1437779-82-2

Upstream product

• 862248-93-9 (3,4,5-trichlorophenyl)boronic acid 
• 1437779-28-6 3,3-dimethyl-5-(5-(3,4,5-trichlorophenyl)-5-(trifluoromethyl)-4,5-dihydroisoxazol-3-yl)benzo[c][1,2]oxaborol-1(3H)-ol 
• 864736-87-8 1,2,3-trichloro-5-(1,1,1-trifluoroprop-2-en-2-yl)benzene 
• 1437779-68-4 N,1-dihydroxy-3,3-dimethyl-1,3-dihydrobenzo[c][1,2]oxaborole-5-carbimidoyl chloride 
• 1393477-37-6 1-hydroxy-3,3-dimethyl-1,3-dihydrobenzo[c][1,2]oxaborole-5-carbaldehyde oxime 
• 1393477-36-5 1-hydroxy-3,3-dimethyl-1,3-dihydrobenzo[c][1,2]oxaborole-5-carbaldehyde 
• 1393477-33-2 3,3,5-trimethylbenzo[c][1,2]oxaborol-1(3H)-ol 
• 1393477-32-1 2-(2-bromo-5-methylphenyl)propan-2-ol 
• 90971-88-3 methyl 2-bromo-5-methylbenzoate 
• 6967-82-4 2-bromo-5-methylbenzoic acid 

Relevant academic research and scientific papers

Discovery of an orally bioavailable isoxazoline benzoxaborole (AN8030) as a long acting animal ectoparasiticide

A novel series of isoxazoline benzoxaborole small molecules was designed and synthesized for a structure-activity relationship (SAR) investigation to assess the ectoparasiticide activity against ticks and fleas. The study identified an orally bioavailable molecule, (S)-3,3-dimethyl-5-(5-(3,4,5-trichlorophenyl)-5-(trifluoromethyl)-4,5-dihydroisoxazol-3-yl)benzo[c][1,2]oxaborol-1(3H)-ol (38, AN8030), which was long lasting in dogs (t1/2 = 22 days). Compound 38 demonstrated 97.6% therapeutic effectiveness within 24 h of treatment, with residual efficacy of 95.3% against American dog ticks (Dermacentor variabilis) on day 30% and 100% against cat fleas (Ctenocephalides felis) on day 32 after a single oral dose at 50 mg/kg in dogs.

BORON-CONTAINING SMALL MOLECULES

This invention provides novel compounds, methods of using the compounds, and pharmaceutical formulations comprising the compounds.