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

US6340706B1 · kind B1 · utility

Assignee

• SCHERING CORPORATION · US

Inventors

• Bernd Buchmann · Hohen Neuendorf, DE
• Wolfgang Frohlich · Berlin, DE
• Claudia Giesen · Berlin, DE
• Hartwig Hennekes · Berlin, DE
• Stefan Jaroch · Berlin, DE
• Werner Skuballa · Berlin, DE

Key dates

• Filing date: Mar 10, 2000
• Grant date: Jan 22, 2002
• Expiry date: Mar 10, 2020

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07C405/00
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The invention relates to leukotriene B4 derivatives of general formula (I) in which R1 stands for CH2OH, CH3, CF3, COOR4, CONR5R6; R2 stands for H or an organic acid radical with 1-15 C atoms; R3 stands for H; R4 is hydrogen, C1-C10-alkyl, C3-C10-cycloalkyl, a C6-C10-aryl radical optionally substituted by 1-3 halogen, phenyl, C1-C4-alkyl, C1-C4-alkoxy, fluoromethyl, chloromethyl, trifluoromethyl, carboxyl or hydroxy, or CH2—CO—(C6-C10) aryl, or a 5-6 link ring with at least 1 heteroatom; A is a trans-, trans-CH═CH—CH═CH, a —CH2CH2—CH═CH— or a tetramethylene group; B is a C1-C10 linear or branched-chain aklylene group or the group (a) or (b); D is a direct bonding, oxygen, sulphur, —C≡C—, —CH═CR7, 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