Patents by Inventor Pascal George

Pascal George 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: 6075021
    Abstract: Compounds of general formula (I) ##STR1## in which the variables are as defined in the specification, their preparation and their application in therapeutics.
    Type: Grant
    Filed: April 7, 1999
    Date of Patent: June 13, 2000
    Assignee: Synthelabo
    Inventors: Yannick Evanno, Mireille Sevrin, Christian Maloizel, Odette Legalloudec, Pascal George
  • Patent number: 5929078
    Abstract: Compounds corresponding to the general formula (I): ##STR1## in which X represents a hydrogen atom, a hydroxyl group, a C.sub.1 -C.sub.3 alkoxy group or a cyclopropylmethoxy group and Y represents a hydrogen atom, a hydroxyl group or a methoxy group and salts and bases thereof. The compounds may exists in the form of a pure enantiomer or as a mixture of enantiomers. Additionally, the compounds of formula (I) are useful for the treatment of diseases associated with serotoninergic receptors, particularly anxiety and/or depression.
    Type: Grant
    Filed: February 3, 1998
    Date of Patent: July 27, 1999
    Assignee: Synthelabo
    Inventors: Pascal George, Mireille Sevrin, Philippe Manoury, Michel Peynot, Daniele De Peretti, Jean Fran.cedilla.ois Gibert, Arlette Tixidre, David Machnik
  • Patent number: 5922739
    Abstract: Compounds of general formula (I) ##STR1## in which R.sub.1 represents a hydrogen atom or a (C.sub.1 -C.sub.4)alkyl, (C.sub.3 -C.sub.6)cycloalkylmethyl or phenyl-(C.sub.1 -C.sub.3)alkyl group optionally substituted on the phenyl ring with one or more atoms or groups chosen from halogens and methyl, trifluoromethyl, methoxy and cyano groups, R.sub.2 represents a hydroxyl or alkoxy group or a group of general formula NR.sub.3 R.sub.4 in which R.sub.3 and R.sub.4 each represent a hydrogen atom, an alkyl group, a cycloalkyl group, a cycloalkylmethyl group, a phenyl group, a phenylmethyl group or a pyridyl group, or alternatively R.sub.3 and R.sub.4 form, together with the nitrogen atom, a pyrrolidine or piptzidine ring, and n represents the number 1, 2 or 3.Application in therapy.
    Type: Grant
    Filed: June 8, 1998
    Date of Patent: July 13, 1999
    Assignee: Synthelabo
    Inventors: Gihad Dargazanli, Yannick Evanno, Jonathan Frost, Patrick Lardenois, Mireille Sevrin, Pascal George
  • Patent number: 5663183
    Abstract: Compounds of the formula: ##STR1## in which R.sub.1 represents a hydrogen or halogen atom or a methyl or C.sub.1 -C.sub.4 alkoxy group, R'.sub.1 represents a hydrogen or halogen atom, R".sub.1 represents a hydrogen atom or a methoxy group, R.sub.3 represents a C.sub.1 -C.sub.3 alkyl group, R.sub.4 represents a 2,3-dihydro-1H-inden-2-yl, 2,3-dihydro-1H-inden-1-yl or 1,2,3,4-tetrahydronaphthalen-1-yl group, or R.sub.3 and R.sub.4 together form, with the adjacent nitrogen atom, a 1,2,3,4-tetrahydroisoquinol-2-yl, 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinol-2-yl, 5,8-dimethoxy-1,2,3,4-tetrahydroisoquinol-2-yl, 1,2,3,4-tetrahydro-9H-pyrido[3,4-b]indol-2-yl, 1,2,3,4-tetrahydro-9H-pyrido[4,3-b]indol-3-yl, 4,5,6,7-tetrahydrothieno[2,3-c]pyrid-6-yl, 2,3-dihydro-1H-isoindol-2-yl or 2,3,4,5-tetra-hydro-1H-3-benzazepin-3-yl, group are useful in the treatment of cerebral disorders.
    Type: Grant
    Filed: May 24, 1996
    Date of Patent: September 2, 1997
    Assignee: Synthelabo
    Inventors: Jonathan Frost, Pascal George, Patrick Pasau, Regine Bartsch, Corinne Rousselle, Paul Howard Williams, Jean Claude Muller
  • Patent number: 5652248
    Abstract: Eliprodil, or an enantiomer thereof, is indicated for combined administration with anticancer agents in order to prevent peripheral neuropathies induced by administration of the anticancer agents.
    Type: Grant
    Filed: October 24, 1994
    Date of Patent: July 29, 1997
    Assignee: Synthelabo
    Inventors: Delphine Lekieffre, Jesus Benavides, Bernard Scatton, Pascal George
  • Patent number: 5550125
    Abstract: Compounds of the general formula (I) ##STR1## wherein R.sub.1 represents a hydrogen, fluorine or chlorine atom or a methyl, C.sub.1 -C.sub.3 alkoxy or nitro group; R.sub.3 represents a hydrogen atom or a C.sub.1 -C.sub.3 alkyl group; R.sub.4 represents a 2,3-dihydro-1H-inden-2-yl, 2,3-dihydro-1H-inden-1-yl or 1,2,3,4-tetrahydronaphthalen-1-yl group; or alternatively R.sub.3 and R.sub.4 complete, with the nitrogen atom to which they are attached, a 1,2,3,4-tetrahydro-9H-pyrido[3,4-b]indol-2-yl, 1,2,3,4-tetrahydro-9H-pyrido[4,3-b]indol-3-yl, 4,5,6,7-tetrahydrothieno[2,3-c]pyrid-6-yl, 4,5,6,7-tetrahydrothieno[3,2-c]pyrid-6-yl or 2,3-dihydro-1H-isoindol-2-yl group; are useful for the treatment and prevention of cerebral disorders.
    Type: Grant
    Filed: February 2, 1995
    Date of Patent: August 27, 1996
    Assignee: Synthelabo
    Inventors: Pascal George, Jonathan Frost, Patrick Pasau, Corinne Rousselle, R egine Bartsch, Paul Howard Williams, Jean Claude Muller
  • Patent number: 5550162
    Abstract: Compounds of the formula: ##STR1## in which R.sub.1 represents a hydrogen or halogen atom or a methyl or C.sub.1 -C.sub.4 alkoxy group, R'.sub.1 represents a hydrogen or halogen atom, R".sub.1 represents a hydrogen atom or a methoxy group, R.sub.3 represents a C.sub.1 -C.sub.3 alkyl group, R.sub.4 represents a 2,3-dihydro-1H-inden-2-yl, 2,3-dihydro-1H-inden-1-yl or 1,2,3,4-tetrahydronaphthalen-1-yl group, or R.sub.3 and R.sub.4 together form, with the adjacent nitrogen atom, a 1,2,3,4-tetrahydroisoquinol-2-yl, 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinol-2-yl, 5,8-dimethoxy-1,2,3,4-tetrahydroisoquinol-2-yl, 1,2,3,4-tetrahydro-9H-pyrido[3,4-b]indol-2-yl, 1,2,3,4-tetrahydro-9H-pyrido[4,3-b]indol-3-yl, 4,5,6,7-tetrahydrothieno[2,3-c]pyrid-6-yl, 2,3-dihydro-1H-isoindol-2-yl or 2,3,4,5-tetra-hydro-1H-3-benzazepin-3-yl, group are useful in the treatment of cerebral disorders.
    Type: Grant
    Filed: February 20, 1995
    Date of Patent: August 27, 1996
    Assignee: SYNTHELABO
    Inventors: Jonathan Frost, Pascal George, Patrick Pasau, R egine Bartsch, Corinne Rousselle, Paul H. Williams, Jean C. Muller
  • Patent number: 5543421
    Abstract: Ifenprodil and its enantiomers are disclosed for the preparation of medicines useful for the treatment of peripheral neuropathies and chronic neurodegenerative diseases of the central nervous system.
    Type: Grant
    Filed: October 24, 1994
    Date of Patent: August 6, 1996
    Assignee: Synthelabo
    Inventors: J esus Benavides, Badia Ferzaz, Pascal George, Bernard Scatton
  • Patent number: 5530002
    Abstract: Compounds of formula: ##STR1## in which X represents a hydrogen atom, a C.sub.1 -C.sub.3 alkoxy group or a cyclopropylmethoxy group and Y represents a hydrogen atom or a methoxy group, are useful in the therapy of conditions.
    Type: Grant
    Filed: February 9, 1995
    Date of Patent: June 25, 1996
    Assignee: Synthelabo
    Inventors: Phillip Manoury, Daniel Obitz, Michel Peynot, Mireille Sevrin, Pascal George
  • Patent number: 5512590
    Abstract: The invention discloses compounds formula (I) ##STR1## in which n represents the number 1 or 2, X represents a hydrogen atom or indicates that the phenyl ring to which it is attached is substituted by one or two substituents independently chosen from halogen, C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy and hydroxyl, and R represents a hydrogen atom, a group of formula --CH.sub.2 --CO.sub.2 --R.sub.1 (in which R.sub.1 represents a hydrogen atom or a C.sub.1 -C.sub.6 alkyl group) or a group of formula --CH.sub.2 --CO--NR.sub.2 R.sub.3 (in which each of R.sub.2 and R.sub.3 is independently a hydrogen atom or a C.sub.1 -C.sub.3 alkyl group), or a pharmaceutically acceptable salt thereof, processes for their preparation and their use in the treatment of disorders of GABAergic transmission.
    Type: Grant
    Filed: May 9, 1995
    Date of Patent: April 30, 1996
    Assignee: Synthelabo
    Inventors: Pascal George, Mireille Sevrin, Michel Peynot
  • Patent number: 5466706
    Abstract: Compound corresponding to the formula: ##STR1## in which X represents one or more of hydrogen, halogen, alkyl, trifluoromethyl, alkoxy, alkylthio, methylsulphonyl, cyano, ethoxycarbonyl, aminocarbonyl and carboxy, Y represents one or more of hydrogen, halogens, alkyl, trifluoromethyl, methoxy and trifluoromethoxy, R.sub.1 represents hydrogen, alkyl, phenylmethyl, 2-phenylethyl, acetyl or alkoxycarbonyl, R.sub.2 and R.sub.3 each represent hydrogen, alkyl which is optionally substituted, prop-2-enyl, prop-2-ynyl, phenyl, 1-(phenylmethyl)piperidin-4-yl, or 1-[(cyclohexen-1-yl)methyl]piperidin-4-yl, or alternatively R.sub.2 and R.sub.3 form, with the nitrogen atom carrying them, an optionally substituted heterocycle. These compounds are useful as hypnotic, anxiolytic and anticonvulsant agents.
    Type: Grant
    Filed: January 14, 1994
    Date of Patent: November 14, 1995
    Assignee: Synthelabo
    Inventors: Pascal George, Danielle De Peretti, Jocelyne Roy, Jean-Paul Schmitt, Mireille Sevrin
  • Patent number: 5447928
    Abstract: Compounds of the formula ##STR1## in which Y represents hydrogen, fluorine, chlorine, methyl or methoxy, R.sub.1 represents phenyl substituted by fluorine, methyl, methoxy, trifluoromethyl or phenyl, or R.sub.1 represents 2-thienyl, R.sub.2 represents methyl, and R.sub.3 represents (C.sub.1 -C.sub.4)-alkyl, or phenyl-(C.sub.1 -C.sub.2)-alkyl optionally substituted on the ring by 2 to 3 methoxy groups, or 2-(2-pyridyl)ethyl, or R.sub.2 and R.sub.3 form, with the adjacent nitrogen, 4-phenyl(1-piperidyl), 4-phenylmethyl(1-piperidyl), 1,2,3,4-tetrahydro-2-isoquinolyl, 6-methoxy-1,2,3,4-tetrahydro-2-isoquinolyl, 5,8-dimethoxy-1,2,3,4-tetrahydro-2-isoquinolyl, 6,7-dimethoxy 1,2,3,4-tetrahydro-2-isoquinolyl, 2,3,4,5-tetrahydro-1H-3-benzazepin-3-yl, or 7,8-dimethoxy-2,3,4,5-tetrahydro-1H-3-benzazepin-3-yl, and X represents carbonyl or sulphonyl, and their salts are useful as neuroprotective and antiiischaemic agents.
    Type: Grant
    Filed: February 24, 1994
    Date of Patent: September 5, 1995
    Assignee: Synthelabo
    Inventors: Howard Williams, Lydia Zard, Thomas Purcell, Daniel Galtier, Jean-Claude Muller, Pascal George, Jonathan Frost, Patrick Pasau, Corinne Rousselle, Regine Bartsch
  • Patent number: 5420130
    Abstract: Compounds corresponding to the general formula (I) ##STR1## in which n represents 0 or 1, R.sub.1 represents a methyl group, in which case R.sub.2 represents a phenoxy(C.sub.1 -C.sub.4)alkyl group (in which the phenoxy group is optionally substituted), or else R.sub.1 and R.sub.2 together form, and with the nitrogen atom which carries them, a 4-(phenoxymethyl)piperid-1-yl group (in which the phenoxy group is optionally substituted) or a 4-phenylpiperazin-1-yl group (in which the phenyl group is optionally substituted), R.sub.3 represents a hydrogen atom or a methyl group, R.sub.4 represents a hydrogen atom and R.sub.5 represents a hydrogen atom or a group of general formula -CH.sub.2 -CH.sub.2 -NH-R.sub.6, R.sub.6 being a hydrogen atom or a tert-butyloxycarbonyl, 4-carbamoylpyrimidin-2-yl or 5-carbamoylpyrazin-2-yl group, are useful in the treatment of diseases and complaints involving hyperactivity of the .alpha.-adrenergic system at the level of the lower urinary apparatus.
    Type: Grant
    Filed: May 16, 1994
    Date of Patent: May 30, 1995
    Assignee: Synthelabo
    Inventors: Pascal George, Benoit Marabout, Jacques Froissant
  • Patent number: 5418248
    Abstract: Compounds of the formula: ##STR1## in which R.sub.1 represents a hydroxy group, a C.sub.1 -C.sub.4 alkoxy group or an amino group of general formula --NR.sub.4 R.sub.5 in which R.sub.4 and R.sub.5 each represent, independently of each other, a hydrogen atom, a straight or branched C.sub.1 -C.sub.4 alkyl group, an allyl group or a methoxyethyl group, or alternatively --NR.sub.4 R.sub.5 represents a heterocycle containing 3 to 6 carbon atoms,Y represents a thienyl group optionally substituted by an alkyl group, andX represents a hydrogen or halogen atom,are useful as anticonvulsants and auxiolytics.
    Type: Grant
    Filed: December 29, 1993
    Date of Patent: May 23, 1995
    Assignee: Synthelabo
    Inventors: Mireille Sevrin, Claude Morel, Michel Mangane, Pascal George
  • Patent number: 5330985
    Abstract: A compound which is a pyrimidine-4-carboxamide derivative of the general formula (I) ##STR1## in which n is 0 or 1, m is 0 or 1,R.sub.1 represents a methyl group whenR.sub.2 represents a phenoxy(C.sub.1 -C.sub.4)alkyl group (in which the phenoxy group optionally carries 1 or 2 substituents selected from halogen atoms and methoxy groups), orR.sub.1 and R.sub.2 form together with the nitrogen atom to which they are attached a 4-phenoxypiperidin-1-yl group (in which the phenoxy group optionally carries 1 or 2 substituents selected from halogen atoms and methoxy groups), a phenoxymethylpiperidin-1-yl group (in which the phenoxy group optionally carries 1 or 2 C.sub.1 -C.sub.4 alkyl groups) or a 4-phenylpiperazin-1-yl group (in which the phenyl group optionally carries 1 or 2 substituents selected from halogen atoms and methoxy groups), and R.sub.3 represents a hydrogen atom or only when n is 1 a hydroxyl group or a methoxy group, or is an addition salt thereof with an acid, is useful as an .alpha.
    Type: Grant
    Filed: July 1, 1993
    Date of Patent: July 19, 1994
    Assignee: Synthelabo
    Inventors: Pascal George, Benoit Marabout, Jacques Froissant, Jean Pierre Merly
  • Patent number: 5272157
    Abstract: Compounds of general formula (I) ##STR1## in which n is 1 or 2;R represents a linear or branched C.sub.1 -C.sub.3 -alkyl group; andX represents at least one substituent chosen from hydrogen, halogen, C.sub.1 -C.sub.3 -alkyl and C.sub.1 -C.sub.3 -alkoxy, in the form of a free base or an acid addition salt thereof, and their therapeutic application.
    Type: Grant
    Filed: November 17, 1992
    Date of Patent: December 21, 1993
    Assignee: Synthelabo
    Inventors: Pascal George, Jacques Froissant, Mireille Sevrin
  • Patent number: 5254560
    Abstract: A compound which is a carboxamide derivative of general formula (I) ##STR1## in which R represents a hydrogen atom, a methyl group or a phenoxyalkyl group of general formula ##STR2## in which X represents one or more substituents independently chosen from hydrogen, fluorine, chlorine, methyl, 1-methylethyl and methoxy andn is 2 or 3,m is 0 or 1 andp is 1 or 2 such that m+p=2q is 0 or 1, andR.sub.1 represents a hydrogen atom or a methyl group,or a pharmaceutically acceptable acid addition salt thereof. Process for their preparation and their therapeutic use.
    Type: Grant
    Filed: June 26, 1992
    Date of Patent: October 19, 1993
    Assignee: Synthelabo
    Inventors: Pascal George, Christian Maloizel, Benoit Marabout, Jean-Pierre Merly
  • Patent number: 5246939
    Abstract: A compound which is a 2-aminopyrimidine carboxamide derivative represented by formula (I) ##STR1## in which X represents hydrogen, fluorine, chlorine, methyl, 1-methylethyl or methoxy, with the proviso that more than one substituent X may be present in which case each X may be the same or different,n represents 2 or 3,m represents 1, in which case p represents 1, or elsem represents 0, in which case p represents 2,q represents 0 or 1, andR.sub.1 represents a hydrogen atom;or a pharmaceutically acceptable acid addition salt thereof.A compound of formula (I) has .alpha..sub.1 -adrenergic receptor antagonist activity and is useful as a therapeutic substance.
    Type: Grant
    Filed: June 26, 1992
    Date of Patent: September 21, 1993
    Assignee: Synthelabo
    Inventors: Pascal George, Christian Maloizel, Benoit Marabout, Jean-Pierre Merly
  • Patent number: 5244901
    Abstract: The present invention provides a compound which is a 4-pyrimidinecarboxamide derivative of general formula (I) ##STR1## in which X represents one or more substituents independently chosen from fluorine, chlorine, methoxy and cyclopropyl,R.sub.1 represents a hydrogen atom or a C.sub.1 -C.sub.3 alkyl group, andR.sub.2 represents a hydrogen atom or a methyl group, or a pharmaceutically acceptable acid addition salt thereof; their preparation and their application in therapy.
    Type: Grant
    Filed: June 26, 1992
    Date of Patent: September 14, 1993
    Assignee: Synthelabo
    Inventors: Pascal George, Jacques Froissant, Arlette Tixidre
  • Patent number: 5244894
    Abstract: Compounds corresponding to the general formula (I) ##STR1## in which n=2 or 3, X=H, F, Cl or OCH.sub.3, R=H or CH.sub.3, R.sub.1 =H or CH.sub.3, R.sub.2 =alkyl, hydroxyalkyl, (hydroxy)(methoxy)alkyl, dimethoxyalkyl, 2-(aminosulphonyl)ethyl, 2-(methylsulphonyl)ethyl, 2-(methylsulphonylamino)ethyl, aminocarbonylmethyl which is optionally substituted by nitrogen, phenylethyl which is optionally substituted, pyrimidinylaminoalkyl or arylcaronylaminoalkyl, or else R.sub.1 and R.sub.2 form, with the nitrogen which carries them, a piperidine, morpholine, thiomorpholine or piperazine ring, optionally substituted by nitrogen. Use in therapeutics.
    Type: Grant
    Filed: June 26, 1992
    Date of Patent: September 14, 1993
    Assignee: Synthelabo
    Inventors: Pascal George, Philippe Manoury, Benoit Marabout, Jacques Froissant, Jean-Pierre Merly