利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

38 条记录 (耗时 0.025 秒)

    1,2,4-Oxadiazine derivatives, process for their preparation and pharmaceutical compositions containing them
    3.
    发明授权
    1,2,4-Oxadiazine derivatives, process for their preparation and pharmaceutical compositions containing them 失效
    1,2,4-恶二嗪衍生物，其制备方法和含有它们的药物组合物

    公开(公告)号：US4308270A

    公开(公告)日：1981-12-29

    申请号：US196034

    申请日：1980-10-10

    申请人： Kalman Takacs ,  Antal Simay ,  Ilona Kiss nee Ajzert ,  Peter L. Nagy ,  Maria Hetyey nee Papp ,  Marian Escery nee Puskas ,  Jozsef Szegy ,  Sandor Virag ,  Sandor J. Nagy

    发明人： Kalman Takacs ,  Antal Simay ,  Ilona Kiss nee Ajzert ,  Peter L. Nagy ,  Maria Hetyey nee Papp ,  Marian Escery nee Puskas ,  Jozsef Szegy ,  Sandor Virag ,  Sandor J. Nagy

    IPC分类号： A61K31/535 ,  A61P7/10 ,  A61P9/00 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P29/00 ,  C07D273/04 ,  C07D413/06

    CPC分类号： C07D273/04 ,  Y10S514/821 ,  Y10S514/869

    摘要： The invention concerns new compounds of the general formula (I) ##STR1## wherein R.sup.1 is hydrogen or phenyl optionally substituted by one or more of the following substituents: alkyl having 1 to 4 carbon atoms, halogen, alkoxy having 1 to 4 carbon atoms or nitro;R.sup.2 is alkyl having 1 to 4 carbon atoms, cycloalkyl having 5 to 7 carbon atoms or phenyl, optionally substituted with one or more of the following groups: alkyl having 1 to 4 carbon atoms, halogen, alkoxy having 1 to 4 carbon atoms or nitro; or R.sup.2 is a naphthyl group;R.sup.3 is alkyl having 1 to 4 carbon atoms, acyl or hydrogen;R.sup.4 hydrogen or alkyl having 1 to 4 carbon atoms;R.sup.5 is cycloalkyl having 5 to 7 carbon atoms, alkyl having 1 to 6 carbon atoms, phenyl-(C.sub.1-4 -alkyl) in which the phenyl moiety may optionally be substituted with alkoxy having 1 to 4 carbon atoms, halogen or nitro;or R.sup.4 and R.sup.5 together represent a group of the general formula (V) ##STR2## wherein R.sup.6 is hydrogen or alkoxy having 1 to 4 carbon atoms, m and n stand for 0, 1 or 2and acid addition and quaternary salts thereof.The compounds of the general formula (I) are potent peripheral vasodilators and hypotensive agents. They increase the coronary blood flow and in addition to their slight antiinflammatory and diuretic acidivity possess strong antiarrhythmic properties.A process for the preparation of these compounds and pharmaceutical compositions containing them are also within the scope of the invention.

    摘要翻译： 本发明涉及通式（I）的新化合物其中R 1为氢或任选被一个或多个下述取代基取代的苯基：具有1-4个碳原子的烷基，卤素，具有1-4个碳原子的烷氧基 碳原子或硝基; R 2是具有1至4个碳原子的烷基，具有5至7个碳原子的环烷基或苯基，任选被一个或多个下列基团取代：具有1至4个碳原子的烷基，卤素，具有1至4个碳原子的烷氧基或硝基 ; 或R 2为萘基; R3是具有1-4个碳原子的烷基，酰基或氢; R4是氢或具有1-4个碳原子的烷基; R5是具有5至7个碳原子的环烷基，具有1至6个碳原子的烷基，苯基部分可任选地被具有1至4个碳原子的烷氧基取代的苯基 - （C 1-4 - 烷基），卤素或硝基; 或者R 4和R 5一起表示通式（V）的基团，其中R 6是氢或具有1至4个碳原子的烷氧基，m和n代表0,1或2，酸加成和季盐 其中。 通式（I）的化合物是有效的外周血管扩张剂和降压药。 它们增加冠状动脉血流量，除了其轻微的抗炎和利尿酸性之外，具有强烈的抗心律失常性质。 制备这些化合物的方法和含有它们的药物组合物也在本发明的范围内。

    Antiphlogistic and anticoagulant condensed pyrimidine derivatives
    7.
    发明授权
    Antiphlogistic and anticoagulant condensed pyrimidine derivatives 失效
    消炎和抗凝血嘧啶衍生物

    公开(公告)号：US4460771A

    公开(公告)日：1984-07-17

    申请号：US742464

    申请日：1976-11-17

    申请人： Zoltan Meszaros ,  Jozsef Knoll ,  Peter Szentmiklosi ,  Istvan Hermes ,  Agnes Horvath ,  Sandor Virag ,  Lelle Vasvari nee Debreczy ,  Agoston David

    发明人： Zoltan Meszaros ,  Jozsef Knoll ,  Peter Szentmiklosi ,  Istvan Hermes ,  Agnes Horvath ,  Sandor Virag ,  Lelle Vasvari nee Debreczy ,  Agoston David

    IPC分类号： A61K31/505 ,  A61K31/519 ,  A61P7/02 ,  A61P25/04 ,  A61P29/00 ,  A61P43/00 ,  C07D471/04

    CPC分类号： C07D471/04

    摘要： New optionally racemic or optically active pyrimido(1,2a) heterocyclic compounds of the formula ##STR1## wherein m is 0, 1 or 2,n is 0, 1 or 2,R is an alkyl group containing one to six carbon atoms,R.sup.1 is hydrogen, alkyl containing one to six carbon atoms,R.sup.2 is hydrogen, alkyl containing one to six carbon atoms, optionally substituted amino, optionally substituted hydroxy, carboxy or a group derived from a carboxylic acid orR.sup.1 and R.sup.2 together form a --(CH.dbd.CH).sub.2 -- group attached to the two adjacent carbon atoms of the ring A and the broken line represents a chemical bond,R.sup.3 is hydrogen, optionally substituted alkyl, optionally substituted aryl, optionally substituted aralkyl, optionally substituted heterocycle, optionally substituted cycloalkyl, optionally substituted acyl or optionally substituted hydroxy,R.sup.4 is hydrogen, optionally substituted alkyl, optionally substituted aryl, optionally substituted aralkyl, optionally substituted heterocycle, optionally substituted cycloalkyl, optionally substituted acyl orR.sup.3 and R.sup.4 together with the nitrogen can form an optionally substituted five-, six- or seven-membered ring, which can contain a further heteroatom or heteroatoms,R.sup.5 is oxygen or an optionally substituted imino group are disclosed as well as a process for the preparation thereof.

    摘要翻译： 新的任选的外消旋或光学活性嘧啶（1,2a）杂环化合物，其中m为0,1或2，n为0,1或2，R为含有1至6个碳原子的烷基，R 1为 是氢，含有1至6个碳原子的烷基，R 2是氢，含1至6个碳原子的烷基，任选取代的氨基，任选取代的羟基，羧基或衍生自羧酸的基团或R 1和R 2一起形成 - （CH = CH）连接到环A的两个相邻碳原子上的2-基团，虚线表示化学键，R 3是氢，任选取代的烷基，任选取代的芳基，任选取代的芳烷基，任选取代的杂环，任选取代的环烷基， 任选取代的酰基或任选取代的羟基，R 4是氢，任选取代的烷基，任选取代的芳基，任选取代的芳烷基，任选取代的杂环，任选取代的环烷基，选择 可以将氮取代的酰基或R3和R4与氮一起形成任选取代的五元，六元或七元环，其可以含有另外的杂原子或杂原子，R5是氧或任选取代的亚氨基， 其制备方法。

    13-Thia-prostacycline derivatives
    9.
    发明授权
    13-Thia-prostacycline derivatives 失效
    13-前列环素衍生物

    公开(公告)号：US4425358A

    公开(公告)日：1984-01-10

    申请号：US370503

    申请日：1982-04-21

    申请人： Csaba Szantay ,  Lajos Novak ,  Jozsef Aszodi ,  Vilmos Simonidesz ,  Geza Galambos ,  Gabor Kovacs ,  Sandor Virag ,  Istvan Stadler ,  Peter Kormoczy

    发明人： Csaba Szantay ,  Lajos Novak ,  Jozsef Aszodi ,  Vilmos Simonidesz ,  Geza Galambos ,  Gabor Kovacs ,  Sandor Virag ,  Istvan Stadler ,  Peter Kormoczy

    IPC分类号： C07D307/935 ,  A61K31/557 ,  A61P7/02 ,  A61P9/12 ,  C07C405/00 ,  C07D307/937 ,  C07D407/12

    CPC分类号： C07D307/937 ,  C07C405/0033 ,  C07D407/12 ,  Y10S514/822

    摘要： The invention relates to new optically active or racemic 13-thia-prostacycline derivatives of the Formula I ##STR1## wherein R.sup.1 is hydrogen, a pharmaceutically acceptable cation or a straight or branched chain alkyl group having 1-5 carbon atoms;R.sup.2 is straight or branched chain alkyl having 4-9 carbon atoms or monosubstituted phenoxymethyl;--A--B-- is --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH-- of Z-- or E-- configuration or --C.tbd.C--;one of the symbols X and Y is hydrogen, methyl or ethyl and the other is hydroxy, tetrahydropyranyoxy, 1-ethoxy-ethoxy or trialkylsilyloxy; orX and Y together form a --O--CH.sub.2 --CH.sub.2 --O-- group;Z is a sulfur atom or a --SO-- group.The compounds of the Formula I can be prepared by reacting a 13-thia-prostaglandine of the Formula III ##STR2## if desired after oxidation into the corresponding 13-oxide derivative--with a halogenating agent; and treating the 5-halogeno-13-thia-prostacycline of the Formula II ##STR3## thus obtained wherein E is halogen with an organic or inorganic base; and thereafter if desired removing the protecting groups X and/or Y and if desired converting a compound of the Formula I obtained into a salt or setting free the same from a salt. The new compounds of the Formula I possess anti-coagulant and hypotensive properties and can be used in therapy.

    摘要翻译： 本发明涉及式I的新的光学活性或外消旋的13-前列环素衍生物，其中R1是氢，可药用阳离子或具有1-5个碳原子的直链或支链烷基; R2是具有4-9个碳原子的直链或支链烷基或单取代的苯氧基甲基; -A-B-是Z-或E-构型的-CH 2 -CH 2 - ， - CH = CH-或-C 3 D C-; 符号X和Y之一是氢，甲基或乙基，另一个是羟基，四氢吡喃基氧基，1-乙氧基 - 乙氧基或三烷基甲硅烷氧基; 或X和Y一起形成-O-CH 2 -CH 2 -O-基团; Z是硫原子或-SO-基。 式I的化合物可以通过使式III的13-前 - 前列腺素（III）反应来制备。