| 摘要 |
The present invention relates to the N-phosphonomethyl substituted tetrazole derivatives of formula (I) and tautomers thereof wherein R0 represents (i) a group of formula (Ia) or (ii) a group of formula -X-COR3 (Ib); R and R' represent independently hydrogen, carbocyclic aryl, 6-tetrahydronaphthyl, 5-indanyl, (alpha)-(trichloromethyl, carboxyl, esterified carboxyl or amidated carboxyl) substituted-(lower alkyl or aryl-lower alkyl), acyloxymethyl optionally monosubstituted on methyl carbon by lower alkyl, by C5-C7-cycloalkyl, by aryl or by aryl-lower alkyl; R1 represents phenyl, or phenyl substituted by lower alkyl, lower alkoxy, halogen or trifluoromethyl; or R1 represents thienyl or furanyl optionally substituted by lower alkyl; or R1 represents hydrogen, if R0 represents a group of formula (Ia); R2 and R4 represent hydrogen, lower alkyl, hydroxy, lower alkoxy, halogen or trifluoromethyl; n is 0, 1 or 2; COR3 carboxyl or carboxyl derivatized in form of a pharmaceutically acceptable ester; X represents a direct bond, C1-4-alkylene or C2-4-alkenylene; and pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising said compounds; methods for preparation of said compounds and for the preparation of intermediates; and methods of treating disorders in mammals which are responsive to the inhibition of neutral endopeptidases by administration of said compounds to mammals in need of such treatment. |
