首页> 外国专利> Aroyloksy- og aroyltiopropanolamin-derivater anvendelige som beta-3-adrenoreseptor-agonister og antagonister for beta-1-og-beta-2-adrenoreseptorer og farmasöytiske blandinger derav

Aroyloksy- og aroyltiopropanolamin-derivater anvendelige som beta-3-adrenoreseptor-agonister og antagonister for beta-1-og-beta-2-adrenoreseptorer og farmasöytiske blandinger derav

机译:可用作β-3-肾上腺素受体激动剂和β-1-和β-2-肾上腺素受体拮抗剂的芳酰氧基和芳基硫代丙醇胺衍生物及其药物混合物

摘要

A compound formula (I) or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate thereof, wherein R0 represents an aryl group optionally substituted with one, two or three substituents selected from the list consisting of: hydroxy, hydroxymethyl, nitro, amino, alkylamino, dialkylamino, alkylsulphonamido, arylsulphonamido, formamido, halogen, alkoxy and allyl; X represents O or S; R1 and R1a each independently represents hydrogen or an alkyl group; R2 represents OCH2CO2H, or an ester or amide thereof, or R2 represents a moiety of formula (b), wherein R4 represents hydrogen, alkyl, hydroxyalkyl, arylalkyl, aryloxyalkyl, aralkyloxyalkyl or cycloalkyl and R5 represents hydroxy, alkoxy, arylalkyloxy, hydroxyalkyloxy, alkoxyalkyloxy, aryloxyalkyloxy, arylalkoxyalkyloxy or cycloalkyloxy or R5 represents hydrogen, alkyl, substituted alkyl, cycloalkyl, aryl, arylalkyl, aryloxyalkyl, arylalkyloxyalkyl or R5 together with OR4 represents O(CH2)nO, wherein n is 2, 3 or 4; and R3 represents hydrogen, halogen, alkyl or alkoxy or R3 together with R2 represents a moiety of formula (c) or an ester or amide thereof; providing that 4-[2-[2-hydroxy-3-(4-hydroxyphenoxy)propylamino]propyl]phenoxyacetic acid and salts and esters thereof and the compounds of examples 1 to 36 disclosed in EP0328251 are excluded from the scope of formula (I); a pharmaceutical composition containing such a compound, a process of preparing such a compound and the use of such a compound in medicine.
机译:化合物式(I)或其药学上可接受的盐或其药学上可接受的溶剂化物,其中R 0代表任选地被一个,两个或三个选自以下的取代基取代的芳基:羟基,羟甲基,硝基,氨基,烷基氨基,二烷基氨基,烷基磺酰胺基,芳基磺酰胺基,甲酰胺基,卤素,烷氧基和烯丙基; X代表O或S; R 1和R 1a各自独立地表示氢或烷基。 R 2代表OCH 2 CO 2 H或其酯或酰胺,或R 2代表式(b)的部分,其中R 4代表氢,烷基,羟烷基,芳基烷基,芳氧基烷基,芳烷氧基烷基或环烷基,R 5代表羟基,烷氧基,芳基烷氧基,羟基烷氧基,烷氧基烷氧基,芳氧基烷氧基,芳基烷氧基烷氧基或环烷氧基或R 5代表氢,烷基,取代的烷基,环烷基,芳基,芳基烷基,芳氧基烷基,芳基烷氧基烷基或R 5与OR 4一起>代表O(CH 2)n O,其中n为2、3或4; R 3表示氢,卤素,烷基或烷氧基或R 3与R 2一起表示式(c)的部分或其酯或酰胺。前提是将4- [2- [2-羟基-3-(4-羟基苯氧基)丙基氨基]丙基]苯氧基乙酸及其盐和酯以及EP0328251中公开的实施例1-36的化合物排除在式(I)的范围之外);包含这种化合物的药物组合物,制备这种化合物的方法以及该化合物在医学中的用途。

著录项

相似文献

  • 专利
  • 外文文献
  • 中文文献
获取专利

客服邮箱:kefu@zhangqiaokeyan.com

京公网安备:11010802029741号 ICP备案号:京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有
  • 客服微信

  • 服务号