Nitrogen Bonded Directly To The Five-membered Hetero Ring By Nonionic Bonding Patents (Class 514/426)
  • Use of iminosugar derivatives to inhibit ion channel activity
    Publication number: 20040110795
    Abstract: Disclosed are methods to treat HCV infection by administering an iminosugar derivative compound that is effective to inhibit the activity of HCV p7 protein, and methods by which to screen for compounds that inhibit the activity of p7 protein or variants thereof. The disclosed N-substituted imino compounds, and pharmaceutical compositions thereof, inhibit the capacity of HCV p7 to permeabilize membranes.
    Type: Application
    Filed: September 23, 2003
    Publication date: June 10, 2004
    Applicant: United Therapeutics Corp.
    Inventors: Nicole Zitzmann, Raymond Allen Dwek Frs
  • Dopamine D4 receptor antagonists as treatment for attention deficit-hyperactivity disorder
    Patent number: 6747029
    Abstract: A method of inhibiting motor hyperactivity in a mammal exhibiting the symptoms of attention deficit-hyperactivity disorder (ADHD) includes administering to a mammal a dopamine D4 receptor-selective antagonist.
    Type: Grant
    Filed: March 12, 2002
    Date of Patent: June 8, 2004
    Assignee: The McLean Hospital Corporation
    Inventors: Ross J. Baldessarini, Kehong Zhang, Frank I. Tarazi
  • N-(4-sulfonylaryl)cyclylamine-2-hydroxyethylamines as beta-3 adrenergic receptor agonists
    Patent number: 6743787
    Abstract: This invention provides compounds of Formula I having the structure wherein R1, R2, R3, R4, W, X, and Y are as defined hereinbefore or a pharmaceutically acceptable salt thereof, which are useful in treating metabolic disorders related to insulin resistance or hyperglycemia.
    Type: Grant
    Filed: July 25, 2002
    Date of Patent: June 1, 2004
    Assignee: Wyeth
    Inventors: Fuk-Wah Sum, Michael Sotirios Malamas
  • Substituted amino-aza-cycloalkanes useful against malaria
    Publication number: 20040102431
    Abstract: The invention relates to novel compounds which are substituted amino-aza-cycloalkane derivatives of the general formula I. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more compounds of general formula I and especially their use as inhibitors of the plasmodium falciparum protease plasmepsin II or related aspartic proteases.
    Type: Application
    Filed: March 25, 2003
    Publication date: May 27, 2004
    Inventors: Christoph Boss, Walter Fischli, Solange Meyer, Sylvia Richard-Bildstein, Thomas Weller
  • Process for preparing aminoguanidines and alkoxyguanidines as protease inhibitors
    Patent number: 6730783
    Abstract: Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: wherein X is O or NR9 and R1-R4, R6-R9, R11, R12, Ra, Rb, Rc, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity.
    Type: Grant
    Filed: April 22, 2003
    Date of Patent: May 4, 2004
    Assignee: 3-Dimensional Pharmaceuticals, Inc.
    Inventors: Bruce E. Tomczuk, Richard M. Soll, Tianbao Lu, Cynthia L. Fedde, Carl R. Illig, Thomas P. Markotan
  • Use of glycogen phosphorylase inhibitors for treatment of cardiovascular diseases
    Publication number: 20040082646
    Abstract: The present invention provides methods which may effectively be used in the treatment and prevention of early cardiac and early cardiovascular diseases, for example of ischemic origin, such as left ventricular hypertrophy, coronary artery disease, essential hypertension, acute hypertensive emergency, cardiomyopathy, heart insufficiency, exercise tolerance, chronic heart failure, arrhythmia, cardiac dysrhythmia, syncopy, arteriosclerosis, mild chronic heart failure, angina pectoris, cardiac bypass reocclusion, intermittent claudication (arteriosclerosis oblitterens), diastolic dysfunction and systolic dysfunction, as well as improving the success of heart transplantations, through administration of glycogen phosphorylase inhibitor compounds.
    Type: Application
    Filed: May 5, 2003
    Publication date: April 29, 2004
    Inventors: Klaus Asger Rytved, Nils Dragsted, Niels Chresten Berg Nyborg, Lars Iversen, Marit Kristiansen
  • Use of glycogen phosphorylase inhibitors for treatment of cardiovascular diseases
    Publication number: 20040082641
    Abstract: The present invention provides methods of treatment and prevention of early cardiac and early cardiovascular diseases, for instance of ischemic origin, such as left ventricular hypertrophy, coronary artery disease, essential hypertension, acute hypertensive emergency, cardiomyopathy, heart insufficiency, exercise tolerance, chronic heart failure, arrhythmia, cardiac dysrhythmia, syncopy, arteriosclerosis, mild chronic heart failure, angina pectoris, cardiac bypass reocclusion, intermittent claudication (arteriosclerosis oblitterens), diastolic dysfunction and systolic dysfunction, as well as improving the success of heart transplantations, through administration of glycogen phosphorylase inhibitor compounds.
    Type: Application
    Filed: May 5, 2003
    Publication date: April 29, 2004
    Inventors: Klaus Asger Rytved, Nils Dragsted, Niels Chresten Berg Nyborg, Lars Iversen, Marit Kristiansen
  • Novel compounds that inhibit factor xa activity
    Publication number: 20040082547
    Abstract: The present invention relates to compounds of the Formula 1
    Type: Application
    Filed: November 20, 2003
    Publication date: April 29, 2004
    Inventors: Seven Nerdinger, Thilo Fuchs, Katrin Illgen, Robert Eckl
  • Abc expression promoters
    Publication number: 20040077689
    Abstract: The ABCA1 mRNA expression-promoting agent, LXR&agr; mRNA expression-promoting agent, ABCG1 mRNA expression-promoting agent, cholesterol efflux-promoting agent, cholesteryl ester accumulation-inhibiting agent, ACAT-1 mRNA expression-inhibiting agent and CEH mRNA expression-promoting agent of the present invention are excellent in the ability to control cholesterol distribution in the body and have low toxicity.
    Type: Application
    Filed: October 16, 2003
    Publication date: April 22, 2004
    Inventors: Yasuo Sugiyama, Hiromatsu Fuse, Masao Hirakata, Ryuichi Tozawa
  • Pyrrole based inhibitors of glycogen synthase kinase 3
    Publication number: 20040077707
    Abstract: New pyrrole based compounds, compositions and methods of inhibiting the activity of glycogen synthase kinase (GSK3) in vitro and of treatment of GSK3 mediated disorders in vivo are provided. The methods, compounds and compositions of the invention may be employed alone, or in combination with other pharmacologically active agents in the treatment of disorders mediated by GSK3 activity, such as diabetes, Alzheimer's disease and other neurodegenerative disorders, obesity, atherosclerotic cardiovascular disease, essential hypertension, polycystic ovary syndrome, syndrome X, ischemia, traumatic brain injury, bipolar disorder, immunodeficiency or cancer.
    Type: Application
    Filed: August 21, 2003
    Publication date: April 22, 2004
    Inventors: Manoj C. Desai, Simon Ng, Zhi-Jie Ni, Keith B. Pfister, Savithri Ramurthy, Sharadah Subramanian, Allan S. Wagman
  • Nucleoside compounds and their use for treating cancer and diseases associated with somatic mutations
    Publication number: 20040067900
    Abstract: The invention encompasses nucleoside compounds, compositions comprising the compounds and methods for treating or preventing diseases associated with nonsense mutations of mRNA by administering these compounds or compositions.
    Type: Application
    Filed: July 22, 2003
    Publication date: April 8, 2004
    Inventors: Richard G. Wilde, Paul D. Kennedy, Neil G. Almstead, Ellen M. Welch, James J. Takasugi, Westley J. Friesen
  • Treatments for restless legs syndrome
    Patent number: 6716854
    Abstract: The invention provides methods and use of heterocyclic amines, and phenylazacycloalkane compounds, and their pharmacologically acceptable salts for the treatment of Restless Legs Syndrome (RLS).
    Type: Grant
    Filed: April 25, 2003
    Date of Patent: April 6, 2004
    Assignee: Pfizer, Inc.
    Inventors: Sylvia McBrinn, Richard Wayne Anderson
  • Modulation of pathogenicity
    Publication number: 20040063765
    Abstract: The present invention relates to the use of compounds of the general Formula (I): 1
    Type: Application
    Filed: May 6, 2003
    Publication date: April 1, 2004
    Applicant: 4 SC AG
    Inventors: Aldo Ammendola, Katharina Aulinger-Fuchs, Astrid Gotschlich, Bernd Kramer, Martin Lang, Wael Saeb, Udo Sinks, Andreas Wuzik
  • Substituted heterocyclic phthalic acid diamide arthropodicides
    Publication number: 20040063738
    Abstract: Compounds of (I), and their N-oxides and agriculturally suitable salts, are disclosed which are useful for controlling invertebrate pests (Formula) wherein J is selected from the group consisting of J-1, J-2, J-3, J-4, J-5, J-6, J-7 and J-8 (I) and R1, R2, R3, R4, R5, R7, R9 and n are as defined in the disclosure. Also disclosed are compositions for controlling an invertebrate pest comprising a biologically effective amount of a compound of (I) and methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound of (I) (e.g., as a composition described herein).
    Type: Application
    Filed: April 30, 2003
    Publication date: April 1, 2004
    Inventors: George Philip Lahm, Thomas Paul Selby
  • Alkanoic acid derivatives process for their production and use thereof
    Publication number: 20040058965
    Abstract: An alkanoic acid derivative useful as a prophylactic or therapeutic agent of diabetes mellitus, hyperlipidemia, impaired glucose tolerance and the like can be provided by a compound represented by the formula 1
    Type: Application
    Filed: June 26, 2003
    Publication date: March 25, 2004
    Inventors: Yu Momose, Tsuyoshi Maekawa, Nobuyuki Takakura, Hiroyuki Odaka, Hiroyuki Kimura, Tatsuya Ito
  • Compounds with analgesic effect
    Patent number: 6710179
    Abstract: Compounds of general formula (I) wherein m is 0 or 1, and n is 1 or 2; are disclosed and claimed in the present application, as well as their pharmaceutically acceptable salts, pharmaceutical compositions comprising the novel compounds and their use in therapy, in particular in the management of pain.
    Type: Grant
    Filed: April 15, 2002
    Date of Patent: March 23, 2004
    Assignee: AstraZeneca Canada Inc.
    Inventors: Benjamin Pelcman, Edward Roberts
  • Cyclic derivatives as modulators of chemokine receptor activity
    Patent number: 6706712
    Abstract: The present application describes modulators of MCP-1 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of rheumatoid arthritis, multiple sclerosis, atherosclerosis and asthma.
    Type: Grant
    Filed: December 20, 2001
    Date of Patent: March 16, 2004
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventor: Robert Cherney
  • Aniline derivatives or salts thereof and cytokine production inhibitors containing the same
    Publication number: 20040048891
    Abstract: The present invention provides a cytokine production inhibitor containing as an active ingredient an aniline derivative of the formula (I) or a salt thereof: 1
    Type: Application
    Filed: June 19, 2003
    Publication date: March 11, 2004
    Inventors: Fuminori Kato, Hirohiko Kimura, Shunji Yuki, Kazuhiro Yamamoto, Takashi Okada
  • Substituted hydrazine derivatives
    Publication number: 20040039025
    Abstract: A method for the inhibition of high affinity glycine transporters, compounds that inhibit these transporters; pharmaceutically active compositions comprising such compounds; and the use of such compounds either as above, or in formulations for the control or prevention of disease states in which glycine is involved are disclosed.
    Type: Application
    Filed: August 28, 2003
    Publication date: February 26, 2004
    Inventors: Syed M. Ali, Kurt R. Brunden, Dario Doller, Brian Herbert, Jack B. Jiang, Amy Jordan
  • Aminoadamantane derivatives as therapeutic agents
    Publication number: 20040029929
    Abstract: The present invention provides novel aminoadamantane derivatives, methods of making the derivatives, compositions including the novel aminoadamantane derivatives, and methods for the treatment and prevention of neurological diseases using the derivatives and compositions.
    Type: Application
    Filed: August 4, 2003
    Publication date: February 12, 2004
    Inventors: Yuqiang Wang, Wenqing Ye, James W. Larrick, Jonathan S. Stamler, Stuart A. Lipton
  • Aminediols for the treatment of Alzheimer's disease
    Publication number: 20040019086
    Abstract: The present invention relates to compounds of formula (I): 1
    Type: Application
    Filed: July 10, 2002
    Publication date: January 29, 2004
    Inventors: Heinrich Josef Schostarez, Robert Alan Chrusciel
  • IL-8 receptor antagonists
    Patent number: 6680317
    Abstract: This invention relates to novel compounds of Formula (I), and compositions thereof, useful in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).
    Type: Grant
    Filed: September 17, 2002
    Date of Patent: January 20, 2004
    Assignee: SmithKline Beecham Corporation
    Inventors: Michael R. Palovich, Katherine L. Widdowson, Hong Nie
  • Biphenyl derivatives and the use thereof as integrin inhibitors
    Publication number: 20040010023
    Abstract: The invention relates to novel biphenyl derivatives of the general formula (I), wherein R4 represents an aromatic heterocycle, and to the physiologically acceptable salts or solvates thereof. The inventive compounds are integrin inhibitors and are used for combating thromboses, cardiac infarction, coronary heart diseases, arteriosclerosis, inflammations, tumors, osteoporosis, infections and restenosis following angioplasty or for pathological processes that are maintained or propagated by angiogenesis.
    Type: Application
    Filed: February 21, 2003
    Publication date: January 15, 2004
    Inventors: Wolfgang Stahle, Gunter Holzemann, Simon Goodman
  • Substituted N-phenyl-N-heteroaralkyl aminoalcohol compounds useful for inhibiting cholesteryl ester transfer protein activity
    Patent number: 6677353
    Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N-phenyl-N-heteroaralkyl aminoalcohols.
    Type: Grant
    Filed: May 23, 2002
    Date of Patent: January 13, 2004
    Assignee: Pharmacia Corporation
    Inventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
  • (R)-Chiral halogenated substituted heteroaryl benzyl aminoalcohol compounds useful for inhibiting cholesteryl ester transfer protein activity
    Patent number: 6677341
    Abstract: The invention relates to substituted aryl and heteroaryl (R)-Chiral Halogenated 1-Substitutedamino-(n+1)-Alkanol compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Novel high yield, stereoselective processes for the preparation of the chiral substituted alkanol compounds from chiral and achiral intermediates are described. Preferred (R)-Chiral 1-Substitutedamino-(n+1)-Alkanol compounds are substituted (R)-Chiral heteroaryl aminoalcohols.
    Type: Grant
    Filed: December 12, 2001
    Date of Patent: January 13, 2004
    Assignee: Pharmacia Corporation
    Inventors: James A. Sikorski, Richard C. Durley, Margaret L. Grapperhaus, Mark A. Massa, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Brian S. Hickory, Monica B. Norton, William F. Vernier, Deborah A. Mischke, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
  • Aminoazetidine,-pyrrolidine and -piperidine derivatives
    Patent number: 6673829
    Abstract: Novel aminoazetidine, -pyrrolidine, and -piperidine derivatives, use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds, and a method of treatment employing these compounds and compositions. The compounds show a high and selective binding affinity to the histamine H3 receptor indicating histamine H3 receptor antagonistic, inverse agonistic or agonistic activity. As a result, the compounds are useful for the treatment of diseases and disorders related to the histamine H3 receptor.
    Type: Grant
    Filed: September 12, 2002
    Date of Patent: January 6, 2004
    Assignee: Novo Nordisk A/S
    Inventors: Florencio Zaragoza Dorwald, Rolf Hohlweg
  • Cyclopropanecarboxylic acid amide compound and pharmaceutical use thereof
    Publication number: 20040002521
    Abstract: The present invention provides an NF-kappa B activation inhibitor, an inflammatory cytokine production inhibitor, a matrix metalloprotease production inhibitor, an inflammatory cell adhesion factor expression inhibitor, and an anti-inflammatory agent, an antirheumatic agent, an immuno-suppressive agent, an antiallergic agent, an antiviral agent, or a therapeutic agent for arteriosclerosis, which comprise, as the active ingredient, a cyclopropanecarboxylic acid amide compound or a pharmaceutically acceptable salt thereof effective for the treatment of inflammatory diseases.
    Type: Application
    Filed: April 30, 2003
    Publication date: January 1, 2004
    Applicant: AJINOMOTO CO. INC
    Inventors: Yukio Iino, Takashi Yamamoto, Tsuyoshi Kobayashi
  • Neuropeptide Y Y5 receptor antagonists
    Patent number: 6667319
    Abstract: The present invention discloses compounds which, are novel receptor antagonists for NPY Y5 as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such NPY Y5 receptor antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.
    Type: Grant
    Filed: July 24, 2002
    Date of Patent: December 23, 2003
    Assignee: Schering-Plough Corporation
    Inventors: Andrew W. Stamford, Ying Huang, Guoqing Li
  • 1,4-Benzofused urea compounds useful in treating cytokine mediated diseases
    Publication number: 20030232865
    Abstract: Disclosed are 1,4-disubstituted benzo-fused urea compounds of formula (I): 1
    Type: Application
    Filed: February 19, 2003
    Publication date: December 18, 2003
    Applicant: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Pier Francesco Cirillo, Abdelhakim Hammach, John Robinson Regan
  • Sulfonamide derivatives
    Publication number: 20030229102
    Abstract: The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof which is useful for the treatment of conditions associated with glutamate hypofunction, such as psychiatric and neurological disorders 1
    Type: Application
    Filed: November 15, 2002
    Publication date: December 11, 2003
    Inventors: James Allen Knobelsdorf, Timothy Alan Shepherd, Eric George Tromiczak, Hamideh Zarrinmayeh, Dennis Michael Zimmerman
  • Compounds useful as anti-inflammatory agents
    Patent number: 6660732
    Abstract: Disclosed are novel aromatic compounds which are useful for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are pharmaceutical compositions containing and processes of making such compounds.
    Type: Grant
    Filed: September 25, 2001
    Date of Patent: December 9, 2003
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Rajashehar Betageri, Steffen Breitfelder, Pier F. Cirillo, Thomas A. Gilmore, Eugene R. Hickey, Thomas M. Kirrane, Monica H. Moriak, Neil Moss, Usha R. Patel, John R. Proudfoot, John R. Regan, Rajiv Sharma, Sanxing Sun, Alan D. Swinamer, Hidenori Takahashi
  • Compounds useful as anti-inflammatory agents
    Patent number: 6656933
    Abstract: Disclosed are novel aromatic compounds which are useful for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are pharmaceutical compositions containing and processes of making such compounds.
    Type: Grant
    Filed: September 25, 2001
    Date of Patent: December 2, 2003
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventor: Eugene R. Hickey
  • Combination of hypertensin converting enzyme inhibitor with a diuretic for treating microcirculation disorders
    Patent number: 6653336
    Abstract: The present invention relates to the use of a combination of an antiotensin-converting enzyme inhibitor (CEI) and of a diuretic for the treatment of arteriolo-capillary microcirculatory disorders and to pharmaceutical compositions containing the same.
    Type: Grant
    Filed: May 18, 2000
    Date of Patent: November 25, 2003
    Assignee: Les Laboratoires Servier
    Inventors: David Guez, Pierre Schiavi, Bernard Levy
  • Succinate derivative compounds useful as cysteine protease inhibitors
    Patent number: 6649642
    Abstract: Disclosed are novel succinate derivative compounds of the formula(I)/(Ia): wherein R1, R2, R3, R4, R5, R6, R7, X and A are defined herein. The compounds are useful as inhibitors of cysteine proteases. Also disclosed are methods of using and methods of making such compounds.
    Type: Grant
    Filed: October 23, 2002
    Date of Patent: November 18, 2003
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Younes Bekkali, Eugene Richard Hickey, Weimin Liu, David S. Thomson
  • Cyclylamine sulfonamides as &bgr;3-adrenergic receptor agonists
    Patent number: 6649603
    Abstract: This invention provides compounds of Formula I having the structure wherein R1, R2, R3, W, X, and Z are as defined hereinbefore or a pharmaceutically acceptable salt thereof, which are useful in treating metabolic disorders related to insulin resistance or hyperglycemia.
    Type: Grant
    Filed: September 5, 2002
    Date of Patent: November 18, 2003
    Assignee: Wyeth
    Inventor: Fuk-Wah Sum
  • Acetylenic alpha-amino acid-based sulfonamide hydroxamic acid tace inhibitors
    Publication number: 20030212049
    Abstract: Compounds of the formula: 1
    Type: Application
    Filed: February 27, 2003
    Publication date: November 13, 2003
    Applicant: Wyeth
    Inventors: Jeremy I. Levin, James Ming Chen, Derek C. Cole, Mila T. Du, Leif M. Laakso
  • Aryl ureas with angiogenisis inhibiting activity
    Publication number: 20030207870
    Abstract: This invention relates to methods of using aryl ureas to treat diseases mediated by the VEGF induced signal transduction pathway characterized by abnormal angiogenesis or hyperpermeability processes.
    Type: Application
    Filed: February 11, 2003
    Publication date: November 6, 2003
    Applicant: BAYER CORPORATION
    Inventors: Jacques Dumas, William J. Scott, James Elting, Holia Hatoum-Makdad
  • Aminoguanidines and alkoxyguanidines as protease inhibitors
    Patent number: 6638931
    Abstract: Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: wherein X is O or NR9 and R1-R4, R6-R9, R11, R12, Ra, Rb, Rc, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity.
    Type: Grant
    Filed: November 28, 2000
    Date of Patent: October 28, 2003
    Assignee: 3-Dimensional Pharmaceuticals, Inc.
    Inventors: Bruce E. Tomczuk, Richard M. Soll, Tianbao Lu, Cynthia L. Fedde, Carl R. Illig, Thomas P. Markotan, Thomas P. Stagnaro
  • Compounds exhibiting thrombopoietin receptor agonism
    Publication number: 20030195231
    Abstract: Pharmaceutical compositions containing as an active ingredient compounds of the general formula (I), prodrugs of the same, pharmaceutically acceptable salts of both, or solvates of them and exhibiting thrombopoietin receptor agonism:
    Type: Application
    Filed: July 2, 2002
    Publication date: October 16, 2003
    Inventors: Hiroshi Takemoto, Takeshi Shiota, Masami Takayama
  • Substituted piperidines
    Publication number: 20030186963
    Abstract: A novel class of substituted piperidines, pharmaceutical compositions comprising them and use thereof in the treatment and/or prevention of diseases and disorders related to the histamine H3 receptor. More particularly, the compounds are useful for the treatment and/or prevention of diseases and disorders in which an interaction with the histamine H3 receptor is beneficial.
    Type: Application
    Filed: September 12, 2002
    Publication date: October 2, 2003
    Inventor: Florencio Zaragoza Dorwald
  • Substituted aza-oxindole derivatives
    Patent number: 6624171
    Abstract: Substituted aza-oxindole derivatives useful as cyclin dependent kinase 11 inhibitors, for preventing/reducing the severity of epithelial cytotoxicity side-effects (e.g., alopecia, plantar-palmar syndrome, mucositis) induced by chemoptherapy and/or radiation therapy in a patient receiving such therapy.
    Type: Grant
    Filed: August 28, 2001
    Date of Patent: September 23, 2003
    Assignee: SmithKline Beecham Corporation
    Inventors: Philip Anthony Harris, Lee Frederick Kuyper, Karen Elizabeth Lackey, James Marvin Veal
  • 1,3-disubstituted and 1,3,3-trisubstituted pyrrolidines as histamine-3 receptor ligands and their therapeutic applications
    Patent number: 6620839
    Abstract: Compounds of formula I are useful in treating diseases or conditions prevented by or ameliorated with histamine-3 receptor ligands. Also disclosed are histamine-3 receptor ligand compositions and methods of antagonizing or agonizing histamine-3 receptors.
    Type: Grant
    Filed: January 11, 2002
    Date of Patent: September 16, 2003
    Assignee: Abbott Laboratories
    Inventors: Yousseff L. Bennani, Ramin Faghih, Wesley J. Dwight, Anil Vasudevan, Scott E. Conner
  • Novel 2-nitromethylidene/2-cyanimino/2-nitro-imino-pyrrolidines and piperidines, intermediates, and their use as pesticides
    Publication number: 20030166635
    Abstract: Compounds of formula 1
    Type: Application
    Filed: January 13, 2003
    Publication date: September 4, 2003
    Inventors: Peter Maienfisch, Jozef Gonda, Olivier Jacob, Laurenz Gsell
  • Fructosamine oxidase: antagonists and inhibitors
    Patent number: 6610693
    Abstract: The present invention relates to methods of treating an individual with diabetes mellitus by administering to said individual an effective amount of copper chelators, hydrazine compounds, and/or substrate analogues. The invention also relates to methods of treating an individual with diabetes mellitus by lessening fructosamine odixase activity in said individual. Provided within is disclosure pertaining to treatment, pharmaceutical compositions, dosage ranges, and uses of fructosamine oxidase enzyme inhibitors to lessen fructosamine oxidase activity.
    Type: Grant
    Filed: October 10, 2001
    Date of Patent: August 26, 2003
    Assignee: Protemix Corporation Limited
    Inventor: John Richard Baker
  • Alpha-and beta-amino acid hydroxyethylamino sulfamic acid derivatives useful as retroviral protease inhibitors
    Publication number: 20030158236
    Abstract: Certain Alpha- and Beta-amino acid hydroxyethylamino sulfamic acid derivatives represented by the following formula are useful as retroviral protease inhibitors: 1
    Type: Application
    Filed: June 25, 2002
    Publication date: August 21, 2003
    Applicant: G.D. Searle & Co.
    Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Eric T. Sun
  • Benzylcycloalkyl amines as modulators of chemokine receptor activity
    Patent number: 6608227
    Abstract: The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of inflammatory diseases such as asthma and other allergic diseases.
    Type: Grant
    Filed: October 13, 2000
    Date of Patent: August 19, 2003
    Assignee: Bristol-Myers Squibb Pharma
    Inventors: Dean A Wacker, John V Duncia, Joseph B Santella, III, Daniel S Gardner
  • Nitroxides as protectors against oxidatives stress
    Patent number: 6605619
    Abstract: The instant invention is directed to the use of a biologically compatible composition, containing an effective amount of a metal-independent nitroxide compound which is preferably represented by the formula wherein R1 is —CH3; R2 is —C2H5, —C3H7, —C4H9, —C5H11, —C6H13, —CH2—CH(CH3)2, —CHCH3C2H5, or —(CH2)7—CH3, or wherein R1 and R2 together form spirocyclopentane, spirocyclohexane, spirocycloheptane, spirocyclooctane, 5-cholestane, or norbornane, R3 is —O. or —OH, or a physiologically acceptable salt thereof, and a pharmaceutically acceptable carrier, as antioxidants capable of protecting cells, tissues, organs, and whole organisms against the deleterious effects of harmful free radical species generated during oxidative stress.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: August 12, 2003
    Assignee: The United States of America as represented by the Secretary of the Department of Health and Human Services
    Inventors: James B. Mitchell, Amran Samuni, William G. Degraff, Stephen Hahn
  • alpha- and beta-amino acid hydroxyethylamino sulfonyl urea derivatives useful as retroviral protease inhibitors
    Publication number: 20030144342
    Abstract: &agr;-and &bgr;-amino acid hydroxyethylamino sulfonyl urea derivative compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Application
    Filed: May 6, 2002
    Publication date: July 31, 2003
    Applicant: G.D. Searle & Co.
    Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Eric T. Sun
  • Novel aminoazetidine,-pyrrolidine and -piperidine derivatives
    Publication number: 20030130253
    Abstract: Novel aminoazetidine, -pyrrolidine, and -piperidine derivatives, use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds, and a method of treatment employing these compounds and compositions. The compounds show a high and selective binding affinity to the histamine H3 receptor indicating histamine H3 receptor antagonistic, inverse agonistic or agonistic activity. As a result, the compounds are useful for the treatment of diseases and disorders related to the histamine H3 receptor.
    Type: Application
    Filed: September 12, 2002
    Publication date: July 10, 2003
    Inventors: Florencio Zaragoza Dorwald, Rolf Hohlweg
  • Substituted N-heteroaryl-N-phenyl aminoalcohol compounds useful for inhibiting cholesteryl ester transfer protein activity
    Patent number: 6586433
    Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N-heteroaryl-N-phenyl aminoalcohols.
    Type: Grant
    Filed: November 14, 2001
    Date of Patent: July 1, 2003
    Assignee: Pharmacia Corporation
    Inventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel