AR120401A1 - BICYCLIC HETEROARYL COMPOUNDS AND USES OF THESE - Google Patents

BICYCLIC HETEROARYL COMPOUNDS AND USES OF THESE

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Publication number
AR120401A1
AR120401A1 ARP200103074A ARP200103074A AR120401A1 AR 120401 A1 AR120401 A1 AR 120401A1 AR P200103074 A ARP200103074 A AR P200103074A AR P200103074 A ARP200103074 A AR P200103074A AR 120401 A1 AR120401 A1 AR 120401A1
Authority
AR
Argentina
Prior art keywords
membered
alkyl
optionally substituted
group
membered heterocyclyl
Prior art date
Application number
ARP200103074A
Other languages
Spanish (es)
Inventor
Adrian Liam Gill
Andreas Buckl
Elena S Koltun
Naing Aay
Arlyn A Tambo-Ong
Severin Thompson
Micah James Gliedt
John E Knox
James Cregg
Anne V Edwards
Yang Liu
G Leslie Burnett
William D Thomas
Original Assignee
Revolution Medicines Inc
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 Revolution Medicines Inc filed Critical Revolution Medicines Inc
Publication of AR120401A1 publication Critical patent/AR120401A1/en

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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

La presente descripción se refiere a moduladores de SOS1 y su uso en el tratamiento de enfermedades. También se describen composiciones farmacéuticas que los comprenden. Reivindicación 1: Un compuesto que tiene la estructura de la fórmula (1) o una sal, solvato, isómero, profármaco o tautómero farmacéuticamente aceptable de estos, caracterizado porque: R¹ se selecciona del grupo que consiste en cicloalquilo de 3 - 6 miembros opcionalmente sustituido, heterociclilo de 3 - 6 miembros opcionalmente sustituido, arilo de 6 miembros opcionalmente sustituido, y heteroarilo de 5 - 6 miembros opcionalmente sustituido; R² se selecciona del grupo que consiste en H, alquilo C₁₋₆, halógeno, -NHR²ᵃ, -OR²ᵃ, ciclopropilo, y -CN; en donde alquilo C₁₋₆ está opcionalmente sustituido con halógeno, -NHR²ᵃ, -OR²ᵃ, o heterociclilo de 5 - 6 miembros, y en donde, además, R²ᵃ se selecciona del grupo que consiste en H, alquilo C₁₋₆, heterociclilo de 3 - 6 miembros, y haloalquilo C₁₋₆; R³ se selecciona del grupo que consiste en H, alquilo C₁₋₃, -OR³ᵃ, ciclopropilo, y heterociclilo de 3 - 6 miembros, en donde cada uno de alquilo C₁₋₃, ciclopropilo, y heterociclilo de 3 - 6 miembros opcionalmente sustituido con R³ᵃ, y en donde, además, R³ᵃ se selecciona del grupo que consiste en alquilo C₁₋₃, halógeno, -OH, o -CN; L⁴ se selecciona del grupo que consiste en enlace, -C(O)-, -C(O)O-, -C(O)NH(CH₂)ₒ-, -NH-, -S-, -S(O)₂-, un compuesto del grupo de fórmulas (2), -(CH₂)ₚ-, y -O-; en donde o es 0, 1, ó 2; y en donde p es un número de 1 a 6; y R⁴ se selecciona del grupo que consiste en H, alquilo C₁₋₆, cicloalquilo de 3 - 14 miembros, cicloalquenilo de 3 - 14 miembros, heterociclilo de 3 - 14 miembros, arilo de 6 - 10 miembros, y heteroarilo de 5 - 10 miembros, en donde cada alquilo C₁₋₆, cicloalquilo de 3 - 14 miembros, cicloalquenilo de 3 - 14 miembros, heterociclilo de 3 - 14 miembros, arilo de 6 - 10 miembros, y heteroarilo de 5 - 10 miembros está opcionalmente sustituido con alquilo C₁₋₆, -R⁴ᵃ, -OR⁴ᵃ, -O-alquilo C₁₋₆-R⁴ᵃ, =O, halógeno, -C(O)R⁴ᵃ, -C(OO)R⁴ᵃ, -C(O)NR⁴ᵇR⁴ᶜ, -NR⁴ᵇC(O)R⁴ᶜ, -CN, =NR⁴ᵃ, -NR⁴ᵇR⁴ᶜ, -SO₂R⁴ᵃ, cicloalquilo de 3 - 6 miembros opcionalmente sustituido con R⁴ᵃ, heterociclilo de 3 - 7 miembros opcionalmente sustituido con R⁴ᵃ, arilo de 6 - 10 miembros opcionalmente sustituido con R⁴ᵃ, o heteroarilo de 5 - 10 miembros opcionalmente sustituido con R⁴ᵃ; en donde R⁴ᵃ es H, alquilo C₁₋₆, haloalquilo C₁₋₆, -C(O)R⁴ᵇ, -C(O)NR⁴ᵇR⁴ᶜ, =O, cicloalquilo de 3 - 6 miembros, arilo de 6 - 10 miembros opcionalmente sustituido con -OR⁴ᵇ, -CN, =N-cicloalquilo de 3 - 6 miembros, heterociclilo de 3 - 7 miembros, -(CH₂)ʳOCH₃, o -(CH₂)ʳOH, en donde r es 1, 2, ó 3; en donde cada R⁴ᵇ es independientemente H, alquilo C₁₋₆; y en donde cada R⁴ᶜ es independientemente H o alquilo C₁₋₆.The present description relates to modulators of SOS1 and their use in the treatment of diseases. Pharmaceutical compositions comprising them are also described. Claim 1: A compound having the structure of formula (1) or a pharmaceutically acceptable salt, solvate, isomer, prodrug or tautomer thereof, characterized in that: R¹ is selected from the group consisting of optionally substituted 3-6 membered cycloalkyl , optionally substituted 3-6 membered heterocyclyl, optionally substituted 6 membered aryl, and optionally substituted 5-6 membered heteroaryl; R² is selected from the group consisting of H, C₁₋₆ alkyl, halogen, -NHR²ᵃ, -OR²ᵃ, cyclopropyl, and -CN; wherein C₁₋₆ alkyl is optionally substituted with halogen, -NHR²ᵃ, -OR²ᵃ, or 5-6 membered heterocyclyl, and wherein further R²ᵃ is selected from the group consisting of H, C₁₋₆ alkyl, 3-membered heterocyclyl - 6 members, and C₁₋₆ haloalkyl; R³ is selected from the group consisting of H, C₁₋₃ alkyl, -OR³ᵃ, cyclopropyl, and 3-6 membered heterocyclyl, wherein each of C₁₋₃ alkyl, cyclopropyl, and 3-6 membered heterocyclyl optionally substituted with R³ᵃ, and wherein, further, R³ᵃ is selected from the group consisting of C₁₋₃ alkyl, halogen, -OH, or -CN; L⁴ is selected from the group consisting of bond, -C(O)-, -C(O)O-, -C(O)NH(CH₂)ₒ-, -NH-, -S-, -S(O) ₂-, a compound of the group of formulas (2), -(CH₂)ₚ-, and -O-; where o is 0, 1, or 2; and where p is a number from 1 to 6; and R⁴ is selected from the group consisting of H, C₁₋₆ alkyl, 3-14 membered cycloalkyl, 3-14 membered cycloalkenyl, 3-14 membered heterocyclyl, 6-10 membered aryl, and 5-10 membered heteroaryl. wherein each C₁₋₆ alkyl, 3-14 membered cycloalkyl, 3-14 membered cycloalkenyl, 3-14 membered heterocyclyl, 6-10 membered aryl, and 5-10 membered heteroaryl is optionally substituted with alkyl C₁₋₆, -R⁴ᵃ, -OR⁴ᵃ, -O-C₁₋₆-R⁴ᵃ-alkyl, =O, halogen, -C(O)R⁴ᵃ, -C(OO)R⁴ᵃ, -C(O)NR⁴ᵇR⁴ᶜ, -NR⁴ᵇC(O )R⁴ᶜ, -CN, =NR⁴ᵃ, -NR⁴ᵇR⁴ᶜ, -SO₂R⁴ᵃ, 3-6 membered cycloalkyl optionally substituted by R⁴ᵃ, 3-7 membered heterocyclyl optionally substituted by R⁴ᵃ, 6-10 membered aryl optionally substituted by R⁴ᵃ, or heteroaryl 5-10 membered optionally substituted with R⁴ᵃ; wherein R⁴ᵃ is H, C₁₋₆ alkyl, C₁₋₆ haloalkyl, -C(O)R⁴ᵇ, -C(O)NR⁴ᵇR⁴ᶜ, =O, 3-6 membered cycloalkyl, 6-10 membered aryl optionally substituted with - OR⁴ᵇ, -CN, =N-3-6 membered cycloalkyl, 3-7 membered heterocyclyl, -(CH₂)ʳOCH₃, or -(CH₂)ʳOH, where r is 1, 2, or 3; wherein each R⁴ᵇ is independently H, C₁₋₆ alkyl; and wherein each R⁴ᶜ is independently H or C₁₋₆ alkyl.

ARP200103074A 2019-11-08 2020-11-05 BICYCLIC HETEROARYL COMPOUNDS AND USES OF THESE AR120401A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201962933141P 2019-11-08 2019-11-08

Publications (1)

Publication Number Publication Date
AR120401A1 true AR120401A1 (en) 2022-02-09

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Application Number Title Priority Date Filing Date
ARP200103074A AR120401A1 (en) 2019-11-08 2020-11-05 BICYCLIC HETEROARYL COMPOUNDS AND USES OF THESE

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Country Link
AR (1) AR120401A1 (en)

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