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    Certain 5-cyano-16-fluoro-prostacyclins and their use as pharmaceuticals
    5.
    发明授权
    Certain 5-cyano-16-fluoro-prostacyclins and their use as pharmaceuticals 失效
    某些5-氰基-16-氟前列环素及其作为药物的用途

    公开(公告)号：US4378370A

    公开(公告)日：1983-03-29

    申请号：US309967

    申请日：1981-10-06

    申请人： Helmut Vorbrueggen ,  Bernd Raduechel ,  Werner Skuballa ,  Gerda Mannesmann ,  Jorge Casals-Stenzel ,  Ekkehard Schillinger

    发明人： Helmut Vorbrueggen ,  Bernd Raduechel ,  Werner Skuballa ,  Gerda Mannesmann ,  Jorge Casals-Stenzel ,  Ekkehard Schillinger

    IPC分类号： C07D307/935 ,  A61K31/34 ,  A61K31/557 ,  A61P43/00 ,  C07D307/93 ,  C07D307/937 ,  C07F7/18

    CPC分类号： C07D307/937 ,  C07F7/1856 ,  Y10S514/826

    摘要： Prostacyclin derivatives of the formula ##STR1## wherein R.sub.1 is OR.sub.3 wherein R.sub.3 is hydrogen or alkyl of 1-10 carbon atoms, or R.sub.1 is NHR.sub.4 wherein R.sub.4 is alkanoyl or alkanesulfonyl,B is alkylene of 1-5 carbon atoms,A is --CH.sub.2 --CH.sub.2 --, cis--CH.dbd.CH--, or trans--CH.dbd.CH--,W is hydroxymethylene or ##STR2## wherein the OH-group is optionally substituted by alkanoyl of 1-4 carbon atoms and the free or substituted OH-group can be in the .alpha.- or .beta.- position,R.sub.2 is alkyl of 1-6 carbon atoms optionally substituted by phenyl, or R.sub.2 is phenyl,R.sub.5 is hydroxy optionally substituted by alkanoyl of 1-4 carbon atoms,R.sub.6 is hydrogen, fluorine, or alkyl of 1-4 carbon atomsor when R.sub.3 is hydrogen, a salt thereof with a physiologically compatible base,have pharmacological activity e.g., blood pressure-lowering and bronchodilatory effects.

    摘要翻译： PCT No.PCT / DE81 / 00031 Sec。 371日期1981年10月6日 102（e）日期1981年10月6日PCT提交1981年2月5日PCT公布。 出版物WO81 / 02296 日本1981年8月20日。其中R 1为OR 3的式（I）其中R 3为氢或1-10个碳原子的烷基，或R 1为NHR 4，其中R 4为烷酰基或链烷磺酰基，B为1- 5个碳原子，A是-CH 2 -CH 2 - ，顺式-CH = CH-或反式-CH = CH-，W是羟基亚甲基或其中OH基任选被1-4个碳原子的烷酰基取代 并且游离或取代的OH基团可以在α或β位，R 2是任选被苯基取代的1-6个碳原子的烷基，或者R 2是苯基，R 5是任选被1-4碳的烷酰基取代的羟基 原子，R6是氢，氟或1-4个碳原子的烷基，或当R3是氢时，其与生理上相容的碱的盐具有药理活性，例如降血压和支气管扩张作用。

    Azaprostacyclins, their preparation and pharmaceutical use
    8.
    发明授权
    Azaprostacyclins, their preparation and pharmaceutical use 失效
    阿沙普罗环素，其制备和药物用途

    公开(公告)号：US4567195A

    公开(公告)日：1986-01-28

    申请号：US591719

    申请日：1984-03-21

    申请人： Norbert Schwarz ,  Werner Skuballa ,  Helmut Vorbrueggen ,  Jorge Casals-Stenzel ,  Ekkehard Schillinger ,  Michael H. Town

    发明人： Norbert Schwarz ,  Werner Skuballa ,  Helmut Vorbrueggen ,  Jorge Casals-Stenzel ,  Ekkehard Schillinger ,  Michael H. Town

    IPC分类号： A61K31/40 ,  A61K31/403 ,  A61K31/557 ,  A61P7/02 ,  A61P9/10 ,  A61P9/12 ,  A61P11/08 ,  C07C57/03 ,  C07C57/13 ,  C07C57/26 ,  C07C57/52 ,  C07C405/00 ,  C07D209/52 ,  C07D307/935 ,  C07F9/40

    CPC分类号： C07D307/935 ,  C07C405/00 ,  C07C405/0041 ,  C07C57/03 ,  C07C57/13 ,  C07C57/26 ,  C07C57/52 ,  C07D209/52 ,  C07F9/4015 ,  C07F9/4018

    摘要： Azaprostacyclins of Formula I ##STR1## wherein R.sub.1 is hydrogen, alkyl, cycloalkyl, aryl, a heterocyclic residue, or a phenacyl residue optionally substituted on the phenyl ring by bromine, phenyl, alkoxy, or dialkoxy,W is a free or functionally modified carbonyl group or a ##STR2## wherein R.sub.8 is hydrogen or alkyl of 1-5 carbon atoms and R.sub.9 is hydrogen or a readily cleavable ether or acyl residue and wherein the OR.sub.9 -group can be in the .alpha.- or .beta.-position,R.sub.2 is a free or functionally modified hydroxy group,R.sub.3 and R.sub.4 each independently is hydrogen, alkyl of 1-5 carbon atoms, or fluorine,D is alkylene of 1-2 carbon atoms which can be substituted by alkyl groups of 1-5 carbon atoms,R.sub.5 is hydrogen or alkyl of 1-2 carbon atoms or, when D is alkylene of 1 or 2 carbon atoms, R.sub.5, together with R.sub.6, represents a bond,R.sub.6 and R.sub.7 each independently is hydrogen or alkyl of 1-2 carbon atoms, whereinR.sub.6 (R.sub.7) is halogen when R.sub.7 (R.sub.6), respectively, is alkyl of 1-2 carbon atoms orR.sub.5 and R.sub.7 each independently is hydrogen or alkyl of 1-2 carbon atoms whenD and R.sub.6 together form a carbocyclic ring closed via (CH.sub.2).sub.1-3 with D as --CH

    摘要翻译： 式I的阿沙普罗环素其中R 1是氢，烷基，环烷基，芳基，杂环残基或任选在苯环上被溴，苯基，烷氧基或二烷氧基取代的苯甲酰甲基残基，W是游离或 官能改性的羰基或其中R8是氢或1-5个碳原子的烷基，R9是氢或易裂解的醚或酰基残基，其中OR9-基团可以是α-或β-位， R2是游离的或官能改性的羟基，R 3和R 4各自独立地是氢，1-5个碳原子的烷基或氟，D是可以被1-5个碳原子的烷基取代的1-2个碳原子的亚烷基 原子，R5是氢或1-2个碳原子的烷基，或当D是1或2个碳原子的亚烷基时，R5与R6一起代表键，R6和R7各自独立地是氢或1-2碳的烷基 原子，其中当R 7（R 6）分别为1-2个碳原子的烷基或R 5和R 7 eac时，R 6（R 7）为卤素 h独立地为氢或1-2个碳原子的烷基，当D和R6一起形成通过（CH 2）1-3封闭的碳环，其中D为-CH 3且R 6为-CH 2 - ，当R 1为氢时， 其与碱的生理上相容的盐具有有价值的药理学性质，例如降血压和支气管扩张活性。

    5-Cyano-prostacyclin derivatives and use as medicines
    10.
    发明授权
    5-Cyano-prostacyclin derivatives and use as medicines 失效
    5-Cyano-prostacyclin衍生物用作药物

    公开(公告)号：US4364950A

    公开(公告)日：1982-12-21

    申请号：US317621

    申请日：1981-11-02

    申请人： Werner Skuballa ,  Helmut Vorbruggen ,  Bernd Raduchel ,  Jorge Casals-Stenzel ,  Ekkehard Schillinger ,  Michael H. Town

    发明人： Werner Skuballa ,  Helmut Vorbruggen ,  Bernd Raduchel ,  Jorge Casals-Stenzel ,  Ekkehard Schillinger ,  Michael H. Town

    IPC分类号： A61K31/557 ,  A61P7/02 ,  A61P9/12 ,  A61P11/08 ,  A61P43/00 ,  C07D307/935 ,  C07D307/937 ,  C07F7/18 ,  C07F9/40

    CPC分类号： C07D307/935 ,  C07D307/937 ,  C07F7/1856 ,  C07F9/4015

    摘要： 5-cyano-prostacyclins of the formula ##STR1## wherein R.sub.1 is OR.sub.2 or NHR.sub.3 ; R.sub.2 and R.sub.3 each independently is (a) H, (b) C.sub.1-10 -alkyl, (c) C.sub.1-10 -alkyl substituted by halo, C.sub.1-4 -alkoxy or phenyl, 1-naphthyl or 2-naphthyl, each optionally substituted as defined below, (d) C.sub.4-10 -cycloalkyl, (e) C.sub.4-10 -cycloalkyl substituted by C.sub.1-4 -alkyl, (f) phenyl, 1-naphthyl or 2-naphthyl, (g) phenyl, 1-naphthyl or 2-naphthyl substituted by 1-3 halogen atoms, phenyl, 1-3 alkyl groups of 1-4 C atoms each, or a chloromethyl-, fluoromethyl-, trifluoromethyl-, carboxyl-, hydroxy- or alkoxy-group of 1-4 C atoms, or (h) an aromatic, 5- or 6-membered heterocyclic ring containing one hetero atom which is O, N or S, the remaining atoms being carbon; R.sub.3 also possibly being an acyl group of a C.sub.1-15 -hydrocarbon carboxylic or sulfonic acid;B is straight chain or branched alkylene of 2-10 C atoms;W is hydroxymethylene or ##STR2## wherein the OH group may be in the alpha or beta position, and is optionally modified by replacement of the H atom of the OH with an ether or acyl group which is conventional for such replacements in prostaglandins and which is readily cleavable at physiological pH's;R.sub.4 is hydroxy, optionally modified as described for W above;R.sub.5, R.sub.6, R.sub.7 and R.sub.8 each independently is hydrogen, alkyl of 1-5 C atoms or methoxy; andR.sub.9 is alkyl of 1-5 C atoms orfor compounds wherein R.sub.2 is H, the salts thereof with physiologically compatible bases have valuable pharmacalogical properties, e.g., hypertonic and bronchodilatory activities.

    摘要翻译： 其中R1是OR2或NHR3的式“IMAGE”的5-氰基 - 前列环素; R 2和R 3各自独立地为（a）H，（b）C 1-10 - 烷基，（c）被卤素，C 1-4 - 烷氧基或苯基，1-萘基或2-萘基取代的C 1-10 - 烷基， （d）C 4-10 - 环烷基，（e）被C 1-4 - 烷基取代的C 4-10 - 环烷基，（f）苯基，1-萘基或2-萘基，（g）苯基， 萘基或被1-3个卤素原子取代的2-萘基，苯基，1-4个C原子的1-3个烷基，或1个氯甲基 - ，氟甲基 - ，三氟甲基 - ，羧基 - ，羟基或烷氧基 -4个C原子，或（h）含有一个杂原子的芳族的5或6元杂环，它是O，N或S，其余的原子是碳; R3也可能是C1-15-烃羧酸或磺酸的酰基; B是2-10个C原子的直链或支链亚烷基; W是羟基亚甲基或其中OH基团可以在α或β位置，并且任选地通过用在前列腺素中这种替代物常规的醚或酰基取代OH的H原子来任意修饰，并且其是 在生理pH值下易于切割; R4是羟基，任选地按照上述W所述进行改性; R5，R6，R7和R8各自独立地为氢，1-5个C原子的烷基或甲氧基; 并且R 9为1-5个C原子的烷基，或对于其中R 2为H的化合物，其与生理上相容的碱的盐具有有价值的药理学性质，例如高渗和支气管扩张活性。