AR121914A1 - Compuestos útiles para inhibir la quinasa ret - Google Patents

Compuestos útiles para inhibir la quinasa ret

Info

Publication number
AR121914A1
AR121914A1 ARP210101083A ARP210101083A AR121914A1 AR 121914 A1 AR121914 A1 AR 121914A1 AR P210101083 A ARP210101083 A AR P210101083A AR P210101083 A ARP210101083 A AR P210101083A AR 121914 A1 AR121914 A1 AR 121914A1
Authority
AR
Argentina
Prior art keywords
alkyl
heteroalkyl
halogen
independently
cycloalkyl
Prior art date
Application number
ARP210101083A
Other languages
English (en)
Inventor
Erin D Anderson
Steven W Andrews
Kevin R Condroski
Thomas C Irvin
Gabrielle R Kolakowski
Manoj Kumar
Elizabeth A Mfaddin
Megan L Mkenney
Michael J Munchhof
michael b Welch
Original Assignee
Lilly Co Eli
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 Lilly Co Eli filed Critical Lilly Co Eli
Publication of AR121914A1 publication Critical patent/AR121914A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42—Oxazoles
    • A61K31/422—Oxazoles 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/427—Thiazoles 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members 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
    • C07D231/38—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members 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
    • C07D231/38—Nitrogen atoms
    • C07D231/40—Acylated on said nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D417/02—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 two hetero rings
    • C07D417/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05—Isotopically modified compounds, e.g. labelled

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Enzymes And Modification Thereof (AREA)

Abstract

En la presente se proporcionan inhibidores de la quinasa RET de acuerdo con la fórmula (1), sales aceptables desde el punto de vista farmacéutico de estos, composiciones farmacéuticas de estos y métodos para su uso en el tratamiento de enfermedades que pueden tratarse con un inhibidor de la quinasa RET, incluidas enfermedades y trastornos asociados a RET. A, R¹, n, X¹, X², X³, X⁴, y R² tienen los significados dados en la memoria descriptiva. Reivindicación 1: Un compuesto de la fórmula (1) en donde A es un arilo o heteroarilo de cinco o seis miembros; Cada R¹ es independientemente hidrógeno, halógeno, C₁-C₆ alquilo, C₁-C₆ heteroalquilo, -(C₀-C₄ alquilo)(C₅-C₆ heteroalquilo), -(C₀-C₄ alquilo)(C₃-C₇ cicloalquilo), -(C₀-C₄ heteroalquilo)(C₃-C₇ cicloalquilo), -(C₀-C₄ alquilo)(C₄-C₇ cicloheteroalquilo), -(C₀-C₄ heteroalquilo)(C₃-C₇ cicloheteroalquilo), -(C₀-C₄ alquilo)(C₄-C₁₀ bicíclico), -(C₀-C₄ alquilo)(C₅-C₆ arilo), -(C₀-C₄ alquil)(C₅-C₆ heteroalquilo), -(C₀-C₄ alquilo)(C₄-C₁₀ heterobicíclico), C₅-C₁₂ espirano, C₅-C₁₂ heterospirano, adamantano, difluorometilsulfano o pentafluorosulfano, en donde cada R¹ está opcionalmente sustituido con uno o más grupos que son independientemente halógeno, ciano, hidroxilo, oxo, metilo, metoxi, hidroximetilo, etilo, etoxi, hidroxietilo, metilamina, N,N-dimetilmetilamina, o mono, di o trihalometilo, y en donde dos grupos R¹ pueden fusionarse para formar una estructura de anillo que incluye una porción de A y es opcionalmente aromática, y n es 1, 2 ó 3; X¹, X², X³, y X⁴ son cada uno independientemente N, CH, C-CH₃, C-CH₂-OH, C-OCH₃, C-CH₂-OCH₃, o C-halógeno; y R² es C₁-C₄ alquilo,-(C₀-C₄ alquilo)(C₃-C₇ cicloalquilo), -(C₀-C₄ alquilo)(C₄-C₇ heterocicloalquilo), -(C₀-C₄ alquilo)(C₄-C₁₀ bicíclico) cada uno opcionalmente sustituido con uno o más grupos que son independientemente deuterio, halógeno, ciano, hidroxilo, oxo, metilo, metoxi, hidroximetilo, etilo, etoxi, hidroxietilo, ciclopropilo, o mono, di o trihalometilo; o una sal aceptable desde el punto de vista farmacéutico de este.
ARP210101083A 2020-04-27 2021-04-22 Compuestos útiles para inhibir la quinasa ret AR121914A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US202063015933P 2020-04-27 2020-04-27

Publications (1)

Publication Number Publication Date
AR121914A1 true AR121914A1 (es) 2022-07-20

Family

ID=75914595

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP210101083A AR121914A1 (es) 2020-04-27 2021-04-22 Compuestos útiles para inhibir la quinasa ret

Country Status (18)

Country Link
US (2) US11613533B2 (es)
EP (1) EP4143184A1 (es)
JP (1) JP7441972B2 (es)
KR (1) KR20230005301A (es)
CN (1) CN115667253A (es)
AR (1) AR121914A1 (es)
AU (1) AU2021263541B2 (es)
BR (1) BR112022021735A2 (es)
CA (1) CA3177080A1 (es)
CL (1) CL2022003000A1 (es)
CO (1) CO2022016013A2 (es)
DO (1) DOP2022000234A (es)
EC (1) ECSP22083926A (es)
IL (1) IL297551B2 (es)
MX (1) MX2022013482A (es)
PE (1) PE20230780A1 (es)
TW (1) TWI777509B (es)
WO (1) WO2021222017A1 (es)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN116438179A (zh) * 2020-11-06 2023-07-14 伊莱利利公司 作为ret激酶抑制剂的吡唑衍生物
WO2024206858A1 (en) 2023-03-30 2024-10-03 Revolution Medicines, Inc. Compositions for inducing ras gtp hydrolysis and uses thereof

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20110189167A1 (en) * 2007-04-20 2011-08-04 Flynn Daniel L Methods and Compositions for the Treatment of Myeloproliferative Diseases and other Proliferative Diseases
BR112015023618A2 (pt) * 2013-03-15 2017-07-18 Glaxosmithkline Ip Dev Ltd derivados de piridina como inibidores de quinase reorganizada durante a transfecção (ret)
WO2017145050A1 (en) * 2016-02-23 2017-08-31 Glaxosmithkline Intellectual Property Development Limited Pyridylpyridone derivative useful as a ret kinase inhibitor in the treatment of ibs and cancer
AR107912A1 (es) * 2016-03-17 2018-06-28 Blueprint Medicines Corp Inhibidores de ret
WO2018136661A1 (en) * 2017-01-18 2018-07-26 Andrews Steven W SUBSTITUTED PYRAZOLO[1,5-a]PYRAZINE COMPOUNDS AS RET KINASE INHIBITORS
CN112566907A (zh) * 2018-08-17 2021-03-26 南京明德新药研发有限公司 作为ret抑制剂的吡唑衍生物

Also Published As

Publication number Publication date
US20210363140A1 (en) 2021-11-25
DOP2022000234A (es) 2022-11-30
CA3177080A1 (en) 2021-11-04
AU2021263541B2 (en) 2024-03-07
CO2022016013A2 (es) 2022-11-18
BR112022021735A2 (pt) 2022-12-06
EP4143184A1 (en) 2023-03-08
MX2022013482A (es) 2022-11-16
US20230312544A1 (en) 2023-10-05
CN115667253A (zh) 2023-01-31
US11613533B2 (en) 2023-03-28
TWI777509B (zh) 2022-09-11
TW202206428A (zh) 2022-02-16
JP2023523315A (ja) 2023-06-02
US11964968B2 (en) 2024-04-23
PE20230780A1 (es) 2023-05-09
WO2021222017A1 (en) 2021-11-04
IL297551B1 (en) 2024-02-01
IL297551B2 (en) 2024-06-01
CL2022003000A1 (es) 2023-06-23
AU2021263541A1 (en) 2022-11-24
KR20230005301A (ko) 2023-01-09
ECSP22083926A (es) 2022-11-30
JP7441972B2 (ja) 2024-03-01
IL297551A (en) 2022-12-01

Similar Documents

Publication Publication Date Title
AR121914A1 (es) Compuestos útiles para inhibir la quinasa ret
PE20231312A1 (es) Derivados triciclicos de carboxamida como inhibidores de la prmt5
AR117424A1 (es) Inhibidores de los receptores erbb
CO5721006A2 (es) Derivados de pirazolo-quinazolina, proceso para su preparacion y su uso como inhibidores de quinasa
AR087328A1 (es) Derivados de imidazo[1,2-b]piridazina e imidazo[4,5-b]piridina como inhibidores de jak
AR112834A1 (es) Derivados de rapamicina
AR124662A2 (es) Formulaciones inmunosupresoras
AR049284A1 (es) Compuestos derivados de 1,3-tiazol; composiciones farmaceuticas que los contienen y su uso en la preparacion de medicamentos para el tratamiento de enfermedades asociadas a la actividad de los ppard
AR099363A1 (es) Pirrolo[2,3-d]pirimidinil, pirrolo[2,3-b]pirazinil y pirrolo[2,3-d]piridinil acrilamidas
AR081994A1 (es) Derivados de [1,8]naftiridina, composiciones farmaceuticas que los contienen, proceso para prepararlos y uso de los mismos para el tratamiento de enfermedades inducidas por quinasas, en particular diferentes tipos de canceres
AR100806A1 (es) Inhibidores de fosfatidilinositol 3-quinasa
AR096846A1 (es) Dihidroquinoxalinonas y dihidropiridopirazinonas modificadas como inhibidores de la proteína bet
AR126693A1 (es) Compuestos de pirazolopiridinona
AR117398A1 (es) Inhibidores de la señalización mediada por tirosina cinasa 2
AR117900A1 (es) Pirazolopiridinas y triazolopiridinas como inhibidores de a2a / a2b
AR127308A1 (es) Inhibidores ras
AR117229A1 (es) Compuestos heteroaromáticos como inhibidores de vanina
AR046793A1 (es) Derivados de pirazol, antagonistas del receptor de la orexina
AR119728A1 (es) Derivados de 1,1-dioxido de 3-amino-4h-benzo[e][1,2,4]tiadiazina como inhibidores de mrgx2
AR124199A1 (es) Nuevos compuestos como inhibidor dual del receptor de andrógenos y de la fosfodiesterasa
AR069304A1 (es) Inhibidores del transportador equilibrativo de nucleosidos ent1
AR119378A1 (es) Formulación de nanopartículas del inhibidor de bcl-2
AR124007A1 (es) Inhibidores de la kinasa ret
BR112016009918A2 (pt) composto tendo maior inibição da atividade da proteína cinase g e método de preparação para tal
AR043921A1 (es) Derivados del acido pirido[2,3 d] pirimidin-7-carboxilico, su elaboracion y su uso como agentes farmaceuticos.