41373-96-0Relevant articles and documents
MODULATORS OF THR-β AND METHODS OF USE THEREOF
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Paragraph 00560, (2020/11/23)
Disclosed herein are compounds of Formula (I) or a pharmaceutically acceptable salt, prodrug, amide or ester thereof, where i) TL is a moiety of Formula IlIa, lIIb, IlIa, IIIb, IIIc, or IIId; ii) CE is a moiety of Formula IV; iii) HD is a moiety of Formula V or VI; where the substituents are as defined herein. Disclosed are also pharmaceutical compositions comprising the above compounds, and methods of treating disease by administering or contact a patient with one or more of the above compounds.
Pyridazinone derivative and application thereof
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Paragraph 0190-0192; 0196-0198, (2020/11/23)
The invention provides a pyridazinone derivative and an application thereof, the pyridazinone derivative with the structure shown in the formula (I) provided by the invention has good activity as a thyroid hormone beta receptor agonist by selecting a specific modification group. The compound can be used for treating and/or preventing diseases caused by thyroid hormone regulation.
Silver-Catalyzed Minisci Reactions Using Selectfluor as a Mild Oxidant
Galloway, Jordan D.,Mai, Duy N.,Baxter, Ryan D.
supporting information, p. 5772 - 5775 (2017/11/10)
A new method for silver-catalyzed Minisci reactions using Selectfluor as a mild oxidant is reported. Heteroarenes and quinones both participate in radical C-H alkylation and arylation from a variety of carboxylic and boronic acid radical precursors. Several oxidatively sensitive and highly reactive radical species are successful, providing structures that are challenging to access by other means.
Facile Synthesis of New [1,2,4]Triazolo[4,3-b]pyridazine
Arghiani,Seyedi,Bakavoli,Eshghi
, p. 1099 - 1107 (2015/08/06)
A number of new [1,2,4]triazolo[4,3-b]pyridazines were prepared by either cyclocondesation of substituted hydrazinopyridazines with orthoesters or oxidative cyclization of their hydrazone analogs in nitrobenzene as an oxidizing agent. A host of other new
DERIVATIVES OF 6-SUBSTITUTED TRIAZOLOPYRIDAZINES AS REV-ERB AGONISTS
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Page/Page column 46; 106, (2013/04/13)
The present invention provides novel 6-substituted [1,2,4]triazolo[4,3-b]pyridazines that are agonists of Rev-Erb. These compounds, and pharmaceutical compositions comprising the same, are suitable means for treating any disease wherein the activation of Rev-Erb has therapeutic effects, for instance in inflammatory and circadian rhythm-related disorders or cardiometabolic diseases.
Design, synthesis, and molecular modelling of pyridazinone and phthalazinone derivatives as protein kinases inhibitors
Elagawany, Mohamed,Ibrahim, Mohamed A.,Ali Ahmed, Hany Emary,El-Etrawy, A.Sh.,Ghiaty, Adel,Abdel-Samii, Zakaria K.,El-Feky, Said A.,Bajorath, Juergen
supporting information, p. 2007 - 2013 (2013/05/09)
The design and synthesis of pyridazinone and phthalazinone derivatives are described. Newly synthesized compounds were tested on a panel of four kinases in order to evaluate their activity and potential selectivity. In addition, the promising compounds were tested on four cancer cell lines to examine cytotoxic effects. The compounds inhibited DYRK1A and GSK3 with different activity. SAR analysis and docking calculations were carried out to aid in the interpretation of the results. Taken together, our findings suggest that pyridazinone and phthalazinone scaffolds are interesting starting points for design of potent GSK3 and DYRK1A inhibitors.
SUBSTITUTED IMIDAZO[1,2-B]PYRIDAZINES
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Paragraph 0585, (2013/08/28)
The invention relates to imidazo[1,2-b]pyridazines of general formula (I) a process for their manufacuture and their use for the treatment of benign and malignant neoplasia.
Iron-mediated direct arylation with arylboronic acids through an aryl radical transfer pathway
Wang, Jian,Wang, Shan,Wang, Gao,Zhang, Ji,Yu, Xiao-Qi
supporting information, p. 11769 - 11771 (2013/01/15)
A novel iron-mediated direct C-H arylation of quinones and pyridine analogues with arylboronic acids has been developed using dichloromethane and water as solvents at ambient temperature. FeS is employed and serves as an efficient catalyst. A detailed reaction mechanism is speculated and expounded.
Discovery of pyrrolopyridazines as novel DGAT1 inhibitors
Fox, Brian M.,Iio, Kiyosei,Li, Kexue,Choi, Rebeka,Inaba, Takashi,Jackson, Simon,Sagawa, Shoichi,Shan, Bei,Tanaka, Masahiro,Yoshida, Atsuhito,Kayser, Frank
scheme or table, p. 6030 - 6033 (2010/11/05)
A new structural class of DGAT1 inhibitors was discovered and the structure-activity relationship was explored. The pyrrolotriazine core of the original lead molecule was changed to a pyrrolopyridazine core providing an increase in potency. Further exploration resulted in optimization of the propyl group at C7 and the discovery that the ester at C6 could be replaced by five-membered heterocyclic rings. The analogs prepared have DGAT1 IC 50 values ranging from >10 μM to 48 nM.
SUBSTITUTED HETEROCYCLIC COMPOUNDS AND METHODS OF USE
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Page/Page column 68-69, (2010/10/20)
The present invention relates to pyridines, pyrimidines and derivatives thereof, and pharmaceutically acceptable salts thereof. Also included is a method of treatment of inflammation, rheumatoid arthritis, Pagets disease, osteoporosis, multiple myeloma, uveititis, acute or chronic myelogenous leukemia, pancreatic beta cell destruction, osteoarthritis, rheumatoid spondylitis, gouty arthritis, inflammatory bowel disease, adult respiratory distress syndrome (ARDS), psoriasis, Crohn's disease, allergic rhinitis, ulcerative colitis, anaphylaxis, contact dermatitis, asthma, muscle degeneration, cachexia, Reiter's syndrome, type I diabetes, type II diabetes, bone resorption diseases, graft vs. host reaction, Alzheimer's disease, stroke, myocardial infarction, ischemia reperfusion injury, atherosclerosis, brain trauma, multiple sclerosis, cerebral malaria, sepsis, septic shock, toxic shock syndrome, fever, myalgias due to HIV-1, HIV-2, HIV-3, cytomegalovirus (CMV), influenza, adenovirus, the herpes viruses or herpes zoster infection in a mammal comprising administering an effective amount a compound as described above.