http://rdf.ncbi.nlm.nih.gov/pubchem/patent/US-2005026994-A1

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filingDate 2001-10-25-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_286017dca927bbdc626895ace6ad37ac
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publicationDate 2005-02-03-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber US-2005026994-A1
titleOfInvention Use of 2, 4diamino-3-hydroxycarboxylic acid derivatives as proteasome inhibitors
abstract The present invention relates to the new use of 2,4-diamino-3-hydroxycarboxylic acids of formula (I), in which A and B independently represent a bond or an unsubstituted or substituted amino acyl moiety; R 1 represents hydrogen; an amino protecting group; or a group of formula R 5 Y— wherein R 5 represents hydrogen or an unsubstituted or substituted alkyl, alkenyl, alkinyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, heterocyclyl or heterocyclylalkyl group; and Y represents —CO—; —NH—CO—; —NH—CS—; —SO 2 —; —O—CO—; or —O—CS—; R 2 represents the side chain of a natural amino acid; an alkyl, arylalkyl, heteroarylalkyl or cycloalkylalkyl group; or trimethylsilylmethyl, 2-thienylmethyl or styrylmethyl; R 3 represents halogen, alkyl, alkoxy or hydroxyalkoxy; and R 4 represents 2(R)-hydroxyindan-1(S)-yl; (S)-2-hydroxy-1-phenylethyl; or 2-hydroxy-benzyl unsubstituted or substituted in 4-position by methoxy; in the manufacture of a pharmaceutical composition for the treatment of a proliferative disease, e.g., of a solid tumor; to a method of treatment of warm-blooded animals; and to 2,4-diamino-3-hydroxycarboxylic acids of formula (I*), wherein A and B independently represent an unsubstituted or substituted amino acyl moiety; R 2 represents arylalkyl; R 3 represents halogen, alkyl, alkoxy or hydroxyalkoxy; R 4 represents 2-hydroxy-benzyl unsubstituted or substituted in 4 position by methoxy; and R 5 represents arylalkyl and Y represents —CO—; or R 5 represents alkyl substituted by cycloalkyl, naphthyl, pyridyl or phenyl in which phenyl is substituted by alkyl or amino; and Y represents —O—CO; pharmaceutically acceptable salts thereof; and the use of such compounds of formula (I*) for the therapeutic treatment of the human or animal body, especially the treatment of proliferative diseases.
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priorityDate 1999-04-27-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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Total number of triples: 466.