公开(公告)号：KR100917039B1

公开(公告)日：2009-09-10

申请号：KR1020070053068

申请日：2007-05-31

Applicant: 한국과학기술연구원

Inventor： 이소하 ,  배애님 ,  임혜원 ,  서선희 ,  정세진 ,  김준석 ,  전제호

IPC: C07D249/12

Abstract: 본 발명은 T-형 칼슘 채널(T-type calcium channel)을 억제하는 효과가 우수하여 간질과 같은 뇌질환, 협심증, 고혈압, 심근경색과 같은 심장질환, 신경성 통증, 그리고 암 등 다양한 종류의 질환을 치료 및 예방에 유용한 트리아졸 유도체와 이 화합물을 포함하는 약제 조성물에 관한 것이다.
트리아졸 유도체, T-형 칼슘 채널, 협심증, 고혈압, 심근경색, 통증, 간질 및 암

公开(公告)号：KR1020080105463A

公开(公告)日：2008-12-04

申请号：KR1020070053068

申请日：2007-05-31

Applicant: 한국과학기술연구원

Inventor： 이소하 ,  배애님 ,  임혜원 ,  서선희 ,  정세진 ,  김준석 ,  전제호

IPC: C07D249/12

Abstract: A triazole derivative useful as a T-type calcium channel blocker, and a pharmaceutical composition containing the derivative rae provided to inhibit the calcium channel of cell membranes, thereby preventing and treating the diseases such as brain disease, heart disease, neurogenic pain and cancer disease. A triazole derivative is represented by the formula 1, wherein R1 is phenyl group, a benzimidazole group, or a benzimidazole C1-C8 alkyl group; R2 is H, a C1-C8 alkyl group, a C1-C20 alkanoyl group, a phenyl group, a benzoyl group, or a thiophenecarbonyl group; R3 is H, or an N-phenylacetamide group; and the benzene ring of a phenyl group, a benzoyl group, a benzimidazole group and an N-phenylacetamide group can be substituted with 1-4 substituents selected from a halogen atom, a nitro group, a C1-C8 alkyl group, a C1-C8 alkoxy group and a C1-C8 haloalkyl group.

Abstract translation: 可用作T型钙通道阻断剂的三唑衍生物和含有衍生物的药物组合物，其用于抑制细胞膜的钙通道，从而预防和治疗脑疾病，心脏病，神经源性疼痛和癌症疾病 。 三唑衍生物由式1表示，其中R1是苯基，苯并咪唑基或苯并咪唑C1-C8烷基; R2是H，C1-C8烷基，C1-C20烷酰基，苯基，苯甲酰基或噻吩羰基; R3是H或N-苯基乙酰胺基团; 苯基，苯甲酰基，苯并咪唑基和N-苯基乙酰胺基的苯环可以被1-4个选自卤素原子，硝基，C1-C8烷基，C1- C8烷氧基和C1-C8卤代烷基。

公开(公告)号：KR100743255B1

公开(公告)日：2007-07-27

申请号：KR1020060040614

申请日：2006-05-04

Applicant: 한국과학기술연구원

Inventor： 조용서 ,  추현아 ,  배애님 ,  차주환 ,  고훈영 ,  김화실 ,  임혜원 ,  서선희

IPC: C07D209/48

Abstract: Novel 1,3-dioxoisoindole derivatives having selective antagonism of T-type calcium channel are provided to treat brain diseases including epilepsy, hypertension and angina pectoris, heart disease and nerve system pain by inhibiting the T-type calcium channel as a representative low-voltage activated calcium channel. The 1,3-dioxoisoindole derivatives represented by the formula(1) or their pharmaceutically acceptable salts are provided, wherein R1 is phenyl group or benzyl group which is substituted or unsubstituted by halogen atom, C1-C6 alkoxy group, C1-C6 alkyl group, or cyano group; R2 is a hetero ring group selected from piperidinyl group, pyrolidinyl group, morpholinyl group and piperazinyl group which is substituted or unsubstituted by C1-C6 alkyl substituent; and n is 1 or 2, provided that a compound in which R2 is morpholinyl group when R1 is C1-C6 alkyl-substituted phenyl group is excluded.

Abstract translation: 通过抑制T型钙通道作为代表性的低电压来提供具有T型钙通道选择性拮抗作用的新型1,3-二氧代异吲哚衍生物来治疗包括癫痫，高血压和心绞痛，心脏病和神经系统疼痛的脑疾病 激活钙通道。 由式（1）表示的1,3-二氧代异吲哚衍生物或它们的药学上可接受的盐，其中R1是被卤素原子，C1-C6烷氧基，C1-C6烷基取代或未被取代的苯基或苄基 或氰基; R2是选自哌啶基，吡咯烷基，吗啉基和由C1-C6烷基取代基取代或未取代的哌嗪基的杂环基; 并且n是1或2，条件是当R 1是C 1 -C 6烷基取代的苯基时，其中R 2是吗啉基的化合物被排除在外。

公开(公告)号：KR1020050001899A

公开(公告)日：2005-01-07

申请号：KR1020030042252

申请日：2003-06-26

Applicant: 한국과학기술연구원

Inventor： 이용섭 ,  김형자 ,  서선희 ,  이재열

IPC: C07C69/757

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 translation: 目的：提供含有抗氧化剂或抗病毒活性的化合物或其药学上可接受的盐，含有化合物的菊花提取物，来自提取物的化合物的分离方法，含有用于治疗或预防HIV或疾病的化合物的药物组合物 涉及细胞成分的氧化，含有该化合物的抗氧化食品添加剂和含有该化合物的抗氧化剂化妆品。 构成：该化合物由式1表示，其中R1和R2是H或咖啡酰基; R3是由式（a）表示的特定的咖啡酰基。 菊花提取物通过使用水和有机溶剂萃取。 优选地，有机溶剂是选自醇，乙酸乙酯，二氯甲烷和丙酮中的至少一种。 通过使用选自硅胶，Sephadex，RP-18，聚酰胺，Toyopearl和XAD树脂的填料进行柱色谱，从提取物中分离式1的化合物。

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

Inventor： 이용섭 ,  박호군 ,  이재열 ,  양범석 ,  서선희

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。