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1. 发明公开

EP0171992A2 Pharmaceuticals containing prostaglandin I2 失效
标题翻译： Arzneimittel死亡前列腺素I2窒息。
公开(公告)号：EP0171992A2
公开(公告)日：1986-02-19
申请号：EP85305611.7
申请日：1985-08-07
申请人： MITSUBISHI KASEI CORPORATION , SAGAMI CHEMICAL RESEARCH CENTER
发明人： Ishibashi, Akira , Horii, Daijiro , Kanayama, Toshiji , Iseki, Katsuhiko , Shinoda, Masaki , Ishiyama, Chiyoko , Hayashi, Yosio , Shibasaki, Masakatsu , Sodeoka, Mikiko , Ogawa, Yuji , Mase, Toshiaki
IPC分类号： A61K31/557
CPC分类号： C07C405/0083 , A61K31/557
摘要： Disclosed is a pharmaceutical having circulation ameliorating effect and antiulcer effect containing a prostaglandin I 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:
wherein R' 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-methythexyl 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 a 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 1 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.
摘要翻译：本发明公开了含有前列腺素I2，由下述通式表示的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的循环改善效果和抗溃疡作用的药物：其中R 1 >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，1,1-二甲基戊基，2-甲基戊基，1-环己基乙基，2-甲基己基基团，2,6-二甲基-5-庚烯基上的1-甲基-3-戊炔基，4-和5-位的碳原子之间的双键是E或Z或其混合物，不对称中心在由A表示的取代基中是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。

2. 发明授权

EP0171992B1 Pharmaceuticals containing prostaglandin I2 失效
标题翻译：含有PROSTAGLANDIN I2的药物
公开(公告)号：EP0171992B1
公开(公告)日：1990-06-06
申请号：EP85305611.7
申请日：1985-08-07
申请人： MITSUBISHI KASEI CORPORATION , SAGAMI CHEMICAL RESEARCH CENTER
发明人： Ishibashi, Akira , Horii, Daijiro , Kanayama, Toshiji , Iseki, Katsuhiko , Shinoda, Masaki , Ishiyama, Chiyoko , Hayashi, Yosio , Shibasaki, Masakatsu , Sodeoka, Mikiko , Ogawa, Yuji , Mase, Toshiaki
IPC分类号： A61K31/557
CPC分类号： C07C405/0083 , A61K31/557

3. 发明公开

EP0171992A3 Pharmaceuticals containing prostaglandin I2 失效
标题翻译：含有PROSTAGLANDIN I2的药物
公开(公告)号：EP0171992A3
公开(公告)日：1986-12-03
申请号：EP85305611
申请日：1985-08-07
申请人： Mitsubishi Yuka Pharmaceutical Co., Ltd. , SAGAMI CHEMICAL RESEARCH CENTER
发明人： Ishibashi, Akira , Horii, Daijiro , Kanayama, Toshiji , Iseki, Katsuhiko , Shinoda, Masaki , Ishiyama, Chiyoko , Hayashi, Yosio , Shibasaki, Masakatsu , Sodeoka, Mikiko , Ogawa, Yuji , Mase, Toshiaki
IPC分类号： A61K31/557 , C07C177/00
CPC分类号： C07C405/0083 , A61K31/557
摘要： Disclosed is a pharmaceutical having circulation ameliorating effect and antiulcer effect containing a prostaglandin I 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:
wherein R' 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-methythexyl 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 a 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 1 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.

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