Phosphorus Attached Directly Or Indirectly To The Diazine Ring By Nonionic Bonding Patents (Class 544/243)
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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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Publication number: 20030105056Abstract: The invention features linker molecules that have at one terminus a amino-protecting group and at the other terminus a phosphorous activating group, typically phosphoramidite. The linker molecules can be used, for example, to produce amino-modified linkers that space an oligonucleotide from a solid support. The invention also features an amino-protected nucleotide that includes an activated phosphorous group such as a phosphoramidite for the production of a 5′ amino-modified oligonucleotide. The invention further provides a phthalimido-modified support that can be used to synthesize a polynucleotide that includes an amino group at the 3′ terminus.Type: ApplicationFiled: September 27, 2002Publication date: June 5, 2003Inventors: Tai-Nang Huang, Ming Shen
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Publication number: 20030105309Abstract: An oligo- or polynucleotide analogue having one or more structures of the general formula 1Type: ApplicationFiled: December 28, 2001Publication date: June 5, 2003Applicant: Takeshi IMANISHIInventors: Takeshi Imanishi, Satoshi Obika
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Publication number: 20030096265Abstract: Photoreactive phosphoramidites useful for attaching photoreactive sites to nucleic acids and oligonucleotides are synthesized. The resultant nucleic acid or oligonucleotide probes incorporating the photoreactive sites are then attached to a polymer-coated support by a [2+2] cycloaddition to form a microarray.Type: ApplicationFiled: June 28, 2002Publication date: May 22, 2003Applicant: Motorola, Inc.Inventors: Charles K. Brush, Robert Elghanian, Yanzheng Xu
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Publication number: 20030092678Abstract: N-Heterocyclic derivatives of the formula (I): 1Type: ApplicationFiled: April 12, 2002Publication date: May 15, 2003Applicant: Berlex Laboratories, Inc.Inventors: Damian O. Arnaiz, John J. Baldwin, David D. Davey, James J. Devlin, Roland Ellwood Dolle, Shawn David Erickson, Kirk McMillan, Michael M. Morrissey, Michael H.J. Ohlmeyer, Gonghua Pan, Vidyadhar Madhav Paradkar, John Parkinson, Gary B. Phillips, Bin Ye, Zuchun Zhao
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Publication number: 20030078236Abstract: According to the invention there is provided a compound the formula I; 1Type: ApplicationFiled: August 29, 2002Publication date: April 24, 2003Applicant: Allergan, Inc.Inventors: Robert M. Burk, Sophie Beauchemin
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Publication number: 20030073669Abstract: N-Heterocyclic derivatives of the formula (I): 1Type: ApplicationFiled: April 12, 2002Publication date: April 17, 2003Applicant: Berlex Laboratories, Inc.Inventors: Damian O. Arnaiz, John J. Baldwin, David D. Davey, James J. Devlin, Roland Ellwood Dolle, Shawn David Erickson, Kirk McMillan, Michael M. Morrissey, Michael H.J. Ohlmeyer, Gonghua Pan, Vidyadhar Madhav Paradkar, John Parkinson, Gary B. Phillips, Bin Ye, Zuchun Zhao
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Publication number: 20030069412Abstract: Synthetic processes are provided for the solution phase synthesis of oligonucleotides, especially phosphorothioate oligonucleotides, and intermediate compounds useful in the processes.Type: ApplicationFiled: October 11, 2002Publication date: April 10, 2003Inventors: Vasulinga Ravikumar, Douglas L. Cole
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Publication number: 20030065146Abstract: Novel ethylene glycol compounds bearing various functional groups are used to prepare oligomeric structures. The ethylene glycol monomers can be joined via standard phosphate linkages including phosphodiester and phosphorothioate linkages. Useful functional groups include nucleobases as well as polar groups, hydrophobic groups, ionic groups, aromatic groups and/or groups that participate in hydrogen-bonding.Type: ApplicationFiled: June 3, 2002Publication date: April 3, 2003Inventors: Phillip D. Cook, Oscar L. Acevedo, Peter W. Davis, David J. Ecker, Normand Hebert
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Publication number: 20030064997Abstract: Novel 2,4,5-triaryl imidazole compounds and compositions for use in therapy.Type: ApplicationFiled: March 27, 2001Publication date: April 3, 2003Applicant: SmithKline Beecham CorporationInventors: Jerry Leroy Adams, Timothy Francis Gallagher, John C. Lee, John Richard White
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Publication number: 20030060452Abstract: N-Heterocyclic derivatives of the formula (I): 1Type: ApplicationFiled: April 12, 2002Publication date: March 27, 2003Applicant: Berlex Laboratories, Inc.Inventors: Damian O. Arnaiz, John J. Baldwin, David D. Davey, James J. Devlin, Roland Ellwood Dolle, Shawn David Erickson, Kirk McMillan, Michael M. Morrissey, Michael H. J. Ohlmeyer, Gonghua Pan, Vidyadhar Madhav Paradkar, John Parkinson, Gary B. Phillips, Bin Ye, Zuchun Zhao
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Publication number: 20030055016Abstract: The present invention provides selenium derivatives of nucleosides, nucleoside phosphoramidites, nucleotides, nucleotide triphosphates, oligonucleotides, polynucleotides, and larger nucleic acids and methods for their synthesis. Selenium derivatives of both ribonucleic acids and deoxyribonulcleic acids, as well as methods for their synthesis, crystallization and uses in structural determinations, particularly by X-ray crystallographic techniques are disclosed. The selenium derivatives of the present invention are also useful as food supplements.Type: ApplicationFiled: March 22, 2002Publication date: March 20, 2003Inventor: Zhen Huang
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Publication number: 20030054365Abstract: Disclosed is a specific regulator of Ii protein expression or immunoregulatory function. Specifically disclosed are several forms of the specific regulator of Ii, including those which function through the formation of a duplex molecule with an RNA molecule encoding mammalian Ii protein to inhibit Ii protein synthesis at the translation level. This class includes copolymers comprised of nucleotide bases which hybridize specifically to the RNA molecule encoding mammalian Ii protein, and also expressible reverse gene constructs. In other aspects, the disclosure relates to MHC class II-positive antigen presenting cells containing a specific regulator of Ii expression. Such cells are useful, for example, in the display of autodeterminant peptides in association with MHC class II proteins. Compositions of the invention find application in methods for treating diseases, for example malignancies and autoimmune disorders, in a patient by enhancing immunological attack on undesired cells.Type: ApplicationFiled: January 22, 2002Publication date: March 20, 2003Applicant: Antigen Express, Inc.Inventors: Minzhen Xu, Gang Qiu, Robert Humphreys
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Patent number: 6531581Abstract: Compounds are described comprising purines substituted at the C-8 position and pyrimidines substituted at the C-4 position with a linker and quencher. These compounds, when incorporated into hairpin oligonucleotides quench the fluorescence of fluorophores linked to the 5′-terminus of the oligonucleotide. These nucleotide-quencher compounds are also easily incorporated into oligonucleotides using conventional or automated oligonucleotide synthetic techniques.Type: GrantFiled: October 26, 2000Date of Patent: March 11, 2003Assignee: Serologicals, Inc.Inventors: Glenn Nardone, Irena Nazarenko, Jila Boal
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Publication number: 20030045698Abstract: Synthetic processes are provided wherein mixed backbone oligomeric compounds are prepared having at least one phosphodiester internucleoside linkage in addition to one or more phosphorothioate, phosphoramidate and boranophosphate internucleoside linkages. Novel H-phosphonate intermediates are also disclosed that are useful in the synthetic processes. The synthetic processes use a novel oxidation step to oxidize H-phosphonate internucleoside linkages to phosphodiester internucleoside linkages without degradation of adjacent phosphorothioate, phosphoramidate and boranophosphate internucleoside linkages. Also provided are synthetic intermediates useful in such processes.Type: ApplicationFiled: April 5, 2002Publication date: March 6, 2003Applicant: Isis Pharmaceuticals, Inc.Inventors: Muthiah Manoharan, Martin A. Maier
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Publication number: 20030032803Abstract: The present application describes novel amides and derivatives thereof of formula 1Type: ApplicationFiled: February 12, 2002Publication date: February 13, 2003Inventors: Jingwu Duan, Carl P. Decicco, David J. Nelson, Chu-Biao Xue
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Publication number: 20030028013Abstract: Conformationally restricted 2′, 4′-bridged nucleoside analogues are described herein. The compounds can be prepared by cyclization at C2′ and C4′ of nucleosides through a linker or linking molecule. These novel nucleosides have a desired, locked sugar pucker and are potentially useful as pharmaceutical ingredients, and especially for use in treatment of HCV.Type: ApplicationFiled: April 30, 2002Publication date: February 6, 2003Inventors: Guangyi Wang, Zhi Hong, Haoyun An
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Publication number: 20030027794Abstract: N-Heterocyclic derivatives of the formula (I): 1Type: ApplicationFiled: April 12, 2002Publication date: February 6, 2003Applicant: Berlex Laboratories, Inc.Inventors: Damian O. Arnaiz, John J. Baldwin, David D. Davey, James J. Devlin, Roland Ellwood Dolle, Shawn David Erickson, Kirk McMillan, Michael M. Morrissey, Michael H. J. Ohlmeyer, Gonghua Pan, Vidyadhar Madhav Paradkar, John Parkinson, Gary B. Phillips, Bin Ye, Zuchun Zhao
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Publication number: 20030004345Abstract: Disclosed are novel unsaturated phosphonate derivatives of certain purines or pyrimidines useful as antiviral agents, methods useful for their preparation and use of these compounds as antiviral agents effective against DNA viruses, retroviruses and viruses involved in tumor formation.Type: ApplicationFiled: June 4, 2002Publication date: January 2, 2003Inventors: Patrick Casara, Jean-Francois Nave, Serge Halazy
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Patent number: 6500811Abstract: Compounds of the formula I are suitable for the production of pharmaceuticals for the prophylaxis and therapy of disorders in the course of which an increased activity of matrix-degrading enzymes is involved.Type: GrantFiled: March 20, 2001Date of Patent: December 31, 2002Assignee: Aventis Pharma Deutschland GmbHInventors: Manfred Schudok, Wilfried Schwab, Gerhard Zoller, Eckart Bartnik, Frank Büttner, Klaus-Ulrich Weithmann
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Publication number: 20020198173Abstract: A method and composition for the treatment of HIV and HBV infections in humans and other host animals is disclosed that includes the administration of an effective amount of a [5-carboxamido or 5-fluoro]-2′,3′-dideoxy-2′,3′-didehydro-pyrimidine nucleoside or a [5-carboxamido or 5-fluoro]-3′-modified-pyrimidine nucleoside, or a mixture or a pharmaceutically acceptable derivative thereof, including a 5′ or N4 alkylated or acylated derivative, or a pharmaceutically acceptable salt thereof, in a pharmaceutically acceptable carrier.Type: ApplicationFiled: May 15, 2002Publication date: December 26, 2002Applicant: Emory UniversityInventors: Raymond F. Schinazi, Dennis C. Liotta
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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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Publication number: 20020187928Abstract: The invention provides a compound of formula (I): 1Type: ApplicationFiled: May 30, 2001Publication date: December 12, 2002Inventors: Lixin Qiao, Rene Etcheberrigaray
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Publication number: 20020182602Abstract: The present invention relates generally to nucleobase polymer functionalizing reagents, to mobility-modified sequence-specific nucleobase polymers, to compositions comprising a plurality of mobility-modified sequence-specific nucleobase polymers, and to the use of such polymers and compositions in a variety of assays, such as, for example, for the detection of a plurality of selected nucleotide sequences within one or more target nucleic acids. The mobility-modifying polymers of the present invention include phosphoramidite reagents which can be joined to other mobility-modifying monomers and to sequence-specific oligonucleobase polymers via uncharged phosphate triester linkages. Addition of the mobility-modifying phosphoramidite reagents of the present invention to oligonucleobase polymers results in unexpectedly large effects the mobility of those modified oligonucleobase polymers, especially upon capillary electrophoresis in non-sieving media.Type: ApplicationFiled: April 16, 2001Publication date: December 5, 2002Inventors: Sam L. Woo, Ron Graham, Jing Tian
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Patent number: 6489333Abstract: This invention relates to novel heterocycles which are useful as antagonists of the &agr;v&bgr;3 integrin, the &agr;2b&bgr;3 integrin, and related cell surface adhesive protein receptors, to pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of cell adhesion, the treatment of angiogenic disorders, inflammation, bone degradation, cancer metastasis, diabetic retinopathy, thrombosis, restenosis, macular degeneration, and other conditions mediated by cell adhesion and/or cell migration and/or angiogenesis.Type: GrantFiled: April 9, 2001Date of Patent: December 3, 2002Assignee: Bristol - Meyers Squibb Pharma CompanyInventors: William J. Pitts, Prabhakar K. Jadhav
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Patent number: 6486332Abstract: Compounds of formula A(B)x, (I) wherein x is an integer from 1 to 4, A is the radical of a chromophore of the quinacridone, anthraquinone, perylene, indigo, quinophthalone, isoindolinone, isoindoline, dioxazine, phthalocyanine or azo series, which radical contains x N-atoms attached to B, preferably with at least one directly adjacent or conjugated carbonyl group, B is a group of formula and, if x is 2, 3 or 4, may also be one, two or three hydrogen atoms. The symbols Q, R1, R2, R3, R4, X, Y, Z, m and n, are as defined in claim 1. These carbamate group-containing soluble chromophores are distinguished by outstanding solid state fluorescence in the UV range as well as the by ease with which they can be converted to the corresponding pigments in the substrate in which they are incorporated.Type: GrantFiled: February 6, 2001Date of Patent: November 26, 2002Assignee: Ciba Specialty Chemicals CorporationInventors: Zhimin Hao, John S. Zambounis, Abul Iqbal
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Publication number: 20020173490Abstract: Novel bisamidate phosphonate prodrugs of FBPase inhibitors of the Formula IA: 1Type: ApplicationFiled: December 22, 2000Publication date: November 21, 2002Applicant: METABASIS THERAPEUTICS, INC.Inventors: Tao Jiang, Srinivas Rao Kasibhatla, K. Raja Reddy
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Publication number: 20020173515Abstract: Novel derivatives of 5-thia- and 5-selenopyrimidinone are found to inhibit the enzyme glycinamide ribonucleotide formyl transferase (GARFT) and amino imidazole carboxamide ribonucleotide formyl transferase (AICARFT). Novel intermediates of these compounds are also disclosed. A novel method of preparing such compounds is also disclosed, as well as methods and compositions for employing the compounds as antiproliferative agents.Type: ApplicationFiled: October 23, 2001Publication date: November 21, 2002Inventors: Michael D. Varney, William H. Romines, Cynthia L. Palmer, Judith G. Deal
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Publication number: 20020173649Abstract: The present invention relates to certain novel pyrimidine intermediates and their salts, processes for their preparation and processes for their conversion to 9-substituted-2-aminopurines which are useful in medical therapy.Type: ApplicationFiled: June 27, 2002Publication date: November 21, 2002Inventors: Susan Mary Daluge, Michelle Joanne Fugett, Michael Tolar Martin
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Publication number: 20020169173Abstract: This invention relates to the novel oxazole compounds of Formula (I) and novel pharmaceutical compositions comprising a compound of Formula (I) and a pharmaceutically acceptable diluent or carrier.Type: ApplicationFiled: January 25, 2001Publication date: November 14, 2002Applicant: SmithKline Beecham CorporationInventors: Jerry Leroy Adams, Timothy Francis Gallagher, Jeffrey Charles Boehm, Susan Mary Thompson
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Publication number: 20020165202Abstract: Novel, heterocyclic compounds having at least one ring nitrogen, disclosed side chains and, in some embodiments, an oxygen ortho to the ring nitrogen inhibit inflammatory responses associated with TNF-&agr; and fibroblast proliferation in vivo and in vitro. The compounds of the invention neither appreciably inhibit the activity of cAMP phosphodiesterase nor the hydrolysis of phosphatidic acid, and are neither cytotoxic nor cytostatic. Preferred compounds of the invention are esters. Methods for the use of the novel compounds to inhibit ceramide-mediated intracellular responses in stimuli in vivo (particularly TN-&agr;) are also described. The methods are expected to be of use in reducing inflammatory responses (for example, after angioplasty), in limiting fibrosis (for example, of the liver in cirrhosis), in inhibiting cell senescence, cell apoptosis and UV induced cutaneous immune suppression. Compounds having enhanced water solubility are also described.Type: ApplicationFiled: September 13, 2001Publication date: November 7, 2002Applicant: The Regents of the University of CaliforniaInventors: Dennis A. Carson, Howard Cottam
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Publication number: 20020165218Abstract: Compounds that inhibit DNA-dependent protein kinase, compositions comprising the compounds, methods to inhibit the DNA-PK biological activity, methods to sensitize cells the agents that cause DNA lesions, and methods to potentiate cancer treatment are disclosed.Type: ApplicationFiled: August 28, 2001Publication date: November 7, 2002Inventors: James Halbrook, Edward A. Kesicki, Laurence E. Burgess, Stephen T. Schlachter, Charles T. Eary, Justin G Schiro, Hongmei Huang, Michael Evans, Yongxin Han
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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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Publication number: 20020155989Abstract: The present invention relates generally to oligonucleotide analogues that include novel protein nucleic acid molecules (PNAs), particularly monomers, dimers, oligomers thereof and methods of making and using these oligonucleotide analogues. The PNAs of the present invention are characterized as including a variety of classes of molecules, such as, for example, hydroxyproline peptide nucleic acids (HypNA), and serine peptide nucleic acids (SerNA). The invention includes monomers, homodimers, heterodimers, homopolymers and heteropolymers of these and other oligonucleotide analogues. The present invention includes methods of using these oligonucleotide analogues in the detection and separating of nucleic acid molecules, including uses that include the utilization of oligonucleotide analogues on a solid support. The present invention also includes methods for purifying or separating nucleic acids, such as mRNA molecules, by hybridization with the oligonucleotides of the present invention.Type: ApplicationFiled: March 13, 2001Publication date: October 24, 2002Inventors: Vladimir Efimov, Joseph Fernandez, Dorothy Archdeacon, John Archdeacon, Oksana Chakhmakhcheva, Alla Buryakova, Mikhail Choob, Kyle Hondorp
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Patent number: 6465474Abstract: Disclosed are compounds which are inhibitors of metalloproteases having the following structure: where Ar, W, X, Y, Z, R1 and R2 have the meanings described in the specification and optical isomers, diastereomers, and enantiomers thereof or a pharmaceutically-acceptable salt, or biohydrolyzable amides, esters, or imides thereof. Also disclosed are pharmaceutical compositions and methods of treating diseases, disorders and conditions characterized by unwanted metalloprotease activity using these compounds or pharmaceutical compositions.Type: GrantFiled: August 29, 2000Date of Patent: October 15, 2002Assignee: The Procter & Gamble CompanyInventors: Stanislaw Pikul, Kelly Lynn McDow-Dunham, Neil Gregory Almstead, Biswanath De, Michael George Natchus, Yetunde Olabisi Taiwo
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Patent number: 6458946Abstract: The invention provides crystals of p1,P4-di(uridine 5′-) tetraphosphate or a salt thereof; a process for producing the crystals; and a process for producing P1,P4-di(uridine 5′-) tetraphosphate (U2P4) or a salt thereof from UMP serving as a starting material and by use of DPC and PPi, which process comprises at least one of the following treatment steps: (a) adding UMP diphenylphosphate (UMP-DPP) in divided portions during a step of reaction of UMP-DPP with a PPi-organic alkali salt; (b) carrying out reaction of UMP-DPP with a PPi-organic alkali salt in the presence of a base; and (c) further treating the synthesized U2P4 with an alkali. The crystals of U2P4 or a salt thereof obtained through the process according to the invention have high purity and stability and a less hygroscopicity as compared with a lyophilized product, to thereby serve as a useful raw material for preparing a pharmaceutical.Type: GrantFiled: July 28, 2000Date of Patent: October 1, 2002Assignee: Yamasa CorporationInventors: Hideaki Maeda, Toshio Yamada, Hiroshi Sato, Yutaka Noda
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Patent number: 6455513Abstract: Aryl substituted phosphoryl derivatives of the formula In which Ar is phenyl, naphthyl, or pyridyl, Y is O or S, X1 is O, NR3, S, CR3R4, CR3W1 or CW1W2, X2 and X6 are a bond or X6 is CH2 and X2 is O, NR3, S, CR3R4, CR3W1 or CW1W2, R3 and R4 are H, alkyl or phenyl, groups, W1 and W2 are heteroatoms, X3 is alkylene, X4 is oxygen or CH2, X5 is a bond or CH2, Z is O, NR5, S, alkyl or phenyl, R5 is H, alkyl or phenyl, J is H, alkyl, phenyl, or a heterocyclic or polycyclic group, Q is O, NR6, S, CR6R7, CR6W3 or CW3W4, R6 and R7 are H, alkyl, or phenyl, and W3 and W4 are hetero atoms, T1 and T2 are H or CH2R8, R8 is H, OH or F, or T1 and T2 together are —CH═CH— or —C(R9)(R10)C(R11)(R12)—, R9 is H, halogeno, CN, NH2, CO-alkyl, or alkyl, R10, R11, and R12 are H, N3, halogen, CN, NH2, CO-alkyl, or alkyl, and B is a purine or pyrimidine base, have antiviral activity, as for example against HIV.Type: GrantFiled: August 24, 1999Date of Patent: September 24, 2002Assignees: University College Cardiff Consultants Ltd., Rega FoundationInventors: Christopher McGuigan, Jan Balzarini
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Patent number: 6451824Abstract: Compounds of formula (I) are suitable for the production of pharmaceuticals for the prophylaxis and therapy of disorders in the course of which an increased activity of matrix-degrading metalloproteinases is involved.Type: GrantFiled: May 8, 1998Date of Patent: September 17, 2002Assignee: Aventis Pharma Deutschland GmbHInventors: Werner Thorwart, Wilfried Schwab, Manfred Schudok, Burkhard Haase
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Patent number: 6448401Abstract: An improved process is provided for preparing water-soluble prodrugs of triazole antifungal compounds containing a secondary or tertiary hydroxyl group. More particularly, the improved process is directed toward preparation of water-soluble triazole antifungal compounds are provided having the general formula wherein A is the non-hydroxy portion of a triazole antifungal compound of the type containing a secondary or tertiary hydroxyl group and R and R1 are as defined in the specification.Type: GrantFiled: October 16, 2001Date of Patent: September 10, 2002Assignee: Bristol-Myers Squibb CompanyInventors: Chung-Pin Chen, Timothy Paul Connolly, Laxma Reddy Kolla, John D. Matiskella, Richard H. Mueller, Yadagiri Pendri, Dejah T. Petsch
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Patent number: 6444656Abstract: The present invention relates to a novel nucleotide analogue having the general formula (I) and pharmaceutically acceptable salts, esters, or salt of such esters: wherein n, X, Q U R1′, R1, Z and R2 are defined here within. The compounds object of the present invention may be a single enantiomers or as mixtures of said enantiomers, the compounds may have a &agr;D, &agr;-L, &bgr;-D, &bgr;-L, R or S configuration at each chiral center or mixtures thereof. This invention also relates to pharmaceutical compositions containing them, alone or in combination with other therapeutic agents, and their use as antiviral agents, particularly against HIV and/or HBV infections in mammals.Type: GrantFiled: March 24, 2000Date of Patent: September 3, 2002Assignee: BioChem Pharma, Inc.Inventors: Nghe Nguyen-Ba, Rabindra Rej
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Patent number: 6440664Abstract: An instrument for sequencing oligonucleotides is loaded with the products of four sequencing reaction mixtures. These products are a combination of A, C, G and T reaction products for several sequencing reactions. The products of the different sequencing reactions are labeled with fluorescent tags which are distinguishable one from the other on the basis of their excitation or emission spectra. After separation of the oligonucleotides by electrophoresis, the order of the detected peaks is used to call the base sequence.Type: GrantFiled: December 9, 1998Date of Patent: August 27, 2002Assignee: Visible Genetics Inc.Inventors: Thomas J. Digby, Alexandre Izmailov
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Publication number: 20020115857Abstract: A cyclopentenecarboxamide derivative represented by the formula (I): 1Type: ApplicationFiled: April 25, 2002Publication date: August 22, 2002Applicant: Kuraray Co., Ltd.Inventors: Nobuya Katagiri, Chikara Kaneko, Junko Sato, Masahiro Torihara, Koichi Kanehira, Yoshin Tamai
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Publication number: 20020102590Abstract: Provided are nucleotide-dye conjugates and related compounds in which a dye is linked to a nucleobase directly or indirectly by an anionic linker. The anionic character of the linker is provided by one or more anionic moieties which are present in the linker, such as phosphate, phosphonate, sulfonate, and carboxylate groups. When the dye is a provided as a donor/acceptor dye pair, the anionic linker can be located between the donor and the acceptor, or between the nucleobase and either the donor or acceptor, or both. In one embodiment, conjugates of the invention provide enhanced electrophoretic mobility characteristics to sequencing fragments, e.g., for dideoxy sequencing using labeled terminators.Type: ApplicationFiled: October 11, 2001Publication date: August 1, 2002Applicant: PE Corporation (NY)Inventors: Meng Taing, Shaheer H. Khan, Steven M. Menchen, Barnett B. Rosenblum
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Publication number: 20020103158Abstract: The present invention relates to certain novel dinucleotide polyphosphates of general Formulae I, II and III, and formulations thereof which are selective agonists of the P2Y purinergic receptors. They are useful in the prevention, management or treatment of diseases and disorders associated with abnormalities of tissue fluid secretion, hydration and clearance, including chronic obstructive pulmonary diseases (chronic bronchitis, PCD, cystic fibrosis, immobility-associated pneumonia), sinusitis, otitis media, nasolacrimal duct obstruction, dry eye disease, glaucoma, retinal degeneration, and edematous retinal disorders, including retinal detachment, vaginal dryness, and gastrointestinal tract disease. Finally, these novel dinucleotides may be useful for diagnostic purposes, such as the facilitation of sputum induction and expectoration for the analysis of respiratory tract secretions.Type: ApplicationFiled: March 23, 2001Publication date: August 1, 2002Inventors: Janet Rideout, Benjamin R. Yerxa, Sammy Ray Shaver, James G. Douglass
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Publication number: 20020087030Abstract: A process for preparing polymerizable biaryl derivatives comprises reacting an aromatic comprising a 6-membered ring which bears ester or benzylic OH groups in the 1,4 position with a second aromatic in a palladium-catalyzed cross-coupling reaction to give a biaryl and converting the ester or benzylic OH groups into polymerizable groups in one or more steps. The biaryls obtained are suitable for preparing polymers which are used as electroluminescence materials.Type: ApplicationFiled: October 16, 2001Publication date: July 4, 2002Inventors: Hubert Spreitzer, Willi Kreuder, Heinrich Becker, Jochen Krause
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Patent number: 6410538Abstract: Benzamidine derivatives of the following formula, analogs thereof and pharmaceutically acceptable salts thereof are provided. These compounds have an effect of inhibiting activated blood-coagulation factor X, and they are useful as agents for preventing or treating various diseases caused by thrombi or emboli.Type: GrantFiled: December 8, 2000Date of Patent: June 25, 2002Assignee: Ajinomoto Co., Inc.Inventors: Tadakiyo Nakagawa, Kazuyuki Sagi, Kaoru Yoshida, Yumiko Fukuda, Masataka Shoji, Shunji Takehana, Takashi Kayahara, Akira Takahara
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Patent number: 6407080Abstract: Disclosed are compounds, compositions and methods for inhibiting interleukin-1&bgr; (IL-&bgr;) protease activity. The compounds, N-(pyrimidinyl)-aspartic acid &agr;-substituted methyl ketones and aspartic acid aldehydes, have the formula (I) set out herein. These compounds are inhibitors of 1&bgr;-converting enzyme and as such are useful whenever such inhibition is desired. For example, they may be used as research tools in pharmacological, diagnostic and related studies and in the treatment of diseases in mammals in which 1L-&bgr; protease activity is implicated.Type: GrantFiled: December 19, 2000Date of Patent: June 18, 2002Assignee: Vertex Pharmaceuticals IncorporatedInventors: Roland E. Dolle, Catherine P. Prouty, Prasad V. Chaturvedula, Stanley J. Schmidt
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Patent number: 6399589Abstract: Compounds of formula RS—P(═O)(QR)—Nu where: R is a radical —(CH2)n—W—X; X is a radical —C(═Z) (Y) or —S—U; Z is O or S; W is O or S; Q is O or S; Y and U are an alkyl, aryl or saccharide radical which is optionally substituted with, for example, an OH, SH or NH group; n is equal to 1 to 4, preferably 1 or 2; and Nu is a radical consisting of a residue of a biologically active compound or the dephosphorylated residue of a compound which is biologically active when it bears a phosphate or phosphonate group.Type: GrantFiled: December 10, 1998Date of Patent: June 4, 2002Assignee: ISIS Pharmaceuticals, Inc.Inventors: Gilles Gosselin, Jean-Louis Imbach, Christian Perigaud
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Patent number: 6399620Abstract: There are described cycloalkyl derivatives of the formula (I) R1—Y—A—B—D—E—F—G (I) in which R1, Y, A, B, D, E, F and G have the meaning indicated herein, their preparation and their use as medicaments. The compounds according to the invention can be used as vitronectin receptor antagonists and as inhibitors of bone resorption.Type: GrantFiled: June 29, 2000Date of Patent: June 4, 2002Assignee: Aventis Pharma S.A.Inventors: Volkmar Wehner, Jochen Knolle, Hans Ulrich Stilz, Jean-Francois Gourvest, Denis Carniato, Thomas Richard Gadek, Robert McDowell, Robert Maurice Pitti, Sarah Catherine Bodary
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Publication number: 20020040014Abstract: Novel FBPase inhibitors of the formula I 1Type: ApplicationFiled: March 7, 2001Publication date: April 4, 2002Applicant: Metabasis Therapeutics, Inc.Inventors: Brett C. Bookser, Qun Dang, K. Raja Reddy