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1.发明申请公开(公告)号：US20110312932A1
公开(公告)日：2011-12-22
申请号：US13217480
申请日：2011-08-25
申请人： Alessandra BARTOLOZZI , Angela BERRY , Eugene Richard HICKEY , Markus OSTERMEIER , Doris RIETHER , Achim SAUER , David Smith THOMSON , Lifen WU , Renee M. ZINDELL , Patricia AMOUZEGH , Nigel James BLUMIRE , Stephen Peter EAST , Monika ERMANN , Someina KHOR , Innocent MUSHI
发明人： Alessandra BARTOLOZZI , Angela BERRY , Eugene Richard HICKEY , Markus OSTERMEIER , Doris RIETHER , Achim SAUER , David Smith THOMSON , Lifen WU , Renee M. ZINDELL , Patricia AMOUZEGH , Nigel James BLUMIRE , Stephen Peter EAST , Monika ERMANN , Someina KHOR , Innocent MUSHI
IPC分类号： A61K31/422 , A61K31/428 , A61K31/42 , A61P25/04 , A61K31/427 , A61K31/433 , A61P29/00 , A61K31/4196 , A61K31/454
CPC分类号： C07D413/12 , C07D249/14 , C07D261/14 , C07D405/12 , C07D413/04 , C07D413/14
摘要： Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
摘要翻译： 公开了式（I）的化合物。 根据本发明的化合物结合并且是CB 2受体的激动剂，拮抗剂或反向激动剂，并且可用于治疗炎症。 作为激动剂的那些化合物另外可用于治疗疼痛。
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2.发明申请公开(公告)号：US20120010184A1
公开(公告)日：2012-01-12
申请号：US13238054
申请日：2011-09-21
申请人： Alessandra BARTOLOZZI , Angela BERRY , Eugene Richard HICKEY , Markus OSTERMEIER , Doris RIETHER , Achim SAUER , David Smith THOMSON , Lifen WU , Renee M. ZINDELL , Patricia AMOUZEGH , Nigel James BLUMIRE , Stephen Peter EAST , Monika ERMANN , Someina KHOR , Innocent MUSHI
发明人： Alessandra BARTOLOZZI , Angela BERRY , Eugene Richard HICKEY , Markus OSTERMEIER , Doris RIETHER , Achim SAUER , David Smith THOMSON , Lifen WU , Renee M. ZINDELL , Patricia AMOUZEGH , Nigel James BLUMIRE , Stephen Peter EAST , Monika ERMANN , Someina KHOR , Innocent MUSHI
IPC分类号： A61K31/422 , A61K31/433 , A61K31/428 , A61K31/426 , A61K31/42 , A61K31/4196 , C07D401/12 , C07D285/135 , C07D417/12 , C07D413/12 , C07D249/14 , C07D261/14 , C07D403/12 , A61P29/00 , A61K31/454
CPC分类号： C07D413/12 , C07D249/14 , C07D261/14 , C07D405/12 , C07D413/04 , C07D413/14
摘要： Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
摘要翻译： 公开了式（I）的化合物。 根据本发明的化合物结合并且是CB 2受体的激动剂，拮抗剂或反向激动剂，并且可用于治疗炎症。 作为激动剂的那些化合物另外可用于治疗疼痛。
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公开(公告)号：US20100081644A1
公开(公告)日：2010-04-01
申请号：US12564132
申请日：2009-09-22
申请人： Alessandra BARTOLOZZI , Angela BERRY , Eugene Richard HICKEY , Markus OSTERMEIER , Doris RIETHER , Achim SAUER , David Smith THOMSON , Lifen WU , Renee M. ZINDELL , Patricia AMOUZEGH , Nigel James BLUMIRE , Stephen Peter EAST , Monika ERMANN , Someina KHOR , Innocent MUSHI
发明人： Alessandra BARTOLOZZI , Angela BERRY , Eugene Richard HICKEY , Markus OSTERMEIER , Doris RIETHER , Achim SAUER , David Smith THOMSON , Lifen WU , Renee M. ZINDELL , Patricia AMOUZEGH , Nigel James BLUMIRE , Stephen Peter EAST , Monika ERMANN , Someina KHOR , Innocent MUSHI
IPC分类号： A61K31/4196 , C07D413/12 , A61K31/422 , C07D417/12 , A61K31/41 , A61K31/454 , C07D249/14
CPC分类号： C07D413/12 , C07D249/14 , C07D261/14 , C07D405/12 , C07D413/04 , C07D413/14
摘要： Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
摘要翻译： 公开了式（I）的化合物。 根据本发明的化合物结合并且是CB 2受体的激动剂，拮抗剂或反向激动剂，并且可用于治疗炎症。 作为激动剂的那些化合物另外可用于治疗疼痛。
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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)
4.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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![Process for preparing spiro[2.5]octane-5,7-dione](/abs-image/US/2014/02/06/US20140039203A1/abs.jpg.150x150.jpg)
公开(公告)号：US20140039203A1
公开(公告)日：2014-02-06
申请号：US13956604
申请日：2013-08-01
申请人： Torsten BUSCH , Sven ANKLAM , Joerg JUNG , Markus OSTERMEIER
发明人： Torsten BUSCH , Sven ANKLAM , Joerg JUNG , Markus OSTERMEIER
IPC分类号： C07D311/96 , C07C45/65
CPC分类号： C07C45/65 , C07C45/455 , C07C49/443 , C07C51/08 , C07C51/083 , C07C59/205 , C07C67/08 , C07C67/30 , C07C67/343 , C07C69/608 , C07C69/635 , C07C69/716 , C07C259/06 , C07C2601/02 , C07C2602/50 , C07D311/96 , C07C55/28
摘要： Disclosed is a method for the synthesis of spiro[2.5]octane-5,7-dione useful as intermediate in the manufacture of pharmaceutically active ingredients. Also disclosed are novel intermediates used in the synthesis of this compound.
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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)
6.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：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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![Process for preparing spiro[2.5]octane-5,7-dione](/abs-image/US/2014/11/13/US20140336405A1/abs.jpg.150x150.jpg)
公开(公告)号：US20140336405A1
公开(公告)日：2014-11-13
申请号：US14445371
申请日：2014-07-29
申请人： Torsten BUSCH , Sven ANKLAM , Joerg JUNG , Markus OSTERMEIER
发明人： Torsten BUSCH , Sven ANKLAM , Joerg JUNG , Markus OSTERMEIER
IPC分类号： C07C45/65 , C07C69/608 , C07C259/06 , C07C69/635 , C07C69/716 , C07C59/205
CPC分类号： C07C45/65 , C07C45/455 , C07C49/443 , C07C51/08 , C07C51/083 , C07C59/205 , C07C67/08 , C07C67/30 , C07C67/343 , C07C69/608 , C07C69/635 , C07C69/716 , C07C259/06 , C07C2601/02 , C07C2602/50 , C07D311/96 , C07C55/28
摘要： Disclosed is a method for the synthesis of spiro[2.5]octane-5,7-dione useful as intermediate in the manufacture of pharmaceutically active ingredients. Also disclosed are novel intermediates used in the synthesis of this compound.
摘要翻译： 公开了用于合成制备药物活性成分的螺[2.5]辛烷-5,7-二酮作为中间体的方法。 还公开了用于合成该化合物的新型中间体。
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公开(公告)号：US20140135495A1
公开(公告)日：2014-05-15
申请号：US14154441
申请日：2014-01-14
IPC分类号： C07D403/12 , C07D241/38
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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![FUMARIC ACID SALT OF 9-[4-(3-CHLORO-2-FLUORO-PHENYLAMINO)-7-METHOXY-QUINAZOLIN-6-YLOXY]-1,4-DIAZA-SPIRO[5.5]UNDECAN-5-ONE, ITS USE AS A MEDICAMENT AND THE PREPARATION THEREOF](/abs-image/US/2014/01/23/US20140024628A1/abs.jpg.150x150.jpg)
10.发明申请FUMARIC ACID SALT OF 9-[4-(3-CHLORO-2-FLUORO-PHENYLAMINO)-7-METHOXY-QUINAZOLIN-6-YLOXY]-1,4-DIAZA-SPIRO[5.5]UNDECAN-5-ONE, ITS USE AS A MEDICAMENT AND THE PREPARATION THEREOF 有权9- [4-（3-氯-2-氟 - 苯基氨基）-7-甲氧基 - 喹唑啉-6-基] -1,4-二氮杂螺[5.5]十二烷-5-磺酸的盐酸盐，其用途 作为药物及其制剂公开(公告)号：US20140024628A1
公开(公告)日：2014-01-23
申请号：US13944323
申请日：2013-07-17
申请人： Markus OSTERMEIER , Peter SIEGER
发明人： Markus OSTERMEIER , Peter SIEGER
IPC分类号： C07D403/12 , C07C51/41 , C07C57/15 , A61K31/517 , A61K45/06
CPC分类号： C07D403/12 , A61K31/517 , A61K45/06 , C07C51/41 , C07C57/15
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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