Patent · US Active

Pyridine derivatives

US10005762B2 · kind B2 · utility

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11Claims
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Key dates

Filing dateDec 4, 2015
Grant dateJun 26, 2018
Priority date
Expiry dateDec 4, 2035

Classification

  • Technology area (CPC C)Chemistry; Metallurgy
  • CPC primaryC07D401/04
  • WIPO fieldPharmaceuticals
  • WIPO sectorChemistry

Abstract

The problem to be solved by the present invention is to provide a compound suitable for a pharmaceutical composition, specifically an agent for treating nocturia.The inventors have assumed that inhibition of nocturnal activity of placental leucine aminopeptidase (P-LAP), i.e. aminopeptidase that cleaves AVP, would maintain and/or increase an endogenous AVP level to enhance the antidiuretic effect, which would contribute to a decreased number of nocturnal voids, and have extensively studied compounds which inhibit P-LAP. As a result, the inventors have found that (2R)-3-amino-2-(pyridylmethyl)-2-hydroxy-propanoic acid derivatives have excellent P-LAP inhibitory activity. The inventors have evaluated antidiuretic effects in water-loaded rats and have found that the compounds increase endogenous AVP levels by inhibiting P-LAP and consequently reduce urine production. The present invention therefore provides compounds expected to be used as an agent for treating nocturia based on P-LAP inhibition.

Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.