91983-31-2Relevant academic research and scientific papers
WDR5-MYC INHIBITORS
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Paragraph 00494; 00554-00555; 00804-00805; 001066-001067, (2021/02/05)
Substituted N-phenyl sulfonamide compounds inhibit WDR5-MYC interactions, and the compounds and their pharmaceutical compositions are useful for treating disorders and conditions in a subject, such as cancer cell proliferation.
Novel aminopyrimidine EGFR inhibitor
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Paragraph 3668-3673, (2021/03/24)
The present invention provides a novel aminopyrimidine compound that is a selective inhibitor of the fourth generation EGFR (T790M/C797S mutation), a pharmaceutical composition containing the compound, a useful intermediate for preparing the compound, and
DUAL ATM AND DNA-PK INHIBITORS FOR USE IN ANTI-TUMOR THERAPY
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Page/Page column 390; 391, (2019/11/12)
Provided herein are compounds of the Formula (I), (II), and (III), as well as pharmaceutically acceptable salts thereof, wherein the substituents are those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of oncologic diseases.
Discovery and Optimization of Salicylic Acid-Derived Sulfonamide Inhibitors of the WD Repeat-Containing Protein 5-MYC Protein-Protein Interaction
Macdonald, Jonathan D.,Chacón Simon, Selena,Han, Changho,Wang, Feng,Shaw, J. Grace,Howes, Jennifer E.,Sai, Jiqing,Yuh, Joannes P.,Camper, Demarco,Alicie, Bethany M.,Alvarado, Joseph,Nikhar, Sameer,Payne, William,Aho, Erin R.,Bauer, Joshua A.,Zhao, Bin,Phan, Jason,Thomas, Lance R.,Rossanese, Olivia W.,Tansey, William P.,Waterson, Alex G.,Stauffer, Shaun R.,Fesik, Stephen W.
, p. 11232 - 11259 (2019/12/25)
The treatment of tumors driven by overexpression or amplification of MYC oncogenes remains a significant challenge in drug discovery. Here, we present a new strategy toward the inhibition of MYC via the disruption of the protein-protein interaction betwee
Benzoheterocycle-carboxamide-pyridone derivatives and preparation method and applications thereof
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, (2018/03/26)
The invention belongs to the field of chemical medicine preparation, and concretely relates to benzoheterocycle-carboxamide-pyridone derivatives, a preparation method and applications thereof. The invention provides the benzoheterocycle-carboxamide-pyridone derivatives, and a structure is represented by a formula I. The present invention also provides the preparation method and the applications ofthe above benzoheterocycle-carboxamide-pyridone derivatives. The benzoheterocycle-carboxamide-pyridone derivatives provided by the invention are novel compounds obtained on the basis of a large number of screening, inhibit EZH2 activity, and provide a novel selection for development and application of medicines for resisting tumors and autoimmune diseases.
BENZOXAZOLE CARBOXAMIDE INHIBITORS OF POLY(ADP-RIBOSE)POLYMERASE (PARP)
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Page/Page column 56, (2009/08/16)
A compound having the structure set forth in Formula (I) or Formula (II): wherein the variables Y, R1, R2, R3, and R4 are as defined herein. Provided herein are inhibitors of poly(ADP-ribose)polymerase activity. Also described herein are pharmaceutical compositions that include at least one compound described herein and the use of a compound or pharmaceutical composition described herein to treat diseases, disorders and conditions that are ameliorated by the inhibition of PARP activity.
Synthesis and pharmacology of 3,4-dihydro-3-oxo-1,4-benzoxazine-8-carboxamide derivatives, a new class of potent serotonin-3 (5-HT3) receptor antagonists
Kawakita,Kuroita,Yasumoto,Sano,Inaba,Fukuda,Tahara
, p. 624 - 630 (2007/10/02)
A series of 3,4-dihydro-3-oxo-1,4-benzoxazine-8-carboxamide derivatives was synthesized and evaluated for serotonin-3 (5-HT3) receptor antagonistic activity assessed by their ability to antagonize the von Bezold-Jarish (BJ) effect in rats. Derivatives bearing 1-azabicyclo[2.2.2]oct-3-yl moiety as a basic function attached to the carboxamide at position 8 showed more potent antagonistic activity than those bearing the other three basic moieties. Structure activity relationships of this series showed that methyl and chloro groups were more effective as substituents at positions 4 and 6, respectively. The representative compound 15 (Y-25130) in this series showed potent antagonistic activity on the BJ effect (ED50 = 1.3 μg/kg i.v.), high affinity for 5-HT3 receptor (K(i) = 2.9 nM) and complete protection against cisplatin-induced emesis in dogs at a dose of 0.1 mg/kg i.v.
