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公开(公告)号：KR100508627B1
公开(公告)日：2005-08-17
申请号：KR1020020015016
申请日：2002-03-20
Applicant: (주)케비젠
IPC: C07C235/78
Abstract: 본 발명은 화학식1로 표시되는 신규한 레티노이드 유도체 화합물 또는 이의 약제학적으로 허용되는 염에 관한 것이다:
화학식 1
상기식에서, X, R
1 , R
2 및 R
3 은 본원에 정의한 바와 같다. 또한, 본 발명은 상기 레티노이드 유도체 화합물의 제조 방법 및 그러한 화합물을 함유하는 항암제 조성물에 관한 것이다. 본 발명에 따른 화학식1의 화합물은 고도의 항암 활성을 나타내면서 유해한 부작용을 유발하지 않는다.-
公开(公告)号：KR1020030089396A
公开(公告)日：2003-11-21
申请号：KR1020020066071
申请日：2002-10-29
Applicant: (주)케비젠
IPC: A61K36/488 , A61P35/00
Abstract: PURPOSE: Provided is an anticancer composition comprising the alcohol extract of Pueraria sp. roots, which has excellent anticancer activity with less adverse effect and is thus useful for the prevention and treatment of cancer. CONSTITUTION: An anticancer composition is characterized by containing the alcohol extract of Pueraria sp. roots including Pueraria mirifica and Pueraria lobata. The alcohol extract is selected from PE1, PE2, PE3, PE4, Sub PE-A, Sub PE-B, Sub PE-C, Sub PE-D, Sub PE-E, Sub PE-F, Sub PE-G, Sub PE-H, Sub PE-D1, Sub PE-D2, and Sub PE-D3.
Abstract translation: 目的：提供包含葛根属酒精提取物的抗癌组合物。 根，具有优异的抗癌活性，副反应较少，因此可用于预防和治疗癌症。 构成：抗癌组合物的特征在于含有葛根属的酒精提取物。 根系包括葛根和葛根。 酒精提取物选自PE1，PE2，PE3，PE4，Sub PE-A，Sub PE-B，Sub PE-C，Sub PE-D，Sub PE-E，Sub PE-F，Sub PE-G，Sub PE-H，Sub-PE-D1，Sub-PE-D2，Sub-PE-D3。
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公开(公告)号：KR1020050033871A
公开(公告)日：2005-04-13
申请号：KR1020050014553
申请日：2005-02-22
Applicant: (주)케비젠
Abstract: Provided are anticancer compositions comprising the alcohol extract of Pueraria sp. root. The compositions have excellent anticancer effects with less adverse side effects and is thus useful for prevention and treatment of various kinds of cancers. Therefore, the compositions are applied to anticancer-pharmaceuticals and cosmetics. The cosmetic composition comprises, as an active ingredient, the alcohol extract of Pueraria sp. root, wherein Pueraria sp. includes Pueraria mirifica and Pueraria lobata. The alcohol extract is at least one kind selected from PE1, PE2, PE3, PE4, Sub PE-A, Sub PE-B, Sub PE-C, Sub PE-D, Sub PE-E, Sub PE-F, Sub PE-G, Sub PE-H, Sub PE-D1, Sub PE-D2 and Sub PE-D3. The extract inhibits the proliferation of cancer cells to prevent and treat cancers. And it has skin stability, increases skin elasticity, has skin moisturizing effect and prevents skin wrinkles.
Abstract translation: 提供的是包含葛根属酒精提取物的抗癌组合物。 根。 该组合物具有优异的抗癌作用，副作用较小，因此可用于预防和治疗各种癌症。 因此，将组合物应用于抗癌药和化妆品。 化妆品组合物包含作为活性成分的葛根属酒精提取物。 根，其中葛根属 包括葛根和葛根。 酒精提取物选自PE1，PE2，PE3，PE4，Sub PE-A，Sub PE-B，Sub PE-C，Sub PE-D，Sub PE-E，Sub PE-F，Sub PE -G，Sub-PE-H，Sub-PE-D1，Sub-PE-D2和Sub-PE-D3。 提取物抑制癌细胞的增殖以预防和治疗癌症。 它具有皮肤稳定性，增加皮肤弹性，具有皮肤保湿效果，防止皮肤皱纹。
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公开(公告)号：KR100424251B1
公开(公告)日：2004-03-22
申请号：KR1020010025012
申请日：2001-05-08
IPC: C07C227/18
Abstract: PURPOSE: A novel method for preparing α-L-aspartyl-L-phenylalanine methyl ester·HCl salt is provided, to reduce the amount of by-products, to allow the by-products to be reused after hydrolysis and to increase the production yield by 20% or more. CONSTITUTION: The method comprises the steps of reacting L-aspartic acid with trimethyl silyl chloride in the presence of an alcohol solvent to esterify the β-COOH selectively to obtain α-L-aspartyl-L-phenylalanine methyl ester·HCl. Preferably the alcohol solvent is selected from the group consisting of methyl alcohol, ethyl alcohol, allyl alcohol and benzyl alcohol. Preferably the method comprises further the steps of protecting an amine group with -CHO, Boc, benzyloxycarbonyl group, or -C(O)OR¬2 (R2 is methyl. ethyl or isobutyl group) by using acetic anhydride and formic acid.
Abstract translation: 目的：提供一种制备α-L-天冬氨酰-L-苯丙氨酸甲酯盐酸盐的新方法，以减少副产物的量，使副产物在水解后重新使用和 将产量提高20％以上。 构成：该方法包括以下步骤：在醇溶剂存在下使L-天冬氨酸与三甲基甲硅烷基氯化物反应以选择性酯化β-COOH以获得α-L-天冬氨酰-L-苯丙氨酸甲酯和amp ; middot; HCl中。 优选醇溶剂选自甲醇，乙醇，烯丙醇和苯甲醇。 优选地，该方法还包括通过使用乙酸酐和甲酸，用-CHO，Boc，苄氧基羰基或-C（O）OR 2（R 2为甲基，乙基或异丁基）保护胺基的步骤。
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公开(公告)号：KR100437102B1
公开(公告)日：2004-06-23
申请号：KR1020020001178
申请日：2002-01-09
Applicant: (주)케비젠
IPC: C07K5/00
Abstract: PURPOSE: Provided are a novel retinol derivative, its preparation method in higher yield, and its use. The novel retinol has excellent light-stability, and shows high reactivity to retinoic acid receptor α, while showing low reactivity to retinoic receptor β and γ. It can applied to medical products, cosmetics, soap, shampoo, functional foods, etc., for the prevention and improvement of skin aging. CONSTITUTION: The novel retinol derivative is characterized by carboester bond of a peptide material having COOH group, wherein the peptide material having COOH group is selected from -di, -tri, -poly peptide including N-L- α-aspartyl-L-phenylalanine 1-methylester(AMP;aspartame), N-protection group-aspartame, neotame and the like. Its manufacturing method comprises the steps of: reacting retinylacetate with methanolic solvent and inorganic slat at 25-40 deg.C in a dark room then extracting the reaction product with ether solvent; removing the solvent then followed by mixing a compound having OH group, natural or separated and purified retinol, diethylazodicarboxylate and triphenylphosphate with methylenechloride solvent, and reacting them at room temperature to obtain the ester derivative of retinol; and performing chromatography with reverse-phase, Merck Silicagel 60 RP 18(40-63) micro meter to separate pure ester derivative of retinol.
Abstract translation: 目的：提供一种新颖的视黄醇衍生物及其制备方法，其收率较高，并且其用途。 该新型视黄醇具有优异的光稳定性，并且对视黄酸受体α具有高反应性，而对视黄酸受体β具有低反应性; 和＆amp; gamma ;. 它可以应用于医疗产品，化妆品，肥皂，洗发水，功能性食品等，以预防和改善皮肤老化。 构成：新颖的视黄醇衍生物的特征在于具有COOH基团的肽材料的羧基酯键，其中具有COOH基团的肽材料选自包括NL-和α-天冬氨酰-L- 苯丙氨酸1-甲酯（AMP;天冬甜素），N-保护基 - 阿斯巴甜，纽甜等。 其制造方法包括以下步骤：在25-40℃，在黑暗的房间内将乙酸视黄醇酯与甲醇溶剂和无机薄片反应，然后用乙醚溶剂萃取反应产物; 然后除去溶剂，然后将具有OH基团的化合物，天然或分离纯化的视黄醇，偶氮二羧酸二乙酯和磷酸三苯酯与二氯甲烷溶剂混合，并在室温下反应，得到视黄醇的酯衍生物; 并用反相色谱（Merck Silicagel 60 RP 18（40-63）微米）进行色谱分离以分离视黄醇的纯酯衍生物。
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Patent Agency Ranking
公开(公告)号：KR1020040020426A
公开(公告)日：2004-03-09
申请号：KR1020020052026
申请日：2002-08-30
Applicant: (주)케비젠
IPC: C07C403/20
Abstract: PURPOSE: Retinoid derivatives in cis form having substantially different chemical structure while having increased antitumor effects but reduced negative side effects compared with the conventional retinoid compounds, are provided. CONSTITUTION: The retinoid derivatives are represented by formula (I) and can be in cis form especially at the position of 9 and/or 13, wherein X is O, NH or S; R1 and R2 are the same or different, and independently -OH, -SH, -NH2, -COOH, -R(CH2)mCH3, -RCOCO(CH2)mCH3, -RCO(CH2)mCHCH3CH3, -RCO(CH2)mNR4CH3, -RCOCHOH(CH2)mCH3, -RCOCH2(CH2)m(CH)3, -RCOCH2CHOH(CH2)mCH3, -RCOCH2(CH2)mCOOH, -RSO2CH2(CH2)mCH4, -RPO2(OH)CH2(CH2)mCH3 or -RCOCH(NHCOCH3)CH2CH2CONH2; and R3 is H, wherein R is CH2, O, NH or S, R4 is H or C1-C6 alkyl, and m is an integer of 0 to 5.
Abstract translation: 目的：提供具有与常规类视黄醇化合物相比具有显着不同化学结构同时具有增加的抗肿瘤作用但降低的副作用的顺式形式的类视黄醇衍生物。 构成：类视黄醇衍生物由式（I）表示，并且可以是顺式，特别是在9和/或13位，其中X是O，NH或S; R1和R2相同或不同，独立地是-OH，-SH，-NH2，-COOH，-R（CH2）mCH3，-RCOCO（CH2）mCH3，-RCO（CH2）mCHCH3CH3，-RCO（CH2）mNR4CH3 ，-RCOCHOH（CH2）mCH3，-RCOCH2（CH2）m（CH）3，-RCOCH2CHOH（CH2）mCH3，-RCOCH2（CH2）mCOOH，-RSO2CH2（CH2）mCH4，-RPO2（OH）CH2（CH2） 或-RCOCH（NHCOCH 3）CH 2 CH 2 CONH 2; 并且R 3是H，其中R是CH 2，O，NH或S，R 4是H或C 1 -C 6烷基，m是0-5的整数。
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公开(公告)号：KR1020020060598A
公开(公告)日：2002-07-18
申请号：KR1020020001178
申请日：2002-01-09
Applicant: (주)케비젠
IPC: C07K5/00
CPC classification number: C07C403/08 , A23L33/155 , A61K8/671 , A61K31/07 , A61Q5/02 , A61Q19/005 , A61Q19/008 , A61Q19/10 , C07K5/04 , C07K19/00
Abstract: PURPOSE: Provided are a novel retinol derivative, its preparation method in higher yield, and its use. The novel retinol has excellent light-stability, and shows high reactivity to retinoic acid receptor α, while showing low reactivity to retinoic receptor β and γ. It can applied to medical products, cosmetics, soap, shampoo, functional foods, etc., for the prevention and improvement of skin aging. CONSTITUTION: The novel retinol derivative is characterized by carboester bond of a peptide material having COOH group, wherein the peptide material having COOH group is selected from -di, -tri, -poly peptide including N-L- α-aspartyl-L-phenylalanine 1-methylester(AMP;aspartame), N-protection group-aspartame, neotame and the like. Its manufacturing method comprises the steps of: reacting retinylacetate with methanolic solvent and inorganic slat at 25-40 deg.C in a dark room then extracting the reaction product with ether solvent; removing the solvent then followed by mixing a compound having OH group, natural or separated and purified retinol, diethylazodicarboxylate and triphenylphosphate with methylenechloride solvent, and reacting them at room temperature to obtain the ester derivative of retinol; and performing chromatography with reverse-phase, Merck Silicagel 60 RP 18(40-63) micro meter to separate pure ester derivative of retinol.
Abstract translation: 目的：提供一种新型视黄醇衍生物，其制备方法较高产率及其用途。 该新型视黄醇具有优异的光稳定性，对视黄酸受体α具有高反应性，而对视黄酸受体β和γ的反应性低。 适用于医疗用品，化妆品，肥皂，洗发水，功能性食品等，用于预防和改善皮肤老化。 构成：新型视黄醇衍生物的特征在于具有COOH基团的肽材料的碳键，其中具有COOH基团的肽材料选自-di，-tri， - 多肽，包括NL-α-天冬氨酰-L-苯丙氨酸1- 甲基酯（AMP;阿斯巴甜），N-保护基 - 阿斯巴甜，neotame等。 其制造方法包括以下步骤：将黑醋酸乙烯酯与甲醇溶剂和无机条板在25-40℃下在暗室中反应，然后用乙醚溶剂萃取反应产物; 除去溶剂，然后将具有OH基团的化合物，天然或分离的纯化的视黄醇，偶氮二甲酸二乙酯和磷酸三苯酯与二氯甲烷溶剂混合，并在室温下使其反应，得到视黄醇的酯衍生物; 并用反相色谱法，Merck Silicagel 60 RP 18（40-63）微米分离纯化的视黄醇酯衍生物。
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公开(公告)号：KR100822757B1
公开(公告)日：2008-04-17
申请号：KR1020020052026
申请日：2002-08-30
Applicant: (주)케비젠
IPC: C07C403/20
Abstract: 본 발명은 화학식(I)로 표시되는 신규한 시스 형태의 레티노이드 유도체 화합물 또는 이의 약제학적으로 허용되는 염에 관한 것이다:
(I)
상기식에서, X, R
1 , R
2 및 R
3 은 본원에 정의한 바와 같다. 또한, 본 발명은 상기 레티노이드 유도체 화합물의 제조 방법 및 그러한 화합물을 함유하는 항암제 조성물에 관한 것이다. 본 발명에 따른 화학식(I)의 화합물은 고도의 항암 활성을 나타내면서 유해한 부작용을 유발하지 않는다.
항암제, 레티노이드 유도체, 아폽토시스-
公开(公告)号：KR100548058B1
公开(公告)日：2006-01-31
申请号：KR1020020066071
申请日：2002-10-29
Applicant: (주)케비젠
IPC: A61K36/488 , A61P35/00
Abstract: 본 발명은 퓨에라리아 속 식물 뿌리의 알콜 추출물을 함유하는 항암용 조성물에 관한 것으로, 항암 효과가 뛰어나며 부작용이 적어 각종 암의 예방과 치료에 유용하게 사용될 수 있다.
또한, 본 발명의 퓨에라리아 속 식물 뿌리의 알콜 추출물은 피부에 안정할 뿐 아니라, 보습효과, 피부 탄력 효과, 잔주름, 기미, 잡티 등의 예방에 효과적이므로, 화장료 조성물로 유용하게 사용될 수 있다.Abstract translation: 本发明涉及含有pyuerariah的在植物根部的醇提取物的抗癌组合物，以及优良的抗肿瘤活性具有副作用少，可以是各种癌症的预防和治疗是有用的。
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公开(公告)号：KR100516378B1
公开(公告)日：2005-09-26
申请号：KR1020050014553
申请日：2005-02-22
Applicant: (주)케비젠
Abstract: 본 발명은 퓨에라리아 속 식물 뿌리의 알콜 추출물을 함유하는 항암용 조성물에 관한 것으로, 항암 효과가 뛰어나며 부작용이 적어 각종 암의 예방과 치료에 유용하게 사용될 수 있다.
또한, 본 발명의 퓨에라리아 속 식물 뿌리의 알콜 추출물은 피부에 안정할 뿐 아니라, 보습효과, 피부 탄력 효과, 잔주름, 기미, 잡티 등의 예방에 효과적이므로, 화장료 조성물로 유용하게 사용될 수 있다.
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