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公开(公告)号：US20120116080A1
公开(公告)日：2012-05-10
申请号：US13057871
申请日：2009-07-23
IPC分类号： C07D471/10 , C07D241/04 , C07D401/12
CPC分类号： C07D241/08 , C07D471/20
摘要： The present invention relates to a process for the stereoselective preparation of compounds of general formula (I) and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids and bases, which have valuable pharmacological properties, particularly an inhibitory effect on signal transduction mediated by tyrosine kinases, the use thereof for the treatment of diseases, particularly tumoral diseases as well as benign prostatic hyperplasia (BPH), diseases of the lungs and airways.
摘要翻译： 本发明涉及具有有价值的药理学特性，特别是对信号的抑制作用的通式（I）化合物及其盐特别是其生理上可接受的盐与无机或有机酸和碱的立体选择性制备方法。 由酪氨酸激酶介导的转导，其用于治疗疾病，特别是肿瘤疾病以及良性前列腺增生（BPH），肺和气道疾病的用途。
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公开(公告)号：US20080086003A1
公开(公告)日：2008-04-10
申请号：US11734520
申请日：2007-04-12
申请人： Uwe RIES , Guenther HUCHLER , Sonja SPROLL , Ulrike WERTHMANN , Andreas ZOPF
发明人： Uwe RIES , Guenther HUCHLER , Sonja SPROLL , Ulrike WERTHMANN , Andreas ZOPF
IPC分类号： C07D401/14 , C07D405/14 , C07D413/14
CPC分类号： C07D401/14 , C07D401/04
摘要： The present invention relates to the new crystalline compounds A of general formula I wherein A1, A2, A3, X, Y1, Y2 and Y3 are defined as in claim 1, and which are present in the form of their physiologically acceptable salts with acids, the acids being selected from the group B comprising hydrochloric acid, hydrobromic acid, sulphuric acid, phosphoric acid, benzenesulphonic acid, p-toluenesulphonic acid, maleic acid, succinic acid, fumaric acid, D-(−)-tartaric acid, L-(+)-tartaric acid, naphthalene-2-sulphonic acid and naphthalene-1,5-disulphonic acid, and the polymorphs, the corresponding solvates and hydrates thereof.
摘要翻译： 本发明涉及通式Ⅰ的新结晶化合物A，其中A 1，A 2，A 3，X，Y 0 Y 1，Y 2和Y 3如权利要求1中所定义，并且以酸的生理学上可接受的盐的形式存在，酸 选自B，包括盐酸，氢溴酸，硫酸，磷酸，苯磺酸，对甲苯磺酸，马来酸，琥珀酸，富马酸，D - （ - ） - 酒石酸，L - （+） - - 酒石酸，萘-2-磺酸和萘-1,5-二磺酸，其多晶型物，其相应的溶剂合物和水合物。
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公开(公告)号：US20080045705A1
公开(公告)日：2008-02-21
申请号：US11840397
申请日：2007-08-17
申请人： Guenther Huchler , Werner Rall , Uwe Ries
发明人： Guenther Huchler , Werner Rall , Uwe Ries
IPC分类号： C07D487/00 , C07C59/01 , C07C69/96 , C07F9/28 , C07D317/44 , C07D413/04
CPC分类号： C07D401/04 , C07C59/52 , C07C59/64 , C07C59/68 , C07C229/42 , C07D401/14
摘要： The present invention relates to a process for preparing compounds of general formula I wherein R1 and R2 are defined as in claim 1, the pharmaceutically acceptable salts and the solvates thereof, which may be prepared starting from compounds of general formula II wherein R1 is defined as in claim 1.
摘要翻译： 本发明涉及一种制备通式Ⅰ化合物的方法，其中R 1和R 2定义如权利要求1，其药学上可接受的盐和溶剂合物， 其可以从通式II的化合物开始制备，其中R 1如权利要求1中所定义。
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![9-[4-(3-CHLORO-2-FLUORO-PHENYLAMINO)-7-METHOXY-QUINAZOLINE-6-YLOXY]-1,4-DIAZA-SPIRO[5.5]UNDECANE-5-ONE DIMALEATE, USE THEREOF AS A MEDICAMENT AND METHOD FOR THE PRODUCTION THEREOF](/abs-image/US/2014/12/18/US20140371226A1/abs.jpg.150x150.jpg)
14.发明申请9-[4-(3-CHLORO-2-FLUORO-PHENYLAMINO)-7-METHOXY-QUINAZOLINE-6-YLOXY]-1,4-DIAZA-SPIRO[5.5]UNDECANE-5-ONE DIMALEATE, USE THEREOF AS A MEDICAMENT AND METHOD FOR THE PRODUCTION THEREOF 有权9- [4-（3-氯代-2-氟 - 苯基）-7-甲氧基喹唑啉-6-甲氧基] -1,4-二氮杂螺[5.5]联苯-5-酮二甲醚，其作为药物使用 及其生产方法公开(公告)号：US20140371226A1
公开(公告)日：2014-12-18
申请号：US14471147
申请日：2014-08-28
IPC分类号： C07D241/38
CPC分类号： C07D241/38 , C07D239/70 , C07D403/12
摘要： The present invention relates to a compound of formula (I), which has valuable pharmacological properties, particularly an inhibiting effect on signal transduction mediated by tyrosine kinases, processes for stereoselectively preparing these compounds, particularly pharmaceutical formulations suitable for inhalation and their use for the treatment of diseases, particularly tumoral diseases, benign prostatic hyperplasia and diseases of the lungs and airways.
摘要翻译： 本发明涉及式（I）化合物，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，立体选择性制备这些化合物的方法，特别是适用于吸入的药物制剂及其用于治疗 的疾病，特别是肿瘤疾病，良性前列腺增生和肺和气道疾病。
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公开(公告)号：US08084634B2
公开(公告)日：2011-12-27
申请号：US12710605
申请日：2010-02-23
申请人： Guenther Huchler , Werner Rall , Uwe Reis
发明人： Guenther Huchler , Werner Rall , Uwe Reis
IPC分类号： C07C69/00 , C07C69/76 , C07C229/00
CPC分类号： C07D401/04 , C07C59/52 , C07C59/64 , C07C59/68 , C07C229/42 , C07D401/14
摘要： The present invention relates to a process for preparing compounds of general formula I wherein R1 and R2 are defined as in claim 1, the pharmaceutically acceptable salts and the solvates thereof, which may be prepared starting from compounds of general formula II wherein R1 is defined as in claim 1.
摘要翻译： 本发明涉及一种制备通式Ⅰ化合物的方法，其中R 1和R 2如权利要求1所定义，其药学上可接受的盐和溶剂化物，其可以从通式II的化合物制备，其中R1定义为 在权利要求1中。
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公开(公告)号：US20110301350A1
公开(公告)日：2011-12-08
申请号：US13058658
申请日：2009-02-13
IPC分类号： C07D295/135 , C07D295/155
CPC分类号： C07D295/14
摘要： The present invention relates to a process for preparing compounds of general formula I wherein m, n, o, R1, R2 and R3 are defined as mentioned hereinafter, the enantiomers thereof and the diastereomers thereof, which are particularly suitable for preparing compounds of general formula II wherein m, o, R1, R2, R3 and R4 are defined as mentioned hereinafter. The compounds of general formula II have B1-antagonistic properties.
摘要翻译： 本发明涉及一种制备通式I化合物的方法，其中m，n，o，R 1，R 2和R 3如下文所定义，其对映体和非对映体特别适用于制备通式 其中m，o，R 1，R 2，R 3和R 4如下文所述定义。 通式II的化合物具有B1拮抗性质。
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公开(公告)号：US07638625B2
公开(公告)日：2009-12-29
申请号：US11734520
申请日：2007-04-12
申请人： Uwe Ries , Guenther Huchler , Sonja Sproll , Ulrike Werthmann , Andreas Zopf
发明人： Uwe Ries , Guenther Huchler , Sonja Sproll , Ulrike Werthmann , Andreas Zopf
IPC分类号： C07D491/04 , C07D491/14
CPC分类号： C07D401/14 , C07D401/04
摘要： The present invention relates to the new crystalline compounds A of general formula I wherein A1, A2, A3, X, Y1, Y2 and Y3 are defined as in claim 1, and which are present in the form of their physiologically acceptable salts with acids, the acids being selected from the group B comprising hydrochloric acid, hydrobromic acid, sulphuric acid, phosphoric acid, benzenesulphonic acid, p-toluenesulphonic acid, maleic acid, succinic acid, fumaric acid, D-(−)-tartaric acid, L-(+)-tartaric acid, naphthalene-2-sulphonic acid and naphthalene-1,5-disulphonic acid, and the polymorphs, the corresponding solvates and hydrates thereof.
摘要翻译： 本发明涉及通式Ⅰ的新的结晶化合物A，其中A1，A2，A3，X，Y1，Y2和Y3如权利要求1中所定义，并且以其与酸的生理上可接受的盐的形式存在， 选自乙酸，氢溴酸，硫酸，磷酸，苯磺酸，对甲苯磺酸，马来酸，琥珀酸，富马酸，D - （ - ） - 酒石酸，L-（ +） - 酒石酸，萘-2-磺酸和萘-1,5-二磺酸，其多晶型物，相应的溶剂合物和水合物。
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![9-[4-(3-CHLORO-2-FLUORO-PHENYLAMINO)-7-METHOXY-QUINAZOLINE-6-YLOXY]-1,4-DIAZA-SPIRO[5.5]UNDECANE-5-ONE DIMALEATE, USE THEREOF AS A MEDICAMENT AND METHOD FOR THE PRODUCTION THEREOF](/abs-image/US/2013/01/31/US20130030003A1/abs.jpg.150x150.jpg)
18.发明申请9-[4-(3-CHLORO-2-FLUORO-PHENYLAMINO)-7-METHOXY-QUINAZOLINE-6-YLOXY]-1,4-DIAZA-SPIRO[5.5]UNDECANE-5-ONE DIMALEATE, USE THEREOF AS A MEDICAMENT AND METHOD FOR THE PRODUCTION THEREOF 有权9- [4-（3-氯代-2-氟 - 苯基）-7-甲氧基喹唑啉-6-甲氧基] -1,4-二氮杂螺[5.5]联苯-5-酮二甲醚，其作为药物使用 及其生产方法公开(公告)号：US20130030003A1
公开(公告)日：2013-01-31
申请号：US13359807
申请日：2012-01-27
IPC分类号： C07D403/12 , A61P11/00 , A61P11/06 , A61K31/517 , C07D241/52
CPC分类号： C07D241/38 , C07D239/70 , C07D403/12
摘要： The present invention relates to a compound of formula (I), which has valuable pharmacological properties, particularly an inhibiting effect on signal transduction mediated by tyrosine kinases, processes for stereoselectively preparing these compounds, particularly pharmaceutical formulations suitable for inhalation and their use for the treatment of diseases, particularly tumoral diseases, benign prostatic hyperplasia and diseases of the lungs and airways.
摘要翻译： 本发明涉及式（I）化合物，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，立体选择性制备这些化合物的方法，特别是适用于吸入的药物制剂及其用于治疗 的疾病，特别是肿瘤疾病，良性前列腺增生和肺和气道疾病。
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公开(公告)号：US20110295000A1
公开(公告)日：2011-12-01
申请号：US13204969
申请日：2011-08-08
申请人： Guenther HUCHLER , Werner RALL , Uwe REIS
发明人： Guenther HUCHLER , Werner RALL , Uwe REIS
IPC分类号： C07D413/04 , C07D401/04 , C07D211/06
CPC分类号： C07D401/04 , C07C59/52 , C07C59/64 , C07C59/68 , C07C229/42 , C07D401/14
摘要： The present invention relates to a process for preparing compounds of general formula I wherein R1 and R2 are defined as in claim 1, the pharmaceutically acceptable salts and the solvates thereof, which may be prepared starting from compounds of general formula II wherein R1 is defined as in claim 1.
摘要翻译： 本发明涉及一种制备通式Ⅰ化合物的方法，其中R 1和R 2如权利要求1所定义，其药学上可接受的盐和溶剂化物，其可以从通式II的化合物开始制备，其中R1定义为 在权利要求1中。
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公开(公告)号：US20110183987A1
公开(公告)日：2011-07-28
申请号：US12846943
申请日：2010-07-30
IPC分类号： A61K31/499 , C07D401/12 , A61P35/00 , A61P11/00
CPC分类号： C07D403/12 , C07D239/70 , C07D241/38 , Y02P20/55
摘要： The present invention relates to a process for the stereoselective preparation of compounds of formulae (1A) and (1B) and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids and bases, which have valuable pharmacological properties, particularly an inhibitory effect on signal transduction mediated by tyrosine kinases, the use thereof for the treatment of diseases, particularly tumoral diseases as well as benign prostatic hyperplasia (BPH), diseases of the lungs and airways.
摘要翻译： 本发明涉及立体选择性制备式（1A）和（1B）化合物及其盐，特别是其与无机或有机酸和碱的生理上可接受的盐，其具有有价值的药理学性质，特别是抑制性 对由酪氨酸激酶介导的信号转导的作用，其用于治疗疾病，特别是肿瘤疾病以及良性前列腺增生（BPH），肺和气道疾病的用途。
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