Adenine Or Substituted Adenine Patents (Class 536/26.13)
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Patent number: 11707531Abstract: Disclosed are compounds and compositions for the activation or induction of expression of a pattern recognition receptor (e.g., STING, RIG-I, MDA5), and methods of use thereof.Type: GrantFiled: September 11, 2018Date of Patent: July 25, 2023Assignee: F-star Therapeutics, Inc.Inventor: Radhakrishnan P. Iyer
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Patent number: 11666594Abstract: The present disclosure provides a compound having a STING agonistic activity, which may be expected to be useful as an agent for the prophylaxis or treatment of STING-related diseases. The present disclosure relates to a compound represented by the formula (I): wherein each symbol is as defined in the description, or a salt thereof.Type: GrantFiled: October 7, 2020Date of Patent: June 6, 2023Assignee: Takeda Pharmaceutical Company LimitedInventors: Masato Yoshikawa, Morihisa Saitoh, Taisuke Kato, Yayoi Nakayama, Tomohiro Seki, Yasuo Nakagawa, Yusuke Tominari, Masaki Seto, Yusuke Sasaki, Masanori Okaniwa, Tsuneo Oda, Akito Shibuya, Kosuke Hidaka, Zenyu Shiokawa, Shumpei Murata, Atsutoshi Okabe, Yoshihisa Nakada, Michiyo Mochizuki, Brian Scott Freeze, Taisuke Tawaraishi, Yasufumi Wada, Paul D. Greenspan
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Patent number: 8927521Abstract: Provided herein are methods of reducing adhesion formation in a subject, for example, post-surgical abdominal and pelvic adhesions. The methods include the step of administering to the subject in need thereof a compound chosen from 2?,3?-cyclic adenosine monophosphate, analogs thereof, and pharmaceutically acceptable salts thereof, able to reduce the formation of adhesions in a subject as compared to adenosine monophosphate, in an amount effective to reduce adhesions.Type: GrantFiled: November 5, 2009Date of Patent: January 6, 2015Assignee: University of Pittsburgh—of the Commonwealth System of Higher EducationInventor: Edwin Kerry Jackson
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Patent number: 8889650Abstract: An antimelancholic pharmaceutical composition or health products prepared with jujuba cAMP materials and a preparative method are provided in the present invention. The present pharmaceutical composition includes jujuba cAMP as a solo effective ingredient for treating the depression. The present method for preparing the jujuba cAMP includes chromatographing a jujuba extract with a macroporous resin bound with an aldehyde group.Type: GrantFiled: November 30, 2007Date of Patent: November 18, 2014Assignees: Beijing Wonner Biotech, Ltd. Co.Inventor: Zuoguang Zhang
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Patent number: 8889125Abstract: The present invention relates to a method of treatment and/or ameliorating the symptoms of Huntington's disease comprising the step of administering an effective amount of adenosine triphosphate, co-carboxylase, nicotinamide, and cyanocobalamin in a physiologically acceptable carrier to an individual in need thereof. Preferably, the administration is via intramuscular injection.Type: GrantFiled: March 15, 2013Date of Patent: November 18, 2014Assignee: Genix Therapeutics Group, LLCInventor: Ragab El-Rashidy
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Patent number: 8877731Abstract: Disclosed herein are nucleosides, nucleotides and analogs thereof, pharmaceutical compositions that include one or more of nucleosides, nucleotides and analogs thereof, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a disease and/or a condition, including an infection from a paramyxovirus and/or an orthomyxovirus, with a nucleoside, a nucleotide and an analog thereof. Examples of viral infections include a respiratory syncytial viral (RSV) and influenza infection.Type: GrantFiled: September 19, 2011Date of Patent: November 4, 2014Assignee: Alios Biopharma, Inc.Inventors: Leonid Beigelman, Jerome Deval, David Bernard Smith, Guangyi Wang, Vivek Kumar Rajwanshi
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Publication number: 20140212382Abstract: The present invention is directed to compounds, compositions and methods for treating or preventing viral infections using nucleoside analog monophosphate prodrugs. More specifically, HCV, Norovirus, Saporovirus, Dengue virus, Chikungunya virus and Yellow fever in human patients or other animal hosts. The compounds are certain 2,6-diamino 2-C-methyl purine nucleoside monophosphate prodrugs and modified prodrug analogs, and pharmaceutically acceptable, salts, prodrugs, and other derivatives thereof. In particular, the compounds show potent antiviral activity against HCV, Norovirus, Saporovirus, Dengue virus, Chikungunya virus and Yellow fever. This invention teaches how to modify the metabolic pathway of 2,6-diamino 2?-C-methyl purine and deliver nucleotide triphosphate(s) to polymerases at heretofore unobtainable therapeutically-relevant concentrations.Type: ApplicationFiled: May 16, 2012Publication date: July 31, 2014Applicants: EMORY UNIVERSITY, RFS PHARMA, LLCInventors: Raymond F. Schinazi, Jong Hyun Cho, Longhu Zhou, Hongwang Zhang, Ugo Pradere, Steven J. Coats
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Publication number: 20140206024Abstract: The present invention provides for stable nicotinamide adenine dinucleotide (NAD/NADH) and nicotinamide adenine dinucleotide phosphate (NADP/NADPH) derivatives of formula (I), enzyme complexes of these derivatives and their use in biochemical detection methods and reagent kits.Type: ApplicationFiled: March 23, 2014Publication date: July 24, 2014Applicant: ROCHE DIAGNOSTICS OPERATIONS, INC.Inventors: Dieter Heindl, Joachim Hoenes, Carina Horn, Claudia Gaessler-Dietsche
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Patent number: 8785619Abstract: This invention relates to n-alkylated synthetic nucleosides and phosphoramidites of high regio-specific purity and stability and for selective deprotection of the protecting group in oligonucleotides for the purpose of synthesis of high purity selectively n-alkylated sequence specific DNA and RNA. Such oligonucleotides are useful for study of mechanism of cytotoxic and mutagenic DNA damage, detection and reversal of cellular cytotoxic and mutagenic damages that occurs from the incorporation of methylated nucleosides, the corresponding phosphates and triphosphates and their precursors, via de novo DNA synthesis. The reagents could be extremely valuable tools as diagnostics and mutagenic reversal reagents.Type: GrantFiled: December 20, 2004Date of Patent: July 22, 2014Assignee: ChemGenes CorporationInventors: Sant K. Srivastav, Suresh C. Srivastava, Satya P Bajpai
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Patent number: 8772474Abstract: Disclosed herein are cyclic nucleotide analogs, methods of synthesizing cyclic nucleotide analogs and methods of treating diseases and/or conditions such as viral infections, cancer, and/or parasitic diseases with cyclic nucleotide analogs.Type: GrantFiled: December 20, 2011Date of Patent: July 8, 2014Assignee: Alios BioPharma, Inc.Inventors: Leonid Beigelman, David Bernard Smith, Jerome Deval, Vivek Kumar Rajwanshi
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Publication number: 20140179627Abstract: Disclosed herein are nucleotide analogs, methods of synthesizing nucleotide analogs and methods of treating diseases and/or conditions such as a HCV infection with one or more nucleotide analogs.Type: ApplicationFiled: December 19, 2013Publication date: June 26, 2014Applicant: ALIOS BIOPHARMA, INC.Inventors: Leonid Beigelman, Guangyi Wang, David Bernard Smith
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Publication number: 20140155345Abstract: The invention provides new biotinylated compounds and methods for their use.Type: ApplicationFiled: December 4, 2013Publication date: June 5, 2014Applicant: Rutgers, the State University of New JerseyInventors: Roger A. Jones, Barbara L. Gaffney
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Publication number: 20140100186Abstract: A method of modifying a nucleotide or a nucleotide analogue to increase its overall effectiveness in treating an antiviral disease is provided. In some cases, a compound comprising a base, sugar, phosphonate moiety, and amino acid residue is provided, where the base-sugar may be a nucleoside, and the amino acid residue may be a tyrosine residue. In certain cases, the tyrosine residue contains a long chain alkyl group on the carboxamide group of the residue. Methods of inhibiting viral replication and methods of treating a viral infection are also provided.Type: ApplicationFiled: May 7, 2012Publication date: April 10, 2014Inventors: Charles E. McKenna, Boris A. Kashemirov, Ivan S. Krylov, Valeria M. Zakharova
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Publication number: 20140099283Abstract: Provided herein are compounds, compositions and methods for the treatment of Flaviviridae infections, including HCV infections. In certain embodiments, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents. In certain embodiments, the compounds are 2?-chloro nucleosides according to Formula 2001: or a pharmaceutically acceptable salt, solvate, stereoisomeric form, tautomeric form or polymorphic form thereof, wherein B, Z and PD are as described herein.Type: ApplicationFiled: October 7, 2013Publication date: April 10, 2014Inventors: Gilles GOSSELIN, Christophe Claude PARSY, Francois-Rene ALEXANDRE, Houcine RAHALI, Jean-Francois GRIFFON, Julien MILHAU, Dominique SURLERAUX, Cyril B. DOUSSON, Claire PIERRA, Adel M. MOUSSA, Benjamin Alexander MAYES
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Publication number: 20140088033Abstract: The present invention relates to novel boranophosphate analogues of cyclic nucleotides. The invention further relates to the use of such compounds as reagents for signal transduction research or as modulators of cyclic nucleotide-regulated binding proteins and isoenzymes thereof, and/or as hydrolysis- and oxidation-resistant ligands for affinity chromatography, for antibody production or for diagnostic applications e.g. on chip surfaces and/or as additive for organ transplantation storage solutions.Type: ApplicationFiled: March 27, 2012Publication date: March 27, 2014Applicant: BIOLOG LIFE SCIENCE INSTITUTE FORSCHUNGSLABOR UND BIOCHEMICA-VERTRIEB GMBHInventor: Hans-Gottfried Genieser
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Publication number: 20140045798Abstract: The present invention provides a compound of Formula Ia, wherein R1 is H or phosphate and the double bond is between N1 and C1 or between N2 and C1; R2 is a mitochondrial targeting moiety; R3 an alkyl, alkylaryl, alkylheteroaryl spacer group, a cleavable linker, or absent; R4 is H or an alkyl, aryl, or heteroaryl group; and R5 is alkyl, aryl, or heteroaryl; or N1 C1, and N3 together form a heterocyclic ring containing at least 5 atoms, wherein N1, N3, and R1-R5 are as defined above, or N3 and R5 together form a heterocyclic ring containing at least four atoms; or a pharmaceutically acceptable salt or prodrug thereof.Type: ApplicationFiled: October 18, 2013Publication date: February 13, 2014Applicant: Gencia CorporationInventor: Shaharyar Khan
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Patent number: 8618279Abstract: The invention provides a novel method for the chemical synthesis of 2?,3?-cyclic phosphate and phosphorothioate of mono and terminated oligonucleotides synthesis. The invention also provides a novel method of for the chemical synthesis of 2?,3?- and 3?,5?-cyclic phosphate and phosphorothioate mononucleotide nucleotides. The process is based on quick and efficient cyclization of phosphoramidate moiety and neighboring hydroxyl group. The present invention is directed towards the synthesis of high purity DNA and RNAs, specifically to introduce cyclic phosphate at 3?-end of oligonucleotides. Such DNA and RNA's have extensive application in therapeutics, diagnostics, drug design, and selective inhibition of an RNA sequence within cellular environment, in pre-tRNA cleavage and in ribozyme ligation. The 2?,3?-cyclic phosphate nucleosides are involved in a vast number of applications in molecular biology in general and mammalian cells in particular.Type: GrantFiled: January 15, 2010Date of Patent: December 31, 2013Assignee: ChemGenes CorporationInventors: Andrei Laikhter, Suresh Chandra Srivastava, Naveen Srivastava
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Patent number: 8575127Abstract: The invention features compounds of formula I and methods of their use as antiplatelet and antithrombotic compounds: H/N=Q?2OOOO?Q2-N, HR6/NIf)(^XMO-M??OM°?X1MQ?)r(^rfHOOHHOOQHiN?iR2 Formula (I).Type: GrantFiled: November 20, 2009Date of Patent: November 5, 2013Assignee: GLSynthesis Inc.Inventors: Ivan Borissov Yanachkov, George Edward Wright
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Publication number: 20130178612Abstract: Chiral auxiliaries useful for efficiently producing a phosphorus atom-modified nucleic acid derivative with high stereoregularity, and compounds represented by the following the general formula (I) or the general formula (XI) for introducing the chiral auxiliaries.Type: ApplicationFiled: September 22, 2011Publication date: July 11, 2013Applicant: CHIRALGEN, LTD.Inventors: Takeshi Wada, Mamoru Shimizu
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Patent number: 8435962Abstract: The invention discloses triacetyl-3-hydroxyphenyladenosine represented by formula (I), the preparation, the pharmaceutical composition and the use thereof. Specially, the invention discloses a new compound of 2?,3?,5?-tri-O-acetyl-N6-(3-hydroxyphenyl)adenosine. Using hypoxanthine nucleoside as starting material, the compound is prepared by acetylating with acetic anhydride, chlorinating with thionyl chloride, and being substituted with 3-hydroxy aniline. The invention also discloses the pharmaceutical composition comprising triacetyl-3-hydroxyphenyladenosine. The dosage forms of the said pharmaceutical composition include tablet, capsule, pill, injection, sustained release preparation, controlled release preparation or particulate delivery system. The medicament for treatment or precaution of hyperlipemia prepared by the compound of the invention has the advantages of significant hypolipidemic activity, less toxicity and adverse effect as well as slow metabolism in vivo.Type: GrantFiled: March 10, 2009Date of Patent: May 7, 2013Assignee: Institute of Mataria Medica, Chinese Academy of Medical SciencesInventors: Haibo Zhu, Song Wu, Linghua Hao, Kai Qu, Ping Zhu, Xing Wang, Wei Li
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Publication number: 20130072462Abstract: The present invention provides a compound of Formula 1a, wherein R1 is H or phosphate and the double bond is between N? and C? or between N2 and C1; R2 is a mitochondrial targeting moiety; R3 an alkyl, alkylaryl, alkylheteroaryl spacer group, a cleavable linker, or absent; R4 is H or an alkyl, aryl, or heteroaryl group; and R5 is alkyl, aryl, or heteroaryl; or N? C?, and N3 together form a heterocyclic ring containing at least 5 atoms, wherein N1, N3, and R1-R5 are as defined above, or N3 and R5 together form a heterocyclic ring containing at least four atoms; or a pharmaceutically acceptable salt or prodrug thereof.Type: ApplicationFiled: August 17, 2012Publication date: March 21, 2013Applicant: Gencia CorporationInventor: Shaharyar Khan
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Patent number: 8318432Abstract: Cross-reacting hybridization probe for detecting HIV-1 and HIV-2 nucleic acids. The probe advantageously exhibited uniformly high signal-to-noise ratios when hybridized to HIV-1 and HIV-2 target nucleic acids. The probe can be used, for example, in screening applications for detecting donated blood contaminated with either of the two analytes.Type: GrantFiled: January 21, 2010Date of Patent: November 27, 2012Assignee: Gen-Probe IncorporatedInventors: Jeffrey M. Linnen, Wen Wu
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Publication number: 20120237480Abstract: The present invention relates to 2?-allene-substituted nucleoside derivatives of the general formula (I): As well as pharmaceutical compositions comprising such compounds and methods to treat or prevent an HIV infection, HBV infection, HCV infection or abnormal cellular proliferation, comprising administering said compounds or compositions. In addition, the present invention includes processes for the preparation of such compounds, and the related ?-D and ?-L-nucleoside derivatives.Type: ApplicationFiled: March 16, 2012Publication date: September 20, 2012Inventors: YAT SUN OR, Jun Ma, Guoqiang Wang, In Jong Kim, Jiang Long, Yao-Ling Qiu
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Publication number: 20120189607Abstract: The present invention relates to a pharmaceutical composition for promoting fertilization comprising cyclic ADP-ribose or its derivative, CD38 and to a method of promoting fertilization by promoting the synthesis of cyclic ADP-ribose to increase sperm motility. Also, the present invention relates to a pharmaceutical composition for contraception and a method for inhibiting fertilization, which can inhibit the expression or function of cyclic ADP-ribose to reduce sperm motility, thereby inhibiting fertilization.Type: ApplicationFiled: January 25, 2012Publication date: July 26, 2012Applicant: Industrial Cooperation Foundation Chonbuk National UniversityInventors: Uh-Hyun Kim, Kwang-Hyun Park, Byung-Ju Kim
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Publication number: 20120190098Abstract: Fluorophores derived from photoactivatable azide-pi-acceptor fluorogens or from a thermal reaction of an azide-pi-acceptor fluorogen with an alkene or alkyne are disclosed. Fluorophores derived from a thermal reaction of an alkyne-pi-acceptor fluorogen with an azide are also disclosed. The fluorophores can readily be activated by light and can be used to label a biomolecule and imaged on a single-molecule level in living cells.Type: ApplicationFiled: March 1, 2012Publication date: July 26, 2012Applicants: LELAND STANFORD JUNIOR UNIVERSITY, KENT STATE UNIVERSITYInventors: ROBERT J. TWIEG, WILLIAM E. MOERNER, SAMUEL J. LORD, NA LIU, REICHEL SAMUEL
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Publication number: 20120165286Abstract: Disclosed herein are cyclic nucleotide analogs, methods of synthesizing cyclic nucleotide analogs and methods of treating diseases and/or conditions such as viral infections, cancer, and/or parasitic diseases with cyclic nucleotide analogs.Type: ApplicationFiled: December 20, 2011Publication date: June 28, 2012Applicant: ALIOS BIOPHARMA, INC.Inventors: Leonid Beigelman, David Bernard Smith, Jerome Deval, Vivek Kumar Rajwanshi
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Publication number: 20120135092Abstract: Compounds for modulating RecA protein activity are provided. In some embodiments, the compounds modulate RecA activity by interfering with assembly of monomeric RecA protein subunits into a nucleoprotein filament. In some embodiments, the compounds modulate RecA activity by interfering with adenosine triphosphate hydrolysis by the RecA protein. In some embodiments, the compound is a N6-modified adenosine compound. Methods of screening for and methods of using the compounds are also provided.Type: ApplicationFiled: March 14, 2008Publication date: May 31, 2012Inventor: Scott Fain Singleton
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Patent number: 8153609Abstract: This invention provides novel 8-carbyl substituted cAMPS and a novel procedures for the preparation of 8-Br-cAMP, a key starting material.Type: GrantFiled: June 20, 2005Date of Patent: April 10, 2012Assignee: Lauras ASInventors: Kjell Undheim, Kjetil Taskén, Jo Klaveness, Geir Langli, Vidar Bjørnstad
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Publication number: 20120039845Abstract: Compounds having the formula I or II, wherein R1, R2, B, and V are as defined herein, are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for treating an HCV infection and inhibiting HCV replication.Type: ApplicationFiled: October 26, 2011Publication date: February 16, 2012Applicant: METABASIS THERAPEUTICS, INC.Inventors: Scott J. HECKER, K. Raja REDDY, Zhili SUN, Brett C. BOOKSER, David Bernard SMITH
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Publication number: 20110178284Abstract: A protective group represented by the following general formula (I) (the oxygen atom attached with * represents oxygen atom of 2?-hydroxyl group of a ribonucleoside, a ribonucleotide or a derivative thereof; R1 and R2 both represent hydrogen atom, or represent a halogen atom, a C1-6 alkyl group, or a C1-6 halo-substituted alkyl group; R3 and R4 represent hydrogen atom, a halogen atom, a C1-6 alkyl group, or a C1-6 halo-substituted alkyl group; and R5 and R6 represent a halogen atom, a C1-6 halo-substituted alkyl group, cyano group, nitro group, or the like), which is stable under the reaction conditions of the nucleic acid synthetic cycles and has little steric hindrance, and can be removed under mild conditions using fluoride ions as a base.Type: ApplicationFiled: September 15, 2010Publication date: July 21, 2011Applicant: CHIRALGEN, LTD.Inventors: Takeshi WADA, Mamoru SHIMIZU
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Patent number: 7906491Abstract: The present invention relates to novel compounds for modulating the activity of exchange proteins directly activated by cAMP (Epacs). In particular, the present invention relates to cAMP analogues that specifically modulate the activity of Epacs. Examples of the compounds of the invention are substituted deoxyadenosine-cyclic monosphosphates. The invention further relates to pharmaceutical compositions comprising the novel compounds, and the use of the compounds in the treatment of diseases like cancer, chronic inflammation, thrombosis and/or type-2 diabetes mellitus in humans and/or animals.Type: GrantFiled: June 10, 2003Date of Patent: March 15, 2011Assignee: Univisitair Medisch Centrum UtrechtInventors: John De Koning, Anne Christensen, Frank Schwede, Hans Gottfired Genieser, Stein Doskeland, Johannes Bos
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Publication number: 20110009356Abstract: Novel cyclic phosphoramidate prodrugs of drugs of formula I their use in delivery of drugs to the liver, their use in enhancing oral bioavailability, and their method of preparation are described.Type: ApplicationFiled: September 24, 2010Publication date: January 13, 2011Applicant: Metabasis Therapeutics, Inc.Inventors: Mark D. ERION, K. Raja Reddy, Serge H. Boyer
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Publication number: 20100330608Abstract: The inventive molecular transporter compound shows significantly high permeability through a biological membrane such as a plasma membrane, nuclear membrane and blood-brain barrier, and accordingly, can be effectively used in delivering various biologically active molecules.Type: ApplicationFiled: August 20, 2010Publication date: December 30, 2010Applicants: Postech Foundation, Postech Academy-Industry FoundationInventors: Sung-Kee Chung, Kaustabh Kumar Maiti, Woo Sirl Lee, Ock-Youm Jeon, Seok-Ho Lee
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Publication number: 20100137237Abstract: This invention relates to a process for the preparation of an (Rp)-8-substituted adenosine-3?,5?-cyclic phosphorothioic acid, or a salt or ester thereof, which comprises P-amidating 8-bromoadenosine-3?,5?-cyclic phosphoric acid, and reacting the P-amidate with a base and with carbon disulphide to yield (Rp)-8-bromoadenosine-3?,5?-cyclic phosphorothioic acid or a salt or ester thereof.Type: ApplicationFiled: September 17, 2007Publication date: June 3, 2010Applicant: LAURAS ASInventors: Kjell Undheim, Mioara Andrei
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Patent number: 7396658Abstract: The present invention relates to rapid, quantitative, specific, high through-put methods for screening test substances for their ability to inhibit activity of an ouabain-resistant Na+—K+-ATPase involved in a variety of biological processes such as regulation of osmotic balance and cell volume, maintenance of the resting membrane potential, establishment of the ionic composition of cerebrospinal fluid and aqueous humor, electrical activity of muscle and nerve, and receptor-mediated endocytosis, cardiac muscle contractility, neurotransmitter metabolism and vascular muscle cell contraction. These methods can be employed to identify compounds for use in therapeutic applications for disease processes in which dysfunction of the Na+—K+-ATPase contributes to a pathological process. The present invention also includes kits which are used in the methods provided herein.Type: GrantFiled: March 16, 2004Date of Patent: July 8, 2008Assignee: The General Hospital CorporationInventor: Garner T. Haupert, Jr.
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Patent number: 7319093Abstract: 2-Substituted-5?-O-(1-boranotriphosphate)adenosine derivatives having at position 2 a radical R1 selected from the group consisting of H; halogen; O-hydrocarbyl; S-hydrocarbyl; NR3R4; and hydrocarbyl optionally substituted by halogen, CN, SCN, NO2, OR3, SR3 or NR3R4; wherein R3 and R4 are each independently H or hydrocarbyl or R3 and R4 together with the nitrogen atom to which they are attached form a saturated or unsaturated heterocyclic ring optionally containing 1-2 further heteroatoms selected from oxygen, nitrogen and sulfur, and pharmaceutically acceptable salts or diastereoisomers thereof or a mixture of diastereoisomers, are useful for treatment of type 2 diabetes.Type: GrantFiled: October 23, 2002Date of Patent: January 15, 2008Assignees: Bar-Ilan University, University of MontpellierInventors: Bilha Fischer, Victoria Kleiman-Nahum, Pierre Petit
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Patent number: 7217815Abstract: Various 2?-beta-methyl-6-substituted adenosine analogs (including 2,6-disubstituted adenosine, 8-aza-6-substituted adenosine, and 2-aza-6-substituted adenosine) are prepared by conventional and combinatorial library approaches. Contemplated compounds are particularly useful as therapeutic agents, and especially as antiviral agents.Type: GrantFiled: October 23, 2002Date of Patent: May 15, 2007Assignee: Valeant Pharmaceuticals North AmericaInventors: Haoyun An, Yili Ding, Stephanie Z. Shaw, Zhi Hong
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Patent number: 7022727Abstract: The present invention relates to a crystalline form of 6-[(2,2-diphenylethyl)amino]-9-(N-ethyl-?-D-ribofuranosyluronamide)-N-(2-{N?-[1-(2-pyridyl)-4-piperidyl]ureido}ethyl)-9H-purine-2-carboxamide and to a process for the preparation of, compositions containing and the uses of such a crystalline form.Type: GrantFiled: September 3, 2004Date of Patent: April 4, 2006Assignee: Pfizer IncInventors: Terence Vernon Silk, Julian Duncan Smith
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Patent number: 6951932Abstract: The invention provides new methods for synthesis of 2-aralkyloxyadenosines and 2-alkoxyadenosines. The invention is particularly useful for synthesis of 2-[2-(4-chlorophenyl)ethoxy]adenosine. Preferred methods of the invention include activating a guanosine compound followed by hydrolysis; alkylating the hydrolyzed compound with subsequent animation to provide a 2-aralkyloxyadenosine or a 2-alkoxyadenosine compound.Type: GrantFiled: October 24, 2002Date of Patent: October 4, 2005Assignee: King Pharmaceuticals Research & Development, Inc.Inventor: Allan R. Moorman
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Patent number: 6875750Abstract: Aziridine derivatives of formula (I) are disclosed which can be used as cofactor for S-adenosyl-L-methionine-dependent methyltransferases.Type: GrantFiled: July 28, 1999Date of Patent: April 5, 2005Assignee: Max-Planck-Gesellschaft zur Foerderung der Wissenschaften E.V.Inventors: Marc Pignot, Elmar Weinhold
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Patent number: 6852746Abstract: The present invention relates to a crystalline form of 6-[(2,2-diphenylethyl)amino]-9-(N-ethyl-?-D-ribofuranosyluronamide)-N-(2-{N?-[1-(2-pyridyl)-4-piperidyl]ureido}ethyl)-9H-purine-2-carboxamide and to a process for the preparation of, compositions containing and the uses of such a crystalline form.Type: GrantFiled: December 3, 2002Date of Patent: February 8, 2005Assignee: Pfizer IncInventors: Terence Vernon Silk, Julian Duncan Smith
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Patent number: 6846646Abstract: The present invention relates to rapid, quantitative, specific, high through-put methods for screening test substances for their ability to inhibit activity of an ouabain-resistant Na+-K+-ATPase involved in a variety of biological processes such as regulation of osmotic balance and cell volume, maintenance of the resting membrane potential, establishment of the ionic composition of cerebrospinal fluid and aqueous humor, electrical activity of muscle and nerve, and receptor-mediated endocytosis, cardiac muscle contractility, neurotransmitter metabolism and vascular muscle cell contraction. These methods can be employed to identify compounds for use in therapeutic applications for disease processes in which dysfunction of the Na+-K+-ATPase contributes to a pathological process. The present invention also includes kits which are used in the methods provided herein.Type: GrantFiled: December 24, 1998Date of Patent: January 25, 2005Assignee: The General Hospital CorporationInventor: Garner T. Haupert, Jr.
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Patent number: 6831072Abstract: The present invention is directed to a method to produce 8-amino-2′deoxyadenosine by treating 8-azido-2′deoxyadenosine with an aqueous solution of methylamine or dimethylamine.Type: GrantFiled: January 22, 2002Date of Patent: December 14, 2004Assignee: Cygene, Inc.Inventors: Ramón Eritja, Ramón Güimil García
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Patent number: 6759395Abstract: The invention provides a novel soft gelatin capsule comprising a fill material consisting essentially of S-adenosylmethionine (SAMe) salt disposed within an enteric coated soft gelatin film.Type: GrantFiled: December 18, 2001Date of Patent: July 6, 2004Assignee: Orchid Chemicals & Pharmaceuticals, Ltd.Inventors: Canakapalli Bhaktavatsala Rao, Prasanta Kumar Chakrabarti, Hema Ravishankar
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Publication number: 20040023920Abstract: The use of adenosine-5′-triphosphate-2′,3′-dialdehyde (oATP) as a medicament useful for the treatment of inflammatory conditions is disclosed.Type: ApplicationFiled: August 29, 2003Publication date: February 5, 2004Inventor: Maria Elena Ferrero
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Patent number: 6635615Abstract: Stable salts of S-adenosyl-1-methionine with polycations such as chitosan are described. The salts according to the invention are very stable and are valuable for use as active constituents in pharmaceutical compositions.Type: GrantFiled: November 16, 2000Date of Patent: October 21, 2003Inventor: Rolland F. Hebert
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Patent number: 6555545Abstract: Hepatic cirrhosis and fibrosis and fatty liver can be prevented and treated by administering to a subject in need thereof an effective amount of at least one adenosine A2A receptor antagonist or at least one adenosine uptake promotor.Type: GrantFiled: February 12, 2001Date of Patent: April 29, 2003Assignee: New York UniversityInventors: Bruce N. Cronstein, Edwin Chan
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Publication number: 20030060400Abstract: A method and composition for treating a host infected with flavivirus or pestivirus comprising administering an effective flavivirus or pestivirus treatment amount of a described 1′, 2′ or 3′-modified nucleoside or a pharmaceutically acceptable salt or prodrug thereof, is provided.Type: ApplicationFiled: May 23, 2001Publication date: March 27, 2003Inventors: Paulo LaColla, Jean-Pierre Sommadossi
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Publication number: 20030050229Abstract: A method and composition for treating a host infected with hepatitis C comprising administering an effective hepatitis C treatment amount of a described 1′, 2′ or 3′-modified nucleoside or a pharmaceutically acceptable salt or prodrug thereof, is provided.Type: ApplicationFiled: May 23, 2001Publication date: March 13, 2003Inventors: Jean-Pierre Sommadossi, Paulo LaColla
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Patent number: RE38416Abstract: This invention is directed to novel substituted nucleotide bases with a crosslinking arm which accomplish crosslinking between specific sites on adjoining strands of oligonucleotides a oligodeoxynucleotides. The invention is also directed to oligonucleotides comprising at least one of these crosslinking agents and to the use of the resulting novel oligonucleotides for diagnostic and therapeutic purposes.Type: GrantFiled: October 19, 2000Date of Patent: February 3, 2004Assignee: Epoch Biosciences, Inc.Inventors: Charles R. Petrie, Rich B. Meyer, John C. Tabone, Gerald D. Hurst