Patents by Inventor Germain Costerousse

Germain Costerousse 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).

  • Patent number: 5663164
    Abstract: Novel 1-dethia-2-thia-cephalosporanic acid derivatives of the formula ##STR1## wherein R is selected from the group consisting of ##STR2## Ra is an organic radical, R.sub.i and R.sub.j are individually selected from the group consisting of hydrogen, aliphatic, aromatic and heterocycle or taken together with the nitrogen atom to which they are attached form an optionally substituted cycle or R.sub.b NH--, R.sub.b is optionally substituted carbocyclic or heterocyclic aryl, R.sub.1 and --COM are as defined in the specification, R.sub.4 is hydrogen or methoxy, n.sub.2 is 0, 1 or 2 and their non-toxic, pharmaceutically acceptable acid addition salts in racemic or optically active form having antibiotic activity and their preparation and novel intermediates.
    Type: Grant
    Filed: April 27, 1995
    Date of Patent: September 2, 1997
    Assignee: Roussel Uclaf
    Inventors: Jean-Georges Teutsch, Alain Bonnet, Jozsef Aszodi, Germain Costerousse, Solange Gouin d'Ambrieres
  • Patent number: 5182381
    Abstract: Novel 3-keto-19-nor-.DELTA..sup.4,9 -steroids of the formula ##STR1## and their non-toxic, pharmaceutically acceptable acid addition salts possessing a remarkable antiglucocorticoidal activity.
    Type: Grant
    Filed: September 10, 1991
    Date of Patent: January 26, 1993
    Assignee: Roussel Ulcaf
    Inventors: Daniel Philibert, Jean G. Teutsch, Germain Costerousse, Roger Deraedt
  • Patent number: 5064822
    Abstract: Novel 3-keto-19-nor-.DELTA..sup.4,9 -steroids of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of naphthyl, phenylphenyl, alkyl of 1 to 6 carbon atoms, alkenyl of 2 to 6 carbon atoms optionally containing additional unsaturations, phenoxy, furyl, cycloalkyl of 3 to 6 carbon atoms, thienyl optionally substituted with at least one member of the group consisting of halogen and alkyl and haloalkyl of 1 to 6 carbon atoms and phenyl optionally substituted with at least one member of the group consisting of --OH, halogen, --CF.sub.3, alkyl and alkoxy of 1 to 6 carbon atoms, alkenyloxy of 2 to 6 carbon atoms, phenoxy and alkylthio of 1 to 6 carbon atoms optionally oxidized to the sulfoxide or sulfone, R.sub.2 is selected from the group consisting of methyl and ethyl, R.sub.
    Type: Grant
    Filed: November 16, 1989
    Date of Patent: November 12, 1991
    Assignee: Roussel Uclaf
    Inventors: Daniel Philibert, Jean G. Teutsch, Germain Costerousse, Roger Deraedt
  • Patent number: 5043332
    Abstract: 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: Grant
    Filed: October 13, 1989
    Date of Patent: August 27, 1991
    Assignee: Roussel Uclaf
    Inventors: Jean-Georges Teutsch, Vesperto Torelli, Roger Deraedt, Daniel Philibert, Germain Costerousse
  • Patent number: 4978657
    Abstract: 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: Grant
    Filed: December 17, 1985
    Date of Patent: December 18, 1990
    Assignee: Roussel Uclaf
    Inventors: Jean-Georges Teutsch, Vesperto Torelli, Roger Deraedt, Daniel Philibert, Germain Costerousse
  • Patent number: 4908359
    Abstract: 1-dethia-2-thia-cephalosporanic acids of the formula ##STR1## wherein R is selected from the group consisting of ##STR2## R.sub.b --NH--and ##STR3## R.sub.a is an organic radical R.sub.i and R.sub.j are individually selected from the group consisting of hydrogen, aliphatic, aromatic and heterocycle or taken together with the nitrogen atom form an optionally substituted heterocycle, R.sub.b is optionally substituted carbocyclic or heterocyclic aryl, R.sub.1B is --[CH.dbd.CH].sub.n1 --CH.sub.2 --S--R.sub.m, n.sub.1 is 0, 1 or 2, Rm is an unsaturated radical including a positively charged and doubly bonded nitrogen atom and bonded to the sulfur atom through a carbon atom, R.sub.4 is hydrogen or methoxy, n.sub.2 is 0, 1 or 2 and A is selected from the group consisting of hydrogen, alkali metal ion, or alkaline earth metal ion, magnesium ion, ammonium ion, an organic amine base and an ester group or --COOA is --COO.sup.
    Type: Grant
    Filed: February 8, 1988
    Date of Patent: March 13, 1990
    Assignee: Roussel Uclaf
    Inventors: Germain Costerousse, Solange Gouin d'Ambrieres, Jean-Georges Teutsch
  • Patent number: 4753932
    Abstract: 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: Grant
    Filed: January 14, 1986
    Date of Patent: June 28, 1988
    Assignee: Roussel Uclaf
    Inventors: Jean-Georges Teutsch, Germain Costerousse, Vesperto Torelli, Daniel Philibert
  • Patent number: 4540686
    Abstract: Novel 3-keto-19-nor-.DELTA..sup.4,9 -steroids of the formula ##STR1## possessing a remarkable antiglucocorticoidal activity.
    Type: Grant
    Filed: June 8, 1984
    Date of Patent: September 10, 1985
    Assignee: Roussel Uclaf
    Inventors: Daniel Philibert, Jean G. Teutsch, Germain Costerousse, Roger Deraedt
  • Patent number: 4519946
    Abstract: 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 carbons 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=A group at position 3 is selected from the group consisting of C-O, ketal, which may be open or closed ##STR2## --C.dbd.NOH,--C--NOAlK.sub.3 and C--CH.sub.2,AlK.sub.1, AlK.sub.2 and AlK.sub.3 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-glucocoritcoid activity and a process for their preparation.
    Type: Grant
    Filed: May 25, 1984
    Date of Patent: May 28, 1985
    Assignee: Roussel Uclaf
    Inventors: Jean G. Teutsch, Germain Costerousse, Daniel Philibert, Roger Deraedt
  • Patent number: 4477445
    Abstract: Novel 3-keto-19-nor-.DELTA.
    Type: Grant
    Filed: February 23, 1983
    Date of Patent: October 16, 1984
    Assignee: Roussel Uclaf
    Inventors: Daniel Philibert, Jean G. Teutsch, Germain Costerousse, Roger Deraedt
  • Patent number: 4447424
    Abstract: 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--O, ketal, which may be open or closed ##STR2## --C.dbd.NOH, --C--NOAlK.sub.3 and C--CH.sub.2, AlK.sub.1, AlK.sub.2 and AlK.sub.3 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: Grant
    Filed: June 10, 1982
    Date of Patent: May 8, 1984
    Assignee: Roussel Uclaf
    Inventors: Jean G. Teutsch, Germain Costerousse, Daniel Philibert, Roger Deraedt
  • Patent number: 4386085
    Abstract: 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, ##STR2## --C.dbd.NOH, --C.dbd.NOAlK.sub.3 and .dbd.CH.sub.2, AlK.sub.1, AlK.sub.2 and AlK.sub.3 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: Grant
    Filed: January 8, 1982
    Date of Patent: May 31, 1983
    Assignee: Roussell Uclaf
    Inventors: Jean G. Teutsch, Germain Costerousse, Daniel Philibert, Roger Deraedt
  • Patent number: 4303654
    Abstract: Novel 21-chloro-20-acetylenic steroids of the formula ##STR1## wherein R.sub.1 is alkyl of 1 to 3 carbon atoms, R is selected from the group consisting of hydrogen and acyl of an organic carboxylic acid of 1 to 18 carbon atoms, X is selected from the group consisting of hydrogen, chlorine, bromine and fluorine, Y is selected from the group consisting of hydrogen, fluorine and methyl and the dotted lines in the A and B rings are one or two optional double bonds in the 1(2) and 6(7) positions with the proviso that Y is not hydrogen when R.sub.1 is methyl, X is hydrogen, the A ring is saturated in the 1(2) position and the B ring is saturated having a remarkable anti-inflammatory activity and their preparation.
    Type: Grant
    Filed: October 9, 1980
    Date of Patent: December 1, 1981
    Assignee: Roussel Uclaf
    Inventors: Roger Deraedt, Jean G. Teutsch, Germain Costerousse
  • Patent number: 4257948
    Abstract: A novel epoxidation agent comprising hydrogen peroxide and hexachloroacetone and a novel process for epoxidizing an acyclic, cyclic or polycyclic compound containing at least one ethylenic unsaturation.
    Type: Grant
    Filed: April 11, 1979
    Date of Patent: March 24, 1981
    Assignee: Roussel Uclaf
    Inventors: Germain Costerousse, Jean G. Teutsch