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1. 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。

2. 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。

3. 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）

4. 发明授权

US5602108A Semisynthetic diastereomerically pure N-glycidylanthracyclines, a process for the stereoselective preparation thereof as the use thereof as cytostatics 失效
标题翻译：半合成非对映异构体纯的N-缩水甘油环内酯，其作为细胞抑制剂的用途的立体选择性制备方法
公开(公告)号：US5602108A
公开(公告)日：1997-02-11
申请号：US464468
申请日：1995-06-05
申请人： Manfred Gerken , Monika Grimm , Ernst Raab , Dieter Hoffmann , Reiner Straub
发明人： Manfred Gerken , Monika Grimm , Ernst Raab , Dieter Hoffmann , Reiner Straub
IPC分类号： A61K31/65 , A61K31/70 , A61K31/704 , A61P35/00 , C07B53/00 , C07C15/62 , C07C50/36 , C07H15/252 , C07H15/26 , A61K37/00 , C07M15/24
CPC分类号： C07H15/26 , C07H15/252
摘要： Semisynthetic diastereomerically pure N-glycidylanthracyclines, a process for the stereoselective preparation thereof and the use thereof as cytostatics. The invention relates to anthracyclines having cytostatic activity and the formula I, which are, where appropriate, in the form of a salt with an inorganic or organic acid, ##STR1## in which R.sup.1 is hydrogen or a hydroxyl group,R.sup.2 is hydrogen, a hydroxyl group or an alkyloxy group (C.sub.1 -C.sub.4),R.sup.3 is hydrogen, a hydroxyl group or a structure of the formula II ##STR2## R.sup.4 is CH.sub.2 CH.sub.3, COCH.sub.3, COCH.sub.2 OH, CHOHCH.sub.3 or CHOHCH.sub.2 OH,R.sup.5 is hydrogen, a hydroxyl group, a methoxycarbonyl group or a structure of the formula II,R.sup.6 is hydrogen, an alkyl group (C.sub.1 -C.sub.4), an allyl group, a benzyl group or mono- or di-methyloxy-substituted benzyl group, a tetrahydropyranyl group,R.sup.7 is hydrogen, an alkyl group (C.sub.1 -C.sub.4), an allyl group, a benzyl group or mono- or di-methyloxy-substituted benzyl group andR.sup.8 is a structure of the formula III or IV ##STR3## and to a process for the preparation of these compounds, which comprises reacting an anthracycline derivative of the structure I in whichR.sup.1, R.sup.2 and R.sup.4 are as defined above, andR.sup.3 is hydrogen, a hydroxyl group or a structure of the formula V ##STR4## R.sup.5 is hydrogen, a hydroxyl group, a methoxycarbonyl group or a structure of the formula V andR.sup.6 and R.sup.7 are as defined above, with (R)- or (S)-glycidyl sulfonate.
摘要翻译：半合成非对映体纯N-缩水甘油环素，其立体选择性制备方法及其作为细胞抑制剂的用途。本发明涉及具有细胞抑制活性的蒽环类抗生素和式I，它们在适当的情况下为无机或有机酸形式的盐，其中R 1为氢或羟基，R 2为氢，羟基或烷氧基（C 1 -C 4），R 3是氢，羟基或式II的结构。R 4是CH 2 CH 3，COCH 3，COCH 2 OH，CHOHCH 3或CHOHCH 2 OH，R 5是氢，羟基，甲氧基羰基或式II的结构，R6是氢，烷基（C1-C4），烯丙基，苄基或单 - 或二 - 甲氧基取代的苄基，四氢吡喃基，R7是氢，烷基（C1-C4），烯丙基，苄基或单 - 或二 - 甲氧基取代的苄基，R8是式III或IV的结构，IV和一种制备这些化合物的方法，其包括使结构I的蒽环衍生物与其中R 1，R 2和/ R 4如上定义，并且R 3是氢，羟基或式V R 5的结构是氢，羟基，甲氧基羰基或式V和R 6和R 7的结构如上定义（R） - 或（S） - 磺酰基磺酰基。

5. 发明授权

US07803524B2 Antigenic HIV gp41 chimeric polypeptides comprising the MVP5180/91 epitope SKGKLIS 有权
标题翻译：包含MVP5180 / 91表位SKGKLIS的抗原HIV gp41嵌合多肽
公开(公告)号：US07803524B2
公开(公告)日：2010-09-28
申请号：US11084858
申请日：2005-03-21
申请人： Stefan Brust , Stefan Knapp , Manfred Gerken , Lutz G. Guertler
发明人： Stefan Brust , Stefan Knapp , Manfred Gerken , Lutz G. Guertler
IPC分类号： C12Q1/70 , A61K39/21 , B01L3/00
CPC分类号： C07K14/005 , A61K39/00 , C07K16/1045 , C07K2317/21 , C12N2740/16022 , C12N2740/16122 , C12N2740/16134 , C12Q1/703
摘要： Immunologically active peptides which are derived from a novel immunodeficiency virus which has the designation MVP5180/91 are described. A diagnostic composition containing such a peptide and methods of detecting an antibody against a retrovirus that causes immune deficiency using such diagnostic composition are also described. A kit containing the immunologically active peptides is also described. An immunogen and method of immunizing a mammal against HIV infection using the immunologically active peptides is described. DNA encoding the peptides and methods of detecting nucleic acids encoding HIV viruses are also described.
摘要翻译：描述了衍生自具有名称MVP5180 / 91的新型免疫缺陷病毒的免疫活性肽。还描述了含有这种肽的诊断组合物和使用这种诊断组合物检测引起免疫缺陷的逆转录病毒抗体的方法。还描述了含有免疫活性肽的试剂盒。描述了使用免疫活性肽免疫哺乳动物抗HIV感染的免疫原和方法。还描述了编码肽的DNA和检测编码HIV病毒的核酸的方法。

6. 发明授权

US06869608B2 Peptides derived from a retrovirus of the HIV group and their use 失效
标题翻译：衍生自HIV组的逆转录病毒的肽及其用途
公开(公告)号：US06869608B2
公开(公告)日：2005-03-22
申请号：US10000321
申请日：2001-12-04
申请人： Stefan Brust , Stefan Knapp , Manfred Gerken , Lutz G. Guertler
发明人： Stefan Brust , Stefan Knapp , Manfred Gerken , Lutz G. Guertler
IPC分类号： G01N33/569 , A61K39/00 , A61K39/21 , A61P31/12 , A61P31/18 , C07K7/08 , C07K14/155 , C07K14/16 , C07K16/00 , C07K16/10 , C12N15/09 , C12N15/48 , C12P21/02 , C12Q1/68 , C12Q1/70 , C12R1/19
CPC分类号： C07K14/005 , A61K39/00 , C07K16/1045 , C07K2317/21 , C12N2740/16022 , C12N2740/16122 , C12N2740/16134 , C12Q1/703
摘要： Immunologically active peptides which are derived from a novel immunodeficiency virus which has the designation MVP5180/91 are described. A diagnostic containing such a peptide and methods of detecting an antibody against a retrovirus that causes immune deficiency using such diagnostic composition are also described. A kit containing the immunologically active peptides is also described. An immunogen and method of immunizing a mammal against HIV infection using the immunologically active peptides is described. DNA encoding the peptides and methods of detecting nucleic acids encoding HIV viruses are also described.
摘要翻译：描述了衍生自具有名称MVP5180 / 91的新型免疫缺陷病毒的免疫活性肽。还描述了含有这种肽的诊断和使用这种诊断组合物检测引起免疫缺陷的逆转录病毒的抗体的方法。还描述了含有免疫活性肽的试剂盒。描述了使用免疫活性肽免疫哺乳动物抗HIV感染的免疫原和方法。还描述了编码肽的DNA和检测编码HIV病毒的核酸的方法。

7. 发明授权

US06335158B2 Methodologies for the detection of human immunodeficiency virus nucleic acids employing oligonucleotide primer derived from the HIV-1 MVP5180/91 genome 有权
标题翻译：使用衍生自HIV-1 MVP5180 / 91基因组的寡核苷酸引物检测人类免疫缺陷病毒核酸的方法
公开(公告)号：US06335158B2
公开(公告)日：2002-01-01
申请号：US09131551
申请日：1998-08-10
申请人： Stefan Brust , Stefan Knapp , Manfred Gerken , Lutz G. Guertler
发明人： Stefan Brust , Stefan Knapp , Manfred Gerken , Lutz G. Guertler
IPC分类号： C12Q170
CPC分类号： C07K14/005 , A61K39/00 , C07K16/1045 , C07K2317/21 , C12N2740/16022 , C12N2740/16122 , C12N2740/16134 , C12Q1/703
摘要： The present invention is directed toward nucleic-acid based methodologies for the detection of human immunodeficiency virus (HIV) nucleic acids in a sample. A novel HIV-1 isolate, designated MVP5180/91, was isolated from a West African Cameroonian patient with immunodeficiency. Nucleic acid and amino acid sequence comparisons of this isolate, with other HIV-1 strains of subtypes A-E and HIV-2 isolates, demonstrated that this virus shares only limited homology with other known HIV-1 and -2 isolates. However, this virus does display some genetic relatedness to another Cameroonian isolate designated ANT-70. These viruses form the basis for a new HIV-1 group which has been designated subtype O. An immunologically important epitope, corresponding to amino acids 601-623 of the MVP5180/91 transmembrane envelope glycoprotein, was identified. Labeled nucleic acids can be prepared from the nucleotide sequence encoding this region and employed in standard hybridization assays to detect HIV-1 nucleic acids. Alternatively, oligonucleotide primers can also be prepared from this region and employed in polymerase chain reaction (PCR) assays to detect viral-specific nucleic acids.
摘要翻译：本发明涉及用于检测样品中的人类免疫缺陷病毒（HIV）核酸的基于核酸的方法。从具有免疫缺陷的西非喀麦隆患者中分离出一种名为MVP5180 / 91的新型HIV-1分离株。该分离株与其他HIV-1亚型A-E和HIV-2分离株的核酸和氨基酸序列比较表明，该病毒与其他已知的HIV-1和-2分离株仅具有有限的同源性。然而，这种病毒确实显示与另一个指定为ANT-70的喀麦隆分离株有一些遗传相关性。这些病毒构成了已被指定为亚型O的新的HIV-1组的基础。鉴定了与MVP5180 / 91跨膜包膜糖蛋白的氨基酸601-623相当的免疫重要的表位。标记的核酸可以从编码该区域的核苷酸序列制备，并用于标准杂交测定以检测HIV-1核酸。或者，也可以从该区域制备寡核苷酸引物，并用于聚合酶链反应（PCR）测定中以检测病毒特异性核酸。

8. 发明授权

US6020315A Preparation having increased in vivo tolerability 失效
标题翻译：制剂具有增加的体内耐受性
公开(公告)号：US6020315A
公开(公告)日：2000-02-01
申请号：US76878
申请日：1998-05-13
申请人： Klaus Bosslet , Jorg Czech , Manfred Gerken , Rainer Straub , Matthias Blumrich
发明人： Klaus Bosslet , Jorg Czech , Manfred Gerken , Rainer Straub , Matthias Blumrich
IPC分类号： C07H15/20 , A61K9/20 , A61K9/48 , A61K31/047 , A61K31/70 , A61K31/7004 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61K31/715 , A61K47/10 , A61K47/26 , A61K47/36 , A61K47/48 , A61P29/00 , A61P35/00 , A61P37/00 , A61P43/00 , C07H5/06 , C07H15/244 , C07H15/252
CPC分类号： A61K47/48092
摘要： A preparation having increased in vivo tolerability comprising a glycosyl-Y[--C(.dbd.Y)--X--].sub.p --W(R).sub.n --X--C(.dbd.Y)-active compound, sugar or sugar alcohol and, optionally divalent ions, and a pharmaceutically tolerable carrier.
摘要翻译：具有增加的体内耐受性的制剂，其包含糖基-Y [-C（= Y）-X-] pW（R）n XC（= Y） - 活性化合物，糖或糖醇以及任选的二价离子和药学上可耐受的载体

9. 发明申请

US20050271678A1 Peptides derived from a retrovirus of the HIV group and their use 有权
标题翻译：衍生自HIV组的逆转录病毒的肽及其用途
公开(公告)号：US20050271678A1
公开(公告)日：2005-12-08
申请号：US11084858
申请日：2005-03-21
申请人： Stefan Brust , Stefan Knapp , Manfred Gerken , Lutz Guertler
发明人： Stefan Brust , Stefan Knapp , Manfred Gerken , Lutz Guertler
IPC分类号： G01N33/569 , A61K39/00 , A61K39/21 , A61P31/12 , A61P31/18 , C07K7/08 , C07K14/155 , C07K14/16 , C07K16/00 , C07K16/10 , C12N15/09 , C12N15/48 , C12P21/02 , C12Q1/68 , C12Q1/70 , C12R1/19
CPC分类号： C07K14/005 , A61K39/00 , C07K16/1045 , C07K2317/21 , C12N2740/16022 , C12N2740/16122 , C12N2740/16134 , C12Q1/703
摘要： Immunologically active peptides which are derived from a novel immunodeficiency virus which has the designation MVP5180/91 are described. A diagnostic composition containing such a peptide and methods of detecting an antibody against a retrovirus that causes immune deficiency using such diagnostic composition are also described. A kit containing the immunologically active peptides is also described. An immunogen and method of immunizing a mammal against HIV infection using the immunologically active peptides is described. DNA encoding the peptides and methods of detecting nucleic acids encoding HIV viruses are also described.
摘要翻译：描述了衍生自具有名称MVP5180 / 91的新型免疫缺陷病毒的免疫活性肽。还描述了含有这种肽的诊断组合物和使用这种诊断组合物检测引起免疫缺陷的逆转录病毒抗体的方法。还描述了含有免疫活性肽的试剂盒。描述了使用免疫活性肽免疫哺乳动物抗HIV感染的免疫原和方法。还描述了编码肽的DNA和检测编码HIV病毒的核酸的方法。

10. 发明授权

US06602866B2 Mercaptoacetylamide derivatives, a process for their preparation and their use 有权
标题翻译：巯基乙酰胺衍生物，其制备方法及其用途
公开(公告)号：US06602866B2
公开(公告)日：2003-08-05
申请号：US10118179
申请日：2002-04-08
申请人： Gary A. Flynn , Barbara A. Anderson , Manfred Gerken , Bernd Jablonka , Heinz-Werner Kleemann , Wolfgang Linz , Werner Seiz , Bernhard Seuring
发明人： Gary A. Flynn , Barbara A. Anderson , Manfred Gerken , Bernd Jablonka , Heinz-Werner Kleemann , Wolfgang Linz , Werner Seiz , Bernhard Seuring
IPC分类号： A61K3155
CPC分类号： C07D471/04
摘要： This invention discloses and claims a series of mercaptoacetylamide derivatives of formula I. Also disclosed and claimed are pharmaceutical compositions incorporating these compounds and processes for preparing said compounds. The use of said compounds for inhibition of the enzymes angiotensin converting enzyme and neutral endopeptidase, and for the treatment of hypertension and congestive heart failure are also disclosed and claimed
摘要翻译：本发明公开并要求一系列式I的巯基乙酰胺衍生物。还公开并要求保护的是掺入这些化合物的药物组合物和制备所述化合物的方法。所述化合物用于抑制酶血管紧张素转化酶和中性肽链内切酶以及用于治疗高血压和充血性心力衰竭的用途也被公开并要求保护

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