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11. 发明公开

KR1020030000779A 결정형 Ⅰ을 갖는 란소프라졸의 제조방법 失效
标题翻译：兰索唑晶体形态的修饰和纯化方法
公开(公告)号：KR1020030000779A
公开(公告)日：2003-01-06
申请号：KR1020010036898
申请日：2001-06-27
申请人： 주식회사 씨트리
发明人： 백용구 , 유정복 , 장동조 , 이동우 , 김민수 , 안현숙 , 박성준 , 김상훈 , 김경수 , 김완주
IPC分类号： C07D401/12
摘要： PURPOSE: Provided is a modification and purification method of Lansoprazole (crystal form II) into Lansoprazole (crystal form I) which is thermodynamically stable and is used as a drug. Lansoprazole, represented by the formula(I), is an inhibitor of proton pump(anti-ulcer agent), has strong antibacterial activity and excellent pharmacological activity, and is thus useful as a therapeutic agent for stomach ulcer. CONSTITUTION: The method comprises the steps of: mixing 1wt.% of Lansoprazole (crystal form II) and 1-100wt.% of an organic solvent; filtering the mixture; and drying the filtrate. The solvent is selected from the groups of ester containing methyl acetate and ethyl acetate; halogenated hydrocarbon such as methylene chloride and chloroform; ethers including tetrahydrofuran, ethyl ether, isopropyl ether and petroleum ether; hydrocarbons with more than 5 carbons such as pentane, hexane, heptane cyclohexane; nitriles such as acetonitrile; ketones such as acetone; and a mixture thereof.
摘要翻译：目的：提供兰索拉唑（晶型II）作为热力学稳定并用作药物的兰索拉唑（晶型I）的改性和纯化方法。由式（I）表示的兰索拉唑是质子泵（抗溃疡剂）的抑制剂，具有强的抗菌活性和优异的药理活性，因此可用作胃溃疡的治疗剂。构成：该方法包括：将1重量％的兰索拉唑（晶型II）和1-100重量％的有机溶剂混合; 过滤混合物; 并干燥滤液。溶剂选自含有乙酸甲酯和乙酸乙酯的酯基; 卤代烃如二氯甲烷和氯仿; 醚类，包括四氢呋喃，乙醚，异丙醚和石油醚; 具有5个以上碳原子的烃，如戊烷，己烷，庚烷环己烷; 腈类如乙腈; 酮类如丙酮; 及其混合物。

12. 发明授权

KR100338921B1 1,3-벤조디티올-2-일리움 테트라플루오로보레이트의제조방법 失效
标题翻译：制备1,3-苯并二硫醇-2-基四氟硼酸盐
公开(公告)号：KR100338921B1
公开(公告)日：2002-05-30
申请号：KR1020000001859
申请日：2000-01-15
申请人： 주식회사 씨트리
发明人： 이태석 , 유창현 , 김경수 , 유정복 , 박성준 , 김완주
IPC分类号： C07D339/06
摘要： 본 발명은 1,3-벤조디티올-2-일리움 테트라플루오로보레이트를 제조하는 방법을 제공하기 위한 것으로, 1,4-다이옥산에 용해시킨 안트라닐산으로부터 2-(3-메틸부톡시)-1,3-벤조디티올을 합성한 후 분리 단계 없이 연속해서 비양성자성 비극성 유기용매를 첨가함과 동시에 사불화붕소수소산-디에틸에테르 용액 또는 삼불화붕소 에테르콤플렉스를 첨가하여서 1,3-벤조디티올-2-일리움 테트라플루오로보레이트(BDTF)를 제조하는 방법인 것이다.
본 발명의 방법은 종래 방법의 문제점인 진한 색깔과 낮은 수율, 불안정성 등을 해결하여 높은 안정성과 옅은 색깔을 띠는 결정성 BDTF를 좀 더 간단하고, 간편하게, 높은 수율로 제조할 수 있는 방법인 것이다.

13. 发明公开

KR1020010073294A 항혈액응고성 살서제인 4-하이드록시쿠마린 중간체의제조방법 失效
标题翻译：制备抗血红蛋白4-羟基喹诺酮中间体的方法
公开(公告)号：KR1020010073294A
公开(公告)日：2001-08-01
申请号：KR1020000001555
申请日：2000-01-13
申请人： 주식회사 씨트리
发明人： 김중영 , 김경수 , 김완주
IPC分类号： C07C51/00
摘要： PURPOSE: A method for manufacturing an anti-blood coagulating rodenticide 4-hydroxycoumarin intermediate is provided to manufacture an anti-blood coagulating rodenticide 4-hydroxy-3- £1,2,3,4-tetrahydro-3-{4-(4-trifluoromethylbenzyloxy)phenyl}-1-naphthyl|coumarin intermediate which is represented in 3-(4-methoxy)phenyl-4-phenylbutanoic acid simply and in a high yield. CONSTITUTION: The method for manufacturing 4-hydroxycoumarin intermediate represented as in the following structural formula (II) comprises a first step of manufacturing a compound represented in the following structural formula (III) by reacting benzyl halide with alkylacrylate under palladium catalyst; a second step of manufacturing a compound represented in the following structural formula (IV) by carrying out the reaction under the palladium catalyst similarly as in the first step; a third step of manufacturing a compound represented as in the following structural formula (V) by reducing a compound of the structural formula (IV) obtained in the second step through hydrogenation reaction using palladium catalyst; and a fourth step of performing the next steps of saponification reaction and acid treatment without separation of a compound of the structural formula (V).
摘要翻译：目的：提供一种制备抗凝血杀鼠剂4-羟基香豆素中间体的方法，以制备抗凝血灭鼠剂4-羟基-3-（1,2,3,4-四氢-3- {4-（4 三氟甲基苄氧基）苯基} -1-萘基|香豆素中间体，其简单且高产率代表在3-（4-甲氧基）苯基-4-苯基丁酸中。构成：如以下结构式（II）所示的制备4-羟基香豆素中间体的方法包括通过在钯催化剂下使苄基卤与烷基丙烯酸酯反应来制备下述结构式（III）所示化合物的第一步骤; 通过与第一步骤类似地在钯催化剂下进行反应来制造下述结构式（IV）所示的化合物的第二步骤; 通过使用钯催化剂通过氢化反应将通过第二步获得的结构式（IV）的化合物还原，制备如下结构式（V）表示的化合物的第三步骤; 以及在不分离结构式（V）的化合物的情况下进行皂化反应和酸处理的下一步骤的第四步骤。

14. 发明公开

KR1020000055522A 이미페넴의 제조방법 失效
标题翻译： IMIPENEM的合成方法
公开(公告)号：KR1020000055522A
公开(公告)日：2000-09-05
申请号：KR1019990004179
申请日：1999-02-08
申请人： 주식회사 씨트리
发明人： 김경수 , 이태석 , 육진수 , 윤정인 , 윤병훈 , 김완주
IPC分类号： C07D477/20
CPC分类号： Y02P20/55
摘要： PURPOSE: Provided is a synthetic method of imipenem which can easily remove a protecting group by using allyl group as the protecting group of 2-carboxy group. CONSTITUTION: A synthetic method comprises the steps of: condensing bicyclic ketoester of formula(II) and a phosphochloridate derivative in the presence of base to prepare a phosphate derivative of formula(III); coupling 2-aminoethantiol hydrochlorate with the produced phosphate derivative of formula(III) in the container to prepare a thienamycin derivative of formula(IV); reacting the produced thienamycin derivative of formula(IV) with benzylimidate in the container to prepare an imipenem derifative of formula(V) with carboxy group as a protecting group; and demasking the imipenem derivative produced using a moupholine dervative and tetrakis triphenylphosphin paladium.
摘要翻译：目的：提供亚胺培南的合成方法，通过使用烯丙基作为2-羧基的保护基，可以容易地除去保护基。构成：合成方法包括以下步骤：在碱存在下将式（II）的双环酮酯和磷酸氯代衍生物缩合制备式（III）的磷酸酯衍生物; 将所述产生的式（III）的磷酸酯衍生物与所述式（III）的磷酸酯衍生物偶联在容器中以制备式（IV）的噻吩霉素衍生物; 使制备的式（Ⅳ）噻吩甲酰胺衍生物与苄基亚氨酸酯在容器中反应以制备具有羧基作为保护基团的式（Ⅴ）亚胺培南衍生物; 并使用莫匹罗线虫和四苯基膦化合物制备亚胺培南衍生物。

15. 发明公开

KR1020040007550A 신규한 알카로이드 유도체 및 이를 함유하는 약제학적조성물 失效
标题翻译：新型碱性衍生物和含有它们的药物组合物
公开(公告)号：KR1020040007550A
公开(公告)日：2004-01-24
申请号：KR1020037014670
申请日：2002-05-27
申请人： 주식회사 씨트리 , 주식회사 케이티앤지
发明人： 김완주 , 김경수 , 김명화 , 박종억 , 장정민 , 최재원 , 김동후 , 이재상 , 장동조 , 윤은영 , 김순옥 , 장석구
IPC分类号： C07C323/41
CPC分类号： C07C69/78 , C07C49/755 , C07C203/10 , C07C233/32 , C07C233/41 , C07C233/76 , C07C235/14 , C07C235/42 , C07C271/24 , C07C323/41 , C07C323/42 , C07C2603/34 , C07D307/93
摘要： PURPOSE: Novel alkaloid derivatives, specifically novel colchicine derivatives having anticancer, antiproliferative and anti-inflammatory effects, and immunosuppressive function and muscle relaxation, and a pharmaceutical composition containing the same are provided. CONSTITUTION: The novel colchicine derivatives have the formula (I), wherein, if R1 is N(R6)C(X1)-A, X2C(X1)-A, N(R6)-A, N(A)2 or X2-A, R2 is X3R7 or N(R7)2, R3 and R4 are independently hydrogen or a methyl group, R5 is hydrogen, a methyl group, or CH2X4R7, wherein R6 and R7 are independently hydrogen or a lower alkyl group, and X, X1, X2, X3 and X4 are independently 0 or S; if R2 is N(R6)C(X1)-A, X2C(X1)-A, N(R6)-A, N(A)2 or X2-A, R1 is N(R6)COCH3, N(R6)COCF3, or NHC(O)OR8, R3 and R4 are independently hydrogen or a methyl group, R5 is hydrogen, a methyl group, or CH2X4R7, wherein R6 and R7 are independently hydrogen or a lower alkyl group, R8 is a lower alkyl, alkenyl, or substituted or unsubstituted aryl, and X, X1, X2 and X4 are independently 0 or S; if R3 and R4 are independently C(X1)-A or -A, R1 is N(R6)COCH3, N(R6)COCF3, or NHC(O)OR8, R2 is X3R7 or N(R-)2, R5 is hydrogen, a methyl group, or CH2X4R7, wherein R6 and R7 are independently hydrogen or a lower alkyl group, R8 is a lower alkyl, alkenyl, or substituted or unsubstituted aryl, and X, X1, X3 or X4 are independently 0 or S; and if R5 is CH2X2C(X1)-A, R1 is N(R6)COCH3, N(R6)COCF3 or NHC(O)OR8, R2 is X3R7 or N(R7)2, R3 and R4 are independently hydrogen or a methyl group, wherein R6 and R7 are independently hydrogen or a lower alkyl group, R8 is a lower alkyl, alkenyl, or substituted or unsubstituted aryl group, and X, X1, X2 and X3 are independently 0 or S, wherein A is represented by the formula (a), (b), (c), (d), (e), (g), (h), (i) or (j).
摘要翻译：目的：提供具有抗癌，抗增殖和抗炎作用，免疫抑制功能和肌肉松弛的新型生物碱衍生物，特别是具有新颖的秋水仙素衍生物，以及包含其的药物组合物。构型：新型秋水仙碱衍生物具有式（I），其中，如果R1是N（R6）C（X1）-A，X2C（X1）-A，N（R6）-A，N（A）2或X2 -A，R2是X3R7或N（R7）2，R3和R4独立地是氢或甲基，R5是氢，甲基或CH2X4R7，其中R6和R7独立地是氢或低级烷基，X X1，X2，X3和X4独立地为0或S; 如果R2是N（R6）C（X1）-A，X2C（X1）-A，N（R6）-A，N（A）2或X2-A，R1是N（R6）COCH3，N（R6） COCF 3或NHC（O）OR 8，R 3和R 4独立地是氢或甲基，R 5是氢，甲基或CH 2 X 4 R 7，其中R 6和R 7独立地是氢或低级烷基，R 8是低级烷基，烯基或取代或未取代的芳基，X，X1，X2和X4独立地为0或S; 如果R3和R4独立地为C（X1）-A或-A，R1为N（R6）COCH3，N（R6）COCF3或NHC（O）OR8，R2为X3R7或N（R-）2，R5为氢，甲基或CH2X4R7，其中R6和R7独立地是氢或低级烷基，R8是低级烷基，烯基或取代或未取代的芳基，X，X1，X3或X4独立地为0或S; 并且如果R 5为CH 2 X 2 C（X 1）-A，则R 1为N（R 6）COCH 3，N（R 6）COCF 3或NHC（O）OR 8，R 2为X 3 R 7或N（R 7）2，R 3和R 4独立地为氢或甲基基团，其中R6和R7独立地是氢或低级烷基，R8是低级烷基，烯基或取代或未取代的芳基，X，X1，X2和X3独立地是0或S，其中A由式（a），（b），（c），（d），（e），（g），（h），（i）或（j）

16. 发明公开

KR1020030026654A 인간 로타바이러스의 활성을 저해하는 항체의 생산용 항원및 그의 제조방법과 이용 无效
标题翻译：用于生产人类脊髓灰质炎抗生素抑制活性的抗原及其生产及其使用
公开(公告)号：KR1020030026654A
公开(公告)日：2003-04-03
申请号：KR1020010059731
申请日：2001-09-26
申请人： 주식회사 씨트리
发明人： 이석준 , 김희주 , 윤순대 , 김순옥 , 김경수 , 김완주
IPC分类号： A61K39/15
摘要： PURPOSE: A process of mass-preparing a specific antigen used for production of an antibody which inhibits the activity of human rotavirus causing diarrhea is provided. The obtained eggs from birds immunized with the antigen have prevention and treatment effects on diarrhea. A functional food containing the egg yolk of the eggs has preventive and therapeutic effects on diarrhea in an infant and a young child. CONSTITUTION: The mass producing method of the specific antigen comprises the step of: selectively separating a gene encoding VP7 antigen by performing RT PCR using, as a template, genomic DNA of human rotavirus; extracting vector DNA by inserting the separated gene into a suitable vector, transforming a suitable strain with the vector and amplifying the vector; amplifying the gene encoding the antigen protein by performing PCR using, as a template, the extracted vector DNA; cloning the amplified gene into a suitable vector and transforming a suitable host with the vector; and culturing the host, followed by overexpressing the antigen.
摘要翻译：目的：提供一种大规模制备用于制备抑制引起腹泻的人轮状病毒活性的抗体的特异性抗原的方法。用抗原免疫的鸟获得的鸡蛋具有对腹泻的预防和治疗作用。含有鸡蛋蛋白的功能性食物对婴儿和幼儿的腹泻具有预防和治疗作用。构成：特定抗原的批量生产方法包括以下步骤：使用人轮状病毒的基因组DNA作为模板，通过进行RT PCR选择性分离编码VP7抗原的基因; 通过将分离的基因插入合适的载体中来提取载体DNA，用载体转化合适的菌株并扩增载体; 通过使用提取的载体DNA作为模板进行PCR来扩增编码抗原蛋白的基因; 将扩增的基因克隆到合适的载体中并用载体转化合适的宿主; 并培养宿主，然后过表达抗原。

17. 发明公开

KR1020010073460A 1,3-벤조디티올-2-일리움 테트라플루오로보레이트의제조방법 失效
标题翻译：生产1,3-二苯并二氢吡喃酮（BDTF）的方法
公开(公告)号：KR1020010073460A
公开(公告)日：2001-08-01
申请号：KR1020000001859
申请日：2000-01-15
申请人： 주식회사 씨트리
发明人： 이태석 , 유창현 , 김경수 , 유정복 , 박성준 , 김완주
IPC分类号： C07D339/06
摘要： PURPOSE: A method for producing 1,3-benzodithiol-2-ilium tetrafluoroborate(BDTF) is provided, thereby the crystalline BDTF having the improved stability and light color can be easily and simply produced in higher yield. CONSTITUTION: The method for producing 1,3-benzodithiol-2-ilium tetrafluoroborate(BDTF) represented by the formula (I) comprises the steps of: preparing 2-(3-methylbutoxy)-1,3-benzodithiol represented by the formula (II) from the anthranilic acid dissolved 1,4-dioxane and continuously adding a nonquantum and nonpolar organic solvent selected from the group consisting of diethylether, THF, toluene, chloroform, hexane, cyclohexane and diisopropylether, and simultaneously adding BF4 or Et2O·BF3 into the compound of the formula (II).
摘要翻译：目的：提供一种生产1,3-苯并二硫醇-2-铱四氟硼酸盐（BDTF）的方法，由此可以容易且简单地以更高的产率生产具有改善的稳定性和浅色的结晶BDTF。构成：由式（I）表示的1,3-苯并二硫醇-2-铱四氟硼酸盐（BDTF）的制备方法包括以下步骤：制备由式（I）表示的2-（3-甲基丁氧基）-1,3-苯并二硫醇 II），连续加入选自二乙醚，THF，甲苯，氯仿，己烷，环己烷和二异丙醚的非极性和非极性有机溶剂，并同时加入BF 4或Et 2 O·BF 3 式（II）的化合物。

18. 发明授权

KR100293121B1 항진균제용 터비나핀 및 그 염산염의 제조방법 有权
标题翻译：特比萘芬及其盐酸盐作为抗真菌剂的制备方法
公开(公告)号：KR100293121B1
公开(公告)日：2001-06-15
申请号：KR1019990012298
申请日：1999-04-08
申请人： 주식회사 씨트리 , 한솔케미언스 주식회사 , 고려제약주식회사
发明人： 이태석 , 안현숙 , 유창현 , 김경수 , 육진수 , 오성수 , 주소경 , 김완주
IPC分类号： C07C209/68
摘要： 본발명은항진균제로서광범위한약효를갖는다음의구조식 (I)과 (Ia)로표시되는터비나핀및 그염산염의신규한제조방법을제공하기위한것이다. 본발명의방법은각 반응단계에서가장반응성이좋은촉매를선택함으로써하나의반응기에서약 2 내지 4시간의짧은시간내에반응을효율적으로수행하여터비나핀염산염을고순도, 고수율(약 70.5%)로합성하는것이다.

19. 发明授权

KR100286083B1 이미페넴의 제조방법 失效
标题翻译：制备IMIPENEM的方法
公开(公告)号：KR100286083B1
公开(公告)日：2001-03-15
申请号：KR1019990004179
申请日：1999-02-08
申请人： 주식회사 씨트리
发明人： 김경수 , 이태석 , 육진수 , 윤정인 , 윤병훈 , 김완주
IPC分类号： C07D477/20
CPC分类号： Y02P20/55
摘要： 본발명은하기의반응식에따라, 일반식 (II)의비사이클릭케토에스테르를염기존재하에서포스포클로리데이트유도체와용매중에서축합시켜하기일반식 (III)의포스페이트유도체를제조하고; 같은반응용기내에서 2-아미노에탄티올의염산염을염기존재하에커플링시켜하기일반식 (IV)의티에나마이신유도체를제조하고; 같은반응용기내에서벤질이미데이트를가하여하기일반식 (V)의카르복실기가보호된이미페넴유도체를제조하고; 같은반응용기내에서테트라키스트리페닐포스핀팔라듐(0)과몰폴린유도체로보호기를제거하여하기일반식 (I)의이미페넴을제조하는방법에관한것이다. 상기식에서, X는수소또는클로라이드를나타낸다.

20. 发明授权

KR100408848B1 클래리스로마이신의 정제방법 失效
标题翻译： 클래리스로마이신의정제방법
公开(公告)号：KR100408848B1
公开(公告)日：2003-12-06
申请号：KR1020010012581
申请日：2001-03-12
申请人： 주식회사 씨트리 , 한솔케미언스 주식회사
发明人： 김완주 , 김경수 , 백용구 , 주소경 , 유정복 , 이동우 , 박성준 , 김상훈 , 장동조 , 김민수
IPC分类号： C07H17/08
摘要： PURPOSE: Provided is a purification process of clarithromycin, which is used for the treatment of stomach ulcer, has strong antibacterial effect and excellent pharmacological activity, in high yield and purity. CONSTITUTION: The purification process of clarithromycin, particularly 6-O-methylerythromycin of the formula(I), comprises the steps of: putting crystal type II of clarithromycin into a mixed solution of water, aqueous organic solvent, and non aqueous organic solvent; stirring the mixture and filtering it; washing it with water, aqueous organic solvent, and non aqueous organic solvent sequentially or with water and non aqueous organic solvent sequentially; then drying it to obtain pure clarithromycin.
摘要翻译：用途：提供克拉霉素纯化工艺，用于治疗胃溃疡，抗菌作用强，药理活性优良，收率高，纯度高。一种克拉霉素，特别是式（I）的6-O-甲基红霉素的纯化方法，包括以下步骤：将晶型II的克拉霉素放入水，有机溶剂水溶液和非水有机溶剂的混合溶液中; 搅拌混合物并过滤; 依次用水，含水有机溶剂和无水有机溶剂依次或用水和非水有机溶剂洗涤; 然后将其干燥以获得纯的克拉霉素。

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