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公开(公告)号：US20100029705A1
公开(公告)日：2010-02-04
申请号：US12577855
申请日：2009-10-13
IPC分类号： A61K31/437 , A61K31/47 , A61P29/00
CPC分类号： A61K31/4709 , A61K45/06 , C07C215/80 , C07C233/43 , C07C311/08 , C07C2602/08 , C07D215/227 , C07D215/26 , C07D405/12
摘要： Compounds of formula in free or salt or solvate form, whereAr is a group of formula Y is carbon or nitrogen and R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, X, n, p, q and r are as defined in the specification, their preparation and their use as pharmaceuticals, particularly for the treatment of obstructive or inflammatory airways diseases.
摘要翻译： 其中Ar为式Y的化合物为碳或氮，R1，R2，R3，R4，R5，R6，R7，R8，R9，R10，X，n，p， q和r如说明书中所定义，它们的制备及其作为药物的用途，特别是用于治疗阻塞性或炎症性气道疾病。
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公开(公告)号：US20150065490A1
公开(公告)日：2015-03-05
申请号：US14534708
申请日：2014-11-06
IPC分类号： C07D417/12 , A61K31/428 , A61K31/5377 , A61K31/454 , A61K31/4545 , A61K31/55 , C07D277/68 , A61K45/06
CPC分类号： C07D417/12 , A61K31/428 , A61K31/454 , A61K31/4545 , A61K31/5377 , A61K31/55 , A61K45/06 , C07D277/68
摘要： Compounds of formula I in free or salt or solvate form, wherein X has the meaning indicated in the specification, are useful for treating conditions that are prevented or alleviated by activation of the β2-adrenoreceptor. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.
摘要翻译： 游离或盐或溶剂合物形式的式I化合物，其中X具有说明书中指出的含义，可用于治疗通过活化2-肾上腺素受体而预防或缓解的病症。 还描述了含有化合物的药物组合物和用于制备化合物的方法。
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公开(公告)号：US20160075670A1
公开(公告)日：2016-03-17
申请号：US14947458
申请日：2015-11-20
申请人： Jun CAO , Bernhard ERB , Robin Alec FAIRHURST , Arnaud GRANDEURY , Shinji HATAKEYAMA , Magdalena KOZICZAK-HOLBRO , Philipp LUSTENBERGER , Bernd RIEBESEHL , Nicola TUFILLI , Thomas ULLRICH , Xiang WU , Jianguang ZHOU
发明人： Jun CAO , Bernhard ERB , Robin Alec FAIRHURST , Arnaud GRANDEURY , Shinji HATAKEYAMA , Magdalena KOZICZAK-HOLBRO , Philipp LUSTENBERGER , Bernd RIEBESEHL , Nicola TUFILLI , Thomas ULLRICH , Xiang WU , Jianguang ZHOU
IPC分类号： C07D277/68 , C07C53/10
CPC分类号： A61K31/428 , A61K31/167 , A61K45/06 , C07B2200/07 , C07C53/10 , C07D277/68 , Y02P20/55
摘要： The present invention provides a compound of formula (I) in free form or in pharmaceutically acceptable salt form a method for manufacturing the compound of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and pharmaceutical compositions.
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4.发明申请Particles of N-(5-cyano-4-((2-methoxyethyl)amino)pyridin-2-yl)-7-formyl-6-((4-methyl-2-oxopiperazin-1-yl)methyl)-3,4-dihydro-1,8-naphthyridine-1(2H)-carboxamide 有权N-（5-氰基-4 - （（2-甲氧基乙基）氨基）吡啶-2-基）-7-甲酰基-6 - （（4-甲基-2-氧代哌嗪-1-基）甲基）-3 ，4-二氢-1,8-二氮杂萘-1（2H） - 甲酰胺公开(公告)号：US20160304489A1
公开(公告)日：2016-10-20
申请号：US15073766
申请日：2016-03-18
申请人： Nicole BUSCHMANN , Robin Alec FAIRHURST , Pascal FURET , Bo HAN , Thomas KNÖPFEL , Catherine LEBLANC , Lv LIAO , Robert MAH , Franck MALLET , Julie MARTZ , Can WANG , Jing XIONG , Xianglin ZHAO
发明人： Nicole BUSCHMANN , Robin Alec FAIRHURST , Pascal FURET , Bo HAN , Thomas KNÖPFEL , Catherine LEBLANC , Lv LIAO , Robert MAH , Franck MALLET , Julie MARTZ , Can WANG , Jing XIONG , Xianglin ZHAO
IPC分类号： C07D401/14 , C07C51/41 , C07C59/265
CPC分类号： C07D401/14 , C07B2200/13 , C07C51/412 , C07C59/265 , C07D471/04
摘要： The present invention relates to particles of N-(5-cyano-4-((2-methoxyethyl)amino)pyridin-2-yl)-7-formyl-6-((4-methyl-2-oxopiperazin-1-yl)methyl)-3,4-dihydro-1,8-naphthyridine-1(2H)-carboxamide, to a process of making said particles, to pharmaceutical compositions comprising said particles and to method of treating cancers using said pharmaceutical compositions.
摘要翻译： 本发明涉及N-（5-氰基-4 - （（2-甲氧基乙基）氨基）吡啶-2-基）-7-甲酰基-6 - （（4-甲基-2-氧代哌嗪-1-基） ）甲基）-3,4-二氢-1,8-二氮杂萘-1（2H） - 甲酰胺，制备所述颗粒的方法，包含所述颗粒的药物组合物和使用所述药物组合物治疗癌症的方法。
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公开(公告)号：US20150336914A1
公开(公告)日：2015-11-26
申请号：US14817175
申请日：2015-08-03
申请人： Jun CAO , Bernhard ERB , Robin Alec FAIRHURST , Arnaud GRANDEURY , Shinji HATAKEYAMA , Magdalena KOZICZAK-HOLBRO , Philipp LUSTENBERGER , Bernd RIEBESEHL , Nicola TUFILLI , Thomas ULLRICH , Xiang WU , Jianguang ZHOU
发明人： Jun CAO , Bernhard ERB , Robin Alec FAIRHURST , Arnaud GRANDEURY , Shinji HATAKEYAMA , Magdalena KOZICZAK-HOLBRO , Philipp LUSTENBERGER , Bernd RIEBESEHL , Nicola TUFILLI , Thomas ULLRICH , Xiang WU , Jianguang ZHOU
IPC分类号： C07D277/68
CPC分类号： A61K31/428 , A61K31/167 , A61K45/06 , C07B2200/07 , C07C53/10 , C07D277/68 , Y02P20/55
摘要： The present invention provides a compound of formula (I) in free form or in pharmaceutically acceptable salt form a method for manufacturing the compound of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and pharmaceutical compositions.
摘要翻译： 本发明提供游离形式或药学上可接受的盐形式的式（I）化合物，其制备本发明化合物的方法及其治疗用途。 本发明还提供药理活性剂和药物组合物的组合。
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公开(公告)号：US20140378450A1
公开(公告)日：2014-12-25
申请号：US14478523
申请日：2014-09-05
申请人： Giorgio CARAVATTI , Robin Alec FAIRHURST , Pascal FURET , Clive MCCARTHY , Heinrich RUEEGER , Frank Hans SEILER , Frédéric STAUFFER
发明人： Giorgio CARAVATTI , Robin Alec FAIRHURST , Pascal FURET , Clive MCCARTHY , Heinrich RUEEGER , Frank Hans SEILER , Frédéric STAUFFER
IPC分类号： C07D498/04 , A61K31/5377 , C07D413/14
CPC分类号： C07D498/04 , A61K31/5377 , A61K45/06 , C07D413/14
摘要： The present invention relates to oxazolidin-2-one substituted pyrimidine compounds that act as PI3K (phosphatidylinositol-3-kinase) inhibitors, as well as pharmaceutical compositions thereof, methods for their manufacture and uses for the treatment of conditions, diseases and disorders dependent on PI3K.
摘要翻译： 本发明涉及作为PI3K（磷脂酰肌醇-3-激酶）抑制剂的恶唑烷-2-酮取代的嘧啶化合物及其药物组合物，其制备方法和用于治疗依赖于 PI3K。
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公开(公告)号：US20160279107A1
公开(公告)日：2016-09-29
申请号：US15178579
申请日：2016-06-10
申请人： Jun CAO , Bernhard ERB , Robin Alec FAIRHURST , Arnaud GRANDEURY , Shinji HATAKEYAMA , Magdalena KOZICZAK-HOLBRO , Xinzhong LAI , Philipp LUSTENBERGER , Bernd Ulrich RIEBESEHL , Nicola TUFILLI , Thomas ULLRICH , Xiang Wu , Jianguang ZHOU
发明人： Jun CAO , Bernhard ERB , Robin Alec FAIRHURST , Arnaud GRANDEURY , Shinji HATAKEYAMA , Magdalena KOZICZAK-HOLBRO , Xinzhong LAI , Philipp LUSTENBERGER , Bernd Ulrich RIEBESEHL , Nicola TUFILLI , Thomas ULLRICH , Xiang Wu , Jianguang ZHOU
IPC分类号： A61K31/428
CPC分类号： A61K31/428 , A61K31/167 , A61K45/06 , C07B2200/07 , C07C53/10 , C07D277/68 , Y02P20/55
摘要： The present invention provides a compound of formula (I) in free form or in pharmaceutically acceptable salt form a method for manufacturing the compound of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and pharmaceutical compositions.
摘要翻译： 制备本发明化合物的方法及其治疗用途。 本发明还提供药理活性剂和药物组合物的组合。
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公开(公告)号：US20150094346A1
公开(公告)日：2015-04-02
申请号：US14566021
申请日：2014-12-10
申请人： Jun CAO , Bernhard ERB , Robin Alec FAIRHURST , Arnaud GRANDEURY , Shinji HATAKEYAMA , Magdalena KOZICZAK-HOLBRO , Philipp LUSTENBERGER , Bernd RIEBESEHL , Nicola TUFILLI , Thomas ULLRICH , Xiang WU , Jianguang ZHOU
发明人： Jun CAO , Bernhard ERB , Robin Alec FAIRHURST , Arnaud GRANDEURY , Shinji HATAKEYAMA , Magdalena KOZICZAK-HOLBRO , Philipp LUSTENBERGER , Bernd RIEBESEHL , Nicola TUFILLI , Thomas ULLRICH , Xiang WU , Jianguang ZHOU
IPC分类号： C07D277/68 , A61K31/167 , A61K31/428
CPC分类号： A61K31/428 , A61K31/167 , A61K45/06 , C07B2200/07 , C07C53/10 , C07D277/68 , Y02P20/55
摘要： The present invention provides a compound of formula (I) in free form or in pharmaceutically acceptable salt form a method for manufacturing the compound of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and pharmaceutical compositions.
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公开(公告)号：US20110003786A1
公开(公告)日：2011-01-06
申请号：US12829526
申请日：2010-07-02
IPC分类号： A61K31/519 , C07D513/04 , A61K31/429 , A61K31/5377 , C07D513/14 , A61K31/437 , A61P35/00
CPC分类号： C07D513/04 , C07D513/14
摘要： The present invention relates to compounds of formula I and salts thereof, wherein the substituents are as defined in the description, to compositions and use of the compounds in the treatment of diseases ameloriated by inhibition of phosphatidylinositol 3-kinase.
摘要翻译： 本发明涉及式I化合物及其盐，其中取代基如本说明书所定义，化合物在治疗通过抑制磷脂酰肌醇3-激酶而变性的疾病中的组合物和用途。
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公开(公告)号：US20160000761A1
公开(公告)日：2016-01-07
申请号：US14770819
申请日：2014-02-26
申请人： Miloud ACHOUR , Robin Alec FAIRHURST , Arnaud GRANDEURY , Shinji HATAKEYAMA , Magdalena KOZICZAK-HOLBRO , Nicola TUFILLI , Thomas ULLRICH
发明人： Miloud ACHOUR , Robin Alec FAIRHURST , Arnaud GRANDEURY , Shinji HATAKEYAMA , Magdalena KOZICZAK-HOLBRO , Nicola TUFILLI , Thomas ULLRICH
IPC分类号： A61K31/428 , A61K9/48 , A61K9/20 , A61K31/19 , A61K9/00
CPC分类号： A61K31/428 , A61K9/0053 , A61K9/2018 , A61K9/2054 , A61K9/485 , A61K9/4858 , A61K9/4866 , A61K31/19
摘要： The present invention relates to a pharmaceutical composition in solid oral dosage form comprising (R)-7-(2-(1-(4-butoxyphenyl)-2-methylpropan-2-ylamino)-1-hydroxyethyl)-5-hydroxybenzo[d]thiazol-2(3H)-one acetate salt.
摘要翻译： 本发明涉及一种固体口服剂型的药物组合物，其包含（R）-7-（2-（1-（4-丁氧基苯基）-2-甲基丙-2-基氨基）-1-羟乙基）-5-羟基苯并[ d]噻唑-2（3H） - 酮乙酸盐。
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