367501-32-4

Upstream product

• 917909-46-7 3-ethoxy-4-nitro-benzoic acid amide 
• 403-21-4 3-fluoro-4-nitrobenzoic acid 
• 64-17-5 ethanol 
• 342044-63-7 ethyl 3-ethoxy-4-nitrobenzoate 

Downstream Products

• 957855-91-3 3-ethoxy-N-(1-methylpiperidin-4-yl)-4-nitrobenzamide 
• 367501-31-3 4-amino-3-ethoxybenzoic acid 
• 1147136-68-2 C₁₇H₂₄N₂O₆ 
• 1578247-84-3 3-(3-ethoxy-4-nitrophenyl)-4-methyl-4H-1,2,4-triazole 
• 1578247-87-6 5-(3-ethoxy-4-nitrophenyl)-4-methyl-4H-1,2,4-triazole-3-thiol 
• 1578247-88-7 3-ethoxy-4-nitrobenzohydrazide 
• 1578245-44-9 N₂-(2-ethoxy-4-(4-methyl-4H-1,2,4-triazol-3-yl)phenyl)-6-methyl-N₈-neopentylpyrido[3,4-d]pyrimidine-2,8-diamine 
• 1578246-82-8 8-chloro-N-(2-ethoxy-4-(4-methyl-4H-1,2,4-triazol-3-yl)phenyl)-6-methylpyrido[3,4-d]pyrimidin-2-amine 
• 1578247-07-0 N-(2-ethoxy-4-(4-methyl-4H-1,2,4-triazol-3-yl)phenyl)formamide 
• 957855-87-7 (R)-4-((8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,7,8-tetrahydropteridin-2-yl)amino)-3-ethoxy-N-(1-methylpiperidin-4-yl)-benzamide 

Relevant academic research and scientific papers

Design, Synthesis, and Conformational Analysis of Oligobenzanilides as Multifacial α-Helix Mimetics

The design, synthesis, and conformational analysis of an oligobenzanilide helix mimetic scaffold capable of simultaneous mimicry of two faces of an α-helix is reported. The synthetic methodology provides access to diverse monomer building blocks amenable to solid-phase assembly in just four synthetic steps. The conformational flexibility of model dimers was investigated using a combination of solid and solution state methodologies supplemented with DFT calculations. The lack of noncovalent constraints allows for significant conformational plasticity in the scaffold, thus permitting it to successfully mimic residues i, i+2, i+4, i+6, i+7, and i+9 of a canonical α-helix.

Introduction of a Methyl Group Curbs Metabolism of Pyrido[3,4- d]pyrimidine Monopolar Spindle 1 (MPS1) Inhibitors and Enables the Discovery of the Phase 1 Clinical Candidate N2-(2-Ethoxy-4-(4-methyl-4 H-1,2,4-triazol-3-yl)phenyl)-6-methyl- N

Monopolar spindle 1 (MPS1) occupies a central role in mitosis and is one of the main components of the spindle assembly checkpoint. The MPS1 kinase is an attractive cancer target, and herein, we report the discovery of the clinical candidate BOS172722. Th

Biosynthesis of branched alkoxy groups: Iterative methyl group alkylation by a cobalamin-dependent radical SAM enzyme

The biosynthesis of branched alkoxy groups, such as the unique t-butyl group found in a variety of natural products, is still poorly understood. Recently, cystobactamids were isolated and identified from Cystobacter sp as novel antibacterials. These metab

(5,6-DIHYDRO)PYRIMIDO[4,5-E]INDOLIZINES

The invention relates to a compound of Formula (I) wherein, R1 and R2 independently are selected from the group consisting of optionally substituted (6-10C)aryl and (1-5C)heteroaryl groups. The compounds can be used in pharmaceutical compositions, in particular in the treatment of cancer.

Design, synthesis, and evaluation of an a-helix mimetic library targeting protein-protein interactions

The design and solution-phase synthesis of an α-helix mimetic library as an integral component of a small-molecule library targeting protein - protein interactions are described. The iterative design, synthesis, and evaluation of the candidate α-helix mimetic was initiated from a precedented triaryl template and refined by screening the designs for inhibition of MDM2/p53 binding. Upon identifying a chemically and biologically satisfactory design and consistent with the screening capabilities of academic collaborators, the corresponding complete library was assembled as 400 mixtures of 20 compounds (20 × 20 × 20-mix),where the added subunits are designed to mimic all possible permutation s of the naturally occurring i, i + 4, i + 7 amino acid side chains of an α-helix. The library (8000 compounds) was prepared using a solution-phase synthetic protocol enlisting acid/base liquid-liquid extractions for purification on a scale that insures its long-term availability for screening campaigns. Screening of the library for inhibition of MDM2/p53 binding not only identified the lead α-helix mimetic upon which the library was based, but also suggests that a digestion of the initial screening results that accompany the use of such a comprehensive library can provide insights into the nature of the interaction (e.g., an α-helix mediated protein-protein interaction) and define the key residues and their characteristics responsible for recognition.

NOVEL COMPOUNDS

There is provided a compound of formula (I): processes for the manufacture thereof, pharmaceutical compositions thereof and uses in therapy.

ESTER COMPOUND AND MEDICINAL USE THEREOF

A novel therapeutic agent for hyperlipidemia, which is an ester compound represented by the formula (1") (wherein ???R1 and R2 are each hydrogen atom or optionally substituted aryl, etc.; ???X is -COO- or -CON(R10)-; ???R3 and R4 are each hydrogen atom, C1-C6 alkyl or C1-C6 alkoxy, etc.; ???R5, R6 and R7 are each hydrogen atom, C1-C6 alkyl or C1-C6 alkoxy, etc.; ???R8 and R9 are each independently hydrogen atom, C1-C6 alkyl, -CON(R18)(R19) or -COO(R20), etc.; ???ring A, ring B and ring C are each independently aryl or heterocycle residue, etc.; ???Alk1 and Alk2 are each independently alkanediyl, etc.; ???l and m are each an integer of 0 or 1 to 3) or a prodrug thereof, or a pharmaceutically acceptable salt of either. The therapeutic agent selectively inhibits MTP in the small intestine, thus causes no such side effect as a fatty liver.

Chemical compounds

The present invention provides a compound of a formula (I): wherein the variables are defined herein; to a process for preparing such a compound; and to the use of such a compound in the treatment of a chemokine (such as CCR3) or H1 mediated disease state.