CN107074861A - 作为bet溴结构域抑制剂的9h嘧啶并[4,5‑b]吲哚和相关类似物 - Google Patents

作为bet溴结构域抑制剂的9h嘧啶并[4,5‑b]吲哚和相关类似物 Download PDF

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Publication number
CN107074861A
CN107074861A CN201580023829.6A CN201580023829A CN107074861A CN 107074861 A CN107074861 A CN 107074861A CN 201580023829 A CN201580023829 A CN 201580023829A CN 107074861 A CN107074861 A CN 107074861A
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bases
methyl
indoles
amine
pyrimidos
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Chinese (zh)
Inventor
王绍梦
赵玉军
周冰
安吉洛·阿圭勒
刘柳
白龙川
堂娜·麦凯克伦
孙度新
温波
罗瑞娟
赵婷
阿鲁·钦奈彦
伊尔凡·A·阿桑加尼
珍妮·斯塔基
詹尼弗·林恩·马尔
冉旭
胡杨
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University of Michigan System
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University of Michigan System
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/4353Heterocyclic 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
    • A61K31/437Heterocyclic 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 five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/5381,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic ring systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/12Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains three hetero rings
    • C07D487/14Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
CN201580023829.6A 2014-02-28 2015-02-27 作为bet溴结构域抑制剂的9h嘧啶并[4,5‑b]吲哚和相关类似物 Pending CN107074861A (zh)

Applications Claiming Priority (9)

Application Number Priority Date Filing Date Title
US201461946501P 2014-02-28 2014-02-28
US61/946,501 2014-02-28
US201461950406P 2014-03-10 2014-03-10
US61/950,406 2014-03-10
US201462031640P 2014-07-31 2014-07-31
US62/031,640 2014-07-31
US201462048388P 2014-09-10 2014-09-10
US62/048,388 2014-09-10
PCT/US2015/017908 WO2015131005A1 (en) 2014-02-28 2015-02-27 9h-pyrimido[4,5-b]indoles and related analogs as bet bromodomain inhibitors

Publications (1)

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CN107074861A true CN107074861A (zh) 2017-08-18

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US (2) US9580430B2 (enExample)
EP (1) EP3110818B1 (enExample)
JP (1) JP2017511801A (enExample)
CN (1) CN107074861A (enExample)
AU (1) AU2015222887B2 (enExample)
CA (1) CA2940554A1 (enExample)
WO (1) WO2015131005A1 (enExample)

Cited By (8)

* Cited by examiner, † Cited by third party
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CN109223792A (zh) * 2018-04-24 2019-01-18 李明霞 一种治疗骨关节炎的药物组合物及其制备方法
CN110003204A (zh) * 2019-04-30 2019-07-12 上海勋和医药科技有限公司 一种bet蛋白抑制剂、其制备方法及用途
CN112851678A (zh) * 2019-11-28 2021-05-28 广东医科大学 2,4,7-三取代嘧啶并吲哚化合物抗肿瘤转移作用
CN112851679A (zh) * 2019-11-28 2021-05-28 广东医科大学 2,4,7-三取代嘧啶并吲哚化合物抗肿瘤作用
CN113018301A (zh) * 2019-12-09 2021-06-25 中国科学院大连化学物理研究所 JQ1与Erlotinib组合物在制备治疗肝癌药物中应用和治疗肝癌药物
CN113227095A (zh) * 2018-11-21 2021-08-06 韩国化学研究院 作为irak4抑制剂的新三环化合物
CN114044754A (zh) * 2021-11-23 2022-02-15 贵州大学 一类5-三氟甲基-4-吡唑衍生物的制备方法及其在抑制肿瘤细胞上的应用
CN114845719A (zh) * 2019-12-18 2022-08-02 蒙特利尔大学 作为抗癌化合物的cullin 3连接蛋白kbtbd4的调节剂

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TWI719464B (zh) 2013-03-15 2021-02-21 美商英塞特控股公司 作為bet蛋白抑制劑之三環雜環
US9309246B2 (en) 2013-12-19 2016-04-12 Incyte Corporation Tricyclic heterocycles as BET protein inhibitors
WO2015131005A1 (en) * 2014-02-28 2015-09-03 The Regents Of The University Of Michigan 9h-pyrimido[4,5-b]indoles and related analogs as bet bromodomain inhibitors
KR20240134245A (ko) 2014-04-23 2024-09-06 인사이트 홀딩스 코포레이션 BET 단백질의 저해제로서의 1H-피롤로[2,3-c]피리딘-7(6H)-온 및 피라졸로[3,4-c]피리딘-7(6H)-온
US9527864B2 (en) 2014-09-15 2016-12-27 Incyte Corporation Tricyclic heterocycles as BET protein inhibitors
EP3262045A1 (en) * 2015-02-27 2018-01-03 The Regents of The University of Michigan 9h-pyrimido [4,5-b]indoles as bet bromodomain inhibitors
US9725449B2 (en) * 2015-05-12 2017-08-08 Bristol-Myers Squibb Company Tricyclic compounds as anticancer agents
US20170121347A1 (en) 2015-10-29 2017-05-04 Incyte Corporation Amorphous solid form of a bet protein inhibitor
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EP3412669A4 (en) * 2016-02-05 2019-09-04 Chia Tai Tianqing Pharmaceutical Group Co.,Ltd TRICYCLIC COMPOUND FOR PROTEIN INHIBITOR CONTAINING BROMODOMAINE AND PREPARATION, PHARMACEUTICAL COMPOSITION AND USE THEREOF
KR102387316B1 (ko) 2016-04-06 2022-04-15 더 리젠츠 오브 더 유니버시티 오브 미시간 Mdm2 단백질 분해제
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KR20210038921A (ko) 2018-07-25 2021-04-08 치아타이 티안큉 파마수티컬 그룹 주식회사 브로모도메인 단백질 억제제로서의 설폭시민 화합물과 약학적 조성물 및 이의 의학적 용도
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US20220002816A1 (en) * 2018-11-13 2022-01-06 Center For Cancer Research & Therapeutic Development, Clark Atlanta University Identification of jund target genes for inhibition of prostate cancer cell growth
WO2020106059A1 (ko) * 2018-11-21 2020-05-28 한국화학연구원 Irak4 저해제로서 신규의 삼중고리 화합물
US11254670B2 (en) 2019-01-18 2022-02-22 Nuvation Bio Inc. 1,8-naphthyridinone compounds and uses thereof
KR20210116550A (ko) 2019-01-18 2021-09-27 누베이션 바이오 인크. 아데노신 길항제로서의 헤테로시클릭 화합물
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CN115057859B (zh) * 2022-05-10 2023-07-21 中国人民解放军海军军医大学 一类具有抗肿瘤抗真菌活性的化合物及其应用
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Cited By (10)

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CN109223792A (zh) * 2018-04-24 2019-01-18 李明霞 一种治疗骨关节炎的药物组合物及其制备方法
CN113227095A (zh) * 2018-11-21 2021-08-06 韩国化学研究院 作为irak4抑制剂的新三环化合物
CN110003204A (zh) * 2019-04-30 2019-07-12 上海勋和医药科技有限公司 一种bet蛋白抑制剂、其制备方法及用途
CN112851678A (zh) * 2019-11-28 2021-05-28 广东医科大学 2,4,7-三取代嘧啶并吲哚化合物抗肿瘤转移作用
CN112851679A (zh) * 2019-11-28 2021-05-28 广东医科大学 2,4,7-三取代嘧啶并吲哚化合物抗肿瘤作用
CN112851679B (zh) * 2019-11-28 2022-03-25 广东医科大学 2,4,7-三取代嘧啶并吲哚化合物抗肿瘤作用
CN112851678B (zh) * 2019-11-28 2022-04-19 广东医科大学 2,4,7-三取代嘧啶并吲哚化合物抗肿瘤转移作用
CN113018301A (zh) * 2019-12-09 2021-06-25 中国科学院大连化学物理研究所 JQ1与Erlotinib组合物在制备治疗肝癌药物中应用和治疗肝癌药物
CN114845719A (zh) * 2019-12-18 2022-08-02 蒙特利尔大学 作为抗癌化合物的cullin 3连接蛋白kbtbd4的调节剂
CN114044754A (zh) * 2021-11-23 2022-02-15 贵州大学 一类5-三氟甲基-4-吡唑衍生物的制备方法及其在抑制肿瘤细胞上的应用

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