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1. 发明授权

KR100450062B1 세래스트롤, 세래판올, 세스퀴테르펜 에스터계 화합물 또는 노박덩굴 추출물을 유효성분으로 함유하는 염증질환,면역질환 또는 암 치료제 失效
标题翻译： 세래스트롤，세래판올，세스퀴테르펜에스터계화합물또는노박덩굴추출물을유효성분으로함유하는염증질환，면역질환또는암치료제
公开(公告)号：KR100450062B1
公开(公告)日：2004-09-24
申请号：KR1020010078375
申请日：2001-12-12
申请人： 한국생명공학연구원
发明人： 이정준 , 이정형 , 김항섭 , 홍영수
IPC分类号： A61K31/56 , C07C65/34
摘要： PURPOSE: A therapeutic agent for inflammatory disease, immune disease and cancer which contains celastrol, celaphanol, a sesquiterpene ester-based compound or a Celastrus orbiculatus Thunb. extract as effective ingredient is provided. The Celastrus orbiculatus Thunb. extract containing the celastrol also can be used as an NF-κB inhibitor. CONSTITUTION: An NF-κB inhibitor contains celastrol of the formula(1), celaphanol of the formula(2) and a sesquiterpene ester-based compound of the formula(3). In formulae, R1 is H, furoic acid or benzoic acid, R3 is H or acetic acid and R4 is furoic acid or benzoic acid. The NF-κB inhibitor also contains a Celastrus orbiculatus Thunb. extract containing the celastrol. The Celastrus orbiculatus Thunb. extract is obtained by extracting in C1-4 alcohol, followed by reextraction in an organic solvent, separation and then purification. The therapeutic agent for inflammatory disease, immune disease and cancer contains the celastrol, celaphanol, sesquiterpene ester-based compound or Celastrus orbiculatus Thunb. extract.
摘要翻译：目的：治疗炎症性疾病，免疫疾病和癌症的治疗剂，其中含有雷公藤红素，celaphanol，倍半萜烯基酯化合物或Celastrus orbiculatus Thunb。提取物作为有效成分。 Celastrus orbiculatus Thunb。含有雷公藤红素的提取物也可以用作NF-κB抑制剂。组成：NF-κB抑制剂含有式（1）的雷公藤红素，式（2）的celaphanol和式（3）的倍半萜酯基化合物。在通式中，R1是H，糠酸或苯甲酸，R3是H或乙酸，R4是糠酸或苯甲酸。 NF-κB抑制剂还含有南蛇藤（Cerabritus orbiculatus Thunb）。含有雷公藤红素的提取物。 Celastrus orbiculatus Thunb。提取物通过在C1-4醇中萃取，然后在有机溶剂中再萃取，分离然后纯化而获得。炎症性疾病，免疫疾病和癌症的治疗剂包含雷公藤红素，celaphanol，倍半萜烯基酯化合物或Celastrus orbiculatus Thunb。提取。

2. 发明公开

KR1020030064327A 간염 치료제 및 예방제 또는 간보호제로 유용한 섬오갈피추출물 失效
标题翻译： ACANTHOPANACIS KOREANUM提取物作为治疗和预防乙型肝炎或保护肝脏的代理商
公开(公告)号：KR1020030064327A
公开(公告)日：2003-07-31
申请号：KR1020030004697
申请日：2003-01-24
申请人： 한국생명공학연구원
发明人： 이정준 , 이정형 , 김항섭 , 홍영수 , 김영호 , 남정범 , 손동환
IPC分类号： A61K36/254 , A61P1/16
CPC分类号： A61K36/254
摘要： PURPOSE: Water and ethanol extracts of Acanthopanacis koreanum and an extract containing polysaccharides having a molecular weight of 12,000 to 14,000 or more among the ethanol extract thereof are provided. The Acanthopanax koreanum extract inhibits the expression of apoptosis-inducing protein of cancer cells activated by TNF-α and cuts DNA of cancer cells into small fractions and a composition containing the extract can be used as an agent for treating and preventing hepatitis or protecting the liver. CONSTITUTION: Acanthopanacis koreanum is extracted in water at 90deg.C. the water extract is reextracted in 50-90% ethanol. The Acanthopanacis koreanum is selected from the group consisting of Acanthopanax senticosus, Acanthopanax divaricatus, Acanthopanax divaricatus, Acanthopanax chiisanensis or the like. An agent for treating and preventing hepatitis or protecting the liver comprises the water and ethanol extracts of Acanthopanacis koreanum and the extract containing polysaccharides having a molecular weight of 12,000 to 14,000 or more among the ethanol extract thereof.
摘要翻译：目的：提供刺五加的水和乙醇提取物和含乙醇提取物中分子量为12,000至14,000以上的多糖的提取物。刺五加提取物抑制由TNF-α激活的癌细胞的细胞凋亡诱导蛋白的表达，并将癌细胞的DNA切成小部分，含有提取物的组合物可用作治疗和预防肝炎或保护肝脏的药剂。规定：将刺五加在90摄氏度的水中萃取。水提取物在50-90％乙醇中再提取。刺五加选自刺五加，刺五加，刺五加，刺五加等。用于治疗和预防肝炎或保护肝脏的药剂包括在其乙醇提取物中分子量为12,000至14,000或更高的刺五加的水和乙醇提取物和含有多糖的提取物。

3. 发明公开

KR1020020046095A 디테르펜계 화합물을 염증질환, 면역질환 및 암 치료제로사용하는 신규한 용도 失效
标题翻译：用于治疗炎症疾病，免疫疾病和癌症的DITERPENE化合物
公开(公告)号：KR1020020046095A
公开(公告)日：2002-06-20
申请号：KR1020000075608
申请日：2000-12-12
申请人： 한국생명공학연구원
发明人： 이정준 , 이정형 , 김항섭 , 홍영수 , 황방연
IPC分类号： A61K31/122
CPC分类号： C07D493/08 , A61K31/122 , C07C45/78 , C07C49/743
摘要： PURPOSE: Provided are diterpene compounds useful for the treatment of inflammatory diseases, immune diseases and cancer. CONSTITUTION: A diterpene compound, kamebanin, represented by formula(1), a diterpene compound, kamebacetal A, represented by formula(2), a diterpene compound, kamebakaurin,represented by formula(3), and a diterpene compound, exisanin A, represented by formula(4) are and useful for treatment of inflammatory disease, immune disease and cancer. The diterpene compounds inhibit the activities of nitric oxide, prostaglandin, and TNF-alpha, as well as effectively inhibit the activities of an inflammation inducing factor and NF-kappa B associated with cell apoptosis. Therefore, a pharmaceutical compositions useful for the treatment of inflammatory diseases, immune diseases and cancer contains the diterpene compounds as active ingredients.
摘要翻译：目的：提供可用于治疗炎性疾病，免疫疾病和癌症的双萜化合物。构成：由式（1）表示的二萜化合物，二甲脒化合物，由式（2）表示的咔咔咔al A，由式（3）表示的二萜化合物，咔咔咔啉，和二萜烯化合物exisanin A，由式（4）表示，可用于治疗炎性疾病，免疫疾病和癌症。双萜化合物抑制一氧化氮，前列腺素和TNF-α的活性，并有效抑制与细胞凋亡相关的炎症诱导因子和NF-κB的活性。因此，用于治疗炎性疾病，免疫疾病和癌症的药物组合物含有双萜化合物作为活性成分。

4. 发明公开

KR1020010087681A 신규 7,8-디히드로-잔테논-8-카르복실산 유도체 및 이를생산하는 신규 미생물 失效
标题翻译：生产7,8-二羟基-8-羟基苯甲酸衍生物的新型微生物
公开(公告)号：KR1020010087681A
公开(公告)日：2001-09-21
申请号：KR1020000011563
申请日：2000-03-08
申请人： 한국생명공학연구원
发明人： 이정준 , 이정형 , 김항섭 , 홍영수 , 박윤주
IPC分类号： C12P7/42
CPC分类号： C12R1/66 , C07D311/86 , C12P17/06
摘要： PURPOSE: Provided is a novel microorganism that produces 7,8-dihydro- xanthenone-8-carboxylic acid derivatives. Therefore, angiogenic diseases related with the vascular endothelial growth factor(VEGF) can be prevented or treated. CONSTITUTION: A microorganism Aspergillus sp. Y80118 (KCTC 0737BP) produces 7,8-dihydro- 1,7-dihydroxy-3- hydroxymethyl- xanthenone-8-carboxylic acid methylester represented by formula (1) and having a VEGF inhibiting activity and anticancer activity. The pharmaceutical composition for the prevention and treatment of angiogenic diseases related with the vascular endothelial growth factor(VEGF) comprises 7,8-dihydro- 1,7-dihydroxy-3- hydroxymethyl- xanthenone-8-carboxylic acid methylester(ACRL-B4) as an active ingredient, in which the diseases include cancer, rheumatism or diabetic retinopathy.
摘要翻译：目的：提供产生7,8-二氢呫吨酮-8-羧酸衍生物的新型微生物。因此，可以预防或治疗与血管内皮生长因子（VEGF）相关的血管生成疾病。构成：微生物曲霉菌 Y80118（KCTC 0737BP）生产由式（1）表示的具有VEGF抑制活性和抗癌活性的7,8-二氢-1,7-二羟基-3-羟甲基 - 呫吨酮-8-羧酸甲酯。用于预防和治疗与血管内皮生长因子（VEGF）相关的血管生成疾病的药物组合物包含7,8-二氢-1,7-二羟基-3-羟甲基 - 呫吨酮-8-羧酸甲酯（ACRL-B4）作为活性成分，其中疾病包括癌症，风湿病或糖尿病性视网膜病变。

5. 发明授权

KR100402714B1 디테르펜계 화합물을 염증질환, 면역질환 및 암 치료제로사용하는 신규한 용도 失效
标题翻译： 디테르펜계화합물을염증질환，역역질환및암암암료제제
公开(公告)号：KR100402714B1
公开(公告)日：2003-11-13
申请号：KR1020020082517
申请日：2002-12-23
申请人： 한국생명공학연구원
发明人： 이정준 , 이정형 , 김항섭 , 홍영수 , 황방연
IPC分类号： A61K31/122
摘要： PURPOSE: Provided is a novel use of diterpene compounds as therapeutic agents of inflammation, immune disease and cancer, particularly, the diterpene compounds includes kamebanin of the formula(1), kamebacetal A of the formula(2), kamebakaurin of the formula(3) and exisanin A of the formula(4) which have excellent anti-inflammatory and anti-cancer activities. CONSTITUTION: The diterpene compounds including kamebanin of the formula(1), kamebacetal A of the formula(2), kamebakaurin of the formula(3) and exisanin A of the formula(4) inhibit NF-kB which is a transcriptional factor in the expression of iNOS or COX-2. Especially kamebakaurin inhibits the expression of Bfl-1/A1, cIAP-1 and cIAP-2 which inhibit cell death. An inhibitor of expression of cell death inhibitory genes contains kamebanin, kamebacetal A, kamebakaurin and exisanin A, or their pharmaceutically acceptable salts as active ingredients.
摘要翻译：目的：提供了二萜化合物作为炎症，免疫疾病和癌症治疗剂的新用途，特别是二萜化合物包括式（1）的kamebanin，式（2）的kamebacetal A，式（3）的kamebakaurin ）和具有优异的抗炎和抗癌活性的式（4）的异黄酮A. 构成：包含式（1）的kamebanin，式（2）的kamebacetal A，式（3）的kamebakaurin和式（4）的exisanin A的二萜化合物抑制NF-kB，其是转录因子表达iNOS或COX-2。尤其是kamebakaurin抑制Bfl-1 / A1，cIAP-1和cIAP-2的表达，抑制细胞死亡。细胞死亡抑制基因的表达抑制剂含有作为有效成分的kamebanin，kamebacetal A，kamebakaurin，exisanin A或它们的药学上可接受的盐。

6. 发明公开

KR1020030048312A ＡＧＩ-7 화합물과 세스칸델린의 효율적 제조방법 失效
标题翻译：制备SESCANDELIN及其类似物的方法AGI-7
公开(公告)号：KR1020030048312A
公开(公告)日：2003-06-19
申请号：KR1020010078376
申请日：2001-12-12
申请人： 한국생명공학연구원
发明人： 이정준 , 김상희 , 김항섭 , 이정형
IPC分类号： C07D311/76
CPC分类号： Y02P20/55
摘要： PURPOSE: A process for preparing sescandelin and analogue thereof AGI-7 is provided, thereby easily preparing sescandelin and AGI-7 having improved angiogenesis-inhibiting activity in higher yield. CONSTITUTION: A process for preparing sescandelin of the formula(1) and AGI-7 of the formula(2) comprises the steps of: (a) reacting a compound of the formula(3) in formic acid or acetic acid or aqueous formic acid to form a ring structure and remove benzyl group as a protecting group, thereby preparing AGI-7 of formula(2); (b) selectively oxidizing 3-methyl-4-formyl isocumarin as a side-product of the step (a) using a oxidizing agent to purify the AGI-7 of the formula(2); and reducing acetyl group at C4 site of AGI-7 of the formula(2) using a reducing agent, wherein R is benzyl; the oxidizing agent is selected from RuO4, Ag2O, NaClO2, CrO3, KMnO4 and O2; and the reducing agent is selected from Li, Na, LiH, BH3, LiBH4, NaBH4, KBH4, Zn(BH4)2, NaBH3CN, LiBHEt3, Bu2AlH, LiAlH4, Et3SiH and SmI2.
摘要翻译：目的：提供制备菊苣苷及其类似物AGI-7的方法，从而容易地制备具有改善的血管发生抑制活性的更高产量的菊苣苷和AGI-7。构型：制备式（1）的西泮丁烷和式（2）的AGI-7的方法包括以下步骤：（a）使式（3）的化合物在甲酸或乙酸或水性甲酸形成环结构并除去苄基作为保护基，从而制备式（2）的AGI-7; （b）使用氧化剂选择性氧化作为步骤（a）的副产物的3-甲基-4-甲酰基异烟酸，以纯化式（2）的AGI-7; 并使用还原剂还原式（2）的AGI-7的C4位点的乙酰基还原，其中R是苄基; 氧化剂选自RuO4，Ag2O，NaClO2，CrO3，KMnO4和O2; 还原剂选自Li，Na，LiH，BH3，LiBH4，NaBH4，KBH4，Zn（BH4）2，NaBH3CN，LiBHEt3，Bu2AlH，LiAlH4，Et3SiH和SmI2。

7. 发明公开

KR1020030064108A 간염 치료제 및 예방제 또는 간보호제로 유용한 오갈피추출물 失效
标题翻译： ACANTHOPANACIS SENTICOSUS EXTRACT有用作为治疗和预防乙型肝炎或保护肝脏的代理商
公开(公告)号：KR1020030064108A
公开(公告)日：2003-07-31
申请号：KR1020020004552
申请日：2002-01-25
申请人： 한국생명공학연구원
发明人： 이정준 , 이정형 , 김항섭 , 김영호 , 손동환
IPC分类号： A61K36/254 , A61P1/16
摘要： PURPOSE: The use of an Acanthopanacis sencortex extract as an agent for treating and preventing hepatitis or protecting the liver is provided. The extract of Acanthopanacis sencortex exhibit excellent hepatitis inhibiting activity and protects the liver in a rat. CONSTITUTION: An agent for treating and preventing hepatitis or protecting the liver comprises a water extract of Acanthopanacis sencortex, a 50-90% ethanol extract of Acanthopanacis cortex and an extract containing polysaccharides having a molecular weight of 12,000 to 14,000 or more among the ethanol extract thereof. The Acanthopanacis cortex is selected from the group consisting of Acanthopanax senticosus, Acanthopanax divaricatus, Acanthopanax divaricatus, Acanthopanax chiisanensis or the like.
摘要翻译：目的：提供刺五加皮质提取物作为治疗和预防肝炎或保护肝脏的药物。刺五加皮质提取物表现出优异的肝炎抑制活性，保护大鼠肝脏。构成：治疗和预防肝炎或保护肝脏的药物包括刺五加皮质水提物，刺五加皮质醇50-90％乙醇提取物和含乙醇提取物中分子量为12,000至14,000或更多的多糖的提取物它们。刺五加皮质选自刺五加，刺五加，刺五加，刺五加等。

8. 发明公开

KR1020030048311A 세래스트롤, 세래판올, 세스퀴테르펜 에스터계 화합물 또는 노박덩굴 추출물을 유효성분으로 함유하는 염증질환,면역질환 또는 암 치료제 失效
标题翻译：用于炎症疾病，免疫疾病和癌症，含有CELASTROL，CELASANOL，SESQUITERPENE ESTER的化合物或CELASTRUS ORBICULATUS THUNB的治疗药物。提取有效
公开(公告)号：KR1020030048311A
公开(公告)日：2003-06-19
申请号：KR1020010078375
申请日：2001-12-12
申请人： 한국생명공학연구원
发明人： 이정준 , 이정형 , 김항섭 , 홍영수
IPC分类号： A61K31/56 , C07C65/34
摘要： PURPOSE: A therapeutic agent for inflammatory disease, immune disease and cancer which contains celastrol, celaphanol, a sesquiterpene ester-based compound or a Celastrus orbiculatus Thunb. extract as effective ingredient is provided. The Celastrus orbiculatus Thunb. extract containing the celastrol also can be used as an NF-κB inhibitor. CONSTITUTION: An NF-κB inhibitor contains celastrol of the formula(1), celaphanol of the formula(2) and a sesquiterpene ester-based compound of the formula(3). In formulae, R1 is H, furoic acid or benzoic acid, R3 is H or acetic acid and R4 is furoic acid or benzoic acid. The NF-κB inhibitor also contains a Celastrus orbiculatus Thunb. extract containing the celastrol. The Celastrus orbiculatus Thunb. extract is obtained by extracting in C1-4 alcohol, followed by reextraction in an organic solvent, separation and then purification. The therapeutic agent for inflammatory disease, immune disease and cancer contains the celastrol, celaphanol, sesquiterpene ester-based compound or Celastrus orbiculatus Thunb. extract.
摘要翻译：目的：用于炎症疾病，免疫疾病和癌症的治疗剂，其包含celastrol，celaphanol，倍半萜酯基化合物或Celastrus orbiculatus Thunb。提取物作为有效成分。西葫芦含有celastrol的提取物也可用作NF-κB抑制剂。构成：NF-κB抑制剂含有式（1）的celastrol，式（2）的细胞油和式（3）的倍半萜酯类化合物。在式中，R 1是H，糠酸或苯甲酸，R 3是H或乙酸，R 4是糠酸或苯甲酸。 NF-κB抑制剂还含有一种Celastrus orbiculatus Thunb。提取物含有celastrol。西葫芦提取物通过在C 1-4醇中提取，然后在有机溶剂中重新萃取，分离然后纯化而获得。炎性疾病，免疫疾病和癌症的治疗剂含有celastrol，celaphanol，倍半萜酯类化合物或Celastrus orbiculatus Thunb。提取。

9. 发明公开

KR1020030003215A 디테르펜계 화합물을 염증질환, 면역질환 및 암 치료제로사용하는 신규한 용도 失效
标题翻译：作为治疗性炎症，免疫疾病和癌症治疗药物的新方法
公开(公告)号：KR1020030003215A
公开(公告)日：2003-01-09
申请号：KR1020020082517
申请日：2002-12-23
申请人： 한국생명공학연구원
发明人： 이정준 , 이정형 , 김항섭 , 홍영수 , 황방연
IPC分类号： A61K31/122
摘要： PURPOSE: Provided is a novel use of diterpene compounds as therapeutic agents of inflammation, immune disease and cancer, particularly, the diterpene compounds includes kamebanin of the formula(1), kamebacetal A of the formula(2), kamebakaurin of the formula(3) and exisanin A of the formula(4) which have excellent anti-inflammatory and anti-cancer activities. CONSTITUTION: The diterpene compounds including kamebanin of the formula(1), kamebacetal A of the formula(2), kamebakaurin of the formula(3) and exisanin A of the formula(4) inhibit NF-kB which is a transcriptional factor in the expression of iNOS or COX-2. Especially kamebakaurin inhibits the expression of Bfl-1/A1, cIAP-1 and cIAP-2 which inhibit cell death. An inhibitor of expression of cell death inhibitory genes contains kamebanin, kamebacetal A, kamebakaurin and exisanin A, or their pharmaceutically acceptable salts as active ingredients.
摘要翻译：目的：提供双萜化合物作为炎症，免疫疾病和癌症的治疗剂的新用途，特别地，二萜化合物包括式（1）的游动素，式（2）的游动乙酰胺A，式（3）的卡米巴龙）和具有优异的抗炎和抗癌活性的式（4）的exisanin A。构成：式（1）的游动素，式（2）的卡宾巴林，式（3）的卡米巴龙和式（4）的前药三甲酸二钠的二萜化合物抑制作为转录因子的NF-kB 表达iNOS或COX-2。特别是kamebakaurin抑制抑制细胞死亡的Bfl-1 / A1，cIAP-1和cIAP-2的表达。细胞死亡抑制基因的表达抑制剂含有kamebanin，kamebacetal A，kamebakaurin和exisanin A或其药学上可接受的盐作为活性成分。

10. 发明公开

KR1020010001270A 혈관신생을 억제하는 새로운 이소쿠마린 유도체 无效
标题翻译：新型异喹诺酮衍生物抑制血管生成
公开(公告)号：KR1020010001270A
公开(公告)日：2001-01-05
申请号：KR1019990020374
申请日：1999-06-03
申请人： 한국생명공학연구원
发明人： 이정준 , 김항섭 , 이정형 , 홍영수 , 박윤주
IPC分类号： C07D311/00
CPC分类号： C07D311/76
摘要： PURPOSE: Provided are novel isocoumarine derivatives inhibiting angiogenesis, a preparation method thereof and a pharmaceutical composition comprising them. The isocoumarine derivatives, especially, 6, 8-dihydroxy-4-acetyl isocoumarine and 6, 8-dihydroxy-4-hydroxyacetyl isocoumarine are excellent in an inhibiting activity of the angiogenesis, therefore is useful in treating an angiogenic disease such as a cancer, a rheumatoid arthritis and diabetic retinopathy. CONSTITUTION: The novel isocoumarine derivative is represented by the following formula (1), wherein R1 is hydrogen, alkyl or allylalkyl; and R2 and R3, which may be the same or different, each represents hydrogen or alkyl. Also, 6, 8-dihydroxy-4-acetyl isocoumarine is represented by the following formula (2), wherein the compound is isolated from Sesquicillium mold strain Y70832. The preparation method of the compound comprises the steps of : extracting the mold strain Y70832 culture with acetone and ethyl acetate; separating the culture by a silica gel chromatography using a solvent mixed methylene chloride with methanol; further separating the culture by Sephadex LH 20 column chromatography using methanol as the solvent; and carrying out a high performance liquid chromatography (HPLC) using acetonitrile as the solvent.
摘要翻译：目的：提供抑制血管发生的新型异香豆素衍生物，其制备方法和包含它们的药物组合物。异香豆素衍生物，特别是6,8-二羟基-4-乙酰基异香豆素和6,8-二羟基-4-羟基乙酰基异香豆素在血管发生的抑制活性方面是优异的，因此可用于治疗血管生成疾病如癌症，类风湿关节炎和糖尿病性视网膜病变。构成：该新颖的异香豆素衍生物由下式（1）表示，其中R 1是氢，烷基或烯丙基烷基; 和可以相同或不同的R 2和R 3各自表示氢或烷基。此外，6,8-二羟基-4-乙酰基异香豆素由下式（2）表示，其中所述化合物从过敏酵母菌株Y70832中分离。该化合物的制备方法包括以下步骤：用丙酮和乙酸乙酯萃取霉菌株Y70832培养; 使用溶剂混合二氯甲烷与甲醇通过硅胶色谱分离培养物; 使用甲醇作为溶剂，通过Sephadex LH 20柱色谱法进一步分离培养物; 并使用乙腈作为溶剂进行高效液相色谱（HPLC）。

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