51659-96-2

Upstream product

• 932-22-9 4,5-dichloro-2H-pyridazin-3-one 
• 75-26-3 isopropyl bromide 
• 766-40-5 Mucochloric acid 
• 87-56-9 mucochloric acid 
• 70629-60-6 isopropylhydrazine hydrochloride 

Downstream Products

• 104565-46-0 4-chloro-5-(3-n-propoxy-4-methoxybenzylamino)-2-i-propyl-3(2H)pyridazinone 
• 104565-45-9 4-Chloro-5-(3-benzyloxybenzylamino)-2-i-propyl-3-(2H)pyridazinone 

Relevant academic research and scientific papers

New Design Rules for Developing Potent Cell-Active Inhibitors of the Nucleosome Remodeling Factor (NURF) via BPTF Bromodomain Inhibition

The nucleosome remodeling factor (NURF) alters chromatin accessibility through interactions with its largest subunit,the bromodomain PHD finger transcription factor BPTF. BPTF is overexpressed in several cancers and is an emerging anticancer target. Targeting the BPTF bromodomain presents a potential strategy for its inhibition and the evaluation of its functional significance; however, inhibitor development for BPTF has lagged behind those of other bromodomains. Here we describe the development of pyridazinone-based BPTF inhibitors. The lead compound,BZ1, possesses a high potency (Kd= 6.3 nM) and >350-fold selectivity over BET bromodomains. We identify an acidic triad in the binding pocket to guide future designs. We show that our inhibitors sensitize 4T1 breast cancer cells to doxorubicin but not BPTF knockdown cells, suggesting a specificity to BPTF. Given the high potency and good physicochemical properties of these inhibitors, we anticipate that they will be useful starting points for chemical tool development to explore the biological roles of BPTF.

PYRIDAZINONE DERIVATIVES AND THEIR USE IN THE TREATMENT OF CANCER

The invention relates to compounds of formula (I) and salts thereof: wherein R1-R3 have any of the values defined in the specification. The compounds and salts are useful for treating PCAF mediated disorders and/or GCN5 mediated disorders. The invention also provides pharmaceutical compositions comprising a compound of formula (I), or a pharmaceutically acceptable salt thereof, as well as and methods of using said compounds, salts, or compositions in the treatment of various disorders.

Contrast agent and for the use of a synthetic composition, method and system (by machine translation)

The present invention provides compounds with imaging moieties for imaging a subject. The present invention also relates to systems, compositions, and methods for the synthesis and use of imaging agents, or precursors thereof. An imaging agent precursor may be converted to an imaging agent using the methods described herein. In some cases, a composition or plurality of imaging agents is enriched in 18 F. In some cases, an imaging agent may be used to image an area of interest in a subject, including, but not limited to, the heart, cardiovascular system, cardiac vessels, brain, and other organs.

COMPOSITIONS, METHODS, AND SYSTEMS FOR THE SYNTHESIS AND USE OF IMAGING AGENTS

The present invention provides compounds with imaging moieties for imaging a subject. The present invention also relates to systems, compositions, and methods for the synthesis and use of imaging agents, or precursors thereof. An imaging agent precursor may be converted to an imaging agent using the methods described herein. In some cases, a composition or plurality of imaging agents is enriched in 18 F. In some cases, an imaging agent may be used to image an area of interest in a subject, including, but not limited to, the heart, cardiovascular system, cardiac vessels, brain, and other organs.

Concurrent Alkylation-Methoxylation of 4,5-Dihalopyridazin-6-ones and Synthesis of 5-Halo-4-hydroxypyridazin-6-ones

1-Alkyl-5-halo-4-methoxypyridazin-6-ones were synthesized from 1-alkyl-4,5-dihalopyridazin-6-ones by the concurrent alkylation-methoxylation. 1-Alkyl-5-halo-4-hydroxypyridazin-6-ones were also prepared.