公开(公告)号：US5149717A

公开(公告)日：1992-09-22

申请号：US795227

申请日：1991-11-15

Applicant: Andreas von Sprecher ,  Andreas Beck ,  Bruno Schaub ,  Robert W. Lang

Inventor： Andreas von Sprecher ,  Andreas Beck ,  Bruno Schaub ,  Robert W. Lang

IPC: C07D311/24 ,  C07D405/04

CPC classification number: C07D405/04 ,  C07D311/24

Abstract: Substituted alkanophenones of general formula ##STR1## in which R.sub.1 is unsubstituted or fluorinated lower alkyl, R.sub.2 is hydrogen, or unsubstituted or fluorinated lower alkyl or lower alkenyl, X is lower alkylene, oxy, thio or a direct bond, alk is lower alkylene, n is 1 or 2, R.sub.3 is phenyl that is unsubstituted or is substituted by unsubstituted or fluorinated lower alkyl, by etherified or esterified hydroxy, by unsubstituted or lower alkylated amino and/or by free, esterified or amidated carboxy, or is lower alkyl that is unsubstituted, substituted by fluoro and chloro or substituted by free esterified or amidated carboxy, R.sub.4 is free, esterified or amidated carboxy or 5-tetrazolyl, and R.sub.5 is hydrogen or lower alkyl, have leucotriene-antagonistic properties and can be used as anti-allergic active ingredients in medicaments.

Abstract translation: 其中R 1为未取代或氟化的低级烷基，R 2为氢或未取代或氟化的低级烷基或低级烯基，X为低级亚烷基，氧基，硫基或直接键的通式为（Ⅰ）的取代的烷基苯醌， 低级亚烷基，n是1或2，R3是未取代的或被未取代或氟化的低级烷基取代的苯基，被醚化或酯化的羟基，被未取代或低级烷基化的氨基和/或被游离的，酯化的或酰胺化的羧基取代，或者是 未取代的低级烷基，被氟和氯取代或被游离的酯化或酰胺化的羧基取代，R4是游离的，酯化的或酰胺化的羧基或5-四唑基，R 5是氢或低级烷基，具有白三烯拮抗性质，并且可以使用 作为药物中的抗过敏活性成分。

公开(公告)号：US4820726A

公开(公告)日：1989-04-11

申请号：US3156

申请日：1987-01-14

Applicant: Andreas Beck ,  Alfred Sallmann ,  Robert W. Lang ,  Paul Wenk

Inventor： Andreas Beck ,  Alfred Sallmann ,  Robert W. Lang ,  Paul Wenk

IPC: C07C39/24 ,  C07C43/225 ,  C07C43/23 ,  C07C45/46 ,  C07C45/71 ,  C07C49/825 ,  C07C49/84 ,  C07C205/37 ,  C07D257/04 ,  C07C103/14 ,  A61K31/165

CPC classification number: C07D257/04 ,  C07C205/37 ,  C07C39/24 ,  C07C39/245 ,  C07C43/225 ,  C07C43/23 ,  C07C45/46 ,  C07C45/71 ,  C07C49/825 ,  C07C49/84

Abstract: 4-Acylresorcinol esthers of the formula ##STR1## in which R.sub.1 is lower alkyl, R.sub.2 is fluorinated lower alkyl, R.sub.3 is hydrogen, lower alkoxy, trifluoromethyl or halogen, alk is an alkylene or hydroxyalkylene radical which is uninterrupted or interrupted by oxygen, one of the radicals R.sub.4, R.sub.5 and R.sub.7 is a group of the formula --NH--C(.dbd.O)--R.sub.8, a radical R.sub.4 or R.sub.5 which differs from this is a radical R.sub.9 and a radical R.sub.7 which differs from this is a radical R.sub.10, R.sub.6 is hydrogen, lower alkyl, trifluoromethyl, halogen, carboxyl which is free, esterified or amidated, cyano or lower alkanoyl, R.sub.8 is carboxyl which is free, esterified or amidated or 5-tetrazolyl, R.sub.9 is hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl and R.sub.10 is hydrogen, lower alkyl, lower alkoxy, halogen, trifluoromethyl, cyano or carboxyl which is free, esterified or amidated, and their salts have antiallergic and antiinflammatory properties. They are prepared, for example, by reacting compounds of the formulae ##STR2## in which one of the radicals X.sub.5 and X.sub.6 is hydroxyl which is free or in salt form and the other is an alkoxy radical substituted by reactive esterified hydroxy or epoxy. The invention also relates to intermediates of the formula ##STR3## in which R.sub.2 is fluorinated lower alkyl, R.sub.3 is hydrogen, lower alkoxy, trifluoromethyl or halogen and R.sub.11 is hydrogen or a group of the formula R.sub.1 --C(--O)--, in which R.sub.1 is lower alkyl, and their salts.

Abstract translation: 其中R 1是低级烷基，R 2是氟化的低级烷基，R 3是氢，低级烷氧基，三氟甲基或卤素的式（Ⅰ）的4-酰基间苯二酚衍生物，alk是不间断或中断的亚烷基或羟基亚烷基 氧，基团R4，R5和R7之一是式-NH-C（= O）-R8的基团，与此不同的基团R 4或R 5是基团R 9和与此不同的基团R 7， 基团R 10，R 6为氢，低级烷基，三氟甲基，卤素，羧基，其游离，酯化或酰胺化，氰基或低级烷酰基，R8为羧基，其为游离的，酯化的或酰胺化的或5-四唑基，R 9为氢，低级烷基 ，低级烷氧基，卤素或三氟甲基，R 10是氢，低级烷基，低级烷氧基，卤素，三氟甲基，氰基或羧基，它们是游离的，酯化的或酰胺化的，并且它们的盐具有抗过敏和抗炎性质。 它们例如通过使其中一个基团X5和X6是游离的或盐形式的羟基的另一种是由活性酯化的羟基或环氧基取代的烷氧基使式（Ⅰ）的化合物反应而制备。 本发明还涉及其中R 2是氟化的低级烷基，R 3是氢，低级烷氧基，三氟甲基或卤素，R 11是氢或式R 1 -C（-O）的基团的式（ⅩⅩⅢ）中间体， - ，其中R1是低级烷基，及其盐。