AR105458A1 - SUBSTITUTED QUINAZOLINE COMPOUNDS AND METHODS FOR THE USE OF THE SAME - Google Patents
SUBSTITUTED QUINAZOLINE COMPOUNDS AND METHODS FOR THE USE OF THE SAMEInfo
- Publication number
- AR105458A1 AR105458A1 ARP160102249A ARP160102249A AR105458A1 AR 105458 A1 AR105458 A1 AR 105458A1 AR P160102249 A ARP160102249 A AR P160102249A AR P160102249 A ARP160102249 A AR P160102249A AR 105458 A1 AR105458 A1 AR 105458A1
- Authority
- AR
- Argentina
- Prior art keywords
- haloarylalkyl
- heteroaryl
- alkyl
- cycloalkyl
- aminylcarbonyl
- Prior art date
Links
Abstract
Reivindicación 1: Un compuesto que tiene la estructura de fórmula (1), o una sal, estereoisómero o profármaco del mismo farmacéuticamente aceptable, en donde: A es N o C; B es oxo, ciano, alquilo, alquenilo, alquinilo, cicloalquilo, heterociclilo, heteroarilo, cicloalquilalquilo, heterocicloalquilo, heteroarilalquilo, amino, alquilamino, arilamino, CO₂H, -CONH₂, aminilcarbonilo, aminilcarbonilalquilo, heteroarilamino, halo, haloalquilo, alcoxilo, haloalcoxilo, arilo o -X-L²-Rᵃ; X es -NRᵇ- o -O-; L¹ es alquileno, cicloalquileno, heterociclileno o está ausente; L² es alquileno o está ausente; R es H, ciano, amino, halo, haloalquilo, hidroxilo, cicloalquilo, heterociclilo, heterocicloalquilo, arilo, heteroarilo, -CO₂H, -CONH₂, aminilcarbonilo, C₁₋₆ alquilo, C₁₋₆ alquilaminilo o C₁₋₆ alcoxilo; Rᵃ es cicloalquilo, heterociclilo, heteroarilo, -(C=O)OH, -(C=O)NH₂ o-(C=O)NHOH; Rᵇ es, en cada caso, independientemente H o C₁₋₆ alquilo; R¹ es arilo o heteroarilo; R²ᵃ, R²ᵇ y R²ᶜ son cada uno independientemente H, amino, ciano, halo, hidroxilo, C₁₋₆ alquilo, C₁₋₆ alquilaminilo, -NRᵇ(C=O)Rᵇ, C₁₋₆ haloalquilo, C₁₋₆ alcoxilo, C₃₋₈ cicloalquilo, heterociclilalquilo, C₁₋₆ alquinilo, C₁₋₆ alquenilo, aminilalquilo, alquilaminilalquilo, cianoalquilo, carboxialquilo, aminilcarbonilalquilo, aminilcarbonilo, heteroarilo o arilo; ⁻ ⁻ ⁻ ⁻ ⁻ es un enlace simple o doble de forma que se satisfacen todas las valencias; y E es una porción electrofílica con capacidad de formar un enlace covalente con el residuo de cisteína en la posición 12 de una proteína mutante G12C de KRAS, HRAS o NRAS.Claim 1: A compound having the structure of formula (1), or a pharmaceutically acceptable salt, stereoisomer or prodrug thereof, wherein: A is N or C; B is oxo, cyano, alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, heteroaryl, cycloalkylalkyl, heterocycloalkyl, heteroarylalkyl, amino, alkylamino, arylamino, CO₂H, -CONH₂, aminylcarbonyl, aminylcarbonylalkyl, haloarylalkyl, haloarylalkyl, haloarylalkyl, haloarylalkyl, haloarylalkyl, haloarylalkyl, haloarylalkyl, haloarylalkyl, haloarylalkyl, haloarylalkyl, haloalkylamino or -X-L²-Rᵃ; X is -NRᵇ- or -O-; L¹ is alkylene, cycloalkylene, heterocyclylene or is absent; L² is alkylene or is absent; R is H, cyano, amino, halo, haloalkyl, hydroxyl, cycloalkyl, heterocyclyl, heterocycloalkyl, aryl, heteroaryl, -CO₂H, -CONH₂, aminylcarbonyl, C₁₋₆ alkyl, C₁₋₆ alkylamino or C₁₋₆ alkoxy; Rᵃ is cycloalkyl, heterocyclyl, heteroaryl, - (C = O) OH, - (C = O) NH₂ or- (C = O) NHOH; Rᵇ is, in each case, independently H or C₁₋₆ alkyl; R¹ is aryl or heteroaryl; R²ᵃ, R²ᵇ and R²ᶜ are each independently H, amino, cyano, halo, hydroxyl, C₁₋₆ alkyl, C₁₋₆ alkylaminyl, -NRᵇ (C = O) Rᵇ, C₁₋₆ haloalkyl, C₁₋₆ alkoxy, C₃₋ ₈ cycloalkyl, heterocyclylalkyl, C₁₋₆ alkynyl, C₁₋₆ alkenyl, aminylalkyl, alkylaminyl alkyl, cyanoalkyl, carboxyalkyl, aminylcarbonylalkyl, aminylcarbonyl, heteroaryl or aryl; ⁻ ⁻ ⁻ ⁻ ⁻ Is a single or double bond so that all valences are satisfied; and E is an electrophilic portion capable of forming a covalent bond with the cysteine residue at position 12 of a G12C mutant protein of KRAS, HRAS or NRAS.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201562195636P | 2015-07-22 | 2015-07-22 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR105458A1 true AR105458A1 (en) | 2017-10-04 |
Family
ID=60244722
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP160102249A AR105458A1 (en) | 2015-07-22 | 2016-07-22 | SUBSTITUTED QUINAZOLINE COMPOUNDS AND METHODS FOR THE USE OF THE SAME |
Country Status (2)
Country | Link |
---|---|
AR (1) | AR105458A1 (en) |
JO (1) | JOP20160150B1 (en) |
-
2016
- 2016-07-21 JO JOP/2016/0150A patent/JOP20160150B1/en active
- 2016-07-22 AR ARP160102249A patent/AR105458A1/en unknown
Also Published As
Publication number | Publication date |
---|---|
JOP20160150B1 (en) | 2021-08-17 |
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