11 α-Amino-androstanes

Claim 2

Compounds of formula ##STR3## (wherein: R 1 is a hydrogen atom, a C 1-8 alkyl group or a C 3-7 cycloalkyl group; and R 2 is a hydrogen atom, a C 1-6 alkyl group or a C 3-6 cycloalkyl group; and the D-homo analogues thereof having the group -CO 2 R 2 (wherein R 2 is as defined above) at the 17aβ-position and salts and zwitterionic forms thereof.

Claim 3

Compounds as claimed in claim 1 wherein R 1 is an isopentyl, hexyl, isohexyl, neohexyl, cyclopentyl or cyclohexyl group and R 2 is a methyl or ethyl group, wherein ring D has 5 members.

Claim 4

Compounds as claimed in either of claims 1 and 2 in the form of physiologically acceptable acid addition salts.

Claim 5

Compounds as claimed in claim 3 in the form of hydrochlorides, hydrobromides, phosphates, sulphates, p-toluenesulphonates, methanesulphonates, citrates, tartrates, acetates, ascorbates, lactates, maleates, succinates, tricarballylates, glutarates and glutaconates.

Claim 6

A compound as claimed in claim 1 which is methyl 11α-cyclohexylamino-3-oxo-5β-androstane-17β-carboxylate and its physiologically acceptable acid addition salts.

Claim 7

A compound as claimed in claim 1 which is methyl 11α-cyclohexylamino-3-oxo-5α-androstane-17β-carboxylate and its physiologically acceptable acid addition salts.

Claim 8

Compounds as claimed in either of claims 5 and 6 in the form of their hydrochlorides.

Claim 9

Pharmaceutical compositions comprising at least one compound of formula (I) as claimed in claim 1 or a physiologically acceptable acid addition salt thereof in admixture with one or more pharmaceutical carriers or excipients.

Claim 10

A process for the manufacture of a compound of formula (I) as claimed in claim 1 which comprises (A) (where a compound in which R 1 is other than hydrogen is desired) reacting a corresponding 11α-amino compound or a corresponding 11α-amino-17β-carboxylic acid with a compound of formula R 1 X wherein R 1 is as defined in claim 1 (other than hydrogen) and X is a readily displaceable atom or group; (B) (where a compound in which R 1 is other than hydrogen is desired) reacting a corresponding 11α-amino compound in the presence of a reducing agent with a monocarbonyl compound serving to introduce the group R 1 as defined in claim 1, other than hydrogen; (C) converting a corresponding N,N-disubstituted 11α-amino into an N-monosubstituted or N-unsubstituted compound; (D) (where a compound in which R 2 is other than hydrogen is desired) esterifying a corresponding 17β-carboxylic acid; (E) reducing a corresponding Δ 16 compound with a suitable reducing agent; (F) (where a compound in which R 2 is hydrogen is desired) hydrolysing a corresponding compound in which R 2 is other than hydrogen; (G) (where a compound in which R 2 is other than hydrogen is desired) transesterifying a corresponding compound having a 17β-ester group other than the desired group R 2 with an alcohol of formula R 2 OH, wherein R 2 is as defined in claim 1, other than hydrogen; (H) oxidising a corresponding 3α or 3β-hydroxy compound; or (I) deprotecting a corresponding compound having a protected 3-oxo group followed, where necessary, by the formation of acid addition or base salts.

Claim 11

A method of treatment or prophylaxis of a human or animal subject suffering from or liable to ventricular dysrhythmias which comprises administering to said subject an effective amount of one or more compounds as claimed in claim 1.