Patents by Inventor Athan Kuliopulos
Athan Kuliopulos 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: 10913781Abstract: Disclosed here is the rational design and use of potent and specific GPCR antagonist pepducins based on GPCR regions such as the third intracellular loop and adjacent regions.Type: GrantFiled: April 9, 2012Date of Patent: February 9, 2021Assignee: Tufts Medical Center, Inc.Inventors: Athan Kuliopulos, Lidija Covic
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Patent number: 9878054Abstract: In certain embodiments, this disclosure relates to pharmaceutical formulations for polypeptide and lipophilic moiety conjugates suitable for injection into humans and other animals and methods of preparation. In certain embodiments, the disclosure relates to a method of preparing the formulation comprising lyophilizing, solubilizing in ammonium acetate, filtering to create mono-disperse particles, re-lyophilizing, and solubilizing the micelles in a dextrose solution for injection.Type: GrantFiled: May 17, 2013Date of Patent: January 30, 2018Assignee: Tufts Medical Center, Inc.Inventor: Athan Kuliopulos
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Publication number: 20170065668Abstract: Matrix metalloproteases (MMPs) play many important roles in normal and pathological remodeling processes including atherothrombotic disease, inflammation, angiogenesis and cancer. This invention relates to the activation of protease-activated receptor-1 (PAR-1) by endogenous platelet MMP-1 collagenase on the surface of platelets. Exposure of platelets to fibrillar collagen converts the surface-bound pro-MMP-1 zymogen to active MMP-1, which promotes aggregation through PAR-1. MMP-1 is shown to cleave the PAR-1 extracellular domain at a novel site, which then strongly activates Rho-GTP signaling pathways, cell shape change and motility, and MAPK signaling. Blockade of MMP-PAR1 suppresses thrombogenesis under arterial flow conditions and inhibited thrombosis in animals. These studies provide a link between matrix-dependent activation of metalloproteases and platelet-G protein signaling and identify MMP-1/PAR-1 as a new target for the treatment and prevention of arterial thrombosis and other thrombotic diseases.Type: ApplicationFiled: May 26, 2016Publication date: March 9, 2017Applicant: Tufts Medical Center, Inc.Inventors: Athan Kuliopulos, Georgios Koukos
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Patent number: 9376499Abstract: Matrix metalloproteases (MMPs) play many important roles in normal and pathological remodeling processes including atherothrombotic disease, inflammation, angiogenesis and cancer. This invention relates to the activation of protease-activated receptor-1 (PAR-1) by endogenous platelet MMP-1 collagenase on the surface of platelets. Exposure of platelets to fibrillar collagen converts the surface-bound pro-MMP-1 zymogen to active MMP-1, which promotes aggregation through PAR-1. MMP-1 is shown to cleave the PAR-1 extracellular domain at a novel site, which then strongly activates Rho-GTP signaling pathways, cell shape change and motility, and MAPK signaling. Blockade of MMP-PAR1 suppresses thrombogenesis under arterial flow conditions and inhibited thrombosis in animals. These studies provide a link between matrix-dependent activation of metalloproteases and platelet-G protein signaling and identify MMP-1/PAR-1 as a new target for the treatment and prevention of arterial thrombosis and other thrombotic diseases.Type: GrantFiled: August 14, 2014Date of Patent: June 28, 2016Assignee: Tufts Medical Center, Inc.Inventors: Athan Kuliopulos, Georgios Koukos
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Publication number: 20150216990Abstract: In certain embodiments, this disclosure relates to pharmaceutical formulations for polypeptide and lipophilic moiety conjugates suitable for injection into humans and other animals and methods of preparation. In certain embodiments, the disclosure relates to a method of preparing the formulation comprising lyophilizing, solubilizing in ammonium acetate, filtering to create mono-disperse particles, re-lyophilizing, and solubilizing the micelles in a dextrose solution for injection.Type: ApplicationFiled: May 17, 2013Publication date: August 6, 2015Inventor: Athan Kuliopulos
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Patent number: 9096646Abstract: The invention relates generally to compounds which are allosteric modulators (e.g., positive and negative allosteric modulators, and allosteric agonists) of the G protein coupled receptor for stromal derived factor 1 (SDF-I), also known as the CXCR4 receptor. The CXCR4 receptor compounds are derived from the intracellular loops and domains of the CXCR4 receptor. The invention also relates to the use of these CXCR4 receptor compounds and pharmaceutical compositions comprising the CXCR4 receptor compounds in the treatment of diseases and conditions associated with CXCR4 modulation such as bone marrow transplantation, chemosensitization, cancer, metastatic disease, inflammatory diseases, HIV infection and stem cell-based regenerative medicine.Type: GrantFiled: November 4, 2009Date of Patent: August 4, 2015Assignee: Anchor Therapeutics, Inc.Inventors: Thomas J. McMurry, Athan Kuliopulos, Lidija Covic, Boris Tchernychev
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Publication number: 20150023975Abstract: Matrix metalloproteases (MMPs) play many important roles in normal and pathological remodeling processes including atherothrombotic disease, inflammation, angiogenesis and cancer. This invention relates to the activation of protease-activated receptor-1 (PAR-1) by endogenous platelet MMP-1 collagenase on the surface of platelets. Exposure of platelets to fibrillar collagen converts the surface-bound pro-MMP-1 zymogen to active MMP-1, which promotes aggregation through PAR-1. MMP-1 is shown to cleave the PAR-1 extracellular domain at a novel site, which then strongly activates Rho-GTP signaling pathways, cell shape change and motility, and MAPK signaling. Blockade of MMP-PAR1 suppresses thrombogenesis under arterial flow conditions and inhibited thrombosis in animals. These studies provide a link between matrix-dependent activation of metalloproteases and platelet-G protein signaling and identify MMP-1/PAR-1 as a new target for the treatment and prevention of arterial thrombosis and other thrombotic diseases.Type: ApplicationFiled: August 14, 2014Publication date: January 22, 2015Inventors: Athan Kuliopulos, Georgios Koukos
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Publication number: 20140227718Abstract: The invention relates generally to G protein coupled receptors and in particular to agonists and antagonists of G protein receptors and methods of using the same.Type: ApplicationFiled: January 30, 2013Publication date: August 14, 2014Applicant: Tufts Medical Center, Inc.Inventors: Athan Kuliopulos, Lidija Covic
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Publication number: 20140087993Abstract: Disclosed here is the rational design and use of potent and specific GPCR antagonist pepducins based on GPCR regions such as the third intracellular loop and adjacent regions.Type: ApplicationFiled: April 9, 2012Publication date: March 27, 2014Applicant: TUFTS MEDICAL CENTER, Inc.Inventors: Athan Kuliopulos, Lidija Covic
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Patent number: 8563519Abstract: The invention relates generally to G protein coupled receptors and in particular to agonists and antagonists of G protein receptors and methods of using the same.Type: GrantFiled: March 7, 2005Date of Patent: October 22, 2013Assignee: Tufts Medical Center, Inc.Inventors: Athan Kuliopulos, Lidija Covic
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Publication number: 20130210709Abstract: The invention relates generally to compounds which are allosteric modulators (e.g., positive and negative allosteric modulators, and allosteric agonists) of the G protein coupled receptor for stromal derived factor 1 (SDF-I), also known as the CX-CR4 receptor. The CXCR4 receptor compounds are derived from the intracellular loops and domains of the CXCR4 receptor. The invention also relates to the use of these CXCR4 receptor compounds and pharmaceutical compositions comprising the CXCR4 receptor compounds in the treatment of diseases and conditions associated with CXCR4 modulation such as bone marrow trans-plantation, chemosensitization, cancer, metastatic disease, inflammatory diseases, HIV infection and stem cell-based regenerative medicine.Type: ApplicationFiled: November 4, 2009Publication date: August 15, 2013Inventors: Thomas J. McMurry, Athan Kuliopulos, Lidija Covic, Boris Tchernychev
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Patent number: 8440627Abstract: The invention relates generally to G protein coupled receptors (GPCRs) and in particular to GPCR agonists and antagonists, use of these compounds and their pharmaceutical compositions, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with GPCRs, such as in treating conditions in which chemokine receptors play a role, e.g., sepsis, arthritis, inflammation and autoimmune diseases.Type: GrantFiled: November 4, 2005Date of Patent: May 14, 2013Assignee: Tufts Medical Center, Inc.Inventors: Athan Kuliopulos, Lidija Covic, Nicole Kaneider
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Patent number: 8389480Abstract: The invention relates generally to G protein coupled receptors and in particular to agonists and antagonists of G protein receptors and methods of using the same.Type: GrantFiled: September 11, 2009Date of Patent: March 5, 2013Assignee: Tufts Medical Center, Inc.Inventors: Athan Kuliopulos, Lidija Covic
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Patent number: 8354378Abstract: The invention relates generally to G protein coupled receptors and in particular to agonists and antagonists of G protein receptors and methods of using the same.Type: GrantFiled: February 27, 2009Date of Patent: January 15, 2013Assignee: Tufts Medical Center, Inc.Inventors: Athan Kuliopulos, Lidija Covic
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Patent number: 8324172Abstract: The invention relates generally to G protein coupled receptors and in particular to agonists and antagonists of G protein receptors and methods of using the same.Type: GrantFiled: November 28, 2006Date of Patent: December 4, 2012Assignee: Tufts Medical Center, Inc.Inventors: Athan Kuliopulos, Lidija Covic
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Publication number: 20120121706Abstract: Matrix metalloproteases (MMPs) play many important roles in normal and pathological remodeling processes including atherothrombotic disease, inflammation, angiogenesis and cancer. This invention relates to the activation of protease-activated receptor-1 (PAR-1) by endogenous platelet MMP-1 collagenase on the surface of platelets. Exposure of platelets to fibrillar collagen converts the surface-bound pro-MMP-1 zymogen to active MMP-1, which promotes aggregation through PAR-1, MMP-1 is shown to cleave the PAR-1 extracellular domain at a novel site, which then strongly activates Rho-GTP signaling pathways, cell shape change and motility, and MAPK signaling. Blockade of MMP-PAR 1 suppresses thrombogenesis under arterial flow conditions and inhibited thrombosis in animals. These studies provide a link between matrix-dependent activation of metalloproteases and platelet-G protein signaling and identify MMP-1/PAR-1 as a new target for the treatment and prevention of arterial thrombosis and other thrombotic diseases.Type: ApplicationFiled: April 12, 2010Publication date: May 17, 2012Applicant: Tufts Medical Center, Inc.Inventors: Athan Kuliopulos, Georgios Koukos
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Publication number: 20120028888Abstract: The invention relates generally to compounds which are allosteric modulators (e.g., negative and positive allosteric modulators, allosteric agonists, and ago-allosteric modulators) of the G protein coupled receptor apelin, also known as the APJ receptor. The APJ receptor compounds are derived from the intracellular loops and domains of the the APJ receptor. The invention also relates to the use of these APJ receptor compounds and pharmaceutical compositions comprising the APJ receptor compounds in the treatment of diseases and conditions associated with APJ receptor modulation, such as heart diseases (e.g., hypertension and tension and heart failure, such as congestive heart failure), cancer, diabetes, stem cell trafficking, fluid homeostasis, cell proliferation, immune function, obesity, metastatic disease, and HIV infection.Type: ApplicationFiled: November 4, 2009Publication date: February 2, 2012Inventors: Jay Janz, Athan Kuliopulos, Thomas J. McMurry
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Publication number: 20110301087Abstract: The invention relates generally to compounds which are allosteric modulators (e.g., negative and positive allosteric modulators, allosteric agonists, and ago-allosteric modulators) of the G protein coupled receptor for corticotrophin releasing hormone (or factor) receptor 1, also known as the CRF1, CRHR1, CRFR1, CRHR, CRF-R. The CRF1 receptor compounds are derived from the intracellular loops and domains of CRF1 receptor. The invention also relates to the use of these CRF1 receptor compounds and pharmaceutical compositions comprising the CRF1 receptor compounds in the treatment of diseases and conditions associated with CRF1 receptor modulation, such as inflammatory bowel disease (peripherally acting), irritable bowel syndrome (IBS), stress response (colonic motor activity), anxiety, sleep disorder, addictive behavior, acute and chronic neurodegeneration, preterm labor and pain.Type: ApplicationFiled: November 4, 2009Publication date: December 8, 2011Inventors: Edward McBride, Athan Kuliopulos, Thomas J. McMurry
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Publication number: 20110300167Abstract: The invention relates generally to compounds which are allosteric modulators (e.g., negative and positive allosteric modulators, allosteric agonists, and ago-allosteric modulators) of the G protein coupled receptor CXCR5. The CXCR5 receptor compounds are derived from the intracellular loops and domains of the CXCR5 receptor. The invention also relates to the use of these CXCR5 receptor compounds and pharmaceutical compositions comprising the CXCR5 receptor compounds in the treatment of diseases and conditions associated with CXCR5 receptor modulation such as autoimmune diseases including lupus, HIV and rheumatoid arthritis, Primary Sjogren's Syndrome, chronic lymphocytic leukemia, Burkitt Lymphoma, colon and breast cancer tumor metastasis, Multiple Sclerosis and compromised immune function.Type: ApplicationFiled: November 4, 2009Publication date: December 8, 2011Inventors: Thomas J. McMurry, Athan Kuliopulos, Lidija Covic
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Publication number: 20110294738Abstract: The invention relates generally to compounds which are allosteric modulators (e.g., negative and positive allosteric modulators, allosteric agonists, and ago-allosteric modulators) of the G protein coupled receptor PTHR1, also known as parathyroid hormone/parathyroid hormone related protein receptor. The PTHR1 compounds are derived from the intracellular loops and domains of the PTHR1 receptor. The invention also relates to the use of these PTHR1 receptor compounds and pharmaceutical compositions comprising the PTHR1 receptor compounds in the treatment of diseases and conditions associated with PTHR1 receptor modulation, such as osteoporosis; humoral hypercalcemia of malignancy; osteolytic and osteoblastic metastasis to bone; primary and secondary hyperparathyroidism associated increase in bone absorption; vascular calcification; psychiatric disorders and cognitive disorders associated with hyperparathyroidism; dermatological disorders; and excess hair growth.Type: ApplicationFiled: November 4, 2009Publication date: December 1, 2011Inventors: Yong Ren, Athan Kuliopulos, Thomas J. McMurry