360-60-1Relevant academic research and scientific papers
SUBSTITUTED BENZIMIDAZOLE CARBOXAMIDES AND THEIR USE IN THE TREATMENT OF MEDICAL DISORDERS
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Paragraph 00295; 00373-00374; 00490, (2021/04/01)
The invention provides substituted benzimidazole carboxamides and related compounds, compositions containing such compounds, medical kits, and methods for using such compounds and compositions to treat a medical disorder, e.g., cancer, lysosomal storage disorder, neurodegenerative disorder, inflammatory disorder, in a patient.
TREATING LONG QT SYNDROME
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, (2020/08/22)
This document relates to compounds useful for treating and preventing disorders associated with long QT syndrome such as cardiac arrhythmia, ventricular arrhythmia, hypertrophic cardiomyopathy, and congestive heart failure. Also provided herein are methods and materials for using such compounds to shorten myocardial repolarization time in a patient.
Chiral linker-bridged bis-N-heterocyclic carbenes: Design, synthesis, palladium complexes, and catalytic properties
Zhang, Dao,He, Yu,Tang, Junkai
, p. 11699 - 11709 (2016/07/28)
A series of chiral bis(benzimidazolium) salts 10-19 with (1R,2R)-cyclohexene, (1R,2R)-diphenylethylene and (aR)-binaphthylene linkers have been designed and synthesized in 30-94% yield. Ten chiral bis(NHC) palladium complexes 20-28 have been synthesized and characterized by NMR, HRMS, elemental analysis and further confirmed by X-ray single crystal analysis. These bis(NHC)-Pd complexes showed obviously different catalytic properties in the asymmetric Suzuki-Miyaura coupling reactions. The (1R,2R)-cyclohexene-bridged bis(NHC)-Pd complex, (R,R)-23, achieved the highest yield of 90%, while complex (aR)-28, with a binaphthylene linker, showed the best enantioselectivity of 60 ee%. The structural analysis of these complexes suggested that such difference of catalytic performance has a close relationship with their coordination surroundings around metal centres.
HETEROCYCLIC COMPOUNDS AND THEIR USES
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Page/Page column 98, (2011/10/13)
Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110δ activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lymphoblastic leukaemia (T-ALL) B-cell Acute Lymphoblastic leukaemia (B-ALL) Non Hodgkins Lymphoma (NHL) B-cell lymphoma and solid tumors, such as breast cancer.
DIHYDROOROTATE DEHYDROGENASE INHIBITORS
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Page/Page column 102, (2010/11/03)
The invention relates to compounds of formula (I) wherein R1, R2, X1, X2, Y, Ra, Rb, Q have the meanings given in claim 1. The compounds are useful e.g. in the treatment of autoimmune disorders, such as multiple sclerosis and also in the treatment of cancer disorders.
QUINOXALINE-BASED LXR MODULATORS
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Page/Page column 21, (2010/06/11)
Disclosed are quinoxaline-based modulators of Liver X receptors (LXRs) and related methods. The modulators include compounds of formula (I): wherein: each of L1 and L2 is, independently, a bond, —O— or —NH—;R2 is C6/
Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist
Hu, Baihua,Unwalla, Rayomand J.,Goljer, Igor,Jetter, James W.,Quinet, Elaine M.,Berrodin, Thomas J.,Basso, Michael D.,Feingold, Irene B.,Nilsson, Annika Goos,Wilhelmsson, Anna,Evans, Mark J.,Wrobel, Jay E.
experimental part, p. 3296 - 3304 (2010/10/02)
A series of phenyl sulfone substituted quinoxaline were prepared and the lead compound 13 (WYE-672) was shown to be a tissue selective LXR Agonist. Compound 13 demonstrated partial agonism for LXRβ in kidney HEK-293 cells but did not activate Gal4 LXRβ fusion proteins in huh-7 liver cells. Although 13 showed potent binding affinity to LXRβ (IC50 = 53 nM), it had little binding affinity for LXRα (IC50 > 1.0 μM) and did not recruit any coactivator/corepressor peptides in the LXRα multiplex assay. However, compound 13 showed good agonism in THP-1 cells with respect to increasing ABCA1 gene expression and good potency on cholesterol efflux in THP-1 foam cells. In an eight-week lesion study in LDLR -/- mice, compound 13 showed reduction of aortic arch lesion progression and no plasma or hepatic triglyceride increase. These results suggest quinoxaline 13 may have an improved biological profile for potential use as a therapeutic agent.
Substituted cycloalkylamine derivatives as modulators of chemokine receptor activity
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Page/Page column 46, (2010/02/11)
The present application describes modulators of MCP-1 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma, multiple sclerosis, artherosclerosis, and rheumatoid arthritis.
