EA201590581A1 - Соединения бис-(фторалкил)-1,4-бензодиазепинона и их пролекарства - Google Patents

Соединения бис-(фторалкил)-1,4-бензодиазепинона и их пролекарства

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Publication number
EA201590581A1
EA201590581A1 EA201590581A EA201590581A EA201590581A1 EA 201590581 A1 EA201590581 A1 EA 201590581A1 EA 201590581 A EA201590581 A EA 201590581A EA 201590581 A EA201590581 A EA 201590581A EA 201590581 A1 EA201590581 A1 EA 201590581A1
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EA
Eurasian Patent Office
Prior art keywords
compounds
fluoroalkyl
bis
treatment
benzodiazepinone compounds
Prior art date
Application number
EA201590581A
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English (en)
Other versions
EA027281B1 (ru
Inventor
Ашвиникумар В. Гаваи
Джордж В. Делукка
Даниэль О'Мэлли
Патрис Гилл
Клауд А. Куэснел
Брайан Е. Финк
Юфэнь Чжао
Фрэнсис Ю. Ли
Original Assignee
Бристол-Майерс Сквибб Компани
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Application filed by Бристол-Майерс Сквибб Компани filed Critical Бристол-Майерс Сквибб Компани
Publication of EA201590581A1 publication Critical patent/EA201590581A1/ru
Publication of EA027281B1 publication Critical patent/EA027281B1/ru

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D243/00—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
    • C07D243/06—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4
    • C07D243/10—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
    • C07D243/14—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines
    • C07D243/16—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines substituted in position 5 by aryl radicals
    • C07D243/18—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines substituted in position 5 by aryl radicals substituted in position 2 by nitrogen, oxygen or sulfur atoms
    • C07D243/24—Oxygen atoms
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    • A61K31/13—Amines
    • A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
    • A61K31/138—Aryloxyalkylamines, e.g. propranolol, tamoxifen, phenoxybenzamine
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    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/337—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
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    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • A61K31/5513—1,4-Benzodiazepines, e.g. diazepam or clozapine
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    • A61K31/57—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
    • A61K31/573—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D243/00—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
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    • C07D243/10—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
    • C07D243/14—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines
    • C07D243/16—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines substituted in position 5 by aryl radicals
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    • C07D243/10—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
    • C07D243/14—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines
    • C07D243/16—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines substituted in position 5 by aryl radicals
    • C07D243/18—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines substituted in position 5 by aryl radicals substituted in position 2 by nitrogen, oxygen or sulfur atoms
    • C07D243/24—Oxygen atoms
    • C07D243/26—Preparation from compounds already containing the benzodiazepine skeleton
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    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
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  • Gastroenterology & Hepatology (AREA)
  • Immunology (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Compounds Containing Sulfur Atoms (AREA)

Abstract

Изобретение относится к соединениям формулы (I) и/или их солямгде Rпредставляет собой -CHCHCF; Rпредставляет собой -CHCHCFили -CHCHCHCF; Rпредставляет собой Н, -СНили R; Rпредставляет собой Н или R; кольцо А представляет собой фенил или пиридинил; и R, R, R, R, у и z являются такими, как определено в данном документе. Также описаны способы применения таких соединений для ингибирования Notch рецептора и фармацевтические композиции, содержащие такие соединения. Эти соединения используются для лечения, предупреждения или замедления развития болезни или расстройства в различных разделах медицины, таких как раковые опухоли; или как пролекарства этих соединений.
EA201590581A 2012-09-21 2013-09-20 Соединения бис (фторалкил)-1,4-бензодиазепинона в качестве ингибиторов notch EA027281B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201261703912P 2012-09-21 2012-09-21
PCT/US2013/060790 WO2014047372A1 (en) 2012-09-21 2013-09-20 Bis(fluoroalkyl)-1,4-benzodiazepinone compounds as notch inhibitors

Publications (2)

Publication Number Publication Date
EA201590581A1 true EA201590581A1 (ru) 2015-07-30
EA027281B1 EA027281B1 (ru) 2017-07-31

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US (2) US8999918B2 (ru)
EP (1) EP2897945B1 (ru)
JP (1) JP6165255B2 (ru)
KR (1) KR102155588B1 (ru)
CN (1) CN104703976B (ru)
AR (1) AR093767A1 (ru)
AU (1) AU2013317923B2 (ru)
BR (1) BR112015005817B1 (ru)
CA (1) CA2885574C (ru)
CL (1) CL2015000711A1 (ru)
CO (1) CO7310522A2 (ru)
CY (1) CY1118739T1 (ru)
DK (1) DK2897945T3 (ru)
EA (1) EA027281B1 (ru)
ES (1) ES2617591T3 (ru)
HR (1) HRP20170352T8 (ru)
HU (1) HUE032038T2 (ru)
IL (1) IL237782A (ru)
LT (1) LT2897945T (ru)
MA (1) MA37929B1 (ru)
MX (1) MX367474B (ru)
MY (1) MY185233A (ru)
NZ (1) NZ707171A (ru)
PE (1) PE20150622A1 (ru)
PH (1) PH12015500414B1 (ru)
PL (1) PL2897945T3 (ru)
PT (1) PT2897945T (ru)
RS (1) RS55779B1 (ru)
SG (1) SG11201501573UA (ru)
SI (1) SI2897945T1 (ru)
TN (1) TN2015000102A1 (ru)
TW (1) TWI614238B (ru)
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WO (1) WO2014047372A1 (ru)

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JP2015534554A (ja) 2012-09-21 2015-12-03 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ アルキル，フルオロアルキル−１，４−ベンゾジアゼピノン化合物
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CN104797584A (zh) 2012-09-21 2015-07-22 百时美施贵宝公司 作为notch抑制剂的三环杂环化合物
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KR20220007050A (ko) 2019-04-08 2022-01-18 프리퀀시 테라퓨틱스, 인크. 난청을 치료하기 위한 chir99021과 발프로산의 조합
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