WO2018086585A8 - 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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Publication number
WO2018086585A8
WO2018086585A8 PCT/CN2017/110438 CN2017110438W WO2018086585A8 WO 2018086585 A8 WO2018086585 A8 WO 2018086585A8 CN 2017110438 W CN2017110438 W CN 2017110438W WO 2018086585 A8 WO2018086585 A8 WO 2018086585A8
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Prior art keywords
nitrogen
containing heterocyclic
heterocyclic compounds
applications
preparation
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PCT/CN2017/110438
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English (en)
French (fr)
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WO2018086585A1 (zh
Inventor
胡永韩
蔡冬梅
董平
朱久香
李曼华
董加强
王铁林
Original Assignee
山东罗欣药业集团股份有限公司
罗欣生物科技（上海）有限公司
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Application filed by 山东罗欣药业集团股份有限公司, 罗欣生物科技（上海）有限公司 filed Critical 山东罗欣药业集团股份有限公司
Priority to CN201780067789.4A priority Critical patent/CN110088101A/zh
Publication of WO2018086585A1 publication Critical patent/WO2018086585A1/zh
Publication of WO2018086585A8 publication Critical patent/WO2018086585A8/zh

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
    • 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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/5025—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/44—Iso-indoles; Hydrogenated iso-indoles
    • C07D209/46—Iso-indoles; Hydrogenated iso-indoles with an oxygen atom in position 1
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/44—Iso-indoles; Hydrogenated iso-indoles
    • C07D209/48—Iso-indoles; Hydrogenated iso-indoles with oxygen atoms in positions 1 and 3, e.g. phthalimide
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/78—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 2
    • C07D239/80—Oxygen atoms
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Transplantation (AREA)
  • Pulmonology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)

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II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，发挥特定作用。
PCT/CN2017/110438 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 WO2018086585A1 (zh)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN201780067789.4A CN110088101A (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

Applications Claiming Priority (2)

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CN201610989839.1 2016-11-10
CN201610989839.1A CN108069959A (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

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WO2018086585A1 WO2018086585A1 (zh) 2018-05-17
WO2018086585A8 true WO2018086585A8 (zh) 2018-06-21

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WO (1) WO2018086585A1 (zh)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN108794477A (zh) * 2018-08-06 2018-11-13 华东师范大学 一种n2取代鸟嘌呤类化合物的制备方法
KR20220023343A (ko) * 2019-05-24 2022-03-02 바이오테릭스, 인코포레이티드 단백질 표적 화합물, 이의 약학 조성물 및 이들의 치료적 적용
CN112079829B (zh) * 2019-06-14 2021-11-26 四川大学 1,2,4-三氮唑并[4,3-a]吡啶类衍生物及其制备方法和用途
CN110183372B (zh) * 2019-06-20 2020-10-30 山东大学 靛红类化合物及其制备方法和应用
CN110272418B (zh) * 2019-07-25 2020-10-16 山东大学 三氮唑类化合物及其制备方法和应用
CN113754541A (zh) * 2020-06-02 2021-12-07 深圳湾实验室 靶向eb病毒核抗原蛋白的小分子抑制剂、制备方法及其应用
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
CN112225741B (zh) * 2020-12-09 2021-03-30 中山大学 1,2,4三唑并4,3-b哒嗪衍生物在制备抗炎症因子风暴药物中的应用
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
CN115557954B (zh) * 2022-11-11 2024-06-11 上海泰坦科技股份有限公司 一种6-溴-[1,2,4]三唑并[4,3-b]哒嗪的制备方法

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Publication number Priority date Publication date Assignee Title
MX2014012635A (es) * 2012-04-20 2015-05-15 Abbvie Inc Derivados de isoindolona.
AU2014249025A1 (en) * 2013-03-11 2015-09-17 Abbvie Inc. Bromodomain inhibitors
PL3290407T3 (pl) * 2013-10-18 2020-09-07 Celgene Quanticel Research, Inc Inhibitory bromodomen
CN105254635A (zh) * 2015-10-30 2016-01-20 中国药科大学 一类咪唑并吡嗪类化合物及其药物组合物和用途

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CN110088101A (zh) 2019-08-02
CN108069959A (zh) 2018-05-25

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