New 2,4-di:substd. derivs. of tetra:hydro-furan - are potent antagonists of platelet activating factor used for treating e.g. asthma, hypertension and inflammation

摘要

derivs. of tetrahydrofuran of formula (I) are new. (X = O or a covalent single bond either the CH2XR1 gp. is in position 2 and the CH2OR2 gp. is in position 4 or the CH2XR1 gp. is in position 4 and the CH2OR2 gp. is in position 2 either R1 is alk(en)yl or alkynyl gp. of 10-24C or R1 is CONR3R4 and X is O, where R3 is alkyl, alkenyl or alkynyl gp. of 10-24C and R4 is H, 1-4C alkyl, 1-4C acyl, haloacetyl or 1-4C alkoxycarbonyl R2 = -Y-(CH2)n-Q.(A-)q Y = a single covalent bond, -C(O)-, -C(O)0 or C(O)NR4 n = 0-10 Q = a neutral heterocycle gp. contg. a non-quaternary N atom and connected to the alkylene chain by a ring C (in which case Q is represented by Q' and q = O) or Q is the same as Q' but quaternised (in which case Q is represented by Q ' ' (+) and q = 1) or Q is a heterocyclic gp. connected to the alkylene chain by a quaternary N (in which case Q is represented by Q''' (+) and q = 1) Q may opt. contain further N atoms, one or more O or S atoms, and may be substd. by one or more 1-6C alkyl, 1-6C alkoxy, carbamoyl, 1-6C hydroxyalkyl or halogen A- = a pharmaceutically acceptable anion such as halide, 1-10C alkyl sulphonate, aryl sulphonate or carboxylate).