Nitrogen In Aglycone Moiety Patents (Class 536/17.4)
  • Patent number: 9617543
    Abstract: A sugar chain-containing polymer that enables targeting to the lesion area of liver fibrosis and is useful for imaging, diagnosis and therapy of liver fibrosis; and a sugar chain-containing polymer complex comprising the polymer as a carrier for an anionic substance useful fix therapy and the like; are provided. The polymer is a sugar chain-containing polymer which is a cationic polymer comprising an amine, which polymer comprises N-acetylglucosamine bound thereto. The polymer preferably has a disulfide bond. The polymer preferably has a structure in which polyethyleneimine is linked via a disulfide bond.
    Type: Grant
    Filed: May 27, 2014
    Date of Patent: April 11, 2017
    Assignees: SOMAR CORP., KOREA RESEARCH INSTITUTE OF BIOSCIENCE AND BIOTECHNOLOGY
    Inventors: Bong Hyun Chung, Hirohiko Ise, Toshihiro Akaike, Sun-Jung Kim
  • Patent number: 9573970
    Abstract: The present invention provides a compound of Formula I or hydrate thereof, useful for the treatment of diabetes.
    Type: Grant
    Filed: October 30, 2014
    Date of Patent: February 21, 2017
    Assignee: Eli Lilly and Company
    Inventor: Susan Marie Reutzel-Edens
  • Patent number: 9296775
    Abstract: The present invention provides a compound of Formula II: wherein X represents the following: or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: February 18, 2014
    Date of Patent: March 29, 2016
    Assignee: ELI LILLY AND COMPANY
    Inventor: Fucheng Qu
  • Publication number: 20150148527
    Abstract: A sugar chain-containing polymer that enables targeting to the lesion area of liver fibrosis and is useful for imaging, diagnosis and therapy of liver fibrosis; and a sugar chain-containing polymer complex comprising the polymer as a carrier for an anionic substance useful fix therapy and the like; are provided. The polymer is a sugar chain-containing polymer which is a cationic polymer comprising an amine, which polymer comprises N-acetylglucosamine bound thereto. The polymer preferably has a disulfide bond. The polymer preferably has a structure in which polyethyleneimine is linked via a disulfide bond.
    Type: Application
    Filed: May 27, 2014
    Publication date: May 28, 2015
    Applicants: SOMAR Corp., KOREAN RESEARCH INSTITUTE OF BIOSCIENCE AND BIOTECHNOLOGY
    Inventors: Bong Hyun CHUNG, Hirohiko ISE, Toshihiro AKAIKE, Sun-Jung KIM
  • Publication number: 20150141631
    Abstract: The present invention provides pyrazole derivatives, uses thereof for medical purposes and so on. More particularly, the present invention relates to pharmaceuticals useful for the prevention or treatment of constipation, which comprise as an active ingredient 3-(3-{4-[3-(?-D-glucopyranosyloxy)-5-isopropyl-1H-pyrazol-4-ylmethyl]-3-methylphenoxy}propylamino)-2,2-dimethylpropionamide, or a pharmaceutically acceptable salt thereof. The pharmaceuticals of the present invention exert an effect of increasing the frequency of bowel movement or the like, and are useful for the prevention or treatment of constipation.
    Type: Application
    Filed: May 2, 2013
    Publication date: May 21, 2015
    Applicant: Kissei Pharmaceutical Co., Ltd.
    Inventors: Masayuki Isaji, Masaaki Takemura, Hidetoshi Isawa, Yukihiko Hotei, Itaru Miyashita
  • Patent number: 9023814
    Abstract: The present invention relates to a calixarene-based glycosylated compound (I) having the formula: (I) wherein D is independently selected in the group comprising a —CH2-group, an oxygen atom, a sulphur atom, a sulfinyl group or a sulfonyl group, E is independently selected in the group comprising a hydrogen, an alkyl having from 1 to 10 carbon atoms, an aryl having from 6 to 20 carbon atoms, a nitrogen dioxide group, an azide group, an amino group, a guanidinium group, a halogen atom, a —CH2 R group wherein R is a hydroxyl, a halogen, an amino group, a N(alkyl)2 group, a NH(alkyl) group, or E represents a —CO—R? wherein R? is a hydrogen atom, a hydroxyl group or an amino, B represents a A-C group wherein A is independently selected in the group comprising an oxygen atom, a sulfur atom, a NH group or a (CH2)i group, i being an integer from 1 to 10, C is independently selected in the group comprising a hydrogen, an alkyl, an alkenyl, an alkynyl, or C is a group of formula (II).
    Type: Grant
    Filed: December 10, 2010
    Date of Patent: May 5, 2015
    Assignees: Centre National de la Recherche Scientifique, Universite Claude Bernard—Lyon 1, Universite Lille 2—Droit et Sante
    Inventors: Anne Imberty, Sébastien Vidal, Susan Matthews, Karine Faure, Benoit Guery, Samy Cecioni
  • Publication number: 20150110808
    Abstract: Methods and compositions using E-selectin antagonists are provided for the treatment and prevention of diseases and disorders treatable by inhibiting binding of E-selectin to an E-selectin ligand. Described herein are E-selectin antagonists including, for example, glycomimetic compounds, antibodies, aptamers and peptides that are useful in methods for treatment of cancers, and treatment and prevention of metastasis, inhibiting infiltration of the cancer cells into bone marrow, reducing or inhibiting adhesion of the cancer cells to endothelial cells including cells in bone marrow, and inhibiting thrombus formation.
    Type: Application
    Filed: December 21, 2012
    Publication date: April 23, 2015
    Applicant: GLYCOMIMETICS, INC.
    Inventors: John L. Magnani, Arun K. Sarkar, Myung-Gi Baek, Frank E. Anderson, III, Yanhong Li
  • Patent number: 9006468
    Abstract: The invention disclosed in this document is related to the field of pesticides and their use in controlling pests. A compound having the following structure is disclosed.
    Type: Grant
    Filed: January 25, 2012
    Date of Patent: April 14, 2015
    Assignee: Dow AgroSciences, LLC.
    Inventors: Gary D. Crouse, Thomas C. Sparks, CaSandra L. McLeod, David A. Demeter, Kristy Bryan, Annette V. Brown, William H. Dent, III, Denise P. Cudworth, Jaime S. Nugent, Ricky Hunter, Jack G. Samaritoni
  • Patent number: 9000135
    Abstract: The present invention relates to a compound of general formula (I): in which: X is OH, NH2, NHOH or RNH, where R may be a linear or branched, saturated or unsaturated, C1-C10 alkyl radical, Y is H, or an electron-withdrawing group, in particular selected from NO2, CF3 or a halogen, R1 and R2 are H or a linear or branched, saturated or unsaturated, C1-C10 alkyl radical, F is a reactive functional group that can be activated by click chemistry.
    Type: Grant
    Filed: May 18, 2011
    Date of Patent: April 7, 2015
    Assignees: Centre Nationale de Recherche Scientifique, Universite de Poitiers
    Inventors: Sebastien Papot, Mickael Thomas
  • Publication number: 20150087609
    Abstract: The present invention is directed to new bifunctional compounds and methods for treating HIV infections. The bifunctional small molecules, generally referred to as CDM-Hs, function through orthogonal pathways, by inhibiting the gp120-CD4 interaction, and by introducing cytotoxic moieties to gp120-expressing cells, thereby causing cell death and preventing cell infection and spread of HIV. It is shown that CDM-Hs bind to gp120 and gp-120 expressing cells competitively with CD4, and these compounds cause cell death of HIV-infected cells, thereby decreasing viral infectivity. Compounds and methods are described herein.
    Type: Application
    Filed: March 15, 2013
    Publication date: March 26, 2015
    Inventors: David Spiegel, Christopher Parker
  • Publication number: 20150080326
    Abstract: The invention disclosed in this document is related to the field of pesticides and their use in controlling pests. A compound having the following structure is disclosed.
    Type: Application
    Filed: November 24, 2014
    Publication date: March 19, 2015
    Applicant: DOW AGROSCIENCES LLC
    Inventors: Gary D. Crouse, Thomas C. Sparks, CaSandra L. McLeod, David A. Demeter, Kristy Bryan, Annette Vitale Brown, William H. Dent, III, Denise Perreault Cudworth, Jaime S. Nugent, Ricky Hunter, Jack Geno Samaritoni
  • Patent number: 8975386
    Abstract: New crystalline forms of macrolide compounds, and pharmaceutical compositions thereof, are described herein. In addition, processes for preparing the crystalline forms are described herein.
    Type: Grant
    Filed: March 22, 2011
    Date of Patent: March 10, 2015
    Assignee: Cempra Pharmaceuticals, Inc.
    Inventor: David E. Pereira
  • Patent number: 8952141
    Abstract: Derivatives of PSAs are synthesised, in which a reducing and/or non-reducing end terminal sialic acid unit is transformed into a N-hydroxysuccinimide (NHS) group. The derivatives may be reacted with substrates, for instance substrates containing amine or hydrazine groups, to form non-cross-linked/crosslinked polysialylated compounds. The substrates may, for instance, be therapeutically useful drugs, peptides or proteins or drug delivery systems.
    Type: Grant
    Filed: January 24, 2014
    Date of Patent: February 10, 2015
    Assignee: Lipoxen Technologies Incorporated
    Inventors: Sanjay Jain, Ioannis Papaioannou, Smita Thobhani
  • Publication number: 20150037360
    Abstract: The present invention relates to a linker for forming conjugates of a protein or peptide with a therapeutically active agent and which comprise a thiomaleamic acid moiety that is susceptible to cleavage under the pH conditions prevalent in the lysosome.
    Type: Application
    Filed: February 5, 2013
    Publication date: February 5, 2015
    Inventor: Mark Edward Brennan Smith
  • Publication number: 20150037275
    Abstract: There is provided a complex comprising rifaximin and a complexing agent, wherein the complexing agent is a polyvinyl pyrrolidone (PVP) or a cyclodextrin. There is also provided a process for preparing the complex, a pharmaceutical composition including the complex and therapeutic uses of the complex.
    Type: Application
    Filed: October 22, 2014
    Publication date: February 5, 2015
    Inventors: Maruti Ganpati Ghagare, Sunilkumar Parasnath Saroj, Dharmaraj Ramachandra Rao, Rajendra Narayanrao Kankan
  • Publication number: 20150031130
    Abstract: Described herein are conjugated modified oligonucleotides that are complementary to a target RNA. The conjugate facilitates cellular uptake of the modified oligonucleotide, resulting improved potency.
    Type: Application
    Filed: April 30, 2014
    Publication date: January 29, 2015
    Applicant: Regulus Therapeutics Inc.
    Inventor: Balkrishen Bhat
  • Patent number: 8940859
    Abstract: 1,3-Dipole-functional compounds (e.g., azide functional compounds) can be reacted with certain alkynes in a cyclization reaction to form heterocyclic compounds. Useful alkynes (e.g., strained, cyclic alkynes) and methods of making such alkynes are also disclosed. The reaction of 1,3-dipole-functional compounds with alkynes can be used for a wide variety of applications including the immobilization of biomolecules on a substrate.
    Type: Grant
    Filed: March 13, 2012
    Date of Patent: January 27, 2015
    Assignee: University of Georgia Research Foundation, Inc.
    Inventors: Geert-Jan Boons, Jun Guo, Xinghai Ning, Margaretha Wolfert
  • Publication number: 20150005245
    Abstract: Sialic acid derivatives of the formula (I) in which the symbols have the definitions stated in the description are suitable as medicaments, more particularly for diseases whose course is influenced by Siglec ligands.
    Type: Application
    Filed: December 21, 2012
    Publication date: January 1, 2015
    Inventors: Reinhard Brossmer, Horst Prescher
  • Patent number: 8921328
    Abstract: Compounds, compositions and methods are provided for inhibiting in vitro and in vivo processes mediated by E-selectin binding. More specifically, particular glycomimetic compounds are described, wherein the compounds are E-selectin antagonists.
    Type: Grant
    Filed: September 12, 2011
    Date of Patent: December 30, 2014
    Assignee: GlycoMimetics, Inc.
    Inventors: Beat Ernst, Céline E. Weckerle, Jonas K. Egger
  • Publication number: 20140378674
    Abstract: Triaryl rhamnose carbamate insecticides are prepared from triaryl acyl azides and tetrahydropyran-2-ols in good yield without the use of a hydride base.
    Type: Application
    Filed: May 28, 2014
    Publication date: December 25, 2014
    Applicant: DOW AGROSCIENCES LLC
    Inventors: Lawrence C. Creemer, Carl DeAmicis, Gary D. Crouse, Peter Borromeo
  • Publication number: 20140364595
    Abstract: The invention provides conjugate-based antifungal or antibacterial prodrugs formed by coupling at least one anti-fungal agent or antibacterial agent with at least one linker and/or carrier. The prodrugs are of formula: (i) (AFA)m-X-(L)n; (ii) [(AFA)m?-X]p-L; (iii) AFA-[X-(L)n?]q; or (iv) (AFA)m?-X, wherein: AFA is an antifungal agent or an antibacterial agent; L is a carrier; X is a linker; m ranges from 1 to 10; n ranges from 2 to 10; m? is 1 to 10; p is 1 to 10; n? is 1 to 10; and q is 1 to 10, provided that q? and n are not both 1; and m? is 1 to 10. The invention also provides nanoparticles comprising the conjugate-based prodrugs. Additionally, the invention also provides non-conjugated antifungal and antibacterial agents in the form of nanoparticles.
    Type: Application
    Filed: June 22, 2012
    Publication date: December 11, 2014
    Applicant: VYOME BIOSCIENCES
    Inventors: Abhijit S. Bapat, Gauthami Mahesh, Rajesh S. Gokhale, Sayali S. Shah, Shiladitya Sengupta, Sudhanand Prasad, Sumana Ghosh, Suresh R. Chawrai, Nidhi Arora, D. Sreedhar Reddy, Malika Mishra, Kirti Bajaj
  • Publication number: 20140364586
    Abstract: Reagents and methods for functionalizing polypeptides with moieties (alkylene glycol) molecules and glycan groups are disclosed that are based on a functionalizing reagent which comprises a nitrogen containing heterocyclic aromatic ring having a vinyl substituent that is capable of reacting with one or more thiol groups that are naturally present, or have been introduced into, the polypeptide, for example by employing a thiol group of one or more cysteine residues. The functionalizing reagent is covalently linked to a poly(alkylene glycol) molecule, such as a polyethylene glycol (PEG) molecule, or a glycan group so that the reaction between the vinyl group and the thiol group in the polypeptide covalently links the polypeptide to the poly(alkylene glycol) molecule and/or the glycan group.
    Type: Application
    Filed: June 26, 2014
    Publication date: December 11, 2014
    Inventors: Andrew Graham WATTS, Terrence Kantner, Amanda Barbara MacKenzie
  • Publication number: 20140357557
    Abstract: Methods and compositions relating to CDP-JAK inhibitor conjugates are described herein.
    Type: Application
    Filed: May 30, 2014
    Publication date: December 4, 2014
    Applicant: CERULEAN PHARMA INC.
    Inventors: Roderic O. Cole, Derek Gregory van der Poll
  • Publication number: 20140356417
    Abstract: Drag derivatives are provided herein which are suitable for loading into liposomal nanoparticle carriers. In some preferred aspects, the derivatives comprise a poorly water-soluble drag derivatized with a weak-base moiety that facilitates active loading of the drag through a LN transmembrane pH or ion gradient into the aqueous interior of the LN. The weak-base moiety can optionally comprise a lipophilic domain that facilitates active loading of the drag to the inner monolayer of the liposomal membrane. Advantageously, LN formulations of the drag derivatives exhibit improved solubility, reduced toxicity, enhanced efficacy, and/or other benefits relative to the corresponding free drags.
    Type: Application
    Filed: June 12, 2014
    Publication date: December 4, 2014
    Inventors: Peter Cullis, Marcel Bally, Marco Ciufolini, Norbert Maurer, Igor Jigaltsev
  • Publication number: 20140343001
    Abstract: The present invention encompasses compounds having general formula (I) able to inhibit the lactate production (lactic acid) involved in the angiogenesis of tumoral tissues, in the glycolytic metabolic process of tumoral cells, of immune system cells in asthmatic diseases, in vascular cells in the pulmonary hypertension, in the treatment of chronic back pain or hyperoxaluria, and in the process by which the parasites protozoan causing malaria obtain most of the necessary energy.
    Type: Application
    Filed: December 19, 2012
    Publication date: November 20, 2014
    Applicant: Universita di Pisa
    Inventors: Filippo Minutolo, Marco Macchia, Carlotta Granchi, Valeria Di Bussolo, Gino Giannaccini, Antonio Lucacchini, Paul J. Hergenrother, Emilia C. Calvaresi
  • Publication number: 20140322247
    Abstract: Disclosed herein are immunoconjugates comprising an inhibitor of Eg5 linked to an antigen binding moiety such as an antibody, that are useful for treating cell proliferative disorders. Also disclosed are novel inhibitors of Eg5 that can be used either alone or as part of an immunoconjugate to treat cell proliferation disorders. The Eg5 inhibitors include compounds of this formula as described herein: The invention further provides pharmaceutical compositions comprising these compounds and immunoconjugates, and compositions comprising the immunoconjugates or compounds with a therapeutic co-agent, and methods to use these compounds, conjugates and compositions for treating cell proliferation disorders.
    Type: Application
    Filed: March 13, 2014
    Publication date: October 30, 2014
    Applicant: NOVARTIS AG
    Inventors: Paul A. Barsanti, Sylvie Chamoin, Lionel Doumampouom-Metoul, Stephanie Guerro-Lagasse, Robert Martin Grotzfeld, Alexei Karpov, Marc Lafrance, Cristina Montserrat Nieto-Oberhuber, Grazia Piizzi
  • Publication number: 20140323418
    Abstract: Provided are pyrimidine compounds for inhibiting of Syk kinase, intermediates used in making such compounds, methods for their preparation, pharmaceutical compositions thereof, methods for inhibition Syk kinase activity, and methods for treating conditions mediated at least in part by Syk kinase activity.
    Type: Application
    Filed: November 23, 2012
    Publication date: October 30, 2014
    Applicant: Portola Pharmaceuticals, Inc.
    Inventors: Zhaozhong J. Jia, Brian Kane, Qing Xu, Shawn M. Bauer, Yonghong Song, Anjali Pandey, Ryan Dick
  • Publication number: 20140315837
    Abstract: This invention relates generally to compositions comprising noribogaine and an excipient to facilitate transport across the blood brain barrier.
    Type: Application
    Filed: July 3, 2014
    Publication date: October 23, 2014
    Inventors: Deborah C. Mash, Richard D. Gless
  • Publication number: 20140309178
    Abstract: Inhibitors of sodium glucose cotransporter 1 (SGLT1), compositions comprising them, and methods of their use to treat diseases and disorders such as diabetes are disclosed. Particular compounds are of the formula: the various substituents of which are defined herein.
    Type: Application
    Filed: November 18, 2013
    Publication date: October 16, 2014
    Applicant: LEXICON PHARMACEUTICALS, INC.
    Inventors: Kenneth Gordon CARSON, Nicole Cathleen GOODWIN, Bryce Alden HARRISON, David Brent RAWLINS, Eric STROBEL, Brian ZAMBROWICZ
  • Publication number: 20140309409
    Abstract: An amine or hydrazide derivative of a sialic acid unit, e.g. in a polysaccharide, is reacted with a bifunctional reagent at least one of the functionalities of which is an ester of N-hydroxy succinimide, to form an amide or hydrazide product. The product has a useful functionality, which allows it to be conjugated, for instance to proteins, drugs, drug delivery systems or the like. The process is of particular utility for derivatising amine groups introduced in sialic acid terminal groups of polysialic acids.
    Type: Application
    Filed: April 12, 2014
    Publication date: October 16, 2014
    Applicants: LIPOXEN TECHNOLOGIES LIMITED, Lipooxen Technologies Limited
    Inventors: Sanjay Jain, Ioannis Papaioannou, Smita Thobhani
  • Publication number: 20140309182
    Abstract: The present invention relates to an insecticidal enriched extract (biopesticide) isolated from the stem of Nothapodites foetida (Wight) Sleumer (formerly Mappia foetida (Miers) useful for the insect free storage and transport of grains and seed. The insecticidal activity of the enriched extract (biopesticide) of the invention is ascribed to compound/s other than camptothecin. The invention further relates to the process for preparation thereof, containing Compounds of general formula 1 and formula 2 (General formula 1) wherein R1=CH3, CH2OAC and wherein R2=COOH, or (I) and R3=H. OH.
    Type: Application
    Filed: June 21, 2012
    Publication date: October 16, 2014
    Inventors: Swati Pramod Joshi, John Pereira, Phool Kumar Patanjali, Sunita Sharad Kunte, Kiran Babasaheb Sonawane, Suresh Gurappa Mummigatti, Sumithra Devi Sanna, Krishnaiah Eraiah Hullukere, Seema Chaudhary
  • Publication number: 20140303360
    Abstract: The present invention relates to compounds involved in nematode signaling.
    Type: Application
    Filed: August 8, 2012
    Publication date: October 9, 2014
    Applicants: California Institute of Technology, Boyce Thompson Institute for Plant Research
    Inventors: Frank C. Schroeder, Stephan H. Von Reuss, Andrea Choe, Paul W. Stemberg
  • Publication number: 20140296169
    Abstract: The present disclosure relates to substituted isothiazolo[5,4-b]pyridine-2-carboxamides of the formula I, in which R1, R2, R3, R10, R11 and X are as defined in the claims. The compounds of the formula I are inhibitors of transglutaminases, in particular transglutaminase 2 (TGM2), and are suitable for the treatment of various diseases, for example degenerative joint diseases such as osteoarthritis. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use as pharmaceuticals, and pharmaceutical compositions comprising them.
    Type: Application
    Filed: June 18, 2014
    Publication date: October 2, 2014
    Inventors: Hauke SZILLAT, Thomas LEEUW, Martin LORENZ
  • Publication number: 20140286970
    Abstract: A compound, or a pharmaceutically acceptable salt or solvate thereof, or conjugates thereof, selected from the group consisting of formula wherein: (a) R10 is H, and R11 is OH, ORA, where RA is saturated C1-4 alkyl; (b) R10 and R11 form a nitrogen-carbon double bond between the nitrogen and carbon atoms to which they are bound; or (c) R10 is H and R11 is S02M, where z is 2 or 3 and M is a monovalent pharmaceutically acceptable cation, or both M together are a divalent pharmaceutically acceptable cation.
    Type: Application
    Filed: October 12, 2012
    Publication date: September 25, 2014
    Inventors: Scott Jeffrey, Patrick Burke, Philip Wilson Howard
  • Publication number: 20140275505
    Abstract: Triaryl rhamnose carbamate insecticides are prepared from triaryl carbamates and the tetrahydropyran-2-ols in good yield without the use of a hydride base.
    Type: Application
    Filed: February 27, 2014
    Publication date: September 18, 2014
    Applicant: Dow AgroSciences LLC
    Inventors: James M. RENGA, Anne M. WILSON, Gary D. CROUSE
  • Publication number: 20140274907
    Abstract: A compound with the formula (I), wherein: R2 is of formula (II), where X is selected from the group comprising: OH, SH, CO2H, COH, N?C?O, NHNH2, CONHNH2, formula (A), formula (B), NHRN, wherein RN is selected from the group comprising H and C1-4 alkyl; RC1, RC2 and RC3 are independently selected from H and unsubstituted C1-2 alkyl; and either: R12 is selected from the group consisting of: (ia) C5-10 aryl group, optionally substituted by one or more substituents selected from the group comprising: halo, nitro, cyano, ether, C1-7 alkyl, C3-7 heterocyclyl and bis-oxy-C1-3 alkylene; (ib) C1-5 saturated aliphatic alkyl; (ic) C3-6 saturated cycloalkyl; (id) formula (C), wherein each of R21, R22 and R23 are independently selected from H, C1-3 saturated alkyl, C2-3 alkenyl, C2-3 alkynyl and cyclopropyl, where the total number of carbon atoms in the R12 group is no more than 5; (ie) formula (D), wherein one of R25a and R25b is H and the other is selected from: phenyl, which phenyl is optionally substituted by a group
    Type: Application
    Filed: October 12, 2012
    Publication date: September 18, 2014
    Applicant: SPIROGEN SARL
    Inventors: Philip Wilson Howard, Arnaud Tiberghien, Scott Jeffrey, Patrick Burke
  • Publication number: 20140275502
    Abstract: Aryl boronic esters and boronic acids containing the rhamnose carbamate moiety are coupled to a triazole with an appropriate leaving group, generating a 4-triazolylphenyl carbamate in good yield and without cleavage of the carbamate linkage.
    Type: Application
    Filed: February 27, 2014
    Publication date: September 18, 2014
    Applicant: Dow AgroSciences LLC
    Inventors: Natalie C. GIAMPIETRO, Lawrence C. CREEMER, Gary D. CROUSE
  • Publication number: 20140274930
    Abstract: The present invention relates to compounds useful for the treatment or prevention of bacteria infections. These compounds have formula I: The invention also provides processes for making the compounds described herein. Furthermore, the present invention provides a composition comprising the compounds described herein, and a pharmaceutically acceptable carrier, adjuvant, or vehicle. The present invention also provides methods of treating or preventing bacteria infection in a subject, comprising administering to the subject an effective amount of the compound or the composition described herein.
    Type: Application
    Filed: March 12, 2014
    Publication date: September 18, 2014
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventors: Evelyne Dietrich, Carl Poisson, Michel Gallant, Stephanie Lessard, Bingcan Liu, Sanjoy Kumar Das, Yeeman Ramtohul, Thumkunta Jagadeeswar Reddy, Julien Martel, Frederic Vallee, Jean-Francois Lévesque
  • Publication number: 20140271474
    Abstract: Radiolabeled tracers for binding to sodium/glucose cotransporters (SGLTs), and their synthesis, are provided. The tracers are high-affinity inhibitors of SGLTs, glycosides labeled with radioactive halogens. Also provided are in vivo and in vitro techniques for using the tracers as analytical tools to study the biodistribution and regulation of SGLTs in health and disease, and to evaluate therapeutic interventions. The ability to monitor radiolabel tracer disposition in real time enables the design of new SGLT inhibitors with lower metabolism and higher efficiency.
    Type: Application
    Filed: June 14, 2012
    Publication date: September 18, 2014
    Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
    Inventors: Ernest M. Wright, Jorge R. Barrio
  • Publication number: 20140256922
    Abstract: The present disclosure provides novel imidazoquinoline derived compounds, derivatives thereof, analogues thereof, and pharmaceutically acceptable salts thereof, and methods of making and using such compounds. The present disclosure also provides TLR7 agonists and TLR7/TLR8 dual agonists, probes, tissue-specific molecules, adjuvants, immunogenic compositions, therapeutic compositions, and self-adjuvanting vaccines including the imidazoquinoline derived compounds, derivatives thereof, analogues thereof, and pharmaceutically acceptable salts thereof. Derivatives of the imidazoquinoline derived compounds also include dendrimers and dimers of the imidazoquinoline derived compounds, and methods of making and using the dendrimeic and dimeric imidazoquinoline derived compounds. The present disclosure also provides dual TLR2/TLR7 hybrid agonists that include imidazoquinoline derived compounds of the present disclosure.
    Type: Application
    Filed: May 16, 2014
    Publication date: September 11, 2014
    Inventors: Sunil David, Nikunj M. Shukla
  • Publication number: 20140256659
    Abstract: The present application relates to the compounds of formula I (I) as well as their use for inhibiting at least one of AKT-1, FAK and PKC? and in the treatment and/or prevention of metastatic diseases.
    Type: Application
    Filed: October 26, 2012
    Publication date: September 11, 2014
    Inventors: Moulay A. Alaoui-Jamali, Krikor Bijian, Jiang Tao
  • Patent number: 8828952
    Abstract: The invention relates to novel compounds that have utility as inhibitors of heparan sulfate-binding proteins; compositions comprising the compounds, and use of the compounds and compositions thereof for the antiangiogenic, antimetastatic, anti-inflammatory, antimicrobial, anticoagulant and/or antithrombotic treatment of a mammalian subject.
    Type: Grant
    Filed: October 16, 2008
    Date of Patent: September 9, 2014
    Assignee: Progen Pharmaceuticals Limited
    Inventors: Vito Ferro, Tomislav Karoli, Ligong Liu, Paul Newton Handley, Kenneth David Johnstone, Norbert Wimmer, Edward Timothy Hammond
  • Publication number: 20140234912
    Abstract: A method for generating human milk oligosaccharides (HMOs) or precursors thereof, compounds obtainable by the method, and uses and compositions involving such compounds. The method comprising the steps of a) providing at least one donor selected from the group of compounds of any of formulae 5 to 10, b) providing at least one acceptor from a group of lactose, LNT, LNnT and derivatives thereof, c) providing at least one enzyme comprising a transglycosidase activity and/or a glycosynthase activity, d) preparing a mixture of the at least one donor, at least one acceptor and at least one enzyme provided in steps a), b) and c); and e) incubating the mixture prepared according to step d).
    Type: Application
    Filed: May 14, 2012
    Publication date: August 21, 2014
    Applicant: GLYCOM A/S
    Inventors: Gyula Dekany, Elise Champion, Andreas Schroven, Markus Hederos
  • Publication number: 20140235839
    Abstract: The present invention provides a novel sialo-sugar chain, a process for producing the sialo-sugar chain, and a device for producing the sialo-sugar chain. A sialo-sugar chain can be easily and efficiently mass-produced by reacting a sugar wherein a hydroxy groups is substituted with an alkynyl group (herein sometimes referred to as “alkynylated sugar”) with a specific sialic acid donor in the presence of a sialic acid-introducing enzyme.
    Type: Application
    Filed: September 11, 2012
    Publication date: August 21, 2014
    Inventor: Masanori Yamaguchi
  • Publication number: 20140234346
    Abstract: A compound with the formula I: wherein: R2 is of formula II: where A is a C5-7 aryl group, X is selected from the group comprising: NHNH2, CONHNH2, formula III, formula IV, and either: (i) Q1 is a single bond, and Q2 is selected from a single bond and —Z—(CH2)n—, where Z is selected from a single bond, O, S and NH and n is from 1 to 3; or (ii) Q1 is —CH?CH—, and Q2 is a single bond; R12 is a C5-10 aryl group, optionally substituted by one or more substituents selected from the group comprising: halo, nitro, cyano, ether, C1-7 alkyl, C3-7 heterocyclyl and bis-oxy-C1-3 alkylene; R6 and R9 are independently selected from H, R, OH, OR, SH, SR, NH2, NHR, NRR?, nitro, Me3Sn and halo; where R and R? are independently selected from optionally substituted C1-12 alkyl, C3-20 heterocyclyl and C5-20 aryl groups; R7 is selected from H, R, OH, OR, SH, SR, NH2, NHR, NHRR?, nitro, Me3Sn and halo; either: (a) R10 is H, and R11 is OH, ORA, where RA is C1-4 alkyl; (b) R10 and R11 form a nitrogen-carbon double bond between the n
    Type: Application
    Filed: October 12, 2012
    Publication date: August 21, 2014
    Applicant: Spirogen Sàrl
    Inventor: Philip Wilson Howard
  • Publication number: 20140234876
    Abstract: The present invention provides a hapten derivative and conjugate of a natural high intensity sweetener containing hydroxyl groups. The conjugate can be used to produce antibodies specific against the natural high intensity sweetener. The present invention further provides a kit and method for detecting and quantifying the natural high intensity sweetener in a sample.
    Type: Application
    Filed: June 22, 2012
    Publication date: August 21, 2014
    Applicant: PURECIRCLE SDN BHD
    Inventors: Jose Antonio Gabaldon Hernandez, Estrella Nunez Delicado, Rosa Puchades Pla, Angel Maquiera, Eva Maria Brun Sanchez, Avetik Markosyan
  • Patent number: 8809285
    Abstract: The present invention provides for monophosphorylated lipid A derivatives and carbohydrate derivatives that are useful as agents in the treatment of diseases and conditions, including cancers. Also provided are pharmaceutical compositions comprising one or more compounds of Formula I-IV. In addition, methods for the treatment of cancers are provided.
    Type: Grant
    Filed: July 30, 2010
    Date of Patent: August 19, 2014
    Assignee: Wayne State University
    Inventors: Zhongwu Guo, Qianli Wang, Shouchu Tang
  • Publication number: 20140228310
    Abstract: Disclosed are methods of modulating a stress activated protein kinase (SAPK) system with an active compound, wherein the active compound exhibits low potency for inhibition of at least one p38 MAPK; and wherein the contacting is conducted at a SAPK-modulating concentration that is at a low percentage inhibitory concentration for inhibition of the at least one p38 MAPK by the compound. Also disclosed are derivatives of pirfenidone. These derivatives can modulate a stress activated protein kinase (SAPK) system.
    Type: Application
    Filed: April 28, 2014
    Publication date: August 14, 2014
    Applicant: InterMune, Inc.
    Inventors: Lawrence M. Blatt, Scott D. Seiwert, Leonid D. Beigelman, Ramachandran Radhakrishnan, Karl Kossen, Vladimir Serebryany
  • Publication number: 20140228551
    Abstract: The invention provides D02S derivatives conjugated to monosaccharide ligands directly or through a linker and optionally chelated to a metal, wherein the D02S derivatives having the following structure: wherein R1?, R2? are each independently —OH or —O-alkyl; R1 is a hydrogen, a linker, or a ligand; R3 is a linker and/or a ligand; and n is an integer from 1 to 10; the linker is an amino acid, a peptide, an amino alcohol, a polyethylylene glycol, an alkyl, an alkenyl, an alkynyl, an azide, an aromatic compound, a carboxylic acid, or an ester, the alkyl, alkenyl, or alkynyl is optionally substituted with an alkyl, a halogen, a nitro group, a hydroxyl group, an amino group, or a carboxyl group; the ligand is a GLUT1 targeting moiety.
    Type: Application
    Filed: June 20, 2012
    Publication date: August 14, 2014
    Applicant: RadioMedix Inc.
    Inventors: Izabela Tworowska, Jennifer Sims-Mourtada, Ebrahim S. Delpassand
  • Patent number: 8802832
    Abstract: This invention relates generally to compositions comprising noribogaine and an excipient to facilitate transport across the blood brain barrier.
    Type: Grant
    Filed: August 4, 2011
    Date of Patent: August 12, 2014
    Assignee: DemeRx, Inc.
    Inventors: Deborah C. Mash, Richard D. Gless, Jr.