Benzoxazole derivatives
AssigneesMeiji Seika Kaisha, Ltd., Koichi Shudo
InventorsKatsuyoshi Iwamatsu, Yasuo Sato, Masaaki Izumi, Fukio Konno, Seiji Shibahara, Shigeharu Inoye, Koichi Shudo, Kazuko Amano
Life of this patent
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Abstract
A benzoxazole derivative of the formula (1) or (2) which has an alicyclic diamine group at the 2-position: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, X.sup.-, m and n are defined herein. The compound shows excellent 5-HT.sub.3 receptor antagonism and is useful as an antiemetic agent, a peristalsis controlling agent, an analgesic agent, an antianxiety agent and a schizophrenia treating agent.
Claims9
A compound represented by the formula (1) ##STR7## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4 may be the same or different and each represents a hydrogen atom, a substituted or unsubstituted lower alkyl group, a substituted or unsubstituted lower alkenyl group, a halogen atom, a hydroxyl group, an amino group, a lower alkoxyl group, a carboxyl group, a carbamoyl group or a nitro group, in which any two groups of R.sup.1 to R.sup.4 may be linked to each other to form a six-membered ring structure comprising carbon atoms alone, which may be substituted;
- R.sup.5 represents a substituted or unsubstituted lower alkyl group, a substituted or unsubstituted lower alkenyl group, a substituted or unsubstituted aralkyl group containing 7 to 10 carbon atoms or an alkoxycarbonyl group, with the proviso that R.sub.5 is a substituted alkyl group and is not an alkyl group substituted with an amino or dialkylamino group when R.sub.1, R.sub.2, R.sub.3 and R.sub.4 represent hydrogen atoms simultaneously;
- and m is an integer of 2 or 3 and n is an integer of 2;
- wherein each substituent is selected from the group consisting of a halogen atom, a hydroxyl group, a cyano group, an alkylcarbonyl group, an alkoxy group, a carboxyl group, an alkoxycarbonyl group, a carbamoyl group, an amino group and a nitro group;
- and said halogen atom is selected from the group consisting of fluorine, chlorine, bromine, and iodine.
A compound represented by the formula (2) ##STR8## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 may be the same or different and each represents a hydrogen atom, a substituted or unsubstituted lower alkyl group, a substituted or unsubstituted lower alkenyl group, a halogen atom, a hydroxyl group, an amino group, a lower alkoxyl group, a carboxyl group, a carbamoyl group or a nitro group, in which any two groups of R.sup.1 to R.sup.4 may be linked to each other to form a six-membered ring structure comprising carbon atoms alone, which may be substituted;
- R.sup.5 and R.sup.6 may be the same or different and each represents a substituted or unsubstituted lower alkyl group, a substituted or unsubstituted lower alkenyl group, a substituted or unsubstituted aralkyl group containing 7 to 10 carbon atoms or an alkoxycarbonyl group, in which R.sup.5 and R.sup.6 may be linked to each other to form a five-membered ring structure comprising carbon atoms, which may be substituted, with the proviso that R.sub.5 is a substituted alkyl group and is not an alkyl group substituted with an amino or dialkylamino group when R.sub.1, R.sub.2, R.sub.3 and R.sub.4 represent hydrogen atoms simultaneously;
- X.sup.- represents a pharmaceutically acceptable anion;
- and m is an integer of 2 or 3 and n is an integer of 2;
- wherein each substituent is selected from the group consisting of a halogen atom, a hydroxyl group, a cyano group, an alkylcarbonyl group, an alkoxy group, a carboxyl group, an alkoxycarbonyl group, a carbamoyl group, an amino group and a nitro group;
- and said halogen atom is selected from the group consisting of fluorine, chlorine, bromine, and iodine.
Dependencies are inferred from the claim text.