Abstract: Although dibasic carbonic anhydrase inhibitors (C.A.I.) can be administered systemically by oral or intravenous routes, attempts to administer them topically were inadvisable because of their elevated pH. The mono-alkali metal salts in the treatment of intraocular hypertension especially the sodium and potassium salts, of dibasic salt-forming C.A.I. are as effective in lowering intraocular pressure as dialkali metal salts of dibasic C.A.I. while having a pH more in harmony with ocular pH. They are found particularly useful when administered in conjunction with an ophthalmologically acceptable water-soluble polymer such as hydroxypropylcellulose in an aqueous carrier.
Abstract: Novel carboxylic acid esters of 5-hydroxy-2-benzothiazolesulfonamide are shown to be useful for the topical treatment of elevated intraocular pressure. Ophthalmic compositions including drops and inserts are also disclosed, as well as methods for preparing the novel compounds.
Abstract: A process for the whole broth extraction of avermectins wherein the pH of the whole broth is adjusted with mineral acid and then contacted with a solvent extractant so that the avermectic active component is taken up by the solvent. The now avermectin rich extractant is then processed through a solvent concentration step and the avermectin isolated by conventional crystallization. The extractant is then recycled with appropriate make-up to extract a subsequent batch of whole broth.
Abstract: Novel carboxylic acid esters of 6-hydroxy-2-benzothiazolesulfonamide are shown to be useful for the topical treatment of elevated intraocular pressure. Ophthalmic compositions including drops and inserts are also disclosed, as well as methods for preparing the novel compounds.
Abstract: This invention relates to ophthalmic preparations which include 5-fluoro-2-methyl-1-(p-methylthiobenzylidene)-3-indenylacetic acid or ophthalmologically acceptable salts thereof as the active entity for reducing or controlling inflammation of the eye.
Abstract: A unit dose applicator for liquid ophthalmic medicaments in solution or suspension has an elongated housing for the medicament; at one end of the housing there is an opening for at least partially emptying the contents of the housing; at the other end of the housing is a second opening; and the second opening is capped by a diaphragm-like seal having a sufficient displacement potential to exude only 1 to 4 drops of the medicament.
Abstract: The invention relates to the treatment of gray matter edema in the brain or spinal chord by the administration of benzofuranyloxyacetic acids, indeno[5,4-b]furancarboxylic acids, their analogs and salts thereof.
Abstract: Antimicrobial agents suitable for use in aqueous systems for their preservation against biodeterioration include substitutedpiperidinomethylpropenenitriles and propanenitriles. The unsaturated compounds are prepared by reaction of a suitable piperidine with cyano acetic acid and formaldehyde: the propane derivatives therefrom by nucleophilic addition.
Type:
Grant
Filed:
March 24, 1982
Date of Patent:
July 5, 1983
Assignee:
Merck & Co., Inc.
Inventors:
Richard A. Dybas, Nathaniel Grier, Bruce E. Witzel
Abstract: The invention relates to the treatment of gray matter edema in the brain or spinal chord by the administration of (indanyloxy)acetic acids, and analogs and salts thereof.
Type:
Grant
Filed:
December 30, 1981
Date of Patent:
June 21, 1983
Assignee:
Merck & Co., Inc.
Inventors:
Robert S. Bourke, Edward J. Cragoe, Jr.
Abstract: Novel pharmaceutically useful derivatives of selected known bio-affecting carboxylic acids are disclosed, said derivatives having the structural formula ##STR1## wherein R.sub.1 and R.sub.2, which can be the same or different, are each hydrogen, C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.5 alkoxy, C.sub.1 -C.sub.5 alkylthio, phenyl, or substituted phenyl having one or more substituents each of which is selected from the group consisting of C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.5 alkoxy, chloro and dialkylamino wherein the alkyl portions, which can be the same or different, each have 1 to 5 carbon atoms, with the proviso that when R.sub.1 is alkoxy or alkylthio, then R.sub.2 cannot be alkoxy or alkylthio; X and X', which can be the same or different, are each hydrogen, C.sub.1 -C.sub.5 alkyl, carboxy, C.sub.2 -C.sub.6 alkoxycarbonyl, halo, C.sub.1 -C.sub.
Abstract: In a process for regenerating the activated carbon and in the purification of brown phosphoric acid or alkali phosphates obtained via the so-called wet process employing mineral acid digestion of crushed phosphate rock, the activated carbon used to filter brown H.sub.3 PO.sub.4 is removed from service, washed with water, the initial washings being recovered to reclaim phosphoric acid, and then steeped in a basic aqueous solution, e.g., aqueous alkali hydroxide, alkali carbonate, ammonium hydroxide, loweralkyl amines or loweralkanol amines. After again water washing the activated carbon, to remove residual base, the activated carbon is either returned to service or steeped in an aqueous solution of mineral acid, e.g., sulfuric, hydrochloric, or nitric acid, again washed with water to remove residual acid and returned to service. Usually, the acid steep need not be employed with every base cycle to maintain good decolorization, although if desired the acid steep can be used with each caustic cycle.
Abstract: 2,4-Disubstituted-1,2,5-thiadiazol-3(2H)-one antimicrobials have broad spectrum antibacterial and antifungal activity. They are found to be especially useful in agriculture to protect plants against diseases such as leaf, stem, and fruit spotting, internal discoloration and decay of fruits and vegetables. These compounds are particularly active against diseases caused by the genera Pseudomonas, Xanthomonas, Erwinia, and Corynebacterium.
Type:
Grant
Filed:
April 21, 1980
Date of Patent:
December 7, 1982
Assignee:
Merck & Co., Inc.
Inventors:
Richard A. Dybas, Bruce E. Witzel, Nathaniel Grier
Abstract: The invention relates to novel [(5,6,9a-substituted-3-oxo-1,2,9,9a-tetrahydro-3H-fluoren-7-yl)oxy]alkanoi c and cycloalkanoic acids, and their analogs, esters, salts and derivatives. These compounds are synthesized by methods selected from a number of synthetic routes depending on the particular structure, choice of intermediate or preferred reaction sequence. The compounds are useful in the treatment and prevention of injury to the brain and spinal chord due to accidents, ischemic stroke and hydrocephalus; compositions for such uses are also disclosed.
Type:
Grant
Filed:
February 19, 1981
Date of Patent:
October 26, 1982
Assignee:
Merck & Co., Inc.
Inventors:
Edward J. Cragoe, Jr., Gerald E. Stokker, Norman P. Gould
Abstract: The invention relates to novel [(5,6,9a-substituted-3-oxo-1,2,9,9a-tetrahydro-3H-fluoren-7-yl)oxy]alkanoi c and cycloalkanoic acids and their analogs, esters, salts and derivatives. These compounds are synthesized by methods selected from a number of synthetic routes depending on the particular structure, choice of intermediate or preferred reaction sequence. The compounds are useful in the treatment and prevention of injury to the brain and spinal chord due to accidents, ischemic stroke and hydrocephalus; compositions for such uses are also disclosed.
Type:
Grant
Filed:
February 19, 1981
Date of Patent:
October 26, 1982
Assignee:
Merck & Co., Inc.
Inventors:
Edward J. Cragoe, Jr., Gerald E. Stokker, Norman P. Gould
Abstract: Water soluble solid ophthalmic inserts for the treatment of dry eye in patients (human and animal), comprising a water soluble solid polymer of appropriate size.
Abstract: Novel halophenyl and loweralkyl substituted halophenyl polyamines are useful antimicrobial agents, as well as algae inhibitors. They are especially useful because of their low toxicity, and as such are advantageously included as the active agent in surgical scrubs, antibacterial soaps, as preservatives in cosmetic preparations, and the like.
Type:
Grant
Filed:
February 4, 1981
Date of Patent:
July 20, 1982
Assignee:
Merck & Co., Inc.
Inventors:
Richard A. Dybas, Nathaniel Grier, Bruce E. Witzel
Abstract: 4-Amino- and 2,4-diaminopyrimidines with a quaternized ring nitrogen and an oxygen bearing substituent such as hydroxyalkyl, alkoxyalkyl, or alkanoyl on one of the exo- or endocyclic nitrogens and a C.sub.6-18 alkyl on another, are highly active antimicrobial agents with a relatively low acute mammalian toxicity.
Type:
Grant
Filed:
July 23, 1979
Date of Patent:
July 13, 1982
Assignee:
Merck & Co., Inc.
Inventors:
Nathaniel Grier, Elbert E. Harris, Henry Joshua, Arthur A. Patchett, Bruce E. Witzel, Richard A. Dybas
Abstract: The invention relates to novel [(5,6,9a-substituted-3-oxo-1,2,9,9a-tetrahydro-3H-fluoren-7-yl)oxy]alkanoi c and cycloalkanoic acid and their analogs, esters, salts and derivatives. These compounds are synthesized by methods selected from a number of synthetic routes depending on the particular structure, choice of intermediate or preferred reaction sequence. The compounds are useful in the treatment and prevention of injury to the brain and spinal chord due to accidents, ischemic stroke and hydrocephalus; compositions for such uses are also disclosed.
Type:
Grant
Filed:
February 19, 1981
Date of Patent:
June 29, 1982
Assignee:
Merck & Co., Inc.
Inventors:
Edward J. Cragoe, Jr., Gerald E. Stokker, Norman P. Gould
Abstract: The invention relates to novel [(5,6,9a-substituted-3-oxo-1,2,9,9a-tetrahydro-3H-fluoren-7-yl)-oxy]alkano ic and cycloalkanoic acids and their analogs, esters, salts and derivatives. These compounds are synthesized by methods selected from a number of synthetic routes depending on the particular structure, choice of intermediate or preferred reaction sequence. The compounds are useful in the treatment and prevention of injury to the brain and spinal chord due to accidents, ischemic stroke and hydrocephalus; compositions for such uses are also disclosed.
Type:
Grant
Filed:
February 19, 1981
Date of Patent:
March 2, 1982
Assignee:
Merck & Co., Inc.
Inventors:
Edward J. Cragoe, Jr., Gerald E. Stokker, Norman P. Gould
Abstract: Compounds of the structure: ##STR1## where A is either ##STR2## where R.sub.1 to R.sub.4 are various substituents are active as antibacterials and antifungals.
Type:
Grant
Filed:
May 5, 1978
Date of Patent:
February 23, 1982
Assignee:
Merck & Co., Inc.
Inventors:
Nathaniel Grier, Richard A. Dybas, Bruce E. Witzel