C - Chemistry – Metallurgy – 07 – C
Patent
C - Chemistry, Metallurgy
07
C
C07C 69/12 (2006.01) A61K 31/045 (2006.01) A61K 31/19 (2006.01) A61K 31/215 (2006.01) A61K 31/365 (2006.01) A61K 31/557 (2006.01) C07C 33/05 (2006.01) C07C 59/46 (2006.01) C07C 69/732 (2006.01) C07C 405/00 (2006.01) C07D 309/30 (2006.01) C08B 37/16 (2006.01)
Patent
CA 2122992
ABSTRACT OF THE DISCLOSURE Leukotriene-B4 derivatives have the formula (1), in which R1 stands for CH2OH, CH3, CF3, COOR5, CONR6R7, or R1 represents together with R2 a carbonyl group; R2 and R3 are different or the same and stand for H or an organic acid residue with 1-15 C atoms; R4 stands for H, C1-C10-alkyl, possibly substituted one or several times by chlorine or bromine, C3-C10-cycloalkyl, a C6-C10-aryl residue possible independently substituted one or several times by chlorine, bromine, phenyl, C1-C4-alkyl, C1-C4-alkoxy, fluoromethyl, chloromethyl, trifluoromethyl, carboxy or hydroxy or a 5-6 membered aromatic heterocyclic ring with at least 1 heteroatom; R5 stands for hydrogen, C1-C10-alkyl, C3-C10- cycloalkyl, an aryl residue possibly substituted by 1-3 chlorine, bromine, phenyl, C1-C4-alkyl, C1-C4-alkoxy, fluoromethyl, chloromethyl, trifluoromethyl, carboxy or hydroxy, CH2-CO-(C6-C10)aryl or a 5-6 membered ring with at least 1 heteroatom; A stands for a trans, trans-CH=CH-CH=CH, -CH2CH2-CH=CH- or a tetramethylene group; B stands for a straight or branched chain C1-C10alkylene group, possibly substituted with fluorine or the group (a); D is a direct bond, oxygen, sulphur, -C?C-, -CH = CR8 or it may represent together with B a direct bond: R6 and R7 are different or the same and stand for H or C1-C4-alkyl or R7 stands for H and R6 stands for C1-C10-alkanoyl or C1-C10-alkansulphonyl; R8 stands for H, C1-C5-alkyl, chlorine, bromine; m stands for the digits 1 or 4 and n equals 3-5. Also disclosed are the salts of these derivatives with physiologically tolerable bases, when R5 stands for hydrogen, and their cyclodextrine clathrates.
Buchmann Bernd
Ekerdt Roland
Frohlich Wolfgang
Giesen Claudia
Heindl Josef
Marks & Clerk
Schering Aktiengesellschaft
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