190330-64-4Relevant academic research and scientific papers
NUCLEIC ACID-BINDING PHOTOPROBES AND USES THEREOF
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Paragraph 0043, (2019/06/17)
The present invention relates to photoactivatable compounds and methods of use thereof for determining binding site and other structural information about RNA transcripts. The invention also provides methods of identifying RNA transcripts that bind compounds and are thus druggable, methods of screening drug candidates, and methods of determining drug binding sites and/or accessible or reactive sites on a target RNA.
Compound of benzyl structure and application of compound
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Paragraph 0195; 0200; 0201, (2019/10/01)
The invention discloses a compound of a benzyl structure and application of the compound. The compound of the benzyl structure comprises hydroxyl, amino, substituted amino and active groups, and can be used as an amino acid or peptide C-end protection reagent. A peptide synthesis reaction using the protection carrier is rapid in reaction speed and high in reagent utilization rate in an appropriatesolvent system; effective purification can be implemented through simple liquid-liquid extraction separation in post-processing, and a product of high purity can be finally obtained; and in the synthesis process, the dissolution degree is slightly changed, the operation process is good in universality, and a universal production method can be developed.
Compound containing fluorene ring structure, and application thereof
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Paragraph 0184, (2019/10/04)
The present invention discloses a compound containing a fluorene ring structure, and an application thereof. The compound containing the fluorene ring structure of the present invention contains a hydroxyl group, an amino group, a substituted amino group and an active group, and can be used as an amino acid or peptide C-terminal protection reagent. The above peptide using a protective carrier has a high reaction speed and a high reagent utilization rate in a suitable solvent system when used in a reaction; post-treatment is carried out by simple liquid-liquid extraction separation to achieve effective purification, so the product with a high purity is finally obtained; and the compound has a small solubility change in the synthesis process, and the operating flow has high versatility, so a synthesis method of the compound can be developed into a universal production method.
Method for preparing ethylene glycol compounds
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Paragraph 0080-0082; 0112; 0113; 0114; 0115, (2018/12/02)
The invention provides a method for preparing ethylene glycol compounds. The preparation method is short in route, the yield is high, and the operation is simple, Compounds VIII and IX serve as intermediates for preparing the ethylene glycol compounds in the invention, and the ethylene glycol compounds disclosed by the invention are prepared by taking the compounds VIII and IX as the intermediates. The method is high in yield, high in purity and suitable for industrial production.
INDOLE DERIVATIVES AS ESTROGEN RECEPTOR DEGRADERS
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Paragraph 0381; 0382, (2018/04/21)
The present disclosure relates to compounds and a pharmaceutically acceptable salt thereof, compositions, combinations and medicaments containing the compounds, and processes for their preparation. The disclosure also relates to the use of the compounds, combinations, compositions and medicaments, for example as inhibitors of the activity of the estrogen receptor, including degrading the estrogen receptor, the treatment of diseases and conditions mediated by the estrogen receptor.
COMPOUNDS AND METHODS FOR THE TARGETED DEGRADATION OF ANDROGEN RECEPTOR
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Paragraph 0795-0796, (2018/04/20)
The present disclosure relates to bifunctional compounds, which find utility to degrade and (inhibit) Androgen Receptor. In particular, the present disclosure is directed to compounds, which contain on one end a cereblon ligand which binds to the E3 ubiquitin ligase and on the other end a moiety which binds Androgen Receptor, such that Androgen Receptor is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of Androgen Receptor. The present disclosure exhibits a broad range of pharmacological activities associated with compounds according to the present disclosure, consistent with the degradation/inhibition of Androgen Receptor.
COMPOUNDS AND METHODS FOR MODULATING RNA FUNCTION
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Paragraph 0069; 0070; 00629, (2018/02/28)
The present invention provides compounds, compositions thereof, and methods of using the same.
Design and synthesis of aminoester heterodimers containing flavone or chromone moieties as modulators of P-glycoprotein-based multidrug resistance (MDR)
Dei, Silvia,Romanelli, Maria Novella,Manetti, Dina,Chiaramonte, Niccolò,Coronnello, Marcella,Salerno, Milena,Teodori, Elisabetta
, p. 50 - 64 (2017/11/29)
In this study, a new series of heterodimers was synthesized. These derivatives are N,N-bis(alkanol)amine aryl esters or N,N-bis(ethoxyethanol)amine aryl esters carrying a methoxylated aryl residue combined with a flavone or chromone moiety. The new compounds were studied to evaluate their P-gp modulating activity on a multidrug-resistant leukemia cell line. Some of the new compounds show a good MDR reversing activity; interestingly this new series of compounds does not comply with the structure-activity relationships (SAR) outlined by previously synthesized analogs carrying different aromatic moieties. In the case of the compounds described in this paper, activity is linked to different features, in particular the characteristics of the spacer, which seem to be critical for the interaction with the pump. This fact indicates that the presence of a flavone or chromone residue influences the SAR of these series of products, and that flexible molecules can find different productive binding modes with the P-gp recognition site. These results support the synthesis of new compounds that might be useful leads for the development of drugs to control P-gp-dependent MDR.
COMPOUNDS AND METHODS OF TREATING RNA-MEDIATED DISEASES
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Sheet 98/122, (2017/12/27)
The present invention provides compounds, compositions thereof, and methods of using the same.
COMPOUNDS AND METHODS FOR THE TARGETED DEGRADATION OF THE ANDROGEN RECEPTOR
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Paragraph 0565; 0566; 0567, (2016/08/17)
The present invention relates to bifunctional compounds, which find utility to degrade and (inhibit) Androgen Receptor. In particular, the present invention is directed to compounds, which contain on one end a VHL ligand which binds to the ubiquitin ligase and on the other end a moiety which binds Androgen Receptor such that Androgen Receptor is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of Androgen Receptor. The present invention exhibits a broad range of pharmacological activities associated with compounds according to the present invention, consistent with the degradation/inhibition of Androgen Receptor.
