Chroman derivatives
AssigneeBeecham Group Limited
InventorEric Alfred Watts
Life of this patent
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Abstract
Anti-hypertensive derivatives of trans-3-hydroxy-4-amino-chroman, their preparation from amines and chroman epoxide derivatives, and pharmaceutical compositions containing such anti-hypertensive derivatives for reducing blood pressure in mammals including humans.
Claims55
A compound of the formula (I):
- ##STR11## or a pharmaceutically acceptable acid addition salt thereof wherein NR.sub.1 R.sub.2 is a 3- to 8-membered heterocycle wherein the nitrogen atom is the only heteroatom, unsubstituted or substituted by 1 or 2 methyl groups;
- R.sub.3 is hydrogen, halogen, alkyl of 1 to 6 carbon atoms, amino, alkylamino of 1 to 6 carbon atoms in the alkyl moiety, dialkylamino of 1 to 6 carbon atoms in each alkyl moiety, nitro, trifluoromethyl or lower alkanoylamino of 2 to 7 carbon atoms;
- R.sub.4 is hydrogen, halogen, methyl or methoxy;
- R.sub.5 is hydrogen, alkyl of 1 to 6 carbon atoms or phenyl;
- and
- R.sub.6 is hydrogen, alkyl of 1 to 6 carbon atoms or phenyl.
A pharmaceutical composition useful for treating hypertension in humans and animals which comprises an antihypertensively effective amount of a compound of the formula (I) ##STR15## or a pharmaceutically acceptable acid addition salt thereof wherein NR.sub.1 R.sub.2 is a 3- to 8-membered heterocycle wherein the nitrogen atom is the only heteroatom, unsubstituted or substituted by 1 or 2 methyl groups;
- R.sub.3 is hydrogen, halogen, alkyl of 1 to 6 carbon atoms, amino, alkylamino of 1 to 6 carbon atoms in the alkyl moiety, dialkylamino of 1 to 6 carbon atoms in each alkyl moiety, nitro, trifluoromethyl or lower alkanoylamino of 2 to 7 carbon atoms;
- R.sub.4 is hydrogen, halogen, methyl or methoxy;
- R.sub.5 is hydrogen, alkyl of 1 to 6 carbon atoms or phenyl;
- and
- R.sub.6 is hydrogen, alkyl of 1 to 6 carbon atoms or phenyl;
- in combination with a pharmaceutically acceptable carrier.
A method of treating hypertension in humans and animals which comprises administering to a human or animal in need thereof an antihypertensively effective amount of a compound of the formula (I) ##STR19## or a pharmaceutically acceptable acid addition salt thereof wherein NR.sub.1 R.sub.2 is a 3- to 8-membered heterocycle wherein the nitrogen atom is the only heteroatom, unsubstituted or substituted by 1 or 2 methyl groups;
- R.sub.3 is hydrogen, halogen, alkyl of 1 to 6 carbon atoms, amino, alkylamino of 1 to 6 carbon atoms in the alkyl moiety, dialkylamino of 1 to 6 carbon atoms in each alkyl moiety, nitro, trifluoromethyl or lower alkanoylamino of 2 to 7 carbon atoms;
- R.sub.4 is hydrogen, halogen, methyl or methoxy;
- R.sub.5 is hydrogen, alkyl of 1 to 6 carbon atoms or phenyl;
- and
- R.sub.6 is hydrogen, alkyl of 1 to 6 carbon atoms or phenyl;
- in combination with a pharmaceutically acceptable carrier.
Dependencies are inferred from the claim text.