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1. 发明授权

US08722694B2 Bicyclic heterocycles, pharmaceutical compositions containing these compounds, their use and processes for preparing them 有权
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：US08722694B2
公开(公告)日：2014-05-13
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
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。

2. 再颁专利

USRE43431E1 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：USRE43431E1
公开(公告)日：2012-05-29
申请号：US12542929
申请日：2009-08-18
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
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。

3. 发明申请

US20090036676A1 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：US20090036676A1
公开(公告)日：2009-02-05
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： C07D413/14 , C07D239/72 , C07D401/02 , C07D413/02
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. 发明申请

US20060270672A1 Bicyclic heterocyclic compounds, pharmaceutical compositions containing these compounds, their use and process for preparing them 审中-公开
公开(公告)号：US20060270672A1
公开(公告)日：2006-11-30
申请号：US11497727
申请日：2006-08-02
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 , C07D413/14 , C07D403/02
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.

5. 发明授权

US07019012B2 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：US07019012B2
公开(公告)日：2006-03-28
申请号：US10023099
申请日：2001-12-17
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： A61K31/5377 , A61K31/517 , C07D239/72 , C07D413/02
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 a是苄基，1-苯乙基或3-氯-4-氟苯基; R b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 - 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）氨基组; 环烷基甲氧基，环丁氧基，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，或其互变异构体，立体异构体或其盐，特别是其具有有价值的药理学性质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，它们在治疗疾病中的用途，特别是肺和气道的肿瘤疾病和疾病及其制备。

6. 发明申请

US20050182043A1 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：US20050182043A1
公开(公告)日：2005-08-18
申请号：US11083247
申请日：2005-03-17
申请人： Frank Himmelsbach , Birgit Jung , Flavio Solca
发明人： Frank Himmelsbach , Birgit Jung , Flavio Solca
IPC分类号： C07D239/94 , C07D401/12 , C07D403/12 , C07D405/12 , C07D405/14 , C07D413/12 , C07D491/08 , A61K31/553 , A61K31/4709 , A61K31/496 , A61K31/517 , A61K31/5377 , A61K31/55
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. 发明授权

US06656946B2 Aminoquinazolines which inhibit signal transduction mediated by tyrosine kinases 有权
标题翻译：抑制由酪氨酸激酶介导的信号转导的氨基喹唑啉
公开(公告)号：US06656946B2
公开(公告)日：2003-12-02
申请号：US09934772
申请日：2001-08-22
申请人： Frank Himmelsbach , Elke Langkopf , Birgit Jung , Stefan Blech , Flavio Solca
发明人： Frank Himmelsbach , Elke Langkopf , Birgit Jung , Stefan Blech , Flavio Solca
IPC分类号： A61K31517
CPC分类号： C07D405/12 , C07D239/94 , C07D413/12 , C07D413/14
摘要： Compounds of the formula having an inhibitory effect on signal transduction mediated by tyrosine kinases and 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：该化合物对由酪氨酸激酶介导的信号转导具有抑制作用及其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。

8. 发明授权

US06403580B1 Quinazolines, pharmaceutical compositions containing these compounds, their use and processes for preparing them 有权
标题翻译：喹唑啉，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：US06403580B1
公开(公告)日：2002-06-11
申请号：US09935498
申请日：2001-08-23
申请人： Frank Himmelsbach , Elke Langkopf , Birgit Jung , Stefan Blech , Flavio Solca
发明人： Frank Himmelsbach , Elke Langkopf , Birgit Jung , Stefan Blech , Flavio Solca
IPC分类号： A61K31517
CPC分类号： C07D405/12 , A61K31/505 , C07D239/94 , C07D413/12
摘要： Quinazolines of the formula having an inhibitory effect on signal transduction mediated by tyrosine kinases, the use thereof for treating diseases, particularly tumoral diseases, diseases of the lungs and respiratory tract, and the preparation thereof.
摘要翻译：该公式的喹唑啉对由酪氨酸激酶介导的信号转导具有抑制作用，其用于治疗疾病，特别是肿瘤性疾病，肺和呼吸道疾病的用途及其制备。

9. 发明授权

US07119084B2 Bicyclic heterocyclic compounds, pharmaceutical compositions containing these compounds, their use and process for preparing them 有权
公开(公告)号：US07119084B2
公开(公告)日：2006-10-10
申请号：US11083247
申请日：2005-03-17
申请人： Frank Himmelsbach , Birgit Jung , Flavio Solca
发明人： Frank Himmelsbach , Birgit Jung , Flavio Solca
IPC分类号： A01N43/00 , A61K31/55
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.

10. 发明授权

US06972288B1 4-amino-quinazoline and quinoline derivatives having an inhibitory effect on signal transduction mediated by tyrosine kinases 有权
标题翻译：对酪氨酸激酶介导的信号转导具有抑制作用的4-氨基 - 喹唑啉和喹啉衍生物
公开(公告)号：US06972288B1
公开(公告)日：2005-12-06
申请号：US09914323
申请日：2000-02-24
申请人： Frank Himmelsbach , Elke Langkopf , Birgit Jung , Thomas Metz , Flavio Solca , Stefan Blech
发明人： Frank Himmelsbach , Elke Langkopf , Birgit Jung , Thomas Metz , Flavio Solca , Stefan Blech
IPC分类号： A61K31/47 , A61K31/4706 , A61K31/4709 , A61K31/496 , A61K31/517 , A61P35/00 , C07D215/42 , C07D215/54 , C07D239/94 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D413/12
CPC分类号： C07D401/12 , A61K31/47 , A61K31/4706 , A61K31/4709 , A61K31/496 , A61K31/517 , C07D215/54 , C07D239/94 , C07D403/12 , C07D405/12 , C07D413/12
摘要： The present invention relates to bicyclic heterocycles of general formula wherein Ra to Rd, A to G and X are defined as in claim 1, the tautomers, the steroisomers and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases which have valuable pharmacological properties, particularly an inhibiting effect on signal transduction mediated by tyrosine kinases, their use for treating diseases, particularly tumoral diseases, 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至R d，A至G和X如权利要求1所定义，互变异构体，立体异构体和其盐，特别是其具有有价值的药理学性质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，其用于治疗疾病，特别是肿瘤疾病，肺和呼吸道疾病道及其制备。

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