Patent · US Expired

Phenylethanolamino- and phenylethanolaminomethyl-tetralines, process for the preparation thereof, intermediates in said process and pharmaceutical compositions containing them

US5449813A · kind A · utility

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2References
6Claims
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Assignee

Inventors

Key dates

Filing dateDec 19, 1994
Grant dateSep 12, 1995
Priority date
Expiry dateDec 19, 2014

Classification

  • Technology area (CPC C)Chemistry; Metallurgy
  • CPC primaryC07C2602/10
  • WIPO fieldOrganic fine chemistry
  • WIPO sectorChemistry

Abstract

Phenylethanolamino- and phenylethanolaminomethyltetralines of formula (I) ##STR1## wherein X represents a hydrogen atom, a halogen atom,a (C.sub.1 -C.sub.4)alkyl group or a trifluoromethyl group, PA1 A represents a bond between the --COOR group and the tetraline ring, a (C.sub.1 -C.sub.4)alkylene or a (C.sub.2 -C.sub.4)alkenylene group, PA1 R is hydrogen or a (C.sub.1 -C.sub.4)alkyl group, and PA1 n is 0 or 1 PA1 and their salts, are typically prepared by reaction of an epoxide of formula (IIa) ##STR2## with a tetraline derivative of formula (III) ##STR3## wherein A and n are as defined above and R' is a (C.sub.1 -C.sub.4)alkyl group, optionally followed by basic hydrolysis to obtain the compounds (I) wherein R is hydrogen. The new compounds show very interesting properties as antidepressant and intestinal spasmolytic agents. The new intermediates of formula (III) are also claimed.

Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.