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    • 6. 发明授权
    • Cephalosporin compounds
    • 头孢菌素化合物
    • US5663331A
    • 1997-09-02
    • US256348
    • 1995-01-23
    • Kee Won KimJae Hoon KangCheon Ho Park
    • Kee Won KimJae Hoon KangCheon Ho Park
    • A61K31/545A61K31/546A61P31/04C07D501/00C07D501/36
    • C07D501/00
    • The present invention relates to new cephalosporin compounds of the formula (I), particularly 3-position of cephem rings thereof substituted with new thione compounds and pharmaceutically acceptable salts thereof, which have broad antibacterial activities against both Gram-positive and Gram-negative bacteria, and the said compounds can be prepared by reacting the compounds of the formula (II) with the new thione compounds of the formula (III). ##STR1## wherein R.sub.1 is a C.sub.1-4 alkyl(preferably methyl or ethyl), C.sub.3-4 alkenyl(preferably allyl), C.sub.3-4 alkynyl (preferably propargyl) group or --C(R.sup.a) (R.sup.b)CO.sub.2 H(preferably --C(CH.sub.3).sub.2 CO.sub.2 H or --CH.sub.2 CO.sub.2 H), wherein R.sup.1 and R.sup.b, same or different, are a hydrogen atom or a C.sub.1-4 alkyl group;R.sub.2 is a C.sub.1-4 alkyl(preferably methyl or ethyl), C.sub.3-4 alkenyl(preferably allyl), C.sub.3-4 cycloalkyl(preferably cyclopropyl) group or carboxyalkyl(preferably --CH.sub.2 CO.sub.2 H) group;R.sub.3 is a 5- or 6-membered heterocyclic compound-containing 1 or 2 nitrogen atom(s) (preferably piperazine, alkylpiperazine-substituted with C.sub.1-4 alkyl at N-- or 2-position of piperazine, imidazole-substituted or unsubstituted with C.sub.1-4 alkyl); R.sub.4 is hydrogen or a carboxylic acid.
    • PCT No.PCT / KR93 / 00005 Sec。 371日期1995年1月24日 102(e)1995年1月24日PCT PCT 1993年1月16日PCT公布。 公开号WO93 / 15084 日期:1993年8月5日本发明涉及式(I)的新型头孢菌素化合物,特别是用新的硫酮化合物及其药学上可接受的盐取代的头孢烯环的3-位,其具有对革兰氏阳性和 革兰氏阴性细菌,所述化合物可以通过使式(II)化合物与式(III)的新型硫酮化合物反应来制备。 (II)甲基或乙基),C3-4烯基(优选烯丙基),C3-4炔基(优选炔丙基)或-C(Ra)(Rb)CO2H( 优选-C(CH 3)2 CO 2 H或-CH 2 CO 2 H),其中R 1和R b相同或不同,为氢原子或C 1-4烷基; R2是C1-4烷基(优选甲基或乙基),C3-4烯基(优选烯丙基),C3-4环烷基(优选环丙基)或羧基烷基(优选-CH2CO2H)基团; R3是含有1或2个氮原子的5或6元杂环化合物(优选哌嗪,哌嗪,被哌嗪的N-或2-位上的C 1-4烷基取代的烷基哌嗪,咪唑取代或未取代的C1 -4烷基); R4是氢或羧酸。
    • 7. 发明授权
    • Buffer composition for catalyzing the preparation of calcitriol or calcifediol and method for preparing calcitriol or calcifediol using same
    • 用于催化骨化三醇或钙二十二醇的制备的缓冲液组合物及使用其制备骨化三醇或钙非二醇的方法
    • US08530205B2
    • 2013-09-10
    • US13162246
    • 2011-06-16
    • Dae-Jung KangJong-Hyuk ImHyun-Jung JungJae-Hoon Kang
    • Dae-Jung KangJong-Hyuk ImHyun-Jung JungJae-Hoon Kang
    • C12P15/00C12N9/52
    • C12P7/22C12N1/38
    • The present invention relates to a buffer composition for promoting production of calcitriol or calcifediol, and a method for producing calcitriol or calcifediol using the same. More particularly, the present invention relates to a buffer composition for promoting production of calcitriol or calcifediol comprising a metallic compound, an organic solvent, cyclodextrin, tris(hydroxymethyl)aminomethane, sodium succinate, sodium chloride, magnesium chloride, and water, and a method for producing calcitriol or calcifediol using the same. In the method for producing calcitiriol or calcifediol, the production yield of calcitriol or calcifediol is high, and the bioconversion is carried out in an enzyme reaction system instead of in a microorganism culture system. Thus, it is not required to maintain a sterile state. Also, the separation/purification following the completion of a biocatalytic reaction can be carried out in a cleaner state than the microorganism culture method. Accordingly, there is an advantage in that a cost required for separation is low and the quality is improved. Furthermore, the buffer composition for promoting production of calcitriol or calcifediol can provide a high productivity of calcitriol or calcifediol.
    • 本发明涉及一种用于促进骨化三醇或钙二十二醇的生产的缓冲组合物,以及使用该缓冲组合物生产骨化三醇或钙二十二醇的方法。 更具体地说,本发明涉及一种用于促进骨化三醇或钙非二醇的生产的缓冲组合物,其包含金属化合物,有机溶剂,环糊精,三(羟甲基)氨基甲烷,琥珀酸钠,氯化钠,氯化镁和水) 用于使用其生产骨化三醇或calcifediol。 在生产calcitiriol或calcifediol的方法中,骨化三醇或calcifediol的产量高,生物转化在酶反应体系中而不是在微生物培养系统中进行。 因此,不需要保持无菌状态。 此外,生物催化反应完成后的分离/纯化可以比微生物培养方法更清洁的状态进行。 因此,存在分离所需的成本低,质量提高的优点。 此外,用于促进骨化三醇或calcifediol的生产的缓冲组合物可以提供高三氧化三萜或calcifediol的生产率。
    • 9. 发明申请
    • BUFFER COMPOSITION FOR CATALYZING THE PREPARATION OF CALCITRIOL OR CALCIFEDIOL AND METHOD FOR PREPARING CALCITRIOL OR CALCIFEDIOL USING SAME
    • 用于催化制备计算机或计算机的缓冲剂组合物及其制备计算机或计算机的方法
    • US20120064584A1
    • 2012-03-15
    • US13162246
    • 2011-06-16
    • Dae-Jung KangJong-Hyuk ImHyun-Jung JungJae-Hoon Kang
    • Dae-Jung KangJong-Hyuk ImHyun-Jung JungJae-Hoon Kang
    • B01J31/32C12P15/00B01J31/26B01J31/30B01J31/28
    • C12P7/22C12N1/38
    • The present invention relates to a buffer composition for promoting production of calcitriol or calcifediol, and a method for producing calcitriol or calcifediol using the same. More particularly, the present invention relates to a buffer composition for promoting production of calcitriol or calcifediol comprising a metallic compound, an organic solvent, cyclodextrin, tris(hydroxymethyl)aminomethane, sodium succinate, sodium chloride, magnesium chloride, and water, and a method for producing calcitriol or calcifediol using the same. In the method for producing calcitiriol or calcifediol, the production yield of calcitriol or calcifediol is high, and the bioconversion is carried out in an enzyme reaction system instead of in a microorganism culture system. Thus, it is not required to maintain a sterile state. Also, the separation/purification following the completion of a biocatalytic reaction can be carried out in a cleaner state than the microorganism culture method. Accordingly, there is an advantage in that a cost required for separation is low and the quality is improved. Furthermore, the buffer composition for promoting production of calcitriol or calcifediol can provide a high productivity of calcitriol or calcifediol.
    • 本发明涉及一种用于促进骨化三醇或钙二十二醇的生产的缓冲组合物,以及使用该缓冲组合物生产骨化三醇或钙二十二醇的方法。 更具体地说,本发明涉及一种用于促进骨化三醇或钙非二醇的生产的缓冲组合物,其包含金属化合物,有机溶剂,环糊精,三(羟甲基)氨基甲烷,琥珀酸钠,氯化钠,氯化镁和水) 用于使用其生产骨化三醇或calcifediol。 在生产calcitiriol或calcifediol的方法中,骨化三醇或calcifediol的产量高,生物转化在酶反应体系中而不是在微生物培养系统中进行。 因此,不需要保持无菌状态。 此外,生物催化反应完成后的分离/纯化可以比微生物培养方法更清洁的状态进行。 因此,存在分离所需的成本低,质量提高的优点。 此外,用于促进骨化三醇或calcifediol的生产的缓冲组合物可以提供高三氧化三萜或calcifediol的生产率。