Patents Represented by Attorney, Agent or Law Firm Elliott Korsen
  • Cyclohexapeptide with basic nitrogen containing alkylamide groups
    Patent number: 5430018
    Abstract: Certain aminoalkyl substituted amides which have a cyclohexapeptidyl group and which are found to have antibiotic activity with physical properties suitable for use in therapeutic compositions are described.
    Type: Grant
    Filed: October 17, 1991
    Date of Patent: July 4, 1995
    Assignee: Merck & Co., Inc.
    Inventor: Robert A. Zambias
  • 1-aminoacetamidopyrroles and 1-amino acetamido-2-(substituted) pyrroles and related compounds
    Patent number: 5428053
    Abstract: There are disclosed 1-aminoacetamidopyrroles and 1-amino-2-(substituted) pyrroles and related compounds of the formula ##STR1## wherein all substituents are defined herein, which are useful as glycine partial agonists and for the enhancement of learning and memory and for the treatment of memory dysfunctions associated with neurodegenerative disorders and are thus indicated in the treatment of Alzheimer's disease and other senile dementias.
    Type: Grant
    Filed: September 28, 1993
    Date of Patent: June 27, 1995
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Lawrence L. Martin, Raymond W. Kosley, Jr., Denise M. Flanagan, Gert U. Kuerzel, Peter A. Nemoto, David G. Wettlaufer
  • Lipopeptide derivatives
    Patent number: 5428009
    Abstract: The present invention is directed to water-soluble derivatives of antibiotic lipopeptides. The derivatives have good solubility properties in aqueous medium, rendering them more useful as therapeutic agents.
    Type: Grant
    Filed: July 16, 1990
    Date of Patent: June 27, 1995
    Assignee: Merck & Co., Inc.
    Inventor: Milton L. Hammond
  • Process for production of an antibiotic compound with Zalerion arboricola
    Patent number: 5426038
    Abstract: A process for producing an antibiotic compound which is normally a minor component in the cultivation of Z. arboricola to be the major product is described.
    Type: Grant
    Filed: February 14, 1994
    Date of Patent: June 20, 1995
    Assignee: Merck & Co, Inc.
    Inventors: Jimmy M. Fountoulakis, Prakash S. Masurekar, Louis Kaplan
  • Antibiotic peptides bearing aminoalkylthioether moieties
    Patent number: 5399552
    Abstract: Certain aminoalkyl thioethers represented by the formula ##STR1## their acid addition salts and quaternary ammonium salts are described. The compounds have useful antimicrobial properties.
    Type: Grant
    Filed: October 17, 1991
    Date of Patent: March 21, 1995
    Assignee: Merck & Co, Inc
    Inventor: Frances A. Bouffard
  • Lipopeptide derivatives
    Patent number: 5386009
    Abstract: The present invention is directed to water-soluble derivatives of antibiotic lipopeptides. The derivatives have good solubility properties in aqueous medium, rendering them more useful as therapeutic agents.
    Type: Grant
    Filed: March 19, 1990
    Date of Patent: January 31, 1995
    Assignee: Merck & Co. Inc.
    Inventors: Milton L. Hammond, Robert E. Schwartz, James M. Balkovec
  • Lipopeptide compounds
    Patent number: 5386010
    Abstract: Antifungal and antiparasital lipopeptide compounds stable in aqueous media are described. Stability in aqueous media render lipopeptides more useful for compositions for therapeutic applications.
    Type: Grant
    Filed: June 15, 1992
    Date of Patent: January 31, 1995
    Assignee: Merck & Co., Inc.
    Inventor: James M. Balkovec
  • Lipopeptide derivatives
    Patent number: 5385884
    Abstract: There are disclosed lipopeptide derviatives of the general formula: ##STR1## where the substituents are defined herein which have antifungal and antiprotozoal activity. There are also disclosed pharmaceutical compositions containing these compounds.
    Type: Grant
    Filed: August 27, 1991
    Date of Patent: January 31, 1995
    Assignee: Merck & Co. Inc.
    Inventors: Milton L. Hammond, Robert E. Schwartz, James M. Balkovec
  • Aza cyclohexapeptide compounds
    Patent number: 5378804
    Abstract: Aza cyclohexapeptide compounds are disclosed with a nitrogen attached to the cyclohexapeptide ring at the 5-carbon of the 4-hydroxyornithine component. Such compounds are represented by the formula: ##STR1## The compounds are disclosed as having antifungal, antiprotozoal and anti-Pneumocystis carinii activity.
    Type: Grant
    Filed: March 16, 1993
    Date of Patent: January 3, 1995
    Assignee: Merck & Co., Inc.
    Inventors: James M. Balkovec, Regina M. Black, Frances A. Bouffard
  • Antibiotic agent
    Patent number: 5366880
    Abstract: A new antibiotic cyclic lipopeptide having the formula ##STR1## wherein R is H or OH and a method of producing is described. The agent has very high activity against human pathogens and is of very low mammalian toxicity.
    Type: Grant
    Filed: May 21, 1993
    Date of Patent: November 22, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Robert E. Schwartz, Prakash S. Masurekar, David F. Sesin, Jerrold M. Liesch, Thomas C. Hallada, Otto D. Hensens
  • Cyclohexapeptidyl hydroxypropionitrile compounds
    Patent number: 5348940
    Abstract: Certain propionitrile compounds which have a cyclohexapeptidyl nucleus and which are found to have antibiotic activity with physical properties suitable for use in therapeutic compositions are described. A novel process for their preparation is also described.
    Type: Grant
    Filed: September 3, 1992
    Date of Patent: September 20, 1994
    Assignee: Merck & Co., Inc.
    Inventors: James M. Balkovec, Robert A. Zambias
  • Antifungal compound and compositions containing the compound
    Patent number: 5348970
    Abstract: A compound of the formula 1: ##STR1## is produced via fermentation of a fungal isolate ATCC no. 74235. The organism is included herein, as well as a process for production of the compound, a pharmaceutical composition and a method of treatment.
    Type: Grant
    Filed: September 22, 1993
    Date of Patent: September 20, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Robert E. Schwartz, Janet C. Onishi, Gerald F. Bills, Robert A. Giacobbe, Fernando Pelaez, Maria T. Diez, Francisca Vicente, Julian Gorrochategui, Gregory L. Helms, Barnali Pramanik
  • 8-azabicyclo[3.2.1]octane methanone and corresponding oximes
    Patent number: 5340936
    Abstract: This invention relates to compounds of the formula ##STR1## where X is --0--, --S--or --NH--;Y is hydrogen, halogen and loweralkoxy;p is 1 or 2;n is 2, 3 or 4;R is hydrogen, loweralkyl, loweralkoxy, hydroxy, halogen, amino, loweralkylamino, nitro, loweralkylthio, trifiuoromethoxy, cyano, trifluoromethyl, ##STR2## where aryl is ##STR3## R.sub.1 is hydrogen, loweralkyl, loweralkoxy, halogen, hydroxy, carboxyl, loweralkylamino, nitro, loweralkylthio, cyano, and trifluoromethyl;m is 1 or 2; a pharmaceutically acceptable acid addition salt thereof and, where applicable the geometric and optical isomers and racemic mixtures thereof.The compounds and compositions of this invention are useful as antipsychotic agent, as 5-HT.sub.3 receptor antagonists and as inhibitors of the reuptake of serotonin.
    Type: Grant
    Filed: March 25, 1993
    Date of Patent: August 23, 1994
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Edward J. Glamkowski, David M. Fink, Barbara E. Kurys, Yulin Chiang
  • Process for crystalline cyclic lipopeptides
    Patent number: 5336756
    Abstract: A process for obtaining a compound of the formula ##STR1## in crystalline form by solubilizing the compound in warm aqueous n-propanol and then allowing the solution to stand at ambient temperature until crystal formation is substantially complete is described. The crystalline compound obtained thereby is also described.
    Type: Grant
    Filed: August 27, 1991
    Date of Patent: August 9, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Robert E. Schwartz, August J. Kempf, David J. Mathre
  • Heteroaryl-8-azabicyclo[3,2,1]octanes as antipsychotic agents, 5-HT.sub.3 receptor antagonists and inhibitors of the reuptake of serotonin
    Patent number: 5334599
    Abstract: This invention relates to compounds of the formula ##STR1## where X is --O--, --S-- or --NH--;Y is hydrogen, halogen and loweralkoxy;p is 1 or 2;n is 2, 3 or 4;R is hydrogen, loweralkyl, loweralkoxy, hydroxy, halogen, amino, loweralkylamino, nitro, loweralkylthio, trifiuoromethoxy, cyano, trifiuoromethyl, ##STR2## R.sub.1 is hydrogen, loweralkyl, loweralkoxy, halogen, hydroxy, carboxyl, loweralkylamino, nitro, loweralkylthio, cyano, and trifiuoromethyl;m is 1 or 2; a pharmaceutically acceptable acid addition salt thereof and, where applicable the geometric and optical isomers and racemic mixtures thereof.The compounds and compositions of this invention are useful as antipsychotic as 5-HT.sub.3 receptor antagonists and as inhibitors of the reuptake of serotonin.
    Type: Grant
    Filed: March 25, 1993
    Date of Patent: August 2, 1994
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Edward J. Glamkowski, David M. Fink, Barbara E. Kurys, Yulin Chiang
  • Assay module transport apparatus for use in an automated analytical instrument
    Patent number: 5332549
    Abstract: An automated analytical instrument for conducting assays for components of interest in fluid samples. The instrument includes a rotably mounted supply unit or segment adapted to hold a plurality of foil-sealed magazines containing assay modules, a testing system for assaying a fluid sample for a component of interest using an assay module, an assay module transport assembly for transporting an assay module from a magazine in the supply unit to the testing system, and a microprocessor for controlling the operation of the automated analytical instrument.
    Type: Grant
    Filed: July 1, 1992
    Date of Patent: July 26, 1994
    Assignee: PB Diagnostic Systems, Inc.
    Inventor: Robert C. MacIndoe, Jr.
  • Lipopeptide derivatives
    Patent number: 5330973
    Abstract: The present invention is directed to water-soluble derivatives of antibiotic lipopeptides. The derivatives have good solubility properties in aqueous medium, rendering them more useful as therapeutic agents.
    Type: Grant
    Filed: March 19, 1990
    Date of Patent: July 19, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Milton L. Hammond, Robert E. Schwartz, James M. Balkovec
  • Analytical assay
    Patent number: 5328852
    Abstract: A method for determining the amount of an analyte in a sample fluid utilizing an assay element which comprises at least one reagent layer. The assay method includes the steps of optically reading a signal producing species, e.g., a fluorescent label, a first time prior to depositing the sample fluid on the assay element and a second time, at the same wavelength and in the same location within the assay element after the sample fluid has been applied to the assay element and the sample analyte has interacted with the reagent(s) present in the assay element. The first, or dry, reading is corrected for relative humidity and/or temperature variations.
    Type: Grant
    Filed: October 16, 1992
    Date of Patent: July 12, 1994
    Assignee: PB Diagnostic Systems, Inc.
    Inventors: John J. Blackwood, Shai Inbar
  • Substituted pyridinylamino 1H-indazoles
    Patent number: 5328918
    Abstract: This invention relates to substituted pyridinylamino-1H-indoles, 1H-indazoles, 2H-indazoles, benzo[b]thiophenes and 1,2-benzisothiazoles of the formula ##STR1## wherein Q is S, N or NR.sub.2 ;Y is CH, N or NR.sub.2 ;R.sub.1 is hydrogen, loweralkyl, loweralkynyl, loweralkenyl, arylloweralkyl, loweralkoxycarbonylaminoloweralkylcarbonyl, arylloweralkoxycarbonylaminoloweralkylcarbonyl, aminoloweralkylcarbonyl, loweralkoxycarbonyl or acyl;R.sub.2 is hydrogen or loweralkyl;R.sub.3 is hydrogen or loweralkyl;X is hydrogen, loweralkyl, halogen; andn is 0 or 1; or a pharmaceutically acceptable acid addition salt thereof.The compounds of this invention are useful in the treatment of memory dysfunctions characterized by a cholinergic deficit such as the type associated with Alzheimer's disease and other memory disorders.
    Type: Grant
    Filed: March 25, 1993
    Date of Patent: July 12, 1994
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Richard C. Effland, Joseph T. Klein, Lawrence L. Martin
  • Pyrazolo[4,3-c]pyridines and their use as serotonin reuptake inhibitors
    Patent number: 5296491
    Abstract: There are disclosed novel pyrazolo[4,3-c]pyridines of the formula ##STR1## where Ar and R.sub.1 are as defined in the specification, which are useful as serotonin reuptake inhibitors and as such may be useful for the treatment of depression, obsessive-compulsive disorders, stuttering and trichotillomania.
    Type: Grant
    Filed: August 17, 1993
    Date of Patent: March 22, 1994
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Gregory M. Shutske, Kevin J. Kapples, John D. Tomer, IV