426463-05-0Relevant academic research and scientific papers
PROTEIN KINASE INHIBITORS
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, (2015/02/18)
A compound of formula (I), wherein R3, R4, G, B, M, and Z are as defined in the claims, and pharmaceutically acceptable salts thereof are disclosed. The compounds of formula (I) possess utility as FGFR inhibitors and are useful in the treatment of a condition, where FGFR kinase inhibition is desired, such as cancer.
ANTI-FIBROTIC PYRIDINONES
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Paragraph 0414, (2015/11/02)
This application relates to polycyclic compounds with a pyridinone or pyridinone derivative core including, substituted pyridinones, 5,6- and 6,6- bicyclic heterocycles and substituted pyridine-thiones. This application also discloses methods of preparing these polycyclic compounds, pharmaceutical compositions and medicaments comprising said compounds and methods to treat, prevent or diagnose diseases, disorders or conditions associated with fibrosis.
ANTI-FIBROTIC PYRIDINONES
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Paragraph 0656; 0658, (2014/04/17)
Disclosed are pyridinone compounds, method for preparing these compounds, and methods for treating fibrotic disorders.
PROTEIN KINASE INHIBITORS
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, (2013/04/25)
A compound of formula (I), wherein R3, R4, G, B, M, and Z are as defined in the claims, and pharmaceutically acceptable salts thereof are disclosed. The compounds of formula (I) possess utility as FGFR inhibitors and are useful in the treatment of a condition, where FGFR kinase inhibition is desired, such as cancer.
Discovery of 1-[4-(3-chlorophenylamino)-1-methyl-1H-pyrrolo[3,2-c]pyridin- 7-yl]-1-morpholin-4-ylmethanone (GSK554418A), a brain penetrant 5-azaindole CB2 agonist for the treatment of chronic pain
Giblin, Gerard M. P.,Billinton, Andrew,Briggs, Michael,Brown, Andrew J.,Chessell, Iain P.,Clayton, Nick M.,Eatherton, Andrew J.,Goldsmith, Paul,Haslam, Carl,Johnson, Matthew R.,Mitchell, William L.,Naylor, Alan,Perboni, Alcide,Slingsby, Brian P.,Wilson, Alex W.
supporting information; experimental part, p. 5785 - 5788 (2010/02/28)
We report the synthesis and SAR of a series of novel azaindole CB 2 agonists. 6-Azaindole 18 showed activity in an acute pain model but was inactive in a chronic model. 18 is a Pgp substrate with low brain penetration. The template was redesign
COMBINATION OF CB2 LIGAND AND PARACETAMOL
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Page/Page column 141, (2008/12/04)
Combination of one or more CB2 modulators and paracetamol are useful of treating conditions which are mediated by the activity of CB2 receptors such as an immune disorder, an inflammatory disorder, pain, rheumatoid arthritis, multiple sclerosis, osteoarthritis, and osteoporosis.
PYRROLOPYRIDINE DERIVATIVES
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Page/Page column 31-32, (2008/06/13)
The present invention relates to novel pyrrolopyridine derivatives, pharmaceutical compositions containing these compounds and their use in the treatment of diseases, particularly pain, which diseases are caused directly or indirectly by an increase or decrease in activity of the cannabinoid receptor.
5-Azidoepibatidine: An Exceptionally Potent Photoaffinity Ligand for Neuronal α4β2 and α7 Nicotinic Acetylcholine Receptors
Zhang, Nanjing,Tomizawa, Motohiro,Casida, John E.
, p. 525 - 528 (2007/10/03)
Racemic 5-azidoepibatidine [(+/-)-1] was synthesized via 5-aminoepibatidine as a candidate photoaffinity ligand with exceptionally high affinity at the mammalian neuronal nicotinic receptors (Ki values of 0.027 nM for α4β2 and 9.7 nM for α7) and excellent photoreactivity.
Compounds and methods for promoting smoking cessation
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, (2008/06/13)
Compounds and methods for promoting smoking cessation. The compounds may be used to treat a variety of other conditions and disease states.
Synthesis, nicotinic acetylcholine receptor binding, and antinociceptive properties of 2-exo-2-(2′,3′-disubstituted 5′-pyridinyl)-7-azabicyclo[2.2.1]heptanes: Epibatidine analogues
Carroll, F. Ivy,Lee, Jeffrey R.,Navarro, Hernán A.,Ma, Wei,Brieaddy, Lawrence E.,Abraham, Philip,Damaj,Martin, Billy R.
, p. 4755 - 4761 (2007/10/03)
A number of 2′,3′-disubstituted epibatidine analogues were synthesized and evaluated in vitro for potency at nicotinic acetylcholine receptors (nAChRs) and in vivo for antinociception activity in the tail-flick and hot-plate models of acute pain and for their ability to affect core body temperature. Compounds that possessed electron-withdrawing groups (F, Cl, Br, and I) in both the 2′- and the 3′-positions showed affinities at the nAChR similar to epibatidine. However, in vivo efficacy did not correlate with affinity. 2-exo-(3′-Amino-2′-chloro-5′- pyridinyl)-7-azabicyclo-[2.2.1]heptane (2i), an epibatidine analogue possessing an electron-releasing amino group in the 3′-position, produced the highest affinity. Compound 2i was also the most selective epibatidine analogue with a Ki of 0.001 nM at αβ nAChRs, which is 26 times greater than that of epibatidine, and a αβ/α7 Ki ratio of 14 000, twice that of epibatidine. In vivo testing revealed that this compound potently inhibited nicotine-induced antinociception with AD50 values below 1 μg/kg. Surprisingly, this same compound was also an agonist at higher doses (ED50 ～20 μg/kg). Thus, the addition of the 3′-amino group to epibatidine confers potent antagonist activity to the compound with little effect on agonist activity. 2,3-Disubstituted epibatidine analogues possessing a 2′-amino group combined with a 3′-bromo or 3′-iodo group showed in vitro and in vivo nAChR properties similar to nicotine.
