Patents by Inventor Yuanjun He
Yuanjun He 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: 20230339886Abstract: The present disclosure provides compounds of Formula IA and Formula IB and their pharmaceutical compositions as selective agonists of REV-ERB-?: where R1, R2, R3, R4, R5, RX1, RX2, nA, nB, X, Y, and Z are described herein. The compounds are useful in various methods and uses, such as in the treatment of diseases including hyperglycemia, dyslipidemia, atherosclerosis, and autoimmune and inflammatory disorders or diseases, and as cancer therapeutics, such as for the treatment of glioblastoma, hepatocellular carcinoma, and colorectal cancer, and for immune-oncology purposes.Type: ApplicationFiled: June 23, 2021Publication date: October 26, 2023Applicants: University of Florida Research Foundation, Incorporated, SHANGPHARMA INNOVATION INC.Inventors: Theodore Mark Kamenecka, Kevin Greenman, Laura Solt, Yuanjun He, Mike Lizarzaburu, Brett C. Bookser
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Publication number: 20220380359Abstract: The present application relates to certain halo-substituted piperidine compounds, pharmaceutical compositions containing them, and methods of using them, including methods for treating substance addiction, panic disorder, anxiety, post-traumatic stress disorder, pain, depression, seasonal affective disorder, an eating disorder, or hypertension.Type: ApplicationFiled: July 20, 2022Publication date: December 1, 2022Inventors: Theodore M. Kamenecka, Jörg Holenz, Steven Wesolowski, Yuanjun He, Roland Bürli
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Patent number: 11434236Abstract: The present application relates to certain halo-substituted piperidine compounds, pharmaceutical compositions containing them, and methods of using them, including methods for treating substance addiction, panic disorder, anxiety, post-traumatic stress disorder, pain, depression, seasonal affective disorder, an eating disorder, or hypertension.Type: GrantFiled: December 9, 2020Date of Patent: September 6, 2022Assignees: ASTRAZENECA AB, EOLAS THERAPEUTICS, INC.Inventors: Theodore M. Kamenecka, Jörg Holenz, Steven Wesolowski, Yuanjun He, Roland Bürli
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Publication number: 20210214348Abstract: The present application relates to certain halo-substituted piperidine compounds, pharmaceutical compositions containing them, and methods of using them, including methods for treating substance addiction, panic disorder, anxiety, post-traumatic stress disorder, pain, depression, seasonal affective disorder, an eating disorder, or hypertension.Type: ApplicationFiled: December 9, 2020Publication date: July 15, 2021Inventors: Theodore M. Kamenecka, Jörg Holenz, Steven Wesolowski, Yuanjun He, Roland Bürli
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Patent number: 10894789Abstract: The present application relates to certain halo-substituted piperidine compounds, pharmaceutical compositions containing them, and methods of using them, including methods for treating substance addiction, panic disorder, anxiety, post-traumatic stress disorder, pain, depression, seasonal affective disorder, an eating disorder, or hypertension.Type: GrantFiled: February 10, 2017Date of Patent: January 19, 2021Assignees: ASTRAZENECA AB, EOLAS THERAPEUTICS, INC.Inventors: Theodore M. Kamenecka, Jörg Holenz, Steven Wesolowski, Yuanjun He, Roland Bürli
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Publication number: 20190135800Abstract: The present application relates to certain halo-substituted piperidine compounds, pharmaceutical compositions containing them, and methods of using them, including methods for treating substance addiction, panic disorder, anxiety, post-traumatic stress disorder, pain, depression, seasonal affective disorder, an eating disorder, or hypertension.Type: ApplicationFiled: February 10, 2017Publication date: May 9, 2019Inventors: Theodore M. Kamenecka, Jörg Holenz, Steven Wesolowski, Yuanjun He, Roland Bürli
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Patent number: 10221170Abstract: The present application relates to certain difluoropyrrolidine compounds, pharmaceutical compositions containing them, and methods of using them, including methods for treating substance addiction, panic disorder, anxiety, post-traumatic stress disorder, pain, depression, seasonal affective disorder, an eating disorder, or hypertension.Type: GrantFiled: August 13, 2015Date of Patent: March 5, 2019Assignee: Eolas Therapeutics, Inc.Inventors: Theodore M. Kamenecka, Yuanjun He
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Patent number: 9896452Abstract: The present invention is directed to compounds that modulate the bioactivity of an orexin receptor such as OX1 or OX2, or both; to pharmaceutical compositions and combinations comprising a compound of the invention; to methods of treatment of malconditions in patients wherein modulation of an orexin receptor is medically indicated; and to methods of preparation of compounds of the invention.Type: GrantFiled: October 20, 2016Date of Patent: February 20, 2018Assignee: EOLAS THERAPEUTICS, INC.Inventors: Theodore M. Kamenecka, Yuanjun He, William Nguyen, Rong Jiang, Xinyi Song, Robert Jason Herr, Qin Jiang
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Publication number: 20170226103Abstract: The present application relates to certain difluoropyrrolidine compounds, pharmaceutical compositions containing them, and methods of using them, including methods for treating substance addiction, panic disorder, anxiety, post-traumatic stress disorder, pain, depression, seasonal affective disorder, an eating disorder, or hypertension.Type: ApplicationFiled: August 13, 2015Publication date: August 10, 2017Inventors: Theodore M. Kamenecka, Yuanjun He
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Publication number: 20170101410Abstract: The present invention is directed to compounds that modulate the bioactivity of an orexin receptor such as OX1 or OX2, or both; to pharmaceutical compositions and combinations comprising a compound of the invention; to methods of treatment of malconditions in patients wherein modulation of an orexin receptor is medically indicated; and to methods of preparation of compounds of the invention.Type: ApplicationFiled: October 20, 2016Publication date: April 13, 2017Inventors: Theodore M. Kamenecka, Yuanjun He, William Nguyen, Rong Jiang, Xinyi Song, Robert Jason Herr, Qin Jiang
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Patent number: 9586928Abstract: The invention provides small molecule modulators of retinoic acid receptor-related orphan receptors such as ROR?, ROR?, or ROR?, of formula with the variable atoms as defined herein and R1 comprising a hydroxyl- or alkoxyl-substituted fluoroalkyl group. Compounds of the invention can be effective modulators at concentrations ineffective to act on LXR receptors, or on other nuclear receptors, or other biological targets. Methods of modulation the RORs and methods of treating metabolic disorders, immune disorders, cancer, and CNS disorders wherein modulation of an ROR is medically indicated are also provided.Type: GrantFiled: May 16, 2012Date of Patent: March 7, 2017Assignee: The Scripps Research InstituteInventors: Theodore Mark Kamenecka, Patrick R. Griffin, Youseung Shin, Yuanjun He, Anne-Laure Blayo, Brent R. Lyda, Marcel Koenig, Naresh Kumar, Thomas Burris
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Patent number: 9580439Abstract: The invention provides inhibitors of focal adhesion kinase, an enzyme involved in the attachment of the cytoskeleton of a cell to an extracellular matrix, which has been implicated in processes such as cell migration, cell proliferation, and cell survival. The inhibitors are derivatives of a 5-substituted 2,4-diaminopyridine wherein the substituents are as defined herein. The invention also provides a method of using the inhibitors in treatment of cancer, and methods of preparation of the inhibitors by use of coupling reactions.Type: GrantFiled: June 19, 2013Date of Patent: February 28, 2017Assignee: The Scripps Research InstituteInventors: Congxin Liang, Marcel Koenig, Yuanjun He, Par Holmberg
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Patent number: 9499517Abstract: The present invention is directed to compounds that modulate the bioactivity of an orexin receptor such as OX1 or OX2, or both; to pharmaceutical compositions and combinations comprising a compound of the invention; to methods of treatment of malconditions in patients wherein modulation of an orexin receptor is medically indicated; and to methods of preparation of compounds of the invention.Type: GrantFiled: February 12, 2014Date of Patent: November 22, 2016Assignee: Eolas Therapeutics, Inc.Inventors: Theodore M. Kamenecka, Yuanjun He, William Nguyen, Rong Jiang, Xinyi Song, Robert Jason Herr, Qin Jiang
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Patent number: 9440982Abstract: The present invention is directed to compounds that modulate the bioactivity of an orexin receptor such as OX1 or OX2, or both; to pharmaceutical compositions and combinations comprising a compound of the invention; to methods of treatment of malconditions in patients wherein modulation of an orexin receptor is medically indicated; and to methods of preparation of compounds of the invention.Type: GrantFiled: August 14, 2014Date of Patent: September 13, 2016Assignee: Eolas Therapeutics, Inc.Inventors: Theodore M. Kamenecka, Yuanjun He, Rong Jiang, William Nguyen, Xinyi Song, Robert Jason Herr, Qin Jiang
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Publication number: 20150246908Abstract: The invention provides potent inhibitors of small molecule inhibitors of Krüppel-like factor 5 (KLF5) expression. Compounds of the invention are small molecule inhibitors of KLF5 expression which can be effective delay or prevent colon cancer onset, halt growth of existing tumors, and/or decrease reoccurrence. The compounds can be effective vs. many tumor types whose progression is in part mediated by KLF5, including colorectal cancers. Lowering KLF5 levels with an inhibitor of this invention may also impact other disease states, including diabetes, obesity, lipid homeostasis, cardiovascular disease, and arthritis.Type: ApplicationFiled: July 26, 2013Publication date: September 3, 2015Inventors: Thomas D. Bannister, Yuanjun He, Agnieszka Bialkowska, Vincent Yang, Melissa Crisp, Peter Hodder
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Patent number: 9051265Abstract: The invention provides molecular entities that bind with high affinity to PPARG (PPAR?), and inhibit kinase-mediated (e.g., cdk5-mediated) phosphorylation of PPARG, but do not exert an agonistic effect on PPARG. Compounds of the invention can be used for treatment of conditions in patients wherein PPARG plays a role, such as diabetes, insulin resistance, impaired glucose tolerance, pre-diabetes, hyperglycemia, hyperinsulinemia, obesity, or inflammation. Side effects such as significant weight gain, edema, impairment of bone growth or formation, or cardiac hypertrophy, or any combination thereof, can be avoided in the mammal receiving the compound. Methods of preparation of the compounds, bioassay methods for evaluating compounds of the invention as non-agonistic PPARG binding compounds, and pharmaceutical compositions are also provided.Type: GrantFiled: June 6, 2012Date of Patent: June 9, 2015Assignee: The Scripps Research InstituteInventors: Theodore Mark Kamenecka, Patrick R. Griffin, Marcel Koenig, Alice Asteian, Anne-Laure Blayo, Yuanjun He, Youseung Shin
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Patent number: 8957093Abstract: The invention provides molecular entities that bind with high affinity to PPARG (PPAR?), inhibit kinase-mediated, e.g., cdk5-mediated, phosphorylation of PPARG, but do not exert an agonistic effect on PPARG. Compounds of the invention can be used for treatment of conditions in patients wherein PPARG plays a role, such as diabetes, insulin resistance, impaired glucose tolerance, pre-diabetes, hyperglycemia, hyperinsulinemia, obesity, or inflammation. In methods of treatment of these conditions using a compound of the invention, the compound can avoid producing side effects of significant weight gain, edema, impairment of bone growth or formation, or cardiac hypertrophy, or any combination thereof, in the patient receiving the compound. Methods of preparation of the compounds, bioassay methods for evaluating compounds of the invention as non-agonistic PPARG binding compounds, and pharmaceutical compositions are also provided.Type: GrantFiled: June 6, 2012Date of Patent: February 17, 2015Assignee: The Scripps Research InstituteInventors: Theodore Mark Kamenecka, Patrick R. Griffin, Marcel Koenig, Alice Asteian, Anne-Laure Blayo, Yuanjun He, Youseung Shin
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Publication number: 20140364432Abstract: The present invention is directed to compounds that modulate the bioactivity of an orexin receptor such as OX1 or OX2, or both; to pharmaceutical compositions and combinations comprising a compound of the invention; to methods of treatment of malconditions in patients wherein modulation of an orexin receptor is medically indicated; and to methods of preparation of compounds of the invention.Type: ApplicationFiled: February 12, 2014Publication date: December 11, 2014Inventors: Theodore M. KAMENECKA, Yuanjun HE, William NGUYEN, Rong Jiang, Xinyi Song
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Publication number: 20140364433Abstract: The present invention is directed to compounds that modulate the bioactivity of an orexin receptor such as OX1 or OX2, or both; to pharmaceutical compositions and combinations comprising a compound of the invention; to methods of treatment of malconditions in patients wherein modulation of an orexin receptor is medically indicated; and to methods of preparation of compounds of the invention.Type: ApplicationFiled: August 14, 2014Publication date: December 11, 2014Inventors: Theodore M. KAMENECKA, Yuanjun HE, Rong JIANG, William NGUYEN, Xinyi SONG
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Publication number: 20140187554Abstract: The invention provides small molecule modulators of retinoic acid receptor-related orphan receptors such as ROR?, ROR?, or ROR?. Compounds of the invention can be effective modulators at concentrations ineffective to act on LXR receptors, or on other nuclear receptors, or other biological targets. Methods of modulation the RORs and methods of treating metabolic disorders, immune disorders, cancer, and CNS disorders wherein modulation of an ROR is medically indicated are also provided.Type: ApplicationFiled: May 16, 2012Publication date: July 3, 2014Applicant: The Scripps Research InstituteInventors: Theodore Mark Kamenecka, Patrick R. Griffin, Youseung Shin, Yuanjun He, Anne-Laure Blayo, Brent R. Lyda, Marcel Koenig, Naresh Kumar, Thomas Burris