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：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：US20100311748A1

公开(公告)日：2010-12-09

申请号：US12675728

申请日：2008-08-29

申请人： Leslie Dakin ,  Benjamin Fauber ,  Alexander Hird ,  James Janetka ,  Daniel John Russell ,  Qibin Su ,  Bin Yang ,  Xiaolan Zheng

发明人： Leslie Dakin ,  Benjamin Fauber ,  Alexander Hird ,  James Janetka ,  Daniel John Russell ,  Qibin Su ,  Bin Yang ,  Xiaolan Zheng

IPC分类号： A61K31/5377 ,  C07D401/12 ,  A61K31/4439 ,  C07D417/14 ,  A61K31/496 ,  C07D513/04 ,  A61K31/444 ,  A61K31/497 ,  A61K31/501 ,  C07D233/64 ,  A61K31/4164 ,  A61P35/00

CPC分类号： C07D401/12 ,  C07D213/30 ,  C07D213/40 ,  C07D213/73 ,  C07D233/61 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D473/00 ,  C07D513/04

摘要： The present disclosure relates to heterocyclic amide compounds, which are useful for inhibiting the Hedgehog pathway, and their use in treating a disease or medical condition mediated alone or in part by Hedgehog pathway inhibition. Also disclosed are methods for manufacture of these compounds, pharmaceutical compositions including these compounds, and use of these compounds in the manufacture of medicaments for treating such diseases and medical conditions in a subject. Formula (IA) with the provisio that either R2 or R3 is (Z).

摘要翻译： 本公开涉及可用于抑制Hedgehog途径的杂环酰胺化合物及其用于治疗单独或部分由Hedgehog通路抑制介导的疾病或医学病症的用途。 还公开了制备这些化合物的方法，包括这些化合物的药物组合物，以及这些化合物在制备用于治疗受试者的这些疾病和医疗状况的药物中的用途。 式（IA），条件是R2或R3为（Z）。

公开(公告)号：US08901307B2

公开(公告)日：2014-12-02

申请号：US13000138

申请日：2009-07-02

申请人： Leslie Dakin ,  James Edward Dowling ,  Michelle Lamb ,  Jon Read ,  Xiaolan Zheng

发明人： Leslie Dakin ,  James Edward Dowling ,  Michelle Lamb ,  Jon Read ,  Xiaolan Zheng

IPC分类号： C07D417/10 ,  A61K31/454 ,  C07D417/14 ,  A61K31/427 ,  C07D277/34 ,  C07D417/06 ,  A61K31/426

CPC分类号： C07D417/10 ,  A61K31/426 ,  A61K31/427 ,  C07D277/34 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14

摘要： The invention relates to chemical compounds of formula (I), and salts thereof. In some embodiments, the invention relates to inhibitors or modulators of PIM-1 and/or PIM-2, and/or PIM-3 protein kinase activity or enzyme function. In still further embodiments, the invention relates to pharmaceutical compositions comprising compounds disclosed herein, and their use in the prevention and treatment of PIM kinase related conditions and diseases, preferably cancer.

摘要翻译： 本发明涉及式（I）化合物及其盐。 在一些实施方案中，本发明涉及PIM-1和/或PIM-2和/或PIM-3蛋白激酶活性或酶功能的抑制剂或调节剂。 在另外的实施方案中，本发明涉及包含本文公开的化合物的药物组合物及其在预防和治疗PIM激酶相关病症和疾病，优选癌症中的用途。

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：US20110218182A1

公开(公告)日：2011-09-08

申请号：US13000138

申请日：2009-07-02

申请人： Leslie Dakin ,  James Edward Dowling ,  Michelle Lamb ,  Jon Read ,  Qibin Su ,  Xiaolan Zheng

发明人： Leslie Dakin ,  James Edward Dowling ,  Michelle Lamb ,  Jon Read ,  Qibin Su ,  Xiaolan Zheng

IPC分类号： A61K31/427 ,  C07D417/10 ,  A61K31/454 ,  C12N9/99 ,  A61P35/00 ,  A61K31/551 ,  A61K31/496 ,  C07D417/14 ,  A61K31/5377 ,  A61K31/541

CPC分类号： C07D417/10 ,  A61K31/426 ,  A61K31/427 ,  C07D277/34 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14

摘要： The invention relates to chemical compounds of formula (I), and salts thereof. In some embodiments, the invention relates to inhibitors or modulators of PIM-1 and/or PIM-2, and/or PIM-3 protein kinase activity or enzyme function. In still further embodiments, the invention relates to pharmaceutical compositions comprising compounds disclosed herein, and their use in the prevention and treatment of PIM kinase related conditions and diseases, preferably cancer.

摘要翻译： 本发明涉及式（I）化合物及其盐。 在一些实施方案中，本发明涉及PIM-1和/或PIM-2和/或PIM-3蛋白激酶活性或酶功能的抑制剂或调节剂。 在另外的实施方案中，本发明涉及包含本文公开的化合物的药物组合物及其在预防和治疗PIM激酶相关病症和疾病，优选癌症中的用途。

公开(公告)号：US20090270450A1

公开(公告)日：2009-10-29

申请号：US12435856

申请日：2009-05-05

申请人： Leslie Dakin ,  Kevin Daly ,  David Del Valle ,  Thomas Gero ,  Claude Afona Ogoe ,  David Scott ,  Xiaolan Zheng

发明人： Leslie Dakin ,  Kevin Daly ,  David Del Valle ,  Thomas Gero ,  Claude Afona Ogoe ,  David Scott ,  Xiaolan Zheng

IPC分类号： A61K31/47 ,  C07D215/44

CPC分类号： C07D215/54 ,  C07D401/04

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：US20090012084A1

公开(公告)日：2009-01-08

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： A61K31/502 ,  C07D237/28 ,  A61K31/5377 ,  A61P35/00 ,  C07D413/02

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。