Invented by Antoni Krasinski, Sreenivas Punna, Solomon Ungashe, Qiang Wang, Yibin Zeng, Chemocentryx Inc

Fused heteroaryl-pyridyl- and phenyl-benzenesulfonamides are a class of compounds that have shown promising results in the treatment of inflammation using CCR2. CCR2 is a chemokine receptor that is involved in the recruitment of monocytes and macrophages to sites of inflammation. Inhibiting CCR2 can reduce the recruitment of these cells and decrease inflammation. The market for fused heteroaryl-pyridyl- and phenyl-benzenesulfonamides is expected to grow in the coming years due to the increasing prevalence of inflammatory diseases such as rheumatoid arthritis, multiple sclerosis, and inflammatory bowel disease. These diseases affect millions of people worldwide and can cause significant morbidity and mortality. Several companies are currently developing fused heteroaryl-pyridyl- and phenyl-benzenesulfonamides for the treatment of inflammation using CCR2. These compounds have shown promising results in preclinical studies, and some have advanced to clinical trials. One such compound is CCX354-C, developed by ChemoCentryx. CCX354-C is a selective CCR2 antagonist that has shown efficacy in preclinical models of rheumatoid arthritis, multiple sclerosis, and psoriasis. In a phase II clinical trial, CCX354-C demonstrated significant improvements in disease activity in patients with rheumatoid arthritis. Another compound in development is PF-04634817, developed by Pfizer. PF-04634817 is a dual CCR2 and CCR5 antagonist that has shown efficacy in preclinical models of inflammatory bowel disease and multiple sclerosis. PF-04634817 is currently in phase II clinical trials for the treatment of Crohn’s disease. The market for fused heteroaryl-pyridyl- and phenyl-benzenesulfonamides is expected to be competitive, with several companies vying for market share. However, the potential benefits of these compounds in the treatment of inflammatory diseases make them an attractive investment for pharmaceutical companies. In conclusion, the market for fused heteroaryl-pyridyl- and phenyl-benzenesulfonamides for the treatment of inflammation using CCR2 is expected to grow in the coming years. These compounds have shown promising results in preclinical and clinical studies and have the potential to provide significant benefits to patients with inflammatory diseases. As more companies invest in the development of these compounds, the market is expected to become increasingly competitive.

The Chemocentryx Inc invention works as follows

Compounds that are potent antagonists to the CCR2 receptor are described. The compounds, which are arylsulfonamides in general, are useful as pharmaceutical compositions, as methods for treating CCR2-mediated disease and as controls for assays to identify CCR2 antagonists.

Background for Fused heteroaryl-pyridyl- and phenyl-benzenesuflonamides for the treatment of inflammation using ccr2

Preferred Embodiments

BiRAM Assay

Calcium Flux Assay

Ligand binding Assay

Methods of Treatment.

Methods for treating or preventing CCR2-mediated conditions or diseases

Preparation Modulators

EXAMPLES

General Procedure for the N-Protection

Example 1

4-Chloro-N-[5-chloro-2-(7H-pyrrolo[2,3-d]pyrimidine-4-carbonyl)-phenyl]-3-trifluoromethyl-benzenesulfonamide

Example 2

4-Chloro-N-[2-(7H-pyrrolo[2,3-d]pyrimidine-4-carbonyl)-pyridin-3-yl]-3-trifluoromethyl-benzenesulfonamide

Example 3

4-Chloro-N-[5-chloro-2-(7-methyl-7H-pyrrolo[2,3-d]pyrimidine-4-carbonyl)-pyridin-3-yl]-3-trifluoromethyl-benzenesulfonamide

Example 4

Preparation of 4-Chloro-N-(5-(methoxymethyl)-2-(7H-pyrrolo[2,3-d]pyrimidine-4-carbonyl)pyridin-3-yl)-3-(trifluoromethyl)benzenesulfonamide

Example 5

4-Chloro-N-[5-methyl-2-(7H-pyrrolo[2,3-d]pyrimidine-4-carbonyl)-pyridin-3-yl]-3-trifluoromethyl-benzenesulfonamide

Example 6

4-Methyl-N-[5-methyl-2-(7H-pyrrolo[2,3-d]pyrimidine-4-carbonyl)-pyridin-3-yl]-3-trifluoromethyl-benzenesulfonamide

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