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PHENYLPROPIONIC ACIDS AND ESTER COMPOUNDS AND METHODS FOR INDUCING BETA-BLOCKADE

机译:苯丙酸和酯类化合物以及诱导β-封锁的方法

摘要

Disclosed are compounds of formula (I) wherein R represents hydrogen or is a C-3 to C-6 cycloalkyl or C-4 to C-10 straight or branched carbon chain alkyl-cycloalkyl or a group -B-D, where B is C-2 to C-10 straight or branched carbon chain alkyl and D is hydroxy or alkyloxy or 2,3-dihydroxypropyl or 2,3-dialkyloxypropyl or 2,2-dialkyl-1,3-dioxolane-5-methyl, where alkyl is C-1 to C-10 straight or branched carbon chain; W represents CH(CH3)CH2-, C(CH3)2CH2-; Z represents hydrogen, -NHCOR2, -NHCONR2R3 or -NHSO2R2 or -NHSO2NR2R3 or -NHCOOR4 wherein R4 is alkyl of from 1 to about 6 carbon atoms, alkoxyalkyl wherein the alkyl groups may be the same or different and contain from 1 to about 6 carbon atoms, alkoxyaryl, cycloalkyl of from 3 to about 8 carbon atoms. R2 and R3 may be the same or different and represent hydrogen, alkyl of from 1 to about 6 carbon atoms, alkoxyalkyl wherein the alkyl groups may be the same or different and contain from 1 to about 6 carbon atoms, alkoxyaryl, cycloalkyl of from 3 to about 8 carbon atoms, a phenyl group substituted or unsubstituted, heteroaryl, furanyl, thiophenyl, imidazolyl, oxazolyl or indolyl or tetrahydrofuranyl, tetrahydropyranyl, dioxanyl, 2,2-dimethyl dioxolane-5-methyl, pyrrolidinyl, piperazinyl and tetrahydrooxazolyl, aralkyl except that R2 and R3 are not hydrogen when Z is -NHSO2R2, or R2 and R3 may together with N form a 5 to 7 membered heterocyclic group; and pharmaceutically acceptable salts thereof; and all stereoisomeric forms, as well as racemic mixtures. The compounds in the present invention relates to compounds, methods, formulation and pharmaceutical compositions for the general treatment or prophylaxis of diseases states which are responsive to attenuation of sympathetic nervous system activity or beta adrenergic blockade namely: coronary artery disease including myocardial ischemic disorders, angina and myocardial infarction; arrhythmia; hypertension; anxiety including panic attack; migraine or glaucoma by the intravenous or sublingual or oral or topical ocular administration.
机译:公开了其中R代表氢或为C-3至C-6环烷基或C-4至C-10直链或支链碳链烷基-环烷基或基团-BD的式(I)化合物,其中B为C- 2至C-10的直链或支链碳链烷基,且D为羟基或烷氧基或2,3-二羟丙基或2,3-二烷氧基丙基或2,2-二烷基-1,3-二氧戊环-5-甲基,其中烷基为C -1至C-10直链或支链碳链; W代表CH(CH3)CH2-,C(CH3)2CH2-; Z代表氢,-NHCOR 2,-NHCONR 2 R 3或-NHSO 2 R 2或-NHSO 2 NR 2 R 3或-NHCOOR 4,其中R 4为具有约1至约6个碳原子的烷基,其中烷氧基烷基的烷基可以相同或不同并且含有1至约6个碳原子原子,烷氧基芳基,3至约8个碳原子的环烷基。 R 2和R 3可以相同或不同,并且代表氢,1至约6个碳原子的烷基,烷氧基烷基,其中烷基可以相同或不同并且包含1至约6个碳原子,烷氧基芳基,3的环烷基到约8个碳原子,取代或未取代的苯基,杂芳基,呋喃基,噻吩基,咪唑基,恶唑基或吲哚基或四氢呋喃基,四氢吡喃基,二恶烷基,2,2-二甲基二氧戊环-5-甲基,吡咯烷基,哌嗪基和四氢恶唑基,芳烷基除外当Z为-NHSO 2 R 2时,R 2和R 3不是氢,或者R 2和R 3可以与N一起形成5至7元杂环基;及其药学上可接受的盐;以及所有立体异构形式以及外消旋混合物。本发明中的化合物涉及用于一般治疗或预防对交感神经系统活性减弱或β-肾上腺素能阻断有反应的疾病状态的化合物,方法,制剂和药物组合物,即:包括心肌缺血性疾病,心绞痛的冠状动脉疾病和心肌梗塞;心律失常;高血压;焦虑,包括惊恐发作;偏头痛或青光眼可通过静脉内或舌下或口服或局部眼部给药。

著录项

  • 公开/公告号WO0042999A1

    专利类型

  • 公开/公告日2000-07-27

    原文格式PDF

  • 申请/专利权人 SELECTUS PHARMACEUTICALS INC.;

    申请/专利号WO2000US01285

  • 发明设计人 MATIER WILLIAM L.;PATIL GHANSHYAM;

    申请日2000-01-20

  • 分类号A61K31/19;A61K31/24;A61K31/335;A61K31/34;A61K31/35;A61K31/535;C07C219/22;C07C229/34;C07D265/32;C07D307/02;C07D309/12;C07D317/34;

  • 国家 WO

  • 入库时间 2022-08-22 01:50:07

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