Patents by Inventor Jeffrey Michael Axten
Jeffrey Michael Axten 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: 11773078Abstract: This invention relates to novel compounds according to Formula (I) which are inhibitors of furin, to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the treatment of fibrotic diseases, including pulmonary fibrosis, renal fibrosis, liver fibrosis, skin fibrosis, ocular fibrosis, cardiac fibrosis, and other miscellaneous fibrotic conditions. The disclosed compounds may also be useful for treating other furin-mediated conditions, including but not limited to, hypertension, cancer, infectious diseases, and genetic disorders (e.g., cystic fibrosis (CF)), and neurodegenerative disorders.Type: GrantFiled: May 10, 2019Date of Patent: October 3, 2023Assignee: Glaxosmithkline Intellectual Property Development LimitedInventors: Jeffrey Michael Axten, Mui Cheung, Michael P. Demartino, Huiping Amy Guan, Yan Hu, Aaron Bayne Miller, Donghui Qin, Chengde Wu, Zhiliu Zhang, Xiaojuan Lin
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Publication number: 20230165848Abstract: The invention is directed to substituted piperidine derivatives. Specifically, the invention is directed to compounds according to Formula IIII: wherein A, B, X, Y, L1, L2, L3, R1, R2, R3, R4 R5, R6, R9, z2, z4, z5, and z6 are as defined herein, and salts thereof.Type: ApplicationFiled: December 6, 2022Publication date: June 1, 2023Inventors: Jeffrey Michael AXTEN, Mui CHEUNG, Michael P. DEMARTINO, Hilary Schenck EIDAM, Raghava Reddy KETHIRI, Biswajit KALITA
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Patent number: 11547704Abstract: The invention is directed to substituted piperidine derivatives. Specifically, the invention is directed to compounds according to Formula IIII: wherein A, B, X, Y, L1, L2, L3, R1, R2, R3, R4, R5, R6, R9, z2, z4, z5, and z6 are as defined herein, and salts thereof.Type: GrantFiled: June 11, 2020Date of Patent: January 10, 2023Assignee: GlaxoSmithKline Intellectual Property Development LimitedInventors: Jeffrey Michael Axten, Mui Cheung, Michael P. Demartino, Hilary Schenck Eidam, Raghava Reddy Kethiri, Biswajit Kalita
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Publication number: 20220315556Abstract: This invention relates to novel compounds according to Formula (I) which are inhibitors of furin, to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the treatment of fibrotic diseases, including pulmonary fibrosis, renal fibrosis, liver fibrosis, skin fibrosis, ocular fibrosis, cardiac fibrosis, and other miscellaneous fibrotic conditions. The disclosed compounds may also be useful for treating other furin-mediated conditions, including but not limited to, hypertension, cancer, infectious diseases, and genetic disorders (e.g., cystic fibrosis (CF)), and neurodegenerative disorders.Type: ApplicationFiled: May 10, 2019Publication date: October 6, 2022Applicant: Glaxosmithkline Intellectual Property Development LimitedInventors: Jeffrey Michael Axten, Mui Cheung, Michael P. Demartino, Huiping Amy Guan, Yan Hu, Aaron Bayne Miller, Donghui Qin, Chengde Wu, Zhiliu Zhang, Xiaojuan Lin
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Publication number: 20210093619Abstract: The invention is directed to substituted bridged cycloalkane derivatives. Specifically, the invention is directed to compounds according to Formula IIIQ: wherein X6?, a, b, C8?, D8?, L82?, L83?, R81?, R82?, R83?, R84?, R85?, R86?, z82?, z84?, z85?, and z86? are as defined herein; or salts thereof. The compounds of the invention are inhibitors of the ATF4 pathway. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting the ATF4 pathway and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.Type: ApplicationFiled: June 7, 2018Publication date: April 1, 2021Inventors: Jeffrey Michael AXTEN, Michael P. DEMARTINO, Karen Anderson EVANS, Biswajit KALITA, Jeffrey M. RALPH
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Patent number: 10851053Abstract: The invention is directed to substituted pyrrolidine derivatives. Specifically, the invention is directed to compounds according to Formula III: wherein A, B, L1, L2, L3, R1, R2, R3, R4, R5, R6, R9, R10, R30, Y1, Y2, z2, z4, z5, and z6 are as defined herein, and salts thereof.Type: GrantFiled: June 7, 2017Date of Patent: December 1, 2020Assignee: GlaxoSmithKline Intellectual Property Development LimitedInventors: Jeffrey Michael Axten, Mui Cheung, Anthony William Dean, Michael P. DeMartino, Hilary Schenck Eidam, Biswajit Kalita, Raghava Reddy Kethiri, Rajendra Kristam
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Publication number: 20200297710Abstract: The invention is directed to substituted piperidine derivatives. Specifically, the invention is directed to compounds according to Formula IIII: wherein A, B, X, Y, L1, L2, L3, R1, R2, R3, R4, R5, R6, R9, z2, z4, z5, and z6 are as defined herein, and salts thereof.Type: ApplicationFiled: June 11, 2020Publication date: September 24, 2020Inventors: Jeffrey Michael AXTEN, Mui CHEUNG, Michael P. DEMARTINO, Hilary Schenck EIDAM, Raghava Reddy KETHIRI, Biswajit KALITA
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Publication number: 20190298705Abstract: The invention is directed to substituted piperidine derivatives. Specifically, the invention is directed to compounds according to Formula IIII: wherein A, B, X, Y, L1, L2, L3, R1, R2, R3, R4, R5, R6, R9, z2, z4, z5, and z6 are as defined herein, and salts thereof.Type: ApplicationFiled: June 7, 2017Publication date: October 3, 2019Inventors: Jeffrey Michael AXTEN, Mui CHEUNG, Michael P. DEMARTINO, Hilary Schenck EIDAM, Raghava Reddy KETHIRI, Biswajit KALITA
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Publication number: 20190241573Abstract: The invention is directed to substituted isoquinoline derivatives and uses thereof. Specifically, the invention is directed to compounds according to Formula I and the use of compounds of Formula (I) in treating disease states: wherein R1, R2, R3, R4, R5, R6, R7 and X are as defined herein.Type: ApplicationFiled: July 18, 2017Publication date: August 8, 2019Applicant: GlaxoSmithKline Intellectual Property Development LimitedInventors: Jeffrey Michael AXTEN, Raghava Reddy KETHIRI, Rajendra KRISTAM, Chandregowda VENKATESHAPPA
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Publication number: 20190144384Abstract: The invention is directed to substituted pyrrolidine derivatives. Specifically, the invention is directed to compounds according to Formula III: wherein A, B, L1, L2, L3, R1, R2, R3, R4, R5, R6, R9, R10, R30, Y1, Y2, z2, z4, z5, and z6 are as defined herein, and salts thereof.Type: ApplicationFiled: June 7, 2017Publication date: May 16, 2019Inventors: Jeffrey Michael AXTEN, Mui CHEUNG, Anthony William DEAN, Michael P. DEMARTINO, Hilary Schenck EIDAM, Biswajit KALITA, Raghava Reddy KETHIRI, Rajendra KRISTAM
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Publication number: 20180237441Abstract: The invention is directed to substituted pyrrolidinone and imidazolidinone derivatives. Specifically, the invention is directed to compounds according to Formula I: wherein R1, R2, R3, R4, R5, R6, R7, X and Y are as defined herein.Type: ApplicationFiled: September 15, 2016Publication date: August 23, 2018Inventors: Jeffrey Michael AXTEN, Alain Claude-Marie DAUGAN, Nicolas Eric FAUCHER, Raghava Reddy KETHIRI, Rajendra KRISTAM, Chandregowda VENKATESHAPPA
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Patent number: 8697685Abstract: The invention is directed to 6-(4-pyrimidinyl)-1H-indazole derivatives. Specifically, the invention is directed to compounds according to Formula (I) wherein R1-R4 are defined herein. The compounds of the invention axe inhibitors of PDK1 and can be useful in the treatment of immune and metabolic diseases and disorders characterized by constitutively activated ACG kinases such as cancer and more specifically cancers of the breast, colon, and lung. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting PDK1 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.Type: GrantFiled: November 18, 2009Date of Patent: April 15, 2014Assignee: GlaxoSmithKline LLCInventors: Jeffrey Michael Axten, Charles William Blackledge, Jr., Gerald Patrick Brady, Jr., Yanhong Feng, Seth W. Grant, Jesus Raul Medina, William H. Miller, Stuart P. Romeril
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Patent number: 8598156Abstract: The invention is directed to substituted indoline derivatives. Specifically, the invention is directed to compounds according to Formula I: wherein R1, R2, and R3 are defined herein. The compounds of the invention are inhibitors of PERK and can be useful in the treatment of cancer, ocular diseases, and diseases associated with activated unfolded protein response pathways, such as Alzheimer's disease, stroke, Type 1 diabetes Parkinson disease, Huntington's disease, amyotrophic lateral sclerosis, myocardial infarction, cardiovascular disease, atherosclerosis, and arrhythmias, and more specifically cancers of the breast, colon, pancreatic, and lung. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting PERK activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.Type: GrantFiled: March 23, 2011Date of Patent: December 3, 2013Assignee: GlaxoSmithKline LLCInventors: Jeffrey Michael Axten, Seth Wilson Grant, Dirk A. Heerding, Jesus Rual Medina, Stuart Paul Romeril, Jun Tang
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Patent number: 8383635Abstract: The invention is directed to pyrido[4,3-d]pyrimidin-5(6H)-one derivatives. Specifically, the invention is directed to compounds according to Formula I: wherein R1, R2, R3, and R4 are defined below. The compounds of the invention are inhibitors of PDK1 and can be useful in the treatment of disorders characterized by constitutively activated ACG kinases such as cancer and more specifically cancers of the breast, colon, and lung. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting PDK1 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.Type: GrantFiled: August 12, 2009Date of Patent: February 26, 2013Assignee: GlaxoSmithKline LLCInventors: Francis Louis Atkinson, Jeffrey Michael Axten, Maria Cichy-Knight, Michael Lee Moore, Vipulkumar Kantibhai Patel, Xinrong Tian, Christopher Roland Wellaway, Allison K. Dunn
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Publication number: 20130018038Abstract: The invention is directed to substituted indoline derivatives. Specifically, the invention is directed to compounds according to Formula I: wherein R1, R2, and R3 are defined herein. The compounds of the invention are inhibitors of PERK and can be useful in the treatment of cancer, ocular diseases, and diseases associated with activated unfolded protein response pathways, such as Alzheimer's disease, stroke, Type 1 diabetes Parkinson disease, Huntington's disease, amyotrophic lateral sclerosis, myocardial infarction, cardiovascular disease, atherosclerosis, and arrhythmias, and more specifically cancers of the breast, colon, pancreatic, and lung. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting PERK activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.Type: ApplicationFiled: March 23, 2011Publication date: January 17, 2013Inventors: Jeffrey Michael Axten, Seth Wilson Grant, Dirk A. Heerding, Jesus Rual Medina, Stuart Paul Romeril, Jun Tang
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Publication number: 20120077828Abstract: The invention is directed to substituted indoline derivatives. Specifically, the invention is directed to compounds according to Formula I: wherein R1, R2, and R3 are defined herein. The compounds of the invention are inhibitors of PERK and can be useful in the treatment of cancer, ocular diseases, and diseases associated with activated unfolded protein response pathways, such as Alzheimer's disease, stroke, Type 1 diabetes Parkinson disease, Huntington's disease, amyotrophic lateral sclerosis, myocardial infarction, cardiovascular disease, atherosclerosis, and arrhythmias, and more specifically cancers of the breast, colon, pancreatic, and lung. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting PERK activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.Type: ApplicationFiled: March 23, 2011Publication date: March 29, 2012Inventors: Jeffrey Michael Axten, Seth Wilson Grant, Dirk A. Heerding, Jesus Raul Medina, Stuart Paul Romeril, Jun Tang
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Publication number: 20110275611Abstract: The invention is directed to 6-(4-pyrimidinyl)-1H-indazole derivatives. Specifically, the invention is directed to compounds according to Formula (I) wherein R1-R4 are defined herein. The compounds of the invention axe inhibitors of PDK1 and can be useful in the treatment of immune and metabolic diseases and disorders characterized by constitutively activated ACG kinases such as cancer and more specifically cancers of the breast, colon, and lung. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention.Type: ApplicationFiled: November 18, 2009Publication date: November 10, 2011Inventors: Jeffrey Michael Axten, Charles William Blackledge, JR., Gerald Patrick Brady, JR., Yanhong Feng, Seth W. Grant, Jesus Raul Medina, William H. Miller, Stuart P. Romeril
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Patent number: 7982053Abstract: Novel PDF inhibitors and novel methods for their use are provided.Type: GrantFiled: July 28, 2006Date of Patent: July 19, 2011Assignee: GlaxoSmithKline LLCInventors: Jeffrey Michael Axten, Jesus R. Medina
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Publication number: 20110136838Abstract: The invention is directed to pyrido[4,3-d]pyrimidin-5(6H)-one derivatives. Specifically, the invention is directed to compounds according to Formula I: wherein R1, R2, R3, and R4 are defined below. The compounds of the invention are inhibitors of PDK1 and can be useful in the treatment of disorders characterized by constitutively activated ACG kinases such as cancer and more specifically cancers of the breast, colon, and lung. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting PDK1 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.Type: ApplicationFiled: August 12, 2009Publication date: June 9, 2011Inventors: Francis Louis Atkinson, Jeffrey Michael Axten, Maria Cichy-Knight, Michael Lee Moore, Vipulkumar Kantibhai Patel, Xinrong Tian, Christopher Roland Wellaway, Allison K. Dunn
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Patent number: 7884098Abstract: The present invention relates to a compound represented by the following formula: or a pharmaceutically acceptable salt thereof; wherein R1, R1? R2, R3, R4, R5, r and s are as defined herein. Compounds of the present invention are useful in the treatment of diseases associated with Aurora kinase activity such as cancer.Type: GrantFiled: January 25, 2008Date of Patent: February 8, 2011Assignee: GlaxoSmithKline LLCInventors: Jeffrey Michael Axten, Deborah L. Bryan, David Harold Drewry, Thomas H Faitg, Timothy Francis Gallagher, Neil W Johnson, Jiri Kasparec, Jeffrey M Ralph, Domingos J. Silva