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1. 发明授权

US06610299B1 Glycosyl-etoposide prodrugs, a process for preparation thereof and the use thereof in combination with functionalized tumor-specific enzyme conjugates 失效
公开(公告)号：US06610299B1
公开(公告)日：2003-08-26
申请号：US08325955
申请日：1994-10-19
申请人： Cenek Kolar , Jörg Czech , Klaus Bosslet , Gerhard Seemann , Hans-Harald Sedlacek , Dieter Hoffmann
发明人： Cenek Kolar , Jörg Czech , Klaus Bosslet , Gerhard Seemann , Hans-Harald Sedlacek , Dieter Hoffmann
IPC分类号： A61K3944
CPC分类号： B82Y5/00 , A61K38/00 , A61K47/549 , A61K47/6815 , A61K47/6851 , A61K47/6899 , A61K2039/505 , C07H17/04 , C07K16/30 , C07K16/3007 , C07K2317/24 , C07K2319/00 , C12N9/2434 , C12Y302/01031
摘要： The present invention relates to glycosyl-etoposide prodrugs, a process for the preparation thereof and the use thereof in combination with functionalized tumor-specific enzyme conjugates for treating cancers.

2. 发明授权

US07241595B2 Glycosyl-etoposide prodrugs, a process for preparation thereof and the use thereof in combination with functionalized tumor-specific enzyme conjugates 失效
标题翻译：糖基 - 依托泊苷前药，其制备方法及其与功能化肿瘤特异性酶缀合物的组合
公开(公告)号：US07241595B2
公开(公告)日：2007-07-10
申请号：US10128493
申请日：2002-04-24
申请人： Cenek Kolar , Jörg Czech , Klaus Bosslet , Gerhard Seemann , Hans-Harald Sedlacek
发明人： Cenek Kolar , Jörg Czech , Klaus Bosslet , Gerhard Seemann , Hans-Harald Sedlacek
IPC分类号： C12P19/60
CPC分类号： B82Y5/00 , A61K38/00 , A61K47/6815 , A61K47/6851 , A61K47/6899 , A61K2039/505 , C07H17/04 , C07K16/30 , C07K16/3007 , C07K2317/24 , C07K2319/00 , C12N9/16 , C12N9/2434 , C12Y301/03001 , C12Y302/01031
摘要： The present invention relates to glycosyl-etoposide prodrugs, a process for the preparation thereof and the use thereof in combination with functionalized tumor-specific enzyme conjugates for treating cancers.
摘要翻译：本发明涉及糖基 - 依托泊苷前药，其制备方法及其与用于治疗癌症的官能化肿瘤特异性酶缀合物的组合的用途。

3. 发明授权

US06475486B1 Glycosyl-etoposide prodrugs, a process for preparation thereof and the use thereof in combination with functionalized tumor-specific enzyme conjugates 失效
标题翻译：糖基 - 依托泊苷前药，其制备方法及其与功能化肿瘤特异性酶缀合物的组合
公开(公告)号：US06475486B1
公开(公告)日：2002-11-05
申请号：US09343698
申请日：1999-06-30
申请人： Cenek Kolar , Jörg Czech , Klaus Bosslet , Gerhard Seemann , Hans-Harald Sedlacek , Dieter Hoffman
发明人： Cenek Kolar , Jörg Czech , Klaus Bosslet , Gerhard Seemann , Hans-Harald Sedlacek , Dieter Hoffman
IPC分类号： A61K39395
CPC分类号： B82Y5/00 , A61K47/6815 , A61K2039/505 , C07K16/3007 , C07K2317/24 , C07K2319/00
摘要： The present invention relates to glycosyl-etoposide prodrugs, a process for the preparation thereof and the use thereof in combination with functionalized tumor-specific enzyme conjugates for treating cancers.
摘要翻译：本发明涉及糖基 - 依托泊苷前药，其制备方法及其与用于治疗癌症的官能化肿瘤特异性酶缀合物的组合的用途。

4. 发明授权

US5561119A Glycosylated prodrugs, their method of preparation and their uses 失效
标题翻译：糖基化前药，其制备方法及其用途
公开(公告)号：US5561119A
公开(公告)日：1996-10-01
申请号：US137167
申请日：1994-05-27
申请人： Jean-Claude Jacquesy , Jean-Pierre Gesson , Claude Monneret , Martine Mondon , Brigitte Renoux , Jean-Claude Florent , Michel Koch , Fran.cedilla.ois Tillequin , Hans H. Sedlacek , Manfred Gerken , Cenek Kolar , Gilbert Gaudel , Klaus Bosslet , J org Czech , Dieter Hoffman , Gerhard Seemann , Hans-Ulrich Schorlemmer , Gerhard Dickneite
发明人： Jean-Claude Jacquesy , Jean-Pierre Gesson , Claude Monneret , Martine Mondon , Brigitte Renoux , Jean-Claude Florent , Michel Koch , Fran.cedilla.ois Tillequin , Hans H. Sedlacek , Manfred Gerken , Cenek Kolar , Gilbert Gaudel , Klaus Bosslet , J org Czech , Dieter Hoffman , Gerhard Seemann , Hans-Ulrich Schorlemmer , Gerhard Dickneite
IPC分类号： A61K38/22 , A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61K38/46 , A61K39/395 , A61P35/00 , A61P43/00 , C07F7/18 , C07H15/203 , C07H15/252 , C07H15/26 , A61K39/44 , C07C50/18 , C07H5/04
CPC分类号： C07H15/203 , C07F7/1852 , C07F7/1856 , C07H15/252 , C07H15/26
摘要： Glycosylated prodrugs, a preparation method therefor, and their use with tumor-specific immunoenzymatic conjugates for the treatment of cancer, are described. These anthracycline prodrugs have formula (I). ##STR1##
摘要翻译： PCT No.PCT / FR92 / 00385 Sec。 371日期：1994年5月27日 102（e）日期1994年5月27日PCT提交1992年4月29日PCT公布。出版物WO92 / 19639 日期：1992年11月12日描述了糖基化前体药物及其制备方法及其与肿瘤特异性免疫酶联用物质治疗癌症的用途。这些蒽环类前体具有式（I）。（一）

5. 发明授权

US6146658A Prodrugs, their preparation and use as pharmaceuticals 失效
标题翻译：前药，其制备和用作药物
公开(公告)号：US6146658A
公开(公告)日：2000-11-14
申请号：US859084
申请日：1997-05-20
申请人： Klaus Bosslet , Jorg Czech , Dieter Hoffmann , Cenek Kolar , Fran.cedilla.ois Tillequin , Jean-Claude Florent , Michel Azoulay , Claude Monneret , Jean-Claude Jacquesy , Jean-Pierre Gesson , Michel Koch
发明人： Klaus Bosslet , Jorg Czech , Dieter Hoffmann , Cenek Kolar , Fran.cedilla.ois Tillequin , Jean-Claude Florent , Michel Azoulay , Claude Monneret , Jean-Claude Jacquesy , Jean-Pierre Gesson , Michel Koch
IPC分类号： A61K31/70 , A23B4/03 , A61K9/127 , A61K31/7024 , A61K31/7028 , A61K31/7034 , A61K31/715 , A61K38/00 , A61K38/16 , A61K45/00 , A61K47/48 , A61P35/00 , A61P37/00 , A61P43/00 , C07H13/08 , C07H13/12 , C07H15/00 , C07H15/04 , C07H15/203 , C07H15/207
CPC分类号： C07H13/08 , A61K47/48 , A61K47/48092 , C07H13/12 , C07H15/203 , Y02P20/55 , Y10S514/01
摘要： Glycosyl-spacer-drugs compounds (prodrugs), their preparation and their use as pharmaceuticals are described.
摘要翻译：描述了糖基间隔物药物化合物（前药），其制备及其作为药物的用途。

6. 发明授权

US5955100A Prodrugs their preparation and use as pharmaceuticals 失效
标题翻译：前药作为药物的制备和使用
公开(公告)号：US5955100A
公开(公告)日：1999-09-21
申请号：US449021
申请日：1995-05-24
申请人： Klaus Bosslet , Jorg Czech , Dieter Hoffmann , Cenek Kolar , Fran.cedilla.ois Tillequin , Jean-Claude Florent , Michel Azoulay , Claude Monneret , Jean-Claude Jacquesy , Jean-Pierre Gesson , Michel Koch
发明人： Klaus Bosslet , Jorg Czech , Dieter Hoffmann , Cenek Kolar , Fran.cedilla.ois Tillequin , Jean-Claude Florent , Michel Azoulay , Claude Monneret , Jean-Claude Jacquesy , Jean-Pierre Gesson , Michel Koch
IPC分类号： A61K31/70 , A23B4/03 , A61K9/127 , A61K31/7024 , A61K31/7028 , A61K31/7034 , A61K31/715 , A61K38/00 , A61K38/16 , A61K45/00 , A61K47/48 , A61P35/00 , A61P37/00 , A61P43/00 , C07H13/08 , C07H13/12 , C07H15/00 , C07H15/04 , C07H15/203 , C07H15/207
CPC分类号： C07H13/08 , A61K47/48 , A61K47/48092 , C07H13/12 , C07H15/203 , Y02P20/55 , Y10S514/01
摘要： Glycosyl-spacer-drugs compounds (prodrugs), their preparation and their use as pharmaceuticals are described.
摘要翻译：描述了糖基间隔物药物化合物（前药），其制备及其作为药物的用途。

7. 发明授权

US4948880A Anthracycline derivatives having cytostatic activity 失效
标题翻译：具有细胞抑制活性的蒽环类衍生物
公开(公告)号：US4948880A
公开(公告)日：1990-08-14
申请号：US129006
申请日：1987-12-04
申请人： Peter Hermentin , Michael Paal , Hans P. Kraemer , Cenek Kolar , Dieter Hoffmann , Manfred Gerken , Hans G. Berscheid , Dirk Bottger
发明人： Peter Hermentin , Michael Paal , Hans P. Kraemer , Cenek Kolar , Dieter Hoffmann , Manfred Gerken , Hans G. Berscheid , Dirk Bottger
IPC分类号： A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P31/12 , A61P35/00 , A61P35/02 , C07H15/252
CPC分类号： C07H15/252
摘要： The invention relates to new anthracycline derivatives having cytostatic activity and the general formula I, which are optionally in the form of a salt of an inorganic or organic acid, ##STR1## in which the substituents have the following meaning: R.sup.1 is hydrogen or a hydroxyl group,R.sup.2 is hydrogen or a hydroxyl or a methoxy group,R.sup.3 is hydrogen or a hydroxyl group,R.sup.4 is hydrogen or a hydroxyl group,R.sup.5 is hydrogen, a hydroxyl or a methoxycarbonyl group, or a substituent of the general formula II, ##STR2## in which R.sup.8a has the meaning indicated for R.sup.8, or a substituent of the formula III, ##STR3## R.sup.6 is ethyl, methylcarbonyl, hydroxymethylcarbonyl, hydroxyalkyl or a dihydroxyalkyl,R.sup.7 is hydrogen or a substituent of the general formula IV, ##STR4## and R.sup.8 is hydrogen or a cyanomethyl group or a substituent of the general formula COR.sup.9 or CH.sub.2 R.sup.10, R.sup.9 being hydrogen, CH.sub.3, CF.sub.3 or CCl.sub.3, and R.sup.10 being C.sub.1 - to C.sub.8 -alkyl, substituted alkyl, phenyl or substituted phenyl, to a process for their preparation and to their use in pharmaceuticals.
摘要翻译：本发明涉及具有细胞抑制活性的新型蒽环类衍生物和通式I，其任选呈无机或有机酸盐的形式，其中取代基具有以下含义：R 1为氢或羟基，R2是氢或羟基或甲氧基，R3是氢或羟基，R4是氢或羟基，R5是氢，羟基或甲氧基羰基或通式II的取代基，其中R8a具有对于R8表示的含义或式III的取代基，其中R 6是乙基，甲基羰基，羟甲基羰基，羟基烷基或二羟基烷基，R 7是氢或通式IV的取代基 IV和R8是氢或氰基甲基或通式为COR9或CH2R10的取代基，R9为氢，CH3，CF3或CCl3，R10为C1-至C8-烷基，取代的烷基，苯基或取代的苯基，为一种方法他们的准备和在药物中的使用。

8. 发明授权

US4914191A Anthracycline derivatives having cytostatic activity 失效
标题翻译：具有细胞抑制活性的蒽环类衍生物
公开(公告)号：US4914191A
公开(公告)日：1990-04-03
申请号：US216199
申请日：1988-07-07
申请人： Peter Hermentin , Michael Paal , Cenek Kolar , Hans P. Kraemer , Dieter Hoffmann , Hans G. Berscheid , Dirk Bottger
发明人： Peter Hermentin , Michael Paal , Cenek Kolar , Hans P. Kraemer , Dieter Hoffmann , Hans G. Berscheid , Dirk Bottger
IPC分类号： A61K31/65 , A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P35/00 , C07C45/00 , C07C50/36 , C07C67/00 , C07H15/252
CPC分类号： C07H15/252
摘要： The invention relates to new anthracycline derivatives having cytostatic activity and the general formula I ##STR1## in which the radicals R.sup.1 is hydrogen or a hydroxyl group, R.sup.2 is hydrogen or a hydroxyl group or a structure of the formula II, and R.sup.3 is a hydroxyl group or a structure of the formula II ##STR2## in which R.sup.4 is an aliphatic or aromatic acyl group, with the proviso that at least one of the radicals R.sup.2 and R.sup.3 has a structure of the formula II, which are optionally in the form of a salt of an inorganic or organic acid, as well as to the process for the preparation thereof, and to the use thereof in pharmaceuticals.
摘要翻译：本发明涉及具有细胞抑制活性的新型蒽环类衍生物和其中基团R 1为氢或羟基，R 2为氢或羟基或式II结构的通式Ⅰ“ 羟基或式II II的结构，其中R 4是脂族或芳族酰基，条件是基团R 2和R 3中的至少一个具有式II的结构，其任选在形式的无机或有机酸的盐，以及其制备方法及其在药物中的用途。

9. 发明授权

US5260425A Anthracycline derivatives having cytostatic activity 失效
标题翻译：具有细胞抑制活性的蒽环类衍生物
公开(公告)号：US5260425A
公开(公告)日：1993-11-09
申请号：US360807
申请日：1989-06-02
申请人： Peter Hermentin , Ernst Raab , Cenek Kolar , Manfred Gerken , Dieter Hoffmann , Hans P. Kraemer , Ulrich Stache
发明人： Peter Hermentin , Ernst Raab , Cenek Kolar , Manfred Gerken , Dieter Hoffmann , Hans P. Kraemer , Ulrich Stache
IPC分类号： A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P35/00 , C07H15/252 , C07H15/26 , C07H15/24
CPC分类号： C07H15/252 , C07H15/26
摘要： The invention relates to new anthracycline derivatives having cytostatic activity and the general formula I, ##STR1## which can optionally also be in the form of an acid addition salt of physiologically acceptable inorganic or organic acids, where R.sup.1 is hydrogen or a hydroxyl group, R.sup.2 is hydrogen, a hydroxyl or a methoxy group, R.sup.3 is hydrogen or a hydroxyl group, R.sup.4 is hydrogen or a hydroxyl group, R.sup.5 hydrogen, a hydroxyl or a methoxycarbonyl group, R.sup.6 is CH.sub.2 CH.sub.3, COCH.sub.3, COCH.sub.2 OH, CHOHCH.sub.3 or CHOHCH.sub.2 OH and R.sup.7 is an organic substituent which has 2 to 6 carbon atoms and which contains at least one oxygen, nitrogen or sulfur atom or a C--C double bond or a C--C triple bond, it being possible for the double bond also to be a constituent of a heteroaromatic system and for the oxygen, nitrogen or sulfur atom to be a constituent of an open-chain or heterocyclic system, to a process for the preparation thereof and to the use thereof in a pharmaceutical.
摘要翻译：本发明涉及具有细胞抑制活性的新型蒽环类衍生物和通式I，其也可以是生理上可接受的无机或有机酸的酸加成盐形式，其中R 1是氢或羟基， R2是氢，羟基或甲氧基，R3是氢或羟基，R4是氢或羟基，R5是氢，羟基或甲氧基羰基，R6是CH2CH3，COCH3，COCH2OH，CHOHCH3或CHOHCH2OH和R7 是具有2至6个碳原子并且含有至少一个氧，氮或硫原子或CC双键或CC三键的有机取代基，双键也可以是杂芳族体系的组分以及氧，氮或硫原子作为开链或杂环体系的组分，其制备方法及其在药物中的用途。

10. 发明授权

US5556941A Glycopeptide derivatives, a process for their preparation and pharmaceutical agents containing these compounds 失效
标题翻译：糖肽衍生物，其制备方法和含有这些化合物的药剂
公开(公告)号：US5556941A
公开(公告)日：1996-09-17
申请号：US291729
申请日：1994-08-16
申请人： Cenek Kolar , Werner Stuber
发明人： Cenek Kolar , Werner Stuber
IPC分类号： A61K38/00 , A61P7/02 , C07K1/113 , C07K9/00 , C07K14/81 , A61K38/14 , C07K5/072
CPC分类号： C07K9/003 , A61K38/00
摘要： Glycopeptide derivatives, a process for their preparation and pharmaceutical agents containing these compounds N-Glycopeptide derivatives of the formula I ##STR1## where aromatic is an unsubstituted or substituted benzene residue, naphthalene residue, chroman residue, chromene residue or coumarone residue,a is 0 to 5, b is 0 to 4, c is 0 or 1, d is 1 or 2R.sup.1 is (C.sub.1 -C.sub.3)-alkyl,R.sup.2 is (C.sub.1 -C.sub.3)-alkyl or (C.sub.1 -C.sub.3)-alkyloxy,R.sup.3 is H, OH, (C.sub.1 -C.sub.3)-alkyloxy, NH.sub.2, NH-(C.sub.1 -C.sub.6)-alkanoyl, NH-benzoyl, NH--SO.sub.3 H or NH-acyl radical of a natural N-acetylated amino acid,R.sup.4 is H, OH, or (C.sub.1 -C.sub.3)-alkyloxy,R.sup.5 is H, OH, (C.sub.1 -C.sub.3)-alkyloxy, fluorine, chlorine or bromine,R.sup.6 is H, CH.sub.3, CH.sub.2 OH, CH.sub.2 O--(C.sub.1 -C.sub.6), CH.sub.2 NHCOCH.sub.3 or CH.sub.2 NH--SO.sub.3 H,R.sup.5 and R.sup.6 are together O--CH.sub.2 --O--CH.sub.2, --O--CH(CH.sub.3)--O--CH.sub.2 or O--C(CH.sub.3).sub.2 --O--CH.sub.2,R.sup.7 is hydroxy-(C.sub.2 -C.sub.4)-alkyl or (C.sub.2 -C.sub.4)-alkyloxy-(C.sub.2 -C.sub.4)-alkyl,R.sup.8 is H or (C.sub.1 -C.sub.6)-alkyl orR.sup.7 -N-R.sup.8 are together a pyrrolidine ring or piperdine ring or morpholine ring, which can be substituted by HO, HOCH.sub.2, CH.sub.3 or COOH,W is --O--, --CONH-- or --C.sub.6 H.sub.4 --CONH andH-X is HCl, a (C.sub.1 -C.sub.7)-alkanoic acid or another pharmacologically tolerated inorganic or organic acid,are described, as are a process for their preparation and a pharmaceutical agent which contains these novel compounds. These pharmaceuticals can be used in particular for the therapy of thrombotic disorders.
摘要翻译：糖肽衍生物，其制备方法和含有这些化合物的药剂N-芳香族是未取代或取代的苯残基，萘残基，苯并二氢吡喃残基，色烯还原或香豆酮残基的式I的N-糖肽衍生物，a为0 （C 1 -C 3） - 烷基或（C 1 -C 3） - 烷氧基，R 3为H，C 1 -C 4烷基， OH，（C 1 -C 3） - 烷氧基，NH 2，NH-（C 1 -C 6） - 烷酰基，NH-苯甲酰基，NH-SO 3 H或NH-酰基自然的N-乙酰化氨基酸，R4is H，OH或（ C1-C3） - 烷氧基，R5isH，OH，（C1-C3） - 烷氧基，氟，氯或溴，R6isH，CH3，CH2OH，CH2O-（C1-C6），CH2NHCOCH3或CH2NH-SO3H，R5和R6 在一起是O-CH 2 -O-CH 2，-O-CH（CH 3）-O-CH 2或OC（CH 3）2 -O-CH 2，R 7是羟基 - （C 2 -C 4） - 烷基或（C 2 -C 4）烷氧基 - （C 2 -C 4） - 烷基，R 8是H或（C 1 -C 6） - 烷基或R 7 -N-R 8一起是可以被HO，HOCH 2，CH 3取代的吡咯烷环或哌啶环或吗啉环， COOH， W是-O - ， - CONH - 或-C6H4-CONH，HX是HCl，（C1-C7） - 链烷酸或另一种药理学上耐受的无机或有机酸，以及其制备方法和药物含有这些新化合物的试剂。这些药物特别可用于治疗血栓形成障碍。

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