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    • 3. 发明公开
    • 세팔로스포린산 유도체의 제조방법
    • 制备碳氢化合物酸衍生物的方法
    • KR1020030021629A
    • 2003-03-15
    • KR1020010054986
    • 2001-09-07
    • 주식회사 엘지생명과학
    • 김영순여재홍우영민허태호오희명
    • C07D501/16
    • PURPOSE: A process for preparing cephalosporanic acid derivative is provided, thereby high quality cephalosporanic derivatives can be simply prepared. CONSTITUTION: The process for preparing cephalosporanic acid derivative comprises reacting 7-aminocephalosporanic acid represented by formula(2) with sodium thiofuroate represented by formula(3) in a solvent in the presence of organic base to prepare 3-furoylthiomethyl-7-amino-3-cephem-4-carboxylic acid represented by formula(1), wherein the organic base is tertiary alkylamine; the tertiary alkylamine is triethylamine, tri-n-butylamine, diisopropylethylamine, N,N-dimethylaniline or pyridine; the amount of the organic base used is 0.3 to 1.5 equivalent based on sodium thiofuroate of formula(3); the solvent is water or a mixture of water and organic solvent; and the organic solvent is acetonitrile, ethylacetate, acetone, methylene chloride, tetrahydro furan or chloroform.
    • 目的:提供一种制备头孢菌酸衍生物的方法,从而可以简单地制备高质量的头孢菌素衍生物。 构成:制备头孢菌酸衍生物的方法包括使式(2)表示的7-氨基头孢烷酸与式(3)表示的硫代呋喃硫酸钠在有机碱存在下,在溶剂中反应,制备3-糠基硫甲基-7-氨基-3 由式(1)表示的头孢烯-4-羧酸,其中有机碱是叔烷基胺; 叔烷基胺是三乙胺,三正丁胺,二异丙基乙胺,N,N-二甲基苯胺或吡啶; 所使用的有机碱的用量相对于式(3)的硫代呋喃硫酸钠为0.3〜1.5当量; 溶剂是水或水和有机溶剂的混合物; 有机溶剂为乙腈,乙酸乙酯,丙酮,二氯甲烷,四氢呋喃或氯仿。
    • 8. 发明公开
    • 이소옥사졸린 구조를 갖는 캐스파제 저해제
    • CASPASE抑制剂含有具有由CASPAS引起的治疗或缓解症状的改善活性的异丙嗪环,包括炎症或病毒性
    • KR1020050022364A
    • 2005-03-07
    • KR1020040066726
    • 2004-08-24
    • 주식회사 엘지생명과학
    • 장혜경오영수박철원장용진박태교김성섭김민정박미정박정규박희동민경식이태수이상균김수헌정희경이선화김화동김애리박기숙신현익최형욱이규웅이재훈허태호김호준권태식
    • C07D261/04C07D413/12
    • C07D261/04C07D413/04C07D413/12C07D413/14
    • PURPOSE: Caspase inhibitors containing an isoxazoline ring are provided, which caspase inhibitors have improved activity of treating or alleviating sympthoms caused by the caspase including inflammation or apoptosis. CONSTITUTION: The caspase inhibitors containing an isoxazoline ring, represented by formula (1), salts thereof or stereochemical isomers thereof are provided, wherein R is H, simple alkyl chain(-SAC), simple cycloalkyl chain(-SCAC), aryl(-Ar) or aryl substituted simple alkyl chain(-SAC-Ar); R1 is -CH2COOH, -CH2COOR3(R3 = SAC) or -CH2CONHSO2R4(R4 = SAC); R2 is H, -SAC, -Ar or -(CH2)nOR7(R7 = -SAC, -SCAC, -Ar or -SAC-Ar, and n = 1 or 2); A is -(CH2)n- (n = 0-4), -O-(CH2)n- (n = 0-4) or -NR 9-(CH2)n-(n = 0-4, and R9 is -SAC, -SCAC, -Ar or -SAC-Ar); B is H, -SAC, -SCAC, -Ar or -SAC-Ar; -R-R1 is -(CH2)n-, -(CH2)n-O-(CH 2)m- or -(CH2)n-NR10-(CH2)m-(n+m
    • 目的:提供含有异恶唑啉环的胱天蛋白酶抑制剂,其中胱天蛋白酶抑制剂具有改善的治疗或减轻由胱天蛋白酶引起的症状(包括炎症或细胞凋亡)的活性。 提供含有式(1)表示的异恶唑啉环的胱天蛋白酶抑制剂,其盐或其立体化学异构体,其中R为H,简单烷基链(-SAC),简单环烷基链(-SCAC),芳基( - Ar)或芳基取代的简单烷基链(-SAC-Ar); R1是-CH2COOH,-CH2COOR3(R3 = SAC)或-CH2CONHSO2R4(R4 = SAC); R2是H,-SAC,-Ar或 - (CH2)nOR7(R7 = -SAC,-SCAC,-Ar或-SAC-Ar,n = 1或2)。 A是 - (CH 2)n - (n = 0-4),-O-(CH 2)n - (n = 0-4)或-NR 9 - (CH 2)n - (n = 0-4, 是-SAC,-SCAC,-Ar或-SAC-Ar); B是H,-SAC,-SCAC,-Ar或-SAC-Ar; -R-R 1是 - (CH 2)n - , - (CH 2)n O-(CH 2)m-或 - (CH 2)n -NR 10 - (CH 2)m - (n + m <9,R 10 = -SAC ,-SCAC,-Ar,-SAC-Ar,-C(= O)-SAC,-C(= O)-SSCAC,-C(= O)-Ar或-C(= O)-SAC-Ar) ; X是-C(= O)CH 2 O 2,-C(= O)CH 2 OC(= O)Ar或-COCH 2 -W(W是-N 2,-F,-Cl,-Br,-I,-NR 15 R 16(R 15和 R 16是独立的-SAC,-SCAC,-Ar或-SAC-Ar)或形成3至6元环饱和或不饱和的环状基团或-SR 17(R 17 = -SAC,-SCAC,-Ar或-SAC- Ar); Y是H,-OH,-OR 18(R 18 = -SAC,-SCAC),-C(= O)R 19(R 19 = -H,-SAC,-SCAC),-F,-Cl,-Br ,-I,-CN,-NC,-N3,-CO2H,CF3,-CO2R20(R20 = -SAC,-SCAC),-C(= O)NHR21(R21 = -SAC,-SCAC)或-C = O)NR22R23(R22和R23独立为-SAC,-SCAC,-Ar或-SAC-Ar)); 和R 24是H,-SAC,-SAC-Ar或-Ar。