Benzyl-, (pyridin-3-yl)methyl- or (pyridin-4-yl)methyl-substituted oxadiazolopyridine derivatives as ghrelin O-acyl transferase (GOAT) inhibitors

A kind of technology of pyridine and substituent, applied in the field of novel diazolopyridine derivatives
CN111655700AActive Publication Date: 2020-09-11BOEHRINGER INGELHEIM INT GMBH
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
BOEHRINGER INGELHEIM INT GMBH
Publication Date
2020-09-11

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Abstract

The present invention relates to compounds of general formula (I), wherein the groups R1 and R2 are defined as in claim 1, which have valuable pharmacological properties, in particular bind to ghrelinO-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.
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Description

technical field

[0001] The present invention relates to: new Oxadiazolopyridine derivatives, which are inhibitors of ghrelin O-acyltransferase (GOAT); preparation methods of these compounds; pharmaceutical compositions comprising these compounds; and their use in the prevention and / or treatment of ghrelin Medicinal use for diseases affected by the modulation of the function of O-acyltransferases (GOATs). In particular, the pharmaceutical composition of the present invention is suitable for the prevention and / or treatment of metabolic diseases, such as obesity, including but not limited to obesity, insulin resistance and diabetes in patients with Prader-Willi syndrome (PWS), in particular is type 2 diabetes. Background technique

[0002] Ghrelin O-acyltransferase (GOAT) is a member of the membrane-embedded O-acyltransferase (MBOAT) protein family and the only enzyme in humans that can promote the acylation reaction of the peptide hormone ghrelin. By linking a medium-chain...

Claims

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