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    • 3. 发明授权
    • Pharmaceuticals containing prostaglandin I.sub.2
    • 含有前列腺素I2的药物
    • US5053526A
    • 1991-10-01
    • US511945
    • 1990-04-16
    • Masakatsu ShibasakiMikiko SodeokaYuji OgawaToshiaki MaseAkira IshibashiDaijiro HoriiToshiji KanayamaKatsuhiko IsekiMasaki ShinodaChiyoko IshiyamaYoshio Hayashi
    • Masakatsu ShibasakiMikiko SodeokaYuji OgawaToshiaki MaseAkira IshibashiDaijiro HoriiToshiji KanayamaKatsuhiko IsekiMasaki ShinodaChiyoko IshiyamaYoshio Hayashi
    • A61K31/557C07C405/00
    • C07C405/0083A61K31/557
    • Disclosed is a pharmaceutical having circulation ameliorating effect and antiulcer effect containing a prostaglandin I.sub.2 analogue represented by the formula shown below or a non-toxic salt of its salt or a cyclodextrin inclusion compound thereof as the effective ingredient: ##STR1## wherein R.sup.1 represents a hydrogen atom, an alkyl group having 1 to 12 carbon atoms, a cycloalkyl group having 4 to 7 carbon atoms or a phenyl group; A represents a pentyl group, a cyclopentyl group, a cyclohexyl group, a 1-methyl-3-hexynyl group, a 2-methyl-3-hexynyl group, a 1-methylhexyl group, a 2-phenethyl group, a 1,1-dimethylpentyl group, a 2-methylpentyl group, a 1-cyclohexylethyl group, a 2-methylhexyl group, a 1-methyl-3-pentynyl group or 1 2,6-dimethyl-5-heptenyl group; the double bond between the carbon atoms at 4- and 5-positions is E or Z or a mixture thereof, the asymmetric center in the substituent represented by A is R-configuration or S-configuration or a mixture thereof.The pharmaceuticals containing, as an active ingredient, prostaglandin I.sub.2 analogues of the present invention have potent platelet aggregation inhibiting effect, blood pressure depressing effect, vasodilative effect and antiulcer effect, and are also low in toxicity.
    • 本发明公开了一种具有循环改善作用和抗溃疡效果的药物,其含有下述式表示的前列腺素I2类似物或其盐的无毒性盐或其环糊精包合物作为有效成分:其中R1表示氢 原子,碳原子数1〜12的烷基,碳原子数4〜7的环烷基或苯基; A表示戊基,环戊基,环己基,1-甲基-3-己炔基,2-甲基-3-己炔基,1-甲基己基,2-苯乙基,1,1 2-甲基戊基,2-甲基戊基,1-环己基乙基,2-甲基己基,1-甲基-3-戊炔基或1,6-二甲基-5-庚烯基; 在4-和5-位碳原子之间的双键是E或Z或其混合物,由A表示的取代基中的不对称中心是R-构型或S-构型或其混合物。 含有本发明的前列腺素I2类似物作为活性成分的药物具有有效的血小板聚集抑制作用,降血压作用,血管扩张作用和抗溃疡作用,毒性也低。
    • 4. 发明授权
    • (2-chloro-3-oxo-1-alkenyl)bicyclo(3.3.0)octane derivative
    • (2-氯-3-氧代-1-烯基)双环(3.3.0)辛烷衍生物
    • US4810805A
    • 1989-03-07
    • US943484
    • 1986-12-19
    • Masakatsu ShibasakiKatsuhiko IsekiMasaki ShinodaChiyoko AokiYoshio Hayashi
    • Masakatsu ShibasakiKatsuhiko IsekiMasaki ShinodaChiyoko AokiYoshio Hayashi
    • C07F9/38C07C67/343C07C69/738C07C405/00C07F9/40C07D309/12
    • C07C405/0083
    • There are disclosed a (2-chloro-3-oxo-1-alkenyl)-bicyclo[3.3.0 octene derivative represented by the formula: ##STR1## wherein R.sup.1 represents --CH.sub.2 CH.sub.2 CH.sub.2 COOR.sup.5, --CH.sub.2 CH.sub.2 --O--CH.sub.2 COOR.sup.5, --CH.dbd.CHCH.sub.2 COOR.sup.5 or --CH.sub.2 CH.sub.2 C.tbd.C--COOR.sup.5 group where R.sup.5 in the groups represents a hydrogen atom or an alkyl group having 1 to 6 carbon atoms; R.sup.2 represents a hydrogen atom, an acyl group having 1 to 7 carbon atoms, a tri(1 to 7 carbon atoms)-hydrocarbylsilyl group or a group forming an acetal bonding with an oxygen atom of a hydroxy group; R.sup.3 represents a straight or branched alkyl group having 3 to 10 carbon atoms, a cycloalkyl group having 4 to 7 carbon atoms, which may be substituted by at least one alkyl group having 1 to 4 carbon atoms, a straight or branched alkenyl group having 3 to 12 carbom atoms, a straight or branched alkynyl group having 3 to 8 carbon atoms, a phenyl group or a phenoxy group which may have substituents, an alkoxy group having 1 to 6 carbon atoms or an alkyl group substituted by a cycloalkyl group having 5 to 8 carbon atoms, and a process for preparing the same which comprises reacting an aldehyde represented by the formula: ##STR2## wherein R.sup.1 and R.sup.2 have the same meanings as defined above, with kotophosphonate represented by the formula: ##STR3## wherein R.sup.3 has the same meaning as defined above and R.sup.4 represents an alkyl group having 1 to 10 carbon atoms, in the presence of a base.
    • 公开了由下式表示的(2-氯-3-氧代-1-烯基) - 二环[3.3.0辛烯衍生物:其中R 1表示-CH 2 CH 2 CH 2 COOR 5,-CH 2 CH 2 -O-CH 2 COOR 5,-CH = CHCH 2 COOR 5 或-CH 2 CH 2 C 3 CON COROR 5基团,其中基团中的R 5表示氢原子或具有1至6个碳原子的烷基; R2表示氢原子,碳原子数1〜7的酰基,三(1〜7个碳原子) - 烃基甲硅烷基或与羟基形成缩醛键的基团。 R3表示可以被至少一个具有1至4个碳原子的烷基取代的具有3至10个碳原子的直链或支链烷基,具有4至7个碳原子的环烷基,具有3个碳原子的直链或支链烯基 至12个碳原子,具有3至8个碳原子的直链或支链炔基,可具有取代基的苯基或苯氧基,具有1至6个碳原子的烷氧基或被具有5个环烷基的环烷基取代的烷基 至8个碳原子,及其制备方法,其包括使由下式表示的醛:其中R 1和R 2具有与上述相同的含义,与下式表示的焦磷酸酯反应:其中R 3具有 在碱的存在下,与上述定义相同,R 4表示具有1至10个碳原子的烷基。