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1. 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）

2. 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.

3. 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）。

4. 发明公开

KR1020020068592A 란소프라졸 및 그 중간체의 제조방법 失效
标题翻译：制备兰索唑及其中间体的方法
公开(公告)号：KR1020020068592A
公开(公告)日：2002-08-28
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： PURPOSE: Provided is a method of preparing 2-(3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridyl)methylsulfinyl-1H-benzimidazol(hereinafter referred to lansoprazole) and its intermediate, 2-(3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridyl)methylthio-1H-benzimidazol. CONSTITUTION: Lansoprazole of the formula(I) is manufactured by; reacting 2-hydroxymethyl-3-methyl-4-(2,2,2-trifluroroethoxy)pyridine or its salt with a halogenating agent or an additive in a reaction solution to manufacture its intermediate, 2-(3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridyl)methylthio-1H-benzimidazol, of the formula(II) in high yield; and oxidizing it with hydrogen peroxide under the presence of a reaction solution and acid catalyst.
摘要翻译：目的：提供2-（3-甲基-4-（2,2,2-三氟乙氧基）-2-吡啶基）甲基亚磺酰基-1H-苯并咪唑（以下称为兰索拉唑）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。组成：式（I）的兰索拉唑由将2-羟甲基-3-甲基-4-（2,2,2-三氟乙氧基）吡啶或其盐与卤化剂或添加剂在反应溶液中反应制备其中间体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，高产率的式（II）并在反应溶液和酸催化剂存在下用过氧化氢氧化。

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