Dihydronaphthalene derivative
AssigneeOno Pharmaceutical Co., Ltd.
InventorsKensuke Kusumi, Haruto Kurata, Atsushi Naganawa, Yasuyo Kodera, Yuichi Inagaki, Hiroya Takizawa, Mark Allan Wolf, Joseph Raker
Life of this patent
Estimating the term…
Abstract
A compound represented by general formula (I) wherein all the symbols are as defined in the specification has a selective S1P5 receptor agonist activity due to having a linker from a phenyl group to a cyclic substituent in a dihydronaphthalene skeleton; i.e., due to having a short linker of one atom or less as L in general formula (I), and can therefore serve as an agent for treating S1P5-mediated disease, e. g., neurodegenerative disease such as schizophrenia.
Claims9
A compound of the following general formula (I):
- wherein, R1 represents a C1-4 alkyl group or a halogen atom;
- R2 represents a C1-3 alkyl group, a halogen atom or a C1-3 haloalkyl group;
- R3 represents a C1-4 alkyl group;
- L represents a bond, —CH2— or —O—;
- Z represents a carboxyl group which may be substituted with a C1-8 alkyl group;
- ring 1 represents (1) cyclopentane, (2) cyclohexane, (3) cycloheptane, (4) cyclopentene, (5) benzene, (6) pyridine, (7) naphthalene, (8) indole, or (9) dihydroindole;
- ring 2 represents (1) azetidine or (2) pyrrolidine;
- m represents an integer of 0 to 2;
- n represents an integer of 0 or 1;
- p represents an integer of 0 or 1;
- and
- when m is 2, a plurality R1s may be the same or different,
- with proviso that when L is —O— and ring 1 is benzene, R2 represents a halogen atom or trifluoromethyl group,
- a salt thereof, a solvate thereof, an N-oxide thereof, or a prodrug thereof.
A method for treating an S1P5-mediated disease, comprising administering to a mammal an effective amount of a compound of the following general formula (I):
- wherein, R1 represents a C1-4 alkyl group, or a halogen atom;
- R2 represents a C1-3 alkyl group, a halogen atom or a C1-3 haloalkyl group;
- R3 represents a C1-4 alkyl group;
- L represents a bond, —CH2— or —O—,
- Z represents a carboxyl group which may be substituted with a C1-8 alkyl group;
- ring 1 represents (1) cyclopentane, (2) cyclohexane, (3) cycloheptane, (4) cyclopentene, (5) benzene, (6) pyridine, (7) naphthalene, (8) indole, or (9) dihydroindole;
- ring 2 represents (1) azetidine or (2) pyrrolidine;
- m represents an integer of 0 to 2;
- n represents an integer of 0 or 1;
- p represents an integer of 0 or 1;
- and
- when m is 2, a plurality R1s may be the same or different;
- a salt thereof, a solvate thereof, an N-oxide thereof, or a prodrug thereof.
Dependencies are inferred from the claim text.