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    Benzimidazole derivatives, their production and use
    1.
    发明申请
    Benzimidazole derivatives, their production and use 失效
    苯并咪唑衍生物，其生产和使用

    公开(公告)号：US20020151723A1

    公开(公告)日：2002-10-17

    申请号：US10046189

    申请日：2002-01-16

    Applicant: TAKEDA CHEMICAL INDUSTRIES, LTD.

    Inventor： Takehiko Naka ,  Kohei Nishikawa ,  Takeshi Kato

    IPC: C07D43/02

    CPC classification number: C07D235/02 ,  C07D235/26 ,  C07D235/28 ,  C07D235/30 ,  C07D403/04 ,  C07D403/10 ,  C07D405/14

    Abstract: A method for producing a compound represented by the formula: 1 wherein the ring A is a benzene ring which may be substituted in addition to the Rnull group; R1 is hydrogen or an optionally substituted hydrocarbon residue; X is a direct bond or a spacer having an atomic length or two or less between the phenylene group and the phenyl group; Y is nullOnull, nullS(O)mnull or nullN(R4)null wherein m is an integer of 0, 1 or 2 and R4 is hydrogen or an optionally substituted alkyl group; Rnull is carboxyl, an ester thereof, an amide thereof or a group capable of forming an anion or a group convertible thereinto; n is an integer of 1 or 2; or a salt thereof, which comprises deprotecting a compound represented by the formula: 2 wherein R is triphenylmethyl, 2-tetrahydropyranyl, methoxymethyl or ethoxy methyl, the other symbols as defined above; or a salt thereof.

    Abstract translation: 一种制备由下式表示的化合物的方法：其中环A是除R'基之外可被取代的苯环; R1是氢或任选取代的烃残基; X是在亚苯基和苯基之间具有原子长度或者两个或更少的直接键或间隔子; Y是-O - ， - S（O）m - 或-N（R4） - ，其中m是0,1或2的整数，R4是氢或任选取代的烷基; R'是羧基，其酯，其酰胺或能够形成阴离子的基团或可转化的基团; n为1或2的整数; 其包括使由下式表示的化合物脱保护：其中R是三苯甲基，2-四氢吡喃基，甲氧基甲基或乙氧基甲基，其它符号如上定义; 或其盐

    Crystallization of alpha monosodium citrate monohydrate
    4.
    发明授权
    Crystallization of alpha monosodium citrate monohydrate 失效
    α单柠檬酸钠一水合物的结晶

    公开(公告)号：US3925465A

    公开(公告)日：1975-12-09

    申请号：US46461474

    申请日：1974-04-25

    Applicant: TAKEDA CHEMICAL INDUSTRIES LTD

    Inventor： NARA KIYOSHI ,  KATAMOTO KAZUYOSHI ,  OHTA KAZUHIKO ,  FUKUDA HIDEO

    IPC: C07C59/265 ,  C07C59/16

    CPC classification number: C07C59/265

    Abstract: Monosodium citrate monohydrate crystals are prepared by evaporating an aqueous solution containing monosodium citrate whilst maintaining said solution between 20*C and 60*C and at a concentration of monosodium citrate of not less than 155 % (W/V) of saturation solubility of gamma -crystals of monosodium citrate. Thus obtained crystals have a good filtrability and separability from a solution and are widely applicable as foods, pharmaceuticals and chemical products.

    Abstract translation: 通过蒸发含有柠檬酸单钠的水溶液制备柠檬酸一钠水合物晶体，同时保持所述溶液在20℃至60℃之间，柠檬酸单钠的浓度不低于γ - 饱和溶解度的155％（W / V） 柠檬酸钠的晶体。 这样获得的晶体具有良好的过滤性和与溶液的分离性，并且广泛用作食品，药品和化学产品。

    6-Aminouracil derivatives
    6.
    发明授权
    6-Aminouracil derivatives 失效
    6-氨基尿嘧啶衍生物

    公开(公告)号：US3923807A

    公开(公告)日：1975-12-02

    申请号：US39544873

    申请日：1973-09-10

    Applicant: TAKEDA CHEMICAL INDUSTRIES LTD

    Inventor： FURUKAWA YOSHIYASU ,  SUNO MASAHIRO ,  NOSE SAWAMI

    IPC: C07D239/54 ,  C07D239/06

    CPC classification number: C07D239/54 ,  Y10S514/822 ,  Y10S514/869

    Abstract: Novel 6-aminouracil derivatives of the formula

    WHEREIN R1 is lower alkyl which may be substituted with hydroxy or lower alkoxy, R2 is halogen, nitro or lower alkyl and n is 0, 1 or 2, show a strong inhibitory action against adenosine -3'', 5'' cyclic phosphate phosphodiesterase in vitro, and exhibit excellent pharmacological actions such as diuretic, platelet aggregation inhibitory and broncho-dilating actions.

    D R A W I N G

    Abstract translation: 新颖的式6-氨基尿嘧啶衍生物，其中，R 1为可被羟基或低级烷氧基取代的低级烷基，R 2为卤素，硝基或低级烷基，n为0,1或2，对腺苷-3' 5'环磷酸二酯酶，体外表现出优异的药理作用，如利尿，血小板聚集抑制和支气管扩张作用。

    Intermediates for producing cephalosporins
    7.
    发明授权
    Intermediates for producing cephalosporins 失效
    用于生产头孢菌素的中间体

    公开(公告)号：US3919207A

    公开(公告)日：1975-11-11

    申请号：US28834372

    申请日：1972-09-12

    Applicant: TAKEDA CHEMICAL INDUSTRIES LTD

    Inventor： TERAO SHINJI ,  MATSUO TAISUKE ,  TSUSHIMA SUSUMU ,  MIYAWAKI TOSHIO ,  MATSUMOTO NORICHIKA

    IPC: A61K31/545 ,  C07D501/02 ,  C07D501/04 ,  C07D501/18

    Abstract: The present invention relates to novel intermediates and a process for producing a compound of formula:

    Abstract translation: 本发明涉及新的中间体及其制备方法，其中R4是被一个或两个苯基，环己烯基，噻吩基，吡啶硫基，氨基或磺基取代的乙酰基，其中氨基被未被保护或用盐酸保护 酸，异冰片氧基羰基，β-甲基磺酰基乙氧基羰基，苯甲酰基或硝基苯甲酰基，A表示式WHEREIN X为氢或乙酰氧基，R5为β-甲基磺酰基，三甲基甲硅烷基，甲氧基甲基或对硝基苄基的头孢菌素部分， 式：R1-C = NA | SR2其中R1是苄基或苯氧基甲基，R2是烷基，A具有与上述相同的含义，与下式的化合物R6-W其中R6是如上定义的乙酰基，W是 氯化物，溴化物，SO 3，NO 3或对甲苯磺酰基，在pH低于8.0的溶剂中。

    Method of producing d-ribose
    8.
    发明授权
    Method of producing d-ribose 失效
    生产D-核糖的方法

    公开(公告)号：US3919046A

    公开(公告)日：1975-11-11

    申请号：US41556173

    申请日：1973-11-14

    Applicant: TAKEDA CHEMICAL INDUSTRIES LTD

    Inventor： SASAJIMA KEN-ICHI ,  YONEDA MASAHIKO

    IPC: C12P19/02 ,  C12D13/02

    CPC classification number: C12P19/02 ,  Y10S435/832 ,  Y10S435/839

    Abstract: D-ribose is produced by cultivating a strain belonging to the genus Bacillus whose transketolase activity is nil to cause said strain to elaborate and accumulate a large amount of D-ribose. The thus accumulated D-ribose can be recovered in a good yield.

    Abstract translation: 通过培养属于芽孢杆菌属的杆菌属的菌株产生D-核糖，其转酮酶活性为零，以使所述菌株精制并积累大量的D-核糖。 可以以良好的收率回收这样积累的D-核糖。

    Process for producing indan-1-carboxylic acid derivatives
    10.
    发明授权
    Process for producing indan-1-carboxylic acid derivatives 失效
    茚满-1-羧酸衍生物的制备方法

    公开(公告)号：US3886207A

    公开(公告)日：1975-05-27

    申请号：US37152773

    申请日：1973-06-19

    Applicant: TAKEDA CHEMICAL INDUSTRIES LTD

    Inventor： KISHIMOTO SHOJI ,  AONO TETSUYA ,  NOGUCHI SHUNSAKU

    IPC: C07C61/39 ,  C07C51/00 ,  C07C61/12 ,  C07C61/40 ,  C07C67/00 ,  C07C69/753 ,  C07C233/58 ,  C07C63/44

    CPC classification number: C07C61/12 ,  Y10S514/916

    Abstract: 5-Cycloalkyl-6-halogenoindan-1-carboxylic acid (cycloalkyl group herein is six- or five-membered one) is produced through halogenation of indan-1-carboxylic acid to introduce halogen at its 6-position selectively, and following alkylation to introduce cycloalkyl group at the 5-position. The latter reaction is effectively conducted by acting on 6-halogenoindan-1-carboxylic acid a cycloalkyhalide, a cycloalkanol, its sulfonates or a cycloalkene. The product may be converted into the form of its pharmaceutically acceptable salts. The products are useful as antipyretic, analgesic or anti-inflammatory agent for human or animal use.

    Abstract translation: 5-环烷基-6-卤代茚满-1-羧酸（本文环烷基是六或五元一个）是通过茚满-1-羧酸的卤化反应制备的，以在其6-位选择性地引入卤素，并在烷基化至 在5位引入环烷基。 后一反应通过作用于6-卤代茚满-1-羧酸环烷基卤化物，环烷醇，其磺酸盐或环烯烃而有效地进行。 产物可以转化为其药学上可接受的盐的形式。 该产品可用作人或动物使用的解热止痛剂或抗炎剂。

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