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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 12389. Отображено 100.
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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26-01-2012 дата публикации

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

Номер: US20120022076A1
Принадлежит: Individual

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

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02-02-2012 дата публикации

Animal ectoparasite-controlling agent

Номер: US20120029038A1
Автор: Kaori Ikari
Принадлежит: Sumitomo Chemical Co Ltd

The present invention provides an animal ectoparasite-controlling agent containing as an active ingredient a hydrazide compound represented by the formula (1) wherein R 3 represents a fluorine atom, a chlorine atom, a bromine atom, a methyl group, an ethyl group or a hydrogen atom, R 5 and R 6 are the same or different each other and each represents a methyl group or a hydrogen atom, R 4 represents a C1-C6 haloalkyl group, which shows excellent controlling effects on animal ectoparasites.

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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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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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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

Compound inhibiting in vivo phosphorus transport and medicine containing the same

Номер: US20120115851A1
Принадлежит: Kyowa Hakko Kirin Co Ltd

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

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10-05-2012 дата публикации

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

Номер: US20120115915A1
Принадлежит: Harvard College

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

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17-05-2012 дата публикации

Compounds, Compositions and Methods for Modulating Uric Acid Levels

Номер: US20120122780A1
Принадлежит: Ardea Biociences Inc

Described herein are compounds useful in the reduction of blood uric acid levels, formulations containing them and methods of making and using them. In some embodiments, the compounds described herein are used in the treatment or prevention of disorders related to aberrant levels of uric acid.

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31-05-2012 дата публикации

Substituted Esters as Cannabinoid-1 Receptor Modulators

Номер: US20120135975A1
Принадлежит: Merck and Co Inc

Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, Alzheimer's disease, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, cirrhosis of the liver, non-alcoholic fatty liver disease (NAFLD), non-alcoholic steatohepatitis (NASH), and the promotion of wakefulness.

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07-06-2012 дата публикации

Compounds as bradykinin b1 antagonists

Номер: US20120142695A1
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

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

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07-06-2012 дата публикации

Synthesis of ttx intermediates

Номер: US20120142911A1

The present invention relates to the synthesis of intermediates which are useful in TTX synthesis and to the preparation thereof.

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14-06-2012 дата публикации

Inhibition of p38 kinase activity using substituted heterocyclic ureas

Номер: US20120149706A1
Принадлежит: Individual

This invention relates to the use of a group of aryl ureas in treating cytokine mediated diseases, other than cancer and proteolytic enzyme mediated diseases, other than cancer, and pharmaceutical compositions for use in such therapy.

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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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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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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

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

Номер: US20120220592A1
Принадлежит: Newron Pharmaceuticals SpA

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

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06-09-2012 дата публикации

Compositions and methods useful for treating diseases

Номер: US20120225851A1
Принадлежит: Eutropics Pharmaceuticals Inc

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

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20-09-2012 дата публикации

Iodine radiolabelling method

Номер: US20120237444A1
Автор: Michelle Avory
Принадлежит: Individual

The present invention provides a novel method of labelling biological targeting molecules (BTMs) of interest with radioiodine. Also provided are novel radioiodinated BTMs prepared using the method, as well as radiopharmaceutical compositions comprising such radioiodinated BTMs. The invention also provides radioiodinated intermediates useful in the method, as well as in vivo imaging methods using the radioiodinated BTMs.

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25-10-2012 дата публикации

Aryl compounds as ppar ligands and their use

Номер: US20120271055A1

The present invention relates to a compound as a peroxisome proliferator activated receptor (PPAR) activator and a hydrate, a solvate, a stereoisomer and a pharmaceutically acceptable salt thereof, and a pharmaceutical composition, a cosmetic composition, a muscle strengthening agent, a memory improving agent, a therapeutic agent for dementia and Parkinson's disease, a functional food and a feed composition containing the same.

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15-11-2012 дата публикации

Novel compounds with high therapeutic index

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

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

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15-11-2012 дата публикации

Compounds for the treatment of proliferative disorders

Номер: US20120289483A1
Принадлежит: Synta Phamaceuticals Corp

The invention relates to compounds of structural formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, and prodrug thereof, wherein R a , R b , and R 2 are defined herein. These compounds inhibit tubulin polymerization and/or target vasculature and are useful for treating proliferative disorders, such as cancer.

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13-12-2012 дата публикации

Isoxazoline derivatives as insecticides

Номер: US20120316124A1
Принадлежит: SYNGENTA CROP PROTECTION LLC

The present invention relates to compounds formula (I), wherein P is P1, P2, heterocyclyl or heterocyclyl substituted by one to five Z; and wherein A 1 , A 2 , A 3 , A 4 , G 1 , R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 17 , R 18 , R 19 and R 20 are as defined in claim 1 ; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising the compounds of formula (I) and to methods of using the compounds of formula (I) to control insect, acarine, nematode and mollusc pests.

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10-01-2013 дата публикации

Fluorine-free fused ring heteroaromatic photoacid generators and resist compositions containing the same

Номер: US20130011788A1
Принадлежит: International Business Machines Corp

The present invention relates to a fluorine-free photoacid generator (PAG) and a photoresist composition containing the same. The PAG is characterized by the presence of an onium cationic component and a fluorine-free fused ring heteroaromatic sulfonate anionic component containing one or more electron withdrawing substituents. The onium cationic component of the PAG is preferably a sulfonium or an iodonium cation. The photoresist composition further contains an acid sensitive imaging polymer. The photoresist composition is especially useful for forming material patterns on a semiconductor substrate using 193 nm (ArF) lithography.

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10-01-2013 дата публикации

Fluorine-free fused ring heteroaromatic photoacid generators and resist compositions containing the same

Номер: US20130011793A1
Принадлежит: International Business Machines Corp

The present invention relates to a fluorine-free photoacid generator (PAG) and a photoresist composition containing the same. The PAG is characterized by the presence of an onium cationic component and a fluorine-free fused ring heteroaromatic sulfonate anionic component containing one or more electron withdrawing substituents. The onium cationic component of the PAG is preferably a sulfonium or an iodonium cation. The photoresist composition further contains an acid sensitive imaging polymer. The photoresist composition is especially useful for forming material patterns on a semiconductor substrate using 193 nm (ArF) lithography.

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21-02-2013 дата публикации

Pharmaceutical composition for inhibiting apoptosis of neuron or neurodegeneration

Номер: US20130046001A1
Принадлежит: SK Biopharmaceuticals Co Ltd

Provided is a pharmaceutical composition for inhibiting apoptosis of neurons or neurodegeneration. The pharmaceutical composition effectively prevents or treats diseases related to apoptosis of neurons or neurodegeneration.

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21-03-2013 дата публикации

LYSOPHOSPHATIDIC ACID RECEPTOR ANTAGONISTS

Номер: US20130072449A1
Принадлежит: INTERMUNE, INC.

Compounds, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds to treat, prevent or diagnose diseases, disorders, or conditions associated with one or more of the lysophosphatidic acid receptors are provided. 5. The compound or pharmaceutically acceptable salt of claim 2 , wherein m=1 claim 2 , and wherein Ris hydrogen and Ris selected from the group consisting of optionally substituted phenyl claim 2 , imidazole claim 2 , pyridine claim 2 , thiazole claim 2 , and oxazole.6. The compound or pharmaceutically acceptable salt thereof of claim 2 , wherein m=1 claim 2 , and wherein Rand Rare joined together with the atom to which they are attached to form an optionally substituted azetidine claim 2 , an optionally substituted oxetane claim 2 , an optionally substituted beta-lactam claim 2 , an optionally substituted tetrahydropyran claim 2 , an optionally substituted cyclopropyl claim 2 , an optionally substituted cyclobutyl claim 2 , an optionally substituted cyclopentyl claim 2 , or an optionally substituted cyclohexyl.711.-. (canceled)13. (canceled)15. (canceled)18. (canceled)20. (canceled)21. (canceled)22. (canceled)24. The compound or salt thereof of claim 1 , selected from compounds of Table 1 claim 1 , and pharmaceutically acceptable salts thereof.25. The compound or salt thereof of claim 1 , selected from compounds of Table 2 claim 1 , and pharmaceutically acceptable salts thereof.26. The compound or salt thereof of claim 1 , selected from compounds of Table 3 claim 1 , and pharmaceutically acceptable salts thereof.28. The compound or pharmaceutically acceptable salt thereof of claim 27 , wherein Rand Rare joined together with the atom to which they are attached to form an optionally substituted azetidine claim 27 , an optionally substituted oxetane claim 27 , an optionally substituted beta-lactam claim 27 , an optionally substituted tetrahydropyran claim 27 , an optionally ...

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21-03-2013 дата публикации

Polycyclic compounds as lysophosphatidic acid receptor antagonists

Номер: US20130072490A1
Принадлежит: Amira Pharmaceuticals Inc

Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases.

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28-03-2013 дата публикации

Benzisoxazoles and Azabenzisoxazoles as MGLUR4 Allosteric Potentiators, Compositions, and Methods of Treating Neurological Dysfunction

Номер: US20130079366A1
Принадлежит: VANDERBILT UNIVERSITY

Benzisoxazole and azabenzisoxazole compounds which are useful as allosteric potentiators/positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds, for example, in treating neurological and psychiatric disorders or other disease state associated with glutamate dysfunction. 2. The method of claim 1 , wherein the mammal is a human.3. The method of claim 1 , wherein the dysfunction is Parkinson's disease.4. The method of claim 1 , wherein the dysfunction is schizophrenia claim 1 , psychosis claim 1 , “schizophrenia-spectrum” disorder claim 1 , depression claim 1 , bipolar disorder claim 1 , cognitive disorder claim 1 , delirium claim 1 , amnestic disorder claim 1 , anxiety disorder claim 1 , attention disorder claim 1 , obesity claim 1 , eating disorder claim 1 , or NMDA receptor-related disorder.5. The method of claim 1 , wherein the dysfunction is Parkinson's disease; anxiety; motor effects after alcohol consumption; neurogenic fate commitment and neuronal survival; epilepsy; or certain cancers claim 1 , for example claim 1 , medulloblastoma claim 1 , inflammation (for example claim 1 , multiple sclerosis) and metabolic disorders (for example claim 1 , diabetes) and taste enhancing associated with glutamatergic dysfunction and diseases in which mGluR4 receptor is involved.6. The method of claim 1 , wherein the mammal has been diagnosed with the dysfunction prior to the administering step.7. The method of claim 1 , further comprising the step of identifying a mammal having a need for treatment of the dysfunction.8. The method of claim 1 , wherein the endogenous ligand for mGluR4 potentiation is glutamate claim 1 , L-SOP claim 1 , or a neurotransmitter.925-. (canceled)28. The compound of claim 26 , wherein one X is CRwith Rbeing H claim 26 , and the other X is N.29. The compound of claim 26 , wherein Y is O ...

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04-04-2013 дата публикации

CARBOXYLATION CATALYSTS

Номер: US20130085276A1
Принадлежит:

The use of a complex of the form Z—M—OR in the carboxylation of a substrate is described. The group Z is a two-electron donor ligand, M is a metal and OR is selected from the group consisting of OH, alkoxy and aryloxy. The substrate may be carboxylated at a C—H or N—H bond. The metal M may be copper, silver or gold. The two-electron donor ligand may be a phosphine, a carbene or a phosphite ligand. Also described are methods of manufacture of the complexes and methods for preparing isotopically labelled caboxylic acids and carboxylic acid derivatives. 134-. (canceled)25. A method of carboxylation of a substrate , the method comprising;{'sub': '2', 'contacting a complex of the form Z—M—OR ,wherein the group Z is a two-electron donor ligand, M is a metal, and OR is selected from the group consisting of OH, alkoxy and aryloxy; with a substrate and a source of CO.'}26. The method according to claim 25 , wherein the metal M is selected from the group consisting of copper claim 25 , silver and gold.27. The method according to claim 25 , wherein the carboxylation is carried out in the presence of a base.28. The method according to claim 27 , wherein the base is an alkali metal hydroxide or alkoxide.29. The method according to claim 25 , wherein the two-electron donor ligand Z is selected from the group consisting of phosphines claim 25 , carbenes claim 25 , or phosphites.30. The method according to claim 29 , wherein the two-electron donor ligand Z is a nitrogen containing heterocyclic carbene ligand.33. The method according to claim 26 , wherein the complex is selected from the group consisting of: [M(OH)(IMes)] claim 26 , [M(OH)(SIMes)] claim 26 , [M(OH)(IPr)] claim 26 , [M(OH)(ItBu)] claim 26 , and [M(OH)(SIPr)] claim 26 , where M is Au claim 26 , Ag or Cu.34. The method according to claim 25 , wherein the substrate is carboxylated at a C—H or N—H bond.35. The method according to claim 25 , wherein the substrate is a substituted or unsubstituted aromatic compound.36. The ...

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18-04-2013 дата публикации

Substituted carbamoylmethylamino acetic acid derivatives as novel NEP inhibitors

Номер: US20130096168A1
Принадлежит: NOVARTIS AG

The present invention provides a compound of formula I; 119-. (canceled)22. The compound according to wherein s is 0; or a pharmaceutically acceptable salt thereof.23. The compounds according to wherein{'sup': '2', 'Xis Cl, or a pharmaceutically acceptable salt thereof.'}24. The compound according to selected from:(S)-2-[(S)-2-(3′-chloro-biphenyl-4-yl)-1-(1H-tetrazol-5-ylcarbamoyl)-ethylamino]-propionic acid ethyl ester;(S)-2-[(S)-2-(3′-chloro-biphenyl-4-yl)-1-(1H-tetrazol-5-ylcarbamoyl)-ethylamino]-propionic acid; and(S)-2-[(S)-2-(3′-Chloro-biphenyl-4-yl)-1-(3-hydroxy-isoxazol-5-ylcarbamoyl)-ethylamino]-propionic acid; or a pharmaceutically acceptable salt thereof.25. A pharmaceutical composition comprising a compound according to or a pharmaceutically acceptable salt thereof and one or more pharmaceutically acceptable carriers.26. A pharmaceutical composition comprising a compound according to or a pharmaceutically acceptable salt thereof and one or more pharmaceutically acceptable carriers.27. A combination comprising: a compound according to claim 20 , or a pharmaceutically acceptable salt thereof and one or more therapeutically active agents selected from HMG-Co-A reductase inhibitor claim 20 , an anigiotensin receptor blocker claim 20 , angiotensin converting enzyme Inhibitor claim 20 , a calcium channel blocker claim 20 , an endothelin antagonist claim 20 , a renin inhibitor claim 20 , a diuretic claim 20 , an ApoA-I mimic claim 20 , an anti-diabetic agent claim 20 , an obesity-reducing agent claim 20 , an aldosterone receptor blocker claim 20 , an endothelin receptor blocker claim 20 , an aldosterone synthase inhibitors claim 20 , a CETP inhibitor and a phophodiesterase type 5 (PDE5) inhibitor.28. A combination comprising: a compound according to or a pharmaceutically acceptable salt thereof and one or more therapeutically active agents selected from HMG-Co-A reductase inhibitor claim 24 , an anigiotensin receptor blocker claim 24 , angiotensin converting ...

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25-04-2013 дата публикации

Process for Producing Imine Compounds for Combating Invertebrate Pests

Номер: US20130102462A1
Принадлежит: BASF SE

The present invention relates to a process for producing aromatic carbonyl compounds of formula I and aromatic imine compounds of formula III 145-. (canceled)48. The process as claimed in claim 46 , where Z is Br claim 46 , I or —OSO—R.49. The process as claimed in claim 48 , where Z is Br claim 48 , I or —OSO—R claim 48 , where Ris selected from the group consisting of CH claim 48 , CFand 4-methylphenyl claim 48 , and is preferably Br.50. The process as claimed in claim 46 , where carbon monoxide and hydrogen are used in a molar ratio of from 20:1 to 1:10.51. The process as claimed in claim 50 , where carbon monoxide and hydrogen are used in a molar ratio of from 2:1 to 1:2 and are preferably used in the form of synthesis gas.52. The process as claimed in claim 46 , where the catalyst is a group VIII metal complex.53. The process as claimed in claim 52 , where the metal is selected from the group consisting of Pd claim 52 , Pt claim 52 , Ni claim 52 , Rh claim 52 , Ir and Ru and is preferably Pd.54. The process as claimed in claim 46 , where the catalyst contains a monodentate and/or bidentate ligand.55. The process as claimed in claim 46 , where the catalyst contains a phosphorus-containing ligand.56. The process as claimed in claim 55 , where the phosphorus-containing ligand is a monodentate ligand selected from the group consisting of phosphorus compounds of formula PRRR claim 55 , where{'sup': a', 'b', 'c', 'd', 'e, 'sub': 3', '12', '3', '12', '3', '10', '3', '10', '5', '18', '5', '18, 'claim-text': or', {'sup': a', 'b', 'e, 'sub': 3', '10, 'Rand Rtogether with the phosphorus atom to which they are bound form a 5-, 6-, 7- or 8-membered heterocyclic ring which may be additionally fused to one, two or three C-C-cycloalkyl, heterocyclyl, aryl or hetaryl groups, where the heterocyclic ring and, if present, the fused-on groups may each independently carry one, two, three or four substituents R;'}, {'sup': d', '1', '2', '1', '2', '3+', '−, 'sub': 3', '10', '3', '10', ...

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25-04-2013 дата публикации

METHOD OF TREATING DIABETES, METABOLIC SYNDROME AND OBESITY USING PHENYLACETAMIDE DERIVATIVE

Номер: US20130102617A1
Принадлежит: Astellas Pharma Inc.

Phenylacetamide compounds of the formula 1. (canceled)2. The method of claim 18 , wherein n is 0.3. The method of claim 2 , wherein Ris methyl claim 2 , trifluoromethyl claim 2 , or cyclopropyl.4. The method of claim 3 , wherein Ris cyclopropyl.6. The method of claim 5 , wherein Ring A is pyrazolyl claim 5 , thiazolyl claim 5 , thiadiazolyl claim 5 , pyridyl or pyrazinyl claim 5 , each of which may be substituted with up to five moieties independently selected from the group consisting of halogen claim 5 , cyano claim 5 , lower alkyl which may be substituted with —OR claim 5 , —OR claim 5 , —O-lower alkylene —OR claim 5 , and —C(O)R.7. The method of claim 6 , wherein [Chem. 21] is a single bond.8. The method of claim 6 , wherein [Chem. 22] is a double bond.9. The method of claim 18 , wherein the compound is selected from the group consisting of:(2E)-2-[3-cyclopropyl-4-(cyclopropylsulfonyl)phenyl]-N-(5-methylpyrazin-2-yl)-3-[(1S)-3-oxocyclopentyl]acrylamide,(2E)-2-[3-cyclopropyl-4-(cyclopropylsulfonyl)phenyl]-N-(1-methyl-1H-pyrazol-3-yl)-3-[(1S)-3-oxocyclopentyl]acrylamide,(2E)-2-[3-cyclopropyl-4-(cyclopropylsulfonyl)phenyl]-N-(5-fluoro-1,3-thiazol-2-yl)-3-[(1S)-3-oxocyclopentyl]acrylamide,(2R)—N-(4-acetyl-1,3-thiazol-2-yl)-2-[3-cyclopropyl-4-(cyclopropylsulfonyl)phenyl]-3-[(1R)-3-oxocyclopentyl]propanamide,(2R)-2-[3-cyclopropyl-4-(cyclopropylsulfonyl)phenyl]-N-(5-methylpyridin-2-yl)-3-[(1R)-3-oxocyclopentyl]propanamide,(2R)-2-[3-cyclopropyl-4-(cyclopropylsulfonyl)phenyl]-N-(5-methylpyrazin-2-yl)-3-[(1R)-3-oxocyclopentyl]propanamide,(2R)-2-[3-cyclopropyl-4-(cyclopropylsulfonyl)phenyl]-N-[5-(hydroxymethyl)pyrazin-2-yl]-3-[(1R)-3-oxocyclopentyl]propanamide,(2R)—N-(5-chloropyrazin-2-yl)-2-[3-cyclopropyl-4-(cyclopropylsulfonyl)phenyl]-3-[(1R)-3-oxocyclopentyl]propanamide,(2R)-2-[3-cyclopropyl-4-(cyclopropylsulfonyl)phenyl]-N-(5-methoxypyrazin-2-yl)-3-[(1R)-3-oxocyclopentyl]propanamide,(2R)-2-[3-cyclopropyl-4-(cyclopropylsulfonyl)phenyl]-3-[(1R)-3-hydroxycyclopentyl]-N-(5 ...

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02-05-2013 дата публикации

C7-Fluoro Substituted Tetracycline Compounds

Номер: US20130109657A1
Принадлежит: Tetraphase Pharmaceuticals Inc

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

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23-05-2013 дата публикации

Compounds and Methods for Inhibiting the Interaction of BCL Proteins with Binding Partners

Номер: US20130131063A1
Принадлежит: INFINITY PHARMACEUTICALS, INC.

The invention relates to isoxazolidine containing compounds that bind to bcl proteins and inhibit Bcl function. The compounds may be used for treating and modulating disorders associated with hyperproliferation, such as cancer. 138-. (canceled)40. The method of claim 39 , wherein the bcl-mediated disorder is cancer or neoplastic disease.41. The method of claim 39 , wherein the bcl-mediated disorder is cancer.42. The method of claim 39 , wherein the bcl-mediated disorder is neoplastic disease.43. The method of claim 39 , wherein the bcl-mediated disorder is selected from the group consisting of acute leukemia claim 39 , acute lymphocytic leukemia claim 39 , acute myelocytic leukemia claim 39 , myeloblastic claim 39 , promyelocytic claim 39 , myelomonocytic claim 39 , monocytic claim 39 , erythroleukemia claim 39 , chronic leukemia claim 39 , chronic myelocytic (granulocytic) leukemia claim 39 , chronic lymphocytic leukemia claim 39 , polycythemia vera claim 39 , Hodgkin's disease claim 39 , non-Hodgkin's disease; multiple myeloma claim 39 , Waldenstrom's macroglobulinemia claim 39 , heavy chain disease claim 39 , fibrosarcoma claim 39 , myxosarcoma claim 39 , liposarcoma claim 39 , chondrosarcoma claim 39 , osteogenic sarcoma claim 39 , chordoma claim 39 , angiosarcoma claim 39 , endotheliosarcoma claim 39 , lymphangiosarcoma claim 39 , lymphangioendotheliosarcoma claim 39 , synovioma claim 39 , mesothelioma claim 39 , Ewing's tumor claim 39 , leiomyosarcoma claim 39 , rhabdomyosarcoma claim 39 , colon carcinoma claim 39 , pancreatic cancer claim 39 , breast cancer claim 39 , ovarian cancer claim 39 , prostate cancer claim 39 , squamous cell carcinoma claim 39 , basal cell carcinoma claim 39 , adenocarcinoma claim 39 , sweat gland carcinoma claim 39 , sebaceous gland carcinoma claim 39 , papillary carcinoma claim 39 , papillary adenocarcinomas claim 39 , stadenocarcinoma claim 39 , medullary carcinoma claim 39 , bronchogenic carcinoma claim 39 , renal cell carcinoma ...

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23-05-2013 дата публикации

PEST CONTROL COMPOSITION

Номер: US20130131115A1
Автор: Ikari Kaori
Принадлежит: Sumitomo Chemical Company, Limited

A pest control composition comprising a hydrazide compound shown by formula (1) below (in the formula, G, M, Q, Q, Q, Q, R, R, R, Rand m have the same meanings described in the specification) and etofenprox and a method for controlling pests whereby an effective dose of the hydrazide compound represented by formula (1) and etofenprox is applied to a pest or a pest habitat. 2. The pest control composition according to claim 1 , wherein in the formula (1) claim 1 , G is a group shown by G-1 claim 1 , Yis an oxygen atom claim 1 , Ris a trifluoromethyl group claim 1 , each of Q claim 1 , Q claim 1 , and Qis a CH group claim 1 , Qis a CRgroup claim 1 , Ris the group defined above claim 1 , (R)is a substituent at 3- and 5-positions claim 1 , m is 2 claim 1 , and Ris a chlorine atom.3. The pest control composition according to claim 1 , wherein in the formula (1) claim 1 , Ris a hydrogen atom.4. The pest control composition according to claim 1 , wherein in the formula (1) claim 1 , Ris a hydrogen atom or a methyl group.5. The pest control composition according to claim 1 , wherein in the formula (1) claim 1 , Ris a halogen atom.6. The pest control composition according to claim 1 , wherein in the formula (1) claim 1 , Ris a chlorine atom.7. The pest control composition according to claim 1 , wherein in the formula (1) claim 1 , Ris a C2 to C6 alkyl group claim 1 , a C1 to C6 haloalkyl group claim 1 , a C3 to C6 cycloalkyl group claim 1 , or a (C1 to C6 alkoxy) C1 to C6 alkyl group.8. The pest control composition according to claim 1 , wherein in the formula (1) claim 1 , Ris a C2 to C6 alkyl group.9. The pest control composition according to claim 1 , wherein in the formula (1) claim 1 , Ris a C1 to C6 haloalkyl group.10. The pest control composition according to claim 1 , wherein in the formula (1) claim 1 , Ris a C3 to C6 cycloalkyl group.11. The pest control composition according to claim 1 , wherein in the formula (1) claim 1 , Ris a (C1 to C6 alkoxy) C1 to C6 alkyl ...

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23-05-2013 дата публикации

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

Номер: US20130131321A1
Принадлежит: GRAFFINITY PHARMACEUTICALS GMBH

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

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30-05-2013 дата публикации

CRYSTALLINE FORM OF 4- [5 - [3 -CHLORO-5 - (TRIFLUOROMETHYL) PHENYL] -4, 5 - DIHYDRO - 5 - (TRIFLUOROMETHYL) -3 - ISOXAZOLYL] -N- [2-0X0-2- [ ( 2, 2, 2 - TRIFLUOROETHYL) AMINO] ETHYL] -1- NAPH-THALENECARBOXAMIDE

Номер: US20130137735A1
Автор: Currie Martin James
Принадлежит: E.I. Du Pont De Nemours and Company

Disclosed is a solid form of 4-[5-[3-chloro-5-(trifluoromethyl)phenyl]-4,5-dihydro-5-(trifluoromethyl)-3-isoxazolyl]-N-[2-oxo-2-[(2,2,2-trifluoroethyl)amino]ethyl]-1-naphthalenecarboxamide (Compound 1). Also disclosed are compositions containing a solid form of Compound 1 and methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a solid form of Compound 1 or a composition containing a solid form of Compound 1. 2. A composition comprising the polymorph Form B of and at least one additional component selected from the group consisting of surfactants claim 1 , solid diluents and liquid diluents claim 1 , said composition optionally further comprising at least one additional biologically active compound or agent.3. A composition for protecting an animal from an invertebrate parasitic pest comprising a parasiticidally effective amount of the polymorph Form B of and at least one carrier.4. The composition of in a dosage form for oral administration.5. A method for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of the polymorph Form B of .6. The method of wherein the environment is a plant.7. The method of wherein the environment is an animal. This invention relates to a solid form of 4-[5-[3-chloro-5-(trifluoromethyl)phenyl]-4,5-dihydro-5-(trifluoromethyl)-3-isoxazolyl]-N-[2-oxo-2-[(2,2,2-trifluoroethyl)amino]ethyl]-1-naphthalenecarboxamide.The solid state of chemical compounds can be amorphous (i.e. no long-range order in the positions of atoms) or crystalline (i.e. atoms arranged in an orderly repeating pattern). While only one crystal form is known for the solid state of many compounds, polymorphs have been discovered for some compounds. The term “polymorph” refers to a particular crystal form (i.e. structure of crystal lattice) of a chemical compound that can exist in more than one crystal ...

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30-05-2013 дата публикации

Nitrogen-containing heterocyclic compound and pest control agent

Номер: US20130137876A1
Принадлежит: Nippon Soda Co Ltd

The present invention offers compounds or their salts expressed by formula (I) (in the formula, X indicates an alkyl group, or the like; Y indicates an alkyl group; Z indicates a respectively independent nitro group, or the like; n indicates any integer from 0 to 3; A indicates carbon atom, or the like, and hydrogen atom is bonded thereto in the case where the carbon atom is not substituted with Z; D indicates oxygen atom, or the like; W indicates hydrogen atom, or the like; R 1 and R 2 indicate respectively independent hydrogen atoms, or the like; R 1 and R 2 may be bonded, and may form a heterocycle together with the nitrogen atom between R 1 and R 2 ).

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06-06-2013 дата публикации

Novel hydroxamates as therapeutic agents

Номер: US20130142758A1
Принадлежит: Pharmacyclics LLC

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

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06-06-2013 дата публикации

Stem cell differentiating agents and uses therefor

Номер: US20130143935A1
Принадлежит: University of Texas System

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

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06-06-2013 дата публикации

PRODUCTION METHOD OF ISOXAZOLINE-SUBSTITUTED BENZOIC ACID AMIDE COMPOUND

Номер: US20130144066A1
Принадлежит: NISSAN CHEMICAL INDUSTRIES, LTD.

A production method of an isoxazoline-substituted benzoic acid amide compound of Formula (1) where X is a halogen atom, Chaloalkyl, etc., Y is a halogen atom, Calkyl, etc., Ris a Chaloalkyl, etc., Rand Rindependently of each other are a hydrogen atom, Calkyl, etc., Ris Calkyl, Chaloalkyl, etc., Ris a hydrogen atom, Calkyl, etc., m is an integer of 0 to 5, n is an integer of 0 to 4, including: reacting an isoxazoline-substituted benzene compound of Formula (3) where X, Y, R, m, and n are the same as defined above, L is a chlorine atom, a bromine atom, —C(O)OH, —C(O)J, etc., J is a halogen atom, with a 2-aminoacetic acid amide compound of Formula (2) where R, R, R, and Rare the same as defined above, or a salt thereof; crystal forms and the production method thereof. 2. The crystal of claim 1 , wherein the crystal is a I-form crystal in which a diffraction angle (2θ) in a powder X-ray diffraction spectrum has peaks at 4.4° claim 1 , 8.7° claim 1 , 11.1° claim 1 , 13.1° claim 1 , 14.4° claim 1 , 17.7° claim 1 , 18.1° claim 1 , 18.8° claim 1 , 19.4° claim 1 , 21.2° claim 1 , 21.9° claim 1 , 22.3° claim 1 , 23.0° claim 1 , 23.9° claim 1 , 26.3° claim 1 , and 27.3°.3. The crystal of claim 2 , further comprising peaks at 14.8° claim 2 , 16.3° claim 2 , 16.9° claim 2 , 17.4° claim 2 , 24.5° claim 2 , and 25.0°.4. The crystal of claim 1 , wherein the crystal is a II-form crystal in which a diffraction angle (2θ) in a powder X-ray diffraction spectrum has peaks at 10.2° claim 1 , 12.3° claim 1 , 14.7° claim 1 , 15.9° claim 1 , 18.4° claim 1 , 20.1° claim 1 , 21.2° claim 1 , 22.0° claim 1 , 22.8° claim 1 , 24.6° claim 1 , and 26.6°.5. The crystal of claim 1 , wherein the crystal is a III-form crystal in which a diffraction angle (2θ) in a powder X-ray diffraction spectrum has peaks at 4.3° claim 1 , 8.7° claim 1 , 11.1° claim 1 , 14.4° claim 1 , 17.7° claim 1 , 18.7° claim 1 , 19.4° claim 1 , 19.9° claim 1 , 21.2° claim 1 , 21.8° claim 1 , 22.3° claim 1 , 23.8° claim 1 , and ...

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27-06-2013 дата публикации

BIPHENYL AND PHENYL-PYRIDINE AMIDES AS P2X3 AND P2X2/3 ANTAGONISTS

Номер: US20130165443A1
Принадлежит:

Compounds of the formula I: 2. The compound of claim 1 , wherein R claim 1 , Rand Rare hydrogen.3. The compound of claim 2 , wherein Ris phenyl substituted at the 4-position with methyl or halo and optionally substituted at the 2-position with halo.4. The compound of claim 2 , wherein Ris 4-methyl-phenyl.5. The compound of claim 2 , wherein Ris pyridin 2-yl substituted with methyl or halo at the 5-position.6. The compound of claim 2 , wherein Ris 5-methyl-pyridin-2-yl.8. The compound of claim 7 , wherein Ris hydrogen.9. The compound of claim 7 , wherein Ris methyl.10. The compound of claim 7 , wherein Ris: Calkyl; Calkyloxy-Calkyl; hydroxy-Calkyl; Calkylsulfanyl-Calkyl; Calkylsulfonyl-Calkyl; amino-Calkyl; N—Calkyl-amino-Calkyl; N claim 7 ,N-di-Calkyl-amino-Calkyl; Ccycloalkyl; optionally substituted phenyl; heteroaryl claim 7 , or heterocyclyl-Calkyl.11. The compound of claim 7 , wherein Ris: Calkyloxy-Calkyl; hydroxy-Calkyl; heteroaryl claim 7 , or heterocyclyl-Calkyl.12. The compound of claim 7 , wherein Ris methoxymethyl.13. The compound of claim 7 , wherein Ris hydroxymethyl.14. The compound of claim 7 , wherein Ris heteroaryl selected from pyridinyl claim 7 , pyrimidinyl claim 7 , or pyrazinyl claim 7 , each of which may be optionally substituted once or twice with methyl.15. The compound of claim 7 , wherein Ris hydroxymethyl claim 7 , methoxymethyl claim 7 , pyrazin-2-yl or 5-methyl-pyrazin-2-yl.16. The compound of claim 7 , wherein Ris Calkyl claim 7 , Ccycloalkyl or Ccycloalkyl-Calkyl.17. The compound of claim 7 , wherein Ris isopropyl claim 7 , isobutyl or tert butyl.18. The compound of claim 1 , wherein said compound is selected from:4-Methyl-thiophene-2-carboxylic acid [5-(2-methoxy-1-methyl-ethylcarbamoyl)-4′-methyl-biphenyl-3-yl]-amide;5-Methyl-thiophene-2-carboxylic acid [5-(2-methoxy-1-methyl-ethylcarbamoyl)-4′-methyl-biphenyl-3-yl]-amide;Furan-2-carboxylic acid [5-(2-methoxy-1-methyl-ethylcarbamoyl)-4′-methyl-biphenyl-3-yl]-amide;Thiophene-2- ...

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27-06-2013 дата публикации

Insecticidal compounds

Номер: US20130165490A1
Принадлежит: SYNGENTA CROP PROTECTION LLC

A compound of formula (I): wherein A 1 , A 2 , A 3 , A 4 , G 1 , G 2 , R 1 , R 2 , R 3 and R 4 are as defined in claim 1 ; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising them and to methods of using them to combat and control insect, acarine, nematode and mollusc pests.

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04-07-2013 дата публикации

NOVEL BENZENESULFONAMIDE COMPOUNDS, METHOD FOR SYNTHESIZING SAME, AND USE THEREOF IN MEDICINE AS WELL AS IN COSMETICS

Номер: US20130172363A1
Принадлежит: GALDERMA RESEARCH & DEVELOPMENT

Benzenesulfonamide compounds having a structure of formula (I) are described. Also described, are methods for synthesizing the compounds and to the use thereof in pharmaceutical compositions for human or veterinary medicine and in cosmetic compositions. 1. A compound having the name (S)—N-hydroxy-3-[4-(2-methylquinolin-4-ylmethoxy)benzenesulfonylamino]-2-[4-(propane-2-sulfonyl)piperazin-1-yl]propionamide.2. A composition comprising the compound as claimed in claim 1 , and an acceptable carrier.3. A pharmaceutical composition comprising the compound claim 1 , as claimed in and a pharmaceutically acceptable carrier.5. The compound as claimed in claim 4 , in which{'sub': '4', 'Ris an alkyl radical containing 1 to 4 carbon atoms; and'}{'sub': '3', 'Ris a polycyclic aromatic heterocylic radical containing the heteroatom N;'}and salts thereof, and enantiomers thereof.6. The compound as claimed in claim 4 , wherein the compound is (S)—N-hydroxy-3-[4-(2-methylquinolin-4-ylmethoxy)benzenesulfonylamino]-2-[4-(propane-2-sulfonyl)piperazin-1-yl]propionamide claim 4 , and salts thereof claim 4 , and enantiomers thereof.7. A composition comprising the compound as claimed in claim 4 , or a salt thereof claim 4 , or an enantiomer thereof claim 4 , and an acceptable carrier.8. A pharmaceutical composition comprising the compound as claimed in claim 4 , a salt thereof claim 4 , or an enantiomer thereof claim 4 , and a pharmaceutically acceptable carrier.9. A method of treating an inflammatory skin disease claim 3 , wherein the method comprises administering the pharmaceutical composition as claimed in claim 3 , to a subject in need thereof.10. The method of claim 9 , wherein the inflammatory skin disease is psoriasis or atopic dermatitis.11. A method of treating an inflammatory skin disease claim 8 , wherein the method comprises administering the pharmaceutical composition as claimed in claim 8 , to a subject in need thereof.12. The method of claim 11 , wherein the inflammatory skin ...

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04-07-2013 дата публикации

CHIRAL SYNTHESIS OF ISOXAZOLINES, ISOXAZOLINE COMPOUNDS, AND USES THEREOF

Номер: US20130172553A1
Принадлежит: CPSI STOCKHOLDER TRUST

Processes for the chiral syntheses of isoxazolines and intermediates are described. Compounds prepared thereby, and methods of using the compounds are also described. 6. The process of claim 5 , wherein the separating is carried out by a process comprising recrystallization claim 5 , chromatography claim 5 , or a combination thereof.9. The process of claim 8 , wherein the separating is carried out by a process comprising recrystallization claim 8 , chromatography claim 8 , or a combination thereof.11. The process of claim 1 , wherein R claim 1 , R claim 1 , R claim 1 , R claim 1 , and Rare each independently hydrogen claim 1 , an alkyl group claim 1 , a cycloalkyl group claim 1 , an alkenyl group claim 1 , an alkynyl group claim 1 , an oxo group claim 1 , an aryl group claim 1 , a heterocyclic group claim 1 , a heteroaryl group claim 1 , an aralkyl group claim 1 , a heteroaralkyl group claim 1 , an amino group claim 1 , an alkylamino group claim 1 , a dialkylamino group claim 1 , an amidine group claim 1 , an amide group claim 1 , an alkylcarbonyl group claim 1 , an alkoxycarbonyl group claim 1 , an alkylaminocarbonyl group claim 1 , a dialkylamino carbonyl group claim 1 , an arylcarbonyl group claim 1 , an aryloxycarbonyl group claim 1 , an alkylsulfonyl group claim 1 , an arylsulfonyl group claim 1 , perhaloalkyl group claim 1 , a perhalocycloalkyl group claim 1 , a perhaloalkenyl group claim 1 , a perhaloalkynyl group claim 1 , a perhaloaryl group claim 1 , or a perhaloaralkyl group; wherein Rand Rmay be taken together to form a cyclic group; wherein Rand Rmay be taken together to form a cyclic group; wherein each group may be optionally and independently straight or branched; wherein each group may be optionally and independently substituted by one or more independent substituents; and wherein one or more than one atom in each group may be optionally and independently replaced with one or more independent heteroatoms.12. The process of claim 1 , wherein R claim ...

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11-07-2013 дата публикации

ISOXAZOLE TREATMENTS FOR DIABETES

Номер: US20130178506A1

The present invention relates to compounds and methods for inducing synthesis and secretion of insulin from pancreatic beta cells. The methods may take place in vitro, ex vivo such as in isolates from adult mammalian tissue, or in vivo. Compounds and methods described herein may find use in the treatment of diabetes. 2. The method of claim 1 , wherein Ris a substituent of formula (A).3. The method of claim 2 , wherein G is S.4. The method of claim 3 , wherein R claim 3 , Ror Ris hydrogen.5. The method of claim 4 , wherein R claim 4 , Rand Rare each hydrogen.6. The method according to claim 1 , wherein Ris hydrogen.7. The method according to claim 1 , wherein Ris —NRR.8. The method of claim 7 , wherein Ror Ris cyclopropyl claim 7 , cyclobutyl claim 7 , cyclopentyl or cyclohexyl.9. The method of claim 8 , wherein Ror Ris cyclopropyl.11. The method of claim 10 , wherein G is S.12. The method of claim 11 , wherein R claim 11 , Ror Ris hydrogen.13. The method of claim 12 , wherein R claim 12 , Rand Rare each hydrogen.14. The method according to claim 1 , wherein Ris hydrogen.15. The method according to claim 1 , wherein Ris cyclopropyl or an aliphaticalcohol or an aliphaticpolyol.17. The method according to claim 1 , wherein said cell is located in an animal subject.18. The method according to claim 1 , wherein said cell is contacted ex vivo.2036-. (canceled)3852-. (canceled)5470-. (canceled)72. (canceled) This application claims benefit of priority to U.S. Provisional Application Ser. Nos. 61/563,419, filed Nov. 23, 2011, and 61/566,056, filed Dec. 2, 2011, the entire contents of both applications being incorporated by reference herein.The invention was made with government support under NIH P60 DK079626, R37 DK34128 and R01 DK55310 awarded by the National Institutes of Health. The government has certain rights in the invention.1. Field of the InventionThe present invention relates generally to the fields of cell biology, developmental biology and medicine. More ...

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18-07-2013 дата публикации

N-((3-BENZYL)-2,2-(BIS-PHENYL)-PROPAN-1-AMINE DERIVATIVES AS CETP INHIBITORS FOR THE TREATMENT OF ATHEROSCLEROSIS AND CARDIOVASCULAR DISEASES

Номер: US20130184279A1
Принадлежит: BRISTOL-MYERS SQUIBB COMPANY

Compounds of formula Ia and Ib 2. The compound of claim 1 , wherein A is:{'sub': 1', '6', '40', '46', '1', '6', '29', '30', '40', '40', '40', '40', '40', '40', '1', '6, "(a) phenyl, which is substituted with one or more substituents selected from the group consisting of: 1) halo, 2) (C-C)-alkyl, which may be optionally substituted with one or more R's, 3) —OR, 4) (C-C)-alkylthio, 5) cyano, 6) nitro, 7) —NRR, 8) aryl, which may be optionally substituted with one or more R's, 9) arylalkyl, which may be optionally substituted with one or more R's, 10) heteroaryl, which may be optionally substituted with one or more R's, 11) heteroarylalkyl, which may be optionally substituted with one or more R's, 12) heterocyclyl, which may be optionally substituted with one or more R's, 13) heterocyclylalkyl, which may be optionally substituted with one or more R's, 14) halo(C-C)alkyl,"}{'sub': 46', 'p', '46', '2', '46', '46, '15) —COR, 16) ═O, 17) —S(O)R, 18) —SONHR, 19) —COOR,'}{'sub': 46', '46', '46', '2', '6', '40', '2', '6', '40', '46', '46', '46', '46', '40, "20) —NHC(CN)NHR, 21) —CONRR, 22) (C-C)-alkynyl, which may be optionally substituted with one or more R's, 23) (C-C)-alkenyl, which may be optionally substituted with one or more R's, 24) —OCOR, 25) —OCOOR, or 26) —OCONRR; or any two adjacent substituents may join together to form a 4- to 8-membered ring, which optionally may contain 1-4 heteroatoms selected from N, O, and S and be optionally substituted with one or more R's;"}{'sub': 1', '6', '40', '46', '1', '6', '29', '30', '40', '40', '40', '40', '40', '40', '1', '6, "(b) heteroaryl, which is substituted with one or more substituents selected from the group consisting of: 1) halo, 2) (C-C)-alkyl, which may be optionally substituted with one or more R's, 3) —OR, 4) (C-C)-alkylthio, 5) cyano, 6) nitro, 7) —NRR, 8) aryl, which may be optionally substituted with one or more R's, 9) arylalkyl, which may be optionally substituted with one or more R's, 10) heteroaryl, which ...

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18-07-2013 дата публикации

Sulfonyl compounds which modulate the cb2 receptor

Номер: US20130184315A1
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

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

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25-07-2013 дата публикации

MODIFIED MACROPHAGE MIGRATION INHIBITORY FACTOR INHIBITORS

Номер: US20130190369A1
Автор: Al-Abed Yousef

Provided are various compounds of Formula I (I). Also provided are various compounds of Formula II (II). Also provided are pharmaceutical compositions comprising the above compounds. Additionally, methods of inhibiting macrophage migration inhibitory factor (MIF) activity in a mammal are provided, as are methods of treating or preventing inflammation in a mammal. Further provided are methods of treating a mammal having sepsis, septicemia, and/or endotoxic shock. Also provided are methods of treating a mammal having an autoimmune disease, and methods of treating a mammal having a tumor. 136-. (canceled)38. The compound of claim 37 , wherein R2 is F.41. A pharmaceutical composition comprising the compound of in a pharmaceutically acceptable excipient. This application claims the benefit of U.S. Provisional Application No. 60/785,898, filed Mar. 24, 2006.(1) Field of the InventionThe present invention relates to cytokine inhibitors. More specifically, the present invention identifies and characterizes several inhibitors of macrophage migration inhibitory factor.(2) Description of the Related ArtMacrophage migration inhibitory factor (MIF) is a proinflammatory cytokine, critically involved in the pathogenesis of inflammatory disorders (Calandra and Roger, 2003; Riedemann et al., 2003). Recent studies have clearly defined MN as a critical factor in the pathophysiology of sepsis (Al-Abed et al., 2005). Abolition of MIF activity during sepsis by antibodies or ISO-1 improves cardio-circulatory efficiency and prevents the lethality associated with sepsis (Al-Abed et al., 2005; Lin et al., 2005). The specific inhibitor ISO-1, an isoxazoline, was designed to fit into the hydrophobic active site of MIF, an interaction confirmed by the crystal structure of the MIF complex with ISO-1 () (Lubetsky et al., 2002). Administration of ISO-1 in a clinically relevant model of sepsis confers moderate protection (80% versus 40% control). These results identify ISO-1 as the first small ...

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08-08-2013 дата публикации

PARASITICIDAL ORAL VETERINARY COMPOSITIONS COMPRISING SYSTEMICALLY-ACTING ACTIVE AGENTS, METHODS AND USES THEREOF

Номер: US20130203692A1
Принадлежит: MERIAL LIMITED

This invention relates to oral veterinary compositions for combating ectoparasites and endoparasites in animals, comprising at least one systemically-acting active agent in combination with a pharmaceutically acceptable carrier. This invention also provides for improved methods for eradicating, controlling, and preventing parasite infections and infestations in an animal comprising administering the compositions of the invention to the animal in need thereof. 2. The soft chewable veterinary composition of claim 1 , wherein:W is O;{'sup': '4', 'sub': 1', '6, 'Ris H or C-Calkyl;'}{'sup': '5', 'sub': 2', '2', '3, 'Ris —CHC(O)NHCHCF;'}{'sup': 1', '2', '3', '4', '5', '6, 'each of A, A, A, A, Aand Ais CH;'}{'sup': 1', '6, 'sub': 1', '6, 'Ris C-Calkyl each optionally substituted with one or more substituents independently selected from R;'}{'sup': '6', 'sub': 1', '6, 'Ris halogen or C-Calkyl; and'}{'sup': 1', '2', '3, 'sub': 1', '6', '1', '6', '1', '6, 'B, B, and Bare independently CH, C-halogen, C—C-Calkyl, C—C-Chaloalkyl, or C—C-Calkoxy.'}3. The soft chewable veterinary composition of claim 1 , wherein:W is O;{'sup': '1', 'sub': '3', 'Ris CF;'}{'sup': '2', 'Bis CH;'}{'sup': '1', 'Bis C—Cl;'}{'sup': '3', 'sub': '3', 'Bis C—CF;'}{'sup': 1', '2', '3', '4', '5', '6, 'each of A, A, A, A, Aand Ais CH;'}{'sup': '4', 'Ris H; and'}{'sup': '5', 'sub': 2', '2', '3, 'Ris —CHC(O)NHCHCF.'}4. The soft chewable veterinary composition of claim 1 , wherein the carrier comprises one or more fillers claim 1 , at least one flavoring agent claim 1 , at least one binder claim 1 , one or more solvents claim 1 , one or more surfactants claim 1 , at least one humectant claim 1 , optionally an antioxidant claim 1 , and optionally a preservative.5. The soft chewable veterinary composition of claim 4 , wherein the one or more fillers is soy protein fines claim 4 , corn starch claim 4 , or a mixture thereof.6. The soft chewable veterinary composition of claim 4 , wherein the binder is ...

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08-08-2013 дата публикации

ACYLSULFONAMIDES AND PROCESSES FOR PRODUCING THE SAME

Номер: US20130203709A1
Принадлежит:

The present disclosure relates to acylsulfonamides and processes for their preparation. The processes involve a target-guided synthesis approach, whereby a thioacid and a sulfonyl azide are reacted in the presence of a biological target protein, a Bcl-2 family protein, to form the acylsulfonamide. 2. The compound of wherein the Bcl-2 family protein is Mcl-1.3. A composition comprising a Bcl-2 claim 1 , Bcl-XL claim 1 , and/or Bcl-w inhibitor; and an Mcl-1 and/or A1/Bfl-1 inhibitor claim 1 , wherein at least one inhibitor is the compound of .4. A method of treating or preventing cancer claim 1 , the method comprising administering the compound of .5. A compound comprising a first fragment selected from SZ1 to SZ31 and a second fragment selected from TA1 to TA15.6. The compound of having the formula selected from SZ31TA2 claim 5 , SZ15TA2 claim 5 , and SZ17TA2.7. A method of screening for an inhibitor claim 5 , as described herein.8. The method of comprising contacting a fragment library with a Bcl-2 family protein.9. The method of wherein the Bcl-2 family protein is selected from one or more of Bcl-2 claim 8 , Bcl-XL claim 8 , Bcl-w claim 8 , Mcl-1 claim 8 , and A1/Bfl-1.10. The method of wherein the Bcl-2 family protein is Mcl-1.11. The compound of claim 1 , wherein Zis aryl claim 1 , substituted aryl claim 1 , or heteroaryl.13. The compound of claim 1 , wherein Z claim 1 , Z claim 1 , Z claim 1 , Z claim 1 , and Zare independently hydrogen claim 1 , hydrocarbyl claim 1 , substituted hydrocarbyl claim 1 , amino claim 1 , alkoxy claim 1 , nitro claim 1 , or trihalomethoxy.15. The compound of claim 1 , wherein Zis substituted or unsubstituted furyl claim 1 , thienyl claim 1 , pyridyl claim 1 , oxazolyl claim 1 , isoxazolyl claim 1 , imidazolyl claim 1 , pyridyl claim 1 , pyrimidyl claim 1 , purinyl claim 1 , triazolyl claim 1 , or thiazolyl.16. The compound of claim 1 , wherein Zis substituted or unsubstituted morpholino claim 1 , pyran claim 1 , tetrahydropyran claim ...

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22-08-2013 дата публикации

Arylsulfonamide ccr3 antagonists

Номер: US20130217687A1
Принадлежит: Axikin Pharmaceuticals Inc

Provided herein are arylsulfonamides that are useful for modulating CCR3 activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a CCR3-mediated disorder, disease, or condition.

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22-08-2013 дата публикации

Naphthalene Isoxazoline Invertebrate Pest Control Agents

Номер: US20130217736A1
Принадлежит:

Disclosed are compounds of Formula 1, 2. A compound of wherein{'sup': '4', 'Ris H; and'}{'sup': '5', 'sub': 1', '6', '1', '6', '1', '6', '1', '6', '2', '7', '2', '7, 'Ris C-Calkyl substituted with one substituent independently selected from C-Calkylthio, C-Calkylsulfinyl, C-Calkylsulfonyl, C-Calkylaminocarbonyl and C-Chaloalkylaminocarbonyl.'}3. A compound of wherein{'sup': '1', 'sub': '3', 'Ris Cl, Br or CF;'}{'sup': '2', 'Ris H; and'}{'sup': '3', 'sub': '3', 'Ris H, F, Cl, Br or CF.'}4. A compound of wherein{'sup': '1', 'sub': '3', 'Ris CF.'}5. A compound of wherein{'sup': '3', 'sub': '3', 'Ris Cl, Br or CF.'}6. A compound of wherein{'sup': '5', 'sub': 1', '6', '2', '7', '3', '7, 'Ris C-Calkyl substituted with one C-Calkylaminocarbonyl or C-Chaloalkylaminocarbonyl.'}7. A compound of that is selected from the group consisting of4-[5-[3-chloro-5-(trifluoromethyl)phenyl]-4,5-dihydro-5-(trifluoromethyl)-3-isoxazolyl]-N-[2-(methylsulfonyl)ethyl]-1-naphthalenecarboxamide,4-[5-[3-bromo-5-(trifluoromethyl)phenyl]-4,5-dihydro-5-(trifluoromethyl)-3-isoxazolyl]-N-[2-(methylsulfonyl)ethyl]-1-naphthalenecarboxamide,4-[5-[3,5-bis(trifluoromethyl)phenyl]-4,5-dihydro-5-(trifluoromethyl)-3-isoxazolyl]-N-[2-(methylsulfonyl)ethyl]-1-naphthalenecarboxamide,4-[5-[3-chloro-5-(trifluoromethyl)phenyl]-4,5-dihydro-5-(trifluoromethyl)-3-isoxazolyl]-N-[2-(methylamino)-2-oxoethyl]-1-naphthalenecarboxamide,4-[5-[3-chloro-5-(trifluoromethyl)phenyl]-4,5-dihydro-5-(trifluoromethyl)-3-isoxazolyl]-N-[2-(ethylamino)-2-oxoethyl]-1-naphthalenecarboxamide,4-[5-[3-chloro-5-(trifluoromethyl)phenyl]-4,5-dihydro-5-(trifluoromethyl)-3-isoxazolyl]-N-[2-[(1-methylethyl)amino]-2-oxoethyl]-1-naphthalenecarboxamide,4-[5-[3-chloro-5-(trifluoromethyl)phenyl]-4,5-dihydro-5-(trifluoromethyl)-3-isoxazolyl]-N-[2-oxo-2-[(2,2,2-trifluoroethyl)amino]ethyl]-1-naphthalenecarboxamide,4-[5-[3-bromo-5-(trifluoromethyl)phenyl]-4,5-dihydro-5-(trifluoromethyl)-3-isoxazolyl]-N-[2-(methylamino)-2-oxoethyl]-1- ...

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22-08-2013 дата публикации

SYNTHESIS OF ENONE INTERMEDIATE

Номер: US20130217886A1

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. 1102-. (canceled)104. The method of claim 103 , wherein Ris hydrogen.105. The method of claim 103 , wherein Rand Rare hydrogen.106. The method of claim 103 , wherein Ris —N(R).107. The method of claim 106 , wherein Ris —N(CH).108. The method of claim 103 , wherein n is not 0 claim 103 , and at least one instance of Ris halogen.109. The method of claim 103 , wherein n is not 0 claim 103 , and at least one instance of Ris —NHC(O)R.110. The method of claim 103 , wherein n is not 0 claim 103 , and at least one instance of Ris —OR.111. The method of claim 103 , wherein n is not 0 claim 103 , and at least one instance of Ris cyclic or acyclic claim 103 , substituted or unsubstituted claim 103 , branched or unbranched heteroaliphatic.112. The method of claim 103 , wherein deprotecting the enolate of the ketone (VII) under suitable conditions comprises use of BBror BCl.114. The method of claim 113 , wherein the lipase is Amano Lipase AK.115. The method of claim 113 , wherein the suitable conditions comprise the presence of vinyl acetate.117. The method of claim 116 , wherein the vinyl reagent is a metal vinyl reagent. The present application is a continuation of and claims priority under 35 U.S.C. §120 to U.S. patent application Ser. No. 13/043,742, filed Mar. 9, 2011, which is a continuation of and claims priority under 35 U.S.C. §120 to U.S. patent application Ser. No. 12/833,628, filed Jul. ...

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29-08-2013 дата публикации

2-(benzyloxy) benzamides as lrrk2 kinase inhibitors

Номер: US20130225584A1
Принадлежит: Individual

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, for example Parkinson's disease or Alzheimer's disease.

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29-08-2013 дата публикации

COMPOUNDS, COMPOSITIONS, PROCESSES OF MAKING, AND METHODS OF USE RELATED TO INHIBITING MACROPHAGE MIGRATION INHIBITORY FACTOR

Номер: US20130225586A1
Принадлежит: CPSI STOCKHOLDER TRUST

The present invention provides a compound having Formula I or II: 2. The compound of claim 1 , which is a compound having Formula I claim 1 , a pharmaceutically acceptable salt thereof or a pharmaceutically acceptable prodrug thereof.3. The compound of claim 1 , which is a compound having Formula II claim 1 , a pharmaceutically acceptable salt thereof or a pharmaceutically acceptable prodrug thereof.7. The compound of claim 1 , wherein B is oxygen.8. The compound of claim 1 , wherein R and Rare each independently selected from the group consisting of hydrogen claim 1 , (C-C)cycloalkyl claim 1 , (C-C)alkoxy claim 1 , (C-C)alkyl claim 1 , phenyl claim 1 , (C-C)heteroaryl claim 1 , (C-C)heterocyclic and (C-C)cycloalkyl; wherein each of the aforesaid (C-C)alkyl claim 1 , phenyl claim 1 , (C-C)heteroaryl claim 1 , (C-C)heterocyclic and (C-C)cycloalkyl substituents may optionally be substituted by one to four moieties independently selected from the group consisting of halo claim 1 , (C-C)alkyl claim 1 , (C-C)alkenyl claim 1 , (C-C)alkynyl claim 1 , perhalo(C-C)alkyl claim 1 , phenyl claim 1 , (C-C)heteroaryl claim 1 , (C-C)heterocyclic claim 1 , (C-C)cycloalkyl claim 1 , hydroxy claim 1 , (C-C)alkoxy claim 1 , perhalo(C-C)alkoxy claim 1 , phenoxy claim 1 , (C-C)heteroaryl-O— claim 1 , (C-C)heterocyclic-O— claim 1 , (C-C)cycloalkyl-O— claim 1 , (C-C)alkyl-S—; wherein two independently chosen Ralkyl-containing groups may be taken together with any nitrogen atom to which they are attached to form a three to forty membered claim 1 , cyclic heterocyclic or heteroaryl ring.9. The compound of claim 1 , wherein R and Rare each independently selected from the group consisting of hydrogen claim 1 , (C-C)cycloalkyl claim 1 , (C-C)alkoxy claim 1 , (C-C)alkyl claim 1 , phenyl claim 1 , (C-C)heteroaryl claim 1 , (C-C)heterocyclic and (C-C)cycloalkyl; wherein each of the aforesaid (C-C)alkyl claim 1 , phenyl claim 1 , (C-C)heteroaryl claim 1 , (C-C)heterocyclic and (C-C)cycloalkyl ...

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29-08-2013 дата публикации

OXAZOLINE AND ISOXAZOLINE DERIVATIVES AS CRAC MODULATORS

Номер: US20130225600A1
Принадлежит: Lupin Limited

The present invention relates to compounds of Formula (I) along with processes for their preparation that are useful for treating, preventing and/or managing the diseases, disorders, syndromes or conditions associated with the modulation of CRAC. The invention further relates to methods of treating, preventing managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of CRAC of Formula (I). 8. The compound of claim 1 , wherein ring W is selected from aryl claim 1 , heteroaryl and cycloalkyl.9. The compound of claim 1 , wherein L is —C(O)NR— or —NRC(O)—;{'sub': '11', 'where Ris hydrogen or alkyl.'}11. The compound of claim 1 , which is selected from:N-(5-(5-(5,5-Dimethyl-4-oxo-4,5-dihydroisoxazol-3-yl)-2-methylphenyl)pyrazine-2-yl)-2,6-difluorobenzamide,N-(5-(5-(5,5-Dimethyl-4-oxo-4,5-dihydroisoxazol-3-yl)-2-methylphenyl)pyrazin-2-yl)-4-methyl-1,2,3-thiadiazole-5-carboxamide,N-(5′-(5,5-Dimethyl-4-oxo-4,5-dihydroisoxazol-3-yl)-2′-methyl-[1,1′-biphenyl]-4-yl-2,6-difluorobenzamide,N-(5-(5-(5,5-Dimethyl-4-oxo-4,5-dihydroisoxazol-3-yl)-2-methylphenyl)pyridin-2-yl)-2,6-difluorobenzamide,N-(5-(5-(5,5-dimethyl-4-oxo-4,5-dihydroisoxazol-3-yl)-2-ethylphenyl)pyrazin-2-yl)-2,6-difluorobenzamide,N-(5′-(5,5-dimethyl-4-oxo-4,5-dihydroisoxazol-3-yl)-2′-ethyl-[1,1′-biphenyl]-4-yl)-2,6-difluorobenzamide,N-(6-(5-(5,5-dimethyl-4-oxo-4,5-dihydroisoxazol-3-yl)-2-ethylphenyl)pyridin-3-yl)-2,6-difluorobenzamide,N-(5-(5-(5,5-dimethyl-4-oxo-4,5-dihydroisoxazol-3-yl)-2-isopropylphenyl)pyrazin-2-yl)-2,6-difluorobenzamide,N-(5′-(5,5-dimethyl-4-oxo-4,5-dihydroisoxazol-3-yl)-2′-isopropyl-[1,1′-biphenyl]-4-yl)-2,6-difluorobenzamide,N-(2′-(tert-butyl)-5′-(5,5-dimethyl-4-oxo-4,5-dihydroisoxazol-3-yl)-[1,1′-biphenyl]-4-yl)-2,6-difluorobenzamide,N-(2′-chloro-5′-(5,5-dimethyl-4 oxo-4,5-dihydroisoxazol-3-yl)-[1,1′-biphenyl]-4-yl)-2,6-difluorobenzamide,N-(5-(5-(5,5-dimethyl-4-oxo-4,5-dihydroisoxazol-3-yl)-2-fluorophenyl)pyrazin-2-yl)-2,6-difluorobenzamide,N ...

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29-08-2013 дата публикации

Method for preparing substituted isoxazoline compounds and their precursors 4-chloro, 4-bromo- or 4-iodobenzaldehyde oximes

Номер: US20130225826A1
Принадлежит: BASF SE

The present invention relates to a method for preparing 4-chloro-, 4-bromo- or 4-iodobenzaldehyde oximes and phenyl-substituted isoxazoline compounds prepared from these oximes. 129-. (canceled)32. The method as claimed in claim 30 , where step (ii) is carried out at a pH of at least 5.1.33. The method as claimed in claim 32 , where step (ii) is carried out at a pH of 5.1 to 14.34. The method as claimed in claim 30 , where step (ii) is carried out in the presence of a Cu(I) salt.35. The method as claimed in claim 34 , where the Cu(I) salt is generated in situ by carrying out step (ii) in the presence of a Cu(II) salt and a reduction agent.36. The method as claimed in claim 35 , where the reduction agent is selected from the group consisting of sulfite salts claim 35 , dithionite salts claim 35 , thiosulfate salts claim 35 , meta-bisulfite salts claim 35 , hydroxymethanesulfinate salts claim 35 , SnCl claim 35 , Zn and hydrazine.37. The method as claimed in claim 30 , where in step (ii) the diazonium salt is added to a solution containing the formoxime claim 30 , a copper salt and claim 30 , if the copper salt is a Cu(II) salt claim 30 , also a reduction agent.38. The method as claimed in claim 37 , where the diazonium salt is cooled to -10 to +15° C. before being added to the solution containing the formoxime claim 37 , a copper salt and claim 37 , if the copper salt is a Cu(II) salt claim 37 , also a reduction agent.39. The method as claimed in claim 37 , where the solution containing the formoxime claim 37 , a copper salt and claim 37 , if the copper salt is a Cu(II) salt claim 37 , also a reduction agent claim 37 , is adjusted to a pH of >5 claim 37 , before the diazonium salt is added.40. The method as claimed in claim 30 , where in the course of the reaction of step (ii) the pH is controlled continuously or periodically and if necessary adjusted to a pH of >5.41. The method as claimed in claim 30 , where the adjustment of the pH is performed by using a system ...

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05-09-2013 дата публикации

Ethynylbenzene derivatives

Номер: US20130231323A1
Автор: Eric J. Toone, Pei Zhou
Принадлежит: Duke University

Disclosed are compounds of formulae (I), (II), and (II)I: and pharmaceutically acceptable salts thereof, wherein the variables, R, R 1 , R 2 , R 3 , R 101 , L, D, Q, Y, X, and Z are defined herein. These compounds are useful for treating Gram-negative bacteria infections.

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05-09-2013 дата публикации

ARYLCYCLOPROPYLAMINE BASED DEMETHYLASE INHIBITORS OF LSD1 AND THEIR MEDICAL USE

Номер: US20130231342A1
Принадлежит: Oryzon Fenomics S.A.

The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula (I) as described and defined herein, and their use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection. Thus, in one specific aspect the invention relates to formulas (II), (III), (IV), (V), (VI), (VII), (VIII), (IX). 2. The compound of wherein (A) is an aryl group or a heteroaryl group claim 1 , wherein said aryl group or said heteroaryl group has n substituents (R3).3. The compound of wherein (A) is phenyl claim 1 , pyridinyl claim 1 , thiophenyl claim 1 , pyrrolyl claim 1 , furanyl claim 1 , or thiazolyl claim 1 , and further wherein (A) has n substituents (R3).4. The compound of wherein (A) is phenyl or pyridyl claim 1 , and further wherein said phenyl or said pyridyl has n substituents (R3).5. The compound of wherein (A) has 0 substituents (R3).6. The compound of wherein (B) is —O—CH-phenyl or phenyl claim 1 , and further wherein said phenyl or the phenyl moiety comprised in said —O—CH-phenyl has n substituents (R2).78-. (canceled)9. The compound of wherein (B) has 0 claim 1 , 1 or 2 substituents (R2).10. (canceled)11. The compound of wherein (D) is thiazolyl claim 1 , oxadiazolyl claim 1 , oxazolyl claim 1 , isoxazolyl claim 1 , thiadiazolyl claim 1 , triazinyl claim 1 , pyridazinyl claim 1 , pyrazinyl claim 1 , pyridinyl or pyrimidinyl claim 1 , and further wherein said thiazolyl claim 1 , said oxadiazolyl claim 1 , said oxazolyl claim 1 , said isoxazolyl claim 1 , said thiadiazolyl claim 1 , said triazinyl claim 1 , said pyridazinyl claim 1 , said pyrazinyl claim 1 , said pyridinyl or said pyrimidinyl has one substituent (R1).12. The compound of wherein (D) is thiazolyl claim 1 , oxadiazolyl or pyrimidinyl claim 1 , and further wherein said thiazolyl claim 1 , said oxadiazolyl or said pyrimidinyl has one substituent (R1).13. The compound of wherein (D) is oxadiazolyl ...

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05-09-2013 дата публикации

NOVEL ORGANOMETALLIC COMPLEXES WHICH EMIT IN THE RED TO GREEN SPECTRAL REGION AND THEIR USE IN OLEDS

Номер: US20130231489A1
Принадлежит: BASF SE

Organometallic complexes which bear at least one ligand which has a unit having a triplet energy of at least 22 000 cm, a process for preparing the organometallic complexes, a mixture comprising at least one inventive organometallic complex, the use of the organometallic complexes or of the mixture in organic light-emitting diodes, the organometallic complexes preferably being used as emitter materials, and specific nitrogen- or phosphorus-substituted triphenylene derivatives and a process for their preparation. 216-. (canceled) The present invention relates to organometallic complexes which bear at least one ligand which has a unit having a triplet energy of at least 22 000 cm, to a process for preparing the organometallic complexes, to a mixture comprising at least one inventive organometallic complex, to the use of the organometallic complexes or of the mixture in organic light-emitting diodes, the organometallic complexes preferably being used as emitter materials, and to specific nitrogen- or phosphorus-substituted triphenylene derivatives and to a process for their preparation.Organic light-emitting diodes (OLEDs) exploit the property of materials to emit light when they are excited by electrical current. OLEDs are of particular interest as an alternative to cathode ray tubes and liquid-crystal displays for the production of flat visual display units and as a particularly efficient light source. Owing to the very compact design and the intrinsically low power consumption, devices comprising OLEDs are suitable especially for mobile applications, for example for applications in cellphones, laptops, digital cameras, etc.The basic principles of the way in which OLEDs function and suitable constructions (layers) of OLEDs are known to those skilled in the art and are specified, for example, in WO 2005/113704 and the literature cited therein. The light-emitting materials (emitters) used may, as well as fluorescent materials (fluorescence emitters), be phosphorescent ...

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12-09-2013 дата публикации

COMPOUNDS AND METHODS FOR KINASE MODULATION, AND INDICATIONS THEREFOR

Номер: US20130237531A1
Принадлежит:

Compounds active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases. 2. The compound of claim 1 , wherein Ris hydrogen.3. The compound of claim 2 , wherein Ris halogen.4. The compound of claim 2 , wherein Ris optionally substituted phenyl.5. The compound of claim 2 , wherein Ris phenyl optionally substituted with one or more halogen substituents.6. The compound of claim 1 , wherein Ris phenyl optionally substituted with one or more fluoro substituents.7. The compound of claim 6 , wherein Ris phenyl substituted with two fluoro substituents.8. The compound of claim 1 , wherein each Ris independently optionally substituted lower alkyl or optionally substituted heteroaryl.9. The compound of claim 8 , wherein one Ris lower alkyl and the other Ris heteroaryl substituted with one or more NHgroups.10. The compound of claim 8 , wherein one Ris lower alkyl and the other Ris pyrimidinyl substituted with one or more NHgroups.11. The compound of claim 10 , wherein one Ris t-butyl and the other Ris pyrimidinyl substituted with NH.13. The compound of claim 12 , wherein Ar is thiazolyl.14. The compound of claim 12 , wherein Ar is 4-thiazolyl.16. A pharmaceutical composition comprising: a compound of and a pharmaceutically acceptable carrier or excipient.17. A pharmaceutical composition comprising: a compound of and a pharmaceutically acceptable carrier or excipient.18. A pharmaceutical composition comprising a compound of and another therapeutic agent.19. A method for treating a subject suffering from melanoma claim 15 , thyroid cancer or colorectal cancer claim 15 , said method comprising: administering to the subject an effective amount of a compound of .20. The method of claim 19 , wherein the melanoma is melanoma having a mutation encoding a V600E amino acid substitution. This application is a continuation application of U.S. application Ser. No. 12/669,450, filed Jan ...

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12-09-2013 дата публикации

AGONISTS OF GPR40

Номер: US20130237571A1
Принадлежит: Conexios Life Sciences PVT. LTD.

The present invention relates to compounds that have the ability to modulate the activity of GPR40 and are therefore useful in the treatment of GPR40 related disorders. In addition the invention relates to the compounds, methods for their preparation, pharmaceutical compositions containing the compounds and the uses of these compounds in the treatment of certain disorders related to GPR40 activity. 2. The compound according to claim 1 , wherein L is selected from the group consisting of —COH claim 1 , —SOH claim 1 , —PO3H claim 1 , —SONH claim 1 , —CONHSOCH claim 1 , and tetrazol-5-yl.3. The compound according to claim 1 , wherein L is —COH.442-. (canceled)43. The compound according to claim 1 , wherein Rand Rare each H.44. The compound according to claim 1 , wherein Z is CRR.45. The compound according to claim 44 , where 1 of Ror Rwhen taken together with one of Rand Rand the atoms to which they are attached forms a cyclic moiety.46. The compound according to claim 45 , wherein the cyclic moiety is a cyclopropyl group.47. The compound according to claim 43 , wherein Ris H.48. The compound according to claim 45 , wherein Ris selected from the group consisting of H claim 45 , cyano and isoxazol-3-yl.49. The compound according to claim 47 , wherein Ris selected from the group consisting of H claim 47 , cyano and isoxazol-3-yl.53. The compound according to claim 1 , wherein Y is selected from the group consisting of:(a) a bond(b) —O—(c) —S—(d) —S(═O)—{'sub': '2', '(e) —S(═O)—'}{'sup': '10', '(f) —N(R)—,'}{'sup': '10', 'sub': '2', '(g) —C(R)—,'}{'sup': '10', 'sub': '2', '(h)—C(R)O—'}{'sup': 10', '10, 'sub': '2', '(i) —C(R)N(R)—'}{'sup': '11', '(j) —C(═R)'}{'sub': '1-5', '(k) —OCalkyl-,'}{'sub': '1-5', '(l) —CalkylO—,'}{'sub': 1-5', '1-5, '(m) —CalkylOCalkyl,'}{'sup': '10', 'sub': '1-5', '(n) —N(R)Calkyl-,'}{'sub': '1-5', 'sup': '10', '(o) —CalkylN(R)—;'}{'sub': 1-5', '1-5, 'sup': '10', '(p) —CalkylN(R)Calkyl-,'}{'sup': '10', '(q) —N(R)CO—,'}{'sup': '10', 'sub': '1-5', ...

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19-09-2013 дата публикации

INDAZOLE, BENZISOXAZOLE, AND BENZISOTHIAZOLE KINASE INHIBITORS

Номер: US20130245015A1
Принадлежит:

Compounds having the formula 3. The compound of wherein X is O.4. The compound of wherein X is NR.5. The compound of wherein L is CHC(O)NR.6. The compound of wherein L is (CH)N(R)C(O)N(R)(CH).7. The compound of wherein X is O and L is (CH)N(R)C(O)N(R)(CH).8. The compound of selected from the group consisting ofN-[4-(3-amino-1,2-benzisoxazol-4-yl)phenyl]-N′-(3-methylphenyl)urea;N-[4-(3-amino-1,2-benzisoxazol-4-yl)phenyl]-N′-[2-(trifluoromethyl)phenyl]urea;N-[4-(3-amino-1,2-benzisoxazol-4-yl)phenyl]-N′-(2-fluoro-5-methylphenyl)urea;N-[4-(3-amino-1,2-benzisoxazol-4-yl)phenyl]-N′-[3-(trifluoromethyl)phenyl]urea;N-[4-(3-amino-1,2-benzisoxazol-4-yl)phenyl]-N′-[2-fluoro-5-(trifluoromethyl)phenyl]urea;N-[4-(3-amino-7-methoxy-1,2-benzisoxazol-4-yl)phenyl]-N′-[2-fluoro-5-(trifluoromethyl)phenyl]urea;N-[4-(3-amino-7-methoxy-1,2-benzisoxazol-4-yl)phenyl]-N′-(3-methylphenyl)urea;N-[4-(3-amino-7-methoxy-1,2-benzisoxazol-4-yl)phenyl]-N′-[3-(trifluoromethyl)phenyl]urea;N-[4-(3-amino-7-methoxy-1,2-benzisoxazol-4-yl)phenyl]-N′-(3-chlorophenyl)urea;N-[4-(3-amino-7-methoxy-1,2-benzisoxazol-4-yl)phenyl]-N′-(2-fluoro-5-methylphenyl)urea;N-{4-[3-amino-7-(4-morpholinylmethyl)-1,2-benzisoxazol-4-yl]phenyl}-N′-[2-fluoro-5-(trifluoromethyl)phenyl]urea;N-{4-[3-amino-7-(4-morpholinylmethyl)-1,2-benzisoxazol-4-yl]phenyl}-N′-[3-(trifluoromethyl)phenyl]urea;N-{4-[3-amino-7-(4-morpholinylmethyl)-1,2-benzisoxazol-4-yl]phenyl}-N′-(3-chlorophenyl)urea;N-{4-[3-amino-7-(4-morpholinylmethyl)-1,2-benzisoxazol-4-yl]phenyl}-N′-(3-methylphenyl)urea;N-{4-[3-amino-7-(4-morpholinylmethyl)-1,2-benzisoxazol-4-yl]phenyl}-N′-(2-fluoro-5-methylphenyl)urea;N-{4-[3-amino-7-(4-morpholinylmethyl)-1,2-benzisoxazol-4-yl]phenyl}-N′-(3,5-dimethylphenyl)urea;N-{4-[3-amino-7-(4-morpholinylmethyl)-1,2-benzisoxazol-4-yl]phenyl}-N′-(3-phenoxyphenyl)urea;N-{4-[3-amino-7-(4-morpholinylmethyl)-1,2-benzisoxazol-4-yl]phenyl}-N′-(3-bromophenyl)urea;N-(4-{3-amino-7-[2-(4-morpholinyl)ethoxy]-1,2-benzisoxazol-4-yl}phenyl)-N′-[3-( ...

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26-09-2013 дата публикации

NOVEL FLUORINATED SULFAMIDES EXHIBITING NEUROPROTECTIVE ACTION AND THEIR METHOD OF USE

Номер: US20130253022A1
Принадлежит:

Pharmaceutical compositions of the invention include fluorinated sulfamide derivatives having a disease-modifying action in the treatment of diseases associated with excitotoxicity and accompanying oxidative stress that include epilepsy, Alzheimer's disease, Parkinson's disease, Huntington's disease, heavy metal toxicity and any neurodegenerative disease involving glutamate toxicity. 2. The compound according to wherein R is phenyl claim 1 , 2-fluorophenyl claim 1 , 3-fluorophenyl claim 1 , 4-fluorophenyl claim 1 , 2 claim 1 ,4-difluorophenyl claim 1 , 2 claim 1 ,5-difluorophenyl claim 1 , 2 claim 1 ,6-difluorophenyl claim 1 , 2-chlorophenyl claim 1 , 2-bromophenyl claim 1 , 2-trifluoromethylphenyl claim 1 , 3-trifluoromethylphenyl claim 1 , 2 claim 1 ,6-dichlorophenyl claim 1 , 2 claim 1 ,4-dichlorophenyl claim 1 , 2-methylphenyl claim 1 , 2-ethylphenyl claim 1 , 2-methoxyphenyl claim 1 , 2-chloro-6-fluorophenyl claim 1 , 2-chloro-4-fluorophenyl claim 1 , 2-fluoro-6-methoxyphenyl claim 1 , 4-fluoro-2-methoxyphenyl claim 1 , 2-chloro-6-methoxyphenyl claim 1 , benzo[b]thiophen-3-yl claim 1 , or benzo[d]isoxazol-3-yl.3. The compound according to wherein Ris methyl or hydrogen.4. The compound according to wherein Ris fluorine.5. The compound according to that is:2,2-Difluoro-2-phenyl-ethyl-1-sulfamide;2,2-Difluoro-2-(2-fluorophenyl)ethyl-1-sulfamide;2,2-Difluoro-2-(3-fluorophenyl)ethyl-1-sulfamide;2,2-Difluoro-2-(4-fluorophenyl)ethyl-1-sulfamide;2,2-Difluoro-2-(2,6-difluorophenyl)ethyl-1-sulfamide;2,2-Difluoro-2-(2,4-difluorophenyl)ethyl-1-sulfamide;2,2-Difluoro-2-(2,5-difluorophenyl)ethyl-1-sulfamide;2,2-Difluoro-2-(2-chlorophenyl)ethyl-1-sulfamide;2,2-Difluoro-2-(2-trifluoromethylphenyl)ethyl-1-sulfamide;2,2-Difluoro-2-(3-trifluoromethylphenyl)ethyl-1-sulfamide;2,2-Difluoro-2-(2,6-dichlorophenyl)ethyl-1-sulfamide;2,2-Difluoro-2-(2,4-dichlorophenyl)ethyl-1-sulfamide;2,2-Difluoro-2-(2-methylphenyl)ethyl-1-sulfamide;2,2-Difluoro-2-(2-methoxyphenyl)ethyl-1-sulfamide;2,2- ...

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26-09-2013 дата публикации

POLYCYCLIC LPA1 ANTAGONIST AND USES THEREOF

Номер: US20130253023A1
Принадлежит:

Described herein is the LPA1 antagonist 1-{4′-[3-methyl-4-((R)-1-phenyl-ethoxycarbonylamino)-isoxazol-5-yl]-bi-phenyl-4-yl}-cyclopropanecarboxylic acid (Compound 1), or pharmaceutically acceptable salts thereof. Also described are methods of preparing the LPA1 antagonist, or pharmaceutically acceptable salts thereof, as well as pharmaceutical compositions suitable for administration to a mammal that include the LPA1 antagonist, or pharmaceutically acceptable salt thereof, and methods of using such pharmaceutical compositions for treating LPA-dependent or LPA-mediated diseases or conditions. 1. A crystalline form of 1-{4′-[3-methyl-4-((R)-1-phenyl-ethoxycarbonylamino)-isoxazol-5-yl]-biphenyl-4-yl}-cyclopropanecarboxylic acid , 1-{4′-[3-methyl-4-((S)-1-phenyl-ethoxycarbonylamino)-isoxazol-5-yl]-biphenyl-4-yl}-cyclopropanecarboxylic acid , or 1-{4′-[3-methyl-4-(1-phenyl-ethoxycarbonylamino)-isoxazol-5-yl]-biphenyl-4-yl}-cyclopropanecarboxylic acid , or a pharmaceutically acceptable salt , or solvate thereof.2. The crystalline form of claim 1 , wherein the pharmaceutically acceptable salt is a sodium salt claim 1 , calcium salt claim 1 , potassium salt claim 1 , ammonium salt claim 1 , L-arginine salt claim 1 , L-lysine salt claim 1 , or N-methyl-D-glucamine salt claim 1 , or solvate thereof.3. The crystalline form of claim 1 , wherein the pharmaceutically acceptable salt is a sodium salt claim 1 , or solvate thereof.4. The crystalline form of that is 1-{4′-[3-methyl-4-((R)-1-phenyl-ethoxycarbonylamino)-isoxazol-5-yl]-biphenyl-4-yl}-cyclopropanecarboxylic acid claim 1 , or a pharmaceutically acceptable salt claim 1 , or solvate thereof.5. The crystalline form of that is a pharmaceutically acceptable salt of 1-{4′-[3-methyl-4-((R)-1-phenyl-ethoxycarbonylamino)-isoxazol-5-yl]-biphenyl-4-yl}-cyclopropanecarboxylic acid claim 1 , or solvate thereof.6. The crystalline form of claim 1 , wherein the crystalline form is a hydrate.7. The crystalline form of that is 1-{4′-[3- ...

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03-10-2013 дата публикации

CRYSTALLINE FORMS OF (R)-3-[N-(3'-CHLOROBIPHENYL-4-YLMETHYL)-N'-(3-HYDROXYISOXAZOLE-5-CARBONYL)HYDRAZINO]-2-HYDROXYPROPIONIC ACID ISOPROPYL ESTER

Номер: US20130259897A1
Принадлежит:

The invention provides crystalline forms of (R)-3-[N-(3′-chlorobiphenyl-4-ylmethyl)-N′—(3-hydroxyisoxazole-5-carbonyl)hydrazino]-2-hydroxypropionic acid isopropyl ester. This invention also provides pharmaceutical compositions comprising the crystalline compound, processes and intermediates for preparing the crystalline compound, and methods of using the crystalline compound to treat diseases. 1. A crystalline (R)-3-[N-(3′-chlorobiphenyl-4-ylmethyl)-N′—(3-hydroxyisoxazole-5-carbonyl)hydrazino]-2-hydroxypropionic acid isopropyl ester , selected from:a neutral monohydrate Form 1 characterized by a powder x-ray diffraction pattern comprising diffraction peaks at 2θ values of 8.26±0.20, 14.68±0.20, 15.64±0.20, 16.36±0.20, 18.52±0.20, 20.40±0.20, 21.08±0.20, 21.48±0.20, 21.68±0.20, 23.18±0.20, 24.50±0.20, 24.80±0.20, 25.34±0.20, and 26.56±0.20;a neutral Form 2 characterized by a powder x-ray diffraction pattern comprising diffraction peaks at 2θ values of 7.48±0.20, 8.02±0.20, 9.38±0.20, 12.24±0.20, 14.86±0.20, 18.72±0.20, 20.94±0.20, 21.34±0.20, 22.32±0.20, and 24.68±0.20;a neutral solvated Form 2′ characterized by a powder x-ray diffraction pattern comprising diffraction peaks at 2θ values of 7.26±0.20, 8.05±0.20, 12.20±0.20, 14.48±0.20, 15.84±0.20, 16.22±0.20, 18.78±0.20, 20.60±0.20, 21.29±0.20, 21.74±0.20, 23.10±0.20, 24.16±0.20, and 24.44±0.20;a neutral anhydrous Form 3 characterized by a powder x-ray diffraction pattern comprising diffraction peaks at 2θ values of 8.12±0.20, 8.86±0.20, 11.92±0.20, 13.68±0.20, 16.10±0.20, 18.12±0.20, 18.46±0.20, 19.06±0.20, 19.48±0.20, 20.60±0.20, 21.28±0.20, 24.46±0.20, 25.94±0.20, and 26.40±0.20;a neutral anhydrous Form 4 characterized by a powder x-ray diffraction pattern comprising diffraction peaks at 2θ values of 8.70±0.20, 13.00±0.20, 16.00±0.20, 16.94±0.20, 17.36±0.20, 18.72±0.20, 19.00±0.20, 19.78±0.20, 20.24±0.20, 21.70±0.20, 23.68±0.20, and 27.94±0.20;a tromethamine salt characterized by a powder x-ray diffraction pattern ...

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03-10-2013 дата публикации

Sulfonyl semicarbazides, semicarbazides and ureas, pharmaceutical compositions thereof, and methods for treating hemorrhagic fever viruses, including infections associated with arena viruses

Номер: US20130261087A1
Принадлежит: Siga Technologies Inc

Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain novel sulfonyl semicarbazides, carbonyl semicarbazides, semicarbazides, ureas and related compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by hemorrhagic fever viruses is disclosed, i.e., including but not limited to, Arenaviridae (Junin, Machupo, Guanarito, Sabia, Lassa, Tacaribe, Pinchinde, and VSV), Filoviridae (ebola and Marburg viruses), Flaviviridae (yellow fever, omsk hemorrhagic fever and Kyasanur Forest disease viruses), and Bunyaviridae (Rift Valley fever).

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03-10-2013 дата публикации

SUBSTITUTED N-(2-ARYLAMINO)ARYL SULFONAMIDE-CONTAINING COMBINATIONS

Номер: US20130261120A1
Принадлежит: Bayer Intellectual Property GmbH

The present invention relates to: 3. The combination according to claim 1 , wherein:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'said component B is one or more N-(2-arylamino) aryl sulfonamide compounds of general formula (II) according to , which is selected from the list consisting ofExample 1: N-(3,4-difluoro-2-(2-fluoro-4-iodophenylamino)phenyl)-methanesulfonamide:Example 2: N-(3,4-difluoro-2-(2-fluoro-4-iodophenylamino)phenyl)cyclopropanesulfonamide:Example 3: N-(3,4-difluoro-2-(2-fluoro-4-iodophenylamino)phenyl)propane-2-sulfonamide:Example 4: N-(3,4-difluoro-2-(2-fluoro-4-iodophenylamino)phenyl)butane-1-sulfonamide:Example 5: N-(3,4-difluoro-2-(2-fluoro-4-iodophenylamino)phenyl)-2,2,2-trifluoro ethane sulfonamide:Example 6: N-(3,4-difluoro-2-(2-fluoro-4-iodophenylamino)phenyl)butane-2-sulfonamide:Example 7: N-(3,4-difluoro-2-(2-fluoro-4-iodophenylamino)phenyl)-N-methyl cyclopropane sulfonamide:Example 8: 1-Chloro-N-(3,4-difluoro-2-(2-fluoro-4-iodophenylamino)phenyl)methane sulfonamide:Example 9: N-(3,4-difluoro-2-(2-fluoro-4-iodophenylamino)phenyl)-2-methylpropane-2-sulfonamide:Example 10: N-(3,4-difluoro-2-(2-fluoro-4-iodophenylamino)phenyl)cyclopentanesulfonamide:Example 11: N-(3,4-difluoro-2-(2-fluoro-4-iodophenylamino)phenyl)cyclohexanesulfonamide:Example 12: N-(3,4-difluoro-2-(2-fluoro-4-iodophenylamino)phenyl)-1-methylcyclopropane-1-sulfonamide:Example 13: N-(3,4-difluoro-2-(2-fluoro-4-iodophenylamino)phenyl)-1-(2,3-dihydroxypropyl)cyclopropane-1-sulfonamide:Example 14: (S)—N-(3,4-difluoro-2-(2-fluoro-4-iodophenylamino)phenyl)-1-(2,3-dihydroxypropyl)cyclopropane-1-sulfonamide:Example 15: (R)—N-(3,4-difluoro-2-(2-fluoro-4-iodophenylamino)phenyl)-1-(2,3-dihydroxypropyl)cyclopropane-1-sulfonamide:Example 16: N-(3,4-difluoro-2-(2-fluoro-4-iodophenylamino)phenyl)-1-(2-hydroxyethyl)cyclopropane-1-sulfonamide:Example 17: N-(3,4-difluoro-2-(2-fluoro-4-iodophenylamino)phenyl)-3-hydroxypropane-1-sulfonamide:Example 18: N-(3,4-difluoro-2-(2-fluoro-4- ...

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03-10-2013 дата публикации

Therapeutic Compounds for Protozoal and Microbial Infections and Cancer

Номер: US20130261133A1
Принадлежит: The University of Montana

The compounds of the invention exhibit antiprotozoal, antimicrobial, and anticancer properties that are useful for the treatment or prevention of infections or cancer in a patient (e.g., a human). For example, the compounds and methods described herein can be used for the treatment or prevention of protozoal infections such as leishmaniasis, malaria, and infections, bacterial infections such as and , and cancers such as breast, colon, lung, or prostate cancer. The invention further provides methods of synthesizing such compounds as well as kits useful for administering the compounds. 2. The compound of claim 1 , wherein said compound is selected from the group consisting of (3S claim 1 ,8R)-8-hydroxyheptadeca-1-en-4 claim 1 ,6-diyn-3-yl acetate; (3R claim 1 ,8R)-8-hydroxyheptadeca-1-en-4 claim 1 ,6-diyn-3-yl acetate; (3R claim 1 ,8S)-8-hydroxyheptadeca-1-en-4 claim 1 ,6-diyn-3-yl acetate; (3S claim 1 ,8R)-8-hydroxyhexadeca-1-en-4 claim 1 ,6-diyn-3-yl acetate; (3S claim 1 ,8S)-8-hydroxyhexadeca-1-en-4 claim 1 ,6-diyn-3-yl acetate; (3R claim 1 ,8R)-8-hydroxyhexadeca-1-en-4 claim 1 ,6-diyn-3-yl acetate; (3R claim 1 ,8S)-8-hydroxyhexadeca-1-en-4 claim 1 ,6-diyn-3-yl acetate; (3S claim 1 ,8R)-8-hydroxypentadeca-1-en-4 claim 1 ,6-diyn-3-yl acetate; (3S claim 1 ,8S)-8-hydroxypentadeca-1-en-4 claim 1 ,6-diyn-3-yl acetate; (3R claim 1 ,8R)-8-hydroxypentadeca-1-en-4 claim 1 ,6-diyn-3-yl acetate; (3R claim 1 ,8S)-8-hydroxypentadeca-1-en-4 claim 1 ,6-diyn-3-yl acetate; (3S claim 1 ,8R)-8-hydroxytetradeca-1-en-4 claim 1 ,6-diyn-3-yl acetate; (3S claim 1 ,8S)-8-hydroxytetradeca-1-en-4 claim 1 ,6-diyn-3-yl acetate; (3R claim 1 ,8R)-8-hydroxytetradeca-1-en-4 claim 1 ,6-diyn-3-yl acetate; (3R claim 1 ,8S)-8-hydroxytetradeca-1-en-4 claim 1 ,6-diyn-3-yl acetate; (3S claim 1 ,8R)-8-hydroxytrideca-1-en-4 claim 1 ,6-diyn-3-yl acetate; (3S claim 1 ,8S)-8-hydroxytrideca-1-en-4 claim 1 ,6-diyn-3-yl acetate; (3R claim 1 ,8R)-8-hydroxytrideca-1-en-4 claim 1 ,6-diyn-3-yl acetate; (3R claim 1 , ...

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03-10-2013 дата публикации

FUNGICIDAL N-(2-PHENOXYETHYL)CARBOXAMIDE DERIVATIVES AND THEIR AZA, THIA AND SILA ANALOGUES

Номер: US20130261158A1
Принадлежит:

The present invention relates to fungicide N-(2-phenoxyethyl)carboxamide derivatives of formula (I), their aza, thia and sila analogues, their process of preparation, their use as fungicides, particularly in the form of fungicidal compositions and methods for the control of phytopathogenic fungi of plants using these compounds or their compositions. Formula (1) wherein A, T, W, X, n and Zto Zrepresent various substituents. 3. A compound according to wherein A is selected in the list consisting of A; A; Aand A.4. A compound according to wherein A represents Aand wherein Rrepresents a C-C-alkyl claim 3 , C-C-halogenoalkyl comprising up to 9 halogen atoms that can be the same or different; or C-C-alkoxy; Rrepresents a hydrogen atom or a halogen atom; Rrepresents a C-C-alkyl.5. A compound according to wherein W represents O or S.6. A compound according to wherein n represents 0 claim 1 , 1 or 2.7. A compound according to wherein X independently represents a halogen atom; C-C-alkyl; C-C-halogenoalkyl comprising up to 9 halogen atoms that can be the same or different; tri(C-C-alkyl)silyl; C-Calkoxy or C-C-halogenoalkoxy comprising up to 9 halogen atoms that can be the same or different or wherein two consecutive substituents X together with the phenyl ring form a substituted or non substituted 1 claim 1 ,3-benzodioxolyl; 1 claim 1 ,2 claim 1 ,3 claim 1 ,4-tetrahydro-quinoxalinyl; 3 claim 1 ,4-dihydro-2H-1 claim 1 ,4-benzoxazinyl; 1 claim 1 ,4-benzodioxanyl; indanyl; 2 claim 1 ,3-dihydrobenzofuranyl; or indolinyl.8. A compound according to wherein Zand Zindependently represent a C-C-alkyl.9. A compound according to wherein Zand Zindependently represent a hydrogen atom or a C-C-alkyl.10. A compound according to wherein Zand Zindependently represent a hydrogen atom or a C-C-alkyl.11. A compound according to wherein Zrepresents a C-Ccycloalkyl substituted by up to 10 groups or atoms that can be the same or different and that can be selected in the list consisting of halogen ...

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10-10-2013 дата публикации

Modulators of Aldehyde Dehydrogenase and Methods of Use Thereof

Номер: US20130267501A1

The present disclosure provides compounds that function as modulators of aldehyde dehydrogenase (ALDH) enzymatic activity, as well as compositions and formulations comprising the compounds. The present disclosure provides therapeutic methods involving administering a subject compound, or a subject pharmaceutical composition. 176.-. (canceled)78. The compound of claim 77 , wherein Xand Xare both O.79. The compound of claim 77 , wherein z is 1.80. The compound of claim 77 , wherein Ar is a substituted phenyl.81. The compound of claim 80 , wherein the phenyl is substituted with a methyl group.82. The compound of claim 81 , wherein the phenyl is further substituted with an isoxazoly group.83. The compound of claim 82 , wherein the isoxazolyl group is substituted with one or more methyl groups.84. The compound of claim 77 , wherein Ar is a substituted thiophenyl group85. The compound of claim 84 , wherein the thiophenyl group is substituted with C(O)NH.87. A pharmaceutical composition comprising:{'claim-ref': {'@idref': 'CLM-00077', 'claim 77'}, 'a) a compound of ; and'}b) a pharmaceutically acceptable excipient.88. A pharmaceutical composition comprising:{'claim-ref': {'@idref': 'CLM-00086', 'claim 86'}, 'a) a compound of ; and'}b) a pharmaceutically acceptable excipient.89. A method of reducing a level of aldehyde present at a toxic level in an individual to below the toxic level comprising administering to an individual an effective amount of a compound of .90. The method of claim 89 , wherein the individual has alcohol intolerance claim 89 , alcohol addiction claim 89 , or an alcohol abuse disorder.91. A method of treating a disease or disorder selected from alcohol intolerance claim 77 , alcohol addiction claim 77 , alcohol abuse disorder claim 77 , methanol poisoning claim 77 , ethylene glycol monomethyl ether poisoning claim 77 , and poisoning due to other xenogenic or biogenic aldehyde compounds claim 77 , comprising administering to an individual an effective ...

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17-10-2013 дата публикации

(2-UREIDOACETAMIDO)ALKYL DERIVATIVES AS FORMYL PEPTIDE RECEPTOR 2 MODULATORS

Номер: US20130274230A1
Принадлежит: ALLERGAN, INC.

The present invention relates to (2-ureidoacetamido)alkyl derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor 2. 2. A compound according to claim 1 , wherein:{'sup': 3', '11', '16, 'sub': 1-8', '3', '2, 'Ris substituted or unsubstituted Calkyl, halogen, —SR, —CFor —S(O)R.'}4. A compound according to claim 1 , wherein:{'sup': 6', '19, 'sub': 1-8', '2, 'Ris substituted or unsubstituted Calkyl, or —CHR.'}5. A compound according to claim 1 , wherein:{'sup': '26', 'Ris hydrogen;'}{'sup': '27', 'Ris hydrogen;'}{'sup': '28', 'Ris hydrogen; and'}{'sup': '29', 'Ris hydrogen;'}8. A compound according to claim 1 , selected from:Diethyl({[(2S)-2-({[(4-bromophenyl)amino]carbonyl}amino)-4-methylpentanoyl]amino}methyl)phosphonate;(2S)-2-({[(4-Bromophenyl)amino]carbonyl}amino)-4-methyl-N-(1H-tetrazol-5-ylmethyl)pentanamide;(2S)-2-({[(4-Bromophenyl)amino]carbonyl}amino)-4-methyl-N-[2-(1H-tetrazol-5-yl)ethyl]pentanamide;(2S)-2-({[(4-Bromophenyl)amino]carbonyl}amino)-N-[(3-hydroxyisoxazol-5-yl)methyl]-4-methylpentanamide;Diethyl({[(2S)-2-({[(4-bromophenyl)amino]carbonyl}amino)-4-methylpentanoyl]amino}methyl)phosphonate;Diethyl({[(2S,3S)-2-({[(4-bromophenyl)amino]carbonyl}amino)-3-methylpentanoyl]amino}methyl)phosphonate;Diethyl({[(2S)-2-({[(4-bromophenyl)amino]carbonyl}amino)pentanoyl]amino}methyl)phosphonate;Diethyl({[(2S)-2-({[(4-bromophenyl)amino]carbonyl}amino)-3-phenylpropanoyl]amino}methyl)phosphonate;Diethyl(2-{[(2S)-2-({[(4-bromophenyl)amino]carbonyl}amino)-4-methylpentanoyl]amino}ethyl)phosphonate;Ethyl hydrogen ({[(2S)-2-({[(4-bromophenyl)amino]carbonyl}amino)-4-methyl pentanoyl]amino}methyl)phosphonate;Ethyl hydrogen ({[(2S,3S)-2-({[(4-bromophenyl)amino]carbonyl}amino)-3-methyl pentanoyl]amino}methyl)phosphonate;Ethyl hydrogen ({[(2S)-2-({[(4-bromophenyl)amino]carbonyl}amino)pentanoyl]amino}methyl)phosphonate;({[(2S)-4-Methyl-2-({[4-(trifluoromethyl)phenyl] ...

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17-10-2013 дата публикации

NOVEL INHIBITORS OF BACTERIAL BIOFILMS AND RELATED METHODS

Номер: US20130274256A1
Принадлежит: SEQUOIA SCIENCES, INC.

Certain multi-cyclic compounds and compositions thereof are useful for reducing or inhibiting the growth of bacterial biofilms and for controlling bacterial biofilm infections. Such compounds and compositions are also useful in methods for reducing or inhibiting the growth of biofilms and for controlling bacterial biofilm infections involving biofilms. 162-. (canceled)65. A compound according to wherein Ris selected from the group consisting of methyl claim 63 , halide claim 63 , lower haloalkyl claim 63 , nitrile claim 63 , lower alkyl nitrile claim 63 , lower alkyl claim 63 , substituted lower alkyl claim 63 , lower alkenyl claim 63 , substituted lower alkenyl claim 63 , lower alkynyl claim 63 , substituted lower alkynyl claim 63 , lower cycloalkyl claim 63 , lower cycloalkenyl claim 63 , aryl claim 63 , substituted aryl claim 63 , heteroaryl claim 63 , and substituted heteroaryl claim 63 , preferably Ris selected from the group consisting of pyrrolyl claim 63 , pyrazolyl claim 63 , imidazolyl claim 63 , oxazolyl claim 63 , isoxazolyl claim 63 , oxadiazolyl claim 63 , thiazolyl claim 63 , isothiazolyl claim 63 , thienyl claim 63 , furanyl claim 63 , furazanyl claim 63 , pyridinyl claim 63 , pyrimidinyl claim 63 , pyridazinyl claim 63 , indolyl claim 63 , 3H-indolyl claim 63 , isoindolyl claim 63 , indolinyl claim 63 , indolizinyl claim 63 , indazolyl claim 63 , dihydroindolyl claim 63 , tetrahydroindolyl claim 63 , purinyl claim 63 , pyrazinyl claim 63 , quinolinyl claim 63 , isoquinolinyl claim 63 , tetrahydroisoquinolinyl claim 63 , quinoxalinyl claim 63 , quinazolinyl claim 63 , cinnolinyl claim 63 , pteridinyl claim 63 , benzimidazolyl claim 63 , benzopyranyl claim 63 , benzoxazolyl claim 63 , benzisoxazolyl claim 63 , benzofuranyl claim 63 , isobenzofuranyl claim 63 , benzothiazolyl claim 63 , benzisothiazolyl claim 63 , benzothienyl claim 63 , furopyridinyl claim 63 , phthalazinyl claim 63 , napthyridinyl claim 63 , pyrazolopyridyl claim 63 , ...

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31-10-2013 дата публикации

Isoxazole Compounds As Inhibitors Of Heat Shock Proteins

Номер: US20130289026A1
Принадлежит:

Isoxazoles of formula (A) or (B) are inhibitors of HSP90 activity, and useful for treatment of, for example cancers: 327-. (canceled)30. (canceled)31. The method as claimed in wherein the compound is selected from:5-(2,4-Dihydroxy-5-isopropyl-phenyl)-4-(4-morpholin-4-ylmethyl-phenyl)-isoxazole-3-carboxylic acid ethylamide5-(2,4-Dihydroxy-5-isopropyl-phenyl)-4-(4-piperidin-1-ylmethyl-phenyl)-isoxazole-3-carboxylic acid ethylamide4-(4-Diethylaminomethyl-phenyl)-5-(2,4-dihydroxy-5-isopropyl-phenyl)-isoxazole-3-carboxylic acid ethylamide5-(2,4-Dihydroxy-5-isopropyl-phenyl)-4-[4-(4-methyl-piperazin-1-ylmethyl)-phenyl]-isoxazole-3-carboxylic acid ethylamide5-(2,4-Dihydroxy-5-isopropyl-phenyl)-4-(4-ethylaminomethyl-phenyl)-isoxazole-3-carboxylic acid ethylamide5-(2,4-Dihydroxy-5-isopropyl-phenyl)-4-[4-(isopropylamino-methyl)-phenyl]-isoxazole-3-carboxylic acid ethylamide4-(4-Cyclohexylaminomethyl-phenyl)-5-(2,4-dihydroxy-5-isopropyl-phenyl)-isoxazole-3-carboxylic acid ethylamide4-[4-(tert-Butylamino-methyl)-phenyl]-5-(2,4-dihydroxy-5-isopropyl-phenyl)-isoxazole-3-carboxylic acid ethylamide5-(2,4-Dihydroxy-5-isopropyl-phenyl)-4-{4-[(2-methoxy-ethylamino)-methyl]-phenyl}-isoxazole-3-carboxylic acid ethylamide5-(2,4-Dihydroxy-5-isopropyl-phenyl)-4-(4-morpholin-4-ylmethyl-phenyl)-isoxazole-3-carboxylic acid isopropylamide5-(2,4-Dihydroxy-5-isopropyl-phenyl)-4-[4-(4-methyl-piperazin-1-ylmethyl)-phenyl]-isoxazole-3-carboxylic acid isopropylamide5-(5-tert-Butyl-2,4-dihydroxy-phenyl)-4-[4-(4-methyl-piperazin-1-ylmethyl)-phenyl]-isoxazole-3-carboxylic acid ethylamide5-(5-tert-Butyl-2,4-dihydroxy-phenyl)-4-(4-piperidin-1-ylmethyl-phenyl)-isoxazole-3-carboxylic acid ethylamide5-(2,4-Dihydroxy-5-isobutyl-phenyl)-4-(4-morpholin-4-ylmethyl-phenyl)-isoxazole-3-carboxylic acid ethylamide5-(2,4-Dihydroxy-5-isobutyl-phenyl)-4-(4-piperidin-1-ylmethyl-phenyl)-isoxazole-3-carboxylic acid ethylamide5-(5-tert-Butyl-2,4-dihydroxy-phenyl)-4-(4-morpholin-4-ylmethyl-phenyl)-isoxazole-3-carboxylic ...

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07-11-2013 дата публикации

THIAZOLE AND OXAZOLE-SUBSTITUTED ARYLAMIDES AS P2X3 AND P2X2/3 ANTAGONISTS

Номер: US20130296310A1
Принадлежит:

Compounds of the formula I: 153-. (canceled)55. The compound of claim 54 , wherein Ris phenyl substituted at the 4-position with methyl or halo and optionally substituted at the 2-position with halo.56. The compound of claim 54 , wherein Ris pyridin 2-yl substituted with methyl or halo at the 5-position.57. The compound of claim 54 , wherein claim 54 , Ris 4-methyl-phenyl claim 54 , 2-fluoro-4-methyl-phenyl claim 54 , 2-chloro-4-fluoro-phenyl claim 54 , 4-chloro-2-fluoro-phenyl claim 54 , 2 claim 54 ,4-dichloro-phenyl claim 54 , 2 claim 54 ,4-difluoro-phenyl claim 54 , or 2-chloro-4-methyl-phenyl.58. The compound of claim 57 , wherein Ris hydrogen.59. The compound of claim 58 , wherein Ris hydrogen.60. The compound of claim 58 , wherein Ris hydrogen.61. The compound of claim 58 , wherein Ris methyl.62. The compound of claim 54 , wherein Ris a group of formula A.63. The compound of claim 54 , wherein X is S.64. The compound of claim 54 , wherein one of Rand Ris hydrogen and the other is: hydrogen; Calkyl; Calkoxy; Calkylsulfonyl-Calkyl; halo-Calkyl; halo-Calkoxy; hetero-Calkyl; C-cycloalkyl; Ccycloalkyl-Calkyl; aminocarbonyl; Calkoxycarbonyl; or cyano.65. The compound of claim 54 , wherein one of Rand Ris hydrogen and the other is Calkyl.66. The compound of claim 54 , wherein Ris: Calkyloxy-Calkyl; hydroxy-Calkyl; heteroaryl claim 54 , or heterocyclyl-Calkyl.67. The compound of claim 54 , wherein Ris hydroxymethyl claim 54 , methoxymethyl claim 54 , pyrazin-2-yl or 5-methyl-pyrazin-2-yl.70. A pharmaceutical composition comprising:(a) a pharmaceutically acceptable carrier; and{'claim-ref': {'@idref': 'CLM-00054', 'claim 54'}, '(b) a compound of .'}71. A method for treating a pain condition selected from inflammatory pain claim 54 , surgical pain claim 54 , visceral pain claim 54 , dental pain claim 54 , premenstrual pain claim 54 , central pain claim 54 , pain due to burns claim 54 , migraine or cluster headaches claim 54 , nerve injury claim 54 , neuritis claim 54 , ...

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07-11-2013 дата публикации

GLUCAGON RECEPTOR MODULATORS

Номер: US20130296355A1
Принадлежит:

The present invention provides a compound of Formula (I) 2. The compound of or a pharmaceutically acceptable salt thereof claim 1 , wherein L is —X—CH(R)—; Ris a 5 membered heteroaryl attached through a nitrogen atom to the carbon between Aand Aof the ring containing A claim 1 , A claim 1 , Aand A; Ris hydrogen; and Ris —(CH)COH.3. The compound of or a pharmaceutically acceptable salt thereof claim 2 , wherein X is O.4. The compound of or a pharmaceutically acceptable salt thereof claim 2 , wherein X is NH.5. The compound of or a pharmaceutically acceptable salt thereof wherein Aand Aare each N and Aand Aare each CR; Rat each occurrence is independently H or methyl; B claim 3 , B claim 3 , Band Bare each CR; and Rat each occurrence is H.6. The compound of or a pharmaceutically acceptable salt thereof wherein Ais N and A claim 4 , Aand Aare each CR; Rat each occurrence is independently H or methyl; B claim 4 , B claim 4 , Band Bare each CR; and Rat each occurrence is independently H or methyl.7. The compound of or a pharmaceutically acceptable salt thereof wherein Ris ethyl claim 5 , propyl claim 5 , isopropyl claim 5 , isobutyl claim 5 , neopentyl claim 5 , cyclopropyl claim 5 , cyclobutyl claim 5 , dimethylcyclobutyl claim 5 , cyclopentyl or cyclopropylmethyl.8. The compound of or a pharmaceutically acceptable salt thereof wherein Ris ethyl claim 6 , propyl claim 6 , isopropyl claim 6 , isobutyl claim 6 , neopentyl claim 6 , cyclopropyl claim 6 , cyclobutyl claim 6 , dimethylcyclobutyl claim 6 , cyclopentyl or cyclopropylmethyl.9. The compound of or a pharmaceutically acceptable salt thereof wherein Ris imidazolyl claim 7 , pyrazolyl claim 7 , triazolyl or indazolyl optionally substituted with one to two substituents each independently selected from methyl claim 7 , trifluoromethyl claim 7 , ethyl claim 7 , propyl claim 7 , isopropyl claim 7 , butyl claim 7 , t-butyl claim 7 , methoxy claim 7 , ethoxy claim 7 , cyano claim 7 , chloro or fluoro.10. The compound of ...

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07-11-2013 дата публикации

ISOXAZOLINE-SUBSTITUTED BENZAMIDE COMPOUND AND PESTICIDE

Номер: US20130296559A1
Принадлежит:

A substituted alkenylbenzene compound of formula (4): 2. The substituted alkenylbenzene compound of formula (4) according to claim 1 , wherein:{'sup': '1', 'sub': 5', '1', '6', '1', '6', '1', '6, 'Xis selected from the group consisting of a halogen atom, —SF, C-Chaloalkyl, C-Chaloalkoxy and C-Chaloalkylthio;'}{'sup': '3', 'sub': 1', '6', '1', '6', '1', '6, 'Xis selected from the group consisting of a hydrogen atom, halogen atom, cyano, nitro, C-Calkyl, C-Chaloalkyl and C-Calkoxy;'}{'sup': '4', 'Xis a hydrogen atom or halogen atom;'}{'sup': 3a', '3b, 'Rand Rare each a fluorine atom;'}{'sup': 3c', '2', '3', '4', '1', '3', '4', '1', '3', '4', '3c, 'Ris selected from the group consisting of a hydrogen atom, fluorine atom, chlorine atom, bromine atom and trifluoromethyl, with a proviso that in case where Xis a fluorine atom, chlorine atom or trifluoromethyl and both Xand Xare a hydrogen atom, in case where both Xand Xare a fluorine atom and Xis a hydrogen atom, and in case where both Xand Xare trifluoromethyl and Xis a hydrogen atom, Ris a hydrogen atom, chlorine atom, bromine atom or trifluoromethyl.'} This is a Divisional Application of application Ser. No. 13/166,294, filed Jun. 22, 2011, which is a Divisional Application of application Ser. No. 12/509,859, filed on Jul. 27, 2009, which is a Divisional Application of application Ser. No. 11/514,921, filed Sep. 5, 2006, which in turn is a Continuation-in-part of International Application No. PCT/JP05/04268, filed Mar. 4, 2005, which claims priority to Japanese Patent Applications Nos. 2004-200119, filed Jul. 7, 2004, and 2004-061749, filed Mar. 5, 2004. The disclosures of the prior applications are hereby incorporated by reference herein in their entirety.The present invention relates to a novel isoxazoline-substituted benzamide compound and the salt thereof, and a pesticide characterized by containing the compound as an active ingredient. The pesticide in the present invention means a pest controlling agent applied ...

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21-11-2013 дата публикации

Alpha, beta-unsaturated imines

Номер: US20130310254A1
Принадлежит: Bayer Intellectual Property GmbH

The present application relates to novel alpha, beta-unsaturated imines, to processes for their preparation, to their use for controlling animal pests including arthropods and in particular insects and to their use in the control of vectors. 2. The compound according to claim 1 , where Arepresents —C(R claim 1 ,R)—.3. The compound according to claim 1 , where Arepresents a —C(R claim 1 ,R)— group and where{'sup': 2', '3, 'said C(R,R)— group forms a double bond with the adjacent B position, or'}{'sup': 2', '3', '1', '2', '1', '2, 'sub': 'n', 'said C(R,R)— group is a bridging group which, together with a further bridging group and any B groups, located between these bridging groups, of the C(═C(W,X-Q)-C(═N-Q)-A-[B]-Aring and a corresponding bridge U forms an unsubstituted or substituted cyclic system, or'}{'sup': 2', '3, 'this said C(R,R)— group carries a substituent V.'}4. The compound according to claim 1 , where Ais part of a cyclic system.5. The compound according to claim 1 , where Ais part of a carbocyclic system comprising 6 ring atoms or part of a 5- or 6-membered heterocyclic system.6. The compound according to claim 5 , where Ais part of an aromatic system comprising 6 ring atoms or part of a 5- or 6-membered heteroaromatic system.7. The compound according to claim 1 , where n is 2.11. An insecticidal composition claim 1 , wherein said insecticidal composition comprises at least one compound according to claim 1 , and an extender and/or surfactant.12. A method for protecting transgenic and/or conventional seed and a plant generated therefrom against attack by pests claim 1 , comprising treating the seed with at least one compound according to .13. A compound according claim 1 , capable of being used for controlling pests.14. A compound according to claim 1 , capable of being used for controlling vectors.15. A seed in which a compound according to claim 1 , has been applied to said seed as a constituent of a casing and/or as a further layer and/or further ...

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21-11-2013 дата публикации

Methods including latent 1,3-dipole-functional compounds and materials prepared thereby

Номер: US20130310570A1

Methods that include latent 1,3-dipole-functional compounds are disclosed herein. The latent 1,3-dipole-functional compound (e.g., an oxime) can be used to form an active 1,3-dipole-functional compound (e.g., a nitrile oxide) that can be used to react with a cyclic alkyne in a dipolar cycloaddition reaction.

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28-11-2013 дата публикации

Chiral3-(benzylsulfinyl)-5,5-dimethyl-4,5-dihydroisoxazole derivatives and 5,5-dimethyl-3-[(1h-pyrazol-4-ylmethyl)sulfinyl]-4,5-dihyddroisoxazole derivatives, method for the production thereof, and use of same as herbicides and plant growth regulators

Номер: US20130316904A1
Принадлежит: Bayer CropScience AG

The invention relates to 3-(benzylsulfinyl)-5,5-dimethyl-4,5-dihydroisoxazole derivatives and 5,5-dimethyl-3-[(1H-pyrazol-4-ylmethyl)sulfinyl]-4,5-dihydroisoxazole derivatives of the formula (I) and their salts 2. The compound of the formula (I) as claimed in wherein{'sup': 1', '5', '9', '10', '9', '10', '9', '10, 'sub': 1', '4', '3', '6', '1', '4', '1', '4', '1', '4', '1', '4', '1', '2', '1', '3', '1', '3', '1', '4', '3', '6', '3', '6', '1', '2', '3', '6', '1', '4', '1', '2', '3', '4', '3', '4', '1', '4', '1', '4', '1', '4', '1', '4', '1', '4', '1', '4', '1', '4', '1', '4', '3', '4', '2', '4', '6', '1', '4', '6', '1', '4', '2', '4', '2', '4', '1', '6', '3', '6', '1', '6', '1', '6', '1', '6, 'the substituents Rto Rare independently of one another selected from the group consisting of hydrogen, hydroxyl, halogen, cyano, nitro, amino, C(O)OH, (C-C)-alkyl, (C-C)-cycloalkyl, (C-C)-haloalkyl, (C-C)-alkoxy, (C-C)-haloalkoxy, (C-C)-alkoxy-(C-C)-alkyl, (C-C)-alkylcarbonyl, (C-C)-alkylcarbonyloxy, (C-C)-alkoxycarbonyl, (C-C)-cycloalkoxycarbonyl, (C-C)-cycloalkyl-(C-C)-alkoxy, (C-C)-cycloalkoxy, (C-C)-alkoxycarbonyl-(C—O)-alkoxy, (C-C)-alkenyloxy, (C-C)-alkynyloxy, (C-C)-alkylthio, (C-C)-haloalkylthio, (C-C)-alkylsulfinyl, (C-C)-haloalkylsulfinyl, (C-C)-alkylsulfonyl, (C-C)-haloalkylsulfonyl, (C-C)-alkylsulfonyloxy, di-(C-C)-alkylamino, (C-C)-alkenyloxycarbonyl, (C-C)-alkynyloxycarbonyl, C-aryl-(C-C)-alkoxycarbonyl, C-aryl-(C-C)-alkoxy, formyl, (C-C)-alkenyl, (C-C)-alkynyl, phenyl, —C(O)NRR, where Rand Rindependently of one another are selected from the group consisting of hydrogen, (C-C)-alkyl, (C-C)-cycloalkyl, (C-C)-haloalkyl, or where Rand Rtogether form a (C-C)-alkylene group which may contain one oxygen or sulfur atom or one or two amino or (C-C)-alkylamino groups;'} {'sub': 1', '6', '1', '6, 'two substituents ortho to one another together form a (C-C)-alkylene group which may contain one or more oxygen and/or sulfur atoms, where the (C-C)-alkylene group may be mono- or ...

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28-11-2013 дата публикации

ANTIOXIDANT INFLAMMATION MODULATORS: OLEANOLIC ACID DERIVATIVES WITH AMINO AND OTHER MODIFICATIONS AT C-17

Номер: US20130317007A1
Принадлежит: REATA PHARMACEUTICALS, INC.

This invention provides, but is not limited to, novel oleanolic acid derivatives having the formula: 34-. (canceled)710-. (canceled)11. The compound of claim 5 , wherein either Xor Xis OR claim 5 , wherein Ris absent.12. The compound of claim 6 , wherein Xis ORand Ris absent.13. The compound of claim 5 , wherein Xis hydrogen.14. (canceled)15. The compound of claim 6 , wherein Y is NRR.1617-. (canceled)18. The compound of claim 6 , wherein Ror Rcomprises a fluoro group.19. The compound of claim 18 , wherein one of Ror Rcomprises a trifluoromethyl group.20. The compound of claim 6 , wherein Rand Rare each independently hydrogen claim 6 , alkyl claim 6 , aryl claim 6 , aralkyl claim 6 , heteroaryl claim 6 , heteroaralkyl claim 6 , or a substituted version of any of these groups.2123-. (canceled)24. The compound of claim 6 , wherein Ris alkylsulfonyl claim 6 , arylsulfonyl claim 6 , aralkylsulfonyl claim 6 , heteroarylsulfonyl claim 6 , heteroaralkylsulfonyl claim 6 , or a substituted version of any of these groups.2529-. (canceled)30. The compound of claim 6 , wherein Ris acyl.31. The compound of claim 6 , wherein Ris substituted acyl.32. (canceled)33. The compound of claim 6 , wherein R′ is cyano.34. (canceled)35. The compound of claim 2 , wherein Ris absent.3637-. (canceled)38. The compound of claim 6 , wherein Rand Rare each methyl.39. The compound of claim 5 , wherein Rand Rare each hydrogen.40. The compound of claim 2 , wherein the bond joining carbon 1 and carbon 2 is a double bond.41. The compound of claim 6 , wherein the bond joining carbon 9 and carbon 11 is a double bond.42. The compound of claim 6 , wherein the bond joining carbon 9 and carbon 11 is a single bond.43. The compound of claim 5 , wherein the bond joining carbon 12 and carbon 13 is a single bond.44. The compound of claim 5 , wherein the bond joining carbon 13 and carbon 18 is a single bond.45. (canceled)47. (canceled)49. (canceled)51. (canceled)53. (canceled)55. (canceled)57. (canceled)59. ( ...

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28-11-2013 дата публикации

Compounds and therapeutic uses thereof

Номер: US20130317027A1
Принадлежит: Myrexis, Inc.

The invention relates to compounds, pharmaceutical compositions and methods useful for treating cancer, systemic or chronic inflammation, rheumatoid arthritis, diabetes, obesity, T-cell mediated autoimmune disease, ischemia, and other complications associated with these diseases and disorders.

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28-11-2013 дата публикации

METHODS OF PEST CONTROL IN SOYBEAN

Номер: US20130317073A1
Принадлежит:

The present invention provides methods comprising applying to a crop of soybean plants, the locus thereof, or propagation material thereof, a compound a compound of formula III wherein A, A, A and A are independently C—H, or nitrogen and wherein #1 indicates the bond to X and #2 indicates the bond to cycle B; cycle B is selected from B1 to B6 wherein #1 indicates the bond to cycle A, #2 indicates the bond to Rand #3 indicates the bond to cycle C; cycle C is phenyl; Ris chloro, bromo, CFor methyl; Ris chlorodifluoromethyl or trifluoromethyl; each Ris independently bromo, chloro, fluoro or trifluoromethyl; p is 2 or 3; and wherein X is defined in the claims. The methods are preferably for the control of stinkbugs, in particular . 2. (canceled)6. A method according to claim 5 , wherein the method is for controlling and/or preventing infestation of the soybean crop by stinkbugs.7. (canceled)8. A method according to claim 5 , wherein X is P4 claim 5 , P5 or P6.9. A method according to claim 4 , wherein cycle B is cycle B1.11Nezara viridula, PiezodorusAcrosternumEuchistus heros.. A method according to claim 4 , wherein stinkbug is spp. claim 4 , spp claim 4 ,12Euschistus.. A method according to claim 4 , wherein stinkbug is13EuschistusEuschistus heros.. A method according to claim 1 , wherein is14. A method or use according to claim 1 , wherein the compound of formula I or formula II is applied in combination with one or more additional active ingredients selected from neonicotinoids claim 1 , pyrethroids claim 1 , strobilurins claim 1 , triazoles and carboxamides.15. A method according to claim 1 , wherein the compound is applied to the crop by foliar application.16. A method according to claim 1 , wherein the compound of formula I or formula II is applied in combination with an attractant selected from glucose claim 1 , saccharose claim 1 , salt claim 1 , glutamate claim 1 , citric acid claim 1 , soybean oil claim 1 , peanut oil and soybean milk. The present invention ...

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05-12-2013 дата публикации

NITRIC OXIDE DONOR NEPRILYSIN INHIBITORS

Номер: US20130323271A1
Принадлежит:

In one aspect, the invention relates to compounds having the formula: 2. The compound of claim 1 , where Ris —Calkyl substituted with 1 or 2 —ONOgroups.3. The compound of claim 2 , where Ris —(CH)(ONO).6. The compound of claim 1 , where Ris —OH and Ris H.7. The compound of claim 1 , where Ris —CHOH and Ris —CH.8. The compound of claim 1 , where X is selected from —COOR claim 1 , pyrazole claim 1 , imidazole claim 1 , triazole claim 1 , benzotriazole claim 1 , furan claim 1 , pyrrole claim 1 , tetrazole claim 1 , pyrazine claim 1 , thiophene claim 1 , oxazole claim 1 , isoxazole claim 1 , thiazole claim 1 , isothiazole claim 1 , oxadiazole claim 1 , thiadiazole claim 1 , pyridazine claim 1 , pyridine claim 1 , pyrimidine claim 1 , pyran claim 1 , benzimidazole claim 1 , benzoxazole claim 1 , benzothiazole claim 1 , pyridylimidazole claim 1 , and pyridyltriazole.10. The compound of claim 8 , where X is —COOR claim 8 , and Ris H.12. The compound of claim 1 , where Ris absent or is selected from H claim 1 , —Calkylene-OH claim 1 , —Calkylene-O—Calkyl claim 1 , —C(O)—Calkyl claim 1 , ═O claim 1 , and phenyl substituted with one halo.13. The compound of claim 1 , where Ris selected from H claim 1 , —OH claim 1 , —Calkyl claim 1 , pyridinyl claim 1 , and phenyl optionally substituted with one halo.14. The compound of claim 1 , where b is 0 or b is 1 and Ris 3′-chloro.15. The compound of claim 1 , where c is 0 claim 1 , or c is 1 and Ris 3′-chloro claim 1 , or c is 0 and Ris 2′-fluoro claim 1 , 5′-chloro or 2′ claim 1 ,5′-dichloro.18. A pharmaceutical composition comprising the compound of and a pharmaceutically acceptable carrier.19. The pharmaceutical composition of claim 18 , further comprising a therapeutic agent selected from adenosine receptor antagonists claim 18 , α-adrenergic receptor antagonists claim 18 , β-adrenergic receptor antagonists claim 18 , β-adrenergic receptor agonists claim 18 , dual-acting β-adrenergic receptor antagonist/α-receptor antagonists claim ...

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12-12-2013 дата публикации

NEPRILYSIN INHIBITORS

Номер: US20130330365A1
Принадлежит:

In one aspect, the invention relates to compounds having the formula X: 7. The compound of claim 6 , where Ris H and Ris —CHCH.21. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and the compound of .22. The pharmaceutical composition of claim 21 , further comprising a therapeutic agent selected from adenosine receptor antagonists claim 21 , α-adrenergic receptor antagonists claim 21 , β-adrenergic receptor antagonists claim 21 , β-adrenergic receptor agonists claim 21 , dual-acting β-adrenergic receptor antagonist/α-receptor antagonists claim 21 , advanced glycation end product breakers claim 21 , aldosterone antagonists claim 21 , aldosterone synthase inhibitors claim 21 , aminopeptidase N inhibitors claim 21 , androgens claim 21 , angiotensin-converting enzyme inhibitors and dual-acting angiotensin-converting enzyme/neprilysin inhibitors claim 21 , angiotensin-converting enzyme 2 activators and stimulators claim 21 , angiotensin-II vaccines claim 21 , anticoagulants claim 21 , anti-diabetic agents claim 21 , antidiarrheal agents claim 21 , anti-glaucoma agents claim 21 , anti-lipid agents claim 21 , antinociceptive agents claim 21 , anti-thrombotic agents claim 21 , ATreceptor antagonists and dual-acting ATreceptor antagonist/neprilysin inhibitors and multifunctional angiotensin receptor blockers claim 21 , bradykinin receptor antagonists claim 21 , calcium channel blockers claim 21 , chymase inhibitors claim 21 , digoxin claim 21 , diuretics claim 21 , dopamine agonists claim 21 , endothelin converting enzyme inhibitors claim 21 , endothelin receptor antagonists claim 21 , HMG-CoA reductase inhibitors claim 21 , estrogens claim 21 , estrogen receptor agonists and/or antagonists claim 21 , monoamine reuptake inhibitors claim 21 , muscle relaxants claim 21 , natriuretic peptides and their analogs claim 21 , natriuretic peptide clearance receptor antagonists claim 21 , neprilysin inhibitors claim 21 , nitric oxide donors claim 21 , non ...

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12-12-2013 дата публикации

NEPRILYSIN INHIBITORS

Номер: US20130330366A1
Принадлежит:

In one aspect, the invention relates to compounds having the formula XII: 3. The compound of claim 2 , where Ris H and Ris selected from H and —CHCH.5. The compound of claim 4 , where Ris H and Ris selected from H and —CHCH.13. The compound of claim 12 , where Ris H and Ris selected from H claim 12 , —CHOC(O)CH claim 12 , —CHOC(O)OCHCH claim 12 , —CHOC(O)OCH(CH) claim 12 , and —C(O)CH[CH(CH)]—NHC(O)OCH.15. The compound of claim 14 , where R is —CH claim 14 , Ris H claim 14 , and Ris selected from —CHOC(O)CH claim 14 , —CHOC(O)OCH(CH) claim 14 , —CHOC(O)OCHCH claim 14 , and —CHOC(O)CH[CH(CH)]—NHC(O)OCH.19. The compound of claim 18 , where Ris H and Ris selected from —CHOC(O)OCHCHand —CHOC(O)CH[CH(CH)]—NHC(O)OCH.21. The compound of claim 20 , where Ris H claim 20 , Ris —CHOP(O)(OH)or —CHOC(O)CH[CH(CH)]NH claim 20 , and Ris —CHCH; or Ris —C(O)CH[CH(CH)]NH claim 20 , Ris H claim 20 , and Ris —CHCH.23. The compound of claim 22 , where R claim 22 , R claim 22 , and Rare H; or Rand Rare H claim 22 , and Ris —CHOC(O)OCHCH.25. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and the compound of .26. The pharmaceutical composition of claim 25 , further comprising a therapeutic agent selected from adenosine receptor antagonists claim 25 , α-adrenergic receptor antagonists claim 25 , β-adrenergic receptor antagonists claim 25 , β-adrenergic receptor agonists claim 25 , dual-acting β-adrenergic receptor antagonist/α-receptor antagonists claim 25 , advanced glycation end product breakers claim 25 , aldosterone antagonists claim 25 , aldosterone synthase inhibitors claim 25 , aminopeptidase N inhibitors claim 25 , androgens claim 25 , angiotensin-converting enzyme inhibitors and dual-acting angiotensin-converting enzyme/neprilysin inhibitors claim 25 , angiotensin-converting enzyme 2 activators and stimulators claim 25 , angiotensin-II vaccines claim 25 , anticoagulants claim 25 , anti-diabetic agents claim 25 , antidiarrheal agents claim 25 , anti- ...

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19-12-2013 дата публикации

uPAR-uPA INTERACTION INHIBITORS AND METHODS FOR TREATING CANCER

Номер: US20130338144A1
Автор: Meroueh Samy

The invention described herein pertains to compounds, compositions and formulations comprising the compounds, and methods for use of the compounds, compositions and/or formulations in the treatment of diseases responsive to the inhibition of uPAR-uPA interactions, such as cancer. 3. The composition of wherein each Ris hydrogen.4. The composition of wherein Y is optionally substituted aryl or optionally substituted heteroaryl claim 1 , substituted with a carboxylic acid claim 1 , or derivative or analog thereof.5. The composition of wherein X is an optionally substituted nitrogen-containing heterocycle attached at nitrogen.6. The composition of further comprising one or more carriers claim 1 , diluents claim 1 , or excipients claim 1 , or a combination thereof.7. A unit dose or unit dosage form for treating cancer claim 1 , the unit dose or unit dosage form comprising a therapeutically effective amount of one or more compositions of for treating cancer.8. A method for treating cancer in a patient claim 1 , the method comprising the step of administering to the patient a therapeutically effective amount of one or more compositions of claim 1 , or one or more unit doses or unit dosage forms thereof claim 1 , or a combination thereof.9. The method of wherein the compound makes an energetically positive interaction with one or more of the residues selected from the group consisting of L150 claim 8 , L155 claim 8 , L168 claim 8 , and R53 on uPAR.10. The method of wherein the compound makes an energetically positive interaction with L168 uPAR.11. The method of wherein the compound makes an energetically positive interaction with R53 uPAR.12. The method of wherein the total of all interactions with uPAR is less than or equal to about −10 kcal/mol.1314-. (canceled)15. The method of wherein the interaction with L150 is less than about −2 kcal/mol.1617-. (canceled)18. The method of wherein the interaction with L168 is less than about −1 kcal/mol.19. The method of wherein the ...

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26-12-2013 дата публикации

METHODS OF TREATING CANCER AND OTHER DISORDERS

Номер: US20130345270A1
Принадлежит: Waake Forest University Health Sciences

Active compounds useful for inhibiting fatty acid synthase in a subject in need thereof are described. The active compounds are, in general, a 5-mercapto-1H-Indazole-4,7-dione or an analog thereof. The compounds are useful for treating subjects afflicted with, cancer, obesity, diabetes, a viral infection, a bacterial infection, a fungal infection, or a protozoal infection. 1. A method of reversibly or irreversibly inhibiting fatty acid synthase in a subject in need thereof , comprising administering to said subject an active compound as described herein in a treatment-effective amount; wherein said active compound is an 5-mercapto-1H-Indazole-4 ,7-dione or an analog thereof.2. The method of claim 1 , wherein said subject is afflicted with cancer.3. The method of claim 1 , wherein said subject is afflicted with obesity.4. The method of claim 1 , wherein said subject is afflicted with diabetes5. The method of claim 1 , wherein said subject is afflicted with a viral infection.6. The method of claim 1 , wherein said subject is afflicted with a bacterial infection.7. The method of claim 1 , wherein said subject is afflicted with a fungal infection.8. The method of claim 1 , wherein said subject is afflicted with a protozoal infection.11. (canceled) The present invention concerns methods of treatment, and compounds and compositions useful for carrying out such methods.A first aspect of the present invention is a method of inhibiting fatty acid synthase in a subject in need thereof, comprising administering to said subject an active compound as described herein in a treatment-effective amount. Examples of subjects in need thereof include, but are not limited to, subjects afflicted with cancer, obesity, diabetes, viral infection, bacterial infection, fungal infection or protozoal infection.A second aspect of the present invention is the use of an active compound as described herein for the preparation of a medicament for carrying out a method as described herein, such as ...

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09-01-2014 дата публикации

ISOXAZOLINE DERIVATIVES AS ANTIPARASITIC AGENTS

Номер: US20140011758A1
Принадлежит:

This invention recites isoxazoline substituted derivatives of Formula (1) stereoisomers thereof, geometric isomers thereof, veterinarily acceptable salts 5 thereof, compositions thereof, and their use as a parasiticide in animals. The variables A, W, R 1a, R 1b, R 1c, R 2, R 3, R 5, and n are as described herein. 10. A compound selected from the group consisting of3-hydroxy-3-{4-[5-(3,4,5-trichloro-phenyl)-5-trifluoromethyl-4,5-dihydro-isoxazol-3-yl]-phenyl}-cyclobutanecarboxylic acid (2,2,2-trifluoro-ethyl)-amide;3-hydroxy-3-{4-[5-(3,4,5-trichloro-phenyl)-5-trifluoromethyl-4,5-dihydro-isoxazol-3-yl]-phenyl}-cyclobutanecarboxylic acid cyclopropylamide;3-hydroxy-3-{4-[5-(3,4,5-trichloro-phenyl)-5-trifluoromethyl-4,5-dihydro-isoxazol-3-yl]-phenyl}-cyclobutanecarboxylic acid methylamide;3-hydroxy-3-{4-[5-(3,4,5-trichloro-phenyl)-5-trifluoromethyl-4,5-dihydro-isoxazol-3-yl]-phenyl}-cyclobutanecarboxylic acid dimethylamide;3-fluoro-3-{4-[5-(3,4,5-trichloro-phenyl)-5-trifluoromethyl-4,5-dihydro-isoxazol-3-yl]-phenyl}-cyclobutanecarboxylic acid cyclopropylamide;3-fluoro-3-{4-[5-(3,4,5-trichloro-phenyl)-5-trifluoromethyl-4,5-dihydro-isoxazol-3-yl]-phenyl}-cyclobutanecarboxylic acid cyclopropylamide;3-fluoro-3-{4-[5-(3,4,5-trichloro-phenyl)-5-trifluoromethyl-4,5-dihydro-isoxazol-3-yl]-phenyl}-cyclobutanecarboxylic acid (2,2,2-trifluoro-ethyl)-amide;3-fluoro-3-{4-[5-(3,4,5-trichloro-phenyl)-5-trifluoromethyl-4,5-dihydro-isoxazol-3-yl]-phenyl}-cyclobutanecarboxylic acid (2,2,2-trifluoro-ethyl)-amide;3-fluoro-3-{4-[5-(3,4,5-trichloro-phenyl)-5-trifluoromethyl-4,5-dihydro-isoxazol-3-yl]-phenyl}-cyclobutanecarboxylic acid methylamide;3-fluoro-3-{4-[5-(3,4,5-trichloro-phenyl)-5-trifluoromethyl-4,5-dihydro-isoxazol-3-yl]-phenyl}-cyclobutanecarboxylic acid methylamide;3-fluoro-3-{4-[5-(3,4,5-trichloro-phenyl)-5-trifluoromethyl-4,5-dihydro-isoxazol-3-yl]-phenyl}-cyclobutanecarboxylic acid dimethylamide;3-fluoro-3-{4-[5-(3,4,5-trichloro-phenyl)-5-trifluoromethyl-4,5-dihydro-isoxazol-3 ...

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09-01-2014 дата публикации

NEPRILYSIN INHIBITORS

Номер: US20140011997A1
Принадлежит: THERAVANCE, INC.

In one aspect, the invention relates to compounds having the formula: 1. (canceled)2. The process of claim 18 , where X is selected from pyrazole claim 18 , imidazole claim 18 , triazole claim 18 , benzotriazole claim 18 , furan claim 18 , pyrrole claim 18 , tetrazole claim 18 , pyrazine claim 18 , thiophene claim 18 , oxazole claim 18 , isoxazole claim 18 , thiazole claim 18 , isothiazole claim 18 , oxadiazole claim 18 , thiadiazole claim 18 , pyridazine claim 18 , pyridine claim 18 , pyrimidine claim 18 , pyran claim 18 , benzimidazole claim 18 , benzoxazole claim 18 , benzothiazole claim 18 , pyridylimidazole claim 18 , and pyridyltriazole.3. The process of claim 2 , where X is selected from pyrazole claim 2 , triazole claim 2 , benzotriazole claim 2 , tetrazole claim 2 , oxazole claim 2 , isoxazole claim 2 , thiazole claim 2 , pyridazine claim 2 , pyrimidine claim 2 , and pyridyltriazole.4. The process of claim 18 , where Ris selected from —ORand —NRR claim 18 , where Ris H claim 18 , Ris H or —OH claim 18 , and Ris H.7. The process of claim 18 , where Ris H.8. The process of claim 18 , where Ris absent or is selected from H; halo; —Calkylene-OH; —NH; —Calkyl; —CF; —Ccycloalkyl; —Calkylene-O—Calkyl; —C(O)R; —Calkylene-COOR; —C(O)NRR; —NHC(O)R; ═O; —NO; —C(CH)═N(OH); phenyl optionally substituted with one or two groups independently selected from halo claim 18 , —OH claim 18 , —CF claim 18 , —OCH claim 18 , —NHC(O)CH claim 18 , and phenyl; naphthalenyl; pyridinyl; pyrazinyl; pyrazolyl optionally substituted with methyl; thiophenyl optionally substituted with methyl or halo; furanyl; and —CH-morpholinyl; and Ris H.10. The process of claim 18 , where Ris absent or is selected from H; halo; —Calkylene-OH; —Calkyl; —Ccycloalkyl; —Calkylene-O—Calkyl; —C(O)R; —Calkylene-COOR; —C(O)NRR; —NHC(O)R; —NHC(O)R; ═O; phenyl optionally substituted with one or two groups independently selected from halo claim 18 , —OH claim 18 , and —OCH; pyridinyl; and pyrazinyl; Ris —Calkyl; ...

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16-01-2014 дата публикации

Sulfonamides as hib protease inhibitors

Номер: US20140018326A1
Принадлежит: Merck Canada Inc

Compounds of Formula I are disclosed: wherein L, A, R 1 , R 2 , R 3A , R 3B , R 4A , R 4B , R 5 , R 6 and R 7 are defined herein. The compounds encompassed by Formula I include compounds which are HIV protease inhibitors and other compounds which can be metabolized in vivo to HIV protease inhibitors. The compounds and their pharmaceutically acceptable salts are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.

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23-01-2014 дата публикации

Isoxazole Derivatives Useful As Antibacterial Agents

Номер: US20140024690A1
Принадлежит: PFIZER INC.

The present invention is directed to a new class of hydroxamic acid derivatives, their use as LpxC inhibitors and, more specifically, their use to treat bacterial infections. 2. The compound according to wherein{'sup': '1', 'sub': 1', '3, 'Ris (C-C)alkyl;'}{'sup': '2', 'sub': 1', '3, 'Ris (C-C)alkyl;'}{'sup': '3', 'Ris hydrogen;'}{'sub': 2', 'n', '2', 'n', '2', 'p', '2', 'n', '2', 'p', '2', 'n', '2', 'p', '2', 'n', '2', '2', 'p', '2', 'n', '2', 'p', '2', 'n', '2', 'p, 'sup': 4', '4', '4', '4, 'L is a bond, —(CH)—, —(CH)O(CH)—, —(CH)S(CH)—, —(CH)NR(CH)—, —(CH)SONR(CH)—, —(CH)CONR(CH)—, or —(CH)NRCO(CH)—;'}{'sup': 4', '5, 'sub': 1', '6', '3', '8, 'Rand Rare independently hydrogen, (C-C)alkyl, or (C-C)cycloalkyl;'}n is 0, 1, or 2;p is 0, 1, or 2;{'sup': 6', '4', '5, 'sub': 1', '6', '1', '6', '1', '6', '1', '6', '6', '12', '6', '12', '3', '8', '5', '12', '1', '10, 'Ris (C-C)alkoxy(C-C)alkyl, (C-C)alkoxycarbonyl, (C-C)alkylthiocarbonyl, (C-C)aryl, (C-C)aryloxy, (C-C)cycloalkyl, (C-C)heteroaryl, hydroxy(C-C)alkyl, or (NRR)carbonyl; and'}{'sup': '7', 'sub': 3', '13, 'Ris absent or (C-C)heterocycle.'}3. The compound according to wherein{'sup': '1', 'Ris methyl;'}{'sup': '2', 'Ris methyl;'}{'sup': '3', 'Ris hydrogen;'}{'sub': 2', 'n', '2', 'n', '2', 'p', '2', 'n', '2', 'p', '2', 'n', '2', 'p', '2', 'n', '2', '2', 'p', '2', 'n', '2', 'p', '2', 'n', '2', 'p, 'sup': 4', '4', '4', '4, 'L is a bond, —(CH)—, —(CH)O(CH)—, —(CH)S(CH)—, —(CH)NR(CH)—, —(CH)SONR(CH)—, —(CH)CONR(CH)—, or —(CH)NRCO(CH)—;'}{'sup': '4', 'sub': 1', '6', '3', '8, 'Ris hydrogen, (C-C)alkyl, or (C-C)cycloalkyl;'}n is 0, 1, or 2;p is 0, 1, or 2;{'sup': '6', 'sub': 6', '12', '6', '12', '6', '12', '1', '6', '1', '6', '1', '6, 'Ris (C-C)aryl or (C-C)aryloxy, wherein the (C-C)aryl group for each is phenyl optionally substituted with 1, 2, or 3 substituents that are independently (C-C)alkoxy, (C-C)alkyl, halo(C-C)alkoxy, halogen, or methylenedioxy; and'}{'sup': '7', 'sub': 3', '13', '3', '13, 'Ris absent or (C-C) ...

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30-01-2014 дата публикации

NOVEL GLP-1 RECEPTOR STABILIZERS AND MODULATORS

Номер: US20140031290A1
Принадлежит:

Compounds that bind the glucagon-like peptide 1 receptor (GLP-1) receptor are provided including compounds which are modulators of the GLP-1 receptors and compounds which are capable of inducing a stabilizing effect on the receptor for use in structural analyses of the GLP-1 receptor. Methods of synthesis, methods of therapeutic and/or prophylactic use, and methods of use in stabilizing GLP-1 receptor in vitro for crystallization of the GLP-1 receptor of such compounds are provided. 2. The compound of wherein the compound has the structure of Formula I-R or a pharmaceutically acceptable salt claim 1 , ester claim 1 , prodrug claim 1 , homolog claim 1 , hydrate or solvate thereof.3. The compound of wherein the compound has the structure of Formula I-S or a pharmaceutically acceptable salt claim 1 , ester claim 1 , prodrug claim 1 , homolog claim 1 , hydrate or solvate thereof.4. The compound of wherein the compound is substantially enantiomerically pure.5. The compound of wherein Wis -L-(CRR)-L-R.6. The compound of wherein Wis -L-(CRR)—R.7. The compound of wherein one of Lis —O—.8. The compound of wherein one of Lis —C(O)O—.9. The compound of wherein one of Lis —S(O)—.10. The compound of wherein one of Lis —S—.11. The compound of wherein one of Lis —N(R).12. The compound of wherein one of Lis —N(R)—C(O)—N(R)—.13. The compound of wherein one of Lis —N(R)—C(O)—.14. The compound of wherein one of Lis —S(O)—N(R)—.15. The compound of wherein Ris H.16. The compound of wherein one of Lis —O—.17. The compound of wherein both Rand Rare H.18. The compound of wherein one of Rand Ris methyl.19. The compound wherein one of Rand Ris methoxy.20. The compound of wherein in at least one instance Rand Rtaken together with the carbon to which they are attached form a cycloalkyl.21. The compound of wherein Ris alkyl substituted with Rand Ris phenyl.22. The compound of wherein Wis —NHC(O)—(CH)-L-R.23. The compound of wherein Ris H or alkyl.24. The compound of wherein Ris cycloalkyl claim ...

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30-01-2014 дата публикации

COMPOUND AS ANTAGONIST OF LYSOPHOSPHATIDIC ACID RECEPTOR, COMPOSITION, AND USE THEREOF

Номер: US20140031353A1
Принадлежит: CUREGENIX, INC.

The present invention relates to a compound as antagonist of LPA receptor, and a pharmaceutical composition comprising the same. The present invention also relates to the use of the compound and the composition, and a method of using the compound to treat, prevent or diagnose diseases, disorders or conditions associated with one or more of the LPA receptors. 32. The compound of any one of - claims 1 , wherein atom in any substituent groups is H claims 1 , H claims 1 , H claims 1 , C claims 1 , C claims 1 , N claims 1 , O claims 1 , O claims 1 , S claims 1 , F claims 1 , I and/or I.4. The compound according to claim 1 , wherein the compound is selected from:1-(2-chlorophenyl)ethyl(5-(1H-indol-5-yl)-3-methylisoxazol-4-yl)carbamate;1-(2-chlorophenyl)ethyl(5-(1H-indazol-5-yl)-3-methylisoxazol-4-yl)carbamate;1-(2-chlorophenyl)ethyl(5-(4-acetamidophenyl)-3-methylisoxazol-4-yl)carbamate;1-(2-chlorophenyl)ethyl(3-methyl-5-(4-propionamidophenyl)isoxazol-4-yl)carbamate;1-(2-chlorophenyl)ethyl(5-(4-isobutyramidophenyl)-3-methylisoxazol-4-yl)carbamate;1-(2-chlorophenyl)ethyl(5-(4-(cyclopropanecarboxamido)phenyl)-3-methylisoxazol-4-yl)carbamate;1-(2-chlorophenyl)ethyl(3-methyl-5-(methyl(4-methylisoxazol-3yl)phenyl)carbamate)carbamate;methyl 3-((4-(4-(((1-(2-chlorophenyl)ethoxy)carbonyl)amino)-3-methylisoxazol-5-yl)phenyl)amino)-3-oxopropanoate;methyl 1-((4-(4-(((1-(2-chlorophenyl)ethoxy)carbonyl)amino)-3-methylisoxazol-5-yl)phenyl)carbamoyl)cyclopropanecarboxylate;1-((4-(4-(((1-(2-chlorophenyl)ethoxy)carbonyl)amino)-3-methylisoxazol-5-yl)phenyl)carbamoyl)cyclopropanecarboxylic acid;4-((4-(4-(((1-(2-chlorophenyl)ethoxy)carbonyl)amino)-3-methylisoxazol-5-yl)phenyl)amino)-4-oxobutanoic acid;1-(2-chlorophenyl)ethyl(3-methyl-5-(4-(2-(methylsulfonyl)acetamido)phenyl)isoxazol-4-yl)carbamate;1-(2-chlorophenyl)ethyl(5-(4-(2-cyanoacetamido)phenyl)-3-methylisoxazol-4-yl)carbamate;1-(2-chlorophenyl)ethyl(5-(4-(2-ethoxyacetamido)phenyl)-3-methylisoxazol-4-yl)carbamate;1-(2-chlorophenyl)ethyl ...

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30-01-2014 дата публикации

PHENYL-ISOXAZOL DERIVATIVES AND PREPARATION PROCESS THEREOF

Номер: US20140031364A1
Принадлежит: IL-YANG PHARM. CO., LTD.

Disclosed are a phenyl-isoxazol derivative compound, which is useful as a treatment material for virus infection, especially, infection of an influenza virus, or its pharmaceutically acceptable derivative, a preparation method thereof, and an illness treatment pharmaceutical composition including the compound as an active ingredient. 2. The compound of or its pharmaceutically acceptable salt claim 1 , hydrate claim 1 , solvate claim 1 , prodrug claim 1 , or composite claim 1 , wherein when Ris the radical of Formula 2:{'sub': 1', '2', '3', '4', '5', '6', '7, 'two from among R, Rand Rare hydrogen, the remaining one is lower alkyl optionally substituted with halogen, lower alkoxy optionally substituted with halogen, or halogen, Ris methyl or amine, and from among R, Rand R, one or two each independently is hydrogen, lower alkyl optionally substituted with halogen, hydroxy, lower alkoxy, or halogen; or'}{'sub': 1', '2', '3', '4', '5', '6', '7, 'two from among R, Rand Rare hydrogen, the remaining one is trifluoromethyl, fluoro, or trifluoromethoxy, Ris methyl or amine, and from among R, Rand R, one or two each independently is hydrogen, methoxy, chlorine, fluoro, trifluoromethyl or hydroxy; or'}{'sub': 1', '4', '2', '3', '5', '7', '6, 'Ris halogen, preferably chlorine, Ris methyl or amine, R, R, R, and Reach is hydrogen, and Ris alkoxy.'}3. The compound of or its pharmaceutically acceptable salt claim 1 , hydrate claim 1 , solvate claim 1 , prodrug claim 1 , or composite claim 1 , wherein when Ris the radical of Formula 2:{'sub': 1', '2', '3', '4', '5', '6', '7, 'Ris trifluoromethyl or trifluoromethoxy, Rand Rare hydrogen, Ris methyl or amine, and from among R, Rand R, one or two each independently is hydrogen, hydroxy, methoxy, or chlorine; or'}{'sub': 1', '4', '2', '3', '5', '7', '6, 'Ris chlorine, Ris methyl, R, R, Rand Reach is hydrogen, and Ris methoxy; or'}{'sub': 2', '1', '3', '4', '5', '6', '7, 'Ris fluoro, trifluoromethyl, or trifluoromethoxy, Rand Reach is ...

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06-02-2014 дата публикации

ISOXAZOLINES FOR CONTROLLING INVERTEBRATE PESTS

Номер: US20140038821A1
Принадлежит: E.I. Du Pont De Nemours and Company

Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N-oxides, and salts thereof, 2. A compound of wherein{'sup': 1', '6, 'sub': 1', '3, 'Ris C-Calkyl optionally substituted with one or more substituents independently selected from R;'}{'sup': '2', 'sub': 1', '6', '1', '6, 'each Ris independently H, halogen, C-Chaloalkyl, C-Chaloalkoxy or —CN; and'}{'sup': '3', 'sub': 1', '6', '1', '6', '3', '6, 'each Ris independently H, halogen, C-Calkyl, C-Chaloalkyl, C-Ccycloalkyl,'}{'sub': 3', '6', '1', '6', '1', '6', '2, 'C-Chalocycloalkyl, C-Calkoxy, C-Chaloalkoxy, —CN or —NO.'}3. A compound of wherein{'sup': 1', '2', '3', '2, 'B, Band Bare independently CR;'}W is O;{'sup': '4', 'sub': 1', '6', '2', '7', '2', '7, 'Ris H, C-Calkyl, C-Calkylcarbonyl or C-Calkoxycarbonyl; and'}{'sup': 5', '11', '12', '1', '7, 'sub': 1', '4', '2', '4', '2', '4', '3', '4', '4', '7', '4', '7, 'Ris H, NRRor Q; or C-Calkyl, C-Calkenyl, C-Calkynyl, C-Ccycloalkyl, C-Calkylcycloalkyl or C-Ccycloalkylalkyl, each optionally substituted with one or more substituents independently selected from R.'}4. A compound of wherein{'sup': '1', 'sub': 1', '3, 'Ris C-Calkyl optionally substituted with halogen;'}{'sup': '2', 'sub': 3', '3, 'each Ris independently H, CF, OCF, halogen or —CN;'}{'sup': '3', 'sub': 1', '4', '1', '4', '3', '6', '1', '4, 'each Ris independently H, C-Calkyl, C-Chaloalkyl, C-Ccyclopropyl, C-Calkoxy or —CN; and'}{'sup': 7', '2, 'sub': 1', '4', '1', '4', '1', '4', '1', '4', '1', '4', '2', '4', '2', '4', '2', '5', '2', '5', '2', '5', '2', '5', '2', '2, 'each Ris independently halogen, C-Calkyl, C-Calkoxy, C-Calkylthio, C-Calkylsulfinyl, C-Calkylsulfonyl, C-Calkylcarbonyl, C-Calkoxycarbonyl, C-Calkylaminocarbonyl, C-Chaloalkylcarbonyl, C-Chaloalkoxycarbonyl, C-Chaloalkylaminocarbonyl, —NH, —CN or —NO; or Q.'}5. A compound of wherein{'sup': '4', 'Ris H;'}{'sup': 5', '7, 'sub': 1', '4, 'Ris C-Calkyl optionally substituted with one of more substituents independently ...

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06-02-2014 дата публикации

Compounds and methods for kinase modulation, and indications therefor

Номер: US20140038948A1
Принадлежит: Plexxikon Inc

Compounds active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.

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06-02-2014 дата публикации

Use of sGC stimulators, sGC activators, alone and combinations with PDE5 inhibitors for the treatment of systemic sclerosis (SSc).

Номер: US20140038956A1
Принадлежит: Bayer Intellectual Property GmbH

The use of sGC stimulators, sGC activators alone, or in combination with PDE5 inhibitors for the prevention and treatment of fibrotic diseases, such as systemic sclerosis, scleroderma, and the concomitant fibrosis of internal organs. 2. The method of claim 1 , comprising the treatment and/or prevention of systemic Sclerosis by administering the compound of formula (1) claim 1 , (2) claim 1 , (3) claim 1 , (4) claim 1 , (5) claim 1 , (6) claim 1 , (7) or (27).3. The method of claim 1 , comprising the treatment and/or prevention of Systemic Sclerosis by administering the compound of one of formulae (1) to (27) in combination with at least one PDE5 Inhibitor selected from the group of:Tadalafil ((6R,12aR)-2,3,6,7,12,12a-Hexahydro-2-methyl-6-(3,4-methylene-dioxyphenyl)pyrazino(1′,2′:1,6)pyrido(3,4-b)indole-1,4-dione), Vardenafil (2-(2-Ethoxy-5-(4-ethylpiperazin-1-yl-1-sulfonyl)phenyl)-5-methyl-7-propyl-3H-imidazo(5,1-f)(1,2,4)triazin-4-one), Sildenafil (3-[2-ethoxy-5-(4-methylpiperazin-1-yl)sulfonyl-phenyl]-7-methyl-9-propyl-2,4,7,8-tetrazabicyclo[4.3.0]nona-3,8,10-trien-5-one), Udenafil 5-[2-propyloxy-5-(1-methyl-2-pyrrolidinylethylamidosulfonyl)phenyl]-methyl-3-propyl-1,6-dihydro-7H-pyrazolo(4,3-d)pyrimidine-7-one, Dasantafil 7-(3-Bromo-4-methoxybenzyl)-1-ethyl-8-[[(1,2)-2-hydroxycyclopentyl]amino]-3-(2-hydroxyethyl)-3,7-dihydro-1-purine-2,6-dione, Avanafil 4-{[(3-chloro-4-methoxyphenyl)methyl]amino]-2-[[(2S)-2-(hydroxymethyl)pyrrolidin-1-yl]-N-(pyrimidin-2-ylmethyl)pyrimidine-5-carboxamide, Mirodenafil, Lodenafil, UK 369.003, UK 371.800, SLx 2101 of Surface Logix, LAS 34179Triazolo[1,2-]xanthine, 6-methyl-4-propyl-2-[2-propoxy-5-(4-methylpiperazino)sulfonyl]phenyl or a salts, hydrates or hydrates of the salts thereof.4. The method of claim 3 ,wherein the PDE5 inhibitor is sildenafil or vardenafil and the combination is administered for the prevention and/or treatment of Systemic Sclerosis (SSc).5. (canceled)6. The method of claim 1 , wherein the compound is ...

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