93652-23-4

Upstream product

• 74882-32-9 1,5-bis(4-methoxyphenyl)pentan-3-one 
• 96415-68-8 1,5-Bis-<4-benzoyloxy-phenyl>-pentanon-(3) 
• 2051-07-2 1,5-bis-(4-methoxyphenyl)-1,4-pentadien-3-one 
• 123-11-5 4-methoxy-benzaldehyde 
• 96469-58-8 1,5-bis-(4-benzoyloxy-phenyl)-penta-1,4-dien-3-one 
• 60-29-7 diethyl ether 

Downstream Products

• 137569-07-4 C₄₅H₅₀O₅ 
• 10365-62-5 4,4'-pentanediyl-di-phenol 

Relevant academic research and scientific papers

Symmetrical bis(heteroarylmethoxyphenyl)alkylcarboxylic acids as inhibitors of leukotriene biosynthesis

Symmetrical bis(quinolylmethoxyphenyl)alkylcarboxylic acids were investigated as inhibitors of leukotriene biosynthesis and 4,4-bis(4-(2-quinolylmethoxy)phenyl)pentanoic acid sodium salt (47·Na) met our design parameters for a drug candidate (ABT-080). This compound was readily synthesized in three steps from commercially available diphenolic acid. Against intact human neutrophils, 47·Na inhibited ionophore-stimulated LTB4 formation with an IC50 = 20 nM. In zymosan-stimulated mouse peritoneal macrophages producing both LTC4 and PGE2, 47·Na showed 9000-fold selectivity for inhibition of LTC4 (IC50 = 0.16 nM) over PGE2 (IC50 = 1500 nM). Preliminary pharmacokinetic evaluation in rat and cynomolgus monkey demonstrated good oral bioavailability and elimination half-lives of 9 and 5 h, respectively. Pharmacological evaluation of leukotriene inhibition with oral dosing was demonstrated in a rat pleural inflammation model (ED50 = 3 mg/kg) and a rat peritoneal passive anaphylaxis model (LTB4, ED50 = 2.5 mg/kg; LTE4, ED50 = 1.0 mg/kg). In a model of airway constriction induced by antigen challenge in actively sensitized guinea pigs, 47·Na dosed orally blocked bronchoconstriction with an ED50 = 0.4 mg/kg, the most potent activity we have observed for any leukotriene inhibitor in this model. The mode of inhibitory action of 47·Na occurs at the stage of 5-lipoxygenase biosynthesis as it blocks both leukotriene pathways leading to LTB4 and LTC4 but not PGH2 biosynthesis. However, 47·Na does not inhibit 5-lipoxygenase catalysis in a broken cell enzyme assay; therefore it is likely that 47·Na acts as a FLAP inhibitor.

Symmetrical bis-heteroarylmethoxyphenyliminoxyalkyl carboxylates as inhibitors of leukotriene biosynthesis

Compounds having the formula: STR1 or a pharmaceutically acceptable salt thereof wherein W and Y at each occurrence are the same and W is selected from the group consisting of optionally substituted quinolyl, optionally substituted benzothiazolyl, optiona

Bisbenzoxazines and pharmaceutical use

Compounds of the formula: STR1 wherein, R is H, alkyl, cycloalkyl, aryl, or heteroaryl; R1 is H, alkyl, cycloalkyl, aryl, heteroaryl, substituted heteroaryl, aralkyl, substituted aryl, halo, OR2, SR2, NR2, CF3, NO2, CN, COOR2, CHO, SO3 H or SO2 NH2, wherein R2 is H, methyl, ethyl or propyl; Y is STR2 Z is O, S, NH or CH2 ; X is --CH2 --, STR3 or --(CH2)n CHOH(CH2)n --; wherein R2 is H, methyl, ethyl or propyl; n is 1-10, and pharmaceutically acceptable salts thereof have antiallergy and antiinflammatory activity.