公开(公告)号：WO2011149874A3

公开(公告)日：2014-03-20

申请号：PCT/US2011037651

申请日：2011-05-24

Applicant: MERCK SHARP & DOHME ,  TSUI HON-CHUNG ,  PALIWAL SUNIL ,  KIM HYUNJIN M ,  KEREKES ANGELA D ,  CAPLEN MARY ANN ,  ESPOSITE SARA J ,  MCKITTRICK BRIAN A ,  FISCHMANN THIERRY OLIVIER ,  DOLL RONALD J ,  RAINKA MATTHEW PAUL ,  LI ANG

Inventor： TSUI HON-CHUNG ,  PALIWAL SUNIL ,  KIM HYUNJIN M ,  KEREKES ANGELA D ,  CAPLEN MARY ANN ,  ESPOSITE SARA J ,  MCKITTRICK BRIAN A ,  FISCHMANN THIERRY OLIVIER ,  DOLL RONALD J ,  RAINKA MATTHEW PAUL ,  LI ANG

IPC: A61K31/497

CPC classification number: A61K45/06 ,  A61K31/4178 ,  A61K31/437 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/4995 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/55 ,  A61K31/551 ,  A61K31/69 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D471/04 ,  C07D471/08 ,  C07D471/10 ,  C07D487/04 ,  C07D487/08 ,  C07D487/10 ,  C07D491/08 ,  C07D491/10 ,  C07D498/08 ,  A61K2300/00

Abstract: The present invention provides Imidazole Carboxamide Compounds of Formula (I): wherein D, T, R1, R2, R3, and R6 are as defined herein, and pharmaceutically acceptable salts of such Imidazole Carboxamide Compounds. The Imidazole Carboxamide Compounds are useful in the treatment of cancer and other aberrant conditions that result from overstimulation of the PDK-1 signaling pathway.

Abstract translation: 本发明提供式（I）的咪唑羧酰胺化合物：其中D，T，R 1，R 2，R 3和R 6如本文所定义，以及这些咪唑羧酰胺化合物的药学上可接受的盐。 咪唑羧酰胺化合物可用于治疗由过度刺激PDK-1信号通路引起的癌症和其他异常病症。

公开(公告)号：WO2011137219A1

公开(公告)日：2011-11-03

申请号：PCT/US2011/034275

申请日：2011-04-28

Applicant: SCHERING CORPORATION ,  PALIWAL, Sunil ,  TSUI, Hon-Chung ,  DOLL, Ronald, J. ,  LI, Ang ,  JIANG, May Xiaowu ,  RAINKA, Matthew Paul

Inventor： PALIWAL, Sunil ,  TSUI, Hon-Chung ,  DOLL, Ronald, J. ,  LI, Ang ,  JIANG, May Xiaowu ,  RAINKA, Matthew Paul

IPC: A61K31/33 ,  A61K31/385

CPC classification number: C07D417/04 ,  C07D417/14

Abstract: The instant invention provides for compounds that inhibit PDK1 activity. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting PDK1 activity by administering the compound to a patient in need of treatment of cancer.

Abstract translation: 本发明提供抑制PDK1活性的化合物。 本发明还提供了包含这种抑制化合物的组合物和通过将该化合物给予需要治疗癌症的患者来抑制PDK1活性的方法。

公开(公告)号：WO2009097233A9

公开(公告)日：2009-08-06

申请号：PCT/US2009/031972

申请日：2009-01-26

Applicant: SCHERING CORPORATION ,  ALBANY MOLECULAR RESEARCH, INC. ,  RAINKA, Matthew, Paul ,  VOSS, Matthew, Ernst ,  PETERSON, Lisa, Helen ,  FLEMING, Mike ,  BELANGER, David, B. ,  CURRAN, Patrick J. ,  KULKARNI, Bheemashankar, A. ,  YU, Tao ,  ZHANG, Yonglian ,  XIAO, Yushi ,  KEREKES, Angela, D. ,  TAGAT, Jayaram, R. ,  DOLL, Ronald J. ,  SIDDIQUI, M., Arshad

Inventor： RAINKA, Matthew, Paul ,  VOSS, Matthew, Ernst ,  PETERSON, Lisa, Helen ,  FLEMING, Mike ,  BELANGER, David, B. ,  CURRAN, Patrick J. ,  KULKARNI, Bheemashankar, A. ,  YU, Tao ,  ZHANG, Yonglian ,  XIAO, Yushi ,  KEREKES, Angela, D. ,  TAGAT, Jayaram, R. ,  DOLL, Ronald J. ,  SIDDIQUI, M., Arshad

IPC: C07D487/04 ,  A61P35/00 ,  A61K31/4985 ,  A61P29/00

Abstract: In its many embodiments, the present invention provides a novel class of imidazopyrazine compounds as inhibitors of protein and/or Aurora kinases, methods of preparing such compounds, pharmaceutical compositions including one or more such compounds, methods of preparing pharmaceutical formulations including one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the protein or Aurora kinases using such compounds or pharmaceutical compositions.

公开(公告)号：WO2011149874A2

公开(公告)日：2011-12-01

申请号：PCT/US2011/037651

申请日：2011-05-24

Applicant: SCHERING CORPORATION ,  TSUI, Hon-Chung ,  PALIWAL, Sunil ,  KIM, Hyunjin, M. ,  KEREKES, Angela, D. ,  CAPLEN, Mary Ann ,  ESPOSITE, Sara, J. ,  MCKITTRICK, Brian, A. ,  FISCHMANN, Thierry Olivier ,  DOLL, Ronald, J. ,  RAINKA, Matthew Paul ,  LI, Ang

Inventor： TSUI, Hon-Chung ,  PALIWAL, Sunil ,  KIM, Hyunjin, M. ,  KEREKES, Angela, D. ,  CAPLEN, Mary Ann ,  ESPOSITE, Sara, J. ,  MCKITTRICK, Brian, A. ,  FISCHMANN, Thierry Olivier ,  DOLL, Ronald, J. ,  RAINKA, Matthew Paul ,  LI, Ang

IPC: C07D403/02

CPC classification number: A61K45/06 ,  A61K31/4178 ,  A61K31/437 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/4995 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/55 ,  A61K31/551 ,  A61K31/69 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D471/04 ,  C07D471/08 ,  C07D471/10 ,  C07D487/04 ,  C07D487/08 ,  C07D487/10 ,  C07D491/08 ,  C07D491/10 ,  C07D498/08 ,  A61K2300/00

Abstract: The present invention provides Imidazole Carboxamide Compounds of Formula (I): wherein D, T, R 1 , R 2 , R 3 , and R 6 are as defined herein, and pharmaceutically acceptable salts of such Imidazole Carboxamide Compounds. The Imidazole Carboxamide Compounds are useful in the treatment of cancer and other aberrant conditions that result from overstimulation of the PDK-1 signaling pathway.

Abstract translation: 本发明提供式（I）的咪唑羧酰胺化合物：其中D，T，R 1，R 2，R 3和R 6如本文所定义，以及这些咪唑羧酰胺化合物的药学上可接受的盐。 咪唑羧酰胺化合物可用于治疗由过度刺激PDK-1信号通路引起的癌症和其他异常病症。

公开(公告)号：WO2009097233A1

公开(公告)日：2009-08-06

申请号：PCT/US2009031972

申请日：2009-01-26

Applicant: SCHERING CORP ,  ALBANY MOLECULAR RES INC ,  RAINKA MATTHEW PAUL ,  VOSS MATTHEW ERNST ,  PETERSON LISA HELEN ,  FLEMING MIKE ,  BELANGER DAVID B ,  CURRAN PATRICK J ,  KULKARNI BHEEMASHANKAR A ,  YU TAO ,  ZHANG YONGLIAN ,  XIAO YUSHI ,  KEREKES ANGELA D ,  TAGAT JAYARAM R ,  DOLL RONALD J ,  SIDDIQUI M ARSHAD

Inventor： RAINKA MATTHEW PAUL ,  VOSS MATTHEW ERNST ,  PETERSON LISA HELEN ,  FLEMING MIKE ,  BELANGER DAVID B ,  CURRAN PATRICK J ,  KULKARNI BHEEMASHANKAR A ,  YU TAO ,  ZHANG YONGLIAN ,  XIAO YUSHI ,  KEREKES ANGELA D ,  TAGAT JAYARAM R ,  DOLL RONALD J ,  SIDDIQUI M ARSHAD

IPC: C07D487/04 ,  A61K31/4985 ,  A61P29/00 ,  A61P35/00

CPC classification number: C07D487/04

Abstract: In its many embodiments, the present invention provides a novel class of imidazopyrazine compounds as inhibitors of protein and/or Aurora kinases, methods of preparing such compounds, pharmaceutical compositions including one or more such compounds, methods of preparing pharmaceutical formulations including one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the protein or Aurora kinases using such compounds or pharmaceutical compositions.