Patents Assigned to Roussel-UCLAF
  • Patent number: 5614614
    Abstract: Novel intermediates for the preparation of the compounds of Formula I wherein the substituents are as defined in the specification.
    Type: Grant
    Filed: February 21, 1995
    Date of Patent: March 25, 1997
    Assignee: Roussel Uclaf
    Inventors: Constantin Agouridas, Alain Bonnefoy, Jean-Francois Chantot, Alexis Denis, Odile Le Martret
  • Patent number: 5605912
    Abstract: A compound of the formula: ##STR1## where Q is phenyl or naphthyl optionally substituted by (a) C.sub.1-6 hydrocarbyl, C.sub.1-6 alkoxy or methylenedioxy, which in turn is optionally substituted by one to five halogen atoms; or(b) halo, cyano, nitro; or(c) a group S(O).sub.n R.sub.7 wherein n=0, 1, or 2 and R.sub.7 is C.sub.1-6 alkyl optionally substituted by halogen, or R.sub.7 is amino optionally substituted by one or two C.sub.1-6 alkyl groups; or a group NR.sub.8 R.sub.9 where R.sub.8 and R.sub.9 are independently selected from hydrogen, C.sub.1-6 alkyl or a group COR.sub.12 where R.sub.12 is C.sub.1-6 alkyl or C.sub.1-6 alkoxy;Q.sub.1 is a 1,2-cyclopropyl ring optionally substituted by a group selected from C.sub.1-13 alkyl, halo, C.sub.1-3 haloalkyl or C.sub.1-13 alkynyl or cyano;R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are the same or different with at least one being hydrogen and the others being independently selected from the group consisting of hydrogen, halo, C.sub.1-4, alkyl or C.sub.
    Type: Grant
    Filed: October 14, 1994
    Date of Patent: February 25, 1997
    Assignee: Roussel Uclaf
    Inventors: George S. Cockerill, David A. Pulman, Robert J. Blade, Malcom H. Black
  • Patent number: 5599830
    Abstract: The invention relates to the products: ##STR1## in which: R.sub.1 =alkyl, alkenyl, alkynyl, alkylthio,R.sub.2B, R.sub.3B representing:hydrogen, mercapto, formyl, acyl, carboxy nitro, cyano,--PO.sub.3 (R).sub.2, R representing hydrogen, alkyl, aryl, amino or carbamoyl,the R.sub.4B radicals; ##STR2## n=0 to 2 X'=arylR.sub.4B either represents --(CH.sub.2).sub.m1 --S(O).sub.m2 --X--R.sub.10, m1=0 to 4, m2=0 to 2either m1 is different from 0, X--R.sub.10 represents amino, or whatever m1 is, X represents a single bond or --NH--, --NH--CO--, --NH--CO--NH--,R.sub.10 =alkyl, alkenyl or aryl, or hydrogen, alkyl, alkenyl, alkynyl, acyl or amino,--S--S--R.sub.4B ', R.sub.4B ' represents R.sub.4B except for amino and alkoxy, and one of R.sub.2B and R.sub.3B represents --OR.sub.4B : ##STR3## m=0 to 2, Y.sub.B ---Y.sub.1B --B--Y.sub.2B,Y.sub.1B =aryl,B=a single bond or --CO--, --O--, --NH--CO--, --CO--NH--, --O--O--(CH.sub.2).sub.p --,p=1 to 3,Y.sub.
    Type: Grant
    Filed: January 9, 1995
    Date of Patent: February 4, 1997
    Assignee: Roussel Uclaf
    Inventors: Jean C. Caille, Alain Corbier, Michel Fortin, Gilles Hamon, Simone Jouquey, Jean P. Vevert
  • Patent number: 5596108
    Abstract: A new process for the preparation of 16.beta.-methyl-steroids of the formula ##STR1## and novel intermediates therefor which compounds are intermediates for betamethasone.
    Type: Grant
    Filed: May 18, 1995
    Date of Patent: January 21, 1997
    Assignee: Roussel Uclaf
    Inventors: Catherine Geurts, Michel Vivat
  • Patent number: 5594127
    Abstract: A compound having a formula ##STR1## in which K is defined as above, C--P being CH.sub.2 or --C.dbd.CH.sub.2 or ##STR2## and J is --SO.sub.2 R.sub.2, or C--P is C.dbd.O and J is --CH.sub.2 Hal.sub.2, or C--P is --CH SO.sub.2 R.sub.2 and J is CO.sub.2 R or Hal.sub.1, R.sub.2 is methyl, phenyl, tolyl or xylyl, R is alkyl of 1 to 6 carbon atoms, aralkyl of 7 to 15 is carbon atoms or a silylated remainder selected from the group consisting of trimethylsilyl, tert.-butyldimethylsilyl, triphenylsilyl and diphenyltert.-butylsilyl, Hal.sub.1 is halogen, Hal.sub.2 is chlorine, bromine or iodine and the wavy lines symbolize any one of the isomer forms or their mixtures which are intermediates.
    Type: Grant
    Filed: November 14, 1995
    Date of Patent: January 14, 1997
    Assignee: Roussel Uclaf
    Inventors: Francis Brion, Jean Buendia, Christian Diolez, Michel Vivat
  • Patent number: 5589497
    Abstract: A compound selected from the group consisting of compounds of the formula ##STR1## wherein R.sub.1 and R.sub.2 are individually selected from the group consisting of --CN, --NO.sub.2, halogen, --CF.sub.3, free carboxy, salified carboxy, and carboxy esterified with lower alkyl; -A-B- is selected from the group consisting of ##STR2## wherein X is --O-- or --S--, R.sub.3 is selected from the group consisting of hydrogen, alkyl, alkenyl, alkynyl, aryl, and aralkyl each of up to 12 carbon atoms, all optionally substituted with at least one member of the group consisting of --OH, halogen, --SH, --CN, acyl and acyloxy of up to 7 carbon atoms, --S-aryl of up to 12 carbon atoms optionally substituted with a member of the group consisting of --CF.sub.3, alkyl, alkoxy, alkenyl, alkenyloxy, alkynyl and alkynyloxy, with the sulfur being optionally oxidized to sulfone or sulfoxide, free, esterified, amidified or salified carboxy, .dbd.NH.sub.
    Type: Grant
    Filed: April 8, 1994
    Date of Patent: December 31, 1996
    Assignee: Roussel Uclaf
    Inventors: Andr e Claussner, Fran.cedilla.ois Goubet, Jean-Georges Teutsch
  • Patent number: 5587372
    Abstract: A syn isomer in (R) or (S) form or a mixture thereof of a compound of the formula ##STR1## syn isomer, in the (R) or (S) form or in the form of an (R,S) mixture, in the form of an internal salt or their salts with organic or mineral acids,wherein the variables are herein below defined, having antibacterial properties.
    Type: Grant
    Filed: December 13, 1993
    Date of Patent: December 24, 1996
    Assignee: Roussel Uclaf
    Inventors: Jozsef Aszodi, Jean-Francois Chantot, Patrick Fauveau, Solange G. D'Ambrieres, Daniel Hunbert, Christophe Dini
  • Patent number: 5585482
    Abstract: A process for the preparation of a compound of the formula ##STR1## wherein R and R' and the A and B are as defined in the specification. ##STR2## K is selected from the group consisting of ##STR3## n is 2 or 3 and the dotted lined is an optional bond.
    Type: Grant
    Filed: October 19, 1995
    Date of Patent: December 17, 1996
    Assignee: Roussel Uclaf
    Inventors: Francis Brion, Jean Buendia, Christian Diolez, Michel Vivat
  • Patent number: 5582822
    Abstract: A method of treating leukemia in warm-blooded animals suffering from leukemia comprising administering to said warm-blooded animals an amount of polypeptide having human interleukin 2 activity sufficient to treat leukemia.
    Type: Grant
    Filed: September 30, 1994
    Date of Patent: December 10, 1996
    Assignee: Roussel Uclaf
    Inventors: Maud Brandely, Dominique Maraninchi
  • Patent number: 5580864
    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, R.sub.3 is a .alpha.- or .beta.-methyl, n is an integer from 2 to 10, R.sub.4 is hydrogen, R.sub.5 is hydrogen, R.sub.6 and R.sub.7 are hydrogen, and their non-toxic, pharmaceutically acceptable acid addition salts in an amount sufficient to control male fertility.
    Type: Grant
    Filed: March 14, 1996
    Date of Patent: December 3, 1996
    Assignee: Roussel UCLAF
    Inventors: Armelle Bonfils, Daniel Philibert
  • Patent number: 5576064
    Abstract: A multiple emulsion to administer at least one water-soluble or liposoluble active ingredient in the form of a water/oil/water emulsion comprising a dispersed phase of a water/oil type and an aqueous dispersion medium which is a gelled aqueous phase useful as cosmetic compositions for external skin application.
    Type: Grant
    Filed: March 3, 1994
    Date of Patent: November 19, 1996
    Assignee: Roussel Uclaf
    Inventor: Alain Fructus
  • Patent number: 5574194
    Abstract: The compound 2,6-bis-(trifluoromethyl)-benzyl alcohol which is useful as an intermediate to compounds having pesticidal properties.
    Type: Grant
    Filed: October 6, 1995
    Date of Patent: November 12, 1996
    Assignee: Roussel Uclaf
    Inventors: Didier Babin, Marc Benoit, Jean-Pierre Demoute
  • Patent number: 5565588
    Abstract: New 9-alpha-hydroxy steroids are prepared by the introduction of substituents on the D-ring of 9-alpha-hydroxy-androst-4-ene-3,17-dione.The resulting compounds are useful intermediates in the synthesis of corticosteroids.
    Type: Grant
    Filed: October 4, 1994
    Date of Patent: October 15, 1996
    Assignee: Roussel UCLAF
    Inventors: Jacobus N. M. Batist, Arthur F. Marx, Willem J. Van Zoest, Jagdish C. Kapur
  • Patent number: 5561118
    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, 11-0 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 A is ##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: March 31, 1994
    Date of Patent: October 1, 1996
    Assignee: Roussel Uclaf
    Inventors: Constantin Agouridas, Yannick Benedetti, Jean-Francois Chantot, Alexis Denis, Claude Fromentin, Odile Le Martret
  • Patent number: 5559130
    Abstract: A compound selected from the group consisting of all possible racemic, enantiomeric and diastereoisomeric forms of a compound of the formula ##STR1## wherein E and G together form a group selected from the group: ##STR2## consisting of a) ##STR3## or, if appropriate, its tautomer ##STR4## and ##STR5## or E is --COOR.sub.3 and G is ##STR6## wherein A, Y, R, Ra, R.sub.1 and R.sub.2 are as defined in the specification.
    Type: Grant
    Filed: November 29, 1994
    Date of Patent: September 24, 1996
    Assignee: Roussel Uclaf
    Inventors: Fran.cedilla.ois Clemence, Michel Fortin, Odile Le Martret
  • Patent number: 5558877
    Abstract: A medical device for insertion into a vaginal cavity comprising an elastomeric ring containing 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 6 carbon atoms, R.sub.2 and R.sub.5 are individually alkyl of 1 to 6 carbon atoms, n is an integer from 2 to 6, R.sub.3 and R.sub.4 are individually aryl of 6 to 12 carbon atoms optionally substituted with 1 or 2 members of the group consisting of halogen and alkyl and alkoxy of 1 to 6 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts for the treatment and prevention of cancer.
    Type: Grant
    Filed: December 15, 1994
    Date of Patent: September 24, 1996
    Assignee: Roussel Uclaf
    Inventors: Stephen A. Matlin, Andrew T. Wilkins
  • Patent number: 5556965
    Abstract: A compound of the formula ##STR1## wherein R is hydrogen or an ester remainder, X is hydrogen or fluorine and Y combined with the doted lines represents ##STR2## or X is hydrogen and and Y combined with the dotted lines is ##STR3## and R.sub.1 is the remainder of an enol ether or ester.
    Type: Grant
    Filed: May 15, 1995
    Date of Patent: September 17, 1996
    Assignee: Roussel Uclaf
    Inventors: Jean-Yves Godard, Philippe Mackiewicz, Denis Prat, Christian Richard
  • Patent number: 5556845
    Abstract: A compound of the formula ##STR1## wherein the substituents are as defined in the specification.
    Type: Grant
    Filed: May 19, 1995
    Date of Patent: September 17, 1996
    Assignee: Roussel Uclaf
    Inventors: Fran.cedilla.ois Nique, Jean-Georges Teutsch, Patrick Van De Velde
  • Patent number: 5556983
    Abstract: Novel phenyimidazolidines having the following formula ##STR1## wherein the substituents are as recited in the specification and their non-toxic, pharmaceutically acceptable acid addition salts having anti-androgenic activity.
    Type: Grant
    Filed: February 13, 1995
    Date of Patent: September 17, 1996
    Assignee: Roussel Uclaf
    Inventors: Andr e Claussner, Francois Goubet, Jean-Georges Teutsch
  • Patent number: 5556962
    Abstract: A compound of the formula ##STR1## wherein K is a protective group of the oxo of the formula ##STR2## wherein n is 2 or 3 and L is a 11.beta.-hydroxy, the dotted line in the 11-position is not a bond and X is chlorine, bromine or iodine which avoids an 11-hydroxylation step in the preparation of hydrocortisone.
    Type: Grant
    Filed: October 2, 1995
    Date of Patent: September 17, 1996
    Assignee: Roussel Uclaf
    Inventors: Francis Brion, Jean Buendia, Christian Diolez, Michel Vivat