| abstract |
These compounds are useful for treating conditions or disorders that can be prevented or improved by histamine-3 receptor ligands. Pharmaceutical compositions comprising histamine-3 receptor ligands and therapeutic treatment methods are also disclosed: attention disorders, memory and learning deficits, schizophrenia, Alzheimer's, epilepsy, mild cognitive impairment. Claim 1: A compound characterized in that it responds to formula (1) or a salt acceptable for pharmaceutical, ester, amide or prodrug use thereof, wherein: one of R1 and R2 is a group of the formula -L2-R6a-L3 -R6b; the other of R1 and R2 is selected from the group consisting of hydrogen, alkyl, alkoxy, halogen, cyano, and thioalkoxy; R3, R3a, and R3b are each independently selected from the group consisting of hydrogen, alkyl, trifluoroalkyl, trifluoroalkoxy, alkoxy, halogen, cyano, and thioalkoxy; R4 and R5 are each independently selected from the group consisting of alkyl, fluoroalkyl, hydroxyalkyl, alkoxyalkyl, and cycloalkyl, or R4 and R5 taken together with the nitrogen atom to which each is attached form a non-aromatic ring of the formula (2) or (3); R7, R8, R9, and R10 each time each is independently selected from the group consisting of hydrogen, hydroxyalkyl, fluoroalkyl, cycloalkyl, and alkyl; R11, R12, R13, and R14 are each independently selected from the group consisting of hydrogen, hydroxyalkyl, alkyl, and fluoroalkyl; R6a is selected from the group consisting of a 5 or 6 membered heteroaryl ring, cyanophenyl, an 8 to 12 membered bicyclic heteroaryl ring, and a 4 to 12 membered heterocyclic ring; R6b is selected from the group consisting of hydrogen, a 5- or 6-membered heteroaryl ring, an aryl ring, an 8 to 12 membered bicyclic heteroaryl ring, and a 4 to 12 membered heterocyclic ring; Q is O or S; L is - [C (R16) (R17)] k; L2 is selected from the group consisting of a union, alkylene, -O-, -C (= O) -, -S-, -NH-, -N (R16) C (= O) -, -C (= O) N (R16), and -N (alkyl) -; L3 is selected from the group consisting of a union, alkylene, -O-, -C (= O) -, -S-, -N (R16) C (= O) -, -C (= O) N ( R16), and -N (R15) -; R15 is selected from the group consisting of hydrogen, alkyl, acyl, alkoxycarbonyl, amido, and formyl; R16 and R17 on each occasion are independently selected from the group consisting of hydrogen and alkyl; Rx and Ry are each independently selected from the group consisting of hydrogen, hydroxy, hydroxyalkyl, alkyl, alkoxy, alkylamino, fluoro, and dialkylamino; k is 1, 2 or 3; and m is an integer from 1 to 5. |