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    Thiaprostaglandin E.sub.1 derivatives, process for production thereof, and pharmaceutical use thereof
    3.
    发明授权
    Thiaprostaglandin E.sub.1 derivatives, process for production thereof, and pharmaceutical use thereof 失效
    Thiaprostaglandin E1衍生物，其制备方法及其药物用途

    公开(公告)号：US4466980A

    公开(公告)日：1984-08-21

    申请号：US316902

    申请日：1981-10-30

    申请人： Toshio Tanaka ,  Takeshi Toru ,  Takeo Oba ,  Noriaki Okamura ,  Kenzo Watanabe ,  Kiyoshi Bannai ,  Atsuo Hazato ,  Seizi Kurozumi ,  Fukuyoshi Kamimoto ,  Akira Ohtsu

    发明人： Toshio Tanaka ,  Takeshi Toru ,  Takeo Oba ,  Noriaki Okamura ,  Kenzo Watanabe ,  Kiyoshi Bannai ,  Atsuo Hazato ,  Seizi Kurozumi ,  Fukuyoshi Kamimoto ,  Akira Ohtsu

    IPC分类号： C07C405/00 ,  C07D309/12 ,  C07C177/00 ,  A61K31/557

    CPC分类号： C07C405/0033 ,  C07D309/12

    摘要： A novel compound selected from the group consisting of 7-(or 6- or 4-)thiaprostaglandin E.sub.1 derivatives of the formula (I). ##STR1## wherein A represents --CH.sub.2 -- or ##STR2## in which n is 0, 1 or 2, provided that only one A cut of three is ##STR3## R.sup.1 -R.sup.7 and G are as defined in the specification, the 15-epimers of said thiaprostaglandin E.sub.1 derivatives, the enatiomers of said thiaprostaglandin E.sub.1 derivatives or their 15-epimers, and mixtures of these compounds.A 7-thiaprostaglandin E.sub.1 derivative and/or its optical isomer may be prepared by reacting a 2-organo-2-cyclopentenone (II) with an organic copper-lithium compound (III) to effect conjugation reaction. A 6-thiaprostaglandin E.sub.1 derivative and/or its optical isomer may be prepared by subjecting an .alpha.,.beta.-unsaturated ketone (IV) and a thiol (V) to the Michael addition reaction. And, 4-thiaprostaglandin derivative and/or its optical isomer may also be prepared by the Michael addition reaction from a 2-allyl substituted cyclopentanone (VI) and a thiol (VIII).Some compounds ((I)-1) amongst the compounds of the formula (I) and/or their optical isomer are useful for controlling vascular actions such as angina pectoris, vasodilation etc.

    摘要翻译： 选自式（I）的7-（或6-或4-）赖氨酸前列腺素E1衍生物的新化合物。 （I）其中A表示-CH 2 - 或，其中n为0,1或2，条件是三个只有一个A切割是R 1 -R 7，G如说明书中所定义， 所述thiaprostaglandin E1衍生物的15-差向异构体，所述thiaprostaglandin E1衍生物或它们的15-差向异构体的对映体，以及这些化合物的混合物。 7-硫代前列腺素E1衍生物和/或其旋光异构体可以通过2-有机-2-环戊烯酮（II）与有机铜 - 锂化合物（III）反应来制备共轭反应。 6-硫代前列腺素E1衍生物和/或其旋光异构体可以通过使α，β-不饱和酮（IV）和硫醇（V）进行迈克尔加成反应来制备。 并且，也可以通过从2-烯丙基取代的环戊酮（VI）和硫醇（VIII）的迈克尔加成反应制备4-硫代前列腺素衍生物和/或其旋光异构体。 式（I）化合物和/或其旋光异构体中的一些化合物（（I）-1）可用于控制血管作用，例如心绞痛，血管舒张等。

    Derivative of thiazolo[3,2-a]pyrimidine and a process for the preparation thereof and a drug containing it
    4.
    发明授权
    Derivative of thiazolo[3,2-a]pyrimidine and a process for the preparation thereof and a drug containing it 失效
    噻唑并[3,2-a]嘧啶的衍生物及其制备方法和含有它的药物

    公开(公告)号：US4383996A

    公开(公告)日：1983-05-17

    申请号：US339460

    申请日：1981-12-28

    申请人： Takeo Oba ,  Kiyoshi Bannai ,  Toshio Tanaka ,  Kenzo Watanabe ,  Tatsuyuki Naruchi ,  Keiji Komoriya ,  Seizi Kurozumi ,  Kenji Hoshina

    发明人： Takeo Oba ,  Kiyoshi Bannai ,  Toshio Tanaka ,  Kenzo Watanabe ,  Tatsuyuki Naruchi ,  Keiji Komoriya ,  Seizi Kurozumi ,  Kenji Hoshina

    IPC分类号： C07D513/04 ,  A61K31/505

    CPC分类号： C07D513/04 ,  Y10S514/825 ,  Y10S514/885

    摘要： A derivative of thiazolo [3,2-a] pyrimidine expressed by formula (I) ##STR1## (where R indicates a phenyl group or a benzyl group which has a halogen atom, a lower alkyl or lower alkyloxy group as a substituent group, an alicyclic group or an arylethyl group), and a process for the preparation of a compound of formula (I) comprising cyclizing a compound expressed by formula (II) by application of heat ##STR2## (where a definition of R is as same as that given in case of formula (I) and R' indicates a halogen atom or lower alkyloxy group). A drug which contains this compound as active ingredient is useful for curing autoimmune diseases such as rheumatoid arthritis, nephritis, etc.

    摘要翻译： PCT No.PCT / JP80 / 00090 Sec。 371日期：1981年12月28日 102（e）日期1981年12月28日PCT提交1980年4月28日PCT公布。 公开号WO81 / 03174 1981年11月12日，由式（I）表示的噻唑并[3,2-a]嘧啶衍生物（I）（其中R表示苯基或具有卤素原子的苄基，较低 烷基或低级烷氧基作为取代基，脂环基或芳乙基），以及制备式（I）化合物的方法，其包括使式（II）表示的化合物通过加热 （II）（其中R的定义与式（I）的情况相同，R'表示卤素原子或低级烷氧基）。 含有该化合物作为活性成分的药物可用于治疗自身免疫性疾病如类风湿性关节炎，肾炎等。

    Thiazolo[3,2-a]pyrimidines, derivatives thereof, processes for production thereof, and pharmaceutical use thereof
    6.
    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。

    Novel isocarbacyclins and processes for production thereof
    9.
    发明授权
    Novel isocarbacyclins and processes for production thereof 失效
    新型异卡波菌素及其制备方法

    公开(公告)号：US4788319A

    公开(公告)日：1988-11-29

    申请号：US44957

    申请日：1987-05-01

    申请人： Atsuo Hazato ,  Toshio Tanaka ,  Noriaki Okamura ,  Kiyoshi Bannai ,  Kurozumi, Seizi ,  Suzuki, Masaaki ,  Noyori, Ryoji

    发明人： Atsuo Hazato ,  Toshio Tanaka ,  Noriaki Okamura ,  Kiyoshi Bannai ,  Kurozumi, Seizi ,  Suzuki, Masaaki ,  Noyori, Ryoji

    IPC分类号： C07C405/00 ,  C07C147/107

    CPC分类号： C07C405/0025 ,  C07C405/0083

    摘要： A novel isocarbacyclin which is a compound represented by the following formula ##STR1## wherein R.sup.1 represents a hydrogen atom, or a C.sub.1 -C.sub.4 alkyl or alkenyl group; R.sup.2 and R.sup.3 are identical or different and each represents a hydrogen atom, a tri(C.sub.1 -C.sub.7)hydrocarbon-silyl group or a group forming an acetal linkage together with the oxygen atom of the hydroxyl group; R.sup.4 represents a hydrogen atom, a methyl group or a vinyl group; R.sup.5 represents an unsubstituted linear or branched C.sub.3 -C.sub.8 alkyl group which may be interrupted by an oxygen atom, a substituted linear or branched C.sub.1 -C.sub.5 group in which the substituent is a C.sub.1 -C.sub.6 alkoxy group or a phenyl, phenoxy or C.sub.3 -C.sub.10 cycloalkyl group which may be substituted further, 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; n is 0 or 1; and Ar represents a substituted or unsubstituted phenyl group, its enantiomorph, or a mixture both in an arbitrary ratio.

    摘要翻译： 一种新颖的异卡巴环素，它是由下式表示的化合物：其中R 1表示氢原子或C 1 -C 4烷基或烯基; R2和R3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; R4表示氢原子，甲基或乙烯基; R5表示可被氧原子取代的未取代的直链或支链C 3 -C 8烷基，其中取代基为C 1 -C 6烷氧基的取代的直链或支链C 1 -C 5基或苯基，苯氧基或C 3 -C 10 可以被取代的环烷基，可被取代的苯基，可被取代的苯氧基或可被取代的C3-C10环烷基; n为0或1; Ar表示取代或未取代的苯基，其对映体或任意比例的混合物。

    Novel 1.alpha.-hydroxy-24-oxovitamin D.sub.3, its preparing process and the novel precursors thereof
    10.
    发明授权
    Novel 1.alpha.-hydroxy-24-oxovitamin D.sub.3, its preparing process and the novel precursors thereof 失效
    新型1α-羟基-24-氧维生素D3，其制备方法及其新型前体

    公开(公告)号：US4199577A

    公开(公告)日：1980-04-22

    申请号：US939043

    申请日：1978-09-01

    申请人： Toru Takeshita ,  Takao Niki ,  Hiroyuki Kawashima ,  Kiyoshi Bannai

    发明人： Toru Takeshita ,  Takao Niki ,  Hiroyuki Kawashima ,  Kiyoshi Bannai

    IPC分类号： A61K31/59 ,  A61P3/02 ,  C07C67/00 ,  C07C401/00 ,  C07J9/00 ,  C07J17/00 ,  C07J51/00

    CPC分类号： C07J17/00 ,  C07J51/00 ,  C07J9/00 ,  Y02P20/55

    摘要： Novel 1.alpha.,3.beta.-dihydroxy-24-oxocholesta-5,7-diene and the hydroxyl group-protected derivatives thereof.Said novel 1.alpha.-hydroxy-24-oxovitamin D.sub.3 and said novel intermediates are also useful as the intermediates of 1.alpha.,24-dihydroxyvitamin D.sub.3.1.alpha.,3.beta.-Dihydroxy-24-oxocholesta-5,7-diene and the hydroxyl group-protected derivatives thereof are prepared from fucosterol via 1.alpha.,3.beta.-diprotected hydroxy-24(24)-ethylenedioxycholest-5-ene. 1.alpha.-hydroxy-24-oxovitamin D.sub.3 is prepared by irradiation with ultraviolet rays to 1.alpha.,3.beta.-dihydroxy-24-oxocholesta-5,7-diene or a hydroxyl group-protected derivatives thereof, isomerization using heat energy, and, when necessary, elimination of the protecting groups.

    摘要翻译： 新的1α，3β-二羟基-24-氧代胆甾-5,7-二烯及其羟基保护的衍生物。 所述新型1α-羟基-24-氧维生素D3和所述新型中间体也可用作1α，24-二羟基维生素D3的中间体。 1α，3β-二羟基-24-氧代胆甾烯-5,7-二烯及其羟基保护的衍生物通过1α，3β-双保护的羟基-24（24） - 亚乙基二氧胆甾-5-烯由岩藻甾醇制备。 1α-羟基-24-氧代维生素D3通过用1α，3β-二羟基-24-氧代胆甾烯-5,7-二烯或其羟基受保护的衍生物用紫外线照射制备，使用热能异构化， 必要时消除保护基团。