Patents by Inventor Bernard Golding
Bernard Golding 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: 20230192642Abstract: Described herein are isotopically enriched analogs of methylone (e.g., deuterated analogs of methylone (e.g., (S)-methylone and (R)-methylone) with improved characteristics. Also described herein are salts (such as hydrochloride salt) and solid forms (e.g., crystalline forms) of methylone. Also described herein are stereoisomers (e.g., enantiomers) of methylone. The present disclosure also provides methods of making and methods of use of the methylone or methylone analogs and solid forms of 3,4-methylenedioxy-N-ethylcathinone hydrochloride described herein to treat brain and neurological disorders such as depression.Type: ApplicationFiled: December 28, 2022Publication date: June 22, 2023Inventors: Matthew DUNCTON, Samuel CLARK, Alistair HENDERSON, Bernard GOLDING, Manuel MONERRIS MASCARO, Lucia JOHNSON, Annette MADRID
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Patent number: 10344017Abstract: The invention provides compounds of formula (I) or a tautomer, stereoisomer, N-oxide, pharmaceutically acceptable salt or solvate thereof. The compounds are useful for the prophylaxis or treatment of a disease state or condition mediated by ERK5, in particular cancers.Type: GrantFiled: September 18, 2015Date of Patent: July 9, 2019Inventors: Tristan Reuillon, Duncan Miller, Stephanie Myers, Lauren Molyneux, Celine Cano, Ian Hardcastle, Roger Griffin, Laurent Rigoreau, Bernard Golding, Martin Noble
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Publication number: 20180170911Abstract: The invention provides compounds of formula (I) or a tautomer, stereoisomer, N-oxide, pharmaceutically acceptable salt or solvate thereof. The compounds are useful for the prophylaxis or treatment of a disease state or condition mediated by ERK5, in particular cancers.Type: ApplicationFiled: September 18, 2015Publication date: June 21, 2018Applicant: CANCER RESEARCH TECHNOLOGY LIMITEDInventors: Tristan REUILLON, Duncan MILLER, Stephanie MYERS, Lauren MOLYNEUX, Celine CANO, Ian HARDCASTLE, Roger GRIFFIN, Laurent RIGOREAU, Bernard GOLDING, Martin NOBLE
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Patent number: 8530651Abstract: The present invention relates to a novel process for producing quinazoline compounds which are useful in therapy. More specifically, the compounds produced by the process of the invention are useful in the treatment of a number of cardiovascular diseases. The process of the invention provides 6,7-dichloro-1,5-dihydroimidazo[2,1-b]quinazolin 2(3H)-one, more commonly known as anagrelide and its analogues in a clean and efficient manner.Type: GrantFiled: November 30, 2009Date of Patent: September 10, 2013Assignee: Shire LLCInventor: Bernard Golding
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Publication number: 20110263850Abstract: The present invention relates to a novel process for producing quinazoline compounds which are useful in therapy. More specifically, the compounds produced by the process of the invention are useful in the treatment of a number of cardiovascular diseases. The process of the invention provides 6,7-dichloro-1,5- dihydroimidazo [2,1 -b] quinazolin 2 (3H)-one, more commonly known as anagrelide and its analogues in a clean and efficient manner.Type: ApplicationFiled: November 30, 2009Publication date: October 27, 2011Applicant: SHIRE LLCInventor: Bernard Golding
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Publication number: 20110130405Abstract: This invention relates to the discovery of 3-and 5-substituted analogues of the selective platelet lowering agent anagrelide with reduced potential for cardiovascular side-effects which should lead to improved patient compliance and safety in the treatment of myeloproliferative diseases. More specifically, the present invention relates to certain imidazoquinazoline derivatives which have the general formula (I) shown below wherein the meanings of the substituents are defined in claim 1 and which have utility as platelet lowering agents in humans. The compounds of the present invention function by inhibiting megakaryocytopoeisis and hence the formation of blood platelets.Type: ApplicationFiled: May 13, 2009Publication date: June 2, 2011Applicant: Shire LLCInventors: Bernard Golding, Richard Franklin, Kim Hirst
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Publication number: 20110130413Abstract: This invention relates to the discovery of prodrugs of substituted analogues of the selective platelet lowering agent anagrelide which have reduced potential for cardiovascular side-effects and which should therefore lead to improved patient compliance and safety in the treatment of myeloproliferative diseases. More specifically, the present invention relates to prodrugs of certain imidazoquinazoline derivatives which have the general formula (I) shown below wherein the substituents have the meanings defined in claim 1 and which have utility as platelet lowering agents in humans. The compounds of the present invention function by inhibiting the formation of blood platelets.Type: ApplicationFiled: May 13, 2009Publication date: June 2, 2011Applicant: Shire LLCInventors: Bernard Golding, Peter Cicala, Richard Franklin, Angus Macleod
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Publication number: 20110086851Abstract: This invention relates to the discovery of substituted analogues of the selective platelet lowering agent anagrelide with reduced potential for cardiovascular side-effects which should lead to improved patient compliance and safety in the treatment of myeloproliferative diseases. More specifically, the present invention relates to certain imidazoquinazoline derivatives which have the general formula shown below wherein the substituents have the meanings defined in claim 1: and which have utility as platelet lowering agents in humans. The compounds of the present invention function by inhibiting megakaryocytopoeisis and hence the formation of blood platelets.Type: ApplicationFiled: May 13, 2009Publication date: April 14, 2011Inventors: Bernard Golding, Richard Franklin
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2H- PYRIMIDO [2, 1-B] QUINAZOLIN-2-ONE DERIVATIVES AND THEIR USE AS PLATELET ANTI-AGGREGATIVE AGENTS
Publication number: 20110071171Abstract: This invention relates to the discovery of substituted analogues of the selective platelet lowering agent anagrelide with reduced potential for cardiovascular side-effects which should lead to improved patient compliance and safety in the treatment of myeloproliferative diseases. More specifically, the present invention relates to certain imidazoquinazoline derivatives which have the general formula shown below wherein the substituents have the meanings defined in claim 1: and which have utility as platelet lowering agents in humans. The compounds of the present invention function by inhibiting megakaryocytopoeisis and hence the formation of blood platelets.Type: ApplicationFiled: May 13, 2009Publication date: March 24, 2011Applicant: Shire LLCInventors: Bernard Golding, Richard Franklin -
Publication number: 20110071174Abstract: This invention relates to the discovery of substituted analogues of the selective platelet lowering agent anagrelide with reduced potential for cardiovascular side-effects which should lead to improved patient compliance and safety in the treatment of myeloproliferative diseases. More specifically, the present invention relates to certain imidazoquinazoline derivatives which have the general formula shown below wherein the substituents have the meanings defined in claim 1: and which have utility as platelet lowering agents in humans. The compounds of the present invention function by inhibiting megakaryocytopoeisis and hence the formation of blood platelets.Type: ApplicationFiled: May 13, 2009Publication date: March 24, 2011Inventors: Bernard Golding, Richard Franklin
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Publication number: 20110071172Abstract: This invention relates to the discovery of substituted analogues of the selective platelet lowering agent anagrelide with reduced potential for cardiovascular side-effects which should lead to improved patient compliance and safety in the treatment of myeloproliferative diseases. More specifically, the present invention relates to certain imidazoquinazoline derivatives which have the general formula shown below wherein the substituents have the meanings defined in claim (I): and which have utility as platelet lowering agents in humans. The compounds of the present invention function by inhibiting megakaryocytopoeisis and hence the formation of blood platelets.Type: ApplicationFiled: May 13, 2009Publication date: March 24, 2011Applicant: Shire LLCInventors: Bernard Golding, Richard Franklin
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Publication number: 20110071173Abstract: This invention relates to the discovery of substituted analogues of the selective platelet lowering agent anagrelide with reduced potential for cardiovascular side-effects which should lead to improved patient compliance and safety in the treatment of myeloproliferative diseases. More specifically, the present invention relates to certain imidazoquinazoline derivatives which have the general formula shown below wherein the substituents have the meanings defined in claim 1: and which have utility as platelet lowering agents in humans. The compounds of the present invention function by inhibiting megakaryocytopoeisis and hence the formation of blood platelets.Type: ApplicationFiled: May 13, 2009Publication date: March 24, 2011Inventors: Bernard Golding, Richard Franklin, Angus Macleod
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Publication number: 20110065735Abstract: This invention relates to the discovery of substituted analogues of the selective platelet lowering agent anagrelide with reduced potential for cardiovascular side-effects which should lead to improved patient compliance and safety in the treatment of myeloproliferative diseases. More specifically, the present invention relates to certain imidazoquinazoline derivatives which have the general formula shown below wherein the substituents have the meanings defined in claim 1: and which have utility as platelet lowering agents in humans. The compounds of the present invention function by inhibiting megakaryocytopoeisis and hence the formation of blood platelets.Type: ApplicationFiled: May 13, 2009Publication date: March 17, 2011Applicant: Shire LLCInventors: Bernard Golding, Richard Franklin, Peter Cicala
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Publication number: 20110065714Abstract: This invention relates to the discovery of 3-and 5-substituted analogues of the selective platelet lowering agent anagrelide with reduced potential for cardiovascular side-effects which should lead to improved patient compliance and safety in the treatment of myeloproliferative diseases. More specifically, the present invention relates to certain imidazoquinazoline derivatives which have the general formula shown below wherein the substituents have the meanings defined in claim 1: and which have utility as platelet lowering agents in humans. The compounds of the present invention function by inhibiting megakaryocytopoeisis and hence the formation of blood platelets.Type: ApplicationFiled: May 13, 2009Publication date: March 17, 2011Applicant: Shire LLCInventors: Bernard Golding, Peter Cicala, Richard Franklin, Kim Hirst
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Publication number: 20070238729Abstract: The invention relates to the use of compounds of formula (I) and isomers, salts, solvates, chemically protected forms, and prodrugs thereof, in the preparation of a medicament for inhibiting the activity of DNA-PK, wherein R1 and R2 are independently hydrogen, an optionally substituted C1-7 alkyl group, C3-20 heterocyclyl group, or C5-20 aryl group, or may together form, along with the nitrogen atom to which they are attached, an optionally substituted heterocyclic ring having from 4 to 8 ring atoms; X and Y are selected from CR4 and O, O and CR?4 and NR?4 and N, where the unsaturation is in the appropriate place in the ring, and where one of R3 and R4 or R?4 is an optionally substituted C3-20 heteroaryl or C5-20 aryl group, and the other of R3 and R4 or R?4 is H, or R3 and R4 or R?4 together are -A-B—, which collectively represent a fused optionally substituted aromatic ring. The compounds also selectively inhibit the activity of DNA-PK compared to PI 3-kinase and/or ATM.Type: ApplicationFiled: June 5, 2007Publication date: October 11, 2007Applicant: CANCER RESEARCH TECHNOLOGY LIMITEDInventors: Niall Martin, Graeme Smith, Roger Griffin, Bernard Golding, Ian Hardcastle, David Newell, Hilary Calvert, Nicola Curtin, Laurent Rigoreau, Xiao-ling Cockcroft, Vincent Junior Loh, Paul Workman, Florence Raynaud, Bernard Nutley
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Publication number: 20070238731Abstract: A compound of formula I: and isomers, salts, solvates, chemically protected forms, and prodrugs thereof, wherein: R1 and R2 are independently selected from hydrogen, an optionally substituted C1-7 alkyl group, C3-20heterocyclyl group, or C5-20 aryl group, or may together form, along with the nitrogen atom to which they are attached, an optionally substituted heterocyclic ring having from 4 to 8 ring atoms; Q is —NH—C(?O)— or —O—; Y is an optionally substituted C1-5 alkylene group; X is selected from SR3 or NR4R5, wherein, R3 or R4 and R5 are independently selected from hydrogen, optionally substituted C1-7 alkyl, C5-20 aryl, or C3-20 heterocyclyl groups, or R4 and R5 may together form, along with the nitrogen atom to which they are attached, an optionally substituted heterocyclic ring having from 4 to 8 ring atoms; if Q is —O—, X is additionally selected from —C(?O)—NR6R7, wherein R6 and R7 are independently selected from hydrogen, optionally substituted C1-7 alkyl, C5-20 aryl, or C3-20 heterocyclyl groups, oType: ApplicationFiled: September 20, 2005Publication date: October 11, 2007Applicants: KUDOS PHARMACEUTICALS LIMITED, CANCER RESEARCH TECHNOLOGY LIMITEDInventors: Graeme Smith, Niall Martin, Roger Griffin, Bernard Golding, Ian Hardcastle, Kappusamy Saravanan, David Newell, Hilary Calvert, Nicola Curtin, Keith Menear, Marc Hummersone
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Publication number: 20060264427Abstract: Compounds of formula I: wherein A, B and D are respectively selected from the group consisting of: (i) CH, NH, C; (ii) CH, N, N;and (iii) CH, O, C; the dotted lines represent two double bonds in the appropriate locations; and where Z is selected from S, O, C(?O), CH2 and NH are disclosed for use in inhibiting DNA-PK.Type: ApplicationFiled: April 13, 2006Publication date: November 23, 2006Applicants: KuDOS Pharmaceuticals Limited, Cancer Research Technology LimitedInventors: Graeme Smith, Niall Martin, Keith Menear, Marc Hummersone, Xiao-ling Cockcroft, Mark Frigerio, Roger Griffin, Bernard Golding, Ian Hardcastle, David Newell, HiIary Calvert, Nicola Curtin, Kappusamy Saravanan, Marine Desage-El Murr
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Publication number: 20060264623Abstract: Compounds of formula l: wherein A, B and D are respectively selected from the group consisting of: (i) CH, NH, C; (ii) CH, N, N;and (iii) CH, O, C; are disclosed for use in inhibiting DNA-PK.Type: ApplicationFiled: April 13, 2006Publication date: November 23, 2006Applicants: KuDOS Pharmaceuticals Limited, Cancer Research Technology LimitedInventors: Graeme Smith, Niall Martin, Keith Menear, Marc Hummersone, Xiao-ling Cockcroft, Mark Frigerio, Roger Griffin, Bernard Golding, Ian Hardcastle, David Newell, Hilary Calvert, Nicola Curtin, Marine Desage-El Murr
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Publication number: 20060106025Abstract: A compound of formula I: and isomers, salts, solvates, chemically protected forms, and prodrugs thereof, wherein: R1 and R2 are independently selected from hydrogen, an optionally substituted C1-7 alkyl group, C3-20 heterocyclyl group, or C5-20 aryl group, or may together form, along with the nitrogen atom to which they are attached, an optionally substituted heterocyclic ring having from 4 to 8 ring atoms; Q is —NH—C(?O)— or —O—; Y is an optionally substituted C1-5 alkylene group; X is selected from SR3 or NR4R5, wherein, R3, or R4 and R5 are independently selected from hydrogen, optionally substituted C1-7 alkyl, C5-20 aryl, or C3-20 heterocyclyl groups, or R4 and R5 may together form, along with the nitrogen atom to which they are attached, an optionally substituted heterocyclic ring having from 4 to 8 ring atoms; if Q is —O—, X is additionally selected from —C(?O)—NR6R7, wherein R6 and R7 are independently selected from hydrogen, optionally substituted C1-7 alkyl, C5-20 aryl, or C3-20 heterocyclyl gType: ApplicationFiled: September 20, 2005Publication date: May 18, 2006Applicants: Kudos Pharmaceuticals Limited, Cancer Research Technology LimitedInventors: Graeme Smith, Niall Martin, Keith Menear, Marc Hummersone, Laurent Rigoreau, Roger Griffin, Bernard Golding, David Newell, Hilary Calvert, Nicola Curtin, Ian Hardcastle, Kappusamy Saravanan
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Publication number: 20050107367Abstract: The present invention provides compounds of formula (I) and isomers, salts, solvates, chemically protected forms, and prodrugs thereof, wherein R1 and R2 are independently hydrogen, an option ally substituted C1-7 alkyl group, C3-20 heterocyclyl group, or C5-20 aryl group, or may together form, along with the nitrogen atom to which they are attached, an optionally substituted heterocyclic ring having from 4 to 8 ring atoms; and R3 is an optionally substituted C3-20 heterocyclyl or C5-20 aryl group, and their use as pharmaceuticals, particularly in treating diseases which are retroviral mediated or ameliorated by the inhibition of DNA-PK,Type: ApplicationFiled: August 14, 2002Publication date: May 19, 2005Inventors: Niall Martin, Graeme Cameron Smith, Roger Griffin, Bernard Golding, Ian Hardcastle, Laurent Rigoreau, David Newell, Hilary Calvert, Nicola Curtin, Paul Workman, Florence Raynaud, Bernard Nutley