Phosphorus Containing Patents (Class 514/51)
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Patent number: 8933052Abstract: Compounds of the formula I: including any possible stereoisomers thereof, wherein: R4 is a monophosphate, diphosphate or triphosphate ester; or R4 is R7 is optionally substituted phenyl, optionally substituted naphthyl, or optionally substituted indolyl; R8 and R8? are hydrogen, C1-C6alkyl, benzyl, or phenyl; or R8 and R8? form C3-C7cycloalkyl; R9 is C1-C10alkyl, C3-C7cycloalkyl, phenyl or phenyl-C1-C6alkyl, wherein the phenyl moiety in phenyl or phenyl-C1-C6alkyl is optionally substituted; or a pharmaceutically acceptable salt or solvate thereof; pharmaceutical formulations and the use of compounds I as HCV inhibitors.Type: GrantFiled: March 15, 2013Date of Patent: January 13, 2015Assignees: Janssen Products, LP, Medivir, ABInventors: Tim Hugo Maria Jonckers, Pierre Jean-Marie Bernard Raboisson, Koen Vandyck, Steven Maurice Paula Van Hoof, Lili Hu, Abdellah Tahri
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Patent number: 8933053Abstract: Phosphoramidate derivatives of 5-fluoro-2?-deoxyuridine are disclosed for use in the treatment of cancer, especially in the treatment of cancer where the patient shows resistance, for example, in a patient with cells with a lowered level of nucleoside transporter proteins and/or with nucleoside kinase-deficient cells and/or with mycoplasma-infected cells and/or with cells with a raised level of thymidylate synthase.Type: GrantFiled: February 29, 2012Date of Patent: January 13, 2015Assignee: NuCana BioMed LimitedInventors: Christopher McGuigan, Jan Balzarini, Magdalena Slusarczyk, Blanka Gonczy, Paola Murziani
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Publication number: 20150011497Abstract: 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 norovirus, with a nucleoside, a nucleotide and an analog thereof.Type: ApplicationFiled: June 24, 2014Publication date: January 8, 2015Inventors: Leonid Beigelman, Jerome Deval, Zhinan Jin
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Publication number: 20150004135Abstract: The present disclosure relates to compounds of Formula (I): Also disclosed are pharmaceutical compositions comprising compounds of Formula (I), methods of using the compounds of Formula (I) and/or compositions comprising the compounds of Formula (I) for the treatment of HCV.Type: ApplicationFiled: December 17, 2012Publication date: January 1, 2015Applicants: HOFFMAN-LA ROCHE INC., RIBOSCIENCE LLCInventors: Jing Zhang, Zhuming Zhang
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Patent number: 8916538Abstract: The present application relates to solid state forms, for example, crystalline forms of 2?-C-methyluridine-5?-(O-phenyl-N—(S)-1-(isopropoxycarbonyl)ethyl)thiophosphoramidate, pharmaceutical compositions that can include one or more solid forms of 2?-C-methyluridine-5?-(O-phenyl-N—(S)-1-(isopropoxycarbonyl)ethyl)thiophosphoramidate, and methods of treating or ameliorating diseases and/or conditions with one or more solid forms of 2?-C-methyluridine-5?-(O-phenyl-N—(S)-1-(isopropoxycarbonyl)ethyl)thiophosphoramidate. Also disclosed herein are methods of treating diseases and/or conditions with one or more solid forms of 2?-C-methyluridine-5?-(O-phenyl-N—(S)-1-(isopropoxycarbonyl)ethyl)thiophosphoramidate in combination with one or more other agents.Type: GrantFiled: March 11, 2013Date of Patent: December 23, 2014Assignee: Vertex Pharmaceuticals IncorporatedInventors: Anuj K. Kuldipkumar, Ales Medek, Lori Ann Ferris, Praveen Mudunuri, Young Chun Jung, David Richard Willcox, Michael Waldo, William Aloysius Nugent
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Publication number: 20140369959Abstract: The present invention relates to the use of nucleoside derivatives of formula (I) wherein the symbols are as the specification, and of pharmaceutically acceptable salts thereof and to pharmaceutical compositions containing such compounds.Type: ApplicationFiled: December 17, 2012Publication date: December 18, 2014Inventors: Mark Smith, Francisco Xavier Talamas, Jing Zhang, Zhuming Zhang
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Patent number: 8906880Abstract: Disclosed herein are phosphoramidate prodrugs of nucleoside derivatives for the treatment of viral infections in mammals, which is a compound, its stereoisomer, salt (acid or basic addition salt), hydrate, solvate, or crystalline form thereof, represented by the following structure: Also disclosed are methods of treatment, uses, and processes for preparing each of which utilize the compound represented by formula I.Type: GrantFiled: April 17, 2014Date of Patent: December 9, 2014Assignee: Gilead Pharmasset LLCInventors: Jinfa Du, Dhanapalan Nagarathnam, Michael Joseph Sofia, Peiyuan Wang
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Publication number: 20140356325Abstract: Compositions and methods relating to 2?-C-methyl nucleoside 5?-monophosphate derivative compounds are provided. In some embodiments, the novel compounds are useful to treat viral infections. In particular, 2?-C-methyl nucleoside 5?-monophosphate derivative compounds, stereoisomers, and pharmaceutically acceptable salts or prodrugs thereof, their preparation, and their uses for the treatment of viral infection are described.Type: ApplicationFiled: January 8, 2013Publication date: December 4, 2014Applicant: Ligand Pharmaceuticals IncorporatedInventors: Lin Zhi, K. Raja Reddy, Mark David Erion, Scott Hecker
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Publication number: 20140357595Abstract: This application describes methods of preventing, treating or reducing the risk of recurrence of a hepatitis C virus infection in a subject after the subject has received a liver transplant. Disclosed herein are methods of preventing or reducing the risk of recurrence of a hepatitis C virus infection in a subject after the subject has received a liver transplant, the methods comprising administering to the subject an effective amount of Compound 1. Also disclosed are methods of reducing HCV RNA levels to about 25 IU/mL or lower in a subject having received a liver transplant comprising administering to the subject an effective amount of Compound 1.Type: ApplicationFiled: June 2, 2014Publication date: December 4, 2014Applicant: Gilead Pharmasset LLCInventors: Jill M. Denning, John George McHutchison, G. Mani Subramanian, William Thomas Symonds, III
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Patent number: 8895531Abstract: The present invention includes compounds and compositions of ®-2?-fluoronucleoside phosphonates, as well as methods to treat HIV, HBV, HCV or abnormal cellular proliferation comprising administering said compounds or compositions.Type: GrantFiled: March 22, 2007Date of Patent: November 25, 2014Assignee: RFS Pharma LLCInventor: Junxing Shi
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Patent number: 8895516Abstract: Saccharide-protein conjugates having a new type of linker are described. The conjugates comprising the new linker are prepared from modified saccharides comprising a moiety of the formula (I): -A-N(R1)-L-M wherein: A is a bond, —C(O)— or —OC(O)—; R1 is selected from H or C1-C6 alkyl; L is a C1-C12 alkylene group; and M is a masked aldehyde group. The new linker is especially useful for preparing conjugates of Neisseria meningitidis serogroup A saccharide. Conjugates having this new linker have improved immunogenicity compared to other types of conjugates.Type: GrantFiled: September 1, 2003Date of Patent: November 25, 2014Assignee: Novartis AGInventors: Aldo Giannozzi, Giovanni Averani, Francesco Norelli, Paolo Costantino
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Publication number: 20140341847Abstract: The present disclosure relates to the compound of Formula I: Also disclosed are pharmaceutical compositions comprising the compound of Formula I, methods of using the compound of Formula I and/or compositions comprising the compound of Formula I for the treatment of HCV.Type: ApplicationFiled: May 15, 2014Publication date: November 20, 2014Applicant: Riboscience LLCInventors: Mark Smith, Klaus G. Klumpp
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Publication number: 20140343008Abstract: Disclosed are methods for treating hepatitis C in a human patient in need thereof that entails administering to the patient of about 350 mg of sofosbuvir and another anti-HCV compound.Type: ApplicationFiled: January 30, 2014Publication date: November 20, 2014Inventor: Cheng Yong Yang
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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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Patent number: 8871737Abstract: Disclosed herein are phosphorothioate nucleotide analogs, such as thiophosphoroamidate prodrugs and thiophosphates (including ?-thiomonophosphates, ?-thiodiphosphates, and ?-thiotriphosphates), methods of synthesizing phosphorothioate nucleotide analogs, such as thiophosphoramidate prodrugs, and thiophosphates and methods of treating viral infections, such as HCV, cancer, and/or parasitic diseases with the phosphorothioate nucleotide analogs, such as thiophosphoramidate prodrugs, and thiophosphates.Type: GrantFiled: September 19, 2011Date of Patent: October 28, 2014Assignee: Alios BioPharma, Inc.Inventors: David Bernard Smith, Jerome Deval, Natalia Dyatkina, Leonid Beigelman, Guangyi Wang
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Publication number: 20140315852Abstract: Disclosed herein are phosphoramidate prodrugs of nucleoside derivatives for the treatment of viral infections in mammals, which is a compound, its stereoisomer, salt (acid or basic addition salt), hydrate, solvate, or crystalline form thereof, represented by the following structure: Also disclosed are methods of treatment, uses, and processes for preparing each of which utilize the compound represented by formula I.Type: ApplicationFiled: April 17, 2014Publication date: October 23, 2014Applicant: Gilead Pharmasset LLCInventors: Jinfa Du, Dhanapalan Nagarathnam, Michael Joseph Sofia, Peiyuan Wang
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Publication number: 20140309164Abstract: Deuterated nucleoside analogs of Formula (I) and the pharmaceutically acceptable salts thereof are provided by this disclosure The variables, e.g., B1, Y, R1, R2, R3, R3?, R4, R5, R6, R7, R8, and R9 carry definitions set forth in the disclosure. Compounds of Formula (I) are deuterated at one or more positions and the deuterium enrichment at each deuterated positions is at least 50%. Compounds and salts of Formula (I) are useful for treating viral infections, including HCV infections.Type: ApplicationFiled: April 14, 2014Publication date: October 16, 2014Applicant: Achillion Pharmaceuticals, Inc.Inventors: Milind Deshpande, Jason Allan Wiles, Akihiro Hashimoto, Avinash Phadke
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Publication number: 20140308342Abstract: The present invention relates to chimeric (preferably, bifunctional) compounds, compositions comprising those compounds and methods of treating cancer in a patient or subject, especially including metastatic cancer where cancer cells exhibit overexpression (heightened expression) of cell surface urokinase-type plasminogen activator receptor (urokinase receptor) compared to normal (non-cancerous) cells. The compounds preferably covalently bind to the urokinase receptor and recruit native antibodies of the patient or subject where the antibodies can selectively degrade and/or deactivate targeted cancer cells through antibody-dependent cellular phagocytosis and/or antibody-dependent cellular cytotoxicity (ADCC) against a large number and variety of cancers, thus providing cancer cell death and/or an inhibition of growth, elaboration and/or metastasis of the cancer, including remission and cure of the patient's cancer.Type: ApplicationFiled: November 7, 2012Publication date: October 16, 2014Inventors: David A. Spiegel, Charles E. Jakobsche
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Publication number: 20140309189Abstract: A deuterated nucleoside analog of the formula and the pharmaceutically acceptable salts thereof are provided by this disclosure. The disclosure also includes pharmaceutical compositions comprising a compound or salt of the formula and a carrier. Compounds and salts of this formula are useful for treating viral infections, including HCV infections. A method for treating a host afflicted with hepatitis C or other disorders is also presented that includes administering an effective treatment amount of a nucleoside or nucleotide that has deuterium with at least 50% enrichment at the 5?-position of the nucleoside or nucleotide.Type: ApplicationFiled: April 14, 2014Publication date: October 16, 2014Applicant: Achillion Pharmaceuticals, Inc.Inventors: Milind Deshpande, Jason Allan Wiles, Akihiro Hashimoto, Avinash Phadke
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Publication number: 20140309187Abstract: Crystalline solid forms and the amorphous form of the anti-HCV compound 5-(3,3-dimethylbutyn-1-yl)-3-[(cis-4-hydroxy-4-{[(3S)-tetrahydrofuran-3-yloxy]methyl}cyclohexyl){[(1R)-4-methylcyclohex-3-en-1-yl]carbonyl}amino]thiophene-2-carboxylic acid (Compound I) were prepared and characterized in the solid state: Also provided are processes of manufacture and methods of using the crystalline forms.Type: ApplicationFiled: June 24, 2014Publication date: October 16, 2014Inventors: Ahmad Hashash, Scott Wolckenhauer, Bing Shi
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Publication number: 20140303108Abstract: 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: June 23, 2014Publication date: October 9, 2014Inventors: Leonid Beigelman, David Bernard Smith, Jerome Deval, Vivek Kumar Rajwanshi
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Publication number: 20140303113Abstract: Described herein is a combination that includes compound (A) and compound (B), or a pharmaceutically acceptable salt of the foregoing, for ameliorating and/or treating a hepatitis C viral infection.Type: ApplicationFiled: April 3, 2014Publication date: October 9, 2014Applicants: ALIOS BIOPHARMA, INC., VERTEX PHARMACEUTICALS, INC.Inventors: Julie Krop, Margaret James Koziel, Lawrence M. Blatt, John Fry, Sushmita Mukherjee Chanda
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Publication number: 20140294769Abstract: Provided herein are compounds, methods and pharmaceutical compositions for use in treatment of viral infections, including hepatitis C virus (HCV) infections, in hosts in need thereof. In certain embodiments, the compounds are 2?,4?-fluoro nucleosides according to Formula 1001: or a pharmaceutically acceptable salt, solvate, stereoisomeric form, tautomeric form, or polymorphic form thereof, wherein Base, RA, and PD are as described herein. In certain embodiments, 2?,4?-fluoro nucleosides are provided which display remarkable efficacy and bioavailability for the treatment of, for example, HCV infection in a human.Type: ApplicationFiled: April 1, 2014Publication date: October 2, 2014Inventors: Benjamin Alexander MAYES, Adel M. MOUSSA, Alistair James STEWART
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Patent number: 8846639Abstract: In certain embodiments, the present invention provides oligomeric compounds having favorable toxicity profiles and therapeutic indexes. Compounds of the present invention comprise bicyclic nucleosides. Certain such bicyclic nucleosides are pyrimidines that do not include a methyl group at the 5-carbon. Oligomeric compounds comprising such nucleosides are less toxic than compounds comprising bicyclic nucleosides that do include a methyl group at the 5-carbon. In certain embodiments, the present invention provides methods of preparing and using such compounds.Type: GrantFiled: April 3, 2009Date of Patent: September 30, 2014Assignee: Isis Pharmaceutical, Inc.Inventors: Eric E. Swayze, Andrew M. Siwkowski
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Patent number: 8846638Abstract: The present invention provides nucleoside phosphoramidate compounds of Formula I, where R1, R2a, R2b, R3, R4, R5a, R5b, R6, R7, R8a, R8b, M and W are as defined herein. The invention further includes pharmaceutical compositions comprising a compound of Formula I, methods of use of these compounds for treating a viral infection, and methods of producing these compounds.Type: GrantFiled: May 17, 2013Date of Patent: September 30, 2014Assignee: Enanta Pharmaceuticals, Inc.Inventors: Yat Sun Or, Jun Ma, Guoqiang Wang
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Patent number: 8846896Abstract: Disclosed herein are methods of preparing a phosphorothioate nucleotide analog, which are useful in treating diseases and/or conditions such as viral infections.Type: GrantFiled: March 11, 2013Date of Patent: September 30, 2014Inventors: Vladimir Serebryany, Jyanwei Liu, Leonid Beigelman, Young Chun Jung, Jamison Rose, Shereen Ibrahim, Cavan McKeon, Luigi Anzalone
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Patent number: 8846636Abstract: The disclosure provides nucleotide analogues that comprise tetrahydrofuranyl or tetrahydrothienyl moieties with quaternary centers at the 3? position, the pharmaceutical formulations comprising the analogues, and methods of using the analogues and formulations for treating, preventing, and/or inhibiting diseases or conditions associated with cancers and viruses.Type: GrantFiled: March 18, 2009Date of Patent: September 30, 2014Assignee: LCB Pharma Inc.Inventor: Yvan Guindon
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Publication number: 20140286903Abstract: This invention is directed to compounds of Formula (I) having the structure that are useful in the treatment of viral infections in mammals, particularly in humans, mediated, at least in part, by a virus in the Flaviviridae family of viruses.Type: ApplicationFiled: November 8, 2012Publication date: September 25, 2014Applicants: INHIBITEX, INC., UNIVERSITY COLLEGE CARDIFF CONSULTANTS LIMITEDInventors: Stanley Chamberlain, John Vernachio, Srinivas K. Battina, Changalvala V.S. Ramamurty, C. Srinivas Rao, Chris McGuigan, Andrea Brancale
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Publication number: 20140288020Abstract: Disclosed herein are phosphoramidate prodrugs of nucleoside derivatives for the treatment of viral infections in mammals, which is a compound, its stereoisomer, salt (acid or basic addition salt), hydrate, solvate, or crystalline form thereof, represented by the following structure: Also disclosed are methods of treatment, uses, and processes for preparing each of which utilize the compound represented by formula I.Type: ApplicationFiled: April 16, 2014Publication date: September 25, 2014Applicant: Gilead Pharmasset LLCInventors: Jinfa Du, Dhanapalan Nagarathnam, Michael Joseph Sofia, Peiyuan Wang
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Publication number: 20140271547Abstract: 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?-cyano, azido or amino nucleosides according to Formula 1001 or 2001: or a pharmaceutically acceptable salt, solvate, stereoisomeric form, tautomeric form, or polymorphic form thereof, wherein Base, W, R1 and R2 are as described herein.Type: ApplicationFiled: March 13, 2014Publication date: September 18, 2014Inventors: David DUKHAN, Christophe Claude PARSY, Gilles GOSSELIN, Jean-Francois GRIFFON, Guillaume BRANDT, Cyril B. DOUSSON
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Patent number: 8836218Abstract: Provided herein are methods of treating a proliferative disease in a subject, comprising administering to the subject a therapeutically effective amount of AC220 and a nucleoside analog, a topoisomerase inhibitor or an anthracycline, or a combination thereof.Type: GrantFiled: January 18, 2013Date of Patent: September 16, 2014Assignee: Ambit Biosciences CorporationInventors: Robert C. Armstrong, Barbara A. Belli
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Publication number: 20140256671Abstract: The invention relates to a composition comprising: (i) one or more of uridine and cytidine, or salts, phosphates, acyl derivatives or esters thereof; and (ii) a lipid fraction comprising at least one of docosahexaenoic acid (22:6; DHA), eicosapentaenoic acid (20:5; EPA) and docosapentaenoic acid (22:5; DPA), or esters thereof, for use in the improvement of executive function of a subject in need thereof, in particular an Alzheimer's or dementia patient.Type: ApplicationFiled: October 30, 2012Publication date: September 11, 2014Inventors: Martine Groenendijk, Anke Bongers
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Publication number: 20140255339Abstract: Provided herein are compounds, compositions and methods for the treatment of liver disorder, including HCV and/or HBV infections. Specifically, compound and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents.Type: ApplicationFiled: March 4, 2014Publication date: September 11, 2014Applicants: Idenix Pharmaceuticals, Inc., Universite Montpellier II, Centre National de la Recherche ScientifiqueInventors: Jean-Pierre SOMMADOSSI, Gilles GOSSELIN, Claire PIERRA, Christian PERIGAUD, Suzanne PEYROTTES
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Publication number: 20140248242Abstract: Provided herein are compounds, compositions and methods for the treatment of Flaviviridae infections, including HCV infections. In certain embodiments, the compounds are according to Formula 2001: where PD, Base, RA and RB are as provided herein. 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.Type: ApplicationFiled: March 3, 2014Publication date: September 4, 2014Inventors: Cyril B. DOUSSON, Benjamin Alexander MAYES, David DUKHAN, Adel M. MOUSSA, Alistair James STEWART
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Publication number: 20140249101Abstract: Disclosed herein is a method of treating a subject infected with hepatitis C virus, said method comprising administering to the subject for a time period an effective amount of sofosbuvir, an effective amount of ribavirin and an effective amount of ledipasvir. In one aspect, the method comprises administering to the subject an interferon-free treatment regimen comprising an effective amount of sofosbuvir, an effective amount of ribavirin and an effective amount of ledipasvir. In a particular aspect, the method is sufficient to produce an undetectable amount of HCV RNA in the subject for at least 12 weeks after the end of the time period.Type: ApplicationFiled: March 3, 2014Publication date: September 4, 2014Inventors: Xiao Ding, Robert H. Hyland, Phillip S. Pang, William Thomas Symonds, III
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Publication number: 20140248241Abstract: 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 3?-deoxy nucleoside compounds according to Formula 3001a or 3001b: or a pharmaceutically acceptable salts, solvates, stereoisomeric forms, tautomeric forms, or polymorphic forms thereof, wherein PD, Base1 and Base2 are as provided herein.Type: ApplicationFiled: March 3, 2014Publication date: September 4, 2014Inventors: Alistair James STEWART, Adel M. MOUSSA, Benjamin Alexander MAYES, Francois-Rene ALEXANDRE, Dominique SURLERAUX, Christophe Claude PARSY, Claire PIERRA, David DUKHAN, Gilles GOSSELIN
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Patent number: 8815830Abstract: The invention provides a compound of formula (I), wherein R1-R6 and X have any of the values described, as well as pharmaceutical compositions comprising such compounds and therapeutic methods comprising the administration of such compounds.Type: GrantFiled: March 28, 2014Date of Patent: August 26, 2014Assignee: Regents of the University of MinnesotaInventor: Carston R. Wagner
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Patent number: 8809265Abstract: The present invention features interferon- and ribavirin-free therapies for the treatment of HCV. Preferably, the treatment is over a shorter duration of treatment, such as no more than 12 weeks. In one aspect, the therapies comprise administering at least two direct acting antiviral agents without interferon and ribavirin to a subject with HCV infection. For example, the therapies comprise administering to a subject an effective amounts of therapeutic agent 1, therapeutic agent 2 (or therapeutic agent 3), and an inhibitor of cytochrome P450 (e.g., ritonavir).Type: GrantFiled: October 19, 2012Date of Patent: August 19, 2014Assignee: AbbVie Inc.Inventors: Barry M. Bernstein, Rajeev M. Menon, Amit Khatri, Sven Mensing, Sandeep Dutta, Daniel E. Cohen, Thomas J. Podsadecki, Scott C. Brun, Walid M. Awni, Emily O. Dumas, Cheri E. Klein
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Publication number: 20140228313Abstract: Contemplated compositions and methods are directed to prevent and/or treat various autoimmune diseases that are typically associated with glycan dysregulation, and especially autoimmune demyelinating diseases. Further especially contemplated aspects include animal models and systems for screening compounds to treat and/or prevent such diseases.Type: ApplicationFiled: January 17, 2014Publication date: August 14, 2014Applicants: The Regents of the University of California, Mount Sinai HospitalInventors: Michael Demetriou, James Dennis, Ken Siu-Kwong Lau
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Publication number: 20140221304Abstract: The present invention relates to 5?-Substituted Nucleoside Analogs of Formula (I): and pharmaceutically acceptable salts thereof, wherein B, X, Z, R1, R2, R3 and R3? are as defined herein. The present invention also relates to compositions comprising at least one 5?-Substituted Nucleoside Analog, and methods of using the 5?-Substituted Nucleoside Analogs for treating or preventing HCV infection in a patient.Type: ApplicationFiled: July 10, 2012Publication date: August 7, 2014Inventors: Vishal A. Verma, Ashok Arasappan, F. George Njoroge, Kevin X. Chen
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Publication number: 20140219958Abstract: In one aspect, the invention provides compounds represented by Formula I, and pharmaceutically acceptable salts, esters, stereoisomers, tautomers, solvates, and combinations thereof, pharmaceutical compositions comprising these compounds and the use of these compounds for treating a viral infection in a subject.Type: ApplicationFiled: January 31, 2014Publication date: August 7, 2014Applicant: ENANTA PHARMACEUTICALS, INC.Inventors: Jay R. Luly, Jun Ma, Guoqiang Wang, Yat Sun Or
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Publication number: 20140221306Abstract: Regarding Diquafosol ophthalmic solution comprising a chelating agent, formation of insoluble precipitates found in Diquafosol ophthalmic solution during its storage, as well as deterioration of the filtration performance in the course of production (filtration sterilization), have been inhibited. Further, in Diquafosol ophthalmic solution comprising a chelating agent, enhancement of preservative effectiveness has been confirmed. Accordingly, the present invention provides Diquafosol ophthalmic solution having physicochemical properties that are stable during the courses of production and distribution as well as the course of storage by a patient. Particularly in the course of production, the solution can be subjected to efficient filtration sterilization. Moreover, the solution has excellent preservative effectiveness.Type: ApplicationFiled: December 27, 2011Publication date: August 7, 2014Applicant: Santen Pharmaceutical Co. LtdInventors: Akiko Sakatani, Tatsuo Ikei, Koji Inagaki, Masaki Sonoda, Yoko Fukui, Mitsuaki Kuwano
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Publication number: 20140212491Abstract: Disclosed are pharmaceutical compositions having an effective amount of substantially amorphous ledipasvir and an effective amount of substantially crystalline sofosbuvir.Type: ApplicationFiled: January 30, 2014Publication date: July 31, 2014Inventors: Ben Chal, Erik Mogalian, Reza Oliyai, Rowchanak Pakdaman, Dimitrios Stefanidis, Vahid Zia
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Publication number: 20140213543Abstract: The invention provides a compound of formula (1), wherein R1-R6 and X have any of the values described, as well as pharmaceutical compositions comprising such compounds and therapeutic methods comprising the administration of such compounds.Type: ApplicationFiled: March 28, 2014Publication date: July 31, 2014Applicant: Regents of the University of MinnesotaInventor: Carston R. Wagner
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Publication number: 20140206640Abstract: The present invention relates to 2?-Azido Substituted Nucleoside Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein B, X, R1, R2 and R3 are as defined herein. The present invention also relates to compositions comprising at least one 2?-Azido Substituted Nucleoside Derivative, and methods of using the 2?-Azido Substituted Nucleoside Derivatives for treating or preventing HCV infection in a patient.Type: ApplicationFiled: April 11, 2012Publication date: July 24, 2014Applicant: Merck Sharp & Dohme Corp.Inventors: Vinay Girijavallabhan, F. George Njoroge, Stephane Bogen, Frank Bennett, Vishal Verma, Ashok Arasappan, Kevin X. Chen, Ying Huang, Angela Kerekes, Latha Nair, Dimitri Pissarnitski, Qun Dang, Ian Davies, David B. Olsen, Andrew Stamford, Joseph P. Vacca
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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: 20140187511Abstract: Disclosed herein are phosphoramidate prodrugs of nucleoside derivatives for the treatment of viral infections in mammals, which is a compound, its stereoisomer, salt (acid or basic addition salt), hydrate, solvate, or crystalline form thereof, represented by the following structure: Also disclosed are methods of treatment, uses, and processes for preparing each of which utilize the compound represented by formula I.Type: ApplicationFiled: August 29, 2013Publication date: July 3, 2014Applicant: GILEAD PHARMASSET LLCInventors: Jinfa Du, Dhanapalan Nagarathnam, Michael Joseph Sofia, Peiyuan Wang
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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: 20140178336Abstract: The disclosure is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.Type: ApplicationFiled: March 14, 2013Publication date: June 26, 2014Inventor: Gilead Sciences, Inc.
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Publication number: 20140178338Abstract: 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 according to Formula 1501: or a pharmaceutically acceptable salt, solvate, stereoisomeric form, tautomeric form or polymorphic form thereof, wherein B, PD, RA, RB, RC, L, M and Z are as described herein.Type: ApplicationFiled: December 17, 2013Publication date: June 26, 2014Inventors: Benjamin Alexander MAYES, Adel M. MOUSSA, Alistair James STEWART, Gilles GOSSELIN