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US 12,129,273 B2Granted
Compound with analgesic effect for use in prevention and treatment of pain
AssigneeAcademia Sinica
InventorsChih-Cheng Chen, Jim-Min Fang, Cheng-Han Lee, Jen-Yao Chang
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Abstract
Compounds for use in prevention and/or treatment of pain are disclosed. The compounds are derived by conjugation of N6-(4-hydroxybenzyl)adenosine and analogous compounds with amino acids or peptides. In one embodiment of the invention, the compound is 5′-glycylcarbonyl-N6-(4-hydroxybenzyl)adenosine (I-a1). In another embodiment of the invention, the compound is 5′-deoxy-5′-(N′-glycylureido)-N6-(4-hydroxybenzyl)adenosine (I-d1). Also disclosed are methods of making and using the same.
Claims6
A compound of formula (II):
- wherein:
- k is 1, 2 or 3;
- X and Y are each independently NH, O or S;
- R2 and R3 are each independently OH, NH2, NO2, haloalkyl, hydroxyalkyl or alkylamino;
- and
- R4 is selected from an amino acid or a peptide,
- wherein when R4 is an amino acid, R4 is linked to the C(═O) in the structure via the backbone amino group or side chain amino group, and the carboxy group of the amino acid is optionally a methyl or ethyl ester, and
- wherein when R4 is a peptide, R4 is linked to the C(═O) in the structure via the N-terminal amino acid group of said peptide, or a side chain amino group of an amino acid in the peptide, wherein the C-terminal of the peptide is optionally modified;
- ring A is a substituted or unsubstituted aromatic heterocycle, wherein the aromatic heterocycle comprises a 5- or 6-membered heterocycle or a fused heterocycle, wherein the heteroatom(s) in the heterocycle are one or more of nitrogen, oxygen, and/or sulfur heteroatoms;
- a tautomer or stereoisomer thereof;
- and
- a pharmaceutically acceptable salt of the foregoing.
9 more elements
Dependencies are inferred from the claim text.