Organic compounds -- part of the class 532-570 series – Organic compounds – Heterocyclic carbon compounds containing a hetero ring...
Patent
1981-09-28
1983-08-02
Daus, Donald G.
Organic compounds -- part of the class 532-570 series
Organic compounds
Heterocyclic carbon compounds containing a hetero ring...
548465, 548492, 548493, C07D51304
Patent
active
043967736
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: 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: 4256751 (1981-03-01), Hayashi et al.
patent: 4303283 (1981-12-01), Kim et al.
patent: 4310461 (1982-01-01), Krapcho et al.
Schor, (Chairman), "Program Gordon Research Conferences," Aug., 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 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, 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).
Kim Dong H.
McCaully Ronald J.
American Home Products Corporation
Daus Donald G.
Hendricks G. M.
Seifert Arthur G.
LandOfFree
1,1'-[Dithiobis(2-alkyl-1-oxo-3,1-propanediyl)]-bis[2,3-dihydro- does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with 1,1'-[Dithiobis(2-alkyl-1-oxo-3,1-propanediyl)]-bis[2,3-dihydro-, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and 1,1'-[Dithiobis(2-alkyl-1-oxo-3,1-propanediyl)]-bis[2,3-dihydro- will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-484885