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Небесная энциклопедия

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

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Мониторинг СМИ

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

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Поддерживает ввод нескольких поисковых фраз (по одной на строку). При поиске обеспечивает поддержку морфологии русского и английского языка
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Применить Всего найдено 12589. Отображено 100.
26-01-2012 дата публикации

Platinum (ii) tetradentate oncn complexes for organic light-emitting diode applications

Номер: US20120018711A1
Принадлежит: University of Hong Kong HKU

Described are novel platinum (II) containing organometallic materials. These materials show green to orange emissions with high emission quantum efficiencies. Using the materials as emitting materials; pure green emitting organic light-emitting diodes can be fabricated. Since the novel platinum (II) containing organometallic materials are soluble in common solvents, solution process methods such as spin coating and printing can be used for device fabrication.

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26-01-2012 дата публикации

Derivatives of n-(arylamino)sulfonamides as inhibitors of mek

Номер: US20120022076A1
Принадлежит: Individual

This invention concerns N-(2-arylamino)aryl sulfonamides, which are inhibitors of MEK and are useful in treatment of cancer and other hyperproliferative diseases.

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09-02-2012 дата публикации

Charge transport compositions and electronic devices made with such compositions

Номер: US20120032158A1
Принадлежит: EI Du Pont de Nemours and Co

The present invention is directed to a photoactive device comprising an anode, a cathode, and a photoactive layer, which device further comprises an electron transport and/or anti-quenching layer which minimizes both electron transfer quenching and energy transfer quenching of the photoactive layer.

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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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03-05-2012 дата публикации

Nitrogen-Containing Ligands And Their Use In Atomic Layer Deposition Methods

Номер: US20120108062A1
Принадлежит: Applied Materials Inc

Methods for deposition of elemental metal films on surfaces using metal coordination complexes comprising nitrogen-containing ligands are provided. Also provided are nitrogen-containing ligands useful in the methods of the invention and metal coordination complexes comprising these ligands.

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10-05-2012 дата публикации

Derivatives of 1-phenyl-2-pyridinyl alkyl alcohols as phosphodiesterase inhibitors

Номер: US20120116091A1
Принадлежит: Chiesi Farmaceutici SpA

Derivatives of 1-phenyl-2-pyridinyl alkyl alcohols are useful as inhibitors of the phosphodiesterase 4 (PDE4) enzyme.

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24-05-2012 дата публикации

Cadherin-11 inhibitors and methods of use thereof

Номер: US20120128693A1
Принадлежит: GEORGETOWN UNIVERSITY

Cadherin-11 inhibitors and methods for the prevention and treatment of cadherin-11 related diseases are described herein. Cadherin-11 related diseases include cancer and rheumatoid arthritis.

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24-05-2012 дата публикации

Piperazinyl derivatives useful as modulators of the neuropeptide y2 receptor

Номер: US20120129870A1
Принадлежит: Janssen Pharmaceutica NV

The present invention is directed to piperidinyl and piperazinyl derivatives of formula (II) useful as inhibitors of the NPY Y2 receptor, pharmaceutical compositions comprising said compounds, processes for the preparation of said compounds and the use of said compounds for the treatment and/or prevention of disorders, diseases and conditions mediated by the NPY Y2 receptor.

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07-06-2012 дата публикации

Method for synthesis of secondary alcohols

Номер: US20120142934A1
Принадлежит: National Tsing Hua University NTHU

A method for synthesis of secondary alcohols is provided for pharmaceutical secondary alcohol by addition of organoboronic acids with aldehydes in presence of the cobalt ion and bidentate ligands as the catalyst. In addition, an enantioselective synthesis method for secondary alcohols is also herein provided in the present invention. The present invention has advantages in using less expensive cobalt ion and commercially available chiral ligands as the catalyst, wide scope of organoboronic acids and aldehydes compatible with this catalytic reaction and achieving excellent yields and/or enantiomeric excess.

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21-06-2012 дата публикации

Phosphorous derivatives as chemokine receptor modulators

Номер: US20120157413A1
Принадлежит: Allergan Inc

The present invention relates to novel phosphorous derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.

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26-07-2012 дата публикации

Process for the preparation of 4-amino-5-fluoro-3-halo-6-(substituted)picolinates

Номер: US20120190860A1
Принадлежит: DOW AGROSCIENCES LLC

4-Amino-5-fluoro-3-halo-6-(substituted)picolinates are conveniently prepared from 4,5,6-trichloropicolinates by a series of steps involving fluorine exchange, amination, halogen exchange, halogenation and transition metal assisted coupling.

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02-08-2012 дата публикации

Electrochromic compound, electrochromic composition, and display element

Номер: US20120194894A1
Принадлежит: Ricoh Co Ltd

Disclosed are electrochromic compounds represented by the formulas defined in the specification.

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02-08-2012 дата публикации

Glycine transporter-1 inhibitors

Номер: US20120195985A1
Принадлежит: AMGEN INC

The present invention provides compounds that are glycine transporter 1 (hereinafter referred to as GlyT-1) inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of GlyT-1 such as cognitive disorders associated with Schizophrenia, ADHD (attention deficit hyperactivity disorder), MCI (mild cognitive impairment), and the like. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.

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23-08-2012 дата публикации

New compounds, pharmaceutical compositions and uses thereof

Номер: US20120214785A1
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

The invention relates to new compounds of the formula I to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.

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30-08-2012 дата публикации

Guanidine-containing compounds useful as muscarinic receptor antagonists

Номер: US20120219509A1
Принадлежит: Theravance Inc

The invention provides compounds of formula I: or a pharmaceutically acceptable salt thereof, wherein R 1-3 , R 5-7 , a, X, Y, Y′, Y″, and Z are as defined in the specification. These compounds are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes for preparing such compounds and methods of using such compounds to, for example, treat pulmonary disorders such as chronic obstructive pulmonary disease and asthma.

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30-08-2012 дата публикации

2-phenylethylamino derivatives as calcium and/or sodium channel modulators

Номер: US20120220592A1
Принадлежит: Newron Pharmaceuticals SpA

2-Phenylethylamino substituted carboxamide derivatives and their use as sodium and/or calcium channel modulators useful in preventing, alleviating and curing a wide range of pathologies are presented.

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06-09-2012 дата публикации

Compounds, compositions and methods for the treatment of amyloid diseases and synucleinopathies such as alzheimer's disease, type 2 diabetes and parkinson's disease

Номер: US20120225890A1
Принадлежит: ProteoTech Inc

Bis- and tris-dihydroxyaryl compounds and their methylenedioxy analogs and pharmaceutically acceptable esters, their synthesis, pharmaceutical compositions containing them, and their use in the treatment of amyloid diseases, especially Aβ amyloidosis, such as observed in Alzheimer's disease, IAPP amyloidosis, such as observed in type 2 diabetes, and synucleinopathies, such as observed in Parkinson's disease, and the manufacture of medicaments for such treatment.

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13-09-2012 дата публикации

Pharmaceutical, dietary supplement, and food grade salts of anatabine

Номер: US20120232115A1
Принадлежит: Rock Creek Pharmaceuticals Inc

Anatabine is obtained by reacting benzophenoneimine with 3-aminomethyl pyridine to form benzylhydrylidene-pyridin-3-yl-methyl-amine. The benzylhydrylidene-pyridin-3-yl-methyl-amine is treated with a non-nucleophilic base and a dielectrophile, such as cis-1,4-dichloro-2-butene, followed by acidification, then basification, to provide anatabine. The resulting anatabine is substantially free from contaminants and displays good stability. In an alternative embodiment, the benzylhydrylidene-pyridin-3-yl-methyl-amine may be used in the synthesis of other alkaloids such as anabasine, nornicotine, N-methylanabasine, and anabaseine.

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25-10-2012 дата публикации

Heterodimers of Glutamic Acid

Номер: US20120269726A1
Принадлежит: Molecular Insight Pharmaceuticals Inc

Compounds of Formula (Ia) wherein R is a C 6 -C 12 substituted or unsubstituted aryl, a C 6 -C 12 substituted or unsubstituted heteroaryl, a C 1 -C 6 substituted or unsubstituted alkyl or —NR′R′, Q is C(O), O, NR′, S, S(O) 2 , C(O) 2 (CH2)p Y is C(O), O, NR′, S, S(O) 2 , C(O) 2 (CH2)p Z is H or C 1 -C 4 alkyl, R′ is H, C(O), S(O) 2 , C(O) 2 , a C 6 -C 12 substituted or unsubstituted aryl, a C 6 -C 12 substituted or unsubstituted heteroaryl or a C 1 -C 6 substituted or unsubstituted alkyl, when substituted, aryl, heteroaryl and alkyl are substituted with halogen, C 1 -C 12 heteroaryl, —NR′R′ or COOZ, which have diagnostic and therapeutic properties, such as the treatment and management of prostate cancer and other diseases related to NAALADase inhibition. Radiolabels can be incorporated into the structure through a variety of prosthetic groups attached at the X amino acid side chain via a carbon or hetero atom linkage.

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25-10-2012 дата публикации

Aryl compounds as ppar ligands and their use

Номер: US20120271055A1

The present invention relates to a compound as a peroxisome proliferator activated receptor (PPAR) activator and a hydrate, a solvate, a stereoisomer and a pharmaceutically acceptable salt thereof, and a pharmaceutical composition, a cosmetic composition, a muscle strengthening agent, a memory improving agent, a therapeutic agent for dementia and Parkinson's disease, a functional food and a feed composition containing the same.

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01-11-2012 дата публикации

Ethanamine Compounds and Methods of Using the Same

Номер: US20120277272A1
Принадлежит: AstraZeneca AB

(S)-2-methyl- 1 -phenyl-2-(pyridin-2-yl)propan-1-amine, pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising the same, uses of said compound or salt for therapy of depression and other conditions, and methods of treating depression and other conditions by administering said compound or salt.

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08-11-2012 дата публикации

[4-(5-aminomethyl-2-fluoro-phenyl)-piperidin-1-yl]-[7-fluoro-1-(2-methoxy-ethyl)-4-trifluoromethoxy-1h-indol-3-yl]-methanone as an inhibitor of mast cell tryptase

Номер: US20120283445A1
Принадлежит: SANOFI SA

The present invention is directed to an indole benzylamine compound of formula I: useful as an inhibitor of tryptase. In addition, the present invention is directed to the use of the compound for treating a patient suffering from, or subject to, a physiological condition in need of amelioration by inhibition of tryptase, comprising administering to the patient of a therapeutically effective amount of the compound, and to a pharmaceutical composition comprising a pharmaceutically effective amount of the compound of formula I, and a pharmaceutically acceptable carrier.

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14-03-2013 дата публикации

Novel amides as fungicides

Номер: US20130065922A1
Принадлежит: SYNGENTA CROP PROTECTION LLC

Compounds of the general formula (I), wherein the substituents are as defined in claim 1 , are useful as fungicides.

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28-03-2013 дата публикации

PYRIDYL-2-METHYLAMINO COMPOUNDS, COMPOSITIONS AND USES THEREOF

Номер: US20130079376A1
Принадлежит:

Compounds are provided according to formula I: 2. (canceled)5. (canceled)6. (canceled)7. (canceled)8. The method according to ; wherein R′″ is H.9. The method according to ; wherein Ris H or Me.10. The method according to ; wherein Ris H.11. The method according to ; wherein Ris H.12. The method according to ; wherein Ris H.13. The method according to ; wherein Ris H.16. (canceled)17. (canceled)18. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a pharmaceutically effective amount of .19. (canceled)21. The method according to claim 1 , wherein the medical condition is selected from Alzheimer's disease claim 1 , Down's syndrome claim 1 , and Parkinson's disease.22. (canceled)23. (canceled)24. The method according to claim 1 , wherein the medical condition is associated with modulation of Aβ production.25. The method according to claim 1 , wherein the medical condition is associated with inhibition of Aβ production.26. The method according to claim 1 , wherein the medical condition is associated with modulation of APP expression or APP translation.27. A method for lowering the load of Aβ plaque claim 1 , which comprises administering to the mammal an effective treating amount of a compound according to formula I claim 1 , IVa claim 1 , IVb claim 1 , or V.28. A method for lowering the brain Aβ level claim 1 , which comprises administering to the mammal an effective treating amount of a compound according to formula I claim 1 , IVa claim 1 , IVb claim 1 , or V. The present application claims the benefit under 35 U.S.C. §119 of U.S. Provisional Application Ser. No. 61/505,511, filed Jul. 7, 2011. The content of said provisional application is hereby incorporated by reference in its entirety.Provided herein are pyridylmethylamine compounds with anti-Aβ production, aggregation, inhibition of oxidative stress, and modulation of amyloid precursor protein (APP) translation properties, and pharmaceutical compositions thereof. Also provided are ...

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02-05-2013 дата публикации

Chemical Compounds

Номер: US20130109708A1
Принадлежит: Pfizer Ltd

The invention relates to sulfonamide derivatives, to their use in medicine, to 5 compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to a new sulfonamide Nav1.7 inhibitors of formula (I):10 X NH O S O O R1 R2 R5 R4 R3 Het1 (I) or a pharmaceutically acceptable salt thereof, wherein X, Het1, R1, R2, R3, R4 and R5 are as defined in the description. 15 Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain.

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16-05-2013 дата публикации

Styryl-based compound, composition containing styryl-based compound, and organic light emitting diode including styryl-based compound

Номер: US20130119355A1
Принадлежит: Samsung Display Co Ltd

A styryl-based compound represented by Formula 1, a composition containing the styryl-based compound, and an organic light-emitting diode (OLED) including the styryl-based compound: The styryl-based compound may exhibit high heat resistance and thus an OLED including the same may have low driving voltage, high brightness, high efficiency, and long lifetime.

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23-05-2013 дата публикации

NOVEL TRPV3 MODULATORS

Номер: US20130131036A1
Принадлежит: AbbVie Inc.

Disclosed herein are modulators of TRPV3 of formula (II): 2. The compound according to claim 1 , or a salt thereof claim 1 , wherein u is 0.3. The compound according to claim 2 , or a salt thereof claim 2 , wherein:{'sup': '1', 'Gis optionally substituted heteroaryl or optionally substituted cycloalkyl;'}{'sup': 2', '2d, 'Gis G; and'}{'sup': '2d', 'Gis optionally substituted aryl or optionally substituted heteroaryl.'}4. The compound according to claim 2 , or a salt thereof claim 2 , wherein:{'sup': '1', 'Gis optionally substituted pyridinyl, pyrimidinyl, thiazolyl, oxazolyl, or pyrazolyl;'}{'sup': 2', '2d, 'Gis G; and'}{'sup': '2d', 'Gis optionally substituted phenyl or optionally substituted pyridinyl.'}5. The compound according to claim 2 , or a salt thereof claim 2 , wherein:{'sup': 1', 'gc, 'sub': 1', '6', '1', '6', '2, 'Gis pyridinyl or pyrimidinyl; each of which is optionally substituted with 1, 2, or 3 substituents independently selected from the group consisting of halogen, C-C-alkyl, C-C-haloalkyl, and N(R);'}{'sup': 'gc', 'sub': 1', '6, 'Ris hydrogen or C-C-alkyl;'}{'sup': 2', '2d, 'Gis G;'}{'sup': 2d', 'f, 'sub': 1', '6', '1', '6, 'Gis phenyl, pyridinyl, or pyrimidinyl; each of which is optionally substituted with 1, 2, or 3 substituents independently selected from the group consisting of halogen, —CN, C-C-alkyl, C-C-haloalkyl, and —OR; and'}{'sup': 'f', 'sub': 1', '6', '1', '6, 'Ris C-C-alkyl or C-C-haloalkyl.'}6. The compound according to claim 2 , or a salt thereof claim 2 , wherein:{'sup': 1', 'gc, 'sub': 1', '4', '1', '4', '2, 'Gis pyridinyl which is optionally substituted with 1 or 2 substituents independently selected from the group consisting of halogen, C-C-alkyl, C-C-haloalkyl, and N(R);'}{'sup': 'gc', 'sub': 1', '4, 'Ris hydrogen or C-C-alkyl;'}{'sup': 2', '2d, 'Gis G;'}{'sup': 2d', 'f, 'sub': 1', '4', '1', '4, 'Gis phenyl or pyridinyl; each of which is optionally substituted with 1, 2, or 3 substituents independently selected from the group ...

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30-05-2013 дата публикации

HETEROARYL (ALKYL) DITHIOCARBAMATE COMPOUNDS, PREPARATION METHODS AND USES THEREOF

Номер: US20130136794A1
Принадлежит: PEKING UNIVERSITY

Heteroaryl(alkyl)dithiocarbamate compounds represented by general formula (I) or their pharmaceutically acceptable salts, their preparing methods, and their uses for preparing antitumor medicines are disclosed, wherein each said substituent is defined as in the description. The compounds are new tyrosine kinase inhibitors useful as an anti-tumor agents, preferably useful in the preparation of medicines for treating breast cancer, liver cancer, non-small cell lung cancer, gastric cancer, colon cancer, leukaemia or nasal cancer. 2. The compound according to claim 1 , wherein the group A is substituted or unsubstituted heterocyclic group claim 1 , is the heterocyclic group being selected from pyridyl claim 1 , pyrimidinyl claim 1 , pyrazinyl claim 1 , furyl claim 1 , oxazolyl claim 1 , pyrazolyl claim 1 , thiazolyl or oxadiazolyl; preferably the group A is substituted or unsubstituted pyridyl claim 1 , or pyridyl fused with benzene or morpholine ring claim 1 , the fused benzene or morpholine ring being unsubstituted or substituted with methyl.3. The compounds according to claim 2 , wherein the Calkyl is methyl claim 2 , the Calkoxy is methoxy claim 2 , the Calkoxycarbonyl is methoxycarbonyl claim 2 , and/or the Calkylamido is pentylamido .4. The compound according to claim 3 , wherein the Rgroup is cyano.5. The compound according to claim 1 , wherein the compound is:3-(furan-2-ylmethyl)-4-hydroxy-1,3-thiazinane-2-thione (compound 1);2-(methoxycarbonyl)ethyl(furan-2-ylmethyl)dithiocarbamate (compound 2);2-cyanoethyl(furan-2-ylmethyl)dithiocarbamate (compound 3);3-(furan-2-ylmethyl)-4-hydroxy-4,5-dimethyl-3,4-dihydro-2H-1,3-thiazine-2-thione (compound 4);2-sulfamoylethyl(furan-2-ylmethyl)dithiocarbamate (compound 5);2-boronoethyl(furan-2-ylmethyl)dithiocarbamate (compound 6);2-(methylsulfinyl)ethyl(furan-2-ylmethyl)dithiocarbamate (compound 7);2-(benzylsulfinyl)ethyl(furan-2-ylmethyl)dithiocarbamate (compound 8);4-hydroxy-3-(pyridin-3-ylmethyl)-1,3-thiazinane-2-thione ( ...

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30-05-2013 дата публикации

4-carboxybenzylamino derivatives as histone deacetylase inhibitors

Номер: US20130137690A1
Принадлежит: Individual

The present invention relates to a novel class of 4-carboxybenzylamino derivatives. The 4-carboxybenzylamino compounds can be used to treat cancer. The 4-carboxybenzylamino compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases. The present invention further provides pharmaceutical compositions comprising the 4-carboxybenzylamino derivatives and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of the 4-carboxybenzylamino derivatives in vivo.

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30-05-2013 дата публикации

ETHANAMINE COMPOUNDS AND METHODS OF USING THE SAME

Номер: US20130137731A1
Принадлежит: AstraZeneca AB

The present invention is directed to ethanamine compounds, pharmaceutical compositions comprising the same, and methods of treatingh depression by administering the ethanamine compound. 148-. (canceled)49. 2-Methyl-1-phenyl-2-(pyridin-2-yl)propan-1-amine or a pharmaceutically acceptable salt thereof.50. A compound as claimed in which is 2-methyl-1-phenyl-2-(pyridin-2-yl)propan-1-amine or a hydrochloric claim 49 , hydrobromic claim 49 , sulfuric claim 49 , phosphoric claim 49 , citric claim 49 , tartaric claim 49 , lactic claim 49 , pyruvic claim 49 , acetic claim 49 , succinic claim 49 , fumaric claim 49 , maleic claim 49 , methanesulphonic or benzenesulphonic acid salt thereof.51. A compound as claimed in which is 2-methyl-1-phenyl-2-(pyridin-2-yl)propan-1-amine fumarate.52. A compound as claimed in which is 2-methyl-1-phenyl-2-(pyridin-2-yl)propan-1-amine.53. A compound as claimed in which is (S)-2-methyl-1-phenyl-2-(pyridin-2-yl)propan-1-amine or a pharmaceutically acceptable salt thereof.54. A compound as claimed in which is (S)-2-methyl-1-phenyl-2-(pyridin-2-yl)propan-1-amine or a hydrochloric claim 49 , hydrobromic claim 49 , sulfuric claim 49 , phosphoric claim 49 , citric claim 49 , tartaric claim 49 , lactic claim 49 , pyruvic claim 49 , acetic claim 49 , succinic claim 49 , fumaric claim 49 , maleic claim 49 , methanesulphonic or benzenesulphonic acid salt thereof.55. A compound as claimed in which is (S)-2-methyl-1-phenyl-2-(pyridin-2-yl)propan-1-amine fumarate.56. A compound as claimed in which is (S)-2-methyl-1-phenyl-2-(pyridin-2-yl)propan-1-amine.57. A method of treating depression in a human which comprises administering to a person in need thereof a therapeutic effective amount of a compound or a pharmaceutically acceptable salt thereof claim 49 , where the compound is 2-methyl-1-phenyl-2-(pyridin-2-yl)propan-1-amine.58. A method of treating depression in a human as claimed in which comprises administering to a person in need thereof a therapeutic ...

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06-06-2013 дата публикации

Guanidine compound

Номер: US20130143860A1
Принадлежит: Astellas Pharma Inc

[Problem] The present invention provides a compound which is useful as an active ingredient of a pharmaceutical composition, in particular, a pharmaceutical composition for preventing and/or treating VAP-1-related diseases. [Means for Solution] The present inventors have conducted intensive studies on a compound having a VAP-1 inhibitory activity, and as a result, they have found that the compound or a salt thereof of the present invention exhibits an excellent VAP-1 inhibitory activity and is useful for preventing and/or treating VAP-1-related diseases, in particular, diabetic nephropathy or diabetic macular edema, thereby completing the present invention. In addition, the present invention relates to a pharmaceutical composition, in particular, a pharmaceutical composition for preventing and/or treating VAP-1-related diseases, which comprises the compound or a salt thereof of the present invention, and an excipient.

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06-06-2013 дата публикации

Bis-pyrinidium compounds

Номер: US20130143928A1
Принадлежит: UNIVERSITY OF SYDNEY

A method of treating, inhibiting, or preventing an infection in a subject is described. The method comprises administering to the subject an effective amount of at least one bis-pyridinium compound. The bis-pyridinium compound comprises two aromatic ring structures. Each of the ring structures comprises a pyridine ring, and the ring structures are linked by a linker group of at least 8 atoms in length, said linker group being attached to the nitrogen atoms of the pyridine rings. At least one substituent on at least one of the ring structures is an alkyl group having at least 2 carbon atoms, and no substituent on either of the ring structures is —OH, —SH or an amine group.

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13-06-2013 дата публикации

PHENYLTHIOACETATE COMPOUNDS, COMPOSITIONS AND METHODS OF USE

Номер: US20130150381A1
Принадлежит: ARDEA BIOSCIENCE, INC.

Described herein are compounds useful in the modulation of blood uric acid levels, formulations containing them and methods of using them. In some embodiments, the compounds described herein are used in the treatment or prevention of dis orders related to aberrant levels of uric acid. 2. (canceled)4. A compound of claim 3 , wherein{'sup': 'y', 'Ris H; and'}{'sup': 'z', 'Ris H.'}5. A compound of claim 4 , wherein Ris CN claim 4 , CHOH or C(O)NH.6. A compound of claim 5 , wherein M is H.7. A compound of claim 5 , wherein M is a pharmaceutically acceptable cation.8. A compound of claim 3 , wherein{'sup': a', 'b, 'sub': 3', '3, 'Ris CHand Ris CH; or'}{'sup': a', 'b, 'Rand Rtogether with the carbon atom to which they are attached form a cyclobutyl ring.'}9. A compound of claim 3 , wherein{'sup': 'w', 'Ris H;'}{'sup': 'x', 'sub': 2', '2, 'Ris CN, CHOH or C(O)NH;'}{'sup': 'y', 'Ris H;'}{'sup': 'z', 'Ris H;'}M is H; and{'sup': a', 'b, 'sub': 3', '3, 'Ris CHand Ris CH; or'}{'sup': a', 'b, 'Rand Rtogether with the carbon atom to which they are attached form a cyclobutyl ring.'}10. (canceled)12. (canceled)14. A compound of claim 1 , wherein{'sup': 'a', 'sub': '3', 'Ris CH; and'}{'sup': 'b', 'sub': '3', 'Ris CH.'}15. A compound of claim 1 , wherein Rand Rtogether with the carbon atom to which they are attached form a 3- claim 1 , 4- claim 1 , 5- or 6-membered ring.17. A compound of claim 1 , wherein each R claim 1 , R claim 1 , Rand Ris H.18. A compound of claim 1 , wherein{'sup': 1', '2', '3', '4, 'each R, R, Rand Ris H;'}W is CH; and{'sup': 'x', 'X is CR.'}19. A compound of claim 1 , wherein Ris fluorine.23. (canceled)24. (canceled)25. (canceled)26. (canceled)27. The method of claim 22 , wherein the condition is gout claim 22 , a recurrent gout attack claim 22 , gouty arthritis claim 22 , hyperuricaemia claim 22 , hypertension claim 22 , a cardiovascular disease claim 22 , coronary heart disease claim 22 , Lesch-Nyhan syndrome claim 22 , Kelley-Seegmiller syndrome claim 22 , ...

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13-06-2013 дата публикации

Novel trpv3 modulators

Номер: US20130150409A1
Принадлежит: AbbVie Inc

Disclosed herein are modulators of TRPV3 of formula (I) wherein G 1 , X 1 , X 2 , X 3 , X 4 , X 5 , G 2 , Z 1 , R a , R b , u, and p are as defined in the specification. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also presented.

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01-08-2013 дата публикации

CYCLOPROPYLAMINE DERIVATIVES USEFUL AS LSD1 INHIBITORS

Номер: US20130197013A1
Принадлежит:

The invention relates to cyclopropylamine compounds, in particular the compounds of Formula (I), and their use in therapy, including e.g. in the treatment or prevention of cancer, a neurological disease or condition, or viral infection. 4. The compound of wherein (G) is a heterocyclyl.5. (canceled)6. The compound of wherein (G) is phenyl.78-. (canceled)9. The compound of wherein E is —X═X— claim 1 , and X claim 1 , X claim 1 , Xand Xare independently C(R2) or N.10. The compound of wherein E is —X═X— claim 1 , and X claim 1 , X claim 1 , Xand Xare independently C(R2).1112-. (canceled)13. The compound of wherein E is —S— claim 1 , and Xand Xare independently C(R2) or N.1420-. (canceled)21. The compound of wherein each (R1) is independently chosen from alkyl claim 1 , aryl claim 1 , amino claim 1 , amido claim 1 , nitro claim 1 , halo claim 1 , haloalkyl claim 1 , haloalkoxy claim 1 , cyano claim 1 , heterocycle claim 1 , sulfonyl claim 1 , sulfonamide claim 1 , hydroxyl claim 1 , or alkoxy.22. The compound of wherein each (R1) is independently chosen from —CF claim 1 , —F claim 1 , —Cl claim 1 , —CN claim 1 , —CH claim 1 , —OH claim 1 , —OCH claim 1 , —C(═O)NH claim 1 , —NH—CO—CH claim 1 , —NH—SO—CH claim 1 , —NH—SO—CH—CH claim 1 , —NH—SO—CH(CH)—CH claim 1 , —NH—SO—(CH) claim 1 , —NH—SO—(CH)—CN claim 1 , —NHSOCF claim 1 , or —S(═O)NHCH.2328-. (canceled)30. The compound of wherein E is —S— or —X═X—.3137-. (canceled)38. The compound of wherein (G) is an aryl or heterocyclyl.3941-. (canceled)42. The compound of wherein each (R1) is independently chosen from alkyl claim 29 , aryl claim 29 , amino claim 29 , amido claim 29 , nitro claim 29 , halo claim 29 , haloalkyl claim 29 , cyano claim 29 , heterocyclyl claim 29 , sulfonyl claim 29 , sulfonamide claim 29 , hydroxyl claim 29 , or alkoxy.4446-. (canceled)47. The compound of wherein (G) is an aryl or heterocyclyl.4850-. (canceled)51. The compound of wherein each (R1) is independently chosen from alkyl claim 43 , aryl ...

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01-08-2013 дата публикации

Method for producing optically active amine compound

Номер: US20130197234A1

The present invention relates to methods for producing an optically active amine compound via a highly enantioselective hydrogenation reaction of an imine compound, wherein the imine compound is hydrogenated using a ruthenium metal complex having high catalytic activity and represented by Formula (1) RuXYAB  (1) such as RuBr 2 [(S,S)-xylskewphos][(S,S)-dpen].

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08-08-2013 дата публикации

SUBSTITUTED 8-ALKOXY-2-AMINOTETRALIN DERIVATIVES, AND USE THEREOF

Номер: US20130203751A1
Принадлежит: Bayer Intellectual Property GmbH

The present application relates to novel substituted 8-alkoxy-2-aminotetraline derivatives, to processes for their preparation, to their use for the treatment and/or prevention of diseases and to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of cardiovascular disorders. 5. (canceled)6. A method for the treatment and/or prevention of heart failure claim 1 , angina pectoris claim 1 , hypertension claim 1 , pulmonary hypertension claim 1 , ischemias claim 1 , vascular disorders claim 1 , thromboembolic disorders and arteriosclerosis comprising administering and effective amount of a compound of to a human or animal in need thereof.7. (canceled)8. A pharmaceutical composition comprising a compound of in combination with one or more inert claim 1 , non-toxic claim 1 , pharmaceutically suitable excipients.9. The pharmaceutical composition of claim 8 , further comprising an at least one active ingredients selected from the group consisting of an organic nitrate claim 8 , an NO donors claim 8 , a cGMP-PDE inhibitor claim 8 , a stimulator of guanylate cyclase claim 8 , an agent having antithrombotic activity claim 8 , an agent lowering blood pressure claim 8 , and an agent altering lipid metabolism.10. (canceled) The present application relates to novel substituted 8-alkoxy-2-aminotetraline derivatives, to processes for their preparation, to their use for the treatment and/or prevention of diseases and to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of cardiovascular disorders.One of the most important cellular transmission systems in mammalian cells is cyclic guanosine monophosphate (cGMP). Together with nitric oxide (NO), which is released from the endothelium and transmits hormonal and mechanical signals, it forms the NO/cGMP system. Guanylate cyclases catalyze the biosynthesis of cGMP from ...

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15-08-2013 дата публикации

Compositions and Methods for Imaging

Номер: US20130209360A1
Принадлежит: UNIVERSITY OF CALIFORNIA

The present disclosure provides compositions for in vivo imaging of hydrogen peroxide; and methods for detecting hydrogen peroxide in vivo. The compositions and methods find use in various diagnostic applications, which are also provided.

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22-08-2013 дата публикации

METHODS OF PRODUCING SULFILIMINE COMPOUNDS

Номер: US20130217883A1
Автор: Adaway Timothy J.
Принадлежит: DOW AGROSCIENCES LLC

Methods of producing a sulfilimine compound, such as N-cyano-S-methyl-S-[1-(6-trifluoromethyl-3-pyridinyl)ethyl]sulfilimine or other substituted sulfilimine compound. The method includes combining a sulfide compound, cyanamide, a hypochlorite compound, and a base, and oxidizing the sulfide compound to form the sulfilimine compound. The sulfide compound may include a 2-trifluoromethyl-5-(1-substituted)alkyl-thiopyridine compound. The base may include sodium hydroxide. A buffer, such as a phosphate buffer, may, optionally, be used in the reaction. 1. A method of producing a sulfilimine compound , comprising:combining a sulfide compound, cyanamide, a hypochlorite compound, and a base; andoxidizing the sulfide compound to form a sulfilimine compound.2. The method of claim 1 , further comprising adding a buffer to the sulfide compound claim 1 , cyanamide claim 1 , hypochlorite compound claim 1 , and base.4. The method of claim 1 , wherein combining a sulfide compound claim 1 , cyanamide claim 1 , a hypochlorite compound claim 1 , and a base comprises combining the sulfide compound claim 1 , cyanamide claim 1 , hypochlorite compound claim 1 , and a base selected from the group consisting of an alkali metal hydroxide claim 1 , an alkali phosphate claim 1 , an alkali metal carbonate claim 1 , and combinations thereof.5. The method of claim 1 , wherein combining a sulfide compound claim 1 , cyanamide claim 1 , a hypochlorite compound claim 1 , and a base to form a sulfilimine compound comprises reacting the sulfide compound claim 1 , cyanamide claim 1 , hypochlorite compound claim 1 , and base at a temperature from about −40° C. to about 30° C.6. A method of producing a sulfilimine compound claim 1 , comprising:combining a 2-trifluoromethyl-5-(1-substituted)alkylthiopyridine compound, cyanamide, a hypochlorite compound, and a base to form a sulfilimine compound.8. The method of claim 6 , wherein combining a 2-trifluoromethyl-5-(1-substituted)alkylthiopyridine compound claim ...

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29-08-2013 дата публикации

SUBSTITUTED HETEROCYCLIC COMPOUNDS FOR DISEASE TREATMENT

Номер: US20130225619A1
Принадлежит: Acucela Inc.

The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are substituted heterocyclic amine derivative compound and pharmaceutical compositions comprising these compounds. The subject compositions are useful for treating and preventing ophthalmic diseases and disorders, including age-related macular degeneration (AMD) and Stargardt's Disease. 14. The compound of wherein Y is alkyl claim 1 , carbocyclyl or heterocyclyl.15. The compound of wherein Y is —C(R)(R)(R);{'sup': 16', '17', '16', '17, 'sub': 1', '13, 'Rand Rare each independently selected from hydrogen, C-Calkyl, halo or fluoroalkyl; or Rand R, together with the carbon to which they are attached form a carbocyclyl or heterocyclyl; and'}{'sup': '18', 'Ris selected from a hydrogen, alkyl, alkoxy, hydroxy, halo or fluoroalkyl.'}16. The compound of wherein Rand R claim 15 , together with the carbon to which they are attached claim 15 , form a carbocyclyl or heterocyclyl.17. The compound of wherein Rand R claim 16 , together with the carbon to which they are attached claim 16 , form a cyclobutyl claim 16 , cyclopentyl claim 16 , cyclohexyl claim 16 , cycloheptyl claim 16 , or cyclooctyl claim 16 , and Ris hydrogen or hydroxy.18. The compound of wherein Rand R claim 17 , together with the carbon to which they are attached claim 17 , form a cyclopentyl claim 17 , cyclohexyl claim 17 , or cycloheptyl claim 17 , and Ris hydrogen or hydroxy.19. The compound of wherein Rand Ris independently selected from C-Calkyl; and Ris hydrogen claim 15 , hydroxy or alkoxy.20. The compound of wherein X is selected from —O—C(R) claim 1 , —S(O)—C(R)— claim 1 , —SO(NR)— claim 1 , —NR—C(R)— claim 1 , —NR—C(═O)— claim 1 , and —NR—S(O)—.21. The compound of wherein X is selected from —C(R)—C(R)— claim 1 , —C(R)═C(R)— claim 1 , —C≡C— claim 1 , —C(═O)—N(R)— claim 1 , —C(R)—O— claim 1 , and —C(R)—NR.22. The ...

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05-09-2013 дата публикации

N-ADAMANTYL BENZAMIDES AS INHIBITORS OF 11-BETA-HYDROXYSTEROID DEHYDROGENASE

Номер: US20130231341A1
Автор: Ebdrup Soren
Принадлежит: HIGH POINT PHARMACEUTICALS, LLC

Novel substituted benzamide based inhibitors, their use in therapy, pharmaceutical compositions comprising the compounds, the use of said compounds in the manufacture of medicaments, and therapeutic methods comprising the administration of said compounds are described. The present compounds modulate the activity of 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, such as the metabolic syndrome. 2. The method of claim 1 , wherein the compound is 4-{2-[3-(5-Hydroxy-adamantan-2-ylcarbamoyl)-phenoxy]-ethyl}-piperidine-1-carboxylic acid isopropylamide or a pharmaceutically acceptable salt thereof.3. The method of claim 1 , wherein the compound is 3-(6-Chloro-pyridin-3-ylmethoxy)-N-(5-hydroxy-adamantan-2-yl)-benzamide or a pharmaceutically acceptable salt thereof.4. The method of claim 1 , wherein the compound is N-(5-Hydroxy-adamantan-2-yl)-3-(tetrahydro-pyran-4-ylmethoxy)-benzamide or a pharmaceutically acceptable salt thereof.5. The method of claim 1 , wherein the compound is N-(5-Hydroxy-adamantan-2-yl)-3-[2-(2-oxo-pyrrolidin-1-yl)-ethoxy]-benzamide or a pharmaceutically acceptable salt thereof.6. The method of claim 1 , wherein the compound is 3-(5-Chloro-pyridin-2-yloxy)-N-(5-hydroxy-adamantan-2-yl)-benzamide or a pharmaceutically acceptable salt thereof.7. The method of claim 1 , wherein the compound is 3-(6-Bromo-pyridin-3-yloxy)-N-(5-hydroxy-adamantan-2-yl)-benzamide or a pharmaceutically acceptable salt thereof.8. The method of claim 1 , wherein the compound is N-(5-Hydroxy-adamantan-2-yl)-3-phenethyloxy-benzamide or a pharmaceutically acceptable salt thereof.9. The method of claim 1 , wherein the compound is N-(5-Hydroxy-adamantan-2-yl)-3-[2-(tetrahydro-pyran-4-yl)-ethoxy]-benzamide or a pharmaceutically acceptable salt thereof.10. The method of claim 1 , wherein the compound is 3-Benzyloxy-N-(5-hydroxy-adamantan-2-yl)-benzamide or a pharmaceutically acceptable ...

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05-09-2013 дата публикации

ARYLOXYUREA COMPOUND AND PEST CONTROL AGENT

Номер: US20130231479A1
Принадлежит:

The present invention provides a pest control agent, acaricide or fungicide that contains, as the active ingredient thereof, at least one type of compound selected from the aryloxyurea compounds represented by formula (V) (wherein Rto Reach independently represents an alkyl group or the like, X is a halogen atom or the like, n is an integer of 0 to 5, and Z is an oxygen atom or sulfur atom) or salts thereof. 3. A pest control agent claim 1 , comprising at least one of the aryloxyurea compound or a salt thereof according to as an active ingredient.4. An acaricide claim 1 , comprising at least one of the aryloxyurea compound or a salt thereof according to as an active ingredient.5. A fungicide claim 1 , comprising at least one of the aryloxyurea compound or a salt thereof according to as an active ingredient.6. A pest control agent claim 2 , comprising at least one of the aryloxyurea compound or a salt thereof according to as an active ingredient.7. An acaricide claim 2 , comprising at least one of the aryloxyurea compound or a salt thereof according to as an active ingredient.8. A fungicide claim 2 , comprising at least one of the aryloxyurea compound or a salt thereof according to as an active ingredient. The present invention relates to a novel pest control agent. More specifically, the present invention relates to an aryloxyurea compound, which is superior in acaricidal activity and/or fungicidal activity, superior in properties and safety, and which can be industrially and advantageously synthesized, and an acaricide and/or fungicide including the aryloxyurea compound as an active ingredient.Priority is claimed on Japanese Patent Application No. 2010-229617, filed Oct. 12, 2010, the content of which is incorporated herein by reference.Compounds represented by formulas (A) to (E), which are structurally relevant to the compound of the present invention, are disclosed in Patent documents 1 to 5.In the formula, Rrepresents a C1-6 alkyl group.Rrepresents a hydrogen ...

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05-09-2013 дата публикации

Use of active ingredients for controlling nematodes in nematode-resistant crops

Номер: US20130232645A1
Принадлежит: Bayer Intellectual Property GmbH

The present invention relates generally to the use of fluopyram and compositions comprising fluopyram for controlling nematodes in nematode resistant crops and/or increasing crop yield and to methods particularly useful for controlling nematodes and/or increasing crop yield in those crops.

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19-09-2013 дата публикации

CYSTEINE PROTEASE INHIBITORS FOR THE TREATMENT OF PARASITIC DISEASES

Номер: US20130244962A1
Принадлежит: Merck Frosst Canada Ltd.

Several parasites responsible for mammalian diseases are dependent on cysteine protease for various life-cycle functions. Inhibition or decreasing function of these proteases can be useful in the treatment and/or prevention of these parasitic diseases including; toxoplasmosis, malaria, African trypanosomiasis, Chagas disease, leishmaniasis, schistosomiasis, amebiasis, giardiasis, clonorchiasis, opisthorchiasis, paragonimiasis, fasciolopsiasis, lymphatic filariasis, onchocerciasis, dracunculiasis, ascariasis, trichuriasis, stronglyoidiasis, trichostrongyliasis, trichomoniasis or cestodiasis. 121.-. (canceled)23. A pharmaceutical composition comprising a compound according to and a pharmaceutically acceptable carrier.24. A pharmaceutical composition of further comprising another agent selected from the group consisting of: nifurtimox claim 23 , benznidazole claim 23 , allopurinol claim 23 , terbinafine claim 23 , lovastatin claim 23 , ketoconazole claim 23 , itraconazole claim 23 , posaconazole claim 23 , miltefosine claim 23 , ilmofosine claim 23 , pamidronate claim 23 , alendronate claim 23 , risedronate claim 23 , chloroquine claim 23 , proguanil claim 23 , mefloquine claim 23 , quinine claim 23 , pyrimethamine-sulphadoxine claim 23 , doxocycline claim 23 , berberine claim 23 , halofantrine claim 23 , primaquine claim 23 , atovaquone claim 23 , pyrimethamine-dapsone claim 23 , artemisinin claim 23 , quinhaosu claim 23 , meglumine antimonite claim 23 , sodium stibogluconate claim 23 , amphotericin B claim 23 , praziquantel claim 23 , oxamniquine claim 23 , pentamidine claim 23 , melarsoprol claim 23 , suramin and eflornithine and the pharmaceutically acceptable salts and mixtures thereof.25. A method of treating a patient having a parasitic disease comprising administering to the patent in need thereof a composition comprising a compound of claim 22 , wherein the parasitic disease is selected from the group consisting of toxoplasmosis claim 22 , malaria claim 22 , ...

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19-09-2013 дата публикации

ACRYLOMIDO DERIVATIVES USEFUL AS INHIBITORS OF THE MITOCHONDRIAL PERMEABILITY TRANSITION

Номер: US20130245019A1
Принадлежит: CONGENIA SRL

Acrylamido derivatives useful as therapeutic agents, particularly for the prevention and/or treatment of diseases and conditions associated with the activity of the mitochondrial permeability transition pore (MPTP), such as the diseases characterized by ischemia/reperfusion, oxidative or degenerative tissue damage, are herein described. These compounds belong to the structural formula (I) wherein R, R′, R″, W and a are as defined in the specification. The invention also relates to the preparation of these compounds, as well as to pharmaceutical compositions comprising them. 110-. (canceled)12. The method according to claim 11 , for the prevention and/or treatment of a diseases resulting from ischemia/reperfusion damage or oxidative damage claim 11 , age-related diseases claim 11 , degenerative and neurodegenerative diseases.13. The method according to claim 12 , for the prevention and/or treatment of acute myocardial infarction claim 12 , heart failure claim 12 , organ ischemia claim 12 , ischemic and traumatic brain damage claim 12 , Duchenne muscular dystrophy claim 12 , Uilrich congenital muscular dystrophy claim 12 , Bentham myopathy claim 12 , amyotrophic lateral sclerosis claim 12 , Huntington's disease claim 12 , Alzheimer's disease claim 12 , Parkinson's disease claim 12 , diabetes type I and type II claim 12 , diabetic complications claim 12 , hyperglycemic tissue damage claim 12 , hypoglycemic tissue damage claim 12 , cholestasis claim 12 , or alcohol-induced damage.1415-. (canceled) The present invention relates to acrylamido derivatives and to their use as therapeutic agents, particularly for the prevention and/or treatment of diseases and conditions associated with the activity of the mitochondrial permeability transition pore (MPTP), such as the diseases characterized by ischemia/reperfusion, oxidative or degenerative tissue damage. The invention also relates to the preparation of these compounds, as well as to pharmaceutical compositions comprising ...

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19-09-2013 дата публикации

PROCESS FOR HOMOGENEOUSLY CATALYZED, HIGHLY SELECTIVE DIRECT AMINATION OF PRIMARY ALCOHOLS WITH AMMONIA TO PRIMARY AMINES WITH A HIGH VOLUME RATIO OF LIQUID PHASE TO GAS PHASE AND/OR HIGH PRESSURES

Номер: US20130245276A1
Принадлежит: EVONIK DEGUSSA GmbH

The present invention relates to a process for preparing primary amines comprising the process steps 1. A process for preparing a primary amine , the process comprisingA)contacting (i) a solution of a primary alcohol in a fluid, nongaseous phase with (ii) free ammonia or an ammonia-releasing compound and (iii) a homogeneous catalyst, to form a primary amine, and optionallyB) isolating the primary aminewherein a volume ratio of a volume of a liquid phase to a volume of a gas phase in the contacting is greater than 0.05 and/orthe contacting is performed at a pressure greater than 10 bar.2. The process of claim 1 , wherein in the contactingthe ammonia is present in a molar ratio based on hydroxyl groups in the primary alcohol of at least 5:1.3. The process of claim 1 , whereinthe primary alcohol comprises a carboxyl or ester group.4. The process of claim 1 , whereinthe primary alcohol comprises an aliphatic alkyl radical comprising at least three carbon atoms covalently bound to one another and no quaternary carbon atom.5. The process of claim 1 , whereinthe primary alcohol comprises no heteroatoms.6. The process of claim 4 , whereinthe aliphatic alkyl radical is a linear or branched alkyl radical comprising at least 4 carbon atoms.7. The process of claim 1 , whereinthe primary alcohol is selected from the group consisting of 1-butanol, 2-methyl-1-propanol, 1-pentanol, 3-methyl-1-butanol, 2-methyl-1-butanol, 1-hexanol, 4-methyl-1-pentanol, 3-methyl-1-pentanol, 2-methyl-1-pentanol, 2-ethyl-1-butanol, tripropylene glycol, an anhydrohexitol, and tripropylene glycol.8. The process of claim 1 , whereina concentration of the primary alcohol in (i) is from 0.1 to 10000 mmol/l.9. The process of claim 1 , whereinthe catalyst is selected from the group consisting of:an alkali metal alkoxide, an aluminum alkoxide, a lanthanide alkoxide,an inorganic compound comprising a noble metal,and a coordination compound comprising one or more noble metals selected from the group consisting ...

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26-09-2013 дата публикации

SULFUR DERIVATIVES AS CHEMOKINE RECEPTOR MODULATORS

Номер: US20130252984A1
Принадлежит: ALLERGAN, INC.

The present invention relates to novel sulfur derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors. 2. A compound according to claim 1 , wherein:{'sup': '5', 'Ris S.'}3. A compound according to claim 1 , wherein:{'sup': '5', 'Ris —S(O)—.'}4. A compound according to claim 1 , wherein:{'sup': '5', 'sub': '2', 'Ris —S(O)—.'}5. A compound according to claim 1 , wherein:{'sup': '1', 'Ris H;'}{'sup': '2', 'sub': 1-6', '3-8', '3-8, 'Ris substituted or unsubstituted Calkyl, substituted or unsubstituted Ccycloalkyl or substituted or unsubstituted Ccycloalkenyl;'}{'sup': '5', 'sub': '2', 'Ris —S—, —S(O)—, or —S(O)—;'}{'sup': '6', 'Ris 4-chloro-3-trifluoromethylphenyl;'}{'sup': '17', 'sub': '1-6', 'Ris H, substituted or unsubstituted Calkyl or halogen;'}{'sup': '18', 'sub': '1-6', 'Ris H, substituted or unsubstituted Calkyl or halogen;'}{'sup': '7', 'sub': 1-6', '1-6', '3-8, 'Ris H, halogen, CN, —OCalkyl, substituted or unsubstituted Calkyl or substituted or unsubstituted Ccycloalkyl; and,'}{'sup': '8', 'sub': '1-6', 'Ris H, substituted or unsubstituted Calkyl, CN or halogen.'}6. A compound according to claim 5 , wherein:{'sup': '1', 'Ris H;'}{'sup': '2', 'sub': '1-6', 'Ris substituted or unsubstituted Calkyl;'}{'sup': '5', 'sub': '2', 'Ris —S—, —S(O)—, or —S(O)—;'}{'sup': '6', 'Ris 4-chloro-3-trifluoromethylphenyl;'}{'sup': '17', 'Ris H;'}{'sup': '18', 'Ris H;'}{'sup': '7', 'sub': '1-6', 'Ris halogen or Calkyl; and,'}{'sup': '8', 'Ris H.'}7. A compound according to claim 6 , wherein:{'sup': '1', 'Ris H;'}{'sup': '2', 'Ris benzyl, methyl-4-benzoic acid, tert-butyl 2-(4-methylbenzamido)acetate, tert-butyl 2-(4-methyl benzamido)acetic acid, methyl-3-methylbenzoate, 4-methyl-N-(2-(pyrrolidin-1-yl)ethyl)benzamide, 4-methyl-N-(2-(1-oxipyrrolidin-1-yl)ethyl)benzamide, 3-methyl-N-(2-(pyrrolidin-1-yl)ethyl)benzamide, methyl-2-methylbenzoate, methyl-2-benzoic acid, N,N- ...

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17-10-2013 дата публикации

Compound for organic light-emitting diode and organic light-emitting diode including the same

Номер: US20130270524A1
Принадлежит: Samsung Display Co Ltd

A compound represented by Formula 1 below may be used in an organic light emitting diode.

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17-10-2013 дата публикации

FLUORENE COMPOUND AND PHARMACEUTICAL USE THEREOF

Номер: US20130274240A1
Принадлежит:

The present invention provides an agent for the prophylactic or treatment of diabetes, diabetic complications, insulin resistance syndrome, metabolic syndrome, hyperglycemia, dyslipidemia, atherosclerosis, cardiac failure, cardiomyopathy, myocardial ischemia, brain ischemia, cerebral apoplexy, pulmonary hypertension, hyperlactacidemia, mitochondrial disease, mitochondrial encephalomyopathy or cancer, namely, a PDHK inhibitor and the like. A compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, or a solvate thereof: 217.-. (canceled)18. A pharmaceutical composition comprising a compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , or a solvate thereof claim 1 , and a pharmaceutically acceptable carrier.1923.-. (canceled)24. A method of inhibiting PDHK in a mammal claim 1 , comprising administering a pharmaceutically effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , or a solvate thereof to the mammal.25. A method of inhibiting PDHK2 in a mammal claim 1 , comprising administering a pharmaceutically effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , or a solvate thereof to the mammal.26. A method of decreasing the blood glucose level in a mammal claim 1 , comprising administering a pharmaceutically effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , or a solvate thereof to the mammal.27. A method of decreasing lactate level in a mammal claim 1 , comprising administering a pharmaceutically effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , or a solvate thereof to the mammal.28. A method for the treatment or prophylaxis of diabetes claim 1 , diabetic complications claim 1 , insulin resistance syndrome claim 1 , metabolic syndrome claim 1 , hyperglycemia claim 1 , dyslipidemia claim 1 , atherosclerosis claim 1 , ...

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17-10-2013 дата публикации

Platinum(ii) complexes for oled applications

Номер: US20130274473A1
Принадлежит: University of Hong Kong HKU

The current invention relates to novel platinum(II) based organometallic materials. These materials show high emission quantum efficiencies and low self-quenching constant. Also provided are high efficiency, green to orange emitting organic light-emitting diode (OLED) that are fabricated using platinum(II) based organometallic materials as the light-emitting material. The organometallic materials of the invention are soluble in common solvents; therefore, solution process methods such as spin coating and printing can be used for device fabrication. The devices fabricated from these materials show low efficiency roll-off.

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24-10-2013 дата публикации

Novel ruthenium complexes and their uses in processes for formation and/or hydrogenation of esters, amides and derivatives thereof

Номер: US20130281664A1
Принадлежит: Yeda Research and Development Co Ltd

The present invention relates to novel Ruthenium catalysts and related borohydride complexes, and the use of such catalysts, inter alia, for (1) hydrogenation of amides (including polyamides) to alcohols and amines; (2) preparing amides from alcohols with amines (including the preparation of polyamides (e.g., polypeptides) by reacting dialcohols and diamines and/or by polymerization of amino alcohols); (3) hydrogenation of esters to alcohols (including hydrogenation of cyclic esters (lactones) or cyclic di-esters (di-lactones) or polyesters); (4) hydrogenation of organic carbonates (including polycarbonates) to alcohols and hydrogenation of carbamates (including polycarbamates) or urea derivatives to alcohols and amines; (5) dehydrogenative coupling of alcohols to esters; (6) hydrogenation of secondary alcohols to ketones; (7) amidation of esters (i.e., synthesis of amides from esters and amines); (8) acylation of alcohols using esters; (9) coupling of alcohols with water to form carboxylic acids; and (10) dehydrogenation of beta-amino alcohols to form pyrazines. The present invention further relates to the novel uses of certain pyridine Ruthenium catalysts.

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24-10-2013 дата публикации

PALLADIUM CATALYST, METHOD FOR ITS PREPARATION AND ITS USE

Номер: US20130281700A1
Принадлежит:

The invention relates to palladium(0)-tris{tri-[3,5-bis(trifluoromethyl)-phenyl]-phosphine} complex of formula (I), as well as to its preparation and use. 2. The composition of in a solid form.3. The composition of having a melting point of 220° C. as determined by DSC in inert atmosphere.4. The composition of claim 1 , having a decomposition point of 169.5° C. as determined by DSC in air under atmospheric pressure.5. A palladium(0) complex comprising three fluorinated phosphine compounds.6. The palladium(0) complex of exhibiting a stability characterized by no measurable decomposition on the basis of P claim 5 , F claim 5 , C and H NMR spectra following 4 months of storage in air at a temperature of 25° C.7. The palladium(0) complex of exhibiting a stability characterized by no measurable decomposition on the basis of P claim 5 , F claim 5 , C and H NMR spectra following 20 months of storage in air at room temperature.8. The palladium(0) complex of having a melting point in inert atmosphere of 220° C.9. The palladium(0) complex of exhibiting stability at any temperature below its melting point.10. The palladium(0) complex of exhibiting insolubility in water at industrially relevant temperatures and stability when stored in water.11. The palladium(0) complex of comprising a yellow solid.12. The palladium(0) complex of that dissolves at around 90° C. in aqueous alcohols.13. The palladium(0) complex of having catalytic activity in cross coupling reactions at a concentration of from 0.1 to 0.3 mole % of the substrate.14. A method for catalysing a C—C claim 5 , C-heteroatom claim 5 , or hydrogenation reaction comprising carrying out the C—C claim 5 , C-heteroatom or hydrogenation reaction in the presence of the palladium(0) complex of .15. The method of claim 14 , wherein the reaction is a C—C cross-coupling reaction.16. The method of claim 14 , wherein the C—C cross-coupling reaction is selected from the group consisting of: Suzuki coupling claim 14 , Heck coupling and ...

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24-10-2013 дата публикации

Compounds for the treatment of metabolic disorders

Номер: US20130281705A1
Автор: Shalini Sharma
Принадлежит: Wellstat Therapeutics Corp

Compounds useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis, are disclosed.

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31-10-2013 дата публикации

1-PHENYL-2-PYRIDINYL ALKYL ALCOHOL COMPOUNDS AS PHOSPHODIESTERASE INHIBITORS

Номер: US20130289010A1
Принадлежит:

1-Phenyl-2-pyridinyl alkyl alcohol compounds are effective as inhibitors of the phosphodiesterase 4 (PDE4) enzyme and may be used to prevent and/or treat certain diseases or conditions. 2. A method according to claim 1 , wherein R1 is —NHSOR4 claim 1 , wherein R4 is methyl claim 1 , R2 is —OR3 claim 1 , wherein R3 is cyclopropylmethyl claim 1 , and n is 0.3. A method according to claim 1 , wherein R1 is —NHSOR4 claim 1 , wherein R4 is methyl claim 1 , R2 is —OR3 claim 1 , wherein R3 is cyclopropylmethyl claim 1 , and n is 1.4. A method according to claim 1 , wherein R1 is —OR3 claim 1 , R2 is —NHSOR4 wherein R4 is methyl claim 1 , and n is 1.5. A method according to claim 1 , wherein R1 is methyl claim 1 , R2 is —NHSOR4 wherein R4 is methyl claim 1 , and n is 1.6. A method according to claim 1 , wherein both R1 and R2 are —NHSOR4 claim 1 , wherein R4 is methyl claim 1 , and n is 0.7. A method according to claim 1 , wherein both R1 and R2 are —NHSOR4 claim 1 , wherein R4 is methyl claim 1 , and n is 1.89-. (canceled)10. A method according to claim 1 , further comprising administering a second pharmaceutical active component selected from the group consisting of a β2 agonist claim 1 , an M3 antagonist claim 1 , and a corticosteroid.11. A method according to claim 10 , wherein said second active component is formoterol or carmoterol.12. A method according to claim 1 , comprising administering a pharmaceutical composition comprising a compound of formula (I) or a salt thereof and one or more pharmaceutically acceptable carriers and/or excipients.13. A method according to claim 1 , comprising administering a pharmaceutical composition comprising:a compound of formula (I) or a salt thereof;a second pharmaceutical active component selected from the group consisting of a β2 agonist, an M3 antagonist, and a corticosteroid; andone or more pharmaceutically acceptable carriers and/or excipients.14. A method according to claim 12 , wherein said administering is carried out with ...

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07-11-2013 дата публикации

Novel compounds and compositions for the inhibition of nampt

Номер: US20130295051A1
Принадлежит: Individual

The present invention relates to compounds and compositions for the inhibition of NAMPT, their synthesis, applications and antidotes. An illustrative compound of the invention is shown below.

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07-11-2013 дата публикации

Diphenyl-amine derivatives: uses, process of synthesis and pharmaceutical compositions

Номер: US20130296346A1
Принадлежит: Faes Farma SA

The invention relates to compounds of formula (I): or a pharmaceutically acceptable salt, prodrug or solvate thereof, a method of synthesis of said compounds, pharmaceutical compositions comprising them and their use as a medicament for treating inflammatory diseases.

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14-11-2013 дата публикации

Pyridine Compounds and the Uses Thereof

Номер: US20130303526A1
Принадлежит: Purdue Pharma LP

The invention relates to substituted pyridine compounds of Formula (I) and the pharmaceutically acceptable salts, prodrugs, and solvates thereof, wherein R 1a , A 1 , A 2 , E, G, Z 1 , and Z 2 are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula I to treat a disorder responsive to the blockade of sodium channels. Compounds of the present invention are especially useful for treating pain.

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14-11-2013 дата публикации

NOVEL INHIBITORS OF MATRIX METALLOPROTEINASES

Номер: US20130303572A1
Принадлежит:

Compounds of general formula (I), salts or solvates thereof and pharmaceutical compositions containing same: 2. (canceled)3. A compound or salts or solvates thereof according to claim 1 , wherein{'sub': 3', '1-4, 'X is CFor COOR3, wherein R3 is H or optionally substituted Calkyl, preferably methyl or ethyl.'}4. A compound or salts or solvates thereof according to claim 1 , wherein R1 is selected from the group of CH-aryl claim 1 , CH-heteroaryl claim 1 , CH-biphenyl or CH—CH-biphenyl claim 1 , diphenyl-methyl claim 1 , 2 claim 1 ,2′-diphenyl-ethyl claim 1 , 3 claim 1 ,3′-diphenyl-propyl claim 1 , C(O)—R5 claim 1 , where R5 is aryl and S(O)—R6 claim 1 , where R6 is aryl claim 1 , where each of the said groups is optionally substituted with halogen in the aromatic part.5. A compound or salts or solvates thereof according to claim 1 , wherein R2 is selected from the group of O—CH-aryl claim 1 , O—CH-heteroaryl claim 1 , O—(Calkyl) which is optionally substituted with 1 or 2 aryl group(s) claim 1 , where each of the said groups is optionally substituted with halogen in the aromatic part.6. A compound or salts or solvates thereof according to claim 1 , wherein Y is O.7. A compound or salts or solvates thereof according to claim 1 , whereinHET is 5-membered heteroaromatic group comprising 1 to 2 heteroatoms independently selected from the group consisting of N, O and S;{'sub': 3', '1-3, 'X is CFor COOR1, wherein R1 is H or Calkyl;'}{'sub': 2', '2', '2, 'R1 is CH-aryl, CH-heteroaryl, CH-biphenyl or 2,2′-diphenyl-ethyl, where each of the said groups is optionally substituted with halogen in the aromatic part;'}{'sub': 2', '2, 'R2 is O—CH-aryl, O—CH-heteroaryl, diphenylmethoxy, where each of the said groups is optionally substituted with halogen in the aromatic part.'}10. The method according to where the disease is selected from the group of diseases where pathological activation of different MMP isoenzymes are involved in the pathomechanism including (i) cardiovascular ...

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14-11-2013 дата публикации

Method for producing urethanes

Номер: US20130303740A1
Принадлежит: Bayer Intellectual Property GmbH

The invention relates to a method for producing urethanes or ureas or mixtures of urethanes and ureas by oxidative carbonylation of organic amines in the presence of carbon monoxide, oxygen and a catalyst, where the catalyst used is a transition metal complex containing the structural feature: [Mn+(O˜N˜O)2−](n-2)+(L)m(Z−)n-2 and the method is carried out under halogen-free reaction conditions. The invention further relates to transition metal complexes containing said structural feature and also to the use of such transition metal complexes as catalysts in the production of urethanes or ureas or mixtures of urethanes and ureas.

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14-11-2013 дата публикации

Method For Producing Beta-Fluoroalcohol

Номер: US20130303774A1
Принадлежит: Central Glass Co Ltd

A production method of a β-fluoroalcohol includes performing a reaction of an α-fluoroester with hydrogen gas (H 2 ) in the presence of a specific ruthenium complex (i.e. a ruthenium complex of the general formula [2], preferably a ruthenium complex of the general formula [4]). This production method can employ a suitable hydrogen pressure of 1 MPa or less by the use of such a specific ruthenium complex and does not require a high-pressure gas production facility when put in industrial practice. In addition, this production method can remarkably reduce the amount of catalyst used therein (to e.g. a substrate/catalyst ratio of 20,000) in comparison to the substrate/catalyst ratio conventional reduction of α-fluoroalcohol. It is possible by these reduction in hydrogen pressure and catalyst amount to largely reduce the production cost of the β-fluoroalcohol.

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14-11-2013 дата публикации

PROCESS FOR PRODUCTION OF AROMATIC ALCOHOL OR HETEROCYCLIC AROMATIC ALCOHOL

Номер: US20130303775A1
Принадлежит: MITSUBISHI GAS CHEMICAL COMPANY, INC.

A process of production of an aromatic alcohol or a heterocyclic aromatic alcohol, containing a step of reacting an aromatic amine or a heterocyclic aromatic amine having an aromatic ring or a heterocyclic aromatic ring having thereon at least one substituent —CHRNRR(wherein R, Rand Reach independently represent hydrogen, an alkyl group having from 1 to 4 carbon atoms, or a benzyl group), with an alcohol, in the presence of a basic catalyst. 1. A process for producing an aromatic alcohol or a heterocyclic aromatic alcohol , the process comprising reacting an aromatic amine or a heterocyclic aromatic amine , comprising at least one substituent —CHRNRR , with an alcohol , in the presence of a basic catalyst ,{'sup': 1', '2', '3, 'wherein R, Rand Reach independently represent hydrogen, an alkyl group having from 1 to 4 carbon atoms, or a benzyl group.'}4. The process of claim 1 , wherein the basic catalyst is at least one selected from the group consisting of metallic sodium claim 1 , metallic potassium claim 1 , a sodium compound and a potassium compound.5. The process of claim 1 , wherein the alcohol is an alcohol having a linear or branched alkyl group having from 1 to 11 carbon atoms claim 1 , a cycloalkyl group having from 3 to 8 carbon atoms claim 1 , or an alkyl group having from 1 to 3 carbon atoms having a phenyl group substituted thereon claim 1 , having a hydroxyl group bonded thereto.6. The process of claim 1 , wherein water is added to the reaction.7. The process of claim 1 , wherein ammonia is added to the reaction.8. The process of claim 2 , wherein the basic catalyst is at least one selected from the group consisting of metallic sodium claim 2 , metallic potassium claim 2 , a sodium compound and a potassium compound.9. The process of claim 2 , wherein the alcohol is an alcohol having a linear or branched alkyl group having from 1 to 11 carbon atoms claim 2 , a cycloalkyl group having from 3 to 8 carbon atoms claim 2 , or an alkyl group having from 1 to ...

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21-11-2013 дата публикации

Processes and Intermediates for Preparing Fused Heterocyclic Kinase Inhibitors

Номер: US20130310564A1
Принадлежит: METHYLGENE INC.

This invention relates to intermediates for manufacturing fused heterocyclic-type kinase inhibitor compounds, such as thienopyridine-based compounds, particularly at an industrial level. 1. Field of the InventionThis invention relates to processes and intermediates for manufacturing fused heterocyclic-type compounds, such as thienopyridine-based kinase inhibitor compounds, and to processes and intermediates for preparing intermediates that are useful in the manufacture of fused heterocyclic-type compounds, such as thienopyridine-based kinase inhibitor compounds, particularly at an industrial level. Fused heterocyclic-type compounds have been found to be useful to inhibit protein tyrosine kinase activity. In particular, fused heterocyclic-type compounds, such as thienopyridine-based compounds, have been found useful to inhibit the protein tyrosine kinase activity of growth factor receptors, resulting in the inhibition of receptor signaling, for example, the inhibition of VEGF receptor signaling and HGF receptor signaling. Fused heterocyclic-type compounds have been found to be useful in the treatment of cancer by inhibiting protein tyrosine kinase activity. The pharmaceutical compositions that comprise these compounds are also useful in the treatment of diseases, other than cancer, which are associated with signal transduction pathways operating through growth factor and anti-angiogenesis receptors such as c-Met.2. Summary of the Related ArtTyrosine kinases may be classified as growth factor receptor (e.g. EGFR, PDGFR, FGFR and erbB2) or non-receptor (e.g. c-src and bcr-abl) kinases. The receptor type tyrosine kinases make up about 20 different subfamilies. The non-receptor type tyrosine kinases make up numerous subfamilies. These tyrosine kinases have diverse biological activity. Receptor tyrosine kinases are large enzymes that span the cell membrane and possess an extracellular binding domain for growth factors, a transmembrane domain, and an intracellular portion ...

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05-12-2013 дата публикации

Indanyloxyphenylcyclopropanecarboxylic acids

Номер: US20130324514A1
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

The present invention relates to compounds of general formula I, wherein the groups R 1 , R 2 , R 3 , m and n are defined as in claim 1 , which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2. Furthermore, the invention relates to novel intermediates, useful for the synthesis of compounds of formula I.

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12-12-2013 дата публикации

STABLE HOMOGENEOUSLY MIXED NANOSCALE COATINGS DERIVED FROM UNIQUE MULTI-FUNCTIONAL AND MULTIDENTATE AROMATIC ADSORBATES

Номер: US20130327251A1
Принадлежит: THE UNIVERSITY OF HOUSTON SYSTEM

Novel tridentate-, bidentate-, and monodentate-based aromatic adsorbates including self-assembled monolayers (SAMs), especially, mixed multi-component SAMs, where the adsorbates comprise an aromatic ring including one head group or a plurality of dentate head groups and one tunable tail group or a plurality of tail groups and methods for making the same, and methods for using same, their use in the preparation of homogeneously mixed multi-component self-assembled monolayers (SAMs). The adsorbants and SAMs derived therefrom are ideally suited for biosensing, biosensing diagnostics, biological interfacial mimics, surface protections for nanoparticles, inert coatings for artificial implants, and corrosion-resistant coatings for microelectronics components. 1. A method for preparing homogeneously self-assembled monolayers (SAMs) comprising:adsorbing a mono-dentate absorbate, a bi-dentate absorbate, a tri-dentate absorbate or a mixture or combination thereof onto a surface of a substrate to form a SAM modified surface,where the adsorbates comprise an aromatic ring including one dentate head group or a plurality of dentate head groups and one tunable tail group or a plurality of tunable tail groups, andwhere the SAM exhibit: (1) homogenous lateral chain distributions, (2) no or substantially no phase separation or islanding across SAM modified surfaces, and (3) enhanced stability as compared to a corresponding linear alkyl thiol monodentate adsorbate.2. The method of claim 1 , wherein the surface comprises a metal surface.3. The method of claim 1 , wherein the absorbate or mixture thereof comprise one monodentate adsorbate or a mixture of monodentate absorbates.4. The method of claim 1 , wherein the absorbate or mixture thereof comprise one bidentate adsorbate or a mixture of bidentate absorbates.5. The method of claim 4 , wherein the bidentate adsorbate or the mixture of bidentate absorbates comprise a non-symmetrical spiroalkanedithiol or a mixture of non-symmetrical ...

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12-12-2013 дата публикации

COMPOUND FOR ORGANIC LIGHT-EMITTING DEVICE AND ORGANIC LIGHT-EMITTING DEVICE INCLUDING THE SAME

Номер: US20130328021A1
Принадлежит: Samsung Display Co., Ltd.

Embodiments of the present disclosure are directed to a compound represented by Formula 1, and to organic light-emitting diodes including the compound. 2. The compound of claim 1 , wherein:{'sub': 1', '2', '1', '30', '5', '30', '3', '30', '6', '30, 'Rand Rare each independently a halogen group, a cyano group, a substituted or unsubstituted C-Calkyl group, a substituted or unsubstituted C-Caryl group, a substituted or unsubstituted C-Cheteroaryl group, or a substituted or unsubstituted C-Ccondensed polycyclic group;'}{'sub': 3', '5', '30', '3', '30', '6', '30, 'Ris hydrogen, deuterium, a halogen group, a cyano group, a substituted or unsubstituted C-Caryl group, a substituted or unsubstituted C-Cheteroaryl group, or a substituted or unsubstituted C-Ccondensed polycyclic group;'}{'sub': 6', '10', '2', '11, 'A is a linking group such as a substituted or unsubstituted C-Carylene group, a substituted or unsubstituted C-Cheteroarylene group, or a linking group in which at least two arylene groups and/or heteroarylene groups are linked; and'}{'sub': 1', '2', '5', '30', '3', '30', '6', '30, 'Arand Arare each independently a substituted or unsubstituted C-Caryl group, a substituted or unsubstituted C-Cheteroaryl group, or a substituted or unsubstituted C-Ccondensed polycyclic group.'}7. The compound of claim 1 , wherein Rand Rcombine to form a ring.9. An organic light-emitting diode comprising:a first electrode;a second electrode; and{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'an organic layer between the first electrode and the second electrode, wherein the organic layer comprises the compound according to .'}10. The organic light-emitting diode of claim 9 , wherein the organic layer is a hole injection layer claim 9 , a hole transport layer claim 9 , or a functional layer having both hole injection and hole transport abilities.11. The organic light-emitting diode of claim 9 , wherein the organic layer is a hole transport layer or a hole injection layer.12. The ...

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12-12-2013 дата публикации

Fluorinated voltage sensitive dyes, preparation thereof, and optical methods of use

Номер: US20130330762A1
Принадлежит: University of Connecticut

A fluorinated voltage sensitive dye has the structure wherein p is 0, 1, or 2; X q− is an anionic counterion having a charge, q, that is 1 or 2; n is 1 or 2; R 1 is an optionally substituted C 1 -C 12 , alkyl; R 2 is hydrogen, and R 3 is hydrogen or fluorine; or R 2 and R 3 collectively form a divalent —CH═CH—CH═CH— group; R 4 and each occurrence of R 5 are each independently hydrogen or fluorine; R 6 is hydrogen or fluorine or trifluoromethyl; and each occurrence of R 7 is independently C 1 -C 6 alkyl; provided that the dye comprises at least one fluorine atom. The dye is particularly useful for monitoring the dynamics of action potentials in axons and/or dendrites.

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12-12-2013 дата публикации

PROCESS FOR THE DIRECT AMINATION OF ALCOHOLS USING AMMONIA TO FORM PRIMARY AMINES BY MEANS OF A XANTPHOS CATALYST SYSTEM

Номер: US20130331580A1
Принадлежит: EVONIK DEGUSSA GmbH

The present invention relates to a chemocatalytic liquid-phase process for the direct one-stage amination of alcohols to primary amines by means of ammonia in high yields using a catalyst system containing at least one transition metal compound and a xantphos ligand. 2. The process according to claim 1 ,wherein{'sup': 1', '2', '3', '4, 'sub': 3', '2, 'R=R=R=R=phenyl, and A=—C(CH)—.'}3. The process according to claim 1 ,whereinthe xantphos ligand is carbonylchlorohydrido[9,9-dimethyl-4,5-bis(diphenylphosphino)xantheno]ruthenium(II)].4. The process according to claim 1 ,whereinthe alcohol is an aliphatic, linear ω-hydroxycarboxylic acid having a carbon chain comprising at least 8 carbon atoms.5. The process according to claim 1 ,whereinthe alcohol has a concentration of from 0.1 to 1000 mmol/l, based on the fluid phase.6. The process according to claim 1 ,wherein the contacting comprises contacting with liquid or supercritical ammonia, with a solution of ammonium salts in a solvent, or both.7. The process according to claim 1 ,wherein in the contacting,the ammonia has a molar ratio to hydroxyl groups in the alcohol of at least 5:1.8. The process according to claim 1 ,wherein the contacting is carried out at a pressure of from 1 to 1000 bar.9. The process according to claim 1 ,wherein the contacting is carried out in a temperature range of from 80 to 220° C.10. The process according to claim 1 ,whereina volume ratio of a liquid phase to a gas phase in the contacting is greater than or equal to 0.05.11. The process according to claim 1 ,wherein the process is carried out in an absence of hydrogen.12. The process according to claim 1 , wherein the alcohol has a concentration of from 0.1 to 100 mmol/l based on the fluid phase.13. The process according to claim 1 , wherein the alcohol has a concentration of from 0.1 to 10 mmol/l based on the fluid phase.14. The process according to claim 1 , wherein in the contacting claim 1 , the ammonia has a molar ratio to hydroxyl ...

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09-01-2014 дата публикации

New palladium catalyst, method for its preparation and its use

Номер: US20140012004A1
Принадлежит: H4SEP KFT

The invention relates to palladium(0) tris{tri-[3,5-bis(trifluoromethyl)-phenyl]-phosphine} complex of formula (I), as well as to its preparation and use. This compound is outstandingly stable, and can be used as catalyst with excellent results.

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23-01-2014 дата публикации

PHENOXY ACETIC ACIDS AND PHENYL PROPIONIC ACIDS AS PPAR DELTA AGONISTS

Номер: US20140024645A1
Принадлежит: HIGH POINT PHARMACEUTICALS, LLC

Phenoxy acetic acids and phenyl propionic acids and their use in treating type I diabetes, type II diabetes, impaired glucose tolerance, insulin resistance, or obesity are provided herein. The present compounds are activators of PPARδ and may be useful for treating conditions mediated by the same. 2. The method of claim 1 , wherein Xis morpholin-4-ylmethyl.3. A method of treating type I diabetes claim 1 , type II diabetes claim 1 , impaired glucose tolerance claim 1 , insulin resistance claim 1 , or obesity claim 1 , the method comprising administering to a subject in need thereof an effective amount of a compound selected from the group consisting of:(E)-[4-[3-(4-Fluorophenyl)-3-[4-[3-(morpholin-4-yl)propynyl]phenyl]allyloxy]-2-methyl-phenoxy]acetic acid; andZ)-[4-[3-(4-Fluorophenyl)-3-[4-[3-(morpholin-4-yl)propynyl]phenyl]allyloxy]-2-methyl-phenoxy]acetic acid; ora pharmaceutically acceptable salt thereof.4. The method of claim 3 , wherein the compound is (E)-[4-[3-(4-Fluorophenyl)-3-[4-[3-(morpholin-4-yl)propynyl]phenyl]allyloxy]-2-methyl-phenoxy]acetic acid or a pharmaceutically acceptable salt thereof.5. The method of claim 3 , wherein the compound is (Z)-[4-[3-(4-Fluorophenyl)-3-[4-[3-(morpholin-4-yl)propynyl]phenyl]allyloxy]-2-methyl-phenoxy]acetic acid or a pharmaceutically acceptable salt thereof.7. The method of claim 6 , wherein Xis morpholin-4-ylmethyl.8. The method of claim 6 , wherein the compound is (E)-[4-[3-(4-Chlorophenyl)-3-[4-[3-(morpholin-4-yl)propynyl]phenyl]allyloxy]-2-methylphenyl]-propionic acid or a pharmaceutically acceptable salt thereof.9. The method of claim 6 , wherein the compound is (Z)-[4-[3-(4-Chlorophenyl)-3-[4-[3-(morpholin-4-yl)propynyl]phenyl]allyloxy]-2-methylphenyl]-propionic acid or a pharmaceutically acceptable salt thereof.10. A method of treating type I diabetes claim 6 , type II diabetes claim 6 , impaired glucose tolerance claim 6 , insulin resistance claim 6 , or obesity claim 6 , the method comprising administering to ...

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30-01-2014 дата публикации

TRPM8 RECEPTOR ANTAGONISTS

Номер: US20140031398A1
Принадлежит:

Compounds acting as selective antagonists of Transient Receptor Potential cation channel subfamily M member 8 (hereinafter referred to as TRPM8), having formula: 2. The compounds according to claim 1 , wherein claim 1 , independently one from the other:R is selected from H, Br and CN;{'sub': 1', '3, 'X is selected from F, Cl and C-Calkyl;'}{'sub': 2', '2, 'Y is selected from —O—, CH, NH and SO;'}{'sub': '3', 'R1 and R2, independently one from the other, are selected from H, F and CH;'}{'sub': '3', 'R3 and R4, independently one from the other, are selected from H and CH;'}{'sup': '+', 'sub': '3', 'Z is selected from NR6 and R6R7N, where R6 and R7, independently one from the other, are selected from H and CH; and'}{'sub': '3', 'R5 is selected from H and CH.'}3. The compounds according to claim 1 , wherein claim 1 , independently one from the other claim 1 ,R is selected from H and CN;X is selected from F and Cl;{'sub': 2', '2, 'Y is selected from CH, O and SO;'}{'sup': '+', 'sub': 3', '2, 'Z is selected from NH and N(CH);'}R5 is H; and{'sub': '3', 'Het is substituted with at least one substituent selected from F, Cl and CH.'}4. The compounds according to claim 1 , wherein Het is 5-substituted pyrrol-2-yl claim 1 , 5-substituted N-methylpyrrol-2-yl claim 1 , or 5-substituted thiophen-2-yl or 5-substituted fur-2-yl.5. The compounds according to claim 1 , selected from the group consisting of:2-[(1-chloronaphthalen-2-yl)oxy]-N-(furan-2-ylmethyl)ethanaminium chloride (1);2-[(1-chloronaphthalen-2-yl)oxy]-N-[(5-methylfuran-2-yl)methyl]ethanaminium chloride (2);N-[(5-chlorofuran-2-yl)methyl]-2-[(1-chloronaphthalen-2-yl)oxy]ethanaminium (3);2-[(1-chloronaphthalen-2-yl)oxy]-N-[(5-chlorothiophen-2-yl)methyl]ethanaminium (4);2-[(1-chloronaphthalen-2-yl)oxy]-N-(thiophen-2-ylmethyl)ethanaminium (5);2-[(1-chloronaphthalen-2-yl)oxy]-N-(pyridin-2-ylmethyl)ethanaminium (6);2-[(1-chloronaphthalen-2-yl)oxy]-N-[(1-methyl-1H-pyrrol-2-yl)methyl]ethanaminium (7);1-[(1-chloronaphthalen-2-yl) ...

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06-02-2014 дата публикации

Compounds, compositions and methods for the treatment of amyloid diseases and synucleinopathies such as alzheimer's disease, type 2 diabetes, and parkinson's disease

Номер: US20140038980A1
Принадлежит: ProteoTech Inc

Bis- and tris-dihydroxyaryl compounds and their methylenedioxy analogs and pharmaceutically acceptable esters, their synthesis, pharmaceutical compositions containing them, and their use in the treatment of amyloid diseases, especially Aβ amyloidosis, such as observed in Alzheimer's disease, IAPP amyloidosis, such as observed in type 2 diabetes, and synucleinopathies, such as observed in Parkinson's disease, and the manufacture of medicaments for such treatment.

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06-02-2014 дата публикации

METHOD FOR PRODUCING N-SUBSTITUTED AMINE COMPOUNDS THROUGH CATALYZED ALKYLATION

Номер: US20140039181A1

The invention relates to a method for producing a N-substituted amine compound by catalyzed alkylation. The method uses amine and alcohol or two kinds of amines as the reaction materials, employs composite metal oxides catalyst at a reaction temperature of 80-180° C. to catalyze the reaction for 6-36 hours, so as to produce the N-substituted amine compound. The reaction condition of the method of the invention is relatively moderate, using a catalyst made of cheap non-noble metals, which is non-caustic and easy to be separated and reused. The reaction does not need any medium and has relatively high conversion rate and selectivity. 2. The method of claim 1 , wherein the molar ratio of Cu to Ni is from 10:1 to 1:10 claim 1 , and the molar ratio of Cu to Fe is from 10:1 to 1:10 in CuO—NiO—FeO.3. The method of claim 1 , wherein the molar ratio of Ni to Fe in NiO—FeOis from 10:1 to 1:10.4. The method of claim 1 , wherein the molar ratio of Cu to Fe in CuO—FeOis from 10:1 to 1:10.5. The method of claim 1 , wherein the molar ratio of Cu to Ni in CuO—NiO is from 10:1 to 1:10.6. (canceled)7. The method of claim 1 , wherein the mass ratio between the composite metal oxide catalyst and the amine is from 0.01:1 to 1.2:1.8. The method of claim 1 , wherein the composite metal oxide catalyst is produced by the following steps:{'sub': 3', '2', '3', '2', '3', '3', '3', '3, '1) adding an aqueous solution of any two or three nitrates selected from Cu(NO), Ni(NO), and Fe(NO), and an aqueous Al(NO)solution, to an aqueous alkali metal oxide or hydroxide solution, aqueous ammonia, or aqueous carbamide solution which functions as a precipitator to coprecipitate;'}2) after step 1), providing a crude catalyst by washing, drying in the air, calcining, and reducing in hydrogen gas;{'sub': 3', '4', '3', '4', '3', '4, '3) using an aqueous alkali metal hydroxide solution to remove any alumina in the crude catalyst obtained in steps 1) and 2) to provide a composite metal oxides catalyst CuO—NiO— ...

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13-02-2014 дата публикации

Inhibitors of PI3K-Delta and Methods of Their Use and Manufacture

Номер: US20140045825A1
Автор: Leahy James William
Принадлежит: Exelixis, Inc.

The invention is directed to Compounds of Formula I: and pharmaceutically acceptable salts or solvates thereof, as well as methods of making and using the compounds. 35-. (canceled)6. The compound of claim 1 , wherein Ris H or methyl.7. The compound of claim 6 , wherein Q is absent or is (C-C)alkylene and Z is absent or is NH claim 6 , N(C-C)alkyl claim 6 , —NH—(C═O)— claim 6 , —N(C-C)alkyl-(C═O)— claim 6 , O claim 6 , or S.8. (canceled)9. The compound of Formula I-g of claim 2 , wherein Y is optionally substituted (C-C)alkylene claim 2 , wherein up to two carbon atoms of the (C-C)alkylene are replaced by NH claim 2 , N(C-C)alkyl claim 2 , —NH—(C═O)— claim 2 , —N(C-C)alkyl-(C═O)— claim 2 , or —(C═O)—.10. The compound of claim 9 , wherein Q is CHor CH(CH).11. The compound of claim 10 , wherein Z is absent or is —NH— claim 10 , —NH—(C═O)— claim 10 , or S.12. (canceled)14. The compound of claim 13 , wherein Ris NH claim 13 , purinyl claim 13 , pyrazinyl claim 13 , pyrazolopyrimidinyl claim 13 , benzodioxinyl claim 13 , phenyl claim 13 , morpholinyl claim 13 , oxadiazolyl claim 13 , cyclopropyl claim 13 , or pyridinyl claim 13 , any of which may be optionally substituted.18. The compound of claim 17 , wherein Z is absent or is O claim 17 , S claim 17 , —NH— or —NH(C═O)—.19. A compound of which is:9-{[2-(2-methylphenyl)quinolin-3-yl]methyl}-9H-purin-6-amine;9-{[3-(2-methylphenyl)quinoxalin-2-yl]methyl}-9H-purin-6-amine;9-{[8-methyl-2-(2-methylphenyl)quinolin-3-yl]methyl}-9H-purin-6-amine;8-methyl-2-(2-methylphenyl)-3-[(9H-purin-6-ylthio)methyl]quinoline;9-{[2-(2-chlorophenyl)-8-methylquinolin-3-yl]methyl}-9H-purin-6-amine;9-({2-[2-(ethyloxy)phenyl]-8-methylquinolin-3-yl}methyl)-9H-purin-6-amine;9-({8-methyl-2-[3-(methyloxy)phenyl]quinolin-3-yl}methyl)-9H-purin-6-amine;9-{[8-methyl-2-(3-{[2-(methyloxy)ethyl]oxy}phenyl)quinolin-3-yl]methyl}-9H-purin-6-amine;9-{[8-methyl-2-(3-methylphenyl)quinolin-3-yl]methyl}-9H-purin-6-amine;9-({8-methyl-2-[2-(trifluoromethyl)phenyl] ...

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20-02-2014 дата публикации

HETEROCYCLIC RESORCINOL DERIVATIVES, PREPARATION OF SAME AND COSMETIC USES THEREOF

Номер: US20140050683A1
Принадлежит: PIERRE FABRE DERMO-COSMETIQUE

The invention relates to a compound of general formula (I) 2. The compound in accordance with claim 1 , characterized in that Ris a methyl group.3. The compound in accordance with claim 1 , characterized in that Ris a heteroaromatic single-ring claim 1 , preferably with 5 or 6 members.4. The compound in accordance with claim 1 , characterized in that Ris selected from the group consisting of a pyridine claim 1 , thiophene and thiazole heterocycle.5. The compound in accordance with claim 1 , characterized in that Ris a methyl group and Ris selected from the group consisting of 3-pyridyl claim 1 , 4-pyridyl claim 1 , 2-furyl claim 1 , 3-furyl claim 1 , 2-thiophenyl claim 1 , 3-thiophenyl claim 1 , and 2-thiazolyl.6. The compound in accordance with claim 1 , characterized in that it is selected from one of the following compounds:4-(1-(pyridin-2-yl)ethyl)benzene-1,3-diol;4-(1-(pyridin-3-yl)ethyl)benzene-1,3-diol;4-(1-(pyridin-4-yl)ethyl)benzene-1,3-diol;4-(1-(thiophene-2-yl)ethyl)benzene-1,3-diol;4-(1-(thiophene-3-yl)ethyl)benzene-1,3-diol;4-(1-(thiazol-2-yl)ethyl)benzene-1,3-diol;4-(1-(1-methyl-1H-benzo[d]imidazol-2-yl)ethyl)benzene-1,3-diol;4-(1-(1-methyl-1H-indol-2-yl)ethyl)benzene-1,3-diol;4-(1-(benzo[1)]thiophene-2-yl)ethyl)benzene-1,3-diol;4-(1-(thiophene-2-yl)butyl)benzene-1,3-diol;4-(3-methyl-1-(thiophene-2-yl)butyl)benzene-1,3-diol.7. A compound as defined in accordance with claim 1 , for use as a cosmetic active ingredient.8. A compound as defined in accordance with claim 1 , for use as a drug.9. A compound as defined in accordance with claim 1 , for use as a depigmenting active ingredient.10. A compound as defined in accordance with claim 1 , for use as an antioxidant active ingredient.11. A pharmaceutical or cosmetic composition claim 1 , characterized in that it includes as active ingredient at least one compound of formula (I) such as defined in accordance with in combination with a pharmaceutically or cosmetically acceptable excipient.13. The cosmetic ...

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27-02-2014 дата публикации

Therapeutic polyamine compositions and their synthesis

Номер: US20140057877A1
Принадлежит:

This invention relates to a process of synthesis and composition of open chain (ring), closed ring, linear branched and or substituted polyamines, polyamine derived tyrosine phosphatase inhibitors and PPAR partial agonists/partial antagonists via a series of substitution reactions and optimizing the bioavailability and biological activities of the compounds. Polyamines prevent the toxicity of neurotoxins and diabetogenic toxins including paraquat, methyphenyl pyridine radical, rotenone, diazoxide, streptozotocin and alloxan. These polyamines can be utilized to treat neurological, cardiovascular, endocrine acquired and inherited mitochondrial DNA damage diseases and other disorders in mammalian subjects, and more specifically to the therapy of Parkinson's disease, Alzheimer's disease, Lou Gehrig's disease, Binswanger's disease, Olivopontine Cerebellar Degeneration, Lewy Body disease, Diabetes, Stroke, Atherosclerosis, Myocardial Ischemia, Cardiomyopathy, Nephropathy, Ischemia, Glaucoma, Presbycussis, Cancer, Osteoporosis, Rheumatoid Arthritis, Inflammatory Bowel Disease, Multiple Sclerosis and as Antidotes to Toxin Exposure. 1. A method of treating degenerative diseases due to acquired mitochondrial DNA damage , redox damage to mitochondrial macromolecules and inherited mitochondrial genetic defects said method comprising the steps of:selecting a composition from a group consisting of predominantly linear tetraamines and polyamines linked by 1,3-propylene and/or ethylene groups, predominately branched tetraamines and polyamines linked by 1,3-propylene and/or ethylene groups, cyclic polyamines linked by 1,3-propylene and/or ethylene groups, combinations of linear, branched and cyclic polyamines linked by one or more 1,3-propylene and/or ethylene groups, substituted polyamines, polyamines derivatized to form tyrosine phosphatase inhibitor molecules with linear or branched chains attached, polyamine derivatives of 2,2′-diaminobiphenyl with linear or branched chains ...

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27-02-2014 дата публикации

DERIVATIVES OF 1-PHENYL-2-PYRIDINYL ALKYL ALCOHOLS AS PHOSPHODIESTERASE INHIBITORS

Номер: US20140057882A1
Принадлежит: CHIESI FARMACEUTICI S.p.A.

Derivatives of 1-phenyl-2-pyridinyl alkyl alcohols are useful as inhibitors of the phosphodiesterase 4 (PDE4) enzyme and the treatment of certain conditions such as COPD. 7. A compound according to claim 1 , which is selected from the group consisting of:3,5-dichloro-4-((S)-2-(3-(cyclopropylmethoxy)-4-(difluoromethoxy)phenyl)-2-((S)-1-(3-(cyclopropylmethoxy)-4-(methylsulfonamido)benzoyl)pyrrolidine-2-carbonyloxy)ethyl)pyridine 1-oxide;3,5-dichloro-4-((S)-2-(3-(cyclopropylmethoxy)-4-(difluoromethoxy)phenyl)-2-((S)-1-(4-methoxy-3-(methylsulfonyloxy)benzoyl)pyrrolidine-2-carbonyloxy)ethyl)pyridine 1-oxide;3,5-dichloro-4-((S)-2-(3-(cyclopropylmethoxy)-4-(difluoromethoxy)phenyl)-2-((S)-1-(3,4-dimethoxyphenylsulfonyl)pyrrolidine-2-carbonyloxy)ethyl)pyridine 1-oxide;4-((2S)-2-(3-(4-aminophenylsulfonyl)thiazolidine-2-carbonyloxy)-2-(3-(cyclopropylmethoxy)-4-(difluoromethoxy)phenyl)ethyl)-3,5-dichloropyridine 1-oxide;3,5-dichloro-4-((2S)-2-(3-(cyclopropylmethoxy)-4-(difluoromethoxy)phenyl)-2-(3-(4-(methylsulfonamido)phenylsulfonyl)thiazolidine-2-carbonyloxy)ethyl)pyridine 1-oxide;3,5-dichloro-4-((2S)-2-(3-(cyclopropylmethoxy)-4-(difluoromethoxy)phenyl)-2-(3-(4-(N-(2-morpholinoethyl)methylsulfonamido)phenylsulfonyl)thiazolidine-2-carbonyloxy)ethyl)pyridine 1-oxide;4-((S)-2-((R)-3-(4-aminophenylsulfonyl)thiazolidine-2-carbonyloxy)-2-(3-(cyclopropylmethoxy)-4-(difluoromethoxy)phenyl)ethyl)-3,5-dichloropyridine 1-oxide;4-((S)-2-((S)-3-(4-aminophenylsulfonyl)thiazolidine-2-carbonyloxy)-2-(3-(cyclopropylmethoxy)-4-(difluoromethoxy)phenyl)ethyl)-3,5-dichloropyridine 1-oxide;4-((S)-2-((S)-1-(4-aminophenylsulfonyl)pyrrolidine-2-carbonyloxy)-2-(3-(cyclopropylmethoxy)-4-(difluoromethoxy)phenyl)ethyl)-3,5-dichloropyridine 1-oxide;3,5-dichloro-4-((2S)-2-(3-(cyclopropylmethoxy)-4-(difluoromethoxy)phenyl)-2-(1-((4-(methoxycarbonyl)-5-methylfuran-2-yl)methyl)pyrrolidine-2-carbonyloxy)ethyl)pyridine 1-oxide;3,5-dichloro-4-((S)-2-(3-(cyclopropylmethoxy)-4-(difluoromethoxy)phenyl)-2-((S)-1-(3 ...

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20-03-2014 дата публикации

NOVEL TRPV3 MODULATORS

Номер: US20140080803A1
Принадлежит: AbbVie Inc.

Disclosed herein are modulators of TRPV3 of Formula (I) 2. (canceled)4. (canceled)5. The compound according to claim 1 , or a salt thereof claim 1 , wherein:{'sup': 1', 'gc, 'sub': 1', '4', '1', '4', '2, 'Gis pyridinyl; each of which is optionally substituted with 1 or 2 substituents independently selected from the group consisting of halogen, C-C-alkyl, C-C-haloalkyl, and N(R);'}{'sup': 'gc', 'sub': 1', '4, 'Ris hydrogen or C-C-alkyl;'}{'sup': 2d', 'f, 'sub': 1', '4', '1', '4, 'Gis phenyl or pyridinyl; each of which is optionally substituted with 1, 2, or 3 substituents independently selected from the group consisting of halogen, C-C-alkyl, C-C-haloalkyl, and —OR; and'}{'sup': 'f', 'sub': 1', '4', '1', '4, 'Ris C-C-alkyl or C-C-haloalkyl.'}6. The compound according to claim 1 , or a salt thereof claim 1 , wherein{'sup': '1', 'Gis unsubstituted pyridinyl;'}{'sup': 2d', 'f, 'sub': 1', '4', '1', '4, 'Gis phenyl or pyridinyl; each of which is optionally substituted with 1, 2, or 3 substituents independently selected from the group consisting of halogen, C-C-alkyl, C-C-haloalkyl, and —OR; and'}{'sup': 'f', 'sub': 1', '4', '1', '4, 'Ris C-C-alkyl or C-C-haloalkyl.'}7. The compound according to claim 5 , or a salt thereof claim 5 , wherein:{'sup': '1', 'Gis unsubstituted pyridin-2-yl;'}{'sup': 2d', 'f, 'sub': 1', '3', '1', '3, 'Gis phenyl or pyridinyl; each of which is optionally substituted with 1, 2, or 3 substituents independently selected from the group consisting of halogen, C-C-alkyl, C-C-haloalkyl, and —OR; and'}{'sup': 'f', 'sub': 1', '3', '1', '3, 'Ris C-C-alkyl or C-C-haloalkyl.'}8. The compound according to claim 7 , or a salt thereof claim 7 , wherein:{'sup': 2d', 'f, 'sub': 1', '3', '1', '3, 'Gis phenyl which is optionally substituted with 1, 2, or 3 substituents independently selected from the group consisting of halogen, C-C-alkyl, C-C-haloalkyl, and —OR; and'}{'sup': 'f', 'sub': 1', '3', '1', '4, 'Ris C-C-alkyl or C-C-haloalkyl.'}9. The compound according ...

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27-03-2014 дата публикации

Small molecule inhibitors of xbp1 splicing

Номер: US20140088148A1
Принадлежит: GEORGETOWN UNIVERSITY

Small molecule inhibitors of XBP1 splicing by IRE1 are provided, as well as methods for their use in treating or preventing cancer (e.g., endocrine resistant breast cancer), diabetes, and obesity.

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03-04-2014 дата публикации

DERIVATIVES OF SULINDAC, USE THEREOF AND PREPARATION THEREOF

Номер: US20140094492A1
Принадлежит: Southern Research Institute

Derivatives of sulindac that lack cyclooxygenase inhibitory activity are provided along with pharmaceutical compositions containing them and use for treatment or prevention of cancer. The derivatives of sulindac are also suitable for treating chronic inflammatory conditions. A method for preparing the derivatives is also provided. 16. The method of wherein the derivative is administered orally claim 15 , intravenously or intraperitoneally.17. The method of wherein the mammal is human.19. The method according to claim 18 , wherein the chronic inflammatory disease is inflammatory bowel disease.21. The method according to claim 20 , wherein the neurodegenerative disease is Alzheimer's disease. This invention was supported by Grants CA 131378, CA 128021 and CA 148817 from the National Cancer Institute of the National Institutes of Health and the US Government has certain rights in the invention.The present disclosure relates to certain derivatives of sulindac and especially amino derivatives of sulindac. The present disclosure also relates to pharmaceutical compositions comprising the disclosed derivatives of sulindac, as well as methods of using the disclosed derivatives of sulindac for the treatment and prevention of precancerous conditions and cancer in a mammal. The disclosed derivatives of sulindac are also suitable for treating chronic inflammatory conditions. The present disclosure also relates to methods for producing the disclosed compounds.Even though significant advances have occurred in the treatment of cancer, it still remains a major health concern. Cancer has been reported as the leading cause of death in the United States with one of every four Americans likely to be diagnosed with the disease. By way of example, colorectal cancer is the third most commonly diagnosed cancer in the world that accounts for approximately 600,000 deaths per year. While a colonoscopy allows for the early detection of the disease and the identification of individuals who are ...

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10-04-2014 дата публикации

Guanidine compound

Номер: US20140100210A1
Принадлежит: Astellas Pharma Inc

[Problem] The present invention provides a compound which is useful as an active ingredient of a pharmaceutical composition, in particular, a pharmaceutical composition for preventing and/or treating VAP-1-related diseases. [Means for Solution] The present inventors have conducted intensive studies on a compound having a VAP-1 inhibitory activity, and as a result, they have found that the compound or a salt thereof of the present invention exhibits an excellent VAP-1 inhibitory activity and is useful for preventing and/or treating VAP-1-related diseases, in particular, diabetic nephropathy or diabetic macular edema, thereby completing the present invention. In addition, the present invention relates to a pharmaceutical composition, in particular, a pharmaceutical composition for preventing and/or treating VAP-1-related diseases, which comprises the compound or a salt thereof of the present invention, and an excipient.

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05-01-2017 дата публикации

ADO-RESISTANT CYSTEAMINE ANALOGS AND USES THEREOF

Номер: US20170002004A1
Принадлежит: RAPTOR PHARMACEUTICALS INC.

The present disclosure is directed to methods for treating diseases for which cysteamine is indicated and compounds useful in such methods. 2. The method of claim 1 , wherein Rand Rare independently selected from the group consisting of H claim 1 , methyl claim 1 , and ethyl.3. The method of claim 1 , wherein Rand R claim 1 , taken together with the nitrogen atom to which they are attached claim 1 , form a 5-membered heterocyclic ring.4. The method of claim 1 , wherein Ris methyl claim 1 , optionally wherein Ris methyl.5. (canceled)6. The method of claim 1 , wherein Rand R claim 1 , taken together with the carbon atom to which they are attached claim 1 , form a 3-membered carbocyclic ring.7. The method of claim 1 , wherein Ris methyl claim 1 , optionally wherein Ris methyl.8. (canceled)9. The method of claim 1 , wherein Rand R claim 1 , taken together with the carbon atom to which they are attached claim 1 , form a 3-membered carbocyclic ring.10. The method of claim 1 , wherein G is —CRRNRR claim 1 , and Rand R claim 1 , taken together with the atoms to which they are attached claim 1 , form a 6-membered heterocyclic ring claim 1 , optionally wherein Ris methyl.11. (canceled)12. The method of claim 1 , wherein G is —NRR claim 1 , and Rand R claim 1 , taken together with the atoms to which they are attached claim 1 , form a 4- or 6-membered heterocyclic ring.13. (canceled)14. (canceled)17. (canceled)18. (canceled)20. The method of wherein L is a 3- claim 19 , 4- claim 19 , 5- claim 19 , 6- claim 19 , 7- claim 19 , or 8-membered cycloalkyl ring or a 6-membered aryl ring.21. The method of wherein L is Calkyl.22. (canceled)23. The method of wherein A is a 3- claim 19 , 4- claim 19 , 5- claim 19 , 6- claim 19 , 7- claim 19 , or 8-membered monocyclic heterocycloalkyl ring claim 19 , a 6- claim 19 , 7- claim 19 , or 8-membered bicyclic heterocycloalkyl ring claim 19 , or a 5- or 6-membered heteroaryl ring.25. (canceled)26. (canceled)27. (canceled)28. (canceled)29. The ...

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03-01-2019 дата публикации

SUBSTITUTED AMIDE DERIVATIVES HAVING MULTIMODAL ACTIVITY AGAINST PAIN

Номер: US20190002443A1
Принадлежит:

The present invention relates to substituted amide derivatives having dual pharmacological activity towards both the sigma (σ) receptor, and the μ-opioid receptor, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy, in particular for the treatment of pain. 116-. (canceled)19. The compound according to claim 18 , wherein W is nitrogen.21. The compound according to claim 17 , whereinX is a bond, C═O, —C(O)O— or —O—.22. The compound according to claim 21 , wherein X is a bond or —O—.23. The compound according to claim 17 , wherein{'sub': 1', '1-6', '2-6', '2-6, 'Ris selected from the group consisting of substituted or unsubstituted Calkyl, substituted or unsubstituted Calkenyl, substituted or unsubstituted Calkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl and substituted or unsubstituted monocyclic heterocyclyl.'}24. The compound according to claim 23 , wherein Ris substituted or unsubstituted ethyl claim 23 , substituted or unsubstituted isobutyl claim 23 , substituted or unsubstituted phenyl claim 23 , substituted or unsubstituted pyridine and substituted or unsubstituted thiazole.25. The compound according to claim 17 , wherein{'sub': Z', '1-6', '2-6', '2-6, 'Ris selected from the group consisting of substituted or unsubstituted Calkyl, substituted or unsubstituted Calkenyl, substituted or unsubstituted Calkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl and substituted or unsubstituted heterocyclyl.'}26. The compound according to claim 25 , wherein Ris selected from the group consisting of substituted or unsubstituted methyl claim 25 , substituted or unsubstituted ethyl claim 25 , substituted or unsubstituted isopropyl claim 25 , substituted or unsubstituted isobutyl claim 25 , —CF claim 25 , —CHCF claim 25 , substituted or unsubstituted phenyl claim 25 , substituted or unsubstituted pyridine claim 25 , substituted or ...

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07-01-2021 дата публикации

BLOCK COPOLYMERS OF CYCLIC ESTERS AND PROCESSES FOR PREPARING SAME

Номер: US20210002417A1
Автор: Kol Moshe, ROSEN Tomer
Принадлежит: Ramot at Tel-Aviv University Ltd.

Novel processes of preparing block polyester copolymers while precisely controlling the stereoconfiguration (e.g., tacticity), chemical composition and/or length of each unit (block) are provided. Block polyester copolymers featuring desirable combinations of two or more blocks featuring different stereoconfiguration (e.g., tacticity), chemical composition and/or length, including triblock, tetrablock and higher block copolymers are also provided. A novel family of organometallic magnesium complexes and uses thereof in preparing polyesters and block polyester copolymers are also provided. 1. A process of ring opening polymerization of a cyclic ester , the process comprising contacting a plurality of monomers of said cyclic ester with a catalyst system comprising an organometallic magnesium complex , said organometallic magnesium complex comprising a Mg—X unit and a divergent {ONNN} ligand in coordination with said Mg—X.2. The process of claim 1 , being for preparing a polyester.3. The process of claim 1 , wherein said cyclic ester is a lactide.5. The process of claim 4 , wherein X is other than alkoxy or aryloxy.6. The process of claim 4 , wherein X is selected from halo and amine.7. The process of claim 4 , wherein at least one of Rand Ris a bulky rigid alkyl.8. The process of claim 1 , wherein said polymer is a block copolymer comprising a plurality of units claim 1 , at least two of said units independently comprise a plurality of polymerized monomers of a cyclic ester claim 1 , at least one unit of said at least two units comprises a plurality of polymerized monomers of a first cyclic ester claim 1 , and at least one another unit of said at least two units comprises a plurality of polymerized monomers of a second cyclic ester claim 1 , said second cyclic ester differing from said first cyclic ester by a stereoconfiguration and/or a chemical composition claim 1 , the process comprising:sequentially contacting a plurality of monomers of said first cyclic ester and ...

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12-01-2017 дата публикации

Cyclic Amines

Номер: US20170008898A1
Принадлежит: H. Lundbeck A/S

The present invention is directed to novel cyclic amines which inhibit the P2Xreceptor. 26-. (canceled)7. The compound or pharmaceutically acceptable salt thereof of claim 1 , wherein Rand Rcombine with the nitrogen to which they are attached to form optionally substituted piperazinyl.8. The compound or pharmaceutically acceptable salt thereof of claim 1 , wherein Rand Rcombine with the nitrogen to which they are attached to form optionally substituted piperidinyl.9. The compound or pharmaceutically acceptable salt thereof of claim 1 , wherein Rand Rcombine with the nitrogen to which they are attached to form optionally substituted morpholinyl.10. The compound or pharmaceutically acceptable salt thereof of claim 1 , wherein Rand Rcombine with the nitrogen to which they are attached to form optionally substituted pyrrolidinyl.11. The compound or pharmaceutically acceptable salt thereof of claim 1 , wherein Rand Rcombine with the nitrogen to which they are attached to form optionally substituted pyrrolo.12. The compound or pharmaceutically acceptable salt thereof of claim 1 , wherein Rand Rcombine with the nitrogen to which they are attached to form optionally substituted imidazo.13. The compound or pharmaceutically acceptable salt thereof of claim 1 , wherein Rand Rcombine with the nitrogen to which they are attached to form optionally substituted 6 to 10 membered spiro(heterocyclyl).14. The compound or pharmaceutically acceptable salt thereof of claim 1 , wherein Rand Rcombine with the nitrogen to which they are attached to form optionally substituted homomorpholinyl.15. The compound or pharmaceutically acceptable salt thereof of claim 1 , wherein Rand Rcombine with the nitrogen to which they are attached to form optionally substituted homopiperidinyl.16. The compound or pharmaceutically acceptable salt thereof of claim 1 , wherein Rand Rcombine with the nitrogen to which they are attached to form optionally substituted homopiperazinyl.17. The compound or ...

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11-01-2018 дата публикации

THERAPEUTIC COMPOUNDS AND USES THEREOF

Номер: US20180009735A1
Принадлежит:

Provided herein are compounds of formula I: 23-. (canceled)4. The compound of claim 1 , wherein X is —CH— claim 1 , —CHCH— or —CHCHCH—.79-. (canceled)11. The compound of claim 1 , wherein X is or —N(R)C(R)—.1214-. (canceled)15. The compound of claim 1 , wherein Ris hydrogen claim 1 , halo claim 1 , heteroaryl claim 1 , —OR claim 1 , CN claim 1 , —C(O)—N(R)or —C(O)—OR claim 1 , wherein any heteroaryl of Ris optionally substituted with one or more Rgroups.1618-. (canceled)2022-. (canceled)2425-. (canceled)27. (canceled)2933-. (canceled)36. (canceled)40. (canceled)42. (canceled)43. A method of treating cancer in an animal comprising administering to the animal in need thereof a compound of formula I or a pharmaceutically acceptable salt thereof as described in .44. A method of treating an LSD1-mediated disorder in an animal comprising administering to the animal in need thereof a compound of formula I or a pharmaceutically acceptable salt thereof as described in .4549-. (canceled)50. A method of increasing efficacy of a cancer treatment comprising a cytotoxic agent in an animal comprising administering to the animal an effective amount of a compound of formula I or a pharmaceutically acceptable salt thereof as described in .51. (canceled)52. A method of delaying or preventing development of cancer resistance to a cytotoxic agent in an animal claim 1 , comprising administering to the animal a compound of formula I or a pharmaceutically acceptable salt thereof as described in .53. A method of extending the duration of response to a cancer therapy in an animal claim 1 , comprising administering to the animal undergoing the cancer therapy a compound of formula I or a pharmaceutically acceptable salt thereof claim 1 , as described in claim 1 , wherein the duration of response to the cancer therapy when the compound of formula I is administered is extended over the duration of response to the cancer therapy in the absence of the administration of the compound of formula I or ...

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14-01-2021 дата публикации

ACYCLIC CXCR4 INHIBITORS AND USES THEREOF

Номер: US20210009557A1
Принадлежит:

The present invention relates to compounds and methods useful for modulation, e.g. inhibition, of C-X-C receptor type 4 (CXCR4). The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using the compositions in the treatment of various disorders. 5. The compound according to claim 3 , wherein Lis selected from —CH— or —CH(CH)—.6. The compound according to claim 5 , wherein Lis —CH—.79-. (canceled)21. A pharmaceutical composition comprising a compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , and a pharmaceutically acceptable excipient.22. A method of treating a cancer selected from glioma claim 1 , astrocytoma claim 1 , glioblastoma multiforme (GBM claim 1 , also known as glioblastoma) claim 1 , medulloblastoma claim 1 , craniopharyngioma claim 1 , ependymoma claim 1 , pinealoma claim 1 , hemangioblastoma claim 1 , acoustic neuroma claim 1 , oligodendroglioma claim 1 , schwannoma claim 1 , neurofibrosarcoma claim 1 , meningioma claim 1 , melanoma claim 1 , neuroblastoma claim 1 , or retinoblastoma claim 1 , comprising administering to a patient in need thereof an effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt thereof.23. A method of treating a cancer selected from acoustic neuroma claim 1 , astrocytoma (Grade I—Pilocytic Astrocytoma claim 1 , Grade II—Low-grade Astrocytoma claim 1 , Grade III—Anaplastic Astrocytoma claim 1 , or Grade IV—Glioblastoma (GBM)) claim 1 , chordoma claim 1 , CNS lymphoma claim 1 , craniopharyngioma claim 1 , brain stem glioma claim 1 , ependymoma claim 1 , mixed glioma claim 1 , optic nerve glioma claim 1 , subependymoma claim 1 , medulloblastoma claim 1 , meningioma claim 1 , metastatic brain tumor claim 1 , oligodendroglioma claim 1 , pituitary tumors claim 1 , primitive neuroectodermal (PNET) tumor claim 1 , or schwannoma claim 1 , comprising administering to a patient in need thereof an effective ...

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10-01-2019 дата публикации

Urea derivative and use therefor

Номер: US20190010117A1
Принадлежит: TORAY INDUSTRIES INC

A compound has inhibitory activity on Discoidin Domain Receptor 1. The compound includes a urea derivative represented by the formula below or a pharmaceutically acceptable salt thereof.

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10-01-2019 дата публикации

Novel Compounds

Номер: US20190010135A1

The invention relates to 1-(3-sulfonylphenyl)-3-(cyclopent-2-en-1-yl)urea derivatives, and their use in treating or preventing diseases and conditions mediated by the CXCR2 receptor. In addition, the invention relates to compositions containing the derivatives and processes for their preparation.

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10-01-2019 дата публикации

ANTIFUNGAL COMPOUND PROCESS

Номер: US20190010140A1
Принадлежит:

The present invention relates to a process for preparing compound 1 that is useful as an antifungal agent. In particular, the invention seeks to provide new methodology for preparing compound 1 and substituted derivatives thereof. This application is a divisional of U.S. application Ser. No. 15/126,420 filed Sep. 15, 2016, which is the U.S. National Stage Application, pursuant to 35 U.S.C. § 371, of International Application No. PCT/US2015/021511, filed Mar. 19, 2015, which claims the benefit of U.S. Provisional Patent Application Ser. No. 61/955,650 filed Mar. 19, 2014, the entire disclosures of which are incorporated by reference herein.This invention was created in the performance of a Cooperative Research and Development Agreement with the National Institutes of Health, an Agency of the Department of Health and Human Services. The Government of the United States has certain rights in this invention.The present invention relates to a process for preparing compound 1 that is useful as an antifungal agent. In particular, the invention seeks to provide a new methodology for preparing compound 1 and substituted derivatives thereof.Living organisms have developed tightly regulated processes that specifically import metals, transport them to intracellular storage sites and ultimately transport them to sites of use. One of the most important functions of metals such as zinc and iron in biological systems is to enable the activity of metalloenzymes. Metalloenzymes are enzymes that incorporate metal ions into the enzyme active site and utilize the metal as a part of the catalytic process. More than one-third of all characterized enzymes are metalloenzymes.The function of metalloenzymes is highly dependent on the presence of the metal ion in the active site of the enzyme. It is well recognized that agents which bind to and inactivate the active site metal ion dramatically decrease the activity of the enzyme. Nature employs this same strategy to decrease the activity of ...

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09-01-2020 дата публикации

COMPOUNDS AND METHODS FOR TREATING CANCER

Номер: US20200010418A1
Принадлежит:

The present application relates to compounds comprising an ester, a thioester, or a hydrazide moiety and methods of synthesizing these compounds. The present application also relates to pharmaceutical compositions containing the compounds and methods of treating cell proliferative disorders mediated by the Hh signaling pathway, such as cancer, by administering the compounds and pharmaceutical compositions to subjects in need thereof. 18. A pharmaceutical composition comprising a compound of or a pharmaceutically acceptable salt thereof claim 1 , and a pharmaceutically acceptable carrier.19. A method of modulating the SMO claim 1 , comprising contacting the SMO with a compound of or a pharmaceutically acceptable salt thereof.20. A method of treating a disorder mediated by the Hh signaling pathway claim 1 , comprising administering to a subject in need thereof claim 1 , a therapeutically effective amount of a compound of or a pharmaceutically acceptable salt thereof. This application is a divisional application of U.S. application Ser. No. 15/577,845, now allowed, which is a U.S. National Phase application, filed under 35 U.S.C. § 371, of International Application No. PCT/US2016/035641, filed on Jun. 3, 2016, which claims priority to, and the benefit of U.S. Provisional Application No. 62/171,783, filed on Jun. 5, 2015, the contents of each of which are incorporated herein by reference in their entireties.Aberrant regulation of the Hedgehog (Hh) signaling pathway drives several cancers, including medulloblastoma (MB) and Basal Cell Carcinoma (BCC), and is often caused by mutations to Patched (PTCH) or Smoothened (SMO) (Amakye et al., 19, 1410 (2013)). Loss of function mutations to PTCH in the germline are responsible for Gorlin syndrome (also known as nevoid basal cell carcinoma syndrome, NBCCS), a serious genetic disorder that predisposes an individual to several forms of cancer, including MB and BCC (Gorlin, Genet. Med. 6, 530 (2004)). Fortunately, SMO has proved ...

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09-01-2020 дата публикации

PYRIDYL INHIBITORS OF HEDGEHOG SIGNALLING

Номер: US20200010420A1
Принадлежит:

The invention provides novel inhibitors of hedgehog signaling that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula I: 3. The compound of claim 2 , wherein A is ring Awherein Zis S and Zis CH or N.4. The compound of claim 2 , wherein A is the ring A.5. The compound of claim 2 , wherein Ror R′ is Cl.7. The compound of claim 1 , wherein X is NRC(O).8. The compound of claim 1 , wherein X is NRSO.9. The compound of claim 7 , wherein Ris H or Me.10. The compound of claim 9 , wherein Ris H.11. The compound of claim 1 , wherein Ris Me or F.12. The compound of claim 1 , wherein Ris Me and m is 1 or 2.13. The compound of claim 1 , wherein Ris F and m is 1 or 2.14. The compound of claim 1 , wherein m is 0.1531.-. (canceled)32. A composition comprising a compound of and a pharmaceutically acceptable carrier.33. A method of treating cancer in a mammal claim 1 , comprising administering to said mammal an effective amount of a compound of .34. The method of claim 33 , wherein said cancer is basal cell carcinoma claim 33 , medullablastoma claim 33 , pancreatic adenocarcinoma claim 33 , small-cell lung carcinoma claim 33 , breast carcinoma claim 33 , rhabdomyosarcoma claim 33 , oesophageal cancer claim 33 , stomach cancer claim 33 , biliary tract cancer.35. A method of inhibiting angiogenesis in a mammal claim 1 , comprising administering to said mammal an effective amount of a compound of .36. A method of inhibiting hedgehog pathway signalling in a cell comprising contacting said cell with an effective amount of a compound of . This application claims priority to provisional patent application 60/607,367 filed on 2 Sep. 2004.The present invention relates to organic compounds useful for therapy and/or prophylaxis in a mammal, in particular to pyridyl compounds that inhibit the hedgehog signaling pathway and are useful in the treatment of hyperproliferative diseases and angiogenesis mediated diseases.Hedgehog (Hh) protein was ...

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09-01-2020 дата публикации

COMPLEX CRYSTAL AND CHEMOSENSOR PROVIDED WITH SAME

Номер: US20200010437A1
Принадлежит:

The complex crystal of the present disclosure is a complex crystal having a structure in which supramolecular units each composed of two or more types of molecules are arrayed. Each of the supramolecular units contains a cyanoacrylic acid derivative and a trisubstituted methylamine as the molecules. The complex crystal has, between the supramolecular units, molecular cavities in each of which a guest molecule for which the supramolecular unit is a host is not disposed. The complex crystal of the present disclosure can have a property of incorporating a chemical substance therein and can exhibit a great change in a characteristic when incorporating the chemical substance therein. 1. A complex crystal having a structure in which supramolecular units each composed of two or more types of molecules are arrayed , whereineach of the supramolecular units contains a cyanoacrylic acid derivative and a trisubstituted methylamine as the molecules, andthe complex crystal has, between the supramolecular units, molecular cavities in each of which a guest molecule for which the supramolecular unit is a host is not disposed.2. The complex crystal according to claim 1 , where the complex crystal does not substantially contain the guest molecule.5. The complex crystal according to claim 1 , wherein the complex crystal is obtained by detaching the guest molecules from a precursor complex crystal having a structure in which the supramolecular units and the guest molecules are arrayed claim 1 , by supercritical drying using supercritical carbon dioxide.6. A chemosensor comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'the complex crystal according to ; and'}a detection unit configured to detect a characteristic of the complex crystal, whereinthe chemosensor detects a predetermined chemical substance on the basis of a change in the characteristic detected by the detection unit.7. The chemosensor according to claim 6 , whereinthe detection unit includes a light source ...

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12-01-2017 дата публикации

COMPOUND AND ORGANIC LIGHT-EMITTING DEVICE INCLUDING THE SAME

Номер: US20170012205A1
Принадлежит:

An organic light-emitting device includes a first electrode; a second electrode facing the first electrode; and an organic emission layer between the first electrode and the second electrode. The organic emission layer may include a compound represented by Formula 1: 2. The compound of claim 1 , wherein claim 1 , in Formula 1 claim 1 , Rto Rare each independently selected from a substituted or unsubstituted C-Calkyl group claim 1 , a substituted or unsubstituted C-Caryl group claim 1 , and a substituted or unsubstituted C-Cheteroaryl group.3. The compound of claim 1 , wherein claim 1 , in Formula 1 claim 1 , adjacent substituents of Rto Rare linked to form a ring.4. The compound of claim 1 , wherein claim 1 , in Formula 1 claim 1 , Arand Arare each independently selected from a substituted or unsubstituted C-Caryl group claim 1 , a substituted or unsubstituted C-Cheteroaryl group claim 1 , a substituted or unsubstituted monovalent non-aromatic condensed polycyclic group claim 1 , and a substituted or unsubstituted monovalent non-aromatic condensed heteropolycyclic group.7. The compound of claim 6 , wherein Rand Rare linked to form a ring.13. An organic light-emitting device comprising:a first electrode;a second electrode facing the first electrode; andan organic layer between the first electrode and the second electrode and comprising an emission layer,{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'wherein the organic layer comprises the compound of .'}14. The organic light-emitting device of claim 13 , wherein:the first electrode is an anode,the second electrode is a cathode, andthe organic layer comprises:i) a hole transport region between the first electrode and the emission layer and comprising a hole transport layer and at least one layer selected from a hole injection layer and an electron blocking layer; andii) an electron transport region between the emission layer and the second electrode and comprising at least one layer selected from an electron ...

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21-01-2016 дата публикации

STILBAZOLIUM DERIVATIVE AND NONLINEAR OPTICAL MATERIAL USING THE SAME

Номер: US20160016905A1
Принадлежит:

Provided is a stilbazolium derivative represented by the general formula (I): 3. The stilbazolium derivative according to claim 1 , wherein Y is a sulfonic acid anion.4. The stilbazolium derivative according to claim 2 , wherein Y is a sulfonic acid anion.6. A nonlinear optical material comprising the stilbazolium derivative according to .7. A nonlinear optical material comprising the stilbazolium derivative according to .8. A nonlinear optical material comprising the stilbazolium derivative according to .9. A light source device comprising the nonlinear optical material according to as a light wavelength conversion element.10. A light source device comprising the nonlinear optical material according to as a light wavelength conversion element.11. A light source device comprising the nonlinear optical material according to as a light wavelength conversion element.12. A terahertz generation device comprising the nonlinear optical material according to .13. A terahertz generation device comprising the nonlinear optical material according to .14. A terahertz generation device comprising the nonlinear optical material according to . Any and all applications for which a foreign or domestic priority claim is identified in the Application Data Sheet as filed with the present application are hereby incorporated by reference under 37 CFR 1.57.This application claims priority to and the benefit of Japanese Patent Application No. 2014-129498 filed in the Japanese Intellectual Property Office on Jun. 24, 2014, the entire contents of which are incorporated herein by reference.1. Field of the InventionThe present invention relates to novel stilbazolium derivatives useful as nonlinear optical materials.2. Description of the Related ArtConventionally, inorganic nonlinear optical materials such as LiNbO(LN) have been used as electro-optical (EO) materials for electro-optical (EO) elements. However, as a result of research for organic materials exhibiting great nonlinear optical ...

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15-01-2015 дата публикации

DERIVATIVES OF 1-PHENYL-2-PYRIDINYL ALKYL ALCOHOLS AS PHOSPHODIESTERASE INHIBITORS

Номер: US20150018321A1
Принадлежит: CHIESI FARMACEUTICI S.p.A.

Derivatives of 1-phenyl-2-pyridinyl alkyl alcohols are useful as inhibitors of the phosphodiesterase 4 (PDE4) enzyme. 2. The compound claim 1 , salt claim 1 , or N-oxide of claim 1 , wherein Ris methyl.3. The compound claim 1 , salt claim 1 , or N-oxide of claim 1 , wherein Ris methyl.4. The compound claim 1 , salt claim 1 , or N-oxide of claim 1 , wherein R′ is t-butyl.5. The compound claim 1 , salt claim 1 , or N-oxide of claim 1 , wherein A is an aryl group claim 1 , a (C-C) cycloalkyl group claim 1 , or a heteroaryl.6. The compound claim 1 , salt claim 1 , or N-oxide of claim 1 , wherein in A at least one ring atom is a heteroatom.7. The compound claim 1 , salt claim 1 , or N-oxide of claim 1 , wherein in A at least one ring atom is a heteroatom selected from N claim 1 , S claim 1 , and O.8. The compound claim 1 , salt claim 1 , or N-oxide of claim 1 , wherein Rand Rtogether with the nitrogen atom to which they are linked form a piperidine ring optionally substituted by (C-C) alkyl claim 1 , an oxazine ring optionally substituted by (C-C) alkyl claim 1 , or an imidazole ring optionally substituted by (C-C) alkyl.9. The compound claim 1 , salt claim 1 , or N-oxide of claim 1 , wherein Rand Rtogether with the nitrogen atom to which they are linked form a piperidyl ring.10. The compound claim 1 , salt claim 1 , or N-oxide of claim 1 , wherein A is a phenyl optionally substituted with one or more Rgroups.11. The compound claim 1 , salt claim 1 , or N-oxide of claim 1 , wherein A is a heteroaryl ring optionally substituted with one or more Rgroups.12. The compound claim 11 , salt claim 11 , or N-oxide of claim 11 , wherein A is a heteroaryl ring selected from the group consisting of pyrrole claim 11 , pyrazole claim 11 , furan claim 11 , thiophene claim 11 , imidazole claim 11 , oxazole claim 11 , isoxazole claim 11 , thiazole claim 11 , pyridine claim 11 , pyrimidine claim 11 , pyrazine claim 11 , pyridazine claim 11 , and pyran.13. The compound claim 1 , salt claim ...

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21-01-2021 дата публикации

BICYCLIC COMPOUNDS AS INHIBITORS OF PD1/PD-L1 INTERACTION/ACTIVATION

Номер: US20210015810A1
Принадлежит:

The compounds of Formula I is described herein along with their polymorphs, stereoisomers, tautomers, prodrugs, solvates, and pharmaceutically acceptable salts thereof. The compounds described herein, their polymorphs, stereoisomers, tautomers, prodrugs, solvates, and pharmaceutically acceptable salts thereof are bicyclic compounds that are inhibitors of PD-1/PD-L1 interaction/activation. 7. The compounds of Formula I or its polymorphs claim 1 , stereoisomers claim 1 , tautomers claim 1 , prodrugs claim 1 , solvates claim 1 , and pharmaceutically acceptable salts thereof claim 1 , as claimed in claim 1 , is selected from a group consisting of:(S)-1-((7-((2-methyl-[1,1′-biphenyl]-3-yl)methoxy)-2,3-dihydro-1H-inden-4-yl)methyl) piperidine-2-carboxylic acid (1),N-(2-(((5-methoxy-7-((2-methyl-[1,1′-biphenyl]-3-yl)methoxy)-2,3-dihydro-1H-inden-4-yl)methyl)amino)ethyl)acetamide (2),(S)-1-((7-((3-(1-(3-(3,3-difluoropyrrolidin-1-yl)propyl)-1H-indol-4-yl)-2-methylbenzyl)oxy)-2,3-dihydro-1H-inden-4-yl)methyl)piperidine-2-carboxylic acid (3),(S)-1-((6-methyl-7-((2-methyl-[1,1′-biphenyl]-3-yl)methoxy)-2,3-dihydro-1H-inden-4-yl)methyl)piperidine-2-carboxylic acid (4),(S)-1-((6-chloro-7-((2-methyl-[1,1′-biphenyl]-3-yl)methoxy)-2,3-dihydro-1H-inden-4-yl)methyl)piperidine-2-carboxylic acid (5),Methyl 7-(((2-acetamidoethyl)amino)methyl)-4-((2-methyl-[1,1′-biphenyl]-3-yl)methoxy)-2,3-dihydro-1H-indene-5-carboxylate (6),(S)-1-((7-((3′-(3-(3,3-difluoropyrrolidin-1-yl)propoxy)-2,2′-dimethyl-[1,1′-biphenyl]-3-yl)methoxy)-5-methoxy-2,3-dihydro-1H-inden-4-yl)methyl)piperidine-2-carboxylic acid (7),(S)-1-((5-((3-cyanobenzyl)oxy)-7-((2-methyl-[1,1′-biphenyl]-3-yl)methoxy)-2,3-dihydro-1H-inden-4-yl)methyl)piperidine-2-carboxylic acid (8),(S)-1-((5-((5-fluoropyridin-3-yl)methoxy)-7-((2-methyl-[1,1′-biphenyl]-3-yl)methoxy)-2,3-dihydro-1H-inden-4-yl)methyl)piperidine-2-carboxylic acid (9)N-(2-(((5-((5-fluoropyridin-3-yl)methoxy)-7-((2-methyl-[1,1′-biphenyl]-3-yl)methoxy)-2,3-dihydro-1H-inden-4- ...

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17-04-2014 дата публикации

Nitrogen-Containing Ligands And Their Use In Atomic Layer Deposition Methods

Номер: US20140102365A1
Принадлежит:

Methods for deposition of elemental metal films on surfaces using metal coordination complexes comprising nitrogen-containing ligands are provided. Also provided are nitrogen-containing ligands useful in the methods of the invention and metal coordination complexes comprising these ligands. 1. A metal coordinating ligand having a formula{'sub': 1', '2', 'x', 'y', '7', '8', '1-6', '2-4', '1', '2', '7', '8', '3', '4', '5', '6, 'a) RRN—(CR)—N—(CR)—NRR, wherein each R is independently hydrogen, Calkyl, acyl, aldehyde, keto or Calkenyl and x and y are independently 2-6, provided that when each of R, R, Rand Ris ethyl, at least one of R, R, Rand Ris not H;'}{'sub': 1', '2', '1', '2', '3', '4', '1-6', '2-4', '1', '2', '1', '2', '3', '4, 'b) RRN—Ar—NH—Ar—NRR, wherein each R is independently hydrogen, Calkyl, acyl, aldehyde, keto or Calkenyl, and Arand Arare aromatic hydrocarbon moieties which may be the same or different, provided that at least one of R, R, Rand Ris not methyl;'}{'sub': 1', '2', '3', '4', 'x', 'Ar', '5', '6', 'y', '7', '8', '1-6', '2-4', 'Ar', '1', '2', '3', '4, 'c) RRN—(CRR)—N—(CRR)—NRR, wherein each R is independently hydrogen, Calkyl, acyl, aldehyde, keto or Calkenyl, and Nis a heterocyclic aromatic moiety wherein the heteroatom is N, provided that at least one of R, R, Rand Ris not methyl, or;'}{'sub': Ar1', '1', '2', 'x', '5', '3', '4', 'y', 'Ar2', '1-6', '2-4', 'Ar1', 'Ar2, 'd) N—(CRR)—NR—(CRR)—N, wherein each R is independently hydrogen, Calkyl, acyl, aldehyde, keto or Calkenyl, and Nand Nmay be the same or different and are heterocyclic aromatic moieties wherein the heteroatom is N.'}3. The metal coordinating ligand of claim 2 , wherein R claim 2 , R claim 2 , Rand Rof formula I are each ethyl (Et) and each of R-Ris independently hydrogen claim 2 , Calkyl claim 2 , acyl claim 2 , aldehyde claim 2 , keto or Calkenyl.4. An apparatus comprising:a deposition chamber; and{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'the metal coordinating ligand of ...

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16-01-2020 дата публикации

COMPOUNDS AND METHODS FOR REGULATING INSULIN SECRETION

Номер: US20200017485A1
Принадлежит:

Disclosed herein are methods for inducing insulin secretion in a glucose-dependent manner and compounds for use in these methods. 6. The compound of claim 1 , wherein Ris aryl substituted with one or more substitutents selected from alkyl claim 1 , cyano claim 1 , or morpholinyl.7. The compound of claim 1 , wherein the aryl of Ris a substituted phenyl claim 1 , where one or more substituents are selected from alkyl claim 1 , cyano claim 1 , or morpholinyl.8. The compound of claim 1 , wherein Ris heteroaryl.9. The compound of claim 8 , wherein the heteroaryl is a piperidinyl.1015-. (canceled)1718-. (canceled)19. The compound according to claim 1 , wherein said compound is Compound 1-7 claim 1 , or 9-99.20. A pharmaceutical composition for modulating insulation secretion comprising an effective amount of a compound of .22. (canceled)2429-. (canceled)30. A method of modulating insulin secretion comprising contacting a β-cell with a compound of claim 1 , wherein insulin secretion from said β-cell occurs only when said blood glucose levels exceed normoglycemic conditions.3136-. (canceled)3843-. (canceled)44. The method according to claim 37 , wherein said compound is selected from Compounds 1-99.4564-. (canceled)6768-. (canceled) The present application claims priority to U.S. Provisional Application Ser. No. 62/473,811, filed Mar. 20, 2017, and U.S. Provisional Application Ser. No. 62/632,865 filed Feb. 20, 2018, the contents of which are hereby incorporated by reference in their entirety.This invention was made with government support under Grant No. 1 R03 DA035188-01 awarded by the National Institutes of Health. The government has certain rights in the invention.Diabetes mellitus type 2 (type 2 diabetes) is a metabolic disorder that results in patients having high blood sugar level and insulin resistance. Long-term complications from high blood sugar include heart disease, strokes, diabetic retinopathy which can result in blindness, kidney failure, and poor blood flow ...

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17-04-2014 дата публикации

Dyes and Labeled Molecules

Номер: US20140106349A1
Принадлежит: AlleLogic Biosciences Corp, Biotium Inc

Dimeric and trimeric nucleic acid dyes, and associated systems and methods are provided. Such a dye may form a hairpin-like structure that enables it to stain nucleic acids via a release-on-demand mechanism, for example. Such a dye may have low background fluorescence in the absence of nucleic acids and high fluorescence in the presence of nucleic acids, upon binding therewith, for example. A dye provided herein may be useful in a variety of applications, such as in DNA quantitation in real-time PCR, for example.

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28-01-2016 дата публикации

INHIBITING NEUROTRANSMITTER REUPTAKE

Номер: US20160024044A1
Принадлежит:

This document relates to compounds as well as methods and materials involved in modulating neurotransmitter reuptake. For example, compounds, methods for synthesizing compounds, and methods for inhibiting neurotransmitter reuptake are provided. Specifically gamma-amino alcohol derivatives that inhibit the reuptake of neurotransmitters such as dopamine, serotonin, epinephrine or norepinephrine are provided as therapeutic agents for the treatment of depression or anxiety in a mammalian subject. 17-. (canceled)9. The compound of claim 8 , wherein Ris optionally substituted with one or two substituents.11. The compound of claim 10 , wherein at least two of R claim 10 , R claim 10 , R claim 10 , R claim 10 , and Rare hydrogen.12. The compound of claim 11 , wherein the remaining R claim 11 , R claim 11 , R claim 11 , R claim 11 , and Rare independently selected from ethyl claim 11 , chloro claim 11 , and bromo.13. The compound of claim 10 , wherein R claim 10 , R claim 10 , and Rare hydrogen; and Rand Rare independently selected from ethyl claim 10 , chloro claim 10 , and bromo.15. The compound of claim 14 , wherein each of Rand Ris not hydrogen.17. The compound of claim 16 , wherein Ris selected from hydrogen claim 16 , lower alkyl claim 16 , halo claim 16 , hydroxyl claim 16 , lower alkoxy claim 16 , methylsulfanyl claim 16 , and methsulfonyl; and Ris selected from hydrogen claim 16 , lower alkyl claim 16 , halo claim 16 , dimethylamino claim 16 , methylsulfanyl claim 16 , and 1 claim 16 ,1 claim 16 ,1-trifluoromethanesulfonamide.1826-. (canceled) This application claims the benefit of U.S. Provisional Application Ser. No. 61/783,122, filed Mar. 14, 2013. The disclosure of the prior application is considered part of (and is incorporated by reference in) the disclosure of this application.1. Technical FieldThis document relates to compounds as well as methods and materials involved in modulating neurotransmitter reuptake.2. Background InformationNeuronal signals are ...

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