Login| Sign Up| Help| Contact|

Patent Searching and Data


Title:
PYRROLIDINO-1,2-DICARBOXY-1-(PHENYLAMIDE)-2-(4-(3-OXO-MORPHOLINO-4-YL)-PHENYLAMIDE) DERIVATIVES AND RELATED COMPOUNDS FOR USE AS INHIBITORS OF COAGULATION FACTOR XA IN THE TREATMENT OF THROMBO-EMBOLIC DISEASES
Document Type and Number:
WIPO Patent Application WO2004087646
Kind Code:
A3
Abstract:
The invention relates to the compounds of formula (I), wherein W represents N, CR<3>, or a sp<2 >hybridized C atom, E, together with W, represents a 3- to 7-membered saturated carbocylic or heterocyclic ring having 0 to 3 N atoms, 0 to 2 O atoms and/or 0 to 2 S atoms, which ring may contain a double bond, D represents a mononuclear or binuclear unsubstituted aromatic carbocycle or heterocycle having 0 to 4 N atoms, O atoms and/or S atoms or being monosubstituted or polysubstituted by Hal, A, OR<3>, N(R<3>)2, NO2, CN, COOR<3> or CON(R<3>)2, G represents -[C(R<4>)2]n-, -[C(R<4>)2]nNR<3>-, -[C(R<4>)2]nO-, -[C(R<4>)2]nS- or -[C(R<4>)=C(R<4>)]n-, X represents -[C(R<4>)2]nCONR<3>[C(R<4>)2]n-, -[C(R<4>)2]nNR<3>CO[C(R<4>)2]n-, -[C(R<4>)2]nNR<3>[C(R<4>)2]n-, -[C(R<4>)2]nO[C(R<4>)2]n-, -[C(R<4>)2]nCO[C(R<4>)2]n- or -[C(R<4>)2]nCOO[C(R<4>)2]n-, Y represents alkylene, cycloalkylene, Het-diyl or Ar-diyl, T represents a mononuclear or binuclear saturated or unsaturated carbocycle or heterocycle having 0 to 4 N atoms, O atoms and/or S atoms, which is monosubstituted or polysubstituted by =O, =S, =NR<3>, =N-CN, =N-NO2, =NOR<3>, =NCOR<3>, =NCOOR<3>, =NOCOR<3> and which may further be monosubstituted, disubstituted or trisubstituted by R<3>, Hal, A,-[C(R<4>)2]n, -Ar, -[C(R<4>)2]n-het, -[C(R<4>)2]n-cycloalkyl, OR<3>, N(R<3>)2, NO2, CN, COOR<3>, CON(R<3>)2, NR<3>COA, NR<3>CON(R<3>)2, NR<3>SO2A, COR<3>, SO2NR<3> and/or S(O)nA, and R<1> and R<2> are defined as in claim 1. The inventive compounds inhibit coagulation factor Xa and can be used in the prophylaxis and/or therapy of thrombo-embolic diseases and for treating tumors.

Inventors:
TSAKLAKIDIS CHRISTOS (DE)
DORSCH DIETER (DE)
MEDERSKI WERNER (DE)
CEZANNE BERTRAM (DE)
GLEITZ JOHANNES (DE)
Application Number:
EP2004002350W
Publication Date:
January 06, 2005
Filing Date:
March 08, 2004
Export Citation:
Click for automatic bibliography generation   Help
Assignee:
MERCK PATENT GMBH (DE)
TSAKLAKIDIS CHRISTOS (DE)
DORSCH DIETER (DE)
MEDERSKI WERNER (DE)
CEZANNE BERTRAM (DE)
GLEITZ JOHANNES (DE)
International Classes:
A61K31/4439; A61K31/444; A61K31/5377; A61P7/02; A61P9/10; A61P25/06; A61P29/00; A61P35/00; C07C275/26; C07D265/32; C07D401/12; C07D401/14; C07D413/12; C07D413/14; C07D417/12; C07D; (IPC1-7): C07D265/32; C07D413/12; C07D413/14; C07D417/12; C07D401/14; C07D401/12; C07C275/26; A61K31/5377; A61K31/444; A61K31/4439; A61P7/02
Domestic Patent References:
WO2001064642A22001-09-07
WO2000071516A22000-11-30
WO2002022575A12002-03-21
WO2002074735A22002-09-26
WO2002014308A12002-02-21
WO2002057236A12002-07-25
WO2002048099A12002-06-20
WO1995023609A11995-09-08
WO2000039118A12000-07-06
WO2002083624A12002-10-24
WO2003045912A12003-06-05
WO2003050088A12003-06-19
Foreign References:
US5691356A1997-11-25
GB1503244A1978-03-08
Other References:
DATABASE BEILSTEIN BEILSTEIN INSTITUTE FOR ORGANIC CHEMISTRY, FRANKFURT-MAIN, DE; 27 June 1988 (1988-06-27), XP002282645, Database accession no. BRN 88135
DATABASE BEILSTEIN BEILSTEIN INSTITUTE FOR ORGANIC CHEMISTRY, FRANKFURT-MAIN, DE; 27 June 1988 (1988-06-27), XP002282646, Database accession no. BRN 102211
DATABASE BEILSTEIN BEILSTEIN INSTITUTE FOR ORGANIC CHEMISTRY, FRANKFURT-MAIN, DE; 19 March 1991 (1991-03-19), XP002282647, Database accession no. BRN 3971830
DATABASE BEILSTEIN BEILSTEIN INSTITUTE FOR ORGANIC CHEMISTRY, FRANKFURT-MAIN, DE; 9 August 1996 (1996-08-09), XP002283422, Database accession no. BRN 7437586
Download PDF: