Disubstituted polycyclic systems as cognition enhancers

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 471/04 (2006.01) A61K 31/435 (2006.01) A61K 31/495 (2006.01) C07D 213/04 (2006.01) C07D 213/06 (2006.01) C07D 213/16 (2006.01) C07D 213/30 (2006.01) C07D 213/40 (2006.01) C07D 213/42 (2006.01) C07D 213/53 (2006.01) C07D 213/55 (2006.01) C07D 213/56 (2006.01) C07D 213/57 (2006.01) C07D 237/08 (2006.01) C07D 239/26 (2006.01) C07D 401/06 (2006.01)

Patent

CA 2128234

2128234 9314092 PCTABS00024 Compounds of formula (I) have been shown to enhance the release of the neurotransmitter acetylcholine, and thus may be useful in the treatment of diseases of man, such as in Alzheimer's disease and other conditions involving learning and cognition, where subnormal levels of this neurochemical are found. The compounds of this invention can be described as shown in formula (I), where Q is (II), (III) and (IV); R1 is 4-, 3-, or 2-pyridyl, pyrimidyl, pyrazinyl, or fluoro-4-pyridyl; R2 and R3 are independently H, F, Cl, Br, NO2, OH, -R4, -O-R4, -CO2R4, -COR4, -CONH2, -CONHR4, -CONR4R4', -S(O)m2-R4, NH2, CF3, NHR4, NR4R4'; R4 and R4' are independently H, alkyl of 1 to 4 carbons, CH2Phe-W or Phe-W; Phe is a phenyl group; R5 is -(CH2)n-Y or -OCOR4; Y is H, OH, NH2, NHR4, NR4R4', NHCOR4, NHCO2R4, NHS(O)2R4; F, Cl, Br, OR4, S(O)mR4, -CO2H, -CO2R4, -CN, -CONR4R4', -CONHR4, -CONH2, -COR4; -CH=CHCO2R4, -OCOR4, Phe, Phe-W, -C=CCO2R4, -CH=CHR4, or -C=C-R4; W is F, Cl, Br, R4, OR4, NO2, NH2, NHR4, NR4R4, CN, S(O)m-R4; m is 0, 1 or 2; n is 1 to 7; and hydrates and physiologically suitable salts thereof.

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