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1. 发明授权

US5089494A 4-phenylphthalazine derivatives which inhibit platelet aggregation 失效
标题翻译：抑制板聚集的4-苯基苯胺衍生物
公开(公告)号：US5089494A
公开(公告)日：1992-02-18
申请号：US675259
申请日：1991-03-27
申请人： Norimichi Iwase , Yasuhiro Morinaka , Yoshikuni Tamao , Toshiji Kanayama
发明人： Norimichi Iwase , Yasuhiro Morinaka , Yoshikuni Tamao , Toshiji Kanayama
IPC分类号： C07D237/34
CPC分类号： C07D237/34
摘要： 4-Phenylphthalazine derivatives having platelet aggregation inhibitory activity of the formula: ##STR1## wherein R.sup.1 is an alkyl or hydroxyalkyl group of 1-5 carbon atoms; R.sup.2 is a hydrogen atom or an alkyl group of 1-5 carbon atoms; or R.sup.1 and R.sup.2, when taken together, may represent an alkylene group of 2-6 carbon atoms, said group optionally containing one or more oxygen atoms; R.sup.3 and R.sup.4 are independently a hydrogen or halogen atom, an alkyl or alkoxy group of 1-4 carbon atoms, or when two of R.sup.3 are adjacently positioned, (R.sup.3)l may represent a --O--(CH.sub.2).sub.p --O-- group and/or when two of R.sup.4 are adjacently positioned, (R.sup.4).sub.m may represent a --O--(CH.sub.2).sub.p --O-- group; R.sup.5 is a hydrogen or halogen atom, an alkyl or alkoxy group of 1-4 carbon atoms, a trifluoromethyl group or a hydroxy group, or when two of R.sup.5 are adjacently positioned, (R.sup.5).sub.n may represent a --O--(CH.sub.2).sub.p --O-- group; p is an integer of 1-3; l and m are independently an integer of 1-2; and n is an integer of 1-3, and optical isomers and pharmaceutically acceptable acid addition salts thereof.

2. 发明授权

US5462941A 3,6-disubstituted pyradazine derivatives 失效
标题翻译： 3,6-二取代的哒嗪衍生物
公开(公告)号：US5462941A
公开(公告)日：1995-10-31
申请号：US215426
申请日：1994-03-21
申请人： Norimichi Iwase , Yasuhiro Morinaka , Yoshikuni Tamao , Toshiji Kanayama , Kumi Yamada
发明人： Norimichi Iwase , Yasuhiro Morinaka , Yoshikuni Tamao , Toshiji Kanayama , Kumi Yamada
IPC分类号： A61K31/50 , A61K31/502 , A61P7/02 , A61P9/00 , A61P9/10 , C07D237/34 , C07D241/44 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/04 , C07D405/14 , C07D409/04 , C07D409/12 , C07D409/14 , C07D417/04 , C07D417/14 , C07D491/04 , C07D491/048 , C07D495/04 , C07D521/00 , C07D247/02
CPC分类号： C07D231/12 , C07D233/56 , C07D237/34 , C07D249/08 , C07D403/04 , C07D405/04 , C07D409/04 , C07D409/12 , C07D409/14 , C07D417/04 , C07D491/04 , C07D495/04
摘要： A 3,6-disubstituted pyridazine derivative having excellent platelet agglutination inhibitory effects. It is useful for a preventive medicine or a therapeutic medicine for a cerebrovascular disorder such as cerebral thrombosis and cerebral embolism, an ischemic heart disease such as myocardial infarction, and a circulation disorder such as peripheral circulation disorder. A pharmaceutical composition containing a compound of the present invention as an effective ingredient and a process for preparing the same are also disclosed. The compound has the formula (I) ##STR1## wherein A represents an alkyl group having 3 to 6 carbon atoms; a cycloalkyl group having 5 to 7 carbon atoms; a phenyl group, a thienyl group, a furyl group, a thiazolyl group, a phenoxy group, a phenylalkyl group having 7 to 9 carbon atoms, a phenylthio group, a 5-6 membered saturated heterocyclic group containing one or more nitrogen atoms, a pyridyl group or an imidazolyl group each of which may have at least one substituent selected from the group consisting of an alkyl group having 1 to 4 carbon atoms, an alkoxy group having 1 to 4 carbon atoms and a halogen atom; B represents (a) --NH--D wherein D represents ##STR2## (4) --CH.sup.3 R.sup.4 ; or (5) an alkyl group having 3 to 8 carbon atoms; or ##STR3## and the ring C represents a benzene ring.
摘要翻译：具有优异的血小板凝集抑制作用的3,6-二取代哒嗪衍生物。对脑血栓形成和脑栓塞，心肌梗死等缺血性心脏病，周围循环障碍等循环障碍的脑血管障碍的预防药或治疗药有用。还公开了含有本发明化合物作为有效成分的药物组合物及其制备方法。该化合物具有式（I）其中A表示具有3至6个碳原子的烷基; 具有5至7个碳原子的环烷基; 苯基，噻吩基，呋喃基，噻唑基，苯氧基，具有7〜9个碳原子的苯基烷基，苯硫基，含有一个或多个氮原子的5-6元饱和杂环基，吡啶基或咪唑基，其各自可具有至少一个选自具有1至4个碳原子的烷基，具有1至4个碳原子的烷氧基和卤素原子的取代基; （A）-NH-D其中D表示（1）图像（2）图像（3）（4）-CH 3 R 4; 或（5）碳原子数为3〜8的烷基; 或（B），环C表示苯环。

3. 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。

4. 发明授权

US4699921A 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：US4699921A
公开(公告)日：1987-10-13
申请号：US763618
申请日：1985-08-08
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： C07C59/46 , A61K31/557 , A61P1/04 , A61P7/02 , A61P9/00 , A61P9/08 , A61P9/12 , C07C51/00 , C07C67/00 , C07C69/732 , C07C405/00
CPC分类号： C07C405/0083 , A61K31/557 , Y02P20/55
摘要： Disclosed is a pharmaceutical composition 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 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 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 in the R-configuration or the S-configuration or a mixture thereof.Pharmaceutical compositions 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组合物，其含有下述式表示的前列腺素I 2类似物或其无毒性盐或环糊精包合物作为有效成分：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 1-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，1-甲基 -3-戊炔基或2,6-二甲基-5-庚烯基; 4-和5-位的碳原子之间的双键是E或Z或它们的混合物; 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组合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。

5. 发明授权

US06174543B1 Antidiabetic external skin application composition 失效
标题翻译：抗糖尿病外用皮肤应用组合物
公开(公告)号：US06174543B1
公开(公告)日：2001-01-16
申请号：US09362733
申请日：1999-07-29
申请人： Rakan Matsui , Yuko Kiyota , Masaya Nakashima , Toshiji Kanayama
发明人： Rakan Matsui , Yuko Kiyota , Masaya Nakashima , Toshiji Kanayama
IPC分类号： A61K970
CPC分类号： A61K31/64 , A61K9/0014 , A61K47/10 , A61K47/26
摘要： An antidiabetic external skin application composition containing glibenclamide and benzyl alcohol and optionally a nonionic surfactant.
摘要翻译：含有格列本脲和苄醇以及任选的非离子表面活性剂的抗糖尿病外用皮肤应用组合物。

6. 发明授权

US5798389A Glomerulonephritis inhibitor 失效
标题翻译：肾小球肾炎抑制剂
公开(公告)号：US5798389A
公开(公告)日：1998-08-25
申请号：US719231
申请日：1996-09-25
申请人： Toshiji Kanayama , Taro Uchiyama , Isao Yanagisawa
发明人： Toshiji Kanayama , Taro Uchiyama , Isao Yanagisawa
IPC分类号： A61K31/16 , A61K31/20 , A61K31/23 , A61K31/232 , A61P13/02 , A61P15/00 , A61P29/00
CPC分类号： A61K31/232
摘要： A medicine effective in inhibiting glomerulonephritis is developed. A glomerulonephritis inhibitor contains, as an effective ingredient thereof, docosahexaenoic acid or a salt, ester, or amide thereof or other docosahexaenoic acid derivative.
摘要翻译：开发了有效抑制肾小球肾炎的药物。肾小球性肾炎抑制剂作为其有效成分含有二十二碳六烯酸或其盐，酯或酰胺或其它二十二碳六烯酸衍生物。

7. 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。

8. 发明授权

US4352928A 5,6-Alkylenepyrimidine derivative 失效
标题翻译： 5,6-亚烷基嘧啶衍生物
公开(公告)号：US4352928A
公开(公告)日：1982-10-05
申请号：US160080
申请日：1980-06-16
申请人： Hidetoshi Hiranuma , Tetsuo Sekiya , Susumu Mizogami , Motokuni Mori , Mitsuo Hanatsuka , Toshiji Kanayama
发明人： Hidetoshi Hiranuma , Tetsuo Sekiya , Susumu Mizogami , Motokuni Mori , Mitsuo Hanatsuka , Toshiji Kanayama
IPC分类号： A61K31/505 , A61K31/517 , A61P3/08 , A61P7/02 , A61P9/12 , A61P29/00 , C07D239/70 , C07D239/95 , C07D401/04 , C07D405/06 , C07D409/06 , C07D403/04 , C07D405/14 , C07D413/04
CPC分类号： C07D239/95 , C07D239/70
摘要： There are provided a novel compound, i.e., a 2-piperazino-4-substituted-5,6-alkylenepyrimidine derivative represented by the formula: ##STR1## wherein Y, Z and n are defined in the specification and claims, and a pharmaceutically acceptable acid addition salt thereof.The compounds of the present invention show, an anti-inflammatory effect, a blood sugar level lowering effect, a blood platelet aggregation suppressive effect, an anorexigenic action and a Serotonin effect.
摘要翻译：提供了一种新的化合物，即由下式表示的2-哌嗪基-4-取代-5,6-亚烷基嘧啶衍生物：其中Y，Z和n在说明书和权利要求书中定义，其药学上可接受的其酸加成盐。本发明的化合物显示出抗炎作用，血糖降低作用，血小板聚集抑制作用，厌食作用和血清素作用。

9. 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。

10. 发明授权

US4330533A Novel polysaccharide and hypocholesterol composition containing the same 失效
标题翻译：含有相同的新型多糖和低胆固醇组合物
公开(公告)号：US4330533A
公开(公告)日：1982-05-18
申请号：US143442
申请日：1980-04-24
申请人： Yoshihiro Takayama , Fujio Endo , Tsuneo Nozawa , Yoshiro Masuda , Motokuni Mori , Toshiji Kanayama
发明人： Yoshihiro Takayama , Fujio Endo , Tsuneo Nozawa , Yoshiro Masuda , Motokuni Mori , Toshiji Kanayama
IPC分类号： C08B37/00 , A61K31/715 , A61K35/74 , A61P3/06 , C07G3/00 , C12P1/04 , C12P19/04 , C12R1/38 , A61K31/71
CPC分类号： A61K31/715 , C12P19/04 , Y10S435/874
摘要： New polysaccharide named M-30-C produced by cultivation of new strain Pseudomonas polysaccharogenes M-30 and having utility as hypocholesterol agents.
摘要翻译：通过培养新菌株多形性假单胞菌M-30产生的新型多糖（命名为M-30-C）并具有用作低胆固醇剂。

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