Patents by Inventor Stephen John Davies
Stephen John Davies 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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Patent number: 10370332Abstract: The present invention provides a compound which is: tert-butyl N-[2-{4-[6-amino-5-(2,4-difluorobenzoyl)-2-oxopyridin-1(2H)-yl]-3,5-difluorophenyl}ethyl)-L-alaninate or a salt, hydrate or solvate thereof. The present invention also provides a pharmaceutical composition comprising the compound together with one or more pharmaceutically acceptable carriers and/or excipients. The compound and composition are useful for inhibiting the activity of a p38 MAP kinase enzyme. As such they may be used in the treatment of a autoimmune or inflammatory disease, or a cell proliferative disease. In addition, the invention provides an acid produced by hydrolysis of the ester group of the compound of the invention. The acid is N-[2-{4-[6-amino-5-(2,4-difluorobenzoyl)-2-oxopyridin-1(2H)-yl]-3,5-difluorophenyl}ethyl)-L-alanine.Type: GrantFiled: January 3, 2018Date of Patent: August 6, 2019Assignee: Macrophage Pharma LimitedInventors: Stéphane Pintat, Stephen John Davies, David Festus Charles Moffat
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Publication number: 20180127371Abstract: The present invention provides a compound which is: tert-butyl N-[2-{4-[6-amino-5-(2,4-difluorobenzoyl)-2-oxopyridin-1(2H)-yl]-3,5-difluorophenyl}ethyl)-L-alaninate or a salt, hydrate or solvate thereof. The present invention also provides a pharmaceutical composition comprising the compound together with one or more pharmaceutically acceptable carriers and/or excipients. The compound and composition are useful for inhibiting the activity of a p38 MAP kinase enzyme. As such they may be used in the treatment of a autoimmune or inflammatory disease, or a cell proliferative disease. In addition, the invention provides an acid produced by hydrolysis of the ester group of the compound of the invention. The acid is N-[2-{4-[6-amino-5-(2,4-difluorobenzoyl)-2-oxopyridin-1(2H)-yl]-3,5-difluorophenyl}ethyl)-L-alanine.Type: ApplicationFiled: January 3, 2018Publication date: May 10, 2018Applicants: Macrophage Pharma Limited, Macrophage Pharma LimitedInventors: Stéphane Pintat, Stephen John Davies, David Festus Charles Moffat
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Patent number: 9896417Abstract: The present invention provides a compound which is: tert-butyl N-[2-{4-[6-amino-5-(2,4-difluorobenzoyl)-2-oxopyridin-1(2H)-yl]-3,5-difluorophenyl}ethyl)-L-alaninate or a salt, hydrate or solvate thereof. The present invention also provides a pharmaceutical composition comprising the compound together with one or more pharmaceutically acceptable carriers and/or excipients. The compound and composition are useful for inhibiting the activity of a p38 MAP kinase enzyme. As such they may be used in the treatment of a autoimmune or inflammatory disease, or a cell proliferative disease. In addition, the invention provides an acid produced by hydrolysis of the ester group of the compound of the invention. The acid is N-[2-{4-[6-amino-5-(2,4-difluorobenzoyl)-2-oxopyridin-1(2H)-yl]-3,5-difluorophenyl}ethyl)-L-alanine.Type: GrantFiled: June 15, 2016Date of Patent: February 20, 2018Assignee: Macrophage Pharma LimitedInventors: Stéphane Pintat, Stephen John Davies, David Festus Charles Moffat
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Publication number: 20170157118Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt, N-oxide, hydrate or solvate thereof: wherein: ring A, R1, R2, n, X, V, W, Z, ring B, [Linker] and R areas defined herein. The compounds are useful as inhibitors of CSF-1R kinase. The compounds can thus be used in medicine.Type: ApplicationFiled: February 20, 2017Publication date: June 8, 2017Inventors: Stephen John Davies, Stéphane Pintat, Carl Leslie North, David F. C. Moffat
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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 -
Patent number: 9604940Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt, N-oxide, hydrate or solvate thereof: wherein: ring A, R1, R2, n, X, V, W, Z, ring B, [Linker] and R areas defined herein. The compounds are useful as inhibitors of CSF-1R kinase. The compounds can thus be used in medicine.Type: GrantFiled: June 26, 2013Date of Patent: March 28, 2017Assignee: Chroma Therapeutics Ltd.Inventors: Stephen John Davies, Stephane Pintat, Carl Leslie North, David Festus Charles Moffat
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Patent number: 9573016Abstract: An exercise device is formed of inelastic, fixed length, substantially rigid straps connected in a T-shaped configuration so as to define an anchor member and two support members. An anchor loop is fixed to the outer end of the anchor member for securing a weighted member thereon or for securing to various stationary objects. A hand grip is coupled to the outer end of each support member such that the user must exert additional effort during various exercises to maintain proper position of their hands relative to one another.Type: GrantFiled: May 28, 2015Date of Patent: February 21, 2017Assignee: MYT EQUIPMENT INC.Inventors: Sami Ishag Jamil Haddad, Stephen John Davies
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Publication number: 20160297760Abstract: The present invention provides a compound which is: tert-butyl N-[2-{4-[6-amino-5-(2,4-difluorobenzoyl)-2-oxopyridin-1(2H)-yl]-3,5-difluorophenyl}ethyl)-L-alaninate or a salt, hydrate or solvate thereof. The present invention also provides a pharmaceutical composition comprising the compound together with one or more pharmaceutically acceptable carriers and/or excipients. The compound and composition are useful for inhibiting the activity of a p38 MAP kinase enzyme. As such they may be used in the treatment of a autoimmune or inflammatory disease, or a cell proliferative disease. In addition, the invention provides an acid produced by hydrolysis of the ester group of the compound of the invention. The acid is N-[2-{4-[6-amino-5-(2,4-difluorobenzoyl)-2-oxopyridin-1(2H)-yl]-3,5-difluorophenyl}ethyl)-L-alanine.Type: ApplicationFiled: June 15, 2016Publication date: October 13, 2016Inventors: Stéphane Pintat, Stephen John Davies, David Festus Charles Moffat
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Patent number: 9388136Abstract: The present invention provides a compound which is: tert-butyl N-[2-{4-[6-amino-5-(2,4-difluorobenzoyl)-2-oxopyridin-1(2H)-yl]-3,5-difluorophenyl}ethyl)-L-alaninate or a salt, hydrate or solvate thereof. The present invention also provides a pharmaceutical composition comprising the compound together with one or more pharmaceutically acceptable carriers and/or excipients. The compound and composition are useful for inhibiting the activity of a p38 MAP kinase enzyme. As such they may be used in the treatment of a autoimmune or inflammatory disease, or a cell proliferative disease. In addition, the invention provides an acid produced by hydrolysis of the ester group of the compound of the invention. The acid is N-[2-{4-[6-amino-5-(2,4-difluorobenzoyl)-2-oxopyridin-1(2H)-yl]-3,5-difluorophenyl}ethyl)-L-alanine.Type: GrantFiled: October 15, 2013Date of Patent: July 12, 2016Assignee: Chroma Therapeutics LtdInventors: Stéphane Pintat, Stephen John Davies, 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: 20160016032Abstract: An exercise device is formed of inelastic, fixed length, substantially rigid straps connected in a T-shaped configuration so as to define an anchor member and two support members. An anchor loop is fixed to the outer end of the anchor member for securing a weighted member thereon or for securing to various stationary objects. A hand grip is coupled to the outer end of each support member such that the user must exert additional effort during various exercises to maintain proper position of their hands relative to one another.Type: ApplicationFiled: May 28, 2015Publication date: January 21, 2016Inventors: Sami Ishag Jamil Haddad, Stephen John Davies
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Publication number: 20150368210Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt, N-oxide, hydrate or solvate thereof: wherein: ring A, R1, R2, n, X, V, W, Z, ring B, [Linker] and R areas defined herein. The compounds are useful as inhibitors of CSF-1R kinase. The compounds can thus be used in medicine.Type: ApplicationFiled: June 26, 2013Publication date: December 24, 2015Applicant: Chroma Therapeutics Ltd.Inventors: Stephen John Davies, Stephane Pintat, Carl Leslie North, David Festus Charles Moffat
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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: 20150246883Abstract: The present invention provides a compound which is: tert-butyl N-[2-{4-[6-amino-5-(2,4-difluorobenzoyl)-2-oxopyridin-1(2H)-yl]-3,5-difluorophenyl}ethyl)-L-alaninate or a salt, hydrate or solvate thereof. The present invention also provides a pharmaceutical composition comprising the compound together with one or more pharmaceutically acceptable carriers and/or excipients. The compound and composition are useful for inhibiting the activity of a p38 MAP kinase enzyme. As such they may be used in the treatment of a autoimmune or inflammatory disease, or a cell proliferative disease. In addition, the invention provides an acid produced by hydrolysis of the ester group of the compound of the invention. The acid is N-[2-{4-[6-amino-5-(2,4-difluorobenzoyl)-2-oxopyridin-1(2H)-yl]-3,5-difluorophenyl}ethyl)-L-alanine.Type: ApplicationFiled: October 15, 2013Publication date: September 3, 2015Applicant: CHROMA THERAPEUTICS LTD.Inventors: Stéphane Pintat, Stephen John Davies, David Festus Charles Moffat
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Patent number: 8778953Abstract: Compounds of formula (I) are p38 MAP kinase inhibitors useful for the treatment of autoimmune and inflammatory diseases: wherein: G is —N? or —CH?; D is an optionally substituted divalent mono- or bi-cyclic aryl or heteroaryl radical having 5-13 ring members; R6 is hydrogen or optionally substituted CrC3 alkyl; P represents hydrogen and U represents a radical of formula (IA); or U represents hydrogen and P represents a radical of formula (IA); wherein A represents an optionally substituted divalent mono- or bicyclic carbocyclic or heterocyclic radical having 5-13 ring members; z is O or 1; —X1-L1-Y— is a linker radical or bond; R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular esterase enzymes to a carboxylic acid group; and R2 and R3 are as defined in the claims.Type: GrantFiled: February 27, 2009Date of Patent: July 15, 2014Assignee: Chroma Therapeutics Ltd.Inventors: David Festus Charles Moffat, Stephen John Davies, Stephane Pintat
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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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Patent number: 8686032Abstract: Compounds of formula (I) are inhibitors of histone deacetylase activity, and are useful in the treatment of, for example, cancers:Type: GrantFiled: December 1, 2010Date of Patent: April 1, 2014Assignee: Chroma Therapeutics Ltd.Inventors: Alan Hornsby Davidson, Sanjay Ratilal Patel, Francesca Ann Mazzei, Stephen John Davies, Alan Hastings Drummond, David Festus Moffat, Kenneth William John Baker, Alistair David Graham Donald
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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: 20130116318Abstract: Compounds of formula (I) are inhibitors of histone deacetylase activity, and are useful in the treatment of, for example, cancers:Type: ApplicationFiled: December 1, 2010Publication date: May 9, 2013Applicant: Chroma Therapeutics Ltd.Inventors: Alan Hornsby Davidson, Sanjay Ratilal Patel, Francesca Ann Mazzei, Stephen John Davies, Alan Hastings Drummond, David Festus Moffat, Kenneth William John Baker, Alistair David Graham Donald
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Publication number: 20120289382Abstract: An exercise device is formed of inelastic, fixed length, substantially rigid straps connected in a Y-shaped configuration so as to define an anchor member and two support members. An anchor loop is fixed to the outer end of the anchor member for securing a weighted member thereon or for securing to various stationary objects. A hand grip is coupled to the outer end of each support member such that the user must exert additional effort during various exercises to maintain proper position of their hands relative to one another.Type: ApplicationFiled: May 9, 2012Publication date: November 15, 2012Inventors: Sami Ishag Jamil Haddad, Stephen John Davies