89523-17-1

Upstream product

• 1493-27-2 ortho-nitrofluorobenzene 
• 21315-09-3 1-(cyclopropylmethoxy)-2-nitrobenzene 
• 88-75-5 2-hydroxynitrobenzene 

Downstream Products

• 1428846-96-1 N-(2-(cyclopropylmethoxy)-4-nitrophenyl)-methanesulfonamide 
• 1428846-97-2 N-(4-amino-2-(cyclopropylmethoxy)phenyl)-methanesulfonamide 
• 1428846-98-3 S-3-(cyclopropylmethoxy)-4-(methylsulfonamido)phenyl O-ethyl carbonodithioate 
• 1428846-99-4 N-(2-(cyclopropylmethoxy)-4-mercaptophenyl)-methanesulfonamide 
• 1428846-95-0 (S)-3,5-dichloro-4-(2-(3-(cyclopropylmethoxy)-4-(difluoromethoxy)phenyl)-2-((3-(cyclopropylmethoxy)-4-(methylsulfonamido)-phenylthio)carbonyloxy)ethyl)pyridine 1-oxide 
• 1445984-99-5 tert-butyl N-[2-(cyclopropylmethyoxy)phenyl]carbamate 
• 1445981-54-3 (S)-N-[2-(cyclopropylmethoxy)phenyl]-1-(2,5-dichlorobenzyl)-N-methylpyrrolidine-2-carboxamide 
• 1445985-03-4 (2S)-N-[2-(cyclopropylmethoxy)phenyl]-N-methyl-pyrrolidine-2-carboxamide 
• 1445985-02-3 C₂₄H₂₈N₂O₄ 
• 1445985-01-2 2-(cyclopropylmethoxy)-N-methylaniline 
• 1445985-00-1 tert-butyl N-[2-(cyclopropylmethyoxy)phenyl]-N-methylcarbamate 

Relevant academic research and scientific papers

Design of Gut-Restricted Thiazolidine Agonists of G Protein-Coupled Bile Acid Receptor 1 (GPBAR1, TGR5)

Bile acid signaling and metabolism in the gastrointestinal tract have wide-ranging influences on systemic disease. G protein-coupled bile acid receptor 1 (GPBAR1, TGR5) is one of the major effectors in bile acid sensing, with demonstrated influence on metabolic, inflammatory, and proliferative processes. The pharmacologic utility of TGR5 agonists has been limited by systemic target-related effects such as excessive gallbladder filling and blockade of gallbladder emptying. Gut-restricted TGR5 agonists, however, have the potential to avoid these side effects and consequently be developed into drugs with acceptable safety profiles. We describe the discovery and optimization of a series of gut-restricted TGR5 agonists that elicit a potent response in mice, with minimal gallbladder-related effects. The series includes 12 (TGR5 EC50: human, 143 nM; mouse, 1.2 nM), a compound with minimal systemic availability that may have therapeutic value to patients with type 2 diabetes mellitus, nonalcoholic steatohepatitis, or inflammatory bowel disease.

NON-SYSTEMIC TGR5 AGONISTS

Compounds of structure (I), or a stereoisomer, tautomer, pharmaceutically acceptable salt or prodrug thereof, wherein R1, R2, R3, R4, R8, R9, R10, R11, R12, A1, A2, X, Y and Z are as defined herein. Uses of such compounds as TGR5 antagonists and for treatment of various indications, including Type II diabetes meletus are also provided.

DERIVATIVES OF 1-PHENYL-2-PYRIDINYL ALKYL ALCOHOLS AS PHOSPHODIESTERASE INHIBITORS

The invention relates to inhibitors of the phosphodiesterase 4 (PDE4) enzyme. More particularly, the invention relates to compounds that are derivatives of 1-phenyl-2-pyridinyl alkyl alcohols, methods of preparing such compounds, compositions containing them and therapeutic use thereof.

DERIVATIVES OF 1-PHENYL-2-PYRIDINYL ALKYL ALCOHOLS AS PHOSPHODIESTERASE INHIBITORS

The invention relates to inhibitors of the phosphodiesterase 4 (PDE4) enzyme. More particularly, the invention relates to compounds that are derivatives of 1-phenyl-2-pyridinyl alkyl alcohols, methods of preparing such compounds, compositions containing them and therapeutic use thereof.

NOVEL USE OF THIENOPYRIMIDINES

The present invention relates to the use of thienopyrimidine compounds for the production of pharmaceutical compositions for the treatment of inflammatory diseases.

THIENOPYRIMIDINES FOR PHARMACEUTICAL COMPOSITIONS

The present invention relates to novel pharmaceutical compositions of general formula (I) comprising thienopyrimidine compounds. Moreover, the present invention relates to the use of the thienopyrimidine compounds of the invention for the production of pharmaceutical compositions for the prophylaxis and/or treatment of diseases which can be influenced by the inhibition of the kinase activity of Mnk1 and/or Mnk2 (Mnk2a or Mnk2b) and/or variants thereof.