UA118549C2 - 2,3-дизаміщені похідні 1-ацил-4-аміно-1,2,3,4-тетрагідрохіноліну та їх застосування як інгібіторів бромодомену - Google Patents

2,3-дизаміщені похідні 1-ацил-4-аміно-1,2,3,4-тетрагідрохіноліну та їх застосування як інгібіторів бромодомену

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Publication number
UA118549C2
UA118549C2 UAA201507943A UAA201507943A UA118549C2 UA 118549 C2 UA118549 C2 UA 118549C2 UA A201507943 A UAA201507943 A UA A201507943A UA A201507943 A UAA201507943 A UA A201507943A UA 118549 C2 UA118549 C2 UA 118549C2
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UA
Ukraine
Prior art keywords
4аlkуl
disubstituted
acyl
amino
bromodomain inhibitors
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Application number
UAA201507943A
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English (en)
Inventor
Домінік Ейманз
Стівен Джон Еткінсон
Лі Ендрю Гаррісон
Дейвід Джонатан Герст
Роберт Пітер Ло
Меттью Ліндон
Елікзендер Престон
Джонатан Томас Сіл
Крістофер Роланд Веллавей
Original Assignee
Ґлаксосмітклайн Інтеллекчуал Проперті (№ 2) Лімітед
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Application filed by Ґлаксосмітклайн Інтеллекчуал Проперті (№ 2) Лімітед filed Critical Ґлаксосмітклайн Інтеллекчуал Проперті (№ 2) Лімітед
Publication of UA118549C2 publication Critical patent/UA118549C2/uk

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    • 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
    • A61K31/495—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
    • A—HUMAN NECESSITIES
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    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4375—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
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    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4706—4-Aminoquinolines; 8-Aminoquinolines, e.g. chloroquine, primaquine
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    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
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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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
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    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
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    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom 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
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Abstract

Винахід стосується нових сполук, таких як (2S,3R,4R)-1-ацетил-2-циклопропіл-3-метил-4-((4-метилпіримідин-2-іл)аміно)-1,2,3,4-тетрагідрохінолін-6-карбоксамід, що має структурну формулу (І): , фармацевтичних композицій, які містять такі сполуки, та їх застосування в лікуванні гострого або хронічного аутоімунного та/або запального стану.
UAA201507943A 2013-03-14 2014-03-12 2,3-дизаміщені похідні 1-ацил-4-аміно-1,2,3,4-тетрагідрохіноліну та їх застосування як інгібіторів бромодомену UA118549C2 (uk)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201361781583P 2013-03-14 2013-03-14
US201361882798P 2013-09-26 2013-09-26
PCT/EP2014/054795 WO2014140076A1 (en) 2013-03-14 2014-03-12 2,3-disubstituted 1 -acyl-4-amino-1,2,3,4-tetrahydroquinoline derivatives and their use as bromodomain inhibitors

Publications (1)

Publication Number Publication Date
UA118549C2 true UA118549C2 (uk) 2019-02-11

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US (5) US9637456B2 (uk)
EP (2) EP3511323B1 (uk)
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KR (1) KR101780784B1 (uk)
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AU (1) AU2014230815B2 (uk)
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