Sigma receptor-binding agent
AssigneeFUJIFILM Toyama Chemical Co., Ltd.
InventorTakeaki Yano
Life of this patent
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Abstract
A sigma receptor-binding agent, which comprises an alkyl ether derivative represented by formula [1] or a salt thereof is provided. wherein R1 and R2, which are the same or different, each represent a hydrogen atom, a halogen atom, an optionally substituted C1-6 alkyl group, an optionally substituted aryl group, or the like; R3 represents an optionally protected hydroxyl group or the like; m and n, which are the same or different, each represent an integer of 1 to 6.
Claims13
A method for inhibition of a sigma receptor, which comprises administering an alkyl ether derivative represented by the formula [1] or a salt thereof to a subject in need of inhibition of a sigma receptor:
- wherein R1 and R2, which are the same or different, each represent at least one member selected from the group consisting of a hydrogen atom, a halogen atom, an optionally substituted C1-6 alkyl group, an optionally substituted aryl group, an optionally substituted ar(C1-6)alkyl group, an optionally substituted C1-6 alkoxy group, an optionally substituted aryloxy group, an optionally substituted C1-6 alkylthio group, an optionally substituted arylthio group, an optionally substituted C2-6 alkenyl group, an optionally substituted C2-6 alkenyloxy group, an optionally substituted C1-6 alkylamino group, an optionally substituted C1-6 alkylsulfonyl group, an optionally substituted arylsulfonyl group, an optionally substituted carbamoyl group, an optionally substituted heterocyclic group, an optionally protected amino group, an optionally protected hydroxyl group, an optionally protected carboxyl group, a nitro group, and an oxo group;
- R3 represents an optionally substituted C1-6 alkylamino group, an optionally protected amino group, or an optionally protected hydroxyl group;
- m and n, which are the same or different, each represent an integer of 1 to 6.
A method for inhibition of a sigma receptor, which comprises administering an alkyl ether derivative represented by the formula [1] or a salt thereof to a subject in need of inhibition of a sigma-1 receptor:
- wherein R1 and R2, which are the same or different, each represent at least one member selected from the group consisting of a hydrogen atom, a halogen atom, an optionally substituted C1-6 alkyl group, an optionally substituted aryl group, an optionally substituted ar(C1-6)alkyl group, an optionally substituted C1-6 alkoxy group, an optionally substituted aryloxy group, an optionally substituted C1-6 alkylthio group, an optionally substituted arylthio group, an optionally substituted C2-6 alkenyl group, an optionally substituted C2-6 alkenyloxy group, an optionally substituted C1-6 alkylamino group, an optionally substituted C1-6 alkylsulfonyl group, an optionally substituted arylsulfonyl group, an optionally substituted carbamoyl group, an optionally substituted heterocyclic group, an optionally protected amino group, an optionally protected hydroxyl group, an optionally protected carboxyl group, a nitro group, and an oxo group;
- R3 represents an optionally substituted C1-6 alkylamino group, an optionally protected amino group, or an optionally protected hydroxyl group;
- m and n, which are the same or different, each represent an integer of 1 to 6.
A method for inhibition of a sigma receptor, which comprises administering 1 (3 (2 (1 benzothiophene-5-yl)ethoxy)propyl)azetidine-3-ol or a salt thereof to a subject in need of inhibition of a sigma-2 receptor.
A method for investigating the physiological function and/or activity of sigma receptors, which comprises
- (i) labeling an alkyl ether derivative represented by the formula [1] or a salt thereof with a label compound;
- (ii) administering the labeled alkyl ether derivative or a salt thereof to cells and/or living body;
- and
- (iii) imaging a distribution of sigma receptor in cells and/or living body by ray and/or radiation which is released from the label compound:
- wherein R1 and R2, which are the same or different, each represent at least one member selected from the group consisting of a hydrogen atom, a halogen atom, an optionally substituted C1-6 alkyl group, an optionally substituted aryl group, an optionally substituted ar(C1-6)alkyl group, an optionally substituted C1-6 alkoxy group, an optionally substituted aryloxy group, an optionally substituted C1-6 alkylthio group, an optionally substituted arylthio group, an optionally substituted C2-6 alkenyl group, an optionally substituted C2-6 alkenyloxy group, an optionally substituted C1-6 alkylamino group, an optionally substituted C1-6 alkylsulfonyl group, an optionally substituted arylsulfonyl group, an optionally substituted carbamoyl group, an optionally substituted heterocyclic group, an optionally protected amino group, an optionally protected hydroxyl group, an optionally protected carboxyl group, a nitro group, and an oxo group;
- R3 represents an optionally substituted C1-6 alkylamino group, an optionally protected amino group, or an optionally protected hydroxyl group;
- m and n, which are the same or different, each represent an integer of 1 to 6.
A method for inhibition of a sigma receptor, which comprises
- (i) identifying a subject in need of inhibition of a sigma receptor by analyzing an expression of sigma receptor gene in a subject and/or measuring an activity of sigma receptor in a subject;
- and
- (ii) administering an alkyl ether derivative represented by the formula [1] or a salt thereof to the subject in need of inhibition of a sigma receptor:
- wherein R1 and R2, which are the same or different, each represent at least one member selected from the group consisting of a hydrogen atom, a halogen atom, an optionally substituted C1-6 alkyl group, an optionally substituted aryl group, an optionally substituted ar(C1-6)alkyl group, an optionally substituted C1-6 alkoxy group, an optionally substituted aryloxy group, an optionally substituted C1-6 alkylthio group, an optionally substituted arylthio group, an optionally substituted C2-6 alkenyl group, an optionally substituted C2-6 alkenyloxy group, an optionally substituted C1-6 alkylamino group, an optionally substituted C1-6 alkylsulfonyl group, an optionally substituted arylsulfonyl group, an optionally substituted carbamoyl group, an optionally substituted heterocyclic group, an optionally protected amino group, an optionally protected hydroxyl group, an optionally protected carboxyl group, a nitro group, and an oxo group;
- R3 represents an optionally substituted C1-6 alkylamino group, an optionally protected amino group, or an optionally protected hydroxyl group;
- m and n, which are the same or different, each represent an integer of 1 to 6.
Dependencies are inferred from the claim text.