Exactly One Oxygen Bonded Directly To The Cyclopentanohydrophenanthrene Ring System (e.g., Cholesterols, Cholestanols, Stigmasterols, Etc.) Patents (Class 552/544)
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Patent number: 12194103Abstract: Zwitterionic phosphatidylserine (ZPS) monomers, ZPS polymers and ZPS copolymers, methods for making the ZPS monomers, ZPS polymers, and ZPS copolymers, compositions and materials that include ZPS polymers and ZPS copolymers, and methods for using the ZPS monomers, ZPS polymers, and ZPS copolymers.Type: GrantFiled: March 25, 2019Date of Patent: January 14, 2025Assignee: University of WashingtonInventors: Shaoyi Jiang, Bowen Li, Priyesh Jain
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Patent number: 11117924Abstract: Compounds are provided according to Formula (I) and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein R1, R2, and R3 are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of conditions.Type: GrantFiled: July 6, 2016Date of Patent: September 14, 2021Assignee: SAGE THERAPEUTICS, INC.Inventors: Francesco G. Salituro, Albert Jean Robichaud, Gabriel Martinez Botella, Boyd L. Harrison
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Patent number: 11103589Abstract: The present application provides PEI compounds comprising a linker, PEI-polypeptide conjugates (e.g., PEI-antibody conjugates), and complexes thereof comprising a biologically active molecule. Methods of preparing and using the compounds, conjugates and complexes are further provided. The PEI-polypeptide conjugates and complexes are useful for delivering biologically active molecules to the cytoplasm of cells and promoting release of the biologically active molecules from the endo-lysosomal pathway.Type: GrantFiled: January 6, 2017Date of Patent: August 31, 2021Assignee: APG Therapeutics, Inc.Inventors: Joaquim Trias, Jaume Pons, David Shelton, Antoni Planas
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Patent number: 10227375Abstract: 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: GrantFiled: March 9, 2018Date of Patent: March 12, 2019Assignee: Sage Therapeutics, Inc.Inventors: Gabriel Martinez Botella, Boyd L. Harrison, Albert J. Robichaud, Francesco G. Salituro
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Patent number: 9907812Abstract: 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: GrantFiled: June 22, 2012Date of Patent: March 6, 2018Assignee: 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
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Patent number: 9504747Abstract: 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: GrantFiled: March 7, 2014Date of Patent: November 29, 2016Assignee: Novartis AGInventors: 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
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Patent number: 9139504Abstract: 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: GrantFiled: January 31, 2013Date of Patent: September 22, 2015Assignee: ALDIVIA SAInventors: Pierre Charlier De Chily, Mikaele Raynard
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Publication number: 20150148524Abstract: 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 sType: ApplicationFiled: July 8, 2013Publication date: May 28, 2015Inventors: Zhen Wang, Andrea Robinson, Nicolas Daniel Spiccia, William Roy Jackson
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Publication number: 20150141678Abstract: 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: ApplicationFiled: November 18, 2014Publication date: May 21, 2015Inventors: Joseph E. Payne, Padmanabh Chivukula
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Publication number: 20150056367Abstract: 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 repreType: ApplicationFiled: March 13, 2013Publication date: February 26, 2015Inventors: Yoshihiro Hosaka, Michihiko Sato, Mo Wu
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Patent number: 8956646Abstract: 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: GrantFiled: August 15, 2011Date of Patent: February 17, 2015Assignee: The Regents of the University of CaliforniaInventors: Francis C. Szoka, Jr., Colin Walsh, Vincent Venditto, Juliane Nguyen, Emily Perttu
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Publication number: 20150018436Abstract: 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: ApplicationFiled: January 14, 2013Publication date: January 15, 2015Applicants: 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
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Patent number: 8920859Abstract: 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: GrantFiled: March 19, 2012Date of Patent: December 30, 2014Assignee: Diageo Great Britain Ltd.Inventors: Daniel Albert Green, H. David Rosenfeld, Michael Jonathan Doby, Scott Winston, Harry Levine, Louise Slade, Dennis Brooks
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Publication number: 20140378645Abstract: 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: ApplicationFiled: January 7, 2013Publication date: December 25, 2014Inventors: Atsushi Kozaki, Michihiko Sato
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Publication number: 20140348900Abstract: 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: ApplicationFiled: March 13, 2014Publication date: November 27, 2014Applicant: Cureport, Inc.Inventor: De-Min Zhu
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Publication number: 20140323456Abstract: 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: ApplicationFiled: November 13, 2012Publication date: October 30, 2014Inventors: Daniel L. Alkon, Thomas J. Nelson
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Publication number: 20140309277Abstract: 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: ApplicationFiled: March 4, 2014Publication date: October 16, 2014Applicant: NOVARTIS AGInventors: Jeremy BARYZA, Keith BOWMAN, Andrew GEALL, Tanzina LABONTE, Cameron LEE, Chandra VARGEESE, Laura WEST, Junping ZHAO
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Publication number: 20140301967Abstract: 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: ApplicationFiled: April 9, 2013Publication date: October 9, 2014Applicants: AGENCY FOR SCIENCE, TECHNOLOGY AND RESEARCH, INTERNATIONAL BUSINESS MACHINES CORPORATIONInventors: 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
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Publication number: 20140235536Abstract: 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: ApplicationFiled: February 12, 2014Publication date: August 21, 2014Applicant: ADOCIAInventors: Olivier SOULA, Richard CHARVET, Alexandre GEISSLER
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Publication number: 20140235824Abstract: 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: ApplicationFiled: October 5, 2012Publication date: August 21, 2014Inventor: Christiaan Matthias Hubertus Gerard Reutelingsperger
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Publication number: 20140234349Abstract: 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: ApplicationFiled: October 1, 2012Publication date: August 21, 2014Inventors: Bror Morein, Saideh Berenjian, Kafei Hu
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Patent number: 8765171Abstract: 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: GrantFiled: March 9, 2010Date of Patent: July 1, 2014Assignees: The Regents of the University of California, Molecular Express, Inc.Inventors: Gary Fujii, Francis C. Szoka, Jr., Douglas S. Watson
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Patent number: 8669244Abstract: 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: GrantFiled: June 30, 2011Date of Patent: March 11, 2014Assignee: National Taiwan UniversityInventors: Ching-Jang Huang, Yueh-Hsiung Kuo, Chin Hsu
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Publication number: 20130345454Abstract: 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: ApplicationFiled: February 25, 2010Publication date: December 26, 2013Applicant: COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCHInventors: Bethala Lakshmi Anu Prabhavathi DEVI, Bhongiri YADAGIRI, Sanjit KANJILAL, Sistla RAMAKRISHNA, Kuncha MADHUSUDHANA, Prakash Vamanrao DlWAN, Rachapudi Badari Narayana PRASAD
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Patent number: 8586770Abstract: 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: GrantFiled: February 18, 2011Date of Patent: November 19, 2013Assignee: Harbor Therapeutics, Inc.Inventor: James M. Frincke
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Patent number: 8524696Abstract: 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: GrantFiled: April 28, 2009Date of Patent: September 3, 2013Assignee: National Research Council of CanadaInventors: Henryk Borowy-Borowski, Marianna Sikorska-Walker, P. Roy Walker
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Patent number: 8524928Abstract: 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: GrantFiled: July 24, 2009Date of Patent: September 3, 2013Assignee: Raisio Nutrition Ltd.Inventors: Jari Ekblom, Antti Hamunen, Rami Hartonen, Marko Hirvijärvi, Juha Holma, Juha Orte
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Publication number: 20130225663Abstract: 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: ApplicationFiled: August 27, 2012Publication date: August 29, 2013Applicant: Dicerna Pharmaceuticals, Inc.Inventor: Bob D. Brown
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Publication number: 20130216607Abstract: 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: ApplicationFiled: August 15, 2011Publication date: August 22, 2013Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventors: Francis C. Szoka, JR., Colin Walsh, Vincent Venditto, Juliane Nguyen, Emily Perttu
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Publication number: 20130195770Abstract: 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: ApplicationFiled: February 22, 2013Publication date: August 1, 2013Applicant: DuPont Nutrition Bioscience ApSInventor: DuPont Nutrition Bioscience ApS
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Publication number: 20130182202Abstract: 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: ApplicationFiled: August 29, 2011Publication date: July 18, 2013Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNGInventors: Archetti Graziano, Andreas Taugerbeck
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Publication number: 20130102577Abstract: 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: ApplicationFiled: April 11, 2011Publication date: April 25, 2013Applicant: The Research Foundation of the State University of New YorkInventors: William G. Kerr, John D. Chisholm
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Publication number: 20130078358Abstract: 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: ApplicationFiled: March 19, 2012Publication date: March 28, 2013Applicant: E I DU PONT DE NEMOURS AND COMPANYInventors: Daniel Albert Green, H. David Rosenfeld, Michael Jonathan Doby, Scott Winston, Harry Levine, Louise Slade, Dennis Brooks
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Publication number: 20130072438Abstract: 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: ApplicationFiled: September 13, 2012Publication date: March 21, 2013Inventor: Joel S. Goldberg
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Patent number: 8399441Abstract: 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: GrantFiled: February 19, 2010Date of Patent: March 19, 2013Assignee: Virginia Commonwealth UniversityInventors: Shunlin Ren, William M. Pandak
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Publication number: 20130052178Abstract: 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: ApplicationFiled: May 6, 2011Publication date: February 28, 2013Applicant: DuPont Nutrition Biosciences ApSInventors: Maria Jadwiga Bauerek, Charlotte Horsmans Poulsen, Jørn Borch Søe, Bent Raungaard, Leif Schauser
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Publication number: 20130053357Abstract: 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: ApplicationFiled: April 27, 2011Publication date: February 28, 2013Applicant: HISAMITSU PHARMACEUTICAL CO., INC.Inventors: Hidekazu Kuma, Kenji Atarashi, Kazuhiro Suzuki, Kazunosuke Aida
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Patent number: 8318961Abstract: 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: GrantFiled: July 11, 2006Date of Patent: November 27, 2012Assignee: PLT Patent & Licensing Trading Ltd.Inventor: Hans-Uwe Wolf
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Publication number: 20120253032Abstract: 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: ApplicationFiled: September 20, 2010Publication date: October 4, 2012Inventors: Mark Cameron, Jennifer R. Davis, Weimin Wang
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Publication number: 20120252772Abstract: 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: ApplicationFiled: June 30, 2011Publication date: October 4, 2012Applicant: NATIONAL TAIWAN UNIVERSITYInventors: CHING-JANG HUANG, YUEH-HSIUNG KUO, CHIN HSU
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Publication number: 20120245110Abstract: 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: ApplicationFiled: October 29, 2010Publication date: September 27, 2012Inventors: Young-Guen Kwon, Young-Ger Suh
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Publication number: 20120219538Abstract: 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: ApplicationFiled: November 1, 2010Publication date: August 30, 2012Applicants: THERAPEOMIC AG, UNIVERSITE DE GENEVEInventors: Gerrit Borchard, Claudia Mueller, Martinus Anne Hobbe Capelle, Tudor Arvinte
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Publication number: 20120189571Abstract: 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: ApplicationFiled: February 4, 2010Publication date: July 26, 2012Applicant: THE BRIGHAM AND WOMEN'S HOSPITAL., INC.Inventors: Shiladitya Sengupta, Abhimanyu Paraskar, Shivani Soni, Sudipta Basu, Poulomi Sengupta
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Publication number: 20120149894Abstract: 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: ApplicationFiled: August 18, 2010Publication date: June 14, 2012Inventors: Mark Cameron, Jennifer R. Davis, Andrea R. Geiser, Matthew G. Stanton, Vladislav V. Telyatnikov, Lu Tian, Weimin Wang
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Publication number: 20120108833Abstract: 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: ApplicationFiled: February 25, 2010Publication date: May 3, 2012Inventors: Bethala Lakshmi Anu Prabhavathi Devi, Bhongiri Yadagiri, Sanjit Kanjilal, Sistla Ramakrishna, Kuncha Madhusudhana, Prakash Vamanrao Diwan, Rachapudi Badari Narayana Prasad
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Patent number: 8163944Abstract: 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: GrantFiled: October 6, 2008Date of Patent: April 24, 2012Assignee: University of Maryland College ParkInventors: Michael P. Doyle, Arthur J. Catino, Hojae Choi, Jason M. Nichols
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Patent number: 8148551Abstract: 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: GrantFiled: December 29, 2006Date of Patent: April 3, 2012Assignee: Merck Patent Gesellschaft MIT Beschraenkter HaftungInventors: Rudolf Eidenschink, Holger Kretzschmann
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Publication number: 20120043491Abstract: 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: ApplicationFiled: December 15, 2008Publication date: February 23, 2012Applicant: Fraunhofer-Gesellschaft Zur Forderung Der Angewandten Forschung E.V.Inventors: Arno Seeboth, Olaf Mühling, Ralf Ruhmann
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Publication number: 20110311583Abstract: (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: ApplicationFiled: November 10, 2009Publication date: December 22, 2011Applicant: ALNYLAM PHARMACEUTICALS, INC.Inventors: Muthiah Manoharan, kallanthottathil G. Rajeev, Muthusamy Jayaraman, David Butler, Jayaprakash K. Narayanannair, Martin Maier, Laxman Eltepu
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Publication number: 20110305769Abstract: 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: ApplicationFiled: July 31, 2009Publication date: December 15, 2011Applicant: ENZON PHARMACEUTICALS, INC.Inventors: Hong Zhao, Weili Yan, Lianjun Shi, Dechun Wu