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RU2013153466A - CRYSTALLINE FORM OF INDAZOLYLAMIDE DERIVATIVES FOR TREATMENT OF MEDICINES WITH GLUCCORTICOID RECEPTORS OF DISORDERS - Google Patents

CRYSTALLINE FORM OF INDAZOLYLAMIDE DERIVATIVES FOR TREATMENT OF MEDICINES WITH GLUCCORTICOID RECEPTORS OF DISORDERS Download PDF

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RU2013153466A
RU2013153466A RU2013153466/04A RU2013153466A RU2013153466A RU 2013153466 A RU2013153466 A RU 2013153466A RU 2013153466/04 A RU2013153466/04 A RU 2013153466/04A RU 2013153466 A RU2013153466 A RU 2013153466A RU 2013153466 A RU2013153466 A RU 2013153466A
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compound
treatment
mammal
medicament
powder
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RU2013153466/04A
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Russian (ru)
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Хелена Ингемо АНДЕРССОН
Келли Ивонн КОНУЭЙ
Майкл Джон КУЭЙЛ
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Астразенека Аб
Байер Интеллекчуал Проперти Гмбх
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Publication of RU2013153466A publication Critical patent/RU2013153466A/en

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
    • C07D231/56—Benzopyrazoles; Hydrogenated benzopyrazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/416—1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pulmonology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Immunology (AREA)
  • Dermatology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

1. Кристаллическая форма, которая представляет собой Форму В 2,2,2-трифтор-N-[(1R,2S)-1-[1-(4-фторфенил)индазол-5-ил]окси-1-(3-метоксифенил)-пропан-2-ил]ацетамида (Форма В соединения (I)).2. Форма В соединения (I) по п.1, характеризующаяся картиной дифракции рентгеновских лучей на порошке, измеренной с использованием длины волны рентгеновских лучей 1,5418 Å, с пиками при 2-тета (в градусах) 9,2, 17,4 и 21,5.3. Форма В соединения (I) по п.1, характеризующаяся картиной дифракции рентгеновских лучей на порошке, измеренной с использованием длины волны рентгеновских лучей 1,5418 Å, с пиками при 2-тета (в градусах) 9,2, 11,8, 15,7, 17,4 и 21,5.4. Форма В соединения (I) по п.1, отличающаяся тем, что указанная форма имеет картину дифракции рентгеновских лучей на порошке, по существу, такую, как показано на Фиг.1.5. Фармацевтическая композиция, содержащая Форму В соединения (I) по любому из пп.1-4 и фармацевтически приемлемый адъювант, разбавитель или носитель.6. Форма В соединения (I) по любому из пп.1-4 для применения в терапии.7. Применение Формы В соединения (I) по любому из пп.1-4 в изготовлении лекарственного средства для лечения респираторного состояния.8. Применение Формы В соединения (I) по любому из пп.1-4 в изготовлении лекарственного средства для лечения COPD (хроническое обструктивное заболевание легких).9. Применение Формы В соединения (I) по любому из пп.1-4 в изготовлении лекарственного средства для лечения астмы.10. Способ лечения респираторного состояния у млекопитающего (такого как человек), включающий введение нуждающемуся в таком лечении млекопитающему эффективного количества Формы В соединения (I) по любому из пп.1-4.11. Способ лечения COPD у млекопитающего (такого как человек), вк1. The crystalline form, which is Form B, 2,2,2-trifluoro-N - [(1R, 2S) -1- [1- (4-fluorophenyl) indazol-5-yl] oxy-1- (3- methoxyphenyl) propan-2-yl] acetamide (Form B of compound (I)). 2. Form B of compound (I) according to claim 1, characterized by a powder X-ray diffraction pattern measured using an X-ray wavelength of 1.5418 Å, with peaks at 2-theta (in degrees) of 9.2, 17.4 and 21 , 5.3. Form B of compound (I) according to claim 1, characterized by a powder X-ray diffraction pattern, measured using an X-ray wavelength of 1.5418 Å, with peaks at 2-theta (degrees) 9.2, 11.8, 15 , 7, 17.4 and 21.5.4. Form B of compound (I) according to claim 1, characterized in that said form has a powder X-ray diffraction pattern substantially as shown in FIG. 1.5. A pharmaceutical composition comprising Form B of compound (I) according to any one of claims 1 to 4 and a pharmaceutically acceptable adjuvant, diluent or carrier. Form B of compound (I) according to any one of claims 1 to 4 for use in therapy. The use of Form B of compound (I) according to any one of claims 1 to 4 in the manufacture of a medicament for the treatment of a respiratory condition. The use of Form B of compound (I) according to any one of claims 1 to 4 in the manufacture of a medicament for the treatment of COPD (chronic obstructive pulmonary disease) .9. The use of Form B of compound (I) according to any one of claims 1 to 4 in the manufacture of a medicament for the treatment of asthma. 10. A method for treating a respiratory condition in a mammal (such as a human), comprising administering to a mammal in need of such treatment an effective amount of Form B of compound (I) according to any one of claims 1 to 4.11. A method of treating COPD in a mammal (such as a human), VK

Claims (13)

1. Кристаллическая форма, которая представляет собой Форму В 2,2,2-трифтор-N-[(1R,2S)-1-[1-(4-фторфенил)индазол-5-ил]окси-1-(3-метоксифенил)-пропан-2-ил]ацетамида (Форма В соединения (I)).1. The crystalline form, which is Form B, 2,2,2-trifluoro-N - [(1R, 2S) -1- [1- (4-fluorophenyl) indazol-5-yl] oxy-1- (3- methoxyphenyl) propan-2-yl] acetamide (Form B of compound (I)). 2. Форма В соединения (I) по п.1, характеризующаяся картиной дифракции рентгеновских лучей на порошке, измеренной с использованием длины волны рентгеновских лучей 1,5418 Å, с пиками при 2-тета (в градусах) 9,2, 17,4 и 21,5.2. Form B of compound (I) according to claim 1, characterized by a powder X-ray diffraction pattern, measured using an X-ray wavelength of 1.5418 Å, with peaks at 2-theta (degrees) 9.2, 17.4 and 21.5. 3. Форма В соединения (I) по п.1, характеризующаяся картиной дифракции рентгеновских лучей на порошке, измеренной с использованием длины волны рентгеновских лучей 1,5418 Å, с пиками при 2-тета (в градусах) 9,2, 11,8, 15,7, 17,4 и 21,5.3. Form B of compound (I) according to claim 1, characterized by a powder X-ray diffraction pattern, measured using an X-ray wavelength of 1.5418 Å, with peaks at 2-theta (in degrees) 9.2, 11.8 , 15.7, 17.4 and 21.5. 4. Форма В соединения (I) по п.1, отличающаяся тем, что указанная форма имеет картину дифракции рентгеновских лучей на порошке, по существу, такую, как показано на Фиг.1.4. Form B of compound (I) according to claim 1, characterized in that said form has a powder X-ray diffraction pattern substantially as shown in FIG. 5. Фармацевтическая композиция, содержащая Форму В соединения (I) по любому из пп.1-4 и фармацевтически приемлемый адъювант, разбавитель или носитель.5. A pharmaceutical composition comprising Form B of compound (I) according to any one of claims 1 to 4, and a pharmaceutically acceptable adjuvant, diluent or carrier. 6. Форма В соединения (I) по любому из пп.1-4 для применения в терапии.6. Form B of compound (I) according to any one of claims 1 to 4 for use in therapy. 7. Применение Формы В соединения (I) по любому из пп.1-4 в изготовлении лекарственного средства для лечения респираторного состояния.7. The use of Form B of compound (I) according to any one of claims 1 to 4 in the manufacture of a medicament for the treatment of a respiratory condition. 8. Применение Формы В соединения (I) по любому из пп.1-4 в изготовлении лекарственного средства для лечения COPD (хроническое обструктивное заболевание легких).8. The use of Form B of compound (I) according to any one of claims 1 to 4 in the manufacture of a medicament for the treatment of COPD (chronic obstructive pulmonary disease). 9. Применение Формы В соединения (I) по любому из пп.1-4 в изготовлении лекарственного средства для лечения астмы.9. The use of Form B of compound (I) according to any one of claims 1 to 4 in the manufacture of a medicament for the treatment of asthma. 10. Способ лечения респираторного состояния у млекопитающего (такого как человек), включающий введение нуждающемуся в таком лечении млекопитающему эффективного количества Формы В соединения (I) по любому из пп.1-4.10. A method of treating a respiratory condition in a mammal (such as a human), comprising administering to a mammal in need of such treatment an effective amount of Form B of compound (I) according to any one of claims 1 to 4. 11. Способ лечения COPD у млекопитающего (такого как человек), включающий введение нуждающемуся в таком лечении млекопитающему эффективного количества Формы В соединения (I) по любому из пп.1-4.11. A method of treating COPD in a mammal (such as a human), comprising administering to a mammal in need of such treatment an effective amount of Form B of compound (I) according to any one of claims 1 to 4. 12. Способ лечения астмы у млекопитающего (такого как человек), включающий введение нуждающемуся в таком лечении млекопитающему эффективного количества Формы В соединения (I) по любому из пп.1-4.12. A method of treating asthma in a mammal (such as a human), comprising administering to a mammal in need of such treatment an effective amount of Form B of compound (I) according to any one of claims 1 to 4. 13. Комбинация Формы В соединения (I) по любому из пп.1-4 и одного или более агентов, выбранных из перечня, включающего следующее:13. The combination of Form B of compound (I) according to any one of claims 1 to 4 and one or more agents selected from the list including the following: - ингибитор PDE4 (фосфодиэстераза 4);- PDE4 inhibitor (phosphodiesterase 4); - селективный агонист β2 адренорецепторов;- selective agonist of β 2 adrenergic receptors; - антагонист мускариновых рецепторов;- antagonist of muscarinic receptors; - стероид;- a steroid; - модулятор функционирования хемокиновых рецепторов;- a modulator of the functioning of chemokine receptors; - ингибитор функционирования р38 киназы;- an inhibitor of the functioning of p38 kinase; - ингибитор матриксных металлопротеиназ (ММР), наиболее предпочтительно нацеленный на ММР-2, -9 или ММР-12; илиan inhibitor of matrix metalloproteinases (MMPs), most preferably targeting MMP-2, -9 or MMP-12; or - ингибитор нейтрофильных сериновых протеаз, наиболее предпочтительно нейтрофильной эластазы или протеиназы 3.an inhibitor of neutrophilic serine proteases, most preferably neutrophilic elastase or proteinase 3.
RU2013153466/04A 2011-06-29 2012-06-27 CRYSTALLINE FORM OF INDAZOLYLAMIDE DERIVATIVES FOR TREATMENT OF MEDICINES WITH GLUCCORTICOID RECEPTORS OF DISORDERS RU2013153466A (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161502656P 2011-06-29 2011-06-29
US61/502,656 2011-06-29
PCT/GB2012/051503 WO2013001294A1 (en) 2011-06-29 2012-06-27 Crystalline form of indazolyl amide derivatives for the treatment glucocorticoid receptor mediated disorders

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Country Status (16)

Country Link
EP (1) EP2726464A1 (en)
JP (1) JP2014527955A (en)
KR (1) KR20140036230A (en)
CN (1) CN103814015A (en)
AR (1) AR086818A1 (en)
AU (1) AU2012277514A1 (en)
BR (1) BR112013031759A2 (en)
CA (1) CA2839398A1 (en)
IN (1) IN2014MN00023A (en)
MX (1) MX2013014566A (en)
RU (1) RU2013153466A (en)
SG (1) SG195309A1 (en)
TW (1) TW201305115A (en)
UY (1) UY34170A (en)
WO (1) WO2013001294A1 (en)
ZA (1) ZA201309480B (en)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
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WO2017161518A1 (en) 2016-03-23 2017-09-28 Astrazeneca Ab New physical form
CN108314670B (en) * 2018-02-06 2020-04-07 江苏八巨药业有限公司 Preparation method of (S) -2-chloro-1- (6-fluoro-1-chroman-2-yl) -ethanol
CN116528696A (en) * 2020-11-27 2023-08-01 未来实验室生物科学有限公司 High-purity beta Nicotinamide Mononucleotide (NMN) and method for producing same
CN116283781A (en) * 2022-12-16 2023-06-23 药康众拓(江苏)医药科技有限公司北京分公司 Deuterated N-phenyl indazole amide compound, pharmaceutical composition and application
KR102571432B1 (en) * 2023-02-08 2023-08-29 주식회사 에스씨엘테라퓨틱스 Composition for treating cancer containing indazolyl ester and amide derivative

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SE9101090D0 (en) 1991-04-11 1991-04-11 Astra Ab PROCESS FOR CONDITIONING OF WATER-SOLUBLE SUBSTANCES
SE9302777D0 (en) 1993-08-27 1993-08-27 Astra Ab Process for conditioning substances
GB0315509D0 (en) 2003-07-02 2003-08-06 Meridica Ltd Dispensing device
JO2754B1 (en) 2006-12-21 2014-03-15 استرازينكا ايه بي Indazolyl amide derivatives for the treatment of glucocorticoid receptor mediated disorders
WO2008079073A1 (en) 2006-12-22 2008-07-03 Astrazeneca Ab Indazolyl sulphonamide derivatives for the treatment of glucocorticoid receptor mediated disorders
CN103118726B (en) 2010-07-21 2015-07-22 阿斯利康(瑞典)有限公司 Inhaler
KR20130036287A (en) 2010-07-21 2013-04-11 아스트라제네카 아베 Inhaler

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AR086818A1 (en) 2014-01-22
CN103814015A (en) 2014-05-21
IN2014MN00023A (en) 2015-06-12
WO2013001294A1 (en) 2013-01-03
TW201305115A (en) 2013-02-01
MX2013014566A (en) 2014-09-25
JP2014527955A (en) 2014-10-23
SG195309A1 (en) 2013-12-30
UY34170A (en) 2013-01-31
KR20140036230A (en) 2014-03-25
AU2012277514A1 (en) 2014-01-09
CA2839398A1 (en) 2013-01-03
EP2726464A1 (en) 2014-05-07
ZA201309480B (en) 2015-10-28
BR112013031759A2 (en) 2016-12-13

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