Nitrogen Containing Patents (Class 514/459)
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Publication number: 20080118509Abstract: The present invention provides an isolated specific binding member capable of binding a sialyltetraosly carbohydrate and directly inducing cell death without the need for immune effector cells. Such a binding member may be an antibody or a part thereof. Also provided are the use of such binding members in medicine and nucleic acids encoding such binding members.Type: ApplicationFiled: May 11, 2005Publication date: May 22, 2008Inventors: Linda Gillian Durrant, Tina Parsons
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Publication number: 20080113924Abstract: There are provided a novel compound having irreversible inhibitory activity against neuraminidase, a therapeutic agent and a detection agent for a disease involving neuraminidase. A compound represented by the following formula (I) and a salt thereof, a production method thereof, and an application method thereof, wherein: A1 represents an aryl group optionally having a substituent group or a heteroaryl group optionally having a substituent group; A2 represents —CX2R6 or —CHXR6 wherein X represents —F, —Cl, —Br, or —I; R1 represents a hydrogen atom or an alkyl group optionally having a substituent group; R2, R3, R4, and R5 represent each independently —OC(?O)R6, —OR6, —N(R6)2, —N3, —NHC(?NH)NHR6, —NHCOR6, —OSO3R6, —OPO3(R6)2, F, Cl, Br, or I; and R6 represents each independently a hydrogen atom, an alkyl group optionally having a substituent group, an aryl group optionally having a substituent group, or an optionally substituted heteroaryl group.Type: ApplicationFiled: December 16, 2005Publication date: May 15, 2008Applicants: NATIONAL INSTITUE OF ADVANCE INDUSTRIAL SCIENCE AND TECHNOLOGY, NATIONAL UNIVERSITY CORPORATION HOKKAIDO UNIVERSITY, SUMITOMO BAKELITE CO., LTD.Inventors: Shinichiro Nishimura, Hiroshi Hinou, Hirosato Kondo, Kazuhiko Fujiwara
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Patent number: 7371772Abstract: The present invention provides a new cyclic compound having a CCR antagonist activity, especially a CCR5 antagonist activity, and the use thereof. The compound of the present invention is represented by the formula: wherein, R1 is a 5- to 6-membered ring group which may be substituted; X1 is a bond or the like; ring A is a 5- to 6-membered ring group which may be substituted; ring B is a 8- to 10-membered ring group which may be substituted; X2 is a bivalent group of 1 to 4 atoms; Z1 is a bivalent cyclic ring group or the like; Z2 is a bond or the like; and R2 is an amino group, a nitrogen-containing heterocyclic group which may be substituted or the like, or a salt thereof.Type: GrantFiled: August 7, 2002Date of Patent: May 13, 2008Assignee: Takeda Pharmaceutical Company LimitedInventors: Mitsuru Shiraishi, Masanori Baba, Katsuji Aikawa, Naoyuki Kanzaki, Masaki Seto, Yuji Iizawa
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Patent number: 7354936Abstract: The present invention relates to 2-(4-sulphonylphenyl)pyran-4-one derivatives of general formula processes for their preparation, pharmaceutical compositions containing them, and their medical uses.Type: GrantFiled: September 16, 2002Date of Patent: April 8, 2008Assignee: Almirall AGInventors: Maria Isabel Crespo Crespo, Juan Miguel Jimenez Mayorga, Josep Lluis Matallana Julia, Joan Feixas Gras
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Publication number: 20080081060Abstract: A biodegradable medicament delivery system comprising a multi-layered calcium-sulfate based drug delivery vehicle. The vehicle comprises a calcium sulfate center or core with the medicament or medicaments, encased in one or more layers of chitosan. The chitosan may be cross-linked with a cross-linking agent. The vehicle may comprise any suitable shape, including, but not limited to, a sphere, bead or pellet. Medicaments include, but are not limited to, antibiotics, anesthetics, growth factors, and proteins. A physician can implant the coated vehicles into the desired site to create a beneficial, localized treatment that produces high local concentrations of medication while reducing the overall serum concentration throughout the body.Type: ApplicationFiled: October 3, 2007Publication date: April 3, 2008Inventors: Warren O. Haggard, Joel D. Bumgardner, Scott Noel, Kelly Richelsoph, Youling Yuan
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Patent number: 7351695Abstract: The invention encompasses novel salts of topiramate, and pharmaceutically acceptable polymorphs, solvates, hydrates, dehydrates, co-crystals, anhydrous, or amorphous forms thereof, as well as pharmaceutical compositions and pharmaceutical unit dosage forms containing the same. In particular, the invention encompasses pharmaceutically acceptable salts of topiramate, including without limitation topiramate sodium, topiramate lithium, topiramate potassium, or polymorphs, solvates, hydrates, dehydrates, co-crystals, anhydrous, and amorphous forms thereof. The invention further encompasses novel co-crystals or complexes of topiramate, as well as pharmaceutical compositions comprising them. The invention also encompasses methods of treating or preventing a variety of diseases and conditions including, but not limited to, seizures, epileptic conditions, tremors, cerebral function disorders, obesity, neuropathic pain, affective disorders, tobacco cessation, migraines, and cluster headache.Type: GrantFiled: November 19, 2003Date of Patent: April 1, 2008Assignee: Ortho-McNeil Pharmaceuticals, Inc.Inventors: Öm Almarssoo, Jules Remenar, Matthew L. Peterson
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Patent number: 7323188Abstract: A composition for controlling harmful bio-organisms comprising (a) at least one imidazole compound represented by formula (I): wherein R represents a lower alkyl group or a lower alkoxy group; and n represents an integer of 1 to 5, as an active ingredient, and (b) at least one inorganic phosphorus compound and/or at least one fungicide for Phycomycetes as an active ingredient or (c) a spreader as an activity-enhancing ingredient, and a method for controlling harmful bio-organisms comprising applying the composition for controlling harmful bio-organisms onto harmful bio-organisms.Type: GrantFiled: July 21, 2005Date of Patent: January 29, 2008Assignee: Ishihara Sangyo Kaisha, Ltd.Inventors: Norifusa Matsuo, Shigeru Mitani, Satoshi Araki, Yasuko Takii, Tomona Yamaguchi
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Patent number: 7276228Abstract: Methods are provided for treating hematological disorders by inhibition of DNA hypomethylation and histone deacetylase. Such disorders include, for example, acute promyelocytic leukemia, acute lymphoblastic leukemia, chronic myelogenous leukemia, myelodysplastic syndromes, and sickle cell anemia. The methods comprise: administering to a patient suffering from the disease a therapeutically effective amount of a DNA methylation inhibitor such as a cysteine analog such as decitabine, in combination with an effective amount of histone deacetylase inhibitor such as hydroxamic acid, cyclic peptide, benzamide, butyrate, and depudecin.Type: GrantFiled: March 15, 2005Date of Patent: October 2, 2007Assignee: SuperGen, Inc.Inventor: Jorge F. DiMartino
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Patent number: 7259166Abstract: 2,3-Di-substituted N-heteroaromatic propionamides with said substitution at the 2-position being a substituted phenyl group and at the 3-position being a polar ring, said propionamides being glucokinase activators which increase insulin secretion in the treatment of type II diabetes.Type: GrantFiled: April 10, 2006Date of Patent: August 21, 2007Assignee: Hoffmann-La Roche Inc.Inventors: Wendy Lea Corbett, Joseph Samuel Grimsby, Nancy-Ellen Haynes, Robert Francis Kester, Paige Erin Mahaney, Jagdish Kumar Racha, Ramakanth Sarabu, Ka Wang
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Patent number: 7253194Abstract: The present invention relates generally to amino acid derivatives and to methods of making the same. In particular, the invention relates to compounds bearing a stereochemical identity, that is, the same stereochemistry, with the chiral ?-carbon of D-?-amino acids and their use in methods of therapy, including the treatment of inflammatory diseases, and to compositions and enantiomeric mixtures containing them.Type: GrantFiled: July 24, 2001Date of Patent: August 7, 2007Assignee: The University of QueenslandInventors: Robert C Reid, Christopher I Clark, Karl Hansford, Martin J Stoermer, Ross P McGeary, David P Fairlie, Karl Schafer
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Patent number: 7230028Abstract: The invention relates to compounds of general formula (I); in which R is an amino or guanidino group; R2 is acetyl or trifluoroacetyl; and n is an integer from 10 to 18 or a pharmaceutically acceptable derivative thereof, methods for their preparation, pharmaceutical formulations containing them or their use in the prevention or treatment of a viral infectionType: GrantFiled: November 8, 2002Date of Patent: June 12, 2007Assignee: Biota Scientific Management Pty Ltd.Inventors: Derek A. Demaine, Graham G. A. Inglis, Simon J. F. MacDonald, Stephen E. Shanahan, Simon P. Tucker, Keith G. Watson, Wen-Yang Wu
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Patent number: 7226918Abstract: The invention relates to the use of compounds of formula (I) and isomers, salts, solvates, chemically protected forms, and prodrugs thereof, in the preparation of a medicament for inhibiting the activity of DNA-PK, wherein R1 and R2 are independently hydrogen, an optionally substituted C1-7 alkyl group, C3-20 heterocyclyl group, or C5-20 aryl group, or may together form, along with the nitrogen atom to which they are attached, an optionally substituted heterocyclic ring having from 4 to 8 ring atoms; X and Y are selected from CR4 and O, O and CR?4 and NR?4 and N, where the unsaturation is in the appropriate place in the ring, and where one of R3 and R4 or R?4 is an optionally substituted C3-20 heteroaryl or C5-20 aryl group, and the other of R3 and R4 or R?4 is H, or R3 and R4 or R?4 together are -A-B—, which collectively represent a fused optionally substituted aromatic ring. The compounds also selectively inhibit the activity of DNA-PK compared to PI 3-kinase and/or ATM.Type: GrantFiled: August 14, 2002Date of Patent: June 5, 2007Assignee: Cancer Research Technology LimitedInventors: Niall Morrison Barr Martin, Graeme Cameron Murray Smith, Roger John Griffin, Bernard Thomas Golding, Ian Robert Hardcastle, David Richard Newell, Hilary Alan Calvert, Nicola Jane Curtin, Laurent Jean Martin Rigoreau, Xiao-ling Fan Cockcroft, Vincent Junior Ming-lai Loh, Paul Workman, Florence Irene Raynaud, Bernard Paul Nutley
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Patent number: 7223790Abstract: The invention relates to compounds of general formula (I); in which R is an amino or guanidino group; R2 is acetyl or trifluoroacetyl; X is CONH, NHCO or O; n is an integer from 2 to 6; and Y is C2–C8 alkyl C3-8 cycloalkyl, C1–C4 alkoxyalkyl, an amino acid or dipeptide, or a pharmaceutically acceptable derivative thereof, methods for their preparation, pharmaceutical formulations containing them or their use in the prevention or treatment of a viral infectionType: GrantFiled: November 8, 2002Date of Patent: May 29, 2007Assignee: Biota Scientific Management Pty Ltd.Inventors: Betty Jin, Simon J. F. MacDonald, Darryl McConnell, Van T. T. Nguyen, Stephen E. Shanahan, Wen-Yang Wu
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Patent number: 7217706Abstract: This invention relates to new propanolamine derivatives or salts thereof represented by the following formula [I]: Wherein each symbol is as defined in the specification or salts thereof which have gut selective sympathomimetic, anti-ulcerous, anti-pancreatitis, lipolytic, anti-urinary incontinence and anti-pollakiuria activities, to processes for the preparation thereof, to a pharmaceutical composition comprising the same and to a method for the prevention and/or treatment diseases indicated in the specification to a human being or an animal.Type: GrantFiled: February 14, 2002Date of Patent: May 15, 2007Assignee: Astellas Pharma Inc.Inventors: Kiyoshi Taniguchi, Minoru Sakurai, Naoaki Fujii, Kumi Hosoi, Yasuyo Tomishima, Hisashi Takasugi, Hajime Sogabe, Hirofumi Ishikawa, Naomi Hanioka
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Patent number: 7214701Abstract: The invention relates to insecticidal mixtures for protecting plants against attack by pests comprising (a) compounds of the formula (I) ?in which W, X, Y, Z, A, B, D and G are each as defined in the disclosure, and (b) specified agonists or antagonists of nicotinic acetylcholine receptors.Type: GrantFiled: June 25, 2004Date of Patent: May 8, 2007Assignee: Bayer CropScience AGInventors: Reiner Fischer, Christoph Erdelen
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Patent number: 7214708Abstract: Synthetic discodermolide analogs having utility as antiproliferative agents, having a structure represented by formula A where RA through RE and XA are as defined herein.Type: GrantFiled: October 28, 2005Date of Patent: May 8, 2007Assignee: Kosan Biosciences IncorporatedInventors: Kurt F. Sundermann, Simon James Shaw, Daniel V. Santi
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Patent number: 7214707Abstract: The invention relates to compounds of general formula (I), in which: R is an amino or guanidino group; R2 is acetyl or trifluoroacetyl; n and q are either the same or different and selected from 0, 1 or 2; and X is an optionally substituted phenyl, optionally substituted naphthyl or optionally substituted phenyl-Y-optionally substituted phenyl in which Y is selected from a covalent bond, CH2, CH2CH2, O or SO2, or a pharmaceutically acceptable derivative thereof, with the proviso that when X is phenyl or naphthyl, n and q are both 2 and when X is phenyl-Y-phenyl in which Y is a covalent bond, then n and q are not both 0, methods for their preparation, pharmaceutical formulations containing them or their use in the prevention or treatment of a viral infectionType: GrantFiled: November 8, 2002Date of Patent: May 8, 2007Assignee: Biota Scientific Management Pty Ltd.Inventors: Derek A. Demaine, Haydn T. Jones, Simon J. F. MacDonald, Andrew McM Mason, Stephen E. Shanahan
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Patent number: 7183100Abstract: A bacterial protein which converts 2-methyl citrate to 2-methyl isocitrate is a previously unknown target for antibacterial agents. The protein of this activity is associated with mucoid bacteria and inhibitors of production or activity of this protein in combination with propionic acid mitigate the virulence of these bacteria.Type: GrantFiled: May 19, 2003Date of Patent: February 27, 2007Assignee: Biological Targets, Inc.Inventors: Mehmet Candas, Lee A. Bulla
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Patent number: 7166622Abstract: Compounds of Formula I, wherein R1–R8 are defined herein are provided, together with pharmaceutically acceptable salts, hydrates, metabolites, and/or prodrugs thereof. Uses of these compounds for inhibiting beta amyloid production and for the prevention and treatment of Alzheimer's Disease and Down's syndrome are described.Type: GrantFiled: June 9, 2003Date of Patent: January 23, 2007Assignees: Wyeth, ArQule, Inc.Inventors: Anthony Frank Kreft, Derek Cecil Cole, Kevin Roger Woller, Joseph Raymond Stock, Kristina Martha Kutterer, Dennis Martin Kubrak, Charles William Mann, William Jay Moore, David Scott Casebier
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Patent number: 7157494Abstract: The invention relates to compounds of general formula (I); in which R is an amino or guanidino group; R2 is acetyl or trifluoroacetyl; X is CONH, SO2NH, NHCO or NHCONH; m is either 0 or 1; n is an integer from 2 to 6; q is an integer from 0 to 3; and Y is hydrogen or an aromatic substituent, or a pharmaceutically acceptable derivative thereof; methods for their preparation, pharmaceutical formulations containing them or their use in the prevention or treatment of a viral infectionType: GrantFiled: November 8, 2002Date of Patent: January 2, 2007Assignee: Biota Scientific Management Pty. Ltd.Inventors: Michael D. Dowle, Betty Jin, Simon J. F. Macdonald, Andrew McM Mason, Darryl McConnell, Van T. T. Nguyen, Stephen E. Shanahan, Wen-Yang Wu
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Patent number: 7157489Abstract: Compounds useful for inhibiting HIV protease are disclosed. Methods of making the compounds, and their use as therapeutic agents, for example, in treating wild-type HIV and of multidrug-resistant strains of HIV, also are disclosed.Type: GrantFiled: March 6, 2003Date of Patent: January 2, 2007Assignee: The Board of Trustees of the University of IllinoisInventors: Arun K. Ghosh, Geoffrey M. Bilcer, Thippeswamy Devasamudram
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Patent number: 7153837Abstract: This invention relates to an agent for the protection of retinal neurons which comprises, as an effective ingredient, sulfamate derivative having the following formula: and to a method for the protection of retinal neurons by using said sulfamate derivative.Type: GrantFiled: June 14, 2002Date of Patent: December 26, 2006Assignee: Ortho-McNeil Pharmaceutical Inc.Inventors: Kaoru Ishigaki, Hiroshi Kojima, Shigehisa Okaguchi, Shinji Yoneda, Hideaki Hara, Nobuaki Miyawaki
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Patent number: 7148218Abstract: The present invention relates to certain substituted polyketides of formula I, wherein A, B and C are as defined herein, pharmaceutical compositions containing said compounds, and the use of said compounds in treating tumors.Type: GrantFiled: September 29, 2004Date of Patent: December 12, 2006Assignee: Novartis AGInventors: Frederick R Kinder, Jr., Kenneth W Bair, Timothy M Ramsey, Michael L Sabio
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Patent number: 7138547Abstract: New spisulosine derivatives of use in treating tumors are of the formula (I) wherein: each X is the same or different, and represents H, OH, OR?, SH, SR?, SOR?, SO2R?, NO2, NH2, NHR?, N(R?)2, CN, halogen, C(?O)H, C(?O)CH3, CO2H, CO2CH3, substituted or unsubstituted C1–C18 alkyl, substituted or unsubstituted C2–C18 alkenyl, substituted or unsubstituted C2–C18 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaromatic, or two groups X may together form ?O; Y is NR1, OR1, PR1, SR1, or halogen, wherein the number of substituents R1 is selected to suit the valency and each R1 is independently selected of H, OH, C(?O)R?, P(?O)R?R?, substituted or unsubstituted C1–C18 alkyl, substituted or unsubstituted C2–C18 alkenyl, substituted or unsubstituted C2–C18 alkynyl, substituted or unsubstituted aryl, and wherein the dotted line indicates an optional double bond; each Z is the same different, and represents H, OH, OR?, SH, SR?, SOR?, SO2R?, NO2, NH2, NHR?, N(R?)2, NHC(O)R?, CN, halogen, C(?OType: GrantFiled: June 6, 2001Date of Patent: November 21, 2006Assignee: Pharma Mar, S.A.Inventors: Jose Luis Aceña, Javier Adrio, Carmen Cuevas, Pilar Gallego, Ignacio Manzanares, Simon Munt, Ignacio Rodriguez
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Patent number: 7115658Abstract: Compounds of formula I are hepatitis C virus (HCV) RNA-dependent RNA polymerase (RdRp) inhibitors, and are useful in therapeutic and prophylactic treatment of persons infected with hepatitis C virusType: GrantFiled: May 9, 2003Date of Patent: October 3, 2006Assignee: Agouron Pharmaceuticals, Inc.Inventors: Allen J. Borchardt, Peter Scott Dragovich, Javier Gonzalez, Tanya Michelle Jewell, Hui Li, Maria Angelica Linton, John Howard Tatlock, Ru Zhou, Thomas Jay Prins, Melwyn A. Abreo
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Patent number: 7109243Abstract: The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at least one other cathepsin isozyme (e.g., cathespin K). The present invention also provides methods for treating a disease state in a subject by selectively inhibiting cathepsin S.Type: GrantFiled: March 23, 2004Date of Patent: September 19, 2006Assignee: IRM LLCInventors: Hong Liu, David Tully, Robert Epple, Badry Bursulaya, Jennifer Williams, Arnab Chatterjee, Jennifer Leslie Harris, Jun Li
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Patent number: 7098188Abstract: The invention relates to novel pharmaceutically acceptable salts of anticonvulsant derivatives, processes for preparation of and pharmaceutical compositions containing said salts, useful in the treatment of epilepsy.Type: GrantFiled: July 3, 2002Date of Patent: August 29, 2006Assignee: Ortho-McNeil Pharmaceutical., Inc.Inventors: Ahmed Abdel-Magid, Cynthia Maryanoff
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Patent number: 7094803Abstract: The subject invention provides novel compositions of biologically active polyketide compounds that can advantageously be used in blocking cellular proliferation and treatment of cancer.Type: GrantFiled: July 12, 2004Date of Patent: August 22, 2006Assignee: Harbor Branch Oceanographic Institution, Inc.Inventors: K. Brian Killday, Amy E. Wright, Shirley A. Pomponi, Ross E. Longley
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Patent number: 7084176Abstract: N-Arylphenylacetamide derivatives represented by the following formula [I]: (wherein R1 is C1-6 alkoxy, etc.; R2 is hydrogen, —(CH2)m—N(R6)(R7) (m is an integer of from 1 to 4; R6 is hydrogen, C1-4 alkyl, etc., R7 is hydrogen, etc.), etc.; R3 is hydrogen, halogen, etc.; R4 is C6-10 alkyl, —Y—R8 (Y is a single bond, C1-6 alkylene, C2-6 alkenylene, C2-6 alkynylene, etc., R8 is aryl, C3-8 cycloalkyl, C6-15 polycycloalkyl, etc.), etc.; R5 is hydrogen, etc.; and X1 is hydrogen), or pharmaceutically acceptable salts thereof or hydrates or solvates of the same, and a pharmaceutical composition containing the same. These compounds are useful as preventives and/or remedies giving no pain at the early stage of administration, which are efficacious in oral administration and have potent analgesic and antiinflammatory effects.Type: GrantFiled: June 6, 2002Date of Patent: August 1, 2006Assignee: Dainippon Pharmaceutical Co., Ltd.Inventors: Toshiya Morie, Keiji Adachi, Kazumi Niidome, Katsuyoshi Kawashima, Isao Shimizu, Daisuke Ishii
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Patent number: 7078400Abstract: The present invention relates to an inhibitor for production of 20-hydroxyeicosatetraenoic acid, comprising, as an effective ingredient, specific hydroxyformamidine derivatives or pharmaceutically-acceptable salts thereof. The inhibitors according to the present invention are useful as therapeutic agents for kidney diseases, cerebrovascular diseases, or circulatory diseases. In addition, the present invention also provides novel hydroxyformamidine derivatives or pharmaceutically-acceptable salts thereof.Type: GrantFiled: July 1, 2003Date of Patent: July 18, 2006Assignee: Taisho Pharmaceutical Co., Ltd.Inventors: Masakazu Sato, Noriyuki Miyata, Takaaki Ishii, Yuko Kobayashi, Hideaki Amada
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Patent number: 7045535Abstract: Certain cyclic compounds are presented as well as their use for inhibiting paramyxovirus neuraminidase.Type: GrantFiled: March 8, 2002Date of Patent: May 16, 2006Assignee: BioCryst Pharmaceuticals, Inc.Inventors: Pooran Chand, Yarlagadda S. Babu, R. Scott Rowland, Tsu-Hsing Lin
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Patent number: 7041650Abstract: The invention relates to novel pharmaceutically acceptable salts of anticonvulsant derivatives, processes for preparation of and pharmaceutical compositions containing said salts, useful in the treatment of epilepsy.Type: GrantFiled: January 3, 2003Date of Patent: May 9, 2006Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Ahmed Abdel-Magid, Cynthia Maryanoff
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Patent number: 7034015Abstract: The invention relates to a novel class of aminobenzophenones derivatives, to pharmaceutical preparations comprising said compounds, to dosage units of such preparations, to methods of treating patients comprising administering said compounds, and to the use of said compounds in the manufacture of pharmaceutical preparations.Type: GrantFiled: August 28, 2002Date of Patent: April 25, 2006Assignee: Leo Pharma A/SInventors: Erik Rytter Ottosen, Anne Marie Horneman, Xifu Liang
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Patent number: 7029703Abstract: A dietary supplement for benefitting human bone health includes a calcium source, a source of vitamin D activity, and an osteoblast stimulant. A preferred calcium source is microcrystalline hydroxyapatite, which also contains protein (mostly collagen), phosphorus, fat, and other minerals. A preferred source of vitamin D activity is cholecalciferol, and a preferred osteoblast stimulant is ipriflavone. In addition to these basic ingredients, the composition can further include various other minerals known to occur in bone, vitamin C, and glucosamine sulfate, all of which exert beneficial effects on growth and maintenance of healthy bone. A method for benefitting human bone health involves administering a daily regimen of the dietary supplement.Type: GrantFiled: September 9, 2002Date of Patent: April 18, 2006Assignee: Metagenics, Inc.Inventors: Kim C. Krumhar, Holly A. Johnson
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Patent number: 7026351Abstract: The present invention provides cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs, methods of making cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs and compositions of cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs. The present invention also provides methods of using cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs and compositions of cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs.Type: GrantFiled: March 20, 2003Date of Patent: April 11, 2006Assignee: Xenoport, Inc.Inventors: Mark A Gallop, Jia-Ning Xiang, Fenmei Yao, Laxminarayan Bhat
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Patent number: 7018983Abstract: A method for treating migraine in non-epileptic subjects which involves administering to subjects an effective amount of a pharmaceutical composition comprising a sulfamate of the following formula:Type: GrantFiled: September 25, 2002Date of Patent: March 28, 2006Assignee: New England Medical Center Hospitals, Inc.Inventors: Bruce L. Ehrenberg, Anita K. Wagner
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Patent number: 7012093Abstract: The present invention provides a novel compound multiple fluorescent natural dye from a marine organism Holothuria Scabra having a chemical structure of of Si—O—R type wherein silica matrix is an integral part of the compound, taking part in the metabolism of the animal, wherein R being an organic moiety and also provides a composition containing the compound having various applications; also a process of extraction, purification and characterization of the novel multiple fluorescent natural dye compound from a marine organism (Holothuria scabra).Type: GrantFiled: October 13, 2004Date of Patent: March 14, 2006Assignee: Council of Scientific & Industrial ResearchInventors: Usha Goswami, Anutosh Ganguly
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Patent number: 6992081Abstract: The present invention is directed toward substituted hydroxyethylene compounds of formulas (XII) (XIII), and (XIV) useful in treating Alzheimer's disease and other similar diseases.Type: GrantFiled: September 21, 2001Date of Patent: January 31, 2006Assignee: Elan Pharmaceuticals, Inc.Inventors: Roy Hom, Shumeye Mamo, Jay Tung, Andrea Gailunas, Varghese John, Lawrence Fang
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Patent number: 6989383Abstract: The present invention relates to methods of treating cancer using a combination of a compound which is an antineoplastic agent and a compound which is a inhibitor of prenyl-protein transferase, which methods comprise administering to said mammal, either sequentially in any order or simultaneously, amounts of at lest two therapeutic agents selected from a group consisting of a compound which is an antineoplastic agent and a compound which is an inhibitor or prenyl-protein transferase. The invention also relates to methods of preparing such compositions.Type: GrantFiled: June 4, 1998Date of Patent: January 24, 2006Assignee: Sloan-Kettering Institute For Cancer ResearchInventors: Neal Rosen, Laura Sepp-Lorenzino, Mark M. Moasser, Allen I. Oliff, Jackson B. Gibbs, Nancy Kohl, Samuel L. Graham, George C. Prendergast
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Patent number: 6949537Abstract: The invention provides novel prodrugs of inhibitors of PI-3 kinase. The novel compounds are LY294002 and analogs thereof comprising a reversibly quaternized amine.Type: GrantFiled: April 5, 2004Date of Patent: September 27, 2005Assignee: Semafore Pharmaceuticals, Inc.Inventors: Joseph R. Garlich, Donald L. Durden, Mary Patterson, Jingdong Su, Robert G. Suhr
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Patent number: 6949538Abstract: Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of KSP are disclosed.Type: GrantFiled: July 17, 2003Date of Patent: September 27, 2005Assignees: Cytokinetics, Inc., Smithkline Beecham CorporationInventors: Andrew McDonald, Gustave Bergnes, David J. Morgans, Jr., Dashyant Dhanak, Steven David Knight
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Patent number: 6906085Abstract: The present invention relates compounds of the formula (I): wherein R1, R2, R3, R4, R5, R6, R7 and R8 represent a variety of substituents; and pharmaceutically acceptable salts thereof. The compounds are of particular use in the treatment or prevention of depression, anxiety, pain, inflammation, migraine, emesis or postherpetic neuralgia.Type: GrantFiled: January 16, 2002Date of Patent: June 14, 2005Assignee: Merck Sharp & Dohme Ltd.Inventors: Jose Luis Castro Pineiro, Piotr Antoni Raubo, Christopher John Swain
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Patent number: 6905669Abstract: Compositions and methods are provided for treating diseases associated with aberrant silencing of gene expression such as cancer by reestablishing the gene expression through inhibition of DNA hypomethylation and histone deacetylase. The method comprises: administering to a patient suffering from the disease a therapeutically effective amount of a DNA methylation inhibitor such as a cysteine analog such as decitabine, in combination with an effective amount of histone deacetylase inhibitor such as hydroxamic acid, cyclic peptide, benzamide, butyrate, and depudecin.Type: GrantFiled: April 24, 2001Date of Patent: June 14, 2005Assignee: SuperGen, Inc.Inventor: Jorge F. DiMartino
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Patent number: 6890910Abstract: This invention provides isolated polynucleotides that encode the MurD protein of Pseudomonas aeruginosa. Purified and isolated MurD recombinant proteins are also provided. Nucleic acid sequences which encode functionally active MurD proteins are described. Assays for the identification of modulators of the of expression of murD and inhibitors of the activity of MurD, are also provided.Type: GrantFiled: May 26, 1999Date of Patent: May 10, 2005Assignee: Merck & Co., Inc.Inventors: Mohammed El-Sherbeini, Barbara Azzolina
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Patent number: 6869974Abstract: Compounds or their salts having general formulas (I) and (II): wherein s is an integer equal to 1 or 2, A is the radical of a drug that satisfies certain pharmacological tests, C and C1 are bivalent radicals, and precursors of the radicals B and B1 satisfy certain pharmacological tests.Type: GrantFiled: April 11, 2000Date of Patent: March 22, 2005Assignee: Nicox S.A.Inventor: Piero Del Soldato
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Patent number: 6864254Abstract: An inhibitor for 20-hydroxyeicosatetraenoic acid production which comprises as the active ingredient a specific hydroxyformamidine derivative or a pharmacologically acceptable salt thereof. It is useful especially as a remedy for kidney diseases, cerebrovascular diseases, or circulatory diseases. The novel hydroxyformamidine derivative or pharmacologically acceptable salt thereof is also provided.Type: GrantFiled: November 1, 2000Date of Patent: March 8, 2005Assignee: Taisho Pharmaceutical Co., Ltd.Inventors: Masakazu Sato, Noriyuki Miyata, Takaaki Ishii, Yuko Kobayashi, Hideaki Amada
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Patent number: 6864276Abstract: The invention relates to insecticidal mixtures for protecting plants against attack by pests comprising (a) compounds of the formula (I) ?in which W, X, Y, Z, A, B, D and G are each as defined in the disclosure, and (b) agonists or antagonists of nicotinic acetylcholine receptors.Type: GrantFiled: May 7, 2001Date of Patent: March 8, 2005Assignee: Bayer Cropscience AGInventors: Reiner Fischer, Christoph Erdelen
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Patent number: 6852717Abstract: Disclosed are compounds useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are processes of making such compounds.Type: GrantFiled: May 10, 2002Date of Patent: February 8, 2005Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Pier Francesco Cirillo, Daniel R. Goldberg, Abdelhakim Hammach, Neil Moss, John Robinson Regan
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Patent number: 6833445Abstract: Provided are reagents and methods useful for the synthesis of guanidinylated compounds. Also provided are methods for assaying molecules, including guanidinylated molecules that modulate viral infection and replication.Type: GrantFiled: January 21, 2003Date of Patent: December 21, 2004Assignee: The Regents of the University of CaliforniaInventors: Murray Goodman, Yitzhak Tor, Tracy Baker, Nathan Luedtke
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Patent number: RE38793Abstract: The present invention is directed to the isolation and bioactive characterization of compounds isolated from the clam Spisula polynyma. These compounds include three sphingoid-type bases, spisulosines 285, 299 and 313 (1-3), each of which shows unique cytotoxicity against L1210 murine lymphocytic leukemia cells. In addition, sphingosine (also referred to as 4-sphingenine or octadeca-4-shpingenine, 4) and two related compounds, nonadeca-4-sphingenine (a one carbon longer homolog, 5) and sphinga-4,10-diene (a dehydrosphingosine deravitive, 6) were also obtained, These compounds also contribute to the cytotoxicity of the Spisula polynyma extracts, but did not cause the morphology changes observed with compounds 1-3.Type: GrantFiled: August 14, 2002Date of Patent: September 6, 2005Inventors: Kenneth L. Rinehart, Nancy L. Gallagher, Robert A. Warwick