Partial and full agonists of A1 adenosine receptors
AssigneeCV Therapeutics, Inc.
InventorsArvinder Dhalla, Elfatih Elzein, Prabha Ibrahim, Venkata Palle, Vaibhav Varkhedkar, Jeff Zablocki
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Abstract
Disclosed are novel compounds a compound of Formula I that are partial and full A1 adenosine receptor agonists, useful for treating various disease states, in particular dyslipidemia, diabetes, decreased insulin sensitivity, Polycystic Ovarian Syndrome, Stein-Leventhal syndrome, and obesity.
Claims22
A method of increasing insulin sensitivity in a mammal in need thereof, comprising administering to a mammal in need thereof a therapeutically effective dose of a compound of Formula I:
- wherein:
- R is hydrogen or lower alkyl;
- R1 is optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted aryl, or optionally substituted heteroaryl;
- or
- R and YR1 when taken together with the nitrogen atom to which they are attached represents optionally substituted heterocyclyl;
- R2 is hydrogen, halo, trifluoromethyl, acyl, or cyano;
- R3 is optionally substituted cycloalkyl, optionally substituted aryl;
- optionally substituted heteroaryl, or optionally substituted heterocyclyl,
- R4 and R5 are independently hydrogen or acyl;
- and
- X and Y are independently a covalent bond or optionally substituted alkylene;
- with the proviso that when R1 is methyl and Y is a covalent bond, R3 cannot be phenyl when X is methylene or ethylene.
A pharmaceutical composition comprising at least one pharmaceutically acceptable excipient and a therapeutically effective amount of a compound of Formula I
- wherein:
- R is hydrogen or lower alkyl;
- R1 is optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted aryl, or optionally substituted heteroaryl;
- or
- R and YR1 when taken together with the nitrogen atom to which they are attached represents optionally substituted heterocyclyl;
- R2 is hydrogen, halo, trifluoromethyl, acyl, or cyano;
- R3 is optionally substituted cycloalkyl, optionally substituted aryl;
- optionally substituted heteroaryl, or optionally substituted heterocyclyl,
- R4 and R5 are independently hydrogen or acyl;
- and
- X and Y are independently a covalent bond or optionally substituted alkylene;
- with the proviso that when R1 is methyl and Y is a covalent bond, R3 cannot be phenyl when X is methylene or ethylene.
Dependencies are inferred from the claim text.