Leukotriene B4 derivatives, process for their production and their use as pharmaceutical agents

US5859054A · kind A · utility

Assignee

• SCHERING CORPORATION · US

Inventors

• Werner Skuballa · Berlin, DE
• Bernd Buchmann · Hohen Neuendorf, DE
• Josef Heindl · Berlin, DE
• Wolfgang Frohlich · Berlin, DE
• Roland Ekerdt · Berlin, DE
• Claudia Giesen · Berlin, DE

Key dates

• Filing date: Nov 8, 1996
• Grant date: Jan 12, 1999
• Expiry date: Nov 8, 2016

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07C2601/14
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Pharmacologically active leukotriene-B.sub.4 derivatives of general formula I, ##STR1## are described, in which PA1 R.sub.1 represents CH.sub.2 OH, CH.sub.3, CF.sub.3, COOR.sub.4, CONR.sub.5 R.sub.6, or PA1 R.sub.2 represents H or an organic acid radical with 1-15 C atoms, PA1 R.sub.3 symbolizes H; C.sub.1 -C.sub.14 alkyl, C.sub.3 -C.sub.10 cycloalkyl optionally substituted singly or multiply; C.sub.6 -C.sub.10 aryl radicals, independently of one another, optionally substituted singly or multiply by halogen, phenyl, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, fluoromethyl, chloromethyl, trifluoromethyl, carbonyl, carboxyl or hydroxy; or a 5- to 6-membered aromatic heterocyclic ring with at least 1 heteroatom, PA1 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 hydroxy; CH.sub.2 --CO--(C.sub.6 -C.sub.10) aryl or a 5- to 6-membered ring with at least 1 heteroatom, PA1 A symbolizes a trans, trans--CH.dbd.CH--CH.dbd.CH, a --CH.sub.2 CH.sub.2 --CH.dbd.CH-- or a tetramet…