Patents Assigned to Vernalis (Cambridge) Limited
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Publication number: 20120252797Abstract: Isoxazoles of formula (A) or (B) wherein R1 is a group of formula (IB) The isoxazoles are inhibitors of HSP90 activity, and useful for the treatment of, for example, cancers.Type: ApplicationFiled: June 18, 2012Publication date: October 4, 2012Applicants: Vernalis (Cambridge) Limited, The Institute of Cancer Research, Cancer Research Technology Ltd.Inventors: Martin James Drysdale, Brian William Dymock, Harry Finch, Paul Webb, Edward McDonald, Karen Elizabeth James, Kwai Ming Cheung, Thomas Peter Matthews
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Publication number: 20110034457Abstract: The use of compounds of formula (I) in therapy, particularly for the treatment of a disorder mediated by excessive or inappropriate HSP90 activity formula (I), wherein R2 is a group of formula (IA): —(Ar1)m-(Alk1)p-(Z)r-(Alk2)S-Q??(IA) Ar1, Alk1, Z, Alk2 and Q being as defined in the specification; m, p, r and s are independently 0 or 1; R3 is hydrogen, an optional substituent, or an optionally substituted (C1-C6)alkyl, aryl or heteroaryl radical; and R4 is a carboxylic ester, carboxamide or sulfonamide group; or a salt, N-oxide, hydrate, or solvate thereof.Type: ApplicationFiled: October 21, 2010Publication date: February 10, 2011Applicant: VERNALIS (CAMBRIDGE) LIMITED.Inventors: Martin James Drysdale, Brian William Dymock, Xavier Barril-Alonso
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Patent number: 7820658Abstract: Compounds of formula (1) are inhibitors of HSP90 activity in vitro or in vivo, and of use in the treatment of inter alia, Cancer: wherein R2 is a group of formula —(Ar1)m-(Alk1)P-(Z)r-(Alk 2)S-Q wherein Ar1 is an optionally substituted aryl or heteroaryl radical, Alk? and Alk 2 are optionally substituted divalent C1-C3 alkylene or C2-C3 alkenylene radicals, m, p, r and s are independently 0 or 1, Z is —O—, —S—, —(C?O)—, —(C?S)—, —SO2—, —C(?O)O—, —C(?O)NRA—, —C(?S)NRA—, —SO2NRA—, —NRAC(?O)_, —NRASO2- or —NRA—wherein RA is hydrogen or C1-C6 alkyl, and Q is hydrogen or an optionally substituted carbocyclic or heterocyclic radical; R3 is hydrogen, an optional substituent, or an optionally substituted (C1-C6)alkyl, aryl or heteroaryl radical; and R4 is a carboxylic ester, carboxamide or sulfonamide group.Type: GrantFiled: August 26, 2004Date of Patent: October 26, 2010Assignees: Vernalis (Cambridge) Limited, Cancer Research Technology Ltd., Institute Of Cancer ResearchInventors: Brian William Dymock, Martin James Drysdale, Christofe Fromont, Allan Jordan, Xavier Barril-Alonso
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Patent number: 7803831Abstract: Compounds of formula (IA) or (IB) or salts, N-oxides, hydrates or solvates thereof are Inhibitors of HSP90, and useful in the treatment of, for example, cancer: formula (IA), formula (IB) wherein Ar is an aryl or heteroaryl radical which is linked via a ring carbon, and which is substituted by a hydroxy group on a carbon in the 2-position, and which is otherwise either unsubstituted or optionally substituted; R1 is hydrogen or optionally substituted C1-C6 alkyl; R2 is hydrogen, optionally substituted cycloalkyl, cycloalkenyl, C1-C6 alkyl, C1-C6alkenyl, or C1-C6 alkynyl; or a carboxyl, carboxamide or carboxyl ester group; and R3 is a carboxamide group.Type: GrantFiled: December 4, 2003Date of Patent: September 28, 2010Assignees: Vernalis (Cambridge) Limited, Cancer Research Technology Ltd., Institute Of Cancer ResearchInventors: Mandy Christine Beswick, Paul Andrew Brough, Martin James Drysdale, Brian William Dymock
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Publication number: 20100179138Abstract: Isoxazoles of formula (A) or (B) are inhibitors of HSP90 activity, and useful for treatment of, for example cancers: wherein R1, is a group of formula (IA): —Ar1-(Alk1)p-(Z)r-(Alk2)s-Q, wherein in any compatible combination Ar1 is an optionally substituted aryl or heteroaryl radical, Alk1 and Alk2 are optionally substituted divalent C1-C6 alkylene or C2-C6 alkenylene radicals, p, r and s are independently 0 or 1, Z is -0-, —S—, —(C?O)—, —(C?S)—, —SO.sub.Type: ApplicationFiled: February 19, 2010Publication date: July 15, 2010Applicants: Vernalis (Cambridge) Limited, Cancer Research Technology Ltd., The Institute Of Cancer ResearchInventors: Martin James Drysdale, Brian William Dymock, Harry Finch, Paul Webb, Edward McDonald, Karen Elizabeth James, Kwai Ming Cheung, Thomas Peter Matthews
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Patent number: 7728016Abstract: Compound of a compound of formula (I) or a salt, N-oxide, hydrate or solvate thereof, in the preparation of a composition for inhibition of HSP90 activity: wherein ring A is an aromatic or non-aromatic carbocyclic or heterocyclic ring having 5 ring atoms, for example 1,2,3-triazolyl or a 1,2,4-triazolyl or a tetrazolyl ring; and R1 R2 R3 are as defined in the specification are inhibitors of HSP90 and therefore of use in the treatment of, for example, cancers, viral disease, inflammatory diseases such as rheumatoid arthritis, asthma, multiple sclerosis, Type I diabetes, lupus, psoriasis and inflammatory bowel disease; cystic fibrosis angiogenesis-related disease such as diabetic retinopathy, haemangiomas, and endometriosis; or for protection of normal cells against chemotherapy-induced toxicity; or diseases where failure to undergo apoptosis is an underlying factor, or protection from hypoxia-ischemic injury due to elevation of Hsp70 in the heart and brain; scrapie/CJD, Huntingdon's and Alzheimer's disease.Type: GrantFiled: June 24, 2004Date of Patent: June 1, 2010Assignees: Vernalis (Cambridge) Limited, Cancer Research Technology Ltd., Institute of Cancer ResearchInventors: Kwai Ming Cheung, Brian William Dymock, Edward McDonald, Martin James Drysdale
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Publication number: 20100120767Abstract: Compounds of formula (1) are inhibitors of HSP90 activity in vitro or in vivo, and of use in the treatment of inter alia, cancer: wherein R2 is a group of formula —(Ar1)m-(Alk1)P-(Z)r-(Alk2)S-Q wherein Ar1 is an optionally substituted aryl or heteroaryl radical, Alk? and Alk 2 are optionally substituted divalent C1-C3 alkylene or C2-C3 alkenylene radicals, m, p, r and s are independently 0 or 1, Z is -0-, —S—, —(C?O)—, —(C?S)—, -S02-, —C(?O)O—, —C(?O)NRA—, —C(?S)NRA—, -S02NRA—, —NRAC(?O)—, —NRAS02- or —NRA— wherein RA is hydrogen or C1-C6 alkyl, and Q is hydrogen or an optionally substituted carbocyclic or heterocyclic radical; R3 is hydrogen, an optional substituent, or an optionally substituted (C1-C6)alkyl, aryl or heteroaryl radical; and R4 is a carboxylic ester, carboxamide or sulfonamide group.Type: ApplicationFiled: January 21, 2010Publication date: May 13, 2010Applicants: Vernalis (Cambridge) Limited, Cancer Research Technology Ltd., The Institute of Cancer ResearchInventors: Brian William Dymock, Martin James Drysdale, Christofe Fromont, Allan Jordan, Xavier Barril-Alonso
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Patent number: 7705027Abstract: Isoxazoles of formula (A) or (B) are inhibitors of HSP90 activity, and useful for treatment of, for example cancers: (A), (B) wherein R1, is a group of formula (IA): —Ar1-(Alk1)p-(Z)r-(Alk2)s-Q, wherein in any compatible combination Ar1 is an optionally substituted aryl or heteroaryl radical, Alk1 and Alk2 are optionally substituted divalent C1-C6 alkylene or C2-C6 alkenylene radicals, p, r and s are independently 0 or 1, Z is —O—, —S—, —(C?O)—, —(C?S)—, —SO2—, —C(?O)O—, —C(?O)NRA—, —C(?S)NRA—, —SO2NRA—, —NRAC(?O)—, —NRASO2— or —NRA— wherein RA is hydrogen or C1-C6 alkyl, and Q is hydrogen or an optionally substituted carbocyclic or heterocyclic radical; R2 is (i) a group of formula (IA) above or (ii) a carboxamide radical; or (iii) a non aromatic carbocyclic or heterocyclic ring wherein a ring carbon is optionally substituted, and/or a ring nitrogen is optionally substituted by a group of formula -(Alk1)p-(Z)r-(Alk2)s-Q wherein Q, Alk1, Alk2, Z, p, r and s are as defined above in relation to group (IA); andType: GrantFiled: February 9, 2004Date of Patent: April 27, 2010Assignees: Vernalis (Cambridge) Limited, Cancer Research Technology Limited, Institute Of Cancer ResearchInventors: Martin James Drysdale, Brian William Dymock, Harry Finch, Paul Webb, Edward McDonald, Karen Elizabeth James, Kwai Ming Cheung, Thomas Peter Matthews
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Patent number: 7632855Abstract: Compounds of formula (I) are inhibitors of HSP90 activity, and useful in the treatment of proliferative disease such as cancers: wherein R1, R2 and R3 are as defined in the specification, and X is —OR4 or —NR4R5 wherein R4 and R5 independently represent hydrogen or optionally substituted C1-C6 alkyl, or R4 and R5 taken together with the nitrogen to which they are attached form an optionally substituted nitrogen-containing ring having 5-8 ring atoms.Type: GrantFiled: April 23, 2004Date of Patent: December 15, 2009Assignees: Vernalis (Cambridge) Limited, Cancer Research Technology, The Institute of CancerInventors: Xavier Barrilalonso, Brian William Dymock, Martin James Drysdale
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Patent number: 7612201Abstract: Compounds of formula (IA) or (IB) or a salt, N-oxide, hydrate or solvate thereof are inhibitors of HSP90, and are of value in the treatment of diseases responsive to HSP90 inhibition such as cancers.Type: GrantFiled: December 18, 2003Date of Patent: November 3, 2009Assignees: Vernalis (Cambridge) Limited, Cancer Research Technology Ltd., The Institute of Cancer ResearchInventors: Mandy Christine Beswick, Martin James Drysdale, Brian William Dymock, Edward McDonald
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Publication number: 20090069336Abstract: Compounds of formula (I) are inhibitors of HSP90, and useful in the treatment of, for example, cancers: wherein R2 is a group of formula (IA): -(Ar1)m-(Alk1)p-(Z)r-(Alk2)s-Q??(IA) wherein in any compatible combination Ar1 is an optionally substituted aryl or heteroaryl radical, Alk1 and Alk2 are optionally substituted divalent C1-C3 alkylene or C2-C3 alkenylene radicals, m, p, r and s are independently 0 or 1, Z is —O—, —S—, —(C?O)—, —(C?S)—, —SO2—, —C(?O)O—, —C(?O)NRA—, —C(?S)NRA—, —SO2NRA—, —NRAC(?O)—, —NRASO2— or —NRA— wherein RA is hydrogen or C1-C6 alkyl, and Q is hydrogen or an optionally substituted carbocyclic or heterocyclic radical; R3 is hydrogen, an optional substituent, or an optionally substituted (C1-C6)alkyl, aryl or heteroaryl radical; and R4 is (i) hydrogen, a —CN group, a nitro group —NO2, or a —C(?NOH)(NH2) group, or (ii) an optionally substituted C1-C6alkyl, aryl, heterocyclic, aryl(C1-C6alkyl)-, or heterocyclic(C1-C6alkyl)- group, or (iii) a group of formula —C(?O)R5 wherein R5 isType: ApplicationFiled: July 18, 2005Publication date: March 12, 2009Applicants: VERNALIS (CAMBRIDGE) LIMITED., CANCER RESEARCH TECHNOLOGY LTD., THE INSTITUTE OF CANCER RESEARCHInventors: Xavier Barril-Alonso, Paul Andrew Brough, Martin James Drysdale, Paul Webb
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Publication number: 20070275961Abstract: Compounds of formula (IA) or (AB) are kinase inhibitors, especially of CDK2, and/or PDK1 and/or CHK1: wherein Ring A is an optionally substituted aryl, heteroaryl, carbocyclic or heterocyclic radical, Alk represents an optionally substituted clivaient C1-C6 alkylene radical; n is 0 or 1; Q represents a radical of formula -(Alk1)p-(X),(Alk2)s-Z wherein in any compatible combination Z is hydrogen or an optionally substituted carbocyclic or heterocyclic ring, p, r and s are 0 or 1, and Alk1, Alk2, X, are as described in the specification, and R1 represents a radical 3 4 3 (CYC)k-(Alk3)a-(Y)b-(Alk4)d-B wherein k, a, b and d are 0 or 1, and Cyc, Alk3, Alk4 and B are as described in the specification.Type: ApplicationFiled: June 2, 2004Publication date: November 29, 2007Applicant: VERNALIS (CAMBRIDGE) LIMITED.Inventors: Justin Bower, Andrew Cansfield, Allan Jordan, Martin Parratt, Lee Walmsley, Douglas Williamson
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Publication number: 20070213328Abstract: The use of compounds of formula (I) in therapy, particularly for the treatment of a disorder mediated by excessive or inappropriate HSP90 activity formula (I), wherein R2 is a group of formula (IA): -(Ar1)m-(Alk1)p-(Z)r-(Alk2)s-Q (IA) Ar1, Alk1, Z, Alk2 and Q being as defined in the specification; m, p, r and s are independently 0 or 1; R3 is hydrogen, an optional substituent, or an optionally substituted (C1-C6)alkyl, aryl or heteroaryl radical; and R4 is a carboxylic ester, carboxamide or sulfonamide group; or a salt, N-oxide, hydrate, or solvate thereof.Type: ApplicationFiled: October 5, 2004Publication date: September 13, 2007Applicant: Vernalis (Cambridge) LimitedInventors: Martin Drysdale, Brian Dymock, Xavier Barril-Alonso
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Publication number: 20070179161Abstract: Compounds of formula (I) or salts, N-oxides, hydrates or solvates thereof are inhibitors of kinase activity, and useful for the treatment of, for example, cancer, psoriasis or restenosis: wherein ring A is an optionally substituted carbocyclic or heterocyclic radical. Alk represents an optionally substituted divalent C1-C6 alkylene radical. n is 0 or 1. Q represents a radical of formula -(Alk1)p (X)r-(Alk2)s-Z wherein in any compatible combination Z is hydrogen or an optionally substituted carbocyclic or heterocyclic ring; Alk1 and Alk2 are optionally substituted divalent C1-C6 alkylene radicals which may contain a —O—, —S— or —NRA— link, wherein RA is hydrogen or C1-C6 alkyl; X represents —O—, —S—, —(C?O)—, —(C?S)—, —SO2—, —SO—, —C(?O)O—, —OC(?O)—, —C(?O)NRA—, —NR AC(?O)—, —C(?S)NRA, —NRAC(?S)—, —SO2NRA—, —NRASO2—, —OC(?O)NRA—, —NRAC(?O)O—, or —NRA— wherein RA is hydrogen or C1-C6 alkyl. p, r and s are independently 0 or 1.Type: ApplicationFiled: March 18, 2004Publication date: August 2, 2007Applicant: VERNALIS (CAMBRIDGE) LIMITED.Inventors: Martin Parratt, Justin Bower, Douglas Williamson, Andrew Cansfield
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Patent number: 7247734Abstract: The present invention pertains to the use of certain 3,4-diarylpyazoles of formula (I), both in vitro and in vivo, to inhibit heat shock protein 90 (HSP90), and in the treatment of conditions mediated by HSP90, including, for example, cancer; wherein: Ar3 is independently: a C5-20aryl group, and is optionally substituted; Ar4 is independently: a C5-20aryl group, and is optionally substituted; R5 is independently: hydrogen; halo; hydroxyl; ether; formyl; acyl; carboxy; ester; acyloxy; oxycarbonyloxy; amido; acylamido; aminocarbonyloxy; tetrazolyl; amino; nitro; cyano; azido; sulfhydryl; thioether; sulfonamide; C1-7alkyl; C3-20heterocycyl; or C5-20aryl; R<SP>N</SP> is independently: —H; C1-7alkyl; C3-20heterocycyl; or, C5-20aryl; and pharmaceutically acceptable salts, solvates, amides, esters, ethers, chemically protected forms, and prodrugs thereof.Type: GrantFiled: December 19, 2002Date of Patent: July 24, 2007Assignees: Vernalis (Cambridge) Limited, Cancer Research Technology Ltd., Institute of Cancer Research of Royal Cancer HospitalInventors: Martin James Drysdale, Brian William Dymock, Xavier Barril-Alonso, Paul Workman, Laurence Harris Pearl, Chrisostomos Prodromou, Edward McDonald
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Publication number: 20070112192Abstract: Compounds of formula (IA) or (IB) or salts, N-oxides. hydrates or solvates thereof are Inhibitors of HSP90, and useful in the treatment of, for example, cancer: formula (IA), formula (IB) wherein Ar is an aryl or heteroaryl radical which is linked via a ring carbon, and which is substituted by a hydroxy group on a carbon in the 2-position, and which is otherwise either unsubstituted or optionally substituted; R1 is hydrogen or optionally substituted C1-C6 alkyl; R2 is hydrogen, optionally substituted cycloalkyl, cycloalkenyl, C1-C6 alkyl, C1-C6alkenyl, or C1-C6 alkynyl; or a carboxyl, carboxamide or carboxyl ester group; and R3 is a carboxamide group.Type: ApplicationFiled: December 4, 2003Publication date: May 17, 2007Applicants: VERNALIS (CAMBRIDGE) LIMITED, CANCER RESEARCH TECHNOLOGY LTD., THE INSTITUTE OF CANCER RESEARCHInventors: Mandy Beswick, Paul Brough, Martin Drysdale, Brian Dymock
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Publication number: 20070072855Abstract: Compounds of formula (I) are inhibitors of HSP90 activity, and useful in the treatment of proliferative disease such as cancers: wherein R1, R2 and R3 are as defined in the specification, and X is —OR4 or —NR4R5 wherein R4 and R5 independently represent hydrogen or optionally substituted C1-C6 alkyl, or R4 and R5 taken together with the nitrogen to which they are attached form an optionally substituted nitrogen-containing ring having 5-8 ring atoms.Type: ApplicationFiled: April 23, 2004Publication date: March 29, 2007Applicants: Vernalis (cambridge) Limited, Cancer Research Technology Ltd, The Institute of Cancer ResearchInventors: Xavier Barrilalonso, Brian Dymock, Martin Drysdale
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Publication number: 20070043044Abstract: Compounds of formula (1) are inhibitors of HSP90 activity in vitro or in vivo, and of use in the treatment of inter alia, cancer wherein R2 is a group of formula —(Ar1)m-(Alk1)P-(Z)r-(Alk2)S-Q wherein Ar1 is an optionally substituted aryl or heteroaryl radical, Alk? and Alk 2 are optionally substituted divalent C1-C3 alkylene or C2-C3 alkenylene radicals, m, p, r and s are independently 0 or 1, Z is —0—, —S—, —(C?O)—, —(C?S)—, —S02-, —C(?O)O—, —C(?O)NRA—, —C(?S)NRA—, —S02NRA—, —NRAC(?O)_, —NRAS02- or —NRA—wherein RA is hydrogen or C1-C6 alkyl, and Q is hydrogen or an optionally substituted carbocyclic or heterocyclic radical; R3 is hydrogen, an optional substituent, or an optionally substituted (C1-C6)alkyl, aryl or heteroaryl radical; and R4 is a carboxylic ester, carboxamide or sulfonamide group.Type: ApplicationFiled: August 26, 2004Publication date: February 22, 2007Applicants: VERNALIS (CAMBRIDGE) LIMITED, CANCER RESEARCH TECHNOLOGY LTD., THE INSTITUTE OF CANCER RESEARCH, BARRIL-ALONSO, Xavier (ES)Inventors: Brian Dymock, Martin Drysdale, Christofe Fromont, Allan Jordan, Xavier Barril-Alonso
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Publication number: 20060235058Abstract: Compound of a compound of formula (1) or a salt, N-oxide, hydrate or solvate thereof, in the preparation of a composition for inhibition of HSP90 activity: wherein ring A is an aromatic or non-aromatic carbocyclic or heterocyclic ring having 5 ring atoms, for example 1,2,3-triazolyl or a 1,2,4-triazolyl or a tetrazolyl ring; and R1 R2 R3 are as defined in the specification are inhibitors of HSP90 and therefore of use in the treatment of, for example, cancers, viral disease, inflammatory diseases such as rheumatoid arthritis, asthma, multiple sclerosis, Type I diabetes, lupus, psoriasis and inflammatory bowel disease; cystic fibrosis angiogenesis-related disease such as diabetic retinopathy, haemangiomas, and endometriosis; or for protection of normal cells against chemotherapy-induced toxicity; or diseases where failure to undergo apoptosis is an underlying factor, or protection from hypoxia-ischemic injury due to elevation of Hsp70 in the heart and brain; scrapie /CJD, Huntingdon's and Alzheimer's disease.Type: ApplicationFiled: June 24, 2004Publication date: October 19, 2006Applicants: Vernalis (Cambridge) Limited, Cancer Research Technology Ltd., The Institute of Cancer ResearchInventors: Kwai Cheung, Brian Dymock, Edward McDonald, Martin Drysdale
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Publication number: 20060148817Abstract: Compounds of formula (IA) or (IB) or a salt, N-oxide, hydrate or solvate thereof are inhibitors of HSP90, and are of value in the treatment of diseases responsive to HSP90 inhibition such as cancers.Type: ApplicationFiled: December 18, 2003Publication date: July 6, 2006Applicants: Vernalis (Cambridge) Limited, Cancer Research Technolgy Technology Ltd., The Institute of Cancer ResearchInventors: Christine Beswick, Martin Drysdale, Brian Dymock, Edward McDonald