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filingDate 2005-12-21-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_ea32573deda329d908b33c6a921462f0
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publicationDate 2007-07-25-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber MX-2007007837-A
titleOfInvention ANTITROMBOTIC DUAL INHIBITORS THAT INCLUDE A BIOTINE WASTE.
abstract The present invention relates to compounds of the oligosaccharide-A (I) separator of formula (I), wherein the oligosaccharide is a negatively charged oligosaccharide residue comprising two to twenty-five monosaccharide units, the charge being compensated for positively charged counterions, and wherein the oligosaccharide residue is derived from an oligosaccharide having anti-Xa activity (mediated by AT-III) per se: the separator is a flexible, essentially pharmacologically inactive, binding residue having a chain length of 10 to 70 atoms; A is the residue -CH [NH-SO2-R1] [CO-NR2-CH (4-benzamidine) -CO-NR3R4] wherein R1 is phenyl, naphthyl, 1,2,3,4-tetrahydronaphthyl, (iso) quinolinyl, tetrahydro (iso) quinolinyl, 3,4-dihydro-1H-isoquinolinyl, chromanyl or the camphor group, whose groups can be optionally substituted with one or more substitutes selected from (1-8C) alkyl or (1-8C) alkoxy; and wherein R2 and R3 are independently H or (1-8C) alkyl; R4 is (1-8C) alkyl or (3-8C) cycloalkyl; or R3 and R4 together with the nitrogen atom to which they join with a non-aromatic ring, consisting of (4-8) members that optionally contain another heteroatom, optionally replacing the ring with (1-8C) alkyl or SO2- ( 1-8C) alkyl; or a pharmaceutically acceptable salt thereof or a pro-drug or solvate thereof; wherein the compound of the formula I further comprises at least one covalent bond with a biotin residue or an analog thereof. The compounds of the invention have anti-thrombotic activity and can be used in the treatment or prevention of thrombosis or other thrombin-related diseases. The anti-thrombotic activity of the compound of this invention can be neutralized in emergency cases after administration of avidin, streptavidin and analogs thereof having high affinity to biotin.
priorityDate 2004-12-23-04:00^^<http://www.w3.org/2001/XMLSchema#date>
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