| abstract |
The present invention addresses the problem of providing a compound suitable as a pharmaceutical composition, especially as a therapeutic agent for nocturia. It was hoped that inhibiting placental leucine aminopeptidase (P-LAP), which is a metabolic enzyme for AVP, during the night would reduce the frequency of nighttime urination via an antidiuretic effect induced by maintaining/increasing the concentration of endogenous AVP. P-LAP–inhibiting compounds were researched, as a result of which it was found that a (2R)-3-amino-2-(pyridylmethyl)-2-hydroxypropanoic acid derivative has a good P-LAP–inhibiting effect, and that, in tests of antidiuretic effects in water-loaded rats, said compound has an inhibiting effect on urine production, said effect being associated with an increase in the endogenous AVP concentration resulting from P-LAP inhibition. Therefore, the present invention provides a compound that is expected to be used as a therapeutic agent for nocturia, said agent having P-LAP inhibition as a mechanism. |