Tri-substituted phenyl derivatives useful as PDE IV inhibitors

US5849770A · kind A · utility

Assignee

• Celltech Therapeutics Limited · GB

Inventors

• John Clifford Head · Maidenhead, GB
• James Thomas Reuberson · Slough, GB

Key dates

• Filing date: Dec 20, 1996
• Grant date: Dec 15, 1998
• Expiry date: Dec 20, 2016

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61P43/00
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Tri-substituted phenyl derivatives and pharmaceutical compositions containing them. In a preferred embodiment, the compounds have the general formula (2): ##STR1## wherein L is preferably --OR; R.sup.a is preferably an optionally substituted alkyl group; R is preferably an optionally substituted cycloalkyl group; R.sup.3 is preferably hydrogen; hydrogen, R.sup.4 is preferably --(CH.sub.2).sub.t Ar, --(CH.sub.2).sub.t --Ar--(L.sup.1).sub.n --Ar' or --(CH.sub.2).sub.t ArN(R.sup.b)CX.sup.1 N(R.sup.b)L.sup.2 (Alk).sub.m Ar; R.sup.5 is preferably --(CH.sub.2).sub.t Ar, --(CH.sub.2).sub.t --Ar--(L.sup.1).sub.n --Ar' or --(CH.sub.2).sub.t ArN(R.sup.b)CX.sup.1 N(R.sup.b)L.sup.2 (Alk).sub.m Ar; R.sup.6 and R.sup.7 are preferably hydrogen, L.sup.1 and L.sup.2 are preferably divalent linking groups; Ar is preferably a monocyclic or bicyclic aryl or heteroaryl group; and Ar' is preferably Ar or an Ar containing group. Compounds of the invention are potent and selective phosphodiesterase type IV inhibitors and are useful in the prophylaxis and treatment of various diseases, such as asthma, which are associated with an unwanted inflammatory response or muscular spasm.