Substituted indoles and methods of use thereof
AssigneeEpizyme, Inc.
InventorsJohn Lampe, John Campbell, Kenneth Duncan, Megan Alene Cloonan Foley, Darren Martin Harvey, Michael John Munchhof, Michael Thomenius, Lawrence Alan Reiter
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Abstract
The present disclosure provides substituted indole compounds of Formula I: (I) and the pharmaceutically acceptable salts and solvates thereof, wherein R1a, R1e, G1, G2, Q1, Q2, Q3, and (II) are defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula I to treat a disease, disorder, or condition such as cancer in a subject.
Claims30
A compound of Formula I:
- wherein:
- R1a is selected from the group consisting of halogen, alkyl, alkoxy, cycloalkyl, (hydroxy)alkyl, and (cycloalkyl)alkyl;
- Q1 is selected from the group consisting of —C(R1b)═ and —N═;
- Q2 is selected from the group consisting of —C(R1c)═ and —N═;
- Q3 is selected from the group consisting of —C(R1d)═ and —N═;
- provided that at least one of Q1, Q2, or Q3 is —C(R1b)=, —C(R1c)=, or —C(R1d)=respectively;
- R1b, R1c, and R1d are each independently selected from the group consisting of hydrogen, halogen, alkyl, alkenyl, (hydroxy)alkyl, and alkoxy;
- R1e is selected from the group consisting of hydrogen, halogen, alkyl, cycloalkyl, (hydroxy)alkyl, and (cycloalkyl)alkyl;
- is a single or double bond;
- G1 is selected from the group consisting of:
- optionally substituted aryl;
- optionally substituted heteroaryl;
- optionally substituted heterocyclo;
- optionally substituted cycloalkyl;
- (aryl)alkyl;
- (heteroaryl)alkyl;
- (heterocyclo)alkyl;
- (amino)(aryl)alkyl;
- (heteroaryl)(aryl)alkyl;
- (heteroaryl)(heterocyclo)alkyl;
- (heteroaryl)(carboxamido)alkyl;
- (heteroaryl)(cycloalkyl)alkyl;
- (aryl)(alkoxycarbonyl)alkyl;
- (cycloalkyl)alkyl;
- (heteroaryl)(amino)alkyl;
- (cycloalkyl)(alkoxycarbonyl)alkyl;
- (heteroaryl)(alkoxycarbonyl)alkyl;
- (heterocyclo)(cycloalkyl)alkyl;
- (aryl)(cycloalkyl)alkyl;
- (aryl)(hydroxy)alkyl;
- (cycloalkyl)(hydroxy)alkyl;
- (hydroxy)alkyl;
- optionally substituted alkyl;
- (aryl)(haloalkyl)alkyl;
- (cycloalkyl)(haloalkyl)alkyl;
- (hydroxy)(haloalkyl)alkyl;
- and (alkoxycarbonyl)(haloalkyl)alkyl;
- and
- G2 is selected from the group consisting of hydrogen and alkyl;
- or
- G1 and G2 taken together with the nitrogen atom to which they are attached form an optionally substituted heterocyclo,
- provided that the compound of Formula I is not N-(1-(1-(L-alanyl)piperidin-4-yl)ethyl)-7-methyl-1H-indole-2-carboxamide;
- N-((1r,4r)-4-(3-aminopropanamido) cyclohexyl)-7-methyl-1H-indole-2-carboxamide;
- or N-((1r,4r)-4-aminocyclohexyl)-7-methyl-1H-indole-2-carboxamide, or a pharmaceutically acceptable salt or solvate thereof.
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Dependencies are inferred from the claim text.