Schering Aktiengesellschaft

Schering Aktiengesellscaft

Wolfgang Frohlich

Werner Skuballa

Bernd Buchmann

Claudia Giesen

Josef Heindl

Roland Ekerdt

Hartwig Hennekes

Stefan Jaroch

Hartmut Rehwinkel

Frank Schneider

Joseph Heindl

Rolalnd Ederdt

The invention relates to leukotriene B derivatives of general formula (I) in which R stands for CH OH, CH , CF , COOR , CONR R ; R stands for H or an organic acid radical with 1-15 C atoms; R stands for H; R is hydrogen, C -C -alkyl, C -C -cycloalkyl, a C -C -aryl radical optionally substituted by 1-3 halogen, phenyl, C -C -alkyl, C -C -alkoxy, fluoromethyl, chloromethyl, trifluoromethyl, carboxyl or hydroxy, or CH &mdash;CO&mdash;(C -C ) aryl, or a 5-6 link ring with at least 1 heteroatom; A is a trans-, trans-CH&boxH;CH&mdash;CH&boxH;CH, a &mdash;CH CH &mdash;CH&boxH;CH&mdash; or a tetramethylene group; B is a C -C linear or branched-chain aklylene group or the group (a) or (b); D is a direct bonding, oxygen, sulphur, &mdash;C&equiv;C&mdash;, &mdash;CH&boxH;CR , or a direct bonding with B. The invention also relates to salts thereof, having physiologically compatible bases and their cyclodextrin clathrates. The inventive substances can be used as pharmaceutical preparations

Leukotriene-B4 derivatives, in particular 7-methylcyclohexyl-LTB4 antagonists

Leukotriene B.sub.4 derivatives, in particular oximo-LTB.sub.4 -

9H-Pyridu ((3,4-b) indole derivatives

Leukotriene B4 derivatives, process for their production and their use

Leukotriene-B4 derivatives, process for their production and their use

Leukotriene-B.sub.4 analogs of formula I ##STR1## in which R.sup.1 means radical COOR.sup.2 with R.sup.2 meaning a hydrogen atom or a (C.sub.1 -C.sub.4)-alkyl group or R.sup.1 means radical CH.sub.2 OH,

New leukotriene-B4 Antagonists and their use as pharmaceutical agents

The present invention relates to a leukotriene-B.sub.4 analog according to formula I ##STR1## in which R.sup.1 is a COOR.sup.2 group, wherein R.sup.2 is a C.sub.2-4 -alkyl group;

Leukotriene-B.sub.4 derivatives, process for their production and their

Leukotriene-B.sub.4 derivatives of formula I ##STR1## are described, in which R.sup.1 means CH.sub.2 OH, CH.sub.3, CF.sub.3, COOR.sup.5, CONR.sup.6 R.sup.7, or R.sup.1 together with R.sup.2 means a carbonyl group, R.sup.4 symbolizes H, C.sub.1 -C.sub.10 alkyl optionally substituted, C.sub.3 -C.sub.10 cycloalkyl, C.sub.6 -C.sub.10 aryl radical optionally substituted, or a 5-6-membered aromatic heterocyclic ring, 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 alkylene group, which optionally can be substituted by fluorine or the group ##STR2## D can mean a direct bond, oxygen, sulfur, --C.tbd.C--, --CH.dbd.CR.sup.6 or together with B can also mean a direct bond, their salts with physiologically compatible bases and their cyclodextrin clathrates.

New leukotriene-B.sub.4 derivatives, process for their production and

1. Leukotriene-B.sub.4 antagonists of formula I ##STR1## are described, in which X is a CH.sub.2 group or an oxygen atom,

Leukotriene-B.sub.4 antagonist compounds and their use as pharmaceutical

##STR1## Compounds of formula (I) in which the residues have the following meanings: a is (II) or (III); R.sup.1 is CH.sub.2 OH, CH.sub.3, CF.sub.3, COOR.sup.5 with R.sup.5 or, A is a trans, trans--CH.dbd.CH--CH.dbd.CH--or tetramethylene group; B is an alkylene group with up to 10 C atoms; D is a direct bond, oxygen, sulphur, a --C.tbd.C--group or a --CH.dbd.CR.sup.7 --group, or (IV); B and D together are a direct bond; R.sup.2 and R.sup.3 are the same or different and denote hydrogen or an organic acid residue with 1 to 15 C atoms, R.sup.1 and R.sup.2 together are a carbonyl group; R.sup.4 is a hydrogen atom or C.sub.1-10 alkyl, and if R.sup.5 denotes a hydrogen atom, their salts with physiologically acceptable bases and their cyclodextrin clathrates.

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Berlin, Germany

Wolfgang Frohlich