CN112351778B - 稠合三环杂环类化合物及其治疗用途 - Google Patents

稠合三环杂环类化合物及其治疗用途 Download PDF

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Publication number
CN112351778B
CN112351778B CN201980043105.6A CN201980043105A CN112351778B CN 112351778 B CN112351778 B CN 112351778B CN 201980043105 A CN201980043105 A CN 201980043105A CN 112351778 B CN112351778 B CN 112351778B
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alkyl
cycloalkyl
aryl
heterocyclyl
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CN112351778A (zh
Inventor
刘�东
陈磊
庄凌航
李璞慧
张鑫竹
宋春英
马修·米勒
胡齐悦
闫玉娜
贺峰
陶维康
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Jiangsu Hengrui Medicine Co Ltd
Shanghai Hengrui Pharmaceutical Co Ltd
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Jiangsu Hengrui Medicine Co Ltd
Shanghai Hengrui Pharmaceutical Co Ltd
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/06Peri-condensed systems
    • 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
    • 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
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • A61K31/5365Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • A61K31/53831,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • 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
    • C07D487/06Peri-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
    • C07D487/16Peri-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/16Peri-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Virology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Rheumatology (AREA)
  • Molecular Biology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • AIDS & HIV (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
CN201980043105.6A 2018-06-28 2019-06-28 稠合三环杂环类化合物及其治疗用途 Active CN112351778B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201862691208P 2018-06-28 2018-06-28
US62/691,208 2018-06-28
PCT/US2019/039860 WO2020006432A1 (en) 2018-06-28 2019-06-28 Fused tricyclic heterocycle compounds and therapeutic uses thereof

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CN112351778A CN112351778A (zh) 2021-02-09
CN112351778B true CN112351778B (zh) 2023-04-04

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US (1) US11535633B2 (https=)
EP (1) EP3813827A4 (https=)
JP (1) JP2021530442A (https=)
KR (1) KR20210025016A (https=)
CN (1) CN112351778B (https=)
TW (1) TW202019408A (https=)
WO (1) WO2020006432A1 (https=)

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JP7570235B2 (ja) 2018-05-25 2024-10-21 インサイト・コーポレイション Sting活性化剤としての三環式複素環式化合物
WO2020028566A1 (en) 2018-07-31 2020-02-06 Incyte Corporation Heteroaryl amide compounds as sting activators
US11008344B2 (en) 2018-07-31 2021-05-18 Incyte Corporation Tricyclic heteroaryl compounds as STING activators
AU2019326633B2 (en) * 2018-08-24 2022-09-08 Adlai Nortye Biopharma Co., Ltd. High activity sting protein agonist
CN111655682B (zh) * 2018-08-29 2024-05-31 杭州阿诺生物医药科技有限公司 一种高活性sting蛋白激动剂化合物
US11596692B1 (en) 2018-11-21 2023-03-07 Incyte Corporation PD-L1/STING conjugates and methods of use
US20220056044A1 (en) * 2018-12-14 2022-02-24 Jiangsu Hengrui Medicine Co., Ltd. Tricyclic compounds as sting agonists, and preparation methods and medicinal uses thereof
WO2020146237A1 (en) 2019-01-07 2020-07-16 Incyte Corporation Heteroaryl amide compounds as sting activators
JP7843695B2 (ja) 2019-08-02 2026-04-10 メルサナ セラピューティクス インコーポレイテッド がんの処置用のSTING(インターフェロン遺伝子刺激因子)アゴニストとしてのビス-[N-((5-カルバモイル)-1H-ベンゾ[d]イミダゾール-2-イル)-ピラゾール-5-カルボキサミド]誘導体および関連化合物
IL296901A (en) 2020-04-02 2022-12-01 Mersana Therapeutics Inc Antibody-drug conjugates comprising sting agonists
TW202200136A (zh) 2020-04-10 2022-01-01 日商小野藥品工業股份有限公司 癌治療方法
CN115554303B (zh) * 2021-09-18 2024-07-09 上海科技大学 一种三环类化合物、其制备方法及其应用
US20250171461A1 (en) * 2022-02-21 2025-05-29 Geode Therapeutics Inc. Stimulator of interferon genes (sting) modulators, and compositions and methods thereof

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FR2731708B1 (fr) * 1995-03-13 1997-04-30 Synthelabo Derives de piperidine, leur procede de preparation et leur application en therapeutique
FR2747678B1 (fr) * 1996-04-22 1998-05-22 Synthelabo Composes derives d'imidazobenzoxazine, leurs procedes de preparation et leurs utilisations en therapeutique
AU9298798A (en) * 1998-05-15 1999-12-06 Guilford Pharmaceuticals Inc. Fused tricyclic compounds which inhibit parp activity
ECSP003637A (es) 1999-08-31 2002-03-25 Agouron Pharma Inhibidores triciclicos de poli (adp-ribosa) polimerasas
CA2324090A1 (en) 1999-10-25 2001-04-25 Leviton Manufacturing Co., Inc. Electrical wiring device with multiple types of wire terminations
US20070032469A1 (en) 2005-08-05 2007-02-08 Astrazeneca Ab Tricyclic benzimidazoles and their use as metabotropic glutamate receptor modulators
JP2011529708A (ja) 2008-08-04 2011-12-15 ユニバーシティ オブ マイアミ 自然免疫応答の調節因子sting(インターフェロン遺伝子の刺激因子)
RU2013138835A (ru) * 2011-02-09 2015-03-20 Ф. Хоффманн-Ля Рош Аг Гетероциклические соединения в качестве ингибиторов pi3 киназы
KR20150004416A (ko) 2012-04-30 2015-01-12 글렌 엔. 바버 면역 반응의 조절
JP6599979B2 (ja) * 2014-09-15 2019-10-30 インサイト・コーポレイション Betタンパク質阻害剤として用いるための三環式複素環化合物
PT3440076T (pt) 2016-04-07 2022-07-29 Glaxosmithkline Ip Dev Ltd Amidas heterocíclicas úteis como modeladores de proteína
JP2019510802A (ja) 2016-04-07 2019-04-18 グラクソスミスクライン、インテレクチュアル、プロパティー、ディベロップメント、リミテッドGlaxosmithkline Intellectual Property Development Limited タンパク質調節物質として有用な複素環アミド

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Publication number Publication date
TW202019408A (zh) 2020-06-01
EP3813827A4 (en) 2022-04-13
JP2021530442A (ja) 2021-11-11
US20210300944A1 (en) 2021-09-30
KR20210025016A (ko) 2021-03-08
US11535633B2 (en) 2022-12-27
WO2020006432A1 (en) 2020-01-02
EP3813827A1 (en) 2021-05-05
CN112351778A (zh) 2021-02-09

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