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).
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Patent number: 5663164Abstract: 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: GrantFiled: April 27, 1995Date of Patent: September 2, 1997Assignee: Roussel UclafInventors: Jean-Georges Teutsch, Alain Bonnet, Jozsef Aszodi, Germain Costerousse, Solange Gouin d'Ambrieres
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Patent number: 5182381Abstract: 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: GrantFiled: September 10, 1991Date of Patent: January 26, 1993Assignee: Roussel UlcafInventors: Daniel Philibert, Jean G. Teutsch, Germain Costerousse, Roger Deraedt
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Patent number: 5064822Abstract: 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: GrantFiled: November 16, 1989Date of Patent: November 12, 1991Assignee: Roussel UclafInventors: Daniel Philibert, Jean G. Teutsch, Germain Costerousse, Roger Deraedt
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Patent number: 5043332Abstract: 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: GrantFiled: October 13, 1989Date of Patent: August 27, 1991Assignee: Roussel UclafInventors: Jean-Georges Teutsch, Vesperto Torelli, Roger Deraedt, Daniel Philibert, Germain Costerousse
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Patent number: 4978657Abstract: 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: GrantFiled: December 17, 1985Date of Patent: December 18, 1990Assignee: Roussel UclafInventors: Jean-Georges Teutsch, Vesperto Torelli, Roger Deraedt, Daniel Philibert, Germain Costerousse
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Patent number: 4908359Abstract: 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: GrantFiled: February 8, 1988Date of Patent: March 13, 1990Assignee: Roussel UclafInventors: Germain Costerousse, Solange Gouin d'Ambrieres, Jean-Georges Teutsch
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Patent number: 4753932Abstract: 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: GrantFiled: January 14, 1986Date of Patent: June 28, 1988Assignee: Roussel UclafInventors: Jean-Georges Teutsch, Germain Costerousse, Vesperto Torelli, Daniel Philibert
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Patent number: 4540686Abstract: Novel 3-keto-19-nor-.DELTA..sup.4,9 -steroids of the formula ##STR1## possessing a remarkable antiglucocorticoidal activity.Type: GrantFiled: June 8, 1984Date of Patent: September 10, 1985Assignee: Roussel UclafInventors: Daniel Philibert, Jean G. Teutsch, Germain Costerousse, Roger Deraedt
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Patent number: 4519946Abstract: 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: GrantFiled: May 25, 1984Date of Patent: May 28, 1985Assignee: Roussel UclafInventors: Jean G. Teutsch, Germain Costerousse, Daniel Philibert, Roger Deraedt
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Patent number: 4477445Abstract: Novel 3-keto-19-nor-.DELTA.Type: GrantFiled: February 23, 1983Date of Patent: October 16, 1984Assignee: Roussel UclafInventors: Daniel Philibert, Jean G. Teutsch, Germain Costerousse, Roger Deraedt
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Patent number: 4447424Abstract: 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: GrantFiled: June 10, 1982Date of Patent: May 8, 1984Assignee: Roussel UclafInventors: Jean G. Teutsch, Germain Costerousse, Daniel Philibert, Roger Deraedt
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Patent number: 4386085Abstract: 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: GrantFiled: January 8, 1982Date of Patent: May 31, 1983Assignee: Roussell UclafInventors: Jean G. Teutsch, Germain Costerousse, Daniel Philibert, Roger Deraedt
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Patent number: 4303654Abstract: 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: GrantFiled: October 9, 1980Date of Patent: December 1, 1981Assignee: Roussel UclafInventors: Roger Deraedt, Jean G. Teutsch, Germain Costerousse
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Patent number: 4257948Abstract: 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: GrantFiled: April 11, 1979Date of Patent: March 24, 1981Assignee: Roussel UclafInventors: Germain Costerousse, Jean G. Teutsch