923023-06-7

Upstream product

• 383-63-1 ethyl trifluoroacetate, 
• 50910-54-8 trans-4-aminocyclohexanol hydrochloride 
• 27489-62-9 trans-4-hydroxycyclohexylamine 

Downstream Products

• 1352624-44-2 N-((1r,4r)-4-(tert-butyldiphenylsilyloxy)cyclohexyl)-2,2,2-trifluoroacetamide 
• 78293-47-7 N-<(Trifluoroacetyl)amino>cyclohex-3-ene 
• 1204401-33-1 cis-N-(4-iodocyclohexyl)-2,2,2-trifluoroacetamide 
• 923023-07-8 2,2,2-trifluoro-N-(4-hydroxy-cyclohexyl)-N-methyl-acetamide 

Relevant academic research and scientific papers

Identification of 2-Imidazopyridine and 2-Aminopyridone Purinones as Potent Pan-Janus Kinase (JAK) Inhibitors for the Inhaled Treatment of Respiratory Diseases

Janus kinases (JAKs) have a key role in regulating the expression and function of relevant inflammatory cytokines involved in asthma and chronic obstructive pulmonary disease. Herein are described the design, synthesis, and pharmacological evaluation of a series of novel purinone JAK inhibitors with profiles suitable for inhaled administration. Replacement of the imidazopyridine hinge binding motif present in the initial compounds of this series with a pyridone ring resulted in the mitigation of cell cytotoxicity. Further systematic structure-activity relationship (SAR) efforts driven by structural biology studies led to the discovery of pyridone 34, a potent pan-JAK inhibitor with good selectivity, long lung retention time, low oral bioavailability, and proven efficacy in the lipopolysaccharide-induced rat model of airway inflammation by the inhaled route.

Heteroaryl imidazolone derivatives as jak inhibitors

New heteroaryl imidazolone derivatives having the chemical structure of formula (I) are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Janus Kinases (JAK).

HETEROARYL IMIDAZOLONE DERIVATIVES AS JAK INHIBITORS

New heteroaryl imidazolone derivatives having the chemical structure of formula (I) disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Janus Kinases (JAK).

CYCLOHEXYLAMIN ISOQUINOLONE DERIVATIVES AS RHO-KINASE INHIBITORS

The invention relates to 6-cyclohexylamine-substituted isoquinolone derivatives of the formula (I) or isoquinoline derivatives of the formula (I’) useful for the treatment and/or prevention of diseases associated with Rho-kinase and/or Rho-kinase mediated phosphorylation of myosin light chain phosphatase, and compositions containing such compounds.