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公开(公告)号：KR100541222B1
公开(公告)日：2006-01-11
申请号：KR1020030027850
申请日：2003-04-30
Applicant: 충남대학교산학협력단
IPC: C07C65/40
Abstract: 본 발명은 만성 알레르기성 염증 치료효과를 갖는 IL-5 저해제로서 저분자이면서 비펩타이드 계열 물질인 신규 찰콘계 유도체 및 그의 제조방법, 인터루킨-5 (IL-5) 저해제로서의 용도에 관한 것이다.
본 발명에 의한 신규 찰콘계 유도체는 저분자의 비펩타이드 계열 물질이기 때문에 종래 알려진 알르레기성 염증 치료제와는 달리 단백질에 대한 비특이적 반응이 없기 때문에 알르레기 억제제로 유용하게 활용될 수 있다.
알르레기, 염증, IL-5, 저해제, 억제제, 과민성-
Patent Agency Ranking
公开(公告)号：KR100529692B1
公开(公告)日：2005-11-17
申请号：KR1020030027849
申请日：2003-04-30
Applicant: 충남대학교산학협력단
IPC: C07D311/30
Abstract: 본 발명은 만성 알레르기성 염증 치료효과를 갖는 IL-5 저해제로서 저분자이면서 비펩타이드 계열 물질인 신규 사이클로헥실아이소플라본논계 유도체 및 그의 제조방법, 인터루킨-5 (IL-5) 저해제로서의 용도에 관한 것이다.
본 발명에 의한 신규 사이클로헥실아이소플라본논계 유도체는 저분자의 비펩타이드 계열 물질이기 때문에 종래 알려진 알르레기성 염증 치료제와는 달리 단백질에 대한 비특이적 반응이 없기 때문에 알르레기 억제제로 유용하게 활용될 수 있다.-
公开(公告)号：KR100580953B1
公开(公告)日：2006-05-16
申请号：KR1020030027369
申请日：2003-04-30
Applicant: 충남대학교산학협력단
IPC: C07D311/36
Abstract: 본 발명은 만성 알레르기성 염증 치료효과를 갖는 IL-5 저해제로서 저분자이면서 비펩타이드 계열 물질인 신규 아이소플라본논계 유도체 및 그의 제조방법, 인터루킨-5 (IL-5) 저해제로서의 용도에 관한 것이다.
본 발명에 의한 신규 아이소플라본논계 유도체는 저분자의 비펩타이드 계열 물질이기 때문에 종래 알려진 알르레기성 염증 치료제와는 달리 단백질에 대한 비특이적 반응이 없기 때문에 알르레기 억제제로 유용하게 활용될 수 있다.
알르레기, 염증, IL-5, 저해제, 억제제, 과민성-
4.发明公开
公开(公告)号：KR1020040093961A
公开(公告)日：2004-11-09
申请号：KR1020030027849
申请日：2003-04-30
Applicant: 충남대학교산학협력단
IPC: C07D311/30
Abstract: PURPOSE: Provided is a cyclohexyl isoflavonone derivative inhibiting IL-5 activity. The derivative inhibits the introduction of eosinophil which is an inflammatory cell causing asthma into the airway, and improves the airway sensitivity to alleviate asthma symptom. CONSTITUTION: The isoflavonone derivative of the formula (1) inhibiting IL-5 activity is provided, wherein R1 is cyclohexylmethoxy, hydrogen or hydroxy; R2 is cyclohexylmethoxy, hydrogen or hydroxy; R3 is hydroxy, -OCH2COOCH3, -OCH2COOH. The method for preparing the isoflavonone derivative of the formula (1) comprises the steps of: reacting a compound of the formula (2) with thallium nitrate trihydrate in lower alcohol to prepare a compound of the formula (1-1); reacting the compound of the formula (1-1) with potassium carbonate and methyl chloroacetate in an organic solvent to prepare a compound of the formula (1-2); and reacting the compound of the formula (1-2) with potassium hydroxide in an organic solvent to prepare a compound of the formula (1-3).
Abstract translation: 目的：提供抑制IL-5活性的环己基异黄酮衍生物。 该衍生物抑制嗜酸性粒细胞的引入，嗜酸粒细胞是导致哮喘进入气道的炎症细胞，并且改善气道敏感性以减轻哮喘症状。 构成：提供了抑制IL-5活性的式（1）的异黄酮衍生物，其中R1是环己基甲氧基，氢或羟基; R2是环己基甲氧基，氢或羟基; R3是羟基，-OCH2COOCH3，-OCH2COOH。 制备式（1）的异黄酮衍生物的方法包括以下步骤：使式（2）化合物与硝酸铊三水合物在低级醇中反应以制备式（1-1）化合物; 使式（1-1）化合物与碳酸钾和氯乙酸甲酯在有机溶剂中反应，制备式（1-2）化合物; 并使式（1-2）的化合物与氢氧化钾在有机溶剂中反应制备式（1-3）的化合物。
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公开(公告)号：KR1020040093962A
公开(公告)日：2004-11-09
申请号：KR1020030027850
申请日：2003-04-30
Applicant: 충남대학교산학협력단
IPC: C07C65/40
Abstract: PURPOSE: A novel chalcone-based derivative is provided, which has an interleukin-5 inhibiting effect and a chronic allergic inflammation curing effect and is a low molecule and a non-peptide material. CONSTITUTION: The novel chalcone-based derivative represented by the formula(1) is produced by condensing a compound represented by the formula(2) and a compound represented by the formula(3) in an alcohol solvent in the presence of a base, wherein the alcohol solvent is a C1-C5 alcohol and the base is sodium hydroxide or potassium hydroxide. In the formulas, R1 and R2 are benzyloxy, cyclohexyl methoxy, hydrogen, or hydroxy and R3 is hydroxy or -COOH.
Abstract translation: 目的：提供一种新型的查耳酮衍生物，其具有白细胞介素-5抑制作用和慢性过敏性炎症治疗效果，是低分子和非肽材料。 构成：由式（1）表示的新型查耳酮系衍生物通过在醇溶剂中在碱存在下将式（2）表示的化合物与式（3）表示的化合物缩合而制备，其中 醇溶剂是C1-C5醇，碱是氢氧化钠或氢氧化钾。 式中R1和R2是苄氧基，环己基甲氧基，氢或羟基，R3是羟基或-COOH。
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公开(公告)号：KR1020040093500A
公开(公告)日：2004-11-06
申请号：KR1020030027369
申请日：2003-04-30
Applicant: 충남대학교산학협력단
IPC: C07D311/36
Abstract: PURPOSE: Isoflavonone derivative which inhibits IL-5 activity are provided. The derivative inhibits the introduction of eosinophil which is an inflammatory cell causing asthma into the airway, and improves the airway sensitivity to alleviate asthma symptom. CONSTITUTION: The isoflavonone derivatives of the formula (1) inhibiting IL-5 activity is provided, wherein R1 is benzyloxy, hydrogen or hydroxy; R2 is benzyloxy, hydrogen or hydroxy; R3 is hydroxy, -OCH2COOCH3, -OCH2COOH or compound groups of formula (2). The method for preparing the isoflavonone derivative of the formula (1) comprises the steps of: reacting a compound of the formula (3) to prepare an isoflavonone derivative of formula (1-1); reacting the compound of the formula (1-1) with benzyl triammonium chloride and glucopyranosyl bromoacetate in the presence of base to prepare a compound of the formula (1-2); reacting the compound of the formula (1-1) with epichlorohydrin in the presence of base to prepare an epoxymethyl derivative of the formula (1-4); and reacting the compound of formula (1-4) with anhydrous sodium acetate and titanium tetraisopropoxide in acetic acid to prepare a compound of the formula (1-5), deprotecting the compound of the formula (1-4) to prepare a compound of the formula (1-6), and reacting the compound of the formula (1-4) with sodium acetate and titanium tetraisopropoxide in methanol to prepare compounds of the formulas (1-7) and (1-8).
Abstract translation: 目的：提供抑制IL-5活性的异黄酮衍生物。 该衍生物抑制嗜酸性粒细胞的引入，嗜酸粒细胞是导致哮喘进入气道的炎症细胞，并且改善气道敏感性以减轻哮喘症状。 构成：提供抑制IL-5活性的式（1）的异黄酮衍生物，其中R1是苄氧基，氢或羟基; R2是苄氧基，氢或羟基; R3是羟基，-OCH2COOCH3，-OCH2COOH或式（2）的化合物基团。 制备式（1）的异黄酮衍生物的方法包括以下步骤：使式（3）的化合物与式（1-1）的异黄酮衍生物反应; 在碱的存在下使式（1-1）的化合物与苄基三氯化铵和溴代吡喃葡萄糖基吡喃酮反应，以制备式（1-2）的化合物; 在碱的存在下使式（1-1）的化合物与表氯醇反应以制备式（1-4）的环氧甲基衍生物; 并使式（1-4）化合物与无水乙酸钠和四异丙醇钛在乙酸中反应，制得式（Ⅰ-1）化合物，使式（1-4）化合物脱保护，制备 式（1-6）表示，并使式（1-4）化合物与乙酸钠和四异丙氧基钛在甲醇中反应，制备式（1-7）和（1-8）的化合物。
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