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31. 发明授权

US06271342B1 Sugar-modified cytostatics 失效
标题翻译：糖改性细胞抑制剂
公开(公告)号：US06271342B1
公开(公告)日：2001-08-07
申请号：US08930546
申请日：1997-09-25
申请人： Hans-Georg Lerchen , Karsten von dem Bruch , Uwe Petersen , Jörg Baumgarten , Norbert Piel , Horst-Peter Antonicek , Walter Weichel , Michael Sperzel , Klaus Dieter Bremm
发明人： Hans-Georg Lerchen , Karsten von dem Bruch , Uwe Petersen , Jörg Baumgarten , Norbert Piel , Horst-Peter Antonicek , Walter Weichel , Michael Sperzel , Klaus Dieter Bremm
IPC分类号： A61K3814
CPC分类号： C07D401/04 , A61K31/02 , C07D487/04 , C07H15/203 , C07K9/001 , Y02P20/55
摘要： The invention relates to cytostatics which, by modification with sugar, are tumor-specific. Suitable spacers ensure serum stability and at the same time an intracellular action.
摘要翻译：本发明涉及通过用糖改性的肿瘤特异性的细胞抑制剂。合适的间隔物确保血清稳定性，并同时进行细胞内作用。

32. 发明授权

US5777075A Octacyclodepsipeptides having an endoparasiticidal action 失效
标题翻译：具有内寄生性杀伤作用的Octacyclodepsipeptide
公开(公告)号：US5777075A
公开(公告)日：1998-07-07
申请号：US510084
申请日：1995-08-01
申请人： Jurgen Scherkenbeck , Peter Jeschke , Hans-Georg Lerchen , Hermann Hagemann , Achim Harder , Norbert Mencke , Andrew Plant
发明人： Jurgen Scherkenbeck , Peter Jeschke , Hans-Georg Lerchen , Hermann Hagemann , Achim Harder , Norbert Mencke , Andrew Plant
IPC分类号： A01N43/72 , A61K31/395 , A61K38/00 , A61P33/10 , C07C235/12 , C07C235/34 , C07D273/00 , C07K1/113 , C07K11/00 , C07K11/02 , A61K38/15
CPC分类号： C07D273/00 , C07C235/12 , C07C235/34
摘要： The present invention relates to the use of open-chain octadepsipeptides of the general formula: ##STR1## wherein the R variables have been defined in the specification.
摘要翻译：本发明涉及以下通式的开链八肽缩氨酸的用途：其中R变量已在说明书中定义。

33. 发明授权

US09040566B2 Adenosine A1 agonists for the treatment of glaucoma and ocular hypertension 有权
标题翻译：腺苷A1激动剂治疗青光眼和高眼压症
公开(公告)号：US09040566B2
公开(公告)日：2015-05-26
申请号：US13819790
申请日：2011-08-29
申请人： Jürgen Klar , Georges Von Degenfeld , Hans-Georg Lerchen , Barbara Albrecht-Küpper , Andreas Knorr , Peter Sandner , Daniel Meibom
发明人： Jürgen Klar , Georges Von Degenfeld , Hans-Georg Lerchen , Barbara Albrecht-Küpper , Andreas Knorr , Peter Sandner , Daniel Meibom
IPC分类号： A01N43/40 , A61K31/44 , C07D409/00 , C07D411/00 , C07D405/00 , C07D417/12 , A61K9/00 , A61K9/08 , A61K31/4439 , A61K45/06 , C07D413/12 , C07D417/14
CPC分类号： A61K31/4439 , A61K9/0048 , A61K9/08 , A61K38/05 , A61K45/06 , C07D413/12 , C07D417/12 , C07D417/14
摘要： The present invention relates to the use of selective adenosine A1 agonists, in particular the dicyanopyridines of formula (I), for the treatment and/or prophylaxis of glaucoma and ocular hypertension as well as the their use for the production of a medicament for the treatment and/or prophylaxis of glaucoma and ocular hypertension.
摘要翻译：本发明涉及选择性腺苷A1激动剂，特别是式（I）的二氰基吡啶用于治疗和/或预防青光眼和高眼压症及其用于生产治疗药物的用途的用途和/或预防青光眼和高眼压症。

34. 发明授权

US07220824B1 Integrin-mediated drug targeting 有权
标题翻译：整合素介导的药物靶向
公开(公告)号：US07220824B1
公开(公告)日：2007-05-22
申请号：US10070208
申请日：2000-08-28
申请人： Hans-Georg Lerchen , Jörg Baumgarten , Ulf Brüggemeier , Markus Albers , Andreas Schoop , Thomas-J. Schulze
发明人： Hans-Georg Lerchen , Jörg Baumgarten , Ulf Brüggemeier , Markus Albers , Andreas Schoop , Thomas-J. Schulze
IPC分类号： A61K38/14
CPC分类号： C07D491/22
摘要： The present invention relates to cytostatics which have a tumour-specific action as a result of linkage to αvβ3 integrin antagonists via preferred linking units. The preferred linking units guarantee serum stability of the conjugate of cytostatic and αvβ3 integrin antagonist and at the same time the desired intracellular action in tumour cells as a result of their enzymatic or hydrolytic cleavability with release of the cytostatic.
摘要翻译：本发明涉及通过优选连接单元与α-β3整联蛋白拮抗剂连接而具有肿瘤特异性作用的细胞抑制剂。优选的连接单元保证细胞生长抑制和α3β3整联蛋白拮抗剂的缀合物的血清稳定性，同时由于它们的结合，肿瘤细胞中期望的细胞内作用酶促或水解裂解性，释放细胞抑制作用。

35. 发明申请

US20050069961A1 Isotope-coded affinity tag 审中-公开
标题翻译：同位素编码亲和力标签
公开(公告)号：US20050069961A1
公开(公告)日：2005-03-31
申请号：US10494997
申请日：2002-10-28
申请人： Oswald Lockoff , Thomas Lehmann , Hans-Georg Lerchen , Dorian Immler , Hans-Ulrich Siegmund
发明人： Oswald Lockoff , Thomas Lehmann , Hans-Georg Lerchen , Dorian Immler , Hans-Ulrich Siegmund
IPC分类号： A61K47/48 , A61K51/08 , G01N33/532 , G01N33/68 , G01N33/53 , C07D498/02
CPC分类号： G01N33/6848 , A61K47/665 , A61K51/088 , B82Y5/00 , G01N33/532
摘要： The invention relates to novel isotope-coded affinity tags for use in mass-spectrometric analysis of proteins. The invention also relates to the production and use of these novel tags.
摘要翻译：本发明涉及用于蛋白质质谱分析的新型同位素编码亲和标签。本发明还涉及这些新型标签的生产和使用。

36. 发明授权

US06369028B1 Octacyclodepsipeptides having an endoparasiticidal action 失效
标题翻译：具有内寄生性杀伤作用的Octacyclodepsipeptide
公开(公告)号：US06369028B1
公开(公告)日：2002-04-09
申请号：US08246029
申请日：1994-05-19
申请人： Jürgen Scherkenbeck , Peter Jeschke , Hans-Georg Lerchen , Hermann Hagemann , Achim Harder , Norbert Mencke , Andrew Plant
发明人： Jürgen Scherkenbeck , Peter Jeschke , Hans-Georg Lerchen , Hermann Hagemann , Achim Harder , Norbert Mencke , Andrew Plant
IPC分类号： A61K3800
CPC分类号： C07D273/00 , C07C235/12 , C07C235/34
摘要： The present invention relates to compounds of the general formula (I) in which R1, R2, R11 and R12 represent the same or different radicals selected from the group of C1-8-alkyl, C1-8-halogenoalkyl, C3-6-cycloalkyl, aralkyl or aryl, R3, R5, R7, R9, represent the same or different radicals selected from the group of hydrogen or straight-chain C1-5-alkyl or branched C4-7-alkyl which may optionally be substituted by hydroxyl, C1-4-alkoxy, carboxyl carboxamide, imidazolyl, indolyl, guanidino, —SH or C1-4-alkylthio, and furthermore represents aryl, aralkyl or heteroarylmethyl which may be substituted by halogen, hydroxyl, C1-4-alkyl, C1-4-alkoxy, nitro or a —NR13R14 group in which R13 and R14 independently from each other represent hydrogen or alkyl or together with the adjoining nitrogen atom forms a 5, 6 or 7-membered ring which is optionally interrupted by O, S or N and which is optionally C1-4-alkyl substituted, R4, R6, R8, R10 represent the same or different radicals selected from the group of hydrogen, straight-chain C1-5-alkyl and represents isopropyl, sec.-butyl, t-butyl, C2-6-alkenyl, C3-7-cycloalkyl, which may optionally be substituted by hydroxyl, C1-4-alkoxy, carboxyl, carboxamide, imidazolyl, indolyl, guanidino, SH or C1-4-alkylthio and represent aryl, aralkyl or heteroarylmethyl which may be substituted by halogen, hydroxyl, C1-4-alkyl, C1-4-alkoxy, and stereoisomers thereof, to processes for their preparation and to their use as endoparasiticides.
摘要翻译：本发明涉及通式（I）的化合物，其中R 1，R 2，R 11和R 12表示相同或不同的选自C 1-8 - 烷基，C 1-8 - 卤代烷基，C 3-6 - 环烷基，芳烷基或芳基，R 3，R 5，R 7，R 9表示相同或不同的选自氢或直链C 1-5烷基或支链C 4-7 - 烷基的基团，其可任选被羟基，C 1-4 烷氧基，羧基羧酰胺，咪唑基，吲哚基，胍基，-SH或C 1-4 - 烷硫基，此外表示可被卤素，羟基，C 1-4 - 烷基，C 1-4 - 烷氧基，硝基取代的芳基，芳烷基或杂芳基甲基或-NR 13 R 14基团，其中R 13和R 14彼此独立地表示氢或烷基或与相邻的氮原子一起形成可选地被O，S或N中断的5,6或7-元环，并且其任选地为C1 R 4，R 6，R 8，R 10表示选自该基团的相同或不同的基团的氢，直链C1-5 - 烷基，代表异丙基，仲丁基，叔丁基，C 2-6 - 烯基，C 3-7 - 环烷基，其可任选被羟基，C 1-4 - 烷氧基，羧基，羧酰胺，咪唑基，吲哚基，胍基，SH或C 1-4 - 烷硫基，代表可被卤素，羟基，C 1-4 - 烷基，C 1-4 - 烷氧基及其立体异构体取代的芳基，芳烷基或杂芳基甲基，其制备方法及其作为内寄生物杀虫剂的用途。

37. 发明授权

US5874438A 2,2'-bridged bis-2,4-diaminoquinazolines 失效
标题翻译： 2,2'-桥连双-2,4-二氨基喹唑啉
公开(公告)号：US5874438A
公开(公告)日：1999-02-23
申请号：US729128
申请日：1996-10-11
申请人： Rudolf Schohe-Loop , Peter-Rudolf Seidel , William Bullock , Walter Hubsch , Achim Feurer , Hans-Georg Lerchen , Georg Terstappen , Joachim Schuhmacher , Franz-Josef van der Staay , Bernard Schmidt , Richard J. Fanelli , Jane C. Chisholm , Richard T. McCarthy
发明人： Rudolf Schohe-Loop , Peter-Rudolf Seidel , William Bullock , Walter Hubsch , Achim Feurer , Hans-Georg Lerchen , Georg Terstappen , Joachim Schuhmacher , Franz-Josef van der Staay , Bernard Schmidt , Richard J. Fanelli , Jane C. Chisholm , Richard T. McCarthy
IPC分类号： C07D239/95 , C07D401/14 , C07D403/14 , A01N43/54 , C07D239/72 , C07D401/00
CPC分类号： C07D401/14 , C07D239/95 , C07D403/14
摘要： The present invention relates to 2,2'-bridged bis-2,4-diaminoquinazolines of the general formula (I): ##STR1## in which the indicated substituents are as defined in the description. The invention also provides processes for the preparation of the compounds of the formula (I), their use for the preparation of drugs, and drugs containing said compounds.
摘要翻译：本发明涉及通式（I）的2,2'-桥连双-2,4-二氨基喹唑啉：其中所述取代基如说明书中所定义。本发明还提供了制备式（I）化合物，其制备药物的用途和含有所述化合物的药物的方法。

38. 发明授权

US5760230A 4, 4'-bridged bis-2, 4-diaminoquinazolines 失效
标题翻译： 4,4'-桥连双-2,4-二氨基喹唑啉
公开(公告)号：US5760230A
公开(公告)日：1998-06-02
申请号：US728927
申请日：1996-10-11
申请人： Rudolf Schohe-Loop , Peter-Rudolf Seidel , William Bullock , Achim Feurer , Hans-Georg Lerchen , Georg Terstappen , Joachim Schuhmacher , Franz-Josef van der Staay , Bernard Schmidt , Richard J. Fanelli , Jane C. Chisholm , Richard T. McCarthy
发明人： Rudolf Schohe-Loop , Peter-Rudolf Seidel , William Bullock , Achim Feurer , Hans-Georg Lerchen , Georg Terstappen , Joachim Schuhmacher , Franz-Josef van der Staay , Bernard Schmidt , Richard J. Fanelli , Jane C. Chisholm , Richard T. McCarthy
IPC分类号： C07D239/95 , C07D239/00 , A61K31/505
CPC分类号： C07D239/95
摘要： 4,4'-Bridged bis-2,4-diaminoquinazolines of the general formula (I) ##STR1## processes for their preparation and use as agents acting on the potassium channels of the brain.
摘要翻译：通式（I）的4,4'-桥联双-2,4-二氨基喹唑啉（I）处理其制备和用作作用于脑的钾通道的试剂。

39. 发明申请

US20140127240A1 Novel Binder-Drug Conjugates (ADCs) and Use of Same 审中-公开
标题翻译：新型粘合剂 - 药物共轭物（ADC）及其使用
公开(公告)号：US20140127240A1
公开(公告)日：2014-05-08
申请号：US14113070
申请日：2012-04-20
申请人： Hans-Georg Lerchen , Lars Linden , Sherif El Sheikh , Jörg Willuda , Charlotte C. Kopitz , Joachim Schuhmacher , Simone Greven , Christoph Mahlert , Beatrix Stelte-Ludwig , Sven Golfier , Rudolf Beier , Iring Heisler , Axel Harrenga , Karl-Heinz Thierauch , Sandra Bruder , Heike Petrul , Hannah Jörißen , Sandra Brokowski
发明人： Hans-Georg Lerchen , Lars Linden , Sherif El Sheikh , Jörg Willuda , Charlotte C. Kopitz , Joachim Schuhmacher , Simone Greven , Christoph Mahlert , Beatrix Stelte-Ludwig , Sven Golfier , Rudolf Beier , Iring Heisler , Axel Harrenga , Karl-Heinz Thierauch , Sandra Bruder , Heike Petrul , Hannah Jörißen , Sandra Brokowski
IPC分类号： A61K47/48 , C07K5/06 , A61K45/06
CPC分类号： A61K31/40 , A61K31/4025 , A61K31/404 , A61K31/422 , A61K31/4245 , A61K31/5355 , A61K31/536 , A61K31/537 , A61K31/5377 , A61K39/3955 , A61K45/06 , A61K47/542 , A61K47/6803 , A61K47/6851 , A61K47/6859 , A61K47/6869 , A61K47/6889 , C07K5/0205 , C07K5/0207 , C07K5/06 , C07K5/06034 , C07K5/06052 , C07K5/0606 , C07K7/02 , C07K7/06 , C07K16/18 , C07K16/28 , C07K16/2812 , C07K16/2863 , C07K16/30 , C07K2317/21 , C07K2317/24 , C07K2317/565 , C07K2317/76
摘要： The present patent application relates to novel binder-drug conjugates (ADCs) of N,N-dialkylauristatins directed against the target epidermal growth factor receptor (EGFR, gene ID 1956), effective metabolites of these ADCs, methods for producing these ADCs, use of these ADCs for treatment and or prevention of diseases as well as the use of these ADCs to produce pharmaceutical drugs for treatment and/or prevention of diseases, in particular hyperproliferative and/or angiogenic diseases such as cancer, for example. Such treatments may be administered as monotherapy or in combination with other pharmaceutical drugs or other therapeutic measures.
摘要翻译：本专利申请涉及针对靶表皮生长因子受体（EGFR，基因ID 1956）的N，N-二烷基硫酸锡的新型粘合剂 - 药物共轭物（ADC），这些ADC的有效代谢物，制备这些ADC的方法，这些ADC用于治疗和/或预防疾病，以及使用这些ADC来制备用于治疗和/或预防疾病，特别是过度增生和/或血管发生疾病例如癌症的药物。这样的治疗可以作为单一疗法或与其它药物或其他治疗措施组合施用。

40. 发明申请

US20140080763A1 N-CARBOXYALKYLAURISTATINS AND USE THEREOF 有权
标题翻译： N-羧酸氧化酶及其用途
公开(公告)号：US20140080763A1
公开(公告)日：2014-03-20
申请号：US14004699
申请日：2012-03-12
申请人： Hans-Georg Lerchen , Sherif El Sheikh , Beatrix Stelte-Ludwig , Joachim Schuhmacher , Mark Gnoth
发明人： Hans-Georg Lerchen , Sherif El Sheikh , Beatrix Stelte-Ludwig , Joachim Schuhmacher , Mark Gnoth
IPC分类号： A61K38/07 , A61K45/06 , C07K5/103
CPC分类号： A61K38/07 , A61K38/00 , A61K45/06 , A61K47/6415 , C07K5/0205
摘要： The present application relates to new derivatives, substituted on the N terminus by a carboxyalkyl group, of monomethylauristatin E and monomethylauristatin F, to processes for preparing these derivatives, to the use of these derivatives for treating and/or preventing diseases, and to the use of these derivatives for producing medicaments for treating and/or preventing diseases, more particularly hyperproliferative and/or angiogenic disorders such as cancer disorders, for example. Such treatments may be applied as a monotherapy or else in combination with other medicaments or further therapeutic measures.
摘要翻译：本申请涉及在N末端被羧基烷基取代的单甲基海洛定蛋白E和单甲基海洛定蛋白F的新衍生物，用于制备这些衍生物的方法，这些衍生物用于治疗和/或预防疾病的用途和用途的这些衍生物用于制备用于治疗和/或预防疾病的药物，更具体地是过度增殖和/或血管生成障碍，例如癌症病症。这样的治疗可以作为单一疗法应用，也可以与其它药物组合使用或其它治疗措施。

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