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    Method for production of peptide, and its intermediate
    2.
    发明授权
    Method for production of peptide, and its intermediate 失效
    生产肽及其中间体的方法

    公开(公告)号：US4436918A

    公开(公告)日：1984-03-13

    申请号：US340337

    申请日：1982-01-18

    Applicant: Satoshi Horii ,  Hiroshi Fukase ,  Eiji Higashide

    Inventor： Satoshi Horii ,  Hiroshi Fukase ,  Eiji Higashide

    IPC: A61K38/00 ,  C07C67/00 ,  C07C231/00 ,  C07C231/12 ,  C07D207/40 ,  C07D207/416 ,  C07K1/113 ,  C07K5/06 ,  C07K14/195 ,  C07K14/41

    CPC classification number: C07D207/40 ,  C07D207/416 ,  A61K38/00 ,  Y02P20/55

    Abstract: The peptide compound represented by the formula: ##STR1## which is useful as a germicide or disinfectant, is produced by reducing a compound of the formula: ##STR2## wherein Y is amino group which may optionally be protected; R.sup.1 is hydrogen or protective group; and R.sup.2 is hydrogen or protective group; and subjecting the reduction product compound to deprotection reaction when required. A compound of the formula: ##STR3## wherein Z is amino group which may optionally be protected; R.sup.1 is hydrogen or protective group; and R.sup.2 is hydrogen or protective group, is a useful as intermediate for production of the first-mentioned compound.

    Abstract translation: 可用作杀菌剂或消毒剂的由下式表示的肽化合物是通过还原下式的化合物制备的：其中Y是可以任选被保护的氨基; R1是氢或保护基; R2是氢或保护基; 并在需要时使还原产物化合物脱保护反应。 下式的化合物：其中Z是可以任选被保护的氨基; R1是氢或保护基; 并且R 2为氢或保护基，可用作生产上述化合物的中间体。

    Alanyl-2-(5-hydroxy-2-oxo-pyrrolidin-3-yl)glycine
    8.
    发明授权
    Alanyl-2-(5-hydroxy-2-oxo-pyrrolidin-3-yl)glycine 失效
    丙酰基-2-（5-羟基-2-氧代 - 吡咯烷-3-基）甘氨酸

    公开(公告)号：US4465844A

    公开(公告)日：1984-08-14

    申请号：US526051

    申请日：1983-08-23

    Applicant: Satoshi Horii ,  Hiroshi Fukase ,  Eiji Higashide

    Inventor： Satoshi Horii ,  Hiroshi Fukase ,  Eiji Higashide

    IPC: A61K38/00 ,  C07C67/00 ,  C07C231/00 ,  C07C231/12 ,  C07D207/40 ,  C07D207/416 ,  C07K1/113 ,  C07K5/06 ,  C07K14/195 ,  C07K14/41 ,  C07D207/26 ,  A61K31/40

    CPC classification number: C07D207/40 ,  C07D207/416 ,  A61K38/00 ,  Y02P20/55

    Abstract: The peptide compound represented by the formula: ##STR1## which is useful as a germicide or disinfectant, is produced by reducing a compound of the formula: ##STR2## wherein Y is amino group which may optionally be protected; R.sup.1 is hydrogen or protective group; and R.sup.2 is hydrogen or protective group; and subjecting the reduction product compound to deprotection reaction when required. A compound of the formula: ##STR3## wherein Z is amino group which may optionally be protected; R.sup.1 is hydrogen or protective group; and R.sup.2 is hydrogen or protective group, is a useful as intermediate for production of the first-mentioned compound.

    Abstract translation: 可用作杀菌剂或消毒剂的由下式表示的肽化合物是通过还原下式的化合物制备的：其中Y是可以任选被保护的氨基; R1是氢或保护基; R2为氢或保护基; 并在需要时使还原产物化合物脱保护反应。 下式的化合物：其中Z是可以任选被保护的氨基; R1是氢或保护基; 并且R 2为氢或保护基，可用作生产上述化合物的中间体。

    Inosose derivatives, production and use thereof
    9.
    发明授权
    Inosose derivatives, production and use thereof 失效
    非糖衍生物，其生产和使用

    公开(公告)号：US4898986A

    公开(公告)日：1990-02-06

    申请号：US90974

    申请日：1987-08-31

    Applicant: Satoshi Horii ,  Hiroshi Fukase

    Inventor： Satoshi Horii ,  Hiroshi Fukase

    IPC: C07C45/29 ,  C07C45/65 ,  C07C45/67 ,  C07C49/255 ,  C07C49/517 ,  C07C49/753 ,  C07D309/12

    CPC classification number: C07D309/12 ,  C07C215/44 ,  C07C323/22 ,  C07C45/29 ,  C07C45/65 ,  C07C45/67 ,  C07C45/673 ,  C07C49/255 ,  C07C49/517 ,  C07C49/753 ,  C07C2101/14 ,  Y02P20/55

    Abstract: Disclosed is a novel inosose compound represented by the general formula: ##STR1## wherein X.sup.1 and X.sup.2 are both halogen; X.sup.1 is hydrogen and X.sup.2 is halogen; or X.sup.1 is --SQ.sup.1 and X.sup.2 is --SQ.sup.2 (each of Q.sup.1 and Q.sup.2 is lower alkyl or Q.sup.1 and Q.sup.2 may form lower alkylene), R.sup.1 is a protective group for hydroxyl and Y is .dbd.O, .dbd.N--Z (Z is hydroxyl which may be protected) or ##STR2## (A is hydrogen or an amine residue), particularly to the compound wherein the symbol Y is oxygen.The inosose compound is useful as intermediates for production of valiolamine and the N-substituted derivatives thereof, which have potent .alpha.-glucosidase inhibiting activities and are useful as preventives or therapeutics for symptoms of hyperglycemia and various diseases derived therefrom in human and animals, such as diabetes, obesity and hyperlipemia.

    Abstract translation: 公开了一种由通式如下的新型无味化合物：其中X1和X2都是卤素; X1是氢，X2是卤素; 或X1为-SQ1，X2为-SQ2（Q1和Q2各自为低级烷基或Q1和Q2可形成低级亚烷基），R1为羟基的保护基，Y为= O，= NZ（Z为羟基， 被保护）或（A是氢或胺残基），特别是其中符号Y是氧的化合物。 该无味化合物可用作生产具有强效α-葡糖苷酶抑制活性的有效的戊酰胺及其N-取代衍生物的中间体，并且可用作预防药物或治疗剂，用于在人和动物中从其衍生的高血糖症和各种疾病，例如 糖尿病，肥胖和高脂血症。

    N-substituted pseudo-aminosugars, their production and use
    10.
    发明授权
    N-substituted pseudo-aminosugars, their production and use 失效
    N-取代的假氨基糖，其生产和使用

    公开(公告)号：US4701559A

    公开(公告)日：1987-10-20

    申请号：US334986

    申请日：1981-12-28

    Applicant: Satoshi Horii ,  Yukihiko Kameda ,  Hiroshi Fukase

    Inventor： Satoshi Horii ,  Yukihiko Kameda ,  Hiroshi Fukase

    IPC: C07D213/38 ,  C07D307/52 ,  C07D333/20 ,  C07C91/16

    CPC classification number: C07D213/38 ,  C07D307/52 ,  C07D333/20

    Abstract: A compound of the formula: ##STR1## wherein A is a chain hydrocarbon group having 1 to 10 carbon atoms optionally substituted by hydroxyl, phenoxy, thienyl, furyl, pyridyl, cyclohexyl or an optionally substituted phenyl group, or a cyclic hydrocarbon group having 3 to 7 carbon atoms optionally substituted by hydroxyl, B is hydrogen or hydroxyl, and their production and use.These compounds exhibit excellent inhibitory activity against .alpha.-glucoside hydrolase, thus are useful for hyperglycemic symptoms and various disorders caused by hyperglycemia.

    Abstract translation: 下式的化合物：其中A是任选被羟基，苯氧基，噻吩基，呋喃基，吡啶基，环己基或任选取代的苯基取代的具有1-10个碳原子的链烃基，或具有3个 至7个碳原子，任选被羟基取代，B是氢或羟基，以及它们的生产和使用。 这些化合物对α-葡糖苷水解酶表现出优异的抑制活性，因此可用于高血糖症状和由高血糖引起的各种疾病。

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