1,4-Oxathianes
    1.
    发明授权

    公开(公告)号:US4125622A

    公开(公告)日:1978-11-14

    申请号:US860355

    申请日:1977-12-14

    IPC分类号: A61K31/39 A61P7/02 C07D327/06

    CPC分类号: C07D327/06 Y10S514/822

    摘要: 1,4-Oxathianes of the formula ##STR1## and the physiologically-acceptable salts thereof wherein R.sup.1 is H or alkyl with 1-4 C-atoms; R.sup.2 is H or alkyl with 1-4 C-atoms; R.sup.3 is H, alkyl with 1-8 C-atoms, phenyl or phenyl substituted by F, Cl, Br, OH, OCH.sub.3, CF.sub.3 or NO.sub.2 ; R.sup.4 is H or CH.sub.3 ; B is a single bond, --CH.sub.2 --, --CH.sub.2 CH.sub.2 -- or --CH.sub.2 O--; and a wavy line ( ) indicates that these bonds can be in the .alpha.- or .beta.- positions possess thrombocyte inhibition properties.

    摘要翻译: 具有式“IMAGE”的1,4-氧硫辛酸和其生理学上可接受的盐,其中R 1是H或具有1-4个C原子的烷基; R2是H或具有1-4个C原子的烷基; R3是H,具有1-8个C原子的烷基,被F,Cl,Br,OH,OCH3,CF3或NO2取代的苯基或苯基; R4是H或CH3; B是单键,-CH 2 - , - CH 2 CH 2 - 或-CH 2 O- 和波浪线()表示这些键可以在α或β位具有血细胞抑制性质。

    Thiaprostaglandins
    6.
    发明授权

    公开(公告)号:US4080458A

    公开(公告)日:1978-03-21

    申请号:US576140

    申请日:1975-05-09

    CPC分类号: C07C405/0033 Y02P20/55

    摘要: 13-Thiaprostanoic acid derivatives of the formula ##STR1## wherein A is --CO-- or --CHOH--, B is --CH.sub.2 --CH.sub.2 -- or --CH=CH--, R.sup.1 is H or alkyl of 1 to 4 carbon atoms, m is a whole number from 0 to 5, n is a whole number from 0 to 3 or, when B is --CH=CH--, additionally 4, 5, 6, 7, 8 or 9, R.sup.2 is alkoxy of 1 to 4 carbon atoms, phenoxy, pyridyl, thienyl, naphthyl, phenyl substituted by F, Cl, Br, OH, OCH.sub.3 or OF.sub.3 or phenoxy substituted by F, Cl, Br, OH, OCH.sub.3, CH.sub.3 or CF.sub.3 or, when B is --CH=CH--, additionally hydrogen, phenyl or tolyl, R.sup.3 is H, methyl or ethyl, possess pharmacological activity, including blood pressure lowering activity.

    摘要翻译: 其中A是-CO-或-CHOH-,B是-CH 2 -CH 2 - 或-CH = CH-,R 1是H或1-4个碳原子的烷基,m是 0至5的整数,n为0至3的整数,或当B为-CH = CH-时,另外为4,5,6,7,8或9,R 2为1至4个碳原子的烷氧基 苯氧基,吡啶基,噻吩基,萘基,被F,Cl,Br,OH,OCH3或OF3取代的苯基或被F,Cl,Br,OH,OCH3,CH3或CF3取代的苯氧基,或当B为-CH = CH- ,另外是氢,苯基或甲苯基,R3是H,甲基或乙基,具有药理活性,包括降血压活性。

    13-Thiaprostaglandin derivatives
    7.
    发明授权
    13-Thiaprostaglandin derivatives 失效
    13-Thiaprostaglandin衍生物

    公开(公告)号:US4309441A

    公开(公告)日:1982-01-05

    申请号:US96348

    申请日:1979-11-21

    摘要: 13-Thiaprostanoic acid derivatives of the general formula I ##STR1## wherein A is --CO-- or --CHOH--; B is --CH.sub.2 CH.sub.2 -- or --CH.dbd.CH--; Q is 1,4-phenylene or 1,4-naphthylene; R.sup.1 is H or OH; R.sup.2 is H or CH.sub.3 ; R.sup.3 is alkyl with 1-8 carbon atoms or alkyl with 1-8 carbon atoms substituted by (a) phenyl, (b) phenyl substituted by at least one of CH.sub.3, F, Cl, Br, OH, OCH.sub.3 or CF.sub.3 ; (c) phenoxy or (d) phenoxy substituted by at least one of CH.sub.3, F, Cl, Br, OH, OCH.sub.3 or CF.sub.3 ; and R.sup.4 is NH.sub.2, CH.sub.3, phenyl, p-acetylaminophenyl, p-benzoylaminophenyl or phenylamino. These compounds are useful for lowering blood pressure as well as for other pharmaceutical purposes. They also are useful intermediates for the preparation of other known pharmaceuticals such s the 13-thiaprostaglandins.

    摘要翻译: 其中A是-CO-或-CHOH-的通式I(I)的13-十三十二烷酸衍生物; B是-CH 2 CH 2 - 或-CH = CH-; Q是1,4-亚苯基或1,4-亚萘基; R1是H或OH; R2是H或CH3; R3是具有1-8个碳原子的烷基或具有1-8个碳原子的烷基,被(a)苯基取代,(b)被至少一个CH 3,F,Cl,Br,OH,OCH 3或CF 3取代的苯基; (c)苯氧基或(d)被至少一个CH 3,F,Cl,Br,OH,OCH 3或CF 3取代的苯氧基; 并且R 4是NH 2,CH 3,苯基,对乙酰氨基苯基,对苯甲酰基氨基苯基或苯基氨基。 这些化合物可用于降低血压以及其它药物目​​的。 它们也是制备其它已知药物如十三硫代前列腺素的有用的中间体。

    Thiaprostaglandins
    8.
    发明授权

    公开(公告)号:US4210651A

    公开(公告)日:1980-07-01

    申请号:US870555

    申请日:1978-01-18

    CPC分类号: C07C405/0033 Y02P20/55

    摘要: 13-Thiaprostanoic acid derivatives of the formula ##STR1## wherein A is --CO-- or --CHOH--, B is --CH.sub.2 --CH.sub.2 -- or --CH.dbd.CH-- R.sup.1 is H or alkyl of 1 to 4 carbon atoms, m is a whole number from 0 to 5, n is a whole number from 0 to 3 or, when B is --CH.dbd.CH--, additionally 4, 5, 6, 7, 8 or 9, R.sup.2 is alkoxy of 1 to 4 carbon atoms, phenoxy, pyridyl, thienyl, naphthyl, phenyl substituted by F, Cl, Br, OH, OCH.sub.3 or OF.sub.3 or phenoxy substituted by F, Cl, Br, OH, OCH.sub.3, CH.sub.3 or CF.sub.3 or, when B is --CH.dbd.CH--, additionally hydrogen, phenyl or tolyl, R.sup.3 is H, methyl or ethyl, possess pharmacological activity, including blood pressure lowering activity.

    摘要翻译: 其中A为-CO-或-CHOH-,B为-CH 2 -CH 2 - 或-CH = CH-R 1的13-十三硫代雄甾烷酸衍生物为H或1至4个碳原子的烷基,m为 0至5的整数,n为0至3的整数,或当B为-CH = CH-时,另外为4,5,6,7,8或9,R 2为1至4个碳原子的烷氧基, 苯氧基,吡啶基,噻吩基,萘基,被F,Cl,Br,OH,OCH3或OF3取代的苯基或被F,Cl,Br,OH,OCH3,CH3或CF3取代的苯氧基,或当B为-CH = CH-时, 另外,氢,苯基或甲苯基,R3是H,甲基或乙基,具有药理活性,包括降血压活性。