- BENZYL-, (PYRIDIN-3-YL)METHYL- OR (PYRIDIN-4-YL)METHYL-SUBSTITUTED OXADIAZOLOPYRIDINE DERIVATIVES AS GHRELIN O-ACYL TRANSFERASE (GOAT) INHIBITORS
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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 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.
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Page/Page column 79; 81; 93
(2019/08/26)
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- (2S,3S)-3-amino-4-(3,3-difluoropyrrolidin-1-yl)-N,N-dimethyl-4-oxo-2-(4-[1, 2,4]triazolo[1,5-a]-pyridin-6-ylphenyl)butanamide: A selective α-amino amide dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes
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A series of β-substituted biarylphenylalanine amides were synthesized and evaluated as inhibitors of dipeptidyl peptidase IV (DPP-4) for the treatment of type 2 diabetes. Optimization of the metabolic profile of early analogues led to the discovery of (2S
- Edmondson, Scott D.,Mastracchio, Anthony,Mathvink, Robert J.,He, Jiafang,Harper, Bart,Park, You-Jung,Beconi, Maria,Di Salvo, Jerry,Eiermann, George J.,He, Huaibing,Leiting, Barbara,Leone, Joseph F.,Levorse, Dorothy A.,Lyons, Kathryn,Patel, Reshma A.,Patel, Sangita B.,Petrov, Aleksandr,Scapin, Giovanna,Shang, Jackie,Roy, Ranabir Sinha,Smith, Aaron,Wu, Joseph K.,Xu, Shiyao,Zhu, Bing,Thornberry, Nancy A.,Weber, Ann E.
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p. 3614 - 3627
(2007/10/03)
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- PHENYLALANINE DERIVATIVES AS DIPEPTIDYL PEPTIDASE INHIBITORS FOR THE TREATMENT OR PREVENTION OF DIABETES
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The present invention is directed to phenylalanine derivatives which are inhibitors of the dipeptidyl peptidase-IV enzyme ("DP-IV inhibitors") and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
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