Anti-anxiety benzothiepino(5,4-c]pyridazines

Details Anti-anxiety benzothiepino(5,4-c]pyridazines Anti-anxiety benzothiepino(5,4-c]pyridazines

1988-03-02

1989-07-18

Schwartz, Richard A.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heterocyclic carbon compounds containing a hetero ring...

544234, A61K 3150, C07D49504

Patent

active

048494216

ABSTRACT:
A benzothiepino 5,4-c]pyridazine compound of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and each is hydrogen, halogen, trifluoromethyl, hydroxy, amino, nitro, cyano, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, or C.sub.2-5 alkanoylamino, R.sup.3 is hydrogen, C.sub.1-8 alkyl, hydroxy-C.sub.1-4 alkyl, C.sub.2-5 alkanoyloxy-C.sub.1-4 alkyl, aryl, aryl-C.sub.1-4 alkyl, heteroaryl, or substituted aryl, aryl-C.sub.1-4 alkyl or heteroaryl by 1 to 3 substituents selected from the group consisting of halogen, trifluoromethyl, hydroxy, amino, nitro, cyano, C.sub.1-4 alkyl, C.sub.1-4 alkoxy and C.sub.2-5 alkanoylamino on the armoatic ring, n is 0, 1 or 2, and the bond between the 4-position and the 4a-position is single bond or double bond.
Said compounds exhibit anti-anxietic activity and are useful as anti-anxiety agent.

REFERENCES:
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patent: 3816438 (1974-06-01), Houlihan
patent: 4602019 (1986-07-01), Sircar et al.
patent: 4692447 (1987-09-01), Cignarella et al.
W. Curran, et al., Journal of Medicinal Chemistry, 1974, vol. 17, No. 3, pp. 273-281.
C. Cignarella et al., Il Farmaco Ed. Sc. 37(2) pp. 133-144 (1981).
T. Yamada, et al., Journal of Medicinal Chemistry, 1982, vol. 25, No. 8, pp. 975-982.
Derwent Abstract 86-015597/03 of EPA Application No. 168350 A, 1/15/86.
J. Lombardino, et al., Journal of Medicinal Chemistry, 1981, vol. 24, pp. 830-834.
M. Ali, et al., Journal Fur Praktische Chemie, vol. 316, No. 2, 1974, pp. 259-266.

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