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    • 4. 发明授权
    • Thiaprostaglandin E.sub.1 derivatives, process for production thereof,
and pharmaceutical use thereof
    • Thiaprostaglandin E1衍生物,其制备方法及其药物用途
    • US4466980A
    • 1984-08-21
    • US316902
    • 1981-10-30
    • Toshio TanakaTakeshi ToruTakeo ObaNoriaki OkamuraKenzo WatanabeKiyoshi BannaiAtsuo HazatoSeizi KurozumiFukuyoshi KamimotoAkira Ohtsu
    • Toshio TanakaTakeshi ToruTakeo ObaNoriaki OkamuraKenzo WatanabeKiyoshi BannaiAtsuo HazatoSeizi KurozumiFukuyoshi KamimotoAkira Ohtsu
    • C07C405/00C07D309/12C07C177/00A61K31/557
    • C07C405/0033C07D309/12
    • A novel compound selected from the group consisting of 7-(or 6- or 4-)thiaprostaglandin E.sub.1 derivatives of the formula (I). ##STR1## wherein A represents --CH.sub.2 -- or ##STR2## in which n is 0, 1 or 2, provided that only one A cut of three is ##STR3## R.sup.1 -R.sup.7 and G are as defined in the specification, the 15-epimers of said thiaprostaglandin E.sub.1 derivatives, the enatiomers of said thiaprostaglandin E.sub.1 derivatives or their 15-epimers, and mixtures of these compounds.A 7-thiaprostaglandin E.sub.1 derivative and/or its optical isomer may be prepared by reacting a 2-organo-2-cyclopentenone (II) with an organic copper-lithium compound (III) to effect conjugation reaction. A 6-thiaprostaglandin E.sub.1 derivative and/or its optical isomer may be prepared by subjecting an .alpha.,.beta.-unsaturated ketone (IV) and a thiol (V) to the Michael addition reaction. And, 4-thiaprostaglandin derivative and/or its optical isomer may also be prepared by the Michael addition reaction from a 2-allyl substituted cyclopentanone (VI) and a thiol (VIII).Some compounds ((I)-1) amongst the compounds of the formula (I) and/or their optical isomer are useful for controlling vascular actions such as angina pectoris, vasodilation etc.
    • 选自式(I)的7-(或6-或4-)赖氨酸前列腺素E1衍生物的新化合物。 (I)其中A表示-CH 2 - 或,其中n为0,1或2,条件是三个只有一个A切割是R 1 -R 7,G如说明书中所定义, 所述thiaprostaglandin E1衍生物的15-差向异构体,所述thiaprostaglandin E1衍生物或它们的15-差向异构体的对映体,以及这些化合物的混合物。 7-硫代前列腺素E1衍生物和/或其旋光异构体可以通过2-有机-2-环戊烯酮(II)与有机铜 - 锂化合物(III)反应来制备共轭反应。 6-硫代前列腺素E1衍生物和/或其旋光异构体可以通过使α,β-不饱和酮(IV)和硫醇(V)进行迈克尔加成反应来制备。 并且,也可以通过从2-烯丙基取代的环戊酮(VI)和硫醇(VIII)的迈克尔加成反应制备4-硫代前列腺素衍生物和/或其旋光异构体。 式(I)化合物和/或其旋光异构体中的一些化合物((I)-1)可用于控制血管作用,例如心绞痛,血管舒张等。
    • 9. 发明授权
    • 7-thiaprostaglandins E, and process for producing same
    • 7-硫代前列腺素E及其制备方法
    • US5159102A
    • 1992-10-27
    • US526682
    • 1990-05-22
    • Toshio TanakaKiyoshi BannaiAtsuo HazatoSeizi Kurozumi
    • Toshio TanakaKiyoshi BannaiAtsuo HazatoSeizi Kurozumi
    • C07C405/00
    • C07C405/0033
    • 7-thiaprostaglandins E.sub.1 which are compounds represented by the following formula [I] or their enantiomers or mixtures thereof in any ratio: ##STR1## where R.sup.1 represents a hydrogen atom, a C.sub.1 -C.sub.10 alkyl group, a C.sub.2 -C.sub.20 alkenyl group, a substituted or unsubstituted phenyl group, a substituted or unsubstituted C.sub.3 -C.sub.10 cycloalkyl group, a substituted or unsubstituted phenyl (C.sub.1 -C.sub.2) alkyl group, or one equivalent cation; R.sup.2 and R.sup.3, which may be the same or different, represent a hydrogen atom, a tri (C.sub.1 -C.sub.7) hydrocarbon silyl group, or a group forming an acetal linkage together with an oxygen atom of a hydroxyl group; R.sup.4 represents a hydrogen atom, a methyl group or a vinyl group; R.sup.5 represents a linear or branched C.sub.3 -C.sub.8 alkyl group, a linear or branched C.sub.3 -C.sub.8 alkenyl group, a linear or branched C.sub.2 -C.sub.8 alkynyl group, a phenyl group which may be substituted, a phenoxy group which may be substituted, a C.sub.3 -C.sub.10 cycloalkyl group which may be substituted, or a linear or branched C.sub.1 -C.sub.5 alkyl group which may be substituted with a C.sub.1 -C.sub.6 alkoxy group, a phenyl group which may be substituted, a phenoxy group which may be substituted or a C.sub.3 -C.sub.10 cycloalkyl group which may be substituted; X represents an ethylene group, a vinylene group or an ethylene group; n represents 0 or 1; the expression represents an ethylene group or a vinylene group, provided that when n is o and x is an ethylene group, R.sup.5 is not a linear or branched C.sub.3 -C.sub.8 alkyl group or a C.sub.3 -C.sub.10 cycloalkyl group which may be substituted.Such compounds are especially useful for the treatment and prevention of digestive organ diseases such as a duodenal ulcer or a gastric ulcer.
    • 作为由下式[I]表示的化合物或其对映异构体或其混合物的7-硫代前列腺素E1为任意比例:其中R 1表示氢原子,C 1 -C 10烷基,C 2 -C 20链烯基 取代或未取代的苯基,取代或未取代的C3-C10环烷基,取代或未取代的苯基(C1-C2)烷基或一个当量的阳离子; R2和R3可以相同或不同,表示氢原子,三(C1-C7)烃甲硅烷基或与羟基的氧原子一起形成缩醛键的基团; R4表示氢原子,甲基或乙烯基; R 5表示直链或支链C 3 -C 8烷基,直链或支链C 3 -C 8烯基,直链或支链C 2 -C 8炔基,可被取代的苯基,可被取代的苯氧基,C3 可以被取代的C 10环烷基,或可以被C 1 -C 6烷氧基取代的直链或支链C 1 -C 5烷基,可被取代的苯基,可被取代的苯氧基或C 3 -C 6烷氧基, 可被取代的C 10环烷基; X表示亚乙基,亚乙烯基或亚乙基; n表示0或1; 该表达式表示亚乙基或亚乙烯基,条件是当n是o且x是亚乙基时,R 5不是直链或支链C 3 -C 8烷基或可被取代的C 3 -C 10环烷基。 这些化合物特别可用于治疗和预防消化器官疾病如十二指肠溃疡或胃溃疡。
    • 10. 发明授权
    • Novel isocarbacyclins and processes for production thereof
    • 新型异卡波菌素及其制备方法
    • US4788319A
    • 1988-11-29
    • US44957
    • 1987-05-01
    • Atsuo HazatoToshio TanakaNoriaki OkamuraKiyoshi BannaiKurozumi, SeiziSuzuki, MasaakiNoyori, Ryoji
    • Atsuo HazatoToshio TanakaNoriaki OkamuraKiyoshi BannaiKurozumi, SeiziSuzuki, MasaakiNoyori, Ryoji
    • C07C405/00C07C147/107
    • C07C405/0025C07C405/0083
    • A novel isocarbacyclin which is a compound represented by the following formula ##STR1## wherein R.sup.1 represents a hydrogen atom, or a C.sub.1 -C.sub.4 alkyl or alkenyl group; R.sup.2 and R.sup.3 are identical or different and each represents a hydrogen atom, a tri(C.sub.1 -C.sub.7)hydrocarbon-silyl group or a group forming an acetal linkage together with the oxygen atom of the hydroxyl group; R.sup.4 represents a hydrogen atom, a methyl group or a vinyl group; R.sup.5 represents an unsubstituted linear or branched C.sub.3 -C.sub.8 alkyl group which may be interrupted by an oxygen atom, a substituted linear or branched C.sub.1 -C.sub.5 group in which the substituent is a C.sub.1 -C.sub.6 alkoxy group or a phenyl, phenoxy or C.sub.3 -C.sub.10 cycloalkyl group which may be substituted further, a phenyl group which may be substituted, a phenoxy group which may be substituted, or a C.sub.3 -C.sub.10 cycloalkyl group which may be substituted; n is 0 or 1; and Ar represents a substituted or unsubstituted phenyl group, its enantiomorph, or a mixture both in an arbitrary ratio.
    • 一种新颖的异卡巴环素,它是由下式表示的化合物:其中R 1表示氢原子或C 1 -C 4烷基或烯基; R2和R3相同或不同,各自表示氢原子,三(C1-C7)烃 - 甲硅烷基或与羟基的氧原子一起形成缩醛键的基团; R4表示氢原子,甲基或乙烯基; R5表示可被氧原子取代的未取代的直链或支链C 3 -C 8烷基,其中取代基为C 1 -C 6烷氧基的取代的直链或支链C 1 -C 5基或苯基,苯氧基或C 3 -C 10 可以被取代的环烷基,可被取代的苯基,可被取代的苯氧基或可被取代的C3-C10环烷基; n为0或1; Ar表示取代或未取代的苯基,其对映体或任意比例的混合物。