Chalcogen Bonded Directly To Ring Carbon Of The Six-membered Hetero Ring Patents (Class 546/24)
  • Publication number: 20110059922
    Abstract: The inventions disclosed include methods of treating cancers and related neoplasias, especially prostate cancer, with pharmaceutically acceptable salts comprising lipophilic cation moieties linked to nitroxide or linked to hydroxylamine anti-oxidant groups.
    Type: Application
    Filed: September 4, 2009
    Publication date: March 10, 2011
    Applicants: COLBY PHARMACEUTICAL COMPANY, MEDICAL COLLEGE OF WISCONSIN, INC.
    Inventors: David A. Zarling, Hirak S. Basu, Balaraman Kalyanaraman, Joy Joseph
  • Publication number: 20110034416
    Abstract: Disclosed are compounds of Formula (I): and salts thereof. Also, disclosed are methods of using the compounds in the treatment of proliferative diseases, such as cancer, and to pharmaceutical compositions comprising at least one compound of Formula (I) or a pharmaceutically acceptable salt.
    Type: Application
    Filed: January 22, 2009
    Publication date: February 10, 2011
    Inventors: Robert M. Borzilleri, Zhen-Wei Cai
  • Publication number: 20100316676
    Abstract: Bisphosphonate compounds and related methods of making and using are disclosed, including pyridinium-1-yl, quinolinium-1-yl, and related compounds. The activity of compounds is disclosed in the context of functional assays such as Leishmania major farnesyl diphosphate synthase (FPPS) inhibition, Dictyostelium discoideum growth inhibition, human gamma delta T cell activation, and bone resorption. The applicability of bisphosphonate compounds in the context of parasitic infections, for example against trypanosomes, is disclosed. Further potential applications of the invention are disclosed regarding the treatment of one or more conditions such as bone resorption disorders, cancer, bone pain, infectious diseases, and in immunotherapy.
    Type: Application
    Filed: June 28, 2010
    Publication date: December 16, 2010
    Inventors: John M. Sanders, Yongcheng Song, Julian M.W. Chan, Eric Oldfield, Yonghui Zhang
  • Publication number: 20100317860
    Abstract: Disclosed are crystals of the compound represented by Formula (1), which has A?-production-reducing effects and is a prodrug of compounds effective in treating neural degenerative diseases of which A? is the cause, for example, diseases such as Alzheimer's disease, Down syndrome, etc., and salts thereof or crystals of salts thereof. These are particularly useful as stock for pharmaceutical products.
    Type: Application
    Filed: January 26, 2009
    Publication date: December 16, 2010
    Inventors: Ikuo Kushida, Nobuaki Sato, Yoshiaki Sato
  • Publication number: 20100279983
    Abstract: This invention provides novel ?-lactamase inhibitors of the aryl- and heteroarylsulfonamidomethylphosphonate monoester class having nitrogen-based cations or quarternary ammonium groups. The compounds inhibit three classes of ?-lactamases and synergize the antibacterial effects of ?-lactam antibiotics (e.g., imipenem and ceftazidime) against those micro-organisms normally resistant to the ?-lactam antibiotics as a result of the presence of the ?-lactamases. Formula (I) or pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: May 21, 2007
    Publication date: November 4, 2010
    Inventors: Frank Dininno, Milton L. Hammond, Kevin Dykstra, Seongkon Kim, Qiang Tan, Katherine Young, Jeffrey Donald Hermes, Helen Chen, Stephane Raeppel, Michael Mannion, Frederic Gaudette, Arkadii Vaisburg, Jubrail Rahil, Nafsika Georgopapadakou, Nancy Z. Zhou
  • Publication number: 20100197635
    Abstract: This invention relates to treatment of Tardive Dyskinesia through the administration of pyridoxal 5?-phosphate. The treatment may be an oral administration of 100-4000 mg/day, for example, 100-750 mg/day or about 250 mg/day. Also provided is the use of pyridoxal 5?-phosphate for the preparation of a medicament for the treatment of tardive dyskinesia, kits comprising pyridoxal 5?-phosphate for the treatment of tardive dyskinesia, and combination drugs for the treatment of tardive dyskinesia.
    Type: Application
    Filed: May 28, 2008
    Publication date: August 5, 2010
    Inventors: Albert Friesen, Dawson James Reimer
  • Patent number: 7763186
    Abstract: Substantially pure ionic liquids and ionic liquid precursors were prepared. The substantially pure ionic liquid precursors were used to prepare substantially pure ionic liquids.
    Type: Grant
    Filed: December 22, 2006
    Date of Patent: July 27, 2010
    Assignee: Los Alamos National Security, LLC
    Inventors: Anthony K. Burrell, Benjamin P. Warner, T. Mark McCleskey, Anoop Agrawal
  • Publication number: 20100016258
    Abstract: The present invention provides ?-hydroxy phosphonate compounds that are autotaxin inhibitors.
    Type: Application
    Filed: January 9, 2009
    Publication date: January 21, 2010
    Inventors: Kevin R. Lynch, Timothy L. Macdonald
  • Publication number: 20090197835
    Abstract: The present invention provides LPA analogs that are antagonists at the LPA receptors.
    Type: Application
    Filed: January 22, 2009
    Publication date: August 6, 2009
    Inventors: Karen M. Carter, Kevin R. Lynch, Timothy L. Macdonald
  • Publication number: 20090197834
    Abstract: [Problem] To provide a compound having excellent platelet aggregation inhibitory activity. [Means for Resolution] It was found that quinolone derivatives characterized in that these have lower alkyl, cycloalkyl or the like at the 1-position; —N(R0)C(O)-lower alkylene-CO2R0, lower alkylene-CO2R0, lower alkenylene-CO2R0, —O-lower alkylene-CO2R0, —O-(lower alkylene which may be substituted with —CO2R0)-aryl or —O-lower alkenylene-CO2R0 (wherein R0 is H or lower alkyl) at the 3-position; halogen at the 6-position; and amino group substituted with a substituent group having a ring structure at the 7-position, respectively, or pharmaceutically acceptable salts thereof, has excellent P2Y12 inhibitory activity. In addition, it was confirmed that these quinolone derivatives also have excellent platelet aggregation inhibitory activity. Based on the above, these quinolone derivatives or pharmaceutically acceptable salts thereof are useful as platelet aggregation inhibitors.
    Type: Application
    Filed: March 14, 2007
    Publication date: August 6, 2009
    Applicant: ASTELLAS PHARMA INC.
    Inventors: Yuji Koga, Takao Okuda, Susumu Watanuki, Takashi Kamikubo, Fukushi Hirayama, Hiroyuki Moritomo, Jiro Fujiyasu, Michihito Kageyama, Toshio Uemura, Jun Takasaki
  • Publication number: 20090137529
    Abstract: The compounds of the present invention are prodrugs of modulators of the Cannabinoid-1 (CB 1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the Cannabinoid-1 (CB 1) receptor. In particular, compounds of the present invention are 5 prodrugs of antagonists or inverse agonists of the CB 1 receptor. The invention is concerned with the use of these compounds to be converted to compounds that modulate the Cannabinoid-1 (CB 1) receptor. As such, the compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, Alzheimer's disease, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-10 Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, movement disorders, and schizophrenia.
    Type: Application
    Filed: May 11, 2007
    Publication date: May 28, 2009
    Inventors: William K. Hagmann, Milton L. Hammond
  • Patent number: 7498319
    Abstract: The present invention relates to phosphinic acid derivatives as GABAB antagonists, their preparation, their use as pharmaceuticals and pharmaceutical compositions containing them.
    Type: Grant
    Filed: November 19, 2004
    Date of Patent: March 3, 2009
    Assignee: Novartis AG
    Inventor: Wolfgang Froestl
  • Patent number: 7494983
    Abstract: This invention relates to potent potassium channel blocker compounds of structural Formula I or a formulation thereof for the treatment of glaucoma and other conditions which leads to elevated intraoccular pressure in the eye of a patient. This invention also relates to the use of such compounds to provide a neuroprotective effect to the eye of mammalian species, particularly humans.
    Type: Grant
    Filed: August 31, 2004
    Date of Patent: February 24, 2009
    Assignee: Merck & Co. Inc.
    Inventors: Meng Hsin Chen, James B. Doherty, Luping Liu, Swaminathan Natarajan, Robert M. Tynebor
  • Publication number: 20090048213
    Abstract: The present invention provides a most suitable prodrug of a cinnamide compound. The prodrug is represented by Formula (I) wherein Ra and Rb each denote a C1-6 alkyl group or the like; Xa denotes a methoxy group or a fluorine atom; Y denotes a phosphono group or the like; and A denotes a cyclic lactam derivative.
    Type: Application
    Filed: July 25, 2007
    Publication date: February 19, 2009
    Inventors: Teiji Kimura, Koki Kawano, Noritaka Kitazawa, Nobuaki Sato, Toshihiko Kaneko, Koichi Ito, Mamoru Takaishi, Ikuo Kushida
  • Patent number: 7358361
    Abstract: Bisphosphonate compounds and related methods of making and using are disclosed, including pyridinium-1-yl, quinolinium-1-yl, and related compounds. The activity of compounds is disclosed in the context of functional assays such as Leishmania major farnesyl diphosphate synthase (FPPS) inhibition, Dictyostelium discoideum growth inhibition, human gamma delta T cell activation, and bone resorption. The applicability of bisphosphonate compounds in the context of parasitic infections, for example against trypanosomes, is disclosed. Further potential applications of the invention are disclosed regarding the treatment of one or more conditions such as bone resorption disorders, cancer, bone pain, infectious diseases, and in immunotherapy.
    Type: Grant
    Filed: October 7, 2005
    Date of Patent: April 15, 2008
    Assignee: The Board of Trustees of the University of Illinois
    Inventors: John M. Sanders, Yongcheng Song, Julian M. W. Chan, Eric Oldfield, Yonghui Zhang
  • Patent number: 7320993
    Abstract: The invention relates to new pyridylalkane, alkene, and alkine acid amides substituted with an aryl and/or heteroaryl residue according to the general formula (I), with a saturated or one or several-fold unsaturated hydrocarbon residue in the carboxylic acid group, methods for the synthesis of these compounds, medicaments containing these and their production as well as their therapeutic use, especially as cytostatic agents and immunosuppressive agents, for example in the treatment or prevention of various types of tumors and control of immune reactions such as autoimmune diseases.
    Type: Grant
    Filed: June 16, 2000
    Date of Patent: January 22, 2008
    Assignee: Astellas Deutschland GmbH
    Inventors: Elfi Biedermann, Max Hasmann, Roland Löser, Benno Rattel, Friedemann Reiter, Barbara Schein, Klaus Seibel, Klaus Vogt, Katja Wosikowski, Isabel Schemainda
  • Patent number: 7312326
    Abstract: Fluorescent labeled reporter compounds having a modified cyanine dye that is coupled to a nucleotide derivative through a linker are disclosed. The compounds are useful for nucleic acid sequence analysis. The fluorescent labeled reporter compounds are ring-locked cyanine dyes that are coupled to a nucleotide derivative, such as a modified DNA base, through a linker. These fluorescent labeled reporter compounds can be used as DNA chain-terminators in DNA synthesis to generate DNA fragments that are fluorescently-labeled at the 3?-terminal end of the DNA fragment.
    Type: Grant
    Filed: April 9, 2004
    Date of Patent: December 25, 2007
    Assignee: Beckman Coulter, Inc.
    Inventors: Gene G.-Y. Shen, Yuan Lin, Josephine M. Michael
  • Patent number: 7129228
    Abstract: One aspect of the present invention relates to novel heterocyclic compounds. A second aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for various cellular receptors, including opiate receptors, other G-protein-coupled receptors, and ion channels. An additional aspect of the present invention relates to the use of the novel heterocyclic compounds as analgesics.
    Type: Grant
    Filed: January 7, 2004
    Date of Patent: October 31, 2006
    Assignee: Sepracor Inc.
    Inventors: Gregory D. Cuny, Liming Shao, James R. Hauske, Michele L. R. Heffernan, Brian M. Aquila, Xinhe Wu, Fengjiang Wang, Thomas D. Bannister
  • Patent number: 7105556
    Abstract: Compounds are provided which have the structure wherein Q is C or N, X1 is C or N, and R1, R2, R2a, R2b, R2c, R3, Y, A, m, n, X2, X3 and X4 are as defined herein, which compounds are useful as antidiabetic, hypolipidemic, and antiobesity agents.
    Type: Grant
    Filed: May 22, 2002
    Date of Patent: September 12, 2006
    Assignee: Bristol-Myers Squibb Company
    Inventors: Peter T. Cheng, Yoon Jeon, Wei Wang
  • Patent number: 7030103
    Abstract: The intention relates to bacterial antibiotic resistance and, in particular, to compositions and methods for overcoming bacterial antibiotic resistance. The invention provides novel ?-lactamase inhibitors, which are structurally unrelated to the natural product and semi-synthetic ?-lactamase inhibitors presently available, and which do not require a ?-lactam pharmacophore. The invention also provides pharmaceutical compositions and methods for inhibiting bacterial growth.
    Type: Grant
    Filed: October 8, 2002
    Date of Patent: April 18, 2006
    Assignee: Methylgene, Inc.
    Inventors: Jeffrey M. Besterman, Daniel Delorme, Jubrail Rahil
  • Patent number: 6977260
    Abstract: The present invention provides a method of treating ocular hypertension or glaucoma which comprises administering to an animal having ocular hypertension or glaucoma therapeutically effective amount of a compound represented by the general formula I; wherein X, Y, Z, D and R3 are as defined in the specification.
    Type: Grant
    Filed: January 22, 2004
    Date of Patent: December 20, 2005
    Assignee: Allergan, Inc.
    Inventors: David W. Old, Danny T. Dinh
  • Patent number: 6921756
    Abstract: The invention relates to bacterial antibiotic resistance and, in particular, to compositions and methods for overcoming bacterial antibiotic resistance. The invention provides novel ?-lactamase inhibitors, which are structurally unrelated to the natural product and semi-synthetic ?-lactamase inhibitors presently available, and which do not require a ?-lactam pharmacophore. The invention also provides pharmaceutical compositions and methods for inhibiting bacterial growth.
    Type: Grant
    Filed: April 8, 2003
    Date of Patent: July 26, 2005
    Assignee: MethylGene, Inc.
    Inventors: Jeffrey M. Besterman, Jubrail Rahil, Arkadii Vaisburg
  • Patent number: 6896871
    Abstract: The present invention is directed to particular bisphosphonate compounds, and in particular, to bisphosphonate conjugates that are useful in the treatment of soft tissues surrounding bone and bone-related diseases, such as bone cancer and osteoporosis.
    Type: Grant
    Filed: April 10, 2001
    Date of Patent: May 24, 2005
    Assignee: MBC Research, Inc.
    Inventors: Alexander Karpeisky, Nelly Padioukova, Sergey Mikhailov, H.B.F. Dixon, Grigorii Tzeitline, Marat Karpeisky
  • Patent number: 6884791
    Abstract: The intention relates to bacterial antibiotic resistance and, in particular, to compositions and methods for overcoming bacterial antibiotic resistance. The invention provides novel ?-lactamase inhibitors, which are structurally unrelated to the natural product and semi-synthetic ?-lactamase inhibitors presently available, and which do not require a ?-lactam pharmacophore. The invention also provides pharmaceutical compositions and methods for inhibiting bacterial growth.
    Type: Grant
    Filed: November 22, 2002
    Date of Patent: April 26, 2005
    Assignee: MethylGene, Inc.
    Inventors: Jeffrey M. Besterman, Jubrail Rahil, Arkadii Vaisburg
  • Patent number: 6872711
    Abstract: The present invention relates to novel ?-substituted-?-aminoethylphosphonate derivatives and their uses for lowering plasma levels of apo (a), Lp(a), apo B, apo B associated lipoproteins (low density lipoproteins and very low density lipoproteins) and for lowering plasma levels of total cholesterol.
    Type: Grant
    Filed: October 22, 2001
    Date of Patent: March 29, 2005
    Assignee: Ilex Oncology Research S.A.
    Inventors: Hieu Trung Phan, Lan Mong Nguyen, Vinh Van Diep, Raymond Azoulay, Eric Joseph Niesor, Craig Leigh Bentzen, Robert John Ife
  • Publication number: 20040220408
    Abstract: Compounds according to formula (I) 1
    Type: Application
    Filed: December 16, 2003
    Publication date: November 4, 2004
    Inventor: Fredrik Bjorkling
  • Publication number: 20040186078
    Abstract: The present invention is directed to substituted N′-(arylcarbonyl)-benzhydrazides, N′-(arylcarbonyl)-benzylidene-hydrazides and analogs thereof, represented by the Formulae I and II: 1
    Type: Application
    Filed: April 5, 2004
    Publication date: September 23, 2004
    Inventors: Sui Xiong Cai, Shailaja Kasibhatla, John Drewe, P. Sanjeeva Reddy, Han-Zhong Zhang
  • Patent number: 6750340
    Abstract: The present invention is directed to particular bisphosphonate compounds, and in particular, to bisphosphonate conjugates that are useful in the treatment of soft tissues surrounding bone and bone-related diseases, such as bone cancer and osteoporosis.
    Type: Grant
    Filed: December 7, 2000
    Date of Patent: June 15, 2004
    Assignee: MBC Research, Inc.
    Inventors: Nelly Padioukova, Sergey Mikhailov, H. B. F. Dixon, Grigorii Tzeitline
  • Patent number: 6747037
    Abstract: The present invention provides a method of treating ocular hypertension or glaucoma which comprises administering to an animal having ocular hypertension or glaucoma therapeutically effective amount of a compound represented by the general formula I; wherein X, Y, Z, D and R3 are as defined in the specification.
    Type: Grant
    Filed: June 6, 2003
    Date of Patent: June 8, 2004
    Assignee: Allergan, Inc.
    Inventors: David W. Old, Thang D. Dinh
  • Patent number: 6727361
    Abstract: New ligands, compositions, metal-ligand complexes and arrays with pyridyl-amine ligands are disclosed that catalyze the polymerization of monomers into polymers. Certain of these catalysts with hafnium metal centers have high performance characteristics, including higher comonomer incorporation into ethylene/olefin copolymers, where such olefins are for example, 1-octene, isobutylene or styrene. Certain of the catalysts are particularly effective at polymerizing propylene to high molecular weight isotactic polypropylene in a solution process at a variety of polymerization conditions.
    Type: Grant
    Filed: November 6, 2001
    Date of Patent: April 27, 2004
    Assignee: Symyx Technologies, Inc.
    Inventors: Anne M. LaPointe, Eric D. Carlson, Thomas Crevier
  • Patent number: 6723711
    Abstract: A compound of the structure A method for the inhibition of the binding of &agr;4&bgr;1 integrin to its receptors, for example VCAM-1(vascular cell adhesion molecule-1) and fibronectin; pharmaceutically active compositions comprising these compounds; and the use of these compounds for the control or prevention of diseases states in which &agr;4&bgr;1 is involved are also disclosed.
    Type: Grant
    Filed: October 9, 2001
    Date of Patent: April 20, 2004
    Assignee: Texas Biotechnology Corporation
    Inventors: Ronald J. Biediger, Brian Dupre, Linda K. Hamaker, George W. Holland, Jamal M. Kassir, Wen Li, Robert V. Market, Noel Nguyen, Ian L. Scott, Chengde Wu, E. Radford Decker
  • Patent number: 6703507
    Abstract: The invention relates to novel ionic liquids and to the production and use thereof. The novel ionic liquids are salts of sulphonated or carboxylated triesters of phosphorous acid as the anionic component and ammonium ions, which can be substituted with organic radicals, as the cationic component.
    Type: Grant
    Filed: October 16, 2001
    Date of Patent: March 9, 2004
    Assignee: Celanese Chemicals Europe GmbH
    Inventors: Helmut Bahrmann, Hans Bohnen
  • Patent number: 6667315
    Abstract: The present invention provides for pyridoxine phosphonate analogues such as, for example, ((2-methyl-3-hydroxy-4-hydroxymethyl-5-pyridyl)alkylphosphonates, and (2-methyl-3-hydroxy-4-hydroxymethyl-5-pyridyl)azaalkylphosphonates) and to pyridoxine malonate analogues, such as, for example, ((2-methyl-3-hydroxy-4-hydroxymethyl-5-pyridylmethyl)malonates), pharmaceutical compositions, and methods for treatment of cardiovascular and related diseases, and diabetes mellitus and related diseases.
    Type: Grant
    Filed: October 28, 2002
    Date of Patent: December 23, 2003
    Assignee: Medicure International Inc.
    Inventor: Wasimul Haque
  • Patent number: 6660860
    Abstract: The invention relates to a process for the selective oxidation of alcohols to ketones or to aldehydes by means of an alkali hypohalite under alkaline conditions, which comprises carrying out the oxidation in the presence of a heterogeneous oxidation catalyst that is insoluble in the reaction medium and is selected from the group comprising the compounds of formula (I) wherein n is a number from 3 to 3000; or a 4-oxy-2,2,6,6-tetramethylpiperidin-1-oxyl that is 4-oxy-bound to a Merrifield polymer. The invention relates also to the compounds of formulae (II) and (III) and to the use of the above-mentioned oxidation catalysts for the oxidation of alcohols.
    Type: Grant
    Filed: June 7, 2002
    Date of Patent: December 9, 2003
    Assignee: Ciba Specialty Chemicals Corporation
    Inventors: Reinhard Sommerlade, Hansjörg Grützmacher, Souâd Boulmaâz
  • Patent number: 6653296
    Abstract: Resolved enantiomers of the formula (IA) and (IB) wherein B is a purine or pyrimidine base or aza and/or deaza analogs thereof are useful in antiviral pharmaceutical compositions to treat retroviral infections.
    Type: Grant
    Filed: February 2, 1995
    Date of Patent: November 25, 2003
    Assignees: Institute of Organic Chemistry and Biochemistry of the Academy of Sciences of the Czech Republic, Rega Stichting v.z.w.
    Inventors: Antonin Holy, Hana Dvorakova, Erik Desire Alice De Clercq, Jan Marie Rene Balzarini
  • Publication number: 20030125559
    Abstract: The present invention relates to novel ether compounds, compositions comprising ether compounds, and methods useful for treating and preventing cardiovascular diseases, dyslipidemias, dysproteinemias, and glucose metabolism disorders comprising administering a composition comprising an ether compound. The compounds, compositions, and methods of the invention are also useful for treating and preventing Alzheimer's Disease, Syndrome X, peroxisome proliferator activated receptor-related disorders, septicemia, thrombotic disorders, obesity, pancreatitis, hypertension, renal disease, cancer, inflammation, and impotence. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.
    Type: Application
    Filed: April 26, 2002
    Publication date: July 3, 2003
    Applicant: Esperion Therapeutics, Inc.
    Inventors: Jean-Louis Henri Dasseux, Carmen Daniela Oniciu
  • Publication number: 20030114678
    Abstract: The present invention provides for pyridoxine phosphonate analogues such as, for example, ((2-methyl-3-hydroxy-4-hydroxymethyl-5-pyridyl)alkylphosphonates, and (2-methyl-3-hydroxy-4-hydroxymethyl-5-pyridyl)azaalkylphosphonates) and to pyridoxine malonate analogues, such as, for example, ((2-methyl-3-hydroxy-4-hydroxymethyl-5-pyridylmethyl)malonates), pharmaceutical compositions, and methods for treatment of cardiovascular and related diseases, and diabetes mellitus and related diseases.
    Type: Application
    Filed: October 28, 2002
    Publication date: June 19, 2003
    Applicant: Medicure International Inc.
    Inventor: Wasimul Haque
  • Publication number: 20030114677
    Abstract: The present invention provides for pyridoxine phosphonate analogues such as, for example, ((2-methyl-3-hydroxy-4-hydroxymethyl-5-pyridyl)alkylphosphonates, and (2-methyl-3-hydroxy-4-hydroxymethyl-5-pyridyl)azaalkylphosphonates) and to pyridoxine malonate analogues, such as, for example, ((2-methyl-3-hydroxy-4-hydroxymethyl-5-pyridylmethyl)malonates), pharmaceutical compositions, and methods for treatment of cardiovascular and related diseases, and diabetes mellitus and related diseases.
    Type: Application
    Filed: October 28, 2002
    Publication date: June 19, 2003
    Applicant: Medicure International Inc.
    Inventor: Wasimul Haque
  • Patent number: 6576760
    Abstract: Polyamines containing at least two nitrogen atoms monosubstituted with pendant arms capable of coordinating metal cations, or with precursors of such pendant arms, all nitrogen atoms of the polyamines except two being fully substituted and the remaining two bearing one H atom each, are cyclized by reaction with a bridging agent that contains two sites that each bear a reactive group capable of undergoing a nucleophilic attack by one of the two N-H groups on the polyamine. Unlike the prior art, cyclization occurs in preference over polymerization of the polyamine, even in reaction mixtures in which the polyamine is at high concentration. A process is also disclosed whereby linear polyamines in which the terminal amine groups are primary amines are substituted with methylenephosphonate ester groups, with one such substituent on each nitrogen atom of the polyamine.
    Type: Grant
    Filed: January 11, 2001
    Date of Patent: June 10, 2003
    Assignee: Chelator LLC
    Inventors: Harry S. Winchell, Rosa L. Cyjon, Joseph Y. Klein, Elliot D. Simhon, Ofer Klein, Haim Zaklad
  • Patent number: 6509359
    Abstract: A compound having the formula: wherein all variables are as defined in the specification, for use as a neuramninidase inhibitor.
    Type: Grant
    Filed: March 17, 2000
    Date of Patent: January 21, 2003
    Inventors: Wayne J. Brouillette, Venkatram Reddy Atigadda, Ming Luo, Yarlagadda S. Babu
  • Patent number: 6498151
    Abstract: The invention encompasses the novel class of compounds represented by the formula below, which are inhibitors of the PTP-1B enzyme. The invention also encompasses pharmaceutical compositions and methods of treating or preventing PTP-1B mediated diseases, including diabetes.
    Type: Grant
    Filed: March 21, 2001
    Date of Patent: December 24, 2002
    Assignee: Merck Frosst Canada & Co.
    Inventors: Chun Sing Li, Christopher Bayly, Jacques Yves Gauthier, Yves Leblanc, Cheuk Kun Lau, Patrick Roy, Michel Therien, Zhaoyin Wang, Claude Dufresne, Rejean Fortin
  • Patent number: 6498161
    Abstract: The present invention is directed to pyrrolidine compounds of the formula I: (wherein R1, R2, R3, R4, R5, R6 and n are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-5 and/or CCR-3.
    Type: Grant
    Filed: April 4, 2000
    Date of Patent: December 24, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Charles G. Caldwell, Kevin T. Chapman, Jeffrey Hale, Dooseop Kim, Christopher Lynch, Malcolm MacCoss, Sander G. Mills, Christopher Willoughby, Scott Berk, Ronald M. Kim
  • Patent number: 6472406
    Abstract: The intention relates to bacterial antibiotic resistance and, in particular, to compositions and methods for overcoming bacterial antibiotic resistance. The invention provides novel &bgr;-lactamase inhibitors, which are structurally unrelated to the natural product and semi-synthetic &bgr;-lactamase inhibitors presently available, and which do not require a &bgr;-lactam pharmacophore. The invention also provides pharmaceutical compositions and methods for inhibiting bacterial growth.
    Type: Grant
    Filed: July 5, 2000
    Date of Patent: October 29, 2002
    Assignee: MethylGene, Inc.
    Inventors: Jeffrey M. Besterman, Daniel Delorme, Jubrail Rahil
  • Patent number: 6451776
    Abstract: The present invention is directed to novel water-soluble prodrugs of aliphatic or aromatic hindered hydroxyl group containing pharmaceuticals.
    Type: Grant
    Filed: December 8, 2000
    Date of Patent: September 17, 2002
    Assignee: University of Kansas
    Inventors: Valentino J. Stella, Jan J. Zygmunt, Ingrid Gunda Georg, Muhammad S. Safadi
  • Publication number: 20020082423
    Abstract: Aminophosphonates alpha substituted by phenol groups, of formula (I) have lipoprotein(a) lowering activity.
    Type: Application
    Filed: September 4, 2001
    Publication date: June 27, 2002
    Applicant: SmithKline Beecham p.l.c. and Symphar
    Inventors: Lan Mong Nguyen, Hieu Trung Phan, Vinh Van Diep, Simon Floret, Raymond Azoulay, Eric Niesor, Craig Leigh Bentzen, Robert John Ife
  • Patent number: 6407235
    Abstract: The invention is a compound of the formula wherein R is a) —C(O)(CH2)nC(O)OH, b)  wherein R1 is —N(R2)(R3), or is a five or six member aromatic or non-aromatic heterocyclic ring having one or more heteroatoms selected from nitrogen, oxygen or sulfur, unsubstituted or substituted by lower alkyl, c) —P(O)(OH)2, or is d) —C(O)(CH2)nNHC(O)(CH2)nN(R2)(R3); and R2/R3 are hydrogen or lower alkyl; n is 1, 2, 3 or 4; or a pharmaceutically acceptable acid addition salt thereof
    Type: Grant
    Filed: August 16, 2001
    Date of Patent: June 18, 2002
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Alexander Alanine, Bernd Buettelmann, Holger Fischer, Marie-Paule Heitz Neidhart, Joerg Huwyler, Georg Jaeschke, Emmanuel Pinard, René Wyler
  • Patent number: 6391895
    Abstract: Chelating agents, in particular dipyridoxyl and aminopolycarboxylic acid based chelating agents, and their metal chelates, when linked directly or indirectly to at least one nitric oxide releasing moiety, or when use in combination with nitric oxide or a nitric oxide releasing moiety have been found to be effective in treating a variety of disorders. In particular, such compounds may be used in treating conditions associated with the presence of free radicals in the body, e.g. reperfusion injuries, and in reducing the cardiotoxicity of anti-tumor agents, e.g. anthracyclines and/or paclitaxel.
    Type: Grant
    Filed: June 23, 2000
    Date of Patent: May 21, 2002
    Assignee: Amersham Health AS
    Inventors: Robertson Towart, Jan Olof Gustav Karlsson, Lars Goran Wistrand, Hakan Malmgren
  • Publication number: 20020042398
    Abstract: The present application describes novel lactams and derivatives thereof of formula I: 1
    Type: Application
    Filed: July 10, 2001
    Publication date: April 11, 2002
    Inventors: Thomas P. Maduskuie, Jingwu Duan, Stephen E. Mercer
  • Publication number: 20020040037
    Abstract: The invention is a compound of the formula 1
    Type: Application
    Filed: August 16, 2001
    Publication date: April 4, 2002
    Inventors: Alexander Alanine, Bernd Buettelmann, Holger Fischer, Marie-Paule Heitz Neidhart, Joerg Huwyler, Georg Jaeschke, Emmanuel Pinard, Rene Wyler
  • Publication number: 20020035259
    Abstract: The present invention provides novel 2-methoxyimino-2-(pyridinyloxymethyl)phenyl acetamide compounds with (derivatised) hydroxyalkyl substituents on the pyridine ring, their use as fungicidal compounds, and their use in fungicidal compositions comprising at least one of the 2-methoxyimino-2-(pyridinyloxymethyl)phenyl acetamide compounds as the active ingredient.
    Type: Application
    Filed: August 30, 2001
    Publication date: March 21, 2002
    Inventors: Emily J. Canada, Christopher S. Galka, Robert P. Gajewski, Neil V. Kirby, Irene M. Morrison, Mary E. Pieczko, Chrislyn M. Carson, Jeannie R. Phillips, Brent J. Rieder, Zhengyu Huang