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11. 发明授权

US5053526A Pharmaceuticals containing prostaglandin I.sub.2 失效
标题翻译：含有前列腺素I2的药物
公开(公告)号：US5053526A
公开(公告)日：1991-10-01
申请号：US511945
申请日：1990-04-16
申请人： Masakatsu Shibasaki , Mikiko Sodeoka , Yuji Ogawa , Toshiaki Mase , Akira Ishibashi , Daijiro Horii , Toshiji Kanayama , Katsuhiko Iseki , Masaki Shinoda , Chiyoko Ishiyama , Yoshio Hayashi
发明人： Masakatsu Shibasaki , Mikiko Sodeoka , Yuji Ogawa , Toshiaki Mase , Akira Ishibashi , Daijiro Horii , Toshiji Kanayama , Katsuhiko Iseki , Masaki Shinoda , Chiyoko Ishiyama , Yoshio Hayashi
IPC分类号： A61K31/557 , C07C405/00
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.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.
摘要翻译：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。

12. 发明授权

US4857542A Prophylactic and therapeutic composition for circulatory disorders and method of treatment 失效
标题翻译：循环障碍的预防和治疗组合物及治疗方法
公开(公告)号：US4857542A
公开(公告)日：1989-08-15
申请号：US122516
申请日：1987-11-19
申请人： Hiroyoshi Nishi , Toshiaki Watanabe , Satoshi Yuki , Yasuhiro Morinaka , Katsuhiko Iseki , Hiroko Sakurai
发明人： Hiroyoshi Nishi , Toshiaki Watanabe , Satoshi Yuki , Yasuhiro Morinaka , Katsuhiko Iseki , Hiroko Sakurai
IPC分类号： C07D231/20 , C07D231/22 , C07D231/26 , C07D231/28 , C07D231/56
CPC分类号： C07D231/56 , C07D231/20 , C07D231/22 , C07D231/26 , C07D231/28
摘要： A prophylactic and therapeutic agent for circulatory disorders, comprising a pyrazolone derivative of the formula: ##STR1## wherein R.sub.1 represents a hydrogen atom, an aryl group, an alkyl group having 1 to 5 carbon atoms or an alkoxycarbonylalkyl group having a total carbon number of 3 to 6; R.sub.2 represents a hydrogen atom, an aryloxy group, an arylmercapto group, an alkyl group having 1 to 5 carbon atoms or hydroxyalkyl group having 1 to 3 carbon atoms; or R.sub.1 and R.sub.2 taken together represent an alkylene group having 3 to 5 carbon atoms; R.sub.3 represents a hydrogen atom, an alkyl group having 1 to 5 carbon atoms, a cycloalkyl group having 5 to 7 carbon atoms, a hydroxyalkyl group having 1 to 3 carbon atoms, a benzyl group, a naphthyl group, or a phenyl group which is unsubstituted or substituted with 1 to 3 substituents which are the same or different selected from the group consisting of alkyl groups having 1 to 5 carbon atoms, alkoxy groups having 1 to 5 carbon atoms, hydroxyalkyl groups having 1 to 3 carbon atoms, alkoxycarbonyl groups having total carbon number of 2 to 5, alkylmercapto groups having 1 to 3 carbon atoms, alkylamino groups having 1 to 4 carbon atoms, dialkylamino groups having total carbon number of 2 to 8, halogen atoms, trifluoromethyl group, carboxyl group, cyano group, hydroxyl group, nitro group, amino group and acetamide group,or a pharmaceutically acceptable salt thereof as an acitve ingredient.The agent of the present invention is useful as a prophylactic and therapeutic agent for circulatory disorders, particularly as an inhibitor agaisnt lipid peroxidation and/or an agent for normalizing cerebral dysfunctions.
摘要翻译：一种循环系统疾病的预防和治疗剂，其包含下式的吡唑啉酮衍生物：其中R 1表示氢原子，芳基，具有1至5个碳原子的烷基或具有总碳数的烷氧基羰基烷基 3至6; R2表示氢原子，芳氧基，芳基巯基，碳原子数1〜5的烷基或碳原子数1〜3的羟烷基。或R 1和R 2一起表示具有3至5个碳原子的亚烷基; R3表示氢原子，碳原子数1〜5的烷基，碳原子数5〜7的环烷基，碳原子数1〜3的羟烷基，苄基，萘基或苯基，未取代或被1〜3个选自碳原子数1〜5的烷基，碳原子数为1〜5的烷氧基，碳原子数1〜3的烷氧基，碳原子数1〜3的烷氧基，烷氧基羰基，总碳数为2至5，具有1至3个碳原子的烷基巯基，具有1至4个碳原子的烷基氨基，总碳数为2至8的二烷基氨基，卤素原子，三氟甲基，羧基，氰基，羟基基团，硝基，氨基和乙酰胺基，或其药学上可接受的盐作为acitve成分。本发明的药剂可用作循环障碍的预防和治疗剂，特别是作为抑制剂脂质过氧化作用的抑制剂和/或用于使脑功能障碍正常化的药剂。

13. 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。

14. 发明授权

US08575175B2 Therapeutic agent for chronic renal failure 有权
标题翻译：慢性肾衰竭治疗剂
公开(公告)号：US08575175B2
公开(公告)日：2013-11-05
申请号：US13055242
申请日：2009-07-23
申请人： Fuko Matsuda , Katsuhiko Iseki , Hajimu Kurumatani , Mitsuko Miyamoto
发明人： Fuko Matsuda , Katsuhiko Iseki , Hajimu Kurumatani , Mitsuko Miyamoto
IPC分类号： A61K31/4965
CPC分类号： C07D241/20 , A61K31/4965
摘要： The present invention aims to provide a therapeutic agent for chronic renal failure, comprising as an effective ingredient a compound represented by General Formula (1) or a pharmaceutically acceptable salt thereof. That is, the present invention provides provision of a drug comprising as an effective ingredient a compound represented by General Formula (1) or a pharmaceutically acceptable salt thereof, which drug is useful not only for amelioration of renal function, but also for amelioration of anemia, activation of SOD and excretion of uremic substances.
摘要翻译：本发明旨在提供一种用于慢性肾功能衰竭的治疗剂，其包含作为有效成分的由通式（1）表示的化合物或其药学上可接受的盐。也就是说，本发明提供包含作为有效成分的由通式（1）表示的化合物或其药学上可接受的盐的药物的提供，该药物不仅可用于改善肾功能，还可用于改善贫血，激活SOD和排泄尿毒症物质。

15. 再颁专利

USRE35801E Prophylactic and therapeutic composition for circulatory disorders and method of treatment 失效
标题翻译：循环障碍的预防和治疗组合物及治疗方法
公开(公告)号：USRE35801E
公开(公告)日：1998-05-19
申请号：US309558
申请日：1994-09-20
申请人： Hiroyoshi Nishi , Toshiaki Watanabe , Satoshi Yuki , Yasuhiro Morinaka , Katsuhiko Iseki , Hiroko Nakajima (nee Sakurai)
发明人： Hiroyoshi Nishi , Toshiaki Watanabe , Satoshi Yuki , Yasuhiro Morinaka , Katsuhiko Iseki , Hiroko Nakajima (nee Sakurai)
IPC分类号： C07D231/20 , C07D231/22 , C07D231/26 , C07D231/28 , C07D231/56 , A61K31/415
CPC分类号： C07D231/56 , C07D231/20 , C07D231/22 , C07D231/26 , C07D231/28
摘要： A prophylactic and therapeutic agent for circulatory disorders, comprising a pyrazolone derivative of the formula: ##STR1## wherein R.sub.1 represents a hydrogen atom, an aryl group, an alkyl group having 1 to 5 carbon atoms or an alkoxycarbonylalkyl group having a total carbon number of 3 to 6; R.sub.2 represents a hydrogen atom, an aryloxy group, an arylmercapto group, an alkyl group having 1 to 5 carbon atoms or hydroxyalkyl group having 1 to 3 carbon atoms or R.sub.1 and R.sub.2 taken together represent an alkylene group having 3 to 5 carbon atoms; R.sub.3 represents a hydrogen atom, an alkyl group having 1 to 5 carbon atoms, a cycloalkyl group having 5 to 7 carbon atoms, a hydroxyalkyl group having 1 to 3 carbon atoms, a benzyl group, a naphthyl group, or a phenyl group which is unsubstituted or substituted with 1 to 3 substituents which are the same or different selected from the group consisting of alkyl groups having 1 to 5 carbon atoms, alkoxy groups having 1 to 5 carbon atoms, hydroxyalkyl groups having 1 to 3 carbon atoms, alkoxycarbonyl groups having total carbon number of 2 to 5, alkylmercapto groups having 1 to 3 carbon atoms, alkylamino groups having 1 to 4 carbon atoms, dialkylamino groups having total carbon number of 2 to 8, halogen atoms, trifluoromethyl group, carboxyl group, cyano group, hydroxyl group, nitro group, amino group and acetamide group, or a pharmaceutically acceptable salt thereof as an active ingredient. The agent of the present invention is useful as a prophylactic and therapeutic agent for circulatory disorders, particularly as an inhibitor against lipid peroxidation and/or an agent for normalizing cerebral dysfunctions.
摘要翻译：一种循环系统疾病的预防和治疗剂，其包含下式的吡唑啉酮衍生物：其中R 1表示氢原子，芳基，具有1至5个碳原子的烷基或具有总碳数的烷氧基羰基烷基 3至6; R 2表示氢原子，芳氧基，芳基巯基，碳原子数1〜5的烷基或碳原子数1〜3的羟烷基，或者R 1和R 2一起表示碳原子数3〜5的亚烷基。 R3表示氢原子，碳原子数1〜5的烷基，碳原子数5〜7的环烷基，碳原子数1〜3的羟烷基，苄基，萘基或苯基，未取代或被1〜3个选自碳原子数1〜5的烷基，碳原子数为1〜5的烷氧基，碳原子数1〜3的烷氧基，碳原子数1〜3的烷氧基，烷氧基羰基，总碳数为2至5，具有1至3个碳原子的烷基巯基，具有1至4个碳原子的烷基氨基，总碳数为2至8的二烷基氨基，卤素原子，三氟甲基，羧基，氰基，羟基基团，硝基，氨基和乙酰胺基，或其药学上可接受的盐作为活性成分。本发明的药剂可用作循环障碍的预防和治疗剂，特别是作为抗脂质过氧化作用的抑制剂和/或用于使脑功能障碍正常化的药剂。

16. 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。

17. 发明授权

US4668677A 4-phenylphthalazine derivatives, their preparation and their use as pharmaceuticals 失效
标题翻译： 4-苯基酞嗪衍生物，它们的制备及其作为药物的用途
公开(公告)号：US4668677A
公开(公告)日：1987-05-26
申请号：US722304
申请日：1985-04-11
申请人： Yasuhiro Morinaka , Katsuhiko Iseki , Toshiji Kanayama , Toshiaki Watanabe , Hiroyoshi Nishi
发明人： Yasuhiro Morinaka , Katsuhiko Iseki , Toshiji Kanayama , Toshiaki Watanabe , Hiroyoshi Nishi
IPC分类号： A61K31/50 , A61K31/502 , A61P7/02 , A61P9/00 , C07D237/34 , C07D237/30
CPC分类号： C07D237/34
摘要： Certain new 1-alkylamino-4-phenylphthalazine derivatives, 1-neopentylamino-4-phenylphthalazine and 1-(1-ethylpropylamino)-4-phenylphthalazine, having prominent activity to ameliorate circulatory disorders and prepared from the corresponding phthalazinones.
摘要翻译：某些新的1-烷基氨基-4-苯基酞嗪衍生物，1-新戊基氨基-4-苯基酞嗪和1-（1-乙基丙基氨基）-4-苯基酞嗪，具有改善循环障碍并由相应的2,3-二氮杂萘酮制备的活性。

18. 发明授权

US08247569B2 Cyclohexane derivative and pharmaceutical use thereof 有权
标题翻译：环己烷衍生物及其药物用途
公开(公告)号：US08247569B2
公开(公告)日：2012-08-21
申请号：US13126901
申请日：2009-10-30
申请人： Yasuhiro Morita , Katsuhiko Iseki , Yuji Sugawara , Hideyuki Tsutsui , Shunsuke Iwano , Naoki Izumimoto , Tadamasa Arai , Hidetoshi Noda , Chihiro Yoshida
发明人： Yasuhiro Morita , Katsuhiko Iseki , Yuji Sugawara , Hideyuki Tsutsui , Shunsuke Iwano , Naoki Izumimoto , Tadamasa Arai , Hidetoshi Noda , Chihiro Yoshida
IPC分类号： C07D401/02 , C07D277/20 , C07D263/30 , C07D231/10
CPC分类号： A61K31/415 , A61K31/421 , A61K31/426 , A61K31/4439 , C07D231/12 , C07D263/32 , C07D277/24 , C07D401/04
摘要： A compound has a strong analgesic action against both nociceptive pain and neuropathic pain and has less side effects, and is medically useful. The compound includes cyclohexane derivatives represented by the following compound, or pharmaceutically acceptable salts thereof or prodrugs thereof.
摘要翻译：化合物对伤害性疼痛和神经性疼痛均具有强烈的镇痛作用，副作用较小，在医学上有用。该化合物包括由以下化合物表示的环己烷衍生物，或其药学上可接受的盐或其前药。

19. 发明申请

US20110178103A1 THERAPEUTIC AGENT FOR CHRONIC RENAL FAILURE 有权
标题翻译：慢性肾衰竭治疗药物
公开(公告)号：US20110178103A1
公开(公告)日：2011-07-21
申请号：US13055242
申请日：2009-07-23
申请人： Fuko Matsuda , Katsuhiko Iseki , Hajimu Kurumatani , Mitsuko Miyamoto
发明人： Fuko Matsuda , Katsuhiko Iseki , Hajimu Kurumatani , Mitsuko Miyamoto
IPC分类号： A61K31/4965 , C07D241/20 , A61P13/12
CPC分类号： C07D241/20 , A61K31/4965
摘要： The present invention aims to provide a therapeutic agent for chronic renal failure, comprising as an effective ingredient a compound represented by General Formula (1) or a pharmaceutically acceptable salt thereof. That is, the present invention provides provision of a drug comprising as an effective ingredient a compound represented by General Formula (1) or a pharmaceutically acceptable salt thereof, which drug is useful not only for amelioration of renal function, but also for amelioration of anemia, activation of SOD and excretion of uremic substances.
摘要翻译：本发明旨在提供一种用于慢性肾功能衰竭的治疗剂，其包含作为有效成分的由通式（1）表示的化合物或其药学上可接受的盐。也就是说，本发明提供包含作为有效成分的由通式（1）表示的化合物或其药学上可接受的盐的药物的提供，该药物不仅可用于改善肾功能，还可用于改善贫血，激活SOD和排泄尿毒症物质。

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