206265-94-3Relevant academic research and scientific papers
TROPOMYOSIN RECEPTOR KINASE (TRK) DEGRADATION COMPOUNDS AND METHODS OF USE
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Page/Page column 262, (2021/09/04)
This disclosure relates to bivalent compounds (e.g., bi-functional small molecule compounds), compositions comprising one or more of the bivalent compounds, and to methods of use the bivalent compounds for the treatment of certain disease in a subject in need thereof. The disclosure also relates to methods for identifying such bivalent compounds.
Small molecule compound based on EZH2 protein degradation, and application thereof
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Paragraph 0103-0106, (2021/08/07)
The invention discloses a series of small molecule compounds capable of selectively degrading EZH2 protein, and application thereof. The compounds can be prepared into proper pharmaceutical dosage forms for EZH2-mediated related tumor treatment.
Heterocyclic compound and application thereof
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Paragraph 1323-1325; 1328, (2021/08/07)
The invention discloses a heterocyclic compound and application thereof. The invention provides a heterocyclic compound as shown in a formula I, or pharmaceutically acceptable salt thereof. The heterocyclic compound can be used for degrading ALK, c-Met and ROS proteins.
Neem PROTAC compound with STAT3 degradation activity and preparation method and application thereof
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, (2022/01/10)
A NEEM PROTAC compound with STAT3 degradation activity, the structure of which is generally formula (I): Y is a specific protein ligand in the E3 ubiquitin ligase complex, a Cereblon protein ligand or A VHL protein ligand; X is a linking group between nee
IRAK DEGRADERS AND USES THEREOF
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Paragraph 00962; 001134; 001135, (2020/06/19)
The present invention provides compounds, compositions thereof, and methods of using the same.
TROPOMYOSIN RECEPTOR KINASE (TRK) DEGRADATION COMPOUNDS AND METHODS OF USE
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Page/Page column 173, (2020/03/15)
Bivalent compounds, compositions comprising one or more of the bivalent compounds, and methods of use the bivalent compounds for the treatment of certain disease in a subject in need thereof are provided. Methods for identifying such bivalent compounds are provided, either.
Compound for targeted degradation of ALK, c-Met and ROS1 proteins, and preparation method thereof
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Paragraph 0115-0118; 0120, (2020/07/07)
The invention provides a novel compound for targeted degradation of ALK, c-Met and ROS1 proteins, wherein the compound is represented by a formula A, is formed by linking an ubiquitin ligase E3 recognition ligand and an ALK, c-Met and ROS1 protein inhibitor compound through a linking arm, and can selectively induce degradation of ALK, c-Met and ROS1 proteins and mutant proteins of the ALK, c-Met and ROS1 proteins. According to the invention, a bifunctional small molecule is obtained; and in-vitro anti-tumor activity data of the compound show that the compound has high-efficiency anti-tumor activity on conventional tumor cells, has strong inhibition activity on mutant cell strains (BaF3/EML4-ALKG1202R, BaF3/EML4-ALKL1196M and BaF3-TEL-ALK-C1156Y) causing the drug resistance, provides a effective antitumor drug for clinical application, has great application value, brings good news for tumor treatment, especially for some drug-resistant patients, and has important social benefits.
IRAK DEGRADERS AND USES THEREOF
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Paragraph 3971; 3972, (2019/07/10)
The present invention provides compounds, compositions thereof, and methods of using the same.
PROTEIN DEGRADERS AND USES THEREOF
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Paragraph 00396; 00399; 00400, (2019/04/16)
The present invention provides compounds, compositions thereof, and methods of using the same for the targeted degradation of proteins, and the treatment of target protein-mediated disorders.
SUBSTITUTED 1-METHYL-1,2,3,4-TETRAHYDROISOQUINOLINE MOLECULES AS PCSK9 ALLOSTERIC BINDERS
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Page/Page column 107; 108, (2018/04/20)
The present invention relates to PCSK9 allosteric binding compounds of Formula I: (Formula (I)) and pharmaceutically acceptable salts thereof, wherein X1, X2, Y, R1, R2, RA, RB and n are as defined herein. The present invention also relates to compositions which comprise an allosteric binding compound of the invention or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier. The invention further relates, inter alia, to methods for inducing PCSK9 protein degradation in a subject, and methods for treating atherosclerosis, hypercholesterolemia, coronary heart disease, metabolic syndrome, acute coronary syndrome, or related cardiovascular disease and cardiometabolic conditions, comprising administering to a subject an effective amount of a compound or a pharmaceutically acceptable salt of the invention. The invention also provides a means for the in vitro labeling, detection and/or quantification of PCSK9 in biological samples.
