35076-32-5Relevant academic research and scientific papers
SMALL MOLECULE CMKLR1 ANTAGONISTS IN INFLAMMATORY DISEASE
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Paragraph 0199; 0230-0231; 0247, (2020/12/01)
α-NETA analogs are provided for the treatment of inflammatory disease.
3-[(BENZO[D][1,3]DIOXOLAN-4-YL)-OXY]-3-ARYLPROPYLAMINE TYPE COMPOUNDS AND APPLICATIONS THEREOF
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Paragraph 0065; 0073; 0103, (2018/02/02)
The present invention relates to 3-[(benzo[d][1,3]dioxolan-4-yl)-oxy]-3-arylpropylamine compounds of formula I or pharmaceutically acceptable salts thereof and use thereof. The compound may be used to prepare an antidepressant agent.
Synthesis and evaluation of analogues of the tuberculosis drug bedaquiline containing heterocyclic B-ring units
Choi, Peter J.,Sutherland, Hamish S.,Tong, Amy S.T.,Blaser, Adrian,Franzblau, Scott G.,Cooper, Christopher B.,Lotlikar, Manisha U.,Upton, Anna M.,Guillemont, Jerome,Motte, Magali,Queguiner, Laurence,Andries, Koen,Van den Broeck, Walter,Denny, William A.,Palmer, Brian D.
supporting information, p. 5190 - 5196 (2017/11/01)
Analogues of bedaquiline where the phenyl B-unit was replaced with monocyclic heterocycles of widely differing lipophilicity (thiophenes, furans, pyridines) were synthesised and evaluated. While there was an expected broad positive correlation between lipophilicity and anti-TB activity, the 4-pyridyl derivatives appeared to have an additional contribution to antibacterial potency. The majority of the compounds were (desirably) more polar and had higher rates of clearance than bedaquiline, and showed acceptable oral bioavailability, but there was only limited (and unpredictable) improvement in their hERG liability.
6-Cyano Analogues of Bedaquiline as Less Lipophilic and Potentially Safer Diarylquinolines for Tuberculosis
Tong, Amy S. T.,Choi, Peter J.,Blaser, Adrian,Sutherland, Hamish S.,Tsang, Sophia K. Y.,Guillemont, Jerome,Motte, Magali,Cooper, Christopher B.,Andries, Koen,Van Den Broeck, Walter,Franzblau, Scott G.,Upton, Anna M.,Denny, William A.,Palmer, Brian D.,Conole, Daniel
supporting information, p. 1019 - 1024 (2017/10/18)
Bedaquiline (1) is a new drug for tuberculosis and the first of the diarylquinoline class. It demonstrates excellent efficacy against TB but induces phospholipidosis at high doses, has a long terminal elimination half-life (due to its high lipophilicity), and exhibits potent hERG channel inhibition, resulting in clinical QTc interval prolongation. A number of structural ring A analogues of bedaquiline have been prepared and evaluated for their anti-M.tb activity (MIC90), with a view to their possible application as less lipophilic second generation compounds. It was previously observed that a range of 6-substituted analogues of 1 demonstrated a positive correlation between potency (MIC90) toward M.tb and drug lipophilicity. Contrary to this trend, we discovered, by virtue of a clogP/M.tb score, that a 6-cyano (CN) substituent provides a substantial reduction in lipophilicity with only modest effects on MIC values, suggesting this substituent as a useful tool in the search for effective and safer analogues of 1.
GAMMA-DIKETONES AS WNT/BETA -CATENIN SIGNALING PATHWAY ACTIVATORS
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Paragraph 1714; 1715; 1716; 1728, (2014/09/03)
The present disclosure provides γ-diketones or analogs thereof, that activate Wnt/β-catenin signaling and thus treat or prevent diseases related to signal transduction, such as osteoporosis and osteoarthropathy; osteogenesis imperfecta, bone defects, bone fractures, periodontal disease, otosclerosis, wound healing, craniofacial defects, oncolytic bone disease, traumatic brain injuries or spine injuries, brain atrophy/neurological disorders related to the differentiation and development of the central nervous system, including Parkinson's disease, strokes, ischemic cerebral disease, epilepsy, Alzheimer's disease, depression, bipolar disorder, schizophrenia; otic disorders like cochlear hair cell loss; eye diseases such as age related macular degeneration, diabetic macular edema or retinitis pigmentosa and diseases related to differentiation and growth of stem cell, such as hair loss, hematopoiesis related diseases and tissue regeneration related diseases.
Process for Producing (1RS,3RS,6RS)-6-dimethylaminomethyl-1-(3-methoxyphenyl)-cyclohexane-1,3-diol
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Page/Page column 9, (2009/10/18)
A process for producing (1R,3R,6R)-6-dimethylaminomethyl-1-(3-methoxyphenyl)-cyclohexane-1,3-diol or (1S,3S,6S)-6-dimethylaminomethyl-1-(3-methoxyphenyl)-cyclohexane-1,3-diol or mixtures thereof.
1-Acyldihydropyrazole Derivatives
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Page/Page column 46, (2008/12/08)
Compounds of the formula (I), in which R1, R2, R3a, R3b, R3c and R3d have the meanings indicated in claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumours.
Synthetic studies on morphine-based analgesics. Intramolecular Diels-Alder approach to a 4a-aryldecahydroisoquinolines
Handa, Sheetal,Jones, keith,Newton, Christopher G.
, p. 1623 - 1634 (2007/10/02)
An efficient, stereospecific synthesis of the trans-4a-aryldecahydroisoquinoline skeleton, a substructure of morphine known to possess analgesic activity, is described.
