58228-89-0Relevant academic research and scientific papers
Chroman Compound, Processes for Its Preparation, and Its Pharmaceutical Use
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Page/Page column 8, (2008/06/13)
The present invention provided a chroman compound, the method of its preparation and pharmaceutical applications. The compound are represented by formula (I) and its pharmaceutical salt, where in :x is for O or S; n is for 2, 3 or 4; R1 is 6-situ or 7-situ halogen, C1-4alkyl, C1-4alkyoxyl, benzyloxy, acylamino; R2 is nitrogen-containing pentatomic or hexahydric substituted heterocyclic ring. The compound is useful to prepare anti-arrhythmic drugs, the reaction conditions of the method are mild, the raw material are plenty and easy to be obtained, and the operation and post-treatment are simple.
Conformational and Steric Modifications of the Pyran Ring of the Potassium-Channel Activator Cromakalim
Buckle, Derek R.,Eggleston, Drake S.,Houge-Frydrych, Catherina S. V.,Pinto, Ivan L.,Readshaw, Simon A.,et al.
, p. 2763 - 2772 (2007/10/02)
The syntheses of analogues of the novel smooth muscle relaxant cromakalim, in which the C-2 methyl groups have been successively replaced by hydrogen, are described and the relative stereochemistry of the two corresponding, isomeric monomethyl compounds,
Spiro hydantoin aldose reductase inhibitors
Sarges,Schnur,Belletire,Peterson
, p. 230 - 243 (2007/10/02)
Sorbitol formation from glucose, catalyzed by the enzyme aldose reductase, is believed to play a role in the development of certain chronic complications of diabetes mellitus. Spiro hydantoin derived from five- and six-membered ketones fused to an aromatic ring or ring system inhibit aldose reductase isolated from calf lens. In vivo these compounds are potent inhibitors of sorbitol formation in sciatic nerves of streptozotocinized rats. Optimum in vivo activity is reached in spiro hydantoins derived from 6-halogenated 2,3-dihydro-4H-1-benzopyran-4-ones (4-chromanones). In 2,4-dihydro-6-fluorospirol[4H-1-benzopyran-4,4'-imidazolidine]-2',5'- ione, the activity resides exclusively in the 4S isomer, compound 115 (CP-45,634, USAN: sorbinil). This compound is currently being used to test, in humans, the value of aldose reductase inhibitors in the therapy of diabetic complications.
