Naphthalene derivatives, process for the preparation therof, and

Details Naphthalene derivatives, process for the preparation therof, and Naphthalene derivatives, process for the preparation therof, and

1996-06-14

1999-12-21

Robinson, Allen J.

Organic compounds -- part of the class 532-570 series

Organic compounds

Four or more ring nitrogens in the bicyclo ring system

544237, 544354, 544355, 544315, 544111, 544124, 544239, 544238, 514299, 514300, 514256, 514259, 5142305, 514318, 514352, C07C 1500, C07D23730, C07D23700, A61K 3144

Patent

active

06005106&

ABSTRACT:
Naphthalene derivatives of the formula [I]: wherein R.sup.1 and R.sup.2 are the same or different and are each H, protected or unprotected OH, one of R.sup.3 and R.sup.4 is protected or unprotected hydroxymethyl, and the other is H, lower alkyl, or protected or unprotected hydroxymethyl, R.sup.5 and R.sup.6 are the same or different and are each H, substituted or unsubstituted lower alkyl, substituted or unsubstituted phenyl or protected or unprotected NH.sub.2, or both combine together with the adjacent N to form substituted or unsubstituted heterocyclic group, and pharmaceutically acceptable salts thereof, these compounds showing excellent bronchoconstriction inhibitory activity, and hence, being useful in the prophylaxis or treatment of asthma.

REFERENCES:
Akio Sakurai et al., "The Cyclization of Ethyl Acetoacetate and Ketones by Ammonium Acetate" Bull. Chem. Soc. Japan, vol. 41, (1968) pp. 165-167.
D.N. Reinhoudt et al., "A Novel Route for the Synthesis of Benzo [b] Thiepins" Tetrahedron, vol. 30, (1974) pp. 2431-2436.
C. David Nicholson et al., "Differential Modulation of Tissue Function and Therapeutic Potential of Selective Inhibitors of Cyclic Nucleotide Phosphodiesterase Isoenzymes" Trends in Pharmacol. vol. 12, p. 19 (1991.

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