1,2,3-triazoles (including Hydrogenated) Patents (Class 548/255)
  • Patent number: 10246427
    Abstract: 1,2,3-triazolyl cyclohexanol derivatives have been disclosed and their use as ligands accelerating the copper(I)-catalyzed azide-alkyne cycloaddition and the zinc(II)-catalyzed azide-nitrile cycloaddition.
    Type: Grant
    Filed: June 7, 2016
    Date of Patent: April 2, 2019
    Assignee: UNIWERSYTET JAGIELLONSKI
    Inventors: Przemyslaw Szafranski, Patryk Kasza, Marek Cegla
  • Patent number: 10093633
    Abstract: The present invention provides novel functionalized mixtures 4- and 5-vinyl substituted regioisomers of 1,2,3-triazoles via 1,3-dipolar cycloaddition. Functionalized alkyne moieties with a terminal alcoholic functionality are reacted with functionalized organic moieties with a terminal leaving group and an azide to provide an alcoholic functionalized mixture of 4- and 5-substituted regioisomers of 1,2,3-triazole moieties. The mixture may be converted to a wide variety of useful functionalized mixtures of 4- and 5-vinyl substituted regioisomers of 1,2,3-triazole moieties, which in turn can be converted to a wide variety of useful polymers The novel alcoholic functionalized mixtures of 4- and 5-substituted regioisomers can be separated by chromatography to provide the purified 4- and 5-alcoholic functionalized substituted 1,2,3-triazole moieties. The novel compounds of the invention can be employed in a wide variety of compositions (Formulae (I), (II)); wherein R1, R2, R3, and R4, are defined herein.
    Type: Grant
    Filed: December 7, 2015
    Date of Patent: October 9, 2018
    Assignee: ISP Investments LLC
    Inventors: Osama M. Musa, Brian Marr
  • Patent number: 10070645
    Abstract: The present invention relates to fungicidal N-cycloalkyl-N-{[2-(1-substitutedcycloalkyl)phenyl]methylene} carboxamide derivatives and their thiocarbonyl derivatives, their process of preparation and intermediate compounds for their preparation, their use as fungicides, particularly in the form of fungicidal compositions and methods for the control of phytopathogenic fungi of plants using these compounds or their compositions.
    Type: Grant
    Filed: December 4, 2014
    Date of Patent: September 11, 2018
    Assignee: BAYER CROPSCIENCE AKTIENGESELLSCHAFT
    Inventors: Pierre Cristau, Philippe Desbordes, Julie Geist, Lionel Nicolas, Philippe Rinolfi, Jan-Peter Schmidt, Tomoki Tsuchiya, Jean-Pierre Vors, Ulrike Wachendorff-Neumann
  • Patent number: 9957294
    Abstract: A peptide is disclosed of the general structure: Z—W—Y, wherein Z and Y are independently a one to eight amino acid sequence wherein the amino acids are selected from glycine and alanine and W is a non-hydrolyzable pHis analogue. Such peptides can be used to produce sequence-independent anti-phosphohistidine antibodies. Also provided are antibodies that specifically bind to a peptide comprising a phosphohistidine (or a non-hydrolyzable pHis analogue) but fail to specifically bind to an identical peptide containing histidine instead of phosphohistidine.
    Type: Grant
    Filed: September 12, 2014
    Date of Patent: May 1, 2018
    Assignees: Salk Institute for Biological Studies, Sanofi
    Inventors: Magda Stankova, Fahad Al-Obeidi, Jacques Mauger, Robert A. Binnie, Tony Hunter, Jill Meisenhelder, Stephen Rush Fuhs
  • Patent number: 9650404
    Abstract: The invention relates to novel curcumin derivatives in which one or two of the phenolic groups have been modified.
    Type: Grant
    Filed: February 25, 2011
    Date of Patent: May 16, 2017
    Assignee: RESEARCH FOUNDATION OF THE CITY UNIVERSITY OF NEW YORK
    Inventors: Krishnaswami Raja, Alejandra Alonso, Probal Banerjee, Sukanta Dolai, Christopher Corbo, Saadyah Averick, Amit Mogha, Shawon Debnath
  • Patent number: 9321738
    Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of inflammatory diseases and disorders such as, for example, pulmonary fibrosis.
    Type: Grant
    Filed: June 17, 2013
    Date of Patent: April 26, 2016
    Assignee: HOFFMAN-LA ROCHE INC.
    Inventors: Stephen Deems Gabriel, Matthew Michael Hamilton, Matthew C. Lucas, Yimin Qian, Achyutharao Sidduri
  • Patent number: 9312499
    Abstract: Compounds having a structure of Formula I, where G1 has the formula having the structure are described. In the structure of Formula I: Z1 to Z24 are each independently selected from group consisting of carbon and nitrogen; p is an integer from 1 to 10; adjacent carbazole groups G11, G12, and G13 are each bonded together either by a 9N-2C bond or a 9N-3C bond; G1 can include at least one 9N-2C intercarbazole bond and at least one 9N-3C intercarbazole bond; L and G2 are each independently selected from the group consisting of alkyl, aryl, or heteroaryl, which may be further substituted; m and n are both integers; and m+n ranges from 1 to the maximum number of possible substituents on L. Formulations and devices, such as an OLEDs, that include the compound of Formula I are also described.
    Type: Grant
    Filed: January 5, 2015
    Date of Patent: April 12, 2016
    Assignee: UNIVERSAL DISPLAY CORPORATION
    Inventor: Lichang Zeng
  • Patent number: 9302997
    Abstract: A copper catalyzed click chemistry ligation process is employed to bind azides and terminal acetylenes to provide 1,4-disubstituted 1,2,3-triazole triazoles. The process comprises contacting a solution of an organic azide and a terminal alkyne with a source of catalytic Cu(I) ion to form a 1,4-disubstituted 1,2,3-triazole, wherein the source of Cu(I) ion comprises Cu(II) and a metal capable of reducing Cu(II) to Cu(I). In some embodiments, the metal capable of reducing Cu(II) to Cu(I) is selected from the group consisting of Al, Be, Co, Cr, Fe, Mg, Mn, Ni, and Zn.
    Type: Grant
    Filed: May 6, 2015
    Date of Patent: April 5, 2016
    Assignee: The Scripps Research Institute
    Inventors: K. Barry Sharpless, Valery Fokin, Vsevold A. Rostovtsev, Luke Green, Fahmi Himo
  • Patent number: 9073892
    Abstract: Compounds of Formula (I) are used for the treatment of inflammation and autoimmune disorders.
    Type: Grant
    Filed: December 16, 2011
    Date of Patent: July 7, 2015
    Assignee: Merck Serono S.A.
    Inventors: Catherine Jorand-Lebrun, Stefano Crosignani, Jerome Dorbais, Tania Grippi-Vallotton, Adeline Pretre
  • Publication number: 20150147273
    Abstract: A method for determining whether compound 0118 is a candidate treatment for a patient includes processing, via a processor, image data of tissue of interest of a patient including a cancer to determine whether a radiolabeled analog of compound 0118 is present in the tissue of interest represented in the image data and generating a signal indicating that compound 0118 is a candidate treatment for the patient in response to the determining that the radiolabeled analog of compound 0118 is present in a predetermined amount in the tissue of interest represented in the image data, wherein the presence of the radiolabeled analog of compound 0118 in the tissue of interest indicates presence of a sub-type of cancer having a galectin-1 molecular target, which is a sub-type of treatable by compound 0118.
    Type: Application
    Filed: June 10, 2013
    Publication date: May 28, 2015
    Applicant: Koninklijke Philips N.V.
    Inventors: Tilman Lappchen, Holger Gruell, Marc Stefan Robillard, Johan Lub
  • Patent number: 9040716
    Abstract: A copper catalyzed click chemistry ligation process is employed to bind azides and terminal acetylenes to provide 1,4-disubstituted 1,2,3-triazole triazoles. The process comprises contacting an organic azide and a terminal alkyne with a source of reactive Cu(I) ion in human blood plasma to form by cycloaddition a 1,4-disubstituted 1,2,3-triazole. The source of reactive Cu(I) ion can be, for example, a Cu(I) salt, Cu(II) ion in the presence of a reducing agent, or copper metal.
    Type: Grant
    Filed: October 7, 2014
    Date of Patent: May 26, 2015
    Assignee: The Scripps Research Institute
    Inventors: K. Barry Sharpless, Valery Fokin, Vsevold A. Rostovtsev, Luke Green, Fahmi Himo
  • Patent number: 9039979
    Abstract: The present disclosure relates to an apparatus and process for forming medical devices from an injectable composition. The apparatus includes a supply assembly configured to maintain and selective dispense a first precursor and a second precursor, a mixing assembly configured to mix the first and second precursors, and at least one catalyzing element including a transition metal ion to aid in the polymerization of the first and second precursors. The process includes dispensing a volume of the first precursor and a volume of the second precursor into a mixing assembly and mixing the first and second precursors. The first and second precursors each possess a core and at least one functional group known to have click reactivity with each other. The mixed precursors are contacted with a transition metal catalyst to produce a flowable composition for use as a medical device.
    Type: Grant
    Filed: February 22, 2010
    Date of Patent: May 26, 2015
    Assignee: Sofradim Production
    Inventors: Sébastien Ladet, Philippe Gravagna
  • Patent number: 9035068
    Abstract: The present invention relates to the phosphohistidine analogs of the present invention which of the formula (I) and the hapten containing the residue of same. It also relates to the hapten conjugated to a carrier molecule and the isolated antibodies raised against the immunogens, said antibodies recognizing polypeptide containing a phosphorylated histidine or the phosphotriazole residue but it does not recognize an amino acid or polypeptide that is not phosphorylated or a polypeptide which is phosphorylated on amino acids other than histidine but not on histidine.
    Type: Grant
    Filed: September 23, 2011
    Date of Patent: May 19, 2015
    Assignee: THE ROCKEFELLER UNIVERSITY
    Inventors: Tom W. Muir, Jung-Min Kee
  • Publication number: 20150133512
    Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of inflammatory diseases and disorders such as, for example, pulmonary fibrosis.
    Type: Application
    Filed: June 17, 2013
    Publication date: May 14, 2015
    Inventors: Stephen Deems Grabriel, Matthew Michael Hamilton, Yimin Qian, Achyutharao Sidduri
  • Publication number: 20150133511
    Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of inflammatory diseases and disorders such as, for example, pulmonary fibrosis . . . .
    Type: Application
    Filed: June 17, 2013
    Publication date: May 14, 2015
    Inventors: Stephen Deems Gabriel, Matthew Michael Hamilton, Matthew C. Lucas, Yimin Qian, Achyutharao Sidduri
  • Publication number: 20150133658
    Abstract: In one aspect, the invention relates to compounds having the formula: where R1, R2a, R2b, R3-R6, a, b, Z, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
    Type: Application
    Filed: August 15, 2014
    Publication date: May 14, 2015
    Applicant: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventors: Melissa Fleury, Roland Gendron, Adam D. Hughes, Cameron Smith
  • Publication number: 20150126708
    Abstract: The present invention provides a method of radio fluorination of biological targeting molecules (BTMs) with the radioisotope 18F. Also provided are novel conjugates useful in the 18F-radio fluorination method, and the use of such conjugates and automated synthesizer apparatus including cassettes for carrying out the method.
    Type: Application
    Filed: December 20, 2012
    Publication date: May 7, 2015
    Applicants: IMPERIAL INNOVATIONS LIMITED, GE HEALTHCARE LIMITED
    Inventors: Sajinder Kaur Luthra, Robin Fortt, Ramala Osman Awais, Eric Ofori Aboagye, Graham Smith
  • Patent number: 9023864
    Abstract: Compound of formula I are antagonists of the PGD2 receptor, CRTH2, and as such are useful in the treatment and/or prevention of CRTH2-mediated diseases such as asthma.
    Type: Grant
    Filed: February 7, 2013
    Date of Patent: May 5, 2015
    Assignees: Merck Sharp & Dohme Corp., Merck Canada Inc.
    Inventors: Carl Berthelette, Michael Boyd, John Colucci, Karine Villeneuve, Joey L. Methot
  • Patent number: 9023318
    Abstract: Novel compounds and pharmaceutical compositions having MMP inhibitory activity are disclosed, which have been found to be particularly useful in the prevention, treatment and diagnostic imaging of diseases associated with an unpaired activity of MMP, amongst others MMP-2, MMP-8, MMP-9 and/or MMP-13 to name a few. The compounds of the present invention are useful for the prevention, the treatment and the in vivo diagnostic imaging of a range of disease states (inflammatory, malignant and degenerative diseases) where specific matrix metalloproteinases are known to be involved.
    Type: Grant
    Filed: March 25, 2013
    Date of Patent: May 5, 2015
    Assignee: Siemens Medical Solutions USA, Inc.
    Inventors: Gang Chen, Umesh B. Gangadharmath, Dhanalakshmi Kasi, Harmuth C. Kolb, Changhui Liu, Anjana Sinha, Anna Katrin Szardenings, Joseph C. Walsh, Eric Wang, Chul Yu, Wei Zhang, Klaus Kopka, Guenter Haufe, Michael Schaefers, Verena Hugenberg, Stefan Wagner, Sven Hermann, Hans-Joerg Breyholz, Andreas Faust
  • Publication number: 20150118179
    Abstract: Biocidally active cationic analogs of N-halamine having two biocidally active groups covalently bonded together in a single molecule and having general Formula (I). Compounds of Formula (I), and precursors thereof, can be in solution form immobilized onto a substrate via physical coating or covalent chemical bonding to functionalize surfaces or added into materials as additives so as to render them biocidal. The biocidal solutions and substrates comprising the compounds or precursors of the present invention can then be used to inactivate pathogenic microorganisms.
    Type: Application
    Filed: May 16, 2013
    Publication date: April 30, 2015
    Applicant: UNIVERSITY OF MANITOBA
    Inventor: Song Liu
  • Publication number: 20150111888
    Abstract: The present invention provides a small compound targeting at TACC3. The present invention further provides a drug, particularly, an anticancer agent, comprising the small compound targeting at TACC3. A compound represented by the general formula (I) or a pharmaceutically acceptable salt, solvate, or ester derivative thereof binds to TACC3 and inhibits cell growth. Thus, these compounds can be used as drugs, particularly, anticancer agents.
    Type: Application
    Filed: April 30, 2013
    Publication date: April 23, 2015
    Inventors: Ryoji Yao, Hiroyuki Osada, Yasumitsu Kondoh
  • Publication number: 20150111875
    Abstract: The present invention relates to aminotetraline and aminoindane derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such aminotetraline and aminoindane derivatives, and the use of such aminotetraline and aminoindane derivatives for therapeutic purposes. The aminotetraline and aminoindane derivatives are GlyT1 inhibitors.
    Type: Application
    Filed: October 17, 2014
    Publication date: April 23, 2015
    Inventors: Wilhelm Amberg, Frauke Pohlki, Udo Lange, Ying Wang, Jason Brewer, Anil Vasudevan, Yanbin Lao, Charles Hutchins, Hongyu Zhao, Huan-Qiu Li
  • Publication number: 20150105378
    Abstract: The present invention provides compounds of Formula (I) or Formula (III): as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.
    Type: Application
    Filed: December 18, 2014
    Publication date: April 16, 2015
    Inventors: Lynn Abell, Leonard Adam, Cullen L. Cavallaro, Heather Finlay, Todd J. Friends, Jon J. Hangeland, Ji Jiang, R. Michael Lawrence, John Lloyd, Zulan Pi, George O. Tora, Jennifer X. Qiao, Carol Hui Hu, Tammy C. Wang
  • Publication number: 20150104387
    Abstract: Prostate-specific membrane antigen (PSMA) targeting compounds are described. Uses of the compounds for imaging, therapy, cell sorting, and tumor mapping are also described.
    Type: Application
    Filed: April 2, 2014
    Publication date: April 16, 2015
    Applicant: THE JOHNS HOPKINS UNIVERSITY
    Inventors: MARTIN G. POMPER, RONNIE C. MEASE, YING CHEN, Sangeeta Ray
  • Patent number: 9006345
    Abstract: In one aspect, the present invention is directed to dendrimers comprised of macromolecules and trifunctional branches. In another aspect, the invention relates to methods for generating dendrimeric compositions comprising macromolecules and trifunctional branches. In certain embodiments, the radial density of the dendrimeric composition is controlled by selective incorporation of branches.
    Type: Grant
    Filed: March 26, 2012
    Date of Patent: April 14, 2015
    Assignee: The Trustees of Columbia University in the City of New York
    Inventors: Jeffrey Lancaster, Jeffrey T. Koberstein, Nicholas J. Turro
  • Publication number: 20150099696
    Abstract: The present invention relates to compounds of the general formula (I), their tautomeric forms, their stereoisomers, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, methods for their preparation, use of these compounds in medicine and the intermediates involved in their preparation. The present invention is directed to compounds suitable for the treatment of Disease conditions such as hyperlipidemia.
    Type: Application
    Filed: June 26, 2012
    Publication date: April 9, 2015
    Applicant: Cadila Healthcare Limited
    Inventors: Harikishore Pingali, Pankaj Makadia, Vrajesh Pandya, Sairam V.V.M. Kalapatapu
  • Publication number: 20150099781
    Abstract: Described herein are compounds, and pharmaceutically acceptable salts and prodrugs thereof, which are useful as inhibitors of IMPDH. In certain embodiments, a compound of the invention selectively inhibits a parasitic IMPDH versus a host IMPDH. Further, the invention provides pharmaceutical compositions comprising one or more compounds of the invention. The invention also relates to methods of treating various parasitic and bacterial infections in mammals. Moreover, the compounds may be used alone or in combination with other therapeutic or prophylactic agents, such as anti-virals, anti-inflammatory agents, antimicrobials and immunosuppressants.
    Type: Application
    Filed: December 16, 2014
    Publication date: April 9, 2015
    Inventors: Lizbeth K. Hedstrom, Gregory D. Cuny, Deviprasad R. Gollapalli, Sivapriya Kirubakaran, Sushil K. Maurya, Boris Striepen, Suresh K. Gorla, Corey R. Johnson, Mandapati Kavitha, Jihan Khan
  • Publication number: 20150099734
    Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, Y and W are as described herein, compositions including the compounds and methods of using the compounds.
    Type: Application
    Filed: December 12, 2014
    Publication date: April 9, 2015
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Daniel HUNZIKER, Patrizio MATTEI, Harald MAUSER, Marco PRUNOTTO, Christoph ULLMER
  • Publication number: 20150094294
    Abstract: The present disclosure provides compounds, specifically pyrimidin-4,6-dicarboxylic acid amide derivatives, or pharmaceutically acceptable salts thereof and pharmaceutical compositions containing said compounds. Also provided are methods for treating a mammal having malaria, or killing or inhibiting the growth of a Plasmodium species, comprising administering to said mammal or contacting said Plasmodium species with, an effective amount of a pyrimidin-4,6-dicarboxylic acid amide derivative.
    Type: Application
    Filed: February 28, 2013
    Publication date: April 2, 2015
    Inventors: Richard W. Scott, Robert W. Kavash, Wenxi Pan, Katie Freeman, Michael J. Costanzo, Doron Greenbaum, Yongjiang Xu, Trevor Young
  • Publication number: 20150094337
    Abstract: The present invention provides a heterocyclic group contained amino-methanol derivative, and salt, a preparation method and use thereof, and belongs to the medical field. The heterocyclic group contained amino-methanol derivative and the salt thereof of the present invention are used for preparing medicines for immune suppression and for the treatment of organ transplant rejection, or medicines for treating immune mediated inflammatory diseases, such as multiple sclerosis, systemic lupus erythematosus and rheumatoid arthritis.
    Type: Application
    Filed: December 8, 2014
    Publication date: April 2, 2015
    Inventors: Xingmin Zhang, Ensi Wang, Jing Guo, Shengxiu Niu, Zhuolin Dai, Nan Zheng, Liping Ji, Zhenfang Wang, Tie Liang
  • Patent number: 8993698
    Abstract: The present invention provides novel 4- and 5-substituted 1,2,3-triazole moieties, with at least one remote polymerizable moiety. The novel mixtures of 4- and 5-substituted regioisomers of 1,2,3-triazole moieties can be separated by chromatography to provide the purified 4- and 5-substituted 1,2,3-triazole moieties. The novel mixtures of 4- and 5-substituted regioisomers of 1,2,3-triazole moieties, and the purified 4- and 5-substituted 1,2,3-triazole moieties, with at least one remote polymerizable moiety, can be converted to a wide variety of useful polymers. The novel compounds of the invention can be employed in a wide variety of compositions. E, Q, Z, X, a, and R1-R4, in the structures below, are defined herein.
    Type: Grant
    Filed: July 7, 2010
    Date of Patent: March 31, 2015
    Assignee: ISP Investments Inc.
    Inventor: Osama M. Musa
  • Publication number: 20150087827
    Abstract: The present invention relates to a process for preparing 1-[6-(morpholin-4-yl)pyrimidin-4-yl]-4-(1H-1,2,3-triazol-1-yl)-1H-pyrazol-5-ol (I—enol form) or 2-[6-(morpholin-4-yl)pyrimidin-4-yl]-4-(1H-1,2,3-triazol-1-yl)-1,2-dihydro-3H-pyrazol-3-one (I—keto form) and sodium 1-[6-(morpholin-4-yl)pyrimidin-4-yl]-4-(1H-1,2,3-triazol-1-yl)-1H-pyrazol-5-olate (II) from 1,2,3-triazole (III), methyl bromoacetate (IV-Me-Br) or ethyl bromoacetate (IV-Et-Br), 4,6-dichloropyrimidine (VIII), morpholine (IX) and hydrazine (XII).
    Type: Application
    Filed: May 6, 2013
    Publication date: March 26, 2015
    Applicant: BAYER PHARMA AKTIENGESELLSCAFT
    Inventors: Hans-Christian Militzer, Johannes Eggert
  • Patent number: 8981111
    Abstract: The present invention relates to hydroximoyl-heterocycle derivatives, their process of preparation, intermediate compounds for their preparation, their use as fungicide active agents, particularly in the form of fungicide compositions, and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions.
    Type: Grant
    Filed: April 21, 2009
    Date of Patent: March 17, 2015
    Assignee: Bayer Cropscience AG
    Inventors: Christian Beier, Jürgen Benting, David Bernier, Isabelle Christian, Pierre-Yves Coqueron, Philippe Desbordes, Christophe Dubost, Pierre Genix, Marie-Claire Grosjean-Cournoyer, Daniela Portz, Rachel Rama, Philippe Rinolfi, Arnd Voerste, Ulrike Wachendorff-Neumann
  • Patent number: 8980886
    Abstract: The present invention relates to novel anthranilic acid derivatives of the general formula (I) in which R1, R2, R3, R4, R5, Qx, A, Qy and n have the meanings given in the description, to their use as insecticides and acaricides for controlling animal pests, also in combination with other agents for activity boosting, and to a plurality of processes for their preparation.
    Type: Grant
    Filed: June 14, 2011
    Date of Patent: March 17, 2015
    Assignee: Bayer Cropscience AG
    Inventors: Rüdiger Fischer, Christoph Grondal, Markus Heil, Heinz-Juergen Wroblowsky, Ernst Rudolf Gesing, Arnd Voerste, Ulrich Görgens
  • Publication number: 20150073026
    Abstract: Triazole derivatives useful as anti-tubercular compounds; process for preparation of the triazoles and a method for inhibiting growth of Mycobacterium bovis BCG and Mycobacterium tuberculosis H37Ra using the triazoles.
    Type: Application
    Filed: September 23, 2014
    Publication date: March 12, 2015
    Inventors: Dhiman SARKAR, Sunita Ranjan DESHPANDE, Shailaja Pramod MAYBHATE, Anjali Prabhakar LIKHITE, Sampa SARKAR, Arshad KHAN, Preeti Madhukar CHAUDHARY, Sayalee Ramchandra CHAVAN
  • Publication number: 20150065711
    Abstract: Disclosed are linear discrete PEG constructs, which can be created and produced in a precise and reproducible way. Key to being able to do these things, where x in the discrete PEGx can vary from about 2 to about 64, is that the processes used to make each linear portion is controlled to give essentially one oligomer/one compound. Having a variable length linear discrete PEG construct that is (a) primarily an linear discrete PEG construct with diagnostic or therapeutic groups attached along a chain of attachment cores, which is attached to a preferential locator; (b) is an m-discrete PEG as the terminal construct on the linear portion, and “hidden”; (c or linear discrete PEG with a terminus group that can be either negatively or positively charged, or neutral; and any of the discrete PEG portions can be designed to be cleaved after entering the cell.
    Type: Application
    Filed: August 15, 2014
    Publication date: March 5, 2015
    Applicant: EquIP, LLC
    Inventor: Paul D. Davis
  • Publication number: 20150065521
    Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is optionally substituted triazolyl, and R2, R3, R4, R5, R6, R7 and R8 are as defined herein. Also disclosed are methods of using the compounds for treating diseases associated with P2X3 and/or a P2X2/3 receptor antagonists and methods of making the compounds.
    Type: Application
    Filed: April 18, 2013
    Publication date: March 5, 2015
    Applicant: Roche Palo Alto LLC
    Inventor: Roche Palo Alto LLC
  • Patent number: 8962580
    Abstract: The invention features compounds of formula I or II: In one embodiment, the invention relates compounds and processes for conjugating ligand to oligonucleotide. The invention further relates to methods for treating various disorders and diseases such as viral infections, bacterial infections, parasitic infections, cancers, allergies, autoimmune diseases, immunodeficiencies and immunosuppression.
    Type: Grant
    Filed: September 23, 2009
    Date of Patent: February 24, 2015
    Assignee: Alnylam Pharmaceuticals, Inc.
    Inventors: Muthiah Manoharan, Kallanthottathil G. Rajeev, Takeshi Yamada, David Butler, Narayanannair K. Jayaprakash, Muthusamy Jayaraman, Shigeo Matsuda, Rajendra K. Pandey, Chang Geng Peng
  • Publication number: 20150045559
    Abstract: The present invention relates to novel compounds derived from oxoazetidine corresponding to general formula (I) to the compositions containing same, to the process for preparation thereof and to the use thereof in pharmaceutical or cosmetic compositions.
    Type: Application
    Filed: September 26, 2014
    Publication date: February 12, 2015
    Inventors: Claire BOUIX-PETER, Itaru SUZUKI, Nicolas RODEVILLE, Pascale MAUVAIS, Jean-Claude PASCAL
  • Publication number: 20150045393
    Abstract: The invention provides for novel cysteine protease inhibitors and compositions comprising novel cysteine protease derivatives. The invention further provides for methods for treatment of neurodegenerative diseases comprising administration novel cysteine protease inhibitors or compositions comprising novel cysteine protease inhibitors. In some embodiments, the cysteine protease inhibitors are calpain inhibitors.
    Type: Application
    Filed: February 1, 2013
    Publication date: February 12, 2015
    Inventors: Greg R. Thatcher, Isaac Thomas Schiefer, Ottavio Arancio, Mauro Fa
  • Publication number: 20150044233
    Abstract: Methods for determining the presence of cancer stem cells by detecting GD2 expression. Also provided are methods for reducing proliferation of cancer stem cells by contacting the cells with a GD2 targeting agent, such as an anti-GD2 antibody or a GD3 synthase inhibitor. GD3 synthase inhibitor compounds are also provided.
    Type: Application
    Filed: February 27, 2013
    Publication date: February 12, 2015
    Inventors: Venkata Battula, Michael Andreeff, Sendurai A. Mani, Tapasree Roy Sarkar
  • Patent number: 8952042
    Abstract: The present invention relates to compounds of formula (1): where R, A, Q and Z are defined herein, or an enantiomer, diastereomer, tautomer, solvate, prodrug or pharmaceutical acceptable salt thereof. These compounds bind to the NR1H4 receptor (FXR) and act as agonists of the NR1H4 receptor (FXR). The invention further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of said nuclear receptor by said compounds, and to a process for the synthesis of said compounds.
    Type: Grant
    Filed: August 19, 2010
    Date of Patent: February 10, 2015
    Assignee: Phenex Pharmaceuticals AG
    Inventors: Claus Kremoser, Ulrich Abel, Christoph Steeneck, Olaf Kinzel
  • Patent number: 8946391
    Abstract: The present invention provides for a practical, universal and efficient method to ligate two large macromolecules (e.g., proteins) using the alkyne-azide 1,3-dipolar cycloaddition reaction to produce a conjugated macromolecule, such as a multivalent scFv. The present invention also provides for conjugate macromolecules comprising a plurality of macromolecule components cross-linked through at least one linking group comprising at least one 1,2,3-triazole moiety, wherein at least 50 percent of the macromolecule components in the conjugate macromolecule has only one site available for cross-linking.
    Type: Grant
    Filed: March 26, 2007
    Date of Patent: February 3, 2015
    Assignee: The Regents of the University of California
    Inventors: Jacquelyn Gervay-Hague, Wenjun Du, Sally Denardo, Arutselvan Natarajan
  • Patent number: 8946426
    Abstract: The present invention is concerned with substituted bicyclic heterocyclic compounds of Formula (I) wherein Het1, Het2, A1, A2, A3 and A4 have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
    Type: Grant
    Filed: February 2, 2010
    Date of Patent: February 3, 2015
    Assignees: Janssen Pharmaceuticals, Inc., Cellzome Limited
    Inventors: Henricus Jacobus Maria Gijsen, Adriana Ingrid Velter, Gregor James MacDonald, François Paul Bischoff, Tongfei Wu, Sven Franciscus Anna Van Brandt, Michel Surkyn, Mirko Zaja, Serge Maria Aloysius Pieters, Didier Jean-Claude Berthelot, Michel Anna Jozef De Cleyn, Daniel Oehlrich
  • Publication number: 20150031738
    Abstract: The present invention provides compounds, or pharmaceutically acceptable salts thereof, for inhibiting the growth of a microbe; treating a mammal having a microbial infection, mucositis, an ophthalmic infection, an otic infection, a cancer, or a Mycobacterium infection; inhibiting the growth of a Mycobacterium species; modulating an immune response in a mammal; or antagonizing unfractionated heparin, low molecular weight heparin, or a heparin/low molecular weight heparin derivative.
    Type: Application
    Filed: December 10, 2012
    Publication date: January 29, 2015
    Applicant: University of Massachusetts
    Inventors: Yan Li, Hitest Thaker, Gregory N. Tew, Dahui Liu, Wenxi Pan
  • Publication number: 20150031895
    Abstract: A copper catalyzed click chemistry ligation process is employed to bind azides and terminal acetylenes to provide 1,4-disubstituted 1,2,3-triazole triazoles. The process comprises contacting an organic azide and a terminal alkyne with a source of reactive Cu(I) ion in human blood plasma to form by cycloaddition a 1,4-disubstituted 1,2,3-triazole. The source of reactive Cu(I) ion can be, for example, a Cu(I) salt, Cu(II) ion in the presence of a reducing agent, or copper metal.
    Type: Application
    Filed: October 7, 2014
    Publication date: January 29, 2015
    Applicant: THE SCRIPPS RESEARCH INSTITUTE
    Inventors: K. Barry SHARPLESS, Valery FOKIN, Vsevold A. ROSTOVTSEV, Luke GREEN, Fahmi HIMO
  • Publication number: 20150018395
    Abstract: The present invention relates to chimeric chemical compounds which are used to recruit antibodies to cancer cells, in particular, prostate cancer cells or metastasized prostate cancer cells. The compounds according to the present invention comprise an antibody binding terminus (ABT) moiety covalently bonded to a cell binding terminus (CBT) through a linker and optionally, a connector molecule.
    Type: Application
    Filed: September 8, 2014
    Publication date: January 15, 2015
    Inventors: David Spiegel, Ryan Murelli, Andrew Zhang
  • Publication number: 20150018337
    Abstract: Compounds are provided that act as potent antagonists of the CCR9 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists.
    Type: Application
    Filed: July 29, 2014
    Publication date: January 15, 2015
    Inventors: Trevor T. Charvat, Cheng Hu, Anita Melikian, Aaron Novack, Andrew M.K. Pennell, Edward J. Sullivan, William D. Thomas, Solomon Ungashe, Penglie Zhang, Jay Powers, Sreenivas Punna
  • Publication number: 20150011773
    Abstract: This invention relates to novel compounds suitable for labeling by 18F and to the corresponding 18F labeled compounds themselves, 19F-fluorinated analogues thereof and their use as reference standards, methods of preparing such compounds, compositions comprising such compounds, kits comprising such compounds or compositions and uses of such compounds, compositions or kits for diagnostic imaging by Positron Emission Tomography (PET).
    Type: Application
    Filed: April 30, 2012
    Publication date: January 8, 2015
    Applicant: PIRAMAL IMAGING SA
    Inventors: Mathias Berndt, Andre Muller, Heribert Schmitt-Willich, Timo Stellfeld, Georg Kettschau, Thomas Brumby, Keith Graham, Lutz Lehmann, Jorma Hassfeld, Martin Kruger
  • Publication number: 20150010474
    Abstract: The invention relates generally to compounds and methods for imaging and/or selective ablation of nitroreductase-expressing cells and/or biological agents. More particularly, although not exclusively, the invention provides compounds that are selectively metabolised by bacterial nitroreductases and are substantially insensitive to metabolism under oxic or hypoxic conditions by human nitroreductase enzymes.
    Type: Application
    Filed: December 21, 2012
    Publication date: January 8, 2015
    Inventors: Robert Forbes Anderson, Jeffery Bruce Smaill, Adam Vorn Patterson, Amir Ashoorzadeh, David Francis Ackerley, Janine Naomi Copp, Alexandra Marie Mowday, Elsie May Williams, Christopher Paul Guise, Cameron Koch, Alex Kachur, William R. Dolbier, JR.