CO2022016245A2 - Heteroarilo halogenado y otros inhibidores de cinasas heterocíclicas y usos de los mismos - Google Patents

Heteroarilo halogenado y otros inhibidores de cinasas heterocíclicas y usos de los mismos

Info

Publication number
CO2022016245A2
CO2022016245A2 CONC2022/0016245A CO2022016245A CO2022016245A2 CO 2022016245 A2 CO2022016245 A2 CO 2022016245A2 CO 2022016245 A CO2022016245 A CO 2022016245A CO 2022016245 A2 CO2022016245 A2 CO 2022016245A2
Authority
CO
Colombia
Prior art keywords
kinase inhibitors
inhibitors
structurally similar
dasatinib
abl
Prior art date
Application number
CONC2022/0016245A
Other languages
English (en)
Inventor
Peter Sennhenn
Stefan Bissinger
Hannes Loferer
David Bancroft
Tillmann Michels
Nisit Khandelwal
Original Assignee
Iomx Therapeutics Ag
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 Iomx Therapeutics Ag filed Critical Iomx Therapeutics Ag
Publication of CO2022016245A2 publication Critical patent/CO2022016245A2/es

Links

Classifications

    • 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
    • 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
    • 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
    • G01N33/574—Immunoassay; Biospecific binding assay; Materials therefor for cancer
    • G01N33/57484—Immunoassay; Biospecific binding assay; Materials therefor for cancer involving compounds serving as markers for tumor, cancer, neoplasia, e.g. cellular determinants, receptors, heat shock/stress proteins, A-protein, oligosaccharides, metabolites
    • G01N33/57496—Immunoassay; Biospecific binding assay; Materials therefor for cancer involving compounds serving as markers for tumor, cancer, neoplasia, e.g. cellular determinants, receptors, heat shock/stress proteins, A-protein, oligosaccharides, 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)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Cell Biology (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Molecular Biology (AREA)
  • Biomedical Technology (AREA)
  • Urology & Nephrology (AREA)
  • Hematology (AREA)
  • Pathology (AREA)
  • Analytical Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Oncology (AREA)
  • Biotechnology (AREA)
  • Hospice & Palliative Care (AREA)
  • Microbiology (AREA)
  • Physics & Mathematics (AREA)
  • Biochemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • General Physics & Mathematics (AREA)
  • Food Science & Technology (AREA)
  • Zoology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Genetics & Genomics (AREA)
  • Epidemiology (AREA)
  • Wood Science & Technology (AREA)
  • Biophysics (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)

Abstract

La invención se refiere a inhibidores de cinasa, en particular inhibidores de la proteína cinasas que incluye la superfamilia SIK CSF1R, ABL/BCR-ABL, SRC, HCK, PDGFR, KIT y/o sus mutantes. Aunque estructuralmente similares al dasatinib, los inhibidores de cinasa de la invención son distintivos; poseen una clase particular de heteroarilos halogenados. Estos inhibidores de cinasa pueden mostrar una o más ciertas propiedades distintas al dasatinib y otros inhibidores de cinasa estructuralmente similares. Los inhibidores de cinasa de la invención o composiciones farmacéuticas que los comprenden se pueden usar en el tratamiento de un trastorno o afección, tal como un trastorno proliferativo, por ejemplo, una leucemia o tumor sólido. 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 fenotípica mezclada (MPAL) - caracterizada por (entre otras cosas) la presencia de la proteína MEF2C, una translocación cromosómica humana en 11q23, y/o una oncoproteína de fusión KMT2A. Los inhibidores de cinasa o composiciones farmacéuticas descritas en la presente se pueden usar tópicamente para modular la pigmentación de la piel en un sujeto, por ejemplo para impartir protección UV y reducir el riesgo de cáncer de piel.
CONC2022/0016245A 2020-04-21 2022-11-11 Heteroarilo halogenado y otros inhibidores de cinasas heterocíclicas y usos de los mismos CO2022016245A2 (es)

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
CO2022016245A2 true CO2022016245A2 (es) 2023-02-27

Family

ID=71108343

Family Applications (1)

Application Number Title Priority Date Filing Date
CONC2022/0016245A CO2022016245A2 (es) 2020-04-21 2022-11-11 Heteroarilo halogenado y otros inhibidores de cinasas heterocíclicas y usos de los mismos

Country Status (17)

Country Link
US (1) US20230348453A1 (es)
EP (2) EP3901151A1 (es)
JP (1) JP2023522124A (es)
KR (1) KR20230015343A (es)
CN (1) CN115667255A (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)
TW (1) TW202204352A (es)
WO (1) WO2021214117A1 (es)
ZA (1) ZA202212631B (es)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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

Family Cites Families (25)

* 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
US4475916A (en) 1982-03-18 1984-10-09 Merck & Co., Inc. Osmotic drug delivery system
US4439196A (en) 1982-03-18 1984-03-27 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
EP1841431A4 (en) 2005-01-26 2009-12-09 Irm Llc COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHIBITORS
EP2061468A4 (en) 2006-09-11 2011-05-04 Curis Inc TYROSINE KINASE INHIBITORS CONTAINING ZINC BINDING CHARACTERISTIC GROUP
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
RU2019129727A (ru) 2017-02-28 2021-03-30 Зэ Дженерал Хоспитал Корпорэйшн Применения пиримидопиримидинонов в качестве ингибиторов sik
DK3391907T3 (da) 2017-04-20 2020-03-09 Iomx Therapeutics Ag Intracellulær kinase sik3, der er associeret med resistens over for antitumorimmunresponser, og anvendelser deraf
EP3643713A1 (en) * 2018-10-23 2020-04-29 iOmx Therapeutics AG Heterocyclic kinase inhibitors and uses thereof

Also Published As

Publication number Publication date
AU2021258431A1 (en) 2022-11-17
EP4139305A1 (en) 2023-03-01
MX2022013160A (es) 2023-02-09
WO2021214117A1 (en) 2021-10-28
IL297481A (en) 2022-12-01
JP2023522124A (ja) 2023-05-26
PE20230462A1 (es) 2023-03-14
ZA202212631B (en) 2023-07-26
EP3901151A1 (en) 2021-10-27
CA3176325A1 (en) 2021-10-28
US20230348453A1 (en) 2023-11-02
BR112022021476A2 (pt) 2023-04-04
TW202204352A (zh) 2022-02-01
KR20230015343A (ko) 2023-01-31
CN115667255A (zh) 2023-01-31
CL2022002899A1 (es) 2023-06-30
CR20220528A (es) 2023-07-13

Similar Documents

Publication Publication Date Title
CO2022016245A2 (es) Heteroarilo halogenado y otros inhibidores de cinasas heterocíclicas y usos de los mismos
ECSP22011692A (es) Compuestos de imidazolil pirimidinilamina como inhibidores de cdk2
WO2021219731A3 (en) Bicyclic kinase inhibitors and uses thereof
CO2019011873A2 (es) Compuestos de heteroarilo bicíclicos 6–6 fusionados y su uso como inhibidores de lats
GT201400113A (es) Benzotienilo-pirrolotriazinas disustituidas y sus usos
CR20170116A (es) Compuestos que inhiben la proteina mcl-1
CO2021017981A2 (es) Inhibidores heterobicíclicos de mat2a y métodos de uso para el tratamiento del cáncer
PE20152000A1 (es) Inhibidores quinazolinicos de formas mutadas activantes del receptor del factor de crecimiento epidermico
CL2021001722A1 (es) Inhibidores aza-heterobicíclicos de mat2a y métodos de uso en el tratamiento de cáncer
CL2012003680A1 (es) Compuestos derivados de (1,8) naftiridinas 2,4 diaril sustituidas inhibidores de quinasas; su procedimiento de obtencion; composicion farmaceutica; y su uso para el tratamiento y/o prevencion de cancer, tumor, tumores malignos, entre otros; kit farmaceutico.
ECSP109957A (es) Derivados de pirimidinil-piridazinona.
CL2011000880A1 (es) Compuestos derivados de pirazolo[1,5-a]pirimidin-3-il, inhibidores de tirosina de la familia trk cinasa; proceso para la preparacion de los compuestos; composicion farmaceutica que comprende a uno de los compuestos; y uso de los compuestos en la preparacion de medicamentos utiles para el tratamiento del dolor y del cancer.
CL2021001721A1 (es) Inhibidores aza-heterobicíclicos de mat2a y métodos de uso para tratar el cáncer
CO2022015054A2 (es) [1,3]diazino[5,4-d]pirimidinas como inhibidores de her2
AR100431A1 (es) Compuestos de pladienolida piridina y métodos de uso
DOP2005000014A (es) Derivados 1h-tieno[2, 3-c] pirazol utiles como inhibidores de quinasa
CL2011000489A1 (es) Compuestos derivados de pirimido[5,4-d]pirimidina, los cuales actuan como inhibidores de tirosina-quinasas; y composiciones farmaceuticas que los comprenden, utiles en el tratamiento de enfermedades que se caracterizan por una proliferacion celular excesiva o anomala
UY38228A (es) Compuestos de triazolopirimidina y su uso en el tratamiento del cáncer
MX2019012847A (es) Compuestos de c5-anilinoquinazolina y su uso en el tratamiento del cancer.
PE20191486A1 (es) COMPUESTOS DE TIPO IMIDAZO[4,5-c]QUINOLIN-2-ONA DEUTERADOS Y SU USO EN EL TRATAMIENTO DEL CANCER
CL2023002633A1 (es) Derivados de uracilo como inhibidores de trpa1
CO2022012884A2 (es) Compuestos de amino pirimidina fusionados
ECSP099539A (es) Derivados de 3-cinolinacarboxamida y su uso para tratar el cáncer
CO2023012903A2 (es) Derivados de pirimidina útiles como inhibidores de la proteína cinasa de repetición 2 rica en leucina (lrrk2)
MX2018008507A (es) Inhibición de proteína relacionada con ataxia telangiectasia y rad3 (atr).