4-AMINOPIPERIDINE DERIVATIVES, METHODS FOR THEIR PREPARING, COMPOUNDS, PHARMACEUTICAL COMPOSITION Russian patent published in 2005 - IPC

FIELD: organic chemistry, chemical technology, medicine, pharmacy.

SUBSTANCE: invention relates to new derivatives of 4-aminopiptidine of the general formula (I): wherein R₁ means (C₁-C₆)-alkyl, -(CH₂)_m-Y-Z₁₁ or -(CH₂)_m-Z₁₂ wherein Z₁₁ means (C₁-C₆)-alkyl; Z₁₂ means bis-phenyl, (C₃-C₇)-cycloalkyl, (C₃-C₇)-heterocycloalkyl with 1 or 2 heteroatoms taken among nitrogen (N) or oxygen (O) atoms, possibly substituted phenyl, naphthyl, possibly substituted (C₅-C₉)-heteroaryl wherein heteroatoms are taken among N; or Z₁₂ means ; Y means O; or R₁ means ; R₂ means -C(Y)-NHX₁, -C(O)X₂ or -SO₂X₃; R₃ means hydrogen atom (H), (C₁-C₄)-alkyl, (C₂-C₄)-alkenyl, possibly substituted heteroarylalkyl or -C(Y)-NHX₁, -(CH₂)_n-C(O)X₂ or -SO₂X₃ wherein X₁-X₃ have different values. Also, invention describes methods for preparing indicated substances by synthesis in liquid and solid phase. These compounds possessing good affinity to definite subtypes of somatostatin receptors can be used in treatment of pathological states or diseases caused by one or some somatostatin receptors.

EFFECT: improved preparing method, valuable medicinal properties of compounds.

14 cl, 4 tbl, 778 ex