- ANTIBACTERIAL COMPOSITIONS
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Compounds of formula (I) have antibacterial activity wherein: m is O or 1; Q is hydrogen or cyclopropyl; AIk is an optionally substituted, divalent C1-C3 alkylene, C2-C3 alkenylene or C2-C3 alkynylene radical; X is - C(=O)NH- or -C(=O)O-; R2 and R3 are as defined in the specification.
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Page/Page column 15
(2009/07/17)
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- PHARMACOLOGICALLY ACTIVE IMIDAZO[4,5-C]PYRIDINES
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The invention relates to 6-substituted imidazo[4,5-c]pyridines of formula 1, in which X is O (oxygen) or NH and Y has either the meaning -CH2-AR or Y denotes the group gp (gp) wherein Z has the meaning -CHR8- or -CHR8-CHR9-. The compounds have gastric secretion inhibiting and excellent gastric and intestinal protective action properties.
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Page/Page column 43
(2010/02/11)
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- The development of a practical and reliable large-scale synthesis of 2,6-diamino-4-bromopyridine
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A novel, safer, and efficient synthetic route to 2,6-diamino-4-bromopyridine has been developed. In discovery research a five-step synthesis afforded 2,6-diamino-4-bromopyridine in 56% yield with a double Curtius rearrangement as a key transformation. Due to potential safety concerns on larger scale an alternative synthetic strategy was necessary. Starting from 2,4-dibromopyridine-N-oxide two complementary procedures have been developed to access 2,6-diamino-4-bromopyridine. The four-step procedure yielded in 28% overall, and the five-step procedure, in 33% overall 2,6-diamino-4-bromopyridine in a safe and straightforward manner using a regioselective 2,6-diamination reaction as key step. Additionally, a general route to unsymmetrical substituted pyridine N-oxide derivatives is disclosed.
- Nettekoven, Matthias,Jenny, Christian
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