Pharmaceutically effective novel 3,4-dihydro-1,2- and 1,3-thiozolo [4,3a] i
s
    1.
    发明授权
    Pharmaceutically effective novel 3,4-dihydro-1,2- and 1,3-thiozolo [4,3a] i s 失效
    药学有效的新型3,4-二氢-1,2-和1,3-噻唑并{8,43a {9 {0异喹啉及其制备方法

    公开(公告)号:US3979397A

    公开(公告)日:1976-09-07

    申请号:US473918

    申请日:1974-05-28

    CPC分类号: C07D513/04

    摘要: The invention relates to new thiazoloisoquinolines of the general formula (I), or salts thereof, ##SPC1##WhereinA stands for a group of the formula ##EQU1## R.sup.1 stands for hydrogen, hydroxy, alkoxy or aralkoxy, R.sup.2 stands for hydrogen, hydroxy, alkoxy or aralkoxy,R.sup.3 stands for hydrogen, alkyl, aryl, nitro, carboxy or a carboxy derivative, andY stands for oxygen, sulfur, or a group of the formula =N--R.sup.4, wherein R.sup.4 stands for hydrogen, alkyl, aryl, acyl, alkylsulfonyl or arylsulfonyl.These new compounds can be used in practice as heart medicines or respiratory analeptics.The new compounds according to the invention can be prepared as follows: an isoquinoline of the general formula (II) or a salt thereof ##SPC2##WhereinR.sup.5 stands for hydrogen, hydroxy, alkoxy or aralkoxy,R.sup.6 stands for hydrogen, hydroxy, alkoxy or aralkoxy,R.sup.7 stands for hydrogen, alkyl, aryl, carboxy or a carboxy derivative, andX stands for hydrogen, halogen or mercapto,Is reacted with a reactive carbonic acid derivative, provided that at least one of the reactants contains a sulfur atom, and/or an isoquinoline of the general formula (III) ##SPC3##wherein R.sup.5, R.sup.6 and R.sup.7 each have the same meanings as defined above, and Y' stands for oxygen, sulfur or a group of the formula =N--R.sup. 8, wherein R.sup.8 represents hydrogen, alkyl, aryl, acyl, arylsulfonyl or alkylsulfonyl, is oxidized, and/or substituents A', R.sup.5, R.sup.6 and R.sup.7 of the obtained thiazoloisoquinoline of the general formula (IA) ##SPC4##wherein A' stands for a group of the formula ##EQU2## and R.sup.5, R.sup.6, R.sup.7 and Y' each have the same meanings as defined above, are converted into those required in the end-products.

    摘要翻译: 本发明涉及通式(I)的新的噻唑并喹啉或其盐,其中A代表式-SC-基团,PARALLEL Y R1代表氢,羟基,烷氧基或芳烷氧基,R2代表氢,羟基 ,烷氧基或芳烷氧基,R3代表氢,烷基,芳基,硝基,羧基或羧基衍生物,Y代表氧,硫或式= N-R4的基团,其中R4代表氢,烷基,芳基 ,酰基,烷基磺酰基或芳基磺酰基。

    Thiazoloisoquinolines with coronary and respiratory effects
    2.
    发明授权
    Thiazoloisoquinolines with coronary and respiratory effects 失效
    具有冠状动脉和呼吸道作用的噻唑并喹啉

    公开(公告)号:US4163786A

    公开(公告)日:1979-08-07

    申请号:US869791

    申请日:1978-01-16

    IPC分类号: C07D513/04 A61K31/47

    CPC分类号: C07D513/04

    摘要: The invention relates to new thiazoloisoquinolines of the formula (I), or pharmaceutically acceptable salts thereof, ##STR1## wherein R.sup.1 is hydrogen, hydroxy, alkoxy or aralkoxy,R.sup.2 is hydrogen, hydroxy, alkoxy or aralkoxy,R.sup.3 is hydrogen, cyano, alkyl, aryl, nitro, carboxy, carboalkoxy or carboxamido, andY is oxygen, sulfur, or a group of the formula .dbd.N--R.sup.4, wherein R.sup.4 stands for hydrogen, alkyl, aryl, acyl, alkyl-sulfonyl or arysulfonyl.These new compounds can be used in practice as heart medicines or respiratory analeptics.

    摘要翻译: 本发明涉及式(I)的新型噻唑并喹啉或其药学上可接受的盐,其中R 1是氢,羟基,烷氧基或芳烷氧基,R 2是氢,羟基,烷氧基或芳烷氧基,R 3是氢, 氰基,烷基,芳基,硝基,羧基,烷氧基或甲酰胺基,Y是氧,硫或式= N-R4的基团,其中R4代表氢,烷基,芳基,酰基,烷基磺酰基或芳磺酰基。

    Highly pure amidoximes
    8.
    发明授权
    Highly pure amidoximes 失效
    高纯度amidoximes

    公开(公告)号:US5278309A

    公开(公告)日:1994-01-11

    申请号:US19603

    申请日:1993-02-19

    摘要: A pure crystalline O-(2-hydroxy-3-piperidino-1-propyl) nicotinic acid amidoxime base of the Formula (Ib) ##STR1## is disclosed characterized by a melting point of 70.degree. to 73.degree. C., giving, when dissolved in an amount of 1 to 10 ml of concentrated sulfuric acid, a yellow homogeneous solution, and showing the following spectral characteristics:IR spectrum (kBr): .gamma. --O--C.dbd.N 1642 cm.sup.-1.sup.1 H-NMR spectrum (CDCL.sub.3, .delta. ppm): 1.48 m, (6H), CH.sub.2 -piperidine; 2.42 m, (6H), 3.times.CH.sub.2 --N; 3.36, br, (1H), CH--O; 4.08 m, (3H), 1--CH.sub.2, OH; 5.2, br, (2H), NH.sub.2 ; 7.30 m (1H), pyridine-5'; 7.92 m, 4', 8.62 m (1H), 6', 8.88 m, (1H), 2'.

    摘要翻译: 公开了式(Ib)(*化学结构*)的纯结晶O-(2-羟基-3-哌啶-1-基 - 丙基)烟酰胺肟基,其特征在于熔点为70-73℃, 当溶解量为1至10ml浓硫酸时,得到黄色均匀溶液,并显示以下光谱特征:IR光谱(kBr):(γ)-OC = N 1642cm -1 1 H-NMR光谱 (CDCL3,(delta)ppm):1.48m,(6H),CH2-哌啶; 2.42m,(6H),3 * CH2-N; 3.36,br,(1H),CH-O; 4.08m,(3H),1-CH 2,OH; 5.2,br,(2H),NH2; 7.30m(1H),吡啶-5'; 7.92m,4',8.62m(1H),6',8.88m,(1H),2'。