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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 226376. Отображено 100.
05-01-2012 дата публикации

Modulators of cytokine mediated signalling pathways and integrin alphavbeta3 receptor antagonists for combination therapy

Номер: US20120003229A1
Принадлежит: Individual

The invention relates to the use of modulators of cytokine mediated signalling pathways in combination with integrin αvβ3 receptor antagonists for the treatment or prevention of diseases, particularly to the use of a pharmaceutical composition, comprising a modulator of cytokine mediated signalling pathways and an integrin αvβ3 receptor antagonist, for the treatment or prevention of inflammatory or autoimmune disorders, particularly for the treatment or prevention of rheumatoid arthritis and to the pharmaceutical composition itself.

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05-01-2012 дата публикации

Process for production of orally ingestible composition containing arabinofuranosyl vitexin, and use of the composition

Номер: US20120004193A1
Автор: Shuichi Kusano
Принадлежит: Fuji Sangyo Co Ltd

A method for producing an orally ingestible composition containing an arabinofuranosyl vitexin and/or a hydrolysate thereof by using Basella alba as a raw material. The product of such method has a sedative effect and a sleep-inducing effect.

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05-01-2012 дата публикации

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

Номер: US20120004206A1

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

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05-01-2012 дата публикации

Novel tetrahydro-quinoline derivatives

Номер: US20120004218A1
Принадлежит: Hoffmann La Roche Inc

A compound of formula (I) or a pharmaceutically acceptable salt or ester thereof, wherein A 1 to A 3 and R 1 to R 10 have the significance given in claim 1 , can be used as a medicament. These compounds are useful in the treatment or prophylaxis of diseases that are related to AMPK regulation, such as obesity, dyslipidemia, hyperglycemia, type 1 or type 2 diabetes and cancers.

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05-01-2012 дата публикации

Triheterocyclic Compounds and Compositions Thereof

Номер: US20120004224A1
Принадлежит: Gemin X Pharmaceuticals Canada Inc

The present invention relates to novel Triheterocyclic Compounds, compositions comprising a Triheterocyclic Compound, and methods useful for treating or preventing cancer or a neoplastic disorder comprising administering a Triheterocyclic Compound. The compounds, compositions, and methods of the invention are also useful for inhibiting the growth of a cancer cell or neoplastic cell, treating or preventing a viral infection, or inhibiting the replication and/or infectivity of a virus.

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05-01-2012 дата публикации

New ccr2 receptor antagonists and uses thereof

Номер: US20120004252A1
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD.

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05-01-2012 дата публикации

Method of treatment or prophylaxis

Номер: US20120004259A1
Принадлежит: SPINIFEX PHARMACEUTICALS PTY LTD

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

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05-01-2012 дата публикации

Intermediates Useful in the Preparation of Maleimide Functionalized Polymers

Номер: US20120004422A1
Принадлежит: Nektar Therapeutics

Methods for forming maleimide functionalized polymers are provided. In one such embodiment, a maleimide functionalized polymer is prepared in a method that includes a step of carrying out a reverse Diels-Alder reaction. Intermediates useful in the methods, as well as methods for preparing the intermediates, are also provided. Also provided are polymeric reagents, methods of using polymeric reagents, compounds and conjugates.

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12-01-2012 дата публикации

Tetrazine monomers and copolymers for use in organic electronic devices

Номер: US20120007026A1
Принадлежит: NATIONAL RESEARCH COUNCIL OF CANADA

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

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12-01-2012 дата публикации

Broad spectrum benzothiophene-nitrothiazolide and other antimicrobials

Номер: US20120010187A1

The invention provides FIG. 1 novel antimicrobial chemical entities based on a nitrothiazolide backbone that exhibit antibacterial and antiparasitic action against a wide range of human pathogens. The new classes of compounds show extended action against Gram positive bacteria including MRSA drug resistant pathogens. In the Gram-positive organisms, they specifically target and functionally inhibit microbial attachment to surfaces and biofilm formation. In Gram-negative bacteria, including enteroaggregative E. coli strains, these compounds function as pilicides by inhibiting the assembly of pilin subunits into adhesive filaments. Several of these compounds show potent antimicrobial action against Gram positive bacteria, perhaps involving novel targets. Many of the benzothiophene derivatives exhibit antimicrobial activity in the low micrograms per ml range and in blocking biofilm formation in the nanomolar range; ranges considered are well within the range of utility as therapeutics.

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12-01-2012 дата публикации

11-Beta-Hydroxysteroid Dehydrogenase Type 1 Active Compounds

Номер: US20120010194A1
Принадлежит: High Point Pharnaceuticals LLC

The use of substituted amides for modulating the activity of 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) and the use of these compounds as pharmaceutical compositions, are described. Also a novel class of substituted amides, of the general formula I. Their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds are modulators and more specifically inhibitors of the activity of 11βHSDI and may be useful in the treatment of a range of medical disorders where a decreased intracellular concentration of active glucocorticoid is desirable.

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12-01-2012 дата публикации

Anthranilic diamide derivatives having cyclic side-chains

Номер: US20120010249A1
Принадлежит: Bayer CropScience AG

The present invention relates to novel anthranilic diamide derivatives of the general formula (I) in which R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , A, Q and n have the meanings given in the description, to their use as insecticides and acaricides for controlling animal pests, also in combination with other agents for activity boosting, and a plurality of processes for their preparation.

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12-01-2012 дата публикации

Anthranilamide derivatives as pesticides

Номер: US20120010250A1
Принадлежит: Bayer CropScience AG

The present invention relates to novel anthranilamide derivatives of the general formula (I) in which R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , A, Q, Y and n are each as defined in the description—, to the use thereof as insecticides and acaricides for control of animal pests, and to several processes for preparation thereof.

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12-01-2012 дата публикации

Acetylene derivatives having mglur 5 antagonistic activity

Номер: US20120010263A1
Принадлежит: Individual

The invention provides compounds of formula I wherein n, A, R, R′, R″, R O , X and Y are as defined in the description, and their preparation. The compounds of formula I are useful as pharmaceuticals.

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19-01-2012 дата публикации

Compounds for the prevention and treatment of cardiovascular diseases

Номер: US20120015905A1
Автор: Henrik C. Hansen
Принадлежит: Resverlogix Corp

The present disclosure relates to compounds, which are useful for regulating the expression of apolipoprotein A-I (ApoA-I), and their use for treatment and prevention of cardiovascular disease and related disease states, including cholesterol- or lipid-related disorders, such as, for example, atherosclerosis.

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19-01-2012 дата публикации

Sulfone Compounds Which Modulate The CB2 Receptor

Номер: US20120015988A1
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

Compounds which modulate the CB2 receptor are disclosed. Compounds according to the invention bind to and are agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.

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19-01-2012 дата публикации

Pharmaceutical composition for external use

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

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

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26-01-2012 дата публикации

Organic electronic device, compounds for same, and terminal

Номер: US20120018717A1
Принадлежит: Duksan Hi Metal Co Ltd

Disclosed are an organic electronic device and a compound thereof, and a terminal.

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26-01-2012 дата публикации

Enhancing Pilot Channel Transmission in TD-SCDMA Multicarrier Systems Using Secondary Carrier Frequencies

Номер: US20120020283A1
Принадлежит: Qualcomm Inc

Wireless communication in a multicarrier radio access network, such as a (TD-SCDMA) network, may be implemented where a user equipment (UE) maintains communication over various carrier frequencies in the multicarrier network. The UE will receive a downlink pilot channel transmitted on every subframe on a primary carrier frequency. The UE will also receive a downlink pilot channel transmitted on less than every subframe on a secondary carrier frequency The downlink pilot channel is sent in subframes on the secondary carrier frequencies using a particular period and offset to reduce or minimize interference.

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26-01-2012 дата публикации

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

Номер: US20120020915A1

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

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26-01-2012 дата публикации

Bicyclic piperidine and piperazine derivatives as gpcr modulators for the treatment of obesity, diabetes and other metabolic disorders

Номер: US20120021976A1
Принадлежит: Individual

The present invention relates to Bicyclic Piperidine and piperazine Derivatives, compositions comprising a Bicyclic Piperidine and piperazine Derivative, and methods of using the Bicyclic Piperidine and piperazine Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a GPCR in a patient.

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26-01-2012 дата публикации

Triazole derivatives for treatment of alzheimer's disease

Номер: US20120022044A1
Принадлежит: Individual

According to the invention there is provided a compound of formula I or a pharmaceutically acceptable salt or hydrate thereof; wherein the variables are as defined herein. The compounds selectively attenuate the production of Aβ42 and hence are useful in treatment of Alzheimer's disease and related conditions.

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26-01-2012 дата публикации

Novel cyanopyrimidine derivative

Номер: US20120022077A1
Принадлежит: Otsuka Pharmaceutical Co Ltd

The present invention relates to a novel cyanopyrimidine compound and a pharmaceutical composition which have a safe and potent adenosine A2a receptor agonistic activity.

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26-01-2012 дата публикации

Heterocyclic antagonists of prostaglandin d2 receptors

Номер: US20120022119A1
Принадлежит: Amira Pharmaceuticals Inc

Described herein are heteroaryl compounds that are antagonists of PGD 2 receptors. Also described are pharmaceutical compositions and medicaments that include the heteroaryl compounds described. Also described herein are methods of using such antagonists of PGD 2 receptors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.

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26-01-2012 дата публикации

Pyrrolidine triple reuptake inhibitors

Номер: US20120022125A1
Автор: Jianguo Ma, Liming Shao
Принадлежит: SUNOVION PHARMACEUTICALS INC

In various embodiments, the present invention provides cycloalkyl pyrrolidine compounds and methods for their use in the treatment and/or prevention of various diseases, conditions and syndromes, including central nervous system (CNS) disorders, such as depression, anxiety, schizophrenia and sleep disorder as well as methods for their synthesis. The invention also relates to pharmaceutical compositions containing the compounds of the invention, as well as methods of inhibiting reuptake of endogenous monoamines, such as dopamine, serotonin and norepinephrine from the synaptic cleft and methods of modulating one or more monoamine transporter.

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02-02-2012 дата публикации

Novel lipids and compositions for the delivery of therapeutics

Номер: US20120027796A1
Принадлежит: Alnylam Pharmaceuticals Inc

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

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02-02-2012 дата публикации

Natural marine source phospholipids comprising polyunsaturated fatty acids and their applications

Номер: US20120028922A1
Автор: Fotini Sampalis
Принадлежит: Individual

A phospholipid extract from a marine or aquatic biomass possesses therapeutic properties. The phospholipid extract comprises a variety of phospholipids, fatty acid, metals and a novel flavonoid.

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02-02-2012 дата публикации

Pyrazole compounds as crth2 antagonists

Номер: US20120028938A1
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

The present invention relates to pyrazole compounds of formula (I) and pharmaceutically acceptable salts thereof having CRTH2-activity, wherein W, L 1 , L 2 , X, L 3 , Y, R 1 and R 2 are as defined in the specification and claims, to their use as medicaments and to pharmaceutical formulations, containing said compounds or containing a combination of said compounds with one or more active substances.

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02-02-2012 дата публикации

Bicyclic mglur5 positive allosteric modulators and methods of making and using same

Номер: US20120028955A1

In one aspect, the invention relates to bicyclic mGluR5 positive allosteric modulators, for example 6-(phenylethynyl)-3,4-dihydroisoquinolin-1(2H)-one, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

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02-02-2012 дата публикации

6 Substituted 2, 3,4,5 Tetrahydro-1H-Benzo[d]Azepines as 5-HT2c Receptor Agonist

Номер: US20120028961A1
Принадлежит: Eli Lilly and Co

The present invention provides 6-substituted 2,3,4,5-tetrahydro-1H-benzo[d]azepines of Formula I as selective 5-HT 2C receptor agonists for the treatment of 5-HT 2C associated disorders including obesity, obsessive/compulsive disorder, depression, and anxiety: where: R 6 is —S—R 14 ; and other substituents are as defined in the specification.

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02-02-2012 дата публикации

Novel compound having 3-heteroarylpyrimidin-4-(3h)-one structure and pharmaceutical preparation containing same

Номер: US20120028983A1
Принадлежит: Kowa Co Ltd

Disclosed is a compound which has both an angiotensin-II receptor antagonistic activity and a PPARγ activation activity and is useful as a prophylactic and/or therapeutic agent for hypertension, heart diseases, angina pectoris, cerebrovascular disorders, cerebral circulatory disorders, ischemic peripheral circulatory disorders, renal diseases, arteriosclerosis, inflammatory diseases, type-2 diabetes, diabetic complications, insulin resistance syndrome, syndrome X, metabolic syndrome and hyperinsulinemia. [In the formula, A represents a 5- to 10-membered heteroaryl group; R 1 and R 2 independently represent a C 1-6 alkyl group; and each of R 3 to R 5 is absent or represents H, a halogen atom, OH, NO 2 , a halo-C 1-6 alkyl group, a (substituted) C 1-6 alkoxy group, a (substituted) C 3-6 cycloalkyloxy group, or a 5- to 10-membered heteroaryl group.]

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02-02-2012 дата публикации

Crystalline form of sunitinib and processes for its preparation

Номер: US20120029046A1
Принадлежит: Generics UK Ltd

The present invention relates to a novel crystalline form of sunitinib free base designated form I and to processes for its preparation. The invention also relates to its use as an API and in the preparation of various forms of sunitinib. Further, the invention relates to pharmaceutical compositions comprising the novel crystalline form and salts, solvates and hydrates prepared according to the invention, and to the uses of said pharmaceutical compositions in the treatment and/or prevention of cancer.

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02-02-2012 дата публикации

Process for the synthesis of cleistanthin

Номер: US20120029179A1
Принадлежит: Godavari Biorefineries Ltd

The present invention relates to a process for preparing compound of formula (I) that is Cleistanthin A. The process comprises the steps of reacting compound of formula (II) with compound of formula (III) in the presence of a first solvent, quarternary ammonium salt and first alkali to form compound of formula (IV). The compound of formula (IV) is further treated with a second solvent and a second alkali to form compound of formula (I). The present invention also relates to the preparation of salt of compound of formula (IV) that is Cleistanthin A acetate.

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02-02-2012 дата публикации

Synthesis of substituted-3-aminopyrazoles

Номер: US20120029204A1
Принадлежит: Schering Corp

The present invention discloses a process of preparing compound of formula (I): wherein A, M, and Z are as defined herein. An example of a compound of formula (I) is 3-amino-1-methyl-1H-1′H-4,4′-bispyrazole.

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09-02-2012 дата публикации

Charge transport compositions and electronic devices made with such compositions

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

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

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09-02-2012 дата публикации

Substituted dihydropyrazolones and their use

Номер: US20120035151A1
Принадлежит: Bayer Pharma AG

The present application relates to novel substituted dihydropyrazolone derivatives, processes for their preparation, their use for treatment and/or prophylaxis of diseases and their use for the preparation of medicaments for treatment and/or prophylaxis of diseases, in particular cardiovascular and haematological diseases and kidney diseases, and for promoting wound healing.

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09-02-2012 дата публикации

Modulators of Cellular Adhesion

Номер: US20120035154A1
Принадлежит: Sarcode Bioscience Inc

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

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09-02-2012 дата публикации

Compounds useful as inhibitors of atr kinase

Номер: US20120035407A1
Принадлежит: Vertex Pharmaceuticals Inc

The present invention relates to pyrazine compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula II: wherein the variables are as defined herein.

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16-02-2012 дата публикации

Insecticidal (1,3,5)-triazinyl phenyl hydrazones

Номер: US20120040837A1
Принадлежит: DOW AGROSCIENCES LLC

(1,3,5)-Triazinyl phenyl hydrazones are effective at controlling insects.

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16-02-2012 дата публикации

Inhibitors of hcv ns5a

Номер: US20120040977A1
Автор: Leping Li, Min Zhong
Принадлежит: Presidio Pharmaceuticals Inc

Provided herein are compounds, pharmaceutical compositions and combination therapies for inhibition of hepatitis C.

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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

Hydroxybenzoate salts of metanicotine compounds

Номер: US20120041033A1
Принадлежит: Individual

Patients susceptible to or suffering from conditions and disorders, such as central nervous system disorders, are treated by administering to a patient in need thereof compositions that are hydroxybenzoate salts of E-metanicotine-type compounds. The formation of hydroxybenzoate salts of the E-metanicotine compounds is also useful in purifying the E-metanicotine compounds, as the hydroxybenzoate salts tend to crystallize out, leaving impurities such as Z-metanicotine compounds, and compounds where the double bond has migrated, in solution. If desired, the hydroxybenzoate salts can be converted to either the free base (the E-metanicotine) or to another pharmaceutically acceptable salt form.

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16-02-2012 дата публикации

Process for making quinolone compounds

Номер: US20120041208A1
Принадлежит: Rib X Pharmaceuticals Inc

The present invention relates to the field of synthesizing anti-infective compounds. More particularly, the invention relates to synthesizing a family of quinolone compounds useful as anti-infective agents. The invention includes a process for preparing a quinolone compound wherein less than about 0.40% of dimeric impurity of the quinolone is produced.

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23-02-2012 дата публикации

Combination therapy with parp inhibitors

Номер: US20120045524A1
Принадлежит: ABBOTT LABORATORIES

The present invention describes benzimidazole derivatives of Formula (I) which constitute potent PARP inhibitors in combination with radiotherapy or in combination with other chemotherapeutic agents.

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23-02-2012 дата публикации

Developers and method of coloring lithographic printing members

Номер: US20120045720A1
Принадлежит: Individual

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

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23-02-2012 дата публикации

Compounds for treating neuropsychiatric conditions

Номер: US20120046283A1
Принадлежит: Afraxis Inc

Provided herein are PAK inhibitors and methods of utilizing PAK inhibitors for the treatment of neuropsychiatric conditions.

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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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23-02-2012 дата публикации

3-substituted propanamine compounds

Номер: US20120046312A1
Принадлежит: SK Biopharmaceuticals Co Ltd

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

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23-02-2012 дата публикации

Pyrazole-based cyanine dye containing quaternary ammonium cation

Номер: US20120046474A1
Принадлежит: Wako Pure Chemical Industries Ltd

Problem Provided is a novel cyanine dye derivative having high fluorescence intensity in a short wavelength region, a structure where a pyrazole skeleton and an indole skeleton are bound to a polymethine chain, and also a controllable migration velocity by further introducing a quaternary ammonium cation into a molecule having said structure. Solution The present invention is the invention of a compound represented by the general formula [1] or a salt thereof: [wherein R1 to R6 each independently represent an alkyl group having, as a substituent, a group represented by the general formula [101]: (wherein R101 to R104 each independently represent a hydrogen atom or an alkyl group of C1 to C3 and m represents an integer from 2 to 6, and two or three of R102 to R104 together with a nitrogen atom to which they are bound may form a heterocyclic ammonium cation); or a group derived from a carboxylic acid represented by the general formula [2] which may have an amide bond: —COOR12  [2] (wherein R12 represents a hydrogen atom, an alkyl group of C1 to C10, an alkali metal atom, an organic ammonium ion, an ammonium ion or anion); or an alkyl group which may have, as a substituent, a group derived from a sulfonic acid represented by the general formula [3] which may have an amide bond: —SO3R13  [3] (wherein R13 represents a hydrogen atom, an alkali metal atom, an organic ammonium ion, an ammonium ion or anion); R7 to R10 each independently represent an alkyl group, an alkynyl group, an aryl group, an alkoxy group, an aryloxy group, an alkylsulfonyl group, an arylsulfonyl group, an amino group, a group derived from a carboxylic acid represented by the general formula [2], a group derived from a sulfonic acid represented by the general formula [3], a halogen atom, a hydrogen atom, a hydroxyl group, a cyano group or a nitro group; R11 represents a hydrogen atom, an alkyl group, an alkynyl group or an aryl group, and n represents an integer from 0 to 3, and at least one of R1 to ...

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01-03-2012 дата публикации

Azafluorene derivative and organic light-emitting device using the derivative

Номер: US20120049176A1
Принадлежит: Canon Inc

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

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01-03-2012 дата публикации

Cyanine dyes

Номер: US20120052506A1
Принадлежит: Pacific Biosciences of California Inc

The invention provides a novel class of cyanine dyes that are functionalized with sulfonic acid groups and a linker moiety that facilitates their conjugation to other species and substituent groups which increase the water-solubility, and optimize the optical properties of the dyes. Also provided are conjugates of the dyes, methods of using the dyes and their conjugates and kits including the dyes and their conjugates.

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01-03-2012 дата публикации

Phospholinked dye analogs with an amino acid linker

Номер: US20120052507A1
Автор: Gene Shen
Принадлежит: Pacific Biosciences of California Inc

In various embodiments, the present invention provides fluorescent dyes that are linked to another species through an amino acid or peptide linker. In an exemplary embodiment, the dye is linked to a polyphosphate nucleic acid through an amino acid or peptide linker. These conjugates find use in single molecule DNA sequencing and other applications. In various embodiments, the dye moiety is a cyanine dye. Cyanine dyes that are highly charged, such as those including muliple sulfonate, alkylsulfonate, carboxylate and/or alkylcarboxylate moieties are examples of cyanine dyes of use in the compounds of the invention.

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01-03-2012 дата публикации

Nitrogen-Containing Fused Heterocyclic Compounds and Their use as Beta Amyloid Production Inhibitors

Номер: US20120053171A1
Принадлежит: Eisai R&D Management Co Ltd

A compound represented by the formula [I]: or a pharmacologically acceptable salt or ester thereof, wherein Ring A represents a five-membered aromatic heterocyclic group or the like fused with a non-aromatic ring group, which may be substituted, Ring B represents a phenyl group or the like which may be substituted, X1 represents a single bond or the like, R1 and R2 each represent a C1-6 alkyl group or the like, m represents an integer of 0 to 3, and n represents an integer of 0 to 2, is effective as a therapeutic agent for a disease caused by Aβ.

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01-03-2012 дата публикации

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

Номер: US20120053188A1
Автор: Stephen Gately, Tong Wang

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

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08-03-2012 дата публикации

Di-azetidinyl diamide as monoacylglycerol lipase inhibitors

Номер: US20120058986A1
Принадлежит: Janssen Pharmaceutica NV

Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein Q and Z are defined herein.

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08-03-2012 дата публикации

Carbazole and carboline kinase inhibitors

Номер: US20120058988A1
Принадлежит: Bristol Myers Squibb Co

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

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08-03-2012 дата публикации

Carbazole carboxamide compounds useful as kinase inhibitors

Номер: US20120058996A1
Принадлежит: Bristol Myers Squibb Co

Compounds having the formula (I), and enantiomers, and diastereomers, pharmaceutically-acceptable salts, thereof, are useful as kinase modulators, including Btk modulation.

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08-03-2012 дата публикации

Novel kinase modulators

Номер: US20120059001A1

The present invention provides PI3K protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them.

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15-03-2012 дата публикации

Isotopologues of thalidomide

Номер: US20120064004A1
Принадлежит: Celgene Corp

Provided herein are thalidomide, which is enriched with isotopes such as deuterium. Pharmaceutical compositions comprising the isotopes-enriched compounds, and methods of using such compounds are also provided.

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15-03-2012 дата публикации

Peptidomimetic protease inhibitors

Номер: US20120064034A1
Принадлежит: Vertex Pharmaceuticals Inc

The present invention relates to peptidomimetic compounds useful as protease inhibitors, particularly as serine protease inhibitors and more particularly as hepatitis C NS3 protease inhibitors; intermediates thereto; their preparation including novel steroselective processes to intermediates. The invention is also directed to pharmaceutical compositions and to methods for using the compounds for inhibiting HCV protease or treating a patient suffering from an HCV infection or physiological condition related to the infection. Also provided are pharmaceutical combinations comprising, in addition to one or more HCV serine protease inhibitors, one or more interferons exhibiting anti-HCV activity and/or one or more compounds having anti HCV activity and a pharmaceutically acceptable carrier, and methods for treating or preventing a HCV infection in a patient using the compositions. The present invention is also directed to a kit or pharmaceutical pack for treating or preventing HCV infection in a patient.

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15-03-2012 дата публикации

Pyridinylcarboxylic Acid Derivatives as Fungicides

Номер: US20120065197A1
Принадлежит: Bayer CropScience AG

Pyridinylcarboxylic acid derivatives of the formula (I) in which the symbols A, X, Y 1 , Y 2 , Y 3 , L 1 , L 2 , R G , and R 1 are each as defined in the description, and also salts, metal complexes and N-oxides of the compounds of the formula (I), and the use thereof for controlling phytopathogenic harmful fungi and processes for preparing compounds of the formula (I).

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15-03-2012 дата публикации

Compounds and their uses 708

Номер: US20120065214A1
Принадлежит: AstraZeneca AB

The present invention relates to pyrazinone derivatives of formula (I): wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 and R 7 are as herein defined; processes for their preparation, pharmaceutical compositions containing them and their use in therapy.

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15-03-2012 дата публикации

Fluorescent mri probe

Номер: US20120065384A1
Принадлежит: University of Tokyo NUC

A fluorescent gadolinium complex compound comprising a residue of gadolinium.1,4,7,10-tetraazacyclododecane-N,N′,N″,N′″-tetraacetic acid or a residue of gadolinium.diethylenetriaminepentaacetic acid bound covalently with a group represented by the following general formula (I) (R 1 represents hydrogen atom or a substituent R 2 , R 4 , R 5 and R 7 represent hydrogen atom, a halogen atom or a C 1-6 alkyl group, and R 3 and R 6 represent hydrogen atom, a halogen atom or a C 1-6 alkyl group), which is easily taken up into cells and useful as a probe observable by the fluorescence method and MRI.

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22-03-2012 дата публикации

Oligomer-Protein Tyrosine Kinase Inhibitor Conjugates

Номер: US20120071491A1
Принадлежит: Nektar Therapeutics

The invention relates to (among other things) oligomer-PTK inhibitor conjugates and related compounds. A compound of the invention, when administered by any of a number of administration routes, exhibits advantages over PTK inhibitor compounds lacking a water-soluble, non-peptidic oligomer.

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22-03-2012 дата публикации

Aminopyrimidinamides As Pest Control Agents

Номер: US20120071496A1
Принадлежит: Bayer CropScience AG

The present application relates to novel aminopyrimidinamides, to processes for their preparation and to their use for controlling animal pests, especially arthropods, in particular insects.

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22-03-2012 дата публикации

Tetrazole Compounds Which Selectively Modulate The CB2 Receptor

Номер: US20120071529A1
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.

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22-03-2012 дата публикации

Estrogen receptor modulators and uses thereof

Номер: US20120071535A1
Принадлежит: Aragon Pharmaceuticals Inc

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

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22-03-2012 дата публикации

Lenalidomide and Thalidomide Immunoassays

Номер: US20120071632A1
Принадлежит: Individual

Novel conjugates and immunogens derived from lenalidomide and antibodies generated by these immunogens are useful in immunoassays for the quantification and monitoring of thalidomide and lenalidomide in biological fluids.

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22-03-2012 дата публикации

Method for producing olmesartan medoxomil

Номер: US20120071665A1
Автор: Shigeo Yanagihara
Принадлежит: Daiichi Sankyo Co Ltd

A method for producing high-purity olmesartan medoxomil is provided in which a solvent containing water is used in steps of tritylation and DMDO esterification of olmesartan.

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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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29-03-2012 дата публикации

Chemical compounds

Номер: US20120077828A1
Принадлежит: GlaxoSmithKline LLC

The invention is directed to substituted indoline derivatives. Specifically, the invention is directed to compounds according to Formula I: wherein R 1 , R 2 , and R 3 are defined herein. The compounds of the invention are inhibitors of PERK and can be useful in the treatment of cancer, ocular diseases, and diseases associated with activated unfolded protein response pathways, such as Alzheimer's disease, stroke, Type 1 diabetes Parkinson disease, Huntington's disease, amyotrophic lateral sclerosis, myocardial infarction, cardiovascular disease, atherosclerosis, and arrhythmias, and more specifically cancers of the breast, colon, pancreatic, and lung. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting PERK activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.

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29-03-2012 дата публикации

Heterocyclic compounds and their use as glycogen synthase kinase-3 inhibitors

Номер: US20120077840A1
Принадлежит: Abbott GmbH and Co KG

The present invention relates to novel heterocyclic compounds which are useful for inhibiting glycogen synthase kinase 3 (GSK-3), methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.

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29-03-2012 дата публикации

Methods for Synthesizing 3-(Substituted Dihydroisoindolinone-2-YL)-2, 6-Dioxopiperidine, and Intermediates Thereof

Номер: US20120077982A1

The present invention discloses methods for synthesizing 3-(substituted dihydroisoindolinone-2-yl)-2,6-dioxopiperidine and intermediates thereof, namely, the synthesis of compounds of the Formula (I), with each substitutional group defined in the patent specification. Owing to the advantages of high productivity, little influence to the environment and material accessibility, the methods of the present invention is suitable for industrial production.

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05-04-2012 дата публикации

Photoelectric conversion element, production method thereof, photosensor, imaging device and their driving method

Номер: US20120080585A1
Принадлежит: Fujifilm Corp

To provide a photoelectric conversion element capable of functioning as a photoelectric conversion element when a compound having a specific structure is applied to the photoelectric conversion element, causing the element to exhibit a low dark current, and reducing the range of increase in the dark current even when the element is heat-treated, and an imaging device equipped with such a photoelectric conversion element. A photoelectric conversion element having a photoelectric conversion film which is sandwiched between a transparent electrically conductive film and an electrically conductive film and contains a photoelectric conversion layer and an electron blocking layer, wherein the electron blocking layer contains a compound having, as a substituent, a substituted amino group containing three or more ring structures.

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05-04-2012 дата публикации

Novel triazole derivatives with improved receptor activity and bioavailability properties as ghrelin antagonists of growth hormone secretagogue receptors

Номер: US20120083494A1

The present invention provides novel triazole derivatives with improved receptor activity and bioavailability properties as ghrelin analogue ligands of growth hormone secretagogue receptors according to formula (I) that are useful in the treatment or prophylaxis of physiological and/or pathophysiological conditions in mammals, preferably humans, that are mediated by GHS receptors. The present invention further provides GHS receptor antagonists and agonists that can be used for modulation of these receptors and are useful for treating above conditions, in particular alcohol disorder, drug abuse, growth retardation, cachexia, short-, medium-, and/or long term regulation of energy balance, short-, medium-, and/or long term regulation (stimulation and/or inhibition) of food intake, intake of rewarding food, adipogenesis, adiposity and/or obesity, body weight gain and/or reduction, diabetes, diabetes type I, diabetes type II, tumor cell proliferation, inflammation, inflammatory effects, gastric postoperative ileus, postoperative ileus and/or gastrectomy (ghrelin replacement therapy).

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12-04-2012 дата публикации

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

Номер: US20120088746A1
Принадлежит: PFIZER INC

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

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12-04-2012 дата публикации

Five-membered heterocycles useful as serine protease inhibitors

Номер: US20120088758A1
Принадлежит: Bristol Myers Squibb Co

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

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12-04-2012 дата публикации

Compounds for enzyme inhibition

Номер: US20120088762A1
Принадлежит: Onyx Therapeutics Inc

One aspect of the invention relates to inhibitors that preferentially inhibit immunoproteasome activity over constitutive proteasome activity. In certain embodiments, the invention relates to the treatment of immune related diseases, comprising administering a compound of the invention. In certain embodiments, the invention relates to the treatment of cancer, comprising administering a compound of the invention.

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12-04-2012 дата публикации

Pinane-substituted pyrimidinediamine derivatives useful as axl inhibitors

Номер: US20120088768A1
Принадлежит: Rigel Pharmaceuticals Inc

Pinane-substituted pyrimidinediamine derivatives and pharmaceutical compositions containing the derivatives are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the derivatives in treating diseases or conditions associated with Axl catalytic activity are also disclosed.

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12-04-2012 дата публикации

Azole derivatives and fused bicyclic azole derivatives as therapeutic agents

Номер: US20120088778A1
Принадлежит: vTvx Holdings I LLC

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

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12-04-2012 дата публикации

Bicyclic Compounds and Methods of Making and Using Same

Номер: US20120088793A1
Принадлежит: Nanotherapeutics Inc

Disclosed herein are compounds that may be modulators of 5-HT receptors, and methods of making and using same.

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12-04-2012 дата публикации

1-heterocyclylsulfonyl, 3-aminomethyl, 5- (hetero-) aryl substituted 1-h-pyrrole derivatives as acid secretion inhibitors

Номер: US20120088797A1
Принадлежит: Takeda Pharmaceutical Co Ltd

The present invention provides a compound having a superior acid secretion inhibitory effect and showing an antiulcer activity and the like. The present invention provides a compound represented by the formula (I) wherein R 1 is a nitrogen-containing monocyclic heterocyclic group optionally condensed with a benzene ring or a heterocycle, the nitrogen-containing monocyclic heterocyclic group optionally condensed with a benzene ring or a heterocycle optionally has substituent(s), R 2 is an optionally substituted C 6-14 aryl group, an optionally substituted thienyl group or an optionally substituted pyridyl group, R 3 and R 4 are each a hydrogen atom, or one of R 3 and R 4 is a hydrogen atom and the other is an optionally substituted lower alkyl pup, an acyl group, a halogen atom, a cyano group or a nitro group, and R 5 is an alkyl group or a salt thereof.

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19-04-2012 дата публикации

Novel Heterocyclic Compounds as Pesticides

Номер: US20120094837A1
Принадлежит: Bayer CropScience AG

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

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19-04-2012 дата публикации

Egfr inhibitors and methods of treating disorders

Номер: US20120094999A1
Принадлежит: Dana Farber Cancer Institute Inc

The present invention relates to novel pyrimidine, pyrrolo-pyrimidine, pyrrolo-pyridine, pyridine, purine and triazine compounds which are able to modulate epidermal growth factor receptor (EGFR), including Her-kinases, and the use of such compounds in the treatment of various diseases, disorders or conditions.

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19-04-2012 дата публикации

Novel Heterocyclic Compounds as Pesticides

Номер: US20120095023A1
Принадлежит: Bayer CropScience AG

The present application relates to novel amides and thioamides, to processes for preparation thereof and to the use thereof for controlling animal pests, in particular arthropods and especially insects.

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19-04-2012 дата публикации

Novel lipids and compositions for the delivery of therapeutics

Номер: US20120095075A1
Принадлежит: Alnylam Pharmaceuticals Inc

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

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26-04-2012 дата публикации

Novel c-aryl glucoside sglt2 inhibitors and pharmaceutical compositions comprising same

Номер: US20120101051A1
Принадлежит: Green Cross Corp Korea

A novel C-aryl glucoside compound, or a pharmaceutically acceptable salt or a prodrug thereof having an inhibitory activity against sodium-dependent glucose cotransporter 2 (SGLT2) being present in the intestine and kidney; and a pharmaceutical composition comprising the same as an active ingredient, which is useful for preventing or treating metabolic disorders, particularly, diabetes, are provided.

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03-05-2012 дата публикации

Compound for an organic photoelectric device and organic photoelectric device including the same

Номер: US20120104941A1
Принадлежит: Cheil Industries Inc

A compound for an organic photoelectric device, an organic photoelectric device, and a display device, the compound being represented by the following Chemical Formula 3a, 3b, or 3c:

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03-05-2012 дата публикации

Bait chemistries in hydrogel particles for serum biomarker analysis

Номер: US20120107959A1

This invention describes the identification of novel organic dye chemistries that can be used as affinity baits to capture proteins and other biomolecules useful in the fields of medical diagnostics, environmental science, toxicology, and infectious disease. Incorporation of unique affinity dye compounds within hydrogel capture particles improves analyte yield and preanalytical precision, and stabilizes the analyte against degradation, while increasing measurement sensitivity. The particles in this invention can be used for routine clinical testing as well as for discovery of low abundance disease biomarkers. Example hydrogel particles containing new high affinity bait chemistries were used to identify a new set of human serum biomarkers.

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03-05-2012 дата публикации

Compounds for the treatment of multi-drug resistant bacterial infections

Номер: US20120108577A1
Принадлежит: AstraZeneca AB

The present invention relates to compounds that demonstrate antibacterial activity, processes for their preparation, pharmaceutical compositions containing them as the active ingredient, to their use as medicaments and to their use in the manufacture of medicaments for use in the treatment of bacterial infections in warm-blooded animals such as humans. In particular this invention relates to compounds useful for the treatment of bacterial infections in warm-blooded animals such as humans, more particularly to the use of these compounds in the manufacture of medicaments for use in the treatment of bacterial infections in warm-blooded animals such as humans.

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03-05-2012 дата публикации

Carbamoyl Compounds as DGAT1 Inhibitors 190

Номер: US20120108602A1
Принадлежит: AstraZeneca AB

DGAT-1 inhibitor compounds of formula (1), pharmaceutically-acceptable salts and pro-drugs thereof are described, together with pharmaceutical compositions, processes for making them and their use in treating, for example, obesity wherein, for example, Ring A is optionally substituted 2,6-pyrazindiyl; X is ═0; Ring B is optionally substituted 1,4-phenylene; Y 1 is a direct bond or —O—; Y 2 is —(CH 2 ) r — wherein r is 2 or 3; n is 0 or n is 1 when Y 1 is a direct bond between Ring B and Ring C and when Ring B is 1,4-phenylene and Ring C is (4-6C)cycloalkane; Ring C is optionally substituted (4-6C)cycloalkane, (7-10C)bicycloalkane, (8-12C)tricycloalkane, phenylene or pryidindiyl; L is a direct bond or —O—; p is 0, 1 or 2 and when p is 1 or 2 R A1 and R A2 are each independently hydrogen or (1-4C)alkyl; Z is carboxy or a mimic or bioisostere thereof.

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03-05-2012 дата публикации

Nitrogen-containing aromatic heterocyclyl compound

Номер: US20120108639A1
Принадлежит: Daiichi Sankyo Co Ltd

The present invention provides a compound having excellent regulating action on blood lipid level that is represented by the following general formula (I) or a pharmacologically acceptable salt thereof, wherein, in one embodiment, A represents a 5-membered nitrogen-containing aromatic heterocyclyl group; R 1 represents COOH; each R 2 represents an alkyl; each R 3 represents an optionally substituted phenyl, an optionally substituted phenylalkyl; m represents 0, 1, 2, or 3; n represents 0 or 1; each of R 4 , R 5 , R 6 , and R 7 represents H, an alkyl; and B represents an optionally substituted naphthyl, an optionally substituted aromatic heterocyclyl, or a group represented by the following formula (II) wherein each of B 1 and B 2 represents an optionally substituted phenyl or an optionally substituted aromatic heterocyclyl.

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03-05-2012 дата публикации

Novel microbiocides

Номер: US20120108645A1
Принадлежит: SYNGENTA CROP PROTECTION LLC

Compounds of formula (I) in which the substituents are as defined in claim 1, are suitable for use as microbiocides.

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10-05-2012 дата публикации

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

Номер: US20120112629A1
Принадлежит: Idemitsu Kosan Co Ltd

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

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10-05-2012 дата публикации

Novel inhibitors of hepatitis c virus

Номер: US20120114600A1
Принадлежит: Theravance Inc

The invention provides compounds of formula (I): wherein the variables are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are inhibitors of replication of the hepatitis C virus. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat hepatitis C viral infections, and processes and intermediates useful for preparing such compounds.

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10-05-2012 дата публикации

Compound inhibiting in vivo phosphorus transport and medicine containing the same

Номер: US20120115851A1
Принадлежит: Kyowa Hakko Kirin Co Ltd

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

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10-05-2012 дата публикации

New Salts of an Indole Derivative and Their Use in Medicine

Номер: US20120115865A1
Принадлежит: AstraZeneca AB

The present invention relates to new pharmaceutically acceptable salts of 2-hydroxy-3-[5-(morpholin-4-yl-methyl)pyridin-2-yl]1H-indole-5-carbonitrile, processes for their preparations, pharmaceutical formulations containing said salts and to the use of said active salts in therapy, and particularly to GSK3 related disorders.

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10-05-2012 дата публикации

Compounds having antiparasitic or anti-infectious activity

Номер: US20120115904A1

Compounds of formula I: or formula II: or a pharmaceutically acceptable salt of formula I or formula II, wherein: R 1 is H, hydroxyl, alkoxy, acyl, alkyl, cycloalkyl, aryl, or heteroaryl; R 2 is methyl or haloalkyl; R 4 is hydroxyl, carbonyloxy, or carbonyldioxy; and R 3 is aliphatic, aryl, aralkyl, or alkylaryl; and R 5 , R 6 , R 7 and R 8 are each individually H, halogen, alkoxy, alkyl, haloalkyl, aryl, nitro, cyano, amino, amido, acyl, carboxyl, substituted carboxyl, or —SO 2 R 10 , wherein R 10 is H, alkyl, amino or haloalkyl; provided that in formula I, R 5 and R are not both H or R 6 is not H or methoxy; and in formula II that if R 4 is carbonyldioxy then R 7 is not methoxy.

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10-05-2012 дата публикации

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

Номер: US20120115915A1
Принадлежит: Harvard College

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

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