[EN] SUBSTITUTED PIPERAZINES, (1,4) DIASZEPINES, AND 2,5-DIAZABICYCLO (2.2.1) HEPTANES AS HISTAMINE H1 AND/OR H3 ANTAGONISTS OR HISTAMINE H3 REVERSE ANTAGONISTS [FR] PIPERAZINES, (1,4) DIAZEPINES, ET 2,5-DIAZABICYCLO (2.2.1) HEPTANES SUBSTITUES EN TANT QU'ANTAGONISTES DE L'HISTAMINE H1 ET/OU H3 OU ANTAGONISTES INVERSES DE L'HISTAMINE H3
1-Amino 1H-imidazoquinoline compounds, pharmaceutical compositions containing the compounds, intermediates, and methods of making and methods of use of these compounds as immunomodulators, for modulating cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.
The invention concerns chromenone derivatives of Formula I
or a pharmaceutically-acceptable salts thereof, wherein each of R
1
, R
2
, R
3
, R
4
, R
5
, R
6
, R
7
, R
8
, n and R
9
has any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the treatment of cell proliferative disorders.
Leukotriene A4 hydrolase (LTA4H) inhibitors, compositions containing them, and methods of use for the inhibition of LTA4H enzyme activity and the treatment, prevention or inhibition of inflammation and/or conditions associated with inflammation.
Synthesis of Piperidine Derivatives by Rhodium- Catalyzed Tandem Reaction of<i>N</i>-Sulfonyl-1,2,3-Triazole and Vinyl Ether
作者:Sisi Yu、Yuehui An、Wenlin Wang、Ze-Feng Xu、Chuan-Ying Li
DOI:10.1002/adsc.201800191
日期:2018.6.5
A chemoselective tandemreaction of 4‐acyloxymethylene‐1‐sulfonyl‐1,2,3‐triazole and vinyl ether was reported, producing polysubstituted piperidinederivatives in up to 96% yield. The key intermediate N‐sulfonyl 1‐azadiene generated by migration of the OAc group to the α‐imino rhodium carbene was isolated and a plausible mechanism was proposed. Several related ring systems were constructed from the