870194-65-3

Upstream product

• 39684-80-5 2-(tert-butoxycarbonylamino)ethyl bromide 
• 120-83-2 2,4-dichlorophenol 
• 96628-67-0 2-(tert-butoxycarbonylamino)ethyl methanesulfonate 
• 26690-80-2 2-(N-tert-butoxycarbonylamino)ethanol 
• 24424-99-5 di-tert-butyl dicarbonate 

Downstream Products

• 26378-66-5 2-(2,4-dichloro-phenoxy)-ethylamine; hydrochloride 
• 870195-29-2 (4-{4-[2-(2,4-dichloro-phenoxy)-ethyl-carbamoyl]-5-phenyl-isoxazol-3-yl}-2-methyl-phenoxy)-acetic acid methyl ester 
• 870194-96-0 LC₁₇₆₅ 
• 927187-47-1 (3-{4-[2-(2,4-dichloro-phenoxy)-ethyl-carbamoyl]-5-phenyl-isoxazol-3-yl}-phenyl)-acetic acid methyl ester 
• 870194-70-0 (3-chloro-4-{4-[2-(2,4-dichloro-phenoxy)-ethylcarbamoyl]-5-phenyl-isoxazol-3-yl}-phenyl)-acetic acid 
• 870194-95-9 (3-chloro-4-{4-[2-(2,4-dichloro-phenoxy)-ethylcarbamoyl]-5-phenyl-isoxazol-3-yl}-phenyl)-acetic acid methyl ester 
• 919284-40-5 (3-chloro-4-{4-[2-(2,4-dichloro-phenoxy)-ethylcarbamoyl]-5-furan-2-yl-isoxazol-3-yl}-phenyl)-acetic acid methyl ester 
• 919284-20-1 (3-chloro-4-{5-cyclopropyl-4-[2-(2,4-dichloro-phenoxy)-ethylcarbamoyl]-isoxazol-3-yl}-phenyl)-acetic acid methyl ester 
• 919284-02-9 (4-{5-tert-butyl-4-[2-(2,4-dichloro-phenoxy)-ethylcarbamoyl]-isoxazol-3-yl}-3-chloro-phenyl)-acetic acid methyl ester 
• 919283-73-1 (3-chloro-4-{4-[2-(2,4-dichloro-phenoxy)-ethylcarbamoyl]-5-ethyl-isoxazol-3-yl}-phenyl)-acetic acid methyl ester 
• 919283-75-3 (3-chloro-4-{4-[2-(2,4-dichloro-phenoxy)-ethylcarbamoyl]-5-isopropyl-isoxazol-3-yl}-phenyl)-acetic acid methyl ester 

Relevant academic research and scientific papers

PYRIDIN-3-YL ACETIC ACID DERIVATIVES AS INHIBITORS OF HUMAN IMMUNODEFICIENCY VIRUS REPLICATION

Disclosed are compounds of Formula I, including pharmaceutically acceptable salts, pharmaceutical compositions comprising the compounds, methods for making the compounds and their use in inhibiting HIV integrase and treating those infected with HIV or AIDS.

Discovery and SAR of novel and selective inhibitors of urokinase plasminogen activator (uPA) with an imidazo[1,2-A]pyridine scaffold

Urokinase plasminogen activator (uPA) is a biomarker and therapeutic target for several cancer types. Its inhibition is regarded as a promising, noncytotoxic approach in cancer therapy by blocking growth and/or metastasis of solid tumors. Earlier, we reported the modified substrate activity screening (MSAS) approach and applied it for the identification of fragments with affinity for uPA's S1 pocket. Here, these fragments are transformed into a novel class of uPA inhibitors with an imidazo[1,2-A]pyridine scaffold. The SAR for uPA inhibition around this scaffold is explored, and the best compounds in the series have nanomolar uPA affinity and selectivity with respect to the related trypsin-like serine proteases (thrombin, tPA, FXa, plasmin, plasma kallikrein, trypsin, FVIIa). Finally, the approach followed for translating fragments into small molecules with a decorated scaffold architecture is conceptually straightforward and can be expected to be broadly applicable in fragment-based drug design.

3,4,5-Trisubstituted isoxazoles as novel PPARδ agonists: Part 1

We report the identification of a novel series of trisubstituted isoxazoles as PPAR activators from a high-throughput screen. A series of structural optimizations led to improved efficacy and excellent functional receptor selectivity for PPARδ. The isoxazoles represent a series of agonists which display a scaffold that lies outside the typical PPAR agonist motif.

COMPOUNDS AND COMPOSITIONS AS PPAR MODULATORS

The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of the Peroxisome Proliferator-Activated Receptor (PPAR) families, particularly the activity of PPAR .