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US 2014/0179633 A1Published application
Composition comprising pyrazino-triazine derivatives
AssigneeJw Pharmaceutical Corporation
InventorsMin-Seok Choi, Young-Hoon Kim
Life of this patent
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Abstract
Disclosed is a composition including a pyrazino-triazine derivative and a pharmaceutically acceptable salt thereof. The composition includes a solubilizer or a stabilizer and thus can exhibit very excellent solubility and stability.
Claims15
A composition, comprising:
- at least one compound selected from the group consisting of a compound represented by Chemical Formula 1 below, an isomer thereof and a pharmaceutically acceptable salt thereof, as an active ingredient,
- wherein the composition comprises a solubilizer and a stabilizer,
- wherein the solubilizer is one or more selected from the group consisting of a saccharide, an alcohol, an acid, a salt and a polymer and the stabilizer including one or more selected from the group consisting of a saccharide, an acid, a salt, an antioxidant, and a polymer:
- wherein R1 is substituted or unsubstituted C3˜C10 aryl, or substituted or unsubstituted C3˜C10 heteroaryl with at least one nitrogen (N) atom;
- R3 is hydrogen, C1˜C6 alkyl, C2˜C6 alkenyl, C2˜C6 alkynyl, C3˜C10 heteroaryl with at least one nitrogen (N) atom, C3˜C10 arylalkyl, or C3˜C10 heteroarylalkyl with at least one nitrogen (N) atom;
- A is hydrogen or C1˜C6 alkyl;
- B is hydrogen or C1˜C6 alkyl;
- X is —O—PO3H2, —O—SO2NH2, carbamate,
- and
- Y is hydrogen, C3˜C10 aryl, C3˜C10 heteroaryl with at least one nitrogen (N) atom, or C1˜C6 alkyl.
7 more elements
A method of stabilizing a composition comprising at least one compound selected from the group consisting of a compound represented by Chemical Formula 1 below, an isomer thereof and a pharmaceutically acceptable salt thereof, as an active ingredient,
- comprising the step of mixing the composition with at least one stabilizer selected from the group consisting of a saccharide, an acid, a salt, an antioxidant and a polymer:
- wherein R1 is substituted or unsubstituted C3˜C10 aryl, or substituted or unsubstituted C3˜C10 heteroaryl with at least one nitrogen (N) atom;
- R3 is hydrogen, C1˜C6 alkyl, C2˜C6 alkenyl, C2˜C6 alkynyl, C3˜C10 heteroaryl with at least one nitrogen (N) atom, C3˜C10 arylalkyl, or C3˜C10 heteroarylalkyl with at least one nitrogen (N) atom;
- A is hydrogen or C1˜C6 alkyl;
- B is hydrogen or C1˜C6 alkyl;
- X is —O—PO3H2, —O—SO2NH2, carbamate,
- and
- Y is hydrogen, C3˜C10 aryl, C3˜C10 heteroaryl with at least one nitrogen (N) atom, or C1˜C6 alkyl.
5 more elements
Dependencies are inferred from the claim text.