Phosphorous containing dhp enzyme inhibitors

Details Phosphorous containing dhp enzyme inhibitors Phosphorous containing dhp enzyme inhibitors

1991-01-09

1992-09-08

Evans, Joseph E.

Organic compounds -- part of the class 532-570 series

Organic compounds

Phosphorus acids or salts thereof

514 79, 514 80, 514 82, 514 89, 514 94, 514 95, 514 96, 514 99, 514100, 514114, 546 22, 546 23, 548112, 548113, 549 5, 549 6, 549218, 549220, C07F 930, A61K 3113, A61K 31185, A61K 3166

Patent

active

051459906

ABSTRACT:
Compounds of the formula: ##STR1## wherein R.sub.1 is C.sub.2- C.sub.12 linear or branched unsubstituted alkyl; C.sub.1- C.sub.12 linear or branched substituted alkyl; C.sub.2 -C.sub.12 linear or branched monoalkenyl; C.sub.2 -C.sub.12 linear or branched alkynyl; C.sub.7 -C.sub.20 aralkyl, wherein the alkyl chain is linear or branched C.sub.1- C.sub.8 and the aryl moiety is C.sub.6- C.sub.12 ; C.sub.4- C.sub.10 cycloalkylalkyl; C.sub.3- C.sub.7 cycloalkyl; wherein these values for R.sub.1, other than C.sub.2- C.sub.12 linear or branched unsubstituted alkyl, can be substituted by one or more of C.sub.1 -C.sub.4 alkoxy, C.sub.3- C.sub.6 cycloalkyloxy, C.sub.3- C.sub.6 cycloalkylthio, C.sub.6- C.sub.12 aryloxy, C.sub.1- C.sub.4 alkylthio, C.sub.6- C.sub.12 arylthio, C.sub.7- C.sub.10 aralkyloxy, C.sub.7- C.sub.16 aralkyl-thio; and R.sub.5 is H or C.sub.1- C.sub.12 linear or branched alkyl; C.sub.2- C.sub.12 linear or branched monoalkenyl; C.sub.7- C.sub.20 aralkyl, wherein the alkyl chain is linear or branched C.sub.1- C.sub.8 and the aryl moiety is C.sub.6- C.sub.12 ; heterocyclic alkyl wherein the alkyl chain is linear or branched C.sub.1- C.sub.8 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; C.sub.4- C.sub.10 cycloalkylalkyl; C.sub.3- C.sub.7 cycloalkyl; wherein the values for R.sub.5 can be substituted by one or more of halo, hydroxy, carboxy, C.sub.1- C.sub.4 alkoxycarbonyl, C.sub.7- C.sub.16 arylalkoxycarbonyl, C.sub.3- C.sub.7 cycloalkyl, C.sub.1- C.sub.4 alkoxy, C.sub.6- C.sub.12 aryloxy, C.sub.3- C.sub.6 cycloalkyloxy, C.sub.3- C.sub.6 cycloalkylthio, amino, mono- or di- C.sub.1- C.sub.8 alkylamino, thio, C.sub.1- C.sub.4 alkylthio, C.sub.6- C.sub.12 arylthio, C.sub.7- C.sub.16 aralkylthio, or the radical --S--(CH.sub.2).sub.n CH(NH.sub.2)COOH. These compounds have dehydropeptidase (DHP) enzyme inhibitor activity.

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