Plural Phosphorus Atoms In N-glycoside Patents (Class 536/26.2)
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Patent number: 11472830Abstract: Disclosed are compounds, compositions and methods for treating viral infections, diseases, syndromes, or disorders that are affected by the modulation of STING. Such compounds are represented by Formula (I) as follows: wherein R1A, R1B, R1c, B1, R2A, and R2B are defined herein.Type: GrantFiled: November 22, 2017Date of Patent: October 18, 2022Assignee: Janssen Biotech, Inc.Inventors: Gilles Bignan, Peter Connolly, James Patrick Edwards, Stuart Emanuel, Sylvie Laquerre, Tianbao Lu, Mark Richter, Leonid Beigelman, Santhosh Kumar Thatikonda, Guangyi Wang, Minghong Zhong
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Patent number: 11427610Abstract: The present invention is directed to compounds of the formula wherein all substituents are defined herein, as well as pharmaceutically acceptable compositions comprising compounds of the invention and methods of using said compositions in the treatment of various disorders.Type: GrantFiled: October 16, 2018Date of Patent: August 30, 2022Assignee: Bristol-Myers Squibb CompanyInventors: Brian E. Fink, Yufen Zhao, Libing Chen, Audris Huang
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Patent number: 11021511Abstract: Disclosed are compounds, compositions and methods for treating of diseases, syndromes, or disorders that are affected by the modulation of STING. Such compounds are represented by Formula (I) as follows: wherein R1A, R1B, R1C, R1D, B1, R2A, R2B, R2C, R2D, and R2E are defined herein and Formula (II) wherein R1H, R1K, R1J, and R2L are defined herein.Type: GrantFiled: January 26, 2018Date of Patent: June 1, 2021Assignee: Janssen Biotech, Inc.Inventors: Stuart Emanuel, Mark Richter, Peter J. Connolly, James Patrick Edwards, Guangyi Wang, Santhosh Kumar Thatikonda, Leonid Beigelman, Minghong Zhong, Gilles Bignan
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Patent number: 10766919Abstract: A class of polycyclic compounds of general formula (I), of general formula (I?), or of general formula (I?), wherein Base1, Base2, Y, Ya, Xa, Xa1, Xb, Xb1, Xc, Xc1, Xd, Xd1, R1, R1a, R2, R2a, R3, R4, R4a, R5, R6, R6a, R7, R7a, R8, and R8a are defined herein, that may be useful as inductors of type I interferon production, specifically as STING active agents, are provided. Also provided are processes for the synthesis and use of compounds.Type: GrantFiled: February 1, 2018Date of Patent: September 8, 2020Assignee: Merck Sharp & Dohme Corp.Inventors: Michael D. Altman, Brian Andresen, Wonsuk Chang, Matthew Lloyd Childers, Jared N. Cumming, Andrew Marc Haidle, Timothy J. Henderson, James P. Jewell, Rui Liang, Jongwon Lim, Hong Liu, Min Lu, Alan B. Northrup, Ryan D. Otte, Tony Siu, Benjamin Wesley Trotter, Quang T. Truong, Shawn P. Walsh, Kake Zhao
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Patent number: 10759825Abstract: A class of polycyclic compounds of general formula (I), of general formula (I?), or of general formula (I?), wherein Base1, Base2, Y, Ya, Xa, Xa1, Xb, Xb1, Xc, Xc1, Xd, Xd1, R1, R1a, R2, R2a, R3, R4, R4a, R5, R6, R6a, R7, R7a, R8, and R8a are defined herein, that may be useful as inductors of type I interferon production, specifically as STING active agents, are provided. Also provided are processes for the synthesis and use of compounds.Type: GrantFiled: February 1, 2018Date of Patent: September 1, 2020Assignee: Merck Sharp & Dohme Corp.Inventors: Michael D. Altman, Brian Andresen, Wonsuk Chang, Matthew Lloyd Childers, Jared N. Cumming, James P. Jewell, Jongwon Lim, Alan B. Northrup, Ryan D. Otte, Benjamin Wesley Trotter, Quang T. Truong, Shawn P. Walsh, Kake Zhao
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Patent number: 10738074Abstract: A class of polycyclic compounds of general formula (II), of general formula (II?), or of general formula (II?), wherein Base1, Base2, Y, Ya, Xa, Xa1, Xb, Xb1, Xc, Xc1, Xd, Xd1, R1, R1a, R2, R2a, R3a, R4, R4a, R5, R6, R6a, R7, R7a, R8, and R8a are defined herein, that may be useful as inductors of type I interferon production, specifically as STING active agents, are provided. Also provided are processes for the synthesis and use of compounds.Type: GrantFiled: August 11, 2016Date of Patent: August 11, 2020Assignee: Merck Sharp & Dohme Corp.Inventors: Michael D. Altman, Brian Andresen, Wonsuk Chang, Matthew Lloyd Childers, Jared N. Cumming, Andrew Marc Haidle, Timothy J. Henderson, James P. Jewell, Min Lu, Alan B. Northrup, Ryan D. Otte, Tony Siu, Benjamin Wesley Trotter, Quang T. Truong
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Patent number: 9402812Abstract: Provided herein are methods for preparing liposomes and uses thereof. In certain embodiments, liposomes are prepared without using heat, organic solvents, proteins, and/or inorganic salts in the process. In certain embodiments, the liposomal preparation contains one or more active agents. In certain embodiments, the liposomal preparations are used in the treatment of diseases or disorders.Type: GrantFiled: September 23, 2010Date of Patent: August 2, 2016Inventors: Indu Javeri, Kaliappanadar Nellaiappan, Bharat Dixit
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Publication number: 20150133362Abstract: Aspects of the invention provide methods for selecting a candidate oligonucleotide for activating expression of a target gene. Further aspects of the invention provide methods of selecting a set of oligonucleotides that is enriched in oligonucleotides that activate expression of a target gene. Further aspects provide single stranded oligonucleotides that modulate gene expression and compositions and kits comprising the same. Methods for modulating gene expression using the single stranded oligonucleotides are also provided.Type: ApplicationFiled: May 16, 2013Publication date: May 14, 2015Applicants: RaNA Therapeutics, Inc., The General Hospital Corporation d/b/a Massachusetts General HospitalInventors: Arthur M. Krieg, Romesh Subramanian, James McSwiggen, Jeannie T. Lee
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Patent number: 8981078Abstract: An agent for inhibiting translesion DNA replication comprises a non-natural adenine ribose analog represented by those as set forth in FIG. 1.Type: GrantFiled: January 4, 2012Date of Patent: March 17, 2015Assignee: Case Western Reserve UniversityInventors: Anthony J. Berdis, Irene Lee, Xuemei Zhang
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Patent number: 8969545Abstract: Alkynyl-derivatized cap analogs, alkynyl-modified capped RNA, 1,4-disubstituted triazole-derivatized capped RNA, methods of preparation, methods of isolation, and uses thereof are provided. The “click” modification facilitates detection and isolation of capped RNAs and the 1,4-disubstituted triazole derivatives formed by the “click” reaction are useful for producing RNA transcripts and encoded protein.Type: GrantFiled: October 18, 2012Date of Patent: March 3, 2015Assignee: Life Technologies CorporationInventors: Anilkumar R. Kore, Shanmugasundaram Muthian, Kyle Gee
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Patent number: 8957201Abstract: A method for the prevention or treatment in a mammal of a disease preventable or treatable by the pharmacologically useful antisense or antigene activity of an oligonucleotide analogue or a pharmacologically acceptable salt thereof in the body of said mammal, which method comprises administering to said mammal in need of such prevention or treatment a pharmaceutically effective amount of an oligonucleotide analogue comprising two or more nucleoside units, wherein at least one of said nucleoside units is a structure of the formula (2): wherein A is methylene; and B is an unsubstituted purin-9-yl, an unsubstituted 2-oxo-pyrimidin-1-yl or a substituted purin-9-yl; or a pharmacologically acceptable salt thereof.Type: GrantFiled: July 22, 2010Date of Patent: February 17, 2015Assignee: Daiichi Sankyo Company, LimitedInventors: Masakatsu Kaneko, Koji Morita, Takeshi Imanishi
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Publication number: 20150031833Abstract: A compound has Formula I: A, B, C, D, W, X, Y, and Z are independently selected from hydrogen, optionally substituted C1-C6 alkyl, optionally substituted C1-C6 alkoxy, aryl, aldehyde, protected aldehyde, CH, N, O, S, null, and bond; Q is selected from aldehyde, protected aldehyde, and null, at least one of A, B, C, D, W, X, Y, Z, or Q is an aldehyde or protected aldehyde; the bonds between each of A-B, B-C, C-D, W-X, X-Y, and Y-Z are selected from single bond, double bond, triple bond, and no bond; L is a linker selected from a C1-C12 alkyl, aralkyl, and aryl, any of which is optionally substituted; one or more methylene unit (CH2) of the C1-C12 alkyl is optionally replaced by any combination of oxygen, carbonyl(C?O), and NH; and R1 and R2 are independently selected from —NR3R4, halogen, C1-C8 alkoxy, aralkoxy, alkenyloxy, alkynyloxy, and OCH2CH2CN; R3 and R4 are independently a C1-C4, straight chain or branched alkyl group.Type: ApplicationFiled: October 10, 2014Publication date: January 29, 2015Inventors: Ryan Christopher SMITH, Randall SMITH, Xiaodong ZHAO
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Patent number: 8674086Abstract: Embodiments of the invention provide non-natural bifunctional nucleotides having both nuclease resistance and nucleic acid synthesis blocking properties and methods of sequencing nucleic acids that employ non-natural bifunctional nucleic acids. Additional embodiments provide non-natural oligonucleotides and methods for sequencing nucleic acids using the non-natural oligonucleotides. Methods according to embodiments of the invention employ electronic detection and fluorescent detection of nucleic acid sequencing reactions.Type: GrantFiled: June 25, 2010Date of Patent: March 18, 2014Assignee: Intel CorporationInventors: Jianquan Liu, Xing Su, Kai Wu
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Patent number: 8603741Abstract: Methods, Compositions, and Systems are provided for nucleic acid sequencing where the sequential incorporation of nucleotides uses two distinct chemical steps. A plurality of nucleotide analogs, each having a labeled leaving group at its 3? hydroxyl can be sequentially added to a growing strand in the presence of a selective cleaving activity that cleaves the 3? hydroxyl leaving group preferentially after it has been incorporated. The selective cleaving agent can comprise an exonuclease activity, and the exonuclease activity can be a polymerase-associated exonuclease activity. Nucleotide analogs having labels on both a cleavable polyphosphate portion and on a 3? hydroxyl leaving group can provide signals characteristic of nucleotide analog incorporation. Systems having illumination optics, collection optics, and substrates observe signals from the labels as they are being incorporated into a growing nucleic acid strand, allowing for the sequencing of template nucleic acids.Type: GrantFiled: February 8, 2011Date of Patent: December 10, 2013Assignee: Pacific Biosciences of California, Inc.Inventors: Robin Emig, Lei Jia, Jeremiah Hanes, Lubomir Sebo
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Patent number: 8569259Abstract: Provided are adenosine analog compounds of the general formula that act as P2Y receptors, e.g., the P2Y2 receptor, including pharmaceutical compositions; and uses thereof to treat or prevent diseases associated with that receptor, e.g., disorders relating to mucus secretion, such as cystic fibrosis, chronic obstructive pulmonary disorder (COPD), asthma, constipation, chronic idiopathic constipation, dry mouth (xerostomia), gum disease, and gastrointestinal problems caused by radiation and chemotherapy for cancer.Type: GrantFiled: November 16, 2007Date of Patent: October 29, 2013Assignee: Microdose Therapeutx, Inc.Inventors: Efrat Ben-Zeev, Vincent Jacques, Yael Marantz, A. Sekar Reddy, Zhaoda Zhang, Oren Becker, Dilara McCauley, Pini Orbach, Sharon Shacham, Ashis K. Saha, Michael Xie
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Patent number: 8481712Abstract: The present invention provides nucleoside compounds and certain derivatives thereof which are inhibitors of RNA-dependent RNA viral polymerase. These compounds are inhibitors of RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependent RNA viral infection. They are particularly useful as inhibitors of hepatitis C virus (HCV) NS5B polymerase, as inhibitors of HCV replication, and/or for the treatment of hepatitis C infection. The invention also describes pharmaceutical compositions containing such nucleoside compounds alone or in combination with other agents active against RNA-dependent RNA viral infection, in particular HCV infection. Also disclosed are methods of inhibiting RNA-dependent RNA polymerase, inhibiting RNA-dependent RNA viral replication, and/or treating RNA-dependent RNA viral infection with the nucleoside compounds of the present invention.Type: GrantFiled: February 2, 2007Date of Patent: July 9, 2013Assignees: Merck Sharp & Dohme Corp., ISIS Pharmaceuticals, Inc.Inventors: Balkrishen Bhat, Anne B. Eldrup, Thazha P. Prakash, Phillip Dan Cook, Robert L. LaFemina, Amy L. Simcoe, Carrie A. Rutkowski, Mario A. Valenciano
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Patent number: 8440812Abstract: The invention relates to analogous compounds of 6-thioguanosine triphosphate of general formula (I). A compound of the general formula (I); wherein the dashed bond in the sugar moiety can be either single or double and wherein R1, R2, R3, R4 or R5, equal or different between each other, have general formula -(Int)m-Ter, wherein m is between 0 and 12 and Int and Ter are Internal and Terminal building blocks, wherein Int is selected from the group consisting of formula (II); and Ter is selected from the group consisting of formula (III).Type: GrantFiled: December 20, 2011Date of Patent: May 14, 2013Assignee: Nogra Pharma LimitedInventors: Giancarlo Naccari, Sergio Baroni
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Publication number: 20130116420Abstract: The present invention provides 5? modified nucleosides and oligomeric compounds prepared therefrom. More particularly, the present invention provides modified nucleosides having at least one 5?-substituent and an optional 2? substituent, oligomeric compounds comprising at least one of these modified nucleosides and methods of using the oligomeric compounds. In some embodiments, the oligomeric compounds provided herein are expected to hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA.Type: ApplicationFiled: April 26, 2011Publication date: May 9, 2013Applicant: Isis Pharmaceuticals, Inc.Inventors: Thazha P. Prakash, Punit P. Seth, Eric E. Swayze
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Publication number: 20130084576Abstract: The present invention provides modified nucleosides, analogs thereof and oligomeric compounds prepared therefrom. More particularly, the present invention provides modified nucleosides and analogs thereof that are useful for incorporation at the terminus of an oligomeric compound. Such oligomeric compounds can also be included in a double stranded composition. In some embodiments, the oligomeric compounds provided herein are expected to hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA.Type: ApplicationFiled: April 26, 2011Publication date: April 4, 2013Applicant: Isis Pharmaceuticals, Inc.Inventors: Thazha P. Prakash, Punit P. Seth, Eric E. Swayze
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Patent number: 8361727Abstract: Provided are novel nucleotides, nucleoside, and their derivatives described herein, that can be used in DNA sequencing technology and other types of DNA analysis. In one embodiment, the nucleotide or nucleoside with an unprotected 3?-OH group is derivatized at the nucleobase to include a fluorescent dye attached via a linker to a photocleavable terminating group. The photocleavable-fluorescent group is designed to terminate DNA synthesis as well as be cleaved so that DNA oligomers can be sequenced efficiently in a parallel format. The design of such rapidly cleavable fluorescent groups on nucleotides and nucleosides can enhance the speed and accuracy of sequencing of large oligomers of DNA in parallel, to allow rapid whole genome sequencing, and the identification of polymorphisms and other valuable genetic information, as well as allowing further manipulation and analysis of nucleic acid molecules in their native state following cleavage of the fluorescent group.Type: GrantFiled: May 24, 2011Date of Patent: January 29, 2013Assignee: Lasergen, Inc.Inventors: Weidong Wu, Vladislav A. Litosh, Brian P. Stupi, Michael L. Metzker
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Patent number: 8349812Abstract: Immunostimulatory oligoribonucleotides (ORN) featuring 5?-triphosphates and various 5?-triphosphate analogs are provided. Also provided are physiologically acceptable salts of the immunostimulatory ORN and pharmaceutical compositions containing the immunostimulatory ORN of the invention. ORN of the invention are useful as adjuvants and can be combined with an antigen to promote an antigen-specific immune response. ORN of the invention are also particularly useful for promoting a Th1-type immune response. Also provided are methods of use of the compounds and pharmaceutical compositions of the invention to enhance an immune response in a subject, as well to treat a number of conditions including cancer, infection, allergy, and asthma, and to vaccinate a subject against an antigen.Type: GrantFiled: October 30, 2008Date of Patent: January 8, 2013Assignee: AdiuTide Pharmaceuticals GmbHInventors: Harald Debelak, Eugen Uhlmann
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Publication number: 20120296076Abstract: The invention provides synthetic processes and synthetic intermediates that can be used to prepare compounds having useful anti-HIV properties.Type: ApplicationFiled: May 18, 2012Publication date: November 22, 2012Inventors: Richard Hung Chiu Yu, Brandon Heath Brown, Richard P. Polniaszek, Benjamin R. Graetz, Keiko Sujino, Duong Duc-Phi Tran, Alan Scott Triman, Kenneth M. Kent, Steven Pfeiffer
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Patent number: 8304529Abstract: Novel cap analogs which are easily synthesized, resulting in high levels of capping efficiency and transcription and improved translation efficiencies are provided. Such caps are methylated at the N7 position of one or both guanosines of the dinucleotide cap as well as at the 3? position on the ribose ring. Substituent groups on the ribose ring also result in the cap being incorporated in the forward orientation. Also provided are methods useful for preparing capped analogs and using mRNA species containing such analogs are also contemplated herein, as well as kits containing the novel cap analogs.Type: GrantFiled: July 10, 2007Date of Patent: November 6, 2012Assignee: Life Technologies CorporationInventors: Anilkumar R. Kore, Muthian Shanmugasundaram
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Publication number: 20120245029Abstract: This invention provides phosphate-modified nucleosides represented by the structural formula (I): wherein W is O or S, and wherein B, R1; R3 and R2. are as defined herein. These compounds are useful as substrates for DNA/RNA polymerases, and as anti-viral agents in particular against HIV-1.Type: ApplicationFiled: May 12, 2010Publication date: September 27, 2012Applicant: Katholieke Universiteit LeuvenInventors: Piet Herdewijn, Philippe Marlière
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Patent number: 8158776Abstract: This invention is directed to a method of enhancing or facilitating the clearance or the lung mucus secretions in a subject. This invention is also directed to a method of facilitating the hydration of the lung mucus secretions in a subject. This invention is further directed to a method of preventing or treating diseases or conditions associated with impaired lung or airway function in a human or other mammal. The method comprises administering to a subject a pharmaceutical composition comprising a therapeutic effective amount of P2Y6 receptor agonist compound, wherein said amount is effective to activate the P2Y6 receptors on the luminal surface of lung epithelia. The P2Y6 receptor agonist compounds useful for this invention include mononucleoside 5?-diphosphates, dinucleoside monophosphate, dinucleoside diphosphates, or dinucleoside triphosphates of general Formula I, or salts, solvates, hydrates thereof. This invention is also directed to novel P2Y6 receptor agonist compounds.Type: GrantFiled: November 4, 2010Date of Patent: April 17, 2012Assignee: Inspire Pharmaceuticals, Inc.Inventors: José L. Boyer, Sammy R. Shaver, James G. Douglass, III, Catherine C. Redick
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Patent number: 8034923Abstract: Processes are disclosed that use 3?-reversibly terminated nucleoside triphosphates to analyze DNA for purposes other than sequencing using cyclic reversible termination. These processes are based on the unexpected ability of terminal transferase to accept these triphosphates as substrates, the unexpected ability of polymerases to add reversibly and irreversibly terminated triphosphates in competition with each other, the development of cleavage conditions to remove the terminating group rapidly, in high yield, and without substantial damage to the terminated oligonucleotide product, and the ability of reversibly terminated primer extension products to capture groups. The presently preferred embodiments of the disclosed processes use a triphosphate having its 3?-OH group blocked as a 3?-ONH2 group, which can be removed in buffered NaNO2 and use variants of Taq DNA polymerase, including one that has a replacement (L616A).Type: GrantFiled: March 27, 2009Date of Patent: October 11, 2011Inventors: Steven Albert Benner, Daniel Hutter, Nicole Aurora Leal, Fei Chen
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Publication number: 20110212437Abstract: Methods, Compositions, and Systems are provided for nucleic acid sequencing where the sequential incorporation of nucleotides uses two distinct chemical steps. A plurality of nucleotide analogs, each having a labeled leaving group at its 3? hydroxyl can be sequentially added to a growing strand in the presence of a selective cleaving activity that cleaves the 3? hydroxyl leaving group preferentially after it has been incorporated. The selective cleaving agent can comprise an exonuclease activity, and the exonuclease activity can be a polymerase-associated exonuclease activity. Nucleotide analogs having labels on both a cleavable polyphosphate portion and on a 3? hydroxyl leaving group can provide signals characteristic of nucleotide analog incorporation. Systems having illumination optics, collection optics, and substrates observe signals from the labels as they are being incorporated into a growing nucleic acid strand, allowing for the sequencing of template nucleic acids.Type: ApplicationFiled: February 8, 2011Publication date: September 1, 2011Applicant: Pacific Biosciences of California, Inc.Inventors: Robin Emig, Lei Jia, Jeremiah Hanes, Lubomir Sebo
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Patent number: 7964352Abstract: Provided are novel nucleotides, nucleoside, and their derivatives described herein, that can be used in DNA sequencing technology and other types of DNA analysis. In one embodiment, the nucleotide or nucleoside with an unprotected 3?-OH group is derivatized at the nucleobase to include a fluorescent dye attached via a linker to a photocleavable terminating group. The photocleavable-fluorescent group is designed to terminate DNA synthesis as well as be cleaved so that DNA oligomers can be sequenced efficiently in a parallel format. The design of such rapidly cleavable fluorescent groups on nucleotides and nucleosides can enhance the speed and accuracy of sequencing of large oligomers of DNA in parallel, to allow rapid whole genome sequencing, and the identification of polymorphisms and other valuable genetic information, as well as allowing further manipulation and analysis of nucleic acid molecules in their native state following cleavage of the fluorescent group.Type: GrantFiled: November 11, 2008Date of Patent: June 21, 2011Assignee: LaserGen, Inc.Inventors: Weidong Wu, Vladislav A. Litosh, Brian P. Stupi, Michael L. Metzker
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Publication number: 20110086813Abstract: The present invention relates to a novel class of guanine nucleotide analogs which inhibit RelA and Relseq synthetic activity and which possess anti-bacterial activity. The present invention also relates to pharmaceutical compositions that include such compounds, and to methods of use of such compounds or compositions for combating bacteria and treating bacterial infections.Type: ApplicationFiled: March 18, 2009Publication date: April 14, 2011Inventors: Gad Glaser, Jehoshua Katzhendler, Rolf Hilgenfeld, Roee Vidavski, Ezequiel Wexselblatt, Tamar Prez-Menahemov, Ilana Kaspy
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Patent number: 7897737Abstract: Provided are novel nucleotides, nucleoside, and their derivatives described herein, that can be used in DNA sequencing technology and other types of DNA analysis. In one embodiment, the nucleotide or nucleoside with an unprotected 3?-OH group is derivatized at the nucleobase to include a fluorescent dye attached via a linker to a photocleavable terminating group. The photocleavable-fluorescent group is designed to terminate DNA synthesis as well as be cleaved so that DNA oligomers can be sequenced efficiently in a parallel format. The design of such rapidly cleavable fluorescent groups on nucleotides and nucleosides can enhance the speed and accuracy of sequencing of large oligomers of DNA in parallel, to allow rapid whole genome sequencing, and the identification of polymorphisms and other valuable genetic information, as well as allowing further manipulation and analysis of nucleic acid molecules in their native state following cleavage of the fluorescent group.Type: GrantFiled: December 5, 2006Date of Patent: March 1, 2011Assignee: LaserGen, Inc.Inventors: Weidong Wu, Vladislav A. Litosh, Brian P. Stupi, Michael L. Metzker
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Patent number: 7893227Abstract: Provided are novel nucleotides, nucleoside, and their derivatives described herein, that can be used in DNA sequencing technology and other types of DNA analysis. In one embodiment, the nucleotide or nucleoside with an unprotected 3?-OH group is derivatized at the nucleobase to include a fluorescent dye attached via a linker to a non-cleavable terminating group. The non-cleavable-fluorescent group is designed to terminate DNA synthesis so that DNA oligomers can be sequenced efficiently in a parallel format. These reagents and methods will lead to more accurate identification of polymorphisms and other valuable genetic information.Type: GrantFiled: December 5, 2006Date of Patent: February 22, 2011Assignee: LaserGen, Inc.Inventors: Weidong Wu, Vladislav A. Litosh, Brian P. Stupi, Michael L. Metzker
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Publication number: 20100290990Abstract: The present invention relates to a method for preparing a 2-fluoropurine marked with the radioisotope 18F comprising a fluorination step for a 2-nitropurine derivative. The present invention comprises a 2-fluoropurine derivative marked with the radioisotope 18F which can be obtained by or during a method according to the invention and its various uses.Type: ApplicationFiled: December 23, 2008Publication date: November 18, 2010Inventors: Louisa Barre, Patrice Marchand
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Patent number: 7816333Abstract: A method for the prevention or treatment in a mammal of a disease preventable or treatable by the pharmacologically useful antisense or antigene activity of an oligonucleotide analogue or a pharmacologically acceptable salt thereof in the body of said mammal, which method comprises administering to said mammal in need of such prevention or treatment a pharmaceutically effective amount of an oligonucleotide analogue comprising two or more nucleoside units, wherein at least one of said nucleoside units is a structure of the formula (2): wherein A is methylene; and B is an unsubstituted purin-9-yl, an unsubstituted 2-oxo-pyrimidin-1-yl or a substituted purin-9-yl; or a pharmacologically acceptable salt thereof.Type: GrantFiled: July 27, 2007Date of Patent: October 19, 2010Assignees: Daiichi Sankyo Company, Limited, Mitsubishi-Kagaku Foods CorporationInventors: Masakatsu Kaneko, Koji Morita, Takeshi Imanishi
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Publication number: 20100227327Abstract: Disclosed herein are methods and compositions for continuous single-molecule nucleic acid sequencing by synthesis with fluorogenic nucleotides.Type: ApplicationFiled: March 5, 2010Publication date: September 9, 2010Inventors: Xiaoliang Sunney Xie, Peter A. Sims, William J. Greenleaf
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Publication number: 20100152424Abstract: Nucleic acid compositions, methods of making and using such compositions that comprise modular functional groups that can be configured to provide desired functionality to different nucleotide types through a swappable and preferably non-covalent linkage component. Such compositions are useful in a variety of applications including nucleic acid analyses.Type: ApplicationFiled: November 18, 2009Publication date: June 17, 2010Applicant: Pacific Biosciences of California, Inc.Inventors: Jonas Korlach, Jeffrey Wegener
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Patent number: 7666851Abstract: This invention relates to the field of nucleic acid chemistry, more specifically to the field of compositions and processes that are nucleic acid analogs. More specifically, it relates to purine analogs that contain three rings, where the third ring bridges the exocyclic substituent at position 6 to position 7, using the purine numbering system. Still more specifically it relates to analogs having this structure that are able to form nucleobase pairs having the Watson-Crick geometry with a pyrimidine or pyrimidine analog, where the nucleobase pair is joined by hydrogen bonding patterns that either present a standard hydrogen bonding pattern, or a non-standard hydrogen bonding pattern. Most specifically, it to nucleoside analogs that are analogs of isoguanosine, but where the 5-6 ring system of the purine ring in isoguanosine is fused to another five- or six-membered ring, where the fused ring joins the exocyclic amino group with an atom that is, by analogy, at position 7 of the isoguanine ring system.Type: GrantFiled: May 18, 2006Date of Patent: February 23, 2010Inventor: Steven Albert Benner
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Publication number: 20100041041Abstract: The present invention relates generally to labeled and unlabled cleavable terminating groups and methods for DNA sequencing and other types of DNA analysis. More particularly, the invention relates in part to nucleotides and nucleosides with chemically cleavable, photocleavable, enzymatically cleavable, or non-photocleavable groups and methods for their use in DNA sequencing and its application in biomedical research.Type: ApplicationFiled: June 11, 2009Publication date: February 18, 2010Inventors: Vladislav A. LITOSH, Megan N. HERSH, Brian P. STUPI, Weidong WU, Michael L. METZKER
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Publication number: 20100016250Abstract: The present invention provides TLR9 agonists comprising, as an active ingredient, a compound represented by formula (I): (wherein a represents 0 or 1; n represents an integer of 0 to 2; m represents an integer of 0 to 5; X1 and X2 each independently represent a hydrogen atom or hydroxy; Y represents an oxygen atom or a sulfur atom; -Q1-represents —O— or the like; -Q2- represents —O— or the like; -Z- represents —O— or the like; R1, R3 and R4 each independently represent hydroxy or the like; R2 and R5 each independently represent a hydrogen atom, hydroxy or the like; and A represents 6-aminopurin-9-yl or the like) or a pharmaceutically acceptable salt thereof, and the like.Type: ApplicationFiled: April 13, 2007Publication date: January 21, 2010Applicant: KYOWA HAKKO KIRIN CO., LTD.Inventors: Hiroyuki Nagata, Michio Ichimura, Rieko Nakatsu, Shun-Ichi Ikeda, Ayako Kawabata, Toshio Ota, Masayuki Abe, Michio Takashima, Makoto Suzuki
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Patent number: 7612047Abstract: The present invention relates to mononucleoside phosphate compounds that have the benefits of a dinucleotide pharmaceutical. These mononucleoside phosphates can be made from a mononucleotide that has been modified by attaching a degradation-resistant substituent on the terminal phosphate of a polyphosphate mononucleotide. By attaching this degradation-resistant substituent, the stability from degradation matches or exceeds those of certain dinucleotides. The mononucleoside phosphate compounds of the present invention are useful in preventing and treating epithelial tissue diseases or diseases or disorders associated with platelet aggregation.Type: GrantFiled: September 10, 2008Date of Patent: November 3, 2009Assignee: Inspire Pharmaceuticals, Inc.Inventors: James G. Douglass, III, Benjamin R. Yerxa, Sammy R. Shaver, Ward M. Peterson, Edward G. Brown, Christopher S. Crean, José L. Boyer
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Patent number: 7598230Abstract: The present invention relates to nucleoside diphosphate mimics and nucleoside triphosphate mimics, which contain diphosphate or triphosphate moiety mimics and optionally sugar-modifications and/or base-modifications. The nucleotide mimics of the present invention, in a form of a pharmaceutically acceptable salt, a pharmaceutically acceptable prodrug, or a pharmaceutical formulation, are useful as antiviral, antimicrobial, and anticancer agents. The present invention provides a method for the treatment of viral infections, microbial infections, and proliferative disorders. The present invention also relates to pharmaceutical compositions comprising the compounds of the present invention optionally in combination with other pharmaceutically active agents.Type: GrantFiled: June 14, 2007Date of Patent: October 6, 2009Assignee: Biota Scientific Management Pty LtdInventors: Phillip D. Cook, Guangyi Wang, Thomas W. Bruice, Nicholas A. Boyle, Janet M. Leeds, Jennifer L. Brooks, Marija Prhavc, Maria Eugenia Ariza, Patrick C. Fagan, Yi Jin, Vivek K. Rajwanshi, Kathleen D. Tucker
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Publication number: 20090215635Abstract: The present invention relates to methods and reagents for detecting analytes, e.g. nucleic acids. The new methods and reagents allow a simple and sensitive detection even in complex biological samples.Type: ApplicationFiled: April 28, 2006Publication date: August 27, 2009Applicant: BASF SEInventors: Thomas Carell, Anja Schwögler, Glenn A. Burley, Johannes Gierlich, Mohammad Reza Mofid
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Publication number: 20090093623Abstract: A set of 4,7-dichlororhodamine compounds useful as fluorescent dyes are disclosed having the structures wherein R1-R6 are hydrogen, fluorine, chlorine, lower alkyl, lower alkene, lower alkyne, sulfonate, sulfone, amino, amido, nitrile, lower alkoxy, linking group, or, when taken together, R1 and R6 is benzo, or, when taken together, R4 and R5 is benzo; R7-R10, R12-R16 and R18 may be hydrogen, fluorine, chlorine, lower alkyl lower alkene, lower alkyne, sulfonate, sulfone, amino, amido, nitrile, lower alkoxy, linking group; R11 and R17 may be hydrogen, lower alkyl lower alkene, lower alkyne, phenyl, aryl, linking group; Y1-Y4 are hydrogen, lower alkyl or cycloalkyl, or, when taken together, Y1 and R2, Y2 and R1 Y3 and R3, and/or Y4 and R4 is propano, ethano, or substituted forms thereof, and X1-X3 taken separately are hydrogen, chlorine, fluorine, lower alkyl, carboxylate, sulfonate, hydroxymethyl, and linking group, or any combinations thereof.Type: ApplicationFiled: August 27, 2008Publication date: April 9, 2009Applicant: Applied Biosystems Inc.Inventors: Linda G. Lee, Scott C. Benson, Barnett B. Rosenblum, Sandra L. Spurgeon, Ronald J. Graham
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Patent number: 7476734Abstract: The invention provides nucleotide analogs for use in sequencing nucleic acid molecules.Type: GrantFiled: December 6, 2005Date of Patent: January 13, 2009Assignee: Helicos Biosciences CorporationInventor: David R. Liu
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Publication number: 20090004101Abstract: The present invention provides a method of enhancing the absorption of molecules across the airway epithelium, thereby enhancing the delivery of desired therapeutic or diagnostic agents across the airway epithelium via the systemic circulation to the target site of action. The method comprises administration of a formulation comprising a pharmaceutical composition comprising a synthetic or natural nucleoside diphosphate, nucleoside triphosphate, or dinucleoside polyphosphate, together with a pharmaceutically acceptable carrier. Preferably the nucleotide is a P2Y receptor agonist which is administered at any time during treatment with a therapeutic or diagnostic agent. A preferred embodiment is a method of administering a pharmaceutical composition comprising a P2Y receptor agonist with enhanced resistance to extracellular hydrolysis, such as dinucleoside polyphosphate compounds.Type: ApplicationFiled: August 1, 2005Publication date: January 1, 2009Applicant: UNIVERSITY COLLEGE CARDIFF CONSULTANTS LIMITEDInventors: Glyn Taylor, Navdeep Thoofer, Richard Evans, Carole Evans, Benjamin Yerxa, Gregory Mossinghoff
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Publication number: 20090005550Abstract: The present invention concerns modified oligonucleotides and processes for their production wherein these oligonucleotides contain at least once the structure P?N-Acc where Acc is an electron acceptor or an electron acceptor substituted with a residue R and R is any organic substituent.Type: ApplicationFiled: May 16, 2008Publication date: January 1, 2009Inventors: Dieter Heindl, Dirk Kessler
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Patent number: 7462733Abstract: Novel phosphonate compounds are provided including a phosphonoglyoxylamide ester, an ?-keto phosphonophosphinate ester, a carbonylbisphosphonate analog of a nucleotide, and a diazomethylenebisphosphonate analog of a nucleotide, as well as methods of making synthetically and medically useful ?-keto phosphonate compounds.Type: GrantFiled: July 30, 2002Date of Patent: December 9, 2008Assignee: University of Southern CaliforniaInventors: Charles E. McKenna, Boris A. Kashemirov, Patricia I. Bonaz-Krause
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Publication number: 20080153774Abstract: The present invention provides a 4?-C-substituted-2-haloadenosine derivative represented by the following formula [I], [II], or [III]: (wherein X represents a halogen atom, R1 represents an ethynyl group or a cyano group, and R2 represents hydrogen, a phosphate residue, or a phosphate derivative residue). The present invention also provides a pharmaceutical composition containing the derivative and a pharmaceutically acceptable carrier therefor.Type: ApplicationFiled: November 19, 2007Publication date: June 26, 2008Inventors: Satoru Kohgo, Hiroshi Ohrui, Eiichi Kodama, Masao Matsuoka, Hiroaki Mitsuya
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Patent number: 7335765Abstract: A compound of the formula (1): wherein R1 and R2 are the same or different and represent a hydrogen atom, a hydroxyl protecting group, a phosphate group, or —P(R3)R4, wherein R3 and R4 are the same or different and represent a hydroxyl group, an amino group, an alkoxy group having from 1 to 4 carbon atoms, a cyanoalkoxy group having from 1 to 5 carbon atoms or an amino group substituted by an alkyl group having from 1 to 4 carbon atoms; A represents an alkylene group having from 1 to 4 carbon atoms and B represents a purin-9-yl group, a 2-oxo-pyrimidin-1-yl group, a substituted purin-9-yl group or a substituted 2-oxo-pyrimidin-1-yl group having a substituent ? selected from the group consisting of a hydroxyl group which may be protected, an alkoxy group having from 1 to 4 carbon atoms, a mercapto group which may be protected, an alkylthio group having from 1 to 4 carbon atoms, an alkoxy group having from 1 to 4 carbon atoms, an amino group which may be protected, a mono- or di-alkylamino group which may bType: GrantFiled: August 9, 2001Date of Patent: February 26, 2008Assignees: Daiichi Sankyo Company, Limited, Mitsubishi-Kagaku Foods CorporationInventors: Masakatsu Kaneko, Koji Morita, Takeshi Imanishi
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Patent number: 7314923Abstract: A probe for a gene or a primer for starting amplification comprising an oligonucleotide analogue comprising two or more nucleoside units, wherein at least one of the nucleoside units is a structure of the formula (2): wherein A represents a C1-C4 alkylene group, and B is an unsubstituted purin-9-yl group, an unsubstituted 2-oxo-pyrimidin-1-yl-group, a substituted purin-9-yl-group or a substituted 2-oxo-pyrimidin-1-yl group. Also a method for preventing or treating a disease preventable or treatable by the antisense or antigene activity of an oligonucleotide by administering the oligonucleotide analogue.Type: GrantFiled: May 5, 2003Date of Patent: January 1, 2008Assignees: Daiichi Sankyo Company, Limited, Mitsubishi-Kagaku Foods CorporationInventors: Masakatsu Kaneko, Koji Morita, Takeshi Imanishi
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Patent number: 7285658Abstract: The present invention relates to nucleoside diphosphate mimics and nucleoside triphosphate mimics, which contain diphosphate or triphosphate moiety mimics and optionally sugar-modifications and/or base-modifications. The nucleotide mimics of the present invention, in a form of a pharmaceutically acceptable salt, a pharmaceutically acceptable prodrug, or a pharmaceutical formulation, are useful as antiviral, antimicrobial, and anticancer agents. The present invention provides a method for the treatment of viral infections, microbial infections, and proliferative disorders. The present invention also relates to pharmaceutical compositions comprising the compounds of the present invention optionally in combination with other pharmaceutically active agents.Type: GrantFiled: February 28, 2003Date of Patent: October 23, 2007Assignee: Biota, Inc.Inventors: Phillip D. Cook, Guangyi Wang, Thomas W. Bruice, Nicholas A. Boyle, Janet M. Leeds, Jennifer L. Brooks, Marija Prhavc, Maria Eugenia Ariza, Patrick C. Fagan, Yi Jin, Vivek K. Rajwanshi, Kathleen D. Tucker