E. R. Squibb Sons, Inc.

Bristol-myers Squibb Compnay

Other

George C Rovnyak

Karnail S Atwal

Spencer David Kimball

John Krapcho

Norma G Delaney

Melanie J Loots

Chester F Turk

Jagabandhu Das

Saleem Ahmad

Michael A Poss

B Richard Vogt

John E Lloyd

Rudiger D Haugwitz

Joel C Barrish

Philip D Stein

David M Floyd

Venkatachala L Narayanan

Charles Z Ding

John T Hunt

Dinos P Santafianos

Thomas J Caulfield

Benzoic acid derivatives and related compounds as antiarrhythmic agents

Compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof wherein X is alkyl, Y is a single bond, --CH.sub.2 --, --C(O)--, --O--, --S-- or --N(R.sup.8)-- where R.sup.8 is hydrogen, alkyl, haloalkyl, aryl, arylalkyl, cycloalkyl or (cycloalkyl)alkyl, and R.sup.1 to R.sup.7 are as defined herein. These compounds have potassium channel activating activity and are useful, therefore for example, as cardiovascular agents.

4-arylamino-benzopyran and related compounds

Compounds of the formula ##STR1## wherein Z is ##STR2## proline, pipecolic acid, an indolecarboxylic acid or an isoquinolinecarboxylic acid. These compounds are useful as cardiovascular agents.

Trifluoromethyl mercaptan and mercaptoacyl derivatives and method of

Compounds of the formula ##STR1## wherein m is zero or 1; n is zero, 1 or 2; p is zero or 1 to 6 provided that m and p are not both zero; R.sub.3 is hydrogen, acyl, or benzyl; and R.sub.1 is hydrogen, alkyl, phenyl, substituted phenyl, phenyl-alkylene, heterocyclic-alkylene, etc. These compounds are useful as cardiovascular agents.

Novel compounds useful, for example, in the treatment of ischemic conditions and arrhythmia having the formula I ##STR1## wherein X is oxygen, sulfur or --NCN and the R groups are as defined herein.

Aryl urea (thiourea) and cyanoguanidine derivatives

Novel compounds are disclosed having the formula ##STR1## wherein X, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7 and R.sub.8 are as defined herein.

Chromanyl substituted indole potassium channel openers

Compounds of the formula ##STR1## wherein Y can be tetrazolyl are disclosed. These compounds are useful as cardiovascular agents.

3,3,3-trifluoro-2-mercaptomethyl-N-tetrazolyl substituted propanamides

Pyrimidine compounds of the formula ##STR1## wherein X is sulfur or oxygen, Y is R.sub.11 or --O--R.sub.1, and R.sub.4 is aryl or heterocyclo are disclosed. These compounds are useful as cardiovascular agents, particularly anti-hypertensive agents, due to their calcium entry blocking vasodilator activity.

2-thio or oxo-4-aryl or heterocyclo-1,5(2H)-pyrimidinedicarboxylic acid

A compound of the formula ##STR1## (symbols defined in the specification), its 3,4-dihydropyrimidine tautomer form and pharmaceutically acceptable salts thereof have calcium entry blocking activity. A process of preparation, pharmaceutical composition and method of using the compound to reduce blood pressure are also provided.

Dihydropyrimidine macrocyclic lactones useful as calcium antagonists and

Novel compounds of the formula ##STR1## wherein X is sulfur or oxygen, R.sub.2 is aryl or heterocyclo and R.sub.1 is as defined herein, are disclosed. Compounds of formula I possess calcium channel activating activity.

Dihydropyrimidine lactone derivatives

Vasodilating activity is exhibited by compounds having the formula ##STR1## wherein X can be --S--or --CH.sub.2 --; and

Benzazepine and benzothiazepine derivatives

Cardiovascular activity is exhibited by compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof wherein X is oxygen or sulfur;

1,2,3,4-Tetrahydro-6-substituted-4-aryl(or heterocyclo)-3-((substituted

Pyridine compounds of the formula ##STR1## wherein R.sub.4 is aryl or heterocyclo are disclosed. These compounds are useful as cardiovascular agents due to their calcium entry blocking vasodilator activity.

Pyrimidinecarboxylic acid derivatives

Angiotensin converted enzyme inhibitor activity if exhibited by compounds having the formula ##STR1## and salts thereof wherein R.sub.1 is hydrogen, aryl, or heteroaryl; R.sub.2 is hydrogen, amino, alkanoylamino, arylcarbonylamino, or heteroarylcarbonylamino;

Dioxolenylmethyl ester prodrugs of phosphinic acid ace inhibitors

Bis-amidine indene ketones are provided having the structure ##STR1## wherein R is hydrogen, lower alkyl or aryl; and R.sup.1 is hydrogen, lower alkyl, halogen, carboxy, trifluoromethyl, lower alkoxy, hydroxy or acyl, and acid-addition salts thereof. In addition, pharmaceutical compositions containing the above compounds and a method of using same to treat inflammatory conditions in mammalian species are also provided.

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Hopewell, NJ, United States of America

George C Rovnyak