4394-03-0Relevant academic research and scientific papers
HETEROCYCLIC KINASE INHIBITORS
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Page/Page column 161, (2016/05/19)
The present disclosure is generally directed to compounds which can inhibit AAK1 (adaptor associated kinase 1), compositions comprising such compounds, and methods for inhibiting AAK1.
Discovery and optimization of a novel series of GPR142 agonists for the treatment of type 2 diabetes mellitus
Lizarzaburu, Mike,Turcotte, Simon,Du, Xiaohui,Duquette, Jason,Fu, Angela,Houze, Jonathan,Li, Leping,Liu, Jinqian,Reagan, Jeff,Yu, Ming,Medina, Julio C.,Murakoshi, Michiko,Oda, Kozo,Okuyama, Ryo,Nara, Futoshi
, p. 5942 - 5947,6 (2020/07/30)
The discovery and initial optimization of a series of phenylalanine based agonists for GPR142 is described. The structure-activity-relationship around the major areas of the molecule was explored to give agonists 90 times more potent than the initial HTS hit in a human GPR142 inositol phosphate accumulation assay. Removal of CYP inhibition by exploration of the pyridine A-ring is also described.
2, 4- DI (PHENYLAMINO) PYRIMIDINES USEFUL IN THE TREATMENT OF NEOPLASTIC DISEASES, INFLAMMATORY AND IMMUNE SYSTEM DISORDERS
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Page 118; 130, (2010/02/08)
Novel pyrimidine derivatives of formula (I), to processes for their production, their use as pharmaceuticals in the treatment of neoplastic diseases, inflammatory and immune system disorders and to pharmaceutical compositions comprising them.
Synthesis and antiarrhythmic activity of disubstituted phenylpyridine derivative
Shigyo,Sato,Shibuya,Takahashi,Yamaguchi,Sonoki,Ohta
, p. 1573 - 1582 (2007/10/02)
A series of disubstituted phenylpyridine derivatives was synthesized and their antiarrhythmic effects against chloroform-induced ventricular arrhythmias in mice were examined. Among them, 2- and 3-[2-(3- aminobutyramido)-4-(2,2,2-trifluoroethoxy)phenyl]pyridines (23h, 24h) and 3- [2-(3-aminobutyramido)-4-ethoxyphenyl]pyridine (24i) showed potent antiarrhythmic activity. They had approximately twice the potency of mexiletine (III). Compound 24i was selected from this series as a candidate for further development; it was found to have a class I B electrophysiological character and to show a slow kinetic rate-dependent block (RDB) of the sodium channel in cardiac muscle.
Cardiotonic Agents. 1. Synthesis and Structure-Activity Relationships in a New Class of 3-,4-, and 5-Pyridyl-2(1H)-quinolone Derivatives
Leclerc, Gerard,Marciniak, Gilbert,Decker, Nicole,Schwartz, Jean
, p. 2427 - 2432 (2007/10/02)
A series of 3-,4-, and 5-pyridyl-2(1H)-quinolone derivatives with H or HO or CH3O substituents in the 8-position were prepared and tested for positive inotropic activity.Several derivatives, especially 29, 9b, and 27 with a pyridyl ring in the 5-position,
