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US 4,072,683 AGranted
3,4-Dihydrocarbostyril derivatives
AssigneeOtsuka Pharmaceutical Co., Ltd.
InventorsKazuyuki Nakagawa, Minoru Uchida, Hiroaki Oka
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AssigneeOtsuka Pharmaceutical Co., Ltd.
InventorsKazuyuki Nakagawa, Minoru Uchida, Hiroaki Oka
Estimating the term…
Novel (3'-alkylamino-2'-hydroxy)propoxy-3,4-dihydrocarbostyril derivatives having .beta.-adrenergic nerves blocking activity and hypotensive activity and useful as a remedy for angina pectoris, irregular pulse and hypertension, etc., represented by the formula, ##STR1## wherein R.sub.1 is hydrogen, C.sub.1 -C.sub.4 alkyl or aralkyl and R.sub.2 is C.sub.1 -C.sub.4 alkyl, are prepared by reacting a 3,4-dihydrocarbostyril derivative represented by the formula, ##STR2## wherein R.sub.1 is C.sub.1 -C.sub.4 alkyl or aralkyl, with an epihalogenohydrin represented by the formula, ##STR3## wherein X is halogen, reacting the resulting product with an alkylamine represented by the formula, R.sub.2 -- NH.sub.2 wherein R.sub.2 is as defined above, and, if necessary, reducing the resulting product.
A compound of the formula, ##STR21## wherein R.sub.1 is hydrogen, C.sub.1 -C.sub.4 alkyl, benzyl or phenethyl and R.sub.2 is C.sub.1 -C.sub.4 alkyl or a pharmaceutically acceptable acid addition salt thereof.
5-(3'-tert-Butylamino-2'- hydroxy)propoxy-8-hydroxy-3,4-dihydrocarbostyril or a pharmaceutically acceptable acid addition salt thereof.
5-(3'-Isopropylamino-2'-hydroxy)propoxy-8-hydroxy-3,4-dihydrocarbostyril or a pharmaceutically acceptable acid addition salt thereof.
5-(3'-sec-Butylamino-2'-hydroxy)propoxy-8-hydroxy-3,4-dihydrocarbostyril or a pharmaceutically acceptable salt thereof.
5-(3'-tert-Butylamino-2'-hydroxy)propoxy-8-m ethoxy-3,4-dihydrocarbostyril or a pharmaceutically acceptable acid addition salt thereof.
5-(3'-tert-Butylamin o-2'-hydroxy)propoxy-8-benzyloxy-3,4-dihydrocarbostyril or a pharmaceutically acceptable acid addition salt thereof.
5-(3'-Isopropylamino-2'-hydroxy)propoxy-8-benzyloxy-3 ,4-dihydrocarbostyril or a pharmaceutically acceptable acid addition salt thereof.
5-(3'- sec-Butylamino-2'-hydroxy)propoxy-8-benzyloxy-3,4-dihydrocarbostyril or a pharmaceutically acceptable acid addition salt thereof.
Dependencies are inferred from the claim text.