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: 4990506
    Abstract: A compound which is a 3-(acylaminomethyl)imidazo[1,2-a]pyridine derivative of formula (I) ##STR1## in which R.sub.1 denotes hydrogen; linear or branched C.sub.1 -C.sub.4 alkyl; or benzyl;R.sub.2 denotes linear or branched C.sub.1 -C.sub.6 alkyl; cyclohexyl; trichloromethyl; 1-propenyl; allyl; phenyl; 4-chlorophenyl; or benzyl:or R.sub.1 and R.sub.2 together denote a C.sub.3 -C.sub.5 aliphatic chain:X denotes halogen; C.sub.1 -C.sub.3 alkyl; methylthio; trifluoromethyl; optionally esterified carboxy of formula --COOR in which R denotes hydrogen or C.sub.1 -C.sub.6 alkyl; cyano; optionally mono- or dialkylated aminocarbonyl of formula --CONR.sub.3 R.sub.4 in which R.sub.3 and R.sub.4 independently denote hydrogen or C.sub.1 -C.sub.4 alkyl or together denote a chain of formula --(CH.sub.2).sub.2 --Z--(CH.sub.2).sub.2 -- in which Z denotes a direct bond, oxygen, sulphur, or a divalent group of formula --CH.sub.2 --, --NH-- or --N(C.sub.1 -C.sub.4 alkyl)--; alkylamino of formula NHR.sub.5 in which R.sub.
    Type: Grant
    Filed: October 24, 1989
    Date of Patent: February 5, 1991
    Assignee: Synthelabo
    Inventors: Pascal George, Claudie Giron, Jacques Froissant
  • Patent number: 4977159
    Abstract: A compound which is a pyrido[3,4-b]derivative of formula (I) ##STR1## in which R is a hydrogen atom or an alkyl carbonyl, arylalkylcarbonyl or arylcarbonyl group of formula COR.sub.1 wherein R.sub.1 is a C.sub.1 -C.sub.6 alkyl group, a benzyl group or a phenyl group unsubstituted or substituted with 1 to 3 substituents chosen from halogen atoms and trifluoromethyl, C.sub.1 -C.sub.3 alkyl and C.sub.1 -C.sub.3 alkoxy groups or R is an alkoxycarbonyl or benzyloxycarbonyl group of formula COOR.sub.2 wherein R.sub.2 is a C.sub.1 -C.sub.6 alkyl group or a benzyl group, or R is a substituted aminocarbonyl group of formula CONHR.sub.3 wherein R.sub.3 is a C.sub.1 -C.sub.6 alkyl group or a phenyl group, or R is an arylsulphonyl group of formula SO.sub.2 R.sub.4 wherein R.sub.4 is a phenyl group, or a pharmacologically acceptable acid addition salt thereof useful for treating hypertension, depressive state or anxiety state.
    Type: Grant
    Filed: August 5, 1988
    Date of Patent: December 11, 1990
    Assignee: Synthelabo
    Inventors: Mireille Sevrin, Pascal George, Jacques Menin, Claude Morel, Dennis Bigg
  • Patent number: 4945096
    Abstract: A compound of formula (I) ##STR1## in which R is (a) a hydrogen atom;(b) a linear or branched (C.sub.1 -C.sub.6) alkyl group; an allyl group; a cycloalkylmethyl group in which the cycloalkyl moiety has from 3 to 6 carbon atoms; a phenylmethyl group unsubstituted or substituted with one to three substituents chosen from halogen atoms and trifluoromethyl, nitro, amino, dimethylamino, cyano, aminocarbonyl, linear or branched (C.sub.1 -C.sub.3) alkyl, liner or branched (C.sub.1 -C.sub.3) alkoxy and linear or branched (C.sub.1 -C.sub.3) alkylthio groups; a 2-phenylethyl group; a 3-phenylpropyl group; a 3-phenyl-2-propenyl group; a phenylcarbonylmethyl group; a naphthylmethyl group; a pyridylmethyl group; a furylmethyl group; or a thienylmethyl group; or(c) a linear or branched (C.sub.2 -C.sub.
    Type: Grant
    Filed: August 30, 1989
    Date of Patent: July 31, 1990
    Assignee: Synthelabo
    Inventors: Pascal George, Mireille Sevrin
  • Patent number: 4931449
    Abstract: A compound of formula (I) ##STR1## in which R is a benzyl, benzoyl, 3-chlorobenzoyl, 3-methylbenzoyl or (C.sub.1 -C.sub.6 alkoxy)carbonyl group, or a pharmacologically acceptable acid addition salt thereof.
    Type: Grant
    Filed: August 5, 1988
    Date of Patent: June 5, 1990
    Assignee: Synthelabo
    Inventors: Mireille Sevrin, Pascal George, Claude Morel
  • Patent number: 4925850
    Abstract: A compound of formula (I): ##STR1## in which: X is hydrogen or a methyl or methoxy group;Y is a halogen or a methyl or methoxy group; andR is a group of formula --Z--R' in which:Z is a --CH.sub.2 -- group, andR' is a phenyl group unsubstituted or substituted by one, two or three substituents selected from halogen atoms and trifluoromethyl, linear or branched (C.sub.1 -C.sub.3) alkyl and linear or branched (C.sub.1 -C.sub.3) alkoxy groups;or a pharmacologically acceptable acid addition salt thereof.
    Type: Grant
    Filed: February 6, 1989
    Date of Patent: May 15, 1990
    Assignee: Synthelabo
    Inventors: Pascal George, Mireille Sevrin, Christian Maloizel, Arlette Tixidre, Jacques Froissant
  • Patent number: 4904670
    Abstract: A compound of formula ##STR1## in which: X denotes hydrogen or a halogen, a C.sub.1 -C.sub.4 alkoxy group or a C.sub.1 -C.sub.6 alkyl group;Y denotes hydrogen or a methyl group;R.sub.1 denotes a C.sub.1 -C.sub.4 alkyl group; andR.sub.2 denotes a C.sub.1 -C.sub.6 alkyl group;or an addition salt thereof with a pharmacologically acceptable acid.
    Type: Grant
    Filed: May 19, 1988
    Date of Patent: February 27, 1990
    Assignee: Synthelabo
    Inventors: Pascal George, Claudie Giron
  • Patent number: 4891371
    Abstract: A compound which is a 3-(acylaminomethyl)imidazo[1,2-a]pyridine derivative of formula (I) ##STR1## in which R.sub.1 denotes hydrogen; linear or branched C.sub.1 -C.sub.4 alkyl; or benzyl:R.sub.2 denotes linear or branched C.sub.1 -C.sub.6 alkyl; cyclohexyl; trichloromethyl; 1-propenyl; allyl; phenyl; 4-chlorophenyl; or benzyl; or R.sub.1 and R.sub.2 together denote a C.sub.3 -C.sub.5 aliphatic chain:X denotes halogen; C.sub.1 -C.sub.3 alkyl; methylthio; trifluoromethyl; optionally esterified carboxy of formula --COOR in which R denotes hydrogen or C.sub.1 -C.sub.6 alkyl; cyano; optionally mono- or dialkylated aminocarbonyl of formula --CONR.sub.3 R.sub.4 in which R.sub.3 and R.sub.4 independently denote hydrogen or C.sub.1 -C.sub.4 alkyl or together denote a chain of formula --(CH.sub.2).sub.2 --Z--(CH.sub.2).sub.2 -- in which Z denotes a direct bond, oxygen, sulphur, or a divalent group of formula --CH.sub.2 --, --NH--or --N(C.sub.1 -C.sub.4 alkyl)--; alkylamino of formula NHR.sub.5 in which R.sub.
    Type: Grant
    Filed: June 10, 1988
    Date of Patent: January 2, 1990
    Assignee: Synthelabo
    Inventors: Pascal George, Claudie Giron, Jacques Froissant
  • Patent number: 4885302
    Abstract: A compound of formula (I) ##STR1## in which R is (a) a hydrogen atom;(b) a linear or branched (C.sub.1 -C.sub.6) alkyl group; an allyl group; a cycloalkylmethyl group in which the cycloalkyl moiety has from 3 to 6 carbon atoms; a phenylmethyl group unsubstituted or substituted with one to three substituents chosen from halogen atoms and trifluoromethyl, nitro, amino, dimethylamino, cyano, aminocarbonyl, linear or branched (C.sub.1 -C.sub.3) alkyl, linear or branched (C.sub.1 -C.sub.3) alkoxy and linear or branched (C.sub.1 -C.sub.3) alkylthio groups; a 2-phenylethyl group; a 3-phenylpropyl group; a 3-phenyl-2-propenyl group; a phenylcarbonylmethyl group; a naphthylmethyl group; a pyridylmethyl group; a furylmethyl group; or a thienylmethyl group; or(c) a linear or branched (C.sub.2 -C.sub.
    Type: Grant
    Filed: August 5, 1988
    Date of Patent: December 5, 1989
    Inventors: Pascal George, Mireille Sevrin, Christian Maloizel
  • Patent number: 4847263
    Abstract: Imidazo[1,2-a]pyridine derivatives of the general formula (I) ##STR1## wherein Y.sub.1 represents hydrogen, halogen or (C.sub.1-4) alkyl, Y.sub.2 represents --SR in which R is hydrogen, (C.sub.1-4) alkyl or (4-alkoxyphenyl)methyl or hydroxy or (C.sub.1-4) alkoxy, X represents hydrogen, halogen, (C.sub.1-4) alkoxy, (C.sub.1-4) alkyl, --CF.sub.3, --CH.sub.3 S, --NO.sub.2 or --NH.sub.2, and R.sub.1 and R2, which may be the same or different, represent hydrogen or (C.sub.1-4) alkyl have useful therapeutic properties.
    Type: Grant
    Filed: March 28, 1988
    Date of Patent: July 11, 1989
    Assignee: Synthelabo
    Inventors: Pascal George, John Allen, Guy Jaurand, Daniele De Peretti
  • Patent number: 4810711
    Abstract: A compound which is a 1-acylaminomethylimidazo[1,2-a]quinoline of formula (I) ##STR1## in which A and B both denote hydrogen or together denote a direct carbon-carbon bond,X denotes hydrogen or a halogen or a (C.sub.1-4)alkyl, (C.sub.1-4)alkoxy, (C.sub.1-4)alkylthio, methylsulphonyl, amino, (C.sub.1-4)alkylamino, di(C.sub.1-4)alkylamino, nitro or trifluormethyl group,Y denotes hydrogen or a halogen or a methyl group and is attached to the aryl ring at position 6, 7 or 8,R.sub.1 denotes hydrogen or a (C.sub.1-4)alkyl group, andR.sub.2 denotes a (C.sub.1-6)alkyl group, or a pharmaceutically acceptable acid addition salt thereof is useful in therapy.
    Type: Grant
    Filed: January 21, 1987
    Date of Patent: March 7, 1989
    Assignee: Synthelabo
    Inventors: Pascal George, Daniele De Peretti
  • Patent number: 4808594
    Abstract: An imidazopyridine of formula (I) ##STR1## in which: either X is CH.sub.3 and Y is CH.sub.2 OR,or, X is CH.sub.2 OR and Y is CH.sub.3,R is a C.sub.1-6 alkyl group,R.sub.1 is a C.sub.1-3 alkyl group, andR.sub.2 is a C.sub.1-3 alkyl group, has useful anxidytic and hypnotic properties.
    Type: Grant
    Filed: November 3, 1987
    Date of Patent: February 28, 1989
    Assignee: Synthelabo
    Inventors: Pascal George, John Allen
  • Patent number: 4767755
    Abstract: A compound which is a 3-(acylaminomethyl)imidazo[1,2-a]pyridine derivative of formula (I) ##STR1## or a pharmacologically acceptable acid addition salt is useful in therapy.
    Type: Grant
    Filed: February 4, 1987
    Date of Patent: August 30, 1988
    Assignee: Synthelabo
    Inventors: Pascal George, Claudie Giron, Jacques Froissant
  • Patent number: 4675323
    Abstract: Compounds which are imidazo[1,2-a]quinoline derivatives of general formula (I) ##STR1## in which X is hydrogen, halogen, (C.sub.1-4)alkyl, (C.sub.1-4)alkoxy, (C.sub.1-4) alkylthio, methylsulphonyl, amino, (C.sub.1-4)alkylamino, di-(C.sub.1-4)alkylamino, nitro or trifluoromethyl, Y is hydrogen, halogen or methyl in position 6, 7 or 8, R.sub.1 and R.sub.2, which may be the same or different, are hydrogen or (C.sub.1-6) alkyl, or R.sub.1 and R.sub.2 together form a tetramethylene, pentamethylene, 3-methyl-3-azapentamethylene, 3-ethoxycarbonyl-3-azapentamethylene group, and A and B both are hydrogen or together form a carbon-carbon bond, and their pharmacologically acceptable acid addition salts have anxiolytic, sleep-inducing, hypnotic, anticonvulsant, analgesic and anti-ulcer properties.
    Type: Grant
    Filed: February 7, 1986
    Date of Patent: June 23, 1987
    Assignee: Synthelabo
    Inventors: Pascal George, Danielle De Peretti
  • Patent number: 4650796
    Abstract: Compounds which are imidazo[1,2-a]pyridine derivatives of general formula (I) ##STR1## in which each of X.sub.1, X.sub.2, X.sub.3, independently of each other, is hydrogen, halogen, C.sub.1 -C.sub.4 alkyl, methoxy, methylthio, ethylthio, methylsulphonyl, nitro, amino, methylamino, dimethylamino, acetylamino or diacethylamino, Y is hydrogen, chlorine or methyl, R.sub.1 is hydrogen, C.sub.1 -C.sub.4 alkyl or benzyl, R.sub.2 is C.sub.1 -C.sub.6 alkyl, cyclohexyl, trichloromethyl, 1-propenyl, allyl, phenyl, 4-chlorophenyl or benzyl, or R.sub.1 and R.sub.2 together represent a divalent C.sub.3 -C.sub.5 alipathic group and their pharmaceutically acceptable acid salts have anxiolytic, sleep-inducing, hypnotic, anticonvulsant, analgesic and anti-ulcer properties.
    Type: Grant
    Filed: February 7, 1986
    Date of Patent: March 17, 1987
    Assignee: Synthelabo
    Inventors: Pascal George, Claude Giron
  • Patent number: 4501745
    Abstract: Imidazo[1,2-a]pyridine derivatives of the general formula: ##STR1## wherein n represents 2, 3 or 4, Y represents a hydrogen or halogen atom or a C.sub.1-4 alkyl radical, Z represents a naphthyl radical; a phenyl radical ##STR2## in which X.sub.1 and X.sub.2 independently of one another each represent a hydrogen or halogen atom, a C.sub.1-4 alkoxy radical, a C.sub.1-6 alkyl radical or the group --CF.sub.3, CH.sub.3 S--, CH.sub.3 SO.sub.2 -- or --NO.sub.2 ; or a thien-2-yl, furan-2-yl or pyridine-2-yl radical optionally carrying a halogen atom or the methyl or ethyl radical in the 5-position, and R represents the hydroxy radical, or a group --NR.sub.1 R.sub.2 in which R.sub.1 and R.sub.2 independently of one another each represent a hydrogen atom; a straight- or branched-chain C.sub.1-5 alkyl radical optionally carrying one or more halogen atoms, a hydroxy radical, a group --N(C.sub.1-4 alkyl).sub.2, a carbamoyl radical or a C.sub.1-4 alkoxy radical; the allyl radical; the propargyl radical; a C.sub.
    Type: Grant
    Filed: April 13, 1983
    Date of Patent: February 26, 1985
    Assignee: Synthelabo
    Inventors: Jean-Pierre Kaplan, Pascal George
  • Patent number: 4492695
    Abstract: An imidazo[1,2-a]pyridine derivative of the formula: ##STR1## wherein Y represents a hydrogen or halogen atom or a C.sub.1-4 alkyl radical, Z represents a furan-2-yl, thien-2-yl or pyridin-2-yl radical optionally carrying a halogen atom or a methyl or ethyl radical in the 5-position, and R represents the hydroxy radical, a C.sub.1-4 alkoxy radical or a group --NR.sub.1 R.sub.2 in which R.sub.1 and R.sub.2 independently of one another each represent a hydrogen atom; a straight- or branched-chain C.sub.1-5 alkyl radical optionally carrying one or more halogen atoms or a hydroxy radical, a group --N(C.sub.1-4 alkyl).sub.2, a carbamoyl radical or a C.sub.1-4 alkoxy radical; the allyl radical; the propargyl radical; a C.sub.3-6 cycloalkyl radical; the benzyl radical; or the phenyl radical, or alternatively --NR.sub.1 R.sub.
    Type: Grant
    Filed: April 13, 1983
    Date of Patent: January 8, 1985
    Assignee: Synthelabo
    Inventors: Jean-Pierre Kaplan, Pascal George, Jean-Michel Bernardon
  • Patent number: 4460592
    Abstract: 6-Methyl-2-(4-methylthiophenyl)-imidazo[1,2-a]-pyridine-3-N,N-dimethylaceta mide is provided, preferably in the form of a pharmaceutically acceptable salt, for example, 6-methyl-2-(4-methylthiophenyl)-imidazo[1,2-a]-pyridine-3-N,N-dimethylacet amide methylsulfate. Also provided is a method of providing a patient with a hypnotic effect which comprises administering to said patient a hynotically effective amount of the compound 6-methyl-2-(4-methylthiophenyl)-imidazo[1,2-a]-pyridine-3-N,N-dimethylacet amide or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: February 10, 1983
    Date of Patent: July 17, 1984
    Assignee: Synthelabo
    Inventors: Jean-Pierre Kaplan, Pascal George
  • Patent number: 4382938
    Abstract: Imidazo[1,2-a] pyridines of the formula: ##STR1## and their acid addition salts in which Y represents a hydrogen or halogen atom or a C.sub.1-4 alkyl radical, Z represents a naphthyl radical or a radical ##STR2## in which each of X.sub.1 and X.sub.2 independently of one another is a hydrogen or halogen atom, a C.sub.1-4 alkoxy radical, a C.sub.1-6 alkyl radical or CF.sub.3, CH.sub.3 S--, CH.sub.3 SO.sub.2 --, --NO.sub.2, --NH.sub.2 or --NHCOCH.sub.3, and each of R.sub.1 and R.sub.2 independently of one another represents a hydrogen atom, a straight or branched C.sub.1-5 alkyl radical which is unsubstituted or substituted by one or more halogen atoms or hydroxyl, --N(C.sub.1-4 alkyl).sub.2, carbamoyl or C.sub.1-4 alkoxy radicals, allyl, propargyl, a C.sub.3-6 cycloalkyl radical, benzyl, or phenyl, not both R.sub.1 and R.sub.2 being hydrogen, or --NR.sub.1 R.sub.
    Type: Grant
    Filed: October 21, 1981
    Date of Patent: May 10, 1983
    Assignee: Synthelabo
    Inventors: Jean-Pierre Kaplan, Pascal George