RU2008105972A - Новая соль i - Google Patents

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RU2008105972A
RU2008105972A RU2008105972/04A RU2008105972A RU2008105972A RU 2008105972 A RU2008105972 A RU 2008105972A RU 2008105972/04 A RU2008105972/04 A RU 2008105972/04A RU 2008105972 A RU2008105972 A RU 2008105972A RU 2008105972 A RU2008105972 A RU 2008105972A
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compound according
powder
ray diffraction
pharmaceutical composition
disease
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RU2008105972/04A
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RU2417220C2 (ru
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Жюльен ДЖОВАННИНИ (GB)
Жюльен ДЖОВАННИНИ
Бо-Йеран ЙОСЕФССОН (SE)
Бо-Йеран ЙОСЕФССОН
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Астразенека Аб (Se)
Астразенека Аб
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/007—Pulmonary tract; Aromatherapy
    • A61K9/0073—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy
    • A61K9/0075—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy for inhalation via a dry powder inhaler [DPI], e.g. comprising micronized drug mixed with lactose carrier particles
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4468—Non condensed piperidines, e.g. piperocaine having a nitrogen directly attached in position 4, e.g. clebopride, fentanyl
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D211/56—Nitrogen atoms
    • C07D211/58—Nitrogen atoms attached in position 4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pulmonology (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Otolaryngology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)

Abstract

1. Соединение, представляющее собой бензоат N-{2-[((2S)-3-{[1-(4-хлорбензил)пиперидин-4-ил]амино}-2-гидрокси-2-метилпропил)окси]-4-гидроксифенил}ацетамида или его сольват. ! 2. Соединение по п.1, являющееся безводным. ! 3. Соединение по п.2, демонстрирующее по меньшей мере следующие характеристические пики дифракции рентгеновских лучей на порошке (выраженные в градусах 2θ): ! (1) 6,1, 10,7 и 19,3, или ! (2) 6,1, 12,2 и 14,1, или ! (3) 6,1, 10,7, 12,2, 14,1, 18,1 и 19,3, или ! (4) 6,1, 10,7, 12,2, 14,1, 15,7, 18,1 и 19,3, или ! (5) 6,1, 10,7, 12,2, 14,1, 15,1 и 19,3, или ! (6) 6,1, 10,7, 12,2, 14,1, 15,1, 15,7, 18,1 и 19,3, или ! (7) 6,1, 10,7, 12,2, 14,1, 15,1, 15,7, 18,1, 19,3, 21,2 и 24,6. ! 4. По существу, чистое соединение по п.3, имеющее, по существу, такую же картину дифракции рентгеновских лучей на порошке, как картина, представленная на Фиг.1. ! 5. Соединение по п.2, демонстрирующее по меньшей мере следующие характеристические пики дифракции рентгеновских лучей на порошке (выраженные в градусах 2θ): ! (1) 6,5, 9,3 и 10,5, или ! (2) 6,5, 9,3, 17,6 и 17,8, или ! (3) 6,5, 9,3, 10,5, 12,0 и 12,4, или ! (4) 6,5, 9,3, 10,5, 12,0, 12,4, 13,0, 13,6, 15,5, 17,6 и 17,8, или ! (5) 6,5, 13,0 и 20,2, или ! (6) 6,5, 9,3, 10,5, 12,0, 12,4, 13,0, 13,6, 15,5, 17,6, 17,8 и 19,2, или ! (7) 6,5, 9,3, 10,5, 12,0, 12,4, 13,0, 13,6, 15,5, 17,6, 17,8, 19,2, 20,2, 22,8 и 26,0, или ! (8) 6,5, 9,3, 10,5, 12,0, 12,4, 13,0, 13,6, 15,5, 17,6, 17,8, 19,2, 20,2, 22,8, 24,2, 26,0 и 30,7. ! 6. По существу, чистое соединение по п.5, имеющее, по существу, такую же картину дифракции рентгеновских лучей на порошке, как картина, представленная на Фиг.2. ! 7. Фармацевтическая композиция, содержащая соединение по любому из пп.1-6 в комбинации с фармацевтически приемлемым адъювантом, разбавителем или носителем. ! 8. Соединение по любому из пп.1-6 или фармацевтическая композиция по п.7 в комбинации с сухим порошковым ингалятором. ! 9. Соединение по любому из пп.1-6 для применения в терапии. ! 10. Применение сое

Claims (13)

1. Соединение, представляющее собой бензоат N-{2-[((2S)-3-{[1-(4-хлорбензил)пиперидин-4-ил]амино}-2-гидрокси-2-метилпропил)окси]-4-гидроксифенил}ацетамида или его сольват.
2. Соединение по п.1, являющееся безводным.
3. Соединение по п.2, демонстрирующее по меньшей мере следующие характеристические пики дифракции рентгеновских лучей на порошке (выраженные в градусах 2θ):
(1) 6,1, 10,7 и 19,3, или
(2) 6,1, 12,2 и 14,1, или
(3) 6,1, 10,7, 12,2, 14,1, 18,1 и 19,3, или
(4) 6,1, 10,7, 12,2, 14,1, 15,7, 18,1 и 19,3, или
(5) 6,1, 10,7, 12,2, 14,1, 15,1 и 19,3, или
(6) 6,1, 10,7, 12,2, 14,1, 15,1, 15,7, 18,1 и 19,3, или
(7) 6,1, 10,7, 12,2, 14,1, 15,1, 15,7, 18,1, 19,3, 21,2 и 24,6.
4. По существу, чистое соединение по п.3, имеющее, по существу, такую же картину дифракции рентгеновских лучей на порошке, как картина, представленная на Фиг.1.
5. Соединение по п.2, демонстрирующее по меньшей мере следующие характеристические пики дифракции рентгеновских лучей на порошке (выраженные в градусах 2θ):
(1) 6,5, 9,3 и 10,5, или
(2) 6,5, 9,3, 17,6 и 17,8, или
(3) 6,5, 9,3, 10,5, 12,0 и 12,4, или
(4) 6,5, 9,3, 10,5, 12,0, 12,4, 13,0, 13,6, 15,5, 17,6 и 17,8, или
(5) 6,5, 13,0 и 20,2, или
(6) 6,5, 9,3, 10,5, 12,0, 12,4, 13,0, 13,6, 15,5, 17,6, 17,8 и 19,2, или
(7) 6,5, 9,3, 10,5, 12,0, 12,4, 13,0, 13,6, 15,5, 17,6, 17,8, 19,2, 20,2, 22,8 и 26,0, или
(8) 6,5, 9,3, 10,5, 12,0, 12,4, 13,0, 13,6, 15,5, 17,6, 17,8, 19,2, 20,2, 22,8, 24,2, 26,0 и 30,7.
6. По существу, чистое соединение по п.5, имеющее, по существу, такую же картину дифракции рентгеновских лучей на порошке, как картина, представленная на Фиг.2.
7. Фармацевтическая композиция, содержащая соединение по любому из пп.1-6 в комбинации с фармацевтически приемлемым адъювантом, разбавителем или носителем.
8. Соединение по любому из пп.1-6 или фармацевтическая композиция по п.7 в комбинации с сухим порошковым ингалятором.
9. Соединение по любому из пп.1-6 для применения в терапии.
10. Применение соединения по любому из пп.1-6 в производстве лекарственного средства для лечения заболеваний или состояний человека, при которых полезна модуляция активности хемокинового рецептора 1 (CCR1).
11. Применение соединения по любому из пп.1-6 в производстве лекарственного средства для применения в лечении хронического обструктивного заболевания легких.
12. Применение соединения по любому из пп.1-6 в производстве лекарственного средства для применения в лечении астмы.
13. Способ лечения заболевания дыхательных путей у пациента, страдающего от указанного заболевания или имеющего риск возникновения указанного заболевания, включающий введение этому пациенту терапевтически эффективного количества соединения по любому из пп.1-6 или фармацевтической композиции по п.7.
RU2008105972/04A 2005-08-02 2006-07-31 Новая соль i RU2417220C2 (ru)

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SE0501768 2005-08-02
SE0501768-6 2005-08-02

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RU2008105972A true RU2008105972A (ru) 2009-09-10
RU2417220C2 RU2417220C2 (ru) 2011-04-27

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US (1) US8148405B2 (ru)
EP (1) EP1912943A1 (ru)
JP (1) JP2009503064A (ru)
KR (1) KR20080031369A (ru)
CN (1) CN101238103A (ru)
AR (1) AR055365A1 (ru)
AU (1) AU2006276344B2 (ru)
BR (1) BRPI0614634A2 (ru)
CA (1) CA2617403A1 (ru)
EC (1) ECSP088219A (ru)
IL (1) IL188474A0 (ru)
MX (1) MX2008001113A (ru)
NO (1) NO20081080L (ru)
RU (1) RU2417220C2 (ru)
TW (1) TW200738634A (ru)
UY (1) UY29714A1 (ru)
WO (1) WO2007015666A1 (ru)
ZA (1) ZA200800515B (ru)

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ECSP088219A (es) 2008-03-26
US8148405B2 (en) 2012-04-03
IL188474A0 (en) 2008-04-13
EP1912943A1 (en) 2008-04-23
KR20080031369A (ko) 2008-04-08
CN101238103A (zh) 2008-08-06
JP2009503064A (ja) 2009-01-29
AU2006276344A1 (en) 2007-02-08
AU2006276344B2 (en) 2010-10-07
US20080227817A1 (en) 2008-09-18
MX2008001113A (es) 2008-03-11
UY29714A1 (es) 2007-02-28
TW200738634A (en) 2007-10-16
BRPI0614634A2 (pt) 2011-04-12
WO2007015666A1 (en) 2007-02-08
NO20081080L (no) 2008-02-29
ZA200800515B (en) 2008-12-31
AR055365A1 (es) 2007-08-22
CA2617403A1 (en) 2007-02-08

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