Methods for increasing levels of acetylcholine

A method for increasing the levels of acetylcholine in the frontal cortex and/or hippocampus regions of the brain in mammals comprising administering to a mammal in need thereof, an effective amount of a compound of formula I:

• 4
• wherein
• either R1 is H or a lower alkyl radical and R2 is a lower alkyl radical, or R1 and R2 are joined together with the adjacent nitrogen atom to form a heterocyclic radical;
• R3 is H or a lower alkyl radical;
• R4 is H, halo, OH, a lower alkyl radical, or is a buta-1,3-dienyl radical which together with the adjacent benzene ring forms a naphthyl radical;
• R5 is H or OH;
• and
• n is 2;
• or a pharmaceutically acceptable salt thereof and optionally an AChE inhibitor.

A method for inhibiting conditions or detrimental effects caused by a deficiency of choline acetyltransferase and/or acetylcholine in the frontal cortex and/or hippocampus regions of the brain in mammals comprising administering to a mammal in need thereof, an effective amount of a compound of formula I:

• 5
• wherein
• either R1 is H or a lower alkyl radical and R2 is a lower alkyl radical, or R1 and R2 are joined together with the adjacent nitrogen atom to form a heterocyclic radical;
• R3 is H or a lower alkyl radical;
• R4 is H, halo, OH, a lower alkyl radical, or is a buta-1,3-dienyl radical which together with the adjacent benzene ring forms a naphthyl radical;
• R5 is H or OH;
• and
• n is 2;
• or a pharmaceutically acceptable salt thereof and optionally an AChE inhibitor.

A pharmaceutical formulation comprising a compound of formula I:

• 6
• wherein
• either R1 is H or a lower alkyl radical and R2 is a lower alkyl radical, or R1 and R2 are joined together with the adjacent nitrogen atom to form a heterocyclic radical;
• R3 is H or a lower alkyl radical;
• R4 is H, halo, OH, a lower alkyl radical, or is a buta-1,3-dienyl radical which together with the adjacent benzene ring forms a naphthyl radical;
• R5 is H or OH;
• and
• n is 2;
• or a pharmaceutically acceptable salt thereof;
• an AChE inhibitor;
• and a pharmaceutical carrier, diluent, or excipient.