Plural Ring Oxygens In The Hetero Ring Patents (Class 514/452)
  • Patent number: 10858371
    Abstract: Embodiments provide, among other compounds, a family of compounds that can be used as therapeutic anti-cancer agents, methods for using such compounds to treat cancer, and methods of making such compounds.
    Type: Grant
    Filed: September 22, 2017
    Date of Patent: December 8, 2020
    Assignee: Purdue Research Foundation
    Inventor: Arun K. Ghosh
  • Patent number: 10822323
    Abstract: This invention relates to an acid labile surfactant. In particular, the surfactants of the present invention include a dioxolane or dioxane functional group which enables the surfactant to hydrolyze in an acidic environment. Surfactants of this type can be utilized to enhance protein solubilization/enzyme digestion. Following hydrolysis to destroy the surfactant (which may chromatographic issues), there are generally two components formed—a hydrophilic one, and a hydrophobic one. By altering the chemistry of the hydrolysable linker, the polarity of the hydrophobic residue can be altered, allowing it to be solubilized by significantly less organic solvent, and to minimize the potential loss of peptide material and to expand the chromatographic conditions that can be utilized.
    Type: Grant
    Filed: February 26, 2019
    Date of Patent: November 3, 2020
    Assignee: Waters Technologies Corporation
    Inventor: Darryl W. Brousmiche
  • Patent number: 10777313
    Abstract: A method, system and computer-readable medium are provided for determining compliance with one or more patient care rules and protocols, the method including the steps of sending infusion information from a pump to a processor pertaining to one or more drugs provided to a patient, sending ventilation information from a ventilator to the processor pertaining to ventilation provided to the patient and determining, with the processor, a variation between actual care of the patient and a set of rules and protocols associated with care of the patient at least in part based on the infusion information and the ventilation information.
    Type: Grant
    Filed: June 13, 2013
    Date of Patent: September 15, 2020
    Assignee: CareFusion 303, Inc.
    Inventors: Tom Steinhauer, Terry Lee Blansfield, Leonard Mulkowsky, Andres Jesus Calderon, III
  • Patent number: 10766885
    Abstract: A compound having the formula (I): is disclosed. A method of preparing the compound of formula (I) is also disclosed.
    Type: Grant
    Filed: May 11, 2020
    Date of Patent: September 8, 2020
    Assignee: SHAANXI UNIVERSITY OF SCIENCE AND TECHNOLOGY
    Inventors: Xingke Ju, Chengyuan Liang, Bin Tian, Yuzhi Liu, Lei Tian, Gennian Mao, Limei Wang, Yuanyuan He, Yongbo Wang, Jingwen Xu, Dan Yang, Liang Qi, Wenbo Yao, Qianqian Zhao, Han Li
  • Patent number: 10688077
    Abstract: Disclosed are methods for treating a meylodysplastic syndrome (MDS) in a subject that involves administering to the subject a therapeutically effective amount of an inflammasome inhibitor. Also disclosed are methods for diagnosing a myelodysplastic syndrome (MDS) in a subject. In some embodiments, the method involves assaying a sample from the subject to detect inflammasome activation, wherein an increase in inflammasome activation in the sample compared to a control is an indication of MDS in the subject. In some embodiments, the method involves assaying a sample from the subject to detect s100A9 protein levels, wherein an increase in s100A9 protein levels in the sample compared to a control is an indication of MDS in the subject. The disclosed methods can further involve treating the subject for MDS if an increase in inflammasome activation and/or s100A9 levels are detected.
    Type: Grant
    Filed: February 26, 2016
    Date of Patent: June 23, 2020
    Assignee: H. Lee Moffitt Cancer Center and Research Institute, Inc.
    Inventors: Sheng Wei, Alan List
  • Patent number: 10639293
    Abstract: The present invention relates to a method for the treatment of cancer in a cancer patient.
    Type: Grant
    Filed: January 14, 2019
    Date of Patent: May 5, 2020
    Assignee: Tapestry Pharmaceuticals, Inc.
    Inventors: Jan Zygmunt, James Ferrara, James D. McChesney
  • Patent number: 10519125
    Abstract: The invention relates to compounds of the following general formula (I) in the form of one of the enantiomers thereof or a mixture of the enantiomers thereof, and the pharmaceutically acceptable salts and/or solvates thereof, especially for the use thereof as a medicament, more specifically in cancer treatment. The invention also relates to pharmaceutical compositions containing same and to the methods for the production thereof.
    Type: Grant
    Filed: December 1, 2017
    Date of Patent: December 31, 2019
    Assignee: PIERRE FABRE MEDICAMENT
    Inventors: Frédéric Marion, El Bachir Kaloun, Frédéric Lieby-Muller, Michel Perez, Jean-Philippe Annereau, Laurent Creancier
  • Patent number: 10471042
    Abstract: The present disclosure provides a composition of artesunate, a process of preparing the same, and a method of treatment.
    Type: Grant
    Filed: January 13, 2017
    Date of Patent: November 12, 2019
    Inventors: Ming Zhao, Li-Ming Zhou
  • Patent number: 10377703
    Abstract: A compound represented by formula (4): can be produced by adding a heterogeneous transition metal catalyst to a solution containing a compound represented by formula (3): obtained by performing a nitration reaction by adding a nitrating agent to a solution containing a compound represented by formula (2): obtained by oxidizing a compound represented by formula (1): with hydrogen peroxide in the presence of sodium tungstate and a saturated C8 carboxylic acid, then adding water to the resultant mixture, and separating the resultant solution.
    Type: Grant
    Filed: July 19, 2016
    Date of Patent: August 13, 2019
    Assignee: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: Yuta Honda, Yohei Tanaka, Kazuya Ueki
  • Patent number: 10307353
    Abstract: The present invention relates to novel compounds of formula (I) to compositions comprising same, and also to the use thereof for preventing and/or cosmetically treating the signs of aging of the skin.
    Type: Grant
    Filed: December 11, 2015
    Date of Patent: June 4, 2019
    Assignee: L'OREAL
    Inventors: Maria Dalko, Julien Hitce
  • Patent number: 10262007
    Abstract: Aspects of the present disclosure involve systems and methods for passing optimization information, which may be used to optimize input/output (“I/O”) requests, from a database management system to a file system, using various protocols of a network file system. The optimization information provided by the database management system may relate to various aspects of an I/O request that may be optimized.
    Type: Grant
    Filed: May 23, 2017
    Date of Patent: April 16, 2019
    Assignee: Oracle International Corporation
    Inventors: Brian Lee Wong, Chunli Zhang, Gerald Thornbrugh, Siddheshwar Mahesh
  • Patent number: 10251862
    Abstract: The present invention relates to a cosmetic composition containing a hydroxypyranone derivative compound as an active ingredient for promoting the differentiation of adipocytes. The composition according to the present invention has an effect of promoting the differentiation of adipocytes, and thus allows the differentiation of adipocyte in a skin layer, thereby increasing the skin volume or elasticity. Therefore, the composition of the present invention can be variously used as a cosmetic composition or a pharmaceutical composition in the field, such as skin damage.
    Type: Grant
    Filed: January 20, 2015
    Date of Patent: April 9, 2019
    Assignee: AMOREPACIFIC CORPORATION
    Inventors: Ho Sik Rho, Heung Soo Baek, Yu Jung Kim, Song Seok Shin, John Hwan Lee
  • Patent number: 10238621
    Abstract: Provided herein are compounds, compositions containing the compounds, and methods for the treatment of cancer in a cancer patient. In particular, the compounds are made by a process comprising treating a first compound represented by either Formula G? or Formula M?: with a second compound of generalized formula R8R9C(OCH3)2 and an acid selected from the group consisting of camphor sulfonic acid (CSA), p-toluene sulfonic acid (PTSA), hydrochloric acid (HCl) and acetic acid (AcOH), wherein R1 and R2 are each selected from H, an alkyl group, an olefinic group, an aromatic group, an O-alkyl group, an O-olefinic group, or an O-aromatic group; R7 is an alkyl group, an olefinic group, or an aromatic group; P1 is a hydroxyl protecting group; P5 is H or an acid labile protecting group at the 7-O position; R8 is H, alkyl group, olefinic or aromatic group; and R9 is: H, alkyl group, olefinic or aromatic or is as defined in the specification.
    Type: Grant
    Filed: October 9, 2017
    Date of Patent: March 26, 2019
    Assignee: TAPESTRY PHARMACEUTICALS, INC.
    Inventors: Jan Zygmunt, James Ferrara, James D. McChesney
  • Patent number: 10226062
    Abstract: This disclosure relates to taste modifiers of formula (I) wherein, n is 1, 2 or 3; R1 is selected from C1-C5 alkyl, C1-C5 hydroxyalkyl, C1-C5 dihydroxyalkyl and —CHYCOOH wherein Y is selected from C1-C3; R3 is hydrogen, hydroxy or C1-C3 alkoxy; R4 is hydrogen, or C1-C3 alkyl; R5 is selected from hydrogen, or C1-C3 alkyl; or R4 and R5 form together a bivalent radical —CH2—; that are able to impart, enhance or modify salt or umami taste.
    Type: Grant
    Filed: December 4, 2014
    Date of Patent: March 12, 2019
    Assignee: Givaudan SA
    Inventors: Jacob Antonius Elings, Stefan Michael Furrer, Abdelmajid Kaouas, Cornelis Winkel
  • Patent number: 10106521
    Abstract: Provided herein are eckol derivatives, methods of synthesis thereof and pharmaceutical compositions thereof. In other embodiments, provided herein are methods of treatment, prevention, or amelioration of a variety of medical disorders such as, for example, Alzheimer's disease, microbial infections, obesity, diabetes, cancer or inflammation using the compounds and pharmaceutical compositions disclosed herein.
    Type: Grant
    Filed: November 9, 2017
    Date of Patent: October 23, 2018
    Assignee: Phloronol, Inc.
    Inventors: Hyeon-Cheol Shin, Hyejeong Hwang, Kwang Yong Park, Seong Ho Kim, Haengwoo Lee
  • Patent number: 10039742
    Abstract: The present invention relates generally to the field of lipids and in particular aims at improving lipid absorption, for example under conditions of lipid maldigestion or malabsorption. One embodiment of the present invention relates to a composition comprising a sn-2 monoacylglycerol derivative, wherein the sn-1 and sn-3 positions are blocked by protective groups. The acyl group may be a fatty acid, for example one with anti-inflammatory properties.
    Type: Grant
    Filed: April 28, 2017
    Date of Patent: August 7, 2018
    Assignees: Nestec S.A., Beth Israel Deaconess Medical Center, Inc.
    Inventors: Bruce Bistrian, Frederic Destaillats, Cristina Cruz-Hernandez, Fabiola Dionisi, Isabelle Masserey-Elmelegy, Manuel Oliveira, Julie Celine Moulin
  • Patent number: 9951053
    Abstract: The present disclosure provides ?-diketones or analogs thereof, that activate Wnt/?-catenin signaling and thus treat or prevent diseases related to signal transduction, such as osteoporosis and osteoarthropathy; osteogenesis imperfecta, bone defects, bone fractures, periodontal disease, otosclerosis, wound healing, craniofacial defects, oncolytic bone disease, traumatic brain injuries or spine injuries, brain atrophy/neurological disorders related to the differentiation and development of the central nervous system, including Parkinson's disease, strokes, ischemic cerebral disease, epilepsy, Alzheimer's disease, depression, bipolar disorder, schizophrenia; otic disorders like cochlear hair cell loss; eye diseases such as age related macular degeneration, diabetic macular edema or retinitis pigmentosa and diseases related to differentiation and growth of stem cell, such as hair loss, hematopoiesis related diseases and tissue regeneration related diseases.
    Type: Grant
    Filed: November 21, 2016
    Date of Patent: April 24, 2018
    Assignee: Samumed, LLC
    Inventors: Sunil Kumar KC, David Mark Wallace, John Hood, Charlene F. Barroga
  • Patent number: 9884053
    Abstract: The present application discloses a compound which is which activates Wnt/?-catenin signaling and thus treats or prevents diseases related to signal transduction, such as osteoporosis and osteoarthropathy; osteogenesis imperfecta, bone defects, bone fractures, periodontal disease, otosclerosis, wound healing, craniofacial defects, oncolytic bone disease, traumatic brain injuries related to the differentiation and development of the central nervous system, comprising Parkinson's disease, strokes, ischemic cerebral disease, epilepsy, Alzheimer's disease, depression, bipolar disorder, schizophrenia; eye diseases such as age related macular degeneration, diabetic macular edema or retinitis pigmentosa and diseases related to differentiation and growth of stem cell, comprising hair loss, hematopoiesis related diseases and tissue regeneration related diseases.
    Type: Grant
    Filed: November 11, 2016
    Date of Patent: February 6, 2018
    Assignee: Samumed, LLC
    Inventors: Sunil Kumar KC, David Mark Wallace, John Hood, Charlene F. Barroga
  • Patent number: 9827223
    Abstract: The present invention provides methods and kits for the selective ablation of pain-sensing neurons. The methods comprise administration of a vanilloid receptor agonist to a ganglion in an amount that causes death of vanilloid receptor-bearing neurons. Accordingly, the present invention provides methods of controlling pain and inflammatory disorders that involve activation of vanilloid receptor-bearing neurons.
    Type: Grant
    Filed: October 24, 2014
    Date of Patent: November 28, 2017
    Assignee: THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES
    Inventors: Michael J. Iadarola, Zoltan Olah, Laszlo Karai
  • Patent number: 9820962
    Abstract: Provided herein are compounds, compositions containing the compounds, and methods for the treatment of cancer in a cancer patient. In particular, the compounds are made by a process comprising treating a first compound represented by either Formula G? or Formula M?: with a second compound of generalized formula R8R9C(OCH3)2 and an acid selected from the group consisting of camphor sulfonic acid (CSA), p-toluene sulfonic acid (PTSA), hydrochloric acid (HCl) and acetic acid (AcOH), wherein R1 and R2 are each selected from H, an alkyl group, an olefinic group, an aromatic group, an O-alkyl group, an O-olefinic group, or an O-aromatic group; R7 is an alkyl group, an olefinic group, or an aromatic group; P1 is a hydroxyl protecting group; P5 is H or an acid labile protecting group at the 7-O position; R8 is H, alkyl group, olefinic or aromatic group; and R9 is: H, alkyl group, olefinic or aromatic or is as defined in the specification.
    Type: Grant
    Filed: July 27, 2016
    Date of Patent: November 21, 2017
    Assignee: Tapestry Pharmaceuticals, Inc.
    Inventors: Jan Zygmunt, James Ferrara, James D. McChesney
  • Patent number: 9763915
    Abstract: The present invention provides a 1,2,4-trioxane or a pharmaceutically acceptable salt, ester, solvate, tautomer or stereoisomer thereof for use as an adjuvant for a tyrosine kinase inhibitor to enhance the activity of said tyrosine kinase inhibitor in a method for the treatment of a patient suffering from cancer, a pharmaceutical composition comprising a tyrosine kinase inhibitor as an active ingredient and said 1,2,4-trioxane adjuvant or a pharmaceutically acceptable salt, ester, solvate, tautomer or stereoisomer thereof in an amount sufficient to enhance the activity of the tyrosine kinase inhibitor, preferably for use in a method for the treatment of cancer.
    Type: Grant
    Filed: February 11, 2016
    Date of Patent: September 19, 2017
    Assignee: PharmOxaco SáRL
    Inventors: Charles William Jefford, Daniel Hoessli
  • Patent number: 9662314
    Abstract: Disclosed are methods of treating a muscle disease and improving normal muscle function by administering a therapeutically effective amount of an isoprenoid antibiotic. Also disclosed are methods of upregulating hnRNP L and hnRNP L targets by administering a therapeutically effective amount of an isoprenoid antibiotic. Methods of screening compounds for use in treating muscle disease and improving muscle function are also described.
    Type: Grant
    Filed: October 19, 2012
    Date of Patent: May 30, 2017
    Assignees: Tufts Medical Center, Inc., Children's Medical Center Corporation
    Inventors: Isabelle Draper, Louis M. Kunkel, Matthew S. Alexander, Alan S. Kopin
  • Patent number: 9605207
    Abstract: A liquid crystal compound is described, having a large dielectric anisotropy, a high voltage holding ratio and stability to heat, light and so forth, maintaining a nematic phase in a wide temperature range, and having a suitable optical anisotropy and an excellent compatibility with other liquid crystal compounds. Particularly, a liquid crystal compound having a large dielectric anisotropy is described. The compound is represented by formula (1): In the formula, for example, R1 is alkyl having 1 to 20 carbons; ring A1, ring A2, ring A3, ring A4, ring A5 and ring A6 are independently 1,4-cyclohexylene or 1,4-phenylene; Z1, Z2, Z3, Z4, Z5, Z6 and Z7 are independently a single bond, —(CH2)2—, —COO—, —OCO—, —CF2O—, —OCF2— or —CH?CH—; X1 is fluorine, —CF3 or —OCF3; and Y1 and Y2 are independently hydrogen or fluorine.
    Type: Grant
    Filed: March 7, 2012
    Date of Patent: March 28, 2017
    Assignees: JNC CORPORATION, JNC PETROCHEMICAL CORPORATION
    Inventor: Tokifumi Masukawa
  • Patent number: 9533976
    Abstract: The present disclosure provides ?-diketones or analogs thereof, that activate Wnt/?-catenin signaling and thus treat or prevent diseases related to signal transduction, such as osteoporosis and osteoarthropathy; osteogenesis imperfecta, bone defects, bone fractures, periodontal disease, otosclerosis, wound healing, craniofacial defects, oncolytic bone disease, traumatic brain injuries or spine injuries, brain atrophy/neurological disorders related to the differentiation and development of the central nervous system, including Parkinson's disease, strokes, ischemic cerebral disease, epilepsy, Alzheimer's disease, depression, bipolar disorder, schizophrenia; otic disorders like cochlear hair cell loss; eye diseases such as age related macular degeneration, diabetic macular edema or retinitis pigmentosa and diseases related to differentiation and growth of stem cell, such as hair loss, hematopoiesis related diseases and tissue regeneration related diseases.
    Type: Grant
    Filed: February 21, 2014
    Date of Patent: January 3, 2017
    Assignee: Samumed, LLC
    Inventors: Sunil Kumar KC, David Mark Wallace, John Hood, Charlene F. Barroga
  • Patent number: 9526753
    Abstract: The invention relates to a preparation containing several amino acids and plant extracts and its alcohol detoxification activity. The component (a) in the preparation contains a mixture of two or more amino acids or derivatives thereof; the component (b) in the preparation contains a mixture of three or more extracts from plants. There are several plant extracts used in this invention such as the extract of ginseng radix, the extract of ginkgo biloba leaf, the extract of Silibinin, the extract of barbury wolfberry fruit and tea polyphenols. The invention also relates to the biological activities of said preparation, such as the liver protection from chemical injury, the tolerance enhancement of hypoxy and the rapid decrease till elimination of the blood alcohol content.
    Type: Grant
    Filed: October 28, 2010
    Date of Patent: December 27, 2016
    Assignees: MODUTECH S.A., HANGZHOU ADAMERCK PHARMSLABS INC.
    Inventors: Youmao Qi, Qing Jie, Fengmin Zhang, Ying Gu, Meiping Yu
  • Patent number: 9493437
    Abstract: The present application discloses a compound which is which activates Wnt/?-catenin signaling and thus treats or prevents diseases related to signal transduction, such as osteoporosis and osteoarthropathy; osteogenesis imperfecta, bone defects, bone fractures, periodontal disease, otosclerosis, wound healing, craniofacial defects, oncolytic bone disease, traumatic brain injuries related to the differentiation and development of the central nervous system, comprising Parkinson's disease, strokes, ischemic cerebral disease, epilepsy, Alzheimer's disease, depression, bipolar disorder, schizophrenia; eye diseases such as age related macular degeneration, diabetic macular edema or retinitis pigmentosa and diseases related to differentiation and growth of stem cell, comprising hair loss, hematopoiesis related diseases and tissue regeneration related diseases.
    Type: Grant
    Filed: November 19, 2014
    Date of Patent: November 15, 2016
    Assignee: Samumed, LLC
    Inventors: Sunil Kumar KC, David Mark Wallace, John Hood, Charlene F. Barroga
  • Patent number: 9399031
    Abstract: A therapy for renal diseases characterized by alterations of the kidney function, such as Chronic Kidney Disease (CKD), acute and chronic renal impairment, and renal diseases that develop in diabetic patients or in patients who underwent an anticancer chemotherapic treatment with a platinum derivative. The invention is a combination of compounds selected from mono- or diamide of a C12-C20 monocarboxylic acid, saturated or monounsaturated, or a C4-C14 dicarboxylic acid, saturated or monounsaturated, with an aminoalkanol, and compounds selected from Silymarin, derivatives thereof or conjugates or complexes thereof, for use in the treatment of renal diseases.
    Type: Grant
    Filed: July 3, 2014
    Date of Patent: July 26, 2016
    Assignee: Epitech Group S.r.l.
    Inventors: Francesco Della Valle, Maria Federica Della Valle, Gabriele Marcolongo, Salvatore Cuzzocrea
  • Patent number: 9279083
    Abstract: A liquid crystal compound of formula (I): where A1, A2, A3, A4, R1, R2, Z1, Z2, Z3, n, and m are as defined in the specification.
    Type: Grant
    Filed: July 1, 2015
    Date of Patent: March 8, 2016
    Assignee: Daxin Materials Corp.
    Inventors: Ching-Tien Lee, Wan-Yu Huang, Chun-Chih Wang
  • Patent number: 9265836
    Abstract: An improved drug delivery composition and method of use is disclosed. The composition comprises one or more biodegradable block copolymer drug carriers; and a reconstitution enhancing and enabling agent comprising polyethylene glycol (PEG), a PEG derivative or a mixture of PEG and a PEG derivative. The composition can be administered as is or after being be dissolved or rapidly reconstituted in an aqueous vehicle to afford a homogeneous solution or uniform colloidal systems.
    Type: Grant
    Filed: December 23, 2013
    Date of Patent: February 23, 2016
    Assignee: Protherics Salt Lake City, Inc.
    Inventors: Chung Shih, Gaylen M. Zentner
  • Patent number: 9266813
    Abstract: The present invention provides a series of derivatives of stilbenoid which are useful as new inhibitory agents against head and neck squamous cell carcinoma (HNSCC) and hepatoma.
    Type: Grant
    Filed: March 28, 2014
    Date of Patent: February 23, 2016
    Assignee: China Medical University
    Inventors: Sheng-Chu Kuo, Jai-Sing Yang, Min-Tsang Hsieh, Tian-Shung Wu, Kuo-Hsiung Lee, Huei-Wen Chen, Li-Jiau Huang, Hsin-Yi Hung, Tzong-Der Way, Ling-Chu Chang, Hui-Yi Lin, Yung-Yi Cheng, Chin-Yu Liu
  • Patent number: 9248115
    Abstract: The invention relates to the use of a silibinin component for the production of a medicament that is adapted for parenteral administration for the treatment of viral hepatitis, preferably of hepatitis B or C, in particular for the reduction of the virus load. The medicament preferably contains no silidianin and/or no silichristin and/or no isosilibinin.
    Type: Grant
    Filed: April 26, 2013
    Date of Patent: February 2, 2016
    Assignee: MADAUS GMBH
    Inventors: Lucio Claudio Rovati, Massimo Maria D'Amato, Ulrich Mengs, Ralf-Torsten Pohl, Peter Ferenci
  • Publication number: 20150133442
    Abstract: The invention features compositions and methods for inhibiting the Pin1 protein, and the treatment of disorders characterized by elevated Pin1 levels.
    Type: Application
    Filed: June 7, 2013
    Publication date: May 14, 2015
    Inventors: Kun Ping Lu, Matthew Brian Boxer, Mindy Irene Emily Davis, Rajan Pragani, Min Shen, Anton Momtchilov Simeonov, Shuo Wei, Xiao Zhen Zhou
  • Publication number: 20150133536
    Abstract: Provided herein are compounds, compositions containing the compounds, and methods for the treatment of cancer in a cancer patient. In particular, the compounds are made by a process comprising treating a first compound represented by either Formula G? or Formula M?: with a second compound of generalized formula R8R9C(OCH3)2 and an acid selected from the group consisting of camphor sulfonic acid (CSA), p-toluene sulfonic acid (PTSA), hydrochloric acid (HCl) and acetic acid (AcOH), wherein R1 and R2 are each selected from H, an alkyl group, an olefinic group, an aromatic group, an O-alkyl group, an O-olefinic group, or an O-aromatic group; R7 is an alkyl group, an olefinic group, or an aromatic group; P1 is a hydroxyl protecting group; P5 is H or an acid labile protecting group at the 7-O position; R8 is H, alkyl group, olefinic or aromatic group; and R9 is: H, alkyl group, olefinic or aromatic or is as defined in the specification.
    Type: Application
    Filed: January 23, 2015
    Publication date: May 14, 2015
    Applicant: Tapestry Pharmaceuticals, Inc.
    Inventors: Jan ZYGMUNT, James FERRARA, James D. MCCHESNEY
  • Patent number: 9023388
    Abstract: A high-efficacy, long-acting formulation of silibinin, comprising silibinin solid dispersion, silibinin-loaded silica nanoparticles, slow-release matrix material and release enhancer, wherein the mass ratio of these components is silibinin solid dispersion:silibinin-loaded silica nanoparticles:slow-release matrix material:release enhancer=1:0.5˜1.25:0.1˜0.3:0.1˜0.3; the drug loading rate of the said silibinin-loaded silica nanoparticles is 51.29˜51.77%; the said silibinin solid dispersion contains povidone K30, soybean lecithin, acrylic resin IV, wherein the mass ratio between silibinin and other medical accessories is silibinin:povidone K30:soybean lecithin:acrylic resin IV=1:1˜3:0.3˜0.8:0.2˜0.5. Compared with the existing formulations, the half life of the high-efficacy, long-acting formulation of silibinin disclosed in this invention is 14.8 times longer while the mean residence time (MRT) of which is 4.
    Type: Grant
    Filed: November 23, 2009
    Date of Patent: May 5, 2015
    Assignee: Jiangsu University
    Inventors: Ximing Xu, Jiangnan Yu, Xia Cao, Yuan Zhu
  • Publication number: 20150119418
    Abstract: Provided is a pharmaceutical agent containing a compound represented by General Formula (1), a pharmaceutically acceptable salt thereof, or a solvate thereof: wherein A represents a C1-C3 linear alkylene group, in which one methylene group is optionally substituted with O or S; n represents an integer of from 3 to 5; X1 and X2 each independently represent CH or N; W1 and W2 each independently represent a carboxyl group or a tetrazolyl group; V represents a C1-C8 linear or branched alkylene group, in which one methylene group is optionally substituted with O or S; and R represents a substituted phenyl group, for example.
    Type: Application
    Filed: April 15, 2013
    Publication date: April 30, 2015
    Applicant: TOA EIYO LTD.
    Inventors: Kazuhiro Uemoto, Yoshimichi Sato, Naoki Okada, Emiko Iimori, Masayuki Kageyama
  • Publication number: 20150119388
    Abstract: An ester of ArOH according to the formula R—X—CO—OAr, wherein ArOH is a pharmaceutically active compound selected from the group consisting of SN-38, PI-103, etoposide and fenretinide, wherein a) R is a residue of cholesterol, sitosterol, SN-38, PI-103, etoposide or fenretinide and X is O—CO-L, wherein L is either a direct bond or a linking group including a branched or unbranched hydrocarbyl moiety that may optionally include in-chain or pendant heteroatom substituents and/or cyclic moieties; b) R—X—CO-0 is an all-trans retinoate radical or the 9-cis or 13-cis isomer thereof; or c) R—X— is a branched or unbranched, saturated or unsaturated hydrocarbyl moiety comprising at least 5 carbon atoms and optionally including at least one in-chain or pendant heteroatom substituent and/or cyclic moiety.
    Type: Application
    Filed: June 14, 2013
    Publication date: April 30, 2015
    Applicant: THE CHILDREN'S HOSPITAL PHILADELPHIA
    Inventors: Ivan Alferiev, Michael Chorny, Garrett M. Brodeur, Robert J. Levy
  • Publication number: 20150111889
    Abstract: The present invention relates to compounds of the formula (I), wherein the residues A, R1 to R5, Z1 and Z2 have the meanings indicated in the claims. The compounds of the formula (I) are valuable pharmacologically active compounds for use in the treatment of diverse disorders, for example cardiovascular disorders like thromboembolic diseases or restenoses. The compounds of the invention are effective antagonists of the platelet LPA receptor LPAR5 (GPR92) and can in general be applied in conditions in which an undesired activation of the platelet LPA receptor LPAR5, the mast cell LPA receptor LPAR5 or the microglia cell LPA receptor LPAR5 is present or for the cure or prevention of which an inhibition of the platelet, mast cell or microglia cell LPA receptor LPAR5 is intended. The invention furthermore relates to processes for the preparation of compounds of the formula (I), their use, in particular as active ingredients in medicaments, and pharmaceutical compositions comprising them.
    Type: Application
    Filed: May 16, 2013
    Publication date: April 23, 2015
    Applicant: SANOFI
    Inventors: Marc Nazare, Detlef Kozian, Martin Bossart, Werngard Czechtizky, Andreas Evers
  • Publication number: 20150104402
    Abstract: Provided are polyglyceryl compositions comprising one or more polyglyceryl compounds having: (a) a node structure comprising at least three contiguous glyceryl remnant units; (b) one or more cationic groups each linked to the node structure by an independently selected linking group; and (c) one or more hydrophobic moieties each independently (i) linked to the node structure by a linking group, or (ii) constituting a portion of one of the one or more cationic groups, wherein the composition has an average degree of polymerization determined by hydroxyl value testing (DPOH) of from about 3 to about 20. Also provided are polyglyceryl compounds which may compose such compositions, and uses of the polyglyceryl compositions and compounds.
    Type: Application
    Filed: December 18, 2014
    Publication date: April 16, 2015
    Inventors: Michael J. Fevola, Frank C. Sun, Stacey E. York
  • Publication number: 20150105453
    Abstract: Small molecule therapeutics for the treatment of parasitic diseases, in particular, semi-synthetic derivatives of the fugally-derived natural product merulin A for the treatment of African Sleeping Sickness.
    Type: Application
    Filed: December 17, 2014
    Publication date: April 16, 2015
    Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
    Inventors: Roger R Linington, Gabriel Navarro, Khanitha Pudhom, James McKerrow
  • Publication number: 20150104437
    Abstract: The present invention relates to methods of the treatment and diagnosis of bone mineral density related disorders. More particularly, the present invention relates to a method of diagnosing or predicting a hone mineral density related disease, or a risk of a bone mineral density related disease, in a subject, which method comprises detecting a mutation in the TBXAS1 gene, wherein the presence of said mutation is indicative of a bone mineral density related disease or of a risk of a bone mineral density related disease. The invention also relates to a compound selected in the group consisting of a thromboxane synthase (TXAS) encoding polynucleotide, a TXAS, thromboxane A2 or an analog thereof for treating or preventing a disease associated with an increased bone mineral density (e.g., Ghosal hematodiaphyseal dysplasia syndrome).
    Type: Application
    Filed: December 19, 2014
    Publication date: April 16, 2015
    Inventors: Valerie Cormier-Daire, Arnold Munnich
  • Publication number: 20150104403
    Abstract: Provided are polyglyceryl compositions comprising one or more polyglyceryl compounds having: (a) a node structure comprising at least three contiguous glyceryl remnant units; (b) one or more cationic groups each linked to the node structure by an independently selected linking group; and (c) one or more hydrophobic moieties each independently (i) linked to the node structure by a linking group, or (ii) constituting a portion of one of the one or more cationic groups, wherein the composition has an average degree of polymerization determined by hydroxyl value testing (DPOH) of from about 3 to about 20. Also provided are polyglyceryl compounds which may compose such compositions, and uses of the polyglyceryl compositions and compounds.
    Type: Application
    Filed: December 18, 2014
    Publication date: April 16, 2015
    Inventors: Michael J. Fevola, Frank C. Sun, Stacey E. York
  • Publication number: 20150099636
    Abstract: The present invention provides diacylhydrazine ligands and chiral diacylhydrazine ligands for use with ecdysone receptor-based inducible gene expression systems. Thus, the present invention is useful for applications such as gene therapy, large scale production of proteins and antibodies, cell-based screening assays, functional genomics, proteomics, metabolomics, and regulation of traits in transgenic organisms, where control of gene expression levels is desirable. An advantage of the present invention is that it provides a means to regulate gene expression and to tailor expression levels to suit the user's requirements.
    Type: Application
    Filed: October 9, 2014
    Publication date: April 9, 2015
    Inventors: Robert Eugene HORMANN, Bing Li
  • Publication number: 20150094307
    Abstract: Amino, amido, and heterocyclic compounds are disclosed. The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, diabetes complications, inflammation, and neurodegeneration, obesity, cancer, ischemia/reperfusion injury, cardiovascular disease and other diseases related to RAGE activity.
    Type: Application
    Filed: October 1, 2014
    Publication date: April 2, 2015
    Inventors: Ann Marie Schmidt, Ravichandran Ramasamy, Alexander Shekhtman, Vivek Rai, Michaele B. Manigrasso
  • Publication number: 20150087598
    Abstract: The invention provides method of treating cancers that express MUC1 by the administration of eIF4A helicase inhibitors. These inhibitors may advantageously be combined with peptides that inhibit MUC1 oligomerization, or with other standard anticancer therapies such as chemo-, radio- and surgical therapies.
    Type: Application
    Filed: May 13, 2013
    Publication date: March 26, 2015
    Applicant: DANA-FARBER CANCER INSTITUTE, INC.
    Inventor: Donald Kufe
  • Patent number: 8986683
    Abstract: The invention discloses a kit which comprises a formulation containing artemisinin or the derivatives thereof, a formulation containing ribonuclease, and a specification.
    Type: Grant
    Filed: September 10, 2012
    Date of Patent: March 24, 2015
    Assignees: Shanghai Biomodel Organism Science & Technology Co., Ltd., Shanghai Research Center for Model Organisms
    Inventors: Qingcheng Wang, Ruling Shen, Jun Li, Jian Fei, Zhugang Wang
  • Patent number: 8986665
    Abstract: Provided are polyglyceryl compositions comprising one or more polyglyceryl compounds having: (a) a node structure comprising at least three contiguous glyceryl remnant units; (b) one or more cationic groups each linked to the node structure by an independently selected linking group; and (c) one or more hydrophobic moieties each independently (i) linked to the node structure by a linking group, or (ii) constituting a portion of one of the one or more cationic groups, wherein the composition has an average degree of polymerization determined by hydroxyl value testing (DPOH) of from about 3 to about 20. Also provided are polyglyceryl compounds which may compose such compositions, and uses of the polyglyceryl compositions and compounds.
    Type: Grant
    Filed: December 20, 2011
    Date of Patent: March 24, 2015
    Assignee: Johnson & Johnson Consumer Companies, Inc.
    Inventors: Michael J. Fevola, Frank C. Sun, Stacey E. York
  • Publication number: 20150080460
    Abstract: There is disclosed a method for administration of a formulation of resiniferatoxin (RTX) to provide cardiac sympathetic afferent denervation when applied in an amount and concentration sufficient to chemically denervate vanilloid 1 receptor (TRPV1)-expressing CSAR (cardiac sympathetic afferent reflex) afferents. There is further disclosed a method for treating heart failure or hypertension and its related indications selected from the group consisting of increased sympatho-excitation, cardiac hypertrophy, increased left ventricular end diastolic pressure (LVEDP), lung edema, and combinations thereof, comprising administering an effective amount of RTX directly to a tissue site selected from the group consisting of epicardium, a T1-T4 dorsal root ganglion and intrathecally to the T1-T4 region of the spinal column.
    Type: Application
    Filed: September 11, 2014
    Publication date: March 19, 2015
    Applicant: Board of Regents of the University of Nebraska
    Inventors: Irving H. Zucker, Hanjun Wang
  • Publication number: 20150079189
    Abstract: In one embodiment, the present application discloses synthetic LDL nanoparticles comprising mixtures of components selected from the group consisting of phospholipids, triglycerides, cholesterol ester and free cholesterol; optionally further comprising an agent selected from the group consisting of natural antioxidants, ubiquinol and vitamin E, and methods for preparing the synthetic nanoparticles. The disclosed synthetic LDL nanoparticles are capable of selectively delivering lipophilic drugs and prodrugs to cellular targets expressing LDL receptors after intra venous injection.
    Type: Application
    Filed: September 13, 2014
    Publication date: March 19, 2015
    Applicant: Arbor Therapeutics, LLC
    Inventors: James D. McChesney, Igor Nikoulin, Steve J. Bannister, Douglas L. Rodenburg
  • Patent number: RE46558
    Abstract: Described herein are compositions and methods for preventing and/or treating diseases involving aberrant angiogenesis employing one or more benzo[c]chromen-6-one derivatives.
    Type: Grant
    Filed: July 1, 2015
    Date of Patent: September 26, 2017
    Assignee: PALOMA PHARMACEUTICALS, INC.
    Inventors: David I. Sherris, Manjinder Gill, Fupeng Ma, Sanjivanjit Kaur Bhal, Robert Dunn-Dufault, Miklos Feher, Peter Redden, Jonathan Schmidt
  • Patent number: RE48346
    Abstract: An olefin polymerization catalyst component comprising an internal electron donor compound shown in formula (I) below is provided in this disclosure: wherein X is O, S, NRa, PRb, or POORc, Ra is independently hydrogen, halogen, carbonyl hydrocarbon, linear or branched unsaturated or saturated alkyl hydrocarbon, cyclic, aromatic, or aliphatic hydrocarbon, Rb is independently hydrogen, halogen, carbonyl hydrocarbon, linear or branched unsaturated or saturated alkyl hydrocarbon, linear or branched unsaturated or saturated alkoxy hydrocarbon, cyclic, aromatic, or aliphatic hydrocarbon, Rc is independently hydrogen, carbonyl hydrocarbon, linear or branched unsaturated or saturated alkyl hydrocarbon, cyclic, aromatic, or aliphatic hydrocarbon, R1-R8 are identical or different hydrogen, halogen, linear or branched unsaturated or saturated C1-C30 alkyl, alone or in combination with C5-C30 substituted or unsubstituted 5-or 6-membered aliphatic or aromatic hydrocarbon rings, each of Ra, Rb, Rc, and/or R1-R8 are op
    Type: Grant
    Filed: May 1, 2019
    Date of Patent: December 8, 2020
    Assignee: BRASKEM AMERICA, INC.
    Inventors: Binh Thanh Nguyen, Jonas Alves Fernandes