- Synthesis and evaluation of the anticoccidial activity of trifluoropyrido[1,2-a]pyrimidin-2-one derivatives
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Screening of our chemical library to discover new molecules exhibiting in vitro activity against the invasion of host cells by Eimeria tenella revealed a lead compound with an IC50 of 15 μM. Structure-activity relationship studies were conducted with 34 newly synthesized compounds to identify more active molecules and enhance in vitro activity against the parasite. Four compounds were more effective in inhibiting MDBK cell invasion in vitro than the lead compound.
- Silpa, Laurence,Niepceron, Alisson,Laurent, Fabrice,Brossier, Fabien,Pénichon, Mélanie,Enguehard-Gueiffier, Cécile,Abarbri, Mohamed,Silvestre, Anne,Petrignet, Julien
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p. 114 - 120
(2015/12/18)
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- SUBSTITUTED PYRIDONE DERIVATIVES AS PDE10 INHIBITORS
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The present invention is directed to substituted pyridinone compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
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- Positive Allosteric Modulators of MGLUR2
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The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds modulate the mGluR2 receptor and may be useful for the treatment of various disorders of the centr
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- Regiocontrolled microwave assisted bifunctionalization of 7,8-dihalogenated imidazo[1,2-a]pyridines: A one pot double-coupling approach
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The reactivity of the 7-chloro-8-iodo- and 8-chloro-7-iodoimidazo[1,2- a]pyridines 1a-e diversely substituted on the 2 position, towards Suzuki-Miyaura, Sonogashira, and Buchwald-Hartwig cross-coupling reactions as well as cyanation was evaluated. Various methodologies are proposed to introduce aryl, heteroaryl, alkyne, amine or cyano groups in the two positions depending on the nature of the substituent present in position 2. In both series, the substitution of the iodine atom was totally regioselective and the difficulty was to substitute the chlorine atom in a second step. Until now, only hetero(aryl) groups could be introduced though Suzuki-Miyaura cross-coupling. We overcame this problem evaluating both regioisomers in parallel. The double coupling approach was also studied allowing the one pot Suzuki/Suzuki, cyanation/Sonogashira and cyanation/Buchwald reactions leading to polyfunctionnalized imidazo[1,2-a]pyridines.
- Marie, Emilie,Boucle, Sebastien,Enguehard-Gueiffier, Cecile,Gueiffier, Alain
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p. 10683 - 10707,25
(2020/09/09)
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- PYRIDONE AMIDES AND ANALOGS EXHIBITING ANTI-CANCER AND ANTI-PROLIFERATIVE ACTIVITES
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Compounds useful in the treatment of mammalian cancers and especially human cancers according to Formula I are disclosed. Pharmaceutical compositions and methods of treatment employing the compounds disclosed herein are also disclosed.
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- Discovery of N-(4-(2-amino-3-chloropyridin-4-yloxy)-3-fluorophenyl)-4- ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide (BMS-777607), a selective and orally efficacious inhibitor of the met kinase superfamily
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Substituted N-(4-(2-aminopyridin-4-yloxy)-3-fluoro-phenyl)- 1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamides were identified as potent and selective Met kinase inhibitors. Substitution of the pyridine 3-position gave improved enzyme potency, while substitution of the pyridone 4-position led to improved aqueous solubility and kinase selectivity. Analogue 10 demonstrated complete tumor stasis in a Met- dependent GTL-16 human gastric carcinoma xenograft model following oral administration. Because of its excellent in vivo efficacy and favorable pharmacokinetic and preclinical safety profiles, 10 has been advanced into phase I clinical trials.
- Schroeder, Gretchen M.,An, Yongmi,Cai, Zhen-Wei,Chen, Xiao-Tao,Clark, Cheryl,Cornelius, Lyndon A. M.,Dai, Jun,Gullo-Brown, Johnni,Gupta, Ashok,Henley, Benjamin,Hunt, John T.,Jeyaseelan, Robert,Kamath, Amrita,Kim, Kyoung,Lippy, Jonathan,Lombardo, Louis J.,Manne, Veeraswamy,Oppenheimer, Simone,Sack, John S.,Schmidt, Robert J.,Shen, Guoxiang,Stefanski, Kevin,Tokarski, John S.,Trainor, George L.,Wautlet, Barri S.,Wei, Donna,Williams, David K.,Zhang, Yingru,Zhang, Yueping,Fargnoli, Joseph,Borzilleri, Robert M.
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supporting information; experimental part
p. 1251 - 1254
(2009/12/07)
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- Monocyclic heterocycles as kinase inhibitors
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The present invention is directed to compounds having the formula and methods for using them for the treatment of cancer.
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Page/Page column 46
(2008/06/13)
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- Nitrogen-containing aromatic derivatives
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Compounds represented by the following general formula: [wherein Ag is an optionally substituted 5- to 14-membered heterocyclic group, etc.; Xg is —O—, —S—, etc.; Yg is an optionally substituted C6-14 aryl group, an optionally substituted 5- to 14-membered heterocyclic group, etc.; and Tg1 is a group represented by the following general formula: (wherein Eg is a single bond or —N(Rg2)—, Rg1 and Rg2 each independently represent a hydrogen atom, an optionally substituted C1-6 alkyl group, etc. and Zg represents a C1-8 alkyl group, a C3-8 alicyclic hydrocarbon group, a C6-14 aryl group, etc.)], salts thereof or hydrates of the foregoing.
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