50508-66-2

Usage

Uses

Used in Organic Synthesis:
2-Amino-3-(p-chlorobenzoyl)-4,5-dimethylthiophene is used as a key intermediate in the synthesis of various organic compounds. Its unique structural features allow for the formation of diverse chemical entities through reactions such as substitution, condensation, and cyclization.
Used in Pharmaceutical Research:
In the pharmaceutical industry, 2-Amino-3-(p-chlorobenzoyl)-4,5-dimethylthiophene is utilized as a potential lead compound for the development of new drugs. Its structural features and pharmacological properties make it a promising candidate for the treatment of various diseases and disorders. Researchers can modify its structure to optimize its biological activity, selectivity, and pharmacokinetic properties, leading to the discovery of novel therapeutic agents.

Upstream product

• 78-93-3 butanone 
• 4640-66-8 p-chlorobenzoylacetonitrile 
• 937-20-2 p-chlorophenacyl chloride 
• 873-76-7 para-Chlorobenzyl alcohol 
• 1126-46-1 Methyl 4-chlorobenzoate 

Downstream Products

• 1268524-66-8 (S)-tert-butyl-3-amino-4-((3-(4-chlorobenzoyl)-4,5-dimethylthiophen-2-yl)amino)-4-oxobutanoate 
• 1268524-67-9 tert-butyl (S)-2-(5-(4-chlorophenyl)-6,7-dimethyl-2-oxo-2,3-dihydro-1H-thieno[2,3-e][1,4]diazepin-3-yl)acetate 
• 1268524-70-4 (S)-tert-butyl 2-(4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)acetate 
• 202592-23-2 (S)-[4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl]acetic acid 

Relevant academic research and scientific papers

Potent Dual BET/HDAC Inhibitors for Efficient Treatment of Pancreatic Cancer

As one of the most aggressive and lethal human malignancies with extremely poor prognosis, there is an urgent demand of more effective therapy for the treatment of pancreatic cancer. Reported here is a new, effective therapeutic strategy and the design of small-molecule inhibitors that simultaneously target bromodomain and extra-terminal (BET) and histone deacetylase (HDAC), potentially serving as promising therapeutic agents for pancreatic cancer. A highly potent dual inhibitor (13 a) is identified to possess excellent and balanced activities against BRD4 BD1 (IC50=11 nm) and HDAC1 (IC50=21 nm). Notably, this compound shows higher in vitro and in vivo antitumor potency than the BET inhibitor (+)-JQ1 and the HDAC inhibitor vorinostat, either alone or and in combination, highlighting the advantages of BET/HDAC dual inhibitors for more effective treatment of pancreatic cancer.

6H-THIENO[2,3-E][1,2,4]TRIAZOLO[3,4-C][1,2,4]TRIAZEPINE DERIVATIVE

The 6H-thieno[2,3-e][1,2,4]triazolo[3,4-c][1,2,4]triazepine derivatives or salts thereof of the present invention have BRD4 inhibitory activity, and thus, they are useful as medicaments, in particular, as prophylaxis and/or therapeutic agents for diseases associated with BRD4.

THIENODIAZEPINE DERIVATIVES AND APPLICATION THEREOF

The present invention relates to a class of thienodiazepine derivatives and an application thereof in the preparation of a drug for the treatment of diseases associated with bromodomain and extra-terminal (BET) Bromodomain inhibitors. Specifically, the present invention relates to compounds represented by formulas (I) and (II), as well as pharmaceutically acceptable salts thereof.

PREPARATION OF CONDENSED TRIAZEPINE DERIVATIVES AND THEIR USE AS BET INHIBITORS

The invention relates to compounds of the formula: and pharmaceutically acceptable salts thereof. These compounds are useful in the treatment of inflammatory diseases, fibtrotic diseases and neoplastic diseases.

PROCESS FOR THE MANUFACTURE OF DIAZEPINE DERIVATIVES

The invention relates to a process for the manufacture of diazepine derivatives as defined in the description and in the claims.

COMPOUNDS AND METHODS FOR THE TARGETED DEGRADATION OF BROMODOMAIN-CONTAINING PROTEINS

The present invention relates to bifunctional compounds, which find utility as modulators of targeted ubiquitination, especially inhibitors of a variety of polypeptides and other proteins which are degraded and/or otherwise inhibited by bifunctional compounds according to the present invention. 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 a target protein such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of that protein. The present invention exhibits a broad range of pharmacological activities associated with compounds according to the present invention, consistent with the degradation/inhibition of targeted polypeptides.

Double HDAC/BRD4 inhibitor and its preparation method and application (by machine translation)

The invention has disclosed a kind of double HDAC/BRD4 inhibitor and its preparation and application, double HDAC/BRD4 inhibitor structural formula such as formula 16 as shown. The invention also discloses the above-mentioned double HDAC/BRD4 inhibitor preparation method and its application in the preparation of medicament. This invention, through the Linker HDAC inhibitors with the pharmacophore BRD4 inhibitor potency of splicing group, with a double HDAC/BRD4 inhibiting effect of the novel dual-HDAC/BRD4 inhibitor. The preparation method of this invention is simple, mild condition, it is easy to realize. (by machine translation)

BROMODOMAIN-INHIBITING COMPOUNDS AND PHARMACEUTICAL COMPOSITION COMPRISING SAME FOR PREVENTING OR TREATING A CANCER

Provided is a novel compound having bromodomain and extra terminal domain (BET) protein inhibiting activities, and a pharmaceutical composition comprising the same which can be useful for prevention or treatment of precancerous transformation or cancer.

Preparation of small-molecule microarrays by trans-cyclooctene tetrazine ligation and their application in the high-throughput screening of protein-protein interaction inhibitors of bromodomains

Fast and efficient: A library of trans-cyclooctene (TCO)-modified small molecules were immobilized on tetrazine-functionalized glass slides by using the fastest bioorthogonal reaction known. The resulting small-molecule microarray was screened against a variety of human bromodomains to identify protein-protein interaction inhibitors. Copyright