586412-86-4Relevant academic research and scientific papers
TYK2 INHIBITORS AND USES THEREOF
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Paragraph 00359, (2020/09/27)
Described herein are compounds that are useful in treating a TYK2-mediated disorder. In some embodiments, the TYK2-mediated disorder is an autoimmune disorder, an inflammatory disorder, a proliferative disorder, an endocrine disorder, a neurological disorder, or a disorder associated with transplantation.
COMPOUNDS AND METHODS FOR THE TARGETED DEGRADATION OF INTERLEUKIN-1 RECEPTOR-ASSOCIATED KINASE 4 POLYPEPTIDES
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Paragraph 1689-1690, (2019/06/07)
The present disclosure relates to bifunctional compounds, which find utility as modulators of Interleukin-1 Receptor-Associated Kinase 4 (IRAK-4); the target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a Von Hppel-Lindau, cereblon, ligand which binds to the E3 ubiquitin ligase and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.
BENZO[b]THIOPHENE COMPOUNDS AS STING AGONISTS
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Paragraph 0515; 0516, (2018/04/18)
Compounds of general formula (Ia), compounds of general formula (Ia′), compounds of general formula (Ib), compounds of general formula (Ib′), compounds of general formula (I), compounds of general formula (I′), and their pharmaceutically acceptable salts,
HETEROCYCLIC DERIVATIVES AND USE THEREOF
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Page/Page column 19; 20, (2016/06/28)
A heterocyclic derivative represented by formula (I), or a pharmaceutically acceptable salt or a stereoisomer thereof, which has an inhibitory effect on the activation of STAT3 protein, and is useful for the prevention or treatment of diseases associated
3,4-Dihydro-2H-benzoxazinones as dual-acting 5-HT1A receptor antagonists and serotonin reuptake inhibitors
Lovell, Peter J.,Blaney, Frank E.,Goodacre, Caroline J.,Scott, Claire M.,Smith, Paul W.,Starr, Kathryn R.,Thewlis, Kevin M.,Vong, Antonio K.K.,Ward, Simon E.,Watson, Jeannette M.
, p. 1033 - 1036 (2007/10/03)
Investigation of halogen substitution in lead compound 1 has led to the identification of analogues which combine high affinity for 5-HT1A receptors and potent serotonin reuptake inhibitory activity. Several compounds show an improved selectivity over 5-HT1B and 5-HT1D receptors and a superior pharmacokinetic profile in the rat.
BENZOXAZINONE DERIVATIVE
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Page/Page column 8-9, (2010/02/07)
The compound 6-(4-(1-(2-(5-(7-Fluoro-2-methyl)quinolinyloxy)ethyl)piperidinyl)methyl)-7-fluoro-4H-benzo[1,4]oxazin-3-one and pharmaceutically acceptable salts thereof are disclosed. Methods of preparation and use in therapy, particularly for a CNS disorde
