CN110177784A - 一种含芳环化合物、其制备方法、药物组合物及应用 - Google Patents

一种含芳环化合物、其制备方法、药物组合物及应用 Download PDF

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CN110177784A
CN110177784A CN201880007037.3A CN201880007037A CN110177784A CN 110177784 A CN110177784 A CN 110177784A CN 201880007037 A CN201880007037 A CN 201880007037A CN 110177784 A CN110177784 A CN 110177784A
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base
hetero atom
methyl
yuan
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胡永韩
蔡冬梅
朱久香
董平
李曼华
林凯文
董加强
王铁林
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Luoxin Biotechnology Shanghai Co ltd
Shandong Luoxin Pharmaceutical Group Co Ltd
Shandong Luoxin Pharmaceutical Co Ltd
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Shandong Luoxin Pharmaceutical Group Co Ltd
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Abstract

本发明公开了一种含芳环化合物、其制备方法、药物组合物及应用。本发明提供了一种如式1所示的含芳环的化合物、其药学上可接受的盐、其立体异构体、其互变异构体或其溶剂化物,该化合物可有效地结合BET家族BRD4、BRD3、BRD2和BRDT的溴结构域,以调控下游基因c‑myc和其相关靶基因的转录,进而调节下游的信号通路,发挥特定作用,包括治疗疾病如炎性疾病、癌症和AIDS;其中部分化合物具有很高的活性,并且具有较好的细胞活性和代谢稳定性,因此可以成为治疗肿瘤的有效药物。

Description

PCT国内申请,说明书已公开。

Claims (27)

  1. PCT国内申请,权利要求书已公开。
CN201880007037.3A 2017-01-16 2018-01-16 一种含芳环化合物、其制备方法、药物组合物及应用 Pending CN110177784A (zh)

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CN201710033493.2A CN108314680A (zh) 2017-01-16 2017-01-16 一种含芳环化合物、其制备方法、药物组合物及应用
CN2017100334932 2017-01-16
PCT/CN2018/072872 WO2018130227A1 (zh) 2017-01-16 2018-01-16 一种含芳环化合物、其制备方法、药物组合物及应用

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KR102622152B1 (ko) * 2019-10-31 2024-01-08 홀로스메딕 주식회사 신규한 화합물 및 이를 포함하는 암 예방 또는 치료용 약학 조성물
CN115667254A (zh) * 2020-05-21 2023-01-31 贝达药业股份有限公司 作为溴结构域蛋白质抑制剂的化合物和组合物

Citations (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008089307A2 (en) * 2007-01-18 2008-07-24 Lexicon Pharmaceuticals, Inc. Delta 5 desaturase inhibitors for the treatment of pain, inflammation and cancer
CN104428293A (zh) * 2012-06-11 2015-03-18 Ucb生物制药私人有限公司 调节TNFα的苯并咪唑类
US20150158854A1 (en) * 2013-12-11 2015-06-11 Development Center For Biotechnology Quinazoline compounds, method for preparing the same and use thereof
CN105073747A (zh) * 2013-03-15 2015-11-18 普莱希科公司 杂环化合物及其应用
CN105324379A (zh) * 2013-05-09 2016-02-10 吉里德科学公司 作为溴结构域抑制剂的苯并咪唑衍生物
CN105407894A (zh) * 2013-03-14 2016-03-16 康威基内有限公司 用于抑制含布罗莫结构域的蛋白质的方法和组合物
CN105407888A (zh) * 2013-06-21 2016-03-16 齐尼思表观遗传学公司 新双环溴结构域抑制剂
TW201613911A (en) * 2014-09-15 2016-04-16 Plexxikon Inc Heterocyclic compounds and uses thereof
WO2016097870A1 (en) * 2014-12-17 2016-06-23 Zenith Epigenetics Corp. Substituted bicyclic compounds as bromodomain inhibitors
CN105814052A (zh) * 2013-12-09 2016-07-27 Ucb生物制药私人有限公司 作为tnf活性调节剂的咪唑并吡啶衍生物
WO2016168682A2 (en) * 2015-04-15 2016-10-20 Celgene Quanticel Research, Inc. Bromodomain inhibitor
WO2017091661A1 (en) * 2015-11-25 2017-06-01 Strovel Jeffrey William Bicyclic bet bromodomain inhibitors and uses thereof
WO2017106630A1 (en) * 2015-12-18 2017-06-22 The General Hospital Corporation Polyacetal polymers, conjugates, particles and uses thereof

Patent Citations (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008089307A2 (en) * 2007-01-18 2008-07-24 Lexicon Pharmaceuticals, Inc. Delta 5 desaturase inhibitors for the treatment of pain, inflammation and cancer
CN104428293A (zh) * 2012-06-11 2015-03-18 Ucb生物制药私人有限公司 调节TNFα的苯并咪唑类
CN105407894A (zh) * 2013-03-14 2016-03-16 康威基内有限公司 用于抑制含布罗莫结构域的蛋白质的方法和组合物
CN105073747A (zh) * 2013-03-15 2015-11-18 普莱希科公司 杂环化合物及其应用
CN105324379A (zh) * 2013-05-09 2016-02-10 吉里德科学公司 作为溴结构域抑制剂的苯并咪唑衍生物
CN105407888A (zh) * 2013-06-21 2016-03-16 齐尼思表观遗传学公司 新双环溴结构域抑制剂
CN105814052A (zh) * 2013-12-09 2016-07-27 Ucb生物制药私人有限公司 作为tnf活性调节剂的咪唑并吡啶衍生物
US20150158854A1 (en) * 2013-12-11 2015-06-11 Development Center For Biotechnology Quinazoline compounds, method for preparing the same and use thereof
TW201613911A (en) * 2014-09-15 2016-04-16 Plexxikon Inc Heterocyclic compounds and uses thereof
WO2016097870A1 (en) * 2014-12-17 2016-06-23 Zenith Epigenetics Corp. Substituted bicyclic compounds as bromodomain inhibitors
WO2016168682A2 (en) * 2015-04-15 2016-10-20 Celgene Quanticel Research, Inc. Bromodomain inhibitor
WO2017091661A1 (en) * 2015-11-25 2017-06-01 Strovel Jeffrey William Bicyclic bet bromodomain inhibitors and uses thereof
WO2017106630A1 (en) * 2015-12-18 2017-06-22 The General Hospital Corporation Polyacetal polymers, conjugates, particles and uses thereof

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
COLUMBUS,OHIO,US: "REGISTRY[Online]", 《REGISTRY》 *
DUNCAN HAY ET AL.: "The Design and Synthesis of 5- and 6-isoxazolylbenzimidazoles as Selective Inhibitors of the BET Bromodomains", 《MED. CHEM. COMM.》 *

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Application publication date: 20190827