BENZISOXAZOLES AND PHENONES AS ALFA-2-ANTAGONISTS, A PROCESS FOR THEIR PREPARATION, PHARMACEUTICAL COMPOSITIONS AND THE USE OF THE SAME FOR THE MANUFACTURE OF A MEDICINAL PRODUCT.
Реферат: La presente invencion se relaciona con compuestos de formula (1) las formas N-oxido, las sales de adicion farmacéuticamente aceptables y las formasestereoquímicamente isoméricas de los mismos, en donde Alk es alcanodiilo C5-12; n es 1 o 2; p es 1 yq es 2; o p es 2 y q es 1; X es -O-, -S-,-S(=O)-,-S(=O)2- o NR2 cada R1 es independientemente hidrogeno, halogeno, alquilo C1-6, nitro, hidroxi o alquiloxi C1-4; R2 es hidrogeno, alquilo C1-6, arilo o alquiloC1-6 sustituido con arilo; arilo esfenilo o fenilo sustituido con un halogeno o alquilo C1-6; D es un 3-bencisoxazolilo o benzofenona opcionalmente sustituida; que tienen actividad antagonista de alfa2-receptores adrenérgicos centrales. Además se relaciona con su preparacion, con suuso far macéutico y concomposiciones. The present invention relates to compounds of formula (1) N-oxide forms, pharmaceutically acceptable addition salts and stereochemically isomeric forms thereof, wherein Alk is C5-12 alkanediyl; n is 1 or 2; p is 1 and q is 2; or p is 2 and q is 1; X is -O-, -S -, - S (= O) -, - S (= O) 2- or NR2 each R1 is independently hydrogen, halogen, C1-6 alkyl, nitro, hydroxy or C1-4 alkyloxy; R2 is hydrogen, C1-6 alkyl, aryl or C1-6 alkyl substituted with aryl; sphenyl or phenyl aryl substituted with a halogen or C1-6 alkyl; D is an optionally substituted 3-bencisoxazolyl or benzophenone; which have antagonistic activity of central alpha2-adrenergic receptors. It is also related to its preparation, with its pharmaceutical pharmaceutical and concompositions.
Fused heteroalkylene quinolinamines, a process and intermediates for their preparation and their use as medicaments
Номер патента: EP0287977B1. Автор: Gregory Michael Shutske,Richard Charles Effland. Владелец: Hoechst Roussel Pharmaceuticals Inc. Дата публикации: 1994-06-29.