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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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Применить Всего найдено 2986. Отображено 100.

22-03-2012 дата публикации

Metallo-beta-lactamase inhibitors

Номер: US20120071457A1

Автор: Akihiro Morinaka, Ken Chikauchi, Mizuyo Ida, Takao Abe, Toshiaki Kudo, Yukiko Hiraiwa

Принадлежит: Individual

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

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Номер записи: 1

06-09-2012 дата публикации

Production of carboxylic acid and salt co-products

Номер: US20120225095A1

Автор: Michael V. Guettler, Robert J. Hanchar, Susanne Kleff

Принадлежит: MICHIGAN BIOTECHNOLOGY INSTITUTE

This invention provide processes for producing carboxylic acid product, along with useful salts. The carboxylic acid product that is produced according to this invention is preferably a C 2 -C 12 carboxylic acid. Among the salts produced in the process of the invention are ammonium salts.

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Номер записи: 2

01-11-2012 дата публикации

Ethanamine Compounds and Methods of Using the Same

Номер: US20120277272A1

Автор: David Nugiel, Glen E. Ernst, John P. Mccauley, Lihong Shen, Michael Balestra, Peter Bernstein, William Frietze

Принадлежит: AstraZeneca AB

(S)-2-methyl- 1 -phenyl-2-(pyridin-2-yl)propan-1-amine, pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising the same, uses of said compound or salt for therapy of depression and other conditions, and methods of treating depression and other conditions by administering said compound or salt.

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Номер записи: 3

21-03-2013 дата публикации

CRYSTALLINE FORMS OF A PURINE DERIVATIVE

Номер: US20130072504A1

Автор: Atherton Jonathan Charles Christian, Fernades Philippe, Northen Julian Scott, Skead Benjamin Mark, Worrall Christopher Peter

Принадлежит: CYCLACEL LIMITED

The present invention relates to new crystalline forms of a purine derivative which exhibits excellent anti-tumour activity. The invention also relates to a pharmaceutical composition containing said crystalline forms as an active ingredient, and use thereof in the prevention or treatment of disease. The invention further relates to a process for preparing the crystalline forms. 2. The crystalline form of which is a tartrate salt.3. The crystalline form of which is characterized by an x-ray powder diffraction pattern having two or more diffraction peaks at 2[theta] values selected from 6.67±0.2 claim 2 , 8.237±0.2 claim 2 , 9.777±0.2 claim 2 , 11.96±0.2 claim 2 , 12.38±0.2 claim 2 , 13.06±0.2 claim 2 , 13.38±0.2 claim 2 , 13.94±0.2 claim 2 , 14.90±0.2 claim 2 , 15.40±0.2 claim 2 , 15.95±0.2 claim 2 , 16.27±0.2 claim 2 , 16.54±0.2 claim 2 , 17.36±0.2 claim 2 , 17.57±0.2 claim 2 , 17.86±0.2 claim 2 , 19.64±0.2 claim 2 , 19.86±0.2 claim 2 , 20.12±0.2 claim 2 , 20.73±0.2 claim 2 , 21.14±0.2 claim 2 , 21.58±0.2 claim 2 , 22.57±0.2 claim 2 , 22.95±0.2 claim 2 , 23.29±0.2 claim 2 , 23.57±0.2 claim 2 , 24.07±0.2 claim 2 , 24.63±0.2 claim 2 , 25.30±0.2 claim 2 , 26.38±0.2 claim 2 , 27.09±0.2 claim 2 , 27.67±0.2 claim 2 , 27.97±0.2 claim 2 , 28.91±0.2 claim 2 , 29.28±0.2 claim 2 , 30.08±0.2 claim 2 , 30.41±0.2 claim 2 , 31.90±0.2 and 34.49±0.2 (Form E).45-. (canceled)6. The crystalline form of which is characterized by a differential scanning calorimetry trace recorded at a heating rate of 20° C. per minute which shows a maximum endothermic peak at a temperature between about 176° C. and about 185° C. claim 2 , or a differential scanning calorimetry trace substantially in accordance with that shown in .7. (canceled)8. The crystalline form of which is characterized by an x-ray powder diffraction pattern having two or more diffraction peaks at 2[theta] values selected from 3.82±0.2 claim 2 , 7.57±0.2 claim 2 , 8.12±0.2 claim 2 , 10.53±0.2 claim 2 , 11.39±0.2 claim 2 , 12.00±0.2 ...

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Номер записи: 4

28-03-2013 дата публикации

PROCESS FOR THE PREPARATION OF PLEUROMUTILINS

Номер: US20130079400A1

Автор: Heilmayer Werner, Riedl Rosemarie, Spence Lee

Принадлежит: NABRIVA THERAPEUTICS AG

Process for the preparation of a compound of formula I 2. A compound of formula I as defined in in the form of a single stereoisomer in crystalline form.3. A compound according to claim 2 , which is 14-O-{[(1R claim 2 ,2R claim 2 ,4R)-4-amino-2-hydroxy-cyclohexylsulfanyl]-acetyl}-mutilin in crystalline Form 1.4. A compound according to claim 2 , which is 14-O-{[(1R claim 2 ,2R claim 2 ,4R)-4-amino-2-hydroxy-cyclohexylsulfanyl]-acetyl}-mutilin in crystalline Form 2 in the form of a n-butanol solvate.5. A compound of formula I as defined in in the form of a single stereoisomer in the form of a crystalline salt.6. A crystalline salt according to claim 5 , which is an acetate claim 5 , lactate or hydrogenmaleate.7. A compound according to claim 5 , which is selected from the group consisting of14-O-{[(1R,2R,4R)-4-amino-2-hydroxy-cyclohexylsulfanyl]-acetyl}-mutilin acetate in crystalline Form A;14-O-{[(1R,2R,4R)-4-amino-2-hydroxy-cyclohexylsulfanyl]-acetyl}-mutilin acetate in crystalline Form B14-O-{[(1R,2R,4R)-4-amino-2-hydroxy-cyclohexylsulfanyl]-acetyl}-mutilin L-lactate in crystalline Form 1, and14-O-{[(1R,2R,4R)-4-amino-2-hydroxy-cyclohexylsulfanyl]-acetyl}-mutilin hydrogenmaleate in crystalline Form 1.11. A compound of formula IIa as defined in claim 5 , for use as an intermediate in a process for the production of a compound of formula I as defined in claim 5 , in the form of a single stereoisomer.12. Pharmaceutical composition comprising crystalline 14-O-{[((1R claim 5 ,2R claim 5 ,4R)-4-amino-2-hydroxy-cyclohexyl) sulfanyl]acetyl}mutilin claim 5 , or comprising an claim 5 , optionally crystalline claim 5 , acetate claim 5 , lactate claim 5 , or hydrogenmaleate of 14-O-{[((1R claim 5 ,2R claim 5 ,4R)-4-amino-2-hydroxy-cyclohexyl)sulfanyl]acetyl}mutilin as an active ingredient in combination with pharmaceutically acceptable carrier or diluent.13. A compound of formula IIIa as defined in claim 5 , for use as an intermediate in a process for the production of a ...

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Номер записи: 5

11-04-2013 дата публикации

SOLID STATE FORMS OF TAPENTADOL SALTS

Номер: US20130090314A1

Автор: Ahirao Vikas Daulatrao, BONDGE Sandipan Prabhurao, Khunt Mayur Devjibhai, Pradhan Nitin Sharadchandra

Принадлежит: ACTAVIS GROUP PTC EHF

Provided herein are novel solid state forms of tapentadol salts, process for their preparation, pharmaceutical compositions, and method of treating thereof. The tapentadol salts include an L-(−)-camphorsulfonate salt, a dibenzoyl-(L)-tartrate salt, a dibenzoyl-(D)-tartrate salt, a malate salt, a maleate salt, or a salicylate salt. 1. Solid state form of a salt of 3-[(1R ,2R)-3-(dimethylamino)-1-ethyl-2-methylpropyl]phenol (tapentadol salt) , wherein the salt of tapentadol is an L-(−)-camphorsulfonate salt , a dibenzoyl-(D)-tartrate salt , a malate salt , a maleate salt , or a salicylate salt.2. The solid state form of tapentadol salt of claim 1 , which is in a crystalline form or in an amorphous form claim 1 , and wherein the solid state form is anhydrous and/or solvent-free form claim 1 , or a hydrate and/or a solvate form.3. The solid state form of tapentadol salt of claim 1 , having the following characteristics claim 1 , wherein: [{'figref': {'@idref': 'DRAWINGS', 'FIG. 1'}, 'i) a powder X-ray diffraction pattern substantially in accordance with ;'}, 'ii) a powder X-ray diffraction pattern having peaks at about 3.93, 5.66, 14.94, 16.16 and 21.52±0.2 degrees 2-theta;', 'iii) a powder X-ray diffraction pattern having additional peaks at about 8.01, 11.36, 14.10, 15.27, 15.91, 16.72, 19.06, 19.88, 21.85, 22.56, 23.92 and 27.12±0.2 degrees 2-theta; and', {'figref': {'@idref': 'DRAWINGS', 'FIG. 2'}, 'iv) a differential scanning calorimetric (DSC) thermogram substantially in accordance with ;'}], 'a) the solid state form of tapentadol L-(−)-camphorsulfonate salt is characterized by one or more of the following properties [{'figref': {'@idref': 'DRAWINGS', 'FIG. 5'}, 'i) a powder X-ray diffraction pattern substantially in accordance with ;'}, 'ii) a powder X-ray diffraction pattern having peaks at about 8.52, 9.39, 11.81, 12.28, 13.46, 14.06, 17.77, 17.97, 18.33, 18.79, 19.58 and 20.05±0.2 degrees 2-theta;', 'iii) a powder X-ray diffraction pattern having additional ...

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Номер записи: 6

18-04-2013 дата публикации

Process for removing, isolating and purifying dicarboxylic acids

Номер: US20130096343A1

Автор: Joachim Schulze, Wolfgang Tietz

Принадлежит: THYSSENKRUPP UHDE GMBH

A process for removing, isolating and purifying dicarboxylic acid from fermentation broths, which includes the following steps: 1) removal of the biomass and any solids present from the fermentation broth in two successive stages, 2) removal of the dicarboxylic acid solution from the biomass-free fermentation broth by simulated moving bed (SMB) chromatography, 3) fine purification of the dicarboxylic acid solution, 4) multistage evaporative concentration and crystallization, and 5) separation and drying of the crystals.

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Номер записи: 7

02-05-2013 дата публикации

OIL COMPOSITION AND METHOD OF PRODUCING THE SAME

Номер: US20130109873A1

Автор: BOOTSMA Jason

Принадлежит:

This invention relates to a corn oil composition comprising unrefined corn oil having a free fatty acid content of less than about 5 weight percent, and methods for producing the same. 1. A corn oil composition comprising unrefined corn oil having a free fatty acid content of less than about 5 weight percent; a moisture content of from about 0.2 to about 1 weight percent; and an alkali metal ion and/or alkaline metal ion content of greater than 10 ppm.2. The corn oil composition of claim 1 , wherein the unrefined corn oil has an insoluble content of less than about 1 weight percent.3. The corn oil composition of claim 1 , wherein the free fatty acid content is less than about 3 weight percent.4. The corn oil composition of claim 1 , wherein the free fatty acid content is less than about 2 weight percent.5. The corn oil composition of claim 1 , wherein the free fatty acid content comprises at least one fatty acid selected from the group consisting of C16 palmitic claim 1 , C18 stearic claim 1 , C18-1 oleic claim 1 , C18-2 linoleic claim 1 , and C18-3 linolenic.6. The corn oil composition of claim 1 , wherein the unrefined corn oil composition has an unsaponifiables content less than about 3 weight percent.7. The corn oil composition of claim 1 , wherein the unrefined corn oil composition further comprises one or more components selected from the group consisting of lutein claim 1 , cis-lutein claim 1 , zeaxanthin claim 1 , alpha-cryptoxanthin claim 1 , beta-cryptoxanthin claim 1 , alpha-carotene claim 1 , beta-carotene claim 1 , cis-beta-carotene claim 1 , alpha-tocopherol claim 1 , beta-tocopherol claim 1 , delta-tocopherol claim 1 , or gamma-tocopherol claim 1 , alpha-tocotrienol claim 1 , beta-tocotrienol claim 1 , gamma-tocotrienol claim 1 , and delta-tocotrienol.8. The corn oil composition of claim 1 , wherein the unrefined corn oil composition has a tocopherol content less than about 1 mg/g.9. The corn oil composition of claim 1 , wherein the unrefined corn oil ...

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Номер записи: 8

23-05-2013 дата публикации

Aminopyrazine Derivative and Medicine

Номер: US20130131082A1

Автор: ASAKI Tetsuo, FUJIHARA Hidetaka, HORI Katsutoshi, NAITO Haruna

Принадлежит: Nippon Shinyaku Co., Ltd

The present invention relates to a compound represented by general formula [1] satisfying the following (I) or (II), or a pharmaceutically acceptable salt of the compound. 1. A compound (S)-N-[1-(4-fluorophenyl)ethyl]-4-(1-methyl-1H-pyrazol-4-yl)-N-(pyrazin-2-yl)pyridine-2 ,6-diamine or a pharmaceutically acceptable salt thereof.2. The pharmaceutically acceptable salt according to claim 1 , which is (S)-N-[1-(4-fluorophenyl)ethyl]-4-(1-methyl-1H-pyrazol-4-yl)-N-(pyrazin-2-yl)pyridine-2 claim 1 ,6-diamine maleate.3. A pharmaceutical composition claim 1 , comprising the compound or pharmaceutically acceptable salt thereof according to as an active ingredient.4. A pharmaceutical composition claim 2 , comprising the pharmaceutically acceptable salt according to as an active ingredient.5. A method of treating polycythemia vera claim 1 , essential thrombocythemia claim 1 , or idiopathic myelofibrosis claim 1 , comprising the step of administering the compound or pharmaceutically acceptable salt thereof according to to a human subject.6. The method of treating polycythemia vera claim 5 , essential thrombocythemia claim 5 , or idiopathic myelofibrosis according to claim 5 , wherein what is administered is (S)-N-[1-(4-fluorophenyl)ethyl]-4-(1-methyl-1H-pyrazol-4-yl)-N-(pyrazin-2-yl)pyridine-2 claim 5 ,6-diamine maleate.7. The method of treating polycythemia vera claim 5 , essential thrombocythemia claim 5 , or idiopathic myelofibrosis according to claim 5 , wherein what is treated is polycythemia vera.8. The method of treating polycythemia vera according to claim 7 , wherein what is administered is (S)-N-[1-(4-fluorophenyl)ethyl]-4-(1-methyl-1H-pyrazol-4-yl)-N-(pyrazin-2-yl)pyridine-2 claim 7 ,6-diamine maleate.9. The method of treating polycythemia vera claim 5 , essential thrombocythemia claim 5 , or idiopathic myelofibrosis according to claim 5 , wherein what is treated is essential thrombocythemia.10. The method of treating essential thrombocythemia according to claim 9 ...

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Номер записи: 9

30-05-2013 дата публикации

ETHANAMINE COMPOUNDS AND METHODS OF USING THE SAME

Номер: US20130137731A1

Автор: Balestra Michael, Bernstein Peter, Ernst Glen E., Frietze William, McCauley John, Nugiel David, Shen Lihong

Принадлежит: AstraZeneca AB

The present invention is directed to ethanamine compounds, pharmaceutical compositions comprising the same, and methods of treatingh depression by administering the ethanamine compound. 148-. (canceled)49. 2-Methyl-1-phenyl-2-(pyridin-2-yl)propan-1-amine or a pharmaceutically acceptable salt thereof.50. A compound as claimed in which is 2-methyl-1-phenyl-2-(pyridin-2-yl)propan-1-amine or a hydrochloric claim 49 , hydrobromic claim 49 , sulfuric claim 49 , phosphoric claim 49 , citric claim 49 , tartaric claim 49 , lactic claim 49 , pyruvic claim 49 , acetic claim 49 , succinic claim 49 , fumaric claim 49 , maleic claim 49 , methanesulphonic or benzenesulphonic acid salt thereof.51. A compound as claimed in which is 2-methyl-1-phenyl-2-(pyridin-2-yl)propan-1-amine fumarate.52. A compound as claimed in which is 2-methyl-1-phenyl-2-(pyridin-2-yl)propan-1-amine.53. A compound as claimed in which is (S)-2-methyl-1-phenyl-2-(pyridin-2-yl)propan-1-amine or a pharmaceutically acceptable salt thereof.54. A compound as claimed in which is (S)-2-methyl-1-phenyl-2-(pyridin-2-yl)propan-1-amine or a hydrochloric claim 49 , hydrobromic claim 49 , sulfuric claim 49 , phosphoric claim 49 , citric claim 49 , tartaric claim 49 , lactic claim 49 , pyruvic claim 49 , acetic claim 49 , succinic claim 49 , fumaric claim 49 , maleic claim 49 , methanesulphonic or benzenesulphonic acid salt thereof.55. A compound as claimed in which is (S)-2-methyl-1-phenyl-2-(pyridin-2-yl)propan-1-amine fumarate.56. A compound as claimed in which is (S)-2-methyl-1-phenyl-2-(pyridin-2-yl)propan-1-amine.57. A method of treating depression in a human which comprises administering to a person in need thereof a therapeutic effective amount of a compound or a pharmaceutically acceptable salt thereof claim 49 , where the compound is 2-methyl-1-phenyl-2-(pyridin-2-yl)propan-1-amine.58. A method of treating depression in a human as claimed in which comprises administering to a person in need thereof a therapeutic ...

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Номер записи: 10

20-06-2013 дата публикации

METAXALONE COCRYSTALS

Номер: US20130158083A1

Автор: Chorlton Alan, Frampton Christopher, Gooding Daniel, Holland Joanne

Принадлежит:

The invention relates to improvements of the physiochemical and/or the pharmaceutical properties of metaxalone. Disclosed herein are several new cocrystals of metaxalone, including: a 1:1 metaxalone adipic acid cocrystal, a 1:0.5 metaxalone fumaric acid cocrystal, a 1:1 metaxalone salicyclic acid cocrystal, a 1:0.5 metaxalone succinic acid cocrystal, and a 1:0.5 metaxalone maleic acid cocrystal. The therapeutic uses of these metaxalone cocrystals are described as well as therapeutic compositions containing them. 1. A metaxalone cocrystal selected from a 1:1 metaxalone adipic acid cocrystal , a 1:0.5 metaxalone fumaric acid cocrystal , a 1:1 metaxalone salicyclic acid cocrystal , a 1:0.5 metaxalone succinic acid cocrystal , and a 1:0.5 metaxalone maleic acid cocrystal.2. A metaxalone cocrystal of claim 1 , wherein the cocrystal is a 1:1 metaxalone adipic acid cocrystal characterized by a powder X-ray diffraction pattern having at least three peaks selected from 8.5 claim 1 , 15.8 claim 1 , 18.9 claim 1 , 20.2 claim 1 , and 23.6 °2θ±0.2°2θ.3. A metaxalone cocrystal of claim 1 , wherein the cocrystal is a 1:1 metaxalone adipic acid cocrystal characterized by a powder X-ray diffraction pattern having peaks selected from 8.5 claim 1 , 15.8 claim 1 , 18.9 claim 1 , 20.2 claim 1 , and 23.6 °2θ±0.2°2θ claim 1 , or by a powder X-ray diffraction pattern substantially similar to .4. A metaxalone cocrystal of claim 1 , wherein the cocrystal is a 1:0.5 metaxalone fumaric acid cocrystal characterized by a powder X-ray diffraction pattern having at least three peaks selected from 5.6 claim 1 , 11.0 claim 1 , 13.1 claim 1 , 18.3 claim 1 , 21.6 claim 1 , and 22.7 °2θ±0.2°2θ.5. A metaxalone cocrystal of claim 1 , wherein the cocrystal is a 1:0.5 metaxalone fumaric acid cocrystal characterized by a powder X-ray diffraction pattern having peaks selected from 5.6 claim 1 , 11.0 claim 1 , 13.1 claim 1 , 18.3 claim 1 , 21.6 claim 1 , and 22.7 °2θ±0.2°2θ claim 1 , or by a powder X-ray ...

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Номер записи: 11

27-06-2013 дата публикации

PROCESS FOR THE PREPARATION OF TENOFOVIR

Номер: US20130165413A1

Автор: CHAVA Satyanarayana, GORANTLA Seeta Ramanjaneyulu, INDUKURI Venkata Sunil Kumar, JOGA Sree Rambabu

Принадлежит: Aptuit Laurus Private Limited

The present invention provides a process for the preparation of tenofovir. The present invention also provides a process for the preparation of tenofovir disoproxil or a salt thereof and its pharmaceutical composition using the tenofovir of the present invention. 2. The process of claim 1 , further comprising the step of converting the tenofovir into a tenofovir disoproxil or a pharmaceutically acceptable salt thereof.3. The process of claim 1 , wherein the Calkyl is selected from the group consisting of methyl claim 1 , ethyl claim 1 , propyl claim 1 , butyl claim 1 , isopropyl claim 1 , and isobutyl.4. The process of claim 1 , wherein the base is selected from the group consisting of alkali metal hydroxides claim 1 , alkali metal hydrides claim 1 , amide bases claim 1 , alkali metal alkoxides claim 1 , and alkyl lithium compounds.5. The process of claim 1 , wherein the base is selected from the group consisting of sodium hydride claim 1 , lithium hydride claim 1 , sodium amide claim 1 , potassium amide claim 1 , sodium dimethyl amide claim 1 , sodium methoxide claim 1 , and butyl lithium.6. The process of claim 1 , wherein the metal salt is represented by the formula MX claim 1 , wherein M represents a divalent metal cation claim 1 , and X represents halide claim 1 , acetate claim 1 , or trifluoromethane sulfonate.7. The process of claim 6 , wherein the divalent metal cation selected from the group consisting of zinc claim 6 , beryllium claim 6 , magnesium claim 6 , calcium claim 6 , strontium claim 6 , and barium.8. The process of claim 6 , wherein the halide is selected from the group consisting of fluoro claim 6 , bromo claim 6 , chloro claim 6 , and iodo.9. The process of claim 1 , wherein the organic solvent is selected from the group consisting of amides claim 1 , ethers claim 1 , aromatic hydrocarbons claim 1 , and nitriles.10. The process of claim 1 , wherein the organic solvent is selected from dimethyl formamide claim 1 , dimethyl acetamide claim 1 , ...

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Номер записи: 12

18-07-2013 дата публикации

ACID ADDITION SALT OF A NORTRIPTYLINE-GABA CONJUGATE AND A PROCESS OF PREPARING SAME

Номер: US20130184347A1

Автор: Gil-ad Irit, Nudelman Abraham, Rephaeli Ada, Shaul Mazal, Weizman Abraham

Принадлежит:

An acid addition salt of a nortriptyline-GABA conjugate, a novel crystalline form of a fumaric acid addition salt of a nortriptyline-GABA conjugate, and processes of preparing the forgoing are disclosed. Uses of the above-indicated forms of a nortriptyline-GABA conjugate in the treatment of CNS disorders, and in the treatment of pain in particular, are also disclosed. Further disclosed in a large-scale process of preparing a nortriptyline-GABA conjugate. 149-. (canceled)50. A fumaric acid addition salt of nortriptyline-4-aminobutyrate.51. A crystalline form of a fumaric acid addition salt of nortriptyline-4-aminobutyrate , characterized by at least one of:{'figref': {'@idref': 'DRAWINGS', 'FIG. 3'}, '(a) an X-Ray Powder Diffraction (XRPD) pattern exhibiting at least four of the peaks shown in ;'}{'figref': {'@idref': 'DRAWINGS', 'FIG. 1'}, '(b) an infrared spectrum exhibiting at least three of the absorption peaks shown in ; and'}(c) a Differential Scanning calorimetry (DSC) exhibiting an endothermic peak maximum that ranges from 155° C. to 160° C.52. The crystalline form of nortriptyline-4-aminobutyrate fumarate of claim 51 , characterized by an X-Ray Powder Diffraction (XRPD) pattern exhibiting at least six of the peaks shown in .53. The crystalline form of nortriptyline-4-aminobutyrate fumarate of claim 51 , characterized by an X-Ray Powder Diffraction (XRPD) pattern exhibiting at least seven of the peaks shown in .54. The crystalline form of nortriptyline-4-aminobutyrate fumarate of claim 51 , characterized by an X-Ray Powder Diffraction (XRPD) pattern substantially identical to the XRPD pattern shown in .55. The crystalline form of nortriptyline-4-aminobutyrate fumarate of claim 51 , characterized by an infrared spectrum exhibiting at least five of the absorption peaks shown in .56. The crystalline form of a fumaric acid addition salt of nortriptyline-4-aminobutyrate of claim 51 , characterized by an infrared spectrum exhibiting absorption peaks substantially ...

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Номер записи: 13

25-07-2013 дата публикации

POLYMERIZABLE GEMINI DICARBOXLATE SURFACTANTS AND LYOTROPIC LIQUID CRYSTALS AND MEMBRANES MADE THEREFROM

Номер: US20130190417A1

Автор: Mahanthappa Mahesh Kalyana, Sorenson Gregory Paul

Принадлежит: WISCONSIN ALUMNI RESEARCH FOUNDATION

The disclosure provides anionic Gemini surfactants comprising at least two carbonyl moieties and at least two aliphatic moieties. In some aspects, at least two of the aliphatic moieties comprise at least seven carbon atoms and at least one pair of conjugated carbon-to-carbon double bonds. The anionic Gemini surfactants are polymerizable and may be used to prepare triply periodic multiply continuous lyotropic phase and polymers thereof that substantially retain triply periodic multiply continuous lyotropic phase structure. 2. The surfactant of claim 1 , wherein{'sub': 1', '2', '1', '2', '2', '2', '1', '8', '3', '3', '1', '8', '3', '1', '8', '3', '1', '8', '3', '3', '1', '8', '3', '1', '8', '3', '1', '8', '3', '2', '3', '1', '8', '3', '2', '1', '8', '3', '2, 'Mand Mare the same or different and at least one Mor Mis a covalently bonded group selected from —OCHCH(OH)CHOH, —NH(C-Calkyl)SOH, —N(CH)(C-Calkyl)SOH, —O(C-Calkyl)SOH, —NH(C-Calkyl)OSOH, —N(CH)(C-Calkyl)OSOH, —O(C-Calkyl)OSOH, —NH(C-Calkyl)POH, —N(CH)(C-Calkyl)POH, and —O(C-Calkyl)POH.'}3. The surfactant of claim 1 , wherein Zand Zeach independently have a value of zero or one.4. The surfactant of claim 1 , wherein each of M is independently selected at each occurrence from the group consisting of lithium ion; sodium ion; potassium ion; cesium ion; zinc ion; magnesium ion; calcium ion; ammonium ion; alkylammonium ion having the structure HRN wherein x is an integer having a value of 0 through 4 and R is selected from the group consisting of methyl claim 1 , ethyl claim 1 , propyl claim 1 , butyl claim 1 , and combinations thereof; tetrakis(hydroxymethyl)phosphonium ion; tetramethylphosphonium ion; choline; imidazolium; bis(quaternary ammonium) ion; and combinations thereof.5. The surfactant of claim 1 , whereinY is a covalently bound, divalent linker chosen from:{'sub': 1', '20', '1', '20, 'an optionally substituted C-Caliphatic group, an optionally substituted C-Cheteroaliphatic group, which aliphatic and ...

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Номер записи: 14

01-08-2013 дата публикации

DIENE-BASED CARBOXYLATE ANION AND SALT THEREOF, AND POLYMERIZABLE OR CURABLE COMPOSITION THEREOF

Номер: US20130197123A1

Автор: Kaneko Tomomasa

Принадлежит: NIPPON SHOKUBAI CO., LTD.

The claimed invention provides a novel compound not having been studied before, that is, a diene carboxylate anion that contains a specific structure, and a salt thereof. The claimed invention further provides a diene carboxylate anion and a salt thereof, especially a metal salt thereof, which are easily soluble in general organic solvents, reactive diluents, and resins, may be in a liquid state at normal temperature depending on the structure, and have high polymerizability. Polymerization/curing of these produces a resin to which many ionic bonds and a metal are introduced, providing various properties such as hardness, scratch resistance, anti-fingerprint property, gas-barrier property, water vapor barrier property, oxygen absorption property, ultraviolet protection, infrared protection, color development and coloring, high refractive index, adhesion, various catalytic abilities, fluorescence ability and light-emitting ability, optical amplification, dispersibility, and antistatic properties. In addition, the anion and the salt can be used for raw materials for functional fine particles and for metal nanoparticle composites, and also for MOD materials. The claimed invention also provides an advantageous method for producing the diene carboxylate anion and the salt thereof. 2. An ionic composition comprising the diene carboxylate anion according to .3. A polymerizable or curable composition comprising the diene carboxylate anion according to .4. The polymerizable or curable composition according to claim 3 , further comprising a radical initiator and/or a dryer.5. A method for polymerizing or curing the diene carboxylate anion according to claim 1 ,comprising a step including at least one method selected from the group consisting of heating, irradiating with active energy beams, and exposing to an atmosphere including oxygen.6. A polymerized or cured product produced by the polymerization or curing method according to .7. A polymerizable or curable composition ...

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Номер записи: 15

08-08-2013 дата публикации

SOLIFENACIN SALTS

Номер: US20130203804A1

Автор: Bonde-Larsen Antonio Lorente, Fuentes Gerardo Gutiérrez, López-Bachiller Jaime del Campo, Rodríguez Celso Sandoval, Sainz Yolanda Fernández

Принадлежит: CRYSTAL PHARMA, S.A.U.

The invention concerns fumarate salts of solifenacin, as well as pharmaceutical compositions comprising fumarate salts of solifenacin. The invention furthermore concerns a process for preparing solifenacin and salts thereof. The fumarate salt provides improved properties over the known solifenacin salts, especially in terms of its stability. The novel process for its preparation is furthermore improved over known processes for preparing solifenacin in that it provides a higher yield and recovers a greater amount of starting material. 1. A fumarate salt of solifenacin.216-. (canceled)17. The fumarate salt according to claim 1 , wherein said fumarate salt is a hydrogenfumarate (1:1) salt.18. The fumarate salt according to claim 1 , wherein said fumarate salt is substantially crystalline.19. A pharmaceutical composition comprising the fumarate salt according to and one or more pharmaceutically acceptable carriers claim 1 , wherein said pharmaceutical composition is a solid formulation.20. The pharmaceutical composition according to claim 19 , wherein said pharmaceutical composition is formulated for oral administration.21. The pharmaceutical composition according to claim 19 , wherein said pharmaceutical composition is in the form of a tablet claim 19 , a capsule claim 19 , a gelcap claim 19 , a granule claim 19 , a sachet or a pill.22. The pharmaceutical composition according to claim 21 , wherein said pharmaceutical composition is in the form of a tablet.23. A process for preparing solifenacin or a pharmaceutically acceptable salt thereof comprising:a) reacting a solifenacin base with a fumaric acid to form a fumarate salt thereof; andb) optionally transforming the fumarate salt obtained in step a) to solifenacin base and/or a different pharmaceutically acceptable salt of solifenacin.24. The process according to claim 23 , wherein step a) is preceded by the steps:a′) reacting 1(S)-1-phenyl-1,2,3,4-tetrahydroisoquinoline with a C1-6 alkyl chloroformate to form a ...

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Номер записи: 16

05-09-2013 дата публикации

Purified Crocetin Compound And Method For Treating, Inhibiting, And/Or Prophylaxis of Cancer, Such As Pancreatic Cancer

Номер: US20130231300A1

Автор: Dhar Animesh, Gutheil William G.

Принадлежит: U.S. Department of Veterans Affairs

A fraction separated from crude crocetin by preparative HPLC, and identified using LC/MS and NMR as crocetinic acid, markedly regressed the proliferation and increased apoptosis in pancreatic cancer cells. Purified crocetinic acid showed more potency than 15 commercial or crude crocetin using proliferation and apoptosis as markers. Purified crocetinic acid also showed significant anti-tumorigenic activity against pancreatic cancer cells in a mouse model of pancreatic cancer. Given crocetinic acid's low toxicity, crocetinic acid could be used as a chemotherapeutic or chemopreventative agent for pancreatic cancer. 16-. (canceled)7. A purified crocetin compound obtained by fractionating crude crocetin.8. The compound of claim 7 , which is 50-times more effective than crude crocetin.9. A composition or formulation comprising the compound of .10. A composition comprising a therapeutically effective amount of the compound of .11. A composition comprising a therapeutically effective amount of crocetinic acid.1215-. (canceled)16. A method of treating claim 7 , inhibiting claim 7 , and/or prophylaxis of cancer claim 7 , comprising:a) administering an effective amount of a purified crocetin compound to a subject in need thereof.17. The method of claim 16 , wherein:a) the crocetin compound comprises crocetinic acid.18. The method of claim 17 , wherein:a) the cancer comprises pancreatic cancer.19. The method of claim 16 , wherein:a) the compound is administered orally or intravenously.20. The method of claim 16 , wherein:a) the compound is administered in conjunction with another anticancer agent.21. The method of claim 20 , wherein:a) the other anticancer agent comprises gemcitabine, 5-FU, or a combination thereof.22. A method of treating claim 20 , inhibiting claim 20 , and/or prophylaxis of pancreatic cancer claim 20 , comprising:a) administering an effective amount of a compound, composition, and/or a pharmaceutical formulation comprising crocetinic acid to a subject in ...

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Номер записи: 17

24-10-2013 дата публикации

MALEATE SALTS OF (E)-N--4-(DIMETHYLAMINO)-2-BUTENAMIDE AND CRYSTALLINE FORMS THEREOF

Номер: US20130281488A1

Автор: Cheal Gloria, Chew Warren, Hadfield Anthony F., Ku Mannching Sherry, Lu Quinhong, MIRMEHRABI Mahmoud

Принадлежит:

The present invention relates to maleate salt forms of (E)-N-{4-[3-chloro-4-(2-pyridinylmethoxy)anilino]-3-cyano-7-ethoxy-6-quinolinyl}-4-(dimethylamino)-2-butenamide, methods of preparing crystalline maleate salt forms, the associated compounds, and pharmaceutical compositions containing the same. The maleate salts are useful in treating cancers, particularly those affected by kinases of the epidermal growth factor receptor family. 135-. (canceled)36. A method of increasing oral absorption of neratinib , comprising:formulating neratinib as a maleate salt, wherein the neratinib maleate salt is prepared according to a method comprising:i) mixing (E)-N-{4-[3-chloro-4-(2-pyridinylmethoxy)anilino]-3-cyano-7-ethoxy-6-quinolinyl}-4-(dimethylamino)-2-butenamide and maleic acid in a water-alcohol solution at a temperature in the range of between about 50° C. to about 60° C.;ii) cooling said solution to a temperature of about 40° C. and maintaining the cooled solution at about 40° C. for about 12 hours to precipitate the maleate salt;iii) further cooling the cooled solution to room temperature (about 25° C.) over a minimum of 4 hours and maintaining the further cooled solution at room temperature (about 25° C.) for at least 2 hours; andiv) filtering the maintained, further cooled solution to obtain crystalline (E)-N-{4-[3-chloro-4-(2-pyridinylmethoxy)anilino]-3-cyano-7-ethoxy-6-quinolinyl}-4-(dimethylamino)-2-butenamide maleate.37. The method of claim 36 , wherein the prepared neratinib maleate salt comprises crystalline (E)-N-{4-[3-chloro-4-(2-pyridinylmethoxy)anilino]-3-cyano-7-ethoxy-6-quinolinyl}-4-(dimethylamino)-2-butenamide maleate claim 36 , monohydrate claim 36 , Form II.38. The method of claim 37 , wherein the crystalline (E)-N-{4-[3-chloro-4-(2-pyridinylmethoxy)anilino]-3-cyano-7-ethoxy-6-quinolinyl}-4-(dimethylamino)-2-butenamide maleate claim 37 , monohydrate claim 37 , Form II is characterized by X-ray diffraction peaks at the following angles (±0.20°) of ...

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Номер записи: 18

24-10-2013 дата публикации

Agents for treating disorders involving modulation of ryanodine receptors

Номер: US20130281512A1

Автор: Jiaming Yan, Mark BERTRAND, Nicole Villeneuve, Sandro Belvedere, Yael Webb

Принадлежит: Armgo Pharma Inc, Laboratoires Servier SAS

The present invention relates to 1,4-benzothiazepine derivatives and their use to treat conditions, disorders and diseases associated with ryanodine receptors (RyRs) that regulate calcium channel functioning in cells. The invention also discloses pharmaceutical compositions comprising the compounds and uses thereof to treat diseases and conditions associated with RyRs, in particular cardiac, musculoskeletal and central nervous system (CNS) disorders.

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Номер записи: 19

31-10-2013 дата публикации

MALEATE SALTS OF 6-(5-CHLORO-2-PYRIDYL)-5-[(4-METHYL-1-PIPERAZINYL)CARBONYLOXY]-7-OXO-6,7-DIHYDRO-5H-PYRROLO[3,4-b]PYRAZINE

Номер: US20130289040A1

Автор: H. Scott Wilkinson, Kostas Saranteas, Patrick Mousaw, Richard Hsia, Tushar Misra

Принадлежит: SUNOVION PHARMACEUTICALS INC

A novel maleate salt of (6-(5-chloro-2-pyridyl)-5-[(4-methyl-1-piperazinyl)carbonyloxy]-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyrazine) is provided.

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Номер записи: 20

31-10-2013 дата публикации

SALTS OF KUKOAMINE B, PREPARATION METHOD AND USE THEREOF

Номер: US20130289112A1

Автор: Cao Hongwei, Huang Min, Li Yan, Liu Xin, Lu Yongling, Wang Ning, Wei Guo, Yang Jingcheng, Yang Yang, Zhao Kecen, Zheng Jiang, Zheng Xinchuan, Zhou Hong, Zhu Yuanfeng

Принадлежит: TIANJIN CHASESUN PHARMACEUTICAL CO., LTD

Salts of kukoamine B, their preparation method and their pharmaceutical use in preparation of drugs for preventing and treating sepsis. Experiments indicate that salts of kukoamine B have a good effect on antagonizing the key factors inducing sepsis, and can be used in the preparation of drugs for preventing and treating sepsis. Under the current circumstances of the lack of effective measures for the treatment of sepsis in clinical practice, the medicinal formulations, which comprise the salts of kukoamine B, pharmaceutically acceptable carrier and/or diluent, provide a new approach for the prevention and treatment of sepsis. 2. The salts of kukoamine B as claimed in claim 1 , wherein A comprises a hydrogenacid claim 1 , and wherein the hydrogenacid is any one of hydrochloric acid and hydrobromic acid.3. The salts of kukoamine B as claimed in claim 1 , wherein A comprises an oxacid claim 1 , and wherein the oxacid is any one of sulfuric acid claim 1 , phosphoric acid claim 1 , and nitric acid.4. The salts of kukoamine B as claimed in claim 1 , wherein A comprises an inorganic acid claim 1 , and wherein the inorganic acid is any one of hydrochloric acid claim 1 , hydrobromic acid claim 1 , sulfuric acid claim 1 , and phosphoric acid.5. The salts of kukoamine B as claimed in claim 1 , wherein A comprises a carboxylic acid claim 1 , and wherein the carboxylic acid is any one of acetic acid claim 1 , propionic acid claim 1 , butyric acid claim 1 , oxalic acid claim 1 , malonic acid claim 1 , succinic acid claim 1 , adipic acid claim 1 , benzoic acid claim 1 , phenylpropionic acid claim 1 , cinnamic acid claim 1 , stearic acid claim 1 , trifluoroacetic acid claim 1 , maleic acid claim 1 , fumaric acid claim 1 , nicotinic acid claim 1 , and palmitic acid.6. The salts of kukoamine B as claimed in claim 1 , wherein A comprises a hydroxy acid claim 1 , and wherein the hydroxy acid is any one of malic acid claim 1 , citric acid claim 1 , lactic acid claim 1 , hydroxybutyric ...

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Номер записи: 21

07-11-2013 дата публикации

POLYMORPHS OF DONEPEZIL SALTS, PREPARATION METHODS AND USES THEREOF

Номер: US20130296283A1

Автор: ZHANG Hesheng

Принадлежит:

Preparation methods of mesylate, para-toluenesulfonate, succinate, tartrate, sulphate, nitrate, phosphate, salicylate, fumarate, maleate, gallate, acetylsalicylate, benzenesulphonate, citrate, aspartate, glutaminate, lactate, gluconate, ascorbate, malonate, malate, sorbate, acetate or formate of 1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine (i.e., Donepezil). Novel polymorphs formed from these salts and their preparation methods. Co-crystals formed from Donepezil hydrochloride and maleic acid, fumaric acid, citric acid, salicylic acid, tartaric acid or succinic acid. 2. The polymorph of claim 1 , wherein the polymorph is selected from the group consisting of:{'b': 8', '1', '8', '2', '8', '3', '8', '4, 'the polymorph of the compound of formula (I), wherein XH represents salicylic acid, having the following physical characteristics: X-ray powder diffraction pattern as shown in FIG. -A-, infrared absorption spectrum as shown in FIG. -A-, thermogravimetric and differential thermal analysis spectrum as shown in -A-, and nuclear magnetic resonance spectrum as shown in FIG. -A-; and'}{'b': 10', '1', '10', '2', '10', '3', '10', '4, 'the polymorph of the compound of formula (I), wherein XH represents maleic acid, having the following physical characteristics: X-ray powder diffraction pattern as shown in FIG. -B-, infrared absorption spectrum as shown in FIG. -B-, thermogravimetric and differential thermal analysis spectrum as shown in -B-, and nuclear magnetic resonance spectrum as shown in FIG. -B-.'}6. The method of claim 5 , wherein the diseases or physiological dysfunctions caused by the low level of acetylcholine include senile dementia (AD) claim 5 , attention deficient disorder of childhood claim 5 , memory deterioration claim 5 , paralysis agitans (demeritia) claim 5 , brain injury claim 5 , multiple sclerosis claim 5 , Down's Syndrome claim 5 , delirium claim 5 , mood disorder claim 5 , Huntington's disease claim 5 , and sleep disorder.7. The method of ...

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Номер записи: 22

28-11-2013 дата публикации

Use of Artemisine Derivatives and Pharmaceutical Salts Thereof

Номер: US20130317095A1

Автор: Cai Xun, Chen Saijuan, LI YANG, LI Ying, LIU Jingjing, Mi Jianqing, Nie Ruimin, Peng Yu, Wang Jin, WANG Yueying, Wang Zhenyi, Zhang Yu

Принадлежит: Shanghai Institute of Materia Medica, Chinese Academy of Sciences

The invention demonstrates the application of an artemisinin derivative and its pharmaceutical salt. The artemisinin derivatives diarteether amine and its pharmaceutical salt inhibit the proliferation of leukemic cells, block the cell cycle of leukemic cells and induce the apoptosis of leukemic cells. Artemisinin derivatives of the present invention and its pharmaceutical salt can be used for the preparation of anti-leukemia medicines, especially for treatment of acute leukemia and, what's more, for the treatment of acute myeloid leukemia. 14-. (canceled)6. The method of claim 5 , wherein said leukemia is an acute leukemia.7. The method of claim 6 , wherein said acute leukemia is an acute myeloid leukemia (ALM).8. The method of claim 7 , wherein said acute myelocytic leukemia is selected from the group consisting of AML with t(8;22)(q22;q22)(AML/ETO) claim 7 , AML with t(15;17)(q22;q21) claim 7 , (PML-RARα) in AML with recurrent genetic abnormalities claim 7 , AML-M2 claim 7 , and AML-M5.10. The method of claim 9 , wherein said diarteethe amine is used for treating an acute leukemia.11. The method of claim 10 , wherein said acute leukemia is an acute myeloid leukemia (ALM).12. The method of claim 11 , wherein said acute myelocytic leukemia is selected from the group consisting of AML with t(8;22)(q22;q22)(AML/ETO) claim 11 , AML with t(15;17)(q22;q21) claim 11 , (PML-RARα) in AML with recurrent genetic abnormalities claim 11 , AML-M2 claim 11 , and AML-M5. This invention belongs to medical field, specifically, relating to the application of a kind of artemisinin-derivatives and its pharmaceutical salts.Leukemia, a group of diseases characterized by the malignant cloning of the HSCs, is one of the malignant tumors of hematologic system, which jeopardizes the health of human beings. Acute leukemia, especially, is a type of rapidly progressing diseases, which lead to the accumulation of a sum of immature blood cells in bone marrow and blood. It can be divided into ...

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Номер записи: 23

05-12-2013 дата публикации

Crystalline Forms of Tenofovir Dipivoxil Fumarate

Номер: US20130324498A1

Автор: Li Qide, Xia Chunguang, Zhang Aming, ZHANG Xiquan

Принадлежит: Jiangsu Chiatai Tianqing Pharmaceutical Co., Ltd

The present invention relates to a crystalline form of tenofovir dipivoxil fumarate, a crystalline composition and a pharmaceutical composition comprising the crystalline form, and also to a process for preparing the same and the use for prophylaxis or treatment of a disease associated with a viral infection. The crystalline form has an X-ray powder diffraction pattern using Cu-Kα radiation, expressed in terms of lattice spacing “d” comprising peaks at about 18.4714 Å, 5.0350 Å, 4.6380 Å, 4.5347 Å, 4.3838 Å, 4.2874 Å and 3.6304 Å. 1. A crystalline form of tenofovir dipivoxil fumarate , having an X-ray powder diffraction pattern using Cu-Kα radiation , expressed in terms of lattice spacing “d” comprising peaks at about 18.4714 Å , 5.0350 Å , 4.6380 Å , 4.5347 Å , 4.3838 Å , 4.2874 Å and 3.6304 Å.2. The crystalline form of claim 1 , having an X-ray powder diffraction pattern using Cu-Kα radiation claim 1 , expressed in terms of lattice spacing “d” comprising peaks at about 18.4714 Å claim 1 , 8.3234 Å claim 1 , 6.0870 Å claim 1 , 5.0350 Å claim 1 , 4.7262 Å claim 1 , 4.6380 Å claim 1 , 4.5347 Å claim 1 , 4.3838 Å claim 1 , 4.2874 Å claim 1 , 3.9414 Å and 3.6304 Å.3. The crystalline form of claim 2 , having an X-ray powder diffraction pattern using Cu-Kα radiation claim 2 , expressed in terms of lattice spacing “d” comprising peaks at about 18.4714 Å claim 2 , 8.3234 Å claim 2 , 6.7220 Å claim 2 , 6.4396 Å claim 2 , 6.0870 Å claim 2 , 5.0350 Å claim 2 , 4.7262 Å claim 2 , 4.6380 Å claim 2 , 4.5347 Å claim 2 , 4.3838 Å claim 2 , 4.2874 Å claim 2 , 3.9414 Å and 3.6304 Å.4. The crystalline form of claim 3 , having an X-ray powder diffraction pattern using Cu-Kα radiation claim 3 , expressed in terms of lattice spacing “d” comprising peaks at about 18.4714 Å claim 3 , 8.7854 Å claim 3 , 8.3234 Å claim 3 , 6.7220 Å claim 3 , 6.4396 Å claim 3 , 6.0870 Å claim 3 , 5.7268 Å claim 3 , 5.3106 Å claim 3 , 5.0350 Å claim 3 , 4.8756 Å claim 3 , 4.7262 Å claim 3 , 4.6380 Å claim 3 , ...

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Номер записи: 24

19-12-2013 дата публикации

PHARMACEUTICALLY ACCEPTABLE SALT OF (E)-N-[4-[[3-CHLORO-4-(2-PYRIDYLMETHOXY)PHENYL]AMINO]-3-CYANO-7-ETHOXY-6-QUINOLYL]-3-[(2R)-1-METHYLPYRROLIDIN-2-YL]PROP-2-ENAMIDE, PREPARATION METHOD THEREOF, AND MEDICAL USE THEREOF

Номер: US20130338190A1

Автор: Li Xin, Wang Bin

Принадлежит:

Provided as represented by formula (I) is a pharmaceutically acceptable salt of (E)-N-[4-[[3-chloro-4-(2-pyridylmethoxy)phenyl]amino]-3-cyano-7-ethoxy-6-quinolyl]-3-[(2R)-1-methylpyrrolidin-2-yl]prop-2-enamide, a preparation method thereof, and a use thereof as a therapeutic agent, and especially as a protein kinase inhibitor. 2. The salt according to claim 1 , wherein said salt is an inorganic salt.3. The salt according to claim 2 , wherein said inorganic salt is selected from the group consisting of phosphate claim 2 , hydrochloride salt claim 2 , sulfate claim 2 , nitrate and hydrobromide salt.4. The salt according to claim 3 , wherein said inorganic salt is the hydrochloride salt.5. The salt according to claim 4 , wherein n is 2.6. The salt according to claim 1 , wherein said salt is an organic salt.7. The salt according to claim 6 , wherein said organic salt is selected from the group consisting of p-toluenesulfonate claim 6 , methanesulfonate claim 6 , maleate claim 6 , tartrate claim 6 , succinate claim 6 , acetate claim 6 , trifluoroacetate claim 6 , fumarate claim 6 , citrate claim 6 , benzenesulfonate claim 6 , benzoate claim 6 , naphthalenesulfonate claim 6 , lactate and L-malate.8. The salt according to claim 7 , wherein said salt is maleate.9. The salt according to claim 8 , wherein n is 2.10. A process of preparing a pharmaceutically acceptable salt according to claim 1 , comprising a step of reacting (E)-N-[4-[[3-chloro-4-(2-pyridylmethoxy)phenyl]amino]-3-cyano-7-ethoxy-6-quinolyl]-3-[(2R)-1-methylpyrrolidin-2-yl]prop-2-enamide with a corresponding acid to form the salt.11. The process according to claim 10 , wherein said acid is an inorganic acid or an organic acid selected from the group consisting of phosphoric acid claim 10 , hydrochloric acid claim 10 , sulfuric acid claim 10 , nitric acid claim 10 , hydrobromic acid claim 10 , p-toluenesulfonic acid claim 10 , methanesulfonic acid claim 10 , maleic acid claim 10 , tartaric acid claim 10 , ...

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Номер записи: 25

02-01-2014 дата публикации

HEMIFUMARATE SALT OF 1-[4-[1-(4-CYCLOHEXYL-3-TRIFLUOROMETHYL-BENZYLOXYIMINO)-ETHYL]-2-ETHYL-BENZYL]-AZETIDINE-3-CARBOXYLIC ACID

Номер: US20140005162A1

Автор: Ciszewski Lech, DE LA CRUZ Marilyn, Karpinski Piotr H., Mutz Michael, RIEGERT Christian, Schneeberger Ricardo, Vogel Caspar

Принадлежит:

This invention relates to a hemifumarate salt of 1-(4-{1-[(E)-4-cyclohexyl-3-trifluoromethyl-benzyloxyimino]-ethyl}-2-ethyl-benzylyazetidine-3-carboxylic acid (Compound I), to pharmaceutical compositions comprising this salt, to processes for forming this salt and to its use in medical treatment. In addition, the present invention also relates to new polymorphic forms of the hemifumarate salt form of Compound I, as well as to pharmaceutical compositions comprising these polymorphic forms, to processes for obtaining them, and their use in medical treatment. 1. A hemifumarate salt of 1-(4-{1-[(E)-4-cyclohexyl-3-trifluoromethyl-benzyloxyimino]-ethyl}-2-ethyl-benzyl)-azetidine-3-carboxylic acid.2. A hemifumarate salt of 1-(4-{1-[(E)-4-cyclohexyl-3-trifluoromethyl-benzyloxyimino]-ethyl}-2-ethyl-benzyl)-azetidine-3-carboxylic acid according to claim 1 , wherein said salt is substantially crystalline.3. Crystalline Form A of the hemifumarate salt of 1-(4-{1-[(E)-4-cyclohexyl-3-trifluoromethyl-benzyloxyimino]-ethyl}-2-ethyl-benzyl)-azetidine-3-carboxylic acid.4. Crystalline Form A of the hemifumarate salt of 1-(4-{1-[(E)-4-cyclohexyl-3-trifluoromethyl-benzyloxyimino]-ethyl}-2-ethyl-benzyl)-azetidine-3-carboxylic acid according to claim 3 , characterised in that the crystalline form has an X-ray powder diffraction pattern having at least one specific peak at about 2-theta=20.7°.5. Crystalline Form A of the hemifumarate salt of 1-(4-{1-[(E)-4-cyclohexyl-3-trifluoromethyl-benzyloxyimino]-ethyl}-2-ethyl-benzyl)-azetidine-3-carboxylic acid according to claim 3 , characterised in that the crystalline form has an X-ray powder diffraction pattern with specific peaks at about 2-theta=6.9° claim 3 , 17.5° claim 3 , 18.1° claim 3 , 20.4° claim 3 , and 20.7°.6. Crystalline Form A of the hemifumarate salt of 1-(4-{1-[(E)-4-cyclohexyl-3-trifluoromethyl-benzyloxyimino]-ethyl}-2-ethyl-benzyl)-azetidine-3-carboxylic acid according to claim 3 , characterised in that the crystalline form has ...

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Номер записи: 26

23-01-2014 дата публикации

FUMARIC ACID SALT OF 9-[4-(3-CHLORO-2-FLUORO-PHENYLAMINO)-7-METHOXY-QUINAZOLIN-6-YLOXY]-1,4-DIAZA-SPIRO[5.5]UNDECAN-5-ONE, ITS USE AS A MEDICAMENT AND THE PREPARATION THEREOF

Номер: US20140024628A1

Автор: OSTERMEIER Markus, SIEGER Peter

Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

The present invention relates to a compound of formula (I), 2. The compound of formula (I) according to claim 1 , wherein n denotes the number 1.5.3. The crystalline compound of formula (I) according to claim 1 , characterised in that reflections in the X-ray powder diagram occur at dvalues of 17.13 claim 1 , 4.55 claim 1 , 3.46 and 3.20 Å.4. A method for the treatment of inflammatory or allergic diseases of the airways comprising administering a therapeutically effective amount of a compound of to a patient in need thereof.7. The process according to claim 5 , for the stereoselective preparation of a compound of formula (I) claim 5 , characterized in that the process consists of process steps (I) claim 5 , (J) claim 5 , (K) claim 5 , (L) and (M) claim 5 , wherein the process steps (I) to (M) take place successively in the sequence specified.8. The process according to claim 6 , for the stereoselective preparation of a compound of formula (I) claim 6 , characterized in that the process consists of process steps (I) claim 6 , (N) claim 6 , (O) claim 6 , (L) and (M) claim 6 , wherein the process steps (I) to (M) take place successively in the sequence specified.9. The process according to for the stereoselective preparation of a compound of formula (II) claim 5 , characterized in that the process consists of process steps (I) claim 5 , (J) claim 5 , (K) and (L) claim 5 , wherein the process steps (I) to (L) in each case take place successively in the sequence specified.10. The process according to for the stereoselective preparation of a compound of formula (II) claim 6 , characterized in that the process consists of process steps (I) claim 6 , (N) claim 6 , (O) and (L) claim 6 , wherein the process steps (I) to (L) in each case take place successively in the sequence specified.11. A pharmaceutical composition containing a compound of formula (I) according to .12. A medicament combination which contains claim 1 , as a further active substance claim 1 , in addition to ...

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Номер записи: 27

06-02-2014 дата публикации

NOVEL SALTS OF 6-HETEROCYCLE SUBSTITUTED HEXAHYDROPHENANTHRIDINE DERIVATIVES

Номер: US20140039001A1

Автор: HUMMEL Rolf-Peter, Kautz Ulrich, SCHEUFLER Christian, WEBEL Matthias

Принадлежит: TAKEDA GMBH

Disclosed herein are salts of 6-heteroaryl substituted hexahydrophenanthridine PDE4 inhibiting compounds, which can be used in the pharmaceutical industry for the production of pharmaceutical compositions. 113-. (canceled)14. A salt selected from the group consisting of(2R,4a R,10bR)-6-(2,6-Dimethoxy-pyridin-3-yl)-9-ethoxy-8-methoxy-1,2,3,4,4a,10b-hexahydro-phenanthridin-2-ol methansulfonate;(2R,4a R,10bR)-6-(2,6-Dimethoxy-pyridin-3-yl)-9-ethoxy-8-methoxy-1,2,3,4,4a,10b-hexahydro-phenanthridin-2-ol fumarate;(2R,4a R,10bR)-6-(2,6-Dimethoxy-pyridin-3-yl)-9-ethoxy-8-methoxy-1,2,3,4,4a,10b-hexahydro-phenanthridin-2-ol edisilate;(2R,4a R,10bR)-6-(2,6-Dimethoxy-pyridin-3-yl)-9-ethoxy-8-methoxy-1,2,3,4,4a,10b-hexahydro-phenanthridin-2-ol esilate;(2R,4a R,10bR)-6-(2,6-Dimethoxy-pyridin-3-yl)-9-ethoxy-8-methoxy-1,2,3,4,4a,10b-hexahydro-phenanthridin-2-ol hydrobromide; and(2R,4a R,10bR)-6-(2,6-Dimethoxy-pyridin-3-yl)-9-ethoxy-8-methoxy-1,2,3,4,4a,10b-hexahydro-phenanthridin-2-ol tosylate.15. A salt according to which is selected from the group consisting of(2R,4aR,10bR)-6-(2,6-Dimethoxy-pyridin-3-yl)-9-ethoxy-8-methoxy-1,2,3,4,4a,10b-hexahydro-phenanthridin-2-ol hexahydro-phenanthridin-2-ol fumarate; and(2R,4aR,10bR)-6-(2,6-Dimethoxy-pyridin-3-yl)-9-ethoxy-8-methoxy-1,2,3,4,4a,10b-hexahydro-phenanthridin-2-ol methansulfonate.16. A salt according to which is selected from the group consisting of(2R,4aR,10bR)-6-(2,6-Dimethoxy-pyridin-3-yl)-9-ethoxy-8-methoxy-1,2,3,4,4a,10b-hexahydro-phenanthridin-2-ol edisilate;(2R,4aR,10bR)-6-(2,6-Dimethoxy-pyridin-3-yl)-9-ethoxy-8-methoxy-1,2,3,4,4a,10b-hexahydro-phenanthridin-2-ol esilate;(2R,4aR,10bR)-6-(2,6-Dimethoxy-pyridin-3-yl)-9-ethoxy-8-methoxy-1,2,3,4,4a,10b-hexahydro-phenanthridin-2-ol hydrobromide; and(2R,4aR,10bR)-6-(2,6-Dimethoxy-pyridin-3-yl)-9-ethoxy-8-methoxy-1,2,3,4,4a,10b-hexahydro-phenanthridin-2-ol tosylate.17. A salt according to which is(2R,4aR,10bR)-6-(2,6-Dimethoxy-pyridin-3-yl)-9-ethoxy-8-methoxy-1,2,3,4,4a,10b- ...

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Номер записи: 28

06-02-2014 дата публикации

PROCESS FOR PREPARING FESOTERODINE

Номер: US20140039216A1

Автор: Ladani Mahesh, Parekh Viral, Patel Ronak, Patel Samir, PATIL Chetan, Raman Jayaraman Venkat, Raval Prashant, Shah Hiral, Thakor Indrajit

Принадлежит: ALEMBIC PHARMACEUTICALS LIMITED

The present invention relates to an improved process for the preparation of Fesoterodine and pharmaceutically acceptable salts thereof. The present invention particularly relates to a process for the preparation of fesoterodine and pharmaceutically acceptable salts thereof which involves use and preparation of R(+)benzyl tolterodine and fumarate salt of R(+)-[4-benzyloxy-3-(3-diisopropylamino-1-phenylpropyl)-phenyl]-methanol. 2. A process according to claim 1 , wherein resolution of racemic compound of formula (III) through formation of the diastereomeric salt thereof with an optically active acid claim 1 , which may be selected from an optically active acid is an optically active carboxylic acid or sulphonic acid.3. (canceled)4. A process according to claim 2 , wherein an optically active acid is selected from (+) tartaric acid claim 2 , (−) tartaric acid claim 2 , (+) 2 claim 2 ,3-dibenzoyl-D-tartaric acid claim 2 , (−) 2 claim 2 ,3-dibenzoyl-L-tartaric acid claim 2 , mandelic acid claim 2 , 3-chloro mendalic acid claim 2 , abietic acid claim 2 , S-(+)-camphorsulfonic acid claim 2 , di-p-tolyl-D-tartaric acid and di-p-tolyl-L-tartaric acid.5. (canceled)6. A process according to claim 1 , wherein the resolution of racemic compound of formula (III) is carried out in a solvent selected from water claim 1 , a dipolar aprotic solvent claim 1 , a C3-C8 ketone claim 1 , a cyclic or acyclic ether claim 1 , an ester claim 1 , a chlorinated solvent and a polar protic solvent claim 1 , or a mixture claim 1 , of two or more typically two claim 1 , of said solvents claim 1 , more preferably isopropyl alcohol.7. (canceled)8. (canceled)10. An acid addition salt according to claim 9 , wherein said addition salt is selected from hydrochloride claim 9 , hydrobromide claim 9 , sulfate claim 9 , methanesulfonate claim 9 , phosphate claim 9 , nitrate claim 9 , benzoate claim 9 , citrate claim 9 , tartarate claim 9 , fumarate or maleate.1315.-. (canceled)17. The process of claim 16 , ...

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Номер записи: 29

20-02-2014 дата публикации

CRYSTALLINE FORM OF CARBAMOYL-CYCLOHEXANE DERIVATIVES

Номер: US20140051710A1

Автор: Grill Andreas, LIAO Xiangmin, Zhu Hiajian (Jim)

Принадлежит:

The present invention relates to novel crystalline forms of carbarmoyl-cyclohexane derivatives and, more particularly, to novel co-crystalline forms of trans-1{4-[2-[4-(2,3-dichlorophenyl-piperazin-1-yl]-ethyl]-cyclohexyl}-3,3-dimethly urea hydrochloride and an acid such as fumaric acid. Processes for preparing these forms, compositions containing these forms, and methods of use thereof are also described. 1. A co-crystal of trans-1{4-[2-[4-(2 ,3-dichlorophenyl)-piperazin-1-yl]-ethyl]-cyclohexyl}-3 ,3-dimethyl urea hydrochloride and an acid.2. The co-crystal of claim 1 , wherein the acid is fumaric acid.3. The co-crystal of claim 2 , having an-X-ray powder diffraction pattern comprising characteristic peaks at about 8.3 and about 38.5±0.2 degrees 2θ.4. The co-crystal of having an-X-ray powder diffraction pattern comprising characteristic peaks at about 8.3 claim 2 , about 36.5 claim 2 , about 38.5 and about 39.5±0.2 degrees 2θ.5. The co-crystal of having an X-ray powder diffraction pattern substantially as shown in .6. The co-crystal of having a melting endotherm at about 170° C. as determined by differential scanning calorimetry and a characteristic peak at about 8.3±0.2 degrees 2θ in an X-ray powder diffraction pattern.7. A process for preparing a co-crystal of trans-1{4-[2-[4-(2 claim 2 ,3-dichlorophenyl)-piperazin-1-yl]-ethyl]-cyclohexyl}-3 claim 2 ,3-dimethyl urea hydrochloride and an acid claim 2 , comprising:(i) combining trans-1{4-[2-[4-(2,3-dichlorophenyl)-piperazin-1-yl]-ethyl]-cyclohexyl}-3,3-dimethyl urea hydrochloride, the acid and an organic solvent to form a mixture, and(ii) grinding the mixture.8. The process of claim 7 , wherein the trans-1{4-[2-[4-(2 claim 7 ,3-dichlorophenyl)-piperazin-1-yl]-ethyl]-cyclohexyl}-3 claim 7 ,3-dimethyl urea hydrochloride and the acid are present in a 1:1 ratio.9. The process of claim 7 , wherein the organic solvent is selected from the group consisting of tetrahydrofuran claim 7 , methanol claim 7 , acetonitrile claim ...

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Номер записи: 30

07-01-2021 дата публикации

NOVEL FATTY ACIDS AND THEIR USE IN CONJUGATION TO BIOMOLECULES

Номер: US20210000964A1

Автор: BARNES David Weninger, BOSE Avirup, BRUCE Alexandra Marshall, DUTTAROY Alokesh, IBEBUNJO Chikwendu, KANTER Aaron, KIRMAN Louise Clare, LOU Changgang, USERA Aimee Richardson, YAMADA Ken, Yuan Jun, ZECRI Frederic

Принадлежит:

The invention provides a conjugate comprising a biomolecule linked to a fatty acid via a linker wherein the fatty acid has the following Formulae A1, A2 or A3: 124-. (canceled)26. The compound according to claim 25 , or an amide claim 25 , ester or pharmaceutically acceptable salt thereof claim 25 , wherein the compound is of Formula A1 wherein at least one of Rand Ris COH.29. A peptide selected from MH(199-308)hGDF15 (SEQ ID NO: 4) claim 25 , MHA(200-308)hGDF15 (SEQ ID NO: 6) claim 25 , AHA(200-308)hGDF15 (SEQ ID NO: 7) claim 25 , AH(199-308)hGDF15 (SEQ ID NO: 5) claim 25 , MHHHHHHM-hGDF15 (SEQ ID NO: 2) and MHHHHHH-hGDF15 (SEQ ID NO: 1). This application is a divisional application of U.S. application Ser. No. 15/985,060, filed on May 21, 2018, now allowed, which is a divisional of Ser. No. 14/738,272, filed on Jun. 12, 2015, now U.S. Pat. No. 10,588,980, which claims priority to, and the benefit under 35 U.S.C. § 119(e) of U.S. Provisional Application No. 62/107,016, filed Jan. 23, 2015, U.S. Provisional Application No. 62/082,327, filed on Nov. 20, 2014, and U.S. Provisional Application No. 62/015,862 filed on Jun. 23, 2014, the entire contents of each of which are incorporated herein by reference in their entireties.The contents of the text file named “PAT056274-US-DIV02_Sequence Listing_ST25.txt,” which was created on May 26, 2020 and is 33 KB in size, are hereby incorporated by reference in their entireties.The present invention relates to novel conjugates of GDF15 which have improved half-life and duration of action, method of making them and using them. The invention further relates to novel fatty acids and their use in extending the half-life of biomolecules via conjugation.Peptides and proteins are widely used in medical practice, and since they can be produced by recombinant DNA technology it can be expected that their importance will increase also in the years to come. The number of known endogenous peptides and proteins with interesting biological ...

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Номер записи: 31

02-01-2020 дата публикации

SALTS AND POLYMORPHS OF 8-FLUORO-2-{4-[(METHYLAMINO)METHYL]PHENYL}-1,3,4,5-TETRAHYDRO-6H-AZEPINO[5,4,3-CD]INDOL-6-ONE

Номер: US20200000821A1

Автор: Basford Patricia Ann, Campeta Anthony Michael, Gillmore Adam, Jones Matthew Cameron, Kougoulos Eleftherios, Luthra Suman, Walton Robert

Принадлежит:

The present invention relates to novel polymorphic forms of 8-fluoro-2-{4-[(methylamino)methyl]phenyl}-1,3,4,5-tetrahydro-6H-azepino[5,4,3-cd]indol-6-one, and to processes for their preparation. Such polymorphic forms may be a component of a pharmaceutical composition and may be used to treat a mammalian disease condition mediated by poly(ADP-ribose) polymerase activity including the disease condition such as cancer. 17-. (canceled)8. A process for preparing a solid dosage form containing a camsylate salt of 8-fluoro-2-{4-[(methylamino)methyl]phenyl}-1 ,3 ,4 ,5-tetrahydro-6H-azepino[5 ,4 ,3-cd]indol-6-one , comprisingi) preparing a first vessel comprising 8-fluoro-2-{4-[(methylamino)methyl] phenyl}-1,3,4,5-tetrahydro-6H-azepino[5,4,3-cd]indol-6-one and a first solvent comprising one or more of water, an alcohol, and an ether;ii) preparing a second vessel comprising camphor sulfonic acid and a second solvent comprising one or more of water, an alcohol, and an ether;iii) combining the contents of the first vessel and the second vessel to form a camsylate salt of 8-fluoro-2-{4-[(methylamino)methyl]phenyl}-1,3,4,5-tetrahydro-6H-azepino[5,4,3-cd]indol-6-one; andiv) isolating the camsylate salt formed in step iii);v) combining the isolated camsylate salt with one or more of a pharmaceutically acceptable carrier, a pharmaceutically acceptable diluent, a pharmaceutically acceptable vehicle, or a pharmaceutically acceptable excipient; andvi) preparing the solid dosage form by one or more processes selected from mixing, granulating, and compressing.9. The process of wherein the camphor sulfonic acid is S-camphor sulfonic acid.10. The process of wherein the camphor sulfonic acid is R-camphor sulfonic acid.11. The process of wherein the camphor sulfonic acid comprises a ratio of R-camphor sulfonic acid and S-camphor sulfonic acid.12. The process of wherein the camphor sulfonic acid is selected from 1R:1S-camphor sulfonic acid claim 11 , 1R:9S-camphor sulfonic acid claim 11 , 1R ...

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Номер записи: 32

04-01-2018 дата публикации

WATER-SOLUBLE PACKETS

Номер: US20180002084A1

Автор: Friedrich Steven G., KEULEERS Robby Renilde Francois, Nii Shinsuke, Yeung Lee K.

Принадлежит:

The disclosure provides a water soluble pouch including at least two sealed compartments, the pouch including outer walls including water soluble film including a water soluble resin, and an inner wall including water soluble film including a water soluble resin, the outer wall films being sealed to the inner wall film, the outer wall films being characterized by: a dissolution time of 300 seconds or less, the water soluble resin of the outer wall films having a viscosity in a range of 14.5 cP to 25cP, and a pouch strength of at least 200 N, and the inner wall film being characterized by: a dissolution time of 300 seconds or less, the water soluble resin of the inner film having viscosity in a range of 12 cP to 14.5 cP, and a tackiness value of at least 1500 g/s. 1. A water soluble pouch defining an interior pouch volume , the pouch comprising at least two water-soluble films , wherein a film of the at least two water-soluble films comprises a polyvinyl alcohol resin comprising a polyvinyl alcohol copolymer comprising an anionic monomer unit , optionally one or more of maleic acid , monoalkyl maleate , dialkyl maleate monomethyl maleate dimethyl maleate , maleic anhydride , alkali metal salts of the foregoing , esters of the foregoing , and combinations of the foregoing , and wherein the water-soluble film comprising a polyvinyl alcohol copolymer comprising an anionic monomer unit is sealed to another film using a sealing solution comprising water , one or more diols and/or glycols , and a surfactant.2. The water-soluble pouch of claim 1 , wherein the surfactant is one or more selected from polyoxyethylenated polyoxypropylene glycols claim 1 , alcohol ethoxylates claim 1 , alkylphenol ethoxylates claim 1 , tertiary acetylenic glycols and alkanolamides (nonionics) claim 1 , polyoxyethylenated amines claim 1 , quaternary ammonium salts and quaternized polyoxyethylenated amines (cationics) claim 1 , amine oxides claim 1 , N-alkylbetaines and sulfobetaines ( ...

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Номер записи: 33

03-01-2019 дата публикации

PROCESS FOR PREPARING AN ANTI-CANCER AGENT, 1-((4-(4-FLUORO-2-METHYL-1H-INDOL-5-YLOXY)-6-METHOXYQUINOLIN-7-YLOXY)METHYL)CYCLOPROPANAMINE, ITS CRYSTALLINE FORM AND ITS SALTS

Номер: US20190002435A1

Автор: Chen Guoqing Paul, Yan Changren

Принадлежит:

The present invention relates a new process to synthesize 1-((4-(4-Fluoro-2-methyl-1H-indol-5-yloxy)-6-methoxyquinolin-7-yloxy)methyl)cyclopropanamine (AL3818). A stable crystalline form of Al3818 has been prepared. Salts and their crystalline forms of AL3818 have been also prepared. Anti-cancer and optometric activities of AL3818 and its salts have been further tested. New process has been outlined in Scheme I. 2. The compound of claim 1 , wherein the characteristic peaks have an intensity greater than about 10%.5. The compound of claim 1 , wherein the 1-((4-(4-Fluoro-2-methyl-1H-indol-5-yloxy)-6-methoxy-quino-lin-7-yloxy)methyl)cyclopropanamine is a bishydrochloride salt.6. A method of treating a neoplastic disease claim 1 , said method comprising:administering to a patient in need thereof a salt of 1-((4-(4-Fluoro-2-methyl-1H-indol-5-yloxy)-6-methoxyquino-lin-7-yloxy)-methyl)-cyclopropanamine; andadministering a second therapeutic agent to the patient;wherein the 1-((4-(4-Fluoro-2-methyl-1H-indol-5-yloxy)-6-methoxyquino-lin-7-yloxy)-methyl)-cyclopropanamine salt is selected from: a bishydrochloride acid salt, a bishydrochloridehydrate acid salt, a bismaleic acid salt and a succinic acid salt;wherein the neoplastic disease comprises solid tumors, selected from lung, renal, colorectal, gastric, melanoma, head/neck, thyroid, pancreatic, liver, prostate, bladder, brain, sarcoma, breast, ovarian, cervical and endometrial cancers; and blood cancers, selected from ALL, CLL, AML, CML and Multiple Myeloma.7. The method of claim 6 , wherein the second therapeutic agent is a chemotherapeutic agent.8. The method of claim 7 , wherein the second therapeutic agent is selected from a platinum-based agent and a taxane-based agents.9. The method of claim 7 , wherein the second therapeutic agent is selected from paclitaxel claim 7 , cisplatin claim 7 , and carboplatin.10. The method of claim 7 , further comprising administering a third therapeutic agent to the patient.11. The ...

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Номер записи: 34

04-01-2018 дата публикации

PROCESS FOR PREPARING AN ANTI-CANCER AGENT, 1-((4-(4-FLUORO-2-METHYL-1H-INDOL-5-YLOXY)-6-METHOXYQUINOLIN-7-YLOXY)METHYL)CYCLOPROPANAMINE, ITS CRYSTALLINE FORM AND ITS SALTS

Номер: US20180002311A1

Автор: Chen Guoqing Paul, Yan Changren

Принадлежит:

The present invention relates a new process to synthesize 1-((4-(4-Fluoro-2-methyl-1H-indol-5-yloxy)-6-methoxyquinolin-7-yloxy)methyl)cyclopropanamine (AL3818). A stable crystalline form of A13818 has been prepared. Salts and their crystalline forms of AL3818 have been also prepared. Anti-cancer and optometric activities of AL3818 and its salts have been further tested. New process has been outlined in Scheme I. 5. The process to prepare intermediate (Z) according to claim 1 , wherein R is H or —OMe claim 1 , KI is used according to first step of Process A1 and A2 with DMF at 80° C. and wherein Lutidine is used according to first step of Process B1 and B2 at 135° C.6. The process to synthesize 1-((4-(4-Fluoro-2-methyl-1H-indol-5-yloxy)-6-methoxyquinolin-7-yloxy)methyl)cyclopropanamine (AL3818) according to claim 1 , wherein R is H claim 1 , HCOONH4/Pd/C is used for the deprotection step at 45° C.; wherein R is —OMe claim 1 , DCM/TFA (10/1) is used for the deprotection step at 25° C.7. A salt of 1-((4-(4-Fluoro-2-methyl-1H-indol-5-yloxy)-6-methoxyquinolin-7-yloxy)-methyl)-cyclopropanamine claim 1 , wherein the salt is selected from: a bishydrochloride acid salt claim 1 , a bishydrochloridehydrate acid salt claim 1 , a bismaleic acid salt and a succinic acid salt.12. A salt of 1-((4-(4-Fluoro-2-methyl-1H-indol-5-yloxy)-6-methoxyquinolin-7-yloxy)methyl)-cyclopropanamine according to with DSC and TGA having following characteristics:{'figref': [{'@idref': 'DRAWINGS', 'FIG. 4'}, {'@idref': 'DRAWINGS', 'FIG. 5'}], 'bishydrochloride acid salt with DSC Melting Range (Exo): 249-280 with Peak Temp=268° C. TGA demonstrating as an unsolvated material with weight loss at about 230° C. (between 225-235° C.), shown in , ;'}{'figref': [{'@idref': 'DRAWINGS', 'FIG. 7'}, {'@idref': 'DRAWINGS', 'FIG. 8'}], 'bishydrochloridehydrate acid salt with DSC Melting Range (Exo): 207-260° C. with Peak Temp=226° C. TGA demonstrating 2.68% (˜3%, 1 water) weight loss till 120° C. (between 115-125° ...

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Номер записи: 35

07-01-2021 дата публикации

NOVEL CRYSTALLINE FORMS OF TAMIBAROTENE FOR TREATMENT OF CANCER

Номер: US20210002209A1

Автор: HANNA Andrew, HANNA Mazen, PERERA Manomi, YAN Jiyu

Принадлежит:

Synthesis and characterization of novel tamibarotene forms suitable for pharmaceutical compositions in drug delivery systems to treat human or warm-blooded mammal diseases. 1. A crystalline form of tamibarotene selected from the group consisting of: tamibarotene:adipic acid , tamibarotene:DL-aspartic acid , tamibarotene:acetylsalicylic acid , tamibarotene:biphenyl-4-carboxylic acid , tamibarotene:caffeic acid , tamibarotene:decanoic acid , tamibarotene:diphenic acid , tamibarotene:gallic acid , tamibarotene:fumaric acid , tamibarotene:ibuprofen , tamibarotene:maleic acid , tamibarotene:nicotinamide , tamibarotene:isonicotinamide , tamibarotene:citric acid , tamibarotene:nicotinic acid , tamibarotene:3 ,4-dihydroxybenzoic acid , tam ibarotene:glutaric acid , and tamibarotene:L-malic acid.2. The crystalline form of claim 1 , wherein the crystalline form is tamibarotene:adipic acid.3. The crystalline form of claim 2 , wherein the crystalline form is characterized by a powder X-ray diffraction pattern comprising one or more powder X-ray diffraction peaks selected from the group consisting of: about 10.5 claim 2 , 12.0 claim 2 , 14.5 claim 2 , 22.0 claim 2 , and 26.0° 2θ±0.2° 2θ.4. The crystalline form of claim 1 , wherein the crystalline form is tamibarotene:DL-aspartic acid.5. The crystalline form of claim 4 , wherein the crystalline form is characterized by a powder X-ray diffraction pattern comprising one or more powder X-ray diffraction peaks selected from the group consisting of: about 6.5 claim 4 , 10.0 claim 4 , 11.5 claim 4 , and 19.5° 2θ±0.2° 2θ.6. The crystalline form of claim 1 , wherein the crystalline form is tamibarotene:acetylsalicylic acid.7. The crystalline form of claim 6 , wherein the crystalline form is characterized by a powder X-ray diffraction pattern comprising one or more powder X-ray diffraction peaks selected from the group consisting of: about 8.0 claim 6 , 8.5 claim 6 , 15.5 claim 6 , 23.0 claim 6 , and 27.0° 2θ±0.2° 2θ.8. The crystalline ...

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Номер записи: 36

04-01-2018 дата публикации

USE OF A FIRST FILM AND A SECOND FILM TO IMPROVE SEAL STRENGTH OF A WATER-SOLUBLE

Номер: US20180002647A1

Автор: COURCHAY Florence Catherine, KEULEERS Robby Renilde Francois, LABEQUE Regine, Renmans Marc Rene Bert, Souter Philip Frank

Принадлежит:

The present invention relates to the use of a first water-soluble film and a second water-soluble film to make a unit dose article and the use of said unit dose article. 1. Use of a first water-soluble film and a second water-soluble film in the manufacture of a water-soluble unit dose article optionally comprising a composition contained within the unit dose article , wherein the first water-soluble film and the second water-soluble film are sealed together along a seal area , in order to improve the seal strength in the seal area;wherein the first water-soluble film and the second water-soluble film are chemically different to one another and wherein the first water-soluble film has a first water capacity, and wherein the second water-soluble film has a second water capacity, wherein the first water capacity is less than the second water capacity, and wherein the difference between the water capacity of the first water soluble film and the second water-soluble film is between 0.01% and 1%;provided that when the composition is a fabric care or household care composition and a film comprises a blend of a polyvinyl alcohol homopolymer resin and an anionic polyvinyl alcohol copolymer resin, then both then first water soluble film and the second water soluble film comprise blends that include 65 wt. % or greater of an anionic polyvinyl alcohol copolymer resin; andprovided that when the composition is a fabric care or household care composition and a film comprises a blend of at least two anionic polyvinyl alcohol copolymer resins, then both then first water soluble film and the second water soluble film comprise blends of at least two anionic polyvinyl alcohol copolymer resins.2. The use according to to improve the seal strength in the seal area to reduce the volume of scrapped material during manufacture of water-soluble unit dose articles.3. The use according to claim 1 , wherein the first water-soluble film has a water capacity from 1% to 10%.4. The use according to ...

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Номер записи: 37

01-01-2015 дата публикации

Novel morpholinyl derivatives useful as mogat-2 inhibitors

Номер: US20150005305A1

Автор: Maria Carmen Fernnandez, Maria Rosario Gonzalez-Garcia

Принадлежит: Eli Lilly and Co

The present invention provides compounds of Formula I or a pharmaceutical salt thereof, methods of treating hypertriglyceridemia using the compounds; and a process for preparing the compounds.

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Номер записи: 38

20-01-2022 дата публикации

Co-crystals of 2-methyl-1 -[(4-[6-(trifluoromethyl)pyridin-2-yl]-6-{[2-(trifluoromethyl) pyridin-4-yl]amino}-1,3,5-triazin-2-yl)amino]propan-2-ol, compositions and methods of use thereof

Номер: US20220017490A1

Автор: Eric A. Fromme, Kevin J. Klopfer

Принадлежит: Celgene Corp

Provided herein are co-crystals comprising Compound 1 and a coformer. Pharmaceutical compositions comprising the co-crystals and methods for treating, preventing and managing disease are also disclosed.

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Номер записи: 39

11-01-2018 дата публикации

SALTS OF AZA-BICYCLIC DI-ARYL ETHERS AND METHODS TO MAKE THEM OR THEIR PRECURSORS

Номер: US20180009801A1

Автор: Bianchi Jean-Claude, Buerger Eckart, Har Denis, Karpinski Piotr H., Marterer Wolfgang, Pignone Massimo, Prashad Mahavir, Stingelin Doris, Sutter Bertrand, Villhauer Edwin Bernard, Vivelo James Anthony, Waykole Liladhar Murlidhar, Wu Raeann

Принадлежит:

The present invention relates to salts of (R)-3-(6-(4-methylphenyl)-pyridin-3-yloxy)-1-aza-bicyclo[2.2.2]octane, to methods for making them or their precursors, to pharmaceutical compositions comprising them, and to their use as medicaments. 1. A salt of (R)-3-(6-(4-methylphenyI)-pyridin-3-yloxy)-1-aza-bicyclo[2.2.2]octane wherein said salt is the fumarate , maleate , chloride , phosphate , succinate , or malonate salt of (R)-3-(6-(4-methylphenyl)-pyridin-3-yloxy)-1-aza-bicyclo[2.2.2]octane.2. The salt according to claim 1 , wherein the salt is the mono-fumarate salt of (R)-3-(6-(4-methylphenyl)-pyridin-3-yloxy)-1-aza-bicyclo[2.2.2]octane in crystalline form.3. The salt according to claim 2 , wherein the salt is characterized by an XRPD pattern substantially the same as the XRPD pattern shown in .4. The salt according to claim 1 , wherein the salt is the mono-fumarate salt of (R)-3-(6-(4-methylphenyl)-pyridin-3-yloxy)-1-aza-bicyclo[2.2.2]octane in crystalline form claim 1 , wherein the mean particle size of the crystals is at least 15 μm.5. The salt according to claim 2 , wherein the salt is the mono-fumarate salt of (R)-3-(6-(4-methylphenyl)-pyridin-3-yloxy)-1-aza-bicyclo[2.2.2]octane in crystalline form claim 2 , and wherein the salt is in substantially pure form.6. The salt according to claim 2 , wherein the salt is the mono-fumarate salt of (R)-3-(6-(4-methylphenyl)-pyridin-3-yloxy)-1-aza-bicyclo[2.2.2]octane in crystalline form claim 2 , and wherein the salt has a purity greater than 90 weight %.7. A method for the prevention claim 1 , treatment claim 1 , and/or delay of progression of a disease or condition claim 1 , in which nAChR α7 activation plays a role or is implicated claim 1 , in a subject in need of such treatment claim 1 , which comprises administering to such subject a therapeutically effective amount of a salt as defined in .8. A method for the prevention claim 1 , treatment claim 1 , and/or delay of progression of psychiatric or neurodegenerative ...

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Номер записи: 40

18-01-2018 дата публикации

4-AZIDOBUTYLAMINES AND PROCESSES FOR PREPARING

Номер: US20180016226A1

Автор: PEREIRA David Eugene, SCHNEIDER Stephen E.

Принадлежит:

Neat 4-azidobutylamine and sails of 4-azidobutylamine and processes for producing the same are described herein. Amines represent a large class of organic compounds containing a basic nitrogen atom having a lone pair of electrons and one or more substituent groups. Many amines are used as precursors and feedstocks in a wide variety of industries such as textiles, agriculture, plastics, and pharmaceuticals. One such amine is 4-azidobutylamine, N3-(CH2)4NH2, an amine of butane that also includes an azide. 1. A process for preparing 4-azidobutylamine , the process comprising isolating the 4-azidobutylamine from a solvent that is substantially free or free of a chlorinated solvent.2. The process of wherein the solvent is N claim 1 , N-dimethyformamide or MTBE claim 1 , or a mixture thereof.3. The process of wherein the solvent is an aqueous solution.4. The process of further comprising raising the pH of the mixture.5. The process of further comprising separating an aqueous layer from the mixture.6. (canceled)7. Isolated 4-azidobutylamine substantially free of or free of a chlorinated solvent.8. An isolated salt of 4-azidobutylamine claim 4 , where the salt comprises a nitrate claim 4 , fluoride claim 4 , bromide claim 4 , iodide claim 4 , sulfate claim 4 , chlorosulfonate claim 4 , methanesulfonate claim 4 , toluenesulfonate claim 4 , phosphate claim 4 , phosphonate claim 4 , oxalate claim 4 , borate claim 4 , citrate claim 4 , malonate claim 4 , formate claim 4 , butyrate claim 4 , maleate claim 4 , propionate claim 4 , pyruvate claim 4 , benzoate claim 4 , or lactate claim 4 , or a combination thereof.910.-. (canceled)11. The salt of comprising an acid claim 8 , wherein the acid is selected from the group consisting of hydroiodide claim 8 , hydrobromide claim 8 , hydrofluoride claim 8 , nitric acid claim 8 , chlorosulfonic acid claim 8 , malonic acid claim 8 , formic acid claim 8 , butyric acid claim 8 , maleic acid claim 8 , propionic acid claim 8 , pyruvic acid ...

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Номер записи: 41

28-01-2016 дата публикации

Salts and solid forms of isoquinolinones and composition comprising and methods of using the same

Номер: US20160024051A1

Автор: Alexander Redvers Eberlin, Andrew B. HAGUE, Daniel G. Genov, Louis Grenier, Ludovic Sylvain Marc RENOU, Susana Del Rio Gancedo

Принадлежит: Infinity Pharmaceuticals Inc

Solid forms of chemical compounds that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein. Also provided herein are processes for preparing compounds, solid forms thereof, and pharmaceutical compositions thereof.

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Номер записи: 42

22-01-2015 дата публикации

Maleate Salts of a Quinazoline Derivative Useful as an Antiangiogenic Agent

Номер: US20150025091A1

Автор: MCCABE James

Принадлежит: AstraZeneca AB

The present invention relates to AZD2171 maleate salt, to particular crystalline forms of AZD2171 maleate salt, to processes for their preparation, to pharmaceutical compositions containing them as active ingredient, to their use in the manufacture of medicaments for use in the production of antiangiogenic and/or vascular permeability reducing effects in warm-blooded animals such as humans, and to their use in methods for the treatment of disease states associated with angiogenesis and/or increased vascular permeability. 1. A maleate salt of AZD2171.2. A maleate salt of AZD2171 claim 1 , according to claim 1 , in the crystalline form claim 1 , Form A.3. A maleate salt of AZD2171 claim 1 , according to claim 1 , in the crystalline form claim 1 , Form B.4. A maleate salt of AZD2171 claim 2 , according to claim 2 , in the crystalline form claim 2 , Form A claim 2 , wherein said salt has an X-ray powder diffraction pattern with at least one specific peak at about 2-theta=21.5°.5. A maleate salt of AZD2171 claim 2 , according to claim 2 , in the crystalline form claim 2 , Form A claim 2 , wherein said salt has an X-ray powder diffraction pattern with at least one specific peak at about 2-theta=16.4°.6. A maleate salt of AZD2171 claim 2 , according to claim 2 , in the crystalline form claim 2 , Form A claim 2 , wherein said salt has an X-ray powder diffraction pattern with at least two specific peaks at about 2-theta=21.5 and 16.4°.7. A maleate salt of AZD2171 claim 2 , according to claim 2 , in the crystalline form claim 2 , Form A claim 2 , wherein said salt has an X-ray powder diffraction pattern with specific peaks at about 2-theta=21.5 claim 2 , 16.4 claim 2 , 24.4 claim 2 , 20.7 claim 2 , 25.0 claim 2 , 16.9 claim 2 , 12.1 claim 2 , 22.2 claim 2 , 17.4 and 17.6°.8. A maleate salt of AZD2171 claim 2 , according to claim 2 , in the crystalline form claim 2 , Form A claim 2 , wherein said salt has an X-ray powder diffraction pattern substantially the same as the X-ray ...

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Номер записи: 43

10-02-2022 дата публикации

Solid forms of n-(4-fluoro-3-(6-(3-methylpyridin-2-yl)-[1,2,4]triazolo[1,5-a]pyrimidin-2-yl)phenyl)-2,4-dimethyloxazole-5-carboxamide

Номер: US20220041604A1

Автор: Andreas Kordikowski, Bo Yu, Hongyong KIM, Irene Xia, Jing Zhang, Siyi JIANG, Yi Zhao, Yudong CAO

Принадлежит: NOVARTIS AG

The application relates to N-(4-fluoro-3-(6-(3-methylpyridin-2-yl)-[1,2,4]triazolo[1,5-a]pyrimidin-2-yl)phenyl)-2,4-dimethyloxazole-5-carboxamide (Compound I) fumaric acid co-crystals and X-ray amorphous complexes of Compound (I) and fumaric acid. The application also provides methods of making the same; pharmaceutical compositions comprising them; and their use in treating, preventing, inhibiting, ameliorating, or eradicating the pathology and/or symptomology of a disease caused by a kinetoplastid parasite, such as leishmaniasis, human African trypanosomiasis and Chagas disease.

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Номер записи: 44

28-01-2021 дата публикации

Functionalized long-chain hydrocarbon mono- and di-carboxylic acids and their use for the prevention or treatment of disease

Номер: US20210024447A1

Автор: Daniela Carmen Oniciu

Принадлежит: Espervita Therapeutics Inc

This invention provides compounds of Formulae (IA), (IB), (IC), (ID), (IE), (IF), (IG), (IH), (IJ), (IK), (IL), (II), (III), (IIIA), and (IIIB); pharmaceutically acceptable salts and solvates thereof; and compositions thereof. This invention further provides methods for treating a disease, including but not limited to, liver disease or an abnormal liver condition; cancer (such as hepatocellular carcinoma or cholangiocarcinoma); a malignant or benign tumor of the lung, liver, gall bladder, bile duct or digestive tract; an intra- or extra-hepatic bile duct disease; a disorder of lipoprotein; a lipid-and-metabolic disorder; cirrhosis; fibrosis; a disorder of glucose metabolism; a cardiovascular or related vascular disorder; a disease resulting from steatosis, fibrosis, or cirrhosis; a disease associated with increased inflammation (such as hepatic inflammation or pulmonary inflammation); hepatocyte ballooning; a peroxisome proliferator activated receptor-associated disorder; an ATP citrate lyase disorder; an acetyl-coenzyme A carboxylase disorder; obesity; pancreatitis; or renal disease.

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Номер записи: 45

28-01-2021 дата публикации

POLYMORPHIC FORMS OF AFATINIB FREE BASE AND AFATINIB DIMALEATE

Номер: US20210024506A1

Автор: AZIM Abul, BHAVANAM Poli Reddy, Cabri Walter, KACHHADIA Nikunj, Lahiri Saswata, MISHRA Bhuwan Bhaskar, PANDA Nilendu, RAY Krishanu, SINGH Kumber

Принадлежит: FRESENIUS KABI ONCOLOGY LIMITED

The present invention relates to crystalline forms of Afatinib and its dimaleate salt. The present invention also relates to processes for the preparation of crystalline forms of Afatinib and its dimaleate salt. The present invention further relates to pharmaceutical compositions of such crystalline forms of Afatinib dimaleate and use thereof in the treatment of a patient in need thereof. 1. A process for preparing a crystalline form of afatinib dimaleate comprising:a) dissolving afatinib in acetonitrileb) adding maleic acid;c) isolating afatinib dimaleate;d) treating with ethyl acetate; ande) isolating the crystalline form of afatinib dimaleate.2. The process of claim 1 , wherein the maleic acid is added as a solution of maleic acid in acetonitrile.3. The process of claim 2 , wherein the solution of afatinib and maleic acid in acetonitrile is obtained at ambient temperature.4. The process of claim 1 , wherein the afatinib dimaleate of step c) is isolated by a method selected from extraction claim 1 , precipitation claim 1 , cooling claim 1 , filtration claim 1 , centrifugation claim 1 , and mixtures thereof.5. The process of claim 4 , wherein the afatinib dimaleate of step c) is isolated by vacuum filtration.6. The process of claim 1 , wherein the isolated afatinib dimaleate of step c) is washed with acetonitrile and then dried.7. The process of claim 1 , wherein the crystalline form of afatinib dimaleate is isolated by a method selected from extraction claim 1 , precipitation claim 1 , cooling claim 1 , filtration claim 1 , centrifugation claim 1 , and mixtures thereof.8. The process of claim 7 , wherein the crystalline form of afatinib dimaleate is isolated by vacuum filtration.9. The process of claim 1 , wherein the crystalline form of afatinib dimaleate is washed with ethyl acetate and then dried.10. A crystalline form of afatinib dimaleate obtained by the process of .11. A pharmaceutical composition comprising the crystalline form of afatinib dimaleate of and ...

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Номер записи: 46

04-02-2016 дата публикации

NOVEL FATTY ACIDS AND THEIR USE IN CONJUGATION TO BIOMOLECULES

Номер: US20160030585A1

Автор: BARNES David Weninger, BOSE Avirup, BRUCE Alexandra Marshall, DUTTAROY Alokesh, IBEBUNJO Chikwendu, KANTER Aaron, KIRMAN Louis Clare, LOU Changgang, USERA Aimee Richardson, YAMADA Ken, Yuan Jun, ZECRI Frederic

Принадлежит: NOVARTIS AG

The invention provides a conjugate comprising a biomolecule linked to a fatty acid via a linker wherein the fatty acid has the following Formulae A1, A2 or A3: 4. A conjugate according to wherein the linker comprises alkyl claim 1 , alkenyl claim 1 , cycloalkyl claim 1 , aryl claim 1 , heteroaryl claim 1 , heterocyclyl claim 1 , polyethylene glycol claim 1 , one or more natural or unnatural amino acids claim 1 , or combination thereof claim 1 , wherein each of the alkyl claim 1 , alkenyl claim 1 , cycloalkyl claim 1 , aryl claim 1 , heteroaryl claim 1 , heterocyclyl claim 1 , polyethylene glycol and/or the natural or unnatural amino acids are optionally combined and linked together or linked to the biomolecule and/or to the fatty acid moiety via a chemical group selected from —C(O)O— claim 1 , —OC(O)— claim 1 , —NHC(O)— claim 1 , —C(O)NH— claim 1 , —O— claim 1 , —NH— claim 1 , —S— claim 1 , —C(O)— claim 1 , —OC(O)NH— claim 1 , —NHC(O)—O— claim 1 , ═NH—O— claim 1 , ═NH—NH— or ═NH—N(alkyl)-; or an amide claim 1 , ester or a pharmaceutically acceptable salt thereof.7. A conjugate according to wherein the linker comprises one or more amino acids independently selected from histidine claim 1 , methionine claim 1 , alanine claim 1 , glutamine claim 1 , asparagine and glycine; or an amide claim 1 , an ester or a pharmaceutically acceptable salt thereof.8. A conjugate according to wherein the biomolecule is selected from: 1) human Growth Differentiation Factor 15 (GDF15) claim 1 , homologs claim 1 , variants claim 1 , mutants claim 1 , fragments and other modified forms thereof or a dimer thereof; 2) an APJ agonist peptide claim 1 , 3) oxytocin receptor agonist peptide claim 1 , 4) serelaxin claim 1 , 5) NPFF claim 1 , 6) a PIP peptide claim 1 , 7) an FGF23 peptide 8) AgRP peptide and 9) a siRNA; or an amide claim 1 , an ester or a pharmaceutically acceptable salt thereof.10. A mixture comprising the conjugate according to having Formula C and the conjugate according to ...

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Номер записи: 47

01-02-2018 дата публикации

METHOD OF PRODUCING POTASSIUM SORBATE PARTICLES

Номер: US20180028995A1

Автор: Chen Lijun, Chen Yuanzhe, Huang Conghui, Lu Anna, Wang Guojun, Wang Handong, Xiao Gongnian

Принадлежит:

The present invention discloses a method of producing potassium sorbate particles, comprising the steps of: 1. A method of producing potassium sorbate particles , comprising the steps of:(1) preparing a potassium sorbate solution;(2) spray drying;(3) spray forming;(4) indirectly drying with steam on a vibration fluidized bed; and(5) swing-type sifting;in step (3), a binder is obtained by spray drying after adding sorbitol to the potassium sorbate solution prepared in step (1), and the binder is mixed with the potassium sorbate powder obtained by spray drying in step (2) to undergo the spray forming process;based on weight ratio, the weight ratio of the sorbitol required to prepare the binder to the potassium sorbate solution required to prepare the binder is 0.05-0.1%:1.2. A method of producing potassium sorbate particles according to claim 1 , wherein the amount of the used binder is 10-15% of the weight of the potassium sorbate powder.3. A method of producing potassium sorbate particles according to claim 1 , wherein the drying temperature in step (2) is 200-260° C.4. A method of producing potassium sorbate particles according to claim 1 , wherein the steam temperature in step (4) is 70-95° C.5. A method of producing potassium sorbate particles according to claim 1 , wherein in step (4) claim 1 , the vibration frequency of the vibration fluidized bed is 300-600 r/min claim 1 , the vibration amplitude is 1-3 mm claim 1 , and the residence time of the formed potassium sorbate particles is 20-50 s.6. A method of producing potassium sorbate particles according to claim 1 , wherein in step (5) claim 1 , the swing rate is 15-30 Hz.7. A method of producing potassium sorbate particles according to claim 1 , wherein a method of preparing the potassium sorbate solution comprises:Step1: based on part by weight, adding a water solution with 400-500 parts of potassium carbonate to 1000 parts of crude sorbic acid;Step2: based on part by weight, adding 45-55 parts of activated ...

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Номер записи: 48

29-01-2015 дата публикации

ARYL METHYL BENZOQUINAZOLINONE M1 RECEPTOR POSITIVE ALLOSTERIC MODULATORS

Номер: US20150031713A1

Автор: Beshore Douglas C., Di Marco Christina Ng, Greshock Thomas J., Kuduk Scott D.

Принадлежит:

The present invention is directed to benzoquinazilinone compounds of formula (I) 162-. (canceled)63. A pharmaceutically acceptable salt of rac-3-[trans-2-hydroxycyclohexyl]-6-[(6-methylpyridin-3-yl)methyl]benzo[h]quinazolin-4(3H)-one , wherein the salt is selected from the group consisting of acetate , trifluoroacetate , benzenesulfonate , benzoate , camphorsulfonate , citrate , ethanesulfonate , fumarate , gluconate , glutamate , hydrobromide , hydrochloride , isethionate , lactate , maleate , malate , mandelate , methanesulfonate , mucate , nitrate , pamoate , pantothenate , phosphate , succinate , sulfate , tartrate , and para-toluenesolfonate.64. The salt according to which is selected from the group consisting of acetate claim 63 , trifluoroacetate claim 63 , fumarate claim 63 , and hydrochloride.65. The salt according to which is selected from the group consisting of fumarate claim 63 , and hydrochloride.66. A pharmaceutically acceptable salt of 3-[(1S claim 63 ,2S)-2-hydroxycyclohexyl]-6-[(6-methylpyridin-3-yl)methyl]benzo[h]quinazolin-4(3H)-one wherein the salt is selected from the group consisting of acetate claim 63 , trifluoroacetate claim 63 , benzenesulfonate claim 63 , benzoate claim 63 , camphorsulfonate claim 63 , citrate claim 63 , ethanesulfonate claim 63 , fumarate claim 63 , gluconate claim 63 , glutamate claim 63 , hydrobromide claim 63 , hydrochloride claim 63 , isethionate claim 63 , lactate claim 63 , maleate claim 63 , malate claim 63 , mandelate claim 63 , methanesulfonate claim 63 , mucate claim 63 , nitrate claim 63 , pamoate claim 63 , pantothenate claim 63 , phosphate claim 63 , succinate claim 63 , sulfate claim 63 , tartrate claim 63 , para-toluenesolfonate.67. The salt according to which is selected from the group consisting of acetate claim 66 , trifluoroacetate claim 66 , fumarate claim 66 , and hydrochloride.68. The salt according to which is selected from the group consisting of fumarate claim 66 , and hydrochloride.69. A ...

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Номер записи: 49

04-02-2016 дата публикации

ANTIMUSCARINIC COMPOUND HAVING A LOW CONTENT OF IMPURITIES

Номер: US20160031796A1

Автор: Allegrini Pietro, Attolino Emanuele, GRAZIOSI Renzo

Принадлежит: DIPHARMA FRANCIS S.R.L.

Substantially stable to degradation Fesoterodine fumarate, a process for its preparation and a process for the synthesis of specific degradation impurities of Fesoterodine fumarate are disclosed. 1. A process for the preparation of a substantially stable to degradation Fesoterodine fumarate , comprising:the salification of Fesoterodine base with fumaric acid in the presence of a solvent wherein the molar ratio between Fesoterodine base and fumaric acid is comprised between about 1:0.10 and about 1:0.88;the precipitation of Fesoterodine fumarate from the resulting solution;the recovery of the solid.2. Process according to wherein the Fesoterodine base to fumaric acid molar ratio is comprised between about 1:0.5 and about 1:0.85.4. Process according to wherein the molar ratio of the compound of formula (IV) to fumaric acid is comprised between about 1:0.4 and about 1:0.80.6. A substantially stable to degradation Fesoterodine fumarate as obtainable according to the process of .7. Fesoterodine fumarate according to claim 5 , having a total content of the impurities of formula (VI) claim 5 , (VII) (VIII) or (IX) equal to or lower than 0.1% claim 5 , and preferably comprised between about 0.1% and about 0.01% claim 5 , calculated as Area % by HPLC.8. A pharmaceutical composition comprising substantially stable to degradation Fesoterodine fumarate according to and a pharmaceutically acceptable carrier and/or excipient.9. A substantially stable to degradation Fesoterodine fumarate claim 5 , according to claim 5 , for use as a medicament claim 5 , in particular in a method of treatment of urinary incontinence in a mammal in need thereof. The invention relates to a process for the preparation of (R)-2-(3-diisopropylamino-1-phenylpropyl)-4-(hydroxymethyl)phenol isobutyrate (Fesoterodine) as fumarate salt, substantially stable as herein defined, that is Fesoterodine fumarate which substantially does not develop degradation impurities; and a method for the preparation of ...

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Номер записи: 50

02-02-2017 дата публикации

POLYMORPHIC FORMS AND CO-CRYSTALS OF A C-MET INHIBITOR

Номер: US20170029443A1

Автор: Bauer David, BIO Matthew, COOKE Melanie, COPELAND Katrina W., PETERSON Matthew, Potashman Michele, SHIMANOVICH Roman, TAN Helming

Принадлежит:

Provided herein are novel polymorphic forms and co-crystals of a compound useful in the treatment, prevention, or amelioration of cancer. In particular, the invention provides polymorphs and co-crystals of 6-{(1R)-1-[8-fluoro-6-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[4,3-a]pyridin-3-yl]ethyl}-3-(2-methoxyethoxy)-1,6-naphthyridin-5(6H)-one, which is an inhibitor of c-Met. 1. A free base form of 6-{(1R)-1-[8-fluoro-6-(1-methyl-1H-pyrazol-4-yl)[1 ,2 ,4]triazolo[4 ,3-a]pyridin-3-yl]ethyl}-3-(2-methoxyethoxy)-1 ,6-naphthyridin-5(6H)-one , wherein the free base form is selected from the group consisting of a monohydrate form , an anhydrous form , an acetone solvate form , a dimethylsulfoxide (DMSO) hemisolvate form , and an amorphous form.2. The free base form of claim 1 , wherein the free base form is the monohydrate form.3. The free base form of claim 1 , wherein the monohydrate form is crystalline.4. The free base form of claim 1 , wherein the monohydrate form is characterized by an X-ray powder diffraction pattern comprising peaks at about 6.6 claim 1 , 7.9 claim 1 , 14.5 claim 1 , 15.1 claim 1 , 15.8 and 22.2 ±0.2° 2θ using Cu Kα radiation.5. A method of preparing the free base form of claim 1 , comprising:(a) preparing a slurry comprising 6-{(1R)-1-[8-fluoro-6-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[4,3-a]pyridin-3-yl]ethyl}-3-(2-methoxyethoxy)-1,6-naphthyridin-5(6H)-one in an organic solvent that is free or substantially free of each or all of DMSO, propylene glycol, PEG 400, and acetone, wherein the slurry comprises at least about 0.25 water activity, and isolating the resulting solid; or,(b) exposing an anhydrous I form of 6-{(1R)-1-[8-fluoro-6-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[4,3-a]pyridin-3-yl]ethyl}-3-(2-methoxyethoxy)-1,6-naphthyridin-5(6H)-one to at least about 25% relative humidity.6. The free base form of claim 1 , wherein the free base form is the acetone solvate form.7. The free base form of claim 1 , wherein the acetone solvate form ...

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Номер записи: 51

01-02-2018 дата публикации

Pyridazinone and pyridone compounds

Номер: US20180029995A1

Автор: Auni Juhakoski, David Smith, Ferenc FÜLÖP, Ferenc Miklos, Istvan Szatmari, Laszlo Lazar, Lorand Kiss, Marjo Pihlavisto, Marta Palko, Zsolt Szakonyi

Принадлежит: Biotie Therapies Corp

The invention relates to pyridazinone and pyridone compounds having formula (I) or (I′), and pharmaceutically acceptable salts, hydrates, and solvates thereof wherein R 1 /R 4 and X and X 3 are as defined in the claims. The invention further relates to their use as inhibitors of copper-containing amine oxidases. The present invention also relates to the preparation of the aforementioned compounds and to pharmaceutical compositions comprising as an active ingredient(s) one or more of the aforementioned compounds, pharmaceutically acceptable salts, hydrates, or solvates thereof.

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Номер записи: 52

17-02-2022 дата публикации

FREE-POLYUNSATURATED-FATTY-ACID-CONTAINING COMPOSITION AND METHOD FOR MANUFACTURING SAME

Номер: US20220049185A1

Автор: Doisaki Nobushige, KOSUGE Yuhei, SATO Seizo, YAMAGUCHI Hideaki

Принадлежит: NIPPON SUISAN KAISHA, LTD.

Provided is a free-polyunsaturated-fatty-acid-containing composition that has a total metal content of 0.1 ppm or less and that comprises at least one free polyunsaturated fatty acid having 20 or more carbon atoms, in an amount that is at least 80.0% of the amount of fatty acids in the composition; and a method for manufacturing a free-polyunsaturated-fatty-acid-containing composition, comprising: providing a raw material composition containing at least one polyunsaturated fatty acid having 20 or more carbon atoms; performing a hydrolysis treatment on a reaction solution prepared by combining the provided raw material composition, a lower alcohol, water having a total metal content of 0.01 ppm or less, and an alkali catalyst; and limiting the contact between the reaction composition and the metal after the hydrolysis treatment so that the product T [cm×days] of the contact surface area [cm] per 1 g and the contact time [days] between the composition and the metal is 100 or less. 18-. (canceled)9. A manufacturing method of a free polyunsaturated fatty acid-containing composition , the method comprising:providing a raw material composition containing at least one polyunsaturated fatty acid having 20 or more carbons;performing hydrolysis treatment on a reaction solution prepared by combining the provided raw material composition, a lower alcohol, water having a total content of metal of 0.01 ppm or less, and an alkali catalyst; and{'sup': 2', '2, 'limiting contact between the reaction composition after the hydrolysis treatment and a metal surface such that a product T (cm×day) of a contact surface area (cm) per 1 g of the composition with the metal surface and contact time (day) becomes 100 or less.'}10. The manufacturing method according to claim 9 , wherein the product T (cm×day) of the contact surface area (cm) per 1 g of the composition with the metal surface and the contact time (day) becomes 80 or less.11. The manufacturing method according to claim 9 , wherein a ...

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Номер записи: 53

31-01-2019 дата публикации

Plant Extract Compositions for Forming Protective Coatings

Номер: US20190031590A1

Автор: Bakus, II Ronald C., Mol Camille, Perez Louis, Rodriguez Gabriel, Rogers James

Принадлежит:

Described herein are methods of preparing cutin-derived monomers, oligomers, or combinations thereof from cutin-containing plant matter. The methods can include heating the cutin-derived plant matter in a solvent at elevated temperature and pressure. In some preferred embodiments, the methods can be carried out without the use of additional acidic or basic species. 3. The method of claim 1 , further comprising adding the cutin to a solvent claim 1 , wherein the decomposing of the cutin is carried out in the solvent.4. The method of claim 3 , wherein the solvent is a nucleophilic solvent.5. The method of claim 3 , wherein the solvent comprises water claim 3 , glycerol claim 3 , methanol claim 3 , ethanol claim 3 , liquid CO claim 3 , supercritical CO claim 3 , or a combination thereof.11. The method of claim 9 , further comprising adding the cutin to a solvent claim 9 , wherein the depolymerizing of the cutin is carried out in the solvent.12. The method of claim 11 , wherein the solvent is a nucleophilic solvent.13. The method of claim 11 , wherein the solvent comprises water claim 11 , glycerol claim 11 , methanol claim 11 , ethanol claim 11 , liquid CO claim 11 , supercritical CO claim 11 , or a combination thereof.14. The method of claim 11 , wherein the decomposing of the compounds of Formula I is also carried out in the solvent.15. The method of claim 9 , further comprising modifying the compounds of Formula II claim 9 , esters thereof claim 9 , or compounds of Formula III to form a second group of compounds of Formula I.19. The method of claim 18 , further comprising adding the cutin to a solvent claim 18 , wherein the decomposing of the cutin is carried out in the solvent.20. The method of claim 19 , wherein the solvent is a nucleophilic solvent.21. The method of claim 19 , wherein the solvent comprises water claim 19 , glycerol claim 19 , methanol claim 19 , ethanol claim 19 , liquid CO claim 19 , supercritical CO claim 19 , or a combination thereof.25. The ...

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Номер записи: 54

31-01-2019 дата публикации

NOVEL ACID ADDITION SALT OF 1-(5-(2,4-DIFLUOROPHENYL)-1-((3-FLUOROPHENYL)SULFONYL)-4-METHOXY-1H-PYRROL-3-YL)-N-METHYLMETHANAMINE

Номер: US20190031609A1

Автор: Cho Kwan Hyung, Kim Aeri

Принадлежит:

The present invention provides a novel acid addition salt of 1-(5-(2,4-difluorophenyl)-1-((3-fluorophenyl)sulfonyl)-4-methoxy-1H-pyrrol-3-yl)-N-methylmethanamine. The above-described acid addition salt can have not only excellent proton pump inhibitory activity, gastric damage inhibitory activity and defensive factor-enhancing effect, but also excellent eradication activity against and thus can be effectively used for the prevention and treatment of gastrointestinal injury due to gastrointestinal track ulcer, gastritis, reflux esophagitis, or 1. An acid addition salt of 1-(5-(2 ,4-difluorophenyl)-1-((3-fluorophenyl)sulfonyl)-4-methoxy-1H-pyrrol-3-yl)-N-methylmethanamine wherein the acid is hydrochloric acid , succinic acid , tartaric acid , or fumaric acid.2. A method for preparing an acid addition salt of 1-(5-(2 claim 1 ,4-difluorophenyl)-1-((3-fluorophenyl)sulfonyl)-4-methoxy-1H-pyrrol-3-yl)-N-methylmethanamine of comprising the steps of:1) dissolving 1-(5-(2,4-difluorophenyl)-1-((3-fluorophenyl)sulfonyl)-4-methoxy-1H-pyrrol-3-yl)-N-methylmethanamine and an acid, respectively, in an organic solvent to prepare a 1-(5-(2,4-difluorophenyl)-1-((3-fluorophenyl)sulfonyl)-4-methoxy-1H-pyrrol-3-yl)-N-methylmethanamine solution and an acid solution; and2) mixing the 1-(5-(2,4-difluorophenyl)-1-((3-fluorophenyl)sulfonyl)-4-methoxy-1H-pyrrol-3-yl)-N-methylmethanamine solution and the acid solution and then stirring the mixed solutions.3. The method for preparing an acid addition salt of 1-(5-(2 claim 2 ,4-difluorophenyl)-1-((3-fluorophenyl)sulfonyl)-4-methoxy-1H-pyrrol-3-yl)-N-methylmethanamine of claim 2 ,wherein the acid is hydrochloric acid, succinic acid, tartaric acid, or fumaric acid.4. The method for preparing an acid addition salt of 1-(5-(2 claim 2 ,4-difluorophenyl)-1-((3-fluorophenyl)sulfonyl)-4-methoxy-1H-pyrrol-3-yl)-N-methyl methanamine of claim 2 ,wherein the organic solvent is one or more selected from the group consisting of n-hexane, ethyl acetate, butyl ...

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Номер записи: 55

07-02-2019 дата публикации

CHEMICAL COMPOUNDS

Номер: US20190038607A1

Автор: Akhtar Nadim, Bradbury Robert Hugh, Buttar David, Currie Gordon Stuart, De Savi Christopher, Donald Craig Samuel, Norman Richard Albert, Osborne Matthew, Rabow Alfred Arthur, Redfearn Heather, Williams Helen Elizabeth, Yavari Neda

Принадлежит: AstraZeneca AB

The invention concerns compounds of Formula (I) 1. A pharmaceutical composition comprising a compound and a pharmaceutically-acceptable diluent or carrier , wherein the compound is (E)-3-(3 ,5-difluoro-4-((1R ,3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-2 ,3 ,4 ,9-tetrahydro-1H-pyrido[3 ,4-b]indol-1-yl)phenyl)acrylic acid or a pharmaceutically-acceptable salt thereof.2. A pharmaceutical composition according to claim 1 , wherein the compound is (E)-3-(3 claim 1 ,5-difluoro-4-((1R claim 1 ,3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-2 claim 1 ,3 claim 1 ,4 claim 1 ,9-tetrahydro-1H-pyrido[3 claim 1 ,4-b]indol-1-yl)phenyl)acrylic acid.3. A pharmaceutical composition according to claim 1 , wherein the compound is the maleic acid salt of (E)-3-(3 claim 1 ,5-difluoro-4-((1R claim 1 ,3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-2 claim 1 ,3 claim 1 ,4 claim 1 ,9-tetrahydro-1H-pyrido[3 claim 1 ,4-b]indol-1-yl)phenyl)acrylic acid.4. A pharmaceutical composition according to claim 1 , wherein the pharmaceutical composition contains less than 5% w/w of (R claim 1 ,E)-3-(3 claim 1 ,5-difluoro-4-(2-(2-fluoro-2-methylpropyl)-3-methyl-4 claim 1 ,9-dihydro-3H-pyrido[3 claim 1 ,4-b]indol-2-ium-1-yl)phenyl)acrylate.5. A pharmaceutical composition according to claim 1 , wherein the pharmaceutical composition further comprises an anti-oxidant and optionally further comprises a metal-chelating agent.7. A method according to claim 6 , wherein the compound of Formula (I) is (E)-3-(3 claim 6 ,5-difluoro-4-((1R claim 6 ,3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-2 claim 6 ,3 claim 6 ,4 claim 6 ,9-tetrahydro-1H-pyrido[3 claim 6 ,4-b]indol-1-yl)phenyl)acrylic acid.8. A method according to claim 7 , wherein Ris methyl.9. (E)-methyl 3-(3 claim 7 ,5-difluoro-4-((1R claim 7 ,3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-2 claim 7 ,3 claim 7 ,4 claim 7 ,9-tetrahydro-1H-pyrido[3 claim 7 ,4-b]indol-1-yl)phenyl)acrylate.11. A method according to claim 10 , wherein the compound of Formula (II) is (E)-methyl 3-(3 claim ...

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Номер записи: 56

07-02-2019 дата публикации

FATTY ACID COMPOUND, PREPARATION METHOD THEREFOR AND USE THEREFOR

Номер: US20190039989A1

Автор: GUO Dongdong, Li Jia, Li Jingya, Nan Fajun, Wang Jingtao, XIE Zhifu, Zhang Mei

Принадлежит:

The present invention relates to a class of fatty acid compounds, a preparation method thereof and use thereof. The fatty acid compounds have the structure of the formula I, which has the ability to activate APMK and inhibit the glucose output in mouse primary hepatocytes. The fatty acid compounds can be used in preparing a medicament for the treatment of obesity or diabetes. 2. The fatty acid compound represented by following formula I according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein:{'sub': 1', '2', '3', '4', '5', '6, 'R, R, R, R, R, and Rare each independently H, C1˜C3 alkyl, C3˜C6 cycloalkyl, C3˜C6 cycloalkenyl, or phenyl,'}{'sub': 1', '2, 'alternatively, Rand Rtogether with their adjacent carbon atoms forth a C3-C7 cycloalkyl group, or together with their adjacent carbon atoms form a C3-C7 cycloalkenyl group;'}{'sub': 3', '4, 'alternatively, Rand Rtogether with their adjacent carbon atoms form a C3˜C7 cycloalkyl group, or together with their adjacent carbon atoms form a C3˜C7 cycloalkenyl group;'}{'sub': 5', '6, 'alternatively, Rand Rtogether with their adjacent carbon atoms form a C3˜C7 cycloalkyl group, or together with their adjacent carbon atoms form a C3˜C7 cycloalkenyl group,'}m, n are each independently 2, 3, 4 or 5,{'sub': 1', '2, 'Yand Yare each independently —COOH;'}{'img': {'@id': 'CUSTOM-CHARACTER-00003', '@he': '2.12mm', '@wi': '3.89mm', '@file': 'US20190039989A1-20190207-P00001.TIF', '@alt': 'custom-character', '@img-content': 'character', '@img-format': 'tif'}, 'represents a double bond or a single bond,'}the double bond is either cis or trans.13. A method for treating obesity or diabetes claim 1 , comprising the step of{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'administering to a subject in need of such treatment an effective amount of the fatty acid compound or pharmaceutically acceptable salts thereof according to .'}14. A pharmaceutical composition for treating obesity or diabetes claim 1 , ...

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Номер записи: 57

07-02-2019 дата публикации

TRIAZOLE DERIVATIVES OF MELAMPOMAGNOLIDE B AND METHODS OF USE THEREOF

Номер: US20190040077A1

Автор: Crooks Peter, Janganati Venumadhav, Jordan Craig, Ponder Jessica

Принадлежит:

The present disclosure relates to triazole derivatives of melampomagnolide B, their synthesis, and their use as anti-cancer compounds. 2. The compound of claim 1 , wherein R is selected from the group consisting of a simple or substituted phenyl claim 1 , a simple or substituted heterocycle claim 1 , and a simple or substituted alkyl.5. The compound of claim 4 , wherein R claim 4 , R claim 4 , R claim 4 , R claim 4 , and Rare each independently selected from the group consisting of hydrogen claim 4 , alkyl claim 4 , substituted alkyl claim 4 , alkynyl claim 4 , methyl claim 4 , trifluoromethyl claim 4 , halogen claim 4 , cyano claim 4 , nitro claim 4 , amidine claim 4 , amino claim 4 , carboxyl claim 4 , ester claim 4 , alkylalkylamino claim 4 , dialkylamino claim 4 , hydroxyl claim 4 , alkoxy or arylalkoxy (e.g. methoxy claim 4 , ethoxy claim 4 , benzyloxy claim 4 , substituted benzyloxy) and combinations thereof.6. The compound of claim 4 , wherein R claim 4 , R claim 4 , R claim 4 , R claim 4 , and Rare each independently selected from the group consisting of hydrogen claim 4 , alkynyl claim 4 , methyl claim 4 , trifluoromethyl claim 4 , halogen claim 4 , amino claim 4 , carboxyl claim 4 , ester claim 4 , hydroxyl claim 4 , alkoxy (e.g. methoxy claim 4 , ethoxy) and combinations thereof.7. (canceled)8. (canceled)9. (canceled)10. (canceled)11. A method of making the compound comprising Formula (I) claim 4 , the method comprising contacting an azido derivative of melampomagnolide B with an acetylenic compound in the presence of copper catalyst claim 4 , a proton acceptor and a solvent to afford a compound of Formula (I).12. (canceled)13. (canceled)14. The method of claim 11 , wherein the acetylenic compound comprises Formula (III):{'br': None, '≡R'}wherein R is selected from the group consisting of hydrocarbyl, substituted hydrocarbyl, alkyl, substituted alkyl, cycloalkyl, substituted cycloalkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, aryl, ...

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Номер записи: 58

06-02-2020 дата публикации

NICOTINE SALTS, CO-CRYSTALS, AND SALT CO-CRYSTAL COMPLEXES

Номер: US20200039954A1

Автор: Carr Andrew, Dull Gary M., Sharp Emma

Принадлежит:

The invention provides certain nicotine salts, co-crystals, and salt co-crystals and provides novel polymorphic forms of certain nicotine salts. In particular, nicotine salts with orotic acid are described. The invention further provides methods of preparation and characterization of such nicotine salts. In addition, tobacco products, including smoking articles, smokeless tobacco products, and electronic smoking articles comprising nicotine salts, co-crystals, and/or salt co-crystals are also provided. 1. A salt or salt-co-crystal of nicotine and orotic acid.2. The salt or salt-co-crystal of claim 1 , wherein the salt-co-crystal is a bis-orotic acid salt-co-crystal.3. The salt or salt-co-crystal of claim 2 , wherein the bis-orotic acid salt-co-crystal is in hemihydrate form.4. The salt or salt-co-crystal of claim 1 , wherein the salt is a mono-orotic acid salt.5. The salt or salt-co-crystal of claim 1 , wherein at least about 50% of the salt or salt-co-crystal is in crystalline form.6. The salt or salt-co-crystal of claim 1 , characterized by an X-ray powder diffraction pattern having peaks at one or more of the following 2-theta diffraction angles: 8.8 claim 1 , 13.4 claim 1 , 17.7 claim 1 , 26.5 claim 1 , and 29.3.7. The salt or salt-co-crystal of claim 1 , characterized by an X-ray powder diffraction pattern having peaks at one or more of the following 2-theta diffraction angles: 9.1 claim 1 , 14.7 claim 1 , 15.4 claim 1 , 17.3 claim 1 , 25.0 claim 1 , 25.4 claim 1 , and 27.0.8. An electronic smoking article comprising an inhalable substance medium contained within a cartridge body and a heating member positioned to provide heat to at least a portion of the inhalable substance medium claim 1 , wherein the inhalable substance medium comprises nicotine fumarate or the salt or salt-co-crystal of nicotine and orotic acid of .9. The electronic smoking article of claim 8 , wherein the inhalable substance medium further comprises one or more of glycerin claim 8 , water ...

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Номер записи: 59

06-02-2020 дата публикации

WATER-SOLUBLE UNIT DOSE ARTICLES MADE FROM A COMBINATION OF DIFFERENT FILMS

Номер: US20200040288A1

Автор: COURCHAY Florence Catherine, Friedrich Steven G., KEULEERS Robby Renilde Francois, LABEQUE Regine, Lee David M., Nii Shinsuke, Renmans Marc Rene Bert, Souter Philip Frank, Yeung Lee K.

Принадлежит:

The present disclosure relates to pouches made from a combination of chemically different water-soluble films and optionally containing a composition (e.g. a household care composition or non-household care composition) that is at least partially enclosed by the water-soluble films in at least one compartment. 153-. (canceled)54. A water-soluble unit dose article comprising at least one sealed compartment optionally comprising at least one composition contained in the article , the water-soluble unit dose article comprisinga first water soluble film comprising a PVOH polymer comprising a first anionic content;and a second water soluble film comprising a PVOH polymer comprising a second anionic content;wherein the first anionic content is in a range of about 0.5 mol % to about 10 mol % of total PVOH polymer in the first water soluble film and the second anionic content is in a range of about 0 mol % to about 5 mol % of total PVOH polymer in the second water soluble film, and the difference between the first anionic content and second anionic content is about 0.05 mol % to about 4 mol %, wherein the anionic content of each film is the molar percentage of anionic monomer units present in the total PVOH polymer of the film, and wherein the first water-soluble film is chemically different from the second water soluble film with respect to the anionic content of the PVOH polymers of the films;wherein the first film is sealed to the second film to form the at least one sealed compartment;provided that when the composition is a fabric care or household care composition and a film comprises a blend of a polyvinyl alcohol homopolymer resin and an anionic polyvinyl alcohol copolymer resin, then both then first water soluble film and the second water soluble film comprise blends that include 65 wt. % or greater of an anionic polyvinyl alcohol copolymer resin, based on the total weight of polyvinyl alcohol resins in the blend; andprovided that when the composition is a fabric ...

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Номер записи: 60

18-02-2021 дата публикации

Synthesis and purification of muconic acid ester from aldaric acid esters

Номер: US20210047260A1

Автор: Anneloes Berghuis, David Thomas, Juha Linnekoski, Martta Asikainen, Nicolaas Van Strien

Принадлежит: Valtion teknillinen tutkimuskeskus

According to an example aspect of the present invention, there is provided a method for producing muconic acid ester from aldaric acid ester, and for separating and purifying the produced muconic acid ester by high vacuum distillation in a total heating environment.

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Номер записи: 61

18-02-2016 дата публикации

SALT OF PYRAZOLOQUINOLINE DERIVATIVE, AND CRYSTAL THEREOF

Номер: US20160046623A1

Автор: Ozaki Shunsuke

Принадлежит:

The present invention provides a salt of (S)-7-(2-methoxy-3,5-dimethylpyridin-4-yl)-1-(tetrahydrofuran-3-yl)-1H-pyrazolo[4,3-c]quinolin-4(5H)-one and an acid selected from the group consisting of hydrochloric acid, hydrobromic acid, sulfuric acid, nitric acid, phosphoric acid, malonic acid, maleic acid, tartaric acid, methanesulfonic acid, benzenesulfonic acid and toluenesulfonic acid; or a crystal thereof with a potential to be used as drug substance in pharmaceuticals. 1. A salt of (S)-7-(2-methoxy-3 ,5-dimethylpyridin-4-yl)-1-(tetrahydrofuran-3-yl)-1H-pyrazolo[4 ,3-c]quinolin-4(5H)-one and an acid selected from the group consisting of hydrochloric acid , hydrobromic acid , sulfuric acid , nitric acid , phosphoric acid , malonic acid , maleic acid , tartaric acid , methanesulfonic acid , benzenesulfonic acid and toluenesulfonic acid.2. (S)-7-(2-methoxy-3 claim 1 ,5-dimethylpyridin-4-yl)-1-(tetrahydrofuran-3-yl)-1H-pyrazolo[4 claim 1 ,3-c]quinolin-4(5H)-one monomaleate salt according to .3. (S)-7-(2-methoxy-3 claim 1 ,5-dimethylpyridin-4-yl)-1-(tetrahydrofuran-3-yl)-1H-pyrazolo[4 claim 1 ,3-c]quinolin-4(5H)-one monobenzenesulfonate salt according to .4. A crystal of the salt according to .5. A crystal of (S)-7-(2-methoxy-3 claim 4 ,5-dimethylpyridin-4-yl)-1-(tetrahydrofuran-3-yl)-1H-pyrazolo[4 claim 4 ,3-c]quinolin-4(5H)-one monomaleate salt according to claim 4 , having a diffraction peak at a diffraction angle (2θ±0.2°) of 10.1° in powder X-ray diffraction.6. A crystal of (S)-7-(2-methoxy-3 claim 4 ,5-dimethylpyridin-4-yl)-1-(tetrahydrofuran-3-yl)-1H-pyrazolo[4 claim 4 ,3-c]quinolin-4(5H)-one monobenzenesulfonate salt according to claim 4 , having a diffraction peak at a diffraction angle (2θ±0.2°) of 9.9° in powder X-ray diffraction.7. A pharmaceutical composition comprising the salt according to as an active ingredient.8. The crystal of (S)-7-(2-methoxy-3 claim 5 ,5-dimethylpyridin-4-yl)-1-(tetrahydrofuran-3-yl)-1H-pyrazolo[4 claim 5 ,3-c]quinolin-4(5H)-one ...

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Номер записи: 62

16-02-2017 дата публикации

SALT COMPOUND

Номер: US20170044118A1

Автор: Bender Robert, Chau Ho-Lun Joseph, Cowart Doug

Принадлежит:

A salt compound, and methods for mitigating neurodegeneration, effecting, neuroprotection and/or effecting cognition enhancement in a subject using the salt compound are described. Neurological or cognitive conditions are treated by administering to a subject an effective amount of a therapeutic salt compound comprising, a nitrate ester. 4. The dry tablet of claim 3 , formulated for oral administration.5. A method for inhibiting neurodegeneration claim 1 , or effecting neuroprotection in a subject in need thereof claim 1 , said method comprising administering to said subject an effective amount of a composition of claim 1 , such that said neurodegeneration is inhibited or said neuroprotection is effected.6. The method of claim 5 , wherein administering the therapeutic compound to said subject modulates levels of cyclic nucleotide cGMP and/or cAMP.7. The method of claim 5 , wherein said neurodegeneration or said neuroprotection is associated with a condition selected from the group consisting of stroke claim 5 , Parkinson's disease claim 5 , Alzheimer's disease claim 5 , Huntington's disease claim 5 , multiple sclerosis claim 5 , amyotrophic lateral sclerosis claim 5 , AIDS-induced dementia claim 5 , epilepsy claim 5 , alcoholism claim 5 , alcohol withdrawal claim 5 , drug-induced seizure claim 5 , viral/bacterial/fever-induced seizure claim 5 , trauma to the head claim 5 , hypoglycemia claim 5 , hypoxia claim 5 , myocardial infarction claim 5 , cerebral vascular occlusion claim 5 , cerebral vascular hemorrhage claim 5 , hemorrhage claim 5 , an environmental excitotoxin claim 5 , dementia claim 5 , trauma claim 5 , drug-induced brain damage claim 5 , and aging.8. The method of claim 5 , wherein said neurodegeneration or said neuroprotection is associated with dementia.9. The method of claim 5 , wherein said neurodegeneration or said neuroprotection is associated with Alzheimer's disease.10. The method of claim 5 , wherein said composition inhibits dementia.11. The ...

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Номер записи: 63

15-02-2018 дата публикации

CRYSTALLINE FORM OF A JAK3 KINASE INHIBITOR

Номер: US20180044336A1

Автор: Holland Joanne

Принадлежит:

The invention relates to novel co-crystals of a drug substance and their use to treat respiratory diseases such as asthma and COPD. 1. A co-crystal of (S)-3-(3-(1-methyl-2-oxo-5-(pyrazolo[1 ,5-a]pyridine-3-yl)-1H-imidazo[4 ,5-b]pyridine-3(2H)-yl)piperidin-1-yl)-3-oxopropanenitrile.2. A 1:1 co-crystal of (S)-3-(3-(1-methyl-2-oxo-5-(pyrazolo[1 ,5-a]pyridine-3-yl)-1H-imidazo[4 ,5-b]pyridine-3(2H)-yl)piperidin-1-yl)-3-oxopropanenitrile with maleic acid.3. A co-crystal according to having an X-ray powder diffraction pattern which shows the following diffraction angles (2Theta) using copper Kα radiation:at approximately 8.4°;at approximately 8.8°;at approximately 11.5°;at approximately 16.2°;at approximately 18.6°;at approximately 21.6°;at approximately 23.9°; andat approximately 25.9°.4. A co-crystal according to having a single endotherm with an onset temperature of 166.2° C. and a peak maximum of 181.4° C.5. A 1:1 co-crystal of (S)-3-(3-(1-methyl-2-oxo-5-(pyrazolo[1 claim 3 ,5-a]pyridine-3-yl)-1H-imidazo[4 claim 3 ,5-b]pyridine-3(2H)-yl)piperidin-1-yl)-3-oxopropanenitrile with gentisic acid.6. A co-crystal according to having an X-ray powder diffraction pattern which shows the following diffraction angles (2Theta) using copper Kα radiation:at approximately 7.1°;at approximately 8.9°;at approximately 14.3°;at approximately 16.3°;at approximately 18.0°;at approximately 21.7°;at approximately 25.8°; andat approximately 28.2°.7. A 2:1 co-crystal of (S)-3-(3-(1-methyl-2-oxo-5-(pyrazolo[1 claim 4 ,5-a]pyridine-3-yl)-1H-imidazo[4 claim 4 ,5-b]pyridine-3(2H)-yl)piperidin-1-yl)-3-oxopropanenitrile with adipic acid.8. A co-crystal according to having an X-ray powder diffraction pattern which shows the following diffraction angles (2Theta) using copper Kα radiation:at approximately 4.6°;at approximately 9.3°;at approximately 10.7°;at approximately 14.3°;at approximately 15.5°;at approximately 17.2°;at approximately 18.5°; andat approximately 22.4°.910-. (canceled)11. A ...

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Номер записи: 64

13-02-2020 дата публикации

SOLID STATE FORMS OF VALBENAZINE

Номер: US20200048244A1

Автор: Azran Sagit, Enav Jonathan, Erlich Motti, Kisin-Finfer Einat, Machtey Victoria, Masarwa Abed, Mittelman Ariel, Nidam Tamar, PIRAN Maytal, Sella-Erez Rotem, Shachan-Tov Sharona, Yarovoy Marina

Принадлежит:

Solid state forms of Valbenazine, Valbenazine salts, processes for preparation thereof and pharmaceutical compositions thereof are disclosed. Processes for the preparation of Valbenazine and intermediates in the preparation thereof are further described. 1. A solid state form of Valbenazine ditosylate selected from: (i) an XRPD pattern having peaks at 6.4, 8.0, 10.9, 15.9 and 22.4 degrees 2-theta±0.2 degrees 2-theta;', {'figref': {'@idref': 'DRAWINGS', 'FIG. 15'}, '(ii) an XRPD pattern as depicted in ;'}, {'sup': '13', '(iii) a solid state C-NMR spectrum with peaks at 168.9, 165.5, 147.2, 106.0 and 75.6 ppm±0.2 ppm;'}, {'sup': '13', '(iv) a solid state C-NMR spectrum having the following chemical shift absolute differences from a peak at 53.0±1 ppm of 115.9, 112.5, 94.2, 53.0 and 22.6±0.1 ppm;'}, {'sup': '13', 'figref': {'@idref': 'DRAWINGS', 'FIG. 23'}, '(v) a solid state C-NMR spectrum substantially as depicted in ; and combinations of any of (i)-(v);'}], '(A) crystalline form T10, which is characterized by data selected from one or more of the followingor (i) an XRPD pattern having peaks at 6.4, 7.6, 12.3, 15.2 and 24.9 degrees 2-theta±0.2 degrees 2-theta;', {'figref': {'@idref': 'DRAWINGS', 'FIG. 16'}, '(ii) an XRPD pattern as depicted in ;'}, {'sup': '13', '(iii) a solid state C-NMR spectrum with peaks at 166.4, 148.1, 126.9, 109.5 and 73.1 ppm±0.2 ppm;'}, {'sup': '13', '(iv) a solid state C-NMR spectrum having the following chemical shift absolute differences from a peak at 54.5±1 ppm of 111.9, 93.6, 72.4, 55.0 and 18.6±0.1 ppm;'}, {'sup': '13', 'figref': {'@idref': 'DRAWINGS', 'FIG. 25'}, '(v) a solid state C-NMR spectrum substantially as depicted in ; and combinations of any of (i)-(v).'}], '(B) crystalline form T12, which is characterized by data selected from one or more of the following2. The crystalline form T10 of Valbenazine ditosylate according to claim 1 , which is characterized by data selected from one or more of the following:(i) an XRPD pattern ...

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Номер записи: 65

23-02-2017 дата публикации

CERTAIN CHEMICAL ENTITIES, COMPOSITIONS, AND METHODS

Номер: US20170050936A1

Автор: Qian Xiangping, Zhu Yong-Liang

Принадлежит:

Chemical entities that are effective as kinase inhibitors, pharmaceutical compositions and methods of treatment are disclosed. The chemical entities disclosed specifically inhibit signal transduction and cellular proliferation by modulating the activity of protein kinases to regulate and modulate abnormal or inappropriate cell proliferation, differentiation, or metabolism. The compounds include a pyrido[3,2-d]pyrimidine scaffold substituted with aromatic and heteroaromatic moieties. 3. (canceled)5. (canceled)8. (canceled)9. (canceled)10. The compound or pharmaceutically acceptable salt of claim 1 , wherein m is 1 claim 1 , 2 claim 1 , or 3; and at least one Q is E.11. The compound or pharmaceutically acceptable salt of claim 1 , wherein n is 1 and Z is optionally substituted heterocycloalkyl.12. The compound or pharmaceutically acceptable salt of claim 11 , wherein Z is optionally substituted piperazinyl.13. (canceled)17. The compound or pharmaceutically acceptable salt of claim 16 , wherein Ris hydrogen claim 16 , cyano claim 16 , halo claim 16 , hydroxy claim 16 , —CONH claim 16 , optionally substituted alkoxy claim 16 , or optionally substituted cycloalkyloxy.18. (canceled)19. The compound or pharmaceutically acceptable salt of claim 16 , wherein R claim 16 , R claim 16 , and Rare independently hydrogen claim 16 , cyano claim 16 , halo claim 16 , hydroxy claim 16 , carboxy claim 16 , optionally substituted alkoxy claim 16 , optionally substituted lower alkyl claim 16 , optionally substituted heterocycloalkyl claim 16 , optionally substituted aryl claim 16 , optionally substituted heteroaryl claim 16 , optionally substituted amino claim 16 , optionally substituted acyl claim 16 , optionally substituted alkoxycarbonyl claim 16 , or optionally substituted aminocarbonyl.20. (canceled)21. The compound or pharmaceutically acceptable salt of claim 19 , wherein Rand Rare hydrogen claim 19 , and Ris optionally substituted morpholinyl claim 19 , optionally substituted ...

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Номер записи: 66

26-02-2015 дата публикации

Synthesis of Triethylenetetramines

Номер: US20150057466A1

Автор: Antonio Soi, Günther Schmidt, Irene Vaulont, Marco Jonas

Принадлежит: PHILERA NEW ZEALAND Ltd

Methods and intermediates for synthesizing triethylenetetramine and salts thereof, as well as novel triethylenetetramine salts and their crystal structure, and triethylenetetramine salts of high purity.

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Номер записи: 67

01-03-2018 дата публикации

IONIC LIQUID FOR FORWARD OSMOSIS PROCESS AND FORWARD OSMOSIS PROCESS

Номер: US20180056241A1

Автор: CHANG Min-Chao, CHUNG Li-Ching, FANG Chih-Hsiang, HO Chia-Hua, HORNG Ren-Yang, HUANG Meng-Shun, LIANG Teh-Ming, LIU Po-I, SHAO Hsin, YANG Tsui Jung

Принадлежит: INDUSTRIAL TECHNOLOGY RESEARCH INSTITUTE

A forward osmosis process is provided, which includes separating a feed part and a draw solution part by a semi-permeable film. An ionic liquid is introduced into the draw solution part, and brine is introduced into the feed part. The brine has an osmotic pressure lower than that of the ionic liquid, so that pure water of the brine permeates through the semi-permeable film, enters the draw solution part, and mixes with the ionic liquid to form a draw solution. The draw solution was obtained out of the draw solution part to be left to stand at room temperature, so that the draw solution separated into a water layer and an ionic liquid layer. The ionic liquid includes 14-. (canceled)68-. (canceled)10. (canceled)12. (canceled)13. The forward osmosis process as claimed in claim 5 , further comprising introducing the ionic liquid layer into the draw solution part after the step of separating the draw solution into the water layer and the ionic liquid layer14. The forward osmosis process as claimed in claim 5 , wherein the step of introducing the brine into the feed part is continuously introducing seawater into the feed part.15. The forward osmosis process as claimed in claim 5 , further comprising a step of stirring the pure water and the ionic liquid in the draw solution part for mixing the pure water and the ionic liquid to form the draw solution. This application claims the benefit of U.S. Provisional Application No. 62/381,187 filed on Aug. 30, 2016, and claims priority from Taiwan Application Serial Number 105139655 filed on Dec. 1, 2016, the entirety of which are incorporated by reference herein.The technical field relates to a draw solute (ionic liquid) for a forward osmosis process.The technical principle of forward osmosis (FO) desalination process utilizes an osmosis pressure difference (between two solutions/solutes in two parts separated by a semi-permeable film) as a driving force. Water in a feed part with a lower osmosis pressure will permeate through a ...

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Номер записи: 68

02-03-2017 дата публикации

PHARMACEUTICALLY ACCEPTABLE SALTS OF beta-GUANIDINOPROPIONIC ACID WITH IMPROVED PROPERTIES AND USES THEREOF

Номер: US20170056352A1

Автор: Andreas G. GRILL, Aniruddh Singh, Eduardo J. Martinez, Padmini Kavuru

Принадлежит: Rgenix Inc

The present invention relates to new pharmaceutical salts of β-GPA which exhibit improved physical properties. In particular, the invention relates to salts of β-GPA with improved flow properties (e.g., improved Carr's index and/or Hausner ratio) such as fumarate salts, succinate salts, and oxalate salts. The invention also relates to pharmaceutical compositions including a pharmaceutically effective amount of one or more salts of β-GPA, as well as methods of treating cancer including administration of a formulation including a β-GPA salt of the invention to a subject in need thereof.

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Номер записи: 69

04-03-2021 дата публикации

Synthetic Nicotine Composition

Номер: US20210061783A1

Автор: Cao Yinghui, Chen Yuefeng, Chen Zheng, HUANG Zhennan, WANG Songfeng, YAN Ningning, YUAN Shenghong, Zhang Yong

Принадлежит:

A synthetic nicotine composition comprising synthetic nicotine, a synthetic nicotine salt and a synthetic nicotine derivative, wherein the synthetic nicotine, the synthetic nicotine salt, and the synthetic nicotine derivative are in mass percentage; the synthetic nicotine accounts for 1-20%, the synthetic nicotine salt accounts for 30-70%, and the synthetic nicotine derivative accounts for 20-50%; and the synthetic nicotine is one or more of S-nicotine and a mixture of R-nicotine containing a racemate and S-nicotine. The synthetic nicotine, synthetic nicotine salt and synthetic nicotine derivative according to the present invention are proportionally mixed to prepare an existing synthetic nicotine product, which relieves the problem of the impact of impurities in natural extracted nicotine products causing an unpleasant smell, a bitter taste and a strong volatility, and can be used in the fields of low temperature heat-not-burn products, snuff, electronic cigarettes, nicotine release patches, insecticides, herbicides, microbicides, drug synthesis, etc. 1. A synthetic nicotine composition comprising synthetic nicotine , a synthetic nicotine salt and a synthetic nicotine derivative , wherein the synthetic nicotine , the synthetic nicotine salt , and the synthetic nicotine derivative are in mass percentage; the synthetic nicotine accounts for 1-20% , the synthetic nicotine salt accounts for 30-70% , and the synthetic nicotine derivative accounts for 20-50%; the synthetic nicotine is one or more of S-nicotine and a mixture of R-nicotine containing a racemate and S-nicotine; the synthetic nicotine salt is formed by reacting the synthetic nicotine with an organic acid mixture; and the nicotine derivative comprises one or more of an imidazole derivative of nicotine , an amine derivative of nicotine , and an amino acid derivative of nicotine.2. The synthetic nicotine composition according to claim 1 , wherein the synthesis organic acid mixture for the synthetic nicotine ...

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Номер записи: 70

05-03-2015 дата публикации

SALTS OF 5-[(1R)-2-(AMINO)-1-HYDROXYETHYL]-8-HYDROXYQUINOLIN-2(1H)-ONE

Номер: US20150065471A1

Автор: Carrera Carrera Francesc, Marchueta Hereu Iolanda, Moyes Valles Enrique, Pérez Garcia Juan Bautista, Puig Duran Carlos

Принадлежит:

The present invention is directed to a pharmaceutically acceptable crystalline addition salt of 5-[(1R)-2-({2-[4-({4-(2,2-difluoro-2-phenylethoxy)phenyl]ethyl}amino)-1-hydroxyethyl]-8-hydroxyquinolin-2(1H)-one, and (ii) a dicarboxylic acid, a sulfonic acid or a sulfimide, or a pharmaceutically acceptable solvate thereof. 1. A pharmaceutically acceptable crystalline addition salt of (i) 5-[(1R)-2-({2-[4-(2 ,2-difluoro-2-phenylethoxy)phenyl]ethyl}amino)-1-hydroxyethyl]-8-hydroxyquinolin-2(1H)-one , and (ii) a dicarboxylic acid , a sulfonic acid or a sulfimide , or a pharmaceutically acceptable solvate thereof.2. [[A]]The salt according to claim 1 , wherein (ii) is a dicarboxylic acid.3. The salt according to claim 2 , chosen from:5-[(1R)-2-({2-[4-(2,2-difluoro-2-phenylethoxy)phenyl]ethyl}amino)-1-hydroxyethyl]-8-hydroxyquinolin-2(1H)-one fumarate; or5-[(1R)-2-({2-[4-(2,2-difluoro-2-phenylethoxy)phenyl]ethyl}amino)-1-hydroxyethyl]-8-hydroxyquinolin-2(1H)-one succinate,or pharmaceutically acceptable solvate thereof.4. The salt according to claim 3 , wherein the salt is 5-[(1R)-2-({2-[4-(2 claim 3 ,2-difluoro-2-phenylethoxy)phenyl]ethyl}amino)-1-hydroxyethyl]-8-hydroxyquinolin-2(1H)-one fumarate or phar aceutically acceptable solvate thereof.5. The salt according to claim 1 , wherein (ii) is a sulfonic acid or a sulfirnide.6. The salt according to claim 5 , chosen from:5-[(1R)-2-({2-[4-(2,2-difluoro-2-phenylethoxy)phenyl]ethyl}amino)-1-hydroxyethyl]-8-hydroxyquinolin-2(1H)-one methanesulphonate; or5-[(1R)-2-({2-[4-(2,2-difluoro-2-phenylethoxy)phenyl]ethyl}amino)-1-hydroxyethyl]-8-hydroxyquinolin-2(1H)-one saccharinate,or pharmaceutically acceptable solvate thereof.7. A pharmaceutical composition comprising a therapeutically effective amount of a salt according to and a pharmaceutically acceptable carrier.8. The pharmaceutical composition according to claim 7 , wherein the pharmaceutical composition is formulated for administration by inhalation as a dry powder.9. The ...

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Номер записи: 71

22-05-2014 дата публикации

STABLE MICRONISED MONOCLINIC FORM OF ASENAPINE MALEATE AND ITS SYNTHESIS

Номер: US20140142158A1

Автор: Bertran Agustì, Terradas Josep

Принадлежит: LABORATORIOS LESVI S.L.

A stable micronised monoclinic form of asenapine maleate is described, which comprises 5% by weight or less of orthorhombic form or any other crystalline form of asenapine maleate, wherein the asenapine maleate has a particle size distribution characterised by a d90 equal to or below 40 μm. Processes for preparing the stable micronised monoclinic form of asenapine maleate are also described. Formula (I). 1. A stable micronised monoclinic form of asenapine maleate , which comprises 5% by weight or less of orthorhombic form or any other crystalline form of asenapine maleate , wherein the asenapine maleate has a particle size distribution characterised by a d90 equal to or below 40 μm , which remains polymorphically stable after 3 months of storage.2. A stable micronised monoclinic form of asenapine maleate according to claim 1 , which comprises 2% by weight or less of orthorhombic form or any other crystalline form of asenapine maleate.3. A stable micronised monoclinic form of asenapine maleate according to having a particle size distribution characterised by a d90 of 30 μm or below.4. A stable micronised monoclinic form of asenapine maleate according to having a particle size distribution characterised by a d90 of 10 μm or below.5. A stable micronised monoclinic form of asenapine maleate according to claim 1 , which comprises 1% by weight or less of any other crystalline form of asenapine maleate.6. (canceled)7. A process for the preparation of a stable micronised monoclinic form of asenapine maleate according to claim 1 , the process comprising the micronisation of monoclinic asenapine maleate wherein the applied micronisation pressure is below 7 bar and the micronisation temperature is 10° C. or below.8. A process according to wherein the applied micronisation pressure is 5 bar or below and the micronisation temperature is −10° C. or below.9. A process according to wherein the applied micronisation pressure is 3 bar or below and the micronisation temperature is −10 ...

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Номер записи: 72

27-02-2020 дата публикации

SOLID FORMS OF AN ASK1 INHIBITOR

Номер: US20200061042A1

Автор: Andres Mark, Burke Chan Brenda J., Carra Ernest A., Chiu Anna, Lapina Olga Viktorovna, Lathrop Stephen P., Notte Gregory, Smolenskaya Valeriya, Yu Lok Him

Принадлежит:

Crystalline forms of 5-(4-cyclopropyl-1H-imidazol-1-yl)-N-(6-(4-isopropyl-4H-1,2,4-triazol-3-yl)pyridin-2-yl)-2-fluoro-4-methylbenzamide (Compound I) were prepared and characterized in the solid state: 191.-. (canceled)92. A method of treating chronic kidney disease in a patient in need thereof comprising administering a therapeutically effective amount of crystalline 5-(4-cyclopropyl-1 H-imidazol-1-yl)-N-(6-(4-isopropyl-4H-1 ,2 ,4-triazol-3-yl)pyridin-2-yl)-2-fluoro-4-methylbenzamide (Compound I Form I) characterized by an X-ray powder diffractogram comprising the following peaks: 16.7 , 21.3 , and 22.8° 2θ±0.2° 2θ , as determined on a diffractometer using Cu-Kα radiation at a wavelength of 1.5406 Å.93. The method of claim 92 , further comprising administering another therapeutic agent.94. The method of claim 93 , wherein the additional therapeutic agent is filgotinib.96. A method of treating diabetic kidney disease in a patient in need thereof comprising administering a therapeutically effective amount of crystalline 5-(4-cyclopropyl-1 H-imidazol-1-yl)-N-(6-(4-isopropyl-4H-1 claim 93 ,2 claim 93 ,4-triazol-3-yl)pyridin-2-yl)-2-fluoro-4-methylbenzamide (Compound I Form I) characterized by an X-ray powder diffractogram comprising the following peaks: 16.7 claim 93 , 21.3 claim 93 , and 22.8° 2θ±0.2° 2θ claim 93 , as determined on a diffractometer using Cu-Kα radiation at a wavelength of 1.5406 Å.97. The method of claim 96 , further comprising administering another therapeutic agent.98. The method of claim 97 , wherein the additional therapeutic agent is filgotinib. This application is a continuation of U.S. application Ser. No. 16/221,249, filed Dec. 14, 2018, which is a continuation of U.S. application Ser. No. 15/873,568, filed Jan. 17, 2018, now abandoned, which is a continuation of U.S. application Ser. No. 15/481,365, filed Apr. 6, 2017, now U.S. Pat. No. 9,907,790, which is a divisional of U.S. application Ser. No. 14/757,585, filed Dec. 22, 2015, now U.S. Pat ...

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Номер записи: 73

15-03-2018 дата публикации

CO-CRYSTALS OF IBRUTINIB WITH CARBOXYLIC ACIDS

Номер: US20180072737A1

Автор: Albrecht Wolfgang, Geier Jens, Perez Palacios David, RABE Sebastian

Принадлежит: ratiopharm GmbH

The present invention relates to co-crystals of ibrutinib, a pharmaceutical composition comprising the same as well as a method of preparing the same. 1. A co-crystal of ibrutinib and carboxylic acid.2. The co-crystal of ibrutinib according to claim 1 , wherein the co-crystal of ibrutinib is ibrutinib benzoic acid.3. The co-crystal of ibrutinib according to claim 2 , wherein said co-crystal has characteristic X-ray powder diffraction peaks at 9.1 claim 2 , 12.1 claim 2 , 13.7 claim 2 , 13.9 and 23.0 degrees 2-theta ±0.2 degrees 2-theta.4. The co-crystal of ibrutinib according to claim 1 , wherein the co-crystal of ibrutinib is ibrutinib fumaric acid.5. The co-crystal of ibrutinib according to claim 4 , wherein said co-crystal has characteristic X-ray powder diffraction peaks at 9.9 claim 4 , 17.4 claim 4 , 18.7 claim 4 , 20.5 and 21.7 degrees 2-theta ±0.2 degrees 2-theta.6. The co-crystal of ibrutinib according to claim 1 , wherein the co-crystal of ibrutinib is ibrutinib succinic acid.7. The co-crystal of ibrutinib according to claim 6 , wherein said co-crystal has characteristic X-ray powder diffraction peaks at 17.3 claim 6 , 17.9 claim 6 , 20.2 claim 6 , 21.5 and 21.8 degrees 2-theta ±0.2 degrees 2-theta.8. A pharmaceutical preparation comprising the co-crystal of ibrutinib according to .9. (canceled)10. A method of treating chronic lymphocytic leukemia (CLL) claim 8 , small lymphocytic lymphoma (SLL) that are B-cell non-hodgkin lymphomas (NHL) and mantle cell lymphoma (MCL) in a patient in need thereof claim 8 , said method comprising the step of administering an effective amount of the pharmaceutical preparation according to to said patient.11. (canceled)12. A method of preparing a co-crystal of ibrutinib comprising the steps ofa) suspending ibrutinib with a carboxylic acid in a suitable solvent,b) heating the obtained suspension until a clear solution is obtained,c) optionally keeping the obtained solution for some time and/or under stirring, andd) ...

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Номер записи: 74

16-03-2017 дата публикации

Method for thermal conversion of ketoacids and hydrotreament to hydrocarbons

Номер: US20170073588A1

Автор: Jukka Myllyoja, Rami Piilola

Принадлежит: Neste Oyj

The present disclosure relates to thermal conversion of ketoacids, including methods for increasing the molecular weight of ketoacids, the method including the steps of providing in a reactor a feedstock comprising at least one ketoacid. The feedstock is then subjected to one or more C-C-coupling reaction(s) by heating the feedstock to temperature of 200-500° C. in the absence of a catalyst.

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Номер записи: 75

22-03-2018 дата публикации

Use of 3-carboxy-n-ethyl-n,n-dimethylpropan-1-aminium salts in the treatment of cardiovascular disease

Номер: US20180079728A1

Автор: Daina LOLA, Edgars Liepins, Einars Loza, Iimars Stonans, Ivars Kalvins, Janis Kuka, Maija Dambrova, Osvalds Pugovics, Reinis Vilskersts, Solveiga Grinberga

Принадлежит: JSC GRINDEKS

Salts of 3-carboxy-N-ethyl-N,N-dimethylpropan-1-aminium, method of preparation thereof and use in the treatment of cardiovascular disease.

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Номер записи: 76

26-03-2015 дата публикации

COMPOSITIONS AND METHODS FOR THE TREATMENT OF MUSCLE PAIN

Номер: US20150087697A1

Автор: Kandula Mahesh

Принадлежит:

The invention relates to the compounds of formula I or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I; and methods for treating or preventing muscle pain, a neurological disease, allergy, respiratory diseases or inflammatory disorder may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of muscle disorders, muscle pain, spasticity, neuropathic pain, fibromyalgia, Parkinson's disease, allergy, chronic obstructive pulmonary disease, allergic rhinitis, headache, chronic pain, sub-chronic pain and local pain or its associated complications. 2. A Pharmaceutical composition comprising a compound of and a pharmaceutically acceptable carrier.3. The pharmaceutical composition of claim 2 , which is formulated to treat the underlying etiology with an effective amount administering the patient in need by oral administration claim 2 , delayed release or sustained release claim 2 , transmucosal claim 2 , syrup claim 2 , topical claim 2 , parenteral administration claim 2 , injection claim 2 , subdermal claim 2 , oral solution claim 2 , rectal administration claim 2 , buccal administration or transdermal administration.4. Compounds and compositions of are formulated for the treatment of muscle disorders claim 3 , muscle pain claim 3 , spasticity claim 3 , neuropathic pain claim 3 , fibromyalgia claim 3 , Parkinson's disease claim 3 , allergy claim 3 , chronic obstructive pulmonary disease claim 3 , allergic rhinitis claim 3 , headache claim 3 , chronic pain claim 3 , sub-chronic pain and local pain.5. A molecular conjugate of N claim 3 ,N-dimethyl-2-(phenyl(o-tolyl)methoxy)ethanamine and R-Lipoic acid.6. A molecular conjugate of N-ethyl-N-methyl-2-(phenyl(o-tolyl)methoxy)ethanamine and R-Lipoic ...

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Номер записи: 77

12-06-2014 дата публикации

Carbamate/urea derivatives

Номер: US20140163036A1

Автор: Dario Braga, Haiyang Jiang, Marco Curzi, Mark Gary Bock, Piotr Karpinski, Stefano Luca Giaffreda, Stephanie Kay Dodd, Thomas J. Troxler, Tielin Wang, Xiaoyang Wang, Xuechun Zhang, Yves Auberson

Принадлежит: Individual

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

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Номер записи: 78

05-04-2018 дата публикации

SALTS AND POLYMORPHS OF 8-FLUORO-2-{4-[(METHYLAMINO)METHYL]PHENYL}-1,3,4,5-TETRAHYDRO-6H-AZEPINO[5,4,3-CD]INDOL-6-ONE

Номер: US20180092925A1

Автор: Basford Patricia Ann, Campeta Anthony Michael, Gillmore Adam, Jones Matthew Cameron, Kougoulos Eleftherios, Luthra Suman, Walton Robert

Принадлежит:

The present invention relates to novel polymorphic forms of 8-fluoro-2-{4-[(methylamino)methyl]phenyl}-1,3,4,5-tetrahydro-6H-azepino[5,4,3-cd]indol-6-one, and to processes for their preparation. Such polymorphic forms may be a component of a pharmaceutical composition and may be used to treat a mammalian disease condition mediated by poly(ADP-ribose) polymerase activity including the disease condition such as cancer. 1. A crystalline camsylate salt of 8-fluoro-2-{4-[(methylamino)methyl]phenyl}-1 ,3 ,4 ,5-tetrahydro-6H-azepino[5 ,4 ,3-cd]indol-6-one , wherein the salt has a powder X-ray diffraction pattern comprising two or more peaks at diffraction angle (2θ) selected from the group consisting of 12.2±0.2 , 13.8±0.2 , 18.3±0.2 , 22.5±0.2 , and 25.4±0.2 , wherein said powder x-ray diffraction pattern is obtained using copper k-alphax-rays at a wave length of 1.5406 Ångstroms.2. The salt of claim 1 , wherein the salt has a solid state NMR spectrum comprising 2 or more C chemical shifts selected from the group consisting of 213.4±0.2 claim 1 , 171.8±0.2 claim 1 , and 17.3±0.2 ppm.3. The salt of claim 1 , wherein the salt has a solid state NMR spectrum comprising F chemical shifts at −118.9±0.2 and −119.7±0.2 ppm.4. The salt of claim 1 , wherein the DSC thermogram of the salt comprises an endotherm onset at 303.2° C.5. The salt of claim 1 , wherein the camsylate comprises S-camsylate.6. The salt of claim 1 , wherein the camsylate comprises R-camsylate.7. A pharmaceutical composition comprising the salt of and a pharmaceutically acceptable carrier. This application is a continuation of U.S. application Ser. No. 14/698,463, filed Apr. 28, 2015, entitled “Salts and Polymorphs of 8-Fluoro-2-{4-[(Methylamino)Methyl]Phenyl}-1,3,4,5-Tetrahydro-6H-Azepino[5,4,3-cd]Indol-6-One”. U.S. application Ser. No. 14/698,463 is a continuation of U.S. application Ser. No. 14/272,589, filed May 8, 2014, now U.S. Pat. No. 9,045,487. U.S. application Ser. No. 14/272,589 is a continuation of U ...

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Номер записи: 79

09-04-2015 дата публикации

Nilotinib Salts And Crystalline Forms Thereof

Номер: US20150099885A1

Автор: PIRAN Maytal, Rendell Jacob

Принадлежит:

Nilotinib salts and crystalline forms thereof have been prepared and characterized. 125-. (canceled)26. A crystalline form of Nilotinib hydrochloride selected from the group consisting of{'figref': [{'@idref': 'DRAWINGS', 'FIG. 1'}, {'@idref': 'DRAWINGS', 'FIG. 2'}], 'a) crystalline form T20 of Nilotinib hydrochloride characterized by data selected from the group consisting of: an X-ray powder diffraction pattern having peaks at 5.3, 7.0, 14.4, 20.1, and 21.1 degrees two theta ±0.2 degrees two theta; an X-ray powder diffraction pattern substantially as depicted in ; an X-ray powder diffraction pattern substantially as depicted in ; and combinations thereof;'}{'figref': {'@idref': 'DRAWINGS', 'FIG. 68'}, 'b) crystalline form T27 of Nilotinib hydrochloride characterized by data selected from the group consisting of: an X-ray powder diffraction pattern having peaks at 6.8, 11.8, 12.6, 13.7, and 25.3 degrees two theta ±0.2 degrees two theta; an X-ray powder diffraction pattern substantially as depicted in ; and combinations thereof;'}{'figref': {'@idref': 'DRAWINGS', 'FIG. 69'}, 'c) crystalline form T28 of Nilotinib hydrochloride characterized by data selected from the group consisting of: an X-ray powder diffraction pattern having peaks at 4.2, 8.5, 11.3, 12.8, and 16.0 degrees two theta ±0.2 degrees two theta; an X-ray powder diffraction pattern substantially as depicted in ; and combinations thereof; and'}{'figref': {'@idref': 'DRAWINGS', 'FIG. 70'}, 'd) crystalline form T29 of Nilotinib hydrochloride characterized by data selected from the group consisting of: an X-ray powder diffraction pattern having peaks at 6.0, 6.4, 8.9, 19.7, and 20.6 degrees two theta ±0.2 degrees two theta; an X-ray powder diffraction pattern substantially as depicted in ; and combinations thereof.'}27. The crystalline form T20 of Nilotinib hydrochloride according to further characterized by data selected from the group consisting of: an X-ray powder diffraction pattern having additional ...

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Номер записи: 80

05-04-2018 дата публикации

CURABLE COMPOSITIONS CONTAINING 1,1-DI-ACTIVATED VINYL COMPOUNDS THAT CURE BY PERICYCLIC REACTION MECHANISMS

Номер: US20180094115A1

Автор: Gottumukkala Aditya Lakshmi Narasimha Raju, Hellring Stuart Damon, Martz Jonathan Thomas, Peskens Ronnie Albertus Johannes, ZALICH MICHAEL ANDREW

Принадлежит:

Curable compositions containing a compound comprising a conjugated diene group and a 1,1-di-activated vinyl compound are described. The curable compositions can cure by pericyclic reaction mechanisms. 1. A curable composition comprising:a compound comprising a conjugated diene group; anda 1,1-di-activated vinyl compound, or a multifunctional form thereof, or a combination thereof.2. The curable composition of claim 1 , wherein the 1 claim 1 ,1-di-activated vinyl compound comprises a methylene dicarbonyl compound claim 1 , a dihalo vinyl compound claim 1 , a dihaloalkyl disubstituted vinyl compound claim 1 , or a cyanoacrylate compound claim 1 , or a multifunctional form of any thereof claim 1 , or a combination of any thereof.3. The curable composition of claim 2 , wherein the 1 claim 2 ,1-di-activated vinyl compound comprises:a dialkyl methylene malonate;a diaryl methylene malonate;a multifunctional form of a dialkyl methylene malonate; ora multifunctional form of a diaryl methylene malonate; ora combination of any thereof.4. The curable composition of claim 3 , wherein the 1 claim 3 ,1-di-activated vinyl compound comprises:diethyl methylene malonate; and/ora multifunctional form of diethyl methylene malonate comprising a transesterification adduct of diethyl methylene malonate and at least one polyol.5. The curable composition of claim 4 , wherein the transesterification adduct of diethyl methylene malonate and at least one polyol comprises a transesterification adduct of diethyl methylene malonate and a diol.6. The curable composition of claim 5 , wherein the diol comprises an alkane diol.7. The curable composition of claim 6 , wherein the alkane diol comprises 1 claim 6 ,5-pentane diol and/or 1 claim 6 ,6-hexanediol.8. The curable composition of claim 1 , wherein the compound comprising a conjugated diene groups comprises a polymer resin comprising pendant and/or terminal conjugated diene groups.9. The curable composition of claim 8 , wherein the resin comprises ...

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Номер записи: 81

14-04-2016 дата публикации

Synthesis of Triethylenetetramines

Номер: US20160102060A1

Автор: Antonio Soi, Günther Schmidt, Irene Vaulont, Marco Jonas

Принадлежит: PHILERA NEW ZEALAND Ltd

Methods and intermediates for synthesizing triethylenetetramine and salts thereof, as well as novel triethylenetetramine salts and their crystal structure, and triethylenetetramine salts of high purity.

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Номер записи: 82

08-04-2021 дата публикации

Free polyunsaturated fatty acid-containing composition and manufacturing method therefor

Номер: US20210102142A1

Автор: Hideaki Yamaguchi, Nobushige Doisaki, Yuhei Kosuge

Принадлежит: Nippon Suisan Kaisha Ltd

The present disclosure is: a free polyunsaturated fatty acid-containing composition, which comprises at least one free polyunsaturated fatty acid having 20 or more carbon atoms, the content being at least 80.0% of the fatty acids in the composition, and satisfies at least one selected from a group consisting of conditions (1) and (2): (1) the content of conjugated unsaturated fatty acid is 1.0% or less of the fatty acids in the composition, and (2) the Gardner color is less than 3+; and a manufacturing method for the free polyunsaturated fatty acid-containing composition comprising the preparation of a raw material composition containing at least one polyunsaturated fatty acid having 20 or more carbon atoms, and hydrolysis of a reaction solution containing the prepared raw material composition, a lower alcohol, water and an alkali catalyst at a temperature of 10° C. or lower.

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Номер записи: 83

29-04-2021 дата публикации

NICOTINE SALTS, CO-CRYSTALS, AND SALT CO-CRYSTAL COMPLEXES

Номер: US20210122728A1

Автор: Carr Andrew, Dull Gary M., Sharp Emma

Принадлежит:

The invention provides certain nicotine salts, co-crystals, and salt co-crystals and provides novel polymorphic forms of certain nicotine salts. In particular, nicotine salts with orotic acid are described. The invention further provides methods of preparation and characterization of such nicotine salts. In addition, tobacco products, including smoking articles, smokeless tobacco products, and electronic smoking articles comprising nicotine salts, co-crystals, and/or salt co-crystals are also provided. 120.-. (canceled)21. An oral product comprising a salt of nicotine and fumaric acid , wherein the salt is a non-solvated mono-salt , characterized by an X-ray powder diffraction pattern having peaks at one or more of the following 2-theta diffraction angles: 14.9 , 18.4 , 19.9 , and 22.4.22. The oral product of claim 21 , in the form of loose moist snuff; loose dry snuff; chewing tobacco; pelletized tobacco pieces; extruded or formed tobacco strips claim 21 , pieces claim 21 , rods claim 21 , cylinders or sticks; finely divided ground powders; finely divided or milled agglomerates of powdered pieces and components; flake-like pieces; molded tobacco pieces; gums; rolls of tape-like films; readily water-dissolvable or water-dispersible films or strips; meltable compositions; lozenges; pastilles; and capsule-like materials possessing an outer shell and an inner region.23. The oral product of claim 21 , in the form of a lozenge claim 21 , wherein the lozenge further comprises at least about 50% by weight isomalt.24. The oral product of claim 21 , in the form of a lozenge claim 21 , wherein the lozenge further comprises at least about 70% by weight isomalt.25. The oral product of claim 21 , in the form of a lozenge claim 21 , wherein the lozenge further comprises at least about 80% by weight isomalt.26. The oral product of claim 23 , further comprising maltitol syrup.27. The oral product of claim 23 , further comprising one or more of a salt claim 23 , sweetener claim 23 , ...

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Номер записи: 84

03-05-2018 дата публикации

HEMIFUMARATE SALT OF 1-[4-[1-(4-CYCLOHEXYL-3-TRIFLUOROMETHYL-BENZYLOXYIMINO)-ETHYL]-2-ETHYL-BENZYL]-AZETIDINE-3-CARBOXYLIC ACID

Номер: US20180118678A1

Автор: Ciszewski Lech, DE LA CRUZ Marilyn, Karpinski Piotr H., Mutz Michael, RIEGERT Christian, Schneeberger Ricardo, Vogel Caspar

Принадлежит:

This invention relates to a hemifumarate salt of 1-(4- 1-[(E)-cyclohexyl-3-tritluoromethy 1-benzy loxyimino ]-ethy 1)-2-ethy1-benzy l)-azetidine-3-carboxy lie acid (Compound) to pharmaceutics compositions comprising this salt, to processes for forming this salt and to its use in medical treatment, addition, the present invention also relates to new polymorphic forms of the hemifumarate salt form of Compound I, as well as to pharmaceutical compositions comprising these polymorphic forms, to processes for obtaining them, and their use in medical treatment. 1. Crystalline form A of 1-(4-{1-[(E)-4-cyclohexyl-1-3-trifluoromethyl-benzyloxyimino]-ethyl}-2-ethyl-benzyl)-azetidine-3-carboxylic acid , (E)-but-2-enedioic acid.2. The crystalline form A of claim 1 , wherein said crystalline form has an X-ray powder diffraction pattern with at least one specific peak at about 2-theta=20.7°.3. The crystalline form A of claim 1 , wherein said crystalline form has an X-ray powder diffraction pattern with specific peaks at about 2-theta=6.9° claim 1 , 17.5° claim 1 , 18.1° and 20.7°.4. The crystalline form A of claim 1 , wherein said crystalline form has an X-ray powder diffraction pattern with at least one specific peak at about 2-theta=6.9° claim 1 , 17.5° claim 1 , 18.1° claim 1 , 20.4° or 20.7°.5. The crystalline form A of claim 1 , wherein said crystalline form has an X-ray powder diffraction pattern with at least one specific peak at about 2-theta =6.9° claim 1 , 10.1° claim 1 , 10.6° claim 1 , 12.1° claim 1 , 17.5° claim 1 , 18.1° or 20.7°.7. The crystalline form A of claim 1 , wherein has a degree of crystallinity greater than about 20%.8. The crystalline form A of claim 1 , wherein has a degree of crystallinity greater than about 90%.9. Crystalline form B of 1-(4-{1-[(E)-4-cyclohexyl-1-3-trifluoromethyl-benzyloxyimino]-ethyl}-2-ethyl-benzyl)-azetidine-3-carboxylic acid claim 1 , (E)-but-2-enedioic acid claim 1 , wherein said crystalline form has an X-ray powder diffraction ...

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Номер записи: 85

03-05-2018 дата публикации

NON-DELIQUESCENT ACID ADDITION SALT OF 3-AMINOQUINUCLIDINE

Номер: US20180118736A1

Автор: NODA Tetsuji, Takeda Yukiko

Принадлежит: YUKI GOSEI KOGYO CO. LTD.

A novel acid addition salt of 3-aminoquinuclidine, which is an industrially useful compound as an intermediate of medicines and does not exhibit deliquescence, is provided. 1. An acid addition salt of 3-aminoquinuclidine selected from the group consisting of racemic 3-aminoquinuclidine , (R)-3-aminoquinuclidine , and (S)-3-aminoquinuclidine , and acid selected from the group consisting of phosphoric acid , sulfuric acid , fumaric acid , terephthalic acid , oxalic acid , p-toluenesulfonic acid , (±)-10-camphorsulfonic acid , and (−)-10-camphorsulfonic acid , wherein the acid addition salt does not exhibit deliquescence.2. The acid addition salt according to claim 1 , of racemic 3-aminoquinuclidine and acid selected from the group consisting of phosphoric acid claim 1 , fumaric acid claim 1 , terephthalic acid claim 1 , oxalic acid claim 1 , p-toluenesulfonic acid claim 1 , and (±)-10-camphorsulfonic acid claim 1 , wherein the acid addition salt does not exhibit deliquescence.3. The acid addition salt according to claim 1 , selected from the group consisting of[1] racemic 3-aminoquinuclidine.sesquiphosphate,[2] racemic 3-aminoquinuclidine.monofumarate,[3] racemic 3-aminoquinuclidine.monoterephthalate,[4] racemic 3-aminoquinuclidine.monooxalate,[5] racemic 3-aminoquinuclidine.mono-p-toluenesulfonate, and[6] racemic 3-aminoquinuclidine.mono-(±)-10-camphorsulfonate.4. The acid addition salt according to claim 1 , of (R)-3-aminoquinuclidine and acid selected from the group consisting of phosphoric acid claim 1 , sulfuric acid claim 1 , fumaric acid claim 1 , terephthalic acid claim 1 , oxalic acid claim 1 , p-toluenesulfonic acid claim 1 , and (−)-10-camphorsulfonic acid claim 1 , wherein the acid addition salt does not exhibit deliquescence.5. The acid addition salt according to claim 1 , selected from the group consisting of[1] (R)-3-aminoquinuclidine sesquiphosphate,[2] (R)-3-aminoquinuclidine.monosulfate,[3] (R)-3-aminoquinuclidine.monofumarate,[4] (R)-3- ...

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Номер записи: 86

07-05-2015 дата публикации

Multicomponent crystals comprising imatinib mesilate and selected co-crystal formers

Номер: US20150126520A1

Автор: Andreas Hafner, Beate Salvador, Marcus Vossen, Rolf Hellmann, Tiziana CHIODO, Tobias Hintermann

Принадлежит: BASF SE

Novel solid forms of imatinib mesilate comprising as active ingredient 4-[(4-methyl-1-piperazinyl)methyl]-N-[4-methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]-phenyl]-benzamide methanesulfonic acid salt and as co-crystal former benzoic acid, fumaric acid or succinic acid are described. The said multi-component crystalline forms possess improved physical and biological properties with respect to the crystalline forms of the active pharmaceutical ingredient previously known.

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Номер записи: 87

25-08-2022 дата публикации

Pharmaceutically Acceptable Salts of [2-(3-fluoro-5-methane-sulfonylphenoxy)ethyl](propyl)amine and Uses Thereof

Номер: US20220267262A1

Автор: Inese Reine

Принадлежит: Individual

There is disclosed a salt of Formula III, a method for manufacturing thereof as well as uses thereof. (Formula III), wherein X is H or OH, Y is H or a cation selected from the group consisting of Li, Na and K, is a single bond or a double bond, and n is 0.5 or 1.

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Номер записи: 88

27-05-2021 дата публикации

Catalyst for Catalytic Oxidation of Furfural to Prepare Maleic Acid and Application Thereof

Номер: US20210154647A1

Автор: Jianru MA, Mingxue SU, Tao Yang, Wenzhi Li

Принадлежит: HEFEI ENERGY RESEARCH INSTITUTE

A catalyst for catalytic oxidation of furfural to prepare maleic acid, relating to the technical field of renewable energy. The catalyst is a mixture of a bromide and a base. A method for preparing the catalyst in catalytic oxidation of furfural to prepare maleic acid. The method includes: mixing the furfural, the bromide-base, an oxidant and a solvent to carry out a reaction to obtain the maleic acid. The present invention has the advantages that the method has a relatively high conversion rate of furfural and a relatively high yield of maleic acid, the conversion rate of furfural is up to 99%, the yield of maleic acid is up to 68.04%; and the catalyst has a high catalytic selectivity and reusability.

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Номер записи: 89

27-05-2021 дата публикации

FRUQUINTINIB EUTECTIC CRYSTAL, PREPARATION METHOD THEREFOR, COMPOSITION, AND USES THEREOF

Номер: US20210155613A1

Автор: SHENG Xiaohong, SHENG Xiaoxia

Принадлежит: Hangzhou SoliPharma Co., Ltd.

Provided are a fruquintinib and a saccharin salt or eutectic crystal, a fruqintinib and a malonic acid eutectic crystal or a fruquintinib and a maleic euctectic crystal, a preparation method therefor, a pharmaceutical composition containing thereof, and uses thereof in preparing drugs for treating and/or preventing diseases related to abnormal angiogenesis, such as cancer, tumors, macular degeneration, chronic inflammation and the like. 2. Compound A according to claim 1 , is a cocrystal or salt claim 1 , preferably a cocrystal.3. Compound A according to or claim 1 , wherein the X-ray powder diffraction pattern of the Crystalline Form of Compound A claim 1 , expressed as 2θ angles claim 1 , has the following characteristic peaks: 5.0±0.2° claim 1 , 13.2±0.2° claim 1 , 15.4±0.2° and 17.0±0.2°.4. Compound A according to claim 3 , wherein the X-ray powder diffraction pattern of the Crystalline Form of Compound A claim 3 , expressed as 2θ angles claim 3 , has the following characteristic peaks: 5.0±0.2° claim 3 , 10.8±0.2° claim 3 , 11.5±0.2° claim 3 , 13.2±0.2° claim 3 , 14.8±0.2° claim 3 , 15.4±0.2° claim 3 , 17.0±0.2° claim 3 , 23.8±0.2° and 25.4±0.2°.6. Compound A according to any one of to claim 3 , wherein claim 3 , the Fourier IR spectrum of the Crystalline Form of Compound A has characteristic peaks at wave number of 1650±2 cm claim 3 , 1507±2 cm claim 3 , 1422±2 cm claim 3 , 1395±2 cm claim 3 , 1371±2 cm claim 3 , 1274±2 cm claim 3 , 1252±2 cm claim 3 , 1226±2 cm claim 3 , 1145±2 cm claim 3 , 937±2 cm claim 3 , 877±2 cmand 756±2 cm.7. Compound A according to any one of to claim 3 , wherein claim 3 , the single crystal of the Crystalline Form of Compound A claim 3 , measured at 106 K claim 3 , belongs to the triclinic system with space group P1 claim 3 , and has the following unit cell parameters: a=8.6 Å±0.2 Å claim 3 , b=9.0 Å±0.2 Å claim 3 , c=17.3 Å±0.2 Å; and dihedral angles: α=84.0°±0.2° claim 3 , β=77.4°±0.2° claim 3 , γ=77.8°±0.2°.8. A method of ...

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Номер записи: 90

12-05-2016 дата публикации

SUBSTITUTED 5-FLUORO-1H-PYRAZOLOPYRIDINES AND THEIR USE

Номер: US20160129004A1

Автор: ACKERSTAFF Jens, BECKER Eva-Maria, BIERER Donald, FOLLMANN Markus, GRIEBENOW Nils, HARTMANN Elke, JAUTELAT Rolf, KNORR Andreas, Kroh Walter, Li Volkhart Min-Jian, MITTENDORF Joachim, REDLICH Gorden, Schlemmer Karl-Heinz, Stasch Johannes-Peter, Wunder Frank

Принадлежит: ADVERIO PHARMA GMBH

The present application relates to novel substituted 5-fluoro-1H-pyrazolopyridines, to processes for their preparation, to their use alone or in combinations for the treatment and/or prophylaxis of diseases, and to their use for producing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders. 3. (canceled)4. (canceled)5. (canceled)6. (canceled)7. (canceled)8. A medicament comprising the compound of in combination with an inert claim 1 , non-toxic claim 1 , pharmaceutically suitable excipient.9. A medicament comprising the compound of in combination with a further active compound selected claim 1 , from the group consisting of organic nitrates claim 1 , NO donors claim 1 , cGMP-PDE inhibitors claim 1 , agents having antithrombotic activity claim 1 , agents lowering blood pressure claim 1 , and agents altering lipid metabolism.10. (canceled)11. (canceled)12. A method of treating or preventing heart failure claim 1 , angina pectoris claim 1 , hypertension claim 1 , pulmonary hypertension claim 1 , ischaemias claim 1 , vascular disorders claim 1 , kidney failure claim 1 , thromboembolic disorders claim 1 , fibrotic disorders and arteriosclerosis comprising administering an effective amount of the compound of to a human or animal in need thereof. The present application relates to novel substituted 5-fluoro-1H-pyrazolopyridines, to processes for their preparation, to their use alone or in combinations for the treatment and/or prophylaxis of diseases, and to their use for producing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders.One of the most important cellular transmission systems in mammalian cells is cyclic guanosine monophosphate (cGMP). Together with nitrogen monoxide (NO), which is released from the endothelium and transmits hormonal and mechanical signals, it forms the NO/cGMP system. ...

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Номер записи: 91

12-05-2016 дата публикации

POLYMERS PREPARED FROM MEVALONOLACTONE AND DERIVATIVES

Номер: US20160130389A1

Автор: Dugar Deepak, Friedberger Tobias

Принадлежит:

Described herein polymer precursor compounds (aka polymer building blocks) of derived from biobased compounds, and specifically biobased mevalonolactone and its related derivatives. Through oxidation these biobased precursors can be reacted to yield building blocks for (unsaturated-) polyesters, polyester polyols and polyamides, as well as precursors for glycidyl esters and omega-alkenyl esters. Through reduction, these biobased precursors can be reacted to yield building blocks for (unsaturated-) polyesters, polyester polyols, polycarbonates, as well as precursors for glycidyl ethers and omega-alkenyl ethers. Through nucleophilic ring opening and/or amidation, these biobased precursors can be reacted to yield building blocks for polyester polyols, chain-extender for polyurethanes, or polyester-amides. 2. The compound of claim 1 , wherein each Y is —N(H) or —N(R).3. The compound of claim 1 , wherein each Ris selected from the group consisting of C-Calkyls.4. The compound of claim 1 , wherein Q is a linear hydrocarbyl selected from the group consisting of C-Calkyls.5. The compound of claim 1 , wherein said compound has a 14C/12C ratio greater than zero.6. A biobased polymer comprising recurring monomeric units synthesized from a compound according to .8. The compound of claim 1 , wherein each Ris selected from the group consisting of C-Calkyls.9. The compound of claim 7 , wherein said compound has a 14C/12C ratio greater than zero.10. A biobased polymer comprising recurring monomeric units synthesized from a compound according to .12. The compound of claim 11 , wherein each Y is —N(H) or —N(R).13. The compound of claim 11 , wherein each Ris selected from the group consisting of C-Calkyls.14. The compound of claim 11 , wherein Q is a linear hydrocarbyl selected from the group consisting of C-Calkyls15. The compound of claim 11 , wherein said compound has a 14C/12C ratio greater than zero.16. A biobased polymer comprising recurring monomeric units synthesized from a ...

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Номер записи: 92

10-05-2018 дата публикации

MALEATE SALTS OF A B-RAF KINASE INHIBITOR, CRYSTALLINE FORMS, METHODS OF PREPARATION, AND USES THEREFORE

Номер: US20180127412A1

Автор: ZHANG Gouliang, Zhou Changyou

Принадлежит:

The invention relates to 5-(((1R,1aS,6bR)-1-(6-(trifluoromethyl)-1H-benzo [d] imidazol-2-yl)-1a,6b-dihydro-1H-cyclopropa [b] benzofuran-5-yl) oxy)-3,4-dihydro-1,8-naphthyridin-2 (1H)-one (Compound 1) maleate salts, in particular the sesqui-maleate salt and its crystalline forms, methods of preparation, pharmaceutical compositions, and therapeutic uses for treatment of diseases or disorders mediated by BRAF or other kinases. 1. A salt of 5-(((1R ,1aS ,6bR)-1-(6-(trifluoromethyl)-1H-benzo[d]imidazol-2-yl)-1a ,6b-dihydro-1H-cyclopropa[b]benzofuran-5-yl)oxy)-3 ,4-dihydro-1 ,8-naphthyridin-2(1H)-one , which is selected from hydrochloride , methanesulfonate , 2-hydroxyethanesulfonate , maleate and oxalate.2. The salt of claim 1 , which is in solid-state.3. The salt of claim 2 , which is in a crystalline form.5. The compound of claim 4 , wherein n is a number selected from the group consisting of 0.5±0.05 claim 4 , 1.0±0.1 claim 4 , and 1.5±0.2.6. The compound of claim 4 , wherein n is 0.5 claim 4 , 1.0 claim 4 , or 1.5.7. The compound of any one of to claim 4 , wherein the compound is in a crystalline form.9. The compound of claim 8 , which is in Crystalline Form A* and is characterized by a powder X-ray diffraction pattern comprising seven or more diffraction peaks having 2θ angle values independently selected from the group consisting of: 6.3±0.2 claim 8 , 8.9±0.2 claim 8 , 9.4±0.2 claim 8 , 11.2±0.2 claim 8 , 12.6±0.2 claim 8 , 13.4±0.2 claim 8 , 17.9±0.2 claim 8 , 18.6±0.2 claim 8 , 18.8±0.2 claim 8 , 19.3±0.2 claim 8 , 20.1±0.2 claim 8 , 20.7±0.2 claim 8 , 21.2±0.2 claim 8 , 21.8±0.2 claim 8 , 22.4±0.2 claim 8 , 22.6±0.2 claim 8 , 23.3±0.2 claim 8 , 23.8±0.2 claim 8 , 24.7±0.2 claim 8 , 25.6±0.2 claim 8 , 26.1±0.2 claim 8 , 27.4±0.2 claim 8 , 28.3±0.2 claim 8 , 28.6±0.2 claim 8 , 29.0±0.2 claim 8 , 29.4±0.2 claim 8 , and 30.4±0.2 degrees.10. The compound of claim 8 , which is in Crystalline Form A** and is a single crystal as substantially illustrated in claim 8 , ...

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Номер записи: 93

10-05-2018 дата публикации

Co-crystals, salts and solid forms of tenofovir alafenamide

Номер: US20180127446A1

Автор: Bing Shi, FANG Wang, Zhuoyi Su

Принадлежит: Gilead Sciences Inc

The present invention relates to co-crystals, salts and crystalline forms of tenofovir alafenamide and methods for preparation, use and isolation of such compounds

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Номер записи: 94

19-05-2016 дата публикации

Chemical Compounds

Номер: US20160136140A1

Автор: Akhtar Nadim, Bradbury Robert Hugh, Buttar David, Currie Gordon Stuart, De Savi Christopher, Donald Craig Samuel, Norman Richard Albert, Osborne Matthew, Rabow Alfred Arthur, Redfearn Heather, Williams Helen Elizabeth, Yavari Neda

Принадлежит: AstraZeneca AB

The invention concerns compounds of Formula (I) 116.-. (canceled)18. A method as claimed in claim 17 , wherein the compound of Formula (I) is (E)-3-(3 claim 17 ,5-Difluoro-4-((1R claim 17 ,3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-2 claim 17 ,3 claim 17 ,4 claim 17 ,9-tetrahydro-1H-pyrido[3 claim 17 ,4-b]indol-1-yl)phenyl)acrylic acid claim 17 , or a pharmaceutically-acceptable salt thereof.19. A method as claimed in claim 17 , wherein the cancer is breast or gynaecological cancer.21. A combination as claimed in claim 20 , wherein the compound of Formula (I) is (E)-3-(3 claim 20 ,5-Difluoro-4-((1R claim 20 ,3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-2 claim 20 ,3 claim 20 ,4 claim 20 ,9-tetrahydro-1H-pyrido[3 claim 20 ,4-b]indol-1-yl)phenyl)acrylic acid claim 20 , or a pharmaceutically-acceptable salt thereof.22. A combination according to wherein the additional anti-tumour agent is selected from antihormonal agents claim 21 , mTOR inhibitors claim 21 , PI3K-α inhibitors and palbociclib claim 21 , and wherein the cancer is breast or gynaecological cancer.23. A crystalline form of (E)-3-(3 claim 21 ,5-Difluoro-4-((1R claim 21 ,3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-2 claim 21 ,3 claim 21 ,4 claim 21 ,9-tetrahydro-1H-pyrido[3 claim 21 ,4-b]indol-1-yl)phenyl)acrylic acid or a pharmaceutically-acceptable salt thereof.24. A crystalline form of (E)-3-(3 claim 23 ,5-Difluoro-4-((1R claim 23 ,3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-2 claim 23 ,3 claim 23 ,4 claim 23 ,9-tetrahydro-1H-pyrido[3 claim 23 ,4-b]indol-1-yl)phenyl)acrylic acid claim 23 , as claimed in .25. A crystalline form as claimed in claim 23 , which is (E)-3-(3 claim 23 ,5-Difluoro-4-((1R claim 23 ,3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-2 claim 23 ,3 claim 23 ,4 claim 23 ,9-tetrahydro-1H-pyrido[3 claim 23 ,4-b]indol-1-yl)phenyl)acrylic acid Form A.26. A crystalline form as claimed in claim 23 , which is (E)-3-(3 claim 23 ,5-Difluoro-4-((1R claim 23 ,3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-2 claim 23 ,3 ...

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Номер записи: 95

23-04-2020 дата публикации

PROCESS FOR THE PREPARATION OF TRIPLE-BOND-CONTAINING OPTICALLY ACTIVE CARBOXYLIC ACIDS, CARBOXYLATE SALTS AND CARBOXYLIC ACID DERIVATIVES

Номер: US20200123578A1

Автор: Ban Tamas, HORTOBÁGYI Irén, KARDOS Zsuzsanna, LÁSZLÓFI István, Molnar Jozsef, Takacs Laszlo

Принадлежит: CHINOIN GYÓGYSZER ÉS VEGYÉSZETI TERMÉKEK GYÁRA ZRT.

The invention provides a new enzimatic process for the preparation of chiral carboxylic acids, their salts and acid derivatives of the general formula (I) by enzymatic hydrolysis of racemic carboxylic acid ester of the general formula (II) and optionally subsequent esterification or acylation. 2. Process as defined in claim 1 , wherein the enzymatic hydrolysis is carried out with hydrolase enzyme.3Candida rugosa, Pseudomonas fluorescens, Candida antarctica A, Candida antarctica B, Burkholderia cepacia, Rhizopus arrhizus, Rhizomucor miehei, Pseudomonas cepacia lipase. Process as defined in claim 2 , wherein as hydrolase enzyme lipase enzyme claim 2 , such as or pig pancrease lipase claim 2 , calf pancrease lipase are applied.4Candida rugosa. Process as defined in claim 3 , wherein as lipase enzyme enzyme is applied.5. Process as defined in claim 1 , wherein the hydrolysis is carried out in the presence of solvent.6. Process as defined in claim 5 , wherein as solvent ethers claim 5 , hydrocarbon-type and aromatic solvents claim 5 , such as diisopropyl ether claim 5 , methyl tert.-butyl ether claim 5 , n-hexane claim 5 , toluene are applied.7. Process as defined in claim 6 , wherein as solvent methyl tert.-butyl ether is applied.8. Process as defined in claim 1 , wherein depending on the amount and activity of the enzyme claim 1 , the reaction time is 2-48 hours.9. Process as defined in claim 1 , wherein the reaction is performed at 20-40° C.10. Process as defined in claim 2 , wherein the hydrolysis is carried out in the presence of solvent.11. Process as defined in claim 3 , wherein the hydrolysis is carried out in the presence of solvent.12. Process as defined in claim 4 , wherein the hydrolysis is carried out in the presence of solvent.13. Process as defined in claim 2 , wherein depending on the amount and activity of the enzyme claim 2 , the reaction time is 2-48 hours.14. Process as defined in claim 3 , wherein depending on the amount and activity of the enzyme ...

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Номер записи: 96

19-05-2016 дата публикации

POLYMORPHIC FORMS OF ICOTINIB MALEATE AND USES THEREOF

Номер: US20160137658A1

Автор: Ding Lieming, Hu Shaojing, Long Wei, WANG FEI, Wang Yinxiang

Принадлежит: BETTA PHARMACEUTICALS CO., LTD.

Provided are Icotinib maleate (the compound of Formula I) and polymorph forms thereof, and methods of preparing and using them. 2. The polymorph form of claim 1 , wherein the polymorph form is of Form I with an X-ray powder diffraction pattern having characteristic peaks at diffraction angles 2θ of approximately 6.1° claim 1 , 8.1° 15.4° claim 1 , 18.5° claim 1 , 20.3° and 24.2°±0.2°.3. The polymorph form of claim 2 , wherein the X-ray powder diffraction pattern has characteristic peaks at diffraction angles 2θ of approximately 6.1° claim 2 , 8.1° claim 2 , 13.4° claim 2 , 15.4° claim 2 , 16.3° claim 2 , 18.5° claim 2 , 20.3° and 24.2°±0.2°.4. The polymorph form of claim 2 , wherein the X-ray powder diffraction pattern is shown as in .5. The polymorph form of claim 2 , wherein the polymorph form has a melting point between 173° C.-176° C.6. The polymorph form of claim 1 , wherein the polymorph form is of Form II with an X-ray powder diffraction pattern having characteristic peaks at diffraction angles 2θ of approximately 7.5° claim 1 , 19.0° and 31.2°±0.2°.7. The polymorph form of claim 6 , wherein the X-ray powder diffraction pattern has characteristic peaks at diffraction angles 2θ of approximately 7.5° claim 6 , 15.0° claim 6 , 19.0° claim 6 , 23.8° and 31.2°±0.2°.8. The polymorph form of claim 6 , wherein the X-ray powder diffraction pattern has characteristic peaks at diffraction angles 2θ of approximately 7.5° claim 6 , 13.8° claim 6 , 15.0° claim 6 , 15.5° claim 6 , 19.0° claim 6 , 22.5° claim 6 , 23.8° and 31.2°±0.2°.9. The polymorph form of claim 6 , wherein the X-ray powder diffraction pattern is shown as in .10. The polymorph form of claim 6 , wherein the polymorph form has a melting point between 182-184° C.13. A pharmaceutical composition comprising a therapeutically effective amount of the polymorph form of and a pharmaceutically acceptable excipient claim 1 , adjuvant or carrier.14. The pharmaceutical composition of claim 13 , wherein the polymorph ...

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Номер записи: 97

07-08-2014 дата публикации

SALTS OF AZA-BICYCLIC DI-ARYL ETHERS AND METHODS TO MAKE THEM OR THEIR PRECURSORS

Номер: US20140220125A1

Автор: Bianchi Jean-Claude, Buerger Eckart, Har Denis, Karpinski Piotr H., Marterer Wolfgang, Pignone Massimo, Prashad Mahavir, Stingelin Doris, Sutter Bertrand, Villhauer Edwin Bernard, Vivelo James Anthony, Waykole Liladhar Murlidhar, Wu Raeann

Принадлежит: NOVARTIS AG

The present invention relates to salts of (R)-3-(6-(4-methylphenyl)-pyridin-3-yloxy)-1-aza-bicyclo[2.2.2]octane, to methods for making them or their precursors, to pharmaceutical compositions comprising them, and to their use as medicaments. 1. A salt of (R)-3-(6-(4-methylphenyl)-pyridin-3-yloxy)-1-aza-bicyclo[2.2.2]octane wherein said salt is the fumarate , maleate , chloride , phosphate , succinate or malonate salt of (R)-3-(6-(4-methylphenyl)-pyridin-3-yloxy)-1-aza-bicyclo[2.2.2]octane.2. The salt according to claim 1 , wherein the salt is the mono-fumarate salt of (R)-3-(6-(4-methylphenyl)-pyridin-3-yloxy)-1-aza-bicyclo[2.2.2]octane in crystalline form.3. The salt according to claim 2 , wherein the salt is characterized by an XRPD pattern substantially the same as the XRPD pattern shown in .4. The salt according to claim 1 , wherein the salt is the mono-fumarate salt of (R)-3-(6-(4-methylphenyl)-pyridin-3-yloxy)-1-aza-bicyclo[2.2.2]octane in crystalline form claim 1 , wherein the mean particle size of the crystals is at least 15 μm.5. The salt according to claim 2 , wherein the salt is the mono-fumarate salt of (R)-3-(6-(4-methylphenyl)-pyridin-3-yloxy)-1-aza-bicyclo[2.2.2]octane in crystalline form claim 2 , and wherein the salt is in substantially pure form.6. The salt according to claim 2 , wherein the salt is the mono-fumarate salt of (R)-3-(6-(4-methylphenyl)-pyridin-3-yloxy)-1-aza-bicyclo[2.2.2]octane in crystalline form claim 2 , and wherein the salt has a purity greater than 90 weight %.7. A pharmaceutical composition claim 1 , which comprises a salt as defined in as active ingredient and at least one pharmaceutically acceptable carrier.8. A pharmaceutical composition claim 1 , which comprises a salt as defined in in combination with one or more further therapeutic agent as active ingredients and at least one pharmaceutically acceptable carrier.9. A pharmaceutical composition comprising mono-fumarate of (R)-3-(6-(4-methylphenyl)-pyridin-3-yloxy)-1-aza- ...

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Номер записи: 98

07-08-2014 дата публикации

Ndm inhibitor

Номер: US20140221330A1

Автор: Akihiro Morinaka, Kazunori Maebashi, Mototsugu Yamada, Muneo Hikida, Takao Abe, Takashi Ida

Принадлежит: Meiji Seika Pharma Co Ltd

An objective of the present invention is to provide a novel NDM (New Delhi metallo-β-lactamase) inhibitor that functions as a drug for restoring the antibacterial activity of β-lactam antibiotics that have been inactivated as a result of decomposition by NDM. According to the present invention, there is provided an NDM inhibitor contains a compound represented by general formula (I):

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Номер записи: 99

09-05-2019 дата публикации

Continuous method for producing muconic acid from aldaric acid

Номер: US20190135727A1

Автор: Asikainen Martta, Jauhiainen Olli, Linnekoski Juha, Martiskainen Miika, Thomas David

Принадлежит:

According to an example aspect of the present invention, there is provided a continuous method of producing muconic acid from aldaric acid in the presence of a solid heterogeneous catalyst and an alcohol solvent with short reaction time. Another aspect of the present invention is the use of a non-expensive solid heterogenous catalyst, which is automatically separated from the product. 1. A continuous method of producing muconic acid from an aldaric acid comprising passing the aldaric acid in a solvent through a pressurized reactor at temperature of 120 to 140° C. with a solid heterogenous rhenium-based catalyst at weight hourly space velocity of 0.1-10 hduring a pre-determined reaction time.2. The method according to claim 1 , wherein the aldaric acid is galactaric acid or glucaric acid claim 1 , either in free acid or ester form.3. The method according to claim 1 , wherein the solvent is an alcohol solvent selected from monovalent or polyvalent C-Calcohols claim 1 , or any combination thereof.4. The method according to claim 1 , wherein the solvent is methanol or butanol.5. The method according to claim 1 , wherein the catalyst is ammonium perrhenate claim 1 , which is fixed in a packed bed inside of the reactor.6. The method according to claim 1 , wherein the reactor is pressurized into 500-2000 kPa with hydrogen claim 1 , argon or nitrogen gas flow through the reactor.7. The method according to claim 1 , wherein the catalyst is activated by heat at temperature of 120 to 130° C. for at least an hour before passing the aldaric acid feed through the reactor.8. The method according to claim 1 , wherein the weight hourly space velocity is 0.2-5 h claim 1 , more preferably about 0.2 h.9. The method according to claim 1 , wherein the reaction time is 1 to 6 hours.10. Use of muconic acid and esters as an intermediate in the production of industrial chemicals and pharmaceutical building blocks wherein the muconic acid and esters are produced by a continuous method of ...

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Номер записи: 100