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    • 1. 发明公开
      KR1020070095236A 피리다지논, 피리미돈 또는 피리돈 구조를 포함하는선택적인 트롬빈 억제제 失效
    • 피리다지논, 피리미돈 또는 피리돈 구조를 포함하는선택적인 트롬빈 억제제
    • 基于吡咯烷酮，吡咯烷酮或吡咯烷酮的选择性硫蛋白抑制剂
    • KR1020070095236A
    • 2007-09-28
    • KR1020070027069
    • 2007-03-20
    • 주식회사 엘지생명과학
    • 박태교 , 이현호 , 박종우 , 송호영 , 최증순 , 박희동 , 김태훈 , 김경희 , 이태수 , 장민선 , 이재익 , 권태식 , 하용화 , 서동욱 , 최윤희 , 이정애 , 오영수 , 백승엽 , 김형진 , 박미정 , 윤하식 , 정수용
    • C07D237/14 , C07D237/22 , C07D401/10
    • A novel compound is provided to secure excellent thrombin inhibitory activity and excellent selectivity on the thrombin and is able to be orally absorbed. And a method for preparing the same and a pharmaceutical composition comprising the same are provided. A compound is represented by the formula(1), wherein A is N or CR^1, B is N or CR^2, each R^3 and R^4 is H, OH, halogen, CN, CF3, or C1-8 alkyl, or R^3 and R^4 together with a carbon atom attached thereto forms C=O, 3 to 8 membered cycloalkyl, or 3 to 8 membered heterocycle having at least one atom selected from the group consisting of N, O and S, R^5 is (a) H, (b) halogen, (c) CN or CH2CN, (d) CF3, OR^6, S(O)0-2R^6, C(=O)R^6, S(O)2NHR^6, and NR^6R^6a, (e) halogen, CN, CF3, OH, and phenyl substituted or unsubstituted by C1-4 alkoxy, (f) halogen, OH, CN, C1-8 alkoxy, COOH, COO-C1-8 alkyl and C1-8 alkyl mono-substituted or poly-substituted by COO-C1-8 alkyl, (g) halogen, OH, CN, C1-8 alkoxy, COOH, COO-C1-8 alkyl and 3 to 8 membered cycloalkyl mono-substituted or poly-substituted by COO-C1-8 alkyl, or (h) 3 to 8 membered heterocycle or 5 to 8 membered heteroaryl including at least one hetero atom selected from the group consisting of N, O and S, m is an integer from 0 to 3, n is an integer from 1 to 6, k is an integer from 0 to 3, and P1 is C1-8 alkyl substituted or unsubstituted by one or two radicals selected from R^7 and R^7, C2-8 alkenyl, 3 to 8 membered cycloalkyl, 4 to 8 membered cycloalkenyl, phenyl, 3 to 8 membered heterocycle including 1-5 heteroatoms selected from the group consisting of N, O and S, or 5 to 8 membered heteroaryl including 1-5 heteroatoms selected from the group consisting of N, O and S.
    • 提供了一种新颖的化合物以确保优良的凝血酶抑制活性和对凝血酶的优异选择性，并且能够被口服吸收。 并提供其制备方法和包含其的药物组合物。 化合物由式（1）表示，其中A是N或CR 1，B是N或CR 2，每个R 3和R 4是H，OH，卤素，CN，CF 3或C1- 8烷基或R 3和R 4与连接的碳原子一起形成C = O 3至8元环烷基或具有至少一个选自N，O的原子的3至8元杂环，以及 S，R 5是（a）H，（b）卤素，（c）CN或CH 2 CN，（d）CF 3，OR 6，S（O）0-2R 6，C（= O） ，（C）卤素，CN，CF 3，OH和被C 1-4烷氧基取代或未取代的苯基，（f）卤素，OH，CN，C 1-8 烷氧基，COOH，COO-C 1-8烷基和被COO-C 1-8烷基单取代或多取代的C 1-8烷基，（g）卤素，OH，CN，C 1-8烷氧基，COOH，COO- 8烷基和3至8元环烷基，其被COO-C 1-8烷基单取代或多取代，或（h）3至8元杂环或5至8元杂芳基，包括至少一个选自以下的杂原子： N，O和S，m为0〜3的整数，n为整数 r为1至6，k为0至3的整数，P1为被一个或两个选自R 7和R 7的基团取代或未取代的C 1-8烷基，C 2-8链烯基，3至8元环烷基 ，4至8元环烯基，苯基，3至8元杂环，包括1-5个选自N，O和S的杂原子，或5至8元杂芳基，包括1-5个选自N， O和S.
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
    • 2. 发明公开
      KR1020030080509A 우레아, 티오우레아 및 설파마이드 유도체를 함유하는항균제 조성물 无效
    • 우레아, 티오우레아 및 설파마이드 유도체를 함유하는항균제 조성물
    • 含有尿素，硫脲和磺酰胺衍生物的抗菌剂组合物
    • KR1020030080509A
    • 2003-10-17
    • KR1020020019177
    • 2002-04-09
    • 주식회사 엘지생명과학
    • 윤주용 , 김원섭 , 이현호 , 임재홍 , 이석원 , 윤승현 , 송정욱 , 김종엽 , 최성필 , 윤하식 , 조양래
    • A61K31/18
    • PURPOSE: An antibacterial agent composition containing urea, thiourea and sulfamide derivatives as an effective ingredient is provided. Therefore, it shows antimicrobial activity and an antibacterial spectrum against wide pathogens containing various Gram positive bacteria and thus is expected to be useful in the prevention and treatment of animal disease caused by bacterial infection. CONSTITUTION: The antibacterial agent composition contains urea, thiourea, sulfamide derivatives and a pharmaceutically acceptable salt, hydrate and solvate thereof represented by the formula I. In formula, each of X and Y is hydrogen, chlorine or trifluoromethyl, Z is -CO-, -CS- or -SO2-. Therefore, it exhibits excellent antibacterial activity against methicillin-resistant Staphylococcus aureus. It can be administered in the form of injectable formulations or oral formulations.
    • 目的：提供含有脲，硫脲和磺酰胺衍生物作为有效成分的抗菌剂组合物。 因此，它表现出抗菌活性和对含有各种革兰氏阳性菌的广病原体的抗菌谱，因此预期可用于预防和治疗由细菌感染引起的动物疾病。 构成：抗菌剂组合物含有式I所示的尿素，硫脲，磺酰胺衍生物及其药学上可接受的盐，水合物和溶剂合物。在式中，X和Y各自为氢，氯或三氟甲基，Z为-CO-， -CS-或-SO 2 - 。 因此，对耐甲氧西林金黄色葡萄球菌具有优异的抗菌活性。 其可以以可注射制剂或口服制剂的形式施用。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
    • 3. 发明公开
      KR1020030064970A 신규 살리실아닐라이드 유도체 및 그를 함유하는 항균제조성물 无效
    • 신규 살리실아닐라이드 유도체 및 그를 함유하는 항균제조성물
    • 新型磺胺衍生物和抗生素组合物
    • KR1020030064970A
    • 2003-08-06
    • KR1020020005069
    • 2002-01-29
    • 주식회사 엘지생명과학
    • 윤승현 , 김원섭 , 이현호 , 임재홍 , 윤주용 , 김종엽 , 송정욱 , 이석원 , 최성필 , 바실리아티모프 , 윤하식 , 조양래
    • C07D213/75
    • PURPOSE: Provided are novel salicylanilide derivatives represented by formula 1 which are useful as antibiotic against methicillin resistant Staphylococcus aureus(MRSA), their pharmaceutically acceptable non toxic salts, their biologically hydrolyzable ester, hydrate, solution product and their isomers. CONSTITUTION: The novel salicylanilide derivatives are represented by formula 1, wherein R is hydrogen, C1-6 alkyl, C1-3 alkoxy, acetyl or benzyl; X and Y are independently hydrogen, halogen, amino or nitro; Z is nitrogen, oxygen, sulfur, -O-(CH2)m-, -(CH2)m-O-, sulfone or sulfonamino where m is an integer of 1 to 3; A is I, V, W substituted hetero aryl containing Q2, V, W substituted bicyclic hetero aryl containing Q2 and Q3 and I, W substituted indane containing Q2, Q3, Q4 where Q1, Q2, Q3 and Q4 are each independently, one selected from N, C and S; G, J, I, V, W are each independently hydrogen, C1-6 alkyl substituted or non-substituted by halogen, C3-6 cyclo alkyl, C1-6 alkoxy, hydroxy, halogen, cyano, nitro, sulfone sulfonamide, hydroxy carbonyl, C1-6alkoxy carbonyl, C6-8 aryl, C5-8 hetero aryl substituted or non-substituted by halogen, which contains one or two atom selected from N, O and S, or C2-9 hetero aryl oxy substituted or non-substituted by halogen, which contains one or two atom selected from N, O and S. The compounds of formula 1 is synthesized by reacting compounds of formula 2 with compounds of formula 3 in a solvent in presence of base and catalyst. In the formula 2 and 3, R, X, Y, Z, A, Q1, G and J are the same as above.
    • 目的：提供由式1表示的新型水杨酰苯胺衍生物，其可用作耐甲氧西林金黄色葡萄球菌（MRSA），其药学上可接受的无毒盐，其生物可水解酯，水合物，溶液产物及其异构体的抗生素。 构成：新型水杨酰苯胺衍生物由式1表示，其中R是氢，C 1-6烷基，C 1-3烷氧基，乙酰基或苄基; X和Y独立地是氢，卤素，氨基或硝基; Z是氮，氧，硫，-O-（CH 2）m - ， - （CH 2）m -O-，砜或磺氨基，其中m是1至3的整数; A是I，V，W取代的含有Q2的杂芳基，V，含有Q2和Q3的W取代的双环杂芳基和I，含有Q 2，Q 3，Q 4的W取代的二氢化茚，其中Q1，Q2，Q3和Q4各自独立地选自 来自N，C和S; G，J，I，V，W各自独立地为氢，被卤素取代或不被取代的C 1-6烷基，C 3-6环烷基，C 1-6烷氧基，羟基，卤素，氰基，硝基，砜磺酰胺，羟基羰基 取代或未被卤素取代的C 1-6烷氧基羰基，C 6-8芳基，C 5-8杂芳基，其含有一个或两个选自N，O和S的原子，或C 2-9杂芳氧基取代或未取代的 通过卤素，其含有一个或两个选自N，O和S的原子。式1的化合物通过在碱和催化剂存在下在溶剂中使式2化合物与式3化合物反应来合成。 在式2和3中，R，X，Y，Z，A，Q 1，G和J与上述相同。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
    • 8. 发明公开
      KR1020100053458A 멜라노코틴 수용체의 항진제 有权
    • 멜라노코틴 수용체의 항진제
    • 梅兰康汀受体激动剂
    • KR1020100053458A
    • 2010-05-20
    • KR1020090108283
    • 2009-11-10
    • 주식회사 엘지생명과학
    • 이구 , 이상대 , 문상필 , 안인애 , 최성필 , 이현호 , 심동섭 , 정수용 , 이현민
    • C07D403/14 , C07D401/14 , A61K31/4025 , A61P3/10
    • C07D417/14 , A61K31/4025 , A61K31/496 , C07D207/16 , C07D401/14 , C07D403/06 , C07D405/14 , C07D409/14
    • PURPOSE: A compound having excellent activity to melanocortin is provided to apply to functional agonist of the melanocortin receptor and to prevent and treat obesity, electrile dysfunction, diabetes, or inflammation. CONSTITUTION: A composition having excellent activity to melanocortin receptor is denoted by chemical formula 1. The compound of chemical formula 1 is obtained by amide-coupling a compound of chemical formula 2 with a compound of chemical formula 3. A method for preparing the compound of chemical formula 1 comprises: a step of deprotecting a compound of chemical formula 1' or 2'; a step of performing reductive amine reaction of oxo substituent with C1-C2 alkyl, C3-C7 cycloalkyl, or heterocycle; or a step of performing coupling reaction with arylhalide or hetero arylhalide. The composition contains pharmaceutically acceptable carrier, and the compound of chemical formula 1, pharmaceutically acceptable salt, or isomer. The composition is used for treating obesity, electrile dysfunction, diabetes, or inflammation.
    • 目的：提供对黑皮质素具有优异活性的化合物以适用于黑皮质素受体的功能性激动剂并预防和治疗肥胖症，电功能障碍，糖尿病或炎症。 构成：化学式1表示对黑皮质素受体具有优异活性的组合物。化学式1的化合物通过化学式2的化合物与化学式3的化合物酰胺偶联而获得。一种制备化合物 化学式1包括：使化学式1'或2'的化合物脱保护的步骤; 氧代取代基与C 1 -C 2烷基，C 3 -C 7环烷基或杂环进行还原胺反应的步骤; 或与芳基卤或异芳基卤化物进行偶联反应的步骤。 组合物含有药学上可接受的载体，化学式1的化合物，药学上可接受的盐或异构体。 该组合物用于治疗肥胖症，电疗功能障碍，糖尿病或炎症。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
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