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US 5,665,752 AGranted
Use of imidazopyrazole derivatives as analgesics and anti-inflammatory agents
AssigneeSankyo Company, Limited
InventorsAtsusuke Terada, Kazuyuki Wachi, Hachio Miyazawa, Yoshio Iizuka, Kazuo Hasegawa, Keiichi Tabata
Life of this patent
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Abstract
Described herein are compounds of formula (I): ##STR1## and pharmaceutically acceptable salts thereof are analgesics and anti-inflammatory agents as well having anti-ulcer and 5-lipoxygenase inhibitory activities.
Claims13
A method of relieving or alleviating allergic reactions by the administration to a mammal suffering from said allergic reactions of an effective amount of an inhibitor of 5-lipoxygenase, wherein said inhibitor is selected from the group consisting of compounds of formula (I):
- ##STR10## in which:
- R.sup.1 and R.sup.2 are independently selected from the group consisting of:
- hydrogen atoms;
- C.sub.1 -C.sub.25 alkyl groups;
- substituted C.sub.1 -C.sub.6 alkyl groups having at least one substituent selected from the group consisting of substituents (a), defined below;
- C.sub.3 -C.sub.8 cycloalkyl groups;
- C.sub.2 -C.sub.6 alkenyl groups;
- aralkyl groups in which the alkyl part is C.sub.1 -C.sub.4 and the aryl part is C.sub.6 -C.sub.10 and is unsubstituted or has at least one substituent selected from the group consisting of substituents (b), defined below;
- arylalkenyl groups in which the aryl part is a C.sub.6 -C.sub.10 aryl group which is unsubstituted or has at least one substituent selected from the group consisting of substituents (b), defined below, and the alkenyl part is C.sub.2 -C.sub.3 alkenyl;
- C.sub.6 -C.sub.10 aryl groups;
- C.sub.6 -C.sub.10 aryl groups having at least one substituent selected from the group consisting of substituents (b), defined below;
- cyano groups;
- and halogen atoms;
- R.sup.3 represents:
- a hydrogen atom;
- a C.sub.1 -C.sub.25 alkyl group;
- a substituted C.sub.1 -C.sub.6 alkyl group having at least one substituent selected from the group consisting of substituents (a), defined below;
- an aralkyl group in which the alkyl part is C.sub.1 -C.sub.4 and the aryl part is C.sub.6 -C.sub.10 and is unsubstituted or has at least one substituent selected from the group consisting of substituents (b), defined below;
- a C.sub.1 -C.sub.6 aliphatic carboxylic acyl group;
- or an aromatic carboxylic acyl group in which the aryl part is a C.sub.6 -C.sub.10 carbocyclic aryl group which is unsubstituted or has at least one substituent selected from the group consisting of substituents (b), defined below;
- R.sup.4 and R.sup.5 are independently selected from the group consisting of:
- hydrogen atoms;
- C.sub.1 -C.sub.25 alkyl groups;
- substituted C.sub.1 -C.sub.6 alkyl groups having at least one substituent selected from the group consisting of substituents (a), defined below;
- C.sub.3 -C.sub.8 cycloalkyl groups;
- C.sub.2 -C.sub.6 alkenyl groups;
- aralkyl groups in which the alkyl part is C.sub.1 -C.sub.4 and the aryl part is C.sub.6 -C.sub.10 and is unsubstituted or has at least one substituent selected from the group consisting of substituents (b), defined below;
- arylalkenyl groups in which the aryl part is a C.sub.6 -C.sub.10 aryl group which is unsubstituted or has at least one substituent selected from the group consisting of substituents (b), defined below, and the alkenyl part is C.sub.2 -C.sub.3 alkenyl;
- C.sub.6 -C.sub.10 aryl groups;
- and C.sub.6 -C.sub.10 aryl groups having at least one substituent selected from the group consisting of substituents (b), defined below;
- substituents (a):
- hydroxy groups, halogen atoms, carboxy groups, cyano groups, and C.sub.2 -C.sub.7 alkoxycarbonyl groups
- substituents (b):
- C.sub.1 -C.sub.6 alkyl groups;
- halogen atoms;
- C.sub.1 -C.sub.6 alkoxy groups;
- aryloxy groups in which the aryl part is an unsubstituted C.sub.6 -C.sub.10 carbocyclic aryl group;
- aralkyloxy groups in which the alkyl part is C.sub.1 -C.sub.4 and the aryl part is C.sub.6 -C.sub.10 and is unsubstituted;
- C.sub.1 -C.sub.6 aliphatic carboxylic acyl groups;
- aromatic carboxylic acyl groups in which the aryl part is a C.sub.6 -C.sub.10 carbocyclic aryl group which is unsubstituted or has at least one substituent selected from the group consisting of C.sub.1 -C.sub.4 alkyl groups, C.sub.1 -C.sub.4 alkoxy groups and halogen atoms;
- C.sub.1 -C.sub.6 aliphatic carboxylic acyloxy groups;
- aromatic carboxylic acyloxy groups in which the aryl part is a C.sub.6 -C.sub.10 carbocyclic aryl group which is unsubstituted or has at least one substituent selected from the group consisting of C.sub.1 -C.sub.4 alkyl groups, C.sub.1 -C.sub.4 alkoxy groups and halogen atoms;
- amino groups;
- C.sub.1 -C.sub.4 alkylamino groups;
- dialkylamino groups in which each alkyl part is C.sub.1 -C.sub.4 ;
- C.sub.1 -C.sub.6 aliphatic carboxylic acylamino groups;
- aromatic carboxylic acylamino groups in which the aryl part is a C.sub.6 -C.sub.10 carbocyclic aryl group which is unsubstituted or has at least one substituent selected from the group consisting of C.sub.1 -C.sub.4 alkyl groups, C.sub.1 - C.sub.4 alkoxy groups and halogen atoms;
- C.sub.1 -C.sub.4 haloalkyl groups;
- carbamoyl groups;
- alkylcarbamoyl and dialkylcarbamoyl groups in which the or each alkyl group is C.sub.1 -C.sub.4 ;
- carboxy groups;
- hydroxy groups;
- cyano groups;
- and C.sub.2 -C.sub.7 alkoxycarbonyl groups;
- and pharmaceutically acceptable salts thereof.
52 more elements
A pharmaceutical composition for the treatment or prophylaxis of pain, inflammation, or ulcers which composition comprises an effective amount of an active compound in admixture with a pharmaceutically acceptable carrier or diluent, wherein said active compound is selected from the group consisting of compounds of formula (I) ##STR11## wherein R.sup.1 =R.sup.3 =R.sup.4 =hydrogen;
- and R.sup.2 =R.sup.5 =phenyl and pharmaceutically acceptable salts thereof.
Dependencies are inferred from the claim text.