http://rdf.ncbi.nlm.nih.gov/pubchem/patent/DD-294176-A5

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assignee http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_313c2ac1c6159e38a96bd17d83b17a2b
classificationIPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/G01N33-573
http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C12Q1-25
http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C12N9-99
filingDate 1990-05-11-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_f1f48ecc7971273c8f6bc1526627050e
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_4bec19b2666e61b143a0c20939fd907f
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_ff733c63d6e9131ae320342f7c19c36a
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_49c478b5b19fb98cd0d4bc6e8e15513f
publicationDate 1991-09-26-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber DD-294176-A5
titleOfInvention NEW INHIBITORS FOR INHIBITING THE CATALYTIC ACTIVITY OF PROLIN-SPECIFIC AND OTHER PROTEOLYTIC ENZYMES AND METHOD FOR THE PRODUCTION THEREOF
abstract The invention serves the development, production and application of highly effective inhibitors for inhibiting undesired activity of enzymes which, as part of their catalytic action on substrates, cleave and bond ester bonds and can cleave, isomerize and synthesize peptide bonds. The invention relates to peptidylammonium (or amono-) methyl ketones of the general formula R ind 1-CO-CH 2 -R ind 2 / X n. The object of the invention is to provide an easily applicable method for controlling the activity of enzymes in their purified form, as well as in normal and pathologically altered body fluids, organs, tissues, cells and cell cultures of human, animal, microbial, viral origin both in vitro and in vivo and for the synthetic recovery of the inhibitors. The radical R ind 1-CO may represent alpha-amino acid or N-protected alpha-amino acid residues, N-protected peptidyl residues or N-unprotected peptidyl residues, these N-protecting groups being alkoxycarbonyl, aralkoxycarbonyl, alkanoyl, cycloalkylcarbonyl, aralkanoyl, aroyl, Heterocyclylcarbonyl, alkylsulphonyl, arylsulphonyl, monoaralkylcarbamoyl, cinnamoyl, alpha-Aralkoxycarbonylaminoalkanoyl groups or together with the nitrogen atom formed cyclic amides. or alipathic, branched, aromatic, and aromatic and substituted and heterocyclic acyl radicals such as aralkoxycarbonyl, alkanoyl, cycloalkylcarbonyl, aralkanoyl, aroyl, heterocyclylcarbonyl, alkylsulphonyl, aryl sulphonyl, monoaralkylcarbamoyl, cinnamoyl, alpha-aralkoxycarbonylaminoalkanoyl. R ind 2 may represent primary secondary amines (including C-terminal protected and unprotected amino acids and peptides other than proline in N-terminal position) and tertiary alipathic or aromatic, branched or heterocyclic substituted and unsubstituted amines (such as methylamine, dimethylamine, pyridines or sarcosine, N-methylalanine, aziridinecarboxylic acid, azetidinecarboxylic acid, dehydropoline, N-methylproline, aminobenzoic acid, nicotinic acid, isonicotinic acid, chiolinic acid, which may also be extended to their carboxyl functions by peptides or protecting groups). R ind 2 may be positively charged {inhibitors; enzymes; Hydrolases; proteases; Aminosäurederivete; Peptide derivatives; reversible inhibition; diagnostics; therapeutics; pharmaceuticals}
isCitedBy http://rdf.ncbi.nlm.nih.gov/pubchem/patent/US-5416117-A
http://rdf.ncbi.nlm.nih.gov/pubchem/patent/US-5639783-A
http://rdf.ncbi.nlm.nih.gov/pubchem/patent/US-5328909-A
priorityDate 1990-05-11-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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