Phosphorous containing dhp enzyme inhibitors

Abstract

Abstract Compounds of the formula: <IMAGE> wherein R1 is C2-C12 linear or branched unsubstituted alkyl; C1-C12 linear or branched substituted alkyl; C2-C12 linear or branched monoalkenyl; C2-C12 linear or branched alkynyl; C7-C20 aralkyl, wherein the alkyl chain is linear or branched C1-C8 and the aryl moiety is C6-C12; C4-C10 cycloalkylalkyl; C3-C7 cycloalkyl; wherein these values for R1, other than C2-C12 linear or branched unsubstituted alkyl, can be substituted by one or more of C1-C4 alkoxy, C3-C6 cycloalkyloxy, C3-C6 cycloalkylthio, C6-C12 aryloxy, C1-C4 alkylthio, C6-C12 arylthio, C7-C10 aralkyloxy, C7-C16 aralkyl-thio; and R5 is H or C1-C12 linear or branched alkyl; C2-C12 linear or branched monoalkenyl; C7-C20 aralkyl, wherein the alkyl chain is linear or branched C1-C8 and the aryl moiety is C6-C12; heterocyclic alkyl wherein the alkyl chain is linear or branched C1-C8 and the heterocyclic ring is 5-6 membered, optionally fused with a benzene ring, fully aromatic, containing 1 to 2 of oxygen, nitrogen or sulfur as heteroatoms; C4-C10 cycloalkylalkyl; C3-C7 cycloalkyl; wherein the values for R5 can be substituted by one or more of halo, hydroxy, carboxy, C1-C4 alkoxycarbonyl, C7-C16 arylalkoxycarbonyl, C3-C7 cycloalkyl, C1-C4 alkoxy, C6-C12 aryloxy, C3-C6 cycloalkyloxy, C3-C6 cycloalkylthio, amino, mono- or di- C1-C8 alkylamino, thio, C1-C4 alkylthio, C6-C12 arylthio, C7-C16 aralkylthio, or the radical -S-(CH2)nCH(NH2)COOH. These compounds have dehydropeptidase (DHP) enzyme inhibitor activity.

Inventors

• 👤 William H. Parsons
• 👤 William R. Schoen
• 👤 Arthur A. Patchett

Bibliographic Details