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21. 发明申请

US20070259899A1 6-(2-Alkyl-Phenyl)-Pyrido[2,3-D]Pyrimidines useful as Proteine Kinase Inhibitors 失效
标题翻译：可用作蛋白激酶抑制剂的6-（2-烷基 - 苯基） - 吡啶并[2,3-D]嘧啶
公开(公告)号：US20070259899A1
公开(公告)日：2007-11-08
申请号：US11660796
申请日：2005-09-20
申请人： Konrad Honold , Wolfgang Schaefer , Stefan Scheiblich
发明人： Konrad Honold , Wolfgang Schaefer , Stefan Scheiblich
IPC分类号： A61K31/519 , C07D487/02
CPC分类号： C07D471/04
摘要： Objects of the present invention are the compounds of formula (I) their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above-mentioned compounds, medicaments containing them and their manufacture, as well as the use of the above-mentioned compounds in the control or prevention of illnesses such as cancer.
摘要翻译：本发明的目的是式（I）化合物的药学上可接受的盐，对映体形式，非对映异构体和外消旋体，上述化合物的制备，含有它们的药物及其制备方法，以及上述用途，提及的化合物在控制或预防诸如癌症的疾病中。

22. 发明申请

US20100120840A1 Heterocyclic benzylamino derivatives, their manufacture and use as pharmaceutical agents 失效
公开(公告)号：US20100120840A1
公开(公告)日：2010-05-13
申请号：US11989272
申请日：2006-07-28
申请人： Edward Boyd , Frederick Brookfield , Jonathan Gridley , Konrad Honold , Raymond Lau , Stefan Scheiblich
发明人： Edward Boyd , Frederick Brookfield , Jonathan Gridley , Konrad Honold , Raymond Lau , Stefan Scheiblich
IPC分类号： A61K31/437 , C07D471/04 , A61P35/00 , A61P37/02
CPC分类号： C07D471/04
摘要： Objects of the present invention are the compounds of formula (I) their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above-mentioned compounds, pharmaceutical compositions containing them and their manufacture, as well as the use of the above-mentioned compounds in the control or prevention of illnesses such as cancer.

23. 发明申请

US20080032970A1 Amide Derivatives of 7-Amino-3-Phenyl-Dihydropyrimido[4,5-D]Pyrimidinones, Their Manufacture and Use as Pharmaceutical Agents 失效
标题翻译： 7-氨基-3-苯基 - 二氢嘧啶并[4,5-D]嘧啶酮的酰胺衍生物及其作为药剂的制造和用途
公开(公告)号：US20080032970A1
公开(公告)日：2008-02-07
申请号：US11660197
申请日：2005-08-30
申请人： Richard Engh , Hubert Hertenberger , Konrad Honold , Birgit Masjost , Petra Rueger , Wolgfang Schaefer , Stefan Scheiblich , Manfred Schwaiger
发明人： Richard Engh , Hubert Hertenberger , Konrad Honold , Birgit Masjost , Petra Rueger , Wolgfang Schaefer , Stefan Scheiblich , Manfred Schwaiger
IPC分类号： A61K31/519 , A61K31/496 , A61K31/535 , A61P43/00 , C07D239/70 , C07D413/00
CPC分类号： C07D487/04
摘要： The present invention relates to novel amide derivatives of 7-amino-3-phenyl dihydropyrimido[4,5-d]pyrimidinones, to a process for their manufacture, medicaments containing them and their manufacture as well as the use of these compounds as pharmaceutically active agents. The present derivatives are new compounds of the general formula (I).
摘要翻译：本发明涉及7-氨基-3-苯基二氢嘧啶并[4,5-d]嘧啶酮的新型酰胺衍生物，其制备方法，含有它们的药物及其制备以及这些化合物作为药物活性的用途代理商本发明的衍生物是通式（I）的新化合物。

24. 发明授权

US07091345B2 Amino-substituted dihydropyrimido[4,5-D]pyrimidinone derivatives 失效
标题翻译：氨基取代的二氢嘧啶并[4,5-D]嘧啶酮衍生物
公开(公告)号：US07091345B2
公开(公告)日：2006-08-15
申请号：US10697543
申请日：2003-10-30
申请人： Jianping Cai , Nikolaos Dimoudis , Konrad Honold , Kin-Chun Luk , Stefan Scheiblich , Hilke Sudergat , Georg Tiefenthaler , Oliver Tonn
发明人： Jianping Cai , Nikolaos Dimoudis , Konrad Honold , Kin-Chun Luk , Stefan Scheiblich , Hilke Sudergat , Georg Tiefenthaler , Oliver Tonn
IPC分类号： C07D471/04 , C07D491/113 , A61K31/519
CPC分类号： C07D487/04 , C07D491/10
摘要： Compounds of formula I are described. These compounds are protein kinase inhibitors, in particular they inhibit the src family tyrosine kinases. Thus, these compounds are useful for the treatment of diseases mediated by src tyrosine kinases, including cell proliferative disorders such as cancer. Also described are methods of making and using compounds of formula I as well as pharmaceutical compositions containing these compounds.
摘要翻译：描述式I化合物。这些化合物是蛋白激酶抑制剂，特别是它们抑制src家族酪氨酸激酶。因此，这些化合物可用于治疗由src酪氨酸激酶介导的疾病，包括细胞增殖性疾病如癌症。还描述了制备和使用式I化合物的方法以及含有这些化合物的药物组合物。

25. 发明授权

US07776878B2 Heterocyclic benzylamino derivatives, their manufacture and use as pharmaceutical agents 失效
标题翻译：杂环苄氨基衍生物，其制备和用作药剂
公开(公告)号：US07776878B2
公开(公告)日：2010-08-17
申请号：US11989272
申请日：2006-07-28
申请人： Edward Boyd , Frederick Brookfield , Jonathan Gridley , Konrad Honold , Raymond Lau , Stefan Scheiblich
发明人： Edward Boyd , Frederick Brookfield , Jonathan Gridley , Konrad Honold , Raymond Lau , Stefan Scheiblich
IPC分类号： A01N47/00 , A61K31/26
CPC分类号： C07D471/04
摘要： Objects of the present invention are the compounds of formula (I) their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above-mentioned compounds, pharmaceutical compositions containing them and their manufacture, as well as the use of the above-mentioned compounds in the control or prevention of illnesses such as cancer.
摘要翻译：本发明的目的是式（I）化合物的药学上可接受的盐，对映体形式，非对映异构体和外消旋体，上述化合物的制备，含有它们的药物组合物及其制备方法以及上述用途用于控制或预防癌症等疾病的化合物。

26. 发明授权

US06673816B1 Rhodanine carboxylic acid derivatives for the treatment and prevention of metabolic bone disorders 失效
标题翻译：用于治疗和预防代谢性骨骼疾病的罗丹明羧酸衍生物
公开(公告)号：US06673816B1
公开(公告)日：2004-01-06
申请号：US09787917
申请日：2001-06-21
申请人： Angelika Esswein , Wolfgang Schaefer , Christos Tsaklakidis , Konrad Honold , Klaus Kaluza
发明人： Angelika Esswein , Wolfgang Schaefer , Christos Tsaklakidis , Konrad Honold , Klaus Kaluza
IPC分类号： A61K31426
CPC分类号： C07D277/20 , C07D277/36 , C07D417/06 , C07D417/12 , C07D493/04
摘要： Compounds of general formula (I), in which m is 0-8, q is a 0-8, a is 0-4, A signifies a single or double bond, R1, R2 signify hydrogen or lower alkyl and, when m signifies 2-8, R1 and R2 in the group CR1═CR2 can have various significances within the following sequence, R3 signifies hydrogen or lower alkyl, X signifies hydrogen or —(CH2)b—COR4 with b=0-4, Y signifies hydrogen, —COR4, phenyl or indolyl residue R4 signifies hydroxyl, lower alkoxy or the NR1R2 residue, W signifies an optionally mono- or polysubstituted saturated or unsaturated mono-, bi- or tricycle which can contain hetero atoms, as well physiologically compatible salts, esters, optically active forms, racemates, tautomers, and derivatives which can be metabolized in vivo to compounds of general formula (I).
摘要翻译：通式（I）的化合物，其中m为0-8，q为0-8，a为0-4，A表示单键或双键，R1，R2表示氢或低级烷基，当m表示 2-8中，基团CR1 = CR2中的R1和R2可以在以下序列中具有各种含义，R3表示氢或低级烷基，X表示氢或 - （CH2）b-COR4，其中b = 0-4，Y表示氢，-COR 4，苯基或吲哚基残基R 4表示羟基，低级烷氧基或NR 1 R 2残基，W表示可以含有杂原子的任选的单取代或多取代的饱和或不饱和单 - ，二 - 或三环，以及生理上相容的盐，酯，光学活性形式，外消旋体，互变异构体和衍生物，其可以在体内被代谢为通式（I）的化合物。

27. 发明授权

US07214532B2 Methods for identifying human cell lines useful for endogenous gene activation, isolated human cell lines identified thereby, and uses thereof 有权
标题翻译：用于鉴定可用于内源基因激活的人细胞系的方法，由此鉴定的分离的人细胞系及其用途
公开(公告)号：US07214532B2
公开(公告)日：2007-05-08
申请号：US10351397
申请日：2003-01-27
申请人： Anne Stern , Michael Brandt , Konrad Honold , Johannes Auer , Hans Koll , Reinhard Franze , Ulrich Pessara
发明人： Anne Stern , Michael Brandt , Konrad Honold , Johannes Auer , Hans Koll , Reinhard Franze , Ulrich Pessara
IPC分类号： C12N15/00
CPC分类号： C07K14/505 , A61K38/00 , C07K2319/02 , C07K2319/036 , C07K2319/75 , C12N15/10 , C12N15/625 , C12P21/005
摘要： The invention concerns human cells which, due to an activation of the endogenous human EPO gene, are able to produce EPO in an adequate quantity and purity to enable a cost-effective production of human EPO as a pharmaceutical preparation. Furthermore the invention concerns a process for the production of such human EPO-producing cells, DNA constructs for the activation of the endogenous EPO gene in human cells as well as a process for the large-scale production of EPO in human cells.
摘要翻译：本发明涉及由于内源性人EPO基因的活化能够产生足够数量和纯度的EPO以使作为药物制剂的人EPO成本有效的生产的人细胞。此外，本发明涉及生产这种人EPO产生细胞的方法，用于激活人细胞内源性EPO基因的DNA构建体以及在人细胞中大规模生产EPO的方法。

28. 发明授权

US07393936B2 Method for the recombinant production and purification of protein kinases 失效
标题翻译：蛋白激酶重组生产和纯化方法
公开(公告)号：US07393936B2
公开(公告)日：2008-07-01
申请号：US11000867
申请日：2004-12-01
申请人： Hubert Hertenberger , Konrad Honold , Christian Klein , Petra Rueger
发明人： Hubert Hertenberger , Konrad Honold , Christian Klein , Petra Rueger
IPC分类号： C07K1/02 , C07K1/14 , C07K1/20 , C12N9/12 , C12N15/70
CPC分类号： C12N9/1205
摘要： A method for the recombinant production and purification of a protein kinase selected from the group consisting of tyrosine protein kinases and serine/threonine kinases by expressing a nucleic acid encoding said kinase in a microbial host cell, forming inclusion bodies containing said kinase, isolating, solubilizing, naturing, and purifying said kinase wherein said purification is performed by hydrophobic interaction with an hydrophobic adsorbent under conditions whereby at least 70% of said protein kinase are not bound to said adsorbent and the protein kinase not bound to said adsorbent is recovered.
摘要翻译：一种通过在微生物宿主细胞中表达编码所述激酶的核酸，重组产生和纯化选自酪氨酸蛋白激酶和丝氨酸/苏氨酸激酶的方法，形成含有所述激酶的包涵体，分离，增溶，变性和纯化所述激酶，其中所述纯化通过与疏水性吸附剂的疏水相互作用进行，其中至少70％的所述蛋白激酶不与所述吸附剂结合，并且不结合所述吸附剂的蛋白激酶被回收。

29. 发明授权

US06548296B1 Methods for identifying human cell lines useful for endogenous gene activation, isolated human lines identified thereby, and uses thereof 失效
标题翻译：用于鉴定可用于内源基因激活的人细胞系的方法，由此鉴定的分离的人系及其用途
公开(公告)号：US06548296B1
公开(公告)日：2003-04-15
申请号：US09113692
申请日：1998-07-10
申请人： Anne Stern , Michael Brandt , Konrad Honold , Johannes Auer , Hans Koll , Reinhard Franze , Ulrich Pessara
发明人： Anne Stern , Michael Brandt , Konrad Honold , Johannes Auer , Hans Koll , Reinhard Franze , Ulrich Pessara
IPC分类号： C12P2106
CPC分类号： C07K14/505 , A61K38/00 , C07K2319/02 , C07K2319/036 , C07K2319/75 , C12N15/10 , C12N15/625 , C12P21/005
摘要： The invention concerns human cells which, due to an activation of the endogenous human EPO gene, are able to produce EPO in an adequate quantity and purity to enable a cost-effective production of human EPO as a pharmaceutical preparation. Furthermore the invention concerns a process for the production of such human EPO-producing cells, DNA constructs for the activation of the endogenous EPO gene in human cells as well as a process for the large-scale production of EPO in human cells.
摘要翻译：本发明涉及由于内源性人EPO基因的活化能够产生足够数量和纯度的EPO以使作为药物制剂的人EPO成本有效的生产的人细胞。此外，本发明涉及生产这种人EPO产生细胞的方法，用于激活人细胞内源性EPO基因的DNA构建体以及在人细胞中大规模生产EPO的方法。

30. 发明授权

US07008764B1 Optimization of cells for endogenous gene activation 有权
标题翻译：内源基因激活的细胞优化
公开(公告)号：US07008764B1
公开(公告)日：2006-03-07
申请号：US09203500
申请日：1998-12-01
申请人： Konrad Honold , Thomas Holtschke , Anne Stern
发明人： Konrad Honold , Thomas Holtschke , Anne Stern
IPC分类号： C12Q1/68
CPC分类号： C07K14/505 , C12N15/63 , C12N15/65 , C12N15/85 , C12N15/90 , C12N15/907 , C12N2800/30 , C12N2830/002 , C12Q1/6897
摘要： The invention concerns a process for optimizing the gene expression in cells. A first aspect concerns a process for changing the expression of a nucleic acid sequence which is present endogenously in a eukaryotic cell by introduction of a heterologous expression control sequence into the genome of the cell by means of homologous recombination as well as site-specific recombinase-mediated excision of inserted foreign DNA and its replacement by further heterologous expression control sequences or/and amplification genes. In addition the invention concerns the introduction of one or several nucleic acid sequences to which an activator protein or an activator protein complex binds e.g. a hypoxia-inducible factor (HIF), into the genome of a eukaryotic cell by homologous recombination in order to change the expression of a target gene. Furthermore the invention concerns a process for testing the influence of 5′ or 3′ non-coding nucleic acid fragments on the expression of a target gene by determining the expression of a reporter gene. In addition the invention concerns a process for providing a DHFR-negative eukaryotic cell containing a recombinase target sequence as well as the expression of a nucleic acid sequence inserted into the recombinase target sequence.
摘要翻译：本发明涉及优化细胞中基因表达的方法。第一方面涉及一种通过将异源表达控制序列通过同源重组以及位点特异性重组酶导入到细胞基因组中而在真核细胞中内源性存在的核酸序列的表达的方法。介导的插入的外源DNA的切除及其通过进一步的异源表达控制序列或/和扩增基因的替代。此外，本发明涉及一种或几种核酸序列的引入，活化蛋白或活化蛋白复合物例如与其结合。缺氧诱导因子（HIF），通过同源重组进入真核细胞的基因组，以改变靶基因的表达。此外，本发明涉及通过测定报告基因的表达来测试5'或3'非编码核酸片段对靶基因表达的影响的方法。此外，本发明涉及提供含有重组酶靶序列的DHFR阴性真核细胞以及插入重组酶靶序列中的核酸序列的表达的方法。

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