Naphthothiophene derivatives and their use as respiratory enhanc

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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514253, 5142282, 5142335, 5142338, 549 43, 549 44, 549 45, 549 46, 549 47, 549 26, 549 24, 549 42, 544 60, 544126, 544361, 548237, 548253, A61K 3138, C07D33374

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047974141

ABSTRACT:
Pharmaceutical preparations containing compounds of formula I ##STR1## wherein ring A is unsubstituted or substituted, R.sub.1 and R.sub.2, independently of one another, each represents hydrogen, lower alkyl, aryl or heteroaryl, or R.sub.1 and R.sub.2 together represent lower alkylene optionally interrupted by oxygen, sulfur or optionally substituted nitrogen, Y is methylene, methylene mono- or disubstituted by lower alkyl, oxygen, sulfur, sulfinyl or sulfonyl, X represents a bivalent radical --S--C[--B--(Z).sub.n ].dbd.CH-- the sulfur group S of which is bonded directly to the .alpha.- or to the .beta. -position of the bicyclic ring system, B denotes a direct bond, alkylene or alkenylene; n is 1 or, in case B is alkylene or alkenylene, may be also 2 or 3; and Z represents free or functionally modified carboxy, masked carboxy that can be cleaved under physiological conditions, free or functionally modified formyl, acyl, free or functionally modified sulfo, free, etherified or esterified hydroxy, free, etherified or oxidized etherified mercapto, unsubstituted or substituted amino, ammonio, nitro or halogen; and novel compounds of formula I are disclosed. The latter are prepared by methods known per se.

REFERENCES:
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Liebigs Ann. Chem. (1981), p. 347.
J. Chem. Soc. Perkin Tr. I (1977), p. 63.
C. A. 84: 74018t, (1976), Application of the method for thiophene heterocycle synthesis using sodium sulfide to the preparation of sulfur analogs of polycyclic aromatic hydrocarbons.
J. Prakt. Chem., 314: p. 499 (1972).
C. A. 72: 111328u, (1970), New heterocyclic systems, III, Heterocycles containing a fused thiophene ring.
C. A. 78: 147716g (1973), Condensation of (.beta.-chlorovinyl)carbonyl compounds with a .alpha.-mercaptocaraaboxylic acids.
J. Chem Soc. Perkin I (1973), p. 2956.
Tetrahedron Letters No. 11 (1968), pp. 1317-1319.

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