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1. WO2000040571 - NOVEL MALONIC ACID DERIVATIVES, PROCESSES FOR THEIR PREPARATION, THEIR USE AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM (INHIBITION OF FACTOR XA ACTIVITY)

Publication Number WO/2000/040571
Publication Date 13.07.2000
International Application No. PCT/EP1999/010340
International Filing Date 23.12.1999
Chapter 2 Demand Filed 21.07.2000
IPC
C07C 257/18 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
257Compounds containing carboxyl groups, the doubly-bound oxygen atom of a carboxyl group being replaced by a doubly-bound nitrogen atom, this nitrogen atom not being further bound to an oxygen atom, e.g. imino-ethers, amidines
10with replacement of the other oxygen atom of the carboxyl group by nitrogen atoms, e.g. amidines
18having carbon atoms of amidino groups bound to carbon atoms of six-membered aromatic rings
C07C 279/14 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
279Derivatives of guanidine, i.e. compounds containing the group the singly-bound nitrogen atoms not being part of nitro or nitroso groups
04having nitrogen atoms of guanidine groups bound to acyclic carbon atoms of a carbon skeleton
14being further substituted by carboxyl groups
CPC
C07C 257/18
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
257Compounds containing carboxyl groups, the doubly-bound oxygen atom of a carboxyl group being replaced by a doubly-bound nitrogen atom, this nitrogen atom not being further bound to an oxygen atom, e.g. imino-ethers, amidines
10with replacement of the other oxygen atom of the carboxyl group by nitrogen atoms, e.g. amidines
18having carbon atoms of amidino groups bound to carbon atoms of six-membered aromatic rings
C07C 279/14
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
279Derivatives of guanidine, i.e. compounds containing the group , the singly-bound nitrogen atoms not being part of nitro or nitroso groups
04having nitrogen atoms of guanidine groups bound to acyclic carbon atoms of a carbon skeleton
14being further substituted by carboxyl groups
Applicants
  • AVENTIS PHARMA DEUTSCHLAND GMBH [DE/DE]; Brüningstrasse 50 D-65929 Frankfurt am Main, DE
Inventors
  • DEFOSSA, Elisabeth; DE
  • HEINELT, Uwe; DE
  • KLINGLER, Otmar; DE
  • ZOLLER, Gerhard; DE
  • MATTER, Hans; DE
  • AL-OBEIDI, Fahad, A.; US
  • WALSER, Armin; US
  • WILDGOOSE, Peter; DE
Priority Data
99100002.702.01.1999EP
99119537.101.10.1999EP
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) NOVEL MALONIC ACID DERIVATIVES, PROCESSES FOR THEIR PREPARATION, THEIR USE AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM (INHIBITION OF FACTOR XA ACTIVITY)
(FR) NOUVEAUX DERIVES D'ACIDE MALONIQUE, PROCEDES DE PREPARATION DE CES DERIVES, LEUR UTILISATION ET COMPOSITIONS PHARMACEUTIQUES LES CONTENANT (INHIBITION DE L'ACTIVITE DU FACTEUR XA)
Abstract
(EN)
The present invention relates to new compounds for the inhibition of blood clotting proteins, and more particularly, to malonic acid derivatives of formula (I), 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.
(FR)
La présente invention se rapporte à de nouveaux composés permettant d'inhiber les protéines intervenant dans la coagulation sanguine, et plus particulièrement à des dérivés de l'acide malonique représentés par la formule (I), dans laquelle R(1), R(2), R(3), R(4), R(5) et R(6) sont tels que définis dans les revendications. Les composés représentés par la formule (I) sont des inhibiteurs du facteur Xa de l'enzyme de coagulation sanguine. Cette invention se rapporte également aux procédés de préparation des composés de la formule (I), aux méthodes d'inhibition de l'activité du facteur Xa et de l'inhibition de la coagulation sanguine, à l'utilisation des composés de la formule (I) dans le traitement et la prophylaxie des troubles pouvant être soignés ou empêchés par l'inhibition de l'activité du facteur Xa, tels que les troubles thromboemboliques, ainsi qu'à l'utilisation des composés de la formule (I) dans la préparation des médicaments utilisés pour soigner de tels troubles. L'invention se rapporte par ailleurs à des compositions renfermant un composé de la formule (I) mélangé ou associé à un transporteur inerte, en particulier des compositions pharmaceutiques contenant un composé de la formule (I) ainsi que des substances transporteuses et/ou auxiliaires pharmaceutiquement acceptables.
Also published as
CZPV2001-2379
ININ/PCT/2001/908/CHE
NO20012983
NZ512670
TR2001/01903
ZA200104770
Latest bibliographic data on file with the International Bureau