Prostaglandin derivatives
    14.
    发明授权

    公开(公告)号:US4190670A

    公开(公告)日:1980-02-26

    申请号:US831949

    申请日:1977-09-09

    摘要: Novel 18.xi.-, 19.xi.- and 20.xi.-hydroxy-prostaglandin derivatives of the formula I ##STR1## wherein the dotted line in the position 8-12 indicates the optional presence of a double bond, the waved lines in position 15 indicate that the hydroxyl group and the group R.sub.4 are either in .alpha.- or .beta.-position and Z represents a --CH.sub.2 CH.sub.2 -- or a cis --CH.dbd.CH-- group, and wherein R represents one of the groups: ##STR2## (wherein the waved lines indicate that the hydroxyl groups are either in .alpha.- or .beta.-position and R.sub.1 represents a hydrogen atom, a methyl or ethyl group), R.sub.2 represents either an oxygen atom or a hydrogen atom and an .alpha.- or .beta.-hydroxyl group, R.sub.3 represents a hydrogen atom or a hydroxyl group and R.sub.4 represents a hydrogen atom or a methyl group, with the proviso that when simultaneously, R.sub.1, R.sub.3 and R.sub.4 each represents a hydrogen atom, R.sub.2 represents an oxygen atom, a double bond is in 8-12 position and the 15-hydroxyl group is in position .alpha., R does not represent the group (b), but that when in addition to these conditions, Z represents a cis --CH.dbd.CH-- group and the 8-12 position is saturated, R either represents the groups (b) or (c); and the pharmaceutically acceptable salts and esters thereof, novel process for their preparation by selective microbiological hydroxylation of compounds formula II ##STR3## wherein the dotted line in the position 10-11 indicates the optional presence of a double bond in case the 8-12 position is saturated and the other symbols are as defined hereinabove, by means of microorganisms of the Division of Eumycota or, as far as the introduction of a hydroxyl group in the 18- or 19-position is concerned, of the Family of Streptomycetaceae, and, if desired, conversion of the 18.xi.-, 19.xi.- and 20.xi.-hydroxy-prostaglandin derivatives thus obtained into pharmaceutically acceptable salts and esters thereof, and pharmaceutical compositions containing at least one of the novel hydroxy-prostaglandin derivatives of formula I.

    (DL)-13-Substituted sulfinyl-prostaglandin-like compounds
    17.
    发明授权
    (DL)-13-Substituted sulfinyl-prostaglandin-like compounds 失效
    (DL)-13-取代的亚磺酰基 - 前列腺素样化合物

    公开(公告)号:US3970685A

    公开(公告)日:1976-07-20

    申请号:US476362

    申请日:1974-06-05

    摘要: (dl)-13-Substituted sulfinyl-prostaglandin-like [(dl)-2.alpha.-substituted-3.beta.-(1.alpha.-substituted sulfinyl-trans-2-alkenyl)-1-oxygenated cyclopentane and (dl)-2.alpha.-substituted -3.beta.-(1.alpha.-substituted sulfinyl-trans-2-alkenyl)-4-oxygenated-1-oxygenated cyclopentane] compounds exhibit prostaglandin-like biological properties and are also useful intermediates in the preparation of known prostaglandins.

    摘要翻译: (dl)-13-取代的亚磺酰基 - 前列腺素样[(dl)-2α-取代-3β-(1α-取代的亚磺酰基 - 反式-2-烯基)-1-氧化环戊烷和(dl)-2α 取代-3β-(1α-取代亚磺酰基 - 反式-2-烯基)-4-氧化-1-氧化环戊烷]化合物表现出前列腺素样生物学性质,并且也是制备已知前列腺素的有用的中间体。