Patents Issued in April 1, 2014
  • Patent number: 8686104
    Abstract: A polymer of formula (I): where: n is an integer from 10 to 5,000; m is an integer from 10 to 5,000; Ar1 and Ar3 are the same or different and are residues derived from a tetra-hydroxy aromatic monomer, the tetra-hydroxy aromatic monomer being wherein R is the same or different and is H or a C1-C8 alkyl, C2-C8 alkenyl or C3-C8 cycloalkyl group; and, Ar2 and Ar4 are the same or different and are residues derived from a tetra-halogenated aromatic monomer, the tetra-halogenated aromatic monomer being wherein X is F, Cl or Br, and R1 and R2 are the same or different and are wherein y is an integer from 1 to 8; with the proviso that when Ar1 is the same as Ar3 and Ar2 is the same as Ar4, R1 and R2 are not both —CN is useful as a material for gas separation, vapor separation, adsorbents or catalysis.
    Type: Grant
    Filed: October 16, 2009
    Date of Patent: April 1, 2014
    Assignee: National Research Council of Canada
    Inventors: Naiying Du, Michael D. Guiver, Gilles P. Robertson
  • Patent number: 8686105
    Abstract: This invention relates to adhesive systems using imines and salts thereof, precursors to electron deficient olefins and coreactants therefor.
    Type: Grant
    Filed: October 24, 2007
    Date of Patent: April 1, 2014
    Assignee: Henkel IP & Holding GmbH
    Inventors: Ciaran B. McArdle, Ligang Zhao
  • Patent number: 8686106
    Abstract: The present invention provides a carbon black-dispersed polyamic acid solution composition having a high solids content and a high carbon black content. The invention further provides an intermediate transfer belt using the polyamic acid solution composition. The carbon black-dispersed polyamic acid solution composition is obtained by uniformly dispersing carbon black in a polyamic acid solution obtained by reacting biphenyltetracarboxylic dianhydride and an aromatic diamine in an organic polar solvent. The biphenyltetracarboxylic dianhydride includes 2,3,3?,4?-biphenyltetracarboxylic dianhydride and 3,3?,4,4?-biphenyltetracarboxylic dianhydride. The aromatic diamine includes 4,4?-diaminodiphenyl ether and p-phenylenediamine. The polyamic acid solution has a solids content of 25 weight % or more.
    Type: Grant
    Filed: December 4, 2008
    Date of Patent: April 1, 2014
    Assignees: Gunze Limited, UBE Industries, Ltd.
    Inventors: Naoki Nishiura, Akira Ichino, Takashi Kuraoka, Toru Murakami, Takeshige Nakayama
  • Patent number: 8686107
    Abstract: A polycarbonate diol comprising repeating units represented by the following formula (A) and a terminal hydroxy group, 60-100 mol % of the repeating units represented by the formula (A) being repeating units represented by the following formula (B) or (C). The amount of the repeating units represented by the formula (B) is 60-100 mol % based on the total amount of the repeating units represented by the formula (A). The polycarbonate diol has a terminal primary OH ratio of 95% or higher. (A) (In the formula, R represents a C2-12 divalent aliphatic or alicyclic hydrocarbon.
    Type: Grant
    Filed: November 4, 2008
    Date of Patent: April 1, 2014
    Assignee: Asahi Kasei Chemicals Corporation
    Inventors: Tetsuo Masubuchi, Eizaburo Ueno
  • Patent number: 8686108
    Abstract: An aluminum chelate latent curing agent is configured such that an aluminum chelating agent and a specific arylsilane compound or a hydrolysate thereof are held in a polymer obtained by subjecting the aluminum chelating agent, the arylsilane compound, and a polyfunctional isocyanate compound to an emulsifying treatment, and then subjecting the polyfunctional isocyanate to interfacial polymerization. The aluminum chelating agent does not have an alkoxy group bonded to the aluminum. The arylsilane compound is a compound represented by the formula (A). (Ar)mSi(OR)n ??(A) In the formula (A), m is 2 or 3, and the sum of m and n is 4. Ar represents an optionally-substituted aryl group. R represents a hydrogen atom, a methyl group, or an ethyl group. When n is two, the two Rs may be the same or different.
    Type: Grant
    Filed: July 5, 2010
    Date of Patent: April 1, 2014
    Assignee: Sony Chemical & Information Device Corporation
    Inventor: Kazunobu Kamiya
  • Patent number: 8686109
    Abstract: The present invention relates to a method for treating a block copolymer solution, wherein the method comprises: providing a solution comprising a block copolymer in a non aqueous solvent; and, treating the solution to remove metals using an ion exchange resin. The invention also relates to a method of forming patterns using the treated block copolymer.
    Type: Grant
    Filed: March 9, 2012
    Date of Patent: April 1, 2014
    Assignee: AZ Electronic Materials (Luxembourg) S.A.R.L.
    Inventors: Jian Yin, Hengpeng Wu, Muthiah Thiyagarajan, SungEun Hong, Mark Neisser, Yi Cao
  • Patent number: 8686110
    Abstract: The present invention relates generally to therapeutic molecules which are useful for modulating apoptosis in a target cell or cell population. More particularly, the present invention provides therapeutic agents which inhibit pro-survival molecules and which are capable of inducing or facilitating apoptosis of a target cell or cell population such as cancer cells. The present invention further provides methods for generating or selecting the therapeutic molecules and pharmaceutical compositions comprising the therapeutic molecules.
    Type: Grant
    Filed: June 23, 2006
    Date of Patent: April 1, 2014
    Assignee: The Walter and Eliza Hall Institute of Medical Research
    Inventors: Peter Malcolm Colman, David Ching Siang Huang, Erinna Faith Lee, Walter Douglas Fairlie
  • Patent number: 8686111
    Abstract: The invention relates to polypeptides comprising an N-terminal portion and a C-terminal portion, wherein said N-terminal portion comprises the signature sequence QGP[P or L] and the amino acid sequence of said C-terminal portion is at least 70% identical to SEQ ID NO: 1, and uses thereof.
    Type: Grant
    Filed: July 25, 2007
    Date of Patent: April 1, 2014
    Assignee: Mintaka Foundation for Medical Research
    Inventor: Oliver Hartley
  • Patent number: 8686112
    Abstract: A molecular probe for use in detection of cancer cells expressing an Ig superfamily cell adhesion molecule that binds in a homophilic fashion in a subject includes a targeting agent that specifically binds to and/or complexes with a proteolytically cleaved extracellular fragment of the Ig superfamily cell adhesion molecule.
    Type: Grant
    Filed: August 14, 2009
    Date of Patent: April 1, 2014
    Assignee: Case Western Reserve University
    Inventor: Susann Brady-Kalnay
  • Patent number: 8686113
    Abstract: The invention relates to a peptide or peptide derivative having the general formula: Sub1-X1-D2K3-P4-P5-Y6-L7-P8-R9-P10-X2-P12-P13-R14-X3-I16-P17/Y17-N18-N19-X4-Sub2, wherein X1 is a non-polar, hydrophobic group or a positively charged group, D2 is asparagine or glutamine, K3, X2, and X4 are positively charged groups, X3 is a positively charged group, proline, or a proline derivative; L7 and I16 are non-polar, hydrophobic groups, Y6 and Y17 are tyrosine, R9 and R14 are arginine, N18 and N19 are asparagine or glutamine, P4, P5, P8, P10, P12, P13, and P17 are proline, hydroxyproline, or derivatives thereof, wherein possibly one or two of the groups selected from D2, P4, P5, P8, P10, P12, P13, P17, and Y17 are replaced by an arbitrary group and/or P13 and R14 are exchanged, Sub1 is the free or modified N-terminus, and Sub2 is the free or modified C-terminus.
    Type: Grant
    Filed: January 29, 2010
    Date of Patent: April 1, 2014
    Assignee: AMP-Therapeutics GmbH
    Inventors: Ralf Hoffmann, Daniel Knappe, Anna Klara Brigitte Hansen
  • Patent number: 8686114
    Abstract: Variant sucrose transporter polypeptides that enable bacterial growth over a wide range of gene expression levels and sucrose concentrations are described. Additionally, recombinant bacteria comprising these variant sucrose transporter polypeptides, and methods of utilizing the bacteria to produce products such as glycerol and glycerol-derived products are provided.
    Type: Grant
    Filed: March 5, 2012
    Date of Patent: April 1, 2014
    Assignee: E I du Pont de Nemours and Company
    Inventors: Dana Michelle Walters Pollak, Tina K Van Dyk
  • Patent number: 8686115
    Abstract: Provided herein are fluorescent lipid binding proteins (FLBPs). The FLBPs comprise a lipid binding domain linked to a fluorophore, whrereby the fluorophore's fluorescence emission undergoes a spectral change upon lipid binding. the fluorophore is selected from the group consisting of 2-dimethylamino-6-acyl-naphthalene (DAN) and RED fluorophore and the lipid binding protein is selected from the group consisting of ENTH domain of epsin 1, C2 domain of bovine lactadherin, C 1B domain of protein kinase C-gamma, C2 domain of cytosolic phospholipase A2-beta, and PH domain of Bruton's tyrosine kinase PH.
    Type: Grant
    Filed: November 5, 2010
    Date of Patent: April 1, 2014
    Assignee: The Board of Trustees of the University of Illinois
    Inventor: Wonhwa Cho
  • Patent number: 8686116
    Abstract: The present invention relates to a milk fraction obtainable by acidification of micellar casein and separation from precipitated casein named acid soluble protein from micellar casein. It was found that the milk fraction and especially certain sub-fractions thereof are bioactive and promote GLP-1 release in vitro. Based on these results, acid soluble protein from micellar casein may be useful in the treatment and the prevention of diabetes type II, obesity and may further be added to formulas directed at other purposes addressing the gastro-intestinal tract.
    Type: Grant
    Filed: October 23, 2009
    Date of Patent: April 1, 2014
    Assignee: Nestec S.A.
    Inventors: Sandrine Gremlich, Lionel Bovetto, Catherine Mace
  • Patent number: 8686117
    Abstract: A platelet aggregation inducing substance containing as an active ingredient a polypeptide having a peptide fragment represented by formula (1) (component A): -(Pro-X-Gly)n-??(1) wherein X represents Pro or Hyp; and n represents an integer of from 20 to 5,000.
    Type: Grant
    Filed: December 12, 2007
    Date of Patent: April 1, 2014
    Assignee: JNC Corporation
    Inventors: Yasuto Umeda, Shinichi Takasaki, Takafumi Takebayashi, Takahiro Kawai
  • Patent number: 8686119
    Abstract: The present invention relates to humanized monoclonal antibodies, pharmaceutical compositions that include the same, and use thereof for the treatment of a variety of indications, particularly cancer and immunodeficiency disorders. In particular, the present invention provides modified antibodies or fragments thereof having specific amino acid modifications compared to the humanized monoclonal immunomodulatory antibody termed hBAT-1.
    Type: Grant
    Filed: July 23, 2012
    Date of Patent: April 1, 2014
    Assignee: CureTech Ltd.
    Inventors: Rinat Rotem-Yehudar, Michael Schickler
  • Patent number: 8686120
    Abstract: This invention features methods and compositions useful for treating and diagnosing diseases of the nervous system, retina, skin, muscle, joint, and cartilage using a Dragon family protein. Protein and nucleic acid sequences of human, murine, zebrafish, and C. elegans Dragon family members are also disclosed.
    Type: Grant
    Filed: February 28, 2012
    Date of Patent: April 1, 2014
    Assignee: The General Hospital Corporation
    Inventors: Clifford J. Woolf, Tarek A. Samad
  • Patent number: 8686121
    Abstract: A method of diagnosing B-CLL in a subject in need thereof is provided. The method comprising determining in a biological sample of the subject a level of CD84 isoform C (SEQ ID NO: 30), wherein an increase in the level of the CD84 isoform C (SEQ ID NO: 30) beyond a predetermined threshold with respect to a level of the CD84 in a biological sample from a healthy individual is indicative of the B-CLL.
    Type: Grant
    Filed: September 23, 2009
    Date of Patent: April 1, 2014
    Assignee: Yeda Research and Development Co. Ltd.
    Inventors: Idit Shachar, Inbal Binsky, Mirko Sobotta
  • Patent number: 8686122
    Abstract: A method is disclosed for making a conjugate of two molecules using a hydrazide thiol linker. In a particular working embodiment, an Fc-specific antibody-enzyme conjugate is made using the method and demonstrated to provide exceptional staining sensitivity and specificity in immunohistochemical and in situ hybridization assays.
    Type: Grant
    Filed: January 14, 2010
    Date of Patent: April 1, 2014
    Assignee: Ventana Medical Systems, Inc.
    Inventors: Christopher Bieniarz, Julia Ashworth-Sharpe, Casey A. Kernag, Jerome W. Kosmeder, Mark Lefever
  • Patent number: 8686123
    Abstract: Improved manganese peroxidases, polynucleotides encoding improved manganese peroxidase and vectors and cells thereof are provided, as well as methods for converting a cellulose-containing biomass feedstock to ethanol using improved manganese peroxidases and cells expressing a heterologous manganese peroxidase as disclosed herein.
    Type: Grant
    Filed: November 15, 2011
    Date of Patent: April 1, 2014
    Assignee: Edeniq, Inc.
    Inventors: Chris DaCunha, Adrian Galvez, Michael Guerini, Manoj Patel, Ngim Ung-Ferrell, Jennifer Headman
  • Patent number: 8686124
    Abstract: Compositions and methods for conferring pesticidal activity, including against lepidopteran pests, to bacteria, plants, plant cells, tissues and seeds are provided. Compositions comprising a coding sequence for a toxin polypeptide are provided. The coding sequences can be used in DNA constructs or expression cassettes for transformation and expression in plants and bacteria. Compositions also comprise transformed bacteria, plants, plant cells, tissues, and seeds. In particular, isolated toxin nucleic acid molecules are provided. Additionally, amino acid sequences corresponding to the polynucleotides are encompassed, and antibodies specifically binding to those amino acid sequences. In particular, the present invention provides for isolated nucleic acid molecules comprising nucleotide sequences encoding the amino acid sequence shown in SEQ ID NO:27 and 28, or the nucleotide sequence set forth in SEQ ID NO:3, 8, 13, and 18, as well as variants and fragments thereof.
    Type: Grant
    Filed: February 18, 2011
    Date of Patent: April 1, 2014
    Assignee: Athenix Corp.
    Inventors: Kimberly Sampson, Daniel Tomso
  • Patent number: 8686125
    Abstract: The invention provides a method for producing a chimeric promoter polynucleotide capable of controlling transcription of an operably linked polynucleotide in a plant cell or plant, wherein the method comprises combining: a) at least one sequence motif comprising a sequence with at least 70% identity to SEQ ID NO:1, 11 or 12, and b) another polynucleotide sequence. The invention also provides chimeric promoters polynucleotides comprising the sequences defined in a) and b). The invention also provides constructs, vectors, host cells, plant cells and plants comprising the chimeric promoter polynucleotides of the invention. The invention also provided methods for modifying gene expression and phenotype of plant cells and plants by transforming the plant cells and plants with the chimeric promoter polynucleotides of the invention.
    Type: Grant
    Filed: May 12, 2009
    Date of Patent: April 1, 2014
    Assignee: The New Zealand Institute for Plant and Food Research Limited
    Inventors: Richard Espley, Roger P. Hellens, Andrew C. Allan, David Chagne, Cyril Brendolise
  • Patent number: 8686126
    Abstract: New polymorphisms in the nucleic acid sequences of the DNA polymerase/reverse transcriptase open reading frame and viral surface antigen open reading frame of the hepatitis B virus are reported. In particular, the present invention relates to the mutation YMDD?YSDD in the HBV reverse transcriptase domain and to the W196V mutation in the small HBV viral surface antigen. Said polymorphisms are affecting the detection of drug resistance mutations by genotypic methods and diagnostic kits based thereon. The present invention relates to methods and diagnostic kits for detection of a HBV virus comprising said nucleic acid polymorphisms. In particular, those methods utilizing oligonucleotides capable of hybridizing to said HBV nucleic acid polymorphisms are envisaged.
    Type: Grant
    Filed: July 19, 2012
    Date of Patent: April 1, 2014
    Assignee: Innogenetics N.V.
    Inventor: Abdurrahman Mithat Bozdayi
  • Patent number: 8686127
    Abstract: This invention relates to an agent, a composition and a product comprising at least one apoptosis-inducing substance, and at least one substance which inhibits expression and/or activity of an apoptosis-inhibiting substance; a method for inducing apoptosis or for treating a proliferative disease using one or more of them; a nucleic acid construct comprising a nucleic acid molecule encoding a protein to be expressed and a nucleic acid molecule which inhibits expression of an undesired protein; and a method for expressing a desired protein in a cell while inhibiting the expression of an undesired protein.
    Type: Grant
    Filed: April 13, 2009
    Date of Patent: April 1, 2014
    Assignee: LSIP, LLC
    Inventors: Masashi Idogawa, Yasushi Sasaki, Takashi Tokino
  • Patent number: 8686128
    Abstract: The present invention provides a method of preventing or reducing restenosis, neointima formation, graft failure, atherosclerosis, angiogenesis and/or solid tumor growth in a subject. The method comprises administering to the subject a prophylactically effective dose of a nucleic acid which decreases the level of c-Jun mRNA, c-Jun mRNA translation or nuclear accumulation or activity of c-Jun. It is preferred that the nucleic acid is a DNAzyme that targets c-Jun mRNA.
    Type: Grant
    Filed: July 12, 2012
    Date of Patent: April 1, 2014
    Inventor: Levon Michael Khachigian
  • Patent number: 8686129
    Abstract: The present invention provides a method for the isolation of biological molecules by the adsorption of the molecules onto a mineral substrate in the presence of an appropriate mixture of salts and sufolane. Preferably, the biological molecules are nucleic acids. Compositions and kits for performing the process according to the invention are also provided.
    Type: Grant
    Filed: March 20, 2007
    Date of Patent: April 1, 2014
    Assignee: Agilent Technologies, Inc.
    Inventors: Jeffrey C. Braman, Lee S. Basehore, Natalia Novoradovskaya
  • Patent number: 8686130
    Abstract: The present invention relates to novel unnatural fluorescent nucleic acid bases, that is, a purine base, a 1-deazapurine base, and a 1,7-deazapurine base each having a functional group which consists of two or more heterocyclic moieties linked together, at the 6-position thereof (the 6-position of purine ring). The present invention also relates to a compound containing the unnatural base, a derivative thereof, and a nucleic acid containing a nucleotide having the unnatural base. The present invention also relates to a method of preparing the nucleic acid. The unnatural base of the present invention has excellent fluorescence characteristics and also has excellent properties as a universal base.
    Type: Grant
    Filed: October 6, 2010
    Date of Patent: April 1, 2014
    Assignees: Riken, Tagcyx Biotechnologies
    Inventors: Ichiro Hirao, Michiko Hirao, Shigeyuki Yokoyama, Tsuneo Mitsui
  • Patent number: 8686131
    Abstract: Preparation and use of synthetic trisaccharides useful for the preparation of synthetic heparinoids.
    Type: Grant
    Filed: December 14, 2011
    Date of Patent: April 1, 2014
    Assignee: Alchemia Limited
    Inventors: Joachim Seifert, Latika Singh, Tracie E. Ramsdale, Michael L. West, Nicholas B. Drinnan
  • Patent number: 8686132
    Abstract: The present invention relates to a process for preparing a chemically modified polysaccharide, preferably starch, by using a microdevice. It further relates to the use of a microdevice for the chemical reactions of polysaccharides in heterogeneous mixtures. Examples of chemical modifications are acetylation, oxidation, hydroxypropylation and the like.
    Type: Grant
    Filed: August 19, 2010
    Date of Patent: April 1, 2014
    Assignee: Cargill, Incorporated
    Inventors: Marc Charles Florent Berckmans, Rita Maria Delrue, Bruno Frédéric Stengel
  • Patent number: 8686133
    Abstract: The invention provides an oxo-titanylphthalocyanine crystal which is stable, is superior in dispersibility in a photoreceptive layer and efficiently contributes to improvements in sensitivity and charge retention rate of an electrophotographic photoreceptor when it is used as a charge generating agent, a method for producing the oxo-titanylphthalocyanine crystal, and an electrophotographic photoreceptor.
    Type: Grant
    Filed: July 11, 2012
    Date of Patent: April 1, 2014
    Assignee: Kyocera Document Solutions Inc.
    Inventors: Daisuke Kuboshima, Jun Azuma, Yoshio Inagaki, Junichiro Otsubo, Keiji Maruo
  • Patent number: 8686134
    Abstract: The invention relates to an ionic liquid composition and a method for preparing the ionic liquid. The ionic liquid comprises a cation containing the Formula I, as herein disclosed, and wherein: n is 2, R1 is selected from the group consisting of: H, C1-C12 alkyl, aryl or together with R2 may form a heterocyclic ring, and R2 is selected from the group consisting of: H, C1-C12 alkyl, aryl or together with R1 may form a heterocyclic ring, and R3 is selected from the group consisting of hydrogen and C1-C12 alkyl, and wherein R1 and R2 are not simultaneously selected from hydrogen.
    Type: Grant
    Filed: July 20, 2011
    Date of Patent: April 1, 2014
    Assignee: Invista North America S.A R.L.
    Inventors: Stewart Forsyth, Kenneth Richard Seddon, Keith Whiston
  • Patent number: 8686135
    Abstract: Provided herein are methods to prepare Heteroaryl Compounds having the following structure: wherein R1-R4 are as defined herein. The Heteroaryl compounds are useful for treating or preventing cancer, inflammatory conditions, immunological conditions, neurodegenerative diseases, diabetes, obesity, neurological disorders, age-related diseases, or cardiovascular conditions.
    Type: Grant
    Filed: April 30, 2013
    Date of Patent: April 1, 2014
    Assignee: Signal Pharmaceuticals, LLC
    Inventors: Patrick Anthony Jokiel, Juan Antonio Gamboa, Philip Pye, William Wei-Hwa Leong, Anusuya Choudhury
  • Patent number: 8686136
    Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic protein family members, compositions containing the compounds and uses of the compounds for preparing medicaments for treating diseases during which occurs expression one or more than one of an anti-apoptotic protein family member.
    Type: Grant
    Filed: December 12, 2012
    Date of Patent: April 1, 2014
    Assignee: AbbVie Inc.
    Inventors: Milan Bruncko, Hong Ding, Aaron Kunzer, Christopher L. Lynch, William McClellan, Cheol-Min Park, Xiaohong Song, Xilu Wang, Michael Wendt
  • Patent number: 8686137
    Abstract: Compounds having the structure which are selective inhibitors of P13K (phosphatidylinositol 3-kinase-delta), for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions.
    Type: Grant
    Filed: June 30, 2011
    Date of Patent: April 1, 2014
    Assignee: Amgen Inc.
    Inventor: Paul John Dransfield
  • Patent number: 8686138
    Abstract: Disclosed are precursors having a pyrrolecarbaldiminates ligand and methods of synthesizing the same. The pyrrolecarbaldiminates ligand may be substituted.
    Type: Grant
    Filed: December 30, 2011
    Date of Patent: April 1, 2014
    Assignee: American Air Liquide, Inc.
    Inventors: Andrey V. Korolev, Clément Lansalot-Matras
  • Patent number: 8686139
    Abstract: The present invention relates to organic electronic devices that include an organic semiconducting material. The organic electronic devices may include organic light-emitting diodes, field-effect transistors, sensors, photodetectors, organic solar cells, organic thin-film transistors, organic integrated circuits, organic field-quench devices, organic light-emitting transistors, light-emitting electrochemical cells, or organic laser diodes.
    Type: Grant
    Filed: November 23, 2010
    Date of Patent: April 1, 2014
    Assignee: Novaled AG
    Inventors: Andrea Lux, Omrane Fadhel, Josef Salbeck, Manfred Kussler
  • Patent number: 8686140
    Abstract: A method of purifying a salt of pemetrexed having a structure of formula (III) by salting-out, wherein if M3+ is H+, then each of M1+ and M2+ is independently H+, Li+, Na+ or K+, provided that both of them are not H+; if M3+ is Li+, Na+ or K+, then each of M1+ and M2+ is independently Li+, Na+ or K+.
    Type: Grant
    Filed: October 21, 2008
    Date of Patent: April 1, 2014
    Assignee: Chongqing Pharmaceutical Research Institute Co., Ltd.
    Inventors: Jie Luo, Meng Lin, Bo Lin, Wenrun Ye, Yongmei Qin, Jie Deng
  • Patent number: 8686141
    Abstract: Processes for preparing certain N-arylalkyl-1-(alkyl or aralkyl)-2-acylaminoalkyl-5-hydroxy-6-oxo-1,6-dihydropyrimidine-4-carboxamides are disclosed. In one embodiment, the process comprises acylating the free amine in the corresponding N-arylalkyl-1-(alkyl or aralkyl)-2-aminoalkyl-5-ester protected hydroxy-6-oxo-1,6-dihydropyrimidine-4-carboxamide and then deprotecting the 5-hydroxy by base hydrolysis. The hydroxypyrimidinone carboxamide products of the process are HTV integrase inhibitors which are useful for treating HTV infection, treating AIDS, or delaying the onset or progression of AIDS. Certain esterified N-arylalkyl hydroxypyrimidinone carboxamides that can be employed as process intermediates are also disclosed.
    Type: Grant
    Filed: December 22, 2008
    Date of Patent: April 1, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Guy R. Humphrey, Ross A. Miller, Peter E. Maligres, Steven Weissman
  • Patent number: 8686142
    Abstract: 2-Aminopyrimidine compounds are described, which are useful as H4 receptor modulators. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, such as allergy, asthma, autoimmune diseases, and pruritis.
    Type: Grant
    Filed: February 12, 2013
    Date of Patent: April 1, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: Frank Chavez, James P. Edwards, Brad M. Savall, Jianmei Wei, Ronald L. Wolin
  • Patent number: 8686143
    Abstract: The present invention relates to compounds useful as inhibitors of protein kinases, particularly of JAK family kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
    Type: Grant
    Filed: October 25, 2011
    Date of Patent: April 1, 2014
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Marion W. Wannamaker, Francesco Salituro, Albert Pierce, Alex Aronov, Gabriel Martinez-Botella, Jian Wang, Luc Farmer, Mark Ledeboer, Tiansheng Wang, Randy Bethiel, Brian Ledford, Emilie Porter Huck
  • Patent number: 8686144
    Abstract: The invention relates to the use of specific compounds of formula (I) and their pharmaceutically-acceptable salts: (Formula 1) (I) as a new family of protein kinase CK2 inhibitors; the invention also relates to the use of compounds of formula (I) for the preparation of pharmaceutical compositions for the prevention and/or treatment of disorders and/or diseases chosen amongst cancers; autoimmune and inflammatory diseases; infectious diseases; diabetes angiogenesis related disorders; retinopathies and cardiac hypertrophy.
    Type: Grant
    Filed: July 28, 2010
    Date of Patent: April 1, 2014
    Assignees: Commissariat a l'Energie Atomique et aux Energie Alternative, Institut National de la Sante et de la Recherche Medicale (INSERM), Institut Curie, Centre National de la Recherche Scientifique
    Inventors: Claude Cochet, Renaud Prudent, Virginie Moucadel, Chi-Hung N'guyen
  • Patent number: 8686145
    Abstract: The present invention relates to a process for the preparation of a compound of the general Formula (I), comprising: a) reacting a compound of the general Formula (II) with a compound of the Formula III R2COOH and a compound of the general Formula IV R3NC under such conditions that compound I is formed, wherein R1 represents a substituted or unsubstituted alkyl, alkenyl, alkynyl, aromatic or non-aromatic, mono-, di- or tricyclic, or heterocyclic structure, and R2 represents a substituted or unsubstituted alkyl, alkenyl, alkynyl, aromatic or non-aromatic, mono-, di- or tricyclic, or heterocyclic structure, and R3 represents a substituted or unsubstituted alkyl, alkenyl, or alkynyl structure. In further aspect the subject invention relates to the use of the obtained products as intermediates for various peptidomimetics, and preferably as a building block in a convergent synthesis of prolyl dipeptide structures.
    Type: Grant
    Filed: September 16, 2010
    Date of Patent: April 1, 2014
    Assignee: Vereniging Voor Christelijk Hoger Onderwijs, Wetenschappelijk Onderzoek en Patientenzorg C/O Technology Transfer Officer VU & Vumc
    Inventors: Eelco Ruijter, Romano Orru, Anass Znabet, Marloes Polak, Nicholas Turner
  • Patent number: 8686146
    Abstract: The invention described herein pertains to substituted azaindenoisoquinoline compounds, in particular 7-, 8-, 9-, and 10-azaindenoisoquinoline compounds, which are inhibitors of topoisomerase I, processes and intermediates for their syntheses, pharmaceutical compositions of the compounds, and methods of using them in the treatment of cancer.
    Type: Grant
    Filed: July 13, 2012
    Date of Patent: April 1, 2014
    Assignee: Purdue Research Foundation
    Inventors: Mark S. Cushman, Evgeny A. Kiselev, Andrew E. Morrell
  • Patent number: 8686147
    Abstract: Compound of formula (I) in which R1, R2 and R3 are defined in the following description, and the pharmaceutically acceptable acid-addition or base-addition salts thereof. The invention also relates to a process and an intermediate for preparing it, and to a pharmaceutical composition comprising it. The invention also relates to the use of a novel 2H-pyrrolo[3,4-c]quinoline compound for preparing a pharmaceutical composition that is active in the treatment of disturbances of the serotoninergic system.
    Type: Grant
    Filed: July 17, 2009
    Date of Patent: April 1, 2014
    Assignee: Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F. S.p.A.
    Inventors: Maria Alessandra Alisi, Nicola Cazzolla, Roberta Costi, Roberto Di Santo, Guido Furlotti, Angelo Guglielmotti, Lorenzo Polenzani
  • Patent number: 8686148
    Abstract: The invention relates to a process for preparing new tiotropium salts, these new tiotropium salts as such, pharmaceutical formulations containing them and their use for preparing a medicament for the treatment of respiratory complaints, particularly for the treatment of COPD (chronic obstructive pulmonary disease) and asthma.
    Type: Grant
    Filed: October 29, 2004
    Date of Patent: April 1, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Rolf Banholzer, Waldemar Pfrengle, Peter Sieger
  • Patent number: 8686149
    Abstract: The present invention relates to compounds defined by formula I wherein the variables R1, R2, R3, R4, and m are defined as in claim 1, possessing valuable pharmacological activity. Particularly, the compounds are inhibitors of 11?-hydroxysteroid dehydrogenase (HSD) 1 and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases, in particular diabetes type 2, obesity, and dyslipidemia.
    Type: Grant
    Filed: November 4, 2011
    Date of Patent: April 1, 2014
    Assignee: Boehringer-Ingelheim International GmbH
    Inventors: Matthias Eckhardt, Hans-Juergen Martin, Martin Schuehle, Sandra Sick
  • Patent number: 8686150
    Abstract: The present invention relates to pyrazolo[3,4-b]pyridine compounds of the formula I, in which R1, R2, R3, R4, R5, R6 and R7 are defined as indicated below. The compounds of the formula I are kinase inhibitors, and are useful for the treatment of diseases associated with diabetes and diabetic complications, such as, diabetic nephropathy, diabetic neuropathy and diabetic retinopathy, for example. The invention furthermore relates to the use of compounds of the formula I, in particular as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.
    Type: Grant
    Filed: September 27, 2012
    Date of Patent: April 1, 2014
    Assignee: Sanofi
    Inventors: Stephanie Hachtel, Oliver Plettenburg, Christian Schoenau, Matthias Loehn, Stefania Pfeiffer-Marek, Maria Mendez-Perez, Aimo Kannt, Juergen Dedio, Markus Kohlmann, Alexander Schiffer, Guillaume Begis, Olivier Duclos, Frederic Jeannot
  • Patent number: 8686151
    Abstract: Disclosed are a novel montelukast 4-halobenzylamine salt, and a method for preparing a montelukast sodium salt by using the same. In the disclosed method, a montelukast 4-halobenzylamine salt represented by Formula 2 or a montelukast sodium salt represented by Formula 1 is prepared by obtaining a compound represented by Formula 3 from a compound represented by Formula 5, in the same reactor, without an additional obtaining process. In Formula 2, X represents F, Cl, Br or I.
    Type: Grant
    Filed: December 28, 2012
    Date of Patent: April 1, 2014
    Assignee: Dong Kook Pharm. Co., Ltd.
    Inventors: Hyuk Chul Kwon, Man Dong Rho, Kyung Hoi Cha
  • Patent number: 8686152
    Abstract: The present invention is directed to 4,4-di-substituted piperidine derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by DPP-1.
    Type: Grant
    Filed: March 9, 2011
    Date of Patent: April 1, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: Bart L. DeCorte, Renee L. DesJarlais, Yifang Huang, Michael H. Parker, Dennis J. Hlasta
  • Patent number: 8686153
    Abstract: The present invention relates to acid addition salts of lenalidomide, wherein said acid has a pKa lower than 1, preferably selected from hydrochloric acid, hydrobromic acid, methane sulfonic acid, ethane sulfonic acid, benzene sulfonic acid and p-toluenesulfonic acid, to processes for their making, and use in medicine, and to purification of lenalidomide base.
    Type: Grant
    Filed: August 12, 2009
    Date of Patent: April 1, 2014
    Assignee: Synthon B.V.
    Inventor: Jacobus Theodorus Henricus Van Eupen
  • Patent number: 8686154
    Abstract: Carrier compounds and compositions therewith which are useful in the delivery of active agents are provided. Methods of administration and preparation are provided as well.
    Type: Grant
    Filed: June 10, 2009
    Date of Patent: April 1, 2014
    Assignee: Emisphere Technologies, Inc.
    Inventors: Donald J. Sarubbi, Eugene N. Barantsevitch