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1. 发明授权

US4810805A (2-chloro-3-oxo-1-alkenyl)bicyclo(3.3.0)octane derivative 失效
标题翻译：（2-氯-3-氧代-1-烯基）双环（3.3.0）辛烷衍生物
公开(公告)号：US4810805A
公开(公告)日：1989-03-07
申请号：US943484
申请日：1986-12-19
申请人： Masakatsu Shibasaki , Katsuhiko Iseki , Masaki Shinoda , Chiyoko Aoki , Yoshio Hayashi
发明人： Masakatsu Shibasaki , Katsuhiko Iseki , Masaki Shinoda , Chiyoko Aoki , Yoshio Hayashi
IPC分类号： C07F9/38 , C07C67/343 , C07C69/738 , C07C405/00 , C07F9/40 , C07D309/12
CPC分类号： C07C405/0083
摘要： 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.
摘要翻译：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。

2. 发明授权

US4839388A Prostacyclins and pharmaceuticals containing the same 失效
标题翻译：前列环素和含有相同的药物
公开(公告)号：US4839388A
公开(公告)日：1989-06-13
申请号：US060870
申请日：1987-05-18
申请人： Masakatsu Sibasaki , Mikiko Sodeoka , Katsuhiko Iseki , Masaki Shinoda , Chiyoko Aoki , Yosio Hayasi , Toshiji Kanayama
发明人： Masakatsu Sibasaki , Mikiko Sodeoka , Katsuhiko Iseki , Masaki Shinoda , Chiyoko Aoki , Yosio Hayasi , Toshiji Kanayama
IPC分类号： C07C59/125 , A61K31/557 , A61K31/695 , A61P1/04 , A61P7/02 , A61P9/08 , A61P9/12 , C07C51/00 , C07C59/46 , C07C59/54 , C07C59/62 , C07C59/64 , C07C59/72 , C07C67/00 , C07C69/03 , C07C69/708 , C07C69/732 , C07C69/734 , C07C231/00 , C07C235/06 , C07C235/30 , C07C235/34 , C07C405/00 , C07D295/18 , C07F7/18
CPC分类号： C07C405/0083
摘要： This invention relates to a novel prostacyclin represented by the formula: ##STR1## [wherein R.sup.1 represents --CO.sub.2 R.sup.5 group or --CONR.sup.6 R.sup.7 group; A is(i) --CH.dbd.CH--CH.sub.2 CH.sub.2 -- or(ii) --CH.sub.2 CH.sub.2 --O--CH.sub.2 --;B represents --C.tbd.C-- group; R.sup.2 represents an alkyl group, a cycloalkyl group, an alkenyl group, an alkynyl group, a phenyl group or a phenoxy group;R.sup.3 represents a hydrogen atom, a methyl group or a vinyl group; R.sup.4 represents a hydrogen atom, an acyl group, a tri(1 to 7 carbon atoms)hydrocarbyl-silyl group or a group forming an acetal bond with an oxygen atom of a hydroxy group; a double bond in the substituent represented by A is E or Z, or a mixture thereof; asymmetric center in the substituent represented by R.sup.2 is an R-configuration or S-configuration, or a mixture thereof];and uses in which they are employed as circulation ameliorating pharmaceuticals for blood flow ameliorating, antithrombus and the like, or antiulcer pharmaceuticals.
摘要翻译： PCT No.PCT / JP86 / 00486 Sec。 371日期1987年5月18日 102（e）日期1987年5月18日PCT提交1986年9月18日PCT公布。公开号WO87 / 01696 日本公开号为1987年3月26日。本发明涉及由下式表示的新型前列环素：其中R1表示-CO2R5基或-CONR6R7基; A是（i）-CH = CH-CH 2 CH 2 - 或（ii）-CH 2 CH 2 -O-CH 2 - ; B表示-C3OND C-基团; R2表示烷基，环烷基，烯基，炔基，苯基或苯氧基; R3表示氢原子，甲基或乙烯基; R 4表示氢原子，酰基，三（1〜7个碳原子）烃基 - 甲硅烷基或与羟基的氧原子形成缩醛键的基团。由A表示的取代基中的双键为E或Z，或其混合物; 由R2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]; 以及它们被用作改善血流改善药物的循环改善剂，抗凝血剂等或抗溃疡药物的用途。

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