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1. 发明申请

US20140018372A1 CRYSTALLINE FORM OF A INDOLINONE DERIVATIVE AND ITS USE 审中-公开
标题翻译：吲哚啉酮衍生物的结晶形式及其用途
公开(公告)号：US20140018372A1
公开(公告)日：2014-01-16
申请号：US13937432
申请日：2013-07-09
申请人： Gerd-Michael MAIER , Anke BAUM , Bodo BETZEMEIER , Manuel HENRY , Rolf HERTER , Ulrich REISER , Patrizia SINI , Dirk WEBER , Ulrike WERTHMANN , Stephan Karl ZAHN
发明人： Gerd-Michael MAIER , Anke BAUM , Bodo BETZEMEIER , Manuel HENRY , Rolf HERTER , Ulrich REISER , Patrizia SINI , Dirk WEBER , Ulrike WERTHMANN , Stephan Karl ZAHN
IPC分类号： C07D209/34 , A61K31/437 , A61K31/506 , A61K31/4045
CPC分类号： C07D209/34 , A61K31/4045 , A61K31/437 , A61K31/506 , C12Q1/6886 , C12Q2600/106 , C12Q2600/156
摘要： A crystalline form of 3-{3-[1-(4-Dimethylaminomethyl-phenylamino)-1-phenyl-meth-(Z)-ylidene]-2-oxo-2,3-dihydro-1H-indol-6-yl}-propynoic acid ethylamide.
摘要翻译： 3- {3- [1-（4-二甲基氨基甲基 - 苯基氨基）-1-苯基 - 甲基 - （Z） - 亚基] -2-氧代-2,3-二氢-1H-吲哚-6-基的结晶形式 } - 丙炔酸乙酰胺。

2. 发明申请

US20110086842A1 Pyrimidines as PLK inhibitors 审中-公开
标题翻译：嘧啶类作为PLK抑制剂
公开(公告)号：US20110086842A1
公开(公告)日：2011-04-14
申请号：US12972976
申请日：2010-12-20
申请人： Heinz STADTMUELLER , Harald ENGELHARDT , Martin STEEGMAIER , Anke BAUM , Ulrich GUERTLER , Andreas SCHOOP , Jens Juergen QUANT , Flavio SOLCA , Rudolf HAUPTMANN , Ulrich REISER , Stephan Karl ZAHN , Lars HERFURTH
发明人： Heinz STADTMUELLER , Harald ENGELHARDT , Martin STEEGMAIER , Anke BAUM , Ulrich GUERTLER , Andreas SCHOOP , Jens Juergen QUANT , Flavio SOLCA , Rudolf HAUPTMANN , Ulrich REISER , Stephan Karl ZAHN , Lars HERFURTH
IPC分类号： A61K31/553 , A61K31/506 , A61K31/5355 , A61P35/00 , A61P31/00 , A61P37/00
CPC分类号： C07D239/42 , C07D239/48 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D413/12 , C07D413/14 , C07D453/02 , C07D471/04 , C07D487/04 , C07D487/08 , C07D491/08 , C07D491/10
摘要： The present invention encompasses compounds of general formula (1), wherein A, W, X, Y, Z, Ra, Rb, Rc, R1 and R3 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a pharmaceutical composition having the above-mentioned properties.
摘要翻译：本发明包括通式（1）的化合物，其中A，W，X，Y，Z，Ra，Rb，Rc，R 1和R 3如权利要求1中所定义，其适用于治疗以过量或异常细胞增殖，以及其用于制备具有上述性质的药物组合物的用途。

3. 发明申请

US20090149438A1 Pyrimidines as PLK inhibitors 审中-公开
公开(公告)号：US20090149438A1
公开(公告)日：2009-06-11
申请号：US12366078
申请日：2009-02-05
申请人： Heinz STADTMUELLER , Harald ENGELHARDT , Martin STEEGMAIER , Anke BAUM , Ulrich GUERTLER , Andreas SCHOOP , Jens Juergen QUANT , Flavio SOLCA , Rudolf HAUPTMANN , Ulrich REISER , Stephan Karl ZAHN , Lars HERFURTH
发明人： Heinz STADTMUELLER , Harald ENGELHARDT , Martin STEEGMAIER , Anke BAUM , Ulrich GUERTLER , Andreas SCHOOP , Jens Juergen QUANT , Flavio SOLCA , Rudolf HAUPTMANN , Ulrich REISER , Stephan Karl ZAHN , Lars HERFURTH
IPC分类号： A61K31/5377 , C07D413/14 , C07D403/12 , A61K31/506 , A61K31/551 , C07D409/14 , A61K31/553
CPC分类号： C07D239/42 , C07D239/48 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D413/12 , C07D413/14 , C07D453/02 , C07D471/04 , C07D487/04 , C07D487/08 , C07D491/08 , C07D491/10
摘要： The present invention encompasses compounds of general formula (1), wherein A, W, X, Y, Z, Ra, Rb, Rc, R1 and R3 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a pharmaceutical composition having the above-mentioned properties.

4. 发明申请

US20090163465A1 Pyrimidines as PLK inhibitors 审中-公开
公开(公告)号：US20090163465A1
公开(公告)日：2009-06-25
申请号：US12366075
申请日：2009-02-05
申请人： Heinz STADTMUELLER , Harald ENGELHARDT , Martin STEEGMAIER , Anke BAUM , Ulrich GUERTLER , Andreas SCHOOP , Jens Juergen QUANT , Flavio SOLCA , Rudolf HAUPTMANN , Ulrich REISER , Stephan Karl ZAHN , Lars HERFURTH
发明人： Heinz STADTMUELLER , Harald ENGELHARDT , Martin STEEGMAIER , Anke BAUM , Ulrich GUERTLER , Andreas SCHOOP , Jens Juergen QUANT , Flavio SOLCA , Rudolf HAUPTMANN , Ulrich REISER , Stephan Karl ZAHN , Lars HERFURTH
IPC分类号： A61K31/506 , A61K31/55 , A61K31/553 , A61K31/551 , A61P35/00
CPC分类号： C07D239/42 , C07D239/48 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D413/12 , C07D413/14 , C07D453/02 , C07D471/04 , C07D487/04 , C07D487/08 , C07D491/08 , C07D491/10
摘要： The present invention encompasses compounds of general formula (1), wherein A, W, X, Y, Z, Ra, Rb, Rc, R1 and R3 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a pharmaceutical composition having the above-mentioned properties.

5. 发明申请

US20110046168A1 METHODS OF TREATING DISEASES USING QUINAZOLINE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 审中-公开
标题翻译：使用喹唑啉衍生物和含有它们的药物组合物治疗疾病的方法
公开(公告)号：US20110046168A1
公开(公告)日：2011-02-24
申请号：US12914003
申请日：2010-10-28
申请人： Frank HIMMELSBACH , Elke LANGKOPF , Stefan BLECH , Birgit JUNG , Anke BAUM , Flavio SOLCA
发明人： Frank HIMMELSBACH , Elke LANGKOPF , Stefan BLECH , Birgit JUNG , Anke BAUM , Flavio SOLCA
IPC分类号： A61K31/517 , A61P35/00 , A61P1/00 , A61P11/00 , A61P17/06
CPC分类号： C07D405/12 , C07D239/94
摘要： A compound of general formula I wherein: Ra is a benzyl, 1-phenylethyl, or 3-chloro-4-fluorophenyl group; Rb is a dimethylamino, N-methyl-N-ethylamino, diethylamino, N-methyl-N-isopropylamino, N-methyl-N-cyclopropylamino, N-methyl-N-(2-methoxyethyl)amino, N-ethyl-N-(2-methoxyethyl)amino, bis(2-methoxyethyl)amino, morpholino, N-methyl-N-(tetrahydrofuran-3-yl)amino, N-methyl-N-(tetrahydrofuran-2-ylmethyl)amino, N-methyl-N-(tetrahydrofuran-3-ylmethyl)amino, N-methyl-N-(tetrahydropyran-4-yl)amino, or N-methyl-N-(tetrahydropyran-4-ylmethyl)amino group; and Rc is a cyclopropylmethoxy, cyclobutyloxy, cyclopentyloxy, tetrahydrofuran-3-yloxy, tetrahydrofuran-2-ylmethoxy, tetrahydrofuran-3-ylmethoxy, tetrahydropyran-4-yloxy, or tetrahydropyran-4-ylmethoxy group, or a tautomer, stereoisomer, or salt thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases which have valuable pharmacological properties, in particular an inhibitory effect on signal transduction mediated by tyrosine kinases, their use in the treatment of diseases, especially tumoral diseases and diseases of the lungs and airways, and the preparation thereof.
摘要翻译：通式I的化合物，其中：R a是苄基，1-苯乙基或3-氯-4-氟苯基; Rb是二甲基氨基，N-甲基-N-乙基氨基，二乙基氨基，N-甲基-N-异丙基氨基，N-甲基-N-环丙基氨基，N-甲基-N-（2-甲氧基乙基）氨基，N-乙基-N- （2-甲氧基乙基）氨基，双（2-甲氧基乙基）氨基，吗啉代，N-甲基-N-（四氢呋喃-3-基）氨基，N-甲基-N-（四氢呋喃-2-基甲基）氨基，N-甲基 -N-（四氢呋喃-3-基甲基）氨基，N-甲基-N-（四氢吡喃-4-基）氨基或N-甲基-N-（四氢吡喃-4-基甲基）氨基; Rc为环丙基甲氧基，环丁氧基，环戊氧基，四氢呋喃-3-基氧基，四氢呋喃-2-基甲氧基，四氢呋喃-3-基甲氧基，四氢吡喃-4-基氧基或四氢吡喃-4-基甲氧基，或互变异构体，立体异构体或盐特别是其具有有价值的药理学特性的无机或有机酸或碱的生理上可接受的盐，特别是对由酪氨酸激酶介导的信号转导的抑制作用，它们在治疗疾病尤其是肿瘤疾病和肺疾病中的用途和气道及其制备。

6. 发明申请

US20090238828A1 Combinations for the Treatment of Diseases involving Cell Proliferation 有权
标题翻译：用于治疗涉及细胞增殖的疾病的组合
公开(公告)号：US20090238828A1
公开(公告)日：2009-09-24
申请号：US12437280
申请日：2009-05-07
申请人： Gerd MUNZERT , Martin STEEGMAIER , Anke BAUM
发明人： Gerd MUNZERT , Martin STEEGMAIER , Anke BAUM
IPC分类号： A61K39/395 , A61K31/519 , A61K31/5377 , A61K31/55
CPC分类号： A61K31/4985 , A61K31/435 , A61K31/4409 , A61K31/519
摘要： Disclosed are pharmaceutical compositions for the treatment of diseases which involve cell proliferation. Also disclosed are methods for the treatment of said diseases, comprising co-administration of a compound 1 of Formula (I) wherein the groups L, R1, R2, R3, R4 and R5 have the meanings given herein and of an effective amount of an active compound 2 and/or co-treatment with radiation therapy, in a ratio which provides an additive and synergistic effect, and to the combined use of a compound 1 of Formula (I) and of an effective amount of an active compound 2 and/or radiotherapy for the manufacture of corresponding pharmaceutical combination preparations.
摘要翻译：公开了用于治疗涉及细胞增殖的疾病的药物组合物。还公开了治疗所述疾病的方法，包括共同给予式（I）的化合物1，其中基团L，R 1，R 2，R 3，R 4和R 5具有本文给出的含义和有效量的活性化合物2和/或以放射疗法共同治疗，以提供添加剂和协同效应的比例，以及组合使用式（I）化合物1和有效量的活性化合物2和/ 或放射治疗用于制造相应的药物组合制剂。

7. 发明申请

US20140093499A1 PHARMACEUTICAL COMBINATIONS COMPRISING DUAL ANGIOPOIETIN-2 / DLL4 BINDERS AND ANTI-VEGF AGENTS 审中-公开
标题翻译：包含双重神经氨酸蛋白酶-2 / DLL4结合蛋白和抗VEGF代谢物的药物组合
公开(公告)号：US20140093499A1
公开(公告)日：2014-04-03
申请号：US14037463
申请日：2013-09-26
申请人： Andreas GSCHWIND , Anke BAUM
发明人： Andreas GSCHWIND , Anke BAUM
IPC分类号： A61K39/395 , A61K38/17 , A61K31/496
CPC分类号： A61K39/3955 , A61K31/496 , A61K38/1761 , A61K2039/505 , A61K2039/507 , A61K2039/545 , C07K16/22 , C07K2317/31 , A61K2300/00
摘要： The present invention relates to pharmaceutical combinations comprising dual Angiopoietin-2/Dll4 binders and anti-VEGF agents for use in treating diseases like cancer and ocular diseases.
摘要翻译：本发明涉及包含双重促血管生成素-2 / Dll4结合剂和用于治疗诸如癌症和眼部疾病之类的疾病的抗VEGF剂的药物组合。

8. 发明申请

US20120329778A1 BICYCLIC HETEROCYCLES, PHARMACEUTICAL COMPOSITIONS CONTAINING THESE COMPOUNDS, THEIR USE AND PROCESSES FOR PREPARING THEM 有权
标题翻译：双相异构体，含有这些化合物的药物组合物，其制备方法及其制备方法
公开(公告)号：US20120329778A1
公开(公告)日：2012-12-27
申请号：US13603476
申请日：2012-09-05
申请人： Frank HIMMELSBACH , Elke LANGKOPF , Thomas METZ , Flavio SOLCA , Birgit JUNG , Anke BAUM
发明人： Frank HIMMELSBACH , Elke LANGKOPF , Thomas METZ , Flavio SOLCA , Birgit JUNG , Anke BAUM
IPC分类号： A61K31/517 , C07D403/12 , C07D413/12 , C07D417/12 , C07D239/94 , C07D405/12 , C07D405/14 , A61K31/551 , A61K31/5377 , A61K31/541 , A61P35/00 , A61P11/00 , A61P1/00 , A61P1/16 , C07D401/12
CPC分类号： C07D405/12 , C07D215/42 , C07D215/54 , C07D239/94 , C07D401/12
摘要： The present invention relates to bicyclic heterocycles of general formula wherein Ra to Rc, A to E and X are defined as in claim 1, the tautomers, stereoisomers and salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases which have valuable pharmacological properties, in particular an inhibitory effect on signal transduction mediated by tyrosine kinases, their use in the treatment of diseases, especially tumoral diseases and diseases of the lungs and airways, and the preparation thereof.
摘要翻译：本发明涉及通式的双环杂环，其中R a至R c，A至E和X如权利要求1中所定义，互变异构体，立体异构体和盐，特别是其与无机或有机酸或碱的生理上可接受的盐，其具有特别是对由酪氨酸激酶介导的信号转导的抑制作用，它们在治疗疾病尤其是肿瘤疾病和肺和气道疾病中的应用及其制备。

9. 发明申请

US20130309225A1 COMBINATION OF CD37 ANTIBODIES WITH ICE 有权
标题翻译： CD37抗体与冰的组合
公开(公告)号：US20130309225A1
公开(公告)日：2013-11-21
申请号：US13894743
申请日：2013-05-15
申请人： Karl-Heinz HEIDER , Anke BAUM , Charlotte Astrid RUSSELL
发明人： Karl-Heinz HEIDER , Anke BAUM , Charlotte Astrid RUSSELL
IPC分类号： A61K39/395 , A61K31/555 , A61K31/7048 , A61K31/661
CPC分类号： A61K39/3955 , A61K31/555 , A61K31/661 , A61K31/675 , A61K31/7048 , A61K39/39558 , A61K2039/505 , A61K2039/545 , C07K16/2896 , C07K2317/24 , C07K2317/56 , C07K2317/565 , A61K2300/00
摘要： The present invention relates to immunotherapies that are based on depletion of CD37-positive cells such as B-cells. The present invention provides methods for reduction of CD37-positive cells such as B-cells in an individual/patient using a combination of CD37 antibody/antibodies and ICE. The combination of CD37 antibodies and ICE is shown to have improved anti-tumor efficacy compared to single agent treatment. The application further provides materials and methods for treatment of diseases involving aberrant B-cell activity.
摘要翻译：本发明涉及基于CD37阳性细胞例如B细胞消耗的免疫疗法。本发明提供使用CD37抗体/抗体和ICE的组合在个体/患者中减少CD37阳性细胞例如B细胞的方法。与单剂治疗相比，CD37抗体和ICE的组合显示出具有改善的抗肿瘤功效。该应用进一步提供了用于治疗涉及异常B细胞活性的疾病的材料和方法。

10. 发明申请

US20120107312A1 Combinations for the Treatment of Diseases involving Cell Proliferation 有权
标题翻译：用于治疗涉及细胞增殖的疾病的组合
公开(公告)号：US20120107312A1
公开(公告)日：2012-05-03
申请号：US13342507
申请日：2012-01-03
申请人： Gerd MUNZERT , Martin STEEGMAIER , Anke BAUM
发明人： Gerd MUNZERT , Martin STEEGMAIER , Anke BAUM
IPC分类号： A61K31/519 , A61K31/55 , A61P35/00 , A61K33/24 , A61K39/395 , A61K31/5377 , A61K31/7068
CPC分类号： A61K31/4985 , A61K31/435 , A61K31/4409 , A61K31/519
摘要： Disclosed are pharmaceutical compositions for the treatment of diseases which involve cell proliferation. Also disclosed are methods for the treatment of said diseases, comprising co-administration of a compound 1 of Formula (I) wherein the groups L, R1, R2, R3, R4 and R5 have the meanings given herein and of an effective amount of an active compound 2 and/or co-treatment with radiation therapy, in a ratio which provides an additive and synergistic effect, and to the combined use of a compound 1 of Formula (I) and of an effective amount of an active compound 2 and/or radiotherapy for the manufacture of corresponding pharmaceutical combination preparations.
摘要翻译：公开了用于治疗涉及细胞增殖的疾病的药物组合物。还公开了治疗所述疾病的方法，包括共同给予式（I）的化合物1，其中基团L，R 1，R 2，R 3，R 4和R 5具有本文给出的含义和有效量的活性化合物2和/或以放射疗法共同治疗，以提供添加剂和协同效应的比例，以及组合使用式（I）化合物1和有效量的活性化合物2和/ 或放射治疗用于制造相应的药物组合制剂。

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