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35 条记录 (耗时 0.031 秒)

    Novel 1-substituted-3-acylpyrrole derivatives, platelet aggregation inhibitors containing them, as active ingredients, and processes for production of said derivatives
    1.
    发明授权
    Novel 1-substituted-3-acylpyrrole derivatives, platelet aggregation inhibitors containing them, as active ingredients, and processes for production of said derivatives 失效
    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。

    Process for producing 16-substituted prostaglandin es.
    3.
    发明授权
    Process for producing 16-substituted prostaglandin es. 失效
    生产16-取代的前列腺素的方法。

    公开(公告)号：US4841091A

    公开(公告)日：1989-06-20

    申请号：US913889

    申请日：1986-09-29

    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 arbitray mixing ratio, ##STR1## wherein R.sup.1 indicates COOR.sup.2, CH.sub.2 OR.sup.3, in which R.sup.2 indicates a hydrogen atom, a dubstituted 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.

    摘要翻译： PCT No.PCT / JP86 / 00034 Sec。 371日期1986年9月29日第 102（e）1986年9月29日PCT PCT公布1986年1月28日PCT公布。 出版物WO86 / 04330 日期：1986年7月31日。一种用于制备16取代的DELTA 7-前列腺素Es的新方法，其包括由下式（I）表示的化合物，其对映异构体或其混合比的混合物， 其中R1表示COOR2，CH2OR3，其中R2表示氢原子，取代或未取代的C1-C10烷基，取代或未取代的C3-C10环烷基或取代或未取代的苯基，R3表示氢原子， 三（C 1 -C 7）烃甲硅烷基，与羟基的氧原子一起形成缩醛键的基团或C 2 -C 7酰基; R4和R5相同或不同，各自表示氢原子，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; R6表示氢原子，C1-C4烷基或乙烯基; R7表示可含有氧原子的直链或支链C 3 -C 8烷基，链烯基或炔基; 可被取代的苯基，苯氧基或C3-C10环烷基; 或被可被取代的C1-C6烷氧基，苯基苯氧基或C3-C10环烷基取代的直链或支链C1-C5烷基; Y表示CH2X或XCH2，其中X表示亚乙基，顺式或反式亚乙烯基或亚乙炔基。

    Thiazolo[3,2-a]pyrimidines, derivatives thereof, processes for production thereof, and pharmaceutical use thereof
    4.
    发明授权
    Thiazolo[3,2-a]pyrimidines, derivatives thereof, processes for production thereof, and pharmaceutical use thereof 失效

    公开(公告)号：US4421914A

    公开(公告)日：1983-12-20

    申请号：US311329

    申请日：1981-10-14

    申请人： Noriaki Okamura ,  Takeshi Toru ,  Takeo Oba ,  Toshio Tanaka ,  Kiyoshi Bannai ,  Kenzo Watanabe ,  Seizi Kurozumi ,  Tatsuyuki Naruchi ,  Keiji Komoriya

    发明人： Noriaki Okamura ,  Takeshi Toru ,  Takeo Oba ,  Toshio Tanaka ,  Kiyoshi Bannai ,  Kenzo Watanabe ,  Seizi Kurozumi ,  Tatsuyuki Naruchi ,  Keiji Komoriya

    IPC分类号： C07D513/04 ,  C07D513/14 ,  A61K31/505

    CPC分类号： C07D513/04

    摘要： A compound selected from thiazolo[3,2-a]pyrimidines or their enolate derivatives represented by the following general formula ##STR1## wherein R.sup.1 and R.sup.2 are identical or different, and each represents a hydrogen atom, an alkyl group having 1 to 10 carbon atoms, an alkenyl group having 3 to 10 carbon atoms, a substituted or unsubstituted phenyl group, a substituted or unsubstituted cycloaliphatic group having 3 to 8 carbon atoms, a substituted or unsubstituted phenylalkyl group or a substituted or unsubstituted acyl group having 2 to 7 carbon atoms, provided that R.sup.1 and R.sup.2 are not simultaneously hydrogen atoms or substituted or unsubstituted acyl groups having 2 to 7 carbon atoms; and R.sup.1 and R.sup.2, when taken together, may form, with the nitrogen atom to which they are bonded, a 5- or 6-membered ring which may further contain one or more hetero atoms;and acid addition salts of these compounds.The thiazolo[3,2-a]pyrimidines may be prepared by a process comprising (a) reacting a malonic acid derivative of the following general formula ##STR2## wherein R.sup.1 and R.sup.2 are as defined with regard to formula (I), and R.sup.4 and R.sup.5 are identical or different and each represents an alkyl group having 1 to 6 carbon atoms,with 2-aminothiazoline under heat, if desired in the presence of an inert organic solvent, to induce cyclocondensation, or (b) performing said condensation reaction in the presence of an alkali metal alkoxide, if desired in the presence of an inert organic solvent, and neutralizing the resulting enolate with an acid; and if desired, reacting the reaction product of (a) or (b) with an acid.The present invention provides also several processes for preparing enolate derivatives thereof.The thiazolo[3,2-a]pyrimidines, their enolate derivatives and acid addition compounds thereof are useful for regulating the immune function of a warm-blooded animal.

    7-thiaprostaglandins E, and process for producing same
    7.
    发明授权
    7-thiaprostaglandins E, and process for producing same 失效
    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。

    Process for the preparation of 4-hydroxycyclopent-2-en-1-one derivatives
    9.
    发明授权
    Process for the preparation of 4-hydroxycyclopent-2-en-1-one derivatives 失效
    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。