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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.

Pending Publication Date: 2022-05-13
BIOCRYST PHARM INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Subsequently, complement proteins create holes, or pores, in the invading organism, leading to its destruction

Method used

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Examples

Experimental program
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Embodiment

[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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Abstract

Compounds of Formula (I) and pharmaceutically acceptable salts thereof are disclosed, which are inhibitors of the complement system. Also provided are pharmaceutical compositions comprising such compounds, and methods of using the compounds and compositions to treat or prevent diseases or conditions characterized by aberrant complement system activity.

Description

[0001] related application [0002] This application claims priority to U.S. Provisional Patent Application No. 62 / 912,929, filed October 9, 2019. Background technique [0003] The complement system is the branch of an organism's immune system that enhances the ability of antibodies and phagocytes to destroy foreign particles, such as pathogens, and remove them from the organism. The complement system comprises a group of plasma proteins that work together to attack the extracellular forms of pathogens and induce a cascade of inflammatory responses to help fight infection. Complement activation can proceed via several pathways. For example, complement activation can occur spontaneously in response to certain pathogens or by antibodies that bind to the pathogen. When complement proteins are activated, a cascade is triggered whereby one complement protein induces the activation of the next protein in the sequence. Activation of a small number of complement proteins at the beg...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/506A61K31/519A61K31/5377
CPCC07D307/80C07D333/56C07D471/04C07D209/12C07D231/56C07D405/04C07D407/12C07D405/06C07D273/04C07D491/048C07D405/12C07D417/12C07D495/04C07C217/48A61K31/343A61K31/381A61K31/437A61K31/404A61K31/416A61K31/5377A61K31/506A61P25/00A61P25/28A61P13/12A61P9/00A61P7/00A61P27/02C07D407/14C07D275/04C07D405/10C07D493/04C07D401/04
Inventor P·L·科蒂安Y·S·巴布张维河吕鹏程A·E·斯保尔丁吕魏党昭K·拉曼
Owner BIOCRYST PHARM INC
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