发明名称 Antithrombotic peptide compounds with saccharide radicals
摘要 Described are 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 substituents selected from (1-8C)alkyl or (1-8C)alkoxy; 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 are bonded are a nonaromatic (4-8)membered ring optionally containing another heteroatom, the ring optionally being substituted with (1-8C)alkyl or SO2-(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 described have antithrombotic activity and can be used in treating or preventing thrombin-related diseases.
申请公布号 NZ508623(A) 申请公布日期 2002.11.26
申请号 NZ19990508623 申请日期 1999.06.11
申请人 AKZO NOBEL N 发明人 BASTEN, JOHANNES EGBERTUS MARIA;VAN BOECKEL, CONSTANT ADRIAAN ANTON;BUIJSMAN, ROGIER CHRISTIAN;DREEF-TROMP, CORNELIA MARIA
分类号 A61K38/00;A61K38/14;A61P7/02;A61P43/00;C07H3/06;C07K9/00;(IPC1-7):C07K9/00 主分类号 A61K38/00
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