CONTROLLED RELEASE OF PHENOL OPIATE Russian patent published in 2012 - IPC C07D489/02 A61K47/48 A61K38/05 A61P25/04 

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention declares a compound of structural formula (I) or its pharmaceutically acceptable salt, solvate or hydrate wherein: X is phenol opiate wherein a hydrogen atom of a hydroxyl phenol group of substituted by a covalent bond with -C(O)-Y-(C(R¹)(R²))_n-N-C(R³)(R⁴);Y is -NR⁵-, R⁵ is (C_1-6)alkyl; n is equal to 2 or 3, each of R¹ and R² is independently hydrogen, alkyl or substituted alkyl; R³ is hydrogen or methyl; R⁴ is a residue of L-amino acid or a residue of their N-acyl derivatives, as well as Hydromorphone 3-(N-methyl-N-(2-N'-acetylarginine amino)ethyl carbamate, or their pharmaceutically acceptable salt. What is also specified is a method for preparing the compound of formula (I) or its pharmaceutically acceptable salt.

EFFECT: what is declared is a pharmaceutical composition controlling phenol opiate release and a method of pain management in a patient in need thereof involving the introduction of an effective amount of the composition.

19 cl, 20 ex, 12 tbl