| abstract |
These compounds have antagonistic activity of the ORL1 receptor; and therefore, they are useful in the manufacture and pharmaceutical compositions and medications for treating diseases or conditions such as pain, various CNS diseases, sleep and eating disorders. Claim 1: A compound of the following formula (1) or a pharmaceutically acceptable ether of such a compound, or a pharmaceutically acceptable salt or solvate thereof, wherein R1 and R2 independently represent an H atom, a halogen atom or a C1-3 alkyl group; R3 represents a C6-10 aryl group in the ring or a heteroaryl group and said heteroaryl group is a 5- to 10-membered heteroaromatic group containing 1 to 3 heteroatoms selected from an O atom, an S atom and an atom of N; said aryl group and heteroaryl group are optionally substituted with 1 to 3 groups selected from a halogen atom, a hydroxy group, a C1-3 alkyl group, a C1-3 alkoxy group, a C1-6 alkyl group interrupted by an atom of Or, a C1-3 hydroxyalkyl group, an amino group, a mono- or di-C1-3 alkylamino group; an aminocarbonyl group, a C1-3 mono- or dialkylaminocarbonyl group in each alkyl group, a C1-3 alkanoylamino group and a C1-3 alkylsulfonylamino group, -XY- represents a group of formula -N (R4) C (= O) -, -C (= O) N (R4) -, N (R4) CH2-, -CH2N (R4) -, -N (R4) SO2-, -SO2N (R4) -, -CH2CH2-, -CH = CH-, -CH (CH2OH) CH2-, -CH2CH (CH2OH) -, -CH2CH (OH) -, - CH (OH) CH2-, -C (R4) (R5) -O or -OC (R4) ( R5) -; R4 represents an atom of H or a C1-3 alkyl group; R5 represents an atom of H, a C1-3 alkyl group or a C1-3 hydroxyalkyl group, n represents an integer 0, 1 or 2. |