公开(公告)号：EP0667773A1

公开(公告)日：1995-08-23

申请号：EP93923853.0

申请日：1993-10-12

申请人： MERCK & CO. INC.

发明人： HARTMAN, George D. ,  PRUGH, John D. ,  EGBERTSON, Melissa S. ,  DUGGAN, Mark E. ,  HOFFMAN, William

IPC分类号： A61K31 ,  A61P7 ,  C07C311 ,  C07D233 ,  C07D333 ,  C07D401 ,  C07D409 ,  C07D413

CPC分类号： C07D401/12 ,  C07C311/06 ,  C07C311/19 ,  C07D333/38 ,  C07D409/06 ,  C07D409/12 ,  C07D413/12

摘要： Novel fibrinogen receptor antagonists of the formula: X-Y-Z-Aryl-A-B and the pharmaceutically acceptable salts thereof, wherein Aryl is a 5-membered aromatic ring system containing 1 or 2 heteroatoms chosen from N, O or S wherein ring atoms may be unsubstituted or substituted with R5 and wherein S may be substituted with 0, 1 or 2 oxygen atoms; and X comprises various Nitrogen substituents including aromatic or nonaromatic systems; Y comprises, for example, alkyl or alkylaminocarbonylalkyl groups and Z and A are substituents which when present are independently chosen from alkyl or alkyloxyalkyl or other groups as defined herein; B is (a) or (b). The claimed compounds exhibit fibrinogen receptor antagonist activity, inhibit platelet aggregation and are therefore useful in modulating or preventing thrombus formation.

公开(公告)号：EP0673247A1

公开(公告)日：1995-09-27

申请号：EP94904069.0

申请日：1993-11-29

申请人： MERCK & CO. INC.

发明人： EGBERTSON, Melissa, S. ,  TURCHI, Laura, M. ,  HARTMAN, George, D. ,  HALCZENKO, Wasyl ,  WHITMAN, David, B. ,  PERKINS, James, J. ,  KRAUSE, Amy, E. 570 W. Dekalb Pike ,  IHLE, Nathan ,  CLAREMON, David, Alan ,  HOFFMAN, William ,  DUGGAN, Mark, E.

IPC分类号： C07D295 ,  A61K31 ,  A61P7 ,  A61P43 ,  C07C255 ,  C07C271 ,  C07C309 ,  C07C311 ,  C07D205 ,  C07D207 ,  C07D211 ,  C07D213 ,  C07D233 ,  C07D401 ,  C07D409 ,  C07D521

CPC分类号： C07D213/30 ,  C07C311/19 ,  C07D205/04 ,  C07D211/22 ,  C07D211/26 ,  C07D211/34 ,  C07D211/46 ,  C07D211/70 ,  C07D213/71 ,  C07D231/12 ,  C07D233/56 ,  C07D233/64 ,  C07D249/08 ,  C07D295/084 ,  C07D295/088 ,  C07D295/096 ,  C07D295/155 ,  C07D401/12 ,  C07D409/12

摘要： Novel fibrinogen receptor antagonists of the formula: X-Y-Z-Aryl-A-B are provided in which the claimed compounds exhibit fibrinogen receptor antagonist activity, inhibit platelet aggregation and are therefore useful in modulating thrombus formation.