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公开(公告)号：US5888995A
公开(公告)日：1999-03-30
申请号：US493733
申请日：1995-06-22
CPC分类号： C07J71/0031
摘要： The invention concerns compounds of formula I ##STR1## in which R.sub.1 is hydrogen or a straight or branched hydrocarbon chain; R.sub.2 is hydrogen or a straight or branched hydrocarbon chain; R.sub.3 is acyl; X.sub.1 is hydrogen, fluorine or chlorine; and X.sub.2 is hydrogen, fluorine or chlorine. Also disclosed are processes for preparation of the compounds, pharmaceutical compositions containing them and methods employing the compounds in the treatment of inflammatory and allergic conditions.
摘要翻译： 本发明涉及其中R 1为氢或直链或支链烃链的式Ⅰ化合物; R2是氢或直链或支链烃链; R3是酰基; X1是氢，氟或氯; X2是氢，氟或氯。 还公开了制备化合物的方法，含有它们的药物组合物和使用该化合物治疗炎性和过敏性疾病的方法。
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2.发明授权Novel stereoisomeric component A of stereoisomeric mixtures of 2'-unsymmetrical 16,17-methylenedioxy steroid 21-acylates, compositions thereof, and method of treating therewith 失效2 {40-不对称16,17-亚甲二氧基甾族化合物21-酰化物，其组合物及其处理方法的立体异构体混合物的新型立体异构体组分A
公开(公告)号：US3996359A
公开(公告)日：1976-12-07
申请号：US629493
申请日：1975-11-06
CPC分类号： C07J71/0031 , A61K31/57
摘要： A process for the resolution of stereoisomeric mixtures of certain steroids obtained by synthesis into its components, comprising subjecting the stereoisomeric mixture to gel filtration, the components in view of different retention volumes being separated and being separately recoverable; and stereoisomeric components A and B thereby obtained, pharmaceutical compositions thereof; and method of treating inflammation therewith.
摘要翻译： 一种用于将通过合成获得的某些类固醇的立体异构混合物拆分成其组分的方法，包括使立体异构体混合物进行凝胶过滤，鉴于不同保留体积的组分被分离并且可单独回收; 和由此获得的立体异构体组分A和B，其药物组合物; 和治疗炎症的方法。
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公开(公告)号：US6140308A
公开(公告)日：2000-10-31
申请号：US261247
申请日：1999-03-03
申请人： Ralph Lennart Brattsand , Peter Edman , Thomas Hogberg , Stinabritt Nilsson , Bror Arne Thalen , Jan Erik Ulmius
发明人： Ralph Lennart Brattsand , Peter Edman , Thomas Hogberg , Stinabritt Nilsson , Bror Arne Thalen , Jan Erik Ulmius
CPC分类号： C07J71/0031
摘要： Novel compounds which are a glucocorticosteroid (GCS) chemically bound to a sugar, having the general formulaGCS.sup.1 --O--Sugar.sup.1for colon- or ileum-specific delivery of the GCS to inflamed bowel mucosa, as well as processes for their preparation, pharmaceutical preparations containing the compounds and the use of said compounds in therapy.
摘要翻译： 化学结合糖的糖皮质激素（GCS）的新型化合物，具有通式GCS1-O-糖1用于结肠或回肠特异性递送GCS至发炎肠粘膜，以及其制备方法，药物制剂 含有化合物和所述化合物在治疗中的用途。
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公开(公告)号：US5908833A
公开(公告)日：1999-06-01
申请号：US764985
申请日：1996-12-13
申请人： Ralph Lennart Brattsand , Peter Edman , Thomas Hogberg , Stinabritt Nilsson , Bror Arne Thalen , Jan Erik Ulmius
发明人： Ralph Lennart Brattsand , Peter Edman , Thomas Hogberg , Stinabritt Nilsson , Bror Arne Thalen , Jan Erik Ulmius
IPC分类号： A61K31/58 , A61P1/00 , A61P29/00 , C07J20060101 , C07J71/00 , A61K31/705
CPC分类号： C07J71/0031
摘要： Novel compounds which are a glucocorticosteroid (GCS) chemically bound to a sugar, having the general formulaGCS.sup.1 --O--Sugar.sup.1for colon- or ileum-specific delivery of the GCS to inflamed bowel mucosa, as well as processes for their preparation, pharmaceutical preparations containing the compounds and the use of said compounds in therapy.
摘要翻译： 化学结合糖的糖皮质激素（GCS）的新型化合物，具有通式GCS1-O-糖1用于结肠或回肠特异性递送GCS至发炎肠粘膜，以及其制备方法，药物制剂 含有化合物和所述化合物在治疗中的用途。
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5.发明授权Compositions and method of treating with component B of stereoisomeric mixtures of 2'-unsymmetrical 16,17-methylenedioxy steriods 失效用2 {40-不对称16,17-亚甲基二氧基立体异构体的立体异构体混合物的组分B处理的组合物和方法
公开(公告)号：US3992534A
公开(公告)日：1976-11-16
申请号：US629390
申请日：1975-11-06
CPC分类号： C07J71/0031
摘要： A process for the resolution of stereoisomeric mixtures of certain steroids obtained by synthesis into its components, comprising subjecting the stereoisomeric mixture to gel filtration, the components in view of different retention volumes being separated and being separately recoverable; and stereoisomeric components A and B thereby obtained, pharmaceutical compositions thereof; and method of treating inflammation therewith.This application claims pharmaceutical compositions and method of employing Component B of the novel steroid stereoisomeric mixtures, including both the free 21-hydroxyl and the 21-acetates thereof.
摘要翻译： 一种用于将通过合成获得的某些类固醇的立体异构混合物拆分成其组分的方法，包括使立体异构体混合物进行凝胶过滤，鉴于不同保留体积的组分被分离并且可单独回收; 和由此获得的立体异构体组分A和B，其药物组合物; 和治疗炎症的方法。
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6.发明授权Compositions and method of treating with stereoisomeric mixtures of 2-unsymmetrical 16,17-methylenedioxy steroids 失效用2-不对称16,17-亚甲二氧基类固醇的立体异构体混合物处理的组合物和方法
公开(公告)号：US3983233A
公开(公告)日：1976-09-28
申请号：US629389
申请日：1975-11-06
IPC分类号： C07J17/00
摘要： Novel steroids having the general formula: ##SPC1##Wherein X and Y are independently selected from hydrogen and fluorine, X being selected from hydrogen and fluorine when Y is hydrogen and X being fluorine when Y is fluorine, Z is selected from hydroxyl and esterified hydroxyl preferably containing a maximum of 12 carbon atoms, if any, in the esterifying group, R is selected from straight and branched hydrocarbon chains having 2-10 carbon atoms; processes for the preparation of said steroids; compositions containing said steroids; and method of treating inflammation therewith. The steroids are physiologically active compounds possessing anti-inflammatory activity. This application claims pharmaceutical compositions and method of treating employing the novel steroid steroisomeric mixtures.
摘要翻译： 具有以下通式的新型类固醇：
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