891785-18-5Relevant academic research and scientific papers
NITROGEN-CONTAINING HETEROARYL COMPOUND AND PHARMACEUTICAL USE THEREOF
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Paragraph 0568-0570, (2019/06/07)
The invention provides a compound having a GLUT9 inhibitory activity. The compound is of Formula [I] wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof.
INHIBITORS OF CATECHOL O-METHYL TRANSFERASE AND THEIR USE IN THE TREATMENT OF PSYCHOTIC DISORDERS
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Page/Page column 37, (2011/10/03)
The present invention relates to 4-pyridinone compounds which are inhibitors of catechol O-methyltransferase (COMT), and are useful in the treatment and prevention of neurological and psychiatric disorders and diseases in which COMT enzyme is involved. Th
A convenient route to functionalized 3-amino-N-methylfuro[3,2-b]pyridine-2- carboxamides
Bretéché, Anne,Marchand, Pascal,Nourrisson, Marie-Renée,Hautefaye, Patrick,De Nanteuil, Guillaume,Duflos, Muriel
, p. 4767 - 4773 (2011/07/31)
The synthesis of novel functionalized 3-amino-N-methylfuro[3,2-b]pyridine- 2-carboxamides is described from cyanopyridine intermediates. Based on the difference in halogen reactivity, ethyl [(5-bromo-2-chloropyridin-3-yl)oxy] acetate was functionalized by a palladium-catalyzed reaction, before the cyclization to the desired furo[3,2-b]pyridines.
Straightforward and efficient synthesis of 3-benzyloxy-4-bromopicolinate ester and 3-benzyloxy-5-bromopicolinate ester, common building blocks for pharmaceuticals and agrochemicals
Verdelet, Tristan,Mercey, Guillaume,Correa, Nobi,Jean, Ludovic,Renard, Pierre-Yves
, p. 8757 - 8762 (2011/11/29)
A practical and rapid preparation of 3-benzyloxy-4-bromo and 3-benzyloxy-5-bromopicolinate esters 10 and 16 was developed in four steps, respectively, in 38% and 31% overall yield. Then their viability as partners for cross-coupling reactions has been evaluated in Suzuki-Miyaura, Hartwig-Buchwald, and Sonogashira reactions to synthesize biologically relevant targets. The preparation of these two highly functionalizable pyridines 10 and 16 has been never described to date in the literature and could be used as common building block for the preparation of several biologically active compounds or agrochemical products.
Isoquinoline-pyridine-based protein kinase B/Akt antagonists: SAR and in vivo antitumor activity
Zhu, Gui-Dong,Gong, Jianchun,Claiborne, Akiyo,Woods, Keith W.,Gandhi, Viraj B.,Thomas, Sheela,Luo, Yan,Liu, Xuesong,Shi, Yan,Guan, Ran,Magnone, Shayna R.,Klinghofer, Vered,Johnson, Eric F.,Bouska, Jennifer,Shoemaker, Alexander,Oleksijew, Anatol,Stoll, Vincent S.,Jong, Ron De,Oltersdorf, Tilman,Li, Qun,Rosenberg, Saul H.,Giranda, Vincent L.
, p. 3150 - 3155 (2007/10/03)
The structure-activity relationships of a series of isoquinoline-pyridine-based protein kinase B/Akt antagonists have been investigated in an effort to improve the major short-comings of the lead compound 3, including poor pharmacokinetic profiles in several species (e.g., mouse iv t1/2 = 0.3 h, po F = 0%). Chlorination at C-1 position of the isoquinoline improved its pharmacokinetic property in mice (iv t1/2 = 5.0 h, po F = 51%) but resulted in >500-fold drop in potency. In a mouse MiaPaCa-2 xenograft model, an amino analog 10y significantly slowed the tumor growth, however was accompanied by toxicity.
Kinase inhibitors
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, (2008/06/13)
Compounds having the formula are useful for inhibiting protein kinases. Also disclosed are compositions which inhibit protein kinases and methods of inhibiting protein kinases in a patient.
Kinase inhibitors
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Page/Page column 18, (2010/01/31)
Compounds having the formula are useful for inhibiting protein kinases. Also disclosed are compositions which inhibit protein kinases and methods of inhibiting protein kinases in a patient.
