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US 4,729,994 AGranted
Benzothiazepine vasodilators having aralkyl substitution
AssigneeMcNeilab, Inc.
InventorJohn R. Carson
Life of this patent
Estimating the term…
Abstract
N-Aminoalkyl 1,5-benzothiazepines of the following formula (I): ##STR1## for the treatment of angina or hypertension or the prevention of heart attacks in mammals, in particular their use as coronary vasodilators.
Claims18
A benzothiazepine of the following formula (I):
- ##STR7## wherein X is a hydrogen atom or a halogen atom;
- R.sup.1 is a phenyl ring which is unsubstituted or independently substituted by 1 to 3 of lower alkyl, lower alkoxy or halogen;
- R.sup.2 is a hydrogen atom or a lower alkanoyl group;
- Y is a straight chain alkylene group of about 2 or 3 carbons;
- R.sup.3 is lower alkyl;
- R.sup.4 is independently lower alkyl;
- p is the integer 0, 1, 2 or 3;
- Alk is a straight chain alkylene of about 2 to 4 carbons;
- R.sup.5 is independently hydroxy, alkyl or phenyl;
- q is 0, 1 or 2 or 3 if Alk is alkylene of about 2 to 4 carbons;
- and
- Ar is a phenyl, phenoxy, thiophenoxy, naphthyl or a 5- or 6-membered heterocyclic aromatic ring which rings may be substituted independently by one or more of alkyl, alkoxy, alkylthio, hydroxy, halogen, fluoroalkyl, nitro, amino or dialkylamino or by methylenedioxy at adjacent ring carbon, and the pharmaceutically acceptable acid addition salts and quaternary ammonium compounds thereof.
9 more elements
The compound of the following formula (VI):
- ##STR8## or a pharmaceutically acceptable acid addition salt thereof.
The compound of the following formula (VII):
- ##STR9## or a pharmaceutically acceptable acid addition salt thereof.
Dependencies are inferred from the claim text.