Patents Assigned to Glaxo Wellcome SpA
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Patent number: 6479488Abstract: 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 cyclType: GrantFiled: October 30, 2000Date of Patent: November 12, 2002Assignee: Glaxo Wellcome SpAInventors: Romano Di-Fabio, Alessandra Pasquarello, Fabio Maria Sabbatini
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Patent number: 6413930Abstract: The use of CCK-B antagonists for the treatment of sleep disorders.Type: GrantFiled: April 10, 1997Date of Patent: July 2, 2002Assignee: Glaxo Wellcome SpaInventors: Emiliangelo Ratti, David Gordon Trist, Giovanni Gaviraghi, Francesco Crespi, Angelo Mario Reggiani
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Publication number: 20010047094Abstract: 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: ApplicationFiled: February 13, 2001Publication date: November 29, 2001Applicant: Glaxo Wellcome SpAInventors: Tino Rossi, Daniele Andreotti, Giovanna Tedesco, Luca Tarsi, Emiliangelo Ratti, Aldo Feriani, Domenica Antonia Pizzi, Giovari Gaviraghi, Stefano Biondi, Gabriella Finizia
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Patent number: 6239287Abstract: 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: GrantFiled: September 7, 1999Date of Patent: May 29, 2001Assignee: Glaxo Wellcome SpAInventors: Simon Charles Dolan, Paolo Maragni, Alcide Perboni
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Patent number: 6100289Abstract: 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: GrantFiled: August 16, 1999Date of Patent: August 8, 2000Assignee: Glaxo Wellcome SpAInventors: Alfredo Cugola, Romano Di Fabio, Giorgio Pentassuglia
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Patent number: 6025487Abstract: 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: GrantFiled: March 27, 1998Date of Patent: February 15, 2000Assignee: Glaxo Wellcome SpAInventors: Stephen Hanessian, Michael John Rozema
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Patent number: 6020359Abstract: 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: GrantFiled: January 12, 1999Date of Patent: February 1, 2000Assignee: Glaxo Wellcome SpAInventors: Andrea Lodi, Maria Teresa Rossato
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Patent number: 5977136Abstract: 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: GrantFiled: March 17, 1998Date of Patent: November 2, 1999Assignee: Glaxo Wellcome SpAInventors: Romano Di Fabio, Simone Giacobbe, Barbara Bertani, Fabrizio Micheli
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Patent number: 5962496Abstract: 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: GrantFiled: May 29, 1998Date of Patent: October 5, 1999Assignee: Glaxo Wellcome SpAInventors: Alfredo Cugola, Romano Di Fabio, Giorgio Pentassuglia
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Patent number: 5886018Abstract: 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: GrantFiled: July 25, 1997Date of Patent: March 23, 1999Assignee: Glaxo Wellcome SpAInventors: Andrea Lodi, Maria Teresa Rossato
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Patent number: 5849907Abstract: 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: GrantFiled: November 7, 1997Date of Patent: December 15, 1998Assignee: Glaxo Wellcome SpAInventor: Garfield Cecil Tughan
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Patent number: 5817806Abstract: 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: GrantFiled: January 3, 1997Date of Patent: October 6, 1998Assignee: Glaxo Wellcome SpAInventors: Tino Rossi, Paola Zarantonello, John Russel Thomas
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Patent number: 5760059Abstract: 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: GrantFiled: March 29, 1996Date of Patent: June 2, 1998Assignee: Glaxo Wellcome SpAInventors: Alfredo Cugola, Romano DiFabio, Giorgio Pentassuglia
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Patent number: 5733867Abstract: 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: GrantFiled: November 4, 1996Date of Patent: March 31, 1998Assignee: Glaxo Wellcome SpAInventors: Giovanni Curotto, Mario Pellegatti, Stefano Polinelli