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1. 发明授权

US4233309A Novel 1-substituted-3-acylpyrrole derivatives, platelet aggregation inhibitors containing them, as active ingredients, and processes for production of said derivatives 失效
标题翻译：新颖的1-取代-3-酰基吡咯衍生物，含有它们的血小板聚集抑制剂作为活性成分，以及所述衍生物的制备方法
公开(公告)号：US4233309A
公开(公告)日：1980-11-11
申请号：US966050
申请日：1978-12-04
申请人： Toshio Tanaka , Akira Otsu , Seizi Kurozumi , Toshio Wakabayashi
发明人： Toshio Tanaka , Akira Otsu , Seizi Kurozumi , Toshio Wakabayashi
IPC分类号： C07D207/32 , C07D207/325 , C07D207/333 , C07D207/00 , A61K31/40
CPC分类号： C07D207/325 , C07D207/333
摘要： Novel 1-substituted-3-acylpyrrole derivatives of the formula ##STR1## wherein all symbols are as defined in the specification; and platelet aggregation inhibiting agents comprising them as active ingredients. These novel 1-substituted-3-acylpyrrole derivatives are prepared by condensing the corresponding 1-substituted pyrrole derivatives with the corresponding acylating agents in the presence of acid catalysts, and if desired, subjecting the products to oxidation, hydrolysis, amidation or acetal-forming reaction. These 1-substituted-3-acylpyrrole derivatives exhibit unique properties in that they have superior platelet aggregation inhibiting actions with low antiinflammatory activity.
摘要翻译：新颖的式（I）的1-取代-3-酰基吡咯衍生物，其中所有符号如说明书中所定义; 和包含它们作为活性成分的血小板聚集抑制剂。这些新的1-取代-3-酰基吡咯衍生物通过在酸催化剂存在下将相应的1-取代吡咯衍生物与相应的酰化剂缩合，并且如果需要，使产物经历氧化，水解，酰胺化或缩醛形成反应。这些1-取代-3-酰基吡咯衍生物具有独特的性质，因为它们具有优异的血小板聚集抑制作用，具有低的抗炎活性。

2. 发明授权

US5364883A Isocarbocyclins for the treatment of liver and kidney diseases 失效
标题翻译： Isocarbocyclins用于治疗肝肾疾病
公开(公告)号：US5364883A
公开(公告)日：1994-11-15
申请号：US55787
申请日：1993-05-03
申请人： Kiyoshi Bannai , Toshio Tanaka , Yoshinori Kato , Tamotsu Koyama , Satoshi Asano , Akira Ohtsu , Seizi Kurozumi , Makoto Ogawa , Yoshio Mori
发明人： Kiyoshi Bannai , Toshio Tanaka , Yoshinori Kato , Tamotsu Koyama , Satoshi Asano , Akira Ohtsu , Seizi Kurozumi , Makoto Ogawa , Yoshio Mori
IPC分类号： A61K31/557
CPC分类号： A61K31/557
摘要： 16(S)-Isocarbacyclins have been found to the useful in the treatment of liver and kidney diseases.
摘要翻译：已发现16（S） - 碳青霉烯可用于治疗肝肾疾病。

3. 发明授权

US4921995A Process for producing 16-substituted prostaglandines 失效
标题翻译：生产16-取代的前列腺素的方法
公开(公告)号：US4921995A
公开(公告)日：1990-05-01
申请号：US153881
申请日：1988-02-09
申请人： Toshio Tanaka , Atsuo Hazato , Seizi Kurozumi , Masahiro Koga
发明人： Toshio Tanaka , Atsuo Hazato , Seizi Kurozumi , Masahiro Koga
IPC分类号： C07C405/00
CPC分类号： C07C405/0033 , C07C405/00
摘要： A novel process for manufacturing 16-substituted .DELTA..sup.7 -prostaglandin Es, which include compounds expressed by the following formula (I), their enanantiomers, or their mixtures of arbitrary mixing ratio, ##STR1## wherein R.sup.1 indicates COOR.sup.2, CH.sub.2 OR.sup.3, or COCH.sub.2 OR.sup.3, in which R.sup.2 indicates a hydrogen atom, a substituted or unsubstituted C.sub.1 -C.sub.10 alkyl group, a substituted or unsubstituted C.sub.3 -C.sub.10 cycloalkyl group, or a substituted or unsubstituted phenyl group, and R.sup.3 indicates a hydrogen atom, a tri(C.sub.1 -C.sub.7) hydrocarbon silyl group, a group which forms an acetal bond together with the oxygen atom of a hydroxyl group, or a C.sub.2 -C.sub.7 acyl group; R.sup.4 and R.sup.5 are identical or different, each representing a hydrogen atom, a tri(C.sub.1 -C.sub.7) hydrocarbon silyl group, or a group which forms an acetal bond together with the oxygen atom of a hydroxyl group; R.sup.6 indicates a hydrogen atom, a C.sub.1 -C.sub.4 alkyl group, or a vinyl group; R.sup.7 indicates a linear or branched C.sub.3 -C.sub.8 alkyl group, an alkyenyl group, or an alkynyl group, which may contain an oxygen atom; a phenyl group, a phenoxy group, or a C.sub.3 - C.sub.10 cycloalkyl group, which may be substituted; or a linear or branched C.sub.1 -C.sub.5 alkyl group which is substituted by a C.sub.1 -C.sub.6 alkoxy group, a phenyl group, a phenoxy group, or a C.sub.3 -C.sub.10 cycloalkyl group, which may be substituted; and Y indicates CH.sub.2 X or XCH.sub.2, in which X represents an ethylene group, a cis -or trans-vinylene group, or an ethynylene group.

4. 发明授权

US4689426A 5-alkylidene-2-halo-4-substituted-2-cyclopentenone and process for production thereof 失效
标题翻译： 5-亚烷基-2-卤代-4-取代-2-环戊烯酮及其制备方法
公开(公告)号：US4689426A
公开(公告)日：1987-08-25
申请号：US628107
申请日：1984-07-05
申请人： Satoshi Sugiura , Toshio Tanaka , Seizi Kurozumi
发明人： Satoshi Sugiura , Toshio Tanaka , Seizi Kurozumi
IPC分类号： C07C405/00 , C07C177/00
CPC分类号： C07C405/00
摘要： Novel 5-alkylidene-2-halo-4-substituted-2-cyclopentenone and process for production thereof. The novel 5-alkylidene-2-halo-4-substituted-2-cyclopentenones are represented by the following formula (I): ##STR1## wherein R.sub.a represents a substituted or unsubstituted aliphatic hydrocarbon group having 1 to 12 carbon atoms or a substituted or unsubstituted phenyl group, R.sub.b represents a substituted or unsubstituted aliphatic hydrocarbon group having 1 to 12 carbon atoms, and X represents a halogen atom. The novel cyclopentenones possess excellent pharmaceutical activities including anti-tumor activity, antiviral activity and antimicrobial activity.
摘要翻译：新型5-亚烷基-2-卤代-4-取代-2-环戊烯酮及其制备方法。新型5-亚烷基-2-卤代-4-取代-2-环戊烯酮由下式（I）表示：其中R a表示取代或未取代的碳原子数为1至12的脂族烃基或取代或未取代的苯基，Rb表示取代或未取代的碳原子数1〜12的脂肪族烃基，X表示卤素原子。新型环戊烯酮具有优异的药物活性，包括抗肿瘤活性，抗病毒活性和抗菌活性。

5. 发明授权

US4039563A Process for preparing cyclopent-2-en-1-one derivatives 失效
标题翻译：制备环戊-2-烯-1-酮衍生物的方法
公开(公告)号：US4039563A
公开(公告)日：1977-08-02
申请号：US572287
申请日：1975-04-28
申请人： Toshio Tanaka , Seizi Kurozumi , Takeshi Toru , Shuji Miura , Makiko Kobayashi , Sachio Ishimoto
发明人： Toshio Tanaka , Seizi Kurozumi , Takeshi Toru , Shuji Miura , Makiko Kobayashi , Sachio Ishimoto
IPC分类号： C07C69/738 , C07C51/00 , C07C59/82 , C07C67/00 , C07C69/74 , C07C69/95 , C07C49/46 , C07B3/00
CPC分类号： C07D309/12
摘要： A process for preparing cyclopent-2-en-1-one derivatives of the formula ##STR1## wherein R.sub.1 is a substituted or unsubstituted alkyl group or a substituted or unsubstituted aryl group, andR.sub.2 is a hydrogen atom or a substituent which is not substantially brominated under the treating conditions, which comprises treating a cyclopentanone derivative of the formula ##STR2## wherein R.sub.1 and R.sub.2 are the same as defined above, with pyridinium hydrobromide perbromide.
摘要翻译：制备式（I）的环戊-2-烯-1-酮衍生物的方法，其中R1是取代或未取代的烷基或取代或未取代的芳基，R2是氢原子或取代基在处理条件下基本上不溴化，其包括用溴化吡啶鎓过溴化物处理式（II）的环戊酮衍生物，其中R1和R2与上述定义相同。

6. 发明授权

US5329035A Process for producing 2,3-disubstituted-4-substituted cyclopentanones, enantiomorphs, or mixtures thereof 失效
标题翻译： 2,3-二取代-4-取代的环戊酮，对映体或其混合物的制备方法
公开(公告)号：US5329035A
公开(公告)日：1994-07-12
申请号：US38066
申请日：1993-03-29
申请人： Ryoji Noyori , Masaaki Suzuki , Toshio Tanaka , Seizi Kurozumi
发明人： Ryoji Noyori , Masaaki Suzuki , Toshio Tanaka , Seizi Kurozumi
IPC分类号： C07C405/00 , C07F7/18
CPC分类号： C07C405/0025 , C07C405/00 , C07F7/1856
摘要： A process for producing a 2,3-disubstituted-4-substituted cyclopentanone, an enantiomorph thereof, or a mixture of these in an arbitrary ratio.The process comprises (A) subjecting a 4-substituted-2-cyclopentenone, an enantiomorph thereof, or a mixture of these in an arbitrary ratio, and an organocopper compound to conjugate addition-reaction, and thereafter (B) reacting the resulting enolate intermediate with a halide in the presence of a phenyl organotin compound.
摘要翻译：制备2,3-二取代-4-取代的环戊酮，其对映体或它们的混合物的任意比例的方法。该方法包括（A）将4-取代-2-环戊烯酮，其对映体或它们的任意比例的混合物与有机聚合物化合物进行共轭加成反应，然后（B）使得到的烯醇化物中间体在苯基有机锡化合物存在下用卤化物。

7. 发明授权

US5159102A 7-thiaprostaglandins E, and process for producing same 失效
标题翻译： 7-硫代前列腺素E及其制备方法
公开(公告)号：US5159102A
公开(公告)日：1992-10-27
申请号：US526682
申请日：1990-05-22
申请人： Toshio Tanaka , Kiyoshi Bannai , Atsuo Hazato , Seizi Kurozumi
发明人： Toshio Tanaka , Kiyoshi Bannai , Atsuo Hazato , Seizi Kurozumi
IPC分类号： C07C405/00
CPC分类号： C07C405/0033
摘要： 7-thiaprostaglandins E.sub.1 which are compounds represented by the following formula [I] or their enantiomers or mixtures thereof in any ratio: ##STR1## where R.sup.1 represents a hydrogen atom, a C.sub.1 -C.sub.10 alkyl group, a C.sub.2 -C.sub.20 alkenyl group, a substituted or unsubstituted phenyl group, a substituted or unsubstituted C.sub.3 -C.sub.10 cycloalkyl group, a substituted or unsubstituted phenyl (C.sub.1 -C.sub.2) alkyl group, or one equivalent cation; R.sup.2 and R.sup.3, which may be the same or different, represent a hydrogen atom, a tri (C.sub.1 -C.sub.7) hydrocarbon silyl group, or a group forming an acetal linkage together with an oxygen atom of a hydroxyl group; R.sup.4 represents a hydrogen atom, a methyl group or a vinyl group; R.sup.5 represents a linear or branched C.sub.3 -C.sub.8 alkyl group, a linear or branched C.sub.3 -C.sub.8 alkenyl group, a linear or branched C.sub.2 -C.sub.8 alkynyl group, a phenyl group which may be substituted, a phenoxy group which may be substituted, a C.sub.3 -C.sub.10 cycloalkyl group which may be substituted, or a linear or branched C.sub.1 -C.sub.5 alkyl group which may be substituted with a C.sub.1 -C.sub.6 alkoxy group, a phenyl group which may be substituted, a phenoxy group which may be substituted or a C.sub.3 -C.sub.10 cycloalkyl group which may be substituted; X represents an ethylene group, a vinylene group or an ethylene group; n represents 0 or 1; the expression represents an ethylene group or a vinylene group, provided that when n is o and x is an ethylene group, R.sup.5 is not a linear or branched C.sub.3 -C.sub.8 alkyl group or a C.sub.3 -C.sub.10 cycloalkyl group which may be substituted.Such compounds are especially useful for the treatment and prevention of digestive organ diseases such as a duodenal ulcer or a gastric ulcer.
摘要翻译：作为由下式[I]表示的化合物或其对映异构体或其混合物的7-硫代前列腺素E1为任意比例：其中R 1表示氢原子，C 1 -C 10烷基，C 2 -C 20链烯基取代或未取代的苯基，取代或未取代的C3-C10环烷基，取代或未取代的苯基（C1-C2）烷基或一个当量的阳离子; R2和R3可以相同或不同，表示氢原子，三（C1-C7）烃甲硅烷基或与羟基的氧原子一起形成缩醛键的基团; R4表示氢原子，甲基或乙烯基; R 5表示直链或支链C 3 -C 8烷基，直链或支链C 3 -C 8烯基，直链或支链C 2 -C 8炔基，可被取代的苯基，可被取代的苯氧基，C3 可以被取代的C 10环烷基，或可以被C 1 -C 6烷氧基取代的直链或支链C 1 -C 5烷基，可被取代的苯基，可被取代的苯氧基或C 3 -C 6烷氧基，可被取代的C 10环烷基; X表示亚乙基，亚乙烯基或亚乙基; n表示0或1; 该表达式表示亚乙基或亚乙烯基，条件是当n是o且x是亚乙基时，R 5不是直链或支链C 3 -C 8烷基或可被取代的C 3 -C 10环烷基。这些化合物特别可用于治疗和预防消化器官疾病如十二指肠溃疡或胃溃疡。

8. 发明授权

US4472428A Halogenated prostacyclins pharmaceutical use thereof and hydroxy intermediates therefore 失效
标题翻译：因此，其卤化前列环素及其羟基中间体
公开(公告)号：US4472428A
公开(公告)日：1984-09-18
申请号：US327741
申请日：1981-12-04
申请人： Takeshi Toru , Kiyoshi Bannai , Takeo Oba , Toshio Tanaka , Noriaki Okamura , Kenzo Wantanabe , Seizi Kurozumi , Akira Ohtsu , Tatsuyuki Naruchi
发明人： Takeshi Toru , Kiyoshi Bannai , Takeo Oba , Toshio Tanaka , Noriaki Okamura , Kenzo Wantanabe , Seizi Kurozumi , Akira Ohtsu , Tatsuyuki Naruchi
IPC分类号： C07D307/937 , A61K31/557 , C07D307/935
CPC分类号： C07D307/937
摘要： Novel 5- or 7-monohalogenated or 5,7-dihalogenated .sup.6 -PGI.sub.1 and 5- or 7-monohalogenated or dihalogenated PGI.sub.2 (except 5-monofluorinated PGI.sub.2). The novel halogenated prostacyclins are useful for controlling vascular actions and also in organ transplantation, extra-corporeal circulation and the like. The present invention also provides processes for preparing the novel halogenated prostacyclins.
摘要翻译： 5-或7-单卤代或5,7-二卤代6-PGI1和5-或7-单卤代或二卤代PGI2（5-单氟化PGI2除外）。新型卤代前列环素可用于控制血管作用，还可用于器官移植，体外循环等。本发明还提供了制备新型卤代前列环素的方法。

9. 发明授权

US4132726A Process for the preparation of 4-hydroxycyclopent-2-en-1-one derivatives 失效
标题翻译： 4-羟基环戊-2-烯-1-酮衍生物的制备方法
公开(公告)号：US4132726A
公开(公告)日：1979-01-02
申请号：US642800
申请日：1975-12-22
申请人： Seizi Kurozumi , Takeshi Toru , Toshio Tanaka , Shuzi Miura , Makiko Kobayashi , Sachio Ishimoto , Sadakazu Matsubara
发明人： Seizi Kurozumi , Takeshi Toru , Toshio Tanaka , Shuzi Miura , Makiko Kobayashi , Sachio Ishimoto , Sadakazu Matsubara
IPC分类号： C07C35/06 , C07C45/67 , C07D309/12 , C07F7/18 , C12P7/38 , C12P41/00
CPC分类号： C07C49/707 , C07C35/06 , C07C45/676 , C07D309/12 , C07F7/1804 , C07F7/1856 , C12P41/004 , C12P7/38 , Y02P20/55
摘要： Novel optically active compounds of 4-protected hydroxy-cyclopent-2-en-1-ones of the formula ##STR1## wherein R is a splittable protective group for an alcoholic hydroxyl group, and a process for preparing the 4-protected hydroxycyclopent-2-en-1-ones by oxidizing monohydroxy-protected derivatives of cyclopent-1-ene-3,5-diol expressed by the following formula ##STR2## wherein R is the same as defined above. Optically active 4-hydroxycyclopent-2-en-1-one which is an optically active isomer of the compound of formula (2); or optically active cyclopent-1-en-3,5-diol (R-isomer) and a novel diacyl derivative of the diol, a novel monoacylmonosilyl-derivative of the diol and a novel monoacylmonotetrahydropyranol-derivative of the diol, which are intermediates for the protective derivative of formula (1). Processes are also provided for preparing the protective derivatives of formula (1) by converting these intermediates by esterification, hydrolysis, enzymatic processes, etc. The optically active compounds of formula (2) are useful as precursors for the preparation of prostaglandin or its analogues.
摘要翻译：新型的具有式（2）的4-保护的羟基 - 环戊-2-烯-1-酮的光学活性化合物，其中R是醇羟基的可裂解的保护基，以及制备4-保护的羟基环戊-2-烯-1-酮通过氧化由下式（1）表示的环戊-1-烯-3,5-二醇的单羟基保护衍生物，其中R与上述定义相同。光学活性的4-羟基环戊-2-烯-1-酮，它是式（2）化合物的旋光异构体; 或光学活性的环戊-1-烯-3,5-二醇（R-异构体）和二醇的新型二酰基衍生物，二醇的新型单酰基单甲硅烷基衍生物和二醇的新型单酰基单四氢吡喃醇衍生物，其为式（1）的保护性衍生物。还提供了通过酯化，水解，酶法等转化这些中间体来制备式（1）的保护性衍生物的方法。式（2）的光学活性化合物可用作制备前列腺素或其类似物的前体。

10. 发明授权

US5283349A 2,6,7-trisubstituted-3-methylenebicyclo(3.3.0)-octanes, and process for production thereof 失效
标题翻译： 2,6,7-三取代-3-亚甲基双环（3.3.0） - 辛烷，及其制备方法
公开(公告)号：US5283349A
公开(公告)日：1994-02-01
申请号：US905976
申请日：1986-09-11
申请人： Toshio Tanaka , Kiyoshi Bannai , Seizi Kurozumi
发明人： Toshio Tanaka , Kiyoshi Bannai , Seizi Kurozumi
IPC分类号： C07C405/00 , C07D303/14 , C07D303/16 , C07F7/18 , C07F9/117 , C07F7/08
CPC分类号： C07D303/14 , C07C405/0083 , C07D303/16 , C07F7/1856 , C07F9/117
摘要： A 2,6,7-trisubstituted-3-methylenebicyclo-[3.3.0]octane of formula (I) or an enantiomer thereof, or a mixture of these in an arbitrary ratio. The compound is a key intermediate for preparation of isocarbacyclins which are useful as medicines for the circulatory system such as an antithrombotic agent, an antilipidemic agent, a hypotensive agent or an antiarterosclerotic agent.
摘要翻译：式（I）的2,6,7-三取代-3-亚甲基双环（3.3.0）辛烷或其对映异构体，或它们的任意比例的混合物。该化合物是制备用于循环系统的药物的异卡巴菌素的关键中间体，例如抗血栓形成剂，抗血脂剂，降血压药或抗动物硬化剂。

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