27650-80-2Relevant academic research and scientific papers
5,6,7,8-TETRAHYDRO-IMIDAZO[1,5-A]PYRAZINE DERIVATIVES
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Page/Page column 47, (2008/12/06)
The invention relates to 5,6,7,8-tetrahydro-imidazo[1,5-a]pyrazine derivatives of formula (I),wherein X represents CH2 or O; R1 represents a phenyl group, which group is independently mono-, di-, or tri-substituted wherein the substituents are independently selected from the group consisting of (C1-4)alkyl, (C1-4)alkoxy, halogen, cyano, trifluoromethoxy and trifluoromethyl; R2 represents (C1-4)alkyl, (C1-4)alkoxy, (C2-4)alkenyl, halogen, cyano, hydroxymethyl, trifluoromethyl, C(O)NR5R6 or cyclopropyl; R3 represents (C1-4)alkyl, (C1-4)alkoxy-methyl or halogen; R4 represents (C1-4)alkyl; R5 represents hydrogen or (C1-4)alkyl; and R6 represents hydrogen or (C1-4)alkyl. The invention also relates to pharmaceutically acceptable salts of such compounds; and to the use of such compounds as medicaments; especially as orexin receptor antagonists.
Bicyclic cyclohexylamines and their use as nmda receptor antagonists
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Page 53, (2010/02/06)
Described are bicycle-substituted cyclohexylamines of Formula (I) and their pharmaceutically acceptable salts thereof. The compounds are antagonists of NMDA receptor channel complexes useful for treating cerebral vascular disorders such as, for example, cerebral ischemia, cardiac arrest, stroke, and Parkinson's specification. disease. The substituents are defined in the specification.
96. Synthesis of 1,3,4,5-tetrahydro-2-benzoxepin derivatives as conformationally restricted analogues of cyclamenaldehyde-type compounds and as intermediates for highly odour-active homologues
Skouroumounis, Georges,Winter, Beat
, p. 1095 - 1109 (2007/10/03)
Nine 1,3,4,5-tetrahydro-2-benzoxepin derivatives have been prepared as mimics of the folded (gauche) conformation of cyclamenaldehyde (1) and related compounds, but none of them showed the typical lily-of-the valley (muguet) odour activity. However, conversion of these substances to previously unknown analogues of 1 having a Me substituent on the aromatic ring in an ortho position to the side chain led to new fragrance substances with remarkable properties. The results indicate that the extended (anti) conformation is more likely to be the 'bioactive' one at the receptor site(s).
