CN110088102A - 一种含氮杂环类化合物、其制备方法、药物组合物及应用 - Google Patents

一种含氮杂环类化合物、其制备方法、药物组合物及应用 Download PDF

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CN110088102A
CN110088102A CN201780067845.4A CN201780067845A CN110088102A CN 110088102 A CN110088102 A CN 110088102A CN 201780067845 A CN201780067845 A CN 201780067845A CN 110088102 A CN110088102 A CN 110088102A
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linear
branched
alkyl group
methyl
branched alkyl
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胡永韩
朱久香
蔡冬梅
董平
黄玮
李曼华
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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Luoxin Biotechnology Shanghai Co ltd
Shandong Luoxin Pharmaceutical Group Co Ltd
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    • 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
    • A61K31/437—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
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
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    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with 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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    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
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Abstract

本发明公开了一种含氮杂环类化合物、其制备方法、药物组合物及应用。本发明的如式I所示的含氮杂环类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 (20)

  1. PCT国内申请，权利要求书已公开。
CN201780067845.4A 2016-11-10 2017-11-10 一种含氮杂环类化合物、其制备方法、药物组合物及应用 Pending CN110088102A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN2016109898334 2016-11-10
CN201610989833.4A CN108069958A (zh) 2016-11-10 2016-11-10 一种含氮杂环类化合物、其制备方法、药物组合物及应用
PCT/CN2017/110539 WO2018086604A1 (zh) 2016-11-10 2017-11-10 一种含氮杂环类化合物、其制备方法、药物组合物及应用

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CN110088102A true CN110088102A (zh) 2019-08-02

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CN201780067845.4A Pending CN110088102A (zh) 2016-11-10 2017-11-10 一种含氮杂环类化合物、其制备方法、药物组合物及应用

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UA119848C2 (uk) 2013-03-15 2019-08-27 Інсайт Холдинґс Корпорейшн Трициклічні гетероцикли як інгібітори білків бет
US9309246B2 (en) 2013-12-19 2016-04-12 Incyte Corporation Tricyclic heterocycles as BET protein inhibitors
LT3134403T (lt) 2014-04-23 2020-05-11 Incyte Corporation 1h-pirolo[2,3-c]piridin-7(6h)-onai ir pirazolo[3,4-c]piridin-7(6h)-onai, kaip bet baltymų inhibitoriai
US9527864B2 (en) 2014-09-15 2016-12-27 Incyte Corporation Tricyclic heterocycles as BET protein inhibitors
TW201722966A (zh) 2015-10-29 2017-07-01 英塞特公司 Bet蛋白質抑制劑之非晶固體形式
EP3472157B1 (en) 2016-06-20 2023-04-12 Incyte Corporation Crystalline solid forms of a bet inhibitor
EP3828183A4 (en) 2018-07-25 2022-03-09 Chia Tai Tianqing Pharmaceutical Group Co., Ltd. SULFOXIMINE COMPOUND AS BROMO-DOMAIN INHIBITOR AND PHARMACEUTICAL COMPOSITION AND MEDICAL USE THEREOF
WO2020092638A1 (en) 2018-10-30 2020-05-07 Nuvation Bio Inc. Heterocyclic compounds as bet inhibitors
US20220185808A1 (en) * 2019-03-17 2022-06-16 Shanghai Ringene Biopharma Co., Ltd. Acylaminopyrrolo-pyridone compound, preparation method therefor and use thereof
US11584756B2 (en) 2019-07-02 2023-02-21 Nuvation Bio Inc. Heterocyclic compounds as BET inhibitors
CN112300154B (zh) * 2019-07-31 2023-01-24 上海弘翊生物科技有限公司 一类含氮杂环化合物、其制备方法和用途
CN112625036A (zh) * 2019-10-08 2021-04-09 上海海和药物研究开发股份有限公司 一类具有brd4抑制活性的化合物、其制备方法及用途
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
WO2022033542A1 (zh) * 2020-08-14 2022-02-17 南京明德新药研发有限公司 5元杂芳环并吡啶酮类化合物及其应用
CN115028646B (zh) * 2022-05-31 2023-06-30 山东第一医科大学(山东省医学科学院) 一种含氮杂环类化合物、制备方法及在抗肿瘤制剂中的应用
CN118388401B (zh) * 2024-06-28 2024-08-20 成都凯斯坦生物医药有限公司 一种4-氨基-2-氯烟醛的制备方法

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Application publication date: 20190802