Patents Represented by Attorney Julian S. Levitt

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  • Broad spectrum antimicrobial compositions containing tris-(hydroxymethyl)aminomethane and polyamines
    Patent number: 4058625
    Abstract: A composition comprising tris-(hydroxymethyl)aminomethane and dibicyclo [3.1.1] and [2.2.1] heptyl and dibicyclo [3.1.1] and [2.2.1] heptenyl polyamines, their acid addition salts, and mixtures thereof are useful as antimicrobial agents. The composition is particularly useful because of the synergistic improvement obtained against strains of the genus Pseudomonas, as well as other genera.
    Type: Grant
    Filed: May 14, 1976
    Date of Patent: November 15, 1977
    Assignee: Merck & Co., Inc.
    Inventors: David P. Jacobus, Eugene L. Dulaney, Nathaniel Grier
  • Broad spectrum antibacterial compositions containing tris (hydroxymethyl)-aminomethane and diphenyl and loweralkyl substituted diphenyl polyamines
    Patent number: 4058624
    Abstract: A composition comprising tris-(hydroxymethyl)aminomethane and diphenyl and loweralkyl substituted diphenyl polyamines, their acid addition salts, and mixtures thereof are useful as antibacterial agents. The composition is particularly useful because of the synergistic improvement obtained against strains of the genus Pseudomonas, as well as other genera.
    Type: Grant
    Filed: May 14, 1976
    Date of Patent: November 15, 1977
    Assignee: Merck & Co., Inc.
    Inventors: David P. Jacobus, Eugene L. Dulaney, Nathaniel Grier
  • Process for the preparation of cephalosporin antibiotics
    Patent number: 4053286
    Abstract: An improved process for preparing the compound 7.beta.-(2-thienylacetamido)-7-methoxy-3-carbamoyloxymethyl-3-cephem-4-car boxylic acid or its esters, from the compound 7.beta.-(D-5-amino-5-carboxyvaleramido)-3-carbamoyloxymethyl-7-methoxy-3-c ephem-4-carboxylic acid, by conducting the transacylation of the latter compound in the presence of commercially available alumino-silicate zeolites, also known as "molecular sieves." The process can be employed to prepare a cephalosporin with a desired 7-acylamido group from cephalosporins having a broad range of different 7-acylamido groups without having to isolate and purify a 7-amino intermediate. The final products have utility as broad spectrum antibiotics.
    Type: Grant
    Filed: May 24, 1976
    Date of Patent: October 11, 1977
    Assignee: Merck & Co., Inc.
    Inventor: Leonard M. Weinstock
  • Process for epimerizing beta-lactam antibiotic compounds by means of an acid quench
    Patent number: 4051132
    Abstract: Total synthesis methods employ 7-amino (6-amino in the case of a penicillin derivative) group in the alpha configuration. The instant invention provides a general route for preparing the 7.beta.-amino (or 6.beta.-amino) compound, through the formation of an imino-containing intermediate, followed by hydrolysis to the desired epimer. Novel intermediate products are provided. The compounds having the desired beta epimer can be converted to acylamino-antibiotics.
    Type: Grant
    Filed: December 24, 1975
    Date of Patent: September 27, 1977
    Assignee: Merck & Co., Inc.
    Inventor: Raymond A. Firestone
  • Fluorodesulfurization of alkyl mercaptans or alkyl dithianes
    Patent number: 4049708
    Abstract: Organic compounds containing a mercapto group or a dithiane moiety can be transformed into the analogous fluoro or difluoro compounds by reacting them with a halogenating reagent in liquid hydrogen fluoride, optionally containing boron trifluoride or antimony pentafluoride solution, at temperatures from about -80.degree. and 15.degree. C. The method may be descriptively termed "fluorodesulfurization".
    Type: Grant
    Filed: March 4, 1976
    Date of Patent: September 20, 1977
    Assignee: Merck & Co., Inc.
    Inventors: Janos Kollonitsch, Stephen Marburg
  • Alicyclic alkylene polyamine microorganism and algae growth inhibitors
    Patent number: 4049417
    Abstract: Novel dicyclohexyl, dicyclohexenyl and cyclohexylcyclohexenylalkyl polyamines are useful antimicrobial agents, as well as algae inhibitors. They are 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: March 8, 1976
    Date of Patent: September 20, 1977
    Assignee: Merck & Co., Inc.
    Inventors: Bruce E. Witzel, Nathaniel Grier, Richard A. Dybas, Robert A. Strelitz
  • Composition for secondary and tertiary oil recovery
    Patent number: 4049559
    Abstract: An antimicrobial composition for secondary and tertiary oil recovery comprising a flooding composition consisting of displacement and driving fluids having incorporated therein an antimicrobially effective amount of a di-bicyclo[3.1.1] or [2.2.1] heptyl or di-bicyclo[3.1.1] and [2.2.1] heptenyl polyamines or salts thereof.
    Type: Grant
    Filed: May 18, 1976
    Date of Patent: September 20, 1977
    Assignee: Merck & Co., Inc.
    Inventors: Nathaniel Grier, Richard A. Dybas, Robert A. Strelitz
  • Process for resolving alanine, 3-fluoro and 2-deutero-3-fluoro-DL-alanine
    Patent number: 4048224
    Abstract: DL-Alanine, 3-fluoro-DL-alanine and 2-deutero-3-fluoro-DL-alanine, are resolved by reaction with a resolving base and a .beta.-dicarbonyl compound. The resulting azomethine diastereomeric salts which are easily separated, the masking group is readily removed under mildly acidic conditions.
    Type: Grant
    Filed: March 5, 1976
    Date of Patent: September 13, 1977
    Assignee: Merck & Co., Inc.
    Inventors: John M. Chemerda, George Gal
  • Acylimine cephalosporins
    Patent number: 4041029
    Abstract: A process is provided which yields derivatives of cephalosporins and penicillins. The process starts with 7-acylaminocephalosporin, or 6-acylaminopenicillin, then the latter compounds are treated with an organolithium compound, followed with t-butyl-hypochlorite. Finally, a defined reagent is added yielding a side chain on the carbon adjacent to the amino-nitrogen. Novel intermediate compounds are also described. The end compounds prepared are active against both gram-positive and gram-negative bacteria.
    Type: Grant
    Filed: September 23, 1975
    Date of Patent: August 9, 1977
    Assignee: Merck & Co., Inc.
    Inventors: Raymond A. Firestone, Lovji D. Cama, Burton G. Christensen
  • Preparation of antibiotics by fermentation
    Patent number: 4036696
    Abstract: A fermentation process for preparing 7-methoxy substituted cephalosporins. The products are useful as antibiotics and exhibit activity against gram-negative and gram-positive bacteria.
    Type: Grant
    Filed: June 14, 1976
    Date of Patent: July 19, 1977
    Assignee: Merck & Co., Inc.
    Inventors: Edward O. Stapley, Justo M. Mata
  • Novel dibicyclo [3.1.1] and [2.2.1] heptyl and dibicyclo [3.1.1] and [2.2.1] heptenyl polyamines and methods for their preparation
    Patent number: 4035174
    Abstract: Novel dibicyclo [3.1.1] and [2.2.1] heptyl and dibicyclo [3.1.1] and [2.2.1] heptenyl polyamines having a cyclohexylene group in the polyamine moiety are useful antimicrobial agents, as well as algae inhibitors. They are especially useful as hard surface disinfectants and as additives to oil well drilling muds, injection brines and industrial waters where microbial control is desired.
    Type: Grant
    Filed: March 26, 1976
    Date of Patent: July 12, 1977
    Assignee: Merck & Co., Inc.
    Inventors: Nathaniel Grier, Richard A. Dybas, Robert A. Strelitz
  • Dibicyclo[3.1.1] and [2.2.1] heptyl and dibicyclo [3.1.1] and [2.2.1] heptenyl polyamines having a piperidine moiety
    Patent number: 4033748
    Abstract: Novel dibicyclo [3.1.1] and [2.2.1] heptyl and dibicyclo [3.1.1] and [2.2.1] heptenylalkyl polyamines are useful antimicrobial agents, as well as algae inhibitors. They are especially useful as hard surface disinfectants and as additives to oil well drilling muds, injection brines and industrial water where bacterial control is desired.
    Type: Grant
    Filed: July 2, 1976
    Date of Patent: July 5, 1977
    Assignee: Merck & Co., Inc.
    Inventors: Nathaniel Grier, Richard A. Dybas, Robert A. Strelitz
  • Cephalosporin phosphonic acid, sulfonic acid and sulfonamide compounds
    Patent number: 4032521
    Abstract: Novel antibiotics of the formula: ##STR1## and its salts, esters and amides wherein R is acyl; B is H, OCH.sub.3, CH.sub.3 or SR" wherein R" is lower alkyl; A is hydrogen, hydroxy, or an organic group; and, Y is a radical of the formula PO(OH).sub.2 ; PO(OH) (OR") wherein R" is loweralkyl; SO.sub.2 (OH); or SO.sub.2 NH.sub.2.The products are prepared by a multi-step process starting with an .alpha.-aminophosphonoacetate and terminating in the acylation of the 7-amino compound, and, if desired, removing the ester blocking group. The products are useful antibiotics.
    Type: Grant
    Filed: November 8, 1973
    Date of Patent: June 28, 1977
    Assignee: Merck & Co., Inc.
    Inventors: Burton G. Christensen, Ronald W. Ratcliffe
  • Preparation of 3-hydroxymethyl-7.beta.-aminoadipoyl-7.alpha.-methoxy-3-cephem-4-carboxy lic acid
    Patent number: 4031085
    Abstract: This invention relates to the preparation of 3-hydroxymethyl-7.beta.-aminoadipoyl-7.alpha.-methoxy-3-cephem-4-carboxyli c acid from 3-(.alpha.-methoxy-p-sulfo-oxycinnamoyloxymethyl)-7.beta.-aminoadipoyl-7.a lpha.-methoxy-3-cephem-4-carboxylic acid or 3-(.alpha.-methoxy-p-hydroxycinnamoyloxymethyl)-7.beta.-aminoadipoyl-7.alp ha.-methoxy-3-cephem-4-carboxylic acid by treatment at 60.degree. C. and pH 3.5-6.5 for about 1 hour. The starting compounds are isolated as fermentation products produced by various Streptomyces species.
    Type: Grant
    Filed: February 17, 1976
    Date of Patent: June 21, 1977
    Assignee: Merck & Co., Inc.
    Inventors: Seemon H. Pines, Matthew A. Kozlowski
  • 1,8-Naphthyridine compounds
    Patent number: 4031103
    Abstract: There is described 2-amino-5,7-disubstituted-naphthyridine and 5,7-disubstituted-naphthyridin-2(1H)-one derivatives with bronchodilating and hypotensive properties prepared by the reaction of 2,6-diaminopyridine with an appropriate .beta.-diketone providing the 2-amino products. The 2-oxo analogs are prepared from the 2-amino products by treatment with nitrous acid.
    Type: Grant
    Filed: December 9, 1975
    Date of Patent: June 21, 1977
    Assignee: Merck Sharp & Dohme (I.A.) Corporation
    Inventors: Hayden Windsor Richard Williams, Clarence Stanley Rooney
  • Process for cleavage of 7-amino-adipoylamino side chain in cephalosporins
    Patent number: 4031086
    Abstract: A process is provided for preparing an ester of 7-amino-7-methoxy-3-acetoxymethyl or methyl-2- or 3-cephem-4-carboxylic acid by reaction of an imino halide ##STR1## wherein R" is a carboxyl blocking group, and R.sup.3 is an amino protecting group, X is halo, preferably bromo or chloro, and A is hydrogen or acetoxy with the following cuprous methyl complex:Li[MeCuBuO]followed by reaction with aqueous ammonia to obtain the desired product.
    Type: Grant
    Filed: March 5, 1976
    Date of Patent: June 21, 1977
    Assignee: Merck & Co., Inc.
    Inventors: Sandor Karady, Joseph S. Amato
  • Substitutive fluorination of organic compounds
    Patent number: 4030994
    Abstract: Organic compounds having at least one replaceable hydrogen atom are fluorinated in the liquid or solid state by treatment with fluoroxyperfluoroalkanes or fluoroxypentafluorosulfur under the influence of a free radical initiator.
    Type: Grant
    Filed: October 9, 1973
    Date of Patent: June 21, 1977
    Assignee: Merck & Co., Inc.
    Inventor: Janos Kollonitsch
  • Antibacterial composition comprising 3-fluoro-D-alanine or deutero analog in combination with auto-antagonist inhibitor
    Patent number: 4031231
    Abstract: Novel antibacterial compositions are prepared by combining 3-fluoro-D-alanine-type compound, such as 3-fluoro-D-alanine and its deutero analogs, and salts and esters thereof, with a 3-fluoro-D-alanine autoantagonist-inhibitor such as cycloserine-type compound. The compositions demonstrate highly effective antibacterial action at high levels of dosage of the 3-fluoro-D-alanine component and, in addition, possess a remarkable synergistic antibacterial action.
    Type: Grant
    Filed: January 23, 1976
    Date of Patent: June 21, 1977
    Assignee: Merck & Co., Inc.
    Inventor: Frederick M. Kahan
  • Fluorinated amino acids
    Patent number: 4028405
    Abstract: Deutero analogs of 3-fluoro-D-alanine prepared by direct photofluorination of the D-amino acids demonstrate in vivo and in vitro antibacterial activity against both gram negative and gram positive microorganisms. Deuters analogs of 3-fluoro-L-alanine and 3-fluoro-D,L-alanine also demonstrate useful in vitro activity.
    Type: Grant
    Filed: June 7, 1976
    Date of Patent: June 7, 1977
    Assignee: Merck & Co., Inc.
    Inventors: Janos Kollonitsch, Frederick M. Kahan
  • Antibiotic FR-02A and therapeutic compositions thereof
    Patent number: 4024251
    Abstract: This invention relates to a new antibiotic agent which also possesses growth promoting activity. The antibiotic is isolated from the fermentation broth of Streptomyces lactamdurans by solvent extraction and designated Efrotomycin.
    Type: Grant
    Filed: February 12, 1976
    Date of Patent: May 17, 1977
    Assignee: Merck & Co., Inc.
    Inventors: William M. Maiese, Richard G. Wax