- 4-ARYLQUINAZOLINE DERIVATIVES AS INHIBITORS OF METHIONINE ADENOSYLTRANSFERASE 2A
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The invention relates to certain derivatives of 4-arylquinazoline formula (I) which are inhibitors of methionine adenosyltransferase 2A (MAT2A). The invention also relates to pharmaceutical compositions comprising such compounds and methods of treating diseases that can be treated by inhibition of MAT2A such as cancer, including cancers characterized by reduced or no activity of methylthioadenosine phosphorylase (MTAP).
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Paragraph 0259
(2021/12/31)
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- Monoacylglycerol Lipase Modulators
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Bridged compounds of Formula (I) and Formula (II), pharmaceutical compositions containing them, methods of making them, and methods of using them including methods for treating disease states, disorders, and conditions associated with MGL modulation, such as those associated with pain, psychiatric disorders, neurological disorders (including, but not limited to major depressive disorder, treatment resistant depression, anxious depression, bipolar disorder), cancers and eye conditions. wherein R2, R3 R4, R5 and R6 are defined herein.
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Paragraph 0410; 0633
(2020/04/24)
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- Versatile synthesis of 6-substituted 8-deazapteridine-2,4-diamines. Formal total synthesis of 8,10-dideazaminopterin
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A new synthesis of 4-amino-4-deoxy-8,10-dideazapteroic acid (11d) and 6-substituted and 5,6-anellated 8-deazapteridine-2,4-diamines, 10a, 10d, 25, is described. Starting from keteneaminals 1 or 12 and enaminones 4 or β-aminoketone 17 the title compounds can be prepared via functional group transformation of 2-amino-3-nitropyridines 5 or nicotinate 13a yielding 3-amino-α-picolinonitriles 9 which are cyclocondensed with guanidine.
- Troschutz,Karger
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p. 1815 - 1821
(2007/10/03)
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