Chalcogen Bonded Directly To Ring Carbon Of The Six-membered Hetero Ring Patents (Class 546/24)
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Publication number: 20110104110Abstract: The present invention relates to Substituted Indole Derivatives, compositions comprising at least one Substituted Indole Derivative, and methods of using these Substituted Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.Type: ApplicationFiled: August 27, 2008Publication date: May 5, 2011Inventors: Gopinadhan N. Anikumar, Frank Bennett, Tin-Yau Chan, Kevin X. Chen, Mousumi Sannigrahi, Francisco Velazquez, Srikanth Venkatraman, Qingbei Zeng, Jose S. Duca, Charles A. Lesburg, Joseph A. Kozlowski, F. George Njoroge, Stuart B. Rosenblum, Neng-Yang Shih
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Publication number: 20110082113Abstract: The present application describes prodrugs of the compound of formula (I): or stereoisomers or pharmaceutically acceptable salts thereof. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis using the prodrug compounds of the invention are disclosed.Type: ApplicationFiled: October 4, 2010Publication date: April 7, 2011Inventors: John Hynes, Percy H. Carter, Lyndon A.M. Cornelius, T.G. Murali Dhar, John V. Duncia, Joseph B. Santella, Hong Wu, Satheesh Nair, Jayakumar S. Warrier
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Publication number: 20110059922Abstract: 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: ApplicationFiled: September 4, 2009Publication date: March 10, 2011Applicants: COLBY PHARMACEUTICAL COMPANY, MEDICAL COLLEGE OF WISCONSIN, INC.Inventors: David A. Zarling, Hirak S. Basu, Balaraman Kalyanaraman, Joy Joseph
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Publication number: 20110034416Abstract: 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: ApplicationFiled: January 22, 2009Publication date: February 10, 2011Inventors: Robert M. Borzilleri, Zhen-Wei Cai
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Publication number: 20100316676Abstract: 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: ApplicationFiled: June 28, 2010Publication date: December 16, 2010Inventors: John M. Sanders, Yongcheng Song, Julian M.W. Chan, Eric Oldfield, Yonghui Zhang
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Publication number: 20100317860Abstract: 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: ApplicationFiled: January 26, 2009Publication date: December 16, 2010Inventors: Ikuo Kushida, Nobuaki Sato, Yoshiaki Sato
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Publication number: 20100279983Abstract: 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: ApplicationFiled: May 21, 2007Publication date: November 4, 2010Inventors: 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
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Publication number: 20100197635Abstract: 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: ApplicationFiled: May 28, 2008Publication date: August 5, 2010Inventors: Albert Friesen, Dawson James Reimer
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Patent number: 7763186Abstract: 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: GrantFiled: December 22, 2006Date of Patent: July 27, 2010Assignee: Los Alamos National Security, LLCInventors: Anthony K. Burrell, Benjamin P. Warner, T. Mark McCleskey, Anoop Agrawal
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Publication number: 20100016258Abstract: The present invention provides ?-hydroxy phosphonate compounds that are autotaxin inhibitors.Type: ApplicationFiled: January 9, 2009Publication date: January 21, 2010Inventors: Kevin R. Lynch, Timothy L. Macdonald
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Publication number: 20090197835Abstract: The present invention provides LPA analogs that are antagonists at the LPA receptors.Type: ApplicationFiled: January 22, 2009Publication date: August 6, 2009Inventors: Karen M. Carter, Kevin R. Lynch, Timothy L. Macdonald
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Publication number: 20090197834Abstract: [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: ApplicationFiled: March 14, 2007Publication date: August 6, 2009Applicant: ASTELLAS PHARMA INC.Inventors: Yuji Koga, Takao Okuda, Susumu Watanuki, Takashi Kamikubo, Fukushi Hirayama, Hiroyuki Moritomo, Jiro Fujiyasu, Michihito Kageyama, Toshio Uemura, Jun Takasaki
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Publication number: 20090137529Abstract: 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: ApplicationFiled: May 11, 2007Publication date: May 28, 2009Inventors: William K. Hagmann, Milton L. Hammond
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Patent number: 7498319Abstract: The present invention relates to phosphinic acid derivatives as GABAB antagonists, their preparation, their use as pharmaceuticals and pharmaceutical compositions containing them.Type: GrantFiled: November 19, 2004Date of Patent: March 3, 2009Assignee: Novartis AGInventor: Wolfgang Froestl
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Patent number: 7494983Abstract: 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: GrantFiled: August 31, 2004Date of Patent: February 24, 2009Assignee: Merck & Co. Inc.Inventors: Meng Hsin Chen, James B. Doherty, Luping Liu, Swaminathan Natarajan, Robert M. Tynebor
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Publication number: 20090048213Abstract: 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: ApplicationFiled: July 25, 2007Publication date: February 19, 2009Inventors: Teiji Kimura, Koki Kawano, Noritaka Kitazawa, Nobuaki Sato, Toshihiko Kaneko, Koichi Ito, Mamoru Takaishi, Ikuo Kushida
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Patent number: 7358361Abstract: 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: GrantFiled: October 7, 2005Date of Patent: April 15, 2008Assignee: The Board of Trustees of the University of IllinoisInventors: John M. Sanders, Yongcheng Song, Julian M. W. Chan, Eric Oldfield, Yonghui Zhang
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Patent number: 7320993Abstract: 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: GrantFiled: June 16, 2000Date of Patent: January 22, 2008Assignee: Astellas Deutschland GmbHInventors: Elfi Biedermann, Max Hasmann, Roland Löser, Benno Rattel, Friedemann Reiter, Barbara Schein, Klaus Seibel, Klaus Vogt, Katja Wosikowski, Isabel Schemainda
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Patent number: 7312326Abstract: 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: GrantFiled: April 9, 2004Date of Patent: December 25, 2007Assignee: Beckman Coulter, Inc.Inventors: Gene G.-Y. Shen, Yuan Lin, Josephine M. Michael
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Patent number: 7129228Abstract: 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: GrantFiled: January 7, 2004Date of Patent: October 31, 2006Assignee: 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
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Patent number: 7105556Abstract: 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: GrantFiled: May 22, 2002Date of Patent: September 12, 2006Assignee: Bristol-Myers Squibb CompanyInventors: Peter T. Cheng, Yoon Jeon, Wei Wang
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Patent number: 7030103Abstract: 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: GrantFiled: October 8, 2002Date of Patent: April 18, 2006Assignee: Methylgene, Inc.Inventors: Jeffrey M. Besterman, Daniel Delorme, Jubrail Rahil
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Patent number: 6977260Abstract: 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: GrantFiled: January 22, 2004Date of Patent: December 20, 2005Assignee: Allergan, Inc.Inventors: David W. Old, Danny T. Dinh
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Patent number: 6921756Abstract: 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: GrantFiled: April 8, 2003Date of Patent: July 26, 2005Assignee: MethylGene, Inc.Inventors: Jeffrey M. Besterman, Jubrail Rahil, Arkadii Vaisburg
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Patent number: 6896871Abstract: 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: GrantFiled: April 10, 2001Date of Patent: May 24, 2005Assignee: MBC Research, Inc.Inventors: Alexander Karpeisky, Nelly Padioukova, Sergey Mikhailov, H.B.F. Dixon, Grigorii Tzeitline, Marat Karpeisky
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Patent number: 6884791Abstract: 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: GrantFiled: November 22, 2002Date of Patent: April 26, 2005Assignee: MethylGene, Inc.Inventors: Jeffrey M. Besterman, Jubrail Rahil, Arkadii Vaisburg
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Patent number: 6872711Abstract: 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: GrantFiled: October 22, 2001Date of Patent: March 29, 2005Assignee: 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
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Publication number: 20040220408Abstract: Compounds according to formula (I) 1Type: ApplicationFiled: December 16, 2003Publication date: November 4, 2004Inventor: Fredrik Bjorkling
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Publication number: 20040186078Abstract: The present invention is directed to substituted N′-(arylcarbonyl)-benzhydrazides, N′-(arylcarbonyl)-benzylidene-hydrazides and analogs thereof, represented by the Formulae I and II: 1Type: ApplicationFiled: April 5, 2004Publication date: September 23, 2004Inventors: Sui Xiong Cai, Shailaja Kasibhatla, John Drewe, P. Sanjeeva Reddy, Han-Zhong Zhang
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Patent number: 6750340Abstract: 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: GrantFiled: December 7, 2000Date of Patent: June 15, 2004Assignee: MBC Research, Inc.Inventors: Nelly Padioukova, Sergey Mikhailov, H. B. F. Dixon, Grigorii Tzeitline
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Patent number: 6747037Abstract: 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: GrantFiled: June 6, 2003Date of Patent: June 8, 2004Assignee: Allergan, Inc.Inventors: David W. Old, Thang D. Dinh
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Patent number: 6727361Abstract: 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: GrantFiled: November 6, 2001Date of Patent: April 27, 2004Assignee: Symyx Technologies, Inc.Inventors: Anne M. LaPointe, Eric D. Carlson, Thomas Crevier
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Patent number: 6723711Abstract: 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: GrantFiled: October 9, 2001Date of Patent: April 20, 2004Assignee: Texas Biotechnology CorporationInventors: 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
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Patent number: 6703507Abstract: 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: GrantFiled: October 16, 2001Date of Patent: March 9, 2004Assignee: Celanese Chemicals Europe GmbHInventors: Helmut Bahrmann, Hans Bohnen
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Patent number: 6667315Abstract: 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: GrantFiled: October 28, 2002Date of Patent: December 23, 2003Assignee: Medicure International Inc.Inventor: Wasimul Haque
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Patent number: 6660860Abstract: 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: GrantFiled: June 7, 2002Date of Patent: December 9, 2003Assignee: Ciba Specialty Chemicals CorporationInventors: Reinhard Sommerlade, Hansjörg Grützmacher, Souâd Boulmaâz
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Patent number: 6653296Abstract: 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: GrantFiled: February 2, 1995Date of Patent: November 25, 2003Assignees: 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
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Publication number: 20030125559Abstract: 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: ApplicationFiled: April 26, 2002Publication date: July 3, 2003Applicant: Esperion Therapeutics, Inc.Inventors: Jean-Louis Henri Dasseux, Carmen Daniela Oniciu
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Publication number: 20030114677Abstract: 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: ApplicationFiled: October 28, 2002Publication date: June 19, 2003Applicant: Medicure International Inc.Inventor: Wasimul Haque
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Publication number: 20030114678Abstract: 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: ApplicationFiled: October 28, 2002Publication date: June 19, 2003Applicant: Medicure International Inc.Inventor: Wasimul Haque
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Patent number: 6576760Abstract: 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: GrantFiled: January 11, 2001Date of Patent: June 10, 2003Assignee: Chelator LLCInventors: Harry S. Winchell, Rosa L. Cyjon, Joseph Y. Klein, Elliot D. Simhon, Ofer Klein, Haim Zaklad
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Patent number: 6509359Abstract: A compound having the formula: wherein all variables are as defined in the specification, for use as a neuramninidase inhibitor.Type: GrantFiled: March 17, 2000Date of Patent: January 21, 2003Inventors: Wayne J. Brouillette, Venkatram Reddy Atigadda, Ming Luo, Yarlagadda S. Babu
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Patent number: 6498161Abstract: 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: GrantFiled: April 4, 2000Date of Patent: December 24, 2002Assignee: 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
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Patent number: 6498151Abstract: 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: GrantFiled: March 21, 2001Date of Patent: December 24, 2002Assignee: 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
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Patent number: 6472406Abstract: 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: GrantFiled: July 5, 2000Date of Patent: October 29, 2002Assignee: MethylGene, Inc.Inventors: Jeffrey M. Besterman, Daniel Delorme, Jubrail Rahil
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Patent number: 6451776Abstract: The present invention is directed to novel water-soluble prodrugs of aliphatic or aromatic hindered hydroxyl group containing pharmaceuticals.Type: GrantFiled: December 8, 2000Date of Patent: September 17, 2002Assignee: University of KansasInventors: Valentino J. Stella, Jan J. Zygmunt, Ingrid Gunda Georg, Muhammad S. Safadi
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Publication number: 20020082423Abstract: Aminophosphonates alpha substituted by phenol groups, of formula (I) have lipoprotein(a) lowering activity.Type: ApplicationFiled: September 4, 2001Publication date: June 27, 2002Applicant: SmithKline Beecham p.l.c. and SympharInventors: Lan Mong Nguyen, Hieu Trung Phan, Vinh Van Diep, Simon Floret, Raymond Azoulay, Eric Niesor, Craig Leigh Bentzen, Robert John Ife
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Patent number: 6407235Abstract: 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 thereofType: GrantFiled: August 16, 2001Date of Patent: June 18, 2002Assignee: Hoffmann-La Roche Inc.Inventors: Alexander Alanine, Bernd Buettelmann, Holger Fischer, Marie-Paule Heitz Neidhart, Joerg Huwyler, Georg Jaeschke, Emmanuel Pinard, René Wyler
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Patent number: 6391895Abstract: 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: GrantFiled: June 23, 2000Date of Patent: May 21, 2002Assignee: Amersham Health ASInventors: Robertson Towart, Jan Olof Gustav Karlsson, Lars Goran Wistrand, Hakan Malmgren
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Publication number: 20020042398Abstract: The present application describes novel lactams and derivatives thereof of formula I: 1Type: ApplicationFiled: July 10, 2001Publication date: April 11, 2002Inventors: Thomas P. Maduskuie, Jingwu Duan, Stephen E. Mercer