CN109111464B - 一种具有细胞坏死抑制活性的杂环化合物 - Google Patents

一种具有细胞坏死抑制活性的杂环化合物 Download PDF

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CN109111464B
CN109111464B CN201810575869.7A CN201810575869A CN109111464B CN 109111464 B CN109111464 B CN 109111464B CN 201810575869 A CN201810575869 A CN 201810575869A CN 109111464 B CN109111464 B CN 109111464B
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synthesis
alkyl
cycloalkyl
room temperature
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Chinese (zh)
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CN109111464A (zh
Inventor
张小虎
马海阔
何苏丹
郑计岳
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Aikono Biomedical Hong Kong Co ltd
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Accro Bioscience Inc
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Priority to EP18819803.0A priority Critical patent/EP3642193B1/en
Priority to JP2019569828A priority patent/JP6950006B2/ja
Priority to PCT/US2018/039180 priority patent/WO2018237370A1/en
Priority to KR1020197036806A priority patent/KR102367257B1/ko
Priority to US16/625,703 priority patent/US11339177B2/en
Priority to ES18819803T priority patent/ES2916549T3/es
Publication of CN109111464A publication Critical patent/CN109111464A/zh
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic 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
    • C07D498/04—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
    • A61K31/435—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
    • A61K31/435—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
    • A61K31/4375—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 six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
    • 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
    • A61K31/4985—Pyrazines or piperazines 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
    • A61K31/535—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
    • A61K31/5383—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
CN201810575869.7A 2017-06-23 2018-06-06 一种具有细胞坏死抑制活性的杂环化合物 Active CN109111464B (zh)

Priority Applications (6)

Application Number Priority Date Filing Date Title
EP18819803.0A EP3642193B1 (en) 2017-06-23 2018-06-23 Heteroaryl compounds as inhibitors of necrosis and related composition
JP2019569828A JP6950006B2 (ja) 2017-06-23 2018-06-23 ネクローシス阻害剤であるヘテロアリール化合物、それを用いる組成物及び方法
PCT/US2018/039180 WO2018237370A1 (en) 2017-06-23 2018-06-23 Heteroaryl compounds as inhibitors of necrosis, composition and method using the same
KR1020197036806A KR102367257B1 (ko) 2017-06-23 2018-06-23 괴사 억제제로서 헤테로아릴 화합물, 이의 조성물 및 이의 이용 방법
US16/625,703 US11339177B2 (en) 2017-06-23 2018-06-23 Heteroaryl compounds as inhibitors of necrosis, composition and method using the same
ES18819803T ES2916549T3 (es) 2017-06-23 2018-06-23 Compuestos heteroarilo como inhibidores de necrosis y composición relacionada

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CN201710483983 2017-06-23
CN2017104839832 2017-06-23

Publications (2)

Publication Number Publication Date
CN109111464A CN109111464A (zh) 2019-01-01
CN109111464B true CN109111464B (zh) 2021-02-26

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Country Link
US (1) US11339177B2 (https=)
EP (1) EP3642193B1 (https=)
JP (1) JP6950006B2 (https=)
KR (1) KR102367257B1 (https=)
CN (1) CN109111464B (https=)
ES (1) ES2916549T3 (https=)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW202116771A (zh) * 2019-07-17 2021-05-01 英屬開曼群島商百濟神州有限公司 作為ｈｐｋ１抑制劑之三環化合物及其用途
CN115894489A (zh) * 2021-09-22 2023-04-04 中国药科大学 一种受体相互作用蛋白激酶1的抑制剂及其制备方法、应用

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MY155517A (en) * 2008-03-31 2015-10-30 C&C Res Lab Heterocyclic derivatives
WO2010008847A2 (en) * 2008-06-24 2010-01-21 Takeda Pharmaceutical Company Limited Pi3k/m tor inhibitors
US20110172217A1 (en) * 2008-09-05 2011-07-14 Shionogi & Co., Ltd. Ring-fused morpholine derivative having pi3k-inhibiting activity
WO2010100144A1 (en) * 2009-03-04 2010-09-10 Merck Serono S.A. Fused bicyclic compounds as inhibitors for pi3 kinase
US9295673B2 (en) * 2011-02-23 2016-03-29 Intellikine Llc Combination of mTOR inhibitors and P13-kinase inhibitors, and uses thereof
US20160256458A1 (en) * 2013-11-18 2016-09-08 Forma Therapeutics, Inc. Benzopiperazine compositions as bet bromodomain inhibitors
CN106029076B (zh) * 2013-11-18 2019-06-07 福马疗法公司 作为bet溴域抑制剂的苯并哌嗪组合物
WO2018017435A1 (en) * 2016-07-22 2018-01-25 Accro Bioscience Inc. Heteroaryl compounds as inhibitors of necrosis, composition and application thereof
CN107641118B (zh) 2016-07-22 2020-11-06 爱科诺生物医药股份有限公司 具有细胞坏死抑制活性的化合物及其组合物和应用
RU2019133646A (ru) * 2017-03-30 2021-04-30 Ф. Хоффманн-Ля Рош Аг Изохинолины в качестве ингибиторов hpk1

Also Published As

Publication number Publication date
JP6950006B2 (ja) 2021-10-13
JP2020525417A (ja) 2020-08-27
EP3642193B1 (en) 2022-04-27
EP3642193A1 (en) 2020-04-29
US20210155635A1 (en) 2021-05-27
CN109111464A (zh) 2019-01-01
KR102367257B1 (ko) 2022-02-24
KR20200017411A (ko) 2020-02-18
ES2916549T3 (es) 2022-07-01
EP3642193A4 (en) 2021-03-10
US11339177B2 (en) 2022-05-24

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Denomination of invention: A heterocyclic compound with cell necrosis inhibitory activity

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