4653-11-6Relevant articles and documents
NOVEL TRICYCLIC CALCIUM SENSING RECEPTOR ANTAGONISTS
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Page/Page column 100, (2015/07/07)
Novel tricyclic compounds of Formula (I) and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing osteoporosis and similar conditions. The compounds are effective as calcium sensing receptor antagonists. Pharmaceutical compositions and methods of treatment are also included.
New combination of pharmacophoric elements of potent σ1 ligands: Design, synthesis and σ receptor affinity of aminoethyl substituted tetrahydrobenzothiophenes
Harel, Dipak,Schepmann, Dirk,Wünsch, Bernhard
, p. 490 - 497 (2013/10/22)
The aminoethyl substituted tetrahydrobenzothiophenes 4 resulted from combination of the pharmacophoric elements of the potent σ1 ligands 2 and 3. The aminoethyl substituted tetrahydrobenzothiophenes 4 were prepared in an 8-step synthesis starting with thiophene. Whereas the σ1 affinity of the N-benzyl derivative 4a is in the medium nanomolar range (Ki = 49 nM), the analogous N-cyclohexylmethyl derivative 4d exhibits low nanomolar affinity (Ki = 5.0 nM). The reduced σ1 affinity and σ2/σ1 selectivity of tetrahydrobenzothiophenes 4 compared to analogous spirocyclic piperidines 3 is attributed to the increased conformational flexibility of the aminoethyl side chain.
SYNTHESIS OF SUBSTITUTED TETRAHYDROINDENYL COMPLEXES
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Page/Page column 17-19, (2010/08/04)
This invention relates to the synthesis of substituted tetrahydroindenyls and the use of the synthesised complexes in the homo- and co-polymerisation of ethylene and alpha-olefins.