Abstract:
PURPOSE: A compound having anti-viral activity and an extract of Chrysanthemum morifolium comprising the same are provided, which compound and Chrysanthemum morifolium extract are useful for treatment of diseases caused by HIV(Human immunodeficiency virus) or alleviation of symptom of the diseases. CONSTITUTION: The compound having anti-viral activity represented by formula (1) and pharmaceutically acceptable salts thereof are provided. The extract of Chrysanthemum morifolium having anti-viral activity is obtained by using water and organic solvent, wherein the organic solvent is selected from alcohol, ethyl acetate, dichloromethane and acetone; the extract of Chrysanthemum morifolium comprises compounds of formula (1) to formula (5) as active components wherein R1 is hydrogen, hydroxyl, glucose or rhamnos, R2 is hydrogen or hydroxyl and R is a compound 8.
Abstract:
PURPOSE: Provided are a compound having an antioxidant or antivirus activity or its pharmaceutically acceptable salt, Chrysanthemum indicum extract containing the compound, a separation method of the compound from the extract, a pharmaceutical composition containing the compound for treating or preventing HIV or the disease due to the oxidation of cell components, an antioxidant food additive containing the compound and an antioxidant cosmetic containing the compound. CONSTITUTION: The compound is represented by the formula 1, wherein R1 and R2 are H or a caffeoyl group; and R3 is a specific caffeoyl group represented by the formula (a). The Chrysanthemum indicum extract is extracted by using water and an organic solvent. Preferably the organic solvent is at least one selected from the group consisting of an alcohol, ethyl acetate, dichloromethane and acetone. The compound of the formula 1 is separated from the extract by carrying out the column chromatography using a filler selected from the group consisting of silica gel, Sephadex, RP-18, polyamide, Toyopearl and XAD resin.
Abstract:
PURPOSE: A compound capable of inhibiting HIV protease with a 6-hydroxy-1,3-dioxin-4-on ring and its producing method are provided, therefore the compound can be useful for the prevention and treatment of HIV. CONSTITUTION: The compound capable of inhibiting HIV protease has a 6-hydroxy-1,3-dioxin-4-on ring represented by formula(I), wherein R1 is methyl, ethyl, propyl, isopropyl, butyl, isobutyl or t-butyl; R2 is methyl, ethyl, propyl, isopropyl, butyl, isobutyl, t-butyl, benzene, 4-aminophenyl, 4-cyanophenyl, 4-nitro, phenyl, phenethyl, 2-(4-pyridyl)ethyl, 4-cyanobenzensulfonamido, 4-aminobenzensulfonamido, 4-nitrobenzensulfonamido, 4-fluoromethylbenzensulfonamido, 5-cyanopyridinesulfonamido, 5-aminopyridinesulfonamido, 5-nitropyridineamido or 5-fluoromethylpyridinesulfonamido; R3 is methyl, ethyl, propyl, isopropyl, cyclopropyl, butyl, isobutyl, cyclobutyl or t-butyl; and R4 is phenyl, 4-aminophenyl, 4-cyanophenyl, 4-nitrophenyl, 2-pyridine, 5-cyanopyridine, 5-aminopyridine, 5-nitropyridine, 5-trifluoromethylpyridine or 1-methyl-4-imidazol.
Abstract:
PURPOSE: Provided are 4-(phenylamino)-(1,4)dioxano(2,3-Q)quinazoline inhibiting the activity of tyrosine kinase which is a receptor of the epidermic growth factor and used for prevention and treatment of cancers, its pharmaceutically acceptable salts, hydrates, solvates and a preparation method thereof. The compounds. CONSTITUTION: 4-(phenylamino)-(1,4)dioxano(2,3-Q)quinazoline is represented by the formula (I) and its preparation method comprises mixing one equivalent of quinazoline derivative of the formula(II) with two equivalent of substituted aniline of the formula(III); and adding HCl then allowing them to react at 20-80 deg.C. In the above formulae, R1 is hydrogen, halogen, hydroxy, C1-6 alkyl, alkoxy, thioalkoxy, and alkoxyamino, C3-6 cycloalkyl, cycloalkoxy and thioalkoxy, (aryl or heteroaryl)oxy, thio(aryl or heteroaryl)oxy, nitro, amino, N-mono(C1-6) alkylamino, N,N-di(C1-6) alkylamino,formamido, iodo, acetiodo, hydroxyamino, hydrazino, trifluoromethyl, trifluroro- methoxy, alkenyl, alkynyl, aryl or heterocycle group; R2 and R3 are the same or different and represent -(CH2)m-R4 wherein m is 0 or 1; R4 is hydrogen, halogen, C1-6 hydroxy, C1-6 alkyl, alkoxy, thioalkoxy,and alkoxyamino, C3-6 cycloalkyl, cycloalkoxy and thioalkoxy, (aryl or heteroaryl)oxy, thio(aryl or heteroaryl)oxy, nitro, amino, N-mono(C1-6) alkylamino, N,N-di(C1-6) alkylamino,formamido, iodo, acetiodo, hydroxyamino, hydrazino, trifluoro-methyl, trifluroro methoxy, alkenyl, alkynyl, aryl or heterocycle, carboxy, alkoxycarbonyl, amido, N-monoalkyl (C1-6) amido, N,N-dialkyl(C1-6)amido, thioamido, N,N-dialkyl(C1-6)thioamido, guanidino, ureido, C1-6sulfaido, C1-6alkylsulfonyl, morphorino, 4-C1-6alkylpiperidino, mono(hydroxy(C1-6)alkyl)amino, mono(pyrrolidine (C1-6)alkyl)amino, di(pyrrolidine (C1-6) alkyl)amino or -N(R5)(CHR6R7), wherein R5 is hydrogen or C1-6 alkyl; R6 is (CH2)nOH, wherein n is an integer 1-4; R7 is hydrogen, C1-5 alkyl, hydroxyalkyl, thiohydroxyalkyl, phenyl C1-5 alkyl, 4-hydroxyphenyl (C1-5) alkyl or heteroaryl alkyl group; and n is 1,2 or 3.
Abstract:
PURPOSE: A compound capable of inhibiting HIV protease with a 6-hydroxy-1,3-dioxin-4-on ring and its producing method are provided, therefore the compound can be useful for the prevention and treatment of HIV. CONSTITUTION: The compound capable of inhibiting HIV protease has a 6-hydroxy-1,3-dioxin-4-on ring represented by formula(I), wherein R1 is methyl, ethyl, propyl, isopropyl, butyl, isobutyl or t-butyl; R2 is methyl, ethyl, propyl, isopropyl, butyl, isobutyl, t-butyl, benzene, 4-aminophenyl, 4-cyanophenyl, 4-nitro, phenyl, phenethyl, 2-(4-pyridyl)ethyl, 4-cyanobenzensulfonamido, 4-aminobenzensulfonamido, 4-nitrobenzensulfonamido, 4-fluoromethylbenzensulfonamido, 5-cyanopyridinesulfonamido, 5-aminopyridinesulfonamido, 5-nitropyridineamido or 5-fluoromethylpyridinesulfonamido; R3 is methyl, ethyl, propyl, isopropyl, cyclopropyl, butyl, isobutyl, cyclobutyl or t-butyl; and R4 is phenyl, 4-aminophenyl, 4-cyanophenyl, 4-nitrophenyl, 2-pyridine, 5-cyanopyridine, 5-aminopyridine, 5-nitropyridine, 5-trifluoromethylpyridine or 1-methyl-4-imidazol.
Abstract translation:目的:提供能够抑制HIV-蛋白酶与6-羟基-1,3-二恶英-4-环的化合物及其制备方法,因此该化合物可用于预防和治疗HIV。 构成:能够抑制HIV蛋白酶的化合物具有由式(I)表示的6-羟基-1,3-二恶英-4-环,其中R 1是甲基,乙基,丙基,异丙基,丁基,异丁基或叔丁基 ; R 2是甲基,乙基,丙基,异丙基,丁基,异丁基,叔丁基,苯,4-氨基苯基,4-氰基苯基,4-硝基,苯基,苯乙基,2-(4-吡啶基)乙基,4-氰基苯磺酰胺基, 4-氨基苯磺酰胺基,4-硝基苯磺酰胺基,4-氟甲基苯磺酰胺基,5-氰基吡啶磺酰胺基,5-氨基吡啶磺酰胺基,5-硝基吡啶酰胺基或5-氟甲基吡啶磺酰胺基; 乙基,丙基,异丙基,环丙基,丁基,异丁基,环丁基或叔丁基; R4是苯基,4-氨基苯基,4-氰基苯基,4-硝基苯基,2-吡啶,5-氰基吡啶,5-氨基吡啶,5-硝基吡啶,5-三氟甲基吡啶或1-甲基-4-咪唑。
Abstract:
본 발명은 신규한 암모니오프로페닐세팔로스포린 화합물 및 그 제조방법에 관한 것이다. 더욱 상세히 말하면, 일반식(II)로 표시되는 화합물과 일반식(III)으로 표시되는 3급 아민 화합물 P를 반응 시킨후 아민보호기 및 카복시 보호기를 제거함으로써 광범위한 항균 범위와 우수한 항균력을 가지는 항생제 임. (I) 일반식(I)에 있어서, P는 하나의 질소를 가지는 동시에 한 개 또는 두 개의 히드록실기를 가지는 비고리형 아민 또는 헤테로시클릭아민으로서 메조-3,4-디히드록시-1-메틸피롤리딘, (3S,4S)-3,4-디히드록시-1-메틸피롤리딘, (3R,4R)-3,4,-디히드록시-1-메틸피롤리딘, (2S,4R)-4-히드록시-1-메틸-2-피롤리딘메탄올, N-메틸디에탄올아민, 3,4-시스-디히드록시-1-메틸피페리딘, 3,4-트란스-디히드록시-1-메틸피롤리딘, 4-히드록시-1-메틸피페리딘, 2-히드록시메틸-1-메틸피페리딘 또는 트로핀을 표시한다. Q는 CII또는 N이다. 또한 이들 세팔로스포린 화합물들의 약학적으로 허용되는 염이 포함됨.
일반식(II)에 있어서, Q는 CII또는 N이며, R 1 은 트리페닐메틸 또는 수소이며, R 2 는 p-메톡시벤질 또는 디페닐메틸이며, X는 할로겐 화합물로서 요오드를 표시함.
일반식(III)에 있어서, P는 메조-3,4-디히드록시-1-메틸피롤리딘, (3S,4S)-3,4-디히드록시-1-메틸피롤리딘, (3R,4R)-3,4-디히드록시-1-메틸피롤리딘, (2S,4R)-4-히드록시-1-메틸-2-피롤리딘메탄올, N-메틸디에탄올아민, 3,4-시스-디히드록시-1-메틸피레리딘, 3,4-트란스-디히드록시-1-메틸피롤리딘, 4-히드록시-1-메틸피페리딘, 2-히드록시메틸-1-메틸피페리딘 또는 트로핀을 표시함.
Abstract:
본 발명은 신규한 암모니오프로페닐세팔로스포린 화합물 및 그 제조방법에 관한 것이다. 더욱 상세히 말하면, 일반식(II)로 표시되는 화합물과 일반식(III)으로 표시되는 3급 아민 화합물 P를 반응시긴 후 아민 보호기 및 카복시 보호기를 제거함으로써 광범위한 항균 범위와 우수한 항균력을 가지는 항생제 임.
일반식(I)에 있어서, P는 하나의 질소를 가지는 동시에 한개 또는 두개의 히드록실기를 가지는 비고리형 아민 또는 헤테로시클릭아민으로서 메조-3,4-디히드록시-1-메틸피롤리딘,(3S,4S)-3,4-디히드록시 -1-메틸피롤리딘, (3R,4R)-3,4-디히드록시 -1-메틸피롤리딘,(2S,4R)-4-히 드록시 -1-메 틸-2-피 롤리 딘메 탄올, N-메 틸 디 에 탄올아민,3,4- 시 스 - 디히드록시-1-메 틸 피 페 리 딘, 3,4-트 란 스 - 디히드록시-1- 메 틸 피 롤리딘, 4-히드록시-1-메틸피페리딘,2-히드록시메틸-1-메틸피페리딘 또는 트로핀을 표시한다.Q는 CH 또는 N이다. 또한, 이들 세팔로 스포린 화합물들의 약학적으로 허용되는 염이 포함 됨.
일반식(II)에 있어서, Q는 CH 또는 N이며, R 1 은 트리페닐메틸 또는 수소이며, R 2 는 p-메톡시벤질 또는 디페닐메틸이며, X는 할로겐 화합물로서 요오드를 표시 함.