577967-67-0Relevant articles and documents
METHODS OF CULTURING AND/OR EXPANDING STEM CELLS AND/OR LINEAGE COMMITTED PROGENITOR CELLS USING AMIDO COMPOUNDS
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Paragraph 0361; 0382, (2020/02/14)
Provided are methods for expanding stem cells and/or lineage committed progenitor cells, such as hematopoietic stems cells and/or lineage committed progenitor cells, at least in part, by using compounds that antagonize AhR. The compounds are represented by formulae (I) (II) (III) (IV), wherein the letters and symbols a, b, c, d, e, f, g, Z, R1b, R2a and R2b have the meanings provided in the specification. Also provided are compositions comprising stem cells and/or lineage committed progenitor cells expanded by methods disclosed herein and methods for the treatment of diseases treatable by same.
AMIDO COMPOUNDS AS AhR MODULATORS
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Paragraph 0230; 0251, (2019/02/06)
Provided herein are compounds, compositions and methods of using the compounds and compositions for the treatment of diseases modulated, as least in part, by AhR. The compounds are represented by formulae Formula (I), (II), (III), (iv): wherein the letters and symbols a, b, c, d, e, f, g, Z, R1b, R2a and R2b have the meanings provided in the specification.
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
, 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.
Development of CXCR3 antagonists. Part 4: Discovery of 2-amino-(4-tropinyl)quinolines
Knight, Roland L.,Allen, Daniel R.,Birch, Helen L.,Chapman, Gayle A.,Galvin, Frances C.,Jopling, Louise A.,Lock, Christopher J.,Meissner, Johannes W.G.,Owen, David A.,Raphy, Gilles,Watson, Robert J.,Williams, Sophie C.
, p. 629 - 633 (2008/09/17)
The synthesis and biological evaluation of a novel series of 2-aminoquinoline substituted piperidines and tropanes incorporating a homotropene moiety is herein described. The series exhibits potent antagonism of the CXCR3 receptor and superior physicochem
ANTIDEPRESSANT ARYLPIPERAZINE DERIVATIVES OF HETEROCYCLE-FUSED BENZODIOXANS
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Page 59-60, (2008/06/13)
Compounds of the formula I: are useful for the treatment of depression (including but not limited to major depressive disorder, childhood depression and dysthymia), anxiety, panic disorder, post-traumatic stress disorder, premenstrual dysphoric disorder (also known as pre-menstrual syndrome), attention deficit disorder (with and without hyperactivity), obsessive-compulsive disorder, social anxiety disorder, generalized anxiety disorder, obesity eating disorders such as anorexia nervosa and bulimia nervosa, vasomotor flushing, cocaine and alcohol addiction, sexual dysfunction and related illnesses.
