Novel bis- and mono-quaternary ammonium derivatives of 2.beta.,1

Drug – bio-affecting and body treating compositions – Antigen – epitope – or other immunospecific immunoeffector – Bacterium or component thereof or substance produced by said...

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2602395, A61K 3158, C07J 4300

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active

043483909

ABSTRACT:
The invention relates to novel bisquaternary ammonium derivatives of 2.beta.,16.beta.-dipiperidino-5.alpha.-androstanes having the formula: ##STR1## wherein ##STR2## R.sub.2 =CH.sub.3, C.sub.2 H.sub.5 or CH.sub.2 CH.dbd.CH.sub.2 ; R.sub.3 =CH.sub.3, C.sub.2 H.sub.5 or CH.sub.2 CH.dbd.CH.sub.2, with the proviso that R.sub.2 and R.sub.3 are not CH.sub.3 simultaneously; R.sub.4 =O or H(.beta.OR.sub.5), wherein R.sub.5 =H or aliphatic carbacyl (1-6 C); and X=a halogen atom, to processes for their preparation and to pharmaceutical preparations. The invention also relates to novel 16-monoquaternary analogs as intermediates.
The compounds possess neuromuscular blocking activity.

REFERENCES:
patent: 4237126 (1980-12-01), Carlyle et al.
patent: 4297351 (1981-10-01), Carlyle et al.
W. R. Buckett et al., Pancuronuim Bromide and Neuromuscular Blocking Agents Containing Acetyl-Choline Fragments, J. Med. Chem. 16 (10) at 1116 to 1123 (1973).

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