- INHIBITORS OF NOTCH SIGNALLING PATHWAY AND USE THEREOF IN TREATMENT OF CANCERS
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The present invention relates to new inhibitors of Notch signalling pathway and its use in the treatment and/or prevention of cancers.
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Page/Page column 98-99; 133-134
(2020/10/21)
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- COMPOUNDS FOR THE TREATMENT OF ONCOVIRUS INDUCED CANCER AND METHODS OF USE THEREOF
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The pesent invention relates to compounds of formula (I) pharmaceutically-acceptable salts, hydrates, solvates, or stereoisomers thereof and their use for the prevention and treatment of oncovirus induced cancer in a subject.
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Page/Page column 90-91; 106-107; 109
(2020/10/21)
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- COMPOUNDS AND METHODS FOR TREATING OXALATE-RELATED DISEASES
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Disclosed herein are compounds and compositions for modulating glycolate oxidase, useful for treating oxalate-related diseases, such as hyperoxaluria, where modulating glycolate oxidase is expected to be therapeutic to a patent in need thereof. Methods of modulating glycolate oxidase activity in a human or animal subject is also provided.
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Paragraph 0283-0284
(2019/09/12)
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- The regioselective homocoupling of meta-hydroxypyridines with hypervalent iodine(iii)
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The C-H homocoupling of meta-hydroxypyridines with phenyliodine(III) diacetate (PIDA) was carried out in dichloromethane at room temperature in the presence of cesium carbonate. The coupling reaction is highly regioselective with respect to the hydroxy group at the pyridine ring. Comparative control experiments with meta-alkoxypyridine suggest that the meta-hydroxy group at the pyridine ring plays a key role during the homocoupling reaction.
- Yang, Ping Syun,Tsai, Mi Ting,Tsai, Meng Han,Ong, Chi Wi
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supporting information
p. 849 - 852
(2015/03/31)
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- Contrasting Anticancer Activity of Half-Sandwich Iridium(III) Complexes Bearing Functionally Diverse 2-Phenylpyridine Ligands
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We report the synthesis, characterization, and antiproliferative activity of 15 iridium(III) half-sandwich complexes of the type [(η5-Cp?)Ir(2-(R′-phenyl)-R-pyridine)Cl] bearing either an electron-donating (-OH, -CH2OH, -CH3) or electron-withdrawing (-F, -CHO, -NO2) group at various positions on the 2-phenylpyridine (2-PhPy) chelating ligand giving rise to six sets of structural isomers. The X-ray crystal structures of [(η5-Cp?)Ir(2-(2′-fluorophenyl)pyridine)Cl] (1) and [(η5-Cp?)Ir(2-(4′-fluorophenyl)pyridine)Cl] (2) exhibit the expected "piano-stool" configuration. DFT calculations showed that substituents caused only localized effects on the electrostatic potential surface of the chelating 2-PhPy ligand of the complexes. Hydrolysis of all complexes is rapid, but readily reversed by addition of NaCl. The complexes show preferential binding to 9-ethylguanine over 9-methyladenine and are active catalysts for the oxidation of NADH to NAD+. Antiproliferative activity experiments in A2780 ovarian, MCF-7 breast, A549 lung, and HCT116 colon cancer cell lines showed IC50 values ranging from 1 to 89 μM, with the most potent complex, [(η5-Cp?)Ir(2-(2′-methylphenyl)pyridine)Cl] (13) (A2780 IC50 = 1.18 μM), being 10× more active than the parent, [(η5-Cp?)Ir(2-phenylpyridine)Cl], and 2× more active than [(η5-CpxPh)Ir(2-phenylpyridine)Cl]. Intriguingly, contrasting biological activities are observed between structural isomers despite exhibiting similar chemical reactivity. For pairs of structural isomers both the nature and position of the functional group can affect the hydrophobicity of the complex. An increase in hydrophobicity resulted in enhanced cellular-iridium accumulation in A2780 ovarian cells, which generally gave rise to an increase in potency. The structural isomers [(η5-Cp?)Ir(2-(4′-fluorophenyl)pyridine)Cl] (2) and [(η5-Cp?)Ir(2-phenyl-5-fluoropyridine)Cl] (4) preferentially localized in the cytosol > membrane and particulate > nucleus > cytoskeleton. This work highlights the strong dependence of biological behavior on the nature and position of the substituent on the chelating ligand and shows how this class of organometallic anticancer complexes can be fine-tuned to increase their potency without using extended cyclopentadienyl systems. (Chemical Equation Presented).
- Millett, Adam J.,Habtemariam, Abraha,Romero-Canelón, Isolda,Clarkson, Guy J.,Sadler, Peter J.
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supporting information
p. 2683 - 2694
(2015/06/23)
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- OXAZOLOBENZIMIDAZOLE DERIVATIVES
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The present invention is directed to oxazolobenzimidazole derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.
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Page/Page column 38
(2009/12/23)
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- Studies on Diazepines. XXV. Syntheses of Fully Unsaturated 1,4-Oxazepines and 1H-1,4-Diazepines Using Photochemical Valence Isomerization of Tricycloheptene Systems
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3-Azatricyclo2,5>hept-3-ene derivatives prepared from pyridines via five steps were found to be useful synthons for fully unsaturated monocyclic seven-membered heterocyclic rings.Photolysis of the 7-oxa derivatives 15 resulted in valenc
- Kurita, Jyoji,Iwata, Kuniyoshi,Tsuchiya, Takashi
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p. 3166 - 3174
(2007/10/02)
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- Synthesis of the First Examples of Fully Unsaturated Monocyclic 1,4-Oxazepines
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Photolysis of the 3-aza-7-oxatricyclo2,5>hept-3-enes (3), prepared from pyridines via five steps, results in ring expension to give the novel 1,4-oxazepines (4).
- Kurita, Jyoji,Iwata, Kuniyoshi,Tsuchiya, Takashi
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p. 1188 - 1189
(2007/10/02)
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