公开(公告)号：US20110077252A1

公开(公告)日：2011-03-31

申请号：US12672485

申请日：2008-08-06

申请人： Sanjay Kumar ,  Kalpana Sanjay Joshi ,  Vijaykumar Deore ,  Mandar Ramesh Bhonde ,  Nilambari Nilkanth Yewalkar ,  Amol Arun Padgaonkar ,  Asha Adrian Kulkarni-Almeida ,  Maggie Joyce Rathos ,  Sapna Parikh ,  Nilesh Madhukar Dagia

发明人： Sanjay Kumar ,  Kalpana Sanjay Joshi ,  Vijaykumar Deore ,  Mandar Ramesh Bhonde ,  Nilambari Nilkanth Yewalkar ,  Amol Arun Padgaonkar ,  Asha Adrian Kulkarni-Almeida ,  Maggie Joyce Rathos ,  Sapna Parikh ,  Nilesh Madhukar Dagia

IPC分类号： A61K31/501 ,  C07D403/04 ,  C07D239/34 ,  A61K31/505 ,  A61P35/00 ,  A61P31/14 ,  A61P31/18 ,  A61P3/10 ,  A61P25/28 ,  A61P37/00 ,  A61P19/02 ,  A61P19/10

CPC分类号： C07D213/73 ,  C07D213/75 ,  C07D213/78 ,  C07D401/04 ,  C07D407/04 ,  C07D413/04

摘要： The present invention relates to pyridyl derivatives capable of inhibiting phosphatidylinositol-3-kinase (PI3k), mammalian target of rapamycin (mTOR) and/or hypoxia inducible factor 1α (HIF-1α) mediated signaling. Also disclosed are processes for preparation of the pyridyl derivatives, and their use in the manufacture of pharmaceutical compositions for the treatment of clinical conditions caused by deregulation of signaling pathways selected from one or more of PI3K, mTOR and HIF-1α pathways. The pyridyl derivatives are also useful for the treatment of conditions or disorders mediated by TNF-α.

摘要翻译： 本发明涉及能够抑制磷脂酰肌醇-3-激酶（PI3k），雷帕霉素哺乳动物靶（mTOR）和/或缺氧诱导因子1α（HIF-1α）介导信号传导的吡啶衍生物。 还公开了制备吡啶基衍生物的方法及其在制备用于治疗由选自PI3K，mTOR和HIF-1α途径中的一种或多种的信号传导途径失调引起的临床病症的药物组合物中的用途。 吡啶基衍生物也可用于治疗由TNF-α介导的病症或病症。

公开(公告)号：US08314103B2

公开(公告)日：2012-11-20

申请号：US12672485

申请日：2008-08-06

申请人： Sanjay Kumar ,  Kalpana Sanjay Joshi ,  Vijaykumar Deore ,  Mandar Ramesh Bhonde ,  Nilambari Nilkanth Yewalkar ,  Amol Arun Padgaonkar ,  Asha Adrian Kulkarni-Almeida ,  Maggie Joyce Rathos ,  Sapna Parikh ,  Nilesh Madhukar Dagia

发明人： Sanjay Kumar ,  Kalpana Sanjay Joshi ,  Vijaykumar Deore ,  Mandar Ramesh Bhonde ,  Nilambari Nilkanth Yewalkar ,  Amol Arun Padgaonkar ,  Asha Adrian Kulkarni-Almeida ,  Maggie Joyce Rathos ,  Sapna Parikh ,  Nilesh Madhukar Dagia

IPC分类号： A61K31/50 ,  C07D401/00

CPC分类号： C07D213/73 ,  C07D213/75 ,  C07D213/78 ,  C07D401/04 ,  C07D407/04 ,  C07D413/04

摘要： The present invention relates to pyridyl derivatives capable of inhibiting phosphatidylinositol-3-kinase (PI3k), mammalian target of rapamycin (mTOR) and/or hypoxia inducible factor 1α (HIF-1α) mediated signaling. Also disclosed are processes for preparation of the pyridyl derivatives, and their use in the manufacture of pharmaceutical compositions for the treatment of clinical conditions caused by deregulation of signaling pathways selected from one or more of PI3K, mTOR and HIF-1α pathways. The pyridyl derivatives are also useful for the treatment of conditions or disorders mediated by TNF-α.

摘要翻译： 本发明涉及能够抑制磷脂酰肌醇-3-激酶（PI3k），雷帕霉素哺乳动物靶（mTOR）和/或缺氧诱导因子1α（HIF-1α）介导信号传导的吡啶衍生物。 还公开了制备吡啶基衍生物的方法及其在制备用于治疗由选自PI3K，mTOR和HIF-1α途径中的一种或多种的信号传导途径失调引起的临床病症的药物组合物中的用途。 吡啶基衍生物也可用于治疗由TNF-α介导的病症或病症。