PHARMACEUTICAL AGENT CONTAINING INHIBITOR OF SODIUM-DEPENDENT PHOSPHATE CARRIER Russian patent published in 2020 - IPC C07D237/04 C07D401/06 C07D401/12 C07D403/12 C07D403/14 C07D405/14 C07D413/14 C07D471/04 C07D487/04 C07D487/08 A61K31/50 A61K31/4545 A61K31/495 A61K31/501 A61K31/5025 A61K31/503 A61K31/506 A61K31/537 A61K31/5377 A61K45/00 A61P3/14 A61P5/18 A61P9/10 A61P13/12 

FIELD: pharmaceuticals.

SUBSTANCE: invention relates to a pharmaceutical composition for inhibiting one or more vectors selected from NaPi-IIb, PiT-1 and PiT-2, containing an active ingredient dihydropyridazine-3,5-dione of formula (I)

,

in which R¹, R⁴ and R⁵ are as defined in any of the following paragraphs from (1) or ( 2): (1) R¹ denotes a hydrogen atom, methyl or ethyl; R⁴ denotes a hydrogen atom, C₁-C₄-alkyl optionally substituted with one or more fluorine atoms, or phenyl; and R⁵ denotes C₁-C₄-alkyl; (2) R¹ and R⁵ together with the carbon atom to which they are bonded form C₄-C₆-saturated carbocyclic ring; and R⁴ denotes methyl; and R³ is C₃, C₅, C₆ or C₈-alkyl, optionally substituted with one or more Rh substituents, or R³ denotes methyl substituted with Re; each Rh is independently selected from a fluorine atom, (ethoxy)-carbonyl group and -(OCH₂ CH₂)₂-OCH₃; Re denotes phenyl, optionally substituted with one or more substituents Ra, or indolyl, optionally substituted with one or more substituents Ra; each Ra is independently selected from a group comprising a halogen atom, a hydroxy group, a nitro group, a cyano group, methoxycarbonyl, oxetanyloxy, tetrahydropyranyloxy, methoxyethylpirrolidinyloxy, methoxyethylazetidinyloxy, methylpiperidinyloxy, C₁, C₃, C₆ and C₇ alkyl optionally substituted with one or more substituents R¹⁰, C₂-C₇-alkynyl, optionally substituted by one or more substituents R¹¹, C₁-C₆-alkoxy group, optionally substituted with one or more substitutes R¹², ethylthio group, optionally substituted with one or more substitutes R¹³, group -(O(CH₂)_q1)_q2-NR⁴¹R⁴² (where q1 is an integer, equal to 1 to 4, and q2 is an integer of from 2 to 6), a group -(O(CH₂)_r1)_r2-C(O)NR⁴³R⁴⁴ (wherein r1 is an integer of from 1 to 4 and r2 is an integer, equal to 1 to 4), group -(O(CH₂)_s1)_s2^_NR⁴⁵-C(O)R⁴⁶ (where s1 and s2 are each independently integer from 2 to 4), -C(O)N(CH₃)-(CH₂)₃OCH₃ group, pyridinyl, pyrrolyl and -NR⁴⁹R⁵⁰Ar¹ group denotes phenyl, furyl, pyridinyl or pyrimidinyl, wherein phenyl, furyl, pyridinyl or pyrimidinyl groups each are optionally substituted with 1–3 substitutes independently selected from Rb, Rc and Rd; values of remaining radicals are presented in claim 1.

EFFECT: what is offered is a pharmaceutical agent containing a sodium-dependent phosphate carrier inhibitor.

37 cl, 45 tbl, 457 ex