Organic compounds -- part of the class 532-570 series – Organic compounds – Heterocyclic carbon compounds containing a hetero ring...
Patent
1982-06-22
1984-06-12
Daus, Donald G.
Organic compounds -- part of the class 532-570 series
Organic compounds
Heterocyclic carbon compounds containing a hetero ring...
C07D20942
Patent
active
044542917
ABSTRACT:
Disclosed herein are 2,3-dihydro-1H-indole-2-carboxylic acids substituted on the nitrogen with 3-mercapto-2-alkyl-1-oxoalkyl, 3-phosphoryl-2-alkyl-1-oxopropyl, or 2-amino-2-alkyl-1-oxoalkyl derivatives which act as inhibitors of angiotensin converting enzyme and as antihypertensive agents. The compounds of the invention (excluding disclosed intermediates) have the general formula: ##STR1## wherein: n is 1 or 0;
REFERENCES:
patent: 3780062 (1975-12-01), 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: 4251444 (1981-02-01), Freed et al.
patent: 4256751 (1981-03-01), Hayashi et al.
Hackh's Chemical Dictionary, fourth edition, J. Grant, editor, McGraw-Hill, N.Y. (1969), p. 595.
Ondetti, M. A., "Orally Active Angiotensin-Converting Enzyme Inhibitors", Gordon Research Conference-Medicinal Chemistry, Colby-Sawyer College, New London, New Hampshire (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).
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).
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 Antiogensin-Converting Enzyme", Prog. in Cardiovasc. Diseases, XXI, No. 3, 176-182 (Nov./Dec., 1978).
Kim Dong H.
McCaully Ronald J.
American Home Products Corporation
Daus Donald G.
Eakin M. C.
Seifert Arthur G.
LandOfFree
N-(2-Substituted-1-oxoalkyl)-2,3-dihydro-1H-indole-2-carboxylic does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with N-(2-Substituted-1-oxoalkyl)-2,3-dihydro-1H-indole-2-carboxylic , we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and N-(2-Substituted-1-oxoalkyl)-2,3-dihydro-1H-indole-2-carboxylic will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-122333