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    • 2. 发明公开
    • 멜라노코틴 수용체의 항진제
    • 梅兰康汀受体激动剂
    • KR1020080007046A
    • 2008-01-17
    • KR1020060066598
    • 2006-07-14
    • 주식회사 엘지생명과학
    • 안인애최성필이상협이상대신미숙이구최덕영심동섭임현주박억이현민정수용김연화
    • C07D403/06C07D405/14C07D417/14
    • A novel compound is provided which is an excellent selective agonist of the human melanocortin-4 receptor(MC-4R), thereby being useful for preventing and treating obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction, and inflammation. A compound as a melanocortin receptor agonist is represented by the formula(1), wherein R^1 is H, C1-10 alkyl, C3-7 cycloalkyl, C1-6 alkylcarbonyl, carbamoyl, thiocarbamoyl, C1-4 alkyl carbamoyl, or C1-4 alkylthiocarbamoyl; R^2 is a C6-10 aryl which is mono- or di-substituted or non-substituted by a substituent selected from the group consisting of halogen, hydroxy, C1-4 alkyl and C1-4 alkoxy; R^3 is C1-6 alkyl, C3-7 cycloalkyl, C2-6 alkenyl, monocyclic heterocycle, monocyclic heteroaryl, carboxy, C1-4 alkyloxycarbonyl, C1-4 alkylcarbonyl, cyano, carbamoyl, thiocarbamoyl, C1-4 alkylcarbamoyl, (C1-4 alkyl)(C1-4 alkyl)carbamoyl, C1-4 alkylthiocarbamoyl or (C1-4 alkyl)(C1-4 alkyl)thiocarbamoyl; R^4 is C3-8 cycloalkyl, C6-10 aryl or heterocycle; and R^5 is C1-6 alkyl, C2-6 alkenyl, C3-6 cycloalkyl, heteroaryl or heterocycle. A method for preparing the compound of the formula(1) comprises a step of amide-coupling a compound represented by the formula(2) with a compound represented by the formula(3). A functional agonist composition of melanocortin receptor comprises a pharmaceutically acceptable carrier, the compound of the formula(1), a pharmaceutically acceptable salt thereof or an isomer thereof.
    • 提供了一种新的化合物,它是人类黑皮质素-4受体(MC-4R)的优异选择性激动剂,因此可用于预防和治疗肥胖,糖尿病,性功能障碍,包括勃起功能障碍和女性性功能障碍以及炎症。 作为黑皮质素受体激动剂的化合物由式(1)表示,其中R 1是H,C 1-10烷基,C 3-7环烷基,C 1-6烷基羰基,氨基甲酰基,硫代氨基甲酰基,C 1-4烷基氨基甲酰基或C 1 -4-烷硫基氨基甲酰基; R 2是被选自卤素,羟基,C 1-4烷基和C 1-4烷氧基的取代基单取代或未被取代或未取代的C6-10芳基; R 3是C 1-6烷基,C 3-7环烷基,C 2-6烯基,单环杂环,单环杂芳基,羧基,C 1-4烷氧基羰基,C 1-4烷基羰基,氰基,氨基甲酰基,硫代氨基甲酰基,C 1-4烷基氨基甲酰基, 1-4烷基)(C 1-4烷基)氨基甲酰基,C 1-4烷硫基氨基甲酰基或(C 1-4烷基)(C 1-4烷基)硫代氨基甲酰基; R 4是C 3-8环烷基,C 6-10芳基或杂环; R 5为C 1-6烷基,C 2-6烯基,C 3-6环烷基,杂芳基或杂环。 制备式(1)化合物的方法包括将由式(2)表示的化合物与式(3)表示的化合物酰胺偶联的步骤。 黑皮质素受体的功能性激动剂组合物包含药学上可接受的载体,式(1)的化合物,其药学上可接受的盐或其异构体。
    • 5. 发明公开
    • 멜라노코틴 수용체의 항진제
    • 梅兰康汀受体激动剂
    • KR1020080007051A
    • 2008-01-17
    • KR1020060066610
    • 2006-07-14
    • 주식회사 엘지생명과학
    • 최성필안인애이상협이상대신미숙이구최덕영심동섭임현주윤민경정수용이정애하용화김영관
    • C07D403/06C07D405/14C07D417/14C07D403/14
    • A novel compound is provided to be effective as melanocortin receptor agonists and particularly effective as selective agonists of melanocortin-4 receptor(MC-4R), thereby being useful for preventing and treating obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction, and inflammation. A compound as a melanocortin receptor agonist is represented by the formula(1), wherein R^1 is H, amidino, C1-4 alkylamidino, C1-4 alkanoylamidino, C1-10 alkyl, C3-7 cycloalkyl, C6-10 aryl, heterocycle, heteroaryl, C1-6 alkylcarbonyl, C3-7 cycloalkylcarbonyl, C1-4 alkoxycarbonyl, (C6-10)-aryl-(C1-4)alkoxycarbonyl, SO2-(C1-4)alkyl, C(O)N(R^5)(R^6) or C(S)N(R^5)(R^6)(each R^5 and R^6 is independently H, C1-6 alkyl or C3-7 cycloalkyl); R^2 is C6-10 aryl which may be mono- or di-substituted by a substituent selected from the group consisting of halogen, hydroxy, C1-4 alkyl and C1-4 alkoxy; R^3 is C3-8 cycloalkyl, heterocycle, C6-10 aryl or heteroaryl; and R^4 is H, C1-6 alkyl, C(O)R^7, (CH2)p-(C6-10)aryl, (CH2)p-heterparyl or (CH2)p-(C3-8)cycloalkyl(where p is 1 or 2, and R^7 is C1-10 alkyl, C2-6 alkenyl, C3-8 cycloalkyl, C3-8 cycloalkenyl, amino, C1-4 alkylamino, (C1-4)alkyl(C1-4 alkyl)amino, SO2-(C1-7)alkyl, C6-10 aryl, heteroaryl or heterocycle). A method for preparing the compound of the formula(1) comprises a step of amide-coupling a compound represented by the formula(2) with a compound represented by the formula(3). A functional agonist composition of melanocortin receptor comprises a pharmaceutically acceptable carrier and the compound of the formula(1), a pharmaceutically acceptable salt thereof or an isomer thereof.
    • 提供新的化合物作为黑皮质素受体激动剂是有效的,并且特别有效作为黑皮质素-4受体(MC-4R)的选择性激动剂,因此可用于预防和治疗肥胖症,糖尿病,性功能障碍,包括勃起功能障碍和女性性功能障碍 ,和炎症。 作为黑皮质素受体激动剂的化合物由式(1)表示,其中R 1是H,脒基,C 1-4烷基脒基,C 1-4烷酰基脒基,C 1-10烷基,C 3-7环烷基,C 6-10芳基, 杂环,杂芳基,C 1-6烷基羰基,C 3-7环烷基羰基,C 1-4烷氧基羰基,(C 6-10) - 芳基 - (C 1-4)烷氧基羰基,SO 2 - (C 1-4)烷基,C(O) (R ^ 6)或C(S)N(R 5)(R 6)(每个R 5和R 6独立地是H,C 1-6烷基或C 3-7环烷基); R 2是可以被选自卤素,羟基,C 1-4烷基和C 1-4烷氧基的取代基单取代或二取代的C 6-10芳基; R 3是C 3-8环烷基,杂环,C 6-10芳基或杂芳基; 且R 4为H,C 1-6烷基,C(O)R 9,(CH 2)p - (C 6-10)芳基,(CH 2)p - 杂芳基或(CH 2) (其中p为1或2,R 7为C 1-10烷基,C 2-6烯基,C 3-8环烷基,C 3-8环烯基,氨基,C 1-4烷基氨基,(C 1-4)烷基(C 1-4) 烷基)氨基,SO 2 - (C 1-7)烷基,C 6-10芳基,杂芳基或杂环)。 制备式(1)化合物的方法包括将由式(2)表示的化合物与式(3)表示的化合物酰胺偶联的步骤。 黑皮质素受体的功能性激动剂组合物包含药学上可接受的载体和式(1)的化合物,其药学上可接受的盐或其异构体。
    • 6. 发明公开
    • 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
    • 윤주용김원섭이현호임재홍이석원윤승현송정욱김종엽최성필윤하식조양래
    • 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。
    • 7. 发明公开
    • 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
    • 윤승현김원섭이현호임재홍윤주용김종엽송정욱이석원최성필바실리아티모프윤하식조양래
    • 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。
    • 10. 发明公开
    • C형 간염 바이러스의 억제제
    • HEPATITIS C病毒抑制剂用于预防和治疗丙型肝炎病毒感染
    • KR1020040107367A
    • 2004-12-20
    • KR1020040040967
    • 2004-06-04
    • 주식회사 엘지생명과학
    • 김원섭윤주용임재홍송정욱성이택강승완송호영김용주최성필김종엽조영규김창명박지현
    • C07D239/22A61K31/505
    • C07D239/22C07D401/12C07D403/12C07D405/12C07D409/12C07D409/14C07D413/12C07D417/12C07D417/14C07D495/04C07D513/04
    • PURPOSE: A novel hepatitis C virus inhibitor is provided which is useful for the prevention and treatment of hepatitis C virus infection. Also, provided are a preparation method thereof and a composition for the prevention and treatment of hepatitis C virus containing the same. CONSTITUTION: The hepatitis C virus inhibitor represented by the formula(1), or pharmaceutically acceptable salts, hydrates, solvates and tautomers thereof are provided, wherein X is O or S; R1 is hydrogen, alkyl which is optionally substituted with 1 to 3 substituents selected from halogen, alkoxy, alkoxycarbonyl, hydroxy, carboxy and aryl, alkoxy, alkoxycarbonyl optionally substituted with aryl, or aryl; R2 and R3 are independently hydrogen, alkyl which is optionally substituted with 1 to 3 substituents selected from halogen, hydroxy, alkoxy, alkylsulfonyl and aralkyloxy, alkoxycarbonyl, alkylsulfonylalkyl, aryl or heteroaryl; R5 is alkyl optionally substituted amino, alkylamino which is optionally substituted with alkylcarbonylamino, alkylcarbonyloxy or dialkylamino; alkoxy which is optionally substituted with 1 to 3 substituents selected from benzoyloxy, alkoxycarbonyl, alkyl, alkylsulfonyl, alkylcarbonylthio, alkoxycarbonylamino, and alkyl and oxo, and is optionally substituted with 1 to 3 substituents of heterocycle containing a double bond, aryl optionally substituted carboxy, or aralkyl optionally substituted with alkylcarbonyloxy; R6 is alkyl; R4 is alkyl which is optionally substituted with 1 to 3 substituents selected from alkoxy optionally substituted with heteroaryl, carboxy, alkylthio, alkoxycarbonyl, alkylaminocarbonyl, biphenyl, aryl, aryloxy, aralkyloxy, alkylaryl, amino optionally substituted with alkyl or alkylaryl, cycloalkyl, cycloalkyloxy, alkylaryl sulfonyl, heteroaryl optionally substituted with halogen and heteroarylthio, alkenyl which is optionally substituted with 1 to 3 substituents selected from halogen, aryl and heteroaryl, alkynyl which is optionally substituted with 1 to 3 substituents selected from alkoxy, alkenyloxy, alkynyloxy, aralkyloxy, aryl and heteroaryl, -(CH2)N-cycloalkyl, -(CH2)N-cycloalkenyl, -(CH2)N-aryl, -(CH2)N-heterocycle or -(CH2)N-heteroaryl in which N is an integer of 1 to 10 and -CH2- group is optionally substituted with halogen when N is not 0.
    • 目的:提供一种新型丙型肝炎病毒抑制剂,可用于预防和治疗丙型肝炎病毒感染。 此外,还提供了其预防和治疗含有该丙型肝炎病毒的丙型肝炎病毒的制备方法和组合物。 构成:提供由式(1)表示的丙型肝炎病毒抑制剂或其药学上可接受的盐,水合物,溶剂化物和互变异构体,其中X为O或S; R 1为氢,任选被1至3个选自卤素,烷氧基,烷氧基羰基,羟基,羧基和芳基的取代基取代的烷基,烷氧基,任选被芳基取代的烷氧羰基或芳基; R2和R3独立地是氢,任选被1至3个选自卤素,羟基,烷氧基,烷基磺酰基和芳烷氧基,烷氧基羰基,烷基磺酰基烷基,芳基或杂芳基的取代基取代的烷基; R5是烷基任选取代的氨基,任选被烷基羰基氨基,烷基羰基氧基或二烷基氨基取代的烷基氨基; 任选被1至3个选自苯甲酰氧基,烷氧基羰基,烷基,烷基磺酰基,烷基羰硫基,烷氧基羰基氨基和烷基和氧代的取代基取代的烷氧基,并且任选被1至3个含有双键的杂环取代基, 或任选被烷基羰基氧基取代的芳烷基; R6是烷基; 羧基,烷硫基,烷氧基羰基,烷基氨基羰基,联苯基,芳基,芳氧基,芳烷氧基,烷基芳基,任选被烷基或烷基芳基取代的氨基,环烷基,环烷基氧基, 烷基芳基磺酰基,任选被卤素和杂芳硫基取代的杂芳基,任选被1至3个选自卤素,芳基和杂芳基的取代基取代的烯基,任选被1至3个选自烷氧基,烯氧基,炔氧基,芳烷氧基,芳基 和(CH 2)N-环烯基, - (CH 2)N - 环烯基, - (CH 2)N - 芳基, - (CH 2)N - 杂环或 - (CH 2) 当N不为0时,-CH 2 - 基团任选被卤素取代。