CN108779110B - 磷脂酰肌醇3-激酶γ的新颖抑制剂 - Google Patents

磷脂酰肌醇3-激酶γ的新颖抑制剂 Download PDF

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Publication number
CN108779110B
CN108779110B CN201780014898.XA CN201780014898A CN108779110B CN 108779110 B CN108779110 B CN 108779110B CN 201780014898 A CN201780014898 A CN 201780014898A CN 108779110 B CN108779110 B CN 108779110B
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dihydro
oxo
isoindol
methyl
thiazol
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Chinese (zh)
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CN108779110A (zh
Inventor
M.莫格马克
N.佩姆伯顿
J.彼得森
M.佩里
K.卡拉贝拉斯
P.兹拉托伊斯基
R.科克斯
C.泰尔钱
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AstraZeneca AB
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AstraZeneca AB
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
    • 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
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • 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
    • A61P11/08—Bronchodilators
    • 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
    • A61P37/08—Antiallergic agents
    • 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)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pulmonology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
CN201780014898.XA 2016-03-10 2017-03-09 磷脂酰肌醇3-激酶γ的新颖抑制剂 Expired - Fee Related CN108779110B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201662306328P 2016-03-10 2016-03-10
US62/306328 2016-03-10
PCT/EP2017/055552 WO2017153527A1 (en) 2016-03-10 2017-03-09 Novel inhibitors of phosphatidylinositol 3-kinase gamma

Publications (2)

Publication Number Publication Date
CN108779110A CN108779110A (zh) 2018-11-09
CN108779110B true CN108779110B (zh) 2021-10-29

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CN201780014898.XA Expired - Fee Related CN108779110B (zh) 2016-03-10 2017-03-09 磷脂酰肌醇3-激酶γ的新颖抑制剂

Country Status (13)

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US (2) US10858355B2 (enExample)
EP (1) EP3426652B1 (enExample)
JP (1) JP6893520B2 (enExample)
KR (1) KR20180117693A (enExample)
CN (1) CN108779110B (enExample)
AR (1) AR107840A1 (enExample)
AU (1) AU2017229445B2 (enExample)
BR (1) BR112018068075A2 (enExample)
CA (1) CA3015893C (enExample)
EA (1) EA036388B1 (enExample)
MX (1) MX387125B (enExample)
TW (1) TWI746525B (enExample)
WO (1) WO2017153527A1 (enExample)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11161838B2 (en) 2018-11-13 2021-11-02 Incyte Corporation Heterocyclic derivatives as PI3K inhibitors
WO2020102216A1 (en) 2018-11-13 2020-05-22 Incyte Corporation Substituted heterocyclic derivatives as pi3k inhibitors
WO2020102198A1 (en) * 2018-11-13 2020-05-22 Incyte Corporation Heterocyclic derivatives as pi3k inhibitors
WO2020210379A1 (en) 2019-04-10 2020-10-15 Hangzhou Zhengxiang Pharmaceuticals Co., Ltd. Phosphatidylinositol 3-kinase inhibitors
AU2020288610A1 (en) 2019-06-04 2022-01-27 Arcus Biosciences, Inc. 2,3,5-trisubstituted pyrazolo[1,5-a]pyrimidine compounds
WO2022017371A1 (zh) * 2020-07-21 2022-01-27 中国医药研究开发中心有限公司 具有磷脂酰肌醇3-激酶δ和γ的双重抑制剂活性的杂环化合物及其医药用途
CN115611883B (zh) * 2021-07-13 2025-03-28 生物岛实验室 一种双环结构的PI3Kα抑制剂及其制备方法和用途
CN119768404A (zh) * 2022-09-01 2025-04-04 上海海雁医药科技有限公司 杂芳基取代的吡啶并吡咯酮衍生物、其药物组合物及应用
EP4585596A4 (en) * 2022-09-09 2025-12-10 Shanghai Yingli Pharm Co Ltd Nitrogen-containing heterocyclic compound, pharmaceutical composition thereof and uses thereof
CN116813608B (zh) * 2023-06-08 2024-03-22 英矽智能科技(上海)有限公司 噻唑类化合物及其应用
EP4734987A1 (en) 2023-06-30 2026-05-06 Forschungsverbund Berlin E.V. Thiazolo tetrahydrochinoline compounds as class ii phosphoinositide 3-kinase inhibitors

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101484452A (zh) * 2006-05-03 2009-07-15 阿斯利康(瑞典)有限公司 噻唑衍生物及其作为抗肿瘤药物的用途
CN101535307A (zh) * 2006-08-30 2009-09-16 塞尔佐姆有限公司 作为激酶抑制剂的三唑衍生物
WO2010096389A1 (en) * 2009-02-17 2010-08-26 Vertex Pharmaceuticals Incorporated Tetrahydrothiazolopyridine inhibitors of phosphatidylinositol 3-kinase
CN102762548A (zh) * 2009-12-22 2012-10-31 沃泰克斯药物股份有限公司 磷脂酰肌醇3-激酶的异吲哚啉酮抑制剂
CN104379573A (zh) * 2012-04-20 2015-02-25 艾伯维公司 异吲哚酮衍生物
CN105722838A (zh) * 2013-09-25 2016-06-29 沃泰克斯药物股份有限公司 磷脂酰肌醇3-激酶-γ的选择性抑制剂

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW200613272A (en) * 2004-08-13 2006-05-01 Astrazeneca Ab Isoindolone compounds and their use as metabotropic glutamate receptor potentiators
US20080287469A1 (en) * 2005-02-17 2008-11-20 Diacovo Thomas G Phosphoinositide 3-Kinase Inhibitors for Inhibiting Leukocyte Accumulation
AU2007207743B2 (en) * 2006-01-18 2010-07-08 Amgen Inc. Thiazole compounds as protein kinase B (PKB) inhibitors
US20110230472A1 (en) * 2008-08-29 2011-09-22 Shionogi & Co., Ltd. Ring-fused azole derivative having pi3k-inhibiting activity
AU2014391610B2 (en) 2014-04-24 2018-01-25 Novartis Ag Pyrazine derivatives as phosphatidylinositol 3-kinase inhibitors
KR20160145780A (ko) 2014-04-24 2016-12-20 노파르티스 아게 포스파티딜이노시톨 3-키나제 억제제로서의 아미노 피리딘 유도체
CA2945212A1 (en) 2014-04-24 2015-10-29 Novartis Ag Amino pyrazine derivatives as phosphatidylinositol 3-kinase inhibitors

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101484452A (zh) * 2006-05-03 2009-07-15 阿斯利康(瑞典)有限公司 噻唑衍生物及其作为抗肿瘤药物的用途
CN101535307A (zh) * 2006-08-30 2009-09-16 塞尔佐姆有限公司 作为激酶抑制剂的三唑衍生物
WO2010096389A1 (en) * 2009-02-17 2010-08-26 Vertex Pharmaceuticals Incorporated Tetrahydrothiazolopyridine inhibitors of phosphatidylinositol 3-kinase
CN102762548A (zh) * 2009-12-22 2012-10-31 沃泰克斯药物股份有限公司 磷脂酰肌醇3-激酶的异吲哚啉酮抑制剂
CN104379573A (zh) * 2012-04-20 2015-02-25 艾伯维公司 异吲哚酮衍生物
CN105722838A (zh) * 2013-09-25 2016-06-29 沃泰克斯药物股份有限公司 磷脂酰肌醇3-激酶-γ的选择性抑制剂

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Publication number Publication date
EA201891931A1 (ru) 2019-04-30
EA036388B1 (ru) 2020-11-03
TW201808945A (zh) 2018-03-16
WO2017153527A1 (en) 2017-09-14
US10858355B2 (en) 2020-12-08
AU2017229445B2 (en) 2019-07-11
US20210047312A1 (en) 2021-02-18
BR112018068075A2 (pt) 2019-01-08
JP6893520B2 (ja) 2021-06-23
JP2019507788A (ja) 2019-03-22
KR20180117693A (ko) 2018-10-29
AR107840A1 (es) 2018-06-13
MX2018010894A (es) 2018-11-09
MX387125B (es) 2025-03-18
US20200299289A1 (en) 2020-09-24
EP3426652A1 (en) 2019-01-16
CA3015893C (en) 2021-11-09
CN108779110A (zh) 2018-11-09
CA3015893A1 (en) 2017-09-14
AU2017229445A1 (en) 2018-10-25
TWI746525B (zh) 2021-11-21
EP3426652B1 (en) 2021-12-01

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