American Home Products Corporation

William H McGregor

Joseph Y Chang

John H Musser

Victor M Garsky

Lisa A Marshall

Larry Stein

Joseph J Dougherty

Surendra K Dheer

James D Beluzzi

There are disclosed compounds of the formula ##STR1## R is --CH.sub.2 OH or --CO.sub.2 R.sup.3 ; R.sup.1 is hydrogen, lower alkyl, lower alkoxy or hydroxybenzyl;

Hydroxy containing amines as phospholipase A2 inhibitors

There are disclosed compounds of the formula

Phospholipase A2 inhibitors

There are disclosed compounds of the formula ##STR1## wherein R.sup.1 is lower alkyl, lower alkoxycarbonyl lower alkyl, aralkoxycarbonyl, aralkoxycarbonyl lower alkyl or indol-2-yllower alkyl;

Phospholipase A.sub.2 inhibitors

2-[1,3,2-dioxaphospholan-2-yloxy]ethyl compounds

The polypeptides R-Gly-L-Cys-Gly-L-Glu-L-Glu-NH.sub.2 or a pharmaceutically acceptable salt thereof act as collagenase inhibitors useful in the treatment of disease involving excessive tissue destruction by collagenase.

Mammalian collagenase inhibitors

The polypeptides ##STR1## in which R is hydrogen, alkanoyl of 2 to 6 carbon atoms, cycloalkylcarbonyl of 2 to 6 carbon atoms or a pharmaceutically acceptable salt thereof act as collagenase inhibitors useful in the treatment of diseases involving excessive tissue destruction by collagenase.

There are disclosed polypeptides having the formula:

Polypeptide compositions

Bestatin and its analogues are compounds capable of inducing analgesia in mammals when administered peripherally.

Method of inducing analgesia

There are disclosed tetrapeptides having the formula:

Novel dipeptides of the formula: A--X--Y--B wherein X is D-Tyr or L-Tyr; Y is D-Ala, L-Ala, D-Ser, L-Ser, or Gly; with the proviso that at least one of X and Y is of the D- configuration; A is hydrogen, allyl, or lower alkyl of 1 to 3 carbon atoms; B is --NH.sub.2, --OMe, or --NHNH.sub.2 ; and the pharmacologically acceptable salts thereof, as well as pharmaceutical compositions containing them, and a process for antagonizing the effects of a narcotic analgesic agent in warm blooded animals are disclosed.

Dipeptide narcotic antagonists

The polypeptides of the formula: ##STR1## in which R is hydrogen, methyl, allyl or cyclopropylmethyl; and

Analgesic polypeptide

The growth hormone release inhibiting undecapeptide of the formula

[Des-Ala.sup.1, Gly.sup.2 -desamino-Cys.sup.3 ]somatostatin

High speed liquid chromatography of synthetically produced somatostatin yields somatostatin free from structural artifacts.

Growing community of inventors

Malvern, PA, United States of America

William H McGregor