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CN114502561A - Lsd1抑制剂 - Google Patents

Lsd1抑制剂 Download PDF

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Publication number
CN114502561A
CN114502561A CN202080068659.4A CN202080068659A CN114502561A CN 114502561 A CN114502561 A CN 114502561A CN 202080068659 A CN202080068659 A CN 202080068659A CN 114502561 A CN114502561 A CN 114502561A
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China
Prior art keywords
compound
isomer
pharmaceutically acceptable
acceptable salt
alkyl
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CN202080068659.4A
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English (en)
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CN114502561B (zh
Inventor
吴凌云
展震
钱薏
王君为
陈曙辉
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Nanchang Hongyi Technology Co Ltd
Nanchang Hongyi Pharmaceutical Co Ltd
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Nanchang Hongyi Technology Co Ltd
Nanchang Hongyi Pharmaceutical Co Ltd
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/13Amines
    • 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
    • A61K31/435Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C217/00Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton
    • C07C217/54Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton
    • C07C217/74Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with rings other than six-membered aromatic rings being part of the carbon skeleton
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D205/00Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
    • C07D205/02Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D205/04Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/10Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D207/14Nitrogen atoms not forming part of a nitro radical
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic 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
    • C07D491/02Heterocyclic 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
    • C07D491/10Spiro-condensed systems
    • C07D491/107Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

一类作为赖氨酸特异性去甲基化酶1(LSD1)抑制剂的杂螺环化合物,及其在制备治疗与LSD1相关疾病的药物中的应用。所述杂螺环化合物是式(Ⅰ)所示化合物、其异构体及其药学上可接受的盐。

Description

PCT国内申请,说明书已公开。

Claims (17)

  1. PCT国内申请,权利要求书已公开。
CN202080068659.4A 2019-09-29 2020-09-29 Lsd1抑制剂 Active CN114502561B (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
CN2019109351824 2019-09-29
CN201910935182 2019-09-29
CN2020108385239 2020-08-19
CN202010838523 2020-08-19
PCT/CN2020/118824 WO2021058024A1 (zh) 2019-09-29 2020-09-29 Lsd1抑制剂

Publications (2)

Publication Number Publication Date
CN114502561A true CN114502561A (zh) 2022-05-13
CN114502561B CN114502561B (zh) 2023-12-26

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
CN202080068659.4A Active CN114502561B (zh) 2019-09-29 2020-09-29 Lsd1抑制剂

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CN (1) CN114502561B (zh)
WO (1) WO2021058024A1 (zh)

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2023217784A1 (en) 2022-05-09 2023-11-16 Oryzon Genomics, S.A. Methods of treating nf1-mutant tumors using lsd1 inhibitors
WO2023217758A1 (en) 2022-05-09 2023-11-16 Oryzon Genomics, S.A. Methods of treating malignant peripheral nerve sheath tumor (mpnst) using lsd1 inhibitors
WO2024110649A1 (en) 2022-11-24 2024-05-30 Oryzon Genomics, S.A. Combinations of lsd1 inhibitors and menin inhibitors for treating cancer
CN119569746A (zh) * 2025-02-06 2025-03-07 纽欧申医药(上海)有限公司 含氮杂环化合物、其药物组合物及应用

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP4319732A1 (en) 2021-04-08 2024-02-14 Oryzon Genomics, S.A. Combinations of lsd1 inhibitors for treating myeloid cancers
WO2024229406A1 (en) 2023-05-04 2024-11-07 Revolution Medicines, Inc. Combination therapy for a ras related disease or disorder
WO2025034702A1 (en) 2023-08-07 2025-02-13 Revolution Medicines, Inc. Rmc-6291 for use in the treatment of ras protein-related disease or disorder
WO2025072637A1 (en) * 2023-09-28 2025-04-03 The Regents Of The University Of Michigan Oxygenated heterocyclic lsd-1 inhibitors and related methods of use
US20250154171A1 (en) 2023-10-12 2025-05-15 Revolution Medicines, Inc. Ras inhibitors
WO2025171296A1 (en) 2024-02-09 2025-08-14 Revolution Medicines, Inc. Ras inhibitors
WO2025240847A1 (en) 2024-05-17 2025-11-20 Revolution Medicines, Inc. Ras inhibitors
WO2025255438A1 (en) 2024-06-07 2025-12-11 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
WO2025265060A1 (en) 2024-06-21 2025-12-26 Revolution Medicines, Inc. Therapeutic compositions and methods for managing treatment-related effects
WO2026006747A1 (en) 2024-06-28 2026-01-02 Revolution Medicines, Inc. Ras inhibitors
WO2026015796A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015801A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015825A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Use of ras inhibitor for treating pancreatic cancer
WO2026015790A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder

Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103857393A (zh) * 2011-03-25 2014-06-11 葛兰素史密斯克莱知识产权(第2号)有限公司 环丙基胺作为lsd1抑制剂
CN104203914A (zh) * 2011-10-20 2014-12-10 奥瑞泽恩基因组学股份有限公司 作为lsd1抑制剂的(杂)芳基环丙胺化合物
WO2015123408A1 (en) * 2014-02-13 2015-08-20 Incyte Corporation Cyclopropylamines as lsd1 inhibitors
CN109153636A (zh) * 2016-05-09 2019-01-04 朱比连特比利斯有限公司 作为双重lsd1/hdac抑制剂的环丙基-酰胺化合物
WO2019025588A1 (en) * 2017-08-03 2019-02-07 Oryzon Genomics, S.A. METHODS OF TREATING ALTERATIONS IN BEHAVIOR
US20190211014A1 (en) * 2014-02-13 2019-07-11 Incyte Corporation Cyclopropylamines as lsd1 inhibitors
CN110248926A (zh) * 2017-01-24 2019-09-17 南京明德新药研发有限公司 Lsd1抑制剂及其制备方法和应用

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103857393A (zh) * 2011-03-25 2014-06-11 葛兰素史密斯克莱知识产权(第2号)有限公司 环丙基胺作为lsd1抑制剂
CN104203914A (zh) * 2011-10-20 2014-12-10 奥瑞泽恩基因组学股份有限公司 作为lsd1抑制剂的(杂)芳基环丙胺化合物
WO2015123408A1 (en) * 2014-02-13 2015-08-20 Incyte Corporation Cyclopropylamines as lsd1 inhibitors
US20190211014A1 (en) * 2014-02-13 2019-07-11 Incyte Corporation Cyclopropylamines as lsd1 inhibitors
CN109153636A (zh) * 2016-05-09 2019-01-04 朱比连特比利斯有限公司 作为双重lsd1/hdac抑制剂的环丙基-酰胺化合物
CN110248926A (zh) * 2017-01-24 2019-09-17 南京明德新药研发有限公司 Lsd1抑制剂及其制备方法和应用
WO2019025588A1 (en) * 2017-08-03 2019-02-07 Oryzon Genomics, S.A. METHODS OF TREATING ALTERATIONS IN BEHAVIOR

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2023217784A1 (en) 2022-05-09 2023-11-16 Oryzon Genomics, S.A. Methods of treating nf1-mutant tumors using lsd1 inhibitors
WO2023217758A1 (en) 2022-05-09 2023-11-16 Oryzon Genomics, S.A. Methods of treating malignant peripheral nerve sheath tumor (mpnst) using lsd1 inhibitors
WO2024110649A1 (en) 2022-11-24 2024-05-30 Oryzon Genomics, S.A. Combinations of lsd1 inhibitors and menin inhibitors for treating cancer
CN119569746A (zh) * 2025-02-06 2025-03-07 纽欧申医药(上海)有限公司 含氮杂环化合物、其药物组合物及应用
CN119569746B (zh) * 2025-02-06 2025-05-13 纽欧申医药(上海)有限公司 含氮杂环化合物、其药物组合物及应用

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WO2021058024A1 (zh) 2021-04-01
CN114502561B (zh) 2023-12-26

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