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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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Форма поиска

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 8595. Отображено 100.
12-01-2012 дата публикации

Prebiotic Formulations for use with Probiotics to Increase Probiotic Growth Rate and Activity

Номер: US20120009239A1
Принадлежит: MASTER SUPPLEMENTS Inc

Naturally occurring lecithins and/or oleic acid stimulate the growth and lactic acid producing activity of Lactobacillus and Bifidobacterium species of probiotic bacteria, and replace polysorbate 80 for those products. They can be used in naturally occurring form, or where they are to be combined with probiotics in a carrier, or they can be treated to yield a stable powdered form of these naturally oily compounds. They can be sold as combined prebiotic/probiotic formulations in the same carrier, or sold as separate dietary supplements, e.g., in capsule or tablet form, to be used with the probiotic formulation as desired.

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08-03-2012 дата публикации

Modulation of drug release rate from electrospun fibers

Номер: US20120058100A1
Принадлежит: Individual

Disclosed are co-electrospun polymeric fibers comprising polymers comprising pharmaceutically active agents and/or biologically active agents and capable of release at a combined release rate. Also disclosed are processes for preparing polymeric fibers capable of release at a combined release rate. Also disclosed are processes of modulating delivery rate of pharmaceutically active agents and/or biologically active agents. Also disclosed are processes of delivering pharmaceutically active agents and/or biologically active agents. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

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03-05-2012 дата публикации

Composition for treatment of menopause

Номер: US20120107344A1
Автор: Isaac Cohen
Принадлежит: Bionovo Inc

A novel herbal extract, MF101, is effective in the treatment of symptoms of menopause.

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24-05-2012 дата публикации

New pharmaceutical compositions for treatment of respiratory and gastrointestinal disorders

Номер: US20120129820A1
Автор: Abhya Gupta, Peter Seither
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

The present invention provides pharmaceutical compositions comprising one or more CRTH2 antagonists 1 and one or more further active compounds 2.

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31-05-2012 дата публикации

Substituted Esters as Cannabinoid-1 Receptor Modulators

Номер: US20120135975A1
Принадлежит: Merck and Co Inc

Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, Alzheimer's disease, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, cirrhosis of the liver, non-alcoholic fatty liver disease (NAFLD), non-alcoholic steatohepatitis (NASH), and the promotion of wakefulness.

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14-06-2012 дата публикации

Lactobacillus acidophilus nucleic acid sequences encoding cell surface protein homologues and uses therefore

Номер: US20120149590A1
Принадлежит: North Carolina State University

Cell wall, cell surface and secreted protein nucleic acid molecules and polypeptides and fragments and variants thereof are disclosed in the current invention. In addition, cell wall, cell surface and secreted fusion proteins, antigenic peptides, and anti-cell wall, cell surface and secreted antibodies are encompassed. The invention also provides recombinant expression vectors containing a nucleic acid molecule of the invention and host cells into which the expression vectors have been introduced. Methods for producing the polypeptides of the invention and methods for their use are further disclosed.

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19-07-2012 дата публикации

Lactoferrin and neuronal health and development in the infant gut

Номер: US20120184483A1
Принадлежит: Nestec SA

The present invention relates generally to the field of neuronal health, neuronal protection and neuronal development. One embodiment of the present invention relates to a composition that can be used for the treatment or prevention of a delayed development of the enteric nervous system. Neuronal cells in the gut can be protected. Disorders linked to a delayed development of the enteric nervous system and/or to an impaired enteric nervous system can be treated or prevented by the administration of lactoferhn containing compositions.

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26-07-2012 дата публикации

Compositions and improved soft tissue replacement methods

Номер: US20120189708A1
Принадлежит: Allergan Inc

The specification discloses compositions and methods for treating a soft tissue defect of an individual.

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09-08-2012 дата публикации

Methods of treating diseases with proanthocyanidin oligomers such as crofelemer

Номер: US20120202876A1

Disclosed herein are methods of treating diseases including gastrointestinal disorders, such as secretory diarrheas, with the proanthocyanidin oligomer, crofelemer. Also disclosed is the anti-secretory effect of crofelemer on Calcium-activated chloride channels (CaCC) and Cystic fibrosis transmembrane conductance regulator (CFTR).

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30-08-2012 дата публикации

Pharmaceutical composition and administrations thereof

Номер: US20120220625A1
Принадлежит: Vertex Pharmaceuticals Inc

The present invention relates to pharmaceutical compositions comprising a solid dispersion of N-[2,4-Bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide, methods of manufacturing pharmaceutical compositions of the present invention, and methods of administering pharmaceutical compositions of the present invention.

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06-09-2012 дата публикации

Dosage form containing oxycodone and naloxone

Номер: US20120225901A1
Принадлежит: Euro Celtique SA

The present invention concerns a dosage form comprising oxycodone and naloxone which is characterized by specific in vivo parameters such as t max , C max , AUCt value, mean bowel function score and/or duration of analgesic efficacy.

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13-09-2012 дата публикации

Methods of treating cancer using 3-(5-amino-2-methyl-4-oxo-4h-quinazolin-3-yl)-piperidine-2,6-dione

Номер: US20120230983A1
Принадлежит: Celgene Corp

Provided herein are methods of treating, preventing and/or managing cancers, which comprise administering to a patient 3-(5-amino-2-methyl-4-oxo-4H-quinazolin-3-yl)-piperidine-2,6-dione, or an enantiomer or a mixture of enantiomers thereof, or a pharmaceutically acceptable salt, solvate, hydrate, co-crystal, clathrate, or polymorph thereof.

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20-09-2012 дата публикации

Anti-constipation composition

Номер: US20120237598A1
Автор: Ryuji Ueno
Принадлежит: SUCAMPO AG

An object of the present invention is to provide an anti-constipation composition containing a halogenated-bi-cyclic compound as an active ingredient in ratio of bi-cyclic/mono-cyclic structure of at least 1:1. The halogenated-bi-cyclic compound is represented by Formula (I): where X 1 and X 2 are preferably both fluorine atoms. The composition can be used to treat constipation with out substantive side-effects, such as stomachache.

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18-10-2012 дата публикации

Quinolinone-carboxamide compounds as 5-ht4 receptor agonists

Номер: US20120264779A1
Принадлежит: Theravance Inc

The invention provides novel quinolinone-carboxamide 5-HT 4 receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5-HT 4 receptor activity, and processes and intermediates useful for preparing such compounds.

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25-10-2012 дата публикации

Nutritional composition for promoting gut microbiota balance and health

Номер: US20120269865A1
Принадлежит: Nestec SA

The present disclosure relates to nutritional compositions comprising a fructo-oligosaccharide (FOS) in an amount of 35 to 44% by weight; a polysaccharide that is not a partially hydrolyzed guar gum such as, for example, an arabinogalactan in an amount of 50% to 38% by weight; and inulin in an amount of 12% to 24% by weight. The FOS and the polysaccharide may be present in a weight ratio of about 1:1. More specifically, the FOS and inulin may be present in a weight ratio of about 7:3. Also provided are methods of promoting gut microbiota balance and health. The methods include administering an effective amount of the nutritional composition to patients in need of same.

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25-10-2012 дата публикации

Nutritional compositions including theanine and exogenous nucleotides

Номер: US20120270830A1
Принадлежит: Nestec SA

Nutritional compositions and methods of making and using the nutritional compositions are provided. In a general embodiment, the present disclosure provides a nutritional composition including theanine and one or more exogenous nucleotides. The nutritional compositions can be specifically used to treat functional bowel disorders, including inflammatory bowel syndrome.

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06-12-2012 дата публикации

Method for treatment of lacto-n-biose-containing solution

Номер: US20120309708A1
Принадлежит: Morinaga Milk Industry Co Ltd

The present invention relates to a method of treating a liquid composition containing lacto-N-biose, the method including: preparing a liquid composition containing lacto-N-biose having a pH at 25° C. of not less than 2.0 and not more than 5.5, and heating the liquid composition at a temperature of 65° C. or higher. The present invention can provide a treatment method that enables thermal decomposition of lacto-N-biose to be suppressed when a liquid composition containing lacto-N-biose is heated at a temperature of 65° C. or higher, a liquid preparation containing lacto-N-biose that is treated using the treatment method, a dried product produced from such a liquid preparation containing lacto-N-biose, and a method of producing a product containing lacto-N-biose.

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10-01-2013 дата публикации

Metabolically Active Micro-Organisms and Methods for Their Production

Номер: US20130011368A1
Автор: Timothy Thurlby
Принадлежит: Individual

The invention relates to a preparation of metabolically active bacteria, compositions comprising such a preparation, e.g., probiotic supplements or animal feeds, and to uses thereof, for example in the treatment of diseases affecting the intestinal microbial balance. Also described are a growth substrate for microorganisms comprising a mixture of complex and simple sugars and a process for the manufacture of preparations of metabolically active microorganisms using this growth substrate.

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10-01-2013 дата публикации

Orally Disintegrating Compositions of Linaclotide

Номер: US20130012454A1

The present invention relates to orally disintegrating or dissolving pharmaceutical compositions comprising linaclotide or pharmaceutically acceptable salts thereof, as well to various methods and processes for the preparation and use of the compositions.

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14-02-2013 дата публикации

Quick Dissolving, Long Acting Zinc Therapeutic Formulations

Номер: US20130039981A1
Принадлежит: Individual

The present invention comprises a quick dissolving, long acting zinc therapeutic cold formulation containing high levels of an active compound encapsulated within bioadhesive/muco-adhesive polymers as a controlled release oral drug delivery system. The composition allows for increased residence time for enhanced prophylactic and therapeutic efficacy within the mouth and oral cavity. This allows for a reduction in the number of doses necessary to achieve therapeutic relief which will result in increased patience compliance.

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28-02-2013 дата публикации

Formulations for oral delivery of adsorbents in the gut

Номер: US20130052269A1
Принадлежит: Da Volterra SAS

The invention relates to a formulation for the delayed and controlled delivery of an adsorbent into the lower intestine of mammals. The formulation includes a carrageenan and an adsorbent, such as activated charcoal. The invention further relates to uses of this formulation, in particular to pharmaceutical uses. In one embodiment, the formulation is used to eliminate or reduce the side effects in the intestine, in particular in the colon, of pharmaceutical agents that are administered as a treatment for a disorder, but that have side effects when they reach the late ileum, the caecum or the colon.

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14-03-2013 дата публикации

Engineered anti-il-23r antibodies

Номер: US20130064817A1
Автор: Leonard G. Presta
Принадлежит: Merck Sharp and Dohme LLC

Antibodies to human IL-23R are provided, as well as uses thereof, e.g. in treatment of inflammatory, autoimmune, and proliferative disorders.

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21-03-2013 дата публикации

Process for Making Modulators of Cystic Fibrosis Transmembrane Conductance Regulator

Номер: US20130072522A1
Принадлежит: Vertex Pharmaceuticals Inc

The invention provides a process for the preparation of a compound of Formula 1, comprising coupling a carboxylic acid of Formula 2 with an aniline of Formula 3 in the presence of a coupling agent.

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28-03-2013 дата публикации

Soft-gelatin capsule formulation

Номер: US20130078303A1
Принадлежит: R Tech Ueno Ltd, SUCAMPO AG

The present invention discloses a soft gelatin capsule formulation of a 15-keto-prostaglandin compound, which comprises: a soft gelatin capsule shell comprising gelatin and sugar alcohol as a plasticizer, and a mixture comprising a 15-keto-prostaglandin compound and a pharmaceutically acceptable vehicle which is filled in the shell. By encapsulating the 15-keto-prostaglandin compound in the specified soft gelatin capsule shell, stability of the compound is significantly improved.

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18-04-2013 дата публикации

Pharmaceutical compositions of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyriodin-2-yl)benzoic acid and administration thereof

Номер: US20130095181A1
Принадлежит: Vertex Pharmaceuticals Inc

A pharmaceutical composition comprising Compound 1, (3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid), and at least one excipient selected from: a filler, a diluent, a disintegrant, a surfactant, a binder, a glidant and a lubricant, the composition being suitable for oral administration to a patient in need thereof to treat a CFTR mediated disease such as Cystic Fibrosis. Methods for treating a patient in need thereof include administering an oral pharmaceutical formulation of Compound 1 to the patient.

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09-05-2013 дата публикации

Agonists of Guanylate Cyclase Useful For the Treatment of Gastrointestinal Disorders, Inflammation, Cancer and Other Disorders

Номер: US20130116199A1
Автор: Kunwar Shailubhai
Принадлежит: Synergy Pharmaceuticals Inc

The invention provides novel guanylate cyclase-C agonist peptides and their use in the treatment of human diseases including gastrointestinal disorders, inflammation or cancer (e.g., a gastrointestinal cancer). The peptides can be administered either alone or in combination with an inhibitor of cGMP-dependent phosphodiesterase. The gastrointestinal disorder may be classified as either irritable bowel syndrome, constipation, or excessive acidity etc. The gastrointestinal disease may be classified as either inflammatory bowel disease or other GI condition including Crohn's disease and ulcerative colitis, and cancer.

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06-06-2013 дата публикации

5-[5-[2-(3,5-bis(trifluoromethyl)phenyl)-2-methylpropanomethylpropanoylmethylamino]-4-(4-fluoro-2-methylphenyl)]-2-pyridinyl-2-alkyl-prolinamide as nk1 receptor antagonists

Номер: US20130143931A1
Принадлежит: GLAXO WELLCOME MANUFACTURING PTE LTD

The invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein R is C 1-4 alkyl useful in the treatment of diseases and conditions for which antagonism of NK1 receptor is beneficial.

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20-06-2013 дата публикации

Stable high lipid liquid formula

Номер: US20130157937A1
Принадлежит: Nutricia NV

The present invention provides a ketogenic diet in the form of a sterile shelf stable ready to use formula, in particular a tube feed, comprising casein and dietary fibre.

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20-06-2013 дата публикации

Sigma receptor inhibitors

Номер: US20130158029A1
Принадлежит: Laboratorios del Dr Esteve SA

The invention refers to compounds of general formula (I) having pharmacological activity towards the sigma receptor, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use for the treatment and or prophylaxis of a disease in which the sigma receptor is involved.

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18-07-2013 дата публикации

Pharmaceutical Composition for Topical Application

Номер: US20130184242A1
Автор: Dov Tamarkin, Meir Eini
Принадлежит: Foamix Ltd

A pharmaceutical or cosmetic carrier or composition for topical application characterized by rheological properties which render the carrier or composition semi-solid at rest and a liquid upon application of shear forces thereto. The composition or carrier are prepared by mixing 1-25 percent of a solidifying agent and 75-99 percent of a hydrophobic solvent, by weight, wherein at least one of them has therapeutic or cosmetic benefits, in the presence or absence of a biologically active substance.

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08-08-2013 дата публикации

Immunoregulatory peptides and methods of use

Номер: US20130203683A1
Принадлежит: 13Therapeutics Inc

Peptides for the treatment of inflammation, and therapeutic uses and methods of using the same are disclosed. Peptides including a transducing sequence are effective for inhibiting cytokine activity and TNF-α secretion through interaction with toll-like receptors. Experiments are described illustrating the efficacy of the compounds in treating otitis media

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15-08-2013 дата публикации

Treatment of IBD and IBS Using Both Probiotic Bacteria and Fermented Cereal as Treatment Effectors

Номер: US20130209404A1
Автор: Hans Israelsen
Принадлежит: Nordisk Rebalance AS

The invention covers a novel treatment strategy that considerably improves conventional probiotic treatments of inflammatory bowel diseases, irritable bowel syndrome and other gastrointestinal disorders. Both probiotic microorganisms and the carrier of the probiotic microorganisms in form of a fermented cereal gruel are used as treatment effectors. Phospholipids may also be an effector. The novel treatment strategy is capable of removing the symptoms of inflammatory bowel diseases regardless of a mild, moderate or severe stage of the disease.

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12-09-2013 дата публикации

Materials and methods for delivering compositions to selected tissues

Номер: US20130236518A1
Принадлежит: UNIVERSITY OF CALIFORNIA

This invention relates to devices, systems and methods for delivering preprogrammed quantities of an active ingredient to a biological system over time without the need for external power or electronics.

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03-10-2013 дата публикации

Exopolysaccharide

Номер: US20130261071A1
Принадлежит: Alimentary Health Ltd, Procter and Gamble Co

An isolated polysaccharide has the structure [-β(1,3)-D-GaIpNAc-β(1,4)-D-Glcp-] n . The polysaccharide may be from a Bifidobacterium strain NCIMB 41003. The polysaccharide exhibits immunomodulatory activity.

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17-10-2013 дата публикации

Stable Solid Formulation of GC-C Receptor Agonist Polypeptide Suitable for Oral Administration

Номер: US20130273169A1
Принадлежит: Ironwood Pharmaceuticals Inc

Solid, stable formulations of linaclotide suitable for oral administration are described herein as are methods for preparing such formulations. The formulations described herein contain a polypeptide consisting of the amino acid sequence Cys Cys Glu Tyr Cys Cys Asn Pro Ala Cys Thr Gly Cys Tyr (“linaclotide”; SEQ ID NO:1) or a pharmaceutically acceptable salt thereof. The linaclotide formulations described herein are stable and have a sufficient shelf life for manufacturing, storing and distributing the drug.

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24-10-2013 дата публикации

Soft Elastic Capsules Containing Tablets and Liquid or Semisolid Fills and Methods for Their Manufacture

Номер: US20130280323A1
Принадлежит: Banner Pharmacaps Inc

Disclosed herein is a soft elastic capsule that includes an acid resistant, capsule shell that defines an encapsulated space having a predetermined volume, a liquid or semisolid fill comprising a first active ingredient located within the encapsulated space, and a first compressed tablet a having a minimal dimension of 2 mm, being located within the encapsulated space, unanchored to the capsule shell, and surrounded by the fill, said tablet comprising a second active ingredient that is substantially insoluble in the fill. A method of manufacturing a soft elastic capsule is also disclosed.

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24-10-2013 дата публикации

Novel 6-Amino-Morphinan Derivatives, Method of Manufacturing Them and Their Application as Analgesics

Номер: US20130281698A1
Принадлежит: AlcaSynn Pharmaceuticals GmbH

This invention provides novel 6-amino-morphinan derivatives, methods of making same, and methods of using same for analgesic purposes. The derivatives of this invention are represented by the following formula:

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14-11-2013 дата публикации

Systems and Methods for Treating an Opioid-Induced Adverse Pharmacodynamic Response

Номер: US20130303561A1
Принадлежит: Purdue Pharma LP

Disclosed in certain embodiments is a method of treating or preventing an opioid-induced adverse pharmacodynamic response comprising administering to a patient in need thereof an effective amount of buprenorphine.

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12-12-2013 дата публикации

Oral formulations and lipophilic salts of methylnaltrexone

Номер: US20130330407A1
Принадлежит: WYETH LLC

The present invention provides compositions comprising methylnaltrexone or a salt thereof, and compositions and formulations thereof, for oral administration.

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23-01-2014 дата публикации

Composition for treating aids and associated conditions

Номер: US20140023731A1
Принадлежит: WILFRED RAMIX Inc

An Aids and associated conditions related to Aids treating compositions is disclosed. The compositions comprise: a medicament selected from an extract of at least one of the following plant families: Apocynaceae ( Pleioscarpa Bicarpellata ); Annonaceae ( Cleistopholis Patens ); Dichapetalaceae ( Dichapetehan Madagasca Riense ); Annoceae ( Uvaristrum Pierreanum ); Cynocynaceae ( Strophantus Gratus ); Asclepiadaceae ( Gongronema Latifolium ); Combretaceae ( Combretum Racemosum ); Apocynaceae ( Alostonia Boonei ); Amaranthaceae ( Alternanthera Pungens ); Aroceae ( Anchomanes Differmis ); Cyperaceae ( Seleria Voivinil ); Anacardiaceae ( Lannea Acida ); Bignodaceae ( Kigelia Africana ); Bombacaceae ( Ceiba Pentanota ); Anarcardiaceae ( Antrocaryon Micraster ); Bombacaceae ( Bombax Bounopozense ): Anarcardiaceae ( Spondias Mombin ); Caricaceae ( Carica Papaya ); a glyceryl ester of any of the foregoing extracts; a saponin of any of the foregoing extracts; an alkaloid of any of the foregoing extracts; a protein of any of the foregoing extracts; a fat of any of the foregoing extracts; a sugar of any of the foregoing extracts; and any mixture of any of the foregoing.

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30-01-2014 дата публикации

Dosage form containing oxycodone and naloxone

Номер: US20140031382A1
Принадлежит: Euro Celtique SA

The present invention concerns a dosage form comprising oxycodone and naloxone which is characterized by specific in vivo parameters such as t max , C max , AUCt value, mean bowel function score and/or duration of analgesic efficacy.

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06-02-2014 дата публикации

Fc Receptor-Binding Polypeptides with Modified Effector Functions

Номер: US20140038287A1
Автор: Greg Elson, Olivier Leger
Принадлежит: Novimmune SA

Disclosed are processes for producing a variant polypeptide (e.g. antibodies) having modified binding characteristics for human Fc gamma receptor IIA (CD32A) leading to increased inhibition of proinflammatory mediators while retaining binding to a target antigen via its Fv portion, which processes comprise altering the polypeptides by substitution of at least two amino acid residues at EU position 325, 326 or 328 of a human IgG CH2 region for a sequence selected from SAAF, SKAF, NAAF and NKAF. Also disclosed are molecules, particularly polypeptides, more particularly immunoglobulins (e.g. antibodies) that include a variant CDR3 region, wherein the variant CDR3 region includes at least one amino acid modified relative to a wild-type CDR3 region. The polypeptides that can be generated according to the methods of the invention are highly variable, and they can include antibodies and fusion proteins that contain an Fc region or a biologically active portion thereof.

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13-02-2014 дата публикации

Botulinum toxin compositions

Номер: US20140044695A1
Автор: Terrence J. Hunt
Принадлежит: Allergan Inc

A high potency botulinum toxin pharmaceutical composition comprising two excipients (such as albumin and sodium chloride) in a weight to weight ratio of between about 1 and about 100.

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20-02-2014 дата публикации

Modulators of atp-binding cassette transporters

Номер: US20140051724A1
Принадлежит: Vertex Pharmaceuticals Inc

The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.

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20-03-2014 дата публикации

8-azabicyclo[3.2.1]octyl-2-hydroxybenzamide compounds as mu opioid receptor antagonists

Номер: US20140080855A1
Принадлежит: Theravance Inc

The invention provides 8-azabicyclo[3.2.1]octyl-2-hydroxybenzamide compounds of formula (I): wherein R 2 , R 7 , and m are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.

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03-04-2014 дата публикации

Triazole Compounds and Methods of Making and Using the Same

Номер: US20140094422A1
Принадлежит: Melinta Therapeutics Inc

The present invention provides triazole macrocyclic compounds useful as therapeutic agents. More particularly, these compounds are useful as anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents. These compounds are represented by the following formula (I): wherein R 1 , R 2 , etc. are defined as in Claim 1.

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27-01-2022 дата публикации

Method for improving intestinal flora

Номер: US20220023396A1
Принадлежит: Amano Enzyme Inc, Hiroshima University NUC

A method for improving intestinal flora increases the number of beneficial bacteria such as lactic acid bacteria and Bifidobacterium to improve intestinal flora by using an enzyme. The method involves providing a protease, which is a polypeptide having an amino acid sequence shown in SEQ ID NO: 1 that can increase beneficial bacteria such as lactic acid bacteria and Bifidobacterium in intestines to exert an excellent effect of improving intestinal flora.

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17-01-2019 дата публикации

Use of microbial communities for human and animal health

Номер: US20190015465A1
Принадлежит: ProDigest BVBA, Universiteit Gent

The present disclosure relates to a mixture of bacteria belonging to at least six or seven different and specific bacterial species preferably for use in preventing or treating gastro-intestinal disorders. Preferably, the mixture of bacteria are grown together in a fermenter prior to administering the mixture to a subject in order to prevent or treat the disorder.

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21-01-2021 дата публикации

COMPOSITIONS AND METHODS FOR INDUCING DEFECATION

Номер: US20210015771A1
Принадлежит:

Methods, pharmaceutical formulations, and kits are provided for using capsaicin to effectuate voluntary defecation in mammals who cannot defecate without external invasion of the bowel or those who defecate involuntarily (i.e., those having fecal incontinence). The pharmaceutical formulations and kits can also be useful for inducing defecation in mammals that do not have defecation dysfunction such as, for example, in a person who is unconscious and may defecate unconsciously or in a pet at a convenient location at a specific time. The methods and compositions provide patients with defecation dysfunction control over when and where they defecate. 1. A method for inducing defecation in a mammal , comprising administering to the mammal a therapeutically effective amount of capsaicin or a pharmaceutically acceptable salt thereof , wherein the administering is by a transmucosal mode.2. The method of claim 1 , wherein the therapeutically effective amount of capsaicin or the pharmaceutically acceptable salt thereof is administered on an as-needed basis.3. The method of claim 1 , wherein the transmucosal administering comprises transrectal.4. The method of claim 3 , wherein the transrectal administering is selected from the group consisting of one or more of rectal suppositories claim 3 , capsules claim 3 , tablets claim 3 , powders claim 3 , creams claim 3 , ointments claim 3 , gels claim 3 , foams claim 3 , solutions claim 3 , emulsions claim 3 , and suspensions.5. The method of claim 1 , wherein the mammal is a human claim 1 , a cat claim 1 , or a dog.6. The method of claim 1 , wherein administering ranges from about 0 minutes to about 30 minutes prior to when the defecation is desired.7. The method of claim 6 , wherein administering ranges from about 0 minutes to about 10 minutes prior to when the defecation is desired.8. A method for treating defecation dysfunction in a mammal in need of treatment claim 6 , comprising administering to the mammal a therapeutically ...

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16-01-2020 дата публикации

Pyrrolopyrimidines as cftr potentiators

Номер: US20200017512A1
Принадлежит: Cystic Fibrosis Foundation

The present invention relates to methods of using compounds of Formula I, wherein R 1a , R 1b , R 2 , R 3 , R 4 , W, Y, and Z are as described herein, and pharmaceutically acceptable salts thereof. The compounds are potentiators of Cystic Fibrosis Transmembrane conductance Regulator (CFTR). The invention also discloses pharmaceutical compositions comprising the compound, optionally in combination with additional therapeutic agents, and methods of potentiating, in mammals, including humans, CFTR by administration of the compounds. These compounds are useful for the treatment of cystic fibrosis (CF), asthma, bronchiectasis, chronic obstructive pulmonary disease (COPD), constipation, Diabetes mellitus, dry eye disease, pancreatitis, rhinosinusitis, Sjögren's Syndrome, and other CFTR associated disorders.

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28-01-2016 дата публикации

Targeted gastrointestinal tract delivery of probiotic organisms and/or therapeutic agents

Номер: US20160022592A1
Принадлежит: Therabiome LLC

The present invention relates to the development of a targeted delivery system for the oral delivery of probiotics or therapeutic agent for various indications, including and not limited to active and prophylaxis treatment of Clostridium difficile infection, antibiotic associated diarrhea, irritable bowel syndrome, Crohn's disease, intestinal flora replacement, supplemental flora treatments for patients taking antibiotics, and for restoration of balance and signaling between the intestinal microbiome and the intestinal cells in patients under treatment of metabolic syndrome manifestations, specifically diabetes, insulin resistance, obesity, hyperlipidemia and hypertension.

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17-04-2014 дата публикации

PHARMACEUTICAL COMPOSITION FOR THE PREPARATION OF INFUSION SOLUTIONS OF ANTIMICROBIAL PREPARATIONS, ITS PRODUCTION PROCESS (variations)

Номер: US20140105936A1
Принадлежит: Individual

The proposed compositions and methods for preparation thereof relate to pharmacology, medicine, veterinary science and pharmaceutical industry. The compositions can be used for preparing infusion solutions of antimicrobial (antibacterial and antifungal) preparations increasing therapeutic efficiency thereof. The compositions include nanostructured colloidal silica and are efficient when treating overwhelming sepsis of tested animals, provoked by Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa and Candida albicans. The pharmaceutical compositions have a proven and significant clinically important potentiating impact on therapeutic efficiency of the infusion solutions, when treating inflammatory diseases, in comparison with traditional solvents. The methods include—obtaining a mixture of colloidal silica with sodium chloride or with dextrose in a certain weight ratio, which mixture includes a mass fraction of fine-dispersed particles of colloidal silica, having dimensions not exceeding 5 micrometers, and —subjecting the mixture to impacting-abrasive actions, until the mass fraction is increased at least twice.

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17-04-2014 дата публикации

Quaternary opioid carboxamides

Номер: US20140107143A1
Автор: Mark P. Wentland
Принадлежит: RENSSELAER POLYTECHNIC INSTITUTE

Compounds of formulas: are disclosed. The compounds are useful for ameliorating the side effects of therapeutic opiates.

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17-04-2014 дата публикации

Pharmaceutical composition

Номер: US20140107197A1
Принадлежит: Ferring International Center SA

A pharmaceutical composition comprising a docusate; an osmotic laxative; and a benzoate.

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25-01-2018 дата публикации

Method for selection of agents influencing intestinal motility disorders and pain

Номер: US20180023150A1
Принадлежит: BIOGAIA AB

A method is provided for evaluating agents for the treatment of different intestinal motility disorders, using distinct methodological parts related to musculature and nerves of the GI tract which communicate with the brain. In particular, the present invention provides a method for the selection of an agent effective for the treatment of an intestinal motility disorder, wherein said method comprises: a) a step of spatiotemporal (ST) mapping carried out on a gastrointestinal segment to analyse the effect of said agent on gastrointestinal motility; and b) a step of ex vivo nerve bundle recording carried out on a gastrointestinal segment to analyse the effect of said agent on mesenteric afferent nerve firing. Bacterial strains selected by the methods of the invention and the use of said bacterial strains in the treatment of intestinal motility disorders are also provided.

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10-02-2022 дата публикации

CONDENSED-CYCLIC COMPOUND

Номер: US20220041581A1
Принадлежит: Takeda Pharmaceutical Company Limited

The present invention aims to provide a compound that may be useful for the prophylaxis or treatment of constipation and the like. The present invention provides a compound represented by the formula (I): 3. The compound according to claim 1 , wherein{'sub': '2', 'X is O or CH;'}{'sup': '1', 'Ris'}(1) a 3- to 14-membered non-aromatic heterocyclic group optionally substituted by 1 to 3 hydroxy groups, or{'sub': '3-10', '(2) a Ccycloalkyl group optionally substituted by 1 to 3 hydroxy groups;'}{'sup': '2', 'Ris'}(1) a halogen atom,{'sub': '1-6', 'claim-text': (a) a halogen atom,', {'sub': '1-6', '(b) a Calkoxy group,'}, {'sub': '1-6', '(c) a Calkylthio group,'}, {'sub': '3-10', '(d) a Ccycloalkyl group,'}, {'sub': '6-14', '(e) a Caryl group, and'}, {'sub': '1-6', '(f) a 3- to 14-membered non-aromatic heterocyclic group optionally substituted by 1 to 3 Calkyl groups, or'}], '(2) a Calkoxy group optionally substituted by 1 to 3 substituents selected from'}(3) a hydroxy group; andring A is (a) a halogen atom,', {'sub': '1-6', 'claim-text': (i) a halogen atom,', '(ii) a cyano group,', '(iii) a hydroxy group,', {'sub': 1-6', '1-6, '(iv) a Calkoxy group optionally substituted by 1 to 3 substituents selected from a halogen atom and a Calkoxy group,'}, {'sub': '3-10', '(v) a Ccycloalkyl group,'}, '(vi) a 3- to 14-membered non-aromatic heterocyclic group,', {'sub': 6-14', '1-6', '1-6, '(vii) a Caryl group optionally substituted by 1 to 3 substituents selected from a hydroxy group, a Calkylthio group and a Calkylsulfonyl group,'}, {'sub': '1-6', '(viii) a 5- to 14-membered aromatic heterocyclic group optionally substituted by 1 to 3 Calkoxy groups,'}, {'sub': '1-6', '(ix) a Calkoxy-carbonyl group,'}, {'sub': '1-6', '(x) a Calkylthio group,'}, {'sub': '1-6', '(xi) a Calkylsulfonyl group,'}, {'sub': '1-6', '(xii) a mono- or di-Calkyl-carbamoyl group,'}, '(xiii) a 3- to 14-membered non-aromatic heterocyclylcarbonyl group, and', {'sub': '1-6', '(xiv) a Calkyl-carbonylamino group ...

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29-01-2015 дата публикации

Modulators of atp-binding cassette transporters

Номер: US20150031722A1
Принадлежит: Vertex Pharmaceuticals Inc

The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.

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31-01-2019 дата публикации

Drug delivery device employing wicking release window

Номер: US20190030306A1
Принадлежит: Auritec Pharmaceuticals

The present invention provides for a drug delivery device. The device can comprise at least one core with a first active pharmaceutical ingredient (API), coated with a first layer that is permeable or semi-permeable to the API, coated with a second layer that is impermeable to the API, and having a delivery window to allow passage of the API through the device and into body fluids or tissues. The device can also have a wicking material to modify the rate of transport of the API into the body fluid or tissues.

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30-01-2020 дата публикации

PROBIOTICS COMPOSITION CONTAINING HERICIUM ERINACEUS

Номер: US20200030395A1
Автор: Lee Dae Hee, Lee Jae Kang
Принадлежит:

The present invention relates to a probiotics composition containing: lactic acid bacteria powder comprising lactic acid bacteria selected from the group consisting of , and ; a mushroom extract; and a fructooligosaccharide. 115-. (canceled)16Bifidobacterium lactis, Bifidobacterium longum, Lactobacillus acidophilus, Lactobacillus plantarumLactobacillus rhamnosus. A method for ameliorating constipation , the method including orally-administering a probiotics composition to a subject , wherein the probiotics composition contains: lactic acid bacteria powders containing lactic acid bacteria selected from a group consisting of , and ; a mushroom extract; and a fructooligosaccharide.17Bifidobacterium lactis. The method for ameliorating constipation of claim 16 , wherein the probiotics composition further contains -containing double-micro capsule powders.18Lactobacillus acidophilusLactobacillus acidophilus. The method for ameliorating constipation of claim 16 , wherein the includes CBG-C13 (Deposition Number KACC 91980P).19Lactobacillus rhamnosusLactobacillus rhamnosus. The method for ameliorating constipation of claim 16 , wherein the includes CBG-C14 (Deposition Number KACC 91981P).20Bifidobacterium lactisBifidobacterium lactis. The method for ameliorating constipation of claim 16 , wherein the lactic acid bacteria powders contains present in a form of a double-micro capsule and being not present in a form of a double-micro capsule at a weight ratio of 1:0.5 to 1.5.21hericium erinaceus. The method for ameliorating constipation of claim 16 , wherein the mushroom extract includes a extract.22hericium erinaceus. The method for ameliorating constipation of claim 16 , wherein the mushroom extract includes a fruit body extract.23Lactococuus lactis, Enterococcus faecium, Enterococcus faecalis, Streptococcus thermophilus, Bifidobacterium bifidum Bifidobacterium breve, Bifidobacterium animalislactis, Lactobacillus casei, Lactobacillus gasseri, Lactobacillus delbrueckiibulgaricus ...

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31-01-2019 дата публикации

Cftr regulators and methods of use thereof

Номер: US20190031622A1
Принадлежит: UNIVERSITY OF CALIFORNIA

Provided herein are compounds that activate CFTR and methods for treating constipation, dry eye disorders, and other diseases and disorders.

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31-01-2019 дата публикации

CFTR REGULATORS AND METHODS OF USE THEREOF

Номер: US20190031630A1
Принадлежит:

Provided herein are compounds that activate CFTR and methods for treating constipation, dry eye disorders or other diseases and disorders. 26-. (canceled)814-. (canceled)1619-. (canceled)2123-. (canceled)25. (canceled)27. (canceled)29. (canceled)3144-. (canceled)4648-. (canceled) This application claims the benefit of U.S. Provisional Application No. 62/387,591, filed Dec. 24, 2015, the contents of which is incorporated herein in its entirety and for all purposes.This invention was made with the government support under Grant Nos. TR000004, EY023981, EY013574, EB000415, DK035124, DK072517 and DK101373, awarded by the National Institutes of Health. The government has certain rights in the invention.Constipation is a common clinical complaint in adults and children that negatively impacts quality of life. The prevalence of chronic constipation has been estimated to be 15% in the U.S. population, with health-care costs estimated at approximately 7 billion dollars annually, with in excess of 500 million dollars spent on laxatives. The mainstay of constipation therapy includes laxatives and many of them are available over the counter (soluble fiber, polyethylene glycol, probiotics, etc.). There are two FDA-approved chloride channel activators, lubiprostone and linaclotide, for treatment of constipation, but clinical trials showed variable and unimpressive efficacy of both drugs. Despite the wide range of therapeutic options, there is a continued need for safe and effective drugs to treat constipation.Dry eye is a heterogeneous tear film disorder that results in eye discomfort, visual disturbance, and ocular surface pathology, and remains an unmet need in ocular disease with limited effective therapeutic options available. Dry eye is a major public health concern in an aging population, affecting up to one-third of the global population, including 5 million Americans aged 50 and over. Over-the-counter artificial tears and implantable punctal plugs are frequently used for ...

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04-02-2021 дата публикации

COMPOSITION FOR IMPROVING QUANTITY OF TEAR FLUID, COMPOSITION FOR IMPROVING CONSTIPATION, AND COMPOSITION FOR IMPROVING SKIN QUALITY

Номер: US20210030830A1
Принадлежит:

The present invention relates to a composition for improving the quantity of tear fluid, a composition for improving constipation, and a composition for improving skin quality. By containing the extract of Black ginger ()), it is possible that the quantity of tear fluid, constipation, and skin quality are improved. 1Kaempferia parviflora. A composition for improving the quantity of tear fluid comprising an extract of Black ginger ().2Kaempferia parviflora. A composition for improving constipation comprising an extract of Black ginger ().3Kaempferia parviflora. A composition for improving skin quality comprising an extract of Black ginger ().4. The composition according to claim 1 , which the composition is a food composition. The present invention is related to a composition for improving the quantity of tear fluid, a composition for improving constipation, and a composition for improving skin quality.Black ginger () is a plant in the genus of the plant family Zingiberaceae, which is known as Thai or Kra chai dahm.Black ginger is cultivated widely in Thai where it is the place of origin, and it is taken on a daily basis from old times. It is used for nourishing tonic, increasing energy, lowering a blood-sugar level, physical recovery, and recovering circulatory organs.In recent years, many effects of Black ginger () are reported such as fat decomposition-promoting action (NON-PATENT DOCUMENT 1, NON-PATENT DOCUMENT 2, PATENT DOCUMENT 1), anti-inflammatory action (NON-PATENT DOCUMENT 3), activation effect for a longevity gene (NON-PATENT DOCUMENT 4, PATENT DOCUMENT 2), anti-saccharification action (NON-PATENT DOCUMENT 4, NON-PATENT DOCUMENT 5), antiallergic action (NON-PATENT DOCUMENT 6), xanthine oxidase inhibition action (PATENT DOCUMENT 3), AMPK activation effect (PATENT DOCUMENT 4), production-inhibiting activity for TNF-a and IL-6 (PATENT DOCUMENT 5), energy metabolism promoting action in muscle cells (PATENT DOCUMENT 6), reinforcement effect for muscle amount ...

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04-02-2021 дата публикации

COMPOSITION AND METHOD FOR IMPROVING QUANTITY OF TEAR FLUID, COMPOSITION, TREATING CONSTIPATION AND IMPROVING SKIN QUALITY

Номер: US20210030831A1
Принадлежит:

The present invention relates to a composition and method for improving the quantity of tear fluid, a composition and method for treating constipation, and a composition and method for improving skin quality. By utilizing an extract of Black ginger ()), the quantity of tear fluid, constipation, and skin quality are improved 1Kaempferia parviflora.. A composition for improving the quantity of tear fluid comprising a pharmalogically effective amount of an extract of2Kaempferia parviflora.. A composition for improving constipation comprising a pharmalogically effective amount of an extract of3Kaempferia parviflora.. A composition for improving skin quality comprising a pharmalogically effective amount of an extract of4. The composition according to claim 1 , wherein the composition is a food composition claim 1 , a pharmaceutical composition claim 1 , or a cosmetic composition.5. A method of improving the quantity of tear fluid in a subject comprising the step of administering the composition of to the subject.6Kaempferia parviflora. The method of claim 5 , wherein the amount of the extract of in the composition administered is 100 mg per day for an adult.7. The method of claim 5 , wherein the composition is administered in a food composition or a pharmaceutical composition.8. A method of treating constipation in a subject comprising the step of administering the composition of to the subject.9. A method of improving skin quality in a subject comprising the step of administering the composition of to the subject. This application is a continuation-in-part of U.S. application Ser. No. 16/727,411, filed Dec. 26, 2019, which claims the benefit of Japanese Application No. 2019-141840, filed Jul. 31, 2019, hereby incorporated herein by reference.The present invention is related to a composition and method for improving the quantity of tear fluid, a composition and method for treating constipation, and a composition and method for improving skin quality.Black ginger () is a ...

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09-02-2017 дата публикации

Delayed release drug formulation

Номер: US20170035698A1
Принадлежит: Tillotts Pharma AG

In a delayed release formulation comprising a core containing a drug and a delayed release coating for providing intestinal release, release of the drug in the colon is accelerated by including an isolation layer between the core and the delayed release coating. The delayed release coating comprises an inner layer and an outer layer. The outer layer comprises a pH dependently soluble polymeric material which has a pH threshold at about pH 5 or above. The inner layer comprises a soluble polymeric material which is soluble in intestinal fluid or gastrointestinal fluid, said soluble polymeric material being selected from the group consisting of a polycarboxylic acid polymer that is at least partially neutralised, and a non-ionic polymer, provided that, where said soluble polymeric material is a non-ionic polymer, said inner layer comprises at least one additive selected from a buffer agent and a base.

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24-02-2022 дата публикации

4-(3-cyanophenyl)-6-pyridinylpyrimidine mglu5 modulators

Номер: US20220056009A1
Принадлежит: Heptares Therapeutics Ltd

The disclosures herein relate to novel compounds of formulawherein R1, R2, R3 and R4 and n are defined herein, and their use in treating, preventing, ameliorating, controlling or reducing the risk of inflammation, neurological or psychiatric disorders associated with modulating mGlu5 receptor function.

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06-02-2020 дата публикации

METHODS OF TREATING CONSTIPATION USING AMINOSTEROL COMPOSITIONS

Номер: US20200038414A1
Принадлежит: Enterin, Inc.

This invention relates to methods of treating constipation and constipation-related symptoms in a subject in need. The methods, which utilize a patient-specific “fixed dose” of an aminosterol, comprise administering a therapeutically effective dose of an aminosterol to a subject in need. 1. A method of treating , preventing , and/or slowing the onset or progression of constipation and/or a constipation-related symptom in a subject in need comprising administering to the subject a therapeutically effective amount of at least one aminosterol , or a salt or derivative thereof , provided that the administering does not comprise oral administration.2. The method of claim 1 , wherein administering comprises administration selected from nasal claim 1 , sublingual claim 1 , buccal claim 1 , rectal claim 1 , vaginal claim 1 , intravenous claim 1 , intra-arterial claim 1 , intradermal claim 1 , intraperitoneal claim 1 , intrathecal claim 1 , intramuscular claim 1 , epidural claim 1 , intracerebral claim 1 , intracerebroventricular claim 1 , transdermal claim 1 , or any combination thereof.3. The method of claim 1 , wherein administering comprises nasal administration.4. The method of claim 1 , wherein the therapeutically effective amount of the at least one aminosterol or a salt or derivative thereof:(a) comprises about 0.1 to about 20 mg/kg body weight of the subject; and/or(b) comprises about 0.1 to about 15 mg/kg body weight of the subject; and/or(c) comprises about 0.1 to about 10 mg/kg body weight of the subject; and/or(d) comprises about 0.1 to about 5 mg/kg body weight of the subject; and/or(e) comprises about 0.1 to about 2.5 mg/kg body weight of the subject; and/or(f) comprises about 0.001 to about 500 mg/day; and/or(g) comprises about 0.001 to about 250 mg/day; and/or(h) comprises about 0.001 to about 125 mg/day; and/or(i) comprises about 0.001 to about 50 mg/day; and/or(j) comprises about 0.001 to about 25 mg/day; and/or(k) comprises about 0.001 to about 10 mg/day; ...

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06-02-2020 дата публикации

Crystalline polymorphs of a muscarinic acetylcholine receptor agonist

Номер: US20200040007A1
Принадлежит: Nsc Therapeutics GmbH

Provided are novel crystalline forms of a spiro-compound which acts as a muscarinic acetylcholine receptor agonist. In particular, isolated crystalline polymorphs of (S)-2-ethyl-8-methyl-1-thia-4,8-diazaspiro[4.5]decane-3-one are described which have favorable properties in pharmaceutical manufacture. Also provided are methods to prepare said crystalline polymorphs, and to convert them into each other as well as methods for preparing medicaments containing the same which are suitable for use in the treatment of diseases and disorders that respond to modulation of the muscarinic acetylcholine receptor.

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16-02-2017 дата публикации

Macrocyclic ghrelin receptor modulators and methods of using the same

Номер: US20170042858A1
Принадлежит: Ocera Therapeutics Inc

The present invention provides novel conformationally-defined macrocyclic compounds that can function as selective modulators of the ghrelin receptor (growth hormone sceretagogue receptor, GHS-R1a and subtypes, isoforms and variants thereof). Methods of synthesizing the novel compounds are also described herein. These compounds are useful as agonists of the ghrelin receptor and as medicaments for treatment and prevention of a range of medical conditions including, but not limited to, metabolic and/or endocrine disorders, gastrointestinal disorders, cardiovascular disorders, obesity and obesity-associated disorders, central nervous system disorders, bone disorders, genetic disorders, hyperproliferative disorders and inflammatory disorders.

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16-02-2017 дата публикации

Selective Opioid Compounds

Номер: US20170042882A1
Принадлежит: Alkermes Inc

The present invention relates to compounds of Formula I or II, or pharmaceutically acceptable salts, esters, or prodrugs thereof: which relates to mophinan compounds useful as μ, δ and/or κ receptor opioid compounds and pharmaceuticals containing same that may be useful for mediating analgesia, combating drug addiction, alcohol addiction, drug overdose, mental illness, bladder dysfunctions, neurogenic bladder, interstitial cystitis, urinary incontinence, premature ejaculation, inflammatory pain, peripherally mediated and neuropathic pain, cough, lung edema, diarrhea, cardiac disorders, cardioprotection, depression, and cognitive, respiratory, diarrhea, irritable bowel syndrome and gastro-intestinal disorders, immunomodulation, and anti-tumor agents.

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16-02-2017 дата публикации

Magnesium oxide granules for pharmaceutical applications or for use as food additives

Номер: US20170042935A1
Автор: Kensho Sakamoto
Принадлежит: Konoshima Chemical Co Ltd

An object of the present invention is to provide magnesium oxide that can be preferably used for pharmaceutical applications or as a food additive. In particular, the object is to provide magnesium oxide granules with which tableting problems and quality defects can be reduced, and in more particular, to provide magnesium oxide granules with which tableting problems and quality defects can be reduced and which has less heavy metal incorporation and high purity of magnesium oxide. Provided are magnesium oxide granules for pharmaceutical applications or for addition to food having a BET specific surface area of 7 to 50 m 2 /g and CAA80/CAA40 of 2 to 7.

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22-02-2018 дата публикации

Enzymatic synthesis of soluble glucan fiber

Номер: US20180049457A1
Принадлежит: EI Du Pont de Nemours and Co

An enzymatically produced soluble α-glucan fiber composition is provided suitable for use as a digestion resistant fiber in food and feed applications. The soluble α-glucan fiber composition can be blended with one or more additional food ingredients to produce fiber-containing compositions. Methods for the production and use of compositions comprising the soluble α-glucan fiber are also provided.

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20-02-2020 дата публикации

Pharmaceutical formulation

Номер: US20200054550A1
Принадлежит: KLARIA PHARMA HOLDING AB

The present invention relates to a film comprising an alginate salt of a monovalent cation or a mixture of alginate salts containing at least one alginate salt of a monovalent cation, and a triptan or a pharmaceutically acceptable salt thereof. The present invention further relates to methods for manufacturing such a film, and the use of such a film in the treatment of disease in a human patient, in particular migraine with or without aura, cluster headache, or trigeminal neuralgia.

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05-03-2015 дата публикации

Modulators of atp-binding cassette transporters

Номер: US20150065487A1
Принадлежит: Vertex Pharmaceuticals Inc

The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.

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10-03-2016 дата публикации

Ask 1 inhibiting pyrrolopyrimidine derivatives

Номер: US20160067251A1
Принадлежит: Calchan Ltd

This invention relates to pyrrolopyrimidine derivatives of formula (I): where R 1 , X, p, R 4 , R 2 and R 3 are as defined herein, and their use as pharmaceuticals.

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17-03-2022 дата публикации

CFTR REGULATORS AND METHODS OF USE THEREOF

Номер: US20220081402A1
Принадлежит:

Provided herein are compounds that activate CFTR and methods for treating constipation, dry eye disorders, and other diseases and disorders. 2. The method of claim 1 , wherein Ris —CHor —CHCH.3. The method of claim 1 , wherein Ris C-Chaloalkyl substituted with at least four fluorines.4. The method of claim 3 , wherein Ris —CH(CF)or —CH-CF—CHF.6. The method of claim 5 , wherein the dry eye disorder is a lacrimal gland disorder.7. The method of claim 5 , further comprising administering to the subject an anti-dry eye agent.9. The method of claim 8 , wherein Ris —CHor —CHCH.10. The method of claim 8 , wherein Ris C-Chaloalkyl substituted with at least four fluorines.11. The method of claim 10 , wherein Ris —CH(CF)or —CH-CF—CHF.14. The method of claim 13 , wherein Ris —CHor —CHCH.15. The method of claim 13 , wherein Ris C-Chaloalkyl substituted with at least four fluorines.16. The method of claim 15 , wherein Ris —CH(CF)or —CH-CF—CHF. This application is a continuation application of U.S. application Ser. No. 16/785,417, filed Feb. 7, 2020; which is is a divisional application of U.S. application Ser. No. 16/016,290, filed on Jun. 22, 2018, now U.S. Pat. No. 10,604,492; which is a national stage application of International Application No. PCT/US2016/068569, filed on Dec. 23, 2016; which claims priority from U.S. Provisional Application No. 62/387,590, filed on Dec. 24, 2015, the entire contents of which are incorporated herein by reference in their entirety and for all purposes.This invention was made with government support under Grant Nos. TR000004, EY023981, EY013574, EB000415, DK035124, DK072517 and DK101373, awarded by the National Institutes of Health. The government has certain rights in the invention.Constipations a common clinical complaint in adults and children that negatively impacts quality of life. The prevalence of chronic constipation has been estimated to be 15% in the U.S. population, with health-care costs estimated at approximately 7 billion dollars ...

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08-03-2018 дата публикации

Treatment of symptoms related to neurodegenerative disorders through pharmacological dermal activation of cranial nerves

Номер: US20180064728A1
Принадлежит: Glia LLC

A method for treating a symptom of a neurodegenerative condition. The method includes topically administering a composition that contains a sex steroid or a cannabinoid or a mixture of both to the forehead, to an area of the outer ear of the subject not including the ear canal, or to both of these anatomical locations. The symptom treatable by the method is a motor symptom or a non-motor symptom.

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19-03-2015 дата публикации

Spirocyclic compounds as tryptophan hydroxylase inhibitors

Номер: US20150080393A1

The present invention is directed to spirocyclic compounds which are inhibitors of tryptophan hydroxylase (TPH), particularly isoform 1 (TPH1), that are useful in the treatment of diseases or disorders associated with peripheral serotonin including, for example, gastrointestinal, cardiovascular, pulmonary, inflammatory, metabolic, and low bone mass diseases, as well as serotonin syndrome, and cancer.

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05-06-2014 дата публикации

Modulators of atp-binding cassette transporters

Номер: US20140155431A1
Принадлежит: Vertex Pharmaceuticals Inc

The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.

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24-03-2016 дата публикации

Polymorph forms

Номер: US20160083381A1
Принадлежит: Raqualia Pharma Inc

The present invention relates to novel crystal forms of 2-amino-N-[2-(3a-(R)-benzyl-2-methyl-3-oxo-2,3,3a,4,6,7-hexahydro-pyrazolo[4,3-c]pyridin-5-yl)-1-(R)-benzyloxymethyl-2-oxo-ethyl]-isobutyramide L-tartrate. More particularly, the invention relates to polymorph forms, and to processes for the preparation of compositions containing and to uses of such polymorph forms.

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23-03-2017 дата публикации

Benzisoxazole derivative salt

Номер: US20170081318A1
Принадлежит: Raqualia Pharma Inc

Salts of 4-{[4-({[4-(2,2,2-trifluoroethoxy)-1,2-benzisoxazol-3-yl]oxy}methyl)piperidin-1-yl]methyl}tetrahydro-2H-pyran-4-carboxylic acid are disclosed. More particularly, salt forms (HCl-salt, HBr-salt, p-toluenesulfonate salt and ethanedisulfonate salt) are disclosed. Furthermore, processes for the preparation of such salt forms, compositions containing such salt forms, and uses of such salt forms are disclosed. A method of treating disease conditions mediated by 5-HT4 receptor activity includes administering an effective amount of such salt forms to an animal, including a human, in need of such treatment.

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19-06-2014 дата публикации

Engineered anti-il-23r antibodies

Номер: US20140170154A1
Автор: Leonard G. Presta
Принадлежит: Merck Sharp and Dohme LLC

Antibodies to human IL-23R are provided, as well as uses thereof, e.g. in treatment of inflammatory, autoimmune, and proliferative disorders.

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28-03-2019 дата публикации

Desmoglein 2 (DSG2) Binding Proteins and Uses Therefor

Номер: US20190092819A1
Автор: Andre Lieber, Hongjie Wang

The present invention provides recombinant adenoviral compositions and methods for their use in treating disorders associated with epithelial tissues.

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02-06-2022 дата публикации

CANNABINOID GLYCOSIDE PRODRUGS AND METHODS OF SYNTHESIS

Номер: US20220168428A1
Принадлежит: Graphium Biosciences, Inc.

The present invention relates to cannabinoid glycoside prodrugs suitable for site- and tissue-specific delivery of cannabinoid molecules. The present invention also relates to methods of forming the cannabinoid glycoside prodrugs through glycosyltransferase mediated glycosylation of cannabinoid molecules. 3. A compound according to claim 2 , wherein A is A′.411.-. (canceled)12. A compound according to claim 2 , wherein A is A″.1320.-. (canceled)21. A compound according to claim 2 , wherein A is A′″.2228.-. (canceled)29. A pharmaceutical composition comprising a compound as defined in and a pharmaceutically acceptable carrier claim 1 , diluent claim 1 , excipient claim 1 , or adjuvant.30. A method for the site-specific delivery of a cannabinoid drug to a subject claim 1 , comprising the step of administering a cannabinoid glycoside prodrug as defined in to a subject in need thereof.31. The method of claim 30 , wherein the cannabinoid glycoside prodrug is formulated for oral claim 30 , parenteral claim 30 , or transdermal administration.32. (canceled)33. (canceled)34. A method for the site-specific delivery of a cannabinoid drug to a subject claim 29 , comprising the step of administering a pharmaceutical composition as defined in to a subject in need thereof.35. The method of claim 34 , wherein the pharmaceutical composition is formulated for oral claim 34 , parenteral claim 34 , or transdermal administration.36. (canceled)37. (canceled)38. A method for facilitating the transport of a cannabinoid drug across the blood brain barrier of a subject comprising administering a cannabinoid glycoside prodrug as defined in to a subject in need thereof.39. An antimicrobial agent comprising an effective amount of a cannabinoid glycoside prodrug as defined in .40. (canceled)41. A detersive agent comprising an effective amount of a cannabinoid glycoside prodrug as defined in .42. (canceled)43. A method of producing a cannabinoid glycoside claim 1 , comprising incubating a ...

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19-04-2018 дата публикации

METHODS OF TREATMENT COMPRISING ADMINISTERING A HIGH DAILY DOSE OF OXYCODONE AND NALOXONE IN A 2:1 WEIGHT RATIO

Номер: US20180104236A1
Принадлежит:

The present invention relates to methods of treatment comprising, inter alia, administering a high daily dose of oxycodone, such as a daily dose of at least 90 mg oxycodone, and naloxone in a 2:1 weight ratio to a patient in need thereof. 1. A method of improving , maintaining , or normalizing bowel function in a patient on opioid therapy comprising orally administering the patient a daily dose comprising oxycodone or a pharmaceutically acceptable salt thereof and naloxone or a pharmaceutically acceptable salt thereof in a 2:1 weight ratio; whereinthe daily dose comprises at least 90 mg of the oxycodone or pharmaceutically acceptable salt thereof; andthe daily dose is administered as two or more prolonged release oral dosage forms.2. (canceled)3. A method of treating pain comprising orally administering to a patient in need thereof a daily dose comprising oxycodone or a pharmaceutically acceptable salt thereof and naloxone or a pharmaceutically acceptable salt thereof in a 2:1 weight ratio; whereinthe daily dose comprises at least 90 mg of the oxycodone or pharmaceutically acceptable salt thereof;the daily dose is administered as two or more prolonged release oral dosage forms; andthe method improves, maintains, or normalizes the bowel function of the patient.4. The method of claim 3 , wherein the improvement in claim 3 , maintenance of claim 3 , or normalization of bowel function is assessed by the difference in bowel function index (BFI) scores following administering the daily dose and a corresponding naloxone-free daily dose claim 3 , and wherein the difference in BFI scores is at least 12.56-. (canceled)7. The method of claim 4 , wherein the difference in BFI scores is at least 18.8. The method of claim 4 , wherein the BFI scores are measured by taking the mean symptom scores of ease of defecation claim 4 , feeling of incomplete bowel evacuation claim 4 , and judgment of constipation.9. The method of claim 3 , wherein improving maintaining claim 3 , or ...

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03-07-2014 дата публикации

7,8-Cyclicmorphinan Analogs

Номер: US20140187571A1
Принадлежит: Purdue Pharma LP

The application is directed to compounds of Formula I-A and pharmaceutically acceptable salts and solvates thereof, wherein Cy, R 1a -R 3a , R 4a , and R 4b are defined as set forth in the specification. The invention is also directed to use of compounds of Formula I-A to treat disorders responsive to the modulation of one or more opioid receptors, or as synthetic intermediates. Certain compounds of the present invention are especially useful for treating pain.

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29-04-2021 дата публикации

Metformin compounded composition and method thereof

Номер: US20210121419A1
Автор: Xinli Lin
Принадлежит: Zhoushan Tritech Biosciences Inc

The present disclosure is related to a metformin compounded composition and application thereof. The disclosure provides active ingredients of composition dosage forms, comprising active ingredients including metformin, omega-3 fatty acid, statin, and vitamins. The whole or part of the active ingredients can be manufactured into a single dosage form for preventing or treating a special disease or enhance health in general. The diseases that can be prevented or treated include cardiovascular diseases, nervous system diseases, cancer, diabetes, autoimmune diseases, or any other diseases that can be treated with the provided formulations. Because of the broad applicability for preventing diseases and enhancing health, the application of the invented formulation may provide “health and longevity” for general population.

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29-04-2021 дата публикации

OPIOID RECEPTOR ANTAGONIST CONJUGATE AND USE THEREOF

Номер: US20210121455A1
Автор: HE Mei
Принадлежит: SHANGHAI HANMAI BIO-PHARMA CO., LTD.

The present invention relates to an opioid receptor antagonist conjugate and a use thereof. In particular, the present invention relates to a covalent coupling conjugate of a hydrophilic polymer and an opioid receptor antagonist and the use thereof. 1. A conjugate as represented by formula (I) or a pharmaceutically acceptable salt thereof:{'br': None, 'i': 'm', 'P—(W)\u2003\u2003 (I)'} W is a non-naloxone opioid receptor antagonist; and', 'm is a natural number between 1 and 10., 'wherein, P is a hydrophilic polymer;'}2. The conjugate according to claim 1 , wherein the hydrophilic polymer is polyethylene glycol.3. The conjugate according to claim 1 , wherein the hydrophilic polymer is a polyethylene glycol having 2 to 45 —CHCHO— structural unit claim 1 , preferably the polyethylene glycol having 2 to 40 —CHCHO— structural unit claim 1 , preferably the polyethylene glycol having 2 to 30 —CHCHO— structural unit claim 1 , preferably the polyethylene glycol having 2 to 20 —CHCHO— structural unit claim 1 , preferably the polyethylene glycol having 2 to 10 —CHCHO— structural unit claim 1 , and more preferably the polyethylene glycol having 2 to 8 —CHCHO— structural unit.4. The conjugate according to claim 3 , wherein the polyethylene glycol is a monodisperse polyethylene glycol.5. The conjugate according to claim 1 , wherein the non-naloxone opioid receptor antagonist is derived from a compound selected from the group consisting of 6-amino-14-hydroxy-17-allyl norfloxacin morphine claim 1 , naltrel claim 1 , naltrexone claim 1 , N-methylnaltrexone claim 1 , nalmefene claim 1 , nalbuphine claim 1 , butorphanol claim 1 , cyclozocine claim 1 , pentazocine claim 1 , nalorphine claim 1 , naltrindole claim 1 , nobelnatofimin claim 1 , oxilorphan claim 1 , levallorphan claim 1 , methylnaltrexone claim 1 , buprenorphine claim 1 , seklowan claim 1 , oxymorphone claim 1 , codeine claim 1 , oxycontin claim 1 , morphine claim 1 , ethylmorphine hydrochloride claim 1 , diacetylmorphine ...

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20-04-2017 дата публикации

Azamorphinan derivatives and use thereof

Номер: US20170107220A1
Принадлежит: Purdue Pharma LP

The application is directed to compounds of Formula (I) and pharmaceutically acceptable salts and solvates thereof, wherein R 1 , R 2 , R 3 , R 4 , Y, and Z are defined as set forth in the specification. The invention is also directed to use of compounds of any one of Formulae I-VIII, and the pharmaceutically acceptable salts and solvates thereof, to treat disorders responsive to the modulation of one or more opioid receptors, or as synthetic intermediates. Certain compounds of the invention are especially useful for treating pain.

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11-04-2019 дата публикации

INTESTINAL FLORA IMPROVEMENT AGENT

Номер: US20190105376A1
Принадлежит:

The purpose of the present invention is to provide an agent for improving intestinal flora which can increase the number of beneficial bacteria such as lactic acid bacteria and to improve intestinal flora by using an enzyme. A protease consisting of a polypeptide having an amino acid sequence shown in SEQ ID NO: 1 can increase beneficial bacteria such as lactic acid bacteria and in intestines to exert an excellent effect of improving intestinal flora. 1. An agent for improving intestinal flora comprising a protease comprising at least one of the following polypeptides (1) to (3) as an active ingredient:(1) a polypeptide consisting of an amino acid sequence shown in SEQ ID NO: 1,(2) a polypeptide comprising an amino acid sequence in which one or a few amino acids are substituted, added, inserted, or deleted in the amino acid sequence shown in SEQ ID NO: 1, and having a protease activity equivalent to that of a polypeptide consisting of an amino acid sequence shown in SEQ ID NO: 1, and(3) a polypeptide comprising an amino acid sequence having 80% or more sequence identity to an amino acid sequence shown in SEQ ID NO: 1, and having a protease activity equivalent to that of a polypeptide consisting of an amino acid sequence shown in SEQ ID NO: 1.2. A drug for oral administration for improving intestinal flora claim 1 , comprising an agent for improving intestinal flora according to .3. A food additive for improving intestinal flora claim 1 , comprising an agent for improving intestinal flora according to .4. Food or drink for improving intestinal flora claim 1 , comprising an agent for improving intestinal flora according to .5. A method for improving intestinal flora claim 1 , comprising orally applying a protease comprising at least one of the following polypeptides (1) to (3) to a person who requires improvement of intestinal flora:(1) a polypeptide consisting of an amino acid sequence shown in SEQ ID NO: 1,(2) a polypeptide comprising an amino acid sequence in which ...

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13-05-2021 дата публикации

HETEROCYCLIC COMPOUND

Номер: US20210139491A1
Принадлежит:

The present invention aims to provide a compound that may be useful for the prophylaxis or treatment of constipation and the like. The present invention provides a compound represented by the following formula (I): 2. The compound according to claim 1 , wherein{'sup': '1', 'claim-text': (1) an optionally substituted 3- to 14-membered non-aromatic heterocyclic group, or', {'sub': '3-10', '(2) an optionally substituted Ccycloalkyl group;'}], 'Ris'}{'sup': '2', 'sub': '1-6', 'Ris a hydrogen atom or an optionally substituted Calkyl group;'} (1) an optionally further substituted benzene ring,', '(2) an optionally further substituted 5- or 6-membered monocyclic aromatic heterocycle,', '(3) an optionally further substituted 4- to 6-membered monocyclic non-aromatic heterocycle, or', '(4) an optionally further substituted 9- to 14-membered fused polycyclic non-aromatic heterocycle; and, 'ring A is'}{'sup': 3', '4, 'sub': '1-6', 'Rand Rare each independently a hydrogen atom, a halogen atom or an optionally substituted Calkyl group,'}or a salt thereof.3. The compound according to claim 1 , wherein{'sup': '1', 'claim-text': (1) a 3- to 14-membered non-aromatic heterocyclic group optionally substituted by 1 to 3 hydroxy groups, or', {'sub': '3-10', '(2) a Ccycloalkyl group optionally substituted by 1 to 3 substituents selected from a hydroxy group and a halogen atom;'}], 'Ris'}{'sup': '2', 'sub': '1-6', 'Ris a hydrogen atom or a Calkyl group;'} [{'sub': 1-6', '1-6', '1-6', '3-10', '6-14', '1-6', '1-6', '1-6', '3-10', '6-14', '1-6, '(1) a benzene ring optionally further substituted by 1 to 3 substituents selected from (a) a halogen atom, (b) a Calkoxy group, (c) a mono- or di-Calkyl-carbamoyl group optionally substituted by 1 or 2 substituents selected from (i) a Calkoxy group, (ii) a Ccycloalkyl group, (iii) a 3- to 14-membered non-aromatic heterocyclic group, (iv) a Caryl group optionally substituted by 1 to 3 hydroxy groups, (v) a Calkoxy-carbonyl group, (vi) a carboxy group, ...

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17-07-2014 дата публикации

Treating inflammation with a binding system

Номер: US20140199412A1
Автор: Alexander L. Huang, Gin Wu
Принадлежит: LiveLeaf Inc

The teachings provided herein generally relate to site-activated binding systems that selectively increase the bioactivity of phenolic compounds at target sites. More particularly, the systems taught here include a phenolic compound bound to a reactive oxygen species, wherein the phenolic compound and the reactive oxygen species react at a target area in the presence of an oxidoreductase enzyme.

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16-04-2020 дата публикации

Agonists of guanylate cyclase useful for downregulation of pro-inflammatory cytokines

Номер: US20200113968A1
Автор: Kunwar Shailubhai
Принадлежит: Bausch Health Ireland Ltd

This invention provides a method to prevent, control, and/or treat an inflammatory disease or disorder by administering at least one agonist of guanalyte cyclase receptor, or pharmaceutical compositions thereof, either alone or either concurrently or sequentially with another compound or an active agent used to treat the disease or disorder, and/or with an inhibitor of cGMP-dependent phosphodieasterases.

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01-09-2022 дата публикации

PLUM EXTRACT AND METHOD FOR IMPROVING PHYSICAL FUNCTION WITH THE SAME

Номер: US20220273749A1
Принадлежит:

Provided is a method for improving physical function, including administering to a subject in need thereof a composition including a plum extract extracted from unripe green plums that are harvested within two to three months after flowering. The plum extract is used for inhibiting accumulation of lipid droplets in cells, increasing a metabolic rate, improving gastrointestinal function, and reducing a weight and/or a waist circumference. 1. A method for improving physical function , comprising administering to a subject in need thereof a composition comprising a plum extract extracted from unripe green plums that are harvested within two to three months after flowering.2. The method according to claim 1 , wherein the improving physical function involves increasing an expression level of a fat loss-related gene in the subject claim 1 , the fat loss-related gene comprises LIPE gene.3. The method according to claim 2 , wherein the improving physical function involves inhibiting accumulation of lipid droplets in cells of the subject.4. The method according to claim 2 , wherein the improving physical function involves increasing a metabolic rate of the subject.5. The method according to claim 4 , wherein the increasing a metabolic rate involves increasing an efficiency of pyruvic acid production of the subject.6. The method according to claim 2 , wherein the improving physical function involves reducing a weight of the subject and/or reducing a waist circumference of the subject.7. The method according to claim 1 , wherein the improving physical function involves improving gastrointestinal function of the subject.8. The method according to claim 7 , wherein the improving gastrointestinal function involves relieving abdominal distension claim 7 , nausea claim 7 , or regurgitation of the subject.9. The method according to claim 7 , wherein the improving gastrointestinal function involves improving claim 7 , intestinal peristalsis claim 7 , relieving constipation claim 7 , ...

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02-05-2019 дата публикации

[1,2,3]triazolo[4,5-d]pyrimidine derivatives with affinity for the type-2 cannabinoid receptor

Номер: US20190127384A1
Принадлежит: Hoffmann La Roche Inc

The invention relates to a compound of formula (I) wherein R 1 to R 4 and n are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.

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21-05-2015 дата публикации

Crystalline forms of a 3-[2-methanesulfonyl-1-(4-trifluoromethyl-phenoxy)ethyl]pyrrolidine compound

Номер: US20150141483A1
Принадлежит: Theravance Biopharma R&D Ip Llc

The invention provides crystalline hydrochloride salts of (S)-3-[(S)-2-methanesulfonyl-1-(4-trifluoromethylphenoxy)ethyl]pyrrolidine. This invention also provides pharmaceutical compositions comprising the crystalline salts, processes and intermediates for preparing the crystalline salts, and methods of using the crystalline salts to treat diseases.

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10-06-2021 дата публикации

Pyrrolopyrimidines as CFTR Potentiators

Номер: US20210171534A1
Принадлежит: Cystic Fibrosis Foundation

The present invention relates to methods of using compounds of Formula I,wherein R1a, R1b, R2, R3, R4, W, Y, and Z are as described herein, and pharmaceutically acceptable salts thereof. The compounds are potentiators of Cystic Fibrosis Transmembrane conductance Regulator (CFTR). The invention also discloses pharmaceutical compositions comprising the compound, optionally in combination with additional therapeutic agents, and methods of potentiating, in mammals, including humans, CFTR by administration of the compounds. These compounds are useful for the treatment of cystic fibrosis (CF), asthma, bronchiectasis, chronic obstructive pulmonary disease (COPD), constipation, Diabetes mellitus, dry eye disease, pancreatitis, rhinosinusitis, Sjögren's Syndrome, and other CFTR associated disorders.

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25-05-2017 дата публикации

Solid formulation and method for stabilizing the same

Номер: US20170143738A1
Принадлежит: EA Pharma Co Ltd

The present invention relates to stabilization of a certain benzothia(dia)zepine derivative in a solid formulation containing the same. In the present invention, in a solid formulation containing (A) the benzothia(dia) zepine derivative mentioned above and (B) a specific plasticizer, the aforementioned ingredient (A) is isolated from the aforementioned ingredient (B), or alternatively, in the case of the aforementioned ingredient (A) not being isolated from the aforementioned ingredient (B), an amount of the aforementioned ingredient (B) is controlled to 0.9% by weight or less based on the total weight of the solid formulation, or the solid formulation is provided with a form containing at least one core and at least one coating layer or capsule layer enclosing at least a part of the core, the aforementioned ingredient (A) is mixed into the core, the aforementioned ingredient (B) is mixed into the coating layer or capsule layer, and an amount of the aforementioned ingredient (B) in the coating layer or capsule layer is controlled to 45% by weight or less based on the total weight of the coating layer or capsule layer.

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14-08-2014 дата публикации

Modulators of Cystic Fibrosis Transmembrane Conductance Regulator

Номер: US20140228399A2
Принадлежит: Vertex Pharmaceuticals Inc

The present invention relates to modulators of cystic fibrosis transmembrane conductance regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating diseases using modulators of CFTR.

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07-05-2020 дата публикации

Cftr regulators and methods of use thereof

Номер: US20200140402A1
Принадлежит: UNIVERSITY OF CALIFORNIA

Provided herein are compounds that activate CFTR and methods for treating constipation, dry eye disorders or other diseases and disorders.

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31-05-2018 дата публикации

Compositions for Colon Cleansing and the Treatment of Gastrointestinal Disorders

Номер: US20180148476A1
Принадлежит:

The present invention provides peptides and compositions that are useful for the treatment of gastrointestinal disorders or for colon cleansing. The present invention also provides compositions and methods of treating gastrointestinal disorders and pharmaceutical compositions for accomplishing the same. In some embodiments, these pharmaceutical compositions include oral dosage forms. 1. A peptide or a pharmaceutically acceptable salt thereof , wherein the peptide comprises the amino acid sequence{'sub': 1', '2', '3', '4', '5', '6', '7', '8', '9', '10', '11', '12', '13', '14', '15', '16', '17', '18', '19', '20', '21, 'XaaXaaXaaXaaXaaXaaXaaXaaXaaXaaXaaXaaXaaXaaAlaXaaXaaGlyXaaXaaXaa(SEQ ID NO: 1), or a pharmaceutically acceptable salt thereof; wherein'}{'sub': '1', 'Xaais BE or is absent;'}{'sub': '2', 'Xaais BK, Asn or is absent;'}{'sub': '3', 'Xaais Asn, Ser or is absent;'}{'sub': '4', 'Xaais Ser or is absent;'}{'sub': '5', 'Xaais Ser, Asn, Ile, BE or is absent;'}{'sub': '6', 'Xaais Tyr, Asp, 4-fluorophenylalanine ((4-F)Phe), BK or is absent;'}{'sub': '7', 'Xaais Cys, cystathionine (Cth), allylglycine (Ag), Hag, or Asp;'}{'sub': '8', 'Xaais Cys, cystathionine (Cth), penicillamine (Pen), or allylglycine (Ag);'}{'sub': '9', 'Xaais Glu, Asp, Ser, Thr, or Gln;'}{'sub': '10', 'Xaais Leu, cyclohexylalanine (Cha), Phe, or 4-fluorophenylalanine ((4-F)Phe);'}{'sub': '11', 'Xaais Cys, Ag, or penicillamine (Pen);'}{'sub': '12', 'Xaais Cys, allylglycine (Ag), Hag, Cth, Dpr, or Val;'}{'sub': '13', 'Xaais Asn or Leu;'}{'sub': '14', 'Xaais Pro, Val, sarcosine (Sar), Leu, or Hydroxyproline (OH-Pro);'}{'sub': '16', 'Xaais Cys, Ag, Pen or Cth;'}{'sub': '17', 'Xaais Tyr, Thr, cyclohexylalanine (Cha), 4-fluorophenylalanine ((4-F)Phe), Phe, Ser, or Ala;'}{'sub': '19', 'Xaais Cys, Ag or Pen;'}{'sub': '20', 'Xaais Tyr, Leu, 4-fluorophenylalanine ((4-F)Phe), cyclohexylalanine (Cha), D-Tyr,'}N-Methyl Tyr (Nme-Tyr) or is absent;{'sub': '21', 'Xaais absent or Asn;'}wherein at least one Xaa is ...

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