1057641-73-2Relevant academic research and scientific papers
C5-Alkyl-2-methylurea-substituted pyridines as a new class of glucokinase activators
Du, Xiaohui,Hinklin, Ronald J.,Xiong, Yumei,Dransfield, Paul,Park, Jaehyeon,Kohn, Todd J.,Pattaropong, Vatee,Lai, Sujen,Fu, Zice,Jiao, Xianyun,Chow, David,Jin, Lixia,Davda, Jasmine,Veniant, Murielle M.,Anderson, Deborah A.,Baer, Brian R.,Bencsik, Josef R.,Boyd, Steven A.,Chicarelli, Mark Joseph,Mohr, Peter J.,Wang, Bin,Condroski, Kevin R.,Dewolf, Walter E.,Conn, Marion,Tran, Thanhvien,Yang, Jerry,Aicher, Thomas D.,Medina, Julio C.,Coward, Peter,Houze, Jonathan B.
, p. 1284 - 1289 (2014)
Glucokinase (GK) activators represent a class of type 2 diabetes therapeutics actively pursued due to the central role that GK plays in regulating glucose homeostasis. Herein we report a novel C5-alkyl-2-methylurea-substituted pyridine series of GK activators derived from our previously reported thiazolylamino pyridine series. Our efforts in optimizing potency, enzyme kinetic properties, and metabolic stability led to the identification of compound 26 (AM-9514). This analogue showed a favorable combination of in vitro potency, enzyme kinetic properties, acceptable pharmacokinetic profiles in preclinical species, and robust efficacy in a rodent PD model.
PYRIDOPYRIMIDINE COMPOUNDS ACTING AS MTORC 1/2 DOUBLE-KINASE INHIBITORS
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Paragraph 0286-0288, (2020/11/30)
Disclosed are a series of pyridopyrimidine compounds and a use of same in the preparation of drugs associated with mTORC 1/2 dual complex inhibitors, and specifically disclosed is a use of the compounds as shown in formula (IV), tautomers thereof or pharmaceutically acceptable salts thereof in the preparation of drugs associated with mTORC 1/2 dual complex inhibitors.
3-(1H-PYRAZOL-4-YL)PYRIDINE ALLOSTERIC MODULATORS OF THE M4 MUSCARINIC ACETYLCHOLINE RECEPTOR
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Page/Page column 60, (2019/01/16)
The present invention is directed to pyrazol-4-yl-pyridine compounds which are allosteric modulators of the M4 muscarinic acetylcholine receptor. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which M4 muscarinic acetylcholine receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which M4 muscarinic acetylcholine receptors are involved.
PYRAZOLO (3, 4-B) PYRIDINE DERIVATIVES AS PHOSPHODIESTERASE INHIBITORS
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Page/Page column 114, (2008/12/07)
The present invention relates to phosphodiesterase (PDE) type 4, phosphodiesterase (PDE) type 7 and dual PDE type 4 /PDE type 7 inhibitors. Compounds disclosed herein having the structure of Formura 1: can be useful in the treatment, prevention, inhibitio
