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US 5,703,050 AGranted
Urea derivatives, their preparation and use
AssigneeHoechst Aktiengesellschaft
InventorsOtmar Klingler, Gerhard Zoller, Bernd Jablonka, Melitta Just, Gerhard Breipohl, Jochen Knolle, Wolfgang Konig, Hans Ulrich Stilz
Life of this patent
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Abstract
Urea derivates are disclosed having the formula (I). ##STR1## in which A, B, W, Z, R, R.sup.1, R.sup.2, R.sup.3 and r have the meaning given in the description, as well as a process for preparing the same and their use as inhibitors of thrombocyte aggregation, carcinom cell metastasis and osteoclast binding to bone surface.
Claims9
Urea derivatives of the formula I ##STR21## in which r denotes an integer from 0 to 1;
- Z denotes oxygen or sulphur;
- W denotes --COW.sup.1 or tetrazolyl;
- W.sup.1 denotes hydroxyl, (C.sub.1 -C.sub.4)-alkoxy, benzyloxy, amino or mono- or di-((C.sub.1 -C.sub.8)-alkyl)amino;
- A denotes ##STR22## in which n stands for an integer from 0 to 1;
- B denotes --NR.sup.b --(CH.sub.2).sub.m --CO--, in which m stands for an integer from 1 to 2;
- R.sup.a and R.sup.b independently of one another denote hydrogen, hydroxyl, (C.sub.1 -C.sub.18)-alkyl, (C.sub.6 -C.sub.14)-aryl, (C.sub.6 -C.sub.14)-aryl-(C.sub.1 -C.sub.8)-alkyl, (C.sub.1 -C.sub.28)-alkoxy, (C.sub.6 -C.sub.14)-aryloxy, or (C.sub.6 -C.sub.14)-aryl-(C.sub.1 -C.sub.8)-alkoxy;
- R denotes hydrogen or (C.sub.1 -C.sub.6)-alkyl;
- R.sup.1 denotes --NHX or --C(.dbd.NX)--NH.sub.2 ;
- X denotes hydrogen, (C.sub.1 -C.sub.6)-alkylcarbonyl, (C.sub.1 -C.sub.6)-alkoxycarbonyl, (C.sub.1 -C.sub.18)-alkylcarbonyloxy(C.sub.1 -C.sub.6)-alkoxycarbonyl, (C.sub.6 -C.sub.14)-aryl-(C.sub.1 -C.sub.6)-alkoxycarbonyl, hydroxyl, or a radical of the formula II
- R'--NH--C(.dbd.N--R")-- (II)
- where R' and R" independently of one another stand for hydrogen, (C.sub.1 -C.sub.6)-alkoxycarbonyl, (C.sub.1 -C.sub.6)-alkylcarbonyl, (C.sub.1 -C.sub.18)-alkylcarbonyloxy-(C.sub.1 -C.sub.6)-alkoxycarbonyl, (C.sub.6 -C.sub.14)-aryl-(C.sub.1 -C.sub.6)-alkoxycarbonyl or hydroxyl;
- R.sup.2 denotes hydrogen or phenyl;
- R.sup.3 denotes --CO--NH--R.sup.4, where --NH--R.sup.4 stands for the radical of an .alpha.-amino acid, its .omega.-amino-(C.sub.2 -C.sub.8)-alkylamide or its (C.sub.1 -C.sub.8)-alkyl or benzyl ester, or where R.sub.4 denotes methyl which is substituted by an amino acid side chain and also by a radical from the series --SO.sub.2 --OH, --SO.sub.2 -- NHR.sup.9 and tetrazolyl;
- R.sup.9 denotes hydrogen, aminocarbonyl, (C.sub.1 -C.sub.18)-alkylaminocarbonyl, (C.sub.3 -C.sub.8)-cycloalkylaminocarbonyl, (C.sub.1 -C.sub.18)-alkyl or (C.sub.3 -C.sub.8)-cycloalkyl;
- and their physiologically tolerable salts.
12 more elements
Dependencies are inferred from the claim text.