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91. 发明申请

WO1996025392A1 NOVEL BORNEOL DERIVATIVES, METHODS OF MANUFACTURING THEM, AND THEIR PHARMACEUTICAL USE 审中-公开
标题翻译：新BORNEOLDERIVATE，PROCESS FOR THEIR和制药用
公开(公告)号：WO1996025392A1
公开(公告)日：1996-08-22
申请号：PCT/DE1996000297
申请日：1996-02-19
申请人： SCHERING AKTIENGESELLSCHAFT , KLAR, Ulrich , GRAF, Hermann , NEEF, Günter , BLECHERT, Siegfried
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： C07C271/22
CPC分类号： C07D303/16 , C07C271/22 , C07C2603/86
摘要： The invention concerns borneol derivatives of general formula (I), wherein: R represents C(O)-CH(OR )-CH(NR R )-R , C(O)-CH(OR )-CH[NH(C(O)-CH(OR )-CH(NR R )-R )] -R ; R and R are identical or different and the same as R ; R and R are identical or different and the same as R ; R is -C(O)R , -SO2R , -C(O)OR , -C(O)SR , -C(O)NHR , -C(O)NR R , (a), alkyl; R is phenyl; R and R are identical or different and stand for alkyl, cycloalkyl, aryl or aralkyl; R are identical or different and stand for hydrogen, alkyl, aryl, acyl, aralkyl, -SO2R , -P(O) (OH)2; R stands for hydrogen, alkyl, aryl, aralkyl. The invention also concerns salts of the said compounds with physiologically tolerable bases, alpha -, beta - or gamma -cyclodextrine clathrates of the said compounds and compounds of formula (I) encapsulated with liposomes. The compounds are active as tubulin polymerisation antagonists.
摘要翻译：本发明betrfifft Borneolderivate通式（I）其中R <1>（O）-CH（OR <6>）C - CH（NR <7A> - [R <7B>） - R的<8>，C（O） -CH（OR <6>） - CH [NH（（O）-CH（OR <6B>）C - CH（NR <7A> - [R <7B>） - R的<8>）] - R的<8>， [R <6A>，R <6B>是相同的或不同的并且R <6>，R <7A>，R <7B>是相同的或不同的并且R <7>，R <7> -C（O）R <12>，-SO 2 R <12>，-C（O）OR <12>，-C（O）SR <12>，-C（O）NHR <9D>，-C（O）NR <9D>ř <9A>中，（a）烷基，R <8>是苯基，R ，R <12>是相同的或不同的并且是烷基，环烷基，芳基，芳烷基，R <6>是相同的或不同的，是氢烷基，芳基，酰基，芳烷基，-SO 2 R <9C>，-P（O）（OH）指2，R <13>为氢，烷基，芳基，芳烷基，以及与生理上可耐受的碱，以及它们的α它们的盐 - ，β - 或伽马-Cyclodextrinclathrate和平均封装有通式（I）的脂质体的化合物。该化合物作为活性聚合的微管蛋白拮抗剂。

92. 发明申请

WO1996023503A1 PROGESTERONE ANTAGONISTS USEFUL FOR PREPARING MEDICAMENTS FOR TREATING DYSFUNCTIONAL UTERINE BLEEDING 审中-公开
标题翻译：孕激素拮抗剂药物的出血功能失调性子宫出血的治疗PRODUCTION
公开(公告)号：WO1996023503A1
公开(公告)日：1996-08-08
申请号：PCT/EP1995000394
申请日：1995-02-02
申请人： SCHERING AKTIENGESELLSCHAFT , CHWALSZ, Kristof , STÖCKEMANN, Klaus
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： A61K31/57
CPC分类号： A61K31/57 , A61K31/575 , Y10S514/899
摘要： Competitive progesterone antagonists (antigestagenes) are useful to prepare medicaments for treating dysfunctional uterine bleeding (metrorrhagia, menorrhagia, hypermenorrhea).
摘要翻译：有竞争力的孕酮拮抗剂（antigestagens）适合于生产药物用于功能性子宫出血的出血合适的治疗（子宫出血，月经过多，月经过多）。

93. 发明申请

WO1996016928A1 NOVEL SUBSTITUTED DTPA DERIVATIVES, THEIR METAL COMPLEXES, PHARMACEUTICAL COMPOSITIONS CONTAINING THESE COMPLEXES AND THEIR USE IN DIAGNOSIS AND THERAPY 审中-公开
标题翻译：创新取代DTPA衍生物，它们的金属络合物，这种复杂的制药含有它们的它们在诊断和治疗
公开(公告)号：WO1996016928A1
公开(公告)日：1996-06-06
申请号：PCT/EP1995004548
申请日：1995-11-20
申请人： SCHERING AKTIENGESELLSCHAFT
发明人： SCHERING AKTIENGESELLSCHAFT , MAIER, Franz-Karl , BAUER, Michael , KRAUSE, Werner , SPECK, Ulrich , SCHUHMANN-GIAMPIERI, Gabriele , MÜHLER, Andreas , BALZER, Thomas , PRESS, Wolf-Rüdiger
IPC分类号： C07C229/76
CPC分类号： A61K49/04 , A61K49/0002 , A61K49/0004 , A61K49/103 , Y10S514/836 , Y10T436/24
摘要： The invention concerns novel diethylenetriamine pentaacetic acid (DTPA) derivatives, their complexes and complex salts, containing an element of the atomic numbers 20 - 32, 39 - 51 or 57 - 83. The invention further concerns pharmaceutical compositions containing these compounds, their preparation and their use as contrast media and antidotes.
摘要翻译：本发明涉及新的Diethylentriaminpentaessigsäurederivate，它们的复合物和含有原子序数20的元件配盐 - 32 39 - 51或57-83，包含这些化合物的药物组合物，它们的制备和它们作为造影剂和解毒剂的用途。

94. 发明申请

WO1996016677A2 USE OF METAL COMPLEXES AS LIVER AND GALL BLADDER RADIODIAGNOSIS AGENTS IN COMPUTER TOMOGRAPHY 审中-公开
标题翻译：金属络合物的AS肝胆光诊断在计算机使用
公开(公告)号：WO1996016677A2
公开(公告)日：1996-06-06
申请号：PCT/DE1995001644
申请日：1995-11-20
申请人： SCHERING AKTIENGESELLSCHAFT
发明人： SCHERING AKTIENGESELLSCHAFT , MAIER, Franz-Karl , BAUER, Michael , KRAUSE, Werner , SPECK, Ulrich , SCHUHMANN-GIAMPIERI, Gabriele , MÜHLER, Andreas , BALZER, Thomas , PRESS, Wolf-Rüdiger
IPC分类号： A61K49/00
CPC分类号： A61K49/04 , A61K49/0002 , A61K49/0004 , A61K49/103 , Y10S514/836 , Y10T436/24
摘要： Metal complexes consisting of a metal of atomic number 39-42, 44-51 or 56-83, and a complexing agent are used to produce X-ray contrast media for use in enhanced-contrast computed tomography of the liver and the bile ducts.
摘要翻译：使用的，包括原子序数39-42，44-51或56-83的金属和用于生产X射线造影介质用于在肝和胆道对比增强计算机断层摄影中使用的配位剂的金属配合物。

95. 发明申请

WO1996013289A2 PROCESS FOR FILLING WITH A FLUID AND CLOSING DISPOSABLE SYRINGES THAT ARE TO BE STERILISED 审中-公开
标题翻译：填充和与FLUIDEM目录合闸方式，需要消毒的一次性注射器
公开(公告)号：WO1996013289A2
公开(公告)日：1996-05-09
申请号：PCT/DE1995001523
申请日：1995-10-27
申请人： SCHERING AKTIENGESELLSCHAFT , SPECK, Ulrich
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： A61M05/28
CPC分类号： A61M5/34 , A61M5/001 , A61M5/1782 , A61M5/28 , A61M5/3134 , A61M5/315 , A61M5/31505 , A61M5/32 , A61M2005/3104 , A61M2005/3118 , A61M2005/3139 , A61M2005/3279 , A61M2207/00 , B65B3/003
摘要： A process is disclosed for filling with a fluid and closing disposable plastic syringes that are to be sterilised. The disposable syringes have an injection cylinder (11) with a shaped front nozzle part (20), a piston or piston plug (30) in at least one piece and a piston stop element (40) arranged in the area of the cylinder gripping plate (12). After inserting the piston (30) into the empty injection cylinder (11), together or not with its own piston rod, the piston is fully pushed up to the front end of the cylinder. The fluid medium is then fed under pressure into the injection cylinder (11) through the nozzle part (20) and pushes the piston (30) in the direction of the piston rod up to the piston stop element (40). After the syringe is filled, the front area (25) of the nozzle part (20) is closed by plastic deformation. This process allows a previously filled disposable syringe to be sterilised in a standard autoclave without any risk of the syringe inner pressure plastically deforming parts of the syringe.
摘要翻译：本发明涉及一种用于填充密封一个与fluidem内容的方法来进行灭菌由塑料制成的，一次性注射器，其中所述一次性注射器注射器筒（11），其具有前整体形成的喷嘴部分（20），一个至少单件式活塞或柱塞止动件（30）和一个在所述范围内气缸把手板（12）位于活塞止挡元件（40）。所述活塞（30）被完全插入时，插入空的注射器筒（11）具有或不具有其自己的活塞杆到其前端之后。随后，经由注射器筒（11）在喷嘴部（20）压力下的流体介质被按压，其中，所述流体介质推动活塞（30）朝向所述活塞杆侧到活塞止挡元件（40）向前。填充喷嘴部分的前部（25）后（20）由塑性变形封闭。使用本发明的方法中，预填充的一次性注射器可在Standardautoklaven进行灭菌而不会由于内压注射器针筒部件有的塑性变形的危险。

96. 发明申请

WO1996012494A1 COMPETITIVE PROGESTERONE ANTAGONISTS FOR REGULATING FEMALE FERTILITY AS REQUIRED 审中-公开
标题翻译：竞争孕激素拮抗剂需求为导向女性生育控制
公开(公告)号：WO1996012494A1
公开(公告)日：1996-05-02
申请号：PCT/EP1995004191
申请日：1995-10-24
申请人： SCHERING AKTIENGESELLSCHAFT , CHWALISZ, Kristof , STÖCKEMANN, Klaus , SCHMIDT-GOLLWITZER, Karin , KLEMANN, Walter
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： A61K31/56
CPC分类号： A61K31/567 , A61K31/00 , A61K31/569 , A61K31/575 , A61K31/58 , Y10S514/843
摘要： The present invention concerns the novel use of competitive progesterone antagonists in the preparation of a drug for regulating female fertility as required (pill to be taken as required). This drug can be administered in a single dose at any time during the menstrual cycle, its dosage being less than the ovulation-inhibiting dosage.
摘要翻译：本发明描述了用于面向需求的雌性节育药物（按需丸），它可以不考虑施加的月经周期的时间的制造中的新用途的竞争孕酮拮抗剂，所述剂量是在一个单次剂量给药的排卵抑制剂量以下单元。

97. 发明申请

WO1996008563A1 PROCESS FOR MANUFACTURE OF A MODIFIED COLLAGEN-INDUCED PLATELET AGGREGATION INHIBITOR PALLIDIPIN 审中-公开
标题翻译：改性胶原诱导型胶原蛋白抑制剂帕拉地平的制备方法
公开(公告)号：WO1996008563A1
公开(公告)日：1996-03-21
申请号：PCT/EP1995003573
申请日：1995-09-11
申请人： SCHERING AKTIENGESELLSCHAFT , NOESKE-JUNGBLUT, Christiane , BECKER, Andreas , HAENDLER, Bernard
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： C12N15/12
CPC分类号： C07K14/435 , A61K38/00 , C07K2319/02 , Y10S514/822
摘要： The invention provides a process for manufacture of a recombinant protein called Asp-Pallidipin. Asp-Pallidipin inhibits the collagen-induced platelet aggregation of mammalian platelets. The Asp-Pallidipin comprises: (i) a protein (Pallidipin) selected from the group of Pallipin proteins, and (ii) the amino acid aspartic acid, wherein the aspartic acid is connected by a peptide bond with the N-terminal end of Pallidipin. The process comprises the steps aa) transfecting at least one bacterium with an appropriate vector, wherein the vector comprises: (i) a DNA or cDNA coding for the recombinant Asp-Pallidipin, (ii) a suitable signal peptide sequence which signal sequence is cleaved so that the amino acid aspartic acid is in the position +1 of the amino acid sequence seen from the position of the Pallidipin and (iii) a suitable promoter; bb) expressing the preprotein comprising Asp-Pallidipin and the signal sequence; cc) transporting the Asp-Pallidipin from the cytoplasm of the bacterium to the periplasm, cleavage of the preprotein by at least one protease during the transport, producing the Asp-Pallidipin, dd) isolating the Asp-Pallidipin by extracting the periplasm, and ee) purifying the Asp-Pallidipin. The protein is used as a medicament for inhibiting of collagen-induced human platelet aggregation or of cancer with metastatic tumor cells.
摘要翻译：本发明提供了称为Asp-Pallidipin的重组蛋白质的制造方法。 Asp-Pallidipin抑制胶原诱导的哺乳动物血小板血小板聚集。 Asp-Pallidipin包含：（i）选自Pallipin蛋白质的蛋白质（Pallidipin），和（ii）氨基酸天冬氨酸，其中天冬氨酸通过肽键与Pallidipin的N-末端连接。该方法包括步骤aa）用合适的载体转染至少一种细菌，其中载体包括：（i）编码重组Asp-Pallidipin的DNA或cDNA，（ii）信号序列被切割的合适的信号肽序列使得氨基酸天冬氨酸位于从Pallidipin的位置看到的氨基酸序列的位置+1，和（iii）合适的启动子; bb）表达包含Asp-Pallidipin和信号序列的前蛋白; cc）将Asp-Pallidipin从细菌的细胞质转运到周质，在运输期间由至少一种蛋白酶切割前蛋白，产生Asp-Pallidipin，dd）通过提取周质来分离Asp-Pallidipin，ee ）纯化Asp-Pallidipin。该蛋白质用作抑制胶原诱导的人血小板聚集或转移性肿瘤细胞癌的药物。

98. 发明申请

WO1996007645A1 NEW PROCESS FOR PREPARING 1-PHENYL-IMIDAZOLE DERIVATIVES 审中-公开
标题翻译：新方法制备1-苯基 - 咪唑衍生物
公开(公告)号：WO1996007645A1
公开(公告)日：1996-03-14
申请号：PCT/DE1995001228
申请日：1995-09-04
申请人： SCHERING AKTIENGESELLSCHAFT , KIRSTEIN, Holger , NICKISCH, Klaus , NEH, Harribert , HAFFER, Gregor
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： C07D233/90
CPC分类号： C07D233/90
摘要： A new process is disclosed for preparing 1-phenyl-imidazole derivatives having the formula (I), in which R stands for hydrogen, halogen, nitro, cyano, C1-4-alkyl, C1-4-alkoxy, C1-4-alkylthio, C1-4-alkylsulfonyl, amino or a C1-4-alkyl, C1-4-alkanoyl or sulfonyl-monosubstituted or -disubstituted amino group; n equals 1, 2 or 3; R stands for hydrogen, nitro or amino; R stands for C1-6-alkyl; and R stands for hydrogen, C1-6-alkyl or C1-4-alkoxy-C1-2-alkyl. The process is characterised in that optionally R -substituted 2,4-difluoronitrobenzol is reacted with optionally R n-substituted alkali phenolate and an alkaline salt of a compound having formula (II), in which R and R have the above meanings. If desired, the nitro group is then reductively desaminated. Also disclosed are the new compounds having formula (I).
摘要翻译：它是式1-苯基咪唑衍生物的制备的新方法（I），其中R <1>是氢，卤素，硝基，氰基，C1-4烷基，C1-4烷氧基，C1-4烷硫基， C 1-4 - 烷基磺酰基，氨基，或氨基基团单 - 或C 1-4烷基，C 1-4烷酰基或二取代的磺酰基，n是1，2或3，R <2>为氢，硝基或氨基，R <3> C 1-6烷基和R <4>为氢，C 1-6 - 烷基或C 1-4 - 烷氧基-C 1-2 - 烷基，与所描述的，其特征在于，如果适当的话，其中R <2>被取代的2,4-二氟硝基苯任选<1>ñ取代的碱金属酚盐和式（II）的化合物，其中R <3>和R <4>具有上述含义的碱金属盐，与R如果期望反应和，随后还原脱氨基硝基。本发明还涉及式（I）的新化合物。

99. 发明申请

WO1996003154A1 USE OF CHELATES AS X-RAY CONTRAST MEDIUMS 审中-公开
标题翻译： USE螯合物作为X造影剂
公开(公告)号：WO1996003154A1
公开(公告)日：1996-02-08
申请号：PCT/EP1995002901
申请日：1995-07-21
申请人： SCHERING AKTIENGESELLSCHAFT , KRAUSE, Werner , SPECK, Ulrich
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： A61K49/04
CPC分类号： A61K49/06 , A61K49/04
摘要： The invention concerns the use of water-soluble, metal-containing chelates as X-ray contrast mediums, with a synchrotron radiation.
摘要翻译：本发明涉及使用水可溶的，含金属螯合物的如使用同步辐射X射线造影剂。

100. 发明申请

WO1996000207A1 CYCLOHEXANONE DERIVATIVES, METHOD OF PREPARING THEM AND INTERMEDIATES USED IN THE METHOD 审中-公开
标题翻译：环己酮衍生物，工艺为自己的产品和对过程的
公开(公告)号：WO1996000207A1
公开(公告)日：1996-01-04
申请号：PCT/EP1995002274
申请日：1995-06-13
申请人： SCHERING AKTIENGESELLSCHAFT , STEINMEYER, Andreas , NEEF, Günter , MÜLLER, Gunnar , KNÖLKER, Hans-Joachim
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： C07C69/013
CPC分类号： C07C49/647 , C07C43/188 , C07C43/196 , C07C45/29 , C07C45/40 , C07C45/69 , C07C49/497 , C07C49/517 , C07C49/577 , C07C69/013 , C07C251/44 , C07F7/1804
摘要： Described are cyclohexanone derivatives of general formula (I), a method of preparing them and intermediates used in the method.
摘要翻译：有通式（I）环己酮衍生物描述它们的制备方法和该方法的中间产物。

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