申请人:Janssen Pharmaceutica N.V.
公开号:US05595988A1
公开(公告)日:1997-01-21
Antiallergic triazolo(pyrrolo, thieno or furano)azepines of formula ##STR1## the pharmaceutically acceptable addition salts and stereochemically isomeric forms thereof, wherein each of the dotted lines independently represents an optional bond; -E-G- is a bivalent radical of formula --X--C(R.sup.1).dbd.CH-- (a-1); or --CH.dbd.C(R.sup.2)--X-- (a-2); X represents O, S or NR.sup.3 ; R.sup.3 represents hydrogen, C.sub.1-6 alkyl or C.sub.1-4 alkylcarbonyl; -B.dbd.D- is a bivalent radical of formula --C(R.sup.4).dbd.N-- (b-1); or --N.dbd.C(R.sup.5)-- (b-2); L represents hydrogen; C.sub.1-6 alkyl; substituted C.sub.1-6 alkyl; C.sub.3-6 alkenyl; C.sub.3-6 alkenyl substituted with aryl; or, L represents a radical of formula -Alk-Y-Het.sup.1 (c-1), -Alk-NH--CO-Het.sup.2 (c-2) or -Alk-Het.sup.3 (c-3). Compositions comprising said compounds, processes of preparing the same and intermediates in the preparation thereof.
抗过敏的三唑环(吡咯、噻吩或呋喃)氮杂环庚烷化合物的化学式为##STR1## 其中,每个虚线独立表示可选键;-E-G-是化学式--X--C(R1).dbd.CH--(a-1)或--CH.dbd.C(R2)--X--(a-2)的二价基团;X代表O、S或NR3;R3代表氢、C1-6烷基或C1-4烷基羰基;-B.dbd.D-是化学式--C(R4).dbd.N--(b-1)或--N.dbd.C(R5)--(b-2)的二价基团;L代表氢、C1-6烷基、取代的C1-6烷基、C3-6烯基、带芳基的取代的C3-6烯基;或者,L代表化学式-Alk-Y-Het1(c-1)、-Alk-NH--CO-Het2(c-2)或-Alk-Het3(c-3)的基团。包含上述化合物的组合物,其制备过程及制备中的中间体。