摘要 |
The present invention relates to compounds of formula (I),;
and their pharmaceutically acceptable salts, solvates, hydrates, geometrical isomers, tautomers, optical isomers or N-oxides, which are inhibitors of SSAO activity. The invention further relates to pharmaceutical compositions comprising these compounds and to the use of these compounds for the treatment of medical conditions wherein inhibition of SSAO activity is beneficial, such as inflammatory diseases and immune disorders. |
主权项 |
1. A compound of formula (I), or a pharmaceutically acceptable salt, solvate, hydrate, geometrical isomer, tautomer, optical isomer or N-oxide thereof, wherein: R1 is selected from:
(a) hydrogen,(b) C1-6-alkyl, and(c) —NR4AR4B; R2 is selected from:
(a) hydrogen,(b) —C(O)OMe,(c) —C(O)NH2, and(d) —C(O)NHMe; R3 is selected from:
(a) C1-6-alkyl,(b) halo-C1-6-alkyl,(c) hydroxy-C1-6-alkyl,(d) C1-6-alkoxy-C1-6-alkyl,(e) halo-C1-6-alkoxy-C1-6-alkyl,(f) N(R4AR4B)—C1-6-alkyl,(g) C6-10-aryl-C1-4-alkyl,(h) heteroaryl-C1-4-alkyl,(i) C6-10-aryloxy-C1-4-alkyl,(j) heteroaryloxy-C1-4-alkyl,(k) C3-8-cycloalkyl,(l) C3-8-cycloalkyl-C1-4-alkyl,(m) heterocyclyl, and(n) heterocyclyl-C1-4-alkyl, wherein any aryl or heteroaryl residue is optionally substituted with one more substituents independently selected from halogen, hydroxy, cyano, nitro, CF3, C1-4-alkyl, C1-4-alkoxy and —NR4AR4B, and wherein any cycloalkyl or heterocyclyl residue is optionally substituted with one or more substituents independently selected from halogen, hydroxy, C1-4-alkyl, C1-4-alkoxy and —NR4AR4B; R4A and R4B are each independently selected from:
(a) hydrogen,(b) C1-6-alkyl, and(c) C1-6-acyl provided that when R1 and R2 are hydrogen, then R3 is not benzyl. |