2-fluoroalkyl-1,4-benzoxaxines as potassium channel mediators

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...

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5142305, 544101, 544105, A61K 31535, C07D26536, C07D26538

Patent

active

054865158

ABSTRACT:
Compounds of formula I ##STR1## wherein X.sup.a, X.sup.b, R, R.sup.1 and R.sup.2 have any of the meanings given in the specification, and their pharmaceutically acceptable salts are useful as potassium channel openers for the treatment of urinary incontinence. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.

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K. Russell et al., "A Highly Potent Series of Fluoroalkyl Benzoxazine Pyridine-N-Oxide Potassium Channel Openers," Bioorganic & Medicinal Chemistry Letters, 3(12), 2727-2728, 1993.
Ashely E. Fenwick "The Synthesis of 2,2-Bis(Trifluoromethyl) Benzopyran Derivatives: A New Route to an Important Class of Potassium Channel", Tetrahedron Letters, (1993), 34, No. 11, 1815-1818.
Hiroshi Koga et al. "Synthesis and Antihypertensive Activity of KC-399, A Benzopyran K+ Channel Opener with Long Duration of Action and Less Tachycardia", Bioorganic & Medicinal Chemistry Letters, (1993), 3, No. 10, 2005-2010.
Derek R. Buckle et al. "Relaxant Activity of 4-Amido-3,4-dihydro-2H-1-benzopyran-3-ols and 4-Amido-2H-1-benzopyrans on Guinea Pig Isolated Trachealis", J. Med. Chem., (1990), 33, 3028-3034.

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