JP2023522124A - ハロゲン化ヘテロアリール及び他のヘテロ環系キナーゼ阻害剤、及びその用途 - Google Patents

ハロゲン化ヘテロアリール及び他のヘテロ環系キナーゼ阻害剤、及びその用途 Download PDF

Info

Publication number
JP2023522124A
JP2023522124A JP2022563872A JP2022563872A JP2023522124A JP 2023522124 A JP2023522124 A JP 2023522124A JP 2022563872 A JP2022563872 A JP 2022563872A JP 2022563872 A JP2022563872 A JP 2022563872A JP 2023522124 A JP2023522124 A JP 2023522124A
Authority
JP
Japan
Prior art keywords
alkyl
group
compound
independently selected
heterocyclyl
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.)
Pending
Application number
JP2022563872A
Other languages
English (en)
Japanese (ja)
Other versions
JP2023522124A5 (https=
JPWO2021214117A5 (https=
Inventor
センネン,ピーター
ビッシンガー,シュテファン
ロフェラー,ハネス
バンクロフト,デビッド
ミケルス,ティルマン
ハンデルワル,ニシット
Original Assignee
イオックス セラピューティクス アーゲー
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 イオックス セラピューティクス アーゲー filed Critical イオックス セラピューティクス アーゲー
Publication of JP2023522124A publication Critical patent/JP2023522124A/ja
Publication of JP2023522124A5 publication Critical patent/JP2023522124A5/ja
Publication of JPWO2021214117A5 publication Critical patent/JPWO2021214117A5/ja
Pending legal-status Critical Current

Links

Images

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/14Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D333/00Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/26Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D333/28Halogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D333/00Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/46Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings substituted on the ring sulfur atom
    • CCHEMISTRY; METALLURGY
    • C12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12QMEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
    • C12Q1/00Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions
    • C12Q1/68Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving nucleic acids
    • C12Q1/6876Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes
    • C12Q1/6883Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes for diseases caused by alterations of genetic material
    • C12Q1/6886Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes for diseases caused by alterations of genetic material for cancer
    • GPHYSICS
    • G01MEASURING; TESTING
    • G01NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/53Immunoassay; Biospecific binding assay; Materials therefor
    • G01N33/575Immunoassay; Biospecific binding assay; Materials therefor for cancer
    • G01N33/5758Immunoassay; Biospecific binding assay; Materials therefor for cancer involving compounds serving as markers for tumours, cancers or neoplasias, e.g. cellular determinants, receptors, heat shock/stress proteins, A-protein, oligosaccharides or metabolites
    • G01N33/57595Immunoassay; Biospecific binding assay; Materials therefor for cancer involving compounds serving as markers for tumours, cancers or neoplasias, e.g. cellular determinants, receptors, heat shock/stress proteins, A-protein, oligosaccharides or metabolites involving intracellular compounds
    • CCHEMISTRY; METALLURGY
    • C12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12QMEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
    • C12Q2600/00Oligonucleotides characterized by their use
    • C12Q2600/156Polymorphic or mutational markers
    • GPHYSICS
    • G01MEASURING; TESTING
    • G01NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2333/00Assays involving biological materials from specific organisms or of a specific nature
    • G01N2333/435Assays involving biological materials from specific organisms or of a specific nature from animals; from humans
    • G01N2333/46Assays involving biological materials from specific organisms or of a specific nature from animals; from humans from vertebrates
    • G01N2333/47Assays involving proteins of known structure or function as defined in the subgroups
    • G01N2333/4701Details
    • G01N2333/4703Regulators; Modulating activity
    • GPHYSICS
    • G01MEASURING; TESTING
    • G01NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2800/00Detection or diagnosis of diseases
    • G01N2800/52Predicting or monitoring the response to treatment, e.g. for selection of therapy based on assay results in personalised medicine; Prognosis

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Immunology (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Molecular Biology (AREA)
  • Urology & Nephrology (AREA)
  • Hematology (AREA)
  • Biomedical Technology (AREA)
  • Analytical Chemistry (AREA)
  • Pathology (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Physics & Mathematics (AREA)
  • Biochemistry (AREA)
  • Microbiology (AREA)
  • Biotechnology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Cell Biology (AREA)
  • Food Science & Technology (AREA)
  • General Physics & Mathematics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Zoology (AREA)
  • Epidemiology (AREA)
  • Genetics & Genomics (AREA)
  • Wood Science & Technology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biophysics (AREA)
  • General Engineering & Computer Science (AREA)
  • Oncology (AREA)
  • Hospice & Palliative Care (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2022563872A 2020-04-21 2021-04-21 ハロゲン化ヘテロアリール及び他のヘテロ環系キナーゼ阻害剤、及びその用途 Pending JP2023522124A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP20170641.3A EP3901151B1 (en) 2020-04-21 2020-04-21 Halogenated-heteroaryl and other heterocyclic kinase inhibitors, and uses thereof
EP20170641.3 2020-04-21
PCT/EP2021/060338 WO2021214117A1 (en) 2020-04-21 2021-04-21 Halogenated-heteroaryl and other heterocyclic kinase inhibitors, and uses thereof

Publications (3)

Publication Number Publication Date
JP2023522124A true JP2023522124A (ja) 2023-05-26
JP2023522124A5 JP2023522124A5 (https=) 2024-04-18
JPWO2021214117A5 JPWO2021214117A5 (https=) 2024-04-18

Family

ID=71108343

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2022563872A Pending JP2023522124A (ja) 2020-04-21 2021-04-21 ハロゲン化ヘテロアリール及び他のヘテロ環系キナーゼ阻害剤、及びその用途

Country Status (18)

Country Link
US (1) US20230348453A1 (https=)
EP (2) EP3901151B1 (https=)
JP (1) JP2023522124A (https=)
KR (1) KR20230015343A (https=)
CN (1) CN115667255B (https=)
AU (1) AU2021258431A1 (https=)
BR (1) BR112022021476A2 (https=)
CA (1) CA3176325A1 (https=)
CL (1) CL2022002899A1 (https=)
CO (1) CO2022016245A2 (https=)
CR (1) CR20220528A (https=)
IL (1) IL297481A (https=)
MX (1) MX2022013160A (https=)
PE (1) PE20230462A1 (https=)
PH (1) PH12022552813A1 (https=)
TW (1) TW202204352A (https=)
WO (1) WO2021214117A1 (https=)
ZA (1) ZA202212631B (https=)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US12030875B2 (en) 2018-09-07 2024-07-09 PIC Therapeutics, Inc. EIF4E inhibitors and uses thereof
AU2021230289A1 (en) 2020-03-03 2022-09-29 PIC Therapeutics, Inc. eIF4E inhibitors and uses thereof
US12157732B2 (en) 2021-08-25 2024-12-03 PIC Therapeutics, Inc. eIF4E inhibitors and uses thereof
JP2024534127A (ja) 2021-08-25 2024-09-18 ピク セラピューティクス, インコーポレイテッド eIF4E阻害剤及びその使用
KR20240115232A (ko) * 2021-10-19 2024-07-25 아이오엠엑스 테라퓨틱스 아게 Sik3 억제제 및 이의 중간체를 제조하기 위한 합성 반응식 및 과정
US20230212522A1 (en) * 2022-01-05 2023-07-06 The Board Of Regents Of The University Of Texas System Methods and reagents for characterizing thsd1 function
EP4257609A1 (en) 2022-04-08 2023-10-11 iOmx Therapeutics AG Combination therapies based on pd-1 inhibitors and sik3 inhibitors
EP4257132A1 (en) 2022-04-08 2023-10-11 iOmx Therapeutics AG Sik3 inhibitors for treating diseases resistant to death receptor signalling
CN116813608B (zh) * 2023-06-08 2024-03-22 英矽智能科技(上海)有限公司 噻唑类化合物及其应用
TW202523302A (zh) 2023-11-02 2025-06-16 美商阿克思生物科學有限公司 噻唑化合物及其使用方法
WO2025157389A1 (en) 2024-01-22 2025-07-31 Iomx Therapeutics Ag Combinations of halogenated heterocyclic kinase inhibitors and vegfr inhibitors
WO2025229127A1 (en) 2024-04-30 2025-11-06 Iomx Therapeutics Ag A halogenated-heteroaryl kinase inhibitor for treating soft tissue sarcoma and vascular tumors
EP4643861A1 (en) 2024-04-30 2025-11-05 iOmx Therapeutics AG A halogenated-heteroaryl kinase inhbitor for treating soft tissue sarcoma and vascular tumors

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2004501914A (ja) * 2000-06-28 2004-01-22 アストラゼネカ アクチボラグ 置換キナゾリン誘導体及び、阻害剤としてのそれらの使用
WO2010054107A2 (en) * 2008-11-05 2010-05-14 Principia Biopharma Inc. Kinase knockdown via electrophilically enhanced inhibitors
CN103172627A (zh) * 2011-12-26 2013-06-26 南京优科生物医药有限公司 杂环嘧啶苯或吡啶苯类化合物及其应用
WO2018193084A1 (en) * 2017-04-20 2018-10-25 Iomx Therapeutics Ag Intracellular kinase associated with resistance against anti-tumour immune responses, and uses thereof

Family Cites Families (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4447233A (en) 1981-04-10 1984-05-08 Parker-Hannifin Corporation Medication infusion pump
US4439196A (en) 1982-03-18 1984-03-27 Merck & Co., Inc. Osmotic drug delivery system
US4475916A (en) 1982-03-18 1984-10-09 Merck & Co., Inc. Osmotic drug delivery system
US4522811A (en) 1982-07-08 1985-06-11 Syntex (U.S.A.) Inc. Serial injection of muramyldipeptides and liposomes enhances the anti-infective activity of muramyldipeptides
US4447224A (en) 1982-09-20 1984-05-08 Infusaid Corporation Variable flow implantable infusion apparatus
US4487603A (en) 1982-11-26 1984-12-11 Cordis Corporation Implantable microinfusion pump system
US4486194A (en) 1983-06-08 1984-12-04 James Ferrara Therapeutic device for administering medicaments through the skin
US4596556A (en) 1985-03-25 1986-06-24 Bioject, Inc. Hypodermic injection apparatus
US5374548A (en) 1986-05-02 1994-12-20 Genentech, Inc. Methods and compositions for the attachment of proteins to liposomes using a glycophospholipid anchor
MX9203291A (es) 1985-06-26 1992-08-01 Liposome Co Inc Metodo para acoplamiento de liposomas.
US4941880A (en) 1987-06-19 1990-07-17 Bioject, Inc. Pre-filled ampule and non-invasive hypodermic injection device assembly
US4790824A (en) 1987-06-19 1988-12-13 Bioject, Inc. Non-invasive hypodermic injection device
US5108921A (en) 1989-04-03 1992-04-28 Purdue Research Foundation Method for enhanced transmembrane transport of exogenous molecules
US5312335A (en) 1989-11-09 1994-05-17 Bioject Inc. Needleless hypodermic injection device
US5064413A (en) 1989-11-09 1991-11-12 Bioject, Inc. Needleless hypodermic injection device
US5383851A (en) 1992-07-24 1995-01-24 Bioject Inc. Needleless hypodermic injection device
RU2368602C2 (ru) 2005-01-26 2009-09-27 Айрм Ллк Соединения и композиции в качестве ингибиторов протеинкиназ
AU2007296743B2 (en) 2006-09-11 2012-02-16 Curis, Inc. Tyrosine kinase inhibitors containing a zinc binding moiety
US8907053B2 (en) 2010-06-25 2014-12-09 Aurigene Discovery Technologies Limited Immunosuppression modulating compounds
US9260426B2 (en) 2012-12-14 2016-02-16 Arrien Pharmaceuticals Llc Substituted 1H-pyrrolo [2, 3-b] pyridine and 1H-pyrazolo [3, 4-b] pyridine derivatives as salt inducible kinase 2 (SIK2) inhibitors
AU2015300782B2 (en) 2014-08-08 2020-04-16 Dana-Farber Cancer Institute, Inc. Uses of salt-inducible kinase (SIK) inhibitors
CN106699744B (zh) * 2015-11-18 2021-05-11 四川海思科制药有限公司 一种杂环类酰胺衍生物及其制备方法和在药学上的应用
BR112019017741A2 (pt) 2017-02-28 2020-04-07 Dana Farber Cancer Inst Inc usos de pirimidopirimidinonas como inibidores de sik
DK3643713T3 (da) * 2018-10-23 2025-11-03 Iomx Therapeutics Ag Heterocykliske kinaseinhibitorer og deres anvendelse

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2004501914A (ja) * 2000-06-28 2004-01-22 アストラゼネカ アクチボラグ 置換キナゾリン誘導体及び、阻害剤としてのそれらの使用
WO2010054107A2 (en) * 2008-11-05 2010-05-14 Principia Biopharma Inc. Kinase knockdown via electrophilically enhanced inhibitors
CN103172627A (zh) * 2011-12-26 2013-06-26 南京优科生物医药有限公司 杂环嘧啶苯或吡啶苯类化合物及其应用
WO2018193084A1 (en) * 2017-04-20 2018-10-25 Iomx Therapeutics Ag Intracellular kinase associated with resistance against anti-tumour immune responses, and uses thereof

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
長野哲雄, 創薬化学 メディシナルケミストへの道, vol. 第1版第1刷, JPN7025000685, 28 September 2018 (2018-09-28), pages 182 - 215, ISSN: 0005699527 *

Also Published As

Publication number Publication date
AU2021258431A1 (en) 2022-11-17
PE20230462A1 (es) 2023-03-14
CN115667255A (zh) 2023-01-31
EP4139305A1 (en) 2023-03-01
US20230348453A1 (en) 2023-11-02
PH12022552813A1 (en) 2024-03-25
WO2021214117A1 (en) 2021-10-28
CL2022002899A1 (es) 2023-06-30
CA3176325A1 (en) 2021-10-28
ZA202212631B (en) 2023-07-26
MX2022013160A (es) 2023-02-09
EP3901151A1 (en) 2021-10-27
CR20220528A (es) 2023-07-13
EP3901151B1 (en) 2026-04-01
BR112022021476A2 (pt) 2023-04-04
IL297481A (en) 2022-12-01
CN115667255B (zh) 2025-10-28
KR20230015343A (ko) 2023-01-31
CO2022016245A2 (es) 2023-02-27
TW202204352A (zh) 2022-02-01

Similar Documents

Publication Publication Date Title
CN115667255B (zh) 卤代杂芳基和其他杂环激酶抑制剂及其用途
JP7667568B2 (ja) 複素環キナーゼ阻害剤及びその使用
US20230192701A1 (en) Bicyclic kinase inhibitors and uses thereof
US12139480B2 (en) 5-thiazolecarboxamide kinase inhibitor and uses thereof
IL297483A (en) Bifunctional compounds and their uses
US20210000825A1 (en) Tyrosine Kinase Non-Receptor 1 (TNK1) Inhibitors and Uses Thereof
HK40062784A (en) Halogenated-heteroaryl and other heterocyclic kinase inhibitors, and uses thereof
HK40067698A (en) Tyrosine kinase non-receptor 1 (tnk1) inhibitors and uses thereof
KR20220132538A (ko) 디하이드로오로테이트 데하이드로게나제를 억제하는 방법 및 조성물

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20240408

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20240408

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20250210

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20250219

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20250515

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20250718

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20250818

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20251001

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20251217

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20260326

A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20260402