Oxadiazolopyridine Derivates for Use as Ghrelin O-Acyl Transferase (GOAT) Inhibitors
申请人:Boehringer Ingelheim International GmbH
公开号:US20180037594A1
公开(公告)日:2018-02-08
The present invention relates to compounds of general formula I,
wherein the groups R
1
, R
2
and n are defined as in claim
1
, which have valuable pharmacological properties, in particular bind to ghrelin O-acyl transferase (GOAT) and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular obesity.
New pentacyclic indeno[1′,2′:4,5]pyrido[2,1-a]isoindol-5-ones were designed which possess quantum yields in the solid state up to 32%. The importance of the substituent in 7-position was highlighted through crystal packing analysis.
Asymmetric Synthesis of Diastereo- and Enantiopure Bioxahelicene 2,2′-Bipyridines
作者:Jiří Klívar、Michal Šámal、Andrej Jančařík、Jaroslav Vacek、Lucie Bednárová、Miloš Buděšínský、Pavel Fiedler、Ivo Starý、Irena G. Stará
DOI:10.1002/ejoc.201800541
日期:2018.10.9
Enantio‐ and diastereopure bioxahelicene 2,2′‐bipyridines were synthesized employing dicyanotetrayne cycloisomerization or triyne cycloisomerization–haloazaoxahelicene homocoupling. An effective central‐to‐helical‐to‐axial chirality transfer was reached.