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Небесная энциклопедия

Космические корабли и станции, автоматические КА и методы их проектирования, бортовые комплексы управления, системы и средства жизнеобеспечения, особенности технологии производства ракетно-космических систем

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Мониторинг СМИ

Мониторинг СМИ и социальных сетей. Сканирование интернета, новостных сайтов, специализированных контентных площадок на базе мессенджеров. Гибкие настройки фильтров и первоначальных источников.

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Поддерживает ввод нескольких поисковых фраз (по одной на строку). При поиске обеспечивает поддержку морфологии русского и английского языка
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Применить Всего найдено 13589. Отображено 100.
12-01-2012 дата публикации

Drug Delivery System for Use in the Treatment of Vascular and Vessel-Related Pathologies

Номер: US20120010557A1
Автор: Michal Heger
Принадлежит: ACADEMISCH MEDISCH CENTRUM

The present invention relates to a drug delivery system for use in the treatment of vascular and vessel-related pathologies, comprising a drug delivery platform that comprises at least one compound capable of exerting an effect on the formation and/or maintenance of a thrombus in the vessel to be treated. The platform is preferably formed by liposomes that are sterically stabilized by grafting of poly(ethylene glycol) onto the liposome surface. The liposomes may further comprise photosensitizers and targeting molecules. The liposomes may be thermosensitive. The compound is suitably tranexamic acid. The drug delivery system is preferably used for the treatment of port wine stains.

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16-02-2012 дата публикации

Genetic polymorphisms associated with venous thrombosis, methods of detection and uses thereof

Номер: US20120039864A1

The present invention is based on the discovery of genetic polymorphisms that are associated with coronary heart disease and in particular VT and response to drug treatment. In particular, the present invention relates to nucleic acid molecules containing the polymorphisms, variant proteins encoded by such nucleic acid molecules, reagents for detecting the polymorphic nucleic acid molecules and proteins, and methods of using the nucleic acid and proteins as well as methods of using reagents for their detection.

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23-02-2012 дата публикации

Methods of reducing the risk of cardiovascular disease in postmenopausal women

Номер: US20120046249A1

The present invention features materials and methods for reducing the risk of cardiovascular disease in postmenopausal or perimenopausal women. More specifically, these methods can be used in women who generally have no apparent cardiovascular disease. We describe herein methods of administering non-antibacterial tetracycline or a sub-antimicrobial amount of antibacterial tetracyclines or tetracycline formulations and their use in reducing the risk that cardiovascular disease will develop in a subject (e.g., in a post- or perimenopausal woman)

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08-03-2012 дата публикации

nanoparticulate compositions of poorly soluble compounds

Номер: US20120058151A1
Принадлежит: CAPSULUTION PHARMA AG

The present invention relates to a method for the production of a nanoparticulate pharmaceutical composition. The method comprises the steps of a) suspending in water a poorly soluble active ingredient without the presence of a detergent, b) mechanically treating said suspension to obtain particles comprising the active ingredient with an effective average size of less than about 5000 nm, c) contacting said active ingredient or suspension with a first polyelectrolyte during and/or before mechanically treating, d) optionally contacting said suspension with a one or more second or further polyelectrolytes during, before and/or after mechanically treating, e) optionally drying said suspension. The invention also pertains to the pharmaceutical compositions obtained by the method of the invention.

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22-03-2012 дата публикации

Treatment of vascularized pigment epithelial detachment with anti-vegf therapy

Номер: US20120070428A1
Принадлежит: Genentech Inc

Methods for treating vascularized pigment epithelial detachment using anti-VEGF agents are disclosed.

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29-03-2012 дата публикации

Antagonists of pcsk9

Номер: US20120077964A1
Принадлежит: Merck Sharp and Dohme LLC

Antagonists of human proprotein convertase subtilisin-kexin type 9 (“PCSK9”) are disclosed. The disclosed antagonists are effective in the inhibition of PCSK9 function and, accordingly, present desirable antagonists for the use in the treatment of conditions associated with PCSK9 activity. The present invention also discloses nucleic acid encoding said antagonists, vectors, host cells, and compositions comprising the antagonists. Methods of making PCSK9-specific antagonists as well as methods of using the antagonists for inhibiting or antagonizing PCSK9 function are also disclosed and form important additional aspects of the present disclosure.

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14-06-2012 дата публикации

(e)-n-monoalkyl-3-oxo-3-(2-thienyl) propenamine and process for producing the same and process for producing (e,z)-n-monoalkyl-3-oxo-3-(2-thienyl) propenamine

Номер: US20120149917A1
Принадлежит: Sumitomo Seika Chemicals Co Ltd

The present invention provides a process for producing (E)-N-monoalkyl-3-oxo-3-(2-thienyl)propenamine represented by Formula (1); wherein R is a C 1-4 alkyl, the method comprising the steps of: maintaining a solution containing (Z)—N-monoalkyl-3-oxo-3-(2-thienyl)propenamine dissolved therein at 25° C. or below to deposit crystals and separating crystals having a particle diameter of 100 μm or less from the deposited crystals; and a process for producing (E,Z)—N-monoalkyl-3-oxo-3-(2-thienyl)propenamine comprising the steps of: reacting an alkali metal salt of β-oxo-β-(2-thienyl)propanal with a monoalkylamine compound; adding a water-insoluble organic solvent to the resulting reaction mixture; adding seed crystals containing (E)-N-monoalkyl-3-oxo-3-(2-thienyl)propenamine to an organic layer obtained by conducting separation; and keeping the resulting mixture at 25° C. or below.

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21-06-2012 дата публикации

Enzyme Treatment of Foodstuffs for Celiac Sprue

Номер: US20120156253A1

Administering an effective dose of glutenase to a Celiac or dermatitis herpetiformis patient reduces levels of toxic gluten oligopeptides, thereby attenuating or eliminating the damaging effects of gluten.

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28-06-2012 дата публикации

Supplement comprising blackcurrants or boysenberries

Номер: US20120164252A1
Принадлежит: Gibb Holdings Nelson Ltd

The present invention relates to a dietary supplement comprising one or more of processed whole blackcurrants, processed whole boysenberries, one or more natural component extracted from blackcurrants, and one or more natural component extracted from boysenberries. The dietary supplement is particularly, but not exclusively, suitable for animals.

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19-07-2012 дата публикации

Heart-slowing drug containing short-acting beta-blocker as teh active ingredient

Номер: US20120184545A1
Принадлежит: Ono Pharmaceutical Co Ltd

The present invention relates to an agent which slows down the heart rate which has an excellent controlling ability in diagnostic imaging comprising a short-acting β-blocker (e.g. landiolol hydrochloride or esmolol hydrochloride). The short-acting β-blocker has a property of slowing down the heart rate and it can temporarily suppress the tachycardia at diagnosis. According to the dose and the method of administration, it can control the period for the heart rate adjustment. Also, the present invention relates to a diagnostic imaging auxiliary comprising a short-acting β-blocker as active ingredient.

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02-08-2012 дата публикации

Ubiquitin interacting motif peptides as cancer therapeutics

Номер: US20120197059A1
Автор: HONG Chen, Yunzhou DONG
Принадлежит: Oklahoma Medical Research Foundation

The present invention involves the use peptides comprising ubiquitin interacting motifs (UIMs) alone or in combination with other agents to treat diseases involving neovascularization, such as cancer.

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23-08-2012 дата публикации

Cardiomyocytes and methods of producing and purifying cardiomyocytes

Номер: US20120213748A1
Автор: Gabriel Nistor
Принадлежит: Individual

The invention provides methods for producing a culture of cardiomyocytes and cultures of cardiomyocytes. Exemplary methods of producing and cultures of cardiomyocytes include a population of cells including cells having spontaneous and periodic electrical activity, and/or including nodal, sino-atrial or pacemaker cells; immature cardiomyocytes (cardiomyoblasts); mature contractile cardiomyocytes; or a mixed population of two or more of such cells.

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23-08-2012 дата публикации

Methods of treating a subject and related particles, polymers and compositions

Номер: US20120213854A1
Автор: Oliver S. Fetzer
Принадлежит: Individual

Described herein are methods for treating a subject with combinations of polymer-agent particles and cyclodextrin polymer agent conjugates. The methods herein may be used to treat subjects identified with cancer, cardiovascular disorders, autoimmune disorders, or inflammatory disorders. Also described herein are compositions, dosage forms, and kits comprising polymer-agent particles and cyclodextrin polymer agent conjugates.

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30-08-2012 дата публикации

Stablized Melanocortin Ligands

Номер: US20120220525A1
Автор: Kenneth A. Gruber
Принадлежит: Tensive Controls Inc

Compositions and methods are disclosed for a non-naturally occurring melanocortin ligand comprised of a melanocortin analog coupled to a degradation-resistant C-terminal extension and, optionally, an N-terminal extension, to produce a stable melanocortin ligand having diminished or abolished cardiovascular activity while retaining desired melanocortin regulatory activity.

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04-10-2012 дата публикации

Oral lysophilisates containing pvp/va

Номер: US20120252795A1
Автор: Thanh-Tam Nguyen
Принадлежит: Cephalon France SAS

The present invention relates to novel oral pharmaceutical compositions in lyophilized form, in which the dissolution and the bioavailability of the active ingredient that they contain are improved. The compositions according to the invention comprise in particular a polyvinyl acetate/polyvinylpyrrolidone copolymer. The oral lyophilisates according to the invention are particularly suitable for the production of medicaments based on active ingredients which have low solubility or very low solubility in water or which are virtually insoluble in water.

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15-11-2012 дата публикации

Rare earth nanoparticles

Номер: US20120288535A1

This document provides methods and materials related to rare earth particles such as rare earth nanorods (e.g., inorganic lanthanide hydroxide nanorods). For example, rare earth (e.g., lanthanide) particles such as europium hydroxide nanorods, methods and materials for making rare earth particles (e.g., europium hydroxide nanorods), and methods and materials for using rare earth particles (e.g., europium hydroxide nanorods) as an imaging agent and/or to promote angiogenesis are provided.

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22-11-2012 дата публикации

Device and method for combining a treatment agent and a gel

Номер: US20120296312A1
Принадлежит: Abbott Cardiovascular Systems Inc

A method including introducing a treatment agent at a treatment site within a mammalian host; and introducing a bioerodable gel material at the treatment site. An apparatus including a first annular member having a first lumen disposed about a length of the first annular member and a first entry port at a proximal end of the first annular member, and a second annular member coupled to the first annular member having a second lumen disposed about a length of the second annular member and a second entry port at a proximal end of the second annular member, wherein the first annular member and the second annular member are positioned to allow a combining of treatment agents introduced through each annular member at the treatment site.

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20-12-2012 дата публикации

Method of producing beraprost

Номер: US20120323025A1
Принадлежит: Lung LLC

An improved method is described for making single isomers of synthetic benzoprostacyclin analogue compounds, in particular the pharmacologically active 314-d isomer of beraprost. In contrast to the prior art, the method is stereoselective and requires fewer steps than the known methods for making these compounds.

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27-12-2012 дата публикации

Oral delivery of peptide pharmaceutical compositions

Номер: US20120328666A1
Принадлежит: Unigene Laboratories Inc

Bioavailability of peptide active agents to be administered orally is enhanced by a pharmaceutical composition providing targeted release of the peptide to the intestine by combining the composition with an absorption enhancer. Bioavailability is further significantly increased by administering the composition in an acid-resistant protective vehicle which transports components of the invention through the stomach. The composition may optionally further include a sufficient amount of a pH-lowering agent to lower local intestinal pH. All components are released together into the intestine with the peptide.

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03-01-2013 дата публикации

Treatment of vascularized pigment epithelial detachment with anti-vegf therapy

Номер: US20130004486A1
Принадлежит: Genentech Inc

Methods for treating vascularized pigment epithelial detachment using anti-VEGF agents are disclosed.

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03-01-2013 дата публикации

Method of treating myocardial injury

Номер: US20130005037A1
Автор: Marc S. Penn
Принадлежит: CLEVELAND CLINIC FOUNDATION

A method of treating a myocardial injury of a subject includes administering a population of at least one of mesenchymal stem cells (MSCs), multipotent adult progenitor cells (MAPCs), embryonic stem cells (ESCs), induced pluripotent stem cells (iPSs), which have down-regulated expression of disabled-2 (Dab2), to the subject.

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17-01-2013 дата публикации

Processes for the preparation of key intermediate for the synthesis of rosuvastatin or pharmaceutically acceptable salts thereof

Номер: US20130018065A1
Принадлежит: Lek Pharmaceuticals dd

The present invention relates in general to the field of organic chemistry and in particular to a process for the preparation of 5-((E)-2-((2S,4R)-4-hydroxy-6-oxotetrahydro-2H-pyran-2-yl)vinyl)-4-(4-fluorophenyl)-6-isopropyl-2-(N-methyl-methanesulfonylamino)pyrimidine (RSVL) as well as a process for preparing crystalline 5-((E)-2-((2S,4R)-4-(tert-butyldimethylsilyloxy)-6-oxotetrahydro-2H-pyran-2-yl)vinyl)-4-(4-fluorophenyl)-6-isopropyl-2-(N-methylmethanesulfonylamino)pyrimidine (RSVLTBS) useful as key intermediates for the preparation of rosuvastatin or pharmaceutically acceptable salts thereof.

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24-01-2013 дата публикации

Carboxylic acid derivatives having an oxazolo[5,4-b]pyridine ring

Номер: US20130023557A1
Принадлежит: SANOFI SA

The invention therefore relates to compounds of the formula I in which X, Y, R 1 , R 2 and R 3 have the given meanings. The compounds of the formula I are suitable, for example, for wound healing.

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07-02-2013 дата публикации

Isotopologues of 4-[9-(tetrahydro-furan-3-yl)-8-(2,4,6-trifluoro-phenylamino)-9h-purin-2-ylamino]-cyclohexan-1-ol

Номер: US20130034495A1
Принадлежит: Signal Pharmaceuticals LLC

Provided herein are isotopologues of Compound 1, which are enriched with isotopes such as, for example, deuterium. Pharmaceutical compositions comprising the isotope-enriched compounds, and methods of using such compounds are also provided.

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28-02-2013 дата публикации

Use of Gold Nanoclusters in Ameliorating Oxidate Stress and/or Aging

Номер: US20130052270A1

Disclosed herein is the novel use of a gold nanocluser for ameliorating oxidative stress and/or aging of a cultured cell or a subject having an oxidative stress and/or aging condition mediated by a vascular factor. The gold nanocluster has a particle size ranging from about 0.1 to 20 nm, and preferably is dihydrolipoic acid (DHLA) coated gold nanocluster.

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07-03-2013 дата публикации

Novel Gene And Protein Associated With Angiogenesis And Endothelial Cell Specific Apoptosis

Номер: US20130058940A1
Принадлежит: CLEVELAND CLINIC FOUNDATION

This invention provides isolated nucleic acid and amino acid sequences encoding VG5Q, a novel angiogenic growth factor protein with pro-angiogenic activity, a forkhead-associated domain, a G-patch domain; characteristic subcellular localization in an in vitro Matrigel model of angiogenesis: towards the cell periphery in early stages of tubulogenesis, between cells in newly formed endothelial tubes, and no nuclear staining after 24 hours; is expressed in endothelial cells; is secreted during angiogenesis; and interacts with TWEAK. The invention also provides for expression vectors containing nucleic acid sequences encoding VG5Q protein, and host cells containing one or more expression vectors for the recombinant expression of VG5Q. The invention also provides for methods of using VG5Q for the diagnosis and treatment of angiogenesis-mediated diseases or disorders.

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21-03-2013 дата публикации

Method for optimising gene expression using synonymous codon optimisation

Номер: US20130074218A1
Автор: Ian Hector Frazer
Принадлежит: University of Queensland UQ

The present invention discloses a method for modulating the quality of a selected phenotype that is displayed by an organism or part thereof and that results from the expression of a polypeptide-encoding polynucleotide by replacing at least one codon of that polynucleotide with a synonymous codon that has a higher or lower preference of usage by the organism or part thereof to produce the selected phenotype than the codon it replaces. The present invention is also directed to the use of a codon-modified polynucleotide so constructed for modulating the quality of a selected phenotype displayed by an organism or part thereof.

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25-04-2013 дата публикации

ANTIMICROBIAL COMPOUNDS OF 1,4-NAPHTOQUINONE STRUCTURE

Номер: US20130102650A1
Принадлежит:

The present invention relates to a compound having formula (I) wherein: Ris chosen from the group consisting of: phenyl group, possibly substituted, —CH—CH—R′group, R′being chosen from the group consisting of: H, —OH, halogen, alkyl, aryl, CHO, —CN, —NO, —SR, —OR, —NRR, —CONRR, —COOR, and —NHCOR, Rand Rrepresenting independently from each other H, an alkyl group or an aryl group, R′being preferably in para position, and —CH—CO—R′ group, R′ representing an aryl or heteroaryl group, said aryl and heteroaryl groups being possibly substituted, Ris chosen from the group consisting of: —OH and halogen, and R, R, Rand Rare in particular H, for its use for the prevention and/or the treatment of bacterial infections. 3. The compound according to claim 1 , wherein Ris a substituted or unsubstituted phenyl group.4. The compound according to claim 1 , wherein Ris a phenyl group claim 1 , substituted by an aryl group.5. The compound according to claim 1 , wherein Ris chosen from the group consisting of: —CH—CH—R′group and —CH—CO—R′ group claim 1 , R′and R′ being as defined in .7. The compound according to claim 6 , wherein R′is a group in para position having formula —OR′ claim 6 , R′being H or an alkyl group comprising from 1 to 6 carbon atoms.8. The compound according to claim 6 , wherein Ris chosen from the groups having formula —CH—CO—R′ claim 6 , R′ being as defined in .9. The compound according to claim 8 , wherein R′ is a substituted and unsubstituted aryl group.10. The compound for the use according to claim 8 , wherein R′ is a substituted or unsubstituted phenyl group.12. The compound according to claim 11 , wherein R′is a group in para position chosen from the alkyl groups comprising from 1 to 6 carbon atoms claim 11 , and the groups having formula —OR′ claim 11 , R′being chosen from H and alkyl groups comprising from 1 to 6 carbon atoms.13. The compound according to claim 1 , wherein R′ is a substituted and unsubstituted heteroaryl group.15. (canceled)16. The ...

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02-05-2013 дата публикации

Use of dabigatran etexilate for treating patients with pulmonary hypertension

Номер: US20130109722A1
Автор: Martin Feuring
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

The invention relates to a new use of dabigatran etexilate of formula I optionally in the form of the pharmaceutically acceptable salts thereof, as well as new medicament formulations which may be used for this purpose.

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09-05-2013 дата публикации

Methods for treating or preventing vascular graft failure

Номер: US20130115256A1
Принадлежит: Moerae Matrix Inc

The described invention provides pharmaceutical compositions and methods for treating or preventing vascular graft failure in a subject in need of such treatment, the method comprising administering a therapeutically effective amount of a composition comprising a polypeptide of amino acid sequence YARAAARQARAKALARQLGVAA (SEQ ID NO: 1) or a functional equivalent thereof, and a pharmaceutically acceptable carrier. The methods also are clinically useful for treating a pre-atherosclerotic intimal hyperplasia condition.

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09-05-2013 дата публикации

RFamide-Related Peptides and Methods Thereof

Номер: US20130116184A1
Принадлежит: University of Michigan

Provided herein methods and compositions directed to RFRP-1 polypeptides for modulating cardiac contractile function, for preventing and/or treating cardiac disorders.

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06-06-2013 дата публикации

(2e)-3-phenyl-n-[2,2,2-trifluoro-1-[[8-quinolineamino)thiomethyl]amino]ethyl]-2-acrylamide and pharmaceutical uses thereof

Номер: US20130143917A1
Принадлежит: CHINESE PLA GENERAL HOSPITAL

The present invention relates to an acrylamide compound of Formula I, or an isomer, pharmaceutically acceptable salt and solvate thereof, to a composition comprising the compound or an isomer, pharmaceutically acceptable salt and solvate thereof, and a pharmaceutically acceptable carrier, excipient or diluent, and to a use of the compound or the composition for prophylaxis and/or treatment of a disease or disorder associated with cardiomyocyte apoptosis

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13-06-2013 дата публикации

Method for treating mechanical allodynia comprising administration of eugenol

Номер: US20130150455A1
Принадлежит: SNU R&DB FOUNDATION

The present invention relates to a pharmaceutical composition for selectively treating mechanical allodynia, which provides eugenol or a pharmaceutically acceptable salt thereof at a concentration lower than that which would inhibit voltage-gated sodium channels (VGSCs), a pharmaceutical composition for blocking hyperpolarization-activated current (I h ), and a transdermal preparation for treating mechanical allodynia comprising the composition. Even though administered at a concentration lower than that which would inhibit VGSCs, the eugenol of the present invention inhibits I h in a cAMP or G-protein coupled receptor (GPCR) independent manner, thereby selectively ameliorating mechanical allodynia. Therefore, when the eugenol of the present invention is formulated into a transdermal preparation to be provided at a concentration lower than that which would inhibit VGSCs, and directly applied to the wound lesion, it can be used as a pharmaceutical composition capable of selectively treating mechanical allodynia.

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20-06-2013 дата публикации

Method for Production and Use of Mite Group 1 Proteins

Номер: US20130157310A1
Принадлежит: Merck Patent GmBH

The present invention includes a method to produce a recombinant mite Group 1 protein in a methyltrophic yeast or an Escherichia coli microorganism. The present invention also relates to a recombinant mite Group 1 protein obtained by such a method, such a recombinant protein being able to selectively bind IgE or cause proliferation of a T cell that proliferates in response to a native mite Group 1 protein. Also included in the present invention is the use of such a recombinant mite Group 1 protein to detect mite allergy or to reduce an allergic response to a mite Group 1 protein. The present invention also includes novel mite Group 1 nucleic acid molecules, proteins, recombinant molecules, and recombinant cells, as well as uses thereof.

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27-06-2013 дата публикации

Fc FUSION PROTEINS

Номер: US20130164286A1

The embodiments of the invention relate to compositions, methods, and kits comprising a fusion protein. The fusion proteins of the embodiments include monomer polypeptides which in one embodiment have at least a binding domain, an optional hinge region, a collagen-like domain and the Fc domain of a human IgG.

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04-07-2013 дата публикации

PLANT ACTIVATOR

Номер: US20130172189A1
Принадлежит:

A compound useful as a plant activator for activating an endogenous defense system of a plant to control disease damage is provided. A compound represented by the formula: (R)NH—(CH)—N(R)—(CH)—NH(R) (one of Rand Rrepresents a linear Calkanoyl group or alkenoyl group, the other represents hydrogen atom or a protective group of amino group; and Rrepresents hydrogen atom or a protective group of amino group). 1. A compound represented by the following general formula (I): (R)NH—(CH)—N(R)—(CH)—NH(R) (In the formula , one of Rand Rrepresents a linear alkanoyl group having 6 to 18 carbon atoms or a linear alkenoyl group having 6 to 18 carbon atoms (the linear alkanoyl group and the linear alkenoyl group may have 1 to 3 hydroxyl groups , and/or 1 to 3 alkyl groups having 1 to 4 carbon atoms) , the other represents hydrogen atom or a protective group of amino group; and Rrepresents hydrogen atom or a protective group of amino group) , or a salt thereof.2. The compound or a salt thereof according to claim 1 , wherein one of Rand Ris a linear alkanoyl group having 8 to 13 carbon atoms or a linear alkenoyl group having 8 to 13 carbon atoms (the linear alkanoyl group and the linear alkenoyl group may have 1 to 3 hydroxyl groups) claim 1 , the other is hydrogen atom or a protective group of amino group claim 1 , and Ris hydrogen atom or a protective group of amino group.3. The compound or a salt thereof according to claim 1 , wherein one Rand Ris a linear alkanoyl group having 8 to 13 carbon atoms (the linear alkanoyl group may have 1 to 3 hydroxyl groups) claim 1 , the other is hydrogen atom or a protective group of amino group claim 1 , and Ris hydrogen atom or a protective group of amino group.4. The compound or a salt thereof according to claim 1 , wherein the linear alkanoyl group is a linear alkanoyl group having 9 to 12 carbon atoms (the linear alkanoyl group may have 1 or 2 hydroxyl groups).5. The compound or a salt thereof according to claim 1 , wherein the linear ...

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25-07-2013 дата публикации

Dietary Supplement For Vascular Health

Номер: US20130189297A1

The present invention relates to an herbal dietary supplement to promote vascular health. The dietary supplement comprises L-Arginine, L-Citrulline, Ginkgo Biloba, Horse chestnut, Red Yeast Rice and Cayanne Pepper.

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25-07-2013 дата публикации

Biotinylated polysaccharides having an antithrombotic activity and improved metabolic stability

Номер: US20130190268A1
Принадлежит: SANOFI SA

The invention relates to novel polysaccharides with an antithrombotic activity, having at least one covalent bond with biotin or a biotin derivative, wherein said covalent bond is resistant to metabolic cleavage and comprises a linkage X selected from the group consisting of —O—, —N(R)—, —N(R)—CO— and —N(R′)—CO—N(R″)—, wherein R is an alkyl group and R′ and R″, which may be identical or different, are, independently of one another, a hydrogen atom or alkyl group.

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15-08-2013 дата публикации

Differentiation of pluripotent cells

Номер: US20130210141A1
Принадлежит: Fujifilm Cellular Dynamics Inc

Provided herein are methods for the in vitro maintenance, expansion, culture, and/or differentiation of pluripotent cells, such as human embryonic stem cells (hESC) or induced pluripotent cells (iPSC), into hematopoietic precursor cells or endothelial cells. The pluripotent cells may be maintained and differentiated under defined conditions; thus, the use of mouse feeder cells or serum is not required in certain embodiments for the differentiation of the pluripotent cells into hematopoietic precursor cells or endothelial cells. The resulting hematopoietic precursor cells may be further differentiated into various myeloid or lymphoid lineages.

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22-08-2013 дата публикации

Omega 3 fatty acid formulations

Номер: US20130213851A1
Принадлежит: CENESTRA LLC

The present invention provides highly purified omega-3 fatty acid formulations. Certain formulations provided herein have greater than 85% omega-3 fatty acids by weight. Certain other formulations provided herein contain EPA and DHA in a ratio of from about 4.01:1 to about 5:1. The invention also provides methods of using the dosage forms to treat a variety of cardiovascular, autoimmune, inflammatory, and central nervous system disorders by administering a formulation of the invention to a patient in need thereof.

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22-08-2013 дата публикации

Purification and isolation of recombinant oxalate degrading enzymes and spray-dried particles containing oxalate degrading enzymes

Номер: US20130216515A1
Принадлежит: OXTHERA INTELLECTUAL PROPERTY AB

The present invention comprises methods and compositions for the reduction of oxalate in humans, and methods for the purification and isolation of recombinant oxalate reducing enzyme proteins. The invention provides methods and compositions for the delivery of oxalate-reducing enzymes in particle compositions. The compositions of the present invention are suitable in methods of treatment or prevention of oxalate-related conditions.

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22-08-2013 дата публикации

Sulfinylbenzyl and thiobenzyl derivatives as sphingosine 1-phosphate (s1p) receptor modulators

Номер: US20130217652A1
Принадлежит: Allergan Inc

The present invention relates to novel thiobenzyl and sulfinylbenzyl derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.

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22-08-2013 дата публикации

CHOLINE ANALOGS AND CHEMICAL SYNTHESIS THEREOF

Номер: US20130217917A1
Принадлежит: VANDERBILT UNIVERSITY

A method of making a betaine aldehyde, comprising ozonizing an allyl trimethylammonium to form the betaine aldehyde. 1. A method of making a betaine aldehyde , comprising ozonizing an allyl trimethylammonium to form the betaine aldehyde.2. The method of claim 1 , wherein the nitrogen atom of the allyl trimethylammonium is isotopically enriched N.3. The method of claim 1 , wherein at least one of the hydrogen atoms of the allyl trimethylammonium is istopically enriched D.4. The method of claim 1 , wherein the allyl trimethylammonium is an allyl trimethylammonium chloride or an allyl trimethylammonium bromide.5. The method of claim 1 , wherein the ozonizing step comprises reacting the ally trimethylammonium with ozone to form a peroxide claim 1 , and reducing the peroxide with dimethyl sulfide to form the betaine aldehyde.6. The method of claim 1 , further comprising synthesizing the allyl trimethylammonium from a trimethylammonium and an allyl.7. The method of claim 6 , wherein the nitrogen atom of the trimethylammonium is isotopically enriched N.8. The method of claim 6 , wherein at least one of the hydrogen atoms of the trimethylammonium is istopically enriched D.9. The method of claim 6 , wherein the trimethylammonium is a trimethylammonium bromide or a trimethylammonium chloride.10. The method of claim 6 , wherein at least one of the hydrogen atoms of the allyl is isotopically enriched D. This patent application is a continuation of U.S. application Ser. No. 13/405,074 filed Feb. 24, 2012, which claims priority to U.S. Provisional Patent Application No. 61/446,391 filed Feb. 24, 2011. The entire content of each of these applications is hereby incorporate by reference.This invention was made with government support under National Institutes of Health grant numbers 1R00CA134749 and 3R00CA134749-02S1. The government has certain rights in the invention.Hyperpolarized MRI offers a sensitivity increase by 4-6 orders of magnitude as compared to conventional MRI. ...

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19-09-2013 дата публикации

Proteomic Antisense Molecular Shield and Targeting

Номер: US20130243700A1
Принадлежит: Individual

The present invention provides compositions and methods for shielding and directing agents to biological targets in cellular systems for therapeutic, prophylactic, and diagnostic uses. Vascular devices are also provided which have coated surfaces that contain proteomic antisense, as well as therapeutic and other biological agents attached thereto.

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19-09-2013 дата публикации

Injectable ibuprofen formulation

Номер: US20130245591A1
Автор: Andrew Vila, Leo Pavliv
Принадлежит: Cumberland Pharmaceuticals Inc

The present invention provides a pharmaceutical composition comprising an aqueous solution of an ibuprofen solubilizing agent and ibuprofen, the ibuprofen solubilizing agent being in an effective amount such that the ibuprofen in the solution remains soluble at concentrations from 100 mg/mL to 5 mg/mL without undergoing a phase transition. The invention further provides a method of treating a condition chosen from pain, inflammation, fever, and/or patent ductus arteriosis, comprising administering to a patient in need thereof an effective amount of an aqueous solution a ibuprofen solubilizing agent and ibuprofen, the ibuprofen solubilizing agent being in an effective amount such that the ibuprofen in the solution remains soluble at concentrations from 100 mg/mL to 5 mg/mL without undergoing a phase transition, as well as a method for manufacturing the composition.

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31-10-2013 дата публикации

POLYMORPHS OF BROMFENAC SODIUM AND METHODS FOR PREPARING BROMFENAC SODIUM POLYMORPHS

Номер: US20130289120A1
Принадлежит:

Different polymorphs of bromfenac sodium may be prepared and interconverted using crystallization/recrystallization, drying and/or hydration techniques. 1. A pharmaceutical formulation comprising a formulated crystalline form of bromfenac sodium sesquihydrate , wherein the crystalline form is characterized by a powder x-ray diffraction pattern having a main peak expressed as 2-theta at about 15.2 , and at least one excipient.2. The pharmaceutical formulation of claim 1 , wherein the pharmaceutical formulation is a liquid.3. The pharmaceutical formulation of claim 2 , wherein the liquid is a solution.4. The pharmaceutical formulation of claim 1 , wherein the pharmaceutical formulation is a suspension.5. The pharmaceutical formulation of claim 3 , wherein the formulated crystalline form of bromfenac sodium sesquihydrate is dissolved in the solution in an amount from about 0.01% to about 5% by weight.6. The pharmaceutical formulation of claim 1 , wherein the at least one excipient is selected from the group consisting of at least one of carriers claim 1 , solvents claim 1 , preservatives claim 1 , stabilizers claim 1 , surfactants claim 1 , pH adjusting agents claim 1 , diluents claim 1 , and fillers.7. The pharmaceutical formulation of claim 1 , wherein the at least one excipient comprises a water soluble polymer.8. The pharmaceutical formulation of claim 1 , wherein the at least one excipient comprises a preservative claim 1 , a chelating agent claim 1 , a pH-adjusting agent claim 1 , a water soluble polymer claim 1 , a sulfite claim 1 , a buffer system claim 1 , and water.9. The pharmaceutical formulation of claim 8 , wherein the pH-adjusting agent comprises sodium hydroxide claim 8 , the water soluble polymer comprises polyvinyl pyrrolidone claim 8 , the sulfite comprises sodium sulfite claim 8 , and the buffer system comprises boric acid and sodium borate.10. The pharmaceutical formulation of claim 9 , wherein the chelating agent comprises sodium edetate.11. The ...

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07-11-2013 дата публикации

NOVEL PHOTOINITIATORS

Номер: US20130296577A1
Принадлежит: COLOPLAST A/S

Novel photoinitiators provide for polyurethane formation, in which a photoinitiator moiety and a tertiary amine are incorporated into the photoinitiator structure, and thus the polyurethane polymer.

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07-11-2013 дата публикации

NOVEL STEREOSPECIFIC SYNTHESIS OF (-) (2S, 3S)-1-DIMETHYLAMINO-3-(3-METHOXYPHENYL)-2-METHYL PENTAN-3-OL

Номер: US20130296608A1
Принадлежит: SYMED LABS LIMITED

The present invention relates to a novel stereospecific synthesis of (−)(2S,3S)-1-dimethylamino-3-(3-methoxyphenyl)-2-methyl pentan-3-ol an intermediate in the synthesis of 3-[(1R,2R)-3-(dimethylamino)-1-ethyl-2-methylpropyl]phenol. 18-. (canceled)10. The process of wherein the solvent employed is selected from the group consisting of ethers claim 9 , halo carbonated solvents claim 9 , and esters.11. The process of wherein the ether is selected from the group consisting of tetrahydrofuran (THF) claim 10 , 1 claim 10 ,4-dioxane claim 10 , diethyl ether or mixtures thereof.12. The process of wherein the halo carbonated solvent is selected from the group consisting of methylene chloride claim 10 , ethylene dichloride claim 10 , chloroform claim 10 , chlorobenzene claim 10 , dichlorobenzene and mixtures thereof.13. The process of wherein the ester is selected from the group consisting of ethyl acetate claim 10 , isopropyl acetate claim 10 , n-butyl acetate claim 10 , tert-butyl acetate and mixtures thereof.14. The process of wherein the solvent is tetrahydrofuran.15. The process of wherein the reaction is performed at a temperature from about 0° C. to about 100° C.16. The process of wherein the reaction is performed at the boiling point of the solvent(s) used.17. The process of wherein the reaction is performed at about 25° C.18. The process of wherein the reaction is carried out at a time period from about 15 minutes to about 10 hours.19. The process of wherein the reaction is carried out at a time period from about 30 minutes to about 2 hours.20. The process of wherein the molar equivalent of the compound of formula IV and reagent used is from about 0.25 to about 7 molar equivalents on the weight of the compound of formula V.21. The process of wherein the molar equivalent of the compound of formula IV and reagent used is about 1 molar equivalent on the weight of the compound of formula V.22. The process of wherein the compound of the formula III obtained has a purity ...

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21-11-2013 дата публикации

Wnt1 for Treatment of Cardiovascular Disorders and Injuries

Номер: US20130309211A1
Автор: Arjun Deb

The present invention relates to the discovery of the role of Wnt1 in multiple cardiovascular processes, including cardiac repair, angiogenesis, and stimulation of endothelial progenitor cells. This discovery provides methods of using Wnt1 to treat cardiovascular disorders and injuries.

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21-11-2013 дата публикации

SYNTHESIS, STRUCTURE AND USE OF FUNCTIONALIZED NAPHTHALENES

Номер: US20130310558A1
Принадлежит:

Methods for the synthesis and use of functionalized, substituted naphthalenes are described. The functionalized, substituted naphthalenes display useful properties including liquid crystals and fluorescence properties, such as solvatochromatic fluorescence, with high quantum yields, Stoke's shift, and show emission maxima that are significantly red-shifted. 2. The naphthalene of claim 1 , wherein Ris —S(O)R claim 1 , —S(O)R claim 1 , P(O)(OR) claim 1 , or —C(Y)R claim 1 , Y is O or NRand Rand Rare independently H claim 1 , C-Calkyl claim 1 , C-Calkoxy claim 1 , phenyl claim 1 , or aryl claim 1 , and{'sup': 2', '6', '6', '6, 'sub': 2', '1', '20, 'each Ris Cl, —N(R), or —OR, where each Ris H, C-Calkyl, substituted or unsubstituted phenyl, or come together to form a cyclyl or heterocyclyl structure having 4-5 carbon atoms.'}3. The naphthalene of claim 2 , wherein Ris —C(Y)R claim 2 , Y is O claim 2 , and Ris H claim 2 , C-Calkyl claim 2 , C-Calkoxy claim 2 , phenyl claim 2 , or aryl.4. The naphthalene of claim 2 , wherein Ris Cl.5. The naphthalene of claim 2 , wherein Ris —N(R) claim 2 , or —OR claim 2 , where each Ris H claim 2 , C-Calkyl claim 2 , substituted or unsubstituted phenyl claim 2 , or come together to form a cyclyl or heterocyclyl structure having 4-5 carbon atoms6. The naphthalene of claim 1 , wherein the Rgroups are combined as ═O claim 1 , X is CH claim 1 , C(R) claim 1 , O claim 1 , NTs claim 1 , NH claim 1 , NCORor NR claim 1 , Ris H claim 1 , C-Calkyl claim 1 , C-Calkoxy claim 1 , phenyl claim 1 , aryl claim 1 , or heteroaryl claim 1 , and{'sup': 2', '6', '6', '6, 'sub': 2', '1', '20, 'each Ris Cl, —N(R), or —OR, where each Ris H, C-Calkyl, substituted or unsubstituted phenyl, or come together to form a cyclyl or heterocyclyl structure having 4-5 carbon atoms.'}8. The naphthalene of claim 1 , wherein the naphthalene is a fluorophore.9. The naphthalene of claim 8 , where the naphthalene has a fluorescent emission maximum at a wavelength of from 450 nm ...

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28-11-2013 дата публикации

Methods and pharmaceutical compositions for the treatment of heart failure

Номер: US20130315932A1
Автор: Frédéric JAISSER

The present invention relates to an inhibitor of NGAL gene expression or a NGAL antagonist for use in the prevention or the treatment of heart failure.

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28-11-2013 дата публикации

Novel crystalline forms

Номер: US20130316982A1
Принадлежит: Thar Pharmaceuticals Inc

Preparation and characterization of novel forms of (1-hydroxy-2-imidazol-1-yl-1-phosphono-ethyl) phosphonic acid, suitable for pharmaceutical compositions in drug delivery systems for humans.

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19-12-2013 дата публикации

Abuse-Deterrent Methadone for the Safe Treatment of Drug Abuse and Pain Relief

Номер: US20130338229A1
Принадлежит: Pisgah National Laboratories, Inc.

Provided is a drug substance and a method of treating an ailment comprising administering an oral dose of a drug product comprising the drug substance wherein the drug substance comprises an organic acid addition salt of methadone. The organic acid addition salt is selected from the group consisting of pamoate and xinafoate wherein the drug substance is bioavailable under gastrointestinal administration but is not bioavailable under administration at a mucosal membrane other than gastrointestinal or release from a depot injectable product. 1. A drug substance comprising an organic acid addition salt of methadone wherein said organic acid addition salt is selected from the group consisting of pamoate and xinafoate.2. The drug substance of wherein said organic acid addition salt is pamoate.3. The drug substance of wherein said drug substance is methadone pamoate 2:1.4. The drug substance of wherein said methadone pamoate 2:1 is amorphous.5. The drug substance of wherein said amorphous methadone pamoate is characterized by at least one method selected from the group consisting of:{'figref': {'@idref': 'DRAWINGS', 'FIG. 5'}, 'a differential scanning calorimetry thermogram of indicating a phase transition of at least 0.4 W/g at 225-275° C.;'}{'figref': {'@idref': 'DRAWINGS', 'FIG. 6'}, 'a fourier transform infrared spectrum of ; and'}{'figref': {'@idref': 'DRAWINGS', 'FIG. 7'}, 'a powder x-ray diffraction diffractogram of .'}6. The drug substance of wherein said drug substance is methadone pamoate 1:1.7. The drug substance of wherein said methadone pamoate 1:1 is polymorphic.8. The drug substance of wherein said polymorphic methadone pamoate is characterized by at least one method selected from the group consisting of:{'figref': {'@idref': 'DRAWINGS', 'FIG. 9'}, 'a differential scanning calorimetry thermogram of indicating a phase transition of at least 1.5 W/g at 200-230° C. and a phase transition of at least 1.0 W/g at 240-260° C.;'}{'figref': {'@idref': 'DRAWINGS', ' ...

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26-12-2013 дата публикации

TREATMENT OF MITOCHONDRIAL DISEASES WITH NAPHTHOQUINONES

Номер: US20130345312A1
Принадлежит:

Methods of treating, preventing or suppressing symptoms associated with mitochondrial diseases, such as Friedreich's ataxia (FRDA), Leber's Hereditary Optic Neuropathy (LHON), dominant optic atrophy (DOA); mitochondrial myopathy, encephalopathy, lactacidosis, stroke (MELAS), Leigh syndrome or Kearns-Sayre Syndrome (KSS) with compounds of Formula (I) are disclosed. Methods of modulating, normalizing, or enhancing energy biomarkers, as well as compounds useful for such methods are also disclosed. 3. The method according to claim 1 , wherein R claim 1 , Rand Rare independently selected from —(C-C)alkyl.4. The method according to claim 1 , wherein Rand Rare hydrogen and Ris —(C-C)alkyl.5. The method according to claim 1 , wherein Rand Rare independently of each other —O(C-C)alkyl and Ris —(C-C)alkyl.7. The method according to claim 6 , wherein R claim 6 , Rand Rare independently of each other —(C-C)alkyl.8. The method according to claim 6 , wherein Rand Rare —O(C-C)alkyl and Ris —(C-C)alkyl.9. The method according to claim 6 , wherein the bond indicated by a dashed line is a double bond.10. The method according to claim 6 , wherein the bond indicated by a dashed line is a single bond.12. The method according to claim 11 , wherein R claim 11 , Rand Rare independently of each other —(C-C)alkyl.13. The method according to claim 11 , wherein Rand Rare hydrogen and Ris —(C-C)alkyl.14. The method according to claim 11 , wherein Rand Rare —O(C-C)alkyl and Ris —(C-C)alkyl.15. The method according to claim 11 , wherein the bond indicated by a dashed line is a double bond.16. The method according to claim 11 , wherein the m′ is 3.17. The method according to claim 11 , wherein the compound is selected from:2-(3-hydroxy-3,7,11,15-tetramethylhexadeca-6,10,14-trien-1-yl)-3-methylnaphthalene-1,4-dione;2-(3-hydroxy-3,7,11,15-tetramethylhexadeca-6,10,14-trien-1-yl)naphthalene-1,4-dione; and any stereoisomer, mixture of stereoisomers, salt, crystalline form, non-crystalline form, hydrate ...

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09-01-2014 дата публикации

POLYMORPHS OF BROMFENAC SODIUM AND METHODS FOR PREPARING BROMFENAC SODIUM POLYMORPHS

Номер: US20140011880A1
Принадлежит: JOHNSON MATTHEY PUBLIC LIMITED COMPANY

Different polymorphs of bromfenac sodium may be prepared and interconverted using crystallization/recrystallization, drying and/or hydration techniques. 1. Bromfenac sodium , characterized by a powder x-ray diffraction pattern having a main peak expressed as 2-theta at about 20.7 degrees.2. Bromfenac sodium in accordance with claim 1 , characterized by a powder x-ray diffraction pattern having additional main peaks expressed as 2-theta at about 18.5 claim 1 , 34.1 claim 1 , and 16.5.3. Bromfenac sodium in accordance with claim 1 , characterized by a powder x-ray diffraction pattern having additional main peaks expressed as 2-theta at about 11.3 claim 1 , 14.4 claim 1 , 17.3 claim 1 , 19.4 claim 1 , 21.0 claim 1 , 22.7 claim 1 , 29.0 claim 1 , 31.8 claim 1 , and 36.1.4. Bromfenac sodium in accordance with claim 1 , characterized by a powder x-ray diffraction pattern exhibiting main peaks substantially in accordance with those shown in .5. Bromfenac sodium in accordance with claim 1 , characterized by an XRPD d-spacing/% intensity pattern substantially in accordance with that shown in Table D.6. A method for converting bromfenac sodium Form I into bromfenac sodium Form II claim 1 , comprising drying bromfenac sodium Form I under vacuum.7. A method for converting bromfenac sodium Form II into bromfenac sodium Form I claim 1 , comprising hydrating the bromfenac sodium Form II.8. The method of claim 7 , where hydrating is accomplished either under vacuum with a wet nitrogen bleed or at atmospheric pressure using a moist atmosphere within an enclosure.9. A method for converting bromfenac sodium Form III into bromfenac sodium Form II claim 7 , comprising crystallizing or recrystallizing bromfenac sodium Form III from a solvent mixture comprised of water claim 7 , at least one dialkoxyalkane claim 7 , and at least one anti-solvent to obtain an intermediate product and drying the intermediate product under vacuum.10. A pharmaceutical formulation comprising a formulated ...

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16-01-2014 дата публикации

POLYMORPHS OF BROMFENAC SODIUM AND METHODS FOR PREPARING BROMFENAC SODIUM POLYMORPHS

Номер: US20140018428A1
Принадлежит: JOHNSON MATTHEY PUBLIC LIMITED COMPANY

Different polymorphs of bromfenac sodium may be prepared and interconverted using crystallization/recrystallization, drying and/or hydration techniques. 1. Bromfenac sodium Form III , characterized by a powder x-ray diffraction pattern having a main peak expressed as 2-theta at about 21.6 degrees.2. Bromfenac sodium Form III in accordance with claim 1 , characterized by a powder x-ray diffraction pattern having additional main peaks expressed as 2-theta at about 22.4 claim 1 , 12.2 claim 1 , 24.0 and 26.3 degrees.3. Bromfenac sodium Form III in accordance with claim 1 , characterized by a powder x-ray diffraction pattern having additional main peaks expressed as 2-theta at about 12.4 claim 1 , 14.1 claim 1 , 17.8 claim 1 , 19.6 claim 1 , and 28.1 degrees.4. Bromfenac sodium Form III in accordance with claim 1 , substantially free of any other physical forms of bromfenac sodium.5. Bromfenac sodium Form III in accordance with claim 1 , characterized by a powder x-ray diffraction pattern substantially in accordance with that shown in FIG.6. Bromfenac sodium Form III in accordance with claim 1 , characterized by an FT-IR spectrum substantially in accordance with that shown in .7. Bromfenac sodium Form III in accordance with claim 1 , characterized by an XRPD d-spacing/% intensity pattern substantially in accordance with that shown in Table B.8. A method of preparing bromfenac sodium Form III claim 1 , comprising crystallizing or recrystallizing bromfenac sodium from a solvent mixture comprising water and at least one alcohol.9. The method of claim 8 , wherein the at least one alcohol includes at least one C-Calcohol.10. The method of claim 8 , wherein the bromfenac sodium has been produced by hydrolysis of 7-(4-bromobenzoyl)indol-2-one and the solvent mixture is additionally comprised of at least one aromatic hydrocarbon and at least one anti-solvent.11. The method of claim 8 , wherein the solvent mixture is comprised of water and 2-propanol or is comprised of water ...

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16-01-2014 дата публикации

DEUTERIUM-ENRICHED BUPROPION

Номер: US20140018436A1
Автор: Czarnik Anthony W.
Принадлежит: DEUTERX, LLC

The present application describes deuterium-enriched bupropion, pharmaceutically acceptable salt forms thereof, and methods of treating using the same. 2. The compound of claim 1 , wherein the compound is a compound of Formula I.5. The compound of claim 1 , wherein the compound is a compound of Formula II.8. A pharmaceutical composition comprising a compound of and a pharmaceutically acceptable carrier.9. A pharmaceutical composition comprising a compound of and a pharmaceutically acceptable carrier.10. A pharmaceutical composition comprising a compound of and a pharmaceutically acceptable carrier.11. A pharmaceutical composition comprising a compound of and a pharmaceutically acceptable carrier.12. A pharmaceutical composition comprising a compound of and a pharmaceutically acceptable carrier.13. A method of treating depression claim 1 , comprising administering a therapeutically effective amount of a compound of to a patient in need thereof to treat the depression.14. A method of treating depression claim 2 , comprising administering a therapeutically effective amount of a compound of to a patient in need thereof to treat the depression.15. A method of treating depression claim 3 , comprising administering a therapeutically effective amount of a compound of to a patient in need thereof to treat the depression.16. A method of treating depression claim 5 , comprising administering a therapeutically effective amount of a compound of to a patient in need thereof to treat the depression.17. A method of treating depression claim 6 , comprising administering a therapeutically effective amount of a compound of to a patient in need thereof to treat the depression.18. A method of treating a patient in need of smoking cessation claim 1 , comprising administering a therapeutically effective amount of a compound of to a patient in need thereof to ameliorate smoking by the patient.19. A method of treating a patient in need of smoking cessation claim 2 , comprising administering ...

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13-02-2014 дата публикации

Procollagen carboxy-terminal propeptides as a target and treatment for angiogenesis related diseases

Номер: US20140044736A1
Принадлежит: JOHNS HOPKINS UNIVERSITY

The present invention relates to the field of angiogenesis. More specifically, the present invention provides methods and compositions for modulating angiogenesis. In a specific embodiment, a method for modulating a blood vessel in a subject in need thereof comprising contacting a cell of the subject with a procollagen carboxy-terminal propeptide, a biologically active fragment or mimetic thereof, thereby modulating the blood vessel.

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27-02-2014 дата публикации

Pharmaceutical composition for treating cardiovascular and cerebrovascular diseases and method of manufacturing the same

Номер: US20140057860A1
Принадлежит: Macau Univ of Science and Technology

The present invention relates to a pharmaceutical composition for treating cardiovascular and cerebrovascular diseases and the method of preparation thereof. The aforesaid pharmaceutical composition is prepared by the following components in weight percent: 0.1%-0.3% scutellarin, 20%-25% co-surfactant, 40-50% surfactant, and 25-30% oil. The method of preparing the aforesaid pharmaceutical composition comprises the steps of: (1) dispersing scutellarin in co-surfactant and surfactant to obtain a mixture; (2) dispersing the mixture from step (1) in oil, and thermostatically and magnetically stirring the dispersion mixture under the temperature of 25° C. to 37° C., such that the components thereof are completely dissolved to obtain the pharmaceutical composition. Through the use of the selected pharmaceutical adjuvants having the ability to inhibit MRP2, the aforesaid pharmaceutical composition effectively improves absorption and bioavailability of scutellarin. The preparation of the aforesaid pharmaceutical composition is simple and convenient, and the pharmaceutical composition can be processed into a variety of dosage forms for oral administration.

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13-03-2014 дата публикации

PROCESS FOR THE PREPARATION OF A STABLE POLYMORPHIC FORM OF ATOVAGUONE

Номер: US20140073816A1
Принадлежит: TARO PHARMACEUTICAL INDUSTRIES LIMITED

The present invention provides a process for the preparation of a stable polymorph III of Atovaquone exhibiting characteristic peaks (expressed in degrees 2θ±0.2°θ) at about 6.9, 9.6, 14.1, 14.7, 17.0, 18.5, 19.1, 19.9, 20.3, 22.0, 22.6, 23.2, 24.2, 26.8, and 28.5, which comprises: (a) providing a sample of Atovaquone particles; (b) heating the sample of Atovaquone particles at a minimal temperature of between 140° C. to 160° C. depending on the particle size of the sample; and (c) cooling the sample to obtain the stable polymorphic form of Atovaquone. 1. A process for the preparation of a stable polymorph III of Atovaquone which comprises:(a) providing a sample of Atovaquone particles;(b) heating the sample of Atovaquone particles of step (a) at a temperature of at least about 160′C for a time sufficient of at least about one hour to obtain a stable polymorphic faun of Atovaquone, having characteristic peaks (expressed in degrees 20±0.2°θ) at approximately one or more of the positions: about 6.9, 9.6, 14.1, 14.7, 17.0, 18.5, 19.1, 19.9, 20.3, 22.0, 22.6, 23.2, 24.2, 26.8, and 28.5; and(c) cooling the sample of step (b).2. A process for the preparation of a stable polymorph III of Atovaquone which comprises:(a) providing a sample of Atovaquone particles wherein at least about 90% of the Atovaquone particles have a volume diameter of equal or less than about 40μ;(b) heating the sample of Atovaquone particles of step (a) at a temperature of at least about 140′C for a time sufficient to obtain a stable polymorphic form of Atovaquone, having characteristic peaks (expressed in degrees 20±0.2°θ) at approximately one or more of the positions: about 6.9, 9.6, 14.1, 14.7, 17.0, 18.5, 19.1, 19.9, 20.3, 22.0, 22.6, 23.2, 24.2, 26.8, and 28.5; and(c) cooling the sample of step (b).3. The process of claim 1 , wherein the Atovaquone particles of step (c) are further micronized if non-micronized particles are used in step (a) claim 1 , to obtain Atovaquone particles having ...

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20-03-2014 дата публикации

Preventive agent for vasculitis

Номер: US20140079695A1
Принадлежит: Chugai Pharmaceutical Co Ltd

To provide a preventive and/or therapeutic agent for vasculitis such as polyarteritis nodosa, the aortitis syndrome, and a vasculitis that is associated with immunological abnormalities, said agent comprising an interleukin-6 (IL-6) antagonist as an active ingredient.

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27-03-2014 дата публикации

Induction of human embryonic stem cell derived cardiac pacemaker or chamber-type cardiomyocytes by manipulation of neuregulin signaling

Номер: US20140087460A1
Принадлежит: UNIVERSITY OF WASHINGTON

The present invention is directed to methods of producing cardiomyocytes having a nodal/pacemaker phenotype and cardiomyocytes having an atrial/ventricular phenotype. Isolated populations of nodal/pacemaker and atrial/ventricular cardiomyocytes are also disclosed. Methods of treating a subject having cardiac arrhythmia and a subject in need of cardiac tissue repair using the isolated populations of nodal/pacemaker cardiomyocytes and atrial/ventricular cardiomyocytes, receptively, are also disclosed.

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27-03-2014 дата публикации

USE OF 3-CARBOXY-N-ETHYL-N,N-DIMETHYLPROPAN-1-AMINIUM SALTS IN THE TREATMENT OF CARDIOVASCULAR DISEASE

Номер: US20140088125A1
Принадлежит: JSC GRINDEKS

Salts of 3-carboxy-N-ethyl-N,N-dimethylpropan-1-aminium, method of preparation thereof and use in the treatment of cardiovascular disease. 19-. (canceled)14. A process for preparing the 3-carboxy-N-ethyl-N claim 10 ,N-dimethylpropan-1-aminium salt according to claim 10 , comprising:a. adding N,N-dimethylethylamine to ethyl 4-bromobutanoate in appropriate solvent to obtain 4-ethoxy-N-ethyl-N,N-dimethyl-4-oxo-1-butanaminium bromide;b. passing 4-ethoxy-N-ethyl-N,N-dimethyl-4-oxo-1-butanaminium bromide through ion exchange resin column to obtain 4-[ethyl(dimethyl)ammonio] butanoate;c. adding acid selected from the group, consisting of fumaric acid, orotic acid and phosphoric acid in appropriate solvent to obtain the corresponding 3-carboxy-N-ethyl-N,N-dimethylpropan-1-aminium salt.15. The process according to claim 14 , wherein in step a) the appropriate solvent is acetonitrile or acetone.16. A method for treating cardiovascular diseases in a subject in need thereof claim 10 , comprising administration of an effective amount of the 3-carboxy-N-ethyl-N claim 10 ,N-dimethylpropan-1-aminium salt of .17. The method according to claim 16 , wherein the cardiovascular disease is ischemic heart disease.18. The method according to claim 16 , wherein wherein the ischemic heart disease is myocardial infarction. The present invention relates to new compound 3-carboxy-N-ethyl-N,N-dimethylpropan-1-aminium salts, and to a method of preparation thereof (compound of formula 4)The present invention relates also to use of 3-carboxy-N-ethyl-N,N-dimethylpropan-1-aminium salts in the treatment of cardiovascular disease.Cardiovascular diseases (CVDs) are a group of disorders of the heart and blood vessels.An estimated 16.7 million—or 29.2% of total global deaths—result from the various forms of cardiovascular disease (CVD).Myocardial infarction (heart attack) is a serious result of coronary artery disease.Myocardial infarction (MI) is the irreversible necrosis of heart muscle secondary to ...

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03-04-2014 дата публикации

Antagonist for (pro)renin receptor for the treatment of hypertension and diabetes

Номер: US20140094409A1
Автор: Yumei FENG
Принадлежит: Individual

Brain prorenin and the (pro)renin receptor (PRR) have a functional role in the development of hypertension. The present disclosure presents functional PRR antagonistic peptides (e.g., PR10, PR20, PR30, and PR40). In addition, modified peptides comprising one or more thioether-bridges that are stable and strong PRR antagonists are also provided. Methods for treating and preventing hypertension, including neurogenic hypertension, and diabetes with a PRR antagonist are also provided.

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10-04-2014 дата публикации

Modulating innate immune cell activity by lunasin and selected cytokines

Номер: US20140099282A1
Автор: Hua-Chen Chang
Принадлежит: Hua-Chen Chang

This disclosure provides compositions and methods for enhancing innate immune system activities and responses by combining lunasin with at least one cytokine. The compositions synergistically enhance the effect of these selected cytokine(s), including but not limited to, activating NK cells, augmenting NK's cytotoxicity against vinises and tumors, regulating NK-mediated anti-allergic inflammation, producing potent NK cells for cellular therapy using adoptive transfer, and facilitating dendritic cells antigen presentation.

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10-04-2014 дата публикации

Methods for the prevention or treatment of heart failure

Номер: US20140100166A1
Принадлежит: CORNELL UNIVERSITY, UNIVERSITY OF WASHINGTON

The disclosure provides methods of preventing or treating heart failure in a mammalian subject. The methods comprise administering to the subject an effective amount of an aromatic-cationic peptide to subjects in need thereof.

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07-01-2021 дата публикации

METHOD OF PROVIDING CELIPROLOL THERAPY TO A PATIENT

Номер: US20210000770A1
Автор: Frank Michael
Принадлежит:

The present disclosure relates to the field of treatment of an orphan disease, in particular treatment of vascular Ehlers-Danlos syndrome (vEDS). More specifically, the present disclosure relates to novel up-titration dosage regimens (e.g., escalating dosage regimens) effective for treating vEDS patients with celiprolol. 1. A method for treating vascular Ehlers-Danlos syndrome , comprising administering to a patient in need thereof a 80 to 100 mg daily dose of celiprolol , or an equivalent amount of a pharmaceutically acceptable salt thereof , and increasing the daily dose to 360 to 440 mg within six months.2. The method of claim 1 , wherein at least a 80 to 100 mg daily dose increase is made within two months.3. The method of claim 1 , wherein at least a 170 to 210 mg daily dose increase is made within four months.4. The method of claim 1 , wherein at least a 260 to 310 mg daily dose increase is made within six months.5. The method of claim 1 , wherein at least a 260 to 310 mg daily dose increase is made within four months.6. A method for treating vascular Ehlers-Danlos syndrome claim 1 , comprising administering to a patient in need thereof an initial daily dose of about 91.25 mg celiprolol claim 1 , or an equivalent amount of a pharmaceutically acceptable salt thereof claim 1 , for about 1 month claim 1 , followed by administering to the patient a second daily dose of about 182.5 mg celiprolol claim 1 , or an equivalent amount of a pharmaceutically acceptable salt thereof claim 1 , for about 1 month claim 1 , followed by administering to the patient a third daily dose of about 273.75 mg celiprolol claim 1 , or an equivalent amount of a pharmaceutically acceptable salt thereof claim 1 , for about 1 month claim 1 , followed by administering to the patient a fourth daily dose of about 365 mg celiprolol claim 1 , or an equivalent amount of a pharmaceutically acceptable salt thereof.7. The method of claim 6 , wherein the second daily dose is administered twice daily.8 ...

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07-01-2021 дата публикации

METHODS FOR REDUCING OR PREVENTING CARDIOVASCULAR EVENTS IN PATIENTS WITH TYPE II DIABETES MELLITUS

Номер: US20210000792A1
Принадлежит:

The present invention is directed to methods for reducing, preventing or slowing the progression of cardiovascular risk factors and/or cardiovascular disease, comprising administration of canagliflozin. 1. A method for reducing or preventing one or more cardiovascular events , each cardiovascular event independently selected from the group consisting of cardiovascular hospitalization , non-fatal myocardial infarction , non-fatal ischemia or stroke , and cardiovascular mortality , comprising administering to a patient in need thereof , a therapeutically effective amount of canagliflozin;wherein the patient in need thereof is a patient diagnosed with Type II diabetes mellitus; and wherein the patient further exhibits symptoms of or is diagnosed with one or more concomitant or comorbid cardiovascular risk factors or cardiovascular disease.2. A method for reducing or preventing one or more major adverse cardiovascular events (MACE) , each major adverse cardiac event independently selected from the group consisting of cardiovascular death , non-fatal myocardial infarction , cardiac arrhythmia , and non-fatal stroke , comprising administering to a patient in need thereof a therapeutically effective amount of canagliflozin;wherein the patient in need thereof is a patient diagnosed with Type II diabetes mellitus; and wherein the patient further exhibits symptoms of or is diagnosed with one or more concomitant or comorbid cardiovascular risk factors or cardiovascular disease.3. A method as in claim 1 , wherein the patient diagnosed with Type II diabetes mellitus has a measured HbA1c in the range of ≥7.0% and ≤10.5%.4. A method as in claim 1 , wherein the patient is further diagnosed with microalbuminuria or macroalbuminuria.5. A method as in claim 1 , wherein the one or more cardiovascular risk factor is selected from the group consisting of obesity claim 1 , hypertension claim 1 , hyperlipidemia claim 1 , elevated triglycerides claim 1 , microalbuminuria and ...

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03-01-2019 дата публикации

Application of anthocyanin extract in preparing pharmaceutical composition for preventing and treating cardiac toxicity induced by Anthracyclines and pharmaceutical composition

Номер: US20190000900A1
Принадлежит:

The disclosure provides an application of an anthocyanin extract in preparing a pharmaceutical composition for preventing and treating cardiac toxicity induced by Anthracyclines and the pharmaceutical composition, wherein the pharmaceutical composition comprises an effective dose of the anthocyanin extract; and the anthocyanin extract refers to an extract obtained from mature fruits of a zygophyllaceous plant and having a total anthocyanin content greater than 700 mg CGE/g and a total antioxidant capacity greater than 200 mg TE/g. Cytobiology and molecular biology studies prove that the anthocyanin extract has obvious protection effect to cardiomyocyte toxicity damage induced by anthracyclines and may be used for preventing and alleviating cardiotoxicity of an antharcyclines anticancer drug, thereby expanding a clinical application of the antharcyclines anticancer drug and relieving toxic and side effects brought by the antharcyclines anticancer drug to a patient and pain of a chemotherapy patient. And additionally, the raw material sources for the anthocyanin extract are wide, the cost is low and the use is safe. 1nitraria. A pharmaceutical composition for preventing and treating cardiac toxicity induced by Anthracyclines , wherein the pharmaceutical composition comprises an effective dose of an anthocyanin extract; and the anthocyanin extract refers to an extract obtained from mature fruits of a zygophyllaceous plant and having a total anthocyanin content greater than 700 mg CGE/g and a total antioxidant capacity greater than 200 mg TE/g.2. The pharmaceutical composition according to claim 1 , wherein an anthocyanidin as a source of the anthocyanin extract comprises cyanidin claim 1 , delphinidin claim 1 , malvidin claim 1 , pelargonidin claim 1 , peonidin and petunidin.3. The pharmaceutical composition according to claim 2 , wherein the anthocyanin extract comprises six or more selected from groups composed of cyanidin-3-O-diglucoside claim 2 , cyanidin-3-O- ...

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03-01-2019 дата публикации

NOVEL BISPHOSPHONIC ACID COMPOUND

Номер: US20190002482A1
Принадлежит: FUJIYAKUHIN CO., LTD.

It is intended to provide a novel bisphosphonic acid compound or a salt thereof which shows a remarkable inhibitory effect on ectopic calcification, and a pharmaceutical composition comprising the same. The present invention provides a bisphosphonic acid compound represented by the following formula (1) or a pharmaceutically acceptable salt thereof: 2: The bisphosphonic acid compound according to or a pharmaceutically acceptable salt thereof claim 1 ,{'img': {'@id': 'CUSTOM-CHARACTER-00009', '@he': '2.46mm', '@wi': '6.01mm', '@file': 'US20190002482A1-20190103-P00001.TIF', '@alt': 'custom-character', '@img-content': 'character', '@img-format': 'tif'}, 'wherein is a single bond.'}3: The bisphosphonic acid compound according to or a pharmaceutically acceptable salt thereof claim 1 ,{'sub': 3-8', '3-8', '1-6', '1-6', '6-10, 'wherein A is a Csaturated cyclic hydrocarbon or a Csaturated heterocyclic ring comprising a sulfur atom or an oxygen atom, wherein the saturated cyclic hydrocarbon or the saturated heterocyclic ring is optionally substituted by 1 to 4 groups selected from the group consisting of a Calkyl group, a Calkoxy group, a Caryloxy group and a halogen atom.'}4: The bisphosphonic acid compound according to or a pharmaceutically acceptable salt thereof claim 1 ,{'sup': 1', '2, 'sub': '1-6', 'wherein Rand Rare each independently a Calkyl group, a halogen atom or a hydrogen atom.'}5: A pharmaceutical composition claim 1 , comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'the bisphosohonic acid compound according to or a salt thereof.'}6: A prophylactic drug for a disease associated with ectopic calcification claim 1 , the prophylactic drug comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'the bisphosphonic acid compound according to or a salt thereof as an active ingredient.'}7: A method for producing a prophylactic drug for a disease associated with ectopic calcification claim 1 , the method comprising:{'claim-ref': {'@idref': 'CLM-00001 ...

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03-01-2019 дата публикации

NOVEL CRYSTALLINE FORMS

Номер: US20190002483A1
Принадлежит: Grünenthal GmbH

Preparation and characterization of novel forms of (1-hydroxy-2-imidazol-1-yl-1-phosphono-ethyl) phosphonic acid, suitable for pharmaceutical compositions in drug delivery systems for humans. 1. A crystalline form of zoledronic acid , DL-lysine , having substantially the same PXRD diffractogram as ; or having substantially the same PXRD diffractogram as .2. The crystalline form of claim 1 , further comprising additional excess of cocrystal formers.3. The crystalline form of claim 2 , wherein the excess cocrystal formers consist of standard amino acids.4. A composition comprising a crystalline form of .5. A pharmaceutical composition comprising the crystalline form of and at least one pharmaceutically acceptable carrier.6. The pharmaceutical composition of claim 5 , wherein the pharmaceutical composition is a solid oral composition.7. The pharmaceutical composition of claim 6 , wherein the solid oral composition is a tablet or capsule.8. The pharmaceutical composition of claim 5 , wherein the pharmaceutical composition is a unit dose.9. A method of treating or preventing a disease for which zoledronic acid is indicated claim 5 , said method comprising the step of administering to a patient in need thereof a therapeutically effective amount of a pharmaceutical composition of .10. The method of claim 9 , wherein said disease is selected from the group consisting of osteoporosis claim 9 , hypercalcemia claim 9 , cancer induced bone metastasis claim 9 , Paget's disease claim 9 , adjuvant cancer therapy and neoadjuvant cancer therapy.11. The method of claim 10 , wherein said hypercalcemia is tumor induced hypercalcemia (TIH).12. The method of claim 10 , wherein said disease is cancer induced bone metastasis.13. A method of making the crystalline form of claim 1 , comprising the steps of: dissolving a zoledronic acid:DL-lysine water complex in acetic acid; forming zoledronic acid:DL-lysine crystals; and purifying said zoledronic acid:DL-lysine crystals from said acetic ...

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05-01-2017 дата публикации

ASSAY FOR METHOXETAMINE

Номер: US20170003308A1
Принадлежит:

Components for enabling immunodetection of methoxetamine are described including immunogens, haptens, antibodies and kits. 2. The immunogen of wherein:X is —NH—;{'sub': 2', 'n′, 'crosslinker is —(CH)—C(O)—; and'}n′ is 1-5.3. The immunogen of wherein:n′ is 5.4. An antibody raisable against the immunogen of .5. The antibody of which has <5% competitive cross-reactivity to any one of ketamine claim 4 , norketamine claim 4 , tramadol and tilidine compared with a 100% competitive cross-reactivity to methoxetamine.6. The antibody of which has an ICof <10 ng/ml for methoxetamine.7. The antibody of wherein the tracer is N-(5-carboxypentyl)-N-desethylmethoxetamine-HRP.8. The antibody of claim 4 , which has been purified.11. The antibody of which has <5% competitive cross-reactivity to any one of ketamine claim 9 , norketamine claim 9 , tramadol and tilidine compared with a 100% competitive cross-reactivity to methoxetamine.12. The antibody of wherein the tracer is N-(5-carboxypentyl)-N-desethylmethoxetamine-HRP.13. The antibody of claim 9 , which has been purified.14. A method of detecting or determining methoxetamine in a sample comprising:{'claim-ref': {'@idref': 'CLM-00004', 'claim 4'}, 'i) acting the sample with a detecting agent and an antibody of ; and'}ii) detecting or determining the amount of detecting agent bound to the antibody.16. The method of claim 15 , wherein the detectable label is horseradish peroxidase (HRP).17. The method of claim 16 , wherein the presence of the detectable label is detected or determined by a colour change in response to reaction of the labelling agent with a substrate.18. The method of claim 17 , wherein the colour change is detected or determined by reading the absorbance at 450 nm.19. A kit comprising an antibody of and optionally a detecting agent. The instant application claims the benefit of priority under 35 USC §119 to United Kingdom Application No. 1511725.2, entitled “Assay” filed 3 Jul. 2015, the entire contents of which are ...

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13-01-2022 дата публикации

THERAPEUTIC, PREVENTIVE, OR IMPROVEMENT AGENT FOR INFLAMMATORY DISEASE AND ALLERGIC DISEASE

Номер: US20220008435A1
Принадлежит:

An object of the present invention is to provide a novel agent for treating, preventing or improving an inflammatory disease or an allergic disease. The present invention provides an agent for treating, preventing or improving an allergic disease, or as an agent for treating, preventing or improving an inflammatory disease or an allergic disease, comprising, as an active ingredient, (±) 5,6-dihydroxy-8Z,11Z,14Z,17Z-eicosatetraenoic acid (5,6-DiHETE). The inflammatory disease can be an inflammatory disease due to an increase of calcium concentration in vascular endothelial cells, and the inflammatory disease can be an inflammatory disease developed in a tissue or organ selected from the group consisting of digestive organs, circulatory organs, respiratory organs, urinary organs, genital organs, brain, skin, eyes, and fat. 115.-. (canceled)16. A method for treating , preventing , or improving an inflammatory disease , comprising administering an effective amount of (±) 5 ,6-dihydroxy-8Z ,11Z ,14Z ,17Z-eicosatetraenoic acid (5 ,6-DiHETE) or a composition comprising the (±) 5 ,6-dihydroxy-8Z ,11Z ,14Z ,17Z-eicosatetraenoic acid (5 ,6-DiHETE) to a subject in need thereof.17. A method for treating , preventing , or improving an allergic disease , comprising administering an effective amount of (±) 5 ,6-dihydroxy-8Z ,11Z ,14Z ,17Z-eicosatetraenoic acid (5 ,6-DiHETE) or a composition comprising the (±) 5 ,6-dihydroxy-8Z ,11Z ,14Z ,17Z-eicosatetraenoic acid (5 ,6-DiHETE) to a subject in need thereof.1819.-. (canceled)20. The method according to claim 16 , wherein the inflammatory disease is an inflammatory disease due to an increase in calcium concentration of vascular endothelial cells.21. The method according to claim 16 , wherein the inflammatory disease is an inflammatory disease developed in a tissue or organ selected from the group consisting of digestive organs claim 16 , circulatory organs claim 16 , respiratory organs claim 16 , urinary organs claim 16 , genital ...

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13-01-2022 дата публикации

Treatment for Giant Cell Arteritis

Номер: US20220010007A1
Автор: Gandhi Rohan, Paolini John
Принадлежит:

The present invention provides, among other things, methods of treating giant cell arteritis, comprising a step of administering to a subject in need of treatment a GM-CSF antagonist (e.g., an anti-GM-CSFRα antibody or an anti-GM-CSF antibody) at a therapeutically effective dose and an administration interval for a treatment period sufficient to improve, stabilize or reduce one or more symptoms of giant cell arteritis relative to a control. 1. A method of treating giant cell arteritis (GCA) , comprising administering to a subject in need of treatment a composition comprising a granulocyte-macrophage colony-stimulating factor (GM-CSF) antagonist.2. The method of claim 1 , wherein the GM-CSF antagonist is a GM-CSF receptor antagonist.3. The method of wherein the GM-CSF receptor antagonist is an antibody specific for human GM-CSFRα.4. The method of claim 3 , wherein the anti-GM-CSFRα antibody is mavrilimumab5. The method of claim 1 , wherein the GM-CSF antagonist is an antibody specific for GM-CSF.6. The method of claim 5 , wherein the anti-GM-CSF antibody is namilumab claim 5 , otilimab claim 5 , gimsilumab claim 5 , lenzilumab or TJM-2.7. The method of any one of preceding claims claim 5 , wherein the subject is between 50 and 85 years of age.8. The method of claim 1 , wherein the giant cell arteritis is new-onset disease.9. The method of claim 1 , wherein the giant cell arteritis is relapsing disease.10. The method of claim 1 , wherein the giant cell arteritis is a refractory disease.11. The method of any of the preceding claims claim 1 , further comprising claim 1 , co-administering a corticosteroid to a subject in need thereof.12. The method of any of the preceding claims claim 1 , wherein the dose of the co-administered corticosteroid is tapered over the course of the treatment with the GM-CSF antagonist.13. The method of claim 1 , wherein the treating results in the prevention claim 1 , reduction or amelioration of at least one of the disease symptoms associated ...

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10-01-2019 дата публикации

LAMINATE CONTAINING CELL SHEET, AGENT FOR TREATING CARDIAC DISEASES, AND FILM FOR BEING LAMINATED ON CELL SHEET

Номер: US20190008791A1
Принадлежит:

An object of the present invention is to provide a laminate containing a cell sheet which has hardness and is easy to handle at the time of transplantation or transport, an agent for treating cardiac diseases using the laminate, and a film for being laminated on a cell sheet. According to the present invention there are provided a laminate including a biocompatible polymer film having a density of 500 μg/cmto 10 mg/cmand a cell sheet disposed on at least one surface of the biocompatible polymer film, an agent for treating cardiac diseases using the laminate, and a film for being laminated on a cell sheet. 1. A laminate comprising:{'sup': 2', '2, 'a biocompatible polymer film having a density of 500 μg/cmto 10 mg/cm; and'}a cell sheet disposed on at least one surface of the biocompatible polymer film. {'br': None, '(swollen film thickness/dry film thickness)×100≥−27.5×dry film thickness+880\u2003\u2003Formula 1, 'wherein the biocompatible polymer film satisfies the following Formula 1,'}where the unit of the swollen film thickness and the dry film thickness is μm.2. (canceled)3. The laminate according to claim 1 , {'br': None, '(swollen film thickness/dry film thickness)×100≥−27.5×dry film thickness+962.5\u2003\u2003Formula 2, 'wherein the biocompatible polymer film satisfies the following Formula 2,'}where the unit of the swollen film thickness and the dry film thickness is μm.4. The laminate according to claim 1 , {'br': None, '(swollen film thickness/dry film thickness)×100\u2003\u2003Formula 3, 'wherein a swelling ratio of the biocompatible polymer film represented by the following Formula 3 is equal to or higher than 230%,'}where the unit of the swollen film thickness and the dry film thickness is μm.5. The laminate according to claim 1 ,wherein the dry film thickness of the biocompatible polymer film is 5 to 200 μm.6. The laminate according to claim 1 ,wherein a wet film thickness of the biocompatible polymer film is 50 to 500 μm.7. The laminate according to ...

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09-01-2020 дата публикации

IN VIVO GENE THERAPY FOR IMMUNE DEFICIENCIES

Номер: US20200009266A1
Принадлежит:

In vivo gene therapies for immune deficiencies are described. The in vivo gene therapies utilize a foamy viral vector including a PGK promoter with a therapeutic gene. The foamy viral vector can be beneficially administered with cell mobilization into the peripheral blood. 1. A method of treating X-linked severe combined immunodeficiency (SCID-X1) in a subject in need thereof comprising administering a therapeutically effective amount of (i) a formulation comprising a foamy viral vector comprising a PGK promoter associated with a sequence encoding a γC protein; (ii) G-CSF; and (iii) AMD3100 , thereby treating SCID-X1 in the subject in need thereof.2. The method of claim 1 , wherein the foamy viral vector comprises a sequence selected from SEQ ID NOs: 1-3 claim 1 , 26 claim 1 , and 28-30.3. The method of claim 1 , wherein the foamy viral vector comprises a sequence encoding a sequence selected from SEQ ID NOs: 4 claim 1 , 5 claim 1 , and 27.4. The method of claim 1 , wherein the γC protein restores functionality to a γC-dependent signaling pathway.5. The method of claim 4 , wherein the functionality of a γC-dependent signaling pathway is determined by measuring tyrosine phosphorylation of STAT3 and/or STAT5 in cells from the subject following in vitro stimulation with IL-21 and IL-2 claim 4 , respectively.6. The method of claim 5 , wherein the tyrosine phosphorylation of STAT3 and/or STAT5 is measured by intracellular antibody staining.7. The method of claim 5 , wherein the cells are peripheral blood mononuclear cells (PBMCs).8. The method of claim 1 , wherein the therapeutically effective amount of the foamy viral vector is 1×10to 10×10infection units (IU).9. The method of claim 1 , wherein the therapeutically effective amount of G-CSF is 1 μg/kg to 10 μg/kg.10. The method of claim 1 , wherein the therapeutically effective amount of AMD3100 is 1 mg/kg to 10 mg/kg.11. The method of claim 1 , wherein the therapeutically effective amount of G-CSF is administered prior ...

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11-01-2018 дата публикации

PESTICIDAL COMPOSITIONS AND PROCESSES RELATED THERETO

Номер: US20180009737A1
Принадлежит: DOW AGROSCIENCES LLC

This disclosure relates to the field of molecules having pesticidal utility against pests in Phyla Nematoda, Arthropoda, and/or Mollusca, processes to produce such molecules and intermediates used in such processes, compositions containing such molecules, and processes of using such molecules against such pests. These molecules may be used, for example, as nematicides, acaricides, insecticides, miticides, and/or molluscicides. This document discloses molecules having the following formula (“Formula One”). 2. A molecule according to wherein:(a) R1 is H;(b) R2 is H, F, Cl, or Br;(c) R3 is H, F, Cl, or Br;(d) R4 is H, F, Cl, or Br;(e) R5 is H;{'sub': 1', '8, '(f) R6 is (C-C)haloalkyl;'}(g) R7 is H;(h) R8 is H;(I) R9 is H;{'sub': 1', '6', '1', '6, '(j) R10 is selected from a group consisting of F, Cl, Br, I, (C-C)alkyl, and (C-C)haloalkyl;'}(k) R11 is H;(I) R12 is H; (1) a linker that is bond connecting the two nitrogen atoms, or', {'sub': 1', '6, '(2) a (C-C)alkyl;'}], '(m) L is'} (1) an H, or', {'sub': 1', '8, '(2) a (C-C)alkyl;'}], '(n) R13 is'}{'sub': 1', '8', '1', '8', '3', '8', '2', '8', '2', '8', '2', '1', '6', '1', '6', '1', '6', '2', '1', '6', '1', '6', '2', '1', '6, '(o) R14 is independently selected from (C-C)alkyl, (C-C)haloalkyl, (C-C)cycloalkyl, (C-C)alkenyl, or (C-C)alkynyl, wherein each said alkyl, haloalkyl, cycloalkyl, alkenyl, and alkynyl has one or more substituents selected from F, Cl, Br, I, CN, NO, OH, oxo, (C-C)alkoxy, S(C-C)alkyl, S(O)(C-C)alkyl, S(O)(C-C)alkyl, and N((C-C)alkyl)wherein each (C-C)alkyl is independently selected, and wherein each said alkyl or alkoxy has one or more substituents independently selected from H, F, Cl, Br, and I.'}3. A molecule according to wherein:(a) R1 is H;(b) R2 is Cl or Br;(c) R3 is H, F, Cl, or Br;(d) R4 is Cl or Br;(e) R5 is H;{'sub': 1', '8, '(f) R6 is (C-C)haloalkyl;'}(g) R7 is H;(h) R8 is H;(I) R9 is H;{'sub': 1', '8', '1', '8, '(j) R10 is Br, (C-C)alkyl, (C-C)haloalkyl;'}(k) R11 is H;(I) R12 is H; (1) a ...

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14-01-2021 дата публикации

ANGIOGENESIS-INDUCING METHOD USING NEURAL STEM CELL

Номер: US20210009950A1
Автор: Joo Kyeung Min, Nam Hyun
Принадлежит:

The present invention relates to an angiogenesis-inducing method using neural stem cells. According to the present invention, neural stem cells derived from human brain tissues release MCP-1 or Gro, thus exhibiting an angiogenesis-inducing effect. When CoClwas treated to the neural stem cells of the present invention and when the neural stem cells were cultured in a hypoxia chamber, it was observed that a hypoxia condition increased the release amounts of MCP-1 and Gro. Therefore, the human brain tissue-derived neural stem cells of the present invention can be used to induce angiogenesis. 1. An angiogenesis-inducing method , comprising:(a) culturing neural stem cells under a hypoxia condition; and(b) injecting the cultured neural stem cells into a subject.2. The method of claim 1 , wherein the neural stem cells are derived from human brain tissue.32. The method of claim 1 , wherein the step (a) includes treating neural stem cells with cobalt (II) chloride (CoCl) or culturing neural stem cells in a hypoxia chamber.4. The method of claim 1 , wherein the step (b) includes injecting vascular endothelial cells along with the neural stem cells into a subject.5. The method of claim 1 , wherein the cultured neural stem cells secrete monocyte chemoattractant protein-1 (MCP-1) or a growth-related oncogene (Gro).6. The method of claim 3 , wherein the culturing the neural stem cells in a hypoxia chamber is performed for 12 to 72 hours.7. The method of claim 3 , wherein the CoClis treated at a concentration of 100 to 500 μM. The present invention relates to an angiogenesis-inducing method using neural stem cells.Stem cells are capable of self-renewal and differentiation into various cells, can be derived from an embryo or fetus. It is also known that resident stem cells in adult tissues can regenerate their own tissues. Mesenchymal stem cells are well known as adult stem cells and are the leading material for clinical researches worldwide.Neural stem cells are stem cells that ...

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14-01-2021 дата публикации

CARDIOMYOCYTE PREPARATION AND PREPARATION METHOD THEREFOR AND USE THEREOF

Номер: US20210009957A1
Принадлежит:

Provided are a cardiomyocyte preparation, a preparation method therefor and the use of the preparation in treating heart failure. The cardiomyocyte preparation comprises cardiomyocytes and fibroblasts, differentiated from pluripotent stem cells, wherein the concentration of the cardiomyocytes in the cardiomyocyte preparation is 0.75×10-1.0×10cells/mL, and the content of the cardiomyocytes is higher than 80% while the content of the fibroblasts is not higher than 20%. The cardiomyocyte preparation can improve cardiac ejection fraction and left ventricular fractional shortening, and increase the thickness of the left ventricular inner wall. 1. A cardiomyocyte formulation comprising cardiomyocytes and fibroblasts differentiated from pluripotent stem cells , wherein the concentration of the cardiomyocytes in the cardiomyocyte formulation is 0.75×10to 1.0×10cells/mL , and the content of the cardiomyocytes is higher than 80% and the content of the fibroblasts is not higher than 20%.2. The cardiomyocyte formulation of claim 1 , wherein the concentration of the cardiomyocytes is 0.5×10to 1.2×10cells/mL.3. The cardiomyocyte formulation of claim 1 , wherein residual amount of the pluripotent stem cells in the cardiomyocyte formulation is not more than 1%.4. The cardiomyocyte formulation of claim 3 , wherein residual amount of the pluripotent stem cells in the cardiomyocyte formulation is not higher than 0.3%.5. A method for preparing the cardiomyocyte formulation of claim 1 , wherein the cardiomyocytes are prepared from pluripotent stem cells by steps of:{'sup': 5', '5', '2, 'sub': '2', '1) pretreating the pluripotent stem cells: seeding the pluripotent stem cells into a pluripotent stem cell culture medium at a density of 0.9×10to 3.0×10cells/cm, culturing the cells at 37° C. with 5% COuntil cell density exceeds 40%;'}2) differentiating to cardiomyocytes: removing the pluripotent stem cell culture medium by suction, adding cardiomyocyte differentiation medium containing 0.01 ...

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10-01-2019 дата публикации

REGULATION OF MESODERMAL SPECIFICATION

Номер: US20190010458A1
Принадлежит:

Disclosed is a method to differentiate stern, progenitor or precursor cells comprising contacting said stem, progenitor or precursor cells with miR-130a, or an RNA having at least 95% identity thereto, so as to yield cells of endothelial lineage. Further disclosed are compositions comprising the endothelial lineage cells obtained and methods of using the compositions for treating diseases including cardiovascular diseases. 1. A method to differentiate cells comprising contacting stem , progenitor or precursor cells with miR-130a , or nucleic acid , such as an RNA , having at least 95% identity thereto , so as to yield cells of endothelial lineage.2. The method of claim 1 , wherein the stem claim 1 , progenitor or precursor cells are embryonic stem cells claim 1 , adult stem cells claim 1 , induce pluripotent stem cells claim 1 , and/or multipotent stem cells claim 1 , such as multipotent mesodermal precursors.3. The method of claim 1 , wherein the stem claim 1 , progenitor or precursor cells are mammalian cells.4. The method of claim 1 , wherein the progenitor cells are hemato-endothelial progenitors.5. The method of claim 1 , wherein the precursor cells are mesodermal precursor cells expressing Flk1/Pdgfra.6. The method of claim 1 , further comprising admixing the endothelial lineage cells with a pharmaceutically acceptable carrier.7. The method of claim 1 , comprising administering the endothelial lineage cells to a subject to a subject in need thereof so as to treat cardiovascular disease claim 1 , wound healing claim 1 , and/or repopulation of vasculature.8. The method of claim 7 , wherein cells administered to the subject are autologous or allogeneic.9. A composition consisting essentially of miR-130a and stem claim 7 , progenitor and/or precursor cells.10. The composition of claim 9 , wherein the cells are mammalian.11. A composition comprising the endothelial lineage cells obtained by the methods of and a cell culture media or a pharmaceutically acceptable ...

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10-01-2019 дата публикации

TREATMENT OF HEART DISEASE BY INHIBTION OF THE ACTION OF MUSCLE A-KINASE ANCHORING PROTEIN (mAKAP)

Номер: US20190010493A1
Автор: Kapiloff Michael S.
Принадлежит:

The present invention provides a method of protecting the heart from damage, by administering to a patient at risk of such damage, a pharmaceutically effective amount of a composition which inhibits the interaction of RSK3 and mAKAPβ, or the expression or activity of one or both of those molecules. This composition is preferably in the form of an siRNA construct, more preferably an shRNA construct, which inhibits the expression of mAKAPβ. 1. A composition comprising a vector encoding a small hairpin ribonucleic acid (“shRNA”) against human mAKAP.2. The composition of claim 1 , wherein the shRNA inhibits the interaction between human RSK3 and human mAKAP.3. The composition of claim 1 , wherein a therapeutically effective amount of said composition administered to a patient in need thereof protects the patient from heart damage.4. The composition of claim 1 , wherein the vector is a viral vector.5. The composition of claim 4 , wherein the viral vector is an adeno-associated virus vector (AAV).6. The composition of claim 1 , wherein the shRNA comprises a sense copy of a human mAKAP mRNA sequence and an antisense copy of a human mAKAP mRNA sequence.7. The composition of claim 6 , wherein the sense and antisense copies of the human mAKAP mRNA sequence are separated by a loop sequence.8. The composition of claim 5 , wherein the sense and antisense copies of the human mAKAP mRNA sequence are 19 nucleotides in length.12. The composition of claim 4 , wherein the viral vector comprises human microRNA (miR)-30a sequences.13. The composition of claim 4 , wherein the viral vector comprises a shRNA minigene claim 4 , wherein the minigene is flanked by a complete AAV2 inverted terminal repeat (ITR) on the 5′ end and a deleted AAV2 ITR on the 3′ end.14. The composition of claim 4 , wherein the viral vector comprises a chicken cardiac troponin T promoter.15. The composition of claim 4 , wherein the viral vector comprises a SV40 polyadenylation site.16. The composition of claim 5 , ...

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03-02-2022 дата публикации

METHODS AND COMPOSITIONS FOR THE TREATMENT OF SENGERS SYNDROME

Номер: US20220031799A1
Принадлежит: Stealth BioTherapeutics Inc.

The disclosure provides methods of preventing or treating Sengers syndrome in a mammalian subject, reducing risk factors associated with Sengers syndrome, and/or reducing the likelihood or severity of Sengers syndrome. The methods comprise administering to the subject an effective amount of an aromatic-cationic peptide to increase expression of AGK in subjects in need thereof. 1. A method for treating or preventing Sengers syndrome in a subject in need thereof , comprising administering to the subject a therapeutically effective amount of the peptide D-Arg-2′6′-Dmt-Lys-Phe-NHor a pharmaceutically acceptable salt thereof.2. The method of claim 1 , wherein the subject displays reduced levels of acylglycerol kinase (AGK) expression compared to a normal control subject.3. The method of any one of - claim 1 , wherein the peptide is administered daily for 6 weeks or more.4. The method of any one of - claim 1 , wherein the peptide is administered daily for 12 weeks or more.5. The method of any one of - claim 1 , wherein the subject has been diagnosed as having Sengers syndrome.6. The method of claim 5 , wherein the Sengers syndrome comprises one or more of cataracts claim 5 , hypertrophic cardiomyopathy claim 5 , reduced cardiac function as assessed by ejection fraction claim 5 , skeletal myopathy claim 5 , exercise intolerance claim 5 , lactic acidosis claim 5 , neutropenia claim 5 , tachydyspnea claim 5 , nystagmus claim 5 , eosinophilia claim 5 , cervical meningocele claim 5 , isolated Complex I deficiency claim 5 , strabismus claim 5 , hypotonia claim 5 , hyporeflexia claim 5 , delayed motor development claim 5 , reduced AGK expression claim 5 , reduced mitochondrial levels of glutamate carrier 1 (GC1) claim 5 , reduced mitochondrial levels of adenine nucleotide transporter type 1 (ANT1) claim 5 , reduced mitochondrial levels of adenine nucleotide transporter type 3 (ANT3) claim 5 , reduced mitochondrial levels of phosphate carrier (PiC) claim 5 , and reduced ...

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03-02-2022 дата публикации

COMPOSITIONS AND METHODS FOR TREATMENT OF CARDIAC DISEASES

Номер: US20220033819A1
Принадлежит:

Disclosed herein include microRNA antagonists, therapeutic compositions that include one or more of such microRNA antagonists, and methods of treating and/or ameliorating cardiac diseases and/or muscular dystrophy disorders with the microRNA antagonists. Also included are combination therapies, wherein a therapeutic composition disclosed herein and an additional therapy agent are provided to a subject having or suspected of having cardiac disease and/or muscular dystrophy disorder. In particular, some embodiments disclosed herein relate to compositions and methods for transiently administering a mixture of microRNA antagonists for promoting cardiomyocyte proliferation and cardiac regeneration. 1. A plurality of microRNA (miR) antagonists , comprising one or more miR-99a-5p antagonists , one or more miR-100-5p antagonists , one or more miR-Let-7a-5p antagonists , and one or more miR-Let-7c-5p antagonists , wherein:(a) at least one of the one or more miR-99a-5p antagonists comprises (i) a nucleotide sequence selected from the group consisting of SEQ ID NOs: 47, 48, 50, 52, and 54, and (ii) a chemical modification selected from the group consisting of a modified internucleoside linkage, a modified nucleotide, a modified sugar moiety, and combinations thereof;(b) at least one of the one or more miR-100-5p antagonists comprises (i) a nucleotide sequence selected from the group consisting of SEQ ID NOs: 46, 49, 51, 53, and 55, and (ii) a chemical modification selected from the group consisting of a modified internucleoside linkage, a modified nucleotide, a modified sugar moiety, and combinations thereof;(c) at least one of the one or more Let-7a-5p antagonists comprises (i) a nucleotide sequence having at least 90% identity to a sequence selected from the group consisting of SEQ ID NOs: 37, 39, and 40-45, and (ii) a chemical modification selected from the group consisting of a modified internucleoside linkage, a modified nucleotide, a modified sugar moiety, and ...

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15-01-2015 дата публикации

Crystal form of (6s)-5-methyltetrahydrofolate salt and method for preparing same

Номер: US20150018357A1

Disclosed are a crystal form of (6S)-5-methyltetrahydrofolate salt and a method for preparing the same. The crystal form is: Form C of the crystal form of (6S)-5-methyltetrahydrofolate calcium salt, where the X-ray diffraction pattern has diffraction peaks at the 2θ angles of 6.3±0.2 and 19.2±0.2; or the crystal form of (6S)-5-methyltetrahydrofolate strontium salt, where the X-ray diffraction pattern has diffraction peaks at the 2θ angles of 6.5±0.2 and 22.0±0.2. The crystal form of (6S)-5-methyltetrahydrofolate salt of the present invention has the advantages of excellent physicochemical properties, good stability, high purity, good reproducibility, and being more suitable for production on an industrial scale.

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15-01-2015 дата публикации

CF3O-CONTAINING ENAMINOKETONES AND THEIR UTILIZATION FOR THE PREPARATION OF CF3O-CONTAINING PYRAZOLES

Номер: US20150018561A1
Принадлежит:

The present invention pertains to novel enaminoketones containing a CFO-group, novel pyrazole-derivatives containing a CFO group as well as to a novel process for their preparation comprising aminoformylation of CFO-ketones and cyclization of the obtained CFO-enaminoketones with hydrazines to trifluoromethoxy pyrazoles. 2. Process according to claim 1 , wherein{'sup': '1', 'Ris 2-furyl, phenyl, or phenyl substituted with one or two chlorine atoms and'}{'sup': 2', '3, 'sub': 1', '6, 'Rand Rare independently C-Calkyl.'}6. Process according to claim 1 , wherein (A) is performed at a temperature of from 50° C. to 150° C.7. Process according to claim 1 , wherein the (A) is performed in a solvent selected from DMF claim 1 , toluene claim 1 , xylenes claim 1 , chlorobenzenes claim 1 , and dimethylacetamide.8. Process according to claim 2 , wherein (B) is performed at a temperature of from 0° C. to 50° C.10. Process according to claim 9 , wherein the compound of formula V-1 is oxidized using an oxidant selected from RuCl/NaIO claim 9 , RuO claim 9 , O claim 9 , KMnO claim 9 , and CrO.11. Process according to claim 9 , wherein the process is performed in a solvent selected from hexane/AcOEt/HO claim 9 , CCl/CHCN/HO claim 9 , HO/MeCN/AcOEt claim 9 , and HO/CHCl/MeCN. The present invention pertains to novel enaminoketones containing a CFO-group, novel pyrazole-derivatives containing a CFO group as well as to a novel process for their preparation comprising aminoformylation of CFO-ketones and cyclization of the obtained CFO-enaminoketones with hydrazines to trifluoromethoxy pyrazoles.Fluorine as a substituent in active ingredients plays a significant and increasingly important role. The biggest group of fluorinated pesticides are the compounds containing a trifluoromethyl group (mainly in aromatic rings), followed by aromatic compounds containing at least one isolated fluorine atom. Only five pesticides contain OCF-groups are on the market. It was estimated that the number of ...

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16-01-2020 дата публикации

IL-23-P19 VACCINES

Номер: US20200016249A1
Принадлежит: Affiris AG

Disclosed is a vaccine, preferably for use in the prevention or treatment of an interleukin 23 (IL-23) related disease, comprising a peptide bound to a pharmaceutically acceptable carrier, wherein said peptide is selected from the group QPEGHH-WETQQIPSLS (SEQ ID No. 103; p8322), GHHWETQQIPSLSPSQPWQRL QPEGHHWETQ (SEQ ID No. 98; p8461), TQQIPSLSPSQ (SEQ ID No. 99; p8400), QPEGHHWETQQIPSLSPSQ (SEQ ID No. 100; p9269), QPEGHHWETQQIPSLSPS (SEQ ID No. 101; p9269-C1), and QPEGHHWETQQIPSLSP (SEQ ID No. 102; p9269-C2), especially QPEGHHWETQQIPSLS (SEQ ID No. 103; p8322) and wherein said IL-23 related disease is selected from the group psoriasis, psoriatic arthritis, rheumatoid arthritis, systemic lupus erythematosus, diabetes, preferably type 1 diabetes, atherosclerosis, inflammatory bowel disease (IBD)/M. Crohn, multiple sclerosis, Behcet disease, ankylosing spondylitis, Vogt-Koyanagi-Harada disease, chronic granulomatous disease, hidratenitis suppurtiva, anti-neutrophil cytoplasmic antibodies (ANCA-) associated vasculitides, neurodegenerative diseases, preferably M. Alzheimer or multiple sclerosis, atopic dermatitis, graft-versus-host disease, cancer, preferably Oesophagal carcinoma, colorectal carcinoma, lung adenocarcinoma, small cell carcinoma, and squamous cell carcinoma of the oral cavity, especially psoriasis, neurodegenerative diseases or IBD. 1: A composition , comprising:{'claim-ref': {'@idref': 'CLM-00014', 'claim 14'}, 'the peptide according to , bound to a pharmaceutically acceptable carrier.'}2: The composition according to claim 1 , wherein at least one cysteine residue is bound to an N- or C-terminus of the peptide.3: The composition according to claim 1 , wherein at least one cysteine residue is bound to an N-terminus of the peptide.4: The composition according to claim 1 , wherein the pharmaceutically acceptable carrier is a protein carrier.5: The composition according to claim 4 , wherein the protein carrier is selected from the group consisting of keyhole ...

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17-01-2019 дата публикации

METHODS FOR TREATING OR PREVENTING GRAFT-VERSUS-HOST DISEASE INVOLVING THE ADMINISTRATION OF ANTI-CCR5 RECEPTOR AGENTS

Номер: US20190016810A1
Автор: Burger Denis R.
Принадлежит:

The present invention provides for inhibition or blockade of immunomodulatory cell receptors to treat or prevent graft-versus-host disease (GVHD). Thus, the invention relates generally to compositions and methods of using anti-CCR5 cell receptor binding agents, such as PRO 140, to treat or prevent GVHD. 1. A method of treating or preventing GVHD comprising administering to a subject in need thereof a competitive inhibitor to a CCR5 cell receptor that does not itself have CCL5 agonist activity.2. The method according to claim 1 , wherein the competitive inhibitor binds to an ECL-2 loop of the CCR5 cell receptor.3. The method according to claim 1 , wherein the competitive inhibitor competes with CCL5 for binding to the CCR5 cell receptor.4. The method according to claim 1 , wherein the competitive inhibitor comprises monoclonal antibody PA14 claim 1 , PRO 140 claim 1 , or CCR5mAb004 claim 1 , or a binding fragment thereof.5. The method according to claim 1 , wherein the competitive inhibitor does not affect cAMP levels when added to CD4+ T cells alone.6. The method according to claim 1 , wherein the competitive inhibitor does not affect chemotaxis of CHO-K1 cells.7. The method according to claim 1 , wherein the subject exhibits at least one of maintained body weight and no physical signs associated with GVHD.8. (canceled)9. The method according to claim 7 , wherein the subject exhibits no physical signs associated with GVHD within one of thirty days following treatment or seventy days following treatment.10. (canceled)11. The method according to claim 1 , wherein the GVHD is one of acute GVHD and chronic GVHD.12. (canceled)13. The method according to claim 1 , wherein the competitive inhibitor is administered to the subject during at least one of before transplant claim 1 , during transplant claim 1 , and after transplant.14. (canceled)15. (canceled)16. A method of treating or preventing GVHD comprising administering to a subject in need thereof an anti-CCR5 cell ...

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17-01-2019 дата публикации

Cetylated fatty acids, system for the preparation thereof and use thereof

Номер: US20190016991A1
Принадлежит: Pharmanutra SpA

The present invention relates to a process for preparing a mixture of cetylated fatty acids and a system for carrying out said process. Furthermore, the present invention relates to a composition comprising, or alternatively, consisting of said mixture of cetylated fatty acids. Finally, the present invention relates to said composition for use in the treatment and/or prevention of: (i) rheumatoid arthritis of inflammatory and non-inflammatory origin, in particular osteoarthritis; (ii) other inflammatory joint conditions; (iii) psoriasis, lupus, periodontal diseases or cardiovascular or heart diseases; (iv) all post-traumatic osteoarticular pathologies including sports injuries; (v) all degenerative joint pathologies (arthrosis, gonarthrosis, coxarthrosis, etc.), and (vi) inflammatory-traumatic tendon and muscular conditions. Furthermore, it is envisaged that the composition of the present invention be used in the treatment and/or prevention of the above-mentioned pathologies and disorders (i)-(vi) in association with a rehabilitative therapy. The composition comprising said mixture is formulated in a pharmaceutical form for oral use (novel food, supplement or medical device), i.e. in the form of a pill, pastille, capsule, tablet, granules, dispersible powder, syrup, solution or sprayable solution; for topical use, i.e. in the form of a cream, unguent, ointment, gel or spray to be used as such for application on the skin, or else for trans dermal use in the form of a patch.

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17-01-2019 дата публикации

Generation of Expandable Cardiovascular Progenitor Cells

Номер: US20190017029A1
Автор: Cao Nan, Ding Sheng, Zhang Yu
Принадлежит:

Methods and compositions for expanding cardiovascular progenitor cells are described herein that include use of compositions and culture media that have at least the following components: BMP4, Activin A, a glycogen synthase kinase 3 inhibitor, and an inhibitor of FGF, VEGF, and PDGF signaling. The methods include contacting cardiovascular progenitor cells with a culture medium having BMP4, Activin A, a glycogen synthase kinase 3 inhibitor, and an inhibitor of FGF, VEGF, and PDGF signaling, to generate an expanded cardiovascular progenitor cell population. 1. A method for expanding cardiovascular progenitor cells comprising contacting the cardiovascular progenitor cells with a culture medium comprising BMP4 , Activin A , a glycogen synthase kinase 3 inhibitor , and an inhibitor of FGF , VEGF , and PDGF signaling , to generate an expanded cardiovascular progenitor cell population.2. The method of claim 1 , wherein the glycogen synthase kinase 3 inhibitor is CHIR99021 claim 1 , 1-azakenpaullone claim 1 , AR-A014418 claim 1 , indirubin-3′-monoxime claim 1 , 5-Iodo-indirubin-3′-monoxime claim 1 , kenpaullone claim 1 , SB-415286 claim 1 , SB-216763 claim 1 , 2-anilino-5-phenyl-1 claim 1 ,3 claim 1 ,4-oxadiazole) claim 1 , (Z)-5-(2 claim 1 ,3-Memylenedioxyphenyl)imidazolidine-2 claim 1 ,4-dione claim 1 , TWS119 claim 1 , CHIR98014 claim 1 , SB415286 claim 1 , Tideglusib claim 1 , LY2090314 claim 1 , a lithium salt claim 1 , or a combination thereof.3. The method of claim 1 , wherein the inhibitor of FGF claim 1 , VEGF claim 1 , and PDGF signaling is SU5402 claim 1 , AP 24534 claim 1 , FIIN 1 hydrochloride claim 1 , R 1530 claim 1 , SU 6668 claim 1 , Sunitinib malate claim 1 , Toceranib; Brivanib alaninate claim 1 , or a combination thereof.4. The method of claim 1 , wherein the BMP4 is present in the culture medium at a concentration of 0.5 to 50 ng/mL claim 1 , about 0.5 to 20 ng/ml.5. The method of claim 1 , wherein the Activin A is present in the culture medium at a ...

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16-01-2020 дата публикации

HETEROCYCLIC COMPOUNDS AS KINASE INHIBITORS

Номер: US20200017520A1
Автор: Gately Stephen, WANG Tong
Принадлежит:

The present invention is directed to certain amides and heterocyclic compounds. The present invention also relates to uses of these compounds to treat several diseases including autoimmune disorders, cardiovascular disorders, inflammation, central nervous system disorders, arterial thrombotic disorders, fibrotic disorders, glaucoma, and neoplastic disorders. 2. The compound of claim 1 ,whereinwherein A is pyrazol-4-yl.3. The compound of claim 2 ,{'sub': '1', 'wherein Gis N, and'}{'sub': 2', '3, 'Gand Gare CH.'}4. The compound of claim 3 , wherein Q is methyl.5. The compound of claim 4 , wherein Ar is a substituted phenyl.6. The compound of claim 5 ,{'sub': a', 'a', '1-6, 'wherein the phenyl is substituted with —OR, and Ris —H or Calkyl.'}7. The compound of claim 51 , wherein R is —H.829-. (canceled)30. A method of treating a neoplastic disease in a subject comprising: administering to the subject a therapeutically effective amount of a compound of .31. The method of claim 30 , wherein the neoplastic disorder is a lymphoma claim 30 , carcinoma claim 30 , leukemia claim 30 , sarcoma claim 30 , or blastoma.32. The method of claim 31 , wherein the neoplastic disorder is acute myeloid leukemia (AML).33. The method of claim 32 , wherein the AML is ITD-FLT3 AML.3438-. (canceled)39. The compound of claim 3 , wherein Ar is a substituted phenyl.40. The compound of claim 39 , wherein the phenyl is substituted with —ORand Ris —H or Calkyl.41. The compound of claim 40 , wherein Ris methyl.42. The compound of claim 41 , wherein R is —H.43. The compound of claim 2 , wherein Ar is a substituted phenyl.44. The compound of claim 43 , wherein the phenyl is substituted with —ORand Ris —H or Calkyl.45. The compound of claim 44 , wherein Ris methyl.46. The compound of claim 45 , wherein R is —H.47. The compound of claim 39 , wherein Q is methyl and W is —H.48. The compound of claim 47 , wherein the configuration of the compound is R.49. The compound of claim 39 , wherein Q is methyl and ...

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16-01-2020 дата публикации

NPRA AGONISTS, COMPOSITIONS, AND USES THEREOF

Номер: US20200017567A1
Принадлежит: PharmaIN Corporation

This disclosure provides a natriuretic peptide derivative of Formula (I), and to compositions including a natriuretic peptide derivative of Formula (I), 1. A composition comprising a natriuretic peptide derivative of Formula (I) ,{'br': None, 'i': z', 'x', 'y, '(fatty acyl)-(B)-(G)-NP\u2003\u2003 (I),'}wherein:z is 1, x is an integer from 2 to 4 and y is 3; orz is 0, x is an integer from 0 to 4 and y is an integer from 1 to 3;fatty acyl comprises from 12 to 24 (e.g., 12 to 18) carbons atoms;B is lysine or arginine;G is glycine;NP is a natriuretic peptide;if present, (fatty acyl)z- is covalently linked to the N-terminus of (B)x;(fatty acyl)z-(B)x- is covalently linked to the N-terminus of (G)y; and(fatty acyl)z-(B)x-(G)y- is covalently linked to the N-terminus of NP,wherein the natriuretic peptide derivative increases the level of blood cGMP when parenterally administered to a mammal to a level higher than the natriuretic peptide NP when parenterally administered to a mammal at an equivalent dose (e.g., mole/Kg dose, mg/Kg dose, or both mole/Kg and mg/Kg dose); andwherein NP is selected from human BNP (Sequence ID 41) and human CNP (Sequence ID 57).27-. (canceled)8. The composition according to claim 1 , wherein B is lysine.9. The composition according to claim 1 , wherein the natriuretic peptide derivative is of Formula (II){'br': None, 'sub': x', '3, 'fatty acyl-(B)(G)-NP\u2003\u2003 (II),'}wherein:the fatty acyl comprises from 12 to 24 (e.g., 12 to 18) carbons atoms;B is lysine or arginine;x is an integer from 2 to 4;G is glycine;NP is a natriuretic peptide selected from human BNP (Sequence ID 41) and human CNP (Sequence ID 57);{'sub': 'x', 'fatty acyl- is covalently linked to the N-terminus of (B);'}{'sub': x', '3, 'fatty acyl-(B)- is covalently linked to the N-terminus of (G); and'}{'sub': x', '3, 'fatty acyl-(B)-(G)- is covalently linked to the N-terminus of NP.'}1012-. (canceled)13. The composition according to claim 9 , wherein fatty acyl comprises 18 carbon ...

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16-01-2020 дата публикации

COMPOSITIONS AND METHODS FOR ALLERGEN DETECTION

Номер: US20200018764A1
Автор: Gilboa-Geffen Adi
Принадлежит:

The present invention is drawn to nucleic acid aptamer based signaling polynucleotides (SPNs) for allergen detection in samples. Disclosed herein include compositions, compounds, assays and methods of using said SPNs to detect one or more allergens in a sample, particularly food allergens in a food product. 1. A method for determining if a food is safe to eat by a person who is allergic to peanut comprising:(a) obtaining a sample of the food to be tested,(b) processing said food sample and extracting proteins from the processed sample using an extraction buffer,(c) mixing the extracted proteins with a signaling polynucleotide (SPN) that comprises a nucleotide sequence selected from the group consisting of sequences presented by SEQ ID NOs.:8 to 10, and(d) detecting the interaction between the SPN and the peanut allergen and determining the presence or absence of the peanut allergen in the food sample.2. The method of wherein the nucleotide sequence or a portion of the nucleotide sequence specifically binds to the peanut allergen.3. The method of wherein the extraction buffer is a universal extraction buffer.4. The method of wherein the interaction between the SPN and the peanut allergen is detected by an enzyme-linked apta-sorbent assay (ELASA) claim 2 , a real-time PCR claim 2 , or a fluorescence resonance energy transfer (FRET) assay.5. A kit for detecting the presence or absence of peanut in a sample comprising: (i) a detection agent that is a nucleic acid molecule comprising a nucleotide sequence selected from the group consisting of sequences presented by SEQ ID NOs.:8 to 10; (ii) one or more extraction buffers for processing the sample and extracting proteins from the sample; and (iii) an instruction that instructs a user how to use the kit.6. The kit of wherein the sample is a food sample.7. The kit of wherein the user is allergic to peanut. This application is a Continuation application of U.S. patent application Ser. No. 15/569,808 filed Oct. 27, 2017, ...

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28-01-2016 дата публикации

HYDROLYSABLE LINKERS AND CROSS-LINKERS FOR ABSORBABLE POLYMERS

Номер: US20160023998A1
Автор: Bezwada Rao S
Принадлежит:

The present invention relates to the discovery of new class of linear and multiarmed hydrolysable linkers and cross linkers for use in the synthesis of biodegradable polymers such as, polyesters, polyurethanes, polyamides, polyureas and degradable epoxy amine resin. The linear and multiarmed hydrolysable linkers of the present invention include symmetrical and/or unsymmetrical ether carboxylic acids, amines, amide diols, amine polyols and isocyanates. This application claims the benefit of U.S. Application No. 60/972,855, filed Sep. 17, 2007, the disclosure of which is hereby incorporated herein by reference in its entirety.The present invention relates a new class of linear and multiarmed hydrolysable linkers and cross linkers and their synthetic intermediates for applications that include the synthesis of biodegradable polymers such as, polyesters, polyurethanes, polyamides, polyureas, and degradable epoxy amine resin. The linear and multiarmed hydrolysable linkers of the present invention include symmetrical and/or unsymmetrical ether carboxylic acids, amines, amide diols, amine polyols, and isocyanates.Much work has been accomplished in the last 20 years in the area of hydrophobic biodegradable polymers, wherein the biodegradable moieties include esters, lactones, orthoesters, carbonates, phosphazines, and anhydrides. Generally the polymers made of these biodegradable linkages are not water-soluble and therefore in themselves are not amenable for use in systems where water is required, such as in hydrogels.Since the mechanism of biodegradation in these polymers is generally through the hydrolytically-active components of water (hydronium and hydroxide ions), the rate of hydrolytic scission of the bonds holding a polymer network together is generally pH sensitive, with these moieties being susceptible to both specific-acid catalyzed hydrolysis and base hydrolysis. Other factors affecting the degradation of materials made of these polymers are the degree of ...

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26-01-2017 дата публикации

NOVEL CRYSTALLINE FORMS

Номер: US20170022225A1
Принадлежит:

Preparation and characterization of novel forms of (1-hydroxy-2-imidazol-1-yl-1-phosphono-ethyl) phosphonic acid, suitable for pharmaceutical compositions in drug delivery systems for humans. 1. A crystalline form of zoledronic acid: DL-lysine , whereinsaid crystalline form is characterized by a powder X-ray diffraction pattern comprising powder X-ray diffraction peaks at about 6.6, 11.0, 14.2, 18.3, 19.7, 22.7 and 27.6±0.2 degrees 2-theta; orsaid crystalline form is characterized by a powder X-ray diffraction pattern comprising powder X-ray diffraction peaks at about 7.2, 14.0, 18.3, 19.1, 20.7, 24.6 and 34.4±0.2 degrees 2-theta.2. A composition comprising a crystalline form of .3. A pharmaceutical composition comprising a crystalline form of and at least one pharmaceutically acceptable carrier.4. The pharmaceutical composition of wherein the pharmaceutical composition is a solid oral composition.5. The pharmaceutical composition of claim 4 , wherein the solid oral composition is a tablet or capsule.6. The pharmaceutical composition of claim 3 , wherein the pharmaceutical composition is a unit dose.7. A method of treating a disease for which zoledronic acid is indicated.8. A treatment method comprising the step of administering to a patient in need a therapeutically effective amount of a pharmaceutical composition of .9. The method of claim 8 , wherein said disease is selected from the group consisting of osteoporosis claim 8 , hypercalcemia claim 8 , cancer induced bone metastasis claim 8 , Paget's disease claim 8 , adjuvant cancer therapy and neoadjuvant cancer therapy.10. A method of treating a disease for which zoledronic acid is indicated claim 1 , said method comprising the step of administering to a patient in need thereof a therapeutically effective amount of a crystalline form of .11. The method of claim 10 , wherein said disease is selected from the group consisting of osteoporosis claim 10 , hypercalcemia claim 10 , cancer induced bone metastasis claim ...

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17-04-2014 дата публикации

Polymeric treatment compositions

Номер: US20140107251A1
Принадлежит: MicroVention Inc

Polymeric compositions are described comprising a biocompatible polymer including a biodegradable linkage to a visualization agent and a non-physiological pH solution; wherein the biocompatible polymer is soluble in the non-physiological pH solution and insoluble at a physiological pH. Methods of forming the solutions and polymers are disclosed as well as methods of therapeutic use.

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10-02-2022 дата публикации

ARYLCYCLOHEXYLAMINE DERIVATIVES AND THEIR USE IN THE TREATMENT OF PSYCHIATRIC DISORDERS

Номер: US20220041540A1
Автор: Kruegel Andrew Carry
Принадлежит:

Provided herein are arylcyclohexylamine derivatives and their use in the treatment of psychiatric disorders. 2. A pharmaceutical composition comprising a compound of and a pharmaceutically acceptable excipient. This application is a continuation of International Application No. PCT/US2020/067235, filed Dec. 28, 2020, which claims priority to U.S. Provisional Application No. 62/953,611, filed Dec. 26, 2019; U.S. Provisional Application No. 63/037,044, filed Jun. 10, 2020; and U.S. Provisional Patent Application No. 63/093,830, filed Oct. 20, 2020, each of which are incorporated herein by reference in their entirety.Approximately one third of patients with major depressive disorder (MDD) fail to achieve remission of their symptoms, even after multiple rounds of treatment with several known classes of antidepressants, including selective serotonin reuptake inhibitors (SSRIs) (Rush et al. 2006). This high prevalence of treatment-resistant depression (TRD) makes clear the need for new, more efficacious pharmacotherapies for depression that will target new mechanisms and/or patient populations. In recent years, ketamine, a drug long used as a dissociative anesthetic, has attracted considerable attention for its secondary use as a rapid-acting antidepressant with robust efficacy, even in patients with TRD (Zarate et al. 2006; Berman et al. 2000). The antidepressant effects of the drug are also notable in that they persist for days or weeks after a single administration. Importantly, the S enantiomer of ketamine (S-ket) has recently been approved by the United States Food and Drug Administration as a treatment for depressionUnfortunately, the potent dissociative anesthetic effects of ketamine and S-ket make these drugs attractive to recreational drug users and limit the broad clinical utility of these compounds by restricting their use to circumstances under the direct supervision of a medical provider. Given that the primary molecular target of ketamine is the N-methyl-D- ...

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24-01-2019 дата публикации

ANTI-JAGGED1 ANTIGEN BINDING PROTEINS

Номер: US20190023802A1
Принадлежит: Amgen Inc.

Methods of treating conditions related to lung disease using an antigen binding protein specific for the Jagged1 polypeptide are provided. 1. A method of treating a subject with a condition related to lung disease , the method comprising administering to the subject a therapeutically effective amount of an antigen binding protein that specifically binds to a protein having an amino acid sequence having at least 90% amino acid sequence identity to an amino acid sequence of a Jagged1.2. The method of claim 1 , wherein the subject is a mammal.3. The method of claim 1 , wherein the subject is human.4. The method of claim 1 , wherein the administering is by nebulization.5. The method of claim 1 , wherein the administering is by subcutaneous injection.6. An isolated antigen binding protein that specifically binds to a Jagged1 polypeptide.7. The isolated antigen binding protein of claim 6 , wherein the human Jagged1 has a sequence comprising SEQ ID NO: 353.8. The isolated antigen binding protein of claim 6 , wherein the antigen binding protein is a monoclonal antibody claim 6 , a polyclonal antibody claim 6 , a recombinant antibody claim 6 , a human antibody claim 6 , a humanized antibody claim 6 , a chimeric antibody claim 6 , a multispecific antibody claim 6 , or an antibody fragment thereof.9. The isolated antigen binding protein of claim 8 , wherein the antibody fragment is a Fab fragment claim 8 , a Fab′ fragment claim 8 , or a F(ab′)2 fragment.10. The isolated antigen binding protein of claim 8 , wherein the antigen binding protein is a human antibody.11. The isolated antigen binding protein of claim 8 , wherein the antigen binding protein is a monoclonal antibody.12. The isolated antigen binding protein of claim 8 , wherein the antigen binding protein is of the IgG1- claim 8 , IgG2- IgG3- or IgG4-type.13. The isolated antigen binding protein of claim 12 , wherein the antigen binding protein is of the IgG1- or the IgG2-type.14. The isolated antigen binding protein of ...

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28-01-2021 дата публикации

COMPOUND WHICH INHIBITS TELOMERE-BINDING PROTEIN, AND TELOMERE-BINDING PROTEIN INHIBITOR CONTAINING SAME

Номер: US20210024455A1
Принадлежит:

The compound according to the present invention is a compound represented by the following chemical formula: 2. The compound according to claim 1 ,wherein, in the above-described chemical formula,{'sub': '1', 'Ris oxygen,'}{'sub': 2', '4, 'Rand Rare each independently hydrogen or a nitro group,'}{'sub': '3', 'Ris hydrogen, a nitro group, a methyl group, a methoxy group or a butyl group,'}{'sub': '5', 'Ris hydrogen, a methyl group, a methoxy group or an acetyl group, and'}{'sub': '6', 'Ris hydrogen or a butyl group.'}5. The method according to claim 4 ,wherein, in the above-described chemical formula,{'sub': '1', 'Ris oxygen or sulfur,'}{'sub': 2', '4, 'Rand Rare each independently hydrogen or a nitro group,'}{'sub': '3', 'Ris hydrogen, a nitro group, a methyl group, a methoxy group or a butyl group,'}{'sub': '5', 'Ris hydrogen, a methyl group, a methoxy group or an acetyl group, and'}{'sub': '6', 'Ris hydrogen or a butyl group.'}7. The method according to claim 4 , wherein the above-described telomere-binding protein is TRF1 claim 4 , TRF2 claim 4 , or POT1.813.-. (canceled)15. The method according to claim 14 , wherein claim 14 , in the above-described chemical formula claim 14 ,{'sub': '1', 'Ris oxygen or sulfur,'}{'sub': 2', '4, 'Rand Rare each independently hydrogen or a nitro group,'}{'sub': '3', 'Ris hydrogen, a nitro group, a methyl group, a methoxy group or a butyl group,'}{'sub': '5', 'Ris hydrogen, a methyl group, a methoxy group or an acetyl group, and'}{'sub': '6', 'Ris hydrogen or butyl group.'} The present invention relates to a compound that inhibits a telomere-binding protein, and a telomere-binding protein inhibitor containing the same.At the end of human chromosomal DNA, a double-stranded DNA composed of a repeating sequence of 5′-TTAGGG-3′ called a telomere is present. At the extreme end of the telomere, 3′ end is protruded and a single-stranded DNA portion composed of 75 to 300 bases called G tail is formed. Usually, the G tail is in a protected ...

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28-01-2021 дата публикации

(S)-CSA Salt Of S-Ketamine, (R)-CSA Salt Of S-Ketamine And Processes For The Preparation Of S-Ketamine

Номер: US20210024461A1
Принадлежит:

The present invention is directed to processes for the preparation of esketamine. The present invention is further directed to processes for the resolution of S-ketamine from a racemic or enantiomerically enriched mixture of ketamine. The present invention is further directed to an (S)-CSA salt of S-ketamine, more particularly a monohydrate form of the (S)-CSA salt of S-ketamine; and to an (R)-CSA salt of R-ketamine. 1. An (S)-camphorsulfonic acid salt of S-ketamine.2. An (S)-camphorsulfonic acid salt of S-ketamine as in claim 1 , wherein the salt is a monohydrate.3. A crystalline monohydrate form of (S)-camphorsulfonic acid salt of S-ketamine.7. A process as in claim 6 , wherein the (S)-camphorsulfonic acid is present in an amount in the range of from about 0.75 to about 1.2 molar equivalents.8. A process as in claim 6 , wherein the (S)-camphorsulfonic acid is present in an amount in the range of from about 0.9 to about 1.1 molar equivalents.9. A process as in claim 6 , wherein the water is present in an amount in the range of from about 5% to about 10%.10. A process as in claim 6 , wherein the water is present in an amount in the range of from about 6% to about 8%.11. A process as in claim 6 , wherein the organic solvent is selected from the group consisting of methyl ethyl ketone and 2-methyl-THF.12. A process as in claim 6 , wherein the organic solvent is 2-methyl-THF.13. A process as in claim 6 , wherein the ketamine is reacted with (S)-camphorsulfonic acid at a temperature in the range of from about 30° C. to about 100° C.14. A process as in claim 6 , wherein the ketamine is reacted with (S)-camphorsulfonic acid at a temperature of about 50° C. to about 80° C.15. A process as in claim 6 , wherein the monohydrate form of (S)-camphorsulfonic acid salt of S-ketamine is present in an enantiomeric excess in the range of from about 75% to about 100%.16. A process as in claim 6 , wherein the monohydrate form of (S)-camphorsulfonic acid salt of S-ketamine is present ...

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28-01-2021 дата публикации

METHODS FOR MODULATION OF LIPOPROTEIN LIPASE AND APOLIPOPROTEIN C2 EXPRESSION AND/OR ACTIVITY IN THE TREATMENT OF PERIPHERAL AND CENTRAL NERVOUS SYSTEM TISSUE DISEASE STATES

Номер: US20210024568A1
Автор: Yarger James G.
Принадлежит:

Methods for modulating lipoprotein lipase (LPL) and Apoliprotein C2 (ApoC2) expression and/or activity in the treatment of peripheral and central nervous system tissue disease states with C-6 substituted estradiol derivatives are presented herein. 2. A method for modulating lipoprotein lipase (LPL) or apolipoprotein C(ApoC2) expression and/or activity claim 1 , the method comprising contacting a cell capable of expressing LPL and/or ApoC2 with an effective amount of the compound according to .3. The method of claim 2 , wherein the cell is a microglial cell or a macrophage cell.4. The method of claim 2 , wherein LPL and/or ApoC2 is upregulated.5. A method for switching claim 1 , polarizing claim 1 , or altering an inflammatory phenotype claim 1 , the method comprising contacting a cell having a pro-inflammatory phenotype with an effective amount of the compound according to claim 1 , thereby switching claim 1 , polarizing claim 1 , or altering the inflammatory phenotype to an anti-inflammatory phenotype.6. The method of claim 5 , wherein the cell is a microglial cell or a macrophage cell.7. The method of claim 5 , wherein an inflammatory gene is down-regulated.8. The method of claim 5 , wherein a reparative gene is upregulated.9. A method for treating a condition claim 1 , disease claim 1 , or disorder in a subject claim 1 , the method comprising administering a therapeutically-effective amount of the compound according to to the subject claim 1 , wherein the subject is in need of a treatment for inflammation.10. The method of claim 9 , wherein the subject is in need of a treatment for inflammation associated with a cell having a pro-inflammatory phenotype and wherein administration of the therapeutically-effective amount of the compound switches claim 9 , polarizes claim 9 , or alters the pro-inflammatory phenotype to an anti-inflammatory phenotype.11. The method of claim 10 , wherein the inflammation is induced by an infection.12. The method of claim 11 , wherein ...

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