Usv Pharmaceutical Corporation

Rorer Pharmaceutical Corporation

Block Drug Company, Inc.

Edward S Neiss

John T Suh

John J Piwinski

Howard Jones

Paul R Menard

John R Regan

Jerry W Skiles

Jeffrey N Barton

David Stevenson

Laurence L Ho

Robert C Liu

Bernard Loev

Raymond D Youssefyeh

Larry M Allen

Rohit M Desai

James J Mencel

Paul Menard

New peptides are disclosed which have biological activity of the same type as known calcitonins and which are amide analogs of natural calcitonins.

Amide analogs of calcitonin

Compounds having the general structure ##STR1## and their pharmaceutically acceptable salts, wherein the substituents are defined herein, which exhibit antihypertensive activity.

Antihypertensive derivatives

Carboxyalkyl dipeptide compounds

Compounds of the formula ##STR1## and their pharmaceutically acceptable salts, wherein the substituents are as defined herein, having antihypertensive activity.

Benzothiadiazole compounds for treating hypertension

Compounds for treating hypertension

Novel compounds possessing both angiotensin enzyme inhibitory activity and diuretic activity are disclosed. The compounds are represented by the general formula ##STR1## in which X is ##STR2## in which R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are hydrogen, alkyl, alkenyl, alkynyl, phenyl-alkyl, and cycloalkyl, and may be the same or different; n is an integer from 0 to 4 inclusive; M is alkenyl, alkynyl, cycloalkyl, cycloalkyl-alkyl, polycycloalkyl, polycycloalkyl-alkyl, aryl, aralkyl, heteroaryl, heteroaryl-alkyl, hetero-cyloalkyl, hetero-cycloalkyl-alkyl, fused aryl-cycloalkyl, fused aryl-cycloalkyl-alkyl, fused heteroaryl-cycloalkyl, fused heteroaryl-cycloalkyl-alkyl, alkoxyalkyl, alkylthioalkyl, alkylamino-alkyl, or dialkylaminoalkyl, or M and R.sub.6 taken together with the nitrogen to which M is bonded and the carbon to which R.sub.6 is bonded form a saturated unsubstituted heterocyclic group containing 3 or 4 ring carbon atoms; Y is hydroxy, alkoxy, amino, or substituted amino, aminoalkanoyl, aryloxy, aminoalkoxy, or hydroxyalkoxy; Z.sub.1 and Z.sub.2 each is a chemical bond, the group X.sub.3 --(CH.sub.2).sub.m, an amino acid group or the group X.sub.3 --(CH.sub.2).sub.m --X.sub.3 wherein X.sub.3 is oxygen, sulfur or NH and m is an integer from 0 to 4 inclusive; A and B each is the same as R.sub.1 or halogen, trifluoromethyl, OR.sub.1, NO.sub.2, NR.sub.1 R.sub.2, SO.sub.2 NH.sub.2, CN, SR.sub.1, SOR.sub.1, SO.sub.2 R.sub.1, CONR.sub.1 R.sub.2, COOR.sub.1 ; C is hydrogen alkyl, heteroallyl, amino, --CR.sub.1 .dbd.CR.sub.2 --, ##STR3## aminoalkyl, furfurylmethylamino, aminoaryl or aminobenzyl; X.sub.1 and X.sub.2 are each S, SO, SO.sub.2, NR.sub.1, O, chemical bond, (CR.sub.9 R.sub.10).sub.m, --CR.sub.9 .dbd.CR.sub.10 --, and CHOH, with the proviso that at least one of X.sub.1 and X.sub.2 be (CR.sub.9 R.sub.10).sub.m, wherein R.sub.9 and R.sub.10 are each hydrogen or lower alkyl, and m is an integer from 1 to 5; Ar is a divalent arylene or heteroarylene; and R.sub.7 and R.sub.8 are each hydrogen, alkyl, halo, cyano, hydroxy, alkoxy, amino, alkylamino, dialkylamino, mercapto, alkylmercapto, nitro, trifluoromethyl, carboxy, carbalkoxy, COY and NHCONHR.sub.1 wherein R.sub.1 and Y are as hereindefined; and pharmaceutically-acceptable salts thereof.

Compounds having angiotensin converting enzyme inhibitory activity and

This invention relates to novel lipoxygenase inhibitors possessing anti-inflammatory and anti-allergic activities. The present new compounds are di- and tetra-hydroquinoline or di- and tetra-hydronapthalene derivatives, more particularly, 1,2-, 1,4-, 5,6-, or 7,8-dihydro; 1,2,3,4-tetrahydro-; 5,8-dihydro-; or 5,6,7,8-tetrahydroquinoline or napthalene derivatives of a compound of the formula: ##STR1## and oxides, quaternary ammonium salts and acid salts thereof; wherein A is CH or N;

1,2-Dihydro; 1,2,3,4-tetrahydro; 5,8 dihydro; and

A composition for the treatment of acne in the form of a solution, lotion or cream containing from about 1 to 10% by weight of a compound of the formula ##STR1## wherein R is an alkyl having up to 6 carbon atoms or aryl having up to 10 carbon atoms and R.sub.1 and R.sub.2 are independently hydrogen, lower alkyl having up to 6 carbon atoms, phenyl, phenyl-lower alkyl, lower alkylphenyl, halogen, halophenyl, trifluoromethyl, trifluoromethylphenyl, lower alkoxy, methylenedioxy, and lower alkoxyphenyl.

Compositions for treating acne

Growing community of inventors

New Canaan, CT, United States of America

Edward S Neiss