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公开(公告)号：KR100385364B1
公开(公告)日：2003-05-27
申请号：KR1020020052421
申请日：2002-09-02
IPC: C07D265/22
Abstract: PURPOSE: Provided are azetidinone compound of the formula(I) as an intermediate useful for the manufacture of carbapenem antibiotics and a process for the preparation thereof. CONSTITUTION: The azetidine compound is represented by the formula(I). It is useful as an intermediate for the manufacture of beta-methylcarbapenem antibiotics and manufactured by reacting 4-acetoxy-azetidine compound of the formula(II) and alpha-halo propionic acid amide compound of the formula(III).
Abstract translation: 目的：提供式（I）的氮杂环丁酮化合物作为可用于制备碳青霉烯类抗生素的中间体及其制备方法。 构成：氮杂环丁烷化合物由式（I）表示。 它可用作制备β-甲基碳青霉烯类抗生素的中间体，并通过使式（II）的4-乙酰氧基 - 氮杂环丁烷化合物与式（III）的α-卤代丙酰胺化合物反应制备。
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公开(公告)号：KR100377448B1
公开(公告)日：2003-03-26
申请号：KR1020000046447
申请日：2000-08-10
IPC: C07D413/14
CPC classification number: C07D413/06 , C07D205/08 , C07D265/06 , C07D265/14 , C07D487/04 , C07F9/65611 , Y02P20/55
Abstract: There is disclosed an azetidinone compound of the formula (I):wherein R is hydrogen, or a hydroxy protecting group, R1 and R2 are each independently alkyl of 1-15 carbon atoms, benzyl or cyclized together with the carbon atom to which they are attached to form a 5 or 6-membered cyclic hydrocarbon or a heterocyclic radical having one or two hetero ring atoms, said hetero ring atoms being selected from the group consisting of O and S; R3 is lower alkyl or -COO(lower alkyl) R4 is phenyl, or phenyl substituted with halogen, lower alkoxy or nitro which is useful as a synthetic intermediate to the 1'beta-methylcarbapenem-type antibacterial agent.
Abstract translation: 公开了式（I）的氮杂环丁酮化合物：其中R是氢或羟基保护基，R 1和R 2各自独立地是1-15个碳原子的烷基，苄基或与它们所连接的碳原子一起环化 连接形成5或6元环烃或具有一个或两个杂环原子的杂环基，所述杂环原子选自O和S; R3是低级烷基或-COO（低级烷基），R4是苯基或被卤素，低级烷氧基或硝基取代的苯基，它可用作1'β-甲基碳代青霉烯类抗菌剂的合成中间体。
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公开(公告)号：KR100323652B1
公开(公告)日：2002-03-29
申请号：KR1019990047103
申请日：1999-10-28
IPC: C07D213/89
Abstract: 본발명은알킬트란스-4-브로모-3-하이드록시-1-피페리딘카르복실레이트를출발물질로하여알킬트란스-4-브로모-3-벤조일아미노카르보닐옥시-1-피페리딘카르복실레이트, 알킬시스-1-벤조일-2-옥소-헥사하이드로-옥사졸로[5,4-c] 피리딘-5-카르복실레이트, 알킬시스-2-옥소-헥사하이드로-옥사졸로[5,4-c] 피리딘-5-카르복실레이트, 시스-1--부톡시카르보닐-5-에톡시카르보닐-2-옥소-헥사하이드로옥사졸로[5,4-c] 피리딘, 알킬시스-4--부톡시카르보닐아미노-3-하이드록시-1-피페리딘카르복실레이트및 알킬시스-4--부톡시카르보닐아미노-3-메톡시-1-피페리딘카르복실레이트의중간물질을거쳐시사프라이드의중간체인알킬시스-4-아미노-3-메톡시-1-피페리딘카르복실레이트염산염을제조하는방법에관한것이다. 본발명은종래기술과는달리모든반응이온화한조건에서진행되고각 단계마다특별히정제과정을필요로하지않으며위험한나트륨하이드라이드나수소가스를사용하지않아종래기술의단점을모두극복함으로써산업화가용이한장점을가지고있으며또한알킬시스-4-아미노-3-메톡시-1-피페리딘카르복실레이트를취급이불편하고순도(80% 이하)가떨어지는종래기술의액상형태와는달리공업적으로다루기쉬운고순도(98% 이상)의분말형태로얻을수 있는장점이있다.
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公开(公告)号：KR1020020079654A
公开(公告)日：2002-10-19
申请号：KR1020020052421
申请日：2002-09-02
IPC: C07D265/22
Abstract: PURPOSE: Provided are azetidinone compound of the formula(I) as an intermediate useful for the manufacture of carbapenem antibiotics and a process for the preparation thereof. CONSTITUTION: The azetidine compound is represented by the formula(I). It is useful as an intermediate for the manufacture of beta-methylcarbapenem antibiotics and manufactured by reacting 4-acetoxy-azetidine compound of the formula(II) and alpha-halo propionic acid amide compound of the formula(III).
Abstract translation: 目的：提供式（I）的氮杂环丁酮化合物作为制备碳青霉烯类抗生素的中间体及其制备方法。 构成：氮杂环丁烷化合物由式（I）表示。 通过使式（II）的4-乙酰氧基 - 氮杂环丁烷化合物与式（III）的α-卤代丙酸酰胺化合物反应制备β-甲基碳青霉烯类抗生素的中间体是有用的。
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公开(公告)号：KR1020020013988A
公开(公告)日：2002-02-25
申请号：KR1020000046447
申请日：2000-08-10
IPC: C07D413/14
CPC classification number: C07D413/06 , C07D205/08 , C07D265/06 , C07D265/14 , C07D487/04 , C07F9/65611 , Y02P20/55
Abstract: PURPOSE: Provided is an intermediate, azetidinone compound which is useful in manufacturing beta-methylcarbapenem antibiotics. And its manufacturing method is provided. CONSTITUTION: The intermediate of carbapenem, azetidinone compound, is represented by the formula(1), wherein R is hydrogen or hydroxy protective group, R1 and R2 are individually C1-C15 alkyl, benzyl, represent 5-6 membered cyclic compound to which R1 and R2 are linked, or hetero cyclic group including at least one oxygen or sulfur atom; R3 is lower alkyl group or lower alkylester group; and R4 is benzene, halogen, lower alkyloxy group, or nitro group substituted benzene ring.
Abstract translation: 目的：提供可用于制备β-甲基碳青霉烯类抗生素的中间体氮杂环丁酮化合物。 并提供其制造方法。 构成：碳青霉烯类氮杂环丁酮化合物的中间体由式（1）表示，其中R是氢或羟基保护基，R1和R2分别是C1-C15烷基，苄基，代表5-6元环状化合物，其中R1 或R 2连接，或包含至少一个氧原子或硫原子的杂环基; R3是低级烷基或低级烷基酯基; R4为苯，卤素，低级烷氧基或硝基取代苯环。
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Patent Agency Ranking
公开(公告)号：KR1020010038923A
公开(公告)日：2001-05-15
申请号：KR1019990047103
申请日：1999-10-28
IPC: C07D213/89
Abstract: PURPOSE: A method for producing alkyl cis-4-amino-3- methoxy-1-piperidine carboxylate hydrochloride is provided, thereby the titled compound having high purity can be easily produced because the further purification steps are not required and the production is performed under the mild conditions. CONSTITUTION: The method for producing alkyl cis-4-amino-3- methoxy-1-piperidine carboxylate hydrochloride represented by formula (I) comprises the steps of: reacting alkyl trans-4-bromo-3- hydroxypiperidine-1-carboxylate of formula (III) with benzoyl isocyanate in organic solvents to produce alkyl trans-4-bromo-3- benzoylaminocarbonyloxy-1-piperidine carboxylate of formula (IV); adding base such as kalium tert-butoxide into the compound of formula (IV) to produce alkyl cis-1-benzoyl-2-oxo- hexahydro-oxazolo(5,4,c) pyridine-5-carboxylate of formula (V); reacting the compound of formula (V) with lithium hydroxide·H2O to produce alkyl cis-2-oxo-hexahydro-oxazolo(5,4-c) pyridine-5-carboxylate of formula (VI); reacting the compound of formula (VI) with triethylamine, di-tert-butoxy dicarbonate, and dimethylaminopyridine to produce cis-1-tert- butoxycarbonyl-5- ethoxycarbonyl-2-oxo- hexahydro- oxazolo(5,4-c) pyridine of formula (VII); reacting the compound of formula (VII) with cesium carbonate to produce alkyl cis-4-tert- butoxycarbonyl amino-3-hydroxy-1-piperidine carboxylate of formula (VIII); adding sodium hydroxide, dimethyl sulfate, and benzyltriethyl ammonium chloride into the compound of formula (VIII) to produce alkyl cis-4-tert-butoxycarbonylamino- 3-methoxy-1-piperidine carboxylate of formula (IX); and adding hydrogen chloride dissolved organic solvent into the compound of formula (IX) to produce alkyl cis-4-amino-3- methoxy-1-piperidine carboxylate hydrochloride of formula (I).
Abstract translation: 目的：制备顺式-4-氨基-3-甲氧基-1-哌啶羧酸烷基酯盐酸盐的方法，由于不需要进一步的纯化步骤，因此可以容易地制备具有高纯度的标题化合物，并且在 温和的条件。 构成：由式（I）表示的顺式-4-氨基-3-甲氧基-1-哌啶羧酸盐酸烷基酯盐酸盐的制备方法包括以下步骤：使反式-4-溴-3-羟基哌啶-1-羧酸烷基酯 （III）与有机溶剂中的苯甲酰异氰酸酯反应以制备式（IV）的反式-4-溴-3-苯甲酰氨基羰基氧基-1-哌啶羧酸烷基酯; 将碱如叔丁醇钾加入到式（IV）化合物中以制备式（V）的顺式-1-苯甲酰基-2-氧代六氢恶唑并（5,4，c）吡啶-5-羧酸烷基酯; 使式（Ⅴ）化合物与氢氧化锂·H 2 O反应生成式（Ⅵ）的烷基顺式-2-氧代 - 六氢 - 恶唑并（5,4-c）吡啶-5-羧酸酯; 使式（VI）化合物与三乙胺，二叔丁氧基二碳酸酯和二甲基氨基吡啶反应，得到顺式-1-叔丁氧基羰基-5-乙氧基羰基-2-氧代六氢 - 恶唑并（5,4-c）吡啶 式（Ⅶ）; 使式（Ⅶ）化合物与碳酸铯反应制得式（Ⅷ）的顺式-4-叔丁氧基羰基氨基-3-羟基-1-哌啶羧酸烷基酯; 向式（Ⅷ）化合物中加入氢氧化钠，硫酸二甲酯和苄基三乙基氯化铵，得到式（Ⅸ）的顺式-4-叔丁氧基羰基氨基-3-甲氧基-1-哌啶羧酸烷基酯; 并向式（IX）化合物中加入氯化氢溶解的有机溶剂，得到式（I）的烷基顺式-4-氨基-3-甲氧基-1-哌啶羧酸盐酸盐。
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公开(公告)号：KR1020020042218A
公开(公告)日：2002-06-05
申请号：KR1020000072016
申请日：2000-11-30
Applicant: 한국화학연구원
CPC classification number: A61K9/1075 , A61K9/4808 , A61K31/366
Abstract: PURPOSE: A pharmaceutical compositions for hypercholesterolemia treatment using of self microemulsifying drug delivery system is provided, thereby improving the solubility and bioavailability of a drug hardly dissolved. CONSTITUTION: The pharmaceutical composition useful for hyperlipidemia treatment using a self microemulsifying drug delivery system(SMEDDS) comprises 1 to 20 wt.% of statin, 5 to 60 wt.% of surfactant, 10 to 60 wt.% of solubilizing agent and 10 to 60 wt.% of co-surfactant, wherein the statin is lovastatin or simvastatin; the surfactant is selected from caster oils, substituted caster oils, twins, spans and bridge; the solubilizing agent is selected from fatty acid ester consisting of propyleneglycol monocaprylate, polyglycolide of oleic acid and linoleic acid, propyleneglycol monolaurate and polyglyceryl dioleate, vegetable oils consisting of coconut oil, olive oil, corn oil, caster oil, macadamia nut oil, apricot oil and unsaturated fatty acid, purified oil, and hydrophobic solubilizing agent; and the co-surfactant is selected from polyethyleneglycol, propylene glycol, dimethylisosorbid and diethyleneglycolmonoethylether.
Abstract translation: 目的：提供使用自微乳化药物递送系统的高胆固醇血症治疗药物组合物，从而提高难溶性药物的溶解度和生物利用度。 构成：使用自微乳化药物递送系统（SMEDDS）用于高脂血症治疗的药物组合物包含1至20重量％的他汀类，5至60重量％的表面活性剂，10至60重量％的增溶剂和10至 60重量％的辅助表面活性剂，其中他汀类是洛伐他汀或辛伐他汀; 表面活性剂选自脚轮油，取代脚轮油，双胞胎，跨度和桥梁; 增溶剂选自由丙二醇单辛酸酯，油酸聚亚油酸和亚油酸组成的脂肪酸酯，单月桂酸丙二醇酯和聚甘油二油酸酯，由椰子油，橄榄油，玉米油，脚轮油，澳洲坚果油，杏仁油组成的植物油 和不饱和脂肪酸，纯化油和疏水增溶剂; 共表面活性剂选自聚乙二醇，丙二醇，二甲基异山梨醇酯和二乙二醇单乙醚。
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公开(公告)号：KR100481618B1
公开(公告)日：2005-04-08
申请号：KR1020020022024
申请日：2002-04-22
Applicant: 한국화학연구원
Abstract: 본 발명은 하기 화학식 1로 표시되는 이트륨 가돌리늄계 적색 형광체의 제조방법에 관한 것으로서, 본 발명의 방법에 따라, 분무 용액 제조시 구연산과 같은 유기산 및 에틸렌글리콜과 같은 다가 알코올 용액을 적정비율로 첨가하고, 또한 탄산나트륨과 같은 융제를 첨가하여 제조된 이트륨 가돌리늄계 적색 형광체는, 속이 찬 나노 크기의 입자이므로, 발광특성이 우수하고 입도 분포가 향상되어 평판 디스플레이 및 삼파장 램프용 발광층에 유용하게 사용될 수 있다:
(Y
1-x Gd
x )
2 O
3 :Eu
y
상기 식에서, 0≤x≤1이고, 0.001≤y≤0.5 이다.-
公开(公告)号：KR1020020070544A
公开(公告)日：2002-09-10
申请号：KR1020010010385
申请日：2001-02-28
Applicant: 주식회사 아모레퍼시픽그룹 , 한국화학연구원 , 선진뷰티사이언스(주)
CPC classification number: A61K8/29 , A61K8/25 , A61K2800/621 , A61Q1/02 , A61Q17/04
Abstract: PURPOSE: A process of preparing double silica-titania composite powders by allowing silica to support titanium dioxide and then coating the surface of the silica with titanium oxide is provided. Whereby, the composite powders are excellent in irregular reflection and low in hiding power and can be used in a make-up product, ultraviolet screening products, etc.. CONSTITUTION: Silica is allowed to support a large amount of titanium dioxide by the reaction of silica, titanium alkoxide and an aqueous alcohol solution to produce a silica-titania composite carried with titanium dioxide, which is reacted with titanium chloride and the aqueous alcohol solution to produce silica-titania composite powder, which are surface-modified with silicon oil or a fatty acid soap to produce the double silica-titania composite powder.
Abstract translation: 目的：提供二氧化硅 - 二氧化钛复合粉末的制备方法，该方法是通过使二氧化硅支持二氧化钛，然后用二氧化钛涂覆二氧化硅表面。 因此，复合粉末的不规则反射性优异，遮盖力低，可用于化妆品，紫外线防护产品等。构成：通过二氧化硅的反应，可以使二氧化硅支持大量的二氧化钛 二氧化硅，钛醇盐和醇水溶液，以制备二氧化钛载体的二氧化硅 - 二氧化钛复合物，其与氯化钛和醇水溶液反应，以生产二氧化硅 - 二氧化钛复合粉末，其用硅油或 脂肪酸皂生产双重二氧化硅 - 二氧化钛复合粉末。
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公开(公告)号：KR1020020006889A
公开(公告)日：2002-01-26
申请号：KR1020000040396
申请日：2000-07-14
Applicant: 한국화학연구원
IPC: C07D205/08
Abstract: PURPOSE: Provided are 2-arylethenyl carbapenem derivative of the formula(1) and its pharmaceutically acceptable salt which have therapeutic effect in methicillin resistant staphylococcus aureus(MRSA) infection. And its manufacturing method and an antibacterial composition containing it as an active ingredient are also provided. CONSTITUTION: 2-arylethenyl carbapenem derivative is represented by the formula(1), wherein R is halogen, nitro, hydroxy or cyano substituted phenyl or fused aryl group; or halogen or C1-3 alkyl group substituted monocyclic, bicyclic or tricyclic 5 or 6 membered hetero aryl group containing at least one of O, S or N atom; and M is hydrogen or zwitterion forming pharmaceutically acceptable salts.
Abstract translation: 目的：提供式（1）的2-亚乙烯基碳青霉烯衍生物及其药用盐，其在耐甲氧西林金黄色葡萄球菌（MRSA）感染中具有治疗作用。 还提供其制造方法和含有它作为活性成分的抗菌组合物。 构成：2-亚乙烯基碳代青霉烯衍生物由式（1）表示，其中R是卤素，硝基，羟基或氰基取代的苯基或稠合芳基; 或含有O，S或N原子中的至少一个的卤素或C 1-3烷基取代的单环，双环或三环5或6元杂芳基; M是氢或两性离子形成药学上可接受的盐。
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