EA026371B1 - Индолкарбонитрилы в качестве модуляторов рецептора андрогенов - Google Patents

Индолкарбонитрилы в качестве модуляторов рецептора андрогенов Download PDF

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EA026371B1
EA026371B1 EA201492237A EA201492237A EA026371B1 EA 026371 B1 EA026371 B1 EA 026371B1 EA 201492237 A EA201492237 A EA 201492237A EA 201492237 A EA201492237 A EA 201492237A EA 026371 B1 EA026371 B1 EA 026371B1
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muscle atrophy
compound according
atrophy associated
compound
accelerating
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Филип Стюарт ТЕРНБУЛЛ
Родольфо Кадилла
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Глаксосмитклайн Интеллекчуал Проперти (№ 2) Дивелопмент Лимитед
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    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/18—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D209/24—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with an alkyl or cycloalkyl radical attached to the ring nitrogen atom
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    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
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    • 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
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
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    • C07D—HETEROCYCLIC COMPOUNDS
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    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
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    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
    • C07D209/42—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals

Abstract

Изобретение относится к нестероидным соединениям, которые являются модуляторами рецептора андрогенов, а также к способам получения и применения таких соединений.

Description

(54) ИНДОЛКАРБОНИТРИЛЫ В КАЧЕСТВЕ МОДУЛЯТОРОВ РЕЦЕПТОРА АНДРОГЕНОВ (31) 61/672,455; 61/748,874 (32) 2012.07.17; 2013.01.04 (33) ϋδ (43) 2015.06.30 (86) РСТДВ2013/001530 (87) \ΥΟ 2014/013309 2014.01.23 (71) (73) Заявитель и патентовладелец:
ГЛАКСОСМИТКЛАЙН ИНТЕЛЛЕКЧУАЛ ПРОПЕРТИ (№ 2) ДИВЕЛОПМЕНТ ЛИМИТЕД (СВ) (72) Изобретатель:
Тернбулл Филип Стюарт, Кадилла Родольфо (ϋδ) (74) Представитель:
Поликарпов А.В. (Κϋ) (56) \¥О-А1-2012097744 АУО-А2-2008042571 \¥0-А1-2010118287 ΥΥΟ-Α2-2007108936 АУО-А1-2005118539 υδ-Α1-2005222148
026371 В1 (57) Изобретение относится к нестероидным соединениям, которые являются модуляторами рецептора андрогенов, а также к способам получения и применения таких соединений.
026371 Β1

Claims (10)

  1. ФОРМУЛА ИЗОБРЕТЕНИЯ
    1. Соединение
  2. 2. Фармацевтическая композиция для лечения расстройств, опосредованных андрогенной активностью, содержащая соединение по п.1 и один или более фармацевтически приемлемых эксципиентов.
    - 42 026371
  3. 3. Способ лечения расстройства, выбранного из мышечной атрофии, ассоциированной с хроническим обструктивным заболеванием легких (СОРЭ), мышечной атрофии, ассоциированной с хроническим заболеванием почек (СКЭ), мышечной атрофии, ассоциированной с хронической сердечной недостаточностью (СИР), и недержания мочи, включающий введение соединения по п. 1 субъекту-человеку.
  4. 4. Применение соединения по п.1 в изготовлении лекарственного средства для лечения расстройства, выбранного из мышечной атрофии, ассоциированной с хроническим обструктивным заболеванием легких (СОРЭ), мышечной атрофии, ассоциированной с хроническим заболеванием почек (СКЭ), мышечной атрофии, ассоциированной с хронической сердечной недостаточностью (СЫР), и недержания мочи.
  5. 5. Способ ускорения репарации и заживления перелома костей тазобедренного сустава, включающий введение соединения по п. 1 субъекту-человеку.
  6. 6. Применение соединения по п.1 в изготовлении лекарственного средства для ускорения репарации и заживления перелома костей тазобедренного сустава.
  7. 7. Способ ускорения заживления ожога, включающий введение соединения по п.1 субъектучеловеку.
  8. 8. Применение соединения по п.1 в изготовлении лекарственного средства для ускорения заживления ожога.
  9. 9. Фармацевтическая композиция по п.2, содержащая 0,1-50 мг соединения.
  10. 10. Способ по любому из пп.3, 5 или 7, при котором вводят 0,1-50 мг соединения.
EA201492237A 2012-07-17 2013-07-15 Индолкарбонитрилы в качестве модуляторов рецептора андрогенов EA026371B8 (ru)

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US201261672455P 2012-07-17 2012-07-17
US201361748874P 2013-01-04 2013-01-04
PCT/IB2013/001530 WO2014013309A1 (en) 2012-07-17 2013-07-15 Indolecarbonitriles as selective androgen receptor modulators

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