211058-80-9Relevant articles and documents
CERAMIDE GALACTOSYLTRANSFERASE INHIBITORS FOR THE TREATMENT OF DISEASE
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Paragraph 00576-00578; 00655-00656; 00658, (2019/06/11)
Described herein are compounds, methods of making such compounds, pharmaceutical compositions and medicaments containing such compounds, and methods of using such compounds to treat or prevent diseases or disorders associated with the enzyme ceramide galactosyltransferase (CGT), such as, for example, lysosomal storage diseases. Examples of lysosomal storage diseases include, for example, Krabbe disease and Metachromatic Leukodystrophy.
Discovery and structural diversity of the hepatitis C virus NS3/4A serine protease inhibitor series leading to clinical candidate IDX320
Parsy, Christophe C.,Alexandre, Fran?ois-René,Bidau, Valérie,Bonnaterre, Florence,Brandt, Guillaume,Caillet, Catherine,Cappelle, Sylvie,Chaves, Dominique,Convard, Thierry,Derock, Michel,Gloux, Damien,Griffon, Yann,Lallos, Lisa B.,Leroy, Frederic,Liuzzi, Michel,Loi, Anna-Giulia,Moulat, Laure,Chiara, Musiu,Rahali, Houcine,Roques, Virginie,Rosinovsky, Elodie,Savin, Simon,Seifer, Maria,Standring, David,Surleraux, Dominique
, p. 5427 - 5436 (2015/11/09)
Exploration of the P2 region by mimicking the proline motif found in BILN2061 resulted in the discovery of two series of potent HCV NS3/4A protease inhibitors. X-ray crystal structure of the ligand in contact with the NS3/4A protein and modulation of the
HETEROCYCLE DERIVATIVE HAVING PGD2 RECEPTOR ANTAGONIST ACTIVITY
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Paragraph 0526-0528, (2014/07/22)
The present invention is related to a compound represented by formula (I), wherein X1, X2, X3, X4, X5, R5, R6, R7, R8, n, p, q, ring A and ring B are as described in the specification, or a
HETEROCYCLIC COMPOUNDS AND METHODS FOR THEIR USE
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, (2013/08/15)
The present invention relates to heterocyclic compounds useful for antagonising angiotensin II Type 2 (AT2) receptor. More particularly the invention relates to piperidine compounds, compositions containing them and their use in methods of treating or preventing disorders or diseases associated with AT2 receptor function including neuropathic pain, inflammatory pain, conditions associated with neuronal hypersensitivity, impaired nerve conduction velocity, cell proliferation disorders, disorders associated with an imbalance between bone resorption and bone formation and disorders associated with aberrant nerve regeneration.
The discovery of CCR3/H1 dual antagonists with reduced hERG risk
Barton, Patrick,Brough, Steven,Evans, Richard,Luckhurst, Christopher A.,Mochel, Tobias,Perry, Matthew W. D.,Rigby, Aaron,Sanganee, Hitesh,Sisson, Adam,Springthorpe, Brian,Bahl, Ash,Bowers, Keith,Riley, Robert J.
, p. 6688 - 6693,6 (2012/12/12)
A series of dual CCR3/H1 antagonists based on a bispiperidine scaffold were discovered. Introduction of an acidic group overcame hERG liability. Bioavailability was optimised by modulation of physico-chemical properties and physical form to del
Validation of high-affinity binding sites for succinic acid through distinguishable binding of gamma-hydroxybutyric acid receptor-specific NCS 382 antipodes
Molnar, Tuende,Visy, Julia,Simon, Agnes,Moldvai, Istvan,Temesvari-Major, Eszter,Doernyei, Gabor,Fekete, Erzsebet Kutine,Kardos, Julianna
supporting information; experimental part, p. 6290 - 6292 (2009/07/18)
Gamma-hydroxybutyric acid (GHB) binding to multiple sites for the tricarboxylic acid cycle intermediate succinic acid (SUC) has been disclosed recently. In order to better characterize these targets, distinguishable binding of GHB receptor-specific NCS 38
Synthesis of all isomers of pulcherrimine, a bitter principle in the sea urchin ovary
Sata, Noriko U,Kuwahara, Ryuji,Murata, Yuko
, p. 115 - 118 (2007/10/03)
All eight isomers of pulcherrimine, a bitter principle of the sea urchin (Hemicentrotus pulcherrimus) ovary have been synthesized, which led to revision of the absolute stereochemistry of pulcherrimine. The synthetic pulcherrimine and the 2S isomer were highly bitter at a concentration of 1.0 mM.
Novel constrained CCK-B dipeptoid antagonists derived from pipecolic acid
Bellier, Bruno,Da Nascimento, Sophie,Meudal, Herve,Gincel, Edith,Roques, Bernard P.,Garbay, Christiane
, p. 1419 - 1424 (2007/10/03)
A new series of 4-substituted pipecolic acid derivatives was prepared and incorporated into dipeptoids. The resulting products behave as moderately potent CCK-B antagonists but their constrained structure and its comparison with structurally related compounds yield valuable information about the conformational requirements for optimal recognition of the CCK-B receptor by antagonists.