Fujisawa Pharmaceutical Company, Ltd.

Teiji Kishimoto

Hiromu Kochi

Yoshiyuki Kaneda

Masayuki Kato

Ikuo Ueda

1,2,3,4-Tetrahydroisoquinolines having the formula: ##STR1## wherein R.sub.1 and R.sub.2 are each hydrogen, lower alkyl, lower alkenyl, acyl, aryl or ar(lower)alkyl, in which aryl and the aryl moiety of the ar(lower)alkyl may contain at least one substituent selected from the group consisting of halogen, lower alkoxy, amino, nitro, hydroxy, acyloxy, ar(lower)alkoxy, lower alkylenedioxy, halo(lower)alkyl, acylamino, ar(lower)alkylamino and aryl, and pharmaceutically acceptable salts thereof, having a relaxant activity on smooth muscles.

1,2,3,4-Tetrahydroisoquinolines 6.10,7,8 dihydroxy

A 1,2,3,4-tetrahydroisoquinoline having smooth muscle relaxant activity of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are each hydrogen or lower alkyl, R.sub.3 is phenyl having substituents selected from the group consisting of lower alkenyloxy, mercapto, lower alkylthio, sulfamoyl and mono or disubstituted sulfamoyl, or a heterocyclic group, R.sub.4 and R.sub.5 are each hydroxy or protected hydroxy and X is --O-- or--S--.

1,2,3,4-Tetrahydroisoquinoline derivatives and the preparation thereof

A 1,2,3,4-tetrahydroisoquinoline having smooth muscle relaxant activity of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are each hydrogen or lower alkyl and X is --O-- or --S--, and pharmaceutically acceptable salts thereof.

1,2,3,4-tetrahydroisoquinolines have the formula: ##STR1## wherein R.sub.1 and R.sub.2 are each hydrogen, lower alkyl, lower alkenyl, acyl, aryl or ar(lower)alkyl, in which aryl and the aryl moiety of the ar(lower)alkyl may contain at least one substituent selected from the group consisting of halogen, lower alkoxy, amino, nitro, hydroxy, acyloxy, ar(lower)alkoxy, lower alkylenedioxy, halo(lower)alkyl, acylamino, ar(lower)alkylamino and aryl, and pharmaceutically acceptable salts thereof.

1,2,3,4-Tetrahydroisoquinolines and the preparation thereof

1,2,3,4-Tetrahydroisoquinolines of the formula ##STR1## wherein R is a heterocyclic group which may have appropriate substituent(s) and pharmaceutically acceptable salts thereof, which have relaxing activity on smooth muscle, are disclosed, together with a method for their preparation.

A 1,2,3,4-tetrahydroisoquinoline having the formula: ##SPC1## Which has relaxing activity on smooth muscles.

The present invention relates to new 1,2,3,4-tetrahydroisoquinoline derivatives, which have relaxing activity on smooth muscles. The present invention also relates to the preparation of new and known 1,2,3,4-tetraydroisoquinoline derivatives.

Growing community of inventors

Kawanishi, Japan

Teiji Kishimoto