公开(公告)号：US10323001B2

公开(公告)日：2019-06-18

申请号：US15387322

申请日：2016-12-21

申请人： Athenex, Inc.

发明人： David G. Hangauer, Jr. ,  Debasis Patra ,  Jeremy A. Cody ,  Grant J. Palmer ,  Paul K. Isbester ,  Jonathon Salsbury

IPC分类号： C07D413/12 ,  A61K31/44 ,  C07D213/56 ,  C07D213/59

摘要： The invention relates to compositions comprising 2-(5-(4-(2-morpholinoethoxy)phenyl) pyridin-2-yl)-N-benzylacetamide and its mesylate and dihydrochloride salts. The invention provides an efficient process for the synthesis of 2-(5-(4-(2-morpholinoethoxy)phenyl)pyridin-2-yl)-N-benzylacetamide and its mesylate and dihydrochloride salts and methods for modulating one or more components of a kinase cascade using the compositions of the invention. The present invention also provides a novel polymorph of the mesylate salt of 2-(5-(4-(2-morpholinoethoxy)phenyl)pyridin-2-yl)-N-benzylacetamide (Form A), characterized by a unique X-ray diffraction pattern and Differential Scanning Calorimetry profile, as well as a unique crystalline structure.

公开(公告)号：US09556120B2

公开(公告)日：2017-01-31

申请号：US14554495

申请日：2014-11-26

申请人： Athenex, Inc.

发明人： David G. Hangauer, Jr. ,  Debasis Patra ,  Jeremy A. Cody ,  Grant J. Palmer ,  Paul K. Isbester ,  Jonathon Salsbury

IPC分类号： A61K31/535 ,  C07D213/56 ,  C07D213/59 ,  C07D413/12 ,  A61K31/44

CPC分类号： C07D213/56 ,  A61K31/44 ,  C07B2200/13 ,  C07D213/59 ,  C07D413/12

摘要： The invention relates to compositions comprising 2-(5-(4-(2-morpholinoethoxyl)phenyl)pyridin-2-yl)-N-benzylacetamide and its mesylate and dihydrochloride salts. The invention provides an efficient process for the synthesis of 2-(5-(4-(2-morpholinoethoxyl)phenyl)pyridin-2-yl)-N-benzylacetamide and its mesylate and dihydrochloride salts and methods for modulating one or more components of a kinase cascade using the compositions of the invention. The present invention also provides a novel polymorph of the mesylate salt of 2-(5-(4-(2-morpholinoethoxyl)phenyl)pyridin-2-yl)-N-benzylacetamide (Form A), characterized by a unique X-ray diffraction pattern and Differential Scanning Calorimetry profile, as well as a unique crystalline structure.

摘要翻译： 本发明涉及包含2-（5-（4-（2-吗啉代乙氧基）苯基）吡啶-2-基）-N-苄基乙酰胺及其甲磺酸盐和二盐酸盐的组合物。 本发明提供了合成2-（5-（4-（2-吗啉代乙氧基）苯基）吡啶-2-基）-N-苄基乙酰胺及其甲磺酸盐和二盐酸盐的有效方法和调节一种或多种组分的方法 使用本发明组合物的激酶级联。 本发明还提供2-（5-（4-（2-吗啉代乙氧基）苯基）吡啶-2-基）-N-苄基乙酰胺（形式A）的甲磺酸盐的新型多晶型物，其特征在于独特的X射线 衍射图和差示扫描量热法，以及独特的晶体结构。