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Небесная энциклопедия

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

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Мониторинг СМИ

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

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Поддерживает ввод нескольких поисковых фраз (по одной на строку). При поиске обеспечивает поддержку морфологии русского и английского языка
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Применить Всего найдено 80460. Отображено 100.
05-01-2012 дата публикации

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

Номер: US20120003229A1
Принадлежит: Individual

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

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05-01-2012 дата публикации

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

Номер: US20120004206A1

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

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05-01-2012 дата публикации

Triheterocyclic Compounds and Compositions Thereof

Номер: US20120004224A1
Принадлежит: Gemin X Pharmaceuticals Canada Inc

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

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05-01-2012 дата публикации

Method of treatment or prophylaxis

Номер: US20120004259A1
Принадлежит: SPINIFEX PHARMACEUTICALS PTY LTD

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

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19-01-2012 дата публикации

Compounds for the prevention and treatment of cardiovascular diseases

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

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

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19-01-2012 дата публикации

Sulfone Compounds Which Modulate The CB2 Receptor

Номер: US20120015988A1
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

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

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19-01-2012 дата публикации

Taspase1 inhibitors and their uses

Номер: US20120015990A1
Автор: Emily Cheng, James Hsieh
Принадлежит: Washington University in St Louis WUSTL

Provided herein are small molecule inhibitors of Taspase1 and methods of using the small molecule inhibitors of Taspase1 to treat neoplasm in subjects in need thereof.

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26-01-2012 дата публикации

Triazole derivatives for treatment of alzheimer's disease

Номер: US20120022044A1
Принадлежит: Individual

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

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26-01-2012 дата публикации

Thiazole and oxazole-substituted arylamides as p2x3 and p2x2/3 antagonists

Номер: US20120022067A1
Принадлежит: Individual

Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R 1 is a group of formula A or formula B, and X, R 2 , R 3 , R 4 , R 5 , R 6 , R a and R b are as defined herein. Also provided are methods of using the compounds for treating diseases mediated by a P2X 3 and/or a P2X 2/3 receptor antagonist and methods of making the subject compounds.

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02-02-2012 дата публикации

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

Номер: US20120028961A1
Принадлежит: Eli Lilly and Co

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

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02-02-2012 дата публикации

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

Номер: US20120028983A1
Принадлежит: Kowa Co Ltd

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

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02-02-2012 дата публикации

Synthesis of enone intermediate

Номер: US20120029199A1
Принадлежит: Harvard College

The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The recent development of a modular synthesis of tetracycline analogs through a chiral enone intermediate has allowed for the efficient synthesis of novel tetracycline analogs never prepared before. The present invention provides a more efficient route for preparing the enone intermediate.

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09-02-2012 дата публикации

Substituted dihydropyrazolones and their use

Номер: US20120035151A1
Принадлежит: Bayer Pharma AG

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

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16-02-2012 дата публикации

Inhibitors of hcv ns5a

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

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

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23-02-2012 дата публикации

Compounds and compositions for cognition-enhancement, methods of making, and methods of treating

Номер: US20120046273A1
Принадлежит: Mithridion Inc

Muscarinic agonists, which are useful for stimulating muscarinic receptors and treating cognitive disorders, are provided. Methods of synthesizing such agonists also are provided. Also provided are compositions for enhancing cognitive function in subjects such as humans, the compositions comprising a muscarinic agonist or a pharmaceutically suitable form thereof. Also provided are methods of treating animals such as humans by administering such compositions.

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01-03-2012 дата публикации

Azafluorene derivative and organic light-emitting device using the derivative

Номер: US20120049176A1
Принадлежит: Canon Inc

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

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01-03-2012 дата публикации

5-aryl isoxazolines for controlling invertebrate pests

Номер: US20120053051A9
Принадлежит: EI Du Pont de Nemours and Co

Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N-oxides, and salts thereof, wherein A 1 , A 2 and A 3 are independently selected from the group consisting of CR 3 and N; B 1 B 2 and B 3 are independently selected from the group consisting of CR 2 and N; Q is a phenyl ring or a 5- or 6-membered saturated or unsaturated heterocyclic ring, each ring optionally substituted with one or more substituents independently selected from halogen, C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, C 3 -C 6 cycloalkyl, C 3 -C 6 halocycloalkyl, C 1 -C 6 alkoxy, C 1 -C 6 haloalkoxy, C 1 -C 6 alkylthio, C 1 -C 6 haloalkylthio, C 1 -C 6 alkylsulfinyl, C 1 -C 6 haloalkylsulfinyl, C 1 -C 6 alkylsulfonyl, C 1 -C 6 haloalkylsulfonyl, —CN, —NO 2 , —N(R 4 )R 5 , —C(W)N(R4)R 5 , —C(O)OR 5 and R 8 ; or —S(O) 2 N(R 21 )R 22 , —S(O) p R 25 or —S(O)(═NR 28 )R 29 ; and R 1 , R 2 , R 3 , R 4 , R 5 , R 8 , R 21 , R 22 , R 25 , R 28 , R 29 ; p and n are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound or a composition' of the invention.

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08-03-2012 дата публикации

Macrolides with Anti-Inflammatory Activity

Номер: US20120058963A1
Принадлежит: Glaxo Group Ltd

The present invention relates to novel semi-synthetic macrolides having anti-inflammatory activity. More particularly, the invention relates to 14- and 15-membered macrolides substituted at the 4″ position, to their pharmaceutically acceptable derivatives, to processes and intermediates for their preparation, to pharmaceutical compositions containing them and to their activity and use in the treatment of inflammatory diseases and conditions in humans and animals, especially those diseases associated with excessive secretion of TNF-α, IL-1, IL-8, IL-2 or IL-5; and/or inhibitor of excessive lymphocyte proliferation; and/or excessive granulocyte degranulation.

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08-03-2012 дата публикации

Di-azetidinyl diamide as monoacylglycerol lipase inhibitors

Номер: US20120058986A1
Принадлежит: Janssen Pharmaceutica NV

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

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08-03-2012 дата публикации

Carbazole and carboline kinase inhibitors

Номер: US20120058988A1
Принадлежит: Bristol Myers Squibb Co

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

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08-03-2012 дата публикации

Carbazole carboxamide compounds useful as kinase inhibitors

Номер: US20120058996A1
Принадлежит: Bristol Myers Squibb Co

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

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08-03-2012 дата публикации

Novel kinase modulators

Номер: US20120059001A1

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

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08-03-2012 дата публикации

Novel crystalline hydrate, amorphous and polymorphic forms of dihydro-benzoxazole-6-yl-acetamide derivative and processes for their preparation

Номер: US20120059034A1
Принадлежит: Richter Gedeon Nyrt

The invention relates to novel crystalline hydrate, amorphous and crystalline polymorphic forms of 2-[4-(4-Fluoro-benzyl)-piperidine-1-yl]-2-oxo-N-(2-oxo-2,3-dihydro-benzoxazole-6-yl)-acetamide (I) (radiprodil). Processes for the preparation of these forms, compositions containing these forms, and methods of use thereof are also described.

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08-03-2012 дата публикации

Intermediate compound for synthesizing pharmaceutical agent and production method thereof

Номер: US20120059165A1
Принадлежит: SANOFI SA

A production method of an optically active 2-{4-(5-substituted-oxadiazolyl) phenyl}morpholine which is useful as an intermediate for synthesizing a pharmaceutical agent is provided and the method comprises the following steps 1) to 4): 1) reacting a bromophenylmorpholine with a hexacyanoferrate(II) or a hydrate thereof at a temperature of from 110° C. to 140° C. in a reaction mixture comprising a Na 2 CO 3 , an organophosphorus compound, and a palladium catalyst in a polar aprotic solvent alone or combination of a polar aprotic solvent and other polar aprotic solvent or hydrocarbon solvent to give a cyanophenylmorpholine; 2) reacting the cyanophenylmorpholine with hydroxylamine or hydroxylamine hydrochloride at a temperature of from 10° C. to 40° C. in an aprotic polar solvent to give a hydroxylamine derivative; 3) reacting the hydroxylamine derivative with an acylation reagent selected from the group consisting of aliphatic acyl halides, aromatic acyl halides, aliphatic acyl anhydrides and aromatic anhydrides; and 4) keeping the mixture obtained after step 3) at a temperature of from 60° C. to 140° C. to give a 2-{4-(5-substituted-oxadiazolyl) phenyl}morpholine.

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15-03-2012 дата публикации

Compounds and their uses 708

Номер: US20120065214A1
Принадлежит: AstraZeneca AB

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

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22-03-2012 дата публикации

Pyrazole oxadiazole derivatives as s1p1 agonists

Номер: US20120071460A1
Принадлежит: MERCK SERONO SA

The present invention relates to pyrazole oxadiazoles derivatives of Formula (I), and their use for treating multiple sclerosis and other diseases, wherein R 1 , R 2 and R 3 are as defined in the description.

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22-03-2012 дата публикации

Estrogen receptor modulators and uses thereof

Номер: US20120071535A1
Принадлежит: Aragon Pharmaceuticals Inc

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

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29-03-2012 дата публикации

Bicyclic compounds and use as antidiabetics

Номер: US20120077812A1
Принадлежит: Individual

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

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29-03-2012 дата публикации

Compounds act at multiple prostaglandin receptors giving a general anti-inflammatory response

Номер: US20120077858A1
Принадлежит: Allergan Inc

The present invention provides compounds, that are N-alkyl-2-(1-(5-substituted-2-(3-oxo-3-(trifluoromethylsulfonamido)propyl)benzyl)pyrrolidin-2-yl)oxazole-4-carboxamide wherein the 5 substituent is selected from the group consisting of halo and alkyloxy radicals. The compound may be represented by the following formula wherein R 1 is selected from the group consisting of CO 2 R 7 and CON(R 7 )SO 2 R 7 wherein R 1 , R 2 , R 3 , R 4 , and R 7 are as defined in the specification. The compounds may be administered to treat DP 1 , FP, EP 1 , EP 3 , TP and/or EP 4 receptor mediated diseases or conditions.

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05-04-2012 дата публикации

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

Номер: US20120080585A1
Принадлежит: Fujifilm Corp

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

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05-04-2012 дата публикации

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

Номер: US20120083494A1

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

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12-04-2012 дата публикации

Five-membered heterocycles useful as serine protease inhibitors

Номер: US20120088758A1
Принадлежит: Bristol Myers Squibb Co

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

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12-04-2012 дата публикации

Pinane-substituted pyrimidinediamine derivatives useful as axl inhibitors

Номер: US20120088768A1
Принадлежит: Rigel Pharmaceuticals Inc

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

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12-04-2012 дата публикации

Azole derivatives and fused bicyclic azole derivatives as therapeutic agents

Номер: US20120088778A1
Принадлежит: vTvx Holdings I LLC

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

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19-04-2012 дата публикации

Novel Heterocyclic Compounds as Pesticides

Номер: US20120094837A1
Принадлежит: Bayer CropScience AG

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

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26-04-2012 дата публикации

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

Номер: US20120101051A1
Принадлежит: Green Cross Corp Korea

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

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26-04-2012 дата публикации

S1p1 agonists comprising a bicyclic n-containing ring

Номер: US20120101083A1
Принадлежит: Glaxo Group Ltd

The present invention relates to novel compounds of formula (I) having S1P1 agonist activity, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders.

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26-04-2012 дата публикации

1,2,4-oxadiazol derivatives, their pharmaceutical compositions and their use as sphingosine 1-phosphate 1 receptor agonists

Номер: US20120101124A1
Автор: Feng Ren, Xichen Lin, Yugui Si
Принадлежит: Glaxo Group Ltd

1,2,4-Oxadiazol derivatives represented by formula (I) useful as sphingosine 1-phosphate 1 (S1P1) receptor agonists, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders mediated via S1P1 receptor are disclosed.

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03-05-2012 дата публикации

Compounds for the treatment of multi-drug resistant bacterial infections

Номер: US20120108577A1
Принадлежит: AstraZeneca AB

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

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03-05-2012 дата публикации

INHIBITORS OF 11beta-HYDROXYSTEROID DEHYDROGENASE 1

Номер: US20120108578A1

This invention relates to novel compounds of the Formula (I), (Ia 1-10 ), (Ib 1-10 ), (Ic 1-10 ), (Id 1-7 ), (Ie 1-5 ) pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11β-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of cortisol in a cell or the inhibition of the conversion of cortisone to cortisol in a cell.

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03-05-2012 дата публикации

Nitrogen-containing aromatic heterocyclyl compound

Номер: US20120108639A1
Принадлежит: Daiichi Sankyo Co Ltd

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

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10-05-2012 дата публикации

Use of selective gaba a alpha 5 negative allosteric modulators for the treatment of central nervous system conditions

Номер: US20120115839A1
Принадлежит: Hoffmann La Roche Inc

The present invention relates to the pharmaceutical use of selective GABA A α5 negative allosteric modulators for the treatment, prevention and/or delay of progression of central nervous system (CNS) conditions related to excessive GABAergic inhibition in the brain.

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10-05-2012 дата публикации

Compounds having antiparasitic or anti-infectious activity

Номер: US20120115904A1

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

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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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17-05-2012 дата публикации

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

Номер: US20120123120A1
Принадлежит: UNIVERSITY OF CALIFORNIA

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

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24-05-2012 дата публикации

Substituted sodium 1H-pyrazol-5-olate

Номер: US20120129857A1
Принадлежит: Bayer Pharma AG

The present application relates to sodium 1-[6-(morpholin-4-yl)pyrimidin-4-yl]-4-(1H-1,2,3-triazol-1-yl)-1 H-pyrazol-5-olate, to processes for its preparation, to its use for the treatment and/or prophylaxis of diseases and to its use for the preparation of medicaments for the treatment and/or prophylaxis of diseases, in particular cardiovascular and haematological diseases and kidney diseases, and for promoting wound healing.

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24-05-2012 дата публикации

Piperazinyl derivatives useful as modulators of the neuropeptide y2 receptor

Номер: US20120129870A1
Принадлежит: Janssen Pharmaceutica NV

The present invention is directed to piperidinyl and piperazinyl derivatives of formula (II) useful as inhibitors of the NPY Y2 receptor, pharmaceutical compositions comprising said compounds, processes for the preparation of said compounds and the use of said compounds for the treatment and/or prevention of disorders, diseases and conditions mediated by the NPY Y2 receptor.

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24-05-2012 дата публикации

Inhibitors of syk and jak protein kinases

Номер: US20120130073A1
Принадлежит: Portola Pharmaceuticals LLC

The present invention is directed to compounds of formula I-V and tautomers thereof or pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of syk kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma.

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31-05-2012 дата публикации

Bis-Benzimidazole Derivatives As Hepatitis C Virus Inhibitors

Номер: US20120135953A1
Принадлежит: Tibotec Pharmaceuticals Ltd

Inhibitors of HCV replication of formula I including stereochemically isomeric forms, and salts, hydrates, solvates thereof, wherein R and R′ have the meaning as defined herein. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use, alone or in combination with other HCV inhibitors, in HCV therapy.

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31-05-2012 дата публикации

Phenyl Ethynyl Derivatives As Hepatitis C Virus Inhibitors

Номер: US20120136027A1
Принадлежит: Individual

Inhibitors of HCV replication of formula I including stereochemically isomeric forms, and salts, hydrates, solvates thereof, wherein R and R* have the meaning defined in the claims. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use, alone or in combination with other HCV inhibitors, in the treatment or prophylaxis of HCV.

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31-05-2012 дата публикации

Method for preparing 5-chloro-n-(methyl)thiophen-2-carboxamide derivative and intermediate used therein

Номер: US20120136149A1

Disclosed are: a method for preparing a 5-chloro-N-({(5S)-2-oxo-3-[4-(5,6-dihydro-4H-[1,2,4]triazin- 1 -yl)phenyl]-1,3-oxazolidin-5-yl}-methyl)thiophene-2-carboxamide derivative, which is a inhibitor of blood coagulation factor Xa, in a high purity and yield; and a novel intermedicate used therein.

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07-06-2012 дата публикации

Light-emitting device material and light-emitting device

Номер: US20120138907A1
Принадлежит: TORAY INDUSTRIES INC

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

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07-06-2012 дата публикации

Oxazolidinone-quinolone hybrid antibiotics

Номер: US20120142635A1

The present invention relates to compounds of the Formula (I) that are useful antimicrobial agents and effective against a variety of multi-drug resistant bacteria:

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07-06-2012 дата публикации

Azetidine 2-Carboxamide Derivatives Which Modulate The CB2 Receptor

Номер: US20120142666A1
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

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

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07-06-2012 дата публикации

Pyrrolidine Compounds Which Modulate The CB2 Receptor

Номер: US20120142677A1
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

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

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07-06-2012 дата публикации

Picolinamide derivatives as ttx-s blockers

Номер: US20120142691A1
Принадлежит: Raqualia Pharma Inc

The present invention relates to picolinamide derivatives which have blocking activities of voltage gated sodium channels as the TTX-S channels, and which are useful in the treatment or prevention of disorders and diseases in which voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which voltage gated sodium channels are involved.

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07-06-2012 дата публикации

Microbiocidal heterocycles

Номер: US20120142700A1
Принадлежит: SYNGENTA CROP PROTECTION LLC

The present invention relates to heterocyclic compounds of formula (I) which have microbiocidal activity, in particular fungicidal activity, as well as methods of using the compounds of formula (I) to control microbes.

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07-06-2012 дата публикации

Substituted pyridine urea compounds

Номер: US20120142708A1
Принадлежит: Confluence Life Sciences Inc

The present disclosure provides pyridine urea compounds useful in the treatment of p38 kinase mediated diseases, such as lymphoma and auto-inflammatory disease, having the structure of Formula (I): wherein R 1 , R 2 , R 3 , R 4 , R 5 , V and W are as defined in the detailed description; pharmaceutical compositions comprising at least one of the compounds; and methods for treating p38 kinase mediated diseases using the compound.

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07-06-2012 дата публикации

Bicyclic compound

Номер: US20120142714A1
Принадлежит: Takeda Pharmaceutical Co Ltd

The present invention provides a compound having an ACC inhibitory action, which is useful as an agent for the prophylaxis or treatment of obesity, diabetes and the like, and having superior efficacy. The present invention relates to a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof.

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07-06-2012 дата публикации

Heteroaryls and uses thereof

Номер: US20120142732A1
Принадлежит: Millennium Pharmaceuticals Inc

This invention provides compounds of formula IA or IB: wherein HY, R 1 , R 2 , and G 1 , are as described in the specification. The compounds are inhibitors of VPS34 and/or PI3K and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.

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07-06-2012 дата публикации

Novel oxadiazole derivatives as sphingosine 1-phosphate (s1p) receptor modulators

Номер: US20120142739A1
Принадлежит: Allergan Inc

The present invention relates to novel oxadiazole derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.

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21-06-2012 дата публикации

Phosphorous derivatives as chemokine receptor modulators

Номер: US20120157413A1
Принадлежит: Allergan Inc

The present invention relates to novel phosphorous derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.

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21-06-2012 дата публикации

Anhydrate Forms Of A Pyridine Derivative

Номер: US20120157450A1

The invention relates to the compound of formula (I) in a crystalline anhydrate form, pharmaceutical formulations containing them, their use in therapy and processes for preparing the same.

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28-06-2012 дата публикации

Novel azabicyclohexanes

Номер: US20120165320A1
Принадлежит: Panacea Biotec Ltd

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

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28-06-2012 дата публикации

Quinoline derivatives as pi3 kinase inhibitors

Номер: US20120165321A1
Принадлежит: GlaxoSmithKline LLC

Invented is a method of inhibiting the activity/function of PI3 kinases using quinoline derivatives. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries by the administration of quinoline derivatives.

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05-07-2012 дата публикации

Heterocyclylaminopyrimidines as kinase inhibitors

Номер: US20120172384A1
Принадлежит: Cellzome Ltd

The invention relates to compounds of formula (I) wherein R 1 to R 6 and T 0 have the meaning as cited in the description and the claims. Said compounds are useful as inhibitors of ZAP-70, Syk or JAK3 for the treatment or prophylaxis of immunological, inflammatory, autoimmune, allergic disorders, immunologically-mediated diseases. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the use as medicaments.

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05-07-2012 дата публикации

Polymerizable ambipolar hosts for phosphorescent guest emitters

Номер: US20120172556A1
Принадлежит: Georgia Tech Research Corp

The inventions describe disclosed and described herein relate to polymerizable ambipolar monomers, useful for making polymer or copolymer host materials for guest phosphorescent metal complexes, which together can form emission layers of organic light emitting diodes (OLEDs). Methods of making the ambipolar monomers are also described. Formula (I) wherein at least one of the R 1 , R 2 and R 3 groups is an optionally substituted carbazole group.

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12-07-2012 дата публикации

Glycoside derivatives and uses thereof

Номер: US20120178680A1
Принадлежит: NOVARTIS AG

This invention relates to compounds represented by formula (I): wherein the variables are defined as herein above, which are useful for treating diseases and conditions mediated by the sodium D-glucose co-transporter (SGLT), e.g. diabetes. The invention also provides methods of treating such diseases and conditions, and compositions etc. for their treatment.

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12-07-2012 дата публикации

Cyanoisoquinoline compounds and methods of use thereof

Номер: US20120178755A1
Принадлежит: Fibrogen Inc

The present invention relates to cyanoisoquinoline compounds suitable for use in treating hypoxia inducible factor-mediated and/or erythropoietin-associated conditions. The cyanoisoquinoline compounds of the invention have the following structure:

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19-07-2012 дата публикации

Compound, a process for its preparation, a pharmaceutical composition, use of a compound, a method for modulating or regulating serine/threonine kinases and a serine/threonine kinases modulating agent

Номер: US20120184535A1
Принадлежит: Selvita Sp zoo

A compound, a process for its preparation, a pharmaceutical composition, use of a compound, a method for modulating or regulating serine/threonine and tyrosine kinases and a serine/threonine and tyrosine kinases modulating agent. Novel small-molecule compounds with kinase inhibitory activity, having superior properties as pharmaceutical agents, production method thereof and uses thereof. In particular, new derivatives of tetrahalogenated benzimidazole with serine/threonine and tyrosine kinases inhibitory properties, preferably selected from the group of PIM, HIPK, DYRK, CLK, CDK, FLT, PKG, Haspin, MER, TAO, MNK, TRK kinases which exhibit superior pharmacological actions, and can be useful for the treatment of disease conditions, especially cancers depending on serine/threonine and tyrosine kinases, such as but not limited to leukemias and solid tumors.

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19-07-2012 дата публикации

Substituted nicotinamides as kcnq2/3 modulators

Номер: US20120184550A1
Принадлежит: GRUENENTHAL GmbH

Substituted nicotinamides, processes for their preparation, medicaments comprising these compounds and methods of using these compounds to treat pain, epilepsy, urinary incontinence, anxiety, dependency, mania, bipolar disorders, migraine, cognitive diseases, and/or dystonia-associated dyskinesias.

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19-07-2012 дата публикации

Novel compounds

Номер: US20120184553A1
Принадлежит: Glaxo Group Ltd

The present invention relates to novel compounds that inhibit LRRK2 kinase activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases characterised by LRRK2 kinase activity, particularly Parkinson's disease and Alzheimer's disease.

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19-07-2012 дата публикации

Quinolines and Their Therapeutic Use

Номер: US20120184579A1
Принадлежит: Individual

Compounds of formula (I) are CRTH2 ligands, useful in the treatment of, for example, asthma and COPD wherein: R 1 is halogen or cyano; R 2 is hydrogen or methyl; R 3 and R 4 are independently —OR 6 , C 1 -C 6 alkyl or C 3 -C 6 cycloalkyl, the latter two groups being optionally substituted by one or more halogen atoms; R 5 is hydrogen or halogen; R 6 is C 1 C 6 alkyl or C 3 -C 6 cycloalkyl, either of which being optionally substituted by one or more halogen atoms; X is —CH 2 —, —S—, or —O—; one of Y and Y 1 is hydrogen and the other is OR 6 , —C(═O)R 7 , NR 8 SO 2 R 6 or a heterocyclic group selected from those referred to in the specification; and R 6 , R 7 and R 8 are as defined in the specification.

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26-07-2012 дата публикации

Benzoimidazolyl-pyrazine compounds for inflammation and immune-related uses

Номер: US20120190853A1
Принадлежит: Synta Phamaceuticals Corp

The invention relates to compounds of structural formula (I) or (III): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, wherein ring A, X 1 , X 2 , X 3 , X 5 , R 1 , R 4 , Y, Z, L, m and n are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.

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02-08-2012 дата публикации

Electrochromic compound, electrochromic composition, and display element

Номер: US20120194894A1
Принадлежит: Ricoh Co Ltd

Disclosed are electrochromic compounds represented by the formulas defined in the specification.

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02-08-2012 дата публикации

2-Oxo-1-Pyrrolidine Derivatives, Processes for Preparing Them and Their Uses

Номер: US20120196866A1
Принадлежит: UCB PHARMA SA

The present invention concerns 2-oxo-1-pyrrolidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.

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02-08-2012 дата публикации

Sulfoximines as kinase inhibitors

Номер: US20120196902A1
Принадлежит: Allergan Inc

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

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09-08-2012 дата публикации

NP-1 Antagonists and Their Therapeutic Use

Номер: US20120201749A1
Принадлежит: Ark Therapeutics Ltd

Compounds of formula (I): or a pharmaceutically acceptable salt thereof, wherein: W is arylene, heteroarylene or formula (a) each L is independently alkylene, alkenylene, alkynylene, a direct bond, arylene, cycloalkylene, alkylene-arylene, alkylene-C═O or —C═O; each X is independently an N-containing heteroarylene, N-containing cycloalkylene or NR; Y is N-containing heteroaryl, N-containing cycloalkyl, NR 2 , OR 1 , CN or CO 2 R; Z 1 is formula (b); are useful in therapy, particularly in the therapy of neurodegeneration and cancer.

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09-08-2012 дата публикации

Compounds for the treatment of hepatitis c

Номер: US20120201783A1
Принадлежит: Bristol Myers Squibb Co

The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.

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09-08-2012 дата публикации

Therapeutic isoxazole compounds

Номер: US20120202786A1
Принадлежит: Dart Neuroscience Cayman Ltd

The invention provides a compound of formula I: wherein A 1 , A 2 , A 3 , R 1 , X, Y, and B have any of the values described herein, as well as salts of such compounds, compositions comprising such compounds, and therapeutic methods that comprise the administration of such compounds. The compounds are inhibitors of monoamine oxidase B (MAO-B) enzyme function and are useful for improving cognitive function and for treating psychiatric disorders in animals.

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09-08-2012 дата публикации

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

Номер: US20120202795A1
Принадлежит: Aventis Pharmaceuticals Inc

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

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16-08-2012 дата публикации

Novel organic electroluminescent compounds and organic electroluminescent device using the same

Номер: US20120206037A1

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

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16-08-2012 дата публикации

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

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

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

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16-08-2012 дата публикации

Heterocyclic Benzoxazole Compositions as Inhibitors of Hepatitis C Virus

Номер: US20120208856A1
Автор: Dawn N. Ward, Paul Smith

This invention relates to benzoxazole compounds, compositions and devices for delivering them, processes for manufacturing them, and methods of using them in the treatment of Hepatitis C Virus.

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23-08-2012 дата публикации

3,4-disubstituted 1h-pyrazole compounds and their use as cyclin dependent kinase and glycogen synthase kinase-3 modulators

Номер: US20120213791A1
Принадлежит: ASTEX THERAPEUTICS LTD

The invention provides compounds of the formula (0) or salts or tautomers or N-oxides or solvates thereof, and combinations thereof with other anti-cancer agents, for use in the prophylaxis or treatment of disease states and conditions such as cancers mediated by cyclin-dependent kinase and glycogen synthase kinase-3.

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23-08-2012 дата публикации

6,5-heterocyclic propargylic alcohol compounds and uses therefor

Номер: US20120214762A1
Принадлежит: Genentech Inc

The invention relates to novel compounds of Formula I: wherein A, Y, R 1 , R 2 and the subscript b each has the meaning as described herein and compounds of Formula I, and stereoisomers, geometric isomers, tautomers, solvates, metabolites, isotopes, pharmaceutically acceptable salts, or prodrugs thereof. 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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23-08-2012 дата публикации

Viral polymerase inhibitors

Номер: US20120214783A1
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

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

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23-08-2012 дата публикации

New compounds, pharmaceutical compositions and uses thereof

Номер: US20120214785A1
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

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

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30-08-2012 дата публикации

Novel organic electroluminescent compounds and organic electroluminescent device using the same

Номер: US20120217485A1

Provided are novel organic electroluminescent compounds and organic electroluminescent devices using the same. Since the organic electroluminescent compound exhibits good luminous efficiency and excellent life property compared to the existing material, it may be used to manufacture OLED devices having superior operation life and consuming less power due to improved power efficiency.

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30-08-2012 дата публикации

Selective calcium channel modulators

Номер: US20120220564A1
Принадлежит: Zalicus Pharmaceuticals Ltd

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

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30-08-2012 дата публикации

Heterocyclic compounds for the inhibition of pask

Номер: US20120220589A1
Принадлежит: Bioenergenix LLC

Disclosed herein are new heterocyclic compounds and compositions and their application as pharmaceuticals for the treatment of disease. Methods of inhibiting PAS Kinase (PASK) activity in a human or animal subject are also provided for the treatment of diseases such as diabetes mellitus.

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30-08-2012 дата публикации

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

Номер: US20120220592A1
Принадлежит: Newron Pharmaceuticals SpA

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

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30-08-2012 дата публикации

Novel spiropiperidine compounds

Номер: US20120220616A1
Принадлежит: Eli Lilly and Co

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

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06-09-2012 дата публикации

Mst1 kinase inhibitors and methods of their use

Номер: US20120225857A1
Принадлежит: Individual

Compounds for the inhibition of mammalian Ste20-like kinase 1 (MST1) are disclosed, along with compositions comprising them and methods of their use in the treatment, management or prevention of an inflammatory or autoimmune diseases or disorders.

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06-09-2012 дата публикации

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

Номер: US20120225890A1
Принадлежит: ProteoTech Inc

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

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06-09-2012 дата публикации

[1,5]-Diazocin Derivatives

Номер: US20120225892A1
Принадлежит: MELLITECH

The present invention relates to compounds of formula (I) compositions, in particular pharmaceutical compositions, and medicaments comprising at least one compound of formula (I). The invention also relates to the use of such a compound for manufacturing a medicament. In particular the medicament and the pharmaceutical composition are intended to treat diseases linked with insulin regulation problems, such as diabetes. This invention aims also to methods for treating or preventing such diseases.

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06-09-2012 дата публикации

Novel 2-pyridone derivative and pharmaceutical product containing same

Номер: US20120225896A1
Принадлежит: Kowa Co Ltd

Disclosed is a novel 2-pyridone derivative represented by general formula (1), which has both angiotensin II receptor antagonist activity and PPAR-γ activating activity and is useful as a prophylactic and/or therapeutic agent for cardiovascular diseases and metabolic diseases. Also disclosed is a pharmaceutical composition which contains the novel 2-pyridone derivative. In general formula (1), R1 represents a C1-6 alkyl group or a C1-6 alkoxy group; R2 represents a C1-6 alkyl group or a C3-8 cycloalkyl group; R3 represents a C1-6 alkyl group, a C6-10 aryl-C1-6 alkyl group, a C1-6 alkoxy-C1-6 alkyl group or a group represented by formula (2) (wherein A represents a nitrogen atom or CH, and R5 represents a hydrogen atom or a C1-6 alkoxy group); and R4 represents a group represented by formula (3) or (4).

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13-09-2012 дата публикации

Methods of Treating or Preventing Autoimmune Diseases With 2,4-Pyrimidinediamine Compounds

Номер: US20120230984A1
Принадлежит: Rigel Pharmaceuticals Inc

The present invention provides methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds, as well as methods of treating, preventing or ameliorating symptoms associated with such diseases. Specific examples of autoimmune diseases that can be treated or prevented with the compounds include rheumatoid arthritis and/or its associated symptoms, systemic lups erythematosis and/or its associated symptoms and multiple sclerosis and/or its associated symptoms.

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13-09-2012 дата публикации

Compositions and Methods for Treatment of Eye Disorders

Номер: US20120232019A1
Принадлежит: Sarcode Bioscience Inc

The present invention provides compounds and methods for the treatment of LFA-1 mediated diseases. In particular, LFA-1 antagonists are described herein and these antagonists are used in the treatment of LFA-1 mediated diseases. One aspect of the invention provides for diagnosis of an LFA-1 mediated disease and administration of a LFA-1 antagonist, after the patient is diagnosed with a LFA-1 mediated disease. In some embodiments, the LFA-1 mediated diseases treated are dry eye disorders. Also provided herein are methods for identifying compounds which are LFA-1 antagonists.

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13-09-2012 дата публикации

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

Номер: US20120232070A1
Принадлежит: Laboratories Fournier SAS

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

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