Patents Assigned to GLAXO S.P.A.
  • Patent number: 5407931
    Abstract: The invention relates to heterocyclic derivatives having antibacterial activity, to processes for their preparation, to compositions containing them, and to their medicinal uses.
    Type: Grant
    Filed: September 7, 1990
    Date of Patent: April 18, 1995
    Assignee: Glaxo S.p.A.
    Inventors: Bruno Tamburini, Alcide Perboni, Tino Rossi, Daniele Donati, Daniele Andreotti, Giovanni Gaviraghi, Roberto Carlesso, Claudio Bismara
  • Patent number: 5374648
    Abstract: The invention relates to compounds of formula (I). ##STR1## or a salt, or metabolically labile ester thereof wherein R represents a group selected from halogen, alkyl, alkoxy, amino, alkylamino, dialkylamino, hydroxy, trifluoromethyl, trifluoromethoxy, nitro, cyano, SO.sub.2 R.sub.1 or COR.sub.1 wherein R.sub.1 represents hydroxy, methoxy, or amino; m is zero or an integer 1 or 2;A represents an ethynyl group or an optionally substituted ethenyl, orcyclopropyl group or a substituted ethenyl group;X represents --O-- or NH;R.sub.2 represents an aryl group and when X represents an oxygen atom R.sub.2 may also represent a hydrogen atom or an alkyl group; which are antagonists of excitatory amino acids, to processes for their preparation and to their use in medicine.
    Type: Grant
    Filed: April 15, 1993
    Date of Patent: December 20, 1994
    Assignee: Glaxo S.p.A.
    Inventors: Alfredo Cugola, Giovanni Gaviraghi, Simone Giacobbe
  • Patent number: 5374649
    Abstract: The invention relates to compounds of formula I. ##STR1## or a salt, or metabolically labile ester thereof wherein A represents an unsubstituted ethenyl, group in the trans configuration, R.sub.1 represents a substituted phenyl group which are antagonists of excitatory amino acids, to processes for their preparation and to their use in medicine.
    Type: Grant
    Filed: April 15, 1993
    Date of Patent: December 20, 1994
    Assignee: Glaxo S.p.A.
    Inventors: Alfredo Cugola, Giovanni Gaviraghi
  • Patent number: 5373018
    Abstract: The invention relates to the compound of formula (I) ##STR1## wherein A represents an unsubstituted ethenyl group in the trans (E) configuration or a physiologically acceptable salt or metabilically labile ester thereof which are antagonists of excitatory amino acids, to processes for their preparation and to their use in medicine.
    Type: Grant
    Filed: April 15, 1993
    Date of Patent: December 13, 1994
    Assignee: Glaxo S.p.A.
    Inventors: Alfredo Cugola, Giovanni Gaviraghi
  • Patent number: 5196528
    Abstract: Compounds of formula ##STR1## in which R.sub.1 is hydrogen or a hydroxyl protecting group and --X--Y-- is --CH.dbd.CH-- or ##STR2## useful as intermediates in the preparation of antibacterially active compounds.
    Type: Grant
    Filed: July 12, 1991
    Date of Patent: March 23, 1993
    Assignee: Glaxo S.p.A.
    Inventors: Alcide Perboni, Claudio Bismara, Giorgio Pentassuglia
  • Patent number: 5162345
    Abstract: Compounds are described of the formula: ##STR1## and physiologically acceptable salts thereof, in which R.sub.1 -R.sub.7 are defined hereinafter.The compounds represented by formula (I) reduce intracellular calcium ion concentration by limiting transmembranal calcium ion concentration and thus may be useful for the treatment of cardiovascular disorders such as hypertension.
    Type: Grant
    Filed: August 20, 1990
    Date of Patent: November 10, 1992
    Assignee: Glaxo, S.p.A.
    Inventors: Claudio Semeraro, Dino Micheli, Daniele Pieraccioli, Giovanni Gaviraghi, Alan D. Borthwick
  • Patent number: 5138048
    Abstract: Compounds of the general formula (I) ##STR1## in which: R.sub.1 represents a hydroxyl protecting group; andR.sub.2 represents a hydrogen or halogen atom, an azido group, a C.sub.1-3 alkyl group, a group (CH.sub.2).sub.m OR.sub.3 wherein m is zero or one and R.sub.3 represents a hydrogen atom or a hydroxyl protecting group, an azidoethoxy group, a protected hydroxyethoxy group or a group XR.sub.4 in which X is an oxygen atom or the group S(O).sub.n in which n is zero, 1 or 2 and R.sub.4 represents a C.sub.1-5 alkyl, C.sub.3-7 cycloalkyl or phenyl group or when X is oxygen or sulphur then R.sub.4 may also represent the group AlkNR.sub.5 R.sub.6 in which Alk represents a C.sub.2-6 straight or branched alkylene chain and R.sub.5 and R.sub.6 independently represent a hydrogen atom or C.sub.1-4 alkyl group or R.sub.5 and R.sub.6 together with the nitrogen atom to which they are attached form a pyrrolidino or piperidino ring or the group NR.sub.5 R.sub.6 represents a protected amino group, or R.sub.
    Type: Grant
    Filed: September 7, 1990
    Date of Patent: August 11, 1992
    Assignee: Glaxo S.p.A.
    Inventors: Bruno Tamburini, Alcide Perboni, Tino Rossi, Daniele Donati, Daniele Andreotti, Giovanni Gaviraghi, Stefano Biondi, Claudio Bismara
  • Patent number: 5091395
    Abstract: Compounds are described of the formula ##STR1## wherein R.sub.1 and R.sub.4 independently represent a C.sub.1-4 alkyl group;R.sub.2 and R.sub.3 independently represent a C.sub.1-6 straight or branched alkyl chain or alkoxy group;R.sub.5 represents a straight or branched chain C.sub.1-13 alkyl group or a C.sub.5-8 cycloalkyl group which may be substituted by a C.sub.1-3 alkyl substituent;R.sub.6 represents a halogen atom or a straight or branched C.sub.1-3 alkyl group.The compounds represented by formula (I) reduce intracellular calcium ion concentration by limiting transmembranal calcium ion reflux and thus may be useful for the treatment of cardiovascular disorders such as hypertension.
    Type: Grant
    Filed: November 4, 1988
    Date of Patent: February 25, 1992
    Assignee: Glaxo S.p.A.
    Inventors: Claudio Semeraro, Dino Micheli, Daniele Pieraccioli, Giovanni Gaviraghi, Alan D. Borthwick
  • Patent number: 5051432
    Abstract: Compounds are described of the formula ##STR1## wherein R.sub.1 and R.sub.4 independently represent a C.sub.1-4 alkyl group:R.sub.2 represents a group ##STR2## (where A is a bond or a methylene group and R.sub.7 is phenyl C.sub.1-4 alkyl; or R.sub.2 represents a group CH.sub.2 CH.sub.2 NR.sub.8 R.sub.9 (where R.sub.8 is hydrogen or C.sub.1-4 alkyl and R.sub.9 is C.sub.1-4 alkyl, phenyl C.sub.1-4 alkyl or benzoyl C.sub.1-4 alkyl); or R.sub.2 represents a C.sub.1-4 alkyl group substituted by nitrile.R.sub.3 represents a C.sub.1-6 straight or brached alkyl chain or alkoxy group;R.sub.5 represents a straight or branched chain C.sub.1-13 alkyl group or a C.sub.5-8 cycloalkyl group which may be substituted by a C.sub.1-3 alkyl substituent;R.sub.6 represents a halogen atom or a straight or branched C.sub.1-3 alkyl group.
    Type: Grant
    Filed: September 19, 1990
    Date of Patent: September 24, 1991
    Assignee: Glaxo, S.p.A.
    Inventors: Claudio Semeraro, Dino Micheli, Daniele Pieraccioli, Giovanni Gaviraghi, Alan D. Borthwick
  • Patent number: 5011848
    Abstract: Compounds are described of the formula ##STR1## wherein R.sub.1 and R.sub.4 independently represent a C.sub.1-4 alkyl group;R.sub.2 and R.sub.3 independently represent a C.sub.1-6 straight or branched alkyl chain which may be interrupted by an oxygen atom;R.sub.5 represents a straight or branched chain C.sub.1-13 alkyl group or a C.sub.5-8 cycloalkyl group which may be substituted by a C.sub.1-3 alkyl substitutent;The compounds represented by formula (I) reduce intracellular calcium ion concentration by limiting transmembranal calcium ion influx and thus may be useful for the treatment of cardiovascular disorders such as hypertension.
    Type: Grant
    Filed: January 23, 1989
    Date of Patent: April 30, 1991
    Assignee: Glaxo, S.p.A.
    Inventors: Claudio Semeraro, Dino Micheli, Daniele Pieraccioli, Giovanni Gaviraghi, Allan D. Borthwick
  • Patent number: 4963571
    Abstract: Compounds are described of the formula ##STR1## wherein R.sub.1 and R.sub.4 independently represent a C.sub.1-4 alkyl group;R.sub.2 and R.sub.3 independently represent a C.sub.1-6 straight or branched alkyl chain or alkoxy group;R.sub.5 represents a straight or branched chain C.sub.1-13 alkyl group or a C.sub.5-8 cycloalkyl group which may be substituted by a C.sub.1-3 alkyl substituent;R.sub.6 represents a halogen atom or a straight or branched C.sub.1-3 alkyl group.R.sub.7 represents a C.sub.1-4 alkyl group [optionally substituted by hydroxy, C.sub.1-3 alkoxy or trifluoromethyl or by a group NR.sub.8 R.sub.9 where NR.sub.8 R.sub.9 forms a saturated 5 to 7 membered ring optionally containing an additional heleroatom which is oxygen]; or R.sub.7 represents a phenylC.sub.1-2 alkyl group in which the portion is optionally substituted by 1 to 3 C.sub.1-3 alkyl or C.sub.1-3 alkoxy groups or halogen atoms.
    Type: Grant
    Filed: November 16, 1988
    Date of Patent: October 16, 1990
    Assignee: Glaxo S.p.A.
    Inventors: Claudio Semeraro, Dino Micheli, Daniele Pieraccioli, Giovanni Gaviraghi, Alan D. Borthwick
  • Patent number: 4946851
    Abstract: Compounds are described of the formula ##STR1## wherein R.sub.1 and R.sub.4 independently represent a C.sub.1-4 alkylgroup;R.sub.2 and R.sub.3 independently represent a C.sub.1-6 straight orbranched alkyl chain or alkoxy group;R.sub.4 represents a C.sub.1-4 alkyl group;R.sub.5 represents a group CH.dbd.CR.sub.6 R.sub.7 where R.sub.6 is a hydrogen atom or C.sub.1-3 alkyl group and R.sub.7 represents an aryl, pyridyl or cyano group; or R.sub.5 represents the group C.tbd.CR.sub.8 where R.sub.8 is an aryl group.The compounds represented by formula (I) reduce intracellular calcium ion concentration by limiting transmembranal calcium ion influx and thus may be useful for the treatment of cardiovascular disorders such as hypertension.
    Type: Grant
    Filed: October 28, 1988
    Date of Patent: August 7, 1990
    Assignee: Glaxo, S.p.A.
    Inventors: Claudio Semeraro, Dino Micheli, Daniele Pieraccioli, Giovanni Gaviraghi, Alan D. Borthwick
  • Patent number: 4935548
    Abstract: Compounds are described of the formula ##STR1## wherein R.sub.1 represents a formyl or nitrile group or a group OCH.sub.2 A where A represents hydroxy, C.sub.1-4 alkoxy or D(CH.sub.2).sub.n NR.sub.7 R.sub.8 (where R.sub.7 and R.sub.8 independently represent hydrogen or C.sub.1-4 alkyl and n is 2 or 3);R.sub.2 and R.sub.3 independently represent a C.sub.1-6 straight or branched alkyl chain or alkoxy group;R.sub.4 represents a C.sub.1-4 alkyl group;R.sub.5 represents a straight or branched chain C.sub.1-13 alkyl group or a C.sub.5-8 cycloalkyl group which may be substituted by a C.sub.1-3 alkyl substituent;R.sub.6 represents a halogen atom or a straight or branched C.sub.1-3 alkyl group.The compounds represented by formula (I) reduce intracellular calcium ion concentration by limiting transmembranal calcium ion influx and thus may be useful for the treatment of cardiovascular disorders such as hypertension.
    Type: Grant
    Filed: October 21, 1988
    Date of Patent: June 19, 1990
    Assignee: Glaxo S.p.A
    Inventors: Claudio Semeraro, Dino Micheli, Daniele Pieraccioli, Giovanni Gaviraghi, Alan D. Borthwick
  • Patent number: 4806533
    Abstract: Compounds are described of the formula ##STR1## wherein R.sub.1 and R.sub.4 independently represent a C.sub.1-4 alkyl group;R.sub.2 and R.sub.3 independently represent a C.sub.1-6 straight or branched alkyl chain or alkoxy group;R.sub.5 represents a straight or branched chain C.sub.1-13 alkyl group or a C.sub.5-8 cycloalkyl group which may be substituted by a C.sub.1-3 alkyl substituent;R.sub.6 represents a halogen atom or a straight or branched C.sub.1-3 alkyl group.R.sub.7 represents a C.sub.1-4 alkyl group [optionally substituted by hydroxy, C.sub.1-3 alkoxy or trifluoromethyl or by a group NR.sub.8 R.sub.9 where NR.sub.8 R.sub.9 forms a saturated 5 to 7 membered ring optionally containing an additional heleroatom which is oxygen]; or R.sub.7 represents a phenylC.sub.1-2 alkyl group in which the phenyl portion is optionally substituted by 1 to 3 C.sub.1-3 alkyl or C.sub.1-3 alkoxy groups or halogen atoms.
    Type: Grant
    Filed: February 19, 1987
    Date of Patent: February 21, 1989
    Assignee: Glaxo, s.p.a.
    Inventors: Claudio Semeraro, Dino Micheli, Daniele Pieraccioli, Giovanni Gaviraghi, Alan D. Borthwick
  • Patent number: 4801599
    Abstract: Compounds are described of the formula ##STR1## wherein R.sub.1 and R.sub.4 independently represent a C.sub.1-4 alkyl group;R.sub.2 and R.sub.3 independently represent a C.sub.1-6 straight or branched alkyl chain which may be interrupted by an oxygen atom;R.sub.5 represents a straight or branched chain C.sub.1-13 alkyl group or a C.sub.5-8 cycloalkyl group which may be substituted by a C.sub.1-3 alkyl substitutent;The compounds represented by formula (I) reduce intracellular calcium ion cencentration by limiting transmembranal calcium ion influx and thus may be useful for the treatment of cardiovascular disorders such as hypertension.
    Type: Grant
    Filed: August 20, 1985
    Date of Patent: January 31, 1989
    Assignee: GLAXO S.P.A.
    Inventors: Claudio Semeraro, Dino Micheli, Daniele Pieraccioli, Giovanni Gaviraghi, Allan D. Borthwick
  • Patent number: 4669502
    Abstract: A device for the automatic selection of the mobile phase to be sent to a chromatographic apparatus, particularly HPLC. The reservoirs containing the different fluids are connected to the lateral channels of a single manifold through solenoid valves controlled by the central processing unit (C.P.U.) of the chromatographic apparatus.
    Type: Grant
    Filed: November 13, 1985
    Date of Patent: June 2, 1987
    Assignee: 501 Glaxo S.p.A.
    Inventors: Silvano Lonardi, Fulvio Ottofaro