1214353-79-3Relevant academic research and scientific papers
TRIAZOLOPYRIMIDINE DERIVATIVES FOR USE AS GHRELIN O-ACYL TRANSFERASE (GOAT) INHIBITORS
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Page/Page column 66, (2019/08/26)
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.
PYRAZOLYL-SUBSTITUTED PYRIDONE COMPOUNDS AS SERINE PROTEASE INHIBITORS
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Paragraph 00383-00384, (2016/04/09)
There are provided inter alia pyrazolyl-substituted pyridone compounds, which exhibit biological activity, e.g., inhibitory action, against serine proteases, including thrombin and various kallikreins. There are additionally provided pharmaceutical compositions. There are additionally provided methods of treating and preventing certain diseases or disorders, which disease or disorder is amenable to treatment or prevention by the inhibition of serine proteases, including thrombin and various kallikreins.
Discovery of a high affinity and selective pyridine analog as a potential positron emission tomography imaging agent for cannabinoid type 2 receptor
Slavik, Roger,Grether, Uwe,Müller Herde, Adrienne,Gobbi, Luca,Fingerle, Jürgen,Ullmer, Christoph,Kr?mer, Stefanie D.,Schibli, Roger,Mu, Linjing,Ametamey, Simon M.
, p. 4266 - 4277 (2015/06/08)
As part of our efforts to develop CB2 PET imaging agents, we investigated 2,5,6-substituted pyridines as a novel class of potential CB2 PET ligands. A total of 21 novel compounds were designed, synthesized, and evaluated for their potency and binding properties toward human and rodent CB1 and CB2. The most promising ligand 6a was radiolabeled with carbon-11 to yield 16 ([11C]RSR-056). Specific binding of 16 to CB2-positive spleen tissue of rats and mice was demonstrated by in vitro autogadiography and verified in vivo in PET and biodistribution experiments. Furthermore, 16 was evaluated in a lipopolysaccharid (LPS) induced murine model of neuroinflammation. Brain radioactivity was strikingly higher in the LPS-treated mice than the control mice. Compound 16 is a promising radiotracer for imaging CB2 in rodents. It might serve as a tool for the investigation of CB2 receptor expression levels in healthy tissues and different neuroinflammatory disorders in humans.
NOVEL PYRIDINE DERIVATIVES
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Page/Page column 34, (2014/06/24)
The invention relates to a compound of formula (I) wherein R1 to R3 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.
PYRIDINE-2-AMIDES USEFUL AS CB2 AGONISTS
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Page/Page column 46, (2014/06/24)
The invention relates to CB2 agonists of formula (I) wherein R1 to R4 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.
AROMATIC RING COMPOUND
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Paragraph 0268, (2015/01/18)
Provided is an aromatic ring compound having a GPR40 agonist activity. A compound represented by the formula (I): wherein each symbol is as described in the DESCRIPTION, or a salt thereof has a GPR40 agonist activity, and is useful as an agent for the prophylaxis or treatment of diabetes and the like.
AROMATIC RING COMPOUND
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Paragraph 0481, (2015/01/18)
Provided is an aromatic ring compound having a GPR40 agonist activity. A compound represented by the formula (I): wherein each symbol is as described in the DESCRIPTION, or a salt thereof has a GPR40 agonist activity, and is useful as an agent for the prophylaxis or treatment of diabetes and the like.
PYRIDIN- 2 -AMIDES USEFUL AS CB2 AGONISTS
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Page/Page column 77, (2013/02/27)
The invention relates to a compound of formula (I) wherein R1 to R4 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.
NOVEL PYRIDINE DERIVATIVES
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Page/Page column 32, (2013/02/27)
The invention relates to a compound of formula (I) wherein R1 to R4 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.
