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    Furyl derivatives of 16-substituted prostaglandins
    9.
    发明授权
    Furyl derivatives of 16-substituted prostaglandins 失效
    16取代前列腺素的呋喃衍生物

    公开(公告)号：US4585791A

    公开(公告)日：1986-04-29

    申请号：US667367

    申请日：1984-11-01

    Applicant: Franco Faustini ,  Achille Panzeri ,  Fabrizio Orzi ,  Enrico di Salle ,  Roberto Ceserani

    Inventor： Franco Faustini ,  Achille Panzeri ,  Fabrizio Orzi ,  Enrico di Salle ,  Roberto Ceserani

    IPC: C07D307/38 ,  A61K31/557 ,  A61P43/00 ,  C07C67/00 ,  C07C401/00 ,  C07D307/54 ,  C07D307/935 ,  A61K31/34

    CPC classification number: C07D307/935 ,  C07D307/54

    Abstract: The present invention relates to new furyl derivatives of 16-substituted prostaglandins, to a process for their preparation and to pharmaceutical and veterinary compositions containing them.The new compounds of the invention are optically active or racemic prostaglandins of the following formula (I) ##STR1## wherein R is(1) --OH or --OR' wherein R' is C.sub.1 -C.sub.6 alkyl optionally substituted by phenyl or by a monocycloalkyl group or by a pentatomic or hexatomic heteromonocyclic ring containing at least one heteroatom chosen from O, S and N;(2) ##STR2## wherein each of R" and R"', is independently, hydrogen; C.sub.1 -C.sub.6 alkyl; phenyl; or a pentatomic or hexatomic heteromonocyclic ring containing at least one heteroatom chosen from O, S and N; or R" and R"', together with the nitrogen atom to which they are linked, form a pentatomic or hexatomic heteromonocyclic ring optionally containing a further heteroatom chosen from O, S and N;(3) --W--(CH.sub.2).sub.n --X wherein W is --O-- or --NH--, n is an integer of 1 to 4 and X represents a group --OR' or a group ##STR3## wherein R', R" and R"' are as defined above;one of R.sub.1 and R.sub.2 is hydrogen and the other is hydroxy orR.sub.1 and R.sub.2, taken together, form an oxo group;one of R.sub.3 and R.sub.4 is hydrogen and the other is hydroxy;one of R.sub.5 and R.sub.6 is hydroxy and the other is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, or phenyl;one of R.sub.7 and R.sub.8 is hydrogen and the other is a C.sub.1 -C.sub.4 alkyl or tri-halo-C.sub.1 -C.sub.4 alkyl group;m is an integer of 1 to 3;R.sub.9 is a 2-furyl or 3-furyl group, optionally substituted by one or more substituents chosen from C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, tri-halo-C.sub.1 -C.sub.4 alkyl and halogen; and the symbol represents a single bond or a cis double bond.

    Abstract translation: 本发明涉及16-取代的前列腺素的新呋喃衍生物，其制备方法和含有它们的药物和兽药组合物。 本发明的新化合物是下式（I）的光学活性或外消旋前列腺素其中R是（1）-OH或-OR'，其中R'是任选被苯基取代的C 1 -C 6烷基或 通过单环烷基或含有至少一个选自O，S和N的杂原子的五原子或六原子杂单环; （2）其中R“和R”'各自独立地为氢; C1-C6烷基; 苯基; 或含有至少一个选自O，S和N的杂原子的五原子或六原子杂单环; 或R“和R”'与它们所连接的氮原子一起形成任选地含有选自O，S和N的另外的杂原子的五原子或六原子异单环; （3）-W-（CH2）nX其中W是-O-或-NH-，n是1至4的整数，X表示基团-OR'或基团，其中R'，R“ 和R“'如上所定义; R 1和R 2之一是氢，另一个是羟基或R 1和R 2一起形成氧代基; R3和R4之一是氢，另一个是羟基; R 5和R 6之一是羟基，另一个是氢，C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6炔基或苯基; R 7和R 8中的一个是氢，另一个是C 1 -C 4烷基或三卤代-C 1 -C 4烷基; m为1〜3的整数。 R9是2-呋喃基或3-呋喃基，任选被一个或多个选自C 1 -C 4烷基，C 1 -C 4烷氧基，三卤代-C 1 -C 4烷基和卤素的取代基取代; 符号表示单键或顺式双键。

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