Pfizer Corporation

Conopco, Inc.

Phytopharm Plc

Jasjit S Bindra

Thomas K Schaaf

Michael Ross Johnson

Hans-Jurgen E Hess

James F Eggler

Elias James Corey

Robert L Rosati

Edward F Kleinman

Praful K Shah

Ian Duncan Rubin

Michael Anthony Cawthorne

Saul B Kadin

The invention relates inter alia to pharmaceutical compositions containing an extract obtainable from a plant of the genusorhaving anti-diabetic activity; and to the use of such extracts and to compound (1) as herein defined and its analogues for the manufacture of medicaments having anti-diabetic activity.

Extracts, compounds and pharmaceutical compositions having anti-diabetic activity and their use

A series of novel polypeptide derivatives, containing 5-amino-2,5-disubstituted-4-hydroxypentanoic acid residues, which are useful for inhibiting the angiotensinogen-cleaving action of the enzyme renin. Particularly valuable precursors for many of these compounds are certain other 5-amino-2,5-disubstituted-4-hydroxypentanoic acid derivatives.

Renin inhibitors containing 5-amino-2,5-disubstituted-4-hydroxypentanoic

11-Desoxy-16-aryloxy-.omega.-tetranorprostaglandins are disclosed. The novel prostaglandins of this invention have been found to have activity profiles comparable to the parent prostaglandins but they exhibit a greater tissue specificity of action.

11-Desoxy-16-aryloxy-.omega.-tetranorprostaglandins

2,4-Diaminoquinazolines of the formula ##STR1## wherein Y.sup.1 is hydrogen or chloro, Y.sup.2 is OR, Y.sup.3 is hydrogen or OR such than when Y.sup.1 is hydrogen, Y.sup.3 is OR and when Y.sup.1 is chloro, Y.sup.3 is hydrogen or OR, and the pharmaceutically acceptable salts thereof; R represents an alkyl group having from one to three carbon atoms;

Chloro- and alkoxy-substituted-2,4-diaminoquinazolines

2,4-Diaminoquinazolines of the formula ##STR1## wherein Y.sup.1 is hydrogen or chloro, Y.sup.2 is OR, Y.sup.3 is hydrogen or OR such that when Y.sup.1 is hydrogen, Y.sup.3 is OR and when Y.sup.1 is chloro, Y.sup.3 is hydrogen or OR, and the pharmaceutically acceptable salts thereof; R represents an alkyl group having from one to three carbon atoms;

Chloro- and alkoxy-substituted-2-chloro-4-aminodquinazolines

Chiral 2-(2-benzyl-3-mercaptopropionylamino)-1-alkanol derivatives and chiral 2-(2-benzyl-3-mercaptopropionylamino)-4-methylthiobutyric acids are inhibitors of enkephalinase enzyme, reflecting their clinical utility as analgesics or anticonvulsant agents, or as therapy for disorders in which endogenous enkephalin levels are below normal.

Enkephalinase enzyme inhibiting compounds

Alkoxy-substituted-6-chloro-quinazoline-2,4-diones

Certain novel 2-[1-hydroxycyclopent-2-yl]acetic acid .gamma.-lactone derivatives are useful as intermediates for the synthesis of naturally-occurring prostaglandins and their analogues.

Prostaglandin intermediates

Substituted novel .omega.-pentanorprostaglandins and various novel intermediates and reagents used in their preparation.

Substituted .omega.-pentanorprostaglandins

The 15 aryl substituted-.omega.-pentanorprostaglandins and various intermediates empolyed in their preparation. The novel prostaglandins of this invention have been found to have activity profiles comparable to the parent prostaglandins, but exhibit a greater tissue specificity of action.

15-Substituted-omega-pentanorprostaglandins

9-Hydroxydibenzo[b,d]pyrans useful as analgesics, hypotensives, immunosuppressants, tranquilizers; as anti-secretory and anti-anxiety drugs; intermediates therefor and derivatives thereof having the formulae ##STR1## wherein R is hydrogen or alkanoyl having from one to five carbon atoms;

Growing community of inventors

Groton, CT, United States of America

Jasjit S Bindra