Invention Grant
US08399668B2 Process for the preparation of 5-(2-amino-pyrimidin-4-yl)-2-aryl-1H-pyrrole-3-carboxamides
有权
制备5-(2-氨基 - 嘧啶-4-基)-2-芳基-1H-吡咯-3-甲酰胺的方法
- Patent Title: Process for the preparation of 5-(2-amino-pyrimidin-4-yl)-2-aryl-1H-pyrrole-3-carboxamides
- Patent Title (中): 制备5-(2-氨基 - 嘧啶-4-基)-2-芳基-1H-吡咯-3-甲酰胺的方法
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Application No.: US12989518Application Date: 2009-04-30
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Publication No.: US08399668B2Publication Date: 2013-03-19
- Inventor: Matteo D'Anello , Carlo Battistini , Maria Gioia Fornaretto , Ermes Vanotti
- Applicant: Matteo D'Anello , Carlo Battistini , Maria Gioia Fornaretto , Ermes Vanotti
- Applicant Address: IT Nerviano (MI)
- Assignee: Nerviano Medical Sciences S. R. L.
- Current Assignee: Nerviano Medical Sciences S. R. L.
- Current Assignee Address: IT Nerviano (MI)
- Agency: Scully, Scott, Murphy & Presser, P.C.
- Priority: EP08155501 20080430
- International Application: PCT/EP2009/055262 WO 20090430
- International Announcement: WO2009/133170 WO 20091105
- Main IPC: C07D403/04
- IPC: C07D403/04

Abstract:
The present invention relates to a process for the preparation of 5-(2-amino-pyrimidin-4-yl)-2-aryl-1H-pyrrole-3-carboxamides and to the useful intermediate compounds of such process. 5-(2-Amino-pyrimidin-4-yl)-2-aryl-1H-pyrrole-3-carboxamides are described and claimed in WO2007110344, which also discloses processes for their preparation. These compounds can be advantageously prepared through a process which allows to obtain the desired products in high yields and purity and with a limited number of steps. The synthesis is starting from a cyano pyrrole derivative, and is characterized from the final hydrolysis of 5-(2-amino-pyrimidin-4-yl)-2-aryl-1H-pyrrole-3-carbonitrile. The compounds prepared according to the process of the present invention are endowed with protein kinase inhibiting activity and, more particularly, Cdc7 or Cdc7/Cdks inhibiting activity. The compounds are therefore useful in the treatment of a variety of cancers, cell proliferative disorders and diseases associated with protein kinases.
Public/Granted literature
- US20110040090A1 PROCESS FOR THE PREPARATION OF 5-(2-AMINO-PYRIMIDIN-4-YL)-2-ARYL-1H-PYRROLE-3-CARBOXAMIDES Public/Granted day:2011-02-17
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