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公开(公告)号：EP1032579A1
公开(公告)日：2000-09-06
申请号：EP98958248.1
申请日：1998-11-16
申请人： Akzo Nobel N.V. , Sanofi-Synthélabo
发明人： VAN BOECKEL, Constant, Adriaan, Anton , PETITOU, Maurice , DUCHAUSSOY, Philippe , DREEF-TROMP, Cornelia, Maria , BASTEN, Johannes, Egbertus, Maria
摘要： The invention relates to a carbohydrate derivative having formula (I) wherein R1 is (1-4C)alkoxy; R?2, R3 and R4¿ are independently (1-4C)alkoxy or OSO¿3?-; the total number of sulfate groups is 4, 5 or 6; and the twisted lines represent bonds either above or below the plane of the six-membered ring to which they are attached; or a pharmaceutically acceptable salt thereof. The compounds of the invention have antithrombotic activity and may be used for treating or preventing thrombosis and for inhibiting smooth muscle cell proliferation.
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公开(公告)号：EP1032579B1
公开(公告)日：2003-05-02
申请号：EP98958248.1
申请日：1998-11-16
申请人： Akzo Nobel N.V. , SANOFI-SYNTHELABO
发明人： VAN BOECKEL, Constant, Adriaan, Anton , PETITOU, Maurice , DUCHAUSSOY, Philippe , DREEF-TROMP, Cornelia, Maria , BASTEN, Johannes, Egbertus, Maria
摘要： The invention relates to a carbohydrate derivative having formula (I) wherein R1 is (1-4C)alkoxy; R?2, R3 and R4¿ are independently (1-4C)alkoxy or OSO¿3?-; the total number of sulfate groups is 4, 5 or 6; and the twisted lines represent bonds either above or below the plane of the six-membered ring to which they are attached; or a pharmaceutically acceptable salt thereof. The compounds of the invention have antithrombotic activity and may be used for treating or preventing thrombosis and for inhibiting smooth muscle cell proliferation.
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公开(公告)号：EP1087992A1
公开(公告)日：2001-04-04
申请号：EP99927976.3
申请日：1999-06-11
发明人： BASTEN, Johannes, Egbertus, Maria , VAN BOECKEL, Constant, Adriaan, Anton , BUIJSMAN, Rogier, Christian , DREEF-TROMP, Cornelia, Maria
摘要： The present invention relates to compounds of formula (I), 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, which groups may optionally be substituted with one or more substitutents selected from (1-8C)alkyl or (1-8C)alkoxy; R?2 and R3¿ are independently H or (1-8C)alkyl; R4 is (1-8C)alkyl or (3-8C)cycloalkyl; or R?3 and R4¿ together with the nitrogen atom to which they are bonded are a nonaromatic (4-8)membered ring optionally containing another heteroatom, the ring optionally being substituted with (1-8C)alkyl or SO¿2?-(1-8C)alkyl; Q is a spacer having a chain length of 10 to 70 atoms; and Z is a negatively charged oligosaccharide residue comprising two to six monosaccharide units, the charge being compensated by positively charged counterions; or a pharmaceutically acceptable salt thereof or a prodrug thereof. The compounds of the invention have antithrombotic activity an can be used in treating or preventing thrombin-related diseases.
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