Patent application number | Description | Published |
20080214451 | G Protein Coupled Receptor Agonists and Antagonists and Methods of Use - 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. | 09-04-2008 |
20090270322 | G PROTEIN COUPLED RECEPTOR ANTAGONISTS AND METHODS OF ACTIVATING AND INHIBITING G PROTEIN COUPLED RECEPTORS USING THE SAME - 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. | 10-29-2009 |
20100137207 | G PROTEIN COUPLED RECEPTOR AGONISTS AND ANTAGONISTS AND METHODS OF ACTIVATING AND INHIBITING G PROTEIN COUPLED RECEPTORS USING THE SAME - 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. | 06-03-2010 |
20110294738 | PTHR1 RECEPTOR COMPOUNDS - 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. | 12-01-2011 |
20110300167 | CXCR5 RECEPTOR COMPOUNDS - 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. | 12-08-2011 |
20110301087 | CRF1 RECEPTOR COMPOUNDS - 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. | 12-08-2011 |
20120028888 | APJ RECEPTOR COMPOUNDS - 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. | 02-02-2012 |
20120121706 | PAR-1 Activation by Metalloproteinase-1 (MMP-1) - 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. | 05-17-2012 |
20130210709 | CXCR4 Receptor Compounds - 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. | 08-15-2013 |
20150023975 | PAR-1 Activation by Metalloproteinase-1 (MMP-1) - 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. | 01-22-2015 |