发明名称 A3 ADENOSINE RECEPTOR ANTAGONISTS
摘要 The present invention provides certain novel pyridine and dihydropyridine derivatives, pharmaceutical compositions comprising one or more of these derivatives, and a method of treating a mammal by selectively blocking an A3 adenosine receptor of the mammal by the administration of a pyridine or dihydropyridine derivative of the present invention. Thus, for example, the present invention provides the following pyridine derivatives of formula (I) or a pharmaceutically acceptable salt thereof; wherein R2 is selected from the group consisting of C1-C6 alkyl, C3-C7 cycloalkyl, and C1-C6 alkoxy C1-C6 alkyl; R3 is selected from the group consisting of C1-C6 alkoxy, C1-C6 alkylsulfanyl, hydroxy, C1-C6 alkoxy C1-C6 alkylsulfanyl, hydroxy C1-C6 alkylsulfanyl, and halo C1-C6 alkylsulfanyl, or R3 together with R4 forms a 3-7 membered heterocyclic ring containing O, N, or S; R4 is selected from the group consisting of C1-C6 alkyl, halo C1-C6 alkyl, hydroxy C1-C6 alkyl, C1-C6 alkoxy, C1-C6 alkylsulfanyl, C1-C6 alkylamino, C1-C6 alkylcarbonyl sulfanyl C1-C6 alkyl, aryl C2-C6 alkenyl, aryl C2-C6 alkynyl, formyl, and acetal; R5 is selected from the group consisting of C1-C6 alkyl, aryl C1-C6 alkyl, hydroxy C1-C6 alkyl, and halo C1-C6 alkyl; and R6 is selected from the group consisting of aryl, C3-C7 cycloalkyl, and haloaryl; wherein said aryl is a phenyl or naphthyl. The compounds of the present invention can be used for inhibiting the binding of ligands to an adenosine receptor of a substrate. The compounds of the present invention can be used for characterizing an adenosine receptor in a substrate.
申请公布号 CA2336967(C) 申请公布日期 2010.06.29
申请号 CA19992336967 申请日期 1999.07.02
申请人 THE UNITED STATES OF AMERICA, REPRESENTED BY THE SECRETARY, DEPARTMENT O F HEALTH AND HUMAN SERVICES 发明人 JACOBSON, KENNETH A.;LI, AN-HU
分类号 C07D213/80;A61K31/451;A61K31/455;A61K31/4738;C07D211/90;C07D213/83;C07D471/04;C07D491/04;C07D495/04 主分类号 C07D213/80
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