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 mismos

Info

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
Application number
PE2022002448A
Other languages
English (en)
Inventor
Peter Sennhenn
Nisit Khandelwal
David Bancroft
Stefan Bissinger
Hannes Loferer
Tillmann Michels
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 PE20230462A1 publication Critical patent/PE20230462A1/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
    • 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
    • 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

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).
PE2022002448A 2020-04-21 2021-04-21 Heteroarilo halogenado y otros inhibidores de cinasas heterociclicas y usos de los mismos PE20230462A1 (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
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 (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
ZA202212631B (en) 2023-07-26
EP3901151A1 (en) 2021-10-27
CA3176325A1 (en) 2021-10-28
CO2022016245A2 (es) 2023-02-27
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
PE20230462A1 (es) Heteroarilo halogenado y otros inhibidores de cinasas heterociclicas y usos de los mismos
PE20040156A1 (es) 2-heteroaril-pirimidinas como inhibidores de quinasa dependiente de ciclina
PE20221283A1 (es) Compuestos triciclicos sustituidos
PE20220592A1 (es) Inhibidores de la autofagia de heteroarilaminopirimidina amida y metodos de uso de estos
PE20220141A1 (es) Inhibidores de la proteina tirosina fosfatasa
AR045762A1 (es) Derivados de quinazolina
PE20141827A1 (es) Inhibidores de proteinas quinasas
CR9690A (es) 3-acilaminobenzanilidas insecticidas
AR067562A1 (es) Compuestos heterociclicos inhibidores de kinasa
PE20170189A1 (es) Nuevos derivados de pirazolo pirimidina y su uso como inhibidores de malt1
AR056691A1 (es) Derivados pirrolopirimidina como inhibidores de syk
PE20060664A1 (es) Amidas biciclicas como inhibidores de cinasa
PE20040927A1 (es) Derivados de 1-propanolol y 1-propilamina, como ligandos de receptores de glucocorticoides
CL2019003198A1 (es) Tienopiridinas y benzotiofenos útiles como inhibidores de cinasa 4 asociada al receptor de interleucina 1 (irak4).
PE20191540A1 (es) DERIVADOS DE PIRROLO [1,2-b] PIRIDAZINA
PE20211049A1 (es) Compuestos de sulfonilurea como inhibidores de la actividad de interleucina 1
PE20120034A1 (es) Compuestos derivados de n-fenilpirimidin-2-amina
CL2021000361A1 (es) Nuevos compuestos heterocíclicos como inhibidores de monoacilglicerol lipasa
PE20211585A1 (es) Agente profilactico o terapeutico para atrofia muscular espinal
PE20130184A1 (es) Compuesto heterociclico
PE20091492A1 (es) Compuestos y composiciones como inhibidores de c-kit y de la cinasa pdgfr
PE20120107A1 (es) Inhibidores de proteina cinasa
EA200801001A1 (ru) Соединения, которые обладают активностью по отношению к рецепторам м, и их применения в медицине
PE20210176A1 (es) Inhibidores de arginasa y sus metodos de uso
PE20120120A1 (es) DERIVADOS DE 2H-PIRAZOLO[3,4-d]PIRIMIDINA-4,6(5H,7H)-DIONA, COMO INHIBIDORES DE PDE1