Abstract: The novel stereoselective and regioselective alkali metal borohydride reduction of 2,5-diketogluconic acid, alkyl esters or salts thereof to form 2-ketogluconic acid together with lesser amounts of 2-ketogluconic acid is disclosed. The 2-ketogluconic acid is readily converted to ascorbic acid.
Abstract: Novel spiro-oxazolidinediones useful as aldose reductase inhibitors and as therapeutic agents for the treatment of chronic diabetic complications are disclosed. Pharmaceutical compositions containing the novel compounds and a method of treating chronic diabetic complications are also disclosed.
Abstract: Novel 2,3,6-substituted-4-pyrones having activity as prostaglandin antagonists are disclosed, together with intermediates useful for the preparation thereof. Methods of using the compounds of this invention as prostaglandin antagonists are described.
Abstract: 2,5-Diketogluconic acid, alkyl esters or salts thereof, are reduced by an amine-borane to 2-ketogulonic acid, an intermediate for the preparation of ascorbic acid.
Abstract: Novel halogen-substituted benzopyran-4-carboxylic acids, benzothiopyran-4-carboxylic acids and derivatives thereof useful as aldose reductase inhibitors and as therapeutic agents for the treatment of chronic diabetic complications are disclosed. Specific compounds disclosed include 6-phenyl-8-chloro-3,4-dihydro-2H-1-benzopyran-4-carboxylic acid, 6,7-dichloro-3,4-dihydrobenzothiopyran-4-carboxylic acid, 6-chloro-8-methyl-3,4-dihydro-2H-1-benzopyran-4-carboxylic acid, 6,8-dichloro-3,4-dihydro-2H-1-benzopyran-4-carboxylic acid, 6-fluoro-3,4-dihydro-2H-1-benzopyran-4-carboxylic acid, 6-chloro-3,4-dihydro-2H-1-benzopyran-4-carboxylic acid, 6-chloro-dihydro-2H-naphtho[1,2-b]pyran-4-carboxylic acid, 6-chloro-3,4-dihydro-2H-1-benzothiopyran-4-carboxylic acid and 6-chloro-3,4-dihydro-2H-1-benzopyran-4-acetic acid. Also disclosed are pharmaceutical compositions containing the novel compounds and a method of using the novel compounds for the treatment of chronic diabetic complications.
Abstract: A novel dental surveyor for use in analyzing and working upon dental models is disclosed. The surveyor contains one or more vertical tools, such as marking tools, wax relieving tools and tapered tools. Rotation of a spindle received within a sleeve about its longitudinal axis, combined with horizontal sliding of tool housings upon tool support means attached to said spindle, allows the tools to contact the entire surface of a dental model while always remaining oriented in the vertical direction. The surveyor may also be equipped with e.g. a grinding or drilling tool and means for locking such a tool against horizontal movement while in use.
Abstract: Novel spiro-oxazolidindiones useful as aldose reductase inhibitors and as therapeutic agents for the treatment of chronic diabetic complications are disclosed. Pharmaceutical compositions containing the novel compounds and a method of treating chronic diabetic complications are also disclosed.
Abstract: Novel spiro-quinolone hydantoin derivatives useful as aldose reductase inhibitors and as therapeutic agents for the treatment of chronic diabetic complications are disclosed. Pharmaceutical compositions containing the novel compounds and a method of treating chronic diabetic complications are also disclosed. Preferred compounds include spiro[2,3-dihydro-1H,5H-benzo[ij]quinolizin[1,4']imidazolidin]-2',5,5.dbd. -trione and 10-chloro-spiro[2,3-dihydro-1H,5H-benzo[ij]quinolizin[1,4']imidazolidin]-2 ',5,5'-trione.
Abstract: A sprayer for repairing a refractory lining comprising a vertical, axially movable and rotatable nozzle pipe; a stationary housing disposed about a portion of the pipe; a pair of parallel, connected turntables rotatably supported within the housing axial with and through which the pipe freely passes; motor-driven wheels mounted on the undersides of the turntables for supporting the pipe and driving it in either axial direction relative to the housing; and the combination of a first gear mounted on the upperside of one turntable coaxial with and through which the pipe freely passes intermeshed with a second, motor-driven gear mounted on the housing for rotating the pipe together with the wheels.
Abstract: An improved process for the preparation of ascorbic acid and erythorbic acid is disclosed, the improvement comprising the removal of borate impurities from a 2-ketogulonate and a 2-ketogluconate prior to formation of the desired acids by base catalyzed cyclization.
Abstract: Derivatives of oleandomycin, erythromycin A and B, erythromycylamine and erythromycin carbonate, having at the 4"-position an acylamido group, their preparation and use as antibacterial agents are described.
Abstract: Novel spiro-quinolylhydantoin derivatives useful as aldose reductase inhibitors and as therapeutic agents for the treatment of chronic diabetic complications are disclosed. Preferred compounds include spiro[imidazolidin-4,4'-pyrano[3,2-h]quinolin]-2,5-dione and spiro[imidazolidin-4,4'-pyrano[2,3-f]quinolin]-2,5-dione.
Abstract: The reaction of isatoic anhydrides with malononitrile in a reaction-inert solvent in the presence of a base to produce 2-amino-3-cyano-4-hydroxyquinolines and 2-amino-.alpha.,.alpha.-dicyanoacetophenones which are then hydrolyzed and decarboxylated under acid or base conditions to produce 2-amino-4-hydroxyquinolines, useful as intermediates for preparation of 1-oxo-1H-6-alkoxypyrimido[1,2-a]quinoline-2-carboxylic acids and esters of value as antiallergy agents.
Abstract: Derivatives of oleandomycin, its 11-monoalkanoyl, 2-monoalkanoyl and 11,2'-dialkanoyl esters having at the 4"-position an amino group substituted with --C(.dbd.O)--C(.dbd.O)--R.sub.3 or --C(.dbd.S)--C(.dbd.O)--R.sub.3 wherein R.sub.3 is alkyl having from one to four carbon atoms, phenyl, substituted phenyl, or a heterocyclyl group, their preparation and use as antibacterial agents is described.
Abstract: The novel stereoselective and regioselective alkali metal borohydride reduction of 2,5-diketogluconic acid, alkyl esters or salts thereof to form 2-ketogulonic acid together with lesser amounts of 2-ketogluconic acid is disclosed. The 2-ketogulonic acid is readily converted to ascorbic acid.
Abstract: A series of 4"-deoxy-4"-amino-erythromycin A antibacterial agents and their preparation from erythromycin A via 4"-deoxy-4"-oxo-erythromycin A intermediates.
Abstract: Azacycloalkanes, and derivatives thereof, including unsaturated analogs, each of which has at the 3-position a 2-hydroxy-4-substituted phenyl group wherein the 4-position substituent is alkyl which can have an oxygen atom as part of the chain, or aralkyl which can have an oxygen atom as part of the alkyl chain, their use for pharmacological and medicinal purposes, intermediates therefor and processes for their preparation.
Type:
Grant
Filed:
September 13, 1977
Date of Patent:
April 3, 1979
Assignee:
Pfizer Inc.
Inventors:
Thomas H. Althuis, Charles A. Harbert, Michael R. Johnson, Lawrence S. Melvin, Jr.
Abstract: Derivatives of oleandomycin, its 11-monoalkanoyl and 11,2'-dialkanoyl esters having at the 4"-position an amino group substituted with a group having the formula --(CH.sub.2).sub.n --Z--R wherein n is an integer from 2 to 4 when Z is O, S, SO, SO.sub.2 or NH, and n is an integer from 1 to 4 when Z is CO or CHOH, and R is a phenyl, substituted phenyl or a heterocyclyl group, their preparation, and use as antibacterial agents is described.
Abstract: A series of 4"-deoxy-4"-sulfonylamino-oleandomycin antibacterial agents and their preparation from semi-synthetic 4"-deoxy-4"-amino-oleandomycin intermediates.