853368-32-8

Upstream product

• 128-08-5 N-Bromosuccinimide 
• 261952-06-1 4-methyl-3-(trifluoromethyl)benzonitrile 

Downstream Products

• 1312704-85-0 4-((5-formylindazol-1-yl)methyl)-3-(trifluoromethyl)benzonitrile 
• 1422127-53-4 C₂₂H₂₅F₃N₄O₂S 
• 1327335-82-9 4-(5-{2-[Bis-(2-hydroxy-ethyl)-amino]-4-oxo-4H-thiazol-5-ylidenemethyl}-indazol-1-ylmethyl)-3-trifluoromethyl-benzonitrile 
• 1141894-75-8 4?(aminomethyl)?3?(trifluoromethyl)benzonitrile 
• 1246527-37-6 tert-butyl 2-((4-cyano-3-(trifluoromethyl)benzyl)(methyl)amino)acetate 

Relevant academic research and scientific papers

Multigram-scale?synthesis?of GSK 2,256,294, an inhibitor of soluble epoxide hydrolase in clinical evaluation

This paper described the development of an improved, practical and efficient protocol method for the multigram-scale synthesis of GSK 2,256,294, an orally bioavailable potent and selective inhibitor of sEH. The key to this optimization was the design and development of a novel synthetic strategy, which involved the preparation of 4-(aminomethyl)-3-(trifluoromethyl)benzonitrile (3) and 4-chloro-N,6-dimethyl-1,3,5-triazin-2-amine (6). The developed process provided an overall yield of 26.8%, which enabled us to rapidly synthesize large quantities of GSK 2,256,294 in 99% purity. Graphical abstract: [Figure not available: see fulltext.].

Pharmacophore-based design of novel oxadiazoles as selective sphingosine-1-phosphate (S1P) receptor agonists with in vivo efficacy

Sphingosine-1-phosphate (S1P) receptor agonists have shown promise as therapeutic agents for multiple sclerosis (MS) due to their regulatory roles within the immune, central nervous system, and cardiovascular system. Here, the design and optimization of novel [1,2,4]oxadiazole derivatives as selective S1P receptor agonists are described. The structure-activity relationship exploration was carried out on the three dominant segments of the series: modification of the polar head group (P), replacement of the oxadiazole linker (L) with different five-membered heterocycles, and the use of diverse 2,2′-disubstituted biphenyl moieties as the hydrophobic tail (H). All three segments have a significant impact on potency, S1P receptor subtype selectivity, physicochemical properties, and in vitro absorption, distribution, metabolism, excretion and toxicity (ADMET) profile of the compounds. From these optimization studies, a selective S1P1 agonist, N-methyl-N-(4-{5-[2-methyl-2′-(trifluoromethyl)biphenyl-4-yl]-1,2,4-oxadiazol-3-yl}benzyl)glycine (45), and a dual S1P1,5 agonist, N-methyl-N-(3-{5-[2′-methyl-2-(trifluoromethyl)biphenyl-4-yl]-1,2,4-oxadiazol-3-yl}benzyl)glycine (49), emerged as frontrunners. These compounds distribute predominantly in lymph nodes and brain over plasma and induce long lasting decreases in lymphocyte count after oral administration. When evaluated head-to-head in an experimental autoimmune encephalomyelitis mouse model, together with the marketed drug fingolimod, a pan-S1P receptor agonist, S1P1,5 agonist 49 demonstrated comparable efficacy while S1P1-selective agonist 45 was less potent. Compound 49 is not a prodrug, and its improved property profile should translate into a safer treatment of relapsing forms of MS.

Pesticidal compositions and processes related thereto

This document discloses molecules having the following formula (“Formula One”): and processes associated therewith.

PESTICIDAL COMPOSITIONS AND PROCESSES RELATED THERETO

This document discloses molecules having the following formula (“Formula One”): and processes associated therewith.

PESTICIDAL COMPOSITIONS AND PROCESSES RELATED THERETO

This document discloses molecules having the following formula ("Formula One"): and processes associated therewith.

PESTICIDAL COMPOSITIONS AND PROCESSES RELATED THERETO

This document discloses molecules having the following formula (“Formula One”): and processes associated therewith.

PESTICIDAL COMPOSITIONS AND PROCESSES RELATED THERETO

This document discloses molecules having the following formula ("Formula One") and processes associated therewith.

PESTICIDAL COMPOSITIONS AND PROCESSES RELATED THERETO

This document discloses molecules having the following formula (“Formula One”): and processes associated therewith.

SUBSTITUTED AMINOTHIAZOLONE INDAZOLES AS ESTROGEN RELATED RECEPTOR-ALPHA MODULATORS

The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalacia, osteoporosis, Paget's disease, periodontal disease, polymyalgia rheumatica, Reiter's syndrome, repetitive stress injury, hyperglycemia, elevated blood glucose level, and insulin resistance.

AMINOTHIAZOLONES AS ESTROGEN RELATED RECEPTOR-ALPHA MODULATORS

The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalacia, osteoporosis, Paget's disease, periodontal disease, polymyalgia rheumatica, Reiter's syndrome, repetitive stress injury, hyperglycemia, elevated blood glucose level, and insulin resistance.