Organic compounds -- part of the class 532-570 series – Organic compounds – Heterocyclic carbon compounds containing a hetero ring...
Patent
1981-09-28
1983-05-24
Bond, Robert T.
Organic compounds -- part of the class 532-570 series
Organic compounds
Heterocyclic carbon compounds containing a hetero ring...
2602393T, 424200, 424274, 548414, 548492, C07D51304
Patent
active
043851800
ABSTRACT:
Disclosed herein are N-(3-mercapto-2-alkyl-1-oxopropyl)-2,5-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 5-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: 3780062 (1973-12-01), Kaiser et al.
patent: 3796723 (1974-03-01), Kaiser et al.
patent: 4046889 (1977-09-01), Ondetti et al.
patent: 4105776 (1978-08-01), Ondetti et al.
patent: 4181799 (1980-01-01), White
patent: 4192945 (1980-03-01), Ondetti
patent: 4225495 (1980-09-01), Ondetti
Laragh, John H., "The Renin System in High Blood Pressure, From Disbelief to Reality: Converting-Enzyme Blockade for Analysis & Treatment", Prog. in Cardiovasc. Diseases, XXI, No. 3, 159-166, (Nov./Dec., 1978).
Oparil, Suzanne, "Angiotensin I Converting Enzyme Inhibitors", Chapter 6.3 in Hypertension, (McGraw-Hill, 1977).
Cushman et al., "Design of New Antihypertensive Drugs: Potent and Specific Inhibitors of Angiotensin-Converting Enzyme", Prog. in Cardiovasc. Diseases, XXI, No. 3, 1976-182, (Nov./Dec., 1978).
Cushman et al., "Design of Potent Competitive Inhibitors of Angiotensin-Converting Enzyme, Carboxyalkanoyl and Mercaptoalkanoyl Amino Acids", Biochemistry, 16, 5484-5491, (1977).
Gavras et al., "Antihypertensive Effect of the Oral Angiotensin Converting-Enzyme Inhibitor SQ 14225 in Man", N. Engl. J. Med., 298, 991-995, (May, 1978).
Wong et al., "The In Vitro Metabolism of .sup.35 S-Captopril (SQ 14,225) An Antihypertensive Agent", The Pharmacologist, 20, 213, Abstract No. 345, (1978).
Ondetti, M. A., "Orally Active Angiotensin-Converting Enzyme Inhibitors", Gordon Research Conference-Medicinal Chemistry, Colby-Sawyer College, New London, N.H., (Jul. 31-Aug. 4, 1978): Program Handout (4 pages).
Soffer et al., "Physiologic, Biochemical, and Immunologic Aspects of Angiotensin-Converting Enzyme", Prog. in Cardiovasc. Diseases, XXI, 167-175, (Nov./Dec., 1978).
Goodman and Gilman, The Pharmacological Basis of Therapeutics, pp. 228-229, (MacMillan Publishing Co., New York, NY, 1975).
Kim Dong H.
McCaully Ronald J.
American Home Products Corporation
Bond Robert T.
Seifert Arthur G.
LandOfFree
10,10a-Dihydro-1H-thiozino[4,3-a,]-indole-1,4(3H)-diones does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with 10,10a-Dihydro-1H-thiozino[4,3-a,]-indole-1,4(3H)-diones, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and 10,10a-Dihydro-1H-thiozino[4,3-a,]-indole-1,4(3H)-diones will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-2147162