Pyrrolo [1,2A] thieno [3,2-F] [1,4] diazepines

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...

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540560, C07D49514, A61K 3155

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active

051531909

ABSTRACT:
The invention relates to pyrrolo [1,2-a] thieno [3,2-f][1,4]diazepine compounds of the formula (I) ##STR1## in which: R.sub.1 is hydrogen; alkyl optionally substituted with alkoxy, hydroxy, cycloalkyl, or phenyl; or alkyl- or arylsulfonyl; R.sub.2 is hydrogen, phenyl, or phenylalkyl; alkyl optionally substituted with hydroxyl, alkoxy, oxo, cycloalkyl or phenyl; or optionally substituted amino; R.sub.3 represents hydrogen or alkyl, and R.sub.4 and R.sub.5 independently represent: hydrogen, alkyl optionally substituted with alkoxy, cycloalkyl, or phenyl; or phenyl; their isomers, diastereoisomers and enantiomers as well as their addition salts with pharmaceutically-acceptable acids. The compounds are useful for treating cerebral ischemia, hypertriglyceridemia, hypercholesterolemia, hyperlipidemia, and hyperglycemia and are obtained in a few steps from the corresponding substituted 2-(1-pyrrolyl)thiophenes ##STR2## Y=--CHO or H; X= CN, CONH.sub.2, CH.sub.2 NHCOR.sub.2, or CH.sub.2 NH.sub.2.

REFERENCES:
Pyrrolothienopyrazine: Synthese de la pyrrolo [1,2-a]thieno [3,2-3]pyrazine et de la pyrrolo[1,2]thieno [2,3-e]pyrazine, S. Rault, et al. Journal of Hetrocyclic Chemistry (1983) vol. 20, pp. 17-21.
2-amino thiophene aus methylenaktiven Nitrilen, carbonyl verbindungen und schwefel, K. Gewald, et al., Chem Ber (1966) 99, pp. 94-101.
2-amino thiophene aus a-oxo-mercaptanen und methylenaktiven Nitrilen K. Gewald, Angew. Chem. Ber (1965) 98, pp. 3571-3577.
Aur Reaktion von a-oxo mercaptanen mit Nitrilen Angew Chem. (1961) 73, pp. 114, Gewald.
C. R. Aead. Se. Paris, t. 285(Oct. 31, 1977), vol. C, pp. 381-383, S. Rault, et al.
C. R. Aead. Se Paris, t. 287 (Sep. 11, 1978), vol. C, pp. 117-120, S. Rault, et al.

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