Patents Examined by N. Harkaway
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Patent number: 4374996Abstract: A process for preparing cimetidine by sulfur extrusion from N-cyano-N'-methyl-N"-[2-(5-methyl-4-imidazolylmethyldithio)ethyl]guanidine .Type: GrantFiled: June 3, 1981Date of Patent: February 22, 1983Assignee: SK & F Lab Co.Inventors: Clifford S. Labaw, George R. Wellman
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Patent number: 4371540Abstract: Two compounds represented by the formula ##STR1## wherein R is hydrogen or a 2-hydroxyethyl radical are reported to have minimum penetration into the brain and nerve tissues combined with maximum penetration into hypoxic tumor cells. This combination of properties makes these compounds the optimal radiosensitizers among electron-affinic 1-substituted 2-nitroinidazoles.Type: GrantFiled: August 22, 1980Date of Patent: February 1, 1983Assignee: The United States of America as represented by the Secretary of the Department of Health and Human ServicesInventors: William W. Lee, J. Martin Brown, Abelardo P. Martinez, Michael J. Cory
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Patent number: 4369183Abstract: The invention concerns novel 2-aryl-1,2-benzisothiazolinone-1,1-dioxide compounds; methods for their preparation; pharmaceutical compositions containing them as an active ingredient; and methods of selectively inhibiting proteases, especially elastase, and of treating emphysema, rheumatoid arthritis, and various inflammatory diseases, for example, bronchial inflammation.Type: GrantFiled: February 2, 1981Date of Patent: January 18, 1983Assignee: Merck & Co., Inc.Inventors: Howard Jones, Robert L. Clark, Morris Zimmerman
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Patent number: 4367235Abstract: 2-benzimidazolinone compounds of the formula ##STR1## wherein R is lower alkyl,R.sub.1 and R.sub.2, which can be the same or different, are lower straight-chained or branched alkyl and one of R.sub.1 and R.sub.2 can also be hydrogen orR.sub.1 and R.sub.2 together represent an alkylene radical and R.sub.3 is hydrogen or acyl, i.e., alkanoyl or aromatic carboxylic acid moieties;and the pharmacologically acceptable salts thereof; have marked .beta.-receptor blocking action and are outstandingly useful in the treatment or prophylaxis of cardiac and circulatory diseases.Type: GrantFiled: July 18, 1980Date of Patent: January 4, 1983Assignee: Boehringer Mannheim GmbHInventors: Carl H. Ross, Walter-Gunar Friebe, Wolfgang Kampe, Wolfgang Bartsch, Egon Roesch
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Patent number: 4360679Abstract: Novel benzofuranyl benzimidazoles of the formula ##STR1## wherein R.sub.1 represents a hydrogen atom, an alkenyloxy or cycloalkyloxy radical, an unsubstituted or substituted alkoxy, phenylalkoxy or phenoxy radical,each ofR.sub.2 and R.sub.3 independently represents a hydrogen atom, an alkyl or alkoxy radical, a halogen atom, or, if R.sub.1 represents hydrogen, together in the ortho-position to each other they represent a radical of the formula --CH.dbd.CH--CH.dbd.CH--, --O--CH.sub.2 --O-- or --O--CH.sub.2 --CH.sub.2 --O--,R.sub.4 represents a hydrogen atom, an alkyl, alkoxy or phenyl radical,R.sub.5 represents a sulpho or carboxyl group or the functional derivatives thereof including the cyano group or the trifluoromethyl group,R.sub.6 represents a hydrogen or halogen atom, an alkyl or alkoxy radical,R.sub.7 represents a cycloalkyl, alkenyl, or unsubstituted or substituted alkyl, phenyl or phenylalkyl radical, or, if n is 0, also represents a hydrogen atom,R.sub.Type: GrantFiled: September 30, 1980Date of Patent: November 23, 1982Assignee: Ciba-Geigy CorporationInventors: Hans R. Meyer, Kurt Weber
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Patent number: 4360680Abstract: A method of treating pain, meliorating inflammation in warm-blooded animals as well as a method for treating fungal and bacterial infections in such animals using certain 3-amino-1-phenyl-2-pyrazolines and 3-amino-1-substituted phenyl-2-pyrazolines and their C4 and C5 analogs, as well as compounds used in the above are disclosed.Type: GrantFiled: July 13, 1981Date of Patent: November 23, 1982Assignee: American Cyanamid CompanyInventors: John P. Dusza, Joseph P. Joseph, Seymour Bernstein
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Patent number: 4358599Abstract: 4-Nitro-1,2-hydrocarbyl pyrazolidines are prepared by a novel route from 1,2-disubstituted hydrazines and 1,3-di-(secondary amino)-2-nitropropanes and reduced to the corresponding 4-amino-1,2-hydrocarbyl pyrazolidines, which latter compounds are intermediates in the preparation of certain pharmaceutical benzamides.The novel 4-nitro-1,2-hydrocarbyl pyrazolidines have the formula: ##STR1## wherein R.sup.1 and R.sup.2 are selected from loweralkyl, lowercycloalkyl or phenyl-loweralkyl and may be the same or different.Type: GrantFiled: June 11, 1981Date of Patent: November 9, 1982Assignee: A. H. Robins Company, Inc.Inventors: Young S. Lo, Harry R. Munson, Jr.
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Patent number: 4357339Abstract: 1,5-Dimethyl-6,7-dioxabicyclo[3.2.1]-octane and 1,5-dimethyl-6,7-diazabicyclo[3.2.1]-oct-6-ene are synthesized. They are analogs of the western and southern pine beetle natural-pheromone, frontalin. They are useful for controlling the multiplication of these harmful insects and for limiting infestation of wooded areas by them.Type: GrantFiled: December 22, 1980Date of Patent: November 2, 1982Assignee: Research CorporationInventors: R. Marshall Wilson, John W. Rekers
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Patent number: 4355035Abstract: Derivatives of certain pyridyliminomethylbenzenes, useful as fungicides.Type: GrantFiled: January 26, 1981Date of Patent: October 19, 1982Assignee: Shell Oil CompanyInventors: Pieter Ten Haken, Shirley B. Webb
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Patent number: 4354031Abstract: New and valuable pyrazole derivatives having a good herbicidal action, herbicides containing these compounds as active ingredients, and processes for controlling the growth of unwanted plants with these compounds.Type: GrantFiled: August 25, 1980Date of Patent: October 12, 1982Assignee: BASF AtiengesellschaftInventors: Peter Plath, Bruno Wuerzer, Wolfgang Rohr
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Patent number: 4353921Abstract: Novel 1,2-disubstituted imidazol(in)es are described herein. The compounds are generally produced by reacting a haloacylanilide with an excess of 2-substituted-imidazol(in)e. The compounds are antiarrhythmic agents.Type: GrantFiled: June 19, 1981Date of Patent: October 12, 1982Assignee: Berlex Laboratories, Inc.Inventors: Julius Diamond, Thomas K. Morgan, Jr., Ronald A. Wohl
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Patent number: 4352813Abstract: A new salt of [(1-benzyl-1H-indazol-3-yl)oxy] acetic acid (or bendazac) with L. lysine.Following oral administrations of this compound in man, the concentrations of bendazac found in the blood are higher than those obtained after administration of bendazac as such.This discovery extends the therapeutic use of bendazac. In fact, whereas up to now bendazac could only be used topically, the L. lysine salt of bendazac makes it possible to perform therapeutic treatments with the oral route of administration as an agent with a normalizing effect on blood lipids.Type: GrantFiled: June 2, 1981Date of Patent: October 5, 1982Assignee: Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F. S.p.A.Inventors: Bruno Silvestrini, Leandro Baiocchi
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Patent number: 4350819Abstract: 1-Hydroxypyrazole and a process for its preparation by conversion of isoxazolineazoxy compounds at 140.degree.-600.degree. C.The end products obtainable by the process of the invention are valuable starting materials for the preparation of dyes, crop protection agents and drugs.Type: GrantFiled: July 17, 1981Date of Patent: September 21, 1982Assignee: BASF AktiengesellschaftInventors: Norbert Rieber, Heinrich Bohm, Rolf Platz, Werner Fuchs
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Patent number: 4349560Abstract: The invention relates to imidazolyl-indenothiophene compounds of Formula (I) and a process for their production. Also included in the invention are antimycotic compositions containing said imidazolyl-indenothiophene compounds and methods for the use of said compounds and compositions.Type: GrantFiled: April 17, 1982Date of Patent: September 14, 1982Assignee: Bayer AktiengesellschaftInventors: Horst Boshagen, Karl H. Buchel, Wilfried Draber, Ingo Haller, Manfred Plempel
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Patent number: 4348527Abstract: This disclosure describes novel 3-substituted amino-1-phenyl-2-pyrazolines and 3-substituted amino-1-mono and disubstituted phenyl-2-pyrazolines and their C.sub.4 and C.sub.5 analogs, effective as anti-inflammatory and analgesic agents, and as antibacterial agents and/or antifungal agents.Type: GrantFiled: July 13, 1981Date of Patent: September 7, 1982Assignee: American Cyanamid CompanyInventors: John P. Dusza, Joseph P. Joseph, Seymour Bernstein
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Patent number: 4348528Abstract: The invention relates to the preparation of 1-phenyl-3-carbamoyl-5-pyrazolones of the formula: ##STR1## in which the two symbols R and R' may be the same or different and each represents a hydrogen atom, an alkyl radical or a substituted alkyl radical containing 1 to 4 carbon atoms.An aqueous paste of diethyl oxalacetate phenylhydrazone is heated at a temperature not greater than 85.degree. C. until the hydrazone is completely melted, and the aqueous phase is then removed and the remaining hydrazone is treated with 2 to 12 molar equivalents of a compound of the formula HNRR' at a temperature between 20.degree. and 100.degree. C. The formation of 1-phenyl-3-carboxy-5-pyrazolone is thus avoided.Type: GrantFiled: July 13, 1981Date of Patent: September 7, 1982Assignee: P C U K Produits Chimiques Ugine KuhlmannInventors: Antoine G. L. J. Breda, Jacques G. R. Roussel
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Patent number: 4343800Abstract: Compounds of the formula ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are hydrogen or substituents of various types;R.sub.4 is hydrogen; alkyl of 1 to 5 carbon atoms; or optionally substituted aralkyl of 7 to 14 carbon atoms;R.sub.5 is heterocycle;D is alkylene of 1 to 12 carbon atoms; andA is hydrogen or acyl;and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as .alpha.- and .beta.-adrenergic receptor blocking agents and antidepressants.Type: GrantFiled: April 20, 1981Date of Patent: August 10, 1982Assignee: Boehringer Ingelheim GmbHInventors: Herbert Koppe, Anton Mentrup, Ernst-Otto Renth, Kurt Schromm, Wolfgang Hoefke, Gojko Muacevic
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Patent number: 4338330Abstract: A derivative of benzimidazole of the general formula I: ##STR1## wherein: R.sub.1 represents a linear or ramified alkyl radical C.sub.1,C.sub.2,C.sub.3,C.sub.4,C.sub.5,C.sub.6,C.sub.7,C.sub.8,C.sub.9,C. sub.10,C.sub.11,C.sub.12,C.sub.13,C.sub.14,C.sub.15, C.sub.16,C.sub.17 or C.sub.18, a cycloalkyl radical C.sub.3,C.sub.4,C.sub.5,C.sub.6,C.sub.7 or C.sub.8, a linear or ramified alkyl radical C.sub.1,C.sub.2,C.sub.3,C.sub.4 or C.sub.5 substituted by one or more radicals selected from the group comprising:phenyl, phenoxy, phenylthio, phenylsufinyl radicals;phenyl, phenoxy, phenylthio, phenylsulfinyl radicals substituted by one or more linear or ramified alkyl radicals C.sub.1,C.sub.2, C.sub.3 or C.sub.4, by one or more linear or ramified alkoxy radicals C.sub.1,C.sub.2, C.sub.3 or C.sub.4, by a methylenedioxy radical, for one or more halogen atoms, such as fluorine, chlorine or bromine;linear or ramified alkylcarboxamido groups C.sub.1,C.sub.2,C.sub.3,C.sub.4,C.sub.5 or C.sub.Type: GrantFiled: April 30, 1980Date of Patent: July 6, 1982Assignee: Continental PharmaInventors: Claude L. Gillet, Joseph L. Roba, Michel Snyers, William R. Van Dorsser, Georges E. Lambelin
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Patent number: 4337263Abstract: 1-Aryl-4-.gamma.-arylsulphonyl-3-aminopropoxy-1H-pyrazoles of the formula: ##STR1## and their acid addition salts. Application of these compounds as medicaments useful in particular as hypolipemiant or hypocholesterolemiant agents.Type: GrantFiled: June 30, 1980Date of Patent: June 29, 1982Assignee: Laboratoire Roger BellonInventors: Henri Techer, Gilles Monnier, Marcel Pesson
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Patent number: 4336385Abstract: Novel phosphate quaternary compound of the formula ##STR1## wherein R is a tertiary amine radical of from 6 to 40 carbon atoms; andX is an anion.Type: GrantFiled: April 4, 1980Date of Patent: June 22, 1982Assignee: Mona Industries, Inc.Inventors: Raymond L. Mayhew, Anthony J. O'Lenick, Jr.