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1. 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。

2. 发明申请

US20100010023A1 QUINAZOLINE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 有权
标题翻译：喹诺酮衍生物和含有它们的药物组合物
公开(公告)号：US20100010023A1
公开(公告)日：2010-01-14
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： A61K31/517 , C07D239/94 , C07D413/02 , C07D405/02 , A61P35/00
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。

3. 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。

4. 发明申请

US20100069414A1 BICYCLIC HETEROCYCLES, PHARMACEUTICAL COMPOSITIONS CONTAINING THESE COMPOUNDS, THEIR USE AND PROCESSES FOR PREPARING THEM 审中-公开
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：US20100069414A1
公开(公告)日：2010-03-18
申请号：US12624875
申请日：2009-11-24
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 , C07D401/02 , C07D239/72 , A61P35/00 , A61P11/00 , A61P1/00
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。

5. 发明申请

US20090203683A1 BICYCLIC HETEROCYCLES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM, THEIR USE, AND PROCESSES FOR PREPARING THEM 审中-公开
标题翻译：双相异构体，含有它们的药物组合物，其使用和制备方法
公开(公告)号：US20090203683A1
公开(公告)日：2009-08-13
申请号：US12423522
申请日：2009-04-14
申请人： Frank HIMMELSBACH , Elke LANGKOPF , Stefan BLECH , Birgit JUNG , Thomas METZ , Flavio SOLCA
发明人： Frank HIMMELSBACH , Elke LANGKOPF , Stefan BLECH , Birgit JUNG , Thomas METZ , Flavio SOLCA
IPC分类号： A61K31/517 , C07D403/12 , C07D413/12 , A61K31/5377 , A61P35/00
CPC分类号： C07D221/00 , C07D401/12 , C07D403/12
摘要： A compound of formula (I) wherein Ra, Rb, Rc, A, B, C, D, and X are as defined herein, or a tautomer, stereoisomer, or salt thereof, particularly a physiologically acceptable salt thereof. In addition, pharmaceutical compositions comprising an effective amount of a compound of formula (I), methods for the treatment or prophylaxis of benign or malignant tumors, diseases of the airways and lungs, polyps, diseases of the gastrointestinal tract, bile duct, gall bladder, kidneys, and skin, and methods for making compounds of formula (I) are disclosed.
摘要翻译：其中Ra，Rb，Rc，A，B，C，D和X如本文所定义的式（I）化合物或其互变异构体，立体异构体或其盐，特别是其生理学上可接受的盐。此外，包含有效量的式（I）化合物，治疗或预防良性或恶性肿瘤的方法，气道和肺部疾病，息肉，胃肠道疾病，胆管，胆囊的药物组合物，肾脏和皮肤，以及制备式（I）化合物的方法。

6. 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。

7. 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。

8. 发明申请

US20140199298A1 COMBINATION TREATMENT OF CANCER COMPRISING EGFR/HER2 INHIBITORS 审中-公开
标题翻译：包含EGFR / HER2抑制剂的癌症的组合治疗
公开(公告)号：US20140199298A1
公开(公告)日：2014-07-17
申请号：US14160700
申请日：2014-01-22
申请人： Flavio SOLCA , Andree AMELSBERG , Gerd STEHLE , Jacobus C.A. VAN MEEL , Anke BAUM
发明人： Flavio SOLCA , Andree AMELSBERG , Gerd STEHLE , Jacobus C.A. VAN MEEL , Anke BAUM
IPC分类号： C07D405/12 , A61K31/517 , A61K39/395
CPC分类号： C07D405/12 , A61K31/00 , A61K31/337 , A61K31/517 , A61K39/39558 , A61K45/06 , A61K2300/00
摘要： The invention relates to a therapy of cancer comprising co-administration to a person in need of such treatment and/or co-treatment of a person in need of such treatment with effective amounts of: (1) a compound 1 of formula (I) wherein the groups Ra to Rd have the meanings given in the claims and specification; and (2) at least a further chemotherapeutic agent 2; optionally in combination with radiotherapy, radio-immunotherapy and/or tumour resection by surgery, furthermore, the invention relates to corresponding medicaments and the preparation thereof.
摘要翻译：本发明涉及癌症治疗，其包括共同给予需要这种治疗和/或共同治疗需要这种治疗的人的人，其有效量为：（1）式（I）化合物1，其中基团Ra至Rd具有权利要求和说明书中给出的含义; 和（2）至少另外一种化学治疗剂2; 任选地与放射治疗，放射免疫治疗和/或手术的肿瘤切除术组合，此外，本发明涉及相应的药物及其制备。

9. 发明申请

US20110136826A1 COMBINATIONS FOR THE TREATMENT OF DISEASES INVOLVING CELL PROLIFERATION, MIGRATION OR APOPTOSIS OF MYELOMA CELLS, OR ANGIOGENESIS 审中-公开
标题翻译：治疗涉及细胞增殖，移植或吞噬MYELOMA细胞或血管生成的疾病的组合
公开(公告)号：US20110136826A1
公开(公告)日：2011-06-09
申请号：US12912098
申请日：2010-11-15
申请人： Frank HILBERG , Flavio SOLCA , Anke BAUM , Jacobus C.A. van MEEL
发明人： Frank HILBERG , Flavio SOLCA , Anke BAUM , Jacobus C.A. van MEEL
IPC分类号： A61K31/517 , A61P35/00
CPC分类号： A61K31/496 , A61K31/404 , A61K31/517 , A61K31/553 , A61K31/56 , A61K45/06 , A61K2300/00
摘要： The present invention relates to a pharmaceutical combination for the treatment of diseases which involves cell proliferation, migration or apoptosis of myeloma cells, or angiogenesis. The invention also relates to a method for the treatment of said diseases, comprising co-administration of effective amounts of specific active compounds and/or co-treatment with radiation therapy, in a ratio which provides an additive and synergistic effect, and to the combined use of these specific compounds and/or radiotherapy for the manufacture of corresponding pharmaceutical combination preparations.
摘要翻译：本发明涉及用于治疗涉及骨髓瘤细胞的细胞增殖，迁移或凋亡或血管发生的疾病的药物组合。本发明还涉及一种治疗所述疾病的方法，包括以提供添加剂和协同效应的比例共同给予有效量的特定活性化合物和/或与放射治疗共同给药，以及组合使用这些特定化合物和/或放射治疗来制造相应的药物组合制剂。

10. 发明申请

US20100324288A1 Dihydropteridinone Compounds 有权
标题翻译：二氢蝶啶酮化合物
公开(公告)号：US20100324288A1
公开(公告)日：2010-12-23
申请号：US12873687
申请日：2010-09-01
申请人： Matthias HOFFMANN , Matthias GRAUERT , Martin STEEGMAIER , Gisela SCHNAPP , Anke BAUM , Jens Juergen QUANT , Flavio SOLCA , Florian COLBATZKY
发明人： Matthias HOFFMANN , Matthias GRAUERT , Martin STEEGMAIER , Gisela SCHNAPP , Anke BAUM , Jens Juergen QUANT , Flavio SOLCA , Florian COLBATZKY
IPC分类号： C07D475/00
CPC分类号： C07D295/073 , C07D475/00
摘要： Disclosed are new dihydropteridinones of general formula (I) wherein the groups L and R1-R5 have the meanings given in the claims and specification, the isomers thereof, intermediates and processes for preparing these dihydropteridinones and the use thereof as pharmaceutical compositions.
摘要翻译：公开了通式（I）的新的二氢蝶啶酮，其中基团L和R 1 -R 5具有权利要求书和说明书中给出的含义，其异构体，制备这些二氢蝶啶烷的中间体和方法及其作为药物组合物的用途。

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