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filingDate 2005-12-21-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationDate 2008-07-17-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber JP-2008525373-A
titleOfInvention Antithrombotic dual inhibitors containing biotin residues
abstract The present invention provides a compound of formula (I): oligosaccharide-spacer-A (I) [wherein the oligosaccharide is a negatively charged oligosaccharide residue comprising 2 to 25 monosaccharide units, the charge being positively charged The oligosaccharide residue is itself derived from an oligosaccharide having anti-Xa activity (mediated by AT-III); the spacer has a chain length of 10 to 70 atoms, essentially And A is a residue —CH [NH—SO 2 —R 1 ] [CO—NR 2 —CH (4-benzamidine) -CO—NR 3 R 4 ] {wherein R 1 is phenyl, naphthyl, 1,2,3,4-tetrahydronaphthyl, (iso) quinolinyl, tetrahydro (iso) quinolinyl, 3,4-dihydro-1H-isoquinolinyl, chromanyl or camphor group And these groups (L-8C) alkyl or (l-8C) may optionally be substituted by one or more substituents selected from alkoxy, R 2 and R 3 are independently H or (l-8C) alkyl Yes; R 4 is (1-8C) alkyl or (3-8C) cycloalkyl; or R 3 and R 4 optionally contain another heteroatom together with the nitrogen atom to which they are attached aromatic (4 to 8) membered ring is formed of, the ring (l-8C) alkyl or SO 2 - is a (l-8C) alkyl optionally substituted with). Wherein the compound of formula I further comprises at least one covalent bond with a biotin residue or analog thereof, or a pharmaceutically acceptable salt, prodrug or It relates to these solvates. The compounds of the present invention have antithrombotic activity and can be used for the treatment or prevention of thrombosis or other thrombin related diseases. The antithrombotic activity of the compounds of the invention can be neutralized in the event of an emergency by the administration of avidin, streptavidin and analogs with high biotin affinity.
priorityDate 2004-12-23-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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