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1. 发明授权

KR100441638B1 새로운 에이사이클릭 뉴클레오사이드 포스포네이트유도체, 그의 염 및 합성 방법 有权
标题翻译： 새로운에이사이클릭뉴클레이，，，법법법법법
公开(公告)号：KR100441638B1
公开(公告)日：2004-07-23
申请号：KR1020020003051
申请日：2002-01-18
申请人： 주식회사 엘지생명과학
发明人： 최종류 , 김정민 , 노기윤 , 조동규 , 임재홍 , 황재택 , 조우영 , 장현숙 , 이장호 , 김태균 , 조승주 , 김경원 , 최태생 , 김청미 , 김용주
IPC分类号： C07F9/38
CPC分类号： C07H19/10 , C07F9/65616 , C07H19/20
摘要： The present invention relates to a nucleoside phosphonate derivative represented by formula (1): pharmaceutically acceptable salts, and stereoisomers. This nucleoside phosphonate derivative is useful as an antiviral agent, particularly, against hepatitis B virus. Also disclosed are processes for the preparation of the nucleoside phosphonate derivative. Also disclosed are methods treating hepatitis B by administering a nucleoside phosphonate derivative of formula (1).
摘要翻译：本发明涉及由式（1）表示的核苷膦酸酯衍生物：药学上可接受的盐和立体异构体。该核苷膦酸酯衍生物可用作抗病毒剂，特别是抗乙型肝炎病毒。还公开了制备核苷膦酸酯衍生物的方法。还公开了通过施用式（1）的核苷膦酸酯衍生物来治疗乙型肝炎的方法。

2. 发明公开

KR1020030070240A 씨형 간염바이러스 복제효소의 활성측정방법 失效
标题翻译：测定丙型肝炎病毒复制活性的方法
公开(公告)号：KR1020030070240A
公开(公告)日：2003-08-29
申请号：KR1020020009304
申请日：2002-02-21
申请人： 주식회사 엘지생명과학
发明人： 이미경 , 김정민 , 조영규 , 노기윤 , 김경원 , 김태균 , 조우영 , 조동규
IPC分类号： G01N33/573
摘要： PURPOSE: A method for measuring activity of hepatitis C virus replicase is provided, thereby automatically carrying out HTS(High-throughput screening) analysis using SPA(Scintillation proximity assay)-based screening technologies. CONSTITUTION: A method for measuring activity of hepatitis C virus replicase comprises the steps of: mixing substrates containing isotope-labeled substrate, HCV(hepatitis C virus) replicase, SPA beads, biotin-15-UTP as a primer, poly A-500 as a template RNA, and buffer solution; carrying out the polymerization using the mixture; and measuring activity of HCV replicase using a liquid scintillation counter, wherein the isotope labeled substrate comprises 5,6-3H-UTP and another UTP; the SPA bead is streptavidin-SPA bead; and inhibitors of the polymerization process contain dimethylsulfoxide.
摘要翻译：目的：提供一种测定丙型肝炎病毒复制酶活性的方法，从而自动进行使用SPA（闪烁邻近测定）筛选技术的HTS（高通量筛选）分析。构成：用于测定丙型肝炎病毒复制酶活性的方法包括以下步骤：将含有同位素标记底物，HCV（丙型肝炎病毒）复制酶，SPA珠粒，生物素-15-UTP作为底物的底物，聚A-500作为模板RNA和缓冲溶液; 使用混合物进行聚合; 并使用液体闪烁计数器测量HCV复制酶的活性，其中同位素标记的底物包含5,6-3H-UTP和另一种UTP; SPA珠是链霉抗生物素蛋白-SPA珠; 并且聚合方法的抑制剂含有二甲亚砜。

3. 发明公开

KR1020020062216A 새로운 에이사이클릭 뉴클레오사이드 포스포네이트유도체, 그의 염 및 합성 방법 有权
标题翻译：新型ACYCLIC核苷酸衍生物及其合成方法及其合成方法
公开(公告)号：KR1020020062216A
公开(公告)日：2002-07-25
申请号：KR1020020003051
申请日：2002-01-18
申请人： 주식회사 엘지생명과학
发明人： 최종류 , 김정민 , 노기윤 , 조동규 , 임재홍 , 황재택 , 조우영 , 장현숙 , 이장호 , 김태균 , 조승주 , 김경원 , 최태생 , 김청미 , 김용주
IPC分类号： C07F9/38
CPC分类号： C07H19/10 , C07F9/65616 , C07H19/20
摘要： PURPOSE: Provided are a novel Acyclic nucleoside phosphonate derivative which is useful as an anti-viral agent(especially hepatitis B virus), its pharmaceutically acceptable salt and stereochemical isomer, and their synthesis method. CONSTITUTION: Acyclic nucleoside phosphonate derivative is represented by the formula(1), wherein R1, R2, R3, R4, R5, R7, R8, Y and Q are as described in the description. It comprises natural base, such as adenine, guanine, uracil, thymine or their derivative. It is manufactured by: (a) reacting a compound of the formula(2) with a compound of the formula(3) of QH; (b) reacting a compound of the formula(9) with a compound of the formula(3) of QH to obtain a compound of the formula(10) then hydrolyzing the compound of the formula(10) in the presence of Lewis acid to obtain a compound of the formula(1a); or (c) introducing R4 and R5 to the compound of the formula(1a) to obtain a compound of the formula(1b) then converting it.
摘要翻译：目的：提供一种可用作抗病毒剂（特别是乙型肝炎病毒），其药学上可接受的盐和立体化学异构体的新型非环型核苷膦酸酯衍生物及其合成方法。构成：无环核苷膦酸酯衍生物由式（1）表示，其中R 1，R 2，R 3，R 4，R 5，R 7，R 8，Y和Q如说明书所述。它包括天然碱，如腺嘌呤，鸟嘌呤，尿嘧啶，胸腺嘧啶或其衍生物。通过以下方法制备：（a）使式（2）的化合物与QH的式（3）的化合物反应; （b）使式（9）的化合物与QH的式（3）的化合物反应，得到式（10）的化合物，然后在路易斯酸的存在下将式（10）的化合物水解成得到式（1a）化合物; 或（c）将R4和R5引入式（1a）化合物，得到式（1b）化合物，然后转化。

4. 发明授权

KR100462328B1 씨형 간염바이러스 복제효소의 활성측정방법 失效
标题翻译： 씨형간염바이러스복제효소의활성측정방법
公开(公告)号：KR100462328B1
公开(公告)日：2004-12-17
申请号：KR1020020009304
申请日：2002-02-21
申请人： 주식회사 엘지생명과학
发明人： 이미경 , 김정민 , 조영규 , 노기윤 , 김경원 , 김태균 , 조우영 , 조동규
IPC分类号： G01N33/573
摘要： PURPOSE: A method for measuring activity of hepatitis C virus replicase is provided, thereby automatically carrying out HTS(High-throughput screening) analysis using SPA(Scintillation proximity assay)-based screening technologies. CONSTITUTION: A method for measuring activity of hepatitis C virus replicase comprises the steps of: mixing substrates containing isotope-labeled substrate, HCV(hepatitis C virus) replicase, SPA beads, biotin-15-UTP as a primer, poly A-500 as a template RNA, and buffer solution; carrying out the polymerization using the mixture; and measuring activity of HCV replicase using a liquid scintillation counter, wherein the isotope labeled substrate comprises 5,6-3H-UTP and another UTP; the SPA bead is streptavidin-SPA bead; and inhibitors of the polymerization process contain dimethylsulfoxide.
摘要翻译：目的：提供一种测量丙型肝炎病毒复制酶活性的方法，从而使用基于SPA（闪烁邻近测定）的筛选技术自动进行HTS（高通量筛选）分析。构成：测定丙型肝炎病毒复制酶活性的方法包括以下步骤：将含有同位素标记的底物，HCV（丙型肝炎病毒）复制酶，SPA珠粒，生物素-15-UTP作为引物，聚A-500的底物模板RNA和缓冲溶液; 使用混合物进行聚合; 并使用液体闪烁计数器测量HCV复制酶的活性，其中同位素标记的底物包含5,6-3H-UTP和另一种UTP; SPA珠是链霉亲和素-SPA珠; 并且聚合过程的抑制剂含有二甲基亚砜。

5. 发明公开

KR1020040027452A (1-포스포노메톡시-2-알킬사이클로프로필)메틸뉴클레오사이드유도체의 (+)-트랜스 이성질체, 그의 입체이성질체의제조방법 및 항바이러스제로서의 용도 无效
标题翻译：（+） - （1-膦酰基-2-羟基-2-甲基-2-环丙基）甲基核苷衍生物的转移异构体，制备其立体异构体的方法及其用途
公开(公告)号：KR1020040027452A
公开(公告)日：2004-04-01
申请号：KR1020030066912
申请日：2003-09-26
申请人： 주식회사 엘지생명과학
发明人： 최종류 , 황재택 , 조동규 , 노기윤 , 김천형 , 김청미 , 한민준 , 김정민 , 조우영 , 김경원 , 안신병
IPC分类号： C07F9/6561
CPC分类号： C07F9/65616 , C07F9/4006 , C07F9/65121
摘要： PURPOSE: A (+)-trans isomer of a (1-phosphonomethoxy-2-alkylcyclopropyl) methyl nucleoside derivative, a process for preparing stereoisomer thereof, and the use thereof are provided. The isomer is useful as an anti-viral agent, especially a hepatitis B virus treating agent. CONSTITUTION: A (+)-trans isomer of (1-phosphonomethoxy-2-alkylcyclopropyl) methyl nucleoside derivative represented by the formula(1), pharmaceutically acceptable salts, hydrate or solvates thereof are provided. In the formula, R1 is C1-C7 alkyl; R2 and R3 are independently hydrogen, halogen, C1-C4 alkoxy, phenoxy, C7-C10 phenylalkoxy, C1-C4 alkyl optionally substituted with C2-C5 acyloxy, C2-C7 acyl, C6-C12 aryl, C1-C7 alkylaminocarbonyl, di(C1-C7 alkyl)aminocarbonyl, C3-C6 cycloalkylaminocarbonyl, or -(CH2)m-OC(=O)-R4; R4 is C1-C12 alkyl, C2-C7 alkenyl, C1-C5 alkoxy, C1-C7 alkylamino, di(C1-C7 alkyl)amino, C3-C6 cycloalkyl or 3- to 6-membered ring heterocycle containing 1 or 2 hetero atoms selected from nitrogen and oxygen; m is an integer of 1 to 12; X1, X2, X3 and X4 are independently hydrogen, amino, hydroxy or halogen, or C1-C7 alkyl optionally substituted with nitro or C1-C5 alkoxy, C1-C5 alkoxy, allyl, hydroxy-C1-C7 alkyl, phenyl, or phenoxy, C6-C10 arylthio optionally substituted with nitro, amino, C1-C6 alkyl or C1-C4 alkoxy, C6-C12 arylamino, C1-C7 alkylamino, di(C1-C7 alkyl)amino, or C3-C6 cycloalkylamino; n is an integer of 1 or 2; Y1 is O, CH2 or N-R; and R is C1-C7 alkyl or C6-C12 aryl.
摘要翻译：目的：提供（1-膦基甲氧基-2-烷基环丙基）甲基核苷衍生物的（+） - 反式异构体，其制备立体异构体的方法及其用途。异构体可用作抗病毒剂，特别是乙型肝炎病毒治疗剂。构成：提供由式（1）表示的（1-膦基甲氧基-2-烷基环丙基）甲基核苷衍生物的（+） - 反式异构体，其药学上可接受的盐，水合物或溶剂合物。在该式中，R 1是C 1 -C 7烷基; R2和R3独立地是氢，卤素，C1-C4烷氧基，苯氧基，C7-C10苯基烷氧基，任选地被C 2 -C 5酰氧基取代的C 1 -C 4烷基，C 2 -C 7酰基，C 6 -C 12芳基，C 1 -C 7烷基氨基羰基， C 1 -C 7烷基）氨基羰基，C 3 -C 6环烷基氨基羰基或 - （CH 2）m OC（= O）-R 4; R4是C1-C12烷基，C2-C7链烯基，C1-C5烷氧基，C1-C7烷基氨基，二（C1-C7烷基）氨基，C3-C6环烷基或含1或2个杂原子的3至6元环杂环选自氮和氧; m为1〜12的整数。任选被硝基或C 1 -C 5烷氧基取代的C 1 -C 7烷基，C 1 -C 5烷氧基，烯丙基，羟基-C 1 -C 7烷基，苯基或苯氧基任选被硝基，氨基，C 1 -C 6烷基或C 1 -C 4烷氧基取代的C 6 -C 10芳硫基，C 6 -C 12芳基氨基，C 1 -C 7烷基氨基，二（C 1 -C 7烷基）氨基或C 3 -C 6环烷基氨基; n是1或2的整数; Y1是O，CH2或N-R; 且R为C 1 -C 7烷基或C 6 -C 12芳基。

6. 发明公开

KR1020020074683A 항바이러스성 2,4-피리미딘디온 유도체 및 그의 제조방법 无效
标题翻译：有害的2,4-二吡啶衍生物及其生产
公开(公告)号：KR1020020074683A
公开(公告)日：2002-10-04
申请号：KR1020010014624
申请日：2001-03-21
申请人： 주식회사 엘지생명과학
发明人： 임재홍 , 최종류 , 김정민 , 조동규 , 노기윤 , 황재택 , 이장호 , 장현숙 , 조우영 , 김은경
IPC分类号： C07D239/46
摘要： PURPOSE: A process of preparing new 2,4-pyrimidinedione derivatives having high antiviral activity against Hepatitis B virus and low toxicity is provided. Whereby, the composition can be effectively used in treatment and prevention of Hepatitis B virus. CONSTITUTION: The titled compound of the formula 1 is prepared by alkylation of a compound of formula 2 with a compound of a formula R-X or 3b. In formula, R, R2 and R3 are each independently H or C1-8 alkyl, with the proviso that R1, R2 and R3 are the same at the same time, A represents two hydrogen atoms, CH2, O, S or NH, Ar represents phenyl or naphtyl capable of being substituted by a substituent selected from the group consisting of C1-4 alkyl, C1-4 alkoxy, amino and C1-4 alkylamino, X represents halogen.
摘要翻译：目的：提供一种制备具有抗乙型肝炎病毒抗病毒活性和毒性低的新型2,4-嘧啶二酮衍生物的方法。因此，该组合物可有效地用于治疗和预防乙型肝炎病毒。构成：式1的标题化合物通过用式R-X或3b的化合物烷基化式2的化合物来制备。在式中，R，R 2和R 3各自独立地为H或C 1-8烷基，条件是R 1，R 2和R 3同时相同，A表示两个氢原子，CH 2，O，S或NH，Ar 表示能够被选自C 1-4烷基，C 1-4烷氧基，氨基和C 1-4烷基氨基的取代基取代的苯基或萘基，X表示卤素。

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