CN114599651B - 作为造血祖细胞激酶1(hpk1)抑制剂的吲唑类药物及其使用方法 - Google Patents

作为造血祖细胞激酶1(hpk1)抑制剂的吲唑类药物及其使用方法

Info

Publication number
CN114599651B
CN114599651B CN202180003282.9A CN202180003282A CN114599651B CN 114599651 B CN114599651 B CN 114599651B CN 202180003282 A CN202180003282 A CN 202180003282A CN 114599651 B CN114599651 B CN 114599651B
Authority
CN
China
Prior art keywords
compound
fluoro
bromo
cancer
mixture
Prior art date
Legal status (The legal status 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 status listed.)
Active
Application number
CN202180003282.9A
Other languages
English (en)
Chinese (zh)
Other versions
CN114599651A (zh
Inventor
J·李
S·赵
K·林
A·Y·朴
加德·昌德夫·戈拉克什纳
H·南
Y·全
Y·黄
J·E·金
M·金
S·M·林
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.)
First Biotherapy Co ltd
Original Assignee
First Biotherapy Co ltd
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 First Biotherapy Co ltd filed Critical First Biotherapy Co ltd
Publication of CN114599651A publication Critical patent/CN114599651A/zh
Application granted granted Critical
Publication of CN114599651B publication Critical patent/CN114599651B/zh
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02—Silicon compounds
    • C07F7/08—Compounds having one or more C—Si linkages
    • C07F7/0803—Compounds with Si-C or Si-Si linkages
    • C07F7/081—Compounds with Si-C or Si-Si linkages comprising at least one atom selected from the elements N, O, halogen, S, Se or Te
    • C07F7/0812—Compounds with Si-C or Si-Si linkages comprising at least one atom selected from the elements N, O, halogen, S, Se or Te comprising a heterocyclic ring
    • 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
    • A61K31/495—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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/5025—Pyridazines; Hydrogenated pyridazines 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
    • A61K31/495—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
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • 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
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • 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
    • 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
    • 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
    • C07D513/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/645—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having two nitrogen atoms as the only ring hetero atoms
    • C07F9/6503—Five-membered rings
    • C07F9/65031—Five-membered rings having the nitrogen atoms in the positions 1 and 2
    • C07F9/65038—Five-membered rings having the nitrogen atoms in the positions 1 and 2 condensed with carbocyclic rings or carbocyclic ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6558—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
    • C07F9/65583—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system each of the hetero rings containing nitrogen as ring hetero atom
    • 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
    • C07B2200/05—Isotopically modified compounds, e.g. labelled

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Immunology (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Oncology (AREA)
  • Transplantation (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
CN202180003282.9A 2020-09-28 2021-09-27 作为造血祖细胞激酶1(hpk1)抑制剂的吲唑类药物及其使用方法 Active CN114599651B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US202063084059P 2020-09-28 2020-09-28
US63/084,059 2020-09-28
PCT/IB2021/058795 WO2022064459A1 (en) 2020-09-28 2021-09-27 Indazoles as hematopoietic progenitor kinase 1 (hpk1) inhibitors and methods of using same

Publications (2)

Publication Number Publication Date
CN114599651A CN114599651A (zh) 2022-06-07
CN114599651B true CN114599651B (zh) 2025-12-16

Family

ID=80821021

Family Applications (2)

Application Number Title Priority Date Filing Date
CN202180003282.9A Active CN114599651B (zh) 2020-09-28 2021-09-27 作为造血祖细胞激酶1(hpk1)抑制剂的吲唑类药物及其使用方法
CN202180003294.1A Active CN114599653B (zh) 2020-09-28 2021-09-27 作为造血祖细胞激酶1(hpk1)抑制剂的吲唑及其使用方法

Family Applications After (1)

Application Number Title Priority Date Filing Date
CN202180003294.1A Active CN114599653B (zh) 2020-09-28 2021-09-27 作为造血祖细胞激酶1(hpk1)抑制剂的吲唑及其使用方法

Country Status (11)

Country Link
US (2) US11834467B2 (https=)
EP (1) EP4217358A4 (https=)
JP (1) JP2023542724A (https=)
KR (1) KR20230104143A (https=)
CN (2) CN114599651B (https=)
AU (1) AU2021347913A1 (https=)
CA (1) CA3193865A1 (https=)
IL (1) IL301244A (https=)
MX (1) MX2023003631A (https=)
TW (1) TWI908894B (https=)
WO (2) WO2022064459A1 (https=)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2022064459A1 (en) * 2020-09-28 2022-03-31 1ST Biotherapeutics, Inc. Indazoles as hematopoietic progenitor kinase 1 (hpk1) inhibitors and methods of using same
EP4499643A4 (en) * 2022-03-25 2026-01-28 1St Biotherapeutics Inc INDAZOLES USED AS HEMATOPOIETIC PROGENITOR KINASE 1 (HPK1) INHIBITORS AND THEIR METHODS OF USE

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010100144A1 (en) * 2009-03-04 2010-09-10 Merck Serono S.A. Fused bicyclic compounds as inhibitors for pi3 kinase
CN111315727A (zh) * 2017-10-02 2020-06-19 第一生物治疗股份有限公司 苯并噻唑化合物及使用其治疗神经退行性疾病的方法

Family Cites Families (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PE20070978A1 (es) * 2006-02-14 2007-11-15 Novartis Ag COMPUESTOS HETEROCICLICOS COMO INHIBIDORES DE FOSFATIDILINOSITOL 3-QUINASAS (PI3Ks)
TW200911798A (en) 2007-08-02 2009-03-16 Amgen Inc PI3 kinase modulators and methods of use
US8993580B2 (en) * 2008-03-14 2015-03-31 Intellikine Llc Benzothiazole kinase inhibitors and methods of use
WO2010008847A2 (en) 2008-06-24 2010-01-21 Takeda Pharmaceutical Company Limited Pi3k/m tor inhibitors
US8450321B2 (en) 2008-12-08 2013-05-28 Gilead Connecticut, Inc. 6-(1H-indazol-6-yl)-N-[4-(morpholin-4-yl)phenyl]imidazo-[1,2-A]pyrazin-8-amine, or a pharmaceutically acceptable salt thereof, as a SYK inhibitor
PL2716157T3 (pl) 2008-12-08 2017-06-30 Gilead Connecticut, Inc. Imidazopirazynowe inhibitory Syk
BRPI1014572B8 (pt) 2009-04-16 2022-07-19 Fundacion Centro Nac De Investigaciones Oncologicas Carlos Iii Imidazopirazinas para uso como inibidores de cinase
US9073927B2 (en) 2010-01-22 2015-07-07 Fundacion Centro Nacional De Investigaciones Oncologicas Carlos Iii Inhibitors of PI3 kinase
WO2012052745A1 (en) 2010-10-21 2012-04-26 Centro Nacional De Investigaciones Oncológicas (Cnio) Combinations of pi3k inhibitors with a second anti -tumor agent
AR086042A1 (es) 2011-04-28 2013-11-13 Galapagos Nv Compuesto util para el tratamiento de enfermedades degenerativas e inflamatorias y composicion farmaceutica
WO2013130855A1 (en) 2012-03-02 2013-09-06 Takeda Pharmaceutical Company Limited Indazole derivatives
PL236355B1 (pl) * 2015-04-02 2021-01-11 Celon Pharma Spolka Akcyjna Pochodne 7-(morfolin-4-ylo)pirazolo[1,5-α]pirymidyny jako inhibitory kinazy PI3
MA42456B1 (fr) * 2015-06-25 2021-06-30 Univ Health Network Inhibiteurs de hpk1 et leurs procédés d'utilisation
CN115819417A (zh) * 2016-09-09 2023-03-21 因赛特公司 作为hpk1调节剂的吡唑并吡啶衍生物及其用于治疗癌症的用途
AU2018244935A1 (en) * 2017-03-30 2019-08-15 F. Hoffmann-La Roche Ag Naphthyridines as inhibitors of HPK1
CN109721620B (zh) * 2017-10-27 2022-05-13 药捷安康(南京)科技股份有限公司 Hpk1抑制剂及其用途
EP3707138B1 (en) * 2017-11-06 2022-07-13 Bristol-Myers Squibb Company Isofuranone compounds useful as hpk1 inhibitors
EP3877371A4 (en) * 2018-11-07 2022-07-27 Dana-Farber Cancer Institute, Inc. IMIDAZOPYRIDINE DERIVATIVES AND AZA-IMIDAZOPYRIDINE DERIVATIVES AS JANUS KINASE 2 INHIBITORS AND USES THEREOF
AU2020224401A1 (en) * 2019-02-22 2021-10-14 1ST Biotherapeutics, Inc. Imidazopyridinyl compounds and use thereof for treatment of neurodegenerative disorders
WO2022064459A1 (en) * 2020-09-28 2022-03-31 1ST Biotherapeutics, Inc. Indazoles as hematopoietic progenitor kinase 1 (hpk1) inhibitors and methods of using same

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010100144A1 (en) * 2009-03-04 2010-09-10 Merck Serono S.A. Fused bicyclic compounds as inhibitors for pi3 kinase
CN111315727A (zh) * 2017-10-02 2020-06-19 第一生物治疗股份有限公司 苯并噻唑化合物及使用其治疗神经退行性疾病的方法

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
RN号为1112980-20-7化合物;ACS;《STN Registry》;20090227;RN号为1112980-20-7化合物 *

Also Published As

Publication number Publication date
US11834467B2 (en) 2023-12-05
TWI908894B (zh) 2025-12-21
JP2023542724A (ja) 2023-10-11
AU2021347913A1 (en) 2023-05-18
CN114599653A (zh) 2022-06-07
CN114599653B (zh) 2025-12-16
IL301244A (en) 2023-05-01
MX2023003631A (es) 2023-04-11
CN114599651A (zh) 2022-06-07
US20220098219A1 (en) 2022-03-31
US20220098193A1 (en) 2022-03-31
EP4217358A1 (en) 2023-08-02
TW202220999A (zh) 2022-06-01
US11649255B2 (en) 2023-05-16
KR20230104143A (ko) 2023-07-07
EP4217358A4 (en) 2025-01-08
WO2022064459A1 (en) 2022-03-31
CA3193865A1 (en) 2022-03-31
AU2021347913A9 (en) 2024-06-27
WO2022064458A1 (en) 2022-03-31

Similar Documents

Publication Publication Date Title
JP7675777B2 (ja) 免疫調節剤としての複素環式化合物
CN113527293B (zh) Kras g12c突变蛋白抑制剂及其药物组合物、制备方法和用途
ES2291628T3 (es) Compuestos triciclicos a base de tiofeno y composiciones farmaceuticas que comprenden dichos compuestos.
JP2024133478A (ja) Ｔａｍ阻害剤としてのピロロトリアジン化合物
AU2023282201B2 (en) Chromene derivatives as inhibitors of TCR-Nck interaction
KR102755652B1 (ko) 고리형 디뉴클레오티드 유사체, 이의 약학 조성물 및 용도
CN114599651B (zh) 作为造血祖细胞激酶1(hpk1)抑制剂的吲唑类药物及其使用方法
US11453688B2 (en) Phosphorus imidazoquinoline amine derivatives, pharmaceutical compositions and therapeutic methods thereof
CN117157284A (zh) Ctla-4小分子降解剂及其应用
RU2854594C1 (ru) Индазолы в качестве ингибиторов киназы 1 гемопоэтического предшественника (hpk1) и способы их применения
HK40097413B (en) Heterocyclic compounds as immunomodulators
HK40097413A (en) Heterocyclic compounds as immunomodulators

Legal Events

Date Code Title Description
PB01 Publication
PB01 Publication
SE01 Entry into force of request for substantive examination
SE01 Entry into force of request for substantive examination
GR01 Patent grant
GR01 Patent grant