Patents Assigned to Synthelabo
  • Patent number: 5620990
    Abstract: The present invention provides a piperidine derivative of formula (I) ##STR1## in which R represents a straight- or branched-chain (C.sub.1 -C.sub.19)alkyl group, a straight- or branched-chain (C.sub.2 -C.sub.19)alkenyl group, a (C.sub.3 -C.sub.6)cycloalkyl group, a cycloalkylmethyl group in which the cycloalkyl moiety has from three to six carbon atoms, a phenyl group which is optionally substituted by a halogen atom or a phenyl methyl group which is optionally substituted by a halogen atom, or an addition salt thereof, in the form of an optically pure enantiomer or of a mixture of enantiomers, a process for making them and their therapeutic application.
    Type: Grant
    Filed: July 11, 1995
    Date of Patent: April 15, 1997
    Assignee: Synthelabo
    Inventors: Jean P. Thenot, Jonathan Frost, Patrick Lardenois, Maria C. Renones, Alexander Wick
  • Patent number: 5614517
    Abstract: A compound of formula (I) ##STR1## wherein X is hydrogen, halogen, C.sub.1 -C.sub.3 alkyl, trifluoromethyl, or C.sub.1 -C.sub.3 alkoxy;Y is hydrogen, halogen, C.sub.1 -C.sub.3 alkyl, or C.sub.1 -C.sub.3 alkoxy;R is hydroxyl, methoxy, or amine; or a pharmaceutically acceptable acid addition salt thereof, useful for treating various neurological conditions.
    Type: Grant
    Filed: December 28, 1995
    Date of Patent: March 25, 1997
    Assignee: Synthelabo
    Inventors: Benoit Marabout, Mireille Sevrin, Jacques Froissant, Emmanuelle Dachary
  • Patent number: 5602149
    Abstract: The present invention provides a compound of formula (I) ##STR1## in which R.sub.1 represents a hydrogen atom or a (C.sub.1 -C.sub.4)alkyl group, R.sub.2 represents a hydrogen atom or a straight or branched (C.sub.1 -C.sub.4)alkyl group, R.sub.3 represents a straight or branched (C.sub.1 -C.sub.7)alkyl group, a group --(CH.sub.2).sub.n OCH.sub.3 (where n is 1, 2 or 3) or a group --CH.sub.2 O(C.sub.2 H.sub.4 O).sub.m CH.sub.3 (where m is 1, 2 or 3), R.sub.4 represents a hydrogen atom or a halogen atom, R.sub.5 represents a straight or branched (C.sub.1 -C.sub.4)alkyl group and A represents phenyl or heterocyclic group optionally substituted with one or more substituents independently chosen from halogen atoms and straight or branched (C.sub.1 -C.sub.4)alkyl, straight or branched (C.sub.1 -C.sub.4)alkoxy and trifluoromethyl groups, or a cyclo(C.sub.5 -C.sub.
    Type: Grant
    Filed: December 22, 1995
    Date of Patent: February 11, 1997
    Assignee: Synthelabo
    Inventors: Jean Michel Altenburger, Gilbert Lassalle
  • Patent number: 5589190
    Abstract: Pharmaceutical compositions which comprises a core comprising alfuzosin hydrochloride which core is coated with a coating whose dissolution is pH-dependent and applications to the preparation of sustained-release dosage compositions which are unable for a once-daily oral administration.
    Type: Grant
    Filed: March 20, 1995
    Date of Patent: December 31, 1996
    Assignee: Synthelabo
    Inventors: Veronique Andrieu, Jean Montel, Alexander Wick
  • Patent number: 5589476
    Abstract: A compound of formula (I): ##STR1## in which R.sub.1 represents a hydrogen atom or a straight or branched (C.sub.1 -C.sub.4)alkyl group; andA represents a 5,6-dihydro-4H-imidazo[4,5,1-ij]quinol-2-yl group, a 4,5-dihydroimidazo[1,5,4-de][1,4]benzoxazin-2-yl group, a 4-methyl-4,5-dihydroimidazo[1,5,4-de][1,4]benzoxazin-2-yl group, a 4-phenyl-4,5-dihydroimidazo[1,5,4-de][1,4]benzoxazin-2-yl group, a 4-phenylmethyl-4,5-dihydroimidazo[1,5,4-de][1,4]benzoxazin-2-yl group, a 5-methyl-4,5-dihydroimidazo[1,5,4-de][1,4]benzoxazin-2-yl group, a 5,6-dihydro-4H-imidazo[1,5,4-de]quinoxalin-2-yl group, a 6-oxo-5,6-dihydro-4H-imidazo[4,5,1-ij]quinol-2-yl group, or a 5-methyl-4,5,6,7-tetrahydroimidazo[4,5,1-jk][1,4]benzodiazepin-2-yl group which may be unsubstituted or substituted in the 6-position by a phenylmethyl group;or an addition salt thereof with a pharmaceutically acceptable acid.
    Type: Grant
    Filed: October 3, 1994
    Date of Patent: December 31, 1996
    Assignee: Synthelabo
    Inventors: Samir Jegham, G erard Defosse, Thomas A. Purcell, Luc Even
  • Patent number: 5585498
    Abstract: Compounds of formula (I) ##STR1## wherein R.sub.1 represents either a hydrogen atom, or a (C.sub.1 -C.sub.4)alkyl group,X represents either a sulphur atom, an oxygen atom or a methylene group,Z.sub.1 represents either a hydrogen atom, or a 1,1-dimethylethyl group,Z.sub.2 represents either a hydrogen atom, a triphenylmethyl group, or a phenylmethoxycarbonyl group, andn=1 or 2,and addition salts to inorganic or organic acids thereof as synthetic intermediates.
    Type: Grant
    Filed: November 5, 1993
    Date of Patent: December 17, 1996
    Assignee: Synthelabo
    Inventors: Gilbert Lassalle, Thomas Purcell, Daniel Galtier, Paul H. Williams, Fr ed eric Galli
  • Patent number: 5583113
    Abstract: A method for inducing thrombolysis, which method comprises administering to a patient a thrombolytically effective amount of a thrombin inhibitor which acts at the active site of thrombin, in the absence of exogenous plasminogen activator. The inhibitor is preferably argatroban, D-Phe-Pro-Arg-chloromethyl ketone, or Ac-(D-Phe)-Pro-boro-Arg-OH.
    Type: Grant
    Filed: February 13, 1995
    Date of Patent: December 10, 1996
    Assignee: Synthelabo
    Inventors: Christopher Berry, Patrice Ferrari
  • Patent number: 5552410
    Abstract: Compounds of the formula: ##STR1## in which R represents a chlorine atom or a hydroxyl group and R.sub.4 represents a (C.sub.1 -C.sub.4)alkyl group in the R or S form are useful as synthetic intermediates.
    Type: Grant
    Filed: September 14, 1994
    Date of Patent: September 3, 1996
    Assignee: Synthelabo
    Inventors: Daniel Galtier, Gilbert Lassalle
  • 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: 5547963
    Abstract: Use of eliprodil and its enantiomers for the preparation of medicines useful for the treatment of peripheral nouropathies and chronic neurodegenerative diseases of the central nervous system.
    Type: Grant
    Filed: July 28, 1995
    Date of Patent: August 20, 1996
    Assignee: Synthelabo
    Inventors: Philippe Poindron, Serge Braun, Badia Ferzaz
  • Patent number: 5545738
    Abstract: Alfuzosin hydrochloride is stabilized as alfuzosin hydrochloride dihydrate, which is useful for the production of antihypertensive agents or dysuria curing agents.
    Type: Grant
    Filed: December 27, 1994
    Date of Patent: August 13, 1996
    Assignee: Synthelabo
    Inventors: Regis Borrega, Satoshi Kitamura
  • Patent number: 5543526
    Abstract: A compound of formula (I) ##STR1## in which R.sub.3 and R.sub.4 together represent the residue of a dihydroxy compound, andR.sub.5 represents a hydrogen atom or a (C.sub.1 -C.sub.4) alkyl group, or a salt thereof, and its use as a synthetic intermediate.
    Type: Grant
    Filed: April 11, 1995
    Date of Patent: August 6, 1996
    Assignee: Synthelabo
    Inventors: Sergio Mallart, Gilbert Lassalle, Thomas Andrew Purcell, Jean Claude 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: 5525619
    Abstract: 1,3,4-Oxadiazol-2(3H)-one derivatives, of formula ##STR1## in which R.sub.1 represents either a hydrogen atom or a linear or branched (C.sub.1-4)alkyl group which is substituted with a hydroxyl group, a phenoxy group, a (C.sub.1-4)alkoxy group, a (C.sub.1-4)alkylthio group, a mercapto group, a (C.sub.1-4)alkoxy-(C.sub.1-4)alkoxy group, a di(C.sub.1-4)alkylamino group or an N-(C.sub.1-4)alkyl-N-propynylamino group, or represents a (C.sub.3-4)alkynyl group, andR.sub.2 either represents a linear or branched (C.sub.1-8)alkyl group which is substituted with one or more halogen atoms and/or a hydroxyl group, a 1-imidazolyl group or a 3-tetrahydropyranyl group, or represents a trifluoro(C.sub.3-5)alkenyl group,in the form of pure enantiomers or mixtures of enantiomers, including racemic mixtures, as well as the addition salts thereof with pharmaceutically acceptable acids, are useful as inhibitors of monoamine oxidase B.
    Type: Grant
    Filed: November 23, 1994
    Date of Patent: June 11, 1996
    Assignee: Synthelabo
    Inventors: Jean-Jacques Koenig, Samir Jegham, Frederic Puech, Philippe Burnier
  • Patent number: 5523094
    Abstract: A pharmaceutical preparation intended for transdermal administration contains alfusozin [(N-[3-[(4-amino-6,7-dimethoxy-2-quinazolinyl)methylamino]propyl]tetrahydr o-2-furancarboxamide] or a salt thereof and a mixture composed of water, at least one organic solvent and at least one absorption promoter.
    Type: Grant
    Filed: July 20, 1994
    Date of Patent: June 4, 1996
    Assignee: Synthelabo
    Inventors: Veronique Andrieu, Louis Henrion, Jean Montel, Alexander Wick
  • Patent number: 5514178
    Abstract: A prothesis intended to be introduced into a bodily canal which includes a flexible tube for preserving the normal passage cross section of the bodily canal and a holding device for immobilizing the flexible tube in position in the canal. The holding device is a tubular structure and is radially deformable so that it can pass from a first state in which its cross section is at most equal to that of the bodily canal into which it is to be introduced to a second state in which its cross section is such that the holding device bears on the wall of an orifice of the bodily canal emerging in a natural cavity. The holding device is linked at a distance to the flexible tube.
    Type: Grant
    Filed: May 27, 1994
    Date of Patent: May 7, 1996
    Assignee: Synthelabo
    Inventor: Gerard Torchio
  • 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: 5476942
    Abstract: Compounds of the formula: ##STR1## in which R.sub.1 represents a hydrogen atom or a (C.sub.1 -C.sub.4)alkyl group, R.sub.2 represents a hydrogen atom, a (C.sub.1 -C.sub.4)alkoxycarbonyl group, a carboxyl group, a sodium carboxylate group, a group --CH.sub.2 OR.sub.4, where R.sub.4 is a hydrogen atom or R.sub.4 is a (C.sub.1 -C.sub.4) alkyl or (C.sub.1 -C.sub.4) acyl group, a group --CONR.sub.5 R.sub.6, or a group --CN.sub.4 R.sub.5, where R.sub.5 is a hydrogen atom or a (C.sub.1 -C.sub.4)alkyl group and R.sub.6 is a hydrogen atom or a (C.sub.1 -C.sub.4)alkyl, hydroxyl or (C.sub.1 -C.sub.4) alkoxy or (C.sub.1 -C.sub.3) alkoxyphenyl group and R.sub.3 represents a (C.sub.1 -C.sub.4)alkyl group, and their acid addition salts are useful as synthetic intermediates.
    Type: Grant
    Filed: September 14, 1994
    Date of Patent: December 19, 1995
    Assignee: Synthelabo
    Inventors: Gilbert Lassalle, Daniel Galtier, Frederic Galli