Patents by Inventor Alastair David Graham Donald
Alastair David Graham Donald has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).
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Publication number: 20240132485Abstract: The present invention relates to compounds with the ability to stimulate/induce ubiquitination of a target protein/target proteins. The compounds of the present invention may stimulate/induce ubiquitination of a target protein/target proteins; i.e. via degradation of a target protein/target proteins by the cullin-RING ubiquitin ligase (CRL). Such target protein/target proteins may be proteins involved in diseases, like cancer, metabolic disorder, infectious disease and/or neurological disorder. The invention also relates to the compounds and composition for use as medicaments as well as pharmaceutical compositions comprising these compounds. Particularly, the compounds of the present invention may degrade proteins associated with cancer, metabolic disorder, infectious disease and/or neurological disorder.Type: ApplicationFiled: October 15, 2021Publication date: April 25, 2024Inventors: Georg WINTER, Cristina MAYOR RUIZ, Stefan KUBICEK, Alastair David Graham DONALD, Grasilda ZENKEVICIUTE
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Patent number: 9725407Abstract: Compounds of formula (I) inhibit HDAC activity: wherein A, B and D independently represent ?C— or ?N—; W is a divalent radical —CH?CH— or CH2CH2—; R1 is an ester group; R2 is the side chain of a natural or non-natural alpha-amino acid; z is 0 or 1; and Y, L1, and X1 are as defined in the claims.Type: GrantFiled: January 22, 2016Date of Patent: August 8, 2017Assignee: GlaxoSmithKline Intellectual Property Development LimitedInventors: Alan Hornsby Davidson, David Festus Charles Moffat, Francesca Ann Day, Alastair David Graham Donald
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Enzyme and receptor modulation using covalent conjugates of alpha,alpha-disubstituted glycine esters
Patent number: 9636409Abstract: Covalent conjugates of an ?,?-disubstituted glycine ester and a modulator of the activity of a target intracellular enzyme or receptor, wherein the ester group of the conjugate is hydrolysable by one or more intracellular carboxylesterase enzymes to the corresponding acid and the ?,?-disubstituted glycine ester is conjugated to the modulator at a position remote from the binding interface between the inhibitor and the target enzyme or receptor pass into cells and the active acid hydrolysis product accumulates within the cells, as in the following compound:Type: GrantFiled: February 8, 2016Date of Patent: May 2, 2017Assignee: GlaxoSmithKline Intellectual Property Development LimitedInventors: Alan Hastings Drummond, Alan Hornsby Davidson, David Festus Charles Moffat, Alastair David Graham Donald, Stephen John Davies -
Publication number: 20160193200Abstract: The invention provides a compound which is (a) a phenylamide derivative of formula (I) or a tautomer thereof, or (b) a pharmaceutically acceptable salt, N-oxide, hydrate, prodrug or solvate thereof: wherein R1, R2, R3, R4, R5, R6 and R7 are as defined herein. The compounds are useful in the treatment of diseases mediated by HSP90.Type: ApplicationFiled: March 17, 2016Publication date: July 7, 2016Inventors: Alastair David Graham Donald, Joanne McDermott, Sanjay Ratilal Patel, David Festus Charles Moffat
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Publication number: 20160151509Abstract: Covalent conjugates of an ?,?-disubstituted glycine ester and a modulator of the activity of a target intracellular enzyme or receptor, wherein the ester group of the conjugate is hydrolysable by one or more intracellular carboxylesterase enzymes to the corresponding acid and the ?,?-disubstituted glycine ester is conjugated to the modulator at a position remote from the binding interface between the inhibitor and the target enzyme or receptor pass into cells and the active acid hydrolysis product accumulates within the cells.Type: ApplicationFiled: February 8, 2016Publication date: June 2, 2016Inventors: Alan Hastings Drummond, Alan Hornsby Davidson, David Festus Charles Moffat, Alastair David Graham Donald, Stephen John Davies, Margaret Struthers Drummond
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Publication number: 20160137594Abstract: Compounds of formula (I) inhibit HDAC activity: wherein A, B and D independently represent ?C— or ?N—; W is a divalent radical —CH?CH— or CH2CH2—; R1 is an ester group; R2 is the side chain of a natural or non-natural alpha-amino acid; z is 0 or 1; and Y, L1, and X1 are as defined in the claims.Type: ApplicationFiled: January 22, 2016Publication date: May 19, 2016Inventors: Alan Hornsby DAVIDSON, David Festus Charles MOFFAT, Francesca Ann DAY, Alastair David Graham DONALD
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Patent number: 9321718Abstract: The invention provides a compound which is (a) a phenylamide derivative of formula (I) or a tautomer thereof, or (b) a pharmaceutically acceptable salt, N-oxide, hydrate, prodrug or solvate thereof: wherein R1, R2, R3, R4, R5, R6 and R7 are as defined herein. The compounds are useful in the treatment of diseases mediated by HSP90.Type: GrantFiled: June 10, 2011Date of Patent: April 26, 2016Assignee: CHROMA THERAPEUTICS LTD.Inventors: Alastair David Graham Donald, Joanne McDermott, Sanjay Ratilal Patel, David Festus Charles Moffat
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Patent number: 9273003Abstract: Compounds of formula (I) inhibit HDAC activity: wherein A, B and D independently represent ?C— or ?N—; W is a divalent radical —CH?CH— or CH2CH2—; R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular carboxyesterase enzymes to a carboxylic acid group; R2 is the side chain of a natural or non-natural alpha amino acid; z is 0 or 1; and Y, L1, and X1 are as defined in the claims.Type: GrantFiled: July 7, 2014Date of Patent: March 1, 2016Assignee: GlaxoSmithKline Intellectual Property Development LimitedInventors: Alan Hornsby Davidson, David Festus Charles Moffat, Francesca Ann Day, Alastair David Graham Donald
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Patent number: 9133104Abstract: Compounds of formula (I) are inhibitors of histone deacetylase activity, and are useful in the treatment of, for example, cancers, wherein R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular carboxyesterase enzymes to a carboxylic acid group; R2 is the side chain of a natural or non-natural alpha amino acid; Y is a bond, —C(?O), —S(?O)2—, —C(?O)O—, —C(O)NR3—, —C(?S)—NR3, —C(?NH)NR3 or —S(?O)2NR3— wherein R3 is hydrogen or optionally substituted C1-C6 alkyl; L1 is a divalent radical of formula -(Alk1)m(Q)n(Alk2)p- wherein m, n and p are independently 0 or 1, Q is (i) an optionally substituted divalent mono- or bicyclic carbocyclic or heterocyclic radical having 5-13 ring members, or (ii), in the case where both m and p are 0, a divalent radical of formula —X2-Q1- or -Q1-X2— wherein X2 is —O—, S— or NRA— wherein RA is hydrogen or optionally substituted C1-C3 alkyl, and Q1 is an optionally substituted divalent mono- or bicyclic carbocyclic or heterocyclic rType: GrantFiled: February 13, 2014Date of Patent: September 15, 2015Assignee: Chroma Therapeutics Ltd.Inventors: Alan Hornsby Davidson, Sanjay Ratilal Patel, Francesca Ann Mazzei, Stephen John Davies, Alan Hastings Drummond, David Festus Charles Moffat, Kenneth William John Baker, Alastair David Graham Donald
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Publication number: 20140323531Abstract: Compounds of formula (I) inhibit HDAC activity: wherein A, B and D independently represent ?C— or ?N—; W is a divalent radical —CH?CH— or CH2CH2—; R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular carboxyesterase enzymes to a carboxylic acid group; R2 is the side chain of a natural or non-natural alpha amino acid; z is 0 or 1; and Y, L1, and X1 are as defined in the claims.Type: ApplicationFiled: July 7, 2014Publication date: October 30, 2014Inventors: Alan Hornsby DAVIDSON, David Festus Charles Moffat, Francesca Ann Day, Alastair David Graham Donald
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Publication number: 20140163042Abstract: Compounds of formula (I) are inhibitors of histone deacetylase activity, and are useful in the treatment of, for example, cancers, wherein R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular carboxyesterase enzymes to a carboxylic acid group; R2 is the side chain of a natural or non-natural alpha amino acid; Y is a bond, —C(?O), —S(?O)2—, —C(?O)O—, —C(O)NR3—, —C(?S)—NR3, —C(?NH)NR3 or —S(?O)2NR3— wherein R3 is hydrogen or optionally substituted C1-C6 alkyl; L1 is a divalent radical of formula -(Alk1)m(Q)n(Alk2)p- wherein m, n and p are independently 0 or 1, Q is (i) an optionally substituted divalent mono- or bicyclic carbocyclic or heterocyclic radical having 5-13 ring members, or (ii), in the case where both m and p are 0, a divalent radical of formula —X2-Q1- or -Q1-X2— wherein X2 is —O—, S— or NRA— wherein RA is hydrogen or optionally substituted C1-C3 alkyl, and Q1 is an optionally substituted divalent mono- or bicyclic carbocyclic or heterocyclic rType: ApplicationFiled: February 13, 2014Publication date: June 12, 2014Applicant: Chroma Therapeutics Ltd.Inventors: Alan Hornsby Davidson, Sanjay Ratilal Patel, Francesca Ann Mazzei, Stephen John Davies, Alan Hastings Drummond, David Festus Charles Moffat, Kenneth William John Baker, Alastair David Graham Donald
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Publication number: 20140155439Abstract: Compounds of formula (I), inhibit HDAC activity: wherein A, B and D independently represent ?CH— or ?N—; W is —CH?CH— Or —CH2CH2—; R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular carboxylesterase enzymes to a carboxylic acid group; R2 and R3 are selected from the side chains of a natural or non-natural alpha amino acid, provided that neither R2 nor R3 is hydrogen, or R2 and R3, taken together with the carbon to which they are attached, form a 3-6 membered saturated cycloalkyl or heterocyclyl ring; Y is a bond, —C(C?O)—, —S(?O)2—, —C(C?O)O—, —C(C?O)NR?—, —C(?S)—NR?, —C(?NH)NR? or —S(?O)2NR— wherein R? is hydrogen or optionally substituted C1-C6 alkyl; L1 is a divalent radical of formula -(Alk1)m(Q)(Alk2)p— wherein in, n, p, Q, AIk1 and AIk2 are as defined in the claims; X1 represents a bond; —C(?O); or —S(?O)2—; —NR4C(?O)—, —C(C?O)NR4—, —NR4C(?O)NR5—, —NR4S(?O)2—, or —S(?O)2NR4— wherein R4 and R5 are independently hydrogen or optionally substituted C1Type: ApplicationFiled: February 7, 2014Publication date: June 5, 2014Applicant: Chroma Therapeutics Ltd.Inventors: Alastair David Graham Donald, David Festus Charles Moffat, Andrew James Belfield, Carl Leslie North, Stewart Andrew Wayne Jones
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Publication number: 20140088159Abstract: Covalent conjugates of an ?,?-disubstituted glycine ester and a modulator of the activity of a target intracellular enzyme or receptor, wherein the ester group of the conjugate is hydrolysable by one or more intracellular carboxylesterase enzymes to the corresponding acid and the ?,?-disubstituted glycine ester is conjugated to the modulator at a position remote from the binding interface between the inhibitor and the target enzyme or receptor pass into cells and the active acid hydrolysis product accumulates within the cells.Type: ApplicationFiled: November 27, 2013Publication date: March 27, 2014Applicant: Chroma Therapeutics Ltd.Inventors: Alan Hastings Drummond, Alan Hornsby Davidson, David Festus Charles Moffat, Alastair David Graham Donald, Stephen John Davies
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Publication number: 20130303576Abstract: Compounds of formula (I), inhibit HDAC activity: wherein A, B and D independently represent ?CH— or ?N—; W is —CH?CH—Or —CH2CH2—; R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular carboxylesterase enzymes to a carboxylic acid group; R2 and R3 are selected from the side chains of a natural or non-natural alpha amino acid, provided that neither R2 nor R3 is hydrogen, or R2 and R3, taken together with the carbon to which they are attached, form a 3-6 membered saturated cycloalkyl or heterocyclyl ring; Y is a bond, —C(?O)—, —S(?O)2—, —C(?O)O—, —C(?O)NR?—, —C(?S)—NR?, —C(?NH)NR? or —S(?O)2NR— wherein R? is hydrogen or optionally substituted C1-C6 alkyl; L1 is a divalent radical of formula -(Alk1)m(Q)n(Alk2)p- wherein m, n, p, Q.Type: ApplicationFiled: July 19, 2013Publication date: November 14, 2013Inventors: Alastair David Graham Donald, David Festus Charles Moffat, Andrew James Belfield, Carl Leslie North, Stewart Andrew Wayne Jones
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Publication number: 20130143926Abstract: The invention provides a compound which is (a) a phenylamide derivative of formula (I) or a tautomer thereof, or (b) a pharmaceutically acceptable salt, N-oxide, hydrate, prodrug or solvate thereof: wherein R1, R2, R3, R4, R5, R6 and R7 are as defined herein. The compounds are useful in the treatment of diseases mediated by HSP90.Type: ApplicationFiled: June 10, 2011Publication date: June 6, 2013Inventors: Alastair David Graham Donald, Joanne McDermott, Sanjay Ratilal Patel, David Festus Charles Moffat
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Publication number: 20120149736Abstract: Compounds of formula (I), inhibit HDAC activity: wherein A, B and D independently represent ?CH— or ?N—; W is —CH?CH— Or —CH2CH2—; R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intra-cellular carboxylesterase enzymes to a carboxylic acid group; R2 and R3 are selected from the side chains of a natural or non-nat-ural alpha amino acid, provided that neither R2 nor R3 is hydrogen, or R2 and R3, taken together with the carbon to which they are attached, form a 3-6 membered saturated cycloalkyl or heterocyclyl ring; Y is a bond, —C(?O)—, —S(?O)2—, —C(?O)O—, —C(?O)NR?—, —C(?5)—NR?, —C(?NH)NR? or —S(?O)2NR — wherein R? is hydrogen or optionally substituted C1—C6 alkyl; L1 is a divalent radical of formula —(Alk1)m,(Q)n(Alk2)p— wherein m, n, p, Q, Alk1 and Alk2 are as defined in the claims; X1 represents a bond; —C(?O); or —S(?O)2—; —NR4C(?O)—, —C(?O)NR4—,— NR4C(?O)NR5—, —NR4S(?O)2—, or —S(?O)2NR4— wherein R4 and R5 are independently hydrogen or optionally substituted C1Type: ApplicationFiled: February 25, 2010Publication date: June 14, 2012Applicant: Chroma Therapeutics Ltd.Inventors: Alastair David Graham Donald, David Festus Charles Moffat, Andrew James Belfield, Carl Leslie North, Stewart Andrew Wayne Jones
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Publication number: 20100010010Abstract: Compounds of formula (I) inhibit HDAC activity, wherein A, B and D independently represent ?C— or ?N—; W is a divalent radical —CH?CH— or CH2CH2—; R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular carboxyesterase enzymes to a carboxylic acid group; R2 is the side chain of a natural or non-natural alpha amino acid; z is 0 or 1; and Y, L1, and X1 are as defined in the claims.Type: ApplicationFiled: September 14, 2007Publication date: January 14, 2010Applicant: CHROMA THERAPEUTICS LTD.Inventors: Alan Hornsby Davidson, David Festus Charles Moffat, Francesca Ann Day, Alastair David Graham Donald