Настройки

Укажите год
-

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

Подробнее
-

Мониторинг СМИ

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

Подробнее

Форма поиска

Поддерживает ввод нескольких поисковых фраз (по одной на строку). При поиске обеспечивает поддержку морфологии русского и английского языка
Ведите корректный номера.
Ведите корректный номера.
Ведите корректный номера.
Ведите корректный номера.
Укажите год
Укажите год

Применить Всего найдено 20762. Отображено 100.
05-01-2012 дата публикации

Chemically stable ingredients as lemon odorant

Номер: US20120003170A1
Автор: Peter Fankhauser
Принадлежит: FIRMENICH SA

The present invention discloses certain nitrile compounds that are chemically stable and are useful as a lemon odorant or to impart a lemon odor to various consumer articles. The invention also relates to the compositions and articles that contain such compounds as well to the use of the compounds in a method of imparting a lemon odor to the compositions and articles.

Подробнее
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.

Подробнее
26-01-2012 дата публикации

3-aminoxalyl-aminobenzamide derivatives and insecticidal and miticidal agents containing same as active ingredient

Номер: US20120022263A1
Принадлежит: Agro Kanesho Co Ltd

The present invention herein provides a 3-aminooxalylaminobenzamide derivative which is used as an insecticide or miticide. The 3-aminooxalylaminobenzamide derivative is one represented by the following general formula [1]: (R 1 and R 2 each represent, for instance, a C 1 to C 3 alkoxy group or a C 1 to C 3 haloalkoxy group; R 3 and R 4 each represent, for instance, a C 1 to C 8 alkyl group or a C 1 to C 8 haloalkyl group; R 5 represents, for instance, a C 1 to C 5 haloalkyl group; R 6 and R 7 each represent, for instance, a hydrogen atom or a C 1 to C 5 alkyl group; Y represents, for instance, a hydrogen atom or a halogen atom; Z represents, for instance, a hydrogen atom; n is an integer ranging from 0 to 4 and m is an integer ranging from 0 to 2).

Подробнее
02-02-2012 дата публикации

Derivatives of aminocyclobutane or aminocyclobutene, their method of preparation and their use as medical products

Номер: US20120029013A1
Принадлежит: Pierre Fabre Medicament SA

The present invention concerns compounds of general formula (1), where in:—-a- is a single or double bond, Ar is an aromatic group, substituted or unsubstituted, R1 and R2 each independently or together are: a hydrogen atom or C 1 -C 6 alkyl group, branched or unbranched, saturated or unsaturated, substituted or unsubstituted; the groups R1 and R2 may also form a heterocycle, R3 and R3′ each independently or together are a hydrogen atom or C 1 -C 6 alkyl group, X is an oxygen atom or a sulphur atom, and the addition salts of the compounds of general formula (1) with pharmaceutically acceptable mineral acids or organic acids.

Подробнее
16-02-2012 дата публикации

Substituted acylguanidine derivatives (as amended)

Номер: US20120041036A1
Принадлежит: Astellas Pharma Inc

An object of the present invention is to provide an excellent agent for treating or preventing dementia, schizophrenia based on serotonin 5-HT 5A receptor modulating action. It was discovered that acylguanidine derivatives, in which the guanidine is bonded to one ring of a naphthalene via a carbonyl group and a cyclic group is bonded to the other ring thereof, exhibit potent the 5-HT 5A receptor modulating action and excellent pharmacological actions based on the action. The present invention is useful as an excellent agent for treating or preventing dementia, schizophrenia, bipolar disorder or attention deficit hyperactivity disorder.

Подробнее
23-02-2012 дата публикации

Diacylethylenediamine compound

Номер: US20120046292A1
Принадлежит: Astellas Pharma Inc

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

Подробнее
15-03-2012 дата публикации

Methods of making lubiprostone and intermediates thereof

Номер: US20120065409A1
Принадлежит: Apotex Pharmachem Inc

There is provided processes for preparing Lubiprostone and intermediates thereof. Also provided are compounds, including intermediates for preparing Lubiprostone as well compositions comprising Lubiprostone and other compounds, including intermediates for preparing Lubiprostone and other compounds. (I)

Подробнее
22-03-2012 дата публикации

Metallo-beta-lactamase inhibitors

Номер: US20120071457A1
Принадлежит: Individual

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

Подробнее
29-03-2012 дата публикации

Process for the preparation of cilastatin and sodium salt

Номер: US20120078009A1

An improved process for preparing Cilastatin Sodium including dissolving Cilastatin acid in a solvent using an organic base, adding sodium salt of a week acid and isolating Cilastatin Sodium.

Подробнее
12-04-2012 дата публикации

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

Номер: US20120088746A1
Принадлежит: PFIZER INC

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

Подробнее
03-05-2012 дата публикации

Cross-Coupled Peptide Nucleic Acids for Detection of Nucleic Acids of Pathogens

Номер: US20120107794A1

The present invention concerns methods for detecting a nucleic acid comprising (i) contacting a solution comprising a first PNA having a first cross-reactive functional group with a substrate having a second PNA affixed thereto, the second PNA having a second first cross-reactive functional group, wherein the first PNA has a reporter molecule attached thereto and the first and second PNAs being complementary to different portions of a target DNA; (ii) contacting a sample suspected of containing the nucleic acid with the first and second PNAs; and (iii) determining the presence of the reporter molecule on the substrate.

Подробнее
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.

Подробнее
17-05-2012 дата публикации

Phenoxy substituted phenylamidine derivatives and their use as fungicides

Номер: US20120122678A1
Принадлежит: Bayer CropScience AG

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

Подробнее
17-05-2012 дата публикации

Substituted carbamoylcycloalkyl acetic acid derivatives as nep

Номер: US20120122764A1
Принадлежит: NOVARTIS AG

The present invention provides a compound of formula I; or a pharmaceutically acceptable salt thereof, wherein R 1 , R 2 , R 3 , R 4 , R 5 , B, X, m and n are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides pharmaceutical composition of compounds of the invention, and a combination of pharmacologically active agents and a compound of the invention.

Подробнее
17-05-2012 дата публикации

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

Номер: US20120122920A1

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

Подробнее
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.

Подробнее
31-05-2012 дата публикации

Fty720-derived anticancer agents

Номер: US20120136063A1

A number of FTY720-derived compounds with antitumor activity are described. These compounds include the compounds of formula I: wherein R 1 is independently selected from the group consisting of hydrogen, methyl. methoxy, and hydroxyl; R 2 is independently selected from the group consisting of hydrogen, methoxy, and hydroxyl; R 3 is independently selected from the group consisting of alkyl and cyclo-alkyl; and n is independently selected from 0 to 6. The compounds have lower immunosuppressive side effects as a result of not being phosphorylated by sphingosine kinase 2.

Подробнее
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.

Подробнее
07-06-2012 дата публикации

Biphenylacetamide derivative

Номер: US20120142771A1
Принадлежит: Sumitomo Dainippon Pharma Co Ltd

The present invention provides a compound of formula (I) or a salt thereof, wherein R 1 , R 2 and R 3 are independently selected from the group consisting of hydrogen atom, fluorine atom, chlorine atom, bromine atom, C 1-6 alkyl, C 1-6 alkoxy substituted with fluorine atom, and others; R 4 and R 5 are independently selected from the group consisting of hydrogen atom, fluorine atom, chlorine atom, C 1-6 alkyl, C 1-6 alkoxy substituted with fluorine atom, and others; R 6 and R 7 are independently selected from the group consisting of hydrogen atom, fluorine atom, methyl, ethyl, hydroxy group, and others; and R 8 and R 9 are independently selected from the group consisting of hydrogen atom, C 1-6 alkyl, and others, which is useful as an agent for treating or preventing various types of epilepsy including partial seizures and/or generalized seizures.

Подробнее
07-06-2012 дата публикации

Process For The Synthesis Of (+) And (-)-1-(3,4-Dichlorophenyl)-3-Azabicycle[3.1.0]Hexane

Номер: US20120142940A1
Принадлежит: Euthymics Bioscience Inc, Merck and Co Inc

The present invention is concerned with novel processes for the preparation of (+)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane or a pharmaceutically acceptable salt thereof, and (−)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane or a pharmaceutically acceptable salt thereof. These compounds have pharmaceutical utility and are known to be useful for treating e.g., depression, anxiety disorders, eating disorders and urinary incontinence.

Подробнее
14-06-2012 дата публикации

Enzyme inhibitors

Номер: US20120149736A1
Принадлежит: Chroma Therapeutics Ltd

Compounds of formula (I), inhibit HDAC activity: wherein A, B and D independently represent ═CH— or ═N—; W is —CH═CH— Or —CH 2 CH 2 —; R 1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intra-cellular carboxylesterase enzymes to a carboxylic acid group; R2 and R3 are selected from the side chains of a natural or non-nat-ural alpha amino acid, provided that neither R2 nor R3 is hydrogen, or R2 and R3, taken together with the carbon to which they are attached, form a 3-6 membered saturated cycloalkyl or heterocyclyl ring; Y is a bond, —C(═O)—, —S(═O)2—, —C(═O)O—, —C(═O)NR′—, —C(═5)—NR′, —C(═NH)NR′ or —S(═O) 2 NR — wherein R′ is hydrogen or optionally substituted C 1 —C 6 alkyl; L 1 is a divalent radical of formula —(Alk 1 ) m ,(Q) n (Alk 2 ) p — wherein m, n, p, Q, Alk 1 and Alk 2 are as defined in the claims; X 1 represents a bond; —C(═O); or —S(═O) 2 —; —NR 4 C(═O)—, —C(═O)NR 4 —,— NR 4 C(═O)NR 5 —, —NR 4 S(═O) 2 —, or —S(═O) 2 NR 4 — wherein R4 and R5 are independently hydrogen or optionally substituted C 1 -C 6 alkyl; and z is 0 or 1.

Подробнее
21-06-2012 дата публикации

Phosphorous derivatives as chemokine receptor modulators

Номер: US20120157413A1
Принадлежит: Allergan Inc

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

Подробнее
28-06-2012 дата публикации

Amino- and amido-aminotetralin derivatives and related compounds as mu opioid receptor antagonists

Номер: US20120165360A1
Принадлежит: Theravance Inc

The invention provides amino- and amido-aminotetralin compounds of formula (I): wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , and n are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.

Подробнее
05-07-2012 дата публикации

Compositions, Synthesis, and Methods of Using Cycloalkylmethylamine Derivatives

Номер: US20120172426A1
Принадлежит: Reviva Pharmaceuticals Inc

The present invention provides novel cycloalkylmethylamine derivatives, and methods of preparing cycloalkylmethylamine derivatives. The present invention also provides methods of using cycloalkylmethylamine derivatives and compositions of cycloalkylmethylamine derivatives. The pharmaceutical compositions of the compounds of the present invention can be advantageously used for treating and/or preventing obesity and obesity related co-morbid indications and depression and depression related co-morbid indications.

Подробнее
09-08-2012 дата публикации

Substituted 4-aminocyclohexane derivatives

Номер: US20120202810A1
Принадлежит: GRUENENTHAL GmbH

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

Подробнее
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.

Подробнее
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.

Подробнее
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.

Подробнее
11-10-2012 дата публикации

Novel ligands that modulate rar receptors

Номер: US20120258996A1
Принадлежит: Galderma Research and Development SNC

Novel ligand compounds having the general formula (I): and pharmaceutical/cosmetic compositions comprised thereof are useful in human and veterinary medicine or, alternatively, in cosmetics.

Подробнее
08-11-2012 дата публикации

Anthranilic acid derivatives

Номер: US20120283326A1
Принадлежит: Chelsea Therapeutics Inc

Compounds of formula (I) are provided, wherein X is CH═CH, CH 2 O wherein the oxygen atom is bound to ring B, or OCH 2 wherein the oxygen atom is bound to ring A; Y is hydrogen, straight or branched C1-C6 alkyl or a pharmaceutically acceptable inorganic cation; R1 is ethyl or cyclopropyl; and R2 and R3 are the same or different and are selected from F, Cl, Br, CF 3 and OCF 3 . The compounds are useful for the treatment of autoimmune diseases, inflammatory diseases, organ transplant rejection, and malignant neoplasia. Pharmaceutical compositions containing the compounds, methods of using the compounds, and methods for preparing the compounds are also provided.

Подробнее
08-11-2012 дата публикации

Dehydrogenation Process

Номер: US20120283494A1
Принадлежит: ExxonMobil Chemical Patents Inc

In a dehydrogenation process a hydrocarbon stream comprising at least one non-aromatic six-membered ring compound and at least one five-membered ring compound is contacted with a first catalyst comprising at least one metal component and at least one support and a second catalyst. The first catalyst is utilized to convert at least a portion of the at least one non-aromatic six-membered ring compound in the hydrocarbon stream to at least one aromatic compound and the second catalyst is utilized to convert at least a portion of the at least one five-membered ring compound in the hydrocarbon stream to at least one paraffin.

Подробнее
20-12-2012 дата публикации

Heterocyclic sulfonamides, uses and pharmaceutical compositions thereof

Номер: US20120322823A1
Принадлежит: PFIZER INC

The invention is directed to a class of compounds, including the pharmaceutically acceptable salts of the compounds, having the structure of formula I: as defined in the specification. The invention is also directed to compositions containing and uses of the compounds of formula I.

Подробнее
20-12-2012 дата публикации

4-((phenoxyalkyl)thio)-phenoxyacetic acids and analogs

Номер: US20120322875A1
Принадлежит: Individual

The invention features 4-((phenoxyalkyl)thio)-phenoxyacetic acids and analogs, compositions containing them, and methods of using them as PPAR delta modulators to treat or inhibit the progression of, for example, dyslipidemia.

Подробнее
27-12-2012 дата публикации

Therapeutic compounds

Номер: US20120329866A1

The invention provides compounds of Formula (I): R 1 ≡R 2   (I) wherein R 1 and R 2 have any of the values or specific values defined herein, as well as compositions comprising such compounds and therapeutic methods comprising the administration of such compounds.

Подробнее
24-01-2013 дата публикации

Arachidonic acid analogs and methods for analgesic treatment using same

Номер: US20130023510A1
Принадлежит: Cytometix Inc

The present invention provides arachidonic acid (AA) analogs and compositions containing those analogs as active agents for use in analgesic treatments. Various methods of manufacturing the inventive compounds are provided and pharmaceutical formulations, including injectable and oral dosages, are described. Certain analogs are additionally useful as antipyretic compositions and in related fever reducing treatments.

Подробнее
31-01-2013 дата публикации

Process for the preparation of lacosamide

Номер: US20130030216A1
Принадлежит: EUTICALS SPA

A novel process for the synthesis of Lacosamide using D,L-serine as starting material is described, where the methylation reaction of hydroxyl is carried out using an inexpensive base such as NaOH and an inexpensive alkylating agent, non-toxic and non-carcinogenic, such as methyl p-toluenesulfonate; the R enantiomer is isolated from the racemic mixture of Lacosamide after selective hydrolysis of the acetamide, salification of the racemic mixture with a chiral acid (HX*) in an organic solvent, resolution of the diastereoisomeric mixture, preferably by precipitation of the R enantiomer, and subsequent acetylation of the optically pure intermediate.

Подробнее
28-02-2013 дата публикации

Diazeniumdiolate cyclopentyl derivatives

Номер: US20130053352A1
Принадлежит: Merck Sharp and Dohme LLC

A compound having the structure or a pharmaceutically acceptable salt thereof, wherein R 1 is hydrogen, —OH, —O—C 1-6 alkyl, ═O, or halogen; R 2 is hydrogen, C(O)OR 8 , C 6 H 5 C(O)OR 8 , (CH 2 ) 1-2 OH, CR 9 R 10 OH, C(O)O(CH 2 ) 0-2 aryl, C(O)NR 9 R 10 , C(O)SO 2 NR 9 R 10 , C 6 H 5 OR 9 , W—C(O)OR 8 , W—OR 9 , Y, or P(O)(OR 9 )(ORlO); R 3 is hydrogen or —C 1-6 alkyl; R 4 is hydrogen, —OH or —C(O)OR 9 ; R 5 is hydrogen or deuterium; R 6 and R 7 are independently —C 1-6 alkyl, fluoro-substituted —C 1-6 alkyl, deutero-substituted —C 1-6 alkyl or —(CH 2 ) 1-2 R 11 , wherein any carbon atom of the fluoro-substituted —C 1-6 alkyl is mono- or di-substituted with fluoro, and any carbon atom of the deutero-substituted —C 1-6 alkyl is mono- or di-substituted with fluoro; R 8 , in each instance in which it occurs, is independently hydrogen, —C 1-6 alkyl, or —(CH 2 ) 2 N + (CH 3 ) 3 ; R 9 and R 10 , in each instance in which they occur, are independently —C 1-6 alkyl; R 11 is —OH, —O—C 1-6 alkyl, -0CD3, —OC(O)OC 1-6 alkyl, —NH 2 , —C 6 H 5 , —N 3 , or W; W is an unsubslituted 5- or 6-raembered heteroaryl ring having 1, 2, or 3 nitrogen atoms, or a substituted 5- or 6-membered heteroaryl ring having 1, 2, or 3 nitrogen atoms that is mono- or di-substituted at any carbon atom with R 6 or R 7 ; Y is a 5- or 6-membered heterocyclic ring having 1, 2, 3 or 4 heteroatoms which are N, O, or S or stereoisomers thereof, or pharmaceutically acceptable salts thereof, or pharmaceutically acceptable salts of stereoisomers thereof, and methods of using the compounds for treating hypertension.

Подробнее
28-02-2013 дата публикации

Cyclopentanecarboxamide derivatives, medicaments containing such compounds and their use

Номер: US20130053412A1
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

The invention relates to cyclopentanecarboxamide derivatives of formula 1, to their use as Fatty Acid Synthase inhibitors, to methods for their therapeutic use and to pharmaceutical compositions containing them, wherein R 1 , R 2 , R 3 , LO, W, AR 1 , n are as defined in claim 1 .

Подробнее
14-03-2013 дата публикации

Fluorine-Containing Sulfonate, Fluorine-Containing Sulfonate Resin, Resist Composition and Pattern Formation Method

Номер: US20130065182A1
Принадлежит: Central Glass Co Ltd

According to the present invention, there is provided a fluorine-containing sulfonate resin having a repeating unit of the following general formula (3). In order to prevent deficiency such as roughness after pattern formation or failure in pattern formation, the fluorine-containing sulfonate resin incorporates therein a photoacid generating function and serves as a resist resin in which “a moiety capable of changing its developer solubility by the action of an acid” and “a moiety having a photoacid generating function” are arranged with regularity.

Подробнее
14-03-2013 дата публикации

Compounds (cystein based lipopeptides) and compositions as tlr2 agonists used for treating infections, inflammations, respiratory diseases etc.

Номер: US20130065861A1
Принадлежит: IRM LLC

The invention provides a novel class of compounds viz. generally lipopeptides like Pam3CSK4, immunogenic compositions and pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with Toll-Like Receptors 2. In one aspect, the compounds are useful as adjuvants for enhancing the effectiveness a vaccine.

Подробнее
16-05-2013 дата публикации

Imaging Agents

Номер: US20130123618A1
Автор: Mark M. Goodman
Принадлежит: EMORY UNIVERSITY

This invention provides amino acid derivatives useful in detecting and evaluating brain and body tumors, including (1S,2S) anti-2-[ 18 F]FACPC and (1R,2R) anti-2-[ 18 F]FACPC.

Подробнее
30-05-2013 дата публикации

Cyclopropene amine compounds

Номер: US20130137575A1
Автор: Edward C. Sisler
Принадлежит: North Carolina State University

Methods of applying cyclopropene amine derivatives and compositions thereof to inhibit ethylene receptors in plants and plant material are disclosed. Methods include applying to the plant an effective ethylene response-inhibiting amount of at least one cyclopropene amine compound or composition thereof. Cyclopropene amine compounds, enantiomers, stereoisomers or salts thereof are also provided.

Подробнее
30-05-2013 дата публикации

4-carboxybenzylamino derivatives as histone deacetylase inhibitors

Номер: US20130137690A1
Принадлежит: Individual

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

Подробнее
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.

Подробнее
04-07-2013 дата публикации

Cysteine protease inhibitors

Номер: US20130172232A1
Принадлежит: Medivir UK Ltd

Compounds of the formula I wherein R 2a and R 2b are independently H, halo, C 1 -C 4 alkyl, C 1 -C 4 haloalkyl or C 1 -C 4 alkoxy, or R 2a and R 2b together with the carbon atom to which they are attached form a C 3 -C 6 cycloalkyl; R 3 is a C 5 -C 10 alkyl, optionally substituted with 1-3 substituents independently selected from halo, C 1 -C 4 haloalkyl, C 1 -C 4 alkoxy, C 1 -C 4 haloalkoxy; or R 3 is a C 2 -C 4 alkyl chain with at least 2 chloro or 3 fluoro substituents; or R 3 is C 3 -C 7 cycloalkylmethyl, optionally substituted with 1-3 substituents independently selected from C 1 -C 4 alkyl, halo, C 1 -C 4 haloalkyl, C 1 -C 4 alkoxy, C 1 -C 4 haloalkoxy; R 4 is C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, C 1 -C 6 alkoxy, C 1 -C 6 haloalkoxy, C 1 -C 6 alkylamino, C 1 -C 6 dialkylamino or; R 4 is Het or Carbocyclyl, either of which is optionally substituted with 1-3 substituents R 4 is Het, carbocyclyl, C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, C 1 -C 6 alkoxy or C 1 -C 6 haloalkoxy; n is 1, 2 or 3; for the use in the prophylaxis or treatment of a disorder characterised by inappropriate expression or activation of cathepsin S.

Подробнее
18-07-2013 дата публикации

Methods and compositions for treatment of cancer and autoimmune disease

Номер: US20130184342A1
Принадлежит: Jackson Laboratory

The technology described herein relates to methods of inducing cell death. The technology described herein further relates to treating conditions including cancers and autoimmune diseases comprising administering inhibitors of double strand break repair. Also described herein are inhibitors of double strand break repair and methods of screening for such inhibitors.

Подробнее
15-08-2013 дата публикации

23-yne-vitamin d3 derivative

Номер: US20130210781A1
Принадлежит: Teijin Pharma Ltd

To provide a novel vitamin D 3 derivative useful as a therapeutic agent for osteoporosis. Provided is a vitamin D 3 derivative represented by the following formula (1) or a medicinally acceptable solvate thereof: wherein R 1 represents a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, an alkylcarbonyloxyalkyl group with each alkyl having 1 to 6 carbon atoms, or an arylcarbonyloxyalkyl group with the aryl having 6 to 10 carbon atoms and the alkyl having 1 to 6 carbon atoms; R 2 represents a hydrogen atom or an alkyl group having 1 to 6 carbon atoms or, together with the other R 2 and the carbon atom to which they are bound to, may form a cyclic alkyl group having 3 to 6 carbon atoms; R 3 represents an alkyl group having 1 to 6 carbon atoms or, together with the other R 3 and the carbon atom to which they are bound to, may form a cyclic alkyl group having 3 to 6 carbon atoms; X represents an oxygen atom or a methylene group; and n represents an integer of 1 or 2.

Подробнее
15-08-2013 дата публикации

Process for preparing carboxamidine compounds

Номер: US20130211130A1
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

The present invention relates to a process of making a compound of formula (I): Wherein, R 1 , R 2 , R 4 and X are as defined herein.

Подробнее
22-08-2013 дата публикации

Entecavir synthesis method and intermediate compound thereof

Номер: US20130217879A1
Автор: Zhiguo Zheng
Принадлежит: AUSUN PHARMATECH CO Ltd

The present invention relates to a preparation method for a medicine and an intermediate compound thereof, specifically, relates to a preparation method for entecavir, an intermediate compound thereof, and a synthesis method for the intermediate compound.

Подробнее
22-08-2013 дата публикации

Process for the preparation of substituted n-(benzyl)cyclopropanamines by imine hydrogenation

Номер: US20130217910A1
Принадлежит: Bayer Intellectual Property GmbH

The present invention relates to a process for the preparation of substituted N-(benzyl)cyclopropanamines of the general formula (II) starting from N-[(aryl)methylene]cyclopropanamine derivatives. The present invention further provides the N-[(arypmethylene]cyclopropanamine derivatives used as starting compounds in this process according to the invention, and their use for the preparation of substituted N (benzyl)cyclopropanamines.

Подробнее
29-08-2013 дата публикации

Continuous process for conversion of lignin to useful compounds

Номер: US20130224816A1
Принадлежит: Chemtex Italia SpA

This specification discloses an operational continuous process to convert lignin as found in ligno-cellulosic biomass before or after converting at least some of the carbohydrates. The continuous process has been demonstrated to create a slurry comprised of lignin, raise the slurry comprised of lignin to ultra-high pressure, deoxygenate the lignin in a lignin conversion reactor over a catalyst which is not a fixed bed without producing char. The conversion products of the carbohydrates or lignin can be further processed into polyester intermediates for use in polyester preforms and bottles.

Подробнее
29-08-2013 дата публикации

Process for the preparation of lubiprostone

Номер: US20130225842A1
Принадлежит: Individual

Processes for preparing and purifying lubiprostone are disclosed. Intermediates and preparation thereof are also disclosed.

Подробнее
29-08-2013 дата публикации

Continuous process for conversion of lignin to useful compounds

Номер: US20130225855A1
Принадлежит: Chemtex Italia SpA

This specification discloses an operational continuous process to convert lignin as found in ligno-cellulosic biomass before or after converting at least some of the carbohydrates. The continuous process has been demonstrated to create a slurry comprised of lignin, raise the slurry comprised of lignin to ultra-high pressure, deoxygenate the lignin in a lignin conversion reactor over a catalyst which is not a fixed bed without producing char. The conversion products of the carbohydrates or lignin can be further processed into polyester intermediates for use in polyester preforms and bottles.

Подробнее
12-09-2013 дата публикации

4-SUBSTITUTED-3-BENZYLOXY-BICYCLO[3.1.0]HEXANE COMPOUNDS AS mGluR 2/3 ANTAGONISTS

Номер: US20130237573A1
Принадлежит: Eli Lilly and Co

A mGlu2/3 receptor antagonist of the formula: its uses, and methods for its preparation are described.

Подробнее
19-09-2013 дата публикации

Calcium-sensing receptor-active compounds

Номер: US20130244995A1
Принадлежит: Leo Pharma AS

Compounds of general formula (I), their use as calcium receptor-active compounds for the prophylaxis, treatment or amelioration of physiological disorders or diseases associated with disturbances of CaSR activity, such as hyperparathyroidism, pharmaceutical compositions comprising said compounds, and methods of treating diseases with said compounds.

Подробнее
03-10-2013 дата публикации

Radiation-sensitive resin composition, pattern-forming method, polymer, and compound

Номер: US20130260315A1
Принадлежит: JSR Corp

A radiation-sensitive resin composition includes a polymer component that includes one or more types of polymers, and a radiation-sensitive acid generator. At least one type of the polymer of the polymer component includes a first structural unit represented by a following formula (1). R 1 represents a hydrogen atom, a fluorine atom, a methyl group or a trifluoromethyl group. R 2 represents a linear alkyl group having 5 to 21 carbon atoms. Z represents a divalent alicyclic hydrocarbon group or an aliphatic heterocyclic group having a ring skeleton which has 4 to 20 atoms. A part or all of hydrogen atoms included in the alicyclic hydrocarbon group and the aliphatic heterocyclic group represented by Z are not substituted or substituted.

Подробнее
03-10-2013 дата публикации

Polymorphic Form of N-(S)-(3,4-Difluoro-2-(2-Fluoro-4-Iodophenylamino)-6-Methoxyphenyl)-1-(2,3-Dihydroxypropyl)Cyclopropane-1-Sulfonamide and uses thereof

Номер: US20130261339A1
Автор: Stuart Dimock
Принадлежит: Ardea Biociences Inc

Disclosed herein, in certain embodiments, is a crystalline polymorph form A of N—(S)-(3,4-difluoro-2-(2-fluoro-4-iodophenylamino)-6-methoxyphenyl)-1-(2,3-dihydroxypropyl)cyclopropane-1-sulfonamide. Further disclosed herein, in certain embodiments, are pharmaceutical compositions comprising the crystalline polymorph form A of N—(S)-(3,4-difluoro-2-(2-fluoro-4-iodophenylamino)-6-methoxyphenyl)-1-(2,3-dihydroxypropyl)cyclopropane-1-sulfonamide.

Подробнее
10-10-2013 дата публикации

Purificiation of precursor compound by crystallisation

Номер: US20130267730A1
Автор: Anne Nilsen, Sondre NILSEN
Принадлежит: GE Healthcare Ltd

The invention relates to a process for preparation of radiopharmaceutical precursors, and in particular protected amino acid derivatives which are used as precursors for production of radiolabelled amino acids for use in vivo imaging procedures such as positron emission tomography (PET). Particularly, the invention relates to a process for preparation of a precursor useful in the preparation of the [ 18 F]-1-amino-3-fluorocyclobutanecarboxylic acid ([ 18 F] FACBC) PET tracer.

Подробнее
17-10-2013 дата публикации

Low molecular weight cationic lipids for oligonucleotide delivery

Номер: US20130274523A1
Принадлежит: Individual

The instant invention provides for novel cationic lipids that can be used in combination with other lipid components such as cholesterol and PEG-lipids to form lipid nanoparticles with oligonucleotides. It is an object of the instant invention to provide a cationic lipid scaffold that demonstrates enhanced efficacy along with lower liver toxicity as a result of lower lipid levels in the liver. The present invention employs low molecular weight cationic lipids with one short lipid chain to enhance the efficiency and tolerability of in vivo delivery of siRNA.

Подробнее
24-10-2013 дата публикации

Novel ruthenium complexes and their uses in processes for formation and/or hydrogenation of esters, amides and derivatives thereof

Номер: US20130281664A1
Принадлежит: Yeda Research and Development Co Ltd

The present invention relates to novel Ruthenium catalysts and related borohydride complexes, and the use of such catalysts, inter alia, for (1) hydrogenation of amides (including polyamides) to alcohols and amines; (2) preparing amides from alcohols with amines (including the preparation of polyamides (e.g., polypeptides) by reacting dialcohols and diamines and/or by polymerization of amino alcohols); (3) hydrogenation of esters to alcohols (including hydrogenation of cyclic esters (lactones) or cyclic di-esters (di-lactones) or polyesters); (4) hydrogenation of organic carbonates (including polycarbonates) to alcohols and hydrogenation of carbamates (including polycarbamates) or urea derivatives to alcohols and amines; (5) dehydrogenative coupling of alcohols to esters; (6) hydrogenation of secondary alcohols to ketones; (7) amidation of esters (i.e., synthesis of amides from esters and amines); (8) acylation of alcohols using esters; (9) coupling of alcohols with water to form carboxylic acids; and (10) dehydrogenation of beta-amino alcohols to form pyrazines. The present invention further relates to the novel uses of certain pyridine Ruthenium catalysts.

Подробнее
24-10-2013 дата публикации

Compounds for the treatment of metabolic disorders

Номер: US20130281705A1
Автор: Shalini Sharma
Принадлежит: Wellstat Therapeutics Corp

Compounds useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis, are disclosed.

Подробнее
31-10-2013 дата публикации

4-(p-QUINONYL)-2-HYDROXYBUTANAMIDE DERIVATIVES FOR TREATMENT OF MITOCHONDRIAL DISEASES

Номер: US20130289034A1
Принадлежит: Edison Phamaceuticals Inc

Methods of treating or suppressing mitochondrial diseases, such as Friedreich's ataxia (FRDA), Leber's Hereditary Optic Neuropathy (LHON), mitochondrial myopathy, encephalopathy, lactacidosis, and stroke (MELAS), Kearns-Sayre Syndrome (KSS), are disclosed, as well as compounds useful in the methods of the invention, such as 4-(p-quinolyl)-2-hydroxybutanamide derivatives. Methods and compounds useful in treating other disorders such as amyotrophic lateral sclerosis (ALS), Huntington's disease, Parkinson's disease, and pervasive developmental disorders such as autism are also disclosed. Energy biomarkers useful in assessing the metabolic state of a subject and the efficacy of treatment are also disclosed. Methods of modulating, normalizing, or enhancing energy biomarkers, as well as compounds useful for such methods, are also disclosed.

Подробнее
14-11-2013 дата публикации

Enzyme inhibitors

Номер: US20130303576A1
Принадлежит: Chroma Therapeutics Ltd

Compounds of formula (I), inhibit HDAC activity: wherein A, B and D independently represent ═CH— or ═N—; W is —CH═CH—Or —CH 2 CH 2 —; R 1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular carboxylesterase enzymes to a carboxylic acid group; R2 and R3 are selected from the side chains of a natural or non-natural alpha amino acid, provided that neither R 2 nor R 3 is hydrogen, or R 2 and R 3 , taken together with the carbon to which they are attached, form a 3-6 membered saturated cycloalkyl or heterocyclyl ring; Y is a bond, —C(═O)—, —S(═O) 2 —, —C(═O)O—, —C(═O)NR′—, —C(═S)—NR′, —C(═NH)NR′ or —S(═O) 2 NR— wherein R′ is hydrogen or optionally substituted C 1 -C 6 alkyl; L 1 is a divalent radical of formula -(Alk 1 ) m (Q) n (Alk 2 ) p - wherein m, n, p, Q. Alk 1 and Alk 2 are as defined in the claims; X 1 represents a bond; —C(═O); or —S(═O) 2 —; —NR 4 C(═O)—, —C(═O)NR 4 —, —NR 4 C(═O)NR 5 —, —NR 4 S(═O) 2 —, or —S(═O) 2 NR 4 — wherein R 4 and R 5 are independently hydrogen or optionally substituted C 1 -C 6 alkyl; and z is 0 or 1.

Подробнее
05-12-2013 дата публикации

Indanyloxyphenylcyclopropanecarboxylic acids

Номер: US20130324514A1
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

The present invention relates to compounds of general formula I, wherein the groups R 1 , R 2 , R 3 , m and n are defined as in claim 1 , which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2. Furthermore, the invention relates to novel intermediates, useful for the synthesis of compounds of formula I.

Подробнее
05-12-2013 дата публикации

Process for preparing styrene derivatives

Номер: US20130324745A1
Принадлежит: Saltigo GmbH

A process is provided which allows the synthesis of a large number of styrene derivatives with formation of C—C bonds, with use being possible of economically advantageous substrates, readily available carbon nucleophiles, and both inexpensive and environmentally unproblematic catalyst systems, permitting reaction under mild conditions and a high compatibility with functional groups on the reactants involved.

Подробнее
19-12-2013 дата публикации

Prostaglandin synthesis and intermediates for use therein

Номер: US20130338379A1
Принадлежит: Alphora Research Inc

Fused cyclopentane—4-substituted 3,5-dioxalane lactone compounds useful as an intermediate in the synthesis of prostaglandin analogs are provided. The compounds have the formula A: wherein R represents an aryl group such as p-methoxyphenyl. This compound can be reacted with a lower alkyl aluminum compound to open the dioxalane ring and reduce the lactone to lactol, without over-reducing to diol. The resulting compound can be functionalized to insert chemical side groups of target prostaglandins, adding the required α-side chain and then the required ω-side chain sequentially and independently of each other. The compounds and process are particularly suitable for preparing lubiprostone.

Подробнее
16-01-2014 дата публикации

Apparatus for generating 1-methylcyclopropene

Номер: US20140017134A1
Принадлежит: ERUM BIOTECHNOLOGIES Inc

Provided is an apparatus for generating 1-methylcyclopropene. The apparatus of the present invention may enable the immediate and convenient generation of 1-methylcyclopropene in a desired location using stable 1-methylcyclopropene precursors.

Подробнее
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.

Подробнее
23-01-2014 дата публикации

Compositions, synthesis, and methods of using phenylcycloalkylmethylamine derivatives

Номер: US20140024679A1
Принадлежит: Reviva Pharmaceuticals Inc

The present invention provides novel phenylcycloalkylmethylamine derivatives, and methods of preparing phenylcycloalkylmethylamine derivatives. The present invention also provides methods of using phenylcycloalkylmethylamine derivatives and compositions of phenylcycloalkylmethylamine derivatives. The pharmaceutical compositions of the compounds of the present invention can be used for treating and/or preventing obesity and obesity related co-morbid indications and depression and depression related co-morbid indications.

Подробнее
30-01-2014 дата публикации

Iminopropene compound and use thereof

Номер: US20140031376A1
Принадлежит: Sumitomo Chemical Co Ltd

The compound (I) or a salt thereof has an excellent controlling activity against pests. Then the compound (I) or a salt thereof is useful for an active ingredient of a pesticidal composition.

Подробнее
30-01-2014 дата публикации

Positive Allosteric Modulators of the Alpha 7 Nicotinic Acetylcholine Receptor and uses Thereof

Номер: US20140031395A1
Принадлежит: Bionomics Ltd

The present invention relates to compounds useful in the positive modulation of the alpha 7 nicotinic acetylcholine receptor (α7nAChR). The invention also relates to the use of these compounds in the treatment or prevention of a broad range of diseases in which the positive modulation of α7nAChR is advantageous, including neurodegenerative and neuropsychiatric diseases and also inflammatory diseases.

Подробнее
27-02-2014 дата публикации

Methods of inhibiting ethylene responses in plants using dicyclopropene compounds

Номер: US20140057788A1
Принадлежит: North Carolina State University

Methods of applying dicyclopropene compounds and compositions thereof to block ethylene receptors in plants are disclosed. Methods include applying to the plant an effective ethylene response-inhibiting amount of a dicyclopropene compound or composition thereof. Dicyclopropene compounds, enantiomers, stereoisomers or salts thereof are also provided.

Подробнее
06-03-2014 дата публикации

Compounds of liquid crystalline medium and use thereof for high-frequency components

Номер: US20140061536A1
Принадлежит: Merck Patent GmBH

The present invention relates to compounds of the formula I to the use thereof for high-frequency components, to liquid-crystalline media comprising the compounds, and to high-frequency components, in particular antennae, especially for the gigahertz range, comprising these media. The liquid-crystalline media serve, for example, for the phase shifting of microwaves for tuneable “phased-array” antennae.

Подробнее
03-04-2014 дата публикации

Process for producing ester compound

Номер: US20140094616A1
Принадлежит: Sumitomo Chemical Co Ltd

Compound (1) or a salt that is useful as an intermediate for the production of a medicine, an agrochemical or the like can be produced by a process including the following steps: (A) reacting an aldehyde (2) with nitromethane to produce a nitroaldehyde; (B) reacting the nitroaldehyde with an alcohol to produce a nitroacetal; (C) reducing the nitroacetal to produce an aminoacetal; (D) protecting an amino group in the aminoacetal to produce a protected aminoacetal; (E) treating the protected aminoacetal with an acid and subsequently with a base and then reacting the resultant product with a cyanating agent to produce a nitrile; (F) hydrolyzing the nitrile to produce a protected amino acid; and (G) substituting a group R 5 in the protected amino acid by a hydrogen atom and protecting a carboxyl group therein.

Подробнее
04-01-2018 дата публикации

USE OF PICOLINAMIDE COMPOUNDS WITH FUNGICIDAL ACTIVITY

Номер: US20180000084A1
Принадлежит:

This disclosure relates to picolinamides of Formula I and their use as fungicides. 2. A composition according to claim 1 , wherein X is hydrogen and Y is Q.3. A composition according to claim 2 , wherein Ris alkoxy.4. A composition according to claim 3 , wherein Ris hydrogen.5. A composition according to claim 4 , wherein Rand Rare independently chosen from hydrogen or alkyl claim 4 , optionally substituted with 0 claim 4 , 1 or multiple R.6. A composition according to claim 4 , wherein Rand Rare independently chosen from hydrogen or alkyl claim 4 , each optionally substituted with 0 claim 4 , 1 or multiple R.7. A composition according to claim 4 , wherein Ris aryl claim 4 , optionally substituted with 0 claim 4 , 1 or multiple R.8. A composition according to claim 4 , wherein Rand Rare independently chosen from hydrogen or alkyl claim 4 , optionally substituted with 0 claim 4 , 1 or multiple R claim 4 , Rand Rare independently chosen from hydrogen or alkyl claim 4 , each optionally substituted with 0 claim 4 , 1 or multiple R claim 4 , and Ris aryl claim 4 , optionally substituted with 0 claim 4 , 1 or multiple R.9. A composition according to claim 3 , wherein Ris chosen from —C(O)R claim 3 , or —CHOC(O)R.10. A composition according to claim 9 , wherein Rand Rare independently chosen from hydrogen or alkyl claim 9 , optionally substituted with 0 claim 9 , 1 or multiple R.11. A composition according to claim 9 , wherein Rand Rare independently chosen from hydrogen or alkyl claim 9 , each optionally substituted with 0 claim 9 , 1 or multiple R.12. A composition according to claim 9 , wherein Ris aryl claim 9 , optionally substituted with 0 claim 9 , 1 or multiple R.13. A composition according to claim 9 , wherein Rand Rare independently chosen from hydrogen or alkyl claim 9 , Rand Rare independently chosen from hydrogen or alkyl claim 9 , each optionally substituted with 0 claim 9 , 1 or multiple R claim 9 , and Ris aryl claim 9 , optionally substituted with 0 claim ...

Подробнее
04-01-2018 дата публикации

Molecules having pesticidal utility, and intermediates, compositions, and processes, related thereto

Номер: US20180000087A1
Принадлежит: DOW AGROSCIENCES LLC

This disclosure relates to the field of molecules having pesticidal utility against pests in Phyla Arthropoda, Mollusca, and Nematoda, processes to produce such molecules, intermediates used in such processes, pesticidal compositions containing such molecules, and processes of using such pesticidal compositions against such pests. These pesticidal compositions may be used, for example, as acaricides, insecticides, miticides, molluscicides, and nematicides. This document discloses molecules having the following formula (“Formula One”). 2. A molecule according to claim 1 , wherein Ris selected from the group consisting of H and Cl.3. A molecule according to claim 1 , wherein Ris selected from the group consisting of H claim 1 , Cl claim 1 , Br claim 1 , CH claim 1 , and CF.4. A molecule according to claim 1 , wherein Ris selected from the group consisting of H claim 1 , F claim 1 , Cl claim 1 , CH claim 1 , CF claim 1 , and OCF.5. A molecule according to claim 1 , wherein Ris selected from the group consisting of H claim 1 , F claim 1 , Cl claim 1 , Br claim 1 , CH claim 1 , and CF.6. A molecule according to claim 1 , wherein R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , and Rare H.7. A molecule according to claim 1 , wherein Ris Cl.8. A molecule according to claim 1 , wherein Ris Cl.9. A molecule according to claim 1 , wherein Ris selected from the group consisting of H claim 1 , Cl claim 1 , and CF.10. A molecule according to claim 1 , wherein Ris selected from the group consisting of H and CH.11. A molecule according to claim 1 , wherein Ris selected from the group consisting of cyclopropyl claim 1 , cyclobutyl claim 1 , cyclopentyl claim 1 , cyclohexyl claim 1 , azetidinyl claim 1 , morpholinyl claim 1 , oxetanyl claim 1 , pyranyl claim 1 , tetrahydrothiophenyl claim 1 , thietanyl claim 1 , thietanyl-oxide claim 1 , and thietanyl-dioxide claim 1 ,{'sub': 3', '3', '3, 'wherein each cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, ...

Подробнее
04-01-2018 дата публикации

METHODS FOR INHIBITING CONVERSION OF CHOLINE TO TRIMETHYLAMINE (TMA)

Номер: US20180000754A1
Принадлежит:

A method of inhibiting the conversion of choline to trimethylamine (TMA) and lowering TMAO by providing a composition comprising a compound set forth in Formula (I): 2. The composition of wherein the compound is selected from the group consisting of: 2-(methoxycarbonyl)-N claim 1 ,N-dimethyl-N-(prop-2-yn-1-yl)prop-2-en-1-aminium bromide claim 1 , 2-carboxy-N claim 1 ,N-dimethyl-N-(prop-2-yn-1-yl)prop-2-en-1-aminium bromide claim 1 , 2-cyano-N-(2-hydroxyethyl)-N claim 1 ,N-dimethylprop-2-en-1-aminium bromide claim 1 , 2-cyano-N claim 1 ,N-dimethyl-N-(prop-2-yn-1-yl)prop-2-en-1-aminium bromide claim 1 , or N-(3-methoxy-2 claim 1 ,3-dioxopropyl)-N claim 1 ,N-dimethylprop-2-yn-1-aminium bromide.3. The composition of wherein{'sub': '12', 'Ris acrylic, acetal, alkoxy, amido, amino, carboxylic, carboxylate, or glyoxyl,'}{'sub': 13', '14', '1', '4, 'Rand Rare independently selected from C-Calkyl; and'}{'sub': '15', 'Ris propargyl'}6. The method of wherein the compound is selected from the group consisting of: 2-(methoxycarbonyl)-N claim 4 ,N-dimethyl-N-(prop-2-yn-1-yl)prop-2-en-1-aminium claim 4 , 4-carboxy-N claim 4 ,N-dimethyl-N-(prop-2-yn-1-yl)butan-1-aminium claim 4 , N-(2 claim 4 ,2-dimethoxyethyl)-N claim 4 ,N-dimethylprop-2-yn-1-aminium claim 4 , N-(2 claim 4 ,2-dihydroxyethyl)-N claim 4 ,N-dimethylprop-2-yn-1-aminium claim 4 , N-(2-hydroxyethyl)-N claim 4 ,N-dimethylbut-3-yn-1-aminium claim 4 , N-(2 claim 4 ,2-diethoxyethyl)-N claim 4 ,N-dimethylprop-2-yn-1-aminium claim 4 , 4-hydroxy-1-methyl-1-(prop-2-yn-1-yl)piperidin-1-ium claim 4 , 2-cyano-N claim 4 ,N-dimethyl-N-(prop-2-yn-1-yl)prop-2-en-1-aminium claim 4 , N-(carboxymethyl)-N claim 4 ,N-dimethylprop-2-yn-1-aminium claim 4 , trimethyl(prop-2-ynyl)ammonium claim 4 , allyl-(cyanomethyl)-dimethyl-ammonium claim 4 , or N-(2-hydroxyethyl)-N claim 4 ,N-dimethylprop-2-yn-1-aminium and a pharmaceutically acceptable salt thereof.9. The method of further comprising administering to the individual a second agent selected ...

Подробнее
04-01-2018 дата публикации

CYCLOPROPYLAMINES AS LSD1 INHIBITORS

Номер: US20180000805A1
Принадлежит:

This invention relates to the use of cyclopropylamine derivatives for the modulation, notably the inhibition of the activity of Lysine-specific demethylase 1 (LSD1). Suitably, the present invention relates to the use of cyclopropylamines in the treatment of cancer. 2. The method of wherein said hematologic cancer is myelodysplastic syndrome.3. The method of claim 1 , further comprising administering an additional therapeutic agent selected from the group consisting of tretinoin claim 1 , azacitidine claim 1 , and decitabine.4. The method of claim 3 , wherein said additional therapeutic agent is tretinoin.5. The method of claim 3 , wherein said additional therapeutic agent is azacitidine.6. The method of claim 3 , wherein said additional therapeutic agent is decitabine.7. The method of claim 3 , wherein said hematologic cancer is myelodysplastic syndrome.8. The method of claim 4 , wherein said hematologic cancer is myelodysplastic syndrome.9. The method of claim 5 , wherein said hematologic cancer is myelodysplastic syndrome.10. The method of claim 6 , wherein said hematologic cancer is myelodysplastic syndrome.11. The method of claim 3 , wherein said hematologic cancer is acute myeloid leukemia.12. The method of claim 4 , wherein said hematologic cancer is acute myeloid leukemia.13. The method of claim 5 , wherein said hematologic cancer is acute myeloid leukemia.14. The method of claim 6 , wherein said hematologic cancer is acute myeloid leukemia. This invention relates to novel cyclopropylamines which are inhibitors of Lysine-specific demethylase 1 (LSD1; also known as BHC110), to pharmaceutical compositions containing them, and to their use in therapy for the treatment of cancers.Chromatin modification plays an essential role in transcriptional regulation (T. Kouzarides, 2007128: 693-705). These modifications, which include DNA methylation, histone acetylation and histone methylation, are disregulated in tumors. This epigenetic disregulation plays an important ...

Подробнее
04-01-2018 дата публикации

Enzyme and receptor modulation

Номер: US20180000952A1

Covalent conjugation of an alpha amino acid ester to a modulator of the activity of a target intracellular enzyme or receptor, wherein the ester group of the conjugate is hydrolysable by one or more intracellular carboxylesterase enzymes to the corresponding acid, leads to accumulation of the carboxylic acid hydrolysis product in the cell and enables improved or more prolonged enzyme or receptor modulation relative to the unconjugated modulator.

Подробнее
04-01-2018 дата публикации

Hypdh inhibitors and methods of use for the treatment of kidney stones

Номер: US20180002275A1

Provided herein are compounds of Formula (I), Formula (II), and Formula (III), and compositions comprising the same, as well as methods of use thereof for controlling or inhibiting the formation of calcium oxalate kidney stones, inhibiting the production of glyoxylate and/or oxalate, and/or inhibiting hydroxyproline dehydrogenase (HYPDH).

Подробнее
03-01-2019 дата публикации

CYCLOBUTANE-1, 3-DIACID BUILDING BLOCKS

Номер: US20190002387A1
Автор: Chu Qianli, Wang Zhihan
Принадлежит:

A method of making polymers utilizes cyclobutane-1,3-diacid (CBDA) molecules as polymer building blocks includes and linker molecules with a non-reactive R group and at least two reactive X groups used to create chemically stable polymers of CBDA. The resulting polymers are thermally, photochemically, and chemically stable. 1. A method of making a polyester comprises:providing a plurality of cyclobutane-1,3-diacid molecules; andpolymerizing the plurality of cyclobutane-1,3-diacid molecules together with a plurality of linker molecules to create a polymer, each of the plurality of linker molecules comprising an R group and at least two X groups, wherein the R group does not react with the cyclobutane-1,3-diacid molecules, and wherein the X groups do react with the cyclobbutane-1,3-diacid molecules.2. The method of claim 1 , wherein the X groups react with a carboxylic acid of the cyclobutane-1 claim 1 ,3-diacid molecule.3. The method of claim 1 , wherein each of the plurality of linker molecules comprises at least two X groups.4. The method of claim 1 , wherein the X groups are selected from the group consisting of nitrogen containing functional groups claim 1 , oxygen containing functional groups claim 1 , halogens claim 1 , carbon containing functional groups claim 1 , sulfur containing functional groups claim 1 , boron containing functional groups claim 1 , phosphorus containing functional groups claim 1 , metals claim 1 , metal cations claim 1 , and combinations thereof5. The method of claim 1 , wherein the R group is selected from the group consisting of an aliphatic chain claim 1 , an aliphatic heterochain claim 1 , a branched aliphatic chain claim 1 , an aliphatic ring claim 1 , an aromatic ring claim 1 , a heterocyclic ring claim 1 , and combinations thereof6. The method of claim 1 , wherein polymerizing the plurality of cyclobutane-1 claim 1 ,3-diacid molecule together comprises: forming a series of alcohols through condensation reactions claim 1 , each of ...

Подробнее
03-01-2019 дата публикации

IDO INHIBITORS

Номер: US20190002402A1
Принадлежит:

There are disclosed compounds that modulate or inhibit the enzymatic activity of indoleamine 2,3-dioxygenase (IDO), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders, such as cancer, viral infections and/or inflammatory disorders utilizing the compounds of the invention. 2. The compound according to wherein Rand Rare independently H claim 1 , Cto Calkyl claim 1 , Cto Calkoxy claim 1 , or join together to form cyclopropyl or cyclobutyl.3. The compound according to wherein Z is —NH— and Ris —SOR claim 1 , halo (C-Calkyl) claim 1 , thiazolyl or oxazolyl claim 1 , wherein Ris Cto Calkyl claim 1 , Cto Ccycloalkyl4. The compound according to wherein Z is O and Ris H.5. The compound according to wherein Ris —COR.6. The compound according to wherein Ris a 5 membered heterocycle containing from 1 to 4 heteroatoms selected from N claim 1 , O claim 1 , and S.7. The compound according to wherein Ris H and Ris —CORor —CONRR; Ris H claim 1 , and Ris phenyl claim 1 , pyridyl claim 1 , isoxazolyl claim 1 , thiadiazolyl claim 1 , indolinyl claim 1 , or benzyl claim 1 , wherein Rmay optionally be substituted with from 1 to 3 substituents selected from the group consisting of halo claim 1 , amino claim 1 , phenoxy claim 1 , benzoxy claim 1 , isoxalyl claim 1 , Cto Calkoxy claim 1 , Cto Calkyl claim 1 , halo-Cto Calkyl claim 1 , and CN.8. The compound according to wherein Ris Cto Ccycloalkyl optionally substituted with halo claim 1 , —OH or Cto Calkoxy; Cto Calkyl optionally substituted with halo claim 1 , —OH or phenyl claim 1 , wherein said phenyl is optionally substituted with Cto Chaloalkyl claim 1 , Cto Calkoxy claim 1 , halo or Cto Calkyl; Cto Calkenyl; Cto Calkoxy; or benzyl optionally substituted with Cto Calkyl claim 1 , halo claim 1 , Cto Calkoxy claim 1 , or haloalkyl.9. The compound according to wherein Ris a Cto Cheterocycloalkyl containing from 1 to 4 heteroatoms selected from O claim 1 , N or S.10. The compound ...

Подробнее
03-01-2019 дата публикации

PREPARATION OF LATANOPROSTENE BUNOD OF DESIRED, PRE-DEFINED QUALITY BY GRAVITY CHROMATOGRAPHY

Номер: US20190002405A1

The subject of the invention is a process for the preparation of Latanoprostene bunod of formula (I) with a purity higher than 95% where chromatography is used applying normal phase gravity silica gel column chromatography where the used silica gel is irregular silica gel or spherical silica gel an as eluent and eluent mixture consisting of an apolar and a polar solvent is used and if desired, contamination of the purified compound of formula I arising from the solvents are removed by silica gel filtration chromatography. 2. Process a.) or b.) as defined in claim 1 , characterized in that claim 1 , the eluent mixture contains as apolar solvent straight- or branched-chain aliphatic claim 1 , cyclic or aromatic hydrocarbons claim 1 , halogenated aliphatic hydrocarbons or ether-type solvents.3. Process as defined in claim 2 , characterized in that claim 2 , as apolar solvent pentane claim 2 , hexane claim 2 , heptane claim 2 , cyclohexane claim 2 , dichloromethane or diisopropyl ether claim 2 , preferably hexane is applied.4. Process a.) or b.) as defined in claim 1 , characterized in that claim 1 , as polar solvent an alcohol- claim 1 , ester- or ketone-type solvent containing straight- or branched-chain alkyl group is applied.5. Process as defined in claim 4 , characterized in that claim 4 , as polar solvent a C1-5 alcohol claim 4 , preferably ethyl alcohol or isopropyl alcohol is applied.6. Process as defined in claim 3 , characterized in that claim 3 , the eluent mixture is a gradient mixture containing hexane and ethyl alcohol in 6:1-8:1 volume ratios.7. Process as defined in claim 4 , characterized in that claim 4 , as polar solvent a ketone-type solvent claim 4 , preferably acetone is applied.8. Process as defined in claim 3 , characterized in that claim 3 , the eluent mixture contains hexane and acetone in 2:1 volume ratio.9. Filtration chromatography process as defined in claim 1 , characterized in that claim 1 , the eluent mixture contains an apolar and a ...

Подробнее
02-01-2020 дата публикации

DUAL MECHANISM INHIBITORS FOR THE TREATMENT OF DISEASE

Номер: US20200002324A1
Принадлежит:

Provided are compounds that are inhibitors of both rho kinase and of a monoamine transporter (MAT) act to improve the disease state or condition. Further provided are compositions comprising the compounds. Further provided are methods for treating diseases or conditions, the methods comprising administering compounds according to the invention. One such disease may be glaucoma for which, among other beneficial effects, a marked reduction in intraocular pressure (IOP) may be achieved. 121-. (canceled)23. A composition claim 22 , comprising the compound of .24. A pharmaceutical composition claim 22 , comprising the compound of and a pharmaceutically acceptable carrier.25. The pharmaceutical composition of claim 24 , wherein the pharmaceutically acceptable carrier is saline buffered to a pH of about 5.5 to about 6.5.26. A method of treating an eye disease in a subject in need thereof claim 22 , comprising administering to the subject an effective amount of the compound of .27. The method of claim 26 , wherein the eye disease comprises glaucoma.28. The method of claim 26 , wherein the eye disease comprises wet age-related macular degeneration claim 26 , dry age-related macular degeneration claim 26 , or diabetic macular edema.29. The method of claim 26 , wherein the eye disease comprises dry eye.30. The method of claim 26 , wherein the eye disease comprises ocular hypertension.31. The method of claim 26 , wherein the administration is topical administration to an eye of the subject.32. A method of treating an eye disease in a subject in need thereof claim 23 , comprising administering to the subject an effective amount of the composition of .33. The method of claim 32 , wherein the eye disease comprises glaucoma.34. The method of claim 32 , wherein the eye disease comprises wet age-related macular degeneration claim 32 , dry age-related macular degeneration claim 32 , or diabetic macular edema.35. The method of claim 32 , wherein the eye disease comprises dry eye.36. ...

Подробнее
04-01-2018 дата публикации

Processes for the preparation of a diarylthiohydantoin compound

Номер: US20180002309A1
Принадлежит: Aragon Pharmaceuticals Inc

Disclosed are processes and intermediates for the preparation of compound (X), which is currently being investigated for the treatment of prostate cancer.

Подробнее
07-01-2021 дата публикации

Metabolites of N-(4-{[6,7-Bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide

Номер: US20210002228A1
Принадлежит:

The invention relates to metabolites of cabozantinib (I) as well as uses thereof. 1. An isolated metabolite of cabozantinib or a pharmaceutically acceptable salt thereof.12. A method of treating a disease treating diseases or disorders associated with uncontrolled , abnormal , and/or unwanted cellular activities , the method comprising administering , to a mammal in need thereof , a therapeutically effective amount of a compound of - , or a pharmaceutically acceptable salt thereof.14. The composition of claim of claim 13 , which is suitable for oral administration.19. The method according to claim 17 , wherein the bodily fluids are selected from the group consisting of plasma claim 17 , bile claim 17 , urine claim 17 , and feces. This application claims priority to U.S. Ser. No. 61/792,413, filed Mar. 15, 2013. The entire contents of the aforementioned application are incorporated herein.This disclosure relates to metabolites of N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy})phenyl)-N′-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide, a c-Met inhibitor.Traditionally, dramatic improvements in the treatment of cancer are associated with identification of therapeutic agents acting through novel mechanisms. One mechanism that can be exploited in cancer treatment is the modulation of protein kinase activity because signal transduction through protein kinase activation is responsible for many of the characteristics of tumor cells. Protein kinase signal transduction is of particular relevance in, for example, thyroid, gastric, head and neck, lung, breast, prostate, and colorectal cancers, as well as in the growth and proliferation of brain tumor cells.Protein kinases can be categorized as receptor type or non-receptor type. Receptor-type tyrosine kinases are comprised of a large number of transmembrane receptors with diverse biological activity. For a detailed discussion of the receptor-type tyrosine kinases, see Plowman et al., DN&P 7(6): 334-339, 1994. Since protein kinases ...

Подробнее
07-01-2021 дата публикации

ARYL CYCLOPROPYL-AMINO-ISOQUINOLINYL AMIDE COMPOUNDS

Номер: US20210002253A1
Принадлежит:

Provided herein are arylcyclopropyl amino-isoquinoline amide compounds. In particular, the disclosure provides compounds that affect the function of kinases in a cell and that are useful as therapeutic agents or with therapeutic agents. The compounds of the disclosure are useful in the treatment of a variety of diseases and conditions including eye diseases such as glaucoma, cardiovascular diseases, diseases characterized by abnormal growth, such as cancers, and inflammatory diseases. The disclosure further provides compositions containing isoquinoline amide compounds. 2. (canceled)3. (canceled)666-. (canceled)6984-. (canceled)85. The compound of claim 67 , wherein Ris H or —Calkyl.86. (canceled)87. (canceled)88. The compound of claim 67 , wherein Ris phenyl claim 67 , pyridinyl claim 67 , —(Calkyl)-pyridinyl claim 67 , —(Calkyl)-N(R)R claim 67 , —(Calkyl)-heterocyclyl or heterocycloalkyl.8994-. (canceled)95. The compound of claim 67 , wherein Ris 2-pyridinyl claim 67 , 3-pyridinyl claim 67 , or 4-pyridinyl.96. The compound of claim 67 , wherein Rand R claim 67 , together with the nitrogen to which they are attached claim 67 , form a heterocyclyl containing six ring atoms.97. The compound of claim 67 , wherein Rand R claim 67 , together with the nitrogen to which they are attached claim 67 , form a heterocyclyl containing six ring atoms claim 67 , wherein one or two of the ring atoms are claim 67 , independently claim 67 , O claim 67 , S or N.98. The compound of claim 67 , wherein Rand R claim 67 , together with the nitrogen to which they are attached claim 67 , form a heterocyclyl containing six ring atoms claim 67 , wherein one or two of the ring atoms are N.99. The compound of claim 67 , wherein Rand Rare H claim 67 , or Rand Rare claim 67 , independently claim 67 , Calkyl.100102-. (canceled)103. The compound of claim 67 , wherein:{'sub': '1-6', 'X is Calkyl, halogen or hydroxyl; and'}Y and Z are H.104. (canceled)105. The compound of claim 67 , wherein X is ...

Подробнее
13-01-2022 дата публикации

MANUFACTURE OF CAROTENOID COMPOSITIONS

Номер: US20220009886A1
Автор: Mehta Sevanti
Принадлежит: Unibar Corporation

A extract composition (600) includes capsanthin in the range from 50% to 80%, zeaxanthin in the range from 5% to 15%, and cryptoxanthin the range from 1% to 5%. 1600Capsicum annum. A extract composition () comprising:capsanthin in the range from 50% to 80%;zeaxanthin in the range from 5% to 15%; andcryptoxanthin in the range from 1% to 5%.2. The composition of claim 1 , wherein the capsanthin comprises trans-capsanthin (3R claim 1 ,3″S claim 1 ,5′R)-3 claim 1 ,3′-Dihydroxy-β claim 1 ,κ-caroten-6′-one) claim 1 , the zeaxanthin comprises trans-zeaxanthin (3R claim 1 , 3′R-β claim 1 ,β-carotene-3 claim 1 ,3′-diol) claim 1 , and the cryptoxanthin comprises beta-cryptoxanthin (3R claim 1 ,6′R)-4′ claim 1 ,5′-Didehydro-5′ claim 1 ,6′-dihydro-β claim 1 ,β-caroten-3-ol.3. The composition of claim 1 , wherein the color value of carotenoids ranges from 800 claim 1 ,000 to 1 claim 1 ,250 claim 1 ,000.4. The composition of claim 1 , wherein the composition aids in the management of age related macular degeneration conditions selected from the group consisting of: blurred vision claim 1 , distorted vision claim 1 , reduced central vision claim 1 , and difficulty in adopting low light levels.5. The composition of claim 1 , wherein the composition protects against blue light induced retinopathy by decreasing oxidative and endoplasmic reticulum stress.6. The composition of claim 1 , wherein the composition provides functional and morphological preservation of photoreceptors against blue light damage.7. The composition of claim 1 , wherein the composition lowers intraocular pressure.8. The composition of claim 1 , wherein the composition provides color for a cosmetic selected from the group consisting of: lipstick claim 1 , chap-stick claim 1 , liquid gloss claim 1 , lipstick paste claim 1 , blush claim 1 , lip liner claim 1 , foundation claim 1 , concealer claim 1 , eye contourer claim 1 , eyeliner claim 1 , mascara claim 1 , nail polish claim 1 , eye shadow claim 1 , and body make ...

Подробнее
01-01-2015 дата публикации

Branched Alkyl And Cycloalkyl Terminated Biodegradable Lipids For The Delivery Of Active Agents

Номер: US20150005363A1
Автор: Steven M Ansell, Xinyao Du
Принадлежит: Alnylam Pharmaceuticals Inc

The present invention relates to a cationic lipid of formula (I) having one or more biodegradable groups located in a lipidic moiety (e.g., a hydrophobic chain) of the cationic lipid. These cationic lipids may be incorporated into a lipid particle for delivering an active agent, such as a nucleic acid. The invention also relates to lipid particles comprising a neutral lipid, a lipid capable of reducing aggregation, a cationic lipid of the present invention, and optionally, a sterol. The lipid particle may further include a therapeutic agent such as a nucleic acid.

Подробнее
01-01-2015 дата публикации

Ester derivatives of bimatoprost compositions and methods

Номер: US20150005377A1
Принадлежит: Allergan Inc

Provided herein, inter alia, are prodrugs of bimatoprost, methods of using the same and compositions including the same.

Подробнее
03-01-2019 дата публикации

FUNCTIONAL ORGANIC SALT FOR LITHIUM-ION BATTERIES

Номер: US20190006712A1
Принадлежит: UCHICAGO ARGONNE, LLC

An electrolyte for a lithium-ion electrochemical cell comprises a non-aqueous solution of a lithium salt and a redox shuttle salt compound in a non-aqueous solvent, wherein the redox shuttle compound comprises an amino-substituted cyclopropenium salt of Formula (I) as described herein. 2. The electrolyte of claim 1 , wherein R and R′ independently are Cto Calkyl.3. The electrolyte of claim 1 , wherein R and R′ are ethyl.4. The electrolyte of claim 1 , wherein X is a halide.5. The electrolyte of claim 1 , wherein X is chloride.6. The electrolyte of claim 1 , wherein X is a sulfonimidate anion.8. The electrolyte of claim 1 , wherein X is bis(trifluoromethanesulfonyl)imidate anion.11. The electrolyte of claim 1 , wherein the lithium salt comprises one or more of lithium bis(trifluoromethanesulfonyl)imidate (LiTFSI) claim 1 , lithium 2-trifluoromethyl-4 claim 1 ,5-dicyanoimidazolate (LiTDI) claim 1 , lithium 4 claim 1 ,5-dicyano-1 claim 1 ,2 claim 1 ,3-triazolate (LiTDI) claim 1 , lithium trifluoromethanesulfonate (LiTf) claim 1 , lithium perchlorate (LiClO) claim 1 , lithium bis(oxalato)borate (LiBOB) claim 1 , lithium difluoro(oxalato)borate (LiDFOB) claim 1 , lithium tetrafluoroborate (LiBF) claim 1 , lithium hexafluorophosphate (LiPF) claim 1 , lithium thiocyanate (LiSCN) claim 1 , lithium bis(fluorosulfonyl)imidate (LIFSI) claim 1 , lithium bis(pentafluoroethylsulfonyl)imidate (LBETI) claim 1 , lithium tetracyanoborate (LiB(CN)) claim 1 , and lithium nitrate.12. The electrolyte of claim 1 , wherein the lithium salt is present in the electrolyte at a concentration in the range of about 0.1 M to about 3 M.13. The electrolyte of claim 1 , wherein the compound of Formula (I) is present in the electrolyte at a concentration in the range of about 0.005 M to about 0.5 M.14. The electrolyte of claim 1 , wherein the non-aqueous solvent comprises one or more of an ether claim 1 , a carbonate ester claim 1 , a nitrile claim 1 , a sulfoxide claim 1 , a sulfone claim 1 , a ...

Подробнее
14-01-2016 дата публикации

3'-substituted-abscisic acid derivatives

Номер: US20160007598A1
Принадлежит: Valent BioSciences LLC

The invention relates to a novel class of (S)-3′-substituted-abscisic acid derivatives and (±)-3′-substituted-abscisic acid derivatives, and methods of synthesizing the derivatives.

Подробнее
11-01-2018 дата публикации

Molecules having pesticidal utility, and intermediates, compositions, and processes, related thereto

Номер: US20180007911A1
Принадлежит: DOW AGROSCIENCES LLC

This disclosure relates to the field of molecules having pesticidal utility against pests in Phyla Arthropoda, Mollusca, and Nematoda, processes to produce such molecules, intermediates used in such processes, pesticidal compositions containing such molecules, and processes of using such pesticidal compositions against such pests. These pesticidal compositions may be used, for example, as acaricides, insecticides, miticides, molluscicides, and nematicides. This document discloses molecules having the following formula (“Formula One”). 2. A molecule according to claim 1 , wherein Ris selected from the group consisting of H claim 1 , F claim 1 , and Cl.3. A molecule according to claim 1 , wherein Ris selected from the group consisting of H claim 1 , F claim 1 , and Cl.4. A molecule according to claim 1 , wherein Ris F or Cl.5. A molecule according to claim 1 , wherein R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , and Rare each independently H.6. A molecule according to claim 1 , wherein Ris selected from the group consisting of Cl and Br.7. A molecule according to claim 1 , wherein Ris selected from the group consisting of Cl and Br.8. A molecule according to claim 1 , wherein Ris selected from the group consisting of H claim 1 , Cl claim 1 , and CF.9. A molecule according to claim 1 , wherein Ris selected from the group consisting of H and CH.10. A molecule according to claim 1 , wherein Ris selected from the group consisting of CH claim 1 , CHCH claim 1 , CHCHCH claim 1 , CHCHCHCH claim 1 , CHCHCHOCHCH claim 1 , CH claim 1 , CHCH claim 1 , CHCHCH claim 1 , CHCHCHCH claim 1 , CHCHCHCHCH claim 1 , CHCHCHCHCHCH claim 1 , CHCH(CH) claim 1 , CHcyclopropyl claim 1 , CHCHcyclopropyl claim 1 , CHcyclobutyl claim 1 , CHphenyl claim 1 , CHCHphenyl claim 1 , CHC═CH claim 1 , CHC═CH claim 1 , CHCF claim 1 , CHCHF claim 1 , CHCHCF claim 1 , CHCFCF claim 1 , CHCHCHCF claim 1 , CHCHCFCF claim 1 , CHCFCFCF claim 1 , CHCHCHCHF claim 1 , CHCHSCH ...

Подробнее
14-01-2021 дата публикации

ESTROGEN RECEPTOR LIGAND TREATMENT FOR NEURODEGENERATIVE DISEASES

Номер: US20210008002A1
Автор: Voskuhl Rhonda R.
Принадлежит:

The present invention relates to treatment of neurological diseases such as multiple sclerosis (MS) and Alzheimer's disease, using an estrogen receptor beta (ERβ) ligand. 185-. (canceled)86. A method of:i) slowing, reversing or halting progression of disability in a subject suffering from a neurodegenerative disease;ii) slowing or halting the progression of memory loss in a subject suffering from a neurodegenerative disease; oriii) slowing or halting the progression of a learning disability in a subject suffering from a neurodegenerative disease; whereinthe method comprises administering an estrogen receptor beta ligand to the subject.87. The method of claim 86 , wherein the method is a method of slowing claim 86 , reversing or halting progression of disability in a subject suffering from a neurodegenerative disease.88. The method of claim 86 , wherein the method is a method of slowing or halting the progression of memory loss in a subject suffering from a neurodegenerative disease.89. The method of claim 86 , wherein the method is a method of slowing or halting the progression of a learning disability in a subject suffering from a neurodegenerative disease.90. The method of claim 86 , wherein the subject has brain gray matter loss.91. The method of claim 90 , wherein the subject has greater than about 0.1% brain gray matter loss per annum.92. The method of claim 90 , wherein the brain gray matter loss per annum is about 0.2% claim 90 , or about 0.3% claim 90 , or about 0.4% claim 90 , or about 0.5% claim 90 , or about 0.6% claim 90 , or about 0.7% claim 90 , or about 0.8% claim 90 , or about 0.9% claim 90 , or about 1.0% claim 90 , or about 1.1% claim 90 , or about 1.2% claim 90 , or about 1.3% claim 90 , or about 1.4% claim 90 , or about 1.5% claim 90 , or about 2.0%.93. The method of claim 90 , wherein the gray matter loss is located in one or more of the total brain claim 90 , cerebral cortex claim 90 , cerebellum claim 90 , thalamus claim 90 , caudate nucleus ...

Подробнее
12-01-2017 дата публикации

Monomer, polymer, positive resist composition, and patterning process

Номер: US20170008982A1
Принадлежит: Shin Etsu Chemical Co Ltd

A polymer comprising recurring units derived from a polymerizable monomer having two structures of hydroxyphenyl methacrylate having a hydroxy group substituted with an acid labile group is used as base resin in a positive resist composition, especially chemically amplified positive resist composition. The resist composition forms a resist film which is processed by lithography into a pattern of good profile having a high resolution, minimal edge roughness, and etch resistance.

Подробнее
10-01-2019 дата публикации

Bis-amines, Compositions, and Uses Related to CXCR4 Inhibition

Номер: US20190008840A1

This disclosure relates bis-amine compounds disclosed herein and uses related to CXCR4 inhibition. In certain embodiments, the compounds have formula (I), salts, derivatives, and prodrugs thereof wherein, A is a bridging aryl or heterocyclyl and R1 and R2 are further disclosed herein. In certain embodiments, the disclosure contemplates pharmaceutical compositions comprising compounds disclosed herein. In certain embodiments, the disclosure relates to methods of treating or preventing CXCR4 related diseases or conditions by administering an effective amount of a compound disclosed herein to a subject in need thereof.

Подробнее
14-01-2016 дата публикации

Tricyclic compound and use thereof

Номер: US20160009677A1
Принадлежит: SK Chemicals Co Ltd

The present invention relates to: a compound selected from the group consisting of a tricyclic compound having the structure of formula I, a pharmaceutically acceptable salt, an isomer, a solvate and a precursor thereof; and a use thereof. The compound effectively controls GPR40, and thus, can be effectively used for the prophylaxis or treatment of diseases associated with GPR40, for example, diabetes and many other diseases.

Подробнее
09-01-2020 дата публикации

NOVEL IMAGING COMPOSITION AND USES THEREOF

Номер: US20200009090A1
Принадлежит:

The invention discussed in this application relates to hydroxamic acid-based compounds that are useful as imaging agents when bound to an appropriate metal centre, particularly for the imaging of tumours. 2. The conjugate of claim 1 , wherein L is OR.3. The conjugate of claim 2 , wherein R is Cto Calkyl.4. The conjugate of claim 2 , wherein OR is selected from O-p-toluenesulfonate claim 2 , O-methanesulfonate claim 2 , O-trifluoromethanesulfonate claim 2 , O-benzenesulfonate claim 2 , and O-m-nitrobenzenesulfonate.5. The conjugate of claim 1 , wherein the target molecule is a polypeptide.6. The conjugate of claim 5 , wherein the polypeptide is an antibody.7. The conjugate of claim 6 , wherein the antibody is selected from trastuzumab claim 6 , rituximab and cetuximab.8. The conjugate of claim 1 , wherein the target molecule is a peptide.9. The conjugate of claim 8 , wherein the peptide is a targeting peptide.10. The conjugate of claim 9 , wherein the targeting peptide is selected from a cyclic RGD sequence claim 9 , bombesin and glu-N(CO)N-lys PSMA. This application is a Continuation of U.S. patent application Ser. No. 15/963,599, filed Apr. 26, 2018, which is a Continuation of U.S. patent application Ser. No. 15/518,333, filed Apr. 11, 2017, now U.S. Pat. No. 9,980,930, issued on May 29, 2018 and is a National Stage Application, filed under 35 U.S.C. 371, of International Application No. PCT/AU2015/050640, filed on Oct. 16, 2015, which claims priority to, and the benefit of, AU Application No. 2014904138, filed Oct. 16, 2014. The contents of each of these applications are incorporated by reference in their entirety.The present invention relates to hydroxamic acid-based compounds that are useful as imaging agents when bound to an appropriate metal centre, particularly for the imaging of tumours. The present invention also relates to compositions including the compounds, and to methods of imaging patients using the compounds.Zirconium-89 (Zr) is a positron-emitting ...

Подробнее
27-01-2022 дата публикации

Process for the preparation of latanoprostene bunod and intermediate thereof and compositions comprising the same

Номер: US20220024849A1
Принадлежит: Chirogate International Inc

Processes for preparing latanoprostene bunod and an intermediate prepared from the process. Also latanoprostene bunod compositions having high-purity latanoprostene bunod.

Подробнее
11-01-2018 дата публикации

HYDROSILANE/LEWIS ACID ADDUCT, PARTICULARLY ALUMINUM, IRON, AND ZINC, METHOD FOR PREPARING SAME, AND USE OF SAID SAME IN REACTIONS FOR REDUCING CARBONYL DERIVATIVES

Номер: US20180009730A1
Принадлежит:

Disclosed is an adduct between a Lewis acid, preferably aluminum trichloride, iron trichloride, or zinc dichloride, and a hydrosilane;—a method for preparing same; and a method for for reducing, particularly, an aldehyde, a ketone, an α,β-unsaturated ketone, an imine, or an α,β-unsaturated imine. 1. A pre-formed adduct between a Lewis acid selected from the salts of zinc (II) , tin (II) or (IV) , iron (II) or iron (III) , copper (I) , palladium (II) , titanium (III) or (IV) , bismuth (III) or aluminium (III) and a hydrosilane.2. An adduct according to claim 1 , wherein the Lewis acid is a salt of zinc (II) claim 1 , especially zinc dichloride claim 1 , a salt of iron (III) claim 1 , especially iron trichloride claim 1 , or a salt of aluminium (III) claim 1 , especially aluminium trichloride.3. An adduct according to claim 1 , wherein the hydrosilane is selected from the trialkylsilanes claim 1 , such as triethylsilane (EtSiH) and tri(isopropyl)silane claim 1 , tris(trimethylsilyl)silane claim 1 , triphenylsilane claim 1 , the polymethylhydrosiloxanes (PMHS) claim 1 , the polydimethylsiloxanes having a terminal Si—H group claim 1 , such as tetramethyldisiloxane claim 1 , the methylhydro-dimethylsiloxane copolymer claim 1 , the methylhydrophenyl-methylsiloxane copolymer claim 1 , the methylhydrocyanopropylsiloxane copolymer claim 1 , the methylhydromethyloctylsiloxane copolymer claim 1 , poly(1 claim 1 ,2-dimethylhydrosilazane) claim 1 , the 1-methyl-hydrosilazane) (1 claim 1 ,2-dimethylhydrosilazane) copolymer claim 1 , and methylhydrocyclosiloxane.4. An adduct according to claim 3 , wherein the hydrosilane is selected from polymethylhydrosiloxane claim 3 , tetramethyldisiloxane and triethylsilane.5. An adduct according to claim 1 , further comprising another Lewis acid claim 1 , a metal salt claim 1 , an alcohol claim 1 , or a dihalogen.6. An adduct according to claim 5 , comprising an alcohol claim 5 , advantageously iso-propanol or tert-butanol claim 5 , ...

Подробнее