14383-51-8Relevant articles and documents
NOVEL PURINE DERIVATIVES AND THEIR USE IN THE TREATMENT OF DISEASE
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Page/Page column 44, (2013/05/21)
The invention relates to PI3K inhibitors of the formula (I) ? in which all of the variables are as defined in the specification, to their preparation, to their medical use, in particular to their use in the treatment of cancer and neurodegenerative disorders, and to medicaments comprising them.
Amido compounds and their use as pharmaceuticals
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Page/Page column 30, (2010/11/26)
The present invention relates to inhibitors of 11-β hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-β hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess.
Manipulation of substituents at nitrogen in tropanes, homotropanes, and dehydro- derivatives
Howarth, Nicola M.,Malpass, John R.,Smith, Craig R.
, p. 10899 - 10914 (2007/10/03)
Trop-6-ene (8-methyl-8-azabicyclo[3.2.1]oct-6-ene) and substituted N- benzylnortrop-6-enes are synthesised. N-Debenzylation of tropanes fails using a wide variety of non-hydrogenolytic conditions despite effective application in model piperidine derivatives; debenzylation of homotropanes is more successful, giving norhomotropane and norhomotrop-7-ene. Bridged N-benzyl compounds react more slowly than N-methyl analogues with chloroformates; the resulting quaternary intermediates are more prone than the N-methyl analogues to suffer competitive reversion to the starting amine, especially in the tropanes, consistent with slower S(N)2 attack at the benzylic carbon during decomposition; the use of an N-p-methoxybenzyl group does allow partial debenzylation to nortrop-6-ene, suggesting greater S(N)1 character in the decomposition step in this case. 'Equatorial' attack is preferred in methylation of N-benzyl-nortrop-6-ene and -homotrop-7-ene with CH3I; subsequent reductive debenzylation of the quaternary salt achieves overall replacement of N-benzyl by N-methyl in both cases. VT NMR studies show the presence of a single 'equatorial' invertomer (CI syn- to the 2C-bridge) in N- chloro-norhomotropanes and -7-enes and by analogy, in the N-alkyl compounds.