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US 6,486,190 B1Granted
5-(2-imidazolinylamino)-benzimidazole derivatives, their preparation and their use as .alpha.-adrenoceptor agonists with improved metabolic stability
AssigneeThe Procter & Gamble Company
InventorsThomas Lee Cupps, Sophie Eva Bogdan, Nick Nikolaides, Sheri Ann Gilbert, Michael Gazda, Roy Lee Dobson, Charles Andrew III Cruze
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Abstract
Benzimidazole compounds having the generic structure: are used to treat alpha-2 mediated disorders, including nasal congestion, glaucoma, asthma, migraine, and diarrhea.
Claims19
A compound having the following structure:
- wherein:
- (a) R1 is alkyl;
- (b) R2 is selected from the group consisting of:
- hydrogen, alkyl, methoxy, cyano, and halo;
- (c) R3 is selected form the group consisting of:
- hydrogen, methyl, hydroxy, cyano and halo;
- (d) R4 is hydrogen;
- (e) R5 is selected from the group consisting of:
- hydrogen, methyl, amino, methoxy, hydroxy, cyano and halo;
- (f) provided that at least one of R2, R3, or R5 is other than hydrogen or fluorine;
- (g) provided that when R1 is methyl and both R2 and R5 are hydrogen, R3 is other than methyl or halo;
- (h) provided that when R3 is cyano, R1 is methyl;
- and any tautomer of the above structure or pharmaceutically acceptable salt, or biohydrolyzable ester, amide, or imide thereof.
10 more elements
Dependencies are inferred from the claim text.