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AR114164A1 - Piridopirimidinonas sustituidas con bencilamino y derivados como inhibidores de sos1 - Google Patents

Piridopirimidinonas sustituidas con bencilamino y derivados como inhibidores de sos1

Info

Publication number
AR114164A1
AR114164A1 ARP180103772A ARP180103772A AR114164A1 AR 114164 A1 AR114164 A1 AR 114164A1 AR P180103772 A ARP180103772 A AR P180103772A AR P180103772 A ARP180103772 A AR P180103772A AR 114164 A1 AR114164 A1 AR 114164A1
Authority
AR
Argentina
Prior art keywords
alkyl
haloalkyl
group
membered
cycloalkyl
Prior art date
Application number
ARP180103772A
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English (en)
Inventor
Heinz Stadtmueller
Christiane Kofink
Juergen Ramharter
Julian Wippich
Marco Santagostino
Stefan Goepper
Annika Gille
Markus Frank
Markus Ostermeier
Fabio Savarese
Dorothea Ingrid RUDOLPH
Michael Gmachl
Anke Baum
Marco Hans Hofmann
Tobias Wunberg
Original Assignee
Boehringer Ingelheim Int
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.)
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Application filed by Boehringer Ingelheim Int filed Critical Boehringer Ingelheim Int
Publication of AR114164A1 publication Critical patent/AR114164A1/es

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • 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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • C07D453/00—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
    • C07D453/02—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

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  • 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)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

Uso de éstos compuestos como inhibidores de SOS1, composiciones farmacéuticas que los contienen y su empleo en el tratamiento y/o prevención de enfermedades oncológicas. Reivindicación 1: Un compuesto caracterizado por la fórmula (1), donde R¹ es Rᵃ¹; Rᵃ¹ se selecciona del grupo que consiste en alquilo C₁₋₆, haloalquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, cicloalquilo C₃₋₁₀, cicloalquenilo C₄₋₁₀, heterociclilo de 3 - 10 miembros, arilo C₆₋₁₀ y heteroarilo de 5 - 10 miembros, donde el alquilo C₁₋₆, haloalquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, cicloalquilo C₃₋₁₀, cicloalquenilo C₄₋₁₀, heterociclilo de 3 - 10 miembros, arilo C₆₋₁₀ y heteroarilo de 5 - 10 miembros están todos opcionalmente sustituidos con uno o más Rᵇ¹ y/o Rᶜ¹ idénticos o diferentes; cada Rᵇ¹ se selecciona de modo independiente del grupo que consiste en -ORᶜ¹, -NRᶜ¹Rᶜ¹, halógeno, -CN, -C(O)Rᶜ¹, -C(O)ORᶜ¹, -C(O)NRᶜ¹Rᶜ¹, -S(O)₂Rᶜ¹, -S(O)₂NRᶜ¹Rᶜ¹, -NHC(O)Rᶜ¹, -N(alquilo C₁₋₄)C(O)Rᶜ¹, -NHC(O)ORᶜ¹ y -N(alquilo C₁₋₄)C(O)ORᶜ¹; cada Rᶜ¹ se selecciona de modo independiente del grupo que consiste en hidrógeno, alquilo C₁₋₆, haloalquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, cicloalquilo C₃₋₁₀, cicloalquenilo C₄₋₁₀, heterociclilo de 3 - 10 miembros, arilo C₆₋₁₀ y heteroarilo de 5 - 10 miembros, donde el alquilo C₁₋₆, haloalquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, cicloalquilo C₃₋₁₀, cicloalquenilo C₄₋₁₀, heterociclilo de 3 - 10 miembros, arilo C₆₋₁₀ y heteroarilo de 5 - 10 miembros están todos opcionalmente sustituidos con uno o más, Rᵈ¹ y/o Rᵉ¹ idénticos o diferentes; cada Rᵈ¹ se selecciona de modo independiente del grupo que consiste en -ORᵉ¹, -NRᵉ¹Rᵉ¹, halógeno, -CN, -C(O)Rᵉ¹, -C(O)ORᵉ¹, -C(O)NRᵉ¹Rᵉ¹, -S(O)₂Rᵉ¹, -S(O)₂NRᵉ¹Rᵉ¹, -NHC(O)Rᵉ¹, -N(alquilo C₁₋₄)C(O)ORᵉ¹, -NHC(O)ORᵉ¹ y -N(alquilo C₁₋₄)C(O)ORᵉ¹; cada Rᵉ¹ se selecciona de modo independiente del grupo que consiste en hidrógeno, alquilo C₁₋₆, haloalquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, cicloalquilo C₃₋₁₀, cicloalquenilo C₄₋₁₀, heterociclilo de 3 - 10 miembros, arilo C₆₋₁₀ y heteroarilo de 5 - 10 miembros; R² se selecciona del grupo que consiste en hidrógeno, alquilo C₁₋₄, cicloalquilo C₃₋₆, heterociclilo de 3 - 6 miembros y halógeno; R³ se selecciona del grupo que consiste en hidrógeno, alquilo C₁₋₄ y haloalquilo C₁₋₄; el sistema anular A se selecciona del grupo que consiste en arilo C₆₋₁₀, heteroarilo de 5 - 10 miembros y heterociclilo bicíclico de 9 - 10 miembros; p indica 1, 2 ó 3; cada R⁴ se selecciona de modo independiente del grupo que consiste en alquilo C₁₋₄, alquenilo C₂₋₄, alquinilo C₂₋₄, haloalquilo C₁₋₄, hidroxi-alquilo C₁₋₄, hidroxi-haloalquilo C₁₋₄, cicloalquilo C₃₋₆, heterociclilo de 3 - 6 miembros, hidroxi-cicloalquilo C₃₋₆, haloalquilo C₁₋₄ sustituido con un heterociclilo de 3 - 6 miembros, heterociclilo de 3 - 6 miembros sustituido con hidroxi, halógeno, -NH₂, -SO₂-alquilo C₁₋₄ y el sustituyente bivalente =O, mientras que =O solo puede ser un sustituyente en un anillo no aromático; o una de sus sales.
ARP180103772A 2017-12-21 2018-12-20 Piridopirimidinonas sustituidas con bencilamino y derivados como inhibidores de sos1 AR114164A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP17209865 2017-12-21

Publications (1)

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AR114164A1 true AR114164A1 (es) 2020-07-29

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ARP180103772A AR114164A1 (es) 2017-12-21 2018-12-20 Piridopirimidinonas sustituidas con bencilamino y derivados como inhibidores de sos1

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US (2) US10829487B2 (es)
EP (2) EP3728254B1 (es)
JP (1) JP7189956B2 (es)
KR (1) KR102746913B1 (es)
CN (1) CN111372932B (es)
AR (1) AR114164A1 (es)
AU (1) AU2018390927B2 (es)
BR (1) BR112020010123A2 (es)
CA (1) CA3085835A1 (es)
CL (2) CL2020001501A1 (es)
CO (1) CO2020007218A2 (es)
CR (2) CR20210307A (es)
DK (1) DK3728254T3 (es)
EA (1) EA202091491A1 (es)
EC (1) ECSP20040257A (es)
ES (1) ES2944306T3 (es)
FI (1) FI3728254T3 (es)
HR (1) HRP20230400T1 (es)
HU (1) HUE062076T2 (es)
IL (1) IL275379B2 (es)
JO (1) JOP20200154A1 (es)
LT (1) LT3728254T (es)
MA (1) MA51290A (es)
MX (1) MX2020006438A (es)
MY (1) MY208632A (es)
PE (1) PE20210163A1 (es)
PH (1) PH12020550786A1 (es)
PL (1) PL3728254T3 (es)
PT (1) PT3728254T (es)
RS (1) RS64167B1 (es)
SA (1) SA520412278B1 (es)
SG (1) SG11202005881YA (es)
SI (1) SI3728254T1 (es)
TW (2) TWI870922B (es)
UA (1) UA126173C2 (es)
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