Title:
【発明の名称】新規のロイコトリエン―B4―誘導体、その製造法および該化合物の医薬品としての使用
Document Type and Number:
Japanese Patent JPH06500566
Kind Code:
A
Abstract:
The invention discloses new leukotriene B4 derivatives of formula (I), wherein R?1 stands for CH2?OH, CH3?, CF3?, COOR?5, CONR?6R?7, or R?1 together with R?2 stands for a carbonyl group, R?2 and R?3 are the same or different and stand for H or an organic acid residue containing 1 to 15 carbon atoms, R?4 stands for H, C1?-C10? alkyl, possibly substituted one or more times by chlorine or bromine, C3?-C10? cycloalkyl, a C6?-C10? aryl residue possibly substituted one or more times by chlorine, bromine or phenyl, C1?-C4? alkyl, C1?-C4? alkoxy, fluoromethyl, chloromethyl, trifluoromethyl, carboxy or hydroxy, or a 5- or 6-membered aromatic heterocyclic ring with at least one heteroatom, R?5 stands for hydrogen, C1?-C10? alkyl, C3?-C10? cycloalkyl, a C6?-C10? aryl residue possibly substituted one to three times by chlorine, bromine or phenyl, C1?-C4? alkyl, C1?-C4? alkoxy, fluoromethyl, chloromethyl, trifluoromethyl, carboxy or hydroxy, CH2?-CO-(C6?-C10?) aryl or a 5- or 6-membered ring with at least one heteroatom, A stands for a trans,trans-CH=CH-CH=CH, a -CH2?CH2?-CH=CH- or a tetramethylene group, B stands for a C1?-C10? straight-chain or branched-chain alkylene group, possibly substituted by fluorine, or the group of formula (a), D stands for a direct bond, oxygen, sulphur, -C=C-, -CH=CR8? or, together with B, for a direct bond, R6? and R7? are the same or different and stand for H or C1?-C4? alkyl or R7? stands for H and R6? stands for C1?-C10? alkanoyl or C1?-C10? alkanesulphonyl, R8? stands for H, C1?-C5? alkyl, chlorine or bromine, n is equal to 3 to 5 and, when R5? stands for hydrogen, their salts with physiologically tolerable bases and their cyclodextrin clathrates.
Inventors:
Sukhbara, Werner
Buchmann, Bernd
Heindle, Joseph
Frerich, Wolfgang
Ekerto, Roland
Giesen, Claudia
Buchmann, Bernd
Heindle, Joseph
Frerich, Wolfgang
Ekerto, Roland
Giesen, Claudia
Application Number:
JP50486692A
Publication Date:
January 20, 1994
Filing Date:
February 24, 1992
Export Citation:
Assignee:
Schering Aktiengesellschaft
International Classes:
A61K31/19; A61P11/00; A61P17/00; A61P29/00; A61P43/00; C07C29/40; C07C31/135; C07C31/27; C07C31/44; C07C33/12; C07C51/347; A61K31/557; C07C59/11; C07C59/13; C07C59/46; C07C69/007; C07C69/732; C07C235/40; C07C323/10; C07C405/00; C07D309/30; C07F7/18; C07C; (IPC1-7): C07C31/135; A61K31/557; C07C29/40; C07C31/27; C07C31/44; C07C51/347; C07C59/11; C07C59/13; C07C235/40; C07C323/10; C07D309/30; C07F7/18
Attorney, Agent or Firm:
Toshio Yano (2 outside)