[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-023/902
C07D-021/178
C07D-027/730
출원번호
US-0204827
(1994-03-02)
발명자
/ 주소
Vazquez Michael L.
Mueller Richard A.
Talley John J.
Getman Daniel P
DeCrescenzo Gary A.
Freskos John N.
Heintz Robert M.
Bertenshaw Deborah E.
출원인 / 주소
G. D. Searle & Co.
대리인 / 주소
Banner & Witcoff, Ltd.
인용정보
피인용 횟수 :
43인용 특허 :
1
초록
.alpha.- and .beta.-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
대표청구항▼
[ What is claimed is:] [1.] A compound represented by the formula: [ STR 495 ] or a pharmaceutically acceptable salt thereof wherein R.sup.2 is an alkyl, aryl, cycloalkyl, cycloalkylalkyl or aralkyl radical, which radical is optionally substituted with a radical selected from the group consisting of
[ What is claimed is:] [1.] A compound represented by the formula: [ STR 495 ] or a pharmaceutically acceptable salt thereof wherein R.sup.2 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, CF.sub.3, --OR.sup.9, and --SR.sup.9 radicals, wherein R.sup.9 is hydrogen or alkyl radicals;R.sup.3 is alkyl, haloalkyl, alkenyl, alkynyl, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkylsulfonylalkyl, cycloalkyl, cycloalkylalkyl, heterocycloalkyl, heteroaryl, heterocycloalkylalkyl, aryl, aralkyl or heteroaralkyl radicals;R.sup.4 is heterocycloalkyl, heteroaryl or aryl radicals;Y is O or S; andA is heterocycloalkyl, heterocycloalkoxy, heterocycloalkylalkyl, heterocycloalkylalkoxy, heteroaralkyl, heteroaralkoxy, heteroaryloxy or heteroaryl radicals; andwherein 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.
Michael L. Vazquez ; Richard A. Mueller ; John J. Talley ; Daniel P Getman ; Gary A. DeCrescenzo ; John N. Freskos ; Robert M. Heintz ; Deborah E. Bertenshaw, .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.
Michael L. Vazquez ; Richard A. Mueller ; John J. Talley ; Daniel Getman ; Gary A. DeCrescenzo ; John N. Freskos, .alpha.-and .beta.-amino acid hydroxyethlamino sulfonamides useful as retroviral protease inhibitors.
Michael L. Vazquez ; Richard A. Mueller ; John J. Talley ; Daniel P. Getman ; Gary A. DeCrescenzo ; John N. Freskos ; Deborah E. Bertenshaw ; Robert M. Heintz, .alpha.-and .beta.-amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors.
Getman, Daniel P; DeCrescenzo, Gary A; Freskos, John N; Vazquez, Michael L; Sikorski, James A; Devadas, Balekudru; Nagarajan, Srinivasan Raj; Brown, David L; McDonald, Joseph J, Bis-amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors.
Getman, Daniel P; DeCrescenzo, Gary A; Freskos, John N; Vazquez, Michael L; Sikorski, James A; Devadas, Balekudru; Nagarajan, Srinivasan Raj; Brown, David L; McDonald, Joseph J, Bis-amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors.
Flentge, Charles A.; Chen, Hui-Ju; DeGoey, David A.; Flosi, William J.; Grampovnik, David J.; Huang, Peggy P.; Kempf, Dale J.; Klein, Larry L.; Krueger, Allan C.; Madigan, Darold L.; Randolph, John T.; Sun, Minghua; Yeung, Ming C.; Zhao, Chen, HIV protease 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.; 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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