Three Or More Carboxamide Groups Patents (Class 564/153)
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Publication number: 20130131382Abstract: The present invention relates to a process for the preparation of 5-[(2-hydroxyacyl)amino]-2,4,6-triiodo-1,3-benzendicarboxamidic derivatives comprising the Smiles rearrangement of a suitable precursor, by contact of an aqueous solution of this latter with an anion exchanger solid phase.Type: ApplicationFiled: July 14, 2011Publication date: May 23, 2013Applicant: BRACCO IMAGING S.P.A.Inventors: Pier Lucio Anelli, Marino Brocchetta, Enrico Cappelletti, Ornella Gazzotti
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Patent number: 8445725Abstract: A process for the preparation of iosimenol comprising reacting 5,5?-[(1,3-dioxo-1,3-propanediyl)diimino]bis[N-(2,3-dihydroxypropyl)-2,4,6-triiodo-1,3-benzenedicarboxamide] (C-VI) with a 3-halo-1,2-propanediol in an aqueous solvent. A process for the preparation of C-VI comprising reacting 3,3?-[(1,3-dioxo-1,3-propanediyl)diimino]bis[5-(aminocarbonyl)-2,4,6-triiodobenzoyl chloride] (C-V) with 3-amino-1,2-propanediol in the presence of an inorganic base and a suitable non-aqueous polar solvent. A process for the preparation of C-V comprising reacting 3-amino-5-(aminocarbonyl)-2,4,6-triiodobenzoyl chloride (C-IV) with malonyl dichloride in a solvent comprising a suitable ester solvent, a suitable nitrile solvent or mixtures thereof.Type: GrantFiled: January 14, 2009Date of Patent: May 21, 2013Assignee: Mallinckrodt LLCInventors: Allan R. Bailey, Michelle M. Jones, Mills T. Kneller, Alexander N. Petrov, David H. White, Oliver Egan, Fiona Rooney
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Patent number: 8445724Abstract: A process for the manufacture of iodixanol by performing a purification process of the crude product in a solvent comprising 1-methoxy-2-propanol. The crude product may be obtained in aqueous solution from dimerization of 5-acetamido-N,N?-bis(2,3-dihydroxypropyl)-2,4,6-triiodo-isophthalamide (“Compound A”).Type: GrantFiled: August 8, 2005Date of Patent: May 21, 2013Assignee: GE Healthcare ASInventors: Jan Cervenka, Khalid Hussain
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Publication number: 20130096092Abstract: Disclosed are inhibitors of retroviral growth of formula (I), that are useful in treatment of retroviral infections such as HIV. Also disclosed are a composition comprising a pharmaceutically acceptable carrier and at least one compound or salt of the invention, a method for inactivating a virus, a method for dissociating a metal ion from a zinc finger-containing protein, and a method for inhibiting the transmission of a virus.Type: ApplicationFiled: June 10, 2011Publication date: April 18, 2013Applicants: Health and Human ServicesInventors: Daniel Appella, Ettore Appella, John K. Inman, Lisa M. Miller Jenkins, Ryo Hayashi, Deyun Wang
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Patent number: 8420857Abstract: A process for separating soluble silica species such as monomeric silicic acid (or monosilicic acid) and low molecular weight soluble polymeric silica from impure water soluble compounds by membrane nanofiltration is provided. A process for separating soluble silica species and colloidal silica from impure water soluble compounds by reverse phase liquid chromatography is also provided.Type: GrantFiled: August 21, 2008Date of Patent: April 16, 2013Assignee: Mallinckrodt LLCInventors: Allan R. Bailey, David H. White, Derick L. Kaspar, Robert E. Vandas, Michael J. Gentilcore, Hung V. Nguyen, Anna K. Fukunaga
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Patent number: 8420858Abstract: The present invention relates to a novel process for preparing iopromide which is used as a contrast agent for X-ray, wherein 5-methoxyacetylamino-2,4,6-triiodoisophthalic acid (2,3-diacetoxypropyl)amide chloride of formula (19) and 5-methoxyacetylamino-2,4,6-triiodoisophthalic acid [(2,3-dihydroxy-N-methylpropyl)-(2,3-diacetoxypropyl)]diamide of formula (20) are introduced as intermediates, by which a bismer by-product generated during the preparation process can be removed even without an additional removal procedure and thus iopromide with high purity can be prepared in high yield.Type: GrantFiled: April 17, 2009Date of Patent: April 16, 2013Assignee: LG Life Sciences Ltd.Inventors: Kook Sang Hwang, Soon Min Chung, Chang Ki Kim, Bok Tae Kim, Ju Young Lee, Byeong Cheol Kim, Goon Ho Joe
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Publication number: 20130085087Abstract: A downhole fluid comprises a base fluid, for example a hydrocarbon base fluid, and a pyromellitamide gelling agent. The pyromellitamide gelling agent may have the general formula of: with R1, R2, R3, R4, R5, R6, R7, and R8 each being a hydrogen or an organic group. A method comprises introducing the downhole fluid into a downhole formation. A method of making a downhole fluid, the method comprising: combining a base fluid and a pyromellitamide gelling agent. A composition for gelling a downhole fluid, the composition comprising a pyromellitamide gelling agent and a wetting agent.Type: ApplicationFiled: September 24, 2012Publication date: April 4, 2013Applicant: SYNOIL FLUIDS HOLDINGS INC.Inventor: SYNOIL FLUIDS HOLDINGS INC.
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Publication number: 20130072719Abstract: The present invention relates to a process for the preparation of iodinated phenols; in particular; it relates to a process including the direct iodination, with suitably activated iodine, of 3,5-disubstituted phenol compounds to the corresponding 3,5-disubstituted-2,4,6-triiodophenols, which are useful intermediates for the synthesis of x-ray contrast media, and to the preparation of the contrast media themselves.Type: ApplicationFiled: June 9, 2011Publication date: March 21, 2013Applicant: BRACCO IMAGING S.P.A.Inventors: Attilio Citterio, Elisa Battistini, Davide Belnome, Federica Buonsanti, Luciano Lattuada, Gabriella Leonardi, Fulvio Uggeri, Evelin Vignale, Massimo Visigalli
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Publication number: 20130065963Abstract: The invention provides novel classes of HDAC inhibitors. Methods of sensitizing a cancer cell to the cytotoxic effects of radiotherapy are also provided as well as methods for treating cancer and methods for treating neurological diseases. Additionally, the invention further provides pharmaceutical compositions comprising an HDAC inhibitor of the invention, and kits comprising a container containing an HDAC inhibitor of the invention.Type: ApplicationFiled: July 17, 2012Publication date: March 14, 2013Applicant: Georgetown UniversityInventors: Alan P. Kozikowski, Anatoly Dritschilo, Mira Jung, Pavel A. Petukhov, Bin Chen
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Patent number: 8389766Abstract: A compound of formula (I): wherein A1, A2, A3, A4, R1, R2, G1, G2, Q1 and Q2 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, molluscicidal and nematicidal compositions comprising them and to methods of using them to combat and control insect, acarine, mollusc and nematode pests.Type: GrantFiled: December 12, 2007Date of Patent: March 5, 2013Assignee: Syngenta Crop Protection LLCInventors: Pierre Jung, Christopher Richard Syles Godfrey, William Lutz, Peter Maienfisch, Andre Stoller, Werner Zambach
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Patent number: 8389765Abstract: A process for the manufacture of iodixanol by performing a purification process of the crude product in a solvent comprising ethanol. The crude product may be obtained in aqueous solution from dimerisation of 5-acetamido-N,N?-bis(2,3-dihydroxypropyl)-2,4,6-triiodo-isophthalamide (“Compound A”).Type: GrantFiled: November 29, 2006Date of Patent: March 5, 2013Assignee: GE Healthcare ASInventor: Bjorg Helga Mellesdal Strandmyr
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Publication number: 20130052130Abstract: Disclosed are general and “substantially pure” branched discrete polyethylene glycol constructs useful in attaching to a variety of biologically active groups, for example, preferential locators, as well as biologics like enzymes, for use in diagnostics, e.g. imaging, therapeutics, theranostics, and moieties specific for other applications. In its simplest intermediate state, a branched discrete polyethylene glycol construct is terminated at one end by a chemically reactive moiety, “A”, a group that is reactive with a biologic material that creates “A”, which is a biologically reactive group, connected through to a branched core (BC) which has attached at least two dPEG-containing chains, indicated by the solid line, , having terminal groups, which can be charged, non-reactive or reactable moieties and containing between about 2 and 64 dPEG residues.Type: ApplicationFiled: August 30, 2012Publication date: February 28, 2013Applicants: UNIVERSITY OF WASHINGTON, QUANTA BIODESIGN, LTD.Inventors: Paul D. Davis, D. Scott Wilbur
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Publication number: 20130048911Abstract: An aromatic amide compound having the following general formula (I) is provided: wherein, X1 and X2 are independently C(O)HN or NHC(O); G1, G2 and G3 are independently hydrogen, C(O)HN-phenyl, or NHC(O)-phenyl, wherein at least one of G1, G2 and G3 is C(O)HN-phenyl or NHC(O)-phenyl; Q1, Q2, and Q3 are independently hydrogen, C(O)HN-phenyl, or NHC(O)-phenyl, wherein at least one of Q1, Q2, and Q3 is C(O)HN-phenyl or NHC(O)-phenyl; R5 is halo, haloalkyl, alkyl, alkenyl, aryl, heteroaryl, cycloalkyl, or heterocyclyl; and m is from 0 to 4.Type: ApplicationFiled: August 27, 2012Publication date: February 28, 2013Applicant: TICONA LLCInventors: Kamlesh P. Nair, Steven D. Gray
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Publication number: 20130040059Abstract: Compounds having building blocks according to the general formulae as shown in FIG. 1., wherein [BB1] is building block 1; [BB2] is building block 2; R1 is H or CH3, Z is a bridging group and is an ester group (—C(?O)O—) or an amide group (—C(?O)—NH—), X is an element selected from nitrogen, phosphorus, oxygen and sulfur; i is an integer which is 2 in case of nitrogen and phosphorus and 1 in case of oxygen and sulfur; Rj denotes groups which may be the same or different and have a C1-C20 hydrocarbyl group; Rk is a C7-C50 hydrocarbyl group; Y? is a negatively charged ion; and wherein the molar fraction of [BB2] in a molecule of the compound is between 0.3 and 1 and the weight average molecular weight of the compound is between 1.000 and 100.000 g/mol, determined with GPC. Compositions comprising such compounds and the use of such compounds as surfactants in a method for coating objects and in a method for preparing a latex composition.Type: ApplicationFiled: November 19, 2010Publication date: February 14, 2013Applicant: AM COATINGS B.V.Inventor: Mahmoud Hossein
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Publication number: 20130029901Abstract: Bone targeted compounds and methods are provided. Compounds can include a Bone Targeting Portion (RT), having an affinity for bone; a Bone Active Portion (RA) for interacting with and affecting bone; and a Linking Portion (RL) connecting the Bone Targeting Portion and the Bone Active Portion.Type: ApplicationFiled: July 30, 2012Publication date: January 31, 2013Inventors: William M. PIERCE, JR., K. Grant TAYLOR, Leonard C. WAITE, Kevyn MERTEN
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Publication number: 20130029070Abstract: Providing a crosslinkable composition and a crosslinking agent is objected to, which are capable forming a crosslinked product that is superior in retort resistance, with suppressed bleeding out from the crosslinked product, and that has favorable interlayer adhesiveness when formed into a multilayered structure crosslinked product. The present invention provides a crosslinkable composition containing (A) a polymer having an SP value of no less than 9.5 (cal/cm3)1/2 and no greater than 16.5 (cal/cm3)1/2, and (B) a crosslinking agent having one or more polar groups that include an oxygen atom and a nitrogen atom not constituting an aromatic ring, and two or more polymerizable groups. The difference between the SP value of the polymer (A) and the SP value of the crosslinking agent (B) is preferably no greater than 2 (cal/cm3)1/2, and more preferably no greater than 1 (cal/cm3)1/2. A decomposition temperature of the crosslinking agent (B) is preferably no less than 240° C.Type: ApplicationFiled: March 10, 2011Publication date: January 31, 2013Applicant: KURARAY CO., LTD.Inventors: Kaoru Ikeda, Kazuhiro Kurosaki
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Publication number: 20130029930Abstract: The invention provides a method of increasing a deacetylated activity of SIRT6 by contacting SIRT6 with an agent that binds SIRT6 and reduces the Km of SIRT6 for a substrate, thereby increasing the deacetylase activity of SIRT6. The invention also provides compounds of the formulas (II) and (III).Type: ApplicationFiled: December 14, 2010Publication date: January 31, 2013Applicant: CORNELL UNIVERSITYInventors: Anthony Sauve, Ping Xu
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Publication number: 20130022647Abstract: Embodiments presented herein relate to various polymers. Some of the polymer embodiments are heparin binding polymers. Some embodiments of the heparin binding polymers can be employed to bind to heparin for methods such as separating, purifying, removing, and/or isolating heparin and heparin like molecules.Type: ApplicationFiled: September 27, 2011Publication date: January 24, 2013Applicant: University of British ColumbiaInventors: Jayachandran N. Kizhakkedathu, Rajesh A. Shenoi, Cedric J. Carter, Donald E. Brooks
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Publication number: 20130017249Abstract: Here described are compounds consisting of the structure (targeting molecule)m-linker-(targeting molecule)n, wherein the targeting molecule is a retinoid or a fat soluble vitamin having a specific receptor on the target cell; wherein m and n are independently 0, 1, 2 or 3; and wherein the linker comprises a polyethylene glycol (PEG) or PEG-like molecule, as well as compositions and pharmaceutical formulations including these compounds which are useful for the targeting and delivery of therapeutic agents; and methods of using these compositions and pharmaceutical formulations.Type: ApplicationFiled: June 8, 2012Publication date: January 17, 2013Inventors: Yoshiro Niitsu, Joseph E. Payne, John A. Gaudette, Zheng Hou, Victor Knopov, Richard P. Witte, Mohammad Ahmadian, Loren A. Perelman, Yasunobu Tanaka, Violetta Akopian
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Patent number: 8354556Abstract: The present invention provides methods for preparing a polymeric compound of Formula I: or pharmaceutically acceptable salt thereof. The present invention also provides useful intermediates for preparing the compound of Formula I or pharmaceutically acceptable salt thereof.Type: GrantFiled: October 21, 2010Date of Patent: January 15, 2013Assignee: PolyMedix, Inc.Inventors: Robert W. Kavash, Haizhong Tang, Carol Mulrooney, Dahui Liu
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Patent number: 8343450Abstract: Methods and compositions to extract radionuclides such as various actinides and lanthanides from organic and/or aqueous solutions by utilizing extractant functionalized carbon nanotubes are disclosed. More particularly, phosphorous-containing (such as phosphine oxides, phosphoric acids or phosphates) organic extractants and other predesigned extractants (such as crown ethers, calncrown derivatives, malonamide and diglycolamide derivatives, polyethylene glycol derivatives, cobalt dicarbollide derivatives, and N-donating heterocyclic ligands) can be covalently and/or non-covalently employed on the surfaces and/or ends (tips) of carbon nanotubes for the purpose of removal radionuclides such as various actinides and lanthanides from organic and/or aqueous solutions. Extractant functionalized carbon nanotubes can be used for extracting radioactive nuclides from nuclear waste or spent nuclear fuel, which are produced and/or reprocessed from the nuclear power generation or other nuclear application.Type: GrantFiled: October 8, 2008Date of Patent: January 1, 2013Assignee: Chemnano Materials, Ltd.Inventor: Pingshan Wang
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Publication number: 20120329724Abstract: The present invention relates to compounds of Formula (I) and their pharmaceutically acceptable salts, wherein the substituents are as described herein, and their use in medicine, in particular as opioid agonists.Type: ApplicationFiled: September 7, 2012Publication date: December 27, 2012Inventors: Christopher Gordon Barber, Dafydd Rhys Owen, Lisa Rosemary Thompson
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Publication number: 20120322878Abstract: Aspects of the present invention relate to compounds and methods useful in modulating angiogenesis and methods of treating or preventing diseases associated with angiogenesis by administering a polycationic compound. The present invention relates to methods of use and compositions for inhibiting angiogenesis-mediated disorders in mammals including animals and humans. Additionally, this invention relates to the combined use of polycations with other anti-angiogenesis agents for the treatment of different angiogenesis-mediated disorders. Additionally, those polycationic compounds can be used with various anti-inflammatory and cytotoxic agents as well as with radio-therapeutic agents in cancer patients to prevent and treat tumor growth and metastasis.Type: ApplicationFiled: June 21, 2012Publication date: December 20, 2012Applicant: POLYMEDIX, INC.Inventors: Shaker Mousa, Dahui Liu
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Publication number: 20120309801Abstract: A class of topomimetic calixarene-based peptide mimetics is described. Calixarene-based peptide mimetics have various biological activities such as, for example, bactericidal activity, antiangiogenic activity, and/or antitumor activity. Methods of use and methods of designing calixarene-based peptide mimetics are described.Type: ApplicationFiled: April 24, 2012Publication date: December 6, 2012Applicant: Regents of the University of MinnesotaInventors: Kevin H. Mayo, Thomas R. Hoye, Xuemei Chen
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Patent number: 8309507Abstract: The invention is directed to a fluid detergent composition comprising a di-amido gellant and a surfactant, and a method for structuring said composition.Type: GrantFiled: February 27, 2012Date of Patent: November 13, 2012Assignee: The Procter & Gamble CompanyInventors: Susana Fernandez Prieto, Johan Smets, Beatriu Escuder Gil, Juan Felipe Miravet Celades, Vincent Josep Nebot Carda
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Publication number: 20120283305Abstract: Compounds of the formula I wherein R1a is H; and R1b is C1-C6alkyl, Carbocyclyl or Het; or R1a and R1b together define a saturated cyclic amine with 3-6 ring atoms; R2a and R2b are independently H, halo, C1-C4alkyl, C1-C4haloalkyl or C1-C4alkoxy, or R2a and R2b together with the carbon atom to which they are attached form a C3-C6cycloalkyl; R3 is a branched C5-C10 alkyl chain, C2-C4haloalkyl or —CH2C3-C7 cycloalkyl; R4 is C1-C6alkyl, C1-C6haloalkyl, C1-C6alkylamino or C1-C6dialkylamino; for use in the prophylaxis or treatment of a disorder characterised by inappropriate expression or activation of cathepsin S.Type: ApplicationFiled: December 10, 2010Publication date: November 8, 2012Applicant: Medivir UK LTDInventors: Susana Ayesa, Peter Carlqvist, Karolina Ersmark, Urszula Grabowska, Ellen Hewitt, Daniel Jönsson, Pia Kahnberg, Björn Klasson, Peter Lind, Lourdes Odén, Kevin Parkes, Daniel Wiktelius
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Publication number: 20120283474Abstract: An improved synthesis method for preparation of iodixanol, and a purification process through macroporous adsorption resin chromatographic column and recrystallization are provided. The synthesis method relates to dimerization of 5-acetamido-N,N?-bis(2,3-dihydroxypropyl)-2,4,6-triiodo-isophthalamide (compound A) to prepare iodixanol, wherein excessive side reactions such as alkylation are effectively inhibited by controlling the pH of the reaction mixture with a boron-containing acidic substance or salts thereof such as boric acid. In this way, the conversion rate of compound A to iodixanol is 85-90%. The iodixanol crude product is purified by a macroporous adsorption resin chromatographic column, obtaining iodixanol product with recovery of 90-95% and purity of 96-98%. The iodixanol crude product is recrystallized in mixed solvent containing 2-methoxyethanol, obtaining iodixanol product with recovery of 90-95% and purity of greater than 99%.Type: ApplicationFiled: November 26, 2009Publication date: November 8, 2012Applicant: HOVIONE CHINA HOLDING LIMITEDInventors: Zhiqi Hu, Huoying Zhang
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Patent number: 8293943Abstract: Preventing skin aging by targeting multiple causes by a single bullet is of primal scientific and consumer interest.Type: GrantFiled: February 18, 2012Date of Patent: October 23, 2012Assignee: Island Kinetics, Inc.Inventors: Shyam K Gupta, Linda Walker
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Publication number: 20120253071Abstract: The present invention relates to a terminal sterilization process for biodegradable PEG-based insoluble hydrogels using irradiation. The presence of a protective solvent ensures that the hydrogel remains intact with functionally preserved three-dimensional and physicochemical properties.Type: ApplicationFiled: October 28, 2010Publication date: October 4, 2012Inventors: Harald Rau, Tobias Voigt, Ulrich Hersel
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Patent number: 8258343Abstract: Preventing skin aging by targeting multiple causes by a single bullet is of primal scientific and consumer interest.Type: GrantFiled: February 15, 2012Date of Patent: September 4, 2012Assignee: Island Kinetics, Inc.Inventors: Shyam K Gupta, Linda Walker
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Patent number: 8236748Abstract: The invention is to pH tunable amido-gellant that are suitable for use in consumer product compositions.Type: GrantFiled: March 11, 2011Date of Patent: August 7, 2012Assignee: The Procter & Gamble CompanyInventors: Susana Fernandez Prieto, Johan Smets, Beatriu Escuder Gil, Juan Felipe Miravet Celades, Vincent Josep Nebot Carda
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Patent number: 8231864Abstract: Provided are oligomeric amidoamines, an oligomeric amidoamine salt of the oligomeric amidoamine, and/or an oligomeric amidoquat of the oligomeric amidoamine. These materials can be used as fabric softeners in fabric softener compositions or as a hair treatment in hair treatment compositions.Type: GrantFiled: June 29, 2006Date of Patent: July 31, 2012Assignee: Colgate-Palmolive CompanyInventors: Jean-Paul Grandmaire, Leopold Laitem, Amjad Farooq
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Patent number: 8232428Abstract: Aspects of the present invention relate to compounds and methods useful in modulating angiogenesis and methods of treating or preventing diseases associated with angiogenesis by administering a polycationic compound. The present invention relates to methods of use and compositions for inhibiting angiogenesis-mediated disorders in mammals including animals and humans. Additionally, this invention relates to the combined use of polycations with other anti-angiogenesis agents for the treatment of different angiogenesis-mediated disorders. Additionally, those polycationic compounds can be used with various anti-inflammatory and cytotoxic agents as well as with radio-therapeutic agents in cancer patients to prevent and treat tumor growth and metastasis.Type: GrantFiled: March 10, 2010Date of Patent: July 31, 2012Assignee: PolyMedix,Inc.Inventors: Shaker Mousa, Dahui Liu
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Patent number: 8232277Abstract: The present invention relates to nordihydroguaiaretic acid derivative compounds, namely, butane bridge modified nordihydroguaiaretic acid (NDGA) compounds and butane bridge modified tetra-O-substituted NDGA compounds, pharmaceutical compositions containing them, methods of making them, and methods of using them and kits including them for the treatment of diseases and disorders, in particular, diseases resulting from or associated with a virus infection, such as HIV infection, HPV infection, or HSV infection, an inflammatory disease, such as various types of arthritis and inflammatory bowel diseases, metabolic diseases, such as diabetes and hypertension, or a proliferative disease, such as diverse types of cancers.Type: GrantFiled: October 2, 2007Date of Patent: July 31, 2012Assignee: Erimos Pharmaceuticals LLCInventors: Qingqi Chen, Jonathan Daniel Heller, Rocio Alejandra Lopez, Amanda Jean Morris
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Publication number: 20120190880Abstract: The invention provides methods and compositions for preparing amphetamine conjugates, such as lisdexamfetamine, homoarginine-D-amphetamine, and salts thereof. In one embodiment, the invention provides methods of preparing an amphetamine conjugate from a chloramphetamine intermediate.Type: ApplicationFiled: June 18, 2010Publication date: July 26, 2012Inventors: Paul Alan Jass, Todd Jeffrey Johnson, Jason Scott Douglas, Matthew Wendell Schiesher
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Publication number: 20120184772Abstract: The present disclosure is directed to a process for preparing an alkylated triiodo-substituted arylamide, such as iodixanol, the process comprising contacting a triiodo-substituted arylamide, such as 5-acetamido-N,N?-bis(2,3-dihydroxylpropyl)-2,4,6-triiodoisophthalamide, and an alkylating agent in the presence of a base and a mixed solvent system comprising a non-aqueous solvent and water, wherein the volume ratio of the non-aqueous solvent to water is greater than 1:1. The process advantageously enables the concentration of any impurities or undesirable byproduct from the reaction to be reduced, while increasing the yield of the desired reaction product.Type: ApplicationFiled: September 28, 2010Publication date: July 19, 2012Inventors: Allan R. Bailey, Michelle M. Jones, Tino J. Caviggiola, III, Mills T. Kneller, Alexander N. Petrov, Michael A. Brown, Benjamin J. Costello
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Publication number: 20120184773Abstract: The present disclosure generally relates to an improved process for alkylating a triiodo-substituted arylamide to form a compound suitable for use as an X-ray contrast agent. More particularly, the present disclosure is directed to such a process that limits the formation of fused bicyclic impurities, such as Impurity G, in the alkylation reaction mixture.Type: ApplicationFiled: September 28, 2010Publication date: July 19, 2012Applicant: MALLINCKRODT LLCInventors: Tino J. Caviggiola, III, Michelle M. Jones
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Publication number: 20120178666Abstract: Prodrugs of guanfacine with amino acids or short peptides, pharmaceutical compositions containing such prodrugs and a method for providing therapeutic benefit in the treatment of ADHD/ODD (attention deficient hyperactivity disorder and oppositional defiance disorder) with guanfacine prodrugs are provided herein. Additionally, methods for minimizing or avoiding the adverse gastrointestinal side effects associated with guanfacine administration, as well as improving the pharmacokinetics of guanfacine are provided herein.Type: ApplicationFiled: September 15, 2010Publication date: July 12, 2012Applicant: SHIRE LLCInventors: Richard Franklin, Robert G. Tyson, Bernard T. Golding, Rhys Whomsley
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Publication number: 20120172449Abstract: Novel polyamine transport inhibitors have been synthesized and demonstrated to block the uptake of native polyamines into human cancer cells. A combination therapy of the transport inhibitor and DFMO (a drug which blocks polyamine biosynthesis) provided synergistic activity against a metastatic human colon cancer cell line. The strategy uses polyamine depletion and polyamine metabolism to generate reactive oxygen species within cells as a novel way to treat cancers. This approach may be implemented for widespread use in the treatment of diseases which rely upon polyamine transport activity for proliferation.Type: ApplicationFiled: June 21, 2010Publication date: July 5, 2012Inventors: Otto Phanstiel, Jennifer J. Archer
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Patent number: 8212076Abstract: Preventing skin aging by targeting multiple causes by a single bullet is of primal scientific and consumer interest.Type: GrantFiled: April 12, 2011Date of Patent: July 3, 2012Assignee: Covalence, Inc.Inventors: Shyam K Gupta, Linda Walker
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Patent number: 8207107Abstract: The invention is to di-amido gellant that are suitable for use in consumer product compositions.Type: GrantFiled: March 11, 2011Date of Patent: June 26, 2012Assignee: The Procter & Gamble CompanyInventors: Susana Fernandez Prieto, Johan Smets, Beatriu Escuder Gil, Juan Felipe Miravet Celades, Vincent Josep Nebot Carda
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Publication number: 20120134933Abstract: The invention relates to a diagnostic or therapeutic composition comprising a monomeric X-ray contrast medium containing iodine, in particular iopromide, for use in an X-ray assisted diagnosis or therapy and for the use of high doses of an X-ray contrast medium given to a patient, in particular patients with restricted kidney function.Type: ApplicationFiled: May 6, 2010Publication date: May 31, 2012Applicant: BAYER PHARMA AKTIENGESELLSCHAFTInventors: Gregor Jost, Hubertus Pietsch, Martin Sieber, Matthias Bräutigam, Sven Golfier
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Publication number: 20120136073Abstract: There are provided for herein novel amine-containing transfection compounds and methods for making and using same. The compounds are generally obtained by reacting a primary amine with an unsaturated compound. Transfection complexes made using the amine-containing transfection compounds in combination with additional compounds to encapsulate biologically active agents such as nucleic acids are also provided for herein. Methods of using the transfection complexes for the in vivo or in vitro delivery of biologically active agents are also described. The transfection complexes of the present invention are highly potent, thereby allowing effective modulation of a biological activity at relatively low doses compared to analogous transfection compounds known in the art.Type: ApplicationFiled: November 15, 2011Publication date: May 31, 2012Applicant: LIFE TECHNOLOGIES CORPORATIONInventors: Zhiwei Yang, Parul Angrish, Xavier de Mollerat du Jeu, Kristin Wiederholt
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Publication number: 20120123145Abstract: Described are antioxidant macromolecules and methods of making and using same.Type: ApplicationFiled: October 4, 2011Publication date: May 17, 2012Applicant: Polnox CorporationInventors: Ashok L. Cholli, Rajesh Kumar
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Patent number: 8178527Abstract: Disclosed are nordihydroguaiaretic acid derivative compounds including various end groups bonded by a carbon atom or heteroatom though a side chain bonded to the respective hydroxy residue O groups by an ether bond or a carbamate bond, pharmaceutical compositions, methods of making them, and methods of using them and kits including them for the treatment of diseases and disorders, in particular, diseases resulting from or associated with a virus infection, such as HIV infection, HPV infection, or HSV infection, an inflammatory disease, such as various types of arthritis and inflammatory bowel diseases, a metabolic disease, such as diabetes, a vascular disease, such as hypertension and macular degeneration, or a proliferative disease, such as diverse types of cancers.Type: GrantFiled: October 2, 2007Date of Patent: May 15, 2012Assignee: Erimos Pharmaceuticals LLCInventors: Qingqi Chen, Rocio Alejandra Lopez, Jonathan Daniel Heller, Amanda Jean Morris
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Publication number: 20120115796Abstract: The present invention relates to a compound comprising a peptide moiety, a spacer moiety and a water-soluble polymer moiety such as a poly(ethylene glycol) moiety. The spacer moiety is between the peptide moiety and the water-soluble polymer moiety. The spacer moiety has the structure: —NH—(CH2)?—[O—(CH2)?]?—O?—(CH2)?—Y— wherein ?, ?, ?, ?, and ? are each integers whose values are independently selected.Type: ApplicationFiled: April 4, 2011Publication date: May 10, 2012Applicant: AFFYMAX, INC.Inventors: Christopher P. Holmes, David Tumelty, Qun Yin
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Patent number: 8168579Abstract: The invention is directed to a fluid detergent composition comprising a di-amido gellant and a surfactant, and a method for structuring said composition.Type: GrantFiled: March 11, 2011Date of Patent: May 1, 2012Assignee: The Procter and Gamble CompanyInventors: Susana Fernandez Prieto, Johan Smets, Beatriu Escuder Gil, Juan Felipe Miravet Celades, Vincent Josep Nebot Carda
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Patent number: 8163965Abstract: The invention describes a process for the purification of iodinated aryl compounds where the purification is performed by continuous crystallization of a crude product in a solvent with removal of at least a fraction of the solvent. The continuous crystallization process is performed in one or more crystallizers at the boiling point of the content of the crystallizer.Type: GrantFiled: July 28, 2006Date of Patent: April 24, 2012Assignee: GE Healthcare ASInventors: Jan Cervenka, Khalid Hussain, Arne W. Aabye
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Patent number: 8158825Abstract: The present invention relates to a novel class of modified malonate derivatives. The modified malonate compounds can be used to treat cancer. The modified malonate compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.Type: GrantFiled: June 21, 2006Date of Patent: April 17, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: Jonathan Grimm, Paul Harrington, Richard Heidebrecht, Jr., Thomas Miller, Karin Otte, Phieng Siliphaivanh, David Sloman, Matthew Stanton, Kevin Wilson, David Witter, Solomon Kattar, Paul Tempest
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Publication number: 20120083625Abstract: A process for the preparation of iodixanol by dimerisation of 5-acetamido-N,N?-bis (2,3-dihydroxypropyl)-2,4,6-triiodo-isophthalamide (“Compound A”) in which, after the dimerisation step, unreacted Compound A is precipitated from the reaction mixture and recovered for re-use. The process substantially increases the net yield of iodixanol and simplifies its purification.Type: ApplicationFiled: October 6, 2011Publication date: April 5, 2012Applicant: GE HEALTHCARE ASInventor: OLE MAGNE HOMESTAD