Patents Assigned to The DuPont Merck Pharmaceutical Company
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Patent number: 6348184Abstract: Novel radiopharmaceutical compositions comprising, in combination with a pharmaceutically acceptable carrier, a radioactive salt of pyrophosphoric acid. Also provided are novel radiopharmaceutical compositions comprising, in combination with one or more polymeric resins, a radioactive salt of pyrophosphoric acid. The compositions and matrices are suitable, inter alia, for use in treatment methods involving brachytherapy.Type: GrantFiled: October 18, 2000Date of Patent: February 19, 2002Assignee: The DuPont Merck Pharmaceutical CompanyInventors: Jorge Osvaldo Nicolini, Ricardo Julio Ughetti
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Patent number: 5990132Abstract: 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: GrantFiled: June 17, 1996Date of Patent: November 23, 1999Assignee: The DuPont Merck Pharmaceutical CompanyInventors: Christopher Allan Teleha, Wendell Wilkie Wilkerson, Richard Alan Earl
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Patent number: 5939418Abstract: Isoxazolines, isothiazolines and pyrazolines which are inhibitors of Factor Xa, pharmaceutical compositions containing these compounds, and methods of using these compounds as anticoagulant agents for treatment and prevention of thromboembolic disorders. The compounds can be represented by the formula: ##STR1## where X is O, S or NR.sup.15.Type: GrantFiled: December 17, 1996Date of Patent: August 17, 1999Assignee: The DuPont Merck Pharmaceutical CompanyInventors: Mimi Lifen Quan, John Wityak, Robert Anthony Galemmo, Jr., Petrus F. W. Stouten, James Russell Pruitt, Donald J. P. Pinto
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Patent number: 5879657Abstract: This invention provides novel radiopharmaceuticals that are radiolabeled cyclic compounds containing carbocyclic or heterocyclic ring systems which act as antagonists of the platelet glycoprotein IIb/IIIa complex; to methods of using said radiopharmaceuticals as imaging agents for the diagnosis of arterial and venous thrombi; to novel reagents for the preparation of said radiopharmaceuticals; and to kits comprising said reagents.Type: GrantFiled: March 28, 1994Date of Patent: March 9, 1999Assignee: The Dupont Merck Pharmaceutical CompanyInventors: William Frank DeGrado, Shaker Ahmed Mousa, Michael Sworin, John Andrew Barrett, Scott David Edwards, Thomas David Harris, Milind Rajopadhye, Shuang Liu
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Patent number: 5866154Abstract: Physically and chemically stable pharmaceutical compositions useful for administering naloxone by injection are described. These compositions are essentially aqueous solutions having a pH between 3.0-3.5, and containing naloxone, an acidic or buffer component, a tonicity-adjusting agent, and a stabilizing agent, said composition being optionally sterilized by autoclaving.Type: GrantFiled: June 25, 1996Date of Patent: February 2, 1999Assignee: The DuPont Merck Pharmaceutical CompanyInventors: Surendra Mohan Bahal, Lei-Shu Wu
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Patent number: 5849693Abstract: This invention relates to novel cyclic compounds linked by a heterocyclic ring system, which are useful as antagonists of the platelet glycoprotein IIb/IIIa complex, to pharmaceutical compositions containing such cyclic compounds, and to methods of using these compounds for the inhibition of platelet aggregation.Type: GrantFiled: March 12, 1997Date of Patent: December 15, 1998Assignee: The DuPont Merck Pharmaceutical CompanyInventors: Gregory James Wells, John Wityak, Anju Parthasarathy, William Frank DeGrado, Sharon Anne Jackson, Shaker Ahmed Mousa
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Patent number: 5849736Abstract: This invention relates to novel isoxazolines and isoxazoles which are useful as antagonists of the platelet glycoprotein IIb/IIIa fibrinogen receptor complex or the vitronectin receptor, to 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: GrantFiled: May 31, 1995Date of Patent: December 15, 1998Assignee: The DuPont Merck Pharmaceutical CompanyInventors: John Wityak, Chu-Biao Xue, Thais Motria Sielecki-Dzurdz, Richard Eric Olson, William Frank Degrado, Gary Avonn Cain, Douglas Guy Batt, Donald Pinto, Munir Alwan Hussain, Shaker Ahmed Mousa
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Patent number: 5811441Abstract: This invention relates to improved isoxazoline compounds including, but not limited to N.sup.2 -(3,5-dimethylisoxazole-4-sulfonyl)-N.sup.3 -?3-(4-amidinophenyl)isoxazolin-5(R)-ylacetyl!-(S)-2,3-diaminopropionic acid, which are useful as antagonists of the platelet glycoprotein IIb/IIIa fibrinogen receptor complex, to pharmaceutical compositions containing 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: GrantFiled: September 3, 1997Date of Patent: September 22, 1998Assignee: The DuPont Merck Pharmaceutical CompanyInventors: Richard Eric Olson, John Wityak
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Patent number: 5811422Abstract: This invention relates to substituted cyclic carbonyls and derivatives thereof useful as retroviral protease inhibitors, to pharmaceutical compositions comprising such compounds, and to methods of using these compounds for treating viral infection. A representative compound of the invention is the compound of formula: ##STR1## wherein R.sup.22 and R.sup.23 are allyl.Type: GrantFiled: November 22, 1996Date of Patent: September 22, 1998Assignee: The DuPont Merck Pharmaceutical CompanyInventors: Patrick Yuk-Sun Lam, Prabhakar Kondaji Jadhav, Charles Joseph Eyermann, Carl Nicholas Hodge, George Vincent De Lucca, James David Rodgers
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Patent number: 5773411Abstract: This invention relates to novel cyclic compounds linked by a heterocyclic ring system, which are useful as antagonists of the platelet glycoprotein IIb/IIIa complex, to pharmaceutical compositions containing such cyclic compounds, and to methods of using these compounds for the inhibition of platelet aggregation. A representative compound of the invention is cyclo-(D-Val-N(Me)Arg-Gly-Asp-?5-aminomethyl!-2-furoate).Type: GrantFiled: November 14, 1994Date of Patent: June 30, 1998Assignee: The DuPont Merck Pharmaceutical CompanyInventors: Gregory James Wells, John Wityak, Anju Parthasarathy, William Frank DeGrado, Sharon Anne Jackson, Shaker Ahmed Mousa
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Patent number: 5769080Abstract: Contrast agents for ultrasonic imaging comprising gas filled liposomes prepared using vacuum drying gas instillation methods, and gas filled liposomes substantially devoid of liquid in the interior thereof, are described. Methods of and apparatus for preparing such liposomes and methods for employing such liposomes in ultrasonic imaging applications are also disclosed. Also described are diagnostic kits for ultrasonic imaging which include the subject contrast agents.Type: GrantFiled: February 22, 1994Date of Patent: June 23, 1998Assignee: DuPont Merck Pharmaceutical CompanyInventors: Evan C. Unger, Guanli Wu
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Patent number: 5763469Abstract: The present invention relates to substituted cyclic ureas and analogs thereof of formula (I): ##STR1## wherein, T is selected from: --N(R.sup.22)C(.dbd.Z)N(R.sup.23)--; --N(R.sup.22)C(.dbd.Z)C(.dbd.Z)N(R.sup.23)--; --N(R.sup.22)S(.dbd.Z')N(R.sup.23)--; --N(R.sup.22)S(.dbd.Z').sub.2 N(R.sup.23)--; or --N(R.sup.22)P(.dbd.O)(R.sup.24a)N(R.sup.23)--;Z is O, S, NR.sup.24 ; and,Z' is O or NR.sup.24 ;or pharmaceutically acceptable salt forms or prodrugs thereof, which are useful as retroviral protease inhibitors, and to pharmaceutical compositions comprising such compounds and methods of using the same for treating viral infection.Type: GrantFiled: August 21, 1996Date of Patent: June 9, 1998Assignee: The DuPont Merck Pharmaceutical CompanyInventor: George Vincent Delucca
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Patent number: 5760028Abstract: This invention relates to novel heterocycles including 3-?1-?3-(imidazolin-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2-(benzylo xycarbonylamino)propionic acid, which are useful as antagonists of the .alpha..sub.v .beta..sub.3 integrin and related cell surface adhesive protein receptors, to 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 cell adhesion, the treatment of angiogenic disorders, inflammation, bone degradation, cancer metastasis, diabetic retinopathy, thrombosis, restenosis, macular degeneration, and other conditions mediated by cell adhesion and/or cell migration and/or angiogenesis.Type: GrantFiled: December 20, 1996Date of Patent: June 2, 1998Assignee: The DuPont Merck Pharmaceutical CompanyInventors: Prabhakar Kondaji Jadhav, Joseph James Petraitis, Douglas Guy Batt
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Patent number: 5760029Abstract: This invention relates to novel heterocycles, including (S)-2-phenylsulfonylamino-3-???8-(2-pyridinylaminomethyl)-!-1-oxa-2-azaspi ro-?4,5!-dec-2-en-3-yl!carbonylamino! propionic acid, which are useful as antagonists of the .alpha..sub.v .beta..sub.3 integrin and related cell surface adhesive protein receptors, to 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 cell adhesion, the treatment of angiogenic disorders, inflammation, bone degradation, cancer metastasis, diabetic retinopathy, thrombosis, restenosis, macular degeneration, and other conditions mediated by cell adhesion and/or cell migration and/or angiogenesis.Type: GrantFiled: March 13, 1997Date of Patent: June 2, 1998Assignee: The DuPont Merck Pharmaceutical CompanyInventors: Prabhakar Kondaji Jadhav, Joanne Marie Smallheer
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Stable hydrazones linked to a peptide moiety as reagents for the preparation of radiopharmaceuticals
Patent number: 5750088Abstract: This invention provides novel reagents for the preparation of radiopharmaceuticals useful as imaging agents for the diagnosis of cardiovascular disorders, infection, inflammation and cancer, diagnostic kits comprising said reagents and intermediate compounds useful for the preparation of said reagents. The reagents are comprised of stable hydrazone modified biologically active molecules that react with gamma emitting radioisotopes to form radiopharmaceuticals that selectively localize at sites of disease and thus allow an image to be obtained of the loci using gamma scintigraphy.Type: GrantFiled: June 7, 1995Date of Patent: May 12, 1998Assignee: The DuPont Merck Pharmaceutical CompanyInventors: Michael Sworin, Milind Rajopadhye, Thomas David Harris, David Scott Edwards, Edward Hollister Cheesman, Shuang Liu -
Patent number: 5750528Abstract: Compounds which block neuronal M-channels are useful for treating conditions involving neurotransmitter deficiencies, traumatic brain injury, or the depressive phase of bipolar disorder. Compounds can be evaluated for utility in treating these conditions by determining whether they are capable of blocking neuronal M-channels.Type: GrantFiled: February 1, 1995Date of Patent: May 12, 1998Assignee: The DuPont Merck Pharmaceutical CompanyInventors: Barry Stephen Brown, Simon Piers Aiken, Robert Zaczek, Paul Richard Hartig, Christopher Allan Teleha, Wendell Wilkie Wilkerson, Richard Alan Earl
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Patent number: 5739163Abstract: 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: GrantFiled: March 8, 1996Date of Patent: April 14, 1998Assignee: The DuPont Merck Pharmaceutical CompanyInventors: Gary Avonn Cain, Charles Joseph Eyermann, Richard Eric Olson
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Patent number: 5731439Abstract: The present invention relates generally to .alpha.-aminoboronic acids and corresponding peptide analogs in which the .alpha.-carbon is substituted with an optionally functionalized piperidine containing alkyl group. These compounds are useful as inhibitors of trypsin-like serine protease enzymes.Type: GrantFiled: March 24, 1995Date of Patent: March 24, 1998Assignee: The DuPont Merck Pharmaceutical CompanyInventors: David John Carini, Joseph Cacciola, Celia Dominguez, John Matthew Fevig
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Patent number: 5726284Abstract: Disclosed are novel crosslinked polymeric ammonium salts wherein in said polymeric salt: about 25% or more of the segments which link ammonium nitrogen atoms are group Y wherein Y is an n-alkylene group or alkyl substituted n-alkylene group, wherein said n-alkylene group has 7 to about 20 carbon atoms; zero to about 75% of segments which link ammonium nitrogen atoms are group Z wherein Z is a hydrocarbylene radical containing 2 or more carbon atoms, said hydrocarbylene radical optionally containing one or more hydroxyl, ether, amino, thioether, keto, or silyl groups or heterocyclic rings; and about 25% or more of the ammonium atoms are secondary ammonium atoms.Type: GrantFiled: May 22, 1996Date of Patent: March 10, 1998Assignees: The DuPont Merck Pharmaceutical Company, E. I. du Pont de Nemour and CompanyInventors: Garret Daniel Figuly, Jose Ricardo Matos
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Patent number: 5710286Abstract: This invention relates to novel compounds and derivatives thereof containing a trioxepane protected diol in addition to a hydrazone, hydrazine, amine, or cyclic urea moiety; methods for the preparation of said compounds; and the use of said compounds in processes to prepare human immunodeficiency virus (HIV) protease inhibitors which effectively inhibit HIV. The novel compounds provided by this invention have the formulae: ##STR1## wherein the substituents are as defined herein.Type: GrantFiled: November 14, 1995Date of Patent: January 20, 1998Assignee: The DuPont Merck Pharmaceutical CompanyInventors: Lucius Thomas Rossano, Young Sek Lo