Abstract: Pyridobenzodioxin compounds, which are useful as pharmacological agents, especially as agents for the treatment of senility and reversal of amnesia, and methods for their preparation are disclosed. Pharmaceutical compositions containing said compounds and methods for using said compositions in treating senility and reversal of amnesia are also taught.
Abstract: An intravenous catheter apparatus comprising an intravenous catheter tube, a manually guidable circumferentially deformable elastomeric bore-defining tubular inserter integral with and in axial alignment with the catheter tube for use with a patient, and a needle concentric within the catheter tube and inserter and extending through at least part of the bore of the inserter to beyond the distal end of the catheter tube, the inserter comprising opposed laterally extending wings adapted to be manually compressed together from an at-rest position to a needle control position, the bore of the inserter being sufficiently large to permit retraction of the needle from the catheter tube and the inserter when the inserter is at rest, and when the inserter wings are compressed to the needle control position being sufficiently constricted to enable the inserter to grip the needle firmly to permit inserter-forced injection of the distal end of the needle into the body of a patient.
Abstract: Antihemophilic factor (AHF) concentrate having enhanced potency and solubility and its process of production are provided. The process includes the steps of removing unwanted protein from an aqueous extract of antihemophilic blood plasma cryoprecipitate by mixing the aqueous extract with aluminum hydroxide at an acid pH in the cold, adjusting the purified aqueous extract to an acid pH and freeze-drying the extract, optionally removing water from the extract just before freeze-drying.
Type:
Grant
Filed:
July 10, 1978
Date of Patent:
October 9, 1979
Assignee:
Warner-Lambert Company
Inventors:
Daniel T. H. Liu, John F. Irwin, Rong-Chang Pai
Abstract: 3,3'-Thiodimethylenebis 2-[(dialkylamino)methyl]indole compounds having in free base form the formula ##STR1## where R.sub.1 and R.sub.2 are lower alkyl groups. The compounds of this invention exhibit antifungal and CNS depressant properties and can be used as antifungal agents or CNS depressant agents.
Abstract: .beta.-[2-[(DIALKYLAMINO)METHYL]-1H-indol-3-yl]-.alpha.,.alpha.-diphenylpro pionitriles and 4-[[2-[(dialkylamino)methyl]-1H-indol-3-yl]methyl]-2,4-dihydro-5-lower alkyl-2-phenyl-3H-pyrazol-3-ones and acid addition salts thereof which are useful pharmacological agents, especially as central nervous system depressants, are disclosed. The compounds can be produced by reacting an anion of an acetonitrile or a pyrazol-3-one with the appropriate quatenary salt of 2-alkyl-1,2,3,4-tetrahydropyrrolo[3,4-b]indole.
Abstract: 3-[2-(Dialkylamino)ethyl]-2-(benzyl)indoles having in free base form the formula ##STR1## where R.sub.1 and R.sub.2 are lower alkyl groups and R.sub.3 is a phenyl, carboalkoxymethyl, lower alkyl or hydroxyethyl group. The compounds of the invention exhibit anti-aggression and anti-secretory properties and are indicated in the management of aggression and gastric hypersecretion.
Abstract: N-(substituted-aminoalkyl)-2-oxo-1-pyrrolidineacetamides which are useful as pharmacological agents, especially cognition activators, are disclosed. They can be produced by reacting a 2-oxo-1-pyrrolidineacetate ester with an appropriate amine.
Abstract: O-2,6-Diamino-2,3,6-trideoxy-.alpha.-D-ribo-hexopyranosyl-(1.fwdarw.4)-O-?. beta.-D-xylofuranosyl-(1.fwdarw.5)!-N.sup.1 -?(S)-4-amino-2-hydroxy-1-oxobutyl!-2-deoxystreptamine, also known as 3'-deoxybutirosin A and acid addition salts of said compound. These compounds exhibit a wide spectrum of antibacterial activity.
Abstract: Lower alkyl 2-oxo-4-phenyl-1-pyrrolidineacetic acid esters which are useful as pharmacological agents, especially cognition activators, are disclosed. They can be produced by reacting 4-phenyl-2-pyrrolidinone with a lower alkyl haloacetate in the presence of a strong base.
Abstract: N,N-dialkyl-3-[(phenylthio)methyl]-1H-indole-2-methanamines or 3-(1H-imidazol-1-ylmethyl)-N,N,-dimethyl-1H-indole-2-methanamines and acid addition salts thereof which are useful pharmacological agents, especially antifungals, are disclosed. The compounds can be produced by reacting a thiophenols or imidazoles with the appropriate 2-alkyl-1,2,3,4-tetrahydropyrrolo[3,4-b]indole.
Abstract: Pharmaceutical capsules with telescopically engaged body and cap portions, also known as hard shell capsules, having enteric properties. The capsule body and cap portions are formed by dip-molding using a homogeneous film-forming mixture comprising (1) hydroxypropyl methylcellulose and an ammonium salt of cellulose acetate phthalate polymer, or (2) gelatin and an ammonium salt of a copolymer of methacrylic acid and methacrylic acid alkyl ester; optionally with the inclusion of plasticizer and/or coloring agent. The capsules are soluble in or disintegrated by the alkaline intestinal secretions but are substantially insoluble or resistant to solution in the acid secretions of the stomach.
Abstract: Novel organic amide compounds which are N-[6-[(aminosulfonyl)phenyl]-1,2-dihydro-2-oxonicotinyl]penicillin and cephalosporin type compounds having broad spectrum antibacterial utility are provided by (a) reacting the free amino acid of the appropriate penicillin or cephalosporin or the acid salt or silylated derivative or complex thereof with a reactive derivative of the corresponding N-6-[(aminosulfonyl)phenyl]-1,2-dihydro-2-oxonicotinic acid or (b) reacting the free amino acid 6-aminopenicillanic acid, 7-aminocephalosporanic acid, 7-amino-3-methylceph-3-em-4-carboxylic acid or a related compound or the acid salt or silylated derivative thereof with a reactive derivative of the corresponding D-N-[6-[(aminosulfonyl)phenyl]-1,2-dihydro-2-oxonicotinyl]-2-substituted glycine. Pharmaceutical compositions containing said compounds and methods for treating infections using said compositions are also disclosed.
Type:
Grant
Filed:
October 27, 1977
Date of Patent:
January 30, 1979
Assignee:
Warner-Lambert
Inventors:
James S. Kaltenbronn, Theodore H. Haskell, Leonard Doub
Abstract: Pyrrolo[1,2-a]indole compounds having in free base form the formulas ##STR1## where R.sub.1, R.sub.2 and R.sub.3 are lower alkyl; R.sub.4 is lower alkyl, phenyl, lower alkoxy or ##STR2## in which R.sub.8 and R.sub.9 are hydrogen, lower alkyl, phenyl or benzyl; R.sub.5 is hydrogen or lower alkyl; A is O or NH; and R.sub.6 and R.sub.7 are lower alkyl, phenyl, or carbo(lower)alkoxy.
Abstract: Bis(2-[(disubstitutedamino)methyl]-1H-indole) compounds wherein said 2-[(disubstitutedamino)methyl]-1H-indol-3-ylmethylene moieties are linked together through a piperazine or 1,3-dihydro-2H-indol-2-one fragment and acid addition salts thereof which are useful pharmacological agents, especially antifungals, are disclosed. The compounds can be produced by reacting a piperazine or 1,3-dihydro-2H-indole-2-one compound with the appropriate quaternary salt of 2-alkyl-1,2,3,4-tetrahydropyrrolo-[3,4-b]indole.
Abstract: 3-Phenoxypyridine monosulfate, a pharmacological agent possessing mood elevating and cardiotonic properties. This compound is produced by reacting 3-phenoxypyridine with an equivalent amount of sulfuric acid.
Abstract: A new decapeptide having the formula, pGlu-His-Trp-Ser-Tyr-Gly-Leu-NO.sub.2 Arg-Pro-Gly(NH.sub.2); salts thereof; production thereof by reacting pGlu-His-Trp-Ser-Tyr(N.sub.3) with Gly-Leu-NO.sub.2 Arg-Pro-Gly(NH.sub.2), by reacting pGlu-His-Trp-Ser-Tyr-Gly(N.sub.3) with Leu-NO.sub.2 Arg-Pro-Gly(NH.sub.2), or by reacting pGlu-His-Trp-Ser-Tyr-Gly-Leu(N.sub.3) with NO.sub.2 Arg-Pro-Gly(NH.sub.2); certain peptide intermediates and their salts used in the production thereof; and the use thereof in the preparation of luteinizing hormone releasing factor.
Type:
Grant
Filed:
May 25, 1972
Date of Patent:
December 5, 1978
Assignee:
Parke, Davis & Company
Inventors:
Mildred C. Rebstock, Ernest D. Nicolaides, Thomas F. Mick, Francis J. Tinney, Eugene L. Wittle
Abstract: A process is provided for the production of 2,2-dimethyl-5-(2,5-xylyloxy)valeric acid which comprises subjecting 2,2-dimethyl-5-(2,5-xylyloxy)valeraldehyde to oxidation with elemental oxygen in a three-phase reaction mixture comprising a water immiscible organic solvent for said valeraldehyde, an aqueous alkaline solution, and a noble metal catalyst.
Abstract: New nonapeptides having the formula R-Trp-Ser(benzyl)-Tyr(benzyl)-D-Phe-Leu-Arg(X)-Pro-Gly-Y wherein X is a protective group, R is pGlu, protected His(benzyl), protected Ser(benzyl) or protected Cys(benzyl), and Y is lower alkoxy, amino, lower alkylamino or di(lower alkyl)amino.
Type:
Grant
Filed:
June 13, 1977
Date of Patent:
November 7, 1978
Assignee:
Warner-Lambert
Inventors:
Francis J. Tinney, Elizabeth A. Lunney, Ernest D. Nicolaides
Abstract: Process for the production of an ester product, 9-(.beta.-D-arabinofuranosyl)adenine, 5'-phosphate, in which the mixture resulting from reaction of 9-(.beta.-D-arabinofuranosyl)adenine with phosphorylating agent in trialkyl phosphate solvent is subjected to aqueous hydrolysis, the pH of the hydrolysis mixture is adjusted upward sufficiently to cause separation into aqueous and non-aqueous liquid phases, the trialkyl phosphate solvent is removed, and the product is precipitated from the residual aqueous mixture and isolated.
Type:
Grant
Filed:
September 12, 1977
Date of Patent:
October 31, 1978
Assignee:
Warner-Lambert Company
Inventors:
Walter E. Behnke, William R. Marsh, Theodore H. Haskell
Abstract: 2-Amino-1-(5-amino-1H-imidazol-4-yl)ethanone, 6,7-dihydroimidazo[4,5-d][1,3]diazepin-8(3H)-one and acid-addition salts thereof are disclosed. 2-Amino-1-(5-amino-1H-imidazol-4-yl)ethanone and its acid-addition salts are prepared by catalytically reducing an acid-addition salt of 2-amino-1-[5-amino-1-(protected)-1H-imidazol-4-yl]ethanone. 6,7-Dihydroimidazo[4,5-d][1,3]-diazepin-8(3H)-one and its acid-addition salts are prepared by reacting an acid-addition salt of 2-amino-1-(5-amino-1H-imidazol-4-yl)ethanone with a compound able to contribute a formyl group. The later product may subsequently be converted into (R)-3-(2-deoxy-.beta.-D-erythro-pentofuranosyl)-3,6,7,8-tetrahydroimidazo[ 4,5-d][1,3]diazepin-8-ol. Furanose derivatives of 6,7-dihydroimidazo[4,5-d][1,3]diazepine are also disclosed and their methods of preparation. Lastly, a method for resolving an isomer mixture of 3-(2-deoxy-.beta.-D-erythro-pentafuranosyl)-3,6,7,8-tetrahydroimidazo[4 ,5-d][1,3]diazepin-8-ol compounds is related.