1087160-01-7Relevant academic research and scientific papers
Novel inhibitors of nicotinamide-n-methyltransferase for the treatment of metabolic disorders
Czech, Joerg,Dhakshinamoorthy, Saravanakumar,Hallur, Mahanandeesha S.,Kannt, Aimo,Kristam, Rajendra,Rajagopal, Sridharan,Ruf, Sven,Schreuder, Herman,Swamy, Indu,Zech, Gernot
supporting information, (2021/06/12)
Nicotinamide-N-methyltransferase (NNMT) is a cytosolic enzyme catalyzing the transfer of a methyl group from S-adenosyl-methionine (SAM) to nicotinamide (Nam). It is expressed in many tissues including the liver, adipose tissue, and skeletal muscle. Its expression in several cancer cell lines has been widely discussed in the literature, and recent work established a link between NNMT expression and metabolic diseases. Here we describe our approach to identify potent small molecule inhibitors of NNMT featuring different binding modes as elucidated by X-ray crystallographic studies.
Multicomponent synthesis of spiropyrrolidine analogues derived from vinylindole/indazole by a 1,3-dipolar cycloaddition reaction
Narayanarao, Manjunatha,Koodlur, Lokesh,Revanasiddappa, Vijayakumar G.,Gopal, Subramanya,Kamila, Susmita
supporting information, p. 2893 - 2897 (2017/01/09)
A new series of spiropyrrolidine compounds containing indole/indazole moieties as side chains have been accomplished via a one-pot multicomponent synthesis. The method uses the 1,3-dipolar cycloaddition reaction between N-alkylvinylindole/indazole and azomethine ylides, prepared in situ from cyclic/acyclic amino acids. The 1,3-dipolar cycloaddition proceeds efficiently under thermal conditions to afford the regio- and stereospecific cyclic adducts.
INHIBITORS OF FATTY ACID AMIDE HYDROLASE
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Paragraph 1284, (2016/01/15)
The present invention provides compounds, and pharmaceutically acceptable compositions thereof, encompassed by any of formulae (I), (II), (III), (IV), (V), or (VI), or subgenera thereof. The present invention also provides methods for treating an FAAH mediated disease, disorder or condition by administering a therapeutically effective amount of a compound or composition comprising a compound of any of formulae (I), (II), (III), (IV), (V), or (VI), or subgenera thereof, to a patient in need thereof. Additionally, the present invention provides methods for inhibiting FAAH by administering a therapeutically effective amount of a compound or composition comprising a compound of any of formulae (I), (II), (III), (IV), (V), or (VI), or subgenera thereof, to a patient in need thereof.
SUBSTITUTED AROMATIC CARBOXAMIDE AND UREA DERIVATIVES AS VANILLOID RECEPTOR LIGANDS
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Page/Page column 118; 119; 120, (2010/11/18)
The invention relates to substituted aromatic carboxamide and urea derivatives, to processes for the preparation thereof, to pharmaceutical compositions containing these compounds and also to the use of these compounds for preparing pharmaceutical compositions (formula (I)).
Indazoles: Regioselective protection and subsequent amine coupling reactions
Slade, David J.,Pelz, Nicholas F.,Bodnar, Wanda,Lampe, John W.,Watson, Paul S.
supporting information; experimental part, p. 6331 - 6334 (2009/12/26)
(Chemical Equation Presented) Indazoles are unselectively protected under strongly basic conditions to give a mixture at N-1 and N-2. Under mildly acidic conditions, regioselective protection at N-2 takes place. Thermodynamic conditions lead to regioselective protection at N-1. This trend applies to various substituted indazoles. Protected 5-bromoindazoles participate in Buchwald reactions with a range of amines to generate novel derivatives.
