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US 5,674,979 AGranted
Agent for inhibiting symmetrical proteins, in particular enzymes
OwnerWolfgang Schramm, Hans J. Schramminventors
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Abstract
The invention relates to substances for the inhibition of symmetric proteins, in particular enzymes, in particular the inhibition of HIV protease, in the form of structurally symmetric or near symmetric enzyme inhibitors, chazacterized by the same symmetry, or approximate or piecewise (yet sufficient for inhibition) symmetry, as the enzyme molecule to be inhibited.
Claims4
A substance for the inhibition of HIV protease which has the formula Y-M-Z, wherein
- M is --NH--CO--CH(C.sub.4 H.sub.9)--CO--, when Y is acetyl-(D)-Arg-(D)-Ala-(D)-Gln-(D)-Leu- and Z is -(L)-Gln-(L)-Ala-(L)-Arg-NH.sub.2 ;
- M is --NH--CH.sub.2 --CH(C.sub.3 H.sub.7)--CO--, when Y is acetyl-(L)-Arg-(L)-Ala-(L)-Asn-(L)-Leu- and Z is -(D)-Asn-(D)-Gln-(D)-Leu-NH.sub.2 ;
- M is --NH--CH.sub.2 --CO--CH.sub.2 --CO--, when Y is acetyl-(D)-Arg-(D)-Ala-(D)-Gln- and Z is -(L)-Gln-(L)-Ala-(L)-Arg-NH.sub.2 ;
- M is -statin-, when Y is acetyl-(D)-Arg-(D)-Ala-(D)-Asn- and Z is -(L)-Asn-(L)-Ala-(L)-Arg-NH.sub.2 ;
- M is -statin-, when Y is acetyl-(L)-Arg-(L)-Ala-(L)-Gin- and Z is -(D)-Gln-(D)-Ala-(D)-Arg-OH;
- M is -statin-, when Y is fluoroacetyl-(L)-Arg-(L)-Ala-(L)-Asn- and Z is -(D)-Asn-(D)-Ala-(D)-Arg-NH.sub.2 ;
- M is -statin-, when Y is acetyl-(D)-Arg-(D)-Ala-(D)-Leu- and Z is -(L)-Leu-(L)-Ala-(L)-Arg-NH.sub.2 ;
- M is --NH--CH.sub.2 --CH(OH)--CH.sub.2 --CO--, when Y is acetyl-(D)-Leu-(D)-Arg-(D)-Asn- and Z is -(L)-Asn-(L)-Arg-(L)-Leu-NH.sub.2 ;
- M is --NH--(CH.sub.2).sub.3 --NH, NH--CH.sub.2 --O--CH.sub.2 --NH--, --NH--CH.sub.2 --CHOH--CH.sub.2 --NH--, or --NH--CH.sub.2 --NH--CH.sub.2 --NCH.sub.3 --, when Y is acetyl-Arg-Leu-Asn- and Z is -Asn-Leu-Arg-acetyl;
- M is --NH--CHF--CO--CHF--NH--, when Y is H-(D)-Leu-(D)-Leu-(D)-Asn- and Z is -(D)-Asn-(D)-Leu-(D)-Arg-H;
- and
- further M groups which may be used with any combination of the above Y and Z groups are:
- --S--S--, --S--, --O--,
- --CO--CHR--CH(OH)--CHR'--CO--, --NR--NR'--,
- --NH--CHR--CH(OH)--CHR'--NH--, --NH--CF.sub.2 --CO--CH.sub.2 --NH--,
- --NH--CF.sub.2 --CO--CF.sub.2 --NH--, --CO--(CH.sub.2).sub.3 --CO--,
- --NH--(CH.sub.2).sub.3 --NH--, --CO--CH.sub.2 --O--CH.sub.2 --CO--, --N(OR)--, --NR--,
- --P(O).sub.n OH--, --CO--CHR--CO--,
- --NH--CH.sub.2 --O--CH.sub.2 --NH--, --CO--CH.sub.2 --NR--CH.sub.2 --CO--,
- --N(C.sub.5 H.sub.11)--CF.sub.2 --CO--CF.sub.2 --N(C.sub.5 H.sub.11)--,
- N(C.sub.4 H.sub.9)--CH.sub.2 --CH(OH)--CH.sub.2 --N(C.sub.4 H.sub.9)--, and
- -(2S,3S)-NH--CH(CH.sub.2 C.sub.6 H.sub.11)--CH(OH)--CH.sub.2 --NR--,
- where R and R' are hydrogen or C.sub.1-12 aryl- or alkyl-groups and n is 1 or 2.
20 more elements
Dependencies are inferred from the claim text.