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US 2003/0078232 A1Published application
Adenosine receptor A3 agonists
OwnerElfatih Elzein, Venkata Palle +2inventors
InventorsElfatih Elzein, Venkata Palle, Vaibhav Varkhedkar, Jeff Zablocki
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Abstract
Disclosed are novel compounds that are A3 adenosine receptor agonists, useful for treating various disease states, including cancer, cardiac ischemia, leukopenia, and neutropennia.
Claims33
A compound of the formula:
- 21
- wherein:
- R1 is optionally substituted lower alkyl, optionally substituted cycloalkyl, optionally substituted aryl, or optionally substituted heteroaryl;
- X is a covalent bond or optionally substituted alkylene;
- R2 is R4—Z—Y—C≡C— or optionally substituted pyrazolyl:
- in which Y is optionally substituted alkylene, Z is oxygen, sulfur or —NH—, and R4 is optionally substituted aryl or optionally substituted heteroaryl;
- and
- R3 is hydroxymethyl or —C(O)—NR5R6;
- in which R5 and R6 are independently hydrogen or lower alkyl.
6 more elements
A process for the preparation of a compound of Formula I:
- 22
- in which R2 is optionally substituted pyrazol-1-yl;
- comprising:
- contacting a compound of the formula:
- 23
- with a compound of formula:
- 24
4 more elements
A process for the preparation of a compound of Formula I:
- 25
- in which R2 is optionally substituted pyrazol-4yl;
- comprising
- contacting a compound of the formula:
- 26
- with a compound of the formula:
- 27
- in the presence of a palladium complex and a copper salt in an inert solvent, and contacting the product with a mild acid.
5 more elements
Dependencies are inferred from the claim text.