864262-97-5

Upstream product

• 4248-19-5 tert-butyl carbazate 
• 57848-46-1 4-bromo-2-fluorobenzaldehyde 
• 105942-08-3 4-bromo-6-fluorobenzonitrile 
• 24424-99-5 di-tert-butyl dicarbonate 
• 112734-22-2 4-bromo-2-fluorobenzylamine 

Downstream Products

• 1351501-44-4 [2-fluoro-4-(4,4,5,5-tetramethyl-[1,3,2]dioxaborolan-2-yl)benzyl]carbamic acid tert-butyl ester 
• 1371630-45-3 methyl 8-(4-((tert-butoxycarbonylamino)methyl)-3-fluorophenyl)-1-cyclopropyl-9-methyl-4-oxo-4H-quinolizine-3-carboxylate 
• 1371630-46-4 8-(4-((tert-butoxycarbonylamino)methyl)-3-fluorophenyl)-1-cyclopropyl-9-methyl-4-oxo-4H-quinolizine-3-carboxylic acid 
• 1371630-52-2 8-[4-(aminomethyl)-3-fluoro-phenyl]-1-cyclopropyl-9-methyl-4-oxo-quinolizine-3-carboxylic acid 

Relevant academic research and scientific papers

Matrix Metalloproteinase 13 Inhibitors for Modulation of Osteoclastogenesis: Enhancement of Solubility and Stability

Matrix metalloproteinase 13 (MMP-13) activity has been correlated to breast cancer bone metastasis. It has been proposed that MMP-13 contributes to bone metastasis through the promotion of osteoclastogenesis. To explore the mechanisms of MMP-13 action, we previously described a highly efficacious and selective MMP-13 inhibitor, RF036. Unfortunately, further pursuit of RF036 as a probe of MMP-13 in vitro and in vivo activities was not practical due to the limited solubility and stability of the inhibitor. Our new study has explored replacing the RF036 backbone sulfur atom and terminal methyl group to create inhibitors with more favorable pharmacokinetic properties. One compound, designated inhibitor 3, in which the backbone sulfur and terminal methyl group of RF036 were replaced by nitrogen and oxetane, respectively, had comparable activity, selectivity, and membrane permeability to RF036, while exhibiting greatly enhanced solubility and stability. Inhibitor 3 effectively inhibited MMP-13-mediated osteoclastogenesis but spared collagenolysis, and thus represents a next-generation MMP-13 probe applicable for in vivo studies of breast cancer metastasis.

STAT DEGRADERS AND USES THEREOF

The present invention provides compounds, compositions thereof, and methods of using the same.

FERROPTOSIS INHIBITORS–DIARYLAMINE PARA-ACETAMIDES

Provided are compounds that inhibit ferroptosis activity, or modulate or inhibit a disease associated with ferroptosis dysregulation, such as neuropathy, ischemia reperfusion injury, acute kidney failure and cancer, including corresponding sulfonamides, and pharmaceutically acceptable salts, hydrates and stereoisomers thereof. The compounds are employed in pharmaceutical compositions, and methods of making and use, including treating a person in need thereof with an effective amount of the compound or composition, and detecting a resultant improvement in the person's health or condition.

A Facile Synthesis of Ligands for the von Hippel-Lindau E3 Ligase

The proteolysis-targeting chimeras (PROTACs) have become an integral part of different stages of drug discovery. This growing field, therefore, benefits from advancements in all segments of the design of these compounds. Herein, an efficient and optimized synthetic protocol to various von Hippel-Lindau (VHL) ligands is presented, which enables easy access to multigram quantities of these essential PROTAC building blocks. Moreover, the elaborated synthesis represents a straightforward approach to further explore the chemical space of VHL ligands.

PYRROLE AND PYRAZOLE COMPOUNDS AND METHODS OF USE THEREOF

The disclosure relates to anti-cancer compounds derived from nuclear steroid receptor binders, to products containing the same, as well as to methods of their use and preparation. The present disclosure provides compounds having hormone receptor antagonis

Benzoquinone derivative, pharmaceutical composition, and applications thereof

The invention discloses a benzoquinone derivative, a pharmaceutical composition, and applications thereof. According to the invention, the benzoquinone derivative (I), and the stereoisomer or the pharmaceutically acceptable salt thereof possess a structure disclosed in the invention. The benzoquinone derivative possesses excellent inhibition effect on STAT3 level both in vivo and in vitro, and further, the benzoquinone derivative is capable of inhibiting balling capacity of cancer cells.

NOVEL ANTIBIOTICS AND METHODS OF USING SAME

The present invention includes novel 3,6-diazabicyclo[3.1.1]heptane antibiotic compounds and any salts or solvates thereof. The present invention further includes methods of preparing such compounds, and methods of treating bacterial infection in a subjec

Structure–Activity Relationship Studies on (R)-PFI-2 Analogues as Inhibitors of Histone Lysine Methyltransferase SETD7

SETD7 is a histone H3K4 lysine methyltransferase involved in human gene regulation. Aberrant expression of SETD7 has been associated with various diseases, including cancer. Therefore, SETD7 is considered a good target for the development of new epigenetic drugs. To date, few selective small-molecule inhibitors have been reported that target SETD7, the most potent being (R)-PFI-2. Herein we report structure–activity relationship studies on (R)-PFI-2 and its analogues. A library of 29 structural analogues of (R)-PFI-2 was synthesized and evaluated for inhibition of recombinantly expressed human SETD7. The key interactions were found to be a salt bridge and a hydrogen bond formed between (R)-PFI-2′s NH2+ group and SETD7′s Asp256 and His252 residue, respectively.

Development of matrix metalloproteinase-13 inhibitors – A structure-activity/structure-property relationship study

A structure-activity/structure-property relationship study based on the physicochemical as well as in vitro pharmacokinetic properties of a first generation matrix metalloproteinase (MMP)-13 inhibitor (2) was undertaken. After systematic variation of inhi

HETEROARYL COMPOUNDS AS BTK INHIBITORS AND USES THEREOF

The present invention relates to imidazo pyridine compounds, and pharmaceutically acceptable compositions thereof, useful as BTK inhibitors.