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CN114286822A - 作为pd-1/pd-l1小分子抑制剂的化合物及其应用 - Google Patents

作为pd-1/pd-l1小分子抑制剂的化合物及其应用 Download PDF

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Publication number
CN114286822A
CN114286822A CN202080060528.1A CN202080060528A CN114286822A CN 114286822 A CN114286822 A CN 114286822A CN 202080060528 A CN202080060528 A CN 202080060528A CN 114286822 A CN114286822 A CN 114286822A
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CN
China
Prior art keywords
compound
alkyl
reaction
mmol
ethyl acetate
Prior art date
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Pending
Application number
CN202080060528.1A
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English (en)
Inventor
吴凌云
王才林
徐雄彬
童海骏
陈曙辉
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.)
Shanghai Qilu Pharmaceutical Research and Development Centre Ltd
Original Assignee
Medshine Discovery Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Medshine Discovery Inc filed Critical Medshine Discovery Inc
Publication of CN114286822A publication Critical patent/CN114286822A/zh
Pending legal-status Critical Current

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    • 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
    • C07D471/04—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
    • A61K31/4375—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 six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61K31/495—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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • 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
    • C07D487/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

Landscapes

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

Abstract

一类联芳基的化合物，具体公开了式(Ⅰ)所示化合物及其药学上可接受的盐。

Description

PCT国内申请，说明书已公开。

Claims (24)

  1. PCT国内申请，权利要求书已公开。
CN202080060528.1A 2019-09-30 2020-09-30 作为pd-1/pd-l1小分子抑制剂的化合物及其应用 Pending CN114286822A (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
CN2019109431937 2019-09-30
CN201910943193 2019-09-30
CN2020109118822 2020-09-02
CN202010911882 2020-09-02
PCT/CN2020/119511 WO2021063404A1 (zh) 2019-09-30 2020-09-30 作为pd-1/pd-l1小分子抑制剂的化合物及其应用

Publications (1)

Publication Number Publication Date
CN114286822A true CN114286822A (zh) 2022-04-05

Family

ID=75336773

Family Applications (1)

Application Number Title Priority Date Filing Date
CN202080060528.1A Pending CN114286822A (zh) 2019-09-30 2020-09-30 作为pd-1/pd-l1小分子抑制剂的化合物及其应用

Country Status (8)

Country Link
US (1) US20220402917A1 (zh)
EP (1) EP4043461A1 (zh)
JP (1) JP2022550427A (zh)
KR (1) KR20220059517A (zh)
CN (1) CN114286822A (zh)
AU (1) AU2020357529A1 (zh)
CA (1) CA3152690A1 (zh)
WO (1) WO2021063404A1 (zh)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2024109462A1 (zh) * 2022-11-22 2024-05-30 西安新通药物研究股份有限公司 新型双环类pd-l1抑制剂及其制备方法与医药用途

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2022152316A1 (zh) * 2021-01-18 2022-07-21 南京明德新药研发有限公司 联苯衍生物及其应用
WO2022206800A1 (zh) * 2021-03-30 2022-10-06 南京明德新药研发有限公司 四氢萘啶化合物晶型、盐型及其制备方法
US12115157B2 (en) * 2021-09-14 2024-10-15 Boehringer Ingelheim International Gmbh 3-phenoxyazetidin-1-yl-heteroaryl pyrrolidine derivatives and the use thereof as medicament
WO2024018403A1 (en) * 2022-07-21 2024-01-25 Arbutus Biopharma Corporation Substituted imidazoamide compounds, and methods using same
TW202430515A (zh) * 2022-09-28 2024-08-01 加拿大商愛彼特生物製藥公司 經取代之1-芳基胺基羰基-1’-雜芳基化合物、經取代之1-雜芳基胺基羰基-1’-雜芳基化合物及其使用方法
CN117343006B (zh) * 2023-10-08 2024-07-09 河南科技大学 一种arb-272572的制备方法

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2018119224A1 (en) * 2016-12-22 2018-06-28 Incyte Corporation Tetrahydro imidazo[4,5-c]pyridine derivatives as pd-l1 internalization inducers
CN111936475A (zh) * 2018-04-03 2020-11-13 贝达药业股份有限公司 免疫调节剂及其组合物和制备方法

Family Cites Families (10)

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MX2016002544A (es) 2013-09-04 2016-06-17 Squibb Bristol Myers Co Compuestos utiles como inmunomoduladores.
MX365218B (es) 2013-09-06 2019-05-27 Aurigene Discovery Tech Ltd Derivados de 1,2,4-oxadiazol como inmunomoduladores.
US9850225B2 (en) 2014-04-14 2017-12-26 Bristol-Myers Squibb Company Compounds useful as immunomodulators
SG10202004618TA (en) * 2015-11-19 2020-06-29 Incyte Corp Heterocyclic compounds as immunomodulators
US20170174671A1 (en) * 2015-12-17 2017-06-22 Incyte Corporation Heterocyclic compounds as immunomodulators
WO2018119263A1 (en) 2016-12-22 2018-06-28 Incyte Corporation Heterocyclic compounds derivatives as pd-l1 internalization inducers
MA47120A (fr) * 2016-12-22 2021-04-28 Incyte Corp Dérivés pyridine utilisés en tant qu'immunomodulateurs
JOP20180040A1 (ar) 2017-04-20 2019-01-30 Gilead Sciences Inc مثبطات pd-1/pd-l1
EA202090746A1 (ru) 2017-11-03 2020-08-17 Ориджен Дискавери Текнолоджис Лимитед Двойные ингибиторы путей tim-3 и pd-1
TWI796596B (zh) 2018-02-13 2023-03-21 美商基利科學股份有限公司 Pd‐1/pd‐l1抑制劑

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2018119224A1 (en) * 2016-12-22 2018-06-28 Incyte Corporation Tetrahydro imidazo[4,5-c]pyridine derivatives as pd-l1 internalization inducers
CN111936475A (zh) * 2018-04-03 2020-11-13 贝达药业股份有限公司 免疫调节剂及其组合物和制备方法

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2024109462A1 (zh) * 2022-11-22 2024-05-30 西安新通药物研究股份有限公司 新型双环类pd-l1抑制剂及其制备方法与医药用途

Also Published As

Publication number Publication date
US20220402917A1 (en) 2022-12-22
AU2020357529A1 (en) 2022-05-19
CA3152690A1 (en) 2021-04-08
EP4043461A1 (en) 2022-08-17
KR20220059517A (ko) 2022-05-10
JP2022550427A (ja) 2022-12-01
WO2021063404A1 (zh) 2021-04-08

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