Substituted thiazolyl and substituted pyridinyl derivatives

US5360807A · kind A · utility

Assignee

• Janssen Pharmaceutica NA · BE

Inventors

• Frans Eduard Janssens · Bonheiden, BE
• François Maria Sommen · Wortel, BE
• Gaston Stanislas Marcella Diels · Turnhout, BE

Key dates

• Filing date: Feb 17, 1994
• Grant date: Nov 1, 1994
• Expiry date: Feb 17, 2014

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D513/04
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

Substituted thiazolyl and substituted pyridinyl derivatives of formula ##STR1## the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein PA1 --A.sup.1 .dbd.A.sup.2 --A.sup.3 .dbd.A.sup.4 -- is a bivalent radical having the formula EQU --CH.dbd.CH--CH.dbd.CH-- (a-1), EQU --N.dbd.CH--CH.dbd.CH-- (a-2), EQU --CH.dbd.N--CH.dbd.CH-- (a-3), EQU --CH.dbd.CH--N.dbd.CH-- (a-4), EQU --CH.dbd.CH--CH.dbd.N-- (a-5), EQU --N.dbd.CH--N.dbd.CH-- (a-6) EQU or EQU --CH.dbd.N--CH.dbd.N-- (a-7); B represents NR.sup.1, CH.sub.2, O, S, SO or SO.sub.2 wherein R.sup.1 is hydrogen or C.sub.1-4 -alkyl; PA0 R is a radical of formula; ##STR2## wherein D is C.sub.1-4 alkanediyl; R.sup.2 is C.sub.1-6 alkyl; n is 0, 1 or 2; PA0 L is hydrogen; C.sub.1-12 alkyl; C.sub.3-6 cycloalkyl; C.sub.3-6 alkenyl optionally substituted with aryl; C.sub.1-6 alkylcarbonyl; C.sub.1-6 alkyloxycarbonyl; arylcarbonyl; arylC.sub.1-6 alkyloxycarbonyl; or a radical of formula EQU --Alk--R.sup.3 (c- 1); EQU --Alk--Y--R.sup.4 (c-2); EQU --Alk--Z.sup.1 --C(.dbd.X)--Z.sup.2 --R.sup.5 (c-3); EQU or EQU --CH.sub.2 --CHOH--CH.sub.2 --O--R.sup.6 (c-4); have antiallergic properties. Compositi…