Patents Assigned to Vernalis Research Limited
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Publication number: 20130245044Abstract: Compounds of formula (I) that are capable of acting as purine receptor antagonists, pharmaceutical compositions including the compounds, and methods of making the compounds, are disclosed. The compounds and compositions can be used in treating or preventing disorders related to purine receptor hyperfunctioning.Type: ApplicationFiled: May 8, 2013Publication date: September 19, 2013Applicant: Vernalis Research LimitedInventors: Samantha Jane Bamford, Roger John Gillespie, Richard Simon Todd
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Publication number: 20100130515Abstract: Polymorphic and solvated forms of solid 3-(4-amino-3-methylbenzyl)-7-(furan-2-yl)-3H-[1,2,3]triazolo[4,5-d]pyrimidin-5-amine, and methods of making them, are described.Type: ApplicationFiled: July 13, 2009Publication date: May 27, 2010Applicants: BIOGEN IDEC INC., VERNALIS RESEARCH LIMITEDInventors: Slawomir Janicki, Hexi Chang, Weirong Chen, William F. Kiesman, Benjamin Lane, Richard Todd
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Patent number: 7629349Abstract: Pharmaceutical compositions and their uses comprising compounds of formula (I): wherein: R1 is selected from: alkyl, alkoxy, aryloxy, alkylthio, arylthio, aryl, halogen, CN, NR6R7, NR5COR6, NR5CONR6R7, NR5CO2R8, and NR5SO2R8; R2 is a heteroaryl attached via an unsaturated ring carbon of said heteroaryl group; R3 is selected from: H, alkyl, halogen, OR5, SR5, and NR6R7; R4 is selected from: H, acyclic alkyl, CONR6R7, CONR5NR6R7, COR6, CO2R8, and SO2R8; 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 hetero cyclic 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.Type: GrantFiled: January 12, 2006Date of Patent: December 8, 2009Assignee: Vernalis Research LimitedInventors: Roger John Gillespie, Joanne Lerpiniere, Suneel Gaur
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Patent number: 7598256Abstract: 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 Rs are in a (CONR6NR7Rs) 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 27, 2006Date of Patent: October 6, 2009Assignee: Vernalis Research LimitedInventors: Roger John Gillespie, Joanne Lerpiniere
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Patent number: 7589097Abstract: The use of a compound of formula (I): wherein R1 is selected from H, alkyl, aryl, alkoxy, aryloxy, alkylthio, arylthio, halogen, CN, NR5R6, NR4COR5, NR4CONR5R6, NR4CO2R7 and NR4SO2R7; R2 is selected from aryl attached via an unsaturated carbon; R3 is selected from H, alkyl, COR5, CO2R7, CONR5R6, CONR4NR5R6 and SO2R7; R4, R5 and R6 are independently selected from H, alkyl and aryl or where R5 and R6 are in an NR5R6 group, R5 and R6 may be linked to form a heterocyclic group, or where R4, R5 and R6 are in a (CONR4NR5R6) group, R4 and R5 may be linked to form a heterocyclic group; and R7 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 said disorder is depression, cognitive or memory impairment,Type: GrantFiled: December 20, 2007Date of Patent: September 15, 2009Assignee: Vernalis Research LimitedInventors: Roger John Gillespie, Joanne Lerpiniere, Suneel Gaur, Samantha Jayne Bamford, Gemma Caroline Stratton, Stefania Leonardi, Scott Murray Weiss
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Publication number: 20090181939Abstract: Compounds of formula (I) and their use in therapy, particularly for the treatment of a disorder mediated by CB1 receptors, such as obesity, wherein: R1 is aryl or heteroaryl; R2 is alkyl, aryl or heteroaryl; R3 is alkyl, aryl, heteroaryl, NR9R10, OR15, or NR16C(O)R17; Y is C?O, C?S, SO2, or (CR7R8)p; m=1 or 2; n=1 or 2; and p=1, 2, 3 or 4, R7 to R17 being as defined in the specification; wherein if —Y—R3 is C(O)NH(alkyl) then: R1 and/or R2 is selected from heteroaryl; and/or m and/or n is 2; and/or R11 and/or R12 is lower alkyl, or a pharmaceutically acceptable salt or prodrug thereof.Type: ApplicationFiled: March 19, 2009Publication date: July 16, 2009Applicant: VERNALIS RESEARCH LIMITED.Inventors: James Edward Paul Davidson, Jonathan Mark Bentley, Claire Elizabeth Dawson, Kerry Harrison, Howard Langham Mansell, Alan Leslie Pither, Robert Mark Pratt, Jonathan Richard Anthony Roffey, Victoria Jane Ruston
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Patent number: 7547699Abstract: The present invention refers to chemical compounds of formula (I) as well as pharmaceutically acceptable salts and esters thereof, wherein R1 to R5 have the significance given in claim 1. These compounds can be used for the preparation of medicaments.Type: GrantFiled: April 26, 2006Date of Patent: June 16, 2009Assignees: Hoffmann-La Roche Inc., Vernalis Research LimitedInventors: Paul Hebeisen, Nathaniel Monck, Hans Richter, Stephan Roever
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Patent number: 7504522Abstract: Compounds of formula (I) and their use in therapy, particularly for the treatment of a disorder mediated by CB1 receptors such as obesity: Formula (I) wherein: R1 and R2 are independently selected from aryl; and R3 is hydrogen or alkyl; or a pharmaceutically acceptable salt or prodrug thereof, wherein at least one of R1 and R2 has a non-hydrogen substituent in the ortho-position(s) thereof relative to the point of attachment to the [—CH—O—] group.Type: GrantFiled: April 29, 2004Date of Patent: March 17, 2009Assignee: Vernalis Research LimitedInventors: James Edward Paul Davidson, Claire Elizabeth Dawson, Kerry Harrison, Howard Langham Mansell, Robert Mark Pratt, Sukhjit Sohal, Victoria Jane Ruston
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Patent number: 7452894Abstract: Use of a compound of formula (I) wherein R1 is selected from alkyl, aryl, alkoxy, aryloxy, 0thioalkyl, thioaryl, CN, halo, NR5R6, NR4COR5, NR4CONR5R6, NR4CO2R7 and NR4SO2R7; R2 is selected from N, O or S-containing heteroaryl groups, wherein the heteroaryl group is attached via an unsaturated carbon atom which is adjacent to one or two N, O or S-heteroatom(s), other than ortho, ortho-disubstituted heteroaryl groups; R3 is selected from H, alkyl, COR8, CONR9R10, CONR8NR9R10, CO2R11 and SO2R11; R4, R5 and R6 are independently selected from H, alkyl and aryl or where R5 and R6 are in an (NR5R6) group then R5 and R6 may be linked to form a heterocyclic ring; R7 is selected from alkyl and aryl; R8, R9 and R10 are independently selected from H, alkyl and aryl, or R9 and R10 may be linked to form a heterocyclic ring, or where R8, R9 and R10 are in a (CONR8NR9R10) group, R8 and R9 may be linked to form a heterocyclic group; and R11, is selected from alkyl and aryl, or a pharmaceutically acceptable salt thereof or proType: GrantFiled: January 10, 2002Date of Patent: November 18, 2008Assignee: Vernalis Research LimitedInventors: Roger John Gillespie, Joanne Lerpiniere, Claire Elizabeth Dawson, Suneel Gaur, Robert Mark Pratt, Gemma Caroline Stratton, Scott Murray Weiss
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Patent number: 7405219Abstract: The use of a compound of formula (I): wherein R1 is selected from H, alkyl, aryl, alkoxy, aryloxy, alkylthio, arylthio, halogen, CN, NR5R6, NR4COR5, NR4CONR5R6, NR4CO2R7 and NR4SO2R7; R2 is selected from aryl attached via an unsaturated carbon; R3 is selected from H, alkyl, COR5, CO2R7, CONR5R6, CONR4NR5R6 and SO2R7; R4, R5 and R6 are independently selected from H, alkyl and aryl or where R5 and R6 are in an NR5R6 group, R5 and R6 may be linked to form a heterocyclic group, or where R4, R5 and R6 are in a (CONR4NR5R6) group, R4 and R5 may be linked to form a heterocyclic group; and R7 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 said disorder is depression, cognitive or memory impairment,Type: GrantFiled: August 22, 2006Date of Patent: July 29, 2008Assignee: Vernalis Research LimitedInventors: Roger John Gillespie, Joanne Lerpiniere, Suneel Gaur, Samantha Jayne Bamford, Gemma Caroline Stratton, Stefania Leonardi, Scott Murray Weiss
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Patent number: 7384949Abstract: A compound of formula (I), wherein X is S or O; R1 is selected from H, alkyl, aryl, hydroxy, alkoxy, aryloxy, thioalkyl, thioaryl, halogen, CN, COR5, CO2R5, CONR6R7, CONR5NR6R7, NR6R7, NR5CONR6R7, NR5COR6, NR5CO2R8, and NR5SO2R8; R2 is selected from aryl attached via an unsaturated carbon atom; R3 is selected from H, alkyl, hydroxy, alkoxy, halogen, CN and NO2; R4 is selected from H, alkyl, aryl, hydroxy, alkoxy, aryloxy, thioalkyl, thioaryl, halogen, CN, NO2, COR5, CO2R5, CONR6R7, CONR5NR6R7, NR6R7, NR5CONR6R7, NR5COR6, NR5CO2R8 and NR5SO2R8; 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, and the use thereof in therapy and in the treatment or prevention of a disorder in which the blockinType: GrantFiled: January 10, 2002Date of Patent: June 10, 2008Assignee: Vernalis Research LimitedInventors: Roger John Gillespie, Joanne Lerpiniere, Claire Elizabeth Dawson, Suneel Gaur, Robert Mark Pratt
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Patent number: 7323487Abstract: 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: December 12, 2006Date of Patent: January 29, 2008Assignee: 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: 7323473Abstract: 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, 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, and sleep apneaType: GrantFiled: December 12, 2006Date of Patent: January 29, 2008Assignee: 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: 7323466Abstract: The present invention refers to chemical compounds of formula (I) as well as pharmaceutically acceptable salts and esters thereof, wherein R1 to R5 have the significance given in claim 1. These compounds can be used for the preparation of medicaments.Type: GrantFiled: January 13, 2006Date of Patent: January 29, 2008Assignees: Hoffman-La Roche Inc., Vernalis Research LimitedInventors: Jonathan Mark Bentley, Claire Elizabeth Dawson, Wolfgang Guba, Paul Hebeisen, Nathaniel Monck, Robert Mark Pratt, Hans Richter, Stephan Roever, Vicki Ruston
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Patent number: 7323486Abstract: 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: December 12, 2006Date of Patent: January 29, 2008Assignee: 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: 7253281Abstract: The present invention is directed to 1,2,3,4,10,10a,-hexahydropyrazino[1,2-a]indole derivatives as well as pharmaceutically acceptable salts, solvates and esters thereof, wherein R1 to R8 have the significance given in claim 1 be used in the form of pharmaceutical preparations for the treatment or prevention of disorders of the central nervous system, damage to the central nervous system, cardiovascular disorders, gastrointestinal disorders, diabetes insipidus, obesity and sleep apnea.Type: GrantFiled: June 28, 2005Date of Patent: August 7, 2007Assignees: Hoffmann-La Roche Inc., Vernalis Research LimitedInventors: Jonathan Mark Bentley, Paul Hebeisen, Patrizio Mattei, Marc Muller, Hans Richter, Stephan Roever, Sven Taylor
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Publication number: 20070173486Abstract: Compounds of formula (I) and their use in therapy, particularly for the treatment of a disorder mediated by CB1 receptors, such as obesity, wherein: R1 is aryl or heteroaryl; R2 is alkyl, aryl or heteroaryl; R3 is alkyl, aryl, heteroaryl, NR9R10, OR15, or NR16C(O)R17; Y is C?O, C?S, SO2, or (CR7R8); m=1 or 2; n=1 or 2; and p=1, 2, 3 or 4, R7 to R17 being as defined in the specification; wherein if —Y—R3 is —C(O)NH(alkyl) then: R1 and/or R2 is selected from heteroaryl; and/or m and/or n is 2; and/or R11 and/or R12 is lower alkyl, or a pharmaceutically acceptable salt or prodrug thereof.Type: ApplicationFiled: April 29, 2004Publication date: July 26, 2007Applicant: VERNALIS RESEARCH LIMITEDInventors: James Davidson, Jonathan Bentley, Claire Dawson, Kerry Harrison, Howard Mansell, Alan Pither, Robert Pratt, Jonathan Roffey, Victoria Ruston
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Patent number: 7208494Abstract: The present invention provides piperazine derivatives of formula (I) as well as pharmaceutically acceptable salts and esters thereof, wherein R1 to R5 have the significance given in the description. They can be used for the treatment of obesity.Type: GrantFiled: June 25, 2004Date of Patent: April 24, 2007Assignees: Hoffmann-La Roche Inc., Vernalis Research LimitedInventors: Toby Jonathan Blench, Paul Hebeisen, Hans Richter, Stephan Roever
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Patent number: 7173056Abstract: 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 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 apnea,Type: GrantFiled: April 29, 2005Date of Patent: February 6, 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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Patent number: 7166632Abstract: 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