| 摘要 |
organic chemistry, pharmacy. SUBSTANCE: invention describes novel derivatives of arylglycineamides of the general formula (I) or their pharmaceutically acceptable salts where Ar means unsubstituted phenyl or phenyl substituted with from 1 to five substituents, or naphthyl substituted with from to two substituents being substituents of phenyl and naphthyl moiety mean independently halogen atoms (fluorine, chlorine, bromine, iodine), hydroxyl group, alkyl with number of carbon atom from one to four, alkoxyl with number of carbon atoms from one to four, trifluoromethyl, trifluoromethoxyl group or the group NR9R10 where R9 and R10 means hydrogen atom, methyl independently each of other; Ar can mean also phenyl substituted with -O(CH2)O- or -O(CH2)O- group; R1 and R2 in common with nitrogen atom to which they are bound form cycle: where p = 2 or 3; X means the group N(CH2)nR6 or CR7R8 where n = 0, 1 or 2; R6 means cycloalkyl with number of carbon atoms from three to seven, phenyl or naphthyl being phenyl can be substituted with from one to three substituents as halogen atom (fluorine, chlorine, bromine, iodine); R7 and R8 have one of the following value: a) R7 and R8 mean hydrogen atom if R3 means phenyl; b) R7 means phenyl, piperidinyl, 1-methylpiperidinyl or groups of the following formulas (a) when R8 means hydrogen atom, carbamoyl, acetylamine, acetyl-N-methylamine or nitrile; c) R7 and R8 in common form residue (b) ; R3 means hydrogen atom or phenyl; R4 means phenylalkyl or naphthylalkyl with number of carbon atoms in alkyl moieties from one to four being phenyl can be substituted with from one to three substituents as halogen atoms (fluorine, chlorine, bromine, iodine), alkyl with number of carbon atoms from one to four, alkoxyl group with number of carbon atoms from one to four or trifluoromethyl group; R5 means hydrogen atom, alkyl with number of carbon atoms from one to four, cycloalkyl with number of carbon atoms from three to six, carboxymethyl or carbamoylmethyl. Compounds show activity of neurokinin antagonist. Invention describes pharmaceutical composition containing these compounds also. EFFECT: new compounds, valuable pharmacological properties. 18 cl
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