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1. 发明专利

HRP970331A2 PYRIDINE FUSED TO A BICYCLIC RING 未知
公开(公告)号：HRP970331A2
公开(公告)日：1998-08-31
申请号：HRP970331
申请日：1997-06-17
申请人： JOACHIM SCHUHMACHER
发明人： SCHUHMACHER JOACHIM
IPC分类号： C07D221/04 , A61K31/435 , A61K31/44 , A61P3/06 , A61P9/00 , A61P9/10 , C07D221/16
摘要： Bicyclic condensed pyridine compounds of formula (I) and their salts and N-oxides are new. A = 6-10C aryl optionally substituted by 1-3 halo, OH, CF3, OCF3 or 1-7C alkyl, acyl, hydroxyalkyl or alkoxy groups, or by one NR3R4 group; R3, R4 = independently H, phenyl or 1-6C alkyl; D = R5-T- or (R6)(R7)(R8)C-; R5, R6 = independently 3-8C cycloalkyl, 6-10C aryl or a 5-7 membered aromatic optionally benzocondensed heterocycle containing 1-3 S, N and/or O heteroatoms, optionally substituted by 1-3 independent halo, OH, CF3, OCF3, COOH, 1-6C alkyl, alkoxy, acyl or alkoxycarbonyl groups, or is substituted by phenyl, phenoxy or thiophenyl groups, themselves optionally substituted by halo, CF3 or OCF3, or the ring systems may be substituted by an NR9R10 group; R9, R10 = as for R3, R4; T = 1-10C alkylene or alkenylene, optionally substituted by 1 or 2 OH groups; R7 = H or halo; R8 = H, halo, azido, CF3, OCF3, OH, 1-5C alkoxy or NR11R12; R11, R12 = as for R3, R4; or R7+R8 = a carbonyl group; E = 3-8C cycloalkyl or 1-8C alkyl which is optionally substituted by 3-8C cycloalkyl or OH; R1+R2 = 1-8C alkylene group which is annelated to a phenyl ring and is substituted by CO, a group of formula (i) or OR13; a = 1-3; R13 = H, 1-6C alkyl, acyl or alkoxycarbonyl or a group of formula Si(R14)(R15)(R16); R14, R15, R16 = independently 1-6C alkyl or phenyl; Both ring systems may be substituted by 1-3 independent halo, COOH or 1-6C alkyl, alkoxy or alkoxycarbonyl groups.

2. 发明授权

US09084829B2 Anti-mesothelin immunoconjugates and uses therefor 有权
标题翻译：抗间皮素免疫缀合物及其用途
公开(公告)号：US09084829B2
公开(公告)日：2015-07-21
申请号：US13318138
申请日：2010-04-16
申请人： Antje Kahnert , Kerstin Berhörster , Iring Heisler , Charlotte Christine Kopitz , Joachim Schuhmacher
发明人： Antje Kahnert , Kerstin Berhörster , Iring Heisler , Charlotte Christine Kopitz , Joachim Schuhmacher
IPC分类号： C07K16/00 , A61K47/48
CPC分类号： C07K16/30 , A61K47/6803 , A61K47/6851 , C07K2317/14 , C07K2317/56 , C07K2317/565
摘要： The present invention provides immunoconjugates composed of antibodies, e.g., monoclonal antibodies, or antibody fragments that bind to mesothelin, that are conjugated to cytotoxic agents, e.g., maytansine, or derivatives thereof, and/or co-administered or formulated with one or more additional anti-cancer agents. The immunoconjugates of the invention can be used in the methods of the invention to treat and/or diagnose and/or monitor cancers, e.g. solid tumors. The immunoconjugates comprise antibodies and functional fragments containing such antigen-binding regions that are specific for the membrane-anchored, 40 kDa mesothelin polypeptide, which is overexpressed in several tumors, such as pancreatic and ovarian tumors, mesothelioma and lung cancer cells.
摘要翻译：本发明提供免疫缀合物，其由抗体组成，例如单克隆抗体或结合间皮素的抗体片段，其与细胞毒性剂例如美登素或其衍生物缀合，和/或与一种或多种另外的附加物共同施用或配制抗癌剂。本发明的免疫缀合物可以用于本发明的方法来治疗和/或诊断和/或监测癌症，例如，实体瘤。免疫缀合物包含抗体和功能片段，其含有对多个肿瘤例如胰腺和卵巢肿瘤，间皮瘤和肺癌细胞中过表达的膜锚定的40kDa间皮素多肽具有特异性的抗原结合区。

3. 发明授权

US08389520B2 Substituted dihydropyrazolones for treating cardiovascular and hematological diseases 有权
公开(公告)号：US08389520B2
公开(公告)日：2013-03-05
申请号：US12447192
申请日：2007-10-12
申请人： Kai Thede , Ingo Flamme , Felix Oehme , Jens-Kerim Ergüden , Friederike Stoll , Joachim Schuhmacher , Hanno Wild , Peter Kolkhof , Hartmut Beck , Jörg Keldenich , Metin Akbaba , Mario Jeske
发明人： Kai Thede , Ingo Flamme , Felix Oehme , Jens-Kerim Ergüden , Friederike Stoll , Joachim Schuhmacher , Hanno Wild , Peter Kolkhof , Hartmut Beck , Jörg Keldenich , Metin Akbaba , Mario Jeske
IPC分类号： A61K31/5377 , C07D413/14
CPC分类号： C07D487/04 , A61K31/427 , A61K31/4439 , A61K31/497 , A61K31/506 , A61K31/5377 , A61K31/55 , A61K31/551 , A61K45/06 , C07D401/14 , C07D403/14 , C07D413/14 , C07D417/14 , C07D471/04
摘要： The present application relates to novel substituted dihydropyrazolone derivatives, processes for their preparation, their use for treatment and/or prophylaxis of diseases and their use for the preparation of medicaments for treatment and/or prophylaxis of diseases, in particular cardiovascular and hematological diseases and kidney diseases, and for promoting wound healing.

4. 发明授权

US08318761B2 Substituted arylsulfonamides as antiviral agents 有权
标题翻译：取代的芳基磺酰胺作为抗病毒剂
公开(公告)号：US08318761B2
公开(公告)日：2012-11-27
申请号：US12203793
申请日：2008-09-03
申请人： Niels Svenstrup , Holger Zimmermann , Dagmar Karthaus , Andreas Goeller , Dirk Heimbach , Kerstin Henninger , Dieter Lang , Daniela Paulsen , Bernd Riedl , Rudolf Schohe-Loop , Joachim Schuhmacher , Tobias Wunberg
发明人： Niels Svenstrup , Holger Zimmermann , Dagmar Karthaus , Andreas Goeller , Dirk Heimbach , Kerstin Henninger , Dieter Lang , Daniela Paulsen , Bernd Riedl , Rudolf Schohe-Loop , Joachim Schuhmacher , Tobias Wunberg
IPC分类号： A01N43/40 , A61K31/435 , A61K31/44
CPC分类号： C07D413/04 , C07D213/73
摘要： The invention relates to substituted arylsulfonamides of formula (I) and methods for their preparation as well as their use for the production of medicaments for the treatment and/or prophylaxis of diseases, especially for use as antiviral agents, particularly against cytomegaloviruses.
摘要翻译：本发明涉及式（I）的取代芳基磺酰胺及其制备方法及其用于生产用于治疗和/或预防疾病的药物的用途，特别是用作抗病毒剂，特别是用于巨细胞病毒的药物。

5. 发明申请

US20120264704A1 SUBSTITUTED DIHYDROPYRAZOLONES AND USE THEREOF AS HIF-PROLYL-4 -HYDROXYLASE INHIBITORS 有权
标题翻译：取代的二氢吡咯烷酮及其作为HIF-PROLYL-4-羟基酶抑制剂的用途
公开(公告)号：US20120264704A1
公开(公告)日：2012-10-18
申请号：US12447201
申请日：2007-10-26
申请人： Kai Thede , Ingo Flamme , Felix Oehme , Jens-Kerim Ergüden , Friederike Stoll , Joachim Schuhmacher , Hanno Wild , Peter Kolkhof , Hartmut Beck , Metin Akbaba , Mario Jeske
发明人： Kai Thede , Ingo Flamme , Felix Oehme , Jens-Kerim Ergüden , Friederike Stoll , Joachim Schuhmacher , Hanno Wild , Peter Kolkhof , Hartmut Beck , Metin Akbaba , Mario Jeske
IPC分类号： A61K31/506 , C07D417/14 , A61K31/4439 , C07D413/14 , A61K31/5377 , A61K31/517 , A61K31/501 , A61K31/4709 , A61K31/497 , A61K31/55 , A61P7/10 , A61K31/616 , A61P31/04 , A61P35/00 , A61K31/7048 , A61P9/00 , A61P7/06 , A61P13/12 , C07D471/04 , A61K31/498 , A61K31/714 , C07D401/14
CPC分类号： C07D417/14 , C07D401/14
摘要： The present application relates to novel substituted dihydropyrazolone derivatives, processes for their preparation, their use for treatment and/or prophylaxis of diseases and their use for the preparation of medicaments for treatment and/or prophylaxis of diseases, in particular cardiovascular and hematological diseases and kidney diseases, and for promoting wound healing.
摘要翻译：本申请涉及新型取代的二氢吡喃酮衍生物，其制备方法，其用于治疗和/或预防疾病及其用于制备用于治疗和/或预防疾病，特别是心血管和血液疾病和肾脏的药物的用途疾病和促进伤口愈合。

6. 发明申请

US20120028950A1 Substituted heterocyclylbenzylpyrazoles and use thereof 失效
标题翻译：取代的杂环基苄基吡唑及其用途
公开(公告)号：US20120028950A1
公开(公告)日：2012-02-02
申请号：US13103305
申请日：2011-05-09
申请人： Michael HÄRTER , Hartmut BECK , Susanne GRESCHAT , Peter ELLINGHAUS , Kerstin BERHÖRSTER , Joachim SCHUHMACHER
发明人： Michael HÄRTER , Hartmut BECK , Susanne GRESCHAT , Peter ELLINGHAUS , Kerstin BERHÖRSTER , Joachim SCHUHMACHER
IPC分类号： A61K31/4245 , A61K31/454 , A61P35/00 , A61P9/10 , A61P9/04 , A61P9/06 , A61P9/12 , A61P11/00 , A61P13/12 , A61P17/06 , A61P27/02 , A61P29/00 , A61P25/00 , A61P7/00 , C07D413/14
CPC分类号： A61K31/454 , A61K31/4245 , A61K45/06 , C07D413/14
摘要： The present application relates to novel substituted 1-[3-(heterocyclyl)benzyl]-1H-pyrazole derivatives, to processes for preparation thereof, to use thereof for treatment and/or prevention of diseases and to use thereof for production of medicaments for treatment and/or prevention of diseases, more particularly for treatment and/or prevention of hyperproliferative and angiogenic diseases and those diseases which arise from metabolic adaptation to hypoxic states. Such treatments can be effected in the form of monotherapy or else in combination with other medicaments or further therapeutic measures.
摘要翻译：本申请涉及新的取代的1- [3-（杂环基）苄基] -1H-吡唑衍生物，其制备方法，其用于治疗和/或预防疾病及其用于生产用于治疗的药物的用途和/或预防疾病，特别是用于治疗和/或预防过度增生和血管生成疾病以及由代谢适应缺氧状态引起的疾病。这样的治疗可以以单一疗法的形式进行，或者与其它药物组合或进一步的治疗措施。

7. 发明申请

US20110143363A1 DETERMINATION OF FREE FRACTIONS 审中-公开
标题翻译：确定自由分类
公开(公告)号：US20110143363A1
公开(公告)日：2011-06-16
申请号：US12815370
申请日：2010-06-14
申请人： Joachim SCHUHMACHER , Christian Kohlsdorfer
发明人： Joachim SCHUHMACHER , Christian Kohlsdorfer
IPC分类号： G01N33/53
CPC分类号： G01N33/5432 , G01N33/94
摘要： The invention relates to methods for the determination of pharmacological properties of substances, such as, e.g., chemical substances. The invention also relates to methods and kits for use in the determination of the free fraction, fu, of pharmacologically active compounds in aqueous solutions and serum. The invention also relates to the above methods in which solid particles, coated with a lipophilic medium, are used.
摘要翻译：本发明涉及用于测定物质（例如化学物质）的药理学性质的方法。本发明还涉及用于测定水溶液和血清中药理活性化合物的游离级分的方法和试剂盒。本发明还涉及其中使用涂有亲脂性介质的固体颗粒的上述方法。

8. 发明授权

US07786079B2 Substituted nonadepsipeptides 失效
标题翻译：取代的非吸收肽
公开(公告)号：US07786079B2
公开(公告)日：2010-08-31
申请号：US11788590
申请日：2007-04-19
申请人： Franz Von Nussbaum , Nina Brunner , Rainer Endermann , Chantal Fuerstner , Elke Hartmann , Jacques Ragot , Guido Schiffer , Joachim Schuhmacher , Niels Svenstrup , Joachim Telser , Sonja Anlauf , Michael-Alexander Bruening
发明人： Franz Von Nussbaum , Nina Brunner , Rainer Endermann , Chantal Fuerstner , Elke Hartmann , Jacques Ragot , Guido Schiffer , Joachim Schuhmacher , Niels Svenstrup , Joachim Telser , Sonja Anlauf , Michael-Alexander Bruening
IPC分类号： A61K38/12 , C07K7/54
CPC分类号： C07K7/06
摘要： The invention relates to nonadepsipeptides and methods for their preparation and their use for the production of medicaments for the treatment and/or prophylaxis of diseases, in particular bacterial infectious diseases.
摘要翻译：本发明涉及非吸收肽及其制备方法及其用于生产用于治疗和/或预防疾病，特别是细菌感染性疾病的药物的用途。

9. 发明授权

US07718611B2 Cyclic nonapeptide amides 失效
标题翻译：环状十肽酰胺
公开(公告)号：US07718611B2
公开(公告)日：2010-05-18
申请号：US11800495
申请日：2007-05-04
申请人： Franz Von Nussbaum , Nina Brunner , Chantal Fuerstner , Rainer Endermann , Jacques Ragot , Joachim Telser , Werner Schroeder , Sonja Anlauf , Joachim Schuhmacher , Elke Hartmann
发明人： Franz Von Nussbaum , Nina Brunner , Chantal Fuerstner , Rainer Endermann , Jacques Ragot , Joachim Telser , Werner Schroeder , Sonja Anlauf , Joachim Schuhmacher , Elke Hartmann
IPC分类号： A61K38/12 , C07K7/54
CPC分类号： C07K7/56
摘要： The invention relates to cyclic nonapeptide amides and to methods for their preparation and to their use for the production of medicaments for the treatment and/or prophylaxis of diseases, especially bacterial infectious diseases.
摘要翻译：本发明涉及环状非肽肽酰胺及其制备方法及其用于生产用于治疗和/或预防疾病，特别是细菌感染性疾病的药物。

10. 发明申请

US20090203582A1 LYSOBACTIN AMIDES 失效
公开(公告)号：US20090203582A1
公开(公告)日：2009-08-13
申请号：US12249888
申请日：2008-10-10
申请人： Franz VON NUSSBAUM , Hartmut Beck , Nina Brunner , Rainer Endermann , Johannes Koebberling , Jacques Ragot , Joachim Telser , Joachim Schuhmacher , Sonja Anlauf , Yolanda Cancho-Grande , Susanne Greschat , Hans-Christian Militzer , Guido Schiffer
发明人： Franz VON NUSSBAUM , Hartmut Beck , Nina Brunner , Rainer Endermann , Johannes Koebberling , Jacques Ragot , Joachim Telser , Joachim Schuhmacher , Sonja Anlauf , Yolanda Cancho-Grande , Susanne Greschat , Hans-Christian Militzer , Guido Schiffer
IPC分类号： A61K38/12 , C07K14/00 , A61P31/04
CPC分类号： C07K7/06 , A61K38/00 , C07K7/56
摘要： The invention relates to lysobactin amides and methods for their preparation, as well as their use for manufacturing medicaments for the treatment and/or prophylaxis of diseases, in particular bacterial infectious diseases.
摘要翻译：本发明涉及溶血酶蛋白酰胺及其制备方法，以及它们用于制备用于治疗和/或预防疾病，特别是细菌感染性疾病的药物的用途。

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