Patents Represented by Attorney Harry E. Westlake
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Patent number: 4429042Abstract: Novel compounds are produced by the fermentation of a nutrient medium with the previously undescribed microorganism Streptomyces avermitilis. They may be isolated by solvent extraction and chromatographic fractionation techniques. The compounds, which are described generically as C-076 have significant parasiticidal activity. The compounds may be included in compositions for the oral or parenteral administration to animals for the prevention and cure of parasitic infections.Type: GrantFiled: December 30, 1981Date of Patent: January 31, 1984Assignee: Merck & Co., Inc.Inventors: George Albers-Schonberg, Hyman Wallick, Robert E. Ormond, Thomas W. Miller, Richard W. Burg
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Patent number: 4328335Abstract: The C-076 compounds are a series of four pairs of macrolides in which the members of each pair are homologous. The instant processes convert the C-076 A2 and B2 compounds isolated from a fermentation broth into the biologically preferred B1 and A1 compounds or into the dihydro derivatives thereof.Type: GrantFiled: December 15, 1980Date of Patent: May 4, 1982Assignee: Merck & Co., Inc.Inventor: Helmut H. Mrozik
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Patent number: 4321274Abstract: Substituted-1-(cinnamylideneamino)-3-benzylideneaminoguanidines, known as effective anti-coccidial agents, are useful as potent anti-giardiasis and anti-trichomoniasis agents.Type: GrantFiled: October 6, 1980Date of Patent: March 23, 1982Assignee: Merck & Co., Inc.Inventors: Ching C. Wang, Michael H. Fisher
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Patent number: 4321267Abstract: 1-Substituted-4(1H)-pyridinone hydrazones, known as effective anti-coccidial agents, are useful as potent anti-giardiasis and anti-trichomoniasis agents.Type: GrantFiled: October 6, 1980Date of Patent: March 23, 1982Assignee: Merck & Co., Inc.Inventors: Ching C. Wang, Michael H. Fisher
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Patent number: 4320129Abstract: Complexes of pyromellitic diimide compounds which are ruminant feed additives and which improve feed efficiency are disclosed. The pyromellitic diimide compounds may be unsubstituted pyromellitic diimide itself, or one of the nitrogen atoms may be substituted with an alkyl or substituted alkyl group. The pyromellitic diimide nucleus may also be substituted. The pyromellitic diimide compound is complexed with a compound containing an amide, amidine or thioamide linkage. The complexing agent may be either cyclic or open chain. Compositions using the complexes as ruminant feed additives are also disclosed.Type: GrantFiled: February 5, 1979Date of Patent: March 16, 1982Assignee: Merck & Co., Inc.Inventors: Michael H. Fisher, Bruce O. Linn
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Patent number: 4317530Abstract: Disclosed is an improved piston operated pump for viscous materials wherein the entrapment of air bubbles in the viscous material is reduced by placing a spring in the pump cylinder. The spring is the same diameter as the pump cylinder and is about as long as the length of travel of the piston. The spring is conical in shape so that it may be fully compressed without substantially affecting the capacity of the pump cylinder or the length of the piston stroke.Type: GrantFiled: December 31, 1979Date of Patent: March 2, 1982Assignee: Merck & Co., Inc.Inventor: Joseph M. Magrath
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Patent number: 4311709Abstract: Loweralkyl substituted diphenyl polyamines are useful antimicrobial agents, as well as algae inhibitors. They are especially useful because of their low toxicity. One particular compound, 1-amino-3-{{3-[4-(1-methylethyl)-phenyl]-1-{2-[4-(methylethyl)-phenyl]ethy l}propyl}amino}-2-propanol, and salts thereof is particularly useful as an udder wash and teat dip for mastitis prevention in lactating cows. Compositions for such use are disclosed.Type: GrantFiled: December 26, 1979Date of Patent: January 19, 1982Assignee: Merck & Co., Inc.Inventors: Richard A. Dybas, Nathaniel Grier, Bruce E. Witzel
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Patent number: 4310519Abstract: Novel compounds are produced by the fermentation of a nutrient medium with the previously undescribed microorganism Streptomyces avermitilis. They may be isolated by solvent extraction and chromatographic fractionation techniques. The compounds, which are described generically as C-076 have significant parasiticidal activity. The compounds may be included in compositions for the oral or parenteral administration to animals for the treatment of parasitic infections.Type: GrantFiled: September 8, 1978Date of Patent: January 12, 1982Assignee: Merck & Co., Inc.Inventors: George Albers-Schonberg, Hyman Wallick, Robert E. Ormond, Thomas W. Miller, Richard W. Burg
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Patent number: 4310518Abstract: 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.Type: GrantFiled: October 1, 1980Date of Patent: January 12, 1982Assignee: Merck & Co., Inc.Inventors: Roger M. Freidinger, Daniel F. Veber
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Patent number: 4310541Abstract: Benzylidene aminoguanidene derivatives, known as effective anti-coccidial agents, are useful as potent anti-giardiasis and anti-trichomoniasis agents.Type: GrantFiled: September 22, 1980Date of Patent: January 12, 1982Assignee: Merck & Co., Inc.Inventors: Ching C. Wang, Nancy J. Dick
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Patent number: 4304720Abstract: Fluorescein esters and ethers including the dioleyl derivative of fluorescein are disclosed. These compounds have the useful property of being fluorescent under the influence of the proper frequency of electromagnetic irradiation. Further, dioleyl fluorescein is readily incorporated into low-density lipoproteins which can then become part of the cell matter; the compounds retain their fluorescent properties during this procedure. The fluorescence allows cells to be identified and separated. The fluorescein esters and ethers are prepared from fluorescein and the novel reagent O-alkenyl-N,N'-dialkylisourea.Type: GrantFiled: April 30, 1980Date of Patent: December 8, 1981Assignee: Merck & Co., Inc.Inventors: Richard T. Dean, Conrad P. Dorn, Jr., Tsung-Ying Shen
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Patent number: 4289760Abstract: Derivatives of C-076 compounds are described in which the C-076 molecule, a series of macrolides, has the 23-hydroxy group thereof oxidized to the 23-keto group. The 23-keto compounds are prepared by selectively oxidizing the suitably protected 23-hydroxy compound using such oxidizing agents as pyridinium dichromate, chromic acid-dimethyl pyrazole, chromic acid, chromic acid-acetic acid, and the like. Alternatively, selective oxidation of the unprotected 23-hydroxy compound may be accomplished by placing the compound in soil. Further reaction of the oxidized C-076 compounds is also possible. The compounds thus produced have profound anthelmintic, insecticidal, ectoparasiticidal, and acaricidal activity. Compositions containing the described C-076 derivatives as the active ingredient thereof are also disclosed.Type: GrantFiled: May 2, 1980Date of Patent: September 15, 1981Assignee: Merck & Co., Inc.Inventors: Helmut H. Mrozik, John G. MacConnell, August J. Kempf
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Patent number: 4289784Abstract: Novel substituted pyromellitic diimides are disclosed wherein the compounds are assymetrically substituted with a variety of substituent groups. Processes for the preparation of such compounds are also disclosed. The novel assymetrically substituted pyromellitic diimides are useful for administration to ruminant animals to increase feed efficiency, shift volatile fatty acid production in the ruminants from acetate with an increase in the more energetically efficient propionate and butyrate and to suppress methane formation in the rumen. Composition and methods of treatment utilizing said compounds as the active ingredient thereof are also disclosed.Type: GrantFiled: April 22, 1980Date of Patent: September 15, 1981Assignee: Merck & Co., Inc.Inventors: Richard J. Bochis, Michael H. Fisher, Bruce O. Linn
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Patent number: 4285963Abstract: There are disclosed certain new derivatives of C-076 compounds which have been isolated from the fermentation broth that produced the original C-076 compounds. The compounds retain the C-076 16-membered cyclic backbone, however, the groups attached thereto are considerably modified from the original C-076 compounds. The new compounds have been found to retain the biological activity of the parent C-076 compounds. The compounds are thus potent antiparasitic agents and compositions and methods for such uses are also disclosed.Type: GrantFiled: August 7, 1980Date of Patent: August 25, 1981Assignee: Merck & Co., Inc.Inventors: Byron H. Arison, Robert T. Goegelman, Vincent P. Gullo
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Patent number: 4283612Abstract: An apparatus for eliminating accidents on power machines such as brake presses which comprises in combination a safety pedal, proximity switch and metal plate.Type: GrantFiled: May 5, 1980Date of Patent: August 11, 1981Assignee: Baltimore Aircoil Co., Inc.Inventor: Edward G. Richards
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Patent number: 4282364Abstract: An improved process for the preparation of thiazoles is disclosed. The process utilizes a substituted imine and sulfur dioxide heated in the presence of a catalyst. The thiazoles are known important chemical intermediates.Type: GrantFiled: May 22, 1980Date of Patent: August 4, 1981Assignee: Merck & Co., Inc.Inventors: Joseph S. Amato, Sandor Karady, Leonard M. Weinstock
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Patent number: 4277603Abstract: This invention relates generally to a novel process for preparing 5-deazariboflavins by the cyclization of the corresponding 6-(N-substituted arylamino)uracils with trialkylorthoformate in the presence of a strong acid catalyst. An improved process for preparing the uracil intermediate is also disclosed. More particularly, it is concerned with the process for preparing 5-deazariboflavin by cyclizing 6-[3,4-dimethyl-N-(D-ribityl)anilino[uracil with trialkylorthoformate in the presence of a strong acid catalyst and hydrolyzing the resulting alkoxymethylene derivative. The corresponding uracil intermediate is prepared by reacting 6-chlorouracil with N-D-ribityl-3,4-xylidine.5-Deazariboflavins having the general Formula (I) herein below: ##STR1## wherein R.sub.7 is hydrogen or methyl, R.sub.8 is methyl, hydroxy or acyloxy and R.sub.Type: GrantFiled: March 12, 1979Date of Patent: July 7, 1981Assignee: Merck & Co., Inc.Inventors: Richard L. Tolman, Wallace T. Ashton, Ronald D. Brown
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Patent number: 4269830Abstract: Compositions comprising substituted 5-nitroimidazoles and diminazene aceturate (Berenil) useful in the treatment of chronic trypanosomiasis infections in humans and animals. The substituted 2- or 5-nitroimidazoles having a 1-alkyl substituent and a 2-substituent, the latter being a .DELTA..sup.2 -4',5'-disubstituted isoxazoline. The 4',5'-substitution on the isoxazoline moiety is a saturated alkyl ring. Method of treatment of chronic trypanosomiasis infections in humans and animals by administering said compositions.Type: GrantFiled: May 17, 1979Date of Patent: May 26, 1981Assignee: Merck & Co., Inc.Inventor: Francis W. Jennings
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Patent number: 4265645Abstract: An injector type cooling apparatus is disclosed wherein multiple flat liquid sprays are directed into a conduit of uniform cross-section to draw cooling air into and through the conduit for mixture with and heat transfer from the liquid. The discharge end of the conduit is fitted with mist eliminators, in addition, holes or slots fitted with mist eliminators are provided in the conduit roof or sides downstream of the liquid sprays. These holes or slots cause increased air flow which results in improved cooling apparatus performance.Type: GrantFiled: January 21, 1980Date of Patent: May 5, 1981Assignee: Baltimore Aircoil Co., Inc.Inventor: Richard P. Merrill
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Patent number: RE31429Abstract: 9-(Dihalobenzyl)adenines are prepared uncontaminated with other positional isomers in a series of mild transformations starting from 4,5,6-triaminopyrimidine and proceeding via 7-(N-formyl-N-dihalobenzyl)amino[1,2,5]-thiadiazolo[3,4-d]pyrimidine. The resulting compounds have anticoccidial activity and are useful in controlling cecal and/or intestinal coccidiosis when administered in minor quantities to animals, in particular to poultry usually in admixture with animal sustenance.Type: GrantFiled: October 23, 1979Date of Patent: October 25, 1983Assignee: Merck & Co., Inc.Inventors: Robert Tull, deceased, George D. Hartman, Leonard M. Weinstock