688357-19-9Relevant academic research and scientific papers
PYRROLO[3,2-C]PYRIDINE DERIVATIVES AS TLR INHIBITORS
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, (2017/01/31)
The present invention provides a heterocyclic compound having a TLR7, TLR9, TLR7/8, TLR7/9 or TLR7/8/9 inhibitory action, which is useful as an agent for the prophylaxis or treatment of autoimmune diseases, inflammatory diseases and the like, in particular, systemic lupus erythematosus, Sjogren's syndrome, rheumatoid arthritis, psoriasis, inflammatory bowel disease and the like. The present invention is a compound represented by the formula (1): wherein each symbol is as described in the specification, or a salt thereof.
PYRROLO[3,2-C]PYRIDINE DERIVATIVES AS TLR INHIBITORS
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, (2016/12/16)
The present invention provides a heterocyclic compound having a TLR7, TLR9, TLR7/8, TLR7/9 or TLR7/8/9 inhibitory action, which is useful as an agent for the prophylaxis or treatment of autoimmune diseases, inflammatory diseases and the like, in particular, systemic lupus erythematosus, Sjogren's syndrome, rheumatoid arthritis, psoriasis, inflammatory bowel disease and the like. The present invention is a compound represented by the formula (1): wherein each symbol is as described in the specification, or a salt thereof.
Maximizing diversity from a kinase screen: Identification of novel and selective pan-Trk inhibitors for chronic pain
Stachel, Shawn J.,Sanders, John M.,Henze, Darrell A.,Rudd, Mike T.,Su, Hua-Poo,Li, Yiwei,Nanda, Kausik K.,Egbertson, Melissa S.,Manley, Peter J.,Jones, Kristen L. G.,Brnardic, Edward J.,Green, Ahren,Grobler, Jay A.,Hanney, Barbara,Leitl, Michael,Lai, Ming-Tain,Munshi, Vandna,Murphy, Dennis,Rickert, Keith,Riley, Daniel,Krasowska-Zoladek, Alicja,Daley, Christopher,Zuck, Paul,Kane, Stephanie A.,Bilodeau, Mark T.
, p. 5800 - 5816 (2014/08/05)
We have identified several series of small molecule inhibitors of TrkA with unique binding modes. The starting leads were chosen to maximize the structural and binding mode diversity derived from a high throughput screen of our internal compound collection. These leads were optimized for potency and selectivity employing a structure based drug design approach adhering to the principles of ligand efficiency to maximize binding affinity without overly relying on lipophilic interactions. This endeavor resulted in the identification of several small molecule pan-Trk inhibitor series that exhibit high selectivity for TrkA/B/C versus a diverse panel of kinases. We have also demonstrated efficacy in both inflammatory and neuropathic pain models upon oral dosing. Herein we describe the identification process, hit-to-lead progression, and binding profiles of these selective pan-Trk kinase inhibitors.
TrkA KINASE INHIBITORS, COMPOSITIONS AND METHODS THEREOF
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Page/Page column 29; 30, (2013/03/26)
The present invention is directed to compounds of formula I and la: which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence are useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, t
Method of Treating Pathological Blushing
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Page/Page column 16, (2010/11/29)
A method of treating pathological blushing is disclosed wherein the patient is administered a DP receptor antagonist. Compositions containing DP antagonists are also included.
NIACIN RECEPTOR AGONISTS, COMPOSITIONS CONTAINING SUCH COMPOUNDS AND METHODS OF TREATMENT
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, (2008/06/13)
The present invention encompasses compounds of Formula I: as well as pharmaceutically acceptable salts and hydrates thereof, that are useful for treating dyslipidemias. Pharmaceutical compositions and methods of use are also included.
METHOD OF TREATING ATHEROSCLEROSIS, DYSLIPIDEMIAS AND RELATED CONDITIONS
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Page/Page column 50, (2008/06/13)
A method of treating atherosclerosis is disclosed wherein nicotinic acid or another nicotinic acid receptor agonist is administered to the patient in combination with a DP receptor antagonist. The DP receptor antagonist is administered to reduce, prevent
METHOD OF TREATING ATHEROSCLEROSIS, DYSLIPIDEMIAS AND RELATED CONDITIONS
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Page/Page column 32, (2010/10/20)
A method of treating atherosclerosis, dyslipidemia and related conditions is disclosed wherein a compound of formula I: or a pharmaceutically acceptable salt or solvate thereof is administered to the patient in combination with a DP receptor antagonist. T
NIACIN RECEPTOR AGONISTS, COMPOSITIONS CONTAINING SUCH COMPOUNDS AND METHODS OF TREATMENT
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Page/Page column 82, (2010/11/08)
The present invention encompasses compounds of Formula (I); as well as pharmaceutically acceptable salts and hydrates thereof, that are useful for treating dyslipidemias. Pharmaceutical compositions and methods of use are also included.
