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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 195892. Отображено 100.
05-01-2012 дата публикации

Yeast ectopically expressing abnormally processed proteins and uses therefor

Номер: US20120003243A1

Disclosed are yeast ectopically expressing abnormally processed proteins and methods of screening to identify compounds that modulate the function of such abnormally processed proteins in yeast. Compounds identified by such screens can be used to treat or prevent diseases associated with abnormally processed proteins or protein misfolding. Such diseases include Parkinson's Disease, Parkinson's Disease with accompanying dementia, Lewy body dementia, Alzheimer's disease with Parkinsonism, and multiple system atrophy.

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05-01-2012 дата публикации

Process for production of orally ingestible composition containing arabinofuranosyl vitexin, and use of the composition

Номер: US20120004193A1
Автор: Shuichi Kusano
Принадлежит: Fuji Sangyo Co Ltd

A method for producing an orally ingestible composition containing an arabinofuranosyl vitexin and/or a hydrolysate thereof by using Basella alba as a raw material. The product of such method has a sedative effect and a sleep-inducing effect.

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05-01-2012 дата публикации

N-oxides of 1,4-diaza-bicyclo[3.2.2]nonyl pyrimidinyl derivatives useful as nicotinic acetylcholine receptor ligands

Номер: US20120004214A1
Принадлежит: Neurosearch AS

This invention relates to novel 1,4-diaza-bicyclo[3.2.2]nonyl pyrimidinyl derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic ligands at the nicotinic acetylcholine receptors. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances. Formula (I) a stereoisomer or a mixture of its stereoisomers, or a pharmaceutically acceptable salt thereof, wherein Ar represents an indolyl group, which indolyl may optionally be substituted one or more times with substituents selected from halo, trifluoromethyl, trifluoromethoxy, cyano, nitro, amino, alkyl, hydroxy and alkoxy.

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05-01-2012 дата публикации

Method of Inhibition of Respiratory Depression Using Positive Allosteric AMPA Receptor Modulators

Номер: US20120004219A1
Автор: John Greer
Принадлежит: University of Alberta

The invention is directed to a method for alleviating respiratory depression in a subject as a result of disease of pharmacological agents such as opiates, opioids or barbiturates. The invention also discloses pharmaceutical compositions for use with the method, the composition containing in combination, an analgesic, anaesthetic, or a sedative and a positive allosteric AMPA receptor modulator in an amount sufficient to reduce or inhibit respiratory depression caused by the analgesic, anaesthetic, or sedative.

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05-01-2012 дата публикации

Method of treatment or prophylaxis

Номер: US20120004259A1
Принадлежит: SPINIFEX PHARMACEUTICALS PTY LTD

The present invention is directed to methods and agents that are useful in the prevention and amelioration of signs and symptoms associated with neuropathic conditions. More particularly, the present invention discloses the use of angiotensin II receptor 2 (AT 2 receptor) antagonists for the treatment, prophylaxis, reversal and/or symptomatic relief of neuropathic pain, including mechanical hyperalgesia, thermal or mechanical allodynia, diabetic pain and entrapment pain, in vertebrate animals and particularly in human subjects. The AT 2 receptor antagonists may be provided alone or in combination with other compounds such as those that are useful in the control of neuropathic conditions.

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05-01-2012 дата публикации

Compounds for the treatment of pathologies associated with aging and degenerative disorders

Номер: US20120004263A1
Принадлежит: University of Pittsburgh

The present invention relates to methods of inhibiting one or more signs of aging and/or degenerative disorder in a subject in need of such treatment, which comprise administering, to the subject, an effective amount of one or more of the compounds as set forth herein. “Inhibiting a sign of aging or degenerative disorder” means reducing the risk of occurrence, delaying the onset, slowing the progression, and/or reducing the severity and/or manifestation, of a sign of aging or degenerative disorder, and includes, but is not limited to, preventing the occurrence, development or progression of a sign of aging or degenerative disorder.

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20-11-2014 дата публикации

УСТАНОВКА ДЛЯ ОСУЩЕСТВЛЕНИЯ СПОСОБА ПОЛУЧЕНИЯ МИКРОСФЕР ОСНОВАНИЯ НАЛТРЕКСОНА, ВКЛЮЧЕННОГО В ПОЛИМЕРНУЮ МАТРИЦУ

Номер: RU0000148050U1

1. Установка для осуществления способа получения микросфер основания налтрексона, включенного в матрицу из биоразлагаемого полимера, выбранного из группы, состоящей из полилактида, полигликолида и полилактид-ко-гликолида, отличающаяся тем, что включает 1) микроканальный модуль, который является проточным реактором с диаметром каналов от 25 мкм до 0,5 мм, имеющим Т-образное или Х-образное пересечение каналов под углом 90°, или Y-образное пересечение каналов под углом от 20 до 70°, предназначенный для смешения объединенного раствора основания налтрексона в первом органическом растворителе, выбранном из группы, состоящей из хлористого метилена, хлороформа, тетрахлорида углерода, этиленхлорида, этилендихлорида и бензилового спирта, и полимера во втором органическом растворителе, выбранном из группы, состоящей из хлористого метилена, хлороформа, тетрахлорида углерода, этиленхлорида, этилендихлорида, этилацетата при условии, что если первый органический растворитель является бензиловым спиртом, то второй органический растворитель является этилацетатом, с первой водной диспергирующей фазой, содержащей 0,5-5,0% (мас./об.) поливинилового спирта (ПВС), для генерирования капель дисперсии за счет разделения потока объединенного раствора потоком первой водной диспергирующей фазы при соотношении постоянных расходов водной фазы и объединенного раствора от 100 до 4 и расходе объединенного раствора 0,05-1,0 мкл/с получением дисперсной системы; и 2) реактор смешения, представляющий каскад из двух или трех реакторов смешения, входом первого реактора связанный по потоку дисперсной системы с выходом микроканального модуля, где - первый из реакторов каскада выходом связан по потоку со входом последующего реактора и предназначен для приготовления второй водной диспергирующей фазы, содержащей 0,25-1,0% (мас./об.) ПВС, объединения дисперсной системы со второй водной диспергирующей фазой и механического воздействия в течение промежутка времени от 8 до 20 часов в интервале температуры от 4 до ...

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12-01-2012 дата публикации

ANTI-Aß OLIGOMER HUMANIZED ANTIBODY

Номер: US20120009179A1
Принадлежит: Kyowa Hakko Kirin Co Ltd

An anti-Aβ oligomer humanized antibody which does not bind to Aβ monomers and specifically binds only to Aβ oligomers; an anti-cognitive dysfunction agent, an agent for treating Alzheimer's disease, an agent for suppressing formation of neuritic plaque and an inhibitor of formation of Aβ amyloid fiber comprising the antibody as an active ingredient; a method for at least one of preventing and treating cognitive dysfunction or Alzheimer's disease, comprising the step of administering the antibody; and a method for suppressing progression of Alzheimer's disease, comprising the step of administering the antibody.

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12-01-2012 дата публикации

Modified Virus Vectors and Methods of Making and Using the Same

Номер: US20120009268A1

The present invention provides AAV capsid proteins (VP1, VP2 and/or VP3) comprising a modification in the amino acid sequence in the three-fold axis loop 4 and virus capsids and virus vectors comprising the modified AAV capsid protein. In particular embodiments, the modification comprises a substitution of one or more amino acids at amino acid positions 585 to 590 (inclusive) of the native AAV2 capsid protein sequence or the corresponding positions of other AAV capsid proteins. The invention also provides methods of administering the virus vectors and virus capsids of the invention to a cell or to a subject in vivo.

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12-01-2012 дата публикации

Self-assembling peptides for regeneration and repair of neural tissue

Номер: US20120010140A1
Принадлежит: Massachusetts Institute of Technology

The present invention provides methods and compositions for enhancing regeneration and/or repair of neural tissue. One method include providing a nanoscale structured material at the site of injury, wherein the nanoscale structured material provides an environment that is permissive for regeneration of neural tissue and allows axon growth from a location on one side of a site of injury or barrier to a location on the other side of the site of injury or barrier. A second method includes introducing a composition comprising self-assembling peptides into the subject at the site of injury, wherein the peptides are amphiphilic peptides that comprise substantially equal proportions of hydrophobic and hydrophilic amino acids and are complementary and structurally compatible. A variety of compositions comprising a nanoscale structured material or precursor thereof, and an additional substance such as a regeneration promoting factor, are also provided. In certain embodiments of the invention the nanoscale structured material or precursor thereof comprises self-assembling peptides. The invention further provides compositions and methods for repair of an intervertebral disc, including nucleus pulpusos repair.

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12-01-2012 дата публикации

Methods of treating neurodegenerative disorders and diseases

Номер: US20120010196A1
Автор: Quingyu QIN, Xiaoning Bl
Принадлежит: WESTERN UNIVERSITY OF HEALTH SCIENCES

This invention is directed to a novel method of treating neurodegenerative disorders and diseases. Another, related aspect of this invention is directed to a screening method of identifying compounds that can be used to treat neurodegenerative disorders and diseases. The foregoing aspects of the invention particularly relate to neurodegenerative disorders and diseases have degeneration of neuronal axons as part of their pathologies. The method of treatment involves administering a pharmaceutical formulation that comprises a compound or mixture of compounds that inhibits one or more intracellular signaling mechanism that regulate axon degeneration or growth cone collapse. The screening method aspect of the invention identifies test compounds that can be used for the treatment or prevention of neurodegenerative disorders based on the test compound's ability to inhibit axon degeneration or growth cone collapse.

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12-01-2012 дата публикации

5-chloro-4-hydroxy-1-methyl-2-oxo-n-phenyl-1,2-dihydroquinoline-3-carboxamide, salts and uses thereof

Номер: US20120010239A1
Автор: Ulf Tomas Fristedt
Принадлежит: Teva Pharmaceutical Industries LTD

The subject invention provides 5-chloro-4-hydroxy-1-methyl-2-oxo-N-phenyl-1,2-dihydroquinoline-3-carboxamide, its salts and uses.

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12-01-2012 дата публикации

Acetylene derivatives having mglur 5 antagonistic activity

Номер: US20120010263A1
Принадлежит: Individual

The invention provides compounds of formula I wherein n, A, R, R′, R″, R O , X and Y are as defined in the description, and their preparation. The compounds of formula I are useful as pharmaceuticals.

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12-01-2012 дата публикации

Modulation of anxiety through blockade of anandamide hydrolysis

Номер: US20120010283A1

Fatty acid amide hydrolase inhibitors of the Formula: are provided wherein X is NH, CH 2 , O, or S; Q is O or S; Z is O or N; R is an aromatic moiety selected from the group consisting of substituted or unsubstituted aryl; substituted or unsubstituted biphenylyl, substituted or unsubstituted naphthyl, and substituted or unsubstituted phenyl; substituted or unsubstituted terphenylyl; substituted or unsubstituted cycloalkyl, heteroaryl, or alkyl; and R 1 and R 2 are independently selected from the group consisting of H, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, and substituted or unsubstituted phenyl, substituted or unsubstituted biphenylyl, substituted or unsubstituted aryl, and substituted or unsubstituted heteroaryl; with the proviso that if Z is O, one of R 1 and R 2 is absent, and that if Z is N, optionally R 1 and R 2 may optionally be taken together to form a substituted or unsubstituted N-heterocycle or substituted or unsubstituted heteroaryl with the N atom to which they are each attached. Pharmaceutical compositions comprising the compounds of Formula I and methods of using them to inhibit FAAH and/or treat appetite disorders, glaucoma, pain, insomnia, and neurological and psychological disorders including anxiety disorders, epilepsy, and depression are provided.

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19-01-2012 дата публикации

Methods and compositions for cns delivery of heparan n-sulfatase

Номер: US20120014936A1
Принадлежит: Shire Human Genetics Therapies Inc

The present invention provides, among other things, compositions and methods for CNS delivery of lysosomal enzymes for effective treatment of lysosomal storage diseases. In some embodiments, the present invention includes a stable formulation for direct CNS intrathecal administration comprising a heparan N-sulfatase (HNS) protein, salt, and a polysorbate surfactant for the treatment of Sanfilippo Syndrome Type A.

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19-01-2012 дата публикации

Dna vaccine for alzheimer's disease

Номер: US20120014987A1
Автор: Yoh Matsumoto

The present invention aims to provide a DNA vaccine for Alzheimer's disease. The present invention provides a recombinant vector which comprises DNA encoding amyloid β and DNA encoding a Th2 cytokine, as well as a DNA vaccine for Alzheimer's disease which comprises this vector.

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19-01-2012 дата публикации

Enterically coated cysteamine, cystamine and derivatives thereof

Номер: US20120015038A1
Принадлежит: UNIVERSITY OF CALIFORNIA

The disclosure provides oral cysteamine and cystamine formulations useful for treating cystinosis and neurodegenerative diseases and disorders. The formulations provide controlled release compositions that improve quality of life and reduced side-effects.

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19-01-2012 дата публикации

Complement receptor 2 targeted complement modulators

Номер: US20120015871A1

Modulation of the complement system represents a therapeutic modality for numerous pathologic conditions associated with complement activation. In a strategy to prepare complement inhibitors that are targeted to sites of complement activation and disease, compositions comprising a complement inhibitor linked to complement receptor (CR) 2 are disclosed. The disclosed are compositions can be used in methods of treating pathogenic diseases and inflammatory conditions by modulating the complement system.

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19-01-2012 дата публикации

Kallikrein-inhibitor therapies

Номер: US20120015881A1
Принадлежит: Dyax Corp

Methods are described for preventing or reducing ischemia, e.g., cerebral ischemia, and/or reperfusion injury, e.g., reperfusion injury associated with cerebral ischemia, in a patient.

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19-01-2012 дата публикации

Novel compounds as cannabinoid receptor ligands

Номер: US20120015929A1
Принадлежит: ABBOTT LABORATORIES

Disclosed herein are compounds of formula (I) wherein R 1 , R 2 , R 3 , R 25a , R 26a , X, and n are as defined in the specification. Pharmaceutical compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and pharmaceutical compositions are also described.

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19-01-2012 дата публикации

Growth factor htter36

Номер: US20120016107A1
Принадлежит: Human Genome Sciences Inc

The present invention discloses Growth Factor HTTER36 (GDF3) polypeptides and polynucleotides encoding such polypeptides. Also provided are antibodies that bind HTTER36, including chimeric, humanized, and single chain antibodies.

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26-01-2012 дата публикации

Process for the purification of eslicarbazepine acetate

Номер: US20120022047A1
Принадлежит: Glenmark Generics LTD

The present invention relates to the purification and particle size of eslicarbazepine acetate. The present invention also relates to the physical characteristics of solid state eslicarbazepine acetate, and pharmaceutical compositions containing the same.

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26-01-2012 дата публикации

Histamine h3 inverse agonists and antagonists and methods of use thereof

Номер: US20120022050A1
Принадлежит: SUNOVION PHARMACEUTICALS INC

Provided herein are fused imidazolyl compounds, methods of synthesis, and methods of use thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as neurological disorders and metabolic disorders. Compounds provided herein inhibit the activity of histamine H3 receptors and modulate the release of various neurotransmitters, such as histamine, acetylcholine, norepinephrine, and dopamine (e.g. at the synapse). Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.

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26-01-2012 дата публикации

Pyrrolidine triple reuptake inhibitors

Номер: US20120022125A1
Автор: Jianguo Ma, Liming Shao
Принадлежит: SUNOVION PHARMACEUTICALS INC

In various embodiments, the present invention provides cycloalkyl pyrrolidine compounds and methods for their use in the treatment and/or prevention of various diseases, conditions and syndromes, including central nervous system (CNS) disorders, such as depression, anxiety, schizophrenia and sleep disorder as well as methods for their synthesis. The invention also relates to pharmaceutical compositions containing the compounds of the invention, as well as methods of inhibiting reuptake of endogenous monoamines, such as dopamine, serotonin and norepinephrine from the synaptic cleft and methods of modulating one or more monoamine transporter.

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02-02-2012 дата публикации

Combination therapy with glatiramer acetate and rasagiline for the treatment of multiple sclerosis

Номер: US20120027718A1
Принадлежит: Teva Pharmaceutical Industries LTD

The subject invention provides a method of treating a subject afflicted with a form of multiple sclerosis comprising periodically administering to the subject an amount of glatiramer acetate and an amount of rasagiline or the pharmaceutically acceptable salt thereof, wherein the amounts when taken together are effective to alleviate a symptom of the form of multiple sclerosis in the subject so as to thereby treat the subject. The subject invention also provides a package comprising glatiramer acetate, rasagiline or the pharmaceutically acceptable salt thereof and instructions for use of the together to alleviate a symptom of a form of multiple sclerosis in a subject. The subject invention further provides a pharmaceutical combination comprising separate dosage forms of an amount of glatiramer acetate and an amount of rasagiline or the pharmaceutically acceptable salt thereof, which combination is useful to alleviate a symptom of a form of multiple sclerosis in a subject.

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02-02-2012 дата публикации

Nicotine immunonanotherapeutics

Номер: US20120027808A1
Автор: Matteo Iannacone

The present invention provides compositions and systems for delivery of nanocarriers to cells of the immune system. The invention provides nanocarriers capable of stimulating an immune response in T cells and/or in B cells. The invention provides nanocarriers that comprise an immunofeature surface having a plurality of nicotine moieties. The invention provides pharmaceutical compositions comprising nanocarriers. The present invention provides methods of designing, manufacturing, and using nanocarriers and pharmaceutical compositions thereof. For example, the present invention describes nanocarriers capable of eliciting an immune response and the production of anti-nicotine antibodies.

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02-02-2012 дата публикации

Natural marine source phospholipids comprising polyunsaturated fatty acids and their applications

Номер: US20120028922A1
Автор: Fotini Sampalis
Принадлежит: Individual

A phospholipid extract from a marine or aquatic biomass possesses therapeutic properties. The phospholipid extract comprises a variety of phospholipids, fatty acid, metals and a novel flavonoid.

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02-02-2012 дата публикации

Bicyclic mglur5 positive allosteric modulators and methods of making and using same

Номер: US20120028955A1

In one aspect, the invention relates to bicyclic mGluR5 positive allosteric modulators, for example 6-(phenylethynyl)-3,4-dihydroisoquinolin-1(2H)-one, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. 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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02-02-2012 дата публикации

6 Substituted 2, 3,4,5 Tetrahydro-1H-Benzo[d]Azepines as 5-HT2c Receptor Agonist

Номер: US20120028961A1
Принадлежит: Eli Lilly and Co

The present invention provides 6-substituted 2,3,4,5-tetrahydro-1H-benzo[d]azepines of Formula I as selective 5-HT 2C receptor agonists for the treatment of 5-HT 2C associated disorders including obesity, obsessive/compulsive disorder, depression, and anxiety: where: R 6 is —S—R 14 ; and other substituents are as defined in the specification.

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02-02-2012 дата публикации

Derivatives of aminocyclobutane or aminocyclobutene, their method of preparation and their use as medical products

Номер: US20120029013A1
Принадлежит: Pierre Fabre Medicament SA

The present invention concerns compounds of general formula (1), where in:—-a- is a single or double bond, Ar is an aromatic group, substituted or unsubstituted, R1 and R2 each independently or together are: a hydrogen atom or C 1 -C 6 alkyl group, branched or unbranched, saturated or unsaturated, substituted or unsubstituted; the groups R1 and R2 may also form a heterocycle, R3 and R3′ each independently or together are a hydrogen atom or C 1 -C 6 alkyl group, X is an oxygen atom or a sulphur atom, and the addition salts of the compounds of general formula (1) with pharmaceutically acceptable mineral acids or organic acids.

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02-02-2012 дата публикации

Use of flavones for treating psychiatric disorders with sensorimotor gating deficits

Номер: US20120029066A1

Novel Use of flavones having 2-phenylchromen-4-one skeleton is disclosed herein. The flavones are useful as lead compounds for manufacturing a medicament or a pharmaceutical composition for treating a patient diagnosed with a psychiatric disorder with sensorimotor gating deficits.

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02-02-2012 дата публикации

Anti-anxiety composition

Номер: US20120029088A1
Принадлежит: JX Nippon Oil and Energy Corp

This invention provides a highly safe anti-anxiety composition that can be used for treatment or prevention of anxiety disorders. Such anti-anxiety composition comprises, as an active ingredient, a carotenoid.

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09-02-2012 дата публикации

Treatment of neurotrophic factor mediated disorders

Номер: US20120034193A1
Принадлежит: Phytopharm Ltd

An agent selected from A/B-cis furostane, furostene, spirostane and spirostene steroidal sapogenins and ester, ether, ketone and glycosylated forms thereof is used to induce self-regulated homeostasis of neurotrophic factors (NFs), for example BDNF and/or GDNF, NFs with limited and manageable side effects in a subject, by modulating NFs in a non-toxic manner under homeostatic control. An effective amount of at least one such agent is administered to the subject, particularly in the treatment or prevention of a range of NF-mediated disorders, particularly neurological, psychiatric, inflammatory, allergic, immune and neoplastic disorders, and in the restoration or normalisation of neuronal and other function in or in relation to any damaged or abnormal tissue, including when assisting tissue (for example, skin, bone, eye and muscle) healing and general skin, bone, eye and muscle health.

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09-02-2012 дата публикации

Irak kinase family as novel target and biomarker for alzheimer

Номер: US20120035076A1

The present invention relates to methods and devices for the diagnosis or drug response prediction of neurological disorders by measuring kinase activity and studying the phosphorylation levels and profiles in samples of said patients. Furthermore the present invention relates to methods of identifying drug compounds relevant to neurological disorders by measuring kinase activity and studying phosphorylation levels. Also, the present invention relates to the use of inhibitors of the IRAK protein kinase family or a pharmaceutical composition thereof in the treatment of neurological disorders such as Alzheimer's disease.

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09-02-2012 дата публикации

Neuronal differentiation-inducing peptide and use thereof

Номер: US20120035112A1
Принадлежит: TOAGOSEI CO LTD

A neuronal differentiation inducer provided by the present invention contains an artificially synthesized peptide which includes an amino acid sequence constituting a signal peptide in amyloid precursor protein (APP), or a partial sequence of the amino acid sequence constituting this signal peptide.

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09-02-2012 дата публикации

Glycolipids as treatment for disease

Номер: US20120035120A1
Автор: Shawn Defrees
Принадлежит: Seneb Biosciences Inc

This invention provides compounds, compositions, and methods for treating a disorder selected from cancer, hyperinsulinemia, hypoglycemia, hyperinsulinemia with hypoglycemia, atypical Parkinson's disease, Huntington's disease, multiple systems atrophy, GM3 synthase deficiency, GM2 synthase deficiency or tauopathy.

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09-02-2012 дата публикации

Compounds, Compositions, and Methods for the Treatment of Beta-Amyloid Diseases and Synucleinopathies

Номер: US20120035230A1
Принадлежит: ProteoTech Inc

Dihydroxyaryl compounds and pharmaceutically acceptable esters, their synthesis, pharmaceutical compositions containing them, and their use in the treatment of synucleinopathies, such as observed in Parkinson's disease, and the manufacture of medicaments for such treatment.

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09-02-2012 дата публикации

Plasmalogen compounds, pharmaceutical compositions containing the same and methods for treating diseases of the aging

Номер: US20120035250A1
Принадлежит: Phenomenome Discoveries Inc

Described herein are routes of synthesis and therapeutic uses of 1-alkyl, 2-acyl glycerol derivatives of formula I: which when administered to mammalian biological systems result in increased cellular concentrations of specific sn-2 substituted ethanolamine plasmalogens independent of the ether lipid synthesis capacity of the system. Elevating levels of the specific sn-2 substituted species in this way can cause lowering of membrane cholesterol levels and the lowering of amyloid secretion. These compounds can be used for the treatment or prevention of diseases of aging associated with increased membrane cholesterol, increased amyloid, and decreased plasmalogen levels, such as neurodegeneration (including Alzheimer's disease, Parkinson's disease and age-related macular degeneration), cognitive impairment, dementia, cancer (e.g. prostate, lung, breast, ovarian, and kidney cancers), osteoporosis, bipolar disorder and vascular diseases (such as atherosclerosis, hypercholesterolemia).

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16-02-2012 дата публикации

Method of treatment of neurodementing diseases using isolated, monoclonal, human, anti-b-amyloid antibody

Номер: US20120039897A1
Принадлежит: Philipps Universitaet Marburg

Isolated, monoclonal, human, anti-β-amyloid antibodies are provided which bind to dimeric forms of Ab with higher affinity than to monomeric forms of Ab and when bound to an Aβ polypeptide comprising Aβ(21-37) shield Aβ(21-37) from proteolytic digestion. The antibodies were shown to inhibit fibril formulation and reduce plaque size in vivo and to not bind brain vessel walls. Accordingly, the antibodies are useful in human and veterinary medicine for the treatment and prophylaxis of Alzheimer's disease and other neurodementing diseases. Methods of detecting or measuring the progression of a neurodementing disease also are provided.

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16-02-2012 дата публикации

Chewing Gum And Particulate Material For Controlled Release Of Active Ingredients

Номер: US20120039981A1
Принадлежит: Fertin Pharma AS

A particulate material for controlled release of active ingredients includes a combination of one or more active ingredients, including nicotine, and an inorganic mineral filler, in which the active ingredient is reversibly absorbed into and/or adsorbed onto the inorganic mineral filler, and the BET specific surface area of the inorganic mineral filler is above 15 m 2 /g, the BET specific surface area measured in accordance with ISO 9277. Further, a chewing gum having the particulate material includes a combination of one or more active ingredients, such as nicotine or a flavoring agent, and an inorganic mineral filler. Finally, the method of producing the chewing gum is provided. The invention is particularly advantageous for controlled release of active ingredients.

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16-02-2012 дата публикации

Method of detecting progression of a neurodementing disease

Номер: US20120040382A1
Принадлежит: Philipps Universitaet Marburg

Isolated, monoclonal, human, anti-β-amyloid antibodies are provided which bind to dimeric forms of Ab with higher affinity than to monomeric forms of Ab and when bound to an Aβ polypeptide comprising Aβ(21-37) shield Aβ(21-37) from proteolytic digestion. The antibodies were shown to inhibit fibril formation and reduce plaque size in vivo and to not bind brain vessel walls. Accordingly, the antibodies are useful in human and veterinary medicine for the treatment and prophylaxis of Alzheimer's disease and other neurodementing diseases. Methods of detecting or measuring the progression of a neurodementing disease also are provided.

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16-02-2012 дата публикации

Methods and materials for delivering molecules

Номер: US20120040432A1

This document relates to methods and materials involved in delivering molecules to a mammal. For example, methods and materials for using nanoparticles to increase the half-life and the bioavailability of molecules administered to a mammal are provided.

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16-02-2012 дата публикации

Tetracyclic terpene series compounds, methods for preparing same, uses thereof as medicines and pharmaceutical compounds containing same

Номер: US20120040930A1

The invention concerns a triterpene alkaloid of general formula (I). The invention also concerns a method for making same and use thereof as medicine.

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16-02-2012 дата публикации

Benzimidazoles which have activity at m1 receptor and their uses in medicine

Номер: US20120041027A1
Принадлежит: Glaxo Group Ltd

Compounds of formula (I) and salts and solvates are provided: wherein Uses of the compounds for therapy, for example in the treatment of psychotic disorders and cognitive impairment, are also disclosed.

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16-02-2012 дата публикации

Hydroxybenzoate salts of metanicotine compounds

Номер: US20120041033A1
Принадлежит: Individual

Patients susceptible to or suffering from conditions and disorders, such as central nervous system disorders, are treated by administering to a patient in need thereof compositions that are hydroxybenzoate salts of E-metanicotine-type compounds. The formation of hydroxybenzoate salts of the E-metanicotine compounds is also useful in purifying the E-metanicotine compounds, as the hydroxybenzoate salts tend to crystallize out, leaving impurities such as Z-metanicotine compounds, and compounds where the double bond has migrated, in solution. If desired, the hydroxybenzoate salts can be converted to either the free base (the E-metanicotine) or to another pharmaceutically acceptable salt form.

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16-02-2012 дата публикации

Substituted acylguanidine derivatives (as amended)

Номер: US20120041036A1
Принадлежит: Astellas Pharma Inc

An object of the present invention is to provide an excellent agent for treating or preventing dementia, schizophrenia based on serotonin 5-HT 5A receptor modulating action. It was discovered that acylguanidine derivatives, in which the guanidine is bonded to one ring of a naphthalene via a carbonyl group and a cyclic group is bonded to the other ring thereof, exhibit potent the 5-HT 5A receptor modulating action and excellent pharmacological actions based on the action. The present invention is useful as an excellent agent for treating or preventing dementia, schizophrenia, bipolar disorder or attention deficit hyperactivity disorder.

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23-02-2012 дата публикации

Methods and uses of hypoxic compartment cells

Номер: US20120045419A1
Принадлежит: UNIVERSITY HEALTH NETWORK

The disclosure relates to methods of maintaining and/or expanding an in vitro population of hypoxia compartment cells comprising culturing said population of cells optionally in an oxygen controlled environment, wherein the population of hypoxia compartment cells is exposed to an oxygen concentration of between about 1.5% and about 10%, preferably between about 2% and about 5%, and uses of cells expanded according to these methods.

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23-02-2012 дата публикации

Compounds and compositions for cognition-enhancement, methods of making, and methods of treating

Номер: US20120046273A1
Принадлежит: Mithridion Inc

Muscarinic agonists, which are useful for stimulating muscarinic receptors and treating cognitive disorders, are provided. Methods of synthesizing such agonists also are provided. Also provided are compositions for enhancing cognitive function in subjects such as humans, the compositions comprising a muscarinic agonist or a pharmaceutically suitable form thereof. Also provided are methods of treating animals such as humans by administering such compositions.

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23-02-2012 дата публикации

Compounds for treating neuropsychiatric conditions

Номер: US20120046283A1
Принадлежит: Afraxis Inc

Provided herein are PAK inhibitors and methods of utilizing PAK inhibitors for the treatment of neuropsychiatric conditions.

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23-02-2012 дата публикации

3-substituted propanamine compounds

Номер: US20120046312A1
Принадлежит: SK Biopharmaceuticals Co Ltd

Racemic or enantiomerically enriched 3-substituted propanamine compounds represented by the following structural formula (I): or a pharmaceutically acceptable salt thereof are disclosed. Pharmaceutical compositions containing the subject compounds are also disclosed. The subject compounds are useful for the treatment of diseases of the central nervous system, such as depression, anxiety and pain disorders.

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23-02-2012 дата публикации

Small molecule inhibitors of kynurenine-3-monooxygenase

Номер: US20120046324A1
Принадлежит: University of Maryland at Baltimore

The present invention relates to compounds of Formula I below and their tautomers or pharmaceutically acceptable salts, compositions and methods of uses thereof.

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23-02-2012 дата публикации

Treatment of dystrophin family related diseases by inhibition of natural antisense transcript to dmd family

Номер: US20120046345A1
Принадлежит: OPKO CURNA LLC

The present invention relates to antisense oligonucleotides that modulate the expression of and/or function of Dystrophin family, in particular, by targeting natural antisense polynucleotides of Dystrophin family. The invention also relates to the identification of these antisense oligonucleotides and their use in treating diseases and disorders associated with the expression of DMD family.

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23-02-2012 дата публикации

Controlled cannabis decarboxylation

Номер: US20120046352A1
Автор: Andrew David Hospodor
Принадлежит: Individual

The invention is a process for the controlled decarboxylation of cannabis wherein Medicinal Delta-9 tetrahydrocannabinol (Δ 9 -THC) and other cannabinoid medicinal substances are decarboxylated through a chemical reaction facilitated by a cofactor. The amount of medicinal cannabis decarboxylated will be directly proportional to the amount of cofactor used. Use a small amount of the cofactor and only some of the medicinal cannabis contained in raw cannabis will be converted from an acidic form into a non-acidic form. Use a large amount of the cofactor and most or all of the medicinal cannabis will be decarboxylated. The reaction is proportional to the molar mass of cofactor.

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23-02-2012 дата публикации

Glutathione-based delivery system

Номер: US20120046445A1
Принадлежит: Individual

A delivery system is provided. The delivery system includes a carrier or an active compound and a glutathione or a glutathione derivative grafted thereon. The invention also provides a compound including a moiety comprising a vitamin E derivative or a phospholipid derivative, a polyethylene glycol (PEG) or a polyethylene glycol derivative bonded thereto, and a glutathione (GSH) or a glutathione derivative bonded to the polyethylene glycol or the polyethylene glycol derivative.

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01-03-2012 дата публикации

Inhibition of undesired sensory effects by the compound camphor

Номер: US20120052021A1
Принадлежит: PHILIP MORRIS USA INC

A smokeless tobacco product or medicinal nicotine product includes nicotine and camphor dissolved in a non-flavored oily carrier. Preferably, the camphor is present in a concentration ranging from about 600 ppm to about 1300 ppm. Also disclosed are methods of making such products.

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01-03-2012 дата публикации

Vaccine composition for prophylaxis and/or therapy of alzheimer's disease

Номер: US20120052086A1
Принадлежит: Hokko Chemical Industry Co Ltd

A vaccine composition for prophylaxis and/or therapy of Alzheimer's disease, which comprises a fusion protein prepared by inserting a single or tandemly repeated multiple copies of amyloid β antigenic peptide having 5 to 15 continuous amino acid residues derived from the N-terminus of amyloid β peptide into a wild type seed storage protein.

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01-03-2012 дата публикации

Nitrogen-Containing Fused Heterocyclic Compounds and Their use as Beta Amyloid Production Inhibitors

Номер: US20120053171A1
Принадлежит: Eisai R&D Management Co Ltd

A compound represented by the formula [I]: or a pharmacologically acceptable salt or ester thereof, wherein Ring A represents a five-membered aromatic heterocyclic group or the like fused with a non-aromatic ring group, which may be substituted, Ring B represents a phenyl group or the like which may be substituted, X1 represents a single bond or the like, R1 and R2 each represent a C1-6 alkyl group or the like, m represents an integer of 0 to 3, and n represents an integer of 0 to 2, is effective as a therapeutic agent for a disease caused by Aβ.

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08-03-2012 дата публикации

Anti- integrin antibodies, compositions, methods and uses

Номер: US20120058128A1
Принадлежит: Janssen Biotech Inc

The present invention relates to at least one novel anti-alpha-V subunit antibodies, including isolated nucleic acids that encode at least one anti-alpha-V subunit antibody, alpha-V subunit, vectors, host cells, transgenic animals or plants, and methods of making and using thereof, including therapeutic compositions, methods and devices.

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08-03-2012 дата публикации

Transdermal Preparation

Номер: US20120058175A1
Принадлежит: Hisamitsu Pharmaceutical Co Inc

Provided is a transdermal preparation, which is capable of long-term (1-day to 7-day) release of a basic drug from a preparation, continuously and at a consistent concentration; shows little reduction over time in the drug content, even if multiple drugs are contained in the preparation; and is produced by a simple process. The transdermal preparation comprises a substrate, and an adhesive layer containing a basic drug and a water-soluble polymer.

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08-03-2012 дата публикации

Antibody against periostin, and a pharmaceutical composition comprising it for preventing or treating a disease in which periostin is involved

Номер: US20120058572A1
Принадлежит: Daiichi Sankyo Co Ltd, Osaka University NUC

The present invention provides an antibody against a periostin isoform having anti-cell adhesive activity, especially an anti-periostin antibody having the ability to neutralize anti-cell adhesive properties, as well as a prophylactic or therapeutic agent for periostin-related diseases comprising the antibody. The present invention also provides methods for detecting and quantifying the periostin isoform in a sample by using the antibody, as well as a method for diagnosing periostin-related diseases comprising measuring the amount of the periostin isoform by the detection or quantification method.

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08-03-2012 дата публикации

Azabicycloalkane-indole and azabicycloalkane-pyrrolo-pyridine mch-1 antagonists, methods of making, and use thereof

Номер: US20120058939A9
Принадлежит: Albany Molecular Research Inc

Novel MCH-1 receptor antagonists are disclosed. These compounds are used in the treatment of various disorders, including obesity, anxiety, depression, non-alcoholic fatty liver disease, and psychiatric disorders. Methods of making these compounds are also described in the present invention.

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08-03-2012 дата публикации

Neuroprotective iron chelators and pharmaceutical compositions comprising them

Номер: US20120058945A1

Novel iron chelators exhibiting neuroprotective and good transport properties are useful in iron chelation therapy for treatment of a disease, disorder or condition associated with iron overload and oxidative stress, e.g., a neurodegenerative or cerebrovascular disease or disorder, a neoplastic disease, hemochromatosis, thalassemia, a cardiovascular disease, diabetes, an inflammatory disorder, anthracycline cardiotoxicity, a viral infection, a protozoal infection, a yeast infection, retarding aging, and prevention and/or treatment of skin aging and skin protection against sunlight and/or UV light. The iron chelator function is provided by a 8-hydroxyquinoline, a hydroxypyridinone or a hydroxamate moiety. The neuroprotective function is imparted to the compound, e.g., by a neuroprotective peptide. A combined antiapoptotic and neuroprotective function is provided by a propargyl group.

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08-03-2012 дата публикации

Methods of Treating Neurological Disorders

Номер: US20120058949A1
Принадлежит: Alon Friedman, Daniela Kaufer, Luisa Cacheaux

The present invention provides methods of treating epilepsy and other neurological disorders. The methods generally involve administering to an individual in need thereof an effective amount of an agent that blocks a transforming growth factor-beta pathway.

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08-03-2012 дата публикации

Method of treating early morning akinesia in subjects having parkinson's disease

Номер: US20120059013A1
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

The present invention provides a method for treating early morning akinesia, comprising continuous administration to a patient in need of such treatment a therapeutically effective amount of a dopamine agonist or a pharmaceutically acceptable salt, enantiomer, solvate, hydrate, polymorph or prodrug thereof.

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08-03-2012 дата публикации

Novel crystalline hydrate, amorphous and polymorphic forms of dihydro-benzoxazole-6-yl-acetamide derivative and processes for their preparation

Номер: US20120059034A1
Принадлежит: Richter Gedeon Nyrt

The invention relates to novel crystalline hydrate, amorphous and crystalline polymorphic forms of 2-[4-(4-Fluoro-benzyl)-piperidine-1-yl]-2-oxo-N-(2-oxo-2,3-dihydro-benzoxazole-6-yl)-acetamide (I) (radiprodil). Processes for the preparation of these forms, compositions containing these forms, and methods of use thereof are also described.

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08-03-2012 дата публикации

Use Of Copolymers Based On Amino-Containing Polymers As Matrix Binders In Preparing Active Compound-Containing Granules And Administration Forms

Номер: US20120059054A1
Принадлежит: BASF SE

Described are matrix binders comprising copolymers based on amino-containing polymers, as well as their use in preparing active compound-containing granules and administration forms The copolymers having basic amino groups can be obtained by radical polymerization of: a) N,N-diethylaminoethyl methacrylate, and b) at least one radically polymerizable compound, selected from esters of α,β-ethylenically unsaturated mono- and dicarboxylic acids with C 1 -C 8 alkanols.

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08-03-2012 дата публикации

Dispersions of rasagiline citrate

Номер: US20120059058A1
Принадлежит: Teva Pharmaceutical Industries LTD

The subject invention provides a solid dispersion of rasagiline citrate, a composition and a process for the manufacture thereof.

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08-03-2012 дата публикации

Intermediate compound for synthesizing pharmaceutical agent and production method thereof

Номер: US20120059165A1
Принадлежит: SANOFI SA

A production method of an optically active 2-{4-(5-substituted-oxadiazolyl) phenyl}morpholine which is useful as an intermediate for synthesizing a pharmaceutical agent is provided and the method comprises the following steps 1) to 4): 1) reacting a bromophenylmorpholine with a hexacyanoferrate(II) or a hydrate thereof at a temperature of from 110° C. to 140° C. in a reaction mixture comprising a Na 2 CO 3 , an organophosphorus compound, and a palladium catalyst in a polar aprotic solvent alone or combination of a polar aprotic solvent and other polar aprotic solvent or hydrocarbon solvent to give a cyanophenylmorpholine; 2) reacting the cyanophenylmorpholine with hydroxylamine or hydroxylamine hydrochloride at a temperature of from 10° C. to 40° C. in an aprotic polar solvent to give a hydroxylamine derivative; 3) reacting the hydroxylamine derivative with an acylation reagent selected from the group consisting of aliphatic acyl halides, aromatic acyl halides, aliphatic acyl anhydrides and aromatic anhydrides; and 4) keeping the mixture obtained after step 3) at a temperature of from 60° C. to 140° C. to give a 2-{4-(5-substituted-oxadiazolyl) phenyl}morpholine.

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15-03-2012 дата публикации

Method for Treating Psoriatic Arthritis by Administering an Anti-IL-12 Antibody

Номер: US20120063998A1
Принадлежит: Individual

Isolated anti-IL-12 antibodies, nucleic acids encoding antibodies or antibody portions, vectors, host cells, and methods of making are useful for production of antibody or portions for treating and/or diagnosing IL-12 related conditions, diseases, and disorders, such as psoriatic arthritis.

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15-03-2012 дата публикации

Efficient Generation of Neurally-Induced Mesenchymal Stem Cells and Applications Thereof

Номер: US20120064041A1
Автор: Arshak Alexanian
Принадлежит: Individual

The present invention provides methods and compositions for reprogramming mammalian mesenchymal stem cells, as well as to methods for using such cells, for example, to prevent or treat various injuries, diseases, and disorders in human and non-human animals.

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15-03-2012 дата публикации

Stabilized biodegradable neurotoxin implants

Номер: US20120065141A1
Принадлежит: Allergan Inc

Biodegradable neurotoxin implants and methods of making and using such implants are provided. Biodegradable neurotoxin implants include a neurotoxin, a biodegradable polymer component, and an acidity regulating component. The biodegradable polymer component is effective in controlling the release of the neurotoxin from the implant when the implant is located in a patient's body. The acidity regulating component is effective in maintaining a pH of the implant in a desired range that may be effective in stabilizing the neurotoxin as the implant biodegrades when the implant is located in a patient's body. In one embodiment, an implant includes a botulinum toxin, a biodegradable polymer, and either monomers from which a biodegradable polymer is derived or oligomers including monomeric units substantially identical to a monomer from which a biodegradable polymer is derived, or a combination of such monomers and oligomers. The oligomers and biodegradable polymer may be derived from a single type of monomer. The implants disclosed herein may be administered to a human or animal patient in which a therapeutic effect is desired for prolonged periods of time.

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15-03-2012 дата публикации

Compounds and their uses 708

Номер: US20120065214A1
Принадлежит: AstraZeneca AB

The present invention relates to pyrazinone derivatives of formula (I): wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 and R 7 are as herein defined; processes for their preparation, pharmaceutical compositions containing them and their use in therapy.

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15-03-2012 дата публикации

Benzothiazole Derivatives

Номер: US20120065403A1
Принадлежит: Biotie Therapies Inc

Provided are compounds and their pharmaceutically acceptable salts that are useful for the treatment of diseases related to the adenosine receptor. Also included are methods of treating patients suffering from or susceptible to at least one symptom of abuse of, dependence on, or withdrawal from at least one substance.

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22-03-2012 дата публикации

Methods for Treating Cognitive/Attention Deficit Disorders Using Tetrahydroindolone Analogues and Derivatives

Номер: US20120070385A1
Принадлежит: Spectrum Pharmaceuticals Inc

The present specification discloses tetrahydroindolone derivatives or analogues and methods for treating cognitive/attention deficit disorders using such tetrahydroindolone derivatives and analogues.

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22-03-2012 дата публикации

Brain-derived gonadotropins and cognition

Номер: US20120070445A1
Принадлежит: Individual

A method of treating or preventing neurodegenerative disease in a subject, the method includes administering to the subject a therapeutically effective amount of at least one physiologically acceptable agent that modulates levels, production, and/or function of brain-derived hormones of the hypothalamic-pituitary-gonadal (HPG) axis or their receptors.

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22-03-2012 дата публикации

Pharmaceutical preparation for the treatment of the symptoms of addiction and method of diagnosing same

Номер: US20120070504A1
Автор: Joan M. Fallon
Принадлежит: Curemark LLC

A therapeutic agent for the treatment of the symptoms of addiction and the method for preparing the therapeutic agent is disclosed. The therapeutic agent is a stable pharmaceutical preparation containing, but not limited to, digestive/pancreatic enzymes. The therapeutic agent may be manufactured by a variety of encapsulation technologies. Delivery of the therapeutic agent may be made orally, through injection, by adherence of a medicated patch or other method. Further, a method of using of a biomarker, the presence of chymotrypsin in the gastrointestinal tract to determine the presence of symptoms of addiction, and the likelihood of relapsing into addiction is disclosed.

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22-03-2012 дата публикации

Method of extraction from withania somnifera and one or more fractions containing pharmacologically active ingredients obtained therefrom

Номер: US20120070521A1
Принадлежит: Bio Ved Pharmaceuticals PVT Ltd

A method of obtaining one or more fractions from a plant material of Withania somnifera (WS) is disclosed. The method includes subjecting the plant material to hydro-alcoholic extraction in presence of a water-insoluble solvent to obtain at least one extract. The method further includes subjecting the at least one extract obtained from the hydro-alcoholic extraction to at least one of de-pigmentation, de-fatting and detoxification process to obtain the one or more fractions. The one or more fractions thus obtained contain Withaferin A in a concentration greater than concentrations of other pharmacologically active ingredients present in the one or more fractions. The one or more fraction thus obtained and one or more compositions containing the one or more fractions are effective in inhibiting proliferation of mammalian cancerous cells.

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22-03-2012 дата публикации

Dihydrobenzoxathiazepine compounds, a process for their preparation and pharmaceutical compositions containing them

Номер: US20120071462A1
Принадлежит: Laboratoires Servier SAS

Compounds of formula (I): wherein R 1 represents a hydrogen atom or a heterocyclic, cyano, alkoxycarbonyl, alkylsulphonylaminoalkyl or N-hydroxycarboximidamide group. Medicinal products containing the same which are useful as modulators of the AMPA receptor.

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22-03-2012 дата публикации

Therapeutic approaches for treating alzheimer disease and related disorders through a modulation of cell stress response

Номер: US20120071483A1
Принадлежит: Pharnext SA

The present invention relates to compositions and methods for the treatment of Alzheimer's disease and related disorders. More particularly, the invention relates to combined therapies that modulate cell stress response for treating said disease.

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22-03-2012 дата публикации

Substituted pyridine derivatives, pharmaceutical compositions, and methods of use to treat oxidative stress

Номер: US20120071505A1
Принадлежит: High Point Pharnaceuticals LLC

Substituted pyridine derivatives, methods of their preparation, pharmaceutical compositions comprising a substituted pyridine derivative, and methods of use in treating inflammation are provided. The substituted pyridine derivatives may control of the activity or the amount or both the activity and the amount of heme-oxygenase.

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22-03-2012 дата публикации

Estrogen receptor modulators and uses thereof

Номер: US20120071535A1
Принадлежит: Aragon Pharmaceuticals Inc

Described herein are compounds that are estrogen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.

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22-03-2012 дата публикации

N-[(2-azabicyclo[2.1.1]hex-1-yl)-aryl-methyl]-benzamide derivatives, preparation thereof, and therapeutic use thereof

Номер: US20120071536A1
Принадлежит: SANOFI SA

The invention relates to N-[(2-aza-bicyclo[2.2.1]hex-1-yl)-aryl-methyl]-benzamide derivatives of the general formula (I) where: R is a hydrogen atom or a (C 1 -C 6 )alkyl group, (C 3 -C 7 )-cycloalkyl, optionally substituted by one or more fluorine, (C 3 -C 7 )-cycloalkyl, (C 2 -C 4 )alkenyl, phenyl, (C 1 -C 6 )alkoxy, hydroxy; R 1 is phenyl or naphtyl optionally substituted by one or more halogen, (C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy, halo-(C 1 -C 6 )alkyl, NR 4 R 5 , (C 1 -C 6 )alkylthio, (C 1 -C 6 )alkyl-SO 2 , phenyl or heteroaryl; R 2 is one or more hydrogen or halogen atoms, halo-(C 1 -C 6 )alkyl, (C 1 -C 6 )alkyl, (C 3 -C 7 )cycloalkyl, (C 3 -C 7 )-cycloalkyl-(C 1 -C 3 )alkyl; R 3 , R 4 and R 5 are independently a hydrogen atom or a (C 1 -C 6 )alkyl group; R 6 is a (C 1 -C 6 )alkyl group; R 3 and R 4 as well as R 3 and R 6 may form, together with the atoms having them, a 5- or 6-member ring; R 4 and R 5 may form together a ring selected from azetidine, pyrrolidine, piperidine, morpholine, thiomorpholine, piperazine, azepine, optionally substituted by a (C 1 -C 6 )alkyl group. The invention also relates to the therapeutic use thereof and to a method for synthesizing same.

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29-03-2012 дата публикации

Methods for Identifying Autophagy Inducing Compounds

Номер: US20120077705A1
Автор: Junying Yuan
Принадлежит: Harvard College

This invention pertains to screening methods for identifying autophagy inducing compounds.

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29-03-2012 дата публикации

Treatment of Central Nervous System Disorders

Номер: US20120077741A1
Принадлежит: NeuroNova AB

The invention relates generally to methods of influencing central nervous system cells to produce progeny useful in the treatment of CNS disorders. More specifically, the invention includes methods of exposing a patient suffering from such a disorder to a reagent that modulates the proliferation, migration, differentiation and survival of central nervous system cells. These methods are useful for reducing at least one symptom of the disorder.

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29-03-2012 дата публикации

Steroid-sparing methods of treating brain edema

Номер: US20120077744A1
Принадлежит: Neutron Ltd

The present invention relates to therapeutic regimens or protocols designed for the treatment, management or prevention of edema. In particular, the invention pertains to methods of treating or managing edema associated with brain tumors involving the administration of a therapeutically effective amount of corticorelin acetate that achieves a steroid-sparing effect.

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29-03-2012 дата публикации

Composition for improving brain function and method for improving brain function

Номер: US20120077752A1
Принадлежит: Individual

The present invention provides a composition which may be ingested orally in a small dose for the purpose of improving brain function, and a method for improving brain function. The present invention is a composition for improving brain function, comprising, as an active ingredient, Phe-Pro.

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29-03-2012 дата публикации

Heterocyclic compound and use thereof

Номер: US20120077799A1
Принадлежит: Takeda Pharmaceutical Co Ltd

Provided is a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof, which has an AMPA (α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid) receptor potentiating action. The compound of the present invention is useful as a prophylactic or therapeutic drug for depression, schizophrenia, Alzheimer's disease or attention deficit hyperactivity disorder (ADHD) and the like.

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29-03-2012 дата публикации

Sulfonamide, sulfamate, and sulfamothioate derivatives

Номер: US20120077814A1
Принадлежит: Individual

The disclosure provides biologically active compounds of formula (I): and pharmaceutically acceptable salts thereof, compositions containing these compounds, and methods of using these compounds in a variety applications, such as treatment of diseases or disorders associated with E1 type activating enzymes, and with Nedd8 activating enzyme (NAE) in particular.

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29-03-2012 дата публикации

Heterocyclic compounds and their use as glycogen synthase kinase-3 inhibitors

Номер: US20120077840A1
Принадлежит: Abbott GmbH and Co KG

The present invention relates to novel heterocyclic compounds which are useful for inhibiting glycogen synthase kinase 3 (GSK-3), methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.

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05-04-2012 дата публикации

Botulinum Neurotoxin B Receptors and Use Thereof

Номер: US20120082672A1
Принадлежит: Individual

It is disclosed here that synaptotagmin I (syt I) and synaptotagmin II (syt II) are the cellular receptors for botulinum neurotoxin B (BoNT/B) that mediate the cellular entry and toxicity of BoNT/B. The BoNT/B binding domains of syt I and II are also disclosed. While syt I needs gangliosides for BoNT/B binding, syt II can bind to BoNT/B in the absence of gangliosides. Various nucleic acids and polypeptides that relate to the BoNT/B binding domain of syt I or II are disclosed. Further disclosed are methods of reducing BoNT/B toxicity, methods of identifying agents that can block the binding between BoNT/B and syt I or II, methods of identifying agents that can bind to the BoNT/B binding domain of syt I or II, methods of detecting BoNT/B or Clostridium botulinum and kits for use thereof.

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05-04-2012 дата публикации

Methods For Modulating The Development Of Dopamine Neuron By The Dopamine D2 Receptor And Compositions Thereof

Номер: US20120083002A1
Автор: Ja hyun Baik, Sung Yul Kim

The present invention relates to a composition for modulating the activation of Nurr1, the composition comprising an agonist or an antagonist of a dopamine D2 receptor, methods for modulating the activation of Nurr1 by the dopamine D2 receptor, a method and composition for treating Nurr1-related diseases using the dopamine D2 receptor, and methods for screening a modulator of a dopamine D2 receptor of a test compound. Accordingly, the activation of Nurr1 can be modulated by treating the dopaminergic neurons with the agonist or the antagonist of the dopamine D2 receptor, thereby enhancing or inhibiting generation of the dopaminergic neurons.

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05-04-2012 дата публикации

Bis-pyridylpyridones as melanin-concentrating hormone receptor antagonists

Номер: US20120083489A1
Принадлежит: GlaxoSmithKline LLC

The invention provides novel bis-pyridylpyridones which are antagonists at the melanin-concentrating hormone receptor 1 (MCHR1), pharmaceutical compositions containing them, processes for their preparation, and their use in therapy and for the treatment of obesity and diabetes.

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05-04-2012 дата публикации

Alpha-2b receptor agonist and anticonvulsant compositions for treating chronic pain

Номер: US20120083508A1
Принадлежит: Allergan Inc

Disclosed herein is a pharmaceutical composition comprising a pain-relieving anticonvulsant and an alpha-2B receptor agonist. The composition is effective for treating chronic pain, and methods of treating chronic pain using the composition and the compounds comprising it are also disclosed.

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12-04-2012 дата публикации

Methods for distributing agents to areas of brain

Номер: US20120087869A1
Принадлежит: MEDTRONIC INC

Broad cerebrospinal fluid (CSF) distribution of an agent is achievable by delivering the agent in a liquid formulation to the CSF at flow rates less than 500 microliters per hour, such as between about 2 microliters per hour and about 100 microliters per hour.

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12-04-2012 дата публикации

Mu-Conotoxin Peptides and Use Thereof as a Local Anesthetic

Номер: US20120087969A1

In one embodiment, the present invention relates to novel mu-conotoxin peptides, biologically active fragments thereof, combinations thereof and/or variants thereof. An embodiment of the invention also relates to their use in pharmaceutical composition for the treatment or prevention of pain, and their use in the preparation of an anesthetic.

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12-04-2012 дата публикации

Extended release opioid abuse deterrent compositions and methods of making same

Номер: US20120087982A1
Принадлежит: Acura Pharmaceuticals Inc

This invention relates to an abuse deterrent dosage form of opioid analgesics, wherein an analgesically effective amount of opioid analgesic is combined with a polymer to form a matrix.

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12-04-2012 дата публикации

Compositions for treating cmt and related disorders

Номер: US20120088744A1
Принадлежит: Pharnext SA

The present invention relates to compositions and methods for the treatment of the Charcot-Marie-Tooth disease and related disorders.

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12-04-2012 дата публикации

Chemically modified small molecules

Номер: US20120088745A1
Принадлежит: Individual

Methods of modifying the rate of systemic absorption of a drug administered to a subject by a pulmonary route, the method comprising covalently conjugating a hydrophilic polymer to a drug, wherein the drug has a half-life of elimination from the lung of less than about 180 minutes, to form a drug-polymer conjugate, wherein the drug-polymer conjugate has a net hydrophilic character and a weight average molecular weight of from about 50 to about 20,000 Daltons, and wherein the half-life of elimination from the lung of the drug-polymer conjugate is at least about 1.5-fold greater than the half-life of elimination from the lung of the drug, wherein the half-life of elimination from the lung is measured by bronchoalveolar lavage followed by assaying residual lung material.

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12-04-2012 дата публикации

Amide derivatives as ion-channel ligands and pharmaceutical compositions and methods of using the same

Номер: US20120088746A1
Принадлежит: PFIZER INC

Compounds are disclosed that have a formula represented by the following: Formula (I). The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, traumatic injury, and others.

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12-04-2012 дата публикации

5-ht1a receptor subtype agonist

Номер: US20120088777A1
Принадлежит: Otsuka Pharmaceutical Co Ltd

The present invention relates to a method of treating a patient suffering from a disorder of the central nervous system associated with 5-HT 1A receptor subtype, comprising as an active ingredient a carbostyril derivative or a salt thereof represented by the formula (1): wherein the carbon-carbon bond between 3- and 4-positions in the carbostyril skeleton is a single or a double bond.

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