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51. 发明申请

US20060100223A1 Quinazoline derivatives and pharmaceutical compositions containing them 审中-公开
公开(公告)号：US20060100223A1
公开(公告)日：2006-05-11
申请号：US11313304
申请日：2005-12-21
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 , C07D405/02 , C07D239/84
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.

52. 发明申请

US20060079541A1 3-methyl-7-butinyl-xanthines, the preparation thereof and their use as pharmaceutical compositions 有权
标题翻译： 3-甲基-7-丁烯基 - 黄嘌呤，其制备及其作为药物组合物的用途
公开(公告)号：US20060079541A1
公开(公告)日：2006-04-13
申请号：US11218056
申请日：2005-09-01
申请人： Elke Langkopf , Matthias Eckhardt , Frank Himmelsbach , Mohammad Tadayyon , Leo Thomas , Ralf Lotz
发明人： Elke Langkopf , Matthias Eckhardt , Frank Himmelsbach , Mohammad Tadayyon , Leo Thomas , Ralf Lotz
IPC分类号： A61K31/522 , C07D473/04
CPC分类号： C07D473/00
摘要： The present invention relates to new substituted xanthines of general formula wherein R1, R2 and X are defined as in the claims, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
摘要翻译：本发明涉及以下通式的新的取代黄嘌呤：其中R 1，R 2和X如权利要求中所定义，互变异构体，对映异构体，非对映异构体，其具有有价值的药理学特性的其混合物及其盐，特别是对二肽基肽酶-IV（DPP-IV）的活性的抑制作用。

53. 发明申请

US20050234108A1 8-[3-amino-piperidin-1-yl]-xanthines, their preparation and their use as pharmaceutical compositions 有权
标题翻译： 8- [3-氨基 - 哌啶-1-基] - 黄嘌呤，它们的制备及其作为药物组合物的用途
公开(公告)号：US20050234108A1
公开(公告)日：2005-10-20
申请号：US11060703
申请日：2005-02-17
申请人： Frank Himmelsbach , Elke Langkopf , Matthias Eckhardt , Mohammad Tadayyon , Leo Thomas
发明人： Frank Himmelsbach , Elke Langkopf , Matthias Eckhardt , Mohammad Tadayyon , Leo Thomas
IPC分类号： A61K31/44
CPC分类号： C07D473/04
摘要： The present invention relates to substituted xanthines of general formula wherein R is defined as in claim 1, the tautomers, the stereoisomers, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
摘要翻译：本发明涉及通式的取代黄嘌呤，其中R如权利要求1所定义，其互变异构体，立体异构体，其混合物及其盐具有有价值的药理学性质，特别是对酶二肽基肽酶的活性的抑制作用 -IV（DPP-IV）。

54. 发明申请

US20050171093A1 New piperazin-1-yl and 2-([1,4]diazepan-1-yl)-imidazo[4,5-d]-pyridazin-4-ones, the preparation thereof and their use as pharmaceutial compositions 有权
标题翻译：新的哌嗪-1-基和2 - （[1,4]二氮杂环庚烷-1-基） - 咪唑并[4,5-d] - 哒嗪-4-酮的制备及其作为药物组合物的用途
公开(公告)号：US20050171093A1
公开(公告)日：2005-08-04
申请号：US11016176
申请日：2004-12-17
申请人： Matthias Eckhardt , Norbert Hauel , Frank Himmelsbach , Iris Kauffman-Hefner , Elke Langkopf , Mohammad Tadayyon , Leo Thomas
发明人： Matthias Eckhardt , Norbert Hauel , Frank Himmelsbach , Iris Kauffman-Hefner , Elke Langkopf , Mohammad Tadayyon , Leo Thomas
IPC分类号： A61K31/503 , A61K31/5377 , A61K31/551 , C07D487/02 , C07D487/04
CPC分类号： C07D487/04
摘要： The present invention relates to substituted imidazo[4,5-d]pyridazin-4-ones of general formula wherein R1 to R3 and n are defined as in claims 1 to 8, the tautomers, enantiomers, diastereomers, mixtures thereof and the salts thereof which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
摘要翻译：本发明涉及以下通式的取代咪唑并[4,5-d]哒嗪-4-酮：其中R 1至R 3和n如权利要求1中所定义至8，其互变异构体，对映异构体，非对映异构体，其混合物及其盐具有有价值的药理学性质，特别是对二肽基肽酶-IV（DPP-IV）的活性的抑制作用。

55. 发明授权

US06740651B2 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：US06740651B2
公开(公告)日：2004-05-25
申请号：US09934631
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： C07D41312
CPC分类号： C07D413/12
摘要： Compounds of the formula having an inhibitory effect on signal transduction mediated by tyrosine kinases, and the use thereof for treating diseases, particularly tumoral diseases, diseases of the lungs and respiratory tract.
摘要翻译：对酪氨酸激酶介导的信号转导具有抑制作用的化学式及其用于治疗疾病，特别是肿瘤疾病，肺和呼吸道疾病的用途。

56. 发明授权

US08735579B2 Benzamides, production thereof, and use thereof as medicaments 有权
标题翻译：苯甲酰胺，其制备及其作为药物的用途
公开(公告)号：US08735579B2
公开(公告)日：2014-05-27
申请号：US13060761
申请日：2009-08-26
申请人： Holger Wagner , Elke Langkopf , Frank Himmelsbach , Rolf Goeggel , Birgit Jung
发明人： Holger Wagner , Elke Langkopf , Frank Himmelsbach , Rolf Goeggel , Birgit Jung
IPC分类号： C07D239/24 , C07D239/34 , C07D239/46 , C07D239/47 , A61K31/505 , A61K31/506 , A61P11/00 , A61P11/06
CPC分类号： C07D403/04 , C07D213/68 , C07D213/74 , C07D213/89 , C07D239/34 , C07D239/42 , C07D239/46 , C07D401/04 , C07D401/06 , C07D401/12
摘要： Heteroaryloxy-substituted benzoic acid amides of general formula I wherein the groups R1 to R7 as well as X and Y are defined according to claim 1, including the tautomers, the stereoisomers, the mixtures and the salts thereof. The compounds according to the invention are suitable for the treatment of respiratory complaints, particularly COPD and asthma.
摘要翻译：通式I的杂芳氧基取代的苯甲酸酰胺，其中基团R 1至R 7以及X和Y如权利要求1所定义，包括互变异构体，立体异构体，其混合物和盐。根据本发明的化合物适合于治疗呼吸道疾病，特别是COPD和哮喘。

57. 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。

58. 发明授权

US08697868B2 8-[3-amino-piperidin-1-yl]-xanthines, their preparation and their use as pharmaceutical compositions 有权
标题翻译： 8- [3-氨基 - 哌啶-1-基] - 黄嘌呤，它们的制备及其作为药物组合物的用途
公开(公告)号：US08697868B2
公开(公告)日：2014-04-15
申请号：US12360392
申请日：2009-01-27
申请人： Frank Himmelsbach , Elke Langkopf , Matthias Eckhardt , Mohammad Tadayyon , Leo Thomas
发明人： Frank Himmelsbach , Elke Langkopf , Matthias Eckhardt , Mohammad Tadayyon , Leo Thomas
IPC分类号： C07D473/00 , C07D473/02 , C07D473/04
CPC分类号： C07D473/04
摘要： Disclosed are substituted xanthines of the formula wherein R is defined as in claim 1, the tautomers, the stereoisomers, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
摘要翻译：公开了下式的取代黄嘌呤：其中R如权利要求1所定义，互变异构体，立体异构体，其混合物及其盐具有有价值的药理学性质，特别是对二肽基肽酶-IV酶活性的抑制作用 DPP-IV）。

59. 发明授权

US08664232B2 8-[3-amino-piperidin-1-yl]-xanthines, the preparation thereof and their use as pharmaceutical compositions 有权
标题翻译： 8- [3-氨基 - 哌啶-1-基] - 黄嘌呤，其制备及其作为药物组合物的用途
公开(公告)号：US08664232B2
公开(公告)日：2014-03-04
申请号：US13448495
申请日：2012-04-17
申请人： Frank Himmelsbach , Elke Langkopf , Matthias Eckhardt , Michael Mark , Roland Maier , Ralf R. H. Lotz , Mohammad Tadayyon
发明人： Frank Himmelsbach , Elke Langkopf , Matthias Eckhardt , Michael Mark , Roland Maier , Ralf R. H. Lotz , Mohammad Tadayyon
IPC分类号： A01N43/90 , C07D473/00
CPC分类号： C07D473/04 , C07D473/06 , C07D473/08 , C07D519/00
摘要： The present invention relates to substituted xanthines of general formula wherein R1 to R3 are as defined herein, the tautomers, the stereoisomers, the mixtures, the prodrugs thereof and the salts thereof which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
摘要翻译：本发明涉及通式为其中R1至R3如本文所定义的取代黄嘌呤，其互变异构体，立体异构体，混合物，其前药及其盐具有有价值的药理学性质，特别是对酶二肽肽酶-IV（DPP-IV）。

60. 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。

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