[미국특허]
.alpha.- and .beta.-amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors
원문보기
IPC분류정보
국가/구분
United States(US) Patent
등록
국제특허분류(IPC7판)
A61K-031/505
C07D-239/02
C07D-211/78
C07D-277/30
출원번호
US-0525161
(2000-03-14)
발명자
/ 주소
Michael L. Vazquez
Richard A. Mueller
John J. Talley
Daniel P Getman
Gary A. DeCrescenzo
John N. Freskos
Robert M. Heintz
Deborah E. Bertenshaw
출원인 / 주소
G. D. Searle & Co.
대리인 / 주소
Banner & Witcoff, Ltd.
인용정보
피인용 횟수 :
14인용 특허 :
27
초록
.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 method of inhibiting a retroviral protease comprising administering a protease inhibiting amount of a compound represented by the formula (I): [EQU496]or a pharmaceutically acceptable salt or ester thereof wherein R2 is an alkyl, aryl, cycloalkyl, cycloalkylalkyl or aralkyl radical, which radic
1. A method of inhibiting a retroviral protease comprising administering a protease inhibiting amount of a compound represented by the formula (I): [EQU496]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 radicals, wherein R9 is hydrogen or alkyl radicals; R3 is alkyl, haloalkyl, alkenyl, alkynyl, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkylsulfonylalkyl, cycloalkyl, cycloalkylalkyl, heterocycloalkyl, heteroaryl, heterocycloalkylalkyl, aryl, aralkyl or heteroaralkyl radicals; R4 is heterocycloalkyl, heteroaryl or aryl radicals; Y is O or S; and A is heterocycloalkyl, heterocycloalkoxy, heterocycloalkylalkyl, heterocycloalkylalkoxy, heteroaralkyl, heteroaralkoxy, heteroaryloxy or heteroaryl radicals; and wherein alkyl, alone or in combination, is a straight-chain or branched-chain alkyl radical containing 1 to 8 carbon atoms; alkenyl, alone or in combination, is a straight-chain or branched-chain hydrocarbon radial having at least one double bond and containing 2 to 8 carbon atoms; alkynyl, alone or in combination, is a straight-chain or branched chain hydrocarbon radical having at least one triple bond and containing 2 to 10 carbon atoms; aryl, alone or in combination, is an unsubstituted phenyl or naphthyl radical or a phenyl or naphthyl radical substituted with alkyl, alkoxy, halogen, hydroxy, amino, alkylamino, dialkylamino, nitro, cyano, carboxy, alkoxycarbonyl, amido, alkylamido, dialkylamido, trifluoromethyl, methylthio, methylsulfinyl or methylsulfonyl radicals; cycloalkyl, alone or in combination, is a saturated or partially saturated monocyclic, bicyclic or tricyclic alkyl radical wherein each cyclic moiety contains 3 to 8 carbon atoms; heterocycloalkyl, alone or in combination, is a monocyclic, bicyclic or tricyclic heterocycle radical having 1-4 nitrogen, nitrogen oxide, oxygen, sulphur, sulfone or sulfoxide heteroatom ring members, optionally benz-fused and optionally substituted on one or more carbon atoms by halogen, alkyl, alkoxy, hydroxy, oxo, aryl or aralkyl radicals, or on a secondary nitrogen atom by hydroxy, alkyl, aralkoxycarbonyl, alkanoyl, phenyl or phenylalkyl radicals; and heteroaryl, alone or in combination, is an aromatic heterocycloalkyl, optionally substituted with respect to aryl and heterocycloalkyl radicals, and optionally a pharmaceutically acceptable carrier.
Vazquez Michael L. ; Mueller Richard A. ; Talley John J. ; Getman Daniel ; DeCrescenzo Gary A. ; Freskos John N., .alpha.- and .beta.-amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors.
Vazquez Michael L. ; Mueller Richard A. ; Talley John J. ; Getman Daniel ; DeCrescenzo Gary A. ; Freskos John N., .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., .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. ; Bertenshaw Deborah E. ; Heintz Robert M., .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. ; Bertenshaw Deborah E. ; Heintz Robert M., .alpha.- and .beta.-amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors.
Vazquez Michael L. ; Mueller Richard A. ; Talley John J. ; Getman Daniel ; DeCrescenzo Gary A. ; Freskos John N., .alpha.-and .beta.-amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors.
Vazquez Michael L. ; Mueller Richard A. ; Talley John J. ; Getman Daniel ; DeCrescenzo Gary A. ; Freskos John N., .alpha.-and .beta.-amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors.
Vazquez Michael L. ; Mueller Richard A. ; Talley John J. ; Getman Daniel ; DeCrescenzo Gary A. ; Freskos John N., .beta.-amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors.
Branca Quirico (Basel CHX) Mrki Hans P. (Basel CHX) Neidhart Werner (Freiburg im Breisgau DEX) Ramuz Henri (Birsfelden CHX) Wostl Wolfgang (Grenzach-Wyhlen DEX), Amino acid derivatives which have renin inhibiting activity.
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.
Vazquez Michael L. ; Mueller Richard A. ; Talley John J. ; Getman Daniel P. ; DeCrescenzo Gary A. ; Freskos John N. ; Bertenshaw Deborah E. ; Heintz Robert M., Hydroxyethylamino sulphonamides useful as retroviral protease inhibitors.
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.
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