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filingDate 2007-11-08-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationDate 2010-12-20-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber RU-2009121559-A
titleOfInvention MICHAEL SYSTEMS AS TRANSGLUTAMINASE INHIBITORS
abstract 1. The peptide or peptidomimetic of the following general formula (I), (II) or (III):! ! where MS is an acceptor-substituted olefin of the following structure:! ! E represents the following group -CH2-, -CF2-, -C2H4-, -CH2-CF2-, -CF2-CH2-, -CH = CH-, -CH (OH) -CH2-, -C (= O) -CH2-, -CH2-NH-, -CH2-O-, -CH (OH) -CH2-NH-, -P (= O) (OH) -NH-, -P (= O) (OH) - O-, P (= O) (OH) -S-, -P (= O) (OH) -CH2-, -CH (OH) -CH2-NH-, -C (= O) -NH-, - C (= O) —O— or —C (= O) —NX ″ -; ! m is 0 or 1; ! residues Z1, Z2, Z3, independently of one another, represent the following groups: —H, —CO— (C1-C6 alkyl), —CO-R6, —CO-R7, —CO- (C1-C6 haloalkyl), —CO - (C3-C10 heteroaryl), -CO- (C6-C15 aryl), -COO- (C1-C6 haloalkyl), -COO- (C3-C10 heteroaryl), -COO- (C6-C15 aryl), -COO- (C1-C6 alkyl ), -COO-R8, -COO-R9, -CN, -F, -Cl, -COOH, -CO-NH (C1-C6 alkyl), -CO-N (C1-C6 alkyl) (C1-C6 alkyl), - CO-NR10R11, -CO-NH2, -CO-N (CR12R13R14) (CR15R16R17), -CH2CN, -CH2F, -CHF2, -CF3, -OCF3, -CH2-CF3, -NO2, -CS- (C1-C6 alkyl), -CS-R18, -CS-R19, -CS-O- (C1-C6 alkyl), -CS-O-R20, -CS-O-R21, -CS-N (C1-C6 alkyl) ( C1-C6 alkyl), -CS-NR22R23, -CS-NH2, -CS-N (CR24R25R26) (CR27R28R29), -SO-R30, -SO-R31, -SO2-R32, -SO2-R33, -SO- CR34R35R36, -SO-CR37R38R39, -SO2-CR40R41R42, -SO2-CR43R44R45, -SO-N (C1-C6 alkyl) (C1-C6 alkyl), -SO-NR46R47, -SO-NH2, -SO-N (CR48R4 9R50) (CR51R52R53), -SO2-N (C1-C6 alkyl) (C1-C6 alkyl), -SO2-NR54R55, -SO2-NH2, -SO2-N (CR56R57R58) (CR59R60R61), -SO2-OH, - SO2-OR62, -SO2-CR63R64R65, -SO2-OCR66R67R68, -O-P (O) (OH) 2, -OP (O) (OR69) (OR70), -O-P (O) (O-C1- C6 alkyl) (O-C1-C6 alkyl), -P (O) (OR71) (OR72), -P (O) (O-C1-C6 alkyl) (O-C1-C6 alkyl), -CF2-P (O) (OR73) (OR74), —CF2-P (O) (O-C1-C6 alkyl) (O-C1-C6 alkyl), wherein at least one of the residues Z1, Z2, Z3 is different from hydrogen; ! residues Z1 and Z2 together may also be the residue —CO — O — CO — CH 2 -, —CO — O — CH 2 —CH 2 -,! residues Z2 and Z3 together may also be the residue -CO-Z'-CH2-, -CO-O-CH2-, -CO-CH2-CH2-, -CO-O-CO-, -CO-NH-CO- or -Z'-CH2-CH2-, where! Z 'represents one of the following groups: -CH2-, -CF2-, -C2H4-, -CF2-CH2-, -CH2-CH2-, -O-, -O-CH2-, -NH- or -NH- CH2-; ! Q and Q 'independently from each other represent a residue of the side chain of a natural amino acid, or Q together with X' forms a propyleneyl residue, or Q 'together with X ”ar
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