Patents by Inventor Francis Barth

Francis Barth 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).

  • Publication number: 20060089345
    Abstract: The present invention provides compounds of formula: and also provides their preparation and the pharmaceutical compositions comprising them. These compounds are ligands of CB2 cannabinoid receptors.
    Type: Application
    Filed: May 15, 2003
    Publication date: April 27, 2006
    Inventors: Francis Barth, Carole Guillaumont, Murielle Rinaldi-Carmona, Claude Vernhet
  • Patent number: 6995184
    Abstract: A subject-matter of the present invention is compounds of formula: and their preparation and the pharmaceutical compositions comprising them. These compounds are agonists for CB2 cannabinoid receptors.
    Type: Grant
    Filed: November 21, 2001
    Date of Patent: February 7, 2006
    Assignee: Sanofi-Aventis
    Inventors: Francis Barth, Christian Congy, Carole Guillaumont, Murielle Rinaldi, Fabienne Vasse, Claude Vernhet
  • Publication number: 20050288356
    Abstract: The invention relates to derivatives of indole-3-carboxamide having general formula (I): wherein: R1 represents a C3-C10 alkyl, a C5-C10 carbocyclic radical that is unsubstituted or substituted one or more times with a methyl group; R2 represents a hydrogen atom or a (C1-C4)alkyl group; R3 represents a halogen atom or a (C1-C4)alkyl group; R4 represents a hydrogen or halogen atom or a (C1-C4)alkyl group; R5 represents a (C1-C4)alkyl group or a trifluoromethyl; X represents a sulfur atom, an —NHSO2— group or an —SO2— group; and n is equal to 2 or 3. The invention also relates to a method of preparing the aforementioned derivatives and to the application of same in therapeutics.
    Type: Application
    Filed: May 26, 2005
    Publication date: December 29, 2005
    Applicant: Sanofi-Aventis
    Inventors: Francis Barth, Mireille Rinaldi-Carmona, Claude Vernhet
  • Patent number: 6979683
    Abstract: The invention relates to benzimidazole derivatives of general formula (I) in which X represents a nitrogen atom or a carbon atom; and when X represents a nitrogen atom R3 represents in particular a hydrogen atom or a (C1-C4)alkyl group, R4 represents in particular a hydrogen atom; a (C1-C6)alkyl; (C3-C7)cycloalkyl; 4-piperidyl; —(CH2)p—NR5R6; —(CH2)p—CONR5R6; —CO—(CH2)p—NR5R6; —(CH2)p-phenyl; —(CH2)p-morpholinyl; —(CH2)p-pyrrolidinyl; —(CH2)p-tetrahydroisoquinoline; —(CH2)p-heteroaryl; heteroarylcarbonyl; phenylcarbonyl; (C1-C6)alkylcarbonyl; —(CH2)p—COOR?; or phenylsulphonyl group; and when X represents a carbon atom R3 represents a hydrogen atom; a group —NR5R6; —NHCOR7; —CONHR5; —COR7; —NHCONH2; —OH or —CH2OH, R4 represents in particular a hydrogen atom; an optionally substituted group —(CH2)p-phenyl; a group —(CH2)p-heteroaryl; or a group —(CH2)tNR7R8. Preparation process and therapeutic application.
    Type: Grant
    Filed: November 21, 2001
    Date of Patent: December 27, 2005
    Assignee: Sanofi-Synthelabo
    Inventors: Francis Barth, Daniel Bichon, Frank Bolkenius, Viviane Van Dorsselaer
  • Publication number: 20050192332
    Abstract: The subject of the invention is tricyclic derivatives of pyrazolecarboxylic acid of formula: in which R1 represents a C3-C15 carboxyl radical or an NR2R3 group. The invention also relates to the method for preparing the compounds of formula (I), pharmaceutical compositions containing them. The compounds of formula (I) are active on cannabinoid CB1 receptors.
    Type: Application
    Filed: April 29, 2005
    Publication date: September 1, 2005
    Applicant: Sanofi-Aventis
    Inventors: Francis Barth, Christian Congy, Serge Martinez, Murielle Rinaldi
  • Patent number: 6916838
    Abstract: Tricyclic derivatives of 1-benzylpyrazole-3-carboxylic acid which are antagonists of the cannabinoid CB2 receptors; their method of preparation and pharmaceutical compositions containing them.
    Type: Grant
    Filed: November 2, 2000
    Date of Patent: July 12, 2005
    Assignee: Sanofi-Aventis
    Inventors: Francis Barth, Joseph Millan, Didier Oustric, Murielle Rinaldi, Martine Vernhet
  • Patent number: 6906080
    Abstract: The subject of the invention is tricyclic derivatives of pyrazolecarboxylic acid of formula: in which R1 represents a C3-C15 carboxyl radical or an NR2R3 group. The invention also relates to the method for preparing the compounds of formula (I), pharmaceutical compositions containing them. The compounds of formula (I) are active on cannabinoid CB1 receptors.
    Type: Grant
    Filed: November 2, 2000
    Date of Patent: June 14, 2005
    Assignee: Sanofi-Aventis
    Inventors: Francis Barth, Christian Congy, Serge Martinez, Murielle Rinaldi
  • Publication number: 20050032779
    Abstract: The invention relates to benzimidazole derivatives of general formula in which X represents a nitrogen atom or a carbon atom; and when X represents a nitrogen atom: R3 represents a hydrogen atom or a C1-C4 alkyl group, or does not exist, to give the compounds of formula (I) comprising a secondary or tertiary amine; R4 represents a hydrogen atom or a C1-C6 alkyl, C3-C7 cycloalkyl, optionally substituted C3-C7 heterocycloalkyl, —(CH2)p-heteroaryl, heteroaryl-carbonyl, phenylcarbonyl, (C1-C6)alkylcarbonyl, —(CH2)pCOOR, optionally substituted phenylsulphonyl or optionally substituted —(CH2)p-phenyl group, and, when X represents a carbon atom: R3 represents a hydrogen atom or a group —NR5R6, —N(R5)3+, —NHCOR7, —CONHR5, —COR7, —NHCONH2, —OH or —CH2OH, R4 represents a hydrogen atom or an optionally substituted —(CH2)p-phenyl, —(CH2)p-heteroaryl or —(CH2)tNR7R8 group. Preparation process and therapeutic application.
    Type: Application
    Filed: September 13, 2004
    Publication date: February 10, 2005
    Inventors: Francis Barth, Daniel Bichon, Frank Bolkenius, Viviane Van Dorsselaer
  • Patent number: 6794382
    Abstract: The invention relates to benzimidazole derivatives of general formula in which X represents a nitrogen atom or a carbon atom; and when X represents a nitrogen atom: R3 represents a hydrogen atom or a C1-C4 alkyl group, or does not exist, to give the compounds of formula (I) comprising a secondary or tertiary amine; R4 represents a hydrogen atom or a C1-C6 alkyl, C3-C7 cycloalkyl, optionally substituted C3-C7 heterocycloalkyl, —(CH2)p-heteroaryl, heteroaryl-carbonyl, phenylcarbonyl, (C1-C6)alkylcarbonyl, —(CH2)pCOOR, optionally substituted phenylsulphonyl or optionally substituted —(CH2)p-phenyl group, and, when X represents a carbon atom: R3 represents a hydrogen atom or a group —NR5R6, —N(R5)3+, —NHCOR7, —CONHR5, —COR7, —NHCONH2, —OH or —CH2OH, R4 represents a hydrogen atom or an optionally substituted —(CH2)p-phenyl, —(CH2)p-heteroaryl or —(CH2)tNR7R8 group.
    Type: Grant
    Filed: January 30, 2003
    Date of Patent: September 21, 2004
    Assignee: Sanofi-Synthelabo
    Inventors: Francis Barth, Daniel Bichon, Frank Bolkenius, Viviane Van Dorsselaer
  • Publication number: 20040039024
    Abstract: N-Piperidino-5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-ethylpyrazole-3-carboxamide and its salts and solvates are powerful antagonists of the CB1 cannabinoid receptors. They are prepared by reacting a functional derivative of 5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-ethylpyrazole-3-carboxylic acid with 1-aminopiperidine, optionally followed by salification.
    Type: Application
    Filed: June 5, 2003
    Publication date: February 26, 2004
    Inventors: Francis Barth, Philippe Camus, Serge Martinez, Murielle Rinaldi
  • Publication number: 20040034090
    Abstract: A subject-matter of the present invention is compounds of formula: 1
    Type: Application
    Filed: May 13, 2003
    Publication date: February 19, 2004
    Inventors: Francis Barth, Christian Congy, Carole Guillaumont, Murielle Rinaldi, Fabienne Vasse, Claude Vernhet
  • Publication number: 20040029866
    Abstract: The invention relates to benzimidazole derivatives of general formula (I) 1
    Type: Application
    Filed: May 23, 2003
    Publication date: February 12, 2004
    Inventors: Francis Barth, Daniel Bichon, Frank Bolkenius, Viviane Van Dorsselaer
  • Patent number: 6645985
    Abstract: N-Piperidino-5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-ethylpyrazole -3-carboxamide and its salts and solvates are powerful antagonists of the CB1 cannabinoid receptors. They are prepared by reacting a functional derivative of 5-(4-bromophenyl)-1-(2,4-dichlorophenyl) -4-ethylpyrazole-3-carboxylic acid with 1-aminopiperidine, optionally followed by salification.
    Type: Grant
    Filed: June 7, 2002
    Date of Patent: November 11, 2003
    Inventors: Francis Barth, Philippe Camus, Serge Martinez, Murielle Rinaldi
  • Publication number: 20030203893
    Abstract: The invention relates to benzimidazole derivatives of general formula 1
    Type: Application
    Filed: January 30, 2003
    Publication date: October 30, 2003
    Inventors: Francis Barth, Daniel Bichon, Frank Bolkenius, Viviane Van Dorsselaer
  • Publication number: 20020188007
    Abstract: N-Piperidino-5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-ethylpyrazole-3-carboxamide and its salts and solvates are powerful antagonists of the CB1 cannabinoid receptors. They are prepared by reacting a functional derivative of 5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-ethylpyrazole-3-carboxylic acid with 1-aminopiperidine, optionally followed by salification.
    Type: Application
    Filed: June 7, 2002
    Publication date: December 12, 2002
    Inventors: Francis Barth, Philippe Camus, Serge Martinez, Murielle Rinaldi
  • Patent number: 6432984
    Abstract: N-Piperidino-5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-ethylpyrazole-3-carboxamide and its salts and solvates are powerful antagonists of the CB1 cannabinoid receptors. They are prepared by reacting a functional derivative of 5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-ethylpyrazole-3-carboxylic acid with 1-aminopiperidine, optionally followed by salification.
    Type: Grant
    Filed: July 27, 2001
    Date of Patent: August 13, 2002
    Assignee: Sanofi-Synthelabo
    Inventors: Francis Barth, Philippe Camus, Serge Martinez, Murielle Rinaldi
  • Patent number: 6028084
    Abstract: Compounds of formula (I), wherein R.sub.1 is fluorine, hydroxy, (C.sub.1-5) alkoxy, (C.sub.1-5) alkylthio, hydroxy(C.sub.1-5)alkoxy, a -NR.sub.10 R.sub.11, group, cyano, (C.sub.1-5) alkyl-sulphonyl or (C.sub.1-5) alkylsulphinyl; R.sub.2 and R.sub.3 are each (C,.sub.4) alkyl or, taken together with the nitrogen atom to which they are attached, form a saturated or unsaturated 5- to 10-membered heterocyclic radical optionally substituted one or more times by (C.sub.1-3) alkyl or (C.sub.1-3) alkoxy; each of R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8 and R.sub.9 is independently hydrogen, halogen or trifluoromethyl, and when R.sub.1 is fluorine, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8 and/or R.sub.9 may also be fluoromethyl; with the proviso that at least one of substituents R.sub.4 or R.sub.7. is other than hydrogen; each of R.sub.10 and R.sub.11 is independently hydrogen or (C.sub.1-5) alkyl, or R.sub.10 and R.sub.
    Type: Grant
    Filed: May 19, 1998
    Date of Patent: February 22, 2000
    Assignee: Sanofi-Synthelabo
    Inventors: Francis Barth, Christian Congy, Serge Martinez, Murielle Rinaldi
  • Patent number: 6013648
    Abstract: The use of human CB.sub.2 receptor-specific agonists of formula (I) or (I') for preparing immunomodulating drugs is disclosed. In formulae (I) and (I'), R.sub.1 is a group selected from --CH.sub.2 CHR.sub.10 NR.sub.6 R.sub.11, --(CH.sub.2).sub.2 NR'.sub.6 R'.sub.11, --CHR.sub.9 CH.sub.2 NR'.sub.6 R'.sub.11, --(CH.sub.2).sub.n Z and --COR.sub.8 ; R'.sub.1 is a --CH.sub.2 CHR.sub.10 NR.sub.6 R.sub.11 or --(CH.sub.2).sub.2 NR'.sub.6 R'.sub.11 group; R.sub.2 and R'.sub.2 are hydrogen, halogen or C.sub.1-4 alkyl; R.sub.3 is hydrogen, C.sub.1-4 alkyl or a group selected from --CH.sub.2 CHR.sub.10 NR.sub.6 R.sub.11, --(CH.sub.2).sub.2 NR'.sub.6 R'.sub.11 and --COR.sub.8 ; R'.sub.3 is a .dbd.CR.sub.6 R.sub.8 group; R.sub.4 has one of the meanings given for R.sub.5 or is a --COR.sub.8 group; R.sub.5 is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, a halogen atom, a CF.sub.3 group, an OCF.sub.3 group or C.sub.1-4 alkylthio; R'.sub.5 has one of the meanings given for R.sub.
    Type: Grant
    Filed: December 22, 1997
    Date of Patent: January 11, 2000
    Assignee: Sanofi
    Inventors: Murielle Rinaldi, Francis Barth, Pierre Casellas, Christian Congy, Didier Oustric, Malcolm R. Bell, Thomas E. D'Ambra, Richard E. Philion
  • Patent number: 5925768
    Abstract: The present invention relates to compounds of the formula ##STR1## in which: X.sub.1 is a group --NR.sub.1 R.sub.2 or a group --OR.sub.2 ;g.sub.2, g.sub.3, g.sub.4, g.sub.5, g.sub.6 and w.sub.2, w.sub.3, w.sub.4, w.sub.5, w.sub.6 are identical or different and are each independently hydrogen, a halogen atom, a (C.sub.1 -C.sub.4)alkyl, a (C.sub.1 -C.sub.4)alkoxy, a trifluoromethyl, a nitro or a (C.sub.1 -C.sub.4)alkylthio, with the proviso that at least one of the substituents g.sub.2, g.sub.3, g.sub.4, g.sub.5, g.sub.6 and at least one of the substituents w.sub.2, w.sub.3, w.sub.4, w.sub.5, w.sub.6 are other than hydrogen;R.sub.1 is hydrogen or a (C.sub.1 -C.sub.4)alkyl;R.sub.2 is a non-aromatic (C.sub.3 -C.sub.15)carbocyclic radical which is unsubstituted or monosubstituted or polysubstituted by a substituent selected from a halogen atom, a (C.sub.1 -C.sub.4)alkyl and a (C.sub.1 -C.sub.4)alkoxy;R.sub.3 is hydrogen or a group --CH.sub.2 R.sub.6 ; andR.sub.4 and R.sub.5 are each independently a hydrogen, a (C.
    Type: Grant
    Filed: June 3, 1998
    Date of Patent: July 20, 1999
    Assignee: Sanofi
    Inventors: Francis Barth, Pierre Casellas, Joseph Millan, Didier Oustric, Murielle Rinaldi, Martine Sarran
  • Patent number: 5624941
    Abstract: The present invention relates to compounds of the formula: ##STR1## These compounds are useful in pharmaceuticals in which cannabis is known to be involved.
    Type: Grant
    Filed: November 29, 1994
    Date of Patent: April 29, 1997
    Assignee: Sanofi
    Inventors: Francis Barth, Pierre Casellas, Christian Congy, Serge Martinez, Murielle Rinaldi, Gilles Anne-Archard