- Imidazopyridine derivatives and the use thereof as medicament
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The present invention relates to imidazopyridines of formula A processes for their preparation, pharmaceutical compositions containing them and their use in therapy, particularly in the treatment or prevention of conditions having an association with NR2B
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Paragraph 0175-0177; 0178-0181
(2019/06/20)
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- TREATMENT OF AUTISM SPECTRUM DISORDERS, OBSESSIVE-COMPULSIVE DISORDER AND ANXIETY DISORDERS
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Disclosed are methods for treating NMDA receptor-mediated disorders by administering certain NR2B subunit-selective NMDA (N methyl-D aspartate) antagonists. NMDA receptor-mediated disorders include autism spectrum disorders, obsessive-compulsive disorder and anxiety disorders.
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Paragraph 0414
(2018/06/12)
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- 3,3-DIFLUOROPIPERIDINE CARBAMATE HETEROCYCLIC COMPOUNDS AS NR2B NMDA RECEPTOR ANTAGONISTS
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Disclosed are chemical entities of Formula (I), wherein R1 and Z are defined herein, as NR2B subtype selective receptor antagonists. Also disclosed are pharmaceutical compositions comprising a chemical entity of Formula (I), and methods of treating various diseases and disorders associated with NR2B antagonism, e.g., diseases and disorders of the CNS, such as depression, by administering a chemical entity of Formula (I).
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Paragraph 0208
(2016/12/22)
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- Synthesis and in vitro characterization of trans- and cis-[ 18F]-4-methylbenzyl 4-[(pyrimidin-2-ylamino)methyl]-3- fluoropiperidine-1-carboxylates as new potential PET radiotracer candidates for the NR2B subtype N-methyl-d-aspartate receptor
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Diastereoisomeric compounds [18F]cis- and [18F]trans- 4-methylbenzyl 4-[(pyrimidin-2-ylamino)methyl]-3-fluoro-piperidine-1- carboxylates were successfully synthesized as new subtype-selective PET radiotracers for imaging the NR2B sub
- Koudih, Radouane,Gilbert, Gwenaelle,Dhilly, Martine,Abbas, Ahmed,Barre, Louisa,Debruyne, Daniele,Sobrio, Franck
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experimental part
p. 408 - 415
(2012/08/13)
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- N-substituted nonaryl-heterocyclo amidyl NMDA/NR2B Antagonists
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Compounds represented by Formula (I): or pharmaceutically acceptable salts thereof, are effective as NMDA NR2B antagonists useful for relieving pain.
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- N-substituted nonaryl-heterocyclic NMDA/NR2B antagonists
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Compounds represented by Formula (I): 1or pharmaceutically acceptable salts thereof, are effective as NMDA NR2B antagonists useful for relieving pain.
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- Amide derivatives
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A compound represented by the following general formula (1); wherein X represents R1(R2)(R3)C— where R1represents a C3-C8cycloalkyl group, an optionally substituted C6-C14/
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- 3-(Arylacetylamino)-N-methylbenzamides: A novel class of selective anti-Helicobacter pylori agents
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After chemical modification preceded by the random screening of our chemical library, a novel class of selective anti-Helicobacter pylori agents was generated. Consequently, the 3-(arylacetylamino)-N-methylbenzamides, which were quite easy to prepare, showed potent inhibitory activity against Helicobacter pylori but exhibited no inhibitory activity against other sorts of bacteria and fungi, e.g., Staphylococcus aureus, Bacillus subtilis, Escherichia coli, Pseudomonas aeruginosa, Bacteroides fragilis, and Candida albicans. These compounds showed potent anti-H. pylori activity under acidic conditions, whereas amoxicillin and clarithromycin decreased activity. The 3-(3-arylpropionylamino)-N-methylbenzamides, 3-(aryloxyacetylamino)-N-methylbenzamides, and (3-methylcarbamoylphenyl)carbamic acid 1-arylmethyl esters also exhibited potent anti-H. pylori activity. Finally, we selected 7n (BAS-118) as a candidate compound for further evaluation.
- Ando,Kawamura,Chiba
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p. 4468 - 4474
(2007/10/03)
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- AMIDE DERIVATIVES
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Amide derivatives represented by the following general formula (I) and their pharmaceutically acceptable salts, as well as solvates and hydrates thereof, which exhibit anti-Helicobacter pylori activity and are useful as active ingredients for pharmaceutic
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