Enlarged hetero-ring prostacyclin analogs
    81.
    发明授权
    Enlarged hetero-ring prostacyclin analogs 失效
    扩大的杂环前列环素类似物

    公开(公告)号:US4262116A

    公开(公告)日:1981-04-14

    申请号:US932981

    申请日:1978-08-11

    申请人: Roy A. Johnson

    发明人: Roy A. Johnson

    摘要: Prostaglandin (PG.sub.1, derivatives having (1) a 5-keto feature, for example ##STR1## or (2) a 9-deoxy-5,9-epoxy feature together with a 4-halo or 5-hydroxy feature, for example ##STR2## or a 4,5-didehydro feature, for example in an enol ether of the formula ##STR3## said derivatives having pharmacological activity. Processes for preparing them and the appropriate intermediates are disclosed.

    摘要翻译: 前列腺素(PG1)具有(1)5-酮基特征的衍生物,例如或(2)9-脱氧-5,9-环氧基特征以及4-卤素或5-羟基特征, IMAGE>或“IMAGE”或4,5-二脱水特征,例如在式(Ⅰ)的烯醇醚中,所述具有药理学活性的衍生物具有制备它们的方法和合适的中间体。

    4 Halo-5,9-epoxy-9-deoxy-PGF.sub.1, amides
    83.
    发明授权
    4 Halo-5,9-epoxy-9-deoxy-PGF.sub.1, amides 失效
    4卤代-5,9-环氧-9-脱氧-PGF1,酰胺

    公开(公告)号:US4259480A

    公开(公告)日:1981-03-31

    申请号:US73455

    申请日:1979-09-07

    申请人: Roy A. Johnson

    发明人: Roy A. Johnson

    摘要: The present invention relates to novel 4-Halo-5,9-epoxy-9-deoxy-PGF.sub.1, amides, which are intermediates useful for the preparation of corresponding 5,9.alpha.-epoxy-9-deoxy-PGF.sub.1 and 5,9-epoxy-9-deoxy-4,5-didehydro-PGF.sub.1 compounds. These end products are employed for induction of a variety of prostacyclinlike pharmacological effects. Accordingly, these end products are useful pharmacological agents for the same purposes for which prostacyclin is employed.

    摘要翻译: 本发明涉及新的4-卤代-5,9-环氧-9-脱氧-PGF1酰胺,其是可用于制备相应的5,9-环氧-9-脱氧-PGF1和5,9-环氧-9-脱氧-PGF1的中间体, 环氧-9-脱氧-4,5-二脱氧-PGF1化合物。 这些最终产品用于诱导各种前列环素样药理作用。 因此,这些最终产品是用于前列环素用于相同目的的有用的药理学试剂。

    Trans-2,3,4,5-tetradehydro-9-deoxy-5,9a-epoxy-PGF.sub.1 amides
    86.
    发明授权
    Trans-2,3,4,5-tetradehydro-9-deoxy-5,9a-epoxy-PGF.sub.1 amides 失效
    反式-2,3,4,5-四脱氢-9-脱氧-5,9a-环氧-PGF1酰胺

    公开(公告)号:US4235783A

    公开(公告)日:1980-11-25

    申请号:US73463

    申请日:1979-09-07

    申请人: Roy A. Johnson

    发明人: Roy A. Johnson

    摘要: The present invention relates to novel trans-2,3,4,5-tetradehydro-9-deoxy-5,9a-epoxy-PGF.sub.1 amides, which are useful for inducing a variety of prostacyclin-like pharmacological effects. Accordingly, these compounds are useful pharmacological agents for the same purposes for which prostacyclin is employed.

    摘要翻译: 本发明涉及新的反式-2,3,4,5-四脱氢-9-脱氧-5,9a-环氧-PGF1酰胺,其可用于诱导各种前列环素样药理作用。 因此,这些化合物是用于前列环素用于相同目的的有用的药理学试剂。

    C.sub.1-4 alkanoylphenyl-esters of 5-hydroxy-PGI.sub.1, .DELTA..sup.4
-PGI.sub.1, and 4-oxo-PGI.sub.1 compounds
    88.
    发明授权
    C.sub.1-4 alkanoylphenyl-esters of 5-hydroxy-PGI.sub.1, .DELTA..sup.4 -PGI.sub.1, and 4-oxo-PGI.sub.1 compounds 失效
    5-羟基-PGI1,DELTA4-PGI1和4-氧代-PGI1化合物的C1-4烷酰基苯基酯

    公开(公告)号:US4220758A

    公开(公告)日:1980-09-02

    申请号:US48494

    申请日:1979-06-14

    申请人: John C. Sih

    发明人: John C. Sih

    CPC分类号: C07D307/937

    摘要: Acyl-substituted phenyl esters of prostacyclin-type compounds, for example the 4-acetylphenyl ester of prostacyclin (PGI.sub.2) illustrated by the formula ##STR1## and including esters of the isomeric 6-hydroxy-PGI.sub.1 and 6-keto-PGF.sub.1.alpha. compounds, said esters having pharmacological activity. Processes for preparing them and the appropriate intermediates are disclosed.

    摘要翻译: 前列环素型化合物的酰基取代的苯基酯,例如式IMAGE所示的前列环素的4-乙酰基苯基酯(PGI 2),并且包括异构体6-羟基-PGI1和6-酮-PGF1α化合物的酯, 所述酯具有药理活性。 公开了制备它们的方法和合适的中间体。

    Prostaglandin analogues
    89.
    发明授权

    公开(公告)号:US4215142A

    公开(公告)日:1980-07-29

    申请号:US940685

    申请日:1978-09-08

    摘要: Prostaglandin E.sub.1 analogues of the general formula: ##STR1## [wherein Y represents ethylene or trans-vinylene, Z represents ethylene or trans-vinylene, R.sup.1 represents a hydrogen atom, an alkyl group containing from 1 to 12 carbon atoms, an aralkyl group containing from 7 to 12 carbon atoms, a cycloalkyl group containing from 4 to 7 carbon atoms and unsubstituted or substituted by at least one alkyl group containing from 1 to 6 carbon atoms, a phenyl group unsubstituted or substituted by at least one chlorine atom, trifluoromethyl group, alkyl group containing from 1 to 4 carbon atoms or phenyl group, a --C.sub.m H.sub.2m COOR.sup.5 group (wherein m represents an integer of from 1 to 12 and R.sup.5 represents a hydrogen atom or an alkyl group containing from 1 to 4 carbon atoms), a --C.sub.n H.sub.2n OR.sup.6 group (wherein R.sup.6 represents a hydrogen atom or an alkyl group containing from 1 to 4 carbon atoms and n represents an integer of from 2 to 12), or a ##STR2## group (wherein R.sup.7 and R.sup.8 each represent a hydrogen atom or an alkyl group containing from 1 to 4 carbon atoms and n is as hereinbefore defined), R.sup.2 represents a hydrogen atom or a methyl or ethyl group, R.sup.3 represents a single bond or an alkylene group containing from 1 to 4 carbon atoms, R.sup.4 represents a hydrogen atom, an alkyl group containing from 1 to 8 carbon atoms, a cycloalkyl group containing from 4 to 7 carbon atoms and unsubstituted or substituted by at least one alkyl group containing from 1 to 8 carbon atoms, or represents a phenyl or phenoxy group unsubstituted or substituted by at least one chlorine atom, trifluoromethyl group or alkyl group containing from 1 to 3 carbon atoms, and the wavy line attached to the C-11 and C-15 carbon atoms represents .alpha.- or .beta.- configuration or mixtures thereof] and cyclodextrin clathrates thereof, and, when R.sup.1 represents a hydrogen atom or a group C.sub.m H.sub.2m COOR.sup.5 in which R.sup.5 represents a hydrogen atom, non-toxic salts thereof and, when R.sup.1 represents a group ##STR3## non-toxic acid addition salts thereof, are new compounds and possess characteristic prostaglandin-like properties.

    Enlarged-hetero-ring prosta-cyclin analogs
    90.
    发明授权
    Enlarged-hetero-ring prosta-cyclin analogs 失效
    扩增异环前列腺 - 细胞周期蛋白类似物

    公开(公告)号:US4210748A

    公开(公告)日:1980-07-01

    申请号:US932899

    申请日:1978-08-11

    申请人: Roy A. Johnson

    发明人: Roy A. Johnson

    摘要: Prostaglandin (PG.sub.1, derivatives having (1) a 5-keto feature, for example ##STR1## or (2) a 9-deoxy-5,9-epoxy feature together with a 4-halo or 5-hydroxy feature, for example ##STR2## or a 4,5-didehydro feature, for example in an enol ether of the formula ##STR3## said derivatives having pharmacological activity. Processes for preparing them and the appropriate intermediates are disclosed.

    摘要翻译: 前列腺素(PG1)具有(1)5-酮基特征的衍生物,例如或(2)9-脱氧-5,9-环氧基特征以及4-卤素或5-羟基特征, IMAGE>或“IMAGE”或4,5-二脱水特征,例如在式(Ⅰ)的烯醇醚中,所述具有药理学活性的衍生物具有制备它们的方法和合适的中间体。