1-PHENYLALKANONES ARE NEW 5-HT RECEPTOR LIGANDS Russian patent published in 2001 - IPC

FIELD: 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