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1. 发明授权

US4855422A Process for the preparation of azoniaspironortropanol esters 失效
标题翻译：制备azoniapironortropanol酯的方法
公开(公告)号：US4855422A
公开(公告)日：1989-08-08
申请号：US945488
申请日：1986-12-23
申请人： Wolf Grimminger , Klaus Gorler , Karl P. Odenthal
发明人： Wolf Grimminger , Klaus Gorler , Karl P. Odenthal
IPC分类号： A61K31/435 , A61K31/46 , A61K31/535 , C07D471/20 , C07D471/22 , C07D487/22 , C07D491/22 , C07D498/20
CPC分类号： C07D471/20 , C07D471/22 , C07D498/20
摘要： A method for preparing azoniaspironotropanol esters, esters thus produced, and methods of use for these is disclosed. The esters are effective as broncholytics and as agents in therapy of asthmatic conditions.
摘要翻译：公开了一种制备如此制备的azoniaspironotropanol酯，酯的方法及其用途。这些酯作为支气管扩张剂是有效的，并且作为治疗哮喘病症的药剂是有效的。

2. 发明授权

US5159080A Indole compounds, a process for their preparation, and pharmaceutical compositions containing them 失效
标题翻译：吲哚化合物，其制备方法和含有它们的药物组合物
公开(公告)号：US5159080A
公开(公告)日：1992-10-27
申请号：US629188
申请日：1990-12-18
申请人： Klaus Goler , Wolf Grimminger , Karl P. Odenthal , Pierre Potier
发明人： Klaus Goler , Wolf Grimminger , Karl P. Odenthal , Pierre Potier
IPC分类号： C07D491/147 , A61K31/405 , A61K31/435 , A61K31/44 , A61K31/55 , A61P9/06 , A61P9/08 , A61P9/10 , A61P9/12 , C07D209/10 , C07D295/04 , C07D401/06 , C07D471/04
CPC分类号： C07D401/06 , C07D471/04
摘要： Compounds of the formula ##STR1## wherein R.sub.1 to R.sub.8, which may be identical to or different from each other, have diverse meanings, and the dotted line between the carbon atoms in the 4- and 4a- position or the 4a- and 5-position or the 42- and 12a position may be a single or double bond, or pharmaceutically acceptable salts thereof, as well as a process for the preparation of these compounds, and pharmaceutical compositions containing these compounds. The compounds and their salts are useful for the treatment of heart-circulation disorders.
摘要翻译：其中R 1〜R 8可以相同或不同，具有不同的含义，4-和4-位的碳原子之间的虚线或4a-和5- 位置或42位和12a位可以是单键或双键，或其药学上可接受的盐，以及制备这些化合物的方法，以及含有这些化合物的药物组合物。化合物及其盐可用于治疗心脏循环障碍。

3. 发明授权

US4780476A Azoniaspironortropanol esters as asthma therapeutics and broncholytics 失效
标题翻译：作为哮喘治疗剂和支气管扩张剂的Azoniaspironortropanol酯
公开(公告)号：US4780476A
公开(公告)日：1988-10-25
申请号：US945773
申请日：1986-12-23
申请人： Wolf Grimminger , Karl P. Odenthal
发明人： Wolf Grimminger , Karl P. Odenthal
IPC分类号： A61K31/495 , A61K31/435 , A61K31/535 , A61P11/00 , A61P11/08 , C07D471/20 , C07D471/22 , C07D498/20 , A61K31/40
CPC分类号： C07D471/20 , C07D471/22 , C07D498/20 , Y10S514/826
摘要： The present invention is concerned with the use of azoniaspironortropanol esters of the general formula: ##STR1## wherein R signifies one of the following radicals: (a) an alkylene radical of the general formula: ##STR2## in which R.sub.3 is a hydrogen atom or an alkyl, benzyl, aryl or alkoxy radical and n is a whole number of from 1 to 4,(b) an alkenyl radical of the general formula: ##STR3## in which R.sub.4 and R.sub.5, which can be the same or different, are hydrogen atoms or alkyl or alkenyl radicals and n is a whole number of from 1 to 4,(c) an azaalkylene radical of the general formula: ##STR4## in which R.sub.6 is a hydrogen atom or an alkyl, alkoxycarbonyl or acyl radical and n is a whole number of from 2 to 4,(d) an oxaalkylene radical of the general formula:--(CH.sub.2).sub.n --O--(CH.sub.2).sub.n -- in which n is a whole number of from 2 to 4,(e) an epoxyalkylene radical of the formula: ##STR5## (f) an o-phenylene radical of the general formula: ##STR6## (g) a per-naphthylene radical of the general formula: ##STR7## or (h) a 2,3-quinoxalinene radical of the general formula: ##STR8## in which in formulae (f) to (h), the symbols X and Y, which can be the same or different, are hydrogen atoms or alkyl or alkoxy radicals;and wherein R.sub.1 and R.sub.2, which can be the same or different, are hydrogen or halogen atoms or alkyl, alkoxy, alkoyl, cyclohexyl, phenyl, alkylphenyl, alkoxyphenyl, halophenyl, thienyl or furyl radicals, the alkyl moieties in the said radicals containing up to 6 carbon atoms and being straight-chained or branched, and A.sup..crclbar. is the anion of a mono- to tribasic mineral acid, as asthma therapeutics or broncholytics.
摘要翻译：本发明涉及通式为：其中R表示以下基团之一的下式的其中之一：（a）通式如下的亚烷基：其中R 3为氢原子或烷基，苄基，芳基或烷氧基，n是1至4的整数，（b）具有以下通式的烯基：其中R 4和R 5可以相同或不同的是氢原子或烷基或链烯基，n是1至4的整数，（c）通式如下的氮杂亚烷基：其中R 6是氢原子或烷基，烷氧基羰基或酰基基团，n为2至4的整数，（d）通式为：（CH 2）n O-（CH 2）n - 的氧杂亚烷基，其中n为2至4的整数，（e ）具有下式的环氧亚烷基：（f）具有以下通式的邻亚苯基：（g）具有以下通式的每萘亚萘基：或（h）具有以下通式的2,3-喹喔啉基团：其中在式（f）至（h）中，符号X和Y可以相同或不同，为氢原子或烷基或烷氧基; 烷氧基，烷酰基，环己基，苯基，烷基苯基，烷氧基苯基，卤代苯基，噻吩基或呋喃基，其中R1和R2可相同或不同，为氢或卤素原子或烷基，烷氧基，至6个碳原子并且是直链或支链的，并且A（ - ）是单 - 三元无机酸的阴离子，作为哮喘治疗剂或支气管扩张剂。

4. 发明授权

US06624192B1 Process for production of diacetylrhein 失效
标题翻译：二乙酰胆碱生产工艺
公开(公告)号：US06624192B1
公开(公告)日：2003-09-23
申请号：US08333202
申请日：1994-11-02
申请人： Alfons Carcasona , Wolf Grimminger , Pentti Hêitala , Klaus Witthohn , Helga Zaeske
发明人： Alfons Carcasona , Wolf Grimminger , Pentti Hêitala , Klaus Witthohn , Helga Zaeske
IPC分类号： A61K3121
CPC分类号： C07C67/08 , C07C67/56 , C07C2603/24 , C07C69/16
摘要： The present invention provides a process for obtaining diacetylrhein, wherein diacetylrhein containing aloe-emodin components is subjected to a liquid—liquid partitioning between a polar organic solvent which is only partly miscible with water and an aqueous phase of pH 6.5 to 7.5 and the diacetylrhein is recovered and optionally recrystallized. The present invention is also concerned with diacetylrhein obtainable by this process and with pharmaceutical compositions containing it.
摘要翻译：本发明提供了一种获得二乙酰胆碱的方法，其中含有芦荟大黄素成分的二乙酰胆碱酯在仅与水部分混溶的极性有机溶剂和pH 6.5-7.5的水相之间进行液 - 液分配，并且二乙酰胆碱是回收并任选重结晶。本发明还涉及可通过该方法获得的二乙酰胆碱和含有它的药物组合物。

5. 发明授权

US5393898A Method of preparing diacetyl rhein 失效
标题翻译：二乙酰大黄酸的制备方法
公开(公告)号：US5393898A
公开(公告)日：1995-02-28
申请号：US234583
申请日：1994-04-28
申请人： Alfons Carcasona , Wolf Grimminger , Pentti Hietala , Helga Zaeske , Klaus Witthohn
发明人： Alfons Carcasona , Wolf Grimminger , Pentti Hietala , Helga Zaeske , Klaus Witthohn
IPC分类号： C07C69/00 , C07C50/34
CPC分类号： C07C69/00 , C07C2103/00
摘要： Diacetylrhein which is substantially free of aloe-emodin components, is prepared by a process whereina) rhein-9-anthrone-8-glusoside containing aloe-emodin components is subjected to a liquid-liquid partitioning of the compounds obtained is carried out between a polar organic solvent which is only partly miscible with water and an aqueous phase,b) the rhein-9-anthrone-8-glucoside contained after the partitioning in the aqueous phase is oxidized to rhein-8-glucoside,c) the glucose residue in the 8-position of the rhein-8-glucoside is split off in an acidic medium and,d) the rhein obtained is acetylated and the diacetylrhein recovered.
摘要翻译：基本上不含芦荟大黄素成分的二乙酰胆碱通过以下方法制备，其中a）将含有芦荟大黄素成分的大黄酸-9-蒽酮-8-莫利斯苷进行所得化合物的液液分配，在极性有机溶剂仅与水和水相部分混溶，b）在水相中分配后含有的大黄酸-9-蒽酮-8-葡萄糖苷被氧化成大黄酸-8-葡萄糖苷，c）葡萄糖残基大黄酸8-葡萄糖苷的8位在酸性介质中分离，并且d）将所得的大黄酸乙酰化，并回收二乙酰胆碱。

6. 发明授权

US5391775A Process for production of diacetylrhein 失效
标题翻译：二乙酰胆碱生产工艺
公开(公告)号：US5391775A
公开(公告)日：1995-02-21
申请号：US236682
申请日：1994-04-29
申请人： Alfons Carcasona , Wolf Grimminger , Pentti Heitala , Klaus Witthohn , Helga Zaeske
发明人： Alfons Carcasona , Wolf Grimminger , Pentti Heitala , Klaus Witthohn , Helga Zaeske
IPC分类号： A61K31/22 , A01N37/10 , A61K31/19 , A61K31/192 , A61K31/222 , A61K31/235 , A61K36/18 , A61P19/02 , A61P25/04 , A61P29/00 , C07C67/48 , C07C67/52 , C07C67/58 , C07C69/00 , C07C69/157 , C07C69/16 , C07C69/95 , C07C50/34
CPC分类号： C07C67/08 , C07C67/56 , C07C2103/24
摘要： The present invention provides a process for obtaining diacetylrhein, wherein diacetylrhein containing aloe-emodin components is subjected to a liquid-liquid partitioning between a polar organic solvent which is only partly miscible with water and an aqueous phase of pH 6.5. to 7.5 and the diacetylrhein is recovered and optionally recrystallised.The present invention is also concerned with diacetylrhein obtainable by this process and with pharmaceutical compositions containing it.
摘要翻译：本发明提供了一种获得二乙酰胆碱的方法，其中含有芦荟大黄素成分的二乙酰胆碱在仅与水部分混溶的极性有机溶剂和pH 6.5的水相之间进行液 - 液分配。至7.5，并回收二乙酰胆碱并任选重结晶。本发明还涉及可通过该方法获得的二乙酰胆碱和含有它的药物组合物。

7. 发明授权

US06596764B1 Method of preparing diacetyl rhein 失效
标题翻译：制备二乙酰大黄酸的方法
公开(公告)号：US06596764B1
公开(公告)日：2003-07-22
申请号：US08337671
申请日：1994-11-10
申请人： Alfons Carcasona , Wolf Grimminger , Pentti Hietala , Helga Zaeske , Klaus Witthohn
发明人： Alfons Carcasona , Wolf Grimminger , Pentti Hietala , Helga Zaeske , Klaus Witthohn
IPC分类号： A61K3121
CPC分类号： C07C67/08 , C07C2603/24 , C07C69/16
摘要： The present invention provides a process for treating arthritis utilizing substantially pure diacetylrhein having an aloe-emodin content of less than 20 ppm.
摘要翻译：本发明提供一种使用芦荟大黄素含量小于20ppm的基本上纯的二乙酰胆碱酯治疗关节炎的方法。

8. 发明授权

US5710260A Method of extracting sennosides A, B and A1 失效
标题翻译：方法A，B和A1的提取
公开(公告)号：US5710260A
公开(公告)日：1998-01-20
申请号：US614772
申请日：1995-12-21
申请人： Alfons Carcasona , Wolf Grimminger , Pentti Hietala , Helga Zaeske , Klaus Witthohn
发明人： Alfons Carcasona , Wolf Grimminger , Pentti Hietala , Helga Zaeske , Klaus Witthohn
IPC分类号： C07H15/24 , C07H15/244 , A61K35/78 , C07H1/00
CPC分类号： C07H15/24
摘要： Sennosides A, B and Al of the formula: ##STR1## which are substantially free from sennosides C, D and Dl, and from aloe-emodin derivatives, are prepared by a process wherein a) a sennoside mixture is reduced to rhein-9-anthrone-8-glucoside and aloe-emodin-9-anthrone-8-glucoside, b) a liquid-liquid partitioning of the compounds obtained is carried out between a polar organic solvent which is only partly miscible with water and an aqueous phase and c) the rhein-9-anthrone-8-glycosides contained after the partitioning in the aqueous phase is again oxidized to the corresponding sennosides and these are recovered.
摘要翻译：通过以下方法制备基本上不含番茄苷C，D和D1以及来自芦荟大黄素衍生物的公式：IMAGE的Sennosides A，B和Al，其中a）将sennoside混合物还原成大黄酸-9- 蒽酮-8-葡萄糖苷和芦荟大黄素-9-蒽酮-8-葡萄糖苷，b）所得化合物的液 - 液分配在仅与水和水相部分混溶的极性有机溶剂和c ）在水相中分配后含有的大黄酸-9-蒽酮-8-糖苷被再次氧化成相应的天花苷，并且这些被回收。

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