Phosphorus Attached Directly Or Indirectly To The Diazine Ring By Nonionic Bonding Patents (Class 544/243)
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Patent number: 8680270Abstract: The presently disclosed subject matter is directed to metallo-oxidoreductase inhibitors having metal binding moities linked to a targeting moiety through a linking group or a direct bond, methods for screening for metallo-oxidoreductase inhibitors, and methods of treating an oxidoreductase related disorder by administering a metallo-oxidoreductase inhibitor to a subject in need of treatment thereof.Type: GrantFiled: November 21, 2007Date of Patent: March 25, 2014Assignee: Viamet Pharmaceuticals, Inc.Inventors: Robert J. Schotzinger, William J. Hoekstra
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Patent number: 8673885Abstract: Aromatic and alkyl thiocarbonates with and without a neighboring group that participates in the hydrolysis of a thiocarbonate are described. The aromatic or alkyl thiocarbonates can be used for the protection of sulfur during oligonucleotide synthesis. Their facile processes of manufacture and methods of using the same are provided.Type: GrantFiled: July 25, 2011Date of Patent: March 18, 2014Inventor: Robert Duff
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Patent number: 8674094Abstract: The present invention provides a new class of solids supports for synthesis of modified oligomers of nucleic acids, and nucleic acid probes that have a format expediently synthesized on the new supports. Exemplary solid supports include at least one quencher bound through a linker to the solid support. Various exemplary embodiments include a moiety that stabilizes a duplex, triplex or higher order aggregation (e.g., hybridization) of nucleic acids of which the oligomer of the invention is a component. Other components of the solid support include moieties that stabilize aggregations of nucleic acids, e.g., intercalators, minor groove binding moieties, bases modified with a stabilizing moiety (e.g., alkynyl moieties, and fluoroalkyl moieties), and conformational stabilizing moieties, such as those described in commonly owned U.S. Patent Application Publication No. 2007/0059752.Type: GrantFiled: July 28, 2011Date of Patent: March 18, 2014Assignee: Biosearch Technologies, Inc.Inventors: Ronald M. Cook, Matt Lyttle
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Patent number: 8673884Abstract: The present invention provides pyrimidinyl compounds of formula (I) and pharmaceutically acceptable salts thereof. These compounds may be used for the inhibition of influenza. In particular, the compounds of the invention may be used for the treatment or prophylaxis of influenza A, most particularly H1N1 or H5N1 influenza. The compounds of the invention can also be used for the treatment or prophylaxis of a disease caused by Vibrio cholerae, Clostridium perfringens, Streptococcus pneumoniae, Arthrobacter sialophilus, an orthomyxovirus, a paramyxovirus, a parainfluenza virus, mumps virus, Newcastle disease virus, fowl plague virus or Sendai virus.Type: GrantFiled: February 4, 2009Date of Patent: March 18, 2014Assignees: Versitech Limited, British Columbia Cancer Agency BranchInventors: Steven J. Jones, Allan Sik-Yin Lau, Jianghong An, Hing Yee Law, Chun Wai Davy Lee, Lit Man Poon
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Publication number: 20140073786Abstract: The present disclosure describes cyclohexenyl nucleic acid analogs, oligomeric compounds prepared therefrom and methods of using the oligomeric compounds. More particularly, cyclohexenyl nucleic acid analogs are provided, having one or more chiral substituents, that are expected to be useful for enhancing properties of oligomeric compounds including nuclease resistance and binding affinity. In some embodiments, the oligomeric compounds provided herein hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA.Type: ApplicationFiled: November 1, 2013Publication date: March 13, 2014Applicant: Isis Pharmaceuticals, Inc.Inventors: Punit P. Seth, Eric E. Swayze
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Publication number: 20140066406Abstract: The invention features compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.Type: ApplicationFiled: March 15, 2013Publication date: March 6, 2014Applicant: ARIAD PHARMACEUTICALS, INC.Inventor: ARIAD PHARMACEUTICALS, INC.
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Publication number: 20140045794Abstract: The present invention relates to phosphonate compounds, compositions containing them, processes for obtaining them, and their use for treating a variety of medical disorders, e.g., osteoporosis and other disorders of bone metabolism, cancer, viral infections, and the like.Type: ApplicationFiled: October 21, 2013Publication date: February 13, 2014Applicant: The Regents of the University of CaliforniaInventors: Karl Y. Hostetler, James R. Beadle
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Publication number: 20140031318Abstract: The invention relates to solid forms of the Formula (I) wherein X is —PO(OH)2, —PO(OH)O?M+, or —PO(O?)2.2M+, wherein M is a monovalent cation such as Na+, K+, Li+, or NH4+. The invention also provides pharmaceutically acceptable compositions comprising the solid form of the compound and method of using the compositions in the treatment of various disorders.Type: ApplicationFiled: July 18, 2013Publication date: January 30, 2014Inventors: Hardwin O'DOWD, DAINIUS MACIKENAS, Bin SONG
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Publication number: 20130316970Abstract: The object of the invention are nucleotide analogues, antiviral pro-nucleotides, a use of nucleotide analogues and pharmaceutical composition, a phosphorylating agent for synthesis of nucleotide analogue, and a method of synthesis of nucleotide analogue. More precisely, the invention applies to the new group of nucleotide analogues and their use in partial or complete inhibition of human immunodeficiency virus (HIV).Type: ApplicationFiled: October 13, 2011Publication date: November 28, 2013Applicants: NARODOWY INSTYTUT LEKOW, INSTYTUT CHEMII BIOORGANICZNEJ PANInventors: Adam Kraszewski, Joanna Romanowska, Michal Sobkowski, Agnieszka Szymanska-Michalak, Jacek Stawinski, Jerzy Boryski, Andrzej Lipniacki, Andrzej Piasek
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Publication number: 20130310342Abstract: Disclosed are compounds, pharmaceutical compositions containing those compounds, and uses of the compounds and compositions as modulators of CK1, CK1?1, CK1?2, CK1?3, CK2, Pim 1, Pim2, Pim3, the TGF? pathway, the Wnt pathway, the JAK/STAT pathway, the AKT pathway, and/or the mTOR pathway. Uses are also disclosed for the treatment or prevention of a range of therapeutic indications due at least in part to aberrant physiological activity of CK1, CK1?1, CK1?2, CK1?3, CK2, Pim 1, Pim2, Pim3, the TGF? pathway, the Wnt pathway, the JAK/STAT pathway, the AKT pathway, and/or the mTOR pathway.Type: ApplicationFiled: October 24, 2012Publication date: November 21, 2013Inventors: Carmen M. Baldino, Justin L. Caserta, Chee-Seng Lee, Stephane A. Dumas, Yvonne L. Flanders
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Patent number: 8586744Abstract: The invention is related to a method of treating disorders associated with hepatitis C by administering to an individual a pharmaceutical composition which comprises a therapeutically effective amount of an anti-viral phosphinate compound.Type: GrantFiled: October 27, 2010Date of Patent: November 19, 2013Assignee: Gilead Sciences, Inc.Inventors: Anthony Casarez, Kleem Chaudhary, Aesop Cho, Michael Clarke, Edward Doerffler, Maria Fardis, Choung U. Kim, Hyungjung Pyun, Xiaoning C. Sheng, Jianying Wang
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Publication number: 20130289002Abstract: The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof wherein X and R are as defined herein. The compounds of formula (I) are useful as gyrase and/or topoisomerase IV inhibitors for treating bacterial infections. The compounds of formula (I) either possess a broad range of anti-bacterial activity and advantageous toxicological properties or are prodrugs of compounds having said activity.Type: ApplicationFiled: June 3, 2013Publication date: October 31, 2013Inventors: Arnaud Le Tiran, Anne-Laure Grillot, Paul S. Charifson, Youssef Laafiret Bennani, Hardwin O'Dowd, Emanuele Perola
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Patent number: 8569478Abstract: Compounds, methods and compositions for treating a host infected with human immunodeficiency virus and hepatitis B virus comprising administering an effective amount of a described 4?-C-substituted ?-D- and ?-L-nucleoside or a pharmaceutically acceptable salt or prodrug thereof, are provided.Type: GrantFiled: September 26, 2006Date of Patent: October 29, 2013Assignee: Gilead Pharmasset LLCInventors: Jinfa Du, Phillip Furman, Michael Joseph Sofia
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Patent number: 8569321Abstract: The disclosure describes methods of synthesis of phosphonate ester derivatives. Preferred methods according to the disclosure allow for large-scale preparation of phosphonate ester compounds having high purity. In some embodiments, preferred methods according to the disclosure also allow for the preparation of phosphonate ester derivatives without the use of chromatographic purification methods and in better yield than previously used methods for preparing such compounds. Also disclosed are morphic forms of phosphonate ester derivatives.Type: GrantFiled: August 31, 2011Date of Patent: October 29, 2013Assignee: Chimerix, Inc.Inventors: Roy W. Ware, Merrick R. Almond, Bernhard M. Lampert
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Patent number: 8563569Abstract: Disclosed are compounds of formula I, compositions containing them, and methods of use for the compounds and compositions in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK 2 and JAK3, are therapeutically useful.Type: GrantFiled: October 27, 2011Date of Patent: October 22, 2013Assignee: Rigel Pharmaceuticals, Inc.Inventors: Yan Chen, Vanessa Taylor, Rajinder Singh
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Patent number: 8563716Abstract: Disclosed are compounds of formula I, compositions containing them, and methods of use for the compounds and compositions in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK2 and JAK3, are therapeutically useful.Type: GrantFiled: September 22, 2011Date of Patent: October 22, 2013Assignee: Rigel Pharmaceuticals, Inc.Inventors: Hui Li, Yan Chen, Rajinder Singh
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Publication number: 20130274465Abstract: Immunopotentiators can be adsorbed to insoluble metal salts, such as aluminium salts, to modify their pharmacokinetics, pharmacodynamics, intramuscular retention time, and/or immunostimulatory effect. Immunopotentiators are modified to introduce a moiety, such as a phosphonate group, which can mediate adsorption. These modified compounds can retain or improve their in vivo immunological activity even when delivered in an adsorbed form.Type: ApplicationFiled: September 1, 2011Publication date: October 17, 2013Applicants: IRM LLC, NOVARTIS AGInventors: Manmohan Singh, David A.G. Skibinski, Tom Yao-Hsiang Wu, Yongkai Li, Alex Cortez, Xiaoyue Zhang, Yefen Zou, Timothy Z. Hoffman, Jianfeng Pan, Kathy Yue
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Patent number: 8552021Abstract: Compounds of formula I: including any possible stereoisomers thereof, wherein: R1 is hydrogen, —C(?O)R6 or —C(?O)CHR7—NH2; R2 is hydrogen; or C1-C6alkyl or phenyl, either of which is optionally substituted with 1, 2 or 3 substituents each independently selected from halo, C1-C6alkyl, C2-C6-alkenyl and C1-C6alkoxy, hydroxy or amino, or R2 is naphtyl; or R2 is indolyl, R3 is hydrogen, C1-C6alkyl, benzyl; R4 is hydrogen, C1-C6alkyl, benzyl; or R3 and R4 together with the carbon atom to which they are attached form C3-C7cycloalkyl; R5 is C1-C10alkyl, C3-C7-cycloalkyl, benzyl, or phenyl, any of which being optionally substituted with 1, 2 or 3 substituents each independently selected from hydroxy, C1-C6alkoxy, amino, mono- and diC1-C6alkylamino; R6 is C1-C6 alkyl; R7 is C1-C6 alkyl; R8 is hydrogen or halogen; or a pharmaceutically acceptable salt or solvate thereof are useful in the prophylaxis or treatment of HCV infections.Type: GrantFiled: September 29, 2010Date of Patent: October 8, 2013Assignees: Janssen Products, L.P., Medivir ABInventors: Tim Hugo Maria Jonckers, Pierre Jean-Marie Bernard Raboisson, Koen Vandyck, Michael Pelcman, Bengt Christian Sund, Horst Jurgen Wahling, Pedro Manuel Passos Pinho, Anna Winqvist, Karl Magnus Nilsson
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Publication number: 20130261086Abstract: Compounds of Formula (I): wherein variables are defined herein, and pharmaceutically acceptable salts, synthesis, intermediates, formulations, and methods of disease treatment therewith, including cancers for which FAK inhibition is beneficial.Type: ApplicationFiled: November 29, 2011Publication date: October 3, 2013Applicant: OSI Pharmaceuticals, LLCInventors: Andrew P. Crew, Hanqing Dong, Caterina Ferraro, Dan Sherman, Kam W. Siu
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Publication number: 20130231307Abstract: Compounds of formula (I) wherein A represents a nucleobase or a derivative thereof, n is equal to 0 or 1 and R?, R? are carbonic chain, and R10 is hydrogen or a carbonic chain for their use as antiviral agents.Type: ApplicationFiled: June 1, 2011Publication date: September 5, 2013Applicants: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE, KATHOLIEKE UNIVERSITEIT LEUVEN-K.U. LEUVEN R&D, UNIVERSITE DE ORLEANSInventors: Luigi A. Agrofoglio, Vincent Roy, Hugo Pradere, Jan Balzarini, Robert Snoeck, Graciela Andrei
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Patent number: 8524901Abstract: Disclosed are compounds of formula I, compositions containing them, and methods of use for the compounds and compositions in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK 2 and JAK3, are therapeutically useful.Type: GrantFiled: September 22, 2011Date of Patent: September 3, 2013Assignee: Rigel Pharmaceuticals, Inc.Inventors: Hui Li, Yan Chen, Rajinder Singh
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Publication number: 20130225528Abstract: The invention features compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.Type: ApplicationFiled: March 15, 2013Publication date: August 29, 2013Applicant: ARIAD PHARMACEUTICALS, INC.Inventor: ARIAD Pharmaceuticals, Inc.
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Publication number: 20130225527Abstract: The invention features compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.Type: ApplicationFiled: March 15, 2013Publication date: August 29, 2013Applicant: ARIAD PHARMACEUTICALS, INC.Inventor: ARIAD PHARMACEUTICALS, INC.
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Patent number: 8518912Abstract: The invention relates to 2-phenyl-pyrimidine derivatives containing a phosphonic acid motif and their use as P2Y12 receptor antagonists in the treatment and/or prevention of peripheral vascular, of visceral-, hepatic- and renal-vascular, of cardiovascular and of cerebrovascular diseases or conditions associated with platelet aggregation, including thrombosis in humans and other mammals. (I).Type: GrantFiled: November 28, 2008Date of Patent: August 27, 2013Assignee: Actelion Pharmaceuticals Ltd.Inventors: Eva Caroff, Kurt Hilpert, Francis Hubler, Emmanuel Meyer, Dorte Renneberg
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Patent number: 8512820Abstract: Ionic mesogenic compounds of formula (I) can be used to form liquid crystal displays, such as ferroelectric liquid crystal displays, having enhanced anti-image sticking properties. The mesogenic compounds may contain a cationic group such as an ammonium or phosphonium group bonded to an alkyl chain that is terminally bonded to a para-substituted pyrimidyl benzene moiety. The counterion can be an organic or inorganic anion. The compounds can be used either as dopants in art ferroelectric liquid crystal compositions to reduce image sticking, or can be used as the primary or predominant component of a liquid crystal display system. Additional compounds, devices, and methods are disclosed.Type: GrantFiled: June 14, 2011Date of Patent: August 20, 2013Assignee: Citizen Finetech Miyota Co., Ltd.Inventors: Yongqiang Zhang, Su Yang
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Publication number: 20130157979Abstract: The present invention relates to phosphate esters of compounds that inhibit bacterial gyrase and/or Topoisomerase IV and pharmaceutical compositions thereof. These phosphate esters are useful for treating bacterial infections.Type: ApplicationFiled: June 20, 2012Publication date: June 20, 2013Inventors: Youssef Laafiret Bennani, Paul S. Charifson, Anne-Laure Grillot, Arnaud Le Tiran, Hardwin O'Dowd
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Publication number: 20130137661Abstract: Disclosed are compounds useful as gonadotrophin-releasing hormone (“GnRH”) receptor antagonist.Type: ApplicationFiled: November 19, 2010Publication date: May 30, 2013Applicant: SK CHEMICALS CO. LTD.Inventors: Seon Mi Kim, Min Hee Lee, Jae Sun Kim, Hoe Chul Jung, So Young Lee, Soo Min Lee, Eun Jeong Kim, Eui Sun Park, Sung Hoon Park, Bong Yong Lee, Key An Um
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Publication number: 20130131019Abstract: The present invention relates to novel compounds that contain PNA units substituted with phosphonic acid ester functions or phosphonic acid functions, and have at least one chiral center. The compounds may be used for the treatment of viral diseases, such as AIDS.Type: ApplicationFiled: June 19, 2012Publication date: May 23, 2013Applicant: Ugichem GmbHInventors: Thomas Lindhorst, Birgit Werner, Holger Bock
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Publication number: 20130126792Abstract: The present invention relates to compounds of the formula (I), to the use of compounds of the formula (I) in electronic devices and electronic devices comprising one or more compounds of the formula (I). The invention furthermore relates to the preparation of the compounds of the formula (I) and to formulations comprising one or more compounds of the formula (I).Type: ApplicationFiled: July 12, 2011Publication date: May 23, 2013Applicant: Merck Patent GmbHInventors: Irina Martynova, Adam W. Franz, Christof Pflumm, Amir Hossain Parham, Arne Buesing, Rémi Manouk Anémian, Anja Gerhard
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Publication number: 20130130378Abstract: This invention relates to acyclic and abasic nucleosides and oligonucleotides prepared therefrom. For instance, oligonucleotides can be prepared having one or more of the following formulas (I-III):, or isomers thereof.Type: ApplicationFiled: April 22, 2011Publication date: May 23, 2013Applicant: ALNYLAM PHARMACEUTICALS, INC.Inventors: Muthiah Manoharan, Kallanthottathil G. Rajeev, Jeremy Lackey, Narayanannair K. Jayaprakash
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Publication number: 20130121963Abstract: This disclosure relates to novel N-phenyl-2-pyrimidineamines and pharmaceutically acceptable salts thereof. This disclosure also provides compositions comprising a compound of this disclosure and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering protein-tyrosine kinase inhibitors.Type: ApplicationFiled: May 16, 2012Publication date: May 16, 2013Applicant: Concert Pharmaceuticals Inc.Inventors: Scott L. Harbeson, Julie F. Liu, Roger Tung
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Patent number: 8426388Abstract: A compound of the formula is disclosed as a prodrug of an HIV protease inhibitor. Methods and compositions for inhibiting HIV protease activity and treating HIV infection are also disclosed.Type: GrantFiled: April 7, 2010Date of Patent: April 23, 2013Assignee: AbbVie Inc.Inventors: David A. DeGoey, William J. Flosi, David J. Grampovnik, Larry L. Klein, Dale J. Kempf, Xiu C. Wang
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Patent number: 8399433Abstract: Compounds of Formula 1, as shown below and defined herein: and pharmaceutically acceptable salts, synthesis, intermediates, formulations, and methods of disease treatment therewith, including cancers mediated at least in part by FAK.Type: GrantFiled: June 1, 2010Date of Patent: March 19, 2013Assignee: OSI Pharmaceuticals, LLCInventors: Rama Devi Appari, Xin Chen, Ramesh Chilukuri, Andrew P. Crew, Hanqing Dong, Caterina Ferraro, Kenneth Foreman, Ramesh C. Gupta, An-Hu Li, Dan Sherman, Kathryn M. Stolz, Brian Volk, Robert Zahler
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Publication number: 20130065858Abstract: The present invention provides compounds useful as inhibitors of Raf protein kinase. The present invention also provides compositions thereof, and methods of treating Raf-mediated diseases.Type: ApplicationFiled: October 22, 2012Publication date: March 14, 2013Applicants: SUNESIS PHARMACEUTICALS, INC., MILLENNIUM PHARMACEUTICALS, INC.Inventors: MILLENNIUM PHARMACEUTICALS, INC., SUNESIS PHARMACEUTICALS, INC.
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Publication number: 20130053345Abstract: Novel compounds of structure Formula I: or an enantiomer, diastereomer, tautomer, prodrug or salt thereof, wherein A, D, Di, E, J, L, n, Q, R2 and R4 are defined herein, are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR119 G protein-coupled receptor modulator therapy. Thus, the disclosure also concerns compositions comprising these novel compounds and methods of treating diseases or conditions related to the activity of the GPR119 G protein-coupled receptor by using any of these novel compounds or a composition comprising any of such novel compounds.Type: ApplicationFiled: May 4, 2011Publication date: February 28, 2013Inventors: Xiang-Yang Ye, Dean A. Wacker, Jeffrey A. Robl, Ying Wang
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Publication number: 20130045950Abstract: The present invention relates to phosphonate compounds, compositions containing them, processes for obtaining them, and their use for treating a variety of medical disorders, e.g., osteoporosis and other disorders of bone metabolism, cancer, viral infections, and the like.Type: ApplicationFiled: October 4, 2012Publication date: February 21, 2013Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventor: THE REGENTS OF THE UNIVERSITY OF CALIF
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Publication number: 20130029940Abstract: There are provided, inter alia, acyclic nucleoside phosphonate compounds having reduced toxicity and enhanced antiviral activity, and pharmaceutically accepted salts and solvates thereof. There are also provided methods of using the disclosed compounds for inhibiting viral RNA-dependent RNA polymerase, inhibiting viral reverse transcriptase, inhibiting replication of virus, including hepatitis C virus or a human retrovirus, and treating a subject infected with a virus, including hepatitis C virus or a human retrovirus.Type: ApplicationFiled: October 11, 2012Publication date: January 31, 2013Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventor: The Regents of the University of California
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Patent number: 8354421Abstract: The invention is related to compounds of Formula (I): or a pharmaceutically acceptable salt, solvate, ester, and/or phosphonate thereof, compositions containing such compounds, and therapeutic methods that include the administration of such compounds.Type: GrantFiled: June 26, 2008Date of Patent: January 15, 2013Assignee: Korea Research Insitute of Chemical TechnologyInventors: Gong-Xin He, Choung U. Kim, Michael L. Mitchell, Lianhong Xu
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Patent number: 8354530Abstract: Present invention represents process for the preparation of HMG-CoA reductase inhibitors, in particular rosuvastatin calcium introducing L-malic acid as the source of chirality for the side chain.Type: GrantFiled: July 26, 2006Date of Patent: January 15, 2013Assignee: Lek Pharmaceuticals d. dInventor: Marko Zlicar
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Patent number: 8349834Abstract: This invention relates to certain unsaturated fatty acid derivatives of therapeutically active 1,3-dioxolane nucleoside analogues and to pharmaceutical formulations containing them. The said derivatives fall within formula (I). Compounds of formula (I) can be used in the treatment of a cancerous disease, including solid tumors and haematological cancers such as leukaemias, lymphomas and multiple myelomas.Type: GrantFiled: December 7, 2006Date of Patent: January 8, 2013Assignee: Clavis Pharma ASInventors: Finn Myhren, Marit Liland Sandvold, Steinar Hagen, Ole Henrik Eriksen
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Publication number: 20120316135Abstract: The invention features compounds, pharmaceutical compositions and methods for treating patients who have an EGFR-driven cancer of formula I: wherein the variables are as defined herein.Type: ApplicationFiled: May 4, 2012Publication date: December 13, 2012Applicant: ARIAD Pharmaceuticals, Inc.Inventors: David C. Dalgarno, Wei-Sheng Huang, William C. Shakespeare, Yihan Wang, Xiaotian Zhu
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Publication number: 20120309705Abstract: The present invention includes novel 3?-deoxy-3?-methylidene-?-L-nucleosides, pharmaceutical composition comprising such compounds, as well as the methods to treat or to prevent viral infections and in particular HBV and/or HIV infections.Type: ApplicationFiled: December 14, 2010Publication date: December 6, 2012Applicant: NOVADEX PHARMACEUTICALS ABInventors: Xiao Xiong Zhou, Staffan Torssell, Olov Wallner, Piaoyang Sun
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Publication number: 20120283219Abstract: The present invention relates novel diaminopteridine derivatives, their compositions and method of treatment comprising the same for use as anti-infectives.Type: ApplicationFiled: March 25, 2010Publication date: November 8, 2012Inventors: Philip D.G. Coish, Phil Wickens, Brian R. Dixon, David Osterman, Uday R. Khire, Manuel Navia, Judd Berman, Harpreet Kaur, Jeffrey Wilson, Dennis Underwood
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Publication number: 20120277191Abstract: Cidofovir is obtained in different forms, including amorphous cidofovir, crystalline anhydrous cidofovir, crystalline cidofovir monohydrate, and crystalline cidofovir dihydrate, including various polymorphs.Type: ApplicationFiled: April 6, 2012Publication date: November 1, 2012Applicant: Johnson Matthey Public Limited CompanyInventors: George Scott Wilson, Angela Barkley, Jurjus Jurayj
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Publication number: 20120277192Abstract: The present invention provides novel pyrimidine amines of formula (I) which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD and rheumatoid arthritis.Type: ApplicationFiled: December 15, 2010Publication date: November 1, 2012Inventors: Michael D. Altman, Brian M. Andresen, Kenneth L. Arrington, Sathesh Bhat, Jason Burch, Kaleen Konrad Childers, Bernard Cote, Maria Emilia Di Francesco, Anthony Donofrio, Kristina Dupont-Gaudet, John Michael Ellis, Christian Fischer, Jean-Francois Fournier, Jacques Yves Gauthier, Jonathan Grimm, Daniel Guay, David Joseph Guerin, Andrew M. Haidle, Solomon Kattar, Sandra Lee Knowles, Chaomin Li, Jongwon Lim, Michelle R. Machacek, Matthew L. Maddess, Alan B. Northrup, Brendan M. O'Boyle, Ryan D. Otte, Alessia Petrocchi, Michael H. Reutershan, Joel S. Robichaud, Eric Romeo, Adam J. Schell, Tony Siu, Kerrie B. Spencer, Brandon M. Taoka, B. Wesley Trotter, Hyun Chong Woo, Hua Zhou
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Publication number: 20120202776Abstract: The invention features compounds of the general formula (I) in which the variable groups are as defined herein, and to their preparation and use.Type: ApplicationFiled: May 21, 2009Publication date: August 9, 2012Applicant: ARIAD Pharmaceuticals, Inc.Inventors: Yihan Wang, Wei-Sheng Huang, Shuangying Liu, William C. Shakespeare, R. Mathew Thomas, Jiwei Qi, Feng Li, Xiaotian Zhu, Anna Kohlmann, David C. Dalgarno, Jan Antoinette C. Romero, Dong Zou
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Publication number: 20120184512Abstract: The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof wherein X and R are as defined herein. The compounds of formula (I) are useful as gyrase and/or topoisomerase IV inhibitors for treating bacterial infections. The compounds of formula (I) either possess a broad range of anti-bacterial activity and advantageous toxicological properties or are prodrugs of compounds having said activity.Type: ApplicationFiled: January 13, 2012Publication date: July 19, 2012Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Arnaud Le Tiran, Anne-Laure Grillot, Paul S. Charifson, Yousef Laafiret Bennani, Hardwin O'Dowd, Emanuele Perola
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Patent number: 8222257Abstract: Compounds and compositions are provided for treatment, prevention, or amelioration of a variety of medical disorders associated with viral infections and/or cell proliferation. The compounds provided herein are 5-phosphono-pent-2-en-1-yl nucleosides and esters thereof.Type: GrantFiled: March 30, 2006Date of Patent: July 17, 2012Assignee: The Regents of the University of CaliforniaInventors: Karl Y. Hostetler, James R. Beadle, Hyunah Choo
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Publication number: 20120177681Abstract: Immunopotentiators can be adsorbed to insoluble metal salts, such as aluminium salts, to modify their pharmacokinetics, pharmacodynamics, intramuscular retention time, and/or immunostimulatory effect. Immunopotentiators are modified to introduce a moiety, such as a phosphonate group, which can mediate adsorption. These modified compounds can retain or improve their in vivo immunological activity even when delivered in an adsorbed form.Type: ApplicationFiled: September 1, 2011Publication date: July 12, 2012Inventors: Manmohan Singh, David A.G. Skibinski, Tom Yao-Hsiang Wu, Yongkai Li, Alex Cortez, Xiaoyue Zhang, Yefen Zou, Timothy Z. Hoffman, Jianfeng Pan, Kathy Yue
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Publication number: 20120157412Abstract: The present invention is directed to substituted pyrimidine compounds of formula (I): and forms thereof, their synthesis and use for treating, preventing or ameliorating a chronic or acute protein kinase mediated disease, disorder or condition.Type: ApplicationFiled: February 28, 2012Publication date: June 21, 2012Inventors: Kathleen A. Battista, Gilles C. Bignan, Guozhang Xu, Lily Lee, Terry V. Hughes, Steven K. Wetter, Peter J. Connolly, Marta C. Abad, Stuart L. Emanuel, Prabha S. Karnachi, Steven A. Middleton