Patents Assigned to Roussel-UCLAF
  • Patent number: 5494907
    Abstract: A compound selected from the group consisting of a compound of the formula ##STR1## wherein the substituents are defined as in the specification having anti-estrogen activity.
    Type: Grant
    Filed: May 19, 1994
    Date of Patent: February 27, 1996
    Assignee: Roussel UCLAF
    Inventors: Francois Nique, Jean-Georges Teutsch, Patrick Van De Velde
  • Patent number: 5493046
    Abstract: The novel process of the invention for the preparation of a compound of the formula ##STR1##
    Type: Grant
    Filed: October 27, 1994
    Date of Patent: February 20, 1996
    Assignee: Roussel-Uclaf
    Inventors: Neerja Bhatnagar, Jean Buendia, Christine Griffoul
  • Patent number: 5478938
    Abstract: Novel bicyclic compounds in all possible racemic, enantiomeric and diasteroisomeric forms of the formula ##STR1## having antagonistic properties for angiotensin II receptors and novel intermediates and process for their preparation.
    Type: Grant
    Filed: March 22, 1994
    Date of Patent: December 26, 1995
    Assignee: Roussel Uclaf
    Inventors: Francois Clemence, Michel Fortin, Jean-Luc Haesslein
  • Patent number: 5478957
    Abstract: A process for the preparation of 6.alpha.,9.alpha.-difluoro steroids of the formula ##STR1## wherein R is hydrogen or an ester remainder.
    Type: Grant
    Filed: January 26, 1994
    Date of Patent: December 26, 1995
    Assignee: Roussel-UCLAF
    Inventors: Jean-Yves Godard, Philippe Mackiewicz, Denis Prat, Christian Richard
  • Patent number: 5478821
    Abstract: A method of accelerating the proliferation of endothelial cells with inhibition of NO synthases in warm-blooded animals comprising administering to warm-blooded animals an amount of at least one compound selected from the group consisting of a .beta.-naphthoquinone of the formula ##STR1## wherein R is selected from the group consisting of --NH--CO--NH.sub.2, --NH--C0--CH.sub.3 and --0H and their non-toxic, pharmaceutically acceptable acid addition salts in an amount sufficient to accelerate the proliferation of endothelial cells.
    Type: Grant
    Filed: June 30, 1994
    Date of Patent: December 26, 1995
    Assignee: Roussel UCLAF
    Inventors: Christian Bloy, Jean-Pierre Cazenave, Bernard Hercelin, Bernard Teisseire
  • Patent number: 5476840
    Abstract: New peptidic derivatives having the general formula (I): X.sub.1 X.sub.2 X.sub.3 Ile X.sub.5 X.sub.6 wherein X.sub.1 is hydrogen, a rest of histidin, of acetyl-histidin or of D-histidin, X.sub.2 is a rest of alanin, of leucin, of tryptophan, of phenylalanin as well as their homologs in D series, X.sub.3 is a rest of alanin as well as its D series homolog, X.sub.5 is a rest of isoleucin, of alanin, of valin, of norleucin, of leucin and of aspanic acid as well as their D series homologs, X.sub.6 is a rest of tryptophan, of leucin, of isoleucin, of norleucin and their D series homologs, method for the preparation and application of such new derivatives as medicaments.
    Type: Grant
    Filed: December 3, 1993
    Date of Patent: December 19, 1995
    Assignee: Roussel Uclaf
    Inventors: Pierre Broto, Giles Hamon, Eve Mahe, Dung Le-Nguyen
  • Patent number: 5476866
    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: August 22, 1994
    Date of Patent: December 19, 1995
    Assignee: Roussel Uclaf
    Inventors: Elizabeth A. Kuo, Robert Westwood
  • Patent number: 5474996
    Abstract: Novel pyrimidine derivatives of the formula ##STR1## represents: either a group: ##STR2## or a group: ##STR3## having angiotensin II inhibiting activity.
    Type: Grant
    Filed: May 22, 1992
    Date of Patent: December 12, 1995
    Assignee: Roussel Uclaf
    Inventors: Jean-Claude Caille, Stanislas Didierlaurent, Jean-Paul Vevert
  • Patent number: 5473087
    Abstract: Mixtures of compounds of ##STR1## or a mixture of the latter and a compound of the formula ##STR2## which are useful intermediates for the preparation 20-keto-21(S)-hydroxy steroids.
    Type: Grant
    Filed: September 16, 1994
    Date of Patent: December 5, 1995
    Assignee: Roussel-Uclaf
    Inventors: Jean Buendia, Jean-Yves Godard, Philippe Mackiewicz, Christian Richard
  • Patent number: 5470867
    Abstract: Imidazoles of the formula ##STR1## and their non-toxic, pharmaceutically acceptable salts with acids and bases having an antagonistic activity against angiotensin II receptors.
    Type: Grant
    Filed: October 17, 1994
    Date of Patent: November 28, 1995
    Assignee: Roussel-Uclaf
    Inventors: Michel Fortin, Daniel Frechet, Gilles Hamon, Simone Jouquey, Jean-Paul Vevert
  • Patent number: 5466710
    Abstract: The present invention provides a class of substituted bicyclooctanes of formula ##STR1## wherein R is a C.sub.2-10 non-aromatic hydrocarbyl optionally substituted by cyano, halo, C.sub.1-4 alkoxy, C.sub.1-4 haloalkoxy or S(O).sub.m R.sup.3 ; R.sup.1 and r.sup.2 are independently hydrogen, halo, a C.sub.1-3 aliphatic group optionally substituted, S(O).sub.m,R.sup.4, or R.sup.1 and R.sup.2 and the carbon atoms to which they are attached form a C.sub.5-7 carbocyclic ring optionally substituted by halo, or a C.sub.1-3 aliphatic or alkoxy group;A-X is a group:(i) A'C.tbd.CX in which A' is a C.sub.3-6 alkyl, alkenyl or alkynyl or a C.sub.3-10 cycloalkyl or cycloalkenyl group all optionally containing one to three hetero atoms.(ii) BX in which B is a group (CH.sub.2).sub.2 O or (CH.sub.2).sub.2 S(O).sub.n or a C.sub.2-6 aliphatic chain optionally containing one or two oxygen or sulphur atoms and/or double bonds and optionally further substituted;X is hydrogen, halo, SiR.sup.5 R.sup.6 R.sup.7 or SnR.sup.5 R.sup.6 R.
    Type: Grant
    Filed: October 6, 1993
    Date of Patent: November 14, 1995
    Assignee: Roussel Uclaf
    Inventors: John B. Weston, John P. Larkin, Ian H. Smith
  • Patent number: 5466458
    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 where the formulation satisfies the following 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 ratio 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 extruded. The formulation may include a pesticide or herbicide. The action of the evaporation retardant is improved.
    Type: Grant
    Filed: February 15, 1994
    Date of Patent: November 14, 1995
    Assignee: Roussel Uclaf
    Inventors: Robert Martin, George R. Cayley, Jonathan R. M. Thacker, Franklin R. Hall, Denise K. North, John M. Groome, David A. Jeffries
  • Patent number: 5459149
    Abstract: The present Application discloses pesticidally active compounds of formula (I):Q(CH.sub.2).sub.a (O).sub.b Q.sup.1 CR.sup.2 =CR.sup.3 CR.sup.4 =CR.sup.5 CXNR.sup.1 R.sup.xor a salt or propesticide thereof, wherein Q is an optionally substituted aromatic monocyclic or fused bicyclic ring system in which at least one ring is aromatic, or Q is a dihalovinyl group or a group R.sup.6 --C=C--where R.sup.6 is C.sub.1-4 alkyl, tri C.sub.1-4 alkylsilyl, halo or hydrogen; Q.sup.1 is a 1,2-cyclopropyl ring optionally substituted by one or more groups selected from C.sub.1-3 alkyl, halo, C.sub.1-3 haloalkyl, C.sub.2-3 alkynyl, or cyano; or Q.sup.1 is (CH.sub.2).sub.7 ; a=0 or 1; b=0 or 1; R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are the same or different with at least one being hydrogen and the others being independently selected from hydrogen, halo, C.sub.1-4 alkyl or C.sub.1-4 haloalkyl; X is oxygen or sulphur;R.sup.1 is phenyl optionally substituted by 1-5 substituents chosen from: a) C.sub.1-4 alkyl, C.sub.
    Type: Grant
    Filed: September 20, 1994
    Date of Patent: October 17, 1995
    Assignee: Roussel Uclaf
    Inventors: John E. Robinson, George S. Cockerill
  • Patent number: 5455238
    Abstract: A syn isomer in (R) or (S) form or a mixture thereof of a compound of the formula ##STR1## in the form of an internal salt or a non-toxic, pharmaceutically acceptable acid addition salt wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.5 are individually defined in the specification, R.sub.4 is --OH or alkoxy of 1 to 8 carbon atoms, A and A' are individually selected from the group consisting of hydrogen, an equivalent of an alkali metal or alkaline earth metal, magnesium, ammonium and an organic amine, or one or two of --COOA or --COOA' ARE --CO.sub.2 --, the wavy line means --CH.sub.2 R.sub.6 can be in the E or Z position, R.sub.6 in the quaternary ammonium form is selected from the group consisting of ##STR2## X is defined as in the specification with the proviso that when R.sub.3 is --OH or alkoxy of 1 to 8 carbon atoms, at least one R.sub.1, R.sub.2 and R.sub.5 is other than hydrogen having antibacterial properties.
    Type: Grant
    Filed: December 11, 1992
    Date of Patent: October 3, 1995
    Assignee: Roussel Uclaf
    Inventors: Jozsef Aszodi, Jean-Francois Chantot, Patrick Fauveau, Solange Gouin D'Ambrieres, Daniel Humbert
  • Patent number: 5455048
    Abstract: Microcapsules containing at least one sun filter having been hardened so as to be impervious with a size of 1 to 1250 micrometers whereby the sun filters do not come in contact with the skin.
    Type: Grant
    Filed: April 16, 1992
    Date of Patent: October 3, 1995
    Assignee: Roussel UCLAF
    Inventors: Paul Lahmani, Lise Simoneau-Agopian
  • Patent number: 5451690
    Abstract: A compound of the formula ##STR1## wherein R is selected from the group consisting of hydrogen, acyl of an organic carboxylic acid of 1 to 8 carbon atoms, allyloxycarbonyl, alkoxycarbonyl and aralkoxycarbonyl of up to 8 carbon atoms and alkylsulfonyl and arylsulfonyl of up to 8 carbon atoms and their use to prepare substituted 16,17-methylenedioxy-steroids and novel intermediates.
    Type: Grant
    Filed: January 13, 1995
    Date of Patent: September 19, 1995
    Assignee: Roussel Uclaf
    Inventors: Luc Devocelle, Philippe Mackiewicz
  • Patent number: 5451696
    Abstract: A compound of the formula ##STR1##
    Type: Grant
    Filed: September 30, 1994
    Date of Patent: September 19, 1995
    Assignee: Roussel-UCLAF
    Inventors: Marc Benoit, Sylvain Laugraud, Jean-Louis Brayer
  • Patent number: 5444051
    Abstract: Compounds of the formula ##STR1## wherein X and X' form C.dbd.O or C.dbd.NOR, R is selected from the group consisting of hydrogen, heterocycle, alkyl, alkenyl, alkynyl, all optionally substituted,or X is ##STR2## R.sub.a and R.sub.b are hydrogen or a hydrocarbon group or form together with the nitrogen a heterocycle, or with A forms a 9-N, 11-O ring, and X' is hydrogen, --Y and Y' have the same definition as X and X', B is hydrogen or OR.sub.4, R.sub.4 is hydrogen or forms together with A a carbonate or a carbamate, A forms with C a double bond or A is OR'.sub.4, R'.sub.4 is hydrogen or forms together with B a carbonate or ##STR3## R.sub.2 is alkyl or --CONH.sub.2, --CONHCOR.sub.11 or --CONHSO.sub.2 R.sub.11, R.sub.11 is a hydrocarbon up to 18 carbon atoms, R.sub.3 is hydrogen, ##STR4## and Z is hydrogen or a carboxylic acid remainder and their non-toxic, pharmaceutically acceptable acid addition salts, their preparation and intermediates useful as antibiotics.
    Type: Grant
    Filed: June 28, 1993
    Date of Patent: August 22, 1995
    Assignee: Roussel UCLAF
    Inventors: Constantin Agouridas, Yannick Benedetti, Jean-Francois Chantot, Alexis Denis, Claude Fromentin, Odile Le Martret
  • Patent number: 5443837
    Abstract: A method of synchronizing estrus in breeding animals comprising parenterally administering to breeding animals an estrus synchronizing amount of 17.alpha.-allyl-.DELTA..sup.4,9,11 -estratriene-17.beta.-ol-3-one.
    Type: Grant
    Filed: October 13, 1993
    Date of Patent: August 22, 1995
    Assignee: Roussel Uclaf
    Inventor: Alain Jobard
  • Patent number: 5439890
    Abstract: A compound of the formula ##STR1## wherein A and B are both hydrogen or A is hydrogen and B is --OH or A and B form a carbon-carbon double bond and Z is hydrogen or acyl of an organic carboxylic acid of 1 to 6 carbon atoms and their nontoxic, pharmaceutically acceptable acid addition salts having antibiotic activity.
    Type: Grant
    Filed: November 14, 1994
    Date of Patent: August 8, 1995
    Assignee: Roussel-Uclaf
    Inventors: Constantin Agouridas, Jean-Francois Chantot, Nicole Tessot