发明名称 ANTAGONISTS OF ADHESION RECEPTORS, METHOD OF THEIR PRODUCTION AND PHARMACEUTICAL AGENTS ON THEIR BASE
摘要 Disclosed are oxazolidine derivatives of the formula (I) wherein Y is aziridino, azetidino, pyrrolidino, piperidino, 1-oxa-8-azaspiro[4.5]dec-8yl, hexahydroazepino or 4-R4-piperazino which is unsubstituted or substituted once by R2, OZ, SZ, N(Z)2 or -oxo; Z is in each case H, A, phenyl-CkH2k or Ac; R1 is phenyl which is substituted once by CN, H2N-CH2-, (A)2N-CH2-, H2N-C(=NH)-, H2N-C(=NH)-NH-, H2N-C(=NH)-NH-CH2-, HO-NH-C(=NH)- alebo HO-NH-C(=NH)-NH-, R2 je -CmH2m-COOR3 or -CnH2n-O-CpH2p-COOR3; R3 is H, A or benzyl; R4 is H, A, benzyl or -CmH2m-COOR3; A is in each case alkyl having 1 - 6 C atoms; Ac is carboxylic acyl having 1 - 11 C atoms; k and m are in each case independently 0, 1, 2 or 3; n is 0, 1 or 2; and p is 1, 2 or 3; or a salt thereof. Said derivatives inhibit the binding of fibrinogen to a fibrinogen receptor and are therefore usable in treating thrombosis, apoplexy, cardiac infarctus, inflammation or arteriosclerosis and tumors; process for the preparation of said derivatives and their use in preparing drugs; pharmaceutical compositions based on these derivatives.
申请公布号 SK48494(A3) 申请公布日期 1995.02.08
申请号 SK19940000484 申请日期 1994.04.26
申请人 MERCK PATENT GMBH 发明人 RADDATZ PETER;GANTE JOACHIM;JURACZYK HORST;WURZIGER HANNA;PRUCHER HELMUT;BERNOTAT DANIELOWSKI S.;MELZER GUIDO
分类号 A61K31/415;A61K31/4166;A61K31/42;A61K31/421;A61K31/422;A61K31/425;A61K31/426;A61K31/4427;A61K31/445;A61K31/495;A61K31/496;A61K31/55;A61P7/02;A61P9/00;A61P9/08;A61P9/10;A61P19/10;A61P29/00;A61P35/00;A61P43/00;C07D233/36;C07D263/00;C07D263/20;C07D277/14;C07D295/00;C07D401/06;C07D403/06;C07D413/06;C07D419/06;C07D491/10;C07D491/107;C07D498/10;(IPC1-7):C07D263/20;C07D233/32;C07D417/06;A61K31/41 主分类号 A61K31/415
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