Nitrogen Atoms Occupy 1 And 3- Positions Patents (Class 514/86)
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Patent number: 6787525Abstract: The invention relates to glyceryl nucleotides of the formula Ia in which a) one of the radicals A1, A2 and A3 is a hydrogen atom or a radical selected from hydroxyl, mercapto, alkyl, alkenyl, polyoxyalkenyl, aryl, acyl, alkyloxy, alkenyloxy, polyoxyalkenyloxy, acyloxy, aryloxy, alkylthio, alkenylthio, acylthio and arylthio, where the alkyl, alkenyl and acyl radicals are optionally substituted by from 1 to 3 aryl radicals; and b1) two of the remaining radicals A1, A2 and A3 are two nucleoside groups which are different from each other; or b2) one of the remaining radicals A1, A2 and A3 is a nucleoside group and the other of the remaining radicals is a hydroxycarbonyl group, where at least one of the nucleoside groups is not a naturally occurring nucleoside group; to processes for preparing these compounds, to pharmaceutical remedies which comprise these compounds, and to the use of these compounds for treating cancer diseases and infectious diseases.Type: GrantFiled: September 12, 2001Date of Patent: September 7, 2004Inventors: Herbert Schott, Peter Stephan Ludwig
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Publication number: 20040171577Abstract: Aryl phosphate derivatives of d4T with para-bromo substitution on the aryl group show markedly increased potency as anti-HIV agents without undesirable levels of cytotoxic activity. In particular, these derivatives are potent inhibitors of HIV reverse transcriptase. In a preferred aspect of the present invention, the phosphorus of the aryl phosphate group is further substituted with an amino acid residue that may be esterified or substituted, such as a methoxy alaninyl group.Type: ApplicationFiled: December 1, 2003Publication date: September 2, 2004Applicant: Parker Hughes InstituteInventors: Fatih M. Uckun, Rakesh Vig
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Publication number: 20040167140Abstract: 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: January 16, 2004Publication date: August 26, 2004Applicant: Emory UniversityInventors: Raymond F. Schinazi, Dennis C. Liotts
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Patent number: 6756391Abstract: The present invention is drawn to novel antiviral compounds, pharmaceutical compositions and their use. More specifically this invention is drawn to derivatives of monocyclic polyamines which have activity in standard tests against HIV-infected cells as well as other biological activity related to binding of ligands to chemokine receptors that mediate a number of mammalian embryonic developmental processes.Type: GrantFiled: May 9, 2002Date of Patent: June 29, 2004Assignee: AnorMed, Inc.Inventors: Gary James Bridger, Eva Maria Boehringer, Zhongren Wang, Dominique Schols, Renato Tony Skerlj, David Earl Bogucki
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Patent number: 6750340Abstract: The present invention is directed to particular bisphosphonate compounds, and in particular, to bisphosphonate conjugates that are useful in the treatment of soft tissues surrounding bone and bone-related diseases, such as bone cancer and osteoporosis.Type: GrantFiled: December 7, 2000Date of Patent: June 15, 2004Assignee: MBC Research, Inc.Inventors: Nelly Padioukova, Sergey Mikhailov, H. B. F. Dixon, Grigorii Tzeitline
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Patent number: 6747036Abstract: The present invention provides a novel method for treating leukemia and more particularly acute myelogenous leukemia (AML) in a host comprising administering to the host a therapeutically effective amount of a compound having the formula I: wherein B is cytosine or 5-fluorocytosine and R is selected from the group comprising H, monophosphate, diphosphate, triphosphate, carbonyl substituted with a C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C6-10 aryl, and wherein each Rc is independently selected from the group comprising H, C1-6 alkyl, C2-6 alkynyl, C2-6 alkynyl and an hydroxy protecting group; and wherein said compound is substantially in the form of the (−) enantiomer.Type: GrantFiled: January 16, 2002Date of Patent: June 8, 2004Assignee: BioChem Pharma Inc.Inventors: Henriette Gourdeau, Francis J. Giles
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Patent number: 6723711Abstract: A compound of the structure A method for the inhibition of the binding of &agr;4&bgr;1 integrin to its receptors, for example VCAM-1(vascular cell adhesion molecule-1) and fibronectin; pharmaceutically active compositions comprising these compounds; and the use of these compounds for the control or prevention of diseases states in which &agr;4&bgr;1 is involved are also disclosed.Type: GrantFiled: October 9, 2001Date of Patent: April 20, 2004Assignee: Texas Biotechnology CorporationInventors: Ronald J. Biediger, Brian Dupre, Linda K. Hamaker, George W. Holland, Jamal M. Kassir, Wen Li, Robert V. Market, Noel Nguyen, Ian L. Scott, Chengde Wu, E. Radford Decker
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Patent number: 6723712Abstract: The invention relates to an antiviral agent for use in combination with an anticancer agent, for the treatment of cancer. Especially, the invention provides means for the treatment of non-virus-associated cancer.Type: GrantFiled: May 2, 2002Date of Patent: April 20, 2004Assignees: Institut Gustave Roussy, Universite Paris-SUD XIInventors: Jean Bourhis, Bassam Abdulkarim, Eric Deutsch
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Publication number: 20040063668Abstract: The present invention relates to an acyclic nucleoside phosphonate derivative which is useful as an antiviral agent (particularly, against hepatitis B virus), pharmaceutically acceptable salts, stereoisomers, and a process for the preparation thereof.Type: ApplicationFiled: June 18, 2003Publication date: April 1, 2004Inventors: Jong-Ryoo Choi, Jeong-Min Kim, Kee-Yoon Roh, Dong-Gyu Cho, Jae-Hong Lim, Jae-Taeg Hwang, Woo-Young Cho, Hyun-Sook Jang, Chang-Ho Lee, Tae-Saeng Choi, Chung-Mi Kim, Yong-Zu Kim, Tae-Kyun Kim, Seung-Joo Cho, Gyoung-Won Kim
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Patent number: 6706698Abstract: The present invention relates to novel &agr;-substituted-&bgr;-aminoethylphosphonate and &agr;-substituted-&bgr;-aminovinylphosphonate derivatives and their uses for lowering plasma levels of apo (a), Lp(a), apo B, apo B associated lipoproteins (low density lipoproteins and very low density lipoproteins) and for lowering plasma levels of total cholesterol.Type: GrantFiled: September 26, 2001Date of Patent: March 16, 2004Assignee: Ilex Products, Inc.Inventors: Hieu Trung Phan, Lan Mong Nguyen, Vinh Van Diep, Raymond Azoulay, Harald Eschenhof, Eric Joseph Niesor, Craig Leigh Bentzen, Robert John Ife
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Patent number: 6703396Abstract: A process for the resolution of a racemic mixture of nucleoside enantiomers that includes the step of exposing the racemic mixture to an enzyme that preferentially catalyzes a reaction in one of the enantiomers. The nucleoside enantiomer (−)-2-hydroxymethyl-5-(5-flurocytosin-1-yl)-1,3-oxathiolane is an effective antiviral agent against HIV, HBV, and other viruses replicating in a similar manner.Type: GrantFiled: March 13, 1995Date of Patent: March 9, 2004Assignee: Emory UniversityInventors: Dennis C. Liotta, Raymond F. Schinazi, Woo-Baeg Choi
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Publication number: 20040014723Abstract: Novel calcilytic compounds and methods of using them are provided.Type: ApplicationFiled: April 24, 2003Publication date: January 22, 2004Inventors: Pradip Bhatnagar, William M Bryan, James F Callahan, William F Huffman
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Publication number: 20040014722Abstract: Compounds represented by the formula: 1Type: ApplicationFiled: May 14, 2003Publication date: January 22, 2004Applicant: BIOCRYST PHARMACEUTICALS, INC.Inventors: Yarlagadda S. Babu, Pooran Chand, Yahya El-Kattan, Minwan Wu
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Publication number: 20040006040Abstract: A method for the identification and treatment of pathogenic microorganism infections by inhibiting one or more enzymes in a metabolic pathway by inhibiting the conversion of substrate to produce the penultimate or ultimate product particularly by inhibiting the activity of one or more of the enzymes in the pathway, and compounds and pharmaceutical compositions for inhibiting infections of pathogenic microorganisms by inhibiting such enzymes.Type: ApplicationFiled: February 14, 2003Publication date: January 8, 2004Applicant: Pyro Pharmaceuticals, Inc.Inventor: Alan M. Schechter
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Patent number: 6670342Abstract: A method for the treatment for hepatitis delta infection in a host, that includes administering an effective amount of a nucleoside or a nucleoside analog that suppresses the expression of the hepatitis B surface or preS1 antigen in the host 100-fold or more relative to pretreatment values in vivo; or to not more than 1 microgram per milliliter in vivo. In a preferred embodiment, the nucleoside is L-FMAU, or a pharmaceutically acceptable salt or prodrug thereof.Type: GrantFiled: March 29, 2001Date of Patent: December 30, 2003Assignees: Georgetown University, Cornell Research Foundation, Inc., University of Georgia Research Foundation, Inc.Inventors: John L. Casey, Brent E. Korba, Paul J. Cote, John L. Gerin, Bud C. Tennant, Chung K. Chu
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Publication number: 20030236218Abstract: Methods and compositions for treating ADV infections and HIV/ADV co-infections by administering an aryl phosphate derivative of d4T having an electron withdrawing substituent on the aryl group and an amino acid substituent on the phosphate group are described. Preferred aryl phosphate derivatives of d4T are d4T-5′-[p-bromophenyl methoxyalaninyl phosphate] and d4T-5′-[p-chlorophenyl methoxyalaninyl phosphate].Type: ApplicationFiled: October 25, 2002Publication date: December 25, 2003Inventor: Fatih M. Uckun
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Patent number: 6653296Abstract: Resolved enantiomers of the formula (IA) and (IB) wherein B is a purine or pyrimidine base or aza and/or deaza analogs thereof are useful in antiviral pharmaceutical compositions to treat retroviral infections.Type: GrantFiled: February 2, 1995Date of Patent: November 25, 2003Assignees: Institute of Organic Chemistry and Biochemistry of the Academy of Sciences of the Czech Republic, Rega Stichting v.z.w.Inventors: Antonin Holy, Hana Dvorakova, Erik Desire Alice De Clercq, Jan Marie Rene Balzarini
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Patent number: 6645972Abstract: The present invention provides a novel method for treating leukemia in a host that has been previously treated with a Bcr-Abl tyrosine kinase inhibitor comprising administering to the host a therapeutically effective amount of a compound having the formula I: wherein B is cytosine or 5-fluorocytosine and R is selected from H, monophosphate, diphosphate, triphosphate, carbonyl substituted with a C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C6-10 aryl, and and where in each Rc is independently selected from the group comprising H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl an hydroxy protecting group.Type: GrantFiled: November 4, 2002Date of Patent: November 11, 2003Assignee: Shire BioChem Inc.Inventors: Jacques Jolivet, Francis Giles, Hagop Kantarjian
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Patent number: 6642245Abstract: A method and composition for the treatment of HIV and HBV infections in humans is disclosed that includes administering an effective amount of 2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane, 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. A process for the resolution of a racemic mixture of nucleoside enantiomers is also disclosed that includes the step of exposing the racemic mixture to an enzyme that preferentially catalyzes a reaction in one of the enantiomers.Type: GrantFiled: June 7, 1995Date of Patent: November 4, 2003Assignee: Emory UniversityInventors: Dennis C. Liotta, Raymond F. Schinazi, Woo-Baeg Choi
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Publication number: 20030191074Abstract: A compound which comprises a backbone having a plurality of chiral carbon atoms, the backbone bearing a plurality of ligands each being individually bound to a chiral carbon atom of the plurality of chiral carbon atoms, the ligands including one or more pair(s) of adjacent ligands each containing a moiety selected from the group consisting of a naturally occurring nucleobase and a nucleobase binding group, wherein moieties of the one or more pair(s) are directly linked to one another via a linker chain; building blocks for synthesizing the compound; and rises of the compound, particularly in antisense therapy.Type: ApplicationFiled: January 29, 2002Publication date: October 9, 2003Applicant: Bio-Rad Laboratories Inc.Inventor: David Segev
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Patent number: 6630480Abstract: The present invention provides a novel method for treating leukemia and more particularly acute myelogenous leukemia (AML) in a host comprising administering to the host a therapeutically effective amount of a compound having the formula I: wherein B is cytosine or 5-fluorocytosine and R is selected from the group comprising H, monophosphate, diphosphate, triphosphate, carbonyl substituted with a C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C6-10 aryl, and wherein each Rc is independently selected from the group comprising H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl and an hydroxy protecting group; and wherein said compound is substantially in the form of the (−) enantiomer.Type: GrantFiled: March 28, 2000Date of Patent: October 7, 2003Assignee: Biochem Pharma Inc.Inventors: Henriette Gourdeau, Francis J. Giles
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Publication number: 20030186928Abstract: The present invention is directed to a method of reducing intraocular pressure. The method comprises administering to a subject a pharmaceutical composition comprising an effective amount of a purinerginic receptor ligand, which is a mononucleoside polyphosphate or dinucleoside polyphosphate defined by general Formula I. The method of the present invention is useful in the treatment or prevention of ocular hypertension, such as glaucoma, including primary and secondary glaucoma. The method can be used alone to reduce intraocular pressure. The method can also be used in conjunction with other therapeutic agents or adjunctive therapy commonly used to treat glaucoma to enhance the therapeutic effect of reducing the intraocular pressure.Type: ApplicationFiled: January 15, 2003Publication date: October 2, 2003Inventors: Benjamin R. Yerxa, Robert Plourde, Edward G. Brown, Ward M. Peterson
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Patent number: 6620796Abstract: The invention provides new methods for synthesis of nucleotide-based compounds and new libraries of such compounds. Compounds of the invention are useful for a variety of therapeutic applications, including treatment of viral or bacterial infections and associated diseases and disorders.Type: GrantFiled: November 8, 2000Date of Patent: September 16, 2003Assignee: Micrologix Biotech Inc.Inventors: Wenqiang Zhou, Yi Jin, Arlene Roland, Radhakrishnan Iyer
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Patent number: 6613773Abstract: The invention provides fungicidal compounds of formula (I) or stereoisomers thereof: wherein X is CH2O; A is hydrogen; E is hydrogen; q is 1; any two of K, L and M are nitrogen and the other is CH; T is oxygen or sulfur; and Z is an optionally substituted phenyl group or an optionally substituted heterocyclyl group.Type: GrantFiled: March 5, 2002Date of Patent: September 2, 2003Assignee: Syngenta LimitedInventors: John Martin Clough, Christopher Richard Ayles Godfrey, Ian Thomas Streeting, Rex Cheetham, Paul John de Fraine, David Bartholomew, James John Eshelby
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Publication number: 20030158147Abstract: The present invention is directed to a method of treating pain. The method comprises administering to a subject a pharmaceutical composition comprising an effective amount of a P2X receptor antagonist. The methods of the present invention are useful in reducing pain, such as traumatic pain, neuropathic pain, organ pain and pain associated with diseases. The P2X receptor antagonists particularly useful for this invention are mononucleoside polyphosphate derivatives or dinucleoside polyphosphate derivatives of general Formula I. The compounds of the present method can be used alone to treat pain. The compounds of the present method can also be used in conjunction with other therapeutic agents or adjunctive therapies commonly used to treat pain, thus enhancing the overall pain-reducing effect in a subject in need of such treatment.Type: ApplicationFiled: January 31, 2003Publication date: August 21, 2003Inventors: Benjamin R. Yerxa, Ward M. Peterson, Christopher S. Crean
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Patent number: 6605602Abstract: Provided are oligonucleotides for the quantitation of BK virus (BKV) viral loads in a sample and methods for the diagnosis and management of BKV-associated nephropathy using PCR or QPCR methods. In addition, a PCR method for quantitating the BKV viral load in urine, serum and tissue using the described nucleic acid primers is also disclosed. Furthermore, a method for the management of BKV-associated nephropathy in renal transplant recipients using cidofovir is disclosed. Lastly, a kit is provided containing the described PCR for use in diagnosing and managing BKV-associated nephropathy.Type: GrantFiled: September 10, 2002Date of Patent: August 12, 2003Assignee: University of Pittsburgh-of the Commonwealth System of Higher EducationInventor: Abhay N. Vats
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Publication number: 20030134808Abstract: Novel oligomers, and synthesis thereof, comprising one or more bi-, tri, or polycyclic nucleoside analogues are disclosed herein. The nucleoside analogues have a “locked” structure, termed Locked Nucleoside Analogues (LNA). LNA's exhibit highly desirable and useful properties. LNA's are capable of forming nucleobase specific duplexes and triplexes with single and double stranded nucleic acids. These complexes exhibit higher thermostability than the corresponding complexes formed with normal nucleic acids. The properties of LNA's allow for a wide range of uses such as diagnostic agents and therapeutic agents in a mammal suffering from or susceptible to, various diseases.Type: ApplicationFiled: November 5, 2001Publication date: July 17, 2003Inventor: Jesper Wengel
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Publication number: 20030120071Abstract: Aryl substituted phosphoryl derivatives of the formula 1Type: ApplicationFiled: August 12, 2002Publication date: June 26, 2003Inventors: Christopher McGuigan, Jan Balzarini
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Publication number: 20030087873Abstract: The disclosed invention is a composition for and a method of treating a Flaviviridae (including BVDV and HCV), Orthomyxoviridae (including Influenza A and B) or Paramyxoviridae (including RSV) infection, or conditions related to abnormal cellular proliferation, in a host, including animals, and especially humans, using a nucleoside of general formula (I)-(XXIII) or its pharmaceutically acceptable salt or prodrug.Type: ApplicationFiled: October 18, 2001Publication date: May 8, 2003Inventors: Lieven Stuyver, Kyoichi Watanabe
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Publication number: 20030083316Abstract: In accordance with the present invention there is provided a pharmaceutical combination useful for the treatment of cancer comprising at least one active compound of formula (I): 1Type: ApplicationFiled: March 25, 2002Publication date: May 1, 2003Applicant: Shire BioChem Inc.Inventors: Francis Giles, Hagpop Kantarjian, Jacques Jolivet
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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: 20030069210Abstract: N-Heterocyclic derivatives of the formula (I): 1Type: ApplicationFiled: April 12, 2002Publication date: April 10, 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: 20030013660Abstract: Dioxolane analogs of the following formula: 1Type: ApplicationFiled: October 15, 2001Publication date: January 16, 2003Applicant: Shire BioChem Inc.Inventors: Giorgio Attardo, Boulos Zacharie, Rabindra Rej, Jean-Francois Lavallee, Louis Vaillancourt, Real Denis, Sophie Levesque
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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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Patent number: 6495553Abstract: This invention provides a method for identifying potential therapeutic agents by contacting a target cell with a candidate therapeutic agent which is a selective substrate for an endogenous, intracellular enzyme in the cell which is enhanced in its expression as a result of selection by biologic or chemotherapy. This invention also provides methods and examples of molecules for selectively killing a pathological cell by contacting the cell with a prodrug that is a selective substrate for an endogenous, intracellular enzyme. The prodrug is subsequently converted to a cellular toxin. Further provided by this invention is a method for treating a pathology characterized by pathological, hyperproliferative cells in a subject by administering to the subject a prodrug that is a selective substrate for an endogenous, overexpressed, intracellular enzyme, and converted by the enzyme to a cellular toxin in the hyperproliferative cell.Type: GrantFiled: August 7, 1998Date of Patent: December 17, 2002Assignee: NewBiotics, Inc.Inventor: H. Michael Shepard
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Publication number: 20020165203Abstract: N-Heterocyclic derivatives of the formula (I): 1Type: ApplicationFiled: April 12, 2002Publication date: November 7, 2002Applicant: 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: 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: 20020151519Abstract: This invention provides methods for treating inflammatory or autoimmune diseases by contacting the affected cell or tissue with a therapeutic compound as described herein. Such pathologies include, but are not limited to rheumatoid arthritis, systemic lupus erythmatosus, psoriatic arthritis, reactive arthritis, Crohn's disease, ulcerative colitis and scleroderma. Therapeutic compounds useful in the methods of this invention are selected from the group consisting of a 1,5-substituted pyrimidine derivative or analog and substituted furano-pyrimidone analog.Type: ApplicationFiled: January 18, 2002Publication date: October 17, 2002Inventor: H. Michael Shepard
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Publication number: 20020147175Abstract: This invention provides compositions containing an effective amount of a novel substrate compound that selectively inhibit the proliferation of hyperproliferative cells, for example, pathological cells that endogenously overexpress a target enzyme that confers resistance to biologic and chemotherapeutic agents and an effective amount of a nucleoside transport antagonistic agents. Further provided by this invention is a method for treating a subject by delivering to the subject the composition as described herein. The compositions of this invention may be used alone or in combination with other chemotherapeutics or alternative anti-cancer therapies such as radiation.Type: ApplicationFiled: November 16, 2001Publication date: October 10, 2002Inventors: H. Michael Shepard, Christopher Boyer
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Publication number: 20020137726Abstract: Methods for increasing the elimination half-life of key metabolites such as d4T by administering an aryl phosphate derivative of d4T having an electron withdrawing substituent on the aryl group and an amino acid substituent on the phosphate group are described. A preferred aryl phosphate derivative of d4T is HI-113 (d4T-5′-[p-bromophenyl methoxyalaninyl phosphate]). The administration of HI-113 results in more prolonged systemic exposure to the key metabolites, Ala-d4T-MP and d4T, than administration of an equimolar dose of either metabolite. Each metabolite has a significantly longer elimination half life when formed in vivo from the administration of HI-113 than when the metabolite is administered directly.Type: ApplicationFiled: October 19, 2001Publication date: September 26, 2002Inventors: Fatih M. Uckun, Chun-Lin Chen, Taracad K. Venkatachalam, Zhoa-Hai Zhu
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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: 20020128224Abstract: The present invention is directed to a method of reducing intraocular pressure. The method comprises administering to a subject a pharmaceutical composition comprising an effective amount of a nucleoside 5′-pyrophosphate pyranoside or analogue, which is defined by general Formula I. The method of the present invention is useful in the treatment or prevention of ocular hypertension, such as found in glaucoma, including primary and secondary glaucoma. The method can be used alone to reduce intraocular pressure. The method can also be used in conjunction with another therapeutic agent or adjunctive therapy commonly used to treat glaucoma to enhance the therapeutic effect of reducing the intraocular pressure. The present invention also provides a novel composition comprising a nucleoside 5′-pyrophosphate pyranoside or analogues.Type: ApplicationFiled: February 27, 2002Publication date: September 12, 2002Inventors: Jose L. Boyer, Benjamin R. Yerxa, Robert Plourde, Edward G. Brown
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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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Publication number: 20020107225Abstract: The present invention provides a novel method for treating leukemia and more particularly acute myelogenous leukemia (AML) in a host comprising administering to the host a therapeutically effective amount of a compound having the formula I: 1Type: ApplicationFiled: January 16, 2002Publication date: August 8, 2002Applicant: BioChem Pharma Inc.Inventors: Henriette Gourdeau, Francis J. Giles
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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: 20020091104Abstract: The invention encompasses the novel class of compounds represented by the formula below, which are inhibitors of the PTP-1B enzyme.Type: ApplicationFiled: March 21, 2001Publication date: July 11, 2002Inventors: Chung Sing Li, Christopher Bayly, Jacques Yves Gauthier, Yves Leblanc, Cheuk Kun Lau, Patrick Roy, Michel Therien, Zhaoyin Wang, Claude Dufresne, Rejean Fortin
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Patent number: 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: 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