公开(公告)号：US20180155351A1

公开(公告)日：2018-06-07

申请号：US15886014

申请日：2018-02-01

申请人： Novartis AG ,  Astex Therapeutics Ltd.

发明人： Gilbert Besong ,  Christopher Thomas Brain ,  Clinton A. Brooks ,  Miles Stuart Congreve ,  Claudio Dagostin ,  Guo He ,  Ying Hou ,  Steven Howard ,  Yue Li ,  Yipin Lu ,  Paul Mortenson ,  Troy Smith ,  Moo Je Sung ,  Steven Woodhead ,  Wojciech Wrona ,  Bharat Lagu

IPC分类号： C07D487/04 ,  A61K31/519

CPC分类号： C07D487/04 ,  A61K31/519 ,  C07D487/08

摘要： The disclosed compounds relate to treatments and therapies for protein kinase-associated disorders. There is also a need for compounds useful in the treatment or prevention or amelioration of one or more symptoms of cancer, transplant rejections, and autoimmune diseases. Furthermore, there is a need for methods for modulating the activity of protein kinases, such as CDK1, CDK2, CDK4, CDK5, CDK6, CDK7, CDK8 and CDK9, using the compounds provided herein.

公开(公告)号：US08962630B2

公开(公告)日：2015-02-24

申请号：US13786955

申请日：2013-03-06

申请人： Novartis AG ,  Astex Therapeutics

发明人： Christopher Thomas Brain ,  Moo Je Sung ,  Bharat Lagu

IPC分类号： C07D487/04 ,  A61K31/519 ,  A61P35/00 ,  A61P35/04 ,  A61P35/02 ,  C07D487/08

CPC分类号： C07D487/04 ,  A61K31/519 ,  C07D487/08

摘要： The disclosed compounds relate to treatments and therapies for protein kinase-associated disorders. There is also a need for compounds useful in the treatment or prevention or amelioration of one or more symptoms of cancer, transplant rejections, and autoimmune diseases. Furthermore, there is a need for methods for modulating the activity of protein kinases, such as CDK1, CDK2, CDK4, CDK5, CDK6, CDK7, CDK8 and CDK9, using the compounds provided herein.

摘要翻译： 所公开的化合物涉及蛋白激酶相关病症的治疗和疗法。 还需要可用于治疗或预防或改善癌症，移植排斥和自身免疫性疾病的一种或多种症状的化合物。 此外，需要使用本文提供的化合物调节蛋白激酶如CDK1，CDK2，CDK4，CDK5，CDK6，CDK7，CDK8和CDK9的活性的方法。

公开(公告)号：US09409871B2

公开(公告)日：2016-08-09

申请号：US13905686

申请日：2013-05-30

申请人： NOVARTIS AG

发明人： Feng He ,  Stefan Peukert ,  Karen Marie Miller-Moslin ,  Naeem Yusuff ,  Zhuoliang Chen ,  Bharat Lagu

IPC分类号： C07D401/14 ,  C07D403/14 ,  C07D403/04 ,  C07D413/14 ,  A61K31/501 ,  A61K31/4523 ,  A61K31/4427 ,  C07D237/20 ,  C07D401/12 ,  C07D403/12 ,  C07D471/04 ,  C07D237/26 ,  A61P35/00

CPC分类号： C07D237/20 ,  A61K31/4427 ,  A61K31/4523 ,  A61K31/501 ,  C07D237/26 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D413/14 ,  C07D471/04

摘要： The present invention relates to compounds of formula I: in which L, W, X, Y, Z, m, p, R1, R2, R3, R4 and R7 are defined in the Summary of the Invention; capable of inhibiting the Hedgehog and Smo signaling pathway. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the diagnosis and treatment of pathologies relating to the Hedgehog and Smo signaling pathway, for example, tumor formation, cancer, neoplasia and non-malignant hyperproliferative disorders.

摘要翻译： 本发明涉及式I化合物：其中L，W，X，Y，Z，m，p，R 1，R 2，R 3，R 4和R 7在发明概述中定义; 能够抑制Hedgehog和Smo信号通路。 本发明还提供了制备本发明化合物的方法，包含这些化合物的药物制剂以及使用这些化合物和组合物诊断和治疗与Hedgehog和Smo信号传导途径有关的病理学的方法，例如肿瘤形成， 癌症，瘤形成和非恶性过度增生性疾病。