发明名称 PHENYLPROPIONIC ACIDS AND ESTER COMPOUNDS AND METHODS FOR INDUCING BETA-BLOCKADE
摘要 <p>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.</p>
申请公布号 WO2000042999(A1) 申请公布日期 2000.07.27
申请号 US2000001285 申请日期 2000.01.20
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