DERIVATIVES OF β--AMINO--α--HYDROXYCARBOXYLIC ACIDS OR THEIR PHARMACEUTICALLY ACCEPTABLE SALTS OR ESTERS, PHARMACEUTICAL COMPOSITION Russian patent published in 1998 - IPC

Abstract RU 2120447 C1

FIELD: organic chemistry. SUBSTANCE: invention relates to derivatives of β--amino--α--hydroxycarboxylic acids of the general formula (I): β- where -α- being A is -CO, R1-NR2-CH(R3)CONHCHR4CHOHCOR5,; Z is O; X = 0 or 1; R is RI=R(Z)xA,-alkyl that can be optionally substituted with phenyl or phenoxy-group, carbocyclic aryl-group containing up to 10 carbon atoms, 5-6-membered heterocyclic group containing from 1 to 4 heteroatoms taken from nitrogen, oxygen, sulfur being heterocyclic group can be fused with benzene nucleus and can be free or substituted with at least one substituent taken from hydroxy-, -SO2,-alkyl, C1-C6-alkoxy, (C1-C6)-alkoxyphenyl, (C1-C6) or R is (C1-C6); H2NCH2COO-, CH3COO- and NRaRb, are taken independently from hydrogen and Ra-aryl, Rb-substituted; (C6-C14) is H; (C1-C3) is hydrogen, R2-alkyl that can be substituted with hydroxyl, carbamoyl, cyano-group, carboxy-group, mono-R3- or di-(C1-C6)-alkylcarbamoyl; (C1-C6) is (C1-C6)-alkyl substituted with phenyl or cyclohexyl; R4 is 5-10-membered heterocyclic system or their pharmaceutically acceptable salts, or esters and pharmaceutical composition based on thereof. The synthesized compounds are used in medicine, for treatment of patients with retroviral infections, in part, with AIDS. EFFECT: improved method of synthesis, enhanced effectiveness of compounds. 19 cl, 1 tbl

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RU 2 120 447 C1

Authors

Juitiro Jabe

Mitsuja Sakurai

Susumu Khigasida

Tomoaki Komai

Takasi Nisigaki

Khirosi Khanda

Dates

1998-10-20Published

1992-02-07Filed