- PYRIDINE DERIVATIVES USEFUL AS GLUCOKINASE ACTIVATORS
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Novel heterocyclic compounds of the formula (I) in which R1, R2, R3, R4 and D have the meanings indicated in Claim 1, are activators of glucokinase and can be used for the prevention and/o treatment of Diabetes Typ 1 and 2, obesity, neuropathy and/or nephropathy.
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Page/Page column 58
(2009/05/30)
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- Identification of 2-amino-5-(thioaryl)thiazoles as inhibitors of nerve growth factor receptor TrkA
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2-Amino-5-(thioaryl)thiazoles are potent inhibitors of TrkA (e.g., 20h, TrkA IC50 = 0.6 nM) that show anti-proliferative effect in cellular assays. A proposed inhibitor binding mode to TrkA active site is consistent with key SAR observations.
- Kim, Soong-Hoon,Tokarski, John S.,Leavitt, Kenneth J.,Fink, Brian E.,Salvati, Mark E.,Moquin, Robert,Obermeier, Mary T.,Trainor, George L.,Vite, Gregory G.,Stadnick, Linda K.,Lippy, Jonathan S.,You, Dan,Lorenzi, Matthew V.,Chen, Ping
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p. 634 - 639
(2008/09/18)
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- Synthesis and biological activity of N-aryl-2-aminothiazoles: Potent pan inhibitors of cyclin-dependent kinases
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N-Aryl aminothiazoles 6-9 were prepared from 2-bromothiazole 5 and found to be CDK inhibitors. In cells they act as potent cytotoxic agents. Selectivity for CDK1, CDK2, and CDK4 was dependent of the nature of the N-aryl group and distinct from the CDK2 se
- Misra, Raj N.,Xiao, Hai-Yun,Williams, David K.,Kim, Kyoung S.,Lu, Songfeng,Keller, Kristen A.,Mulheron, Janet G.,Batorsky, Roberta,Tokarski, John S.,Sack, John S.,Kimball, S. David,Lee, Francis Y.,Webster, Kevin R.
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p. 2973 - 2977
(2007/10/03)
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