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Небесная энциклопедия

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

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Мониторинг СМИ

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

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Форма поиска

Поддерживает ввод нескольких поисковых фраз (по одной на строку). При поиске обеспечивает поддержку морфологии русского и английского языка
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Применить Всего найдено 41116. Отображено 100.
05-01-2012 дата публикации

Clathrate, curing agent, cure accelerator, epoxy resin composition, and epoxy resin composition for encapsulation of semiconductor

Номер: US20120004377A1
Автор: Kazuo Ono, Masami Kaneko
Принадлежит: Nippon Soda Co Ltd

It is an object of the present invention to provide a clathrate that suppresses a curing reaction at low temperature to promote an improvement in storage stability (one-component stability), and can effectively cure a resin by heating treatment. A clathrate suitable for the clathrate is a clathrate containing (b1) at least one selected from the group consisting of an aliphatic polyvalent carboxylic acid, 5-nitroisophthalic acid, 5-tert-butylisophthalic acid, 5-hydroxyisophthalic acid, isophthalic acid, and benzophenone-4,4′-dicarboxylic acid; and (b2) at least one selected from the group consisting of an imidazole compound represented by the following formula (I), and 1,8-diazabicyclo[5.4.0]undecene-7, at a molar ratio of 1:1.

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19-01-2012 дата публикации

(2,5-dioxoimidazolidin-i-yl)-n-hydroxy-acetamides as metalloproteinase inhibitors

Номер: US20120015994A1
Принадлежит: Medivir AB

The invention provides compounds of the formula (I) wherein the variables are as defined in the specification. The compounds of the invention are inhibitors of metalloproteinase MMP-12 and are among other things useful for the treatment of obstructive airway diseases, such as chronic obstructive pulmonary disease (COPD).

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26-01-2012 дата публикации

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

Номер: US20120020915A1

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

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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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26-01-2012 дата публикации

Fluorine-containing n-alkylsulfonylimide compound, manufacturing method therefor, and method of manufacturing an ionic compound

Номер: US20120022269A1

According to the method for producing fluorine-containing N-alkylsulfonylimide compound, the fluorine-containing N-alkylsulfonylimide compound can be produced safely with a high recovery rate by alkylating fluorine-containing sulfonylimide acid or fluorine-containing sulfonylimide acid salt with dialkylsulfuric acid or dialkylcarbonic acid.

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02-02-2012 дата публикации

Novel lipids and compositions for the delivery of therapeutics

Номер: US20120027796A1
Принадлежит: Alnylam Pharmaceuticals Inc

The present invention provides lipids that are advantageously used in lipid particles for the in vivo delivery of therapeutic agents to cells. In particular, the invention provides lipids having the following structures: (Formula (I) or (XXXV)).

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09-02-2012 дата публикации

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

Номер: US20120035230A1
Принадлежит: ProteoTech Inc

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

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09-02-2012 дата публикации

Volatile Imidazoles and Group 2 Imidazole Based Metal Precursors

Номер: US20120035351A1
Принадлежит: Air Products and Chemicals Inc

Sterically hindered imidazole ligands are described, along with their synthesis, which are capable of coordinating to Group 2 metals, such as: calcium, magnesium, strontium, in an eta-5 coordination mode which permits the formation of monomeric or dimeric volatile complexes. A compound comprising one or more polysubstituted imidazolate anions coordinated to a metal selected from the group consisting of barium, strontium, magnesium, radium or calcium or mixtures thereof. Alternatively, one anion can be substituted with and a second non-imidazolate anion. Synthesis of the novel compounds and their use to form BST films is also contemplated

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01-03-2012 дата публикации

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

Номер: US20120052441A1
Принадлежит: Shin Etsu Chemical Co Ltd

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

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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

Five-membered heterocycles useful as serine protease inhibitors

Номер: US20120088758A1
Принадлежит: Bristol Myers Squibb Co

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

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12-04-2012 дата публикации

Azole derivatives and fused bicyclic azole derivatives as therapeutic agents

Номер: US20120088778A1
Принадлежит: vTvx Holdings I LLC

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

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19-04-2012 дата публикации

Ionic liquid solvents of perhalide type for metals and metal compounds

Номер: US20120090430A1
Принадлежит: Individual

The present invention relates to a process for dissolving metals in perhalide containing ionic liquids, and to the extraction of metals from mineral ores; the remediation of materials contaminated with heavy, toxic or radioactive metals; and to the removal of heavy and toxic metals from hydrocarbon streams.

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19-04-2012 дата публикации

Novel lipids and compositions for the delivery of therapeutics

Номер: US20120095075A1
Принадлежит: Alnylam Pharmaceuticals Inc

The present invention provides lipids that are advantageously used in lipid particles for the in vivo delivery of therapeutic agents to cells. In particular, the invention provides lipids having the following structure:

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26-04-2012 дата публикации

Compositions and articles comprising polymerizable ionic liquid mixture, and methods of curing

Номер: US20120101184A1
Принадлежит: 3M Innovative Properties Co

Presently described are curable compositions comprising a mixture of at least one (e.g. free-radically) polymerizable ionic liquid and at least one other ethylenically unsaturated monomer, oligomer, or polymer. The polymerizable ionic liquid is characterized as having an air to nitrogen curing exotherm ratio of at least 0.70. Also described are articles and methods of making articles from such curable compositions. A monofunctional polymerizable ionic liquid is also described comprising a non-polymerizable substituted imidazolium cationic group and a polymerizable sulfonate anion.

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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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10-05-2012 дата публикации

Crystalline forms of an alkoxyimidazol-1-ylmethyl biphenyl carboxylic acid

Номер: US20120115920A1
Принадлежит: Theravance Inc

The invention provides crystalline salt forms of 4′-{2-ethoxy-4-ethyl-5-[((S)-2-mercapto-4-methylpentanoylamino)methyl]-imidazol-1-ylmethyl}-3′-fluorobiphenyl-2-carboxylic acid. This invention also provides pharmaceutical compositions comprising the crystalline compounds, processes and intermediates for preparing the crystalline compounds, and methods of using the crystalline compounds to treat diseases such as hypertension.

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17-05-2012 дата публикации

Compounds, Compositions and Methods for Modulating Uric Acid Levels

Номер: US20120122780A1
Принадлежит: Ardea Biociences Inc

Described herein are compounds useful in the reduction of blood uric acid levels, formulations containing them and methods of making and using them. In some embodiments, the compounds described herein are used in the treatment or prevention of disorders related to aberrant levels of uric acid.

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17-05-2012 дата публикации

No-Carrier-Added Nucleophilic [F-18] Fluorination of Aromatic Compounds

Номер: US20120123120A1
Принадлежит: UNIVERSITY OF CALIFORNIA

Phenyliodonium ylide derivatives substituted with electron donating as well as electron withdrawing groups on the aromatic ring are shown for use as precursors in aromatic nucleophilic substitution reactions. The iodonium ylide group is substituted by nucleophiles such as halide ions to provide the corresponding haloaryl derivatives. No-carrier-added [F-18]fluoride ion exclusively substitutes the iodonium ylide moiety in these derivatives and provides high specific activity F-18 labeled fluoro derivatives. Protected L-dopa-6-iodonium ylide derivative have been synthesized as a precursors for the preparation of no-carrier-added 6-[F-18]fluoro-L-dopa. The iodonium ylide group in this L-dopa.derivative is nucleophilically substituted by no-carrier-added [F-18]fluoride ion to provide a [F-18]fluoro intermediates which upon acid hydrolysis yielded 6-[F-18]fluoro-L-dopa.

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17-05-2012 дата публикации

Process for the preparation of strontium ranelate

Номер: US20120123131A1
Принадлежит: Individual

The present invention relates to an improved process for the synthesis of strontium ranelate or hydrates thereof. More particularly, the present invention relates to an effective process for the preparation of a compound of formula III, which is a useful intermediate in the synthesis of strontium ranelate. wherein R 1 and R 2 represents substituted or unsubstituted linear or branched C 1 -C 6 alkyl group or C 3 -C 12 cyclic group.

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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

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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24-05-2012 дата публикации

Triterpenoid derivatives useful as antiproliferative agents

Номер: US20120129901A1
Принадлежит: Individual

Formula (I) and (II). The present invention relates to the use of a new lupane derivative of general formula (I) or (II), or a pharmaceutically acceptable salt, crystal form, complex, hydrate, or hydrolysable ester thereof, for preventing and/or inhibiting tumor growth and for treating cancer and other proliferative diseases, more particularly for treating leukemia, liver, cervical, colon and prostate cancer. The present invention also relates to the synthesis of these compounds and to pharmaceutical compositions which contain them.

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24-05-2012 дата публикации

Histidinol dehydrogenase inhibitors, and use thereof as medicaments

Номер: US20120129907A1

Compounds of general formula (I) below: are characterized in that A represents in particular a C 5 -C 10 heterocyclic group, Y represents in particular a single bond, and B represents in particular an aryl or heteroaryl group.

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31-05-2012 дата публикации

Substituted Esters as Cannabinoid-1 Receptor Modulators

Номер: US20120135975A1
Принадлежит: Merck and Co Inc

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

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31-05-2012 дата публикации

Inhibitors of human phosphatidylinositol 3-kinase delta

Номер: US20120135994A1
Принадлежит: Icos Corp

Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3Kδ) activity, and methods of treating diseases, such as disorders of immunity and inflammation, in which PI3Kδ plays a role in leukocyte function are disclosed. Preferably, the methods employ active agents that selectively inhibit PI3Kδ, while not significantly inhibiting activity of other PI3K isoforms. Compounds are provided that inhibit PI3Kδ activity, including compounds that selectively inhibit PI3Kδ activity. Methods of using PI3Kδ inhibitory compounds to inhibit cancer cell growth or proliferation are also provided. Accordingly, the invention provides methods of using PI3Kδ inhibitory compounds to inhibit PI3Kδ-mediated processes in vitro and in vivo.

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07-06-2012 дата публикации

Compounds as bradykinin b1 antagonists

Номер: US20120142695A1
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

Compounds of the formula I wherein n, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 , R 10 , R 11 and X are defined as described in the specification, which are bradykinin B1 antagonists, and their use as medicaments.

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07-06-2012 дата публикации

Method for production of n-(2-amino-1,2-dicyanovinyl)imidates, method for production of n-(2-amino-1,2-dicyanovinyl)formamidine, and method for production of aminoimidazole derivatives

Номер: US20120142957A1
Принадлежит: Nippon Soda Co Ltd

A method for producing N-(2-amino-1,2-dicyanovinyl)formamidine, including the steps of reacting an N-(2-amino-1,2-dicyanovinyl)formimidate and ammonia by adding aqueous ammonia to a solution or suspension of an N-(2-amino-1,2-dicyanovinyl)formimidate in ether, or alternatively directly adding an N-(2-amino-1,2-dicyanovinyl)formimidate or adding a solution or suspension of an N-(2-amino-1,2-dicyanovinyl)formimidate in ether to a liquid containing ether and aqueous ammonia.

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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

Pyrimidine derivatives and analogs, preparation method and use thereof

Номер: US20120178915A1
Автор: Lifeng Xu
Принадлежит: Individual

This invention relates with the arylheterocycle-fused pyrimidines, derivatives and analogs of formula I: or stereoisomers, tautoers, prodrugs, pharmaceutically acceptable salts, complex salts or solvates thereof, wherein: A-cycle is of 3-8 saturated or unsaturated arylheterocycles or aliheterocyclic, containing 1-4 heteroatoms, B-cycle 5-8 member saturated or unsaturated heterocycle containing 1-4 heteroatoms; X 1 , X 2 , X 3 , X 4 are, independently at each occurrence, C, O, S, Se, N and P elements; R 1 , R 2 , R 3 is a substituent containing alicyclic group, arylcycle group, heterocyclic group, adamantane alkyl, adamantane heterocycle, adamantane analogs, sugar group, hydroxyl group, amino acid group or a combination of the above substituents. This invention also relates with their preparative methods and applications.

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19-07-2012 дата публикации

Novel n-halamine acrylamide monomers and copolymers thereof for biocidal coatings

Номер: US20120183494A1
Принадлежит: AUBURN UNIVERSITY

Novel acrylamide and methacrylamide hydantoin monomers which can be reacted with other acrylamide, methacrylamide, acrylate, and methacrylate monomers to form copolymers, which upon halogenation, provide oxidative coatings which are biocidal for use with various materials including, but not limited to, textiles, filters, and latex paints.

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26-07-2012 дата публикации

Diarylthiohydantoin compounds

Номер: US20120190718A1
Принадлежит: UNIVERSITY OF CALIFORNIA

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

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16-08-2012 дата публикации

Chemokine receptor antagonists and use thereof

Номер: US20120207765A1
Принадлежит: Ono Pharmaceutical Co Ltd

A compound represented by general formula (I): a salt thereof, a solvate thereof, or a prodrug thereof wherein all symbols are as defined in the specification has an antagonistic activity against CXCR4 and is therefore useful as a preventive and/or therapeutic agent for CXCR4-mediated diseases, for example, inflammatory and immune diseases (for example, rheumatoid arthritis, arthritis, systemic erythematosus, retinopathy, macular degeneration, pulmonary fibrosis, transplanted organ rejection, etc.), allergic diseases, infections (for example, human immunodeficiency virus infection, acquired immunodeficiency syndrome, etc.), psychoneurotic diseases, cerebral diseases, cardiac/vascular disease (for example, arteriosclerosis, myocardial infarction, stenocardia, cerebral infarction, chronic arterial occlusive disease, etc.), metabolic diseases, and cancerous diseases (for example, cancer, cancer metastasis, etc.), a preventive and/or therapeutic agent for cancerous diseases or infections, or an agent for regeneration therapy.

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16-08-2012 дата публикации

Novel Dihydropyrimidin-2(1H)-one Compounds as S-Nitrosoglutathione Reductase Inhibitors

Номер: US20120208817A1
Автор: Jian Qiu, Xicheng Sun
Принадлежит: N30 Pharmaceuticals Inc

The present invention is directed to novel dihydropyrimidin-2(1H)-one compounds useful as S-nitrosoglutathione reductase (GSNOR) inhibitors, pharmaceutical compositions comprising such compounds, and methods of making and using the same.

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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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23-08-2012 дата публикации

High Stability Diionic Liquid Salts

Номер: US20120215005A1
Принадлежит: Sigma Aldrich Co LLC

The present invention relates to diionic liquid salts of dicationic or dianionic molecules, as well as solvents comprising diionic liquids and the use of diionic liquids as the stationary phase in a gas chromatographic column.

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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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30-08-2012 дата публикации

Amino Acid Compounds

Номер: US20120220642A1
Принадлежит: Thermolife International LLC

Methods for increasing the bioabsorption of amino acids and for preventing the development of nitrate tolerances in a human or animal are disclosed. The methods include administering to the human or animal a pharmaceutically effective amount of an amino acid compound consisting essentially of a nitrate or nitrite of an amino acid selected from the group consisting of Aspartic Acid, Cysteine, Glycine, Lysine, Methionine, Proline, Tyrosine, Phenylalanine, Carnitine, Taurine, and Betaine.

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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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04-10-2012 дата публикации

Compounds, compositions, and methods for the treatment of beta-amyloid diseases and synucleinopathies

Номер: US20120252858A1
Принадлежит: ProteoTech Inc

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

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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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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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27-12-2012 дата публикации

Method for preparing polybiotinylated compounds

Номер: US20120330028A1
Автор: Xavier Lacoux
Принадлежит: Individual

The present invention relates to a novel method for preparing compounds having the formula (I), where X is biotin or Y being biotin or Z being biotin or V being biotin or It also relates to compounds having the formula (I) and their use in clinical and industrial diagnosis.

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03-01-2013 дата публикации

Cyclic amine bace-1 inhibitors having a benzamide substituent

Номер: US20130004518A1
Принадлежит: Merck Sharp and Dohme LLC

Disclosed are compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R 1 is R is —C(O)—N(R 27 )(R 28 ) or and the remaining variables are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease. Also disclosed are pharmaceutical compositions and methods of treating cognitive or neurodegenerative diseases comprising the compounds of formula I in combination with a β-secretase inhibitor other than those of formula I, an HMG-CoA reductase inhibitor, a gamma-secretase inhibitor, a non-steroidal anti-inflammatory agent, an N-methyl-D-aspartate receptor antagonist, a cholinesterase inhibitor or an anti-amyloid antibody.

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31-01-2013 дата публикации

Compounds, compositions, and methods for controlling biofilms

Номер: US20130029981A1
Принадлежит: Katholieke Universiteit Leuven

The invention relates to substituted 2-aminoimidazoles and their imidazo[1,2- a ]pyrimidinium salts precursors being active against biofilm formation. The invention also relates to imidazo[1,2- a ]pyrimidinium salts bearing an azidoalkyl substituent, and to substituted 2-aminoimidazoles wherein the amino group bears a terminal heterocyclic group such as a triazolyl group which are formed through azide-alkyne Huisgen cycloaddition starting from said imidazo[1,2- a ]pyrimidinium salts bearing an azidoalkyl substituent. The invention also relates to a class of N-(azidoalkyl)pyrimidin-2-amines useful as starting materials for the synthesis of said imidazo[1,2- a ]pyrimidinium salts bearing an azidoalkyl substituent. The invention also relates to antimicrobial compositions that include a microbial biofilm formation inhibiting amount of such substituted 2-aminoimidazoles or imidazo[1,2- a ]pyrimidinium salts in combination with excipients. Methods for inhibiting or controlling microbial biofilm formation in a plant, a body part of a human or an animal, or a surface with which a human or an animal may come into contact are also disclosed.

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21-02-2013 дата публикации

Compositions and Methods for Enhancing Proteasome Activity

Номер: US20130045992A1
Принадлежит: Harvard College

Proteinopathies result from the proteasome not acting efficiently enough to eliminate harmful proteins and prevent the formation of the pathogenic aggregates. As described herein, inhibition of proteasome-associated deubiquitinase Usp 14 results in increased proteasome efficiency. The present invention therefore provides novel compositions and methods for inhibition of Usp14, enhancement of proteasome activity and treatment of proteinopathies.

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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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04-04-2013 дата публикации

CARBOXYLATION CATALYSTS

Номер: US20130085276A1
Принадлежит:

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

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11-04-2013 дата публикации

ESTER COMPOUND AND USE THEREOF

Номер: US20130090363A1
Автор: Matsuo Noritada
Принадлежит: Sumitomo Chemical Company, Limited

An ester compound represented by formula (1): wherein Rrepresents hydrogen or methyl, Rrepresents hydrogen or C1-C4 alkyl, and Rrepresents hydrogen or C1-C4 alkyl; has an excellent pest control effect and is therefore useful as an active ingredient of a pest control agent. 2. The ester compound according to claim 1 , wherein a relative configuration of the substituent at the 1-position of the cyclopropane ring and the substituent at the 3-position of the cyclopropane ring is a trans configuration in formula (1).3. The ester compound according to claim 1 , wherein an absolute configuration of the 1-position of the cyclopropane ring is an R configuration in formula (1).4. The ester compound according to claim 1 , wherein an absolute configuration of the 1-position of the cyclopropane ring is an R configuration claim 1 , and a relative configuration of the substituent at the 1-position of the cyclopropane ring and the substituent at the 3-position of the cyclopropane ring is a trans configuration in formula (1).5. The ester compound according to claim 1 , wherein a relative configuration of the substituent of the 1′-position existing on the substituent at the 3-position of the cyclopropane ring is Z-configuration in formula (1).6. The ester compound according to claim 1 , wherein an absolute configuration of the 1-position of the cyclopropane ring is an R configuration and a relative configuration of the substituent of the 1′-position existing on the substituent at the 3-position of the cyclopropane ring is Z-configuration in formula (1).7. The ester compound according to claim 1 , wherein an absolute configuration of the 1-position of the cyclopropane ring is an R configuration claim 1 , a relative configuration of the substituent at the 1-position of the cyclopropane ring and the substituent at the 3-position of the cyclopropane ring is a trans configuration claim 1 , and a relative configuration of the substituent of the 1′-position existing on the substituent at ...

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11-04-2013 дата публикации

NOVEL COMPOUNDS AS OPIOID RECEPTOR MODULATORS

Номер: US20130090478A1
Принадлежит:

The present invention is directed to novel opioid receptor modulators of Formula (I). 1. A compound , wherein said compound is 5-({[2-Amino-3-(4-carbamoyl-2 ,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-4 ,5-dihydro-1H-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid.3. A hydrobromic , hydriodic , perchloric , sulfuric , nitric , phosphoric , acetic , propionic , glycolic , lactic , succinic , maleic , fumaric , malic , tartaric , citric , benzoic , mandelic , methanesulfonic , hydroxyethanesulfonic , benzenesulfonic , oxalic , pamoic , 2-naphthalenesulfonic , p-toluenesulfonic , cyclohexanesulfamic , salicylic , saccharinic or trifluoroacetic acid salt of 5-({[2-Amino-3-(4-carbamoyl-2 ,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-4 ,5-dihydro-1H-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid.4. A benzathine , chloroprocaine , choline , diethanolamine , ethylenediamine , meglumine , procaine , aluminum , calcium , lithium , magnesium , potassium , sodium , or zinc salt of 5-({[2-Amino-3-(4-carbamoyl-2 ,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-4 ,5-dihydro-1H-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid. The present application is a divisional of U.S. Ser. No. 12/838,825, filed Jul. 19, 2010, which is a divisional of U.S. Ser. No. 11/877,747, filed Oct. 24, 2007 (now U.S. Pat. No. 7,786,158), which is a continuation of U.S. Ser. No. 11/079,647, filed Mar. 14, 2005 (now U.S. Pat. No. 7,741,356), which claims the benefit of U.S. Provisional App. No. 60/553,342, filed Mar. 14, 2004, the entire contents of each of which are hereby incorporated by reference.The present invention is directed to novel opioid receptor modulators of Formula (I). The invention further relates to methods for preparing such compounds, pharmaceutical compositions containing them, and their use in the treatment of opioid modulated disorders.The opioid receptors were identified in the mid-1970's, and were quickly categorized into three sub-sets of receptors (mu, ...

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18-04-2013 дата публикации

Nilotinib hcl crystalline forms

Номер: US20130096304A1
Принадлежит: Teva Pharmaceutical Industries LTD

Crystalline forms of Nilotinib HCl are described.

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18-04-2013 дата публикации

CERTAIN CHEMICAL ENTITIES, COMPOSITIONS AND METHODS

Номер: US20130096315A1
Принадлежит:

Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of one or more mitotic kinesins are disclosed. 146.-. (canceled)48. The compound of claim 47 , or a pharmaceutically acceptable salt thereof claim 47 , wherein Ris lower alkyl substituted with hydroxy.49. The compound of claim 48 , or a pharmaceutically acceptable salt thereof claim 48 , wherein Ris 2-hydroxyethyl.50. The compound of claim 47 , or a pharmaceutically acceptable salt thereof claim 47 , wherein Ris lower alkyl substituted with optionally substituted amino.51. The compound of claim 50 , or a pharmaceutically acceptable salt thereof claim 50 , wherein Ris lower alkyl substituted 2-dimethylamino-acetylamino.52. The compound of claim 47 , or a pharmaceutically acceptable salt thereof claim 47 , wherein Ris halo.53. The compound of claim 52 , or a pharmaceutically acceptable salt thereof claim 52 , wherein Ris chloro.54. The compound of claim 47 , or a pharmaceutically acceptable salt thereof claim 47 , wherein Ris optionally substituted isopropoxy.55. The compound of claim 54 , or a pharmaceutically acceptable salt thereof claim 54 , wherein Ris 2 claim 54 ,2 claim 54 ,2-trifluoro-1-methyl-ethoxy.56. The compound of claim 47 , or a pharmaceutically acceptable salt thereof claim 47 , wherein Ris chloro and Ris 2 claim 47 ,2 claim 47 ,2-trifluoro-1-methyl-ethoxy.57. The compound of claim 47 , or a pharmaceutically acceptable salt thereof claim 47 , wherein Ris selected from 1-methyl-1H-imidazol-4-yl and 1-ethyl-1H-imidazol-4-yl claim 47 , each optionally substituted with optionally substituted lower alkyl.58. The compound of claim 57 , or a pharmaceutically acceptable salt thereof claim 57 , wherein Ris selected from 1-methyl-1H-imidazol-4-yl and 1-ethyl-1H-imidazol-4-yl claim 57 , each optionally substituted with 1-hydroxy-1-methyl-ethyl.59. The compound of claim 57 , or a pharmaceutically acceptable salt thereof claim 57 , wherein Ris selected from 1- ...

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25-04-2013 дата публикации

OXAZOLE TYROSINE KINASE INHIBITORS

Номер: US20130102592A1
Принадлежит: SAREUM LIMITED

The invention provides a compound which is an amide of the formula (1), or a salt, solvate, N-oxide or tautomer thereof; wherein: a is 0 or 1; b is 0 or 1: provided that the sum of a and b is 0 or 1; T is O or NH Aris a monocyclic or bicyclic 5- to 10-membered aryl or heteroaryl group containing up to 4 heteroatoms selected from O, N and S, and being optionally substituted en by one or more substituents R; ArJs a monocyclic or bicyclic 5- to 10-membered aryl or heteroaryl group containing up to 4 heteroatoms selected from O, N and S and being optionally substituted by one or more substituents R; and Rand Rare as defined in the claims. The compounds are inhibitors of kinases and in particular FLT3, FLT4 and Aurora kinases. 176-. (canceled)85. A compound according to wherein Aris selected from substituted monocyclic 5- and 6-membered aryl and heteroaryl rings containing up to 2 heteroatoms selected from O claim 77 , N and S claim 77 , each of the aryl and heteroaryl rings being optionally substituted by one or more substituents R.86. A compound according to wherein Aris selected from optionally substituted phenyl claim 85 , thiophene claim 85 , furan claim 85 , pyridine and pyrazole rings.87. A compound according to wherein Aris phenyl optionally substituted by one or more substituent groups R.88. A compound according to wherein the aryl or heteroaryl group Aris substituted by 0 claim 77 , 1 or 2 substituents R.89. A compound according to wherein Ris selected from halogen; cyano; or a group R—R;{'sup': aa', 'cc', 'cc', 'cc', 'cc', 'cc', 'cc', 'cc, 'sub': 2', '2', '2, 'Ris a bond, O, CO, OC(O), C(O)O, NRC(O), C(O)NR, NR, OC(O)O, NRC(O)O, OC(O)NR, NRC(O)NR, S, SO, SO, SONR″ or NR″SOwherein'}{'sup': 'bb', 'claim-text': hydrogen; or', {'sup': '3a', 'a 3 to 8-membered non-aromatic carbocyclic or heterocyclic ring containing up to 2 heteroatoms selected from O, N and S and being optionally substituted by one or more substituents R; or'}, {'sup': '3a', 'a 5- or 6-membered ...

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25-04-2013 дата публикации

HAFNIUM COMPLEXES OF HETEROCYCLIC ORGANIC LIGANDS

Номер: US20130102789A1
Принадлежит: Dow Global Technologies LLC

Hafnium complexes of heterocyclic organic ligands having improved solubility in aliphatic hydrocarbon solvents and their use as components of olefin polymerization catalysts as well as novel syntheses of component parts thereof are disclosed. 2. The process of wherein Ris methyl claim 1 , Ris bromo claim 1 , and the reaction is conducted in an organic solvent comprising an aliphatic ether at −80° C. This application is a divisional application of the U.S. patent application Ser. No. 12/299,519, filed on Nov. 4, 2008, entitled “HAFNIUM COMPLEXES OF HETEROCYCLIC ORGANIC LIGANDS,” and which is a 371 national phase of PCT application number PCT/US07/07882, filed on Mar. 29, 2007, which claims the benefit of U.S. Provisional Patent Application No. 60/798,108, filed on May 5, 2006, the teachings of which are incorporated by reference herein, as if reproduced in full hereinbelow.This invention is directed to certain hafnium complexes, to catalyst compositions comprising the same, and to addition polymerization processes, especially olefin polymerization processes, using such hafnium complexes as one component of a coordination polymerization catalyst composition.Advances in polymerization and catalysis have resulted in the capability to produce many new polymers having improved physical and chemical properties useful in a wide variety of superior products and applications. With the development of new catalysts the choice of polymerization-type (solution, slurry, high pressure or gas phase) for producing a particular polymer has been greatly expanded. Also, advances in polymerization technology have provided more efficient, highly productive and economically enhanced processes. Recently, several new disclosures related to metal complexes based on polyvalent metal-centered, heteroaryl donor ligands have published. Among these are U.S. Pat. No. 6,103,657, U.S. Pat. No. 6,320,005, U.S. Pat. No. 6,653,417, U.S. Pat. No. 6,637,660, U.S. Pat. No. 6,906,160, U.S. Pat. No. 6,919, ...

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02-05-2013 дата публикации

HAPTEN CONJUGATES FOR TARGET DETECTION

Номер: US20130109019A1
Принадлежит:

Embodiments of hapten conjugates including a hapten, an optional linker, and a peroxidase-activatable aryl moiety are disclosed. In some embodiments, the peroxidase-activatable aryl moiety is tyramine or a tyramine derivative. Embodiments of methods for making and using the hapten conjugates also are disclosed. In particular embodiments, the hapten conjugates are used in a signal amplification assay. In certain embodiments, the hapten is an oxazole, a pyrazole, a thiazole, a benzofurazan, a triterpene, a urea, a thiourea other than a rhodamine thiourea, a nitroaryl other than dinitrophenyl or trinitrophenyl, a rotenoid, a cyclolignan, a heterobiaryl, an azoaryl, a benzodiazepine, or 7-diethylamino-3-carboxycoumarin. The hapten is coupled to the peroxidase-activatable aryl moiety directly or indirectly via a linker. In certain embodiments, the hapten conjugates are used in multiplexed assays. 1. A hapten conjugate , comprising:a hapten selected from an oxazole, a pyrazole, a thiazole, a benzofurazan, a triterpene, a urea, a thiourea other than a rhodamine thiourea, a nitroaryl other than dinitrophenyl or trinitrophenyl, a rotenoid, a cyclolignan, a heterobiaryl, an azoaryl, a benzodiazepine, 2,3,6,7-tetrahydro-11-oxo-1H,5H,11H-[1]benzopyrano[6,7,8-ij]quinolizine-10-carboxylic acid, or 7-diethylamino-3-carboxycoumarin;a linker; anda tyramine or a tyramine derivative.2. (canceled)6. (canceled)811.-. (canceled)1332.-. (canceled)33. A method , comprising:(a) immobilizing a first peroxidase on a first target in a sample, wherein the first peroxidase is capable of reacting with a peroxidase-activatable aryl moiety;(b) contacting the sample with a solution comprising a first hapten conjugate, the first hapten conjugate comprising a first hapten selected from an oxazole, a pyrazole, a thiazole, a benzofurazan, a triterpene, a urea, a thiourea other than a rhodamine thiourea, a nitroaryl other than dinitrophenyl or trinitrophenyl, a rotenoid, a cyclolignan, a heterobiaryl, an ...

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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

GRP94 INHIBITORS

Номер: US20130109684A1
Принадлежит: University of Kansas

The present disclosure provides a series of compounds which exhibit isoform selective inhibition of GRP94, a homologue of Hsp90 that is localized to the endoplasmic recticulum. Through GRP94 inhibition, these compounds are likely to manifest anti-cancer, anti-inflammatory, anti-metastasis, and immunosuppressive activities, as well as utility in the treatment of neurodegenerative diseases, and diabetes. 4. The compound or pharmaceutically acceptable salt according to whereinV is N;X is CH;Y is CH; andZ is N.5. The compound or pharmaceutically acceptable salt according to wherein Ris F claim 1 , Cl claim 1 , Br claim 1 , or I.6. The compound or pharmaceutically acceptable salt according to wherein Ris Cl;{'sup': '2', 'Ris OH; and'}{'sup': '3', 'Ris OH.'}13. A pharmaceutical composition comprising a compound or salt according to and a pharmaceutically acceptable carrier.14. A method of treating or preventing a GRP94 related disorder in a patient in need thereof comprising administering a therapeutically effective amount of a pharmaceutical composition comprising a compound or salt according to claim 1 , and a pharmaceutically acceptable carrier or excipient to the patient.15. The method according to claim 14 , wherein the GRP94 related disorder is selected from the group consisting of cancer claim 14 , metastasis claim 14 , an inflammatory disorder claim 14 , a neurodegenerative disorder claim 14 , and diabetes. This application claims the benefit of priority to U.S. Provisional Application Ser. No. 61/473,343, filed Apr. 8, 2011, which is hereby incorporated herein by reference.This invention was made with Government support under National Institutes of Health (NIH) Grant Nos. AG18001, GM077480, DK053058 and CA109265, awarded by the National Cancer Institute. The Government has certain rights in this invention.1. Field of the InventionThe present disclosure provides a series of compounds which exhibit isoform selective inhibition of Glucose-related protein 94 (Grp94), ...

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02-05-2013 дата публикации

HETERO-SUBSTITUTED ACETANILIDE DERIVATIVES AS ANALGESIC AGENTS

Номер: US20130109863A1
Принадлежит: Janssen Pharmaceutica N.V.

Hetero-substituted acetanilide derivatives are disclosed as analgesic agents. The compounds of the invention are useful in methods for treating a disease or condition in a mammal characterized by pain and/or fever. 123-. (canceled)251. A compound of claim wherein Rand Rtaken together form an optionally substituted imidazole and enantiomers , diastereomers , tautomers , or pharmaceutically acceptable salts thereof.26. A compound selected from the group consisting of:pyridine-2-carboxylic acid (4-hydroxy-phenyl)-amide;5-Methyl-1H-pyrazole-3-carboxylic acid (4-hydroxy-phenyl)-amide; and3H-Imidazole-4-carboxylic acid (4-hydroxy-phenyl)-amide;and enantiomers, diastereomers, tautomers, or pharmaceutically acceptable salts thereof.27. A compound of claim 26 , wherein the compound is pyridine-2-carboxylic acid (4-hydroxy-phenyl)-amide and enantiomers claim 26 , diastereomers claim 26 , tautomers claim 26 , or pharmaceutically acceptable salts thereof.28. A compound of claim 26 , wherein the compound is 5-Methyl-1H-pyrazole-3-carboxylic acid (4-hydroxy-phenyl)-amide and enantiomers claim 26 , diastereomers claim 26 , tautomers claim 26 , or pharmaceutically acceptable salts thereof.30. A composition of claim 29 , wherein Rand Rtaken together form an optionally substituted imidazole and enantiomers claim 29 , diastereomers claim 29 , tautomers claim 29 , or pharmaceutically acceptable salts thereof.31. A composition comprising a compound selected from the group consisting of:pyridine-2-carboxylic acid (4-hydroxy-phenyl)-amide;5-Methyl-1H-pyrazole-3-carboxylic acid (4-hydroxy-phenyl)-amide; and3H-Imidazole-4-carboxylic acid (4-hydroxy-phenyl)-amide;and enantiomers, diastereomers, tautomers, or pharmaceutically acceptable salts thereof.32. The composition of wherein the compound is pyridine-2-carboxylic acid (4-hydroxy-phenyl)-amide and enantiomers claim 31 , diastereomers claim 31 , tautomers claim 31 , or pharmaceutically acceptable salts thereof.33. The composition of ...

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02-05-2013 дата публикации

METHODS OF PREPARING 1-(4-((1R,2S,3R)-1,2,3,4-TETRAHYDROXYBUTYL)-1H-IMIDAZOL-2-YL)ETHANONE

Номер: US20130109865A1
Автор: Wu Wenxue
Принадлежит:

Methods of preparing 1-(4-((1R,2S,3R)-1,2,3,4-tetrahydroxybutyl)-1H-imidazol-2-yl)ethanone and derivatives thereof are disclosed. 1. A method of preparing 1-(4-((1R ,2S ,3R)-1 ,2 ,3 ,4-tetrahydroxybutyl)-1H-imidazol-2-yl)ethanone , which comprises:contacting 2-ethoxyacrylimidate with a weak acid salt of D-glucosamine to provide a first mixture;contacting the first mixture with a base to provide a second mixture;adding an aqueous acid to the second mixture to provide a third mixture;maintaining the third mixture at a temperature of greater than 30° C. for at least 0.5 hours; andisolating 1-(4-((1R,2S,3R)-1,2,3,4-tetrahydroxybutyl)-1H-imidazol-2-yl)ethanone from the third mixture.2. The method of claim 1 , wherein the weak acid salt of D-glucosamine is D-glucosamine acetate.3. The method of claim 2 , wherein the base is an alkaline or alkaline earth metal alkoxide claim 2 , hydroxide claim 2 , carbonate claim 2 , phosphate claim 2 , or trialkylamine.4. The method of claim 3 , wherein the base is methoxide.5. The method of claim 1 , wherein the first mixture is maintained at a temperature of greater than 10° C. for at least 0.5 hours.6. The method of claim 1 , wherein the second mixture is maintained at a temperature of greater than 5° C. for at least 1 hour.7. The method of claim 1 , wherein the third mixture is maintained at a temperature of greater than 50° C. claim 1 , for at least 0.5 hours.8. The method of claim 1 , wherein the aqueous acid has a pKof from 0 to 10.9. The method of claim 8 , wherein the aqueous acid is formic claim 8 , acetic claim 8 , or trichloroacetic acid.10. The method of claim 9 , wherein the aqueous acid is acetic acid.11. The method of claim 1 , wherein the 1-(4-((1R claim 1 ,2S claim 1 ,3R)-1 claim 1 ,2 claim 1 ,3 claim 1 ,4-tetrahydroxybutyl)-1H-imidazol-2-yl)ethanone is isolated by filtering a slurry prepared by concentrating claim 1 , cooling and/or diluting the third mixture with water.12. (canceled)13. The method of claim 1 , wherein ...

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02-05-2013 дата публикации

AMIDE DERIVATIVES OF N-UREA SUBSTITUTED AMINO ACIDS AS FORMYL PEPTIDE RECEPTOR LIKE-1 (FPRL-1) RECEPTOR MODULATORS

Номер: US20130109866A1
Принадлежит: ALLERGAN, INC.

The present invention relates to novel amide derivatives of N-urea substituted amino acids, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor. 2. A compound according to claim 1 , wherein:a is 1 and b is 0.3. A compound according to claim 1 , wherein:a is 1 and b is 0; and{'sup': 5', '14, 'sub': 'n', 'Ris —S(O)R.'}4. A compound according to claim 1 , wherein:a is 1 and b is 0; and{'sup': '5', 'sub': '3', 'Ris —CF.'}5) A compound according to claim 1 , wherein:a is 1 and b is 0; and{'sup': '5', 'Ris halogen.'}6. A compound according to claim 1 , wherein:a is 1 and b is 0;{'sup': 1', '11', '12', '13, 'sub': '1-8', 'Ris optionally substituted Calkyl, —NRRor —OR;'}{'sup': '2', 'sub': '1-8', 'Ris optionally substituted Calkyl;'}{'sup': 3', '15', '13', '11', '12, 'sub': '1-8', 'Ris hydrogen, optionally substituted Calkyl, halogen, —COOR, —OR, —NRR;'}{'sup': 4', '15', '13', '11', '12, 'sub': '1-8', 'Ris hydrogen, optionally substituted Calkyl, halogen, —COOR, —OR, —NRR;'}{'sup': 5', '14, 'sub': 3', 'n, 'Ris halogen, —CFor —S(O)R;'}n is 0, 1 or 2;{'sup': 6', '15', '13', '11', '−12, 'sub': '1-8', 'Ris hydrogen, optionally substituted Calkyl, halogen, —COOR, —OR, —NRR;'}{'sup': 7', '15', '13', '11', '12, 'sub': '1-8', 'Ris hydrogen, optionally substituted Calkyl, halogen, —COOR, —OR, —NRR;'}{'sup': '8', 'sub': '1-8', 'Ris hydrogen or optionally substituted Calkyl;'}{'sup': '9', 'sub': 1-8', '6-10, 'Ris hydrogen, optionally substituted Calkyl or optionally substituted Caryl;'}{'sup': '10', 'sub': '1-8', 'Ris hydrogen or optionally substituted C;'}{'sup': '11', 'sub': '1-8', 'Ris hydrogen or optionally substituted Calkyl;'}{'sup': '12', 'sub': '1-8', 'Ris hydrogen or optionally substituted Calkyl;'}{'sup': '13', 'sub': '1-8', 'Ris hydrogen or optionally substituted Calkyl;'}{'sup': '14', 'sub': '1-8', 'Ris hydrogen or optionally substituted Calkyl; ...

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09-05-2013 дата публикации

Cyclic n,n'-diarylthioureas and n,n'-diarylureas - androgen receptor antagonists, anticancer agent, method for preparation and use thereof

Номер: US20130116269A1

The present invention relates to novel cyclic N,N′-diarylureas and N,N′-diarylthioureas—androgen receptor antagonists, anti-cancer agent, pharmaceutical composition, medicament, and method for treatment of cancerous diseases, among them prostate cancer. Cyclic N,N′-diarylthioureas or N,N′-diarylureas of the general formula 1, their optical (R)- and (S)-isomers and pharmaceutically acceptable salts thereof exhibiting properties of androgen receptor antagonists have been proposed, wherein: X represents oxygen or sulfur; m=0 or 1; R1 represents C 1 -C 3 alkyl; R2 and R3 represent hydrogen; or R2 and R3 together with C-atom they are attached to form C═O group; R4 and R5 represent hydrogen; or R4 represents hydrogen, R5 represents methyl; or R4 represents methyl, R5 represents CH 2 R6 group in which R6 represents C 1 -C 3 alkoxycarbonyl, carboxyl, hydroxyl group optionally substituted with methyl or benzyl; or R4 and R5 together with C-atom they are attached to form 5- or 6-membered heterocycle comprising at least one oxygen atom or nitrogen atom optionally substituted with methyl; or R4 and R5 together with C-atom they are attached to form NH group.

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09-05-2013 дата публикации

Chemical Compounds

Номер: US20130116285A1
Принадлежит: PFIZER LIMITED

The invention relates to sulfonamide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to a new sulfonamide Nav1.7 inhibitors of formula 10 (I):(I) or a pharmaceutically acceptable salt thereof, wherein Z, R1, R2, R3, R4 and R5 are as defined in the description. Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain. 2. A compound according to wherein Z is phenyl optionally independently substituted by one to three substituents selected from Yand Y.3. A compound according to wherein Z is phenyl optionally independently substituted by one or two substituents selected from Yand Y.4. A compound according to wherein Z is phenyl para-substituted by Y.5. A compound according to wherein Z is a 6-membered heteroaryl comprising one to three nitrogen atoms claim 1 , said heteroaryl being optionally independently substituted by one to three substituents selected from Yand Y.6. A compound according to wherein Z is pyridyl optionally independently substituted by one to three substituents selected from Yand Y.7. A compound according to wherein Z is pyridyl optionally independently substituted by one or two substituents selected from Yand Y.9. A compound according to wherein said pyridyl is 2-substituted or claim 8 , where di-substituted claim 8 , 2- and 3-substituted.10. A compound according to wherein Ris (C-C)alkyl or (C-C)cycloalkyl.11. A compound according to wherein R claim 1 , Rand Rare independently H or F.12. A compound according to wherein Ris (i) phenyl optionally substituted by one or two substituents independently selected from CN claim 1 , Cl claim 1 , F and R; or (ii) a 5- or 6-membered heteroaryl comprising one or two nitrogen atoms claim 1 , said heteroaryl being optionally substituted by one or two substituents selected from F claim 1 , Cl claim 1 , CN and R.13. A compound ...

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09-05-2013 дата публикации

PROCESS AND INTERMEDIATES FOR PREPARING INTEGRASE INHIBITORS

Номер: US20130116437A1
Принадлежит: Gilead Sciences, Inc.

The invention provides synthetic processes and synthetic intermediates that can be used to prepare 4-oxoquinolone compounds having useful integrase inhibiting properties. 19-. (canceled)11. The method of wherein the compound of formula 3 is converted to the compound of formula 4 by treatment with a silane reducing agent in the presence of an acid.12. The method of wherein the silane reducing agent is triethylsilane and the acid is trifluoroacetic acid.19. The method of wherein the compound of formula 9 is converted to the compound of formula 10 by treatment with a base.2023-. (canceled) This application is a continuation of Ser. No. 12/892,682, filed on 28 Sep. 2010, which is a continuation of Ser. No. 11/853,606, filed on 11 Sep. 2007, now U.S. Pat. No. 7,825,252, granted on 2 Nov. 2010, and claims priority under 35 U.S.C. 119(e) from U.S. Provisional Patent Application No. 60/844,020 filed 12 Sep. 2006, and from U.S. Provisional Patent Application No. 60/905,365 filed 7 Mar. 2007.International Patent Application Publication Number WO 2004/046115 provides certain 4-oxoquinolone compounds that are useful as HIV integrase inhibitors. The compounds are reported to be useful as anti-HIV agents.International Patent Application Publication Number WO 2005/113508 provides certain specific crystalline forms of one of these 4-oxoquinolone compounds, 6-(3-chloro-2-fluorobenzyl)-1-[(S)-1-hydroxymethyl-2-methylpropyl]-7-methoxy-4-oxo-1,4-dihydroquinolone-3-carboxylic acid. The specific crystalline forms are reported to have superior physical and chemical stability compared to other physical forms of the compound.There is currently a need for improved methods for preparing the 4-oxoquinolone compounds reported in International Patent Application Publication Number WO 2004/046115 and in International Patent Application Publication Number WO 2005/113508. In particular, there is a need for new synthetic methods that are simpler or less expensive to carry out, that provide an ...

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16-05-2013 дата публикации

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

Номер: US20130123215A1
Принадлежит: ALLERGAN, INC.

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

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16-05-2013 дата публикации

SUBSTITUTED IMIDAZOLONES, COMPOSITIONS CONTAINING SUCH COMPOUNDS AND METHODS OF USE

Номер: US20130123315A1
Принадлежит:

The present invention relates to compounds of the general structure shown in Formula (A): (A): and includes pharmaceutically acceptable salts, solvates, esters, prodrugs, tautomers, and isomers of said compounds. Pharmaceutical compositions and methods of treatment are also included. 2. A compound in accordance with wherein each V is independently selected from the group consisting of: Calkyl and cycloalkyl.3. A compound in accordance with wherein:G is selected from the group consisting of:{'sub': 2', '2, '(1a) hydrogen, halo, —NH, —OH, COH, cyano;'}{'sup': '1', '(2a) cycloalkyl, —O-cycloalkyl, —N(R)-cycloalkyl;'}{'sup': '1', '(3a) heterocycloalkyl, —O-heterocycloalkyl, —N(R)-heterocycloalkyl;'}{'sup': '1', '(6a) alkyl, —O-alkyl and —N(R)alkyl;'}{'sup': '1', '(7a) heteroalkyl, —O-heteroalkyl, —N(R)-heteroalkyl;'}{'sup': '1', '(8a) alkenyl, —O-alkenyl, —N(R)-alkenyl,'}{'sup': '1', '(9a) alkynyl, —O-alkynyl, —N(R)-alkynyl;'}{'sub': '2', 'sup': 1', '21, '(10a) aryl, —O—aryl, —C(O)-aryl, —S-aryl, —S(O)-aryl, —S(O)-aryl, —N(R)-aryl, —C(O)—N(R)-aryl;'}{'sub': '2', 'sup': 1', '21, '(11a) heteroaryl, —O-heteroaryl, —C(O)-heteroaryl, —S-heteroaryl, —S(O)-heteroaryl, —S(O)-heteroaryl, —N(R)-heteroaryl, —C(O)—N(R)-heteroaryl;'}wherein said heteroalkyl, heterocycloalkyl, heterocycloalkenyl, and heteroaryl of G are connected through any available carbon or heteroatom,{'sup': '2', 'and wherein said alkyl, heteroalkyl, cycloalkyl, heterocycloalkyl, aryl, said heteroaryl, alkenyl, alkynyl, cycloalkenyl, and heterocycloalkenyl of G are unsubstituted or substituted with one or more groups independently selected from R.'}4. A compound in accordance with wherein G represents a phenyl group optionally substituted with 1-3 groups selected from halo claim 1 , Calkyl claim 1 , Calkoxy claim 1 , haloCalkyl and haloCalkoxy claim 1 , or with one phenyl ring that is optionally substituted with 1-3 halo atoms.5. A compound in accordance with wherein Lis selected from the group consisting of —N( ...

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16-05-2013 дата публикации

NOVEL CATIONIC LIPIDS AND METHODS OF USE THEREOF

Номер: US20130123338A1
Принадлежит: Protiva Biotherapeutics, Inc.

The present invention provides compositions and methods for the delivery of therapeutic agents to cells. In particular, these include novel cationic lipids and nucleic acid-lipid particles that provide efficient encapsulation of nucleic acids and efficient delivery of the encapsulated nucleic acid to cells in vivo. The compositions of the present invention are highly potent, thereby allowing effective knock-down of a specific target protein at relatively low doses. In addition, the compositions and methods of the present invention are less toxic and provide a greater therapeutic index compared to compositions and methods previously known in the art. 2. The cationic lipid of claim 1 , wherein Rand Rare independently selected from the group consisting of a methyl group and an ethyl group.3. The cationic lipid of claim 1 , wherein Rand Rare both methyl groups.4. The cationic lipid of claim 1 , wherein Rand Rare joined to form an optionally substituted heterocyclic ring having from 2 to 5 carbon atoms and from 1 to 3 heteroatoms selected from the group consisting of nitrogen (N) claim 1 , oxygen (O) claim 1 , sulfur (S) claim 1 , and combinations thereof.5. The cationic lipid of claim 1 , wherein X is O claim 1 , C(O)O claim 1 , C(O)N(R) claim 1 , N(R)C(O)O claim 1 , or C(O)S.6. The cationic lipid of claim 1 , wherein Ris selected from the group consisting of hydrogen (H) and an optionally substituted methyl group claim 1 , ethyl group claim 1 , or C-Calkyl claim 1 , alkenyl claim 1 , or alkynyl group.7. The cationic lipid of claim 1 , wherein X is an optionally substituted heterocyclic ring having from 2 to 5 carbon atoms and from 1 to 3 heteroatoms selected from the group consisting of nitrogen (N) claim 1 , oxygen (O) claim 1 , sulfur (S) claim 1 , and combinations thereof.8. The cationic lipid of claim 1 , wherein Y is (CH)and n is 0 claim 1 , 1 claim 1 , 2 claim 1 , 3 claim 1 , 4 claim 1 , 5 claim 1 , or 6.9. The cationic lipid of claim 8 , wherein n is 2 claim 8 , ...

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16-05-2013 дата публикации

PROCESS FOR THE SYNTHESIS OF SUBSTITUTED UREA COMPOUNDS

Номер: US20130123493A1
Принадлежит: BIAL - PORTELA & CA, S.A.

A process for preparing a substitute urea of Formula (II) or Formula (I), or a pharmaceutically acceptable salt or ester thereof, Formula (II): Formula (I): the process comprising the reaction of a carbamate of Formula (II′): or formula (I′): with a primary or secondary amine of the formula: R1R2NH, wherein ring A, and R1, R2, R5, V, W, X, Y and Z are as defined herein. 3. A process according to or , wherein the compound has the Formula IIa , and wherein the carbamate of Formula II′ has a corresponding structure in which the —NR1R2 group of Formula IIa is replaced by the —C(O)O-Ph-J group of Formula II′.4. The process according to claim 3 , wherein the compound is of Formula IIa claim 3 , and wherein:{'sub': '1-4', 'R1 is selected from H and Calkyl,'}{'sub': 1-6', '3-10', '1-6', '1-6', '1-6', '3-10', '1-6', '2', '2', '2', '2', '2', '2', '2', '2', '3', '2', '2', '2', '1-6', '1-6', '3-8, 'R2 is selected from Calkyl, aryl, heteroaryl, heterocyclyl, Ccycloalkyl, aryl Calkyl, heteroaryl Calkyl, heterocyclyl Calkyl and Ccycloalkyl Calkyl, each of which may optionally be substituted with one or more groups selected from R2a, halogen, OH, OR2a, OCOR2a, SH, SR2a, SCOR2a, NH, NHR2a, NHSONH, NHSOR2a, NR2aCOR2b, NHC(NH)NH, NHCOR2a, NR2aR2b, COR2a, CSR2a, CN, COOH, COOR2a, CONH, CONHOH, CONHR2a, CONHOR2a, C(NOH)NH, SOR2a, SOH, SONH, CONR2aR2b, SONR2aR2b, wherein R2a and R2b are independently selected from Calkyl, substituted Calkyl, aryl, heteroaryl, Ccycloalkyl and heterocyclyl, or R2a and R2b, together with the heteroatom to which they are joined, can form heterocyclyl,'}{'sub': 1-6', '1-6', '3-8', '2', '2', '2', '2', '2', '2', '2', '2', '3', '2', '2', '2', '1-6', '1-6', '3-8, 'wherein, when the substituent of R2 is Calkyl, substituted Calkyl, aryl, heteroaryl, Ccycloalkyl, heterocyclyl or a group containing one or more of these moieties, each of these moieties may optionally be substituted with one or more groups selected from R2c, halogen, OH, OR2c, OCOR2c, SH, SR2c, SCOR2c, ...

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23-05-2013 дата публикации

Graft polymer to which combined nitrogen molecules are grafted

Номер: US20130131279A1

The present invention relates to a modified polymer obtained by grafting of a compound comprising at least one group Q and at least one group A, bonded together by at least, and preferably, one “spacer” group Sp in which: Q comprises a dipole containing at least, and preferably, one nitrogen atom, capable of being grafted onto the polymer chain by [1,3]-dipolar cycloaddition, A comprises an associative group comprising at least one nitrogen atom, Sp is an atom or a group of atoms forming a bond between Q and A.

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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

COMBRETASTATIN ANALOGS FOR USE IN THE TREATMENT OF CANCER

Номер: US20130137740A1
Принадлежит:

The present invention relates to specific analogs of combretastatin, in particular the compounds of formula (I) as described and defined herein, and pharmaceutical compositions comprising the compounds, as well as their medical use, in particular in the treatment or prevention of cancer, including multidrug-resistant cancer. 2. The compound of claim 1 , wherein Ris selected from —Cl claim 1 , —Br claim 1 , or —NH.3. The compound of claim 1 , wherein Ris selected from hydrogen claim 1 , halogen claim 1 , —OH claim 1 , or —NH.4. The compound of claim 1 , wherein Ris selected from —O—CH claim 1 , —O—CH—CH claim 1 , or —N(CH).5. The compound of claim 1 , wherein Ris selected from —O—CHor —N(CH).6. The compound of claim 1 , wherein Rand Rjointly form a group —C(Cl)═CH—N(CH)—.7. The compound of claim 1 , wherein X is selected from O and N(CH).8. The compound of claim 1 , wherein the compound is selected from 1-methyl-5-(3-amino-4-methoxyphenyl)-4-(3-chloro-4 claim 1 ,5-dimethoxyphenyl)-imidazole claim 1 , 1-methyl-5-(3-amino-4-methoxyphenyl)-4-(3-bromo-4 claim 1 ,5-dimethoxyphenyl)-imidazole claim 1 , 1-methyl-5-(3-amino-4-ethoxyphenyl)-4-(3-chloro-4 claim 1 ,5-dimethoxyphenyl)-imidazole or 1-methyl-5-(3-amino-4-ethoxyphenyl)-4-(3-bromo-4 claim 1 ,5-dimethoxyphenyl)-imidazole claim 1 , or a pharmaceutically acceptable salt claim 1 , solvate claim 1 , or prodrug thereof.9. The compound of claim 1 , wherein the compound is selected from 1-methyl-4-(3-chloro-4 claim 1 ,5-dimethoxyphenyl)-5-(3-fluoro-4-ethoxyphenyl)-imidazole or 1-methyl-4-(3-bromo-4 claim 1 ,5-dimethoxyphenyl)-5-(3-fluoro-4-ethoxyphenyl)-imidazole claim 1 , or a pharmaceutically acceptable salt claim 1 , solvate claim 1 , or prodrug thereof.10. The compound of claim 1 , wherein the compound is selected from 1-methyl-4-(3-amino-4 claim 1 ,5-dimethoxyphenyl)-5-(N-methyl-3-chloroindol-5-yl)-imidazole claim 1 , 1-methyl-4-(3-chloro-4 claim 1 ,5-dimethoxyphenyl)-5-(N-methyl-3-chloroindol-5-yl)-imidazole or 1- ...

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06-06-2013 дата публикации

FUNGICIDAL IMIDAZOLES

Номер: US20130143929A1
Принадлежит: EI DU PONT DE NEMOURS AND COMPANY

Disclosed are compounds of Formula 1, including all stereoisomers, N-oxides, and salts thereof, 2. A compound of wherein:{'sup': 1', '5a', '5a, 'Qis a phenyl ring substituted with 1 to 3 substituents independently selected from R; or a pyridinyl or pyrimidinyl ring optionally substituted with up to 3 substituents independently selected from R;'}{'sup': 2', '5a', '5a, 'Qis a phenyl ring substituted with 1 to 3 substituents independently selected from R; or a pyrazolyl, pyridinyl or pyrimidinyl ring optionally substituted with up to 3 substituents independently selected from Ron carbon atom ring members and methyl on the nitrogen atom ring member;'}{'sup': 1', '2, 'sub': 1', '3, 'Rand Rare each independently H, halogen, cyano, C-Calkyl or cyclopropyl;'}{'sup': 3', '6, 'Ris Br, Cl, F, —ORor —SC≡N;'}{'sup': '4', 'Ris H or methyl;'}{'sup': '5a', 'sub': 1', '2', '1', '2', '1', '2', '1', '2, 'each Ris independently halogen, cyano, C-Calkyl, C-Chaloalkyl, cyclopropyl, C-Calkoxy, C-Calkylthio or -T-U—V;'}{'sup': '6', 'sub': 1', '3', '1', '2', '2', '3', '2', '4', '2', '4', '2', '4', '2', '4', '2', '4, 'Ris H, —CH(═O), C-Calkyl, C-Chaloalkyl, C-Calkoxyalkyl, C-Ccyanoalkyl, C-Calkylcarbonyl, C-Calkoxycarbonyl, C-C(alkylthio)carbonyl or C-Calkoxy(thiocarbonyl);'}each T is independently O, NH or a direct bond;{'sub': 1', '3, 'each U is independently C-Calkylene, wherein up to 1 carbon atom is selected from C(═O);'}{'sup': 8a', '8b', '9, 'each V is independently N(R)(R) or OR;'}{'sup': 8a', '8b, 'each Rand Ris independently H or methyl; and'}{'sup': '9', 'each Ris independently H, methyl or halomethyl.'}3. A compound of wherein{'sup': 1', '5a, 'Qis a phenyl ring substituted with 1 to 3 substituents independently selected from R;'}{'sup': 2', '5a, 'Qis a phenyl ring substituted with 1 to 3 substituents independently selected from R;'}{'sup': 1', '2, 'sub': 1', '2, 'Rand Rare each independently H, Cl, Br, I or C-Calkyl; and'}{'sup': '5a', 'each Ris independently halogen, cyano, ...

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06-06-2013 дата публикации

IMIDO-ACID SALTS AND METHODS OF USE

Номер: US20130143939A1
Автор: Bara Jason E.

Imido-acid salts and compositions containing imido-acid salts are described herein. Methods of their preparation and use are also described herein. The methods of using the imido-acid salts include the reduction of volatile compounds from gas and liquid streams and the delivery of pharmaceutical agents to subjects. 2. The compound of claim 1 , wherein L is substituted or unsubstituted Calkyl.3. The compound of claim 1 , wherein M is substituted or unsubstituted imidazolium or substituted or unsubstituted pyridinium.4. The compound of claim 1 , wherein Rand Rare combined to form substituted or unsubstituted aryl claim 1 , substituted or unsubstituted heteroaryl claim 1 , substituted or unsubstituted cycloalkyl claim 1 , substituted or unsubstituted cycloalkenyl claim 1 , substituted or unsubstituted cycloalkynyl claim 1 , substituted or unsubstituted heterocycloalkyl claim 1 , substituted or unsubstituted heterocycloalkenyl claim 1 , or substituted or unsubstituted heterocycloalkynyl.5. The compound of claim 1 , wherein Xis CO or SO.6. A composition comprising the compound of and a pharmaceutically acceptable carrier.10. The method of claim 9 , wherein the volatile compound is carbon dioxide claim 9 , sulfur dioxide claim 9 , or hydrogen sulfide.11. The method of claim 9 , wherein the system further comprises an amine.12. The method of claim 11 , wherein the amine is selected from the group consisting of primary amines claim 11 , secondary amines claim 11 , tertiary amines claim 11 , cyclic amines claim 11 , or mixtures thereof.14. The method of claim 13 , wherein the primary amine is selected from the group consisting of monoethanolamine claim 13 , diglycolamine claim 13 , 2-amino-2-methylpropanol claim 13 , or mixtures thereof.15. The method of claim 13 , wherein the secondary amine is selected from the group consisting of diethanolamine claim 13 , diisopropanolamine claim 13 , or mixtures thereof.16. The method of claim 13 , wherein the tertiary amine is N- ...

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13-06-2013 дата публикации

CARBOXAMIDE COMPOUNDS AND THEIR USE AS CALPAIN INHIBITORS

Номер: US20130150367A1
Принадлежит:

The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. 2. The carboxamide compound of claim 1 , in which A is C═O.3. The carboxamide compound of claim 1 , in which Q is CHor CHC.4. The carboxamide compound of claim 1 , in which Ris selected from:{'sub': 3', '10, 'sup': '1a', 'C-C-alkyl which is unsubstituted or may be partly or completely halogenated and/or have substituents R,'}{'sub': 1', '4', '1', '4, 'sup': '1c', 'phenyl-C-C-alkyl and hetaryl-C-C-alkyl, where phenyl and hetaryl in the last 2 radicals mentioned may be unsubstituted or carry 1, 2, 3 or 4 identical or different radicals R.'}5. The carboxamide compound of claim 1 , in which Ris phenyl claim 1 , which is unsubstituted or carries 1 claim 1 , 2 claim 1 , 3 or 4 identical or different radicals R.7. The carboxamide compound of claim 6 , in which X is C(O)—NH.8. The carboxamide compound of claim 6 , in which X is C(O)—NHR claim 6 , where Ris CN claim 6 , C-C-alkyl claim 6 , C-C-haloalkyl claim 6 , C-C-alkyl which has 1 claim 6 , 2 or 3 substituents R claim 6 , C-C-alkenyl claim 6 , C-C-alkynyl claim 6 , C-C-cycloalkyl claim 6 , C-C-cycloalkyl-C-C-alkyl claim 6 , C-C-heterocycloalkyl-C-C-alkyl claim 6 , C-C-alkoxy-C-C-alkyl claim 6 , aryl claim 6 , hetaryl claim 6 , aryl-C-C-alkyl or hetaryl-C-C-alkyl claim 6 , where aryl and hetaryl in the last 4 radicals mentioned are unsubstituted or have 1 claim 6 , 2 or 3 substituents R.9. The carboxamide compound of claim 8 , in which Ris C-C-alkyl claim 8 , C-C-cycloalkyl claim 8 , phenyl-C-C-alkyl or hetaryl-C-C-alkyl claim 8 , where aryl and hetaryl in the last 4 radicals mentioned are unsubstituted or have 1 claim 8 , 2 or 3 substituents Rand hetaryl is a 5- or 6- ...

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20-06-2013 дата публикации

AMINO ACID-, PEPTIDE-AND POLYPEPTIDE-LIPIDS, ISOMERS, COMPOSITIONS, AND USES THEREOF

Номер: US20130158021A1
Принадлежит: Massachusetts Institute of Technology

Described herein are compounds and compositions characterized, in certain embodiments, by conjugation of various groups, such as lipophilic groups, to an amino or amide group of an amino acid, a linear or cyclic peptide, a linear or cyclic polypeptide, or structural isomer thereof, to provide compounds of the present invention, collectively referred to herein as “APPLs”. Such APPLs are deemed useful for a variety of applications, such as, for example, improved nucleotide delivery. Exemplary APPLs include, but are not limited to, compounds of Formula (I), (II), (III), (IV), (V), and (VI), and salts thereof, as described herein: 2. (canceled)3. The compound of claim 1 , wherein each instance of Q is O.4. The compound of claim 1 , wherein at least one instance of Ris H.5. The compound of claim 1 , wherein Ris a group of formula (iv).6. The compound of claim 1 , wherein L is an optionally substituted alkylene.811-. (canceled)1534-. (canceled)3750-. (canceled)5359-. (canceled)61. (canceled)62. The composition of claim 60 , wherein the composition is a pharmaceutical composition claim 60 , a cosmetic composition claim 60 , a nutraceutical composition claim 60 , or a composition with non-medical application.6377-. (canceled)79. The method of claim 78 , wherein the desired property is solubility in water claim 78 , solubility at different pH claim 78 , ability to bind polynucleotides claim 78 , ability to bind heparin claim 78 , ability to bind small molecules claim 78 , ability to bind protein claim 78 , ability to form microparticles claim 78 , ability to increase transfection efficiency claim 78 , ability to support cell growth claim 78 , ability to support cell attachment claim 78 , ability to support tissue growth claim 78 , and/or intracellular delivery of the APPL and/or an agent complexed or attached thereto to aid in bioprocessing.81. The method of claim 80 , wherein the disease claim 80 , disorder claim 80 , or condition is selected from the group consisting of ...

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20-06-2013 дата публикации

METRONIDAZOLE ESTERS FOR TREATING ROSACEA

Номер: US20130158090A1
Принадлежит: GALDERMA RESEARCH & DEVELOPMENT

A compound of formula (I): 2. The method as defined in claim 1 , for treating rosacea.3. (canceled)4. The method as defined in claim 1 , wherein the salt of the compound of formula (I) or of an enantiomer thereof is a salt of the compound or an enantiomer thereof with a pharmaceutically acceptable acid.5. The method as defined in claim 4 , wherein the pharmaceutically acceptable acid is selected from the group consisting of:a) a pharmaceutically acceptable inorganic acid; andb) a pharmaceutically acceptable organic acid.6. The method as defined in claim 1 , wherein the compound is selected from the group consisting of a compound of formula (I) claim 1 , a hydrochloride of the compound of formula (I) claim 1 , a citrate of the compound of formula (I) claim 1 , a salicylate of the compound of formula (I) claim 1 , a benzoate of the compound of formula (I) claim 1 , and an S enantiomer of any one of these compounds.7. The method as defined in claim 1 , wherein the compound is 2-(2-methyl-5-nitroimidazol-1-yl)ethyl (S)-2-(4-isobutylphenyl)propionate.8. The method as defined in claim 1 , wherein the compound is in the form of a pharmaceutical composition for topical application.9. The method as defined in claim 8 , wherein the pharmaceutical composition is in the form of a solution claim 8 , a gel or an emulsion.10. The method as defined in claim 8 , wherein the compound is present in an amount of 0.001% to 10% by weight relative to the total weight of the composition.12. The method as defined in claim 5 , wherein the pharmaceutically acceptable inorganic acid is selected from the group consisting of hydrochloric acid claim 5 , sulfuric acid claim 5 , phosphoric acid claim 5 , nitric acid claim 5 , and hydrobromic acid.13. The method as defined in claim 5 , wherein the pharmaceutically acceptable organic acid is selected from the group consisting of acetic acid claim 5 , tartaric acid claim 5 , maleic acid claim 5 , hydroxymaleic acid claim 5 , fumaric acid claim 5 , ...

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27-06-2013 дата публикации

SULFUR DERIVATIVES AS CHEMOKINE RECEPTOR MODULATORS

Номер: US20130165460A1
Принадлежит: ALLERGAN, INC.

The present invention relates to novel sulfur derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors. 2. A compound according to claim 1 , wherein:{'sup': '5', 'Ris S.'}3. A compound according to claim 1 , wherein:{'sup': '5', 'Ris —S(O)—.'}4. A compound according to claim 1 , wherein:{'sup': '5', 'sub': '2', 'Ris —S(O)—.'}5. A compound according to claim 1 , wherein:{'sup': '2', 'Ris methyl, isopropyl, 2-hydroxyethyl, methylpropionate, 2-methylpyridine, 3-methylpyridine, ethylacetate, N,N-dimethylpropanamide, N-isopropylpropanamide, N-(propan-2-yl)propanamide, propanamide hydroxycyclopent-3-yl, ethyl, N,N-dimethylacetamide, N-methylacetamide, 2-aminoethyl, H-imidazol-2-ylmethyl, 1H-imidazol-4-ylmethyl or ethyl-acetamide.'}6. A compound according to claim 1 , wherein:{'sup': '17', 'sub': '1-6', 'Ris H, substituted or unsubstituted Calkyl or halogen;'}{'sup': '18', 'sub': '1-6', 'Ris H, substituted or unsubstituted Calkyl or halogen;'}{'sup': '7', 'sub': 1-6', '1-6', '3-8, 'Ris halogen, CN, —OCalkyl, substituted or unsubstituted Calkyl or substituted or unsubstituted Ccycloalkyl; and'}{'sup': '8', 'sub': '1-6', 'Ris H, substituted or unsubstituted Calkyl or halogen.'}7. A compound according to claim 1 , wherein:{'sup': '17', 'Ris H;'}{'sup': '18', 'Ris H;'}{'sup': '7', 'sub': '1-6', 'Ris halogen, CN or —OCalkyl; and'}{'sup': '8', 'Ris H.'}8. A compound according to claim 1 , wherein:{'sup': '2', 'Ris methyl, isopropyl, 2-hydroxyethyl, methylpropionate, 2-methylpyridine, 3-methylpyridine, ethylacetate, N,N-dimethylpropanamide, N-isopropylpropanamide, N-(propan-2-yl)propanamide, propanamide hydroxycyclopent-3-yl, ethyl, N,N-dimethylacetamide, N-methylacetamide, 2-aminoethyl, H-imidazol-2-ylmethyl, 1H-imidazol-4-ylmethyl or ethyl-acetamide;'}{'sup': '5', 'sub': '2', 'Ris —S—, —S(O)—, or —S(O)—;'}{'sup': '17', 'Ris H;'}{'sup': '18', 'Ris H;'}{'sup': '7', 'sub': '1-6', ' ...

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27-06-2013 дата публикации

Small Molecule Modulators of HIV-1 Capsid Stability and Methods Thereof

Номер: US20130165489A1
Принадлежит:

The present invention includes a method of inhibiting, suppressing or preventing a viral infection in a subject, comprising administering to the subject a pharmaceutical composition comprising one or more of the compounds useful within the invention. 2. The composition of claim 1 , wherein in Formula (III) Rand Rare such that:{'sup': 5', '4, '(i) if ‘a’ is a double bond and ‘b’ is a single bond, then Ris N or CH, and Ris NH or N-alkyl, or'}{'sup': 5', '4, '(ii) if ‘a’ is a single bond and ‘b’ is a double bond, then Ris NH or N-alkyl, and Ris N or CH.'}3. The composition of claim 2 , wherein in Formula (III) Rand Rare such that:{'sup': 5', '4, '(i) if ‘a’ is a double bond and ‘b’ is a single bond, then Ris N, and Ris NH or N-alkyl, or'}{'sup': 5', '4, '(ii) if ‘a’ is a single bond and ‘b’ is a double bond, then Ris NH or N-alkyl, and Ris N.'}4. The composition of claim 1 , wherein said compound is 4-(4 claim 1 ,5-diphenyl-1H-imidazol-2-yl)benzoic acid (CMPD-E) or a salt thereof.5. The composition of claim 1 , further comprising a pharmaceutically acceptable carrier.7. The composition of claim 6 , wherein said compound is 4-(5-(dibenzo[b claim 6 ,d]furan-2-yl)-4-phenyl-1H-imidazol-2-yl)benzoic acid (CMPD-C) or a salt thereof.8. The composition of claim 6 , further comprising a pharmaceutically acceptable carrier.12. The method of claim 9 , wherein in said compound of Formula (III) Rand Rare such that:{'sup': 5', '4, '(i) if ‘a’ is a double bond and ‘b’ is a single bond, then Ris N, and Ris NH or N-alkyl, or'}{'sup': 5', '4, '(ii) if ‘a’ is a single bond and ‘b’ is a double bond, then Ris NH or N-alkyl, and Ris N.'}13. The method of claim 9 , wherein said compound is selected from the group consisting of 4 claim 9 ,4′-(5 claim 9 ,5′-(dibenzo[b claim 9 ,d]furan-2 claim 9 ,8-diyl)bis(4-phenyl-1H-imidazole-5 claim 9 ,2-diyl))dibenzoic acid (CMPD-A) claim 9 , dimethyl 4 claim 9 ,4′-(5 claim 9 ,5′-(dibenzo[b claim 9 ,d]furan-2 claim 9 ,8-diyl)bis(4-phenyl-1H-imidazole-5 ...

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04-07-2013 дата публикации

Novel Imidazolium Salts and Carbene Metal Complexes Based Thereon for Use as Bioanalytical Markers for Biomolecules

Номер: US20130171071A1
Автор: Kuehl Olaf

The present invention relates to imidazolium salts, particularly imidazolium salts of the general formula I as well as the respective carbene metal complexes and their utilisation as bioanalytical tags for biomolecules. 2. Imidazolium salts according to claim 1 , wherein the groups R claim 1 , R claim 1 , and R claim 1 , where applicable claim 1 , are the same or different and chosen from the group of C-C-n-alkyl groups.3. Imidazolium salts according to claim 1 , wherein n claim 1 , m claim 1 , and q claim 1 , where applicable claim 1 , are zero or 1 and b and l are zero.4. Imidazolium salts according to claim 1 , wherein R″ is a C-C-n-alkyl group.7. Carbene metal complexes according to claim 6 , wherein the metal is chosen from the group consisting of copper claim 6 , iron claim 6 , ruthenium claim 6 , nickel claim 6 , and palladium or from the group consisting of technetium claim 6 , rhenium and cobalt.8. Carbene metal complexes according to claim 6 , wherein the ligand L is chosen from the group consisting ofCO;nitrile;isonitrile;nitrosyl;halogenide ion;hydrogen atom;{'sub': 1', '12', '6', '14', '1', '12', '6', '14', '1', '12', '6', '14', '1', '12', '6', '14', '6', '14', '1', '12', '1', '12, 'C-C-alkyl anion, allyl anion, methylallyl anion, benzyl anion, C-C-aryl anion, C-C-alkoxy anion, C-C-aryloxy anion, C-C-heteroalkyl anion, C-C-heteroaryl anion, C-C-heteroalkoxy anion, C-C-heteroaryloxy anion or C-C-heteroaryloxy anion, which is unsubstituted or the same or differently substituted by one or more C-C-alkyl groups or C-C-heteroalkyl groups, whereby the heteroatoms are chosen from the group B, Al, Ga, In, N, P, As, Sb, Bi, Si, Ge, Sn, Pb, O, S, Se, and Te and wherein the anions are unsubstituted or wholly or partially substituted with one or more than one, same, or different heteroatoms from the same group, in the form of functional groups, wherein the cyclic and aromatic systems are single rings or several annelated or isolated rings;'}primary, secondary, ...

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04-07-2013 дата публикации

Cysteine protease inhibitors

Номер: US20130172232A1
Принадлежит: Medivir UK Ltd

Compounds of the formula I wherein R 2a and R 2b are independently H, halo, C 1 -C 4 alkyl, C 1 -C 4 haloalkyl or C 1 -C 4 alkoxy, or R 2a and R 2b together with the carbon atom to which they are attached form a C 3 -C 6 cycloalkyl; R 3 is a C 5 -C 10 alkyl, optionally substituted with 1-3 substituents independently selected from halo, C 1 -C 4 haloalkyl, C 1 -C 4 alkoxy, C 1 -C 4 haloalkoxy; or R 3 is a C 2 -C 4 alkyl chain with at least 2 chloro or 3 fluoro substituents; or R 3 is C 3 -C 7 cycloalkylmethyl, optionally substituted with 1-3 substituents independently selected from C 1 -C 4 alkyl, halo, C 1 -C 4 haloalkyl, C 1 -C 4 alkoxy, C 1 -C 4 haloalkoxy; R 4 is C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, C 1 -C 6 alkoxy, C 1 -C 6 haloalkoxy, C 1 -C 6 alkylamino, C 1 -C 6 dialkylamino or; R 4 is Het or Carbocyclyl, either of which is optionally substituted with 1-3 substituents R 4 is Het, carbocyclyl, C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, C 1 -C 6 alkoxy or C 1 -C 6 haloalkoxy; n is 1, 2 or 3; for the use in the prophylaxis or treatment of a disorder characterised by inappropriate expression or activation of cathepsin S.

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04-07-2013 дата публикации

5-membered heterocycle-based p38 kinase inhibitors

Номер: US20130172352A1
Принадлежит: NOVARTIS AG

Provided are 5-membered heterocycle-based p38 kinase inhibitors. Further provided are pyrazole and imidazole-based p38 kinase, including p38α, and p38β kinase, inhibitors. Pharmaceutical compositions containing the compounds are also provided. Methods of use of the compounds and compositions are also provided, including methods of treatment, prevention, or amelioration of one or more symptoms of p38 kinase mediated diseases and disorders, including, but not limited to, inflammatory diseases and disorders.

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04-07-2013 дата публикации

BASE GENERATOR

Номер: US20130172569A1
Принадлежит: ETERNAL CHEMICAL CO., LTD.

The present invention provides a base generator having the structure of formula (1): 5. The base generator according to claim 1 , wherein R claim 1 , Rand Rare the same or different and are each independently H claim 1 , methyl claim 1 , ethyl claim 1 , n-propyl claim 1 , isopropyl claim 1 , n-butyl claim 1 , isobutyl claim 1 , tert-butyl claim 1 , pentyl claim 1 , hexyl claim 1 , hydroxymethyl claim 1 , hydroxyethyl claim 1 , hydroxypropyl claim 1 , hydroxybutyl claim 1 , hydroxypentyl claim 1 , hydroxyhexyl claim 1 , cyanomethyl claim 1 , cyanoethyl claim 1 , cyanopropyl claim 1 , cyanobutyl claim 1 , cyanopentyl claim 1 , cyanohexyl claim 1 , phenyl claim 1 , benzyl or diphenylmethyl.6. The base generator according to claim 1 , wherein R claim 1 , Rand Rare the same or different and are each independently H claim 1 , methyl claim 1 , ethyl claim 1 , n-propyl or isopropyl.7. The base generator according to claim 1 , wherein the anionic group is selected from a group consisting of halide ion claim 1 , sulfate claim 1 , nitrate claim 1 , phosphate claim 1 , sulfonate claim 1 , carbonate claim 1 , tetrafluoborate claim 1 , borate claim 1 , chlorate claim 1 , iodate claim 1 , hexafluorophosphate claim 1 , perchlorate claim 1 , trifluoromethanesulfonate claim 1 , trifluoroacetate claim 1 , acetate claim 1 , tert-butylcarbonate claim 1 , (CFSO)N and tert-butyloxy.8. The base generator according to claim 1 , wherein the anionic group is a halide ion or tetrafluoroborate.9. The base generator according to claim 1 , which is an optical base generator or a thermal base generator. The present invention relates to a base generator, and particularly to a base generator which exhibits good storage stability, can generate a base by exposure to heating or irradiation of light, and can be used for imidization of a polyimide precursor, promoting crosslinking of epoxy monomers, or crosslinking of polyurethane or polyurea.Polyimide is the first choice among high performance polymer ...

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11-07-2013 дата публикации

Imidazole Derivatives Useful for Controlling Microbial Growth

Номер: US20130177621A1
Принадлежит:

Disclosure is provided for 1,4,5-substituted amino imidazole compounds useful to control microbial growth, compositions including these compounds, devices including these compounds, and methods of using the same. 5. The compound of claim 4 , wherein one of D1 claim 4 , D2 claim 4 , D3 claim 4 , D4 or D5 is C1-C15 alkyl claim 4 , and the others are H.6. The compound of claim 4 , wherein one of D1 claim 4 , D2 claim 4 , D3 claim 4 , D4 or D5 is a C1 claim 4 , C3 claim 4 , C5 claim 4 , C7 claim 4 , C9 or C11 alkyl claim 4 , and the others are H.10. A composition comprising a carrier and an effective amount of the compound of .11. The composition of claim 10 , wherein said composition is an ointment claim 10 , cream claim 10 , lotion claim 10 , paste claim 10 , gel claim 10 , foam claim 10 , spray claim 10 , aerosol claim 10 , or oil.12. A composition comprising the compound of covalently coupled to a substrate.13. A bacterial growth inhibiting coating composition claim 1 , comprising:(a) a film-forming resin;(b) a solvent that disperses said resin;{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, '(c) an effective amount of the compound of , wherein said effective amount of said compound inhibits the growth of bacteria thereon; and'}(d) optionally, at least one pigment.14. A substrate coated with the coating composition of .15. A method of reducing microbial growth on a substrate comprising the step of contacting the compound of to said substrate in an amount effective to reduce said microbial growth.16. The method of claim 15 , wherein said microbial growth is Gram-positive bacterial growth.17Staphylococcus aureus.. The method of claim 15 , wherein said bacterial growth is18Staphylococcus aureus. The method of claim 15 , wherein bacterial growth is methicillin-resistant (MRSA).19. A method for treating a bacterial infection in a subject in need thereof claim 1 , comprising administering to said subject the compound of in an amount effective to reduce a bacterial ...

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11-07-2013 дата публикации

2,4,5-TRISUBSTITUTED IMIDAZOLES AND THEIR USE AS ANTI-MICROBIAL AGENTS

Номер: US20130177632A1
Принадлежит:

The present invention provides therapeutically effective 2,4,5-trisubstituted imidazole compounds, methods of preparing the same, and compositions comprising the compounds alone or in combination with other agents. The present invention further provides for the use of the compounds as anti-microbial agents. The anti-microbial properties of the compounds include anti-bacterial and/or anti-fungal activity. 2. The compound according to claim 1 , wherein R2 and R3 are independently phenyl claim 1 , substituted phenyl claim 1 , naphthyl claim 1 , substituted naphthyl claim 1 , pyridyl claim 1 , thienyl claim 1 , substituted pyridyl claim 1 , or substituted thienyl5. The compound according to claim 4 , wherein said compound is selected from compounds: 5 claim 4 , 6 claim 4 , 7 claim 4 , 8 claim 4 , 9 claim 4 , 10 claim 4 , 11 claim 4 , 13 claim 4 , 17 claim 4 , 19 claim 4 , 20 claim 4 , 21 claim 4 , 23 claim 4 , 25 claim 4 , 26 claim 4 , 27 claim 4 , 28 claim 4 , 29 claim 4 , 31 claim 4 , 32 claim 4 , 33 claim 4 , 34 claim 4 , 35 claim 4 , 36 claim 4 , 42 claim 4 , 43 claim 4 , 48 claim 4 , 49 claim 4 , 51 claim 4 , 54 claim 4 , 55 claim 4 , 56 claim 4 , 75 claim 4 , 83 or 84.6. The compound according to claim 5 , wherein said compound is: 8.7. The compound according to claim 5 , wherein said compound is: 30.9. The anti-microbial composition according to claim 8 , wherein said anti-microbial composition is for inhibiting the growth and/or proliferation of a drug-resistant bacterium and said one or more compounds have anti-bacterial activity.10Staphylococcus aureusEnterococcus.. The anti-microbial composition according to claim 9 , wherein said drug-resistant bacterium is methicillin-resistant cell or vancomycin-resistant11. The anti-microbial composition according to claim 8 , wherein said composition is a liposomal formulation.12. The anti-microbial composition according to claim 8 , wherein said composition is a pharmaceutical formulation.13. The anti-microbial ...

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11-07-2013 дата публикации

MODULATORS OF ATP-BINDING CASSETTE TRANSPORTERS

Номер: US20130178471A1
Принадлежит: Vextex Pharmaceuticals Incorporated

Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention. 2. The compound of claim 1 , wherein two R taken together form —OCFO— claim 1 , Ris H claim 1 , and Ris F.3. The compound of claim 1 , wherein two R taken together form —OCFO— claim 1 , Ris H claim 1 , Ris F claim 1 , and Ris H.4. The compound of claim 1 , wherein two R taken together form —OCFO— claim 1 , Ris H claim 1 , Ris F claim 1 , Ris H claim 1 , and Ris H.5. The compound of claim 1 , wherein two R taken together form —OCFO— claim 1 , Ris H claim 1 , Ris F claim 1 , Ris H claim 1 , and Ris —CHCHN(CH).6. The compound of claim 1 , wherein two R taken together form —OCFO— claim 1 , Ris H claim 1 , Ris F claim 1 , Ris H claim 1 , and Ris —CHCH(OH)CHOH.7. The compound of claim 1 , wherein two R taken together form —OCFO— claim 1 , Ris H claim 1 , Ris F claim 1 , Ris H claim 1 , and Ris (R)—CHCH(OH)CHOH.8. The compound of claim 1 , wherein two R taken together form —OCFO— claim 1 , Ris H claim 1 , Ris F claim 1 , Ris H claim 1 , and Ris (S)—CHCH(OH)CHOH9. The compound of claim 1 , wherein two R taken together form —OCFO— claim 1 , Ris H claim 1 , Ris F claim 1 , Ris H claim 1 , and Rand Rtaken together form a fused pyrrolidine ring.10. The compound of claim 1 , wherein two R taken together form —OCHO— claim 1 , Ris H claim 1 , and Ris F.11. The compound of claim 1 , wherein two R taken together form —OCHO— claim 1 , Ris H claim 1 , Ris F claim 1 , and Ris H.12. The compound of claim 1 , wherein two R taken together form —OCHO— claim 1 , Ris H claim 1 , Ris F claim 1 , Ris H claim 1 , and Ris —CHCH(OH)CHOH.13. The compound of claim 1 , wherein two R taken together form —OCHO— claim 1 , ...

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18-07-2013 дата публикации

THERAPEUTICALLY ACTIVE COMPOSITIONS AND THEIR METHODS OF USE

Номер: US20130184222A1
Принадлежит: AGIOS PHARMACEUTICALS, INC

Provided are methods of treating a cancer characterized by the presence of a mutant allele of IDH1 comprising administering to a subject in need thereof a compound described here. 2. The compound of claim 1 , wherein Ris 3-fluorophenyl.3. The compound of or claim 1 , wherein:{'sup': '1', 'Ris selected from cyclohexyl, cyclopentyl, cycloheptyl, 3,3-difluorocyclobutyl, 4,4,-difluorocyclohexyl, and bicyclo[2.2.1]heptanyl; and'}{'sup': '4', 'Ris selected from 1-(methylmethoxycarbonylamino)ethyl, 1,2,3,4-tetrahydroquinolin-1-yl, 1-ethoxycarbonylpiperidin-2-yl, 1-ethoxycarbonylpyrrolidin-2-yl, 1H-benzimidazol-1-ylmethyl, 1H-indazol-3-ylmethyl, indolin-1-ylmethyl, 1H-indol-3-ylmethyl, 1H-indol-5-ylmethyl, 1H-pyrrolo[2,3-b]pyridine-3-ylmethyl, 1H-pyrrolo[3,2-b]pyridin-3-ylmethyl, 1-methoxycarbonylpiperidin-2-yl, 1-methoxycarbonylpyrrolidin-2-yl, 2-fluoropyridin-3-ylaminomethyl, 2-imino-4-fluoropyridin-1-ylmethyl, 2-methoxyphenylaminomethyl, 2-methyl-1H-benzimidazol-1-ylmethyl, 2-methylimidazol-1-ylmethyl, 2-trifluoromethyl-1H-imidazol-1-yl, 3-cyanophenylaminomethyl, 3-fluoropyridin-2-ylaminomethyl, 3-methoxyphenylaminomethyl, 4-(1,3,4-oxadiazole-2-yl)phenylaminomethyl, 4-(dimethylaminocarbonyloxy)phenylmethyl, 4,5-dichloroimidazol-1-ylmethyl, 4-cyanophenylaminomethyl, 4-fluorophenylaminomethyl, 4-fluoropyridin-2-ylaminomethyl, 4-hydroxyphenylmethyl, 4-methoxycarbonylmorpholin-3-yl, 4-methoxycarbonylpiperazin-1-ylmethyl, 4-methoxyphenylaminomethyl, 4-methylcarbonyloxyphenylmethyl, 5-fluoropyridin-2-aminomethyl, 5-fluoropyridin-2-oxymethyl, 6-fluoropyridin-3-ylaminomethyl, benzomorpholin-4-ylmethyl, methoxycarbonylaminomethyl, methylmethoxycarbonylaminomethyl, methylphenylaminomethyl, phenylaminomethyl, pyridin-2-oxymethyl, pyridin-2-ylaminomethyl, pyridin-2-yloxymethyl, pyridin-3-oxymethyl, pyridin-3-ylmethyl, pyridin-4-ylmethyl, thiazol-4-ylmethyl, and thien-2-ylmethyl.'}4. The compound of claim 1 , wherein the compound is selected from any one of Compound numbers 104 claim ...

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25-07-2013 дата публикации

SULFUR DERIVATIVES AS CHEMOKINE RECEPTOR MODULATORS

Номер: US20130190338A1
Принадлежит: ALLERGAN, INC.

The present invention relates to novel sulfur derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors. 2. A compound according to claim 1 , wherein:{'sup': '5', 'Ris S.'}3. A compound according to claim 1 , wherein:{'sup': '5', 'Ris —S(O)—.'}4. A compound according to claim 1 , wherein:{'sup': '5', 'sub': '2', 'Ris —S(O)—.'}5. A compound according to claim 1 , wherein:{'sup': '1', 'Ris H;'}{'sup': '2', 'sub': 1-6', '3-8', '3-8, 'Ris substituted or unsubstituted Calkyl, substituted or unsubstituted Ccycloalkyl or substituted or unsubstituted Ccycloalkenyl;'}{'sup': '5', 'sub': '2', 'Ris —S—, —S(O)—, or —S(O)—;'}{'sup': '6', 'Ris optionally substituted 1-benzofuran;'}{'sup': '17', 'sub': '1-6', 'Ris H, substituted or unsubstituted Calkyl or halogen;'}{'sup': '18', 'sub': '1-6', 'Ris H, substituted or unsubstituted Calkyl or halogen;'}{'sup': '7', 'sub': 1-6', '1-6', '3-8, 'Ris H, halogen, CN, —OCalkyl, substituted or unsubstituted Calkyl or substituted or unsubstituted Ccycloalkyl; and'}{'sup': '8', 'sub': '1-6', 'Ris H, substituted or unsubstituted Calkyl, CN or halogen.'}6. A compound according to claim 5 , wherein:{'sup': '1', 'Ris H;'}{'sup': '2', 'sub': '1-6', 'Ris substituted or unsubstituted Calkyl;'}{'sup': '5', 'sub': '2', 'Ris —S—, —S(O)—, or —S(O)—;'}{'sup': '6', 'Ris optionally substituted 1-benzofuran;'}{'sup': '17', 'Ris H;'}{'sup': '18', 'Ris H;'}{'sup': '7', 'sub': '1-6', 'Ris H, halogen or Calkyl; and'}{'sup': '8', 'Ris H or CN.'}7. A compound according to claim 6 , wherein:{'sup': '1', 'Ris H;'}{'sup': '2', 'Ris methyl propionate, methyl-2-benzoic acid, methyl-2-methylbenzoate, methyl-3-methylphenylacetamide, methyl-3-methylphenylsulfonamide, methyl acetic acid, methyl-2-methylphenylcarboxylate or propionic acid;'}{'sup': '5', 'sub': '2', 'Ris —S(O)—, S or —S(O)—;'}{'sup': '6', 'Ris optionally substituted 1-benzofuran;'}{'sup': '7', 'Ris chlorine, ...

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25-07-2013 дата публикации

DUAL INHIBITORS OF FARNESYLTRANSFERASE AND GERANYLGERANYLTRANSFERASE I

Номер: US20130190355A1
Принадлежит:

Many GTPases such as Ras, Ral and Rho require post-translational farnestylation or geranylgeranylation for mediating malignant transformation. Dual farnesyltransferase (FT) (FTI) and geranylgeranyltransferase-I (GGT-1) inhibitors (GGTI) were developed as anticancer agents from based on an ethylenediamine scaffold. On the basis of a 4-fold substituted ethylenediamine scaffold, the inhibitors are structurally simple and readily derivatized, facilitating extensive structure-activity relationship studies. The most potent inhibitor is compound exhibited an in vitro hFTase ICvalue of 25 nM and a whole cell H-Ras processing ICvalue of 90 nM. Several of the inhibitors proved highly selective for hFTase over the related prenyltransferase enzyme geranylgeranyltransferase-I (GGTase-I). A crystal structure of an inhibitor cocrystallized with farnesyl pyrophosphate in the active site of rat FTase illustrates that the para-benzonitrile moiety is stabilized by a π-π stacking interaction with the Y361β residue, suggesting an importance of this component of the inhibitors. 2. The composition of claim 1 , wherein the aniline ring comprises a substitution at the ortho position claim 1 , where the substitution is a N or CF.3. The composition of claim 1 , wherein the aniline ring comprises a substitution at the meta position claim 1 , where the substitution is a CF.4. The composition of claim 1 , wherein the aniline ring comprises a bromine at the para position.5. The composition of claim 1 , wherein the aniline ring comprises a cyano in the para position.8. The method of claim 7 , wherein the aniline ring comprises a substitution at the ortho position claim 7 , where the substitution is a N or CF.9. The method of claim 7 , wherein the aniline ring comprises a substitution at the meta position claim 7 , where the substitution is a CF.10. The method of claim 7 , wherein the aniline ring comprises a bromine at the para position.11. The method of claim 7 , wherein the aniline ring ...

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25-07-2013 дата публикации

THERAPEUTIC AGENT FOR NEUROLOGICAL DISEASES

Номер: US20130190363A1
Принадлежит:

An object of the present invention is to provide a pharmaceutical agent useful for treating and preventing neurological disease, having satisfactory solubility and oxidative stress-mediated cell death suppressive activity as well as capable of exhibiting excellent blood-brain barrier permeability. The present invention is directed to an acylaminoimidazole derivative represented by general formula (I) or a salt thereof, and a pharmaceutical and a therapeutic or preventive agent for neurological disease containing the same, as an active ingredient. 2. The acylaminoimidazole derivative or a salt thereof according to claim 1 , wherein Ris a group of formula (Ia) claim 1 , Ris a hydrogen atom and X is a nitrogen atom.3. The acylaminoimidazole derivative or a salt thereof according to claim 1 , wherein the acylaminoimidazole derivative is (2R)-2-(mesityloxy)-N-[4-(pyridin-2-yl)-1H-imidazol-2-yl]propanamide.4. The acylaminoimidazole derivative or a salt thereof according to claim 1 , wherein the acylaminoimidazole derivative is 2-(mesitylamino)-N-[4-(pyridin-2-yl)-1H-imidazol-2-yl]acetamide.5. The acylaminoimidazole derivative or a salt thereof according to claim 1 , wherein the acylaminoimidazole derivative is 2-[mesityl(methyl)amino]-N-[4-(pyridin-2-yl)-1H-imidazol-2-yl]acetamide.6. A pharmaceutical comprising the acylaminoimidazole derivative or a salt thereof according to any one of to claim 1 , as an active ingredient.7. A therapeutic or preventive agent for neurological disease comprising the acylaminoimidazole derivative or a salt thereof according to any one of to claim 1 , as an active ingredient.8. An oxidative stress-mediated cell death suppressant comprising the acylaminoimidazole derivative or a salt thereof according to any one of to claim 1 , as an active ingredient.9. The therapeutic or preventive agent for neurological disease according to claim 7 , wherein the neurological disease is a neurodegenerative disease having cell degeneration due to oxidative ...

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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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25-07-2013 дата публикации

PROCESSES FOR THE SYNTHESIS OF DIARYLTHIOHYDANTOIN AND DIARYLHYDANTOIN COMPOUNDS

Номер: US20130190507A1
Принадлежит:

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

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01-08-2013 дата публикации

METRONIDAZOLE ESTERS FOR TREATING ROSACEA

Номер: US20130197048A1
Принадлежит: GALDERMA RESEARCH & DEVELOPMENT

A compound of formula (I): 2. The compound as defined in claim 1 , wherein the compound is incorporated into a medicament.3. The compound as defined in claim 1 , wherein the compound is effective in treating rosacea.4. The compound as defined in claim 1 , wherein the salt of the compound of formula (I) is a salt of the compound with a pharmaceutically acceptable acid.5. The compound as defined in claim 1 , wherein the pharmaceutically acceptable acid is selected from the group consisting of:a) pharmaceutically acceptable inorganic acid; andb) a pharmaceutically acceptable organic acid.6. The compound as defined in claim 1 , wherein the compound is selected from the group consisting of a compound of formula (I) claim 1 , a hydrochloride of the compound of formula (I) claim 1 , a citrate of the compound of formula (I) claim 1 , a salicylate of the compound of formula (I) and a benzoate of the compound of formula (I).7. The compound as defined in claim 1 , wherein the compound is 2-(2-methyl-5-nitroimidazol-1-yl)ethyl [2-(2 claim 1 ,6-dichlorophenylamino)phenyl]acetate.8. A pharmaceutical composition for topical application comprising a compound as defined in and a pharmaceutical carrier.9. The composition as defined in claim 8 , said composition being in the form of a solution claim 8 , a gel or an emulsion.10. The composition as defined in claim 8 , wherein the compound is present in an amount of 0.001% to 10% by weight relative to the total weight of the composition.11. The compound as defined in claim 5 , wherein the pharmaceutically acceptable inorganic acid is selected from the group consisting of hydrochloric acid claim 5 , sulfuric acid claim 5 , phosphoric acid claim 5 , nitric acid and hydrobromic acid.12. The compound as defined in claim 5 , wherein the pharmaceutically acceptable organic acid is selected from the group consisting of acetic acid claim 5 , tartaric acid claim 5 , maleic acid claim 5 , hydroxymaleic acid claim 5 , fumaric acid claim 5 , citric ...

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01-08-2013 дата публикации

COMPOUNDS FOR TREATMENT OF CANCER

Номер: US20130197049A1
Принадлежит:

The present invention relates to novel compounds having anti-cancer activity, methods of making these compounds, and their use for treating cancer and drug-resistant tumors, e.g. melanoma, metastatic melanoma, drug resistant melanoma, prostate cancer and drug resistant prostate cancer. 4. The compound of claim 1 , wherein said compound is(4-phenyl-1H-imidazol-2-yl)(3,4,5-trimethoxyphenyl)methanone (70a);(4-(4-fluorophenyl)-1H-imidazol-2-yl)(3,4,5-trimethoxyphenyl)methanone (70b);(4-(4-chlorophenyl)-1H-imidazol-2-yl)(3,4,5-trimethoxyphenyl)methanone (70c);(4-(4-bromophenyl)-1H-imidazol-2-yl)(3,4,5-trimethoxyphenyl)methanone (70d);(4-(4-(trifluoromethyl)phenyl)-1H-imidazol-2-yl)(3,4,5-trimethoxyphenyl)methanone (70e);(4-p-tolyl-1H-imidazol-2-yl)(3,4,5-trimethoxyphenyl)methanone (70f);(4-(4-methoxyphenyl)-1H-imidazol-2-yl)(3,4,5-trimethoxyphenyl)methanone (70g);(4-(4-(dimethylamino)phenyl)-1H-imidazol-2-yl)(3,4,5-trimethoxyphenyl)methanone (70h);(4-(4-hydroxyphenyl)-1H-imidazol-2-yl)(3,4,5-trimethoxyphenyl)methanone (70i);(5-methyl-4-phenyl-1H-imidazol-2-yl)(3,4,5-trimethoxyphenyl)methanone (70j);(5-ethyl-4-phenyl-1H-imidazol-2-yl)(3,4,5-trimethoxyphenyl)methanone (70k);(4-phenyl-5-propyl-1H-imidazol-2-yl)(3,4,5-trimethoxyphenyl)methanone (70l);(1-methyl-4-phenyl-1H-imidazol-2-yl)(3,4,5-trimethoxyphenyl)methanone (70m);(1-ethyl-4-phenyl-1H-imidazol-2-yl)(3,4,5-trimethoxyphenyl)methanone (70n);(1-benzyl-4-phenyl-1H-imidazol-2-yl)(3,4,5-trimethoxyphenyl)methanone (70o); or(1-cyclopentyl-4-phenyl-1H-imidazol-2-yl)(3,4,5-trimethoxyphenyl)methanone (70p).5. A pharmaceutical composition comprising a compound according to and a pharmaceutically acceptable carrier.6. A method of treating claim 1 , suppressing claim 1 , reducing the severity claim 1 , reducing the risk claim 1 , inhibiting cancer comprising administering a compound according to to a subject having cancer under conditions effective to treat the cancer.7. The method of claim 6 , wherein said cancer is selected ...

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01-08-2013 дата публикации

MOLECULES HAVING COMBINABLE GROUPS

Номер: US20130197237A1
Принадлежит: Arkema France

The present invention relates to nitrogenous associative molecules comprising at least one unit rendering them capable of associating with one another or with a filler, via noncovalent bonds, and comprising a function capable of reacting with a polymer containing unsaturations so as to form a covalent bond with said polymer. 18-. (canceled)9. A compound comprising at least one group Q and at least one group A linked together by at least one spacer group Sp , wherein:group Q comprises a dipole comprising at least one nitrogen atom;group A comprises an associative group comprising at least one nitrogen atom; andSp is an atom or a group of atoms forming a link between group Q and group A.10. The compound of claim 9 , wherein the group Q comprises a dipole having one nitrogen atom.11. The compound of claim 9 , wherein the group A is chosen from imidazolidinyl claim 9 , triazoyl claim 9 , ureyl claim 9 , bis-ureyl claim 9 , and ureidopyrimidyl groups.14. The compound of claim 9 , wherein the group Q comprises a nitrile oxide claim 9 , nitrone or nitrile imine function.16. The compound of claim 9 , wherein the spacer group Sp is a linear or branched C-Calkyl chain claim 9 , optionally comprising one or more nitrogen or oxygen atoms.17. The compound of claim 16 , wherein the spacer group Sp is a linear or branched C-Calkyl chain claim 16 , optionally comprising one or more nitrogen or oxygen atoms.18. The compound of claim 16 , wherein the spacer group Sp is a linear C-Calkyl chain claim 16 , optionally comprising one or more nitrogen or oxygen atoms. This application is the U.S. National Phase application of PCT International Application No. PCT/FR2011/051651, filed Jul. 12, 2011, and claims priority to French Patent Application No. 1055717, filed Jul. 13, 2010, the disclosures of which are incorporated by reference in their entirety for all purposes.The present invention relates to nitrogenous associative molecules comprising at least one unit rendering them capable of ...

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08-08-2013 дата публикации

Mitochondria-Targeted Inhibitors of Cytochrome C Peroxidase for Protection from Apoptosis

Номер: US20130203829A1
Принадлежит: Individual

The present application is directed to novel imidazole-substituted fatty acids that have been functionalized with an alkyl triphenylphosphonium group, compositions comprising these compounds and their use as inhibitors of cytochrome c peroxidase, in particular for the treatment and prevention of apoptosis.

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08-08-2013 дата публикации

Compounds for Prevention of Cell Injury

Номер: US20130203830A1
Принадлежит: SULFATEQ B.V.

The invention is related to compounds for prevention of cell injury or protection of cells. The compounds are involved in the maintenance or the increase of hydrogen sulphide in cells, which results in a protection of the cells or the prevention of cell injury. The compounds of the invention can be used in cell culture and tissue culture techniques. They can also be used in several medical conditions such as ischemia, reperfusion and hypothermia, or for preserving organs which are used for transplantation. 1. A compound capable of increasing or maintaining the H2S level in a cell for use in the prevention of cell injury and/or protection of a cell.2. The compound of claim 1 , wherein the increase or maintenance of the H2S level in the cell is mediated by endogenous H2S production in a cell for use in the prevention of cell injury and/or protection of a cell.3. The compound of claim 1 , wherein the compound is selected from the group consisting of serotonin claim 1 , baclofen claim 1 , dopamine claim 1 , propofol claim 1 , melatonin claim 1 , histamine claim 1 , D/L phenylserine claim 1 , trolox claim 1 , reduced trolox and/or a salt claim 1 , a derivate claim 1 , or a precursor thereof.4. The compound of claim 1 , wherein the endogenous H2S production is mediated by cystathionine beta synthase (CBS).5. The compound of claim 1 , wherein the compound is transferred into the cell via active transport.6. The compound of claim 1 , wherein the prevention of cell injury and/or the protection of a cell against injury is achieved in the treatment of subjects suffering from a disorder that mediates oxidative stress to cells.7. The compound of claim 1 , wherein the prevention of cell injury and/or protection of the cells is achieved in the treatment of subjects suffering from ischemic injury and/or reperfusion claim 1 , neuromodulation claim 1 , hypertension claim 1 , inflammation claim 1 , hemorrhagic shock claim 1 , hypothermia claim 1 , diabetes or edema.8. The compound of ...

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15-08-2013 дата публикации

COMPOUNDS AND COMPOSITIONS AS INHIBITORS OF CANNABINOID RECEPTOR 1 ACTIVITY

Номер: US20130210769A1
Принадлежит: IRM LLC

The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of Cannabinoid Receptor 1 (CB1). 2. The compound of in which Ris selected from cyano claim 1 , methyl-carbonyl-amino-sulfonyl-ethyl claim 1 , pyrrolidin-2-onyl-ethyl claim 1 , imidazolyl-ethyl claim 1 , oxazolidin-2-only-ethyl claim 1 , 1-pyrazolyl-ethyl claim 1 , cyano-methyl claim 1 , 4′-(4-chlorophenoxy)phenyl claim 1 , 1 claim 1 ,3-dioxanyl-ethyl claim 1 , allyl claim 1 , phenyl claim 1 , pyrazinyl claim 1 , piperazinyl-sulfonyl-ethyl claim 1 , azetidinyl-sulfonyl-ethyl claim 1 , morpholino-sulfonyl-ethyl claim 1 , pyrrolidinyl-sulfonyl-ethyl claim 1 , pyrrolidinyl-propyl claim 1 , pyrrolidinyl-ethyl claim 1 , piperazinyl-propyl claim 1 , piperidinyl-sulfonyl-ethyl claim 1 , pyridazinyl claim 1 , (5-(4-methoxyphenyl)-1 claim 1 ,2 claim 1 ,4-oxadiazol-3-yl)methyl claim 1 , isoxazolyl claim 1 , piperidinyl-carbonyl-methyl claim 1 , 3-(N claim 1 ,N-bis(4-methoxyphenyl)sulfamoyl)propyl claim 1 , methyl-phenyl-sulfonyl claim 1 , cyanomethyl claim 1 , 2-oxo-2-(piperidin-1-ylamino)ethyl claim 1 , propyl-amino-carbonyl-methyl claim 1 , 2-(carboxymethylamino)-2-oxoethyl) claim 1 , bis-hydroxyethyl-amino-sulfonyl-ethyl claim 1 , carboxy-methyl-amino-carbonyl-methyl claim 1 , amino-carbonyl-ethyl claim 1 , amino-sulfonyl-ethyl claim 1 , amino-sulfonyl-propyl claim 1 , methyl-amino-ethyl claim 1 , piperidinyl-ethyl claim 1 , piperazinyl-ethyl claim 1 , methyl-sulfonyl-ethyl claim 1 , carboxy-methyl claim 1 , tetrazole-methyl claim 1 , benzyl claim 1 , 1 claim 1 ,2 claim 1 ,4-oxadiazole claim 1 , 1 claim 1 ,2 claim 1 ,4-oxadiazole-methyl claim 1 , 1 claim 1 ,2 claim 1 ,4-oxadiazole-ethyl claim 1 , isoxazole-methyl claim 1 , 2-(2-hydroxyethylamino)-2-oxoethyl claim 1 , dimethylamino-ethyl-amino-carbonyl-methyl claim 1 , hydroxyl-ethyl claim 1 , methoxy-ethyl claim 1 , hydroxyl-ethyl- ...

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15-08-2013 дата публикации

NEW SALT OF A PYRIMIDIN DERIVATIVE

Номер: US20130210848A1
Принадлежит: LABORATORIOS SENOSIAIN S.A. DE C.V.

The present invention relates to a salt of a pyrimidin derivative of the acid (3R,5S,6E)-7-[4-(4-fluorophenyl)-2-(N-methylmethanesulfonamide)-6-(propan-2-yl)pyrimidin-5-yl]-3,5-dihydroxyhept-6-enoic, to a method for preparing same and to the use thereof in formulating pharmaceutical formulations. 19-. (canceled)10. (3R ,5S ,6E)-7-[4-(4-fluorophenyl)-2-(N-methylmethanesulfonamide)-6-(propan-2-yl) pyrimidin-5-yl]-3 ,5-dihydroxihept-6-enoic amino acid salt , wherein the amino acid is lysine and wherein the bond formed between these two entities is a non-covalent bond.11. (3R ,5 S ,6E)-7-[4-(4-fluorophenyl)-2-(N-methylmethanesulfonamide)-6-(propan-2-yl)pyrimidin-5-yl]-3 ,5-dihydroxihept-6-enoic amino acid salt , wherein the amino acid is histidine and wherein the bond formed between these two entities in a non-covalent bond.12. A pharmaceutical composition comprising the salt of claim 10 , in combination with a pharmaceutically acceptable carrier.13. A pharmaceutical composition comprising the salt of claim 11 , in combination with a pharmaceutically acceptable carrier.14. A method of manufacturing a pharmaceutical composition comprising the step of adding the salt of to a pharmaceutically acceptable carrier.15. A method of manufacturing a pharmaceutical composition comprising the step of adding the salt of to a pharmaceutically acceptable carrier.16. The method according to claim 14 , wherein the pharmaceutical compositions are in the form of tablets or capsules.17. A method of manufacturing medicaments for the prevention or treatment of cardiovascular diseases comprising the step of adding the compound of to a pharmaceutically acceptable carrier.18. A process for synthesizing a rosuvastatin-lysine salt claim 10 , comprising the steps:a) subjecting the rosuvastatin calcium salt to a dissociation process; andb) mixing the acid rosuvastatin resulting from the previous step with an aqueous solution containing lysine for forming the salt in the presence of a methanol/ethyl ...

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15-08-2013 дата публикации

MOLECULES HAVING COMBINABLE GROUPS

Номер: US20130211057A1
Принадлежит: Arkema France

The present invention relates to nitrogenous associative molecules comprising at least one unit rendering them capable of associating with one another or with a filler by noncovalent bonds, and comprising a function capable of reacting with a polymer containing unsaturations so as to form a covalent bond with said polymer. 19-. (canceled)10. A compound comprising at least one group Q and at least one group A , wherein the groups Q and A are linked together by at least one spacer group Sp:wherein:group Q comprises an azodicarbonyl function;group A comprises an associative group comprising at least one nitrogen atom; andspacer group Sp is an atom or a group of atoms forming a link between group Q and group A.11. The compound of claim 10 , wherein the associative group is chosen from imidazolidinyl claim 10 , triazolyl claim 10 , ureyl claim 10 , bis-ureyl claim 10 , and ureidopyrimidyl groups.13. The compound of claim 12 , wherein X denotes an oxygen atom.15. The compound of claim 14 , wherein W represents a group of formula:{'br': None, 'R′—Z—'}{'sub': 1', '6, 'wherein R′ represents a C-Calkyl group.'}16. The compound of claim 15 , wherein R′ represents a C-Calkyl group.17. The compound of claim 15 , wherein R′ represents a methyl or ethyl group.20. The compound of claim 19 , wherein R represents a C-Calkoxyl group.21. The compound of claim 19 , wherein R represents a methyoxyl or ethoxyl group.22. The compound of claim 10 , wherein the spacer group Sp is a linear or branched C-Calkyl chain claim 10 , optionally comprising one or more heteroatoms chosen from nitrogen claim 10 , sulfur claim 10 , silicon claim 10 , and oxygen atoms.23. The compound of claim 22 , wherein the spacer group Sp is a linear or branched C-Calkyl chain claim 22 , optionally comprising one or more heteroatoms chosen from nitrogen claim 22 , sulfur claim 22 , silicon claim 22 , and oxygen atoms.24. The compound of claim 22 , wherein the spacer group Sp is a linear C-Calkyl chain optionally ...

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