Biguanide derivative, a preparation method thereof and a pharmaceutical composition containing the biguanide derivative as an active ingredient

摘要

A biguanide derivative compound with N1-N5 substitution, which is represented by Formula 1, or a pharmaceutically acceptable salt thereof, a method of preparing the same, and a pharmaceutical composition containing the same as an active ingredient are provided. The biguanide derivative may exhibit excellent effect on activation of AMPKα and inhibition of cancer cell proliferation in a low dose, compared to conventional drugs, and thus, may be useful to treat diabetes mellitus, obesity, hyperlipidemia, hypercholesterolemia, fatty liver, coronary artery disease, osteoporosis, polycystic ovarian syndrome, metabolic syndrome, cancer, etc.

主权项

1. A compound of Formula 1 or a pharmaceutically acceptable salt thereof: wherein R1 is unsubstituted C1-7 alkyl; C1-4 alkyl substituted with C5-12 aryl; or C5-12 aryl,
R2 is hydrogen; or unsubstituted C1-7 alkyl,R3 is hydrogen; or C5-12 aryl,R4 is a non-hydrogen substituent selected from the group consisting of unsubstituted C6-7 alkyl; C1-4 alkyl substituted with at least one non-hydrogen substituent selected from the group consisting of C5-12 heteroaryl and C1-4 alkoxycarbonyl; unsubstituted C5-7 cycloalkyl; C5-12 aryl; and C5-12 heteroaryl, andthe aryl and heteroaryl may be unsubstituted or substituted with at least one non-hydrogen substituent selected from the group consisting of C1-4 alkoxy, hydroxyl and halogen, and the aryl and heteroaryl may be selected from the group consisting of phenyl, pyridinyl, furanyl and isoquinolinyl.