http://rdf.ncbi.nlm.nih.gov/pubchem/patent/WO-2021154122-A2

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filingDate 2021-03-17-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_cc2f1c51f66b1cd70cb2d1739b045c49
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_6a1b81bb79eb5fb16ba7e2c50244ee48
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publicationDate 2021-08-05-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber WO-2021154122-A2
titleOfInvention L-, u-modifications of 5-chloro-n-({(5s)-2-oxo-3-[4-3-oxo-4-morpholinyl)-phenyl]-1,3-oxazolidin-5-yl}-methyl)-2-thiophenecarboxamide, solvate with dimethyl sulfoxide, methods for producing same, factor xa-inhibiting pharmaceutical compositions based thereon
abstract The invention relates to organic chemistry, and more particularly to novel modifications of the compound 5-chloro-N-({(5S)-2-oxo-3-[4-3-oxo-4-morpholinyl-phenyl]-1,3-oxazolidin-5-yl}-methyl)-2-thiophenecarboxamide, named L- and U-modifications, a solvate of said compound with dimethyl sulfoxide (DMSO), methods for producing same, as well as pharmaceutical compositions based thereon and the use thereof as a factor Xa inhibitor for treating cardiovascular diseases. The technical result of the invention is that of broadening the range of highly active forms of 5-chloro-N-({(5S)-2-oxo-3-[4-3-oxo-4-morpholinyl-phenyl]-1,3-oxazolidin-5-yl}-methyl)-2-thiophenecarboxamide and pharmaceutical compositions based thereon which can be used as an Xa factor inhibitor for the treatment and prophylaxis of cardiovascular diseases as a result of the improved solubility of the novel U- and L-modifications and of a solvate thereof with DMSO, as well as that of improving the biological activity of rivaroxaban with respect to factor Xa inhibition while remaining stable for 3 years.
priorityDate 2020-01-28-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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