Exactly One Oxygen Bonded Directly To The Cyclopentanohydrophenanthrene Ring System (e.g., Cholesterols, Cholestanols, Stigmasterols, Etc.) Patents (Class 552/544)
  • Patent number: 10227375
    Abstract: Compounds are provided according to Formula (I): and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein R1, R2, R3a, R3b, R4, R5a, R5b, R6a, and R6b are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of CNS-related conditions.
    Type: Grant
    Filed: March 9, 2018
    Date of Patent: March 12, 2019
    Assignee: Sage Therapeutics, Inc.
    Inventors: Gabriel Martinez Botella, Boyd L. Harrison, Albert J. Robichaud, Francesco G. Salituro
  • Patent number: 9907812
    Abstract: The invention provides conjugate-based antifungal or antibacterial prodrugs formed by coupling at least one anti-fungal agent or antibacterial agent with at least one linker and/or carrier. The prodrugs are of formula: (i) (AFA)m-X-(L)n; (ii) [(AFA)m?-X]p-L; (iii) AFA-[X-(L)n?]q; or (iv) (AFA)m?-X, wherein: AFA is an antifungal agent or an antibacterial agent; L is a carrier; X is a linker; m ranges from 1 to 10; n ranges from 2 to 10; m? is 1 to 10; p is 1 to 10; n? is 1 to 10; and q is 1 to 10, provided that q? and n are not both 1; and m? is 1 to 10. The invention also provides nanoparticles comprising the conjugate-based prodrugs. Additionally, the invention also provides non-conjugated antifungal and antibacterial agents in the form of nanoparticles.
    Type: Grant
    Filed: June 22, 2012
    Date of Patent: March 6, 2018
    Assignee: VYOME BIOSCIENCES PVT. LTD.
    Inventors: Abhijit S. Bapat, Gauthami Mahesh, Rajesh S. Gokhale, Sayali S. Shah, Shiladitya Sengupta, Sudhanand Prasad, Sumana Ghosh, Suresh R. Chawrai, Nidhi Arora, D. Sreedhar Reddy, Mallika Mishra, Kirti Bajaj
  • Patent number: 9504747
    Abstract: This invention provides for a compound of formula (I): or a pharmaceutically acceptable salt thereof, wherein R1-R4, L and X are defined herein. The compounds of formula (I) and pharmaceutically acceptable salts thereof are cationic lipids useful in the delivery of biologically active agents to cells and tissues.
    Type: Grant
    Filed: March 7, 2014
    Date of Patent: November 29, 2016
    Assignee: Novartis AG
    Inventors: Jeremy Lee Baryza, Rohan Eric John Beckwith, Keith Bowman, Crystal Byers, Tanzina Fazal, Gabriel Grant Gamber, Cameron Chuck-munn Lee, Ritesh Bhanudasji Tichkule, Chandra Vargeese, Shuangxi Wang, Laura Ellen West, Thomas Zabawa, Junping Zhao
  • Patent number: 9139504
    Abstract: This invention proposes a lanolin substitute, capable of absorbing up to at least twice its weight of water or aqueous solution or aqueous suspension. It forms true emulsions, stable over time with a capacity for water absorption superior to that of lanolin. It also possesses the known emollient, moisturizing and occlusive properties of lanolin. This substitute is usable in all the present and future areas of application of lanolin: in the cosmetics industry, dermatology, and in industrial applications (polishes, lubricants . . . ). It is obtained by hemi-synthesis from a mixture of unsaturated fatty acids, esters of unsaturated fatty acids, unsaturated hydrocarbons or unsaturated derivatives of the latter and compounds comprising or generating hydroxyl functions, such as glycerol, preferably without a catalyst and in an atmosphere devoid of oxygen. Classical thermal treatment or preferably treatment by dielectric heating.
    Type: Grant
    Filed: January 31, 2013
    Date of Patent: September 22, 2015
    Assignee: ALDIVIA SA
    Inventors: Pierre Charlier De Chily, Mikaele Raynard
  • Publication number: 20150148524
    Abstract: A method for the synthesis of an amino acid analogue or a salt, solvate, derivative, isomer or tautomer thereof comprising the steps of: (i) subjecting an amino acid containing a metathesisable group to metathesis with a compound containing a complementary metathesisable group of formula (I) or (II): (Formulae (I), (II)) wherein R1 and R2 are independently selected from H and substituted or unsubstituted C1 to C4 alkyl; each R3 is either absent or independently selected from a heteroatom, a substituted or unsubstituted C1 to C20 alkyl, and a substituted or unsubstituted C1 to C20 alkyl group interrupted by one or more heteroatoms; and each X is independently selected from H and an effector molecule; in the presence of a reagent to catalyse the metathesis to form a dicarba bridge between the amino acid containing a metathesisable group and the compound containing a complementary metathesisable group; and (ii) reducing the dicarba bridge to form a saturated dicarba bridge, wherein the reagent used to catalyse s
    Type: Application
    Filed: July 8, 2013
    Publication date: May 28, 2015
    Inventors: Zhen Wang, Andrea Robinson, Nicolas Daniel Spiccia, William Roy Jackson
  • Publication number: 20150141678
    Abstract: What is described is a compound of formula (1) wherein R1 and R2 are the same or different, each a linear or branched alkyl with 1-9 carbons, or an alkenyl or alkynyl with 2 to 11 carbon atoms; L1 and L2 are the same or different, each a linear alkyl having 5 to 18 carbon atoms, or form a heterocycle with N; X1 is a bond, or is —CO—O— whereby L2-CO—O—R2 is formed; X2 is S or O; L3 is a bond or a lower alkyl, or form a heterocycle with N; R3 is a lower alkyl; and R4 and R5 are the same or different, each a lower alkyl; or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: November 18, 2014
    Publication date: May 21, 2015
    Inventors: Joseph E. Payne, Padmanabh Chivukula
  • Publication number: 20150056367
    Abstract: The present invention, which enables to align a liquid crystal molecule, when no voltage is applied thereto, and also to control pretilt angle of the liquid crystal molecule, relates to a composition for a liquid crystal alignment film comprising components represented by the following (A) to (D): (A) a meta-phenylene diamine derivative represented by the general formula [1]; (B) a meta-phenylene diamine derivative represented by the general formula [2]; (C) a para-arylene diamine represented by the general formula [3]; (D) a tetracarboxylic acid represented by the general formula [4] or a tetracarboxylic acid anhydride represented by the general formula [4?]; (wherein R1 represents an alkyl group having 1 to 6 carbon atoms or the like, R2 represents an alkyl group having 8 to 20 carbon atoms or the like, t moieties of Ra represent an alkyl group having 1 to 3 carbon atoms or the like, n represents an integer of 1 to 3, t represents an integer of 0 to 4, T represents an oxygen atom or the like, Y repre
    Type: Application
    Filed: March 13, 2013
    Publication date: February 26, 2015
    Inventors: Yoshihiro Hosaka, Michihiko Sato, Mo Wu
  • Patent number: 8956646
    Abstract: In various embodiments, the present invention provides zwitterionic lipids, encapsulants incorporating these zwitterionic lipids and such encapsulants encapsulating one or more bioactive agent. An exemplary bioactive agent is a nucleic acid. Also provided are pharmaceutical formulations of the encapsulants and methods of using such formulations to deliver a bioactive agent to a subject in treating or diagnosing disease in that subject.
    Type: Grant
    Filed: August 15, 2011
    Date of Patent: February 17, 2015
    Assignee: The Regents of the University of California
    Inventors: Francis C. Szoka, Jr., Colin Walsh, Vincent Venditto, Juliane Nguyen, Emily Perttu
  • Publication number: 20150018436
    Abstract: The invention provides new lipopolyamines of spermine type of the general formula I, wherein X is C—N bond or aminopolyethyleneglycolcarboxamide linker or o-hydroxy-alkylcarboxamide linker or ?-hydroxyalkylcarboxamidopolyethyleneglycol-carboxamide linker, and wherein a hydrophobic domain Y is an acyl symmetrically branched in the position C(2) or cholesteryl. The invention further provides a method of preparation of said lipopolyamines and their use for construction of polycationic liposomal drug carriers.
    Type: Application
    Filed: January 14, 2013
    Publication date: January 15, 2015
    Applicants: VYZKUMNY USTAV VETERINARNIHO LEKARSTVI, V.V.I., USTAV ORGANICKE CHEMIE A BIOCHEMIE AV CR, V.V.I.
    Inventors: Lukas Drasar, Miroslav Ledvina, Zina Korvasova, Jaroslav Turanek
  • Patent number: 8920859
    Abstract: A stigmasterol-rich phytosterol composition is prepared wherein the composition comprises at least 50% stigmasterol, based on the total weight of phytosterols, no more than 1000 ppm water, no more than 50 ppm ethanol, and wherein stigmasterol is at least 98% in the anhydrous form. A ready-to-freeze beverage is provided comprising the stigmasterol-rich composition and water, with optional additives. A frozen beverage is prepared from the ready-to-freeze beverage as a pourable slush. There are further provided processes to prepare the ready-to-freeze beverage and the frozen slush beverage.
    Type: Grant
    Filed: March 19, 2012
    Date of Patent: December 30, 2014
    Assignee: Diageo Great Britain Ltd.
    Inventors: Daniel Albert Green, H. David Rosenfeld, Michael Jonathan Doby, Scott Winston, Harry Levine, Louise Slade, Dennis Brooks
  • Publication number: 20140378645
    Abstract: A problem of the present invention is to provide a liquid crystal aligning agent which never deteriorates even in a method where UV is irradiated such as a liquid crystal dropping method or the like, and is capable of forming a liquid crystal alignment film having high UV resistance.
    Type: Application
    Filed: January 7, 2013
    Publication date: December 25, 2014
    Inventors: Atsushi Kozaki, Michihiko Sato
  • Publication number: 20140348900
    Abstract: The present invention provides for a process for preparing liposomes, lipid discs, and other lipid nanoparticles using a multi-port manifold, wherein the lipid solution stream, containing an organic solvent, is mixed with two or more streams of aqueous solution (e.g., buffer). In some aspects, at least some of the streams of the lipid and aqueous solutions are not directly opposite of each other. Thus, the process does not require dilution of the organic solvent as an additional step. In some embodiments, one of the solutions may also contain an active pharmaceutical ingredient (API). This invention provides a robust process of liposome manufacturing with different lipid formulations and different payloads. Particle size, morphology, and the manufacturing scale can be controlled by altering the port size and number of the manifold ports, and by selecting the flow rate or flow velocity of the lipid and aqueous solutions.
    Type: Application
    Filed: March 13, 2014
    Publication date: November 27, 2014
    Applicant: Cureport, Inc.
    Inventor: De-Min Zhu
  • Publication number: 20140323456
    Abstract: The present disclosure relates to esters of 8-[2-(2-pentyl-cyclopropylmethyl)cyclopropyl]-octanoic acid (“DCPLA”). The disclosure further relates to compositions, kits, and methods for treatment using the esters.
    Type: Application
    Filed: November 13, 2012
    Publication date: October 30, 2014
    Inventors: Daniel L. Alkon, Thomas J. Nelson
  • Publication number: 20140309277
    Abstract: Disclosed are formulation and optimization protocols for delivery of therapeutically effective amounts of biologically active agents to liver, tumors, and/or other cells or tissues. Also provided are compositions and uses for cationic lipid compounds of formula (I). The invention also relates to compositions and uses for stealth lipids of formula (XI). Also provided are processes for making such compounds, compositions, and formulations, plus methods and uses of such compounds, compositions, and formulations to deliver biologically active agents to cells and/or tissues.
    Type: Application
    Filed: March 4, 2014
    Publication date: October 16, 2014
    Applicant: NOVARTIS AG
    Inventors: Jeremy BARYZA, Keith BOWMAN, Andrew GEALL, Tanzina LABONTE, Cameron LEE, Chandra VARGEESE, Laura WEST, Junping ZHAO
  • Publication number: 20140301967
    Abstract: Antimicrobial cationic polymers having one or two cationic polycarbonate chains were prepared by organocatalyzed ring opening polymerization. One antimicrobial cationic polymer has a polymer chain consisting essentially of cationic carbonate repeat units linked to one or two end groups. The end groups can comprise a covalently bound form of biologically active compound such as cholesterol. Other antimicrobial cationic polymers have a random copolycarbonate chain comprising a minor mole fraction of hydrophobic repeat units bearing a covalently bound form of a vitamin E and/or vitamin D2. The cationic polymers exhibit high activity and selectivity against Gram-negative and Gram-positive microbes and fungi.
    Type: Application
    Filed: April 9, 2013
    Publication date: October 9, 2014
    Applicants: AGENCY FOR SCIENCE, TECHNOLOGY AND RESEARCH, INTERNATIONAL BUSINESS MACHINES CORPORATION
    Inventors: Willy Chin, Daniel J. Coady, Richard A. Dipietro, Amanda C. Engler, James L. Hedrick, Ashlynn L. Z. Lee, Victor W. L. Ng, Zhan-Yuin Ong, Yi Yan Yang
  • Publication number: 20140235536
    Abstract: A composition in the form of an injectable aqueous solution, the pH of which is from 6.6 to 7.8, comprises at least: a) a basal insulin, the isoelectric point pI of which is between 5.8 and 8.5; and b) an anionic compound bearing carboxylate charges and hydrophobic radicals. The composition may also include a prandial insulin.
    Type: Application
    Filed: February 12, 2014
    Publication date: August 21, 2014
    Applicant: ADOCIA
    Inventors: Olivier SOULA, Richard CHARVET, Alexandre GEISSLER
  • Publication number: 20140235824
    Abstract: A method to wash wool containing lanolin and impurities includes the steps of providing a volume of an aqueous liquid at a temperature below a melting temperature of the lanolin, soaking the wool in the volume of the liquid, creating air bubbles in the liquid and allowing the air bubbles to pass through the wool to attach the impurities, removing the air bubbles and attached impurities from the volume, and separating lanolin from wool containing lanolin and impurities, along with the wool and lanolin obtainable by this method.
    Type: Application
    Filed: October 5, 2012
    Publication date: August 21, 2014
    Inventor: Christiaan Matthias Hubertus Gerard Reutelingsperger
  • Publication number: 20140234349
    Abstract: The present invention regards nanoparticles comprising a sterol and a component derived from Quillaja saponaria Molina selected from quillaja acid and quillaja saponin, which nanoparticles do not comprise a phospholipid. It also relates to a composition comprising the nanoparticles, and the use thereof as adjuvant, especially in vaccines, as carriers for amphipathic or hydrophobic molecules and as agents for treatment of cancer. Further, it regards a method for producing the phospholipid-free nanoparticles, a method for the treatment of cancer and a method for assessing the applicability of the cancer treating method.
    Type: Application
    Filed: October 1, 2012
    Publication date: August 21, 2014
    Inventors: Bror Morein, Saideh Berenjian, Kafei Hu
  • Patent number: 8765171
    Abstract: The present invention relates to liposomal vaccine compositions, methods for the manufacture thereof, and methods for the use thereof to stimulate an immune response in an animal. These compositions comprise dimyristoylphosphatidylcholine (“DMPC”); either dimyristoylphosphatidylglycerol (“DMPG”) or dimyristoyltrimethylammonium propane (“DMTAP”) or both DMPC and DMTAP; and at least one sterol derivative providing a covalent anchor for one or more immunogenic polypeptide(s) or carbohydrate(s).
    Type: Grant
    Filed: March 9, 2010
    Date of Patent: July 1, 2014
    Assignees: The Regents of the University of California, Molecular Express, Inc.
    Inventors: Gary Fujii, Francis C. Szoka, Jr., Douglas S. Watson
  • Patent number: 8669244
    Abstract: Disclosed is a cucurbitane-triterpenoid compound for activating estrogen receptor activity, and a pharmaceutical composition, use and preparation method thereof. The cucurbitane-triterpenoid compound is presented as formula (I): wherein a single bond or a double bond is formed between C5 and C10, and a single bond or a double bond is fromed between C8 and C9; when a single bond is formed between C5 and C10, the R1 is oxygen; while a single bond is formed between C8 and C9, R2 is carbonyl group (—C?O), methyl hydroxyl group (—CH(OH)), methyl ketone or methyl dimethoxy group (—CH(OCH3)2); and wherein while R1 is oxygen (—O—) and R2 is carbonyl group (—C?O) or methyl hydroxyl group (—CH(OH)), a single bond is formed between R1 (—O—) and C19 of R2 such that R1 and R2 are formed tetrahydro-2H-pyran-2-one or hemiacetal ring.
    Type: Grant
    Filed: June 30, 2011
    Date of Patent: March 11, 2014
    Assignee: National Taiwan University
    Inventors: Ching-Jang Huang, Yueh-Hsiung Kuo, Chin Hsu
  • Publication number: 20130345454
    Abstract: The present invention relates to a synthetic method for the preparation of phytosteryl ferulate using ferulic acid and phytosterols (isolated from soybean oil deodorizer distillate) comprising of (a) acetylation of ferulic acid to ferulic acid acetate; (b) esterification of ferulic acid acetate with phytosterols to obtain phytosteryl ferulate acetate; (c) deprotection of phytosteryl ferulate acetate to phytosteryl ferulate. The phytosteryl ferulate was evaluated for hypocholesteremic activity in hamsters in comparison with that of natural oryzanol isolated from rice bran oil soap stock. This study confirmed that the phytosteryl ferulate significantly lowers the elevated cholesterol levels and also interferes with the absorption of cholesterol and the effect is comparable with that of natural oryzanol and is useful as nutraceutical/food supplement. Hence phytosteryl ferulate is a potential substitute for natural oryzanol for several applications.
    Type: Application
    Filed: February 25, 2010
    Publication date: December 26, 2013
    Applicant: COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCH
    Inventors: Bethala Lakshmi Anu Prabhavathi DEVI, Bhongiri YADAGIRI, Sanjit KANJILAL, Sistla RAMAKRISHNA, Kuncha MADHUSUDHANA, Prakash Vamanrao DlWAN, Rachapudi Badari Narayana PRASAD
  • Patent number: 8586770
    Abstract: The invention relates to methods to manipulate stem cells in vivo and in vitro to treat, e.g., a condition where cell or tissue repair is needed.
    Type: Grant
    Filed: February 18, 2011
    Date of Patent: November 19, 2013
    Assignee: Harbor Therapeutics, Inc.
    Inventor: James M. Frincke
  • Patent number: 8524928
    Abstract: The invention relates to an effective process for producing plant stanol by hydrogenating plant sterol in an organic solvent at a hydrogen pressure of 1-200 bar in the presence of a hydrogenation catalyst.
    Type: Grant
    Filed: July 24, 2009
    Date of Patent: September 3, 2013
    Assignee: Raisio Nutrition Ltd.
    Inventors: Jari Ekblom, Antti Hamunen, Rami Hartonen, Marko Hirvijärvi, Juha Holma, Juha Orte
  • Patent number: 8524696
    Abstract: Water-soluble compositions comprising a lipophilic compound and a solubilizing agent of the general formula: {X—OOC—[(CH2)n—COO]m}p—Y??(I) wherein: X is a residue of a hydrophobic moiety, Y is a residue of a hydrophilic moiety, p is 1 or 2, m is 0 or 1, and n is an integer greater than or equal to 0 are disclosed. The lipophilic compound is preferably selected from the group consisting of water-insoluble ubiquinones, ubiquinols, vitamins, provitamins, polyene macrolide antibiotics, and mixtures thereof. The hydrophobic moiety is preferably a sterol or a tocopherol and the hydrophilic moiety is preferably a polyalkylene glycol. In some embodiments, the sterol is cholesterol or sitosterol, the tocopherol is ?-(+)-tocopherol, the polyalkylene glycol is a polyethylene glycol or its methyl monoether having an average molecular weight between 400 and 1000, p is equal to 1 or 2, m is equal to 0 or 1 and n is an integer between 2 and 18.
    Type: Grant
    Filed: April 28, 2009
    Date of Patent: September 3, 2013
    Assignee: National Research Council of Canada
    Inventors: Henryk Borowy-Borowski, Marianna Sikorska-Walker, P. Roy Walker
  • Publication number: 20130225663
    Abstract: The invention provides formulations that contain an immunogenic or immunostimulatory cargo, delivery moiety and/or lipid, and a lipid that functions to reduce or prevent induction in a subject of an immune response which would otherwise occur when the immunogenic or immunostimulatory cargo, delivery moiety and/or lipid is administered to a subject as a component of an appropriate control formulation lacking the immune response reducing lipid. Specific immune response reducing lipids and uses thereof are further provided.
    Type: Application
    Filed: August 27, 2012
    Publication date: August 29, 2013
    Applicant: Dicerna Pharmaceuticals, Inc.
    Inventor: Bob D. Brown
  • Publication number: 20130216607
    Abstract: In various embodiments, the present invention provides zwitterionic lipids, encapsulants incorporating these zwitterionic lipids and such encapsulants encapsulating one or more bioactive agent. An exemplary bioactive agent is a nucleic acid. Also provided are pharmaceutical formulations of the encapsulants and methods of using such formulations to deliver a bioactive agent to a subject in treating or diagnosing disease in that subject.
    Type: Application
    Filed: August 15, 2011
    Publication date: August 22, 2013
    Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
    Inventors: Francis C. Szoka, JR., Colin Walsh, Vincent Venditto, Juliane Nguyen, Emily Perttu
  • Publication number: 20130195770
    Abstract: The present invention relates to a method for reducing cholesterol absorption and the occurrence of atherosclerotic lesions in an animal comprising administering to the animal a composition comprising an effective amount of at least one cholesterol ester.
    Type: Application
    Filed: February 22, 2013
    Publication date: August 1, 2013
    Applicant: DuPont Nutrition Bioscience ApS
    Inventor: DuPont Nutrition Bioscience ApS
  • Publication number: 20130182202
    Abstract: The present invention relates to liquid-crystalline media (LC media) having negative or positive dielectric anisotropy comprising self-aligning mesogens (SAMs) which effect homeotropic (vertical) alignment of the LC media at a surface or the cell walls of a liquid-crystal display (LC display). The invention therefore also encompasses LC displays having homeotropic alignment of the liquid-crystalline medium (LC medium) without conventional imide alignment layers. The LC media may be supplemented by a polymerisable or polymerised component, which serves for stabilisation of the alignment, for adjustment of the tilt angle and/or as passivation layer.
    Type: Application
    Filed: August 29, 2011
    Publication date: July 18, 2013
    Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNG
    Inventors: Archetti Graziano, Andreas Taugerbeck
  • Publication number: 20130102577
    Abstract: The present invention relates to SHIP inhibitor compounds and methods for using these compounds. In particular, the present invention discloses the following methods: (i) a method of treating graft versus host disease in a subject; (ii) a method of inhibiting a SHIP1 protein in a cell; (iii) a method of selectively inhibiting a SHIP1 protein in a cell; (iv) a method for treating or preventing graft-versus-host disease (GVHD) in a recipient of an organ or tissue transplant; (v) a method of modulating SHIP activity in a cell expressing SHIP1 or SHIP2; (vi) a method of ex vivo or in vitro treatment of transplants; (vii) a method of inhibiting tumor growth and metastasis in a subject; (viii) a method of treating a hematologic malignancy in a subject; (ix) a method of inducing apoptosis of multiple myeloma cells; (x) a method of treating multiple myeloma in a subject; (xi) a method of inhibiting the proliferation of a human breast cancer cell; and (xii) a method of treating breast cancer in a subject.
    Type: Application
    Filed: April 11, 2011
    Publication date: April 25, 2013
    Applicant: The Research Foundation of the State University of New York
    Inventors: William G. Kerr, John D. Chisholm
  • Publication number: 20130078358
    Abstract: A stigmasterol-rich phytosterol composition is prepared wherein the composition comprises at least 50% stigmasterol, based on the total weight of phytosterols, no more than 1000 ppm water, no more than 50 ppm ethanol, and wherein stigmasterol is at least 98% in the anhydrous form. A ready-to-freeze beverage is provided comprising the stigmasterol-rich composition and water, with optional additives. A frozen beverage is prepared from the ready-to-freeze beverage as a pourable slush. There are further provided processes to prepare the ready-to-freeze beverage and the frozen slush beverage.
    Type: Application
    Filed: March 19, 2012
    Publication date: March 28, 2013
    Applicant: E I DU PONT DE NEMOURS AND COMPANY
    Inventors: Daniel Albert Green, H. David Rosenfeld, Michael Jonathan Doby, Scott Winston, Harry Levine, Louise Slade, Dennis Brooks
  • Publication number: 20130072438
    Abstract: Disclosed herein are opioid peptide conjugates (for example, opioid peptide esters). In some embodiments, the disclosed conjugates include an opioid peptide consisting of two to six amino acids and a moiety conjugated to the opioid peptide by an ester bond. In some examples, the moiety is an alcohol, a sugar, a lipid, or dehydroascorbic acid. Also disclosed are methods of altering nociception including administering an effective amount of one or more disclosed opioid peptide conjugates to a subject (such as a human subject).
    Type: Application
    Filed: September 13, 2012
    Publication date: March 21, 2013
    Inventor: Joel S. Goldberg
  • Patent number: 8399441
    Abstract: The sulfated oxysterol 5-cholesten-3?, 25-diol 3-sulphate, a nuclear cholesterol metabolite that decreases lipid biosynthesis and increases cholesterol secretion and degradation, is provided as an agent to lower intracellular and serum cholesterol and/or triglycerides, and to prevent or treat lipid accumulation-associated inflammation and conditions associated with such inflammation. Methods which involve the use of this sulfated oxysterol to treat conditions associated with high cholesterol and/or high triglycerides and/or inflammation (e.g. hypercholesterolemia, hypertriglyceridemia, non-alcoholic fatty liver diseases, atherosclerosis, etc.) are also provided.
    Type: Grant
    Filed: February 19, 2010
    Date of Patent: March 19, 2013
    Assignee: Virginia Commonwealth University
    Inventors: Shunlin Ren, William M. Pandak
  • Publication number: 20130052178
    Abstract: The present invention relates to a method for reducing cholesterol absorption in an animal comprising administering to the animal a composition comprising an effective amount of at least one cholesterol ester.
    Type: Application
    Filed: May 6, 2011
    Publication date: February 28, 2013
    Applicant: DuPont Nutrition Biosciences ApS
    Inventors: Maria Jadwiga Bauerek, Charlotte Horsmans Poulsen, Jørn Borch Søe, Bent Raungaard, Leif Schauser
  • Publication number: 20130053357
    Abstract: Provided is a skin irritation suppressant for transdermal preparations, having a sufficient reduction effect of skin irritation due to a drug. Also provided is a transdermal preparation comprising the skin irritation suppressant. One embodiment of the invention is a skin irritation suppressant for suppressing the skin irritation due to a drug and a pharmaceutical ingredient to be used in a transdermal preparation other than the drug, the skin irritation suppressant comprising a sterol compound selected from the group consisting of cholesterol, cholesterol derivatives and cholesterol analogs, and the drug is one or more basic drugs selected from the group consisting of tolterodine, asenapine, bisoprolol, risperidone, nicotine and citalopram, and their pharmaceutically acceptable salts.
    Type: Application
    Filed: April 27, 2011
    Publication date: February 28, 2013
    Applicant: HISAMITSU PHARMACEUTICAL CO., INC.
    Inventors: Hidekazu Kuma, Kenji Atarashi, Kazuhiro Suzuki, Kazunosuke Aida
  • Patent number: 8318961
    Abstract: The invention relates to new substances which are derived from cholesterol, cholesterol sulphate and cholesterol esters of a natural, semi-synthetic or synthetic origin in that they represent oligomers with a specific type of cross-linkage of the starting substances based on cholesterol.
    Type: Grant
    Filed: July 11, 2006
    Date of Patent: November 27, 2012
    Assignee: PLT Patent & Licensing Trading Ltd.
    Inventor: Hans-Uwe Wolf
  • Publication number: 20120252772
    Abstract: Disclosed is a cucurbitane-triterpenoid compound for activating estrogen receptor activity, and a pharmaceutical composition, use and preparation method thereof. The cucurbitane-triterpenoid compound is presented as formula (I): wherein a single bond or a double bond is formed between C5 and C10, and a single bond or a double bond is fromed between C8 and C9; when a single bond is formed between C5 and C10, the R1 is oxygen; while a single bond is formed between C8 and C9, R2 is carbonyl group (—C?O), methyl hydroxyl group (—CH(OH)), methyl ketone or methyl dimethoxy group (—CH(OCH3)2); and wherein while R1 is oxygen (—O—) and R2 is carbonyl group (—C?O) or methyl hydroxyl group (—CH(OH)), a single bond is formed between R1 (—O—) and C19 of R2 such that R1 and R2 are formed tetrahydro-2H-pyran-2-one or hemiacetal ring.
    Type: Application
    Filed: June 30, 2011
    Publication date: October 4, 2012
    Applicant: NATIONAL TAIWAN UNIVERSITY
    Inventors: CHING-JANG HUANG, YUEH-HSIUNG KUO, CHIN HSU
  • Publication number: 20120253032
    Abstract: The instant invention provides for novel cationic lipids with short lipid chains that can be used in combination with other lipid components such as cholesterol and PEG-lipids to form lipid nanoparticles with oligonucleotides, to facilitate the cellular uptake and endosomal escape, and to knockdown target mRNA both in vitro and in vivo while decreasing inflammatory toxicities.
    Type: Application
    Filed: September 20, 2010
    Publication date: October 4, 2012
    Inventors: Mark Cameron, Jennifer R. Davis, Weimin Wang
  • Publication number: 20120245110
    Abstract: The present disclosure relates to a novel vascular leakage inhibitor. The novel vascular leakage inhibitor of the present disclosure inhibits the apoptosis of vascular endothelial cells, inhibits the formation of actin stress fibers induced by VEGF, enhances the cortical actin ring structure, and improves the stability of the tight junctions (TJs) between vascular cells, thereby inhibiting vascular leakage. The vascular leakage inhibitor of the present disclosure has the activity of not only reducing vascular permeability but also recovering the integrity of damaged blood vessels. Accordingly, the vascular leakage inhibitor of the present disclosure can prevent or treat various diseases caused by vascular leakage. Since the vascular leakage inhibitor of the present disclosure is synthesized from commercially available or easily synthesizable cholesterols, it has remarkably superior feasibility of commercial synthesis.
    Type: Application
    Filed: October 29, 2010
    Publication date: September 27, 2012
    Inventors: Young-Guen Kwon, Young-Ger Suh
  • Publication number: 20120219538
    Abstract: The present invention is directed to stable protein formulations, related methods and uses thereof. In particular, the invention relates to a method of stabilizing therapeutic proteins in aqueous solution.
    Type: Application
    Filed: November 1, 2010
    Publication date: August 30, 2012
    Applicants: THERAPEOMIC AG, UNIVERSITE DE GENEVE
    Inventors: Gerrit Borchard, Claudia Mueller, Martinus Anne Hobbe Capelle, Tudor Arvinte
  • Publication number: 20120189571
    Abstract: The invention is directed to biocompatible conjugated polymer nanoparticles including a copolymer backbone, a plurality of sidechains covalently linked to said backbone, and a plurality of platinum compounds dissociably linked to said backbone. The invention is also directed to dicarbonyl-lipid compounds wherein a platinum compound is dissociably linked to the dicarbonyl compound. The invention is also directed to methods of treating cancer or metastasis. The methods includes selecting a subject in need of treatment for cancer or metastasis and administering to the subject an effective amount of any of the nanoparticles, compounds, or compositions of the invention.
    Type: Application
    Filed: February 4, 2010
    Publication date: July 26, 2012
    Applicant: THE BRIGHAM AND WOMEN'S HOSPITAL., INC.
    Inventors: Shiladitya Sengupta, Abhimanyu Paraskar, Shivani Soni, Sudipta Basu, Poulomi Sengupta
  • Publication number: 20120149894
    Abstract: The instant invention provides for novel cationic lipids that can be used in combination with other lipid components such as cholesterol and PEG-lipids to form lipid nanoparticles with siRNA, to facilitate the cellular uptake and endosomal escape, and to knockdown target mRNA both in vitro and in vivo.
    Type: Application
    Filed: August 18, 2010
    Publication date: June 14, 2012
    Inventors: Mark Cameron, Jennifer R. Davis, Andrea R. Geiser, Matthew G. Stanton, Vladislav V. Telyatnikov, Lu Tian, Weimin Wang
  • Publication number: 20120108833
    Abstract: A method is provided for controlling the operating temperature of a catalytic reactor using a closed-loop system that provides for varying the reactor input and other operating parameters in order to maintain the operating temperature of the reactor at or near the initial setpoint temperature for operation of the reactor. In one example, maximum and minimum operating temperatures with a catalytic partial oxidation reactor are controlled, as well as maintaining control over the corresponding minimum required ratio of oxygen atoms to carbon atoms, such that the operating temperature within the reactor is maintained below the material limits but above threshold temperatures for coking.
    Type: Application
    Filed: February 25, 2010
    Publication date: May 3, 2012
    Inventors: Bethala Lakshmi Anu Prabhavathi Devi, Bhongiri Yadagiri, Sanjit Kanjilal, Sistla Ramakrishna, Kuncha Madhusudhana, Prakash Vamanrao Diwan, Rachapudi Badari Narayana Prasad
  • Patent number: 8163944
    Abstract: The present invention relates to compositions and methods for achieving the efficient allylic oxidation of organic molecules, especially olefins and steroids, under aqueous conditions. The invention concerns the use of dirhodium (II,II) “paddlewheel complexes, and in particular, dirhodium carboximate and tert-butyl hydroperoxide as catalysts for the reaction. The use of aqueous conditions is particularly advantageous in the allylic oxidation of 7-keto steroids, which could not be effectively oxidized using anhydrous methods, and in extending allylic oxidation to enamides and enol ethers.
    Type: Grant
    Filed: October 6, 2008
    Date of Patent: April 24, 2012
    Assignee: University of Maryland College Park
    Inventors: Michael P. Doyle, Arthur J. Catino, Hojae Choi, Jason M. Nichols
  • Patent number: 8148551
    Abstract: The invention relates to tricyclic aromatics of the general formula I in which A1, A2, A3, A4, Q1-Q2, R1, R2, X1, X2, X3, Z1, Z2, Z3, Z4, q, r, s, t and u have the meaning indicated, and to the use thereof as components of liquid-crystalline media and to an electro-optical display element containing same.
    Type: Grant
    Filed: December 29, 2006
    Date of Patent: April 3, 2012
    Assignee: Merck Patent Gesellschaft MIT Beschraenkter Haftung
    Inventors: Rudolf Eidenschink, Holger Kretzschmann
  • Publication number: 20120043491
    Abstract: The invention relates to doping capsules which have a substance which displays a decreasing transparency with increasing temperature within a defined temperature range due to physicochemical interactions with the polymer matrix to be doped. Likewise, the invention relates to composite systems which have a polymer matrix doped with the doping capsules. The capsules according to the invention are used for sun protection or heat reflection.
    Type: Application
    Filed: December 15, 2008
    Publication date: February 23, 2012
    Applicant: Fraunhofer-Gesellschaft Zur Forderung Der Angewandten Forschung E.V.
    Inventors: Arno Seeboth, Olaf Mühling, Ralf Ruhmann
  • Publication number: 20110311583
    Abstract: (A1) Translate this text The present invention provides lipids that are advantageously used in lipid particles for the in vivo delivery of therapeutic agents to cells.
    Type: Application
    Filed: November 10, 2009
    Publication date: December 22, 2011
    Applicant: ALNYLAM PHARMACEUTICALS, INC.
    Inventors: Muthiah Manoharan, kallanthottathil G. Rajeev, Muthusamy Jayaraman, David Butler, Jayaprakash K. Narayanannair, Martin Maier, Laxman Eltepu
  • Publication number: 20110305769
    Abstract: The present invention is directed to cationic lipid for the delivery of oligonucleotides and methods of modulating an expression of a targeted gene using the nanoparticle compositions. In particular, the invention relates to cholesterol and its derivatives having multiple positively charged moieties via branching spacers, and nanoparticle compositions of oligonucleotides encapsulated in a mixture of a cationic lipid, a fusogenic lipid and a PEG lipid.
    Type: Application
    Filed: July 31, 2009
    Publication date: December 15, 2011
    Applicant: ENZON PHARMACEUTICALS, INC.
    Inventors: Hong Zhao, Weili Yan, Lianjun Shi, Dechun Wu
  • Patent number: 8056362
    Abstract: This invention relates to a method and a device for purifying and/or separating preferably high melting organic raw products or compound mixtures containing, in particular, high melting and/or degradable sterols, by layer crystallization on first heat exchanger surfaces. The raw product is received in a solvent or solvent mixture, and then brought into contact with heat exchanger surfaces. The desired product crystallizes on the heat exchanger surfaces by slow cooling. Solvent evaporating during the crystallization or sweating process is condensed and returned to the mixture.
    Type: Grant
    Filed: July 26, 2006
    Date of Patent: November 15, 2011
    Assignees: Sulzer Chemtech AG, Resitec Participacoes Ltda
    Inventors: Rodolfo Rohr, Ali Nikzad, Andrzej K. Kuszlik
  • Publication number: 20110236602
    Abstract: Diamine compounds, which in particular are useful as precursors for the production of liquid crystal alignment layers, are represented by the general formula I: wherein A1 represents an organic group of 1 to 40 carbon atoms; A2 represents a hydrogen atom or an organic group of 1 to 40 carbon atoms.
    Type: Application
    Filed: June 13, 2011
    Publication date: September 29, 2011
    Applicant: ROLIC AG
    Inventors: Guy MARCK, Olivier MULLER
  • Publication number: 20110229581
    Abstract: The present invention is directed to releasable cationic lipids and nanoparticle compositions for the delivery of nucleic acids and methods of modulating an expression of a target gene using the same. In particular, the invention relates to cationic lipids including an acid labile linker, and nanoparticle compositions containing the same.
    Type: Application
    Filed: November 17, 2009
    Publication date: September 22, 2011
    Applicant: ENZON PHARMACEUTICALS, INC.
    Inventors: Hong Zhao, Weili Yan, Lianjun Shi, Dechun Wu, Maksim Royzen