85907-78-4

Upstream product

• 64-17-5 ethanol 
• 621-43-2 (3,4-diamino-phenyl)-acetic acid 
• 116435-82-6 2-(4-amino-3-nitrophenyl)acetic acid 
• 90916-02-2 4-Acetamino-3-nitro-phenylessigsaeure 
• 1197-55-3 4-aminophenylacetic acid 

Downstream Products

• 195505-47-6 ethyl 2-(2,1,3-benzothiadiazol-5-yl)-acetate 
• 195505-46-5 ethyl 2-(2,1,3-benzothiadiazol-5-yl)-4-(4-methoxyphenyl)-4-oxobutanoate 
• 195505-56-7 3-(2,1,3-benzothiadiazol-5-yl)-4-(3,4,5-trimethoxybenzyl)-5-hydroxy-5-(4-methoxyphenyl)-5H-furan-2-one 
• 1246639-71-3 4-chlorobenzyl 4-(2-1H-benzotriazol-5-ylacetyl)piperazine-1-carboxylate 
• 491612-10-3 C₈H₇N₃O₂ 

Relevant academic research and scientific papers

COMPOUNDS AND METHODS

The present invention relates to novel retinoid-related orphan receptor gamma (RORγ) modulators and their use in the treatment of diseases mediated by RORy.

2. ENDOTHELIN antagonists: Evaluation of 2,1,3-benzothiadiazole as a methylendioxyphenyl bioisoster

The methylendioxyphenyl group is present in a number of endothelin receptor antagonists thus far reported. By means of a Kohonen neural network we discovered with a benzothiadiazole a bioisosteric replacement instead. This group should be devoid of the negative metabolic interactions with cytochrome P450 ascribed to methylendioxyphenyl in vivo. The synthesis of a potent benzothiadiazole analogue EMD 122801 together with in vitro studies of different methylendioxyphenyl, benzothiadiazole and benzofurazan derivatives is described.