Patents Assigned to Glaxo Wellcome SpA
  • Patent number: 6479488
    Abstract: Compounds of formula (I) or salt, or metabolically labile ester thereof wherein R represents a group selected from halogen, alkyl, alkoxy, amino, alkylamino, dialkylamino, hydroxy, trifluoromethoxy, nitro, cyano, SO2R2 or COR2 wherein R2 represents hydroxy, methoxy, amino, alkylamino or dialkylamino; m is zero or an integer 1 or 2; R1 represents cyano or the group (CH2)nCN, —CH═CHR3, CH2)nNHCOCH2R4 or O(CH2)pNR5R6; R3 represents cyano or the group COR7; R4 represents alkoxy or a group NHCOR8; R5 and R6 each represent independently hydrogen or alkyl, or R5 and R6 together with the nitrogen atom to which they are attached represent a heterocyclic group, or R5 is hydrogen and R6 is the group COR9; R7 represents an alkoxy, amino or hydroxyl group; R8 represents a hydrogen atom or optionally substituted alkyl, alkoxy, aryl, or heterocyclic group; R9 is the group R8 or the group NR10R11 wherein R10 represents hydrogen or alkyl group; R11 represents optionally substituted alkyl, aryl, heterocyclic or cycl
    Type: Grant
    Filed: October 30, 2000
    Date of Patent: November 12, 2002
    Assignee: Glaxo Wellcome SpA
    Inventors: Romano Di-Fabio, Alessandra Pasquarello, Fabio Maria Sabbatini
  • Patent number: 6413930
    Abstract: The use of CCK-B antagonists for the treatment of sleep disorders.
    Type: Grant
    Filed: April 10, 1997
    Date of Patent: July 2, 2002
    Assignee: Glaxo Wellcome Spa
    Inventors: Emiliangelo Ratti, David Gordon Trist, Giovanni Gaviraghi, Francesco Crespi, Angelo Mario Reggiani
  • Publication number: 20010047094
    Abstract: A compound of formula (1), salts and metabolically labile esters thereof, wherein R represents optionally substituted aryl or heteroaryl group; A represents a propylene chain or A is a chain of 3 members one of which is selected from an oxygen or sulphur atom orthe group NH or a substituted derivative thereof and the other two members are methylene groups, having antibacterial activity, processes for their preparation and to their use in medicine.
    Type: Application
    Filed: February 13, 2001
    Publication date: November 29, 2001
    Applicant: Glaxo Wellcome SpA
    Inventors: Tino Rossi, Daniele Andreotti, Giovanna Tedesco, Luca Tarsi, Emiliangelo Ratti, Aldo Feriani, Domenica Antonia Pizzi, Giovari Gaviraghi, Stefano Biondi, Gabriella Finizia
  • Patent number: 6239287
    Abstract: A process for the preparation of the phosphonium compound of formula (1), which comprises reacting N-phenylpyrrolidinone (II), with pyridinium bromide perbromide, in the presence of a tertiary organic base and a suitable lewis acid and then treating the resultant bromo derivative (III) with the phosphine (IV, R1R2R1P) and the use of compound (I) when so prepared for the preparation of the glycine antagonist.
    Type: Grant
    Filed: September 7, 1999
    Date of Patent: May 29, 2001
    Assignee: Glaxo Wellcome SpA
    Inventors: Simon Charles Dolan, Paolo Maragni, Alcide Perboni
  • Patent number: 6100289
    Abstract: This invention relates to compounds of formula ##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.2 or COR.sub.2 where R.sub.2 represents hydroxy, methoxy, amino, alkylamino, or dialkylamino; m is zero or an integer 1 or 2;R.sub.1 represents a cycloalkyl, bridged cycloalkyl, heteroaryl, bridged heterocyclic or optionally substituted phenyl or fused bicyclic carbocylic group;A represents a C.sub.1-4 alkylene chain or the chain (CH.sub.2).sub.p Y(CH.sub.2).sub.q wherein Y is O, S(O)n or NR.sub.3 and which chains may be substituted by one or two groups selected from C.sub.1-6 alkyl optionally substituted by hydroxy, amino, alkylamino or dialkylamino, or which chains may be substituted by the group .dbd.O;R.sub.
    Type: Grant
    Filed: August 16, 1999
    Date of Patent: August 8, 2000
    Assignee: Glaxo Wellcome SpA
    Inventors: Alfredo Cugola, Romano Di Fabio, Giorgio Pentassuglia
  • Patent number: 6025487
    Abstract: A process for the preparation of a compound (I) ##STR1## wherein R is a hydroxyl protecting group which comprises isomerising a compound of formula (I) wherein R is a hydroxyl protecting group by reacting the compound of formula (I) with a sterically hindered organic base in the presence of a Lewis acid and a compound of forumula (III) ##STR2## wherein R.sub.1 and R.sub.2 each independently represent cyano, COR.sub.5 or COR.sub.2 R.sub.6 or R.sub.1 andR.sub.2 together with the carbon atom to which they are attached from a C.dbd.O group;R.sub.5 represents alkyl, cycloalkyl, amino, alkylamino, dialkyl amino or optionally substituted phenyl or phenylalkyl group;R.sub.6 represents alkyl, cycloalkyl or optionally substituted phenyl or phenylalkyl group;R.sub.3 and R.sub.4 represent each independently hydrogen, alkyl, alkoxy or optionally substituted phenyl group.
    Type: Grant
    Filed: March 27, 1998
    Date of Patent: February 15, 2000
    Assignee: Glaxo Wellcome SpA
    Inventors: Stephen Hanessian, Michael John Rozema
  • Patent number: 6020359
    Abstract: A Pharmaceutical composition in a form suitable for parenteral administration comprising a solution of the glycine antagonist (E)-3-[2-phenylcarbamoyl) ethenyl]-4,6-dichloroindole-2-carboxylic, acid or a physiologically acceptable salt thereof, in an isotonic sugar solution containing a water miscible organic solvent for the compound, said formulation having a pH within the range of 7 to 9.
    Type: Grant
    Filed: January 12, 1999
    Date of Patent: February 1, 2000
    Assignee: Glaxo Wellcome SpA
    Inventors: Andrea Lodi, Maria Teresa Rossato
  • Patent number: 5977136
    Abstract: Compounds of formula (I) or a salt, or metabolically labile ester thereof, processes for the preparation thereof and their use as antagonists of excitatory amino acids.
    Type: Grant
    Filed: March 17, 1998
    Date of Patent: November 2, 1999
    Assignee: Glaxo Wellcome SpA
    Inventors: Romano Di Fabio, Simone Giacobbe, Barbara Bertani, Fabrizio Micheli
  • Patent number: 5962496
    Abstract: This invention relates to compounds of formula ##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.2 or COR.sub.2 wherein R.sub.2 represents hydroxy, methoxy, amino, alkylamino, or dialkylamino; m is zero or an integer 1 or 2;R.sub.1 represents a cycloalkyl, bridged cycloalkyl, heteroaryl, bridged heterocyclic or optionally substituted phenyl or fused bicyclic carbocylic group;A represents a C.sub.1-4 alkylene chain or the chain (CH.sub.2).sub.p Y(CH.sub.2).sub.q wherein Y is O, S(O)n or NR.sub.3 and which chains may be substituted by one or two groups selected from C.sub.1-6 alkyl optionally substituted by hydroxy, amino, alkylamino or dialkylamino, or which chains may be substituted by the group=O;R.sub.
    Type: Grant
    Filed: May 29, 1998
    Date of Patent: October 5, 1999
    Assignee: Glaxo Wellcome SpA
    Inventors: Alfredo Cugola, Romano Di Fabio, Giorgio Pentassuglia
  • Patent number: 5886018
    Abstract: A pharmaceutical composition is disclosed in a form suitable for parenteral administration, comprising a solution of the glycine antagonist, (E)-3-?2-(phenylcarbamoyl) ethenyl!-4,6-dichloroindole-2-carboxylic acid, or a physiologically acceptable salt thereof, in an isotonic sugar solution containing a water miscible organic solvent for the compound, said formulation having a pH within the range of 7 to 9.
    Type: Grant
    Filed: July 25, 1997
    Date of Patent: March 23, 1999
    Assignee: Glaxo Wellcome SpA
    Inventors: Andrea Lodi, Maria Teresa Rossato
  • Patent number: 5849907
    Abstract: A process for the preparation of the antibacterial compound ##STR1## or a salt thereof which comprises hydrogenolysis of the novel compound of formula (II) ##STR2## and if necessary or desired isolating the resultant carboxylic acid as a salt thereof.
    Type: Grant
    Filed: November 7, 1997
    Date of Patent: December 15, 1998
    Assignee: Glaxo Wellcome SpA
    Inventor: Garfield Cecil Tughan
  • Patent number: 5817806
    Abstract: 1. A process for the preparation of compounds of formula (I) wherein R.sub.1 is a hydroxyl protecting group ##STR1## which comprises reacting the azetidinone (II) with the homochiral (2S)-2- methoxycyclohexane (III) or the complex thereof formed with one molecule of stannic chloide.
    Type: Grant
    Filed: January 3, 1997
    Date of Patent: October 6, 1998
    Assignee: Glaxo Wellcome SpA
    Inventors: Tino Rossi, Paola Zarantonello, John Russel Thomas
  • Patent number: 5760059
    Abstract: This invention relates to compounds of formula ##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.2 or COR.sub.2 wherein R.sub.2 represents hydroxy, methoxy, amino, alkylamino, or dialkylamino; m is zero or an integer 1 or 2;R.sub.1 represents a cycloalkyl, bridged cycloalkyl, heteroaryl, bridged heterocyclic or optionally substituted phenyl or fused bicyclic carbocylic group;A represents a C.sub.1-4 alkylene chain or the chain (CH.sub.2).sub.p Y(CH.sub.2).sub.q wherein Y is O, S(O)n or NR.sub.3 and which chains may be substituted by one or two groups selected from C.sub.1-6 alkyl optionally substituted by hydroxy, amino, alkylamino or dialkylamino, or which chains may be substituted by the group .dbd.O;R.sub.
    Type: Grant
    Filed: March 29, 1996
    Date of Patent: June 2, 1998
    Assignee: Glaxo Wellcome SpA
    Inventors: Alfredo Cugola, Romano DiFabio, Giorgio Pentassuglia
  • Patent number: 5733867
    Abstract: Compounds of general formula (I) ##STR1## wherein R.sup.1 represents a phenyl, C.sub.3-7 cycloalkyl, C.sub.7-11 bridgedcycloalkyl or C.sub.1-6 alkyl group which alkyl group may be substituted by a hydroxy, phenyl, C.sub.1-6 alkoxycarbonyl, C.sub.3-7 cycloalkyl, or C.sub.3-7 bridgedcycloalkyl group;R.sup.2 represents phenyl substituted by a group (CH.sub.2).sub.n NR.sup.4 R.sup.5, O(CH.sub.2).sub.p R.sup.6, or (CH.sub.2).sub.n CO.sub.2 R.sup.11 ;R.sup.3 represents phenyl optionally substituted by one or 2 halogen atoms;R.sup.4 represents hydrogen or C.sub.1-4 alkyl;R.sup.5 represents acyl, or C.sub.2-4 alkyl substituted by one or more hydroxy; carboxyl and/or amino groups or R.sup.4 and R.sup.5 together with the nitrogen atom to which they are attached form a 5-7 saturated heterocyclic ring which contain an additional heteroatom selected from oxygen, sulphur or nitrogen and/or may be substituted by 1 or 2 C.sub.1-4 alkyl or hydroxy groups.R.sup.6 represents hydroxy, C.sub.1-4 alkoxy, CO.sub.2 R.sup.7 or NR.
    Type: Grant
    Filed: November 4, 1996
    Date of Patent: March 31, 1998
    Assignee: Glaxo Wellcome SpA
    Inventors: Giovanni Curotto, Mario Pellegatti, Stefano Polinelli