Patents Assigned to Roussel-UCLAF
  • Patent number: 5268169
    Abstract: A method of treating ovarian cancer in warm-blooded animals comprising intraperitoneally administering to warm-blooded animals by perfusion a recombinant polypeptide of human gamma interferon type with a specific activity at least equal to 1.times.10.sup.7 U/mg in an anti-cancer effective amount.
    Type: Grant
    Filed: April 13, 1992
    Date of Patent: December 7, 1993
    Assignee: Roussel Uclaf
    Inventors: Maud Brandely, Danielle Lando
  • Patent number: 5262438
    Abstract: All possible stereoisomers and mixtures thereof of a compound of the formula ##STR1## wherein X is selected from the group consisting of hydrogen, fluorine, chlorine and bromine, R is selected from the group consisting of optionally substituted alkyl, alkenyl, alkynyl and cycloalkyl of up to 8 carbon atoms, optionally substituted aryl and aralkyl of up to 14 carbon atoms and optionally substituted heterocyclic and Z is selected from the group consisting of hydrogen, methyl, --CN and --C.tbd.CH having pesticidal, particularly insecticidal properties.
    Type: Grant
    Filed: July 1, 1992
    Date of Patent: November 16, 1993
    Assignee: Roussel-UCLAF
    Inventors: Marc Benoit, Jacques Demassey, Jean-Pierre Demoute
  • Patent number: 5260463
    Abstract: An improved process for the preparation of hydrocortisone and novel intermediates which avoids an 11-hydroxylation step and results in improved yields.
    Type: Grant
    Filed: August 25, 1992
    Date of Patent: November 9, 1993
    Assignee: ROUSSEL-UCLAF
    Inventors: Francis Brion, Jean Buendia, Christian Diolez, Michel Vivat
  • Patent number: 5254566
    Abstract: A compound selected from the group consisting of racemates, enantiomeric and diastereoisomeric forms of a compound of the formula ##STR1## wherein R.sub.1 and R.sub.2 are individually selected from the group consisting of hydrogen and alkyl of 1 to 5 carbon atoms optionally substituted with at least one halogen, hydroxy, alkyl or alkoxy of 1 to 4 carbon atoms or taken together with the nitrogen to which they are attached form a heterocycle optionally containing a heteroatom selected from the group consisting of --O--, --S-- and nitrogen optionally substituted with alkyl or alkoxy of 1 to 5 carbon atoms, optionally substituted benzyl and phenyl, R.sub.3 and R.sub.4 are individually selected from the group consisting of hydrogen, halogen, hydroxy and alkyl and alkoxy of 1 to 5 carbon atoms optionally substituted with at least one substituent selected from the group consisting of halogen, hydroxy, phenyl and alkyl and alkoxy of 1 to 4 carbon atoms, R.sub.
    Type: Grant
    Filed: September 22, 1992
    Date of Patent: October 19, 1993
    Assignee: Roussel Uclaf
    Inventors: Francois Clemence, Gilles Hamon, Odile Le Martret
  • Patent number: 5252708
    Abstract: Preparation process for a protein comprising at least one intramolecular disulphide bridge, and optionally one or more additional cysteines, comprising the oxidation of the corresponding reduced recombinant protein using an oxidizing agent and characterized in that an aqueous solution of the reduced protein is reacted at a pH of less than 5.0.
    Type: Grant
    Filed: May 6, 1992
    Date of Patent: October 12, 1993
    Assignee: Roussel Uclaf
    Inventors: Pierre Y. Abecassis, Jacques Leclaire, Philippe Riberon
  • Patent number: 5248773
    Abstract: A compound of the formula ##STR1## in which ##STR2## is either a 3-keto-.DELTA.4-system or a 3-keto -.DELTA.1,4-system or a 3-OR.sub.4 -.DELTA.5-system in which R.sub.4 is hydrogen or a protector group of hydroxy, R is methyl, --CH.sub.2 OH or --CH.sub.2 OR', in which R' is a protector group of hydroxy, R.sub.1 and R'.sub.1 are individually selected from the group consisting of methyl, a branched alkyl not possessing hydrogen in the .beta. position of 5 to 8 carbon atoms, aryl of up to 10 carbon atoms, heteroaryl of up to 10 carbon atoms and at least one heteroatom chosen from nitrogen, sulfur and oxygen and benzyl, n and m, are individually numbers 0 or 1, R.sub.2 and R.sub.3 are hydrogen or R.sub.2 is fluorine and R.sub.3 is formyloxy or acetyloxy and the dotted lines in position 9(11) indicate the optional presence of a second bond which are useful for the preparation of compounds of formula A.
    Type: Grant
    Filed: June 25, 1992
    Date of Patent: September 28, 1993
    Assignee: Roussel-UCLAF
    Inventors: Jean Boivin, Christine Chauvet, Samir Zard
  • Patent number: 5247079
    Abstract: A compound selected from the group consisting of a compound of the formula ##STR1## wherein Y is a nitrogen atom or carbon atom bearing Z, Z is selected from the group consisting of hydrogen, halogen, --C.ident.N, --N.sub.3 and --C(Hal).sub.3, Hal is a halogen, X is cycloalkyl of 3 to 6 carbon atoms or hydrogen with the proviso that when X is hydrogen, Y must be nitrogen, R is selected from the group consisting of hydrogen, alkyl of 1 to 5 carbon atoms, phenyl and substituted phenyl and their non-toxic, pharmaceutically acceptable acid addition salts, a process and intermediate for preparing them, having tranquillizing properties.
    Type: Grant
    Filed: October 23, 1991
    Date of Patent: September 21, 1993
    Assignee: Roussel Uclaf
    Inventors: Charles J. R. Hedgecock, Stuart D. Jones
  • Patent number: 5245073
    Abstract: Novel 2,2-dimethyl-cyclopropane carboxylic acid derivatives of the formula ##STR1## wherein X.sub.1 and X.sub.2 are individually halogen, R.sub.1 is selected from the group consisting of halogen, alkyl of 1 to 8 carbon atoms, optionally substituted aryl of 6 to 14 carbon atoms, perfluoroalkyl of 1 to 8 carbon atoms, --CN and ##STR2## R' is alkyl of 1 to 8 carbon atoms, Y is selected from the group consisting of --SO.sub.2 Alk.sub.1, --SO.sub.2 Ar, ##STR3## Alk.sub.1 is optionally unsaturated alkyl of 1 to 8 carbon atoms optionally substituted with at least one halogen, Ar is aryl of 6 to 14 carbon atoms optionally substituted with at least one halogen Alk.sub.2 and Alk.sub.3 and Alk.sub.2 ' and Alk.sub.
    Type: Grant
    Filed: August 20, 1991
    Date of Patent: September 14, 1993
    Assignee: Roussel Uclaf
    Inventors: Joseph Cadiergue, Jean-Pierre Demoute, Jean Tessier
  • Patent number: 5243043
    Abstract: Novel syn isomers of 3-alkoxymethyl or 3-alkylthio-methyl-7-[2-(2-amino-4-thiazolyl)-2-oximino-acetamido]-cephalo sporanic acid compounds of the formula ##STR1## wherein R is selected from the group consisting of hydrogen, alkyl of 1 to 6 carbon atoms, alkenyl and alkynyl of 2 to 6 carbon atoms, cycloalkyl of 3 to 6 carbon atoms, acyl of an organic carboxylic acid of 1 to 18 carbon atoms and alkoxy carbonyl of 2 to 6 carbon atoms, A is selected from the group consisting of hydrogen, alkali metal, alkaline earth metal, --NH.sub.
    Type: Grant
    Filed: October 31, 1990
    Date of Patent: September 7, 1993
    Assignee: Roussel Uclaf
    Inventor: Rene Heymes
  • Patent number: 5240960
    Abstract: A compound selected from the group consisting of all tautomeric forms of a cycloalky-propanamide of the formula ##STR1## wherein R.sub.1 is cycloalkyl of 3 to 6 carbon atoms, R.sub.2 is hydrogen or alkyl of 1 to 3 carbon atoms, R.sub.3, R.sub.4, R.sub.5, R.sub.6 and R.sub.7 are individually selected from the group consisting of hydrogen, halogen, --NO.sub.2, azido, --CN, alkyl, alkoxy and alkylthio of 1 to 6 carbon atoms, --(CH.sub.2).sub.m --CF.sub.3, --O--(CH.sub.2).sub.m --CF.sub.3, --S--(CH.sub.2).sub.m --CF.sub.3, m is an integer from 0 to 3, --CF.sub.2 --Hal, --OCF.sub.2 --Hal, ##STR2## n is an integer from 1 to 3, Hal, Hal.sub.1, Hal.sub.2 and Hal.sub.3 are individually halogen, and --COR', R' is --OH or alkyl or alkoxy of 1 to 3 carbon atoms or R.sub.4 and R.sub.5 together are --O--CH.sub.2 --O-- and their non-toxic, pharmaceutically acceptable basic salts having anti-inflammatory activity.
    Type: Grant
    Filed: October 30, 1991
    Date of Patent: August 31, 1993
    Assignee: Roussel Uclaf
    Inventors: Philip T. Hambleton, Charles J. R. Hedgecock, David P. Kay, Elizabeth A. Kuo, Wilfred R. Tully
  • Patent number: 5234944
    Abstract: A compound selected from the group consisting of enantiomers and diastereoisomer forms and mixtures thereof of the formula ##STR1## wherein R.sub.6 is selected from the group consisting of hydrogen, halogen and alkyl and alkoxy of 1 to 5 carbon atoms, R.sub.1 and R.sub.2 are individually hydrogen or alkyl of 1 to 5 carbon atoms or taken together with the carbon atoms to which they are attached form a cycloalkyl of 3 to 6 carbon atoms optionally containing a heteroatom selected from the group consisting of --S--, --O-- and --N--, one of A and B has the formula ##STR2## and the other has the formula ##STR3## R is selected from the group consisting of hydrogen and alkyl of 1 to 5 carbon atoms, Z is selected from the group consisting of --(CH.sub.2).sub.n --, branched alkylene of 2 to 8 carbon atoms and --CH.sub.2 O--, n is an integer of 0 to 5, X, X' and X" are individually selected from the group consisting of hydrogen, alkyl and alkoxy of 1 to 4 carbon atoms, halogen, --OH, --CF.sub.3, --NO.sub.2, --NH.sub.
    Type: Grant
    Filed: November 3, 1992
    Date of Patent: August 10, 1993
    Assignee: Roussel UCLAF
    Inventors: Francois Clemence, Odile Le Martret, Francoise Delevallee, Michel Fortin
  • Patent number: 5231107
    Abstract: Compounds useful in the treatment of patients suffering from senile dementia, Alzheimer's disease or memory defects, of the formula ##STR1## in which R' represents hydrogen, a linear, branched or cyclic alkyl, alkenyl or alkynyl, containing up to 8 carbon atoms, and R represents a linear, branched or cyclic alkyl, alkenyl, or alkynyl, containing up to 18 carbon atoms, possibly substituted, aryl containing up to 14 carbon atoms, possibly substituted, aralkyl containing up to 18 carbon atoms, possibly substituted, as well as their addition salts with organic or mineral acids, and to compounds of formula (I) in which R represents phenyl substituted in the 4 position by Br, F, CH.sub.3, NO.sub.2 or C(CH.sub.3).sub.2 C(CH.sub.3).sub.3 and R' represents CH.sub.3.
    Type: Grant
    Filed: April 1, 1992
    Date of Patent: July 27, 1993
    Assignee: Roussel Uclaf
    Inventors: Guilio Galliani, Fernando Barzaghi, Carla Bonetti, Emilio Toja
  • Patent number: 5219872
    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: February 26, 1987
    Date of Patent: June 15, 1993
    Assignee: Roussel UCLAF
    Inventors: Giulio Galliani, Fernando Barzaghi, Alina Butti, Carla Bonetti, Emilio Toja
  • Patent number: 5219873
    Abstract: Compounds useful in the treatment of Alzheimer's disease, senile dimentia and memory disorders of the formula ##STR1## in which R represents hydrogen, hydroxyl, a linear, branched or cyclic, saturated or unsaturated, alkyl, containing up to 8 carbon atoms, possibly substituted by free or esterified carboxy or R represents aralkyl containing up to 10 carbon atoms or --COOZ in which Z represents a linear, branched or cyclic saturated or unsaturated, alkyl containing up to 8 carbon atoms and R.sub.2 represents hydrogen or a linear or branched, saturated or unsaturated alkyl containing up to 8 carbon atoms, COalk.sub.1 radical or (CH.sub.2).sub.2 N(alk.sub.2).sub.2, alk.sub.1 and alk.sub.2 representing an alkyl containing up to 8 carbon atoms, as well as their addition salts with acids provided that if R represents an alkyl R.sub.2 does not represent hydrogen; also therapeutic compositions containing at least one said compound and method of treating patients with said compounds.
    Type: Grant
    Filed: September 15, 1989
    Date of Patent: June 15, 1993
    Assignee: Roussel UCLAF
    Inventors: Giulio Galliani, Fernando Barzaghi, Carla Bonetti, Emilio Toja
  • Patent number: 5219565
    Abstract: A method for treating primary cancers of the pleura in humans comprising administering to humans an amount of a polyprotein having human interleukin activity sufficient to treat primary cancers of the pleura.
    Type: Grant
    Filed: June 8, 1990
    Date of Patent: June 15, 1993
    Assignee: Roussel Uclaf
    Inventors: Maud Brandely, Danielle Lando
  • Patent number: 5210093
    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: March 16, 1992
    Date of Patent: May 11, 1993
    Assignee: Roussel Uclaf
    Inventors: Jean-Louis Brayer, Jean-Pierre Demoute, Gilles Mourioux
  • Patent number: 5204094
    Abstract: A method of treating pneumothoraxes in warm-blooded animals comprising administering to warm-blooded animals an amount of polypeptide having human interleukin 2 activity sufficient to treat pneumothoraxes.
    Type: Grant
    Filed: January 16, 1992
    Date of Patent: April 20, 1993
    Assignee: Roussel Uclaf
    Inventors: Maud Brandely, Christian Boutin
  • Patent number: 5204479
    Abstract: The subject of the invention is the compounds of formula (I): ##STR1## in which: R represents a hydrogen atom, a saturated or unsaturated, linear, branched or cyclic alkyl radical containing up to 8 carbon atoms,R' represents an amine-containing moiety of an .alpha.-amino acid or a peptide, containing as an end group an amine-containing moiety of an .alpha.-amino acid as well as their addition salts with organic or mineral acids.The compounds of formula (I) have useful pharmacological properties which justify their use in therapeutics.
    Type: Grant
    Filed: May 15, 1991
    Date of Patent: April 20, 1993
    Assignee: Roussel Uclaf
    Inventors: Emilio Toja, Carla Bonetti, Fernando Barzaghi, Giulio Galliani
  • Patent number: 5204341
    Abstract: 1-arylsulphonyl-2-pyrrolidone derivatives for treating spasmodic disorders in gastro-enterology, in gynaecology, in obstetrics, in urology; intermediates in the preparation of such products; methods for preparing such products and pharmaceutical preparations containing such products.
    Type: Grant
    Filed: December 11, 1991
    Date of Patent: April 20, 1993
    Assignee: Roussel Uclaf
    Inventors: Emilio Toja, Carla Bonetti, Fernando Barzaghi, Giulio Galliani
  • Patent number: 5202316
    Abstract: A compound selected from the group consisting of a compound of the formula ##STR1## wherein R.sub.A, R'.sub.A, R.sub.B and R'.sub.B are individually selected from the group consisting of hydrogen and alkyl of 1 to 4 carbon atoms or R.sub.A and R'.sub.A or R.sub.B and R'.sub.B together with the nitrogen atom to which they are attached form a 5- to 6-member heterocycle optionally substituted with alkyl of 1 to 3 carbon atoms and Y is hydrogen or ##STR2## wherein R.sub.6 is selected from the group consisting of hydrogen, --CH.sub.3, --F and --Cl, R.sub.9 and R.sub.11 form a second bond at 9(11) or R.sub.9 is hydrogen or --F is hydrogen, --OH or .dbd.O, R.sub.16 is --CH.sub.3 or hydrogen, R.sub.17 is hydrogen, --OH or acyloxy, the dotted lines indicate the possible presence of a second bond at 1(2) and 6(7)-positions and the wavy line indicates the .alpha.- and .beta.-position and their non-toxic, pharmaceutically acceptable acid addition salts having anti-inflammatory and antioxidant activity.
    Type: Grant
    Filed: October 9, 1991
    Date of Patent: April 13, 1993
    Assignee: Roussel Uclaf
    Inventors: Andre Claussner, Jacques Leclaire, Lucien Nedelec, Daniel Philibert