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11. 发明申请

WO1992011278A1 14'beta'-H-, 14- AND 15-EN-11'beta'-aryl-4-ESTRENES 审中-公开
标题翻译： 14β-H，14-和15-EN-11β-芳基-4-元素
公开(公告)号：WO1992011278A1
公开(公告)日：1992-07-09
申请号：PCT/EP1991002494
申请日：1991-12-21
申请人： SCHERING AKTIENGESELLSCHAFT BERLIN UND BERGKAMEN , SCHWEDE, Wolfgang , OTTOW, Eckhard , NEEF, Günter , CLEVE, Arwed , CHWALISZ, Krzysztof , MICHNA, Horst , FUHRMANN, Ulrike
发明人： SCHERING AKTIENGESELLSCHAFT BERLIN UND BERGKAMEN
IPC分类号： C07J41/00
CPC分类号： C07J1/0092 , C07J1/0088 , C07J1/0096 , C07J9/00 , C07J17/00 , C07J33/002 , C07J41/0094 , C07J43/003
摘要： New compounds having the general formula (I), as well as their pharmacologically acceptable addition salts with acids, are disclosed. In the formula (I), either (Ia) R11 stands for a hydrogen atom in the β position, whereas R?12 and R13¿ each represent a hydrogen atom, or (Ib) R11 stands for a hydrogen atom in the β position, whereas R?12 and R13¿ together represent a second bond, or (Ic) R?11 and R12¿ together represent a second bond, whereas R13 stands for a hydrogen atom, or (Id) R11 stands for a hydrogen atom in the α position, whereas R?12 and R13¿ together represent a second bond. In all cases (Ia, Ib, Ic or Id), X stands for an oxygen atom, the hydroxymino grouping >N∩OH or two hydrogen atoms, R1 stands for a hydrogen atom or a methyl group; R2 stands for a hydroxy group, a C¿1?-C10 alkoxy or C1-C10 acyloxy group, whereas R?3 and R4¿ have the usual meanings for competitive pregesterone antagonists, given in the description. Also disclosed are processes for producing these new compounds, pharmaceutical compositions containing these compounds, their use to produce medicaments and new intermediate products required for the process. These new compounds have a strong affinity for the gestagen receptor, as well as strong antigestagenous, antiglucorticoidal, antimineralcorticoidal and antiandrogenous properties.

12. 发明申请

WO1992011277A1 6,7-MODIFIED 11'beta'-ARYL-4-ESTRENES 审中-公开
标题翻译： 6,7修饰的11β-ARYL-4-ESTRENES
公开(公告)号：WO1992011277A1
公开(公告)日：1992-07-09
申请号：PCT/EP1991002493
申请日：1991-12-21
申请人： SCHERING AKTIENGESELLSCHAFT BERLIN UND BERGKAMEN , OTTOW, Eckhard , SCHWEDE, Wolfgang , CLEVE, Arwed , ELGER, Walter , CHWALISZ, Krzysztof , SCHNEIDER, Martin , FUHRMANN, Ulrike
发明人： SCHERING AKTIENGESELLSCHAFT BERLIN UND BERGKAMEN
IPC分类号： C07J01/00
CPC分类号： C07J1/0092 , C07J1/0096 , C07J17/00 , C07J31/006 , C07J41/0083 , C07J41/0094 , C07J43/003 , C07J71/001
摘要： Compounds have general formula (I), in which X stands for an oxygen atom or for the hydroxyimino grouping >N∩OH; R1 stands for a hydrogen atom or for a methyl group; G stands for a hydrogen, halogen atom, a C¿1?-C4 alkyl residue, when M and Q stand for hydrogen atoms or for a common additional bond; Q stands for a C1-C4 alkyl residue when M and G stand for hydrogen atoms; and G and M represent together a methylene or ethylene group when Q stands for a hydrogen atom; R?2, R3 and R4¿ have the meanings given in the description. These new compounds have strong antigestagenous, antiglucocorticoidal, antimineralcorticoidal and antiandrogenous properties and are useful for producing medicaments.

13. 发明申请

WO1992009573A2 CYCLOPENTANE ETHER DERIVATIVES, METHODS FOR PREPARING THEM AND THEIR USE IN PHARMACEUTICALS 审中-公开
标题翻译：环戊烷衍生物，其制备方法及其在药物中的应用
公开(公告)号：WO1992009573A2
公开(公告)日：1992-06-11
申请号：PCT/DE1991000925
申请日：1991-11-23
申请人： SCHERING AKTIENGESELLSCHAFT BERLIN UND BERGKAMEN , REHWINKEL, Hartmut , KLAR, Ulrich , VORBRÜGGEN, Helmut , THIERAUCH, Karl-Heinz , VERHALLEN, Peter
发明人： SCHERING AKTIENGESELLSCHAFT BERLIN UND BERGKAMEN
IPC分类号： C07C405/00
CPC分类号： C07C405/00
摘要： The invention concerns cyclopentane ether derivatives of formula (I), their salts with physiologically tolerable bases, as well as the α, β- and η-cyclodextrin clathrates and compounds of formula (I) encapsulated with liposomes. The invention also concerns methods for preparing these compounds and their use in pharmaceuticals.

14. 发明申请

WO1991018918A1 PROCESS FOR PRODUCING 10'beta'-H-STEROIDS 审中-公开
标题翻译：生产10（BETA）-H-甾体的方法
公开(公告)号：WO1991018918A1
公开(公告)日：1991-12-12
申请号：PCT/EP1991001018
申请日：1991-06-03
申请人： SCHERING AKTIENGESELLSCHAFT BERLIN UND BERGKAMEN , OTTOW, Eckhard , NEEF, Günter , CLEVE, Arwed , WIECHERT, Rudolf
发明人： SCHERING AKTIENGESELLSCHAFT BERLIN UND BERGKAMEN
IPC分类号： C07J21/00
CPC分类号： C07J1/0059 , C07J21/006 , C07J21/008 , C07J31/006 , C07J33/002 , C07J41/0083 , C07J43/003 , C07J51/00
摘要： Compounds of general formula (III), in which A and B together stand for an additional bond and D stands for a hydrogen atom or B and D together stand for an additional bond and A stands for a hydrogen atom and Y and Y' each stand for a protected keto group and R?1 and R4¿ have the meaning given in the description, can be reduced with an electropositive metal, without destroying the aromatic system and the 5,6 double bond, to compounds of general formula (IIa), which can be converted to compounds of general formule (Ia) or (Ib) which are useful in the synthesis of antigestagens.

15. 发明申请

WO1991017175A1 2-IODO-3-KETO-DELTA4-STEROIDS, PROCESS FOR PRODUCING THEM AND THEIR FURTHER PROCESSING 审中-公开
标题翻译： 2-IODO-3-KETO-DELTA 4 -STEROIDS，其生产方法及其进一步加工
公开(公告)号：WO1991017175A1
公开(公告)日：1991-11-14
申请号：PCT/DE1991000386
申请日：1991-05-08
申请人： SCHERING AKTIENGESELLSCHAFT BERLIN UND BERGKAMEN , WESTERMANN, Jürgen , NICKISCH, Klaus , HARRE, Michael , ROHDE, Ralph
发明人： SCHERING AKTIENGESELLSCHAFT BERLIN UND BERGKAMEN
IPC分类号： C07J01/00
CPC分类号： C07J1/0059 , C07J1/0011 , C07J1/0025 , C07J1/0074
摘要： The novel intermediate products of general formula (I) in which: R1 is a hydrogen atom or a straight-chained or branched alkyl group with 1 to 4 carbon atoms; R2 is a hydrogen atom or a methyl group; R3 is a hydrogen atom; and R4 is an acyloxy group with 1 to 4 carbon atoms in the acyl radical; or R?3 and R4¿ jointly stand for a keto-oxygen atom; are eminently suitable for introducing a delta1 double bond in the steroid backbone with the simultaneous presence of a delta4 double bond and saturated carbonyl groups by the separation of hydrogen iodide with a base in an amidic solvent at high temperature. If R2 is a hydrogen atom, the A ring is aromatised after the separation of the hydrogen iodide. Special iodisation processes which also partly permit a stereoselective control of iodisation are used to produce the novel intermediate products.

16. 发明申请

WO1991016039A1 PROCESS FOR THE PREPARATION OF AQUEOUS LIPOSOME SUSPENSIONS CONTAINING ACTIVE SUBSTANCES 审中-公开
标题翻译：制备含活性物质的水性液体悬浮液的方法
公开(公告)号：WO1991016039A1
公开(公告)日：1991-10-31
申请号：PCT/DE1991000294
申请日：1991-04-04
申请人： SCHERING AKTIENGESELLSCHAFT BERLIN UND BERGKAMEN
发明人： SCHERING AKTIENGESELLSCHAFT BERLIN UND BERGKAMEN , Rößling, Georg , SACHSE, Andreas , SCHRÖTER, Hans-Joachim , SPRENGER, Claudia , WAWRETSCHEK, Cornelia
IPC分类号： A61K09/127
CPC分类号： A61K9/1277
摘要： Described is a process for the preparation of aqueous liposome suspensions containing active substances, the suspensions being prepared from a solution of a liposome-forming substance, or mixture of such substances, in a lower alcohol with a maximum of three carbon atoms and an aqueous phase, the active ingredients being dissolved or suspended in the lipid solution and/or the aqueous phase. The process is characterized in that the aqueous phase is incorporated, by mixing, in the alcoholic solution and the lower alcohol removed by vacuum distillation and, if necessary, the liposome suspension freeze-dried.

17. 发明申请

WO1990014329A1 LEUKOTRIENE B4 DERIVATIVES, PROCESS FOR PRODUCING THEM AND THEIR USE AS DRUGS 审中-公开
标题翻译： LEKOTRIENE B4衍生物，生产方法及其作为药物使用
公开(公告)号：WO1990014329A1
公开(公告)日：1990-11-29
申请号：PCT/DE1990000397
申请日：1990-05-25
申请人： SCHERING AKTIENGESELLSCHAFT BERLIN UND BERGKAMEN , SKUBALLA, Werner , BUCHMANN, Bernd , HEINDL, Joseph , FRÖHLICH, Wolfgang , EKERDT, Roland
发明人： SCHERING AKTIENGESELLSCHAFT BERLIN UND BERGKAMEN
IPC分类号： C07C69/18
CPC分类号： C07C403/12 , C07C33/14 , C07C59/46 , C07C59/48 , C07C403/08 , C07C405/0066 , C07C2601/16
摘要： Compounds of formula (I) in which the residues have the following meanings: a is (II) or (III); R is CH2OH, CH3, CF3, COOR with R or, A is a trans, trans-CH=CH-CH=CH- or tetramethylene group; B is an alkylene group with up to 10 C atoms; D is a direct bond, oxygen, sulphur, a -C=C- group or a -CH=CR -group, or (IV); B and D together are a direct bond; R and R are the same or different and denote hydrogen or an organic acid residue with 1 to 15 C atoms; R and R together are a carbonyl group; R is a hydrogen atom or C1-10 alkyl, and, if R denotes a hydrogen atom, their salts with physiologically acceptable bases and their cyclodextrin clathrates.
摘要翻译：式（I）的化合物，其中残基具有以下含义：a是（II）或（III）; R 1是CH 2 OH，CH 3，CF 3，COOR 5，其中R 5或A是反式，反式-CH = CH-CH = CH-或四亚甲基; B是具有至多10个C原子的亚烷基; D是直接键，氧，硫，-C = C-基或-CH = CR 7 - 基或（IV）; B和D一起是直接的联系; R 2和R 3相同或不同，表示氢或具有1至15个C原子的有机酸残基; R 1和R 2一起是羰基; R 4是氢原子或C 1-10烷基，如果R 5表示氢原子，则其与生理上可接受的碱的盐和它们的环糊精包合物。

18. 发明申请

WO1990011276A1 NOVEL PROCESS FOR PRODUCING OPTICALLY ACTIVE BICYCLO [3.3.0] -OCTANE DERIVATIVES 审中-公开
标题翻译：用于生产光学活性双环[3.3.0] - 甲烷衍生物的新方法
公开(公告)号：WO1990011276A1
公开(公告)日：1990-10-04
申请号：PCT/DE1990000219
申请日：1990-03-19
申请人： SCHERING AKTIENGESELLSCHAFT BERLIN UND BERGKAMEN , GAIS, Hans-Joachim , HEMMERLE, Horst
发明人： SCHERING AKTIENGESELLSCHAFT BERLIN UND BERGKAMEN
IPC分类号： C07C405/00
CPC分类号： C07C405/0083 , Y02P20/55
摘要： The invention concerns a process for producing optically active bicyclo [3.3.0]-octane derivatives of formula (I), characterized in that 3-cyclopentylpropine derivatives of formula (II) in which X and R1 have the meanings given are reacted with NaI in the presence of azobisisobutyronitrile and with tributyl tin hydride and acetylated, after the protective group is split off, in the presence of DMAP. The bicyclo [3.3.0]-octane derivatives of formula (III) so obtained are reacted with chloromagnesium copper compounds of formula (IVa) ClMgCu(R4)2 or with the iodine zinc copper compound of formula (IVb) IZnCu(CN)(CH2)3COOCH3.

19. 发明申请

WO1990005720A1 PROCESS FOR PRODUCING CARBACYCLIN DERIVATIVES BY STEREOSELECTIVE INTRODUCTION OF THE 5.6 DOUBLE BOND 审中-公开
标题翻译：通过5.6双重键的简单介绍生产碳水化合物衍生物的方法
公开(公告)号：WO1990005720A1
公开(公告)日：1990-05-31
申请号：PCT/DE1989000730
申请日：1989-11-17
申请人： SCHERING AKTIENGESELLSCHAFT BERLIN UND BERGKAMEN
发明人： SCHERING AKTIENGESELLSCHAFT BERLIN UND BERGKAMEN , HARRE, Michael , WESTERMANN, Jürgen
IPC分类号： C07C405/00
CPC分类号： C07C405/0083
摘要： Process for producing carbacyclins of formula (I) wherein R1 is a straight-chain or branched C1-C7 alkyl group, a straight-chain or branched C2-C7 alkenyl group or a straight-chain or branched C2-C7 alkinyl group, and R2 and R3 can be the same or different and can stand for hydrogen, C1-C2 alkyl, chlorine or bromine or together with the double bond a triple bond, characterized in that a bicyclic ketone of formula (II) wherein R1, R2 an R3 have the above mentioned meanings is reacted with 5-10 equivalents of a reagent of formula (VI) in the presence of 8-10 equivalents of a base at 0-40°C for 0.5 to 4 hours in the solvents dimethoxyethane, 1,3-dimethylimidazolidin-2-one, dimethylformamide, dimethylsulfoxide, tetrahydrofurane, toluol, dibenzo-18-crown-6 or in mixtures thereof.

20. 发明申请

WO1990004566A1 FILLING DEVICE 审中-公开
标题翻译：填充设备
公开(公告)号：WO1990004566A1
公开(公告)日：1990-05-03
申请号：PCT/EP1989001120
申请日：1989-09-26
申请人： SCHERING AKTIENGESELLSCHAFT BERLIN UND BERGKAMEN , SCHIRMACHER, Manfred
发明人： SCHERING AKTIENGESELLSCHAFT BERLIN UND BERGKAMEN
IPC分类号： B67D05/32
CPC分类号： B67D7/0294 , B67D7/0478 , B67D7/34 , B67D7/54 , B67D2007/545 , Y10T137/86332
摘要： Many filling devices used for filling transportable containers with environmentally harmful liquids are unsafe because pollution may occur, in particular, due to faulty operation. Known filling devices which must be connected to exhaust gas disposal installations when filling certain types of liquid are incompletely adapted for use with these installations. The filling device (1) according to the invention is characterized by a valve (24) arranged at the end of a filling pipe (4), an air-release valve (20) and a switch (30). The valves (24, 20) and the switch (30) can be actuated in function of the state of the coupling between the filling device (1) and the pipe socket (2) of a tank container (34). Faulty operation due to incorrect coupling of the filling device (1) is thereby precluded. At the same time, only a minimal volume of exhaust gas needs to be disposed of.
摘要翻译：用于填充具有环境有害液体的可运输容器的许多填充装置是不安全的，因为可能发生污染，特别是由于操作故障。在填充某些类型的液体时必须连接到废气处理设备的已知填充装置不完全适用于这些装置。根据本发明的灌装装置（1）的特征在于设置在灌装管（4）端部的一个阀门（24），一个放气阀（20）和一个开关（30）。可以根据填充装置（1）和储罐容器（34）的管座（2）之间的联接状态来致动阀门（24,20）和开关（30）。因此，排除由于填充装置（1）的错误耦合而导致的操作错误。同时，只需排放最少量的废气。

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