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US 2003/0171579 A1Published application
Urethane derivatives
OwnerWerner Mederski, Horst Juraszyk +4inventors
InventorsWerner Mederski, Horst Juraszyk, Dieter Dorsch, Christos Tsaklakidis, Johannes Gleitz, Christopher Barnes
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Abstract
The invention relates to novel compounds of formula (I), wherein R, R1 and R2 have the meaning as cited claim 1. According to the invention, the compounds are inhibitors of the coagulation factors Xa and VIIa and can be used for treating thrombosis, myocardial infarct, arteriosclerosis, inflammation, apoplexy, angina pectoris, restenosis post-angioplasty, intermittent claudication, tumours, tumour related illnesses and/or tumour metastases.
Claims18
Compounds of the formula I
- 16
- in which
- R is CN, CH2NH2, —NH—C(═NH)—NH2, —CO—N═C(NH2)2, —C(═NH)—NH2, which may also be monosubstituted by Ar′, OH, O—COA, O—COAr, OCOOA, OCOO(CH2)nN(A)2, —COO(CH2)nNA2, OCOO(CH2)mHet, COO—(CH2)m-Het, CO—C(A)2-R3, COOA, COSA, COSAr, COOAr, COOAr′, COA, COAr, COAr′ or by a conventional amino-protecting group
- 17
- R1 is R4 Ar, Ar′ or X,
- R2 is phenyl which is monosubstituted by SA, SOA, SO2A, SONHA, SO2NHA, CF3, COOA, CH2NHA, CN or OA,
- R3 is CHal3, OCOA or
- 18
- R4 is alkyl having 1-20 carbon atoms in which one or two CH2 groups may be replaced by O or S atoms and/or by —CH═CH— groups and/or 1-7 H atoms may be replaced by F,
- A is H or alkyl having 1-20 carbon atoms,
- A′ is alkyl having 1-10 carbon atoms,
- Ar is phenyl or naphthyl, each of which is unsubstituted or monosubstituted, disubstituted or trisubstituted by A′, OH, OA′, NH2, NHA′, NA′2, NO2, CF3, CN, Hal, NHCOA, COOA, CONH2, CONHA′, CONA′2, SA, SOA, SO2A, SO2NH2, SO2NHA′ or SO2NA′2,
- Ar′ is (CH2)n—Ar,
- Het is a monocyclic or bicyclic saturated, unsaturated or aromatic heterocycle having 1 to 4 N, O and/or S atoms, which may be unsubstituted or monosubstituted, disubstituted or trisubstituted by A′, OA′, NH2, NHA′, NA′2, NO2, CN, Hal, NHCOA′, NHSO2A′, COOA, CONH2, CONHA′, CONA′2, COA, SO2NH2, SA′, SOA′, SO2A′ and/or carbonyl oxygen,
- X is (CH2)nY,
- Y is COOA or
- 19
- Hal is F, Cl, Br or I,
- n is 1, 2, 3, 4, 5 or 6, and
- m is 0 or 1,
- and their pharmaceutically tolerated salts and solvates.
18 more elements
Dependencies are inferred from the claim text.