PE20230462A1 - Heteroarilo halogenado y otros inhibidores de cinasas heterociclicas y usos de los mismos - Google Patents
Heteroarilo halogenado y otros inhibidores de cinasas heterociclicas y usos de los mismosInfo
- Publication number
- PE20230462A1 PE20230462A1 PE2022002448A PE2022002448A PE20230462A1 PE 20230462 A1 PE20230462 A1 PE 20230462A1 PE 2022002448 A PE2022002448 A PE 2022002448A PE 2022002448 A PE2022002448 A PE 2022002448A PE 20230462 A1 PE20230462 A1 PE 20230462A1
- Authority
- PE
- Peru
- Prior art keywords
- alkynyl
- cycloalkyl
- alkenyl
- aryl
- alkyl
- Prior art date
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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
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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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
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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
- 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
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- 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
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- 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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- G01N33/57595—
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- 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
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- 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
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- 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)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Pathology (AREA)
- Analytical Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Zoology (AREA)
- Wood Science & Technology (AREA)
- Genetics & Genomics (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Molecular Biology (AREA)
- Microbiology (AREA)
- Biotechnology (AREA)
- Physics & Mathematics (AREA)
- Oncology (AREA)
- Hospice & Palliative Care (AREA)
- Biochemistry (AREA)
- Biophysics (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Engineering & Computer Science (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Cell Biology (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Biomedical Technology (AREA)
- Hematology (AREA)
- Urology & Nephrology (AREA)
- Plural Heterocyclic Compounds (AREA)
- Food Science & Technology (AREA)
Abstract
Referida a un compuesto seleccionado del grupo CARACTERIZADO porque consiste en un inhibidor de cinasa de la formula (Ia), donde: Hy es a heteroarilo o heterociclilo que se sustituyen opcionalmente con R1e; R1e es R1a , R1b, R1c o R1d; R1a y R1d son H, alquilo, alquenilo, alquinilo, cicloalquilo, arilo, heterociclilo, entre otros; R1b y R1c son H, alquilo de C1-6, alquenilo de C2-6, alquinilo de C2-6, cicloalquilo de C3-7, arilo de C6-10, heteroarilo de 3 a 7 miembros, entre otros; R2 es H; R3 es H, alquilo, alquenilo, alquinilo, cicloalquilo, arilo, entre otros; R4 es H; R5 es -L-R6 15 ; L es una union, alquileno de C1-6, alquenileno de C2-6, entre otros; R6 es a heteroarilo monociclico de 5 miembros que contiene al menos un atomo de anillo S y que se sustituye con uno o mas independientemente seleccionado R7; R7 es alquilo, alquenilo, alquinilo, cicloalquilo, arilo, heterociclilo, heteroarilo, halogeno, -CN, azido, -NO2, entre otros; E es O, o S. Dichos compuestos son inhibidores de cinasa, en particular inhibidores de la proteina cinasas que incluye la superfamilia SIK CSF1R, ABL/BCR-ABL, SRC, HCK, PDGFR, KIT y/o sus mutantes. En particular, estos y otros inhibidores de cinasa estructuralmente similares se pueden usar en el tratamiento de un trastorno proliferativo tal como una leucemia aguda fenotipica mezclada (MPAL).
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP20170641.3A EP3901151A1 (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 (1)
| Publication Number | Publication Date |
|---|---|
| PE20230462A1 true PE20230462A1 (es) | 2023-03-14 |
Family
ID=71108343
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2022002448A PE20230462A1 (es) | 2020-04-21 | 2021-04-21 | Heteroarilo halogenado y otros inhibidores de cinasas heterociclicas y usos de los mismos |
Country Status (18)
| Country | Link |
|---|---|
| US (1) | US20230348453A1 (es) |
| EP (2) | EP3901151A1 (es) |
| JP (1) | JP2023522124A (es) |
| KR (1) | KR20230015343A (es) |
| CN (1) | CN115667255B (es) |
| AU (1) | AU2021258431A1 (es) |
| BR (1) | BR112022021476A2 (es) |
| CA (1) | CA3176325A1 (es) |
| CL (1) | CL2022002899A1 (es) |
| CO (1) | CO2022016245A2 (es) |
| CR (1) | CR20220528A (es) |
| IL (1) | IL297481A (es) |
| MX (1) | MX2022013160A (es) |
| PE (1) | PE20230462A1 (es) |
| PH (1) | PH12022552813A1 (es) |
| TW (1) | TW202204352A (es) |
| WO (1) | WO2021214117A1 (es) |
| ZA (1) | ZA202212631B (es) |
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 |
| TW202146393A (zh) | 2020-03-03 | 2021-12-16 | 美商皮克醫療公司 | Eif4e抑制劑及其用途 |
| JP2024532276A (ja) | 2021-08-25 | 2024-09-05 | 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 |
| US12234231B2 (en) | 2021-08-25 | 2025-02-25 | PIC Therapeutics, Inc. | EIF4E inhibitors and uses thereof |
| US20250296928A1 (en) * | 2021-10-19 | 2025-09-25 | 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 |
| EP4257132A1 (en) | 2022-04-08 | 2023-10-11 | iOmx Therapeutics AG | Sik3 inhibitors for treating diseases resistant to death receptor signalling |
| EP4257609A1 (en) | 2022-04-08 | 2023-10-11 | iOmx Therapeutics AG | Combination therapies based on pd-1 inhibitors and sik3 inhibitors |
| 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 |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| 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 |
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| CA2593803A1 (en) | 2005-01-26 | 2006-08-03 | Irm Llc | Thiazole-amide compounds and compsitions as protein kinase inhibitors |
| EP2061468A4 (en) | 2006-09-11 | 2011-05-04 | Curis Inc | TYROSINE KINASE INHIBITORS CONTAINING ZINC BINDING CHARACTERISTIC GROUP |
| US20100113520A1 (en) * | 2008-11-05 | 2010-05-06 | Principia Biopharma, Inc. | Kinase knockdown via electrophilically enhanced inhibitors |
| US8907053B2 (en) | 2010-06-25 | 2014-12-09 | Aurigene Discovery Technologies Limited | Immunosuppression modulating compounds |
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| 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 |
| BR112019017741A2 (pt) | 2017-02-28 | 2020-04-07 | Dana Farber Cancer Inst Inc | usos de pirimidopirimidinonas como inibidores de sik |
| EP3391907B8 (en) | 2017-04-20 | 2020-03-04 | iOmx Therapeutics AG | Intracellular kinase sik3 associated with resistance against anti-tumour immune responses, and uses thereof |
| 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/EP3901151A1/en active Pending
-
2021
- 2021-04-21 EP EP21718920.8A patent/EP4139305A1/en active Pending
- 2021-04-21 BR BR112022021476A patent/BR112022021476A2/pt unknown
- 2021-04-21 AU AU2021258431A patent/AU2021258431A1/en active Pending
- 2021-04-21 MX MX2022013160A patent/MX2022013160A/es unknown
- 2021-04-21 KR KR1020227040346A patent/KR20230015343A/ko active Pending
- 2021-04-21 CN CN202180027921.5A patent/CN115667255B/zh active Active
- 2021-04-21 WO PCT/EP2021/060338 patent/WO2021214117A1/en not_active Ceased
- 2021-04-21 CR CR20220528A patent/CR20220528A/es unknown
- 2021-04-21 TW TW110114388A patent/TW202204352A/zh unknown
- 2021-04-21 JP JP2022563872A patent/JP2023522124A/ja active Pending
- 2021-04-21 CA CA3176325A patent/CA3176325A1/en active Pending
- 2021-04-21 PE PE2022002448A patent/PE20230462A1/es unknown
- 2021-04-21 US US17/996,514 patent/US20230348453A1/en active Pending
- 2021-04-21 IL IL297481A patent/IL297481A/en unknown
- 2021-04-21 PH PH1/2022/552813A patent/PH12022552813A1/en unknown
-
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
Also Published As
| Publication number | Publication date |
|---|---|
| EP3901151A1 (en) | 2021-10-27 |
| BR112022021476A2 (pt) | 2023-04-04 |
| ZA202212631B (en) | 2023-07-26 |
| JP2023522124A (ja) | 2023-05-26 |
| CA3176325A1 (en) | 2021-10-28 |
| KR20230015343A (ko) | 2023-01-31 |
| MX2022013160A (es) | 2023-02-09 |
| PH12022552813A1 (en) | 2024-03-25 |
| AU2021258431A1 (en) | 2022-11-17 |
| US20230348453A1 (en) | 2023-11-02 |
| CN115667255A (zh) | 2023-01-31 |
| WO2021214117A1 (en) | 2021-10-28 |
| CL2022002899A1 (es) | 2023-06-30 |
| EP4139305A1 (en) | 2023-03-01 |
| CN115667255B (zh) | 2025-10-28 |
| TW202204352A (zh) | 2022-02-01 |
| CO2022016245A2 (es) | 2023-02-27 |
| CR20220528A (es) | 2023-07-13 |
| IL297481A (en) | 2022-12-01 |
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