| 摘要 |
pharmaceutical industry. SUBSTANCE: described are 1- phenylalkanones which are new 5-HT4- receptors ligands of formula I: wherein R1 is halogen; R2 is H and C1-C4 alkoxy; R3 is C1-C4- alkoxy, phenyl C1-C4 alkoxy wherein phenyl is optically substituted by 1-3 substituents independently selected from C1-C4 alkyl, C1-C4 alkoxy, 3,4- methylenedioxy; R2 and R3 together are methylenedioxy and ethylenedioxy; R4 is group of formula (a): or (b): wherein n= 3,4,5; p=0; q=1 or 2; R5 and R6 is each C1-C4, alkyl or together wherein R8 and R11 each is H or together (CH2)t- wherein t=1; R9 is H, OH, C1-C8 alkyl and C1-C4 alkyloxy; R10 is H, C1-C8 alkyl, phenyl, (CH2)xR12 wherein x=0,1,2,3; R12 is OH, C1-C4 alkyloxy, C(O)NR13R14,, NR13C(O)OR14,, SO2NR13R14, NR13SO2R14,, -NR13SO2NR14R15,; NR13C(O)NR14R15; R13, R14, R15 are independently H, C1-C4 alkyl, CF3; R7 is H, C1-C8 alkyl, C3-C8 alkenyl, phenyl C1-C4 alkyl wherein phenyl is optionally substituted by C1-C4 alkyloxy, methylenedioxy and ethylenedioxy; or R7 is (CH2)z-R12 wherein z=2 or 3. Compounds I are new 5-HT4-receptor ligands, and this makes it possible to use them in pharmaceutical composition and in method of treating states selected from central nervous system disorders, disorders of gastrointestinal tract, cardiovascular system and urinary tracts. EFFECT: improved properties of the title compounds. 39 cl, 23 ex
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