93748-19-7Relevant academic research and scientific papers
Triazolopyridine ethers as potent, orally active mGlu2positive allosteric modulators for treating schizophrenia
Higgins, Mendi A.,Marcin, Lawrence R.,Christopher Zusi,Gentles, Robert,Ding, Min,Pearce, Bradley C.,Easton, Amy,Kostich, Walter A.,Seager, Matthew A.,Bourin, Clotilde,Bristow, Linda J.,Johnson, Kim A.,Miller, Regina,Hogan, John,Whiterock, Valerie,Gulianello, Michael,Ferrante, Meredith,Huang, Yanling,Hendricson, Adam,Alt, Andrew,Macor, John E.,Bronson, Joanne J.
, p. 496 - 513 (2016/12/30)
Triazolopyridine ethers with mGlu2positive allosteric modulator (PAM) activity are disclosed. The synthesis, in vitro activity, and metabolic stability data for a series of analogs is provided. The effort resulted in the discovery of a potent, selective, and brain penetrant lead molecule BMT-133218 ((+)-7m). After oral administration at 10 mg/kg, BMT-133218 demonstrated full reversal of PCP-stimulated locomotor activity and prevented MK-801-induced working memory deficits in separate mouse models. Also, reversal of impairments in executive function were observed in rat set-shifting studies at 3 and 10 mg/kg (p.o.). Extensive plasma protein binding as the result of high lipophilicity likely limited activity at lower doses. Optimized triazolopyridine ethers offer utility as mGlu2PAMs for the treatment of schizophrenia and merit further preclinical investigation.
A α - (4 - substituted phenyl) of isobutyric acid preparation method
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Paragraph 0071, (2017/08/26)
The invention relates to the field of organic chemical synthesis and discloses a preparation method of alpha-(4-substituted phenyl)isobutyric acid. The method comprises the steps of respectively carrying out Friedel-Crafts acylation, condensation reaction, rearrangement reaction and hydrolytic acidification reaction on single substituted benzene and 2-haloisobutyryl halide or isobutyryl halide serving as an acylating agent to finally prepare a finished product of alpha-(4-substituted phenyl)isobutyric acid. The preparation method provided by the invention has the advantages that the raw materials are easily obtained and are relatively low in toxicity, a catalysis system of the rearrangement reaction can effectively promote the rearrangement reaction, the obtained product is relatively high in purity and yield, the whole preparation method is simple, the adopted reagent is safe, and the preparation method is beneficial to industrial production.
TRIAZOLOPYRIDINE ETHER DERIVATIVES AND THEIR USE IN NEUROLOGICAL AND PYSCHIATRIC DISORDERS
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Page/Page column 25, (2015/04/15)
The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds modulate the mGluR2 receptor and may be useful for the treatment of various disorders of the central nervous system.
Palladium(II)-catalyzed directed trifluoromethylthiolation of unactivated C(sp3)-H bonds
Xiong, Heng-Ying,Besset, Tatiana,Cahard, Dominique,Pannecoucke, Xavier
, p. 4204 - 4212 (2015/05/05)
The synthesis of trifluoromethylthiolated aliphatic acid derivatives by Pd-catalyzed C(sp3)-H bond functionalization was developed. Using a bidentate directing group, the direct and selective introduction of a SCF3 moiety was possible on a range of amides with remarkable selectivity for C(sp3)-centers with an electrophilic SCF3 source and pivalic acid as an additive. This work constitutes an example of the unactivated C(sp3)-SCF3 bond formation by C-H activation offering a new access to relevant molecules.
IL-8 RECEPTOR ANTAGONISTS
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Page/Page column 27, (2008/12/06)
This invention relates to novel compounds, compositions and combinations thereof, useful in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).
NAPHTHALENONE COMPOUNDS EXHIBITING PROLYL HYDROXYLASE INHIBITORY ACTIVITY, COMPOSITIONS, AND USES THEREOF
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Page/Page column 77-78, (2008/12/06)
Compounds of Formula (I) and Formula (II) are useful as inhibitors of HIF prolyl hydroxylases. Compounds of Formula(I) and Formula (II) have the following structures, where the definitions of the variables are provided herein.
