Novel benzamidine derivatives, process for the preparation thereof and pharmaceutical composition for preventing or treating osteporosis comprising the same

A benzamidine derivative represented by the following Formula 1 or a pharmaceutically acceptable salt thereof:

• wherein R1 is methyl, ethyl, isopropyl, phenyl, pyridinyl, cyclohexyl, morpholinyl,
• which is unsubstituted or substituted with C1˜C6 alkyl, NR6R7 or CH2NR6R7;
• R2 is a primary or secondary amine, which is NR8R9,
• piperidine, pyrrolidine, imidazole or triazole;
• R3 and R4 are each independently hydrogen, methyl, ethyl, halogen, hydroxy or methoxy group;
• R5 is a hydroxy group;
• R6 and R7 are each independently hydrogen, methyl, ethyl, propyl, hydroxyethyl, methoxyethyl, 2-morpholinoethyl, benzyl, pyridin-3-ylmethyl, pyridin-4-ylmethyl, 3-pyridinylcarbonyl or ethanesulfonyl;
• R8 and R9 are each independently hydrogen;
• methyl;
• ethyl;
• propyl;
• isopropyl;
• butyl;
• isobutyl;
• t-butyl;
• hydroxyethyl;
• methoxyethyl;
• 2-morpholinoethyl;
• benzyl;
• 3-imidazol-1-yl-propyl;
• cyclopropyl;
• or carbonyl substituted with one group selected from 3-pyridinyl and 4-pyridinyl;
• R10 and R11 are each independently hydrogen or methyl;
• X1 and X3 are each independently oxygen, sulfur, amine or methylamine group;
• X2 is propylene, butylene, pentylene, hexylene, ethylene-O-ethylene, ethylene-NH-ethylene, butylene carbonyl, 2-butenyl, methylene-1,2-phenylene-methylene, methylene-1,3-phenylene-methylene, methylene-1,4-phenylene-methylene or methylene-pyridinyl-methylene;
• Y is O, S or methylamino or CH2 group;
• and
• n is an integer of 0 or 1.