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Небесная энциклопедия

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

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Мониторинг СМИ

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

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Поддерживает ввод нескольких поисковых фраз (по одной на строку). При поиске обеспечивает поддержку морфологии русского и английского языка
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Применить Всего найдено 41029. Отображено 100.
05-01-2012 дата публикации

Inhibitors of the 11-beta-hydroxysteroid dehydrogenase type 1 enzyme

Номер: US20120004206A1

The present invention relates to compounds which are inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme. The present invention further relates to the use of inhibitors of 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme for the treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome, and other diseases and conditions that are mediated by excessive glucocorticoid action.

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05-01-2012 дата публикации

NOVEL PIPERAZINE DERIVATIVES AS INHIBITORS OF STEAROYL-CoA DESATURASE

Номер: US20120004213A1
Принадлежит: Forest Laboratories Holdings Ltd

The present invention relates to piperazine derivatives that act as inhibitors of stearoyl-CoA desaturase. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and to methods of treatment using the compounds.

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05-01-2012 дата публикации

Modulators of atp-binding cassette transporters

Номер: US20120004216A1
Принадлежит: Vertex Pharmaceuticals Inc

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

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26-01-2012 дата публикации

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

Номер: US20120022076A1
Принадлежит: Individual

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

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09-02-2012 дата публикации

Modulators of Cellular Adhesion

Номер: US20120035154A1
Принадлежит: Sarcode Bioscience Inc

The present invention provides compounds having formula (I): and pharmaceutically acceptable derivatives thereof, wherein R 1 -R 4 , n, p, A, B, D, E, L and AR 1 are as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of disorders mediated by the CD11/CD18 family of cellular adhesion molecules (e.g., LFA-1).

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16-02-2012 дата публикации

Design, synthesis and evaluation of procaspase activating compounds as personalized anti-cancer drugs

Номер: US20120040995A1
Принадлежит: University of Illinois

Compositions and methods are disclosed in embodiments relating to induction of cell death such as in cancer cells. Compounds and related methods for synthesis and use thereof, including the use of compounds in therapy for the treatment of cancer and selective induction of apoptosis in cells are disclosed. Compounds are disclosed that have lower neurotoxicity effects than other compounds.

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23-02-2012 дата публикации

Diacylethylenediamine compound

Номер: US20120046292A1
Принадлежит: Astellas Pharma Inc

[Problem] A compound which is useful as an anti-obesity agent is provided. [Means for Solution] The present inventors have investigated a compound having a DGAT1 inhibitory action, which is promising as an active ingredient of a pharmaceutical composition for treating obesity, type II diabetes mellitus, fatty liver, and diseases associated with these diseases, and as a result, they have found that the diacylethylenediamine compound of the present invention has an excellent DGAT1 inhibitory action, thereby completing the present invention. That is, the diacylethylenediamine compound of the present invention has a DGAT1 inhibitory action, and can be therefore used as an agent for preventing and/or treating obesity, type II diabetes mellitus, fatty liver, and diseases associated with these diseases.

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08-03-2012 дата публикации

Neuroprotective iron chelators and pharmaceutical compositions comprising them

Номер: US20120058945A1

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

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22-03-2012 дата публикации

Metallo-beta-lactamase inhibitors

Номер: US20120071457A1
Принадлежит: Individual

A new metallo-β-lactamase inhibitor which acts as a medicament for inhibiting the inactivation of β-lactam antibiotics and recovering anti-bacterial activities is disclosed. The maleic acid derivatives having the general formula (I) have metallo-β-lactamase inhibiting activities. It is possible to recover the anti-bacterial activities of β-lactam antibiotics against metallo-β-lactamase producing bacteria by combining the compound of the general formula (I) with β-lactam antibiotics.

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05-04-2012 дата публикации

Ionic liquids, the method for preparing the same and method for removing acetylenes from olefin mixtures using the ionic liquids

Номер: US20120083642A1

There are provided an ionic liquid having ether group(s) in which a copper(I) compound is included, a method for preparing the same, and a method for removing traces amounts of acetylene-based hydrocarbon compounds included in olefin by absorption or extraction using the same. When the disclosed solution is used, oxidation of Cu(I) to Cu(II) is prevented since CuX is stabilized by the ionic liquid. Thus, selective removal efficiency of acetylenic compounds is improved greatly while the removal performance is retained for a long period of time. Further, since the solution according to the present disclosure is applicable as an extractant as well as an absorbent, the associated operation is simple and apparatus cost can be decreased.

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12-04-2012 дата публикации

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

Номер: US20120088746A1
Принадлежит: PFIZER INC

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

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19-04-2012 дата публикации

Organic Compounds Having Cooling Properties

Номер: US20120095042A1
Автор: Stefan Michael Furrer
Принадлежит: Givaudan SA

Provided are compounds of formula (I) wherein m is 0, 1 or 2; R I is a mono- or bicyclic heterocyclic ring system including one, two or three heteroatoms selected from nitrogen, sulphur and oxygen; R 2 is selected from hydrogen, methyl and ethyl; I) R 3 is hydrogen, methyl, or ethyl; and R 4 and R 5 are independently selected from ethyl and isopropyl; and R 3 , R 4 and R 5 together have at least 6 carbon atoms: or II) any two or all of R 3 , R 4 and R 5 form together with the carbon atom to which they are attached 3-para-menthyl, bornyl, or adamantyl; having cooling properties, their use as cooling agent and compositions including them.

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26-04-2012 дата публикации

Methylphenidate Derivatives and Uses of Them

Номер: US20120101129A1
Принадлежит: David Bar-Or, Rao Nagaraja R K

The present invention provides methods of using compounds of formula I: and salts and prodrugs thereof, wherein n, R 1 and R 2 are defined herein. The invention also provides certain novel compounds of formula I and pharmaceutical compositions comprising them.

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03-05-2012 дата публикации

Disubstituted-aminodifluorosulfinium salts, process for preparing same and method of use as deoxofluorination reagents

Номер: US20120108801A1
Принадлежит: OMEGACHEM INC

The invention relates to disubstituted-aminodifluorosulfinium salts represented by the formula (I). Processes for preparing same and methods of use as deoxofluorinating reagent is also provided.

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03-05-2012 дата публикации

Process for preparing 1,4-bishydroxyethylpiperazine

Номер: US20120108816A1
Принадлежит: BASF SE

Process for preparing 1,4-bishydroxyethylpiperazine (BHEPIP) of the formula I wherein diethanolamine (DEOA) of the formula II is reacted in the liquid phase in a reactor at a temperature in the range from 130 to 300° C. in the presence of a copper-comprising, chromium-free heterogeneous catalyst.

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10-05-2012 дата публикации

Compound inhibiting in vivo phosphorus transport and medicine containing the same

Номер: US20120115851A1
Принадлежит: Kyowa Hakko Kirin Co Ltd

An objective of the present invention is to provide compounds that can effectively suppress the concentration of phosphorus in serum to effectively prevent or treat diseases induced by an increase in concentration of phosphate in serum. The compounds according to the present invention are compounds represented by formula (I) and pharmaceutically acceptable salts and solvates thereof: wherein A represents an optionally substituted five- to nine-membered unsaturated carbocyclic moiety or a five- to nine-membered unsaturated heterocyclic moiety, and represents a single bond or a double bond, R 5 represents optionally substituted aryl or the like, Z represents —N═CHR 6 R 7 or the like, R 6 and R 7 represent H, optionally substituted alkyl, optionally substituted aryl or the like, R 101 and R 102 together form ═O, and R 103 and R 104 represent H, or R 101 and R 104 together from a bond, and R 102 and R 103 together form a bond.

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10-05-2012 дата публикации

N,n'-diarylurea compounds and n,n'-diarylthiourea compounds as inhibitors of translation initiation

Номер: US20120115915A1
Принадлежит: Harvard College

Compositions and methods for inhibiting translation initiation are provided. Compositions, methods and kits for treating (1) cellular proliferative disorders, (2) non-proliferative, degenerative disorders, (3) viral infections, and/or (4) disorders associated with viral infections, using N,N′-diarylureas and/or N,N′-diarylthiourea compounds are described.

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17-05-2012 дата публикации

Compounds and compositions comprising cdk inhibitors and methods for treating cancer

Номер: US20120121692A1

Disclosed herein are compounds suitable for use as antitumor agents, methods for treating cancer wherein the disclosed compounds are used in making a medicament for the treatment of cancer, methods for treating a tumor comprising, administering to a subject a composition comprising one or more of the disclosed cytotoxic agents, and methods for preparing the disclosed antitumor agents.

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17-05-2012 дата публикации

Phenoxy substituted phenylamidine derivatives and their use as fungicides

Номер: US20120122678A1
Принадлежит: Bayer CropScience AG

The present invention relates to 3-substituted phenylamidines of the general formula (I), to a process for their preparation, to the use of the amidines according to the invention for controlling unwanted microorganisms and also to a composition for this purpose, comprising the phenoxyamidines according to the invention. Furthermore, the invention relates to a method for controlling unwanted microorganisms by applying the compounds according to the invention to the microorganisms and/or their habitat.

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17-05-2012 дата публикации

Substituted carbamoylcycloalkyl acetic acid derivatives as nep

Номер: US20120122764A1
Принадлежит: NOVARTIS AG

The present invention provides a compound of formula I; or a pharmaceutically acceptable salt thereof, wherein R 1 , R 2 , R 3 , R 4 , R 5 , B, X, m and n are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides pharmaceutical composition of compounds of the invention, and a combination of pharmacologically active agents and a compound of the invention.

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24-05-2012 дата публикации

Lipid compositions

Номер: US20120128760A1
Принадлежит: Alnylam Pharmaceuticals Inc

Disclosed herein are lipid compositions comprising a cationic lipid of formula (I), a neutral lipid, a sterol and a PEG or PEG-modified lipid, wherein formula (I) is (F). Also disclosed are methods of producing the cationic lipid of formula (I).

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24-05-2012 дата публикации

Derivatives of Fluorene, Anthracene, Xanthene, Dibenzosuberone and Acridine and Uses Thereof

Номер: US20120129837A1
Принадлежит: Clinical Data Inc

Chemical agents, such as disulfonamide derivatives of fluorene, anthracene, xanthene, dibenzosuberone and acridine, and similar heterocyclic ring structures, including salts thereof, that act as anti-cancer and anti-tumor agents, especially where such agents modulate the activity of the Wnt/β-catenin signaling pathway, and serve to reduce β-catenin levels present in cells, such as cancer cells, or where the agents modulate levels of gene expression in cellular systems, including cancer cells, are disclosed, along with methods for preparing such agents, as well as pharmaceutical compositions containing such agents as active ingredients and methods of using these as therapeutic agents.

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24-05-2012 дата публикации

Piperazinyl derivatives useful as modulators of the neuropeptide y2 receptor

Номер: US20120129870A1
Принадлежит: Janssen Pharmaceutica NV

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

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07-06-2012 дата публикации

N-phenyl-(homo)piperazinyl-benzenesulfonyl or benzenesulfonamide compounds suitable for treating disorders that respond to the modulation of the serotonin 5-ht6 receptor

Номер: US20120142674A1
Принадлежит: Abbott GmbH and Co KG, ABBOTT LABORATORIES

The present invention relates to N-Phenyl-(homo)piperazinyl-benzenesulfonyl or benzenesulfonamide compounds of formula I wherein the variables have the meanings given in the claims and the description, pharmaceutical compositions containing them, and their use in therapy. The compounds possess valuable therapeutic properties and are particularly suitable for treating diseases that respond to modulation of the serotonin 5-HT 6 receptor.

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21-06-2012 дата публикации

Phosphorous derivatives as chemokine receptor modulators

Номер: US20120157413A1
Принадлежит: Allergan Inc

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

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12-07-2012 дата публикации

Polymerizable composition, color filter, and method of producing the same, solid-state imaging device, and planographic printing plate precursor, and novel compound

Номер: US20120176571A1
Автор: Masaomi Makino
Принадлежит: Fujifilm Corp

Disclosed is a photopolymerizable composition which contains a photopolymerization initiator (A) that has a partial structure represented by the following Formula (1) and a polymerizable compound (B). In General formula (1), R 3 and R 4 each independently represents a hydrogen atom, an alkyl group, an alkenyl group, an alkynyl group, an aryl group, a heteroaryl group or an alkoxy group; R 3 and R 4 may form a ring with each other; and X represents OR 5 , SR 6 , or NR 17 R 18 . The photopolymerizable composition is capable of forming a cured film that has high sensitivity, excellent intra-membrane curability and excellent adhesion to a support. The cured film is able to maintain a patterned shape even during post-heating after development and has good pattern formability, while coloring due to heating with passage of time being suppressed.

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26-07-2012 дата публикации

Michael addition reaction product and active energy ray-curable composition

Номер: US20120190846A1
Принадлежит: DIC Corp

The present invention provides a Michael addition reaction product between a specified compound having a group which functions as a Michael donor and a monomer or polymer having a group which functions as a Michael acceptor, a photoinitiator containing the Michael addition reaction product, and an active energy ray-curable composition containing the photoinitiator. The compound having a group functioning as a Michael donor used in the present invention is a phenyl ketone derivative and is characterized by having an amino group or a mercapto group as the group functioning as a Michael donor.

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02-08-2012 дата публикации

Glycine transporter-1 inhibitors

Номер: US20120195985A1
Принадлежит: AMGEN INC

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

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09-08-2012 дата публикации

Substituted 4-aminocyclohexane derivatives

Номер: US20120202810A1
Принадлежит: GRUENENTHAL GmbH

The invention relates to compounds that have an affinity to the μ-opioid receptor and the ORL 1-receptor, methods for their production, medications containing these compounds and the use of these compounds for the treatment of pain and other conditions.

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23-08-2012 дата публикации

New compounds, pharmaceutical compositions and uses thereof

Номер: US20120214785A1
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

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

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30-08-2012 дата публикации

Guanidine-containing compounds useful as muscarinic receptor antagonists

Номер: US20120219509A1
Принадлежит: Theravance Inc

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

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30-08-2012 дата публикации

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

Номер: US20120220592A1
Принадлежит: Newron Pharmaceuticals SpA

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

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06-09-2012 дата публикации

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

Номер: US20120225890A1
Принадлежит: ProteoTech Inc

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

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13-09-2012 дата публикации

Methods of treating emesis using growth hormone secretagogues

Номер: US20120232113A1
Принадлежит: Helsinn Therapeutics Us Inc

The present invention relates to methods of treating or preventing emesis and improving a subject's ASAS score by administering to the subject an effective amount of a growth hormone secretagogue compound or a pharmaceutically acceptable salt, hydrate or solvate thereof.

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20-09-2012 дата публикации

Sphingosine kinase type 1 inhibitors, and processes for using same

Номер: US20120237448A9

Provided are novel compositions and analogs which are useful in a number of applications, indications and diseases, as well as for monitoring pharmakinetics and patient management. These compounds and analogs are applicable to treating tumors of the central nervous system, e.g., glioblastoma (GBM).

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11-10-2012 дата публикации

Novel ligands that modulate rar receptors

Номер: US20120258996A1
Принадлежит: Galderma Research and Development SNC

Novel ligand compounds having the general formula (I): and pharmaceutical/cosmetic compositions comprised thereof are useful in human and veterinary medicine or, alternatively, in cosmetics.

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18-10-2012 дата публикации

Salt forms of [R-(R*,R*)]-2-(4-flurorophenyl)-beta, delta-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid

Номер: US20120264934A1
Принадлежит: PFIZER INC

Novel salt forms of [R—(R*,R*)]-2-(4-fluorophenyl)-β,δ-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid characterized by their X-ray powder diffraction pattern and solid-state NMR spectra are described, as well as methods for the preparation and pharmaceutical composition of the same, which are useful as agents for treating hyperlipidemia, hypercholesterolemia, osteoporosis, benign prostatic hyperplasia, and Alzheimer's Disease.

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18-10-2012 дата публикации

Biological Buffers with Wide Buffering Ranges

Номер: US20120264945A1
Автор: Thomas Daly
Принадлежит: Thomas Daly

Amines and amine derivatives that improve the buffering range, and/or reduce the chelation and other negative interactions of the buffer and the system to be buffered. The reaction of amines or polyamines with various molecules to form polyamines with differing pKa's will extend the buffering range, derivatives that result in polyamines that have the same pKa yields a greater buffering capacity. Derivatives that result in zwitterionic buffers improve yield by allowing a greater range of stability.

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08-11-2012 дата публикации

Novel processes for the preparation of cyclopropyl-amide derivatives

Номер: US20120283433A1
Принадлежит: Individual

The present invention is directed to novel processes for the preparation of cyclopropyl-amide derivatives, useful for the treatment of disorders and conditions mediated by the histamine receptor.

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15-11-2012 дата публикации

Novel compounds with high therapeutic index

Номер: US20120289471A1
Автор: V. Ravi Chandran
Принадлежит: Signature R&D Holdings LLC

The present invention is directed to novel therapeutic compounds comprised of an amino acid bonded to a medicament or drug having a hydroxy, amino, carboxy or acylating derivative thereon. These high therapeutic index derivatives have the same utility as the drug from which they are made, and they have enhanced pharmacological and pharmaceutical properties. In fact, the novel drug derivatives of the present invention enhance at least one therapeutic quality, as defined herein. The present invention is also directed to pharmaceutical compositions containing same.

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22-11-2012 дата публикации

Novel Lipids and Compositions for Intracellular Delivery of Biologically Active Compounds

Номер: US20120295832A1
Принадлежит: Arrowhead Research Corp

The present invention provides novel amino-lipids, compositions comprising such amino-lipids and methods of producing them. In addition, lipid nanoparticles comprising the novel amino-lipids and a biologically active compound are provided, as well as methods of production and their use for intracellular drug delivery.

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22-11-2012 дата публикации

3-Arylamino Pyridine Derivatives

Номер: US20120295889A1
Принадлежит: MERCK SERONO SA

The invention provides novel, substituted 3-arylamino pyridine compounds pharmaceutically acceptable salts, solvates and prodrug compounds thereof, wherein W, R1, R2, R9, R10, R11, R12, R13, R14 are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer, restenosis and inflammation. Also disclosed is the use of such compounds in the treatment of hyperproliferative diseases in mammals, especially humans, and pharmaceutical compositions containing such compounds.

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06-12-2012 дата публикации

Semiconducting polymers

Номер: US20120305853A1
Принадлежит: Merck Patent GmBH

The invention relates to novel polymers containing repeating units based on benzodithiophene or derivatives thereof, monomers and methods for their preparation, their use as semiconductors in organic electronic (OE) devices, especially in organic photovoltaic (OPV) devices, and to OE and OPV devices comprising these polymers.

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06-12-2012 дата публикации

Process for the preparation of perfluoroalkylcyano- or perfluoroalkylcyanofluoroborates

Номер: US20120309981A1
Принадлежит: Merck Patent GmBH

The invention relates to a process for the preparation of salts having perfluoroalkyltricyano- or perfluoroalkylcyanofluoroborate anions, ((per)fluoro)phenyltricyano- or ((per)fluoro)phenylcyanofluoroborate anions, phenyltricyanoborate anions which are mono- or disubstituted by perfluoroalkyl groups having 1 to 4 C atoms or phenylcyanofluoroborate anions which are mono- or disubstituted by perfluoroalkyl groups having 1 to 4 C atoms, by reaction of alkali metal trifluoroperfluoroalkylborate with trialkylsilyl cyanide and a subsequent salt-exchange reaction or by direct reaction of an organic trifluoroperfluoroalkyl borate with trialkylsilyl cyanide.

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13-12-2012 дата публикации

Method for preparing chemical compounds of interest by nucleophilic aromatic substitution of aromatic carboxylic acid derivatives supporting at least one electro-attractive group

Номер: US20120316337A1

Method for preparing carboxylic acid derivatives by aromatic nucleophilic substitution, in which a carboxylic acid derivative having a single carboxyl functional group, or one of the salts thereof, the carboxylic acid derivative having, in the ortho position of the carboxyl functional group, a leaving group, which is preferably an atom of fluorine or of chlorine or an alkoxy group, chiral or not, preferably a methoxy group, the carboxylic acid derivative not being substituted by an electro attractive group other than the leaving group if any; is reacted with a reactant MNu, where M is a metal and Nu is a nucleophile, chiral or not, the aromatic nucleophilic substitution reaction being carried out without a catalyst and without a step of protecting/deprotecting the acid functional group of the starting compound.

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20-12-2012 дата публикации

Deuterated compounds useful for treating neurodegenerative diseases

Номер: US20120322799A1
Автор: GOPAL Damodara
Принадлежит: Pharmatrophix Inc

The present application is related to deuterated compounds which are novel neurotrophin mimetics. The application also discloses the treatment of disorders involving degradation or dysfunction of cells expressing p75 in a mammal by administering an effective amount of such deuterated compounds.

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20-12-2012 дата публикации

Heterocyclic sulfonamides, uses and pharmaceutical compositions thereof

Номер: US20120322823A1
Принадлежит: PFIZER INC

The invention is directed to a class of compounds, including the pharmaceutically acceptable salts of the compounds, having the structure of formula I: as defined in the specification. The invention is also directed to compositions containing and uses of the compounds of formula I.

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03-01-2013 дата публикации

Crystalline forms of neurotrophin mimetic compounds and their salts

Номер: US20130005731A1
Принадлежит: Pharmatrophix Inc

The present invention includes crystalline forms of 2-amino-3-methyl-N-(2-morpholinoethyl)-pentanamide and crystalline forms of salts and/or solvates of 2-amino-3-methyl-N-(2-morpholinoethyl)-pentanamide. Furthermore, the present invention provides compositions comprising the crystalline forms and therapeutic use of the crystalline forms.

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07-02-2013 дата публикации

Therapeutic peptides

Номер: US20130035296A1
Принадлежит: LYTIX BIOPHARMA AS

The present invention provides a peptide, peptidomimetic or amino acid derivative having a net positive charge of at least +2 and incorporating a disubstituted β amino acid, each of the substituting groups in the β amino acid, which may be the same or different, comprises at least (7) non-hydrogen atoms, is lipophilic and has at least one cyclic group, one or more cyclic groups within a substituting group may be linked or fused to one or more cyclic groups within the other substituting group and where cyclic groups are fused in this way the combined total number of non-hydrogen atoms for the two substituting groups is at least (12), for use as a cytolytic therapeutic agent; as well as non therapeutic uses of these molecules and certain defined novel compounds from within this definition.

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21-02-2013 дата публикации

Novel compound and use thereof

Номер: US20130043137A1
Принадлежит: JCU Corp

Provided is a copper plating technique that enables the filling of high aspect-ratio via-holes and through-holes in semiconductor substrates such as silicon substrates, organic material substrates or ceramic substrates. The disclosed technique involves a tertiary amine compound, which is obtained by reacting a heterocyclic compound with the epoxy group of a glycidyl ether group of a compound that has three or more glycidyl ether groups, and a quaternary amine compound thereof, as well as a copper plating additive, a copper plating bath, and a copper plating method employing the compounds.

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14-03-2013 дата публикации

RADIOLABELED COMPOUNDS AND METHODS THEREOF

Номер: US20130064770A1
Принадлежит: GE HEALTHCARE LIMITED

The present invention relates to radiodiagnostic compounds, methods of making those compounds, and methods of use thereof as imaging agents for preferably a HA serotonin 5-HT1A receptor for use in PET or SPECT, preferably PET. Compositions comprising an imaging-effective amount of radiolabeled compounds are also disclosed. The present invention also relates to non-radiolabeled compounds, methods of making those compounds, and methods of use thereof to treat various neurological and/or psychiatric disorders. 2. The compound of claim 1 , wherein the compound is radiolabeled.3. The compound of claim 1 , wherein the compound is not radiolabeled.4. The compound of claim 1 , wherein the compound comprises an F or a C atom.5. The compound of claim 1 , wherein an F or an C atom is attached directly to Ar.6. The compound of claim 1 , wherein a —OCHF group or —OCHgroup is directly attached to Ar claim 1 , wherein n is 1 to 4 and m is 2 to 8 claim 1 , respectively.7. The compound of claim 1 , wherein an F or an C atom is attached directly to Z or to a suitable group on Z.8. The compound of claim 1 , wherein an F or an C atom is attached directly to Lor Lor to a suitable group on Lor L.11. A composition comprising the compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , and a physiologically acceptable carrier or vehicle.12. A method for imaging one or more 5-HTreceptors in a subject in vivo claim 1 , the method comprising:{'claim-ref': {'@idref': 'CLM-00002', 'claim 2'}, '(a) administering to the subject an imaging-effective amount of a compound of , or a pharmaceutically acceptable salt thereof; and'}{'claim-ref': {'@idref': 'CLM-00002', 'claim 2'}, '(b) detecting the radioactive emission of the radiolabel on the compound of , or salt thereof, following its administration to the subject.'}13. The method of claim 12 , wherein the radioactive emission is detected using PET or SPECT.14. The method of claim 12 , wherein the radioactive emission is ...

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14-03-2013 дата публикации

2,5-disubstituted arylsulfonamide ccr3 antagonists

Номер: US20130065889A1
Принадлежит: Axikin Pharmaceuticals Inc

Provided herein are 2,5-disubstituted arylsulfonamide CCR3 antagonists, e.g., compounds of Formula I, and pharmaceutical compositions thereof: Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a CCR3-mediated disorder, disease, or condition.

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21-03-2013 дата публикации

PROPHYLACTIC OR THERAPEUTIC AGENT FOR DIABETES OR OBESITY

Номер: US20130072491A1
Принадлежит: AJINOMOTO CO., INC.

An object is to provide a CaSR agonist agent that has excellent CaSR agonist effects, and particularly, a pharmaceutical product that can prevent or remedy diabetes or obesity by the effect of CaSR activation. The aforementioned object is achieved by a composition that contains a compound represented by the following General Formula (I) or a salt thereof (refer to the Description for the definitions of the symbols used in the formula). 7. The method according to claim 6 , comprising administering 2-amino-3-{[(5-chloro-2-hydroxy-3-sulfophenyl)carbamoyl]amino}propanoic acid claim 6 , 2-amino-3-{[(3-chloro-4-methyl-5-sulfophenyl)carbamothioyl]amino}propanoic acid claim 6 , or 2-amino-3-{[(3-chloro-2-methyl-5-sulfophenyl)carbamoyl]amino}propanoic acid as an active component. This application is a continuation of International Patent Application No. PCT/JP2011/055124, filed on Mar. 4, 2011, and claims priority to Japanese Patent Application No. 2010-048310, filed on Mar. 4, 2010, and Japanese Patent Application No. 2010-086548, filed on Apr. 2, 2010, all of which are incorporated herein by reference in their entireties.The present invention relates to an alkylamine derivative or a salt thereof, and a pharmaceutical agent comprising the same. More particularly, the present invention relates to a prophylactic or therapeutic agent for diabetes or obesity, which comprises an alkylamine derivative or a pharmaceutically acceptable salt thereof as an active component.Energy metabolism in the body is controlled by insulin produced by pancreatic beta-cells. Insulin plays an important role in controlling the blood sugar level by affecting and promoting the peripheral tissues or cells to take up sugar from the blood. However, insulin sensitivity of the cells is reduced by continuous intake of high caloric diet, an increase in the blood sugar level as well as oversecretion of insulin proceed at the same time. As a result, pancreatic beta-cells are worn out and thus become ...

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28-03-2013 дата публикации

"OMEGA-AMINOALKYLAMIDES OF R-2-ARYL-PROPIONIC ACIDS AS INHIBITORS OF THE CHEMOTAXIS OF POLYMORPHONUCLEATE AND MONONUCLEATE CELLS"

Номер: US20130079514A1
Принадлежит: Dompé S.p.A.

(R)-2-Arylpropionamide compounds of formula (I), pharmaceutical preparations of the compounds and a process for making the compounds are described. 2. The composition claim according to claim 1 , wherein the compound of the formula I has activity as an inhibitor of IL-8 induced chemotaxis of polymorphonucleate leukocytes.3. The composition of claim 1 , containing said compound in an amount effective for the treatment of a pathology selected from the group consisting of psoriasis claim 1 , pemphigus and pemphigoid claim 1 , rheumatoid arthritis claim 1 , intestinal chronic inflammatory pathologies claim 1 , acute respiratory distress syndrome claim 1 , idiopathic fibrosis claim 1 , cystic fibrosis claim 1 , chronic obstructive pulmonary disease and glomerulonephritis.4. The composition of claim 1 , wherein X together with the nitrogen atom of the omega-amino group to which it is bound and with the R1 and R2 groups forms a non-aromatic nitrogen containing ring selected from 1-methyl-piperydin-4-yl and N-exo-8-methyl-8-aza-bicyclo[3.2.1]oct-3-yl.5. The composition according to claim 1 , wherein said compound of formula (I) is selected from the group consisting of(R)-2-[(4-isobutyl)phenyl]-N-(1-methylpiperidin-4-yl)propionamide;(R)-2-[(4-isobutyl)phenyl]-N(exo-8-methyl-8-aza-bicyclo[3.2.1]oct-3-yl)propionamide. This application is a Divisional application that claims priority under 35 U.S.C. §120 of application Ser. No. 10/469,094 filed on Aug. 25, 2003, and application Ser. No. 10/469,094 is the National Phase under 35 U.S.C. §371 of International Application No. PCT/EP2002/001974 filed on Feb. 25, 2002, which claims priority under 35 U.S.C. §119(a-d) of Application No. MI2001A000395 filed in the Italian Patent Office on Feb. 27, 2001. All of these applications are hereby incorporated by reference for all purposes.The present invention relates to omega-aminoalkylamides of (R) 2-aryl-propionic acids as inhibitors of the chemotaxis of polymorphonucleate and mononucleate ...

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11-04-2013 дата публикации

Process for the Preparation of Ranolazine

Номер: US20130090475A1
Автор: Li Dan, Shi Mingfeng, Xu Ling
Принадлежит:

A process for the preparation of ranolazine comprises the step of condensing N-(2,6-dimethylphenyl)-1-piperazinyl acetamide with a compound of formula (I) to obtain ranolazine, in which X is chlorine or bromine Ranolazine is prepared by condensing ring-opening halide which replaces epoxide in this process. 2. The process according to claim 1 , wherein the condensation is carried out in the presence of alcohol claim 1 , toluene claim 1 , or mixtures thereof.3. The process according to claim 1 , wherein a mole ratio of N-(2 claim 1 ,6-dimethylphenyl)-1-piperazinylacetamide to the compound of formula (I) is 0.8˜1.3:1.4. The process according to claim 1 , wherein the condensation reaction is carried out for 3˜5 h.5. The process according to claim 2 , wherein the alcohol is selected from the group consisting of methanol claim 2 , ethanol claim 2 , normal propyl alcohol claim 2 , and isopropyl alcohol.6. (canceled)7. The process according to claim 1 , further comprising a step of heating the condensate under reflux in an alkaline environment.8. The process according to claim 7 , wherein the alkaline environment is formed by sodium carbonate claim 7 , sodium bicarbonate claim 7 , potassium carbonate claim 7 , potassium bicarbonate claim 7 , or mixtures thereof. The present invention relates to the technical field of chemicals, and more particularly to a process for the preparation of an antianginal agent ranolazine.Ranolazine, chemically known as (±)-N-(2,6-dimethylplenyl)-4-[2-hydroxy-3-(2-methoxyphenoxy)propyl]-1-piperazineacetamide, is represented by the formula as given below.Ranolazine, a novel agent used to treat angina pectoris type coronary heart disease, was developed by American CV Therapeutica Company (now known as Gilead Sciences Company). Ranolazine has firstly been appeared on the market in US in 2006 and could be used to treat myocardial infarction, congestive heart disease, angina and arhythmia etc. The mechanism of action of ranolazine is to inhibit ...

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18-04-2013 дата публикации

PROCASPASE-ACTIVATING COMPOUNDS AND COMPOSITIONS

Номер: US20130096133A1
Автор: HERGENROTHER Paul J.

The invention provides compounds and compositions useful for the modulation of certain enzymes. The compounds and compositions can induce of cell death, particularly cancer cell death. The invention also provides methods for the synthesis and use of the compounds and compositions, including the use of compounds and compositions in therapy for the treatment of cancer and selective induction of apoptosis in cells. 2. The compound of wherein n is 1 or 2.3. The compound of wherein Ris methyl claim 1 , t-butyl claim 1 , methoxy claim 1 , hydroxy claim 1 , fluoro claim 1 , chloro claim 1 , bromo claim 1 , iodo claim 1 , amino claim 1 , ethylamino claim 1 , diethylamino claim 1 , trifluoromethoxy claim 1 , benzyl claim 1 , benzyloxy claim 1 , nitro claim 1 , 2-propenyl claim 1 , acetylene claim 1 , N-methyl-triazole claim 1 , or N-benzyl-triazole.4. The compound of wherein n is 2 and two Rgroups form an ortho-fused benzo group.5. The compound of wherein n is 2 and each Ris t-butyl.6. The compound of wherein n is 1 and Ris 2-propenyl.7. The compound of wherein Ris a methoxy-benzyl; dimethoxy-benzyl; benzyloxy-benzyl; t-butyl-benzyl; naphthylmethylene; or ethyl-benzyl.8. The compound of wherein Ris 4-methoxy-benzyl; 2 claim 1 ,5-dimethoxy-benzyl; 4-benzyloxy-benzyl; 4-t-butyl-benzyl; 2-naphthylmethylene; or 4-ethyl-benzyl.11. The compound of wherein the compound induces death of cancer cells in culture.12. A pharmaceutical composition comprising a compound of and a pharmaceutically acceptable diluent claim 1 , excipient claim 1 , or carrier.13. A method of treating a cancer cell comprising (a) identifying a susceptibility to treatment of a cancer cell with a procaspase activator compound; and (b) exposing a cancer cell to an effective amount of the procaspase activator compound; wherein the procaspase activator compound is a compound of .14. A method of inducing apoptosis in a cell comprising administering to a cell an effective amount of a compound of . This application ...

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18-04-2013 дата публикации

NOVEL THIOUREA OR UREA DERIVATIVE, PREPARATION METHOD THEREOF, AND PHARMACEUTICAL COMPOSITION FOR PREVENTING OR TREATING AIDS, CONTAINING SAME AS ACTIVE INGREDIENT

Номер: US20130096138A1
Принадлежит: AVIXGEN INC.

Disclosed are novel thiourea or urea derivatives inhibitory of HIV activity. Also provided are a method for preparing the thiourea or urea derivatives, and a pharmaceutical composition for the prophylaxis or therapy of AIDS comprising the derivatives. Having high inhibitory activity against HIV, the thiourea or urea derivatives can be effectively used in the prophylaxis or therapy of AIDS. 3. The thiourea or urea derivative claim 1 , or the pharmaceutically acceptable salt of claim 1 , wherein the thiourea or urea derivative is selected from the group consisting of:1-(4-tert-butyl-benzoyl)-3-(5-hydroxy-naphthalen-1-yl)-thiourea1-(4-tert-butyl-benzoyl)-3-(3-dimethylamino-propyl)-thiourea,1-(4-tert-butyl-benzoyl)-3-(3-dimethylamino-2,2-dimethyl-propyl)-thiourea,4-tert-butyl-N-(4-ethyl-piperazin-1-carbothioyl)-benzoamide,3-(4-tert-butyl-benzoyl)-1-(2-diethylamino-ethyl)-1-methyl-thiourea,3-(4-tert-butyl-benzoyl)-1-(2-dimethylamino-ethyl)-1-methyl-thiourea,1-(4-tert-butyl-benzoyl)-3-(4-diethylamino-1-methyl-butyl)-thiourea,1-(4-tert-butyl-benzoyl)-3-(4-methyl-benzyl)-thiourea,1-(4-tert-butyl-benzoyl)-3-(2-methyl-benzyl)-thiourea,1(4 tert-butyl-benzoyl)-3-(3-propylamino-propyl)-thiourea,1(4 tert-butyl-benzoyl)-3-phenethyl-thiourea,1-(4-tert-butyl-benzoyl)-3-(4-chloro-benzyl)-thiourea,1-(4-tert-butyl-benzoyl)-3-(3-chloro-benzyl)-thiourea,1-(4-tert-butyl-benzoyl)-3-(naphthalen-2-ylmethyl)-thiourea,4-tert-butyl-N-[4-(4-fluoro-phenyl)-piperazin-1-carbothioyl]-benzamide,1-(4-tert-butyl-benzoyl)-3-cyclohexyl-thiourea,1-(4-tert-butyl-benzoyl)-3-(2-fluoro-benzyl)-thiourea,1-benzoyl-3-(naphthalen-2-ylmethyl)-thiourea,1-benzoyl-3-[2-(4-chloro-phenyl)-ethyl]-thiourea,1-benzoyl-3-(4-diethylamino-1-methyl-butyl)-thiourea,3-benzoyl-1-(2-diethylamino-ethyl)-1-methyl-thiourea,N-(4-ethyl-piperazin-1-carbothioyl)-4-methyl-benzamide,1-cyclohexyl-3-(4-methyl-benzoyl)-thiourea,1-(4-chloro-benzyl)-3-(4-methyl-benzoyl)-thiourea,1-(3-dimethylamino-propyl)-3-(4-methyl-benzoyl)-thiourea,1-(4- ...

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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 ...

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02-05-2013 дата публикации

C7-Fluoro Substituted Tetracycline Compounds

Номер: US20130109657A1
Принадлежит: Tetraphase Pharmaceuticals Inc

The present invention is directed to a compound represented by Structural Formula (A): or a pharmaceutically acceptable salt thereof. The variables for Structural Formula (A) are defined herein. Also described is a pharmaceutical composition comprising the compound of Structural Formula (A) and its therapeutic use.

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02-05-2013 дата публикации

Small Molecule Inhibitors of Functions of the HIV-1 Matrix Protein

Номер: US20130109698A1
Автор: Simon Cocklin
Принадлежит: Simon Cocklin

The present invention includes a method of inhibiting, suppressing or preventing retroviral infection in a subject in need thereof, comprising administering to the subject a pharmaceutical composition comprising one or more of the compounds of the invention.

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09-05-2013 дата публикации

Synthesis of mse-framework type molecular sieves

Номер: US20130115163A1
Принадлежит: ExxonMobil Research and Engineering Co

A method of synthesizing a crystalline molecular sieve having an MSE framework type comprises crystallizing a reaction mixture comprising a source of water, a source of an oxide of a tetravalent element, Y, selected from at least one of silicon, tin, titanium, vanadium, and germanium, optionally a source of a trivalent element, X, a source of an alkali or alkaline earth metal, M, and a source of organic dications, Q, such as 3-hydroxy-1-(4-(1-methylpiperidin-1-ium-1 yl)butyl)quinuclidin-1-ium, 3-hydroxy-1-(5-(1-methylpiperidin-1-ium-1-yl)pentyl)quinuclidin-1-ium, 1,1′-(butane-1,4-diyl)bis(1-methylpiperidin-1-ium), 1,1′-(pentane-1,5-diyl)bis(1-methylpiperidin-1-ium), 1,1′-(hexane-1,6-diyl)bis(1-methylpiperidin-1-ium), and 1,1′-((3as,6as)-octahydropentalene-2,5-diyl)bis(1-methylpiperidin-1-ium).

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09-05-2013 дата публикации

BIARYL AMIDE DERIVATIVE OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF

Номер: US20130116227A1
Принадлежит: DAINIPPON SUMITOMO PHARMA CO., LTD.

Disclosed is a novel biaryl amide derivative represented by formula (1) and having an affinity for the aldosterone receptor; also disclosed is a pharmaceutically acceptable salt thereof. (In the formula, A is any of the groups represented by formula (a); L is —CONH—, etc.; Ris a substitutable aminosulfonyl group, etc.; Ris a hydrogen atom, etc.; Ris a hydrogen atom, etc.; Ris a hydrogen atom, a halogen atom, hydroxy group, a substitutable amino group, a substitutable Calkoxy group, a substitutable 4- to 7-membered cyclic amino group, etc.; R, Rand Rare each independently hydrogen atoms, etc.; Ris a halogen atom, a cyano group, etc.; Rand Rare each independently a hydrogen atom, etc.; and m is an integer such as 0.) 2. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein A is a group of formula (a).3. The compound of either claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein L is —NHCO—.4. The compound of either claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein L is —CONH—.5. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris [{'sub': '1-6', 'claim-text': [{'sub': '1-6', '(i) amino (in which the amino may be optionally substituted with the same or different 1 to 2 Calkyl),'}, {'sub': '1-6', '(ii) Calkoxy, or'}, '(iii) 4- to 7-membered cyclic amino),, '(a) Calkyl (in which the group may be optionally substituted with'}, {'sub': '1-6', '(b) Calkylcarbonyl,'}, '(c) aminocarbonyl, and', {'sub': '2', '(d) —C(═NH)—NH),'}], '1: aminosulfonyl group (in which the amino may be optionally substituted with the same or different 1 to 2 groups selected from the group consisting of'}{'sub': '1-6', '2: Calkylsulfonyl group, or'}{'sub': '1-6', '3: Calkylsulfonylamino group, or a pharmaceutically acceptable salt thereof.'}6. The compound of claim 5 , wherein Ris aminosulfonyl group claim 5 , or a pharmaceutically acceptable salt thereof.7. The compound of claim ...

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09-05-2013 дата публикации

HEXENONE COMPOUNDS AND MEDICAL USE THEREOF

Номер: US20130116256A1

The present invention relates to a compound of Formula I, or an isomer, pharmaceutically acceptable salt and solvate thereof; to a composition comprising a compound of Formula I, or an isomer, pharmaceutically acceptable salt and solvate thereof, and a pharmaceutically acceptable carrier, excipient or diluent; and also to use of a compound of Formula I, or an isomer, pharmaceutically acceptable salt and solvate thereof for combating apoptosis, or preventing or treating a disease or disorder associated with apoptosis; and especially use for protecting cardiomyocyte, or preventing or treating a disease or disorder associated with cardiomyocyte apoptosis. 4. The compound according to having the following structure claim 1 , or its isomers claim 1 , pharmaceutically acceptable salts and solvates:(1) (1E)-1-phenyl-5-(1-morpholinylthiocarboxamido)-6,6,6-trichloro-1-ene-3-hexanone.5. A pharmaceutical composition comprising a compound or an isomer claim 1 , pharmaceutically acceptable salt and solvate thereof according to claim 1 , and a pharmaceutically acceptable carrier claim 1 , excipient or diluent.6. Use of the compound or an isomer claim 1 , pharmaceutically acceptable salt and solvate thereof according to in manufacture of a medicament for combating apoptosis claim 1 , or preventing or treating a disease or disorder associated with apoptosis.7. Use of the compound or an isomer claim 1 , pharmaceutically acceptable salt and solvate thereof according to in manufacture of a medicament for protecting cardiomyocyte claim 1 , or preventing or treating a disease or disorder associated with cardiomyocyte apoptosis.8. A method for combating apoptosis claim 1 , or preventing or treating a disease or disorder associated with apoptosis comprising administering a subject in such need a therapeutically effective amount of a compound or an isomer claim 1 , pharmaceutically acceptable salt and solvate thereof according to .9. A method for protecting cardiomyocyte claim 1 , or ...

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16-05-2013 дата публикации

DIAMINE DERIVATIVES AS INHIBITORS OF LEUKOTRIENE A4 HYDROLASE

Номер: US20130123243A1
Принадлежит:

This invention is directed to compounds of formula (I): 3. A compound according to wherein{'sup': 1a', '13', '10', '13', '10, 'Ris hydrogen, —R—C(O)OR, —R—C(O)R, alkyl, halo, haloalkyl, cyano, optionally substituted cycloalkyl, optionally substituted cycloalkylalkyl, optionally substituted aryl, optionally substituted aralkyl, optionally substituted heteroaryl, optionally substituted heteroarylalkyl, optionally substituted heterocyclyl, or optionally substituted heterocyclylalkyl; and'}{'sup': 1b', '1c', '1d', '1e, 'R, R, Rand Rare each independently hydrogen or halo.'}4. A compound according to wherein{'sup': 1a', '13', '10', '13', '10, 'Ris hydrogen, —R—C(O)OR, —R—C(O)R, alkyl, halo, haloalkyl, optionally substituted phenyl, furanyl, thienyl, thiazolyl, or optionally substituted oxazolyl; and'}{'sup': 1b', '1c', '1d', '1e, 'R, R, Rand Rare each hydrogen.'}6. A compound according to wherein R an optionally substituted heteroaryl.7. A compound according to wherein R is furanyl claim 6 , oxazoyl claim 6 , pyrazolyl claim 6 , pyridinyl claim 6 , triazolyl claim 6 , thiazolyl claim 6 , or benzothiazolyl claim 6 , each of which is optionally substituted.8. A compound according to wherein:{'sup': 2', '7', '5a', '5b', '5c, 'Rand R, together with the nitrogens to which they are attached and one of R, Rand R, form an optionally substituted 6- to 10-membered bridged N-heterocyclyl.'}10. A compound according to wherein:{'sup': 3', '12', '12', '12, 'Ris a direct bond, —O—, —R—O—, —O—R—, —O—R—O—, or an optionally substituted straight or branched alkylene chain;'}{'sup': 4', '12a, 'Ris a direct bond, —O—R— or an optionally substituted straight or branched alkylene chain;'}{'sup': 8', '13', '10', '13', '10', '13', '10', '11, 'Ris aralkyl optionally substituted with one or more substituents selected from the group consisting of —R—OR, —R—C(═O)ORand —R—C(═O)N(R)R;'}{'sup': 9', '10, 'each Ris independently alkyl, halo or —O—R;'}{'sup': '12', 'Ris an optionally substituted straight ...

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23-05-2013 дата публикации

DERIVATIVES OF AMINOINDANES, THEIR PREPARATION AND THEIR APPLICATION IN THERAPEUTICS

Номер: US20130131034A1
Принадлежит: SANOFI

The instant invention relates to derivatives of formula (I) 5. A pharmaceutical composition comprising compound of claim 1 , or an addition salt of said compound to a pharmaceutically acceptable salt claim 1 , or an hydrate or solvate of said compound.6. The pharmaceutical composition according to further comprising at least one pharmaceutically acceptable excipient.7. A method of treating or preventing fibrotic disorders claim 5 , skeletal muscle dysfunction claim 5 , renal failure claim 5 , atherosclerosis claim 5 , heart failure claim 5 , cancer chronic obstructive pulmonary disease claim 5 , pain claim 5 , pulmonary hypertension claim 5 , ischemic stroke claim 5 , myocardial infarction claim 5 , inflammation or peripheral arterial occlusive disease in a patient in need thereof comprising administering to said patient a therapeutically effective amount of the pharmaceutical composition of .8. The method according to claim 7 , wherein said fibrotic disorder is focal segmental glomerulosclerosis.9. The method according to wherein said cancer is oesophageal cancer or breast cancer. The instant invention relates to derivatives of aminoindanes, to their preparation and to their application in therapeutics.Transient receptor potential cation channel, subfamily C, member 6, also known as TRPC6, is a human gene encoding a protein of the same name. TRPC6 has been associated with fibrotic disorders, such as focal segmental glomerulosclerosis (a) Winn et al, 2005, 308, 1801-1804. b) Hsu et al., 2007, 1772, 928-936. c) Kriz, 2005, 11, 527-530. d) Winn et al, 2005, 17, 378-387), skeletal muscle dysfunction (Millay et al., 2009, 106, 19023-19028), renal failure, atherosclerosis, heart failure (Kuwahara et al., 2006, 116, 3114-26), cancer (e.g. oesophageal cancer, breast cancer) (a) Aydar et al., 2009, 9, 23. b) Cai et al., 2009, 125, 2281-2287. c) Shi et al., 2009, 58, 1443-1450), chronic obstructive pulmonary disease (Sel et al., 2008, 38, 1548-1558), pain (Alessandri-Haber ...

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23-05-2013 дата публикации

Process for Producing SN-Comprising Catalysts

Номер: US20130131339A1
Принадлежит: BASF SE

The present invention relates to a process for producing a supported tin-comprising catalyst, wherein a solution (S) comprising tin nitrate and at least one complexing agent is applied to the support, where the solution (S) does not comprise any solid or has a solids content of not more than 0.5% by weight based on the total amount of dissolved components. 120.-. (canceled)21. A process for producing a supported tin-comprising catalyst , wherein a solution (S) comprising tin nitrate and at least one complexing agent is applied to the support , where the solution (S) does not comprise any solid or comprises a solids content of not more than 0.5% by weight based on the total amount of dissolved components.22. The process according to claim 21 , wherein the solution (S) is an aqueous solution.23. The process according to claim 21 , wherein the solution (S) additionally comprises at least one further metal salt.24. The process according to claim 23 , wherein the further metal salt is nickel nitrate claim 23 , cobalt nitrate or copper nitrate.25. The process according to claim 21 , wherein the support is aluminum oxide.26. The process according to claim 21 , wherein the complexing agent is selected from among glycolic acid claim 21 , lactic acid claim 21 , hydracylic acid claim 21 , hydroxybutyric acid claim 21 , hydroxyvaleric acid claim 21 , malic acid claim 21 , mandelic acid claim 21 , citric acid claim 21 , sugar acids claim 21 , tartronic acid claim 21 , tartaric acid claim 21 , oxalic acid claim 21 , malonic acid claim 21 , maleic acid claim 21 , succinic acid claim 21 , glutaric acid claim 21 , adipic acid claim 21 , glycine claim 21 , hippuric acid claim 21 , EDTA claim 21 , alanine claim 21 , valine claim 21 , leucine and isoleucine.27. The process according to claim 21 , wherein the solution (S) comprises tin nitrate claim 21 , nickel nitrate claim 21 , cobalt nitrate claim 21 , copper nitrate and citric acid.28. The process according to claim 21 , wherein the ...

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30-05-2013 дата публикации

4-carboxybenzylamino derivatives as histone deacetylase inhibitors

Номер: US20130137690A1
Принадлежит: Individual

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

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30-05-2013 дата публикации

INDANE ESTROGEN RECEPTOR MODULATORS AND USES THEREOF

Номер: US20130137746A1
Принадлежит: ARAGON PHARMACEUTICALS, INC.

Described herein are compounds that are estrogen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors. 2. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein:{'sup': '1', 'sub': 1', '4, 'Ris C-Calkyl;'}{'sup': 2', '8, 'Ris H or R;'}{'sup': 3', '8, 'Ris R;'}or{'sup': 2', '3, 'Rand Rare taken together with the N atom to which they are attached to form a substituted or unsubstituted monocyclic heterocycloalkyl, a substituted or unsubstituted bicyclic heterocycloalkyl, a substituted or unsubstituted monocyclic heteroaryl, or a substituted or unsubstituted bicyclic heteroaryl;'}{'sup': '4', 'sub': 1', '6', '1', '6', '1', '6', '1', '6', '1', '6, 'each Ris independently selected from H, halogen, —CN, —OH, C-Calkyl, C-Cfluoroalkyl, C-Cfluoroalkoxy, C-Calkoxy, and C-Cheteroalkyl;'}{'sup': 5', '7', '7', '8', '8', '8, 'sub': 2', '2', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6, 'each Ris independently selected from H, halogen, —CN, —OH, —OR, —SR, —S(═O)R, —S(═O)R, —NHS(═O)R, C-Calkyl, C-Cfluoroalkyl, C-Cfluoroalkoxy, C-Calkoxy, and C-Cheteroalkyl;'}{'sup': '5', 'or two Ron adjacent carbon atoms are taken together with the carbon atoms to which they are attached to form a fused substituted or unsubstituted monocyclic heterocycle;'}{'sup': 6', '7', '7', '8', '8', '8, 'sub': 2', '2', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6, 'each Ris independently selected from H, halogen, —CN, —OH, —OR, —SR, —S(═O)R, —S(═O)R, —NHS(═O)R, C-Calkyl, C-Cfluoroalkyl, C-Cfluoroalkoxy, C-Calkoxy, and C-Cheteroalkyl;'}{'sup': '6', 'or two Ron adjacent carbon atoms are taken together with the carbon atoms to which they are attached to form a fused substituted or unsubstituted ...

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06-06-2013 дата публикации

COMPOUNDS AND THEIR USE AS IKACH BLOCKERS

Номер: US20130143858A1
Принадлежит: AstraZeneca AB

The invention relates to compounds according to Formula I: 111-. (canceled)1516-. (canceled) The present invention relates to a novel class of compounds which are pharmacologically effective as potassium channel inhibitors, in particular inhibitors of the acetylcholine operated inward rectifying potassium channel current, i.e. IKACh blockers.The invention also relates to processes for preparing such compounds, to pharmaceutical compositions containing them, to the use of such compounds and to methods for their therapeutic use, particularly in the treatment of cardiac arrhythmias.The normal electrophysiologic behaviour of the heart is determined by ordered propagation of excitatory stimuli that result in rapid depolarization of the cardiac cell, followed by a slower repolarization. The sum of these events creates the cardiac action potential in individual myocytes. Cardiac rhythm disturbances can be caused by abnormalities of impulse generation, propagation or the duration and configuration of such individual cardiac action potentials. The action potentials are generated by the integrated activity of specific ion currents through various transmembrane spanning ion channels with specific selectivity for individual ions (e.g. potassium, sodium, calcium, see Grant AO. Circ. Arrhythmia Electrophysiol. 2009; 2:185-194). The majority of these ion channels have been cloned and thus, their molecular components are known. This knowledge has enabled a more effective search for selective ion channel blockers, as specific ion channel targets can be recombinantly over-expressed in mammalian cells and be used for high capacity screening.Electrophysiological studies in the early 1950s showed the importance of the movement of K out of the cell to produce repolarization after the rapid depolarizing spike. Over the last 60 years, the introduction of single channel recording techniques and molecular cloning has resulted in a deeper understanding of cardiac repolarization and of the ...

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06-06-2013 дата публикации

Guanidine compound

Номер: US20130143860A1
Принадлежит: Astellas Pharma Inc

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

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06-06-2013 дата публикации

(METH)ACRYLIC ACID ESTER, ACTIVATION ENERGY RAY CURING COMPOSITION, AND INKJET RECORDING INK

Номер: US20130144057A1
Автор: MORITA Mitsunobu
Принадлежит:

(Meth)acrylic acid ester, which contains one or more partial structures each represented by the following formula 1 in a molecule thereof, wherein the partial structure is a urethane structure which does not have a hydrogen atom directly bonded to a nitrogen atom of the following formula 1: 3. The (meth)acrylic acid ester according to claim 2 ,wherein the ring structure A in the formula 3 is a morpholine ring.5. The (meth)acrylic acid ester according to claim 4 , wherein the ring structure B in the formula 4 is a piperidine ring.7. The (meth)acrylic acid ester according to claim 1 , wherein the (meth)acrylic acid ester contains two or more partial structures each represented by the formula 1 in a molecule thereof. 1. Field of the InventionThe present invention relates to novel (meth)acrylic acid ester, and an activation energy ray curing composition using the same, and an inkjet recording ink using the same.2. Description of the Related ArtAs a method for forming an image on a recording medium, such as paper, there are various methods, such as electrophotography, sublimation recording, thermal transfer recording, and inkjet recording. Among them, the inkjet recording has high efficiency in ink consumption, and therefore is excellent in resources saving, and can keep an ink cost per unit recording low. However, there are various problems when an aqueous ink is used. There are inks using organic solvent instead of water, but these inks also have different problems.Because of the reasons as mentioned, attentions have recently been attracted to inkjet recording using an activation energy ray-curing ink. The activation energy ray-curing ink has been described as a UV ray-curing ink composition in various literatures, and documents. Typically, the activation energy ray-curing ink contains a polymerization initiator and monomers as essential components, and optionally contains substances such as a pigment, oligomers, polymers, and a sensitizing agent (Optical Applied ...

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13-06-2013 дата публикации

Pharmaceutical composition comprising a curcumin derivative

Номер: US20130150628A1
Автор: Thomas M. DiMauro
Принадлежит: Individual

The present invention is directed to a pharmaceutical composition comprising:

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20-06-2013 дата публикации

Stabilized protease composition

Номер: US20130157339A1
Принадлежит: TROBIO AB

A composition is provided, which comprises a serine protease; a reversible inhibitor of said serine protease; and a stabilizing agent M having the formula I: Also provided are uses of the composition as a medicament, and other uses and methods employing its various properties.

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20-06-2013 дата публикации

PHENYLAMIDINES HAVING A HIGH FUNGICIDAL ACTIVITY AND USE THEREOF

Номер: US20130157851A1
Принадлежит: ISAGRO S.P.A.

New phenylamidines are described, having general formula (I): 4. Fungicidal compositions comprising one or more compounds having formula (I) claim 1 , according to claim 1 , a solvent and/or a solid or liquid diluent claim 1 , optionally a surfactant.5. The compositions according to claim 4 , also comprising active principles compatible with the compounds having general formula (I) claim 4 , selected from fungicides other than the compounds having general formula (I) claim 4 , phytoregulators claim 4 , antibiotics claim 4 , herbicides claim 4 , insecticides claim 4 , fertilizers and/or mixtures thereof claim 4 , antifreeze agents claim 4 , adhesion agents.6. The compositions according to claim 4 , wherein the concentration of compounds having general formula (I) ranges from 1 to 90% by weight with respect to the total weight of the composition claim 4 , preferably from 5 to 50% by weight with respect to the total weight of the composition.8. Use of the compounds according to claim 2 , for the control of phytopatogenic fungi in agricultural crops.9. Use of the compositions according to for the control of phytopatogenic fungi in agricultural crops.10PucciniaUstilagoTilletiaUromycesPhakopsoraRhizoctoniaErysipheSphaerothecaPodosphaeraUncinulaHelminthosporiumRhynchosporiumPyrenophoraMoniliniaSclerotiniaSeptoriaMycosphaerellaVenturiaBotrytisAlternariaFusariumCercosporaCercosporella herpotrichoides, ColletotrichumPyricularia oryzae, SclerotiumPhytophtoraPythiumPlasmopara viticola, PeronosporaPseudoperonospora cubensis, Bremia lactucae.. Use according to claim 7 , for the control of phytopatogenic fungi belonging to the group of Basidiomycetes claim 7 , Ascomycetes claim 7 , Deuteromycetes or imperfect fungi claim 7 , Oomycetes: spp. claim 7 , spp. claim 7 , spp. claim 7 , spp. claim 7 , spp. claim 7 , spp. claim 7 , spp. claim 7 , spp. claim 7 , spp. claim 7 , spp. claim 7 , spp. claim 7 , spp. claim 7 , spp. claim 7 , spp. claim 7 , spp. claim 7 , spp. (spp.) claim 7 , ...

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20-06-2013 дата публикации

Acrylamide Compounds And Use Thereof For Inhibiting Apoptosis

Номер: US20130158022A1
Принадлежит: CHINESE PLA GENERAL HOSPITAL

The present invention relates to a compound of Formula I, or an isomer, pharmaceutically acceptable salt and solvate of the compound, and to a composition comprising the compound of Formula I, or the isomer, pharmaceutically acceptable salt and solvate thereof, and a pharmaceutically acceptable carrier, excipient or diluents. The present invention also relates to use of the compound of Formula I, or the isomer, pharmaceutically acceptable salt and solvate thereof for combating apoptosis, preventing or treating a disease or disorder associated with apoptosis; and especially use for protecting cardiomyocyte, and for preventing or treating a disease or disorder associated with cardiomyocyte apoptosis. 4. The compound according to having any one of the following structures claim 1 , or their isomers claim 1 , pharmaceutically acceptable salts and solvates:(1) (2E)-3-(2-thienyl)-N-[1-(8-quinolylamino)thioformylamino-2,2,2-trichloroethyl]-2-acrylamide;(2) (2E)-3-(3-thienyl)-N-[1-(8-quinolylamino)thioformylamino-2,2,2-trichloroethyl]-2-acrylamide;(3) (2E)-3-(2-thienyl)-N-[1-(4-tolylamino)thioformylamino-2,2,2-trichloroethyl]-2-acrylamide;(4) (2E)-3-(2-thienyl)-N-[1-(2-methoxyanilino)thioformylamino-2,2,2-trichloroethyl]-2-acrylamide;(5) (2E)-3-(2-thienyl)-N-(1-benzylaminothioformylamino-2,2,2-trichloroethyl)-2-acrylamide;(6) (2E)-3-(2-thienyl)-N-(1-cyclohexylaminothioformylamino-2,2,2-trichloroethyl)-2-acrylamide;(7) (2E)-3-(2-thienyl)-N-[1-isopropylaminothioformylamino-2,2,2-trichloroethyl]-2-acrylamide;(8) (2E)-3-(2-thienyl)-N-[1-(2-fluoroanilino)thioformylamino-2,2,2-trichloroethyl]-2-acrylamide;(9) (2E)-3-(2-thienyl)-N-[1-(3-isopropoxypropylamino)thioformylamino-2,2,2-trichloroethyl]-2-acrylamide;(10) (2E)-3-(2-thienyl)-N-[1-(2-methoxyformylanilino)thioformylamino-2,2,2-trichloroethyl]-2-acrylamide;(11) (2E)-3-(2-thienyl)-N-(1-cycloheptylaminothioformylamino-2,2,2-trichloroethyl)-2-acrylamide;(12) (2E)-3-(2-thienyl)-N-[1-(1-morpholinyl)thioformylamino-2,2,2- ...

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04-07-2013 дата публикации

SULFUR-CONTAINING COMPOUND, METHOD OF PREPARATION AND PHARMACEUTICAL USES THEREOF

Номер: US20130172355A1
Принадлежит: NATIONAL SUN YAT-SEN UNIVERSITY

The invention relates to a sulfur-containing compound and the preparation thereof. The invention also relates to the uses of the sulfur-containing compound in inhibiting inducible nitric oxide synthase and/or cyclooxygenase-2 and in treating the diseases associated with inducible nitric oxide synthase and/or cyclooxygenase-2. This invention also describes a series of chemical analogues of the said sulfur-containing compound and the preparation of these compounds. 2. The method according to claim 1 , wherein Ris selected from the group consisting of methyl claim 1 , ethyl claim 1 , and unsubstituted phenyl.6. The method according to claim 5 , wherein Ris selected from the group consisting of methyl claim 5 , ethyl claim 5 , and unsubstituted phenyl.9. The method according to claim 5 , wherein the disease is selected from the group consisting of inflammation claim 5 , atherosclerosis claim 5 , neuropathic pain claim 5 , inflammatory neointimal proliferation claim 5 , arthritis claim 5 , multiple sclerosis claim 5 , inflammatory pain claim 5 , and spinal cord injury.10. The method according to claim 5 , wherein the compound is administered by injection. This application is a Divisional of the pending U.S. patent application Ser. No. 12/172,633 filed on Jul. 14, 2008, all of which is hereby incorporated by reference in its entirety.Although incorporated by reference in its entirety, no arguments or disclaimers made in the parent application apply to this divisional application. Any disclaimer that may have occurred during the prosecution of the above-referenced application(s) is hereby expressly rescinded. Consequently, the Patent Office is asked to review the new set of claims in view of the entire prior art of record and any search that the Office deems appropriate.1. Field of the InventionThe invention relates to a novel sulfur-containing compound. Said sulfur-containing compound has ability to inhibit the function of inducible nitric oxide synthase (iNOS) and/or ...

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04-07-2013 дата публикации

NOVEL BENZENESULFONAMIDE COMPOUNDS, METHOD FOR SYNTHESIZING SAME, AND USE THEREOF IN MEDICINE AS WELL AS IN COSMETICS

Номер: US20130172363A1
Принадлежит: GALDERMA RESEARCH & DEVELOPMENT

Benzenesulfonamide compounds having a structure of formula (I) are described. Also described, are methods for synthesizing the compounds and to the use thereof in pharmaceutical compositions for human or veterinary medicine and in cosmetic compositions. 1. A compound having the name (S)—N-hydroxy-3-[4-(2-methylquinolin-4-ylmethoxy)benzenesulfonylamino]-2-[4-(propane-2-sulfonyl)piperazin-1-yl]propionamide.2. A composition comprising the compound as claimed in claim 1 , and an acceptable carrier.3. A pharmaceutical composition comprising the compound claim 1 , as claimed in and a pharmaceutically acceptable carrier.5. The compound as claimed in claim 4 , in which{'sub': '4', 'Ris an alkyl radical containing 1 to 4 carbon atoms; and'}{'sub': '3', 'Ris a polycyclic aromatic heterocylic radical containing the heteroatom N;'}and salts thereof, and enantiomers thereof.6. The compound as claimed in claim 4 , wherein the compound is (S)—N-hydroxy-3-[4-(2-methylquinolin-4-ylmethoxy)benzenesulfonylamino]-2-[4-(propane-2-sulfonyl)piperazin-1-yl]propionamide claim 4 , and salts thereof claim 4 , and enantiomers thereof.7. A composition comprising the compound as claimed in claim 4 , or a salt thereof claim 4 , or an enantiomer thereof claim 4 , and an acceptable carrier.8. A pharmaceutical composition comprising the compound as claimed in claim 4 , a salt thereof claim 4 , or an enantiomer thereof claim 4 , and a pharmaceutically acceptable carrier.9. A method of treating an inflammatory skin disease claim 3 , wherein the method comprises administering the pharmaceutical composition as claimed in claim 3 , to a subject in need thereof.10. The method of claim 9 , wherein the inflammatory skin disease is psoriasis or atopic dermatitis.11. A method of treating an inflammatory skin disease claim 8 , wherein the method comprises administering the pharmaceutical composition as claimed in claim 8 , to a subject in need thereof.12. The method of claim 11 , wherein the inflammatory skin ...

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04-07-2013 дата публикации

PROCESSES FOR MAKING CYCLOPROPYL AMIDE DERIVATIVES AND INTERMEDIATES ASSOCIATED THEREWITH

Номер: US20130172560A1
Автор: Stranne Robert
Принадлежит: AstraZeneca AB

Presented herein are processes for making cyclopropyl amide derivatives of formula I, and/or pharmaceutically acceptable salts thereof, and intermediates associated therewith. At least one cyclopropyl amide derivative of formula I, or pharmaceutically acceptable salt thereof is useful to treat at least one histamine H3 receptor associated condition. 3. The process of claim 2 , wherein said base is sodium hydroxide.4. The process of claim 2 , wherein said peroxide is hydrogen peroxide.5. The process of claim 2 , wherein said acidic solution is an aqueous solution of sodium hydrogen sulfate.7. The process of claim 6 , wherein X is Br.8. The process of claim 6 , wherein said metal is zinc.9. The process of claim 6 , wherein said metal cyanide is zinc-(II)-cyanide.10. The process of claim 6 , wherein said catalyst is bis(tri-t-butylphosphine)palladium(0).15. The process of claim 14 , wherein said activating agent is 1 claim 14 ,1′-carbonyldiimidazole.19. The process of claim 18 , wherein the activating agent is a mixture of 1-hydroxybenzotriazole and 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride.21. The process of claim 16 , wherein said acid is hydrochloric acid.23. The process of claim 17 , wherein said reducing agent is sodium triacetoxy borohydride. Presented herein are processes for making cyclopropyl amide derivatives of formula I, and/or pharmaceutically acceptable salts thereof, and intermediates associated therewith. At least one cyclopropyl amide derivative of formula I, or pharmaceutically acceptable salt thereof is useful to treat at least one histamine H3 receptor associated condition.The histamine H3 receptor is of current interest in developing new medicaments. The H3 receptor is a presynaptic autoreceptor located both in the central and peripheral nervous systems, the skin, and in organs, such as, for example, the lung, the intestine, probably the spleen, and the gastrointestinal tract. Recent evidence suggests the H3 receptor has intrinsic ...

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04-07-2013 дата публикации

Method for producing alcohol and/or amine from amide compound

Номер: US20130172619A1
Принадлежит: Takasago International Corp

Disclosed herein is a method for producing an alcohol and an amine from an amide under an atmosphere of hydrogen with the use of, as a catalyst, a ruthenium complex that is easily prepared, easy to handle, and relatively cheaply obtained. Specifically, the method is a method for producing an alcohol and/or an amine from an amide compound under an atmosphere of hydrogen with the use of as a catalyst, a ruthenium carbonyl complex represented by the following general formula (1): RuXY(CO)(L) (1) wherein X and Y may be the same or different from each other and each represents an anionic ligand and L represents a tridentate aminodiphosphine ligand containing two phosphino groups and a —NH— group.

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11-07-2013 дата публикации

Composition for maintaining function of platelets

Номер: US20130177900A1

A composition for maintaining a function of platelets, the composition comprising, as an active ingredient, a compound represented by the following general formula (I) or a salt thereof, or a solvate thereof: wherein X represents a phenylene group; Y represents any one of a hydrogen atom and —(CH 2 ) m R 1 ; wherein m represents an integer of any one of 0 to 4; and R 1 is any one of —NR 5 COR 2 , —NR 5 SO 2 R 2 , and —NR 3 R 4 ; wherein R 2 represents any one of a C1 to C6 alkyl group, an aryl group, a C1 to C6 alkoxy group, and the like; R 3 and R 4 represent a C1 to C6 alkyl group or the like; and R 5 represents any one of a hydrogen atom, a C1 to C6 alkyl group, and the like; and Z represents any one of a hydrogen atom and a C1 to C6 alkyl group.

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11-07-2013 дата публикации

Cannabinoid receptor modulators

Номер: US20130178457A1
Принадлежит: Lupin Ltd

Compounds of Formula (I) along with processes for their preparation that are useful for treating, managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of cannabinoid (CB) receptors. Methods of treating, managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of cannabinoid (CB) receptors of Formula (I).

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18-07-2013 дата публикации

AMINOTETRALINE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM, AND THEIR USE IN THERAPY

Номер: US20130184238A1
Принадлежит:

The present invention relates to aminotetraline derivatives of the formula (I) 4. Compound as claimed in claim 1 , wherein Ris hydrogen claim 1 , halogen or C-C-alkoxy.6. Compound as claimed in claim 1 , wherein Ris hydrogen or C-C-alkyl.8. Compound as claimed in claim 1 , wherein Ris hydrogen claim 1 , C-C-alkyl claim 1 , C-C-cycloalkyl-C-C-alkyl claim 1 , halogenated C-C-alkyl claim 1 , amino-C-C-alkyl claim 1 , CHCN claim 1 , —CHO claim 1 , C-C-alkylcarbonyl claim 1 , (halogenated C-C-alkyl)carbonyl claim 1 , C-C-arylcarbonyl claim 1 , C-C-alkoxycarbonyl claim 1 , C-C-aryloxycarbonyl claim 1 , —C(═NH)NH claim 1 , —C(═NH)NHCN claim 1 , C-C-alkylsulfonyl claim 1 , amino claim 1 , —NO or C-C-heterocyclyl.9. Compound as claimed in claim 1 , wherein Ris hydrogen or C-C-alkyl.10. Compound as claimed in claim 1 , wherein R claim 1 , Rtogether are optionally substituted C-C-alkylene claim 1 , wherein one —CH— of C-C-alkylene may be replaced by an oxygen atom.11. Compound as claimed in claim 1 , wherein Xis CRR.12. Compound as claimed in claim 11 , wherein Xis a bond.13. Compound as claimed in claim 1 , wherein Ris hydrogen or C-C-alkyl and Ris hydrogen or C-C-alkyl.14. Compound as claimed in claim 1 , wherein R claim 1 , Rtogether are optionally substituted C-C-alkylene.15. Compound as claimed in claim 1 , wherein Ris optionally substituted aryl or optionally substituted C-C-cycloalkyl.17. Compound as claimed in claim 1 , wherein n is 1.18. Compound as claimed in claim 1 , which is:7-Amino-8-(3,4-dichlorobenzyl)-5,6,7,8-tetrahydronaphthalene-2-carbonitrile;7-Amino-8-(4-chlorobenzyl)-5,6,7,8-tetrahydronaphthalene-2-carbonitrile;Ethyl [7-cyano-1-(3,4-dichlorobenzyl)-1,2,3,4-tetrahydronaphthalen-2-yl]carbamate;tert-Butyl [7-cyano-1-(3,4-dichlorobenzyl)-1,2,3,4-tetrahydronaphthalen-2-yl]carbamate,or a physiologically tolerated salt thereof.19. A pharmaceutical composition comprising a carrier and a compound of .20. A method for treating a neurologic or psychiatric disorder ...

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18-07-2013 дата публикации

APOPTOSIS-INDUCING AGENTS FOR THE TREATMENT OF CANCER AND IMMUNE AND AUTOIMMUNE DISEASES

Номер: US20130184278A1
Принадлежит: ABBOTT LABORATORIES

Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein. 5. The compound of claim 1 , or therapeutically acceptable salt thereof claim 1 , wherein the compound is selected from the group consisting of:4-[4-(cyclohexylmethyl)-4-methoxypiperidin-1-yl]-N-{[5-({(1R)-3-(dimethylamino)-1-[(phenylthio)methyl]propyl}amino)-4-nitrothien-2-yl]sulfonyl}benzamide;N-{[5-({(1R)-3-(dimethylamino)-1-[(phenylthio)methyl]propyl}amino)-4-nitrothien-2-yl]sulfonyl}-4-[4-methoxy-4-(3-methylbenzyl)piperidin-1-yl]benzamide;N-{[5-({(1R)-3-(dimethylamino)-1-[(phenylthio)methyl]propyl}amino)-4-nitrothien-2-yl]sulfonyl}-4-[4-(3,3-diphenylprop-2-enyl)piperazin-1-yl]benzamide;4-{4-[(4′-chloro-1,1′-biphenyl-2-yl)methyl]piperazin-1-yl}-N-[(4-{[2-(phenylthio)ethyl]amino}piperidin-1-yl)sulfonyl]benzamide;N-[(4-{acetyl[2-(phenylthio)ethyl]amino}piperidin-1-yl)sulfonyl]-4-{4-[(4′-chloro-1,1′-biphenyl-2-yl)methyl]piperazin-1-yl}benzamide;4-{4-[(4′-chloro-1,1′-biphenyl-2-yl)methyl]piperazin-1-yl}-N-[(4-{methyl[2-(phenylthio)ethyl]amino}piperidin-1-yl)sulfonyl]benzamide;4-{4-[(4′-chloro-1,1′-biphenyl-2-yl)methyl]piperazin-1-yl}-N-{[5-({(1R)-3-[isopropyl(methyl)amino]-1-[(phenylthio)methyl]propyl}amino)-4-nitrothien-2-yl]sulfonyl}benzamide;4-(4-{[2-(4-chlorophenyl)cyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[5-({(1R)-3-[isopropyl(methyl)amino]-1-[(phenylthio)methyl]propyl}amino)-4-nitrothien-2-yl]sulfonyl}benzamide;4-(4-{[2-(4-chlorophenyl)-5,5-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[5-({(1R)-3-[isopropyl(methyl)amino]-1-[(phenylthio)methyl]propyl}amino)-4-nitrothien-2-yl]sulfonyl}benzamide;N-{[(5Z)-5-(acetylimino)-4-methyl-4,5-dihydro-1,3,4-thiadiazol-2-yl]sulfonyl}-4-{4-[(4′-chloro-1,1′-biphenyl-2-yl)methyl]piperazin-1-yl}benzamide;N-({5-[(benzoylamino)methyl]thien-2-yl}sulfonyl)-4-{4-[(4′-chloro-1,1′-biphenyl-2-yl)methyl]piperazin-1-yl ...

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25-07-2013 дата публикации

BENZYL SULFONAMIDE DERIVATIVES AS RORC MODULATORS

Номер: US20130190288A1
Принадлежит: Genentech, Inc.

Compounds of the formula I: 2. The compound of claim 1 , wherein n is 0 or 1.3. The compound of claim 1 , wherein X claim 1 , X claim 1 , Xand Xare CR.4. The compound of claim 1 , wherein m is from 0 to 2 and each Ris independently: Calkyl; halo; Calkoxy; cyano; halo-Calkyl; or halo-Calkoxy.5. The compound of claim 1 , wherein Ris: Calkyl; Ccycloalkyl; or Ccycloalkyl-Calkyl; each of which may be optionally substituted one or more times with R.6. The compound of claim 1 , wherein Ris Ccycloalkyl.7. The compound of claim 1 , wherein Ris cyclobutyl.8. The compound of claim 1 , wherein Rand Rare hydrogen.9. The compound of claim 1 , wherein Rand Rare hydrogen.11. The compound of claim 1 , wherein Y is N.12. The compound of claim 1 , wherein Z is —CRR—.13. The compound of claim 1 , wherein Y is CH.14. The compound of claim 1 , wherein Z is —NR—.15. The compound of claim 1 , wherein p is 2.16. The compound of claim 1 , wherein q is 2.17. The compound of claim 1 , wherein each Ris indepently: hydrogen; Calkyl; or halo.18. The compound of claim 1 , wherein Rand Rare hydrogen.19. The compound of claim 1 , wherein Ris acetyl.22. The compound of claim 1 , wherein A is: pyrrolidin-1-yl; 4-hydroxy-piperidin-1-yl; 2-methoxy-ethylamino; morpholin-4-yl; 4-methyl-piperazin-1-yl; 2-hydroxy-ethylamino; 3-oxo-piperazin-1-yl; 2-dimethylamino-ethylamino; 4-(dimethylaminocarbonyl)-piperidin-1-yl; 4-methoxymethyl-piperidin-1-yl; 4-hydroxymethyl-piperidin-1-yl; 4-(aminocarbonyl)-piperidin-1-yl; 4-(dimethylamino)-piperidin-1-yl; 4-(cyanomethyl)-piperidin-1-yl; 3-hydroxy-pyrrolidin-1-yl; 4-(methanesulfonyl)-piperazin-1-yl; 4-acetyl-piperazin-1-yl; 4-methoxy-piperidin-1-yl; 3-hydroxy-piperidin-1-yl; 3-(aminocarbonyl)-pyrrolidin-1-yl; 1 claim 1 ,1-Dioxo-thiomorpholin-4-yl; 4-(methoxycarbonyl)-piperazin-1-yl; 4-(methylcarbonylamino)-piperidin-1-yl; 3-methanesulfonyl-pyrrolidin-1-yl; 3-hydroxy-azetidin-1-yl; 4-(ethoxycarbonyl)-piperazin-1-yl; 3-(aminocarbonyl)-azetidin-1-yl; 3-( ...

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25-07-2013 дата публикации

COMPOSITIONS AND METHODS FOR THE TREATMENT OF DISEASE ASSOCIATED WITH TRP-P8 EXPRESSION

Номер: US20130190296A1
Принадлежит: Dendreon Corporation

Provided are small-molecule Trp-p8 modulators, including Trp-p8 agonists and Tip-p8 antagonists, and compositions comprising small-molecule Trp-p8 agonists as well as methods for identifying and characterizing novel small-molecule Trp-p8 modulators and methods for decreasing viability and/or inhibiting growth of Trp-p8 expressing cells, methods for activating Trp-p8-mediated cation influx, methods for stimulating apoptosis and/or necrosis, and related methods for the treatment of diseases, including cancers such as lung, breast, colon, and/or prostate cancers as well as other diseases, such as benign prostatic hyperplasia, that are associated with Trp-p8 expression. 24.-. (canceled)5. A composition comprising a compound of and a pharmaceutically acceptable excipient or diluent.67.-. (canceled)8. A method for decreasing the viability of a Trp-p8 expressing cell claim 1 , said method comprising the step of contacting said cell with a small-molecule Trp-p8 modulator in a concentration and for a time required to decrease the viability of said cell.9. The method of wherein said small-molecule Trp-p8 modulator is selected from the group consisting of a compound of Formula I claim 8 , a compound of Formula II claim 8 , a compound of Formula III claim 8 , a compound of Formula IV claim 8 , a compound of Formula V claim 8 , a compound of Formula VI claim 8 , a compound of Formula VII claim 8 , and a compound of Formula VIII.1417-. (canceled)19. (canceled)22. A method for inducing apoptosis and/or necrosis in a cell expressing Trp-p8 or for treating a disease associate with Trp-p8 expression claim 8 , said method comprising the step of administering to said cell a small-molecule Trp-p8 modulator selected from the group consisting of a compound of Formula I claim 8 , a compound of Formula II claim 8 , a compound of Formula III claim 8 , a compound of Formula IV claim 8 , a compound of Formula V claim 8 , a compound of Formula VI claim 8 , a compound of Formula VII claim 8 , ...

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25-07-2013 дата публикации

BIS-FATTY ACID CONJUGATES AND THEIR USES

Номер: US20130190327A1
Принадлежит: CATABASIS PHARMACEUTICALS INC

The invention relates to bis-fatty acid conjugates; compositions comprising an effective amount of a bis-fatty acid conjugate; and methods for treating or preventing cancer, a metabolic disease or a neurodegenerative disease comprising the administration of an effective amount of a bis-fatty acid conjugate. 1. A molecular conjugate , directly or indirectly covalently linked wherein the linker comprises at least one amide , comprising two or more fatty acids selected from the group consisting of omega-3 fatty acids , fatty acids that are metabolized in vivo to omega-3 fatty acids , and lipoic acid , with the proviso that the molecular conjugate is not (4Z ,7Z ,10Z ,13Z ,16Z ,19Z)-docosa-4 ,7 ,10 ,13 ,16 ,19-hexaenoic acid {2-[2-((4Z ,7Z ,10Z ,13Z ,16Z ,19Z)-docosa-4 ,7 ,10 ,13 ,16 ,19-hexaenoylamino)-ethylamino]-ethyl}-amide (A); (5Z ,8Z ,11Z ,14Z ,17Z)-icosa-5 ,8 ,11 ,14 ,17-pentaenoic acid {2-[2-((5Z ,8Z ,11Z ,14Z ,17Z)-icosa-5 ,8 ,11 ,14 ,17-pentaenoylamino)-ethylamino]-ethyl}-amide (B); (4Z ,7Z ,10Z ,13Z ,16Z ,19Z)-docosa-4 ,7 ,10 ,13 ,16 ,19-hexaenoic acid {2-[2-((4Z ,7Z ,10Z ,13Z ,16Z ,19Z)-docosa-4 ,7 ,10 ,13 ,16 ,19-hexaenoylamino)-ethoxy]-ethyl}-amide (C); (5Z ,8Z ,11Z ,14Z ,17Z)-icosa-5 ,8 ,11 ,14 ,17-pentaenoic acid {2-[2-((5Z ,8Z ,11Z ,14Z ,17Z)-icosa-5 ,8 ,11 ,14 ,17-pentaenoylamino)-ethoxy]-ethyl}-amide (D); or (S)-2 ,6-Bis-((4Z ,7Z ,10Z ,13Z ,16Z ,19Z)-docosa-4 ,7 ,10 ,13 ,16 ,19-hexaenoylamino)-hexanoic acid (E).2. The molecular conjugate of claim 1 , wherein the fatty acid is selected from the group consisting of all-cis-7 claim 1 ,10 claim 1 ,13-hexadecatrienoic acid claim 1 , α-linolenic acid claim 1 , stearidonic acid claim 1 , eicosatrienoic acid claim 1 , eicosatetraenoic acid claim 1 , eicosapentaenoic acid (EPA) claim 1 , docosapentaenoic acid claim 1 , docosahexaenoic acid (DHA) claim 1 , tetracosapentaenoic acid claim 1 , tetracosahexaenoic acid and lipoic acid.3. The molecular conjugate of claim 2 , wherein the fatty acid is selected from ...

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25-07-2013 дата публикации

APOPTOSIS PROMOTERS

Номер: US20130190488A1
Принадлежит: ABBOTT LABORATORIES

Disclosed are compounds which inhibit the activity of anti-apoptotic protein family members, compositions containing the compounds and uses of the compounds for preparing medicaments for treating diseases during which occurs expression one or more than one of an anti-apoptotic protein family member. 19-. (canceled)10. A compound , or a therapeutically acceptable salt thereof , wherein the compound is selected from the group consisting of:N-(4-(4-((4′-chloro(1,1′-biphenyl)-2-yl)methyl)piperazin-1-yl(benzoyl)-4-(((1R)-3-(dimethylamino)-1-((phenylsulfanyl)methyl)propyl)amino)-3-(trifluoromethyl)benzenesulfonamide;N-(4-(4-((4′-chloro(1,1′-biphenyl)-2-yl)methyl)piperazin-1-yl)benzoyl)-4-(((1R)-3-(morpholin-4-yl)-1-((phenylsulfanyl)methyl)propyl)amino)-3-(trifluoromethyl)benzenesulfonamide;N-(4-(4-((4′-chloro(1,1′-biphenyl)-2-yl)methyl)piperazin-1-yl(benzoyl)-4-(((1R)-3-(5,6-dihydro-1(4H)-pyrimidin-1-yl)-1-((phenylsulfanyl)methyl)propyl)amino)-3-(trifluoromethyl)benzenesulfonamide;N-(4-(4-((4′-chloro(1,1′-biphenyl)-2-yl)methyl)piperazin-1-yl(benzoyl)-4-(((1R)-3-(2,4-dimenthyl-4,5-dihydro-1H-imidazol-1-yl)-1-((phenylsulfanyl)methyl)propyl)amino)-3-(trifluoromethyl)benzenesulfonamide;N-(4-(4-((4′-chloro(1,1′-biphenyl)-2-yl)methyl)piperazin-1-yl)benzoyl)-4-(((1R)-3-methyl-4,5-dihydro-1H-imidazol-1-yl)-1-((phenylsulfanyl)methyl)propyl)amino)-3-(trifluoromethyl)benzenesulfonamide;N-(4-(4-((4′-chloro(1,1′-biphenyl)-2-yl)methyl)piperazin-1-yl)benzoyl)-4-(((1R)-3-(4,4-dimethyl-4,5-dihydro-1H-imidazol-1-yl)-1-((phenylsulfanyl)methyl)propyl)amino)-3-(trifluoromethyl)benzenesulfonamide;N-(4-(4-((2-(4-chlorophenyl)-1-cyclohexen-1-yl)methyl)piperazin-1-yl(benzoyl)-4-(((1R)-3-(dimethylamino)-1-((phenylsulfanyl)methyl)propyl)oxy)-3-(trifluoromethyl)benzenesulfonamide;N-(4-(4-((2-(4-chlorophenyl)cyclohept-1-en-1-yl)methyl)piperazin-1-yl)benzoyl)-4-(((1R)-3-(dimethylamino)-1-((phenylsulfanyl)methyl)propyl)amino)-3-(trifluoromethyl)benzenesulfonamide;4-(((1R)-3-(bis(2-methoxyethyl)amino)-1 ...

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08-08-2013 дата публикации

NAPHT-2-YLACETIC ACID DERIVATIVES TO TREAT AIDS

Номер: US20130203727A1
Принадлежит: Gilead Sciences, Inc.

The invention provides compounds of formula (I): or a salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula (I), intermediates useful for preparing compounds of formula I and therapeutic methods for treating the proliferation of the HIV virus, treating AIDS or delaying the onset of AIDS or ARC symptoms in a mammal using compounds of formula (I). 2. The compound of wherein Ris (C-C)alkyl claim 1 , (C-C)alkenyl or —O(C-C)alkyl wherein any (C-C)alkyl or (C-C)alkenyl of Ris optionally substituted with one or more groups selected from —O(C-C)alkyl claim 1 , halo claim 1 , oxo and —CN; and wherein Ris H.4. The compound of wherein Ris selected from:{'sub': 1', '6', '2', '6', '1', '6', '3', '7', '1', '6', '1', '6', '2', '1', '6', '1', '6', '2', '1', '6', '1', '6, 'a) aryl, heterocycle and heteroaryl, wherein any aryl, heterocycle and heteroaryl is optionally substituted with one or more groups each independently selected from halo, (C-C)alkyl, (C-C)alkenyl, (C-C)haloalkyl, (C-C)cycloalkyl, —OH, —O(C-C)alkyl, —SH, —S(C-C)alkyl, —NH, —NH(C-C)alkyl and —N((C-C)alkyl), wherein (C-C)alkyl is optionally substituted with hydroxy, —O(C-C)alkyl, cyano or oxo;'}{'sub': 3', '14', '3', '14', '3', '7, 'sup': 1', '1, 'b) (C-C)carbocycle, wherein (C-C)carbocycle is optionally substituted with one or more Zgroups, wherein two Zgroups together with the atom or atoms to which they are attached optionally form a (C-C)carbocycle or heterocycle; and'}{'sup': 7', '1, 'c) aryl, heteroaryl and fused-heterocycle, wherein any aryl, heteroaryl and fused-heterocycle is substituted with one or more Zgroups and optionally substituted with one or more Zgroups.'}5. The compound of wherein Ris selected from:{'sub': 1', '6', '2', '6', '1', '6', '3', '7', '1', '6', '1', '6', '2', '1', '6', '1', '6', '2', '1', '6', '1', '6, 'a) aryl, heterocycle and heteroaryl, wherein any aryl, heterocycle and ...

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08-08-2013 дата публикации

COMPOSITIONS AND METHODS FOR MODULATING INTERACTION BETWEEN POLYPEPTIDES

Номер: US20130203733A1
Принадлежит:

The present invention is based, in part, on assays we conducted that revealed compounds that may be used to treat or prevent diseases characterized by an abnormal or undesirable association of one protein with another. 2. The composition of claim 1 , wherein Z is O.3. The composition of claim 1 , wherein Y is NR.4. The composition of claim 1 , wherein Ris H.5. The composition of claim 1 , wherein Y is CRR.6. The composition of claim 1 , wherein each Rand Ris independently halo or hydroxy.79-. (canceled)10. The composition of claim 1 , wherein{'sup': '22', 'Ris halo; and'}q is 1.11. The composition of claim 10 , wherein p is 0.12. The composition of claim 10 , wherein Ris bromo.1324-. (canceled)25. A pharmaceutical composition comprising:4-Bromo-N-(4-bromo-phenyl)-3-cyclohexylsulfamoyl-benzamide;N-(4-Bromo-phenyl)-3-(4-bromo-phenylsulfamoyl)-benzamide;3-(4-Bromo-phenylsulfamoyl)-N-phenyl-benzamide;4-Bromo-3-cyclohexylsulfamoyl-N-phenyl-benzamide;N-(4-Bromo-phenyl)-3-cyclohexylsulfamoyl-benzamide; or1-[3-(Azepane-1-sulfonyl)-2-bromo-phenyl]-2-(3-hydroxy-phenyl)-ethanone.2628-. (canceled)29. A method of treating a subject who has been diagnosed as having claim 1 , or who is at risk of developing claim 1 , a disorder characterized by an undesirable association of proteins claim 1 , the method comprising identifying the subject and administering to the subject a therapeutically effective amount of the pharmaceutical composition of .30. The method of claim 29 , wherein the subject has been diagnosed as having claim 29 , or is at risk of developing claim 29 , Huntington's disease.31. The method of claim 29 , wherein the subject has been diagnosed as having claim 29 , or is at risk of developing claim 29 , Parkinson's disease.32. The method of claim 29 , wherein the subject has been diagnosed as having claim 29 , or is at risk of developing claim 29 , spinal and bulbar muscular atrophy claim 29 , dentatorubral-pallidoluysian atrophy claim 29 , spinocerebellar ataxia type 1 ...

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08-08-2013 дата публикации

BISARYL (THIO)MORPHOLINE DERIVATIVES AS S1P MODULATORS

Номер: US20130203745A1
Принадлежит: AbbVie B.V.

The present invention relates to bisaryl(thio)morpholine derivatives of the formula (I) 3. The compound of claim 1 , wherein R3 is selected from —(CH)—OH claim 1 , —CH—COOH claim 1 , —(CH)—COOH claim 1 , —(CH)—COOH claim 1 , —CH—CHCH—COOH claim 1 , —CH—C(CH)—COOH claim 1 , —CHCH—CH—COOH claim 1 , —CH—CF—COOH claim 1 , —CO—CH—COOH claim 1 , —(CH)—POH claim 1 , —(CH)—POH claim 1 , —(CH)—OPOH claim 1 , —(CH)OPOH claim 1 , —CH-tetrazol-5-yl claim 1 , —(CH)-tetrazol-5-yl claim 1 , and —(CH)-tetrazol-5-yl;and R4 is H.4. The compound of claim 2 , wherein R3 is —(CH)—COOH.5. The compound of claim 1 , wherein W is selected from —O— and —S— claim 1 , and R2 is selected from H and halogen.6. The compound of claim 1 , wherein the ring structure B is phenylene.7. The compound of claim 1 , wherein R5 is H.8. The compound of claim 1 , wherein R1 is selected from pyridyl claim 1 , pyrimidinyl claim 1 , biphenyl claim 1 , naphthyl claim 1 , dihydrobenzofuranyl optionally substituted with oxo claim 1 , benzdioxanyl claim 1 , quinolinyl claim 1 , isoquinolinyl and phenyl wherein{'sub': '2', 'each is optionally substituted with at least one substituent independently selected from halogen, a (1-6C)alkyl group, a di(1-4C)alkylamino group, a —SO-(1-4C)alkyl group, a —CO-(1-4C)alkyl group, a —CO—O-(1-4C)alkyl group, a —NH—CO-(1-4C)alkyl group, a difluoromethyl group, a trifluoromethyl group, a difluoromethoxy group, and a trifluoromethoxy group, or each is optionally substituted with a substituent selected from phenoxy, benzyl, benzyloxy, phenylethyl, and morpholinyl.'}9. The compound of claim 1 , wherein A is selected from —CO— claim 1 , —NH— claim 1 , and —O—.10. The compound of claim 1 , wherein the compound is selected from:3-{2-[4-(2,6-Dichloro-phenylamino)-phenyl]-morpholin-4-yl}-propionic acid,3-{2-[4-(2,6-Dimethyl-phenylamino)-phenyl]-morpholin-4-yl}-propionic acid,3-{2-[4-(2,6-Dimethyl-benzoyl)-phenyl]-morpholin-4-yl}-propionic acid,3-{2-[4-(3-Trifluoromethyl-benzoyl)-phenyl]- ...

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08-08-2013 дата публикации

Compounds And Compositions For Treating Cancer

Номер: US20130203757A1
Принадлежит:

The invention relates to compounds and composition for the treatment and prevention of cancer. The invention also covers all diseases that may be treated by selective modulation of levels of reactive oxygen species in diseased cells versus normal cells. Methods for the preparation and administration of such compositions are also disclosed. 4. A pharmaceutical composition comprising one or more compounds of claim 1 , or its pharmaceutically acceptable salt claim 1 , and a pharmaceutically acceptable carrier.5. The pharmaceutical composition of claim 4 , further comprising one or more chemotherapeutic agents.6. A kit comprising a pharmaceutical composition comprising a therapeutically effective amount of a compound of or its salt or analog claim 1 , and instructions for preparation and/or administration of the pharmaceutical composition.7. The kit of claim 6 , further comprising one or more chemotherapeutic agents.8. A method for treating a cancer in a subject claim 1 , the method comprising: administering to a subject in need of such treatment a therapeutically effective amount of a compound of or its salt or analog claim 1 , to an individual in need thereof.9. The method of claim 8 , wherein treatment inhibits further growth of the cancer.10. The method of wherein the cancer is a carcinoma claim 8 , a sarcoma claim 8 , a melanoma claim 8 , a pancreatic cancer claim 8 , a breast cancer or a bladder cancer.11. The method of wherein the effective amount is from about 2.5 mg/kg to about 100 mg/kg of a compound of formula 1.12. A method for inhibiting cell proliferation claim 1 , the method comprising: contacting a cell with an effective amount of a composition comprising a compound of to inhibit the proliferation of the cell.13. A method for increasing apoptosis of a cell or in a population of cells claim 1 , the method comprising: contacting the cell or population of cells with an effective amount of a composition comprising a compound of to increase apoptosis in the ...

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08-08-2013 дата публикации

Nicotinic receptor non-competitive antagonists

Номер: US20130203860A1
Принадлежит: Individual

The present invention relates to compounds that modulate nicotinic receptors as non-competitive antagonists, methods for their synthesis, methods for use, and their pharmaceutical compositions.

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15-08-2013 дата публикации

CANNABIDINOID DERIVATIVES

Номер: US20130209483A1
Автор: McAllister Sean D.
Принадлежит: Sutter West Bay Hospitals

The disclosure relates to cannabinoid derivative compounds, pharmaceutical compositions made thereof, and methods for treating various diseases and disorders including cancer. 2. The compound of claim 1 , wherein Ris selected from the group consisting of methyl claim 1 , ethyl claim 1 , n-propyl claim 1 , n-butyl claim 1 , n-pentyl claim 1 , n-hexyl claim 1 , n-heptyl claim 1 , isopropyl claim 1 , sec-butyl claim 1 , (1-methyl)butyl claim 1 , (1-methyl)pentyl claim 1 , (1-methyl)hexyl claim 1 , (1-methyl)heptyl claim 1 , (1 claim 1 ,1-dimethyl)propyl claim 1 , (1 claim 1 ,1-dimethyl)butyl claim 1 , (1 claim 1 ,1-dimethyl)pentyl claim 1 , (1 claim 1 ,1-dimethyl)hexyl claim 1 , (1 claim 1 ,1-dimethyl)heptyl claim 1 , (1 claim 1 ,2-dimethyl)propyl claim 1 , (1 claim 1 ,2-dimethyl)butyl claim 1 , (1 claim 1 ,2-dimethyl)pentyl claim 1 , (1 claim 1 ,2-dimethyl)hexyl claim 1 , (1 claim 1 ,2-dimethyl)heptyl claim 1 , (1 claim 1 ,3-dimethyl)butyl claim 1 , (1 claim 1 ,3-dimethyl)pentyl claim 1 , (1 claim 1 ,3-dimethyl)hexyl claim 1 , (1 claim 1 ,3-dimethyl)heptyl claim 1 , (1 claim 1 ,4-dimethyl)pentyl claim 1 , (1 claim 1 ,4-dimethyl)hexyl claim 1 , (1 claim 1 ,4-dimethyl)heptyl claim 1 , (1 claim 1 ,5-dimethyl)hexyl claim 1 , (1 claim 1 ,5-dimethyl)heptyl claim 1 , (1 claim 1 ,6-dimethyl)heptyl claim 1 , (1 claim 1 ,2-diethyl)butyl claim 1 , (1 claim 1 ,2-diethyl)pentyl claim 1 , (1 claim 1 ,2-diethyl)hexyl claim 1 , (1 claim 1 ,2-diethyl)heptyl claim 1 , (1 claim 1 ,2-diethyl)pentyl claim 1 , (1 claim 1 ,3-diethyl)pentyl claim 1 , (1 claim 1 ,3-diethyl)hexyl claim 1 , (1 claim 1 ,3-diethyl)heptyl claim 1 , (1 claim 1 ,4-diethyl)pentyl claim 1 , (1 claim 1 ,4-diethyl)hexyl claim 1 , (1 claim 1 ,4-diethyl)heptyl claim 1 , (1 claim 1 ,5-diethyl)hexyl claim 1 , (1 claim 1 ,5-diethyl)heptyl claim 1 , (1 claim 1 ,6-diethyl)heptyl claim 1 , (1 claim 1 ,2 claim 1 ,3-trimethyl)butyl claim 1 , (1 claim 1 ,1 claim 1 ,2-trimethyl)butyl claim 1 , (1 claim 1 ,1 claim 1 ,3-trimethyl) ...

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15-08-2013 дата публикации

Cycloalkyl Substituted Pyrimidinediamine Compounds And Their Uses

Номер: US20130210814A1
Принадлежит: Rigel Pharmaceuticals, Inc.

The present disclosure provides 2,4-pyrimidinediamine compounds having antiproliferative activity, compositions comprising the compounds and methods of using the compounds to inhibit cellular proliferation and to treat proliferate diseases such as tumorigenic cancers. 148.-. (canceled)50. The method according to wherein the cell is a human cancer cell.51. The method according to wherein the cell is a breast claim 50 , colon claim 50 , renal claim 50 , cervical claim 50 , neuroblastomer claim 50 , melanoma claim 50 , pancreatic claim 50 , prostate claim 50 , or other type of solid tumor.53. The method according to claim 52 , wherein the Aurora kinase-mediated disease or disorder is melanoma claim 52 , leukemia claim 52 , or a solid tumor cancer selected from the group consisting of colon claim 52 , breast claim 52 , gastric claim 52 , ovarian claim 52 , cervical claim 52 , melanoma claim 52 , renal claim 52 , prostate claim 52 , lymphoma claim 52 , neuroblastoma claim 52 , pancreatic and bladder cancers. This application claims priority under 35 U.S.C. §119(e) to U.S. application No. 60/572,534 filed May 18, 2004, U.S. application No. 60/572,507 filed May 18, 2004, U.S. application No. 60/580,765 filed Jun. 18, 2004, U.S. application No. 60/628,496 filed Nov. 15, 2004, U.S. application No. 60/628,199 filed Nov. 15, 2004, and U.S. application No. 60/650,195 filed Feb. 3, 2005, the disclosures of which are incorporated herein by reference in their entireties.The present disclosure provides 2,4-pyrimidinediamine compounds that exhibit antiproliferative activity, prodrugs of the compounds, intermediates and methods of synthesizing the compounds and/or prodrugs, pharmaceutical compositions comprising the compounds and/or prodrugs and methods of using the compounds and/or prodrugs in a variety of contexts, including, for example, in the treatment and/or prevention of proliferative disorders, such as tumors and cancers.Cancer is a group of varied diseases characterized by ...

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15-08-2013 дата публикации

Pharmaceutical Compounds

Номер: US20130210820A1
Принадлежит: ASTEX THERAPEUTICS LTD

The invention provides a compound of the formula (1): or a salt, solvate, N-oxide or tautomer thereof.

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15-08-2013 дата публикации

APPLICATION OF 5-HT6 RECEPTOR ANTAGONISTS FOR THE ALLEVIATION OF COGNITIVE DEFICITS OF DOWN SYNDROME

Номер: US20130210829A1
Принадлежит:

Methods for treating Down syndrome and improving cognitive function of a patient with an intellectual disability are disclosed. 5-hydroxytryptamine sub-receptor six (5-HT) receptor antagonists are provided for improving the cognition of a Down syndrome patient. 1. A method of treating Down syndrome , comprising administering to a subject in need thereof an effective amount of a 5-HTreceptor antagonist.2. The method of claim 1 , where the 5-HTreceptor antagonist is chosen from: a 5-HTreceptor inverse agonist claim 1 , a 5-HTreceptor competitive antagonist claim 1 , or a 5-HTreceptor inhibitor.3. The method of claim 2 , wherein the 5-HTreceptor antagonist is a 5-HTreceptor competitive antagonist.4. The method of claim 1 , wherein the 5-HTreceptor antagonist directly binds to the 5-HTreceptor.5. The method of claim 1 , wherein the 5-HTreceptor antagonist is a small molecule 5-HTreceptor antagonist.6. The method of claim 5 , wherein the small molecule 5-HTreceptor antagonist has a molecular weight of less than 800 Daltons.9. The method of claim 1 , wherein the subject is administered a pharmaceutical composition comprising a 5-HTreceptor antagonist or a pharmaceutically acceptable salt thereof claim 1 , and a pharmaceutically acceptable carrier.10. The method of claim 1 , wherein the route of administration of the 5-HTantagonist is selected from at least one of the following: intravenous claim 1 , intraperitoneal claim 1 , subcutaneous claim 1 , parenteral claim 1 , intramuscular claim 1 , oral claim 1 , topical claim 1 , transmucosal claim 1 , intraventricular claim 1 , or intrathecal administration.11. The method of claim 1 , wherein the subject suffers from a comorbid disorder associated with Down syndrome comprising Autism spectrum disorders claim 1 , attention deficit hyperactivity disorder claim 1 , obsessive compulsive disorder claim 1 , and disorders involving speech and language.12. The method of claim 1 , wherein the 5-HTantagonist is administered in ...

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15-08-2013 дата публикации

PROCESS FOR THE PREPARATION OF CHIRAL TRIAZOLONES

Номер: US20130210833A1
Принадлежит: SANDOZ AG

A process for the preparation of a chiral compound, in particular posaconazole, wherein the process comprises mixing and reacting the compounds of formula (I) Y—NH; of formula (IIa) 0=C═N—Yand/or of formula (IIb) and of formula (III) in a solvent in any order to obtain a reaction mixture containing a chiral compound of formula (IV) and/or formula (V). 2. The process of claim 1 , wherein in (2) claim 1 ,(2.1) the compounds of formulae (I) and (IIb) are mixed and at least partially reacted in a solvent to obtain a reaction mixture;(2.2) adding the compound of formula (III) to the reaction mixture obtained from (2.1).3. The process of claim 1 , wherein reacting in (2) is carried out in the absence of a compound of formula Cl—C(═O)—O-Ph claim 1 , in particular in the absence of an ester of a halogenated formic acid.4. The process of claim 1 , wherein in (2) claim 1 , the solvent is a polar aprotic solvent or a mixture of two or more thereof claim 1 , preferably selected from the group consisting of dichloromethane DCM claim 1 , tetrahydrofurane (THF) claim 1 , methyl tetrahydrofurane (MeTHF) claim 1 , acetonitrile (AN) claim 1 , an ester claim 1 , preferably butylacetate (BuAc) or ethylacetate (EtAc) claim 1 , dimethylformamide (DMF) and a mixture of two or more thereof claim 1 , preferably DCM or THF.5. The process of claim 1 , wherein reacting in (2) is carried out at a temperature in the range of from −20 to +40° C.6. The process of claim 1 , wherein reacting in (2) is carried out in the presence of an acid claim 1 , preferably in the presence of a substoichiometric amount of an acid claim 1 , which acid is at least partially soluble in the solvent employed in (2) claim 1 , the acid preferably being trifluoroacetic acid (TFA).8. The process of claim 1 , wherein in the compound of formula (III) claim 1 , Ris an alkyl residue having from 1 to 4 carbon atoms claim 1 , preferably 1 or 2 carbon atoms claim 1 , most preferably 2 carbon atoms claim 1 , in particular ethyl ...

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15-08-2013 дата публикации

Novel uses of esteramide compounds

Номер: US20130210933A1
Принадлежит: Rhodia Operations SAS

The use of an esteramide compound, alone or as a mixture of the following formula (I): R 1 OOC-A-CONR 2 R 3   (I) is described, wherein: A is a covalent bond or a methylene group —CH 2 —, R 1 is an optionally substituted hydrocarbon group having from 1 to 36 carbon atoms, R 2 and R 3 , either identical or different, are groups selected from a hydrogen atom and optionally substituted hydrocarbon groups comprising from 1 to 36 carbon atoms, R 2 and R 3 may form together a ring having the nitrogen atom to which they are bound, said ring being, if need be, substituted and/or having an additional heteroatom and R 2 and R 3 not being simultaneously hydrogens. Also described, are applications for using the esteramide compound as a solvent, a co-solvent, a coalescence agent, a crystallization inhibitor, a plasticizer or an agent for increasing biological activity.

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15-08-2013 дата публикации

PROCESS FOR THE MANUFACTURE OF TMHQ

Номер: US20130211080A1
Принадлежит: DSM IP ASSETS B.V.

The present invention is directed to a process for the manufacture of 2,3,5-trimethyl-hydro-p-benzoquinone comprising the following steps: a) hydrogenating 2,6-dimethyl-p-benzoquinone with hydrogen in the presence of a hydrogenation catalyst in an organic solvent to obtain 2,6-dimethyl-hydro-p-benzoquinone; b) reacting 2,6-dimethyl-hydro-p-benzoquinone with a secondary amine and formal-dehyde in an organic solvent to obtain 2,6-dimethyl-3-(N,N-disubstituted aminomethyl)-hydro-p-benzoquinone; c) reacting 2,6-dimethyl-3-(N,N-disubstituted aminomethyl)-hydro-p-benzoquinone with hydrogen in the presence of a hydrogenolysis catalyst in an organic solvent to obtain 2,3,5-trimethylhydro-p-benzoquinone; wherein the organic solvent in all steps a), b) and c) is independently selected from the group consisting of methyl tert.-butyl ether, ethyl tert.-butyl ether, tert.-amyl ether, methoxycyclopentane and any mixtures thereof. Preferably the organic solvent used in all steps a), b) and c) is the same. 1. A process for the manufacture of 2 ,3 ,5-trimethyl-hydro-p-benzoquinone comprising the following steps:a) hydrogenating 2,6-dimethyl-p-benzoquinone with hydrogen in the presence of a hydrogenation catalyst in an organic solvent to obtain 2,6-dimethyl-hydro-p-benzoquinone;b) reacting 2,6-dimethyl-hydro-p-benzoquinone with a secondary amine and formaldehyde in an organic solvent to obtain 2,6-dimethyl-3-(N,N-disubstituted aminomethyl)-hydro-p-benzoquinone;c) reacting 2,6-dimethyl-3-(N,N-disubstituted aminomethyl)-hydro-p-benzoquinone with hydrogen in the presence of a hydrogenolysis catalyst in an organic solvent to obtain 2,3,5-trimethylhydro-p-benzoquinone;wherein the organic solvent used in steps a), b) and c) is independently selected from the group consisting of methyl tert.-butyl ether, ethyl tert.-butyl ether, methyl tert.-amyl ether, methoxycyclopentane and any mixtures thereof.2. The process according to claim 1 , wherein the organic solvent in all steps a) claim 1 , b) ...

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22-08-2013 дата публикации

NOVEL PROLYLCARBOXYPEPTIDASE INHIBITORS

Номер: US20130217660A1
Принадлежит:

Compounds of structural formula I are inhibitors of prolylcarboxypeptidase (PrCP). The compounds of the present invention are useful for the prevention and treatment of conditions related to the enzymatic activity of PrCP such as abnormal metabolism, including obesity; diabetes; metabolic syndrome; obesity related disorders; and diabetes related disorders. 2. The compound of wherein R claim 1 , R claim 1 , and Rare hydrogen; or a pharmaceutically acceptable salt thereof.4. The compound of wherein Ris phenyl claim 1 , wherein phenyl is unsubstituted or substituted with one to three substituents selected from R; or a pharmaceutically acceptable salt thereof.9. The compound of wherein Ris —C(O)—(CH)N(R)and Ris hydrogen; or Rand Rform a morpholine ring; or a pharmaceutically acceptable salt thereof.10. The compound of wherein q is 0 or 1; or a pharmaceutically acceptable salt thereof.12. The compound of wherein{'sup': '1', 'claim-text': (1) hydrogen,', {'sub': 2', '1-6, '(2) —COCalkyl,'}, {'sub': 2', 'p, '(3) —C(O)—(CH)-halogen,'}, {'sub': 2', 'p', '2, 'sup': 'f', '(4) —C(O)—(CH)N(R),'}, {'sub': 2', 'p', '2-6, '(5) —C(O)—(CH)—Ccycloheteroalkyl,'}, {'sub': 2', 'p, '(6) —C(O)—(CH)-heteroaryl, and'}, {'sub': 2', '2-3', '1-6, '(7) —(CH)—O—Calkyl,'}], 'Ris independently selected from the group consisting of{'sub': '2', 'sup': 'b', 'wherein each CH, alkyl, cycloheteroalkyl, and heteroaryl is unsubstituted or substituted with one to two groups independently selected from R;'}{'sup': '2', 'claim-text': (1) hydrogen,', {'sub': '1-6', '(2) —Calkyl, and'}, {'sub': '1-6', '(3) —Calkoxy,'}], 'Ris selected from the group consisting of{'sup': 'c', 'wherein each alkyl and alkoxy is unsubstituted or substituted with one to four substituents selected from R, or'}{'sup': 1', '2, 'sub': '1-3', 'Rand Rform a morpholine ring, wherein the morpholine ring is unsubstituted or substituted with —Calkyl and oxo;'}{'sup': 3', '4', '5, 'R, R, and Rare hydrogen;'}{'sup': '6', 'claim-text': [{'sub': 2 ...

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