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    19 Hydroxy prostaglandins
    2.
    再颁专利
    19 Hydroxy prostaglandins 失效
    19羟基前列腺素

    公开(公告)号：USRE30287E

    公开(公告)日：1980-05-27

    申请号：US955005

    申请日：1978-10-26

    申请人： Arthur F. Marx ,  Jean Doodewaard

    发明人： Arthur F. Marx ,  Jean Doodewaard

    IPC分类号： C07C405/00 ,  C07F1/00 ,  C07F1/08 ,  C12P31/00

    CPC分类号： C12P31/00 ,  C07C405/00 ,  C07F1/00 ,  C07F1/08

    摘要： Novel 18 -, 19 - and 20 -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 of 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- 19- and 20-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.

    8.beta.-PGE.sub.2 and related compounds
    3.
    发明授权
    8.beta.-PGE.sub.2 and related compounds 失效
    8 {62 -PGE {HD 2 {B及相关化合物

    公开(公告)号：US3988361A

    公开(公告)日：1976-10-26

    申请号：US527749

    申请日：1974-11-27

    申请人： William P. Schneider

    发明人： William P. Schneider

    IPC分类号： C07C35/27 ,  C07C405/00 ,  C07D309/12 ,  C07D317/26 ,  C07D317/30 ,  C12P31/00 ,  C07C177/00

    CPC分类号： C07D317/26 ,  C07C35/27 ,  C07C405/00 ,  C07D309/12 ,  C07D317/30 ,  C12P31/00

    摘要： This invention is a group of compounds of the formula: ##SPC1##Wherein R.sub.1 is hydrogen, alkyl of one to 8 carbon atoms, inclusive, cycloalkyl of 3 to 10 carbon atoms, inclusive, aralkyl of 7 to 12 carbon atoms, inclusive, phenyl, phenyl substituted with one to 3 chloro, or alkyl of one to 4 carbon atoms, inclusive, or ethyl substituted in the .beta.-position with 3 chloro, 2 or 3 bromo, or 1, 2, or 3 iodo; wherein R.sub.2 is hydrogen or alkyl of one to 10 carbon atoms, inclusive, substituted with zero to 3 fluoro; wherein R.sub.3 and R.sub.4 are hydrogen or alkyl of one to 4 carbon atoms, inclusive; wherein A is alkylene of one to 10 carbon atoms, inclusive, substituted with zero to 2 fluoro, and with one to 5 carbon atoms, inclusive, between --COOR.sub.1 and ##EQU1## and pharmacologically acceptable salts thereof when R.sub.1 is hydrogen. These compounds are useful for a variety of pharmacological purposes, including lowering of blood pressure, control of the mammalian reproductive cycle, and increase of nasal patency.

    摘要翻译： 本发明是一组下式的化合物：