Partial and full agonists of A1 adenosine receptors
OwnerJeff Zablocki, Venkata Palle +2inventors
InventorsJeff Zablocki, Venkata Palle, Elfatih Elzein, Xiaofen Li
Life of this patent
Estimating the term…
Abstract
Disclosed are novel compounds that are partial and full A1 adenosine receptor agonists, useful for treating various disease states, in particular the supraventricular tachycardias, emesis, angina, myocardial infarction and hyperlipidemia.
Claims34
A compound of the formula:
- wherein:
- R1 is optionally substituted cycloalkyl, optionally substituted heterocyclyl, optionally substituted aryl, or optionally substituted heteroaryl;
- R2 is hydrogen, halo, trifluoromethyl, or cyano;
- R3 is hydrogen, optionally substituted cycloalkyl, optionally substituted aryl, optionally substituted heteroaryl, or optionally substituted heterocyclyl,
- R4 and R5 are independently hydrogen or optionally substituted acyl;
- X is a covalent bond or lower alkylene optionally substituted by cycloalkyl;
- X1 is a covalent bond or alkylene.
- Y is a covalent bond or lower alkylene optionally substituted by hydroxy or cycloalkyl;
- and
- Z is —C≡C—, —R6C═CR7—, or —CHR6CHR7—, in which R6 and R7 at each occurrence are hydrogen or lower alkyl.
A pharmaceutical composition comprising at least one pharmaceutically acceptable excipient and a therapeutically effective amount of a compound of Formula I.
- wherein:
- R1 is optionally substituted cycloalkyl, optionally substituted heterocyclyl, optionally substituted aryl, or optionally substituted heteroaryl;
- R2 is hydrogen, halo, trifluoromethyl, or cyano;
- R3 is optionally substituted cycloalkyl, optionally substituted aryl, optionally substituted heteroaryl, or optionally substituted heterocyclyl,
- R4 and R5 are independently hydrogen or optionally substituted acyl;
- X is a covalent bond or lower alkylene optionally substituted by cycloalkyl;
- X1 is a covalent bond or alkylene;
- Y is a covalent bond or lower alkylene optionally substituted by hydroxy or cycloalkyl;
- and
- Z is —C≡C—, —R6C═CR7—, or —CHR6CHR7—, in which R6 and R7 at each occurrence are hydrogen or lower alkyl.
The method of claim 33, wherein the disease state is selected from atrial fibrillation, supraventricular tachycardia and atrial flutter.
The method of claim 33, wherein the disease state is chosen from diabetes and obesity.
Dependencies are inferred from the claim text.