SIGMA LIGANDS FOR POTENTIATING ANALGESIC EFFECT OF OPIOIDS AND OPIATES IN POSTOPERATIVE PAIN AND ATTENUATING DEPENDENCY THEREOF Russian patent published in 2015 - IPC A61K31/4155 A61K31/5377 A61P25/04

Abstract RU 2563460 C2

FIELD: chemistry.

SUBSTANCE: invention relates to simultaneous, separate or sequential administration of a combination, comprising at least one sigma ligand of formula

at least one opioid or opiate compound selected from the group consisting of morphine, tramadol, sufentanil, remifentanil, fentanyl, tapentadol, oxycodone, buprenorphine for use in the prevention and/or treatment of pain developed as a consequence of surgery. In formula (I) R₁ is selected from the group formed by hydrogen, unsubstituted C₁-C₈alkyl and -COR₈; R₂ is selected from the group formed by hydrogen, unsubstituted C₁-C₈alkyl and unsubstituted phenyl; R₃ and R₄ are independently selected from the group formed by hydrogen, unsubstituted C₁-C₈alkyl, unsubstituted phenyl, unsubstituted C₆-C₁₈aryl C₁-C₈alkyl, -OR₈ and halogen; or together they form an optionally substituted fused ring system; n is selected from 2, 3 or 4; R₈ is an unsubstituted C₁-C₈alkyl; R₅ and R₆are given in the claims.

EFFECT: invention also refers to the sigma ligand of formula (I) for use in potentiating the analgesic effects of an opioid or opiate.

10 cl, 12 dwg, 2 ex

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RU 2 563 460 C2

Authors

Vela Ehrnandes Khose Migel'

Samanil'O-Kastanedo Daniehl'

Dates

2015-09-20—Published

2011-02-04—Filed