792172-61-3

Upstream product

• 93830-58-1 diethyl (pyridin-4-yl)borane 
• 102878-14-8 6-chloro-2-naphthalenesulphonic acid 
• 102153-63-9 6-chloronaphth-2-ylsulfonyl chloride 
• 17100-63-9 methyl 4-bromo-3-methoxybenzoate 
• 91-58-7 2-chloronaphthalene 
• 859140-23-1 methyl 3-methoxy-4-(pyridin-4-yl)benzoate 
• 216866-88-5 1-(tert-butoxycarbonyl)-4-(6-chloronaphthalene-2-sulfonyl)piperazine 

Relevant academic research and scientific papers

Design, synthesis, and biological activity of non-basic compounds as factor Xa inhibitors: SAR study of S1 and aryl binding sites

Compound 7 was identified as the active metabolite of 6 by HPLC and mass spectral analysis. Modification of lead compound 7 by transformation of its N-oxide 6-6 biaryl ring system and fused aromatics produced a series of non-basic fXa inhibitors with excellent potency in anti-fXa and anticoagulant assays. The optimized compounds 73b and 75b showed sub to one digit micromolar anticoagulant activity (PTCT2). Particularly, anti-fXa activity was detected in plasma of rats orally administered with 1 mg/kg of compound 75b.

Sulfonyl derivatives

Sulfonyl derivatives represented by general formula (I), salts of the same, and solvates of both: and application of them as drugs: [wherein R1is hydrogen, hydroxyl, nitro or the like; R2and R3are each independently hydrogen, halogeno or the like; R4and R5are each dependently hydrogen, halogeno or the like; Q1is an optionally substituted saturated or unsaturated 5- or 6-membered cyclic hydrocarbon group or the like; Q2is a single bond, oxygen or the like; Q3is, e.g., a group represented by formula (a): T1is carbonyl or the like; and X1and X2are each independently methylidyne or nitrogen]. These compounds exhibit potent Fxa inhibiting activities and serve as excellent anticoagulants which speedily exert satisfactory and persistent anti-thrombotic effects through oral administration and little cause adverse effects.