CN115052866A - 含氮杂芳类衍生物自由碱的晶型 - Google Patents

含氮杂芳类衍生物自由碱的晶型 Download PDF

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Publication number
CN115052866A
CN115052866A CN202180011135.6A CN202180011135A CN115052866A CN 115052866 A CN115052866 A CN 115052866A CN 202180011135 A CN202180011135 A CN 202180011135A CN 115052866 A CN115052866 A CN 115052866A
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degrees
amino
cycloalkyl
radical
diffraction peaks
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CN202180011135.6A
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詹小兰
呙临松
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Jiangsu Hansoh Pharmaceutical Group Co Ltd
Shanghai Hansoh Biomedical Co Ltd
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Jiangsu Hansoh Pharmaceutical Group Co Ltd
Shanghai Hansoh Biomedical 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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines 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
    • A61K31/535—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
    • 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
    • C07D471/10—Spiro-condensed systems
    • 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
    • C07D498/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Liquid Crystal Substances (AREA)

Abstract

本发明涉及一种含氮杂芳类衍生物自由碱的晶型。具体涉及一种具有通式(I)化合物自由碱的晶型、制备方法和含有治疗有效量的该晶型的药物组合物，及其作为蛋白酪氨酸磷酸酶‑2C(SHP2)抑制剂，在治疗白血病、神经母细胞瘤、黑色素瘤、乳癌、肺癌及其结肠癌等疾病或病症的用途。

Description

PCT国内申请，说明书已公开。

Claims (23)

  1. PCT国内申请，权利要求书已公开。
CN202180011135.6A 2020-04-03 2021-04-02 含氮杂芳类衍生物自由碱的晶型 Pending CN115052866A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN202010261479X 2020-04-03
CN202010261479 2020-04-03
PCT/CN2021/085155 WO2021197452A1 (zh) 2020-04-03 2021-04-02 含氮杂芳类衍生物自由碱的晶型

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Publication Number Publication Date
CN115052866A true CN115052866A (zh) 2022-09-13

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CN202180011135.6A Pending CN115052866A (zh) 2020-04-03 2021-04-02 含氮杂芳类衍生物自由碱的晶型

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US (1) US20230134869A1 (zh)
EP (1) EP4129987A4 (zh)
JP (1) JP2023521023A (zh)
KR (1) KR20220163985A (zh)
CN (1) CN115052866A (zh)
AU (1) AU2021245897A1 (zh)
CA (1) CA3173060A1 (zh)
TW (1) TW202144334A (zh)
WO (1) WO2021197452A1 (zh)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20230011245A (ko) 2021-07-09 2023-01-20 주식회사 카나프테라퓨틱스 Shp2 억제제 및 이의 용도
CN118019537A (zh) * 2021-09-28 2024-05-10 上海翰森生物医药科技有限公司 Shp2抑制剂联合egfr-tki治疗和预防肿瘤疾病的医药用途
CN117088887A (zh) * 2022-05-20 2023-11-21 安徽中科拓苒药物科学研究有限公司 Shp2抑制剂及其用途

Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2015107495A1 (en) * 2014-01-17 2015-07-23 Novartis Ag N-azaspirocycloalkane substituted n-heteroaryl compounds and compositions for inhibiting the activity of shp2
WO2018172984A1 (en) * 2017-03-23 2018-09-27 Jacobio Pharmaceuticals Co., Ltd. Novel heterocyclic derivatives useful as shp2 inhibitors
CN109983001A (zh) * 2016-07-12 2019-07-05 锐新医药公司 作为变构shp2抑制剂的2,5-双取代型3-甲基吡嗪及2,5,6-三取代型3-甲基吡嗪
CN110143949A (zh) * 2018-05-09 2019-08-20 北京加科思新药研发有限公司 可用作shp2抑制剂的新型杂环衍生物
WO2019183367A1 (en) * 2018-03-21 2019-09-26 Relay Therapeutics, Inc. Shp2 phosphatase inhibitors and methods of use thereof
WO2020063760A1 (en) * 2018-09-26 2020-04-02 Jacobio Pharmaceuticals Co., Ltd. Novel heterocyclic derivatives useful as shp2 inhibitors
WO2020073949A1 (zh) * 2018-10-10 2020-04-16 江苏豪森药业集团有限公司 含氮杂芳类衍生物调节剂、其制备方法和应用

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN112625028A (zh) * 2015-06-19 2021-04-09 诺华股份有限公司 用于抑制shp2活性的化合物和组合物
WO2019051084A1 (en) * 2017-09-07 2019-03-14 Revolution Medicines, Inc. SHP2 INHIBITOR COMPOSITIONS AND METHODS OF TREATING CANCER

Patent Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2015107495A1 (en) * 2014-01-17 2015-07-23 Novartis Ag N-azaspirocycloalkane substituted n-heteroaryl compounds and compositions for inhibiting the activity of shp2
CN105916845A (zh) * 2014-01-17 2016-08-31 诺华股份有限公司 用于抑制shp2活性的n-氮杂螺环烷取代的n-杂芳基化合物和组合物
CN109983001A (zh) * 2016-07-12 2019-07-05 锐新医药公司 作为变构shp2抑制剂的2,5-双取代型3-甲基吡嗪及2,5,6-三取代型3-甲基吡嗪
WO2018172984A1 (en) * 2017-03-23 2018-09-27 Jacobio Pharmaceuticals Co., Ltd. Novel heterocyclic derivatives useful as shp2 inhibitors
WO2019183367A1 (en) * 2018-03-21 2019-09-26 Relay Therapeutics, Inc. Shp2 phosphatase inhibitors and methods of use thereof
CN110143949A (zh) * 2018-05-09 2019-08-20 北京加科思新药研发有限公司 可用作shp2抑制剂的新型杂环衍生物
WO2020063760A1 (en) * 2018-09-26 2020-04-02 Jacobio Pharmaceuticals Co., Ltd. Novel heterocyclic derivatives useful as shp2 inhibitors
WO2020073949A1 (zh) * 2018-10-10 2020-04-16 江苏豪森药业集团有限公司 含氮杂芳类衍生物调节剂、其制备方法和应用

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JP2023521023A (ja) 2023-05-23
US20230134869A1 (en) 2023-05-04
AU2021245897A1 (en) 2022-10-06
KR20220163985A (ko) 2022-12-12
TW202144334A (zh) 2021-12-01
CA3173060A1 (en) 2021-10-07
EP4129987A1 (en) 2023-02-08
EP4129987A4 (en) 2024-05-15
WO2021197452A1 (zh) 2021-10-07

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