β-LACTAMS, METHOD FOR PREPARING INDICATED COMPOUNDS AND SERUM HYPOCHOLESTEROLEMIC AGENTS CONTAINING SUCH COMPOUNDS Russian patent published in 2007 - IPC C07D205/08 C07D405/10 A61K31/351 A61P3/06

Abstract RU 2301799 C2

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to novel compounds of the formula (I): wherein A₁ means hydrogen atom (H), halogen atom, (C₁-C₅)-alkyl, group of the formula (a): ; A₂ means (C₁-C₅)-alkyl, (C₁-C₅)-alkoxyl chain, (C₁-C₅)-alkenyl, hydroxy-(C₁-C₅)-alkyl, carbonyl-(C₁-C₅)-alkyl; A₃ means halogen atom or group of the formula (a); A₄ means (C₁-C₅)-alkyl, H, halogen atom, -COOR₁, (C₁-C₅)-alkoxy-group, group of the formulae (a) and (b): wherein R₁ means hydrogen atom, (C₁-C₅)-alkyl; R₂ means -CH₂OH, -COOR₁; R₃ means -OH, -OC(O)-R₁; R₄ means -(CH₂)_k-R₅(CH₂)_l-; R₅ means a simple bond (-), -CH=CH-, -OCH₂-, carbonyl group or -CH(OH)-, and R₄ is bound with tetrahydropyrane ring by the carbon-carbon bond; k and l = 0, 1 or a whole number above 1; k + l = 10 or lesser number; n = 0 or 1; p, g, r = 0 being one value among A₁, A₃ and A₄ in the formula (I) must represent group of the formula (a), or to their pharmaceutically acceptable salts. Also, invention describes method for synthesis of proposed compounds. Proposed compounds of the formula (I) can be used as hypocholesterolemic agents for decreasing the serum blood cholesterol level.

EFFECT: valuable medicinal properties of compounds and pharmaceutical composition, improved method of synthesis.

5 cl, 3 tbl, 35 ex

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RU 2 301 799 C2

Authors

Tomijama Khirosi

Jokota Masajuki

Noda Atsusi

Okhno Akira

Dates

2007-06-27—Published

2002-02-20—Filed