Fused thiophene derivatives, their production and use

Details Fused thiophene derivatives, their production and use Fused thiophene derivatives, their production and use

1993-04-19

1994-02-08

Page, Thurman K.

Drug, bio-affecting and body treating compositions

Preparations characterized by special physical form

Tablets, lozenges, or pills

5142338, 514253, 514301, 514321, 514258, 544127, 544362, 544278, 546114, 546198, A61K 920, C07D49504

Patent

active

052846610

ABSTRACT:
Novel fused thiophene derivatives of the formula (I): ##STR1## wherein W is ##STR2## R.sup.1 and R.sup.2 which may be same or different, are each independently hydrogen, halogen, cyano, nitro, acylamino, or a hydrocarbon residue which may be substituted; R.sup.3 is hydrogen, optionally substituted alkyl or alkenyl, or --COD wherein D is hydrogen, alkoxy, hydroxy, halogen, or optionally substituted amino; R.sup.4 is hydrogen, halogen or nitro; R.sup.5 is a residue capable of forming an anion or a residue convertible into an anion; R.sup.6 is hydrogen or optionally substituted alkyl or alkenyl; A is a direct bond or a spacer having atomic length of two or less between the phenylene group and the phenyl group; and n is an integer of 1 or 2; and the pharmaceutically acceptable salts thereof have potent angiotensin II antagonist activity and antihypertensive activity, thus being useful as therapeutic agents for treating circulatory system diseases such as hypertensive diseases, heart diseases, strokes, etc.

REFERENCES:
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patent: 4835157 (1989-05-01), Press
patent: 4880804 (1989-11-01), Carini et al.
CA 89:129437q (1978) Synthesis and antibacterial evaluation of 4,7-dihydro-4-oxothieno[2,3-b]pyridine-5-carboxylic acids by Gilis et al.
Ronald K. Russell et al., "Thiophene Systems. 9. Thienopyrimidinedione Derivatives as Potential Antihypertensive Agents", J. Med. Chem. 1988, vol. 31, pp. 1786-1793.
Chemical Abstracts, 99(3): 22419q (Jul. 19, 1983), p. 616, Colombus, Ohio.
Pancras C. Wong et al., "Nonpeptide Angiotensin II Receptor Antagonists. IV. EXP6155 and EXP6803" Hypertension, vol. 13 (1989), pp. 489-497, Dallas, Texas.
Pancras C. Wong et al., "Nonpeptide Angiotensin II Receptor Anatgonists. I. Pharmacological Characterization of 2-n-Butyl-4-chloro- . . . ", J. Pharm. and Exper. Therapeutics, vol. 247, No. 1 (Oct. 1988) pp. 1-7.

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