CN107698593A - 作为fgfr抑制剂的杂环化合物 - Google Patents

作为fgfr抑制剂的杂环化合物 Download PDF

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Publication number
CN107698593A
CN107698593A CN201610647295.0A CN201610647295A CN107698593A CN 107698593 A CN107698593 A CN 107698593A CN 201610647295 A CN201610647295 A CN 201610647295A CN 107698593 A CN107698593 A CN 107698593A
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China
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alkyl
ring
independently selected
compound
substituted
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Pending
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CN201610647295.0A
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English (en)
Chinese (zh)
Inventor
孔祥龙
周超
陈向阳
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Nanjing Innocare Pharma Tech Co ltd
Original Assignee
Nanjing Tian Jian Hua Medicine Technology Co Ltd
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Application filed by Nanjing Tian Jian Hua Medicine Technology Co Ltd filed Critical Nanjing Tian Jian Hua Medicine Technology Co Ltd
Priority to CN201610647295.0A priority Critical patent/CN107698593A/zh
Priority to EP17838568.8A priority patent/EP3498706A4/en
Priority to CA3032921A priority patent/CA3032921A1/en
Priority to JP2019529309A priority patent/JP6959663B2/ja
Priority to CN201780045675.XA priority patent/CN109715626B/zh
Priority to US16/324,189 priority patent/US10752631B2/en
Priority to PCT/CN2017/094620 priority patent/WO2018028438A1/zh
Priority to KR1020197006637A priority patent/KR20190035870A/ko
Publication of CN107698593A publication Critical patent/CN107698593A/zh
Pending legal-status Critical Current

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    • 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
    • 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
    • A61K31/495—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
    • A61K31/525—Isoalloxazines, e.g. riboflavins, vitamin B2
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
CN201610647295.0A 2016-08-09 2016-08-09 作为fgfr抑制剂的杂环化合物 Pending CN107698593A (zh)

Priority Applications (8)

Application Number Priority Date Filing Date Title
CN201610647295.0A CN107698593A (zh) 2016-08-09 2016-08-09 作为fgfr抑制剂的杂环化合物
EP17838568.8A EP3498706A4 (en) 2016-08-09 2017-07-27 HETEROCYCLIC COMPOUND USED AS AN FGFR INHIBITOR
CA3032921A CA3032921A1 (en) 2016-08-09 2017-07-27 Heterocyclic compounds as fgfr inhibitors
JP2019529309A JP6959663B2 (ja) 2016-08-09 2017-07-27 Ｆｇｆｒ阻害剤としての複素環化合物
CN201780045675.XA CN109715626B (zh) 2016-08-09 2017-07-27 作为fgfr抑制剂的杂环化合物
US16/324,189 US10752631B2 (en) 2016-08-09 2017-07-27 Heterocyclic compounds as FGFR inhibitors
PCT/CN2017/094620 WO2018028438A1 (zh) 2016-08-09 2017-07-27 作为fgfr抑制剂的杂环化合物
KR1020197006637A KR20190035870A (ko) 2016-08-09 2017-07-27 Fgfr 저해제로서 헤테로시클릭 화합물

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
CN201610647295.0A CN107698593A (zh) 2016-08-09 2016-08-09 作为fgfr抑制剂的杂环化合物

Publications (1)

Publication Number Publication Date
CN107698593A true CN107698593A (zh) 2018-02-16

Family

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Family Applications (2)

Application Number Title Priority Date Filing Date
CN201610647295.0A Pending CN107698593A (zh) 2016-08-09 2016-08-09 作为fgfr抑制剂的杂环化合物
CN201780045675.XA Active CN109715626B (zh) 2016-08-09 2017-07-27 作为fgfr抑制剂的杂环化合物

Family Applications After (1)

Application Number Title Priority Date Filing Date
CN201780045675.XA Active CN109715626B (zh) 2016-08-09 2017-07-27 作为fgfr抑制剂的杂环化合物

Country Status (7)

Country Link
US (1) US10752631B2 (cg-RX-API-DMAC7.html)
EP (1) EP3498706A4 (cg-RX-API-DMAC7.html)
JP (1) JP6959663B2 (cg-RX-API-DMAC7.html)
KR (1) KR20190035870A (cg-RX-API-DMAC7.html)
CN (2) CN107698593A (cg-RX-API-DMAC7.html)
CA (1) CA3032921A1 (cg-RX-API-DMAC7.html)
WO (1) WO2018028438A1 (cg-RX-API-DMAC7.html)

Cited By (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN112480109A (zh) * 2020-11-16 2021-03-12 浙江大学 吡啶并[2,3-b]吡嗪-3(4H)-酮类衍生物及其用途
CN114127051A (zh) * 2019-05-17 2022-03-01 金耐特生物制药公司 成纤维细胞生长因子受体激酶的抑制剂
CN114853739A (zh) * 2021-02-03 2022-08-05 药雅科技(上海)有限公司 一种炔代吡嗪类fgfr抑制剂及其制备方法和用途
CN115043832A (zh) * 2021-03-08 2022-09-13 药雅科技(上海)有限公司 一种fgfr抑制剂炔代杂环类化合物及其制备方法和用途
CN116096707A (zh) * 2020-06-05 2023-05-09 金耐特生物制药公司 成纤维细胞生长因子受体激酶的抑制剂
WO2024083111A1 (zh) * 2022-10-18 2024-04-25 首药控股(北京)股份有限公司 一种新型杂环化合物
US12331039B2 (en) 2020-06-05 2025-06-17 Khora Spv 1, Llc Inhibitors of fibroblast growth factor receptor kinases

Families Citing this family (31)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR102945203B1 (ko) 2017-05-08 2026-03-31 시애틀 프로젝트 코포레이션 알파바이러스 신생항원 벡터
KR20210090650A (ko) 2018-11-07 2021-07-20 그릿스톤 바이오, 인코포레이티드 알파바이러스 신생항원 벡터 및 인터페론 억제제
CA3129665A1 (en) 2019-03-21 2020-09-24 Onxeo A dbait molecule in combination with kinase inhibitor for the treatment of cancer
SG11202113187WA (en) 2019-05-30 2021-12-30 Gritstone Bio Inc Modified adenoviruses
KR20220098759A (ko) 2019-11-08 2022-07-12 인쎄름 (엥스띠뛰 나씨오날 드 라 쌍떼 에 드 라 흐쉐르슈 메디깔) 키나제 억제제에 대해 내성을 획득한 암의 치료 방법
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
IL300026A (en) 2020-08-06 2023-03-01 Gritstone Bio Inc Multiepitope vaccine cassettes
MX2023008186A (es) * 2021-01-12 2023-07-18 Beijing Innocare Pharma Tech Co Ltd Proceso para preparar (s)-1-(1-acriloilpirrolidin-3-il)-3-((3,5-di metoxifenil)etinil)-5-(metilamino)-1h-pirazol-4-carboxamida.
CN121487738A (zh) 2023-03-30 2026-02-06 锐新医药公司 诱导ras gtp水解的组合物和其用途
KR20260019479A (ko) 2023-05-04 2026-02-10 레볼루션 메디슨즈, 인크. Ras 관련 질환 또는 장애를 위한 병용 요법
CN121889155A (zh) 2023-08-07 2026-04-17 锐新医药公司 用于治疗ras蛋白相关疾病或病症的rmc-6291
AU2024360465A1 (en) 2023-10-12 2026-04-09 Revolution Medicines, Inc. Macrocyclic 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
US20250375445A1 (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
WO2026015825A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Use of ras inhibitor for treating pancreatic cancer
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
WO2026015790A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026050446A1 (en) 2024-08-29 2026-03-05 Revolution Medicines, Inc. Ras inhibitors
WO2026072904A2 (en) 2024-09-26 2026-04-02 Revolution Medicines, Inc. Compositions and methods for treating lung cancer
WO2026090116A2 (en) 2024-10-21 2026-04-30 Revolution Medicines, Inc. Ras inhibitors
US20260108528A1 (en) 2024-10-22 2026-04-23 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
WO2026090245A1 (en) 2024-10-22 2026-04-30 Revolution Medicines, Inc. Use of ras inhibitors for treating cancer
WO2026106912A1 (en) 2024-11-12 2026-05-21 Revolution Medicines, Inc. Ras inhibitors
WO2026112260A1 (en) 2024-11-21 2026-05-28 Revolution Medicines, Inc. Ras inhibitors
WO2026122764A2 (en) 2024-12-06 2026-06-11 Revolution Medicines, Inc. Ras inhibitors
WO2026128688A2 (en) 2024-12-13 2026-06-18 Revolution Medicines, Inc. Ras inhibitors
WO2026161839A1 (en) 2025-01-27 2026-07-30 Revolution Medicines, Inc. Ras inhibitors

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007087395A2 (en) * 2006-01-25 2007-08-02 Osi Pharmaceuticals, Inc. UNSATURATED mTOR INHIBITORS
CN103958512A (zh) * 2012-01-19 2014-07-30 大鹏药品工业株式会社 3,5-双取代炔基苯化合物及其盐
CN104341388A (zh) * 2013-10-16 2015-02-11 上海润诺生物科技有限公司 芳香族酰胺类衍生物、其制备方法及其在医药上的应用
CN104341425A (zh) * 2013-08-08 2015-02-11 上海医药集团股份有限公司 氘代乙炔衍生物、其药物组合物及应用
US20160031888A1 (en) * 2013-03-13 2016-02-04 Boston Biomedical, Inc. 3-(aryl or heteroaryl) methyleneindolin-2-one derivatives as inhibitors of cancer stem cell pathway kinases for the treatment of cancer
EP3023100A1 (en) * 2013-07-18 2016-05-25 Taiho Pharmaceutical Co., Ltd. Antitumor drug for intermittent administration of fgfr inhibitor

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP6084292B2 (ja) 2013-07-18 2017-02-22 大鵬薬品工業株式会社 Ｆｇｆｒ阻害剤耐性癌の治療薬
EP3184521B1 (en) * 2014-08-19 2021-10-06 Shanghai Haihe Pharmaceutical Co., Ltd. Indazole compounds as fgfr kinase inhibitors, preparation and use thereof

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007087395A2 (en) * 2006-01-25 2007-08-02 Osi Pharmaceuticals, Inc. UNSATURATED mTOR INHIBITORS
CN103958512A (zh) * 2012-01-19 2014-07-30 大鹏药品工业株式会社 3,5-双取代炔基苯化合物及其盐
US20160031888A1 (en) * 2013-03-13 2016-02-04 Boston Biomedical, Inc. 3-(aryl or heteroaryl) methyleneindolin-2-one derivatives as inhibitors of cancer stem cell pathway kinases for the treatment of cancer
EP3023100A1 (en) * 2013-07-18 2016-05-25 Taiho Pharmaceutical Co., Ltd. Antitumor drug for intermittent administration of fgfr inhibitor
US20160193210A1 (en) * 2013-07-18 2016-07-07 Taiho Pharmaceutical Co., Ltd. Antitumor drug for intermittent administration of fgfr inhibitor
CN104341425A (zh) * 2013-08-08 2015-02-11 上海医药集团股份有限公司 氘代乙炔衍生物、其药物组合物及应用
CN104341388A (zh) * 2013-10-16 2015-02-11 上海润诺生物科技有限公司 芳香族酰胺类衍生物、其制备方法及其在医药上的应用

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
张媛等: "以c-Met为肿瘤治疗靶点的受体酪氨酸激酶抑制剂的研究进展", 《中国药科大学学报》 *
朱贺敏等: "癌症靶标Aurora A激酶结构、功能与抑制剂研究进展", 《中国药学杂志》 *

Cited By (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN114127051A (zh) * 2019-05-17 2022-03-01 金耐特生物制药公司 成纤维细胞生长因子受体激酶的抑制剂
CN116096707A (zh) * 2020-06-05 2023-05-09 金耐特生物制药公司 成纤维细胞生长因子受体激酶的抑制剂
US12331039B2 (en) 2020-06-05 2025-06-17 Khora Spv 1, Llc Inhibitors of fibroblast growth factor receptor kinases
CN112480109A (zh) * 2020-11-16 2021-03-12 浙江大学 吡啶并[2,3-b]吡嗪-3(4H)-酮类衍生物及其用途
CN114853739A (zh) * 2021-02-03 2022-08-05 药雅科技(上海)有限公司 一种炔代吡嗪类fgfr抑制剂及其制备方法和用途
CN114853739B (zh) * 2021-02-03 2023-09-22 药雅科技(上海)有限公司 一种炔代吡嗪类fgfr抑制剂及其制备方法和用途
CN115043832A (zh) * 2021-03-08 2022-09-13 药雅科技(上海)有限公司 一种fgfr抑制剂炔代杂环类化合物及其制备方法和用途
CN115043832B (zh) * 2021-03-08 2023-08-22 药雅科技(上海)有限公司 一种fgfr抑制剂炔代杂环类化合物及其制备方法和用途
WO2024083111A1 (zh) * 2022-10-18 2024-04-25 首药控股(北京)股份有限公司 一种新型杂环化合物

Also Published As

Publication number Publication date
KR20190035870A (ko) 2019-04-03
WO2018028438A1 (zh) 2018-02-15
EP3498706A1 (en) 2019-06-19
JP6959663B2 (ja) 2021-11-02
CN109715626A (zh) 2019-05-03
EP3498706A4 (en) 2020-02-26
US10752631B2 (en) 2020-08-25
CA3032921A1 (en) 2018-02-15
US20190177333A1 (en) 2019-06-13
CN109715626B (zh) 2022-04-26
JP2019524883A (ja) 2019-09-05

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Application publication date: 20180216