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Claims for Patent: 4,894,369

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Claims for Patent: 4,894,369

Title: Novel 2.beta.-morpholino-androstane derivatives
Abstract:Compounds having the formula: ##STR1## wherein R.sub.1 is H or an optionally substituted acyl group having 1-12 carbon atoms, R.sub.2 is H or an acyl group having 1-12 carbon atoms and R.sub.3 is C, N--CH.sub.3 or a direct bond; and mono- or bisquaternary ammonium compounds thereof and acid addition salts of the non- or mono-quaternary ammonium compounds. Process for the preparation of these compounds. Compositions comprising at least one of the above compounds as the active ingredient. The compounds are favorable neuromuscular blocking agents.
Inventor(s): Sleigh; Thomas (Wishaw, GB6), Savage; David S. (New Mearns, GB6), Carlyle; Ian C. (Hamilton, GB6)
Assignee: Akzo N.V. (Arnhem, NL)
Application Number:07/181,139
Patent Claims: 1. Compounds having the formula: ##STR4## wherein R.sub.1 is H or an optionally substituted acyl group having 1-12 carbon atoms,

R.sub.2 is H or an acyl group having 1-12 carbon atoms and

R.sub.3 is C, N--CH.sub.3 or a direct bond, and mono- or bisquaternary ammonium compounds thereof and acid addition salts of the non- or mono-quaternary ammonium compounds.

2. Compounds according to claim 1, wherein R.sub.1 is H.

3. Compounds according to claim 1, wherein the compounds are 16.beta.-monoquaternary ammonium compounds.

4. Compounds according to claim 1, wherein R.sub.2 is a saturated acyl group having 1-6 carbon atoms.

5. Compounds according to claim 1, wherein R.sub.3 is C or a direct bond.

6. Compositions having neuromuscular blocking activity comprising an aqueous solution of at least one of the compounds claimed in claim 1 in a pharmaceutically effective amount.
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