Patents Represented by Attorney Stephen L. Nesbitt
  • Patent number: 4935449
    Abstract: The importance of polyamines in biological systems is discussed as well as the implications of polyamines in the treatment of various diseases. Novel N-substituted-2,3-butadienyl tri- and tetra-aminoalkanes are disclosed as well as their use inthe treatment of diseases and the pharmaceutical compositions.
    Type: Grant
    Filed: August 4, 1988
    Date of Patent: June 19, 1990
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: Philippe Bey, David M. Stemerick, Michael L. Edwards, Alan J. Bitonti
  • Patent number: 4912095
    Abstract: This invention relates to novel 5-(R.sub.n -phenyl)-2,4-dialkyl-3H-1,2,4-triazole-3-thiones and to their use as antidepressants.
    Type: Grant
    Filed: February 8, 1989
    Date of Patent: March 27, 1990
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: John M. Kane, Francis P. Miller
  • Patent number: 4902719
    Abstract: This invention relates to ornithine derivatives substituted at the 5 position with an R group which can be a --CH.sub.2 F, --CHF.sub.2, --CHClF, --C.tbd.CH, --CH.dbd.CH.sub.2, or --CH.dbd.C.dbd.CH.sub.2 group and the pharmaceutically acceptable acid addition salts thereof which are specific inhibitors of OAT and can be used in the treatment of conditional deficiencies of ornithine.
    Type: Grant
    Filed: February 1, 1989
    Date of Patent: February 20, 1990
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: Fritz E. Gerhart, Nikolaus J. Seiler
  • Patent number: 4900743
    Abstract: This invention relates to derivatives of 3-aryl-5-alkylthio-4H-1,2,4-triazoles, to their pharmacological properties and to their use as muscle relaxants, spasmolytics, anticonvulsants and anxiolytics.
    Type: Grant
    Filed: December 4, 1987
    Date of Patent: February 13, 1990
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: John M. Kane, Francis P. Miller
  • Patent number: 4882419
    Abstract: Process for preparing antibiotic L, 17392 by catalytically hydrogenating a deglucoteicoplanin ester of formula ##STR1## wherein A, B and Z represent hydrogen atoms, R represents benzyl or substituted benzyl, wherein the phenyl group is substituted with at least a substituent selected from chloro, bromo, fluoro, nitro, (C.sub.1 -C.sub.3)alkyl, (C.sub.1 -C.sub.3)alkoxy and the like, with the exclusion of the tri-nitro phenyl group, or acid addition salts thereof, to catalytic hydrogenolysis in the presence of a poisoned hydrogenation catalyst at a temperature from 10.degree. C. to 40.degree. C. and a pressure between ambient pressure and 5 atm, in an inert organic solvent preferably in the presence of a mineral acid.
    Type: Grant
    Filed: February 6, 1986
    Date of Patent: November 21, 1989
    Assignee: Gruppo Lepetit S.p.A.
    Inventors: Adriano Malabarba, Paolo Strazzolini, Bruno Cavalleri
  • Patent number: 4868182
    Abstract: This invention relates to the synergistic enhancement of certain antihypertensives by the conjunctive use of certain cardiotonic agents. More specifically, this invention relates to the enhancement of the blood pressure lowering effect achieved with alpha.sub.1 -adrenoceptor antagonists by the conjunctive administration of cardiotonic agents possessing the ability to specifically inhibit cyclic AMP-phosphodiesterase.
    Type: Grant
    Filed: February 3, 1988
    Date of Patent: September 19, 1989
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventor: Richard C. Dage
  • Patent number: 4866182
    Abstract: Alkanoyl or aroyl oxazolones enhance myocardial contractile force and are useful as cardiotonics in the treatment of heart failure.
    Type: Grant
    Filed: February 18, 1988
    Date of Patent: September 12, 1989
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: Richard A. Schnettler, Winton D. Jones, Richard C. Dage
  • Patent number: 4866085
    Abstract: Phenyloxazolones are useful as cardiotonics in the treatment of heart failure and enhance cardiac function.
    Type: Grant
    Filed: November 24, 1987
    Date of Patent: September 12, 1989
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: Richard A. Schnettler, George P. Claxton, Winton D. Jones, Jr.
  • Patent number: 4861756
    Abstract: Certain polypeptide-phospholipid complexes consisting of the amphipathic, helical portion of human apo A and its analogs and a phospholipid are useful in the treatment of neonatal respiratory distress syndrome.
    Type: Grant
    Filed: October 26, 1988
    Date of Patent: August 29, 1989
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventor: Richard L. Jackson
  • Patent number: 4857526
    Abstract: This invention relates to aromatic 2-aminoalkyl derivatives of 1,2-benzoisothiazol-3(2H)one-1,1-dioxides, processes for the preparation of same, and to their use as anxiolytic and antihypertensive agents.
    Type: Grant
    Filed: September 12, 1988
    Date of Patent: August 15, 1989
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: Marcel Hibert, Maurice W. Gittos
  • Patent number: 4853395
    Abstract: Novel 5-acyl-2-(1H)pyridinones and their use as cardiotonic agents. Typical of the compounds is 5-acetyl-1,2-dihydro-6-methyl-2-oxo-3-pyridinecarbonitrile which is prepared by condensing anionic cyano acetamide with 3-[(dimethylamino)methylenyl]-2,4-pentanedione in an inert organic solvent.
    Type: Grant
    Filed: November 17, 1987
    Date of Patent: August 1, 1989
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: Winton D. Jones, Richard A. Schnettler, Richard C. Dage
  • Patent number: 4851447
    Abstract: 1. A compound of the formula:H.sub.2 C.dbd.C.dbd.CHCH.sub.2 NHCH.sub.2 --Z--CH.sub.2 NHRwherein:Z is --CH.sub.2 CH.sub.2 -- or trans--CH.dbd.CH--,R is H, CH.sub.3 --, CH.sub.3 CH.sub.2, CH.sub.3 (CH.sub.2).sub.2 --, --(CH.sub.2).sub.3 NH.sub.2, --(CH.sub.2).sub.3 NHCOCH.sub.3, --CH.sub.2 CH.dbd.CH.sub.2, or --CH.sub.2 CH.dbd.C.dbd.CH.sub.2, or a pharmaceutically acceptable acid addition salt thereof are inhibitors of polyamine oxidase.
    Type: Grant
    Filed: January 5, 1988
    Date of Patent: July 25, 1989
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventor: Philippe Bey
  • Patent number: 4849522
    Abstract: This invention relates to alkoxyimino ether derivatives of 5-acyl-2(1H)-pyridinones and to their use as cardiotonic agents useful in treating cardiac failure, and to the process useful in the preparation thereof.
    Type: Grant
    Filed: March 10, 1988
    Date of Patent: July 18, 1989
    Assignee: Merrell Dow Pharmaceuticals
    Inventors: Winton D. Jones, Richard C. Dage, Richard A. Schnettler
  • Patent number: 4847401
    Abstract: The large scale preparation of ethyl 2,2-difluoro-4- pentenoate and 2-fluorinated methyl aminoacetonitriles by reaction of 2-H-perfluoroethyl allyl ether and n-butyl lithium and fluoromethylacetonitrile and a Grignard reagent, respectively, is largly unsuccessful because of side reactions which convert intermediate products and reactants to undesired products. Applicants have overcome these problems by performing the reactions with cooling in a continuous manner in a flow reactor with short residence time.
    Type: Grant
    Filed: January 15, 1988
    Date of Patent: July 11, 1989
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: Fritz Gerhart, Michael Kolb
  • Patent number: 4832849
    Abstract: Applicant has isolated a Factor X.sub.a inhibiting substance from the salivary gland extract of the leech H.ghilianii. The extract is subjected to separation using both DEAE-cellulose and heparin-agarose chromatography resins eluting with an increasing salt gradient. The extract is subjected to affinity chromatography using Factor X.sub.a bound to an Affi-Gel-15 resin eluting with HEPES containing benzamidine. Reverse phase chromatography yields several purified peptides or proteins having Factor X.sub.a inhibiting activity. The properties and clinical compositions of these FX.sub.a inhibitors are described.
    Type: Grant
    Filed: June 16, 1988
    Date of Patent: May 23, 1989
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventor: Alan D. Cardin
  • Patent number: 4804534
    Abstract: A novel antibiotic, A 42867, is prepared by cultivating the strain Nocardia sp. ATCC 53492, or an antibiotic A 42867-producing mutant or variant thereof, under submerged aerobic conditions in the presence of assimilable sources of carbon, nitrogen and inorganic salts. The antibiotic and its addition salts are useful in the treatment of infectious diseases and as growth promotant agents.
    Type: Grant
    Filed: July 28, 1987
    Date of Patent: February 14, 1989
    Assignee: Gruppo Lepetit S.p.A.
    Inventors: Ernesto Riva, Enrico Selva, Maurizio Denaro, Giovanni Cassani, Francesco Parenti
  • Patent number: 4804682
    Abstract: The compound, 2-chloro-4-((cyanomethyl)thiolphenyl N-methyl carbamate, is a therapeutic agent in the treatment of patients afflicted with carcinomas or lymphocytic leukemia.
    Type: Grant
    Filed: November 14, 1986
    Date of Patent: February 14, 1989
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventor: Walter Reifschneider
  • Patent number: 4803210
    Abstract: Tricyclic oxazolones enhance myocardial contractile force and are useful as cardiotonics in the treatment of heart failure.
    Type: Grant
    Filed: April 14, 1988
    Date of Patent: February 7, 1989
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: Winton D. Jones, Richard A. Schnettler, George P. Claxton, Richard C. Dage
  • Patent number: 4789676
    Abstract: This invention relates to aromatic 2-aminoalkyl derivatives of 1,2-benzoisothiazol-3(2H)one-1,1-dioxides, processes for the preparation of same, and to their use as anxiolytic and antihypertensive agents.
    Type: Grant
    Filed: February 22, 1988
    Date of Patent: December 6, 1988
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: Marcel Hibert, Maurice W. Gittos
  • Patent number: 4789661
    Abstract: The present invention is directed to new de-(acetylglucosaminyl-di(dehydro)deoxy teicoplanin derivatives which possess antibiotic activity mainly against gram positive bacteria.The new compounds are obtained by chemical modification of a teicoplanin antibiotic substance.
    Type: Grant
    Filed: July 17, 1987
    Date of Patent: December 6, 1988
    Assignee: Gruppo Lepetit S.p.A.
    Inventors: Adriano Malabarba, Aldo Trani, Pietro Ferrari, Giorgio Tarzia