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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cycloalkyl
aryl
heterocyclyl
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CN112351778A (zh
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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)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Virology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Molecular Biology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • AIDS & HIV (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

Publications (2)

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

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

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ES2929415T3 (es) 2018-05-25 2022-11-29 Incyte Corp Compuestos heterocíclicos tricíclicos como activadores de STING
WO2020028565A1 (en) 2018-07-31 2020-02-06 Incyte Corporation Tricyclic heteraryl compounds as sting activators
US10875872B2 (en) 2018-07-31 2020-12-29 Incyte Corporation Heteroaryl amide compounds as sting activators
CN112552314B (zh) * 2018-08-24 2022-03-04 杭州阿诺生物医药科技有限公司 Sting激动剂小分子抗肿瘤化合物及其应用
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
WO2020124059A1 (en) * 2018-12-14 2020-06-18 Eternity Bioscience Inc. Tricyclic compounds as sting agonists, and preparation methods and medicinal uses thereof
US12129267B2 (en) 2019-01-07 2024-10-29 Incyte Corporation Heteroaryl amide compounds as sting activators
US11155567B2 (en) 2019-08-02 2021-10-26 Mersana Therapeutics, Inc. Sting agonist compounds and methods of use
MY210304A (en) 2020-04-02 2025-09-10 Mersana Therapeutics Inc Antibody drug conjugates comprising sting agonists
US20230141284A1 (en) 2020-04-10 2023-05-11 Ono Pharmaceutical Co., Ltd. Cancer therapeutic method
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

Family Cites Families (12)

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Publication number Priority date Publication date Assignee Title
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
CA2332239A1 (en) 1998-05-15 1999-11-25 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
JP2009503069A (ja) 2005-08-05 2009-01-29 アストラゼネカ アクチボラグ 三環式ベンゾイミダゾール類、および代謝性グルタミン酸塩受容体のモジュレータとしてのそれらの使用
US20110262485A1 (en) 2008-08-04 2011-10-27 University Of Miami Sting (stimulator of interferon genes), a regulator of innate immune responses
CA2825028A1 (en) * 2011-02-09 2012-08-16 F. Hoffman-La Roche Ag Heterocyclic compounds as pi3 kinase inhibitors
CN104540945A (zh) 2012-04-30 2015-04-22 格伦·N·巴伯 调节免疫应答
US9527864B2 (en) * 2014-09-15 2016-12-27 Incyte Corporation Tricyclic heterocycles as BET protein inhibitors
SI3440076T1 (sl) 2016-04-07 2022-09-30 Glaxosmithkline Intellectual Property Development Limited Heterociklični amidi uporabni kot proteinski modulatorji
CN109563081A (zh) 2016-04-07 2019-04-02 葛兰素史克知识产权开发有限公司 可用作蛋白调节剂的杂环酰胺类

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

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