CN113853373A - 取代的杂环并环类化合物，其制法与医药上的用途 - Google Patents

取代的杂环并环类化合物，其制法与医药上的用途 Download PDF

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CN113853373A
CN113853373A CN202080034074.0A CN202080034074A CN113853373A CN 113853373 A CN113853373 A CN 113853373A CN 202080034074 A CN202080034074 A CN 202080034074A CN 113853373 A CN113853373 A CN 113853373A
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CN113853373B (zh
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周福生
蒋涛
林崇懒
蔡礼健
何宛
兰炯
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Genfleet Therapeutics Shanghai Inc
Zhejiang Genfleet Therapeutics Co Ltd
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Genfleet Therapeutics Shanghai Inc
Zhejiang Genfleet Therapeutics Co Ltd
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    • 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
    • C07D498/22—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 four 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
    • 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
    • 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
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
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    • 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
    • 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
    • C07D471/12—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 three hetero rings
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    • 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
    • C07D471/12—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 three hetero rings
    • C07D471/16—Peri-condensed systems
    • 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
    • C07D471/22—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 systems contains four or more hetero rings

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
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  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
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  • Chemical Kinetics & Catalysis (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

一种如式(I)或式(IA)所示的对KRAS基因突变具有选择抑制作用的取代的杂环并环类化合物或其药学上可接受的盐、立体异构体、溶剂合物或其前药，包含该化合物的药物组合物及其在制备癌症药物中的应用。

Description

PCT国内申请，说明书已公开。

Claims (27)

  1. PCT国内申请，权利要求书已公开。
CN202080034074.0A 2019-10-30 2020-10-28 取代的杂环并环类化合物，其制法与医药上的用途 Active CN113853373B (zh)

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CN202210818001.1A CN115057872A (zh) 2019-10-30 2020-10-28 取代的杂环并环类化合物，其制法与医药上的用途
CN202311339164.2A CN117645614A (zh) 2019-10-30 2020-10-28 取代的杂环并环类化合物，其制法与医药上的用途

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Application Number Priority Date Filing Date Title
CN201911045542 2019-10-30
CN201911045542X 2019-10-30
CN202010272563 2020-04-09
CN2020102725631 2020-04-09
CN202011140832 2020-10-22
CN2020111408325 2020-10-22
PCT/CN2020/124226 WO2021083167A1 (zh) 2019-10-30 2020-10-28 取代的杂环并环类化合物，其制法与医药上的用途

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CN202210818001.1A Division CN115057872A (zh) 2019-10-30 2020-10-28 取代的杂环并环类化合物，其制法与医药上的用途

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US (1) US20230084095A1 (zh)
EP (2) EP4328229A2 (zh)
JP (2) JP2023502891A (zh)
KR (1) KR20220106765A (zh)
CN (3) CN117645614A (zh)
AU (1) AU2020374844B2 (zh)
BR (1) BR112022008375A2 (zh)
CA (1) CA3156777A1 (zh)
TW (1) TWI754438B (zh)
WO (1) WO2021083167A1 (zh)
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CN114728968A (zh) * 2019-09-20 2022-07-08 上海济煜医药科技有限公司 稠合吡啶酮类化合物及其制备方法和应用
CN116406363A (zh) * 2020-08-21 2023-07-07 浙江海正药业股份有限公司 四环类衍生物、其制备方法及其医药上的用途

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US11932633B2 (en) 2018-05-07 2024-03-19 Mirati Therapeutics, Inc. KRas G12C inhibitors
EP3908283A4 (en) 2019-01-10 2022-10-12 Mirati Therapeutics, Inc. KRAS G12C INHIBITORS
US11453683B1 (en) 2019-08-29 2022-09-27 Mirati Therapeutics, Inc. KRas G12D inhibitors
MX2022003537A (es) 2019-09-24 2022-07-11 Mirati Therapeutics Inc Terapias de combinacion.
JP7340100B2 (ja) 2019-10-28 2023-09-06 メルク・シャープ・アンド・ドーム・エルエルシー Ｋｒａｓ ｇ１２ｃ変異型の小分子阻害薬
KR20220130126A (ko) 2019-12-20 2022-09-26 미라티 테라퓨틱스, 인크. Sos1 억제제
CN115916778A (zh) * 2020-09-12 2023-04-04 赛诺哈勃药业（成都）有限公司 甲硫氨酸腺苷转移酶抑制剂、其制备方法及应用
US20230107642A1 (en) 2020-12-18 2023-04-06 Erasca, Inc. Tricyclic pyridones and pyrimidones
TW202246267A (zh) * 2021-03-25 2022-12-01 大陸商上海濟煜醫藥科技有限公司 稠合吡啶酮類化合物鹽型、晶型及其應用
CN115124533A (zh) * 2021-03-26 2022-09-30 浙江海正药业股份有限公司 四环类衍生物、其制备方法和其医药上的用途
CN116848111A (zh) * 2021-03-26 2023-10-03 浙江海正药业股份有限公司 一种kras抑制剂关键中间体及其制备方法
WO2022206723A1 (zh) * 2021-03-30 2022-10-06 浙江海正药业股份有限公司 杂环类衍生物、其制备方法及其医药上的用途
WO2022223037A1 (zh) * 2021-04-22 2022-10-27 劲方医药科技(上海)有限公司 Kras抑制剂的盐或多晶型物
CA3226720A1 (en) * 2021-07-23 2023-01-26 Suzhou Zanrong Pharma Limited Kras g12d inhibitors and uses thereof
TW202327593A (zh) * 2021-12-24 2023-07-16 大陸商勁方醫藥科技(上海)有限公司 Kras抑制劑的多晶型物及其製備方法和用途
CN116327956A (zh) * 2022-04-01 2023-06-27 劲方医药科技(上海)有限公司 药物组合物、其用途及癌症的治疗方法
WO2024061267A1 (zh) * 2022-09-21 2024-03-28 劲方医药科技(上海)有限公司 一种药物组合物及其制备方法和用途
WO2024081674A1 (en) 2022-10-11 2024-04-18 Aadi Bioscience, Inc. Combination therapies for the treatment of cancer

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WO2018217651A1 (en) * 2017-05-22 2018-11-29 Amgen Inc. Kras g12c inhibitors and methods of using the same
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ES2928576T3 (es) * 2017-09-08 2022-11-21 Amgen Inc Inhibidores de KRAS G12C y métodos de uso de los mismos
WO2019099524A1 (en) * 2017-11-15 2019-05-23 Mirati Therapeutics, Inc. Kras g12c inhibitors
AU2019262589B2 (en) * 2018-05-04 2022-07-07 Amgen Inc. KRAS G12C inhibitors and methods of using the same

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CN106488910A (zh) * 2013-10-10 2017-03-08 亚瑞克西斯制药公司 Kras g12c的抑制剂
WO2018217651A1 (en) * 2017-05-22 2018-11-29 Amgen Inc. Kras g12c inhibitors and methods of using the same
US20190177338A1 (en) * 2017-12-08 2019-06-13 Astrazeneca Ab Chemical compounds
CN113396147A (zh) * 2019-05-31 2021-09-14 上海翰森生物医药科技有限公司 芳香杂环类衍生物调节剂、其制备方法和应用
CN112300194A (zh) * 2019-07-30 2021-02-02 上海凌达生物医药有限公司 一类稠环吡啶酮类化合物、制备方法和用途
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Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN114728968A (zh) * 2019-09-20 2022-07-08 上海济煜医药科技有限公司 稠合吡啶酮类化合物及其制备方法和应用
CN116406363A (zh) * 2020-08-21 2023-07-07 浙江海正药业股份有限公司 四环类衍生物、其制备方法及其医药上的用途

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JP2023175993A (ja) 2023-12-12
CN117645614A (zh) 2024-03-05
JP2023502891A (ja) 2023-01-26
KR20220106765A (ko) 2022-07-29
EP4053118A4 (en) 2023-01-04
US20230084095A1 (en) 2023-03-16
EP4328229A2 (en) 2024-02-28
EP4053118A1 (en) 2022-09-07
CA3156777A1 (en) 2021-05-06
WO2021083167A1 (zh) 2021-05-06
AU2020374844B2 (en) 2024-01-25
AU2020374844A1 (en) 2022-06-16
TW202128701A (zh) 2021-08-01
CN115057872A (zh) 2022-09-16
CN113853373B (zh) 2022-08-05
TWI754438B (zh) 2022-02-01
ZA202205758B (en) 2023-02-22
BR112022008375A2 (pt) 2022-07-12

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