1,4-dihydropyridine compounds with PAF-antagonistic activity

Details 1,4-dihydropyridine compounds with PAF-antagonistic activity 1,4-dihydropyridine compounds with PAF-antagonistic activity

1992-08-03

1994-03-29

Ivy, C. Warren

Organic compounds -- part of the class 532-570 series

Organic compounds

Four or more ring nitrogens in the bicyclo ring system

546283, 546322, C07D21186

Patent

active

052986195

ABSTRACT:
4-alkyl-1,4-dihydropyridines with activity antagonistic of the PAF-"acether" of formula (I) are described, in which R is a saturated alkyl chain C1-2; R' is a saturated or unsaturated C1-16 lineal, branched or cyclic chain that can be interrupted by an oxygen atom and can also represent a 2-(N-morpholine) ethyl group; n is 2 or 3, X is oxygen, sulphur or SO2; Ar represents an aromatic ring that cannot be phenyl when X=S and n=2. The compounds (I) can be prepared (a) by reaction of (II) with (III) and with (IV); or (b) by reacting (V) with (VI) and (IV); or (c) by reaction of (VII) with (VI). In these formulas the different radicals have the meaning given above.
Compounds of formula (I) are used for the treatment of pathologic states and disorders in which the PAF-"acether" participates, being used, for example, in treatment of inflammatory processes, psoriasis, glomerulitis, transplant rejection, acute and chronic bronchitis, bronchial asthma, states of shock and allergies Likewise it is used for the treatment of pathologic states and disorders in which it is necessary to stimulate the cellular immunity such as in immunodeficient syndromes and other situations in which the defense capacity is reduced. ##STR1##

REFERENCES:
Sunkel, Journal of Med. Chem., vol. 33, No. 12, Dec. 1990, pp. 3205-3210.
Sunkel, Chem. Abstracts, vol. 111, No. 25, Abstract No. 232,582e, Dec. 18, 1989, p. 767.
Ortega et al., J. of Pharm. & Exp. Ther., vol. 255, No. 1, 1990, pp. 28-33.
Gallardo et al, J. of Pharm & Exp. Ther.: vol. 255, No. 1 1990, pp. 34-39.

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