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US 2010/0075977 A1Published application
Beta-3 receptor ligands and their use in therapy
AssigneeUniversita' Degli Studi Di Bari
InventorsAntonio Scilimati, Maria Grazia Perrone, Ernesto Santandrea
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Abstract
The present invention relates to new compounds, ligands of the beta-3 adrenergic receptor, their preparation and their use in therapy or as research tools for said receptor; the invention also relates to a process for the preparation of the compounds of the invention and the use of inverse agonists of the beta-3 adrenergic receptor as medicaments.
Claims32
A compound of formula (I)
- wherein:
- R represents a hydrogen atom, a hydroxyl group, an alkoxyl group, an alkyl group, a carbaldoxime group or a halogen atom;
- R1 represents a hydrogen atom or a methyl group;
- R2 represents a hydrogen atom, a hydroxyl group, an alkoxyl group, an alkyl group or a halogen atom;
- R3, R4 each independently represents an alkyl group or R3 represents an atom of hydrogen and R4 is an alkyl group;
- R5 represents a hydrogen atom or an alkyl group;
- and its salts and solvates.
4 more elements
A compound of formula (II)
- wherein
- Y is CH or N;
- Z is a direct bond or a —O—CH2— group wherein the oxygen atom is bound to the ring;
- n is 0, 1 or 2, provided that when n is 1 or 2, X is N and when n is 0, X is NH, O or S;
- R6 is a hydrogen atom, an alkyl group, an optionally substituted aryl group, a optionally substituted heteroaryl group, a halogen atom, —OH, NH2, —O-alkyl, optionally substituted-O-aryl, optionally substituted-O-heteroaryl, —NH—CO—R8, -optionally substituted —NH—CO-aryl, optionally substituted —NH—CO-heteroaryl, —NH—SO2-alkyl, optionally substituted NH—SO2-aryl, optionally substituted —NH—SO2-heteroaryl, —NH—SO2—R8, a nitro group;
- or when Y is CH, R6 is an aromatic group or heteroaromatic fused with the benzene ring to form a naphthalene or carbazole group;
- R7 is R8SO2—, optionally substituted R8CO—, —CO-aryl, optionally substituted —CO-heteroaryl, optionally substituted —SO2-aryl, optionally substituted —SO2-heteroaryl;
- R8 is an alkyl group;
- and its salts and solvates.
6 more elements
Use of a compound as inverse agonist of the beta-3 adrenergic receptor for the preparation of a medicament for the treatment of metabolic syndrome, cachexia and heart failure.
Dependencies are inferred from the claim text.