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classificationIPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D475-06
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filingDate 1991-04-23-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_3c4d9bf600e5a074013ac0d572a61502
publicationDate 1993-02-17-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber EP-0527185-A1
titleOfInvention Amethopterin precursors (methotrexate) intermediates, processes for their preparation and compositions containing them.
abstract The present invention relates to the synthesis of gem-diphosphonic analogs of amethopterin (methotrexate), and their use as pharmaceutical compositions, for various therapeutic applications. The objective is in particular to associate the concept of prodrug with the pharmacological vectorization of antineoplastic agents with respect to bone carcinomas, by diphosphonic acids. According to the invention, the gem-diphosphonic compounds of amethopterin (methotrexate) and of deaza N-10 amethopterin are in the form of an amethopterin prodrug whose gem-diphosphonic group is linked to the pteroylglutamic group by a peptide bond . These compounds are in particular usable in pharmaceutical compositions for oncology, in particular for the treatment of tumors or metastases in particular bone, and / or rheumatology, in particular for the treatment of rebellious psoriatic arthritis, polymyositis, Reiter's disease and polyarthritis rheumatoid.
priorityDate 1990-04-23-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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