Abstract: This invention relates to 4r-amino-1t-phenyl-1c-ethoxycarbonyl-cyclohexenes-(2) of formula I: ##STR1## wherein R.sub.1 and R.sub.2 are the same or different and are hydrogen or alkyl having 1 to 4 carbon atoms, or one of the two groups is allyl, phenalkyl having 7 to 9 carbon atoms or .alpha.-methyl-.beta.-hydroxyethyl; or R.sub.1 and R.sub.2 together form a morpholino group, piperazino group substituted at the 4- position by methyl, benzyl, phenyl, 3-chlorophenyl, 4-chlorophenyl, 2-phenethyl or benzoyl, or a piperidino group substituted at the 4- position by hydroxyl, phenyl, 2-methoxyphenyl, 4-methoxyphenyl, methyl or benzyl and medically acceptable addition compounds derived from inorganic and organic acids or lower alkyl halides. The compounds of the present invention are prepared by separation of 4-amino-1-phenyl-1-ethoxycarbonyl-cyclohexenes-(2), described in U.S. Pat. application Ser. No. 226,509, filed Feb. 15, 1972, now U.S. Pat. No. 3,957,851 into the two possible geometrical isomers.
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 intermediate VI, upon further treatment, undergoes a second rearrangement to obtain the desired anti-inflammatory compound I.
Type:
Grant
Filed:
June 18, 1976
Date of Patent:
April 19, 1977
Assignee:
Warner-Lambert Company
Inventors:
Arthur C. Fabian, Jerome D. Genzer, Charles Francis Kasulanis, John Shavel, Jr., Harold Zinnes
Abstract: The present invention is concerned with new pharmacologically effective 5-phenyl-thiazolidin-4-one derivatives and with the preparation thereof. These compounds are useful for treating liver dysfunctions.
Abstract: 2-Aryl substituted isoxazolo[2,3-a]pyridinyl halides having the formula I: ##STR1## 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; the pharmaceutically acceptable, acid addition salts thereof; 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:
May 27, 1976
Date of Patent:
April 19, 1977
Assignee:
Warner-Lambert Company
Inventors:
David T. Connor, Patricia A. Young, Maximilian VON Strandtmann
Abstract: A compound of the formula: ##STR1## wherein A represents a grouping of the formula: ##STR2## , R.sup.1 represents a hydrogen atom or a straight- or branched-chain alkyl group containing from 1 to 6 carbon atoms, R.sup.2 represents a hydrogen atom or a straight- or branched-chain alkyl group containing from 1 to 12 carbon atoms, X represents trans-vinylene or ethylene, and the wavy line indicates attachment of the hydroxy radical in .alpha.- or .beta.-configuration and cyclodextrin clathrates thereof and, when R.sup.2 represents a hydrogen atom, non-toxic salts thereof. These compounds exhibit characteristic prostaglandin activity.
Abstract: Compounds of the formula: ##STR1## are disclosed, wherein R.sub.1 and R.sub.2 are hydrogen; or where R.sub.1 is methyl, R.sub.2 is hydrogen, phenyl, or phenyl substituted in the para-position by hydroxy, alkoxy, chloro, phenyl or alkyl having 1-6 carbon atoms. The compounds of this invention are useful in the treatment of bronchial asthma. These compounds exhibit unique biological properties in that they provide the desired bronchial dilation effect without accompanying cardiac stimulation.
Abstract: The present invention relates to novel benzo(b)thiophene derivatives of the general formula: ##STR1## wherein Y represents a hydrogen or halogen atom; A represents a hydrogen atom or a phenyl group which may be substituted with a halogen atom or a lower alkoxy group; B represents a radical of the formula OR' or NR.sup.2 N.sup.3, wherein R' is an alkyl radical of 1 to 5 carbons which may be substituted with hydroxy, lower alkoxy, phenyl or phenoxy groups or a cycloalkyl or phenyl group which may be substituted by lower alkoxy or halogen atoms; R.sup.2 and R.sup.3, which may be identical or different, represent, if identical, hydrogen, alkyl radicals of 1 to 5 carbon atoms which may be substituted by hydroxy, lower alkoxy, phenoxy, di-lower alkylamino, or phenyl groups; or, if R.sup.2 is hydrogen, R.sup.
Type:
Grant
Filed:
May 12, 1976
Date of Patent:
April 19, 1977
Assignee:
Warner-Lambert Company
Inventors:
Peter Johannes Stoss, Manfred Franz Reinhold Herrmann, Gerhard Satzinger
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:
March 8, 1976
Date of Patent:
April 19, 1977
Assignee:
Warner-Lambert Company
Inventors:
Albert R. Le Boeuf, William R. Grovesteen
Abstract: The present invention relates to substituted [4-oxo-4H-1-benzopyran-2-yl]cyclopropane carboxylic acids and esters having the following structural formula: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are hydrogen, alkyl, lower alkoxy, phenyl or when R.sub.1 and R.sub.2 are hydrogen, R.sub.3 and R.sub.4 taken together form an additional aromatic ring and A is hydrogen or ethyl. The compounds of this invention exhibit anti-allergy properties and are indicated in the management of allergic manifestations such as bronchial asthma.
Type:
Grant
Filed:
November 20, 1975
Date of Patent:
April 19, 1977
Assignee:
Warner-Lambert Company
Inventors:
Marvin P. Cohen, John Shavel, Jr., Max Von Strandtmann
Abstract: The present invention relates to cyclic and acyclic amide derivatives of the antibiotic substance, designated acid S, produced by Polyangium cellulosum var. fulvum (ATTC No. 25532), to the acetates thereof and to processes for the production of the amides and their corresponding diacetates. The amide derivatives of acid S of this invention are useful as antifungal and antibacterial agents.
Type:
Grant
Filed:
August 7, 1975
Date of Patent:
April 5, 1977
Assignee:
Warner-Lambert Company
Inventors:
David T. Connor, Samuel M. Ringel, Maximilian VON Strandtmann
Abstract: Processes for the production of the compounds of the formula: ##STR1## are disclosed. In the above formula, R.sub.1 is aryl which may be substituted or unsubstituted; R.sub.2 is hydrogen, alkyl, aryl, aralkyl, alkoxy, halogen, cyano, nitro, trifluoromethyl and the like.These compounds are prepared by the following reaction schemes: ##STR2## These compounds are useful as anti-inflammatory agents.
Abstract: A clear gel composition containing a topically active anti-inflammatory steroid and a neomycin salt is disclosed. The clear gel composition is prepared by dissolving the steroid in a polyhydroxy alcohol/lower alcohol solvent, a major proportion of the polyhydroxy alcohol solvent being propylene glycol, and adding a hydroxycellulose ingredient; an aqueous solution of the neomycin salt is then added to the steroid formulation and, upon the addition of an alkali metal chloride salt, such as sodium chloride, a clear gel is obtained. The pH may be adjusted to 4-5. The resulting composition is indicated for the relief of corticosteroid-responsive dermatoses.
Abstract: The present invention relates to a method for reducing blood pressure in a hypertensive mammal by the administration of a novel hydroxypyrimidine of the formula: ##STR1##
Type:
Grant
Filed:
September 29, 1975
Date of Patent:
March 22, 1977
Assignee:
Warner-Lambert Company
Inventors:
Glenn C. Morrison, Wiaczeslaw A. Cetenko
Abstract: There is disclosed 2,3-dihydro-3-(2-pyridinyl)-4H-1-benzopyran-4-one N-oxides of the formula: ##STR1## in which R.sub.1 is hydrogen, halogen, lower alkyl, hydroxy, lower alkoxy or amino; R.sub.2 is hydrogen or --CH.sub.2 OH. These compounds are indicated in the treatment of gastric ulcers.
Type:
Grant
Filed:
April 13, 1976
Date of Patent:
March 22, 1977
Assignee:
Warner-Lambert Company
Inventors:
David T. Connor, Patricia Young, Max Von Strandtmann
Abstract: Substituted benzopyrano[3,4-c]pyridines having the following structural formula are disclosed: ##STR1## In the above formula, R.sub.1 R.sub.2 are hydrogen, a hydroxyl group or a lower alkoxyl group of from 1 to 6 carbon atoms; R.sub.3 is hydrogen or a lower alkyl 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: This invention relates to substituted 2-aminothiochromones of the general structure I: ##STR1## wherein R.sub.1 and R.sub.2 may be hydrogen; lower alkyl or lower alkoxy of 1 to 6 carbon atoms; or halogen such as chloro or bromo; and X may be cyano or carboxamido. The compounds are prepared using a thiosalicylic acid or a substituted thiosalicylic acid as starting material.The compounds of this invention are active in the prevention of allergic and asthmatic reactions in mammals.
Abstract: Compounds of the formula: ##STR1## are disclosed wherein X is NH, O or S and the tautomers thereof when X is nitrogen, and Y is hydrogen, lower alkyl, hydroxy, lower alkoxy, chloro, bromo or aryl. These compounds are useful in the management of allergic manifestations such as bronchial asthma.
Type:
Grant
Filed:
March 3, 1975
Date of Patent:
March 15, 1977
Assignee:
Warner-Lambert Company
Inventors:
Sylvester Klutchko, John Shavel, Jr., Max Von Strandtmann
Abstract: An apparatus comprising a sterilizing capsule for the sterilizing of soft contact lenses in an aqueous hydrogen peroxide solution is disclosed.