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Небесная энциклопедия

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

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Мониторинг СМИ

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

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Форма поиска

Поддерживает ввод нескольких поисковых фраз (по одной на строку). При поиске обеспечивает поддержку морфологии русского и английского языка
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Применить Всего найдено 29708. Отображено 100.
05-01-2012 дата публикации

Pyrazolo[1,5-a]pyrimidines for antiviral treatment

Номер: US20120003215A1
Принадлежит: Gilead Sciences Inc

The invention provides compounds of Formula I or Formula II: or a pharmaceutically acceptable salt or ester, thereof, as described herein. The compounds and compositions thereof are useful for treating Pneumovirinae virus infections. The compounds, compositions, and methods provided are particularly useful for the treatment of Human respiratory syncytial virus infections.

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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

Diketopyrrolopyrrole polymers for use in organic semiconductor devices

Номер: US20120059140A1
Принадлежит: BASF SE

The present invention relates to polymers comprising one or more (repeating) unit(s) of the formula (I) which are characterized in that Ar 1 and Ar 1 ′ are independently of each other are an annulated (aromatic) heterocyclic ring system, containing at least one thiophene ring, which may be optionally substituted by one, or more groups, and their use as organic semiconductor in organic devices, especially in organic photovoltaics (solar cells) and photodiodes, or in a device containing a diode and/or an organic field effect transistor. The polymers according to the invention have excellent solubility in organic solvents and excellent film-forming properties. In addition, high efficiency of energy conversion, excellent field-effect mobility, good on/off current ratios and/or excellent stability can be observed, when the polymers according to the invention are used in organic field effect transistors, organic photovoltaics (solar cells) and photodiodes.

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15-03-2012 дата публикации

Treatment of cancer

Номер: US20120064071A1
Автор: John Ryan
Принадлежит: Cerulean Pharma Inc

Provided are methods relating to compositions that include a CDP-topoisomerase inhibitor, e.g., a CDP-camptothecin or camptothecin derivative conjugate, e.g., CRLX101.

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26-04-2012 дата публикации

Diaza-spiro[5.5]undecanes

Номер: US20120101110A1
Принадлежит: Individual

The invention relates to compound of the formula I in which the substituents are as defined in the specification; in free form or in salt form; to its preparation, to its use as medicament and to medicaments comprising it.

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03-05-2012 дата публикации

Trioxane Monomers and Dimers

Номер: US20120108545A1
Принадлежит: JOHNS HOPKINS UNIVERSITY

Monomeric and dimeric trioxane fluoroaryl amides, 5-carbon-linked, C-10 non-acetal trioxane dimer esters; trioxane silylamides; and trioxane dimer orthoesters and methods of their use for treating subjects infected with malaria or other parasitic infectious diseases including, but not limited to, toxoplasmic infection; subjects afflicted with psychiatric conditions associated with toxoplasmic infection; and subjects afflicted with cancer.

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03-05-2012 дата публикации

N1/n2-lactam acetyl-coa carboxylase inhibitors

Номер: US20120108619A1
Принадлежит: PFIZER INC

The invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof; wherein G is R 1 , R 2 and R 3 are as described herein; pharmaceutical compositions thereof; and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl-CoA carboxylase enzyme(s) in an animal.

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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

Aryl- and Heteroarylcarbonyl derivatives of substituted nortropanes, medicaments containing such compounds and their use

Номер: US20120115853A1
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

The present invention relates to compounds defined by formula (I) wherein the groups R 1 and R 2 are defined as in claim 1 , possessing valuable pharmacological activity. Particularly the compounds are inhibitors of 11 β-hydroxysteroid dehydrogenase (HSD) 1 and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases, in particular diabetes type 2, obesity, and dyslipidemia.

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10-05-2012 дата публикации

Porphyrin compounds comprising one or more pyridone moieties

Номер: US20120115901A1
Принадлежит: VENTANA RESEARCH Corp

Various porphyrin compounds comprising one or more pyridone moieties, intermediates thereof, compositions thereof, and, methods of making and using thereof.

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17-05-2012 дата публикации

Heterocyclic compounds and uses thereof

Номер: US20120122838A1

Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.

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21-06-2012 дата публикации

Antimicrobial heterocyclic compounds for treatment of bacterial infections

Номер: US20120157434A1
Принадлежит: CSO of MicuRx Pharmaceuticals Inc

The present invention provides heterocyclic compounds of the following formula I: or pharmaceutically acceptable salts, prodrugs, solvates, or hydrates thereof useful as antibacterial agents, pharmaceutical compositions containing them, methods for their use, and methods for preparing these compounds.

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16-08-2012 дата публикации

Thieno- and furo-pyrimidine modulators of the histamine h4 receptor

Номер: US20120208793A1
Принадлежит: Individual

Thieno- and furo-pyrimidine compounds are described, which are useful as H 4 receptor modulators. Such compounds may be used in pharmaceutical compositions and methods for the modulation of histamine H 4 receptor activity and for the treatment of disease states, disorders, and conditions mediated by H 4 receptor activity, such as inflammation.

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16-08-2012 дата публикации

8-[3-amino-piperidin-1-yl]-xanthines, the preparation thereof and their use as pharmaceutical compositions

Номер: US20120208831A1

The present invention relates to substituted xanthines of general formula wherein R 1 to R 3 are as defined herein, the tautomers, the stereoisomers, the mixtures, the prodrugs thereof and the salts thereof which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).

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23-08-2012 дата публикации

Heteroaryls and uses thereof

Номер: US20120214794A1
Принадлежит: Millennium Pharmaceuticals Inc

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

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30-08-2012 дата публикации

Imidazopyrazine syk inhibitors

Номер: US20120220582A1
Принадлежит: Gilead Connecticut Inc

Certain imidazopyrazines and pharmaceutical compositions thereof are provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are provided. Also provided are methods for determining the presence or absence of Syk kinase in a sample.

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13-09-2012 дата публикации

Organic compound and photovoltaic device comprising the same

Номер: US20120227802A1
Принадлежит: Cryscade Solar Ltd

The present invention provides a organic compound of the general structural formula 1 and photovoltaic device and photovoltaic layer comprising thereof Said organic compound forms rod-like supramolecules and absorbs electromagnetic radiation in at least one predetermined spectral subrange within a wavelength range from 400 to 3000 nm with excitation of electron-hole pairs. The polycyclic core Cor 1 , the bridging group B, and the polycyclic core Cor 2 form a molecular system selected from the list comprising donor-bridge-acceptor-bridge-donor and acceptor-bridge-donor-bridge-acceptor in which a dissociation of excited electron-hole pairs is carried out. A solution of the organic compound or its salt forms a solid photovoltaic layer on a substrate.

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13-09-2012 дата публикации

Compound having a substituted anthracene ring structure and pyridoindole ring structure, and organic electroluminescent device

Номер: US20120228598A1
Принадлежит: Hodogaya Chemical Co Ltd

The present invention relates to a compound having a substituted anthracene ring structure and a pyridoindole ring structure, which is represented by the following general formula (1) or the following general formula (2); and an organic electroluminescent device having a pair of electrodes and at least one organic layer interposed therebetween, in which the compound having a substituted anthracene ring structure and a pyridoindole ring structure, which is represented by the following general formula (1) or the following general formula (2), is used as a constituent material of the aforementioned at least one organic layer.

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13-09-2012 дата публикации

Quinolizidinone carboxamide m1 receptor positive allosteric modulators

Номер: US20120232076A1
Принадлежит: Individual

The present invention is directed to compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.

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04-10-2012 дата публикации

Thiazole derivatives for the treatment of diseases such as cancer

Номер: US20120252759A1
Принадлежит: Merck Patent GmBH

Compounds of the formula Ia and Ib, in which R 1 , R 1′ , R 2 , R 3 , R 5 , R 6 and R 7 have the meanings indicated in claim 1 , are kinase inhibitors and can be employed, inter alia, for the treatment of tumours.

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11-10-2012 дата публикации

Inhibitors of e1 activating enzymes

Номер: US20120258927A1
Принадлежит: Millennium Pharmaceuticals Inc

This invention relates to compounds that inhibit E1 activating enzymes, pharmaceutical compositions comprising the compounds, and methods of using the compounds. The compounds are useful for treating disorders, particularly cell proliferation disorders, including cancers, inflammatory and neurodegenerative disorders; and inflammation associated with infection and cachexia.

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11-10-2012 дата публикации

Substituted N-(1H-Indazol-4-yl)Imidazo[1,2-a]Pyridine-3-Carboxamide Compounds as cFMS Inhibitors

Номер: US20120258952A1
Принадлежит: Array Biopharma Inc

Compounds of Formula (I): and pharmaceutically acceptable salts thereof in which R 1 , R 2 , R 3 , R 4 and R 5 have the meanings given in the specification, are inhibitors of cFMS and are useful in the treatment of bone-related diseases, cancer, autoimmune disorders, inflammatory diseases, cardiovascular diseases and pain.

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15-11-2012 дата публикации

3,4,4A,10B-TETRAHYDRO-1H-THIOPYRANO-[4,3-c] ISOQUINOLINE DERIVATIVES

Номер: US20120289474A1
Принадлежит: NYCOMED GMBH

The compounds of Formula (1), in which A, R1, R2, R3 and R5 have the meanings as given in the description, are novel effective inhibitors of type 4 and 5 phosphodiesterase.

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22-11-2012 дата публикации

Gabaergic receptor subtype selective ligands and their uses

Номер: US20120295892A1
Принадлежит: UWM Research Foundation Inc

Described herein are α3 or α2 or α2/α3 GABAergic receptor subtype selective ligands, pharmaceutical compositions, and methods of use of such ligands and compositions in treatment of anxiety disorders, epilepsy and schizophrenia with reduced sedative and ataxic side effects. In embodiments, such as α3 or α2 or α2/α3 GABAergic receptor subtype selective ligands lack ester linkages and may be thus relatively insensitive to hydrolysis by esterases.

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22-11-2012 дата публикации

Azabenzimidazoles as fatty acid synthase inhibitors

Номер: US20120295915A1
Принадлежит: Individual

Disclosed are compounds having Formula (I), wherein R 1 , R 2 , R 3 , R 4 , Ra, Rb, X, Y, m, and n are defined herein and methods of using the same.

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29-11-2012 дата публикации

Compound having pyridoindole ring structure having substituted pyridyl group attached thereto, and organic electroluminescence element

Номер: US20120298969A1
Принадлежит: Hodogaya Chemical Co Ltd

The invention relates to a compound having a pyridoindole ring structure having a substituted pyridyl group of formula (1); and to an organic electroluminescent device comprising a pair of electrodes and at least one organic layer interposed between the electrodes, wherein at least one of the organic layer(s) contains the compound: wherein Ar represents a substituted or unsubstituted aromatic hydrocarbon group, a substituted or unsubstituted aromatic heterocyclic group, or a substituted or unsubstituted condensed polycyclic aromatic group; R1 to R10 may be the same or different from one another and each independently represents a hydrogen atom, a fluorine atom, a cyano group, an alkyl group, or a substituted or unsubstituted aromatic hydrocarbon group; Z represents a 6-membered aromatic heterocyclic ring containing one nitrogen atom; and m and n each independently represents an integer of 1 to 3, provided that n is 1 when m is 2 or 3.

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29-11-2012 дата публикации

Pyrrolotriazine kinase inhibitors

Номер: US20120302747A1
Принадлежит: Bristol Myers Squibb Co

The invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity thereby making them useful as anticancer agents and for the treatment of Alzheimer's Disease.

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06-12-2012 дата публикации

HIV Integrase Inhibitors

Номер: US20120309698A1
Принадлежит: Bristol Myers Squibb Co

The disclosure generally relates to the novel compounds of formula I, including their salts, which inhibit HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses pharmaceutical compositions and methods for treating those infected with HIV.

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27-12-2012 дата публикации

Novel kinase inhibitors

Номер: US20120329780A1
Принадлежит: Origenis Gmbh

The present invention relates to novel compounds of formula (I) that are capable of inhibiting one or more kinases, especially SYK (Spleen Tyrosine Kinase), LRRK2 (Leucine-rich repeat kinase 2) and/or MYLK (Myosin light chain kinase) or mutants thereof. The compounds find applications in the treatment of a variety of diseases. These diseases include autoimmune diseases, inflammatory diseases, bone diseases, metabolic diseases, neurological and neurodegenerative diseases, cancer, cardiovascular diseases, allergies, asthma, alzheimer's disease, parkinson's disease, skin disorders, eye diseases, infectious diseases and hormone-related diseases.

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03-01-2013 дата публикации

Aminotriazolopyridines, compositions thereof, and methods of treatment therewith

Номер: US20130005707A1
Принадлежит: Individual

Provided herein are Heteroaryl Compounds of formula (I): wherein R 1 and R 2 are as defined herein, compositions comprising an effective amount of a Heteroaryl Compound and methods for treating or preventing inflammatory conditions or cancer, and conditions treatable or preventable by inhibition of a kinase or a kinase pathway comprising administering an effective amount of a Heteroaryl Compound to a subject in need thereof.

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07-02-2013 дата публикации

Heterocyclic compounds and uses thereof

Номер: US20130035324A1
Принадлежит: INTELLIKINE LLC

Heterocyclic entities that modulate PI3 kinase activity, pharmaceutical compositions containing the heterocyclic entities, and methods of using these chemical entities for treating diseases and conditions associated with PI3 kinase activity are described herein.

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14-02-2013 дата публикации

Electroluminescent materials comprising fluorene derivatives

Номер: US20130037752A1
Автор: Gene Carl Koch
Принадлежит: Lomox Ltd

OLED compounds of the general structure: B—S-A-S—B in which rod-like nuclei A includes a condensed aromatic ring structure in turn having fluorene ring structures condensed with at least one additional fluorene ring structures wherein the fluorene ring systems provided by the condensed aromatic structure are substituted at the 9-position, and in which the 9-positions of the fluorenes are not susceptible to oxidation.

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14-02-2013 дата публикации

PYRAZOLO[3,4-c]PYRIDINE COMPOUNDS AND METHODS OF USE

Номер: US20130039906A1
Принадлежит: Genentech Inc

Pyrazolo[3,4-c]pyridine compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, wherein R 1 and R 2 are as defined herein, are useful for inhibiting Pim kinase, and for treating disorders such as cancer mediated by Pim kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.

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14-02-2013 дата публикации

Azaindoles as janus kinase inhibitors

Номер: US20130040933A1
Принадлежит: Individual

The present invention provides compounds of formula I: or a pharmaceutically acceptable salt thereof. Compounds of formula I are inhibitors of Janus kinases and as such are useful for the treatment of various diseases and conditions mediated by said enzymes, such as rheumatoid arthritis, asthma, COPD, ALS, and the like.

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07-03-2013 дата публикации

Pyrrolobenzodiazepines used to treat proliferative diseases

Номер: US20130059800A1

Pyrrolobenzodiazepine dimers I having a C2-C3 double bond and an aryl group at the C2 position on one monomer unit, and a C2-C3 double bond and either a conjugated double or triple bond at the C2 position or an alkyl group at the C2 position on the other monomer unit, and conjugates of these compounds.

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21-03-2013 дата публикации

Soluble mtor complexes and modulators thereof

Номер: US20130072485A1

The present invention relates to small molecule modulators of mTORC1 and mTORC2, syntheses thereof, and intermediates thereto. Such small molecule modulators are useful in the treatment of proliferative diseases (e.g., benign neoplasms, cancers, inflammatory diseases, autoimmune diseases, diabetic retinopathy) and metabolic diseases. Novel small molecules are provided that inhibit one or more of mTORC1, mTORC2, and PI3K-related proteins. Novel methods of providing soluble mTORC1 and mTORC2 complexes are discussed, as well as methods of using the soluble complexes in a high-throughput manner to screen for inhibitory compounds.

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11-04-2013 дата публикации

Heteroaryl imidazolone derivatives as jak inhibitors

Номер: US20130089512A1

New heteroaryl imidazolone derivatives having the chemical structure of formula (I) are disclosed, as well as processes for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Janus Kinases (JAK).

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18-04-2013 дата публикации

Pyridone derivative having integrase inhibitory activity

Номер: US20130096109A1
Принадлежит: Shionogi and Co Ltd

An object of the present invention is to provide a novel integrase inhibitor. The present invention relates to a novel compound having an antiviral effect, more specifically, a pyridone derivative having HIV integrase inhibitory activity, and a medicament containing the same, in particular, an anti-HIV agent. The compound of the present invention has integrase inhibitory activity and/or cell proliferation inhibitory activity against viruses, in particular, HIV and drug-resistant strains thereof. Thus, the compound is useful in preventing or treating various diseases, viral infections (for example, AIDS), and the like in which integrase participates.

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18-04-2013 дата публикации

BICYCLIC HETEROCYCLE DERIVATIVES AND METHODS OF USE THEREOF

Номер: US20130096141A1
Принадлежит:

Compounds of structural formula I: are GPR119 agonists and are useful for the treatment, control or prevention of disorders responsive to agonism of GPR119, such as metabolic-related disorders such as type I diabetes, type II diabetes, inadequate glucose tolerance, insulin resistance, hyperglycemia, hyperlipidemia, hypertriglyceridemia, hypercholesterolemia, dyslipidemia or syndrome X. The compounds are also reported as being useful for controlling weight gain, controlling food intake, and inducing satiety in mammals. 142-. (canceled)44. The compound of claim 43 , wherein A is —O—.47. The compound of claim 43 , wherein W is —C(O)O— or —C(O)—.48. The compound of claim 43 , wherein W is a bond.49. The compound of claim 43 , wherein Ris C-Calkyl claim 43 , haloalkyl claim 43 , heteroaryl or cycloalkyl.50. The compound of claim 43 , wherein Ar is aryl or heteroaryl.51. The compound of claim 43 , wherein Ar is phenyl.52. The compound of claim 43 , wherein Ar is pyridyl.54. The compound of claim 43 , wherein J and M are each —N—.55. The compound of claim 43 , wherein A is —O— and W is —C(O)O— claim 43 , a bond or —CH—.58. A compound of or pharmaceutically acceptable salt thereof claim 57 , wherein X is —S—.59. A compound of or pharmaceutically acceptable salt thereof claim 57 , wherein X is —NC-Calkyl-.61. A pharmaceutical composition comprising a compound of claim 43 , or a pharmaceutically acceptable salt thereof claim 43 , and a pharmaceutically acceptable carrier.62. A method for the treatment of a condition selected from the group consisting of obesity and diabetes comprising administering to an individual a pharmaceutical composition comprising the compound of . The present invention relates to bicyclic heterocycle derivatives, compositions comprising a bicyclic heterocycle derivative, and methods of using the bicyclic heterocycle derivatives for treating or preventing obesity, diabetes, a diabetic complication, a metabolic disorder, a cardiovascular disease or a ...

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18-04-2013 дата публикации

NOVEL CEPHEM DERIVATIVE

Номер: US20130096299A1
Принадлежит: Shionogi & Co., Ltd.

Provided is a cephem compound which has a wide antimicrobial spectrum, and in particular exhibit potent antimicrobial activity against beta-lactamase producing Gram negative bacteria, and pharmaceutical composition comprising the same. 2. The compound , or an ester , a protected compound at the amino on the ring in the 7-side chain , a pharmaceutically acceptable salt , or a solvate thereof according to , wherein D is a single bond , —NH— , or —R—NH— wherein Ris as defined in .3. The compound claim 1 , or an ester claim 1 , a protected compound at the amino on the ring in the 7-side chain claim 1 , a pharmaceutically acceptable salt claim 1 , or a solvate thereof according to claim 1 , wherein D is —NH— claim 1 , —CH—NH— claim 1 , or —CH—CH—NH—.4. The compound claim 1 , or an ester claim 1 , a protected compound at the amino on the ring in the 7-side chain claim 1 , a pharmaceutically acceptable salt claim 1 , or a solvate thereof according to claim 1 , wherein D is a single bond.6. The compound claim 1 , or an ester claim 1 , a protected compound at the amino on the ring in the 7-side chain claim 1 , a pharmaceutically acceptable salt claim 1 , or a solvate thereof according to claim 1 , wherein E is selected from formulae (1) to (9) claim 1 , (11) to (40) claim 1 , (47) to (49) claim 1 , (51) and (52).7. The compound claim 1 , or an ester claim 1 , a protected compound at the amino on the ring in the 7-side chain claim 1 , a pharmaceutically acceptable salt claim 1 , or a solvate thereof according to claim 1 , wherein E is selected from formulae (5) claim 1 , (6) claim 1 , (9) to (11) claim 1 , (26) claim 1 , (29) to (34) claim 1 , (36) claim 1 , (37) and (50).8. The compound claim 1 , or an ester claim 1 , a protected compound at the amino on the ring in the 7-side chain claim 1 , a pharmaceutically acceptable salt claim 1 , or a solvate thereof according to claim 1 , wherein E is selected from formulae (5) claim 1 , (6) claim 1 , (10) and (11).9. The compound ...

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25-04-2013 дата публикации

Sirtuin activators and activation assays

Номер: US20130102009A1

Provided are methods and compositions for detecting a compound that activates a sirtuin deacetylase activity on a fluorescent-free activation substrate in vitro. Further provided are sirtuin modulating compounds of the formulas (I)-(XXI), and related compounds (XXXI), (XXXII), (XXXIII), and (XXXIV), including the fluorescent free-substrate SIRT1 activator compounds of formulas (XL), (XI), (XII), and (XIII).

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25-04-2013 дата публикации

Cephem compound having catechol group

Номер: US20130102583A1
Принадлежит: Shionogi and Co Ltd

A compound of the formula: wherein X is —N═, —CH═, or the like; W is —CH 2 — or the like; U is —S— or the like; R 1 and R 2 are each independently hydrogen, halogen, optionally substituted lower alkyl, or the like; R 3 is hydrogen or the like; each R 4 is independently hydrogen, halogen, or the like; m is an integer from 0 to 2; Q is a single bond, or the like; G is —C(═O)—, or the like; D is a single bond, —NH—, or the like; and E is a cyclic quaternary ammonium group, or an ester, a protected compound at the amino on the ring in the 7-side chain, a pharmaceutically acceptable salt, or a solvate thereof.

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25-04-2013 дата публикации

Treatment of cancers having k-ras mutations

Номер: US20130102595A1
Принадлежит: Curis Inc

The present invention provides a method of treating a cancer associated with a K-ras mutation in a subject in need thereof. The method comprises the steps of: (1) identifying a subject with a cancer associated with a K-ras mutation; and (2) administering to the subject (i) an inhibitor of PI3 kinase and (ii) an HDAC inhibitor, wherein the PI3 kinase inhibitor and the HDAC inhibitor are administered in amounts which together are therapeutically effective.

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09-05-2013 дата публикации

NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A

Номер: US20130116233A1
Принадлежит:

The present invention relates to novel compounds of the formula I which are inhibitors of phosphodiesterase type 10A and to their use for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders. 3. The compound of claim 1 , where Xis selected from O claim 1 , S claim 1 , —X═C(R)— claim 1 , where C(R) is bound to the carbon atom which carries R.4. The compound of claim 1 , where A is selected from A claim 1 , A claim 1 , Aand A.5. The compound of claim 1 , where Xis C—R.6. The compound of claim 5 , where Ris hydrogen or Y-Cyc.7. The compound of claim 1 , where Xis N.8. The compound of claim 1 , where Xis CH.9. The compound of claim 1 , where Xis S.10. The compound of claim 1 , where Xis O.11. The compound of claim 1 , where Xis C(R)═C(R).12. The compound of claim 1 , where Xis N═(CR).13. The compound of claim 11 , where Ris hydrogen or Y-Cyc3.14. The compound of claim 1 , where Xis N═C(R).15. The compound of claim 11 , where Ris hydrogen.16. The compound of claim 1 , where Ris a radical Y-Cyc.17. The compound of claim 1 , where Ris selected from the group consisting of hydrogen claim 1 , fluorine claim 1 , C-C-alkyl claim 1 , C-C-fluoroalkyl claim 1 , C-C-alkoxy claim 1 , C-C-fluoroalkoxy claim 1 , cyclopropyl claim 1 , optionally substituted by 1 claim 1 , 2 or 3 methyl groups claim 1 , and fluorinated cyclopropyl.18. The compound of claim 17 , where Ris hydrogen.19. The compound of claim 1 , where A is A.20. The compound of claim 19 , where R claim 19 , Rare selected from hydrogen and fluorine.21. The compound of claim 19 , where Rand Rare claim 19 , independently of each other claim 19 , selected from the group consisting of hydrogen claim 19 , fluorine and methyl.22. The compound of claim 1 , where A is A.23. The compound of claim 1 , where A is ...

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09-05-2013 дата публикации

HETEROARYL PYRIDONE AND AZA-PYRIDONE COMPOUNDS

Номер: US20130116235A1
Принадлежит: Genentech, Inc.

Heteroaryl pyridone and aza-pyridone compounds of Formula I are provided, where one or two of X, X, and Xare N, and including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed. 2. The compound of wherein Xis N.3. The compound of wherein Xis N.4. The compound of wherein Xis N.5. The compound of wherein Xand Xare N claim 1 , Xand Xare N claim 1 , or Xand Xare N.6. The compound of wherein Ris optionally substituted C-Cheteroaryl selected from pyrazolyl claim 1 , pyridinyl claim 1 , pyrimidinyl claim 1 , 5-methyl-4 claim 1 ,5 claim 1 ,6 claim 1 ,7-tetrahydropyrazolo[1 claim 1 ,5-a]pyrazin-2-yl claim 1 , 5-acetyl-4 claim 1 ,5 claim 1 ,6 claim 1 ,7-tetrahydropyrazolo[1 claim 1 ,5-a]pyrazin-2-yl claim 1 , 6 claim 1 ,7-dihydro-4H-pyrazolo[5 claim 1 ,1-c][1 claim 1 ,4]oxazin-2-yl claim 1 , and 1-methyl-5-(5-(4-methylpiperazin-1-yl)pyridin-2-yl.7. The compound of wherein Ris —(C-Cheteroaryl)-(C-Cheterocyclyl) where heteroaryl is optionally substituted pyridinyl and heterocyclyl is optionally substituted piperazinyl.8. The compound of wherein Ris phenyl claim 1 , optionally substituted with one or more groups selected from F claim 1 , Cl claim 1 , —CH claim 1 , —S(O)CH claim 1 , cyclopropyl claim 1 , azetidinyl claim 1 , oxetanyl claim 1 , and morpholino.11. The compound of wherein Ris CH.12. The compound of wherein Yis CH and Yis N.13. The compound of wherein Yis N and Yis CH.14. The compound of wherein Yand Yare each CH.15. The compound of wherein Yand Yare each CH claim 1 , and Ris CH.16. The compound of selected from Table 1.17. The compound of selected from Table 218. A pharmaceutical composition comprised of a compound of and a pharmaceutically ...

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23-05-2013 дата публикации

SPIROXAZOLIDINONE COMPOUNDS

Номер: US20130131042A1
Принадлежит: Merck Sharp & Dohme Corp.

Substituted spirocyclic amines of structural formula (I) are selective antagonists of the somatostatin subtype receptor 5 (SSTR5) and are useful for the treatment, control or prevention of disorders responsive to antagonism of SSTR5, such as Type 2 diabetes, insulin resistance, lipid disorders, obesity, atherosclerosis, Metabolic Syndrome, depression, and anxiety. 2. A compound of or a pharmaceutically acceptable salt thereof claim 1 , wherein at each occurrence of Ra claim 1 , Ra is hydrogen.3. A compound of or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris phenyl.4. A compound of or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris pyridine.5. A compound of or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris substituted with OH claim 1 , —C-Calkyl claim 1 , —COOH claim 1 , COO—C-Calkyl claim 1 , —O—C-Calkyl —C-Ccycloalkyl claim 1 , —CON(C-Calkyl)NH(C-Calkyl) or heterocycle claim 1 , wherein the —C-Calkyl claim 1 , —C-Ccycloalkyl or —OC-Calkyl is unsubstituted or substituted with 1-4 substituents selected from the group consisting of halogen and —COOH.6. A compound of or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris imidazole claim 1 , naphthalene claim 1 , phenyl claim 1 , pyridine claim 1 , benzimidazole claim 1 , indole claim 1 , oxazole claim 1 , thiazole claim 1 , benzofuran claim 1 , benzocyclopentane claim 1 , benzotetrahydropyran or pyrazole.7. A compound of or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris phenyl.8. A compound of or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris pyridine.9. A compound of or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris imidazole.10. A compound of or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris substituted with two substituents independently selected from α.11. A compound of or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris substituted with three substituents ...

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13-06-2013 дата публикации

PYRAZOLOQUINOLINES

Номер: US20130150359A1

The invention relates to compounds of the formulae (I), (II) and (III), and/or physiologically acceptable salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios. The compounds of the formula (I) can be used for the inhibition of serine/threonine protein kinases and for the sensitisation of cancer cells to anticancer agents and/or ionising radiation. The invention also relates to the use of the compounds of the formula (I) in the prophylaxis, therapy or progress control of cancer, tumours, metastases or angiogenesis disorders, in combination with radiotherapy and/or an anticancer agent. The invention furthermore relates to a process for the preparation of the compounds of the formula (I) by reaction of compounds of the formula (II) or (III) and optionally conversion of a base or acid of the compounds of the formula (I) into one of its salts 7. A compound according to claim 6 , in whichR1, R2, independently of one another, denote A or -Alk-Ar,R10 denotes Hal,Alk denotes alkylene having 1-3 C atoms, in which 1-2 H atoms are optionally replaced by Hal,R4 denote Y,Y denotes H or A,A denotes unbranched or branched alkyl having 1-4 C atoms, in which, independently of one another, 1-3 H atoms are optionally replaced by Hal,Ar denotes phenyl which is unsubstituted or monosubstituted by Hal, andHal denotes F, Cl, Br or I,or a physiologically acceptable salt or tautomer thereof.11. A method for inhibiting a serine/threonine protein kinase claim 1 , a PIKK claim 1 , or DNA-PK claim 1 , comprising bringing together an effective amount of a compound of with said serine/threonine protein kinase claim 1 , a PIKK claim 1 , or DNA-PK.12. A method for sensitizing cancer cells to anticancer agents and/or ionising radiation claim 1 , comprising bringing together an effective amount of a compound of with said cancer cells with the proviso that the sensitisation does not take place in vivo on the human body.13. A pharmaceutical composition comprising a ...

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04-07-2013 дата публикации

FUSED HETEROCYCLIC COMPOUNDS

Номер: US20130172292A1
Принадлежит: Takeda Pharmaceutical Company Limited

The present invention provides a compound which has the effect of PDE 10A inhibition, and which is useful as a medicament for preventing or treating schizophrenia or so on. A compound represented by the formula (1′): wherein, Ring A′ represents an optionally substituted pyridine ring, an optionally substituted pyridazine ring, a pyrimidine ring, or 10 a pyrazine ring, R1′ represents (1) wherein, R represents an optionally substituted phenyl group, or an optionally substituted 5- to 10-membered heterocyclic group, Ring B2 represents a bond, —S—, -0-, —CO—, an optionally substituted methylene group, or —NR-(R represents a hydrogen atom, or an optionally substituted Calkyl group), and Ring B represents an optionally further substituted 6- to 10-membered aromatic hydrocarbon ring, or an optionally further substituted 5- to 10-membered aromatic heterocyclic ring, or alternatively, L′ and R may be taken together to form an optionally substituted bicyclic or tricyclic fused heterocyclic group, or (2), wherein, R represents an optionally substituted phenyl group, or an optionally substituted 5- to 10-membered heterocyclic group, Ring B represents an optionally substituted benzene ring, an optionally substituted pyridine ring, an optionally substituted pyrimidine ring, an optionally substituted pyrazine ring, or an optionally substituted pyridazine ring, Ring D′ represents an optionally further substituted 5- or 6-membered ring, R represents a hydrogen atom, or a substituent, X′ represents ═N— or ═CR—(R represents a hydrogen atom, or a substituent), - - - - - represents that R and R may form, taken together with the carbon atom and the nitrogen atom to which they are each adjacent, an optionally substituted 5- to 7-membered ring when.X′ is ═CR, or a salt thereof. 3. The compound according to claim 2 , wherein Ring A is a pyridine ring which may be substituted by substituent(s) selected from the group consisting of (i) an optionally substituted Calkyl group claim 2 , (ii) an ...

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04-07-2013 дата публикации

FUSED HETEROCYCLIC COMPOUNDS AS PHOSPHODIESTERASES (PDES) INHIBITORS

Номер: US20130172328A1
Принадлежит: CROSSWING INC.

The present invention provides a compound which has the effect of PDE inhibition, and which is useful as an agent for preventing or treating schizophrenia or so on represented by the formula (I): 2. The compound according to claim 1 , wherein any one of Zto Zis —N═ claim 1 , and the others are —CH═ claim 1 ,or a salt thereof.4. The compound according to claim 1 , wherein L is an oxygen atom claim 1 , or —NR— wherein Rrepresents a hydrogen atom or an optionally substituted Calkyl group claim 1 , or L and Rin combination optionally form an optionally substituted bi- or tri-cyclic fused heterocyclic group claim 1 ,or a salt thereof.8. The compound according to claim 1 , wherein ring Bis an optionally substituted benzene ring claim 1 , or a salt thereof.9. The compound according to claim 1 , wherein Ris a 5- to 10-membered heterocyclic group which may be substituted claim 1 , or a salt thereof.11. 1-Ethyl-6-methyl-3-{4-[(3-methyl-3H-imidazo[4 claim 1 ,5-b]pyridin-2-yl)oxy]phenyl}-1 claim 1 ,3-dihydro-2H-imidazo[4 claim 1 ,5-b]pyridin-2-one claim 1 , or a salt thereof.12. 1-Ethyl-6-methoxy-3-{4-[(3-methyl-3H-imidazo[4 claim 1 ,5-b]pyridin-2-yl)oxy]phenyl}-1 claim 1 ,3-dihydro-2H-imidazo[4 claim 1 ,5-b]pyridin-2-one claim 1 , or a salt thereof.13. 1-Ethyl-7-methyl-3-{4-[(3-methyl-3H-imidazo[4 claim 1 ,5-b]pyridin-2-yl)oxy]phenyl}-1 claim 1 ,3-dihydro-2H-imidazo[4 claim 1 ,5-b]pyridin-2-one claim 1 , or a salt thereof.14. 6-Methyl-1-(1-methylethyl)-3-{4-[(3-methyl-3H-imidazo[4 claim 1 ,5-b]pyridin-2-yl)oxy]phenyl}-1 claim 1 ,3-dihydro-2H-imidazo[4 claim 1 ,5-b]pyridin-2-one claim 1 , or a salt thereof.15. 1-Ethyl-6-fluoro-3-{4-[(3-methyl-3H-imidazo[4 claim 1 ,5-b]pyridin-2-yl)oxy]phenyl}-1 claim 1 ,3-dihydro-2H-imidazo[4 claim 1 ,5-b]pyridin-2-one claim 1 , or a salt thereof.16. 1 claim 1 ,7-Dimethyl-3-{4-[(3-methyl-3H-imidazo[4 claim 1 ,5-b]pyridin-2-yl)oxy]phenyl}-1 claim 1 ,3-dihydro-2H-imidazo[4 claim 1 ,5-b]pyridin-2-one claim 1 , or a salt thereof.17. 1-Ethyl-7-( ...

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11-07-2013 дата публикации

Cannabinoid Agonists

Номер: US20130178453A1
Принадлежит: Ironwood Pharmaceuticals Inc

The present disclosure relates to compounds useful as agonists of the cannabinoid receptors. The disclosure also provides pharmaceutically acceptable compositions comprising the compounds of the disclosure and methods of using the compositions in the treatment of various disorders, either alone or in combination therapy. The compounds of the invention have Formula (I).

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18-07-2013 дата публикации

Compositions And Methods For Treating Neoplasia, Inflammatory Disease And Other Disorders

Номер: US20130184264A1
Принадлежит: Dana Farber Cancer Institute Inc

The invention features compositions and methods for treating or preventing a neoplasia. More specifically, the invention provides compositions and methods for disrupting the interaction of a BET family polypeptide comprising a bromodomain with chromatin (e.g., disrupting a bromodomain interaction with an acetyl-lysine modification present on a histone N-terminal tail).

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01-08-2013 дата публикации

NOVEL COMPOUND OF A REVERSE-TURN MIMETIC AND A PRODUCTION METHOD AND USE THEREFOR

Номер: US20130196972A1
Принадлежит: JW Pharmaceutical Corporation

This invention relates to novel compounds of reverse-turn mimetics, having pyrazino-triazinone as a basic framework, and a method of preparing the same, and the use thereof to treat diseases such as cancer, in particular, acute myeloid leukemia. 2. The compound or pharmaceutically acceptable salt thereof of claim 1 , wherein Ris C-Calkyl group or C-Calkenyl group; and Ris H.3. The compound or pharmaceutically acceptable salt thereof of claim 1 , wherein Ris a methyl group.8. A method of treating cancer comprising administering to a subject in need thereof a pharmaceutical composition comprising a compound or a pharmaceutically acceptable salt thereof according to .9. The method of claim 8 , wherein the cancer is acute myeloid leukemia.10. A method of treating cancer comprising administering to a subject in need thereof an injectable pharmaceutical composition comprising a compound or a pharmaceutically acceptable salt thereof according to .11. The method of claim 10 , wherein the cancer is acute myeloid leukemia.12. A method of preparing the compound of claim 1 , comprising:introducing a cyano group (—CN) to position 3 of indole-7-carbaldehyde;introducing a methyl group and an aminoacetal group to the indole-7-carbaldehyde in which a cyano group (—CN) is introduced;performing stereoselective amidation with Cbz-tyrosine-OtBu and 2-(1-allyl-4-benzylsemicarbazido)acetic acid for the indole-7-carbaldehyde in which a cyano group (—CN), a methyl group and an aminoacetal group are introduced;performing cyclization using formic acid for the amidated compound; andconverting the cyano group (—CN) of the resulting compound into a carboxyl group and then performing amidation.13. A method of preparing the compound of claim 1 , comprising:iodizing indole-7-carbaldehyde so that iodine is introduced to position 3 of the indole-7-carbaldehyde;introducing a methyl group and an aminoacetal group to the indole-7-carbaldehyde in which a iodine is introduced;performing stereoselective ...

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08-08-2013 дата публикации

Formulations for organic electroluminescent devices

Номер: US20130200357A1
Принадлежит: Merck Patent GmBH

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

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08-08-2013 дата публикации

Tetracyclic compounds

Номер: US20130203746A1
Принадлежит: Medivation Technologies LLC

This disclosure relates to new tetracyclic compounds that may be used to modulate a histamine receptor in an individual. The compounds in one embodiment are tetracyclic [4,3-b]indoles. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.

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08-08-2013 дата публикации

ISOINDOLINE PDE10 INHIBITORS

Номер: US20130203756A1
Принадлежит:

The present invention is directed to isoindolinone compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction. 4. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , (1) benzimidazolyl,', '(2) imidazopyridinyl,', '(3) naphthyridinyl,', '(4) pyridopyrimidinone,', '(5) quinazolinone,', '(6) quinolinyl,', '(7) quinoxalinyl, and', '(8) tetrahydroquinolinyl., 'wherein A is selected from the group consisting of5. The compound of claim 4 , or a pharmaceutically acceptable salt thereof claim 4 , (1) benzimidazol-2-yl,', '(2) imidazo[1,2-a]pyridin-2-yl,', '(3) 1,5-naphthyridin-2-yl,', '(4) pyrido[2,3-d]pyrimidin-4(3H)-one,', '(5) quinazolin-4(3H)-one,', '(6) quinoxalin-2-yl,', '(7) quinolin-2-yl, and', '(8) 5,6,7,8-tetrahydroquinolin-2-yl., 'wherein A is selected from the group consisting of6. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 ,{'sup': 1a', '1b', '1c, 'claim-text': (1) hydrogen,', '(2) halogen,', '(3) hydroxyl,', {'sub': 1-6', '3-6, '(4) Calkyl, which is unsubstituted or substituted with Ccycloalkyl, halogen, hydroxyl, phenyl or naphthyl,'}, {'sub': '1-6', '(5) —O—Calkyl, which is unsubstituted or substituted with halogen, hydroxyl or phenyl,'}, {'sub': 3-6', '1-6, '(6) Ccycloalkyl, which is unsubstituted or substituted with Calkyl, halogen, hydroxyl, or phenyl,'}, {'sub': 1-6', '1-6', '2, '(7) heteroaryl, wherein heteroaryl is selected from pyrrolyl, imidazolyl, indolyl, pyridyl, and pyrimidinyl, which is unsubstituted or substituted with halogen, hydroxyl, Calkyl, —O—Calkyl or —NO, and'}, {'sub': 1-6', '1-6', '2, '(8) phenyl, which is unsubstituted or substituted ...

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15-08-2013 дата публикации

POSITIVE ALLOSTERIC MODULATORS OF MGLUR2

Номер: US20130210768A1
Принадлежит:

The present invention is directed to 5-substituted 1,3-dihydro-2H-imidazo[4,5-b]pyridine-2-one derivatives which are positive allosteric modulators of the mGluR2 receptor, useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 receptor is involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved, such as schizophrenia. 2. The compound according to wherein Y is methyl.3. The compound according to wherein Ris selected from the group consisting of: cyclopropylmethyl claim 1 , 2 claim 1 ,2-difluorocyclopropylmethyl claim 1 , 2 claim 1 ,2-difluoro-1-methylcyclopropylmethyl claim 1 , 1-(trifluoromethyl)cyclopropylmethyl claim 1 , 4 claim 1 ,4 claim 1 ,4-trifluoro-2 claim 1 ,2-dimethylbutyl claim 1 , cyclobutylmethyl claim 1 , 2 claim 1 ,2-dimethylpropyl claim 1 , prop-2-enyl claim 1 , biphenyl and benzyl claim 1 , optionally substituted with methoxy or —OCF.5. The compound according to wherein Ris selected from the group consisting of: halo claim 4 , —CN claim 4 , —N(O) claim 4 , amino claim 4 , —N(Calkyl) claim 4 , —C(O)—O—Calkyl claim 4 , —C(O)—Calkyl claim 4 , —S(O)—Calkyl claim 4 , Ccycloalkyl claim 4 , —C(Calkyl)-NHC(O)—O—Calkyl and Calkyl optionally substituted with 1 to 4 substituents independently selected from hydroxy and halo.7. The compound according to wherein Ris selected from the group consisting of: halo claim 6 , —CN claim 6 , —N(O) claim 6 , amino claim 6 , —N(Calkyl) claim 6 , —C(O)—O—Calkyl claim 6 , —C(O)—Calkyl claim 6 , —S(O)—Calkyl claim 6 , Ccycloalkyl and Calkyl optionally substituted with 1 to 4 substituents independently selected from hydroxy and halo.9. The compound according to wherein ring B is pyridyl.11. The compound according to wherein ring C is ...

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15-08-2013 дата публикации

2-quinolinyl-acetic acid derivatives as hiv antiviral compounds

Номер: US20130210801A1
Принадлежит: Gilead Sciences Inc

The invention provides compounds of formula (I): or a salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula (I), processes for preparing compounds of formula (I), intermediates useful for preparing compounds of formula I and therapeutic methods for treating the proliferation of the HIV virus, treating AIDS or delaying the onset of AIDS or ARC symptoms in a mammal using compounds of formula (I).

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22-08-2013 дата публикации

Tricyclic compounds and methods of use therefor

Номер: US20130217666A1
Принадлежит: Genentech Inc

The invention relates to novel compounds of Formula I: wherein A 1 , A 2 , A 3 , A 4 , A 5 , A 6 , R 2 , R 4 , R 5 , R 6 , R 7 , R 8 and subscripts m and n each has the meaning as described herein. Compounds of Formula I and pharmaceutical compositions thereof are useful in the treatment of disease and disorders in which undesired or over-activation of NF-kB signaling is observed.

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29-08-2013 дата публикации

Triazolopyrazine derivatives

Номер: US20130225568A1
Принадлежит: Merck Patent GmBH

Compounds of the formula I in which R 1 and R 2 have the meanings indicated in claim 1 , are inhibitors of Syk, and can be employed, inter alia, for the treatment of rheumatoid arthritis.

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29-08-2013 дата публикации

FUROPYRIDINE DERIVATIVES

Номер: US20130225569A1

Compounds of the formula I 2. Compounds according to in which{'sup': 1', '4, 'sub': 2', 'n', '2', 'n, 'Hetdenotes furyl, thienyl, pyrrolyl, imidazolyl, pyrazolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, pyridyl, pyrimidinyl, triazolyl, tetrazolyl, oxadiazolyl, thiadiazolyl, pyridazinyl, pyrazinyl, quinolyl, isoquinolyl, benzimidazolyl, benzotriazolyl, indolyl, benzo-1,3-dioxolyl, 2,3-dihydro-benzo[1,4]dioxinyl, indazolyl or benzothiadiazolyl, each of which is unsubstituted or mono-, di- or trisubstituted by Het, A, benzyl, (CH)OH and/or (CH)OA,'}and pharmaceutically acceptable solvates, salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios.3. Compounds according to in which{'sup': 2', '4', '4', '4, 'sub': 2', 'n', '2', 'n', '2', 'n', '2', 'n', '2', 'p', '2', 'p', '2', 'p', '2', 'p', '2', 'n', '2', 'n', '2', '2', 'n', '2', 'n', '2', '2', 'p', '2', '2', '2', '2, 'Hetdenotes piperidinyl, piperazinyl, pyrrolidinyl, morpholinyl, furyl, thienyl, pyrrolyl, imidazolyl, pyrazolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, pyridyl, pyrimidinyl, triazolyl, tetrazolyl, oxadiazolyl, thiadiazolyl, pyridazinyl, pyrazinyl, quinolyl, isoquinolyl, benzimidazolyl, benzothiophenyl, benzotriazolyl, indolyl, indolinyl, benzo-1,3-dioxolyl, 2,3-dihydro-benzo[1,4]dioxinyl, 1,3-dihydro-indolyl, 1,3-dihydrobenzimidazolyl, dihydropyranyl, 3,4-dihydro-2H-pyrano[2,3-b]pyridinyl, 1,2,3,4-tetrahydro-[1,8]naphthyridinyl, furopyridinyl, indazolyl, benzo[1,4]oxazinyl, pyrido[3,2-b][1,4]oxazinyl or benzothiadiazolyl, each of which is unsubstituted or mono-, di- or trisubstituted by Hal, (CH)Het, NH(CH)Het, OHet, A, (CH)OH, (CH)OA, (CH)CH(OH)(CH)OH, (CH)CH(OH)(CH)OA, (CH)COOA, phenyl, benzyl, CHO, COA, (CH)NH, (CH)NHA, (CH)NA, NH(CH)NH, CN, NHSOA, NASOA, SOA and/or ═O,'}and pharmaceutically acceptable solvates, salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios.4. Compounds according to in which{'sup': 3', '3, 'sub': 2', 'n', ...

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29-08-2013 дата публикации

Imidothiazole kinase inhibitors

Номер: US20130225591A1
Принадлежит: Individual

The present invention is directed to novel kinase inhibitors of general formula (I) and pharmaceutically acceptable salts thereof, and to the use of the kinase inhibitors of general formula (I) for treating diseases or disorders in which tau phosphorylation and cell cycle regulation is implicated, such as Alzheimer's Disease and cancer.

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05-09-2013 дата публикации

Spiro bicyclic diamine derivatives as hiv attachment inhibitors

Номер: US20130231324A1
Принадлежит: Bristol Myers Squibb Co

Compounds of Formula I, including pharmaceutically acceptable salts thereof: wherein A is selected from the group consisting of: are useful as HIV attachment inhibitors.

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05-09-2013 дата публикации

IMIDAZOPYRIZINE SYK INHIBITORS

Номер: US20130231330A1
Принадлежит: Gilead Connecticut, Inc.

Certain imidazopyrazines and pharmaceutical compositions thereof are provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are provided. Also provided are methods for determining the presence or absence of Syk kinase in a sample. 2: At least one chemical entity of claim 1 , wherein Ris pyridinyl substituted with one or more groups chosen fromhydroxy;{'sup': b', 'c', 'b', 'c, 'sub': 1', '6', '1', '4', '1', '4', '1', '4, '—NRRwherein Ris chosen from hydrogen and C-Calkyl optionally substituted with one or two groups chosen from hydroxy and —OC-Calkyl and Ris independently chosen from hydrogen and C-Calkyl optionally substituted with one or two groups chosen from hydroxy and —OC-Calkyl;'}{'sub': 3', '6', '1', '4', '1', '4', '1', '4', '1', '4', '1', '4', '2', '1', '4', '1', '4', '1', '4', '1', '4, 'heterocycloalkyl optionally substituted with one or two groups chosen from hydroxy, C-Ccycloalkyl, C-Calkyl, —C-Calkyl-OH, —C-Calkyl-O—C-Calkyl, —C-Calkyl-NH, —N(C-Calkyl)(C-Calkyl), —NH(C-Calkyl), and —OC-Calkyl;'}{'sub': 1', '6', '3', '6', '1', '4', '1', '4', '1', '4', '1', '4', '1', '4', '2', '1', '4', '1', '4', '1', '4', '1', '4, '—OC-Calkyl optionally substituted with one or two groups chosen from hydroxy, C-Ccycloalkyl, C-Calkyl, —C-Calkyl-OH, —C-Calkyl-O—C-Calkyl, —C-Calkyl-NH, —N(C-Calkyl)(C-Calkyl), —NH(C-Calkyl), and —OC-Calkyl;'}{'sub': 1', '6', '3', '6', '1', '4', '1', '4', '1', '4', '1', '4', '1', '4', '2', '1', '4', '1', '4', '1', '4', '1', '4, 'C-Calkyl optionally substituted with one or two groups chosen from hydroxy, C-Ccycloalkyl, C-Calkyl, —C-Calkyl-OH, —C-Calkyl-O—C-Calkyl, —C-Calkyl-NH, —N(C-Calkyl)(C-Calkyl), —NH(C-Calkyl), and —OC-Calkyl; and'}{'sub': 3', '6', '1', '4', '1', '4', '1', '4', '1', '4', '1', '4', '2', '1', ...

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12-09-2013 дата публикации

Cdk inhibitors

Номер: US20130237544A1
Принадлежит: G1 Therapeutics Inc

Compounds of formulae I, II or III, and pharmaceutically acceptable salts thereof, are useful as CDK inhibitors.

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19-09-2013 дата публикации

FUSED HETEROAROMATIC PYRROLIDINONES

Номер: US20130245031A1
Принадлежит: Takeda Phamaceutical Company Limited

Disclosed are compounds of Formula 1, 2. A method according to claim 1 , wherein Lis —NH—.34-. (canceled)5. A method according to claim 1 , wherein Lis a bond.6. (canceled)7. A method according to claim 1 , wherein G is C(R).8. A method according to claim 1 , wherein Rand Rare both hydrogen.9. A method according to claim 1 , wherein Ris Ccycloalkyl claim 1 , optionally substituted with from one to five substituents independently selected from halo claim 1 , oxo claim 1 , —NO claim 1 , —CN claim 1 , R claim 1 , and R.10. (canceled)11. A method according to claim 9 , wherein Ris 2-amino-cyclohex-1-yl optionally substituted with from one to four substituents independently selected from halo claim 9 , oxo claim 9 , —NO claim 9 , —CN claim 9 , R claim 9 , and R.1215-. (canceled)16. A method according to claim 1 , wherein Ris Cheterocyclyl optionally substituted with from one to five substituents independently selected from halo claim 1 , oxo claim 1 , —NO claim 1 , —CN claim 1 , R claim 1 , and R.17. (canceled)18. A method according to claim 16 , wherein Ris 3-aminotetrahydro-2H-pyran-4-yl optionally substituted with from one to four substituents independently selected from halo claim 16 , oxo claim 16 , —NO claim 16 , —CN claim 16 , R claim 16 , and R.1921-. (canceled)22. A method according to claim 1 , wherein Ris Cheteroaryl optionally substituted with from one to five substituents independently selected from halo claim 1 , oxo claim 1 , —CN claim 1 , R claim 1 , and R.23. A method according to claim 22 , wherein Ris a monocyclic Cheteroaryl optionally substituted with from one to four substituents independently selected from halo claim 22 , —CN claim 22 , R claim 22 , and R.24. A method according to claim 23 , wherein Ris selected from pyrrolyl claim 23 , furanyl claim 23 , thiopheneyl claim 23 , pyrazolyl claim 23 , imidazolyl claim 23 , isoxazolyl claim 23 , oxazolyl claim 23 , isothiazolyl claim 23 , and thiazolyl claim 23 , each optionally substituted with from ...

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26-09-2013 дата публикации

FUSED TRICYCLIC COMPOUNDS AS ADENOSINE RECEPTOR ANTAGONIST

Номер: US20130252885A1
Принадлежит: Advinus Therapeutics Limited

The present disclosure relates to fused tricyclic compounds of formula (I) or its tautomers, polymorphs, stereoisomers, prodrugs, solvate or a pharmaceutically acceptable salts, or pharmaceutical compositions containing them and methods of treating conditions and diseases that are mediated by thereof as A2A adenosine receptor antagonists. The compounds of the present disclosure are useful in the treatment, prevention or suppression of diseases and disorders that may be susceptible to improvement by the mediation of adenosine A2A receptor. Such conditions include, but are not limited to, Parkinsons disease, restless leg syndrome, Alzheimers disease, neurodegenerative disorder, inflammation, wound healing, dermal fibrosis, nocturnal myoclonus, cerebral ischaemia, myocardial ischemia, Huntington's disease, multiple system atrophy, corticobasal degeneration, Wilson's disease or other disorders of basal ganglia which results in dyskinesias, post traumatic stress disorder, hepatic cirrhosis, sepsis, spinal cord injury, retinopathy, hypertension, social memory impairment, depression, neuroprotection, narcolepsy or other sleep related disorders, attention deficit hyperactivity disorder, drug addiction, post traumatic stress disorder and vascular injury and the like. The present disclosure also relates to methods for the preparation of such compounds, and to pharmaceutical compositions containing them. 2. A compound of formula (I) as claimed in or its tautomers claim 1 , polymorphs claim 1 , stereoisomers claim 1 , prodrugs claim 1 , solvate or a pharmaceutically acceptable salts thereof claim 1 , wherein— represents a double bond;{'sup': 'a', 'X is selected from O, S or NR;'}{'sub': '1', 'Yis selected from N or CH;'}{'sub': '2', 'sup': 5', '5', '6, 'Yis selected from NRor CRR;'}{'sub': 3', '2, 'Yis selected from N, CH or CH;'}{'sub': '4', 'Yis selected from N or C;'}{'sup': 1', '2, 'Rand Rare independently selected from hydrogen or alkyl;'}{'sup': '3', 'claim-text': {'sup': ...

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26-09-2013 дата публикации

TRI-CYCLIC PYRAZOLOPYRIDINE KINASE INHIBITORS

Номер: US20130252939A1
Принадлежит: VERTEX PHARMACEUTICALS INCORPORATED

The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions. 2. (canceled)5. The compound of wherein:{'sub': 1', 'a', 'b, 'Ris —H, halogen, C1-C10 aliphatic optionally and independently substituted with one or more J, or C3-C8 cycloaliphatic optionally and independently substituted with one or more J; and'}{'sub': 2', 'a', 'b, 'Ris —H, halogen, C1-C10 aliphatic optionally and independently substituted with one or more J, or C3-C8 cycloaliphatic optionally and independently substituted with one or more J.'}6. The compound of wherein:{'sub': '2', 'Ris —H.'}7. The compound of wherein:{'sub': '1', 'Ris —H, halogen or C1-C10 haloalkyl.'}9. (canceled)10. (canceled)11. The compound of wherein:{'sub': 'c', 'ring B is pyrimidinyl optionally substituted with one Y and independently further and optionally and independently substituted with one or more J.'}12. The compound of wherein:{'sub': 'c', 'ring B is pyrazinyl optionally substituted with one Y and independently further and optionally and independently substituted with one or more J.'}13. The compound of wherein:{'sub': 'b', 'ring C is selected from the group consisting of cyclopropyl, cyclopentyl, cyclobutyl, cyclohexyl, cyclohexenyl, phenyl, pyridyl, pyrazinyl, pyrimidinyl, pyrrolyl, imidazolyl, pyrazolyl, oxazalolyl, oxadiazolyl, thiazolyl, thiadiazolyl, piperidinyl, piperizinyl, pyrrolidinyl, pyrazolidinyl, imidazolidinyl, azepanyl, diazepanyl, triazepanyl, azocanyl, diazocanyl, triazocanyl, indolyl, indazolyl, benzimidazolyl, quinolyl, quinoxalyl, indolinyl, oxazolidinyl, isoxazolidinyl, thiazolidinyl, isothiazolidinyl, oxazocanyl, oxazepanyl, azabicyclopentyl, azabicyclohexyl, azabicycloheptyl, azabicyclooctyl, ...

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03-10-2013 дата публикации

PYRIDAZINONES, METHOD OF MAKING, AND METHOD OF USE THEREOF

Номер: US20130261103A1
Принадлежит:

Pyridazinone compounds of Formula I including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed. 2. The compound of wherein Ris H or CH.4. The compound of wherein Ris selected from cyclopropyl claim 1 , azetidinyl claim 1 , azetidinylmethyl claim 1 , piperidinyl claim 1 , oxopiperidinyl claim 1 , piperazinyl claim 1 , and oxopiperazinyl claim 1 , optionally substituted with F claim 1 , CHor COCH.5. The compound of wherein Ris H claim 1 , t-butyl claim 1 , N-pyrrolidinyl claim 1 , N-piperidinyl claim 1 , N-azepanyl claim 1 , 2-hydroxy-2-methylpropyl claim 1 , prop-1-en-2-yl claim 1 , —N(CH)Et claim 1 , i-propyl claim 1 , cyclopentyl claim 1 , cyclohexyl claim 1 , 3-methylbutan-2-yl claim 1 , —N(CH)(i-Pr) claim 1 , or —NH(cyclopropyl).6. The compound of wherein Ris H or F.7. The compound of wherein Ris H claim 1 , CH claim 1 , F claim 1 , or CHOH.8. The compound of wherein Ris H or F.9. The compound of wherein B is pyrazolo[1 claim 1 ,5-a]pyrazin-2-yl claim 1 , pyrazol-3-yl claim 1 , pyrimidin-4-yl claim 1 , or pyridin-2-yl.14. The compound of chosen from Table 1.15. The compound of chosen from Table 2.16. A pharmaceutical composition comprised of a compound of and a pharmaceutically acceptable carrier claim 1 , glidant claim 1 , diluent claim 1 , or excipient.17. The pharmaceutical composition according to claim 16 , further comprising a second therapeutic agent.18. A process for making a pharmaceutical composition which comprises combining a compound of with a pharmaceutically acceptable carrier.19. A method of treating a disease or disorder which comprises administering a therapeutically effective amount of a compound of to a patient with a ...

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10-10-2013 дата публикации

Fused heterocyclic azaindane carboxamide cgrp receptor antagonists

Номер: US20130267541A1
Принадлежит: Individual

The present invention is directed to fused heterocyclic azaindane carboxamide derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.

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17-10-2013 дата публикации

COMPOUNDS AND METHODS FOR ANTIVIRAL TREATMENT

Номер: US20130273037A1
Принадлежит:

Compounds and pharmaceutically acceptable salts and esters and compositions thereof, for treating viral infections are provided. The compounds and compositions are useful for treating Pneumovirinae virus infections. The compounds, compositions, and methods provided are particularly useful for the treatment of Human respiratory syncytial virus infections. 2. The compound of wherein:{'sup': 1', '2', '3', '8′', '4', '5', '2′', '2', '1', '2', '3', '4', '5', '2′, 'a) Yis N, NH or CH, Yis C, Yis N or CR, Yis N or C and Yis N, NR or CR, wherein at least two of Y, Y, Y, Yand Yare independently N, NH or NR; or'}{'sup': 1', '2', '3', '8′', '4', '5', '2′', '1', '2', '3', '4', '5', '2′, 'b) Yis N, NH or CH, Yis N or C, Yis N or CR, Yis N or C, and Yis N or NR, wherein at least two of Y, Y, Y, Yand Yare independently N, NH or NR; or'}{'sup': 1', '2', '3', '8′', '4', '5', '2′', '2', '1', '2', '3', '4', '5', '2′, 'c) Yis N, NH or CH, Yis N or C, Yis CR, Yis N or C, and Yis N, NR or CR, wherein at least two of Y, Y, Y, Yand Yare independently N, NH or NR;'}the dashed bonds ---- are selected from single bonds and double bonds so as to provide an aromatic ring system;{'sup': 4', '4′', '4', '4′', '4', '4′', 'a, 'sub': n', 'n', 'p, 'A is —(CRR)— wherein any one CRR of said —(CRR)— may be optionally replaced with —O—, —S—, —S(O)—, NH or NR;'}n is 3, 4, 5 or 6;each p is 1 or 2;{'sub': 2', '20', '6', '20', '2', '20', '6', '20, 'sup': '6', 'Ar is a C-Cheterocyclyl group or a C-Caryl group, wherein the C-Cheterocyclyl group or the C-Caryl group is optionally substituted with 1 to 5 R;'}{'sup': 13', '14', '14, 'sub': '2', 'X is —C(R)(R)—, —N(CHR)— or —NH—, or X is absent;'}{'sup': 1', '11', '11', '12', '11', '11', '11', '11', '11', '11', '12', '11', 'a', '11', 'a', '11', '11', '11', '12', '11', '11', '11', '12', '11', '11', '11', '11', '12', '11', '11', '11', '12, 'sub': 3', '2', 'p', 'p', 'p', '2', 'p', 'p', '1', '8', '2', '8', '2', '8', '1', '8', '6', '20', '2', '20', '2', '20', '1', '8', ...

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17-10-2013 дата публикации

IAP INHIBITORS

Номер: US20130274278A1
Принадлежит:

The present invention describes compounds, processes for their preparation, pharmaceutical compositions containing them, and their use in therapy. 2. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein:R is selected from H; alkyl; substituted alkyl; alkenyl; substituted alkenyl; aryl; substituted aryl; cycloalkyl; substituted cycloalkyl; heteroaryl; or substituted heteroaryl; wherein the alkyl, alkenyl, aryl, cycloalkyl, and heteroaryl substitutents are selected from the group consisting of halogen, hydroxy, oxo, mercapto, carboxyl, alkyl, cycloalkyl, aryl, alkoxy, amino, heteroaryl, and nitro;R1a and R1b are each independently selected from H; alkyl; or substituted alkyl; wherein the alkyl substitutents are selected from the group consisting of halogen, hydroxy, oxo, mercapto, carboxyl, cycloalkyl, aryl, alkoxy, amino, heteroaryl, and nitro;R2 is selected from alkyl; substituted alkyl, wherein the alkyl substituents are selected from the group consisting of halogen, hydroxy, oxo, alkoxy, cycloalkyl, aryl, heterocycloalkyl and heteroaryl; cycloalkyl; substituted cycloalkyl, wherein the cycloalkyl substituents are selected from the group consisting of halogen, hydroxy, oxo, mercapto, carboxyl, alkyl, cycloalkyl, aryl, alkoxy, amino, heteroaryl, and nitro; aryl; substituted aryl, wherein the aryl substituents are selected from the group consisting of alkyl, halogen, hydroxy, mercapto, carboxyl, cycloalkyl, aryl, alkoxy, amino, heteroaryl, nitro, alkylsulfonyl and arylsulfonyl; heterocycloalkyl; substituted heterocycloalkyl, wherein the heterocycloalkyl substituents are selected from the group consisting of halogen, hydroxy, mercapto, carboxyl, alkyl, cycloalkyl, aryl, alkoxy, amino, heteroaryl, and nitro; heteroaryl, or substituted heteroaryl wherein the heteroaryl substituents are selected from the group consisting of halogen, hydroxy, mercapto, carboxyl, alkyl, cycloalkyl, aryl, alkoxy, amino, heteroaryl, and nitro;R4 and R5 are ...

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31-10-2013 дата публикации

PYRAZINO[2,3-b]PYRAZINE mTOR KINASE INHIBITORS FOR ONCOLOGY INDICATIONS AND DISEASES ASSOCIATED WITH THE mTOR/PI3K/AKT PATHWAY

Номер: US20130289271A1
Принадлежит: Signal Pharmaceuticals LLC

Provided herein are Heteroaryl Compounds having the following structure: wherein R 1 -R 4 are as defined herein, compositions comprising an effective amount of a Heteroaryl Compound and methods for treating or preventing cancer, inflammatory conditions, immunological conditions, neurodegenerative diseases, diabetes, obesity, neurological disorders, age-related diseases, or cardiovascular conditions, comprising administering an effective amount of a Heteroaryl Compound to a patient in need thereof.

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07-11-2013 дата публикации

1h-pyrazolo[3,4-b]pyridines and therapeutic uses thereof

Номер: US20130296307A1
Принадлежит: Samumed LLC

Provided herein are compounds according to Formula I and pharmaceutically acceptable salts thereof, and compositions comprising the same, for use in various methods, including treating cancers such as colon, ovarian, pancreatic, breast, liver, prostate and hematologic cancers:

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07-11-2013 дата публикации

N1-PYRAZOLOSPIROKETONE ACETYL-CoA CARBOXYLASE INHIBITORS

Номер: US20130296319A1
Принадлежит:

The invention provides a compound of Formula (I) 2. The compound according to wherein Ris (C-C)alkyl claim 1 , (C-C)cycloalkyl claim 1 , or tetrahydrofuranyl; and Ris hydrogen or methyl.3. The compound according to wherein Ris isopropyl or t-butyl; Ris hydrogen; and each Ris hydrogen.4. A pharmaceutical composition comprising a therapeutically effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , and a pharmaceutically acceptable excipient claim 1 , diluent or carrier. This application is a continuation of U.S. application Ser. No. 13/644,415 filed Oct. 4, 2012, which is a continuation of U.S. application Ser. No. 12/941,133 filed Nov. 8, 2010, now granted U.S. Pat. No. 8,288,405, which claims the benefit of priority from U.S. Provisional Application No. 61/259,823 filed Nov. 10, 2009, each of which are herein incorporated by reference.This invention relates to substituted pyrazolospiroketone compounds that act as inhibitors of an acetyl-CoA carboxylase(s) and their use in treating diseases, conditions or disorders modulated by the inhibition of acetyl-CoA carboxylase enzyme(s).Acetyl-CoA carboxylases (ACC) are a family of enzymes found in most species and are associated with fatty acid synthesis and metabolism through catalyzing the production of malonyl-CoA from acetyl-CoA. In mammals, two isoforms of the ACC enzyme have been identified. ACC1, which is expressed at high levels in lipogenic tissues, such as fat and the liver, controls the first committed step in the biosynthesis of long-chain fatty acids. If acetyl-CoA is not carboxylated to form malonyl-CoA, it is metabolized through the Krebs cycle. ACC2, a minor component of hepatic ACC but the predominant isoform in heart and skeletal muscle, catalyzes the production of malonyl-CoA at the cytosolic surface of mitochondria, and regulates how much fatty acid is utilized in β-oxidation by inhibiting carnitine palmitoyl transferase. Thus, by increasing fatty acid ...

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07-11-2013 дата публикации

Quinoxaline compound

Номер: US20130296329A1
Принадлежит: Astellas Pharma Inc

The present inventors have investigated a compound which has a PDE9-inhibitory action and is useful as an active ingredient for an agent for treating and/or preventing storage dysfunction, voiding dysfunction, and bladder/urethral diseases, and the like, and thus, have found that an imidazoquinoxaline compound or a triazoloquinoxaline compound has a PDE9-inhibitory action, thereby completing the present invention.

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14-11-2013 дата публикации

Fused heterocyclic derivatives and methods of use

Номер: US20130303529A1
Принадлежит: AMGEN INC

Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

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14-11-2013 дата публикации

Fused heterocyclic compounds

Номер: US20130303553A1
Принадлежит: Takeda Pharmaceutical Co Ltd

The present invention provides a compound which has the effect of PDE inhibition, and which is useful as an agent for preventing or treating schizophrenia. The compound is represented by the formula (I): wherein the symbols are defined in the specification.

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21-11-2013 дата публикации

7-AZAINDOLE DERIVATIVES

Номер: US20130310391A1
Принадлежит: Merck Patent GmBH

Compounds of the formula (I) in which R, R, Rand Rhave the meanings indicated in Claim , are inhibitors of PDK1 and cell proliferation/cell vitality and can be employed for the treatment of tumours. 2. Compounds according to in which{'sup': '2', 'Rdenotes H, benzyl or A′, and pharmaceutically usable salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios.'}3. Compounds according to in which{'sup': 3', '6, 'sub': 2', 'n, 'Rdenotes H, A or —[C(R)]-Het, and pharmaceutically usable salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios.'}12. Medicaments comprising at least one compound of the formula I according to and/or pharmaceutically usable salts claim 1 , tautomers and stereoisomers thereof claim 1 , including mixtures thereof in all ratios claim 1 , and optionally excipients and/or adjuvants.13. Compounds of the formula I according to and pharmaceutically usable salts claim 1 , tautomers and stereoisomers thereof claim 1 , including mixtures thereof in all ratios claim 1 , for use for the treatment of tumours claim 1 , tumour growth claim 1 , tumour metastases and/or AIDS.14. Compounds of the formula I according to and/or physiologically acceptable salts claim 1 , tautomers and stereoisomers thereof for use for the treatment of tumours claim 1 , where a therapeutically effective amount of a compound of the formula I is administered in combination with a compound from the group 1) oestrogen receptor modulator claim 1 , 2) androgen receptor modulator claim 1 , 3) retinoid receptor modulator claim 1 , 4) cytotoxic agent claim 1 , 5) antiproliferative agent claim 1 , 6) prenyl-protein transferase inhibitor claim 1 , 7) HMG-CoA reductase inhibitor claim 1 , 8) HIV protease inhibitor claim 1 , 9) reverse transcriptase inhibitor and 10) further angiogenesis inhibitors.15. Compounds of the formula I according to and/or physiologically acceptable salts claim 1 , tautomers and stereoisomers thereof for use for the ...

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21-11-2013 дата публикации

Inhibitors of hcv ns5a protein

Номер: US20130310427A1
Автор: Leping Li, Min Zhong
Принадлежит: Presidio Pharmaceuticals Inc

Antiviral compounds may be used to inhibit or reduce the activity of Hepatitis C virus (HCV), particularly HCV's NS5A protein. In these contexts, inhibition and reduction of activity of the NS5A protein refers to a lower level of the measured activity relative to a control experiment in which the cells or the subjects are not treated with the test compound. The inhibition or reduction in the measured activity is at least a 10% reduction or inhibition. The compounds and their isomeric forms and pharmaceutically acceptable salts thereof are useful in treating and preventing HCV infection alone or when used in combination with other compounds targeting viral or cellular elements or functions involved in the HCV lifecycle.

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05-12-2013 дата публикации

Porphyrin compounds comprising one or more pyridone moieties

Номер: US20130324714A1
Принадлежит: VENTANA RESEARCH Corp

Various porphyrin compounds comprising one or more pyridone moieties, intermediates thereof, compositions thereof, and, methods of making and using thereof.

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12-12-2013 дата публикации

COMPOSITIONS AND METHODS FOR MODULATING FXR

Номер: US20130331349A1
Принадлежит:

The present invention relates to compounds of Formula (I), a stereoisomer, enantiomer, a pharmaceutically acceptable salt or an amino acid conjugate thereof; wherein variables are as defined herein; and their pharmaceutical compositions, which are useful as modulators of the activity of Farnesiod X receptors (FXR). 2. The compound of claim 1 , wherein Ris cyclopropyl.3. The compound of claim 1 , wherein Z is phenylene claim 1 , pyridylene claim 1 , pyrimidinylene claim 1 , pyrazinylene claim 1 , pyridazinylene claim 1 , thiazolylene claim 1 , benzothiazolyl claim 1 , benzo[d]isothiazolyl claim 1 , imidazo[1 claim 1 ,2-a]pyridinyl claim 1 , quinolinyl claim 1 , 1H-indolyl claim 1 , pyrrolo[1 claim 1 ,2-b]pyridazinyl claim 1 , benzofuranyl claim 1 , benzo[b]thiophenyl claim 1 , 1H-indazolyl claim 1 , benzo[d]isoxazolyl claim 1 , quinazolinyl claim 1 , 1H-pyrrolo[3 claim 1 ,2-c]pyridinyl claim 1 , pyrazolo[1 claim 1 ,5-a]pyrimidinyl claim 1 , imidazo[1 claim 1 ,2-b]pyridazinyl claim 1 , pyrazolo[1 claim 1 ,5-a]pyridinyl; each of which is optionally substituted with 1-2 Rradicals selected from halogen claim 1 , Calkyl claim 1 , haloCalkyl claim 1 , Calkoxy claim 1 , haloCalkoxy claim 1 , or cyclopropyl.7. The compound of claim 1 , wherein Ris phenyl substituted with 1-3 R; and{'sup': '1a', 'sub': 1-6', '1-6', '1-6', '1-6, 'Ris halogen, Calkyl, haloCalkyl, Calkoxy, haloCalkoxy.'}8. The compound of claim 1 , wherein Ris —X—COR; X is a bond and Ris hydrogen or Calkyl.9. The compound of claim 1 ,{'sup': '6', 'wherein Ris methyl, methoxy, fluoro or trifluoromethoxy.'}10. The compound of claim 1 , wherein said compound is selected frommethyl 2-[3-({5-cyclopropyl-3-[2-(trifluoromethoxy)phenyl]-1,2-oxazol-4-yl}methoxy)-8-azabicyclo[3.2.1]octan-8-yl]-4-fluoro-1,3-benzothiazole-6-carboxylate;methyl 2-[(1R,3r,5S)-3-({5-cyclopropyl-3-[2-(trifluoromethoxy)phenyl]-1,2-oxazol-4-yl}methoxy)-8-azabicyclo[3.2.1]octan-8-yl]-4-fluoro-1,3-benzothiazole-6-carboxylate;2-[3-({5-cyclopropyl-3-[ ...

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12-12-2013 дата публикации

Protein Kinase C Inhibitors and Uses Thereof

Номер: US20130331374A1
Принадлежит:

This disclosure concerns compounds which are useful as inhibitors of protein kinase C (PKC) and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC. This disclosure also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes. 2. The compound of claim 1 , wherein G is —NYAr.3. The compound of claim 1 , wherein G is halogen.4. The compound of claim 1 , wherein Aris aryl or substituted aryl.5. The compound of claim 1 , wherein Aris heteroaryl or substituted heteroaryl.10. The compound of claim 7 , wherein the compound is optically active.11. The compound of claim 10 , having an enantiomeric excess of 90% or more.12. The compound of claim 11 , wherein the enantiomeric excess is 95% or more.13. The compound of claim 11 , wherein the enantiomeric excess is 99% or more.15. The compound of claim 14 , wherein Q is C.16. The compound of claim 14 , wherein Q is N.17. The compound of claim 14 , wherein R claim 14 , R claim 14 , R claim 14 , R claim 14 , and Rare independently selected from hydrogen claim 14 , alkyl claim 14 , substituted alkyl claim 14 , halogen claim 14 , cyano claim 14 , hydroxyl claim 14 , alkoxy claim 14 , substituted alkoxy claim 14 , amino claim 14 , substituted amino claim 14 , acylamino claim 14 , aminocarbonylamino claim 14 , acyl claim 14 , aminoacyl claim 14 , aminocarbonyloxy claim 14 , sulfur pentafluoride claim 14 , aryl claim 14 , substituted aryl claim 14 , cycloalkyl claim 14 , substituted cycloalkyl claim 14 , heteroaryl claim 14 , substituted heteroaryl claim 14 , heterocyclyl claim 14 , substituted heterocyclyl claim 14 , heterocyclyloxy claim 14 , and substituted heterocyclyloxy claim 14 , or Rand Rtogether with the carbon atoms to which they are attached form aryl claim 14 , substituted aryl ...

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19-12-2013 дата публикации

Substituted annellated pyrimidines and use thereof

Номер: US20130338137A1
Принадлежит: Bayer Intellectual Property GmbH

The present application relates to novel substituted annellated pyrimidines, methods for production thereof, use thereof alone or in combinations for treating and/or preventing diseases and use thereof for the production of medicinal products for treating and/or preventing diseases, in particular for treating and/or preventing cardiovascular diseases.

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26-12-2013 дата публикации

SUBSTITUTED ADIPIC ACID AMIDES AND USES THEREOF

Номер: US20130345123A1
Принадлежит: BRISTOL-MYERS SQUIBB COMPANY

The present invention provides compounds of Formula (I), or a pharmaceutically acceptable salt thereof, wherein A is a five to eight membered monocyclic or a nine to twelve membered bicyclic heterocyclic ring, as further defined herein; Y is S, CH, or CH; Z is CH or N; Rand Rare hydrogen or (C-C)alkyl; Ris (C-C)alkoxy, OH, CN, (C-C)alkyl, halogen, or CF; r and s are 0, 1, or 2; and Rand Rare as further defined herein. These compounds are agonists, partial agonists and/or modulators of the NPY4 receptor and may be used for the treatment and prophylaxis of obesity, food intake, and other diseases and conditions modulated by the NPY4 receptor. 7. The compound according to claim 6 , wherein:X is S;{'sup': 5', '6, 'sub': 'm', 'Q is (CRR);'}{'sup': '1', 'sub': 2', '1', '3', '1', '4, 'Ris —CH-phenyl, wherein the phenyl is optionally substituted with halogen, (C-C)alkyl, and (C-C)alkoxyl;'}{'sup': 3a', '4a, 'sub': '3', 'Rand Rare independently hydrogen or COOCH;'}{'sup': 3b', '4b, 'sub': '3', 'Rand Rare each either hydrogen or CF;'}{'sup': 5', '6, 'sub': '3', 'Rand Rare each hydrogen or CH;'}m is 2; andt is 1.9. The compound according to claim 8 , wherein:{'sup': '1', 'sub': 2', '1', '3', '1', '4, 'Ris —CH-phenyl, wherein the phenyl is optionally substituted with one of halogen, (C-C)alkyl, or (C-C)alkoxyl;'}{'sup': '3a', 'sub': '3', 'Ris independently hydrogen or CF;'}{'sup': '3b', 'sub': '3', 'Ris independently hydrogen or CF; and'}{'sup': '10', 'sub': '3', 'Ris phenyl optionally substituted with —OCH.'}12. The compound according to claim 11 , wherein:{'sup': '3a', 'sub': 3', '3', '2', '3', '3, 'Ris hydrogen, CN, CF, CH,CHCH, propylene, or COOCH; and'}{'sup': '10', 'sub': 3', '3, 'Ris isobutyl, phenyl, or benzyl, wherein the phenyl or benzyl optionally are substituted ortho with —CHor —OCH.'}1312. A pharmaceutical composition comprising one or more compounds according to any one of through claims 1 , and a pharmaceutically acceptable carrier.14. Use of a composition ...

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26-12-2013 дата публикации

Heterocyclic tyrosine kinase inhibitors

Номер: US20130345192A1

The present invention provides compounds useful as inhibitors of Tec family kinases, compositions thereof, and methods of using the same.

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02-01-2014 дата публикации

Aromatic heterocyclic derivative, material for organic eletroluminescent element, and organic electroluminescent element

Номер: US20140001456A1
Принадлежит: Idemitsu Kosan Co Ltd

An organic EL device includes an anode, an emitting layer, an electron transporting zone and a cathode in this sequence, in which the electron transporting zone contains an aromatic heterocyclic derivative represented by a formula (1) below. In the formula (1), X 1 to X 3 are a nitrogen atom or CR 1 , and A is represented by a formula (2) below. In the formula (2), L 1 is s single bond or a linking group, and HAr is represented by a formula (3) below. In the formula (3), Y 1 is an oxygen atom, a sulfur atom or the like, and one of X 11 to X 18 is a carbon atom bonded to L 1 by a single bond and the rest of X 11 to X 18 are a nitrogen atom or CR 13 .

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02-01-2014 дата публикации

Aryl Methyl Benzoquinazolinone M1 Receptor Positive Allosteric Modulators

Номер: US20140005182A1
Принадлежит: Merck Sharp & Dohme Corp.

The present invention is directed to benzoquinazilinone compounds of formula (I) 126-. (canceled)28. A compound of claim 27 , or a pharmaceutically acceptable salt thereof claim 27 , wherein:Q is C, X and Y are each CH and Z is N;X, Y and Z are each CH, and Q is C, orX and Z are each CH, Q is C and Y is N.30. A compound of claim 27 , or a pharmaceutically acceptable salt thereof claim 27 , wherein Ris:{'sub': '3-8', 'claim-text': (a) hydroxy,', {'sub': '1-6', '(b) —O—Calkyl, or'}, '(c) oxo., '(1) —Ccycloalkyl, optionally substituted with one or more'}(2) aryl,(3) heteroaryl, or{'sub': '1-6', 'claim-text': (a) halogen,', '(b) hydroxy,', {'sub': '1-6', '(c) —O—Calkyl,'}, {'sub': '1-6', '(d) —Calkyl,'}, '(e) —CN,', {'sub': 'm', 'sup': '6', '(f) —C(═O)—(O)—R,'}, {'sup': 5A', '5B, '(g) —NRR,'}, '(h) oxo,', '(i) aryl, and', '(j) heteroaryl., '(4) —Calkyl, wherein said aryl, heteroaryl or alkyl is optionally substituted with one or more'}31. A compound of or a pharmaceutically acceptable salt thereof claim 27 , wherein Ris hydrogen.32. A compound of claim 27 , or a pharmaceutically acceptable salt thereof claim 27 , which is selected from the group consisting ofrac-3-[trans-2-hydroxycyclohexyl]-6-[(6-methylpyridin-3-yl)methyl]benzo[h]quinazolin-4(3H)-one;3-[(1S,2S)-2-hydroxycyclohexyl]-6-[(6-methylpyridin-3-yl)methyl]benzo[h]quinazolin-4(3H)-one;6-(4-methoxybenzyl)-3-(5-methyl)-1H-pyrazol-3-yl)benzo[h]quinazolin-4(3H)-one;6-(4-methoxybenzyl)-3-pyridin-3-ylbenzo[h]quinazolin-4(3H)-one;rac-3-[trans-2-hydroxycyclohexyl]-6-{[6-(1-methyl-1H-pyrazol-4-yl)pyridine-3-yl]methyl}benzo[h]quinazolin-4(3H)-one;rac-3-[trans-2-hydroxycyclohexyl]-6-{[6-(1H-pyrazol-1-yl)pyridin-3-yl]methyl}benzo[h]quinazolin-4(3H)-one;rac-5-({3-[trans-2-hydroxycyclohexyl]-4-oxo-3,4-dihydrobenzo[h]quinazolin-6-yl}methyl)pyridine-2-carbonitrile;rac-3-[trans-2-hydroxycyclohexyl]-6-{[6-methylsulfonyl)pyridine-3-yl]methyl}benzo[h]quinazolin-4(3H)-one;rac-3-[trans-2-hydroxycyclohexyl]-6-[(6-methoxypyridin-3-yl) ...

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02-01-2014 дата публикации

Novel 4-(Substituted Amino)-7H-Pyrrolo[2,3-d] Pyrimidines As LRRK2 Inhibitors

Номер: US20140005183A1
Принадлежит:

The present invention provides novel 4,5-disubstituted-7H-pyrrolo[2,3-d]pyrimidine derivatives of Formula I, and the pharmaceutically acceptable salts thereof 2. The compound of wherein Rand Rare each hydrogen; or a pharmaceutically acceptable salt thereof.4. The compound of wherein Rand Rtaken together with the substituted with a hydroxy claim 3 , methyl or 5-methyl-1 claim 3 ,2 claim 3 ,4-oxadiazol-3-yl; or a pharmaceutically acceptable salt thereof.5. The compound of wherein Rand Rtaken together with the nitrogen to which they are attached are morpholin-4-yl optionally substituted with a methyl or 5-methyl-1 claim 4 ,2 claim 4 ,4-oxadiazol-3-yl; or a pharmaceutically acceptable salt thereof.6. The compound of wherein Rand Rtaken together with the nitrogen to which they are attached are methylamino claim 2 , dimethylamino claim 2 , diethylamino claim 2 , N-methylcyclopropylamino or pyrazolylamino; each of which is optionally substituted with one to three R; or a pharmaceutically acceptable salt thereof.7. The compound of wherein Ris phenyl substituted with one or two R; and each Ris independently selected from cyano claim 3 , fluoro claim 3 , chloro or methoxy; or a pharmaceutically acceptable salt thereof.8. The compound of wherein Ris pyrazolyl claim 3 , isothiazolyl claim 3 , or pyridinyl claim 3 , each optionally substituted with one R; and Ris cyano or methyl; or a pharmaceutically acceptable salt thereof.12. The compound of wherein{'sup': '3', 'Ris 3-cyanophenyl, 1-methylpyrazol-4-yl or 5-cyano-1-methylpyrrol-3-yl;'}or a pharmaceutically acceptable salt thereof.13. The compound of wherein{'sup': 1', '2, 'Rand Rtaken together with the nitrogen to which they are attached are piperidinyl or 3-hydroxypiperidinyl;'}{'sup': '3', 'Ris 1-methylpyrazol-4-yl, 1H-pyrazol-4-yl, 2-cyanopyridin-6-yl, 3-methyl-1,2-thiazol-5-yl, 3-methylpyridin-5-yl, 3-cyanophenyl, 2-fluorophenyl, 3-fluorophenyl, 2,3-difluorophenyl, 2-fluoro-5-chlorophenyl, 2-fluoro-3-cyanophenyl or 2- ...

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02-01-2014 дата публикации

Tricyclic imidazole compounds as PDE10 inhibitors

Номер: US20140005201A1
Принадлежит: H Lundbeck AS

This invention is directed to compounds, which are PDE10A enzyme inhibitors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The present invention also provides processes for the preparation of the compounds of formula I. The present invention further provides a method of treating a subject suffering from a neurodegenerative disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention also provides a method of treating a subject suffering from a drug addiction comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention further provides a method of treating a subject suffering from a psychiatric disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I.

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23-01-2014 дата публикации

5-ht3 receptor antagonists

Номер: US20140024644A1

The present invention provides 5-HT3 receptor antagonists of Formula (I): which are useful for the treatment of diseases treatable by inhibition of 5-HT3 receptor such as emesis, pain, drug addiction, neurodegenerative and psychiatric disorders, and GI disorders. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.

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06-02-2014 дата публикации

Ring-fused heterocyclic derivative

Номер: US20140038941A1
Принадлежит: Kyowa Hakko Kirin Co Ltd

A ring-fused heterocyclic derivative represented by the following general formula (I) or a pharmaceutically acceptable salt thereof having a T-type calcium channel regulatory effect and useful as a pruritus therapeutic and/or preventive agent, and the like are provided. In the general formula (I), R 1 represents optionally substituted lower alkyl, and the like; R 2 represents an optionally substituted cycloalkyl, and the like; Q represents a hydrogen atom, and the like; R 3 represents —C(═O)NR 8 R 9 (wherein R 8 and R 9 may be the same or different, and each represents a hydrogen atom, and the like), and the like; L 1 represents —CR 11A R 11B — (wherein R 11A and R 11B may be the same or different, and each represents a hydrogen atom, and the like), and the like; and W 1 and W 2 may be the same or different, and each represents C—R 12 (wherein R 12 represents a hydrogen atom, and the like), and the like.

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06-02-2014 дата публикации

NOVEL ISO-ERGOLINE DERIVATIVES

Номер: US20140039188A1
Автор: Cook Robert O., Zhang Jian
Принадлежит: MAP Pharmaceuticals, Inc.

Provided herein are novel iso-ergoline derivatives and compositions thereof. In other embodiments, provided herein are methods of treatment, prevention, or amelioration of a variety of medical disorders such as, for example, migraine using the compounds and compositions disclosed herein. In still other embodiments, provided herein are methods of agonizing receptors such as, for example, the 5-HTand/or the 5-HTreceptor, without agonizing the 5-HTreceptor using the compounds and compositions disclosed herein. In still other embodiments, provided herein are methods of antagonizing or inhibiting activity at receptors such as, for example, the adrenergic alphaand/or the alphareceptors using the compounds and compositions disclosed herein. 2. The compound of claim 1 , wherein Ris hydrogen or (C-C) alkyl substituted with one or more fluorine atoms claim 1 , n is 0 claim 1 , Ris hydrogen or (C-C) alkyl claim 1 , Ris substituted alkyl or —NRR claim 1 , Ris methyl substituted with one or more fluorine atoms and Ris hydrogen claim 1 , substituted alkyl claim 1 , substituted acyl or —CONRR.3. The compound of claim 1 , wherein Ris hydrogen claim 1 , methyl or methyl substituted with one or more fluorine atoms claim 1 , Ris alkyl claim 1 , halo claim 1 , —OR claim 1 , n is 1 claim 1 , Ris hydrogen claim 1 , methyl or allyl claim 1 , Ris substituted alkyl or —NRR claim 1 , Ris methyl substituted with one or more fluorine atoms and Ris hydrogen claim 1 , substituted alkyl claim 1 , substituted acyl or —CONRR.4. The compound of claim 1 , wherein Ris hydrogen claim 1 , methyl or methyl substituted with one or more fluorine atoms claim 1 , n is 0 claim 1 , Ris hydrogen claim 1 , methyl or allyl claim 1 , Ris substituted alkyl or —NRR claim 1 , Ris methyl substituted with one or more fluorine atoms and Ris hydrogen claim 1 , substituted alkyl claim 1 , substituted acyl or —CONRR.9. The compound of claim 1 , wherein Ris hydrogen claim 1 , n is 0 claim 1 , Ris allyl claim 1 , Ris —NRRor ...

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13-02-2014 дата публикации

Pyrazine derivatives as fgfr inhibitors

Номер: US20140045814A1
Принадлежит: Incyte Corp

The present invention relates to pyrazine derivatives, and pharmaceutical compositions including the same, that are inhibitors of one or more FGFR enzymes and are useful in the treatment of FGFR-associated diseases such as cancer.

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13-02-2014 дата публикации

Aldosterone synthase inhibitors

Номер: US20140045819A1
Принадлежит: ElexoPharm GmbH, Schering Corp

This invention relates to tricyclic triazole analogues of the formula I or their pharmaceutically acceptable salts, wherein the variable are defined herein. The inventive compounds selectively inhibit aldosterone synthetase. This invention also provides for pharmaceutical compositions comprising the compounds of Formula I or their salts as well as to methods for the treatment, amelioration or prevention of conditions that could be treated by inhibiting aldosterone synthetase.

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13-02-2014 дата публикации

NOVEL ANTIFUNGAL 5,6-DIHYDRO-4H-PYRROLO[1,2-a][1,4]BENZO-DIAZEPINES AND 6H-PYRROLO[1,2-a][1,4]BENZODIAZEPINES SUBSTITUTED WITH HETEROCYCLIC DERIVATIVES

Номер: US20140045827A1
Принадлежит: Janssen Pharmaceutica NV

The present invention is concerned with novel antifungal 5,6-dihydro-4H-pyrrolo-[1,2-a][1,4]benzodiazepines and 6H-pyrrolo[1,2-a][1,4]benzodiazepines substituted with heterocyclic derivatives of Formula (I) wherein R 1 , R 2 , R 3 , R 4 and Het have the meaning defined in the claims. The compounds according to the present invention are active mainly against dermatophytes and systemic fungal infections. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.

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13-02-2014 дата публикации

Compounds and methods for inhibiting mitotic progression

Номер: US20140046055A1
Принадлежит: Millennium Pharmaceuticals Inc

This invention relates to compounds and methods for the treatment of cancer. In particular, the invention provides compounds that inhibit Aurora kinase, pharmaceutical compositions comprising the compounds, and methods of using the compounds for the treatment of cancer.

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20-02-2014 дата публикации

Polycyclic Agents for the Treatment of Respiratory Syncytial Virus Infections

Номер: US20140051689A1
Принадлежит: Biota Scientific Management Pty Ltd.

Compounds of formula (I), and their use as in the treatment of infections involving viruses of the Pneumovirinae sub-family (RSV) are disclosed. In the formula ring (A) may be phenyl, pyridyl etc., (B-C) may be CH—CHetc., (R) may be phenyl and substituted forms thereof, (R) may be assorted substituents. 2. The method according to wherein Ris not an unsubstituted —Calkyl or unsubstituted —C(O)—Calkyl.3. The method according to wherein ring A is an optionally substituted aryl ring.4. The method according to wherein ring A is an optionally substituted phenyl ring.5. The method according to wherein ring A is an optionally substituted heteroaryl ring.6. The method according to wherein ring A together with the atoms to which it is attached claim 1 , represents an optionally substituted pyridyl claim 1 , pyridazinyl claim 1 , pyrimidinyl claim 1 , pyrazinyl claim 1 , pyrrolyl claim 1 , furyl claim 1 , thienyl claim 1 , imidazolyl claim 1 , oxazolyl or isoxazolyl ring.7. The method according to wherein ring A is an optionally substituted pyridyl claim 1 , pyridazinyl claim 1 , pyrimidinyl or pyrazinyl ring.8. The method according to wherein ring A is optionally substituted pyridyl ring.9. The method according to wherein ring A is optionally substituted with one or more substituents independently selected from halo claim 1 , —NH claim 1 , NO claim 1 , Calkyl claim 1 , aryl and heterocyclyl claim 1 , the aryl and heterocyclyl groups optionally substituted with halo claim 1 , Calkyl or halo substituted Calkyl and claim 1 , when ring A contains one or more ring nitrogens claim 1 , the optional substituents include N-oxides of one or more of the ring nitrogens and pyridinium salts thereof.10. The method according to wherein ring A is optionally substituted with a substituent selected from halo claim 1 , alkyl claim 1 , CH—CH—CH— claim 1 , CF—CH— claim 1 , pyridyl claim 1 , NOand when ring A contains one or more ring nitrogens claim 1 , the optional substituent also include an N- ...

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27-02-2014 дата публикации

PYRIDONE AND AZA-PYRIDONE COMPOUNDS AND METHODS OF USE

Номер: US20140057896A1
Принадлежит:

Pyridone and aza-pyridone compounds of Formula I are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed. 10. The compound of wherein R claim 1 , R claim 1 , R claim 1 , and Rare each H.11. The compound of wherein Ris F claim 1 , —CH claim 1 , —CHF claim 1 , —CHF claim 1 , or —CF.12. The compound of wherein Ris —CHOH.13. The compound of wherein Ris F.14. The compound of wherein Ris —CHOH claim 1 , Rand Rare each H claim 1 , and Ris F.15. The compound of wherein Ris optionally substituted phenyl or naphthyl.16. The compound of wherein Ris optionally substituted C-Ccyclopropyl claim 1 , cyclobutyl claim 1 , cyclopentyl claim 1 , cyclohexyl claim 1 , or cycloheptyl.17. The compound of wherein Ris optionally substituted oxetanyl claim 1 , azetidinyl claim 1 , pyrrolidinyl claim 1 , tetrahydrofuryl claim 1 , piperidinyl claim 1 , piperazinyl claim 1 , morpholinyl claim 1 , or tetrahydropyranyl.18. The compound of wherein Ris optionally substituted pyrazolyl claim 1 , pyridinyl claim 1 , pyrimidinyl claim 1 , 5-methyl-4 claim 1 ,5 claim 1 ,6 claim 1 ,7-tetrahydropyrazolo[1 claim 1 ,5-a]pyrazin-2-yl claim 1 , 5-acetyl-4 claim 1 ,5 claim 1 ,6 claim 1 ,7-tetrahydropyrazolo[1 claim 1 ,5-a]pyrazin-2-yl claim 1 , 6 claim 1 ,7-dihydro-4H-pyrazolo[5 claim 1 ,1-c][1 claim 1 ,4]oxazin-2-yl claim 1 , or 1-methyl-5-(5-(4-methylpiperazin-1-yl)pyridin-2-yl.19. The compound of wherein Ris substituted with one or more of F claim 18 , Cl claim 18 , —CH claim 18 , cyclopropyl claim 18 , azetidinyl claim 18 , oxetanyl claim 18 , or morpholino.21. The compound of wherein Ris H.22. The compound of wherein X is S.23. The compound of wherein X is N.24. The ...

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27-02-2014 дата публикации

BIVALENT INHIBITORS OF IAP PROTEINS AND THERAPEUTIC METHODS USING THE SAME

Номер: US20140057924A1

Inhibitors of IAP proteins and compositions containing the same are disclosed. Methods of using the IAP protein inhibitors in the treatment of diseases and conditions wherein inhibition of IAP proteins provides a benefit, like cancers, also are disclosed. 2. The compound of wherein the B ring is phenyl claim 1 , naphthyl claim 1 , pyridinyl claim 1 , pyridazinyl claim 1 , pyrazinyl claim 1 , or pyrimidinyl.8. The compound of wherein X is SOand Y is null.14. A pharmaceutical composition comprising a compound of and a pharmaceutically acceptable carrier or vehicle.15. A composition comprising (a) compound of claim 1 , (b) a second therapeutic agent useful in the treatment of a disease or condition wherein inhibition of an TAP protein provides a benefit claim 1 , and (c) an optional excipient and/or pharmaceutically acceptable carrier.16. The composition of wherein the second therapeutic agent comprises a chemotherapeutic agent useful in the treatment of cancer.17. A method of treating a disease or condition wherein inhibition of an TAP protein provides a benefit comprising administering a therapeutically effective amount of a compound of to an individual in need thereof.18. The method of further comprising administering a therapeutically effective amount of a second therapeutic agent useful in the treatment of the disease or condition.19. The method of wherein the compound of and the second therapeutic agent are administered simultaneously.20. The method of wherein the compound of and the second therapeutic agent are administered separately.21. The method of wherein the disease or condition is a cancer.22. The method of wherein the disease is a cancer and the second therapeutic agent is one or more of a chemotherapeutic agent and radiation.23. The method of wherein the disease is a cancer and the second therapeutic agent is selected from the agents disclosed in paragraph [0107] and paragraphs [0126] through [0131].24. The method of wherein the second therapeutic agent ...

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27-02-2014 дата публикации

Organic compound, photovoltaic layer and organic photovoltaic device

Номер: US20140058080A1
Автор: Pavel Lazarev
Принадлежит: Cryscade Solar Ltd

The present invention relates generally to the field of photovoltaic devices and particularly to the organic photovoltaic layer. More specifically, the organic photovoltaic layer comprises at least one organic compound of the general structural formula where Het 1 and Het 2 are predominantly planar polycyclic molecular systems; A is a bridging group providing a lateral bond of the molecular systems; and X is a counterion from a list comprising H+, Li+, Na+, K+, NH4+, Ba++, Zn++, Sr++, Ca++, Mg++, and any combination thereof. The photovoltaic layer is formed of column-like or planar supramolecules, it has absorption of electromagnetic radiation in at least one predetermined spectral subrange within a wavelength range from 400 to 3000 nm, and the molecular system Het1, the bridging group A, and the molecular system Het2 form a donor-bridge-acceptor system providing dissociation of excited electron-hole pairs.

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