Method for the treatment of pancreatitis
Inventors
LEE, Heon Jong • Jung, Hoe Yune • Lee, In-Kyu • Jeon, Jae-Han • Cho, Sung Jin
Assignees
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Publication Number
US-11413270-B2
Publication Date
2022-08-16
Expiration Date
Abstract
A composition for preventing and/or treating pancreatitis and a method of prevention and/or treatment of pancreatitis are disclosed. The composition include an aryl ethene compound, a pharmaceutically acceptable salt thereof, or a solvate thereof, as an active ingredient. The method includes administering the aryl ethene compound, an isomer, a pharmaceutically acceptable salt thereof, or a solvate thereof, in an effective amount to a subject in need thereof.
Core Innovation
The disclosure relates to methods for treating and/or preventing pancreatitis in a subject in need thereof by administering an effective amount of selected compounds. The disclosed compounds are aryl-ethene (ERRγ-inhibiting) compounds defined by chemical formulas, together with pharmaceutically acceptable salts, solvates, and isomers, and illustrative scaffolds and example compounds including DMRC200434 and related analogs.
A biological rationale is presented that the compounds act as ERRγ inverse agonists/antagonists, with binding information and selectivity for ERRγ. The disclosure further relates the activity to ERRγ protein, Esrrg mRNA, and related markers, and also references ERRα/ERRγ regulation.
Pharmacological effects are described in acute pancreatitis contexts, including mouse models such as caerulein-induced pancreatitis, TLCS (taurolithocholic acid 3-sulfate), and sodium taurocholate-induced acute pancreatitis. Reported effects include reductions in serum amylase and serum lipase, decreased tissue trypsin activity, improved histopathology, and effects exemplified by DMRC200434.
Claims Coverage
The provided independent claims include two independent methods, each directed to administering an effective amount of a specified compound for pancreatitis prevention and/or treatment. Across the independent claims, the core inventive feature centers on selected aryl-ethene compounds, including isomer, pharmaceutically acceptable salt, solvate, or therapeutically acceptable salt variants.
Administering a selected aryl-ethene compound for pancreatitis prevention and/or treatment
A method for treating and/or preventing pancreatitis in a subject in need thereof comprising administering an effective amount of a compound selected from the disclosed compounds, or an isomer, a pharmaceutically acceptable salt thereof, or a solvate thereof.
Administering (E)-5-(4-hydroxyphenyl)-5-(4-(4-isopropylpiperazin-1-yl)phenyl)-4-phenylpent-4-en-1-ol for pancreatitis prevention and/or treatment
A method for preventing and/or treating pancreatitis in a subject in need thereof comprising administering an effective amount of (E)-5-(4-hydroxyphenyl)-5-(4-(4-isopropylpiperazin-1-yl)phenyl)-4-phenylpent-4-en-1-ol, or a therapeutically acceptable salt thereof, to the subject.
Together, the independent claims cover administering effective amounts of specified aryl-ethene (ERRγ-inhibiting) compounds, including explicit compound selection and specific compound identity, with coverage for isomer and pharmaceutically or therapeutically acceptable salt or solvate forms, in methods for preventing and/or treating pancreatitis.
Stated Advantages
Reductions in serum amylase and serum lipase.
Decreased tissue trypsin activity.
Improved histopathology.
Treating and/or preventing pancreatitis in a subject in need thereof.
Documented Applications
Acute pancreatitis efficacy in a mouse model using caerulein-induced pancreatitis.
Acute pancreatitis efficacy in a mouse model using TLCS (taurocholic acid 3-sulfate).
Methods for treating and/or preventing pancreatitis, including acute pancreatitis, in a subject (including a mammal, notably human).
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