- Structure-based design and synthesis of benzimidazole derivatives as dipeptidyl peptidase IV inhibitors
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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
- Wallace, Michael B.,Feng, Jun,Zhang, Zhiyuan,Skene, Robert J.,Shi, Lihong,Caster, Christopher L.,Kassel, Daniel B.,Xu, Rongda,Gwaltney II, Stephen L.
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p. 2362 - 2367
(2008/09/20)
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- INHIBITORS OF TYROSINE KINASES AND USES THEREOF
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Disclosed herein are compounds that inhibit the activity of particular tyrosine kinases. Methods for the preparation of such compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the compounds disclosed, alone or in combination with other therapeutic agents, for the treatment of tyrosine kinase-rnediated diseases or conditions or tyrosine, kinase-dependent diseases or conditions are provided.
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Page/Page column 106-107
(2008/06/13)
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- Optimization of 2-phenylaminoimidazo[4,5-h]isoquinolin-9-ones: Orally active inhibitors of lck kinase
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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
- 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
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p. 1337 - 1349
(2007/10/03)
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- Heterocyclic compounds useful as inhibitors of tyrosine kinases
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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
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- Isoquinolinone synthesis by SNAr reaction: A versatile route to imidazo[4,5-h]isoquinolin-9-ones
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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
- 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
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p. 7553 - 7556
(2007/10/03)
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- Heterocyclic compounds useful as inhibitors of tyrosine kinases
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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
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- Heterocyclic compounds useful as inhibitors of tyrosine kinases
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Disclosed are novel compounds of formula (I): wherein Ar1, X, Y, P, Q and Het are defined herein, which are useful as inhibitors of certain protein tyrosine kinases and are thus useful for treating diseases resulting from inappropriate cell proliferation, which include autoimmune diseases, chronic inflammatory diseases, allergic diseases, transplant rejection and cancer, as well as conditions resulting from cerebral ischemia, such as stroke. Also disclosed are pharmaceutical compositions comprising these compounds, processes for preparing these compounds and novel intermediate compounds useful in these processes.
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