AMINOBENZOPHENONES AS INHIBITORS OF IL-1-BETA AND TNF-ALPHA Russian patent published in 2004 - IPC

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to compounds of the general formula (I):

wherein R₁ means independently one or some similar or different substituents taken among the group consisting of halogen atom, (C₁-C₃)-alkyl, (C₁-C₃)-alkoxy-group under condition that when R₁ means one substituent then it is in the ortho-position; when R₁ means more one substituents then at least one substituent R₁ is in the ortho-position; R₂ means one substituent in the ortho-position being indicated substituent is taken among the group consisting of halogen atom, (C₁-C₃)-alkoxy-group; R₃ means halogen atom; R₄ means hydrogen atom; X means oxygen atom, and to its salt with pharmaceutically acceptable acid, or their hydrate, or solvate. Invention proposes a method for preparing compound of the formula (I) comprising the coupling reaction of amine of the formula (II) with acid of the formula (III) given in the invention claim or its activated derivative, especially, trifluoroacetic anhydride. Invention proposes a pharmaceutical composition eliciting inhibitory activity with respect to secretion of 1β-interleukin, α-factor of tumor necrosis of cells and polymorphous nuclear superoxide containing aminobenzophenones of the formula (I) as an active component in common with pharmaceutically acceptable carrier and, optionally, in common with the second active component taken optionally among the group comprising glucocorticoids, vitamins D, antihistaminic agents, antagonists of platelet activation factor, anticholinergic agents, methylxanthines, β-adrenergic agents, salicylates, indometacin, fluphenamate, naproxen, timegadin, gold salts, penicillamine, agents reducing serum blood cholesterol level, retinoids, zinc salts and salicylazosulfapyridine (salazopyrine). Also, invention proposes a pharmaceutical composition for treatment and/or prophylaxis of asthma, allergy, arthritis including rheumatic arthritis and spondyloarthritis, gout, atherosclerosis, intestine chronic inflammation (Crohn's disease), skin proliferative and inflammatory diseases, such as psoriasis, atopic dermatitis, uveitis, septic shock, AIDS, osteoporosis and acne containing aminobenzophenones of the formula (I) as an active component in common with a pharmaceutically acceptable carrier and, optionally, in common with the second active component.

EFFECT: valuable medicinal properties of compounds.

10 cl, 2 tbl, 16 ex