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81. 发明申请

WO2001066154A2 RADIOACTIVELY LABELED EPOTHILONE DERIVATIVES, METHOD FOR THE PRODUCTION THEREOF, AND THEIR BIOCHEMICAL AND PHARMACEUTICAL USE 审中-公开
标题翻译：放射性注明埃博霉素衍生物，进程中为其及其生化和制药用
公开(公告)号：WO2001066154A2
公开(公告)日：2001-09-13
申请号：PCT/EP2001002699
申请日：2001-03-09
申请人： SCHERING AKTIENGESELLSCHAFT , KLAR, Ulrich , GAY, Jürgen , SKUBALLA, Werner , SCHWEDE, Wolfgang , BUCHMANN, Bernd , BUNTE, Thomas , LICHTNER, Rosemarie
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： A61K51/00
CPC分类号： A61K51/0455 , A61K51/0453
摘要： The invention relates to novel radioactively labeled pharmacologically effective epothilone derivatives of general formula (I), wherein: R1 represents O-PG and hydroxyl, wherein PG is a protective group; R2a, R2b are the same or different and represent, independent of one another, hydrogen C1-C10 alkyl, aryl, C7-C20 aralkyl or, together, represent a (CH2)m group, wherein m is equal to 1, 2, 3, 4 or 5; R3 represents a C2-C10 alkyl group, a C2-C10 alkenyl group or a C8-C20 aralkyl each containing 2n tritium atoms, wherein n equals 1 or 2; R4 represents O-PG and hydroxyl; R5 represents hydrogen C1-C10 alkyl, aryl, C7-C20 aralkyl and halogen; W-Z represents a CH2-CH2, CH2-O or O-CH2 group; R6 represents hydrogen, C1-C10 alkyl, aryl, C7-C20 aralkyl, (CH2)s-V and halogen, wherein s equals 1, 2, 3 or 4 and V represents O-PG, hydroxyl or halogen; R7, R8 each represent a hydrogen atom and, together, represent an additional bond or an oxygen atom; A represents aryl, C7-C20 aralkyl, and a group R10-CH=C9-, wherein R9 represents hydrogen, halogen, CN, C1-C20 alkyl, aryl, and C7-C20 aralkyl, and R10 represents hydrogen, C1-C20 alkyl-, aryl-, C7-C20 aralkyl, and; X-Y represents an O-C(=O), an O-CH2, a CH2-C(=O), an NR11-C(=O) and an NR11-SO2 group, wherein R11 represents hydrogen and C1-C10 alkyl. The novel compounds of formula (I) are valuable pharmaceuticals and valuable diagnostic probes for elucidating, for example, active mechanisms and biochemical, pharmacocinketic and/or pharmacodynamic processes.
摘要翻译：本发明涉及通式的新颖放射性标记的药理学活性的埃坡霉素衍生物，其中R <1> O型PG，羟基，其中PG是保护基，R <2A>，R <2B>是相同的或不同的，并独立地氢，C1-C10烷基，芳基，C7-C20芳烷基，或一起为 - （CH 2）M组，其中m是1，2，3，4或5，R <3> C 2 -C 10 - 烷基，C2-C10链烯基或C 8 -C 20 - 芳烷基，各自含有的2n氚原子，其中n是1或2，R <4> O型PG，羟基，R <5>为氢，C1-C10-烷基，芳基，C7-C20芳烷基，卤素，WZ一个CH2-CH2，CH2-O或O-CH 2基团，R <6>是氢，C1-C10烷基，芳基，C7-C20芳烷基，（CH 2）SV，卤素，其中s为1，2，3或4和V O型PG，是羟基或卤素，R <7> - [R <8>是氢原子，一起附加的键或氧原子，a为芳基，C7-C20 芳烷基，基团R <10> -CH = CR <9> - ，其中R <9>为氢，卤素，CN，C1-C20烷基，芳基，C7-C20芳烷基，并且R <10>为氢，C 1 -C C20 是烷基，芳基，C7-C20芳烷基，一个XY OC（= O），O-CH 2，CH 2 C（= O），NR <11> -C（= O），NR <11> -SO 2基团，其中R <11>为氢，C1-C10烷基，式bedeuten.Die新化合物是有价值的药物和用于作用机制的阐明有价值的诊断探针，例如，生物化学，药代动力学和/或药效学过程。

82. 发明申请

WO2000049020A2 NOVEL EPOTHILON DERIVATIVES, METHOD FOR THE PRODUCTION THEREOF AND THEIR PHARMACEUTICAL APPLICATION 审中-公开
标题翻译：新型爱替酮衍生物，其制备方法及其药物应用
公开(公告)号：WO2000049020A2
公开(公告)日：2000-08-24
申请号：PCT/EP2000001332
申请日：2000-02-18
申请人： SCHERING AKTIENGESELLSCHAFT , KLAR, Ulrich , SCHWEDE, Wolfgang , BUCHMANN, Bernd , SKUBALLA, Werner , SCHIRNER, Michael , GRIMM, Michael
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： C07D493/00
CPC分类号： C07D417/06 , Y02P20/55
摘要： The invention relates to novel epothilon derivatives of general formula (I), wherein the substituents Y, Z, R1a¿, R1b¿, R2a¿, R2b¿, R3a¿, R3b¿, E, R5¿, R6¿, R7¿, R8¿, R14¿ and X have the meanings cited more specifically in the description. The novel compounds interact with tubulin by stabilizing the formed microtubuli. The compounds are able to influence the cell division in a phase-specific manner and are suited for treating malignant tumors, for example, ovarian cancer, gastric carcinoma, colon cancer, breast cancer, lung cancer, head and neck cancer, malignant melanoma, and acute lymphocytic and myelocytic leukemia. The inventive compounds are suited for use in anti-angiogenic therapy as well as for treating chronic inflammatory diseases (psoriasis, arthritis). In order to prevent uncontrolled cell proliferations and to improve the compatibility of medical implants, the inventive compounds can be applied or incorporated in polymeric materials. The inventive compounds can be used alone or, in order to achieve additive or synergistic effects, in conjunction with additional constituents and substance classes which can be use in tumor therapy.
摘要翻译：本发明涉及通式（I）的新型埃博霉素衍生物，其中取代基Y，Z，R 1a和取代基R 1b和取代基R 2a和取代基R 2b和取代基R 3a和取代基R 3b和取代基E， ;，R6＆Iquest; R7＆Iquest; R8＆Iquest; R14＆Iquest; 和X具有在说明书中更具体引用的含义。新化合物通过稳定形成的微管与微管蛋白相互作用。这些化合物能够以相特异性方式影响细胞分裂，并且适用于治疗恶性肿瘤，例如卵巢癌，胃癌，结肠癌，乳腺癌，肺癌，头颈癌，恶性黑素瘤和急性淋巴细胞和粒细胞白血病。本发明化合物适用于抗血管生成疗法以及治疗慢性炎症疾病（牛皮癣，关节炎）。为了防止不受控制的细胞增殖并改善医用植入物的相容性，可以将本发明的化合物应用或掺入聚合物材料中。本发明的化合物可以单独使用，或者为了实现累加或协同效应，可以与可用于肿瘤治疗的其他成分和物质类别结合使用。

83. 发明申请

WO1998028322A1 BISSTEROIDAL COMPOUNDS AND THEIR USE FOR THE PREPARATION OF CHIRAL COMPLEXES 审中-公开
标题翻译：双组分化合物及其用于制备复合物的用途
公开(公告)号：WO1998028322A1
公开(公告)日：1998-07-02
申请号：PCT/EP1997007098
申请日：1997-12-18
申请人： SCHERING AKTIENGESELLSCHAFT , MOHR, Jörg-Torsten , ENEV, Valentien , EWERS, Christian , HARRE, Michael , HICKISCH, Klaus
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： C07J01/00
CPC分类号： C07J31/006 , C07J1/0055 , C07J1/0077 , C07J51/00
摘要： Bissteroidal compounds of general formula (I), in which R1 stands for hydrogen, alkyl, acyl, fluorine, and X1R5, where X1 stands for oxygen and sulfur and R5 can either be hydrogen, alkyl, aryl; R2 stands for hydrogen and alkyl; the stereochemistry of C-13, C-14 and C-17 may either be a or b; X stands for oxygen, hydroxyl, trifluormethylsulfonyloxy, or (R6)2P, where R6 can be aryl, alkyl and cycloalkyl; R3 stands for hydrogen, alkyl, aryl, trialkylsilyl, fluorine and X2R6, where X2 stands for oxygen and sulfur and R6 stands for hydrogen, trifluormethylsulfonyl, alkyl, cycloalkyl or aryl. R4 can either be a substituent in the 6 or 7 position of the steroid with the meaning of hydrogen, alkyl, aryl, fluorine, and X3R7, where X3 stands for oxygen, sulfur or trialkylsilyl and R7 stands for hydrogen, trifluormethylsulfonyl, alkyl or aryl, and the B-ring of the steroid contains none or two double bonds. Enantio- and Diastereomeric derivatives of compounds of general formula (I), metal complexes thereof and their use in enantioselective reactions.
摘要翻译：通式（I）的双星型化合物，其中R1代表氢，烷基，酰基，氟和X1R5，其中X1代表氧和硫，R5可以是氢，烷基，芳基; R2代表氢和烷基; C-13，C-14和C-17的立体化学可能是a或b; X代表氧，羟基，三氟甲基磺酰氧基或（R6）2P，其中R6可以是芳基，烷基和环烷基; R3代表氢，烷基，芳基，三烷基甲硅烷基，氟和X2R6，其中X2代表氧和硫，R6代表氢，三氟甲基磺酰基，烷基，环烷基或芳基。 R4可以是类固醇6或7位的取代基，具有氢，烷基，芳基，氟和X3R7的含义，其中X3表示氧，硫或三烷基甲硅烷基，R7表示氢，三氟甲磺酰基，烷基或芳基，并且类固醇的B环含有无或两个双键。通式（I）化合物的对映异构体和非对映体衍生物，其金属络合物及其在对映选择性反应中的用途。

84. 发明申请

WO1998023634A1 CYCLOALKYL STEROIDS, METHOD FOR THE PRODUCTION THEREOF, PHARMACEUTICAL PREPARATIONS CONTAINING SAME CYCLOALKYL STEROIDS AND THE USE THEREOF AS MEDICAMENTS 审中-公开
标题翻译： CYCLOALKYLSTEROIDE，加工生产这些CYCLOALKYLSTEROIDE药物制剂和它们在药品生产
公开(公告)号：WO1998023634A1
公开(公告)日：1998-06-04
申请号：PCT/EP1997006542
申请日：1997-11-24
申请人： SCHERING AKTIENGESELLSCHAFT , KASCH, Helmut , SCHÖLLKOPF, Klaus , FRITZEMEIER, Karl-Heinrich , KRATTENMACHER, Rolf , MUHN, Hans-Peter
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： C07J53/00
CPC分类号： C07J53/002
摘要： Novel 16 alpha , 17 alpha carbocylic steroids of general formula (I), wherein R =C2-C5 alcanoyl, but not acetyl, when R and R both mean a hydrogen atom, C2-C5-(1-hydroxy)-alkyl, C2-C5 -(1-aroyloxy)-alkyl, C2-C5-(1-C1-C5-alkanoyloxy)-alkyl, C2-C5-1(aroyloxy)-alkyl, C2-C5-(1-aroyloxy)-alkyl, C2-C5-(2-hydroxy)-alcanoyl, cyano, (hydroxyamino)-carbonyl, (C1-C5-alcoxyamino)-carbonyl, C1-C5-(1 hydroxyimino)-alkyl, C1-C5-(1-C1-C5-alcoxyimino)-alkyl, C1-C5-(1-C1-C5- alkylimino)-alkyl, C1-C5-(1-C1-C5-alkanoyloximino)-alkyl, C1-C5-(1-alkylaminocarbonyloxy)-alkyl, C2-C5-(1-arylaminocarbonyloxy)-alkyl, R =methyl or ethyl, R , R , R mean individually a hydrogen atom or a methyl group, C -C mean a C-C- single or double bond, X means 2 hydrogen atoms, a hydrogen atom and a hydroxy group, a radical of formula -S-(CH2)n-S- with n=2,3,4 or 5, an oxygen atom, a hydroxyimino-, C1-C6-alcoxy-, C1-C6-alcanoyl, C1-C6 alcoxycarbonylimino, C1-C6-alcoxyimimino, C1-C6-alcoxycarbonyloximino- or a C1-C6 alkanoyloximino group. The invention also describes a method for the production thereof. The compounds of formula (I) exhibit high progestogenic efficiency, and are suitable for the production of medicaments.
摘要翻译：有通式I，其中R，如果R <2 '>和R <3'>是<17> = C2-C5烷酰基，但不乙酰基，各自代表氢原子的新的16α，17的α-碳环甾族化合物， C2〜C5的（1-羟基）烷基，C2〜C5的（1-C1-C5烷氧基）烷基，C2〜C5的（1-C 1 -C 5烷酰氧基）烷基，C2〜C5的（1 芳酰氧基）烷基，C2〜C5的（2-羟基）烷酰基，氰基，（羟氨基）羰基，（C1-C5烷氧基）羰基，C1-C5（1-羟基亚氨基）烷基，C 1 -C C5（1-C 1 -C 5烷氧基亚氨基）烷基，C1-C5（1-C 1 -C 5烷基亚氨基）烷基，C1-C5（1-C1-C5-Alkanoyloximino）烷基，C1-C5 （1-烷基氨基羰）烷基，C1-C5（1- arylaminocarbonyloxy）烷基，R <13> =甲基或乙基，R <2 '>，R <3'>，R <4“>独立地为氢原子，意味着或甲基，C <2“> - Visual C <3”>是CC单键或双键，X代表两个氢原子，一个氢原子和一个羟基基团，一个基团的式-S-（CH 2）n的S-，其中n = 2 ，3，4或5，氧原子，羟基亚，C1-C6烷氧基，C1-C6烷酰基，C1-C6-Alkoxyca rbonylimino-，C1-C6烷氧基亚，C1-C6-Alkoxycarbonyloximino-或C1-C6-Alkanoyloximinogruppe装置描述以及它们的制备方法。式I的化合物具有很强的促孕活性和适用于药物的制备。

85. 发明申请

WO1998007730A1 TIN DENDRIMERS, THEIR USE AS X-RAY CONTRAST AGENTS AND PROCESSES FOR THEIR PREPARATION 审中-公开
标题翻译： ZINNDENDRIMERE，其作为X射线造影剂和工艺用自己的
公开(公告)号：WO1998007730A1
公开(公告)日：1998-02-26
申请号：PCT/DE1997001821
申请日：1997-08-18
申请人： SCHERING AKTIENGESELLSCHAFT , KRAUSE, Werner , SCHUMANN, Herbert
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： C07F07/22
CPC分类号： C07F9/5009 , A61K49/0002 , A61K49/04 , C07F7/2208
摘要： The invention concerns dendrimeric organometallic tin compounds (tin dendrimers) which can advantageously be used as X-ray contrast agents. The invention also concerns processes for their preparation.
摘要翻译：本发明涉及有机金属树枝状锡化合物（Zinndendrimere），其可以有利地用作X-射线造影剂和它们的制备方法。

86. 发明申请

WO1998005366A1 TERMINAL STERILISATION PROCESS FOR FILLED SYRINGES UNDER AN AUXILIARY PRESSURE 审中-公开
标题翻译：法支护压力充式注射器的最终灭菌
公开(公告)号：WO1998005366A1
公开(公告)日：1998-02-12
申请号：PCT/DE1997001671
申请日：1997-08-01
申请人： SCHERING AKTIENGESELLSCHAFT , KOLBERG, Reiner
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： A61L02/04
CPC分类号： A61L2/20 , A61L2/04 , A61L2/07 , A61L2/12 , A61M5/24 , A61M2005/3123
摘要： A process is disclosed for manufacturing a previously filled, sterile syringe. The syringe has a syringe body (2) with a proximal (5) and a distal end, a syringe outlet at its distal end, a closure, a stopper (8), a fluid and a gaseous medium. The fluid medium is a contrasting agent. The process has the following steps: a syringe body (2) sealed by a closure at its distal outlet is filled through its proximal end (5). A compression device (1) introduces the stopper (8) into the proximal end (5) of the syringe body (2) and extracts air from the syringe body (2) through needles (6). The piston is lowered into the syringe body (2) and the compression device (1) is removed therefrom. Finally, the syringe is treated by autoclave in a sterilisation chamber.
摘要翻译：本发明包括一种制造预填充，无菌注射器的方法。注射器包括注射器本体（2）具有近端（5）和远端，在其远端的注射器出口件，封闭，插塞（8）和一个流体和气态介质。流体介质是造影剂。该方法包括以下步骤：a注射器本体（2），其已经被密封在与闭合远端注射器出口，穿过近侧端（5）被填充。一种压缩装置（1）承载在近端插头（8）所述注射器本体（5）（2）。在这种情况下，由压缩装置（1）通过针（6）的空气从注射器主体（2）的装置抽吸。将烧瓶被留在注射器本体（2），压缩装置（1）被取出。然后将注射器在一个消毒腔室高压灭菌。

87. 发明申请

WO1997040020A1 PHTHALAZINE DERIVATIVES, THEIR PREPARATION AND THEIR USE AS DRUGS 审中-公开
标题翻译：酞嗪，生产与应用，药物
公开(公告)号：WO1997040020A1
公开(公告)日：1997-10-30
申请号：PCT/DE1997000828
申请日：1997-04-22
申请人： SCHERING AKTIENGESELLSCHAFT , OTTOW, Eckhard , HUTH, Andreas , NEUHAUS, Roland , SCHNEIDER, Herbert , TURSKI, Lechoslaw , DYRKS, Thomas
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： C07D237/30
CPC分类号： C07D237/30
摘要： Described are compounds of formula (I), their preparation and their use as drugs.
摘要翻译：是式（I），它们的制备的化合物及其作为药物的用途。

88. 发明申请

WO1997026862A2 IMPROVED CONCENTRATED INJECTION AND INFUSION SOLUTIONS FOR INTRAVENOUS ADMINISTRATION 审中-公开
标题翻译：改进的浓注射液和输注液为应用血管内
公开(公告)号：WO1997026862A2
公开(公告)日：1997-07-31
申请号：PCT/DE1997000170
申请日：1997-01-27
申请人： SCHERING AKTIENGESELLSCHAFT , SPECK, Ulrich , SCHUHMANN-GIAMPIERI, Gabriele , MUSCHICK, Peter , KRAUSE, Werner
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： A61K09/08
CPC分类号： A61K49/0452 , A61K9/0019 , A61K45/06 , A61K47/02 , A61K47/183
摘要： The description relates to additives for concentrated injection and infusion solutions which prevent or reduce acute or delayed oversensitivity reactions and injection and infusion solutions containing said additives.
摘要翻译：有添加剂浓缩注射和输注的解决方案，避免急性或延迟性的过敏反应或减少以及含有这些添加剂描述的注射和输注溶液。

89. 发明申请

WO1997025305A1 NOVEL MONOFUNCTIONALISED EDTA, DTPA AND TTHA DERIVATIVES AND THEIR USE IN MEDICAL DIAGNOSIS AND THERAPY 审中-公开
标题翻译： NEW单官能EDTA，DTPA和TTHA衍生物和它们在医疗诊断和治疗
公开(公告)号：WO1997025305A1
公开(公告)日：1997-07-17
申请号：PCT/DE1996002476
申请日：1996-12-20
申请人： SCHERING AKTIENGESELLSCHAFT , PLATZEK, Johannes , MARESKI, Peter , NIEDBALLA, Ulrich , RADÜCHEL, Bernd
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： C07C229/16
CPC分类号： C07C229/16 , C07C2601/14
摘要： The invention relates to novel monofunctionalised ethylene diamine tetracetic acid, diethylene triamine pentacetic acid and triethylene tetramine hexacetic acid derivatives, their production and their use in the production of pharmaceutical agents.
摘要翻译：本发明涉及新的单官能化的乙二胺四乙酸，三亚乙基四胺和酸衍生物Diethylentriaminpentaessigsäure-，其制备方法及其用于制备药物组合物的用途。

90. 发明申请

WO1997019066A1 NEW QUINOXALINDIONE DERIVATIVES, THEIR PREPARATION AND USE IN MEDICAMENTS 审中-公开
标题翻译：新喹喔啉衍生物，生产和使用药物
公开(公告)号：WO1997019066A1
公开(公告)日：1997-05-29
申请号：PCT/DE1996002227
申请日：1996-11-15
申请人： SCHERING AKTIENGESELLSCHAFT , HUTH, Andreas , KRÜGER, Martin , OTTOW, Eckhard , SEIDELMANN, Dieter , NEUHAUS, Roland , SCHNEIDER, Herbert , TURSKI, Lechoslaw
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： C07D241/44
CPC分类号： C07D241/44 , C07F9/650994
摘要： New quinoxalindone derivatives are disclosed having formula (I), in which R , R , R and R have the meanings given in the description, as well as their preparation and use in medicaments.
摘要翻译：有（I）其中，R <1>，R <5> - [R <6>和R <7>已经在应用程序中所示的含义描述它们的制备和在药物中使用的式新喹喔啉二酮衍生物。

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