.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: [EQU362]or a pharmaceutically acceptable salt, prodrug, or ester thereof wherein:P1 represents alkoxycarbonyl, aralkoxycarbonyl, alkylcarbonyl, cycloalkylcarbonyl, cycloalkylalkoxycarbonyl, cycloalkylalkanoyl, alkanoyl, aralkanoyl, aroyl, aryloxycarbonyl, ar
1. A compound represented by the formula: [EQU362]or a pharmaceutically acceptable salt, prodrug, or ester thereof wherein:P1 represents alkoxycarbonyl, aralkoxycarbonyl, alkylcarbonyl, cycloalkylcarbonyl, cycloalkylalkoxycarbonyl, cycloalkylalkanoyl, alkanoyl, aralkanoyl, aroyl, aryloxycarbonyl, aryloxycarbonylalkyl, aryloxyalkanoyl, heterocyclylcarbonyl, heterocyclyloxycarbonyl, heterocyclylalkanoyl, heterocyclylalkoxycarbonyl, heteroaralkanoyl, heteroaralkoxycarbonyl, heteroaryloxycarbonyl, heteroaroyl, alkyl, alkenyl, cycloalkyl, aryl, aralkyl, aryloxyalkyl, heteroaryloxyalkyl, hydroxyalkyl, aminocarbonyl, aminoalkanoyl, mono- and disubstituted aminocarbonyl or mono- and disubstituted aminoalkanoyl radical wherein the substituents are selected from alkyl, aryl, aralkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, heteroaralkyl, heterocycloalkyl, and heterocycloalkylalkyl radicals, or where said aminoalkanoyl radical is disubstituted, said substituents along with the nitrogen atom to which they are attached form a heterocycloalkyl or heteroaryl radical; P2 represents hydrogen; R2 represents alkyl, aryl, cycloalkyl, cycloalkylalkyl or aralkyl radical, which radical is optionally substituted with a group selected from alkyl and halogen radical, -NO2, -C≡N, CF3, -OR9, -SR9, wherein R9 represents hydrogen, alkyl, or halogen radical; R3 represents hydrogen, alkyl, haloalkyl, alkenyl, alkynyl, hydroxyalkyl, alkoxyalkyl, cycloalkyl, cycloalkylalkyl, heterocycloalkyl, heteroaryl, heterocycloalkylalkyl, aryl, aralkyl, heteroaralkyl, aminoalkyl or mono- and disubstituted aminoalkyl radical, wherein said substituents are selected from alkyl, aryl, aralkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, heteroaralkyl, heterocycloalkyl, and heterocycloalkylalkyl radical, or in the case of a disubstituted aminoalkyl radical, said substituents along with the nitrogen atom to which they are attached, form a heterocycloalkyl or a heteroaryl radical; and R4 represents radical as defined by R3 except for hydrogen.
Vazquez Michael L. ; Mueller Richard A. ; Talley John J. ; Getman Daniel P ; DeCrescenzo Gary A. ; Freskos John N. ; Heintz Robert M. ; Bertenshaw Deborah E., .alpha.- and .beta.-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.
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.
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