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154 条记录 (耗时 0.032 秒)

    Thiaprostaglandin E.sub.1 derivatives, process for production thereof, and pharmaceutical use thereof
    11.
    发明授权
    Thiaprostaglandin E.sub.1 derivatives, process for production thereof, and pharmaceutical use thereof 失效
    Thiaprostaglandin E1衍生物，其制备方法及其药物用途

    公开(公告)号：US4466980A

    公开(公告)日：1984-08-21

    申请号：US316902

    申请日：1981-10-30

    申请人： Toshio Tanaka ,  Takeshi Toru ,  Takeo Oba ,  Noriaki Okamura ,  Kenzo Watanabe ,  Kiyoshi Bannai ,  Atsuo Hazato ,  Seizi Kurozumi ,  Fukuyoshi Kamimoto ,  Akira Ohtsu

    发明人： Toshio Tanaka ,  Takeshi Toru ,  Takeo Oba ,  Noriaki Okamura ,  Kenzo Watanabe ,  Kiyoshi Bannai ,  Atsuo Hazato ,  Seizi Kurozumi ,  Fukuyoshi Kamimoto ,  Akira Ohtsu

    IPC分类号： C07C405/00 ,  C07D309/12 ,  C07C177/00 ,  A61K31/557

    CPC分类号： C07C405/0033 ,  C07D309/12

    摘要： A novel compound selected from the group consisting of 7-(or 6- or 4-)thiaprostaglandin E.sub.1 derivatives of the formula (I). ##STR1## wherein A represents --CH.sub.2 -- or ##STR2## in which n is 0, 1 or 2, provided that only one A cut of three is ##STR3## R.sup.1 -R.sup.7 and G are as defined in the specification, the 15-epimers of said thiaprostaglandin E.sub.1 derivatives, the enatiomers of said thiaprostaglandin E.sub.1 derivatives or their 15-epimers, and mixtures of these compounds.A 7-thiaprostaglandin E.sub.1 derivative and/or its optical isomer may be prepared by reacting a 2-organo-2-cyclopentenone (II) with an organic copper-lithium compound (III) to effect conjugation reaction. A 6-thiaprostaglandin E.sub.1 derivative and/or its optical isomer may be prepared by subjecting an .alpha.,.beta.-unsaturated ketone (IV) and a thiol (V) to the Michael addition reaction. And, 4-thiaprostaglandin derivative and/or its optical isomer may also be prepared by the Michael addition reaction from a 2-allyl substituted cyclopentanone (VI) and a thiol (VIII).Some compounds ((I)-1) amongst the compounds of the formula (I) and/or their optical isomer are useful for controlling vascular actions such as angina pectoris, vasodilation etc.

    摘要翻译： 选自式（I）的7-（或6-或4-）赖氨酸前列腺素E1衍生物的新化合物。 （I）其中A表示-CH 2 - 或，其中n为0,1或2，条件是三个只有一个A切割是R 1 -R 7，G如说明书中所定义， 所述thiaprostaglandin E1衍生物的15-差向异构体，所述thiaprostaglandin E1衍生物或它们的15-差向异构体的对映体，以及这些化合物的混合物。 7-硫代前列腺素E1衍生物和/或其旋光异构体可以通过2-有机-2-环戊烯酮（II）与有机铜 - 锂化合物（III）反应来制备共轭反应。 6-硫代前列腺素E1衍生物和/或其旋光异构体可以通过使α，β-不饱和酮（IV）和硫醇（V）进行迈克尔加成反应来制备。 并且，也可以通过从2-烯丙基取代的环戊酮（VI）和硫醇（VIII）的迈克尔加成反应制备4-硫代前列腺素衍生物和/或其旋光异构体。 式（I）化合物和/或其旋光异构体中的一些化合物（（I）-1）可用于控制血管作用，例如心绞痛，血管舒张等。

    Prostacyclin analogues
    13.
    发明授权
    Prostacyclin analogues 失效

    公开(公告)号：US4367237A

    公开(公告)日：1983-01-04

    申请号：US097675

    申请日：1979-11-27

    申请人： Hirohisa Wakatsuka ,  Katsuichi Shimoji ,  Sadahiko Iguchi ,  Yoshitaka Konishi ,  Hisashi Suga ,  Yasuyuki Miyata ,  Yoichi Iguchi ,  Hajimu Miyake ,  Masaki Hayashi

    发明人： Hirohisa Wakatsuka ,  Katsuichi Shimoji ,  Sadahiko Iguchi ,  Yoshitaka Konishi ,  Hisashi Suga ,  Yasuyuki Miyata ,  Yoichi Iguchi ,  Hajimu Miyake ,  Masaki Hayashi

    IPC分类号： C07C405/00 ,  C07D333/78 ,  C07D335/04 ,  A61K31/38

    CPC分类号： C07C405/0033 ,  C07C405/00 ,  C07D333/78 ,  C07D335/04

    摘要： Prostaglandin analogues of the general formula: ##STR1## [wherein the ring A represents: ##STR2## the ring B represents: ##STR3## (wherein R.sup.6 represents hydrogen, methyl or ethyl, and r is zero, one or two), Y represents ethylene, cis- or trans-vinylene or ethynylene, Z represents a grouping of the formula: --(CH.sub.2).sub.m --, --(CH.sub.2).sub.3 --CHR.sup.7 --, --(CH.sub.2).sub.2 --CHR.sup.7 --CH.sub.2 --, --CH.sub.2 --CHR.sup.7 --(CH.sub.2).sub.2 --, --CHR.sup.7 --(CH.sub.2).sub.3 --, or trans--(CH.sub.2).sub.2 --CH.dbd.CH-- (wherein m is 3, 4 or 5, and R.sup.7 represents methyl or ethyl), R.sup.1 represents a grouping of the formula: --COOR.sup.8, ##STR4## or --CH.sub.2 OR.sup.11 (wherein R.sup.8 represents hydrogen, alkyl, aralkyl, cycloalkyl which is unsubstituted or substituted by at least one alkyl group, or R.sup.8 represents phenyl which is unsubstituted or substituted by halogen, trifluoromethyl, alkyl, alkoxy, alkylthio or phenyl, or represents naphthyl, 2,3- or 1,3-dihydroxypropyl, 2,3- or 1,3-bisalkanoyloxypropyl, a grouping of the formula: -D.sub.1 --COOR.sup.12, ##STR5## -D.sub.2 -R.sup.15 or -D.sub.3 -R.sup.16, wherein D.sub.1 represents alkylene, D.sub.2 represents alkylene, D.sub.3 represents a single bond or alkylene, R.sup.12, R.sup.13 and R.sup.14, each represent alkyl, R.sup.15 represents hydroxy, alkoxy or alkylthio and R.sup.16 represents a heterocyclic ring, or R.sup.8 represents a grouping of the formula: ##STR6## R.sup.9 and R.sup.10, each represent hydrogen, alkyl, alkylsulphonyl, alkanoyl or ##STR7## represents a heterocyclic ring, and R.sup.11 represents hydrogen or alkanoyl, R.sup.2 represents hydrogen, methyl or ethyl, R.sup.3 represents a single bond or alkylene, R.sup.4 represents hydrogen, alkyl, alkoxy, cycloalkyl or cycloalkyloxy unsubstituted or substituted by alkyl, or represents phenyl or phenoxy unsubstituted or substituted by halogen, trifluoromethyl or alkyl with the proviso that, when R.sup.3 represents a single bond, R.sup.4 does not represent alkoxy, cycloalkyloxy or phenoxy, R.sup.5 represents hydrogen, methyl or ethyl and with the proviso that, when one of the groups R.sup.5, R.sup.6 and R.sup.7 represents methyl or ethyl the other two groups are hydrogen atoms] and cyclodextrin clathrates, non-toxic salts and non-toxic acid addition salts thereof, possess selective strong stimulatory activity on uterine contraction in female mammals.

    Prostaglandin precursors
    20.
    发明授权
    Prostaglandin precursors 失效
    前列腺素前体

    公开(公告)号：US4212984A

    公开(公告)日：1980-07-15

    申请号：US862329

    申请日：1977-12-20

    申请人： Kiyosi Kondo ,  Daiei Tunemoto ,  Teruo Umemoto

    发明人： Kiyosi Kondo ,  Daiei Tunemoto ,  Teruo Umemoto

    IPC分类号： C07C29/14 ,  C07C405/00 ,  C07F7/18 ,  C07C177/00

    CPC分类号： C07C321/00 ,  C07C405/0033 ,  C07F7/1856 ,  Y02P20/55

    摘要： 4-Oxy-6-alkenyl-bicyclo[3.1.0]hexan-2-one compounds represented by the formula (I) ##STR1## wherein R represents a hydrogen atom or a protective group for a hydroxy group, R.sup.1 represents an alkyl group having 1 to 4 carbon atoms or an aryl group, R.sup.2 represents a substituted or unsubstituted alkyl group having 1 to 8 carbon atoms and R.sup.3 represents a hydrogen atom or an alkyl group having 1 to 4 carbon atoms;4-oxycyclopentanone compounds represented by the formula (II) ##STR2## wherein R, R.sup.2 and R.sup.3 are as defined above, R.sup.4 represents a hydroxymethyl group, a methylene group (.dbd.CH.sub.2) or a --COOR.sup.1 group wherein R.sup.1 is as defined above, and R.sup.5 represents an alkyl group having 1 to 4 carbon atoms or an aryl group, useful as prostaglandin precursors; and processes for preparing the same.

    摘要翻译： 由式（I）表示的4-氧基-6-烯基 - 双环[3.1.0]己-2-酮化合物其中R表示氢原子或羟基保护基，R 1表示 具有1〜4个碳原子的烷基或芳基，R 2表示取代或未取代的碳原子数1〜8的烷基，R 3表示氢原子或碳原子数1〜4的烷基。 由式（II）表示的4-羟基环戊酮化合物其中R，R 2和R 3如上所定义，R 4表示羟甲基，亚甲基（= CH 2）或-COOR 1基团，其中R 1为 R5代表具有1-4个碳原子的烷基或芳基，可用作前列腺素前体; 及其制备方法。