ##STR1## wherein R is ##STR2## m and n are individually integers from 0 to 6, A and B are individually a member selected from the group consisting of hydrogen, halogen and alkyl of 1 to 8 carbon atoms, the double bond geometry being E or Z or E+Z or A and B form a third bond between the carbon atoms to which they are attached, Ar is selected from the group consisting of a) carbocyclic aryl of up to 18 carbon atoms optionally substituted with at least one member of the group consisting of free carboxy, alkoxycarbonyl, carboxy salified with a non-toxic, pharmaceutically acceptable base, amidified carboxy, --OH, halogen, --NO.sub.2, --CN, alkyl, alkenyl, alkynyl, alkoxy, alkenyloxy, alkynyloxy, alkylthio, alkenylthio and alkynylthio of up to 12 carbon atoms, N-alkyl, N-alkenyl and N-alkynyl of up to 12 carbon atoms and cycloalkyl of 3 to 12 carbon atoms, all optionally substituted with at least one halogen and ##STR3## R.sub.1 and R.sub.
    Type: Grant
    Filed: November 1, 1993
    Date of Patent: August 6, 1996
    Assignee: Roussel Uclaf
    Inventors: Constantin Agouridas, Alain Bonnefoy, Jean-Fran.cedilla.ois Chantot, Alexis Denis, Odile Le Martret
  • Patent number: 5541318
    Abstract: A compound selected from the group consisting of a syn isomer of a compound of the formula: ##STR1## in the R or S form or in the form of an R, S mixture wherein the variables are herein below defined, and their non-toxic, pharmaceutically acceptable acid addition salts having anti-bacterial activity.
    Type: Grant
    Filed: May 24, 1995
    Date of Patent: July 30, 1996
    Assignee: ROUSSEL UCLAF
    Inventors: Jozsef Aszodi, Jean-Francois Chantot, Solange G. D'Ambrieres
  • Patent number: 5538963
    Abstract: The syn isomer of a compound of the formula ##STR1## in the R or S form or a mixture of R and S forms wherein selected from the group consisting of ##STR2## and their non-toxic, pharmaceutically acceptable acid addition salts wherein the substituents are defined as in the specification having antibacterial activity and their preparation.
    Type: Grant
    Filed: September 27, 1994
    Date of Patent: July 23, 1996
    Assignee: Roussel Uclaf
    Inventors: Jean-Francois Chantot, Solange G. D'Ambrieres, Daniel Humbert, Jean-Georges Teutsch
  • Patent number: 5532375
    Abstract: Compounds useful in the treatment of Alzheimer's disease, senile dementia, or memory disorders which have the formula ##STR1## in which R represents a hydrogen atom, a linear, branched or cyclic alkyl radical, saturated or unsaturated, containing up to 8 carbon atoms, possibly substituted by a free or esterified carboxy radical or R represents an aralkyl radical containing up to 10 carbon atoms and R' represents a linear or branched, saturated or unsaturated, alkyl radical, containing up to 8 carbon atoms, a radical --COalk.sub.1 or a radical --(CH.sub.2).sub.2 N(alk.sub.2).sub.2, alk.sub.1 and alk.sub.2 representing an alkyl radical containing up to 8 carbon atoms, as well as their addition salts with acids. Also compositions containing the same, method of preparation and method of treatment using the same.
    Type: Grant
    Filed: September 30, 1994
    Date of Patent: July 2, 1996
    Assignee: Roussel-UCLAF
    Inventors: Giulio Galliani, Fernando Barzashi, Alina Butti, Carla Bonetti, Emilio Toja
  • Patent number: 5530022
    Abstract: A compound in all possible stereoisomeric forms and their mixtures of the formula ##STR1## wherein R is selected from the group consisting of ##STR2## having excellent pesticidal, particularly insecticidal, properties.
    Type: Grant
    Filed: August 9, 1994
    Date of Patent: June 25, 1996
    Assignee: Roussel-Uclaf
    Inventors: Didier Babin, Marc Benoit, Jean P. Demoute
  • Patent number: 5527823
    Abstract: A formulation suitable for spraying or for dilution with water to form a sprayable preparation, the formulation comprising an active ingredient, optionally a carrier or solvent for the active ingredient, an emulsifier and an evaporation retardant, characterized in that the formulation satisfies formula ##EQU1## where L is less than or equal to 15, A=700376, B=-1.51, C=0.8472, M.sub.oil is the weighted average relative molar mass of the oil phase M.sub.retardant is the weighted average relative molar mass of the retardant, and X=(M.sub.oil) 1.8/Y, where Y is the molar solubility ration of the formulation, defined as the minimum number of moles of the oil phase which will dissolve the retardant, divided by the number of moles of retardant, provided that, in the formula above, any solvent which has no liquid phase at 27.degree. C. at atmospheric pressure is excluded. The formulation may comprise a pesticide or herbicide. The action of the evaporation retardant is improved.
    Type: Grant
    Filed: February 8, 1994
    Date of Patent: June 18, 1996
    Assignee: Roussel UCLAF
    Inventors: Robert Martin, David A. Jeffries, Denise K. North, John M. Groome, Peter L. Crampton, Andrew J. Huson
  • Patent number: 5527780
    Abstract: A compound selected from the group consisting of a compound of the formula ##STR1## wherein R is --(CH.sub.2).sub.n --Ar.sub.1 or --XAr.sub.2, n is an integer from 1 to 6, Ar.sub.1 and Ar.sub.2 are individually selected from the group consisting of a) carbocyclic aryl of up to 18 carbon atoms substituted by at least one member of the group consisting of free carboxy, alkoxy carbonyl and carboxyl salified with a pharmaceutically acceptable base, --OH, halogen, --NO.sub.2, --CN, ##STR2## and alkyl, cycloalkyl, alkenyl, alkynyl, alkoxy, alkenyloxy, alkynyloxy, alkylthio, alkenylthio, alkynylthio, N-alkyl, N-alkenyl and N-alkynyl of up to 12 carbon atoms optionally substituted with at least one halogen, R.sub.1 and R.sub.2 are individually hydrogen or alkyl of 1 to 12 carbon atoms, b) ##STR3## wherein R.sub.
    Type: Grant
    Filed: November 1, 1993
    Date of Patent: June 18, 1996
    Assignee: Roussel Uclaf
    Inventors: Constantin Agouridas, Alain Bonnefoy, Jean-Francois Chantot, Alexis Denis, Odile Le Martret
  • Patent number: 5527919
    Abstract: A novel process for the preparation of a compound of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are defined in the text.
    Type: Grant
    Filed: January 4, 1994
    Date of Patent: June 18, 1996
    Assignee: Roussel Uclaf
    Inventors: Neerja Bhatnagar, Jean Buendia, Christine Griffoul, Holger Heitsch, Adalbert Wagner
  • Patent number: 5525594
    Abstract: A method of treating hyperandrogenism in warm-blooded animals comprising administering to warm-blooded animals an antiandro genically effective amount of oenotheine B and a process for the preparation of oenotheine B.
    Type: Grant
    Filed: November 14, 1994
    Date of Patent: June 11, 1996
    Assignee: Roussel Uclaf
    Inventors: Jean-Francois Gourvest, Alexander Kasal, Dominique Lesuisse, Jean-Georges Teutsch
  • Patent number: 5523322
    Abstract: A method of inhibiting blood-platelet aggregation in warm-blooded animals comprising administering to warm-blooded animals a blood-platelet aggregation inhibiting effective amount of a compound selected from the group consisting of a compound of the formula ##STR1## wherein R is selected from the group consisting of --NH--CO--NH.sub.2, --NH--CO--CH.sub.3, --OH and their non-toxic, pharmaceutically acceptable acid addition salts.
    Type: Grant
    Filed: June 30, 1994
    Date of Patent: June 4, 1996
    Assignee: Roussel UCLAF
    Inventors: Denis Blache, Christian Bloy, Bernard Hercelin
  • Patent number: 5510331
    Abstract: Peptides of the formulaR.sub.1 --HX.sub.1 DX.sub.2 IX.sub.3 Iwherein R.sub.1, X.sub.1, X.sub.2 and X.sub.3 are defined as in the specification having antihypertensive activity without vascoconstricting activity.
    Type: Grant
    Filed: October 13, 1994
    Date of Patent: April 23, 1996
    Assignee: Roussel UCLAF
    Inventors: Gilles Hamon, Eve Mahe, Dung Le-Nguyen
  • Patent number: 5508452
    Abstract: A process for the preparation of a compound of the formula ##STR1## in which rings A and B are a remainder: ##STR2## in which the 3-ketone function is optionally protected in the form of a ketal, thioketal, hemithioketal or enol ether, or a remainder: ##STR3## wherein R is methyl or --CH.sub.2 --OR', R' is hydrogen or ether remainder or ester remainder, R.sub.1 and R.sub.2 together form a second bond, or R.sub.1 and R.sub.2 form together an epoxide in beta position, or R.sub.1 is hydrogen, ketone or .alpha.- or .beta.- hydroxy, free or protected in the form of an ether or ester and R.sub.2 is hydrogen, or R.sub.1 is hydrogen and R.sub.2 is .alpha.-hydroxy function, or R.sub.1 is .beta.-hydroxy, free or protected in the form of an ether or ester and R.sub.2 is .alpha.-fluorine or bromine and R.sub.3 is hydrogen or .alpha. or .beta. fluorine or methyl comprising reacting a compound of the formula ##STR4## in which A, B, R, R.sub.1, R.sub.2 and R.sub.
    Type: Grant
    Filed: January 12, 1994
    Date of Patent: April 16, 1996
    Assignee: Roussel Uclaf
    Inventors: Patrick Roussel, Michel Vivat
  • Patent number: 5508414
    Abstract: A compound of the formula ##STR1## wherein Ar is phenyl optionally substituted with at least one member of the group consisting of halogen, methylenedioxy, phenyl, phenoxy, --CF.sub.3 and alkyl, alkoxy and alkylthio of 1 to 6 carbon atoms, Z is selected from the group consisting of hydrogen, chlorine, --CF.sub.3 and alkyl, alkoxy and alkylthio of 1 to 6 carbon atoms, R.sub.1 and R.sub.2 are individually alkyl of 1 to 6 carbon atoms and the exocyclic double bonds independently have (E) or (Z) geometry having fungicidal activity and a process for their preparation.
    Type: Grant
    Filed: November 18, 1994
    Date of Patent: April 16, 1996
    Assignee: Roussel UCLAF
    Inventors: Jean-Louis Brayer, Jean-Pierre Demoute, Gilles Mourioux
  • Patent number: 5506249
    Abstract: A compound selected from the group consisting of a compound of the formula ##STR1## wherein R.sub.1 is hydrogen or alkyl of 1 to 3 carbon atoms; R.sub.2 is cycloalkyl of 3 to 6 carbon atoms; R.sub.4 is selected from the group consisting of halogen, nitrile, nitro, --SCH.sub.3, -alkylcarbonyl of 1 to 6 carbon atoms, cycloalkylcarbonyl of 3 to 6 carbon atoms, --CX.sub.3, 'WCX.sub.3, --(CH.sub.2).sub.n CX.sub.3, --(CX.sub.2).sub.n CX.sub.3, --W(CX.sub.2).sub.n CX.sub.3 and a --W(CH.sub.2).sub.n CX.sub.3, in which X is halogen, W is oxygen or sulfur, and n is 1, 2 or 3; and R.sub.5 is selected from the group consisting of hydrogen, alkyl of 1 to 3 carbon atoms and cycloalkyl of 3 to 6 carbon atoms; with the proviso that if R.sub.5 is hydrogen, R.sub.4 is not --SCH.sub.3 or --CF.sub.3 and their non-toxic pharmaceutically acceptable salts having anti-prolifera-tive, anti-inflammatory and anti-tumor activity.
    Type: Grant
    Filed: December 5, 1994
    Date of Patent: April 9, 1996
    Assignee: Roussel UCLAF
    Inventors: Elizabeth A. Kuo, Robert Westwood
  • Patent number: 5504203
    Abstract: A compound of the formula ##STR1## wherein R is=0 or ##STR2## and the rings A and B are selected from the group consisting of ##STR3## K is oxo or a protector group of oxo of the formula ##STR4## n is 2 or 3 and R.sub.1 is an ether or ester remainder, K' is oxo or a protector oxime, hydrazone or semicarbazone group and the wavy lines symbolize an isomer mixture, a process for their preparation and their use as intermediates.
    Type: Grant
    Filed: March 9, 1995
    Date of Patent: April 2, 1996
    Assignee: Roussel Uclaf
    Inventors: Jean Buendia, Remi Chauvin, Michel Vivat
  • Patent number: 5504112
    Abstract: A compound in all possible stereoisomeric forms and their mixtures of the formula ##STR1## wherein X is selected from the group consisting of hydrogen, --CN, alkyl, alkenyl and alkynyl of up to 4 carbon atoms and aralkynyl of up to 10 carbon atoms, Y is selected from the group consisting of halogen, --CF.sub.3, --CH.sub.2 F and --CHF.sub.2 and R.sub.1 is hydrogen and R.sub.2 is halogen or R.sub.1 and R.sub.2 are --CF.sub.3 or R.sub.1 and R.sub.2 are individually halogen.
    Type: Grant
    Filed: May 15, 1995
    Date of Patent: April 2, 1996
    Assignee: Roussel Uclaf
    Inventors: Didier Babin, Marc Benoit, Raphael Bouchet, Jean-Pierre Demoute
  • Patent number: 5502182
    Abstract: A compound of the formula ##STR1## wherein K represents a protective group of the oxo of the formula ##STR2## wherein n is 2 or 3, and M is chlorine, bromine, or ##STR3## wherein R.sub.a and R.sub.b are individually selected from the group consisting of hydrogen, --OH, and alkyl and alkoxy of 1 to 4 carbon atoms and R is selected from the group consisting of alkyl of 1 to 6 carbon atoms, aralkyl of 7 to 15 carbon atoms, trialkyl silyl triphenyl silyl and diphenyl alkyl silyl.
    Type: Grant
    Filed: December 22, 1994
    Date of Patent: March 26, 1996
    Assignee: Roussel Uclaf
    Inventors: Francis Brion, Jean Buendia, Christian Diolez, Michel Vivat
  • Patent number: 5502223
    Abstract: A process for the preparation of a compound of the formula ##STR1## wherein R.sub.1 is acyl of an organic carboxylic acid of 1 to 8 carbon atoms useful as intermediates for synthesis of therapeutically active steroids.
    Type: Grant
    Filed: February 21, 1995
    Date of Patent: March 26, 1996
    Assignee: Roussel Uclaf
    Inventors: Francis Brion, Jean Buendia, Christian Diolez, Michel Vivat