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DERIVATIVES OF 4- (4-HETEROCICLILALCOXIFENIL) -1- (HETEROCICLILCARBONIL) PIPERIDINE AND RELATED COMPOUNDS AS HISTAMINE H3 ANTAGONISTS FOR THE TREATMENT OF NEUROLOGICAL DISEASES SUCH AS ALZHEIMER.
DERIVATIVES OF 4- (4-HETEROCICLILALCOXIFENIL) -1- (HETEROCICLILCARBONIL) PIPERIDINE AND RELATED COMPOUNDS AS HISTAMINE H3 ANTAGONISTS FOR THE TREATMENT OF NEUROLOGICAL DISEASES SUCH AS ALZHEIMER.
A compound of formula (I): wherein: R 1 represents -C 1-6 alkyl-O-C 1-6 alkyl, -C 3-8 cycloalkyl, aryl, heterocyclyl, heteroaryl, -C 1-6 alkyl-aryl, -C 1 alkyl -6-heteroaryl, -C 1-6 alkyl-heterocyclyl, -aryl-X-aryl, -aryl-X-heteroaryl, -aryl-X-heterocyclyl, -heteroaryl-X-aryl, -heteroaryl-X-heteroaryl, -heteroaryl -X-heterocyclyl, -heterocyclyl-X-aryl, -heterocyclyl-X-heteroaryl or -heterocyclyl-X-heterocyclyl, wherein said C1-6 alkyl, C3-8 cycloalkyl, aryl, heteroaryl and heterocyclyl groups of R1 may be optionally substituted with one or more (for example, 1, 2 or 3) substituents that may be the same or different, and which are selected from the group consisting of halogen, hydroxyl, cyano, nitro, oxo, haloalkyl C1-6, polyhaloalkyl C1- 6, C1-6 haloalkoxy, C1-6 polyhaloalkoxy, C1-6 alkyl, C1-6 alkoxy, C1-6 alkylthio, C1-6 alkoxy-C1-6 alkyl, C3-7 cycloalkyl-C1-6 alkoxy, C1- alkanoyl 6, C1-6 alkoxycarbonyl, C1-6 alkyl sulfonyl, alk C1-6-sulfinyl, C1-6-sulfonyloxy alkyl, C1-6-alkyl-sulfonylalkyl- C1-6 alkyl, C1-6-sulfonamidoalkyl C1-6, alkyl C1-6-amidoalkyl C1-6, arylsulfonyl, arylsulfonyloxy, aryloxy, arylsulfonamido, arylcarboxamido, aroyl, or a group NR15R16, -CONR15R16, -NR15COR16, -NR15SO2R16 or -SO2NR15R16, in which R15 and R16 independently represent hydrogen or C1-6 alkyl or together form a heterocyclic ring; X represents a bond, O, CO, OCH2, CH2O or SO2; Z represents CO, CONR10 or SO2; R 10 represents hydrogen, C 1-6 alkyl, C 3-8 cycloalkyl, aryl, heterocyclyl, heteroaryl; represents a single or double bond; m and n independently represent 0, 1 or 2; R2 represents hydrogen, C1-6 alkyl or C1-6 alkoxy; R3 represents halogen, C1-6 alkyl, hydroxyl, C1-6 alkoxy, cyano, amino, -CO-C1-6 alkyl, -SO2-C1-6 alkyl or trifluoromethyl; R4 represents - (CH2) q-NR11R12 or a group of formula (i): in which q represents 3 or 4; -NR11R12 represents a heterocyclic group, optionally substituted with one or more R17 groups; R13 represents C1-6 alkyl; C3-8 cycloalkyl, -C 1-6 alkyl-C 1-6 alkoxy, -C 1-6 alkyl-C 3-8 cycloalkyl; R14 and R17 independently represent halogen, C1-6 alkyl, haloalkyl, OH or C1-6 alkoxy; f is 0 or 1; g is 1 or 2; k is 0, 1 or 2; or a pharmaceutically acceptable salt thereof.
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