Abstract: A genus of tripeptide amides and fifteen species thereof of Examples 4-18, which are useful as analgesics and/or opiate antagonists, three processes for preparation thereof, pharmaceutical compositions thereof, and the three tripeptide amide species of Examples 1-3, which are not within the genus and are useful as analgesics and/or opiate antagonists, are disclosed.
Abstract: Antiplaque dentifrices containing as the antiplaque ingredient the saccharin salt of an amino or quaternary ammonium antimicrobial agent, particularly chlorhexidine saccharin salt or octenidine saccharin salt, and the method of inhibiting, reducing and preventing dental plaque therewith are disclosed.
Type:
Grant
Filed:
December 9, 1983
Date of Patent:
September 30, 1986
Assignee:
Sterling Drug Inc.
Inventors:
William G. Gorman, Karl F. Popp, Kenneth M. Mavica
Abstract: The method of preparing a 2.alpha.-cyano-4.alpha.,5.alpha.-epoxy-3-oxo steroid or a steroid fused at the 2- and 3-positions with a heterocyclic ring of controlled particle size which comprises dissolving the steroid in an organic solvent, precipitating the steroid by mixing a non-solvent for the steroid with the resulting solution, and controlling the time of mixing and the degree of agitation during mixing.
Abstract: N-[1-(alkyl or arylmethyl)-4(1H)-pyridinylidine]-alkanamine and pharmaceutically acceptable acid addition salts thereof, for example, N-(1-octyl-4(1H)-pyridinylidine)octanamine monohydrochloride salt, which are useful as antimicrobial agents, especially on living tissues and nonliving surfaces and most especially against pathogenic dental microbes, and a process for preparation, methods of use and compositions thereof are disclosed.
Abstract: Antimicrobial surface degerming compositions comprising a bis[4-(substituted-amino)-1-pyridinium]alkane, especially octenidine hydrochloride, as the antimicrobial agent, one or more compounds selected from the group consisting of higher-alkyldilower-alkylamine oxides, higher-alkylaminoalkanoic acids, higher-alkyldiloweralkylammoniumalkanoate betaines and quaternary nitrogen-containing cellulose ethers, and an aqueous vehicle, especially antimicrobial skin cleansing compositions and antimicrobial bovine teat dip compositions, and method of use thereof are disclosed.
Type:
Grant
Filed:
March 23, 1984
Date of Patent:
September 17, 1985
Assignee:
Sterling Drug Inc.
Inventors:
William G. Gorman, Karl F. Popp, Jennifer C. Galloway, David M. Sedlock
Abstract: A genus of dipeptide amides including as the preferred subgenus the dipeptide amides having the structural formula HTyrD-AlaNR.sub.2 R.sub.3 wherein R.sub.2 is phenylalkyl or substituted-phenylalkyl and R.sub.3 is hydrogen, alkyl, phenylalkyl, substituted-phenylalkyl or X-alkyl wherein X is an electronegative moiety are prepared by condensing the dipeptide with the amine or the amino acid with the amino acid amide and are useful as analgesics.
Abstract: A genus of dipeptide amides including as the preferred subgenus the dipeptide amides having the structural formula R.sub.1 TyrR.sub.2 D-AlaNHR.sub.4 wherein R.sub.1 and R.sub.2 are each hydrogen or alkyl provided that at least one of them is other than hydrogen and R.sub.4 is phenylalkyl or substituted-phenylalkyl are prepared by condensing the dipeptide with the amine or the amino acid with the amino acid amide and are useful as analgesics.
Abstract: N-Terminal L-prolyl or D-prolyl hexapeptide amides useful as Substance P agonists and/or antagonists and as analgesics and/or antihypertensives and a process for preparing them are disclosed.
Abstract: A genus of dipeptide amides including as the preferred subgenus the dipeptide amides having the structural formula R.sub.1 TyrR.sub.2 D-Q-NR.sub.4 R.sub.5 wherein Q is Met, Met(O), Gln or Ser, R.sub.1 and R.sub.2 are each hydrogen or alkyl, R.sub.4 is phenylalkyl or substituted-phenylalkyl and R.sub.5 is hydrogen, alkyl, phenylalkyl, substituted-phenylalkyl or X-alkyl wherein X is an electronegative group are prepared by condensing the dipeptide with the amine or the amino acid with the amino acid amide and are useful as analgesics.
Abstract: A genus of dipeptide amides including as the preferred subgenus the dipeptide amides having the structural formula R.sub.1 TyrProNR.sub.4 R.sub.5 wherein R.sub.1 is hydrogen or alkyl, R.sub.4 is phenylalkyl or substituted-phenylalkyl and R.sub.5 is hydrogen, alkyl, phenylalkyl or substituted-phenylalkyl are prepared by condensing the dipeptide with the amine or the amino acid with the amino acid amide and are useful as analgesics.
Abstract: Basic amino or ammonium antimicrobial agent (especially bisbiguanide, quaternary ammonium salt and bispyridine)-polyethylene glycol ester surfactant-betaine and/or amine oxide surfactant antimicrobial skin cleansing compositions and method of use thereof are disclosed.
Abstract: A sustained-release pharmaceutical tablet consisting essentially of drug pellets encapsulated with a water-soluble film-forming substance and a water-insoluble film-forming substance and blended and compressed into tablet form with a compressible tableting mixture and a process for preparation thereof are disclosed.
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: Basic amino or ammonium antimicrobial agent (especially bisbiguanide, quarternary ammonium salt and bispyridine)-polyethylene glycol ester surfactant-betaine and/or amine oxide surfactant antimicrobial skin cleansing compositions and method of use thereof are disclosed.