Patents Assigned to The DuPont Merck Pharmaceutical Company
  • Patent number: 5635477
    Abstract: This invention relates to novel cyclic compounds containing carbocyclic ring systems useful as antagonists of the platelet glycoprotein IIb/IIIa complex, to pharmaceutical compositions containing such cyclic compounds, with or without other therapeutic agents, and to methods of using these compounds, with or without other therapeutic agents, for the inhibition of platelet aggregation, as thrombolytics, and/or for the treatment of other thromboembolic disorders. This invention also relates to methods of using the cyclic compounds of the invention in combination with anti-coagulants such as warfarin or heparin, or additional anti-platelet agents such as aspirin, piroxicam or ticlopidine, or thrombin inhibitors such as boropeptides, hirudin or argatroban, or thrombolytic agents such as tissue plasminogen activator, anistreplase, urokinase or streptokinase, or combinations thereof, for the treatment of thromboembolic disorders. A representative compound of the invention is cyclo(D-Val-(.sup..alpha.
    Type: Grant
    Filed: June 5, 1995
    Date of Patent: June 3, 1997
    Assignee: The DuPont Merck Pharmaceutical Company
    Inventors: William F. Degrado, Sharon A. Jackson, Shaker A. Mousa, Anju Parthasarathy, Michael Sworin, Maria Rafalski
  • Patent number: 5618944
    Abstract: This invention relates to compounds, including 5-chloro-2-[2-[[(4-methylphenyl)sulfonyl]oxy]ethyl]-7-[2,4,6-trimethylphen yl)methoxy]anthra[1,9-cd]pyrazol-6(2H)-one and analogs thereof, which are useful as intermediates for the synthesis of anthrapyrazolone anticancer agents, including losoxantrone. This invention also relates to methods for the synthesis of anthrapyrazolone anticancer agents, including losoxantrone.
    Type: Grant
    Filed: January 10, 1995
    Date of Patent: April 8, 1997
    Assignee: The DuPont Merck Pharmaceutical Company
    Inventors: Lin-Hua Zhang, Joseph Auerbach
  • Patent number: 5616578
    Abstract: This invention relates to a method of treating human immunodeficiency virus (HIV) infection in a mammal comprising administering to the mammal a therapeutically effective amount of a combination of: (i) at least one cyclic HIV protease inhibitor and (ii) at least one HIV reverse transcriptase inhibitor.
    Type: Grant
    Filed: August 26, 1993
    Date of Patent: April 1, 1997
    Assignee: The Dupont Merck Pharmaceutical Company
    Inventor: Michael J. Otto
  • Patent number: 5608075
    Abstract: Polymorphic forms of Losartan (Formula I) ##STR1## and a process for the preparation of Form II of Losartan. Losartan is known to be useful in the treatment of hypertension.
    Type: Grant
    Filed: January 12, 1995
    Date of Patent: March 4, 1997
    Assignees: Merck & Co., Inc., E. I. Du Pont de Nemours & Company, The DuPont Merck Pharmaceutical Company
    Inventors: Gordon C. Campbell, Jr., Anil M. Dwivedi, Dorothy A. Levorse, James A. McCauley, Krishnaswamy S. Raghavan
  • Patent number: 5604112
    Abstract: The present invention provides methods of testing the cardiotoxicity of compounds and kits useful for the same.
    Type: Grant
    Filed: February 26, 1993
    Date of Patent: February 18, 1997
    Assignee: The Dupont Merck Pharmaceutical Company
    Inventors: Paul D. Crane, Cesare Orlandi
  • Patent number: 5597916
    Abstract: Compounds of Formula I have been shown to enhance the release of the neurotransmitter acetylcholine, and thus may be useful as chemical intermediates and as pharmacological agents in the treatment of diseases of man, such as in Alzheimer's Disease and other conditions involving learning and cognition, where subnormal levels of this neurochemical are found.
    Type: Grant
    Filed: February 21, 1996
    Date of Patent: January 28, 1997
    Assignee: The DuPont Merck Pharmaceutical Company
    Inventor: Christopher A. Teleha
  • Patent number: 5593994
    Abstract: This invention relates to ortho substituted phenyl compounds as inhibitors of prostaglandin synthase, to pharmaceutical compositions comprising such compounds and to methods of using such compounds as antiinflammatory and antipyretic agents.
    Type: Grant
    Filed: September 29, 1994
    Date of Patent: January 14, 1997
    Assignee: The DuPont Merck Pharmaceutical Company
    Inventors: Douglas G. Batt, Donald J. P. Pinto, Michael J. Orwat, Joseph J. Petraitis, William J. Pitts
  • Patent number: 5594001
    Abstract: Compounds of Formula (I) have been shown to enhance the release of the neurotransmitter acetylcholine, and thus may be useful in the treatment of diseases of man where subnormal levels of this neurochemical are found, such as in Alzheimer's disease, and other conditions involving learning and cognition.
    Type: Grant
    Filed: March 28, 1994
    Date of Patent: January 14, 1997
    Assignee: The DuPont Merck Pharmaceutical Company
    Inventors: Christopher A. Teleha, Wendell W. Wilkerson, Richard A. Earl
  • Patent number: 5585382
    Abstract: Anticancer compounds of formula I: ##STR1## and pharmaceutically acceptable salts thereof, wherein: R.sup.1, R.sup.2, R.sup.3, R.sup.9 and R.sup.10 are independently selected from the group H, C.sub.1 -C.sub.4 alkyl, OR.sup.4, N(R.sup.4).sub.2, NO.sub.2, CN, F, Cl, Br, I, Ph, and CF.sub.3, and NHC(O)R.sup.4 ;R.sup.4 is independently selected from the group H, C.sub.1 -C.sub.4 alkyl, Ph, and CH.sub.2 Ph;X.sup.1 and Y.sup.1, and X.sup.2 and Y.sup.2 when present, join together to form:a benzene ring substituted with 1-4 R.sup.3 ;a five membered heterocycle having 1-2N, NH, O or S atoms and substituted with 1-2 R.sup.3 ;a six membered heterocycle having 1-2N and substituted with 1-2 R.sup.3 ; orthe group: ##STR2## wherein one of W or Z is C.dbd.O and the other is C.dbd.O, NH, S or O; or when X.sup.2 and Y.sup.2 are present and not joined together and when R.sup.2 is in the 4-position, then X.sup.2 and R.sup.2 may join together to form an ethylene bridge;are addressed.
    Type: Grant
    Filed: February 21, 1995
    Date of Patent: December 17, 1996
    Assignee: The DuPont Merck Pharmaceutical Company
    Inventors: Arthur D. Patten, Gregory Pacofsky, Steven P. Seitz, Emeka A. Akamike, Robert J. Cherney, Robert F. Kaltenbach, III, Michael J. Orwat
  • Patent number: 5583147
    Abstract: This invention provides amide compounds as inhibitors of acyl-Coenzyme A: cholesterol O-acyltransferase (ACAT), pharmaceutical compositions containing such compounds, processes for the preparation of such compounds, and the use of such compounds as antihypercholesterolemic and/or antiatherosclerotic agents.
    Type: Grant
    Filed: March 23, 1994
    Date of Patent: December 10, 1996
    Assignee: The Dupont Merck Pharmaceutical Company
    Inventors: Soo S. Ko, Richard G. Wilde, Indawati DeLucca, Hui-Yin Li, Hollis S. Kezar, III, George A. Boswell, Anurag S. Srivastava
  • Patent number: 5580871
    Abstract: There are provided novel 1,4-dihydropyridine compounds, compositions containing them and methods of using them to treat congestive heart failure.
    Type: Grant
    Filed: March 9, 1995
    Date of Patent: December 3, 1996
    Assignee: The Dupont Merck Pharmaceutical Company
    Inventor: Richard A. Earl
  • Patent number: 5578609
    Abstract: This invention relates to 2-carbocyclic and 2-heterocyclic quinoline-4-carbocyclic acid compounds, and salts thereof, to pharmaceutical compositions comprising such compounds, and to methods of using such compounds for the treatment and/or prevention of organ transplantation rejection, graft versus host disease, and chronic inflammatory diseases, including but not limited to psoriasis and rheumatoid arthritis, in a mammal.
    Type: Grant
    Filed: August 3, 1995
    Date of Patent: November 26, 1996
    Assignee: The DuPont Merck Pharmaceutical Company
    Inventors: Douglas G. Batt, Joseph J. Petraitis, Susan R. Sherk
  • Patent number: 5563127
    Abstract: Novel boronic acid and ester and carboxyl-modified amino acid compounds of the Formula I, which are inhibitors of trypsin-like enzymes, are disclosed :R.sup.1 --Z--CHR.sup.2 --A,where R.sup.1, Z, R.sup.2 and A are defined within.
    Type: Grant
    Filed: December 27, 1994
    Date of Patent: October 8, 1996
    Assignee: The DuPont Merck Pharmaceutical Company
    Inventors: Eugene C. Amparo, William H. Miller, Gregory J. Pacofsky, John Wityak, Patricia C. Weber, John J. V. Duncia, Joseph B. Santella, III
  • Patent number: 5563158
    Abstract: This invention relates to novel compounds containing basic and acidic termini, pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of platelet aggregation, as thrombolytics, and/or for the treatment of thromboembolic disorders.
    Type: Grant
    Filed: November 22, 1994
    Date of Patent: October 8, 1996
    Assignee: The Dupont Merck Pharmaceutical Company
    Inventors: William F. DeGrado, Chu-Biao Xue
  • Patent number: 5559252
    Abstract: The present invention provides a process for the preparation of compounds of formula (V) below, and analogs thereof, which are useful as intermediates for the synthesis of HIV protease inhibitors, including cyclic ureas.
    Type: Grant
    Filed: June 30, 1994
    Date of Patent: September 24, 1996
    Assignee: The DuPont Merck Pharmaceutical Company
    Inventor: Robert F. Kaltenbach III
  • Patent number: 5559110
    Abstract: Compositions comprising a cyclic urea type compound in a liquid or solid vehicle comprising a fatty acid ester of glycerol, or a fatty acid ester of polyethylene glycol, or a mixture thereof, wherein said vehicle has an hydrophil-lipophil balance of at least about 10, and, optionally, other excipients are described. The compositions are useful for providing good systemic absorption of the cyclic urea compounds when administered enterally, especially orally. The subject compounds and compositions are useful for treating viral infections, particularly HIV infection, in a mammal.
    Type: Grant
    Filed: March 9, 1994
    Date of Patent: September 24, 1996
    Assignee: The DuPont Merck Pharmaceutical Company
    Inventor: Bruce J. Aungst
  • Patent number: 5545651
    Abstract: Novel substituted imidazoles of Formula (I), which are useful as angiotensin II antagonists, are disclosed: ##STR1##
    Type: Grant
    Filed: November 28, 1994
    Date of Patent: August 13, 1996
    Assignee: The DuPont Merck Pharmaceutical Company
    Inventors: John J. V. Duncia, Carol L. Ensinger, Richard E. Olson, Mimi L. Quan, Joseph B. Santella, III, Mary K. Vanatten
  • Patent number: 5543517
    Abstract: This invention relates to substituted bicyclic phosphoramides and derivatives thereof, useful as retroviral protease inhibitors and as standards and reagents in determining the ability of a potential pharmaceutical to inhibit viral replication or HIV protease, to pharmaceutical compositions comprising such compounds, and to methods of using these compounds for treating viral infection.
    Type: Grant
    Filed: January 13, 1994
    Date of Patent: August 6, 1996
    Assignee: The DuPont Merck Pharmaceutical Company
    Inventor: Joanne M. Smallheer
  • Patent number: 5532356
    Abstract: The present invention relates to methods for the preparation of disubstituted cyclic ureas of the formula (IV): ##STR1## from linear diaminodiols. These cyclic urea compounds are useful as HIV protease inhibitor compounds for the treatment of HIV infection.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: July 2, 1996
    Assignee: The DuPont Merck Pharmaceutical Company
    Inventors: Thomas E. Smyser, Pasquale N. Confalone
  • Patent number: 5532249
    Abstract: Compounds of Formula I have been shown to enhance the release of the neurotransmitter acetylcholine, and thus may be useful in the treatment of diseases of man, such as in Alzheimer's disease and other conditions involving learning and cognition, where subnormal levels of this neurochemical are found.The compounds of this invention can be described as shown in Formula I ##STR1## where Q is ##STR2## R.sup.1 is 4-,3-, or 2-pyridyl, pyrimidyl, pyrazinyl, or fluoro-4-pyridyl; R.sup.2 and R.sup.3 are independently H, F, Cl, Br, NO.sub.2, OH, --R.sup.4, --O--R.sup.4, --CO.sub.2 R.sup.4, --COR.sup.4, --CONH.sub.2, --CONHR.sup.4, --CONR.sup.4 R.sup.4', --S(O).sub.m2 -- R.sup.4, NH.sub.2, CF.sub.3, NHR.sup.4, NR.sup.4 R.sup.4' ;R.sup.4 and R.sup.4' are independently H, alkyl of 1 to 4 carbons, CH.sub.2 Phe-W or Phe-W;and hydrates and physiologically suitable salts thereof.
    Type: Grant
    Filed: September 26, 1994
    Date of Patent: July 2, 1996
    Assignee: The DuPont Merck Pharmaceutical Company
    Inventors: Wendell W. Wilkerson, Christopher A. Teleha