Pyrrolidine derivatives and their use as chymase inhibitor

   
   

Novel pyrrolidine derivatives, being useful as chymase inhibitor or intermediate for synthesis of the active compounds, which has the formula (I): wherein R.sup.1 is cycloalkyl, substituted or unsubstituted phenyl or naphthyl, indanyl, thienyl, furyl, substituted or unsubstituted indolyl, benzofuryl, substituted or unsubstituted benzothienyl, etc.; R.sup.2 is H, alkyl, phenyl-lower alkyl, cycloalkyl or cycloalkyl-lower alkyl; R.sup.3 is (i) substituted or unsubstituted monocyclic heterocyclic group, (ii) substituted or unsubstituted benzene- or pyridine-fused heterocyclic group, or (iii) a group (a): R.sup.4 and R.sup.5 are independently H or OH, but R.sup.4 and R.sup.5 are not simultaneously H, or both form oxo; n is 0, 1, 2 or 3; or a salt thereof. ##STR1##

Derivatives do pyrrolidine da novela, sendo útil como o inibidor ou o intermediário do chymase para a síntese dos compostos ativos, que tem a fórmula (i): wherein R.sup.1 é phenyl substituído ou unsubstituted do cycloalkyl, ou naphthyl, de indolyl de indanyl, de thienyl, benzothienyl substituído ou unsubstituted furyl, substituído ou unsubstituted, de benzofuryl, etc.; R.sup.2 é H, alkyl, um alkyl phenyl-mais baixo, um cycloalkyl ou um alkyl cycloalkyl-mais baixo; R.sup.3 é (i) grupo heterocyclic monocyclic substituído ou unsubstituted, (ii) benzene- substituído ou unsubstituted ou pyridine-fundiu o grupo heterocyclic, ou (iii) um o grupo (a): R.sup.4 e R.sup.5 são independentemente H ou OH, mas R.sup.4 e R.sup.5 não são simultaneamente H, ou ambo formulário oxo; n é 0, 1, 2 ou 3; ou um sal disso. ## do ## STR1

 
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