1425045-01-7Relevant articles and documents
Structure-Based Design of an in Vivo Active Selective BRD9 Inhibitor
Martin, Laetitia J.,Koegl, Manfred,Bader, Gerd,Cockcroft, Xiao-Ling,Fedorov, Oleg,Fiegen, Dennis,Gerstberger, Thomas,Hofmann, Marco H.,Hohmann, Anja F.,Kessler, Dirk,Knapp, Stefan,Knesl, Petr,Kornigg, Stefan,Müller, Susanne,Nar, Herbert,Rogers, Catherine,Rumpel, Klaus,Schaaf, Otmar,Steurer, Steffen,Tallant, Cynthia,Vakoc, Christopher R.,Zeeb, Markus,Zoephel, Andreas,Pearson, Mark,Boehmelt, Guido,McConnell, Darryl
, p. 4462 - 4475 (2016)
Components of the chromatin remodelling switch/sucrose nonfermentable (SWI/SNF) complex are recurrently mutated in tumors, suggesting that altering the activity of the complex plays a role in oncogenesis. However, the role that the individual subunits play in this process is not clear. We set out to develop an inhibitor compound targeting the bromodomain of BRD9 in order to evaluate its function within the SWI/SNF complex. Here, we present the discovery and development of a potent and selective BRD9 bromodomain inhibitor series based on a new pyridinone-like scaffold. Crystallographic information on the inhibitors bound to BRD9 guided their development with respect to potency for BRD9 and selectivity against BRD4. These compounds modulate BRD9 bromodomain cellular function and display antitumor activity in an AML xenograft model. Two chemical probes, BI-7273 (1) and BI-9564 (2), were identified that should prove to be useful in further exploring BRD9 bromodomain biology in both in vitro and in vivo settings.
PYRIDINONE COMPOUNDS FOR THE TREATMENT OF AUTOIMMUNE DISEASE
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Page/Page column 20; 21, (2022/02/15)
The present invention relates to compounds of formula (I), (I), wherein R1, R2, R3, R4 and A are as described herein, and their pharmaceutically acceptable salt thereof, and compositions including the compounds and methods of using the compounds.
BRD9 BIFUNCTIONAL DEGRADERS AND THEIR METHODS OF USE
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Page/Page column 190, (2021/04/01)
The disclosure provides BRD9 bifunctional compounds of Formula (A) or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, to their preparation, to pharmaceutical compositions comprising them, and to their use in the treatment of diseases and disorders mediated by a bromodomain-containing protein, such as bromodoma in-containing protein 9 (BRD9)
COMPOUNDS AND USES THEREOF
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Page/Page column 262-263, (2020/08/22)
The present invention relates to compositions and methods for the treatment of BAF-related disorders, such as cancers and viral infections.
COMPOUND FUNCTIONING AS BROMODOMAIN PROTEIN INHIBITOR, AND COMPOSITION
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Paragraph 0194; 0195, (2020/11/22)
The invention relates to a bromodomain inhibitor. The invention also provides compositions and formulations comprising such compounds, and methods of using and preparing such compounds.
BET protein inhibitor and preparation method and application thereof
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Paragraph 0119-0124, (2019/07/29)
The invention belongs to the technical field of biological medicine, and particularly relates to a BET protein inhibitor and a preparation method and application thereof. Compared with the prior art,structural improvement is further conducted on the basis
NOVEL TRICYCLIC COMPOUNDS
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, (2019/05/15)
This invention relates to certain novel tricyclic compounds as bromodomain and extra-terminal (BET) inhibitors, their synthesis and their use for treating diseases. More particularly, this invention is directed to fused heterocyclic derivatives useful as
New Pyridinones and Isoquinolinones as Inhibitors of the Bromodomain BRD9
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, (2018/03/25)
The present invention encompasses compounds of general formula (I) wherein the groups R1 to R9, X1 and X2 have the meanings given in the claims and in the specification. The compounds of the invention are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation, e.g. cancer, pharmaceutical preparations containing such compounds and their uses as a medicament.
METHODS OF USING SUBSTITUTED PYRAZOLE AND PYRAZOLE COMPOUNDS AND FOR TREATMENT OF HYPERPROLIFERATIVE DISEASES
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Paragraph 693; 694, (2018/06/21)
Disclosed are methods of treating hyperproliferative disorders such as cancer, methods of arresting the cell cycle in cancer cells, methods of inhibiting glutathione synthesis in cancer cells, and associated compounds for use and uses in medicaments. In certain embodiments, the methods, uses and compounds are provided with reference to compounds of the structural formula (I), in which X1, X2, Z1, Z2, the ring system denoted by "a", R1, L1, L2, Q, L3, R3, L4, R4, L5, and R5 are as described herein. In certain embodiments, compounds disclosed herein are especially active against cancers having a mutant KRAS gene.
Iridium-Catalyzed Site-Selective C-H Borylation of 2-Pyridones
Miura, Wataru,Hirano, Koji,Miura, Masahiro
, p. 4745 - 4752 (2017/09/30)
An iridium-catalyzed site-selective C-H borylation of 2-pyridones has been developed. The site selectivity is predominantly controlled by steric factors, and we can access C4, C5, and C6 C-H on the 2-pyridone ring by the judicious choice of ligand and sol
