|1.||Take, K: 1 article (12/2000)|
|2.||Taniguchi, K: 1 article (12/2000)|
|3.||Tsubaki, K: 1 article (12/2000)|
|4.||Okumura, K: 1 article (12/2000)|
|5.||Shiokawa, Y: 1 article (12/2000)|
|1.||Overactive Urinary Bladder (Overactive Bladder)
12/01/2000 - "Asymmetric synthesis and determination of the absolute configuration of FK584, an agent for the treatment of overactive detrusor."
12/01/2000 - "FK584[(-)-N-tert-butyl-4,4-diphenyl-2-cyclopentenylamine hydrochloride, (-)-4-HCl], a potential candidate for the treatment of overactive detrusor, was synthesized in a 4-step approach starting with Sharpless oxidation of cyclopentenol 6 (kinetic resolution). "
10/01/1996 - "Using di-p-toluoyltartaric acid as a resolving agent, the synthetic (+/-)-3 was resolved into its optically pure forms, (-)- and (+)-3. The (-)-enantiomer (-)-3.HCl (FK584) showed about ten times more potent inhibitory activity on urinary bladder rhythmic contraction in rats (ED30 = 0.18 mg/kg, i.v.) than terodiline (ED30 = 1.9 mg/kg, i.v.), while the (+)-enantiomer (+)-3.HCl showed no inhibitory activity at 1.0 mg/kg i.v. Compound (-)-3.HCl (FK584) has pharmacological properties similar to those of terodiline, as evaluated by in vitro assay and is currently in clinical development for the treatment of overactive detrusor."
|2.||terodiline (TD 758)