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1. 发明申请

WO1997023245A1 CASCADE POLYMER COMPLEXES, PROCESS FOR PRODUCING THE SAME AND PHARMACEUTICALS CONTAINING THE SAME 审中-公开
标题翻译： CASCADE聚合物复合，方法用于生产和制药含
公开(公告)号：WO1997023245A1
公开(公告)日：1997-07-03
申请号：PCT/EP1996005315
申请日：1996-11-29
申请人： SCHERING AKTIENGESELLSCHAFT , SCHMITT-WILLICH, Heribert , PLATZEK, Johannes , RADÜCHEL, Bernd , Weinmann, Hanns-Joachim , EBERT, Wolfgang , MISSELWITZ, Bernd , MÜHLER, Andreas , FRENZEL, Thomas
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： A61K49/00
CPC分类号： A61K49/085 , A61K49/04 , A61K49/124 , Y10S514/836
摘要： Cascade polymer complexes contain: (a) complexing ligands of general formula (I), in which A stands for a nitrogenated cascade core of basic multiplicity a; X and Y independently represent a direct bond or a cascade reproduction unit of reproduction multiplicity x or y; Z and W independently represent a cascade reproduction unit of reproduction multiplicity z or w; K stands for a complexing agent residue; a equals 2 to 12; x, y, z and w independently represent the integers 1 to 4, provided that at least two reproduction units be different, that 16
摘要翻译：包括级联聚合物络合物A）络合物形成通式（I），其中A是碱多个一个的含氮级联核，X和Y独立地独立地表示直接键合或再现多重x或y，Z和W的级联再现单元的配位体彼此，再现多重Z或W的级联再现单元的，K是基团络合剂，支架为数字2〜12，X，Y，Z和W彼此独立地编号1〜4中，其前提是至少两个是，对于多重的产品应用于不同的再现单元16

2. 发明申请

WO1995017451A1 METAL COMPLEXES OF DENDRIMERIC MOLECULES, DIAGNOSTIC AGENTS CONTAINING THEM AND PROCESS FOR PRODUCING THE COMPLEXES AND AGENTS 审中-公开
标题翻译：树枝状高分子的金属络合物包含诊断剂及其制备方法的复杂性和MEANS
公开(公告)号：WO1995017451A1
公开(公告)日：1995-06-29
申请号：PCT/EP1994004016
申请日：1994-12-02
申请人： SCHERING AKTIENGESELLSCHAFT , SCHMITT-WILLICH, Heribert , PLATZEK, Johannes , MÜHLER, Andreas , FRENZEL, Thomas
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： C08G85/00
CPC分类号： A61K49/124 , A61K51/04 , B82Y5/00 , C08G73/0206 , C08G73/06 , C08G83/00
摘要： The invention relates to novel metal complexes of dendrimeric macromolecules containing 8 to 64 ions of an element of atomic number the 21-29, 39, 42-44 or 57-83 and a polymeric, complex-forming ligand of formula (I) A-(X)b, in which A, X and b have different meanings, agents containing these compounds and their use in diagnosis. The invention also relates to a process for producing the complexes and agents.
摘要翻译：本发明涉及一种含有8至64离子原子序数21-29，39，42-44，或57-83和聚合物，式配位体形成配合物的（I）A-（X）B的一个元素的树枝状大分子的新的金属配合物，在有A，X和b具有不同的含义，这些化合物含有-以及在诊断中使用的这些。本发明还涉及一种用于复合物和试剂的制备方法。

3. 发明申请

WO1994017029A1 DERIVATED DTPA COMPLEXES, PHARMACEUTICALS CONTAINING THESE COMPOUNDS, THEIR USE AS NMR- AND RADIOGRAPHIC CONTRASTING AGENTS AND PROCESS FOR PRODUCING THE SAME 审中-公开
标题翻译：衍生化DTPA络合物，含有它们的制药，其作为核磁共振和X射线造影剂和方法使用其
公开(公告)号：WO1994017029A1
公开(公告)日：1994-08-04
申请号：PCT/EP1994000033
申请日：1994-01-08
申请人： SCHERING AKTIENGESELLSCHAFT , SCHMITT-WILLICH, Heribert , PLATZEK, Johannes , GRIES, Heinz , RADÜCHEL, Bernd , PETROV, Orlin , MÜHLER, Andreas , FRENZEL, Thomas , VOGLER, Hubert , BAUER, Hans , NICKISCH, Klaus , HILSCHER, Jean-Claude
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： C07C229/16
CPC分类号： A61K49/06 , C07C229/16 , C07C229/76 , Y10S514/836 , Y10T436/24
摘要： Complex compounds and their salts consist of at least one metal ion and a complexing agent having general formula (I), in which Z and Z represent independently from each other a hydrogen atom, the residue -(CH2)m-(C6H4)q-(O)k-(CH2)n-(C6H4)l-(O)r-R, or the residue -(CH2)m-(C6H10)q-(O)k-(CH2)n-(C6H10)l-(O)r-R, in which m and n are the numbers 0-5, q, k, l and r are the numbers 0 or 1 and s is the number 1 or 2; R stands for a hydrogen atom, an if required OR - substituted, straight-chain or branched-chain C1-C6-alkyl residue or a CH2-COOR group, in which R stands for a hydrogen atom, a C1-C6-alkyl residue or a benzyl group, with the proviso that one of the substituents Z or Z stands for a hydrogen atom and the other does not, and that a direct oxygen-oxygen bond is not allowed. Also disclosed is their use for producing radiotherapy agents and NMR and radiographic diagnosing agents, in particular for contrasting the hepatobiliary system. A process for producing these compounds and agents is further disclosed.

4. 发明申请

WO1996001655A1 CASCADE-POLYMER COMPLEXES AND METHODS OF PRODUCING THE SAME 审中-公开
标题翻译： CASCADE聚合物复合和方法
公开(公告)号：WO1996001655A1
公开(公告)日：1996-01-25
申请号：PCT/EP1995002577
申请日：1995-07-04
申请人： SCHERING AKTIENGESELLSCHAFT , SCHMITT-WILLICH, Heribert , PLATZEK, Johannes , NIEDBALLA, Ulrich , RADÜCHEL, Bernd , MÜHLER, Andreas , FRENZEL, Thomas , EBERT, Wolfgang
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： A61K49/00
CPC分类号： A61K49/04 , A61K38/00 , A61K49/085 , A61K49/124 , C07C237/12 , C07C271/22 , C07D251/64 , C07D257/02 , C07K5/0215 , Y10S424/16
摘要： The proposed cascade-polymer complexes contain the following components: (a) complex-forming ligands of the general formula (I): A-{X-[Y-(Z- z)y]x}a, wherein A represents a nitrogen-containing cascade nucleus of base multiplicity a; X and Y independently of each other represent a direct bond or a cascade reproduction unit of reproduction multiplicity x or y; Z and W independently of each other represent a cascade reproduction unit of reproduction multiplicity z or w; K represents a complexing agent group; a is an integer between 2 and 12; x, y, z, and w independently of each other represent integers between 1 and 4; a condition being that at least two reproduction units are different and the product of the multiplicities must be such that 16 x y z w
摘要翻译：级联聚合物络合物包括（a）形成络合物的通式（I）的配体A- {X- [Y-（Z- Z）Y] x}一个，其中A是碱多个一个的含氮级联核，X和Y独立地是直接键或再现多重x或y，Z和W彼此独立地级联再现单元，再现多重的z或瓦特级联再现单元，K是基团络合剂，a表示数2〜12， X，Y，Z和W彼此独立地的，代表数字1至4，条件是至少两个再现单元是不同的，且为多重，16

5. 发明申请

WO1996035456A2 USE OF POLYMERIC CONTRAST AGENTS OF MEDIUM MOLECULAR WEIGHT FOR DIFFERENTIATING BETWEEN BENIGN AND MALIGNANT TUMOURS USING MODERN IMAGING TECHNIQUES 审中-公开
标题翻译： FOR造影剂聚合物的使用AVERAGE分化的良性和恶性肿瘤的分子量是指现代成像方法
公开(公告)号：WO1996035456A2
公开(公告)日：1996-11-14
申请号：PCT/EP1996001740
申请日：1996-04-26
申请人： SCHERING AKTIENGESELLSCHAFT , SCHMITT-WILLICH, Heribert , PLATZEK, Johannes , MÜHLER, Andreas , ADAM, Gerhard , GÜNTHER, Rolf
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： A61K49/00
CPC分类号： A61K49/12 , A61K49/085 , A61K49/124
摘要： It has been found surprisingly that by using metal complex-conjugates with a polymeric basic structure and a mean molecular weight of between 10,000 and 40,000 dalton, it is possible to otbtain excellent differentiation between malignant and benign tumours in areas of the body without a blood-brain barrier. Contrast agents of this type not only permit reliable differentiation between malignant and benign tumours, they are also characterised by the fact that they can be completely eliminated from the body and thus have good tolerability. Suitable metal complex-conjugates with a polymeric basic structure and a means molecular weight in the range indicated above are disclosed in the German patent applications DE 39 38 992 and DE 195 25 924, as well as in the US patents US 5,338,532; 4,507,466; 4,631,337; 4,587,329; 4,568,737 and 4,507,466. Such polymeric basic structures are referred to as cascades or dendrimers, and contrast agents containing conjugates of these polymers with metal complexes can be referred to as cascade or dendrimeric contrast agents. Preference is given in particular to metal complex-conjugates carrying between 24 and 36 paramagnetic metal complexes, in particular metal complexes of gadolinium, at the end-position groups of the polymeric basic structure.
摘要翻译：已经发现，使用金属络合物时缀合物在身体区域良性和恶性肿瘤的无血 - 脑屏障优异的分化是可能的聚合物主链和在10,000至40,000道尔顿的平均分子量，令人惊讶的。这样的对比剂不仅可以让恶性和良性肿瘤的可靠分化，他们的特点是，除其他外，此外，特征还在于，它们完全从体内排出，因而是良好耐受的。与聚合物主链和在上述范围内的平均分子量的合适的金属配合物的结合物是关节内在德国专利申请DE 39 38 992和DE 195 25 924和在美国专利5338532; 4,507,466; 4631337; 4,587,329; 4568737和4507466中描述。这样的聚合物主链也称为含或这些聚合物与金属络合物作为级联，或树突状造影剂的级联树枝状聚合物造影剂的缀合物。特别是金属的复共轭，所述顺磁性与聚合物骨架24至36的金属配合物的末端基团，在钆的特定的金属配合物，磨损是优选的。

6. 发明申请

WO1998001163A2 PSEUDOPOLYROTAXANES 审中-公开
标题翻译： pseudopolyrotaxanes
公开(公告)号：WO1998001163A2
公开(公告)日：1998-01-15
申请号：PCT/EP1997003344
申请日：1997-06-25
申请人： SCHERING AKTIENGESELLSCHAFT , PLATZEK, Johannes , SCHMITT-WILLICH, Heribert
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： A61K49/00
CPC分类号： A61K49/12 , A61K49/04 , A61K49/0442 , A61K49/085 , C08B37/0015 , C08L71/02 , Y10S514/836 , C08L2666/26
摘要： The invention concerns novel pseudopolyrotaxanes which contain metal complexes or iodine-containing benzene derivatives and are valuable compounds for diagnostic purposes. The pseudopolyrotaxane complexes have the general formula (I), in which n designates the numbers 6, 7 or 8, m designates the numbers 2 to 50; X is a direct bond or the group -O-CO-CH(CH3)-; R1 and Y have the meanings given in the description; and R3-Y-R4 are polyalkylene glycols.
摘要翻译：本发明涉及新的金属配合物或含有pseudopolyrotaxanes含碘苯衍生物。它们是诊断有价值的化合物。准聚轮烷配合物具有通式（I），其中n为6，7或8中，m是数字2〜50，X为直接键或基团-O-CO-CH（CH 3） - ，R 1和Y 具有在说明书中给出的含义，并且构成R3-Y-R 4的聚亚烷基二醇。

7. 发明申请

WO1996041830A1 CASCADE POLYMERS WITH IODINE-CONTAINING AROMATIC COMPOUNDS 审中-公开
标题翻译： CASCADES WITH iodoaromatics聚合物
公开(公告)号：WO1996041830A1
公开(公告)日：1996-12-27
申请号：PCT/EP1996002517
申请日：1996-06-11
申请人： SCHERING AKTIENGESELLSCHAFT , KRAUSE, Werner , MAIER, Franz, Karl , SCHMITT-WILLICH, Heribert , PLATZEK, Johannes , PRESS, Wolf-Rüdiger , SCHUHMANN-GIAMPIERI, Gabriele
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： C08G73/02
CPC分类号： C07K14/001 , A61K49/0442 , C07C237/46 , C07F9/3808 , C07F9/4006 , C07K5/0215
摘要： Iodine-containing dendritic polymers are useful as radiological diagnostic agents.
摘要翻译：树枝状聚合物含碘是有价值的透视诊断。

8. 发明申请

WO1996005167A1 DIMER DTPA DERIVATIVES AND THEIR METAL COMPLEXES, PHARMACEUTICALS CONTAINING THE SAME, THEIR USE IN DIAGNOSIS AND THERAPY AND PROCESS FOR PREPARING SAID COMPLEXES AND PHARMACEUTICALS 审中-公开
标题翻译：二聚体DTPA衍生物及其金属络合物，这种复杂的含制药诊断和治疗和方法使用用于生产复杂和手段
公开(公告)号：WO1996005167A1
公开(公告)日：1996-02-22
申请号：PCT/EP1995003142
申请日：1995-08-08
申请人： SCHERING AKTIENGESELLSCHAFT , KRAUSE, Werner , MAIER, Franz-Karl , BAUER, Michael , PRESS, Wolf-Rüdiger , SCHUHMANN-GIAMPIERI, Gabriele , PLATZEK, Johannes , SCHMITT-WILLICH, Heribert
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： C07C229/26
CPC分类号： C07C237/08 , A61K49/06 , A61K51/048 , C07C229/16 , C07C229/36 , C07C229/76 , C07C237/06
摘要： New dimer DTPA derivatives have the general formula (I) that consists of the increments (A) and (B) which are interconnected by one of the pairs of substituents R and R , R and R , R and R , R and R , R and R , R and R , R and R , R and R , R and R . The interconnecting substituent pairs stand for heterocycle, a phenylene residue, a C0-C30-alkylene or C7-C30-aralkylene chain, which may be optionally substituted by 1-4 hydroxy, C1-C6-alkoxy, carboxy or mercapto groups and/or interrupted by 1 to 6 oxygen, nitrogen or sulphur atoms or sulfinyl and/or sulfonyl groups; Y stands for a hydrogen atom and/or a metal ion equivalent of an element having atomic numbers 21-32, 37-39, 42-51 and 57-83; and X and X' stand for a group -OY or -CONR R . Also disclosed is the use of said metal complexes in NMR and/or röntgen diagnosis, in radiodiagnosis and radiotherapy, as well as a process for preparing the same.
摘要翻译：本发明涉及通式（I）的新的二聚DTPA衍生物，选自由增量（A）和（B），其中通过取代基R <1>中的一个和R <1'的增量（A）和（B） >，R <2>和R <2 '>，R <15>和R <15'>，R <1>和R <2 '>，R <1'>和R <2>，R <1 >和R <15>，R <1>和R <15 '>，R <2>和R <15'>，R <2“>和R <15>连接在一起，其中用于杂环取代基的相应的联，一个苯基基团，一个C0-C30亚烷基或C7-C30亚芳烷基任选被1-4个羟基，C1-C6烷氧基，羧基或巯基和/或由1至6个氧取代的，氮，硫原子，亚磺酰基和/或磺酰基中断，且每个Y是氢原子和/或金属离子当量原子序数21-32，37-39，42-51和57-83，以及X和X的元素是“的基团-OY，或-CONR <5> - [R <6>; 和使用在NMR和/或X射线诊断，放射诊断和放射治疗的金属配合物，以及它们的制备方法。

9. 发明申请

WO1994017033A1 PROCESS FOR PREPARING C-SUBSTITUTED DIETHYLENE TRIAMINES 审中-公开
标题翻译：用于生产C-取代二亚乙基
公开(公告)号：WO1994017033A1
公开(公告)日：1994-08-04
申请号：PCT/EP1994000034
申请日：1994-01-08
申请人： SCHERING AKTIENGESELLSCHAFT , PETROV, Orlin , HILSCHER, Jean-Claude , NICKISCH, Klaus , SCHMITT-WILLICH, Heribert , GRIES, Heinz , RADÜCHEL, Bernd , PLATZEK, Johannes
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： C07C269/06
CPC分类号： C07C303/30 , C07C217/62 , C07C269/06 , C07C271/20 , C07C2601/08 , C07C2601/14 , Y02P20/55 , C07C309/66
摘要： A process for preparing C-substituted diethylene triamines having general formula (I) is characterized in that a nitrogen-protected aminoethyl alcohol having general formula (II) is reacted with methane sulphonic acid chloride, tosyl chloride or trifluoroacetic acid anhydride in an organic solvent, with addition of a base, to give the corresponding mesylate, tosylate or triflate, is then filtered and the filtrate is reacted with an ethylene diamine having general formula (III) to give the desired nitrogen-protected, carbon-substituted triamine having general formula (I), in which R stands for a -(CH2)m-(C6H4)q-(O)k-(CH2)n-(C6H4)l-(O)r-R group or for a -(CH2)m-(C6H10)q-(O)k-(CH2)n-(C6H10)l-(O)r-R group; R and R each stand for a hydrogen atom or form together a -(CH2)p-alkylene bridge; and R stands for an amino protecting group, preferably for a benzyloxycarbonyl group.

10. 发明申请

WO1997004811A2 USE OF LIPOSOMAL PREPARATIONS IN INDIRECT MRI LYMPHOGRAPHY 审中-公开
标题翻译：脂质体制剂间接MRT淋巴USE
公开(公告)号：WO1997004811A2
公开(公告)日：1997-02-13
申请号：PCT/DE1996001433
申请日：1996-07-25
申请人： SCHERING AKTIENGESELLSCHAFT , SACHSE, Andreas , PLATZEK, Johannes , MISSELWITZ, Bernd , MÜHLER, Andreas , ROESSLING, Georg
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： A61K49/00
CPC分类号： A61K49/1812
摘要： The invention concerns the use of liposomes charged with contrasting agents for interstitial lymphography.
摘要翻译：本发明涉及使用造影加载脂质体的间质性淋巴。

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