2103656-92-2Relevant academic research and scientific papers
Chemoselective Synthesis of Lenalidomide-Based PROTAC Library Using Alkylation Reaction
Qiu, Xing,Sun, Ning,Kong, Ying,Li, Yan,Yang, Xiaobao,Jiang, Biao
, p. 3838 - 3841 (2019)
An organic base-promoted chemoselective alkylation of lenalidomide with different halides was developed, which offers a novel approach to a highly functionalized lenalidomide-based PROTAC library under mild reaction conditions. DIPEA was found to act as an efficient base to trigger facile generation of arylamine alkylation products compared with inorganic bases. This library was successfully applied to BET PROTAC, which not only degraded BET protein but also effectively inhibited cancer cell proliferation.
MOLECULES AND METHODS RELATED TO TREATMENT OF UNCONTROLLED CELLULAR PROLIFERATION
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Paragraph 00444, (2021/02/05)
The present disclosure relates to chemical compounds that modulate cellular proliferation for the treatment of uncontrolled cellular proliferation disorders (such as cancer), pharmaceutical compositions containing such compounds, and their use in treatment. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INIDBITORS WITH E3 LIGASE LIGAND AND METHODS OF USE
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Paragraph 0261; 0263, (2021/02/05)
Disclosed herein are novel bifunctional compounds formed by conjugating BTK inhibitor moieties with E3 ligase Ligand moieties, which function to recruit targeted proteins to E3 ubiquitin ligase for degradation, and methods of preparation and uses thereof.
TARGETED UBIQUITINATION DEGRADATION BRD4 PROTEIN COMPOUND, PREPARATION METHOD THEREFOR AND APPLICATION THEREOF
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Paragraph 0063; 0065, (2021/12/18)
The present invention relates to a compound represented by formula (I) or a tautomer, optical isomer, deuterated substance, oxynitride, solvate, pharmaceutically acceptable salt or prodrug thereof, a preparation method for the compound, a pharmaceutical c
Process for the preparation of lenalidomide derivatives (by machine translation)
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Paragraph 0084-0085, (2020/01/08)
The present disclosure relates to processes (I) for the preparation, of compounds of: formula (II) I, comprising the selective (III) hydrogenation of the amino groups of the compounds of formula, I with the (I) compound. of formula I in the (I) presence. of an organic base in the presence of an organic base to give the compound of the formula IV wherein the present disclosure also relates to the compound of the formula IV. R1 LIN (LIN (III).) (by machine translation)
ALK (anaplastic lymphoma kinase) protein degradation agent and anti-tumor application thereof
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Paragraph 0449-0451, (2019/07/04)
The invention discloses a compound in a formula (I) and an anti-tumor application thereof. The compound in the formula (I) has degradation and inhabitation functions on ALK target protein and mainly comprises four parts, the first part ALK-TKIs is a compound with ALK tyrosine kinase inhabitation activity; the second part LIN is different linkers; the third part ULM (ubiquitin ligase binding moiety) of VHL, CRBN or other protease micromolecular ligand with a ubiquitination function; the fourth part group A is carboxyl or deficiency and covalently binds ALK-TKIs with LIN and covalently binds LINwith ULM. A series of designed and synthesized compounds have wide pharmacological activity, have functions of degrading ALK protein and inhibiting ALK activity and can be applied to related tumor therapy.
COMPOSITIONS AND METHODS FOR TREATING CDK4/6-MEDIATED CANCER
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Page/Page column 85; 127; 128, (2018/06/30)
Methods for designing heterobifunctional small molecules which selectively degrade/disrupt CDK4/6 and compositions and methods of using such degraders/disruptors to treat CDK4/6-mediated cancer are provided.
