公开(公告)号：US09630956B2

公开(公告)日：2017-04-25

申请号：US13106476

申请日：2011-05-12

申请人： Jean-Damien Charrier ,  Hayley Marie Binch ,  Dennis James Hurley ,  Thomas Cleveland ,  Pramod Joshi ,  Lev Tyler Dewey Fanning ,  Joanne Pinder ,  Michael O'Donnell ,  Anisa Nizarali Virani ,  Ronald Marcellus Alphonsus Knegtel ,  Steven John Durrant ,  Stephen Clinton Young ,  Pierre-Henri Storck ,  David Kay ,  Philip Michael Reaper ,  Matthew Paul Grote

发明人： Jean-Damien Charrier ,  Hayley Marie Binch ,  Dennis James Hurley ,  Thomas Cleveland ,  Pramod Joshi ,  Lev Tyler Dewey Fanning ,  Joanne Pinder ,  Michael O'Donnell ,  Anisa Nizarali Virani ,  Ronald Marcellus Alphonsus Knegtel ,  Steven John Durrant ,  Stephen Clinton Young ,  Pierre-Henri Storck ,  David Kay ,  Philip Michael Reaper ,  Matthew Paul Grote

IPC分类号： A61K31/497 ,  A61K33/24 ,  C07D413/14 ,  C07D401/14 ,  C07D241/10

CPC分类号： C07D413/14

摘要： The present invention relates to pyrazine and pyridine compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors.The compounds of this invention have formula I: wherein the variables are as defined herein.

公开(公告)号：US20120027874A1

公开(公告)日：2012-02-02

申请号：US13106476

申请日：2011-05-12

申请人： Jean-Damien Charrier ,  Hayley Marie Binch ,  Dennis James Hurley ,  Thomas Cleveland ,  Pramod Joshi ,  Lev Tyler Dewey Fanning ,  Joanne Pinder ,  Michael O'Donnell ,  Anisa Nizarali Virani ,  Ronald Marcellus Alphonsus Knegtel ,  Steven John Durrant ,  Stephen Clinton Young ,  Pierre-Henri Storck ,  David Kay ,  Philip Michael Reaper

发明人： Jean-Damien Charrier ,  Hayley Marie Binch ,  Dennis James Hurley ,  Thomas Cleveland ,  Pramod Joshi ,  Lev Tyler Dewey Fanning ,  Joanne Pinder ,  Michael O'Donnell ,  Anisa Nizarali Virani ,  Ronald Marcellus Alphonsus Knegtel ,  Steven John Durrant ,  Stephen Clinton Young ,  Pierre-Henri Storck ,  David Kay ,  Philip Michael Reaper

IPC分类号： A61K31/497 ,  A61K33/24 ,  A61P35/00 ,  C07D413/14

CPC分类号： C07D413/14

摘要： The present invention relates to pyrazine and pyridine compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors.The compounds of this invention have formula I: wherein the variables are as defined herein.

公开(公告)号：US08410112B2

公开(公告)日：2013-04-02

申请号：US13104291

申请日：2011-10-27

申请人： Jean-Damien Charrier ,  Steven John Durrant ,  David Kay ,  Michael O'Donnell ,  Ronald Marcellus Alphonsus Knegtel ,  Somhairle MacCormick ,  Joanne Pinder ,  Stephen Clinton Young ,  Hayley Marie Binch ,  Thomas Cleveland ,  Lev Tyler Dewey Fanning ,  Dennis James Hurley ,  Pramod Joshi ,  Urvi Jagdishbhai Sheth ,  Alina Silina ,  Philip Michael Reaper ,  Anisa Nizarali Virani

发明人： Jean-Damien Charrier ,  Steven John Durrant ,  David Kay ,  Michael O'Donnell ,  Ronald Marcellus Alphonsus Knegtel ,  Somhairle MacCormick ,  Joanne Pinder ,  Stephen Clinton Young ,  Hayley Marie Binch ,  Thomas Cleveland ,  Lev Tyler Dewey Fanning ,  Dennis James Hurley ,  Pramod Joshi ,  Urvi Jagdishbhai Sheth ,  Alina Silina ,  Philip Michael Reaper ,  Anisa Nizarali Virani

IPC分类号： A61K31/4965 ,  C07D403/00

CPC分类号： C07D403/14 ,  A61K31/497 ,  A61K31/541 ,  A61K31/551 ,  A61K45/06 ,  C07D241/28 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D405/04 ,  C07D405/14 ,  C07D409/04 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D487/10 ,  C07D491/113

摘要： The present disclosure relates to pyrazine compounds of formula I: wherein L, n, R1, and R2 are as described in the specification. These compounds are useful as inhibitors of ATR protein kinase. The disclosure also relates to pharmaceutically acceptable compositions comprising the compounds of the disclosure; methods of treating of various diseases, disorders, and conditions using the compounds of the disclosure; processes for preparing the compounds of the disclosure; intermediates for the preparation of the compounds of the disclosure; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors.

摘要翻译： 本公开涉及式I的吡嗪化合物：其中L，n，R 1和R 2如说明书中所述。 这些化合物可用作ATR蛋白激酶的抑制剂。 本公开还涉及包含本公开内容的化合物的药学上可接受的组合物; 使用本公开的化合物治疗各种疾病，病症和病症的方法; 制备本公开的化合物的方法; 用于制备本公开的化合物的中间体; 以及在体外应用中使用化合物的方法，如生物和病理现象中激酶的研究; 由这种激酶介导的细胞内信号转导途径的研究; 和新型激酶抑制剂的比较评估。

公开(公告)号：US20120040020A1

公开(公告)日：2012-02-16

申请号：US13104291

申请日：2011-10-27

申请人： Jean-Damien Charrier ,  Steven John Durrant ,  David Kay ,  Michael O'Donnell ,  Ronald Marcellus Alphonsus Knegtel ,  Somhairle MacCormick ,  Joanne Pinder ,  Stephen Clinton Young ,  Haley Marie Binch ,  Thomas Cleveland ,  Lev Tyler Dewey Fanning ,  Dennis James Hurley ,  Pramod Joshi ,  Urvi Jagdishbhai Sheth ,  Alina Silina ,  Philip Michael Reaper ,  Anisa Nizarali Virani

发明人： Jean-Damien Charrier ,  Steven John Durrant ,  David Kay ,  Michael O'Donnell ,  Ronald Marcellus Alphonsus Knegtel ,  Somhairle MacCormick ,  Joanne Pinder ,  Stephen Clinton Young ,  Haley Marie Binch ,  Thomas Cleveland ,  Lev Tyler Dewey Fanning ,  Dennis James Hurley ,  Pramod Joshi ,  Urvi Jagdishbhai Sheth ,  Alina Silina ,  Philip Michael Reaper ,  Anisa Nizarali Virani

IPC分类号： A61K33/24 ,  C07D401/14 ,  C07D413/14 ,  A61K31/551 ,  A61K31/497 ,  A61K31/5377 ,  C07D417/14 ,  A61K31/541 ,  C07D405/14 ,  C07D471/04 ,  C07D491/113 ,  A61K31/506 ,  C07D513/04 ,  C07D409/14 ,  C07D487/04 ,  A61K31/4985 ,  C07D487/10 ,  A61K38/16 ,  A61K31/704 ,  A61K31/675 ,  A61K31/7068 ,  A61K31/7072 ,  A61K31/706 ,  A61K38/12 ,  A61P17/06 ,  A61P35/00 ,  A61P31/18 ,  A61P1/16 ,  A61P31/20 ,  C07D403/14

CPC分类号： C07D403/14 ,  A61K31/497 ,  A61K31/541 ,  A61K31/551 ,  A61K45/06 ,  C07D241/28 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D405/04 ,  C07D405/14 ,  C07D409/04 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D487/10 ,  C07D491/113

摘要： The present disclosure relates to pyrazine compounds of formula I: wherein L, n, R1, and R2 are as described in the specification. These compounds are useful as inhibitors of ATR protein kinase. The disclosure also relates to pharmaceutically acceptable compositions comprising the compounds of the disclosure; methods of treating of various diseases, disorders, and conditions using the compounds of the disclosure; processes for preparing the compounds of the disclosure; intermediates for the preparation of the compounds of the disclosure; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors.

摘要翻译： 本公开涉及式I的吡嗪化合物：其中L，n，R 1和R 2如说明书中所述。 这些化合物可用作ATR蛋白激酶的抑制剂。 本公开还涉及包含本公开内容的化合物的药学上可接受的组合物; 使用本公开的化合物治疗各种疾病，病症和病症的方法; 制备本公开的化合物的方法; 用于制备本公开的化合物的中间体; 以及在体外应用中使用化合物的方法，如生物和病理现象中激酶的研究; 由这种激酶介导的细胞内信号转导途径的研究; 和新型激酶抑制剂的比较评估。

公开(公告)号：US08828996B2

公开(公告)日：2014-09-09

申请号：US13418737

申请日：2012-03-13

申请人： Sara Sabina Hadida-Ruah ,  Hayley Marie Binch ,  Michael Paul DeNinno ,  Lev Tyler Dewey Fanning ,  Bryan A. Frieman ,  Peter Diederik Jan Grootenhuis ,  Nicole Hilgraf ,  Pramod Joshi ,  Edward Adam Kallel ,  Mark Thomas Miller ,  Joseph Pontillo ,  Alina Silina ,  Urvi Jagdishbhai Sheth ,  Dennis James Hurley ,  Vijayalaksmi Arumugam

发明人： Sara Sabina Hadida-Ruah ,  Hayley Marie Binch ,  Michael Paul DeNinno ,  Lev Tyler Dewey Fanning ,  Bryan A. Frieman ,  Peter Diederik Jan Grootenhuis ,  Nicole Hilgraf ,  Pramod Joshi ,  Edward Adam Kallel ,  Mark Thomas Miller ,  Joseph Pontillo ,  Alina Silina ,  Urvi Jagdishbhai Sheth ,  Dennis James Hurley ,  Vijayalaksmi Arumugam

IPC分类号： C07D498/10 ,  A61K31/537

CPC分类号： C07D498/10

摘要： The invention relates to morpholine spirocyclic piperidine amide compounds useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.

摘要翻译： 本发明涉及可用作离子通道抑制剂的吗啉螺环哌啶酰胺化合物。 本发明还提供包含本发明化合物的药学上可接受的组合物和使用该组合物治疗各种疾病的方法。

公开(公告)号：US20120264749A1

公开(公告)日：2012-10-18

申请号：US13418737

申请日：2012-03-13

申请人： Sara Sabina Hadida-Ruah ,  Hayley Marie Binch ,  Michael Paul DeNinno ,  Lev Tyler Dewey Fanning ,  Bryan A. Frieman ,  Peter Diederik Jan Grootenhuis ,  Nicole Hilgraf ,  Pramod Joshi ,  Edward Adam Kallel ,  Mark Thomas Miller ,  Joseph Pontillo ,  Alina Silina ,  Urvi Jagdishbhai Sheth ,  Dennis James Hurley ,  Vijayalaksmi Arumugam

发明人： Sara Sabina Hadida-Ruah ,  Hayley Marie Binch ,  Michael Paul DeNinno ,  Lev Tyler Dewey Fanning ,  Bryan A. Frieman ,  Peter Diederik Jan Grootenhuis ,  Nicole Hilgraf ,  Pramod Joshi ,  Edward Adam Kallel ,  Mark Thomas Miller ,  Joseph Pontillo ,  Alina Silina ,  Urvi Jagdishbhai Sheth ,  Dennis James Hurley ,  Vijayalaksmi Arumugam

IPC分类号： A61K31/537 ,  A61K31/5377 ,  A61P25/00 ,  A61P19/02 ,  A61P25/06 ,  A61P25/08 ,  A61P25/28 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P9/06 ,  A61P25/14 ,  A61P1/00 ,  A61P9/12 ,  A61P29/00 ,  A61P1/18 ,  A61P13/10 ,  A61P13/08 ,  A61P17/04 ,  C12N5/071 ,  C07D498/10

CPC分类号： C07D498/10

摘要： The invention relates to morpholine spirocyclic piperidine amide compounds useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.

摘要翻译： 本发明涉及可用作离子通道抑制剂的吗啉螺环哌啶酰胺化合物。 本发明还提供包含本发明化合物的药学上可接受的组合物和使用该组合物治疗各种疾病的方法。

公开(公告)号：US20100160316A1

公开(公告)日：2010-06-24

申请号：US12714871

申请日：2010-03-01

申请人： Jesus E. Gonzalez, III ,  Dean M. Wilson ,  Andreas P. Termin ,  Peter D. J. Grootenhuis ,  Yulian Zhang ,  Benjamin J. Petzoldt ,  Lev Tyler Dewey Fanning ,  Timothy D. Neubert ,  Roger D. Tung ,  Esther Martinborough ,  Nicole Zimmerman

发明人： Jesus E. Gonzalez, III ,  Dean M. Wilson ,  Andreas P. Termin ,  Peter D. J. Grootenhuis ,  Yulian Zhang ,  Benjamin J. Petzoldt ,  Lev Tyler Dewey Fanning ,  Timothy D. Neubert ,  Roger D. Tung ,  Esther Martinborough ,  Nicole Zimmerman

IPC分类号： A61K31/5377 ,  C07D239/86 ,  A61K31/517 ,  C07D239/88 ,  C07D413/10 ,  A61K31/496 ,  A61P19/10 ,  A61P19/02 ,  A61P17/02 ,  A61P21/00 ,  A61P13/02 ,  A61P11/00 ,  C07D403/04

CPC分类号： C07D239/91 ,  C07D239/94 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/04 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04

摘要： The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels and calcium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.

公开(公告)号：US20130035310A1

公开(公告)日：2013-02-07

申请号：US13633478

申请日：2012-10-02

申请人： Esther Ann Martinborough ,  Lev Tyler Dewey Fanning ,  Urvi Jagdishbhai Sheth ,  Dean Mitchell Wilson ,  Andreas P. Termin ,  Timothy Donald Neubert ,  Nicole Hilgraf ,  Tara Leanne Hampton ,  Tara Whitney ,  Aarti Sameer Kawatkar ,  Danielle Lehsten ,  Dean Stamos ,  Jinglan Zhou ,  Vijayalaksmi Arumugam ,  Corey Anderson

发明人： Esther Ann Martinborough ,  Lev Tyler Dewey Fanning ,  Urvi Jagdishbhai Sheth ,  Dean Mitchell Wilson ,  Andreas P. Termin ,  Timothy Donald Neubert ,  Nicole Hilgraf ,  Tara Leanne Hampton ,  Tara Whitney ,  Aarti Sameer Kawatkar ,  Danielle Lehsten ,  Dean Stamos ,  Jinglan Zhou ,  Vijayalaksmi Arumugam ,  Corey Anderson

IPC分类号： A61K31/635 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/427 ,  A61K31/695 ,  A61P29/00 ,  A61P25/06 ,  A61P25/00 ,  A61P25/22 ,  A61P25/24 ,  A61P25/08 ,  A61P9/06 ,  A61P25/28 ,  A61P19/02 ,  A61P9/12 ,  A61P1/00 ,  A61K31/506

CPC分类号： C07D417/12 ,  C07D239/42 ,  C07D401/12 ,  C07D405/12 ,  C07D417/14 ,  C07D471/10 ,  C07D491/10

摘要： The present invention relates to piperidine and piperazine phenyl sulfonamides useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders, including for example the treatment of pain.

摘要翻译： 本发明涉及可用作离子通道抑制剂的哌啶和哌嗪苯基磺酰胺。 本发明还提供包含本发明化合物的药学上可接受的组合物和使用该组合物治疗各种疾病（包括例如治疗疼痛）的方法。

公开(公告)号：US07713983B2

公开(公告)日：2010-05-11

申请号：US10935008

申请日：2004-09-02

申请人： Jesus E. Gonzalez, III ,  Dean M. Wilson ,  Andreas P. Termin ,  Peter D. J. Grootenhuis ,  Yulian Zhang ,  Benjamin J. Petzoldt ,  Lev Tyler Dewey Fanning ,  Timothy D. Neubert ,  Roger D. Tung ,  Esther Martinborough ,  Nicole Zimmerman

发明人： Jesus E. Gonzalez, III ,  Dean M. Wilson ,  Andreas P. Termin ,  Peter D. J. Grootenhuis ,  Yulian Zhang ,  Benjamin J. Petzoldt ,  Lev Tyler Dewey Fanning ,  Timothy D. Neubert ,  Roger D. Tung ,  Esther Martinborough ,  Nicole Zimmerman

IPC分类号： C07D239/94 ,  C07D403/12 ,  A61K31/517 ,  A61P35/00

CPC分类号： C07D239/91 ,  C07D239/94 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/04 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04

摘要： The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels and calcium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.

摘要翻译： 本发明涉及可用作电压门控钠通道和钙通道抑制剂的化合物。 本发明还提供包含本发明化合物的药学上可接受的组合物和使用该组合物治疗各种疾病的方法。

公开(公告)号：US08309587B2

公开(公告)日：2012-11-13

申请号：US13419936

申请日：2012-03-14

申请人： Esther Ann Martinborough ,  Lev Tyler Dewey Fanning ,  Urvi Jagdishbhai Sheth ,  Dean Mitchell Wilson ,  Andreas P. Termin ,  Timothy Donald Neubert ,  Nicole Hilgraf ,  Tara Leanne Hampton ,  Tara Whitney ,  Aarti Sameer Kawatkar ,  Danielle Lehsten ,  Dean Stamos ,  Jinglan Zhou ,  Vijayalaksmi Arumugam ,  Corey Anderson

发明人： Esther Ann Martinborough ,  Lev Tyler Dewey Fanning ,  Urvi Jagdishbhai Sheth ,  Dean Mitchell Wilson ,  Andreas P. Termin ,  Timothy Donald Neubert ,  Nicole Hilgraf ,  Tara Leanne Hampton ,  Tara Whitney ,  Aarti Sameer Kawatkar ,  Danielle Lehsten ,  Dean Stamos ,  Jinglan Zhou ,  Vijayalaksmi Arumugam ,  Corey Anderson

IPC分类号： A01N43/78 ,  A61K31/425

CPC分类号： C07D417/12 ,  C07D239/42 ,  C07D401/12 ,  C07D405/12 ,  C07D417/14 ,  C07D471/10 ,  C07D491/10

摘要： The present invention relates to piperidine and piperazine phenyl sulfonamides useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders, including for example the treatment of pain.

摘要翻译： 本发明涉及可用作离子通道抑制剂的哌啶和哌嗪苯基磺酰胺。 本发明还提供包含本发明化合物的药学上可接受的组合物和使用该组合物治疗各种疾病（包括例如治疗疼痛）的方法。