Merck + Co., Inc.

Jason M Elliott

John J Baldwin

David A Claremon

Harold G Selnick

David C Remy

Gerald S Ponticello

Nigel J Liverton

Nitrogen-containing spirocycles

Benzodiazepines

Spirocycles of general structural formula: ##STR1## are Class III antiarrhythmic agents.

Benzo-(1,5)-diazepine derivatives with an amide or urea function in the 3-position are useful in the treatment of arrhythmia. The compounds have structural formulae: ##STR1##

Antiarrhythmic benzodiazepines

Benzodiazepine derivatives with an amide or urea function in the 3-position are useful in the treatment of arrhythmia. The compounds have structural formulae: ##STR1##

3-Acylamino-5-Aminobenzo[1,5]diazepines are useful in the treatment of arrhythmia. The compounds have structural formulae: ##STR1##

3-acylaminobenzodiazepines

Spirocycles of the general structural formulae: ##STR1## wherein: X is O, CH.sub.2 or SO.sub.m ; R.sup.1 is AlkylSO.sub.2 NH--, AlkylO--, AlkylSO.sub.2 --, AlkylCONH--, or NO.sub.2 --; R.sup.2 is --H, --OAlkyl, or --Alkyl; R.sup.3 is --NHCOCH.sub.2 SO.sub.m Phenyl, --NHCOCH.sub.2 SO.sub.m Alkyl, --NHCOC(CH.sub.3).sub.2 OH, or NHSO.sub.2 Alkyl; R.sup.4 and R.sup.5 are --H, or --Alkyl; R.sup.6 is ##STR2## R.sup.7 is --H, --CN, --NHSO.sub.2 Alkyl, --Br, --OAlkyl, --NH.sub.2, --NO.sub.2, --NHCOAlkyl, or NHCONHAlkyl; R.sub.8 is --H, --OH, --CN, --OAlkyl, --CONHAlkyl, --NHSO.sub.2 Alkyl, --NHCOAlkyl, --SO.sub.m Alkyl, or --CO.sub.2 Alkyl; and m is 0-2; or a pharmaceutically acceptable salt, hydrate or crystal form thereof; which are Class III antiarrhythmic agents.

Spirocycles

Compounds of structural formula: ##STR1## wherein Ar is an aromatic ring, B is a cyclic moiety fused to Ar of 5-7 members, X and Y are bridging groups, Q is a nitrogen containing heterocycle, R.sup.2 and R.sup.3 are H, substituted or unsubtituted C.sub.1-3 alkyl, C.sub.1-3 alkoxy, N(R).sub.2, halogen, CF.sub.3 or R.sup.5 and R.sup.1 is H or an aryl group.

Nitrogen-containing heterocyclic compounds as class III antiarrhythmic

Compounds of structural formula: ##STR1## wherein R' is hydrogen or an aromatic ring system, and Q is a substituted nitrogen or a nitrogen containing heterocycle, X and Y are bridging groups and p is 0 or 1, and E is --S-- or --O--, are Class III antiarrhythmic agents.

Benzofuran compounds as class III antiarrhythmic agents

Compounds of structural formula: ##STR1## wherein R' is hydrogen or an aromatic ring system, and Q is a substituted nitrogen or a nitrogen containing heterocycle, and E is --S-- or --O--, are Class III antiarrhythmic agents.

Class III antiarrhythmic agents

Compounds of structural formula: ##STR1## wherein Ar is an aromatic ring, B is a cyclic moiety fused to Ar of 5-7 members and Q is a nitrogen containing heterocycle, are antiarrhythmic agents.

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Jason M Elliott