104670-74-8Relevant articles and documents
Phenanthridin-6-one derivatives as the first class of non-steroidal pharmacological chaperones for Niemann-Pick disease type C1 protein
Fukuda, Hiromitsu,Karaki, Fumika,Dodo, Kosuke,Noguchi-Yachide, Tomomi,Ishikawa, Minoru,Hashimoto, Yuichi,Ohgane, Kenji
, p. 2781 - 2787 (2017)
Niemann-Pick disease type C is a fatal, progressive neurodegenerative disease mostly caused by mutations in Nieamnn-Pick type C1 (NPC1), a late endosomal membrane protein that is essential for intracellular cholesterol transport. The most prevalent mutation, I1061T (Ile to Thr), interferes with the protein folding process. Consequently, mutated but intrinsically functional NPC1 proteins are prematurely degraded via proteasome, leading to loss of NPC1 function. Previously, we reported sterol derivatives as pharmacological chaperones for NPC1, and showed that these derivatives can normalize folding-defective phenotypes of I1061T NPC1 mutant by directly binding to, and stabilizing, the protein. Here, we report a series of compounds containing a phenanthridin-6-one scaffold as the first class of non-steroidal pharmacological chaperones for NPC1. We also examined their structure-activity relationships.
QUINOXALINE DERIVATIVES
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Page/Page column 65, (2021/07/24)
The present invention relates to compounds according to general formula (I), which act as modulators of the glucocorticoid receptor and can be used in the treatment and/or prophylaxis of disorders which are at least partially mediated by the glucocorticoid receptor.
Biphenyl compound as well as preparation method and medical application thereof
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Paragraph 0297-0303; 0579-0585, (2020/11/22)
The invention discloses a biphenyl compound as well as a preparation method and medical application thereof, the structure of the biphenyl compound is shown as a formula (I) or a formula (II), and thebiphenyl compound or pharmaceutically acceptable salt, tautomer, meso-isomer, raceme, stereoisomer, metabolite, metabolite precursor, prodrug or solvate thereof is a PD-L1 inhibitor. The compound hasa remarkable inhibiting effect on the interaction of PD-1 and PD-L1 protein, so that the compound can be applied to the preparation of PD-L1 inhibitors and immunomodulator drugs for preventing or treating tumors, autoimmune diseases, organ transplant rejection, infectious diseases and inflammatory diseases.
SUBSTITUTED TRIAZOLO QUINOXALINE DERIVATIVES
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Page/Page column 85, (2020/02/14)
The present invention relates to compounds according to general formula (I) which act as modulators of the glucocorticoid receptor and can be used in the treatment and/or prophylaxis of disorders which are at least partially mediated by the glucocorticoid receptor.
HERBICIDAL CINNOLINIUM COMPOUNDS
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Page/Page column 69, (2020/07/14)
Compounds of the formula (I) wherein the substituents are as defined in claim 1, useful as a pesticides, especially as herbicides.
Discovery of VU6027459: A First-in-Class Selective and CNS Penetrant mGlu7Positive Allosteric Modulator Tool Compound
Reed, Carson W.,Kalbfleisch, Jacob J.,Wong, Madison J.,Washecheck, Jordan P.,Hunter, Ashton,Rodriguez, Alice L.,Blobaum, Anna L.,Conn, P. Jeffrey,Niswender, Colleen M.,Lindsley, Craig W.
supporting information, p. 1773 - 1779 (2020/10/19)
Herein, we report the discovery of the first selective and CNS penetrant mGlu7 PAM (VU6027459) derived from a "molecular switch"within a selective mGlu7 NAM chemotype. VU6027459 displayed CNS penetration in both mice (Kp = 2.74) and rats (Kp= 4.78), it was orally bioavailable in rats (%F = 69.5), and undesired activity at DAT was ablated.
Benzoxadiazole compound and preparation method and medical use thereof
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Paragraph 0216-0222, (2019/06/07)
The invention discloses a benzoxadiazole compound and a preparation method and medical use thereof. The benzoxadiazole compound has the general structure shown in formula (I). The compound or pharmaceutically acceptable salts, tautomers, mesomers, racemates, stereoisomers, metabolites, metabolic precursors, prodrugs or solvates of the benzoxadiazole compound have an obvious inhibiting effect on PD-1/PD-L1 protein-protein interaction, so that the benzoxadiazole compound shown in the description can be applied to the preparation of an inhibitor with a PD-1/ PD-L1 inhibitory activity and the immunotherapy of tumors as an immunocheckpoint inhibitor.
EBNA1 INHIBITORS AND THEIR METHOD OF USE
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Paragraph 0253-0254; 0413, (2015/06/03)
Pharmaceutical compositions of the invention comprise EBNA1 inhibitors useful for the treatment of diseases caused by EBNA1 activity such as cancer, infectious mononucleosis, chronic fatigue syndrome, multiple sclerosis, systemic lupus erythematosus and rheumatoid arthritis. Pharmaceutical compositions of the invention also comprise EBNA1 inhibitors useful for the treatment of diseases caused by latent Epstein-Barr Virus (EBV) infection. Pharmaceutical compositions of the invention also comprise EBNA1 inhibitors useful for the treatment of diseases caused by lytic Epstein-Barr Virus (EBV) infection.
Ammonium chloride-catalyzed one-pot synthesis of 4(3H)-quinazolinones under solvent-free conditions
Huang, Guoli,Liu, Bo,Teng, Mingyu,Chen, Yegao
supporting information, p. 1786 - 1794 (2014/06/09)
Ammonium chloride, which is a very inexpensive and readily available reagent, can efficiently catalyze three-component, one-pot condensation reactions of 2-amino-benzoic acid esters, ortho esters, and aromatic amines to afford the corresponding 4(3H)-quinazolinones in good to excellent yields under solvent-free conditions.
Synthesis and biological evaluation of thieno[3,2-d]- pyrimidinones, thieno[3,2-d]pyrimidines and quinazolinones: Conformationally restricted 17β-hydroxysteroid dehydrogenase type 2 (17β-HSD2) inhibitors
Perspicace, Enrico,Marchais-Oberwinkler, Sandrine,Hartmann, Rolf W.
, p. 4487 - 4509 (2013/06/05)
In this study, a series of conformationally restricted thieno[3,2-d] pyrimidinones, thieno[3,2-d]pyrimidines and quinazolinones was designed and synthesized with the goal of improving the biological activity as 17β-hydroxysteroid dehydrogenase type 2 inhi