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US 4,539,410 AGranted
N-Substituted-2-(1-imidazolyl)indoles
AssigneeCiba-Geigy Corporation
InventorHarris B. Renfroe
Life of this patent
Estimating the term…
Abstract
Various 1-carboxylic acid substituted-2-(1-imidazolyl)indoles and functional derivatives thereof are highly specific thromboxane synthetase inhibitors. Synthesis of, pharmaceutical compositions thereof, methods of treatment utilizing such compounds and intermediates for their synthesis are included.
Claims9
A compound of the formula ##STR9## wherein R.sub.1 represents hydrogen or lower alkyl;
- Im represents 1-imidazolyl unsubstituted or substituted by lower alkyl, carboxy, lower alkoxycarbonyl or carbamoyl;
- R.sub.2 and R.sub.3 independently represent hydrogen, lower alkyl, halogen, trifluoromethyl, hydroxy, lower alkoxy, lower alkyl-(thio, sulfinyl or sulfonyl);
- or R.sub.2 and R.sub.3 together when attached to adjacent carbons represent lower alkylenedioxy;
- A represents alkylene of 1 to 12 carbon atoms, alkenylene of 2 to 12 carbon atoms, alkynylene of 2 to 12 carbon atoms, lower alkylenephenylene-lower alkylene, lower alkylenephenylene, phenylene-lower alkylene, phenylene, a direct bond, lower alkylene-(thio or oxy)-lower alkylene, (thio or oxy)-phenylene, lower alkylene-(thio- or oxy)-phenylene, phenylene-(thio or oxy)-lower alkylene or phenylene-lower alkenylene;
- B represents hydroxycarbamoyl, 5-tetrazolyl or formyl;
- the N-oxide thereof;
- or a pharmaceutically acceptable salt thereof.
4 more elements
A compound of the formula I ##STR10## wherein R.sub.1 represents hydrogen or lower alkyl;
- Im represents 1-imidazolyl unsubstituted or substituted by lower alkyl, carboxy, lower alkoxycarbonyl or carbamoyl;
- R.sub.2 and R.sub.3 independently represent hydrogen, lower alkyl, halogen, trifluoromethyl, hydroxy, lower alkoxy, lower alkyl-(thio, sulfinyl or sulfonyl);
- or R.sub.2 and R.sub.3 together when attached to adjacent carbons represent lower alkylenedioxy;
- A represents (thio- or oxy)-phenylene, phenylene-(thio or oxy)-lower alkylene or phenylene-lower alkenylene;
- B represents carboxy, lower alkoxycarbonyl, carbamoyl, mono- or di-lower alkylcarbamoyl, cyano, hydroxymethyl, hydroxycarbamoyl, 5-tetrazolyl or formyl;
- the N-oxide thereof;
- or a pharmaceutically acceptable salt thereof.
4 more elements
A compound of the formula IV ##STR11## wherein R.sub.1 represents hydrogen or lower alkyl;
- Im represents 1-imidazolyl unsubstituted or substituted by lower alkyl, carboxy, lower alkoxycarbonyl or carbamoyl;
- R.sub.2 and R.sub.3 independently represent hydrogen, lower alkyl, halogen, trifluoromethyl, hydroxy, lower alkoxy, lower alkyl-(thio, sulfinyl or sulfonyl);
- or R.sub.2 and R.sub.3 together when attached to adjacent carbons represent lower alkylenedioxy;
- or an acid-addition salt thereof.
1 more element
Dependencies are inferred from the claim text.