[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-038/00
A61K-031/555
A61K-031/18
C07D-213/79
C07D-239/02
출원번호
US-0694785
(2000-10-24)
발명자
/ 주소
Vazquez, Michael L.
Mueller, Richard A.
Talley, John J.
Getman, Daniel
DeCrescenzo, Gary A.
Freskos, John N.
출원인 / 주소
G.D. Searle
대리인 / 주소
Banner & Witcoff, Ltd.
인용정보
피인용 횟수 :
17인용 특허 :
22
초록
α- and β-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
대표청구항▼
1. Compound represented by the formula: wherein: R represents hydrogen, alkoxycarbonyl, aralkoxycarbonyl, alkylcarbonyl, cycloalkylcarbonyl, cycloalkylalkoxycarbonyl, cycloalkylalkanoyl, alkanoyl, aralkanoyl, aroyl, aryloxycarbonyl, aryloxycarbonylalkyl, aryloxyalkanoyl, heterocyclylcarbonyl, h
1. Compound represented by the formula: wherein: R represents hydrogen, 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, or mono- or disubstituted aminocarbonyl or mono- or disubstituted aminoalkanoyl radicals, 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; R' represents hydrogen or radicals as defined for R3or R and R' together with the nitrogen to which they are attached represent heterocycloalkyl or heteroaryl radical; R1represents hydrogen, --CH2SO2NH2,--CH2CO2CH3,--CO2CH3,--CONH2,--CH2C(O)NHCH3,--C(CH3)2(SH), --C(CH3)2(SCH3), --C(CH3)2(S[O]CH3), --C(CH3)2(S[O]2CH3), alkyl, haloalkyl, alkenyl, alkynyl or cycloalkyl radicals, or amino acid side chains selected from asparagine, S-methyl cysteine and the sulfoxide (SO) and sulfone (SO2) derivatives thereof, isoleucine, allo-isoleucine, alanine, leucine, tert-leucine, phenylalanine, omithine, histidine, norleucine, glutamine, threonine, glycine, allo-threonine, serine, O-methyl serine, asparatic acid, beta-cyano alanine and valine side chains;
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 ; 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.
Gante Joachim (Darmstadt DEX) Raddatz Peter (Darmstadt DEX) Sombroek Johannes (Darmstadt DEX) Schmitges Claus J. (Gross-Umstadt DEX) Minck Klaus O. (Ober-Ramstadt DEX), Aminoacid derivatives inhibiting renin.
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.
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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