Dinaciclib - zliming2004 - zliming2004的博客

 CDK5/p25 Inhibitors CDK1/Cyclin B Inhibitors
CDK9/Cyclin T1 Inhibitors
CDK2/Cyclin A Inhibitors

SCH-727965 is an apoptosis inducer currently in phase III clinical trials at Merck & Co. for the treatment of refractory chronic lymphocytic leukemia. Phase II clinical trials at Merck & Co. for the treatment of advanced breast cancer, non-small cell lung cancer (NSCLC), acute lymphocytic leukemia, acute myeloid leukemia and for the treatment of mantle cell lymphoma. The National Cancer Institute is also investigating the drug candidate in early clinical trials for the treatment of stage IV melanoma and for the treatment of relapsed or refractory multiple myeloma.

The compound is a novel pyrazolo (1,5-a) pyrimidine which potently and selectively inhibits the cyclin-dependent kinases CDK1, CDK2, CDK5 and CDK9. Inhibition of CDK2/CDK1 in tumor cells leads to cell cycle arrest and apoptosis. To date, SCH-727965 demonstrated activity against a broad panel of tumor cell lines including breast, small cell and non-small cell lung, colon and prostate cancers.

In 2011, orphan drug designation was assigned in the U.S. for the treatment of chronic lymphocytic leukemia.

Phase Organization ConditionPhase IIIMerck & Co.Leukemia, chronic lymphocyticPhase IINational Cancer Institute (NCI)Melanoma, metastaticPhase IINational Cancer Institute (NCI)Multiple myeloma

Dinaciclib - zliming2004 - zliming2004的博客


Patent NumberApplicantTitleConditionSubject MatterUS 2004209878
US 7119200
JP 2007522220
WO 2005077954
EP 1720882
JP 2010215675
 Schering Corp.  Pyrazolopyrimidine-derivatives as cyclin dependent kinase inhibitorsDinaciclib - zliming2004 - zliming2004的博客  


Dinaciclib - zliming2004 - zliming2004的博客  Drug Substances
 EP 2051963
JP 2010501487
US 7786306
WO 2008021509
US 2008051579
  Schering Corp.   Process for resolving chiral piperidine alcohol and process for synthesis of pyrazolo[1,5-a]pyrimidine derivatives using sameDinaciclib - zliming2004 - zliming2004的博客  


Dinaciclib - zliming2004 - zliming2004的博客  Processes
 US 2008058518
EP 2057166
JP 2010502607
US 8076479
WO 2008027220
  Schering Corp.   Process and intermediates for the synthesis of (3-alkyl-5-piperidin-1-yl-3,3a-dihydro-pyrazolo[1,5-a]pyrimidin-7-yl)-amino derivativesDinaciclib - zliming2004 - zliming2004的博客  


Dinaciclib - zliming2004 - zliming2004的博客  Synthesis