JP7864352B2 - 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Info
- Publication number
- JP7864352B2 JP7864352B2 JP2022563872A JP2022563872A JP7864352B2 JP 7864352 B2 JP7864352 B2 JP 7864352B2 JP 2022563872 A JP2022563872 A JP 2022563872A JP 2022563872 A JP2022563872 A JP 2022563872A JP 7864352 B2 JP7864352 B2 JP 7864352B2
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- JP
- Japan
- Prior art keywords
- compound
- alkyl
- group
- pharmaceutical composition
- formula
- 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.)
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Classifications
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- 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
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- 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
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and 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
- A61K31/55—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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
- C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
- C07D333/04—Heterocyclic 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
- C07D333/26—Heterocyclic 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
- C07D333/28—Halogen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
- C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
- C07D333/46—Heterocyclic 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
-
- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12Q—MEASURING 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
- C12Q1/00—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions
- C12Q1/68—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving nucleic acids
- C12Q1/6876—Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes
- C12Q1/6883—Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes for diseases caused by alterations of genetic material
- C12Q1/6886—Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes for diseases caused by alterations of genetic material for cancer
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- G—PHYSICS
- G01—MEASURING; TESTING
- G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
- G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
- G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
- G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
- G01N33/53—Immunoassay; Biospecific binding assay; Materials therefor
- G01N33/575—Immunoassay; Biospecific binding assay; Materials therefor for cancer
- G01N33/5758—Immunoassay; 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
- G01N33/57595—Immunoassay; 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
-
- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12Q—MEASURING 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
- C12Q2600/00—Oligonucleotides characterized by their use
- C12Q2600/156—Polymorphic or mutational markers
-
- G—PHYSICS
- G01—MEASURING; TESTING
- G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
- G01N2333/00—Assays involving biological materials from specific organisms or of a specific nature
- G01N2333/435—Assays involving biological materials from specific organisms or of a specific nature from animals; from humans
- G01N2333/46—Assays involving biological materials from specific organisms or of a specific nature from animals; from humans from vertebrates
- G01N2333/47—Assays involving proteins of known structure or function as defined in the subgroups
- G01N2333/4701—Details
- G01N2333/4703—Regulators; Modulating activity
-
- G—PHYSICS
- G01—MEASURING; TESTING
- G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
- G01N2800/00—Detection or diagnosis of diseases
- G01N2800/52—Predicting 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)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Microbiology (AREA)
- Physics & Mathematics (AREA)
- Biochemistry (AREA)
- Biotechnology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Cell Biology (AREA)
- General Physics & Mathematics (AREA)
- Food Science & Technology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Zoology (AREA)
- Wood Science & Technology (AREA)
- Genetics & Genomics (AREA)
- Epidemiology (AREA)
- Biophysics (AREA)
- Oncology (AREA)
- Hospice & Palliative Care (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Engineering & Computer Science (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP20170641.3 | 2020-04-21 | ||
| EP20170641.3A EP3901151B1 (en) | 2020-04-21 | 2020-04-21 | Halogenated-heteroaryl and other heterocyclic kinase inhibitors, and uses thereof |
| 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 JP2023522124A (ja) | 2023-05-26 |
| JP2023522124A5 JP2023522124A5 (enExample) | 2024-04-18 |
| JP7864352B2 true JP7864352B2 (ja) | 2026-05-25 |
Family
ID=71108343
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022563872A Active JP7864352B2 (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 (17)
| Country | Link |
|---|---|
| US (1) | US20230348453A1 (enExample) |
| EP (2) | EP3901151B1 (enExample) |
| JP (1) | JP7864352B2 (enExample) |
| KR (1) | KR20230015343A (enExample) |
| CN (1) | CN115667255B (enExample) |
| AU (1) | AU2021258431A1 (enExample) |
| BR (1) | BR112022021476A2 (enExample) |
| CA (1) | CA3176325A1 (enExample) |
| CL (1) | CL2022002899A1 (enExample) |
| CO (1) | CO2022016245A2 (enExample) |
| CR (1) | CR20220528A (enExample) |
| IL (1) | IL297481A (enExample) |
| MX (1) | MX2022013160A (enExample) |
| PE (1) | PE20230462A1 (enExample) |
| PH (1) | PH12022552813A1 (enExample) |
| WO (1) | WO2021214117A1 (enExample) |
| ZA (1) | ZA202212631B (enExample) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3846793B1 (en) | 2018-09-07 | 2024-01-24 | PIC Therapeutics, Inc. | Eif4e inhibitors and uses thereof |
| AR121506A1 (es) | 2020-03-03 | 2022-06-08 | Pic Therapeutics Inc | Inhibidores del eif4e y sus usos |
| US12157732B2 (en) | 2021-08-25 | 2024-12-03 | PIC Therapeutics, Inc. | eIF4E inhibitors and uses thereof |
| IL310924A (en) | 2021-08-25 | 2024-04-01 | Pic Therapeutics Inc | Eif4e inhibitors and uses thereof |
| WO2023067021A1 (en) * | 2021-10-19 | 2023-04-27 | Iomx Therapeutics Ag | A synthesis scheme and procedures for preparing a sik3 inhibitor and intermediates thereof |
| US20230212246A1 (en) * | 2022-01-05 | 2023-07-06 | The Board Of Regents Of The University Of Texas System | Tgf-b as a therapeutic target for intracranial aneurysm |
| 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 |
| US12384773B2 (en) | 2023-11-02 | 2025-08-12 | Arcus Biosciences, Inc. | Thiazole compounds and methods of use thereof |
| 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 |
| EP4643861B1 (en) | 2024-04-30 | 2026-07-29 | iOmx Therapeutics AG | A halogenated heteroaryl kinase inhibitor for use in treating angiosarcoma |
Citations (4)
| 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)
| 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 |
| US5064413A (en) | 1989-11-09 | 1991-11-12 | Bioject, Inc. | Needleless hypodermic injection device |
| US5312335A (en) | 1989-11-09 | 1994-05-17 | Bioject Inc. | Needleless hypodermic injection device |
| US5383851A (en) | 1992-07-24 | 1995-01-24 | Bioject Inc. | Needleless hypodermic injection device |
| KR100919905B1 (ko) | 2005-01-26 | 2009-10-06 | 아이알엠 엘엘씨 | 단백질 키나제 억제제로서의 화합물 및 조성물 |
| WO2008033746A2 (en) | 2006-09-11 | 2008-03-20 | 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 |
| EP3177295A4 (en) | 2014-08-08 | 2018-06-13 | 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 |
| EP3589284A4 (en) | 2017-02-28 | 2020-12-16 | The General Hospital Corporation | USES OF PYRIMIDOPYRIMIDINONES AS SIK INHIBITORS |
| EP3643713B1 (en) * | 2018-10-23 | 2025-07-30 | iOmx Therapeutics AG | Heterocyclic kinase inhibitors and uses thereof |
-
2020
- 2020-04-21 EP EP20170641.3A patent/EP3901151B1/en active Active
-
2021
- 2021-04-21 US US17/996,514 patent/US20230348453A1/en active Pending
- 2021-04-21 PH PH1/2022/552813A patent/PH12022552813A1/en unknown
- 2021-04-21 MX MX2022013160A patent/MX2022013160A/es unknown
- 2021-04-21 AU AU2021258431A patent/AU2021258431A1/en active Pending
- 2021-04-21 CA CA3176325A patent/CA3176325A1/en active Pending
- 2021-04-21 KR KR1020227040346A patent/KR20230015343A/ko active Pending
- 2021-04-21 PE PE2022002448A patent/PE20230462A1/es unknown
- 2021-04-21 JP JP2022563872A patent/JP7864352B2/ja active Active
- 2021-04-21 WO PCT/EP2021/060338 patent/WO2021214117A1/en not_active Ceased
- 2021-04-21 EP EP21718920.8A patent/EP4139305A1/en active Pending
- 2021-04-21 IL IL297481A patent/IL297481A/en unknown
- 2021-04-21 BR BR112022021476A patent/BR112022021476A2/pt unknown
- 2021-04-21 CR CR20220528A patent/CR20220528A/es unknown
- 2021-04-21 CN CN202180027921.5A patent/CN115667255B/zh active Active
-
2022
- 2022-10-20 CL CL2022002899A patent/CL2022002899A1/es unknown
- 2022-11-11 CO CONC2022/0016245A patent/CO2022016245A2/es unknown
- 2022-11-21 ZA ZA2022/12631A patent/ZA202212631B/en unknown
Patent Citations (4)
| 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)
| Title |
|---|
| 長野哲雄,創薬化学 メディシナルケミストへの道,第1版第1刷,株式会社東京化学同人,2018年09月28日,第182-215頁,第7章創薬の実践的手法(2)ヒット化合物からの合成展開 |
Also Published As
| Publication number | Publication date |
|---|---|
| PH12022552813A1 (en) | 2024-03-25 |
| MX2022013160A (es) | 2023-02-09 |
| KR20230015343A (ko) | 2023-01-31 |
| CN115667255A (zh) | 2023-01-31 |
| US20230348453A1 (en) | 2023-11-02 |
| EP3901151B1 (en) | 2026-04-01 |
| CR20220528A (es) | 2023-07-13 |
| ZA202212631B (en) | 2023-07-26 |
| CL2022002899A1 (es) | 2023-06-30 |
| CN115667255B (zh) | 2025-10-28 |
| AU2021258431A1 (en) | 2022-11-17 |
| BR112022021476A2 (pt) | 2023-04-04 |
| EP4139305A1 (en) | 2023-03-01 |
| EP3901151A1 (en) | 2021-10-27 |
| PE20230462A1 (es) | 2023-03-14 |
| TW202204352A (zh) | 2022-02-01 |
| CO2022016245A2 (es) | 2023-02-27 |
| IL297481A (en) | 2022-12-01 |
| WO2021214117A1 (en) | 2021-10-28 |
| CA3176325A1 (en) | 2021-10-28 |
| JP2023522124A (ja) | 2023-05-26 |
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