EXTRACTS OF: PHOLIDOTA CHINESIS LINDL. THE PREPARATION METHODS AND PHARMACEUTICAL USE THEREOF

    公开(公告)号:WO2006012778A1

    公开(公告)日:2006-02-09

    申请号:PCT/CN2004/000906

    申请日:2004-08-06

    IPC分类号: C07C43/243

    摘要: This invention relates to extracts of Pholidota Chinesis Lindl. the preparation methods and pharrriaceutical use thereof. The methods of extracting active compound from Pholidota Chinesis Lindl. incudes the following steps: 1) extracting the Pholidota Chinesis Lindl. by ethanol, concentrating at reduced pressure to make extractive; 2) ectracting the extractive in turn of n-butane, ethyl acetate, n-butanol; 3) directing the extractive of ethyl acetate through chromatography column, eluting by methanol;4) separating and purifying the elent collected in step 3) by high pressure liquid chromatography to get active compounds. The formula of the extracted active compound (3-10) is: (I); active compound (1) is: (II); active compound (2) is: (III). The compound or its salts, enantiomers, racemes, tautomers and physiologic functional derivates extracted from the Pholidota Chinesis Lindl. Are useful in production of the medicament for the treatment or prevention of inflammatory disease.

    EXTRACTS OF: PHOLIDOTA CHINESIS LINDL. THE PREPARATION METHODS AND PHARMACEUTICAL USE THEREOF
    5.
    发明申请
    EXTRACTS OF: PHOLIDOTA CHINESIS LINDL. THE PREPARATION METHODS AND PHARMACEUTICAL USE THEREOF 审中-公开
    提取物:PHOLIDOTA CHINESIS LINDL。 其制备方法及其药物应用

    公开(公告)号:WO2006012778A8

    公开(公告)日:2007-05-10

    申请号:PCT/CN2004000906

    申请日:2004-08-06

    摘要: This invention relates to extracts of Pholidota Chinesis Lindl. the preparation methods and pharrriaceutical use thereof. The methods of extracting active compound from Pholidota Chinesis Lindl. incudes the following steps: 1) extracting the Pholidota Chinesis Lindl. by ethanol, concentrating at reduced pressure to make extractive; 2) ectracting the extractive in turn of n-butane, ethyl acetate, n-butanol; 3) directing the extractive of ethyl acetate through chromatography column, eluting by methanol;4) separating and purifying the elent collected in step 3) by high pressure liquid chromatography to get active compounds. The formula of the extracted active compound (3-10) is: (I); active compound (1) is: (II); active compound (2) is: (III). The compound or its salts, enantiomers, racemes, tautomers and physiologic functional derivates extracted from the Pholidota Chinesis Lindl. Are useful in production of the medicament for the treatment or prevention of inflammatory disease.

    摘要翻译: 本发明涉及中华百草枯提取物。 其制备方法和药物用途。 从Pholidota Chinesis Lindl提取活性化合物的方法。 包括以下步骤:1)提取Pholidota Chinesis Lindl。 用乙醇浓缩,减压浓缩; 2)将正丁醇,乙酸乙酯,正丁醇依次取出; 3)通过色谱柱引导乙酸乙酯萃取,用甲醇洗脱; 4)通过高压液相色谱法分离纯化步骤3)中收集的洗脱液,得到活性化合物。 提取的活性化合物(3-10)的配方为:(I); 活性化合物(1)为:(II); 活性化合物(2)为:(III)。 从PholidotaChinesis Lindl提取的化合物或其盐,对映异构体,总状花序,互变异构体和生理功能衍生物。 可用于生产用于治疗或预防炎性疾病的药物。

    STYRIL DERIVATIVES AND PROCESSES FOR THEIR PREPARATION
    10.
    发明申请
    STYRIL DERIVATIVES AND PROCESSES FOR THEIR PREPARATION 审中-公开
    STYRIL衍生物及其制备方法

    公开(公告)号:WO1994014800A1

    公开(公告)日:1994-07-07

    申请号:PCT/GB1993002627

    申请日:1993-12-22

    申请人: CELLTECH LIMITED

    IPC分类号: C07D405/06

    摘要: Compounds of general formula (1) are described, wherein Y is a halogen atom or a group -OR , wherein R is an optionally substituted alkyl group; X is -O-, -S- or -N(R )-, where R is a hydrogen atom or an alkyl group; R is an optionally substituted alkyl, alkenyl, cycloalkyl or cycloalkenyl group; R and R , which may be the same or different, is each a group -(CH2)nAr, where Ar is a monocyclic or bicyclic aryl group optionally containing one or more heteroatoms selected from oxygen, sulphur or nitrogen atoms and n is zero or an integer 1, 2 or 3; R is a hydrogen atom or an optionally substituted alkyl group; and the salts, solvates, hydrates and N-oxides thereof. Compounds according to the invention are potent, selective and orally active PDE IV inhibitors and are useful in the prophylaxis and treatment of asthma and other diseases.

    摘要翻译: 描述通式(1)的化合物,其中Y是卤素原子或-OR 1基团,其中R 1是任选取代的烷基; X是-O - , - S-或-N(R 6) - ,其中R 6是氢原子或烷基; R 2是任选取代的烷基,烯基,环烷基或环烯基; R 3和R 4可以相同或不同,各自为 - (CH 2)nAr基团,其中Ar是任选含有一个或多个选自氧,硫或氮的杂原子的单环或双环芳基 原子和n为零或整数1,2或3; R 5是氢原子或任选取代的烷基; 及其盐,溶剂合物,水合物和N-氧化物。 根据本发明的化合物是有效的,选择性和口服活性的PDE IV抑制剂,并且可用于预防和治疗哮喘和其它疾病。