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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 15344. Отображено 100.
09-02-2012 дата публикации

Volatile Imidazoles and Group 2 Imidazole Based Metal Precursors

Номер: US20120035351A1
Принадлежит: Air Products and Chemicals Inc

Sterically hindered imidazole ligands are described, along with their synthesis, which are capable of coordinating to Group 2 metals, such as: calcium, magnesium, strontium, in an eta-5 coordination mode which permits the formation of monomeric or dimeric volatile complexes. A compound comprising one or more polysubstituted imidazolate anions coordinated to a metal selected from the group consisting of barium, strontium, magnesium, radium or calcium or mixtures thereof. Alternatively, one anion can be substituted with and a second non-imidazolate anion. Synthesis of the novel compounds and their use to form BST films is also contemplated

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07-06-2012 дата публикации

Method for production of n-(2-amino-1,2-dicyanovinyl)imidates, method for production of n-(2-amino-1,2-dicyanovinyl)formamidine, and method for production of aminoimidazole derivatives

Номер: US20120142957A1
Принадлежит: Nippon Soda Co Ltd

A method for producing N-(2-amino-1,2-dicyanovinyl)formamidine, including the steps of reacting an N-(2-amino-1,2-dicyanovinyl)formimidate and ammonia by adding aqueous ammonia to a solution or suspension of an N-(2-amino-1,2-dicyanovinyl)formimidate in ether, or alternatively directly adding an N-(2-amino-1,2-dicyanovinyl)formimidate or adding a solution or suspension of an N-(2-amino-1,2-dicyanovinyl)formimidate in ether to a liquid containing ether and aqueous ammonia.

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19-07-2012 дата публикации

Novel n-halamine acrylamide monomers and copolymers thereof for biocidal coatings

Номер: US20120183494A1
Принадлежит: AUBURN UNIVERSITY

Novel acrylamide and methacrylamide hydantoin monomers which can be reacted with other acrylamide, methacrylamide, acrylate, and methacrylate monomers to form copolymers, which upon halogenation, provide oxidative coatings which are biocidal for use with various materials including, but not limited to, textiles, filters, and latex paints.

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26-07-2012 дата публикации

Diarylthiohydantoin compounds

Номер: US20120190718A1
Принадлежит: UNIVERSITY OF CALIFORNIA

The present invention relates to diarylthiohydantoin compounds and methods for synthesizing them and using them in the treatment of hormone refractory prostate cancer.

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30-08-2012 дата публикации

Amino Acid Compounds

Номер: US20120220642A1
Принадлежит: Thermolife International LLC

Methods for increasing the bioabsorption of amino acids and for preventing the development of nitrate tolerances in a human or animal are disclosed. The methods include administering to the human or animal a pharmaceutically effective amount of an amino acid compound consisting essentially of a nitrate or nitrite of an amino acid selected from the group consisting of Aspartic Acid, Cysteine, Glycine, Lysine, Methionine, Proline, Tyrosine, Phenylalanine, Carnitine, Taurine, and Betaine.

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27-12-2012 дата публикации

Method for preparing polybiotinylated compounds

Номер: US20120330028A1
Автор: Xavier Lacoux
Принадлежит: Individual

The present invention relates to a novel method for preparing compounds having the formula (I), where X is biotin or Y being biotin or Z being biotin or V being biotin or It also relates to compounds having the formula (I) and their use in clinical and industrial diagnosis.

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11-04-2013 дата публикации

ESTER COMPOUND AND USE THEREOF

Номер: US20130090363A1
Автор: Matsuo Noritada
Принадлежит: Sumitomo Chemical Company, Limited

An ester compound represented by formula (1): wherein Rrepresents hydrogen or methyl, Rrepresents hydrogen or C1-C4 alkyl, and Rrepresents hydrogen or C1-C4 alkyl; has an excellent pest control effect and is therefore useful as an active ingredient of a pest control agent. 2. The ester compound according to claim 1 , wherein a relative configuration of the substituent at the 1-position of the cyclopropane ring and the substituent at the 3-position of the cyclopropane ring is a trans configuration in formula (1).3. The ester compound according to claim 1 , wherein an absolute configuration of the 1-position of the cyclopropane ring is an R configuration in formula (1).4. The ester compound according to claim 1 , wherein an absolute configuration of the 1-position of the cyclopropane ring is an R configuration claim 1 , and a relative configuration of the substituent at the 1-position of the cyclopropane ring and the substituent at the 3-position of the cyclopropane ring is a trans configuration in formula (1).5. The ester compound according to claim 1 , wherein a relative configuration of the substituent of the 1′-position existing on the substituent at the 3-position of the cyclopropane ring is Z-configuration in formula (1).6. The ester compound according to claim 1 , wherein an absolute configuration of the 1-position of the cyclopropane ring is an R configuration and a relative configuration of the substituent of the 1′-position existing on the substituent at the 3-position of the cyclopropane ring is Z-configuration in formula (1).7. The ester compound according to claim 1 , wherein an absolute configuration of the 1-position of the cyclopropane ring is an R configuration claim 1 , a relative configuration of the substituent at the 1-position of the cyclopropane ring and the substituent at the 3-position of the cyclopropane ring is a trans configuration claim 1 , and a relative configuration of the substituent of the 1′-position existing on the substituent at ...

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11-04-2013 дата публикации

NOVEL COMPOUNDS AS OPIOID RECEPTOR MODULATORS

Номер: US20130090478A1
Принадлежит:

The present invention is directed to novel opioid receptor modulators of Formula (I). 1. A compound , wherein said compound is 5-({[2-Amino-3-(4-carbamoyl-2 ,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-4 ,5-dihydro-1H-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid.3. A hydrobromic , hydriodic , perchloric , sulfuric , nitric , phosphoric , acetic , propionic , glycolic , lactic , succinic , maleic , fumaric , malic , tartaric , citric , benzoic , mandelic , methanesulfonic , hydroxyethanesulfonic , benzenesulfonic , oxalic , pamoic , 2-naphthalenesulfonic , p-toluenesulfonic , cyclohexanesulfamic , salicylic , saccharinic or trifluoroacetic acid salt of 5-({[2-Amino-3-(4-carbamoyl-2 ,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-4 ,5-dihydro-1H-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid.4. A benzathine , chloroprocaine , choline , diethanolamine , ethylenediamine , meglumine , procaine , aluminum , calcium , lithium , magnesium , potassium , sodium , or zinc salt of 5-({[2-Amino-3-(4-carbamoyl-2 ,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-4 ,5-dihydro-1H-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid. The present application is a divisional of U.S. Ser. No. 12/838,825, filed Jul. 19, 2010, which is a divisional of U.S. Ser. No. 11/877,747, filed Oct. 24, 2007 (now U.S. Pat. No. 7,786,158), which is a continuation of U.S. Ser. No. 11/079,647, filed Mar. 14, 2005 (now U.S. Pat. No. 7,741,356), which claims the benefit of U.S. Provisional App. No. 60/553,342, filed Mar. 14, 2004, the entire contents of each of which are hereby incorporated by reference.The present invention is directed to novel opioid receptor modulators of Formula (I). The invention further relates to methods for preparing such compounds, pharmaceutical compositions containing them, and their use in the treatment of opioid modulated disorders.The opioid receptors were identified in the mid-1970's, and were quickly categorized into three sub-sets of receptors (mu, ...

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18-04-2013 дата публикации

CERTAIN CHEMICAL ENTITIES, COMPOSITIONS AND METHODS

Номер: US20130096315A1
Принадлежит:

Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of one or more mitotic kinesins are disclosed. 146.-. (canceled)48. The compound of claim 47 , or a pharmaceutically acceptable salt thereof claim 47 , wherein Ris lower alkyl substituted with hydroxy.49. The compound of claim 48 , or a pharmaceutically acceptable salt thereof claim 48 , wherein Ris 2-hydroxyethyl.50. The compound of claim 47 , or a pharmaceutically acceptable salt thereof claim 47 , wherein Ris lower alkyl substituted with optionally substituted amino.51. The compound of claim 50 , or a pharmaceutically acceptable salt thereof claim 50 , wherein Ris lower alkyl substituted 2-dimethylamino-acetylamino.52. The compound of claim 47 , or a pharmaceutically acceptable salt thereof claim 47 , wherein Ris halo.53. The compound of claim 52 , or a pharmaceutically acceptable salt thereof claim 52 , wherein Ris chloro.54. The compound of claim 47 , or a pharmaceutically acceptable salt thereof claim 47 , wherein Ris optionally substituted isopropoxy.55. The compound of claim 54 , or a pharmaceutically acceptable salt thereof claim 54 , wherein Ris 2 claim 54 ,2 claim 54 ,2-trifluoro-1-methyl-ethoxy.56. The compound of claim 47 , or a pharmaceutically acceptable salt thereof claim 47 , wherein Ris chloro and Ris 2 claim 47 ,2 claim 47 ,2-trifluoro-1-methyl-ethoxy.57. The compound of claim 47 , or a pharmaceutically acceptable salt thereof claim 47 , wherein Ris selected from 1-methyl-1H-imidazol-4-yl and 1-ethyl-1H-imidazol-4-yl claim 47 , each optionally substituted with optionally substituted lower alkyl.58. The compound of claim 57 , or a pharmaceutically acceptable salt thereof claim 57 , wherein Ris selected from 1-methyl-1H-imidazol-4-yl and 1-ethyl-1H-imidazol-4-yl claim 57 , each optionally substituted with 1-hydroxy-1-methyl-ethyl.59. The compound of claim 57 , or a pharmaceutically acceptable salt thereof claim 57 , wherein Ris selected from 1- ...

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25-04-2013 дата публикации

HAFNIUM COMPLEXES OF HETEROCYCLIC ORGANIC LIGANDS

Номер: US20130102789A1
Принадлежит: Dow Global Technologies LLC

Hafnium complexes of heterocyclic organic ligands having improved solubility in aliphatic hydrocarbon solvents and their use as components of olefin polymerization catalysts as well as novel syntheses of component parts thereof are disclosed. 2. The process of wherein Ris methyl claim 1 , Ris bromo claim 1 , and the reaction is conducted in an organic solvent comprising an aliphatic ether at −80° C. This application is a divisional application of the U.S. patent application Ser. No. 12/299,519, filed on Nov. 4, 2008, entitled “HAFNIUM COMPLEXES OF HETEROCYCLIC ORGANIC LIGANDS,” and which is a 371 national phase of PCT application number PCT/US07/07882, filed on Mar. 29, 2007, which claims the benefit of U.S. Provisional Patent Application No. 60/798,108, filed on May 5, 2006, the teachings of which are incorporated by reference herein, as if reproduced in full hereinbelow.This invention is directed to certain hafnium complexes, to catalyst compositions comprising the same, and to addition polymerization processes, especially olefin polymerization processes, using such hafnium complexes as one component of a coordination polymerization catalyst composition.Advances in polymerization and catalysis have resulted in the capability to produce many new polymers having improved physical and chemical properties useful in a wide variety of superior products and applications. With the development of new catalysts the choice of polymerization-type (solution, slurry, high pressure or gas phase) for producing a particular polymer has been greatly expanded. Also, advances in polymerization technology have provided more efficient, highly productive and economically enhanced processes. Recently, several new disclosures related to metal complexes based on polyvalent metal-centered, heteroaryl donor ligands have published. Among these are U.S. Pat. No. 6,103,657, U.S. Pat. No. 6,320,005, U.S. Pat. No. 6,653,417, U.S. Pat. No. 6,637,660, U.S. Pat. No. 6,906,160, U.S. Pat. No. 6,919, ...

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02-05-2013 дата публикации

HAPTEN CONJUGATES FOR TARGET DETECTION

Номер: US20130109019A1
Принадлежит:

Embodiments of hapten conjugates including a hapten, an optional linker, and a peroxidase-activatable aryl moiety are disclosed. In some embodiments, the peroxidase-activatable aryl moiety is tyramine or a tyramine derivative. Embodiments of methods for making and using the hapten conjugates also are disclosed. In particular embodiments, the hapten conjugates are used in a signal amplification assay. In certain embodiments, the hapten is an oxazole, a pyrazole, a thiazole, a benzofurazan, a triterpene, a urea, a thiourea other than a rhodamine thiourea, a nitroaryl other than dinitrophenyl or trinitrophenyl, a rotenoid, a cyclolignan, a heterobiaryl, an azoaryl, a benzodiazepine, or 7-diethylamino-3-carboxycoumarin. The hapten is coupled to the peroxidase-activatable aryl moiety directly or indirectly via a linker. In certain embodiments, the hapten conjugates are used in multiplexed assays. 1. A hapten conjugate , comprising:a hapten selected from an oxazole, a pyrazole, a thiazole, a benzofurazan, a triterpene, a urea, a thiourea other than a rhodamine thiourea, a nitroaryl other than dinitrophenyl or trinitrophenyl, a rotenoid, a cyclolignan, a heterobiaryl, an azoaryl, a benzodiazepine, 2,3,6,7-tetrahydro-11-oxo-1H,5H,11H-[1]benzopyrano[6,7,8-ij]quinolizine-10-carboxylic acid, or 7-diethylamino-3-carboxycoumarin;a linker; anda tyramine or a tyramine derivative.2. (canceled)6. (canceled)811.-. (canceled)1332.-. (canceled)33. A method , comprising:(a) immobilizing a first peroxidase on a first target in a sample, wherein the first peroxidase is capable of reacting with a peroxidase-activatable aryl moiety;(b) contacting the sample with a solution comprising a first hapten conjugate, the first hapten conjugate comprising a first hapten selected from an oxazole, a pyrazole, a thiazole, a benzofurazan, a triterpene, a urea, a thiourea other than a rhodamine thiourea, a nitroaryl other than dinitrophenyl or trinitrophenyl, a rotenoid, a cyclolignan, a heterobiaryl, an ...

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02-05-2013 дата публикации

METHODS OF PREPARING 1-(4-((1R,2S,3R)-1,2,3,4-TETRAHYDROXYBUTYL)-1H-IMIDAZOL-2-YL)ETHANONE

Номер: US20130109865A1
Автор: Wu Wenxue
Принадлежит:

Methods of preparing 1-(4-((1R,2S,3R)-1,2,3,4-tetrahydroxybutyl)-1H-imidazol-2-yl)ethanone and derivatives thereof are disclosed. 1. A method of preparing 1-(4-((1R ,2S ,3R)-1 ,2 ,3 ,4-tetrahydroxybutyl)-1H-imidazol-2-yl)ethanone , which comprises:contacting 2-ethoxyacrylimidate with a weak acid salt of D-glucosamine to provide a first mixture;contacting the first mixture with a base to provide a second mixture;adding an aqueous acid to the second mixture to provide a third mixture;maintaining the third mixture at a temperature of greater than 30° C. for at least 0.5 hours; andisolating 1-(4-((1R,2S,3R)-1,2,3,4-tetrahydroxybutyl)-1H-imidazol-2-yl)ethanone from the third mixture.2. The method of claim 1 , wherein the weak acid salt of D-glucosamine is D-glucosamine acetate.3. The method of claim 2 , wherein the base is an alkaline or alkaline earth metal alkoxide claim 2 , hydroxide claim 2 , carbonate claim 2 , phosphate claim 2 , or trialkylamine.4. The method of claim 3 , wherein the base is methoxide.5. The method of claim 1 , wherein the first mixture is maintained at a temperature of greater than 10° C. for at least 0.5 hours.6. The method of claim 1 , wherein the second mixture is maintained at a temperature of greater than 5° C. for at least 1 hour.7. The method of claim 1 , wherein the third mixture is maintained at a temperature of greater than 50° C. claim 1 , for at least 0.5 hours.8. The method of claim 1 , wherein the aqueous acid has a pKof from 0 to 10.9. The method of claim 8 , wherein the aqueous acid is formic claim 8 , acetic claim 8 , or trichloroacetic acid.10. The method of claim 9 , wherein the aqueous acid is acetic acid.11. The method of claim 1 , wherein the 1-(4-((1R claim 1 ,2S claim 1 ,3R)-1 claim 1 ,2 claim 1 ,3 claim 1 ,4-tetrahydroxybutyl)-1H-imidazol-2-yl)ethanone is isolated by filtering a slurry prepared by concentrating claim 1 , cooling and/or diluting the third mixture with water.12. (canceled)13. The method of claim 1 , wherein ...

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09-05-2013 дата публикации

Cyclic n,n'-diarylthioureas and n,n'-diarylureas - androgen receptor antagonists, anticancer agent, method for preparation and use thereof

Номер: US20130116269A1

The present invention relates to novel cyclic N,N′-diarylureas and N,N′-diarylthioureas—androgen receptor antagonists, anti-cancer agent, pharmaceutical composition, medicament, and method for treatment of cancerous diseases, among them prostate cancer. Cyclic N,N′-diarylthioureas or N,N′-diarylureas of the general formula 1, their optical (R)- and (S)-isomers and pharmaceutically acceptable salts thereof exhibiting properties of androgen receptor antagonists have been proposed, wherein: X represents oxygen or sulfur; m=0 or 1; R1 represents C 1 -C 3 alkyl; R2 and R3 represent hydrogen; or R2 and R3 together with C-atom they are attached to form C═O group; R4 and R5 represent hydrogen; or R4 represents hydrogen, R5 represents methyl; or R4 represents methyl, R5 represents CH 2 R6 group in which R6 represents C 1 -C 3 alkoxycarbonyl, carboxyl, hydroxyl group optionally substituted with methyl or benzyl; or R4 and R5 together with C-atom they are attached to form 5- or 6-membered heterocycle comprising at least one oxygen atom or nitrogen atom optionally substituted with methyl; or R4 and R5 together with C-atom they are attached to form NH group.

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16-05-2013 дата публикации

SUBSTITUTED IMIDAZOLONES, COMPOSITIONS CONTAINING SUCH COMPOUNDS AND METHODS OF USE

Номер: US20130123315A1
Принадлежит:

The present invention relates to compounds of the general structure shown in Formula (A): (A): and includes pharmaceutically acceptable salts, solvates, esters, prodrugs, tautomers, and isomers of said compounds. Pharmaceutical compositions and methods of treatment are also included. 2. A compound in accordance with wherein each V is independently selected from the group consisting of: Calkyl and cycloalkyl.3. A compound in accordance with wherein:G is selected from the group consisting of:{'sub': 2', '2, '(1a) hydrogen, halo, —NH, —OH, COH, cyano;'}{'sup': '1', '(2a) cycloalkyl, —O-cycloalkyl, —N(R)-cycloalkyl;'}{'sup': '1', '(3a) heterocycloalkyl, —O-heterocycloalkyl, —N(R)-heterocycloalkyl;'}{'sup': '1', '(6a) alkyl, —O-alkyl and —N(R)alkyl;'}{'sup': '1', '(7a) heteroalkyl, —O-heteroalkyl, —N(R)-heteroalkyl;'}{'sup': '1', '(8a) alkenyl, —O-alkenyl, —N(R)-alkenyl,'}{'sup': '1', '(9a) alkynyl, —O-alkynyl, —N(R)-alkynyl;'}{'sub': '2', 'sup': 1', '21, '(10a) aryl, —O—aryl, —C(O)-aryl, —S-aryl, —S(O)-aryl, —S(O)-aryl, —N(R)-aryl, —C(O)—N(R)-aryl;'}{'sub': '2', 'sup': 1', '21, '(11a) heteroaryl, —O-heteroaryl, —C(O)-heteroaryl, —S-heteroaryl, —S(O)-heteroaryl, —S(O)-heteroaryl, —N(R)-heteroaryl, —C(O)—N(R)-heteroaryl;'}wherein said heteroalkyl, heterocycloalkyl, heterocycloalkenyl, and heteroaryl of G are connected through any available carbon or heteroatom,{'sup': '2', 'and wherein said alkyl, heteroalkyl, cycloalkyl, heterocycloalkyl, aryl, said heteroaryl, alkenyl, alkynyl, cycloalkenyl, and heterocycloalkenyl of G are unsubstituted or substituted with one or more groups independently selected from R.'}4. A compound in accordance with wherein G represents a phenyl group optionally substituted with 1-3 groups selected from halo claim 1 , Calkyl claim 1 , Calkoxy claim 1 , haloCalkyl and haloCalkoxy claim 1 , or with one phenyl ring that is optionally substituted with 1-3 halo atoms.5. A compound in accordance with wherein Lis selected from the group consisting of —N( ...

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23-05-2013 дата публикации

BENZAZEPINE COMPOUND

Номер: US20130131045A1
Автор: Kan Keizo, Ohtani Tadaaki
Принадлежит: OTSUKA PHARMACEUTICAL CO., LTD.

An object of the present invention is to provide a novel benzazepine compound or a salt thereof, which has excellent vasopressin antagonistic activity. 2. A benzazepine compound selected from the group consisting of:(1) N-(4-(7-chloro-5-hydroxy-2,3,4-trihydro-5-deutero-1H-benzo[b]azepine-1-carbonyl)-3-methylphenyl)-2-methylbenzamide,(2) N-(4-(7-chloro-2,3-dihydro-5-hydroxy-4,4,5-trideutero-1H-benzo[b]azepine-1-carbonyl)-3-methylphenyl)-2-methylbenzamide,(3) N-(4-(7-chloro-5-hydroxy-2,2-dideutero-3,4,5-trihydro-1H-benzo[b]azepine-1-carbonyl)-3-methylphenyl)-2-methylbenzamide,(4) N-(4-(7-chloro-5-hydroxy-2,2,4,4,5-pentadeutero-1H-benzo[b]azepine-1-carbonyl)-3-methylphenyl)-2-methylbenzamide, and(5) N- {4-(7-chloro-5-hydroxy-2,3,4,5-tetrahydro-1H-benzo[b]azepine-1-carbonyl)-3-methylphenyl} -3,4,5,6-tetradeutero -2-trideutero methylbenzamide,or a salt thereof.3. A pharmaceutical composition or a salt thereof comprising claim 1 , as an active ingredient claim 1 , the benzazepine compound of claim 1 , and a pharmaceutically acceptable carrier.4. Use of the benzazepine compound or a salt thereof of claim 1 , as a drug.5. A vasopressin antagonist comprising claim 1 , as an active ingredient claim 1 , the benzazepine compound or a salt thereof of .6. The pharmaceutical composition according to claim 3 , which is for preventing or treating at least one disease selected from the group consisting of hypertension claim 3 , edema claim 3 , ascites claim 3 , heart failure claim 3 , renal dysfunction claim 3 , syndrome of inappropriate secretion of antidiuretic hormone (SIADH) claim 3 , liver cirrhosis claim 3 , hyponatremia claim 3 , hypokalemia claim 3 , diabetes claim 3 , circulatory failure claim 3 , motion sickness claim 3 , water-metabolism disorder claim 3 , renal failure claim 3 , cerebral infarction claim 3 , cardiac infarction claim 3 , and polycystic kidney disease (PKD).7. The pharmaceutical composition according to claim 3 , which is for use as at least one drug ...

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06-06-2013 дата публикации

FUNGICIDAL IMIDAZOLES

Номер: US20130143929A1
Принадлежит: EI DU PONT DE NEMOURS AND COMPANY

Disclosed are compounds of Formula 1, including all stereoisomers, N-oxides, and salts thereof, 2. A compound of wherein:{'sup': 1', '5a', '5a, 'Qis a phenyl ring substituted with 1 to 3 substituents independently selected from R; or a pyridinyl or pyrimidinyl ring optionally substituted with up to 3 substituents independently selected from R;'}{'sup': 2', '5a', '5a, 'Qis a phenyl ring substituted with 1 to 3 substituents independently selected from R; or a pyrazolyl, pyridinyl or pyrimidinyl ring optionally substituted with up to 3 substituents independently selected from Ron carbon atom ring members and methyl on the nitrogen atom ring member;'}{'sup': 1', '2, 'sub': 1', '3, 'Rand Rare each independently H, halogen, cyano, C-Calkyl or cyclopropyl;'}{'sup': 3', '6, 'Ris Br, Cl, F, —ORor —SC≡N;'}{'sup': '4', 'Ris H or methyl;'}{'sup': '5a', 'sub': 1', '2', '1', '2', '1', '2', '1', '2, 'each Ris independently halogen, cyano, C-Calkyl, C-Chaloalkyl, cyclopropyl, C-Calkoxy, C-Calkylthio or -T-U—V;'}{'sup': '6', 'sub': 1', '3', '1', '2', '2', '3', '2', '4', '2', '4', '2', '4', '2', '4', '2', '4, 'Ris H, —CH(═O), C-Calkyl, C-Chaloalkyl, C-Calkoxyalkyl, C-Ccyanoalkyl, C-Calkylcarbonyl, C-Calkoxycarbonyl, C-C(alkylthio)carbonyl or C-Calkoxy(thiocarbonyl);'}each T is independently O, NH or a direct bond;{'sub': 1', '3, 'each U is independently C-Calkylene, wherein up to 1 carbon atom is selected from C(═O);'}{'sup': 8a', '8b', '9, 'each V is independently N(R)(R) or OR;'}{'sup': 8a', '8b, 'each Rand Ris independently H or methyl; and'}{'sup': '9', 'each Ris independently H, methyl or halomethyl.'}3. A compound of wherein{'sup': 1', '5a, 'Qis a phenyl ring substituted with 1 to 3 substituents independently selected from R;'}{'sup': 2', '5a, 'Qis a phenyl ring substituted with 1 to 3 substituents independently selected from R;'}{'sup': 1', '2, 'sub': 1', '2, 'Rand Rare each independently H, Cl, Br, I or C-Calkyl; and'}{'sup': '5a', 'each Ris independently halogen, cyano, ...

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06-06-2013 дата публикации

IMIDO-ACID SALTS AND METHODS OF USE

Номер: US20130143939A1
Автор: Bara Jason E.

Imido-acid salts and compositions containing imido-acid salts are described herein. Methods of their preparation and use are also described herein. The methods of using the imido-acid salts include the reduction of volatile compounds from gas and liquid streams and the delivery of pharmaceutical agents to subjects. 2. The compound of claim 1 , wherein L is substituted or unsubstituted Calkyl.3. The compound of claim 1 , wherein M is substituted or unsubstituted imidazolium or substituted or unsubstituted pyridinium.4. The compound of claim 1 , wherein Rand Rare combined to form substituted or unsubstituted aryl claim 1 , substituted or unsubstituted heteroaryl claim 1 , substituted or unsubstituted cycloalkyl claim 1 , substituted or unsubstituted cycloalkenyl claim 1 , substituted or unsubstituted cycloalkynyl claim 1 , substituted or unsubstituted heterocycloalkyl claim 1 , substituted or unsubstituted heterocycloalkenyl claim 1 , or substituted or unsubstituted heterocycloalkynyl.5. The compound of claim 1 , wherein Xis CO or SO.6. A composition comprising the compound of and a pharmaceutically acceptable carrier.10. The method of claim 9 , wherein the volatile compound is carbon dioxide claim 9 , sulfur dioxide claim 9 , or hydrogen sulfide.11. The method of claim 9 , wherein the system further comprises an amine.12. The method of claim 11 , wherein the amine is selected from the group consisting of primary amines claim 11 , secondary amines claim 11 , tertiary amines claim 11 , cyclic amines claim 11 , or mixtures thereof.14. The method of claim 13 , wherein the primary amine is selected from the group consisting of monoethanolamine claim 13 , diglycolamine claim 13 , 2-amino-2-methylpropanol claim 13 , or mixtures thereof.15. The method of claim 13 , wherein the secondary amine is selected from the group consisting of diethanolamine claim 13 , diisopropanolamine claim 13 , or mixtures thereof.16. The method of claim 13 , wherein the tertiary amine is N- ...

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20-06-2013 дата публикации

METRONIDAZOLE ESTERS FOR TREATING ROSACEA

Номер: US20130158090A1
Принадлежит: GALDERMA RESEARCH & DEVELOPMENT

A compound of formula (I): 2. The method as defined in claim 1 , for treating rosacea.3. (canceled)4. The method as defined in claim 1 , wherein the salt of the compound of formula (I) or of an enantiomer thereof is a salt of the compound or an enantiomer thereof with a pharmaceutically acceptable acid.5. The method as defined in claim 4 , wherein the pharmaceutically acceptable acid is selected from the group consisting of:a) a pharmaceutically acceptable inorganic acid; andb) a pharmaceutically acceptable organic acid.6. The method as defined in claim 1 , wherein the compound is selected from the group consisting of a compound of formula (I) claim 1 , a hydrochloride of the compound of formula (I) claim 1 , a citrate of the compound of formula (I) claim 1 , a salicylate of the compound of formula (I) claim 1 , a benzoate of the compound of formula (I) claim 1 , and an S enantiomer of any one of these compounds.7. The method as defined in claim 1 , wherein the compound is 2-(2-methyl-5-nitroimidazol-1-yl)ethyl (S)-2-(4-isobutylphenyl)propionate.8. The method as defined in claim 1 , wherein the compound is in the form of a pharmaceutical composition for topical application.9. The method as defined in claim 8 , wherein the pharmaceutical composition is in the form of a solution claim 8 , a gel or an emulsion.10. The method as defined in claim 8 , wherein the compound is present in an amount of 0.001% to 10% by weight relative to the total weight of the composition.12. The method as defined in claim 5 , wherein the pharmaceutically acceptable inorganic acid is selected from the group consisting of hydrochloric acid claim 5 , sulfuric acid claim 5 , phosphoric acid claim 5 , nitric acid claim 5 , and hydrobromic acid.13. The method as defined in claim 5 , wherein the pharmaceutically acceptable organic acid is selected from the group consisting of acetic acid claim 5 , tartaric acid claim 5 , maleic acid claim 5 , hydroxymaleic acid claim 5 , fumaric acid claim 5 , ...

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20-06-2013 дата публикации

PROCESS FOR THE SYNTHESIS OF IVABRADINE AND ADDITION SALTS THEREOF WITH A PHARMACEUTICALLY ACCEPTABLE ACID

Номер: US20130158257A1
Принадлежит: LES LABORATOIRES SERVIER

Process for the synthesis of ivabradine of formula (I): 2. The process according to claim 1 , wherein the reductive amination reaction is carried out in the absence of solvent.3. The process according to claim 1 , wherein the amount of formic acid used in the reductive amination reaction is from 2 to 50 equivalents per equivalent of aldehyde.4. The process according to claim 1 , wherein the amount of triethylamine used in the reductive amination reaction is from 2 to 50 equivalents per equivalent of aldehyde.5. The process according to claim 1 , wherein the temperature of the reductive amination reaction is from 30 to 100° C. The present invention relates to a process for the synthesis of ivabradine of formula (I):or 3-{3-[{[7S)-3,4-dimethoxybicyclo[4.2.0]octa-1,3,5-trien-7-yl]methyl}(methyl)amino]-propyl}-7,8-dimethoxy-1,3,4,5-tetrahydro-2H-3-benzazepin-2-one, addition salts thereof with a pharmaceutically acceptable acid, and hydrates thereof.Ivabradine, and its addition salts with a pharmaceutically acceptable acid, and more especially its hydrochloride, have very valuable pharmacological and therapeutic properties, especially bradycardic properties, making those compounds useful in the treatment or prevention of various clinical situations of myocardial ischaemia such as angina pectoris, myocardial infarct and associated rhythm disturbances, and also in various pathologies involving rhythm disturbances, especially supraventricular rhythm disturbances, and in heart failure.The preparation and therapeutic use of ivabradine and its addition salts with a pharmaceutically acceptable acid, and more especially its hydrochloride, have been described in the European patent specification EP 0 534 859. Unfortunately, the ivabradine synthesis route described in that patent specification results in the expected product in a yield of only 1%.Another ivabradine synthesis route, which is based on a reductive amination reaction, has been described in the European patent ...

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27-06-2013 дата публикации

PROCESSES FOR PREPARING 3-BENZAZEPINES

Номер: US20130165648A1
Принадлежит:

The present invention provides processes and intermediates for the preparation of 3-benzazepines and salts thereof which can be useful as serotonin (5-HT) receptor agonists for the treatment of, for example, central nervous system disorders such as obesity. 1651.-. (canceled)653. A process according to claim 652 , wherein said halogenating/sulfonating reagent is SOBror SOCl.654. A process according to claim 652 , wherein Xis Cl.655. A process according to claim 652 , wherein Xis Br.656. A process according to claim 652 , wherein the reaction of said compound of Formula X with said halogenating/sulfonating reagent is carried out in the presence of solvent claim 652 , and said solvent comprises dimethylformamide or toluene.657. A process according to claim 652 , wherein the reaction of said compound of Formula X with said halogenating/sulfonating reagent is carried out at a temperature of about −40 to about 80° C.658. A process according to claim 652 , wherein Ris H claim 652 , Ris Me claim 652 , Ris H claim 652 , Ris Cl claim 652 , Ris H claim 652 , Ris H claim 652 , Ris H claim 652 , Ris H claim 652 , Ris H claim 652 , and Ris H.660. A compound according to claim 659 , wherein Xis Br.661. A compound according to claim 659 , wherein Xis Cl.662. A compound according to claim 659 , wherein Ris H claim 659 , Ris Me claim 659 , Ris H claim 659 , Ris Cl claim 659 , Ris H claim 659 , Ris H claim 659 , Ris H claim 659 , Ris H claim 659 , Ris H claim 659 , and Ris H.664. A process according to claim 663 , wherein the reaction of said compound of Formula XI to give said compound of Formula X is carried out at a temperature of about 80 to about 110° C.665. A process according to claim 663 , wherein Xis Br.666. A process according to claim 663 , wherein Ris H claim 663 , Ris Me claim 663 , Ris H claim 663 , Ris Cl claim 663 , Ris H claim 663 , Ris H claim 663 , Ris H claim 663 , Ris H claim 663 , Ris H claim 663 , and Ris H.668. A compound according to claim 667 , wherein Ris H ...

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04-07-2013 дата публикации

Novel Imidazolium Salts and Carbene Metal Complexes Based Thereon for Use as Bioanalytical Markers for Biomolecules

Номер: US20130171071A1
Автор: Kuehl Olaf

The present invention relates to imidazolium salts, particularly imidazolium salts of the general formula I as well as the respective carbene metal complexes and their utilisation as bioanalytical tags for biomolecules. 2. Imidazolium salts according to claim 1 , wherein the groups R claim 1 , R claim 1 , and R claim 1 , where applicable claim 1 , are the same or different and chosen from the group of C-C-n-alkyl groups.3. Imidazolium salts according to claim 1 , wherein n claim 1 , m claim 1 , and q claim 1 , where applicable claim 1 , are zero or 1 and b and l are zero.4. Imidazolium salts according to claim 1 , wherein R″ is a C-C-n-alkyl group.7. Carbene metal complexes according to claim 6 , wherein the metal is chosen from the group consisting of copper claim 6 , iron claim 6 , ruthenium claim 6 , nickel claim 6 , and palladium or from the group consisting of technetium claim 6 , rhenium and cobalt.8. Carbene metal complexes according to claim 6 , wherein the ligand L is chosen from the group consisting ofCO;nitrile;isonitrile;nitrosyl;halogenide ion;hydrogen atom;{'sub': 1', '12', '6', '14', '1', '12', '6', '14', '1', '12', '6', '14', '1', '12', '6', '14', '6', '14', '1', '12', '1', '12, 'C-C-alkyl anion, allyl anion, methylallyl anion, benzyl anion, C-C-aryl anion, C-C-alkoxy anion, C-C-aryloxy anion, C-C-heteroalkyl anion, C-C-heteroaryl anion, C-C-heteroalkoxy anion, C-C-heteroaryloxy anion or C-C-heteroaryloxy anion, which is unsubstituted or the same or differently substituted by one or more C-C-alkyl groups or C-C-heteroalkyl groups, whereby the heteroatoms are chosen from the group B, Al, Ga, In, N, P, As, Sb, Bi, Si, Ge, Sn, Pb, O, S, Se, and Te and wherein the anions are unsubstituted or wholly or partially substituted with one or more than one, same, or different heteroatoms from the same group, in the form of functional groups, wherein the cyclic and aromatic systems are single rings or several annelated or isolated rings;'}primary, secondary, ...

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04-07-2013 дата публикации

BASE GENERATOR

Номер: US20130172569A1
Принадлежит: ETERNAL CHEMICAL CO., LTD.

The present invention provides a base generator having the structure of formula (1): 5. The base generator according to claim 1 , wherein R claim 1 , Rand Rare the same or different and are each independently H claim 1 , methyl claim 1 , ethyl claim 1 , n-propyl claim 1 , isopropyl claim 1 , n-butyl claim 1 , isobutyl claim 1 , tert-butyl claim 1 , pentyl claim 1 , hexyl claim 1 , hydroxymethyl claim 1 , hydroxyethyl claim 1 , hydroxypropyl claim 1 , hydroxybutyl claim 1 , hydroxypentyl claim 1 , hydroxyhexyl claim 1 , cyanomethyl claim 1 , cyanoethyl claim 1 , cyanopropyl claim 1 , cyanobutyl claim 1 , cyanopentyl claim 1 , cyanohexyl claim 1 , phenyl claim 1 , benzyl or diphenylmethyl.6. The base generator according to claim 1 , wherein R claim 1 , Rand Rare the same or different and are each independently H claim 1 , methyl claim 1 , ethyl claim 1 , n-propyl or isopropyl.7. The base generator according to claim 1 , wherein the anionic group is selected from a group consisting of halide ion claim 1 , sulfate claim 1 , nitrate claim 1 , phosphate claim 1 , sulfonate claim 1 , carbonate claim 1 , tetrafluoborate claim 1 , borate claim 1 , chlorate claim 1 , iodate claim 1 , hexafluorophosphate claim 1 , perchlorate claim 1 , trifluoromethanesulfonate claim 1 , trifluoroacetate claim 1 , acetate claim 1 , tert-butylcarbonate claim 1 , (CFSO)N and tert-butyloxy.8. The base generator according to claim 1 , wherein the anionic group is a halide ion or tetrafluoroborate.9. The base generator according to claim 1 , which is an optical base generator or a thermal base generator. The present invention relates to a base generator, and particularly to a base generator which exhibits good storage stability, can generate a base by exposure to heating or irradiation of light, and can be used for imidization of a polyimide precursor, promoting crosslinking of epoxy monomers, or crosslinking of polyurethane or polyurea.Polyimide is the first choice among high performance polymer ...

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11-07-2013 дата публикации

Imidazole Derivatives Useful for Controlling Microbial Growth

Номер: US20130177621A1
Принадлежит:

Disclosure is provided for 1,4,5-substituted amino imidazole compounds useful to control microbial growth, compositions including these compounds, devices including these compounds, and methods of using the same. 5. The compound of claim 4 , wherein one of D1 claim 4 , D2 claim 4 , D3 claim 4 , D4 or D5 is C1-C15 alkyl claim 4 , and the others are H.6. The compound of claim 4 , wherein one of D1 claim 4 , D2 claim 4 , D3 claim 4 , D4 or D5 is a C1 claim 4 , C3 claim 4 , C5 claim 4 , C7 claim 4 , C9 or C11 alkyl claim 4 , and the others are H.10. A composition comprising a carrier and an effective amount of the compound of .11. The composition of claim 10 , wherein said composition is an ointment claim 10 , cream claim 10 , lotion claim 10 , paste claim 10 , gel claim 10 , foam claim 10 , spray claim 10 , aerosol claim 10 , or oil.12. A composition comprising the compound of covalently coupled to a substrate.13. A bacterial growth inhibiting coating composition claim 1 , comprising:(a) a film-forming resin;(b) a solvent that disperses said resin;{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, '(c) an effective amount of the compound of , wherein said effective amount of said compound inhibits the growth of bacteria thereon; and'}(d) optionally, at least one pigment.14. A substrate coated with the coating composition of .15. A method of reducing microbial growth on a substrate comprising the step of contacting the compound of to said substrate in an amount effective to reduce said microbial growth.16. The method of claim 15 , wherein said microbial growth is Gram-positive bacterial growth.17Staphylococcus aureus.. The method of claim 15 , wherein said bacterial growth is18Staphylococcus aureus. The method of claim 15 , wherein bacterial growth is methicillin-resistant (MRSA).19. A method for treating a bacterial infection in a subject in need thereof claim 1 , comprising administering to said subject the compound of in an amount effective to reduce a bacterial ...

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11-07-2013 дата публикации

PROCESSES FOR THE PREPARATION OF 8-CHLORO-1-METHYL-2,3,4,5-TETRAHYDRO-1H-3-BENZAZEPINE AND INTERMEDIATES RELATED THERETO

Номер: US20130178619A1
Принадлежит:

The present invention provides processes, methods and intermediates for the preparation of 8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine, salts, hydrates and crystal forms thereof which are useful as serotonin (5-HT) receptor agonists for the treatment of, for example, central nervous system disorders such as obesity. 127.-. (canceled)29. The method according to claim 28 , wherein the L-(+)-tartaric acid salt of said compound of Formula (Ia) has a chiral purity of greater than 98.0% enantiomeric excess.30. The method according to claim 28 , wherein the L-(+)-tartaric acid salt of said compound of Formula (Ia) has a chiral purity of greater than 99.0% enantiomeric excess.31. The method according to claim 28 , further comprising recrystallizing the L-(+)-tartaric acid salt of said compound of Formula (Ia) from acetone and water.32. The method according to claim 31 , wherein the recrystallized L-(+)-tartaric acid salt of said compound of Formula (Ia) has a chiral purity of greater than 98.0% enantiomeric excess.33. The method according to claim 31 , wherein the recrystallized L-(+)-tartaric acid salt of said compound of Formula (Ia) has a chiral purity of greater than 99.0% enantiomeric excess.35. The method according to claim 34 , wherein the L-(+)-tartaric acid salt of said compound of Formula (Ia) has a chiral purity of greater than 98.0% enantiomeric excess.36. The method according to claim 34 , wherein the L-(+)-tartaric acid salt of said compound of Formula (Ia) has a chiral purity of greater than 99.0% enantiomeric excess.37. The method according to claim 34 , further comprising recrystallizing the L-(+)-tartaric acid salt of said compound of Formula (Ia) from acetone and water.38. The method according to claim 37 , wherein the recrystallized L-(+)-tartaric acid salt of said compound of Formula (Ia) has a chiral purity of greater than 98.0% enantiomeric excess.39. The method according to claim 37 , wherein the recrystallized L-(+)-tartaric acid salt of ...

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25-07-2013 дата публикации

THERAPEUTIC AGENT FOR NEUROLOGICAL DISEASES

Номер: US20130190363A1
Принадлежит:

An object of the present invention is to provide a pharmaceutical agent useful for treating and preventing neurological disease, having satisfactory solubility and oxidative stress-mediated cell death suppressive activity as well as capable of exhibiting excellent blood-brain barrier permeability. The present invention is directed to an acylaminoimidazole derivative represented by general formula (I) or a salt thereof, and a pharmaceutical and a therapeutic or preventive agent for neurological disease containing the same, as an active ingredient. 2. The acylaminoimidazole derivative or a salt thereof according to claim 1 , wherein Ris a group of formula (Ia) claim 1 , Ris a hydrogen atom and X is a nitrogen atom.3. The acylaminoimidazole derivative or a salt thereof according to claim 1 , wherein the acylaminoimidazole derivative is (2R)-2-(mesityloxy)-N-[4-(pyridin-2-yl)-1H-imidazol-2-yl]propanamide.4. The acylaminoimidazole derivative or a salt thereof according to claim 1 , wherein the acylaminoimidazole derivative is 2-(mesitylamino)-N-[4-(pyridin-2-yl)-1H-imidazol-2-yl]acetamide.5. The acylaminoimidazole derivative or a salt thereof according to claim 1 , wherein the acylaminoimidazole derivative is 2-[mesityl(methyl)amino]-N-[4-(pyridin-2-yl)-1H-imidazol-2-yl]acetamide.6. A pharmaceutical comprising the acylaminoimidazole derivative or a salt thereof according to any one of to claim 1 , as an active ingredient.7. A therapeutic or preventive agent for neurological disease comprising the acylaminoimidazole derivative or a salt thereof according to any one of to claim 1 , as an active ingredient.8. An oxidative stress-mediated cell death suppressant comprising the acylaminoimidazole derivative or a salt thereof according to any one of to claim 1 , as an active ingredient.9. The therapeutic or preventive agent for neurological disease according to claim 7 , wherein the neurological disease is a neurodegenerative disease having cell degeneration due to oxidative ...

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25-07-2013 дата публикации

PROCESS FOR PREPARING TOLVAPTAN INTERMEDIATES

Номер: US20130190490A1
Принадлежит: HETERO RESEARCH FOUNDATION

The present invention provides a novel process for the preparation of 7-chloro-2,3,4,5-tetrahydro-1H-1-benzazepin-5-one. The present invention also provides an improved process for the preparation of 7-chloro-1-(2-methyl-4-nitrobenzoyl)-5-oxo-2,3,4,5-tetrahydro-1H-1-benzazepine. The present invention further provides an improved process for the preparation of 7-chloro-1-[2-methyl-4-[(2-methylbenzoyl)amino]benzoyl]-5-oxo-2,3,4,5-tetrahydro-1H-1-benzazepine. 1. A process for the preparation of 7-chloro-5-oxo-2 ,3 ,4 ,5-tetrahydro-1H-1-benzazepine , comprising:a. reacting 7chloro-4-ethoxycarbonyl-5-oxo-N-p-toluenesufonyl-2,3,4,5-tetrahydro-1H-benzazepine with sulfuric acid;b. maintaining the contents obtained in step (a) at above 50° C. to form reaction mass;c. cooling the first reaction mass obtained in step (b) at room temperature;d. pouring the reaction mass into water;e. adjusting the pH of the reaction mass to about 7.0 to 8.5 with a base; andf. isolating 7-chloro-5-oxo-2,3,4,5-tetrahydro-1H-1-benzazepine from the reaction mass.2. The process of claim 1 , wherein the sulfuric acid is used in step (a) in the form of aqueous sulfuric acid.3. The process of claim 1 , wherein step (b) is carried out at a temperature of about 60 to 100° C.4. The process of claim 1 , wherein the base used in step (e) is an organic base or inorganic base.54. The process of claim 1 , wherein the base is an inorganic base selected from alkali metal hydroxides claim 1 , alkali metal carbonates and alkali metal bicarbonates.6. The process of claim 5 , wherein the inorganic base is sodium hydroxide or potassium hydroxide.7. The process of claim 1 , wherein the pH in step (e) is adjusted to 7.2 to 8.2.8. A process for the preparation of 7-chloro-1-(2-methyl-4-1-nitrobenzoyl)-5-oxo-2 claim 1 ,3 claim 1 ,4 claim 1 ,5-tetrahydro-1H-1-benzazepine claim 1 , comprising reacting 7-chloro-5-oxo-2 claim 1 ,3 claim 1 ,4 claim 1 ,5-tetrahydro-1H-1-benzazepine with 2-methyl-4-nitobenzoyl chloride in the ...

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25-07-2013 дата публикации

PROCESSES FOR THE SYNTHESIS OF DIARYLTHIOHYDANTOIN AND DIARYLHYDANTOIN COMPOUNDS

Номер: US20130190507A1
Принадлежит:

Processes are provided for the synthesis of diarylthiohydantoin and diarylhydantoin compounds. Medicinal products containing the same find particular use in treating prostate cancer, including castration-resistant prostate cancer and/or hormone-sensitive prostate cancer. 3. The process of claim 1 , wherein X is S.4. The process of claim 1 , wherein Yand Yare both methyl.5. The process of claim 1 , wherein Yand Ytogether with the carbon to which they are attached combine to form a cyclobutyl ring or a cyclopentyl ring.6. The process of claim 1 , wherein Lis a single bond.7. The process of claim 1 , wherein Ris —C(═O)—NHCH.8. The process of claim 1 , wherein Ris —C(═O)—NH.9. The process of claim 1 , wherein Ris F.10. The process of claim 1 , wherein Yand Yare both methyl claim 1 , Ris —C(═O)—NHCH claim 1 , and Ris F.11. The process of claim 1 , wherein Yand Yare both methyl claim 1 , Ris —C(═O)—NH claim 1 , and Ris F.13. The process of claim 12 , wherein X is S.1412. The process of claim 12 , wherein Yand Yare both methyl claim 12 , Ris —C(═O)—OH claim 12 , and Ris F. This patent application is a continuation of Ser. No. 13/580,718 filed Aug. 23, 2012 as a national phase application of PCT/US2011/026135 filed on Feb. 24, 2011, which claims priority to Ser. No. 61/307,796, filed Feb. 24, 2010. Each of these applications is incorporated herein by reference in its entirety.Not applicable.The invention is in the field of cancer therapeutics, such as processes for the synthesis of prostate cancer therapeutics.According to the American Cancer Society, prostate cancer is the most commonly diagnosed cancer among men in the United States, other than skin cancer. The American Cancer Society estimates that approximately 186,000 new cases of prostate cancer were diagnosed, and approximately 29,000 men died of prostate cancer in the United States alone during 2008. Prostate cancer is thus the second-leading cause of cancer death in men in the United States, after lung cancer. ...

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01-08-2013 дата публикации

METRONIDAZOLE ESTERS FOR TREATING ROSACEA

Номер: US20130197048A1
Принадлежит: GALDERMA RESEARCH & DEVELOPMENT

A compound of formula (I): 2. The compound as defined in claim 1 , wherein the compound is incorporated into a medicament.3. The compound as defined in claim 1 , wherein the compound is effective in treating rosacea.4. The compound as defined in claim 1 , wherein the salt of the compound of formula (I) is a salt of the compound with a pharmaceutically acceptable acid.5. The compound as defined in claim 1 , wherein the pharmaceutically acceptable acid is selected from the group consisting of:a) pharmaceutically acceptable inorganic acid; andb) a pharmaceutically acceptable organic acid.6. The compound as defined in claim 1 , wherein the compound is selected from the group consisting of a compound of formula (I) claim 1 , a hydrochloride of the compound of formula (I) claim 1 , a citrate of the compound of formula (I) claim 1 , a salicylate of the compound of formula (I) and a benzoate of the compound of formula (I).7. The compound as defined in claim 1 , wherein the compound is 2-(2-methyl-5-nitroimidazol-1-yl)ethyl [2-(2 claim 1 ,6-dichlorophenylamino)phenyl]acetate.8. A pharmaceutical composition for topical application comprising a compound as defined in and a pharmaceutical carrier.9. The composition as defined in claim 8 , said composition being in the form of a solution claim 8 , a gel or an emulsion.10. The composition as defined in claim 8 , wherein the compound is present in an amount of 0.001% to 10% by weight relative to the total weight of the composition.11. The compound as defined in claim 5 , wherein the pharmaceutically acceptable inorganic acid is selected from the group consisting of hydrochloric acid claim 5 , sulfuric acid claim 5 , phosphoric acid claim 5 , nitric acid and hydrobromic acid.12. The compound as defined in claim 5 , wherein the pharmaceutically acceptable organic acid is selected from the group consisting of acetic acid claim 5 , tartaric acid claim 5 , maleic acid claim 5 , hydroxymaleic acid claim 5 , fumaric acid claim 5 , citric ...

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01-08-2013 дата публикации

COMPOUNDS FOR TREATMENT OF CANCER

Номер: US20130197049A1
Принадлежит:

The present invention relates to novel compounds having anti-cancer activity, methods of making these compounds, and their use for treating cancer and drug-resistant tumors, e.g. melanoma, metastatic melanoma, drug resistant melanoma, prostate cancer and drug resistant prostate cancer. 4. The compound of claim 1 , wherein said compound is(4-phenyl-1H-imidazol-2-yl)(3,4,5-trimethoxyphenyl)methanone (70a);(4-(4-fluorophenyl)-1H-imidazol-2-yl)(3,4,5-trimethoxyphenyl)methanone (70b);(4-(4-chlorophenyl)-1H-imidazol-2-yl)(3,4,5-trimethoxyphenyl)methanone (70c);(4-(4-bromophenyl)-1H-imidazol-2-yl)(3,4,5-trimethoxyphenyl)methanone (70d);(4-(4-(trifluoromethyl)phenyl)-1H-imidazol-2-yl)(3,4,5-trimethoxyphenyl)methanone (70e);(4-p-tolyl-1H-imidazol-2-yl)(3,4,5-trimethoxyphenyl)methanone (70f);(4-(4-methoxyphenyl)-1H-imidazol-2-yl)(3,4,5-trimethoxyphenyl)methanone (70g);(4-(4-(dimethylamino)phenyl)-1H-imidazol-2-yl)(3,4,5-trimethoxyphenyl)methanone (70h);(4-(4-hydroxyphenyl)-1H-imidazol-2-yl)(3,4,5-trimethoxyphenyl)methanone (70i);(5-methyl-4-phenyl-1H-imidazol-2-yl)(3,4,5-trimethoxyphenyl)methanone (70j);(5-ethyl-4-phenyl-1H-imidazol-2-yl)(3,4,5-trimethoxyphenyl)methanone (70k);(4-phenyl-5-propyl-1H-imidazol-2-yl)(3,4,5-trimethoxyphenyl)methanone (70l);(1-methyl-4-phenyl-1H-imidazol-2-yl)(3,4,5-trimethoxyphenyl)methanone (70m);(1-ethyl-4-phenyl-1H-imidazol-2-yl)(3,4,5-trimethoxyphenyl)methanone (70n);(1-benzyl-4-phenyl-1H-imidazol-2-yl)(3,4,5-trimethoxyphenyl)methanone (70o); or(1-cyclopentyl-4-phenyl-1H-imidazol-2-yl)(3,4,5-trimethoxyphenyl)methanone (70p).5. A pharmaceutical composition comprising a compound according to and a pharmaceutically acceptable carrier.6. A method of treating claim 1 , suppressing claim 1 , reducing the severity claim 1 , reducing the risk claim 1 , inhibiting cancer comprising administering a compound according to to a subject having cancer under conditions effective to treat the cancer.7. The method of claim 6 , wherein said cancer is selected ...

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01-08-2013 дата публикации

MOLECULES HAVING COMBINABLE GROUPS

Номер: US20130197237A1
Принадлежит: Arkema France

The present invention relates to nitrogenous associative molecules comprising at least one unit rendering them capable of associating with one another or with a filler, via noncovalent bonds, and comprising a function capable of reacting with a polymer containing unsaturations so as to form a covalent bond with said polymer. 18-. (canceled)9. A compound comprising at least one group Q and at least one group A linked together by at least one spacer group Sp , wherein:group Q comprises a dipole comprising at least one nitrogen atom;group A comprises an associative group comprising at least one nitrogen atom; andSp is an atom or a group of atoms forming a link between group Q and group A.10. The compound of claim 9 , wherein the group Q comprises a dipole having one nitrogen atom.11. The compound of claim 9 , wherein the group A is chosen from imidazolidinyl claim 9 , triazoyl claim 9 , ureyl claim 9 , bis-ureyl claim 9 , and ureidopyrimidyl groups.14. The compound of claim 9 , wherein the group Q comprises a nitrile oxide claim 9 , nitrone or nitrile imine function.16. The compound of claim 9 , wherein the spacer group Sp is a linear or branched C-Calkyl chain claim 9 , optionally comprising one or more nitrogen or oxygen atoms.17. The compound of claim 16 , wherein the spacer group Sp is a linear or branched C-Calkyl chain claim 16 , optionally comprising one or more nitrogen or oxygen atoms.18. The compound of claim 16 , wherein the spacer group Sp is a linear C-Calkyl chain claim 16 , optionally comprising one or more nitrogen or oxygen atoms. This application is the U.S. National Phase application of PCT International Application No. PCT/FR2011/051651, filed Jul. 12, 2011, and claims priority to French Patent Application No. 1055717, filed Jul. 13, 2010, the disclosures of which are incorporated by reference in their entirety for all purposes.The present invention relates to nitrogenous associative molecules comprising at least one unit rendering them capable of ...

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08-08-2013 дата публикации

Mitochondria-Targeted Inhibitors of Cytochrome C Peroxidase for Protection from Apoptosis

Номер: US20130203829A1
Принадлежит: Individual

The present application is directed to novel imidazole-substituted fatty acids that have been functionalized with an alkyl triphenylphosphonium group, compositions comprising these compounds and their use as inhibitors of cytochrome c peroxidase, in particular for the treatment and prevention of apoptosis.

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15-08-2013 дата публикации

COMPOUNDS AND COMPOSITIONS AS INHIBITORS OF CANNABINOID RECEPTOR 1 ACTIVITY

Номер: US20130210769A1
Принадлежит: IRM LLC

The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of Cannabinoid Receptor 1 (CB1). 2. The compound of in which Ris selected from cyano claim 1 , methyl-carbonyl-amino-sulfonyl-ethyl claim 1 , pyrrolidin-2-onyl-ethyl claim 1 , imidazolyl-ethyl claim 1 , oxazolidin-2-only-ethyl claim 1 , 1-pyrazolyl-ethyl claim 1 , cyano-methyl claim 1 , 4′-(4-chlorophenoxy)phenyl claim 1 , 1 claim 1 ,3-dioxanyl-ethyl claim 1 , allyl claim 1 , phenyl claim 1 , pyrazinyl claim 1 , piperazinyl-sulfonyl-ethyl claim 1 , azetidinyl-sulfonyl-ethyl claim 1 , morpholino-sulfonyl-ethyl claim 1 , pyrrolidinyl-sulfonyl-ethyl claim 1 , pyrrolidinyl-propyl claim 1 , pyrrolidinyl-ethyl claim 1 , piperazinyl-propyl claim 1 , piperidinyl-sulfonyl-ethyl claim 1 , pyridazinyl claim 1 , (5-(4-methoxyphenyl)-1 claim 1 ,2 claim 1 ,4-oxadiazol-3-yl)methyl claim 1 , isoxazolyl claim 1 , piperidinyl-carbonyl-methyl claim 1 , 3-(N claim 1 ,N-bis(4-methoxyphenyl)sulfamoyl)propyl claim 1 , methyl-phenyl-sulfonyl claim 1 , cyanomethyl claim 1 , 2-oxo-2-(piperidin-1-ylamino)ethyl claim 1 , propyl-amino-carbonyl-methyl claim 1 , 2-(carboxymethylamino)-2-oxoethyl) claim 1 , bis-hydroxyethyl-amino-sulfonyl-ethyl claim 1 , carboxy-methyl-amino-carbonyl-methyl claim 1 , amino-carbonyl-ethyl claim 1 , amino-sulfonyl-ethyl claim 1 , amino-sulfonyl-propyl claim 1 , methyl-amino-ethyl claim 1 , piperidinyl-ethyl claim 1 , piperazinyl-ethyl claim 1 , methyl-sulfonyl-ethyl claim 1 , carboxy-methyl claim 1 , tetrazole-methyl claim 1 , benzyl claim 1 , 1 claim 1 ,2 claim 1 ,4-oxadiazole claim 1 , 1 claim 1 ,2 claim 1 ,4-oxadiazole-methyl claim 1 , 1 claim 1 ,2 claim 1 ,4-oxadiazole-ethyl claim 1 , isoxazole-methyl claim 1 , 2-(2-hydroxyethylamino)-2-oxoethyl claim 1 , dimethylamino-ethyl-amino-carbonyl-methyl claim 1 , hydroxyl-ethyl claim 1 , methoxy-ethyl claim 1 , hydroxyl-ethyl- ...

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15-08-2013 дата публикации

NEW SALT OF A PYRIMIDIN DERIVATIVE

Номер: US20130210848A1
Принадлежит: LABORATORIOS SENOSIAIN S.A. DE C.V.

The present invention relates to a salt of a pyrimidin derivative of the acid (3R,5S,6E)-7-[4-(4-fluorophenyl)-2-(N-methylmethanesulfonamide)-6-(propan-2-yl)pyrimidin-5-yl]-3,5-dihydroxyhept-6-enoic, to a method for preparing same and to the use thereof in formulating pharmaceutical formulations. 19-. (canceled)10. (3R ,5S ,6E)-7-[4-(4-fluorophenyl)-2-(N-methylmethanesulfonamide)-6-(propan-2-yl) pyrimidin-5-yl]-3 ,5-dihydroxihept-6-enoic amino acid salt , wherein the amino acid is lysine and wherein the bond formed between these two entities is a non-covalent bond.11. (3R ,5 S ,6E)-7-[4-(4-fluorophenyl)-2-(N-methylmethanesulfonamide)-6-(propan-2-yl)pyrimidin-5-yl]-3 ,5-dihydroxihept-6-enoic amino acid salt , wherein the amino acid is histidine and wherein the bond formed between these two entities in a non-covalent bond.12. A pharmaceutical composition comprising the salt of claim 10 , in combination with a pharmaceutically acceptable carrier.13. A pharmaceutical composition comprising the salt of claim 11 , in combination with a pharmaceutically acceptable carrier.14. A method of manufacturing a pharmaceutical composition comprising the step of adding the salt of to a pharmaceutically acceptable carrier.15. A method of manufacturing a pharmaceutical composition comprising the step of adding the salt of to a pharmaceutically acceptable carrier.16. The method according to claim 14 , wherein the pharmaceutical compositions are in the form of tablets or capsules.17. A method of manufacturing medicaments for the prevention or treatment of cardiovascular diseases comprising the step of adding the compound of to a pharmaceutically acceptable carrier.18. A process for synthesizing a rosuvastatin-lysine salt claim 10 , comprising the steps:a) subjecting the rosuvastatin calcium salt to a dissociation process; andb) mixing the acid rosuvastatin resulting from the previous step with an aqueous solution containing lysine for forming the salt in the presence of a methanol/ethyl ...

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15-08-2013 дата публикации

MOLECULES HAVING COMBINABLE GROUPS

Номер: US20130211057A1
Принадлежит: Arkema France

The present invention relates to nitrogenous associative molecules comprising at least one unit rendering them capable of associating with one another or with a filler by noncovalent bonds, and comprising a function capable of reacting with a polymer containing unsaturations so as to form a covalent bond with said polymer. 19-. (canceled)10. A compound comprising at least one group Q and at least one group A , wherein the groups Q and A are linked together by at least one spacer group Sp:wherein:group Q comprises an azodicarbonyl function;group A comprises an associative group comprising at least one nitrogen atom; andspacer group Sp is an atom or a group of atoms forming a link between group Q and group A.11. The compound of claim 10 , wherein the associative group is chosen from imidazolidinyl claim 10 , triazolyl claim 10 , ureyl claim 10 , bis-ureyl claim 10 , and ureidopyrimidyl groups.13. The compound of claim 12 , wherein X denotes an oxygen atom.15. The compound of claim 14 , wherein W represents a group of formula:{'br': None, 'R′—Z—'}{'sub': 1', '6, 'wherein R′ represents a C-Calkyl group.'}16. The compound of claim 15 , wherein R′ represents a C-Calkyl group.17. The compound of claim 15 , wherein R′ represents a methyl or ethyl group.20. The compound of claim 19 , wherein R represents a C-Calkoxyl group.21. The compound of claim 19 , wherein R represents a methyoxyl or ethoxyl group.22. The compound of claim 10 , wherein the spacer group Sp is a linear or branched C-Calkyl chain claim 10 , optionally comprising one or more heteroatoms chosen from nitrogen claim 10 , sulfur claim 10 , silicon claim 10 , and oxygen atoms.23. The compound of claim 22 , wherein the spacer group Sp is a linear or branched C-Calkyl chain claim 22 , optionally comprising one or more heteroatoms chosen from nitrogen claim 22 , sulfur claim 22 , silicon claim 22 , and oxygen atoms.24. The compound of claim 22 , wherein the spacer group Sp is a linear C-Calkyl chain optionally ...

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22-08-2013 дата публикации

Non-Natural Amino Acids

Номер: US20130217632A1
Автор: Dix Thomas A.

This invention relates in one aspect to non-natural desamino alkyl amino acid compounds, methods of making these compounds, and peptides containing these compounds. In one embodiment, the peptide is neurotensin (8-13) in which the N-terminus is an alpha-desamino, alpha-methyl-N,N-dimethyl-homolysine residue of the invention. 157-. (canceled)59. The compound of claim 58 , wherein the compound is a compound of Formula (I) and the stereochemistry at Cα is S.60. The compound of claim 58 , wherein the compound is a compound of Formula (I) and R claim 58 , R claim 58 , and Rare independently H or methyl.61. The compound of claim 58 , wherein the compound is a compound of Formula (I) and R is methyl.62. The compound of claim 58 , wherein the compound is:a compound of Formula (I), wherein n is 3, 4 or 5;a compound of Formula (II), wherein n is 2, 3, 4 or 5, and z is 2, 3 or 4;a compound of Formula (III), wherein n is 2, 3, 4 or 5, and z is z is 2, 3 or 4 ora compound of Formula (IV), wherein n is 2, 3 or 4.63. The compound of claim 58 , wherein the compound is selected from the group consisting of compounds 22-43 recited in Scheme 2.64. The compound of claim 58 , wherein the compound is a compound of Formula (I) and the protecting group is BOC (t-butoxy carbonyl) claim 58 , FMOC (fluorenylmethoxycarbonyl) claim 58 , Alloc (allyloxycarbonyl) claim 58 , CBZ (benzyloxycarbonyl) claim 58 , Pbf (2 claim 58 ,2 claim 58 ,4 claim 58 ,6 claim 58 ,7-pentamethyl-dihydrobenzofuran-5-sulfonyl) claim 58 , NO(nitro) claim 58 , Pmc (2 claim 58 ,2 claim 58 ,5 claim 58 ,7 claim 58 ,8-pentamethylchroman-6-sulfonyl) claim 58 , Mtr (4-methoxy-2 claim 58 ,3 claim 58 ,6-trimethylbenzenesulfonyl) claim 58 , or Tos (tosyl).66. The peptide of claim 65 , wherein the peptide is a known peptide claim 65 , further wherein the residue is covalently coupled through an amide bond to the N-terminus amine group of the known peptide claim 65 , a substitute for its corresponding analogous natural amino acid ...

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22-08-2013 дата публикации

5HT2C RECEPTOR MODULATORS

Номер: US20130217676A1
Автор: SMITH BRIAN, Smith Jeffrey
Принадлежит:

The present invention relates to novel compounds of Formula (I): 112.-. (canceled)13. A composition comprising (R)-8-chloro-1-methyl-2 ,3 ,4 ,5-tetrahydro-1H-3-benzazepine or a pharmaceutically acceptable salt thereof and ethyl acetate.15. The process of claim 14 , further comprising the step of: forming a pharmaceutically acceptable salt of a compound of Formula H.16. The process of claim 14 , further comprising the step of: preparing a composition comprising a compound of Formula H.17. The process of claim 15 , further comprising the step of: preparing a composition comprising a pharmaceutically acceptable salt of a compound of Formula H.18. A process for preparing 8-chloro-1-methyl-2 claim 15 ,3 claim 15 ,4 claim 15 ,5-tetrahydro-1H-3-benz azepine comprising the step of: deprotecting N-trifluoroacetyl-8-chloro-1-methyl-2 claim 15 ,3 claim 15 ,4 claim 15 ,5-tetrahydro-1H-3-benzazepine to form 8-chloro-1-methyl-2 claim 15 ,3 claim 15 ,4 claim 15 ,5-tetrahydro-1H-3-benzazepine.19. The process of claim 18 , wherein the N-trifluoroacetyl-8-chloro-1-methyl-2 claim 18 ,3 claim 18 ,4 claim 18 ,5-tetrahydro-1H-3-benzazepine is prepared by a process comprising the step of: hydrogenating N-trifluoroacetyl-8-chloro-1-methylene-2 claim 18 ,3 claim 18 ,4 claim 18 ,5-trihydro-1H-3-benzazepine.20. The process of claim 19 , wherein the N-trifluoroacetyl-8-chloro-1-methylene-2 claim 19 ,3 claim 19 ,4 claim 19 ,5-trihydro-1H-3-benzazepine is prepared by a processing the step of: reacting N-allyl claim 19 , N-trifluoroacetyl-2-iodo-4-chlorophenethylamine under conditions suitable for a Heck coupling reaction.21. The process of claim 18 , further comprising the step of: forming a pharmaceutically acceptable salt of the 8-chloro-1-methyl-2 claim 18 ,3 claim 18 ,4 claim 18 ,5-tetrahydro-1H-3-benzazepine.22. The process of claim 18 , further comprising the step of: preparing a composition comprising the 8-chloro-1-methyl-2 claim 18 ,3 claim 18 ,4 claim 18 ,5-tetrahydro-1H-3-benzazepine. ...

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22-08-2013 дата публикации

THERAPEUTIC COMPOUNDS

Номер: US20130217739A1
Принадлежит: ALLERGAN, INC.

Disclosed herein is a compound having a structure 2. The compound of wherein R claim 1 , R claim 1 , R claim 1 , and Rare independently selected from H claim 1 , methyl claim 1 , ethyl claim 1 , Calkyl claim 1 , and Calkyl claim 1 , F claim 1 , Cl claim 1 , Br claim 1 , —CHOH claim 1 , —CHNH claim 1 , —CHNH(Calkyl) claim 1 , —CN(Calkyl) claim 1 , —CHCN claim 1 , and CF.3. The compound of wherein Ris H or methyl.5. A method of reducing intraocular pressure comprising administering a compound of to a mammal in need thereof.6. A method of treating pain comprising administering a compound of to a mammal in need thereof. This application is a divisional application of U.S. patent application Ser. No. 12/673,351, filed Apr. 6, 2011, which is a national stage application under 35 U.S.C. §371 of PCT patent application PCT/US2008/073110, filed Aug. 14, 2008 which claims the benefit of U.S. Provisional Application Ser. No. 60/955,972, filed Aug. 15, 2007, which is hereby incorporated by reference in its entirety.There is a continuing need for alpha adrenergic compounds for treating pain, glauco ma and other conditions.Disclosed herein is a compound having a structurewherein X is O, S, or NH; n is 2 or 3; R, R, R, and Rare stable moieties independently consisting of: from 0 to 4 carbon atoms, from 0 to 10 hydrogen atoms, from 0 to 2 oxygen atoms, from 0 to 1 sulfur atoms, from 0 to 1 nitrogen atoms, from 0 to 3 fluorine atoms, from 0 to 1 chlorine atoms, and from 0 to 1 bromine atoms; and Ris H or Calkyl.These compounds are useful for the treatment of pain, glaucoma, and the reduction of intraocular pressure. The compound is incorporated into a dosage form or a medicament and administered to the mammal in need thereof. For example, a liquid composition may be administered as an eye drop for the treatment of glaucoma or lowering intraocular pressure. A solid dosage form may also be administered orally for any of these conditions. Other types of dosage forms and medicaments are ...

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22-08-2013 дата публикации

METRONIDAZOLE ESTERS FOR TREATING ROSACEA

Номер: US20130217740A1
Принадлежит: GALDERMA RESEARCH & DEVELOPMENT

A compound of formula (I): 2. The compound as defined in claim 1 , wherein the compound is incorporated into a medicament.3. The compound as defined in claim 1 , wherein the compound is effective in treating rosacea.4. The compound as defined in claim 1 , wherein the compound is effective in treating an inflammatory pathology.5. The compound as defined in claim 1 , wherein the salt of the compound of formula (I) or of an enantiomer thereof is a salt of the compound or an enantiomer thereof with a pharmaceutically acceptable acid.6. The compound as defined in claim 1 , wherein the pharmaceutically acceptable acid is selected from the group consisting of:a) a pharmaceutically acceptable inorganic acid; andb) a pharmaceutically acceptable organic acid.7. The compound as defined in claim 1 , wherein the compound is selected from the group consisting of a compound of formula (I) claim 1 , a hydrochloride of the compound of formula (I) claim 1 , a citrate of the compound of formula (I) claim 1 , a salicylate of the compound of formula (I) claim 1 , a benzoate of the compound of formula (I) claim 1 , and an S enantiomer of any one of these compounds.8. The compound as defined in claim 1 , wherein the compound is 2-(2-methyl-5-nitroimidazol-1-yl)ethyl (S)-2-(2-fluorobiphenyl-4-yl)propionate.9. A pharmaceutical composition for topical application comprising a compound as defined in and a pharmaceutical carrier.10. The composition as defined in claim 9 , said composition being in the form of a solution claim 9 , a gel or an emulsion.11. The composition as defined in claim 9 , wherein the compound is present in an amount of 0.001% to 10% by weight relative to the total weight of the composition.12. The compound as defined in claim 6 , wherein the pharmaceutically acceptable inorganic acid is selected from the group consisting of hydrochloric acid claim 6 , sulfuric acid claim 6 , phosphoric acid claim 6 , nitric acid claim 6 , and hydrobromic acid.13. The compound as defined ...

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12-09-2013 дата публикации

METHOD FOR MANUFACTURE OF 2-OXOIMIDAZOLIDINES

Номер: US20130237705A1
Принадлежит:

A method for the manufacture of 2-oxoimidazolidines comprising the steps of converting an isocyanate and an amine to a urea, and then performing a ring closure of the urea to yield the 2-oxoimidazolidine is disclosed. The 2-oxoimidazolidines produced may then be used in the production of Pramiconazole and other structurally related compounds. 2. The method of further comprising the step of:converting said 2-oxoimidazolidine to Pramiconazole.3. The method of claim 1 , wherein said amine of Formula IV contains a chiral center and is substantially comprised of a single enantiomer to produce said 2-oxoimidazolidine of Formula I in optically pure form.4. The method of claim 1 , wherein said Rand said Rform a bivalent radical —R-R— chosen from —CHCH— claim 1 , —CHCHCH— claim 1 , —CH(CH)CH— and —CH(CH)CH—. This application is a continuation-in-part and claims priority to U.S. Ser. No. 12/714,614, entitled METHOD FOR MANUFACTURE OF 2-OXOIMIDAZOLIDINES, filed Mar. 1, 2010 and is incorporated herein by reference.Pramiconazole, a triazole antifungal compound, may be used for the treatment of acute and chronic seborrheic dermatitis and other fungal skin infections in humans. The structure of Pramiconazole is provided below in Structure I:Pramiconazole may be produced from 2-oxoimidazolidine, which is shown below in Structure II in a generalized chemical structure. The 2-oxoimidazolidine ring within the Pramiconazole is one of two requisite structural components for providing anti-fungal activity.As a result of the favorable clinical indications of Pramiconazole and structurally related drugs, there may be an interest in methods that provide 2-oxoimidazolidine, especially those methods that may be more cost effective relative to the prior art.This Summary is provided to introduce a selection of concepts in a simplified form that are further described below in the Detailed Description. This Summary is not intended to identify key factors or essential features of the claimed ...

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19-09-2013 дата публикации

BENZIMIDAZOLE DERIVATIVES USEFUL AS TRPM8 CHANNEL MODULATORS

Номер: US20130245085A1
Принадлежит: Janssen Pharmaceutica, NV

Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: 18-. (canceled)11. A method as in claim 10 , wherein the inflammatory pain is due to inflammatory bowel disease claim 10 , visceral pain claim 10 , migraine claim 10 , post operative pain claim 10 , osteoarthritis claim 10 , rheumatoid arthritis claim 10 , back pain claim 10 , lower back pain claim 10 , joint pain claim 10 , abdominal pain claim 10 , chest pain claim 10 , labor claim 10 , musculoskeletal diseases claim 10 , skin diseases claim 10 , toothache claim 10 , pyresis claim 10 , burn claim 10 , sunburn claim 10 , snake bite claim 10 , venomous snake bite claim 10 , spider bite claim 10 , insect sting claim 10 , neurogenic bladder claim 10 , interstitial cystitis claim 10 , urinary tract infection claim 10 , rhinitis claim 10 , contact dermatitis/hypersensitivity claim 10 , itch claim 10 , eczema claim 10 , pharyngitis claim 10 , mucositis claim 10 , enteritis claim 10 , irritable bowel syndrome claim 10 , cholecystitis claim 10 , pancreatitis claim 10 , postmastectomy pain syndrome claim 10 , menstrual pain claim 10 , endometriosis claim 10 , sinus headache claim 10 , tension headache claim 10 , or arachnoiditis.12. A method as in claim 10 , wherein the inflammatory pain is inflammatory hyperalgesia.13. A method as in claim 12 , wherein the inflammatory hyperalgesia is inflammatory somatic hyperalgesia or inflammatory visceral hyperalgesia.14. A method as in claim 12 , wherein the inflammatory hyperalgesia is due to inflammation claim 12 , osteoarthritis claim 12 , rheumatoid arthritis claim 12 , back pain claim 12 , joint pain claim 12 , abdominal pain claim 12 , musculoskeletal diseases claim 12 , skin diseases claim 12 , post operative pain claim 12 , headaches claim 12 , fibromyalgia claim 12 , toothache claim 12 , burn claim 12 , sunburn claim 12 , insect sting ...

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19-09-2013 дата публикации

DUAL-ACTING IMIDAZOLE ANTIHYPERTENSIVE AGENTS

Номер: US20130245087A1
Принадлежит:

The invention is directed to compounds having the formula: 125-. (canceled)26. A pharmaceutical composition comprising the compound of and a pharmaceutically acceptable carrier.27. The pharmaceutical composition of further comprising a second therapeutic agent selected from the group consisting of diuretics claim 26 , βadrenergic receptor blockers claim 26 , calcium channel blockers claim 26 , angiotensin-converting enzyme inhibitors claim 26 , ATreceptor antagonists claim 26 , neprilysin inhibitors claim 26 , non-steroidal anti-inflammatory agents claim 26 , prostaglandins claim 26 , anti-lipid agents claim 26 , anti-diabetic agents claim 26 , anti-thrombotic agents claim 26 , renin inhibitors claim 26 , endothelin receptor antagonists claim 26 , endothelin converting enzyme inhibitors claim 26 , aldosterone antagonists claim 26 , angiotensin-converting enzyme/neprilysin inhibitors claim 26 , vasopressin receptor antagonists claim 26 , and combinations thereof.2830-. (canceled)31. A method for causing regression of claim 39 , suppressing claim 39 , or alleviating the symptoms of hypertension claim 39 , comprising administering to a patient a therapeutically effective amount of a compound of .32. A method for causing regression of claim 39 , suppressing claim 39 , or alleviating the symptoms of heart failure claim 39 , comprising administering to a patient a therapeutically effective amount of a compound of .33. A method of causing regression of claim 39 , suppressing claim 39 , or alleviating the symptoms of chronic kidney disease claim 39 , comprising administering to a patient a therapeutically effective amount of a compound of .3438-. (canceled)39. 4′-{4-Cyclopropyl-2-ethoxy-5-[((S)-2-mercapto-4-methylpentanoylamino)-methyl]imidazol-1-ylmethyl}-3′-fluorobiphenyl-2-carboxylic acid claim 39 , or a pharmaceutically acceptable salt thereof. This application claims the benefit of U.S. Provisional Application No. 60/925,931, filed on Apr. 24, 2007; the entire ...

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19-09-2013 дата публикации

AMINE COMPOUND AND USE FOR SAME

Номер: US20130245280A1
Принадлежит: KUREHA CORPORATION

Provided is an ester of 3-[(4-dipropylamino-butyl)(4-{[(1H-imidazole-2-ylmethyl)(1-methyl-1H-imidazole-2-ylmethyl)amino]methyl}benzyl)amino]propionic acid which is easily hydrolyzed in serum. The amine compound of the present invention is an ester compound represented by general formula (1). (In general formula (1), n is 1-4, and Rand Rrepresent an alkyl group having 1-3 carbon atoms.) 2. An amine compound or a pharmacologically acceptable salt thereof according to claim 1 , wherein n in the general formula (1) is 2 or 3.3. An amine compound or a pharmacologically acceptable salt thereof according to claim 2 , wherein n in the general formula (1) is 2 claim 2 , and Rand Rin the general formula (1) represent a methyl group or an ethyl group.4. An amine compound or a pharmacologically acceptable salt thereof according to claim 1 , wherein the amine compound represented by the general formula (1) is 2-dimethylaminoethyl 3-[(4-dipropylaminobutyl)(4-{[(1H-imidazol-2-ylmethyl)(1-methyl-1H-imidazol-2-ylmethyl)amino]methyl}benzyl)amino]propionate.5. An amine compound or a pharmacologically acceptable salt thereof according to claim 4 , wherein the pharmacologically acceptable salt is a citrate of 2-dimethylaminoethyl 3-[(4-dipropylaminobutyl)(4-{[(1H-imidazol-2-ylmethyl)(1-methyl-1H-imidazol-2-ylmethyl)amino]methyl}benzyl)amino]propionate.6. A pharmaceutical composition comprising as an active ingredient the amine compound or the pharmacologically acceptable salt thereof according to .7. A pharmaceutical composition according to claim 1 , comprising as a prodrug the amine compound or the pharmacologically acceptable salt thereof according to .8. A CXCR4 antagonist comprising as an active ingredient the amine compound or the pharmacologically acceptable salt thereof according to .9. An antiviral drug comprising as an active ingredient the amine compound or the pharmacologically acceptable salt thereof according to .10. An anti-rheumatic disease agent based on CXCR4 ...

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26-09-2013 дата публикации

CYCLIC N,N'-DIARYLTHIOUREA - ANDROGEN RECEPTOR ANTAGONIST, ANTI BREAST CANCER COMPOSITION AND USE THEREOF

Номер: US20130252992A1
Принадлежит:

The present invention relates to novel cyclic N,N′-diarylurea-androgen receptor antagonist, anti-cancer agent, pharmaceutical composition, medicament, and method for treatment of breast cancer disease. 4. The composition of in the form of a tablet claim 1 , a capsule claim 1 , or an injection placed in a pharmaceutically acceptable package.5. A method for treating a breast cancer in a subject comprising administering an effective dose of a pharmaceutical composition according to to a subject in need thereof. This application is a continuation-in-part of U.S. application Ser. No. 13/811,282 filed Jan. 21, 2013, which claims benefit of priority to the International application PCT/RU2011/000476 filed Jul. 1, 2011, which claims benefit of foreign priority to the Russian Federation application RU 2010130618 of Jul. 22, 2010. The priority applications are hereby incorporated by reference in their entirety.The invention relates to novel cyclic N,N′-diarylthioureas and N,N′-diarylureas-androgen receptor antagonists, anticancer agent, pharmaceutical composition, medicament and method for treatment of cancer including prostate cancer.There are known androgen receptor antagonists which are—1,3-diaryl-5,5-dimethyl-2-thioxoimidazolidin-4-ones I, 5,7-diaryl-6-thioxo-5,7-diazaspiro[3,4]octan-8-ones II and 1,3-diaryl-2-thioxo-1,3-diazaspiro[4,4]nonan-4-ones III exhibiting anticancer activity [WO2006124118, WO2007127010]. Amongst these compounds the most promoted is 4-[3-[4-cyano-3-(trifluoromethyl)phenyl]-5,5-dimethyl-4-oxo-2-thioxoimidazolidin-1-yl]-2-fluoro-N-methylbenzamide MDV3100 (androgen receptor antagonist with IC=36 nM), which is now in the III phase of clinical trials as medicament for prostate cancer treatment [2009, 31(6), 609].Searching for highly effective anticancer medicaments exhibiting enhanced activity and reduced toxicity, is still one of the main directions in the development of novel pharmacological remedies for cancer treatment, including prostate cancer. In ...

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10-10-2013 дата публикации

HETEROCYCLIC SULFONAMIDES

Номер: US20130267537A1
Принадлежит: CYTOKINETICS, INC.

Certain substituted sulfonamide derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure. 114-. (canceled)16. The compound of claim 15 , or a pharmaceutically acceptable salt thereof claim 15 , wherein Ris a phenyl claim 15 , isoxazolyl claim 15 , oxazolyl claim 15 , pyridinyl claim 15 , pyrazinyl claim 15 , pyrimidinyl claim 15 , tetrazol-5-yl claim 15 , thiazolyl claim 15 , thiadiazolyl or imidazolyl group claim 15 , which is optionally substituted with a halogen claim 15 , lower alkoxy claim 15 , aryl or heteroaryl group.17. The compound of claim 15 , or a pharmaceutically acceptable salt thereof claim 15 , wherein Ris a [1 claim 15 ,3 claim 15 ,4]thiadiazol-2-yl group which is optionally substituted with a phenyl group.18. The compound of claim 15 , or a pharmaceutically acceptable salt thereof claim 15 , wherein Ris 5-phenyl-[1 claim 15 ,3 claim 15 ,4]thiadiazol-2-yl.19. The compound of claim 18 , or a pharmaceutically acceptable salt thereof claim 18 , wherein{'sup': '4', 'Rchloro; and'}{'sup': 5', '6', '7, 'R, Rand Rare hydrogen.'}20. The compound of claim 15 , or a pharmaceutically acceptable salt thereof claim 15 , wherein Ris a 1H-imidazol-2-yl group.21. The compound of claim 20 , or a pharmaceutically acceptable salt thereof claim 20 , wherein{'sup': '4', 'Ris chloro; and'}{'sup': 5', '6', '7, 'R, Rand Rare hydrogen.'}22. The compound of claim 15 , or a pharmaceutically acceptable salt thereof claim 15 , wherein Ris thiazol-2-yl.23. The compound of claim 22 , or a pharmaceutically acceptable salt thereof claim 22 , wherein{'sup': '4', 'Ris chloro; and'}{'sup': 5', '6', '7, 'R, Rand Rare hydrogen.'}24. The compound of claim 15 , or a pharmaceutically acceptable salt thereof claim 15 , wherein{'sup': '4', 'Ris chloro; and'}{'sup': 5', '6', '7, 'R, Rand Rare hydrogen.'}25. The compound of claim 15 , or a pharmaceutically ...

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17-10-2013 дата публикации

CANCER TARGETING USING CARBONIC ANHYDRASE ISOFORM IX INHIBITORS

Номер: US20130274305A1
Принадлежит:

The present invention concerns novel carbonic anhydrase IX inhibitors comprising a nitroimidazole moiety and their use in therapy of hypoxic conditions, in particular cancer treatment, especially chemotherapy and radiotherapy. The compounds of the invention have an increased specificity for the carbonic anhydrase IX enzyme compared to the art. The present invention relates to novel nitroimidazole derivates represented by formula (1). 135-. (canceled)38. The compound or salt according to wherein Rand Rare claim 36 , each independently claim 36 , H or CH.39. The compound or salt according to wherein R═R═H.40. The compound or salt according to wherein R═R═R.41. The compound or salt according to wherein R═R═R═H.42. The compound or salt according to wherein Ror Ris sulfonamide.43. The compound or salt according to wherein n=0 claim 36 , 1 or 2.44. The compound or salt according to wherein R═H and R═CH.45. The compound or salt according to wherein n=1.46. The compound or salt according to wherein X is sulfamate or sulfamide.471. The compound or salt according to claim wherein Y═S.48. The pharmaceutical composition comprising a compound or salt of and a pharmaceutically acceptable carrier.49. A method of inhibiting a carbonic anhydrase (CA) enzyme in a subject in need thereof comprising administering an effective amount of a compound or salt of .50. A method of treating a subject afflicted with a disease characterized by overexpression of one or more carbonic anhydrase enzymes claim 36 , comprising administering to the subject an effective amount of a compound or salt of .51. The method of claim 50 , wherein the disease is a pre-cancerous or cancerous disease claim 50 , wherein said disease is characterized by overexpression of MN/CA IX protein.52. The method of claim 51 , wherein the cancerous disease is a cancer of breast claim 51 , brain claim 51 , kidney claim 51 , colorectum claim 51 , lung claim 51 , head and neck or bladder.53. The method of claim 51 , wherein the ...

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24-10-2013 дата публикации

Process for producing alpha-hydroxyketone compound

Номер: US20130281709A1
Автор: Koji Hagiya
Принадлежит: Sumitomo Chemical Co Ltd

An object of the present invention is to produce an α-hydroxyketone compound easily and effectively. Provided is a process for producing an α-hydroxyketone compound comprising a stirring step of stirring one or more aldehyde compounds or polymers thereof in the presence of a base and an imidazolinium salt represented by the formula (1): wherein R 1 and R 2 each independently represent a hydrogen atom, an alkyl group optionally having a substituent or an aryl group optionally having a substituent, or R 1 and R 2 are bound to each other to form a ring together with carbon atoms to which they bind, R 3 and R 4 each independently represent an aryl group having one or more electron withdrawing groups, and X − represents an anion.

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31-10-2013 дата публикации

HETEROARYLTHIO DERIVATIVES AND ANALOGUES

Номер: US20130289047A1
Автор: Fick David, Helton David
Принадлежит: EPIOMED THERAPEUTICS, INC.

Heteroarylthio compounds covalently linked to an arylpiperazine moiety for the treatment of neurological conditions. 7. The heteroarylthio compound of claim 1 , wherein m is selected from the group consisting of 2 claim 1 , 3 claim 1 , and 4.8. The heteroarylthio compound of claim 1 , wherein L is substituted with alkyl groups.14. The heteroarylthio compound of claim 1 , wherein the compound is selected from the group consisting of:1-{2-[(1-methyl-1H-imidazol-2-yl)thio]ethyl}-4-[3-(trifluoromethyl)phenyl]piperazine;1-[2-(5-pyridin-4-yl-[1,3,4]oxadiazol-2-ylsulfanyl)ethyl]-4-(3-trifluoromethylphenyl)piperazine;1-{3-[(1-methyl-1H-imidazol-2-yl)thio]propyl}-4-[3-chlorophenyl]piperazine;1-[3-(1-phenyl-1H-tetrazol-5-ylsulfanyl)propyl]-4-(3-chlorophenyl)piperazine; and1-[2-(5-pyridin-4-yl-[1,3,4]oxadiazol-2-ylsulfanyl)ethyl]-4-(3-trifluoromethylphenyl)piperazine.1518-. (canceled)19. The heteroarylthio compound of claim 1 , wherein the compound is selected from the group consisting of:4-{4-[3-(1-methyl-1H-imidazol-2-ylsulfanyl)propyl]piperazin-1-yl}furo[3,2-c]pyridine;4-{4-[3-(1-phenyl-1H-tetrazol-5-ylsulfanyl)propyl]piperazin-1-yl}furo[3,2-c]pyridine; and4-{4-[3-(5-pyridin-4-yl-[1,3,4]oxadiazol-2-sulfanyl)propyl]piperazin-1-yl}furo[3,2-c]pyridine.2021-. (canceled)22. A pharmaceutical composition comprising the heteroarylthio compound of and one or more pharmaceutically acceptable excipients.23. A method of treating a neurological condition claim 1 , comprising the step of administering the heteroarylthio compound of to a subject in need thereof.24. (canceled) This patent application claims the benefit of priority from U.S. Patent Application No. 61/393,349, filed on Oct. 14, 2010 and entitled HETEROARYLTHIO DERIVATIVES AND ANALOGUES. The disclosure of this application is hereby incorporated by reference herein in its entirety.The serotonin receptors, also known as 5-hydroxytryptamine receptors or 5-HT receptors, are a group of G protein-coupled receptors (GPCRs) and ...

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31-10-2013 дата публикации

ESTER PRO-DRUGS OF [3-(1-(1H-IMIDAZOL-4-YL)ETHYL)-2-METHYLPHENYL] METHANOL FOR LOWERING INTRAOCULAR PRESSURE

Номер: US20130289088A1
Принадлежит:

The present invention relates to method of lowering intraocular pressure in a subject in need of such treatment, which comprises administering a therapeutically effective amount of a composition comprising a ester pro-drugs of [3-(1-(1H-imidazol-4-yl)ethyl)-2-methylphenyl]methanol, of enantiomers thereof, of tautomers thereof, pharmaceutical compositions containing them and their use as pharmaceuticals. 2. The pharmaceutical composition according to claim 1 , wherein the compound having a structure of Formula II is selected from:iso-Butyric acid 3-[(S)-1-(1H-imidazol-4-yl)-ethyl]-2-methyl-benzyl ester;2,2-Dimethyl-propionic acid 3-[(S)-1-(1H-imidazol-4-yl)ethyl]-2-methyl-benzyl ester;Acetic acid 3-[(S)-1-(1H-imidazol-4-yl)ethyl]-2-methyl-benzyl ester;Benzoic acid 3-[(S)-1-(1H-imidazol-4-yl)ethyl]-2-methyl-benzyl ester;3-Methyl-butyric acid 3-[(S)-1-(1H-imidazol-4-yl)ethyl]-2-methyl-benzyl ester;3-Phenyl-propionic acid 3-[(S)-1-(1H-imidazol-4-yl)ethyl]-2-methyl-benzyl ester;2-Amino-3-methyl-butyric acid 3-[(S)-1-(1H-imidazol-4-yl)-ethyl]-2-methyl-benzyl ester;2-(2-Amino-3-methyl-butyrylamino)-3-methyl-butyric acid 3-[(S)-1-(1H-imidazol-4-yl)-ethyl]-2-methyl-benzyl ester;2-(2-Amino-acetylamino)-3-methyl-butyric acid 3-[(S)-1-(1H-imidazol-4-yl)-ethyl]-2-methyl-benzyl ester; and2-Amino-3-phenyl-propionic acid 3-[(S)-1-(1H-imidazol-4-yl)-ethyl]-2-methyl-benzyl ester.3. The pharmaceutical composition according to claim 1 , wherein the buffering agents include: sodium chloride claim 1 , potassium chloride claim 1 , calcium chloride dihydrate claim 1 , magnesium chloride hexahydrate claim 1 , boric acid and sodium borate decahydrate.4. The pharmaceutical composition according to claim 1 , wherein the viscosity building agents include: polyvinyl alcohol claim 1 , polyvinyl pyrrolidone claim 1 , methyl cellulose claim 1 , hydroxypropyl methylcellulose claim 1 , hydroxyethyl cellulose claim 1 , carboxymethyl cellulose and hydroxypropyl cellulose.5. The pharmaceutical ...

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07-11-2013 дата публикации

METHOD FOR CONTROLLING CLUBROOT

Номер: US20130296393A1
Принадлежит: ISHIHARA SANGYO KAISHA, LTD.

In order to control the clubroot of brassica vegetables which is settled-planted in a farm field, it is necessary to previously treat the seedling with a chemical before settled planting or treat the soil with a chemical, but the clubroot is sometimes not controlled depending on the weather or soil conditions. In addition, the treatment with a fungicidal compound at a high concentration causes a problem of phytotoxicity or crop persistence. An object of the present invention is to solve these problems and provide a method for easily and simply controlling clubroot without causing a problem of phytotoxicity or crop persistence. The present invention provides a method for controlling clubroot, comprising applying cyazofamid to brassica vegetables after seeding or settled planting in a farm field. 1. A method for controlling clubroot , comprising applying cyazofamid to brassica vegetables after seeding or settled planting in a farm field.2. The method according to claim 1 , wherein cyazofamid is applied by a foliage application or a soil treatment.3. The method according to claim 1 , wherein cyazofamid is applied by a soil treatment.4. The method according to claim 3 , wherein the soil treatment is a soil drench.5. The method according to or claim 3 , wherein the soil treatment comprises spraying cyazofamid to cultivation soil at 0.05 to 50 g/m.6. The method according to claim 4 , which comprises (1) diluting a suspension concentrate of cyazofamid with water to a concentration of 1 to 1 claim 4 ,000 ppm and then (2) treating the base of brassica vegetables after seeding or settled plantation by drenching the chemical solution obtained in (1) at 1 to 1 claim 4 ,000 ml per plant.7. The method according to claim 1 , wherein cyazofamid is applied to the brassica vegetable within 30 days after seeding or settled planting in the farm field.8Brassica campestrisBrassica rapaBrassica campestrisBrassica rapaBrassica rapaBrassica campestris. The method according to claim 1 , ...

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14-11-2013 дата публикации

METHOD FOR PREPARING AMINOETHYL IMIDAZOLIDINONE AND THE THIOCARBONYL THEREOF

Номер: US20130303784A1
Принадлежит:

The present invention relates to a method for preparing 1-(2-aminoethyl)imidazolidin-2-one or the thiocarbonyl thereof, and also to the product that can be obtained according to this method, and which has a purity of at least 98%, and to the uses thereof. 2. The method as claimed in claim 1 , wherein the DETA/urea compound molar ratio is between 1.3 and 1.7.3. The method as claimed in claim 1 , wherein the distillation is carried out at a temperature claim 1 , at the bottom of the column claim 1 , of between 100 and 140° C.4. The method as claimed in claim 1 , wherein the distillation is carried out under a pressure of from 1 to 30 mbar.5. The method as claimed in claim 1 , wherein the distillation is a molecular distillation.6. The method as claimed in claim 5 , wherein the molecular distillation process comprises the following two successive steps:1—a first distillation at a temperature of from 110° C. to 120° C., under a pressure of from 1 to 2 mbar,2—a second distillation at a temperature between more than 120° C. and 135° C., under a pressure of from 0.01 to 0.02 mbar.7. The method as claimed in claim 1 , wherein the urea compound is introduced sequentially into the reaction medium.8. The method as claimed in claim 1 , wherein the urea compound is introduced into the heated reaction medium containing the DETA.9. The method as claimed in claim 1 , wherein the reaction is carried out at a temperature of between 100 and 250° C.10. The method as claimed in claim 9 , wherein the reaction medium is brought claim 9 , during the reaction claim 9 , from 110-140° C. to 150-190° C.11. The method as claimed in claim 1 , wherein the DETA removed is recycled into the process.12. The method as claimed in claim 1 , wherein the DETA/urea compound molar ratio is between 1.2 and 1.9.13. The method as claimed in claim 1 , wherein the DETA/urea compound molar ratio is between 1.3 and 1.6.14. The method as claimed in claim 1 , wherein the distillation is carried out at a temperature ...

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05-12-2013 дата публикации

New 6,11-dihydro-5H-benzo[d]imidazo[1,2-a]azepines derivatives as histamine H4 receptor ligands

Номер: US20130324506A1
Принадлежит:

The present patent application concerns new ligands of the H4-receptor, their process of preparation and their therapeutic use. 5. A compound according to where R1 is N-Me-piperidin-4-yl; as well as its enantiomers claim 1 , diastereomers claim 1 , mixtures thereof and pharmaceutically acceptable salts claim 1 , tautomers claim 1 , hydrates and solvates.6. A compound according to chosen from:4-(1-Methyl-piperidin-4-yloxy)-2-trifluoromethyl-9,10-dihydro-4H-3,10a-diaza-benzo[f]azulene4-(1-Methyl-piperidin-4-yloxy)-1-trifluoromethyl-9,10-dihydro-4H-3,10a-diaza-benzo[f]azulene2-Iodo-4-(1-methyl-piperidin-4-yloxy)-9,10-dihydro-4H-3,10a-diaza-benzo[f]azulene1-Iodo-4-(1-methyl-piperidin-4-yloxy)-9,10-dihydro-4H-3,10a-diaza-benzo[f]azulene4-(1-Methyl-piperidin-4-yloxy)-2-phenyl-9,10-dihydro-4H-3,10a-diaza-benzo[f]azulene4-(1-Methyl-piperidin-4-yloxy)-2-p-tolyl-9,10-dihydro-4H-3,10a-diaza-benzo[f]azulene4-(1-Methyl-piperidin-4-yloxy)-2-m-tolyl-9,10-dihydro-4H-3,10a-diaza-benzo[f]azulene2-Iodo-4-(1-methyl-azetidin-3-ylmethoxy)-9,10-dihydro-4H-3,10a-diaza-benzo[f]azulene4-(1-Methyl-piperidin-4-yloxy)-2-o-tolyl-9,10-dihydro-4H-3,10a-diaza-benzo[f]azulene4-(1-Methyl-piperidin-4-yloxy)-2-vinyl-9,10-dihydro-4H-3,10a-diaza-benzo[f]azulene2-(4-tert-Butyl-phenyl)-4-(1-methyl-piperidin-4-yloxy)-9,10-dihydro-4H-3,10a-diaza-benzo[f]azulene1-{4-[4-(1-Methyl-piperidin-4-yloxy)-9,10-dihydro-4H-3,10a-diaza-benzo[f]azulen-2-yl]-phenyl}-ethanone4-(1-Methyl-piperidin-4-yloxy)-2-thiophen-3-yl-9,10-dihydro-4H-3,10a-diaza-benzo[f]azulene2-Ethyl-4-(1-methyl-piperidin-4-yloxy)-9,10-dihydro-4H-3,10a-diaza-benzo[f]azulene2-(4-Methoxy-phenyl)-4-(1-methyl-piperidin-4-yloxy)-9,10-dihydro-4H-3,10a-diaza-benzo[f]azulene4-(1-Methyl-piperidin-4-yloxy)-2-(4-trifluoromethoxy-phenyl)-9,10-dihydro-4H-3,10a-diaza-benzo[f]azulene4-[4-(1-Methyl-piperidin-4-yloxy)-9,10-dihydro-4H-3,10a-diaza-benzo[f]azulen-2-yl]-phenylamine2-(4-Methanesulfonyl-phenyl)-4-(1-methyl-piperidin-4-yloxy)-9,10-dihydro-4H-3,10a-diaza-benzo ...

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12-12-2013 дата публикации

SPECIFIC DIARYLHYDANTOIN AND DIARYLTHIOHYDANTOIN COMPOUNDS

Номер: US20130331421A1
Принадлежит: MEDIVATION PROSTATE THERAPEUTICS, INC.

Compositions, such as pharmaceutical compositions, comprising specific diarylhydantoin and diarylthiohydantoin compounds, or salts or solvates thereof, are provided. Isolated and purified forms of the compounds are also described, as are unit dosage forms, compositions of substantially pure compound and kits comprising the compounds. The compounds and pharmaceutical compositions thereof may find use in the prevention and/or treatment of a variety of conditions, including prostate cancer, Parkinson's disease, Alzheimer's disease, and others. 2. The pharmaceutical composition of claim 1 , wherein X is S and Ris OH or NH.3. The pharmaceutical composition of claim 1 , wherein X is O and Ris OH claim 1 , NHor NHMe.10. The composition of claim 9 , wherein X is S and Ris OH or NH.11. The composition of claim 9 , wherein X is O and Ris OH claim 9 , NHor NHMe.1716. The composition of any of - claims 9 , wherein the composition contains less than about 10 weight percent impurity.19. The method of claim 18 , wherein X is S and Ris OH or NH.20. The method of claim 18 , wherein X is O and Ris OH claim 18 , NHor NHMe.2120. The method of any of - claims 18 , wherein the therapy is the treatment of prostate cancer.2220. The method of any of - claims 18 , wherein the therapy is the treatment of Parkinson's disease or Alzheimer's disease.24. The kit of claim 23 , wherein X is S and Ris OH or NH.25. The kit of claim 23 , wherein X is O and Ris OH claim 23 , NHor NHMe.2625. The kit of any of - claims 23 , wherein the kit further comprises instructions for use.27. The kit of any of claim 26 , wherein the instructions are for use of the compound in the treatment of prostate cancer.28. The kit of claim 26 , wherein the instructions are for use of the compound in the treatment of Parkinson's disease or Alzheimer's disease.30. The unit dosage form of claim 29 , wherein X is S and Ris OH or NH.31. The unit dosage form of claim 29 , wherein X is O and Ris OH claim 29 , NHor NHMe.33. The ...

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19-12-2013 дата публикации

Substituted Imidazoline Compounds

Номер: US20130338372A1
Автор: Hamby James, Tepe Jetze
Принадлежит:

The invention relates to compositions comprising substituted imidazoline compounds including prodrugs, and salts thereof. In some embodiments, the invention relates to the use of these compositions as therapeutic agents, preferably for the treatment of arthritis or cancer. In further embodiments, The invention relates to the pharmaceutical compositions with effective amounts of substituted imidazoline compounds disclosed herein that function as agonist or antagonists of the genetic expression or interactions with transcription factor NF-κB. 1. A compound having the following formula: The invention relates to compositions comprising substituted imidazoline compounds including prodrugs, enantiomers and salts thereof. In some embodiments, the invention relates to the use of these compositions as therapeutic agents, preferably for the treatment of arthritis or cancer. In further embodiments, The invention relates to the pharmaceutical compositions with effective amounts of substituted imidazoline compounds disclosed herein that function as agonist or antagonists of the genetic expression or interactions with transcription factor NF-kB.The NF-kappaB/Rel signaling system is a paradigm for gene activation in response to inflammatory and menacing stimuli. A growing body of evidence provides a significant role of NF-kappaB for the onset of autoimmune diseases and different types of cancer. NF-kappaB is a drug target for the adjuvant therapy of these diseases. U.S. Pat. No. 6,878,735 discloses multi-substituted imidazolines as inhibitors or NF-kB. However, there remains a need for improved NF-kB inhibitors that have optimized therapeutic properties such as improved efficacy and reduced adverse drug reactions.The invention relates to compositions comprising substituted imidazoline compounds including prodrugs, and salts thereof. In some embodiments, the invention relates to the use of these compositions as therapeutic agents, preferably for the treatment of arthritis or cancer ...

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02-01-2014 дата публикации

FAMILY OF POLYAMINE ARYLETHYLAMIDE COMPOUNDS, AND THEIR COSMETIC OR DERMOCOSMETIC USE

Номер: US20140005244A1
Принадлежит: EXSYMOL

The invention relates to a family of stable polyamine arylethylamide compounds, and to the use of these compounds as agents inhibiting DNA damages induced by by-products of the non-enzymatic glycosylation of skin tissues. 2. The compound according to claim 1 , which is selected from the group consisting of N-((4-imidazolyl)ethyl)-α claim 1 ,γ-diaminobutanamide claim 1 , N-((4-imidazolyl)ethyl)-α claim 1 ,β-diamino-propanamide and pharmaceutically acceptable salts of these compounds.3. The compound according to claim 2 , which is N--((4-imidazolyl)ethyl)-α claim 2 ,β-diaminopropanamide or a pharmaceutically acceptable salt thereof.4. A cosmetic or dermocosmetic composition claim 1 , which comprises as main active ingredient a compound as defined in claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , in combination with an additive which is physiologically acceptable with skin.5. The composition according to claim 4 , wherein said compound is selected from the group consisting of N-((4-imidazolyl)ethyl)-α claim 4 ,γ-diaminobutanamide claim 4 , N-((4-imidazolyl)-ethyl)-α claim 4 ,β-diaminopropanamide claim 4 , and pharmaceutically acceptable salts of these compounds.6. The composition according to claim 5 , wherein said compound is N-((4-imidazolyl)ethyl)-α claim 5 ,β-diaminopropanamide or a pharmaceutically acceptable salt thereof.7. The composition according to claim 4 , wherein the amount of said compound is comprised between 0.01% and 1% in weight based on the total weight of the composition.8. The composition according to claim 4 , which further comprises one or several additional active ingredients selected from the group consisting of deglycation agents claim 4 , agents that increase the synthesis of collagen or elastin or prevent their degradation claim 4 , agents that increase the synthesis of glycosaminoglycans or proteoglycans or prevent their degradation claim 4 , agents that increase the cell proliferation claim 4 , depigmenting or pro- ...

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09-01-2014 дата публикации

Novel crystals and process of making 5-(-METHYL)-2-METHOXY-BENZOIC ACID

Номер: US20140011851A1
Принадлежит:

The present invention relates to a novel crystals of 5-({[2-amino-3-(4-carbamoyl-2,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-1h-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid and methods of making the zwitterion of 5-({[2-amino-3-(4-carbamoyl-2,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-1h-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid. 17-. (canceled)8. Form α crystal of 5-({[2-amino-3-(4-carbamoyl-2 ,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-1h-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid.9. The α crystal of claim 8 , wherein said crystal is characterized by a powder X-ray diffraction pattern having powder X-ray diffraction peaks at about 14.0 claim 8 , 14.3 claim 8 , and 14.7 degrees 2-theta.10. The α crystal of claim 8 , wherein said crystal is characterized by a powder X-ray diffraction pattern having powder X-ray diffraction peaks at about 10.2 claim 8 , 11.3 claim 8 , 14.0 claim 8 , 14.3 claim 8 , and 14.7 degrees 2-theta.11. The α crystal of claim 8 , wherein said crystal is characterized by a powder X-ray diffraction pattern having powder X-ray diffraction peaks at about 10.2 claim 8 , 11.3 claim 8 , 11.8 claim 8 , 14.0 claim 8 , 14.3 claim 8 , 14.7 claim 8 , 16.1 claim 8 , and 18.3 degrees 2-theta.12. The α crystal of claim 8 , wherein said crystal is characterized by a powder X-ray diffraction pattern having powder X-ray diffraction peaks substantially as shown in Table 1.13. The α crystal of claim 8 , wherein said crystal is characterized by a powder X-ray diffraction pattern having powder X-ray diffraction peaks substantially similar to the powder X-ray diffraction peaks of .14. The α crystal of claim 8 , wherein said crystal is characterized by a thermal gravimetric analysis (TGA) substantially similar to the TGA in .15. The α crystal of claim 8 , wherein said crystal is characterized by a differential scanning calorimetry (DSC) measurement substantially similar to the DSC in .16. A method of treating a mammal ...

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09-01-2014 дата публикации

POLYETHER COMPOUND AND ELECTROLYTE COMPOSITION

Номер: US20140012012A1
Принадлежит: ZEON CORPORATION

A polyether compound containing oxirane monomer units in an average number per molecule of to , wherein the polyether compound contains repeating units which are represented by the general formula () as at least part of the oxirane monomer units is provided. According to the present invention, it is possible to provide a polymer material which has suitable fluidity and is excellent in ion conductivity. 2. The polyether compound as set forth in wherein claim 1 , in the general formula (2) claim 1 , the anion which is represented by X and is comprised of 2 to 25 atoms is any of OH claim 1 , SCN claim 1 , BF claim 1 , PF claim 1 , ClO claim 1 , (FSO)N claim 1 , (CFSO)N claim 1 , (CFCFSO)N claim 1 , CHSO claim 1 , CFSO claim 1 , CFCOO claim 1 , and PhCOO.3. The polyether compound as set forth in claim 1 , wherein claim 1 , in the repeating units which are expressed by the general formula (1) claim 1 , the ratio of the repeating units which are represented by the general formula (2) is 2 mol % or more.4. The polyether compound as set forth in claim 1 , wherein claim 1 , in the repeating units which are represented by the general formula (1) claim 1 , the units other than the repeating units which are represented by the general formula (2) include at least one unit selected from units where the monovalent group which is represented by A in the general formula (1) is a hydrogen atom claim 1 , units where it is an alkyl group claim 1 , and units where it is a haloalkyl group claim 1 , and units which have the same structure as the repeating units which are represented by the general formula (2) except anions where X is comprised of a single atom.5. An electrolyte composition which contains the polyether compound as set forth in .6. A method of production of the polyether compound as set forth in comprising claim 1 ,a step of ring opening polymerizing a monomer composition which contains epichlorohydrin in the presence of an onium salt of a compound which contains atoms of ...

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16-01-2014 дата публикации

Process For Producing N-Halogenated Hydantoins

Номер: US20140017290A1
Автор: Elnagar Hassan Y.
Принадлежит: Albemarle Corporation

This invention provides a process for the N-halogenation of at least one 5-hydrocarbyl hydantoin and/or at least one 5,5-dihydrocarbyl hydantoin. The process comprises concurrently feeding into a reaction zone (i) water, inorganic base, and 5,5-dimethylhydantoin, these being fed separately and/or in any combination(s), (ii) a separate feed of a brominating agent, and (iii) a separate feed of a chlorinating agent, in proportions such that during all or substantially all of the time the concurrent feeding is occurring halogenation of the 5-hydrocarbyl hydantoin and/or 5,5-dihydrocarbyl hydantoin occurs and resultant halogenated product precipitates in the liquid phase of an aqueous reaction mixture, and in which the pH of the liquid phase is continuously or substantially continuously maintained in the range of about 2.0 to about 8.0 during all or substantially all of the time the concurrent feeding is occurring. Also provided by this invention is a composition of matter which is a halogenated 5-hydrocarbyl hydantoin or a halogenated 5,5-dihydrocarbyl hydantoin, which is a mixture of the 1,3-dibromo-, 1,3-dichloro-, and/or N,N′-bromochloro-species of the halogenated hydantoin. 1. A composition of matter which comprises a mixture of differently-halogenated 5-hydrocarbyl hydantoins and/or a mixture of differently-halogenated 5 ,5-dihydrocarbyl hydantoins , which composition is a mixture of the 1 ,3-dibromo- , 1 ,3-dichloro- and/or N ,N′-bromochloro-species of said halogenated hydantoins , as produced by a single halogenation step or operation at a temperature in the range of about 40° C. to about 60° C. , wherein the N ,N′-bromochloro-species is predominate , wherein the N ,N′-bromochloro-species comprises about 40% or more of the composition , while the 1 ,3-dibromo-species comprises about 30% or more of the composition , and wherein the composition has an average particle size of about 50 microns or more.2. A composition of wherein said halogenated 5-hydrocarbyl ...

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16-01-2014 дата публикации

IMIDAZOLE PRODRUG LXR MODULATORS

Номер: US20140018321A1
Принадлежит:

Imidazole prodrugs, pharmaceutically acceptable salts, or isomers thereof, of the invention are disclosed, which are useful as modulators of the activity of liver X receptors (LXR). Pharmaceutical compositions containing the compounds and methods of using the compounds are also disclosed. 6. The compound of that is a pharmaceutically acceptable salt of said compound.7. The compound of claim 6 , wherein the pharmaceutically acceptable salt comprises the di-(2-amino-2-(hydroxymethyl)propanediol) ethanolate salt.8. A composition comprising at least one compound of and one or more pharmaceutically acceptable carriers.9. The composition of further comprising at least one additional therapeutic agent.10. A method of treating a disease or disorder comprising administering to a subject in need thereof a therapeutically effective amount of at least one compound of claim 1 , wherein the disease or disorder is atherosclerosis claim 1 , insulin resistance claim 1 , osteoarthritis claim 1 , stroke claim 1 , hyperglycemia claim 1 , dyslipidemia claim 1 , psoriasis claim 1 , aged and UV skin wrinkling claim 1 , diabetes claim 1 , cancer claim 1 , inflammation claim 1 , immunological disorders claim 1 , lipid disorders claim 1 , obesity claim 1 , macular degeneration claim 1 , conditions characterized by a perturbed epidermal barrier function claim 1 , conditions of disturbed differentiation or excess proliferation of the epidermis or mucous membrane claim 1 , or cardiovascular disorders.11. The method of wherein the disease or disorder is atherosclerosis claim 10 , diabetes or dyslipidemia.12. The method of wherein the disease or disorder is atherosclerosis.13. The method of wherein the disease or disorder is diabetes.14. A composition comprising at least one compound of and one or more pharmaceutically acceptable carriers.15. The composition of further comprising at least one additional therapeutic agent.16. A method of treating a disease or disorder comprising administering to a ...

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23-01-2014 дата публикации

Inhibition of bacterial biofilms and microbial growth with imidazole derivatives

Номер: US20140023691A1
Принадлежит: North Carolina State University

Disclosure is provided for imidazole derivative compounds useful to inhibit the formation of biofilms and/or inhibit microbial growth, compositions including these compounds, devices including these compounds, and methods of using the same.

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23-01-2014 дата публикации

COMPOSITIONS OF DIBROMOMALONAMIDE AND THEIR USE AS BIOCIDES

Номер: US20140023727A1
Принадлежит: Dow Global Technologies LLC

A biocidal composition comprising 2,2-dibromomalonamide and an oxidizing biocide, and its use for the control of microorganisms in aqueous and water-containing systems. 1. A biocidal composition comprising: 2 ,2-dibromomalonamide and an oxidizing biocide comprising hypochlorous acid or a salt thereof , monohalodimethylhydantoin , dichlorodimethylhydantoin , or dibromodimethylhydantoin.2. A composition according to wherein the weight ratio of 2 claim 1 ,2-dibromomalonamide to the oxidizing biocide is between 16:1 and 1:8.3. A composition according to wherein the oxidizing biocide comprises hypochlorous acid or a salt thereof claim 1 , and the weight ratio of 2 claim 1 ,2-dibromomalonamide to hypochlorous acid or salt thereof is between 16:1 and 1:1.4. A composition according to wherein the oxidizing biocide comprises a monohalodimethylhydantoin and the weight ratio of the 2 claim 1 ,2-dibromomalonamide to the monohalodimethylhydantoin is between 1:1 and 1:4.5. A composition according to wherein the oxidizing comprises dichlorodimethylhydantoin and the weight ratio of the 2 claim 1 ,2-dibromomalonamide to the dichlorodimethylhydantoin is between 16:1 and 1:2.6. A composition according to wherein the oxidizing biocide comprises dibromodimethylhydantoin and the weight ratio of the 2 claim 1 ,2-dibromomalonamide to the dibromodimethylhydantoin is between 16:1 and 1:8.76. A composition according to any one of - which is: paint claims 1 , coating claims 1 , aqueous emulsion claims 1 , latex claims 1 , adhesive claims 1 , ink claims 1 , pigment dispersion claims 1 , household or industrial cleaner claims 1 , detergent claims 1 , dish detergent claims 1 , mineral slurry polymer emulsion claims 1 , caulk claims 1 , adhesive claims 1 , tape joint compound claims 1 , disinfectant claims 1 , sanitizer claims 1 , metalworking fluid claims 1 , construction product claims 1 , personal care product claims 1 , textile fluid claims 1 , spin finish claims 1 , industrial process water ...

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23-01-2014 дата публикации

DUAL-ACTING ANTIHYPERTENSIVE AGENTS

Номер: US20140024835A1
Принадлежит: THERAVANCE, INC.

The invention is directed to compounds having the formula: 14-. (canceled)5. The process of claim 33 , wherein Ris selected from —COOH claim 33 , —SONHR claim 33 , and tetrazol-5-yl.6. (canceled)7. The process of claim 33 , wherein Y represents —C(R)— claim 33 , Z is —N— claim 33 , Q is —N— and W is a bond.8. The process of claim 33 , wherein Y represents —C(R)— claim 33 , Z is —CH— claim 33 , Q is —C(R)— and W is —C(O)—.9. The process of claim 33 , wherein Y represents —N— claim 33 , Z is —C(R)— claim 33 , Q is —C(R)— and W is a bond.10. The process of claim 33 , wherein Y represents —C(R)— claim 33 , Z is —CH— claim 33 , Q is —N— and W is a bond.11. The process of claim 33 , wherein Ris selected from H claim 33 , halo claim 33 , —Calkyl claim 33 , —Ccycloalkyl claim 33 , and —Calkylene-OR.12. The process of claim 33 , wherein Ris selected from —Calkyl and —Calkylene-O—Calkylene-R claim 33 , where Ris —Calkyl.1314-. (canceled)15. The process of claim 33 , wherein X is selected from: —C(O)NH—; —CH—NHC(O)—; —C(O)NH—CH—; —C(O)NH—NHC(O)—; —CH═C(—CH-2-thiophene)-C(O)NH—; —(CH)—NHC(O)—; —C(O)NH—CH—CH(COOH)—CH—; —C(O)NH—CH(benzyl)-CH—NHC(O)—; —C(O)NH—CH(benzyl)-CH—C(O)NH—; —CH—NHC(O)—CH—NHC(O)—; —CH—NHC(O)-cyclohexylene-NHC(O)—; —CH—N(OH)C(O)-cyclohexylene-NHC(O)—; —CH—NHC(O)—CH—CH(COOH)—NHC(O)—; —CH—NHC(O)—(CH)—NHC(O)—; —C(O)NH—(CH)—C(O)N(OH)—CH—; —C(O)NH—(CH)—CH(COOH)—NHC(O)—; —C(O)NH—(CH)—NHC(O)—; —CH—NHC(O)—(CH)—CH(COOH)—NHC(O)—; —C(O)NH—(CH)—CH(COOH)—NHC(O)—; —C(O)NH—(CH)—NHC(O)—CH—NHC(O)—; —C(O)NH—(CH)—NHC(O)-cyclohexylene-NHC(O)—; —CH—NHC(O)—(CH)—NHC(O)—; —C(O)NH—(CH)—CH(COOH)—NHC(O)—; —CH—NHC(O)—(CH)—NHC(O)-cyclohexylene-NHC(O)—; —CH—C(O)NH—(CH)—NHC(O)-cyclohexylene-NHC(O)—; —C(O)NH—(CH)—NHC(O)—CH—NHC(O)—; —C(O)NH—(CH)—NHC(O)-cyclohexylene-NHC(O)—; —CH—NHC(O)—(CH)—NHC(O)—; —CH—NHC(O)—(CH)—NHC(O)-cyclohexylene-NHC(O)—; —C(O)NH—(CH)—NHC(O)-cyclohexylene-NHC(O)—; and —CH—NHC(O)—(CH)—NHC(O)-cyclohexylene-NHC(O)—.16. The process of claim 15 , wherein X is selected from ...

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06-02-2014 дата публикации

Oligomer-Containing Hydantoin Compounds

Номер: US20140039020A1
Принадлежит: Nektar Therapeutics

The invention relates to (among other things) oligomer-containing hydantoin compounds. A compound of the invention, when administered by any of a number of administration routes, exhibits one or more advantages over corresponding compounds lacking the oligomer. 1. A compound comprising a hydantoin residue covalently attached via a linkage to a water-soluble , non-peptidic oligomer.5. The compound of claim 1 , wherein the hydantoin residue is a residue of a hydantoin moiety selected from the group consisting of ethotoin claim 1 , mephenyloin claim 1 , phenyloin and fosphenyloin.6. The compound of claim 5 , wherein the hydantoin residue is a residue of phenyloin.7. The compound of claim 1 , wherein the water-soluble claim 1 , non-peptidic oligomer is a poly(alkylene oxide).8. The compound of claim 7 , wherein the poly(alkylene oxide) is a poly(ethylene oxide).9. The compound of claim 1 , wherein water-soluble claim 1 , non-peptidic oligomer has from about 1 to about 30 monomers.10. The compound of claim 9 , wherein the water-soluble claim 9 , non-peptidic oligomer has from about 1 to about 10 monomers.11. The compound of claim 7 , wherein the poly(alkylene oxide) includes an alkoxy or hydroxy end-capping moiety.12. The compound of claim 1 , wherein a single water-soluble claim 1 , non-peptidic oligomer is attached to the hydantoin residue.13. The compound of claim 1 , wherein more than one water-soluble claim 1 , non-peptidic oligomer is attached to the hydantoin residue.14. The compound of claim 1 , wherein the linkage is a stable linkage.15. The compound of claim 1 , wherein the linkage is a releasable linkage.16. A composition comprising a compound comprising a hydantoin residue covalently attached via a linkage to a water-soluble claim 1 , non-peptidic oligomer claim 1 , and optionally claim 1 , a pharmaceutically acceptable excipient.17. A composition of matter comprising a compound comprising a hydantoin residue covalently attached via a linkage to a water- ...

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06-02-2014 дата публикации

SOLID GERMICIDAL COMPOSITION AND DISINFECTION METHOD

Номер: US20140039023A1
Принадлежит: UENO FINE CHEMICALS INDUSTRY, LTD.

A solid germicidal composition containing a compound of the formula (I), a carbonate compound and an organic acid with a solubility in water at 20° C. of 0.25 to 35%: 2. The composition according to claim 1 , wherein the compound of the formula (I) is one or more compounds selected from the group consisting of1,10-di(3-decyl-2-methylimidazolium)decane dichloride,1,10-di(3-decyl-2-methylimidazolium)decane dibromide,1,12-di(3-decyl-2-methylimidazolium)dodecane dichloride and1,12-di(3-octyl-2-methylimidazolium)dodecane dichloride.3. The composition according to claim 1 , wherein the compound of the formula (I) is1,10-di(3-decyl-2-methylimidazolium)decane dichloride.4. The composition according to claim 1 , which comprises 0.05 to 18 parts by weight of the carbonate compound relative to 1 part by weight of the compound of the formula (I).5. The composition according to claim 1 , which comprises 0.05 to 18 parts by weight of the organic acid with a solubility in water at 20° C. of 0.25 to 35% relative to 1 part by weight of the compound of the formula (I).6. The composition according to claim 1 , wherein the carbonate compound is sodium bicarbonate or sodium carbonate.7. The composition according to claim 1 , wherein the organic acid is succinic acid or adipic acid.8. An aqueous solution of the composition according to .9. A method for disinfecting an object claim 1 , which comprises contacting an aqueous solution of the composition according to with the object.10. The method according to claim 9 , wherein the object is an object in or on which microorganisms resistant to quaternary ammonium salts and/or biguanide germicides exist or an object to which quaternary ammonium salts and/or biguanide germicides are being applied or were previously applied. The present invention relates to a solid germicidal composition which is mainly used for disinfection of floors, walls, tools, facilities and the like in, for example, food factories, and a disinfection method using such ...

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06-02-2014 дата публикации

NOVEL COMPOUNDS AS OPIOID RECEPTOR MODULATORS

Номер: US20140039024A1
Принадлежит:

The present invention is directed to novel opioid receptor modulators of Formula (I). 6. The method according to claim 1 , comprising administering to the subject a therapeutically effective amount of a pharmaceutically acceptable salt of said compound.7. The method according to claim 6 , wherein the salt is a hydrochloric claim 6 , hydrobromic claim 6 , hydriodic claim 6 , perchloric claim 6 , sulfuric claim 6 , nitric claim 6 , phosphoric claim 6 , acetic claim 6 , propionic claim 6 , glycolic claim 6 , lactic claim 6 , succinic claim 6 , maleic claim 6 , fumaric claim 6 , malic claim 6 , tartaric claim 6 , citric claim 6 , benzoic claim 6 , mandelic claim 6 , methanesulfonic claim 6 , hydroxyethanesulfonic claim 6 , benzenesulfonic claim 6 , oxalic claim 6 , pamoic claim 6 , 2-naphthalenesulfonic claim 6 , p-toluenesulfonic claim 6 , cyclohexanesulfamic claim 6 , salicylic claim 6 , saccharinic claim 6 , or trifluoroacetic acid salt.8. The method according to claim 6 , wherein the salt is a benzathine claim 6 , chloroprocaine claim 6 , choline claim 6 , diethanolamine claim 6 , ethylenediamine claim 6 , meglumine claim 6 , procaine claim 6 , aluminum claim 6 , calcium claim 6 , lithium claim 6 , magnesium claim 6 , potassium claim 6 , sodium claim 6 , or zinc salt.9. The method according to claim 1 , wherein the chronic pain is selected from the group consisting of neuropathic pain conditions claim 1 , diabetic peripheral neuropathy claim 1 , post-herpetic neuralgia claim 1 , trigeminal neuralgia claim 1 , post-stroke pain syndromes and cluster or migraine headaches.10. The method of claim 1 , wherein the method is for treating centrally mediated pain.11. The method according to claim 1 , wherein the method is for treating peripherally mediated pain.12. The method according to claim 1 , wherein the method is for treating structural or soft tissue injury related pain.13. The method according to claim 1 , wherein the method is for treating pain related to ...

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06-02-2014 дата публикации

Substituted Imidazole Derivatives and Methods of Use Thereof

Номер: US20140039025A1
Принадлежит: TransTech Pharma, Inc.

The present invention provides imidazole derivatives of Formula (I) and pharmaceutically acceptable salts thereof. 2. The method of claim 1 , wherein the compound is (R)-1-(4-{2-butyl-1-[4-(4-chloro-phenoxy)-phenyl]-1H-imidazol-4-yl}-phenoxy)-3-dimethylamino-propan-2-ol or a pharmaceutically acceptable salt thereof.3. The method of claim 1 , wherein the compound is (R)-1-(4-{2-butyl-1-[4-(4-chloro-phenoxy)-phenyl]-1H-imidazol-4-yl}-phenoxy)-3-diethylamino-propan-2-ol or a pharmaceutically acceptable salt thereof.4. The method of claim 1 , wherein the compound is (S)-1-(4-{2-butyl-1-[4-(4-chloro-phenoxy)-phenyl]-1H-imidazol-4-yl}-phenoxy)-3-dimethylamino-propan-2-ol or a pharmaceutically acceptable salt thereof.5. The method of claim 1 , wherein the compound is (S)-1-(4-{2-butyl-1-[4-(4-chloro-phenoxy)-phenyl]-1H-imidazol-4-yl}-phenoxy)-3-diethylamino-propan-2-ol or a pharmaceutically acceptable salt thereof.6. The method of claim 1 , wherein the compound is (R)-1-(4-{1-[4-(4-chloro-phenoxy)-phenyl]-2-ethoxymethyl-1H-imidazol-4-yl}-phenoxy)-3-dimethylamino-propan-2-ol or a pharmaceutically acceptable salt thereof.7. The method of claim 1 , wherein the compound is (S)-1-(4-{1-[4-(4-chloro-phenoxy)-phenyl]-2-ethoxymethyl-1H-imidazol-4-yl}-phenoxy)-3-dimethylamino-propan-2-ol or a pharmaceutically acceptable salt thereof.8. The method of claim 1 , wherein the compound is (R)-1-(4-{1-[4-(4-chloro-phenoxy)-phenyl]-2-ethoxymethyl-1H-imidazol-4-yl}-phenoxy)-3-diethylamino-propan-2-ol or a pharmaceutically acceptable salt thereof.9. The method of claim 1 , wherein the compound is (S)-1-(4-{1-[4-(4-chloro-phenoxy)-phenyl]-2-ethoxymethyl-1H-imidazol-4-yl}-phenoxy)-3-diethylamino-propan-2-ol or a pharmaceutically acceptable salt thereof.10. The method of claim 1 , wherein the disease or condition is Alzheimer's Disease.11. The method of claim 1 , wherein the disease or condition is sepsis.12. The method of claim 1 , wherein the disease or condition is diabetes.13. The method of ...

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06-02-2014 дата публикации

Novel process for the preparation of acylguanidines and acylthioureas

Номер: US20140039189A1
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

The present invention relates to a novel process for the preparation of compounds of general formula (I) and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids and bases, which have valuable pharmacological properties, particularly an inhibitory effect on epithelial sodium channels, the use thereof for the treatment of diseases, particularly diseases of the lungs and airways.

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20-02-2014 дата публикации

CRYSTALLINE FORMS OF (R)-8-CHLORO-1-METHYL-2,3,4,5-TETRAHYDRO-1H-3-BENZAZEPINE HYDROCHLORIDE

Номер: US20140051684A1
Принадлежит:

The present invention is directed to crystalline forms of (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine, compositions containing the same and uses thereof. 140.-. (canceled)41. A method of treatment of obesity comprising administering to an individual in need of such treatment a therapeutically effective amount of (R)-8-chloro-1-methyl-2 ,3 ,4 ,5-tetrahydro-1H-3-benzazepine hydrochloride hemihydrate.42. A method of decreasing food intake comprising administering to an individual in need of such administration a therapeutically effective amount of (R)-8-chloro-1-methyl-2 ,3 ,4 ,5-tetrahydro-1H-3-benzazepine hydrochloride hemihydrate.43. A method of inducing satiety comprising administering to an individual in need of such administration a therapeutically effective amount of (R)-8-chloro-1-methyl-2 ,3 ,4 ,5-tetrahydro-1H-3-benzazepine hydrochloride hemihydrate.44. A method of controlling weight gain comprising administering to an individual in need of such administration a therapeutically effective amount of (R)-8-chloro-1-methyl-2 ,3 ,4 ,5-tetrahydro-1H-3-benzazepine hydrochloride hemihydrate.45. A method of treatment of a disorder of the central nervous system , damage to the central nervous system , a cardiovascular disorder , a gastrointestinal disorder , diabetes insipidus , or sleep apnea comprising administering to an individual in need of such treatment a therapeutically effective amount of (R)-8-chloro-1-methyl-2 ,3 ,4 ,5-tetrahydro-1H-3-benzazepine hydrochloride hemihydrate.46. A method of treatment of depression , atypical depression , a bipolar disorder , an anxiety disorder , an obsessive-compulsive disorder , a social phobia or panic state , a sleep disorder , sexual dysfunction , a psychosis , schizophrenia , migraine or a condition associated with cephalic pain or other pain , raised intracranial pressure , epilepsy , a personality disorder , an age-related behavioral disorder , a behavioral disorder associated with dementia , organic ...

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27-02-2014 дата публикации

CIS-ALKOXY-SUBSTITUTED SPIROCYCLIC 1-H-PYRROLIDINE-2,4-DIONE DERIVATIVES

Номер: US20140058114A1
Принадлежит: Bayer Intellectual Property GmbH

Process for preparing cis-alkoxy-substituted spirocyclic 1-H-pyrrolidine-2,4-dione derivatives and alkali metal salts and alkaline earth metal salts thereof. 2. The process according to claim 1 , where A represents C-C-alkyl.3. The process according to claim 1 , where A represents methyl claim 1 , ethyl claim 1 , propyl claim 1 , isopropyl claim 1 , butyl or isobutyl.4. The process according to claim 1 , where A represents methyl.5. The process according to claim 1 , wherein lithium hydroxide claim 1 , sodium hydroxide claim 1 , potassium hydroxide claim 1 , cesium hydroxide claim 1 , magnesium hydroxide claim 1 , rubidium hydroxide claim 1 , calcium hydroxide or barium hydroxide is used.9. A hydrate of a compound of formula (cis-IV) according to . The present invention relates to processes for preparing cis-alkoxy-substituted spirocyclic 1H-pyrrolidine-2,4-dione derivatives and alkali metal salts and alkaline earth metal salts thereof.Alkoxy-substituted spirocyclic 1H-pyrrolidine-2,4-dione derivatives of the general formula (I) having acaricidal, insecticidal and herbicidal action are known: EP-A 596 298, WO95/20572, WO 95/26954, WO 95/20572, EP-A 668 267, WO 96/25395, WO 96/35664, WO 97/01535, WO 97/02243, WO 97/36868, WO 98/05638, WO 99/43649, WO 99/48869, WO 99/55673, WO 01/74770, WO 01/96333, WO 03/035643, WO 04/007448, WO 04/065366, WO 04/111042, WO 05/066125, WO 05/049569, WO 05/044796, WO 05/092897, WO 06/056282, WO 06/056281, WO 06/029799, WO 07/096058, WO 08/067910, WO 08/138551, WO 10/102758.Such compounds are usually prepared starting with the corresponding cis-substituted hydantoins of the formula (cis-II).In the formulae (I), (II) and (cis-II),It is already known that in particular the cis-substituted compounds of the formula (I) have biologically advantageous properties (activity, toxicological profile) (WO2004/007448). Accordingly, there is an increased demand for cis-substituted hydantoins of the formula (cis-II) as starting materials.However, owing ...

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06-03-2014 дата публикации

REL INHIBITORS AND METHODS OF USE THEREOF

Номер: US20140066486A1

This invention provides REL inhibitors which interfere with the DNA binding capacity of a REL protein. Additionally this invention provides methods of treating, abrogating, or preventing diseases which respond with a positive clinical score to a REL inhibitor. Methods of identifying REL inhibitor based on a REL protein three dimensional model are described. 2. The composition of claim 1 , wherein the inhibitor interact with L1 cavity on the surface of the c-Rel.3. The composition of claim 1 , wherein said L1 cavity comprises amino acids Arg 21 claim 1 , Cys 26 claim 1 , Glu 27 claim 1 , Lys 110 claim 1 , and Lys 111.5. The composition of claim 1 , comprising the compound represented by the structure of formula (IV) claim 1 , (V) or their pharmaceutical salt.7. Use of the composition of for preventing claim 1 , inhibiting claim 1 , suppressing or ameliorating symptoms associated with inflammatory conditions that are multiple sclerosis claim 1 , arthritis claim 1 , diabetes claim 1 , colitis claim 1 , lupus claim 1 , autoimmunity claim 1 , graft rejection claim 1 , or a combination thereof.8. A method of inhibiting or suppressing the interaction between c-Rel and a DNA claim 1 , comprising the step of contacting the c-Rel with a compound capable of masking the L1 cavity of the c-Rel claim 1 , thereby inhibiting or suppressing the interaction between c-Rel and a DNA and inflammatory immune response.10. The method of claim 9 , wherein said inhibitor further inhibits the production of interleukin-2 claim 9 , interferon-gamma claim 9 , or the combination thereof.11. The method of claim 9 , wherein said L1 cavity comprises the amino acids Arg 21 claim 9 , Cys 26 claim 9 , Glu 27 claim 9 , Lys 110 claim 9 , and Lys 111.13. The method of claim 9 , whereby the compound capable of masking the L1 cavity of the c-Rel is represented by the structure of formula (IV) claim 9 , (V) or their pharmaceutical salt.15. A method of treating claim 9 , inhibiting or suppressing claim 9 , or ...

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03-04-2014 дата публикации

IMIDAZOLE COMPOUNDS THAT MODULATE HSP90 ACTIVITY

Номер: US20140094436A1
Принадлежит: Synta Pharmaceuticals Corp.

Compounds of formula (I), pharmaceutical compositions comprising compounds of formula (I) and methods of inhibiting Hsp90 in a cell, treating or preventing a proliferation disorder in a mammal and treating cancer in a mammal comprising administering a compound of formula (I) to a patient or a cell. 122-. (canceled)24. The compound of claim 23 , wherein Ris substituted with one or more group represented by R claim 23 , wherein R claim 23 , for each occurrence claim 23 , are independently an optionally substituted alkyl claim 23 , an optionally substituted alkenyl claim 23 , an optionally substituted alkynyl claim 23 , an optionally substituted cycloalkyl claim 23 , an optionally substituted cycloalkenyl claim 23 , an optionally substituted heterocyclyl claim 23 , an optionally substituted aryl claim 23 , an optionally substituted heteroaryl claim 23 , an optionally substituted aralkyl claim 23 , an optionally substituted heteraralkyl claim 23 , halo claim 23 , cyano claim 23 , nitro claim 23 , guanadino claim 23 , a haloalkyl claim 23 , a heteroalkyl claim 23 , alkoxy claim 23 , haloalkoxy claim 23 , —NRR claim 23 , —OR claim 23 , —C(O)R claim 23 , —C(O)OR claim 23 , —C(S)R claim 23 , —C(O)SR claim 23 , —C(S)SR claim 23 , —C(S)OR claim 23 , —C(S)NRR claim 23 , —C(NR)OR claim 23 , —C(NR)R claim 23 , —C(NR)NRR claim 23 , —C(NR)SR claim 23 , —OC(O)R claim 23 , —OC(O)OR claim 23 , —OC(S)OR claim 23 , —OC(NR)OR claim 23 , —SC(O)R claim 23 , —SC(O)OR claim 23 , —SC(NR)OR claim 23 , —OC(S)R claim 23 , —SC(S)R claim 23 , —SC(S)OR claim 23 , —OC(O)NRR claim 23 , —OC(S)NRR claim 23 , —OC(NR)NRR claim 23 , —SC(O)NRR claim 23 , —SC(NR)NRR claim 23 , —SC(S)NRR claim 23 , —OC(NR)R claim 23 , —SC(NR)R claim 23 , —C(O)NRR claim 23 , —NRC(O)R claim 23 , —NRC(S)R claim 23 , —NRC(S)OR claim 23 , —NRC(NR)R claim 23 , —NRC(O)OR claim 23 , —NRC(NR)OR claim 23 , —NRC(O)NRR claim 23 , —NRC(S)NRR claim 23 , —NRC(NR)NRR claim 23 , —SR claim 23 , —S(O)R claim 23 , —OS(O)R claim 23 , —OS(O)OR ...

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03-04-2014 дата публикации

Antimicrobial Haloalkyl Heterocycle Compounds

Номер: US20140094495A1
Принадлежит: NovaBay Pharmaceuticals, Inc.

This application describes compounds useful as anti-microbial agents, including as antibacterial, disinfectant, antifungal, germicidal or antiviral agents. 2. The compound of claim 1 , wherein Z is O.3. The compound of claim 2 , wherein X is Cl.4. The compound of claim 3 , wherein Ris methyl.5. The compound of claim 1 , wherein Z is NR.6. The compound of claim 1 , wherein Z is CRR.7. The compound of claim 1 , wherein Ris chloromethyl.8. A compound selected from the group consisting of:3-chloro-4-(fluoromethyl)-4-methyloxazolidin-2-one,3-chloro-4-(chloromethyl)-4-methyloxazolidin-2-one,3-chloro-4-(bromomethyl)-4-methyloxazolidin-2-one,3-chloro-4-(2,2,2-trifluoroethyl)-4-methyloxazolidin-2-one,3-chloro-4,4-bis(chloromethyl)oxazolidin-2-one,3-bromo-4-(chloromethyl)-4-methyloxazolidin-2-one,3-chloro-4-(chloromethyl)-1,4-dimethylimidazolidin-2-one,and 1-chloro-5-(chloromethyl)-5-methylpyrrolidin-2-one.9. A pharmaceutically acceptable salt of a compound of .10. An antimicrobial composition comprising a compound of claim 1 , formulated as an aerosol claim 1 , cream claim 1 , emulsion claim 1 , gel claim 1 , lotion claim 1 , ointment claim 1 , paste claim 1 , powder claim 1 , solid claim 1 , solution or suspension.11. A method for treating a microbial ailment claim 1 , condition or infection in a subject claim 1 , comprising administering an effective amount of a compound of to the subject.12. A method for treating a medical device claim 1 , comprising administering an effective amount of a compound of to the device. This application claims the benefit of U.S. Provisional Application No. 61/559,414 filed Nov. 14, 2011, which is incorporated herein by reference.This application describes compounds useful as anti-microbial agents, including as antibacterial, disinfectant, antifungal, germicidal or antiviral agents.One aspect of the current disclosure relates to compounds of Formula Ior a derivative thereof, whereinIn some compounds of Formula I, X is Cl. In some compounds of ...

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10-04-2014 дата публикации

PRODUCTION METHOD OF IMIDAZOLE DERIVATIVES

Номер: US20140100373A1
Принадлежит: Takeda Pharmaceutical Company Limited

The present invention provides an advantageous production method of an imidazole derivative, which is suitable for industrial production. 5. The method of any of to , wherein PG is trityl.6. The method of any of to , wherein PG is tosyl , benzenesulfonyl or N ,N-dimethylaminosulfonyl. The present invention relates to an industrially advantageous production method of an imidazole derivative.It is known that an imidazole derivative represented by the following formula (Ia):wherein n is an integer of 1 to 3, and Ar is an aromatic ring optionally having substituent(s), or a salt thereof has high safety and superior steroid Clyase inhibitory activity, and is useful for the prophylaxis or treatment of diseases for which androgen or estrogen is an aggravating factor (patent document 1).As the production method of the above-mentioned imidazole derivative, the methods described in patent document 1 and patent document 2 are known.However, there is a demand for an advantageous production method of the imidazole derivative, which is suitable for industrial production.In the production method of patent document 2, the synthetic reaction of the following formula (Ib):wherein Ar is an aromatic hydrocarbon group optionally having substituent(s), and PG is an imidazole-protecting group, which is an intermediate for synthesizing the above-mentioned formula (Ia), needs to be carried out in the presence of an organic lithium compound at an ultralow temperature of −65° C.In view of such situation, an object of the present invention is to provide a novel production method of an imidazole derivative represented by the above-mentioned formula (Ia), particularly 6-(7-hydroxy-6,7-dihydro-5H-pyrrolo[1,2-c]imidazol-7-yl)-N-methyl-2-naphthamide or a salt thereof, which is suitable for efficient and convenient industrial production. In addition, another object of the present invention is to provide a production method of a compound useful as an intermediate for synthesizing 6-(7-hydroxy-6,7- ...

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04-01-2018 дата публикации

ALKALOIDS FROM SPONGE, SCAFFOLDS FOR THE INHIBITION OF HUMAN IMMUNODEFICIENCY VIRUS (HIV)

Номер: US20180000787A1
Принадлежит:

Anti-viral compounds with low cytotoxicity are identified from screening of products found in Red Sea sponges, including the sponge Stylissa carteri. The identified compounds can be brominated pyrrole-2-aminoimidazole alkaloids and derivatives thereof. Specific examples of identified compounds include oroidin, hymenialdisine, and debromohymenialdisine, as well as derivatives thereof. The compounds also can be useful scaffolds or pharmacores for further chemical modification and derivatization. Selected compounds, particularly oroidin, show selective anti-viral HIV-1 activity coupled with reduced cytotoxicity. The compounds can function as HIV reverse-transcriptase inhibitors, and molecular modeling can be used to confirm inhibition. 1. A method comprising:subjecting crude extracts of Stylissa carteri sponge to solid phase extraction to produce a library of fractions;conducting at least one first screening assay of the library of fractions for inhibition of HIV and for cytotoxicity including selecting at least one fraction for further fractionation,fractionating the at least one fraction further to produce at least one additional fraction;conducting at least one second screening assay of the at least one additional fraction for inhibition of HIV and for cytotoxicity, including selecting one or more fractions with decreased cytotoxicity for further identification study;identifying HIV inhibitor molecule candidate(s) based on the inhibition of HIV and decreased cytotoxicity.2. The method of claim 1 , wherein the library of fractions comprises at least four fractions.3. The method of any one of - claim 1 , wherein the first screening assay is an HIV replication assay.4. The method of any one of - claim 1 , wherein the second screening assay is an HIV replication assay.5. The method of any one of - claim 1 , wherein the first screening assay and the second screening assay are HIV replication assays.6. The method of any one of - claim 1 , wherein the first screening assay ...

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05-01-2017 дата публикации

Processes for the Synthesis of Substituted Urea Compounds

Номер: US20170001962A1
Принадлежит: Bial-Portela & CA, S.A.

The present invention concerns a process for preparing a compound having the Formula A: 2. The process according to claim 1 , wherein the oxidation of the derivative of R5 and R6 employs an inorganic acid.3. The process according to claim 2 , wherein the inorganic acid is HX claim 2 , where X is a halogen atom.4. The process according to claim 3 , wherein the inorganic acid is HCl or HBr.5. The process according to any preceding claim claim 3 , wherein DMSO is used as a solvent and oxidising agent in the oxidation of the derivative of R5 and R6.6. The process according to any preceding claim claim 3 , wherein R1 is selected from H and Calkyl.7. The process according to claim 6 , wherein R1 is selected from H claim 6 , methyl and ethyl.8. The process according to any preceding claim claim 6 , wherein R2 is selected from aryl claim 6 , heteroaryl claim 6 , heterocyclyl claim 6 , Ccycloalkyl claim 6 , aryl Calkyl claim 6 , heteroaryl Calkyl claim 6 , heterocyclyl Calkyl and Ccycloalkyl Calkyl claim 6 , each of which may be substituted or unsubstituted.9. The process according to claim 8 , wherein R2 is selected from aryl claim 8 , heteroaryl claim 8 , heterocyclyl claim 8 , and Ccycloalkyl each of which may be substituted or unsubstituted.10. The process according to or claim 8 , wherein R2 is selected from fully saturated heterocyclyl claim 8 , and Ccycloalkyl each of which are monocyclic and may be substituted or unsubstituted.11. The process according to claim 10 , wherein R2 is an unsubstituted cyclopentyl or unsubstituted cyclohexyl.12. The process according to claim 10 , wherein R2 is a fully saturated heterocyclyl claim 10 , and wherein the heterocyclyl ring contains a single heteroatom claim 10 , such as nitrogen or oxygen.13. The process according to claim 12 , wherein the heterocyclyl is six membered and the heteroatom in the said heterocyclyl group is at the 4-position relative to the position of attachment of the heterocyclyl group R2 to the urea nitrogen. ...

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05-01-2017 дата публикации

N-Substituted Imidazole Carboxylic Ester Chiral Compound Containing an Ether Side Chain, Its Preparation and Application

Номер: US20170001963A1
Принадлежит:

The present invention relates to an N-substituted imidazole carboxylic ester chiral compound containing an ether side chain and to its preparation and application. The structure of this compound is represented by Formula (I). This compound can induce a rapid and reversible general anesthesia effect. Animal experiments show that this compound has rapid and short-acting pharmacological characteristics, so that it can be used as a rapid and short-acting general anesthesia medicine. Compared with etomidate, this compound can reduce the inhibition on the synthesis of adrenal cortical hormone, with an advantage of rapid and full recovery of the post-operative patient. The only chiral carbon in the compound structure belongs to the R form. This imidazole ring in the compound structure has acidifiable N atoms, so that this compound or its related pharmaceutically-acceptable salts can be used in preparation of the central inhibitory medicines, which can produce sedative, hypnotic and/or anesthetic effects on animals or human beings via their intravenous or non-intravenous administration. 2. According to claim 1 , the pharmaceutically-acceptable salts is chosen from hydrochloride claim 1 , hydrobromide or trifluoroacetate.4. According to claim 3 , the specific feature of the preparation process is that halogen X is Br or Cl.5. According to claim 3 , the specific feature of the preparation process is that the reaction solvent is DMF.6. According to claim 3 , the specific feature of the preparation process is that the base is an inorganic base.7. According to claim 6 , the specific feature of the preparation process is that the inorganic base is selected from alkali metal hydroxides or carbonates.8. The process for preparation of the related pharmaceutically-acceptable salts of claim 1 , is that the compound of the Formula (I) compound is combined with the pharmaceutically-acceptable acid radicals claim 1 , so that the corresponding salts can be obtained.9. The use of the N- ...

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02-01-2020 дата публикации

Photoredox-Catalyzed Direct C-H Functionalization of Arenes

Номер: US20200002284A1
Автор: Nicewicz David
Принадлежит:

The invention generally relates to methods of making substituted arenes via direct C—H amination. More specifically, methods of making para- and ortho-substituted arenes via direct C—H amination are disclosed. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention. 2. The method of claim 1 , wherein the electron donating group is selected from —OH claim 1 , —SH claim 1 , —NH claim 1 , C1-C8 alkyl claim 1 , C1-C8 alkoxy claim 1 , C1-C8 thioalkoxy claim 1 , C1-C8 alkylamino claim 1 , (C1-C8)(C1-C8) dialkylamino claim 1 , —OC(═O)R claim 1 , —NHC(═O)R claim 1 , and Ar;{'sup': 6', '7, 'wherein each of Rand Ris independently selected from C1-C8 alkyl; and'}{'sup': '2', 'wherein Aris selected from aryl and heteroaryl and substituted with 0, 1, 2, or 3 groups independently selected from halogen and C1-C8 alkyl.'}3. The method of claim 1 , wherein Z is F.48-. (canceled)12. (canceled)13. The method of claim 1 , wherein the fluoride is selected from ammonium fluoride claim 1 , cesium fluoride claim 1 , and triethylamine hydrofluoride.1415-. (canceled)16. The method of claim 1 , wherein the oxidant is molecular oxygen.17. The method of claim 1 , wherein the oxidant is 2 claim 1 ,2 claim 1 ,6 claim 1 ,6-tetramethyl-1-piperidinyloxy radical (TEMPO).1820-. (canceled)21. The method of claim 1 , wherein Z is —CN.29. The method of claim 1 , wherein the compound is isotopically-labeled.30. The method of claim 25 , wherein the compound contains a radioactive isotope.31. The method of claim 1 , wherein the compound is not isotopically-labeled. This application is a continuation of U.S. application Ser. No. 15/826,092, filed Nov. 29, 2017, which is a continuation of International Application No. PCT/US2016/035549 with an international filing date of Jun. 2, 2016, which claims priority to U.S. Provisional Application No. 62/170,632 filed on Jun. 3, 2015, the contents of which are incorporated ...

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02-01-2020 дата публикации

BACKFUNCTIONALIZED IMIDAZOLINIUM SALTS AND NHC CARBENE-METAL COMPLEXES

Номер: US20200002286A1

Backfunctionalized imidazolinium salts and methods of synthesizing the same and NHC carbene-metal complexes therefrom. For backfunctionalized imidazolinium salts of the formula: 2. The ionic liquid of claim 1 , wherein the ionic liquid has a chemical name of 2-ethylhexyl imidazolinium salt.3. A plasticizer for a propellant formulation claim 1 , the plasticizer comprising the ionic liquid of .4. The plasticizer of claim 3 , wherein the propellant formulation further comprises:ammonium perchorate-based propellants.5. The plasticizer of claim 3 , wherein the propellant formulation further comprises:ammonium dinitramide-based propellants6. The plasticizer of claim 3 , wherein the propellant formulation further comprises:furazan-based propellants7. A method of synthesizing a backfluorinated imidazolinium salt claim 3 , the method comprising:cyclization of a halogenated, fluorinated allyl ether with Hünig's base in polar aprotic solvent.8. The method of claim 7 , wherein the polar aprotic solvent is selected from the group consisting of ethylene glycol dimethyl ether claim 7 , diethylene glycol dimethyl ether claim 7 , and triethylene glycol dimethyl ether.9. A method of synthesizing backfluorinated second generation Grubbs' and Grubbs-Hoveyda catalysts claim 7 , the method comprising:reacting a backfluorinated NHC carbene with a first generation Grubbs' and Grubbs-Hoveyda catalyst.10. The method of claim 9 , wherein the backfluorinated second generation Grubbs' and Grubbs-Hoveyda catalysts are active for olefin metathesis and ring opening metathesis polymerization. Pursuant to 37 C.F.R. § 1.78(a)(4), this application is a continuation of U.S. application Ser. No. 16/103,267, filed Aug. 14, 2018, which was a divisional of U.S. application Ser. No. 14/880,147, filed Oct. 9, 2015, which claimed the benefit of and priority to Provisional Application Ser. No. 62/062,069, filed 9 Oct. 2014. The disclosure of each of these applications is expressly incorporated herein by ...

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02-01-2020 дата публикации

BACKFUNCTIONALIZED IMIDAZOLINIUM SALTS AND NHC CARBENE-METAL COMPLEXES

Номер: US20200002287A1

Backfunctionalized imidazolinium salts and methods of synthesizing the same and NHC carbene-metal complexes therefrom. For backfunctionalized imidazolinium salts of the formula: 2. The backfunctionalized imidazolinium salt of claim 1 , wherein each of Rand Ris mesityl.3. A free N-heterocyclic carbene synthesized by deprotonation of the backfunctionalized imidazolinium salt of claim 1 , wherein deprotonation includes reacting the backfunctionalized imidazolinium salt with silver oxide.4. A free N-heterocyclic carbene synthesized by deprotonation of the backfunctionalized imidazolinium salt of claim 1 , wherein deprotonation includes reacting the backfunctionalized imidazolinium salt with a strong base selected from the group consisting of potassium bis(trimethylsilyl)amide claim 1 , potassium tert-butoxide claim 1 , and an alkali metal hydroxide.5. An N-heterocyclic carbene-metal complex comprising:a metal; and{'claim-ref': {'@idref': 'CLM-00004', 'claim 4'}, 'a first ligand comprising the free N-heterocyclic carbene of , the first ligand being coordinated to the metal.'}6. The N-heterocyclic carbene-metal complex of claim 5 , wherein the metal is selected from the group consisting of rhenium claim 5 , ruthenium claim 5 , osmium claim 5 , rhodium claim 5 , iridium claim 5 , palladium claim 5 , platinum claim 5 , silver claim 5 , and gold.7. The N-heterocyclic carbene-metal complex of claim 5 , further comprising:{'b': '54', 'a second ligand comprising another free N-heterocyclic carbene of claim , the second ligand being coordinated to the metal.'}8. The N-heterocyclic carbene-metal complex of claim 7 , further comprising:a third ligand selected from the group consisting of an acetylacetonate, alkoxy, alkyl, aryl, aryloxy, carbonyl, halide, imido, oxo, pyridine, trialkylphosphine, and triarylphosphine, the third ligand being coordinated to the metal.9. The N-heterocyclic carbene-metal complex of claim 5 , further comprising:a second ligand selected from the group ...

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02-01-2020 дата публикации

BACKFUNCTIONALIZED IMIDAZOLINIUM SALTS AND NHC CARBENE-METAL COMPLEXES

Номер: US20200002288A1

Backfunctionalized imidazolinium salts and methods of synthesizing the same and NHC carbene-metal complexes therefrom. For backfunctionalized imidazolinium salts of the formula: 2. The backfunctionalized imidazolinium salt of claim 1 , wherein X is a halogen anion.3. The backfunctionalized imidazolinium salt of claim 1 , wherein Ris in a trans-configuration with respect to R.4. A free N-heterocyclic carbene synthesized by deprotonation of the backfunctionalized imidazolinium salt of claim 1 , wherein deprotonation includes reacting the backfunctionalized imidazolinium salt with silver oxide.5. An N-heterocyclic carbene-metal complex comprising:a metal; and{'claim-ref': {'@idref': 'CLM-00004', 'claim 4'}, 'a first ligand comprising the free N-heterocyclic carbene of , the first ligand being coordinated to the metal.'}6. The N-heterocyclic carbene-metal complex of claim 5 , wherein the metal is selected from the group consisting of rhenium claim 5 , ruthenium claim 5 , osmium claim 5 , rhodium claim 5 , iridium claim 5 , palladium claim 5 , platinum claim 5 , silver claim 5 , and gold.7. The N-heterocyclic carbene-metal complex of claim 5 , further comprising:{'b': '41', 'a second ligand comprising another free N-heterocyclic carbene of claim , the second ligand being coordinated to the metal.'}8. The N-heterocyclic carbene-metal complex of claim 7 , further comprising:a third ligand selected from the group consisting of an acetylacetonate, alkoxy, alkyl, aryl, aryloxy, carbonyl, halide, imido, oxo, pyridine, trialkylphosphine, and triarylphosphine, the third ligand being coordinated to the metal.9. The N-heterocyclic carbene-metal complex of claim 5 , further comprising:a second ligand selected from the group consisting of an acetylacetonate, alkoxy, alkyl, aryl, aryloxy, carbonyl, halide, imido, oxo, pyridine, trialkylphosphine, and triarylphosphine, the second ligand being coordinated to the metal.10. A method of synthesizing the backfunctionalized imidazolinium ...

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02-01-2020 дата публикации

BACKFUNCTIONALIZED IMIDAZOLINIUM SALTS AND NHC CARBENE-METAL COMPLEXES

Номер: US20200002289A1

Backfunctionalized imidazolinium salts and methods of synthesizing the same and NHC carbene-metal complexes therefrom. For backfunctionalized imidazolinium salts of the formula: 2. The method of claim 1 , further comprising:coordinating a second ligand to the metal, the second ligand being a second free N-heterocyclic carbene.3. The method of claim 2 , further comprising:coordinating a third ligand to the metal, the third ligand selected from the group consisting of an acetylacetonate, alkoxy, alkyl, aryl, aryloxy, carbonyl, halide, imido, oxo, pyridine, trialkylphosphine, and triarylphosphine,4. The method of claim 1 , wherein the metal selected from the group consisting of rhenium claim 1 , ruthenium claim 1 , osmium claim 1 , rhodium claim 1 , iridium claim 1 , palladium claim 1 , platinum claim 1 , silver claim 1 , and gold.5. The method of claim 1 , wherein the solvent in formamidine cyclization of the halogenated acrylate is a polar aprotic solvent.6. The method of claim 5 , wherein the polar aprotic solvent is selected from the group consisting of ethylene glycol dimethyl ether claim 5 , diethylene glycol dimethyl ether claim 5 , and triethylene glycol dimethyl ether.7. The method of claim 1 , wherein the primary base in formamidine cyclization of the halogenated acrylate is Hünig's base. Pursuant to 37 C.F.R. § 1.78(a)(4), this application is a divisional of U.S. application Ser. No. 16/103,267, filed Aug. 14, 2018, which was a divisional of U.S. application Ser. No. 14/880,147, filed Oct. 9, 2015, which claimed the benefit of and priority to Provisional Application Ser. No. 62/062,069, filed 9 Oct. 2014. The disclosure of each of these applications is expressly incorporated herein by reference, each in its entirety.The invention described herein may be manufactured and used by or for the Government of the United States for all governmental purposes without the payment of any royalty.The present invention relates generally to inorganic carbene complexes and, ...

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02-01-2020 дата публикации

REVERSIBLY PROTECTED TRIAZABUTADIENES

Номер: US20200002290A1
Принадлежит:

Triazabutadiene molecules and methods of use of triazabutadiene molecules, for example methods and compositions for yielding an aryl diazonium species from a triazabutadiene molecule, e.g., a protected aryl diazonium species in the form of a triazabutadiene. In some embodiments, an enzyme catalyzes the reaction yielding the aryl diazonium species from the triazabutadiene molecule. As an example, the methods and compositions herein may be used for delivery of drugs. 2. The compound of claim 1 , wherein Xand Yare both alkyl.3. The compound of claim 1 , wherein Xis methyl.4. The compound of claim 1 , wherein Yis methyl.5. The compound of claim 1 , wherein Xand Yare methyl.6. The compound of claim 1 , wherein Yis t-butyl.7. The compound of claim 1 , wherein Xand Yare both t-butyl.9. The method of claim 8 , wherein the trigger is basic conditions.10. The method of claim 8 , wherein the trigger is an enzyme.11. The method of claim 8 , wherein the trigger is a redox environment.12. The method of claim 8 , wherein the trigger is a redox environment inside a cell.13. The method of claim 8 , wherein the trigger is light.14. The method of claim 8 , wherein the compound of Formula B is stable in acidic conditions having a pH of 6.0 or less.15. The method of claim 8 , wherein the derivative of Zis a drug or a pro-drug.16. The method of claim 8 , wherein the active triazabutadiene molecule yields an aryl diazonium species.17. The method of claim 8 , wherein Xand Yare both alkyl.18. The method of claim 8 , wherein Xor Yis methyl.19. The method of claim 8 , wherein Xand Yare both methyl.20. The method of claim 8 , wherein X claim 8 , Y claim 8 , or both Xand Yare t-butyl. This application is continuation-in-part of PCT Patent Application No. PCT/US18/22046 filed Mar. 12, 2018, which claims benefit of U.S. Provisional Patent Application No. 62/469,677 filed Mar. 10, 2017, the specifications of which are incorporated herein in their entirety by reference.This application is a ...

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03-01-2019 дата публикации

Methods and systems for mask alignment in manufacturing process of arrays

Номер: US20190002410A1
Принадлежит: HealthTell Inc

Provided herein are molecules and salts thereof, arrays containing molecules and salts thereof, solid supports containing molecules and salts thereof, kits containing molecules or salts thereof, and methods of determining alignment of photolithographic masks comprising molecules or salts thereof.

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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.

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07-01-2021 дата публикации

PHENYL CYCLOHEXANONE DERIVATIVES AND METHODS OF MAKING AND USING THEM

Номер: US20210002214A1
Автор: Wainer Irving W.
Принадлежит:

Phenyl cyclohexanone based active agents, pharmaceutical preparations containing such active agents, methods of modifying cellular activity by contacting cells with such active agents, and methods of treating various conditions by administering such active agents to a patient are described. 2. A stereoisomer of a compound of .4. A phenyl cyclohexanone compound of wherein there is a cis stereochemical relationship between the C2 and C6 chiral centers on the cyclohexanone ring.5. A phenyl cyclohexanone compound of wherein the C2 carbon of the cyclohexanone ring is in an S configuration.6. A pharmaceutical composition comprising a phenyl cyclohexanone compound in accordance with and a pharmaceutically acceptable carrier.7. A method of treatment comprising administering a pharmaceutical composition in accordance with to a patient in need of treatment claim 6 , the compound being present in a therapeutically effective amount.8. The method of wherein the compound or composition is administered to a patient in need of treatment for bipolar depression claim 7 , major depressive disorder claim 7 , schizophrenia claim 7 , Alzheimer's dementia claim 7 , amyotrophic lateral sclerosis claim 7 , complex regional pain syndrome (CRPS) claim 7 , chronic pain claim 7 , or neuropathic pain.9. A method of inhibiting MNDA receptor activity comprising contacting cells with a concentration of a compound in accordance with sufficient to inhibit MNDA receptor activity.10. A method of modifying endogenous concentrations of D-Serine comprising contacting cells with a concentration of a compound in accordance with sufficient to modify endogenous concentrations of D-Serine.11. A method of stimulating the activating phosphorylation of mTOR comprising contacting cells with a concentration of a compound in accordance with sufficient to stimulate the activating phosphorylation of mTOR.12. A method of inhibiting nAChR activity comprising contacting cells with a concentration of a compound in ...

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07-01-2016 дата публикации

SYNTHESIS AND USE OF BIOBASED IMIDAZOLIUM CARBOXYLATES

Номер: US20160002796A1
Принадлежит:

The present invention relates to a new method for preparation of biobased imidazolium salts and derivatives thereof; in particular, for the preparation of imidazolium hydrogenooxalate. The present invention also relates to uses of imidazolium hydrogenooxalate salts, especially as a precursor of imidazolium carboxylate compounds. The present invention also refers to a green electrochemical process providing imidazolium compounds, especially imidazolium carboxylate compounds. Especially, the invention refers to a one-compartment electrochemical cell and its use for the preparation of imidazolium carboxylate compounds of formula (II): 2. The method of claim 1 , wherein the supporting electrolyte is a halogen-free imidazolium salt.3. The method of claim 1 , wherein the supporting electrolyte is imidazolium hydrogeno-oxalate salts and derivatives thereof.4. The method of claim 1 , wherein the imidazolium salt is a biosourced compound.5. The method of claim 1 , wherein the electrochemical cell is constituted by only one compartment.6. The method of claim 1 , further comprising a carbon dioxide source.7. The method of claim 1 , wherein the products of the oxidation step do not contaminate the products of the reduction step.9. The one-compartment electrochemical cell of claim 8 , wherein subproducts of an oxidation reaction occurring within the cell are non-toxic compounds claim 8 , easy to remove from a final reaction medium.10. The one-compartment electrochemical cell of claim 8 , further comprising a source of carbon dioxide.15. A cyclic process for delivering carbon dioxide stocked in a material claim 8 , membrane support claim 8 , solid or liquid claim 8 , comprising:contacting an imidazolium carboxylate compound with oxalic acid or formic acid to synthesize an imidazolium hydrogeno-oxalate or imidazolium formate salt and produce carbon dioxide; andregenerating an imidazolium carboxylate compound by an electrochemical process from the imidazolium hydrogeno-oxalate or ...

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04-01-2018 дата публикации

AGENTS FOR IMPROVED DELIVERY OF NUCLEIC ACIDS TO EUKARYOTIC CELLS

Номер: US20180002724A1
Принадлежит:

New cationic lipids are provided that are useful for delivering macromolecules, such as nucleic acids, into eukaryotic cells. The lipids can be used alone, in combination with other lipids and/or in combination with other transfection enhancing reagents to prepare transfection complexes. 213-. (canceled)14. A composition comprising a compound according to and at least one cationic lipid.15. A composition comprising a compound according to and at least one neutral lipid.1617-. (canceled)18. The composition according to further comprising at least one additional neutral lipid.19. (canceled)20. A composition comprising a compound according to and a polyamine transfection agent.21. (canceled)22. A composition comprising a compound according to and a fusion agent.2324-. (canceled)25. A composition comprising a compound according to and a cell surface ligand claim 1 , wherein said cell surface ligand optionally comprises a polycationic nucleic acid binding moiety.26. (canceled)27. A composition comprising a compound according to and a nuclear localization peptide or protein claim 1 , wherein said nuclear localization peptide or protein optionally comprises a polycationic nucleic acid binding moiety.2829-. (canceled)30. A composition according to claim 1 , further comprising an amphipathic peptide claim 1 , wherein said amphipathic peptide optionally comprises a polycationic nucleic acid binding moiety.31. (canceled)32. A composition according to claim 1 , further comprising a nucleic acid.33. A method of introducing a nucleic acid into a eukaryotic cell claim 1 , comprising contacting the cell with the nucleic acid and a composition according to claim 1 , thereby introducing the nucleic acid claim 1 , protein claim 1 , or peptide into the cell.3435-. (canceled)36. A kit comprising a compound according to and a neutral lipid.37. A kit comprising a compound according to and one or more reagents selected from the group consisting of a cationic lipid claim 1 , an amphipathic ...

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01-01-2015 дата публикации

BACKFLUORINATED NHC CARBENES AND COMPLEXES

Номер: US20150004322A1
Автор: Blanski Rusty Lew
Принадлежит:

N-heterocyclic (“NHC”) carbenes and NHC carbene-metal complexes. The NHC carbene having a formula: 3. An N-heterocyclic carbene-metal complex comprising:an inorganic metal complex; and{'claim-ref': {'@idref': 'CLM-00002', 'claim 2'}, 'at least one ligand selected from the N- heterocyclic carbene of .'}4. The N-heterocyclic carbene-metal complex of claim 3 , wherein the metal is selected from the group consisting of rhenium claim 3 , ruthenium claim 3 , osmium claim 3 , rhodium claim 3 , iridium claim 3 , palladium claim 3 , platinum claim 3 , silver claim 3 , gold claim 3 , cobalt claim 3 , nickel claim 3 , palladium claim 3 , platinum claim 3 , and copper.6. The N-heterocyclic carbene-metal complex of claim 5 , wherein M is selected from the group consisting of rhenium claim 5 , ruthenium claim 5 , osmium claim 5 , rhodium claim 5 , iridium claim 5 , palladium claim 5 , platinum claim 5 , silver claim 5 , gold claim 5 , cobalt claim 5 , nickel claim 5 , palladium claim 5 , platinum claim 5 , and copper.7. The N-heterocyclic carbene-metal complex of claim 2 , wherein each of Rand Ris further substituted with a fluorinated or partially fluorinated group claim 2 , C-Calkyl claim 2 , C-Calkoxy claim 2 , C-Calkyl claim 2 , C-Calkoxy claim 2 , and a halogen substituted phenyl group.8. The N-heterocyclic carbene-metal complex of claim 1 , wherein M is selected from the group consisting of rhenium claim 1 , ruthenium claim 1 , osmium claim 1 , rhodium claim 1 , iridium claim 1 , palladium claim 1 , platinum claim 1 , silver claim 1 , gold claim 1 , cobalt claim 1 , nickel claim 1 , palladium claim 1 , platinum claim 1 , and copper.9. A method of depositing a noble metal onto a substrate using a supercritical fluid deposition process in a cold wall reactor claim 1 , the method comprising:exposing the substrate to a supercritical solvent in a supercritical state;{'claim-ref': {'@idref': 'CLM-00007', 'claim 7'}, 'dissolving the N-heterocyclic carbene-metal complex of in the ...

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12-01-2017 дата публикации

ETHYNYL DERIVATIVES

Номер: US20170008854A1
Принадлежит: Hoffmann-La Roche Inc.

The present invention relates to compounds useful for the treatment of Parkinson's disease, anxiety, emesis, obsessive compulsive disorder, autism, neuroprotection, cancer, depression and diabetes type 2. 3. A compound of formula I according to claim 1 , wherein the compound is3-[2,6-difluoro-4-(2-phenylethynyl)phenyl]-1-isopropyl-imidazolidine-2,4-dione(5RS)-3-[2,6-difluoro-4-(2-phenylethynyl)phenyl]-1-isopropyl-5-methyl-imidazolidine-2,4-dione3-[2,6-difluoro-4-(2-phenylethynyl)phenyl]-1-isopropyl-5,5-dimethyl-imidazolidine-2,4-dione3-[2,6-difluoro-4-(2-phenylethynyl)phenyl]-5,5-dimethyl-1-phenyl-imidazolidine-2,4-dione 1-tert-butyl-3-[2,6-difluoro-4-(2-phenylethynyl)phenyl]imidazolidine-2,4-dione1-cyclopropyl-3-[2,6-difluoro-4-(2-phenylethynyl)phenyl]imidazolidine-2,4-dione or7-[2,6-difluoro-4-(2-phenylethynyl)phenyl]-5-isopropyl-2-oxa-5,7-diazaspiro[3.4]octane-6,8-dione.5. A compound of formula I according to claim 1 , wherein the compound is(5RS,8aRS)-2-[2,6-difluoro-4-(2-phenylethynyl)phenyl]-5-methyl-5,6,8,8a-tetrahydroimidazo[5,1-c][1,4]oxazine-1,3-dione(3aRS)-2-[2,6-difluoro-4-(2-phenylethynyl)phenyl]-3a,4-dihydroimidazo[1,5-a]indole-1,3-dione(3aRS)-2-[2,6-difluoro-4-(2-phenylethynyl)phenyl]-4,5-dihydro-3aH-imidazo[1,5-a]quinoline-1,3-dione(10aRS)-2-[2,6-difluoro-4-(2-phenylethynyl)phenyl]-10,10a-dihydro-5H-imidazo[1,5-b]isoquinoline-1,3-dione(5RS,8aRS)-2-[2-chloro-4-(2-phenylethynyl)phenyl]-5-methyl-6,7,8,8a-tetrahydro-5H-imidazo[1,5-a]pyridine-1,3-dione or(5RS,8aRS)-2-[2-chloro-6-fluoro-4-[2-(3-pyridyl)ethynyl]phenyl]-5-methyl-6,7,8,8a-tetrahydro-5H-imidazo[1,5-a]pyridine-1,3-dione.7. A pharmaceutical composition comprising a compound of formula I according to and a pharmaceutically acceptable excipient.8. A method for the treatment of Parkinson's disease claim 1 , anxiety claim 1 , emesis claim 1 , obsessive compulsive disorder claim 1 , autism claim 1 , neuroprotection claim 1 , cancer claim 1 , depression claim 1 , schizophrenia and diabetes type 2 of a ...

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14-01-2016 дата публикации

SUPRAMOLECULAR MATERIALS MADE OF OLIGOAMIDES

Номер: US20160009656A1
Принадлежит:

The present invention relates to novel supramolecular materials made of straight or branched oligoamides, terminated at each of the ends thereof by an associative group including a nitrogen heterocycle supported by a specific sequence. The invention also relates to the method for preparing said materials, as well as to the uses thereof. 1. A material comprising linear or branched oligoamides X.Y terminated at more than 90% by number of their ends by one and the same group -M-L-CO-L-A , where A is an associative group comprising a nitrogenous heterocycle; Lis a chemical bond or a spacer arm consisting of a saturated or unsaturated and cyclic or noncyclic hydrocarbon chain optionally interrupted by one or more oxygen and/or nitrogen atoms; Lis a saturated or unsaturated and cyclic or noncyclic hydrocarbon chain which includes at least 4 carbon atoms , which is optionally interrupted by one or more oxo groups and which is optionally substituted by one or more —OH groups and/or one or more chlorine atoms; and M is selected from the group consisting of CO , NH and O groups.2. The material as claimed in claim 1 , wherein the material comprises oligomers corresponding to the formula (Ia) below:{'br': None, 'sub': 'a', 'X—NH—Ra—NH—[CO—Rb—CO—NH—Ra—NH—]—X \u2003\u2003(Ia)'}where:Ra denotes a saturated or unsaturated hydrocarbon chain optionally interrupted by one or more oxygen and/or nitrogen atoms,Rb denotes a saturated or unsaturated hydrocarbon chain,a denotes the mean number of units per chain and is greater than 0 and less than or equal to 20,{'sub': 1', '2, 'X denotes an A-L-CO-L-CO— group'} A is an associative group comprising a nitrogenous heterocycle,', {'sub': '1', 'Lis a chemical bond or a spacer arm consisting of a saturated or unsaturated and cyclic or noncyclic hydrocarbon chain optionally interrupted by one or more nitrogen and/or oxygen atoms, and'}, {'sub': '2', 'Lis a saturated or unsaturated and cyclic or noncyclic hydrocarbon chain which includes at least ...

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14-01-2021 дата публикации

COMPOUND AND ORGANIC ELECTROLUMINESCENCE DEVICE USING THE SAME

Номер: US20210009527A1
Принадлежит: IDEMITSU KOSAN CO.,LTD.

A compound represented by the following formula (1), wherein Xis O or S, and two or more of Y, Yand Yare N, provided that the case where one or both of —Ar—Arand —Ar—Aris a p-terphenyl-3-yl group is excluded. 2. The compound according to claim 1 , wherein Arand Arare independentlyan unsubstituted phenyl group,a substituted or unsubstituted naphthyl group,a substituted or unsubstituted phenanthryl group, ora substituted or unsubstituted anthryl group.3. The compound according to or claim 1 , wherein{'sub': 1', '3', '2', '4, 'when Arand Arare an unsubstituted phenylene group, Arand Arare independently'}an unsubstituted phenyl group,a substituted or unsubstituted naphthyl group,a substituted or unsubstituted phenanthryl group, ora substituted or unsubstituted anthryl group.4. The compound according to claim 1 , wherein Arand Are claim 1 , and Arand Arindependently do not form a ring by bonding with each other.5. The compound according to claim 1 , wherein{'sub': 1', '4, 'when Arto Arare substituted by a substituent, the substituent is'}an unsubstituted phenyl group,an unsubstituted naphthyl group,an unsubstituted phenanthryl group,an unsubstituted anthryl group,an unsubstituted biphenyl group,an unsubstituted alkyl group including 1 to 50 carbon atoms, oran unsubstituted cycloalkyl group including 3 to 50 ring carbon atoms.10. the compound according to claim 6 ,{'sub': 'a', "wherein the one or more sets of adjacent two or more R's do not form a ring by bonding with each other."}11. The compound according to claim 1 , wherein Arand Arare independentlyan unsubstituted phenyl group,an unsubstituted naphthyl group,an unsubstituted anthryl group, oran unsubstituted phenanthryl group.12. The compound according to claim 1 , wherein Xis S.13. The compound according to claim 1 , wherein Yto Yare N.23. An electron-transporting material for an organic electroluminescence device claim 1 , which comprises the compound according to .24. An organic electroluminescence device ...

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11-01-2018 дата публикации

Ionic Liquid, Lubricant, and Magnetic Recording Medium

Номер: US20180012623A1
Принадлежит:

A lubricant including an ionic liquid including a conjugate base and a conjugate acid, wherein the conjugate acid includes a straight-chain hydrocarbon group having 6 or greater carbon atoms and a straight chain hydrocarbon group s having 6 or greater but 14 or less carbon atoms, and wherein a pKa of an acid that is a source of the conjugate base in acetonitrile is 10 or less. 1. A lubricant comprising:an ionic liquid including a conjugate base and a conjugate acid,wherein the conjugate acid includes a straight-chain hydrocarbon group having 6 or greater carbon atoms and a straight-chain hydrocarbon group having 6 or greater but 14 or less carbon atoms, andwherein a pKa of an acid that is a source of the conjugate base in acetonitrile is 10 or less.5. A magnetic recording medium comprising:a non-magnetic support;a magnetic layer disposed on the non-magnetic support; and{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'the lubricant according to , disposed on the magnetic layer.'}6. An ionic liquid comprising:a conjugate base; anda conjugate acid,wherein the conjugate acid includes a straight-chain hydrocarbon group having 6 or greater carbon atoms and a straight-chain hydrocarbon group having 6 or greater but 14 or less carbon atoms, andwherein a pKa of an acid that is a source of the conjugate base in acetonitrile is 10 or less. The present invention relates to an ionic liquid, a lubricant containing the ionic liquid, and a magnetic recording medium using the lubricant.Conventionally, in a thin film magnetic recording medium, a lubricant is applied onto a surface of a magnetic layer for the purpose of reducing frictions between a magnetic head and the surface of the magnetic recording medium, or reducing abrasion. In order to avoid adhesion, such as sticktion, an actual film thickness of the lubricant is of a molecular order. Accordingly, it is not exaggeration to say that the most important thing for a thin film magnetic recording medium is to select a lubricant ...

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03-02-2022 дата публикации

OPHTHALMIC COMPOSITIONS AND METHODS FOR THE TREATMENT OF SKIN DISEASES AND EYE DISEASES

Номер: US20220033360A1
Автор: Kandula Mahesh
Принадлежит: Cellix Bio Private Limited

The invention relates to the compounds or its pharmaceutical acceptable polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, formula II, formula III and formula IV and the methods for the treatment of eye disorders and skin diseases and may be formulated for the topical eye drop, topical paste, ocular solution, device-drug delivery, oral, buccal, rectal, topical, transdermal, transmucosal, lozenge, spray, intravenous, oral solution, nasal spray, oral solution, cream, dermal ointment, gels, lotions, suspension, oral spray, buccal mucosal layer tablet, parenteral administration, syrup, or injection. Such compositions may be used to treatment of skin diseases and eye diseases. 24.-. (canceled)5. A pharmaceutical composition comprising a compound of and a pharmaceutically acceptable carrier.6. The pharmaceutical composition of claim 5 , wherein said pharmaceutical composition is formulated for topical eye drop claim 5 , topical paste claim 5 , ocular solution claim 5 , device-drug delivery claim 5 , oral admiration claim 5 , buccal admiration claim 5 , rectal admiration claim 5 , topical admiration claim 5 , transdermal admiration claim 5 , transmucosal admiration claim 5 , lozenge claim 5 , spray claim 5 , intravenous admiration claim 5 , oral solution claim 5 , nasal spray claim 5 , cream claim 5 , dermal ointment claim 5 , gels claim 5 , lotions claim 5 , suspension claim 5 , oral spray claim 5 , buccal mucosal layer tablet claim 5 , parenteral administration claim 5 , syrup claim 5 , or injection.7. The pharmaceutical compositions of claim 6 , wherein said pharmaceutical compositions are formulated for the treatment of eye disorders and skin diseases.816.-. (canceled)18. A pharmaceutical composition comprising a compound of and a pharmaceutically acceptable carrier.19. The pharmaceutical composition of claim 18 , wherein said pharmaceutical composition is ...

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15-01-2015 дата публикации

ARGININE-BASED LIPIDS FOR DELIVERY OF THERAPEUTICS

Номер: US20150017233A1
Принадлежит:

This disclosure provides a range of amino acid lipid compounds and compositions useful for drug delivery, therapeutics, and the diagnosis and treatment of diseases and conditions. The amino acid lipid compounds and compositions can be used for delivery of various agents such as nucleic acid therapeutics to cells, tissues, organs, and subjects. 2. The compound of claim 1 , wherein Rand Rare C(12-22)alkyl and are the same or different.3. The compound of claim 1 , wherein Rand Rare C(12-22)alkenyl and are the same or different.4. The compound of claim 1 , wherein Ris C(12-22)alkyl and Ris C(12-22)alkenyl.5. The compound of claim 1 , wherein Ris C(12-22)alkyl and Ris C(12-22)alkenyl.6. The compound of claim 1 , wherein a peptide is attached to the side chain of Xaa.7. The compound of claim 1 , selected from (C12acyl)-nor-norarginine-NH—(C12alkyl) claim 1 , (C14acyl)-nor-norarginine-NH—(C14alkyl) claim 1 , (C16acyl)-nor-norarginine —NH—(C16alkyl) claim 1 , (C18acyl)-nor-norarginine-NH—(C18alkyl) claim 1 , (C12acyl)-homoarginine-NH—(C12alkyl) claim 1 , (C14acyl)-homoarginine-NH—(C14alkyl) claim 1 , (C16acyl)-homoarginine-NH—(C16alkyl) claim 1 , and (C18acyl)-homoarginine-NH—(C18alkyl).8. The compound (C12acyl)-nor-norarginine-NH—(C12alkyl).9. A composition comprising one or more compounds according to and one or more therapeutic nucleic acids.10. The composition of claim 9 , wherein the therapeutic nucleic acid is a gene silencing agent.11. The composition of claim 9 , wherein the therapeutic nucleic acid is a RNAi-inducing agent.12. The composition of claim 9 , wherein the therapeutic nucleic acid is a double-stranded RNA.13. The composition of claim 9 , wherein the therapeutic nucleic acid is an mdRNA.14. The composition of claim 9 , wherein the therapeutic nucleic acid contains a modified nucleoside.15. The composition of claim 9 , further comprising cholesteryl hemisuccinate.16. The composition of claim 9 , further comprising one or more cationic lipids.17. The ...

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15-01-2015 дата публикации

IMIDAZOLIDINEDIONE DERIVATIVES

Номер: US20150018377A1
Принадлежит: AUTIFONY THERAPEUTICS LIMITED

The invention provides a compound of formula (Ia), and pharmaceutically acceptable salts thereof. The invention also provides use of the compounds or salts as modulators of Kv3.1 and/or Kv3.2, and in the treatment of diseases or disorders where a modulator of Kv3.1 and/or Kv3.2 is required, such as depression and mood disorders, hearing disorders, schizophrenia, substance abuse disorders, sleep disorders or epilepsy. 114-. (canceled) This application is a continuation of U.S. application Ser. No. 13/515,097 (U.S. Pat. No. 8,722,695 issued May 13, 2014), filed Jun. 11, 2012 (published as US 2012-0289526 A1), which is a U.S. national phase of International Application No. PCT/EP2010/068946 filed 6 Dec. 2010, which designated the U.S. and claims priority to GB 0921760.5 filed 11 Dec. 2009 and GB 1012924.5 filed 30 Jul. 2010, the entire contents of each of which are hereby incorporated by reference.This invention relates to novel compounds, pharmaceutical compositions containing them and their use in therapy, in particular as antipsychotic agents.The Kv3 voltage-gated potassium channel family includes four members, Kv3.1, Kv3.2, KV3.3, and Kv3.4. Genes for each of these subtypes can generate multiple isoforms by alternative splicing, producing versions with different C-terminal domains. Thirteen isoforms have been identified in mammals to date, but the currents expressed by these variants appear identical (Rudy and McBain, 2001, Trends in Neurosciences 24, 517-526). Kv3 channels are activated by depolarization of the plasma membrane to voltages more positive than −20 mV; furthermore, the channels deactivate rapidly upon repolarization of the membrane. These biophysical properties ensure that the channels open towards the peak of the depolarizing phase of the neuronal action potential to initiate repolarization. Rapid termination of the action potential mediated by Kv3 channels allows the neuron to recover more quickly to reach sub-threshold membrane potentials from ...

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17-01-2019 дата публикации

IMIDAZOLINE COMPOUND, MOBILITY CONTROL SYSTEM, PLUGGING AGENT FOR GAS CHANNELING, AND METHOD FOR CARBON DIOXIDE FLOODING

Номер: US20190016683A1
Принадлежит:

An imidazoline compound, a mobility control system, a plugging agent for gas channeling, and a method for carbon dioxide flooding. The structure of the imidazoline compound is represented by formula (1), in which R is pentadecyl, heptadecenyl, or heptadecyl. A mobility control system that contains the imidazoline compound can interact with carbon dioxide to form a plugging agent for gas channeling, and thereby attains a plugging effect for carbon dioxide channeling in a carbon dioxide flooding process. 2. A mobility control system claim 1 , comprising the imidazoline compound of claim 1 , a mobility control additive claim 1 , and water.3. The mobility control system of claim 2 , wherein claim 2 , the mobility control additive is selected from the group consisting of sodium salicylate claim 2 , maleic acid claim 2 , sodium p-toluene sulfonate claim 2 , and combinations thereof.4. The mobility control system of claim 3 , wherein claim 3 , R is pentadecyl claim 3 , and the mobility control additive is sodium p-toluene sulfonate.5. The mobility control system of claim 2 , wherein claim 2 , as percentages of the weight of the mobility control system claim 2 , the content of the imidazoline compound is 1-10 wt. % claim 2 , the content of the mobility control additive is 0.1-2 wt. % claim 2 , and the content of water is 88-98.9 wt. %.6. The mobility control system of claim 5 , wherein claim 5 , as percentages of the weight of the mobility control system claim 5 , the content of the imidazoline compound is 2-6 wt. % claim 5 , the content of the mobility control additive is 0.4-0.8 wt. % claim 5 , and the content of water is 93.2-97.6 wt. %.7. A plugging agent for gas channeling claim 2 , wherein the plugging agent for gas channeling is a mixture obtained by introducing carbon dioxide into the mobility control system of to form a gel.8. The plugging agent for gas channeling of claim 7 , wherein the mobility control additive is selected from the group consisting of sodium ...

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16-01-2020 дата публикации

NOVEL 5-ACYLSULFANYL-HISTIDINE COMPOUNDS AS PRECURSORS OF THE CORRESPONDING 5-SULFANYLHISTIDINES AND THEIR DISULFIDES

Номер: US20200017479A1
Принадлежит:

The invention relates to a 5-acylsulfanyl-histidine compound and the derivatives thereof, of general formula (I), 2. The compound of claim 1 , wherein Rrepresents hydrogen claim 1 , methyl claim 1 , acetyl claim 1 , benzoyl claim 1 , α-aminoacyl or β-alanyl (HNCHCH(C═O).3. A 5-sulfanylhistidine compound selected from the group consisting of:the disulfide of L-5-sulfanyl-α,N(methyl)-histidine (Compound 22);L-5-sulfanyl-α,N(methyl)-histidine (Compound 23);the disulfide of L-5-sulfanyl-α,N,N(dimethyl)-histidine (Compound 24);L-5-sulfanyl-α,N,N(dimethyl)-histidine (Compound 25);L-5-sulfanyl-α,N,N,N(trimethyl)-histidine (Compound 26);the disulfide of L-5-sulfanyl-α,N,N,N(trimethyl)-histidine (Compound 27);the disulfide of L-5-sulfanyl-α,N(acetyl)-histidine (Compound 28);L-5-sulfanyl-α,N(acetyl)-histidine (Compound 29);L-5-sulfanylcarnosine (Compound 30);the disulfide of iso-ovothiol A (Compound 31);L-5-sulfanyl-1-methyl-histidine named iso-ovothiol A (Compound 32);the disulfide of L-5-sulfanyl-α,N,N(dimethyl)-1-methylhistidine (Compound 33);L-5-sulfanyl-α,N,N,N(trimethyl)-1-methylhistidine (Compound 34);L-5-sulfanyl-α,N(L-alanyl)-histidine (Compound 35); andthe disulfide of 5-sulfanyl-α,N(pentanoyl)-histidine (Compound 36).5. The compound of claim 4 , wherein the mineral acid is selected from the group consisting of hydrochloric claim 4 , hydrobromic claim 4 , hydroiodic claim 4 , sulfuric claim 4 , and phosphoric acid.6. The compound of claim 4 , wherein the organic acid is selected from the group consisting of formic claim 4 , acetic claim 4 , tartaric claim 4 , trifluoroacetic claim 4 , propionic claim 4 , benzoic claim 4 , maleic claim 4 , fumaric claim 4 , succinic claim 4 , citric claim 4 , oxalic claim 4 , glyoxylic claim 4 , and aspartic acid.7. The compound of claim 4 , wherein the alkanesulfonic acid is selected from the group consisting of methanesulfonic claim 4 , trifluoromethanesulfonic claim 4 , and ethanesulfonic acid.8. The compound of claim 4 , wherein ...

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21-01-2021 дата публикации

1,4-DIPHENYL-1H-IMIDAZOLE AND 2,4-DIPHENYLTHIAZOLE DERIVATIVES AND PREPARATION METHOD THEREFOR AND USE THEREOF

Номер: US20210017189A1
Принадлежит: SOUTHERN MEDICAL UNIVERSITY

Provided are 1,4-diphenyl-1H-imidazole and 2,4-diphenylthiazole derivatives having a structure represented by Formula I, a preparation method therefor and uses thereof: 9. A pharmaceutical composition claim 1 , comprising the compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , a pharmaceutically acceptable carrier thereof or an excipient thereof.10. A method of preparing of anti-inflammatory adjuvants claim 1 , TLR1 or TLR2 agonists claim 1 , and anti-tumor agents claim 1 , comprising the step using the compound according to .11. A method for regulating an activity activation level of TLR1 and TLR2 alkaline phosphatases in vitro and in vivo claim 1 , comprising administering the compound according to to a subject. This application is the national phase entry of International Application No. PCT/CN2018/082243, filed on Apr. 9, 2018, the entire contents of which are incorporated herein by reference.The present invention relates to the fields of medicine and health and chemical engineering, and specifically to a series of compounds of TLR1/2 agonists, which can be used in the fields of scientific research, health care and chemical engineering.The immune system is an important system for the body to implement immune responses and immune functions. It is composed of immune organs, immune cells and immune molecules. The function of the immune system is to recognize and eliminate antigenic foreign bodies to maintain a stable environment and physiological balance in the body. Autoimmune diseases are mainly caused by the accumulation of a large number of immune cells and immunoglobulins as a result of an excessive immune response.The growth and development of mammals are accompanied by immune system disorders and inflammatory responses. The inflammatory response protects the body from harmful stimuli and invading pathogens by activating innate and adaptive immune responses to repair the immune system of damaged tissues. In this process, ...

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28-01-2016 дата публикации

Compounds Useful for Promoting Protein Degradation and Methods Using Same

Номер: US20160022642A1
Принадлежит:

The present description includes compounds that act as degraders of a target protein, wherein degradation is independent of the class of the target protein or its localization. In certain embodiments, the description includes a compound comprising a protein degradation moiety covalently bound to a linker, wherein the ClogP of the compound is equal to or higher than 1.5. The target protein contemplated within the description comprises an androgen receptor. Compounds of the present description may be used to treat disease states wherein protein degradation is a viable therapeutic approach, such as cancer or any sort of oxidative stress disease state. 2. The composition of claim 1 , wherein L-DM has a ClogP value equal to or higher than about 2.0.3. The composition of claim 1 , wherein L-DM has a ClogP value equal to or higher than about 3.0.5. The composition of claim 1 , wherein L ranges in length from 2 to 60 atoms.6. The composition of claim 5 , wherein L ranges in length from 2 to 8 atoms.7. The composition of claim 1 , wherein L comprises from 1 to 15 ethylene oxide groups.9. The composition of claim 8 , wherein each occurrence of ‘i’ is independently an integer ranging from 1 to 8.13. The composition of claim 1 , further comprising a pharmaceutically acceptable carrier.14. The composition of claim 1 , further comprising a bioactive agent.15. The composition of claim 14 , wherein the bioactive agent comprises a HSP90 modulator or a HSP70 modulator.16. The composition of claim 15 , wherein the HSP90 modulator comprises geldanamycin claim 15 , 17AAG/KOS953 claim 15 , 17-DMAG claim 15 , CNF1010 claim 15 , tanespimycin claim 15 , alvespimycin claim 15 , KOS 1022 claim 15 , retaspimycin or 17-AAG hydroquinone claim 15 , KOSN 1559 claim 15 , PU3 claim 15 , PUH58 claim 15 , PU24S claim 15 , PU24FCl claim 15 , BIIBO21 claim 15 , CCT018159 claim 15 , G3219 claim 15 , G3130 claim 15 , VER49009/CCT0129397 claim 15 , VER50589 claim 15 , STA-9090 claim 15 , VER52296/NVP- ...

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22-01-2015 дата публикации

Treatment and Diagnosis of Melanoma

Номер: US20150023955A1
Принадлежит: THE ROCKEFELLER UNIVERSITY

The present invention discloses novel agents and methods for diagnosis and treatment of melanoma. Also disclosed are related arrays, kits, and screening methods. 1. A method of treating cancer in a subject in need thereof , comprising administering to the subject a LXRβ agonist , or a pharmaceutically acceptable salt thereof , wherein the cancer is melanoma.2. The method of claim 1 , wherein said LXRβ agonist is selective for LXRβ over LXRα.5. The method of claim 1 , wherein said LXRβ agonist is compound 2 claim 1 , compound 12 claim 1 , compound 25 claim 1 , compound 38 claim 1 , or compound 39 claim 1 , or a pharmaceutically acceptable salt thereof.6. The method of claim 1 , comprising administration of an additional anticancer therapy.7. The method of claim 6 , wherein said additional anticancer therapy is an antiproliferative.8. The method of claim 7 , wherein said antiproliferative is a BRAF inhibitor claim 7 , a CTLA-4 inhibitor claim 7 , a PD1 inhibitor claim 7 , a MEK inhibitor claim 7 , an ERK inhibitor claim 7 , and/or a PDL1 inhibitor.9. The method of claim 8 , wherein said antiproliferative is vemurafenib claim 8 , dacarbazine claim 8 , trametinib claim 8 , dabrafenib claim 8 , MEDI-4736 claim 8 , a PD1 antibody claim 8 , a PDL-1 antibody claim 8 , and/or a CTLA-4 antibody.10. The method of claim 8 , wherein said antiproliferative is a CTLA-4 antibody that is ipilimumab or a PD1 antibody that is pembrolizumab or nivolumab.11. The method of claim 1 , wherein said melanoma is metastatic.12. The method of claim 1 , wherein said melanoma is drug resistant.13. The method of claim 12 , wherein said melanoma is resistant to a BRAF inhibitor claim 12 , a CTLA4 inhibitor claim 12 , a PD1 inhibitor claim 12 , a MEK inhibitor claim 12 , an ERK inhibitor claim 12 , and/or a PDL1 inhibitor.14. The method of claim 13 , wherein said melanoma is resistant to vemurafenib claim 13 , ipilimumab claim 13 , trametinib claim 13 , dabrafenib claim 13 , pembrolizumab claim 13 , ...

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28-01-2016 дата публикации

COMPOUNDS AND METHOD FOR ENHANCED OIL RECOVERY USING SULFUR SURFACTANTS

Номер: US20160024373A1
Принадлежит: Ingevity South Carolina, LLC

A method of enhanced oil recovery wherein: (a) a flooding composition is delivered into a subterranean reservoir; (b) the flooding composition includes a sulfur surfactant; and (c) the fluid produced from the subterranean reservoir can also be analyzed to determine if the surfactant is present in the fluid. The surfactant preferably includes a sulfonate moiety or other sulfur-containing moiety. The presence of the surfactant in the fluid produced from the subterranean reservoir is preferably determined by X-ray fluorescence spectroscopy, HPLC-AES, or HPLC-ICP. This application claims the benefit of U.S. Provisional Patent Application Ser. No. 61/786,662 filed on Mar. 15, 2013 and incorporates said provisional application by reference into this document as if fully set out at this point.The present invention relates to compounds, compositions, and methods for enhanced oil recovery using novel surfactants and methods of detection.A need exists for improved reservoir flooding compositions, surfactants, and methods for enhanced oil recovery. In particular, a need exists for such improved compositions and surfactants which can be used to: (1) increase oil recovery from the reservoir; (2) reduce adsorption of the surfactant on the rock formation surface; (3) better analyze and understand the geology of the reservoir during trials, (4) detect and quantify the adsorption of the flooding surfactant on the formation rock; (5) understand other phenomena occurring in the reservoir during enhanced oil recovery; and (6) optimize final commercial flooding operations and other enhanced oil recovery procedures performed in the reservoir.The present invention provides a composition, method, and compounds for enhanced oil recovery which satisfy the needs and alleviate the problems discussed above.In one aspect, there is provided an inventive method of enhanced oil recovery from a subterranean reservoir comprising the step of delivering an inventive flooding composition into the ...

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