Vitronectin receptor antagonists
View Patent ↗Compounds of the formula (I) are disclosed which are vitronectin receptor antagonists and are useful in the treatment of osteoporosis: wherein R 1 is Het or Ar R 2 is or a pharmaceutically acceptable salt thereof.
1. A compound according to formula (I):
wherein:
R 1 is
in which R′ is C 1-4 alkyl and R″ is phenyl, benzyl or —CH 2 CF 3 ; or R′ and R″ are joined to form a morpholinyl ring;
R 2 is
or a pharmaceutically acceptable salt thereof.
2. A compound according to claim 1 in which R 2 is:
3. A compound according to claim 1 in which R 2 is:
4. A compound which is:
(±)-4-[4-[2-[6-(methylamino)pyridin-2-yl]-1-ethoxy]phenyl]-3-[4-(trifluoromethyl)phenyl]butanoic acid;
(±)-4-[4-[2-[6-(methylamino)pyridin-2-yl]-1-ethoxy]phenyl]-3-[4-[(N-methyl-N-phenylamino)carbonyl]-1,3-oxazol-2-yl]butanoic acid;
(±)-4-[4-[2-[6-(methylamino)pyridin-2-yl]-1-ethoxy]phenyl]-3-[4[(morpholin-4-yl)carbonyl]-1,3-oxazol-2-yl]butanoic acid;
(±)-4-[4-[2-[6-(methylamino)pyridin-2-yl]-1-ethoxy]phenyl]-3-[4-[[N-methyl-N-(2,2,2-trifluoroethyl)amino]carbonyl]-1,3-oxazol-2-yl]butanoic acid;
(±)-4-[4-[2-[6-(methylamino)pyridin-2-yl]-1-ethoxy]phenyl]-3-[4-(trifluoromethyl)thiazol-2-yl]butanoic acid;
(±)-4-[4-[2-[6-(methylamino)pyridin-2-yl]-1-ethoxy]phenyl]-3-(3-methylthiazol-2-yl)butanoic acid;
(S)-3-(3-fluorophenyl)-4-[4-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethoxy]phenyl]butanoic acid;
(±)-4-[4-[2-[6-(methylamino)pyridin-2-yl]ethoxy]phenyl]-3-(pyridin-3-yl)butanoic acid;
(S)-4-[4-[2-[6-(methylamino)pyridin-2-yl]ethoxy]phenyl]-3-(pyridin-3-yl) butanoic acid; or
(S)-3-(pyridin-3-yl)-4-[4-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethoxy]phenyl]butanoic acid;
or a pharmaceutically acceptable salt thereof.
5. A pharmaceutical composition which comprises a compound according to claim 1 and a pharmaceutically acceptable carrier.
6. A method of treating osteoporosis which comprises administering to a subject in need thereof a therapeutically effective amount of a compound according to claim 1 .