Triazolopyridazine derivatives
AssigneeHoffmann-La Roche Inc.
InventorsCedric H. Hassall, Christopher J. Moody
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Abstract
The present disclosure is directed to 1-substituted or unsubstituted lower alkylene, 5-carboxy, alkanoyloxy or carbamoyloxy triazolopyridazine derivatives, salts of the acids and pharmaceutically-acceptable bases thereof. The triazolopyridazine derivatives provided by the present invention are useful as angiotensin-related antihypertensive agents.
Claims32
A triazolopyridazine derivative of the formula:
- ##STR12## wherein A is methylene, ethylene or propylene which may be substituted by lower alkyl;
- R.sup.1 is halogen, carboxyl, lower alkoxycarbonyl, aminocarbonyl, hydroxyaminocarbonyl, hydrazinocarbonyl, mercapto, lower alkanoylthio or aryl-lower alkylthio;
- R.sup.2 is hydroxy, lower alkoxy or amino;
- R.sup.3 and R.sup.4 each is hydrogen or halogen or R.sup.3 is hydrogen and R.sup.4 is hydroxy;
- and R.sup.5 is hydrogen, lower alkyl, aryl, carboxy, lower alkoxycarbonyl or aminocarbonyl;
- and the broken line denotes an optional carbon-carbon bond which can be present only when R.sup.3 and R.sup.4 each is hydrogen, or a salt of an acid of formula I with a pharmaceutically acceptable base.
A compound of the formula ##STR13## wherein R.sup.2 is hydroxy, lower alkoxy or amino;
- R.sup.3 and R.sup.4 each is hydrogen or halogen, or R.sup.3 is hydrogen and R.sup.4 is hydroxy;
- and R.sup.5 is hydrogen or lower alkyl, aryl, carboxy, lower alkoxycarbonyl or aminocarbonyl;
- and the broken line denotes an optional carbon-carbon bond which can be present only when R.sup.3 and R.sup.4 each is hydrogen, with the proviso that when a double bond is present in the 6,7-position and R.sup.2 is hydroxy, or when R.sup.3 and R.sup.4 each is hydrogen and R.sup.2 is hydroxy, R.sup.5 is other than hydrogen.
An antihypertensive composition which comprises effective amounts of a triazolopyridazine derivative of the formula ##STR14## wherein A is methylene, ethylene or propylene which may be substituted by lower alkyl;
- R.sup.1 is halogen, carboxyl, lower alkoxycarbonyl, aminocarbonyl, hydroxyaminocarbonyl, hydrazinocarbonyl, mercapto, lower alkanoylthio or aryl-lower alkylthio;
- R.sup.2 is hydroxy, lower alkoxy or amino;
- R.sup.3 and R.sup.4 each is hydrogen or halogen or R.sup.3 is hydrogen and R.sup.4 is hydroxy;
- and R.sup.5 is hydrogen, lower alkyl, aryl, carboxy, lower alkoxycarbonyl or aminocarbonyl;
- and the broken line denotes an optional carbon-carbon bond which can be present only when R.sup.3 and R.sup.4 each is hydrogen, or a pharmaceutically-acceptable salt of an acid thereof and a pharmaceutically-acceptable carrier.
Compounds of the general formula ##STR15## wherein A is methylene, ethylene or propylene which may be substituted by lower alkyl;
- and R.sup.10 is halogen, carboxyl or lower alkoxycarbonyl.
Compounds of the general formula ##STR16## wherein A is methylene, ethylene or propylene which may be substituted by lower alkyl;
- R.sup.1 is halogen, carboxyl, lower alkoxycarbonyl, aminocarbonyl, hydroxyaminocarbonyl, hydrazinocarbonyl, mercapto, lower alkanoylthio or aryl-lower alkylthio;
- R.sup.2 is hydroxy, lower alkoxy or amino;
- R.sup.3 and R.sup.4 each is hydrogen or halogen or R.sup.3 is hydrogen and R.sup.4 is hydroxy;
- R.sup.5 is hydrogen, lower alkyl, aryl, carboxy, lower alkoxycarbonyl or aminocarbonyl;
- and the broken line denotes an optional carbon-carbon bond which can be present only when R.sup.3 and R.sup.4 each is hydrogen.
Compounds of the general formula ##STR17## wherein R.sup.2 is hydroxy, lower alkoxy or amino;
- R.sup.3 and R.sup.4 each is hydrogen or halogen or R.sup.3 is hydrogen and R.sup.4 is hydroxy;
- and R.sup.5 is hydrogen, lower alkyl, aryl, carboxy, lower alkoxycarbonyl or aminocarbonyl;
- and the broken line denotes an optional carbon-carbon bond which can be present only when R.sup.3 and R.sup.4 each is hydrogen.
Dependencies are inferred from the claim text.