公开(公告)号：US09776970B2

公开(公告)日：2017-10-03

申请号：US15120226

申请日：2015-02-20

申请人： Apotex Inc.

发明人： Padiyath Mohammed Akbarali ,  Venkata Ramana Kintali ,  Heggadde Nanjunda Bhatta Shreenivasa Murthy ,  Girisha Meenkere ,  Somanath Bhupal Venkata ,  Raja Ramesh Manda ,  Vishal Amrutlal Sodha ,  Abbulu Kante

IPC分类号： C07D401/12 ,  A61K31/496 ,  C07D215/54 ,  A61K31/4706 ,  A61K9/14

CPC分类号： C07D215/54 ,  A61K9/146 ,  A61K31/4706

摘要： The present subject matter relates to solvates and the amorphous form of bosutinib; the solvates namely being a propylene glycol solvate and an acetonitrile solvate. Also provided are processes for preparing the propylene glycol solvate, the amorphous form and the crystalline acetonitrile solvate of bosutinib; as well as compositions comprising said forms. Bosutinib is a 3-quinolinecarbonitrile kinase inhibitor and is indicated for the treatment of adult patients with chronic, accelerated, or blast phase Ph+ chronic myelogenous leukemia (CMS) with resistance or intolerance to prior therapy.

公开(公告)号：US20170057923A1

公开(公告)日：2017-03-02

申请号：US15120226

申请日：2015-02-20

申请人： Apotex Inc.

发明人： Padiyath Mohammed Akbarali ,  Venkata Ramana Kintali ,  Heggadde Nanjunda Bhatta Shreenivasa Murthy ,  Girisha Meenkere ,  Somanath Bhupal Venkata ,  Raja Ramesh Manda ,  Vishal Amrutlal Sodha ,  Abbulu Kante

IPC分类号： C07D215/54

CPC分类号： C07D215/54 ,  A61K9/146 ,  A61K31/4706

摘要： The present subject matter relates to solvates and the amorphous form of bosutinib; the solvates namely being a propylene glycol solvate and an acetonitrile solvate. Also provided are processes for preparing the propylene glycol solvate, the amorphous form and the crystalline acetonitrile solvate of bosutinib; as well as compositions comprising said forms. Bosutinib is a 3-quinolinecarbonitrile kinase inhibitor and is indicated for the treatment of adult patients with chronic, accelerated, or blast phase Ph+ chronic myelogenous leukemia (CMS) with resistance or intolerance to prior therapy.

摘要翻译： 本主题涉及溶剂化物和博丝替尼的无定形形式; 溶剂化物即丙二醇溶剂合物和乙腈溶剂合物。 还提供了制备波生菌素的丙二醇溶剂化物，无定形形式和结晶乙腈溶剂合物的方法; 以及包含所述形式的组合物。 Bosutinib是一种3-喹啉腈激酶抑制剂，用于治疗慢性，加速或爆发期Ph +慢性粒细胞白血病（CMS）的成年患者，其具有耐药性或不耐受以前的治疗。