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1. 发明授权

US08586608B2 Quinazoline derivatives and pharmaceutical compositions containing them 有权
标题翻译：喹唑啉衍生物和含有它们的药物组合物
公开(公告)号：US08586608B2
公开(公告)日：2013-11-19
申请号：US12563340
申请日：2009-09-21
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： A61K31/47 , A01N43/42
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-(tetra-hydrofuran-3-yl)amino, N-methyl-N-(tetrahydrofuran-2-ylmethyl)amino, N-methyl-N-(tetra-hydrofuran-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。

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

US20110077246A1 BICYCLIC HETEROCYCLIC COMPOUNDS PHARMACEUTICAL COMPOSITIONS CONTAINING THESE COMPOUNDS, THEIR USE AND PROCESS FOR PREPARING THE SAME 有权
标题翻译：双环杂环化合物包含这些化合物的药物组合物，其使用及其制备方法
公开(公告)号：US20110077246A1
公开(公告)日：2011-03-31
申请号：US12961109
申请日：2010-12-06
申请人： Frank HIMMELSBACH , Birgit JUNG , Flavio SOLCA
发明人： Frank HIMMELSBACH , Birgit JUNG , Flavio SOLCA
IPC分类号： A61K31/5377 , A61K31/517 , A61P29/00 , A61P11/06 , A61P11/08 , A61P11/14 , A61P11/00
CPC分类号： C07D401/12 , C07D239/94 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D413/12 , C07D413/14 , C07D491/08
摘要： The present invention relates methods for treating disease conditions selected from the list consisting of benign or malignant tumors, diseases of the airways and lungs, diseases of the gastrointestinal tract, the bile duct and the gall bladder by administration to a patient in need thereof of a therapeutically effective amount of a bicyclic heterocyclic groups of general formula wherein said substituents are as defined herein.
摘要翻译：本发明涉及用于治疗选自良性或恶性肿瘤，气道和肺疾病，胃肠道疾病，胆管和胆囊中的疾病的方法，通过给予有需要的患者治疗有效量的通式的双环杂环基团，其中所述取代基如本文所定义。

4. 发明授权

US07910731B2 Bicyclic heterocyclic compounds, pharmaceutical compositions containing these compounds, their use and process for preparing them 有权
标题翻译：双环杂环化合物，含有这些化合物的药物组合物，它们的用途和制备方法
公开(公告)号：US07910731B2
公开(公告)日：2011-03-22
申请号：US12072510
申请日：2008-02-26
申请人： Frank Himmelsbach , Birgit Jung , Flavio Solca
发明人： Frank Himmelsbach , Birgit Jung , Flavio Solca
IPC分类号： C07D413/00
CPC分类号： C07D401/12 , C07D239/94 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D413/12 , C07D413/14 , C07D491/08
摘要： The present invention relates methods for treating disease conditions selected from the list consisting of benign or malignant tumors, diseases of the airways and lungs, diseases of the gastrointestinal tract, the bile duct and the gall bladder by administration to a patient in need thereof of a therapeutically effective amount of a bicyclic heterocyclic groups of general formula wherein said substituents are as defined herein.
摘要翻译：本发明涉及用于治疗选自良性或恶性肿瘤，气道和肺疾病，胃肠道疾病，胆管和胆囊中的疾病的方法，通过给予有需要的患者治疗有效量的通式的双环杂环基团，其中所述取代基如本文所定义。

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. 发明授权

US07863281B2 Bicyclic heterocycles, pharmaceutical compositions containing these compounds, their use and processes for the preparation thereof 有权
标题翻译：双环杂环，含有这些化合物的药物组合物，其用途及其制备方法
公开(公告)号：US07863281B2
公开(公告)日：2011-01-04
申请号：US11960322
申请日：2007-12-19
申请人： Frank Himmelsbach , Birgit Jung , Flavio Solca
发明人： Frank Himmelsbach , Birgit Jung , Flavio Solca
IPC分类号： A61K31/517 , C07D239/70
CPC分类号： C07D451/02 , C07D405/14 , C07D471/08 , C07D487/08 , C07D491/08 , C07D493/08 , C07D498/08
摘要： The present invention relates to bicyclic heterocycles of general formula wherein Ra, Rb, Rc, A, B, C, D, E and X are defined as in claim 1, the tautomers, the stereoisomers, the mixtures and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids which have valuable pharmacological properties, particularly an inhibitory effect on signal transduction mediated by tyrosine kinases, the use thereof for treating diseases, particularly tumoral diseases, as well as benign prostatic hyperplasia (BPH), diseases of the lungs and respiratory tract, and the preparation thereof.
摘要翻译：本发明涉及通式的双环杂环，其中Ra，Rb，Rc，A，B，C，D，E和X如权利要求1所定义，互变异构体，立体异构体，其混合物和盐，特别是其生理学上可接受的盐与具有有价值的药理学特性的无机或有机酸特别是对由酪氨酸激酶介导的信号转导的抑制作用，其用于治疗疾病，特别是肿瘤性疾病以及良性前列腺增生（BPH）的使用，肺和呼吸道及其制备。

7. 发明授权

US07569561B2 2,4-diaminopyrimidines useful for treating cell proliferation diseases 有权
标题翻译：可用于治疗细胞增殖疾病的2,4-二氨基嘧啶
公开(公告)号：US07569561B2
公开(公告)日：2009-08-04
申请号：US11675936
申请日：2007-02-16
申请人： Heinz Stadtmueller , Anke Baum , Guido Boehmelt , Harald Engelhardt , Jens Juergen Quant , Flavio Solca , Martin Steegmaier , Stephan Karl Zahn
发明人： Heinz Stadtmueller , Anke Baum , Guido Boehmelt , Harald Engelhardt , Jens Juergen Quant , Flavio Solca , Martin Steegmaier , Stephan Karl Zahn
IPC分类号： C07D403/12 , C07D413/12 , C07D498/04 , C07D487/04 , A61K31/551 , A61K31/553 , A61P29/00 , A61P35/00 , A61P37/00
CPC分类号： C07D498/04 , C07D403/12 , C07D413/12 , C07D487/04
摘要： The present invention encompasses compounds of general formula (1) wherein R1 to R6, X and Y are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or anomalous cell proliferation, as well as the use thereof for preparing a pharmaceutical composition with the above-mentioned properties.
摘要翻译：本发明包括通式（1）的化合物，其中R 1至R 6，X和Y如权利要求1中所定义，其适用于治疗以过度或异常细胞增殖为特征的疾病，以及其用于制备具有上述性质的药物组合物。

8. 发明申请

US20080319193A1 New dihydropteridione derivatives, process for their manufacture and their use as medicament 有权
公开(公告)号：US20080319193A1
公开(公告)日：2008-12-25
申请号：US12192448
申请日：2008-08-15
申请人： Matthias GRAUERT , Matthias HOFFMANN , Martin STEEGMAIER , Flavio SOLCA , Jens Juergen QUANT
发明人： Matthias GRAUERT , Matthias HOFFMANN , Martin STEEGMAIER , Flavio SOLCA , Jens Juergen QUANT
IPC分类号： C07D475/00
CPC分类号： C07D295/155 , C07D487/04 , Y02P20/55
摘要： Disclosed are new dihydropteridinones of the formula (I) wherein the groups L, R1, R2, R3, R4 and R5 have the meanings provided herein, the isomers thereof, processes for preparing these dihydropteridinones and their use as pharmaceutical compositions.

9. 发明申请

US20080103161A1 BICYCLIC HETEROCYCLES, PHARMACEUTICAL COMPOSITIONS CONTAINING THESE COMPOUNDS, THEIR USE AND PROCESSES FOR THE PREPARATION THEREOF 有权
标题翻译：双相异构体，包含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：US20080103161A1
公开(公告)日：2008-05-01
申请号：US11960322
申请日：2007-12-19
申请人： Frank Himmelsbach , Birgit Jung , Flavio Solca
发明人： Frank Himmelsbach , Birgit Jung , Flavio Solca
IPC分类号： A61K31/517 , A61P1/16 , C07D401/02
CPC分类号： C07D451/02 , C07D405/14 , C07D471/08 , C07D487/08 , C07D491/08 , C07D493/08 , C07D498/08
摘要： The present invention relates to bicyclic heterocycles of general formula wherein Ra, Rb, Rc, A, B, C, D, E and X are defined as in claim 1, the tautomers, the stereoisomers, the mixtures and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids which have valuable pharmacological properties, particularly an inhibitory effect on signal transduction mediated by tyrosine kinases, the use thereof for treating diseases, particularly tumoral diseases, as well as benign prostatic hyperplasia (BPH), diseases of the lungs and respiratory tract, and the preparation thereof.
摘要翻译：本发明涉及以下通式的双环杂环：其中R a，R b，R b，R c，A，B，C，D，E 和X如权利要求1所定义，其互变异构体，立体异构体，其混合物及其盐，特别是其与具有有价值药理学性质的无机或有机酸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，其用于治疗疾病，特别是肿瘤疾病以及良性前列腺增生（BPH），肺和呼吸道疾病及其制备的用途。

10. 发明申请

US20070185081A1 Bicyclic heterocylces, pharmaceutical compositions containing these compounds, their use and processes for preparing them 审中-公开
标题翻译：双环杂环，含有这些化合物的药物组合物，它们的用途和制备方法
公开(公告)号：US20070185081A1
公开(公告)日：2007-08-09
申请号：US11736909
申请日：2007-04-18
申请人： Frank HIMMELSBACH , Flavio Solca
发明人： Frank HIMMELSBACH , Flavio Solca
IPC分类号： A61K31/554 , C07D267/02
CPC分类号： C07D413/14 , C07D413/12
摘要： The present invention relates to bicyclic heterocycles of general formula wherein Ra, Rb, Rc, Rd, Re and X are defined as in claim 1, the tautomers, the stereoisomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids, which have valuable pharmacological properties, particularly an inhibitory effect on signal transduction mediated by tyrosine kinases, the use thereof for treating diseases, particularly tumoral diseases and benign prostatic hyperplasia (BPH), diseases of the lungs and respiratory tract, and the preparation thereof.
摘要翻译：本发明涉及通式的双环杂环，其中R a，R b，R c，R d，R d， R e和X如权利要求1中所定义，互变异构体，立体异构体，其混合物及其盐，特别是其与无机或有机酸的生理上可接受的盐，其具有有价值的药理学性质特别是对由酪氨酸激酶介导的信号转导的抑制作用，其用于治疗疾病，特别是肿瘤疾病和良性前列腺增生（BPH），肺和呼吸道疾病及其制备的用途。

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