Patents Assigned to G. D. Searle
  • N-protected/N-substituted-beta-amino-hydroxy sulfonates
    Patent number: 6147253
    Abstract: N-protected/N-substituted alpha-amino aldehydes, which are useful as pharmaceuticals and pharmaceutical intermediates, can be stored and shipped in a more stable form as N-protected/N-substituted-beta-amino hydroxy sulfonates which can be readily converted back into the aldehyde under mild conditions. The present invention relates to N-protected/N-substituted-beta-amino hydroxy sulfonates and their preparation and use.
    Type: Grant
    Filed: August 16, 1999
    Date of Patent: November 14, 2000
    Assignee: G. D. Searle & Co.
    Inventor: Joseph J. Wieczorek
  • Sulfonylalkanoylamino hydroxyethylamino sulfonamides useful as retroviral protease inhibitors
    Patent number: 6147117
    Abstract: Sulfonamide-containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Grant
    Filed: July 13, 1999
    Date of Patent: November 14, 2000
    Assignee: G. D. Searle & Co.
    Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel Getman, Gary A. DeCrescenzo, John N. Freskos
  • Bis-amino acid hydroxyethlamino sulfonamide retroviral protease inhibitors
    Patent number: 6143788
    Abstract: Selected bis-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.
    Type: Grant
    Filed: January 21, 1998
    Date of Patent: November 7, 2000
    Assignee: G.D. Searle & Co.
    Inventors: Daniel P. Getman, Gary A. Decrescenzo, John N. Freskos, Michael L. Vazquez, James A. Sikorski, Belekudru Devadas, Srinivasan RAJ Nagarajan, David L. Brown, Joseph J. McDonald
  • Bis-sulfonamide hydroxyethylamino retroviral protease inhibitors
    Patent number: 6143747
    Abstract: Bis-sulfonamido hydroxyethylamino compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to retroviral protease inhibiting compounds of the formula: ##STR1## or a pharmaceutically acceptable salt, prodrug or ester thereof, wherein the variables are as defined herein.
    Type: Grant
    Filed: February 26, 1998
    Date of Patent: November 7, 2000
    Assignee: G. D. Searle & Co.
    Inventors: John N. Freskos, Daniel P. Getman, John J. Talley, James A. Sikorski
  • Process for making 5-substituted pyrazoles
    Patent number: 6143892
    Abstract: This invention relates to a novel process of preparing selected 5-substituted pyrazoles useful as p38 kinase and COX-2 inhibitors.
    Type: Grant
    Filed: November 18, 1999
    Date of Patent: November 7, 2000
    Assignee: G. D. Searle & Co.
    Inventors: Matthew J. Graneto, Michael L. Vazquez, Susan J. Hartmann, Suzanne Metz, John J. Talley, David L. Brown, Richard M. Weier, Michael A. Stealey, Xiaodong C. Xu
  • L-N.sup.6 -(1-iminoethyl)lysine derivatives useful as nitric oxide synthase inhibitors
    Patent number: 6143790
    Abstract: There is disclosed a novel amino glycol derivatives of L-N.sup.6 -(1-iminoethyl)lysine, pharmaceutical compositions containing these novel compounds, and to their use in therapy, in particular their use as nitric oxide synthase inhibitors.
    Type: Grant
    Filed: September 6, 1996
    Date of Patent: November 7, 2000
    Assignee: G.D. Searle & Co.
    Inventors: E. Ann Hallinan, Foe S. Tjoeng, Kam F. Fok, Timothy J. Hagen, Mihaly V. Toth, Sofya Tsymbalov, Barnett S. Pitzele
  • Synthesis of benzo fused heterocyclic sulfonyl chlorides
    Patent number: 6140505
    Abstract: A process for preparing a benzo fused heterocyclic sulfonyl halide comprising reacting a benzo fused heterocyclic compound with an SO.sub.3 complex in the presence of a water immiscible, non-reactive solvent, at a temperature of from about 0.degree. C. to about 75.degree. C., cooling, if necessary, to a temperature of from about -25.degree. C. to about 65.degree. C. and then adding oxalyl halide.
    Type: Grant
    Filed: May 19, 1998
    Date of Patent: October 31, 2000
    Assignee: G. D. Searle & Co.
    Inventors: Sastry A. Kunda, Leo J. Letendre, Gary A. De Crescenzo
  • Oxathiadiazole derivatives usful as iNOS inhibitors
    Patent number: 6136829
    Abstract: 1,3-diazolino and 1,3-diazolidino heterocycle derivatives useful as nitric oxide synthase inhibitors.
    Type: Grant
    Filed: July 19, 1999
    Date of Patent: October 24, 2000
    Assignee: G.D. Searle & Co.
    Inventors: Donald W. Hansen, Jr., Ariia A. Bergmanis, Timothy J. Hagen, E. Ann Hallinan, Steven W. Kramer, Suzanne Metz, Karen B. Peterson, Barnett S. Pitzele, Foe S. Tjoeng, Mihaly V. Toth, Mahima Trivedi, R. Keith Webber, Sofya Tsymbalov, Rolando E. Gapud
  • Treatment of inflammation and inflammation-related disorders with a combination of a cyclooxygenase-2 inhibitor and a 5-lipoxygenase inhibitor
    Patent number: 6136839
    Abstract: Combinations of a cyclooxygenase-2 inhibitor and a 5-lipoxygenase inhibitor are described for treatment of inflammation and inflammation-related disorders.
    Type: Grant
    Filed: June 11, 1996
    Date of Patent: October 24, 2000
    Assignee: G. D. Searle & Co.
    Inventors: Peter C Isakson, Gary D Anderson, Susan A Gregory
  • Human interleukin-3 (IL-3) variant fusion proteins
    Patent number: 6132991
    Abstract: The present invention relates to fusion molecules composed of human interleukin-3 (hIL-3) variant or mutant proteins (muteins) functionally joined to a second colony stimulating factor (CSF), cytokine, lymphokine, interleukin or IL-3 variant. These hIL-3 variants contain amino acid substitutions and may also have amino acid deletions at both the N- and C-termini. The invention also relates to pharmaceutical compositions containing the fusion molecules and methods for using them.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: October 17, 2000
    Assignee: G. D. Searle & Co.
    Inventors: S. Christopher Bauer, Mark Allen Abrams, Sarah Ruth Braford-Goldberg, Maire Helena Caparon, Alan Michael Easton, Barbara Kure Klein, John Patrick McKearn, Peter O. Olins, Kumnan Paik, John Warren Thomas
  • Radiopharmaceutical compositions capable of localizing at sites of thrombus
    Patent number: 6132697
    Abstract: A radiopharmaceutical capable of localizing at a site of thrombus containing activated platelets within a mammalian body is provided wherein the radiopharmaceutical comprises a linear peptidomimetic containing ligand capable of specifically binding to the GPIIb/IIIa integrin receptor of platelets in the thrombus and a radionuclide covalently bound to the peptidomimetic containing ligand. The ligand compositions of the invention are provided complexed with a selected metal radionuclide to form a diagnostic or therapeutic radiopharmaceutical to image a site of thrombus or provide radiotherapy to the site of thrombus, respectively.
    Type: Grant
    Filed: June 5, 1997
    Date of Patent: October 17, 2000
    Assignee: G. D. Searle & Co.
    Inventors: Ananthachari Srinivasan, Larry P. Feigen, Daniel Lee Flynn, Jeffery Alan Zablocki, Philip Needleman, Michelle A. Schmidt
  • Epoxide formation by continuous in-situ synthesis process
    Patent number: 6127556
    Abstract: In a method of preparing an aminoepoxide wherein a protected aminoaldehyde is reacted with a halomethyl organometallic reagent in an appropriate solvent at a temperature above -80.degree. C., wherein said halomethyl organometallic reagent is formed by reaction between an organometallic reagent and a dihalomethane, the improvement comprising flowing said protected aminoaldehyde into a mixing zone maintained at a temperature below 0.degree. C., also flowing said halomethyl organometallic reagent in said mixing zone for contacting in said mixing zone with said protected aminoaldehyde and also withdrawing from said mixing zone reaction products of said protected aminoaldehyde and said halomethyl organometallic reagent.
    Type: Grant
    Filed: December 16, 1997
    Date of Patent: October 3, 2000
    Assignee: G. D. Searle & Co.
    Inventors: Chin Liu, John S. Ng, James R. Behling, Arthur L. Campbell
  • Primer sets for analyzing cytochrome P450 isoenzymes expression
    Patent number: 6127117
    Abstract: Hepatocyte culturing system, primer sets and an analytical method for selectively detecting and quantitatively assessing the levels of mRNA expression of the major isoenzymes of cytochrome P450 (CYP450 1A1, 1A2, 2B1/2, 2C11, 2E1, 3A1, 3A2 and 4A1), fatty acyl-CoA oxidase (FACO) and select Phase II conjugating enzymes (UDPGT, GST and ST) in the rat using specific 5' and 3' oligonucleotide primers and reverse transcriptase-polymerase chain reaction. The method closely reproduces the expression obtained from rat liver tissue following treatment with the same enzyme inducers. Constitutive and inducible expression was maintained by resuspending, culturing and then overlaying adult rat hepatocytes with an extracellular matrix such as Matrigel.RTM..
    Type: Grant
    Filed: May 13, 1997
    Date of Patent: October 3, 2000
    Assignee: G. D. Searle & Co.
    Inventors: Dale Lynn Morris, Julio Cesar Davila
  • Non-heterocyclic .beta.-phenyl-.alpha.-aminopropionic acid n-phenyl amides for treatment of neurotoxic injury
    Patent number: 6114381
    Abstract: Compounds, compositions and methods of treatment are described to control brain damage associated with anoxia or ischemia which typically follows stroke, cardiac arrest or perinatal asphyxia. The treatment includes administration of a .beta.-phenyl-.alpha.-aminopropionic acid N phenyl amide compound as an antagonist to inhibit excitotoxic actions at major neuronal excitatory amino acid receptor sites. Compounds of most interest are those of the formula ##STR1## wherein each of R.sup.1 and R.sup.5 is independently selected from hydrido, fluoro, chloro, bromo, methyl and ethyl; wherein R.sup.3 is selected from hydroxy, methoxy, ethoxy, methoxycarbonyloxy, ethoxycarbonyloxy, (2-methylpropoxy)carbonyloxy and (2-propenyloxy) carbonyloxy; wherein each of R.sup.6, R.sup.7 and R.sup.8 is hydrido; wherein each of R.sup.9 and R.sup.10 is independently selected from hydrido, methyl and ethyl; wherein R.sup.
    Type: Grant
    Filed: October 13, 1998
    Date of Patent: September 5, 2000
    Assignee: G. D. Searle & Co.
    Inventors: Barnett S. Pitzele, Nizal S. Chandrakumar, Michael Clare
  • LTA.sub.4, hydrolase inhibitors
    Patent number: 6110944
    Abstract: The present invention provides compounds having the structureAr.sub.1 --Q--Ar.sub.2 --O--(CH.sub.2).sub.n --Zand pharmaceutically acceptable salts and stereoisomers thereof that are useful in the treatment of inflammatory diseases which are mediated by LTB.sub.4 production, such as psoriasis, ulcerative colitis, IBD, and asthma.
    Type: Grant
    Filed: March 12, 1997
    Date of Patent: August 29, 2000
    Assignee: G. D. Searle & Co.
    Inventors: Barbara Baosheng Chen, Helen Chen, Mark Andrew Russell
  • Substituted 5-aryl-benzothiepines having activity as inhibitors of ileal bile acid transport and taurocholate uptake
    Patent number: 6107494
    Abstract: Provided are novel benzothiepines, derivatives, and analogs thereof; pharmaceutical compositions containing them; and methods of using these compounds and compositions in medicine, particularly in the prophylaxis and treatment of hyperlipidemic conditions such as those associated with atherosclerosis or hypercholesterolemia, in mammals.
    Type: Grant
    Filed: March 24, 1999
    Date of Patent: August 22, 2000
    Assignee: G.D. Searle and Company
    Inventors: Len F. Lee, Shyamal C. Banerjee, Horng-Chih Huang, Jinglin J. Li, Raymond E. Miller, David B. Reitz, Samuel J. Tremont
  • Modified-release metronidazole compositions and methods for making and using same
    Patent number: 6103262
    Abstract: Pharmaceutical compositions having a modified release profile for once daily dosing of metronidazole, methods for making the pharmaceutical compositions, and methods for treating a microbial infection with once daily dosing of the pharmaceutical compositions of the invention are provided. The compositions given once daily exhibit substantial bioequivalence to immediate release metronidazole given three times per day. The compositions of the invention comprise:(a) a first portion of metronidazole which is about 59 wt % to about 79 wt % metronidazole;(b) about 1.5 wt % to about 3.0 wt % of an aqueous insoluble poly(meth)acrylic acid ester copolymer which is aqueous permeable, aqueous expandable and pH-independent;(c) about 0.1 wt % to about 2.
    Type: Grant
    Filed: January 27, 1994
    Date of Patent: August 15, 2000
    Assignee: G. D. Searle & Company
    Inventors: Subhash Desai, Alan Mark Mancini, Steven Charles Schumann
  • Amino benzenepropanoic acid compounds and derivatives thereof
    Patent number: 6100423
    Abstract: The present invention is directed to compounds of the formula ##STR1## where R.sup.1 is BOC or H, R is H or lower alkyl; X and Y are the same or different halo atoms selected from the group consisting of Cl, Br or I and pharmaceutically acceptable salts and isomers thereof.
    Type: Grant
    Filed: March 3, 1999
    Date of Patent: August 8, 2000
    Assignee: G. D. Searle & Co.
    Inventors: Joe T. Collins, Balekudru Devadas, Hwang-fun Lu, James W. Malecha, Julie Marion Miyashiro, Srinivasan Nagarajan, Joseph Gerace Rico, Thomas E. Rogers
  • G-CSF receptor agonists
    Patent number: 6100070
    Abstract: Disclosed are novel G-CSF receptor agonist proteins, DNAs which encode the multi-functional hematopoietic receptor agonists proteins, methods of making the multi-functional hematopoietic receptor agonists proteins and methods of using the multi-functional hematopoietic receptor agonists proteins.
    Type: Grant
    Filed: April 4, 1997
    Date of Patent: August 8, 2000
    Assignee: G. D. Searle & Co.
    Inventors: Linda L. Zurfluh, Barbara K. Klein, Charles A. McWherrter, Yiqing Feng, John P. McKearn, Sarah Ruth Braford-Goldberg
  • Retroviral protease inhibitor combinations
    Patent number: 6100277
    Abstract: The present invention is directed to a method for the treatment of mammalian retrovirus infections, such as HIV, using combinations of retroviral protease inhibitors which are effective in preventing the replication of the retroviruses in vitro or in vivo. This invention, in particular, relates to protease inhibitor compounds used in combination therapy with other protease inhibitor compounds. This invention also relates to combination therapy with a combination of protease inhibitors and antiviral agents other than protease inhibitors.
    Type: Grant
    Filed: June 2, 1995
    Date of Patent: August 8, 2000
    Assignee: G.D. Searle & Co.
    Inventors: Simon P Tucker, Martin L Bryant, Karen E Potts, Mary L Smidt