Abstract: The present invention is concerned with novel tricyclic sulphoximides and with the preparation thereof. This family of compounds has been found to possess antihistaminic, antitussive, antiinflammatory, sedative, and diuretic properties.
Type:
Grant
Filed:
August 12, 1974
Date of Patent:
November 16, 1976
Assignee:
Warner-Lambert Company
Inventors:
Peter Stoss, Gerhard Satzinger, Manfred Herrmann
Abstract: An improved composition and method for detecting fibrinogen, fibrinogen split products and/or fibrin split products in blood comprises utilizing killed, dyed Staphylococcus aureus cells which can be prepared by either of two methods. In the first method, Staphylococcus aureus organisms are incubated in a nutrient medium containing a polyalkylene glycol having a molecular weight of from 1000 to 5000 to which is added triphenyltetrazolium chloride; the growing organisms reduce the triphenyltetrazolium chloride to triphenylformazan which imparts coloration to the cells; the dyed Staphylococcus aureus cells are killed and substantially all untrapped dye is removed. In an alternate method, a suspension of Fast Black Salt K is added to a suspension of killed Staphylococcus aureus cells, and the dyed cells which result are washed to remove substantially all unfixed dye. The killed, dyed Staphylococcus aureus cells prepared by either method are suspended in an imidazole buffer to maintain a pH of 7.4.
Type:
Grant
Filed:
March 7, 1975
Date of Patent:
November 9, 1976
Assignee:
Warner-Lambert Company
Inventors:
James R. Butler, Walter E. Jacobson, Donald Paul Kronish, James E. Turner, Lee S. Zuriff
Abstract: This invention relates to novel substituted benzo[c][2,7]naphthyridines and their preparation. The compounds of this invention are active as bronchodilators.
Type:
Grant
Filed:
January 17, 1975
Date of Patent:
November 9, 1976
Assignee:
Warner-Lambert Company
Inventors:
Richard E. Brown, Chester Puchalski, John Shavel, Jr.
Abstract: Compounds of the formula: ##SPC1##Are disclosed. In this structural formula X is ##SPC2##And Y is hydrogen, lower alkyl, hydroxy, lower alkoxy, chloro, bromo or aryl. Included within the scope of this invention are tautomers of the above compound. These compounds and their tautomers are indicated in the management of allergic manifestations such as bronchial asthma.
Type:
Grant
Filed:
March 3, 1975
Date of Patent:
November 9, 1976
Assignee:
Warner-Lambert Company
Inventors:
Sylvester Klutchko, Max Von Strandtmann
Abstract: A prefilled syringe having a barrel to hold a liquid medium is disclosed. The rear end of the barrel is sealed by means of a rubber diaphragm whereas the front end of the syringe is sealed by a stopper and a novel needle hub assembly whereby the integrity of the liquid medium remains static until the assembly is activated and the stopper pierced.
Abstract: The present invention discloses 3-phenylhydroindoles having the formula: ##SPC1##Wherein R.sub.1 may be hydrogen, lower alkyl, phenyl or may be absent; R.sub.2 may be hydrogen, hydroxy, lower alkyl or absent; or where R.sub.1 is absent R.sub.2 may be CH.sub.3.sup.+ I.sup.- or O; and R.sub.3 and R.sub.4 may be hydrogen, hydroxy or lower alkoxy. The compounds possess anti-viral activity.
Type:
Grant
Filed:
October 21, 1974
Date of Patent:
November 2, 1976
Assignee:
Warner-Lambert Company
Inventors:
Sylvester Klutchko, Arch Christian Sonntag, John Shavel, Jr.
Abstract: Novel 2-hydroxy-phenyl-1-oxa-4-azaspiroalkane derivatives, the preparation thereof, and pharmaceutical compositions containing these 2-hydroxyphenyl-1-oxa-4-azaspiroalkane derivatives are disclosed. These derivatives possess unexpectedly valuable thereapeutic properties which make them outstandingly useful for the treatment of cardiovascular circulatory insufficiencies and hypotonic states.
Abstract: This invention relates to a process for the preparation of 1-{[5-(4-hydroxy-2H-1,2-benzothiazin-3-yl)-1,2,4-oxadiazol-3-yl]methyl}eth anone S,S-dioxide (III), a novel intermediate useful in the preparation of the known anti-inflammatory agent, 4-hydroxy-3-(5-methyl-3-isoxazolylcarbamoyl)-2-methyl-2H-1,2-benzothiazine 1,1-dioxide (IV). According to the process of this invention, the saccharin compound, 2,3-dihydro-N-(5-methyl-3-isoxazolyl)-3-oxo-1,2-benzisothiazole-2-acetamid e 1,1-dioxide (I) is reacted with an alkali metal alkoxide of a lower alcohol in an inert solvent at temperatures below 30.degree. C. to form the benzenesulfonylglycineamide, alkyl 2-{[({[(5-methyl-3-isoxazolyl)amino]carbonyl}methyl)amino]sulfonyl}benzoat e (II), which is ring closed and rearranged by reaction with an alkali metal alkoxide of a lower alcohol in an inert solvent at temperatures of from 60.degree. C. to 70.degree. C. to form the desired oxadiazole compound III.
Type:
Grant
Filed:
May 21, 1975
Date of Patent:
October 19, 1976
Assignee:
Warner-Lambert Company
Inventors:
Arthur C. Fabian, Jerome D. Genzer, Charles Francis Kasulanis, John Shavel, Jr., Harold Zinnes
Abstract: Substituted benzopyrano[3,4-c]pyridines having the following structural formula are disclosed: ##SPC1##In the above formula, R.sub.1 and R.sub.2 are hydrogen, a hydroxyl group or a lower alkoxyl group of from 1 to 6 carbon atoms; and X is an oxygen atom, a sulfur atom, a methylene group or a nitrogen atom substituted by hydrogen, a lower alkyl group of from 1 to 6 carbon atoms or a lower alkanoyl group of from 1 to 6 carbon atoms. The compounds of this invention are prepared by reacting an R.sub.1, R.sub.2 -substituted phenol with a 3-carbethoxy-4-piperidone in the presence of an acid catalyst to give an intermediate R.sub.1, R.sub.2 -substituted benzopyrano[3,4-c]pyridine. N-aminoalkylbenzopyrano[3,4-c]pyridines are obtained by treating the benzopyrano[3,4-c]pyridine with an appropriately substituted alkyl halide. The compounds of this invention are useful as bronchodilators for the treatment of bronchial asthma.
Abstract: 2-Aryl substituted isoxazolo[2,3-a]pyridinyl halides having the formula I: ##SPC1##wherein R.sub.1, R.sub.2 and R.sub.3 are each hydrogen, halogen, hydroxy, lower alkyl, lower alkoxy or lower alkanoyl; R.sub.4 is hydrogen or lower alkyl; X is a bromide, chloride or iodide salt; and processes for the preparation thereof, are described. The compounds of the invention are useful as anti-inflammatory agents and for the treatment of hyperacidity.
Type:
Grant
Filed:
September 8, 1975
Date of Patent:
September 28, 1976
Assignee:
Warner-Lambert Company
Inventors:
David T. Connor, Patricia A. Young, Maximilian VON Strandtmann
Abstract: The present invention relates to novel 1-(aryl)-2-(arylalkyl)-3-(or-4-)-[4'-(substituted alkyl-)-piperazino-1']-butanols-2, and butenes-1 showing antimicrobial action, to their pharmaceutically acceptable salts, and to the process of manufacture thereof.
Abstract: The present invention is concerned with tricyclic sulphoximides and with the preparation thereof. This family of compounds has been found to possess antihistominic, antitussive, antiinflammatory, sedative, and diuretic properties.
Abstract: A synergistic composition comprising as active ingredients a PGF.sub.2.sub..alpha. compound or its cyclodextrin clathrate thereof and a PGE.sub.2 compound or its cyclodextrin clathrate thereof, at a weight ratio of from about 1:0.33 to about 1:1.
Abstract: A novel process for preparing 4-hydroxy-3-(5-methyl-3-isoxazolylcarbamoyl)-2-methyl-2H-1,2-benzothiazine 1,1-dioxide (I), starting with 3-amino-5-methylisoxazole (II) is disclosed. Compound I exhibits anti-inflammatory properties and is useful for treating inflammation. In the process of the invention an intermediate obtained, 2,3-dihydro-N-(5-methyl-3-isoxazolyl)-3-oxo-1,2-benzisothiazole-2-acetamid e 1,1-dioxide (IV) undergoes rearrangement to provide 1-{[5-(4-hydroxy-2H-1,2-benzothiazin-3-yl)-1,2,4-oxadiazol-3-yl]methyl}eth anone S,S-dioxide (V), which is methylated, according to conventional procedures. The methylated intermediates VI, upon further treatment, undergoes a second rearrangement to obtain the desired anti-inflammatory compound I.
Type:
Grant
Filed:
December 29, 1975
Date of Patent:
August 31, 1976
Assignee:
Warner-Lambert Company
Inventors:
Arthur C. Fabian, Jerome D. Genzer, Charles Francis Kasulanis, John Shavel, Jr., Harold Zinnes
Abstract: A contact lens composition, having improved dimensional stability, suitable for use in the preparation of a corrective hydrated lens or an eye bandage, comprises polymerized random graft copolymers containing (in the dry state) from 67.2 to 79.3% HEMA; from 14.25 to 35% PVP; from 0.1 to 4.04% EDMA; from 0.1 to 2.5% MA; from 0.1 to 5.0% water; from 0 to 4 ppm HQ inhibitor; and from 50 to 250 ppm MEHQ inhibitor. The contact lens composition contains from 45 to 65% water after hydration. An improved method for shaping, polymerizing, and cutting and hydrating the contact lens composition is provided. The polymerization is conducted using only a low temperature initiator, by de-gassing prior to polymerization to remove substantially all oxygen, and by conducting the initial polymerization reaction at from 23.degree. to 30.degree.C for 16 to 30 hours, during which the heat of the reaction is continuously absorbed to control the reaction exotherm.
Type:
Grant
Filed:
November 21, 1974
Date of Patent:
August 31, 1976
Assignee:
Warner-Lambert Company
Inventors:
Albert R. Le Boeuf, William R. Grovesteen
Abstract: The present invention relates to a process for 3r-N-Monomethylamino-4 cis-phenyl-4 trans-ethoxycarbonyl-cyclohexene and its N-substitution products which are generally useful as analgesics.
Abstract: The present invention relates to a method for reducing blood pressue in a hypertensive mammal by the administration of a novel hydroxypyrimidine of the formula: ##SPC1##Wherein R.sub.1 is -CH.sub.3 or -NH.sub.2 ; and R.sub.
Type:
Grant
Filed:
August 5, 1974
Date of Patent:
August 3, 1976
Assignee:
Warner-Lambert Company
Inventors:
Glenn C. Morrison, Wiaczeslaw A. Cetenko