Patents Assigned to Vernalis Research Limited
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Patent number: 7166613Abstract: A chemical compound of formula (I) wherein R1 and R2 are independently selected from hydrogen and alkyl; R3 is alkyl; R4 and R5 are selected from hydrogen and alkyl; R6 and R7 are independently selected from hydrogen, halogen, hydroxyl, alkyl, aryl, amino, alkylamino, dialkylamino, alkoxy, aryloxy, alkylthio, alkylsulfoxyl, nitro, carbonitrile, carbo-alkoxy, carbo-aryloxy and carboxyl; and A is a 5- or 6-membered ring optionally containing one or more heteroatoms wherein the atoms of the ring A, other than the unsaturated carbon atoms of the phenyl ring to which the ring A is fused, are saturated or unsaturated, and pharmaceutically acceptable salts, addition compounds and prodrugs thereof; and the use thereof in therapy, particularly as an agonist or antagonist of a 5HT receptor, particularly a 5HT2C receptor, for instance in the treatment of disorders of the central nervous system; damage to the central nervous system; cardiovascular disorders; gastrointestinal disorders; diabetes insipidus, and sleep apneaType: GrantFiled: April 29, 2005Date of Patent: January 23, 2007Assignee: Vernalis Research LimitedInventors: Jonathan Richard Anthony Roffey, James Edward Paul Davidson, Howard Langham Mansell, Richard John Hamlyn, David Reginald Adams
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Publication number: 20060276452Abstract: The use of a compound of formula (1): wherein: R1 is aryl; R2 is H, alkyl or aryl; and R3 is hydrogen or alkyl; or a pharmaceutically acceptable salt or prodrug thereof, in the manufacture of a medicament for the treatment of a disorder mediated by CB1 receptors.Type: ApplicationFiled: April 29, 2004Publication date: December 7, 2006Applicant: VERNALIS RESEARCH LIMITEDInventors: James Davidson, David Adams, Michael Bickerdike, Alan Fletcher
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Patent number: 7145009Abstract: Chemical compounds of formula (I): and pharmaceutically acceptable salts and addition compounds and prodrugs thereof are useful in therapy, particularly for the treatment of disorders of the central nervous system; damage to the central nervous system; cardiovascular disorders; gastrointestinal disorders; diabetes inspidus, and sleep apnea.Type: GrantFiled: October 16, 2003Date of Patent: December 5, 2006Assignee: Vernalis Research LimitedInventors: David Reginald Adams, Jon Mark Bentley, James Davidson, Matthew Alexander James Duncton, Richard Hugh Phillip Porter
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Patent number: 7098333Abstract: Use of a compound of the formula (I) wherein R1 is selected from alkyl, alkoxy, aryloxy, alkylthio, arylthio, aryl, halogen, CN, NR7R8, NR6COR7, NR6CO2R9 and NR6SO2R9; R2 is selected from aryl attached via an unsaturated carbon; R3 and R4 are independently selected from H, alkyl, halogen, alkoxy, alkylthio, CN and NR7R8; R5 is selected from H, acyclic alkyl, COR6, CONR7R8, CONR6NR7R8, CO2R9 and SO2R9; R6, R7 and R8 are independently selected from H, alkyl and aryl or where R7 and R8 are in an NR7R8 group R7 and R8 may be linked to form a hererocyclic group, or where R6, R7 and R8 are in a (CONR6NR7R8) group, R6 and R7 may be linked to form a hererocyclic group; and R9 is selected from alkyl and aryl, or a pharmaceutically acceptable salt thereof or prodrug thereof, in the manufacture of a medicament for the treatment or prevention of a disorder in which the blocking of purine receptors, particularly adenosine receptors and more particularly A2A receptors, may be beneficial, particularly wherein said disorderType: GrantFiled: January 10, 2002Date of Patent: August 29, 2006Assignee: Vernalis Research LimitedInventors: Roger John Gillespie, Joanne Lerpiniere
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Patent number: 7098337Abstract: The present invention relates to compounds of formula (I) as well as pharmaceutically acceptable salts, solvates and esters thereof. These compounds can be used to prepare pharmaceutical compositions for the treatment or prevention of disorders of the central nervous system, damage to the central nervous system, cardiovascular disorders, gastrointestinal disorders, diabetes, obesity and sleep apnoea.Type: GrantFiled: January 24, 2003Date of Patent: August 29, 2006Assignees: Hoffmann-La Roche Inc., Vernalis Research LimitedInventors: David Reginald Adams, Jonathan Mark Bentley, Toby Jonathan Blench, Paul Hebeisen, Nathaniel Julius Thomas Monck, Hans Richter, Stephan Roever, Jonathan Richard Anthony Roffey, Sven Taylor
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Patent number: 7087754Abstract: Use of a compound of formula (I): wherein R1 is selected from alkyl, alkoxy, aryloxy, alkylthio, arylthio, aryl, halogen, CN, NR6R7, NR5COR6, NR5CONR6R7, NR5CO2R8 and NR5SO2R8; R2 is selected from heteroaryl attached via an unsaturated carbon; R3 is selected from H, alkyl, halogen, OR5, SR5 and NR6R7; R4 is selected from H, acyclic alkyl, CONR6R7, CONR5NR6R7, COR6, CO2R8 and SO2R; R5, R6 and R7 are independently selected from H, alkyl and aryl, or where R6 and R7 are in an NR6R7 group, R6 and R7 may be linked to form a heterocyclic group, or where R5, R6 and R7 are in a (CONR5NR6R7) group, R5 and R6 may be linked to form a heterocyclic group; and R8 is selected from alkyl and aryl, or a pharmaceutically acceptable salt thereof or prodrug thereof, in the treatment or prevention of a disorder in which the blocking of purine receptors, particularly adenosine receptors and more particularly A2A receptors, may be beneficial, particularly wherein said disorder is a movement disorder such as Parkinson's disease or sType: GrantFiled: January 10, 2002Date of Patent: August 8, 2006Assignee: Vernalis Research LimitedInventors: Roger John Gillespie, Joanne Lerpiniere, Suneel Gaur
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Patent number: 7022707Abstract: The present invention is a chemical compound of formula (I) or a pharmaceutically acceptable salts, solvates and esters thereof, wherein R1 to R4, A1, A2 m and n are as described in the specification.Type: GrantFiled: June 23, 2004Date of Patent: April 4, 2006Assignees: Hoffman-La Roche Inc., Vernalis Research LimitedInventors: David Reginald Adams, Jonathan Mark Bentley, James Edward Paul Davidson, Claire Elizabeth Dawson, Ashley Roger George, Howard Langham Mansell, Patrizio Mattei, Jacques Mizrahi, Matthias Heinrich Nettekoven, Robert Mark Pratt, Stephan Roever, Jonathan Richard Anthony Roffey, Jean-Luc Specklin, Henri Stalder, Kerry Wilkinson
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Patent number: 6962939Abstract: A chemical compound of formula (I) wherein R1 and R2 are independently selected from hydrogen and alkyl; R3 is alkyl; R4 and R5 are selected from hydrogen and alkyl; R6 and R7 are independently selected from hydrogen, halogen, hydroxy, alkyl, aryl, amino, alkylamino, dialkylamino, alkoxy, aryloxy, alkylthio, alkylsulfoxyl, alkylsulfonyl, nitro, carbonitrile, carbo-alkoxy, carbo-aryloxy and carboxyl; and A is a 5- or 6-membered ring optionally containing one or more heteroatoms wherein the atoms of the ring A, other than the unsaturated carbon atoms of the phenyl ring to which the ring A is fused, are saturated or unsaturated, and pharmaceutically acceptable salts, addition compounds and prodrugs thereof; and the use thereof in therapy, particularly as an agonist or antagonist of a 5HT receptor, particularly a 5HT2C receptor, for instance in the treatment of disorders of the central nervous system; damage to the central nervous system; cardiovascular disorders; gastrointestinal disorders; diabetes insipidus, aType: GrantFiled: August 4, 2000Date of Patent: November 8, 2005Assignee: Vernalis Research LimitedInventors: Jonathan Richard Anthony Roffey, James Edward Paul Davidson, Howard Langham Mansell, Richard John Hamlyn, David Reginald Adams
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Patent number: 6933387Abstract: The present invention is directed to 1,2,3,4,10,10a-hexahydropyrazino [1,2-a]indole derivatives of formula (I): as well as pharmaceutically acceptable salts, hydrates and esters thereof, wherein the substituents have the meanings provided in the specification. Compounds of the present invention may be used in the treatment or prevention of obesity or Type II diabetes.Type: GrantFiled: March 25, 2003Date of Patent: August 23, 2005Assignees: Hoffmann-La Roche Inc., Vernalis Research LimitedInventors: Jonathan Mark Bentley, Paul Hebeisen, Marc Muller, Hans Richter, Stephan Roever
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Patent number: 6831078Abstract: A compound of formula (1) wherein R1 is aryl; and R2 is hydrogen or alkyl; pharmaceutically acceptable addition compounds thereof; and their use in therapy, particularly for the treatment and prophylaxis of CNS disorders such as anxiety and epilepsy.Type: GrantFiled: February 12, 2001Date of Patent: December 14, 2004Assignee: Vernalis Research LimitedInventors: David Reginald Adams, Jon Bentley, Corinna Dagmar Bodkin, Ian Anthony Cliffe, James Edward Paul Davidson, Howard Langham Mansell, Nathaniel Julius Monck, Robin Gerald Shepherd, by Joy Miriam Shepherd
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Patent number: 6828318Abstract: Compounds of formula (1): wherein R1, R2, R3, R4, R5 and R6 are independently selected from hydrogen, alkyl, aryl and non-aromatic heterocyclic groups, or each of one or more pair(s) of the substituent groups R1 to R6 may together form a 3,4,5,6,7 or 8-membered ring containing 0,1 or 2 heteroatom(s); R7 is selected from alkyl, aryl and non-aromatic heterocyclic groups; and R8 is selected from hydrogen, halogen, alkyl, aryl and non-aromatic heterocyclic groups; and pharmaceutically acceptable salts and prodrugs thereof, are useful for treating conditions generally associated with abnormalities in glutamatergic transmission.Type: GrantFiled: March 31, 2003Date of Patent: December 7, 2004Assignee: Vernalis Research LimitedInventors: Michael Frederick Snape, Roger John Gillespie, Claire Elizabeth Dawson, Steven Michael McAteer, Suneel Gaur
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Patent number: 6800627Abstract: Chemical compounds of formula (I): and pharmaceutically acceptable salts and addition compounds and prodrugs thereof are useful in therapy, particularly for the treatment of disorders of the central nervous system; damage to the central nervous system; cardiovascular disorders; gastrointestinal disorders; diabetes inspidus, and sleep apnea.Type: GrantFiled: October 9, 2001Date of Patent: October 5, 2004Assignee: Vernalis Research LimitedInventors: David Reginald Adams, Jon Mark Bentley, James Davidson, Matthew Alexander James Duncton, Richard Hugh Phillip Porter
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Patent number: 6787541Abstract: Compounds of formula (I): wherein X is S. Compounds can be used for treating a disorder in which the blocking of purine receptors is beneficial.Type: GrantFiled: March 13, 2002Date of Patent: September 7, 2004Assignee: Vernalis Research LimitedInventors: Roger John Gillespie, Joanne Lerpiniere, Paul Richard Giles, Claire Elizabeth Dawson, David Bebbington
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Publication number: 20040092525Abstract: Chemical compounds of formula (I): 1Type: ApplicationFiled: October 16, 2003Publication date: May 13, 2004Applicant: VERNALIS RESEARCH LIMITEDInventors: David Reginald Adams, Jon Mark Bentley, James Davidson, Matthew Alexander James Duncton, Richard Hugh Phillip Porter
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Patent number: 6706750Abstract: A chemical compound of formula (I) wherein: R1 and R2 are independently selected from hydrogen and alkyl; R3 is alkyl; R4, R6 and R7 are independently selected from hydrogen, halogen, hydroxy, alkyl, aryl, amino, alkylamino, dialkylamino, alkoxy, aryloxy, alkylthio, alkylsufoxyl, alkylsulfonyl, nitro, carbonitrile, carbo-alkoxy, carbo-aryloxy and carboxyl; R5 is selected from hydrogen, halogen, hydroxy, alkyl, aryl, amino, alkylamino, dialkylamino, alkoxy, aryloxy, alkylthio, alkylsulfoxyl, alkylsulfonyl, nitro, carbonitrile, carbo-alkoxy, carbo-aryloxy and carboxyl; A is a 5- or 6-membered partially unsaturated or aromatic heterocyclic ring or a 5- or 6-membered partially unsaturated carbocyclic ring, wherein if A is a 6-membered partially unsaturated carbocyclic ring then at least one of R4 to R7 is other than hydrogen, and pharmaceutically acceptable salts, addition compounds and prodrugs thereof, and the use thereof in therapy, particularly as an agonist or antagonist of a 5HT receptor, particularly a 5HTType: GrantFiled: March 11, 2002Date of Patent: March 16, 2004Assignee: Vernalis Research LimitedInventors: Jonathan Mark Bentley, Jonathan Richard Anthony Roffey, James Edward Paul Davidson, Howard Langham Mansell, Richard John Hamlyn, Ian Anthony Cliffe, David Reginald Adams, Nathaniel Julius Monck
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Publication number: 20040039200Abstract: Chemical compounds of formula (I): 1Type: ApplicationFiled: August 5, 2003Publication date: February 26, 2004Applicant: VERNALIS RESEARCH LIMITEDInventors: David Reginald Adams, Jon Mark Bentley, James Davidson, Matthew Alexander James Dunction, Richard Hugh Phillip Porter
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Patent number: 6664397Abstract: Use of (+)-(11R,2′S)-&agr;-2-piperidinyl-2,8-bis(trifluoromethyl)-4-quinolinemethanol or a pharmaceutically acceptable salt thereof substantially free of its (−)-enantiomer in the manufacture of a medicament having reduced side-effect compared to the racemic (±)-(R*,S*)-&agr;-2-piperidinyl-2,8-bis(trifluoromethyl)-4-quinolinemethanol for treating or preventing malaria in a subject. A method of treating or preventing malaria with reduced side-effects comprising administration of (+)-(11R,2′S)-&agr;-2-piperidinyl-2,8-bis(trifluoromethyl)-4-quinolinemethanol or a pharmaceutically acceptable salt thereof substantially free of its (−)-enantiomer.Type: GrantFiled: November 22, 1999Date of Patent: December 16, 2003Assignee: Vernalis Research LimitedInventors: Allan Fletcher, Robin Shepherd
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Patent number: 6610685Abstract: The present invention is a chemical compound of formula (I) or a pharmaceutically acceptable salt, solvate and ester thereof, wherein R1 to R4 and n are as defined in the specification. A compound of formula 1 is useful as a pharmaceutical composition for the treatment or prevention of disorders of the central nervous system, cardiovascular disorders, gastrointestinal disorders, diabetes, obesity and sleep apnoea.Type: GrantFiled: December 14, 2001Date of Patent: August 26, 2003Assignees: Hoffmann-La Roche Inc., Vernalis Research LimitedInventors: Jonathan Mark Bentley, Michael John Bickerdike, Paul Hebeisen, Guy Anthony Kennett, Sean Lightowler, Patrizio Mattei, Jacques Mizrahi, Timothy James Morley, Jean-Marc Plancher, Hans Richter, Stephan Roever, Sven Taylor, Steven Paul Vickers
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Patent number: 6608085Abstract: Use of a compound of formula (I) as defined herein, or a pharmaceutically acceptable salt or prodrug thereof, in the manufacture of a medicament for the treatment or prevention of a disorder in which the blocking of purine receptors, particularly adenosine receptors and more particularly A2a receptors, may be beneficial, such as a movement disorder, for example, Parkinson's Disease or progressive supemuclear palsy, Huntingtons disease, multiple system atrophy, corticobasal degeneration, Wilsons disease, Hallerrorder-Spatz disease, progressive pallidal atrophy, Dopa-responsive dystonia-Parkinsonism, spasticity, Alzheimer's disease or other disorders of the basal ganglia which result in dyskinesias.Type: GrantFiled: May 9, 2001Date of Patent: August 19, 2003Assignee: Vernalis Research LimitedInventors: Roger John Gillespie, Joanne Lerpiniere, Paul Richard Giles, David Reginald Adams, Lars Jacob Stray Knutsen, Ian Anthony Cliffe
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Publication number: 20030130354Abstract: Use of a compound of the formula (1), wherein X is an alkylene chain comprising 0, 1, 2, 3 or 4 carbon atoms; R1, R2 and R3 are independently selected from hydrogen, alkyl and aryl; R4, R5 and R6 are independently selected from hydrogen, alkyl, aryl, halogen and alkoxy; and prodrugs thereof and pharmaceutically acceptable salts thereof; in the manufacture of a medicament for use in the treatment of a condition generally associated with abnormalities in glutamatergic transmission.Type: ApplicationFiled: November 12, 2002Publication date: July 10, 2003Applicant: VERNALIS RESEARCH LIMITEDInventors: Roger John Gillespie, Michael Frederick Snape, Simon Edward Ward