Patent ID: 6160012
Filing Date: 2000-12-12
Classification: A61P,C07C,C07D

Abstract:
Leukotriene-B.sub.4 derivatives of general formula I ##STR18## in which R.sub.1 represents H, CF.sub.3, CH.sub.2 OH, COOR.sub.4, CONR.sub.5 R.sub.6, andR.sub.2 represents H or an organic acid radical with 1-15 C atoms,R.sub.3 symbolizes H; C.sub.1 -C.sub.14 alkyl, C.sub.3 -C.sub.10 cycloalkyl optionally substituted in one or more places; C.sub.6 -C.sub.10 aryl radicals, independently of one another, optionally substituted in one or more places by halogen, phenyl, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, fluoromethyl, chloromethyl, trifluoromethyl, carbonyl, carboxyl or hydroxyl; or a 5- to 6-membered aromatic heterocyclic ring with at least 1 heteroatom,R.sub.4 means hydrogen, C.sub.1 -C.sub.10 alkyl, C.sub.3 -C.sub.10 cycloalkyl; C.sub.6 -C.sub.10 aryl radicals optionally substituted by 1-3 halogen, phenyl, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, fluoromethyl, chloromethyl, trifluoromethyl, carboxyl or hydroxyl; CH.sub.2 --CO--(C.sub.6 -C.sub.10) aryl or a 5- to 6-membered ring with at least 1 heteroatom,A symbolizes a trans, trans--CH.dbd.CH--CH.dbd.CH, a --CH.sub.2 CH.sub.2 --CH.dbd.CH-- or a tetramethylene group,B symbolizes a C.sub.1 -C.sub.10 straight-chain or branched-chain alkylene group, which optionally can be substituted by fluorine or the group ##STR19## D means a direct bond, oxygen, sulfur, --C.tbd.C--, --CH.dbd.CR.sub.7, or together with B can also mean a direct bond,R.sub.5 and R.sub.6 are the same or different, and represent H or C.sub.1 -C.sub.4 alkyl optionally substituted by hydroxyl groups, or R.sub.6 represents H and R.sub.5 represents C.sub.1 -C.sub.15 alkanoyl or R.sub.8 SO.sub.2,R.sub.7 means H, C.sub.1 -C.sub.5 alkyl, chlorine, bromine,R.sub.8 has the same meaning as R.sub.3,m means 1-3,o means 0-5,p means 0-5,X is a direct bond, oxygen, sulfur, an aromatic compound or heteroaromatic compound,Y is a C.sub.1 -C.sub.8 alkyl optionally substituted in one or more places, C.sub.3 -C.sub.10 cycloalkyl, optionally substituted by aryl,n is 2-5,and, if R.sub.4 means hydrogen, their salts with physiologically compatible bases and their cyclodextrin clathrates.