Certain chemical entities, compositions, and methods
AssigneeRetune Pharma Inc.
InventorsAndrew I. MCDONALD, Shawn QIAN
Life of this patent
Estimating the term…
Abstract
Provided herein are inhibitors of IGF-1R, pharmaceutical compositions comprising said inhibitory compounds, and methods for using said IGF-1R inhibitory compounds for the treatment of disease.
Claims53
A compound, or pharmaceutically acceptable salt or solvate thereof, having the structure of Formula (I):
- wherein,
- X is optionally substituted alkyl, optionally substituted carbocyclyl, optionally substituted carbocyclylalkyl, optionally substituted aryl, optionally substituted aralkyl, optionally substituted heteroaryl, optionally substituted heteroaralkyl, optionally substituted heterocyclyl, or optionally substituted heterocyclylalkyl;
- L is a bond, or optionally substituted carbocyclyl, optionally substituted carbocyclylalkyl, optionally substituted heterocyclyl, or optionally substituted heterocyclylalkyl;
- R2 is optionally substituted carbocyclyl, optionally substituted aryl, optionally substituted heteroaryl, or optionally substituted heterocyclyl;
- wherein the optional substitution of the optionally substituted carbocyclyl, optionally substituted aryl, optionally substituted heteroaryl, or optionally substituted heterocyclyl is selected from the group consisting of cyano, halo, hydroxy, azido, amino, nitro, —CO2H, —S(O)—R10, —S—R10, —S(O)2—R10, optionally substituted C1-C6 alkoxy, optionally substituted aryloxy, optionally substituted heteroaryloxy, optionally substituted (heterocyclyl)-O—, optionally substituted C1-C6 alkyl, optionally substituted C2-C6 alkynyl, optionally substituted carbocyclyl, optionally substituted C2-C6 alkenyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted heterocyclyl, —N(R11)2, —CO—R10, —CO2—R10, —CON(R11)2, —NR11CO—R10, —NR11CO2—R10, —SO2N(R11)2, —C(═NR12)—N(R11)2, —NR11CO—N(R10)2, or —NR11SO2—N(R10)2;
- X3 is N or C—R3;
- X4 is N or C—R4;
- X5 is N or C—R5;
- X6 is N or C—R6;
- X8 is N or C—R8;
- R3, R4, R5, R6, and R8 are independently selected from the group consisting of hydrogen, cyano, halo, hydroxy, azido, amino, nitro, —CO2H, —S(O)—R10, —S—R10, —S(O)2—R10, optionally substituted C1-C6 alkoxy, optionally substituted C1-C6 alkyl, optionally substituted C2-C6 alkynyl, optionally substituted carbocyclyl, optionally substituted C2-C6 alkenyl, optionally substituted heterocyclyl, —N(R11)2, —CO—R10, —CO2—R10, —CON(R11)2, —NR11CO—R10, —NR11CO2—R10, —SO2N(R11)2, —C(═NR12)—N(R11)2, —NR11CO—N(R10)2, and —NR11SO2—N(R10)2;
- each R10 is independently selected from the group consisting of optionally substituted C1-C6 alkyl, optionally substituted C3-C8 carbocyclyl, optionally substituted heterocyclyl, optionally substituted aryl, and optionally substituted heteroaryl;
- each R11 is independently selected from the group consisting of hydrogen, optionally substituted C1-C6 alkyl, optionally substituted C3-C8 carbocyclyl, optionally substituted heterocyclyl, optionally substituted aryl, and optionally substituted heteroaryl;
- R12 is H or optionally substituted C1-C6 alkyl;
- R9 is selected from hydrogen, optionally substituted C1-C6 alkyl, optionally substituted C3-C8 carbocyclyl, or optionally substituted C4-C10 carbocyclylalkyl;
- wherein either R9 and L, or R9 and X, may be joined together with any intervening atoms to form an optionally substituted heterocyclyl ring.
The compound of any one of the preceding claims, or pharmaceutically acceptable salt or solvate thereof, wherein X8 is N.
The compound of any one of the preceding claims, or pharmaceutically acceptable salt or solvate thereof, wherein R9 is H.
The compound of any one of the preceding claims, or pharmaceutically acceptable salt or solvate thereof, wherein R2 is optionally substituted aryl.
The compound of any one of the preceding claims, or pharmaceutically acceptable salt or solvate thereof, wherein X6 is N.
The compound of any one of the preceding claims, or pharmaceutically acceptable salt or solvate thereof, wherein X5 is N.
A compound, or pharmaceutically acceptable salt or solvate thereof, having the structure of a compound provided in Table 1A or Table 1B.
Dependencies are inferred from the claim text.