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1. 发明授权

EP0171992B1 Pharmaceuticals containing prostaglandin I2 有权转让
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

2. 发明公开

EP0171992A2 Pharmaceuticals containing prostaglandin I2 有权转让
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。

3. 发明公开

EP0171992A3 Pharmaceuticals containing prostaglandin I2 有权转让
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.

4. 发明公开

EP0219436A2 Thiazole derivative and leukotriene antagonist containing the same as the effective ingredients 失效转让
标题翻译：噻唑衍生物以及含有它们作为活性成分的白三烯拮抗剂。
公开(公告)号：EP0219436A2
公开(公告)日：1987-04-22
申请号：EP86402327.0
申请日：1986-10-16
申请人： MITSUBISHI KASEI CORPORATION
发明人： Hayasi, Yosio , Oguri, Tomei , Shinoda, Masaki , Tsutsui, Mikio , Takahashi, Kazuo , Miida, Hitoshi
IPC分类号： C07D277/64 , A61K31/425 , C07D277/30 , C07D277/24 , C07D277/56 , C07D277/82 , C07D277/28 , C07D417/10 , A61K31/41
CPC分类号： C07D277/82 , C07D277/24 , C07D277/28 , C07D277/30 , C07D277/56 , C07D277/64
摘要： Disclosed are a thiazole derivative represented by the following formula, a pharmaceutically acceptable salt thereof and leukotriene antagonist containing the same as the active ingredients:
wherein R, and R z each independently represent a hydrogen atom, an alkyl group having 1 to 8 carbon atoms, a lower alkoxycarbonyl group or a substituted or unsubstituted phenyl group or cooperatively represent a tetramethylene group corresponding to a fused cyclohexane ring or a butadienylene group which is unsubstituted or substituted with a halogen atom, a lower alkoxy group, a lower alkoxycarbonyl group or an alkyl group having 1 to 3 carbon atoms corresponding to a fused benzene ring; R 3 , R 4 , R 5 and R 6 each independently represent a hydrogen atom, a hydroxyl group, a lower alkoxy group, an alkyl group having 1 to 3 carbon atoms or a halogen atom; A represents a linking group having 2 to 4 chain members; B represents a linking group having 2 to 5 chain members; and Q represents a carboxyl group, a lower alkoxy group, a hydroxyl group, an alkoxycarbonyl group having 2 to 6 carbon atoms or a 5-tetrazolyl group.

5. 发明公开

EP0228959A2 Aminostyryl compound, leukotriene antagonistic composition containing the same as effective ingredients and method of antagonizing SRS by employing the same 失效转让
标题翻译：氨基苯乙烯基化合物，以及含有它们作为有效成分的白三烯拮抗物组合物和方法通过其使用SRS来抵消。
公开(公告)号：EP0228959A2
公开(公告)日：1987-07-15
申请号：EP86402855.0
申请日：1986-12-18
申请人： MITSUBISHI KASEI CORPORATION
发明人： Hayashi, Yoshio , Oguri, Tomei , Shinoda, Masaki , Takahashi, Kazuo
IPC分类号： C07D215/12 , C07D333/58 , C07D263/56 , C07D235/14 , C07D213/40 , C07D217/18 , C07D239/91 , C07D239/74 , C07D241/12 , C07D239/26 , A61K31/33
CPC分类号： C07D213/40 , C07C233/07 , C07C233/09 , C07D215/12 , C07D217/18 , C07D235/14 , C07D237/08 , C07D239/26 , C07D239/74 , C07D239/91 , C07D241/12 , C07D263/56 , C07D333/58
摘要： Disclosed are an aminostyryl compound represented by Formula I:
wherein A represents a linking group having 3 to 4 chain members; B represents an unsubstituted or substituted 5 to 6-membered monocyclic type heterocyclic residue containing 1 to 2 hetero atoms, an unsubstituted or substituted condensed heterocyclic residue which contains 5 to 6-membered monocyclic type heterocycle containing 1 to 2 hetero atoms, a naphthyl group or an alkyl group having 5 to 7 carbon atoms. a composition having leukotriene antagonism which contains an aminostyryl compound represented by Formula I as the effective ingredient, and a method of antagonizing SRS based on leukotriene antagonistic activity by employing the same.

6. 发明授权

EP0219436B1 Thiazole derivative and leukotriene antagonist containing the same as the effective ingredients 失效转让
标题翻译：噻唑衍生物以及含有它们作为活性成分的白三烯拮抗剂。
公开(公告)号：EP0219436B1
公开(公告)日：1993-12-22
申请号：EP86402327.0
申请日：1986-10-16
申请人： MITSUBISHI KASEI CORPORATION
发明人： Hayasi, Yosio , Oguri, Tomei , Shinoda, Masaki , Tsutsui, Mikio , Takahashi, Kazuo , Miida, Hitoshi
IPC分类号： C07D277/64 , A61K31/425 , C07D277/30 , C07D277/24 , C07D277/56 , C07D277/82 , C07D277/28 , C07D417/10 , A61K31/41
CPC分类号： C07D277/82 , C07D277/24 , C07D277/28 , C07D277/30 , C07D277/56 , C07D277/64

7. 发明公开

EP0234158A1 (2-Chloro-3-oxo-1-alkenyl)bicyclo (3.3.0.) octene derivative and process for preparing the same 失效
标题翻译：（2-氯-3-氧代-1-烯基）-bicyclo¬3.3.0octenderivat和过程及其制备
公开(公告)号：EP0234158A1
公开(公告)日：1987-09-02
申请号：EP86402925.1
申请日：1986-12-23
申请人： MITSUBISHI KASEI CORPORATION
发明人： Shibasaki, Masakatsu , Iseki, Katsuhiko , Shinoda, Masaki , Aoki, Chiyoko , Hayashi, Yoshio
IPC分类号： C07C177/00
CPC分类号： C07C405/0083
摘要： There are disclosed a (2-chloro-3-oxo-l-alkenyl)bicyclo[3.3.0]octene derivative represented by the formula:
wherein R' represents -CH 2 CH 2 CH 2 CH 2 COOR 5 , -CH 2 CH 2 -O-CH 2 COOR 5 , -CH=CHCH 2 CH 2 COOR 5 or -CH 2 CH 2 C≡C-COOR 5 group where R 5 in the groups represents a hydrogen atom or an alkyl group having I to 6 carbon atoms; R 2 represents a hydrogen atom, an acyl group having I to 7 carbon atoms, a tri(I to 7 carbon atoms)hydrocarbylsilyl group or a group forming an acetal bonding with an oxygen atom of a hydroxy group; R 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 I to 4 carbon atoms, a straight or branched alkenyl group having 3 to 12 carbon 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 I 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:
wherein R 1 and R 2 have the same meanings as defined above, with kotophosphonate represented by the formula:
wherein R 3 has the same meaning as defined above and R 4 represents an alkyl group having I to 10 carbon atoms, in the presence of a base.

8. 发明授权

EP0287471B1 Carboxystyrene derivatives and drugs containing them as effective ingredients 失效
标题翻译：羧甲基衍生物和含有它们作为有效成分的药物
公开(公告)号：EP0287471B1
公开(公告)日：1992-09-09
申请号：EP88400910.1
申请日：1988-04-14
申请人： MITSUBISHI KASEI CORPORATION
发明人： Hayashi, Yoshio , Oguri, Tomei , Shinoda, Masaki , Takahashi Kazuo , Hashimoto, Munehiro
IPC分类号： C07D277/30 , C07D277/64 , C07D215/12 , C07D239/91 , C07D239/74 , C07D241/38 , C07D235/16 , A61K31/425 , A61K31/47 , A61K31/495 , A61K31/40
CPC分类号： C07D233/64 , C07D215/12 , C07D235/16 , C07D239/74 , C07D239/90 , C07D241/42 , C07D277/30 , C07D277/56 , C07D277/64

9. 发明公开

EP0396973A1 4-Imidazoline derivatives and their use in preparing pharmaceutical compositions 失效
标题翻译： 4-咪唑啉衍生物和它们用于制备药物制剂的用途。
公开(公告)号：EP0396973A1
公开(公告)日：1990-11-14
申请号：EP90107993.9
申请日：1990-04-26
申请人： MITSUBISHI KASEI CORPORATION
发明人： Hayashi, Yoshio , Morinaka, Yasuhiro , Shinoda, Masaki , Nishi, Hiroyoshi , Watanabe, Kazutoshi , Fukushima, Nobuko
IPC分类号： C07D233/70 , A61K31/415
CPC分类号： C07D233/70
摘要： 4-lmidazoline derivatives represented by the formula (I) and/or formula (II):
wherein R 1 represents C 1 -C 8 alkyl, C 3 -C 8 alkenyl, C 3 -Cs alkynyl, C 3 -C 8 cycloalkyl, or optionally substituted aralkyl; R 2 and R 3 independently represent hydrogen, C 3 -C 20 alkyl, C 3 -C 20 alkenyl, C 3 -C 20 alkynyl, C 3 -C 20 alkoxy, C 3 -C 20 alkenyloxy, C 3 -C 20 alkynyloxy, C 3 -C S cycloalkyl, C 1 -C 10 alkylthio, or optionally substituted aralkyl or aralkyloxy; R 4 represents C 1 -C 6 alkyl, C 3 -C 8 cycloalkyl, or optionally substituted aralkyl; provided that R 2 and R 3 cannot be hydrogen at the same time, and pharmaceutically acceptable salts thereof. A pharmaceutical formulation containing the compound is also provided.
摘要翻译：由式（I）和/或式表示的4-咪唑啉衍生物（II）：其中，R <1>表示C1-C8烷基，C3-C8链烯基，C3-C8炔基，C3-C8环烷基，或任选取代的芳烷基; [R <3>代表氢unabhängig<2>和R，C3-C20烷基，C3-C20链烯基，C3-C20炔基，C3-C20烷氧基，C3-C20链烯氧基，C3-C20炔氧基，C3-C8环烷基，C1 C10烷硫基，或任选取代的芳烷基或芳烷氧基; [R <4> darstellt C1-C6烷基，C3-C8环烷基，或任选取代的芳烷基; 提供确实ř<2>和R <3>不能同时为氢，以及它们药学上可接受的盐。因此，提供含有该化合物的药物制剂。

10. 发明公开

EP0219436A3 Thiazole derivative and leukotriene antagonist containing the same as the effective ingredients 失效转让
标题翻译：含有有效成分的噻唑衍生物和亮氨酸拮抗剂
公开(公告)号：EP0219436A3
公开(公告)日：1989-12-27
申请号：EP86402327.0
申请日：1986-10-16
申请人： MITSUBISHI KASEI CORPORATION
发明人： Hayasi, Yosio , Oguri, Tomei , Shinoda, Masaki , Tsutsui, Mikio , Takahashi, Kazuo , Miida, Hitoshi
IPC分类号： C07D277/64 , A61K31/425 , C07D277/30 , C07D277/24 , C07D277/56 , C07D277/82 , C07D277/28 , C07D417/10 , A61K31/41
CPC分类号： C07D277/82 , C07D277/24 , C07D277/28 , C07D277/30 , C07D277/56 , C07D277/64
摘要： Disclosed are a thiazole derivative represented by the following formula, a pharmaceutically acceptable salt thereof and leukotriene antagonist containing the same as the active ingredients:
wherein R, and R z each independently represent a hydrogen atom, an alkyl group having 1 to 8 carbon atoms, a lower alkoxycarbonyl group or a substituted or unsubstituted phenyl group or cooperatively represent a tetramethylene group corresponding to a fused cyclohexane ring or a butadienylene group which is unsubstituted or substituted with a halogen atom, a lower alkoxy group, a lower alkoxycarbonyl group or an alkyl group having 1 to 3 carbon atoms corresponding to a fused benzene ring; R 3 , R 4 , R 5 and R 6 each independently represent a hydrogen atom, a hydroxyl group, a lower alkoxy group, an alkyl group having 1 to 3 carbon atoms or a halogen atom; A represents a linking group having 2 to 4 chain members; B represents a linking group having 2 to 5 chain members; and Q represents a carboxyl group, a lower alkoxy group, a hydroxyl group, an alkoxycarbonyl group having 2 to 6 carbon atoms or a 5-tetrazolyl group.

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