80909-96-2

Upstream product

• 58885-58-8 N-tert-butoxycarbonyl-3-aminopropanol 
• 98-59-9 p-toluenesulfonyl chloride 
• 41840-28-2 S-tert-butoxycarbonyl-4,6-dimethyl-2-mercaptopyrimidine 
• 156-87-6 propan-1-ol-3-amine 
• 34619-03-9 tert-butyldicarbonate 
• 24424-99-5 di-tert-butyl dicarbonate 

Downstream Products

• 955359-92-9 1,1-dimethylethyl (3-{4-[4-[(4-chlorophenyl)methyl]-1-oxo-2(1H)-phthalazinyl]hexahydro-1H-azepin-1-yl}propyl)carbamate 
• 913642-21-4 1,1-dimethylethyl [3-({3-[2-(4-amino-1,2,5-oxadiazol-3-yl)-1-ethyl-4-(3-hydroxy-3-methyl-1-butyn-1-yl)-1H-imidazo[4,5-c]pyridin-6-yl]phenyl}oxy)propyl]carbamate 
• 1085928-20-6 tert-butyl (3-(4-(2-methoxyphenyl)piperazin-1-yl)propyl)carbamate 
• 1426687-03-7 tert-butyl (3-(((4S)-6-(4-chlorophenyl)-4-(2-(ethylamino)-2-oxoethyl)-1-methyl-4H-benzo[f][1,2,4]triazolo[4,3-a][1,4]diazepin-8-yl)oxy)propyl)carbamate 
• 129392-84-3 tert-butyl N-(3-azidopropyl)carbamate 

Relevant academic research and scientific papers

COMPOUNDS AND USES THEREOF

The present disclosure features compounds useful for the treatment of BAF complex-related disorders.

SMARCA DEGRADERS AND USES THEREOF

The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same for the modulation of one or more SWI/SNF-related matrix associated actin dependent regulator of chromatin subfamily A (SMARCA) and/or polybromo-1 (PB-1) protein via ubiqitination and/or degradation by compounds. The compounds are bifunctional molecules that link a cereblon-binding moiety to a ligand that binds SMARCA and/or PB1 proteins.

Azido-Desferrioxamine Siderophores as Functional Click-Chemistry Probes Generated in Culture upon Adding a Diazo-Transfer Reagent

This work aimed to undertake the in situ conversion of the terminal amine groups of bacterial desferrioxamine (DFO) siderophores, including desferrioxamine B (DFOB), to azide groups to enable downstream click chemistry. Initial studies trialed a precursor-directed biosynthesis (PDB) approach. Supplementing Streptomyces pilosus culture with blunt-end azido/amine non-native substrates designed to replace 1,5-diaminopentane as the native diamine substrate in the terminal amine position of DFOB did not produce azido-DFOB. Addition of the diazo-transfer reagent imidazole-1-sulfonyl azide hydrogen sulfate to spent S. pilosus medium that had been cultured in the presence of 1,4-diaminobutane, as a viable native substrate to expand the suite of native DFO-type siderophores, successfully generated the cognate suite of azido-DFO analogues. CuI-mediated or strain-promoted CuI-free click chemistry reactions between this minimally processed mixture and the appropriate alkyne-bearing biotin reagents produced the cognate suite of 1,4-disubstituted triazole-linked DFO-biotin compounds as potential molecular probes, detected as FeIII-loaded species. The amine-to-azide transformation of amine-bearing natural products in complex mixtures by the direct addition of a diazo-transfer reagent to deliver functional click chemistry reagents adds to the toolbox for chemical proteomics, chemical biology, and drug discovery.

Modular RNA regulators and methods

This disclosure describes modular miRNA regulator molecules and methods of using modular miRNA regulator molecules. Generally, the modular miRNA regulator molecules include a recognition module and an inhibition module. Generally, the recognition module includes a polynucleotide in which at least a portion of the polynucleotide recognizes at least a portion of a preselected pre-miRNA. Generally, the inhibition module includes a moiety that inhibits nuclease processing of the preselected pre-RNA to a mature RNA.

For the treatment of tumor macrocyclic derivatives (by machine translation)

The invention discloses a method for modulating protein kinase activity, and is used for the treatment or prevention of protein kinase related disorders. Specifically, the invention relates to a method for the treatment of tumor of the macrocyclic derivatives, which belongs to the regulating Anaplastic lymphoma kinase (ALK) active compound, and provides the preparation method of the compound, and the compound used for the treatment or prevention of diseases associated with the ALK pharmaceutical use. (by machine translation)

Design, radiosynthesis, and evaluation of radiotracers for positron emission tomography imaging of stearoyl-CoA desaturase-1

Design, radiosynthesis, and biological evaluation of two radiotracers (N-(3-[18F]fluoropropyl)-6-(4-(trifluoromethyl)benzoyl)-piperazin-1-yl)pyridazine-3-carboxamide (18F-FPPPT) and (N-(4-[18F]fluoroaniline)-6-(4-(trifluoromethyl)benzoyl)-piperazin-1-yl)pyridazine-3-carboxamide (18F-FAPPT)) are described for noninvasive assessment of stearoyl-CoA desaturase-1 (SCD-1). The overexpression of SCD-1 in multiple solid tumors associates with poor survival in cancer patients. The two radiotracers,18F-FPPPT and18F-FAPPT, were each prepared in three steps in radiochemical yields of 21% and 3%, respectively. The practicality of imaging SCD-1 with18F-FPPPT was tested in two mouse models bearing xenograft tumors with different levels of SCD-1 expression, which afforded a 1.8-fold uptake difference correspondingly. Our work indicates that it is possible to develop SCD-1 specific imaging probes from previously reported SCD-1 inhibitors.

SURFACE FUNCTIONALIZED, HOST-GUEST POLYMER NANO-ASSEMBLIES AND METHODS THEREOF

The invention generally relates to polymer-based nano-structures. More particularly, the invention relates to novel, surface-functionalized, guest-host polymer nano-assemblies and nano-delivery vehicles useful in diverse fields including drug delivery, diagnostics and specialty materials. The nano-assemblies and nano-delivery vehicles of the invention are afforded via simplify and reliable approaches.

Regioselective rapid synthesis of fully substituted 1,2,3-triazoles mediated by propargyl cations

Regioselective rapid triazole syntheses at low temperature are described. Organic azides and propargyl cations generated by acids gave fully substituted 1H-1,2,3-triazoles. Most reactions could be performed in 5 min at not only rt but also -90 C. Both terminal and internal alkynes were acceptable, and the sterically bulky substituents could afford the products smoothly. Various types of three-component coupling reactions were demonstrated, and the presence of allenylaminodiazonium intermediates was indicated.

ANTIFUNGAL AGENTS

Compounds and compositions useful as antifungals are provided, as are methods of use and preparation of such compounds and compositions containing such compounds. In some embodiments, the compounds are bifunctional, comprising two active moieties connected by a linking moiety. The compounds of the invention are useful for treating infections by microorganisms.

COMPSITIONS, SYNTHESIS, AND METHODS OF USING QUINOLINE BASED ATYPICAL ANTIPSYCHOTIC AGENTS

The present invention provides novel quinolinone derivatives which can be advantageously used for treating schizophrenia and related psychoses such as acute manic, bipolar disorder, autistic disorder, and depression.