Naphthalene derivatives, process for the preparation thereof, an

Details Naphthalene derivatives, process for the preparation thereof, an Naphthalene derivatives, process for the preparation thereof, an

1998-07-02

1999-10-19

Dees, Jose' G.

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

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

546 14, 546152, 546156, 546304, 546311, 546312, 544106, 544111, 544149, 544151, 544358, 544359, 544360, 544361, 544363, 544180, 544194, 514352, 5142315, 514311, 514333, 514334, C07D21500, C07D29500, C07D40300, C07D40100

Patent

active

059691409

ABSTRACT:
Naphthalene derivatives of the formula [I]: ##STR1## 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:
patent: 5342841 (1994-08-01), Iwasaki et al.
Sakurai et al., "The Cyclization of Ethyl Acetoacetate and Ketones by Ammonium Acetate," Bull. Chem. Soc. Japan, 41:165-167 (1968).
Reinhoudt et al., "A Novel Route for the Synthesis of Benzo[b] Thiepins," Tetrahedron, 30:2431-2436 (1974).
Nicholson et al., "Differential Modulation of Tissue Function and Therapeutic Potential of Selective Inhibitors of Cyclic Nucleotide Phosphodiesterase Isoenzymes," Trends in Pharmacol., 12:19 (1991).

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