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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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic 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
    • 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
    • A61K31/435—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
    • A61K31/4353—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
    • A61K31/437—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 five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • A61K31/535—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
    • 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
    • A61K31/535—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
    • A61K31/538—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/12—Heterocyclic 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
    • C07D487/14—Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (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)

Publication Number Publication Date
CN107074861A true CN107074861A (zh) 2017-08-18

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

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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
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
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
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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US9580430B2 (en) * 2014-02-28 2017-02-28 The Regents Of The University Of Michigan 9H-pyrimido[4,5-B]indoles and related analogs as BET bromodomain inhibitors
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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
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CN115716827A (zh) 2018-07-25 2023-02-28 正大天晴药业集团股份有限公司 作为溴区结构域蛋白抑制剂的亚氨基砜类化合物、药物组合物及其医药用途
CN113226322A (zh) 2018-10-30 2021-08-06 诺维逊生物股份有限公司 作为bet抑制剂的杂环化合物
WO2020101909A2 (en) * 2018-11-13 2020-05-22 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
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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
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
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
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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