Title:
【発明の名称】新規マロン酸誘導体、それらの製造法、第Xa因子活性の抑制剤としてのそれらの使用、およびそれらを含有する医薬組成物
Document Type and Number:
Japanese Patent JP2003524001
Kind Code:
A
Abstract:
The present invention relates to new compounds for the inhibition of blood clotting proteins, and more particularly, to malonic acid derivatives of the formula 1, wherein R(1), R(2), R(3), R(4), R(5), and R(6) have the meanings indicated in the claims. The compounds of formula I are inhibitors of the blood clotting enzyme factor Xa. The invention also relates to processes for the preparation of the compounds of formula I, to methods of inhibiting factor Xa activity and of inhibiting blood clotting, to the use of the compounds of formula I in the treatment and prophylaxis of diseases, which can be treated or prevented by the inhibition of factor Xa activity such as thromboembolic diseases, and to the use of the compounds of formula I in the preparation of medicaments to be applied in such diseases. The invention further relates to compositions containing a compound of formula I in admixture or otherwise in association with an inert carrier, in particular pharmaceutical compositions containing a compound of formula I together with pharmaceutically acceptable carrier substances and auxiliary substances.
Inventors:
Fahd Al-Obaydi
Armin Walther
Peter Wild Goose
Armin Walther
Peter Wild Goose
Application Number:
JP2001562517A
Publication Date:
August 12, 2003
Filing Date:
February 21, 2001
Export Citation:
Assignee:
Aventis Pharma Deutsche Land Gesellschaft Mitt Beschlenktel Haftung
International Classes:
A61K31/06; A61K31/165; A61K31/215; A61K31/40; A61K31/435; A61P7/02; A61P9/00; A61P9/10; A61P9/14; A61P11/00; A61P31/00; C07C257/18; C07D207/16; C07C277/08; C07C279/14; C07D207/08; C07D213/56; C07D217/14; C07K5/02; C07K5/06; C07K5/08; A61K38/00; (IPC1-7): C07C257/18; A61K31/165; A61K31/215; A61K31/40; A61P7/02; A61P9/00; A61P9/10; A61P9/14; A61P11/00; A61P31/00; C07C277/08; C07C279/14; C07D207/16
Domestic Patent References:
| JP2002534420A | 2002-10-15 | |||
| JP2001524467A | 2001-12-04 | |||
| JP2000136190A | 2000-05-16 | |||
| JPH10503477A | 1998-03-31 | |||
| JP2002534420A | 2002-10-15 | |||
| JP2001524467A | 2001-12-04 | |||
| JP2000136190A | 2000-05-16 |
Attorney, Agent or Firm:
Chika Takagi (2 outside)