N,N-bis (quinolin-4-yl)-diamine derivatives, their preparation and their use as antimalarials
AssigneeHoffman-La Roche Inc.
InventorsWerner Hofheinz, Werner Leupin
Life of this patent
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Abstract
Disclosed are N,N'-bis(quinolin-4-yl)diamine derivatives of general formula I wherein R.sup.1 signifies halogen or trifluoromethyl, R.sup.2 signifies hydrogen or halogen, A signifies cyclohexane-1,3-diyl, 2-methyl-cyclohexane-1,3-diyl, cyclohexane-1,4-diyl, dicyclohexylmethane-4,4'-diyl, cyclopentane-1,3-diyl, phenylene-1,4, phenylene-1,3 and phenylene-1,2; n is 1 or 2; m is 1 or 2, as well as their pharmaceutically acceptable salts. These products are useful as agents for preventing malaria and for treating it, especially where the pathogens are resistant to chloroquine. ##STR1##
Claims10
Compounds of the formula, ##STR4## wherein R.sup.1 is halogen or trifluoromethyl;
- R.sup.2 is hydrogen or halogen;
- A is selected from the group consisting of cyclohexane-1,3-diyl, 2-methyl-cyclohexane-1,3,-diyl, cyclohexane-1,4-diyl, dicyclohexylmethane-4,4'-diyl, cyclopentane-1,3-diyl, phenylene-1,4, phenylene-1,3 and phenylene-1,2;
- n is 1 or 2;
- m is 1 or 2;
- and pharmaceutically acceptable acid addition salts.
A pharmaceutical composition comprising a compound of the formula ##STR5## wherein R.sup.1 is halogen or trifluoromethyl;
- R.sup.2 is hydrogen or halogen;
- A is selected from the group consisting of cyclohexane-1,3-diyl, 2-methyl-cyclohexane-1,3-diyl, cyclohexane-1,4-diyl, dicyclohexylmethane-4,4'-diyl, cyclopentane-1,3-diyl, phenylene-1,4, phenylene-1,3 and phenylene-1,2;
- n is 1 or 2;
- m is 1 or 2;
- and pharmaceutically acceptable acid addition salts.
A method for the treatment of malaria comprising administering to a patient an effective amount of a compound of the formula ##STR6## wherein R.sup.1 is halogen or trifluoromethyl;
- R.sup.2 is hydrogen or halogen;
- A is selected from the group consisting of cyclohexane-1,3-diyl, 2-methyl-cyclohexane-1,3-diyl, cyclohexane-1,4-diyl, dicyclohexylmethane-4,4'-diyl, cyclopentane-1,3-diyl, phenylene-1,4, phenylene-1,3 and phenylene-1,2;
- n is 1 or 2;
- m is 1 or 2;
- and pharmaceutically acceptable acid addition salts.
A compound selected from the group consisting of
- (7-chloroquinolin-4-yl)-amine,
- (7-chloroquinolin-4-yl)-amine,
- (7-chloroquinolin-4-yl)-amine,
- (7-chloroquinolin-4-yl)-amine.
Dependencies are inferred from the claim text.