Compositions and methods for treating heart failure
AssigneeCytokinetics, Inc.
InventorsFady Malik, Adam Lewis Tomasi, Bainian Feng, Erica Anne Kraynack, Kathleen A. Elias, Pu-Ping Lu, Whitney Walter Smith, Xiangping Qian, David J. Morgans, JR.
Life of this patent
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Abstract
Certain substituted benzamide derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure.
Claims48
A compound represented by Formula I
- 6
- wherein:
- R1 is alkyl, substituted alkyl, aryl, substituted aryl, heteroaryl or substituted heteroaryl;
- R2 is acetyl, acetylamino, acetylene, alkoxycarbonyl, carboxamido, cyano, halo, heteroaryl, hydrogen, nitrile or trifluoromethyl;
- and
- R3 is aryl, substituted aryl, heteroaryl or substituted heteroaryl;
- or a single stereoisomer, or mixture of stereoisomers, or a pharmaceutically acceptable salt thereof.
A compound represented by Formula I
- 7
- wherein:
- R1 is alkyl, substituted alkyl, aryl, substituted aryl, heteroaryl or substituted heteroaryl;
- R2 is nitro;
- and
- R3 is aryl, substituted aryl, heteroaryl or substituted heteroaryl;
- provided that:
- when R1 is pyridin-3-yl, R3 is not 3-bromophenyl, 3-fluorophenyl, 4-fluorophenyl, furan-2-yl, 4-methoxyphenyl or 1-methyl-1H-pyrazol-3-yl;
- when R1 is 4-hydroxyophenyl, R3 is not furan-2-yl;
- when R1 is 4-fluorophenyl, R3 is not furan-2-yl or pyridin-4-yl;
- and
- when R3 is pyridin-4-yl, R1 is not phenyl, 3-chlorophenyl, 4-hydroxyphenyl or 3-methylphenyl;
- or a single stereoisomer, or mixture of stereoisomers, or a pharmaceutically acceptable salt thereof.
A method of treatment for heart failure, comprising administering to a mammal in need thereof a therapeutically effective amount of a compound represented by Formula I
- 8
- wherein:
- R1 is alkyl, substituted alkyl, aryl, substituted aryl, heteroaryl or substituted heteroaryl;
- R2 is acetyl, acetylamino, acetylene, alkoxycarbonyl, carboxamido, cyano, halo, heteroaryl, hydrogen, nitrile, nitro or trifluoromethyl;
- and
- R3 is aryl, substituted aryl, heteroaryl or substituted heteroaryl;
- or a single stereoisomer, or mixture of stereoisomers, or a pharmaceutically acceptable salt thereof.
A pharmaceutical formulation comprising a pharmaceutically accepted excipient and a therapeutically effective amount of a compound represented by Formula I
- 9
- wherein:
- R1 is alkyl, substituted alkyl, aryl, substituted aryl, heteroaryl or substituted heteroaryl;
- R2 is acetyl, acetylamino, acetylene, alkoxycarbonyl, carboxamido, cyano, halo, heteroaryl, hydrogen, nitrile, nitro or trifluoromethyl;
- and
- R3 is aryl, substituted aryl, heteroaryl or substituted heteroaryl;
- or a single stereoisomer, or mixture of stereoisomers, or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.