Diphenoxyacetic acid derivatives
    1.
    发明授权
    Diphenoxyacetic acid derivatives 失效
    二苯氧基乙酸衍生物

    公开(公告)号:US4051170A

    公开(公告)日:1977-09-27

    申请号:US531475

    申请日:1974-12-11

    摘要: Diphenoxyacetic acid derivatives of the general formula ##STR1## wherein R.sub.1 is H or alkyl of 1-4 carbon atoms, R.sub.2 is H or Cl, R.sub.2 is H or Cl, R.sub.3 is piperidino, 4-piperidinophenyl, 1,2,3,4-tetrahydroquinolino, 1-R.sub.4 -1,2,3,4-tetrahydro-4-quinolyl, 4-oxo-1,2,3,4-tetrahydroquinolino, 4-chromanyl, 4-thiochromanyl or 4-chlorophenoxy, and R.sub.4 is H or alkyl of 1-4 carbon atoms, and the physiologically acceptable salts thereof, possess cholesterol level lowering activity and can be prepared by reacting a phenol of the formula ##STR2## with a compound of the formula ##STR3## wherein X is OH, esterified OH, Cl, Br or I, one R is R.sub.2 and the other is R.sub.3 ; or by cyclizing a compound of the formula ##STR4## wherein X.sub.1 is Cl, Br, I, NH.sub.2 OH or an esterified or etherified OH-group and n is 0 or 1; or by treating a compound of the formula ##STR5## wherein Z is a functionally modified carboxyl group different from COOR.sub.1, with a solvolyzing agent, R.sub.1, R.sub.2 and R.sub.3 in each instance having the values given above.

    摘要翻译: 其中R 1为H或1-4个碳原子的烷基,R 2为H或Cl,R 2为H或Cl,R 3为哌啶子基,4-哌啶子基苯基,1,2,3,4 1-四氢喹啉,1-R4-1,2,3,4-四氢-4-喹啉基,4-氧代-1,2,3,4-四氢喹啉,4-苯并二氢吡喃基,4-硫代苯并二氢吡喃基或4-氯苯氧基,R4是 H或1-4个碳原子的烷基及其生理上可接受的盐具有降低胆固醇水平的活性,并且可以通过使下式的苯酚与下式化合物(IMAGE)反应来制备,其中X是OH, 酯化的OH,Cl,Br或I,一个R是R 2,另一个是R 3; 或者通过环化式(VI)的化合物,其中X 1是Cl,Br,I,NH 2 + L,OH或酯化或醚化的OH-基团,n是0或1; 或者通过用溶剂分解剂,R 1,R 2和R 3在每种情况下处理具有上述给定值的式“IMAGE”的化合物,其中Z是不同于COOR1的官能改性羧基。

    2-Methyl-2-[4-(4-piperidinophenyl)-phenoxy]-propionic acid
1-methyl-4-piperidyl ester
    8.
    发明授权
    2-Methyl-2-[4-(4-piperidinophenyl)-phenoxy]-propionic acid 1-methyl-4-piperidyl ester 失效
    2-甲基-2- {8 4-(4-哌啶基苯基) - 苯氧基{9-丙酸1-甲基-4-哌啶基酯

    公开(公告)号:US3956334A

    公开(公告)日:1976-05-11

    申请号:US483408

    申请日:1974-06-26

    CPC分类号: C07D295/096

    摘要: Piperidines of the formula ##SPC1##Wherein R is --CH.sub.2 OH, CO--NR,R.sub.2 in which R.sub.1 and R.sub.2 each are H or alkyl of 1-4 carbon atoms, --NHCH.sub.2 CH.sub.2 OH, --N(CH.sub.2 CH.sub.2 OH).sub.2, --NHCH.sub.2 CH.sub.2 SO.sub.3 H, --NHNH.sub.2 or --NHCH.sub.2 COOH, or --COOR.sub.3 in which R.sub.3 is 3-pyridylmethyl, 2-acetamidoethyl, 1-methyl-4-piperidyl or 2,3-dihydroxypropyl and the physiologically acceptable salts thereof, have cholesterol-level-lowering and triglyceride-level-lowering activity and can be prepared from 2-methyl-2-[4-(4-piperidinophenyl)-phenoxy]-propionic acid or a functional derivative thereof by reduction or by reaction with a compound of the formula HZ.

    摘要翻译: 式WHEREIN R是-CH 2 OH,CO-NR,R 2,其中R 1和R 2各自为H或1-4个碳原子的烷基,-NHCH 2 CH 2 OH,-N(CH 2 CH 2 OH)2,-NHCH 2 CH 2 SO 3 H,-NHNH 2或-NHCH 2 COOH 或其中R3为3-吡啶基甲基,2-乙酰氨基乙基,1-甲基-4-哌啶基或2,3-二羟基丙基的-COOR 3及其生理学上可接受的盐具有降低胆固醇含量和降低甘油三酯水平的活性, 可以由2-甲基-2- [4-(4-哌啶基苯基) - 苯氧基] - 丙酸或其官能衍生物通过还原或与式HZ的化合物反应来制备。

    Biphenylyl ethers and method of use
    9.
    发明授权
    Biphenylyl ethers and method of use 失效
    联苯醚和使用方法

    公开(公告)号:US4060609A

    公开(公告)日:1977-11-29

    申请号:US518811

    申请日:1974-10-29

    CPC分类号: C07D295/088

    摘要: Biphenylyl ethers of the formula R--O--CH.sub.2 --CR.sub.1 (OH)--CH.sub.2 Z wherein R.sub.1 is H or CH.sub.3 ; Z is dialkylamino of 2-8 carbon atoms, morpholino, pyrrolidino, piperidino, homopiperidino, hydroxypyrrolidino, hydroxypiperidino or hydroxyhomopiperidino; R is either biphenylyl substituted by at least one of F, Cl, Br, I, CF.sub.3, NO.sub.2 and piperidino or, when R.sub.1 is CH.sub.3 or when Z is homopiperidino, hydroxypyrrolidino, hydroxypiperidino or hydroxyhomopiperidino, unsubstituted biphenyl, and the physiologically acceptable acid addition salts thereof, possess cholesterol blood-level-lowering activity and can be produced by reacting a compound of the formula R--O--CH.sub.2 --Y wherein Y is ##STR1## or --CR.sub.1 (OH)--CH.sub.2 X, X being Cl, Br, I or a free or functionally modified OH-group, with an amine of the formula H-Z.

    摘要翻译: 式R-O-CH 2 -CR 1(OH)-CH 2 Z的联苯基醚,其中R 1是H或CH 3; Z是2-8个碳原子的二烷基氨基,吗啉代,吡咯烷子基,哌啶子基,高哌啶基,羟基吡咯烷基,羟基哌啶子基或羟基高哌啶子基; R是由F,Cl,Br,I,CF 3,NO 2和哌啶子中至少一种取代的联苯基,或当R 1为CH 3或Z为高哌啶基,羟基吡咯烷基,羟基哌啶子基或羟基高哌啶子基,未取代的联苯基和生理上可接受的酸加成 其盐具有胆固醇血液中降低水平的活性,并且可以通过使式RO-CH2-Y的化合物(其中Y是或-CR1(OH)-CH2X,X是Cl,Br,I或 游离的或官能改性的OH-基团与式HZ的胺反应。

    Phenoxyalkanol derivatives
    10.
    发明授权
    Phenoxyalkanol derivatives 失效
    苯氧基醇衍生物

    公开(公告)号:US4051173A

    公开(公告)日:1977-09-27

    申请号:US694447

    申请日:1976-06-09

    摘要: Phenoxylakanols of the formula ##STR1## wherein R.sup.1 is H or CH.sub.3 ; R.sup.2 is CH.sub.3 or C.sub.6 H.sub.5 ; R.sup.3 is 4-Hal-phenoxymethyl, 1,2,3,4-tetrahydro-1-naphthyl, 1-pyrryl, piperidino, isoindoline, 1,2,3,4-tetrahydroquinoline, 1,2,3,4-tetrahydro-1-R.sup.5 -4-quinolyl, 4-chromanyl, 4-thiochromanyl, or, when at least one of R.sup.1 and R.sup.2 is other than CH.sub.3, also Hal, phenyl, 4-Hal-phenyl or 4-Hal-phenoxy, wherein R.sup.4 is H or alkanoyl of 2-4 carbon atoms, R.sup.5 is H or CH.sub.3 and Hal if F, Cl or Br; and physiologically acceptable acid addition salts thereof possess pharmacological activity, particularly cholesterol, triglyceride and uric acid blood-level lowering activity and are also useful as intermediates for the production of the corresponding phenoxyacetic acids.

    摘要翻译: 其中R 1为H或CH 3的通式为“IMAGE”的苯氧基烷醇; R2是CH3或C6H5; R3是4-卤代苯氧基甲基,1,2,3,4-四氢-1-萘基,1-吡咯基,哌啶子基,异吲哚啉,1,2,3,4-四氢喹啉,1,2,3,4-四氢喹啉, 1-R5-4-喹啉基,4-苯并二氢吡喃基,4-硫代苯并二氢吡喃基,或者当R 1和R 2中的至少一个不是CH 3时,Hal,苯基,4-卤代苯基或4-卤代苯氧基,其中R4 是2-4个碳原子的H或烷酰基,R5是H或CH3,Hal如果F,Cl或Br; 其生理上可接受的酸加成盐具有药理活性,特别是胆固醇,甘油三酸酯和尿酸血液中降低水平的活性,也可用作生产相应的苯氧基乙酸的中间体。