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11. 发明申请

WO1991009618A1 COMBINED PREPARATION WITH THROMBOLYTIC ACTION 审中-公开
标题翻译：组合制备与血栓形成的作用
公开(公告)号：WO1991009618A1
公开(公告)日：1991-07-11
申请号：PCT/DE1990000995
申请日：1990-12-21
申请人： SCHERING AKTIENGESELLSCHAFT, BERLIN UND BERGKAMEN
发明人： SCHERING AKTIENGESELLSCHAFT, BERLIN UND BERGKAMEN , DONNER, Peter , SCHLEUNING, Wolf-Dieter
IPC分类号： A61K37/54
CPC分类号： C12N9/6456 , A61K38/00
摘要： The invention concerns a preparation with thrombolytic action, consisting of a combination of the non-fibrin-binding form of the thrombolytic agent v-PA and a fibrin-binding plasminogen activator.

12. 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。

13. 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.

14. 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.

15. 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。

16. 发明申请

WO1990003385A1 11'beta'-PHENYL-14'beta'H-STEROIDS 审中-公开
标题翻译： 11β-PHENYL-14β-H-STEROIDS
公开(公告)号：WO1990003385A1
公开(公告)日：1990-04-05
申请号：PCT/EP1989001090
申请日：1989-09-20
申请人： SCHERING AKTIENGESELLSCHAFT BERLIN UND BERGKAMEN , SCHOLZ, Stefan , NEEF, Günter , OTTOW, Eckhard , ELGER, Walter , BEIER, Sybille , CHWALISZ, Krzysztof
发明人： SCHERING AKTIENGESELLSCHAFT BERLIN UND BERGKAMEN
IPC分类号： C07J43/00
CPC分类号： C07J53/002 , C07J1/0033 , C07J1/0081 , C07J1/0096 , C07J41/0038 , C07J41/0083 , C07J43/003
摘要： New 11 beta -phenyl-14 beta H-steroids of general formula (I), where Z is an oxygen atom or the hydroxyimino-grouping N SIMILAR OH, and M and N are either jointly a second compound or L is a hydrogen atom and M is an alpha -permanent hydroxy group and either A and B together are a second compound and D is a hydrogen atom, where R is a five or six-part heteroalkyl residue or a cycloalkyl, cycloalkenyl or aryl residue or A is a hydrogen atom and B and D together are a methylene bridge, where R besides the aforementioned residues may be a possibly substituted hydrocarbon residue with up to 10 C atoms, a possibly substituted amino group, a hydroxy or C1-8 alkoxy, mercapto or thioalkyl group, R is a methyl or ethyl residue, and R /R represents the usual combination of substituents on the C17 atom in steroid chemistry, having antigestagenic and other properties.
摘要翻译：通式（I）的新的11β-苯基-14β-H-类固醇，其中Z是氧原子或羟基亚氨基基团N-Si OH，M和N是共同的第二种化合物，或L是氢原子， M是α-永久性羟基，A和B一起是第二化合物，D是氢原子，其中R 1是五或六部分杂烷基残基或环烷基，环烯基或芳基，或A是氢原子和B和D一起是亚甲基桥，其中除了上述残基之外，R 1可以是具有至多10个C原子的可能取代的烃残基，可能被取代的氨基，羟基或C 1-8烷氧基，巯基或硫代烷基，R 2是甲基或乙基残基，R 3 / R 4代表类固醇化学中C17原子上的取代基的通常组合，具有抗原原性和其它性质。

17. 发明申请

WO1990002728A2 6-OXO-9-FLUOR-PROSTAGLANDIN DERIVATIVES, PROCESS FOR PRODUCING THEM AND THEIR USE AS DRUGS 审中-公开
标题翻译： 6-OXO-9-FLUOR-PROSTAGLANDIN衍生物，其生产方法及其作为药物使用的方法
公开(公告)号：WO1990002728A2
公开(公告)日：1990-03-22
申请号：PCT/DE1989000588
申请日：1989-09-10
申请人： SCHERING AKTIENGESELLSCHAFT BERLIN UND BERGKAMEN , KLAR, Ulrich , VORBRÜGGEN, Helmut , STÜRZEBECHER, Claus-Steffen , THIERAUCH, Karl-Heinz
发明人： SCHERING AKTIENGESELLSCHAFT BERLIN UND BERGKAMEN
IPC分类号： C07C177/00
CPC分类号： C07C405/00
摘要： The invention concerns 6-oxo-9-fluor-prostaglandin derivatives of formula (I) in which R1 is a COOR2 or CONHSO¿2R?2 residue in which R2 is a C¿5? to C6 cycloalkyl group or a C6 to C12 aryl group or a 5- or 6-membered heterocyclic residue, or if R?1¿ is COOR2, R2 is a hydrogen atom or a free phenacyl or a phenacyl substituted with 1 to 3 halogen atoms; A is an E-configured CH=CH- or -C=C-group; W is a free of functionally modified hydroxymethyl group or a free or functionally modified group (a), in which the OH group in each case can be in the α or β position; D is a straight-chain or branched alkylene group with 1 to 5 carbon atoms or a direct bond; E is a -C=C- group, a C¿2? to C4 alkylene group or a group (b); R?3¿ is a hydrogen atom, a C¿1? to C10 alkenyl group, a C3 to C10 cycloalkyl group or a possibly substituted C6 to C12 aryl group or a 5- or 6-membered heterocyclic group; R?4¿ is a hydrogen atom, a methyl group or a free or functionally modified hydroxy group, and if R2 is a hydrogen atom, their salts with physiologically compatible bases, the α, β or η cyclodextrin clathrates and the liposome-encapsulated compounds of formula (I), a process for producing them and their use as drugs.

18. 发明申请

WO1989000578A1 11'beta'-PHENYL-4,9,15-ESTRATRIENES, THEIR MANUFACTURE, AND PHARMACEUTICAL PREPARATIONS CONTAINING THEM 审中-公开
标题翻译： 11β-PHENYL-4,9,15-ESTRATRIENES，其制造和含有它们的药物制剂
公开(公告)号：WO1989000578A1
公开(公告)日：1989-01-26
申请号：PCT/DE1988000447
申请日：1988-07-15
申请人： SCHERING AKTIENGESELLSCHAFT BERLIN UND BERGKAMEN , OTTOW, Eckhard , HOFMEISTER, Helmut , SCHOLZ, Stefan , NEEF, Günter , ELGER, Walter , BEIER, Sybille , CHWALISZ, Krzysztof
发明人： SCHERING AKTIENGESELLSCHAFT BERLIN UND BERGKAMEN
IPC分类号： C07J01/00
CPC分类号： C07J51/00 , C07J1/0096 , C07J21/006 , C07J41/0083
摘要： New 11 beta -phenyl-4,9,15-estratrienes have general formula (I) where X is an oxygen atom or an N-OH hydroxyimino grouping, R is a hydrogen atom or a methyl group, R is a hydrogen atom, or an alkyl or acyl residue with 1 to 10 carbon atoms, R is a hydrogen atom, a cyanomethyl group, -(CCH2)nCH2Z, where n = 0,1, 2, 3, 4 or 5, Z = -H or -OR , where R is a hydrogen atom or an alkyl or acyl group with 1 to 10 C atoms, or -(CH2)mC=C-Y, where m = 0-2 and Y is a hydrogen, chlorine, fluorine, iodine or bromine atom, an alkyl, hydroxyalkyl, alkoxyalkyl or acyloxyalkyl group with 1 to 10 C atoms, R is a straight-chain or branched-chain, saturated or unsaturated hydrocarbon residue with up to 8 carbon atoms, containing the grouping represented by formula (a), where X is as defined above. The compounds possess antigestagen and antiglucocorticoid properties.
摘要翻译：新的11β-苯基-4,9,15-雌三烯具有通式（I），其中X是氧原子或N-OH羟基亚氨基，R 1是氢原子或甲基，R 2是是氢原子或具有1-10个碳原子的烷基或酰基残基，R 3是氢原子，氰基甲基， - （CCH 2）n CH 2 Z，其中n = 0,1,2,3,4或 5，Z = -H或-OR 5，其中R 5为氢原子或具有1至10个C原子的烷基或酰基，或 - （CH 2）m C = CY，其中m = 0-2 和Y是氢，氯，氟，碘或溴原子，具有1-10个碳原子的烷基，羟基烷基，烷氧基烷基或酰氧基烷基，R 4是直链或支链的饱和或不饱和烃残基含有至多8个碳原子，含有由式（a）表示的基团，其中X如上所定义。这些化合物具有抗老化和抗糖皮质激素特性。

19. 发明申请

WO1988000046A1 MEDICAMENTS WITH DELAYED RELEASE OF ACTIVE INGREDIENT 审中-公开
标题翻译：具有延迟释放活性成分的药物
公开(公告)号：WO1988000046A1
公开(公告)日：1988-01-14
申请号：PCT/DE1987000295
申请日：1987-06-29
申请人： SCHERING AKTIENGESELLSCHAFT BERLIN UND BERGKAMEN , FECHNER, Christian , HÜMPEL, Michael , WINDT-HANKE, Fred , TACK, Johannes
发明人： SCHERING AKTIENGESELLSCHAFT BERLIN UND BERGKAMEN
IPC分类号： A61K09/52
CPC分类号： A61K9/5026 , A61K9/5078
摘要： Medicaments with delayed release of the active ingredient, containing a poorly water-insoluble active ingredient and additives, characterized in that the active ingredient is distributed in or on pellets in a microcrystalline or molecularly dispersed form, and that said pellets are coated with a permeable membrane which delays the release of the active ingredient.

20. 发明申请

WO1993001185A1 2,14-DISUBSTITUTED ERGOLINES, THEIR PRODUCTION AND USE IN MEDICAMENTS 审中-公开
标题翻译： 2,14-消除性胆固醇，其生产和用于药物
公开(公告)号：WO1993001185A1
公开(公告)日：1993-01-21
申请号：PCT/DE1992000569
申请日：1992-07-09
申请人： SCHERING AKTIENGESELLSCHAFT BERLIN UND BERGKAMEN , SAUER, Gerhard , WACHTEL, Helmut , LÖSCHMANN, Peter-Andreas
发明人： SCHERING AKTIENGESELLSCHAFT BERLIN UND BERGKAMEN
IPC分类号： C07D457/12
CPC分类号： C07D457/12
摘要： The description relates to 2,14-disubstituted ergolines of formula (I) in which R, R?2, R6, R14¿ and X have the meanings shown in the application, and their production and use in medicaments.

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