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公开(公告)号：US20130245279A1
公开(公告)日：2013-09-19
申请号：US13614941
申请日：2012-09-13
Applicant: John Demattei , Sagar Shakya , Anthony D. Piscopio , Bruno P. Hache , Matthew Charles Evans , James Gair Ford , Simon Mark Pointon , Koen Peeters , Timothy John Lilley , John Leonard
Inventor： John Demattei , Sagar Shakya , Anthony D. Piscopio , Bruno P. Hache , Matthew Charles Evans , James Gair Ford , Simon Mark Pointon , Koen Peeters , Timothy John Lilley , John Leonard
IPC: C07D235/06
CPC classification number: C07D235/06 , C07C201/08 , C07C205/58 , C07C227/04 , C07C227/08 , C07C227/18 , C07C229/60
Abstract: Provided are processes for the preparation of benzimidazole structures having Formula VIIIb-1: and salts and solvates thereof, wherein Z, X5, R2b, R2c and R10 are as defined herein. Compounds of Formula VIIIb-1 are useful for the preparation of benzimidazole derivatives.
Abstract translation: 提供制备具有式VIIIb-1的苯并咪唑结构的方法及其盐和溶剂化物，其中Z，X5，R2b，R2c和R10如本文所定义。 式VIIIb-1的化合物可用于制备苯并咪唑衍生物。
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公开(公告)号：US09024040B2
公开(公告)日：2015-05-05
申请号：US13614941
申请日：2012-09-13
Applicant: John DeMattei , Sagar Shakya , Anthony D. Piscopio , Bruno P. Hache , Matthew Charles Evans , James Gair Ford , Simon Mark Pointon , Koen Peeters , Timothy John Lilley , John Leonard
Inventor： John DeMattei , Sagar Shakya , Anthony D. Piscopio , Bruno P. Hache , Matthew Charles Evans , James Gair Ford , Simon Mark Pointon , Koen Peeters , Timothy John Lilley , John Leonard
IPC: C07D235/00 , C07D403/02 , C07D235/18 , C07D235/06 , C07C205/58 , C07C229/60 , C07C201/08 , C07C227/04 , C07C227/08 , C07C227/18
CPC classification number: C07D235/06 , C07C201/08 , C07C205/58 , C07C227/04 , C07C227/08 , C07C227/18 , C07C229/60
Abstract: Provided are processes for the preparation of benzimidazole structures having Formula VIIIb-1: and salts and solvates thereof, wherein Z, X5, R2b, R2c and R10 are as defined herein. Compounds of Formula VIIIb-1 are useful for the preparation of benzimidazole derivatives.
Abstract translation: 提供制备具有式VIIIb-1的苯并咪唑结构的方法及其盐和溶剂化物，其中Z，X5，R2b，R2c和R10如本文所定义。 式VIIIb-1的化合物可用于制备苯并咪唑衍生物。
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公开(公告)号：US20110319631A1
公开(公告)日：2011-12-29
申请号：US13229459
申请日：2011-09-09
Applicant: John Demattei , Sagar Shakya , Anthony D. Piscopio , Bruno P. Hache , Matthew Charles Evans , James Gair Ford , Simon Mark Pointon , Koen Peeters , Timothy John Lilley , John Leonard
Inventor： John Demattei , Sagar Shakya , Anthony D. Piscopio , Bruno P. Hache , Matthew Charles Evans , James Gair Ford , Simon Mark Pointon , Koen Peeters , Timothy John Lilley , John Leonard
IPC: C07D235/06
CPC classification number: C07D235/06 , C07C201/08 , C07C205/58 , C07C227/04 , C07C227/08 , C07C227/18 , C07C229/60
Abstract: Provided are methods for the synthesis of heterocyclic compounds such as benzimidazole carboxylic acid core structures having Formula Ib-1: wherein Z, X1, X2, X5, R2b and R10 are as defined herein. Compounds of Formula Ib-1 can be used to prepare heterocyclic derivatives such as benzimidazole derivatives.
Abstract translation: 提供了用于合成杂环化合物的方法，例如具有式Ib-1的苯并咪唑羧酸核心结构：其中Z，X1，X2，X5，R2b和R10如本文所定义。 式Ib-1的化合物可用于制备杂环衍生物如苯并咪唑衍生物。
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公开(公告)号：US08383832B2
公开(公告)日：2013-02-26
申请号：US13229459
申请日：2011-09-09
Applicant: John Demattei , Sagar Shakya , Anthony D. Piscopio , Bruno P. Hache , Matthew Charles Evans , James Gair Ford , Simon Mark Pointon , Koen Peeters , Timothy John Lilley , John Leonard
Inventor： John Demattei , Sagar Shakya , Anthony D. Piscopio , Bruno P. Hache , Matthew Charles Evans , James Gair Ford , Simon Mark Pointon , Koen Peeters , Timothy John Lilley , John Leonard
IPC: C07D235/04 , C07D403/02 , C07D235/18
CPC classification number: C07D235/06 , C07C201/08 , C07C205/58 , C07C227/04 , C07C227/08 , C07C227/18 , C07C229/60
Abstract: Provided are methods for the synthesis of heterocyclic compounds such as benzimidazole carboxylic acid core structures having Formula Ib-1: wherein Z, X1, X2, X5, R2b and R10 are as defined herein. Compounds of Formula Ib-1 can be used to prepare heterocyclic derivatives such as benzimidazole derivatives.
Abstract translation: 提供了用于合成杂环化合物的方法，例如具有式Ib-1的苯并咪唑羧酸核心结构：其中Z，X1，X2，X5，R2b和R10如本文所定义。 式Ib-1的化合物可用于制备杂环衍生物如苯并咪唑衍生物。
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![Crystalline forms of 4-(6-chloro-2,3-methylenedioxyanilino)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5-tetrahydropyran-4-yloxyquinazoline](/abs-image/US/2012/11/06/US08304417B2/abs.jpg.150x150.jpg)
5.发明授权Crystalline forms of 4-(6-chloro-2,3-methylenedioxyanilino)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5-tetrahydropyran-4-yloxyquinazoline 有权4-（6-氯-2,3-亚甲二氧基苯胺基）-7- [2-（4-甲基哌嗪-1-基）乙氧基] -5-四氢吡喃-4-基氧基喹唑啉的结晶形式公开(公告)号：US08304417B2
公开(公告)日：2012-11-06
申请号：US11793064
申请日：2005-12-14
Applicant: James Gair Ford , James Francis McCabe , Anne O'Kearney-McMullan , Simon Mark Pointon , Lyn Powell , Philip O'Keefe , Mark Purdie , Jane Withnall
Inventor： James Gair Ford , James Francis McCabe , Anne O'Kearney-McMullan , Simon Mark Pointon , Lyn Powell , Philip O'Keefe , Mark Purdie , Jane Withnall
IPC: A01N43/90 , A61K31/519 , C07D487/00
CPC classification number: C07D405/12
Abstract: The present invention relates to chemical processes useful in the manufacture of the compound 4-(6-chloro-2,3-methylenedioxyanilino)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5-tetrahydropyran-4-yloxyquinazoline (the active entity within AZD0530), to intermediates useful in the manufacture of that compound and to processes for the manufacture of those intermediates. The invention also relates to particular crystalline forms of that compound such as a difumarate salt and a trihydrate and to pharmaceutical compositions containing such crystalline forms.
Abstract translation: 本发明涉及可用于制备化合物4-（6-氯-2,3-亚甲二氧基苯胺基）-7- [2-（4-甲基哌嗪-1-基）乙氧基] -5-四氢吡喃-4 - 氧基喹唑啉（AZD0530中的活性实体），可用于制备该化合物的中间体和用于制备这些中间体的方法。 本发明还涉及该化合物的特定结晶形式，例如二磺酸盐和三水合物，以及含有这种结晶形式的药物组合物。
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Patent Agency Ranking
公开(公告)号：US20110319632A1
公开(公告)日：2011-12-29
申请号：US13229491
申请日：2011-09-09
Applicant: John Demattei , Sagar Shakya , Anthony D. Piscopio , Bruno P. Hache , Matthew Charles Evans , James Gair Ford , Simon Mark Pointon , Koen Peeters , Timothy John Lilley , John Leonard
Inventor： John Demattei , Sagar Shakya , Anthony D. Piscopio , Bruno P. Hache , Matthew Charles Evans , James Gair Ford , Simon Mark Pointon , Koen Peeters , Timothy John Lilley , John Leonard
IPC: C07D235/06
CPC classification number: C07D235/06 , C07C201/08 , C07C205/58 , C07C227/04 , C07C227/08 , C07C227/18 , C07C229/60
Abstract: Provided are compounds having Formula VIIIa-1: wherein Z, X5, R2, R2a and R10 are as defined herein. Compounds of Formula VIIIa-1 can be used to prepare heterocyclic derivatives such as benzimidazole derivatives.
Abstract translation: 提供具有式VIIIa-1的化合物：其中Z，X5，R2，R2a和R10如本文所定义。 式VIIIa-1的化合物可用于制备杂环衍生物如苯并咪唑衍生物。
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公开(公告)号：US20100145065A1
公开(公告)日：2010-06-10
申请号：US11993745
申请日：2006-06-21
Applicant: John Demattei , Sagar Shakya , Anthony D. Piscopio , Bruno P. Hache , Matthew Charles Evans , James Gair Ford , Simon Mark Pointon , Koen Peeters , Timothy John Lilley , John Leonard
Inventor： John Demattei , Sagar Shakya , Anthony D. Piscopio , Bruno P. Hache , Matthew Charles Evans , James Gair Ford , Simon Mark Pointon , Koen Peeters , Timothy John Lilley , John Leonard
IPC: C07D235/04 , C07C229/60 , C07C205/58
CPC classification number: C07D235/06 , C07C201/08 , C07C205/58 , C07C227/04 , C07C227/08 , C07C227/18 , C07C229/60
Abstract: Provided are methods for the synthesis of heterocyclic compounds such as benzimidazole carboxylic acid core structures having Formula Ia-1 and their synthetic intermediates: wherein Z, X1, X2, X5, R2 and R10 are as defined herein. Compounds of Formula Ia-1 and their synthetic intermediates can be used to prepare heterocyclic derivatives such as benzimidazole derivatives.
Abstract translation: 提供了用于合成杂环化合物的方法，例如具有式Ia-1的苯并咪唑羧酸核心结构及其合成中间体：其中Z，X1，X2，X5，R2和R10如本文所定义。 式Ia-1及其合成中间体的化合物可用于制备杂环衍生物如苯并咪唑衍生物。
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公开(公告)号：US20090099196A1
公开(公告)日：2009-04-16
申请号：US11793064
申请日：2005-12-14
Applicant: James Gair Ford , James Francis McCabe , Anne O'Kearney-McMullan , Simon Mark Pointon , Lyn Powell , Philip O'Keefe , Mark Purdie , Jane Withnall
Inventor： James Gair Ford , James Francis McCabe , Anne O'Kearney-McMullan , Simon Mark Pointon , Lyn Powell , Philip O'Keefe , Mark Purdie , Jane Withnall
IPC: A61K31/496 , C07D405/14 , A61P35/00
CPC classification number: C07D405/12
Abstract: The present invention relates to chemical processes useful in the manufacture of the compound 4-(6-chloro-2,3-methylenedioxyanilino)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5-tetrahydropyran-4-yloxyquinazoline (the active entity within AZD0530), to intermediates useful in the manufacture of that compound and to processes for the manufacture of those intermediates. The invention also relates to particular crystalline forms of that compound such as a difumarate salt and a trihydrate and to pharmaceutical compositions containing such crystalline forms.
Abstract translation: 本发明涉及可用于制备化合物4-（6-氯-2,3-亚甲二氧基苯胺基）-7- [2-（4-甲基哌嗪-1-基）乙氧基] -5-四氢吡喃-4 - 氧基喹唑啉（AZD0530中的活性实体），可用于制备该化合物的中间体和用于制备这些中间体的方法。 本发明还涉及该化合物的特定结晶形式，例如二磺酸盐和三水合物，以及含有这种结晶形式的药物组合物。
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公开(公告)号：US08501956B2
公开(公告)日：2013-08-06
申请号：US13229491
申请日：2011-09-09
Applicant: John Demattei , Sagar Shakya , Anthony D. Piscopio , Bruno P. Hache , Matthew Charles Evans , James Gair Ford , Simon Mark Pointon , Koen Peeters , Timothy John Lilley , John Leonard
Inventor： John Demattei , Sagar Shakya , Anthony D. Piscopio , Bruno P. Hache , Matthew Charles Evans , James Gair Ford , Simon Mark Pointon , Koen Peeters , Timothy John Lilley , John Leonard
IPC: C07D235/06 , C07D235/08 , C07D403/04 , C07D403/06
CPC classification number: C07D235/06 , C07C201/08 , C07C205/58 , C07C227/04 , C07C227/08 , C07C227/18 , C07C229/60
Abstract: Provided are compounds having Formula VIIIa-1: wherein Z, X5, R2, R2a and R10 are as defined herein. Compounds of Formula VIIIa-1 can be used to prepare heterocyclic derivatives such as benzimidazole derivatives.
Abstract translation: 提供具有式VIIIa-1的化合物：其中Z，X5，R2，R2a和R10如本文所定义。 式VIIIa-1的化合物可用于制备杂环衍生物如苯并咪唑衍生物。
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公开(公告)号：US08039637B2
公开(公告)日：2011-10-18
申请号：US11993745
申请日：2006-06-21
Applicant: John DeMattei , Sagar Shakya , Anthony D. Piscopio , Bruno P. Hache , Matthew Charles Evans , James Gair Ford , Simon Mark Pointon , Koen Peeters , Timothy John Lilley , John Leonard
Inventor： John DeMattei , Sagar Shakya , Anthony D. Piscopio , Bruno P. Hache , Matthew Charles Evans , James Gair Ford , Simon Mark Pointon , Koen Peeters , Timothy John Lilley , John Leonard
IPC: C07D235/06 , C07D235/08 , C07D403/04 , C07D403/06
CPC classification number: C07D235/06 , C07C201/08 , C07C205/58 , C07C227/04 , C07C227/08 , C07C227/18 , C07C229/60
Abstract: Provided are methods for the synthesis of heterocyclic compounds such as benzimidazole carboxylic acid core structures having Formula Ia-1 and their synthetic intermediates: wherein Z, X1, X2, X5, R2 and R10 are as defined herein. Compounds of Formula Ia-1 and their synthetic intermediates can be used to prepare heterocyclic derivatives such as benzimidazole derivatives.
Abstract translation: 提供了用于合成杂环化合物的方法，例如具有式Ia-1的苯并咪唑羧酸核心结构及其合成中间体：其中Z，X1，X2，X5，R2和R10如本文所定义。 式Ia-1及其合成中间体的化合物可用于制备杂环衍生物如苯并咪唑衍生物。
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