Heteroaryl-linked 5-(1H-benzimidazol-1-yl)-2-thiophenecarboxamides: Potent inhibitors of polo-like kinase 1 (PLK1) with improved drug-like properties
Potent inhibitors of PLK1 with acceptable solubility, mouse iv clearance, and reduced CYP450 inhibition were identified. Drug-like properties were improved using a heteroaryl ring as a functional handle for manipulation of inhibitors' physiochemical and DMPK properties.
Rheault, Tara R.,Donaldson, Kelly H.,Badiang-Alberti, Jennifer G.,Davis-Ward, Ronda G.,Andrews, C. Webb,Bambal, Ramesh,Jackson, Jeffrey R.,Cheung, Mui
scheme or table
p. 4587 - 4592
(2010/10/02)
5- AND 6- SUBSTITUTED BENZIMIDAZOLE THIOPHENE COMPOUNDS
The present invention provides 5- and 6-substituted benzimidazole thiophene compounds pharmaceutical compositions containing the same, processes for preparing the same and their use as pharmaceutical agents.
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Page/Page column 34-35
(2010/04/23)
BENZIMIDAZOLE THIOPHENE COMPOUNDS AS PLK MODULATORS
The present invention provides 5-heteroaryl substituted benzimidazole thiophene compounds pharmaceutical compositions containing the same, processes for preparing the same and their use as pharmaceutical agents.
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Page/Page column 82
(2008/06/13)
REGIOSELECTIVE PROCESS FOR PREPARING BENZIMIDAZOLE THIOPHENES
The present invention provides a process for preparing benzimidazole thiophene compounds of formula I. Intermediates used in the process are also claimed.
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Page/Page column 82
(2010/11/26)
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