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公开(公告)号：US08263585B2
公开(公告)日：2012-09-11
申请号：US12180969
申请日：2008-07-28
申请人： Ian Bruce , Andrew Dunstan , Thomas Anthony Hunt , Catherine Howsham , Thomas Ullrich , Amarylla Horvath
发明人： Ian Bruce , Andrew Dunstan , Thomas Anthony Hunt , Catherine Howsham , Thomas Ullrich , Amarylla Horvath
IPC分类号： A61K31/395 , A61K31/505 , A61K31/535 , C07D239/02 , C07D413/12
CPC分类号： C07D405/12 , C07D239/42 , C07D401/12 , C07D403/12
摘要： The present invention concerns a compound of formula (I) or a salt, suitably a pharmaceutically acceptable salt, or solvate thereof, wherein the groups R1, R2, Ar′, A and B are 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）化合物或其盐，合适的其药学上可接受的盐或溶剂化物，其中R1，R2，Ar'，A和B基团在说明书中定义为组合物和用途 通过抑制磷脂酰肌醇3-激酶治疗疾病的化合物。
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公开(公告)号：US20090163463A1
公开(公告)日：2009-06-25
申请号：US12180969
申请日：2008-07-28
IPC分类号： A61K31/505 , C07D239/42 , C07D413/12 , A61K31/5377 , A61K31/397 , A61P19/00 , A61P35/00 , A61P3/00 , A61P37/08
CPC分类号： C07D405/12 , C07D239/42 , C07D401/12 , C07D403/12
摘要： The present invention concerns a compound of formula (I) or a salt, suitably a pharmaceutically acceptable salt, or solvate thereof, wherein the groups R1, R2, Ar′, A and B are 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）化合物或其盐，合适的其药学上可接受的盐或溶剂化物，其中R1，R2，Ar'，A和B基团在说明书中定义为组合物和用途 通过抑制磷脂酰肌醇3-激酶治疗疾病的化合物。
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3.发明申请TREATING DISEASES MEDIATED BY BLOCKADE OF THE EPITHELIAL SODIUM CHANNEL WITH PYRAZINE-2-CARBOXAMIDE DERIVATIVES 审中-公开用吡嗪-2-羧酰胺衍生物治疗由上皮细胞通道引起的疾病公开(公告)号：US20140171421A1
公开(公告)日：2014-06-19
申请号：US14186904
申请日：2014-02-21
申请人： Gurdip Bhalay , Emma Budd , Graham Charles Bloomfield , Stephen Paul Collingwood , Andrew Dunstan , Lee Edwards , Peter Gedeck , Catherine Howsham , Peter Hunt , Thomas Anthony Hunt , Paul Oakley , Nichola Smith
发明人： Gurdip Bhalay , Emma Budd , Graham Charles Bloomfield , Stephen Paul Collingwood , Andrew Dunstan , Lee Edwards , Peter Gedeck , Catherine Howsham , Peter Hunt , Thomas Anthony Hunt , Paul Oakley , Nichola Smith
IPC分类号： C07D471/10 , C07D519/00
CPC分类号： C07D519/00 , A61K31/497 , C07D403/12 , C07D471/04 , C07D471/10 , C07D471/20 , C07D473/34 , C07D487/04 , C07D487/10
摘要： A compound of Formula I in free or salt or solvate form, where R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and R11 have the meanings as indicated in the specification, is useful for treating diseases which respond to the blockade of the epithelial sodium channel. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.
摘要翻译： 式Ⅰ化合物，其中R1，R2，R3，R4，R5，R6，R7，R8，R9，R10和R11具有说明书中所述的含义，可用于治疗疾病， 对上皮钠通道的阻断作出反应。 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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4.发明授权Pyrazine-2-carboxamide derivatives to treat diseases mediated by blockade of the epithelial sodium channel 有权吡嗪-2-甲酰胺衍生物治疗由上皮钠通道阻断介导的疾病公开(公告)号：US08039472B2
公开(公告)日：2011-10-18
申请号：US12332086
申请日：2008-12-10
申请人： Gurdip Bhalay , Emma Budd , Graham Charles Bloomfield , Stephen Paul Collingwood , Andrew Dunstan , Lee Edwards , Peter Gedeck , Catherine Howsham , Peter Hunt , Thomas Anthony Hunt , Paul Oakley , Nichola Smith
发明人： Gurdip Bhalay , Emma Budd , Graham Charles Bloomfield , Stephen Paul Collingwood , Andrew Dunstan , Lee Edwards , Peter Gedeck , Catherine Howsham , Peter Hunt , Thomas Anthony Hunt , Paul Oakley , Nichola Smith
IPC分类号： A61K31/497 , A61K31/50 , C07D237/00
CPC分类号： C07D519/00 , A61K31/497 , C07D403/12 , C07D471/04 , C07D471/10 , C07D471/20 , C07D473/34 , C07D487/04 , C07D487/10
摘要： A compound of Formula I in free or salt or solvate form, where R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and R11 have the meanings as indicated in the specification, is useful for treating diseases which respond to the blockade of the epithelial sodium channel. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.
摘要翻译： 式Ⅰ化合物，其中R1，R2，R3，R4，R5，R6，R7，R8，R9，R10和R11具有说明书中所述的含义，可用于治疗疾病， 对上皮钠通道的阻断作出反应。 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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5.发明申请Treating diseases mediated by blockade of the epithelial sodium channel with pyrazine-2-carboxamide derivatives 审中-公开用吡嗪-2-甲酰胺衍生物治疗由上皮钠通道阻断介导的疾病公开(公告)号：US20110237572A1
公开(公告)日：2011-09-29
申请号：US13157893
申请日：2011-06-10
申请人： Gurpid Bhalay , Emma Budd , Graham Charles Bloomfield , Stephen Paul Collingwood , Andrew Dunstan , Lee Edwards , Peter Gedeck , Catherine Howsham , Peter Hunt , Thomas Anthony Hunt , Paul Oakley , Nichola Smith
发明人： Gurpid Bhalay , Emma Budd , Graham Charles Bloomfield , Stephen Paul Collingwood , Andrew Dunstan , Lee Edwards , Peter Gedeck , Catherine Howsham , Peter Hunt , Thomas Anthony Hunt , Paul Oakley , Nichola Smith
IPC分类号： A61K31/551 , A61K31/497 , A61K31/506 , A61K31/5377 , A61P29/00 , A61P37/08 , A61P11/00 , A61P11/08 , A61P11/06 , A61P35/00
CPC分类号： C07D519/00 , A61K31/497 , C07D403/12 , C07D471/04 , C07D471/10 , C07D471/20 , C07D473/34 , C07D487/04 , C07D487/10
摘要： A compound of Formula I in free or salt or solvate form, where R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and R11 have the meanings as indicated in the specification, is useful for treating diseases which respond to the blockade of the epithelial sodium channel. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.
摘要翻译： 式Ⅰ化合物，其中R1，R2，R3，R4，R5，R6，R7，R8，R9，R10和R11具有说明书中所述的含义，可用于治疗疾病， 对上皮钠通道的阻断作出反应。 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：US20100130506A1
公开(公告)日：2010-05-27
申请号：US12332086
申请日：2008-12-10
申请人： Gurdip BHALAY , Emma Budd , Graham Charles Bloomfield , Stephen Paul Collingwood , Andrew Dunstan , Lee Edwards , Peter Gedeck , Catherine Howsham , Peter Hunt , Thomas Anthony Hunt , Paul Oakley , Nichola Smith
发明人： Gurdip BHALAY , Emma Budd , Graham Charles Bloomfield , Stephen Paul Collingwood , Andrew Dunstan , Lee Edwards , Peter Gedeck , Catherine Howsham , Peter Hunt , Thomas Anthony Hunt , Paul Oakley , Nichola Smith
IPC分类号： A61K31/496 , A61K31/519 , A61K31/497 , C07D409/14 , C07D403/12 , C07D473/00 , C07D403/14 , A61P35/00 , A61P29/00 , A61P11/08 , A61P11/06
CPC分类号： C07D519/00 , A61K31/497 , C07D403/12 , C07D471/04 , C07D471/10 , C07D471/20 , C07D473/34 , C07D487/04 , C07D487/10
摘要： A compound of Formula I in free or salt or solvate form, where R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and R11 have the meanings as indicated in the specification, is useful for treating diseases which respond to the blockade of the epithelial sodium channel. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.
摘要翻译： 式Ⅰ化合物，其中R1，R2，R3，R4，R5，R6，R7，R8，R9，R10和R11具有说明书中所述的含义，可用于治疗疾病， 对上皮钠通道的阻断作出反应。 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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7.发明授权Treating diseases mediated by blockade of the epithelial sodium channel with pyrazine-2-carboxamide derivatives 有权用吡嗪-2-甲酰胺衍生物治疗由上皮钠通道阻断介导的疾病公开(公告)号：US08697687B2
公开(公告)日：2014-04-15
申请号：US13613495
申请日：2012-09-13
申请人： Gurdip Bhalay , Emma Budd , Graham Charles Bloomfield , Stephen Paul Collingwood , Andrew Dunstan , Lee Edwards , Peter Gedeck , Catherine Howsham , Peter Hunt , Thomas Anthony Hunt , Paul Oakley , Nichola Smith
发明人： Gurdip Bhalay , Emma Budd , Graham Charles Bloomfield , Stephen Paul Collingwood , Andrew Dunstan , Lee Edwards , Peter Gedeck , Catherine Howsham , Peter Hunt , Thomas Anthony Hunt , Paul Oakley , Nichola Smith
IPC分类号： A01N43/62 , A61K31/55 , A61K31/4965 , A61K31/535 , C07D237/00 , C07D239/00 , C07D241/00 , C07D413/00 , C07D243/08
CPC分类号： C07D519/00 , A61K31/497 , C07D403/12 , C07D471/04 , C07D471/10 , C07D471/20 , C07D473/34 , C07D487/04 , C07D487/10
摘要： A compound of Formula I in free or salt or solvate form, where R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and R11 have the meanings as indicated in the specification, is useful for treating diseases which respond to the blockade of the epithelial sodium channel. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.
摘要翻译： 式Ⅰ化合物，其中R1，R2，R3，R4，R5，R6，R7，R8，R9，R10和R11具有说明书中所述的含义，可用于治疗疾病， 对上皮钠通道的阻断作出反应。 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：US09643983B2
公开(公告)日：2017-05-09
申请号：US14847262
申请日：2015-09-08
申请人： Gurdip Bhalay , Emma Budd , Graham Charles Bloomfield , Stephen Paul Collingwood , Andrew Dunstan , Lee Edwards , Peter Gedeck , Catherine Howsham , Peter Hunt , Thomas Anthony Hunt , Paul Oakley , Nichola Smith
发明人： Gurdip Bhalay , Emma Budd , Graham Charles Bloomfield , Stephen Paul Collingwood , Andrew Dunstan , Lee Edwards , Peter Gedeck , Catherine Howsham , Peter Hunt , Thomas Anthony Hunt , Paul Oakley , Nichola Smith
IPC分类号： C07D519/00 , C07D403/12 , C07D471/10 , A61K31/497 , C07D471/04 , C07D471/20 , C07D473/34 , C07D487/04 , C07D487/10
CPC分类号： C07D519/00 , A61K31/497 , C07D403/12 , C07D471/04 , C07D471/10 , C07D471/20 , C07D473/34 , C07D487/04 , C07D487/10
摘要： A compound of Formula I in free or salt or solvate form, where R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and R11 have the meanings as indicated in the specification, is useful for treating diseases which respond to the blockade of the epithelial sodium channel. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.
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9.发明授权Treating diseases mediated by blockade of the epithelial sodium channel with pyrazine-2-carboxamide derivatives 有权用吡嗪-2-甲酰胺衍生物治疗由上皮钠通道阻断介导的疾病公开(公告)号：US09139586B2
公开(公告)日：2015-09-22
申请号：US14186904
申请日：2014-02-21
申请人： Gurdip Bhalay , Emma Budd , Graham Charles Bloomfield , Stephen Paul Collingwood , Andrew Dunstan , Lee Edwards , Peter Gedeck , Catherine Howsham , Peter Hunt , Thomas Anthony Hunt , Paul Oakley , Nichola Smith
发明人： Gurdip Bhalay , Emma Budd , Graham Charles Bloomfield , Stephen Paul Collingwood , Andrew Dunstan , Lee Edwards , Peter Gedeck , Catherine Howsham , Peter Hunt , Thomas Anthony Hunt , Paul Oakley , Nichola Smith
IPC分类号： A61K31/55 , A61K31/4965 , C07D471/10 , C07D403/12 , C07D471/04 , C07D471/20 , C07D473/34 , C07D487/04 , C07D487/10 , C07D519/00
CPC分类号： C07D519/00 , A61K31/497 , C07D403/12 , C07D471/04 , C07D471/10 , C07D471/20 , C07D473/34 , C07D487/04 , C07D487/10
摘要： A compound of Formula I in free or salt or solvate form, where R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and R11 have the meanings as indicated in the specification, is useful for treating diseases which respond to the blockade of the epithelial sodium channel. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.
摘要翻译： 式Ⅰ化合物，其中R1，R2，R3，R4，R5，R6，R7，R8，R9，R10和R11具有说明书中所述的含义，可用于治疗疾病， 对上皮钠通道的阻断作出反应。 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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10.发明授权3,5-diamino-6-chloro-pyrazine-2-carboxylic acid derivatives and their use as epithelial sodium channel blockers for the treatment of airway diseases 有权3,5-二氨基-6-氯 - 吡嗪-2-羧酸衍生物及其作为用于治疗气道疾病的上皮钠通道阻滞剂的用途公开(公告)号：US08664228B2
公开(公告)日：2014-03-04
申请号：US12990905
申请日：2009-05-11
IPC分类号： A61K31/4965
CPC分类号： C07D241/28 , C07D401/12 , C07D403/12
摘要： A compound of Formula I in free or salt or solvate form, where R1, R2, R3, R4, R5, R6, R7, R8 and R9 have the meanings as indicated in the specification, is useful for treating diseases which respond to the blockade of the epithelial sodium channel. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.
摘要翻译： 游离或盐或溶剂化物形式的式I化合物，其中R 1，R 2，R 3，R 4，R 5，R 6，R 7，R 8和R 9具有说明书中指出的含义，可用于治疗对阻断作出反应的疾病 的上皮钠通道。 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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