The invention relates to novel compounds that are derivatives of 1,4-benzodiazepin-2-one, having the general formula I: and being limited to structural variants 1-6: on condition that: a) structures 1 (R1=Br, R4=F), 3 (R1=OCF3, R4=H), 5 (R1=NO2, R4=Cl) and 6 (R1=NO2, R4=F) have the following substituents R2 and R3: R2=H, CH2COCH3, CH2COOCH3, CH2CONHNH2; R3=OAlk, NHAr, where Alk=C2H5, C3H7, C4H9, (CH2)2OH, (CH2)2OCH3, R5=o-, m-, p-COCH3, Cl, F, Br, NO2, CF3; b) structure 2 (R1=Cl, R4=H) has the following substituents R2 and R3: if R2=H, then R3=OAlk, NHAr, where Alk=(CH2)2OCH3, R5=m-, p-COCH3, o-, m-, p-F, Br, CF3;  if R2=CH2COCH3, CH2COOCH3, CH2CONHNH2, then R3=OAlk, NHAr, where Alk=C2H5, C3H7, C4H9, (CH2)2OH, (CH2)2OCH3, R5=o-, m-, p-COCH3, Cl, F, Br, NO2, CF3; c) structure 4 (R1=NO2, R4=H) has the following substituents R2 and R3: if R2=H, then R3=OAlk, NHAr, where Alk=(CH2)2OCH3, R5=o-, m-, p-COCH3, Cl, F, Br, NO2, CF3;  if R2=CH2COCH3, CH2COOCH3, CH2CONHNH2, then R3=OAlk, NHAr, where Alk=C2H5, C3H7, C4H9, (CH2)2OH, (CH2)2OCH3, R5=o-, m-, p-COCH3, Cl, F, Br, NO2, CF3 and the use of said compounds in the field of medicine as analgesics, anorexigenic or orexigenic agents for weight regulation (loss or gain), antidepressants and anxiolytics for treating psychological disorders, and also antihypoxic and nootropic agents for the prophylaxis and treatment of central nervous system disorders.