72130-97-3Relevant academic research and scientific papers
PROTEIN SECRETION INHIBITORS
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Paragraph 00410, (2022/03/09)
Provided herein are secretion inhibitors, such as inhibitors of Sec61 for example of Formula (I), methods for their preparation, related pharmaceutical compositions, and method for using the same.
METHODS AND COMPOUNDS FOR RESTORING MUTANT p53 FUNCTION
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Paragraph 0668, (2021/11/20)
Mutations in oncogenes and tumor suppressors contribute to the development and progression of cancer. The present disclosure describes compounds and methods to recover wild-type function to p53 mutants. The compounds of the present disclosure can bind to mutant p53 and restore the ability of the p53 mutant to bind DNA and activate downstream effectors involved in tumor suppression. The disclosed compounds can be used to reduce the progression of cancers that contain a p53 mutation.
COMPOUNDS AND USES THEREOF
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Page/Page column 93-94, (2020/08/22)
The present disclosure features compounds useful for the treatment of BAF complex-related disorders.
In vitro and in vivo characterization of a novel, highly potent p53-MDM2 inhibitor
Vaupel, Andrea,Holzer, Philipp,Ferretti, Stephane,Guagnano, Vito,Kallen, Joerg,Mah, Robert,Masuya, Keiichi,Ruetz, Stephan,Rynn, Caroline,Schlapbach, Achim,Stachyra, Thérèse,Stutz, Stefan,Todorov, Milen,Jeay, Sébastien,Furet, Pascal
supporting information, p. 3404 - 3408 (2018/09/17)
Small molecule inhibitors of the p53-MDM2 protein complex are under intense investigation in clinical trials as anti-cancer agents, including our first generation inhibitor NVP-CGM097. We recently described the rational design of a novel pyrazolopyrrolidinone core as a new lead structure and now we report on the synthesis and optimization of this to provide a highly potent lead compound. This new compound displayed excellent oral efficacy in our preclinical mechanistic in vivo model and marked a significant milestone towards the identification of our second generation clinical candidate NVP-HDM201.
five Yuan fragrance heterocyclic structure containing the anti-hepatitis c compound and its preparation and use
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Paragraph 0087; 0088-0090, (2016/11/21)
The invention discloses an anti-HCV (hepatitis C) compound containing a five-membered heteroaromatic ring structure, as well as a preparation method and applications thereof. The compound has a structure shown as the formula I, the compound has excellent anti-HCV virus activity, can be used for preparing anti-HCV drugs, the prepared drugs can be applied by adopting oral administration, intravenous injection or intramuscular injection.
IMIDAZOPYRAZINONE DERIVATIVES
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Page/Page column 38-39, (2015/07/15)
Compounds of the formula (I) in which R1 and R2 have the meanings indicated in Claim 1, are inhibitors of Tankyrase, and can be employed, inter alia, for the treatment of diseases such as cancer, cardiovascular diseases, central nerv
SUBSTITUTED PURINONE COMPOUNDS
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Page/Page column 64; 65, (2014/08/07)
The invention relates to compounds of formula (I): (I) as described herein, pharmaceutical preparations comprising such compounds, uses and methods of use for such compounds in the treatment of a disorder or a disease mediated by the activity of MDM2 and/or MDM4, and combinations comprising such compounds.
IMIDAZOPYRROLIDINONE DERIVATIVES AND THEIR USE IN THE TREATMENT OF DISEASE
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Page/Page column 62, (2014/12/12)
The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
IMIDAZOLE DERIVATIVES AND THEIR USE FOR MODULATING THE GABA-A RECEPTOR COMPLEX
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Page/Page column 16, (2008/06/13)
This invention relates to novel imidazole derivatives of formula (I), pharmaceutical compositions containing these compounds, and methods of treatment therewith. The compounds of the invention are useful in the treatment of central nervous system diseases and disorders, which are responsive to modulation of the GABAA receptor complex, and in particular for combating anxiety and related diseases.
A concise and regioselective synthesis of 1-alkyl-4-imidazolecarboxylates
Helal, Christopher J.,Lucas, John C.
, p. 4133 - 4134 (2007/10/03)
(formula presented) Reaction between ethyl 3-N,N-(dimethylamino)-2-isocyanoacrylate (1) and a primary amine (2) regioselectively affords 1-alkyl-4-imidazolecarboxylates (3) in good yields (52-89%). The method is applicable to unhindered and hindered amine
