189952-45-2Relevant academic research and scientific papers
CERAMIDE GALACTOSYLTRANSFERASE INHIBITORS FOR THE TREATMENT OF DISEASE
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Paragraph 00576-00578; 00720-00721; 00724, (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
Disubstituted piperidines as potent orexin (hypocretin) receptor antagonists
Jiang, Rong,Song, Xinyi,Bali, Purva,Smith, Anthony,Bayona, Claudia Ruiz,Lin, Li,Cameron, Michael D.,McDonald, Patricia H.,Kenny, Paul J.,Kamenecka, Theodore M.
scheme or table, p. 3890 - 3894 (2012/07/13)
A series of orexin receptor antagonists was synthesized based on a substituted piperidine scaffold. Through traditional medicinal chemistry structure-activity relationships (SAR), installation of various groups at the 3-6-positions of the piperidine led to modest enhancement in receptor selectivity. Compounds were profiled in vivo for plasma and brain levels in order to identify candidates suitable for efficacy in a model of drug addiction.
MACROCYCLIC SERINE PROTEASE INHIBITORS
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, (2010/11/03)
Provided herein are macrocyclic serine protease inhibitor compounds, for example, of Formula Ia or Ib, pharmaceutical compositions comprising the compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of an HCV infection in a host in need thereof.
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
The synthesis of 4-hydroxypipecolic acids by stereoselective cycloaddition of configurationally stable nitrones
Cordero, Franca M.,Bonollo, Simona,Machetti, Fabrizio,Brandi, Alberto
, p. 3235 - 3241 (2007/10/03)
The diastereoselective synthesis of trans- and cis-4-hydroxypipecolic acids has been achieved with geometry-controlled nitrone cycloaddition chemistry. The cycloaddition of 3-butenol to enantiopure C-aminocarbonyl and C-alkoxycarbonyl nitrones having a de
NEW COMPOUNDS
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Page 44-45, (2010/02/06)
The present invention relates to new compounds of formula I, wherein P Q X1 X2 X3 X4 X5 R R1 R2 R3 R4R5 G M1 M2 M3 m and n are defined as in formula I, a process for their preparation and new intermediates prepared therein, pharmaceutical formulations containing said compounds and to the use of said compounds in therapy.
