JP7654008B2 - 置換ピリミジンまたはピリジルアミン誘導体、その組成物及び医薬的使用 - Google Patents

置換ピリミジンまたはピリジルアミン誘導体、その組成物及び医薬的使用 Download PDF

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JP7654008B2
JP7654008B2 JP2022556468A JP2022556468A JP7654008B2 JP 7654008 B2 JP7654008 B2 JP 7654008B2 JP 2022556468 A JP2022556468 A JP 2022556468A JP 2022556468 A JP2022556468 A JP 2022556468A JP 7654008 B2 JP7654008 B2 JP 7654008B2
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劉力鋒
趙志明
許峰
王海龍
席宝信
童忠安
關慧平
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Shanghai Haiyan Pharmaceutical Technology Co Ltd
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with 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
    • A61K31/535—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
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61P35/00—Antineoplastic agents
    • 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
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
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    • 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
    • C07D417/14—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 three or more hetero rings
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    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
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    • C07D—HETEROCYCLIC COMPOUNDS
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    • 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
    • C07D487/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems
    • C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
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    • 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
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    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6558—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
    • C07F9/65583—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system each of the hetero rings containing nitrogen as ring hetero atom

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth 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)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Engineering & Computer Science (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
JP2022556468A 2020-03-16 2021-03-16 置換ピリミジンまたはピリジルアミン誘導体、その組成物及び医薬的使用 Active JP7654008B2 (ja)

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CN202010183457 2020-03-16
CN202010183457.6 2020-03-16
CN202011279917 2020-11-16
CN202011279917.1 2020-11-16
PCT/CN2021/081126 WO2021185256A1 (zh) 2020-03-16 2021-03-16 取代的嘧啶或吡啶胺衍生物、其组合物及医药上的用途

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JP2023518774A JP2023518774A (ja) 2023-05-08
JP2023518774A5 JP2023518774A5 (https=) 2024-06-24
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EP (1) EP4122927A4 (https=)
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KR (1) KR20220147124A (https=)
CN (2) CN118373808A (https=)
AU (1) AU2021239135B2 (https=)
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MX2022007376A (es) 2019-12-20 2022-09-02 Tenaya Therapeutics Inc Fluoroalqull-oxadiazoles y sus usos.
WO2022166796A1 (zh) * 2021-02-05 2022-08-11 上海齐鲁制药研究中心有限公司 嘧啶或吡啶并杂环类腺苷受体抑制剂及其制备方法和用途
US20240252502A1 (en) 2021-05-04 2024-08-01 Tenaya Therapeutics, Inc. Hdac6 inhibitors for treatment of metabolic disease and hfpef
EP4337202A4 (en) 2021-06-18 2025-04-02 Aligos Therapeutics, Inc. METHODS AND COMPOSITIONS FOR TARGETING PD-L1
WO2023040876A1 (zh) * 2021-09-15 2023-03-23 上海海雁医药科技有限公司 氮杂芳环类化合物及其药学上可接受的盐的多晶型物、药物组合物和应用
AU2022347682B2 (en) * 2021-09-15 2025-08-28 Shanghai Haiyan Pharmaceutical Technology Co., Ltd. Polymorph and application of pyrimidine derivative and pharmaceutically acceptable salt thereof
CN116063292A (zh) * 2021-10-29 2023-05-05 山东晶源生物医药有限公司 一种含氮化合物、其中间体、其组合物、其制备方法及其应用
EP4448512A4 (en) 2021-12-16 2025-11-19 Aligos Therapeutics Inc METHODS AND COMPOSITIONS FOR TARGETING PD-L1
JP2025512384A (ja) 2022-04-13 2025-04-17 ギリアード サイエンシーズ， インコーポレイテッド Ｔｒｏｐ－２発現がんを治療するための併用療法
JP2024005443A (ja) * 2022-06-30 2024-01-17 ユニマテック株式会社 塩素化された含フッ素ピリミジン化合物の製造方法
JP2024005442A (ja) * 2022-06-30 2024-01-17 ユニマテック株式会社 塩素化された含フッ素ピリミジン化合物の製造方法
WO2025137640A1 (en) 2023-12-22 2025-06-26 Gilead Sciences, Inc. Azaspiro wrn inhibitors

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JP2005298449A (ja) 2004-04-15 2005-10-27 Astellas Pharma Inc ４−アミノピリミジン誘導体
JP2011509279A (ja) 2008-01-11 2011-03-24 ノバルティス アーゲー ピロロピリミジン類およびピロロピリジン類
JP2013523711A (ja) 2010-03-31 2013-06-17 パロビオファルマ，エス．エル． アデノシンａ２ａ受容体拮抗薬としての４−アミノピリミジン誘導体
WO2013124246A1 (de) 2012-02-22 2013-08-29 Bayer Intellectual Property Gmbh Herbizid wirksame 4-dialkoxymethyl-2-phenylpyrimidine
WO2015091531A1 (en) 2013-12-19 2015-06-25 Almirall, S.A. Imidazolopyrimidin-2-yl derivatives as jak inhibitors
WO2017088755A1 (en) 2015-11-23 2017-06-01 Suzhou Yunxuan Yiyao Keji Youxian Gongsi Aminopyrimidine heterocyclic compound with adenosine receptor antagonistic activity
CN109651358A (zh) 2017-10-11 2019-04-19 上海迪诺医药科技有限公司 4-氨基吡啶衍生物、其药物组合物、制备方法及应用
JP2019524638A (ja) 2017-01-20 2019-09-05 アーカス バイオサイエンシズ インコーポレイティド 癌関連障害の治療のためのアゾロピリミジン

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JP2011509279A (ja) 2008-01-11 2011-03-24 ノバルティス アーゲー ピロロピリミジン類およびピロロピリジン類
JP2013523711A (ja) 2010-03-31 2013-06-17 パロビオファルマ，エス．エル． アデノシンａ２ａ受容体拮抗薬としての４−アミノピリミジン誘導体
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CN109651358A (zh) 2017-10-11 2019-04-19 上海迪诺医药科技有限公司 4-氨基吡啶衍生物、其药物组合物、制备方法及应用

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Bucevicius, Jonas et al，2,4-Bis(4-aryl-1,2,3-triazol-1-yl)pyrrolo[2,3-d]pyrimidines: synthesis and tuning of optical properties by polar substituents，RSC Advances，2015年，Vol.5(48)，p.38610-38622
Bucevicius, Jonas et al，Easy Access to Isomeric 7-Deazapurine-1,2,3-Triazole Conjugates via S N Ar and CuAAC Reactions of 2,6-Diazido-7-deazapurines，Synlett，2018年，Vol.29(4)，p.525-529
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ラトビア国特許第１４８５１号，2014年07月20日

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WO2021185256A1 (zh) 2021-09-23
CA3171774C (en) 2025-05-20
KR20220147124A (ko) 2022-11-02
EP4122927A1 (en) 2023-01-25
AU2021239135B2 (en) 2024-05-02
CN113748110A (zh) 2021-12-03
AU2021239135A1 (en) 2022-10-20
EP4122927A4 (en) 2024-07-03
JP2023518774A (ja) 2023-05-08
CN118373808A (zh) 2024-07-23
CN113748110B (zh) 2024-05-14
CA3171774A1 (en) 2021-09-23
US20230145793A1 (en) 2023-05-11

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