.alpha.- and .beta.-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
대표청구항▼
1. A compound represented by the formula (A): [EQU470]or a pharmaceutically acceptable salt, or ester thereof, wherein:R2 is an alkyl, aryl, cycloalkyl, cycloalkylalkyl or aralkyl radical, which radical is optionally substituted with a radical selected from the group consisting of alkyl, halo, nitro
1. A compound represented by the formula (A): [EQU470]or a pharmaceutically acceptable salt, or ester thereof, wherein:R2 is an alkyl, aryl, cycloalkyl, cycloalkylalkyl or aralkyl radical, which radical is optionally substituted with a radical selected from the group consisting of alkyl, halo, nitro, cyano, CF3, -OR9, and -SR9, wherein R9 is a radical selected from the group consisting of hydrogen and alkyl; R3 is a hydrogen, alkyl haloalkyl, alkenyl, alkynyl, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkylsulfonylalkyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, aminoalkyl or mono- or disubstituted aminoalkyl radicals, wherein said substituents are selected from the group consisting of alkyl, aryl, aralkyl, cycloalkyl and cycloalkylalkyl radicals; R4 is an alkyl, haloalkyl, alkenyl, alkynyl, hydroxyalkyl, alkoxyalkyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, aralkenyl, aminoalkyl or mono- or disubstituted aminoalkyl radical, wherein said substituents are selected from the group consisting of alkyl, aryl, aralkyl, cycloalkyl and cycloalkylalkyl radicals; R6 is a hydrogen or alkyl radical; x is 1 or 2; Y is 0 or S; and A is an alkoxy, alkenoxy, aralkoxy, alkyl, cycloalkyl, cycloalkylalkoxy, [EQU471]cycloalkylalkyl, aralkyl, aryl, aryloxy, alkenyl, aryloxyalkyl, hydroxyalkyl, amino, or mono- or disubstituted amino radical, wherein the substituents are selected from the group consisting of alkyl, aryl, aralkyl, cycloalkyl and cycloalkylalkyl radicals; or is represented by the formula (B): [EQU472]t is 0or 1; wherein R is a hydrogen, alkoxycarbonyl, aralkoxycarbonyl, alkylcarbonyl, cycloalkylcarbonyl, cycloalkylalkoxycarbonyl, cycloalkylalkanoyl, carboxyalkanoyl, alkanoyl, aralkanoyl, aroyl, aryloxycarbonyl, aryloxycarbonylalkyl, aryloxyalkanoyl, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, aralkyl, aryloxyalkyl, hydroxyalkyl, aminocarbonyl, aminoalkanoyl, or mono- or disubstituted aminocarbonyl or mon- or disubstituted aminoalkanoyl radical, wherein the substituents are selected from the group consisting of alkyl, aryl, aralkyl, cycloalkyl and cycloalkylalkyl radicals; R' is a radical as defined for R3 or R′SO2-, wherein R′ is a radical as defined for R3; R1 is a hydrogen, -CO2CH3, -CH2CO2CH3, -CO2H, -CH2CO2H, -CH2CH2CONH2, -CH2CONH2, -CONH2, -CH2C(O)NHCH3, -CH2C(O)N(CH3)2, -CONHCH3, -CONH(CH3)2, -CH2SO2NH2, -CH2CH2SO2NH2, -CH2S(O)CH3, -CH2S(O)2CH3, -C(CH3)2(S(O)CH3), -C(CH3)2(S(O)2CH3), alkyl, hydroxyalkyl, cyanoalkyl, haloalkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, alkylthioalkyl, aralkyl, aminoalkyl or mono- or disubstituted aminoalkyl radical, wherein said substituents are selected from the group consisting of alkyl, aryl, aralkyl, cycloalkyl and cycloalkylalkyl radicals; and each of R1' and R1′ are independently a radical as defined for R1; or one of R1' and R1′ together with R1 and the carbon atoms to which R1, R1' and R1′ are attached, form a cycloalkyl radical.
Rosenberg Saul H. (Libertyville IL) Luly Jay R. (Libertyville IL) Plattner Jacob J. (Libertyville IL), Functionalized peptidyl aminodiols and -triols 4-amino-5-cyclohexyl-3-hydroxy-1,2-oxopentane and derivatives thereof.
Gordon Eric M. (Pennington NJ) Godfrey ; Jr. Jollie D. (Lawrenceville NJ) Natarajan Sesha I. (Neshanic Station NJ), Hydroxy substituted peptide compounds.
Luly Jay R. (Libertyville IL) Dellaria Joseph (Lindenhurst IL) Fung Anthony K. L. (Waukegan IL) Kempf Dale J. (Lake Villa IL) Plattner Jacob J. (Libertyville IL) Rosenberg Saul H. (Libertyville IL) S, Renin inhibiting compounds.
Vazquez, Michael L.; Mueller, Richard A.; Talley, John J.; Getman, Daniel P.; DeCrescenzo, Gary A.; Freskos, John N.; Heintz, Robert M.; Bertenshaw, Deborah E., α- and β- amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors.
Vazquez, Michael L.; Mueller, Richard A.; Talley, John J.; Getman, Daniel P.; DeCrescenzo, Gary A.; Freskos, John N.; Bertenshaw, Deborah E.; Heintz, Robert M., α- and β-amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors.
Vazquez, Michael L.; Mueller, Richard A.; Talley, John J.; Getman, Daniel P.; DeCrescenzo, Gary A.; Freskos, John N.; Bertenshaw, Deborah E.; Heintz, Robert M., α- and β-amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors.
Vazquez, Michael L.; Mueller, Richard A.; Talley, John J.; Getman, Daniel P.; DeCrescenzo, Gary A.; Freskos, John N.; Heintz, Robert M.; Bertenshaw, Deborah E., α- and β-amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors.
Vazquez, Michael L.; Mueller, Richard A.; Talley, John J.; Getman, Daniel P.; DeCrescenzo, Gary A.; Freskos, John N.; Heintz, Robert M.; Bertenshaw, Deborah E., α- and β-amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors.
Vazquez, Michael L.; Mueller, Richard A.; Talley, John J.; Getman, Daniel P.; DeCrescenzo, Gary A.; Freskos, John N.; Bertenshaw, Deborah E.; Heintz, Robert M., α-and β-Amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors.
※ AI-Helper는 부적절한 답변을 할 수 있습니다.