EA201791973A1 - Производные бензимидазола в качестве ингибиторов бромодомена - Google Patents

Производные бензимидазола в качестве ингибиторов бромодомена

Info

Publication number
EA201791973A1
EA201791973A1 EA201791973A EA201791973A EA201791973A1 EA 201791973 A1 EA201791973 A1 EA 201791973A1 EA 201791973 A EA201791973 A EA 201791973A EA 201791973 A EA201791973 A EA 201791973A EA 201791973 A1 EA201791973 A1 EA 201791973A1
Authority
EA
Eurasian Patent Office
Prior art keywords
benzimidazole
derivatives
bromodomain inhibitors
salts
compounds
Prior art date
Application number
EA201791973A
Other languages
English (en)
Other versions
EA033594B1 (ru
Inventor
Рино Антонио Бит
Джон Александер Браун
Филип Дж. Хамфрис
Кэтрин Луис Джонс
Original Assignee
Глаксосмитклайн Интеллекчуал Проперти Дивелопмент Лимитед
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Глаксосмитклайн Интеллекчуал Проперти Дивелопмент Лимитед filed Critical Глаксосмитклайн Интеллекчуал Проперти Дивелопмент Лимитед
Publication of EA201791973A1 publication Critical patent/EA201791973A1/ru
Publication of EA033594B1 publication Critical patent/EA033594B1/ru

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Classifications

    • 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
    • A61P35/00—Antineoplastic agents
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—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
    • 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
    • C07D401/04—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—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
    • C07D401/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • 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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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Engineering & Computer Science (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Epidemiology (AREA)

Abstract

Соединения формулы (I) и их соли, где R, R, R, Rявляются такими, как определено в данной заявке. Было обнаружено, что соединения формулы (I) и их соли ингибируют связывание семейства BET из бромодоменовых белков, например, с ацетилированными лизиновыми остатками, и таким образом могут использоваться в терапии, например, в лечении аутоиммунных и воспалительных заболеваний, таких как ревматоидный артрит, и раковых заболеваний.
EA201791973A 2015-03-19 2016-03-17 Производные бензимидазола в качестве ингибиторов бромодомена EA033594B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GBGB1504689.9A GB201504689D0 (en) 2015-03-19 2015-03-19 Chemical compounds
PCT/EP2016/055792 WO2016146738A1 (en) 2015-03-19 2016-03-17 Benzimidazole derivatives as bromodomain inhibitors

Publications (2)

Publication Number Publication Date
EA201791973A1 true EA201791973A1 (ru) 2018-07-31
EA033594B1 EA033594B1 (ru) 2019-11-07

Family

ID=53052091

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201791973A EA033594B1 (ru) 2015-03-19 2016-03-17 Производные бензимидазола в качестве ингибиторов бромодомена

Country Status (35)

Country Link
US (2) US10442786B2 (ru)
EP (2) EP3549939A1 (ru)
JP (1) JP6419990B2 (ru)
KR (1) KR102072850B1 (ru)
CN (1) CN107635989B (ru)
AR (1) AR103934A1 (ru)
AU (1) AU2016232217B2 (ru)
BR (1) BR112017019779B1 (ru)
CA (1) CA2979504C (ru)
CL (1) CL2017002332A1 (ru)
CO (1) CO2017009992A2 (ru)
CR (1) CR20170430A (ru)
CY (1) CY1121855T1 (ru)
DK (1) DK3271349T3 (ru)
DO (1) DOP2017000213A (ru)
EA (1) EA033594B1 (ru)
ES (1) ES2735417T3 (ru)
GB (1) GB201504689D0 (ru)
HR (1) HRP20191186T1 (ru)
HU (1) HUE044414T2 (ru)
IL (1) IL254318B (ru)
LT (1) LT3271349T (ru)
MA (2) MA46981A (ru)
ME (1) ME03485B (ru)
MX (1) MX2017012023A (ru)
PE (1) PE20180032A1 (ru)
PH (1) PH12017501620A1 (ru)
PL (1) PL3271349T3 (ru)
PT (1) PT3271349T (ru)
RS (1) RS59056B1 (ru)
SG (1) SG11201707356QA (ru)
SI (1) SI3271349T1 (ru)
TW (1) TW201706257A (ru)
UY (1) UY36589A (ru)
WO (1) WO2016146738A1 (ru)

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GB201504689D0 (en) * 2015-03-19 2015-05-06 Glaxosmithkline Ip Dev Ltd Chemical compounds
WO2017024406A1 (en) 2015-08-11 2017-02-16 Neomed Institute N-substituted bicyclic lactams, their preparation and their use as pharmaceuticals
JP2018527340A (ja) 2015-08-11 2018-09-20 ネオメド インスティテュートＮｅｏｍｅｄ Ｉｎｓｔｉｔｕｔｅ アリール置換ジヒドロキノリノン、その調製及び医薬品としてのその使用
KR20180039669A (ko) 2015-08-12 2018-04-18 네오메드 인스티튜트 치환된 벤즈이미다졸, 그의 제조법 및 제약으로서의 그의 용도
WO2017066876A1 (en) 2015-10-21 2017-04-27 Neomed Institute Substituted imidazopyridines, their preparation and their use as pharmaceuticals
WO2017127930A1 (en) 2016-01-28 2017-08-03 Neomed Institute Substituted [1,2,4]triazolo[4,3-a]pyridines, their preparation and their use as pharmaceuticals
GB201614939D0 (en) 2016-09-02 2016-10-19 Glaxosmithkline Ip Dev Ltd Crystalline hydrate
GB201614934D0 (en) * 2016-09-02 2016-10-19 Glaxosmithkline Intellectual Property (No 2) Ltd Chemical compounds
GB201614940D0 (en) * 2016-09-02 2016-10-19 Glaxosmithkline Intellectual Property (No 2) Ltd Chemical compounds
WO2018195155A1 (en) 2017-04-18 2018-10-25 Celgene Quanticel Research, Inc. Therapeutic compounds
CN109280046B (zh) * 2017-07-21 2021-02-02 浙江海正药业股份有限公司 苯并咪唑类衍生物及其制备方法及其在医药上的用途
JP2021512960A (ja) * 2018-02-06 2021-05-20 シャンハイ ハイファ ファーマシューティカル カンパニー，リミティッド Ｂｅｔ阻害活性を有する化合物並びにその製造方法及び使用
CN109369432B (zh) * 2018-11-02 2021-06-25 永农生物科学有限公司 (s)-4-氯-2-氨基丁酸酯的制备方法
JP2022053557A (ja) * 2019-02-08 2022-04-06 マルホ株式会社 ピリドン誘導体
WO2020190780A1 (en) * 2019-03-15 2020-09-24 Forma Therapeutics, Inc. Inhibiting cyclic amp-responsive element-binding protein (creb)
WO2020219168A1 (en) * 2019-04-24 2020-10-29 Convergene, Llc Small molecule bromodomain inhibitors and uses thereof
WO2020223370A1 (en) * 2019-04-29 2020-11-05 The Board Of Regents Of The University Of Texas System Compositions and methods for treating schistosoma infections

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GB201614939D0 (en) * 2016-09-02 2016-10-19 Glaxosmithkline Ip Dev Ltd Crystalline hydrate

Also Published As

Publication number Publication date
PL3271349T3 (pl) 2019-10-31
CN107635989B (zh) 2020-12-08
HRP20191186T1 (hr) 2019-10-04
EA033594B1 (ru) 2019-11-07
MA41778A (fr) 2018-01-24
PE20180032A1 (es) 2018-01-09
CN107635989A (zh) 2018-01-26
DOP2017000213A (es) 2017-10-15
HUE044414T2 (hu) 2019-10-28
CO2017009992A2 (es) 2018-01-05
PH12017501620A1 (en) 2018-02-12
KR20170129871A (ko) 2017-11-27
KR102072850B1 (ko) 2020-02-03
BR112017019779B1 (pt) 2023-10-03
CA2979504A1 (en) 2016-09-22
CR20170430A (es) 2017-11-08
AU2016232217A1 (en) 2017-10-12
EP3271349A1 (en) 2018-01-24
JP2018507903A (ja) 2018-03-22
DK3271349T3 (da) 2019-08-05
LT3271349T (lt) 2019-07-10
WO2016146738A1 (en) 2016-09-22
JP6419990B2 (ja) 2018-11-07
ME03485B (me) 2020-01-20
AU2016232217B2 (en) 2019-04-04
US10442786B2 (en) 2019-10-15
IL254318A0 (en) 2017-11-30
SI3271349T1 (sl) 2019-08-30
CL2017002332A1 (es) 2018-03-16
BR112017019779A2 (pt) 2018-05-22
EP3549939A1 (en) 2019-10-09
US20180044317A1 (en) 2018-02-15
UY36589A (es) 2016-10-31
US20200039953A1 (en) 2020-02-06
TW201706257A (zh) 2017-02-16
CA2979504C (en) 2023-10-10
US11053212B2 (en) 2021-07-06
PT3271349T (pt) 2019-08-19
CY1121855T1 (el) 2020-07-31
ES2735417T3 (es) 2019-12-18
MX2017012023A (es) 2018-01-30
AR103934A1 (es) 2017-06-14
EP3271349B1 (en) 2019-05-15
IL254318B (en) 2019-08-29
GB201504689D0 (en) 2015-05-06
RS59056B1 (sr) 2019-08-30
MA46981A (fr) 2019-10-09
SG11201707356QA (en) 2017-10-30

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MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM KG TM

MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AZ BY KZ TJ RU