Indazolanonyl derivatives of benzopyrans

Details Indazolanonyl derivatives of benzopyrans Indazolanonyl derivatives of benzopyrans

1992-05-08

1993-01-12

Ramsuer, Robert W.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

5483615, A61K 31415, A61K23156

Patent

active

051791188

ABSTRACT:
The compounds of the formula: ##STR1## wherein R.sub.1 is 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 alkylsulfonamindo, 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, or C.sub.2-12 mono- or di-alkylcarbamoyl; R.sub.2 is hydrogen, 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.1-12 arylsulfonyl, carboxyl, or C.sub.2-12 mono- or di-alkylcarboamoyl; R.sub.3 and R.sub.4, independent from each other, are C.sub.1-6 alkyl; 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 R.sub.6 together are a bond; R.sub.7 and R.sub.8, 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.1-6 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; and R.sub.9 is hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkylcarbonyl or C.sub.2-6 alkylsulfonyl; or a pharmaceutically acceptable salt thereof are useful as smooth muscle relaxants, as antihypertensives and K channel activators.

REFERENCES:
patent: 4616021 (1986-10-01), Ashwood et al.
patent: 4908378 (1990-03-01), Soll et al.
patent: 4925839 (1990-05-01), Quagliato et al.
patent: 4983612 (1991-01-01), Quagliato et al.
Longman et al., Medicinal Research Reviews, 1992, 12, 73.
Robertson, et al., J. Med. Chem., 1990, 33, 1529.
Weston, et al., TiPS, 1990, 11, 417.
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