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    Novel 11-oxoprostaglandin derivatives
    1.
    发明授权
    Novel 11-oxoprostaglandin derivatives 失效
    新型11-氧代前列腺素衍生物

    公开(公告)号：US4346228A

    公开(公告)日：1982-08-24

    申请号：US677420

    申请日：1976-04-15

    申请人： Werner Skuballa ,  Bernd Raduechel ,  Helmut Vorbrueggen ,  Walter Elger ,  Olaf Loge ,  Eckehard Schillinger

    发明人： Werner Skuballa ,  Bernd Raduechel ,  Helmut Vorbrueggen ,  Walter Elger ,  Olaf Loge ,  Eckehard Schillinger

    IPC分类号： A61K31/23 ,  C07C67/00 ,  C07C401/00 ,  C07C405/00 ,  C07D213/30 ,  C07D307/20 ,  C07D307/935 ,  C07D309/12 ,  C07D521/00 ,  C07C177/00

    CPC分类号： C07D307/935 ,  C07C405/00 ,  C07D309/12

    摘要： 11-Oxoprostaglandin derivatives of the formula ##STR1## wherein R.sub.2 is a hydrogen atom or alkyl of 1-5 carbon atoms,R.sub.3 is alkyl of 1-5 carbon atoms, alkylaryl, cycloalkyl of 5-6 ring carbon atoms and a total of 5-10 carbon atoms; benzodioxol-2-yl, phenyl, naphthyl or phenyl or naphthyl substituted by phenyl, halogen, alkyl of 1-4 carbon atoms, chloromethyl, fluoromethyl, carboxyl or hydroxy;A is --CH.sub.2 --CH.sub.2 --, cis--CH.dbd.CH--, or trans--CH.dbd.CH--;B is --CH.sub.2 --CH.sub.2 -- or trans--CH.dbd.CH--,D and E collectively are a direct bond or D is alkylene of 1-5 carbon atoms and E is an oxygen or sulfur atom; esters thereof; readily cleavable 9,15 and 9,15 ethers thereof; methanesulfonylamides thereof, and physiologically acceptable salts thereof with bases; possess the activity of the corresponding natural prostaglandins with a surprisingly longer duration of effectiveness, greater selectivity, and better effects, and can be produced, e.g., by oxidation of the corresponding 9-hydroxy prostaglandins.

    摘要翻译： 其中R2是氢原子或1-5个碳原子的烷基，R3是1-5个碳原子的烷基，烷基芳基，5-6个环碳原子的环烷基和总共5个碳原子的11-前列酰乳糖衍生物 -10个碳原子; 苯基二氧杂环戊烯-2-基，苯基，萘基或被苯基，卤素，1-4个碳原子的烷基取代的苯基或萘基，氯甲基，氟甲基，羧基或羟基; A是-CH 2 -CH 2 - ，顺式-CH = CH-或反式-CH = CH-; B是-CH 2 -CH 2 - 或反式-CH = CH-，D和E共同是直接键或D是1-5个碳原子的亚烷基，E是氧或硫原子; 其酯; 易于切割的9,15和9,15醚; 甲磺酰胺及其与碱的生理学上可接受的盐; 具有相当的天然前列腺素的活性，具有惊人的更长的有效期，更高的选择性和更好的效果，并且可以例如通过相应的9-羟基前列腺素的氧化来产生。

    Novel acetylenic prostaglandin analogs
    2.
    发明授权
    Novel acetylenic prostaglandin analogs 失效
    新型炔类前列腺素类似物

    公开(公告)号：US4073934A

    公开(公告)日：1978-02-14

    申请号：US677861

    申请日：1976-04-16

    申请人： Werner Skuballa ,  Bernd Raduechel ,  Helmut Vorbrueggen ,  Walter Elger ,  Olaf Loge ,  Eckehard Schillinger

    发明人： Werner Skuballa ,  Bernd Raduechel ,  Helmut Vorbrueggen ,  Walter Elger ,  Olaf Loge ,  Eckehard Schillinger

    IPC分类号： A61K31/23 ,  C07C67/00 ,  C07C401/00 ,  C07C405/00 ,  C07D213/30 ,  C07D213/55 ,  C07D307/38 ,  C07D307/54 ,  C07D307/935 ,  C07D333/06 ,  C07C177/00 ,  A61K31/19 ,  A61K31/215

    CPC分类号： C07D307/935 ,  C07C405/00

    摘要： Optically active and racemic prostaglandin derivatives of the formula ##STR1## wherein R.sub.1 is --OR.sub.5 ; --NHSO.sub.2 CH.sub.3 ; or --O--CH.sub.2 --U--V; R.sub.5 is hydrogen, alkyl, aryl, or a heterocyclic group; U is a direct bond, carbonyl or carbonyloxy; and V is phenyl substituted by 1-3 phenyl, alkoxy of 1-2 carbon atoms, or halogen, preferably bromine;R.sub.2 is hydrogen or alkyl of 1-5 carbon atoms;R.sub.3 is alkyl, substituted or unsubstituted cycloalkyl, straight-chain or branched alkyl of 1-5 carbon atoms substituted by aryl or substituted aryl, when R.sub.1 is as above; or R.sub.3 is aryl or substituted aryl group when R.sub.1 is --OR.sub.5 ', --NHSO.sub.2 CH.sub.3, or --O--CH.sub.2 --U--V and R.sub.5 ' is aryl or a heterocyclic group and U and V are as above;R.sub.4 is hydrogen or an ether or acyl residue;A is --CH.sub.2 --CH.sub.2 -- or cis--CH.dbd.CH--;B is --CH.sub.2 --CH.sub.2 -- or trans--CH.dbd.CH--;D is a direct bond, oxygen, or sulfur;Z is carbonyl or >CH OR.sub.4 wherein OR.sub.4 is in the .alpha.- or .beta.-position; andX y is ##STR2## when Z is >CH OR.sub.4 --, or ##STR3## or --CH.dbd.CH-- when Z is carbonyl; AND, WHEN R.sub.1 is hydroxy, the physiologically compatible salts thereof with bases, have more prolonged activity than naturally-occurring prostaglandins.

    摘要翻译： 式（Ⅰ）的光学活性和外消旋前列腺素衍生物，其中R1为-OR5; -NHSO 2 CH 3; 或-O-CH 2 -U-V; R5是氢，烷基，芳基或杂环基; U是直接键，羰基或羰氧基; 并且V是被1-3个苯基，1-2个碳原子的烷氧基或卤素，优选溴取代的苯基; R2是氢或1-5个碳原子的烷基; R 3为烷基，取代或未取代的环烷基，被芳基或取代芳基取代的1-5个碳原子的直链或支链烷基，当R 1如上所述时; 或当R 1为-OR 5'，-NHSO 2 CH 3或-O-CH 2 -U-V且R 5'为芳基或杂环基时，R 3为芳基或取代的芳基，U和V如上所述; R4是氢或醚或酰基残基; A是-CH 2 -CH 2 - 或顺式-CH = CH-; B是-CH 2 -CH 2 - 或反式-CH = CH-; D是直接键合，氧或硫; Z是羰基或> CH OR 4，其中OR 4在α或β-位; 当Z为羰基时Z为> CH OR4-或或-CH = CH-时，X Y为 当R1是羟基时，其与碱的生理上相容的盐比天然存在的前列腺素具有更长的活性。