DERIVATIVE OF TRIAZASPIRO5,5UNDECANE AND PHARMACEUTICAL COMPOSITION COMPRISING ITS AS ACTIVE COMPONENT

摘要

FIELD: organic chemistry, medicine, pharmacy.;SUBSTANCE: invention relates to derivative of triazaspiro[5.5]undecane of the formula (I): wherein R¹ means compound of the formula (1): or (2): wherein G represents a bond, (C₁-C₄)-alkylene, (C₂-C₄)-alkenylene or -CO-; ring A represents: (1) C5-10-membered mono- or bicarbocyclic ring or (2) 5-10-membered mono- or bicyclic heterocycle comprising 1-2 nitrogen atoms and/or 1-2 oxygen atoms; substitute R⁶ means the following values: (1) (C₁-C₄)-alkyl, (2) halogen atom, (3) nitrile group, (4) trifluoromethyl group and others; R² represents: (1) (C₁-C₄)-alkyl, (2) (C₂-C₄)alkynyl or (3) (C₁-C₄)-alkyl substituted with a substitute represented in claim 1 of the invention claim; each R³ and R⁴ represents independently: (1) hydrogen atom, (2) (C₁-C₄)-alkyl or (3) (C₁-C₄)-alkyl substituted with 1-2 substituted taken among: (a) Cyc 2 and (b) hydroxy-group (wherein Cyc 2 represents (1) C5-6-membered monocarbocyclic ring or (2) 5-6-membered monocyclic heterocycle comprising 1-2 nitrogen atoms and/or one oxygen atom), or R³ and R⁴ form in common group of the formula: wherein R²⁶ represents (C₁-C₄)-alkyl or Cyc 2; R⁵ represents hydrogen atom or (C₁-C₄)-alkyl, its quaternary ammonium salt, its N-oxide or its nontoxic salt. Also, invention relates to pharmaceutical composition inhibiting HIV, regulator of chemokine/chemokine receptor and agent used in treatment and prophylaxis of some diseases, such as inflammatory diseases, asthma, atopic dermatitis, nettle rash, allergic diseases, nephritis, hepatitis, arthritis and other diseases that comprise as an active component above described compound of the formula (I) or its quaternary ammonium salt, its N-oxide or its nontoxic salt. Also, invention relates to (3R)-1-butyl-2,5-dioxo-3-((1R)-1-hydroxy-1-cyclohexylmethyl)-9-(4-(4-carboxyphenyloxy)phenylmethyl)-1,4,9-triazaspiro[5.5]undecane or its pharmaceutically acceptable salt and pharmaceutical composition based on thereof, and to (3R)-1-butyl-2,5-dioxo-3-((1R)-1-hydroxy-1-cyclohexylmethyl)-9-(4-(4-carboxyphenyloxy)phenylmethyl)-1,4,9-triazaspiro[5.5]undecane hydrochloride and pharmaceutical composition based on thereof.;EFFECT: valuable medicinal properties of derivative and composition.;16 cl, 32 ex