Patents by Inventor Alexei Degterev
Alexei Degterev 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: 20220194937Abstract: Identified compounds demonstrate protein kinase inhibitory activity. More specifically, the compounds are demonstrated to inhibit receptor interacting kinase 2 (RIPK2) and/or Activin-like kinase 2 (ALK2) and/or receptor interacting kinase 3 (RIPK3). Compounds that are either dual RIPK2/ALK2 inhibitors or that preferentially inhibit RIPK2 or ALK2 or RIPK3 could provide therapeutic benefit. Compounds that function as RIPK3 inhibitors provide therapeutic benefit in the treatment of inflammatory and degenerative conditions.Type: ApplicationFiled: May 14, 2020Publication date: June 23, 2022Inventors: Gregory Cuny, Alexei Degterev, Sameer Nikhar, Siddharth Balachandran
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Publication number: 20220064163Abstract: Identified compounds demonstrate protein kinase inhibitory activity. More specifically, the compounds are demonstrated to inhibit receptor interacting kinase 2 (RIPK2) and/or Activin-like kinase 2 (ALK2). Compounds that are either dual RIPK2/ALK2 inhibitors or that preferentially inhibit RIPK2 or ALK2 could provide therapeutic benefit.Type: ApplicationFiled: October 13, 2021Publication date: March 3, 2022Applicants: UNIVERSITY OF HOUSTON SYSTEM, TRUSTEES OF TUFTS COLLEGEInventors: Gregory Cuny, Sameer Nikhar, Alexei Degterev
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Patent number: 11174255Abstract: Identified compounds demonstrate protein kinase inhibitory activity. More specifically, the compounds having the structures below (I) are demonstrated to inhibit receptor interacting kinase 2 (RIPK2) and/or Activin-like kinase 2 (ALK2). Compounds that are either dual RIPK2/ALK2 inhibitors or that preferentially inhibit RIPK2 or ALK2 could provide therapeutic benefit.Type: GrantFiled: May 15, 2018Date of Patent: November 16, 2021Assignees: UNIVERSITY OF HOUSTON SYSTEM, TRUSTEES OF TUFTS COLLEGEInventors: Gregory Cuny, Sameer Nikhar, Alexei Degterev
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Patent number: 11135209Abstract: Identified compounds demonstrate protein kinase inhibitory activity and inhibition of dependent cell signaling pathways, such as NOD2 cell signaling. More specifically, the compounds are demonstrated to inhibit receptor interacting kinase 2 (RIPK2) and/or Activin-like kinase 2 (ALK2). Compounds that are either dual RIPK2/ALK2 inhibitors or that preferentially inhibit RIPK2 or ALK2 could provide therapeutic benefit.Type: GrantFiled: March 29, 2018Date of Patent: October 5, 2021Assignees: University of Houston System, Trustees of Tufts CollegeInventors: Gregory Cuny, Chalada Suebsuwong, Alexei Degterev
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Publication number: 20200172536Abstract: Identified compounds demonstrate protein kinase inhibitory activity. More specifically, the compounds having the structures below (I) are demonstrated to inhibit receptor interacting kinase 2 (RIPK2) and/or Activin-like kinase 2 (ALK2). Compounds that are either dual RIPK2/ALK2 inhibitors or that preferentially inhibit RIPK2 or ALK2 could provide therapeutic benefit.Type: ApplicationFiled: May 15, 2018Publication date: June 4, 2020Applicants: UNIVERSITY OF HOUSTON SYSTEM, TRUSTEES OF TUFTS COLLEGEInventors: Gregory Cuny, Sameer Nikhar, Alexei Degterev
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Publication number: 20200030303Abstract: Identified compounds demonstrate protein kinase inhibitory activity and inhibition of dependent cell signaling pathways, such as NOD2 cell signaling. More specifically, the compounds are demonstrated to inhibit receptor interacting kinase 2 (RIPK2) and/or Activin-like kinase 2 (ALK2). Compounds that are either dual RIPK2/ALK2 inhibitors or that preferentially inhibit RIPK2 or ALK2 could provide therapeutic benefit.Type: ApplicationFiled: March 29, 2018Publication date: January 30, 2020Applicants: UNIVERSITY OF HOUSTON SYSTEM, TRUSTEES OF TUFTS COLLEGEInventors: Gregory Cuny, Chalada Suebsuwong, Alexei Degterev
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Patent number: 9725452Abstract: The present invention relates to heterocyclic compounds (e.g., compounds described by Formula (I)) and pharmaceutically acceptable salts thereof. The invention also features pharmaceutical compositions that include these compounds and their use in therapy for treating conditions in which necroptosis is likely to play a substantial role. The heterocyclic compounds described herein can also achieve improved activity and selectivity towards RIP1 and/or RIP3.Type: GrantFiled: March 14, 2014Date of Patent: August 8, 2017Assignees: Presidents and Fellows of Harvard College, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, Tufts University, University of HoustonInventors: Junying Yuan, Alexei Degterev, Gregory D. Cuny
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Patent number: 9701646Abstract: Provided are certain 1,2,3-triazole and 1,2,3-triazole dimer analogs of DM-PIT-1 which are second-generation selective non-phosphoinositide small molecule inhibitors of phosphatidylinositol-3,4,5-trisphosphate (PIP3), including 1,2,3-triazoles represented by formula (I) where: Ar represents aryl or heteroaryl; X represents O or S; each of Ra, Rb, Rc, and Rd independently represents hydrogen, halogen, C1-C10alkyl, —OH, —CF3, aryl, amino, or nitro; and Ar is optionally substituted with one or more substituents independently selected from the group consisting of halogen, C1-C10alkyl, —OH, —CF3, amino, and nitro. Also provided are pharmaceutical compositions comprising compounds of the invention and a pharmaceutical carrier. Also provided are methods of inhibiting PIP3-mediated signaling in a cell and treating cancer using compounds of the invention.Type: GrantFiled: March 18, 2014Date of Patent: July 11, 2017Assignees: TUFTS UNIVERSITY, COUNCIL OF SCIENTIFIC AND INDUSTRIAL RESEARCHInventors: Alexei Degterev, Chepuri V. Ramana, Jinbo Lee, Yadagiri Kommagalla
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Publication number: 20160297777Abstract: Provided are certain 1,2,3-triazole and 1,2,3-triazole dimer analogs of DM-PIT-1 which are second-generation selective non-phosphoinositide small molecule inhibitors of phosphatidylinositol-3,4,5-trisphosphate (PIP3), including 1,2,3-triazoles represented by formula (I) where: Ar represents aryl or heteroaryl; X represents O or S; each of Ra, Rb, Rc, and Rd independently represents hydrogen, halogen, C1-C10alkyl, —OH, —CF3, aryl, amino, or nitro; and Ar is optionally substituted with one or more substituents independently selected from the group consisting of halogen, C1-C10alkyl, —OH, —CF3, amino, and nitro. Also provided are pharmaceutical compositions comprising compounds of the invention and a pharmaceutical carrier. Also provided are methods of inhibiting PIP3-mediated signaling in a cell and treating cancer using compounds of the invention.Type: ApplicationFiled: March 18, 2014Publication date: October 13, 2016Inventors: Alexei Degterev, Chepuri V. Ramana, Jinbo Lee, Yadagiri Kommagalla
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Publication number: 20160102053Abstract: The invention features a series of heterocyclic derivatives that inhibit tumor necrosis factor alpha (TNF-?) induced necroptosis. The heterocyclic compounds of the invention are described by Formulas (I) and (Ia)-(Ie) and are shown to inhibit TNF-? induced necroptosis in FADD-deficient variant of human Jurkat T cells. The invention further features pharmaceutical compositions featuring the compounds of the invention. The compounds and compositions of the invention may also be used to treat disorders where necroptosis is likely to play a substantial role.Type: ApplicationFiled: July 10, 2015Publication date: April 14, 2016Inventors: Gregory D. CUNY, Xin TENG, Junying YUAN, Alexei DEGTEREV, John A. PORCO, JR.
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Publication number: 20160024098Abstract: The present invention relates to heterocyclic compounds (e.g., compounds described by Formula (I)) and pharmaceutically acceptable salts thereof. The invention also features pharmaceutical compositions that include these compounds and their use in therapy for treating conditions in which necroptosis is likely to play a substantial role. The heterocyclic compounds described herein can also achieve improved activity and selectivity towards RIP1 and/or RIP3.Type: ApplicationFiled: March 14, 2014Publication date: January 28, 2016Inventors: Junying YUAN, Alexei DEGTEREV, Gregory D. CUNY
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Patent number: 9108955Abstract: The invention features a series of heterocyclic derivatives that inhibit tumor necrosis factor alpha (TNF-?) induced necroptosis. The heterocyclic compounds of the invention are described by Formulas (I) and (Ia)-(Ie) and are shown to inhibit TNF-? induced necroptosis in FADD-deficient variant of human Jurkat T cells. The invention further features pharmaceutical compositions featuring the compounds of the invention. The compounds and compositions of the invention may also be used to treat disorders where necroptosis is likely to play a substantial role.Type: GrantFiled: January 10, 2014Date of Patent: August 18, 2015Assignees: President and Fellows of Harvard College, Tufts University, The Brigham and Women's Hospital, Inc., Trustees of Boston UniversityInventors: Gregory D. Cuny, Xin Teng, Junying Yuan, Alexei Degterev, John A. Porco, Jr.
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Patent number: 9040585Abstract: Disclosed are new members of a class of non-lipid small molecule inhibitors which interfere with the interaction between phosphoinositol-3,4,5-triphosphate (PIP3) and pleckstrin homology (PH) domains. These molecules target a broad range of PIP3-dependent signaling events in vitro and exert significant anti-tumor activity in vivo, with improved activity and selectivity toward particular PH domains. The small molecule inhibitors of the invention can be used alone or together with tumor necrosis factor (TNF)-related apoptosis-inducing ligand (TRAIL) or other cancer medicament to treat cancer. Small molecule inhibitors of the invention act synergistically in combination with TRAIL and with other Akt inhibitors in treating cancer. Pharmaceutical compositions and methods for treating cancer are provided.Type: GrantFiled: December 11, 2013Date of Patent: May 26, 2015Assignees: Tufts University, Council of Scientific and Industrial ResearchInventors: Alexei Degterev, Chepuri Venkata Ramana, Benchun Miao
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Publication number: 20140323489Abstract: The present invention relates to heterocyclic compounds (e.g., compounds described by Formula (I)) and pharmaceutically acceptable salts thereof. The invention also features pharmaceutical compositions that include these compounds and their use in therapy for treating conditions in which necroptosis is likely to play a substantial role. The heterocyclic compounds described herein can also achieve improved activity and selectivity towards RIP1 and/or RIP3.Type: ApplicationFiled: March 14, 2014Publication date: October 30, 2014Applicants: President and Fellows of Harvard College, University of Houston, Tufts University, Shanghai Institute of Organic Chemistry, Chinese Academy of SciencessInventors: Junying YUAN, Alexei DEGTEREV, Gregory D. CUNY
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Publication number: 20140187639Abstract: Disclosed are new members of a class of non-lipid small molecule inhibitors which interfere with the interaction between phosphoinositol-3,4,5-triphosphate (PIP3) and pleckstrin homology (PH) domains. These molecules target a broad range of PIP3-dependent signaling events in vitro and exert significant anti-tumor activity in vivo, with improved activity and selectivity toward particular PH domains. The small molecule inhibitors of the invention can be used alone or together with tumor necrosis factor (TNF)-related apoptosis-inducing ligand (TRAIL) or other cancer medicament to treat cancer. Small molecule inhibitors of the invention act synergistically in combination with TRAIL and with other Akt inhibitors in treating cancer. Pharmaceutical compositions and methods for treating cancer are provided.Type: ApplicationFiled: December 11, 2013Publication date: July 3, 2014Applicants: Council of Scientific and Industrial Research, Tufts UniversityInventors: Alexei Degterev, Chepuri Venkata Ramana, Benchun Miao
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Patent number: 8741942Abstract: The present invention relates to compounds and pharmaceutical preparations and their use in therapy for preventing or treating trauma, ischemia, stroke and degenerative diseases associated with cell death. Methods and compositions of the invention are particularly useful for treating neurological disorders associated with cellular necrosis.Type: GrantFiled: February 21, 2012Date of Patent: June 3, 2014Assignees: President and Fellows of Harvard College, The Brigham and Women's Hospital, Inc.Inventors: Gregory D. Cuny, Prakash Jagtap, Junying Yuan, Alexei Degterev
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Patent number: 8658689Abstract: The invention features a series of heterocyclic derivatives that inhibit tumor necrosis factor alpha (TNF-?) induced necroptosis. The heterocyclic compounds of the invention are described by Formulas (I) and (Ia)-(Ie) and are shown to inhibit TNF-? induced necroptosis in FADD-deficient variant of human Jurkat T cells. The invention further features pharmaceutical compositions featuring the compounds of the invention. The compounds and compositions of the invention may also be used to treat disorders where necroptosis is likely to play a substantial role.Type: GrantFiled: August 20, 2012Date of Patent: February 25, 2014Assignees: President and Fellows of Harvard College, The Brigham and Women's Hospital, Inc., Tufts University, Trustees of Boston UniversityInventors: Gregory D. Cuny, Xin Teng, Junying Yuan, Alexei Degterev, John A. Porco, Jr.
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Publication number: 20140024662Abstract: The present invention features compounds of Formula (I), pharmaceutical compositions, methods of synthesis, and methods for treating diseases and conditions associate with cellular necrosis. Screening assays for identifying compounds useful for treating these conditions are also described.Type: ApplicationFiled: September 25, 2013Publication date: January 23, 2014Applicants: Shanghai Institute of Organic Chemistry, President and Fellows of Harvard CollegeInventors: Junying YUAN, Chengye Yuan, Alexei Degterev
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Patent number: 8628961Abstract: Disclosed are new members of a class of non-lipid small molecule inhibitors which interfere with the interaction between phosphoinositol-3,4,5-triphosphate (PIP3) and pleckstrin homology (PH) domains. These molecules target a broad range of PIP3-dependent signaling events in vitro and exert significant anti-tumor activity in vivo, with improved activity and selectivity toward particular PH domains. The small molecule inhibitors of the invention can be used alone or together with tumor necrosis factor (TNF)-related apoptosis-inducing ligand (TRAIL) or other cancer medicament to treat cancer. Small molecule inhibitors of the invention act synergistically in combination with TRAIL and with other Akt inhibitors in treating cancer. Pharmaceutical compositions and methods for treating cancer are provided.Type: GrantFiled: May 17, 2011Date of Patent: January 14, 2014Assignees: Tufts University, Council of Scientific and Industrial ResearchInventors: Alexei Degterev, Chepuri Venkata Ramana, Benchun Miao
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Publication number: 20130158024Abstract: The present invention features compounds, pharmaceutical compositions, and methods for treating trauma, ischemia, stroke, degenerative diseases associated with cellular necrosis, and other conditions. Screening assays for identifying compounds useful for treating these conditions are also described.Type: ApplicationFiled: October 31, 2012Publication date: June 20, 2013Inventors: Junying Yuan, Alexei Degterev, Junichi Hitomi, Gregory D. Cuny, Prakash Jagtap