156001-53-5Relevant academic research and scientific papers
IMMUNOMODULATORS, COMPOSITIONS AND METHODS THEREOF
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Page/Page column 103, (2020/08/22)
Provided herein are compounds of Formula (I), methods of using the compounds as immunomodulators, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections.
Discovery of BIIB068: A Selective, Potent, Reversible Bruton's Tyrosine Kinase Inhibitor as an Orally Efficacious Agent for Autoimmune Diseases
Ma, Bin,Bohnert, Tonika,Otipoby, Kevin L.,Tien, Eric,Arefayene, Million,Bai, Judy,Bajrami, Bekim,Bame, Eris,Chan, Timothy R.,Humora, Michael,Macphee, J. Michael,Marcotte, Douglas,Mehta, Devangi,Metrick, Claire M.,Moniz, George,Polack, Evelyne,Poreci, Urjana,Prefontaine, Annick,Sheikh, Sarah,Schroeder, Patricia,Smirnakis, Karen,Zhang, Lei,Zheng, Fengmei,Hopkins, Brian T.
supporting information, p. 12526 - 12541 (2020/12/17)
Autoreactive B cell-derived antibodies form immune complexes that likely play a pathogenic role in autoimmune diseases. In systemic lupus erythematosus (SLE), these antibodies bind Fc receptors on myeloid cells and induce proinflammatory cytokine producti
BIARYL COMPOUND, PREPARATION METHOD AND USE THEREFOR
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Paragraph 0051-0052; 0257-0258, (2020/01/02)
The present invention belongs to the technical field of chemical pharmaceuticals, and relates to a compound represented by general formula (I) or formula (II) and a preparation method thereof. The compounds are biaryl derivatives with RORγt activation activity. The biaryl derivatives disclosed in this invention can effectively activate the RORγt protein receptor, and thereby promote the differentiation of Th17 cells and increasing the production of IL-17, which can be used as an immune modulator for the treatment of various cancers or viral infection-related diseases.
BRM TARGETING COMPOUNDS AND ASSOCIATED METHODS OF USE
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Paragraph 1476-1478, (2019/10/23)
The present disclosure relates to bifunctional compounds, which find utility as modulators of SMARCA2 or BRM (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a ligand that binds to the Von Hippel-Lindau 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.
APOPTOSIS SIGNAL-REGULATING KINASE INHIBITORS AND USES THEREOF
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Paragraph 00423, (2019/04/09)
Described herein are ASK1 inhibitors and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for the treatment of blood disease, autoimmune disorders, pulmonary disorders, hypertension, inflammatory diseases, fibrotic diseases, diabetes, diabetic nephropathy, renal diseases, respiratory diseases, cardiovascular diseases, acute lung injuries, acute or chronic liver diseases, and neurodegenerative diseases.
From RORλt Agonist to Two Types of RORλt Inverse Agonists
Wang, Yonghui,Cai, Wei,Tang, Ting,Liu, Qian,Yang, Ting,Yang, Liuqing,Ma, Yingli,Zhang, Guifeng,Huang, Yafei,Song, Xiaoxia,Orband-Miller, Lisa A.,Wu, Qianqian,Zhou, Ling,Xiang, Zhijun,Xiang, Jia-Ning,Leung, Stewart,Shao, Liming,Lin, Xichen,Lobera, Mercedes,Ren, Feng
supporting information, p. 120 - 124 (2018/02/19)
Biaryl amides as new RORλt modulators were discovered. The crystal structure of biaryl amide agonist 6 in complex with RORλt ligand binding domain (LBD) was resolved, and both "short" and "long" inverse agonists were obtained by removing from 6 or adding
TETRAHYDRO-PYRIDO[3,4-b]INDOLE ESTROGEN RECEPTOR MODULATORS AND USES THEREOF
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Paragraph 0464; 0465, (2018/01/18)
Described herein are tetrahydro-pyrido[3,4-b]indol-1-yl compounds with estrogen receptor modulation activity or function having the Formula I structure: and stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, and with the substituents and structural features described herein. Also described are pharmaceutical compositions and medicaments that include the Formula I compounds, as well as methods of using such estrogen receptor modulators, alone and in combination with other therapeutic agents, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.
Modulators of the nuclear hormone receptor ROR
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Page/Page column 163; 164, (2017/03/28)
The invention provides small molecule modulators of retinoic acid receptor-related orphan receptors such as RORα, RORβ, or RORγ, of formula with the variable atoms as defined herein and R1 comprising a hydroxyl- or alkoxyl-substituted fluoroalkyl group. Compounds of the invention can be effective modulators at concentrations ineffective to act on LXR receptors, or on other nuclear receptors, or other biological targets. Methods of modulation the RORs and methods of treating metabolic disorders, immune disorders, cancer, and CNS disorders wherein modulation of an ROR is medically indicated are also provided.
TBK/IKK INHIBITOR COMPOUNDS AND USES THEREOF
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Paragraph 0341; 0342, (2017/01/23)
The present invention relates to compounds of Formula I and pharmaceutically acceptable compositions thereof, useful as TBK/IKKε inhibitors.
BIARYL COMPOUNDS USEFUL FOR THE TREATMENT OF HUMAN DISEASES IN ONCOLOGY, NEUROLOGY AND IMMUNOLOGY
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Paragraph 0206, (2015/06/25)
The present invention provides compounds and compositions thereof which are useful as inhibitors of Bruton's tyrosine kinase and which exhibit desirable characteristics for the same.
