-
公开(公告)号：KR1019950000710A
公开(公告)日：1995-01-03
申请号：KR1019930010442
申请日：1993-06-09
Applicant: 한국과학기술연구원
IPC: C07D501/46
Abstract: 본 발명에서는 다음 일반식(Ⅰ)으로 표시되는 세팔로스포린 화합물 및 그의 제조방법이 제공된다;
상기식에서 Q는 질소 혹은 CH이고, P는 하나의 질소를 가지는 동시에 한개 또는 두개의 히드록실기를 가지는 비고리형 아민 또는 헤테로시클릭아민으로서 N-메틸-비스(2-히드록시에틸)아민, 라세믹-3,4-트란스-디히드록시-1-메틸피롤리딘, (3S,4S)-3,4-디히드록시-1-메틸피롤리딘, (3R,4R)-3,4-디히드록시-1-메틸피롤리딘, 메조-3,4-디히드록시-1-메틸피롤리딘, (2S,4R)-4-히드록시-1-메틸-2-피롤리딘메탄올, 3,4-시스-디히드록시-1-메틸피페리딘, 3,4-트란스-디히드록시-1-메틸피페리딘, 또는 트로핀이다.
본 발명의 세팔로스포린 화합물은 세프타지딤보다 더 광범위하며 월등한 향균력을 나타낸다.-
公开(公告)号：KR100033774B1
公开(公告)日：1990-06-15
申请号：KR1019860008538
申请日：1986-10-11
Applicant: 한국과학기술연구원
IPC: C07D231/10
-
-
公开(公告)号：KR1020030088906A
公开(公告)日：2003-11-21
申请号：KR1020020026650
申请日：2002-05-15
Applicant: 한국과학기술연구원
IPC: A61K31/353
Abstract: PURPOSE: Provided is a composition for treating sexual dysfunction which contains a flavonoid compound represented by the formula 1 or 2, and an extract of Sophora flavescens containing them, as active ingredients. The composition inhibits on cGMP-PDE5 and is thus useful for the prevention and treatment of sexual disfunction. CONSTITUTION: A composition for treating sexual dysfunction is characterized by containing, as active ingredients, a flavonoid compound represented by the formula 1 or 2, wherein R1 is a unsubstituted or hydroxy group-substituted linear or branched alkenyl group; R2 is hydrogen, hydroxy or C1-C3 alkoxy; R3 and R4 are individually hydrogen or a hydroxy group; and a dotted line represents single or double bond, and its pharmaceutically acceptable salt, hydrates, solvate, isomer or their mixture.
Abstract translation: 目的：提供一种用于治疗性功能障碍的组合物，其含有由式1或2表示的类黄酮化合物和含有它们的苦参皂甙提取物作为活性成分。 该组合物抑制cGMP-PDE5，因此可用于预防和治疗性功能障碍。 构成：用于治疗性功能障碍的组合物的特征在于，含有作为活性成分的由式1或2表示的类黄酮化合物，其中R1是未取代的或羟基取代的直链或支链烯基; R2是氢，羟基或C1-C3烷氧基; R3和R4分别是氢或羟基; 虚线表示单键或双键，以及其药学上可接受的盐，水合物，溶剂合物，异构体或它们的混合物。
-
公开(公告)号：KR100386310B1
公开(公告)日：2003-06-02
申请号：KR1020000041969
申请日：2000-07-21
Applicant: 한국과학기술연구원
IPC: A61K36/855 , A61P31/18 , A61P37/00
Abstract: PURPOSE: An anti-HIV agent containing an alcohol extract of Clerodendron trichotomum and a purified compound separated therefrom an as effective component, in particular an inhibitor for HIV integrase is provided, which has no drug resistance or side effects as defects of a reverse transciptase inhibitor and a protease inhibitor. CONSTITUTION: An alcohol extract of Clerodendron trichotomum having a formula 1 has an anti-HIV activity, in particular an inhibiting activity against HIV integrase. In formula, R1 is H or methyl, R2 is H, caffeoyl, or feruloyl, R3 is H, caffeoyl or feruloyl. For an example, 4.8kg Clerodendron trichotomum is extracted in methanol at room temperature and fractionated into dichloromethane and water. The fraction is subjected to column chromatography with sephadex LH-20 and then silica gel column chromatography to produce 880.8mg compound of the formula 1.
Abstract translation: 目的：提供一种含有Clerodendron trichotomum的醇提取物和从其中分离出作为有效成分的纯化化合物的抗HIV剂，特别是HIV整合酶的抑制剂，其没有作为逆转录酶抑制剂缺陷的抗药性或副作用 和蛋白酶抑制剂。 组成：具有式1的Clerodendron trichotomum的醇提取物具有抗HIV活性，特别是对HIV整合酶的抑制活性。 在通式中，R1是H或甲基，R2是H，咖啡酰或阿魏酰，R3是H，咖啡酰或阿魏酰。 举例来说，在室温下将4.8kg Clerodendron trichotomum在甲醇中萃取并分馏成二氯甲烷和水。 将馏分用交联葡聚糖LH-20进行柱层析，然后进行硅胶柱层析，得到880.8mg式1化合物。
-
Patent Agency Ranking26.发明授权6-히드록시-1, 3-디옥신-4-온 고리를 가진인간면역결핍바이러스 프로테아제 억제 화합물 및 그의제조방법 失效6-히드록시-1，3-디옥신-4온고리를가진인간면역결핍바이러스프로테아제억제화합물및그의제조방6-
公开(公告)号：KR100374326B1
公开(公告)日：2003-03-03
申请号：KR1020000071437
申请日：2000-11-29
Applicant: 한국과학기술연구원
IPC: C07D407/14
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：提供一种能够用6-羟基-1,3-二恶英-4-酮环抑制HIV蛋白酶的化合物及其生产方法，因此该化合物可用于HIV的预防和治疗。 构成：能够抑制HIV蛋白酶的化合物具有式（I）所示的6-羟基-1,3-二恶英-4-酮环，其中R 1是甲基，乙基，丙基，异丙基，丁基，异丁基或叔丁基 ; R2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-氰基苯磺酰氨基，4 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; R3是甲基，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。
-
公开(公告)号：KR1020030001992A
公开(公告)日：2003-01-08
申请号：KR1020010037867
申请日：2001-06-28
Applicant: 한국과학기술연구원
IPC: C07D491/08
CPC classification number: C07D491/04
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 translation: 目的：提供4-（苯基氨基） - （1,4）二氧杂环丁烷（2,3-Q）喹唑啉，其抑制作为表皮生长因子受体的酪氨酸激酶的活性，并用于预防和治疗癌症 可接受的盐，水合物，溶剂合物及其制备方法。 化合物。 构成：4-（苯基氨基） - （1,4）二氧杂环丁烷（2,3-Q）喹唑啉由式（I）表示，其制备方法包括将一当量的式（II）喹唑啉衍生物与两当量 的式（III）的取代苯胺; 并加入HCl，然后使其在20-80℃反应。 在上式中，R 1是氢，卤素，羟基，C 1-6烷基，烷氧基，硫代烷氧基和烷氧基氨基，C 3-6环烷基，环烷氧基和硫代烷氧基，（芳基或杂芳基）氧基，硫代（芳基或杂芳基） ，氨基，N-单（C 1-6）烷基氨基，N，N-二（C 1-6）烷基氨基，甲酰氨基，碘，乙酰氧基，羟基氨基，肼基，三氟甲基，三氟甲氧基，烯基，炔基，芳基或杂环基团; R2和R3相同或不同，表示 - （CH2）m -R4，其中m为0或1; R4是氢，卤素，C1-6羟基，C1-6烷基，烷氧基，硫代烷氧基和烷氧基氨基，C3-6环烷基，环烷氧基和硫代烷氧基，（芳基或杂芳基）氧基，硫代（芳基或杂芳基） ，N-单（C 1-6）烷基氨基，N，N-二（C 1-6）烷基氨基，甲酰氨基，碘，乙酰氧基，羟基氨基，肼基，三氟甲基，三氟甲氧基，烯基，炔基，芳基或杂环， 烷氧基羰基，酰氨基，N-单烷基（C 1-6）酰胺基，N，N-二烷基（C 1-6）酰氨基，硫代酰氨基，N，N-二烷基（C 1-6）硫代酰氨基，胍基，脲基，C 1-6亚硫酰基， 氨基，单（吡咯烷（C 1-6）烷基）氨基，二（吡咯烷（C 1-6）烷基）氨基或-N（R 5（C 1-6）烷基）氨基， ）（CHR 6 R 7），其中R 5是氢或C 1-6烷基; R6是（CH2）nOH，其中n是整数1-4; R 7是氢，C 1-5烷基，羟烷基，硫代羟烷基，苯基C 1-5烷基，4-羟基苯基（C 1-5）烷基或杂芳基烷基; n为1,2或3。
-
公开(公告)号：KR100346136B1
公开(公告)日：2002-08-01
申请号：KR1019990020951
申请日：1999-06-07
Applicant: 한국과학기술연구원
IPC: C07H21/02
Abstract: 본발명은친지성물질, 특히콜레스테롤또는이의유도체에특이적으로결합하는 RNA서열을제공하고, 또한친지성물질, 특히콜레스테롤또는이의유도체에특이적으로결합하고콜레스테롤에스터라제활성을갖는 RNA서열을제공하며, 이러한서열을이용하여미량의친지성물질, 특히 LDL을탐지하는방법및 이를제거하는방법을제공한다. 종래에밝혀진대부분의 RNA가친수성물질에결합함에비해친지성물질에결합가능한 RNA서열을밝힘으로써이를이용한미량의친지성물질을정량할수 있으며, 상기 RNA서열이콜레스테롤에스터라제활성을갖는성질을이용하여본발명의 RNA서열은환경호르몬에의한생체내의작용을억제할수 있는억제제로사용될수 있을것이며동맥경화와고혈압의근본적인원인인혈류내의 LDL 덩어리를제거하기위한수단으로사용될수 있고 RNA로이루어진인공촉매로서부작용이없는치료제로개발할수 있어그 이용분야가매우넓다.
-
29.发明公开
公开(公告)号：KR1020020041836A
公开(公告)日：2002-06-05
申请号：KR1020000071437
申请日：2000-11-29
Applicant: 한국과학기술연구원
IPC: C07D407/14
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。
-
公开(公告)号：KR1020010002016A
公开(公告)日：2001-01-05
申请号：KR1019990021582
申请日：1999-06-10
Applicant: 한국과학기술연구원
IPC: C12Q1/00
Abstract: PURPOSE: A method for quantifying sugar attached to a solid surface is provided to precisely quantifying the sugar through a gentle reaction by using an enzyme for separating the sugar from a reporter substance without any preprocessing procedure. CONSTITUTION: A method for quantifying sugar attached to a solid surface includes the steps of attaching sugar coupled with reporter molecules such as p-nitrophenyle on a surface of a solid such as a hydrogel selected from Cephalos or Agarose, dissolving glycoside coupling between the sugar and the reporter molecules with an enzyme such as glucosidase, amyloglucosidase, cellulase, fucosidase, mannosidase and galactosidase, and quantifying the dissolved reporter molecules
Abstract translation: 目的：提供一种定量连接到固体表面的糖的方法，通过使用酶从报告物质中分离糖而无需任何预处理程序，通过温和反应精确定量糖。 构成：用于定量连接到固体表面的糖的方法包括将糖与诸如对硝基苯的报告分子连接的糖连接到固体表面上的步骤，例如选自头孢菌素或琼脂糖的水凝胶，将糖与糖和糖 报告分子用酶如葡糖苷酶，淀粉葡糖苷酶，纤维素酶，岩藻糖苷酶，甘露糖苷酶和半乳糖苷酶分子，并定量溶解的报道分子
-
-
-
-
-
-
-
-
-
Search Results
69
records
(took 0.027 seconds)
