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US 2017/0362235 A1Published application
Adenylyl cyclase inhibitors, pharmaceutical compositions and method of use thereof
OwnerDaniel E. Levy, Patricio Abarzúainventors
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Abstract
The present invention relates to novel adenine based inhibitors of adenylyl cyclase of the formula: wherein X, L, R1, R2, R5 are those defined herein. Compounds of the present invention are useful to treat cardiovascular diseases. The present invention also relates to a method of preventing heart failure by administering an effective amount of compound according to the invention following vascular injury and reperfusion therapy.
Claims12
A compound of Formula I wherein,
- wherein,
- R1 is COOH, COOCH3, CONH2 or CONHOH;
- Each R2 is independently H, C1-C6 alkyl or —(CH2)m—R3, wherein at least 3 R2 groups must be H;
- or, independently of other R2 groups, two R2 groups residing on adjacent carbon atoms join to form a carbon-carbon double bond;
- Each R3 is independently OR4, N(R4)2, SR4, COOH, COOCH3 or CONH2;
- Each R4 is independently H or C1-C6 alkyl;
- Each R5 is independently F, Cl, Br, I, OH, OR6, N(R6)2, SR6, C1-C6 alkyl, CF3, NO2, COOH, COOCH3, CONH2 SO3H, PO3H or CN;
- Each R6 is independently H or C1-C6 alkyl;
- R7 is H or C1-C6 alkyl;
- L is a direct link or —(CH2)n—Y—(CH2)o—;
- Each X is independently N or CH;
- Y is a direct link, O, S or NR7;
- m is an integer from 0 to 5;
- n is an integer from 0 to 5;
- o is an integer from 0 to 5, wherein if L is not a direct link, o is not 0;
- Each stereogenic center is independently either R or S;
- and,
- If all R2 groups are H, at least one of R5 is not H or at least one of X is not N.
15 more elements
Dependencies are inferred from the claim text.