Disilacyclohexane derivatives in anti-fertility agents

Abstract

This disclosure relates to the aspermatogenesis activity of compounds of the following formula: ##STR1## where R.sub.1 and R.sub.2 each independently represent hydrogen, halo having an atomic weight of about 19 to 36, lower alkyl having 1 to 4 carbon atoms, lower alkoxy having 1 to 4 carbon atoms, trifluoromethyl, orR.sub.1 is ##STR2## and R.sub.2 is hydrogen, whereinR.sub.7 and R.sub.8 are each independently hydrogen or lower alkyl having 1 to 2 carbon atoms,n is 0 or 1, andR.sub.3, R.sub.4, R.sub.5 and R.sub.6 each independently represent lower alkyl having 1 to 2 carbon atoms ora pharmaceutically acceptable salt thereof.

Description

Claims

1. A method of inducing aspermatogenesis in male mammals in need of anti-fertility treatment which comprises administering to the mammal an anti-fertility effective amount of a compound of the formula: ##STR5## where R.sub.1 and R.sub.2 each independently represent hydrogen, halo having an atomic weight of about 19 to 36, lower alkyl having 1 to 4 carbon atoms, lower alkoxy having 1 to 4 carbon atoms, trifluoromethyl, or

R.sub.1 is ##STR6## and R.sub.2 is hydrogen,

wherein

R.sub.7 and R.sub.8 are each independently hydrogen or lower alkyl having 1 to 2 carbon atoms,

n is 0 or 1, and

R.sub.3, R.sub.4, R.sub.5 and R.sub.6 each independently represent lower alkyl having 1 to 2 carbon atoms or

a pharmaceutically acceptable salt thereof.

2. A method according to claim 1 in which 200 to 2000 milligrams of the compound are administered daily.

3. A method according to claim 1 in which 500 to 1000 milligrams of the compound are administered daily.

4. A method according to claim 1 in which 100 to 1000 milligrams of the compound are administered per unit dose.

5. A method according to claim 1 in which 250 to 500 milligrams of the compound are administered per unit dose.

6. The method according to claim 1 in which the compound is 4-(m-methoxybenzyl)-2,2,6,6-tetramethyl-1-oxa-4-aza-2,6-disilacycyclohexane or a pharmaceutically acceptable acid addition salt thereof.

7. The method according to claim 1 in which the compound is

(a) 4-(p-chlorobenzyl)-2,2,6,6-tetramethyl-1-oxa-4-aza-2,6-disilacycyclohexane

(b) 4-(p-fluorobenzyl)-2,2,6,6-tetramethyl-1-oxa-4-aza-2,6-disilacycyclohexane

(c) 4-(p-methylbenzyl)-2,2,6,6-tetramethyl-1-oxa-4-aza-2,6-disilacycyclohexane

(d) 4-(p-methoxybenzyl)-2,2,6,6-tetramethyl-1-oxa-4-aza-2,6-disilacycyclohexane,

(e) 4-(3,4-dichlorobenzyl)-2,2,6,6-tetramethyl-1-oxa-4-aza-2,6-disilacycyclohexane,

(f) 4-(3-trifluoromethylbenzyl)-2,2,6,6-tetramethyl-1-oxa-4-aza-2,6-disilacycyclohexane,

(g) 4-(4-dimethylaminobenzyl)-2,2,6,6-tetramethyl-1-oxa-4-aza-2,6-disilacycyclohexane,

(h) 4-(4-dimethylaminomethylbenzyl)-2,2,6,6-tetramethyl-1-oxa-4-aza-2,6-disilacycyclohexane,

(i) 4-(m-chlorobenzyl)-2,2,6,6-tetramethyl-1-oxa-4-aza-2,6-disilacycyclohexane

(j) 4-(m-methylbenzyl)-2,2,6,6-tetramethyl-1-oxa-4-aza-2,6-disilacycyclohexane

(k) 4-(o-chlorobenzyl)-2,2,6,6-tetramethyl-1-oxa-4-aza-2,6-disilacycyclohexane

or a pharmaceutically acceptable acid addition salt thereof.