Patents Represented by Attorney, Agent or Law Firm Blair Q. Ferguson
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Patent number: 6713042Abstract: The invention relates to the use of ascorbic acid analogs as buffering reagents and chelating agents for the preparation of metalloradiopharmaceuticals. Also, invention relates to the use of ascorbic acid as a buffering reagent, a chelating agent, and a stabilizer for the preparation and stabilization of radiopharmaceuticals and processes for making and using the same.Type: GrantFiled: February 22, 2002Date of Patent: March 30, 2004Assignee: Bristol-Myers Squibb Pharma CompanyInventor: Shuang Liu
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Patent number: 6569402Abstract: The present invention describes novel compounds of the formula: (Q)d—Ln—Ch, useful for the diagnosis and treatment of cancer, methods of imaging tumors in a patient, and methods of treating cancer in a patient. The present invention also provides novel compounds useful for monitoring therapeutic angiogenesis treatment and destruction of new angiogenic vasculature. The present invention further provides novel compounds useful for imaging atherosclerosis, restenosis, cardiac ischemia and myocardial reperfusion injury. The present invention still further provides novel compounds useful for the treatment of rheumatoid arthritis. The pharmaceuticals are comprised of a targeting moiety that binds to a receptor that is upregulated during angiogenesis, an optional linking group, and a therapeutically effective radioisotope or diagnostically effective imageable moiety.Type: GrantFiled: June 21, 2000Date of Patent: May 27, 2003Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Edward H. Cheesman, John A. Barrett, Alan P. Carpenter, Jr., Milind Rajopadhye, Michael Sworin
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Patent number: 6562965Abstract: The present invention relates to processes for the production of &agr;-aryl-&bgr;-ketonitriles, which serve as synthetic intermediates in the preparation of a series of biologically important molecules such as corticotropin releasing factor (CRF) receptor antagonists.Type: GrantFiled: July 6, 2000Date of Patent: May 13, 2003Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Jiacheng Zhou, Lynette May Oh, Philip Ma
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Patent number: 6399609Abstract: Corticotropin releasing factor (CRF) antagonists of formula I: and their use in treating anxiety, depression, and other psychiatric and neurological disorders.Type: GrantFiled: May 11, 2000Date of Patent: June 4, 2002Assignee: Bristol-Myers Squibb Pharma CompanyInventor: Richard Gerald Wilde
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Patent number: 6191131Abstract: Corticotropin releasing factor (CRF) antagonists of formula I or II: and their use in treating anxiety, depression, and other psychiatric, neurological disorders as well as treatment of immunological, cardiovascular or heart-related diseases and colonic hypersensitivity associated with psychopathological disturbance and stress.Type: GrantFiled: January 28, 1998Date of Patent: February 20, 2001Assignee: DuPont Pharmaceuticals CompanyInventors: Liqi He, Paul Gilligan, Robert Chorvat, Argyrios Georgios Arvanitis
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Patent number: 6187918Abstract: Novel chiral aminoalcohol catalysts and methods for their preparation are provided. The first catalyst is prepared via selective hydrogenation of one of two benzene rings in a precursor. The aminoalcohol promotes the asymmetric addition of organozinc reagents to aldehydes to afford optically active alcohols or their esters. The second catalyst is prepared by selective dialkylation of 3-exo-aminoisoborneol with a 2-haloethyl ether. The aminoalcohol promotes the addition of organozinc reagents to aliphatic aldehydes containing a &bgr;-branch with greatly enhanced enantioselectivity relative to DAIB.Type: GrantFiled: March 10, 2000Date of Patent: February 13, 2001Assignee: DuPont Pharmaceuticals CompanyInventor: William A. Nugent
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Patent number: 6174912Abstract: Corticotropin releasing factor (CRF) antagonists of Formulae (I) or (II): and their use in treating psychiatric disorders and neurological diseases including major depression, anxiety-related disorders, post-traumatic stress disorder, supranuclear palsy and feeding disorders as well as treatment of immunological, cardiovascular or heart-related diseases and colonic hypersensitivity associated with psychopathological disturbance and stress.Type: GrantFiled: August 21, 1998Date of Patent: January 16, 2001Assignee: DuPont Pharmaceuticals CompanyInventors: James P. Beck, Paul J. Gilligan
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Patent number: 6027695Abstract: An apparatus for holding liquid, such as a microtiter plate, in which a plurality of wells are formed. Each of the wells have side walls that intersect in an edge that defines the boundary between adjacent wells. The edge boundary prevents liquid from collecting between the wells, thereby causing all of the liquid applied to the plate to enter one of the wells. The microtiter plate can be formed from a material having a reflectance and/or fluorescence that is optimized for the particular application in which the microtiter plate will be used. Microtiter plates for use in fluorescence measurement applications are made from material having low fluorescence, such as a liquid crystal polymer, while microtiter plates for use in luminescence measurements are made from material having a high reflectance. Microtiter plates for spectrophotometric applications are made with wells having clear bottoms and opaque walls.Type: GrantFiled: April 1, 1998Date of Patent: February 22, 2000Assignee: DuPont Pharmaceuticals CompanyInventors: Kevin R. Oldenburg, Gregory F. Hollis, Thomas D. Y. Chung
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Patent number: 5880295Abstract: 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: GrantFiled: June 19, 1996Date of Patent: March 9, 1999Assignee: DuPont Pharmaceuticals CompanyInventor: Robert Frank Kaltenbach, III
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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: 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: 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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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: 5710159Abstract: This invention relates to novel heterocycle compounds including but not limited to 3-?3-?3-(imidazolin-2-yl amino)propyloxy!isoxazol-5-ylcarbonylamino!-2-(benzyloxycarbonylamino)-pro pionic acid, which are useful as antagonists of the .alpha..sub.v .beta..sub.3 and related integrin 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 and the treatment of angiogenic disorders, inflammation, bone degradation, tumors, metastases, thrombosis, and other cell aggregation-related conditions.Type: GrantFiled: May 9, 1996Date of Patent: January 20, 1998Assignee: The DuPont Merck Pharmaceutical CompanyInventors: Matthew Ernst Voss, Prabhakar Kondaji Jadhav, Joanne Marie Smallheer, Douglas Guy Batt, William John Pitts, John Wityak
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Patent number: 5696119Abstract: This invention relates to (2-quinoxalinyloxy)phenoxypropanoic acids, related derivatives thereof, enantiomeric and diastereomeric forms thereof, mixtures of enantiomeric diastereomeric forms thereof, and pharmaceutically acceptable salt forms thereof, pharmaceutical compositions containing them, processes for their preparation, and methods of using them to treat cancer, particularly solid tumors, in mammals.Type: GrantFiled: December 28, 1994Date of Patent: December 9, 1997Assignee: The DuPont Merck Pharmaceutical CompanyInventors: Carl Henry Behrens, Betsy Ann Dusak, Barbara Ann Harrison, Michael James Orwat
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Patent number: 5683999Abstract: This invention relates to substituted cyclic ureas and derivatives thereof, including compounds of formula (II): ##STR1## said compounds being useful as inhibitors of HIV protease. The present invention also relates to pharmaceutical compositions comprising such compounds and to method of using these compounds for the treatment HIV infection. The present invention also relates to the use of such compounds in processes for the identification of HIV protease inhibitors and for the inhibition or detection of HIV in a bodily fluid sample.Type: GrantFiled: March 11, 1996Date of Patent: November 4, 1997Assignee: The DuPont Merck Pharmaceutical CompanyInventors: Prabhakar Kondaji Jadhav, Soo Sung Ko
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Carbocyclic and heterocyclic fused-ring quinolinecarboxylic acids useful as immunosuppressive agents
Patent number: 5639759Abstract: This invention relates to carbocyclic and heterocyclic fused-ring quinolinecarboxylic acid compounds, 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, autoimmune diseases, chronic inflammatory diseases, including but not limited to psoriasis and rheumatoid arthritis, and cancer in a mammal.Type: GrantFiled: March 27, 1995Date of Patent: June 17, 1997Assignee: The DuPont Merck Pharmaceutical CompanyInventors: Ronald Louis Magolda, William John Pitts, Irina Cipora Jacobson, Carl Henry Behrens, Michael James Orwat, Douglas Guy Batt -
Patent number: 5635477Abstract: 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: GrantFiled: June 5, 1995Date of Patent: June 3, 1997Assignee: The DuPont Merck Pharmaceutical CompanyInventors: William F. Degrado, Sharon A. Jackson, Shaker A. Mousa, Anju Parthasarathy, Michael Sworin, Maria Rafalski
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Patent number: 5616578Abstract: 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: GrantFiled: August 26, 1993Date of Patent: April 1, 1997Assignee: The Dupont Merck Pharmaceutical CompanyInventor: Michael J. Otto
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Patent number: 5610294Abstract: 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: February 16, 1994Date of Patent: March 11, 1997Assignee: The Du Pont Merck Pharmaceutical CompanyInventors: Patrick Y. Lam, Prabhakar K. Jadhav, Charles J. Eyermann, Carl N. Hodge, George V. De Lucca, James D. Rodgers