Oral complement factor D inhibitors
An alkyl, cycloalkyl technology, applied in the field of oral complement factor D inhibitors, which can solve problems such as destruction, generation of holes or holes, etc.
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[0348] Now that the invention has been described in detail, it will be more clearly understood by reference to the following examples, which are included herein for purposes of illustration only and are not intended to limit the invention.
[0349] plan 1
[0350]
[0351] Preparation of 2-((5-(3-(aminomethyl)phenyl)benzofuran-3-yl)methoxy)benzoic acid (1f)
[0352] Step-1: Preparation of methyl 2-((5-bromobenzofuran-3-yl)methoxy)benzoate (1c)
[0353] To a solution of 5-bromo-3-(bromomethyl)benzofuran (1a) (250mg, 0.862mmol; CAS#137242-43-4), potassium carbonate (477mg, 3.45mmol) in acetone (3mL) Methyl 2-hydroxybenzoate (1b) (157 mg, 1.035 mmol; CAS# 119-36-8) was added. The resulting mixture was stirred overnight at room temperature. The suspension was filtered through a pad of celite, and the filtrate was concentrated to dryness in vacuo. The obtained residue was purified by flash column chromatography [silica gel (12 g), eluting with 0-50% EtOAc / hexanes] to afford ...
Embodiment 334
[3749] ICs for compounds were calculated according to the procedure reported in U.S. Patent 6,653,340 B1, e.g., column 74 (incorporated by reference) 50 value (ie, the concentration of compound that inhibits 50% of the enzyme activity).
[3750] Specifically, compounds were dissolved in stock solutions in DMSO at 10.0 or 100 mM. Add a portion of this stock solution to the assay buffer to a final volume of 50 μL. Controls included buffer alone and enzyme solutions to which DMSO was added. Substrate is added to the wells either immediately or after incubation at room temperature. The reaction rate was measured spectrophotometrically by generating product at 405 nm for 600 seconds. The background absorbance at 690 nm was measured for each well and subtracted from the absorbance at 405 nm.
[3751] The reaction rate of the enzyme alone is compared to the rate of the enzyme in the presence of the inhibitor, and the percent inhibition is calculated as follows:
[3752] Percent in...
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