Substituted azacyclohexyl derivatives of rifamycins

Details Substituted azacyclohexyl derivatives of rifamycins Substituted azacyclohexyl derivatives of rifamycins

1989-04-26

1991-03-26

Shen, Cecilia

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

Organic compounds

Nitrogen attached directly or indirectly to the purine ring...

514824, 544360, 544364, 546198, A61K 31495, A61K 31445, C07D49818

Patent

active

050030701

ABSTRACT:
The invention relates to novel substituted azacyclohexyl derivatives of formula ##STR1## and salts of thereof in which the structural elements --A.sub.1 -A.sub.2, --A.sub.3 -A.sub.4 -- and --A.sub.5 -A.sub.6 -- are each ethylene or vinylene or the elements --A.sub.1 -A.sub.2 -- and --A.sub.3 -A.sub.4 -- are each ethylene and --A.sub.5 -A.sub.6 -- is vinylene, X is >CR.sub.6 -- or >N-- and R.sub.6 is alkyl or hydrogen, alk is an aliphatic hydrocarbon radical or a bond, R.sub.1 is hydrogen or acyl, R.sub.2 is hydrogen or acetyl, R.sub.3 and R.sub.4 together are a bond or each is hydrogen, R.sub.5 is hydrogen, a cycloaliphatic hydrocarbon radical, aryl or heteroaryl and R.sub.7 is hydrogen or alkyl, with the proviso that when --A.sub.1 -A.sub.2 --, --A.sub.3 -A.sub.4 -- and --A.sub.5 -A.sub.6 -- are each vinylene, X is >N--, R.sub.1 is hydrogen or trialkylacetyl, R.sub.2 is hydrogen or acetyl, R.sub.3 and R.sub.4 together are a bond and alk is methylene, R.sub.5 is other than 2,6-dimethyl-4-alkylphenyl, which can be used as active ingredients in medicaments, to their preparation and use and to pharmaceutical preparations.

REFERENCES:
patent: 4005077 (1977-01-01), Bickel et al.
patent: 4327096 (1982-04-01), Marsili et al.
patent: 4353826 (1982-10-01), Bickel et al.
Abstract of WO-A-8,702,361.
Chemical Pharmaceutical Bulletin, vol. 33, No. 5, pp. 2133-2136 (1965).
Abstract of EPA 314,624.

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