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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 22535. Отображено 100.
05-01-2012 дата публикации

Method of treatment or prophylaxis

Номер: US20120004259A1
Принадлежит: SPINIFEX PHARMACEUTICALS PTY LTD

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

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12-01-2012 дата публикации

Tetrazine monomers and copolymers for use in organic electronic devices

Номер: US20120007026A1
Принадлежит: NATIONAL RESEARCH COUNCIL OF CANADA

Copolymers of formula (I): where each A is S, Se or C═C; each x is an integer from 1 to 4; each R1 is independently H, F, CN or a C 1 -C 20 linear or branched aliphatic group; Ar is one or more substituted or unsubstituted aromatic units; and, n is an integer 5 or greater, can be formed into films or membranes that are useful as active layers in organic electronic device, such as PV solar cells, providing high power conversion efficiencies and good thermal stability. Such copolymers may be synthesized from monomers of formula (II): by Stille or Suzuki coupling reactions. Such monomers may be synthesized by a variation of the Pinner synthesis.

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19-01-2012 дата публикации

Pharmaceutical composition for external use

Номер: US20120015997A1
Принадлежит: Nihon Nohyaku Co Ltd, Pola Pharma Inc

Provided is a pharmaceutical composition for external use, including: (i) a compound represented by structural formula (2) and/or a salt thereof; and (ii) N-methyl-2-pyrrolidone.

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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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09-02-2012 дата публикации

Charge transport compositions and electronic devices made with such compositions

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

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

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23-02-2012 дата публикации

Developers and method of coloring lithographic printing members

Номер: US20120045720A1
Принадлежит: Individual

A color contrast image in imaged lithographic printing precursors can be obtained by contacting the imaged precursor with a coloration solution containing a colorless form of a photochromic compound. Residual amounts of this compound attached to the oleophilic surface of the imaged precursor can be changed to its colored form when exposed to UV light. The coloration solution can be an alkaline or acidic developer or an alkaline or acidic solution used separately after development. The coloration solution can also be a gum solution.

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23-02-2012 дата публикации

3-substituted propanamine compounds

Номер: US20120046312A1
Принадлежит: SK Biopharmaceuticals Co Ltd

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

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01-03-2012 дата публикации

Azafluorene derivative and organic light-emitting device using the derivative

Номер: US20120049176A1
Принадлежит: Canon Inc

A novel azafluorene derivative and an organic light-emitting device having the derivative are provided. The organic light-emitting device includes a pair of electrodes composed of an anode and a cathode one of which is a transparent or semi-transparent electrode, and an organic compound layer interposed between the pair of electrodes. The organic compound layer contains the azafluorene derivative represented by the following general formula (I):

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08-03-2012 дата публикации

Carbazole and carboline kinase inhibitors

Номер: US20120058988A1
Принадлежит: Bristol Myers Squibb Co

The present invention provides compounds of Formula (I) and pharmaceutically acceptable salts thereof The Formula (I) compounds inhibit tyrosine kinase activity of Jak2, thereby making them useful as antiproliferative agents for the treatment of cancer and other diseases.

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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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19-04-2012 дата публикации

Novel Heterocyclic Compounds as Pesticides

Номер: US20120094837A1
Принадлежит: Bayer CropScience AG

The present invention relates to novel heterocyclic compounds, to processes for preparation thereof and to the use thereof for controlling animal pests, which include arthropods and especially insects.

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10-05-2012 дата публикации

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

Номер: US20120115915A1
Принадлежит: Harvard College

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

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17-05-2012 дата публикации

Pyruvate kinase m2 modulators, therapeutic compositions and related methods of use

Номер: US20120122885A1
Принадлежит: Agios Pharmaceuticals Inc

Compositions comprising compounds that modulate pyruvate kinase M2 (PKM2) are described herein. Also described herein are methods of using the compounds that modulate PKM2 in the treatment of cancer.

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31-05-2012 дата публикации

Cyclic triazo sodium channel blockers

Номер: US20120135993A1
Принадлежит: University of Greenwich

The present invention relates to triazine compounds having sodium channel blocking properties, and to use of the compounds for preparation of medicaments for treatment of associated disorders. The triazine compounds are of formula (I) wherein: R1 is hydrogen or a substituent group; R2 is amino or a substituent group; N* is amino when R1 is hydrogen or ═NH when R1 is a substituent group; R3 and R4 are both carbocyclic, heterocyclic or alkyl groups and may be same or different; and R5 is hydrogen, alkyl or a cyclic aryl group, with the proviso that: when R3 and R4 are both alkyl they are linked to form a cycloalkyl group, and R5 is a cyclic aromatic group; and when R3 and R4 are both carbocyclic or heterocyclic groups, R5 is hydrogen or an alkyl group; or a salt thereof.

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07-06-2012 дата публикации

Light-emitting device material and light-emitting device

Номер: US20120138907A1
Принадлежит: TORAY INDUSTRIES INC

Embodiments provide a light emitting device material characterized by containing an anthracene compound represented by the following general formula. where R 19 to R 37 are a hydrogen atom, alkyl group, cycloalkyl group, heterocyclic group or the like; n is 1 or 2; and A is a heteroarylene group or arylene group. Any one of the R 19 to R 27 and any one of the R 28 to R 37 are used for linking with A. The present teachings allow a light emitting device having high luminous efficiency and excellent durability.

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28-06-2012 дата публикации

Novel azabicyclohexanes

Номер: US20120165320A1
Принадлежит: Panacea Biotec Ltd

The present invention relates to novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, stereoisomers including R and S isomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The invention also relates to processes for the synthesis of novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, stereoisomers, polymorphs, prodrugs, metabolites, salts or solvates thereof.

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05-07-2012 дата публикации

Second-order nonlinear optical compound and nonlinear optical element comprising the same

Номер: US20120172599A1
Принадлежит: Individual

Problem to Be Solved: to provide a chromophore having a far superior nonlinear optical activity to conventional chromophores and to provide a nonlinear optical element comprising said chromophore. Solution: a chromophore comprising a donor structure D, a π-conjugated bridge structure B, and an acceptor structure A, the donor structure D comprising an aryl group substituted with a substituted oxy group; and a nonlinear optical element comprising said chromophore.

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02-08-2012 дата публикации

Sulfoximines as kinase inhibitors

Номер: US20120196902A1
Принадлежит: Allergan Inc

The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.

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09-08-2012 дата публикации

Substituted pyridones as inhibitors of poly(adp-ribose) polymerase (parp)

Номер: US20120202795A1
Принадлежит: Aventis Pharmaceuticals Inc

The present invention relates to a series of 2,3,5-substituted pyridone derivatives of formula I: wherein R, R 1 , R 2 , R 3 and R 4 are as defined herein. This invention also relates to methods of making these compounds. The compounds of this invention are inhibitors of poly(adenosine 5′-diphosphate ribose) polymerase (PARP) and are therefore useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases, including diseases associated with the central nervous system and cardiovascular disorders.

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09-08-2012 дата публикации

Dual small molecule inhibitors of cancer and angiogenesis

Номер: US20120202800A1
Автор: Milton L. Brown

The present invention provides analogs and derivatives of thalidomide which inhibit cancer and angiogenesis. The present invention further provides compounds which disrupt microtubule polymerization. The present further provides methods of treating cancers comprising mutant p53.

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09-08-2012 дата публикации

Substituted 4-aminocyclohexane derivatives

Номер: US20120202810A1
Принадлежит: GRUENENTHAL GmbH

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

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09-08-2012 дата публикации

Heteroaryls and uses thereof

Номер: US20120202812A1
Принадлежит: Millennium Pharmaceuticals Inc

This invention provides compounds of formula I: wherein R 1 , R 2 , CY, Y 1 , Y 2 , X 1 , X 2 , and X 3 are as described in the specification. The compounds are inhibitors of PI3K and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.

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16-08-2012 дата публикации

Novel organic electroluminescent compounds and organic electroluminescent device using the same

Номер: US20120206037A1

Provided are a novel organic electroluminescent compound and an organic electroluminescent device using the same. When used as a host material of an organic electroluminescent material of an OLED device, the organic electroluminescent compound disclosed herein exhibits good luminous efficiency and excellent life property as compared to the existing host material. Therefore, it may be used to manufacture OLEDs having very superior operation life.

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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

Viral polymerase inhibitors

Номер: US20120214783A1
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

Compounds of formula I: wherein X, R 2 , R 3 , R 3a , R 3b , R 5 and R 6 are defined herein, are useful as inhibitors of the hepatitis C virus NS5B polymerase.

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23-08-2012 дата публикации

Heteroaryls and uses thereof

Номер: US20120214794A1
Принадлежит: Millennium Pharmaceuticals Inc

This invention provides compounds of formula I-A or I-B: wherein HY, G 1 , G 2 , R 2 , R 12 , W 1 , W 2 , n, and Ring A are as described in the specification. The compounds are inhibitors of PI3K and/or mTor and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.

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30-08-2012 дата публикации

Novel spiropiperidine compounds

Номер: US20120220616A1
Принадлежит: Eli Lilly and Co

A compound of the formula: or a pharmaceutically acceptable salt thereof as well as a pharmaceutical composition, and a method for treating diabetes.

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13-09-2012 дата публикации

Use of Indole Derivatives as Nurr-1 Activators for the Application Thereof as a Medicament for the Treatment of Parkinson's Disease

Номер: US20120232070A1
Принадлежит: Laboratories Fournier SAS

Compounds derived from indole, notably useful in therapeutics, selected from: i) the compounds of formula: and ii) the pharmaceutically acceptable salts of the compounds of formula (I); in which R1, R2, R3, R4, R5, R6, R8, R9 and Cy have defined meanings, and the use of such compounds in pharmaceuticals for the treatment of neurodegenerative diseases, particularly Parkinson's disease.

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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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01-11-2012 дата публикации

Aromatic heterocyclic derivative and organic electroluminescence device using the same

Номер: US20120273766A1
Принадлежит: Idemitsu Kosan Co Ltd

An aromatic heterocyclic derivative represented by the following formula (1), a material for an organic electroluminescence device and an organic electroluminescence device including these:

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15-11-2012 дата публикации

Novel compounds with high therapeutic index

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

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

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22-11-2012 дата публикации

Chromone Inhibitors of S-Nitrosoglutathione Reductase

Номер: US20120295966A1
Принадлежит: N30 Pharmaceuticals Inc

The present invention is directed to inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same.

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29-11-2012 дата публикации

Novel sulfamides exhibiting neuroprotective action and methods for use thereof

Номер: US20120302546A1

Pharmaceutical compositions of the invention include sulfamide derivatives having a disease-modifying action in the treatment of diseases associated with excitotoxicity and accompanying oxidative stress that include epilepsy, Alzheimer's disease, and any neurodegenerative disease involving glutamate toxicity.

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20-12-2012 дата публикации

Heterocyclic sulfonamides, uses and pharmaceutical compositions thereof

Номер: US20120322823A1
Принадлежит: PFIZER INC

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

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03-01-2013 дата публикации

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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24-01-2013 дата публикации

Catalysts based on heterocyclic-8-anilinoquinoline ligands

Номер: US20130023635A1
Принадлежит: EQUISTAR CHEMICALS LP

A catalyst system useful for polymerizing olefins is disclosed. The catalyst system comprises an activator and a Group 4 metal complex. The complex incorporates a dianionic, tridentate heterocyclic-8-anilinoquinoline ligand. In one aspect, a supported catalyst system is prepared by first combining a boron compound having Lewis acidity with excess alumoxane to produce an activator mixture, followed by combining the activator mixture with a support and the dianionic, tridentate Group 4 metal complex. The Group 4 metal complexes are easy to synthesize, support, and activate, and they enable facile production of high-molecular-weight polyolefins.

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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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14-02-2013 дата публикации

Multisubstituted aromatic compounds as inhibitors of thrombin

Номер: US20130040950A1
Принадлежит: Verseon Corp

There are provided inter alia multisubstituted aromatic compounds useful for the inhibition of thrombin, which compounds include substituted pyrazolyl or substituted triazolyl. There are additionally provided pharmaceutical compositions. There are additionally provided methods of treating and preventing a disease or disorder, which disease or disorder is amenable to treatment or prevention by the inhibition of thrombin.

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07-03-2013 дата публикации

Maleimide-based compound, and tautomer or stereoisomer thereof, dye for photoelectric conversion, and semiconductor electrode, photoelectric conversion element and photoelectrochemical cell using the same

Номер: US20130056690A1
Принадлежит: NEC Corp

It is an object to provide a maleimide-based compound having excellent photoelectric conversion characteristics, and a tautomer or a stereoisomer thereof, a dye for photoelectric conversion, a semiconductor electrode, a photoelectric conversion element, and a photoelectrochemical cell. In order to accomplish the above-described objects, a dye for photoelectric conversion including at least one compound represented by the following general formula (1) is provided. (In the formula (1), R 1 represents a direct bond, or a substituted or unsubstituted alkylene group. X represents an acidic group. D represents an organic group containing an electron-donating substituent. Z represents a linking group that has at least one hydrocarbon group selected from aromatic rings or heterocyclic rings).

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07-03-2013 дата публикации

Methods of identifying modulators of gpr17

Номер: US20130059899A1

The present invention is related to a method of determining a test compound's ability to modify the biological activity of a GPR17. Said method comprises, among others, the step of contacting the test compound with a GPR17, or a functional GPR17 fragment in the presence of a suitable amount of a GPR17 agonist of formula I.

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07-03-2013 дата публикации

Synthesis of substituted pyrazoline carboxamidine derivatives

Номер: US20130060041A1

This invention relates to organic chemistry, in particular to processes for the preparation of pyrazoline carboxamidine derivatives of formula (I), known as potent 5-HT6 antagonists. The invention also relates to novel intermediates of these compounds. wherein the symbols have the meanings given in the description.

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21-03-2013 дата публикации

PROLYL HYDROXYLASE INHIBITORS

Номер: US20130072487A1
Принадлежит: GlaxoSmithKline LLC

The invention described herein relates to certain pyrimidinetrione N-substituted glycine derivatives of formula (I) 2. The method according to wherein:X is O;Y is O;{'sup': 1', '4, 'sub': 1-', '10', '2-', '10', '2-', '10', '3', '8', '3', '8', '1-', '10', '5', '8', '5', '8', '1-', '10', '3', '8', '3', '8', '1-', '10', '1-', '10', '1-', '10, 'Rand Rare each independently selected from the group consisting of hydrogen, CCalkyl, CCalkenyl, CCalkynyl, C-Ccycloalkyl, C-Ccycloalkyl-CCalkyl, C-Ccycloalkenyl, C-Ccycloalkenyl-CCalkyl, C-Cheterocycloalkyl, C-Cheterocycloalkyl-CCalkyl, aryl, aryl-CCalkyl, heteroaryl and heteroaryl-CCalkyl;'}{'sup': 2', '7', '8', '9, 'Ris —NRRor —OR;'}{'sup': '3', 'sub': 1-', '4, 'claim-text': [{'sup': 7', '8, 'sub': 1-', '10', '2-', '10', '2-', '10', '3', '8', '3', '8, 'where Rand Rare each independently selected from the group consisting of hydrogen, CCalkyl, CCalkenyl, CCalkynyl, C-Ccycloalkyl, C-Cheterocycloalkyl, aryl and heteroaryl, and'}, {'sup': '9', 'sub': 1-', '10', '3', '6, 'Ris H or a cation, or CCalkyl which is unsubstituted or substituted with one or more substituents independently selected from the group consisting of C-Ccycloalkyl, heterocycloalkyl, aryl and heteroaryl,'}, {'sup': 1', '2', '3', '4', '7', '8', '9', '10', '5', '6', '10', '10', '10', '10', '10', '5', '6', '5', '6', '5', '10', '5', '10', '5', '6', '5', '5', '6', '5', '6', '5', '10', '5', '6', '10, 'sub': 1', '6', '1', '6', '2', '2', '2', '2', '10', '2', '10', '3', '6', '3', '6', '1', '6', '1', '6', '1-', '10', '2-', '10', '2-', '10', '1', '4', '3', '6', '3', '6', '2', '1', '4', '3', '8', '3', '8', '6', '14', '1-', '10', '1-', '10, 'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'where any carbon or heteroatom of R, R, R, R, R, R, Ris unsubstituted or is substituted with one or more substituents independently selected from C-Calkyl, C-Chaloalkyl, halogen, —OR, —NRR, oxo, cyano, nitro, —C(O)R, —C(O)OR, —SR, —S(O)R, —S(O)R, —NRR, —CONRR, —N(R)C(O)R, —N(R)C(O)OR, —OC(O) ...

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21-03-2013 дата публикации

INHIBITORS OF JUN N-TERMINAL KINASE

Номер: US20130072494A1
Принадлежит:

The present disclosure provides inhibitors of c-Jun N-terminal kinases (JNK) having a structure according to the following formula: 3. The compound of claim 1 , wherein ring A is chosen from thiophene claim 1 , thiazole claim 1 , and pyrazole claim 1 , wherein the thiophene claim 1 , the thiazole claim 1 , or the pyrazole is optionally substituted with 1 or 2 substituents chosen from C-C-alkyl claim 1 , C-C-alkenyl claim 1 , C-C-alkynyl claim 1 , C-C-haloalkyl claim 1 , 2- to 4-membered heteroalkyl claim 1 , C-C-cycloalkyl claim 1 , 3- to 6-membered heterocycloalkyl claim 1 , CN claim 1 , and halogen.6. The compound of claim 1 , wherein W is methylene (—CH—).7. The compound of claim 1 , wherein Ris H.8. The compound of claim 1 , wherein Cy is chosen from phenyl claim 1 , naphthyl claim 1 , quinoline claim 1 , isoquinoline claim 1 , quinoxaline claim 1 , quinazoline claim 1 , 3 claim 1 ,4-dihydroquinolin-2-one claim 1 , and 3 claim 1 ,4-dihydro-1 claim 1 ,6-naphthyridin-2-one claim 1 , each optionally substituted with 1-6 substituents independently chosen from C-C-alkyl claim 1 , C-C-alkenyl claim 1 , C-C-alkynyl claim 1 , C-C-haloalkyl claim 1 , 2- to 6-membered heteroalkyl claim 1 , C-C-cycloalkyl claim 1 , 3- to 8-membered heterocycloalkyl claim 1 , aryl claim 1 , 5- or 6-membered heteroaryl claim 1 , CN claim 1 , halogen claim 1 , OR claim 1 , SR claim 1 , NRR claim 1 , C(O)R claim 1 , C(O)NRR claim 1 , OC(O)NRR claim 1 , C(O)OR claim 1 , NRC(O)R claim 1 , NRC(O)OR claim 1 , NRC(O)NRR claim 1 , NRC(S)NRR claim 1 , NRS(O)R claim 1 , S(O)NRR claim 1 , S(O)Rand S(O)R claim 1 ,wherein{'sup': 52', '53', '55', '52', '53, 'sub': 1', '6', '3', '8, 'R, Rand Rare independently chosen from H, acyl, C-C-alkyl, 2- to 6-membered heteroalkyl, aryl, 5- or 6-membered heteroaryl, C-Ccycloalkyl and 3- to 8-membered heterocycloalkyl, wherein Rand R, together with the nitrogen atom to which they are bound are optionally joined to form a 5- to 7-membered heterocyclic ring; and'}{'sup ...

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28-03-2013 дата публикации

NOVEL IODO PYRIMIDINE DERIVATIVES USEFUL FOR THE TREATMENT OF MACROPHAGE MIGRATION INHIBITORY FACTOR (MIF)-IMPLICATED DISEASES AND CONDITIONS

Номер: US20130079361A1
Принадлежит:

Compounds useful for the inhibition of macrophage migration inhibitory factor (MIF) are provided herein, having the Formula (I): wherein A is selected from the group consisting of aromatic or non-aromatic rings, bicyclic rings, polycyclic rings, alkenes or alkynes; B is H, OH, OR, SR, NH2, NHR, or alkyl; R is H or alkyl, and X and Y are independently N or CH, but one of X and Y must be N. Also provided are pharmaceutical compositions comprising a Formula I compound and methods for the treatment of MIF-implicated diseases or conditions, comprising administering a safe and effective amount of a Formula I compound. 2. The compound of selected from the group set forth in Table 1.3. The compound of claim 1 , wherein X and Y are both N.4. The compound of claim 3 , wherein B is H.5. The compound of claim 1 , wherein A is halo claim 1 , B is A claim 1 , and X and Y are both N.6. The compound of claim 1 , wherein X is N claim 1 , and Y is CH.7. The compound of claim 6 , wherein B is H.8. The compound of claim 1 , wherein X is CH claim 1 , and Y is N.9. The compound of claim 8 , wherein B is H.10. The compound of claim 1 , wherein A is selected from the group consisting of indole claim 1 , quinoline claim 1 , and naphthalene.11. The compound of claim 1 , wherein the compound is 4-Iodo-6-(2-fluorophenyl)pyrimidine or 4-Iodo-6-(3-aminocarbonylphenyl)pyrimidine.13. The pharmaceutical composition of claim 12 , wherein the compound is selected from the group set forth in Table 1.15. The method of claim 14 , wherein the MIF-implicated disease is selected from the group consisting of inflammatory disease and cancer.16. The method of claim 15 , wherein the inflammatory disease is selected from the group consisting of dermatitis claim 15 , arthritis claim 15 , rheumatoid arthritis claim 15 , insulin-dependent diabetes claim 15 , proliferative vascular disease claim 15 , acute respiratory distress syndrome claim 15 , sepsis claim 15 , septic shock claim 15 , psoriasis claim 15 , asthma ...

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04-04-2013 дата публикации

5H-CYCLOPENTA[D]PYRIMIDINES AS AKT PROTEIN KINASE INHIBITORS

Номер: US20130085135A1
Принадлежит:

Compounds of Formula I are useful for inhibiting AKT protein kinases. Methods of using compounds of Formula I and stereoisomers and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed. 13. The method of claim 1 , wherein X is a direct bond from L to Y claim 1 , Y is CH and Z is O.14. The method of claim 1 , wherein X is C(═O)NH claim 1 , Y is CH and Z is absent.15. The method of claim 1 , wherein X is a direct bond from L to Y claim 1 , Y is CH and Z is absent.16. The method of claim 1 , wherein X is NH claim 1 , Y is CH and Z is absent.17. The method of claim 1 , wherein X is C═O claim 1 , Y is N claim 1 , Z is absent and b is 1 or 2.18. The method of claim 1 , wherein X is C═O claim 1 , Y is CH and Z is absent.19. The method of claim 1 , wherein Ris hydrogen.20. The method of claim 1 , wherein Ris methyl.21. The method of claim 1 , wherein Ris hydrogen.22. The method of claim 1 , wherein Ris methyl.23. The method of claim 1 , wherein Ris hydrogen.24. The method of claim 1 , wherein Ris C-Calkyl.25. The method of claim 1 , wherein Ris selected from methyl claim 1 , isopropyl and tert-butyl.26. The method of claim 1 , wherein Ris hydrogen.27. The method of claim 1 , wherein Ris methyl.29. The method of claim 28 , wherein c is 1.31. The method of claim 1 , wherein G is selected from the group consisting of 4-chlorophenyl claim 1 , 4-bromophenyl claim 1 , 4-trifluoromethylphenyl and 2 claim 1 ,4-dichlorophenyl.32. The method of wherein:(5R,7R)-4-(4-((S)-(4-chlorophenyl)(2-(dimethylamino)ethoxy)methyl)piperidin-1-yl)-5-methyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-7-ol;(5R,7R)-4-(4-((R)-(4-chlorophenyl)(2-(dimethylamino)ethoxy)methyl)piperidin-1-yl)-5-methyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-7-ol;N—((S)-1-amino-3-(2,4-dichlorophenyl)propan-2-yl)-5-((R)-5-methyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl)thiophene-2- ...

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18-04-2013 дата публикации

Inhibitors of human 12-lipoxygenase

Номер: US20130096159A1

Disclosed are inhibitors of human 12-lipoxygenase of Formula (I) or (II), wherein R 1 , R 2 , R 3 , and R 4 are as defined herein, that are useful in treating or preventing a 12-lipoxygenase mediated disease or disorder, e.g., diabetes. Also disclosed are a composition comprising a pharmaceutically acceptable carrier and at least one inhibitor of the invention, and a method of treating or preventing such disease or disorder in a mammal.

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18-04-2013 дата публикации

Novel Dihydropyridin-2(1H)-One Compounds as S-Nitrosoglutathione Reductase Inhibitors and Neurokinin-3 Receptor Antagonists

Номер: US20130096161A1
Автор: Qiu Jian, Sun Xicheng
Принадлежит: N30 PHARMACEUTICALS, INC.

The present invention is directed to novel dihydropyridin-2(1H)-one compounds useful as S-nitrosoglutathione reductase (GSNOR) inhibitors and/or Neurokinin-3 (NK3) receptor antagonists, pharmaceutical compositions comprising such compounds, and methods of making and using the same. 2. The compound of wherein Ris selected from the group consisting of hydroxyl claim 1 , carboxyl claim 1 , and tetrazol-5-yl.3. The compound of wherein R claim 1 , Rand Rare independently selected from the group consisting of hydrogen and methyl;{'sub': 3', '1', '6, 'Ris selected from the group consisting of hydrogen, nitro, cyano, carboxyl, carbamoyl, methylsulfonamido, fluoro, chloro, bromo, hydroxyl, methylsulfonyl, and methylsulfinyl, isoxazol-4-yl, C-Calkoxy, —C(NH)NHOH, sulfonic acid, and acetyl;'}{'sub': '4', 'Ris selected from the group consisting of hydroxyl, carboxyl, and tetrazol-5-yl;'}{'sub': 5', '2', '2', '2', '1', '6', '2', '2', '3', '2', '2', '3, 'Ris selected from the group consisting of hydrogen, hydroxyl, carboxyl, chloro, fluoro, cyano, —O(CH)NMe, C-Calkyl, —O(CH)OCH, —O(CH)OH, acetyl, CF, methoxy, ethoxy, isopropoxy, and n-propoxy; and'}{'sub': '6', 'Ris hydrogen.'}4. The compound of wherein Ris selected from the group consisting of hydrogen claim 3 , nitro claim 3 , and hydroxyl; Ris selected from the group consisting of hydroxyl claim 3 , carboxyl claim 3 , and tetrazol-5-yl; and Ris selected from the group consisting of hydrogen claim 3 , ethoxy claim 3 , fluoro claim 3 , and —O(CH)OH.5. The compound of wherein X is selected from the group consisting of aryl claim 1 , substituted aryl claim 1 , heteroaryl claim 1 , and substituted heteroaryl.6. The compound of wherein X is selected from the group consisting of phenyl claim 1 , substituted phenyl claim 1 , thiophen-yl claim 1 , substituted thiophen-yl claim 1 , thiazol-yl claim 1 , substituted thiazol-yl claim 1 , pyrazin-yl claim 1 , substituted pyrazin-yl claim 1 , pyridin-yl claim 1 , and substituted pyridin-yl ...

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25-04-2013 дата публикации

AZETIDINYL DIAMIDES AS MONOACYLGLYCEROL LIPASE INHIBITORS

Номер: US20130102585A1
Принадлежит: Janssen Pharmaceutica NV

Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: 118.-. (canceled)20. A pharmaceutical composition comprising a compound of and at least one of a pharmaceutically acceptable carrier claim 19 , a pharmaceutically acceptable excipient and a pharmaceutically acceptable diluent.21. A pharmaceutical composition of claim 20 , wherein the composition is a solid oral dosage form.22. A pharmaceutical composition of claim 20 , wherein the composition is a syrup claim 20 , an elixir or a suspension. This application claims priority to U.S. provisional patent application Nos. 61/171,658 and 61/171,649, each filed Apr. 22, 2009, which are hereby incorporated by reference in their entirety.The research and development of the invention described below was not federally sponsored.Cannabis sativa has been used for the treatment of pain for many years. Δ-tetrahydrocannabinol is a major active ingredient from Cannabis sativa and an agonist of cannabinoid receptors (Pertwee, 2008, 153, 199-215). Two cannabinoid G protein-coupled receptors have been cloned, cannabinoid receptor type 1 (CBMatsuda et al., 1990, 346, 561-4) and cannabinoid receptor type 2 (CBMunro et al., 1993, 365, 61-5). CBis expressed centrally in brain areas, such as the hypothalamus and nucleus accumbens as well as peripherally in the liver, gastrointestinal tract, pancreas, adipose tissue, and skeletal muscle (Di Marzo et al., 2007, 18, 129-140). CBis predominantly expressed in immune cells, such as monocytes (Pacher et al., 2008, 294, H1133-H1134), and under certain conditions, also in the brain (Benito et al., 2008, 153, 277-285) and in skeletal (Cavuoto et al., 2007, 364, 105-110) and cardiac (Hajrasouliha et al., 2008, 579, 246-252) muscle. An abundance of pharmacological, anatomical and electrophysiological data, using synthetic agonists, indicate that increased ...

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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

COMPOUNDS AND METHODS FOR TREATING INFLAMMATORY AND FIBROTIC DISORDERS

Номер: US20130102597A1
Принадлежит: INTERMUNE, INC.

Disclosed are compounds and methods for treating inflammatory and fibrotic disorders, including methods of modulating a stress activated protein kinase (SAPK) system with an active compound, wherein the active compound exhibits low potency for inhibition of the p38 MAPK; and wherein the contacting is conducted at a SAPK-modulating concentration that is at a low percentage inhibitory concentration for inhibition of the p38 MAPK by the compound. Also disclosed are derivatives and analogs of pirfenidone, useful for modulating a stress activated protein kinase (SAPK) system. 3. The method of claim 2 , wherein{'sup': '1', 'Ris selected from the group consisting of hydrogen, alkyl, cycloalkyl, alkenyl, cyano, sulfonamido, halo, alkenylenearyl, and heteroaryl;'}{'sup': 2', '2', '1, 'sub': 3', '2', '2', '2', '2', '2, 'Ris selected from the group consisting of aryl; unsubstituted heteroaryl; heteroaryl substituted with one or more substituents selected from halo, unsubstituted alkyl, alkenyl, OCF, NO, CN, NC, OH, alkoxy, haloalkoxy, amino, COH, and COalkyl; haloalkylcarbonyl; cycloalkyl; hydroxylalkyl; sulfonamide; unsubstituted cycloheteroalkyl and cycloheteroalkyl substituted with one to three substituents independently selected from alkyleneOH, C(O)NH, NH, aryl, haloalkyl, halo, and OH; or Rand Rtogether form an optionally substituted 5-membered nitrogen-containing heterocyclic ring;'}{'sup': '4', 'Ris selected from the group consisting of hydrogen, haloalkyl, alkoxy, alkenyl, and alkenylenearyl; and'}{'sup': '5', 'Xis hydrogen.'}4. The method of claim 1 , wherein one of X claim 1 , X claim 1 , and Xis not hydrogen.5. The method of claim 4 , wherein Ris selected from the group consisting of aryl; unsubstituted heteroaryl; heteroaryl substituted with one or more substituents selected from halo claim 4 , unsubstituted alkyl claim 4 , alkenyl claim 4 , OCF claim 4 , NO claim 4 , CN claim 4 , NC claim 4 , OH claim 4 , alkoxy claim 4 , haloalkoxy claim 4 , amino claim 4 , COH ...

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25-04-2013 дата публикации

METHOD OF MAKING COUPLED HETEROARYL COMPOUNDS VIA REARRANGEMENT OF HALOGENATED HETEROAROMATICS FOLLOWED BY OXIDATIVE COUPLING

Номер: US20130102785A1
Принадлежит: GEORGIA TECH RESEARCH CORPORATION

The inventions disclosed and described herein relate to new and efficient generic methods for making a wide variety of compounds having Formulas (I) and (II) as shown below (Formulas (I) and (II)) wherein HAr is an optionally substituted five or six membered heteroaryl ring, and Hal is a halogen, and Y is a bridging radical, such as S, Se, NRC(O), C(O)C(O), Si(R), SO, SO, PR, BR, C(R)or P(O)R. The synthetic methods employ a “Base-Catalyzed Halogen Dance” reaction to prepare a metallated compound comprising a five or six membered heteroaryl ring comprising a halogen atom, and then oxidatively coupling the reactive intermediate compound. The compounds of Formula (II) and/or oligomer or polymers comprising repeat units having Formula (II) can be useful for making semi-conducting materials, and/or electronic devices comprising those materials. 2. The method of wherein Hal is Br or I.3. The method of wherein HAr is an optionally substituted five membered heteroaryl ring.87. The method of any one of - wherein Ris a C-Caryl or heteroaryl optionally substituted by one to four ring substituents independently selected from halides claims 4 , alkyl claims 4 , alkynyl claims 4 , perfluoroalkyl claims 4 , alkoxide claims 4 , perfluoroalkoxide claims 4 , —Sn(R) claims 4 , —Si(R) claims 4 , —Si(OR)or —B(—OR)wherein each Ris an independently selected alkyl or aryl claims 4 , and each Ris an independently selected alkyl or aryl claims 4 , or the Rgroups together form an optionally substituted alkylene group to form a ring bridging the oxygen atoms.1110. The method of any one of - wherein the strongly basic compound is an alkyl lithium compound.1210. The method of any one of - wherein the strongly basic compound is a lithium dialkylamide compound.1310. The method of any one of - wherein the oxidizing agent is a Cu(II) salt.1410. The method of any one of - wherein the bishalo-bisheteroaryl compound is a 2 claims 1 ,2′-bishalo-1 claims 1 ,1′-bisheteroaryl compound.21. The method of ...

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09-05-2013 дата публикации

NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A

Номер: US20130116229A1
Принадлежит:

The present invention relates to compounds which are inhibitors of phosphodiesterase type 10A and to their use for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders. 2. The compound of claim 1 , where Ris selected from the group consisting of halogen claim 1 , CN claim 1 , OH claim 1 , C-C-alkyl claim 1 , fluorinated C-C-alkyl claim 1 , C-C-alkoxy claim 1 , fluorinated C-C-alkoxy claim 1 , C-C-cycloalkyl claim 1 , fluorinated C-C-cycloalkyl claim 1 , N(R)(R) claim 1 , C-C-alkyl-N(R)(R) claim 1 , C(O)O—R claim 1 , C(O)N(R)(R) claim 1 , N(R)S(O)(R) and S(O)N(R)(R).3. The compound of claim 1 , where Xis C—H.4. The compound of claim 1 , where Xis N.5. The compound of claim 1 , where Xis C—R.6. The compound of claim 1 , where Xis N.7. The compound of claim 1 , where Y is O.8. The compound of claim 1 , where Ris C-C-alkyl claim 1 , C-C-cycloalkyl or C-C-cycloalkylmethyl.9. The compound of claim 8 , where Ris a radical of the formula CHRR claim 8 , where Ris selected from the group consisting of hydrogen and C-C-alkyl and where Ris selected from the group consisting of C-C-alkyl.10. The compound of claim 1 , where Ris a moiety Z—Ar.11. The compound of claim 1 , where Ris a radical of the formula CRRR.12. The compound of claim 11 , where{'sup': 21', '22', 'g', 'h', 'h', 'g, 'sub': '2', 'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'Rand Rtogether with the carbon atom, to which they are bound form a saturated 5- to 7-membered carbocyclic ring or a saturated 5- to 7-membered heterocyclic ring which has 1, 2 or 3 heteroatoms or heteroatom containing groups selected from the group of O, N, S, SO and SOas ring members, where the carbocyclic ring and the heterocyclic ring may be unsubstituted or may be substituted by 1, 2 or 3 identical or different ...

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09-05-2013 дата публикации

3-aminopyrrolidine derivatives as modulators of chemokine receptors

Номер: US20130116230A1
Принадлежит: Incyte Corp

The present invention relates to 3-aminopyrrolidine derivatives of the formula I: (wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , X, Y and X are as defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of chemokine receptors and more specifically as a modulator of the CCR2 and/or CCR5 receptor. The compounds and compositions of the invention may bind to chemokine receptors, e.g., the CCR2 and/or CCR5 chemokine receptors, and are useful for treating diseases associated with chemokine, e.g., CCR2 and/or CCR5, activity, such as atherosclerosis, restenosis, lupus, organ transplant rejection and rheumatoid arthritis.

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09-05-2013 дата публикации

IRE-1alpha INHIBITORS

Номер: US20130116247A1
Принадлежит: MANNKIND CORPORATION

Compounds which directly inhibit IRE-1α activity in vitro, prodrugs, and pharmaceutically acceptable salts there-of. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response or with regulated IRE1-dependent decay (RIDD) and can be used as single agents or in combination therapies. 114-. (canceled)16. A product comprising a compound of , wherein the product is selected from the group consisting of (a) a pharmaceutical composition comprising the compound of and a pharmaceutically acceptable vehicle; and (b) a complex comprising IRE-1α and the compound of .17. A method of inhibiting IRE-1α activity claim 15 , comprising contacting IRE-1α with a compound of or a prodrug or pharmaceutically acceptable salt thereof.18. The method of wherein the IRE-1α activity is selected from the group consisting of cleavage of RNA claim 17 , cleavage of mRNA claim 17 , RNA splicing claim 17 , and mRNA splicing.19. The method of wherein the IRE-1α activity is cleavage of mRNA and wherein the mRNA is selected from the group consisting of Blos1 mRNA claim 18 , DGAT2 mRNA claim 18 , CD59 mRNA claim 18 , and IRE-1α mRNA.20. The method of claim 18 , wherein the IRE-1α activity is inhibited to treat a disorder associated with the unfolded protein response claim 18 , comprising administering to a patient in need thereof the compound of or the prodrug or pharmaceutically acceptable salt thereof.21. The method of further comprising administering a therapeutic agent that induces or up-regulates IRE-1α expression.2202. The method of claim further comprising administering a therapeutic agent which is less effective when IRE-1α is expressed.23. The method of claim 20 , further comprising administering to the patient a proteasome inhibitor.24. The method of claim 20 , wherein the IRE-1α activity is inhibited to treat a disorder associated with a target of regulated IRE 1-dependent decay (RIDD) claim 20 , comprising administering to a patient in need ...

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09-05-2013 дата публикации

LIPOIC ACID AND NITROXIDE DERIVATIVES AND USES THEREOF

Номер: US20130116284A1
Автор: Salzman Andrew Lurie
Принадлежит: RADIKAL THERAPEUTICS INC.

Provided are bifunctional compounds comprising a poly(ADP-ribose) polymerase (PARP) inhibitor moiety and a reactive oxygen species (ROS) scavenger moiety, more particularly, a lipoic acid or cyclic nitroxide derivative, covalently attached either directly or via a linker, as well as pharmaceutical compositions comprising them. The compounds and pharmaceutical compositions are useful for prevention, treatment, or management of diseases, disorders and conditions associated with elevated PARP activity or expression. 3. The compound of claim 2 , wherein said PARP inhibitor moiety is the radical of the formula A claim 2 , wherein Y and Z are each H; the radical of the formula A claim 2 , wherein Z is H; or the radical of the formula A claim 2 , wherein Y and Z are each H.5. The compound of claim 1 , wherein said PARP inhibitor is selected from the group consisting of benzamide derivatives claim 1 , benzimidazole derivatives claim 1 , phthalizinone derivatives claim 1 , isoindolinone derivatives claim 1 , phenanthridinone derivatives claim 1 , and indenoisoquinolinone derivatives.7. The compound of claim 1 , wherein X represents:{'sub': 1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6, 'one divalent moiety selected from the group consisting of —O—, —S—, CO—, —NH—, —NHCONH—, —(C-C)alkylene-, —N—(C-C)alkylene-, —(C-C)alkylene-O—CO—(C-C)alkylene-, —(C-C)alkylene-O—CO—, —(C-C)alkylene-NH—CO—(C-C)alkylene-, —(C-C)alkylene-NH—CO—, —O—(C-C)alkylene-, —O—CO—(C-C)alkylene-, and —O—C(O)—;'}{'sub': a', 'b', 'a', '6', '14', '4', '12', '2', '2', '1', '4', '1', '4', '1', '4', 'b', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6, 'two divalent moieties linked to each other —X—X—, wherein Xis selected from the group consisting of pyrrolidine-diyl, piperidine-diyl, (C-C)arylene-diyl, (C-C)cycloalkane-diyl, and 4-12-membered heterocyclic-diyl, optionally substituted with one or more ...

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16-05-2013 дата публикации

Novel nicotine derivatives

Номер: US20130123106A1
Автор: Gandhi Paresh T.
Принадлежит:

Described are novel nicotine derivatives represented by general formulas (I) and (III), and salts thereof, and herbicide & pharmaceutical compositions containing the same as the active ingredient. The compound and salts thereof can control annual or perennial weed growing on the land where various crops such as rice plant, wheat, cotton and corn grow for a wide period ranging from the pre-emergence to growth in a remarkably small dose. The compounds and salts thereof can be useful as an anti-microbial and anti-fungal agents and also for the treatment of blood pressure, skeletal muscle, attention deficit disorder, mental disorders, schizophrenia, Alzheimer disease, Parkinson's disease and depression. Also described is the preparation of the nicotine derivatives having formula (I) and (III). 2. The compound as claimed in claim 1 , which is selected from the group consisting of:3-(5-(5-acetylthiophen-2-yl)nicotinoyl)-1-methylpyrrolidin-2-one;3-(5-(4-fluorophenyl)nicotinoyl)-1-methylpyrrolidin-2-one;3-(5-(1-methyl-2-oxopyrrolidine-3-carbonyl)pyridin-3-yl)benzaldehyde;1-methyl-3-(5-m-tolylnicotinoyl)pyrrolidin-2-one;3-(5-(4-chlorophenyl)nicotinoyl)-1-methylpyrrolidin-2-one;4-(5-(1-methyl-2-oxopyrrolidine-3-carbonyl)pyridin-3-yl)benzaldehyde;3-(5-(3-methoxyphenyl)nicotinoyl)-1-methylpyrrolidin-2-one;3-(5-(4-methoxyphenyl)nicotinoyl)-1-methylpyrrolidin-2-one;1-methyl-3-(5-p-tolylnicotinoyl)pyrrolidin-2-one;1-methyl-3-(5-phenylnicotinoyl)pyrrolidin-2-one;3-(5-(3-fluorophenyl)nicotinoyl)-1-methylpyrrolidin-2-one;1-methyl-3-(5-(3-nitrophenyl)nicotinoyl)pyrrolidin-2-one;3-(5-(2-methoxyphenyl)nicotinoyl)-1-methylpyrrolidin-2-one;1-methyl-3-(5-o-tolylnicotinoyl)pyrrolidin-2-one;3-(5-(3,5-dichlorophenyl)nicotinoyl)-1-methylpyrrolidin-2-one;1-methyl-3-(5-(naphthalen-1-yl)nicotinoyl)pyrrolidin-2-one;3-(5-(3-acetylphenyl)nicotinoyl)-1-methylpyrrolidin-2-one;3-(5-cyclopropylnicotinoyl)-1-methylpyrrolidin-2-one;1-methyl-3-(5-(naphthalen-2-yl)nicotinoyl)pyrrolidin-2-one;4-(5-(1-methyl- ...

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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

2-Thiopyrimidinones

Номер: US20130123230A1
Принадлежит:

Myeloperoxidase inhibitors, pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat, for example, cardiovascular conditions. 111.-. (canceled)12. The compound 2-(6-(5-chloro-2-methoxyphenyl)-4-oxo-2-thioxo-3 ,4-dihydropyrimidin-1(2H)-yl)acetamide or a pharmaceutically acceptable salt thereof.13. (canceled)15. A method of treating cardiovascular conditions comprising administering to a mammal in need of such treatment a therapeutically effective amount of a compound of or a prodrug thereof or a pharmaceutically acceptable salt of said compound or of said prodrug.16. A method as recited in wherein the cardiovascular condition is heart failure claim 15 , congestive heart failure claim 15 , peripheral arterial disease claim 15 , pulmonary hypertension or vasculitis.17. A method as recited in wherein the mammal has unstable angina or has experienced myocardial infarction.18. A pharmaceutical composition which comprises a therapeutically effective amount of a compound of or a prodrug thereof or a pharmaceutically acceptable salt of said compound or of said prodrug and a pharmaceutically acceptable carrier claim 12 , vehicle or diluent.19. A pharmaceutical combination composition comprising: a therapeutically effective amount of a composition comprising:{'claim-ref': {'@idref': 'CLM-00012', 'claim 12'}, 'a first compound, said first compound being a compound of , a prodrug thereof, or a pharmaceutically acceptable salt of said compound or of said prodrug;'}a second compound, said second compound being an angiotensin converting enzyme inhibitor, a HMG-CoA reductase inhibitor, a non-steroidal anti-inflammatory agent, a Factor Xa inhibitor or warfarin; anda pharmaceutical carrier, vehicle or diluents.2029.-. (canceled) This nonprovisional application claims priority from U.S. Provisional Application No. 61/558,605, filed on Nov. 11, 2011.This invention relates to compounds that are myeloperoxidase inhibitors, pharmaceutical compositions ...

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16-05-2013 дата публикации

COMPOUNDS AND METHODS FOR THE TREATMENT OR PREVENTION OF FLAVIVIRUS INFECTIONS

Номер: US20130123242A1

The present invention provides novel compounds represented by formula I: 197.-. (canceled)101. A compound according to claim 98 , wherein Z is H.102. A compound according to claim 98 , wherein Ris Calkyl claim 98 , Caryl claim 98 , or Cheterocycle claim 98 , which in each case is substituted or unsubstituted.103. A compound according to claim 98 , wherein Ris H claim 98 , Calkyl claim 98 , Caralkyl claim 98 , Cheterocycle claim 98 , or Cheteroaralkyl claim 98 , which in each case is substituted or unsubstituted.104. A compound according to claim 98 , wherein{'sub': 3', '3', '3', '12', '3', 'c', 'd', '13', '14', '1-6', '2-6', '2-6', '6-12', '6-12', '1-6', '2-6', '2-6', '6-12', '1-6', '2-6', '2-6', '6-12', '6-12', '3-10', '13', '14', '12, 'Ris H, or Ris methyl, ethyl, isopropyl, cyclopropyl, cyclohexyl, allyl, piperidinyl, piperazinyl, pyrrolidinyl, azetidinyl, aziridinyl, pyridinyl, piperidinylmethyl, dioxanyl, azepanyl or benzyl, which in each case is unsubstituted or substituted by one or more substituents chosen from halogen, nitro, nitroso, SOR, PORR, CONRR, Calkyl, Calkenyl, Calkynyl, Caralkyl, Caryl, Calkyloxy, Calkenyloxy, Calkynyloxy, Caryloxy, C(O)Calkyl, C(O)Calkenyl, C(O)Calkynyl, C(O)Caryl, C(O)Caralkyl, Cheterocycle, hydroxyl, NRR, C(O)OR, cyano, azido, amidino, and guanido; and'}{'sub': 12', 'c', 'd', '13', '14', '1-12', '2-12', '2-12', '6-14', '3-12', '3-18', '6-18, 'R, R, R, Rand Rare each independently H, Calkyl, Calkenyl, Calkynyl, Caryl, Cheterocycle, Cheteroaralkyl, or Caralkyl,'}{'sub': c', 'd, 'or Rand R, taken together with the oxygens, form a 5 to 10 membered heterocycle,'}{'sub': 13', '14, 'or Rand R, taken together with the nitrogen, form a 3 to 10 membered heterocycle.'}105. A compound according to claim 104 , wherein Ris isopropyl or cyclohexyl claim 104 , which in each case is substituted or unsubstituted.106. A compound according to claim 98 , wherein Ris Calkyl claim 98 , Caryl claim 98 , or Cheterocycle claim 98 , which in each case is ...

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16-05-2013 дата публикации

2,3,5-Trisubstituted Thiophene Compounds and Uses Thereof

Номер: US20130123252A1
Принадлежит: NOVARTIS AG

The present invention provides a compound of formula I: 5. The compound of claim 1 , wherein Ris tert-butylethynyl claim 1 , phenyl claim 1 , or phenyl para-substituted with F claim 1 , Cl claim 1 , Me.6. The compound of claim 5 , wherein Ris tert-butylethynyl.7. The compound of claim 1 , wherein Ris COH.8. The compound of claim 1 , wherein Ris cyclohexyl.9. The compound of claim 3 , wherein Ris hydrogen;{'sub': 10', '1', '6, 'Ris hydrogen or hydroxyC-Calkyl; and'}{'sub': '11', 'Ris hydrogen, methyl, hydroxy or fluoro.'}10. The compound of claim 4 , wherein Ris hydroxyC-Calkyl;{'sub': '11', 'Ris hydrogen or methyl; and'}{'sub': '12', 'Ris hydrogen or methyl.'}11. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , selected from the group consisting of:3-((S)-2-Cyclohexyl-5-oxo-pyrrolidin-1-yl)-5-phenyl-thiophene-2-carboxylic acid;3-(2-Cyclohexyl-6-oxo-piperidin-1-yl)-5-phenyl-thiophene-2-carboxylic acid;3-(3-Cyclohexyl-5-oxo-morpholin-4-yl)-5-phenyl-thiophene-2-carboxylic acid;3-[(R)-2-Cyclohexyl-6-oxo-4-(toluene-4-sulfonyl)-piperazin-1-yl]-5-phenyl-thiophene-2-carboxylic acid;3-(2-Cyclohexyl-6-oxo-piperidin-1-yl)-5-(3,3-dimethyl-but-1-ynyl)-thiophene-2-carboxylic acid;3-((S)-2-Cyclohexyl-6-oxo-piperidin-1-yl)-5-(3,3-dimethyl-but-1-ynyl)-thiophene-2-carboxylic acid;3-(2-Cyclohexyl-6-oxo-piperidin-1-yl)-5-(4-fluoro-phenyl)-thiophene-2-carboxylic acid;3-(2-Cyclohexyl-6-oxo-piperidin-1-yl)-5-p-tolyl-thiophene-2-carboxylic acid;5-(4-Chloro-phenyl)-3-(2-cyclohexyl-6-oxo-piperidin-1-yl)-thiophene-2-carboxylic acid;3-[2-Cyclohexyl-4-(6-dipropylamino-pyridine-3-sulfonyl)-6-oxo-piperazin-1-yl]-5-phenyl-thiophene-2-carboxylic acid;3-{(R)-2-Cyclohexyl-4-[6-((R)-2-methyl-pyrrolidin-1-yl)-pyridine-3-sulfonyl]-6-oxo-piperazin-1-yl}-5-phenyl-thiophene-2-carboxylic acid;3-[(R)-2-Cyclohexyl-6-oxo-4-(6-pyrrolidin-1-yl-pyridine-3-sulfonyl)-piperazin-1-yl]-5-phenyl-thiophene-2-carboxylic acid;3-{(R)-2-Cyclohexyl-4-[6-((2S,5R)-2,5-dimethyl-pyrrolidin-1-yl)- ...

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16-05-2013 дата публикации

Novel triazinedione derivatives as gabab receptor modulators

Номер: US20130123262A1
Принадлежит: Addex Pharmaceuticals SA

The present invention provides novel compounds of formula I wherein W 1 , W 2 , W 3 , W 4 , W 5 , B, X 1 , X 2 , X 3 , X 4 , X 5 , E and L are as defined herein; invention compounds are gamma amino butyrique acid receptor-subtype B (“GABA B ”) positive allosteric modulators (enhancers), which are useful to provide methods of treating or preventing diseases or disorders, including treatment of anxiety, depression, epilepsy, schizophrenia, cognitive disorders, spasticity and skeletal muscle rigidity, spinal cord injury, multiple sclerosis, amyotrophic lateral sclerosis, cerebral palsy, neuropathic pain and craving associated with cocaine and nicotine, panic disorder, posttraumatic stress disorders, urge urinary incontinence, gastroesophageal reflux disease, transient lower oesophageal sphincter relaxations, functional gastrointestinal disorders and irritable bowel syndrome.

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16-05-2013 дата публикации

PYRIDINE NON-CLASSICAL CANNABINOID COMPOUNDS AND RELATED METHODS OF USE

Номер: US20130123304A1

Disclosed are compounds of the formula I: 2. A method according to whereinX is selected from cycloheptyl and cyclohexyl optionally substituted with one to three groups independently selected from halo, carbonyl, hydroxyl, alkyl and alkoxy;Y is selected from carbonyl, dimethylmethylene and hydroxymethylene; andZ is selected from alkyl, cycloalkyl, substituted cycloalkyl, phenyl, substituted phenyl, thiophenyl and substituted thiophenyl.3. A method according to wherein X is selected from cycloheptyl and cyclohexyl optionally substituted with carbonyl or hydroxyl.4. A method according to wherein Y is dimethylmethylene.5. A method according to wherein Z is alkyl claim 2 , phenyl or cycloalkyl.6. A method according to wherein the compound is selected froma) 3-(3-Hydroxycyclohexyl)-6-(2-methyloctan-2-yl)pyridine-2,4-diol;b) 3-(2,4-Dihydroxy-6-(2-methyloctan-2-yl)pyridin-3-yl)cyclohexanone;c) 4-(4,6-Dihydroxy-2-(2-phenylpropan-2-yl)pyridin-5-yl)-6,6-dimethylbicyclo[3.1.1]heptan-2-one;d) 4-Allyl-3-(4,6-dihydroxy-2-(2-phenylpropan-2-yl)pyridin-5-yl)cyclohexanone;e) 6-(2-Cyclohexylpropan-2-yl)-3-(5-hydroxy-2-(3-hydroxypropyl)cyclohexyl)pyridine-2,4-diol; andf) 3-(5-Hydroxy-2-(3-hydroxypropyl)cyclohexyl)-6-(2-(thiophen-2-yl)propan-2-yl)pyridine-2,4-diol. This application is a continuation of and claims priority benefit from application Ser. No. 12/579,282 filed Oct. 13, 2009, which is a continuation in-part of and claims priority benefit from application Ser. No. 12/468,776 filed May 19, 2009 which claims priority benefit from application Ser. No. 61/128,088 filed May 19, 2008, and from prior provisional application Ser. No. 61/105,143 filed Oct. 14, 2008, incorporated herein by reference in its entirety.The classical cannabinoid, delta-9-tetrahydrocannabinol (Δ-THC), is the major active constituent extracted from . The effects of cannabinoids are due to an interaction with specific high-affinity receptors. Presently, two cannabinoid receptors have been characterized: CB-1, a ...

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23-05-2013 дата публикации

Novel Estrogen Receptor Ligands

Номер: US20130131061A1
Принадлежит: KARO BIO AB

The invention provides a compound of formula (I) or a pharmaceutically acceptable ester, amide, carbamate, solvate or salt thereof, including a salt of such an ester, amide or carbamate, and a solvate of such an ester, amide, carbamate or salt. The invention also provides also provides the use of such compounds in the treatment or prophylaxis of a condition associated with a disease or disorder associated with estrogen receptor activity, wherein R, R, R, Rand Rare as defined in the specification. 125.-. (canceled)27. A method as claimed in claim 26 , in which each Ris independently selected from the group consisting of hydrogen claim 26 , Calkyl claim 26 , Calkenyl claim 26 , Calkynyl claim 26 , Ccycloalkyl claim 26 , phenyl and benzyl.28. A method as claimed in claim 27 , in which each Rindependently represents hydrogen or Calkyl.29. A method as claimed in claim 26 , in which each Ris independently selected from the group consisting of hydrogen and Calkyl.30. A method as claimed in claim 26 , in which is selected from the group consisting of OR claim 26 , N(R) claim 26 , —C(O)Calkyl claim 26 , Calkyl claim 26 , Calkenyl claim 26 , Calkynyl claim 26 , haloCalkyl claim 26 , dihaloCalkyl claim 26 , trihaloCalkyl claim 26 , haloCalkenyl claim 26 , dihaloCalkenyl claim 26 , trihaloCalkenyl claim 26 , phenyl claim 26 , and 5-6 membered heterocyclyl claim 26 , wherein said phenyl or heterocyclyl group can either be unsubstituted or substituted by 1 to 3 substituents selected from the group consisting of OR claim 26 , halogen claim 26 , cyano claim 26 , —C(O)Calkyl claim 26 , Calkyl claim 26 , Calkenyl claim 26 , Calkynyl claim 26 , haloCalkyl claim 26 , dihaloCalkyl and trihaloCalkyl.31. A method as claimed in claim 30 , in which Ris selected from the group consisting of OR claim 30 , N(R) claim 30 , —C(O)Calkyl claim 30 , Calkyl claim 30 , Calkenyl claim 30 , Calkynyl claim 30 , phenyl claim 30 , and 5-6 membered heterocyclyl claim 30 , wherein said phenyl or ...

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23-05-2013 дата публикации

Flufenoxine derivatives for the treatment and prevention of amyloid pathologies

Номер: US20130131079A1
Принадлежит: Faes Farma SA

The present invention is directed to a compound of formula (I) for use in a method to treat or ameliorate amyloid or tau pathologies, such as Alzheimer's disease, or symptoms thereof. The invention is also directed to new compounds of formula (I), of subformula (II), (III), (IV), or (V).

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23-05-2013 дата публикации

Novel Dihydropyrimidin-2(1H)-One Compounds As Neurokinin-3 Receptor Antagonists

Номер: US20130131093A1
Автор: Qiu Jian, Sun Xicheng
Принадлежит: N30 PHARMACEUTICALS, INC.

The present invention is directed to novel dihydropyrimidin-2(1H)-one compounds useful as Neurokinin-3 (NK3) receptor antagonists, pharmaceutical compositions comprising such compounds, and methods of making and using the same. 2. The method of treatment of wherein R claim 1 , Rand Rare independently selected from the group consisting of hydrogen and methyl;{'sub': 3', '1', '6, 'Ris selected from the group consisting of hydrogen, nitro, cyano, carboxyl, carbamoyl, methylsulfonamido, fluoro, chloro, bromo, methylsulfonyl, and methylsulfinyl, isoxazol-4-yl, C-Calkoxy, —C(NH)NHOH, sulfonic acid, and acetyl;'}{'sub': '4', 'Ris selected from the group consisting of hydroxy, carboxyl, and tetrazol-5-yl;'}{'sub': 5', '2', '2', '2', '1', '6', '2', '2', '3', '2', '2', '3, 'Ris selected from the group consisting of hydrogen, hydroxyl, carboxy, chloro, fluoro, cyano, —O(CH)NMe, C-Calkyl, —O(CH)OCH, —O(CH)OH, acetyl, CF, methoxy, ethoxy, isopropoxy, and n-propoxy; and'}{'sub': '6', 'Ris hydrogen.'}3. The method of treatment of wherein X is selected from the group consisting of phenyl claim 1 , substituted phenyl claim 1 , thiophen-yl claim 1 , substituted thiophen-yl claim 1 , thiazol-yl claim 1 , substituted thiazol-yl claim 1 , pyrazin-yl claim 1 , substituted pyrazin-yl claim 1 , pyridin-yl claim 1 , and substituted pyridin-yl claim 1 , cyclohexyl claim 1 , and substituted cyclohexyl.4. The method of treatment of wherein X is selected from the group consisting of phenyl claim 1 , thiophen-2-yl claim 1 , thiophen-3-yl claim 1 , thiazol-2-yl claim 1 , 2-fluorophenyl claim 1 , p-tolyl claim 1 , m-tolyl claim 1 , biphenyl-4-yl claim 1 , 4-methoxyphenyl claim 1 , 3-chlorophenyl claim 1 , 3 claim 1 ,4-dichlorophenyl claim 1 , 3-methoxyphenyl claim 1 , 3 claim 1 ,4-dimethoxyphenyl claim 1 , 4-bromophenyl claim 1 , o-tolyl claim 1 , 4-chlorophenyl claim 1 , 2-chlorophenyl claim 1 , 3-cyanophenyl claim 1 , 3 claim 1 ,4-difluorophenyl claim 1 , 4-cyanophenyl claim 1 , 3- ...

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23-05-2013 дата публикации

NOVEL ALKENE OXINDOLE DERIVATIVES

Номер: US20130131114A1
Принадлежит: Hoffmann-La Roche Inc.

The present invention provides compounds of formula (I), 2. The method according to claim 1 , wherein Ris selected from the group consisting of: hydrogen claim 1 , halogen and alkoxy.3. The method according to claim 1 , wherein Ris selected from the group consisting of: hydrogen claim 1 , fluoro and chloro.4. The method according to claim 1 , wherein Ris selected from the group consisting of: hydrogen claim 1 , halogen and alkoxy.5. The method according to claim 1 , wherein Ris hydrogen or fluoro.6. The method according to claim 1 , wherein Ris selected from the group consisting of: hydrogen claim 1 , halogen and alkoxy.7. The method according to claim 1 , wherein Ris selected from the group consisting of: hydrogen claim 1 , fluoro claim 1 , chloro and methoxy.8. The method according to claim 1 , wherein Ris selected from the group consisting of: hydrogen claim 1 , halogen and alkoxy.9. The method according to claim 1 , wherein Ris hydrogen or fluoro.10. The method according to claim 1 , wherein Ris selected from the group consisting of: alkyl claim 1 , halophenylalkyl claim 1 , phenyl claim 1 , substituted phenyl claim 1 , thiophenyl and pyridinyl claim 1 , wherein said substituted phenyl is phenyl substituted with one to three substituents independently selected from the group consisting of alkyl claim 1 , alkoxy claim 1 , halogen claim 1 , cyano claim 1 , haloalkyl claim 1 , alkylsulfanyl claim 1 , aminosulfonyl claim 1 , alkylsulfonyl claim 1 , haloalkoxy and alkylcarbonyl.11. The method according to claim 1 , wherein Ris halophenyl or cyanophenyl.12. The method according to claim 1 , wherein Ris chlorophenyl or cyanophenyl.13. The method according to claim 1 , wherein Ris selected from the group consisting of: alkyl claim 1 , hydroxyalkyl claim 1 , cycloalkyl claim 1 , phenyl and halophenyl.14. The method according to claim 1 , wherein Ris alkyl or phenyl.15. The method according to claim 1 , wherein Ris isopropyl or phenyl.16. The method according to claim 1 , ...

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23-05-2013 дата публикации

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

Номер: US20130131321A1
Принадлежит: GRAFFINITY PHARMACEUTICALS GMBH

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

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30-05-2013 дата публикации

Heterocyclic compound and use thereof

Номер: US20130137675A1
Принадлежит: Takeda Pharmaceutical Co Ltd

The present invention aims to provide a compound having a PDE inhibitory action and useful as a medicament for the prophylaxis or treatment of schizophrenia and the like. A compound represented by the formula (1 x ): wherein each symbol is as described in the DESCRIPTION, or the formula (1): W 1 —W 2   (1) wherein each symbol is as described in the DESCRIPTION, or a salt thereof.

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30-05-2013 дата публикации

HAEMATOPOIETIC-PROSTAGLANDIN D2 SYNTHASE INHIBITORS

Номер: US20130137684A1
Принадлежит: The University of Queensland

The present invention generally relates to compounds that inhibit haematopoietic-prostaglandin Dsynthase (H-PGDS), to compositions containing them and to their use in treating or preventing conditions and diseases associated with H-PGDS, such as allergies and inflammation. 2. The method according to claim 1 , wherein Y is CH.5. The method according to claim 1 , wherein Ris unsubstituted or substituted thienyl.6. The method according to claim 5 , wherein the thienyl is substituted with one or more of cyano claim 5 , nitro claim 5 , halo claim 5 , —Calkyl claim 5 , —C(═O)—R claim 5 , —C(═O)—O—Ror —O—C(═O)—R; wherein Ris selected H or —Calkyl.7. The method according to claim 1 , wherein Ris —C(═O)—NRR.8. The method according to claim 7 , wherein Ris —CHRR.9. The method according to claim 8 , wherein Ris —CONH claim 8 , —CONR—CHR—CONHor optionally substituted aryl.10. The method according to wherein Rand Rare independently selected from hydrogen or alkyl.11. The method according to claim 8 , wherein Ris hydrogen claim 8 , —Calkyl claim 8 , —Cperfluoroalkyl or —Calkylaryl.12. The method according to claim 7 , wherein Ris hydrogen.13. The method according to wherein Rand Rtogether form a heterocyclyl or heteroaryl ring.16. The method according to claim 1 , wherein the haematopoietic-prostaglandin Dsynthase associated disease or condition is selected from allergies claim 1 , inflammation claim 1 , pain claim 1 , bronchoconstriction claim 1 , muscle necrosis claim 1 , cancer claim 1 , arthritis claim 1 , irritable bowel diseases claim 1 , irritable bowel syndrome claim 1 , skin inflammation and irritation claim 1 , or cardiovascular diseases or conditions.19. The compound according to claim 17 , wherein L and M are both CR.20. The compound according to wherein each Ris independently selected from hydrogen cyano claim 19 , nitro claim 19 , halo claim 19 , —Calkyl claim 19 , —Calkenyl claim 19 , —Calkynyl claim 19 , —C(═O)—R claim 19 , —C(═O)—O—R claim 19 , —O—C(═O)—R claim ...

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06-06-2013 дата публикации

Novel hydroxamates as therapeutic agents

Номер: US20130142758A1
Принадлежит: Pharmacyclics LLC

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

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06-06-2013 дата публикации

BENZOHETEROCYCLIC ANTI-BACTERIAL AGENTS

Номер: US20130143841A1
Принадлежит: University of Notre Dame du Lac

Embodiments herein provide compounds and methods of making and using such compounds for prevention and treatment of multidrug resistant bacteria. In particular, embodiments are directed to anti-bacterial agents from benzo[d]heterocyclic scaffolds for prevention and treatment of multidrug resistant bacteria. 2. A method of treating a drug-resistant bacterial strain , comprising:{'i': 'Staphylococcus aureus', 'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'administering a compound to an individual infected with or suspected of being infected with a methicillin-resistant strain, a vancomycin-resistant strain, or a linezolid-resistant strain, a compound of .'} This application is a continuation of U.S. patent application Ser. No. 12/995,437, filed Nov. 30, 2010, which is a continuation of International Application No. PCT/US2009/045737, filed May 29, 2009, which claims priority to U.S. Provisional Patent Application No. 61/057,282, filed May 30, 2008, the entire disclosures of which are hereby incorporated by reference in their entirety.This invention was made with government support under Grant No. R01 AI 054193 awarded by the National Institutes of Health. The United States Government has certain rights in the invention.Embodiments herein relate to anti-bacterial agents, and, more specifically, to anti-bacterial agents from benzo[d]heterocyclic scaffolds for prevention and treatment of multidrug resistant bacteria.In 2004, the IDSA (Infectious Disease Society of America) reported that each year 90,000 of the 2 million people who acquire a hospital bacterial infection will die. That is a 4.5% mortality rate arising from just being within the hospital. Multi-drug resistance bacterial strains are a major problem and one that has been increasing very rapidly every year during the last few decades. In brief, from its discovery in 1968 multi-drug resistant (MRSA) had already accounted for greater than 50% of patient isolates by 1999 in ICUs (intensive care units) within ...

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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

Stem cell differentiating agents and uses therefor

Номер: US20130143935A1
Принадлежит: University of Texas System

The present invention relates to screens for compounds that can induce stem cell differentiation. In addition, isoxazoles and sulfonyl hydrazones are identified as general classes of compounds that can induce differentiation of stem cells into cells of neuronal and cardiac fate, respectively.

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13-06-2013 дата публикации

Autotaxin inhibitors and uses thereof

Номер: US20130150326A1
Принадлежит: Amira Pharmaceuticals Inc

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

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13-06-2013 дата публикации

Derivatives of 1-Phenyl-1,5-Dihydro-Benzo[B] [1,4]Diazepine-2,4-Dione as Inhibitors of HIV Replication

Номер: US20130150350A1
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

Compounds of formula (I) wherein m, R, R, R, X and Y are defined herein, are useful as inhibitors of HIV replication. 2. The compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris phenyl.3. The compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris thiophene.4. The compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein m is 1 and Ris selected from Cl claim 1 , F claim 1 , CHand CF.5. The compound according to claim 4 , or a pharmaceutically acceptable salt thereof claim 4 , wherein Ris CF.6. The compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris H or (C)alkyl.12. (canceled)13. A pharmaceutical composition comprising a a compound of formula (I) claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , according to and a pharmaceutically acceptable carrier.14. (canceled)15. A method for treating HIV which comprises administering to a host infected by HIV a therapeutically effective amount of a compound according to . This application claims benefit of U.S. Ser. No. 61/305,108, filed Feb. 16, 2010, herein incorporated by reference.The present invention relates to compounds and their use as inhibitors of capsid assembly, pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of human immunodeficiency virus (HIV) infection.To date, over 20 FDA-approved drugs make up the antiretroviral arsenal against HIV (1). These compounds generally target the viral enzymes or the viral entry process and can be divided within 6 mechanistic classes. The standard of care is a multi-drug therapeutic regime, often referred to as highly active antiretroviral therapy (HAART), where combinations of at least three drugs targeting the virus are administered. Although HAART can successfully restrict viral replication for many years, drug resistance can still ...

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20-06-2013 дата публикации

HETEROARYL COMPOUNDS AND METHODS OF USE THEREOF

Номер: US20130158003A1
Принадлежит: SUNOVION PHARMACEUTICALS INC

Provided herein are heteroaryl compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. In one embodiment, the compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as CNS disorders and metabolic disorders, including, but not limited to, e.g., neurological disorders, psychosis, schizophrenia, obesity, and diabetes. 2. The compound of claim 1 , wherein L is —CH—CH— claim 1 , —CH═CH— claim 1 , —O—CH— claim 1 , —NH—CH— claim 1 , —CH—NH— claim 1 , —CH—S— claim 1 , or —S—.3. The compound of claim 2 , wherein L is —CH—CH—.5. The compound of claim 4 , wherein Ais NR; and Ris (i) hydrogen; or (ii) (C-C)alkyl claim 4 , (C-C)alkenyl claim 4 , (C-C)heteroalkyl claim 4 , (C-C)cycloalkyl claim 4 , (6 to 10 membered) aryl claim 4 , (5 to 10 membered) heteroaryl claim 4 , (3 to 12 membered)heterocyclyl claim 4 , carbonyl claim 4 , or sulfonyl claim 4 , each of which is optionally substituted with one or more R; or (iii) Rand Rtogether with the atoms to which they are attached form a ring optionally substituted with one or more R.6. The compound of claim 5 , wherein Ris H or CH.8. The compound of claim 7 , wherein Ris (i) hydrogen; or (ii) alkyl claim 7 , aryl claim 7 , or heteroaryl claim 7 , each of which is optionally substituted with one or more R.9. The compound of claim 7 , wherein Ris (i) hydrogen; or (ii) alkyl claim 7 , aryl claim 7 , or heteroaryl claim 7 , each of which is optionally substituted with one or more R.10. The compound of claim 7 , wherein Ris (i) hydrogen; or (ii) alkyl claim 7 , aryl claim 7 , or heteroaryl claim 7 , each of which is optionally substituted with one or more R.11. The compound of claim 7 , wherein each occurrence of Ris independently (i) hydrogen; or (ii) alky claim 7 , aryl or heteroaryl claim 7 , each of which is optionally substituted with one or more R.14. The compound of any claim 4 , wherein Rand Rtogether with the ...

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27-06-2013 дата публикации

JAK1 Inhibitors

Номер: US20130165440A1
Принадлежит: Exelixis, Inc.

JAK1 inhibitors of structural formula (I), wherein Ar, Ar, Q, W, X, Y, and Z are defined in the specification, pharmaceutically acceptable salts thereof, compositions thereof, and use of the compounds and compositions for treating diseases. The invention also comprises use of the compounds in and for the manufacture of medicaments, particularly for treating diseases. 2. The compound according to wherein:{'sup': 1', '1', '2, 'Aris phenyl optionally substituted with 1-2 Rgroups, or heteroaryl optionally substituted with 1-2 Rgroups;'}{'sup': 2', '5, 'Aris phenyl optionally substituted with 1-3 Rgroups;'}{'sup': 1', '3', '3', '4', '3', '4', '3, 'sub': '2', 'each Ris independently —C(O)OR, —C(O)R, —C(O)N(H)alkylR, —N(H)C(O)alkyl, —C(O)N(R)(R), or —SOR;'}{'sup': 2', '3', '4', '3, 'each Ris independently —N(R)(R), alkyl, or —C(O)OR;'}{'sup': '3', 'Ris H or alkyl;'}{'sup': '4', 'Ris H or alkyl optionally substituted with heterocyclyl;'}{'sup': 5', '3', '6', '6', '3', '6', '3, 'each Ris independently halo, —CN, —C(O)OR, R, —OR, —N(R)R, alkyl optionally substituted with 1-3 halo, alkoxy optionally substituted with 1-3 halo, or heterocyclyl optionally substituted with R;'}{'sup': 6', '3', '7, 'Ris alkyl optionally substituted with —NRR;'}{'sup': '7', 'Ris H or alkyl;'}Q is C(H) or N;W is C(H) or N;X is C(H) or N;Y is C(H) or N; andZ is C(H) or N.4. The compound according to claim 3 , wherein:{'sup': 1', '1', '2, 'Aris phenyl optionally substituted with 1-2 Rgroups or heteroaryl optionally substituted with 1-2 Rgroups, wherein the heteroaryl is 1H-indazolyl, pyrazolyl, benzotriazolyl, or benzofuranyl, isoindolyl;'}{'sup': 5', '3', '6', '6', '3', '6', '3, 'sub': 1', '3, 'each Ris independently halo, —CN, —C(O)OR, R, —OR, —N(R)R, (C-C)alkyl optionally substituted with 1-3 halo, alkoxy optionally substituted with 1-3 halo, or heterocyclyl optionally substituted with R; and'}{'sup': '7', 'sub': 1', '3, 'Ris H or (C-C)alkyl.'}12. A composition comprising a compound according to and ...

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04-07-2013 дата публикации

SULFONAMIDE COMPOUNDS

Номер: US20130172339A1
Принадлежит: KANCERA AB

A compound of formula (I), wherein A is S, O or a double bond, and L is a substituted thiazolyl, phenyl or pyridyl. The compound is useful for the treatment of inflammation and cancer. 119-. (canceled)21. The compound of claim 20 , wherein A is O or S; or a pharmaceutically acceptable salt claim 20 , hydrate claim 20 , solvate claim 20 , or N-oxide thereof.22. The compound of claim 21 , wherein A is S; or a pharmaceutically acceptable salt claim 21 , hydrate claim 21 , solvate claim 21 , or N-oxide thereof.23. The compound of claim 21 , wherein{'sup': '1', 'Ris selected from H; halogen; and C1-C6 alkyl optionally substituted with at least one halogen; and'}{'sup': 2', '3', '6', '6, 'Rand Rform, together with the carbon atoms to which they are attached, a benzene ring, optionally substituted with at least one R; or a 5- or 6-membered heteroaromatic or heterocyclic ring, optionally substituted with at least one R; or'}{'sup': 1', '2', '6', '6, 'Rand Rform, together with the carbon atoms to which they are attached, a benzene ring optionally substituted with at least one R; or a 5- or 6-membered heteroaromatic or heterocyclic ring, optionally substituted with at least one R; and'}{'sup': '3', 'Ris selected from H; halogen; C1-C6 alkyl optionally substituted with at least one halogen;'}or a pharmaceutically acceptable salt, hydrate, solvate, or N-oxide thereof.24. The compound of claim 21 , wherein{'sup': '1', 'Ris selected from H; halogen; and C1-C6 alkyl optionally substituted with at least one halogen;'}{'sup': 2', '3', '6', '6', '6, 'claim-text': [{'sup': 2', '3, 'at least one of Rand Ris selected from said phenyl, heteroaryl, arylsulfonyl and heteroarylsulfonyl, and'}, {'sup': 2', '3, 'when L is (a), neither Rnor Ris unsubstituted phenyl;'}], 'Rand Rare independently selected from H; halogen; C1-C6 alkyl optionally substituted with at least one halogen; phenyl optionally substituted with at least one R; 5- or 6-membered heteroaryl optionally substituted with at ...

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04-07-2013 дата публикации

4-oxoquinoline compound and use thereof as hiv integrase inhibitor

Номер: US20130172344A1
Принадлежит: Japan Tobacco Inc

An anti-HIV agent containing, as an active ingredient, a 4-oxoquinoline compound represented by the following formula [I] wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof. The compound of the present invention has HIV integrase inhibitory action and is useful as an anti-HIV agent for the prophylaxis or therapy of AIDS. Moreover, by a combined use with other anti-HIV agents such as protease inhibitors, reverse transcriptase inhibitors and the like, the compound can become a more effective anti-HIV agent. Since the compound has high inhibitory activity specific for integrases, it can provide a safe pharmaceutical agent with a fewer side effects for human.

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04-07-2013 дата публикации

ARYLOSULFONAMIDES FOR THE TREATMENT OF CNS DISEASES

Номер: US20130172365A1
Принадлежит: ADAMED SP. Z.O.O.

Arylsulphonamide derivatives of formula (I) and pharmaceutically acceptable salts thereof. The compounds may be useful for the treatment and/or prevention of disorders of the central nervous system. 5. (canceled)6. The compound or salt according to claim 1 , wherein E represents N.7. The compound or salt according to claim 1 , wherein E represents CH.8. The compounds according to claim 1 , wherein E represents C.9. The compound or salt according to claim 1 , wherein D represents unsubstituted phenyl or phenyl substituted with one or more substituents independently selected from the group consisting of branched C-C-alkyl; straight C-C-alkyl in ortho or meta position with respect to sulphonamide group; C-C-alkyloxy; halogeno-C-C-alkyl; halogeno-C-C-alkyloxy; halogen atom; —CN; —OH; and phenyl.10. The compound or salt according to claim 1 , wherein D represents unsubstituted naphthyl or naphthyl substituted with one or more substituents independently selected from the group consisting of C-C-alkyl; C-C-alkyloxy; halogeno-C-C-alkyl; halogen atom; —CN; —OH; and phenyl.1112-. (canceled)13. The compound or salt according to claim 1 , wherein D represents benzene ring fused with 5-membered aromatic heterocyclic ring having 1 to 3 heteroatoms independently selected from the group consisting of N claim 1 , O claim 1 , S claim 1 , and wherein D is unsubstituted or substituted with one or more substituents independently selected from the group consisting of C-C-alkyl; C-C-alkyloxy; halogeno-C-C-alkyl; halogen atom claim 1 , —CN; —OH; and phenyl.1418-. (canceled)19. The compound or salt according to claim 1 , wherein n is 2.20. The compound or salt according to claim 1 , wherein n is 3.21. The compound or salt according to claim 1 , wherein n is 4.22. (canceled)23. The compound or salt according to claim 1 , wherein A is linked to E through carbon atom of heterocyclic ring.24. The compound according to selected from the group consisting of the following compounds:N-(4-(4-(1,2- ...

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04-07-2013 дата публикации

P2X4 RECEPTOR ANTAGONIST

Номер: US20130172550A1
Принадлежит: NIPPON CHEMIPHAR CO., LTD.

A diazepine derivative having the following formula (III) or a pharmacologically acceptable salt thereof is used as A P2Xreceptor antagonist: 122-. (canceled)25. A diazepine derivative or a pharmacologically acceptable salt thereof defined in claim 24 , wherein Ris hydrogen claim 24 , a Calkyl group claim 24 , a Calkenyl group claim 24 , a Calkyl group having one to three halogen atoms claim 24 , a halogen atom claim 24 , hydroxyl claim 24 , amino claim 24 , a Calkylamino group claim 24 , a Cdialkylamino group claim 24 , or a Cacylamino group.26. A diazepine derivative or a pharmacologically acceptable salt thereof defined in claim 24 , wherein Ris hydrogen claim 24 , a Calkyl group claim 24 , a Calkoxy group claim 24 , a Calkyl group having one to three halogen atoms claim 24 , a Calkoxy group having one to three halogen atoms claim 24 , a halogen atom claim 24 , hydroxyl claim 24 , nitro claim 24 , cyano claim 24 , amino claim 24 , a Calkylamino group claim 24 , a Cdialkylamino group claim 24 , a Cacylamino group claim 24 , or a Cacylamino group having one to three halogen atoms.27. A diazepine derivative or a pharmacologically acceptable salt thereof defined in claim 24 , wherein Ris hydrogen claim 24 , a Calkyl group claim 24 , or a Calkyl group having one to three halogen atoms.28. A diazepine derivative or a pharmacologically acceptable salt thereof defined in claim 24 , wherein each of Rand Rindependently is hydrogen claim 24 , a Calkyl group claim 24 , or a Calkyl group having one to three halogen atoms.29. A diazepine derivative or a pharmacologically acceptable salt thereof defined in claim 24 , wherein Ris hydrogen claim 24 , a Calkyl group claim 24 , a Calkenyl group claim 24 , a Calkoxy group claim 24 , a Calkyl group having one to three halogen atoms claim 24 , a Calkoxy group having one to three halogen atoms claim 24 , a halogen atom claim 24 , hydroxyl claim 24 , nitro claim 24 , cyano claim 24 , amino claim 24 , a Calkylamino group claim 24 , a ...

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11-07-2013 дата публикации

Novel Substituted Quinoline Compounds as S-Nitrosoglutathione Reductase Inhibitors

Номер: US20130178499A1
Принадлежит: N30 PHARMACEUTICALS, INC.

The present invention is directed to novel quinoline compounds useful as S-nitrosoglutathione reductase (GSNOR) inhibitors, pharmaceutical compositions comprising such compounds, and methods of making and using the same. 3. The compound of wherein m is selected from the group consisting of 0 and 1; Rand Rare independently selected from the group consisting of hydrogen claim 1 , chloro claim 1 , fluoro claim 1 , methyl claim 1 , trifluoromethyl claim 1 , cyano claim 1 , methoxy claim 1 , and N(CH); n is selected from the group consisting of 0 and 1; and Ris independently selected from the group consisting of fluoro claim 1 , chloro claim 1 , bromo claim 1 , methyl claim 1 , trifluoromethyl claim 1 , cyano claim 1 , hydroxy claim 1 , methoxy claim 1 , and N(CH).5. The compound of wherein A is COOH.6. The compound of selected from the group consisting of4-(6-hydroxy-3-methylquinolin-2-yl)benzoic acid;2-(4-(1H-tetrazol-5-yl)phenyl)-3-methylquinolin-6-ol;4-(6-hydroxyquinolin-2-yl)benzoic acid;2-(4-(1H-tetrazol-5-yl)phenyl)quinolin-6-ol;1-(6-hydroxyquinolin-2-yl)piperidine-4-carboxylic acid;(1r,4r)-4-(6-hydroxyquinolin-2-yl)cyclohexanecarboxylic acid;(1s,4s)-4-(6-hydroxyquinolin-2-yl)cyclohexanecarboxylic acid;3-chloro-4-(6-hydroxyquinolin-2-yl)benzoic acid;2-chloro-4-(6-hydroxyquinolin-2-yl)benzoic acid;2-fluoro-4-(6-hydroxyquinolin-2-yl)benzoic acid;2-(4-(2H-tetrazol-5-yl)phenyl)-4-chloroquinolin-6-ol;3-(4-(6-hydroxyquinolin-2-yl)phenyl)-1,2,4-oxadiazol-5(2H)-one;3-fluoro-4-(6-hydroxyquinolin-2-yl)benzoic acid;4-(6-hydroxyquinolin-2-yl)-3-methoxybenzoic acid;5-(6-hydroxyquinolin-2-yl)thiophene-2-carboxylic acid;4-(6-hydroxyquinolin-2-yl)cyclohex-3-enecarboxylic acid;4-(3-fluoro-6-hydroxyquinolin-2-yl)benzoic acid;4-(4-chloro-3-fluoro-6-hydroxyquinolin-2-yl)benzoic acid;4-(3-chloro-6-hydroxyquinolin-2-yl)benzoic acid;3-(2-fluoro-4-(6-hydroxyquinolin-2-yl)phenyl)-1,2,4-oxadiazol-5(4H)-one;3-(3-fluoro-4-(6-hydroxyquinolin-2-yl)phenyl)-1,2,4-oxadiazol-5(4H)-one;4-(4-chloro- ...

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11-07-2013 дата публикации

Transition-Metal-Catalyzed Carbon-Nitrogen and Carbon-Carbon Bond-Forming Reactions

Номер: US20130178632A1
Принадлежит: Massachusetts Institute of Technology

One aspect of the present invention relates to ligands for transition metals. A second aspect of the present invention relates to the use of catalysts comprising these ligands in various transition-metal-catalyzed carbon-heteroatom and carbon-carbon bond-forming reactions. The subject methods provide improvements in many features of the transition-metal-catalyzed reactions, including the range of suitable substrates, number of catalyst turnovers, reaction conditions, and efficiency. For example, improvements have been realized in transition metal-catalyzed: aryl amination reactions; aryl amidation reactions; Suzuki couplings; and Sonogashira couplings. In certain embodiments, the invention relates to catalysts and methods of using them that operate in aqueous solvent systems. 112-. (canceled)14. The method of claim 13 , wherein the transition metal is palladium.15. The method of claim 14 , further comprising irradiating with microwave radiation.16. The method of claim 14 , wherein R is cyclohexyl; Ris hydrogen; Rand Rare selected independently from the group consisting of hydrogen claim 14 , alkyl and alkoxy; Ris R; and Rand Rare hydrogen.17. The method of claim 14 , wherein R is cyclohexyl; Ris hydrogen; Rand Rare selected independently from the group consisting of hydrogen claim 14 , alkyl and alkoxy; Ris R; and Rand Rare hydrogen.18. The method of claim 14 , wherein R is cyclohexyl; Ris hydrogen; Rand Rare methoxy; Ris —S(O)ONa; and Rand Rare hydrogen.19. The method of claim 14 , wherein R is cyclohexyl; Ris hydrogen; Rand Rare isopropyl; Ris —S(O)ONa; and Rand Rare hydrogen. This application claims the benefit of priority to U.S. Provisional Patent Application Ser. No. 60/642,774, filed Jan. 10, 2005; hereby incorporated by reference in its entirety.The present invention was made with support provided by the National Institutes of Health (Grant Number GM-58160); the government, therefore, has certain rights in the invention.Transition metal catalyst complexes ...

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18-07-2013 дата публикации

Novel IDO Inhibitors and Methods of Use Thereof

Номер: US20130183388A1
Принадлежит: LANKENAU INSTITUTE FOR MEDICAL RESEARCH

Novel indoleamine 2,3-dioxygenase (IDO) inhibitors, compositions comprising the same, and methods of use thereof are disclosed. 1. (canceled)3. (canceled)4. (canceled)5. A pharmaceutical composition for the treatment of cancer comprising a pharmaceutically acceptable carrier and an effective amount at least one indoleamine 2 claim 2 ,3-dioxygenase (IDO) inhibitor claim 2 , wherein at least one of said IDO inhibitors is the compound of .616-. (canceled)17. The pharmaceutical composition of claim 5 , further comprising at least one signal transduction inhibitor (STI).18. (canceled)19. (canceled)20. The pharmaceutical composition of claim 5 , further comprising at least one chemotherapeutic agent.21. (canceled)22. (canceled)23. The pharmaceutical composition of claim 20 , wherein said at least one chemotherapeutic agent is selected from the group consisting of paclitaxel (Taxol®) claim 20 , cisplatin claim 20 , docetaxol claim 20 , carboplatin claim 20 , vincristine claim 20 , vinblastine claim 20 , methotrexate claim 20 , cyclophosphamide claim 20 , CPT-11 claim 20 , 5-fluorouracil (5-FU) claim 20 , gemcitabine claim 20 , estramustine claim 20 , carmustine claim 20 , adriamycin (doxorubicin) claim 20 , etoposide claim 20 , arsenic trioxide claim 20 , irinotecan claim 20 , and epothilone derivatives.2434.-. (canceled)35. A compound which is the hydroquinone form of the compound of .36. (canceled)37. The compound of claim 2 , wherein X claim 2 , X claim 2 , X claim 2 , X claim 2 , X claim 2 , X claim 2 , and Xare H.38. The compound of claim 2 , wherein Xis R.39. The compound of claim 38 , wherein R is aryl.40. The compound of claim 37 , wherein Xis R.41. The compound of claim 39 , wherein R is aryl. This application claims priority under 35 U.S.C. §119(e) to U.S. Provisional Patent Application No. 60/918,516, filed on Mar. 16, 2007. The foregoing application is incorporated by reference herein.Pursuant to 35 U.S.C. Section 202(c), it is acknowledged that the United ...

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18-07-2013 дата публикации

Naphthalene Derivative

Номер: US20130184241A1
Принадлежит: KYOTO UNIVERSITY

The present invention provides compounds which can regulate VCP activity. The present invention provides the compound of formula (I) 2. The compound according to or oxides , esters , prodrugs , pharmaceutically acceptable salts or solvates thereof , wherein R is selected from phenyl , pyridyl , quinolinyl and thiophenyl , and may be unsubstituted or independently of one another substituted with one or more Ra , in which Ra is as defined in .3. The compound according to or oxides , esters , prodrugs , pharmaceutically acceptable salts or solvates thereof , wherein Ra is absent or independently of one another selected from the group consisting of halo , alkyl , substituted alkyl , alkenyl , substituted alkenyl , aryl , substituted aryl , heteroaryl , substituted heteroaryl , heterocyclyl , substituted heterocyclyl , cyano , nitro , acyl , acylamino , alkoxy , substituted alkoxy , carboxyl , carboxyl ester , alkylthio , substituted alkylthio and aminocarbonyl , in which the substituted alkyl , the substituted alkenyl , the substituted aryl , the substituted heteroaryl , the substituted heterocyclyl , the substituted alkoxy or the substituted alkylthio independently of one another refer to the respective groups substituted with one or more substituent Rb or Rc , the substituent Rb and Rc being as defined in .6. The compound according to or oxides , esters , prodrugs , pharmaceutically acceptable salts or solvates thereof , wherein Ra is selected from the group consisting of alkenyl , substituted alkenyl , aryl , substituted aryl , heteroaryl , substituted heteroaryl , cyano , carboxyl ester , alkylthio , substituted alkylthio and aminocarbonyl , in which substituted alkenyl , substituted aryl , substituted heteroaryl , substituted alkylthio independently of one another refer to the respective groups substituted with one or more substituent Rb or Rc , the substituent Rb and Rc being as defined in .7. A pharmaceutical composition comprising the compound according to or ...

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25-07-2013 дата публикации

Bisaryl-bonded aryltriazolones and use thereof

Номер: US20130190330A1
Принадлежит: Bayer Intellectual Property GmbH

The present application relates to novel bisaryl-linked 5-aryl-1,2,4-triazolone derivatives, to processes for preparing them, to their use alone or in combinations for the treatment and/or prevention of diseases and also to their use for the production of medicaments for the treatment and/or prevention of diseases, more particularly for the treatment and/or prevention of cardiovascular disorders.

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25-07-2013 дата публикации

BENZYL SULFONAMIDE DERIVATIVES AS RORC MODULATORS

Номер: US20130190356A1
Принадлежит: Genentech, Inc.

Compounds of the formula I: 2. The compound of claim 1 , wherein C is a group of formula (i).3. The compound of claim 2 , wherein A is a group of formula (a).4. The compound of claim 3 , wherein B is a group of formula (e).5. The compound of claim 3 , wherein B is a group of formula (f).6. The compound of claim 3 , wherein m is 0.7. The compound of claim 3 , wherein m is 1.8. The compound of claim 3 , wherein Rand Rare hydrogen.9. The compound of claim 3 , wherein Rand Rare hydrogen.10. The compound of claim 3 , wherein Ris: Calkyl; Ccycloalkyl; or Ccycloalkyl-Calkyl; each of which may be optionally substituted one or more times with halo.11. The compound of claim 3 , wherein Ris Calkyl.12. The compound of claim 3 , wherein Ris isobutyl.14. The compound of claim 13 , wherein Ris: —SO—R; —(CH)—C(O)—NRR; —(CH)—SO—NRR; —(CH)—NR—C(O)—R; or —(CH)—NR—SO—R.18. A composition comprising:(a) a pharmaceutically acceptable carrier; and{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, '(b) a compound of .'}19. A method for treating arthritis claim 1 , said method comprising administering to a subject in need thereof an effective amount of a compound of . This application claims the benefit under 35 USC §119 of U.S. Provisional Application Ser. No. 61/579,255 filed on Dec. 22, 2011, the disclosure of which is incorporated herein by reference.The invention pertains to compounds that modulate the function of retinoid-receptor related orphan receptor RORc (RORγ) and use of such compounds for treatment of autoimmune diseases.T helper 17 cells (Th17) are interleukin (IL)-17 secreting CD4+ T cells involved in pathogenesis of autoimmune diseases such as rheumatoid arthritis, irritable bowel disease, psoriasis, psoriatic arthritis and spondyloarthridities. The retinoic acid-related orphan receptor γ (RORγ or RORc) is recognized as a transcription factor necessary for Th17 cell differentiation. RORc is an orphan member of the nuclear hormone receptor subfamily that includes RORα (RORa) ...

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01-08-2013 дата публикации

CYCLOPROPYLAMINE DERIVATIVES USEFUL AS LSD1 INHIBITORS

Номер: US20130197013A1
Принадлежит:

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

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08-08-2013 дата публикации

Formulations for organic electroluminescent devices

Номер: US20130200357A1
Принадлежит: Merck Patent GmBH

The present invention relates to a formulation, in particular for use in organic electroluminescent devices, comprising a carbazole compound, an electron-transport compound, a triplet emitter compound and at least one solvent, where the electron-transport compound encompasses a ketone compound or a triazine compound and where the carbazole compound contains at least two carbazole groups whose N atoms are connected to one another via an aromatic or heteroaromatic ring system. The invention is furthermore directed to organic electro-luminescent devices which comprise the mixtures according to the invention.

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08-08-2013 дата публикации

COMPOUNDS THAT MODULATE INTRACELLULAR CALCIUM

Номер: US20130203818A1
Принадлежит: CalciMedica, Inc.

Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity. 111.-. (canceled)1346.-. (canceled)4855.-. (canceled)56. The compound of wherein Lis —NH—C(═O).57. The compound of wherein Ris aryl.58. The compound of wherein aryl is phenyl.59. The compound of wherein the phenyl group is substituted with at least one Rselected from F claim 58 , Cl claim 58 , Br claim 58 , I claim 58 , —CN claim 58 , —OH claim 58 , —CF claim 58 , —OCF claim 58 , —OR claim 58 , —N(R) claim 58 , and C-Calkyl.60. The compound of wherein Ris selected from —CF claim 59 , —OCF claim 59 , —OR claim 59 , C-Calkyl claim 59 , and C-Ccycloalkyl.61. The compound of wherein Ris C-Calkyl.62. The compound of wherein Ris —CFand Ris —CH.63. The compound of wherein n is 1.64. The compound of wherein Ris fluorine.65. The compound of wherein phenyl is substituted with at least 2 substituents.66. The compound of wherein phenyl is substituted with at least 3 substituents.67. The compound of wherein Ris heteroaryl.68. The compound of wherein heteroaryl is selected from thienyl claim 67 , thianthrenyl claim 67 , furyl claim 67 , pyranyl claim 67 , thiadiazolyl claim 67 , benzothiadiazolyl claim 67 , isobenzofuranyl claim 67 , chromenyl claim 67 , xanthenyl claim 67 , phenoxathiinyl claim 67 , pyrrolyl claim 67 , imidazolyl claim 67 , pyrazolyl claim 67 , isothiazolyl claim 67 , isoxazolyl claim 67 , pyridyl claim 67 , pyrazinyl claim 67 , pyrimidinyl claim 67 , pyridazinyl claim 67 , pyrazolo-pyrimidinyl claim 67 , triazolo-pyrimidinyl claim 67 , imidazo-pyrimidinyl claim 67 , indolizinyl claim 67 , isoindolyl claim 67 , 3H-indolyl claim 67 , indolyl claim 67 , indazolyl claim 67 , purinyl claim 67 , 4H- ...

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15-08-2013 дата публикации

Method for preparing polypropylene using transition metal compound containing thiophene-fused cyclopentadienyl ligand

Номер: US20130211021A1
Принадлежит: Lotte Chemical Corp

The present invention relates to a preparation method for polypropylene that comprises polymerizing a propylene monomer in the presence of a catalyst comprising a novel transition metal compound. Using the novel transition metal compound as a catalyst, the preparation method for polypropylene according to the present invention can not only acquire high catalytic activity for polymerization to achieve high efficiency of the process but allow it to easily control the fine-structure characteristics of the polymer, thereby providing polypropylene having desired properties with ease.

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22-08-2013 дата публикации

AZETIDINYL DIAMIDES AS MONOACYLGLYCEROL LIPASE INHIBITORS

Номер: US20130217669A1
Принадлежит: Janssen Pharmaceutica, NV

Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: 118-. (canceled)20. A pharmaceutical composition comprising a compound of and at least one of a pharmaceutically acceptable carrier claim 19 , a pharmaceutically acceptable excipient claim 19 , and a pharmaceutically acceptable diluent.21. A pharmaceutical composition of claim 20 , wherein the composition is a solid oral dosage form.22. A pharmaceutical composition of claim 20 , wherein the composition is a syrup claim 20 , an elixir claim 20 , or a suspension. This application claims priority to U.S. provisional patent application Nos. 61/171,658 and 61/171,649, each filed Apr. 22, 2009, which are hereby incorporated by reference in their entirety.The research and development of the invention described below was not federally sponsored.has been used for the treatment of pain for many years. Δ-tetrahydrocannabinol is a major active ingredient from and an agonist of cannabinoid receptors (Pertwee, 2008, 153, 199-215). Two cannabinoid G protein-coupled receptors have been cloned, cannabinoid receptor type 1 (CBMatsuda et al., 1990, 346, 561-4) and cannabinoid receptor type 2 (CBMunro et al., 1993, 365, 61-5). CBis expressed centrally in brain areas, such as the hypothalamus and nucleus accumbens as well as peripherally in the liver, gastrointestinal tract, pancreas, adipose tissue, and skeletal muscle (Di Marzo et al., 2007, 18, 129-140). CBis predominantly expressed in immune cells, such as monocytes (Pacher et al., 2008, 294, H1133-H1134), and under certain conditions, also in the brain (Benito et al., 2008, 153, 277-285) and in skeletal (Cavuoto et al., 2007, 364, 105-110) and cardiac (Hajrasouliha et al., 2008, 579, 246-252) muscle. An abundance of pharmacological, anatomical and electrophysiological data, using synthetic agonists, indicate that increased cannabinoid ...

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22-08-2013 дата публикации

QUINOLINE DERIVATIVES AND MELK INHIBITORS CONTAINING THE SAME

Номер: US20130217671A1
Принадлежит:

The present invention directs a compound represented by formula (I). 2. The compound or a pharmaceutically acceptable salt thereof of claim 1 , wherein Ris a hydrogen atom or a halogen and Ris a hydrogen atom.3. The compound or a pharmaceutically acceptable salt thereof of claim 2 , wherein Ris R[Rrepresents a cyano claim 2 , a C-Calkylsulfinyl claim 2 , a C-Calkylsulfonyl claim 2 , or —CO—R(wherein claim 2 , Rrepresents a C-Calkyl claim 2 , or a C-Ccycloalkyl)] claim 2 ,{'sup': 2', '2A', '2A', '6A', '7A', '6A', '7A', '10A', '10A', '6A', '7A, 'sub': 2', 'n', '3', '10', '1', '6, 'Ris R{Rrepresents an optionally substituted aryl which may have a substituent group selected from Substituent Group C, an optionally substituted aromatic heterocyclic group which may have a substituent group selected from Substituent Group H, or —NRR[wherein, Rrepresents a hydrogen atom, and Rrepresents —(CH)—R(wherein, n represents an integer of 0 to 6, and Rrepresents an optionally substituted C-Ccycloalkyl which may have a substituent group selected from Substituent Group D, an optionally substituted aryl which may have a substituent group selected from Substituent Group E, an aliphatic heterocyclic group which may be substituted with a C-Calkyl, an aromatic heterocyclic group which may have a substituent group selected from Substituent Group I), or Rand Rform with an adjacent nitrogen atom an optionally substituted heterocyclic group which may have a substituent group selected from Substituent Group F]},'}{'sup': 3', '3A', '3A, 'Ris R(Rrepresents an optionally substituted aryl which may have a substituent group selected from Substituent Group G, or an optionally substituted aromatic heterocyclic group which may have a substituent group selected from Substituent Group H), and'}{'sup': '4', 'Ris a hydrogen atom or a halogen, and'} [{'sub': 1', '6', '1', '6, 'Substituent Group C: a halogen, a hydroxy, a C-Calkoxy, and a di(C-Calkyl) amino;'}, {'sub': 1', '6', '1', '6', '1', '6', '1', '6', ' ...

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22-08-2013 дата публикации

PHARMACEUTICAL AGENT COMPRISING QUINOLONE COMPOUND

Номер: US20130217678A1
Принадлежит: OTSUKA PHARMACEUTICAL CO., LTD.

The present invention provides a pharmaceutical agent that inhibits the chronic progression of Parkinson's disease or protects dopamine neurons from disease etiology, thereby suppressing the progression of neurological dysfunction, so as to prolong the period of time until L-dopa is administered while also improving neuronal function; the pharmaceutical agent of the invention comprising as an active ingredient a quinolone compound represented by Formula (1): 2. The method according to claim 1 , wherein the neurodegenerative disease is selected from the group consisting of Parkinson's disease claim 1 , Parkinson's syndrome claim 1 , juvenile parkinsonism claim 1 , striatonigral degeneration claim 1 , progressive supranuclear palsy claim 1 , pure akinesia claim 1 , Alzheimer's disease claim 1 , Pick's disease claim 1 , prion disease claim 1 , corticobasal degeneration claim 1 , diffuse Lewy body disease claim 1 , Huntington's disease claim 1 , chorea-acanthocytosis claim 1 , benign hereditary chorea claim 1 , paroxysmal choreoathetosis claim 1 , essential tremor claim 1 , essential myoclonus claim 1 , Gilles de la Tourette's syndrome claim 1 , Rett's syndrome claim 1 , degenerative ballism claim 1 , dystonia musculorum deformans claim 1 , athetosis claim 1 , spasmodic torticollis claim 1 , Meige syndrome claim 1 , cerebral palsy claim 1 , Wilson's disease claim 1 , Segawa's disease claim 1 , Hallervorden-Spatz syndrome claim 1 , neuroaxonal dystrophy claim 1 , pallidal atrophy claim 1 , spinocerebellar degeneration claim 1 , cerebral cortical atrophy claim 1 , Holmes-type cerebellar atrophy claim 1 , olivopontocerebellar atrophy claim 1 , hereditary olivopontocerebellar atrophy claim 1 , Joseph disease claim 1 , dentatorubropallidoluysian atrophy claim 1 , Gerstmann-Straussler-Scheinker disease claim 1 , Friedreich's ataxia claim 1 , Roussy-Levy syndrome claim 1 , May-White syndrome claim 1 , congenital cerebellar ataxia claim 1 , hereditary episodic ataxia claim 1 , ...

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22-08-2013 дата публикации

HETEROARYLS AND USES THEREOF

Номер: US20130217689A1
Принадлежит: Millennium Pharmaceuticals, Inc.

This invention provides compounds of formula I: 2. The compound of claim 1 , wherein one or more substituents are selected from:{'sub': '1', '(a) Yis S;'}{'sub': '2', '(b) Yis C'}{'sup': '1', '(c) Ris CN or H;'}{'sup': '2', '(d) Ris an optionally substituted 6-10-membered aryl, or 5-10-membered heteroaryl having 1-5 heteroatoms independently selected from nitrogen, oxygen, or sulfur;'}(e) n is 0-2; or{'sup': 4', '4a, '(f) Ris —R.'}4. The compound of claim 1 , wherein Ris a 3-10-membered cycloaliphatic claim 1 , 4-10-membered heterocyclyl having 1-5 heteroatoms independently selected from nitrogen claim 1 , oxygen claim 1 , or sulfur 6-10-membered aryl claim 1 , or 5-10-membered heteroaryl having 1-5 heteroatoms independently selected from nitrogen claim 1 , oxygen claim 1 , or sulfur claim 1 , optionally substituted with 1-4 independent occurrences of R claim 1 , wherein Ris —R claim 1 , -T-R claim 1 , or —V-T-R claim 1 , and:{'sup': 9a', '9c', '9b', '9b', '9c', '9c', '9b', '9b', '9b', '9b', '9b', '9e', '9b', '9e', '9c', '9e', '9b', '9e', '9b', '9e', '9b', '9b, 'sub': 2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2, 'each occurrence of Ris independently halogen, —CN, —NO, —R, —N(R), —OR, —SR, —S(O)R, —C(O)R, —C(O)OR, —C(O)N(R), —S(O)N(R), —OC(O)N(R), —N(R)C(O)R, —N(R)SOR, —N(R)C(O)OR, —N(R)C(O)N(R), or —N(R)SON(R), or two occurrences of R, taken together with a nitrogen atom to which they are bound, form an optionally substituted 4-7-membered heterocyclyl ring having 0-1 additional heteroatoms selected from nitrogen, oxygen, or sulfur;'}{'sup': '9b', 'sub': 1', '6, 'each occurrence of Ris independently hydrogen or an optionally substituted group selected from C-Caliphatic, 3-10-membered cycloaliphatic, 4-10-membered heterocyclyl having 1-5 heteroatoms independently selected from nitrogen, oxygen, or sulfur, 6-10-membered aryl, or 5-10-membered heteroaryl having 1-5 heteroatoms independently selected from nitrogen, oxygen, or sulfur;'}{'sup': '9c', 'sub': 1', '6, ...

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22-08-2013 дата публикации

CYCLIC AMIDE DERIVATIVE

Номер: US20130217692A1
Принадлежит: DAINIPPON SUMITOMO PHARMA CO., LTD.

Provided is a compound represented by formula (1) or a pharmacologically acceptable salt thereof. (In the formula, A is Carylene, etc.; R, Rand Reach independently is a hydrogen atom, a halogen atom, a Calkyl group, a Calkoxy group, etc.; Ris an optionally substituted Caryl group, an optionally substituted 5- to 12-membered monocyclic or polycyclic heteroaryl group, an optionally substituted Caralkyl group, etc.; m is 0, etc.; n is an integer of 0 to 2.) 2. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein A is 1 claim 1 ,3-phenylene claim 1 , or 1 claim 1 ,4-phenylene.3. The compound of claim 2 , or a pharmaceutically acceptable salt thereof claim 2 , wherein A is 1 claim 2 ,4-phenylene.6. The compound of claim 5 , or a pharmaceutically acceptable salt thereof claim 5 , wherein Ris(1) halogen atom,(2) cyano group,{'sub': '1-4', 'claim-text': (a) 1 to 3 halogen atom(s), or', {'sub': '1-4', '(b) Calkoxy (in which the group may be optionally substituted by 1 to 3 halogen atom(s))),'}], '(3) Calkyl group (in which the group may be optionally substituted by'}{'sub': '1-4', 'claim-text': (a) 1 to 3 halogen atom(s), or', {'sub': '1-4', '(b) Calkoxy (in which the group may be optionally substituted by 1 to 3 halogen atom(s))),'}], '(4) Calkoxy group (in which the group may be optionally substituted by'}{'sub': '3-6', '(5) Ccycloalkyl group,'}{'sub': '3-6', '(6) Ccycloalkoxy group,'}(7) heterocyclic oxy group, or{'sub': '7-16', '(8) Caralkyloxy group.'}7. The compound of claim 6 , or a pharmaceutically acceptable salt thereof claim 6 , wherein Ris Calkyl group which may be optionally substituted by Calkoxy.8. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris(1) hydrogen atom,{'sub': '1-4', '(2) Calkyl group,'}{'sub': '1-4', '(3) Calkoxy group, or'}{'sub': '3-6', '(4) Ccycloalkyl group.'}9. The compound of claim 8 , or a pharmaceutically acceptable salt thereof claim 8 , wherein Ris hydrogen ...

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22-08-2013 дата публикации

Sulphonamine Compounds and Methods of Making and Using Same

Номер: US20130217759A1
Принадлежит: Zafgen Inc.

The invention provides sulphonamide compounds and their use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of making various sulphone compounds are provided. The compounds are contemplated to have activity against methionyl aminopeptidase 2. 2. The compound of claim 1 , wherein A is phenyl.3. The compound of claim 1 , wherein A is pyridinyl.4. The compound of claim 1 , wherein X is S or NR.5. The compound of claim 1 , wherein X is S.6. The compound of wherein Ris H.7. The compound of claim 1 , wherein Ris selected from the group consisting of H claim 1 , Calkoxy claim 1 , Calkyl claim 1 , Calkenyl claim 1 , Calkynyl claim 1 , Ccycloalkyl claim 1 , Calkoxy claim 1 , CcycloalkylCalkyl- claim 1 , Calkyl-S(O)— wherein w is 0 claim 1 , 1 or 2 claim 1 , Calkyl-N(R)-carbonyl claim 1 , Calkyl-carbonyl-N(R)— claim 1 , Calkyl-N(R)-carbonyl-N(R)— claim 1 , and Calkyl-N(R)— claim 1 , wherein Calkyl claim 1 , Calkoxy claim 1 , Calkenyl claim 1 , Ccycloalkyl and Calkynyl may be optionally substituted by RRN—.8. The compound of claim 1 , wherein Ris selected from the group consisting of Calkyl claim 1 , phenyl or heteroaryl.9. The compound of claim 1 , wherein Ris selected from the group consisting of H claim 1 , Calkyl claim 1 , or Calkoxy claim 1 , wherein Calkyl or Calkoxy is optionally substituted by one or more substituents selected from halogen and RRN—.11. The compounds 2-benzenesulphonylamino-4 claim 1 ,5 claim 1 ,6 claim 1 ,7-tetrahydrobenzo[b]thiophene-3-carboxylic acid claim 1 , 2-(4-fluorobenzenesulphonylamino)-4 claim 1 ,5 claim 1 ,6 claim 1 ,7-tetrahydrobenzo[b]thiophene-3-carboxylic acid claim 1 , 2-benzenesulphonylaminobenzo[b]thiophene-3-carboxylic acid claim 1 , 2-benzenesulphonylamino-5-ethyl-4-methylthiophene-3-carboxylic acid claim 1 , 2-benzenesulphonylamino-4 claim 1 ,7-dihydro-5H-thieno[2 claim 1 ,3-c]pyran-3-carboxylic acid claim 1 , 2-benzenesulphonylamino-5-phenylthiophene-3-carboxylic acid claim 1 , 2- ...

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29-08-2013 дата публикации

NOVEL HETEROCYCLIC DERIVATIVE AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME (AS AMENDED)

Номер: US20130225596A1
Принадлежит:

The present invention provides novel compounds having a P2Xand/or P2Xreceptor antagonistic effect. 2. The pharmaceutical composition having a P2Xand/or P2Xreceptor antagonistic effect according to claim 1 , comprising the compound wherein ring A is a substituted or unsubstituted cyclohexane ring claim 1 , a substituted or unsubstituted cyclohexadiene ring claim 1 , a substituted or unsubstituted cyclohexene ring claim 1 , a substituted or unsubstituted benzene ring claim 1 , a substituted or unsubstituted pyridine ring claim 1 , a substituted or unsubstituted dihydropyridine ring claim 1 , a substituted or unsubstituted tetrahydropyridine ring claim 1 , a substituted or unsubstituted pyrimidine ring claim 1 , a substituted or unsubstituted dihydropyrimidine ring claim 1 , a substituted or unsubstituted tetrahydropyrimidine ring claim 1 , a substituted or unsubstituted hexahydropyrimidine ring claim 1 , a substituted or unsubstituted piperidine ring claim 1 , a substituted or unsubstituted piperazine ring claim 1 , a substituted or unsubstituted pyrazine ring claim 1 , a substituted or unsubstituted dihydropyrazine ring claim 1 , a substituted or unsubstituted tetrahydropyrazine ring claim 1 , a substituted or unsubstituted pyridazine ring claim 1 , a substituted or unsubstituted dihydropyridazine ring claim 1 , a substituted or unsubstituted tetrahydropyridazine ring claim 1 , a substituted or unsubstituted indene ring claim 1 , a substituted or unsubstituted benzofuran ring claim 1 , a substituted or unsubstituted benzofuran ring claim 1 , a substituted or unsubstituted benzo(b)thiophene ring claim 1 , a substituted or unsubstituted benzo(c)thiophene ring claim 1 , a substituted or unsubstituted indoline ring claim 1 , a substituted or unsubstituted indole ring claim 1 , a substituted or unsubstituted benzimidazole ring claim 1 , a substituted or unsubstituted cyclopenta[b]pyridine ring claim 1 , a substituted or unsubstituted 1H-indazole ring claim 1 , a ...

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29-08-2013 дата публикации

INDOLES AND THEIR THERAPEUTIC USE

Номер: US20130225617A1
Принадлежит: PULMAGEN THERAPEUTICS (ASTHMA) LIMITED

Compounds of the invention are ligands of the CRTH2 receptor, useful inter alia for treatment of inflammatory conditions. 2. The compound as claimed in wherein Ris hydrogen and Ris fluoro or chloro.3. The compound as claimed in wherein X is *—SONR— wherein the bond marked with an asterisk is attached to Ar.4. The compound as claimed in wherein the radical ArSO— or ArN(R)SO— is in the meta- or para-position of the ring Arrelative to the point of attachment of Arto the rest of the molecule.5. The compound as claimed in wherein the radical ArSO— or ArN(R)SO— is in the ortho-position of the ring Arrelative to the point of attachment of Arto the rest of the molecule.6. The compound as claimed in wherein Aris phenyl and Aris selected from pyrrolyl claim 1 , furanyl claim 1 , thienyl claim 1 , oxazolyl claim 1 , thiazolyl claim 1 , imidazolyl claim 1 , pyrazolyl claim 1 , isoxazolyl claim 1 , isothiazolyl claim 1 , pyridinyl claim 1 , pyridazinyl claim 1 , pyrimidinyl and pyrazinyl.7. The compound as claimed in wherein Aris selected from furanyl claim 1 , thienyl claim 1 , oxazolyl claim 1 , thiazolyl claim 1 , imidazolyl claim 1 , pyrazolyl claim 1 , isoxazolyl claim 1 , isothiazolyl claim 1 , pyridinyl claim 1 , pyridazinyl claim 1 , pyrimidinyl claim 1 , and pyrazinyl claim 1 , and Aris phenyl.8. The compound as claimed in wherein when ring Aris heteroaryl it is selected from thienyl claim 1 , pyridinyl claim 1 , pyrimidinyl claim 1 , thiazolyl claim 1 , isothiazolyl and imidazolyl.9. The compound as claimed in wherein when ring Aris heteroaryl it is selected from thienyl claim 1 , pyridinyl claim 1 , and pyrimidinyl.10. The compound as claimed in wherein optional substituents in Arand Arare selected from chloro claim 1 , fluoro claim 1 , —CN and methyl.11. The compound as claimed in which is the subject of any of the Examples herein claim 1 , or which is a pharmaceutically acceptable salt of the subject of any of the Examples herein.12. A pharmaceutical composition ...

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29-08-2013 дата публикации

SUBSTITUTED N-PHENETHYLTRIAZOLONEACETAMIDES AND USE THEREOF

Номер: US20130225646A1
Принадлежит: Bayer Intellectual Property GmbH

The present application relates to novel substituted N-phenethyltriazoloneacetamides, to processes for preparing them, to their use alone or in combinations for the treatment and/or prevention of diseases and also to their use for the production of medicaments for the treatment and/or prevention of diseases, more particularly for the treatment and/or prevention of cardiovascular disorders. 5. (canceled)6. A method of treatment and/or prevention of acute and chronic heart failure claim 1 , hypervolaemic and euvolaemic hyponatraemia claim 1 , cirrhosis of the liver claim 1 , ascites claim 1 , oedema and the syndrome of inadequate ADH secretion (SIADH) comprising administering a compound of to a patient in need thereof.7. (canceled)8. A pharmaceutical composition comprising a compound of and one or more inert non-toxic pharmaceutically suitable auxiliaries.9. The pharmaceutical composition comprising a compound of and at least one active substance selected from the group consisting of a diuretic claim 1 , an angiotensin AII antagonist claim 1 , an ACE inhibitor claim 1 , a beta-receptor blocker claim 1 , a mineralocorticoid receptor antagonist claim 1 , an organic nitrate claim 1 , an NO donor and a positive-inotropic active substance.10. A method of treatment and/or prevention of acute and chronic heart failure claim 8 , hypervolaemic and euvolaemic hyponatraemia claim 8 , cirrhosis of the liver claim 8 , ascites claim 8 , oedema and the syndrome of inadequate ADH secretion (SIADH) comprising administering the pharmaceutical composition of to a patient in need thereof. The present application relates to novel substituted N-phenethyltriazoloneacetamides, to processes for preparing them, to their use alone or in combinations for the treatment and/or prevention of diseases and also to their use for the production of medicaments for the treatment and/or prevention of diseases, more particularly for the treatment and/or prevention of cardiovascular disorders.The liquid ...

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