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US 6,686,366 B1Granted
Compounds specific to adenosine A3 receptor and uses thereof
AssigneeOSI Pharmaceuticals, Inc.
InventorsArlindo L. Castelhano, Bryan McKibben, David J. Witter
Life of this patent
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Abstract
This invention pertains to compounds which specifically inhibit the adenosine A3 receptor and the use of these compounds to treat a disease associated with A3 adenosine receptor in a subject, comprising administering to the subject a therapeutically effective amount of the compounds.
Claims50
A compound having the structure:
- wherein R1 is H and R2 is cyclopropyl methylamino carbonylethyl, cis-3-hydroxy cyclopentyl, acetamido butyl, methylamino carbonylamino butyl, ethylamino carbonylamino propyl, methylamino carbonylamino propyl, 2-acetyl amino-3-methyl butyl, N,N-diethylamino carbonylamino ethyl, thioacetamido ethyl, 3-amino acetyloxy cyclopentyl, 3-hydroxy cyclopentyl, 2-pyrrolyl carbonyl aminoethyl, 2-imidazolidinone ethyl, 1-aminocarbonyl-2-methyl propyl, 1-aminocarbonyl-2-phenyl ethyl, 3-hydroxy azetidino, 2-imidazolyl ethyl, acetamido ethyl, 1-(R)-phenyl-2-hydroxyethyl, N-methylaminocarbonyl pyridyl-2-methyl, or R1, R2 and the nitrogen together are 3-acetamido piperadino, 3-hydroxy pyrrolidino, 3-methyloxy carbonylmethyl pyrrolidino, 3-aminocarbonylmethyl pyrrolidino, or 3-hydroxymethyl piperadino;
- wherein R3 is a substituted or unsubstituted four to six membered cycloalkyl or aryl ring;
- wherein R5 is H, alkyl, substituted alkyl, aryl, or substituted aryl;
- and
- wherein R6 is H, alkyl, substituted alkyl, or cycloalkyl.
2 more elements
A compound having the structure:
- wherein m is 0, 1, or 2;
- wherein R1 is cyclopropyl methyl, methyl, methylamino, or aminomethyl;
- wherein R3 is aryl, substituted aryl, heteroaryl;
- wherein R5 is H, alkyl, substituted alkyl, aryl, arylalkyl, amino, substituted aryl, wherein said substituted alkyl is —C(R9)(R10)NR7R8, wherein R9 and R10 are each H or alkyl, wherein R7 and R8 are each alkyl or cycloalkyl, or R7, R8 and the nitrogen together form a ring system of between 4 and 7 members;
- and
- wherein R6 is H, alkyl, substituted alkyl, or cycloalkyl.
3 more elements
A compound having the structure:
- wherein R3 is unsubstituted aryl;
- wherein R5 is H, alkyl, substituted alkyl, aryl, arylalkyl, amino, substituted aryl, wherein said substituted alkyl is —C(R9)(R10)NR7R8, wherein R9 and R10 are each H or alkyl, wherein R7 and R8 are each alkyl or cycloalkyl, or R7, R8 and the nitrogen together form a ring system of between 4 and 7 members;
- and
- wherein R6 is H, alkyl, substituted alkyl, or cycloalkyl.
1 more element
Dependencies are inferred from the claim text.