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    • 2. 发明授权
    • 2-O-α-D-글루코실-L-아스코르빈산 무수결정 함유 분말과 그의 제조방법 및 용도
    • 2-O-β-D-葡糖基-L-抗坏血酸无水晶体粉末及其制备方法和用途
    • KR101781360B1
    • 2017-09-25
    • KR1020150033034
    • 2015-03-10
    • 가부시기가이샤하야시바라
    • 시부야타카시이자와세이스케니시모토토모유키후쿠다시게하루미야케토시오
    • C07H7/06C07H1/06A61K8/67A61K31/375
    • C12P19/60A23L33/10A23L33/15A61K8/0241A61K8/676A61K8/732A61K31/7048A61K2800/57A61K2800/654A61Q19/02C07H17/04Y10T428/2982
    • 종래로부터범용되고있는의약부외품급의아스코르빈산 2-글루코시드무수결정함유분말에비해유의하게고결하기어려운아스코르빈산 2-글루코시드무수결정함유분말과그의제조방법및 용도를제공하는것을과제로한다. 무수물환산으로아스코르빈산 2-글루코시드를98.0중량% 초과하고 99.9중량% 미만함유하며, 분말 X선회절프로필에기초하여산출되는아스코르빈산 2-글루코시드무수결정에대한결정화도가 90% 이상이거나질소기류하에서분말중의유리수분을제거한후, 온도 25℃, 상대습도 35중량%에서 12시간동안유지한때의동적수분흡착량이 0.01중량% 이하인아스코르빈산 2-글루코시드무수결정함유분말, 및그의제조방법및 용도를제공하는것에의해해결한다. 무수물환산으로 2-0-α-D-글루코실-L-아스코르빈산을 98.0중량% 초과하고 99.9중량% 미만함유하며, 질소기류하에서분말중의수분을제거한후, 온도 25℃, 상대습도 35중량%에서 12시간동안유지한때의동적수분흡착량이 0.01% 이하이며, D-글루코스및/또는 L-아스코르빈산을함유하고, 또한, 분말전체의환원력이 1% 미만인것을특징으로하는 2-0-α-D-글루코실-L-아스코르빈산무수결정함유분말을제공한다.
    • 是提供一种抗粘结甲挑战显著与含有准药品级的无水结晶粉末的抗坏血酸2-葡萄糖苷,其是由含有无水结晶粉末的现有技术的硬抗坏血酸2-葡萄糖苷的通用及其制造的方法,和使用 的。 酐中抗坏血酸2-葡萄糖苷的术语和按重量计大于98.0%和按重量计含有小于99.9%,为无水结晶抗坏血酸2-葡萄糖苷的粉末X-射线结晶度是基于衍射曲线计算的,或至少90%的 除去在粉末中的游离水含量的混合物在氮气氛中进行后,温度25℃,按重量计无水结晶抗坏血酸含有2-葡萄糖苷粉末的在35%或更低的相对湿度维持一次的0.01%的量(重量)的动态水分吸附12小时的,以及它们的制备 本发明的方法和用途。 酸酐当量超过2-0-α-D-葡糖基-L-抗坏血酸98.0%(重量),并含有小于99.9%(重量),除去在粉末中的水含量后在氮气氛中进行的,温度25℃,相对按重量计的35份湿度 保持在%12小时一次动态水分吸附量为0.01%或更低的,含有D-葡萄糖和/或L-抗坏血酸,并且,2-O-,其特征在于该粉末的总还原能力不足1% α-D-葡糖基-L-抗坏血酸无水结晶粉末。
    • 6. 发明公开
    • Process for preparing of 2'-deoxy-2'2'-difluorocytidine
    • 制备2'-脱氧-2'-脱氧胆碱的方法
    • KR20100039837A
    • 2010-04-16
    • KR20100026091
    • 2010-03-24
    • DONGWOO SYNTECH CO LTD
    • PARK SU JINOH CHUN RIMKIM YOUNG DEUCK
    • C07D405/04C07D317/22C07H7/06
    • PURPOSE: A method for preparing 2'-deoxy-2',2'-difluorocytidine is provided to obtain useful compound in manufacturing gemcitabine with high yield and high purity. CONSTITUTION: A method for preparing 2'-deoxy-2'2'-difluorocytidine of chemical formula 1 and salt thereof comprises: a step of reacting ethyl 3-hydroxy propanic acid ester compound of chemical formula 9 with optically pure amine-based compound to obtain 3R-hydroxy propane amide compound of chemical formula 8; a step of protecting hydroxyl group of the compound of chemical formula 8 to obtain a compound of chemical formula 7; a step of hydrolyzing the compound of chemical formula 7 to D-etythro-1-oxoriboxe compound of chemical formula 6; a step of protecting hydroxyl group of the D-erythro-1-oxoribose 5th site to obtain a d-erythro-1-oxoribose compound of chemical formula 5; a step of reducing the D-erythro-1-oxoribose compound of chemical formula 5 to obtain a lactol compound of chemical formula 4; a step of reacting the lactol compound of chemical formula 4 with methansulfonyl chloride to obtain D-erythro-1-methansulfonyloxyribopurnose derivative of chemical formula 3; a step of mixing the compound of chemical formula 3 and nucleo base in organic solvent to obtain nucleoside of chemical formula 2; and a step of deprotecting the nucleoside of chemical formula 2.
    • 目的:提供制备2'-脱氧-2',2'-二氟胞苷的方法,以制备高产率,高纯度吉西他滨的有用化合物。 构成:化学式1的2'-脱氧-2'2'-二氟胞苷及其盐的制备方法包括:使化学式9的3-羟基丙酸酯化合物与光学纯胺类化合物反应的步骤 得到化学式8的3R-羟基丙烷酰胺化合物; 保护化学式8的化合物的羟基以获得化学式7的化合物的步骤; 将化学式7的化合物水解成化学式6的D-ethth-1-oxoriboxe化合物的步骤; 保护D-赤式-1-氧代半乳糖5位羟基的步骤,得到化学式5的d-赤式-1-氧代核糖化合物; 降低化学式5的D-赤式-1-氧代核糖化合物以获得化学式4的内酯化合物的步骤; 使化学式4的内酰胺化合物与甲磺酰氯反应以获得化学式3的D-赤式-1-甲磺酰氧基糠醛衍生物的步骤; 将化学式3的化合物和核碱在有机溶剂中混合以获得化学式2的核苷的步骤; 和使化学式2的核苷脱保护的步骤。
    • 7. 发明公开
    • 티오글루코오스 스피로케탈 유도체, 및 그 당뇨병 치료약으로서의 사용
    • 作为糖尿病的治疗药物,可以使用硫羟考酮衍生物及其用途
    • KR1020090065551A
    • 2009-06-22
    • KR1020097009822
    • 2007-10-12
    • 추가이 세이야쿠 가부시키가이샤
    • 사토츠토무
    • C07H7/06A61K31/7048A61P13/12A61P3/04
    • C07H7/06
    • Disclosed are a compound represented by the formula (II), a prodrug thereof, a pharmaceutically acceptable salt of the compound or the prodrug, a pharmaceutical agent and a pharmacologically composition each comprising the compound, and others. (II) wherein R1, R2, R3 and R4 is independently selected from a hydrogen atom, a C1-C6 alkyl group which may be substituted, a C7-C14 aralkyl group which may be substituted and-C(=O)Rx; Rx represents a C1-C6 alkyl group which may be substituted, an aryl group which may be substituted, a heteroaryl group which may be substituted, a C1-C6 alkoxy group which may be substituted, or-NReRf; Ar1 represents an aromatic carbon ring which may be substituted and which may be fused, or an aromatic heterocyclic ring; Q represents-(CH2)m-(L)p-or-(L)p-(CH2)m-; m represents an integer selected from 0 to 2; n represents an integer selected from 1 and 2; p represents an integer selected from 0 and 1; L represents-O-,-S-or-NR5-; and A represents an aryl group which may be substituted or a heteroaryl group which may be substituted.
    • 公开了由式(II)表示的化合物,其前药,化合物或前药的药学上可接受的盐,各自包含该化合物的药物和药理学组合物等。 (II)其中R1,R2,R3和R4独立地选自氢原子,可被取代的C1-C6烷基,可被取代的C7-C14芳烷基和-C(= O)Rx; Rx表示可以被取代的C1-C6烷基,可被取代的芳基,可被取代的杂芳基,可被取代的C1-C6烷氧基或-NReRf; Ar 1表示可以被取代且可以被稠合的芳香族碳环,或芳香族杂环; Q表示 - (CH 2)m - (L)p - 或 - (L)p-(CH 2)m - ; m表示选自0〜2的整数; n表示选自1和2的整数; p表示选自0和1的整数; L代表-O - , - S-或-NR5-; A表示可被取代的芳基或可被取代的杂芳基。