公开(公告)号：US07723337B2

公开(公告)日：2010-05-25

申请号：US12210588

申请日：2008-09-15

申请人： Leslie Dakin ,  Claude Afona Ogoe ,  David Scott ,  XiaoLan Zheng

发明人： Leslie Dakin ,  Claude Afona Ogoe ,  David Scott ,  XiaoLan Zheng

IPC分类号： A01N43/58 ,  A01N43/60 ,  A61K31/50 ,  A61K31/495 ,  A61K31/4965 ,  C07D237/26 ,  C07D487/00 ,  C07D237/28 ,  C07D241/04 ,  C07D295/00

CPC分类号： C07D237/28

摘要： The invention relates to chemical compounds of formula (I): or pharmaceutically acceptable salts thereof which possess CSF-1R kinase inhibitory activity and are accordingly useful for their anti-cancer activity and thus in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments of use in the production of an anti-cancer effect in a warm-blooded animal such as man.

摘要翻译： 本发明涉及具有CSF-1R激酶抑制活性的式（I）化合物或其药学上可接受的盐，因此可用于其抗癌活性，因此可用于治疗人或动物体的方法。 本发明还涉及制备所述化合物的方法，含有它们的药物组合物及其在制造用于在温血动物如人中产生抗癌作用的药物中的用途。

公开(公告)号：US20090054411A1

公开(公告)日：2009-02-26

申请号：US12250314

申请日：2008-10-13

申请人： Donald Cook ,  Leslie Dakin ,  David Del Valle ,  Thomas Gero ,  David Scott ,  Xiaolan Zheng

发明人： Donald Cook ,  Leslie Dakin ,  David Del Valle ,  Thomas Gero ,  David Scott ,  Xiaolan Zheng

IPC分类号： A61K31/496 ,  C07D401/04 ,  A61K31/5377 ,  A61P35/00 ,  A61K31/551 ,  C07D413/04

CPC分类号： C07D215/54 ,  C07D401/04

摘要： The invention relates to chemical compounds of formula IA or IB: or pharmaceutically acceptable salts thereof which possess CSF-1R kinase inhibitory activity and are accordingly useful for their anti-cancer activity and thus in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments of use in the production of an anti-cancer effect in a warm-blooded animal such as man.

摘要翻译： 本发明涉及具有CSF-1R激酶抑制活性的式IA或IB化学化合物或其药学上可接受的盐，因此可用于其抗癌活性，因此可用于治疗人或动物体的方法。 本发明还涉及制备所述化合物的方法，含有它们的药物组合物及其在制造用于在温血动物如人中产生抗癌作用的药物中的用途。

公开(公告)号：US20110098283A1

公开(公告)日：2011-04-28

申请号：US12781277

申请日：2010-05-17

申请人： Leslie Dakin ,  Claude Afona Ogoe ,  David Scott ,  XiaoLan Zheng

发明人： Leslie Dakin ,  Claude Afona Ogoe ,  David Scott ,  XiaoLan Zheng

IPC分类号： A61K31/502 ,  C07D237/28 ,  C07D401/10 ,  C07D403/10 ,  C07D413/10 ,  A61K31/55 ,  A61K31/5377 ,  A61P35/00 ,  C12N9/99

CPC分类号： C07D237/28

摘要： The invention relates to chemical compounds of formula (I): or pharmaceutically acceptable salts thereof which possess CSF-1R kinase inhibitory activity and are accordingly useful for their anti-cancer activity and thus in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments of use in the production of an anti-cancer effect in a warm-blooded animal such as man.

摘要翻译： 本发明涉及具有CSF-1R激酶抑制活性的式（I）化合物或其药学上可接受的盐，因此可用于其抗癌活性，因此可用于治疗人或动物体的方法。 本发明还涉及制备所述化合物的方法，含有它们的药物组合物及其在制造用于在温血动物如人中产生抗癌作用的药物中的用途。

公开(公告)号：US20090118261A1

公开(公告)日：2009-05-07

申请号：US11574031

申请日：2005-08-26

申请人： Brian Aquila ,  Leslie Dakin ,  Jayachandran Ezhuthachan ,  Stephen Lee ,  Paul Lyne ,  Timothy Pontz ,  XiaoLan Zheng

发明人： Brian Aquila ,  Leslie Dakin ,  Jayachandran Ezhuthachan ,  Stephen Lee ,  Paul Lyne ,  Timothy Pontz ,  XiaoLan Zheng

IPC分类号： A61K31/55 ,  C07D239/72 ,  A61K31/517 ,  C07D413/02 ,  A61K31/5377 ,  A61P35/00 ,  C07D471/02 ,  A61K31/519 ,  A61K31/496 ,  C07D403/02

CPC分类号： C07D471/04 ,  C07D239/90 ,  C07D401/12 ,  C07D403/12 ,  C07D405/06 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12

摘要： The invention relates to chemical compounds of the formula (I): or pharmaceutically acceptable salts thereof, which possess B Raf inhibitory activity and are accordingly useful for their anti cancer activity and thus in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments of use in the production of an anti-cancer effect in a warm blooded animal such as man.

摘要翻译： 本发明涉及具有B Raf抑制活性的式（I）化合物或其药学上可接受的盐，因此可用于其抗癌活性，因此可用于治疗人或动物体的方法。 本发明还涉及制备所述化合物的方法，含有它们的药物组合物及其在制备用于在温血动物如人中产生抗癌作用的药物中的用途。

公开(公告)号：US07498333B2

公开(公告)日：2009-03-03

申请号：US11207128

申请日：2005-08-18

申请人： Brian Aquila ,  Michael Howard Block ,  Audrey Davies ,  Jayachandran Ezhuthachan ,  Sandra Ann Filla ,  Timothy Pontz ,  Daniel John Russell ,  Maria-Elena Theoclitou ,  XiaoLan Zheng

发明人： Brian Aquila ,  Michael Howard Block ,  Audrey Davies ,  Jayachandran Ezhuthachan ,  Sandra Ann Filla ,  Timothy Pontz ,  Daniel John Russell ,  Maria-Elena Theoclitou ,  XiaoLan Zheng

IPC分类号： C07D498/04 ,  A61K31/505

CPC分类号： C07D498/04 ,  C07D513/04

摘要： This invention relates to novel compounds having the structural formula (I) and to their pharmaceutical compositions and to their methods of use. These novel compounds provide a treatment or prophylaxis of cancer.

摘要翻译： 本发明涉及具有结构式（I）的新化合物及其药物组合物及其使用方法。 这些新化合物提供癌症的治疗或预防。

公开(公告)号：US20080312206A1

公开(公告)日：2008-12-18

申请号：US12097652

申请日：2006-12-19

申请人： Brian Aquila ,  Donald Cook ,  Leslie Dakin ,  Stephanos Ioannidis ,  Paul Lyne ,  David Scott ,  Xiaolan Zheng

发明人： Brian Aquila ,  Donald Cook ,  Leslie Dakin ,  Stephanos Ioannidis ,  Paul Lyne ,  David Scott ,  Xiaolan Zheng

IPC分类号： A61K31/427 ,  C07D277/46 ,  A61K31/426 ,  A61P35/00 ,  C07D417/02

CPC分类号： C07D277/46 ,  C07D417/12

摘要： The invention relates to chemical compounds, or pharmaceutically acceptable salts thereof of the formula which possess CSF 1R kinase inhibitory activity and are accordingly useful for their anti cancer activity and thus in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments of use in the production of an anti-cancer effect in a warm blooded animal such as man.

摘要翻译： 本发明涉及具有CSF 1R激酶抑制活性的化学化合物或其药学上可接受的盐，其具有CSF 1R激酶抑制活性，因此可用于其抗癌活性，因此可用于治疗人或动物体的方法。 本发明还涉及制备所述化合物的方法，含有它们的药物组合物及其在制备用于在温血动物如人中产生抗癌作用的药物中的用途。

公开(公告)号：US20080306096A1

公开(公告)日：2008-12-11

申请号：US12097965

申请日：2006-12-19

申请人： Brian Aquila ,  Jayachandran Ezhuthachan ,  Paul Lyne ,  Timothy Pontz ,  Xiaolan Zheng

发明人： Brian Aquila ,  Jayachandran Ezhuthachan ,  Paul Lyne ,  Timothy Pontz ,  Xiaolan Zheng

IPC分类号： A61K31/517 ,  A61P35/00 ,  C07D239/94 ,  C07D403/12 ,  C07D405/02 ,  C07D409/02 ,  C07D401/02

CPC分类号： C07D239/94 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12

摘要： The invention relates to chemical compounds of the formula (I) or pharmaceutically acceptable salts thereof, which possess B Raf inhibitory activity and are accordingly useful for their anti cancer activity and thus in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments of use in the production of an anti-cancer effect in a warm blooded animal such as man.

摘要翻译： 本发明涉及具有B Raf抑制活性的式（I）化合物或其药学上可接受的盐，因此可用于其抗癌活性，因此可用于治疗人或动物体的方法。 本发明还涉及制备所述化合物的方法，含有它们的药物组合物及其在制备用于在温血动物如人中产生抗癌作用的药物中的用途。

公开(公告)号：US20070249636A1

公开(公告)日：2007-10-25

申请号：US11573671

申请日：2005-08-16

申请人： Brian Aquila ,  Michael Block ,  Audrey Davies ,  Jayachandran Ezhuthachan ,  Timothy Pontz ,  Daniel Russell ,  Marie-Elena Theoclitou ,  XiaoLan Zheng

发明人： Brian Aquila ,  Michael Block ,  Audrey Davies ,  Jayachandran Ezhuthachan ,  Timothy Pontz ,  Daniel Russell ,  Marie-Elena Theoclitou ,  XiaoLan Zheng

IPC分类号： A61K31/519 ,  A61P35/00 ,  C07D239/00 ,  C07D261/00 ,  C07D275/00 ,  C07D487/14 ,  C07D498/04 ,  C07D513/04

CPC分类号： C07D513/04

摘要： This invention relates to novel compounds having the structural formula (I) and to their pharmaceutical compositions and to their methods of use. These novel compounds provide a treatment or prophylaxis of cancer.

摘要翻译： 本发明涉及具有结构式（I）的新化合物及其药物组合物及其使用方法。 这些新化合物提供癌症的治疗或预防。

公开(公告)号：US20060063751A1

公开(公告)日：2006-03-23

申请号：US11207089

申请日：2005-08-18

申请人： Brian Aquila ,  Michael Block ,  Audrey Davies ,  Jayachandran Ezhuthachan ,  Sandra Filla ,  Richard Luke ,  Timothy Pontz ,  Daniel Russell ,  Maria-Elena Theoclitou ,  XiaoLan Zheng

发明人： Brian Aquila ,  Michael Block ,  Audrey Davies ,  Jayachandran Ezhuthachan ,  Sandra Filla ,  Richard Luke ,  Timothy Pontz ,  Daniel Russell ,  Maria-Elena Theoclitou ,  XiaoLan Zheng

IPC分类号： A61K31/513 ,  C07D417/02 ,  C07D413/02 ,  C07D403/02

CPC分类号： C07D513/04

摘要： This invention relates to novel compounds having the formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8 and R9 are as defined in the specification and to their pharmaceutical compositions and to their methods of use. These novel compounds provide a treatment or prophylaxis of cancer.

摘要翻译： 本发明涉及具有式（I）的新化合物，

公开(公告)号：US20060041128A1

公开(公告)日：2006-02-23

申请号：US11206888

申请日：2005-08-18

申请人： Brian Aquila ,  Michael Block ,  Audrey Davies ,  Jayachandran Ezhuthachan ,  Timothy Pontz ,  Daniel Russell ,  Maria-Elena Theoclitou ,  XiaoLan Zheng

发明人： Brian Aquila ,  Michael Block ,  Audrey Davies ,  Jayachandran Ezhuthachan ,  Timothy Pontz ,  Daniel Russell ,  Maria-Elena Theoclitou ,  XiaoLan Zheng

IPC分类号： A61K31/519 ,  C07D498/02 ,  C07D491/02

CPC分类号： C07D513/04

摘要： This invention relates to novel compounds having the structural formula (I) and to their pharmaceutical compositions and to their methods of use. These novel compounds provide a treatment or prophylaxis of cancer.

摘要翻译： 本发明涉及具有结构式（I）的新化合物及其药物组合物及其使用方法。 这些新化合物提供癌症的治疗或预防。