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Небесная энциклопедия

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

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Мониторинг СМИ

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

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Поддерживает ввод нескольких поисковых фраз (по одной на строку). При поиске обеспечивает поддержку морфологии русского и английского языка
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Применить Всего найдено 37303. Отображено 100.
05-01-2012 дата публикации

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

Номер: US20120004206A1

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

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12-01-2012 дата публикации

Modulation of anxiety through blockade of anandamide hydrolysis

Номер: US20120010283A1

Fatty acid amide hydrolase inhibitors of the Formula: are provided wherein X is NH, CH 2 , O, or S; Q is O or S; Z is O or N; R is an aromatic moiety selected from the group consisting of substituted or unsubstituted aryl; substituted or unsubstituted biphenylyl, substituted or unsubstituted naphthyl, and substituted or unsubstituted phenyl; substituted or unsubstituted terphenylyl; substituted or unsubstituted cycloalkyl, heteroaryl, or alkyl; and R 1 and R 2 are independently selected from the group consisting of H, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, and substituted or unsubstituted phenyl, substituted or unsubstituted biphenylyl, substituted or unsubstituted aryl, and substituted or unsubstituted heteroaryl; with the proviso that if Z is O, one of R 1 and R 2 is absent, and that if Z is N, optionally R 1 and R 2 may optionally be taken together to form a substituted or unsubstituted N-heterocycle or substituted or unsubstituted heteroaryl with the N atom to which they are each attached. Pharmaceutical compositions comprising the compounds of Formula I and methods of using them to inhibit FAAH and/or treat appetite disorders, glaucoma, pain, insomnia, and neurological and psychological disorders including anxiety disorders, epilepsy, and depression are provided.

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26-01-2012 дата публикации

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

Номер: US20120022076A1
Принадлежит: Individual

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

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02-02-2012 дата публикации

Nitroxide Free Radical Synergized Antineoplastic Agents

Номер: US20120029021A1
Автор: Errol V. Mathias, Yong Ba
Принадлежит: California State University

Nitroxide free radicals attached to antineoplastic agents can synergize their potencies to cancer cells. This invention relates to any antineoplastic agents and their derivatives chemically attached with nitroxide free radicals, such as TEMPO and its radical derivatives. This invention also relates to precursors of such compounds, as well as the products formed from the adducts after administration.

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16-02-2012 дата публикации

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

Номер: US20120040995A1
Принадлежит: University of Illinois

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

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16-02-2012 дата публикации

Dihydrolipoic Acid Derivatives Comprising Nitric Oxide and Therapeutic Uses Thereof

Номер: US20120041025A1
Автор: Sampath Parthasarathy
Принадлежит: Invasc Therapeutics Inc

Compounds are provided that comprise dinitroso-derivatives of dihydrolipoic acid. Pharmaceutical compositions comprising the compounds and methods of using the compounds for treating various diseases and disorders, including angina, hypertension, diabetes, dyslipidemia, renal insufficiency, myocardial infarction, stroke, atherosclerosis, and the target organ damage that accompanies these various diseases and disorders, are further provided. The compounds are useful in improving vasodilation, reducing low-density lipoprotein oxidation, and reducing inflammation in a subject.

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23-02-2012 дата публикации

Diacylethylenediamine compound

Номер: US20120046292A1
Принадлежит: Astellas Pharma Inc

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

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22-03-2012 дата публикации

Metallo-beta-lactamase inhibitors

Номер: US20120071457A1
Принадлежит: Individual

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

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29-03-2012 дата публикации

Methods for Identifying Autophagy Inducing Compounds

Номер: US20120077705A1
Автор: Junying Yuan
Принадлежит: Harvard College

This invention pertains to screening methods for identifying autophagy inducing compounds.

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29-03-2012 дата публикации

Bicyclic compounds and use as antidiabetics

Номер: US20120077812A1
Принадлежит: Individual

The present invention relates to novel compounds that are useful in the treatment of metabolic disorders, particularly type II diabetes mellitus and related disorders, and also to the methods for the making and use of such compounds.

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19-04-2012 дата публикации

5-ht receptor modulating compounds

Номер: US20120094989A1
Принадлежит: SERODUS AS

The present invention relates to compounds having 5-hydroxytryptamine receptor modulating activity, in particular compounds having an acidic moiety held distant from the 5-HT pharmacophore by a rigid linker group, to compositions containing such compounds and methods of treatment using them. Such compounds have an increased affinity for the 5-HT receptor and a reduced hERG effect. Certain compounds of the invention further exhibit an angiotensin II receptor modulating activity. Claimed are compounds of formula (I): HT-L-A. HT is a 5-HT receptor modulating moiety containing a basic nitrogen atom; A is an acid moiety; L is a linker moiety.

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19-04-2012 дата публикации

Triglyceride-lowering agent and hyperinsulinism-ameliorating agent

Номер: US20120095043A1
Автор: Taro Aoki, Toru Yokoyama
Принадлежит: Kowa Co Ltd, Nissan Chemical Corp

The present invention is directed to a triglyceride-lowering agent, exhibiting excellent triglyceride-lowering effect and a hyperinsulinemia-ameliorating agent. The triglyceride-lowering agent and hyperinsulinemia-ameliorating agent are characterized by containing a pitavastatin compound, and amlodipine or a salt thereof.

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10-05-2012 дата публикации

Compound inhibiting in vivo phosphorus transport and medicine containing the same

Номер: US20120115851A1
Принадлежит: Kyowa Hakko Kirin Co Ltd

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

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17-05-2012 дата публикации

Phenoxy substituted phenylamidine derivatives and their use as fungicides

Номер: US20120122678A1
Принадлежит: Bayer CropScience AG

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

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17-05-2012 дата публикации

Libraries of n-substituted-n-phenylethylsulfonamides for drug discovery

Номер: US20120122920A1

New compounds are continually being sought for the treatment and prevention of disorders. The invention relates to N-substituted-N-phenylethylsulfonamides libraries which can be used in the search for, and identification of, new lead compounds that could modulate the functional activity of a biological target.

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24-05-2012 дата публикации

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

Номер: US20120129837A1
Принадлежит: Clinical Data Inc

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

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07-06-2012 дата публикации

Compounds as bradykinin b1 antagonists

Номер: US20120142695A1
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

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

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05-07-2012 дата публикации

Zinc cluster

Номер: US20120172601A1
Принадлежит: Takasago International Corp

Disclosed is a novel zinc cluster compound represented by general formula (1): Zn 4 O (OCOR) 6 (RCOOH) n , wherein R represents an alkyl group which has 1 to 4 carbon atoms and may be substituted with a halogen atom, and n represents 0.1 to 1, and also disclosed are a method for producing the compound and a reaction using the compound.

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26-07-2012 дата публикации

Ionic liquids

Номер: US20120190844A1
Принадлежит: Invista North America LLC

The invention relates to an ionic liquid composition and a method for preparing the ionic liquid. The ionic liquid comprises a cation containing the Formula I, as herein disclosed, and wherein: n is 2, R 1 is selected from the group consisting of: H, C 1 -C 12 alkyl, aryl or together with R 2 may form a heterocyclic ring, and R 2 is selected from the group consisting of: H, C 1 -C 12 alkyl, aryl or together with R 1 may form a heterocyclic ring, and R 3 is selected from the group consisting of hydrogen and C 1 -C 12 alkyl, and wherein R 1 and R 2 are not simultaneously selected from hydrogen.

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09-08-2012 дата публикации

Substituted 4-aminocyclohexane derivatives

Номер: US20120202810A1
Принадлежит: GRUENENTHAL GmbH

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

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23-08-2012 дата публикации

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

New compounds, pharmaceutical compositions and uses thereof

Номер: US20120214785A1
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

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

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30-08-2012 дата публикации

Selective calcium channel modulators

Номер: US20120220564A1
Принадлежит: Zalicus Pharmaceuticals Ltd

Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted T-type calcium channel activity are disclosed using a series of compounds containing N-acylated cyclic amines linked to an aπl ring as shown in formula (I).

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30-08-2012 дата публикации

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

Номер: US20120220592A1
Принадлежит: Newron Pharmaceuticals SpA

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

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06-09-2012 дата публикации

Compositions and methods useful for treating diseases

Номер: US20120225851A1
Принадлежит: Eutropics Pharmaceuticals Inc

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

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06-09-2012 дата публикации

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

Номер: US20120225890A1
Принадлежит: ProteoTech Inc

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

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13-09-2012 дата публикации

Methods of treating emesis using growth hormone secretagogues

Номер: US20120232113A1
Принадлежит: Helsinn Therapeutics Us Inc

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

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04-10-2012 дата публикации

Pyridinecarboxamides, useful-plant-protecting composition comprising them and processes for their preparation and their use

Номер: US20120252670A1
Принадлежит: Individual

Compounds of the formula (I), or salts thereof, in which R 1 to R 4 are as defined in formula (I) of claim 1 are suitable as useful-plant-protecting agents for reducing or preventing harmful effects of agrochemicals on the useful plants and their method of preparation are described.

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11-10-2012 дата публикации

Pyrrolo[2,3-d]pyrimidine derivatives: their intermediates and synthesis

Номер: US20120259115A1
Принадлежит: PFIZER INC

This invention relates to methods and intermediates useful for the synthesis of pyrrolo [2,3-d] pyrimidine compounds. Specifically novel synthetic methods and intermediates for the synthesis of 3-{(3R,4R)-4-methyl-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-amino}-piperidin-1-yl)-3-oxo-propionitrile and its corresponding citrate salt are disclosed.

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01-11-2012 дата публикации

Novel heterocyclic acrylamides and their use as pharmaceuticals

Номер: US20120277207A1
Принадлежит: FAB PHARMA Sas

The invention relates to novel heterocyclic acrylamide compounds (I), to the preparation of the compounds and intermediates used therein, to the use of the compounds as antibacterial medicaments and pharmaceutical compositions containing the compounds.

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08-11-2012 дата публикации

Inhibitors of Atypical Protein Kinase C and Their Use in Treating Hedgehog Pathway-Dependent Cancers

Номер: US20120283194A1
Принадлежит: Leland Stanford Junior University

Methods and compositions are provided for modulating Hedgehog (Hh) pathway signaling in a cell. Aspects of the methods include methods for inhibiting Hh pathway-promoted cancer proliferation and/or metastasis that is promoted by Hh pathway signaling, methods for treating cancers promoted by Hh pathway signaling, and methods for screening candidate agents for the ability to treat a cancer promoted by Hh pathway signaling. In addition, reagents and kits thereof that find use in practicing the subject methods are provided.

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08-11-2012 дата публикации

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

Номер: US20120283445A1
Принадлежит: SANOFI SA

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

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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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29-11-2012 дата публикации

Process of making alpha-aminooxyketone/alpha-aminooxyaldehyde and alpha-hydroxyketone/alpha-hydroxyaldehyde compounds and a process making reaction products from cyclic alpha, beta-unsaturated ketone substrates and nitroso substrates

Номер: US20120302792A1
Принадлежит: JAPAN SCIENCE AND TECHNOLOGY AGENCY

The present invention is directed to a process of making α-aminooxyketone and α-hydroxyketone compounds. The synthetic pathway generally involves reacting an aldehyde or ketone substrate and a nitroso substrate in the presence of a catalyst of the formula (IV): wherein X a -X c represent independently nitrogen, carbon, oxygen or sulfur and Z represents a 4 to 10-membered ring with or without a substituent and optionally a further step to convert the α-aminooxyketone compound formed to the α-hydroxyketone compound. The present invention results in α-aminooxyketone and α-hydroxyketone compounds with high enantioselectivity and high purity. The present invention is also directed to a catalytic asymmetric O-nitroso Aldol/Michael reaction. The substrates of this reaction are generally cyclic α,β-unsaturated ketone substrate and a nitroso substrate. This methodology generally involves reacting the cyclic α,β-unsaturated ketone substrate and the nitroso substrate in the presence of a proline-based catalyst, to provide a heterocyclic product.

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06-12-2012 дата публикации

Preparation of 2-(4-bromophenyl)-2-methylpropanoic acid

Номер: US20120309973A1
Принадлежит: Divis Laboratories Ltd

Selective bromination of 2-methyl-2-phenylpropanoic acid in aqueous medium is described to obtain pure 2-(4-bromophenyl)-2-methylpropanoic acid, which is a useful key intermediate in the process of manufacturing pure fexofenadine.

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20-12-2012 дата публикации

Development of Novel Detergents for Use in PCR Systems

Номер: US20120322066A1
Принадлежит: Life Technologies Corp

This disclosure relates to novel detergents for use in various procedures including, for example, nucleic acid amplification reactions such as polymerase chain reaction (PCR). Methods for preparing the modified detergents are also described.

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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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10-01-2013 дата публикации

Substituted phenyl compounds

Номер: US20130012711A1
Принадлежит: SANOFI SA

The present invention relates to novel substituted phenyl compounds of the formula and to a process for making them. The compounds can be used as intermediates for making 6-substituted-1-(2H)-isoquinolinone derivatives.

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24-01-2013 дата публикации

Piperidinyl derivative as a modulator of chemokine receptor activity

Номер: US20130023564A1
Автор: Joseph B. Santella
Принадлежит: Bristol Myers Squibb Co

The present application describes the compound of formula (I): or stereoisomers or pharmaceutically acceptable salts thereof. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and arthrosclerosis using the compound of the invention are disclosed.

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14-02-2013 дата публикации

Chemoselective enrichment for compound isolation

Номер: US20130041106A1

Chemoselective isolation of hydroxyl group-containing and carboxyl group-containing compounds is accomplished via formation of polymeric silyl ethers and polymeric siloxyl esters, respectively. Preparation of chemoselective polymeric reagents for capture of hydroxyl group containing compounds and carboxyl group containing compounds is described.

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21-02-2013 дата публикации

4-fluoro-4-arylpiperdin-1-yl derivatives as mu opioid function moderators

Номер: US20130045165A1
Автор: David J. Fairfax
Принадлежит: KINENTIA BIOSCIENCES LLC

4-Fluoro-4-phenylpiperidin- 1 -yl μ antagonists of general structure as well as pharmaceutical compositions comprising compounds of formula I, are disclosed. These compounds and compositions are useful as treatments of conditions or diseases associated with binding opioid receptors including pain, obesity, hyperalgesia, inflammation, osteoarthritis, drug addiction, and cancer. These compounds and compositions are also useful as treatments for tardive dyskinesia.

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14-03-2013 дата публикации

2,5-disubstituted arylsulfonamide ccr3 antagonists

Номер: US20130065889A1
Принадлежит: Axikin Pharmaceuticals Inc

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

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14-03-2013 дата публикации

N-piperidinyl acetamide derivatives as calcium channel blockers

Номер: US20130065926A1
Принадлежит: Zalicus Pharmaceuticals Ltd

Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted T-type calcium channel activity are disclosed. Specifically, a series of compounds containing N-piperidinyl acetamide derivatives as shown in formula (1).

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28-03-2013 дата публикации

Amine Substituted Methanesulfonamide Derivatives as Vanilloid Receptor Ligands

Номер: US20130079320A1
Принадлежит: GRUENENTHAL GmbH

The invention relates to amine substituted methanesulfonamide derivatives as vanilloid receptor ligands, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders. 2. The substituted compound according to claim 1 , wherein{'sup': 1', '2', '9', '10, 'sub': 2', '2, 'claim-text': [{'sup': '9', 'sub': 3', '2', '5, 'wherein Rrepresents H, CH, or CH, and'}, {'sup': '10', 'sub': 2', '3', '2', '5, 'wherein Rrepresents NH, CH, or CH,'}], 'one of residues Rand Rdenotes CH—N(R)—S(═O)—R,'}{'sup': 1', '2, 'sub': 3', '2', '2', '3', '3', '3, 'and the respective remaining residue of Rand Ris selected from the group consisting of H, F, Cl, Br, I, CH, CH—OH, CH—O—CH, CF, OH, and O—CH.'}3. The substituted compound according to claim 1 , wherein{'sup': 2', '9', '10, 'sub': 2', '2, 'claim-text': [{'sup': '9', 'sub': 3', '2', '5, 'wherein Rrepresents H, CH, or CH, and'}, {'sup': '10', 'sub': 2', '3', '2', '5, 'wherein Rrepresents NH, CH, or CH,'}], 'Rdenotes CH—N(R)—S(═O)—R,'}{'sup': '1', 'sub': 3', '2', '2', '3', '3', '3, 'and Ris selected from the group consisting of H, F, Cl, Br, I, CH, CH—OH, CH—O—CH, CF, OH, and O—CH.'}4. The substituted compound according to claim 1 , wherein{'sup': '3', 'sub': 3', '3', '3, 'Ris selected from the group consisting of H, F, Cl, CH, CF, OH and O—CH.'}5. The substituted compound according to claim 1 , whereinZ represents N and{'sup': '4a', 'Rrepresents H,'}or{'sup': '4b', 'claim-text': {'sup': '4b', 'sub': '3', 'wherein Rrepresents H or CH, and'}, 'Z represents C—R,'}{'sup': '4a', 'Rrepresents H.'}6. The substituted compound according to claim 1 , wherein{'sup': '5', 'Rrepresents H.'}7. The substituted compound according to claim 1 , whereinX represents N.8. The substituted compound according to claim 1 , wherein{'sup': '6', 'sub': '3', 'Rrepresents CF, tert.-Butyl or cyclopropyl.'}9. The substituted compound according to claim 1 , ...

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28-03-2013 дата публикации

Substituted Phenylcarbamoyl Alkylamino Arene Compounds and N,N'-BIS-Arylurea Compounds

Номер: US20130079372A1
Принадлежит: MEDIVATION TECHNOLOGIES, INC.

Substituted phenylcarbamoyl alkylamino arenes; substituted phenylthiocarbamyl alkylamino arenes; substituted phenylcarbamoyl alkylamino heteroarenes; substituted phenylthiocarbamyl alkylamino heteroarenes; N-substituted aryl, N′-substituted aryl urea compounds; N-substituted aryl, N′-substituted heteroaryl urea compounds; N-substituted aryl, N′-substituted aryl thiourea compounds and N-substituted aryl, N′-substituted heteroaryl thiourea compounds are provided and may find use as androgen receptor modulators. The compounds may find particular use in treating prostate cancer, including castration-resistant prostate cancer and/or hormone-sensitive prostate cancer. 2. The compound of or a pharmaceutically acceptable salt thereof claim 1 , wherein:{'sup': 1', 'a', 'b, 'sub': 1', '8, '(a) Ris —C-Calkyl-NRR;'}{'sup': 1', 'a', 'b', '2, 'sub': 1', '8, '(b) Ris —C-Calkyl-NRRand Ris halo; or'}{'sup': 1', 'a', 'b', '2, 'sub': 1', '8, 'claim-text': [{'sup': '1', '(i) Wis CN;'}, {'sup': '2', '(ii) Wis perhaloalkyl;'}, '(iii) Z is O;', {'sup': 1', '2, '(iv) Yand Yare both methyl; and'}, '(v) T is C., '(b) Ris —C-Calkyl-NRR, Ris halo, and at least one of (i)-(v) applies3. The compound of or a pharmaceutically acceptable salt thereof claim 1 , wherein;{'sup': '1', 'sub': 1', '8, '(a) Ris —O—C-Calkyl-NR′R;'}{'sup': 1', 'c', '2, 'sub': 1', '8, '(b) Ris —O—C-Calkyl-NRR and Ris hydrogen; or'}{'sup': 1', 'c', '2, 'sub': 1', '8, 'claim-text': [{'sup': '1', '(i) Wis CN;'}, {'sup': '2', '(ii) Wis perhaloalkyl;'}, '(iii) Z is O;', {'sup': 1', '2, '(iv) Yand Yare both methyl and'}, '(v) T is C, '(c) Ris —O—C-Calkyl-NRR, Ris hydrogen, and at least one of (i)-(v) applies4. The compound of or a pharmaceutically acceptable salt thereof claim 1 , wherein:{'sup': 1', 'e', 'f, '(a) Ris —C(O)NRR;'}{'sup': 1', 'e', 'f', '2, '(b) Ris —C(O)NRRand Ris halo; or'}{'sup': 1', 'e', 'f', '2, 'claim-text': [{'sup': '1', '(i) Wis CN;'}, {'sup': '2', '(ii) Wis perhaloalkyl;'}, '(iii) Z is O;', {'sup': 1', '2, ...

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28-03-2013 дата публикации

PYRENYLOXYSULFONIC ACID FLUORESCENT AGENTS

Номер: US20130079497A1
Принадлежит: LIFE TECHNOLOGIES CORPORATION

The invention provides a novel class of reactive fluorescent agents that are based on a pyrene sulfonic acid nucleus. The agents are readily incorporated into conjugates with other species by reacting the reactive group with a group of complementary reactivity on the other species of the conjugate. Also provided are methods of using the compounds of the invention to detect and/or quantify an analyte in a sample. In an exemplary embodiment, the invention provides multi-color assays incorporating the compounds of the invention. 125.-. (canceled)27. The compound of wherein s is 1 and t is 2.28. The compound of wherein the linker arm comprises a straight-chain claim 26 , saturated chain of atoms and includes unsubstituted polyalkylene.30. The compound of wherein s is 1 and t is 2.32. The conjugate of wherein s is 1 and t is 2.33. The conjugate of wherein the linker arm comprises a straight-chain claim 31 , saturated chain of atoms and includes unsubstituted polyalkylene.35. The conjugate of claim 34 , wherein the linker arm comprises a cleavable group.36. The conjugate of claim 34 , wherein the linker arm comprises —C(O)NH— claim 34 , —C(O)O— claim 34 , —NH— claim 34 , —S— claim 34 , or —O—.37. The conjugate of claim 34 , wherein s is 1 claim 34 , and t is 2.38. A kit for the detection of an analyte in a sample claim 26 , wherein said kit comprises a compound of .39. A kit for the detection of an analyte in a sample claim 29 , wherein said kit comprises a compound of .40. A kit for the detection of an analyte in a sample claim 31 , wherein said kit comprises a conjugate of .41. A kit for the detection of an analyte in a sample claim 34 , wherein said kit comprises a conjugate of . NOT APPLICABLENOT APPLICABLENOT APPLICABLEThe present invention relates to novel fluorescent compounds that have utility in detecting one or more selected analytes in a sample. The invention is of use in a variety of fields including immunology, diagnostics, molecular biology and fluorescence ...

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28-03-2013 дата публикации

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

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

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

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28-03-2013 дата публикации

METHOD FOR PRODUCING OPTICALLY ACTIVE 3-AMINOPIPERIDINE OR SALT THEREOF

Номер: US20130079525A1
Принадлежит: KANEKA CORPORATION

The present invention relates to a method for producing an optically active 3-aminopiperidine or salt thereof. In the method, a racemic nipecotamide is stereoselectively hydrolyzed to obtain an optically active nipecotamide and an optically active nipecotic acid in the presence of an enzyme source derived from an organism, and then the optically active nipecotamide is derived into an optically active aminopiperidine or salt thereof by aroylation, Hofmann rearrangement, deprotection of the amino group and further deprotection; or the optically active nipecotamide is derived into an optically active aminopiperidine or salt thereof by selective protection with BOC, Hofmann rearrangement and further deprotection. It is possible by the present invention to produce an optically active 3-aminopiperidine or salt thereof useful as a pharmaceutical intermediate from an inexpensive and easily available starting material by easy method applicable to industrial manufacturing. 118.-. (canceled) The present invention relates to a method for producing an optically active 3-aminopiperidine or salt thereof useful as a pharmaceutical intermediate, and to intermediates useful for producing the 3-aminopiperidine.As methods for producing an optically active 3-aminopiperidine or salt thereof, or a derivative of optically active 3-aminopiperidine, for example, the following methods are known:1) a method, wherein L-ornithine monohydrochloride is methyl-esterified, and then (S)-3-amino piperidone is obtained by chromatography with an ion exchange resin, the (S)-3-amino piperidone is reacted with lithium aluminum hydride to be (S)-3-aminopiperidine, an inorganic salt is removed by filtration, and the target compound is purified (Non-patent Document 1);2) a method, wherein ethyl nipecotate is optically resolved using L-tartaric acid, the nitrogen atom is protected with benzyloxycarbonyl group, the ethyl ester is hydrolyzed in alkaline condition, Curtius rearrangement is carried out using ...

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04-04-2013 дата публикации

HETEROCYCLIC COMPOUND AND H1 RECEPTOR ANTAGONIST

Номер: US20130085127A1
Принадлежит: ASKA Pharmaceutical Co., Ltd

A heterocyclic compound useful as an antiallergic agent is provided. 3. A heterocyclic compound or a salt thereof according to claim 1 , whereinthe ring A is a benzene ring or an aromatic 5- or 6-membered heterocyclic ring;the ring B is an aliphatic 4- to 10-membered heterocyclic ring;{'sup': '1', 'sub': '1-4', 'Ris a straight chain or branched chain Calkylene group;'}{'sup': 2a', '2b, 'sub': 1-6', '1-6', '1-6', '1-6, 'Rand Rare the same or different and each are a benzene ring which may have at least one substituent selected from the group consisting of a halogen atom, a Calkyl group, a haloCalkyl group, a Calkoxy group and a haloCalkoxy group;'}{'sub': 1-4', '1-4', '1-4, 'Z is a hydroxyl group; a Calkoxy group; an amino group; or an N-substituted amino group in which the nitrogen atom has at least one substituent selected from the group consisting of a Calkyl group and a Calkyl-carbonyl group; and'}when G is CH, X is an oxygen atom and n is 1; when G is N, n is 0.4. A heterocyclic compound or a salt thereof according to claim 1 , whereinthe ring A is an aromatic heterocyclic ring containing at least one hetero atom selected from the group consisting of a nitrogen atom, an oxygen atom and a sulfur atom;the ring B is an aliphatic 5- or 6-membered heterocyclic ring;{'sup': '1', 'sub': '1-3', 'Ris a straight chain or branched chain Calkylene group;'}{'sup': 2a', '2b, 'sub': 1-3', '1-3', '1-3', '1-3, 'Rand Rare the same or different and each are a benzene ring which may have at least one substituent selected from the group consisting of a fluorine atom, a chlorine atom, a Calkyl group, a haloCalkyl group, a Calkoxy group and a haloCalkoxy group; and'}{'sub': 1-3', '1-3', '1-3, 'Z is a hydroxyl group; a Calkoxy group; an amino group; or an N-substituted amino group in which the nitrogen atom has at least one substituent selected from the group consisting of a Calkyl group and a Calkyl-carbonyl group.'}5. A heterocyclic compound or a salt thereof according to claim 1 , ...

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04-04-2013 дата публикации

NOVEL BENZAMIDE DERIVATIVES

Номер: US20130085160A1
Принадлежит:

The present invention provides a novel benzamide derivative or a pharmaceutically acceptable salt thereof, a method for preparing the same, and a 5-HTreceptor agonist containing the same as an active ingredient. Benzamide derivatives of the present invention have a superior affinity for 5-HTreceptors, a capability to reduce a gastric emptying time and a low toxicity, and consequently are therapeutically effective for the treatment of a variety of diseases associated with -HTreceptors. 2. The compound of formula 1 of claim 1 , wherein m represents an integer of 1 to 5; and Q represents a heteroaromatic ring or phenyl wherein the heteroaromatic ring or phenyl is independently substituted by 0 claim 1 , 1 claim 1 , 2 or 3 substituents selected from among C-Calkyl claim 1 , C-Calkoxy claim 1 , hydroxy and halogen claim 1 , wherein the heteroaromatic ring is a C-Caromatic ring or C-Cbicyclic aromatic ring independently containing 1 to 4 hetero atoms selected from among N claim 1 , O and S.3. The compound of formula 1 of that is selected from among the following compounds:N-((1-(3-(1,2,4-triazol-1-yl)propyl)piperidin-4-yl)methyl)-4-amino-5-chloro-2-methoxybenzamide,N-((1-(3-(tetrazol-1-yl)propyl)piperidin-4-yl)methyl)-4-amino-5-chloro-2-methoxybenzamide,N-((1-(3-(indol-1-yl)propyl)piperidin-4-yl)methyl)-4-amino-5-chloro-2-methoxybenzamide,N-((1-(3-(2-methylimidazol-1-yl)propyl)piperidin-4-yl)methyl)-4-amino-5-chloro-2-methoxybenzamide,N-((1-(5-(indol-1-yl)pentyl)piperidin-4-yl)methyl)-4-amino-5-chloro-2-methoxybenzamide,N-((1-(5-(1,2,3-triazol-1-yl)pentyl)piperidin-4-yl)methyl)-4-amino-5-chloro-2-methoxybenzamide,N-((1-(3-(1,2,3-triazol-1-yl)propyl)piperidin-4-yl)methyl)-4-amino-5-chloro-2-methoxybenzamide,N-((1-(3-(1,2,3-triazol-2-yl)propyl)piperidin-4-yl)methyl)-4-amino-5-chloro-2-methoxybenzamide,N-((1-(pyridin-3-ylmethyl)piperidin-4-yl)methyl)-4-amino-5-chloro-2-methoxybenzamide,N-((1((1-methylindol-3-yl)methyl)piperidin-4-yl)methyl)-4-amino-5-chloro-2- ...

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04-04-2013 дата публикации

AMIDO COMPOUNDS AS RORyT MODULATORS AND USES THEREOF

Номер: US20130085162A1
Принадлежит:

Amido compounds are disclosed that have a formula represented by the following: 2. The method according to claim 1 , wherein each Rand Ris independently selected from H claim 1 , Me claim 1 , Et claim 1 , n-Pr claim 1 , i-Pr claim 1 , n-Bu claim 1 , t-Bu claim 1 , hydroxyethyl claim 1 , hydroxypropyl claim 1 , aminoethyl claim 1 , aminopropyl claim 1 , dimethylaminoethyl claim 1 , dimethylaminopropyl claim 1 , piperidinoethyl claim 1 , morpholinoethyl claim 1 , cyclopropylmethyl claim 1 , benzyl claim 1 , phenethyl claim 1 , furanylmethyl claim 1 , cyclopropyl claim 1 , cyclobutyl claim 1 , cyclopentyl claim 1 , cyclohexyl claim 1 , and substituted and unsubstituted phenyl.3. (canceled)4. (canceled)5. (canceled)6. (canceled)7. (canceled)8. (canceled)9. (canceled)10. (canceled)11. (canceled)12. (canceled)14. The method according to claim 13 , wherein Cy is azetidinyl claim 13 , pyrrolidinyl claim 13 , piperidinyl claim 13 , piperizinyl claim 13 , morpholinyl claim 13 , tetrahydroquinolinyl claim 13 , indolinyl claim 13 , or azepinyl claim 13 , unsubstituted or substituted with alkyl claim 13 , substituted alkyl claim 13 , haloalkyl claim 13 , alkoxyalkyl claim 13 , hydroxyalkyl claim 13 , alkoxy claim 13 , hydroxyl claim 13 , CN claim 13 , substituted or unsubstituted aryl claim 13 , substituted or unsubstituted heteroaryl claim 13 , amido claim 13 , acyl claim 13 , aroyl claim 13 , or —CO-alkoxy.16. (canceled)17. (canceled)18. (canceled)21. (canceled)22. The method according to claim 19 , wherein each of Rand Ris independently OH claim 19 , substituted or unsubstituted alkyl claim 19 , substituted or unsubstituted alkoxy claim 19 , CN claim 19 , halo claim 19 , amido claim 19 , or haloalkyl.23. (canceled)24. (canceled)25. (canceled)26. (canceled)27. (canceled)28. The method according to claim 1 , wherein Rand Ris independently H claim 1 , CN claim 1 , or Me.29. (canceled)30. (canceled)31. (canceled)32. (canceled)33. The method according to claim 1 , wherein Ris H ...

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04-04-2013 дата публикации

NITROGENOUS HETEROCYCLIC DERIVATIVE AND MEDICINE CONTAINING THE SAME AS AN ACTIVE INGREDIENT

Номер: US20130085275A1
Принадлежит: ONO PHARMACEUTICAL CO., LTD.

A compound represented by formula (I), a salt thereof, an N-oxide thereof, a solvate thereof or a prodrug thereof: 133-. (canceled)34. A compound selected from the group consisting of(1) N-[6-(4-{[4-(butyl{[(2,4-difluorophenyl)amino]carbonyl}amino)-1-piperidinyl]methyl}phenoxy)-3-pyridinyl]methanesulfonamide,(3) N-{4-[4-({4-[{[(2-hydroxybutyl)amino]carbonyl}(phenyl)amino]-1-piperidinyl}methyl)phenoxy]phenyl}methanesulfonamide,(4) N-{4-[4-({4-[butyl({[1-(2-hydroxyethyl)-1H-pyrazol-4-yl]amino}carbonyl)amino]-1-piperidinyl}methyl)phenoxy]phenyl}methanesulfonamide,(5) 5-[({butyl[1-(4-{4-[(methylsulfonyl)amino]phenoxy}benzyl)-4-piperidinyl]amino}carbonyl)amino]-2,4-difluoro-N-methylbenzamide,(6) N-{4-[4-({4-[{[(4-hydroxycyclohexyl)amino]carbonyl}(phenyl)amino]-1-piperidinyl}methyl)phenoxy]phenyl}methanesulfonamide,(7) N-[4-(4-{[4-(3-butenyl {[(2-hydroxybutyl)amino]carbonyl}amino)-1-piperidinyl]methyl}phenoxy)phenyl]methanesulfonamide,(8) N-butyl-N′-(2,4-difluorophenyl)-N-(1-{4-[4-(4-morpholinylsulfonyl)phenoxy]benzyl}-4-piperidinyl)urea,(9) N-butyl-2-(2,4-difluorophenyl)-N-[1-(4-{4-[(methylsulfonyl)amino]phenoxy}benzyl)-4-piperidinyl]acetamide,(10) N-{4-[(5-{[4-(butyl{[(1-methyl-1H-pyrazol-4-yl)amino]carbonyl}amino)-1-piperidinyl]methyl}-2-pyridinyl)oxy]phenyl}methanesulfonamide,(11) N-(4-{4-[(4-{{[(4-fluorophenyl)amino]carbonyl}[4-(methylsulfanyl)phenyl]amino}-1-piperidinyl)methyl]phenoxy}phenyl)methanesulfonamide,(12) N-(4-{4-[(4-{{[(4-fluorophenyl)amino]carbonyl}[3-(methylsulfanyl)phenyl]amino}-1-piperidinyl)methyl]phenoxy}phenyl)methanesulfonamide,(13) N-butyl-2,4-difluoro-N-[1-(4-{4-[(methylsulfonyl)amino]phenoxy}benzyl)-4-piperidinyl]benzamide,(14) N-(4-{4-[(4-{{[(4-fluorophenyl)amino]carbonyl}[4-(methylsulfinyl)phenyl]amino}-1-piperidinyl)methyl]phenoxy}phenyl)methanesulfonamide,(15) N-(4-{4-[(4-{{[(4-fluorophenyl)amino]carbonyl}[3-(methylsulfinyl)phenyl]amino}-1-piperidinyl)methyl]phenoxy}phenyl)methanesulfonamide,(16) N-(4-{4-[(4-{{[(4-fluorophenyl)amino] ...

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11-04-2013 дата публикации

DEUTERIUM-ENRICHED DONEPEZIL

Номер: US20130090357A1
Автор: Czarnik Anthony W.
Принадлежит: DEUTERIA PHARMACEUTICALS INC

The present application describes deuterium-enriched donepezil, pharmaceutically acceptable salt forms thereof, and methods of treating using the same. 2. (canceled)3. (canceled)4. (canceled)5. (canceled)6. (canceled)7. (canceled)8. (canceled)9. (canceled)10. (canceled)11. (canceled)12. (canceled)13. (canceled)14. (canceled)15. (canceled)16. (canceled)17. (canceled)18. (canceled)19. A pharmaceutical composition claim 1 , comprising: a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound of or a pharmaceutically acceptable salt form thereof.20. A method for treating Alzheimer's disease comprising: administering claim 1 , to a21. in need thereof claim 1 , a therapeutically effective amount of a compound of or a pharmaceutically acceptable salt form thereof. The present application claims priority benefit under 35 U.S.C. §119(e) of U.S. Provisional Patent Application Ser. No. 60/971,892 filed 12 Sep. 2007. The disclosure of this application is incorporated herein by reference.This invention relates generally to deuterium-enriched donepezil, pharmaceutical compositions containing the same, and methods of using the same.Donepezil, shown below, is a well known centrally acting reversible acetyl cholinesterase inhibitor.Since donepezil is a known and useful pharmaceutical, it is desirable to discover novel derivatives thereof. Donepezil is described in U.S. Pat. Nos. 4,895,841, and 5,100,901; the contents of which are incorporated herein by reference.Accordingly, one object of the present invention is to provide deuterium-enriched donepezil or a pharmaceutically acceptable salt thereof.It is another object of the present invention to provide pharmaceutical compositions comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of at least one of the deuterium-enriched compounds of the present invention or a pharmaceutically acceptable salt thereof.It is another object of the present invention to provide a ...

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18-04-2013 дата публикации

ArylSulfonamide Based Matrix Metalloprotease Inhibitors

Номер: US20130096105A1
Принадлежит: NOVARTIS AG

The present invention provides a compound of formula (I): 2. The compound of claim 1 , wherein Ris selected from (C-C) aryl claim 1 , (5-14) membered heteroaryl claim 1 , and (4-14) membered heterocycloalkyl claim 1 , each of which is optionally substituted by one to three substituents selected from the group consisting of HC(O)— claim 1 , (5-9) membered heteroaryl claim 1 , and (4-9) membered heterocycloalkyl claim 1 , (C-C) alkyl claim 1 , (C-C) cycloakyl claim 1 , R—O— claim 1 , R—C(O)— claim 1 , R—SO— claim 1 , (R)NH—C(O)— claim 1 , and (R)(R)N— claim 1 , wherein R claim 1 , R claim 1 , R claim 1 , R claim 1 , Rand Rare independently (C-C) alkyl or (C-C) aryl claim 1 , each of which is further optionally substituted by one to two substituents selected from the group consisting of (C-C) alkyl claim 1 , halo claim 1 , hydroxy claim 1 , (C-C) alkoxy claim 1 , (C-C) aryl claim 1 , (C-C) dialkylamino claim 1 , and (4-9) membered heterocycloalkyl; Rand Rare independently hydrogen claim 1 , or (C-C) alkyl; X is selected from hydrogen claim 1 , amine claim 1 , cyano claim 1 , halogen claim 1 , nitro claim 1 , alkyl-S— claim 1 , alkyl-SO— claim 1 , alkyl-SO— claim 1 , HN—SO— claim 1 , R—C(O)— claim 1 , alkyl claim 1 , and R—O claim 1 , wherein Rand Rare defined above; ora pharmaceutically acceptable salt thereof, or an optical isomer thereof; or a mixture of optical isomers.4. The compound of claim 3 , wherein R′ claim 3 , is selected from (C-C) alkyl claim 3 , (C-C) cycloalkyl claim 3 , (C-C) alkoxy claim 3 , HC(O)— claim 3 , (5-9) membered heteroaryl claim 3 , and (4-9) membered heterocycloalkyl claim 3 , or (C-C) aryl claim 3 , said (C-C) aryl claim 3 , (5-9) membered heteroaryl claim 3 , and (4-9) membered heterocycloalkyl are optionally substituted by one or two substituents selected from hydroxy claim 3 , halo claim 3 , (C-C) alkyl claim 3 , carboxyl claim 3 , (C-C) alkoxycarbonyl claim 3 , and HC(O)—;{'sub': 2', '3, 'Rand Rare hydrogen;'}{'sub': 1', '7, 'X is ...

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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

TARGETED NITROXIDE AGENTS

Номер: US20130102626A1
Принадлежит:

Provided herein are compositions and related methods useful for free radical scavenging, with particular selectivity for mitochondria. The compounds comprise a nitroxide-containing group attached to a mitochondria-targeting group. The compounds can be cross-linked into dimers without loss of activity. Also provided herein are methods, for preventing, mitigating and treating damage caused by radiation. The method comprises delivering a compound, as described herein, to a patient in an amount and dosage regimen effective to prevent, mitigate or treat damage caused by radiation. 45-. (canceled)6. The compound of claim 1 , in which R is Ac claim 1 , Boc claim 1 , Cbz claim 1 , or —P(O)-Ph.7. The compound of claim 1 , in which R claim 1 , R claim 1 , Rand Rare independently chosen from hydrogen claim 1 , methyl claim 1 , ethyl claim 1 , propyl claim 1 , 2-propyl claim 1 , butyl claim 1 , t-butyl claim 1 , pentyl claim 1 , hexyl claim 1 , benzyl claim 1 , hydroxybenzyl claim 1 , phenyl and hydroxyphenyl.8. The compound of claim 1 , wherein when X is —CH═CR— claim 1 , Ris hydrogen claim 1 , methyl or ethyl.912-. (canceled)13. The compound of in which R1 claim 1 , R2 and R3 independently are methyl claim 1 , ethyl claim 1 , propyl claim 1 , 2-propyl claim 1 , butyl claim 1 , t-butyl claim 1 , pentyl claim 1 , hexyl claim 1 , benzyl claim 1 , hydroxybenzyl claim 1 , phenyl and hydroxyphenyl.1421-. (canceled)27. A method of making a targeted antioxidant compound claim 1 , comprising:{'sub': 1', '1', '1', '6', '6', '5, 'a. reacting an aldehyde of structure R—C(O)— with (R)-2-methylpropane-2-sulfinamide to form an imine, in which Ris C-Cstraight or branched-chain alkyl, optionally including a phenyl (CH) group, that optionally is methyl-, hydroxyl- or fluoro-substituted;'}{'sub': 2', '2', '2, 'b. reacting a terminal alkyne-1-ol (HCC—R—CH—OH), in which Ris not present or is branched or straight-chained alkylene, with a tert-butyl)diphenylsilane salt to produce an alkyne;'}c. ...

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25-04-2013 дата публикации

Inhibitors of protein prenyltransferases

Номер: US20130102639A1
Принадлежит: UNIVERSITY OF CALIFORNIA

The present invention is directed to novel compounds. These compounds can be useful in inhibiting the activity of protein prenyltransferases including GGTase I and/or RabGGTase. The compounds can also be used as anti-cancer therapeutics including as part of methods for treating cancer, in assays, and in kits.

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25-04-2013 дата публикации

THIONATION PROCESS AND A THIONATING AGENT

Номер: US20130102774A1
Принадлежит: Vironova AB

A process for transforming a group >C═O (I) in a compound into a group >C═S (II) or into a tautomeric form of group (II) in a reaction giving a thionated reaction product, by use of crystalline PS.2 CHN as a thionating agent. A thionating agent which is crystalline PS.2 CHN. 1. A process for transforming a group >C═O (I) in a compound into a group >C═S (II) or into a tautomeric form of group (II) in a reaction giving a thionated reaction product , by use of crystalline PS.2 CHN as a thionating agent.2. A process according to claim 1 , wherein the thionating agent and the compound are allowed to react with each other in a liquid solvent medium for the compound and for the thionating agent.3. The process according to claim 1 , wherein the liquid solvent medium comprises pyridine claim 1 , a C1-C3 alkylnitrile claim 1 , a cyclic sulfone and/or a C1-C3 dialkylsulfone.4. The process according to claim 1 , wherein the liquid solvent medium comprises pyridine claim 1 , sulfolane claim 1 , dimethyl sulfone and/or acetonitrile.5. The process according to claim 1 , wherein the reaction is performed at a temperature of 60° C. to 180° C.6. The process according to claim 5 , wherein the reaction is performed at temperature of 115° C. to 175° C.7. The process according to claim 1 , wherein the compound comprises a group (I) that is present in an amide function.8. The process according to claim 1 , wherein the compound comprises a group (I) that is present in a ketone function.9. The process according to claim 1 , wherein the thionating agent is used at a molar ratio to the group (I) to be transformed of 1 mole PS.2 CHN per 1-4 moles of group (I).10. The process according to claim 1 , comprising separating the thionated reaction product from the reaction.11. The process according to claim 10 , wherein water is added to the reaction and the thionated reaction product is separated as a solid material claim 10 , by precipitation or crystallization.12. A thionating agent which is ...

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25-04-2013 дата публикации

Substituted Tetracycline Compounds

Номер: US20130102779A1
Автор: Abato Paul
Принадлежит: PARATEK PHARMACEUTICALS, INC.

The present invention pertains to tetracycline compounds of formula (VIIa): 2. The tetracycline compound of claim 1 , wherein Ris oxazolyl.3. The tetracycline compound of claim 2 , wherein oxazolyl is substituted with methyl or isopropyl.4. The tetracycline compound of claim 1 , wherein Ris oxadiazolyl.5. The tetracycline compound of claim 4 , wherein oxadiazolyl is substituted with alkyl.6. The tetracycline compound of claim 1 , wherein Ris isoxazolyl.7. The tetracycline compound of claim 1 , wherein Ris pyrazolyl.8. The tetracycline compound of claim 7 , wherein Ris methylpyrazolyl.9. The tetracycline compound of claim 1 , wherein Ris —CONRR claim 1 , in which Ris hydrogen and Ris hydroxyl claim 1 , hydroyxalkyl claim 1 , alkoxy claim 1 , phenyl claim 1 , or alkyl.10. The tetracycline compound of claim 1 , wherein Ris wherein Ris —CONRR claim 1 , in which Ris alkyl and Ris alkyl or hydroxyl.11. The tetracycline compound of claim 1 , wherein Ris dialkylamino.12. The tetracycline compound of claim 11 , wherein Ris dimethylamino.13. The tetracycline compound of claim 1 , wherein each of R claim 1 , R claim 1 , R claim 1 , and R is hydrogen.14. The tetracycline compound of claim 13 , wherein Ris dialkylamino.15. The tetracycline compound of claim 14 , wherein Ris dimethylamino.19. A pharmaceutical composition comprising a tetracycline compound of and a pharmaceutically acceptable carrier.20. A method for treating a tetracycline responsive state in a subject claim 1 , comprising administering to said subject an effective amount of a tetracycline compound of claim 1 , such that said subject is treated. This application is a divisional application of U.S. Ser. No. 11/963,540, filed on Dec. 21, 2007 and issued as U.S. Pat. No. 8,318,706 on Nov. 27, 2012, which claims priority to U.S. Provisional Patent Application No. 60/876,313, filed on Dec. 21, 2006 and U.S. Provisional Patent Application No. 60/943,003, filed Jun. 8, 2007. The contents of the foregoing applications ...

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02-05-2013 дата публикации

Bile Acid Recycling Inhibitors for Treatment of Hypercholemia and Cholestatic Liver Disease

Номер: US20130108573A1
Принадлежит: Lumena Pharmaceuticals, Inc.

Provided herein are methods of treating or ameliorating hypercholemia or a cholestatic liver disease by administering to an individual in need thereof a therapeutically effective amount of an Apical Sodium-dependent Bile Acid Transporter Inhibitor (ASBTI) or a pharmaceutically acceptable salt thereof. Also provided are methods for treating or ameliorating a liver disease, decreasing the levels of serum bile acids or hepatic bile acids, treating or ameliorating pruritis, reducing liver enzymes, or reducing bilirubin comprising administering to an individual in need thereof a therapeutically effective amount of ASBTI or a pharmaceutically acceptable salt thereof. 1. A method for treating or ameliorating hypercholemia comprising non-systemically administering to an individual in need thereof a therapeutically effective amount of an Apical Sodium-dependent Bile Acid Transporter Inhibitor (ASBTI) or a pharmaceutically acceptable salt thereof.2. The method of claim 1 , wherein the method comprises decreasing at least 20% of serum bile acid or hepatic bile acid levels in the patient.3. The method of claim 1 , wherein less than 10% of the ASBTI is systemically absorbed.5. The method of claim 4 , wherein:q is 1;n is 2;{'sup': 'x', 'sub': 3', '2, 'Ris N(CH);'}{'sup': 7', '8, 'Rand Rare independently H;'}{'sup': 1', '2, 'Rand Ris alkyl;'}{'sup': 3', '4, 'Ris H, and Ris OH;'}{'sup': 5', '6', '9', '9', '9', '9', '9, 'sub': 2', '3', 'Z', 'Z, 'claim-text': wherein z is 1, 2 or 3; each L is independently a substituted or unsubstituted alkyl, a substituted or unsubstituted heteroalkyl, a substituted or unsubstituted alkoxy, a substituted or unsubstituted aminoalkyl group, a substituted or unsubstituted aryl, a substituted or unsubstituted heteroaryl, a substituted or unsubstituted cycloalkyl, or a substituted or unsubstituted heterocycloalkyl; each K is a moiety that prevents systemic absorption;', {'sup': 15', '13', '13', '14', '13', '14', '13', '13', '13', '13', '13', '14', '13', ...

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02-05-2013 дата публикации

C7-Fluoro Substituted Tetracycline Compounds

Номер: US20130109657A1
Принадлежит: Tetraphase Pharmaceuticals Inc

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

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02-05-2013 дата публикации

Chemical Compounds

Номер: US20130109701A1
Принадлежит: PFIZER LIMITED

The invention relates to sulfonamide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to a new sulfon-amide Nav1.7 inhibitors of formula (I): or a pharmaceutically acceptable salt thereof, wherein X, Ar, R, R, R, Rand Rare as defined in the description. Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain. 2. A compound according to wherein X is —OCH—.3. A compound according to wherein X is —CHO—.4. A compound according to wherein Aris phenyl independently substituted by one to three Y.5. A compound according to wherein Arphenyl independently substituted by one or two Y.6. A compound according to wherein Aris phenyl meta-substituted by Y claim 1 , para-substituted by Y claim 1 , or meta- and para-substituted by independent Y.7. A compound according to wherein Y is F; Cl; CN; (C-C)alkyl claim 1 , optionally substituted by (C-C)cycloalkyl or one to three F; (C-C)cycloalkyl claim 1 , optionally substituted by one to three F; (C-C)alkyloxy claim 1 , optionally substituted by one to three F; or (C-C)cycloalkyloxy.8. A compound according to wherein Ris (C-C)alkyl or (C-C)cycloalkyl.9. A compound according to wherein Ris (C-C)alkyl or (C-C)cycloalkyl.10. A compound according to wherein R claim 1 , Rand Rare independently H claim 1 , F or Cl.11. A compound according to wherein Ris H; CN; F; Cl; (C-C)alkyl claim 1 , optionally substituted by one to three F; or (C-C)alkyloxy claim 1 , optionally substituted by one to three F.12. A pharmaceutical composition comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof together claim 1 , as defined in claim 1 , with one or more pharmaceutically acceptable excipients.13. A pharmaceutical composition according to including one or more additional therapeutic agents.14. (canceled)15. (canceled)16. (canceled)17. ( ...

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09-05-2013 дата публикации

Synthesis of mse-framework type molecular sieves

Номер: US20130115163A1
Принадлежит: ExxonMobil Research and Engineering Co

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

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16-05-2013 дата публикации

CHEMICAL AND BIOLOGICAL AGENTS FOR THE CONTROL OF MOLLUSCS

Номер: US20130121978A1
Принадлежит: MARRONE BIO INNOVATIONS, INC.

Compositions and methods for controlling molluscs, members of the Gastropoda and Bivalvia classes which includes but is not limited to lactones, lactams, carbamates, amides, and/or carboxylic acid containing compounds as active ingredients and/or compounds derived from and/or . Also provided are methods and compositions for increasing the efficacy of chemical and biological control for invasive molluscs in open waters, power plants, and drinking water treatment facilities under coldwater conditions. 1. A combination comprising at least one or more substances effective for controlling a member of a Gastropoda and Bivalvia class and an inert material.2PseudomonasPseudomonas. The combination according to claim 1 , wherein said substances are derived from a species or cell suspension or toxin derived from a species.3Pseudomonas fluorescensPseudomonas fluorescens.. The combination according to claim 1 , wherein said substances are derived from a or cell suspension derived from4PseudomonasPseudomonas. The combination according to claim 1 , wherein said substances are derived from a strain claim 1 , having the identifying characteristics of ATCC 55799.5Pseudomonas. The combination according to claim 1 , wherein the composition comprises a substance that is a cell suspension comprising cells having the toxin producing characteristics of ATCC 55799.6. The combination of claim 1 , wherein said combination is a composition.7ErwiniaPseudomonas. A method for controlling one or more molluscs in a location where control is desired comprising introducing into said location at least one of (a) a cell suspension or extract derived from sp. Cells; (b) one or more compounds claim 1 , wherein said compounds are lactone claim 1 , lactam claim 1 , carbamate claim 1 , carboxylic acid and/or amide compounds or composition comprising said compounds claim 1 , with the proviso that said compounds are not gamma-octalactone claim 1 , gamma-nonalactone claim 1 , gamma-decanolactone claim 1 , ...

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16-05-2013 дата публикации

DIAMINE DERIVATIVES AS INHIBITORS OF LEUKOTRIENE A4 HYDROLASE

Номер: US20130123243A1
Принадлежит:

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

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23-05-2013 дата публикации

STYRYLPYRIDINE DERIVATIVES AND THEIR USE FOR BINDING AND IMAGING AMYLOID PLAQUES

Номер: US20130129624A1

This invention relates to a method of imaging amyloid deposits and to styrylpyridine compounds, and methods of making radiolabeled styrylpyridine compounds useful in imaging amyloid deposits. This invention also relates to compounds, and methods of making compounds for inhibiting the aggregation of amyloid proteins to form amyloid deposits, and a method of delivering a therapeutic agent to amyloid deposits. 3. The compound of claim 1 , wherein n is one.4. The compound of claim 1 , wherein at least one halogen is a radiohalogen.5. The compound of claim 1 , wherein at least one halogen is I claim 1 , I claim 1 , I claim 1 , I claim 1 , Br claim 1 , Br claim 1 , Br claim 1 , F or F.6. The compound of claim 5 , wherein Ris —(CH)NRR claim 5 , wherein Rand Rare independently hydrogen or Calkyl and p is 0.8. The compound of claim 7 , wherein q is an integer from 1 to 5.9. The compound of claim 8 , wherein R claim 8 , R claim 8 , Rand Rare each hydrogen.14. The compound of claim 13 , wherein q is an integer from 1 to 5.15. The compound of claim 14 , wherein R claim 14 , R claim 14 , Rand Rare each hydrogen claim 14 , and q is 1 claim 14 , 2 or 3.17. The compound of claim 16 , wherein R claim 16 , R claim 16 , Rand R claim 16 , R claim 16 , Rand Rare each hydrogen.20. A composition comprising a compound according to wherein said compound contains a C isotope claim 1 , said isotope present in an amount above natural abundance claim 1 , and said compound containing said C isotope having a specific activity above background level.22. The compound of claim 21 , wherein one of R′ and R″ is hydrogen claim 21 , the other is Calkyl.23. A pharmaceutical composition comprising a compound of any one of or and a pharmaceutically acceptable carrier or diluent.24. A diagnostic composition for imaging amyloid deposits claim 21 , comprising a radiolabeled compound of any one of or and a pharmaceutically acceptable carrier or diluent.25. A method of imaging amyloid deposits in a mammal claim ...

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23-05-2013 дата публикации

DERIVATIVES OF AMINOINDANES, THEIR PREPARATION AND THEIR APPLICATION IN THERAPEUTICS

Номер: US20130131034A1
Принадлежит: SANOFI

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

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23-05-2013 дата публикации

Amelioration Of The Development Of Cataracts And Other Ophthalmic Diseases

Номер: US20130131052A1
Принадлежит:

Ophthalmically acceptable compositions used in arresting the development of cataracts or macular degeneration comprising a pharmaceutically acceptable carrier or diluent and a compound having the formula: 1. An ophthalmic composition comprising an ophthalmically acceptable carrier or diluent and a compound having an N-hydroxy piperidine portion bound to a solubility modifying portion , the compound having a solubility in water at 25° C. of at least about 0.25% by weight and a water-n-octonal partition coefficient at 25° C. of at least about 5.2. The composition of wherein the N-hydroxy piperidine portion is cleaved from the compound under conditions found in the eye.3. The composition of wherein the N-hydroxy piperidine portion is cleaved from the compound under conditions found in the lens of the eye.4. The composition of wherein the N-hydroxy piperidine portion is cleaved enzymatically.5. The composition of wherein the N-hydroxy piperidine portion is 1-oxyl-4-hydroxy-2 claim 1 ,2 claim 1 ,6 claim 1 ,6-tetramethylpiperidyl.6. The composition of further comprising a reducing agent.7. The composition of wherein the reducing agent is a sulfhydryl compound.8. The composition of further comprising mercaptopropionyl glycine claim 1 , N-acetyl cysteine claim 1 , β-mercaptoethylamine claim 1 , or glutathione.9. A method of administering an antioxidant to a mammal comprising contacting the mammal with a composition comprising a pharmaceutically acceptable carrier or diluent and a compound having an N-hydroxy piperidine portion bound to a solubility modifying portion claim 1 , the compound having a solubility in water at 25° C. of at least about 0.25% by weight and a water-n-octonal partition coefficient at 25° C. of at least about 5.10. The method of wherein the composition further comprises a reducing agent.11. The method of further comprising coadministering a reducing agent to the patient.12. The method of wherein the reducing agent is a sulfhydryl compound.13. The ...

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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

O-CYCLOPROPYLCYCLOHEXYL-CARBOXANILIDES AND THEIR USE AS FUNGICIDES

Номер: US20130131124A1
Принадлежит: Bayer Intellectual Property GmbH

The present invention relates to O-CYCLOPROPYLCYCLOHEXYL-CARBOXANILIDES derivatives of formula (I); their process of preparation, their use as fungicide, particularly in the form of fungicide compositions, and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions. 2. A compound of formula (I) as claimed in claim 1 , wherein{'sup': 1', '2, 'Rand Rare, independently, hydrogen or fluoro;'}{'sup': '3', 'sub': 2-6', '3-8, 'Ris Calkyl, optionally substituted Ccycloalkyl, phenyl, thienyl or furyl;'}A represents one of the radicals A1, A2, A3, A4, A5, A6, A9, A10, A11, A12 or A17;{'sup': '18', 'sub': 1', '2', '1', '2, 'Rrepresents hydrogen, cyano, fluorine, chlorine, bromine, iodine, methyl, ethyl, isopropyl, methoxy, ethoxy, methylthio, ethylthio, cyclopropyl, C-Chaloalkyl C-C-haloalkoxy having in each case 1 to 5 fluorine, chlorine and/or bromine atoms, trifluoromethylthio, difluoromethylthio, aminocarbonyl, aminocarbonylmethyl or aminocarbonylethyl;'}{'sup': '19', 'Rrepresents hydrogen, fluorine, chlorine, bromine, iodine, methyl, ethyl, methoxy, ethoxy, methylthio or ethylthio;'}{'sup': '20', 'sub': 1', '2, 'Rrepresents hydrogen, methyl, ethyl, n-propyl, isopropyl, C-C-haloalkyl having 1 to 5 fluorine, chlorine and/or bromine atoms, hydroxymethyl, hydroxyethyl, cyclopropyl, cyclopentyl, cyclohexyl or phenyl.'}{'sup': 21', '22, 'sub': 1', '2, 'Rand Rindependently of one another represent hydrogen, fluorine, chlorine, bromine, methyl, ethyl or C-C-haloalkyl having 1 to 5 fluorine, chlorine and/or bromine atoms;'}{'sup': '23', 'sub': 1', '2', '1', '2, 'Rrepresents fluorine, chlorine, bromine, cyano, methyl, ethyl, C-C-haloalkyl or C-C-haloalkoxy having in each case 1 to 5 fluorine, chlorine and/or bromine atoms;'}{'sup': 24', '25, 'sub': 1', '2, 'Rand Rindependently of one another represent hydrogen, fluorine, chlorine, bromine, methyl, ethyl or C-C-haloalkyl having 1 to 5 fluorine, chlorine and/or bromine atoms;'}{'sup ...

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23-05-2013 дата публикации

DERIVATIVES OF 1,4-DIHYDROPYRIDINE POSSESSING ANTIVIRAL EFFICACY

Номер: US20130131126A1
Принадлежит: JSC GRINDEKS

2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylic acid ester type compounds having general formula I 112-. (canceled)17. A process for preparing a compound according to claim 13 , comprising the steps of:a) reaction of a derivative of formaldehyde with a derivative of acetoacetic acid ester and enamine in an appropriate solvent;b) treatment with sodium hydroxide in an appropriate solvent.18. The process according to claim 17 , wherein claim 17 , in step a) claim 17 , the derivative of formaldehyde is formaldehyde or glyoxylic acid.19. The process according to claim 17 , wherein claim 17 , in step a) claim 17 , the derivative of acetoacetic acid ester is 2-methoxycarbonyl methyl ester of acetoacetate or 2-ethoxycarbonyl methyl ester of acetoacetate.20. The process according to claim 17 , wherein claim 17 , in step a) claim 17 , the derivative of enamine is methyl-β-aminocrotonate claim 17 , ethyl-β-aminocrotonate or 2-ethoxycarbonyl methyl ester of β-aminocrotonate.21. The process according to claim 17 , wherein claim 17 , in step a) and b) claim 17 , the appropriate solvent is selected from methanol claim 17 , ethanol claim 17 , propanol and butanol.22. A pharmaceutical composition comprising as active ingredient a compound according to claim 13 , optionally together with one or more pharmaceutically acceptable excipients.23. A method of treating a condition requiring an antiviral agent in a subject in need thereof claim 13 , comprising administering an effective amount of a compound according to .24. A method of treating influenza in a subject in need thereof claim 13 , comprising administering an effective amount of a compound according to . The present invention relates to new 2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylic acid ester type compounds having general formula IwhereinNew 2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylic acid ester type compounds with general formula I possessing antiviral activity.Influenza, commonly called “the flu,” is an illness ...

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30-05-2013 дата публикации

4-carboxybenzylamino derivatives as histone deacetylase inhibitors

Номер: US20130137690A1
Принадлежит: Individual

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

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30-05-2013 дата публикации

HISTONE DEMETHYLASE INHIBITORS AND METHODS FOR USING THE SAME

Номер: US20130137720A1
Автор: Wang Xiang, Xu Wenqing

The present invention provides compounds, or derivatives or prodrugs thereof, that comprise a methyllysine mimic, and an α-ketoglutarate mimic that are attached through a linker and methods for using and producing the same. In some embodiments, compounds of the invention are of the formula: M-L-K, or a derivative or a prodrug thereof, wherein M is a methyllysine mimic, L is a linker, and K is an α-ketoglutarate mimic. 1. A compound of the formula: M-L-K , or a derivative or a prodrug thereof , wherein M is a methyllysine mimic , L is a linker , and K is an α-ketoglutarate mimic.3. The compound according to claim 2 , wherein Ris phenyl claim 2 , naphthyl claim 2 , benzyl claim 2 , or naphthylalkyl claim 2 , each of which is optionally substituted claim 2 , or fluorescein.4. The compound according to claim 2 , wherein X is NH.5. The compound according to claim 2 , wherein Y is O.6. The compound according to claim 2 , wherein Z is O.7. The compound according to claim 2 , wherein Ris C-Calkylene.8. The compound according to claim 2 , wherein Rand Rare methylene.9. The compound according to claim 2 , wherein Aris phenylene.10. The compound according to claim 2 , wherein Ris H or methyl.11. The compound according to claim 2 , wherein Ris alkyl or absent.13. The compound according to claim 12 , wherein Ris hydrogen or C-Calkyl.14. The compound according to claim 12 , wherein Xand Xare O.15. The compound according to claim 12 , wherein Yis —OR.16. The compound according to claim 12 , wherein Lis C-Calkylene or C-Calkenylene.17. A method for treating a clinic condition associated with activity of Jumonji C Domain-Containing Histone Demethylase comprising administering to the subject in need of such a treatment a therapeutically effective amount of a compound of .18. The method of claim 17 , wherein the clinical condition is a cancer or a mental retardation.19. A method for treating a clinic condition associated with overexpression of Jumonji C Domain-Containing Histone ...

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30-05-2013 дата публикации

CONFORMATIONALLY RESTRICTED UREA INHIBITORS OF SOLUBLE EPOXIDE HYDROLASE

Номер: US20130137726A1

Inhibitors of the soluble epoxide hydrolase (sEH) are provided that incorporate multiple pharmacophores and are useful in the treatment of diseases. 3. The method in accordance with or , wherein Ris adamantyl.4. The method in accordance with or , wherein Ris cycloheptyl or cyclohexyl.5. The method in accordance with or , wherein L is a —C(O)—.6. The method in accordance with or , wherein Ris selected from the group consisting of hydrogen , C-Calkyl , and arylC-Calkyl.7. The method in accordance with or , wherein Ris C—Calkyl.8. A method in accordance with claim 2 , wherein said compound is selected from the group consisting of:N-(1-acetylpiperidin-4-yl)-N′-(adamant-1-yl)urea;N-(1-propionylpiperidin-4-yl)-N′-(adamant-1-yl)urea;N-(1-butyrylpiperidine-4-yl)-N′-(adamant-1-yl)urea;N-(1-benzoyl piperidin-4-yl)-N′-(adamant-1-yl)urea;4-[4-(3-adamantan-1-yl-ureido)-piperidin-1-yl]-4-oxo-butanoic acid methyl ester;5-[4-(3-adamantan-1-yl-ureido)-piperidin-1-yl]-5-oxo-pentanoic acid methyl ester;2-[4-(3-adamantan-1-yl-ureido)-piperidine-1-carbonyl]-benzoic acid methyl ester;3-[4-(3-adamantan-1-yl-ureido)-piperidine-1-carbonyl]-benzoic acid methyl ester;4-[4-(3-adamantan-1-yl-ureido)-piperidine-1-carbonyl]-benzoic acid methyl ester;1-(1-acetyl-piperidin-4-yl)-3-(4-trifluoromethoxyphenyl)urea;1-(1-trifluoromethylcarbonylpiperidin-4-yl)-3-(4-trifluoromethoxyphenyl)urea; and1-(1-acetyl-piperidin-4-yl)-3-cycloheptyl)urea;or a pharmaceutically acceptable salt thereof.9. The method in accordance with claim 8 , wherein said compound is selected from the group consisting of:N-(1-acetylpiperidin-4-yl)-N′-(adamant-1-yl)urea;N-(1-propionylpiperidin-4-yl)-N′-(adamant-1-yl)urea;N-(1-butyrylpiperidine-4-yl)-N′-(adamant-1-yl)urea; andN-(1-benzoylpiperidin-4-yl)-N′-(adamant-1-yl)ureaor a pharmaceutically acceptable salt thereof.10. The method in accordance with claim 8 , wherein said compound is N-(1-acetylpiperidin-4-yl)-N′-(adamant-1-yl)urea or a pharmaceutically acceptable salt thereof.11. ...

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30-05-2013 дата публикации

Selective serotonin 2a/2c receptor inverse agonists as therapeutics for neurodegenerative diseases

Номер: US20130137727A1
Принадлежит: Acadia Pharmaceuticals Inc

Behavioral pharmacological data with the compound of formula (I), a novel and selective 5HT2A/2C receptor inverse agonist, demonstrate in vivo efficacy in models of psychosis and dyskinesias. This includes activity in reversing MK-801 induced locomotor behaviors, suggesting that this compound may be an efficacious anti-psychotic, and activity in an MPTP primate model of dyskinesias, suggesting efficacy as an anti-dyskinesia agent. These data support the hypothesis that 5HT2A/2C receptor inverse agonism may confer antipsychotic and anti-dyskinetic efficacy in humans, and indicate a use of the compound of formula (I) and related agents as novel therapeutics for Parkinson's Disease, related human neurodegenerative diseases, and psychosis.

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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

ARYL DIHYDROPYRIDINONE AND PIPERIDINONE MGAT2 INHIBITORS

Номер: US20130143843A1
Принадлежит:

The present invention provides compounds of Formula (I): 3. A compound according to claim 2 , wherein:{'sup': 11', '15, 'sub': '1-4', 'Rand Rare independently selected from the group consisting of: H, Calkyl and halo;'}{'sup': 12', '14, 'sub': 1-4', '1-4, 'Rand Rare independently selected from the group consisting of: H, halo, Calkyl and Calkoxy; and'}{'sup': 13', 'i', 'f', 'j', 'j', 'e, 'sub': 1-4', '1-4', '1-4', '1-4', '2', 'm', '3-4', '2', '1-4', '2', '1-4, 'Ris independently selected from the group consisting of: H, halo, Calkyl substituted with 0-1 R, Calkoxy, Chaloalkyl, Chaloalkoxy, —(CH)—Ccycloalkyl, CN, NRR, SR, NHCO(Calkyl), NHSO(Calkyl), and a 4- to 6-membered heterocycle comprising: carbon atoms and 1-4 heteroatoms selected from N, NR, O, and S.'}11. A pharmaceutical composition claim 1 , comprising: a pharmaceutically acceptable carrier and a compound of claim 1 , or a stereoisomer claim 1 , a tautomer claim 1 , or a pharmaceutically acceptable salt thereof.12. A pharmaceutical composition claim 9 , comprising: a pharmaceutically acceptable carrier and a compound of claim 9 , or a stereoisomer claim 9 , a tautomer claim 9 , or a pharmaceutically acceptable salt thereof.13. A pharmaceutical composition claim 10 , comprising: a pharmaceutically acceptable carrier and a compound of any one of claim 10 , or a stereoisomer claim 10 , a tautomer claim 10 , or a pharmaceutically acceptable salt thereof.14. The pharmaceutical composition according to claim 11 , further comprising one or more other suitable therapeutic agents useful in the treatment of the aforementioned disorders including: anti-diabetic agents claim 11 , anti-hyperglycemic agents claim 11 , anti-hyperinsulinemic agents claim 11 , anti-retinopathic agents claim 11 , anti-neuropathic agents claim 11 , anti-nephropathic agents claim 11 , anti-atherosclerotic agents claim 11 , anti-ischemic agents claim 11 , anti-hypertensive agents claim 11 , anti-obesity agents claim 11 , anti-dyslipidemic ...

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06-06-2013 дата публикации

COMPOUNDS AND THEIR USE AS IKACH BLOCKERS

Номер: US20130143858A1
Принадлежит: AstraZeneca AB

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

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06-06-2013 дата публикации

Guanidine compound

Номер: US20130143860A1
Принадлежит: Astellas Pharma Inc

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

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06-06-2013 дата публикации

New piperidine derivatives, pharmaceutical compositions and uses thereof

Номер: US20130143876A1
Принадлежит: Individual

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

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06-06-2013 дата публикации

ACYL PIPERIDINE INHIBITORS OF SOLUBLE EPOXIDE HYDROLASE

Номер: US20130143925A1

Inhibitors of the soluble epoxide hydrolase (sEH) are provided that incorporate multiple pharmacophores and are useful in the treatment of diseases. 125.-. (canceled)26. A pharmaceutical composition comprising a compound of and a pharmaceutically acceptable excipient.27. A method for inhibiting a soluble epoxide hydrolase claim 29 , the method comprising contacting the soluble epoxide hydrolase with an amount of a compound of sufficient to inhibit the soluble epoxide hydrolase.28. A method for monitoring the activity of a soluble epoxide hydrolase claim 29 , the method comprising contacting the soluble epoxide hydrolase with an amount of a compound of sufficient to produce a detectable change in the fluorescence of the soluble epoxide hydrolase by interacting with one or more tryptophan residues present in the catalytic site of said sEH.29. A compound is selected from the group consisting of1-(4-Methoxyphenyl)-3-(1-propionylpiperidin-4-yl)urea,1-(4-Phenoxyphenyl)-3-(1-propionylpiperidin-4-yl)urea,1-(4-Fluorophenyl)-3-(1-propionylpiperidin-4-yl)urea,1-(4-Chlorophenyl)-3-(1-propionylpiperidin-4-yl)urea,1-(4-Iodophenyl)-3-(1-propionylpiperidin-4-yl)urea,1-(3,5-Dichlorophenyl)-3-(1-propionylpiperidin-4-yl)urea,1-(4-Chloro-3-(trifluoromethyl)phenyl)-3-(1-propionylpiperidin-4-yl)urea,1-(4-Perfluoroisopropylphenyl)-3-(1-propionylpiperidin-4-yl)urea,1-(1-cyclopropanecarbonylpiperidin-4-yl)-3-(4-(trifluoromethyl)phenyl)urea,1-(1-(2-methylbutyryl)piperidin-4-yl)-3-(4-(trifluoromethyl)phenyl)urea,1-(1-(3,3,3-trifluoropropionyl)piperidin-4-yl)-3-(4-(trifluoromethyl)phenyl)urea,1-(1-(4,4,4-trifluorobutyryl)piperidin-4-yl)-3-(4-(trifluoromethyl)phenyl)urea,1-(1-Propionylpiperidin-4-yl)-3-(4-(trifluoromethoxy)phenyl)urea,1-(1-(Cyclopropanecarbonyl)piperidin-4-yl)-3-(4-(trifluoromethoxy)phenyl)urea,1-(1-(Trifluoroacetyl)piperidin-4-yl)-3-(4-(trifluoromethoxy)phenyl)urea,1-(1-(propylsulfonyl)piperidin-4-yl)-3-(4-(trifluoromethyl)phenyl)urea,1-(1-(butylsulfonyl)piperidin-4-yl)-3-(4-( ...

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06-06-2013 дата публикации

BENZAMIDE DERIVATIVES AND THEIR USE AS HSP90 INHIBTORS

Номер: US20130143926A1
Принадлежит:

The invention provides a compound which is (a) a phenylamide derivative of formula (I) or a tautomer thereof, or (b) a pharmaceutically acceptable salt, N-oxide, hydrate, prodrug or solvate thereof: wherein R, R, R, R, R, Rand Rare as defined herein. The compounds are useful in the treatment of diseases mediated by HSP90. 2. A compound as claimed in wherein Ris hydroxy.3. A compound as claimed in wherein R claim 1 , R claim 1 , Rand Rare the same or different and represent hydrogen or halogen atoms or hydroxy claim 1 , unsubstituted Calkyl or unsubstituted Calkoxy groups.4. A compound as claimed in wherein either:{'sup': 6', '7', '8', '9', '8', '9, 'sub': 3', '1-4', '1-4, '(i) Rrepresents —CH, Rrepresents —CRR-A wherein Rand Rare the same or different and represent a hydrogen or halogen atom or an unsubstituted Calkyl or Calkoxy group, and A represents a phenyl ring substituted with a group W; or'}{'sup': 6', '7, 'sub': 1-4', '1-4', '1-4', '1-4', '1-4', '1-2, '(ii) Rand R, together with the nitrogen atom to which they are bonded, form a pyrrolidinyl, piperidinyl or isoindolinyl group which is substituted with a group W and is optionally further substituted with 1 or 2 groups which are the same or different and are selected from halogen atoms and unsubstituted Calkyl, Calkoxy, hydroxyl, Chaloalkyl, Chaloalkoxy, Chydroxyalkyl, cyano, nitro, —SR′ and —NR′R″ groups where R′ and R″ are the same or different and represent hydrogen or unsubstituted Calkyl.'}5. A compound as claimed in wherein Alkrepresents a bond claim 1 , an unsubstituted Calkylene group claim 1 , or an unsubstituted —(Calkylene)-NH—(Calkylene)- group.6. A compound as claimed in wherein either:{'sup': 12', '13, 'sub': 1-6', '3-7', '6-10', '1-4', '6-10', '1-4', '3-7, '(i) Rand Rare the same or different and represent hydrogen, Calkyl, Ccarbocyclyl, Caryl, —(Calkyl)-(Caryl), or —(Calkyl)-(Ccarbocyclyl); or'}{'sup': 12', '13, 'sub': '3-7', '(ii) Rand R, together with the carbon atom to which they are bonded, ...

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06-06-2013 дата публикации

OPTICAL ENANTIOMERS OF PHENYRAMIDOL AND PROCESS FOR CHIRAL SYNTHESIS

Номер: US20130143932A1
Принадлежит: FERMENTA BIOTECH (UK) LIMITED

The present invention discloses optically pure (R) and (S) Phenyramidol enantiomers and their pharmaceutically acceptable salts, a process for synthesizing such enantiomers by means of a styrene oxide based synthesis, and also a clinical evaluation of (R) and (S) enantiomers of Phenyramidol, their salts and compositions thereof for enhanced/newer therapeutic benefits. 2. The enantiomer of claim 1 , wherein the enantiomer has an optical purity of at least 99%.3. A pharmaceutical composition comprising the enantiomer or its pharmaceutically acceptable salt thereof of .4. A method of using the pharmaceutical composition of as an analgesic or anti-arthritic agent for treating a subject in need of such an agent claim 3 , comprising administering said agent to the subject.5. (canceled)6. The method of wherein the composition comprises an (R) enantiomer or a pharmaceutically acceptable salt thereof as an analgesic.7. The method of wherein the composition comprises an oxalate salt of the enantiomer as an anti-arthritic agent.8. A process of producing (R) or (S) Phenyramidol claim 4 , or a pharmaceutically acceptable salt thereof claim 4 , comprising the steps of:(a) contacting 2-aminopyridine with an alkali metal amide in an organic solvent to obtain an alkali metal salt of 2-aminopyridine; and(b) condensing the alkali metal salt of 2-aminopyridine with (R) or (S) styrene oxide to produce a free base of (R) or (S) Phenyramidol, respectively, wherein the (R) or (S) Phenyramidol, or a pharmaceutically acceptable salt thereof, is produced from said free base.9. The process of claim 8 , wherein said alkali metal amide is selected from the group consisting of sodium amide claim 8 , potassium amide and lithium amide.10. The process of claim 8 , wherein the molar ratio of 2-aminopyridine to alkali metal amide is from 1:1 to 1:1.5.11. The process of claim 8 , wherein the organic solvent is selected from the group consisting of N-methyl-2-pyrrolidone (NMP) claim 8 , tetrahydrofuran ...

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13-06-2013 дата публикации

CARBOXAMIDE COMPOUNDS AND THEIR USE AS CALPAIN INHIBITORS

Номер: US20130150367A1
Принадлежит:

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

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13-06-2013 дата публикации

HYDROBROMIDE SALT OF PRIDOPIDINE

Номер: US20130150406A1
Принадлежит: IVAX INTERNATIONAL GMBH

This invention relates to a new salt of Pridopidine, a drug substance currently in development for the treatment of Huntington's disease. More specifically the invention provides the pharmaceutically acceptable hydrobromide salt, pharmaceutical compositions comprising this salt, and uses of this salt as a drug substance. 1. A hydrobromide salt of 4-(3-methanesulfonyl-phenyl)-1-propyl-piperidine (Pridopidine).2. The hydrobromide salt of provided in an anhydrous form.3. The hydrobromide salt of provided in an anhydrous form and non-solvated form.4. The hydrobromide salt of provided in an anhydrous form which is in a substantially crystalline form.5. The hydrobromide salt of having an X-ray powder diffraction pattern with reflections corresponding to the d-spacing values 6.0 and 3.8.6. The hydrobromide salt of having an X-ray powder diffraction pattern with reflections corresponding to the d-spacing values 3.6 and 4.0.7. The hydrobromide salt of having an X-ray powder diffraction pattern with reflections corresponding to the d-spacing values 7.6 claim 1 , 6.9 claim 1 , 6.0 claim 1 , 5.4 claim 1 , 4.3 claim 1 , 4.2 claim 1 , 4.0 claim 1 , 3.8 claim 1 , 3.6 claim 1 , 3.1.8. The hydrobromide salt of having an x-ray powder diffraction pattern with reflections corresponding to the d-spacing values 10.8 claim 1 , 7.6 claim 1 , 6.9 claim 1 , 6.0 claim 1 , 5.7 claim 1 , 5.4 claim 1 , 5.3 claim 1 , 5.2 claim 1 , 4.7 claim 1 , 4.6 claim 1 , 4.3 claim 1 , 4.2 claim 1 , 4.0 claim 1 , 3.8 claim 1 , 3.7 claim 1 , 3.6 claim 1 , 3.5 claim 1 , 3.4 claim 1 , 3.3 claim 1 , 3.2 claim 1 , 3.1.9. The hydrobromide salt of characterized by having an endotherm with an onset of about 196° C. claim 1 , as obtained with DSC.10. The hydrobromide salt of characterized by having an IR spectrum with absorptions at about 2950 cm-1 claim 1 , 2700-2500 cm-1 claim 1 , 1550 cm-1 claim 1 , 1450 cm-1 claim 1 , 1300 cm-1 claim 1 , 1150 cm-1 claim 1 , 1100 cm-1 claim 1 , 950 cm-1 claim 1 , 900 cm-1 claim 1 , ...

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13-06-2013 дата публикации

PIPERIDINYL NAPHTHYLACETIC ACIDS

Номер: US20130150407A1
Принадлежит: Hoffmann-La Roche Inc.

The invention is concerned with the compounds of formula (I): 2. The compound according to claim 1 , wherein X is —SO—.3. The compound according to claim 1 , wherein X is —C(O)—.4. The compound according to claim 1 , wherein Ris fluorine.5. The compound according to claim 1 , wherein X is —SO— and Ris phenyl claim 1 , unsubstituted or mono- or bi-substituted independently with lower alkyl claim 1 , halogen claim 1 , alkoxy claim 1 , —SO-lower alkyl or —CF; unsubstituted heteroaryl; or lower alkyl claim 1 , unsubstituted or substituted with unsubstituted phenyl or phenyl substituted with halogen claim 1 , NOor NH.6. The compound according to claim 1 , wherein X is —SO— and Ris unsubstituted cycloalkyl; unsubstituted heterocycloalkyl; or NH-phenyl claim 1 , said phenyl being unsubstituted or substituted with halogen claim 1 , lower alkyl claim 1 , haloalkyl claim 1 , —SO-lower alkyl or alkoxy.7. The compound according to claim 1 , wherein Ris phenyl claim 1 , methylphenyl claim 1 , chlorophenyl claim 1 , methanesulfonylphenyl claim 1 , dichlorophenyl claim 1 , difluorophenyl claim 1 , trifluoromethylphenyl claim 1 , bis-trifluoromethylphenyl claim 1 , methoxyphenyl claim 1 , nitrophenyl or aminophenyl.8. The compound according to claim 1 , wherein Ris pyridinyl.9. The compound according to claim 1 , wherein Ris methyl or methyl substituted with phenyl claim 1 , chlorophenyl claim 1 , nitrophenyl or aminophenyl.10. The compound according to claim 1 , wherein Ris cyclopentyl.11. The compound according to claim 1 , wherein Ris pyrrolidinyl.12. The compound according to claim 1 , wherein Ris —NH-difluorophenyl claim 1 , —NH-dichlorophenyl claim 1 , —NH-chlorophenyl claim 1 , —NH-phenylmethoxy or —NH-trifluoromethylphenyl.13. The compound according to claim 1 , wherein Ris methyl.14. The compound according to claim 1 , wherein Ris hydrogen.15. The compound according to claim 1 , wherein said compound is:[4-(1-Benzenesulfonyl-piperidin-4-yl)-6-fluoro-naphthalen-2-yl]-acetic ...

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20-06-2013 дата публикации

PIPERIDINE DERIVATIVES

Номер: US20130158050A1
Принадлежит: Hoffmann-La Roche Inc.

The present invention relates to a compound of formula I 2. A compound of claim 1 , wherein Ris lower alkyl.3. A compound of claim 2 , wherein the phenyl group for Ar is substituted by at least two CFgroups.4. A compound of claim 3 , selected from the group consisting ofrac-2-fluoro-N-(1-methyl-3-phenyl-piperidin-3-yl)-4,6-bis-trifluoromethyl-benzamide;rac-2-methoxy-N-(1-methyl-3-phenyl-piperidin-3-yl)-4,6-bis-trifluoromethyl-benzamide;rac-2-ethyl-N-(1-methyl-3-phenyl-piperidin-3-yl)-4,6-bis-trifluoromethyl-benzamide;rac-N-[3-(4-fluoro-phenyl)-1-methyl-piperidin-3-yl]-2-methoxy-4,6-bis-trifluoromethyl-benzamide; and2-methoxy-N—((R)-1-methyl-3-phenyl-piperidin-3-yl)-4,6-bis-trifluoromethyl-benzamide.5. A compound of claim 1 , wherein the phenyl group for Ar is substituted by at least one CFgroup.6. A compound of claim 5 , selected from the group consisting ofrac-2-ethyl-N-(1-methyl-3-phenyl-piperidin-3-yl)-4-trifluoromethyl-benzamide;rac-2-bromo-6-methoxy-N-(1-methyl-3-phenyl-piperidin-3-yl)-4-trifluoromethyl-benzamide;rac-N-(1,2-dimethyl-3-phenyl-piperidin-3-yl)-2-methoxy-6-methylsulfanyl-4-trifluoromethyl-benzamide;rac-2-cyclopropyl-N-(1-methyl-3-phenyl-piperidin-3-yl)-4-trifluoromethyl-benzamide;rac-2-methoxy-N-(1-methyl-3-phenyl-piperidin-3-yl)-6-methylsulfanyl-4-trifluoromethyl-benzamide;rac-N-(1-methyl-3-phenyl-piperidin-3-yl)-2-methylsulfanyl-4-trifluoromethyl-benzamide;rac-N-[3-(4-fluoro-phenyl)-1-methyl-piperidin-3-yl]-2-methoxy-6-methylsulfanyl-4-trifluoromethyl-benzamide;rac-N-[3-(4-chloro-phenyl)-1-methyl-piperidin-3-yl]-2-methoxy-6-methylsulfanyl-4-trifluoromethyl-benzamide;2-methoxy-N-((S)-1-methyl-3-phenyl-piperidin-3-yl)-6-methylsulfanyl-4-trifluoromethyl-benzamide;2-methoxy-N—((R)-1-methyl-3-phenyl-piperidin-3-yl)-6-methylsulfanyl-4-trifluoromethyl-benzamide; andrac-2-difluoromethoxy-N-(1-methyl-3-phenyl-piperidin-3-yl)-4-trifluoromethyl-benzamide.7. A compound of claim 5 , selected from the group consisting ofrac-N-[3-(3-chloro-phenyl)-1-methyl- ...

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27-06-2013 дата публикации

HEXAFLUOROISOPROPYL CARBAMATE DERIVATIVES, THEIR PREPARATION AND THEIR THERAPEUTIC APPLICATION

Номер: US20130165422A1
Принадлежит: SANOFI

The disclosure relates to hexafluoroisopropyl carbamate derivatives of general formula (I): 2. The compound of formula (I) according to claim 1 , wherein:{'sup': '1', 'Rrepresents a phenyl, naphthyl, indanyl, benzoxazole, benzisoxazole, benzimidazole, benzotriazole, oxadiazole, indazole, isoxazole, pyridine, pyrazine, pyrimidine, thienyl, thiazole, benzothiophene, indole, dihydrobenzodioxane, benzothiadiazole, pyrazole, dihydrobenzoxazine or indoline group;'}{'sup': '2', 'sub': 3', '3', '2', '2', '2', '2', '2, 'Rrepresents one or more groups chosen from a halogen atom or a methyl, trifluoromethyl, methoxy, trifluoromethoxy, cyano, oxo, CHNHCO, CHSO, NHCO, NHSOand pyrrolidine-SOgroup;'}{'sup': '3', 'Rrepresents a group chosen from a phenyl and an oxazole; and also the compound 2,2,2-trifluoro-1-(trifluoromethyl)ethyl 4-{[3-(2-methylpyrimidin-4-yl)benzenesulphonylamino]methyl}piperidine-1-carboxylate,'}in the form of the base or of an addition salt with an acid.3. The compound of formula (I) according to claim 1 , wherein:{'sub': 2', '2', '2', '2', '3', '2, 'Z represents a bond or a CH, (CH), CH═CH, C≡C, OCHor OC(CH)group,'}in the form of the base or of an addition salt with an acid.4. The compound of formula (I) according to claim 1 , wherein:{'sub': 2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '3', '2', '2', '2', '3', '2', '2', '2', '3', '2, 'A represents a bond, an oxygen atom, a sulphur atom, an OCHgroup, an O—(CH)group, an NH, NHCHor NH(CH)group, an SOor CO group, a CONH group, a CONHCHor CONH(CH)group, an SONH group, an SONHCHor SONH(CH)group, an SONHCO, SONHCONH or SONHCONHCHgroup, an OCONH group, an NHCONH group, an NHCONHCHgroup, an N(CH)CONHCH, NHCONH(CH)or N(CH)CONH(CH)group or an SON(CH)CHgroup,'}in the form of the base or of an addition salt with an acid.5. The compound of formula (I) according claim 1 , wherein m and n represent 1 claim 1 , in the form of the base or of an addition salt with an ...

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27-06-2013 дата публикации

PROSTAGLANDIN D SYNTHASE INHIBITORY PIPERIDINE COMPOUNDS

Номер: US20130165438A1
Принадлежит: TAIHO PHARMACEUTICAL CO., LTD.

The present invention provides a piperidine compound represented by Formula (I) 2. The piperidine compound or a salt thereof according to wherein{'sup': 1', '2', '3, 'Xis nitrogen, and Xand Xare the same or different and each represents CH; or'}{'sup': 1', '3', '1', '2, 'Xand Xare the same or different and each represents C—R, and Xis CH; and'}{'sup': '1', 'Ris halogen.'}3. A pharmaceutical composition comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'an effective amount of at least one of the compounds according to or a pharmaceutically acceptable salt thereof, and'}a pharmaceutically acceptable carrier.4. A prostaglandin D synthase inhibitor comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'an effective amount of the compound according to or a pharmaceutically acceptable salt thereof, and'}a pharmaceutically acceptable carrier.5. An agent for preventing or treating a disease in which prostaglandin D2 or a metabolite thereof participates claim 1 , the agent comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'an effective amount of the compound according to or a pharmaceutically acceptable salt thereof, and'}a pharmaceutically acceptable carrier.6. The agent according to claim 5 , wherein the disease in which prostaglandin D2 or a metabolite thereof participates is an allergic disease or an inflammatory disease.7. A method for preventing or treating a disease in which prostaglandin D2 or a metabolite thereof participates claim 1 , comprising administering claim 1 , to a mammal claim 1 , the compound or a salt thereof according to in an amount effective for preventing or treating the disease.8. Use of the compound or a salt thereof according to for producing an agent for preventing or treating a disease in which prostaglandin D2 or a metabolite thereof participates.9. The compound or a salt thereof according to for use in a method for preventing or treating a disease in which prostaglandin D2 or a metabolite thereof participates. The ...

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27-06-2013 дата публикации

Piperidine Derivatives

Номер: US20130165444A1
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

Piperidine derivatives of which the following is exemplary and their use in the treatment of obesity, diabetes or dyslipidemia.

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27-06-2013 дата публикации

PEST CONTROL AGENT

Номер: US20130165482A1
Принадлежит: MEIJI SEIKA PHARMA CO., LTD.

Specific amine derivatives have been found to possess excellent activities as pest control agents. 124-. (canceled)26. The amine derivative or a salt thereof according to claim 25 , wherein Y in formula (Ie′) is a hydrogen atom or a halogen atom.27. The amine derivative or a salt thereof according to claim 25 , wherein the compound of formula (Ie′) is a compound selected from the group consisting of N-[1-((6-chloropyridin-3-yl)methyl)pyridin-2(1H)-ylidene]-2 claim 25 ,2 claim 25 ,2-trifluoroacetamide claim 25 , N-[1-((6-chloro-5-fluoropyridin-3-yl)methyl)pyridin-2(1H)-ylidine]-2 claim 25 ,2 claim 25 ,2-trifluoroacetamide claim 25 , N-[1-((6-fluoropyridin-3-yl)methyl)pyridin-2(1H)-ylidene]-2 claim 25 ,2 claim 25 ,2-trifluoroacetamide claim 25 , N-[1-((6-bromopyridin-3-yl)methyl)pyridin-2(1H)-ylidene]-2 claim 25 ,2 claim 25 ,2-trifluoroacetamide claim 25 , N-[1-(1-(6-chloropyridin-3-yl)ethyl)pyridin-2(1H)-ylidene]-2 claim 25 ,2 claim 25 ,2-trifluoroacetamide claim 25 , N-[1-((6-chloropyridin-3-yl)methyl)pyridin-2(1H)-ylidene]-2 claim 25 ,2-difluoroacetamide claim 25 , 2-chloro-N-[1-((6-chloropyridin-3-yl)methyl)pyridin-2(1H)-ylidene]-2 claim 25 ,2-difluoroacetamide claim 25 , N-[1-((2-chloropyrimidin-5-yl)methyl)pyridin-2(1H)-ylidene]-2 claim 25 ,2 claim 25 ,2-trifluoroacetamide and N-[1-((6-chloropyridin-3-yl)methyl)pyridin-2(1H)-ylidene]-2 claim 25 ,2 claim 25 ,3 claim 25 ,3 claim 25 ,3-pentafluoropropanamide.28. The amine derivative or a salt thereof according to claim 25 , which has a pest control activity on at least one type of pest selected from the group consisting of lepidopterous pests claim 25 , hemipterous pests claim 25 , thysanopterous pests claim 25 , dipterous pests claim 25 , coleopterous pests claim 25 , animal parasitic fleas and ticks claim 25 , and canine heartworms.29. A pest control agent comprising at least one amine derivative or a salt thereof according to .32. The method according to or claim 25 , wherein the pest is an agricultural/ ...

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27-06-2013 дата публикации

RUTHENIUM COMPLEXES FOR USE IN OLEFIN METATHESIS

Номер: US20130165649A1
Автор: Cazin Catherine
Принадлежит:

Cls ruthenium complexes that can be used as catalysts are described. The complexes are generally square pyramidal in nature, having two anionic ligands X adjacent to each other. The complexes can be used as catalysts, for example in olefin metathesis reactions. Corresponding trans ruthenium complexes are also described, together with cationic complexes where one or both of the anionic ligands X are replaced by a non-co-ordinating anionic ligand. 2. The cis ruthenium complex according to wherein the anionic ligands X are independently selected from the group consisting of halogen claim 1 , benzoate claim 1 , C-Ccarboxylates claim 1 , C-Calkoxy claim 1 , phenoxy claim 1 , C-Calkyl thio groups claim 1 , tosylate claim 1 , mesylate claim 1 , brosylate claim 1 , trifluoromethane sulfonate claim 1 , and pseudo-halogens.3. The cis ruthenium complex according to wherein the groups Rand Rare H and aryl.4. The cis ruthenium complex according to wherein the groups Rand Rare fused to form a substituted or unsubstituted indenylidene moiety.6. The cis ruthenium complex according to wherein the phosphite group is selected from the group consisting of P(OMe)P(OEt) claim 5 , P(OiPr)and P(OPh).7. The cis ruthenium complex according to wherein the group A is a nucleophilic carbene having a four claim 1 , five claim 1 , six or seven membered ring containing the carbene carbon.8. The cis ruthenium complex according to wherein the group A is an N-heterocyclic carbene.9. The cis ruthenium complex according to wherein the N-heterocyclic carbene ligand contains more than one nitrogen atom in the ring and/or contains at least one of O or S in the ring.11. The cis ruthenium complex according to wherein the N-heterocyclic carbene ligand contains two nitrogen atoms in the ring claim 9 , each adjacent the carbene carbon.18. The method of wherein the leaving group L is selected from the group cnsisting of; substituted or unsubstituted pyridine claim 17 , phosphine claim 17 , phosphite claim 17 , ...

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27-06-2013 дата публикации

PROCESS FOR THE PREPARATION OF IODIDES

Номер: US20130165658A1
Принадлежит:

This invention is directed to a process for the preparation of high yield alkyl or aryl iodide from its corresponding carboxylic acid using N-iodo amides. 1. A process for the preparation of iodide , represented by scheme (1):{'br': None, 'R—COOH→R—I\u2003\u2003(1)'}comprising reacting R—COOH with N-iodo amide to yield R—I; wherein R is saturated, linear or branched, substituted or unsubstituted alkyl; substituted or unsubstituted aryl; saturated or unsaturated, substituted or unsubstituted mono- or poly-carbocyclic or heterocyclic ring.2. The process of claim 1 , wherein said amide is carboxamide or sulfonamide.3. The process of claim 1 , wherein said amide is lactame claim 1 , carbamate claim 1 , imide or ureide.4. The process of claim 1 , wherein said amide is 5 claim 1 ,5-dimethylhydantoin claim 1 , 3-benzyl-5 claim 1 ,5-dimethylhydantoin claim 1 , 5-methyl-5-phenylhydantoin claim 1 , 5 claim 1 ,5-diphenylhydantoin claim 1 , 5 claim 1 ,5-hexamethylenehydantoin claim 1 , 5 claim 1 ,5-pentamethylenehydantoin claim 1 , 5 claim 1 ,5-tetramethylenehydantoin claim 1 , succinimide claim 1 , phthalimide claim 1 , saccharine claim 1 , isocyanuric acid claim 1 , 5 claim 1 ,5-dimethylbarbituric acid claim 1 ,-glycoluril claim 1 , 3a claim 1 ,6a-diphenylglycoluril claim 1 , 3a claim 1 ,6a-dimethylglycoluril claim 1 , 4 claim 1 ,4 claim 1 ,5 claim 1 ,5-tetramethyl-2-imidazolidinone claim 1 , 4 claim 1 ,4-dimethyl-2-oxazolidinone or mixture thereof.5. The process of claim 1 , wherein said N-iodo amide is 1 claim 1 ,3-diiodo-5 claim 1 ,5-dimethylhydantoin (DIH) claim 1 , N-iodosuccinimide (NIS) claim 1 , triiodoisocyanuric acid (TICA) claim 1 , 2 claim 1 ,4 claim 1 ,6 claim 1 ,8-tetraiodoglycoluril (TIG) claim 1 , N-iodosaccharine (NISac) claim 1 , or mixture thereof.6. The process of claim 1 , which comprises subjecting the mixture of the R—COOH and N-iodoamide to heat claim 1 , ultrasound claim 1 , or electromagnetic radiation or combination thereof.7. The process of claim 1 ...

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27-06-2013 дата публикации

PRODUCTION METHOD OF INTERMEDIATE COMPOUND FOR SYNTHESIZING MEDICAMENT

Номер: US20130165659A1
Принадлежит: LG LIFE SCIENCES LTD.

The present invention relates to a novel method for preparing a compound of formula (2) as the intermediate, which can be effectively used for preparation of a compound of formula (1) exhibiting good inhibitory activity against dipeptidyl peptidase IV enzyme. 3. The method according to claim 1 , wherein Pis t-butyl group claim 1 , and Pis methyl or ethyl group.4. The method according to claim 1 , wherein GO is triflate claim 1 , mesylate claim 1 , tosylate claim 1 , besylate or nonaflate.5. The method according to claim 1 , wherein R3 and R4 are hydrogen claim 1 , and R5 and R6 are fluorine.6. The method according to claim 2 , wherein in step (a) C-Ctrialkylamine is used as the base.7. The method according to claim 2 , wherein in step (b) acetic acid is used as the acid.8. The method according to claim 2 , wherein in the case of the compound of formula (2a) wherein Pis Boc and Pis t-butyl claim 2 , the hydrolysis of said step (c) is conducted under the basic condition to selectively remove only Pamong the protecting groups Pand Pto provide the compound of formula (2).9. The method according to claim 8 , wherein aqueous sodium hydroxide solution is used as the base.11. The method according to claim 10 , wherein in step (a) the reduction is conducted using NaBH.12. The method according to claim 10 , wherein in step (b) the Gcompound is selected from the group consisting of trifluoromethane sulfonic acid anhydride (TfO) claim 10 , trifluoromethane sulfonyl chloride (TfCl) claim 10 , methanesulfonyl chloride (MsCl) claim 10 , toluenesulfonyl chloride (TsCl) claim 10 , bromobenzenesulfonyl chloride (BsCl) claim 10 , (CF(CF)SO)F and (CF(CF)SO)O.14. The method according to claim 13 , wherein Pis Boc claim 13 , Pis i-propyl group or t-butyl group claim 13 , and GO is triflate or nonaflate.17. The method according to claim 16 , wherein Pis Boc claim 16 , and Pis i-propyl or t-butyl.18. The method according to claim 16 , wherein in step (a) chloroformate or BocO is used as ...

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04-07-2013 дата публикации

BIPHENYL COMPOUNDS USEFUL AS MUSCARINIC RECEPTOR ANTAGONISTS

Номер: US20130172301A1
Принадлежит: THERAVANCE, INC.

This invention provides compounds of formula I: 214-. (canceled)15. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and the compound of .16. The pharmaceutical composition of claim 15 , wherein the composition further comprises an agent selected from βadrenergic receptor agonists claim 15 , steroidal anti-inflammatory agents claim 15 , phosphodiesterase-4 inhibitors claim 15 , and combinations thereof.17. The pharmaceutical composition of claim 16 , wherein the composition comprises a βadrenergic receptor agonist and a steroidal anti-inflammatory agent.1823-. (canceled)24. A method for treating a pulmonary disorder claim 1 , the method comprising administering to a patient a therapeutically effective amount of the compound of .25. A method of producing bronchodilation in a patient claim 1 , the method comprising administering to a patient a bronchodilation-producing amount of the compound of .26. A method of treating chronic obstructive pulmonary disease or asthma claim 1 , the method comprising administering to a patient a therapeutically effective amount of the compound of . This application claims the benefit of U.S. Provisional Application No. 60/552,443, filed on Mar. 11, 2004; the entire disclosure of which is incorporated herein by reference in its entirety.1. Field of the InventionThe present invention relates to novel biphenyl compounds having muscarinic receptor antagonist or anticholinergic activity. This invention also relates to pharmaceutical compositions comprising such biphenyl compounds, processes and intermediates for preparing such biphenyl compounds and methods of using such biphenyl compounds to treat pulmonary disorders.2. State of the ArtPulmonary or respiratory disorders, such as chronic obstructive pulmonary disease (COPD) and asthma, afflict many millions of people worldwide and such disorders are a leading cause of morbidity and mortality.Muscarinic receptor antagonists are known to provide bronchoprotective ...

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04-07-2013 дата публикации

SUBSTITUTED ANILINES AS CCR(4) ANTAGONISTS

Номер: US20130172315A1
Принадлежит: ChemoCentryx, Inc.

Aniline compounds are provided which bind to CCR(4) and are useful for the treatment of diseases such as allergic diseases, autoimmune diseases, graft rejection and cancer. 2. A compound of claim 1 , wherein X and Y are not both N.3. A compound of claim 1 , wherein Ris H claim 1 , and each Ris a member independently selected from the group consisting of Calkyl claim 1 , Chaloalkyl claim 1 , halogen and —CN.5. A compound of claim 4 , wherein X is C or CH.8. A compound of claim 7 , wherein n is 1 claim 7 , and Ris hydrogen or methyl.10. A compound of claim 9 , wherein n is 1 claim 9 , and Ris hydrogen or methyl.12. A compound of claim 11 , wherein n is 1 claim 11 , and Ris hydrogen or methyl.14. A compound of claim 1 , wherein B is C(O).15. A compound of claim 1 , wherein the ring having Z as a ring vertex is selected from the group consisting of pyrrolidine and piperidine.16. A compound of claim 1 , wherein the ring having Z as a ring vertex is selected from the group consisting of pyrrolidin-2-yl and piperidin-2-yl claim 1 , and at least one of R claim 1 , Rand Ris other than hydrogen.17. A compound of claim 1 , wherein B is a bond.18. A compound of claim 1 , wherein B is a bond and the ring having Z as a ring vertex is selected from the group consisting of pyrrolidine claim 1 , piperidine and cyclohexane.19. A compound of claim 1 , wherein B is a bond and the ring having Z as a ring vertex is selected from the group consisting of pyrrolidin-1-yl claim 1 , pyrrolidin-2-yl claim 1 , piperidin-1-yl claim 1 , piperidin-2-yl claim 1 , piperidin-3-yl and cyclohexane.20. A compound of claim 1 , wherein B is a bond and the ring having Z as a ring vertex is selected from the group consisting of pyrrolidin-1-yl claim 1 , pyrrolidin-2-yl claim 1 , piperidin-1-yl claim 1 , piperidin-2-yl claim 1 , piperidin-3-yl and cyclohexane; and at least one of R claim 1 , Rand Ris other than hydrogen.21. A compound of claim 1 , wherein Z is CH or N.23. A pharmaceutical composition ...

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04-07-2013 дата публикации

ANTI-INFLAMMATORY AGENTS

Номер: US20130172318A1
Принадлежит:

Disclosed herein are methods of preventing or treating inflammatory diseases using 3-aminolactam compounds, each with aromatic “tail groups”. Compounds as defined by formulae (I) and (I′), and the medical uses of the compounds, are described herein. 3. (canceled)4. (canceled)6. A compound of{'claim-ref': {'@idref': 'CLM-00002', 'claim 2'}, ','}provided that the compound is not selected from the group consisting of: (S)-3-(4′-methoxybenzoylamino)-caprolactam, (S)-3-(4′-methylbenzoylamino)-caprolactam, (S)-3-(3′-trifluoromethylbenzoylamino)-caprolactam, (S)-3-(2′-carboxybenzoyl-amino)-caprolactam, and (S)-3-(3′,4′,5′-trimethoxybenzoylamino)-caprolactam.7. A pharmaceutical composition comprising claim 5 , as active ingredient claim 5 , a compound as defined in claim 5 , or a pharmaceutically acceptable salt thereof claim 5 , and at least one pharmaceutically acceptable excipient and/or carrier.8. The compound according to claim 1 , wherein n=2.9. The compound according to claim 1 , wherein n=3.10. The compound according to claim 1 , wherein X is haloalkyl.11. The compound according to claim 2 , wherein the compound is selected from the group consisting of:(S)-3-(4′-methylbenzoylamino)-caprolactam, and(S)-3-(3′,5′-dimethylbenzoylamino)-caprolactam,and pharmaceutically acceptable salts thereof.12. A compound according to claim 2 , selected from the group consisting of:(S)-3-fluoro-N-(2-oxopiperidin-3-yl)benzamide,(S)-2-fluoro-N-(2-oxopiperidin-3-yl)benzamide,(S)-4-fluoro-N-(2-oxopiperidin-3-yl)benzamide,(S)—N-(2-oxopiperidin-3-yl)-4-(trifluoromethyl)benzamide,(S)—N-(2-oxopiperidin-3-yl)-3-(trifluoromethyl)benzamide,(S)—N-(2-oxopiperidin-3-yl)-2-(trifluoromethyl)benzamide,(S)-2,3-difluoro-N-(2-oxopiperidin-3-yl)benzamide,(S)-2,4-difluoro-N-(2-oxopiperidin-3-yl)benzamide,(S)-2,5-difluoro-N-(2-oxopiperidin-3-yl)benzamide,(S)-2,6-difluoro-N-(2-oxopiperidin-3-yl)benzamide,(S)-3,4-difluoro-N-(2-oxopiperidin-3-yl)benzamide,(S)-3,5-difluoro-N-(2-oxopiperidin-3-yl)benzamide,(S)-3 ...

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04-07-2013 дата публикации

Alpha-AminoCycloLactam Ligands for G-Protein Coupled Receptors, and Methods of Using Same

Номер: US20130172319A1
Принадлежит:

The invention relates to the generation of a library of compounds enriched in agonist and antagonists for members of the G-protein coupled class of receptors (GPCRs). 4. A library composed of claim 1 , or enriched in claim 1 , library elements which are compounds according to .5. A method of screening in an assay claim 4 , a library according to claim 4 , to identify agent(s) which modulate signalling through GPCRs.6. The method according to claim 5 , wherein the agent(s) identified are antagonists at one or more GPCRs.7. The method according to claim 5 , wherein the agent(s) identified are agonists at one or more GPCRs.8. The method according to claim 5 , wherein the GPCR is selected from the group consisting of adrenalin receptors claim 5 , endothelin receptors claim 5 , chemokine receptors claim 5 , EDG receptors claim 5 , VIP/PECAP receptors claim 5 , dopamine receptors claim 5 , serotonin receptors claim 5 , purine receptors claim 5 , metabotropic glutamate receptors claim 5 , acetyl choline receptors claim 5 , C5a receptors claim 5 , fMLP receptors claim 5 , glucagon or GLP receptors claim 5 , NPY receptors claim 5 , MSH receptors claim 5 , glycoprotein hormone receptors claim 5 , protease activated receptors (PARs) claim 5 , somatostatin receptors claim 5 , angiotensin receptors claim 5 , cholecystokinin receptors claim 5 , and melatonin receptors. This application is a continuation of application Ser. No. 13/193,274, now U.S. Pat. No. 8,389,279, which is a continuation of application Ser. No. 11/574,656, now U.S. Pat. No. 8,008,289, which is the U.S. national stage of PCT/GB2005/003134, filed Aug. 10, 2005 and published in English as WO 2006/024815 A1 on Mar. 9, 2006, which claims the benefit of priority under 35 U.S.C. §119 to United Kingdom application serial no. 0419517.8, filed Sep. 2, 2004, all of which applications and publications are incorporated herein by reference.The invention relates to the generation of a library of compounds enriched in agonist ...

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04-07-2013 дата публикации

C5ar antagonists

Номер: US20130172347A1
Принадлежит: Individual

Compounds are provided that are modulators of the C5a receptor. The compounds are substituted piperidines and are useful in pharmaceutical compositions, methods for the treatment of diseases and disorders involving the pathologic activation of C5a receptors.

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04-07-2013 дата публикации

ANTHELMINTICS FOR PREVENTING PARASITIC INFECTIONS IN HUMANS AND ANIMALS

Номер: US20130172385A1
Принадлежит: LANXESS DEUTSCHLAND GMBH

The present invention relates to compositions comprising certain active compounds which are suitable as repellents, and to their use for preventing an infection of humans or of animals by the infectious states of parasitic flatworms (platyhelminths). 2. Compositions for deterring helmintic parasites according to claim 1 , characterized in that they comprise at least one compound of the formula (I) in which{'sub': 1', '6, 'Y represents hydrogen, C-C-alkyl or the radical O—X,'}{'sup': 11', '13, 'X represents hydrogen, CORor R,'}{'sup': '1', 'sub': 3', '7', '3', '7', '1', '2', '3', '7', '1', '2', '3', '7', '1', '6', '1', '6, 'Rrepresents C-C-cycloalkyl, C-C-cycloalkenyl, C-C-alkyl-C-C-cycloalkyl, C-C-alkyl-C-C-cycloalkenyl, where the cycloalkyl or cycloalkenyl rings of the abovementioned radicals are optionally substituted up to three times by C-C-alkyl or by a C-C-dialkylene bridge, or'}{'sup': '1', 'sub': 1', '7', '2', 'r', '2', 'r, 'Rrepresents C-C-alkyl, C-Calkenyl or C-Calkinyl,'}{'sup': 2', '11', '13, 'sub': 1', '6, 'R, R, Rare identical or different and represent C-C-alkyl,'}{'sup': 3', '8', '2', '3', '3', '7', '3', '5', '5', '7, 'sub': 1', '6, 'Rto Rare identical or different and represent hydrogen or C-C-alkyl, where Rand Ror Rand Ror Rand Ror Rand Rtogether with the atoms to which they are attached may also form a 5- or 6- membered monocyclic ring and'}n represents 1 and m represents 0.4. (canceled)5. Process for preparing compositions for deterring helminthic parasites claim 1 , characterized in that compounds of the formula (I) according to are mixed with extenders and/or surfactants.7. The method according to claim 3 , wherein the effective amount is 0.03 to 1 mg of compounds according to formula (I) per cmof skin. This application is a continuation of U.S. patent application Ser. No. 10/311,41 8 filed Jun. 12, 2003, incorporated herein by reference.The present invention relates to compositions comprising certain active compounds which are suitable as ...

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