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1. 发明授权

KR100600158B1 신규한 알카로이드 유도체 및 이를 함유하는 약제학적조성물 失效
标题翻译：新型碱性衍生物和含有其的药物组合物
公开(公告)号：KR100600158B1
公开(公告)日：2006-07-12
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： 본 발명은 다음 화학식 (Ⅰ)로 표시되는 신규한 할로겐기나 니트릭 에스테르 (nitric ester)기를 갖는 콜히친 유도체 및 그의 약제학적으로 허용되는 염 및 이 화합물을 활성성분으로 함유하는 항암작용, 항증식작용 및 면역억제작용을 갖는 약제학적 조성물을 제공하기 위한 것이다.

2. 发明公开

KR1020030026653A 프로피오니박테리움 아크네스의 활성을 저해하는 항체의생산용 항원 및 그의 제조방법과 이용 无效
标题翻译：抗生素抗生素抑制活性及其生产和使用的抗生素
公开(公告)号：KR1020030026653A
公开(公告)日：2003-04-03
申请号：KR1020010059730
申请日：2001-09-26
申请人： 주식회사 씨트리
发明人： 이석준 , 김희주 , 윤순대 , 김순옥 , 김경수 , 김완주
IPC分类号： A61K39/02
摘要： PURPOSE: Provided is a process of preparing a specific antigen used for the production of an antibody which inhibits the activity of Propionibacterium acnes as cause bacteria of acne. Therefore, eggs obtained from birds injected with the specific antigen have prevention and treatment effects on acne. CONSTITUTION: The preparing method of the specific antigen comprises the steps of: selectively separating a gene encoding any one of antigen selected from the group consisting of lipase, dnaK, groEL and hyase by performing PCR using, as a template, genomic DNA of P. acnes; extracting vector DNA by inserting the separated gene into a suitable vector, transforming an E. coli with the vector and amplifying the vector; amplifying the gene encoding the antigen 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 antigenic protein and extracting it.
摘要翻译：目的：提供一种制备用于产生抗体的特异性抗原的方法，所述抗体抑制痤疮丙酸杆菌作为引起痤疮细菌的活性。因此，从注射特定抗原的鸟获得的卵对痤疮具有预防和治疗作用。构成：特异性抗原的制备方法包括以下步骤：通过使用P的基因组DNA作为模板，通过PCR来选择性分离编码选自脂肪酶，dnaK，groEL和hyase中的任一种的抗原的基因。痤疮; 通过将分离的基因插入合适的载体中提取载体DNA，用载体转化大肠杆菌并扩增载体; 通过使用提取的载体DNA作为模板进行PCR扩增编码抗原的基因; 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; 培养宿主，然后过表达抗原蛋白并提取。

3. 发明公开

KR1020020016276A 항진균제용 터비나핀 및 그 염산염의 제조방법 无效
标题翻译：生产用于抗真菌药物的丝氨酸蛋白酶及其盐酸盐的方法
公开(公告)号：KR1020020016276A
公开(公告)日：2002-03-04
申请号：KR1020000049521
申请日：2000-08-25
申请人： 주식회사 씨트리
发明人： 백용구 , 김경수 , 이동우 , 유정복 , 박성준 , 김완주
IPC分类号： C07C209/10
摘要： PURPOSE: Provided is a process for producing terbinafine and hydrochloride thereof used as an antifungal agent, which can be used for oral administration and hardly has toxicity. CONSTITUTION: The process comprises the steps of: preparing a halide intermediate by reacting 6,6-dimethyl-2-(E)-heptene-4-ynil alcohol(formula III) and a halogenating agent such as SOCl2, SOBr2, HCl, HBr, PCl3, PCl5, and etc.; preparing (E)-N-(6,6-dimethyl-2-heptyne-4-ynil)-N-methyl-1-naphthaleneamine(terbinafine)(formula I) by reacting the halide intermediate(formula IV) with N-methyl-1-naphthalene methanamine in the presence of potassium carbonate; preparing the hydrochloride(formula II) of the terbinafine by acidifying the terbinafine in a methanolic HCl solution and then performing recrystallization.
摘要翻译：目的：提供用作抗真菌剂的特比萘芬和盐酸盐的制备方法，其可用于口服给药，几乎不具有毒性。方法：该方法包括以下步骤：通过使6,6-二甲基-2-（E） - 庚烯-4-炔醇（式III）和卤化剂如SOCl 2，SOBr 2，HCl，HBr反应制备卤化物中间体，PCl3，PCl5等; 通过使卤化物中间体（式IV）与N-甲基（式II）反应制备（E）-N-（6,6-二甲基-2-庚炔-4-基）-N-甲基-1-萘胺（特比萘芬）（式I） -1-萘甲胺在碳酸钾存在下反应; 通过在甲醇HCl溶液中酸化特比萘芬，然后进行重结晶，制备特比萘芬的盐酸盐（式II）。

4. 发明公开

KR1020010081232A 산도에 민감한 중합체를 이용한 달걀 면역 항체의캡슐화방법 无效
标题翻译：使用聚合物对酸性敏感的蛋黄免疫球蛋白包埋方法
公开(公告)号：KR1020010081232A
公开(公告)日：2001-08-29
申请号：KR1020000006415
申请日：2000-02-11
申请人： 주식회사 씨트리
发明人： 김완주 , 김경수 , 이유정 , 요시노리미네
IPC分类号： A61K9/48
CPC分类号： Y02A50/473 , Y02A50/481 , Y02A50/483 , A61K9/5026 , A61K9/4833 , A61K39/395 , A61K2039/505
摘要： PURPOSE: A method for encapsulating egg yolk antibodies IgY by using a methacrylate monomer or polymer solution sensitive to acidity is provided, which increases stability to heat, low pH such as gastric acid and proteinase present in an alimentary system. CONSTITUTION: Encapsulation method of egg yolk immunoglobulins (IgY) comprises adding 0.1 to 10% methacrylate monomer or polymer solution to egg yolk containing specific antibodies and freeze-drying. The specific antibodies are anti-H. pylori IgY, anti-Rotavirus IgY, anti-enterotoxigenic E. coli IgY, anti-Y. reckeri IgY, anti-Edward tarda IgY, anti-Edward siella Igy, anti-Vibrio Igy, anti-Salmonella gallinarum IgY, anti-Salmonella enteritidis IgY, anti-Streptococcus iniae IgY and anti-Fowl Typhoid IgY.
摘要翻译：目的：提供一种通过使用对酸度敏感的甲基丙烯酸酯单体或聚合物溶液来包封蛋黄抗体IgY的方法，其增加了耐热性，低pH（例如存在于消化系统中的胃酸和蛋白酶）的稳定性。构成：蛋黄免疫球蛋白（IgY）的包封方法包括向含有特异性抗体的蛋黄中加入0.1〜10％的甲基丙烯酸酯单体或聚合物溶液并进行冷冻干燥。特异性抗体为抗H。幽门螺杆菌IgY，抗轮状病毒IgY，抗肠毒素性大肠杆菌IgY，抗Y。 reckeri IgY，抗Edward tarda IgY，抗Edward siella Igy，抗弧菌Igy，抗沙门氏菌IgY，抗肠炎沙门氏菌IgY，抗链球菌IgY和抗家禽伤寒IgY。

5. 发明公开

KR1020000065691A 항진균제용 터비나핀 및 그 염산염의 제조방법 有权
标题翻译：作为抗生素剂及其盐酸盐的生产酪氨酸蛋白酶
公开(公告)号：KR1020000065691A
公开(公告)日：2000-11-15
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： PURPOSE: A process for preparing the titled compound by using N-methyl-1-naphthalenemethaneamine or its hydrochloric acid salt and 1,3-dichloropropene as a starting material and reacting in the presence of a palladium catalyst system and an alkali is provided which produces a terbinafine compound in high yield and inhibits side reactions. CONSTITUTION: N-methyl-1-naphthalenemethaneamine or its hydrochloric acid salt and 1,3-dichloropropene are reacted with 0.5 to 5% by mole of a palladium catalyst selected from (PPh3)2PdCl2, (PhCN)2PdCl2 or (PPh3)4Pd in a nonpolar solvent in the presence of an alkali at 0 to 50°C for 1 to 2 hr to give N-methyl-N-(3-chloro-1-propene-2-yl)-naphthalenemethaneamine of formula (II), which is added with cul and amine, 3,3-dimethyl-1-butine successively to give (E)-terbinafine of formula (I).
摘要翻译：目的：提供使用N-甲基-1-萘甲烷或其盐酸盐和1,3-二氯丙烯作为原料并在钯催化剂体系和碱的存在下反应制备标题化合物的方法，其产生特比萘芬化合物高产量并抑制副反应。构成：将N-甲基-1-萘甲烷或其盐酸盐和1,3-二氯丙烯与0.5〜5摩尔％的选自（PPh 3）2 PdCl 2，（PhCN）2 PdCl 2或（PPh 3）4 Pd的钯催化剂反应，非碱性溶剂，在碱存在下，在0〜50℃下反应1〜2小时，得到式（II）的N-甲基-N-（3-氯-1-丙烯-2-基） - 萘甲烷胺，其中加入苦味胺和3,3-二甲基-1-丁胺，得到式（I）的（E） - 喋呤。

6. 发明授权

KR101872726B1 텔미사르탄 메탄술폰산염 및 이를 포함하는 약제학적 조성물 有权
公开(公告)号：KR101872726B1
公开(公告)日：2018-06-29
申请号：KR1020160096285
申请日：2016-07-28
申请人： 주식회사 씨트리
发明人： 김경수 , 이동엽 , 공준수 , 김병수 , 최혁 , 김완주
IPC分类号： C07D235/20 , A61K31/4184 , A61K9/20
摘要： 본발명은텔미사르탄메탄술폰산염및 이를포함하는약제학적조성물에관한것이다. 본발명에따른텔미사르탄메탄술폰산염은안정성, 용해도및 고체흐름성이우수할뿐만아니라, 간단한직접압축법에의해용출율이우수한정제를제조할수 있어약제학적조성물에효과적으로사용될수 있다.

7. 发明授权

KR100430575B1 란소프라졸 및 그 중간체의 제조방법 失效
标题翻译： 란프프졸졸졸및법법법법법법법
公开(公告)号：KR100430575B1
公开(公告)日：2004-05-10
申请号：KR1020010008677
申请日：2001-02-21
申请人： 주식회사 씨트리 , 한솔케미언스 주식회사
发明人： 김경수 , 박종억 , 장정민 , 최재원 , 김명화 , 김완주 , 백용구 , 유용상
IPC分类号： C07D401/12
CPC分类号： C07D401/12
摘要： The present invention relates to a process for preparing lansoprazole of the following formula (I) and its intermediate, 2-[3-methyl-4(2,2,2-trifluoroethoxy)-2-pyridil]methylthio-1H-benzimidazole of the following formula (II), which comprises reacting 2-hydroxymethyl-3-methyl-4-(2,2,2-trifluoroethoxy) pyridine or its salt with 2-mercaptobenzimidazole in the presence of a halogenating agent and reaction solvent, and then oxidizing the resulting compound (II) with hydrogen peroxide in the presence of a benzeneseleninic acid catalyst and reaction solution to obtain lansoprazole(I).
摘要翻译：本发明涉及制备下式（I）的兰索拉唑及其中间体2- [3-甲基-4-（2,2,2-三氟乙氧基）-2-吡啶基]甲硫基-1H-苯并咪唑的方法其包括在卤化剂和反应溶剂存在下使2-羟甲基-3-甲基-4-（2,2,2-三氟乙氧基）吡啶或其盐与2-巯基苯并咪唑反应，然后氧化在苯亚磺酸催化剂和反应溶液存在下用过氧化氢将所得化合物（II）与所述化合物（II）反应以获得兰索拉唑（I）。

8. 发明授权

KR100367201B1 항혈액응고성 살서제인 4-하이드록시쿠마린 중간체의제조방법 失效
标题翻译： 항혈액응고성살서제인인4하이드록시쿠마린중체체의제조방항
公开(公告)号：KR100367201B1
公开(公告)日：2003-01-14
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：提供一种制造抗凝血杀鼠剂4-羟基香豆素中间体的方法，以制备抗凝血杀鼠剂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，其以3-（4-甲氧基）苯基-4-苯基丁酸简单且高产率地表示。构成：如下述结构式（II）所示的4-羟基香豆素中间体的制造方法包括：在钯催化下，使苄基卤与丙烯酸烷基酯反应，制造下述结构式（III）所示的化合物的第1工序; 类似于第一步骤，通过在钯催化剂下进行反应来制造下列结构式（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还原第二步中获得的结构式（IV）的化合物来制造如下结构式（V）所示的化合物的第三步骤; 以及不分离结构式（V）的化合物而进行皂化反应和酸处理的下一步骤的第四步骤。

9. 发明公开

KR1020180013107A 텔미사르탄 메탄술폰산염 및 이를 포함하는 약제학적 조성물 有权
标题翻译：替米沙坦甲磺酸盐及包含其的药物组合物
公开(公告)号：KR1020180013107A
公开(公告)日：2018-02-07
申请号：KR1020160096285
申请日：2016-07-28
申请人： 주식회사 씨트리
发明人： 김경수 , 이동엽 , 공준수 , 김병수 , 최혁 , 김완주
IPC分类号： C07D235/20 , A61K31/4184 , A61K9/20
CPC分类号： C07D235/20 , A61K9/20 , A61K31/4184 , C07B2200/13
摘要： 본발명은텔미사르탄메탄술폰산염및 이를포함하는약제학적조성물에관한것이다. 본발명에따른텔미사르탄메탄술폰산염은안정성, 용해도및 고체흐름성이우수할뿐만아니라, 간단한직접압축법에의해용출율이우수한정제를제조할수 있어약제학적조성물에효과적으로사용될수 있다.
摘要翻译：本发明涉及替米沙坦甲磺酸盐和包含其的药物组合物。根据本发明它可以产生一个稳定的，固体的溶解性和流动性能，由该压缩方法的简单直接优良片剂的溶解速率以及yiwoosu可以有效地在药物组合物中使用替米沙坦甲磺酸酯。

10. 发明授权

KR100433735B1 결정형 Ⅰ을 갖는 란소프라졸의 제조방법 失效
标题翻译： 결정형I을갖는란소프라졸의제조방법
公开(公告)号：KR100433735B1
公开(公告)日：2004-06-04
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：用途：提供一种将兰索拉唑（晶形II）改性和纯化为兰索拉唑（晶型I）的方法，该兰索拉唑是热力学稳定的并用作药物。由式（I）表示的兰索拉唑是质子泵（抗溃疡剂）的抑制剂，具有强抗菌活性和优异的药理学活性，因此可用作胃溃疡的治疗剂。构成：该方法包括以下步骤：将1重量％的兰索拉唑（晶形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; 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; 具有多于5个碳的烃，如戊烷，己烷，庚烷环己烷; 腈如乙腈; 酮如丙酮; 及其混合物。

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