1H,5H-[1,4]Thiazepino[4,3-a]indole-1,5-diones

Details 1H,5H-[1,4]Thiazepino[4,3-a]indole-1,5-diones 1H,5H-[1,4]Thiazepino[4,3-a]indole-1,5-diones

1980-07-01

1981-12-01

Bond, Robert T.

Chemistry of carbon compounds

Miscellaneous organic carbon compounds

C-metal

26032612R, 26032613C, 26032613D, 424274, 424200, 544 32, C07D51304

Patent

active

043035833

ABSTRACT:
Disclosed herein are N-(3-mercapto-2-alkyl-1-oxopropyl)-2,3-dihydro-1H-indole-2-carboxylic acids and derivatives thereof which act as inhibitors of angiotensin converting enzyme and as anti-hypertensive agents. Derivatives include those in which the 3-mercapto group is substituted with phosphate derivatives or is replaced by a variously substituted amino group. The compounds of the invention (excluding disclosed intermediates) have the general formula: ##STR1## wherein: n is 1 or 0;

REFERENCES:
patent: 4046889 (1977-09-01), Ondetti et al.
patent: 4105776 (1978-08-01), Ondetti et al.
Genest et al., (Editors), "Hypertension", (McGraw-Hill) (1977), pp. 134-155, 260-311.
Laragh, "Progress in Cardiovascular Diseases", Nov.-Dec., 1978, vol. 21, No. 3, pp. 159-166.
Oparil, "Hypertension", (McGraw-Hill) (1977), pp. 156-167.
Cushman et al., "Progress in Cardiovascular Diseases", vol. 21, No. 3, (Nov.-Dec. 1978), pp. 176-182.
Cushman et al., "Biochemistry", vol. 16, No. 25, 1977, pp. 5484-5491.
Gavras et al., "New England Journal of Medicine", vol. 298, No. 18, (1978), pp. 991-995.
Wong et al., "The Pharmacologist", vol. 20, p. 213, Abstract No. 345 (1978).
Soffer et al., "Progress in Cardiovascular Diseases", vol. 21, No. 3, (Nov.-Dec. 1978), pp. 167-175.
Ondetti, "Gordon Research Conference-Medicinal Chemistry", Colby-Sawyer College, (1978), (Handout), 4 pages, (New London, New Hampshire).

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