Abstract: The invention encompasses novel compounds of Formula I, which are nitric oxide-releasing prodrugs of diaryl-2-(5H) furanones useful in the treatment of cyclooxygenase-2 mediated diseases. The invention also encompasses certain pharmaceutical compositions and methods for treatment of cyclooxygenase-2 mediated diseases comprising the use of compounds of Formula I.
Type:
Grant
Filed:
July 24, 2003
Date of Patent:
April 3, 2007
Assignee:
Merck Frosst Company
Inventors:
Carl Berthelette, Nicholas Lachance, Lianhai Li, Claudio Sturino, Zhaoyin Wang, Robert N. Young, Claude Dufresne
Abstract: The invention encompasses novel compounds of Formula I, which are nitric oxide-releasing prodrugs of diaryl-2-(5H) furanones useful in the treatment of cyclooxygenase-2 mediated diseases. The invention also encompasses certain pharmaceutical compositions and methods for treating cyclooxygenase-2 mediated diseases comprising the use of compounds of Formula I. The above compounds may be used as a combination therapy with low-dose aspirin to treat chronic cyclooxygenase-2 mediated diseases or conditions while also reducing the risk of thrombotic cardiovascular events.
Type:
Grant
Filed:
March 1, 2004
Date of Patent:
January 30, 2007
Assignee:
Merck Frosst Company
Inventors:
Carl Berthelette, Lianhai Li, Claudio Sturino, Zhaoyin Wang
Abstract: 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:
Grant
Filed:
October 18, 2000
Date of Patent:
February 19, 2002
Assignee:
The DuPont Merck Pharmaceutical Company
Inventors:
Jorge Osvaldo Nicolini, Ricardo Julio Ughetti
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:
June 17, 1996
Date of Patent:
November 23, 1999
Assignee:
The DuPont Merck Pharmaceutical Company
Inventors:
Christopher Allan Teleha, Wendell Wilkie Wilkerson, Richard Alan Earl
Abstract: 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:
Grant
Filed:
December 17, 1996
Date of Patent:
August 17, 1999
Assignee:
The DuPont Merck Pharmaceutical Company
Inventors:
Mimi Lifen Quan, John Wityak, Robert Anthony Galemmo, Jr., Petrus F. W. Stouten, James Russell Pruitt, Donald J. P. Pinto
Abstract: 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:
Grant
Filed:
March 28, 1994
Date of Patent:
March 9, 1999
Assignee:
The Dupont Merck Pharmaceutical Company
Inventors:
William Frank DeGrado, Shaker Ahmed Mousa, Michael Sworin, John Andrew Barrett, Scott David Edwards, Thomas David Harris, Milind Rajopadhye, Shuang Liu
Abstract: 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.
Abstract: 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:
Grant
Filed:
March 12, 1997
Date of Patent:
December 15, 1998
Assignee:
The DuPont Merck Pharmaceutical Company
Inventors:
Gregory James Wells, John Wityak, Anju Parthasarathy, William Frank DeGrado, Sharon Anne Jackson, Shaker Ahmed Mousa
Abstract: 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:
Grant
Filed:
May 31, 1995
Date of Patent:
December 15, 1998
Assignee:
The DuPont Merck Pharmaceutical Company
Inventors:
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
Abstract: 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:
Grant
Filed:
November 22, 1996
Date of Patent:
September 22, 1998
Assignee:
The DuPont Merck Pharmaceutical Company
Inventors:
Patrick Yuk-Sun Lam, Prabhakar Kondaji Jadhav, Charles Joseph Eyermann, Carl Nicholas Hodge, George Vincent De Lucca, James David Rodgers
Abstract: 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.
Abstract: 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:
Grant
Filed:
November 14, 1994
Date of Patent:
June 30, 1998
Assignee:
The DuPont Merck Pharmaceutical Company
Inventors:
Gregory James Wells, John Wityak, Anju Parthasarathy, William Frank DeGrado, Sharon Anne Jackson, Shaker Ahmed Mousa
Abstract: 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.
Abstract: 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.
Abstract: 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:
Grant
Filed:
December 20, 1996
Date of Patent:
June 2, 1998
Assignee:
The DuPont Merck Pharmaceutical Company
Inventors:
Prabhakar Kondaji Jadhav, Joseph James Petraitis, Douglas Guy Batt
Abstract: 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:
Grant
Filed:
March 13, 1997
Date of Patent:
June 2, 1998
Assignee:
The DuPont Merck Pharmaceutical Company
Inventors:
Prabhakar Kondaji Jadhav, Joanne Marie Smallheer
Abstract: 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:
Grant
Filed:
June 7, 1995
Date of Patent:
May 12, 1998
Assignee:
The DuPont Merck Pharmaceutical Company
Inventors:
Michael Sworin, Milind Rajopadhye, Thomas David Harris, David Scott Edwards, Edward Hollister Cheesman, Shuang Liu
Abstract: 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:
Grant
Filed:
February 1, 1995
Date of Patent:
May 12, 1998
Assignee:
The DuPont Merck Pharmaceutical Company
Inventors:
Barry Stephen Brown, Simon Piers Aiken, Robert Zaczek, Paul Richard Hartig, Christopher Allan Teleha, Wendell Wilkie Wilkerson, Richard Alan Earl
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:
March 8, 1996
Date of Patent:
April 14, 1998
Assignee:
The DuPont Merck Pharmaceutical Company
Inventors:
Gary Avonn Cain, Charles Joseph Eyermann, Richard Eric Olson
Abstract: 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:
Grant
Filed:
March 24, 1995
Date of Patent:
March 24, 1998
Assignee:
The DuPont Merck Pharmaceutical Company
Inventors:
David John Carini, Joseph Cacciola, Celia Dominguez, John Matthew Fevig