Thiadiazolyl-amino derivatives of benzopyrans and indanes

A pharmaceutical composition comprising a sufficient amount of a compound to activate potassium channels in a mammal in need thereof and a pharmaceutically acceptable carrier, wherein said compound is of the formula:

• ##STR8## wherein:
• R.sub.1 and R.sub.2, independent from each other, are selected from the following:
• C.sub.1-6 perfluoroalkoxy, C.sub.1-6 perfluoroalkyl, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, hydroxyl, C.sub.2-6 alkoxycarbonyl, nitro, cyano, halogeno, C.sub.1-6 alkylsulfonamido, C.sub.1-6 perfluoroalkylsulfonamido, amino, C.sub.2-6 alkanoylamino, C.sub.2-6 perfluoroalkanoylamino, C.sub.1-12 mono- or di-alkylamino, C.sub.1-6 alkylsulfonyl, C.sub.6-12 arylsulfonyl, carboxyl, C.sub.2-12 mono- or di-alkylcarbamoyl, or hydrogen;
• a and b together form an --O-- linkage or a direct bond;
• R.sub.3 and R.sub.4, independent from each other, are C.sub.1-6 alkyl when a and b form an --O-- linkage or, H or C.sub.1-6 alkyl when a and b form a direct bond;
• either R.sub.5 is hydrogen, hydroxyl, C.sub.2-6 alkanoyloxy, C.sub.7-12 aroyloxy, carbamoyloxy, formyloxy, C.sub.2-6 alkoxycarbonyloxy, mono or di C.sub.2-12 alkylcarbamoyloxy, and R.sub.6 is hydrogen, or R.sub.5 and R.sub.6 together are a bond;
• R.sub.7 is hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkanocarbonyl, or C.sub.1-6 alkanosulfonyl;
• X is selected from the following:
• --NR.sub.8 R.sub.9, wherein R.sub.8 and R.sub.9, independent from each other are hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkylcarbonyl, C.sub.7-12 arylalkyl, thienylmethyl, pyridinylmethyl, piperazinylmethyl, or pyrimidinylmethyl, or R.sub.8 and R.sub.9 taken together are polymethylene of 3-10 carbon atoms or R.sub.8 and R.sub.9 taken with the nitrogen atom to which they are attached complete a piperazine, morpholine, pyrrolidine, pyrrolidinone, imidazole, imidazolone, piperidine or piperidinone ring structure;
• or --OR.sub.10, wherein R.sub.10 is hydrogen, C.sub.1-6 alkyl or C.sub.2-6 alkylcarbonyl;
• and n is an integer from 0-2;
• or a pharmaceutically acceptable salt thereof.

A pharmaceutical composition comprising an antihypertensive amount of a compound of the formula:

• ##STR9## wherein:
• R.sub.1 and R.sub.2, independent from each other, are selected from the following:
• C.sub.1-6 perfluoroalkoxy, C.sub.1-6 perfluoroalkyl, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, hydroxyl, C.sub.2-6 alkoxycarbonyl, nitro, cyano, halogeno, C.sub.1-6 alkylsulfonamido, C.sub.1-6 perfluoroalkylsulfonamido, amino, C.sub.2-6 alkanoylamino, C.sub.2-6 perfluoroalkanoylamino, C.sub.1-12 mono- or di-alkylamino, C.sub.1-6 alkylsulfonyl, C.sub.6-12 arylsulfonyl, carboxyl, C.sub.2-12 mono- or di-alkylcarbamoyl, or hydrogen;
• a and b together form an --O-- linkage or a direct bond;
• R.sub.3 and R.sub.4, independent from each other, are C.sub.1-6 alkyl when a and b form an --O-- linkage or, H or C.sub.1-6 alkyl when a and b form a direct bond;
• either R.sub.5 is hydrogen, hydroxyl, C.sub.2-6 alkanoyloxy, C.sub.7-12 aroyloxy, carbamoyloxy, formyloxy, C.sub.2-6 alkoxycarbonyloxy, mono or di C.sub.2-12 alkylcarbamoyloxy, and R.sub.6 is hydrogen, or R.sub.5 and R.sub.6 together are a bond;
• R.sub.7 is hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkanocarbonyl, or C.sub.1-6 alkanosulfonyl;
• X is selected from the following:
• --NR.sub.8 R.sub.9, wherein R.sub.8 and R.sub.9, independent from each other are hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkylcarbonyl, C.sub.7-12 arylalkyl, thienylmethyl, pyridinylmethyl, piperazinylmethyl, or pyrimidinylmethyl, or R.sub.8 and R.sub.9 taken together are polymethylene of 3-10 carbon atoms or R.sub.8 and R.sub.9 taken with the nitrogen atom to which they are attached complete a piperazine, morpholine, pyrrolidine, pyrrolidinone, imidazole, imidazolone, piperidine or piperidinone ring structure;
• or --OR.sub.10, wherein R.sub.10 is hydrogen, C.sub.1-6 alkyl or C.sub.2-6 alkylcarbonyl;
• and n is an integer from 0-2;
• or a pharmaceutically acceptable carrier thereof.