Polycyclo Ring System Having The Diazine Ring As One Of The Cyclos Patents (Class 544/244)
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Publication number: 20030018015Abstract: The present invention relates to novel compounds, compositions and methods for inhibiting the growth, elaboration and/or replication of HIV in human patients and to the prevention and treatment of human acquired immunodeficiency syndrome (AIDS) and other diseases caused by retroviral infection. More particularly, in preferred aspects, the present invention provides a method for the use of novel prodrug forms of 9-(2,3-Dideoxy-&bgr;-D-glycero-pent-2-enofuranosyl)guanine (d4G) for the prevention and treatment of both wild type and drug-resistant Human Immunodeficiency Virus (HIV), the causative pathogen of AIDS.Type: ApplicationFiled: February 5, 2002Publication date: January 23, 2003Inventors: Karen S. Anderson, Adrian Staffin Ray, Chung K. Chu, Yang Zhenjun
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Publication number: 20030008848Abstract: Compound of the formula I, II, III or IV 1Type: ApplicationFiled: December 5, 2001Publication date: January 9, 2003Inventors: Roman Wolfgang Fleck, Terence Alfred Kelly, Jin Mi Kim, Jinbo Lee, Rene Marc Lemieux, Ronald John Sorcek, Jiang-Ping Wu
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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: 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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Publication number: 20020160383Abstract: The present invention pertains to certain nucleic acid analogs and related kits that are useful for the capture, recognition, detection, identification, or quantification of certain chemical or biological entities.Type: ApplicationFiled: October 23, 2001Publication date: October 31, 2002Inventors: Ole Buchardt, Michael Egholm, Peter E. Nielsen, Rolf H. Berg
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Patent number: 6472393Abstract: Compounds having the structure shown below wherein A, B, N1, N2, X, Y, Q, R2, R5 and R6 are as defined herein are useful to inhibit serine protease enzymes, such as TF/factor VIIa factor Xa, thrombin and kallikrein. These compounds may be used in methods of preventing and/or treating clotting disorders.Type: GrantFiled: March 21, 2000Date of Patent: October 29, 2002Assignee: Genentech, Inc.Inventors: Ignacio Aliagas-Martin, Dean R. Artis, Michael S. Dina, John A. Flygare, Richard A. Goldsmith, Regina A. Munroe, Alan G. Olivero, Richard Pastor, Thomas E. Rawson, Kirk D. Robarge, Daniel P. Sutherlin, Kenneth J. Weese, Aihe Zhou, Yan Zhu
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Publication number: 20020156050Abstract: A compound of formula I: 1Type: ApplicationFiled: April 1, 2002Publication date: October 24, 2002Applicant: Guilford Pharmaceuticals Inc.Inventors: Jia-He Li, Jie Zhang
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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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Publication number: 20020151556Abstract: A method and associated compounds for forming nanotubes are disclosed.Type: ApplicationFiled: January 16, 2002Publication date: October 17, 2002Inventor: Hicham Fenniri
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Patent number: 6465649Abstract: Disclosed are methods for the dealkylation of phosphonate esters by use of trimethylchlorosilane as the dealkylating agent. In particular, this invention is directed to the discovery that high yields for the dealkylation of phosphonate esters can be achieved within relatively short reaction times by the use of trimethylchlorosilane provided that the dealkylation procedure occurs in a sealed vessel containing a compatible solvent.Type: GrantFiled: August 17, 2000Date of Patent: October 15, 2002Assignee: Gilead Sciences, Inc.Inventors: Arnold J. Gutierrez, Ernest J. Prisbe, John C. Rohloff
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Publication number: 20020137718Abstract: Nucleozymes containing ribonucleotides and deoxyribonucleotides or nucleic acid analogues are described herein. The nucleozymes have catalytic activity and are significantly more resistant to degradation than their all-RNA ribozyme counterparts. Also described are methods for preparing the nucleozymes along with methods of using nucleozymes, e.g., as therapeutic agents.Type: ApplicationFiled: March 19, 2002Publication date: September 26, 2002Applicant: University of Montreal and Massachusetts Institute of TechnologyInventors: Nassim Usman, Robert J. Cedergren, Jean-Pierre Perreault, Jing-Hua Yang, Alexander Rich
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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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Publication number: 20020132819Abstract: Novel purines and uses of these compounds for the treatment of bone related disorders and cancer is disclosed.Type: ApplicationFiled: December 18, 2000Publication date: September 19, 2002Inventors: Chester A. Metcalf, Manfred Weigele, Tomi K. Sawyer, Regine Bohacek, William C. Shakespeare, Rajeswari Sundaramoorthi, Yihan Wang, David C. Dalgarno
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Patent number: 6452004Abstract: A cyclopentenecarboxamide derivative represented by the formula (I): and a method for preparing the cyclopentencarboxamide derivative. A bicycloamide derivative represented by the formula (II): and a method for preparing the bicycloamide derivative.Type: GrantFiled: July 11, 2000Date of Patent: September 17, 2002Assignee: Kuraray Co., Ltd.Inventors: Nobuya Katagiri, Chikara Kaneko, Junko Sato, Masahiro Torihara, Koichi Kanehira, Yoshin Tamai
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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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Patent number: 6437125Abstract: The invention provides a method of rearranging a compound of formula (I), wherein R and R′ are selected independently from hydrogen and C1-12alkyl; and R1 and R2 are selected independently from hydrogen, hydroxy, halo, C1-12alkyl- or aryl carbonate, amino, mono- or di-C1-12alkylamino, C1-12alkyl or arylamido, C1-12alkyl- or arylcarbonyl, C1-12alkyl- or arylcarboxy, C1-12alkyl- or arylcarbamoyl, C1-12alkyl, C2-12alkenyl, C2-12alkynyl, aryl, heteroaryl, C1-12alkoxy, aryloxy, azido, C1-12alkyl- or arylthio, C1-12alkyl- or arylsulfonyl, C1-12alkyl- or arylsilyl, C1-12alkyl- or arylphosphoryl, and phosphato; to form a compound of formula (II), wherein R, R′, R1 and R2 are as defined for formula (I); said method comprising treating the compound of formula (I) with a palladium (0) catalyst and a (diphenylphosphino)nC1-6 alkane, wherein n is an integer of 1-6. The invention also provides methods of R making penciclovir and famciclovir using this rearrangement reaction.Type: GrantFiled: November 1, 2000Date of Patent: August 20, 2002Assignee: Novartis International Pharmaceutical Ltd.Inventors: Graham Richard Geen, Andrew Colin Share
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Publication number: 20020111333Abstract: Compounds of Formula I and II are disclosed as antagonists of subtype A1 adenosine receptors. These compounds are useful for treatment of various diseases and disorders, including systemic hypertension, renal failure, diabetes, asthma, an edematous condition, congestive heart failure, and renal dysfunction.Type: ApplicationFiled: November 30, 2001Publication date: August 15, 2002Inventors: Ko-Chung Lin, Chi Vu
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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: 20020095033Abstract: Novel monocyclic L-Nucleoside compounds have the general formula 1Type: ApplicationFiled: December 31, 2001Publication date: July 18, 2002Applicant: ICN Pharmaceuticals, Inc.Inventors: Kandasamy Ramasamy, Robert Tam, Devron Averett
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Publication number: 20020068721Abstract: This invention relates to compounds of the general formula: 1Type: ApplicationFiled: December 18, 2000Publication date: June 6, 2002Inventors: Manfred Weigele, Tomi K. Sawyer, Regine Bohacek, William C. Shakespeare, Rajeswari Sundaramoorthi, Yihan Wang, David C. Dalgarno, Chester A. Metcalf
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Patent number: 6399392Abstract: The quenching compounds of the invention are nitrogen-substituted xanthenes that are substituted by one or more aromatic or heteroaromatic quenching moieties. The quenching compounds of the invention exhibit little or no observable fluorescence and efficiently quench a broad spectrum of luminescent compounds. The chemically reactive quenching compounds possess utility for labeling a wide variety of substances, including biomolecules. These labeled substances are highly useful for a variety of energy-transfer assays and applications.Type: GrantFiled: April 21, 2000Date of Patent: June 4, 2002Assignee: Molecular Probes, Inc.Inventors: Richard P. Haugland, Victoria L. Singer, Stephen T. Yue
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Publication number: 20020061896Abstract: The present invention accordingly provides imidazopyrimidine nucleoside compounds of formula (I) 1Type: ApplicationFiled: December 28, 2000Publication date: May 23, 2002Inventors: Arshad Siddiqul, Alex Cimpoia, Patrice Preville
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Publication number: 20020045599Abstract: The invention provides crystalline forms of adefovir dipivoxil and methods to prepare the crystals. The compositions and methods of the present invention have desirable properties for large scale synthesis of crystalline adefovir dipivoxil or for its formulation into therapeutic dosages. Invention compositions include an anhydrous crystal form of adefovir dipivoxil.Type: ApplicationFiled: September 10, 2001Publication date: April 18, 2002Applicant: Gilead Sciences, Inc.Inventors: Murty N. Arimilli, Daphne E. Kelly, Thomas T.K. Lee, Lawrence V. Manes, John D. Munger, Ernest J. Prisbe, Lisa M. Schultze
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Patent number: 6362171Abstract: Antiviral compounds and the water-soluble salts thereof have formula (I), wherein n is from 1 to 8; R1 is selected from the group consisting of (a), wherein m is zero, 1, 2 or 3; and (b), wherein q is from 1 to 20; R2 is independently selected from the group consisting of oxygen and sulfur; R3 is independently selected from the group consisting of hydrogen and hydroxyl; and R4 is selected from the group consisting of hydrogen, hydroxyl and (b); R5 is selected from the group consisting of hydroxyl and (b); R6 is selected from the group consisting of (c), (d) et (e), wherein x is from 1 to 20; provided that one of R1, R4 and R5 is (b) wherein R6 is defined as above; or water soluble salt thereof.Type: GrantFiled: December 9, 1999Date of Patent: March 26, 2002Assignee: Temple University-of the Commonwealth System of Higher EducationInventors: Robert J. Suhadolnik, Wolfgang Pfleiderer
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Patent number: 6362193Abstract: Novel pyridyl or pyrimidinyl substituted cycloalkenyl compounds and compositions for use in therapy.Type: GrantFiled: April 7, 2000Date of Patent: March 26, 2002Assignee: SmithKline Beecham CorporationInventors: Jerry L. Adams, Ravi Garigipati
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Publication number: 20020016309Abstract: The present invention concerns antiviral compounds, their methods of preparation and their compositions, and use in the treatment of viral infections. More particularly, the invention provides imidazopyridine and imidazopyrimidine derivatives (Formula I) for the treatment of respiratory syncytial virus infection.Type: ApplicationFiled: April 23, 2001Publication date: February 7, 2002Inventors: Kuo-Long Yu, Rita L. Civiello, Keith D. Combrink, Hatice Belgin Gulgeze, Ny Sin, Xiangdong Wang, Nicholas A. Meanwell, Brian Lee Venables
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Patent number: 6340754Abstract: The invention relates to a compound of formula (I) Wherein: B is adenine, guanine or hypoxanthine Z is hydrogen or a negative charge R is —[CH2CH(R1)—O]n—R2, —CH2CH2X, in which R1 is hydrogen or (C1-C6) alkyl R2 is hydrogen or (C1-C6) alkyl n is a number from 1 to 6 X is OH, F, NR3R4 R3 and R4 are independently from each other hydrogen or (C1-C6) alkyl and to methods of enzymatically treating these compounds with biocatalysts having cyclic phosphodiesterase activity.Type: GrantFiled: September 18, 2000Date of Patent: January 22, 2002Assignee: Novartis AGInventors: Oreste Ghisalba, Guy Joel Christian Marais, Pierre Martin
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Publication number: 20010049372Abstract: In accordance with the present invention there is provided a nucleoside analogue of formula (I) or (Ia) which is useful as an antiviral agent.Type: ApplicationFiled: June 29, 2001Publication date: December 6, 2001Applicant: BioChem Pharma Inc.Inventor: Nghe Nguyen-Ba
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Patent number: 6316429Abstract: The present invention relates to novel 3-idene-2-indolinone compounds and physiologically acceptable salts thereof which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related cellular disorders such as cancer.Type: GrantFiled: May 7, 1998Date of Patent: November 13, 2001Assignee: Sugen, Inc.Inventors: Peng Cho Tang, Li Sun, Gerald McMahon
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Patent number: 6316620Abstract: A new class of chiral bidentate ligands to transition metals is disclosed which compounds have the following structure: wherein the substituents are as defined herein.Type: GrantFiled: September 5, 2000Date of Patent: November 13, 2001Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventor: Carl A. Busacca
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Publication number: 20010031745Abstract: Chemical compounds comprising nucleoside phosphoramides, their preparation and their therapeutic use in treating viral infections, particularly HIV and HBV are disclosed. The compounds contain a substituted adenine analogue moiety comprising 2-amino-6-(cyclopropylamino)-9H-purin-9-yl. The compounds show both anti-viral activity and acid stability. Salts and esters of the phosphoramidates are included. A representative compound is (1S, 4R), -4-[2-amino-6-(cyclopropylamino)-9H-purin-9-yl]-2-cyclopentene-1-methanol1 O-[phenyl-(methoxy-L-alaninyl)]-phosphate.Type: ApplicationFiled: March 27, 2001Publication date: October 18, 2001Inventors: Christopher McGuigan, Jan Balzarini
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Patent number: 6284748Abstract: Novel purine compounds of the following structure and their use as fructose-1,6-bisphosphatase inhibitors is described.Type: GrantFiled: March 6, 1998Date of Patent: September 4, 2001Assignee: Metabasis Therapeutics, Inc.Inventors: Qun Dang, Mark D. Erion, M. Rami Reddy, Edward D. Robinson, Srinivas Rao Kasibhatla, K. Raja Reddy
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Patent number: 6281201Abstract: Antiviral compounds have the formula wherein m is zero, 1, 2 or 3; n is from 1 to 8, preferably 1, 2 or 3; most preferably 1 or 2; R is independently selected from the group consisting of provided that all R may not be R1 is independently selected from the group consisting of hydroxyl and hydrogen; R2 is independently selected from the group consisting of oxygen and sulfur; or water soluble salts thereof.Type: GrantFiled: December 8, 1999Date of Patent: August 28, 2001Assignee: Temple University- of the Commonwealth System of Higher EducationInventors: Robert J. Suhadolnik, Wolfgang Pfleiderer
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Publication number: 20010012893Abstract: Disclosed are novel prodrugs represented by the following structural formula: 1Type: ApplicationFiled: December 6, 2000Publication date: August 9, 2001Applicant: Drug Innovation & Design, Inc.Inventors: Arnold Glazier, Milka Yanachkova, Ivan Yanachkov
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Patent number: 6245910Abstract: Purine derivatives in which a desired substituent is introduced into the 9-position only are synthesized by first introducing an easily-removable substituent in the 7-position of a purine base of natural purine nucleosides obtained through fermentation or derivatives thereof, then hydrolyzing the ribose moiety to form purine derivatives having the substituent in the 7-position, subsequently introducing the desired substituent in the 9-position, and then removing the substituent in the 7-position.Type: GrantFiled: October 27, 1999Date of Patent: June 12, 2001Assignee: Ajinomoto Co., Inc.Inventors: Kunisuke Izawa, Hiroshi Shiragami, Keizo Yamashita
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Patent number: 6214811Abstract: Disclosed are novel prodrugs represented by the following structural formula; Z is oxygen or sulfur; Y is, together with a hydroxy group, acyclovir or an analog of acyclovir; A is a substituted benzyl group with one or more protected hydroxy or protected amine groups in the ortho or para positions, relative to the phosphate ester, which can be converted in vivo to a hydroxy or amino group. Also disclosed is a method of treating a viral infection in an individual or animal. The method comprises administering to the individual or animal a therapeutically effective amount of a prodrug represented by structural formula shown above.Type: GrantFiled: February 28, 2000Date of Patent: April 10, 2001Assignee: Drug Innovation & Design, Inc.Inventors: Arnold Glazier, Milka Yanachkova, Ivan Yanachkov
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Patent number: 6197777Abstract: A method and composition for the treatment of HIV infection, HBV infection, or abnormal cellular proliferation in humans and other host animals is disclosed that includes the administration of an effective amount of a 1,3-oxaselenolane nucleoside or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable carrier.Type: GrantFiled: March 3, 2000Date of Patent: March 6, 2001Assignees: Emory University, The University of Georgia Research Foundation, Inc.Inventors: Raymond F. Schinazi, Chung K. Chu, Jinfa Du
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Patent number: 6194576Abstract: Nucleotide analogues having the general formula (I) and pharmaceutically acceptable derivatives: wherein n is 0 or an integer; X is O or S, CH2, CH-halogen, CH—N3, or C═CH2; Q and U are independently selected from: O, S, and CH(Ra) wherein Ra is hydrogen, OH, halogen, N3 ,NH2, SH, carboxyl, C1-6 alkyl or Ra is CH2(Rb) wherein Rb is hydrogen, OH, SH, NH2, C1-6 alkyl or carboxyl; or both Q and U are CH when Q and U are linked by a double bond; Z is selected from: O, a C1-6 alkoxy, a C1-6 thioalkyl, a C1-6 aminoalkyl, (CH2)m wherein m is 0 or an integer, and N(Rc)2 wherein both Rc are independently hydrogen or a C1-6 alkyl; and R2 is a purine or pyrimidine base or an analogue or derivative thereof. Members of this series of analogues possess anti-viral activity.Type: GrantFiled: October 4, 1999Date of Patent: February 27, 2001Assignee: BioChem Pharma, Inc.Inventors: Nghe Nguyen-Ba, Miguel Quimpere, Laval Chan Chun Kong, William L. Brown, Gervais Dionne
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Patent number: 6194398Abstract: A phosphonate nucleotide compound represented by formula (I): (wherein R1 is a C1-C6 alkyl group or the like, R2 is a hydrogen atom, a C1-C4 alkyl group substituted by one or more halogen atoms or the like, R3 is a hydrogen atom, a C1-C4 alkyl group substituted by one or more halogen atoms or the like, R4 is a hydrogen atom, a C1-C4 alkyl group substituted by one or more halogen atoms and X is a carbon atom or a nitrogen atom), a salt thereof, a hydrate thereof or a solvate thereof, as well as a medicament containing the same. It is useful as an antiviral agent for human immunodeficiency virus, herpes simplex virus, hepatitis B virus or the like and as an antitumor agent.Type: GrantFiled: June 17, 1999Date of Patent: February 27, 2001Assignee: Mitsubishi Chemical CorporationInventors: Masaru Ubasawa, Kouichi Sekiya, Hideaki Takashima, Naoko Ueda, Satoshi Yuasa, Naohiro Kamiya
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Patent number: 6187914Abstract: The invention relates to nucleoside derivatives bearing electrolabile protector groupings and their use in an oligonucleotide synthesis method comprising at least one step of electronic deprotection.Type: GrantFiled: December 3, 1998Date of Patent: February 13, 2001Assignee: Cis Bio InternationalInventors: Robert Teoule, André Roget, Thierry Livache
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Patent number: 6180790Abstract: Disclosed are novel prodrugs represented by the following structural formula: Z is oxygen or sulfur; Y is, together with a hydroxy group, acyclovir or an analog of acyclovir; A is a substituted benzyl group with one or more protected hydroxy or protected amine groups in the ortho or para positions, relative to the phosphate ester, which can be converted in vivo to a hydroxy or amino group. Also disclosed is a method of treating a viral infection in an individual or animal. The method comprises administering to the individual or animal a therapeutically effective amount of a prodrug represented by structural formula shown above.Type: GrantFiled: December 10, 1999Date of Patent: January 30, 2001Assignee: Drug Innovation and Design, Inc.Inventors: Arnold Glazier, Milka Yanachkova, Ivan Yanachkov
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Patent number: 6177379Abstract: A method of initiating free-radical addition polymerization, which entails effecting a free-radical addition polymerization in the presence of an initiator, which contains, as a structural feature, a Diels-Alder adduct of an azo group (—N═N—) with a conjugated double bond (diene).Type: GrantFiled: May 18, 1998Date of Patent: January 23, 2001Assignee: BASF AktiengesellschaftInventors: Rainer Königer, Reinhold Schwalm, Roman Benedikt Raether
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Patent number: 6156739Abstract: Phosphate derivatives are disclosed of quinazolinone compounds having structural formula (I) or a pharmaceutically acceptable salt thereof, wherein X' represent hydroxyl, alkyl, alkoxy, or O--Z where Z is a phosphate or phosphate derivative; Y' represents hydrogen, alkyl or an optionally substituted aryl group or optionally substituted aralkyl group; and R' is hydrogen, alkyl, or CH.sub.2 --O--Z where Z is again a phosphate or phosphate derivative; subject to the proviso that if neither X' nor R' contains Z, Y' is an aryl or aralkyl group having an O--Z substituent therein with Z once again being a phosphate or phosphate derivative as hereinabove defined. These compounds are useful as prodrugs for providing active PARP inhibiting substances for medical use in conjunction with a cytotoxic drug or radiotherapy in order to increase the effectiveness of the latter, especially in connection with antitumor treatment.Type: GrantFiled: July 29, 1999Date of Patent: December 5, 2000Assignee: Newcastle University Ventures LimitedInventors: Roger John Griffin, Alan Hilary Calvert, Jane Nicola Curtin, David Richard Newell, Bernard Thomas Golding
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Patent number: 6150370Abstract: Disclosed are compounds which are inhibitors of metalloproteases having the following structure: ##STR1## where Ar, W, X, Y, Z, R.sub.1 and R.sub.2 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 26, 1997Date of Patent: November 21, 2000Assignee: The Procter & Gamble CompanyInventors: Stanislaw Pikul, Kelly Lynn McDow-Dunham, Neil Gregory Almstead, Biswanath De, Michael George Natchus, Yetunde Olabisi Taiwo