149353-73-1Relevant articles and documents
BENZAZEPINE DERIVATIVES AND THEIR USE AS HSTAMINE H3 ANTAGONISTS
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Page/Page column 21; 23, (2010/04/03)
A compound having the formula (1) wherein: R1 is a group selected from C3-8 cycloalkyl, C1-6 alkyl, C1-6 alkylene-C3-8 cycloalkyl, each of which groups may optionally be substituted with C1-6 alkyl, halogen, haloC1-6 alkyl or OR15, or R1 is heterocyclyl, optionally substituted with C1-6 alkyl, haloC1-6 alkyl or OR15; n is 0, 1, 2, 3 or 4, the alkylene group -(CH2)n- formed thereby being optionally substituted with a group selected from C1-4 alkyl, C3-8 cycloalkyl and arylsulfonyl; A is a group selected from -N(R2)CO-, -CON(R2)-, -OC(O)-, -C(O)O-, -CO-, -C(R2)(OR3)-, -C(=N-O-R3)-, - C(=CR2R3)-, -C3-8 cycloalkylene-, -C(R2)(haloC1-6 alkyl)-, C1-4 alkylene and -C(OR3)(haloC1-6 alkyl)-; R2 and R3 are each independently selected from H, C1-6 alkyl, and C3-8 cycloalkyl, or, when A is -N(R2)CO- and X is absent, R2 may form, together with the adjacent nitrogen atom and Z, an N-containing heterocyclyl group, which may optionally be substituted; X is absent or is C1-4 alkylene or C2-4 alkenylene, each of which may optionally be substituted with one or more C1-4 alkyl groups, OR16, halogen or haloC1-6 alkyl; Z is selected from aryl, heteroaryl, C3-8 cycloalkyl, and heterocyclyl, each of which may optionally be substituted by a group selected from -Y-aryl, -Y-heteroaryl, -Y-C3-8 cycloalkyl and -Y-heterocyclyl, or, when X is present, Z may be H, or, when X is absent and A is -C(R2)(OR3)- or -N(R2)CO-, Z may be H, or, when A is -N(R2)CO- and X is absent, Z may form, together with the adjacent nitrogen atom and R2, an N-containing heterocyclyl group which may optionally be substituted, wherein, when A is -CO-, Z is linked to X or A via a carbon atom and wherein, when A is -N(R2)CO- and Z is H, R1 is C3-8 cycloalkyl; and Y represents a bond, C1-6 alkylene, CO, NR14, COC2-6 alkenylene, O, SO2 or NHCOC1-6 alkylene; wherein said cycloalkyl, aryl, heteroaryl and heterocyclyl groups Z may be optionally substituted by one or more substituents which may be the same or different, and which are selected from halogen, haloC1-6 alkyl, hydroxy, cyano, nitro, =O, -R4, -CO2R4, -COR4, -NR5R6, -C1-6 alkyl-NR5R6, -C3-8 cycloalkyl-NR5R6, - CONR12R13, -NR12COR13, -NR5SO2R6, -OCONR5R6, -NR5CO2R6, -NR4CONR5R6 or -SO2NR5R6- SHR8, -alkyl-OR8, -SOR8, -OR9, -SO2R9, -OSO2R9, -alkyl-SO2R9, -alkyl-CONHR9, -alkyl-SONHR9, -alkyl-COR10, -CO-alkyl-R10, -O-alkyl-R11 (wherein R4, R5 and R6 independently represent hydrogen, C1-6 alkyl, -C3-8 cycloalkyl, -C1-6 alkylene-C3-8 cycloalkyl, aryl, heterocyclyl or heteroaryl, wherein R8 represents C1-6 alkyl, wherein R9 represents C1-6 alkyl or aryl, wherein R10 represents aryl, wherein R11 represents C3-8 cycloalkyl or aryl, R12, R13, R14, R15 and R16 each independently represent H or C1-6 alkyl, and wherein -NR5R6 and -NR12R13 may represent a nitrogen containing heterocyclyl group); wherein said R4, R5, R6 R8, R9, R11 and R11 groups may be optionally substituted by one or more substituents which may be the same or different, and which are selected from the group consisting of halogen, hydroxy, C1-6 alkyl, C1-6 alkoxy, cyano, amino, =O or trifluoromethyl; and wherein substituents of Z selected from -Y-aryl, -Y-heteroaryl, -Y-C3-8cycloalkyl and -Y-heterocyclyl may be optionally substituted by one or more substituents selected from =O, hydroxy, cyano, nitro, halogen, haloC1-6 alkyl and C1-6alkyl; and wherein, when A is C1-4 alkylene, said cycloalkyl, aryl, heteroaryl or heterocyclyl group Z (such as a heterocyclyl group Z) is substituted at least with hydroxy, CF3, or =0; and wherein, when A is CON(R2) n is 1; or a pharmaceutically acceptable salt or ester thereof, provided that: when A is -CO-, R1 is CH3, C3-8 cycloalkyl-substituted C1-6 alkylene or n-butyl, n is 0 and X is -CH2CH2-, Z is not N-benzyl substituted 4-piperidinyl, N-(3-fluorobenzyl)-substituted 4-piperidinyl or N-acetyl substituted 4-piperidinyl; when A is -OC(O)-, R1 is cyclobutyl, n is 0 and X is -CH2CH2-, Z is not H; when A is -OC(O)-, R1 is n-propyl, n is 0 and X is -CH2-, Z is not H; and when A is -CO-, R1 is CH3, n is 0 and X is CH2, Z is not H.
COMPOUNDS HAVING AFFINITY FOR DOPAMINE D3 RECEPTOR AND USES THEREOF
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Page/Page column 48, (2010/02/15)
Compounds of formula (I) and salts thereof are disclosed: wherein A, R1, m, R2, n, R3, R4, q, W1, W2, R5 and R6 are as defined in the description. Methods of preparing the compounds and uses thereof in medicine, for example in the treatment of schizophrenia or drug dependency, are also disclosed.
USE OF POLYPEPTIDE
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, (2008/06/13)
The present invention provides uses of a polypeptide having a ligand activity to a sensory epithelium neuropeptide-like receptor (SENR) which is a G protein-coupled receptor protein, and a DNA encoding the same. More specifically, the present invention provides an anti-attention-deficit-disorder or anti-narcolepsy agent, which comprises a polypeptide having a ligand activity for SENR or a salt thereof, as well as a method for screening compounds having an anti-attention-deficit-disorder or anti-narcolepsy activity or compounds having an anti-anxiety, anti-depression, anti-insomnia, anti-schizophrenia or anti-fear activity or salts thereof, which comprises using the above polypeptide or a precursor protein of the polypeptide or a salt thereof.
