Discovery of pyridone-containing imidazolines as potent and selective inhibitors of neuropeptide Y Y5 receptor
摘要:
A series of 2-pyridone-containing imidazoline derivatives was synthesized and evaluated as neuropeptide Y Y5 receptor antagonists. Optimization of the 2-pyridone structure on the 2-position of the imidazoline ring led to identification of 1-(difluoromethyl)-5-[(4S,5S)-4-(4-fluorophenyl)-4-(6-fluoropyridin- 3-yl)-5-methyl-4,5-dihydro-1H-imidazol-2-yl] pyridin-2(1H)-one (7m). Compound 7m displayed statistically significant inhibition of food intake in an agonist-induced food intake model in SD rats and no adverse cardiovascular effects in anesthetized dogs. In addition, markedly higher brain penetrability and a lower plasma Occ90 value were observed in P-gp-deficient mdr1a (-/-) mice compared to mdr1a (+/+) mice after oral administration of 7m. (C) 2009 Elsevier Ltd. All rights reserved.
Mikrobiologisches Verfahren zur Herstellung von heteroaromatischen Carbonsäuren mittels Mikroorganismen der Gattung Alcaligenes
申请人:LONZA AG
公开号:EP0747486B1
公开(公告)日:1999-11-03
2-METHOXYIMINO-2-(PYRIDINYLOXYMETHYL)PHENYL ACETAMIDES WITH 5 MEMBERED HETEROCYCLIC RINGS ON THE PYRIDINE RING AS FUNGICIDES
申请人:Dow AgroSciences LLC
公开号:EP1114045A1
公开(公告)日:2001-07-11
US4766219A
申请人:——
公开号:US4766219A
公开(公告)日:1988-08-23
US5702930A
申请人:——
公开号:US5702930A
公开(公告)日:1997-12-30
[EN] 2-METHOXYIMINO -2-(PYRIDINYLOXYMETHYL) PHENYL ACETAMIDES WITH 5 MEMBERED HETEROCYCLIC RINGS ON THE PYRIDINE RING AS FUNGICIDES<br/>[FR] 2-METHOXYIMINO -2-(PYRIDINYLOXYMETHYLE) PHENYLE ACETAMIDES COMPRENANT DES HETEROCYCLES A 5 CHAINONS SUR LE CYCLE PYRIDINE, UTILISES COMME FONGICIDES
申请人:DOW AGROSCIENCES LLC
公开号:WO2000015637A1
公开(公告)日:2000-03-23
The present invention provides novel 2-methoxyimino -2-(pyridinyloxymethyl) phenyl acetamide compounds with 5 membered heterocyclic rings on the pyridine ring, their use as fungicidal compounds, and their use in fungicidal compositions comprising at least one of the 2-methoxyimino-2-(pyridinyloxymethyl)phenyl acetamide compounds as the active ingredient.