Abstract: 4.alpha.,5.alpha.-Epoxy-3,20-dioxopregnane-2.alpha.,16.alpha.-dicarbonitril e is prepared by decyclizing 4.alpha.,5.alpha.-epoxy-20-oxopregn-2-eno-[2,3-d]isoxazole-16.alpha.-carbo nitrile with strong base and is useful as an inhibitor of mineralocorticoid production and/or action without concomitant glucocorticoid inhibition in primates.
Type:
Grant
Filed:
June 19, 1981
Date of Patent:
May 25, 1982
Assignee:
Sterling Drug Inc.
Inventors:
Robert G. Christiansen, Malcolm R. Bell, Harry P. Schane, Jr.
Abstract: 4-Q-9-RR'N-3,4,5,6-tetrahydro-2H-1,5-methano-1,4-benzodiazocines whereinQ is propyl, isobutyl, neopentyl, allyl, 2-methyl-2-propenyl, 2-chloro-2-propenyl, cis-3-chloro-2-propenyl, cis-3-chloro-2-butenyl, trans-3-chloro-2-butenyl, propargyl, cyclopropylmethyl or (2,2-dichlorocyclopropyl)methyl; andR and R' are both hydrogens or both methyls; orR is hydrogen and R' is methyl, ethyl, propyl, butyl, isobutyl or benzyland acid addition salts thereof are useful as strong analgesics and are prepared from the known 3,4,5,6-tetrahydro-2H-1,5-methano-1,4-benzodiazocine by multi-step processes including acylation (including acetylation), nitration, nitro reduction, amide reduction, deacetylation, alkylation and dimethylation.
Abstract: The method of producing anesthesia in a mammal comprising administering intravenously to the mammal an anesthetically effective amount of a pharmaceutically acceptable salt of racemic ketazocine or levo-ketazocine with or without diazepam premedication and the method of producing analgesia in a human which comprises administering intramuscularly to the human an anesthetically effective amount of at least 1 mg. of a pharmaceutically acceptable salt of racemic ketazocine or levo-ketazocine are disclosed.
Abstract: A method of treating dermatological conditions associated with androgenic stimulatory influence which comprises applying to the affected skin area a composition comprising an antiandrogenically and glucocorticoidally effective amount of 17.beta.-hydroxy-6.alpha.-methyl-17.alpha.-propynyl-4-androsteno[3,2-c]pyr azole in a pharmaceutical formulation suitable for topical application is disclosed.
Abstract: A method of making 2,4,5-trichlorophenol by chlorinating 2,5-dichlorophenol is characterized by reacting 2,5-dichlorophenol with chlorine in the presence of a liquid inert polar aprotic reaction medium such as nitrobenzene or a chlorinated hydrocarbon reaction medium, particularly 1,2-dichloroethane, and preferable a Lewis acid catalyst, particularly aluminium chloride. The product contains a higher ratio of 2,4,5-trichlorophenol to 2,3,6-trichlorophenol than has been obtainable previously.
Abstract: Substituted 3,3-diphenylphthalides, useful as color precursors, particularly in the art of pressure-sensitive duplicating systems and heat-sensitive marking systems, are prepared by condensing substituted 2-benzoylbenzoic acids with substituted anilines.
Abstract: The method of producing anesthesia in a mammal comprising administering intravenously to the mammal an anesthetically effective amount of a pharmaceutically acceptable salt of racemic ketazocine or levo-ketazocine with or without diazepam premedication and the method of producing analgesia in a human which comprises administering intramuscularly to the human an anesthetically effective amount of at least 1 mg. of a pharmaceutically acceptable salt of racemic ketazocine or levo-ketazocine are disclosed.