Epizyme, Inc.

Megan Alene Cloonan Foley

Kevin Wayne Kuntz

Lorna Helen Mitchell

Michael John Munchhof

Richard Chesworth

Darren Martin Harvey

James Edward John Mills

Jennifer C Petter

Carl Eric Schwartz

Kenneth William Duncan

John Emmerson Campbell

Lawrence Alan Reiter

John W Lampe

Michael Thomenius

Compounds of Formula I: (I) and the pharmaceutically acceptable salts and solvates thereof, wherein R, R, G1, G2, Q, Q, Q, and (II) are defined as set forth in the specification, as are uses of compounds of Formula I to treat a disease, disorder, or condition such as cancer in a subject.

Substituted indoles and methods of use thereof

The present disclosure provides provides substituted isoxazole carboxamides having Formula (I), and the pharmaceutically acceptable salts and solvates thereof, wherein R, R, R, R, R, X, n, and m 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 disorder responsive to the blockade of SMYD proteins such as SMYD3 or SMYD2. Compounds of the present disclosure are especially useful for treating cancer. 

Isoxazole carboxamides as irreversible SMYD inhibitors

The present disclosure provides substituted piperidine compounds having Formula (I), and the pharmaceutically acceptable salts and solvates thereof, wherein R, B, X, and Z 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 disorder responsive to the blockade of SMYD proteins such as SMYD3 or SMYD2. Compounds of the present disclosure are especially useful for treating cancer. 

Substituted piperidine compounds

The present disclosure provides substituted isoxazole carboxamide compounds having Formula (I) and the pharmaceutically acceptable salts and solvates thereof, wherein R, R, A, X, and Z 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 disorder responsive to the blockade of SMYD proteins such as SMYD3 or SMYD2. Compounds of the present disclosure are especially useful for treating cancer. 

Isoxazole carboxamide compounds

The present disclosure provides carboxamides and sulfonamides having Formula (I): and the pharmaceutically acceptable salts and solvates thereof, wherein A, Y, B, X, and Z 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 disorder responsive to the blockade of SMYD proteins such as SMYD3 or SMYD2. Compounds of the present disclosure are especially useful for treating cancer. 

Substituted 1,2,3-triazoles as SMYD inhibitors for treating cancer

The present disclosure provides substituted isoxazole carboxamides having Formula (I), and the pharmaceutically acceptable salts and solvates thereof, wherein R, R, R, R, R, X, n, and m 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 disorder responsive to the blockade of SMYD proteins such as SMYD3 or SMYD2. Compounds of the present disclosure are especially useful for treating cancer. 

The present disclosure provides substituted cyclohexylamine compounds having Formula (I): and the pharmaceutically acceptable salts and solvates thereof, wherein R, R, R, R, R, R, R, and Rare defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula I to treat a disorder responsive to the blockade of SMYD proteins such as SMYD3 or SMYD2. Compounds of the present disclosure are especially useful for treating cancer. 

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Somerville, MA, United States of America

Megan Alene Cloonan Foley