American Home Products Corporation

Biomega, Inc.

Bio-mega/boehringer Ingelheim Research Inc.

Ayerst, Mckenna & Harrison, Inc.

Sumanas Rakhit

Jehan F Bagli

Pierre Lavallee

Raymond Plante

Gregory P Cosentino

Mahesh H Goghari

Yvan Guindon

Pierre Louis Beaulieu

Julian Adams

Disclosed herein are pentapeptide derivatives of the formula (SEQ ID NO: 24) XNR.sup.1 --CH(R.sup.2)--C(O)--NH--CH(R.sup.3 --C(O)--NR.sup.4 --CH(CH.sub.2 Y)--CO--NH--CH[CR.sup.5 (R.sup.6)--COOH]--C(W)--NH--CH(R.sup.7)--Z wherein X is a terminal group, for example, alkanoyl or phenylalkanoyl radicals, R.sup.1 is alkyl or phenylalkyl, R.sup.2, R.sup.3 and R.sup.7 are selected from the side chains of amino acid or derived amino acid residues, R.sup.4, R.sup.5, and R.sup.6 are hydrogen or lower alkyl, W is oxo or thioxo, Y is carboxy, carbamyl or 5-1H-tetrazolyl and Z is carboxy or 5-1H-tetrazolyl. The derivatives are useful for treating herpes infections.

Antiherpes pentapeptides

Disclosed herein are derivatives of atrial natriuretic peptides which are characterized by having (at positions 106 and/or 124) a phenylalanyl residue bearing a fluoro or trifluoromethyl substituent on the aromatic portion thereof. Optionally, the exocyclic N-terminal peptide segment and the first cystienyl residue (at position 105) are replaced by an optionally substituted thioalkanoyl residue. The derivatives possess useful diuretic, natriuretic and antihypertensive activities.

Fluorine containing atrial natriuretic peptides

Disclosed herein are peptides of the formula

Inhibitors of bacterial ribonucleotide reductase

Disclosed herein are derivatives of atrial natriuretic peptides which are characterized by having (at position 124 or at positions 106 and 124) a phenylalanyl residue bearing a fluoro or trifluoromethyl substituent on the aromatic portion thereof. Optionally, the exocyclic N-terminal peptide segment and the first cystienyl residue (at position 105) are replaced by an optionally substituted thioalkanoyl residue. The derivatives possess useful diuretic, natriuretic and antihypertensive activities.

Ribonucleotide reductase inhibitors

Herein is disclosed 2-(1-piperazinyl)-4-pyrimidinamine derivatives, acid addition salts thereof, processes for their preparation, methods of using the derivatives and pharmaceutical compositions of the derivatives. The derivatives are distinguished most readily by having novel substituents at position 4 of the piperazinyl radical, the substituents being selected from the group consisting of 2-thiazoylyl, oxazolo(4,5-b)pyridin-2-yl and optionally substituted 1-(lower alkyl)-1H-benzimidazol-2-yl. The derivatives are useful for treating hypertension in a mammal.

2-(Piperazinyl)-4-pyrimidinamines

Herein is disclosed 2-(1-piperazinyl)-4-pyrimidinamine derivatives, acid addition salts thereof, processes for their preparation, methods of using the derivatives and pharmaceutical compositions of the derivatives. The derivatives are distinguished most readily by having novel substituents at position 4 of the piperazinyl radical, the substituents being selected from the group consisting of optionally substituted 2-cycloheptimidazolyl, 1,4,5,6,7,8-hexahydrocycloheptimidazol-2-yl, 2-benzoxazolyl, benzthiazol-2-yl, 1H-2-benzimidazolyl and 1-oxo-2,4,6-cycloheptarien-2-yl. The derivatives are useful for treating hypertension in a mammal.

2-(Piperazinyl)-4-pyrimioinamines

Disclosed are monoacyl and diacyl derivatives of rapamycin, processes for their preparation, methods of using the derivatives and pharmaceutical compositions of the derivatives. The derivatives are useful, inter alia, as antifungal antibiotics.

Acyl derivatives of rapamycin

Lactone esters of formula ##STR1## in which X is chloro, bromo or lower alkyl and Y is ##STR2## are disclosed. The lactone esters possess antihyperlipoproteinemic activity. Methods for the preparation and use, as well as pharmaceutical compositions of the lactone esters, also are disclosed.

Lactone esters of phenoxyisobutyric acids

Glycosyl esters of formula ##STR1## in which X is chloro, bromo, or lower alkyl and Y is tetra-(lower alkanoyl) or tetrabenzoyl .beta.-D-glucosyl or tri(lower alkanoyl) or tribenzoyl .beta.-D-ribosyl are disclosed. These esters possess antihyperlipoproteinemic activity. Methods for preparation and use, as well as pharmaceutical compositions of the glycosyl esters, also are disclosed.

Growing community of inventors

Dollard des Ormeaux, Canada

Sumanas Rakhit