58584-86-4Relevant academic research and scientific papers
Boron-Containing Small Molecules as Anti-Inflammatory Agents
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Paragraph 0722-0723, (2015/11/16)
Compounds and methods of treating anti-inflammatory conditions are disclosed.
Identification of (R)-6-(1-(4-cyano-3-methylphenyl)-5-cyclopentyl-4,5- dihydro-1H-pyrazol-3-yl)-2-methoxynicotinic acid, a highly potent and selective nonsteroidal mineralocorticoid receptor antagonist
Casimiro-Garcia, Agustin,Piotrowski, David W.,Ambler, Catherine,Arhancet, Graciela B.,Banker, Mary Ellen,Banks, Tereece,Boustany-Kari, Carine M.,Cai, Cuiman,Chen, Xiangyang,Eudy, Rena,Hepworth, David,Hulford, Catherine A.,Jennings, Sandra M.,Loria, Paula M.,Meyers, Marvin J.,Petersen, Donna N.,Raheja, Neil K.,Sammons, Matthew,She, Li,Song, Kun,Vrieze, Derek,Wei, Liuqing
, p. 4273 - 4288 (2014/06/09)
A novel series of nonsteroidal mineralocorticoid receptor (MR) antagonists identified as part of our strategy to follow up on the clinical candidate PF-03882845 (2) is reported. Optimization departed from the previously described pyrazoline 3a and focused on improving the selectivity for MR versus the progesterone receptor (PR) as an approach to avoid potential sex-hormone-related adverse effects and improving biopharmaceutical properties. From this effort, (R)-14c was identified as a potent nonsteroidal MR antagonist (IC50 = 4.5 nM) with higher than 500-fold selectivity versus PR and other related nuclear hormone receptors, with improved solubility as compared to 2 and pharmacokinetic properties suitable for oral administration. (R)-14c was evaluated in vivo using the increase of urinary Na+/K+ ratio in rat as a mechanism biomarker of MR antagonism. Treatment with (R)-14c by oral administration resulted in significant increases in urinary Na +/K+ ratio and demonstrated this novel compound acts as an MR antagonist.
4, 5-DIHYDRO-LH-PYRAZOLE COMPOUNDS AND THEIR PHARMACEUTICAL USES
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Page/Page column 65, (2010/11/03)
Mineralocorticoid receptor antagonists (MRa), pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat, for example, diabetic nephropathy and hypertension in mammals, including humans.
2,4'-BIPYRIDINYL COMPOUNDS AS PROTEIN KINASE D INHIBITORS USEFUL FOR THE TREATMENT OF IA HEART FAILURE AND CANCER
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Page/Page column 134, (2010/01/07)
The present invention provides novel organic compounds of Formula I: methods of use, and pharmaceutical compositions thereof.
2-AMINOBENZAMIDE DERIVATIVE
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Page/Page column 20, (2008/12/07)
To provide a novel and excellent agent for treating or preventing nociceptive pain, neuropathic pain, cancer pain, headache, bladder function disorder and the like, based on the inhibitory action on the capsaicin receptor VR1 activation. The present inven
NEW PYRIDINE ANALOGUES VIII 518
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Page/Page column 184-185, (2008/12/07)
The present invention relates to certain new pyridin analogues of Formula ( I ) to processes for preparing such compounds, to their utility as P2Y12 inhibitors and as anti-trombotic agents etc, their use as medicaments in cardiovascular diseases as well as pharmaceutical compositions containing them.
New Pyridine Analogues IX 519
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Page/Page column 39-40, (2008/12/06)
The present invention relates to certain new pyridin analogues of Formula (I) to processes for preparing such compounds, to their utility as P2Y12 inhibitors and as anti-trombotic agents etc, their use as medicaments in cardiovascular diseases as well as pharmaceutical compositions containing them.
Amide derivatives as ion-channel ligands and pharmaceutical compositions and methods of using the same
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Page/Page column 38-39, (2008/06/13)
Compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, traumatic injury, and others.
AZAINDOLE DERIVATIVES AS INHIBITORS OF P38 KINASE
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Page/Page column 66-67, (2010/11/24)
The invention is directed to methods to inhibit p38 kinase, preferably p38-α using compounds which are azaindoles wherein the azaindoles are coupled through an azacyclic linker to another cyclic moiety.
Diels-Alder reactions of 6-alkyl-3,5-dichloro-2H-1,4-oxazin-2-ones with alkynes: Synthesis of 3,5-disubstituted 2,6-dichloropyridines
Meerpoel,Deroover,Van Aken,Lux,Hoornaert
, p. 765 - 768 (2007/10/02)
The Diels-Alder reactiion of 6-alkyl-3,5-dichloro-2H-1,4-oxazin-2-ones 1 with different types of acetylenic compounds 2 is shown to be a versatile method for the generation of variously substituted 2,6-dichloropyridines. In most cases a high degree of reg
