Abstract: 1-(Alkoxy or aroxy)carbonyloxyalkyl esters of diflunisal and related compounds are stable in aqueous medium and non-irritant to mucous membranes of mouth, throat, and stomach. Accordingly, they are useful Prodrugs of the analgesic and anti-inflammatory drug, diflunisal.
Abstract: 5-allyl-2-(3,4-dimethoxyphenyl)-3a,.alpha.-methoxy-3-methyl-2,3,3a,6-tetrah ydro-6-oxobenzofuran and analogs thereof as PAF-antagonists have been isolated from Piper futokadsura Sieb. et Zucc. and its analogs prepared. These neolignan compounds are found to have potent and specific PAF (Platelet-Activating-Factor) antagonistic activities and are thereby useful in the treatment of various diseases or disorders mediated by the PAF, for example, inflammation, cardiovascular disorder, asthma, lung edema, and adult respiratory distress syndrome.
Abstract: New fermentation products useful in the treatment of tardive dyskinesia by inhibition of choline oxidase are produced by fermentation of a nutrient medium with a microorganism, Streptomyces hygroscopicus.
Abstract: Analogs of 2,5-Diaryl tetrahydrofurans which were substituted or unsubstituted at 3,4-positions were prepared.These compounds are found to have potent and specific PAF (Platelet Activating Factor) antagonistic activities and thereby useful in the treatment of various diseases or disorders mediated by the PAF, for example, inflammation, cardiovascular disorder, asthma, lung edema, adult respiratory distress syndrome, pain, and aggregation of platelets.
Type:
Grant
Filed:
November 14, 1983
Date of Patent:
September 3, 1985
Assignee:
Merck & Co., Inc.
Inventors:
Tesfaye Biftu, San-Bao Hwang, Thomas W. Doebber, Thomas R. Beattie, Tsung-Ying Shen
Abstract: Substituted cinnamyl-2,3-dihydrobenzofurans and analogs were prepared from the nucleophilic substitution of a cinnamylhalide with a 2,3-dihydrobenzofuran anion or an analog thereof. These compounds were found to be potent topical anti-inflammatory agents.
Type:
Grant
Filed:
October 12, 1983
Date of Patent:
August 27, 1985
Assignee:
Merck & Co., Inc.
Inventors:
Michael N. Chang, Milton L. Hammond, Norman P. Jensen, John McDonald, Robert A. Zambias
Abstract: New 5-(2,3-dihydro-1H-pyrrolizin-5-oyl)-, 5-(2,3-dihydro-1H-pyrrolo[2,1-b]thiazol-5-oyl)-, 5-(2,3-dihydro-1H-pyrrolo[2,1-b]imidazol-5-oyl)-, and 5-(2,3-dihydro-1H-pyrrolo[2,1-b]oxazol-5-oyl)-derivatives of substituted 2,3-dihydro-1H-pyrrolizine-1-alkanoic or carboxylic acids have been prepared. They are found to be effective inhibitors of platelet aggregation and are analgesic/anti-inflammatory agents with low ulcerogenic side effects.
Type:
Grant
Filed:
October 8, 1982
Date of Patent:
August 20, 1985
Assignee:
Merck & Co., Inc.
Inventors:
Tesfaye Biftu, Bruce E. Witzel, Peter L. Barker
Abstract: New 5-(2,3-dihydro-1H-pyrrolizin-5-oyl)-, 5-(2,3-dihydro-1H-pyrrolo[2,1-b]thiazol-5-oyl)-, 5-(2,3-dihydro-1H-pyrrolo[2,1-b]imidazol-5-oyl)-, and 5-(2,3-dihydro-1H-pyrrolo[2,1-b]oxazol-5-oyl)-pyrrole-2-alkanoic acid derivatives have been prepared. They are found to be effective inhibitors of platelet aggregation and are analgesic and anti-inflammatory agents with low ulcerogenic side effects.
Type:
Grant
Filed:
October 8, 1982
Date of Patent:
August 6, 1985
Assignee:
Merck & Co., Inc.
Inventors:
Tesfaye Biftu, Bruce E. Witzel, Peter L. Barker
Abstract: This invention involves complexes of quinoline carboxylic acid derivatives with guanidine and guanidine carbonate. The complexes have a greater solubility and dissolution rate when compared to the parent quinoline carboxylic acid derivatives and thus are more effective anti bacterials than the parent acids.
Abstract: There are disclosed novel avermectin compounds wherein certain double bonds are oxidized to epoxides. The epoxides are prepared by oxidizing an avermectin compound with a mild oxidizing agent. The avermectin epoxide compounds have utility as anti-parasitic agents and compositions for that use are also disclosed. The compounds are also highly potent insecticides against agricultural pests.
Abstract: A forced draft crossflow evaporative heat exchange has a turbulent air-liquid interchange zone downstream from the air propulsion means and intermediate the air propulsion means and the heat exchange media. The media is inclined so the upper portion is closer to the air propulsion means than the lower portion.
Type:
Grant
Filed:
January 22, 1981
Date of Patent:
July 23, 1985
Assignee:
Baltimore Aircoil Company, Inc.
Inventors:
Robert E. Cates, Richard H. Harrison, Jr., Thomas P. Carter
Abstract: Somatostatin analogs are prepared wherein a cyclic hexapeptide contains a secondary amino acid which replaces seven of the ring amino acids of somatostatin. The cyclic hexapeptides are easier to synthesize, have a longer duration of activity, and many have a greater level of activity than somatostatin. The compounds have the properties of inhibiting the release of glucagon, growth hormone and insulin. Certain of the compounds also are capable of inhibiting the release of gastric acid secretions. The compounds are particularly useful in the treatment of acromegaly, diabetes, diabetic retinopathy and peptic ulcers. These cyclic hexapeptides are prepared by the solid phase method.
Abstract: A contact body or evaporative heat and mass exchanger packing composed of a plurality of side-by-side thin sheets interlocked with one another. The sheets are grooved with a serpentine-like, continuously-variable, cross section form to produce a plurality of liquid and gas channels between the sheets. The sheets have integrally-formed knobs and sockets specifically located to provide up-spaced alternate sheet support without utilizing adhesives of any type. The sheets are preferably composed of a thermoplastic material of any desired length, being continuously pressure-vacuum formed from long sheet rolls. The groove crests abut adjacent sheets apices at continuously-variable spacings of both greater and lesser dimension than the basic edge spacing of the serpentine grooves. The flat crests or apices of grooves are also infinitely variable in width dimension while maintaining a constant sidewall groove angle.
Type:
Grant
Filed:
January 20, 1983
Date of Patent:
May 21, 1985
Assignee:
Baltimore Aircoil Company, Inc.
Inventors:
Thomas P. Carter, Edward N. Schinner, Richard H. Harrison, Jr., Robert E. Cates
Abstract: Compounds of the efrotomycin class having a 4-hydroxy-2-pyridone terminal group are converted into 4-amino-4-dehydroxy compounds. The amino group may be substituted with various substituents. The processes for the preparation of such compounds are also disclosed. The amino derivatives have antimicrobial, and growth promotion properties and compositions for such uses are also disclosed.
Abstract: The instant invention is directed to a variable permeability liquid crystalline membrane, comprising a porous structure containing a polymeric liquid crystal which can undergo a phase change.The instant invention is also directed to a process for regulating the flow of solutes or permeants through a liquid crystalline membrane, comprising changing the phase of a polymeric liquid crystal supported by a porous structure.
Abstract: The invention relates to dipeptide compounds containing thialysine and related amino acids which are useful as converting enzyme inhibitors and as antihypertensives.
Abstract: A process for producing polypeptides is disclosed wherein potassium, rubidium, or cesium serves as the counterion for both the carbonate buffer system and the amino acid or peptide salts employed.
Abstract: A process for preparing .alpha.-alkyl amino acids by enantioretentive .alpha.-alkylation of .alpha.-amino acids is described. The products are bioactive compounds including some useful as therapeutic agents.
Type:
Grant
Filed:
June 28, 1984
Date of Patent:
April 2, 1985
Assignee:
Merck & Co., Inc.
Inventors:
Joseph S. Amato, Leonard M. Weinstock, Sandor Karady
Abstract: This invention relates to new organic compounds that are prodrugs of the antiviral agent Ara-A which is 9-(.beta.-D-arabinofuranosyl)adenine. These compounds by virtue of their high lipid solubility will penetrate the stratum cornium and on entry the enzymatic cleavage will regenerate the antiviral compound Ara-A.
Abstract: Thyrotropin Releasing Hormone (TRH) and related synthetic peptides extend the rapid growth phase of poultry thereby decreasing the time required to produce fowl of marketable size.