333459-71-5Relevant academic research and scientific papers
Structure-based design and synthesis of benzimidazole derivatives as dipeptidyl peptidase IV inhibitors
Wallace, Michael B.,Feng, Jun,Zhang, Zhiyuan,Skene, Robert J.,Shi, Lihong,Caster, Christopher L.,Kassel, Daniel B.,Xu, Rongda,Gwaltney II, Stephen L.
, p. 2362 - 2367 (2008/09/20)
A novel series of non-covalent, benzimidazole-based inhibitors of DPP-4 has been developed from a small fragment hit using structure-based drug design. A highly versatile synthetic route was created for the development of SAR, which led to the discovery o
NOVEL SUBSTITUTED BENZIMIDAZOLE DERIVATIVES
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Page 19, (2010/02/09)
The invention provides a compound of Formula I (I) wherein n is 1 or 2; R1 is selected from hydrogen, halogen, CN, COOR6, CONR6R7 or CH2OR6; R2 is selected from hydrogen, halogen
Optimization of 2-phenylaminoimidazo[4,5-h]isoquinolin-9-ones: Orally active inhibitors of lck kinase
Goldberg, Daniel R.,Butz, Tanja,Cardozo, Mario G.,Eckner, Robert J.,Hammach, Abdelhakim,Huang, Jessica,Jakes, Scott,Kapadia, Suresh,Kashem, Mohammed,Lukas, Susan,Morwick, Tina M.,Panzenbeck, Maret,Patel, Usha,Pav, Susan,Peet, Gregory W.,Peterson, Jeffrey D.,Prokopowicz III, Anthony S.,Snow, Roger J.,Sellati, Rosemarie,Takahashi, Hidenori,Tan, Jonathan,Tschantz, Matt A.,Wang, Xiao-Jun,Wang, Yong,Wolak, John,Xiong, Pla,Moss, Neil
, p. 1337 - 1349 (2007/10/03)
The tyrosine kinase p56lck (lck) is essential for T cell activation; thus, inhibitors of lck have potential utility as autoimmune agents. Our initial disclosure of a new class of lck inhibitors based on the phenylaminoimidazoisoquinolin-9-one showed reaso
Heterocyclic compounds useful as inhibitors of tyrosine kinases
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, (2008/06/13)
Disclosed are novel compounds of formula (I): wherein Ar1, Ra, R4, R5, X and Y are defined below, which are useful as inhibitors of certain protein tyrosine kinases and are thus useful for treating diseases asso
Isoquinolinone synthesis by SNAr reaction: A versatile route to imidazo[4,5-h]isoquinolin-9-ones
Snow, Roger J.,Butz, Tanja,Hammach, Abdelhakim,Kapadia, Suresh,Morwick, Tina M.,Prokopowicz III, Anthony S.,Takahashi, Hidenori,Tan, Jonathan D.,Tschantz, Matt A.,Wang, Xiao-Jun
, p. 7553 - 7556 (2007/10/03)
Reaction of 2-chlorobenzonitriles with β-ketoesters in an SNAr reaction, followed by cyclization in acid provides a versatile route to isoquinolones. Starting from 2,6-dichloro-3-nitrobenzonitrile 7, sequential displacement of the chlorines by
Heterocyclic compounds useful as inhibitors of tyrosine kinases
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, (2008/06/13)
Disclosed are novel compounds of formula (I): wherein Ar1, Ra, R4, R5, X and Y are defined below, which are useful as inhibitors of certain protein tyrosine kinases and are thus useful for treating diseases asso
