Pyrazine-containing compound
Inventors
Velicelebi, Gonul • Stauderman, Kenneth • Dunn, Michael • Roos, Jack
Assignees
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Abstract
Compositions and methods related to the amelioration of pancreatitis through the pharmaceutical manipulation of calcium signaling are disclosed. Such compositions and methods may be used to ameliorate symptoms of acute or chronic pancreatitis or to reduce the chance or severity of pancreatitis in an individual at risk of the condition. In other embodiments, disclosed herein are compositions and methods related to the amelioration of viral diseases through the pharmaceutical manipulation of calcium signaling. In further embodiments, disclosed herein are compositions and methods related to the amelioration of Th17-induced diseases through the pharmaceutical manipulation of calcium signaling.
Core Innovation
The document describes intracellular calcium signaling inhibitors, including inhibitors of SOC/CRAC calcium channels targeting STIM1 and Orai proteins, as a way to ameliorate or prevent acute pancreatitis and chronic pancreatitis. The concept prevents excessive Ca2+ influx through SOC/CRAC channels and is linked to reducing inappropriate premature trypsin activation and pancreatic autodigestion/necrosis.
The disclosure extends to viral disease contexts, including hemorrhagic fever viruses such as Ebola, Marburg, and Lassa. It further extends to Th17-induced autoimmune/inflammatory diseases by blocking Th17 differentiation using intracellular calcium signaling inhibition.
The disclosure includes a set of specific small-molecule calcium channel inhibitor candidates, including Compound I and a broad “Compound A” structure group, along with specific named exemplified compounds. It also enumerates symptom sets for acute and chronic pancreatitis and describes prophylactic use in at-risk individuals with CRAC/SOC inhibitors.
Claims Coverage
Only one independent claim is explicitly provided in the partial content: clm-00001. The claim coverage centers on a single specifically named compound (or a pharmaceutically acceptable salt), with one dependent refinement directed to a pharmaceutical composition including that compound and a pharmaceutically acceptable excipient.
N-(5-(2,5-dimethylbenzo[d]oxazol-6-yl)thiazol-2-yl)-2,3,6-trifluorobenzamide compound
A compound having the chemical name N-(5-(2,5-dimethylbenzo[d]oxazol-6-yl)thiazol-2-yl)-2,3,6-trifluorobenzamide or a pharmaceutically acceptable salt thereof.
Pharmaceutical composition including the compound and an excipient
A pharmaceutical composition that includes the compound of the named chemical formula together with a pharmaceutically acceptable excipient.
Based on the provided claim text, the patent claim coverage is limited to a specifically named compound (or pharmaceutically acceptable salt) and a pharmaceutical composition that includes the compound with a pharmaceutically acceptable excipient. No additional inventive features beyond these elements are explicitly provided in the partial claim set.
Stated Advantages
Not explicitly described in patent.
Documented Applications
Ameliorating or preventing acute pancreatitis and chronic pancreatitis by preventing excessive Ca2+ influx and reducing inappropriate premature trypsin activation and pancreatic autodigestion/necrosis.
Treatment or prevention of viral diseases, including hemorrhagic fever viruses such as Ebola, Marburg, and Lassa, using intracellular calcium signaling inhibition.
Addressing Th17-induced autoimmune/inflammatory diseases by blocking Th17 differentiation.
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