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1. 发明授权

US5837462A Tumorigenic cell lines altered by genetic engineering and their use for the testing of antitumor drugs 失效
标题翻译：通过基因工程改变的致瘤细胞系及其用于测试抗肿瘤药物
公开(公告)号：US5837462A
公开(公告)日：1998-11-17
申请号：US746383
申请日：1996-11-08
申请人： Thomas Beckers , Thomas Klenner , Silke Baasner
发明人： Thomas Beckers , Thomas Klenner , Silke Baasner
IPC分类号： C12N15/09 , A61P35/00 , C07H21/04 , C07K14/71 , C12N5/10 , C12N9/12 , C12N9/16 , C12Q1/18 , C12Q1/42 , C12R1/91 , C12Q1/68
CPC分类号： C12N9/16 , C07K14/71 , C12Q1/42 , C07K2319/02
摘要： The invention describes a novel method for determining the mass of vital tumor cells of xenotransplants in animal models. Cells altered by genetic engineering which form a tumor after transplantation synthesize an excreted reporter gene. This is shown by way of example for a secreted form of human placenta-specific, alkaline phosphate (SEAP). The latter can be demonstrated in the serum of test animals or in culture supernatants. The activity of SEAP in the serum correlates with the number of vital tumor cells in the animal and can be measured prior to the formation of a palpable tumor. The invention shows the use of cell lines altered by genetic engineering in such a manner in subcutaneous and orthotopic tumor models. Dicistronic, eukaryotic expression vectors are used for the stable transfection of the mammalian cell lines or tumor cells used. These vectors contain, under the control of a constitutive or inducible promotor element, the gene coding for SEAP, coupled with a second gene. This latter gene codes e.g. for a receptor tyrosine kinase such as erbB2/HER2 which transforms during overexpression.
摘要翻译：本发明描述了用于确定动物模型中异种移植物的重要肿瘤细胞的质量的新方法。通过基因工程改变的细胞在移植后形成肿瘤合成排泄的报道基因。这通过例如人胎盘特异性碱性磷酸盐（SEAP）的分泌形式的方式示出。后者可以在测试动物的血清或培养物上清液中证实。血清中SEAP的活性与动物中重要的肿瘤细胞的数量相关，并且可以在形成可触及的肿瘤之前测量。本发明显示了通过基因工程改变的细胞系在皮下和原位肿瘤模型中的使用。双顺反子，真核表达载体用于稳定转染所用的哺乳动物细胞系或肿瘤细胞。这些载体在组成型或诱导型启动子元件的控制下含有编码SEAP的基因，加上第二个基因。后一种基因编码例如用于在过表达期间转化的受体酪氨酸激酶如erbB2 / HER2。

2. 发明授权

US06403636B1 Xanthone compounds, their preparation and use as medicament 失效
标题翻译：呫吨酮化合物，其制备和用作药物
公开(公告)号：US06403636B1
公开(公告)日：2002-06-11
申请号：US09605650
申请日：2000-06-28
申请人： Vichai Reutrakul , Thaiwatchai Santisuk , Gerhard Noessner , Juergen Schmidt , Bernd Nickel , Thomas Klenner , Sebastian Hose
发明人： Vichai Reutrakul , Thaiwatchai Santisuk , Gerhard Noessner , Juergen Schmidt , Bernd Nickel , Thomas Klenner , Sebastian Hose
IPC分类号： A61K31352
CPC分类号： C07D493/20
摘要： This invention relates to novel xanthone compounds, their preparation and use as medicament. More particularly this invention is directed to the isolation of the novel xanthone natural product sootepenseone from Dasymaschalon sootepense Craib, Annonaceae, its identification and derivatization, and the use of sootepenseone and its derivatives as anticancer agents.
摘要翻译：本发明涉及新型的呫吨酮化合物，其制备和作为药物的用途。更具体地，本发明涉及从Dasymaschalon sootepense Craib，Annonaceae分离出新型呫吨酮天然产物白藜芦酮，其鉴定和衍生化，以及使用烟灰one素及其衍生物作为抗癌剂。

3. 发明授权

US5942493A LH-RH antagonists having improved action 失效
标题翻译：具有改善作用的LH-RH拮抗剂
公开(公告)号：US5942493A
公开(公告)日：1999-08-24
申请号：US87274
申请日：1998-05-28
申请人： Bernhard Kutscher , Michael Bernd , Thomas Beckers , Thomas Klenner , Peter-Paul Emig , Patricia-Marie Charpentier
发明人： Bernhard Kutscher , Michael Bernd , Thomas Beckers , Thomas Klenner , Peter-Paul Emig , Patricia-Marie Charpentier
IPC分类号： C07D207/26 , C07D207/27 , C07D209/08 , C07D213/61 , C07D213/64 , C07D213/75 , C07D213/80 , C07D215/22 , C07D231/56 , C07D233/26 , C07D235/14 , C07D239/42 , C07D257/04 , C07D307/52 , C07D471/04 , C07D521/00 , A61K38/00 , A61K38/02 , C07K5/00 , C07K7/00
CPC分类号： C07D249/08 , C07D207/27 , C07D209/08 , C07D213/61 , C07D213/64 , C07D213/75 , C07D213/80 , C07D215/22 , C07D231/12 , C07D231/56 , C07D233/26 , C07D233/56 , C07D235/14 , C07D239/42 , C07D257/04 , C07D307/52 , C07D471/04
摘要： New LH-RH antagonists are disclosed, in particular peptidomimetics and peptides modified in a side chain, their salts with pharmaceutically acceptable acids and a process for preparing these LH-RH antagonists and their salts. The disclosed peptides represent analogues of the luteinising hormone releasing hormone (LH-RH). The disclosed compounds have a high antagonistic power and are free of undesirable side effects, in particular edematogenic effects.
摘要翻译：公开了新的LH-RH拮抗剂，特别是肽模拟物和侧链修饰的肽，其与药学上可接受的酸的盐和制备这些LH-RH拮抗剂及其盐的方法。所公开的肽代表黄体生成激素释放激素（LH-RH）的类似物。所公开的化合物具有高的拮抗力并且没有不期望的副作用，特别是水肿作用。

4. 发明授权

US07452910B2 Indolyl-3-glyoxylic acid derivatives having therapeutically valuable properties 失效
标题翻译：具有治疗有价值性质的吲哚基-3-乙醛酸衍生物
公开(公告)号：US07452910B2
公开(公告)日：2008-11-18
申请号：US10686809
申请日：2003-10-17
申请人： Bernd Nickel , Gerald Bacher , Thomas Klenner , Thomas Beckers , Peter Emig , Jürgen Engel , Erik Bruyneel , Günter Kamp , Kirsten Peters
发明人： Bernd Nickel , Gerald Bacher , Thomas Klenner , Thomas Beckers , Peter Emig , Jürgen Engel , Erik Bruyneel , Günter Kamp , Kirsten Peters
IPC分类号： A61K31/44
CPC分类号： A61K31/496 , A61K31/404 , A61K31/4178 , A61K31/4427 , A61K31/4439 , A61K31/444 , A61K31/4709
摘要： The invention relates to the use of N-substituted indole-3-glyoxylamides of the general Formula I: and to pharmaceutical compositions having antitumor action.
摘要翻译：本发明涉及通式I的N-取代的吲哚-3-乙醛酰胺以及具有抗肿瘤作用的药物组合物。

5. 发明申请

US20080057124A1 Indolyl-3-glyoxylic acid derivatives having therapeutically valuable properties 审中-公开
标题翻译：具有治疗有价值性质的吲哚基-3-乙醛酸衍生物
公开(公告)号：US20080057124A1
公开(公告)日：2008-03-06
申请号：US11894729
申请日：2007-08-20
申请人： Bernd Nickel , Gerald Bacher , Thomas Klenner , Thomas Beckers , Peter Emig , Jurgen Engel , Erik Bruyneel , Gunter Kamp , Kirsten Peters
发明人： Bernd Nickel , Gerald Bacher , Thomas Klenner , Thomas Beckers , Peter Emig , Jurgen Engel , Erik Bruyneel , Gunter Kamp , Kirsten Peters
IPC分类号： A61K9/28 , A61K31/404 , A61K31/4427 , A61P35/00 , A61K31/496
CPC分类号： A61K31/496 , A61K31/404 , A61K31/4178 , A61K31/4427 , A61K31/4439 , A61K31/444 , A61K31/4709
摘要： The invention relates to the use of N-substituted indole-3-glyoxylamides of the general and to pharmaceutical compositions having antitumor action.
摘要翻译：本发明涉及具有抗肿瘤作用的一般药物组合物和N-取代吲哚-3-乙醛酰胺的用途。

6. 发明授权

US06696428B2 Use of dopamine receptor antagonists in palliative tumor therapy 失效
标题翻译：多巴胺受体拮抗剂在姑息性肿瘤治疗中的应用
公开(公告)号：US06696428B2
公开(公告)日：2004-02-24
申请号：US10210881
申请日：2002-08-02
申请人： Bernd Nickel , Peter Hilgard , Thomas Klenner , Jürgen Engel
发明人： Bernd Nickel , Peter Hilgard , Thomas Klenner , Jürgen Engel
IPC分类号： A61K31685
CPC分类号： A61K31/685 , A61K31/454 , A61K2300/00
摘要： The side effect of decrease in body weight caused by the alkylphosphocholines such as miltefosine can be antagonized by certain acetylcholine receptor antagonists such as domperidone and pimozide. The combination of alkylphosphocholine plus the antagonist does not have any effect on the anti-tumor action of the alkylphosphocholine. The combination also caused no new side effects in the animals.
摘要翻译：某些乙酰胆碱受体拮抗剂如多潘立酮和匹莫齐特可以拮抗由诸如米替芬等烷基磷酰胆碱引起的体重下降的副作用。烷基磷酸加上拮抗剂的组合对烷基磷酸胆碱的抗肿瘤作用没有任何影响。该组合也不会在动物中产生新的副作用。

7. 发明授权

US06693119B2 Indolyl-3-glyoxylic acid derivatives having therapeutically valuable properties 失效
标题翻译：具有治疗有价值性质的吲哚基-3-乙醛酸衍生物
公开(公告)号：US06693119B2
公开(公告)日：2004-02-17
申请号：US09492531
申请日：2000-01-27
申请人： Bernd Nickel , Gerald Bacher , Thomas Klenner , Thomas Beckers , Peter Emig , Jürgen Engel , Erik Bruyneel , Günter Kamp , Kirsten Peters
发明人： Bernd Nickel , Gerald Bacher , Thomas Klenner , Thomas Beckers , Peter Emig , Jürgen Engel , Erik Bruyneel , Günter Kamp , Kirsten Peters
IPC分类号： A61K3144
CPC分类号： A61K31/496 , A61K31/404 , A61K31/4178 , A61K31/4427 , A61K31/4439 , A61K31/444 , A61K31/4709
摘要： The invention relates to the use of N-substituted indole-3-glyoxylamides of the general Formula I and to pharmaceutical compositions having antitumor action.
摘要翻译：本发明涉及通式I的N-取代吲哚-3-乙醛酰胺与具有抗肿瘤作用的药物组合物的用途。

8. 发明授权

US06272017B1 Adaptor for connecting a chip card to a computer slot 失效
标题翻译：用于将芯片卡连接到计算机插槽的适配器
公开(公告)号：US06272017B1
公开(公告)日：2001-08-07
申请号：US09212846
申请日：1998-12-16
申请人： Dieter Klatt , Heinz Ungermann , Bernhard Pelke , Arnd Bäcker , Thomas Klenner
发明人： Dieter Klatt , Heinz Ungermann , Bernhard Pelke , Arnd Bäcker , Thomas Klenner
IPC分类号： H05K114
CPC分类号： G06K7/0021 , Y10S439/945
摘要： An adaptor for connecting a chip card to a PCMCIA-standard computer slot has a housing with a top cover, a separate bottom cover, and at least one intermediate insulative element or frame connecting the top cover to the bottom cover at a spacing to one another. The top cover and bottom cover have substantially congruent outer contours. The housing has a receiving channel. A printed circuit board is mounted in the housing and extends parallel to the receiving channel. The circuit board has contact elements for electrically contacting a chip card received in the receiving channel. The housing has a front face and a back face wherein the front face has an insertion slot communicating with the receiving channel. The back face has a contact plug electrically connected to the printed circuit board and adapted to electrically contact the PCMCIA-standard computer slot. Cams at the channel entrance are used for card retention. The intermediate element is formed of plural parts which are joined by pins fitted into holes and which are molded about tabs that extend from the covers.
摘要翻译：用于将芯片卡连接到PCMCIA标准计算机插槽的适配器具有壳体，其具有顶盖，单独的底盖以及至少一个中间绝缘元件或框架，所述至少一个中间绝缘元件或框架以彼此间隔连接顶盖至底盖。顶盖和底盖具有大致一致的外轮廓。外壳有一个接收通道。印刷电路板安装在壳体中并且平行于接收通道延伸。电路板具有用于电接触接收在接收通道中的芯片卡的接触元件。壳体具有前表面和后表面，其中前表面具有与接收通道连通的插槽。背面具有电连接到印刷电路板并且适于电接触PCMCIA标准计算机插槽的接触插头。通道入口处的凸轮用于卡片保持。中间元件由多个部件形成，所述多个部件通过装配到孔中的销连接并且围绕从盖延伸的突出部成型。

9. 发明授权

US6093704A Use of dopamine receptor antagonists in palliative tumor therapy 失效
公开(公告)号：US6093704A
公开(公告)日：2000-07-25
申请号：US986235
申请日：1997-12-05
申请人： Bernd Nickel , Peter Hilgard , Thomas Klenner , Jurgen Engel
发明人： Bernd Nickel , Peter Hilgard , Thomas Klenner , Jurgen Engel
IPC分类号： A61K45/00 , A61K31/445 , A61K31/454 , A61K31/685 , A61P35/00 , A61P39/00 , A61P43/00
CPC分类号： A61K31/685 , A61K31/454
摘要： The side effect of decrease in body weight caused by the alkylphosphocholines such as miltefosine can be antagonized by certain acetylcholine receptor antagonists such as domperidone and pimozide. The combination of alkylphosphocholine plus the antagonist does not have any effect on the anti-tumor action of the alkylphosphocholine. The combination also caused no new side effects in the animals.

10. 发明授权

US5556836A Use of D-glucopyranuronic acids and their derivatives for incorporation in pharmacologically active peptides and their salts 失效
标题翻译： D-吡喃葡萄糖醛酸及其衍生物在药理学活性肽及其盐中的应用
公开(公告)号：US5556836A
公开(公告)日：1996-09-17
申请号：US332071
申请日：1994-11-01
申请人： Erich G. Roedern , Horst Kessler , Bernhard Kutscher , Michael Bernd , Thomas Klenner
发明人： Erich G. Roedern , Horst Kessler , Bernhard Kutscher , Michael Bernd , Thomas Klenner
IPC分类号： C07H7/027 , A61K38/00 , C07D309/10 , C07D309/14 , C07H15/04 , C07K7/23 , C07K9/00 , C07K14/575 , C07K14/655 , A61K38/09 , A61K38/14
CPC分类号： C07H15/04 , C07D309/10 , C07D309/14 , C07K14/6555 , C07K7/23 , C07K9/001 , C07K9/006 , A61K38/00 , Y02P20/582 , Y10S930/13
摘要： Use of 7-amino-L-glycero-L-gulo-2,6-anhydro-7-desoxy-heptonic acid and 2-benzoxycarbonylamino-0.sup.1 -methyl-2-desoxy-.beta.-glucopyranuronic acid, their derivatives and the enantiomorphous compounds for incorporation and for manufacture in pharmacologically active peptide hormones.
摘要翻译：使用7-氨基-L-甘油基-L-古洛-2,6-脱水-7-脱氧庚糖酸和2-苯氧基羰基氨基-α-甲基-2-脱氧-β-吡喃葡萄糖醛酸，其衍生物和对映体化合物用于药物活性肽激素的并入和制造。

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