Настройки

Укажите год
-

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

Подробнее
-

Мониторинг СМИ

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

Подробнее

Форма поиска

Поддерживает ввод нескольких поисковых фраз (по одной на строку). При поиске обеспечивает поддержку морфологии русского и английского языка
Ведите корректный номера.
Ведите корректный номера.
Ведите корректный номера.
Ведите корректный номера.
Укажите год
Укажите год

Применить Всего найдено 17523. Отображено 100.
26-01-2012 дата публикации

Compounds and Methods for Treating Cancer and Diseases of the Central Nervous System

Номер: US20120020915A1

Disclosed are compounds of the general formula (I): compositions comprising an effective amount of said compounds either alone or in combination with other chemotherapeutic agents, and methods useful for treating or preventing cancer and for inhibiting tumour tissue growth. These compounds attenuate the oxidative damage associated with increased heme-oxygenase activity and can reduce cell proliferation in transformed cells. In addition, the described compounds and compositions are useful as neuroprotectants and for treating or preventing neurodegenerative disorders and other diseases of the central nervous system.

Подробнее
16-02-2012 дата публикации

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

Номер: US20120041027A1
Принадлежит: Glaxo Group Ltd

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

Подробнее
01-03-2012 дата публикации

Nitrogen-containing organic compound, chemically amplified positive resist composition, and patterning process

Номер: US20120052441A1
Принадлежит: Shin Etsu Chemical Co Ltd

An aralkylcarbamate of imidazole base is effective as the quencher. In a chemically amplified positive resist composition comprising the carbamate, deprotection reaction of carbamate takes place by reacting with the acid generated upon exposure to high-energy radiation, whereby the composition changes its basicity before and after exposure, resulting in a pattern profile with advantages including high resolution, rectangular shape, and minimized dark-bright difference.

Подробнее
01-03-2012 дата публикации

Compounds, pharmaceutical compositions and methods of use of hydroxamic acid derivatives

Номер: US20120053188A1
Автор: Stephen Gately, Tong Wang

The invention encompasses a compound derived from hydroxamic acid that may be used to slow the expansion of cancer cells and thus is effective in the treatment of cancer. Generally, the disclosed compound includes a benzimidazole group coupled to a hydroxyamide of five or more unsubstituted carbon atoms and any pharmaceutically acceptable salts, solvates and chemically protected forms thereof. Also disclosed are pharmacological compositions including the compound and methods of using the compound to slow the expansion of cancer cells as well as methods of using the compound to treat cancer.

Подробнее
22-03-2012 дата публикации

Novel solid forms of bendamustine hydrochloride

Номер: US20120071532A1
Принадлежит: Cephalon Inc

Novel solid forms of bendamustine hydrochloride are described, as well as methods of their preparation and use.

Подробнее
12-04-2012 дата публикации

Five-membered heterocycles useful as serine protease inhibitors

Номер: US20120088758A1
Принадлежит: Bristol Myers Squibb Co

The present invention provides a method for treating a thrombotic or an inflammatory disorder administering to a patient in need thereof a therapeutically effective amount of at least one compound of Formula (I) or Formula (V): or a stereoisomer or pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L, Z, R 3 , R 4 , R 6 , R 11 , X 1 , X 2 , and X 3 are as defined herein. The compounds of Formula (I) are useful as selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors. This invention also provides compounds within the scope of Formula I and relates to pharmaceutical compositions comprising these compounds.

Подробнее
12-04-2012 дата публикации

Azole derivatives and fused bicyclic azole derivatives as therapeutic agents

Номер: US20120088778A1
Принадлежит: vTvx Holdings I LLC

This invention provides certain compounds, methods of their preparation, pharmaceutical compositions comprising the compounds, and their use in treating human or animal disorders. The compounds of the invention are useful as modulators of the interaction between the receptor for advanced glycated end products (RAGE) and its ligands, such as advanced glycated end products (AGEs), S100/calgranulin/EN-RAGE, β-amyloid and amphoterin, and for the management, treatment, control, or as an adjunct treatment for diseases in humans caused by RAGE. Such diseases or disease states include acute and chronic inflammation, the development of diabetic late complications such as increased vascular permeability, nephropathy, atherosclerosis, and retinopathy, the development of Alzheimer's disease, erectile dysfunction, and tumor invasion and metastasis.

Подробнее
10-05-2012 дата публикации

Material for organic electroluminescence device and organic electroluminescence device using the same

Номер: US20120112629A1
Принадлежит: Idemitsu Kosan Co Ltd

Provided are an organic electroluminescence device, which: shows high luminous efficiency; is free of any pixel defect; and has a long lifetime, and a material for an organic electroluminescence device for realizing the device. The material for an organic electroluminescence device is a compound of a specific structure having a π-conjugated heteroacene skeleton crosslinked with a carbon atom, nitrogen atom, or oxygen atom. The organic electroluminescence device has one or more organic thin film layers including a light emitting layer between a cathode and an anode, and at least one layer of the organic thin film layers contains the material for an organic electroluminescence device.

Подробнее
17-05-2012 дата публикации

Tricyclic n-heteroaryl-carboxamide derivatives containing a benzimidazole unit, method for preparing same and their therapeutic use

Номер: US20120122852A1
Принадлежит: Sanofi Aventis France

The invention concerns tricyclic N-heteroaryl-carboxamide derivatives containing a benzimidazole unit of general formula (I): Wherein A, P, Y, R 1 , R 2 and R 3 are as defined herein. The invention also concerns a method of preparing the compounds and their therapeutic use.

Подробнее
17-05-2012 дата публикации

New salts

Номер: US20120122883A1
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

The present invention relates to new crystalline salt forms of flibanserine which have valuable pharmacological properties, to a process for their manufacture, to pharmaceutical formulations containing them and to their use as medicament.

Подробнее
24-05-2012 дата публикации

Materials for organic electroluminescent devices

Номер: US20120126179A1
Принадлежит: Merck Patent GmBH

The present invention relates to 4,4′-substituted spirobifluorenes which are suitable, owing to excellent properties, as functional materials in organic electroluminescent devices. In addition, the present invention relates to a process for the preparation of 4,4′-substituted spirobifluorenes and to the use of these compounds in organic electroluminescent devices.

Подробнее
14-06-2012 дата публикации

Heterocyclic Radical or Diradical, The Dimers, Oligomers, Polymers, Dispiro Compounds and Polycycles Thereof, the Use Thereof, Organic Semiconductive Material and Electronic or Optoelectronic Component

Номер: US20120146012A1
Принадлежит: NOVALED GMBH

The present invention relates to heterocyclic radicals or diradicals, the dimers, oligomers, polymers, dispiro compounds and polycycles thereof, to the use thereof, to organic semiconductive materials and to electronic and optoelectronic components.

Подробнее
28-06-2012 дата публикации

Compounds and their use as BACE Inhibitors

Номер: US20120165347A1
Принадлежит: AstraZeneca AB

The present invention relates to compounds of formula (I) and their pharmaceutical compositions. In addition, the present invention relates to therapeutic methods for the treatment and/or prevention of Aβ-related pathologies such as Down's syndrome, β-amyloid angiopathy such as but not limited to cerebral amyloid angiopathy or hereditary cerebral hemorrhage, disorders associated with cognitive impairment such as but not limited to MCI (“mild cognitive impairment”), Alzheimer's disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegeneration associated with diseases such as Alzheimer's disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration.

Подробнее
19-07-2012 дата публикации

Compound, a process for its preparation, a pharmaceutical composition, use of a compound, a method for modulating or regulating serine/threonine kinases and a serine/threonine kinases modulating agent

Номер: US20120184535A1
Принадлежит: Selvita Sp zoo

A compound, a process for its preparation, a pharmaceutical composition, use of a compound, a method for modulating or regulating serine/threonine and tyrosine kinases and a serine/threonine and tyrosine kinases modulating agent. Novel small-molecule compounds with kinase inhibitory activity, having superior properties as pharmaceutical agents, production method thereof and uses thereof. In particular, new derivatives of tetrahalogenated benzimidazole with serine/threonine and tyrosine kinases inhibitory properties, preferably selected from the group of PIM, HIPK, DYRK, CLK, CDK, FLT, PKG, Haspin, MER, TAO, MNK, TRK kinases which exhibit superior pharmacological actions, and can be useful for the treatment of disease conditions, especially cancers depending on serine/threonine and tyrosine kinases, such as but not limited to leukemias and solid tumors.

Подробнее
26-07-2012 дата публикации

Diarylthiohydantoin compounds

Номер: US20120190718A1
Принадлежит: UNIVERSITY OF CALIFORNIA

The present invention relates to diarylthiohydantoin compounds and methods for synthesizing them and using them in the treatment of hormone refractory prostate cancer.

Подробнее
06-09-2012 дата публикации

Compositions and methods useful for treating diseases

Номер: US20120225851A1
Принадлежит: Eutropics Pharmaceuticals Inc

The present invention relates to a chemotherapeutic cancer treatment in which compounds of Formula Ia′, Ib′, Ic′, or II′ (referred to as a group as BH3Is) are administered to a mammal for the treatment of B-cell Lymphoma or other hematopoietic cancers, including diseases associated with MCL-1. In another aspect, the invention provides a method for treating particular types of hematopoietic cancers, such as B-cell lymphoma, using a combination of one or more compounds selected from the group consisting of compounds or Formula Ia, Ib, Ic, or II in combination with other therapies, for example, a class of therapeutics known as 26S proteosome inhibitors, such as, for example, Bortezomib. In another aspect the present invention relates to autoimmune treatment with pharmaceutical compositions comprising one or more compounds of Formula Ia′, Ib′, Ic′, or II′. In another aspect, this invention relates to methods for identifying compounds, for example, compounds of the BH3 mimic class, that have unique in vitro properties that predict in vivo efficacy against B-cell lymphoma tumors and other cancers as well as autoimmune disease.

Подробнее
01-11-2012 дата публикации

Methods of Treating a Hyperproliferative Disorder or Inhibiting Cell Growth in a Mammal

Номер: US20120277277A1
Принадлежит: Array Biopharma Inc

Disclosed are methods for inhibiting abnormal cell growth or treating hyperproliferative diseases in mammals, comprising administering to a mammal in heed thereof a pharmaceutical composition comprising 6-(4-bromo-2-fluorophenylamino)-7-fluoro-3-methyl-3H-benzoimidazole-5-carboxylic acid (2-hydroxy-ethoxy)-amide, or a pharmaceutically acceptable salt thereof, in combination with an effective amount of an anti-tumour agent or in combination with radiation therapy.

Подробнее
27-12-2012 дата публикации

Triarylamine Compound, Light-Emitting Element, Light-Emitting Device, Electronic Device, and Lighting Device

Номер: US20120330025A1
Принадлежит: Semiconductor Energy Laboratory Co Ltd

A novel triarylamine compound having a bipolar property is provided. The triarylamine compound can be used for a hole-injection layer, a hole-transport layer, a light-emitting layer, or an electron-transport layer in a light-emitting element. The triarylamine compound can also be used as a host material with a light-emitting material which emits relatively short-wavelength light, in a structure where the host material and the guest material constitute a light-emitting layer. The triarylamine compound of the present invention is a fluorescent compound and therefore can also be used as a light-emitting substance of a light-emitting layer. A light-emitting element having high emission efficiency is provided. A light-emitting device, an electronic device, or a lighting device having low power consumption is provided.

Подробнее
28-02-2013 дата публикации

Compound for electroluminescent device and organic electroluminescent devices using the same

Номер: US20130048956A1
Принадлежит: E Ray Optoelectronics Technology Co Ltd

The present invention provides a compound of formula (I) for an organic electroluminescent device: wherein X 1 , X 2 , X 3 , Y, Ar 1 , Ar 2 , Ar 3 , Ar 4 , Ar 5 , Ar 6 , and Ar 7 are as defined in the description.

Подробнее
28-02-2013 дата публикации

Cyclopentanecarboxamide derivatives, medicaments containing such compounds and their use

Номер: US20130053412A1
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

The invention relates to cyclopentanecarboxamide derivatives of formula 1, to their use as Fatty Acid Synthase inhibitors, to methods for their therapeutic use and to pharmaceutical compositions containing them, wherein R 1 , R 2 , R 3 , LO, W, AR 1 , n are as defined in claim 1 .

Подробнее
28-03-2013 дата публикации

HETEROCYCLIC COMPOUND AND p27Kip1 DEGRADATION INHIBITOR

Номер: US20130079306A1
Принадлежит: Individual

A novel heterocyclic compound or a salt thereof useful for selectively inhibiting the degradation of p27 Kip1 is provided. The compound or the salt thereof is represented by the following formula (1): wherein A represents an alkyl group, a cycloalkyl group, an aryl group or a heterocyclic group, the group A may have a substituent; the ring B represents a 5- to 8-membered monocyclic heterocyclic ring or a condensed ring containing the monocyclic heterocyclic ring, the ring B may have a substituent; the ring C represents an aromatic ring, the ring C may have a substituent; L represents a linker comprising a main chain having 3 to 5 atoms selected from the group consisting of a carbon atom, a nitrogen atom, an oxygen atom and a sulfur atom, wherein at least one atom in the main chain is a hetero atom selected from the group consisting of a nitrogen atom, an oxygen atom and a sulfur atom, the linker L may have a substituent; and n is 0 or 1.

Подробнее
28-03-2013 дата публикации

TRPV1 VANILLOID RECEPTOR ANTAGONISTS WITH A BICYCLIC PORTION

Номер: US20130079339A1
Принадлежит: PHARMESTE S.R.L.

The invention discloses compounds of formula I 3. Compounds according to wherein R1 and R2 are independently pyrrolidin-1-yl claim 2 , piperidin-1-yl claim 2 , morpholin-4-yl claim 2 , or 2-(dimethylamino)ethoxy.4. A compound according to selected from the group consisting of:1-(4-(trifluoromethyl)benzyl)-3-(2,3-dihydro-2-oxo-1H-benzo[d]imidazol-4-yl)urea,1-(2-fluoro-4-(trifluoromethyl)benzyl)-3-(2,3-dihydro-2-oxo-1H-benzo[d]imidazol-4-yl)urea,1-(2-chloro-4-(trifluoromethyl)benzyl)-3-(2,3-dihydro-2-oxo-1H-benzo[d]imidazol-4-yl)urea,1-(2-(dimethylamino)-4-(trifluoromethyl)benzyl)-3-(2,3-dihydro-2-oxo-1H-benzo[d]imidazol-4-yl)urea,1-(4-(trifluoromethyl)-2-(pyrrolidin-1-yl)benzyl)-3-(2,3-dihydro-2-oxo-1H-benzo[d]imidazol-4-yl)urea,1-(4-(trifluoromethyl)-2-(piperidin-1-yl)benzyl)-3-(2,3-dihydro-2-oxo-1H-benzo[d]imidazol-4-yl)urea,1-(4-(trifluoromethyl)-2-morpholinobenzyl)-3-(2,3-dihydro-2-oxo-1H-benzo[d]imidazol-4-yl)urea,1-(4-(trifluoromethyl)-2-(1H-1,2,4-triazol-1-yl)benzyl)-3-(2,3-dihydro-2-oxo-1H-benzo[d]imidazol-4-yl)urea,1-(4-fluorobenzyl)-3-(2,3-dihydro-2-oxo-1H-benzo[d]imidazol-4-yl)urea,1-(4-chlorobenzyl)-3-(2,3-dihydro-2-oxo-1H-benzo[d]imidazol-4-yl)urea,1-(4-chloro-2-(dimethylamino)benzyl)-3-(2,3-dihydro-2-oxo-1H-benzo[d]imidazol-4-yl)urea,1-(4-chloro-2-(pyrrolidin-1-yl)benzyl)-3-(2,3-dihydro-2-oxo-1H-benzo[d]imidazol-4-yl)urea,1-(4-chloro-2-(piperidin-1-yl)benzyl)-3-(2,3-dihydro-2-oxo-1H-benzo[d]imidazol-4-yl)urea,1-(4-(dimethylamino)benzyl)-3-(2,3-dihydro-2-oxo-1H-benzo[d]imidazol-4-yl)urea,1-(4-(pyrrolidin-1-yl)benzyl)-3-(2,3-dihydro-2-oxo-1H-benzo[d]imidazol-4-yl)urea,1-(4-(piperidin-1-yl)benzyl)-3-(2,3-dihydro-2-oxo-1H-benzo[d]imidazol-4-yl)urea,1-(4-methylbenzyl)-3-(2,3-dihydro-2-oxo-1H-benzo[d]imidazol-4-yl)urea,1-(2-(dimethylamino)-4-methylbenzyl)-3-(2,3-dihydro-2-oxo-1H-benzo[d]imidazol-4-yl)urea,1-(4-methyl-2-(piperidin-1-yl)benzyl)-3-(2,3-dihydro-2-oxo-1H-benzo[d]imidazol-4-yl)urea,1-(2,3-dihydro-2-oxo-1H-benzo[d]imidazol-4-yl)-3-((pyridin-4-yl) ...

Подробнее
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 ...

Подробнее
04-04-2013 дата публикации

CARBOXYLATION CATALYSTS

Номер: US20130085276A1
Принадлежит:

The use of a complex of the form Z—M—OR in the carboxylation of a substrate is described. The group Z is a two-electron donor ligand, M is a metal and OR is selected from the group consisting of OH, alkoxy and aryloxy. The substrate may be carboxylated at a C—H or N—H bond. The metal M may be copper, silver or gold. The two-electron donor ligand may be a phosphine, a carbene or a phosphite ligand. Also described are methods of manufacture of the complexes and methods for preparing isotopically labelled caboxylic acids and carboxylic acid derivatives. 134-. (canceled)25. A method of carboxylation of a substrate , the method comprising;{'sub': '2', 'contacting a complex of the form Z—M—OR ,wherein the group Z is a two-electron donor ligand, M is a metal, and OR is selected from the group consisting of OH, alkoxy and aryloxy; with a substrate and a source of CO.'}26. The method according to claim 25 , wherein the metal M is selected from the group consisting of copper claim 25 , silver and gold.27. The method according to claim 25 , wherein the carboxylation is carried out in the presence of a base.28. The method according to claim 27 , wherein the base is an alkali metal hydroxide or alkoxide.29. The method according to claim 25 , wherein the two-electron donor ligand Z is selected from the group consisting of phosphines claim 25 , carbenes claim 25 , or phosphites.30. The method according to claim 29 , wherein the two-electron donor ligand Z is a nitrogen containing heterocyclic carbene ligand.33. The method according to claim 26 , wherein the complex is selected from the group consisting of: [M(OH)(IMes)] claim 26 , [M(OH)(SIMes)] claim 26 , [M(OH)(IPr)] claim 26 , [M(OH)(ItBu)] claim 26 , and [M(OH)(SIPr)] claim 26 , where M is Au claim 26 , Ag or Cu.34. The method according to claim 25 , wherein the substrate is carboxylated at a C—H or N—H bond.35. The method according to claim 25 , wherein the substrate is a substituted or unsubstituted aromatic compound.36. The ...

Подробнее
11-04-2013 дата публикации

BIPHENYL SUBSTITUTED 1,3-DIHYDRO-BENZOIMIDAZOL-2-YLIDENEAMINE DERIVATIVES

Номер: US20130090342A1
Принадлежит: NOVARTIS AG

The invention relates to new derivatives of formula (I), 7. The compound according to claim 1 , or a salt thereof claim 1 , wherein{'sup': '5', 'sub': 1-5', '1-5', '1-5', '1-4, 'Rrepresents, together with the phenyl ring, an unsubstituted or substituted indolyl, benzimidazolyl, benztriazolyl, the substituents being selected from the group consisting of hydroxy, halo, cyano, carboxy, amino-carbonyl, amino, Calkylamino, di (Calkyl)amino, Calkyl, Calkoxy, phenyl.'}8. The compound according to claim 1 , or a salt thereof claim 1 , wherein{'sup': '5', 'Rrepresents methyl, methoxy, acetylamino, chloro, cyano, or trifluoromethyl.'}9. The compound according to claim 1 , or a salt thereof claim 1 , wherein{'sup': '5', 'q represents 2 and the substituents Rbeing located in the 2- and 5-position or'}{'sup': '5', 'q represents 1 and the substituent Rbeing located in the 2- or 3-position.'}10. The compound according to claim 1 , or a salt thereof claim 1 , whereinR′ represents halogen orR′ represents, together with the phenyl ring, an unsubstituted or substituted indolyl, isoindolyl, indazolyl, benzimidazolyl, benztriazolyl, chinolinyl, isochinnolinyl, cinnolinyl, phtalazinyl, chinazolinyl, chinoxalinyl, naphtalenyl, tetrahydro-naphtalenyl, indenyl, or dihydro-indenyl, the substituents being selected from the group consisting of halogen.11. The compound according to claim 1 , or a salt thereof claim 1 , wherein{'sup': '3', 'sub': 1-4', '1-4', '3-6, 'Rrepresents hydrogen, Calkyl which is optionally substituted by halo or Calkyloxy-carbonyl, Ccycloalkyl which is optionally substituted by halo.'}12. A pharmaceutical composition comprising a therapeutically effective amount of a compound of formula (I) according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , and one or more pharmaceutically acceptable carriers13. The composition of further comprising one or more therapeutically active agents claim 12 , selected from antiproliferative agents.1418-. (canceled)19. ...

Подробнее
18-04-2013 дата публикации

Materials for electronic devices

Номер: US20130092922A1
Принадлежит: Merck Patent GmBH

The present invention relates to an electronic device comprising anode, cathode and at least one organic layer which comprises a compound of the formula (I) to (IV). The invention furthermore encompasses the use of compounds of the formula (I) to (IV) in an electronic device and to a compound of the formula (Ic) to (IVc).

Подробнее
18-04-2013 дата публикации

NOVEL YELLOW PIGMENT COMPOSITION, AND METHOD FOR PRODUCING YELLOW PIGMENT MICROPARTICLES

Номер: US20130095322A1
Принадлежит: M. TECHNIQUE CO., LTD.

Disclosed are: a yellow pigment composition which contains at least one kind of yellow pigment microparticle having excellent transmission characteristics; and a method for producing the yellow pigment microparticle. Specifically disclosed are: a yellow pigment composition which contains at least one kind of yellow pigment microparticle that are characterized in that the difference between the maximum transmittance (Tmax) and the minimum transmittance (Tmin), namely (Tmax−Tmin) is 80% or more in the transmission spectrum at 350-800 nm; and a method for producing the yellow pigment microparticle. 1. A yellow pigment composition containing at least one kind of yellow pigment microparticle , wherein difference (Tmax−Tmin) between the maximum transmittance (Tmax) and the minimum transmittance (Tmin) of a transmission spectrum thereof in a region of 350 nm to 800 nm is 80% or more.2. The yellow pigment composition according to claim 1 , wherein the yellow pigment microparticle is an organic pigment.3. The yellow pigment composition according to claim 1 , wherein the yellow pigment microparticle is an azo pigment or an isoindoline pigment.4. The yellow pigment composition according to claim 1 , wherein the yellow pigment microparticle is formed by a process comprising:a fluid to be processed is supplied between processing surfaces being capable of approaching to and separating from each other and displacing relative to each other,pressure of force to move in the direction of approaching, including supply pressure of the fluid to be processed and pressure applied between the rotating processing surfaces, is balanced with pressure of force to move in the direction of separation thereby keeping a minute space in a distance between the processing surfaces,the minute space kept between two processing surfaces is used as a flow path of the fluid to be processed, thereby forming a thin film fluid of the fluid to be processed, andthe microparticle is formed in this thin film ...

Подробнее
25-04-2013 дата публикации

BIARYL OXYACETIC ACID COMPOUNDS

Номер: US20130102609A1
Принадлежит: LIGAND PHARMACEUTICALS INC.

The present invention provides biaryl oxyacetic acid compounds which may be useful for treating inflammatory disorders, including disorders affecting the respiratory system and skin. The compounds provided include those of the general formula I: 2. A compound or salt according to wherein R claim 1 , R claim 1 , Rand Rare each independently selected from hydrogen and methyl.3. (canceled)4. A compound or salt according to claim 1 , wherein Ris selected from hydrogen claim 1 , methyl claim 1 , ethyl claim 1 , propyl and isopropyl.5. (canceled)6. A compound or salt according to claim 1 , wherein Ris selected from aryl and heteroaryl claim 1 , each optionally substituted with one to four substituents independently selected from halogen claim 1 , cyano claim 1 , (C-C) haloalkyl claim 1 , (C-C) alkoxy claim 1 , (C-C) haloalkoxy claim 1 , (C-C) alkyl claim 1 , and (C-C) alkylsulfonyl.9. A compound or salt according to claim 8 , wherein Ris selected from hydrogen claim 8 , methyl claim 8 , fluoro claim 8 , chloro claim 8 , cyano claim 8 , —CFand methoxy; and Ris selected from hydrogen claim 8 , fluoro claim 8 , chloro claim 8 , methyl claim 8 , methoxy claim 8 , cyano claim 8 , —CFand —SOCH.10. A compound or salt according to wherein Rand Rare each independently selected from fluoro claim 9 , chloro claim 9 , methoxy and hydrogen.11. (canceled)13. A compound or salt according to wherein Ris selected from naphthyl claim 6 , pyridinyl and quinolinyl claim 6 , each optionally substituted with one to four substituents independently selected from halogen claim 6 , cyano claim 6 , (C-C) haloalkyl claim 6 , (C-C) alkoxy claim 6 , (C-C) haloalkoxy claim 6 , (C-C) alkyl and alkylsulfonyl.14. A compound or salt according to claim 1 , wherein Rand Rare each hydrogen.15. A compound or salt according to claim 1 , wherein A is selected from phenyl claim 1 , pyridinyl claim 1 , benzimidazolyl claim 1 , quinolinyl claim 1 , indolyl claim 1 , pyrimidinyl and imidazopyridinyl.16. A compound ...

Подробнее
02-05-2013 дата публикации

ACTIVATORS OF HUMAN PYRUVATE KINASE

Номер: US20130109672A1

Disclosed are pyruvate kinase M2 activators which are compounds of Formula (I), including those of Formula (II), wherein A, A, L, R, Rto R, Xto X, k, n, and m are as defined herein, that are useful in treating a number of diseases that are treatable by the activation of PKM2, for example, cancer. A-NR-L-A(I). 2. (canceled)3. The compound or salt of claim 1 , wherein the phenyl ring of the bicyclic ring of R′ is fused with an aryl claim 1 , a heteroaryl claim 1 , a cyclyl claim 1 , or a heterocyclyl claim 1 , each of which is optionally substituted with one or more substituents selected from the group consisting of aryl claim 1 , heteroaryl claim 1 , cyclyl claim 1 , alkyl claim 1 , alkoxyl claim 1 , halogen claim 1 , NH claim 1 , NH—(C-C)alkyl claim 1 , N—(C-C)alkyl-(C-C)alkyl claim 1 , (C-C)alkyl-OC— claim 1 , and heterocyclyl claim 1 , each of which other than halogen and NHis further optionally substituted with one or more substituents selected from the group consisting of NH claim 1 , OH claim 1 , NH—(C-C)alkyl and N—(C-C)alkyl-(C-C)alkyl.4. The compound or salt of claim 1 , wherein the cyclyl or heterocyclyl of R′ or R″ is a five-membered claim 1 , six-membered claim 1 , or seven-membered ring.5. The compound or salt of claim 1 , wherein the heterocyclyl contains one or two heteroatoms.6. The compound or salt of claim 1 , wherein R is methyl or H.8. The compound or salt of claim 7 , wherein one Ris at the ortho position relative to the carbon attached to the NR-L moiety.9. The compound or salt of claim 7 , wherein one Ris H claim 7 , F claim 7 , Cl claim 7 , Br claim 7 , methyl claim 7 , N(Me) claim 7 , NHMe claim 7 , 1-piperidinyl claim 7 , 2-(dimethylamino)ethyl)(methyl)amino claim 7 , pyrrolidin-1-yl claim 7 , 3-(dimethylamino)pyrrolidin-1-yl claim 7 , 2-hydroxy-2-methylpropylamino claim 7 , isopropylamino claim 7 , diethylamino claim 7 , 1-hydroxypropan-2-ylamino claim 7 , 2-hydroxyethylamino claim 7 , or phenyl.10. The compound or salt of claim 1 , wherein ...

Подробнее
09-05-2013 дата публикации

Organic light-emitting device, method of manufacturing the same, and flat panel display device including the same

Номер: US20130112949A1
Принадлежит: Samsung Display Co Ltd

An organic light-emitting device including: a substrate; a first electrode; a second electrode; an emission layer between the first electrode and the second electrode; and an electron transport layer between the emission layer and the second electrode, wherein the emission layer includes a blue emission layer, the electron transport layer includes a unit that includes a first single layer including a first material, a first mixed layer on the first single layer and including the first material and a second material, a second single layer on the first mixed layer and including the second material, a second mixed layer on the second single layer and including the first and second materials, and a third single layer on the second mixed layer and including the first material, wherein the first mixed layer has a thickness that is larger than that of the second mixed layer.

Подробнее
16-05-2013 дата публикации

2,5-DIOXOIMIDAZOLIDIN-1-YL-3-PHENYLUREA DERIVATIVES AS FORMYL PEPTIDE RECEPTOR LIKE-1 (FPRL-1) RECEPTOR MODULATORS

Номер: US20130123215A1
Принадлежит: ALLERGAN, INC.

The present invention relates to novel 2,5-dioxoimidazolidin-1-yl-3-phenylurea derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor. 2. A compound according to claim 1 , wherein:{'sup': '1', 'sub': '1-8', 'Ris halogen, hydrogen or optionally substituted Calkyl;'}{'sup': 2', '15', '9, 'sub': 1-8', '3, 'Ris halogen, optionally substituted Calkyl, CF, SR, ORor CN;'}{'sup': '3', 'sub': 1-8', '3-8', '3-8, 'Ris hydrogen, optionally substituted Calkyl, optionally substituted Ccycloalkyl or optionally substituted Ccycloalkenyl;'}{'sup': '4', 'sub': 1-8', '3-8', '3-8', '6-10, 'Ris optionally substituted Calkyl, optionally substituted Ccycloalkyl, optionally substituted Ccycloalkenyl, optionally substituted Caryl or optionally substituted heterocycle;'}{'sup': '5', 'sub': 1-8', '3-8', '3-8', '6-10, 'Ris optionally substituted Calkyl, optionally substituted Ccycloalkyl, optionally substituted Ccycloalkenyl, optionally substituted Caryl or optionally substituted heterocycle;'}{'sup': '6', 'sub': '1-8', 'Ris halogen, hydrogen or optionally substituted Calkyl;'}{'sup': '7', 'sub': '1-8', 'Ris halogen, hydrogen or optionally substituted Calkyl;'}{'sup': '8', 'sub': '1-8', 'Ris halogen, hydrogen or optionally substituted Calkyl;'}{'sup': '9', 'sub': 1-8', '1-8, 'Ris hydrogen, C(O)(Calkyl) or optionally substituted Calkyl; and'}{'sup': '15', 'sub': 1-8', '1-8, 'Ris hydrogen, optionally substituted Calkyl or O(Calkyl).'}7. A compound according to claim 1 , wherein:{'sup': '1', 'sub': '1-8', 'Ris halogen, hydrogen or optionally substituted Calkyl;'}{'sup': 2', '15', '9, 'sub': 1-8', '3, 'Ris halogen, optionally substituted Calkyl, SR, CF, ORor CN;'}{'sup': '3', 'sub': 1-8', '3-8', '3-8, 'Ris hydrogen, optionally substituted Calkyl, optionally substituted Ccycloalkyl or optionally substituted Ccycloalkenyl;'}{'sup': '4', 'sub': '1-8', 'Ris ...

Подробнее
23-05-2013 дата публикации

Heterocyclic Compound and Light-Emitting Element, Light-Emitting Device, Lighting Device, and Electronic Device Using the Same

Номер: US20130130061A1
Принадлежит: Semiconductor Energy Laboratory Co Ltd

To provide a novel heterocyclic compound having a bipolar property. To improve element characteristics of a light-emitting element by application of the novel heterocyclic compound to the light-emitting element. A heterocyclic compound represented by a general formula (G1) and a light-emitting element formed using the heterocyclic compound represented by the general formula (G1) are provided. When the heterocyclic compound represented by the general formula (G1) is used for the light-emitting element, the characteristics of the light-emitting element can be improved.

Подробнее
23-05-2013 дата публикации

LIGANDS FOR ANTIBODY AND Fc-FUSION PROTEIN PURIFICATION BY AFFINITY CHROMATOGRAPHY

Номер: US20130131321A1
Принадлежит: GRAFFINITY PHARMACEUTICALS GMBH

The present invention relates to the use for affinity purification of an antibody or an fragment of an antibody, of a ligand-substituted matrix comprising a support material and at least one ligand covalently bonded to the support material, the ligand being represented by formula (I) 2. The use of wherein Aris phenylene claim 1 , preferably methoxy-substituted phenylene.3. The use of wherein the C═O and the NH group are bonded to Arin meta position to each other.4. The use of wherein the 5- or 6-membered heterocyclic aromatic ring of Aris attached to the C═O group via a carbon ring atom which is adjacent to a ring heteroatom claim 1 , preferably a nitrogen or oxygen atom.5. The use of wherein the 5- or 6-membered heterocyclic aromatic ring of Arcontains two or more nitrogen atoms or one or more nitrogen atoms and an oxygen atom.6. The use of wherein the 5- or 6-membered heterocyclic aromatic ring of Aris N-methyl-substituted pyrazole claim 5 , pyridine claim 5 , isoxazole or oxadiazole.7. The use according to wherein the support material comprises a material selected from carbohydrates or crosslinked carbohydrates claim 1 , preferably agarose claim 1 , cellulose claim 1 , dextran claim 1 , starch claim 1 , alginate and carrageenan claim 1 , Sepharose claim 1 , Sephadex; synthetic polymers claim 1 , preferably polystyrene claim 1 , styrene-divinylbenzene copolymers claim 1 , polyacrylates claim 1 , PEG-Polycacrylate copolymers polymethacrylates claim 1 , polyvinyl alcohol claim 1 , polyamides and perfluorocarbons; inorganic materials claim 1 , preferably glass claim 1 , silica and metal oxides; and composite materials.8. The use according to wherein the protein is an antibody claim 1 , preferably an IgG type antibody claim 1 , or an Fc fusion protein.9. The use of wherein the purification is attained by binding of the ligand of the ligand-substituted matrix to an Fc fragment or domain of the antibody or the fusion protein.10. The use according to wherein the Fc ...

Подробнее
30-05-2013 дата публикации

Inhibition and Dispersion of Bacterial Biofilms with 2-Aminobenzimidazole Derivatives

Номер: US20130136782A1
Принадлежит: Individual

Compounds described herein inhibit biofilm formation or disperse pre-formed biofilms of Gram-negative bacteria. Biofilm-inhibitory compounds can be encapsulated or contained in a polymer matrix for controlled release. Coatings, films, multilayer films, hydrogels, microspheres and nanospheres as well as pharmaceutical compositions and disinfecting compositions containing biofilm-inhibitory compounds are also provided. Methods for inhibiting formation of biofilms or dispersing already formed biofilms are provided. Methods for treating infections of gram-negative bacteria which form biofilms, particularly those of Pseudomonas and more particularly P. aeruginosa.

Подробнее
30-05-2013 дата публикации

PROCESS FOR MANUFACTURE OF TELMISARTAN

Номер: US20130137878A1
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

A process for preparing telmisartan by reacting 2-n-propyl-4-methyl-6-(1′-methylbenzimidazol-2′-yl)benzimidazole with a compound of formula (IV) 128-. (canceled)30. The process according to claim 29 , wherein the product of step (a) is worked up before step (b) is performed.31. The process according to claim 29 , wherein the telmisartan product of step (b) is worked up and converted into the hydrochloride.32. The process according to claim 29 , wherein the product of step (a) is worked up before step (b) is performed and the telmisartan product of step (b) is worked up and converted into the hydrochloride.33. The process according to claim 29 , wherein Z is a halogen atom or a substituted sulfonyloxy group.34. The process according to claim 29 , wherein Z is a bromine atom.35. The process according to claim 29 , wherein the first solvent is selected from methylene chloride claim 29 , diethyl ether claim 29 , tetrahydrofuran claim 29 , dioxane claim 29 , dimethylsulfoxide claim 29 , dimethylformamide claim 29 , dimethylacetamide claim 29 , dimethylformamide/tert-butanol claim 29 , dimethylacetamide/tert-butanol claim 29 , toluene claim 29 , benzene claim 29 , or a mixture thereof.36. The process according to claim 35 , wherein step (a) is carried out in the presence of an acid-binding agent.37. The process according to claim 36 , wherein the acid-binding agent is selected from sodium carbonate claim 36 , potassium carbonate claim 36 , sodium hydroxide claim 36 , potassium hydroxide claim 36 , sodium methoxide claim 36 , potassium methoxide claim 36 , potassium tert-pentoxide claim 36 , potassium tert-butoxide claim 36 , potassium n-butoxide claim 36 , sodium hydride claim 36 , triethylamine claim 36 , and pyridine.38. The process according to claim 29 , wherein step (a) is carried out at a temperature between 0° C. and 100° C.39. The process according to claim 30 , wherein step (a) is carried out at a temperature between 0° C. and 100° C.40. The process according to ...

Подробнее
06-06-2013 дата публикации

Novel hydroxamates as therapeutic agents

Номер: US20130142758A1
Принадлежит: Pharmacyclics LLC

The present invention is directed to certain hydroxamate derivatives that are useful in the treatment of hepatitis C. These compounds are also inhibitors of histone deacetylase and are therefore useful in the treatment of diseases associated with histone deacetylase activity. Pharmaceutical compositions and processes for preparing these compounds are also disclosed.

Подробнее
06-06-2013 дата публикации

POSITIVE ALLOSTERIC MODULATORS OF MGLUR2

Номер: US20130143880A1
Принадлежит:

The present invention is directed to benzimidazolone derivatives which are positive allosteric modulators of the mGluRreceptor, useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluRreceptor is involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved, such as schizophrenia. 2. The compound according to wherein Y is methyl.3. The compound according to wherein Ris selected from the group consisting of: cyclopropylmethyl claim 1 , 2 claim 1 ,2-difluorocyclopropylmethyl claim 1 , 2 claim 1 ,2-difluoro-1-methylcyclopropylmethyl claim 1 , 1-(trifluoromethyl)cyclopropylmethyl claim 1 , 4 claim 1 ,4 claim 1 ,4-trifluoro-2 claim 1 ,2-dimethylbutyl claim 1 , cyclobutylmethyl claim 1 , 2 claim 1 ,2-dimethylpropyl claim 1 , prop-2-enyl claim 1 , biphenyl and benzyl claim 1 , optionally substituted with methoxy or —OCF.5. The compound according to wherein Ris selected from the group consisting of halo claim 4 , —CN claim 4 , —N(O) claim 4 , amino claim 4 , —N(Calkyl) claim 4 , —C(O)—O—Calkyl claim 4 , —C(O)—Calkyl claim 4 , —S(O)—Calkyl claim 4 , Ccycloalkyl claim 4 , —C(Calkyl)-NHC(O)—O—Calkyl and Calkyl optionally substituted with 1 to 4 substituents independently selected from hydroxy and halo.7. The compound according to wherein Ris selected from the group consisting of: halo claim 6 , —CN claim 6 , —N(O) claim 6 , amino claim 6 , —N(Calkyl) claim 6 , —C(O)—O—Calkyl claim 6 , —C(O)—Calkyl claim 6 , —S(O)—Calkyl claim 6 , Ccycloalkyl and Calkyl optionally substituted with 1 to 4 substituents independently selected from hydroxy and halo.9. The compound according to wherein ring B is phenyl.10. The compound according to wherein ring B is pyridyl.11. The compound according to wherein Eis C and ...

Подробнее
20-06-2013 дата публикации

2-(2-Hydroxybiphenyl-3-yl)-1H-Benzoimidazole-5-Carboxamidine Derivatives as Factor VIIA Inhibitors

Номер: US20130157298A1
Принадлежит: Pharmacyclics LLC

The present invention relates to novel inhibitors of Factors VIIa, IXa, Xa, XIa, in particular Factor VIIa, pharmaceutical compositions comprising these inhibitors, and methods for using these inhibitors for treating or preventing thromboembolic disorders, cancer or rheumatoid arthritis. Processes for preparing these inhibitors are also disclosed.

Подробнее
20-06-2013 дата публикации

NOVEL HETEROCYCLIC COMPOUND, AND COMPOSITION FOR TREATING INFLAMMATORY DISEASES USING SAME

Номер: US20130158047A1
Принадлежит: NEOPHARM CO., LTD.

Provided are heterocyclic compounds, having effects of treating and preventing inflammatory diseases and treating skin wounds, and particularly, exhibiting effects of recovering disrupted skin barriers, mitigating inflammation, and pruritus. Also, a composition containing the compound as an effective component can be used to mitigate various inflammatory diseases and protease activated receptor-2 (PAR-2)-overexpressed diseases, and can be particularly used as a composition having an anti-inflammatory function in inflammatory skin diseases including atopic dermatitis and the like, by inhibiting PAR-2 activity. 6. A pharmaceutical composition claim 1 , comprising the heterocyclic compound or a pharmaceutically acceptable salt thereof according to and a pharmaceutically acceptable carrier.7. The pharmaceutical composition of claim 6 , which is effective in treating and preventing inflammatory skin diseases covering acne claim 6 , rosacea claim 6 , seborrheic dermatitis claim 6 , atopic dermatitis claim 6 , post-inflammatory hyperpigmentation (PIH) claim 6 , contact dermatitis claim 6 , pruritus claim 6 , psoriasis claim 6 , Lichen planus claim 6 , eczema claim 6 , skin infections claim 6 , and Netherton Syndrome.8. A method for treating skin wounds claim 1 , comprising administering an effective amount of the heterocyclic compound or a pharmaceutically acceptable salt thereof according to to a subject in need thereof.9. A method for treating and preventing metastasis of cancer claim 1 , gastrointestinal disease claim 1 , asthma claim 1 , and liver cirrhosis claim 1 , comprising administering an effective amount of the heterocyclic compound of or a pharmaceutically acceptable salt thereof according to to a subject in need thereof.10. A protease activated receptor-2 (PAR-2) inhibitor composition comprising the heterocyclic compound or a pharmaceutically acceptable salt thereof according to .11. A cosmetic composition comprising the heterocyclic compound or a ...

Подробнее
20-06-2013 дата публикации

MANUFACTURE, COMPOSITIONS AND USES OF COAGULATION FACTOR VIIa MODULATOR

Номер: US20130158089A1
Автор: David Loury, Tarak Mody
Принадлежит: Pharmacyclics LLC

Treatment of cancer and thromboembolic disorders using inhibitors of Factor VIIa are disclosed herein using a compound of Formula I:

Подробнее
20-06-2013 дата публикации

PREPARATION OF BENDAMUSTINE AND ITS SALTS

Номер: US20130158273A1
Принадлежит:

The present application relate to processes for the preparation of bendamustine and its pharmaceutically acceptable salts. 2. The process of claim 1 , wherein the 2-haloethanol consists of 2-chloroethanol claim 1 , 2-bromoethanol claim 1 , or 2-iodoethanol.3. The process of claim 1 , wherein the organic base consists of triethylamine claim 1 , diisopropyl amine claim 1 , diisopropyl-ethylamine claim 1 , DABCO claim 1 , pyridine claim 1 , lutidine claim 1 , 4-dimethylaminopyridine claim 1 , or 4-methylmorpholine.4. The process of claim 1 , wherein the organic base consists of triethylamine claim 1 , diisopropyl amine claim 1 , or diisopropyl-ethylamine.5. The process of claim 1 , wherein the chlorinating agent used in step b) consists of sulphuryl chloride claim 1 , thionyl chloride claim 1 , phosphorous trichloride claim 1 , phosphorous pentachloride claim 1 , or phosphorous oxychloride.6. The process of claim 1 , wherein step b) is carried out in the presence of a halogenated hydrocarbon solvent.7. The process of claim 1 , where in step b) consists of:a) reacting the compound of formula (Ill) with a chlorinating agent in the presence of a halogenated hydrocarbon solvent;b) adding water;c) separating the organic layer, optionally concentrating to a minimum volume;{'sub': 5', '8, 'd) adding an anti-solvent selected from a C-Calkane, such as pentane, hexane, or heptane; and'}e) isolating the compound of formula (IV) as a solid.8. The process of claim 1 , wherein step c) is carried out using aqueous hydrochloric acid.9. The process of claim 1 , wherein step c) is carried out using aqueous hydrochloric acid having concentration from about 0.5 N to about 5 N.10. The process of claim 1 , wherein step c) is carried out using aqueous hydrochloric acid and at temperatures less than about 60° C.11. A process for the purification of bendamustine hydrochloride claim 1 , comprising:a) combining bendamustine hydrochloride, aqueous hydrochloric acid, and acetonitrile;b) heating ...

Подробнее
04-07-2013 дата публикации

2,3-DIARYL- OR HETEROARYL-SUBSTITUTED 1,1,1-TRIFLUORO-2-HYDROXYPROPYL COMPOUNDS

Номер: US20130172335A1
Принадлежит: Hoffmann-La Roche Inc.

The present invention relates to compounds of formula I 2. A compound according to claim 1 , wherein A is C—R.3. A compound according to claim 1 , wherein one of Rand Ris selected from the group consisting of:{'sub': 1-7', '1-7', '1-7', '1-7', '1-7, 'phenyl, said phenyl being substituted by a group selected from carboxyl, carboxyl-C-alkyl, carboxyl-C-alkoxy, C-alkoxycarbonyl, C-alkoxycarbonyl-C-alkyl,'}{'sub': 1-7', '1-7', '1-7', '1-7', '1-7', '1-7, 'C-alkoxycarbonyl-C-alkoxy and aminocarbonyl, and, in addition, optionally substituted by one or two substituents selected from the group consisting of C-alkyl, halogen, halogen-C-alkyl, C-alkoxy and halogen-C-alkoxy;'}{'sub': 1-7', '1-7', '1-7', '1-7', '1-7', '1-7', '1-7', '1-7', '1-7', '1-7', '1-7', '1-7', '1-7', '1-7', '1-7', '1-7', '1-7', '1-7', '1-7', '1-7', '1-7, 'phenyloxy, wherein the phenyl ring is unsubstituted or substituted by one, two or three substituents selected from the group consisting of C-alkyl, halogen, halogen-C-alkyl, C-alkoxy, halogen-C-alkoxy; carboxyl, carboxyl-C-alkyl, carboxyl-C-alkoxy, C-alkoxycarbonyl, C-alkoxycarbonyl-C-alkyl, C-alkoxycarbonyl-C-alkoxy and aminocarbonyl, heteroaryl selected from the group consisting of pyridyl, pyridazinyl, pyrimidinyl and pyrazinyl, said heteroaryl being unsubstituted or substituted by one, two or three substituents selected from the group consisting of C-alkyl, halogen, halogen-C-alkyl, C-alkoxy, halogen-C-alkoxy, carboxyl, carboxyl-C-alkyl, carboxyl-C-alkoxy, C-alkoxycarbonyl, C-alkoxycarbonyl-C-alkyl, C-alkoxycarbonyl-'}{'sub': '1-7', 'C-alkoxy and aminocarbonyl;'}{'sub': 1-7', '1-7', '1-7', '1-7', '1-7', '1-7', '1-7', '1-7', '1-7', '1-7', '1-7, 'heteroaryloxy, wherein heteroaryl is selected from the group consisting of pyridyl, pyridazinyl, pyrimidinyl and pyrazinyl, and is unsubstituted or substituted by one, two or three substituents selected from the group consisting of C-alkyl, halogen, halogen-C-alkyl, C-alkoxy, halogen-C-alkoxy; carboxyl, ...

Подробнее
04-07-2013 дата публикации

Benzimidazole derivatives as selective blockers of persistent sodium current

Номер: US20130172342A1
Принадлежит: Allergan Inc

The present invention is directed to methods of treating diseases or conditions mediated by elevated persistent sodium channel, such as ocular disorders, pain, multiple sclerosis, and seizure disorders utilizing a compound of Formula I or a pharmaceutically acceptable salt thereof or a pharmaceutical composition comprising said compound, wherein variables R, R 1 , R 2 , R 3 , R 4 , R 5 , m, and n in Formula I are as defined herein.

Подробнее
04-07-2013 дата публикации

NOVEL CANNABINOID RECEPTOR 2 (CB2) INVERSE AGONISTS AND THERAPEUTIC POTENTIAL FOR MULTIPLE MYELOMA AND OSTEOPOROSIS BONE DISEASES

Номер: US20130172388A1

Cannabionid receptor-2 inverse antagonists include compounds represented by Formula IV, or a pharmaceutically acceptable salt thereof: 3. The compound according to claim 2 , wherein R′″ is (C-C)heterocycloalkyl.4. The compound according to claim 3 , wherein R′″ is oxetanyl claim 3 , tetrahydrofuranyl claim 3 , tetrahydropyranyl claim 3 , oxepanyl claim 3 , tetrahydrothiophenyl claim 3 , tetrahydrothiopyranyl claim 3 , 1 claim 3 ,3-dioxanyl claim 3 , oxazolidinyl claim 3 , azetidinyl claim 3 , pyrrolidinyl claim 3 , piperidinyl claim 3 , azepinyl claim 3 , piperazinyl claim 3 , morpholinyl claim 3 , tetrahydrothiopyranyl-1-oxide claim 3 , tetrahydrothiopyranyl-1 claim 3 ,1-dioxide claim 3 , pyrrolidinonyl claim 3 , piperidinonyl claim 3 , azepinonyl claim 3 , piperazidinonyl claim 3 , oxazidilinonyl claim 3 , azetidinonyl claim 3 , or morpholinonyl.7. (canceled)8. The compound according to claim 1 , wherein the compound conforms to Formula I′ and whereinD is H;D′ is phenyl;{'sub': 1', '6, 'B and Q are independently (C-C)alkylene;'}e is 0 and each of f and g is 1; and{'sup': a′', 'a″', 'a′″, 'sub': 1', '6, 'each of R, R, and R is independently selected from the group consisting of H, and straight or branched chain (C-C)alkyl.'}10. (canceled)12. The compound according to claim 11 , wherein subscripts h and k independently are 0 and subscript j is 1.14. (canceled)16. The compound according to claim 15 , wherein substituent X is N claim 15 , T and R are each independently S(O)— and Q′ is (C-C)alkyl.17. The compound according to claim 15 , wherein substituent X is CH— and each of Q′ claim 15 , R and T are independently —O—(CH)—O— claim 15 , —OC(O)— or (CH)—OC(O)—.2022-. (canceled)23. A pharmaceutical composition comprising a therapeutically effective amount of a compound according to claim 1 , or a pharmaceutically acceptable salt thereof; and a pharmaceutically acceptable carrier.24. (canceled)25. A method for treating multiple myeloma or osteoporosis in a subject by ...

Подробнее
04-07-2013 дата публикации

BENZIMIDAZOLE DERIVATIVES AS SELECTIVE BLOCKERS OF PERSISTENT SODIUM CURRENT

Номер: US20130172389A1
Принадлежит: Allegan, Inc.

The present invention is directed to a compound of Formula I 2. The compound of claim 1 , wherein R is and unsubstituted straight chain or branched Calkyl.3. The compound of claim 1 , wherein R is Calkyl which is substituted with a Caryloxy group.4. The compound of claim 3 , wherein the “aryl” portion of said Caryloxy group is unsubstituted or substituted with 1-2 Calkyl or Calkoxy substitutents.5. The compound of claim 1 , wherein R is Calkyl which is substituted with a heteroaryl substitutent claim 1 , wherein said heteroaryl group is five- to six-membered ring containing 1-2 ring N atoms claim 1 , and wherein when said five- to six-membered ring containing 1-2 ring N atoms has two substituents on adjacent carbon atoms claim 1 , said substituents together with the carbon atoms to which they are attached can optionally form a phenyl ring claim 1 , and wherein said six-membered ring containing 1-2 ring N atoms claim 1 , optionally with said phenyl ring is optionally further substituted with a ring system substituent.6. The compound of claim 5 , wherein said five- to six-membered ring containing 1-2 ring N atoms claim 5 , optionally with said phenyl ring is selected from the group consisting of pyrzolyl claim 5 , imidazolyl claim 5 , pyrimidinyl claim 5 , pyrazinyl claim 5 , and benzimidazolyl.7. The compound of claim 6 , wherein said five- to six-membered ring containing 1-2 ring N atoms claim 6 , optionally with said phenyl ring is selected from the group consisting of is imidazolyl and benzimidazolyl.8. The compound of claim 1 , wherein R is Calkyl which is substituted with a —N(Calkyl)substituent.10. The compound of claim 1 , wherein Rand Rare both H.11. The compound of claim 10 , wherein m is 1 or 2.12. The compound of claim 10 , wherein m is 1 claim 10 , and X is O.13. The compound of claim 10 , wherein m is 2 claim 10 , and X is a covalent bond.14. The compound of claim 10 , wherein m is 1 claim 10 , and X is —S(═O)—.15. The compound of claim 10 , wherein m is ...

Подробнее
18-07-2013 дата публикации

Compounds acting at multiple prostaglandin receptors giving a general anti-inflammatory response

Номер: US20130184463A1
Принадлежит: Allergan Inc

The present invention provides a compound, that is a 1-({halo-2-[(2-hydrocarbyl or substituted hydrocarbyl)oxy]phenyl}methyl)-(fused bicyclic nitrogen heteroaryl) carboxylic acid or an ester or sulfonamide thereof. The compound may be represented by the following formula Wherein R 1 , R 2 , R 3 , R 4 A, X, W, Z and Y are as defined in the specification. The compounds may be administered to treat DP, FP, EP1, TP and/or EP4 receptor-mediated diseases or conditions.

Подробнее
18-07-2013 дата публикации

Process for the preparation of bendamustine hydrochloride and related compounds

Номер: US20130184471A1
Принадлежит: Arevipharma GmbH

The present invention relates to a process for preparing bendamustine hydrochloride, derivatives and related compounds thereof. 2. The process according to claim 1 , wherein the reaction is carried out in the absence of a solvent.3. The process according to claim 1 , wherein 5 to 9 molar equivalents of POClare used relative to the molar amount of compound of formula I.4. The process according to claim 1 , wherein the POClis heated to about 60-70° C. before addition of the compound of formula I.5. The process according to claim 1 , wherein subsequent to a complete addition of compound of formula I claim 1 , the resulting reaction mixture is heated to reflux temperature for a predetermined time.7. The process according to claim 6 , wherein the aqueous HCl has a concentration of 15 to 32% by weight relative to the total weight of aqueous HCl.8. The process according to claim 6 , wherein 25 to 50 molar equivalent HCl are used relative to the molar amount of crude compound of formula II.9. The process according to claim 1 , wherein Ris C1-C6 alkyl claim 1 , Ris C1-C6 alkylene claim 1 , Yand Yrepresent oxygen claim 1 , and Prot is C1-C4 alkyl.11. The process according to claim 10 , wherein the chlorinating agent is POCl.12. The process according to claim 10 , wherein chlorination by means of POClis carried out by applying a process according to .13. The process according to claim 10 , wherein the solubilizer is an end-capped ethylene glycol or polyethyleneglycol of formula{'br': None, 'sub': 2', '2', 'n, 'A-(CH—CH)—B'}wherein n=1 to 30 and A and B independently from each other represent C1-C12 alkyl.15. The process according to claim 14 , wherein the aqueous HCl has a concentration of 15 to 32% by weight relative to the total weight of aqueous HCl.16. The process according to claim 14 , wherein 25 to 50 molar equivalent HCl are used relative to the molar amount of crude compound of formula II.17. The process according to claim 10 , wherein Ris C1-C6 alkyl claim 10 , Ris ...

Подробнее
25-07-2013 дата публикации

Mediators of Hedgehog Signaling Pathways, Compositions and Uses Related Thereto

Номер: US20130190350A1
Принадлежит: CURIS, INC.

The present invention makes available methods and reagents for inhibiting aberrant growth states resulting from hedgehog gain-of-function, ptc loss-of-function or smoothened gain-of-function comprising contacting the cell with a hedgehog antagonist, such as a small molecule, in a sufficient amount to aberrant growth state, e.g., to agonize a normal ptc pathway or antagonize smoothened or hedgehog activity. 136.-. (canceled)38. The compound of claim 37 , wherein X—Y—Z includes an amide claim 37 , urea claim 37 , or sulfonamide.39. The compound of claim 37 , wherein Ris optionally substituted with from 1-5 substituents.40. The compound of claim 37 , wherein the substituents on Rare selected from nitro claim 37 , halogen claim 37 , cyano claim 37 , lower alkyl claim 37 , acylamino claim 37 , alkoxy claim 37 , alkylamino claim 37 , a substituted or unsubstituted cycloalkyl claim 37 , heterocyclyl claim 37 , aryl claim 37 , and heteroaryl fused to the aryl or heteroaryl ring.41. The compound of claim 37 , wherein Rrepresents from 1-4 substituents as defined.42. The compound of claim 41 , wherein Rrepresents from 1-4 substituents selected from halogen claim 41 , cyano claim 41 , nitro claim 41 , alkoxy claim 41 , amino claim 41 , acylamino claim 41 , a substituted or unsubstituted cycloalkyl claim 41 , heterocyclyl claim 41 , aryl claim 41 , or heteroaryl fused to G claim 41 , and substituted or unsubstituted lower alkyl.43. The compound of claim 37 , wherein Rrepresents a substituted or unsubstituted benzene ring claim 37 , cyclopentyl ring claim 37 , cyclohexyl ring claim 37 , thiophene ring claim 37 , furan ring claim 37 , isobenzofuran ring claim 37 , pyridine ring claim 37 , benzodioxane ring claim 37 , or benzodioxole ring.44. The compound of claim 37 , wherein Rrepresents a substituted or unsubstituted benzene ring or pyridine ring.46. A pharmaceutical composition comprising one or more compounds according to formulated together with one or more pharmaceutically ...

Подробнее
25-07-2013 дата публикации

PROCESSES FOR THE SYNTHESIS OF DIARYLTHIOHYDANTOIN AND DIARYLHYDANTOIN COMPOUNDS

Номер: US20130190507A1
Принадлежит:

Processes are provided for the synthesis of diarylthiohydantoin and diarylhydantoin compounds. Medicinal products containing the same find particular use in treating prostate cancer, including castration-resistant prostate cancer and/or hormone-sensitive prostate cancer. 3. The process of claim 1 , wherein X is S.4. The process of claim 1 , wherein Yand Yare both methyl.5. The process of claim 1 , wherein Yand Ytogether with the carbon to which they are attached combine to form a cyclobutyl ring or a cyclopentyl ring.6. The process of claim 1 , wherein Lis a single bond.7. The process of claim 1 , wherein Ris —C(═O)—NHCH.8. The process of claim 1 , wherein Ris —C(═O)—NH.9. The process of claim 1 , wherein Ris F.10. The process of claim 1 , wherein Yand Yare both methyl claim 1 , Ris —C(═O)—NHCH claim 1 , and Ris F.11. The process of claim 1 , wherein Yand Yare both methyl claim 1 , Ris —C(═O)—NH claim 1 , and Ris F.13. The process of claim 12 , wherein X is S.1412. The process of claim 12 , wherein Yand Yare both methyl claim 12 , Ris —C(═O)—OH claim 12 , and Ris F. This patent application is a continuation of Ser. No. 13/580,718 filed Aug. 23, 2012 as a national phase application of PCT/US2011/026135 filed on Feb. 24, 2011, which claims priority to Ser. No. 61/307,796, filed Feb. 24, 2010. Each of these applications is incorporated herein by reference in its entirety.Not applicable.The invention is in the field of cancer therapeutics, such as processes for the synthesis of prostate cancer therapeutics.According to the American Cancer Society, prostate cancer is the most commonly diagnosed cancer among men in the United States, other than skin cancer. The American Cancer Society estimates that approximately 186,000 new cases of prostate cancer were diagnosed, and approximately 29,000 men died of prostate cancer in the United States alone during 2008. Prostate cancer is thus the second-leading cause of cancer death in men in the United States, after lung cancer. ...

Подробнее
01-08-2013 дата публикации

Benzimidazole Derivatives As PI3 Kinase Inhibitors

Номер: US20130196990A1
Принадлежит:

This invention relates to the use of benzimidazole derivatives for the modulation, notably the inhibition of the activity or function of the phosphoinositide 3′ OH kinase family (hereinafter PI3 kinases), suitably, PI3Kα, PI3Kδ, PI3Kβ, and/or PI3Kγ. Suitably, the present invention relates to the use of benzimidazoles in the treatment of one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries. More suitably, the present invention relates to PI3Kβ selective benzimidazoles compounds for treating cancer. 116.-. (canceled) This invention relates to the use of benzimidazole derivatives for the modulation, notably the inhibition of the activity or function of the phosphoinositide 3′ OH kinase family (hereinafter PI3 kinases), suitably, PI3Kα, PI3Kδ, PI3Kβ, and/or PI3Kγ. Suitably, the present invention relates to the use of benzimidazoles in the treatment of one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries. More suitably, the present invention relates to PI3Kβ selective benzimidazoles compounds for treating cancer.The phosphoinositide 3-kinase (PI3K) pathway is among the most commonly activated in human cancer and the importance in carcinogenesis is well established (Samuels Y and Ericson K. Oncogenic PI3K and its role in cancer. 2006; 18:77-82). Initiation of signaling begins with the phosphorylation of phosphatidylinositol-4,5-bisphosphate (PIP2) to produce phosphatidylinositol-3,4,5-P3 (PIP3). PIP3 is a critical second messenger which recruits proteins ...

Подробнее
01-08-2013 дата публикации

Benzimidazole Derivatives As PI3 Kinase Inhibitors

Номер: US20130197221A1
Принадлежит: GlaxoSmithKline LLC

This invention relates to the use of benzimidazole derivatives for the modulation, notably the inhibition of the activity or function of the phosphoinositide 3′ OH kinase family (hereinafter PI3 kinases), suitably, PI3Kα, PI3Kδ, PI3Kβ, and/or PI3Kγ. Suitably, the present invention relates to the use of benzimidazoles in the treatment of one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries. More suitably, the present invention relates to PI3Kβ selective benzimidazoles compounds for treating cancer. 1. A process for the preparation of the benzimidazole of formula (3)comprising the steps ofester hydrolyzing the methyl ester of formula (2)with lithium hydroxide in THF/water,wherein{'sub': 3', '2', '1-6, 'R2 is selected from H, —NHRa, alkoxy, halogen, —CF, —CHF, and Calkyl;'}R3 is selected from aryl and heteroaryl, wherein said aryl or heteroaryl may be substituted by one to three Rc;R4 is selected from H or Ra;{'sub': '1-6', 'each R5 is independently selected from Calkyl;'}{'sub': '1-3', 'each Ra is independently selected from Calkyl;'}{'sub': 1-3', '3, 'each Rc is independently selected from Calkyl, halogen, —CF, and hydroxy; and'}n is 0-2,or a pharmaceutically acceptable salt thereof. This application is filed as a continuation application of U.S. Ser. No. 13/251,476, filed Oct. 3, 2011, and claims priority to U.S. Provisional Application Ser. No. 61/390,314, filed Oct. 6, 2010, and U.S. Provisional Application Ser. No. 61/528,397, filed Aug. 29, 2011, both of which are incorporated herein by reference.This invention relates to the use of benzimidazole derivatives for the modulation, notably the inhibition of the activity or function of the phosphoinositide 3′ OH kinase family (hereinafter PI3 kinases), ...

Подробнее
08-08-2013 дата публикации

PROCESS FOR PREPARING BENZOIC ACID ESTERS

Номер: US20130204009A1
Принадлежит: Daiichi Sankyo Company, Limited

There is provided a more industrially advantageous process for preparing novel pyridine derivatives expected to be used as medicines. A process for preparing 3-[(6-hydroxy-1-methyl-1H-benzimidazol-2-yl)methoxy]benzoic acid esters as intermediates with high quality, in short steps and in a high yield, as well as novel benzoic acid esters as their precursors and a process for preparing the same. 2. The preparation process according to claim 1 , wherein A is a methyl group.3. The preparation process according to claim 1 , wherein B is a phenyl group.4. The preparation process according to claim 1 , wherein the solvent is a halogenated hydrocarbon claim 1 , a nitrile claim 1 , an ether or a mixed solvent thereof.5. The preparation process according to claim 1 , wherein the solvent is tetrahydrofuran.6. The preparation process according to claim 1 , wherein the solvent is a halogenated hydrocarbon claim 1 , a nitrile claim 1 , an ether claim 1 , an amide claim 1 , a carboxylate or a mixed solvent thereof.7. The preparation process according to claim 1 , wherein the solvent is N claim 1 ,N-dimethylacetamide.8. The preparation process according to claim 1 , wherein the preparation process proceeds in the presence of a halogenating agent.9. The preparation process according to claim 8 , wherein the halogenating agent is thionyl chloride claim 8 , oxalyl chloride or phosphorus pentachloride.10. The preparation process according to claim 8 , wherein the halogenating agent is thionyl chloride.11. The preparation process according to claim 8 , wherein the compound represented by the general formula (1) and the compound represented by the general formula (2) are previously mixed and the halogenating agent is added thereto.12. The preparation process according to claim 1 , wherein the preparation process proceeds in the presence of a base.13. The preparation process according to claim 12 , wherein the base is an alkali metal hydride.14. The preparation process according to claim ...

Подробнее
15-08-2013 дата публикации

Compounds and Their Use as BACE Inhibitors

Номер: US20130210837A1
Принадлежит: AstraZeneca Intellectual Property

The present invention relates to compounds of formula (I) and their pharmaceutical compositions. In addition, the present invention relates to therapeutic methods for the treatment and/or prevention of Aβ-related pathologies such as Down's syndrome, β-amyloid angiopathy such as but not limited to cerebral amyloid angiopathy or hereditary cerebral hemorrhage, disorders associated with cognitive impairment such as but not limited to MCI (“mild cognitive impairment”), Alzheimer's disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegeneration associated with diseases such as Alzheimer's disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration. 125-. (canceled)27. A compound according to or a pharmaceutically acceptable salt thereof claim 26 , wherein Ris Calkyl.28. A compound according to or a pharmaceutically acceptable salt thereof claim 27 , wherein Ris methyl or ethyl.29. A compound according to or a pharmaceutically acceptable salt thereof claim 26 , wherein Ris aryl claim 26 , heteroaryl claim 26 , Calkynyl claim 26 , halogen claim 26 , NHC(O)Ror ORwherein:{'sub': '2-6', 'sup': '7', 'said aryl, heteroaryl, or Calkynyl is optionally substituted with one to three R.'}30. A compound according to or a pharmaceutically acceptable salt thereof claim 26 , wherein Rand Rare independently hydrogen or heterocyclyl wherein:{'sub': '1-6', 'sup': '8', 'said heterocyclyl is optionally substituted with one or two substituents independently selected from Calkyl or OR.'}31. A compound according to or a pharmaceutically acceptable salt thereof claim 26 , wherein Rand R claim 26 , together with the carbon to which they are attached claim 26 , form a ring B claim 26 , wherein ring B is:{'sub': '1-6', 'sup': '8', 'a 3-14 membered cycloalkyl or heterocyclyl monocyclic ring, ...

Подробнее
22-08-2013 дата публикации

Tricyclic compounds and methods of use therefor

Номер: US20130217666A1
Принадлежит: Genentech Inc

The invention relates to novel compounds of Formula I: wherein A 1 , A 2 , A 3 , A 4 , A 5 , A 6 , R 2 , R 4 , R 5 , R 6 , R 7 , R 8 and subscripts m and n each has the meaning as described herein. Compounds of Formula I and pharmaceutical compositions thereof are useful in the treatment of disease and disorders in which undesired or over-activation of NF-kB signaling is observed.

Подробнее
22-08-2013 дата публикации

BENZIMIDAZOLE AND AZABENZIMIDAZOLE COMPOUNDS THAT INHIBIT ANAPLASTIC LYMPHOMA KINASE

Номер: US20130217668A1
Принадлежит: Amgen Inc.

Compounds of Formula (I) are useful inhibitors of anaplastic lymphoma kinase. Compounds of Formula (I) have the following structure: where the definitions of the variables are provided herein. 2. The compound of claim 1 , wherein X is N claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , tautomer thereof claim 1 , a pharmaceutically acceptable salt of the tautomer claim 1 , or a stereoisomer of any of the foregoing.3. The compound of claim 1 , wherein X is CR claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , tautomer thereof claim 1 , a pharmaceutically acceptable salt of the tautomer claim 1 , or a stereoisomer of any of the foregoing.4. The compound of claim 3 , wherein Ris —H claim 3 , or a pharmaceutically acceptable salt thereof claim 3 , tautomer thereof claim 3 , a pharmaceutically acceptable salt of the tautomer claim 3 , or a stereoisomer of any of the foregoing.5. The compound of claim 1 , wherein Ris —H claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , tautomer thereof claim 1 , a pharmaceutically acceptable salt of the tautomer claim 1 , or a stereoisomer of any of the foregoing.6. The compound of claim 1 , wherein Z is selected from —OMe or —NH-cyclohexyl; or an unsubstituted or substituted phenyl claim 1 , pyridyl claim 1 , benzothiophenyl claim 1 , thiazolyl claim 1 , pyradizinyl claim 1 , pyrimidinyl claim 1 , indolyl claim 1 , cyclohexyl claim 1 , morpholinyl claim 1 , pyrrolidinyl claim 1 , piperazinyl claim 1 , or piperidinyl group claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , tautomer thereof claim 1 , a pharmaceutically acceptable salt of the tautomer claim 1 , or a stereoisomer of any of the foregoing.7. The compound of claim 1 , wherein Z is an unsubstituted or substituted phenyl claim 1 , pyridyl claim 1 , benzothiophenyl claim 1 , thiazolyl claim 1 , pyradizinyl claim 1 , pyrimidinyl claim 1 , indolyl claim 1 , cyclohexyl claim 1 , morpholinyl claim 1 , pyrrolidinyl claim 1 , ...

Подробнее
22-08-2013 дата публикации

COMPOUNDS FOR MODULATING RNA BINDING PROTEINS AND USES THEREFOR

Номер: US20130217685A1
Автор: Ryder Sean
Принадлежит: University of Massachusetts

The invention relates to compositions and methods for inhibiting RNA binding proteins (e.g., MEX-3, MEX-5 and POS-1), as well as methods for treating and preventing disorders associated with parasitic infections and inflammatory disorders. 1. A method for treating or preventing a parasitic associated state in a subject comprising administering to said subject an effective amount of an RNA binding modulatory compound , such that said parasitic associate state is treated or prevented.3. The method of claim 1 , wherein the RNA binding modulatory compound is a compound of Table 1 or Table 2 claim 1 , and pharmaceutically acceptable salts thereof.4. The method of claim 1 , wherein said subject is a plant claim 1 , an animal or a human.56-. (canceled)7. The method of claim 1 , wherein said parasitic associated state is a parasitic infestation or parasitic re-infestation or a disease caused by a parasitic infestation.8. (canceled)9. The method of claim 1 , wherein said method includes protecting plants from a parasitic infestation claim 1 , inhibiting embryogenesis in a parasite or in a subject suffering from a parasitic infestation claim 1 , or reducing parasitic burden in soil claim 1 , in plants or in an animal suffering from a parasitic infection.10. The method of claim 1 , wherein said parasite is a helminth.11. The method of claim 10 , wherein said helminth is selected from the group consisting of a cestode claim 10 , a trematode and a nematode.12. (canceled)13. A method for inhibiting embryogenesis in a parasite claim 10 , comprising contacting said parasite with an effective amount of an RNA binding modulatory compound claim 10 , such that said embryogenesis is inhibited.15. The method of claim 13 , wherein the RNA binding modulatory compound is a compound of Table 1 or Table 2 claim 13 , and pharmaceutically acceptable salts thereof.16. The method of claim 13 , wherein the parasite is present in a subject.1719-. (canceled)20. The method of claim 13 , wherein said ...

Подробнее
22-08-2013 дата публикации

PROCESS FOR PREPARING BENDAMUS TINE HYDROCHLORIDE MONOHYDRATE

Номер: US20130217888A1
Принадлежит: SHAILPA MEDICARE LIMITED

The present invention provide processes for the preparation of Bendamustine hydrochloride monohydrate of formula (I) 21. A process of preparation of Bendamustine hydrochloride monohydrate according to claim- , wherein reducing agent used in step D) is Raney Nickel or similar transition metals.3. A process of purification of Bendamustine hydrochloride or monohydrate comprising the steps ofa). reacting the crude Bendamustine Hydrochloride anhydrous or its hydrate or mixture thereof obtained from any source with aqueous hydrochloric acid solutionb). heating the contents upto a temperature ranging between 40 to 65° C.c). maintaining the reaction mass at heated temperature of step b) till desired acceptable purity profiled). cooling the mass to ambient temperature and stirred for time between 1 to 4 hours.e). isolating the product as substantially pure crystalline Form-SMf). optionally repeating the steps b) to step e)4. Substantially pure Bendamustine hydrochloride monohydrate crystalline Form-SM having purity by HPLC is more than about 98%.6. A process of preparation of Bendamustine hydrochloride monohydrate crystalline Form-SM comprising the steps ofa). reacting the crude Bendamustine or its pharmaceutically acceptable salts and their hydrates thereof obtained from any source with aqueous hydrochloric acid solutionb). heating the contents upto a temperature ranging between 40 to 65° C.c). maintaining the reaction mass at heated temperature of step b) till desired acceptable purity profiled). cooling the mass to ambient temperature and stirred for time between 1 to 4 hours.e). isolating the product as crystalline Form-SMf). optionally repeating the steps b) to step e)7. Bendamustine hydrochloride monohydrate crystalline Form-SM characterized by X-ray powder diffraction pattern comprising at least 5 characteristic peaks selected from the XRPD 2 theta degrees peaks at 7.42 , 10.60 , 11.17 , 16.43 , 17.94 , 22.89 , 26.33 , 28.77 , 30.28 , 31.92 , 40.89±0.1 2θ° and further ...

Подробнее
05-09-2013 дата публикации

PACTAMYCIN ANALOGS AND METHODS OF USE

Номер: US20130231377A1
Автор: Mahmud Taifo
Принадлежит:

Disclosed are pactamycin analogs, pharmaceutical compositions including the analogs, and methods of using the analogs, such as to inhibit tumor growth or a pathogenic infection such as a bacterial or parasitic infection. The pactamycin analogs have a general formula 4. The method of claim 1 , wherein Rand Rtogether form a heterocyclic 5-membered ring.56-. (canceled)7. The method of claim 1 , wherein Rand Rtogether form a heterocyclic 5-membered ring.8. (canceled)9. The method of claim 1 , wherein Ris a substituted benzoyl group.10. (canceled)1213-. (canceled)17. The compound of claim 14 , wherein Rand Rtogether form a heterocyclic 5-membered ring.18. (canceled)19. The compound of claim 14 , wherein Rand Rtogether form a heterocyclic 5-membered ring.20. (canceled)21. The compound of claim 14 , wherein Ris a substituted benzoyl group.22. (canceled)24. A pharmaceutical composition claim 14 , comprising a compound according to and a pharmaceutically acceptable carrier.25. A method of inhibiting a tumor in a subject claim 14 , comprising:selecting a subject for treatment that has, or is at risk for developing, a tumor;{'claim-ref': {'@idref': 'CLM-00024', 'claim 24'}, 'administering to the subject an effective amount of the pharmaceutical composition of , thereby treating the tumor in the subject.'}26. A method of treating an infection from a pathogen of interest in a subject claim 14 , comprising:selecting a subject for treatment that has, or is at risk for developing, an infection by a pathogen of interest;{'claim-ref': {'@idref': 'CLM-00024', 'claim 24'}, 'administering to the subject an effective amount of the pharmaceutical composition of , thereby treating the infection from the pathogen of interest in the subject.'}27. The method of claim 26 , wherein the pathogen of interest is a Gram-positive or Gram-negative bacterial pathogen.28. A method of inhibiting growth of a pathogen claim 14 , comprising contacting the pathogen with a composition of claim 14 , wherein ...

Подробнее
05-09-2013 дата публикации

NOVEL METHOD OF PREPARING BENZOIMIDAZOLE DERIVATIVES

Номер: US20130231477A1
Принадлежит: DAEWOONG PHARMACEUTICAL CO., LTD.

This invention relates to a method of preparing a benzoimidazole derivative at high purity and high yield so as to enable the production of the benzoimidazole derivative compound as an antagonist against a vanilloid reactor-1, and particularly to a method of preparing a benzoimidazole derivative at high purity and high yield, wherein the benzoimidazole derivative is synthesized using a novel intermediate, namely, benzaldehyde, and thereby the preparation process is simple so that it can be applied to production. 3. The method of or , wherein said palladium catalyst is any one selected from the group consisting of Pd(PPh) , Pd(dba) , PdCl(PPh)and Pd(PtBu).4. The method of or , wherein the step in 1) of or the step 1) of is further performed in the presence of a base.5. The method of claim 4 , wherein the base is an inorganic base or an organic base.6. The method of claim 5 , wherein the inorganic base is any one selected from the group consisting of calcium carbonate claim 5 , sodium carbonate claim 5 , potassium hydroxide claim 5 , sodium hydroxide claim 5 , cesium carbonate claim 5 , potassium tert-butoxide (t-BuOK) and lithium hydroxide.7. The method of claim 5 , wherein the organic base is any one selected from the group consisting of triethylamine claim 5 , tert-butylamine claim 5 , and diisopropylethylamine.8. The method of or claim 5 , wherein the step 1) of or the step 1) of is performed using any one solvent selected from the group consisting of ethanol claim 5 , toluene claim 5 , 1 claim 5 ,2-dimethoxyethane claim 5 , a mixture of water and ethanol claim 5 , a mixture of water and toluene claim 5 , or a mixture of water and 1 claim 5 ,2-dimethoxyethane.9. The method of claim 8 , wherein in the mixture of water and ethanol claim 8 , the mixture of water and toluene claim 8 , and the mixture of water and 1 claim 8 ,2-dimethoxyethane claim 8 , a ratio of water and ethanol claim 8 , water and toluene claim 8 , and water and 1 claim 8 ,2-dimethoxyethane is 100:1 ...

Подробнее
12-09-2013 дата публикации

4-SUBSTITUTED-3-BENZYLOXY-BICYCLO[3.1.0]HEXANE COMPOUNDS AS mGluR 2/3 ANTAGONISTS

Номер: US20130237573A1
Принадлежит: Eli Lilly and Co

A mGlu2/3 receptor antagonist of the formula: its uses, and methods for its preparation are described.

Подробнее
12-09-2013 дата публикации

Process for the synthesis of halogenated cyclic compounds

Номер: US20130237710A1
Автор: Max Braun
Принадлежит: SOLVAY SA

A process for the manufacture of a cyclic compound of formula (I) which comprises (a) adding an acid halide of formula R 1 —C (O)—X, to a vinyl ether of formula (II): CH 2 ═CH—OR 2 , to produce an addition product, and (b) reacting the addition product with a compound of formula (III): Y-A-Z; wherein R 1 is a halogenated alkyl group; wherein X is fluorine, chlorine, or bromine; wherein R 2 is an alkyl group, an aralkyl group, or an aryl group; wherein Z and Y designate independently carbon or a heteroatom; and wherein A is a linking group between Z and Y comprising 0, 1, 2 or 3 atoms in the cycle.

Подробнее
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 ...

Подробнее
19-09-2013 дата публикации

NOVEL NEUROTRYPSIN INHIBITORS

Номер: US20130245064A1
Принадлежит:

The invention relates to novel acylamino-hydroxy-benzamides of formula (I), wherein Ris phenyl substituted by phenyl, phenoxy, phenylamino or heteroaryl, all optionally further substituted; bicyclic aryl, monocyclic heteroaryl substituted by optionally substituted phenyl, or bicyclic heteroaryl, Ris hydrogen or methyl, and Rand Rhave the meanings indicated in the description. These compounds are useful for the treatment and/or prophylaxis of skeletal muscle atrophy, schizophrenia and Alzheimer's disease, and as cognitive enhancers. 2. The compound according to of formula (I) wherein{'sup': '1', 'sub': 5', '6, 'Ris optionally substituted biphenylyl, phenoxyphenyl or phenylaminophenyl, optionally substituted 1H-benzimidazol-2-yl-phenyl, optionally substituted benzo-C- or C-cycloalkyl or -cycloalkenyl, optionally substituted phenyl-thiophenyl or benzothiophenyl, optionally substituted 1H-benz[d]imidazol-2-yl, optionally substituted indolyl, optionally substituted quinolinyl, or optionally substituted phenyl-1,3-thiazol-2-yl or benzo-1,3-thiazol-2-yl;'}{'sup': '2', 'Ris hydrogen or methyl;'}{'sup': '3', 'Ris alkyl, optionally substituted benzyl, optionally substituted phenylethyl, optionally substituted phenyl; and'}{'sup': '4', 'Ris hydrogen or lower alkyl; or'}{'sup': 3', '4, 'Rand Rtogether with the nitrogen atom, to which they are bound, are optionally substituted pyrrolidino, optionally substituted piperidino, 1,2,3,4-tetrahydro-quinol-1-yl or 1,2,3,4-tetrahydro-isoquinol-2-yl, morpholino, or optionally substituted piperazino.'}3. The compound according to of formula (I) wherein{'sup': '1', 'Ris optionally substituted biphenylyl, phenoxyphenyl or phenylaminophenyl with one to three substituents, wherein the substituents are selected from the group consisting of lower alkyl, hydroxy, lower alkoxy, halo or cyano; 1H-benzimidazol-2-yl-phenyl optionally substituted at nitrogen by methyl or carboxymethyl and at the benzo residue by carboxy, chloro or dichloro; 2-indanyl ...

Подробнее
19-09-2013 дата публикации

Novel Solid Forms Of Bendamustine Hydrochloride

Номер: US20130245086A1
Принадлежит: CEPHALON, INC.

Novel solid forms of bendamustine hydrochloride are described, as well as methods of their preparation and use. 1. A solid form of bendamustine hydrochloride that is bendamustine hydrochloride Form 3 that produces an X-ray powder diffraction pattern comprising the following reflections: 15.5 , 19.7 , and 26.1±0.2 degrees 2θ.2. The bendamustine hydrochloride according to that produces an X-ray powder diffraction pattern further comprising one or more of the following reflections: 7.9 claim 1 , 10.6 claim 1 , and/or 23.3±0.2 degrees 2θ.3. The bendamustine hydrochloride according to that is substantially free of other crystalline forms of bendamustine hydrochloride.4. A composition comprising the solid form of bendamustine hydrochloride according to .5. The composition according to claim 4 , further comprising at least one pharmaceutically acceptable excipient.6. The composition according to claim 4 , wherein the composition is substantially free of other crystalline forms of bendamustine hydrochloride.7. The composition according to claim 5 , wherein the composition is substantially free of other crystalline forms of bendamustine hydrochloride.8. The composition according to claim 4 , wherein the composition further comprises amorphous bendamustine hydrochloride.9. The composition according to claim 5 , wherein the composition further comprises amorphous bendamustine hydrochloride.10. The composition according claim 4 , wherein the pharmaceutically acceptable excipient is sodium phosphate claim 4 , potassium phosphate claim 4 , citric acid claim 4 , tartaric acid claim 4 , gelatin claim 4 , glycine claim 4 , mannitol claim 4 , lactose claim 4 , sucrose claim 4 , maltose claim 4 , glycerin claim 4 , dextrose claim 4 , dextran claim 4 , trehalose claim 4 , hetastarch claim 4 , or a mixture thereof.11. The composition according to wherein the excipient is mannitol.12. The composition according to wherein the composition is a pharmaceutical composition.13. A lyophilized ...

Подробнее
19-09-2013 дата публикации

Compound having hetero ring skeleton, and process for producing optically active compound using the aforementioned compound as asymmetric catalyst

Номер: US20130245257A1
Принадлежит: KYOTO UNIVERSITY, Sumitomo Chemical Co Ltd

The invention provides a compound having a heterocyclic skeleton of formula (I): wherein the substituents are as defined in the specification, as well as a tautomer thereof or a salt thereof. The invention also provides asymmetric synthesis methods involving the use of such a compound, tautomer thereof, or salt thereof, as a catalyst.

Подробнее
19-09-2013 дата публикации

Processes for preparing benzimidazole compounds

Номер: US20130245279A1
Принадлежит: Array Biopharma Inc, AstraZeneca AB

Provided are processes for the preparation of benzimidazole structures having Formula VIIIb-1: and salts and solvates thereof, wherein Z, X 5 , R 2b , R 2c and R 10 are as defined herein. Compounds of Formula VIIIb-1 are useful for the preparation of benzimidazole derivatives.

Подробнее
10-10-2013 дата публикации

TRICYCLIC COMPOUND

Номер: US20130267711A1
Принадлежит:

The invention provides a method of activating PPAR γ and a method of treating or preventing a disease associated with PPAR γ by administering a tricyclic compound having a PPAR γ agonist activity, which is represented by the formula (I) wherein Z represents a single bond or the like, Y represents a hydrogen atom, lower alkyl optionally having substituent(s) or the like, X represents a hydrogen atom or the like, A represents aryl or the like, B and C are the same or different and each represents an aromatic carbocycle or the like, R-Rare the same or different and each represents hydrogen or the like, V represents a single bond or the like, Rand Rare the same or different and each represents hydrogen or the like, or a pharmaceutically acceptable salt thereof or the like: 3. The method of claim 2 , wherein the disease associated with PPAR γ is type 2 diabetes claim 2 , impaired glucose tolerance claim 2 , insulin resistance syndrome claim 2 , hypertension claim 2 , hyperlipidemia claim 2 , metabolic syndrome claim 2 , visceral obesity claim 2 , obesity claim 2 , hypertriglyceridemia claim 2 , or tumor.4. The method of claim 3 , wherein the subject has the disease associated with PPAR γ claim 3 , and administering the tricyclic compound claim 3 , or the pharmaceutically salt thereof claim 3 , to the subject treats the disease associated with PPAR γ in the subject.12. The method of claim 2 , wherein V is O claim 2 , NRwherein Ris as defined above claim 2 , or S.13. The method of claim 2 , wherein at least one of Rand Ris lower alkyl.17. The method of claim 10 , wherein V is O claim 10 , NRwherein Ris as defined above claim 10 , or S.22. The method of claim 10 , wherein at least one of Rand Ris lower alkyl. This patent application is a divisional of copending U.S. patent application Ser. No. 13/057,599, filed on Apr. 28, 2011, which is the U.S. national phase of International Patent Application PCT/JP2009/063957, filed on Aug. 6, 2009, which claims the benefit of Japanese ...

Подробнее
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.

Подробнее
17-10-2013 дата публикации

Chemical Compounds

Номер: US20130274243A1
Принадлежит: Pfizer Ltd

The invention relates to benzimidazole and imidazopyridine derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to new Na v 1.8 modulators of formula (I) or pharmaceutically acceptable salts thereof, wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , X and Y are as defined in the description. Na v 1.8 modulators are potentially useful in the treatment of a wide range of disorders, particularly pain.

Подробнее
17-10-2013 дата публикации

NOVEL INHIBITORS OF BACTERIAL BIOFILMS AND RELATED METHODS

Номер: US20130274256A1
Принадлежит: SEQUOIA SCIENCES, INC.

Certain multi-cyclic compounds and compositions thereof are useful for reducing or inhibiting the growth of bacterial biofilms and for controlling bacterial biofilm infections. Such compounds and compositions are also useful in methods for reducing or inhibiting the growth of biofilms and for controlling bacterial biofilm infections involving biofilms. 162-. (canceled)65. A compound according to wherein Ris selected from the group consisting of methyl claim 63 , halide claim 63 , lower haloalkyl claim 63 , nitrile claim 63 , lower alkyl nitrile claim 63 , lower alkyl claim 63 , substituted lower alkyl claim 63 , lower alkenyl claim 63 , substituted lower alkenyl claim 63 , lower alkynyl claim 63 , substituted lower alkynyl claim 63 , lower cycloalkyl claim 63 , lower cycloalkenyl claim 63 , aryl claim 63 , substituted aryl claim 63 , heteroaryl claim 63 , and substituted heteroaryl claim 63 , preferably Ris selected from the group consisting of pyrrolyl claim 63 , pyrazolyl claim 63 , imidazolyl claim 63 , oxazolyl claim 63 , isoxazolyl claim 63 , oxadiazolyl claim 63 , thiazolyl claim 63 , isothiazolyl claim 63 , thienyl claim 63 , furanyl claim 63 , furazanyl claim 63 , pyridinyl claim 63 , pyrimidinyl claim 63 , pyridazinyl claim 63 , indolyl claim 63 , 3H-indolyl claim 63 , isoindolyl claim 63 , indolinyl claim 63 , indolizinyl claim 63 , indazolyl claim 63 , dihydroindolyl claim 63 , tetrahydroindolyl claim 63 , purinyl claim 63 , pyrazinyl claim 63 , quinolinyl claim 63 , isoquinolinyl claim 63 , tetrahydroisoquinolinyl claim 63 , quinoxalinyl claim 63 , quinazolinyl claim 63 , cinnolinyl claim 63 , pteridinyl claim 63 , benzimidazolyl claim 63 , benzopyranyl claim 63 , benzoxazolyl claim 63 , benzisoxazolyl claim 63 , benzofuranyl claim 63 , isobenzofuranyl claim 63 , benzothiazolyl claim 63 , benzisothiazolyl claim 63 , benzothienyl claim 63 , furopyridinyl claim 63 , phthalazinyl claim 63 , napthyridinyl claim 63 , pyrazolopyridyl claim 63 , ...

Подробнее
17-10-2013 дата публикации

Monocyclic cyanoenones and methods of use thereof

Номер: US20130274480A1
Принадлежит: Dartmouth College

The present invention features monocyclic cyanoenone compositions and methods for using the same in the treatment of diseases such as cancer, inflammatory diseases and neurodegenerative diseases.

Подробнее
24-10-2013 дата публикации

PARASITICIDAL COMPOSITIONS COMPRISING BENZIMIDAZOLE DERIVATIVES, METHODS AND USES THEREOF

Номер: US20130281392A1
Автор: Meng Charles Q.
Принадлежит: MERIAL LIMITED

The invention relates to oral, topical or injectable compositions for combating liver fluke parasites in mammals, comprising at least one benzimidazole derivative active agent. The invention also provides for an improved method for eradicating and controlling liver fluke parasite infections and infestations in a mammal comprising administering the compositions of the invention to the mammal in need thereof. 2. A compound according to wherein Ris (C-C)-alkyl substituted with fluorine.3. A compound according to wherein Ris Cl.4. A compound according to wherein Ris a mono- or bi-halogen substituted phenyl ether.5. A compound according to wherein Ris a bi- or tri-halogen substituted phenyl.6. A compound according to or wherein the halogen is chlorine claim 1 , bromine or fluorine.7. A compound according to wherein Ris chlorine.8. A compound according to wherein Ris hydrogen.9. A compound according to that is 6-chloro-5-(4-chlorophenyl)-2-trifluoromethylbenzimidazole. (#130)10. A compound according to that is 6-chloro-5-(2 claim 1 ,3-dichlorophenoxy)-2-heptafluoropropylbenzimidazole. (#140)11. A compound according to that is 6-chloro-5-(3 claim 1 ,5-dichlorophenyl)-2-trifluoromethylbenzimidazole. (#247)12. A compound according to that is 6-chloro-5-(3 claim 1 ,4-dichlorophenyl)-2-trifluoromethylbenzimidazole. (#258)13. A compound according to that is 6-chloro-5-(2 claim 1 ,4-dichlorophenyl)-2-trifluoromethylbenzimidazole. (#260)14. A compound according to that is 6-chloro-5-(2 claim 1 ,3 claim 1 ,5-trichlorophenyl)-2-trifluoromethylbenzimidazole. (#261)15. A compound according to that is 5-chloro-6-(2 claim 1 ,4-dichlorophenoxy)-2-(heptafluoropropyl)-1H-1 claim 1 ,3-benzodiazole. (#273)16. A composition for treating helminth infestation comprising an anthelmintically effective amount of the compound of claim 1 , claim 1 , claim 1 , claim 1 , claim 1 , claim 1 , or and a pharmaceutically acceptable carrier.17. A composition for treating helminth infestation according to ...

Подробнее
31-10-2013 дата публикации

ESTERS OF BENDAMUSTINE AND RELATED COMPOUNDS, AND MEDICAL USE THEREOF

Номер: US20130289032A1
Принадлежит:

The present invention relates to particular esters of bendamustine and related compounds, and medical uses thereof. 2. The compound according to claim 1 , wherein the optional ring structure formed by Rand Rneither comprises a C—C double bond representing an integral part of the ring structure claim 1 , nor are the carbon atoms adjacent to the nitrogen located between Rand Rsubstituted with an oxygen (═O) forming a carbonyl moiety with the respective carbon atom.3. The compound according to claim 1 , wherein Ris C1-C6 alkyl claim 1 , Rand Rindependently from each other represent C1-C6 alkanediyl claim 1 , Yand Yrepresent oxygen claim 1 , and Rand Rindependently from each other represent C1-C4 alkyl claim 1 , preferably Ris C1-C4 alkyl claim 1 , Rand Rindependently from each other represent C1-C4 alkanediyl claim 1 , Yand Yrepresent oxygen claim 1 , and Rand Rindependently from each other represent C1-C4 alkyl or form a 5- to 7-membered ring structure together with the nitrogen located between Rand R.4. The compound according to claim 1 , wherein Ris C1-C3 alkyl claim 1 , Rand Rindependently from each other represent C1-C3 alkanediyl claim 1 , Yand Yrepresent oxygen claim 1 , and Rand Rare the same and represent C1-C3 alkyl or Rand Rform a 5- to 7-membered ring structure together with the nitrogen located between Rand R.5. The compound according to claim 1 , characterized by at least one of structural features i) to v):{'sub': 4', '5', '4', '5, 'i) wherein in the ring structure formed by Rand Rtogether with the nitrogen located between Rand R, one carbon atom is replaced by one nitrogen atom or one oxygen atom;'}{'sub': '6', 'ii) in a ring structure according to structural feature i), a further nitrogen atom is substituted (—NR—) or unsubstituted (—NH—);'}{'sub': 4', '5', '4', '5, 'iii) the ring structure formed by Rand Rtogether with the nitrogen located between Rand Ris in the form of a 5- or 6-membered ring;'}{'sub': 4', '5', '4', '5, 'iv) the ring structure ...

Подробнее
31-10-2013 дата публикации

INHIBITORS OF BETA-SECRETASE

Номер: US20130289050A1
Принадлежит:

The present invention relates to spirocyclic acylguanidines and their use as inhibitors of the β-secretase enzyme (BACE1) activity, pharmaceutical compositions containing the same, and methods of using the same as therapeutic agents in the treatment of neurodegenerative disorders, disorders characterized by cognitive decline, cognitive impairment, dementia and diseases characterized by production of β-amyloid aggregates. 2. A compound according to or a pharmaceutically acceptable salt thereof for use as a medicament.3. A pharmaceutical composition comprising at least one compound according to or a pharmaceutically acceptable salt thereof in admixture with a pharmaceutically acceptable adjuvant claim 1 , diluent and/or carrier.4. A compound according to or a pharmaceutically acceptable salt thereof for use in the treatment of a BACE1 mediated disorder or disease.5. A compound or a pharmaceutically acceptable salt thereof for use according to claim 4 , wherein the BACE1 mediated disorder or disease is selected from the group consisting of a neurodegenerative disorder claim 4 , cognitive decline claim 4 , cognitive impairment claim 4 , dementia claim 4 , and disease characterized by the production of β-amyloid deposits or neurofibrillary tangles.6. A compound or a pharmaceutically acceptable salt thereof for use according to claim 5 , wherein the disorder or disease is selected from the group consisting of Alzheimer's disease claim 5 , Trisomy 21 (Down Syndrome) claim 5 , Hereditary Cerebral Hemorrhage with Amyloidosis of the Dutch-type (HCHWA-D) claim 5 , senile dementia claim 5 , cerebral amyloid angiopathy claim 5 , degenerative dementia claim 5 , dementias of mixed vascular and degenerative origin claim 5 , dementia associated with Parkinson's disease claim 5 , dementia associated with progressive supranuclear palsy claim 5 , dementia associated with cortical basal degeneration claim 5 , diffuse Lewy body type of Alzheimer's disease claim 5 , dry age related ...

Подробнее
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.

Подробнее
14-11-2013 дата публикации

Capsule-type Compound, Anion Removing Agent, and Method for Removing Anion

Номер: US20130299431A1
Автор: Kondo Mitsuru

The present invention provides a capsule-type compound consisting of: a capsule-type divalent cation consisting of a capsule framework represented by the following formula (1) and a sulfate ion (SO) encapsulated in the capsule framework; and a sulfate ion (SO) as a counter ion to the capsule-type divalent cation. In the formula (1), R, R, R, R, R, R, R, R, R, R, R, R, and Reach independently represent a hydrogen atom or a methyl group; and Mand Meach independently represent Cu, Fe, Ni, Co, or Zn. 2. The capsule-type compound according to claim 1 , wherein Mand Mare the same.3. The capsule-type compound according to claim 1 , wherein Mand Mare Cu.4. The capsule-type compound according claim 1 , wherein R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , and Rare all hydrogen atoms.5. An anion removing agent comprising claim 1 , as an active component claim 1 , the capsule-type compound according .6. A method for removing an anion claim 1 , comprising a step of bringing a water-based sample containing water and at least one anion selected from the group consisting of ClO claim 1 , BF claim 1 , NO claim 1 , Br claim 1 , and I claim 1 , and the capsule-type compound according to into contact with each other to remove the anion from the water-based sample.7. The method for removing an anion according to claim 6 , wherein the water-based sample contains at least ClO. The present invention relates to a capsule-type compound, an anion removing agent, and a method for removing an anion.A perchlorate ion (ClO), a tetrafluoroborate ion (BF), a nitrate ion (NO), and a bromide ion (Br) have high solubility in water, although being harmful ions, and are therefore anions that are difficult to remove from aqueous solutions. In addition to the anions, an iodide ion (I) also has high solubility in water and is an anion that is difficult to remove from aqueous solutions.For example, it has been ...

Подробнее
14-11-2013 дата публикации

NOVEL BICYCLIC HETEROCYCLIC COMPOUND

Номер: US20130303535A1
Принадлежит:

The invention provides a compound for the treatment or prophylaxis of pathology involving SNS, specifically diseases such as neuropathic pain, nociceptive pain, dysuria, multiple sclerosis and the like. The compound is represented by formula (1) or a pharmaceutically acceptable salt thereof wherein Ris a hydrogen atom or the like, L is a single bond, —O— or the like, Ris a phenyl group or the like, X is a carbon atom or a nitrogen atom, and R, R, R, R, Rand Rare each independently a substituted or unsubstituted alkyl group or the like: 4. The method of claim 1 , wherein Ris a substituted or unsubstituted phenyl group claim 1 , or a pharmaceutically acceptable salt thereof.5. The method of claim 1 , wherein Ris a substituted or unsubstituted alkyl group having 1 to 6 carbon atoms claim 1 , a substituted or unsubstituted 3- to 8-membered cycloalkyl group claim 1 , a substituted or unsubstituted 4- to 8-membered saturated aliphatic heterocyclic group claim 1 , or a substituted or unsubstituted 5- to 10-membered unsaturated aliphatic heterocyclic group claim 1 , or a pharmaceutically acceptable salt thereof.6. The method of claim 1 , wherein Rand Rare each independently a hydrogen atom claim 1 , a substituted or unsubstituted alkyl group having 1 to 6 carbon atoms claim 1 , a haloalkyl group having 1 to 6 carbon atoms claim 1 , a substituted or unsubstituted 3- to 8-membered cycloalkyl group claim 1 , a substituted or unsubstituted 4- to 8-membered saturated aliphatic heterocyclic group claim 1 , or a substituted or unsubstituted 5- to 10-membered unsaturated aliphatic heterocyclic group claim 1 , or Rand Rare optionally bonded to form claim 1 , together with the nitrogen atom that they are bond to claim 1 , a substituted or unsubstituted 4- to 8-membered saturated nitrogen-containing aliphatic heterocycle claim 1 , or a substituted or unsubstituted 5- to 10-membered unsaturated nitrogen-containing aliphatic heterocycle (the saturated or unsaturated nitrogen-containing ...

Подробнее
14-11-2013 дата публикации

NEW COMPOUNDS

Номер: US20130303571A1
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

The present invention relates to compounds of general formula I 16. A pharmaceutical composition comprising at least one compound according to and a pharmaceutically acceptable adjuvant claim 1 , diluent or carrier.17. A method for treating pain or inflammation in a patient comprising administering to said patient a therapeutically effective amount of a compound according to or a pharmaceutically acceptable salt thereof.18. A method according to claim 17 , wherein the condition to be treated is pain. This invention relates to novel compounds, which are inhibitors of the microsomal prostaglandin Esynthase-1 (mPGES-1), pharmaceutical compositions containing them, and their use as medicaments for the treatment and/or prevention of inflammatory diseases and associated conditions.There are many acute and chronic diseases/disorders that are inflammatory in their nature including but not limited to rheumatoid diseases e.g. rheumatoid arthritis, osteoarthritis, diseases of the visceral system e.g. inflammatory bowel syndrome, autoimmune diseases, e.g. lupus erythematodes, lung diseases like asthma and COPD. Current treatment with non-steroidal anti-inflammatory drugs (NSAIDs) and Cyclooxygenase (COX)-2 inhibitors are efficacious, but show a prevalence for gastrointestinal and cardiovascular side effects. There is a high need for new treatment options showing equivalent efficacy with an improved side effect profile.NSAIDs and COX-2 inhibitors reduce inflammation and pain through inhibition of one or both isoformes of COX enzymes. The cyclooxygenase (COX) enzyme exists in two forms, one that is constitutively expressed in many cells and tissues (COX-1), and one that in most cells and tissues is induced by pro-inflammatory stimuli, such as cytokines, during an inflammatory response (COX-2). COXs metabolise arachidonic acid to the unstable intermediate prostaglandin H(PGH). PGHis further metabolized to other prostaglandins including PGE, PGF, PGD, prostacyclin and thromboxane A ...

Подробнее
14-11-2013 дата публикации

PROCESS FOR PREPARATION OF TRICLABENDAZOLE

Номер: US20130303781A1
Принадлежит: Sequent Scientific Limited

The present invention discloses a method for preparing Triclabendazole comprising condensing N-(4,5-dichloro-2-ni-trophenyl)acetamide with 2,3-dichlorophenol to obtain 4-chloro-5(2,3-dichlorophenoxy)-2-nitrophenyl acetamide and it to obtain 4-chloro-5(2,3-dichlorophenoxy)-2-nitroaniline; reducing 4-chloro-5(2,3-dichlorophenoxy)-2-nitroaniline in presence of Raney nickel to obtain 4-chloro-5-(2,3-dichlorophenoxy)benzene-1,2-diamine of; cyclising 4-chloro-5-(2,3-dichlorophenoxy)benzene-1,2-diamine in presence of carbondisulfide to obtain 6-chloro-5-(2,3-dichlorophenoxy)-1H-benzimidazole-2-thiol; methylating 6-chloro-5-(2,3-dichlorophenoxy)-1H-benzimidazole-2-thiol using a methylating agent to obtain triclabendazole methanesulfonate salt; converting triclabendazole methanesulfonate salt to hydrochloride salt of Triclabendazole and hydrolysing it to obtain Triclabendazole. 1. A process for the preparation of Triclabendazole comprising:a) condensing N-(4,5-dichloro-2-nitrophenyl)acetamide with 2,3-dichlorophenol to obtain 4-chloro-5(2,3-dichlorophenoxy)-2-nitrophenyl acetamide;b) hydrolysing 4-chloro-5(2,3-dichlorophenoxy)-2-nitrophenyl acetamide to obtain 4-chloro-5(2,3-dichlorophenoxy)-2-nitroaniline of;c) reducing 4-chloro-5(2,3-dichlorophenoxy)-2-nitroaniline in the presence of Raney nickel to obtain 4-chloro-5-(2,3-dichlorophenoxy)benzene-1,2-diamine;d) cyclising 4-chloro-5-(2,3-dichlorophenoxy)benzene-1,2-diamine in presence of carbondisulfide to obtain 6-chloro-5-(2,3-dichlorophenoxy)-1H-1-benzimidazole-2-thiol; ande) methylating 6-chloro-5-(2,3-dichlorophenoxy)-1H-benzimidazole-2-thiol using a methylating agent to obtain Triclabendazole.2. A process for the preparation of Triclabendazole according to claim 1 , wherein the condensation and hydrolysis in step a) and b) is carried out in-situ in presence of solvent selected from the group consisting of dimethylformamide (DMF) claim 1 , DMSO claim 1 , sulfolane claim 1 , N-methylpyrrolidinone and methanol at a ...

Подробнее
14-11-2013 дата публикации

PROCESS FOR PREPARATION OF ALBENDAZOLE

Номер: US20130303782A1
Принадлежит: Sequent Scientific Limited

The present invention discloses a novel, cost-effective process for preparation of a benzimidazole carbamates compound. Specifically, it relates to the process for the preparation of anti-parasite bulk drug albendazole. The process comprises a) thiocyanating 2-nitroaniline of formula VI with ammonium thiocyanated in presence of a halogen to obtain 2-nitro-4-thiocyanoaniline of formula V; b)propylating 2-nitro-4-thiocyanoaniline of formula V with propylbromide in presence of n-propanol and a base in absence of a phase transfer catalyst to obtain 4-propylthio-2-nitroaniline of formula III; C) reducing the nitro group of 4-propylthio-2-nitroaniline prepared in step b) by reacting an aqueous alkali metal sulphide or an alkaline metal sulphide to obtain 4-propylthio-o-phenylenediamine of formula II; and d)condensing 4-propylthio-o-phenylenediamine of formula II with alkali or alkaline earth metal salt of methylcyano carbamate in presence of an acid to form Albendazole of formula I. 2. A process according to claim 1 , wherein the halogen in step (a) is chlorine or bromine.3. A process according to claim 1 , wherein the alcoholic solvent in step (b) is selected from the group consisting of methanol claim 1 , ethanol and n-propanol.4. (canceled)5. A process according to claim 1 , wherein the nitro group of 4-propylthio-2-nitroaniline is reduced in the presence of Raney nickel at a hydrogen pressure of 10 kg/cmfor 4 to 6 hrs to obtain 4-propylthio-o-phenylenediamine of formula II.6. A process according to claim 1 , wherein the alkali metal salt of methylcyano carbamate is sodium methylcyano carbamate7. A process according to claim 1 , wherein the condensation of 4-propylthio-o-phenylenediamine of formula II with the alkali or alkaline earth metal salt of methylcyano carbamate is carried out in the presence of acetone and water as a solvent and in the presence of a mineral acid at a pH in the range of 4 to 4.5.8. A process according to claim 1 , wherein the reducing step ...

Подробнее
21-11-2013 дата публикации

Nitrogenated heterocyclic derivative, electron-transporting material for organic electroluminescent elements, and organic electroluminescent element using same

Номер: US20130306955A1
Принадлежит: Idemitsu Kosan Co Ltd

A specific nitrogen-containing heterocyclic compound having a urea structure, an electron transporting material containing the nitrogen-containing heterocyclic compound, and an organic electroluminescence device including a light emitting layer and an electron transporting layer between a cathode and an anode in which the electron transporting layer includes the electron transporting material or the nitrogen-containing heterocyclic derivative. An organic EL device exhibiting high emission efficiency even at low voltage and a material for organic EL devices are described.

Подробнее
21-11-2013 дата публикации

METHODS FOR THE PREPARATION OF BENDAMUSTINE

Номер: US20130310571A1
Принадлежит: Cephalon, Inc

Improved methods for the preparation and purification of bendamustine hydrochloride are described; such as method of preparing bendamustine hydrochloride comprising contacting a compound of formula HBI: with thionyl chloride 2. The method of claim 1 , wherein the organic solvent is chloroform.3. The method of claim 1 , wherein contacting step (a) is performed for 20 to 24 hours.4. The method of claim 1 , wherein the aqueous solution of hydrochloric acid is about 32% hydrochloric acid in water.5. The method of claim 1 , wherein charcoal is added to the first aqueous mixture prior to heating step (d).6. The method of claim 5 , wherein the charcoal is filtered from the first aqueous mixture prior to distilling step (e).7. The method of claim 1 , wherein distilling step (e) is performed under reduced pressure.8. The method of claim 1 , wherein heating step (h) is performed for at least one hour.9. The method of claim 1 , wherein heating step (h) is performed at least three consecutive times.10. The method of claim 1 , wherein heating step (h) is performed four consecutive times.11. The method of claim 1 , wherein each of the isolation steps is via filtration.12. The method of further comprising the following steps:(j) dissolving the second portion of bendamustine hydrochloride in an aqueous solution of hydrochloric acid to form a third aqueous mixture;(k) heating the third aqueous mixture at 85° C. to 90° C. for 4 to 5 hours;(l) distilling the third aqueous mixture at between 50° C. to 60° C. to remove up to half of the solvent to provide a fourth aqueous mixture;(m) crystallizing a third portion of bendamustine hydrochloride from the fourth aqueous mixture;(n) isolating the third portion of bendamustine hydrochloride from the fourth aqueous mixture;(o) heating the third portion of bendamustine hydrochloride in acetone to provide a fourth portion of bendamustine hydrochloride; and(p) isolating the fourth portion of bendamustine hydrochloride.13. The method of claim 12 , ...

Подробнее
28-11-2013 дата публикации

Organic Electroluminescent Element

Номер: US20130313531A1
Принадлежит: UDC Ireland Ltd

Disclosed is an organic electroluminescent element which is excellent with respect to luminous efficiency and driving voltage and rarely undergoes initial luminance drop. Specifically disclosed is an organic electroluminescent element which comprises, on a substrate, a pair of electrodes composed of an anode and a cathode and a light-emitting layer arranged between the electrodes, and additionally comprises at least one organic layer arranged between the light-emitting layer and the cathode, where in the light-emitting layer contains, for example, a compound (A-1), and the at least one layer arranged between the light-emitting layer and the cathode contains, for example, a compound (e-4).

Подробнее
28-11-2013 дата публикации

Compounds and therapeutic uses thereof

Номер: US20130317027A1
Принадлежит: Myrexis, Inc.

The invention relates to compounds, pharmaceutical compositions and methods useful for treating cancer, systemic or chronic inflammation, rheumatoid arthritis, diabetes, obesity, T-cell mediated autoimmune disease, ischemia, and other complications associated with these diseases and disorders.

Подробнее
28-11-2013 дата публикации

Process for Preparation of Intermediates of Bendamustine

Номер: US20130317234A1
Принадлежит: Biophore India Pharmaceuticals Pvt. Ltd

The present invention relates to a process for the preparation of 4-{5-{Bis-(2-hydroxyl-ethyl)-amino}-1-methyl-1H-Benzoimidazol-2yl}-butyric acid alkyl ester of formula IV, a key intermediate in the process for the preparation of Bendamustine HCl (I) 2. The process according to wherein 2-haloethanol is 2-chloroethanol and the base employed is sodium carbonate3. The process according to wherein the reaction is carried out at a temperature of 65-70° C. for 8-12 h.4. A process for the preparation of Bendamustine by the hydrolysis of compound of Formula IV claim 1 , wherein the process involvesa) addition of thionyl chloride to Formula IV at a temp of 0-5 ° C.b) raising the reaction temperature to 40-45 ° C.c) distilling the reaction mass to dryness and adding conc. HCl (3 volumes) followed by heating to 55-65 ° C. for 6-8 hd) cooling the reaction mass followed by filtering to obtain Bendamustine hydrochloride. The present invention relates to a process for the preparation of 4-{5-[Bis-(2-hydroxyl-ethyl)-amino]-1-methyl-1H-Benzoimidazol-2yl}-butyric acid ethyl ester of formula IV, a key intermediate in the process for the preparation of Bendamustine HCl (I).Bendamustine (I) acts as an alkylating agent and is used to treat chronic lymphocytic leukemia, Hodgkins disease, non-Hodgkin's lymphoma, multiple myeloma and breast cancer.Bendamustine was originally reported by Ozegowaski and Krebs in Journal fur Praktische Chemie 20, 1963, pp 178-186 and was available from 1971 to 1992 in Germany under the name Cytostasan. Since that time, it has been marketed in Germany under the tradename Ribomustin. Recently Bendamustine was approved by USFDA for the treatment of indolent b-cell non-Hodgkin's lymphoma and marketed as Treanda.Journal fur Praktische Chemie 20, 1963, pp178-186 described the synthesis of Bendamustine via the synthesis of intermediate of Formula IV by alkylation reaction of Formula III in presence of ethylene oxide.DD134727 discloses a method of preparing ...

Подробнее
05-12-2013 дата публикации

GUANIDINE COMPOUNDS, AND USE THEREOF AS BINDING PARTNERS FOR 5-HT5 RECEPTORS

Номер: US20130324537A1
Принадлежит:

The present invention relates to guanidine compounds of the general formula I 3. Guanadine compound according to or , wherein the given moieties have the following definition:W: W1;{'sub': 3', '2', '3', '2, 'claim-text': [{'sub': 1', '6', '2', '6, 'each optionally substituted C-C-alkyl or C-C-alkenyl,'}, {'sub': 2', 'A', 'A', 'A', 'A', 'A', 'A', 'A', 'A', 'A, 'sup': 1', '1', '1', '2', '3', '4', '1', '4', '1, 'O—CH—COO—R, O—R, S—R, NRR, NR—CO—Ror CO—NRR;'}], 'A: halogen, OH, CN, CF, CHF, OCF, OCHF, or'}{'sub': A', '1', '4', '3', '7, 'sup': '1', 'R: each optionally substituted C-C-alkyl, C-C-cycloalkyl, phenyl or benzyl;'}{'sub': 'A', 'sup': '2', 'claim-text': {'sub': 1', '4', '1', '4', '1', '4', '2', '1', '4', '2', '2', '2', '1', '4, 'each optionally substituted C-C-alkyl, phenyl, benzyl, phenethyl, CO—C-C-alkyl, CO-aryl, CO—O—C-C-alkyl, SO—C-C-alkyl, SO-aryl, SO-hetaryl or SO—C-C-alkylene-aryl;'}, 'R: hydrogen, or'}{'sub': A', '1', '4', '1', '4', '1', '4', '2', '1', '4', '2', '2', '2', '1', '4, 'sup': '3', 'claim-text': {'sub': A', 'A, 'sup': 2', '3, 'or the moieties Rand Rtogether form an optionally substituted 5- or 6-membered saturated or unsaturated ring, which can contain up to two identical or different heteroatoms from the group O and N;'}, 'R: each optionally substituted C-C-alkyl, phenyl, benzyl, phenethyl, CO—C-C-alkyl, CO-aryl, CO—O—C-C-alkyl, SO—C-C-alkyl, SO-aryl, SO-hetaryl, or SO—C-C-alkylene-aryl;'}{'sub': A', '1', '4, 'sup': '4', 'R: hydrogen or an optionally substituted C-C-alkyl moiety;'}B: hydrogen or as moiety A is defined;{'sub': W', '3', '3, 'sup': '1', 'claim-text': {'sub': 1', '4', '1', '6', '1', '6, 'each optionally substituted C-C-alkyl, aryl, C-C-alkylamino or C-C-dialkylamino;'}, 'R: hydrogen, F, Cl, CN, CF, O—CF, or'}in the formula Z1 the sum of a, b and c is 1, 2 or 3;{'sub': Z', 'Z', 'Z', 'Z, 'sup': 1', '2', '3', '4, 'claim-text': {'sub': 1', '6, 'hydrogen, halogen, OH, optionally substituted C-C-alkyl;'}, 'R, R, R, Rindependently of ...

Подробнее
26-12-2013 дата публикации

2H-Imidazol-4-Amine Compounds and Their Use as Bace Inhibitors

Номер: US20130345246A1
Принадлежит: AstraZeneca AB

2H-imidazol-4-amine compounds, therapeutically acceptable salts thereof, processes for preparation thereof, therapeutic uses of such compounds for treating Aβ-related pathologies such as Down's syndrome, β-amyloid angiopathy, Alzheimer's disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegeneration associated with diseases such as Alzheimer's disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration. methods of therapy, and pharmaceutical compositions containing such compounds. 2. A compound according to selected from the group consisting of:(1r,4r)-4″-Amino-5″-methyl-6′-(2-methylpropoxy)-3′H-dispiro[cyclohexane-1,2′-indene-1′,2″-imidazol]-4-ol;(1r, 1′R,4R)-4″-Amino-5″-methyl-6′-(2-methylpropoxy)-3′H-dispiro[cyclohexane-1,2′-indene-1,2″-imidazol]-4-ol;(1r,1′S,4S)-4″-Amino-5″-methyl-6′-(2-methylpropoxy)-3′H-dispiro[cyclohexane-1,2′-indene-1,2″-imidazol]-4-ol;(1r,4r)-6′-(2,2-Difluoropropoxy)-4-methoxy-5″-methyl-3′H-dispiro[cyclohexane-1,2′-indene-1,2″-imidazol]-4″-amine;(1r,4r)-4″-Amino-6′-bromo-5″-methyl-3′H-dispiro[cyclohexane-1,2′-indene-1,2″-imidazol]-4-ol;(1r,1′R,4R)-4″-Amino-6′-bromo-5″-methyl-3′H-dispiro[cyclohexane-1,2′-indene-1,2″-imidazol]-4-ol;(1r,1′S,4S)-4″-Amino-6′-bromo-5″-methyl-3′H-dispiro[cyclohexane-1,2′-indene-1,2″-imidazol]-4-ol;(1r,4r)-6′-(Cyclobutylethynyl)-4-methoxy-5″-methyl-3′H-dispiro[cyclohexane-1,2′-indene-1′,2″-imidazol]-4″-amine;(1r,1′R,4R)-6′-(Cyclobutylethynyl)-4-methoxy-5″-methyl-3′H-dispiro[cyclohexane-1,2′-indene-1,2″-imidazol]-4″-amine;(1r,1′S,4S)-6′-(Cyclobutylethynyl)-4-methoxy-5″-methyl-3′H-dispiro[cyclohexane-1,2′-indene-1,2″-imidazol]-4″-amine;(1r,4r)-4-Methoxy-5″-methyl-6′-(3-methylbut-1-yn-1-yl)-3′H-dispiro[cyclohexane-1,2′-indene-1,2″-imidazol]-4″-amine;(1r,1′R,4R)-4-Methoxy-5″-methyl-6′-(3-methylbut-1-yn-1-yl)-3′ ...

Подробнее
26-12-2013 дата публикации

Cyclohexane-1,2'-Indene-1',2"-Imidazol Compounds and Their Use as Bace Inhibitors

Номер: US20130345247A1
Принадлежит: AstraZeneca AB

Cyclohexane-1,2′-indene-1′,2″-imidazole compounds, therapeutically acceptable salts thereof, processes for preparation thereof, therapeutic uses of such compounds for treating Aβ-related pathologies such as Down's syndrome, β-amyloid angiopathy, Alzheimer's disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegeneration associated with diseases such as Alzheimer's disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration, methods of therapy using such compounds, and pharmaceutical compositions containing such compounds. 2. A compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris Calkyl.3. A compound according to claim 2 , or a pharmaceutically acceptable salt thereof claim 2 , wherein Ris methyl or ethyl.4. A compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris aryl claim 1 , heteroaryl claim 1 , Calkynyl claim 1 , halogen claim 1 , NHC(O)Ror OR claim 1 , wherein said aryl claim 1 , heteroaryl claim 1 , or Calkynyl is optionally substituted with one to three R.5. A compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Rand Rare independently hydrogen claim 1 , Ccycloalkyl or heterocyclyl wherein said Ccycloalkyl or heterocyclyl is optionally substituted with one or two substituents independently selected from Calkyl or OR.6. A compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Rand Rtogether with the carbon to which they are attached claim 1 , form a ring B claim 1 , which is a 3-6 membered cycloalkyl or heterocyclyl monocyclic ring; and wherein ring B is optionally substituted by one or two substituents independently selected from oxo claim 1 , halogen claim 1 , Calkyl or OR.7. A ...

Подробнее
26-12-2013 дата публикации

Cyclohexane-1,2'-Naphthalene-1',2"-Imidazol Compounds and Their Use as Bace

Номер: US20130345248A1
Принадлежит: AstraZeneca AB

Cyclohexane-1,2′-naphthalene-1′,2″-imidazole compounds, therapeutically acceptable salts thereof, processes for preparation thereof, therapeutic uses of such compounds for treating Aβ-related pathologies such as Down's syndrome, β-amyloid angiopathy, Alzheimer's disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegeneration associated with diseases such as Alzheimer's disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration, methods of therapy using such compounds, and pharmaceutical compositions containing such compounds. 2. A compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris Calkyl.3. A compound according to claim 2 , or a pharmaceutically acceptable salt thereof claim 2 , wherein Ris methyl or ethyl.4. A compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris aryl claim 1 , heteroaryl claim 1 , Calkynyl claim 1 , halogen claim 1 , NHC(O)Ror OR claim 1 , wherein said aryl claim 1 , heteroaryl claim 1 , or Calkynyl is optionally substituted with one to three R.5. A compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Rand Rare independently hydrogen claim 1 , Ccycloalkyl or heterocyclyl wherein said Ccycloalkyl or heterocyclyl is optionally substituted with one or two substituents independently selected from Calkyl or OR.6. A compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Rand Rtogether with the carbon to which they are attached claim 1 , form a ring B claim 1 , which is a 3-14 membered cycloalkyl or heterocyclyl monocyclic ring; and wherein ring B is optionally substituted by one or two substituents independently selected from oxo claim 1 , halogen claim 1 , Calkyl or OR ...

Подробнее
26-12-2013 дата публикации

BENZIMIDAZOLE INHIBITION OF BIOFILM FORMATION

Номер: US20130345261A1
Принадлежит:

The various embodiments relate to a compound comprising: 2. A composition comprising a compound of and a carrier.5. The method of claim 4 , wherein the compound or a combination thereof is administered topically or locally.6. The method of claim 4 , wherein the compound or a combination thereof is administered to the site of an infection.7. The method of claim 4 , wherein the pathogen is a gram negative bacterium.8. The method of claim 4 , wherein the pathogen is a gram positive bacteria.9. The method of claim 4 , wherein the pathogen is a drug-resistant pathogen.10Vibrio cholerae, P. aeruginosa, Klebsiella pneumoniae, Erwinia amylovora, Shigella boydii, Staphylococcus aureus. The method of claim 4 , wherein the pathogen is selected from and combinations thereof.11. The method of claim 4 , wherein the infection by a pathogen is related claim 4 , or leads claim 4 , to endocarditis claim 4 , otitis media claim 4 , chronic prostatitis claim 4 , periodontal disease claim 4 , chronic urinary tract infection claim 4 , cystic fibrosis claim 4 , an infection on an indwelling medical device claim 4 , or a chronic non-healing wound.12. The method of claim 4 , wherein a therapeutically effective amount is administered.13. The method of claim 12 , wherein a therapeutically effective amount is an amount effective to inhibit biofilm formation by the pathogen.14. A method of inhibiting biofilm formation in biofilm-forming pathogens comprising contacting the pathogen with the compound of to thereby inhibit biofilm formation of the pathogen.15. The method of claim 14 , wherein contacting comprises administering or applying the compound to a surface suspected of containing the pathogen. This application claims the benefit under 35 U.S.C. 119 (e) of U.S. Provisional Application Ser. No. 61/444,531 filed on Feb. 18, 2011, hereby incorporated by reference in its entirety.This invention was made with support of the United States Government under National Institute of Health Contract No. ...

Подробнее
26-12-2013 дата публикации

Cycloalkyl Ether Compounds and Their Use as Bace Inhibitors

Номер: US20130345272A1
Принадлежит: AstraZeneca AB

Cycloalkyl ether compounds, therapeutically acceptable salts thereof, processes for preparation thereof, therapeutic uses of such compounds for treating Aβ-related pathologies such as Down's syndrome, β-amyloid angiopathy, Alzheimer's disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegeneration associated with diseases such as Alzheimer's disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration and pharmaceutical compositions containing such compounds. 2. A compound according to selected from the group consisting of:(1r,4r)-4-Methoxy-5″-methyl-6′-[(1-methylcyclopropyl)methoxy]-3′H-dispiro[cyclohexane-1,2′-indene-1,2″-imidazol]-4″-amine;(1r,4r)-6′-[(3,3-Difluorocyclobutyl)methoxy]-4-methoxy-5″-methyl-3′H-dispiro[cyclohexane-1,2′-indene-1′,2″-imidazol]-4″-amine;(1r,4r)-6′-(Cyclopropylmethoxy)-4-methoxy-5″-methyl-3′H-dispiro[cyclohexane-1,2′-indene-1,2″-imidazol]-4″-amine;(1r, 1′R,4R)-6′-(Cyclopropylmethoxy)-4-methoxy-5″-methyl-3′H-dispiro[cyclohexane-1,2′-indene-1,2″-imidazol]-4″-amine;(1r, 1′S,4S)-6′-(Cyclopropylmethoxy)-4-methoxy-5″-methyl-3′H-dispiro[cyclohexane-1,2′-indene-1,2″-imidazol]-4″-amine;(1r,4r)-6′-[(2,2-Difluorocyclopropyl)methoxy]-4-methoxy-5″-methyl-3′H-dispiro[cyclohexane-1,2′-indene-1′,2″-imidazol]-4″-amine;(1r,4r)-6′-(Cyclobutylmethoxy)-4-methoxy-5″-methyl-3′H-dispiro[cyclohexane-1,2′-indene-1,2″-imidazol]-4″-amine;(1 r, 1′R,4R)-6′-(Cyclobutylmethoxy)-4-methoxy-5″-methyl-3′H-dispiro[cyclohexane-1,2′-indene-1,2″-imidazol]-4″-amine;(1r, 1′S,4S)-6′-(Cyclobutylmethoxy)-4-methoxy-5″-methyl-3′H-dispiro[cyclohexane-1,2′-indene-1,2″-imidazol]-4″-amine, and(1r,4r)-6′-(2-Cyclopropylethoxy)-4-methoxy-5″-methyl-3′H-dispiro[cyclohexane-1,2′-indene-1,2″-imidazol]-4″-amine,or a pharmaceutically acceptable salt of any foregoing compound.3. A ...

Подробнее
26-12-2013 дата публикации

method for preparing 2-(N-substituted)-amino-benzimidazole derivatives

Номер: US20130345436A1
Принадлежит: ABA Chemicals Corp

A method for preparing 2-(N-substituted)-amino-benzimidazole derivatives is provided, which comprises the following steps: (1) reacting a compound of 2-(N-protecting group)-O-aryl diamine with a compound of N-phenoxycarbonyl monosubstituted amine to obtain a compound of 2-(N-protecting group)-amino aryl urea; (2) in a suitable organic solvent, performing dehydrating cyclization reaction of the compound of 2-(N-protecting group)-amino aryl urea in the presence of an organic base and dichloro triphenylphosphine prepared by triphenylphosphine oxide with oxalyl chloride or diphosgene or triphosgene, or dibromo triphenylphosphine prepared by triphenylphosphine oxide with bromine, to produce a compound of 1-protecting group-2-(N-substituted)-amino-benzimidazole; (3) deprotecting the resulting compound of 1-protecting group-2-(N-substituted)-amino-benzimidazole to obtain the compound 2-(N-substituted)-amino-benzimidazole.

Подробнее
02-01-2014 дата публикации

Wnt pathway antagonists

Номер: US20140005164A1
Принадлежит: Siena Biotech SpA

The present invention relates to novel compounds of formula (I): as herein described and pharmaceutical compositions thereof. The compounds of formula (I) have inhibitory effect on the Wnt pathway and are therefore useful in the preparation of a medicament, in particular for the treatment of cancer.

Подробнее
02-01-2014 дата публикации

Benzimidazole derivatives: preparation and pharmaceutical applications

Номер: US20140005194A1
Принадлежит: Mei Pharma Inc

The present invention relates to hydroxamate compounds which are inhibitors of histone deacetylase. More particularly, the present invention relates to benzimidazole containing compounds and methods for their preparation. These compounds may be useful as medicaments for the treatment of proliferative disorders as well as other diseases involving, relating to or associated with dysregulation of histone deacetylase (HDAC).

Подробнее
02-01-2014 дата публикации

RING-FUSED COMPOUND

Номер: US20140005221A1
Принадлежит: SATO PHARMACEUTICAL CO., LTD.

The present invention relates to a compound that has URAT1 inhibitory action, and a URAT1 inhibitor, a blood uric acid level-reducing agent and a pharmaceutical composition comprising the compound. More specifically, the present invention relates to a compound represented by Formula (I) below. 3. The compound according to claim 2 , wherein{'sup': 3', '4', '5, 'W, Wand Ware each independently a nitrogen atom, or a methine group that may have a substituent selected from the group consisting of a halogen atom and a lower alkyl group, or a pharmaceutically acceptable salt or ester of the compound.'}4. The compound according to claim 3 , wherein{'sup': 'X', 'X is a single bond, an oxygen atom, a carbonyl group, a vinylene group or a group represented by the general formula: —N(R)—, or a pharmaceutically acceptable salt or ester of the compound.'}5. The compound according to claim 4 , wherein{'sup': 1', '1', '1, 'Ris a group represented by a general formula -Q-A, or a pharmaceutically acceptable salt or ester of the compound.'}6. The compound according to claim 5 , wherein{'sup': '1', 'Qis a single bond or a lower alkylene group that may be substituted with a lower alkyl group, or a pharmaceutically acceptable salt or ester of the compound.'}7. The compound according to claim 6 , wherein{'sup': Yi', 'Yi′', 'Y1', 'Y1′', 'Y1', 'Y1′', 'Y1', 'Y1′', 'Y2', 'Y2′', 'Y1', 'Y1′', 'Y2', 'Y2′', 'Y3', 'Y3′', 'Y1', 'Y1′', 'Y2', 'Y2′', 'Y3', 'Y3′', 'Y4', 'Y4′', 'Y1', 'Y1′', 'Y2', 'Y2′', 'Y3', 'Y3′', 'Y4', 'Y4′', 'Y5', 'Y5′', 'Y1', 'Y′', 'Y2', 'Y2′', 'Y3', 'Y3′', 'Y4', 'Y4′', 'Y5', 'Y5′', 'Y6', 'Y6′', 'Y1', 'Y1′', 'Y2', 'Y2′', 'Y3', 'Y3′', 'Y4', 'Y4′', 'Y5', 'Y5′', 'Y6', 'Y6′, 'sub': n', 'n, 'Y is a single bond or (CRR)(herein n is any integer of 1 to 6, i is any integer of 1 to n, and (CRR)represents (CRR) when n=1; represents (CRR)—(CRR) when n=2; represents (CRR)—(CRR)—(CRR) when n=3; represents (CRR)—(CRR)—(CRR)—(CRR) when n=4; represents (CRR)—(CRR)—(CRR)—(CRR)—(CRR) when n=5; and ...

Подробнее
02-01-2014 дата публикации

COMPOUNDS AND COMPOSITIONS FOR USE AS MODULATORS OF TAU AGGREGATION AND ALLEVIATION OF TAUOPATHIES

Номер: US20140005240A1
Принадлежит:

This invention relates to the use of bis- and tris-dihydroxyaryl compounds as well as sulfonamides, heteroaryls, tricycloalkyl and their analogs and pharmaceutically acceptable salts, for modulating tau aggregation and alleviating tauopathies, such as Alzheimer's disease (AD), Pick's disease (PiD), progressive supranuclear palsy (PSP), corticobasal degeneration (CBD) and familial frontotemporal dementia/Parkinsonism linked to chromosome 17 (FTDP-17), amyotrophic lateral sclerosis/Parkinsonism-dementia complex, argyrophilic grain dementia, dementia pugilistic, diffuse neurofibrillary tangles with calcification, progressive subcortical gliosis and tangle only dementia. 2. The method of claim 1 , wherein the mammal is a human.3. The method of claim 1 , wherein the amount of the compound administered is between 0.1 mg/Kg/day and 1000 mg/Kg/day.4. The method of claim 1 , wherein the amount of compound administered is between 1 mg/Kg/day and 100 mg/Kg/day.5. The method of claim 1 , wherein the amount of compound administered is between 10 mg/Kg/day and 100 mg/Kg/day.6. The method of claim 1 , wherein the tauopathy is selected from the group consisting of Alzheimer's disease claim 1 , Pick's disease claim 1 , progressive supranuclear palsy claim 1 , corticobasal degeneration claim 1 , familial frontotemporal dementia/Parkinsonism linked to chromosome 17 claim 1 , amyotrophic lateral sclerosis/Parkinsonism-dementia complex claim 1 , argyrophilic grain dementia claim 1 , dementia pugilistic claim 1 , diffuse neurofibrillary tangles with calcification claim 1 , progressive subcortical gliosis and tangle only dementia.7. The method of wherein the compound administered is administered by one of routes selected from claim 1 , oral claim 1 , topical claim 1 , systemic or parenteral.8. A method of disrupting or causing the dissolution of tau aggregates in a mammal suffering from a tauopathy claim 1 , comprising administering to the mammal suffering from a tauopathy an effective ...

Подробнее
16-01-2014 дата публикации

Hedgehog antagonists having zinc binding moieties

Номер: US20140018368A1
Принадлежит: Curis Inc, Genentech Inc

The present invention provides compounds which antagonize hedgehog signaling and inhibit HDAC activity. The compounds can be used in methods of treating proliferative diseases and disorders such as cancer.

Подробнее
16-01-2014 дата публикации

Benzimidazole Derivatives As PI3 Kinase Inhibitors

Номер: US20140018534A1
Принадлежит: GlaxoSmithKline LLC

This invention relates to the use of benzimidazole derivatives for the modulation, notably the inhibition of the activity or function of the phosphoinositide 3′ OH kinase family (hereinafter PI3 kinases), suitably, PI3Kβ, PI3Kδ, PI3Kβ, and/or PI3Kγ. Suitably, the present invention relates to the use of benzimidazoles in the treatment of one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries. More suitably, the present invention relates to PI3Kβ selective benzimidazoles compounds for treating cancer. 1. A process for the production of the compound of formulacomprising the step ofadding iron powder to a solution of methyl 3-amino-5-(4-morpholinyl)-2-nitrobenzoate in HOAc. This application is filed as a continuation application of U.S. Ser. No. 13/876,853 filed on Mar. 29, 2013, which is filed pursuant to 35 USC 371 as a United States National Phase Application of International Patent Application Serial No. PCT/US2011/052857 filed on Sep. 23, 2011, which claims priority from 61/390,314 filed on Oct. 6, 2010 and 61/528,397 filed on Aug. 29, 2011 in the United States.This invention relates to the use of benzimidazole derivatives for the modulation, notably the inhibition of the activity or function of the phosphoinositide 3′ OH kinase family (hereinafter PI3 kinases), suitably, PI3Kα, PI3Kδ, PI3Kβ, and/or PI3Kγ. Suitably, the present invention relates to the use of benzimidazoles in the treatment of one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries. More ...

Подробнее
23-01-2014 дата публикации

Methods of Treating Neuropathic Pain with Benzimidazole Derivative Agonists of PPARgamma

Номер: US20140024692A1
Принадлежит: Aestus Therapeutics, Inc.

Embodiments of the invention relate to the treatment of neuropathic pain in mammals. Embodiments of the invention include methods for treating neuropathic pain with benzimidazole derivatives with PPARgamma agonist activity, as well as methods for preparing medicaments used in such treatments of mammalian pain. 2. The method of treating neuropathic pain of claim 1 , wherein the mammal is a human.3. The method of treating neuropathic pain of claim 2 , wherein the agonist of PPARγ is 3-(2 claim 2 ,4-dichlorobenzyl)-2-methyl-N-(pentylsulfonyl)-3H-benzimidazole-5-carboxamide or a pharmaceutically acceptable salt thereof.5. The method of treating neuropathic pain of claim 4 , wherein{'sub': '27', 'Rrepresents an aryllower alkyl group whose aryl moiety may be substituted by one or two substituents selected from the group consisting of a halogen atom, a lower alkyl group, a halo-lower alkyl group, a cyanoaryl group, an amino group, a lower alkoxy group, a nitro group, a cyano group, an aryl group, a haloaryl group, an arylsulfonyl-lower alkyl group, an arylsulfonylamino group, an aryl-lower alkyloxy group, an aryl-lower alkyl group, a heterocyclic group, an arylcarbonyl group, an arylcarbonylamino group, and an aryl-lower alkyloxy group substituted by one or two halogen atoms;'}Y represents a carbonyl group; andA represents a single bond.6. The method of treating neuropathic pain of claim 5 , wherein{'sub': '27', 'Rrepresents an aryl lower alkyl group whose aryl moiety may be substituted by one or two substituents selected from a halogen atom or an aryl group;'}{'sub': '28', 'Rrepresents a lower alkyl group or a lower cycloalkyl group;'}{'sub': '25', 'Rrepresents an alkyl group having up to 8 carbon atoms or an aryl group;'}Y represents a carbonyl group; andA represents a single bond.7. The method of treating neuropathic pain of claim 2 , wherein the agonist of PPARγ is selected from the group consisting of 6-benzenesulfonylcarbamoyl-1-(2-chlorobenzyl)-2-methylbenzimidazole ...

Подробнее
30-01-2014 дата публикации

Solid Forms of Curcumin

Номер: US20140031403A1
Принадлежит:

The present invention provides forms of curcumin and the pharmaceutical compositions thereof. The forms of curcumin disclosed herein are curcumin polymorph Form III, curcumin-2-aminobenzimidazole co-crystal, and curcumin-L-lysine co-crystal. Further, the invention provides methods inhibiting cancer cells and HSV-1 using these curcumin novel solid forms. 1. A co-crystal form of curcumin , wherein the co-crystal form is curcumin-2-aminobenzimidazole.2. The co-crystal form of claim 1 , wherein curcumin-2-aminobenzimidazole exhibits an X-ray powder diffraction pattern having characteristic peaks expressed in degrees-2-theta at about 6.2 claim 1 , about 9.0 claim 1 , about 12.3 claim 1 , about 14.5 claim 1 , about 17.3 claim 1 , about 18.0 claim 1 , about 19.0 claim 1 , about 20.0 claim 1 , about 21.2 claim 1 , about 24.5 claim 1 , about 25.05 claim 1 , and about 27.1 claim 1 , and further exhibits an endothermic transition with an onset of about 118.1° C. as measured by differential scanning calorimetry.3. (canceled)4. (canceled)5. (canceled)6. (canceled)7. (canceled)8. A co-crystal form of curcumin claim 1 , wherein the co-crystal form is curcumin-L-lysine.9. The co-crystal form of claim 8 , wherein curcumin-L-lysine is an amorphous form of curcumin co-crystal; and exhibits a first exotherm at onset 36.7° C. with peak 43.6° C. claim 8 , a second exotherm at onset 93.7° C. with peak 97.8° C. claim 8 , and an endotherm at onset 135.5° C. with peak 136.0° C.10. (canceled)11. (canceled)12. (canceled)13. (canceled)14. (canceled)15. A polymorph form of curcumin claim 8 , wherein the polymorph form is Form III.16. The polymorph form of claim 15 , wherein Form III exhibits X-ray powder diffraction pattern having characteristic peaks expressed in degrees 2-theta at about 9.56 claim 15 , about 14.51 claim 15 , about 17.90 claim 15 , and about 26.86 claim 15 , and exhibits an endothermic transition with an onset of about 162.6° C. as measured by differential scanning calorimetry. ...

Подробнее