Antithrombotic azacycloalkylalkanoyl peptides and pseudopeptides
AssigneeAventis Pharmaceuticals Inc.
InventorsScott I. Klein, Bruce F. Molino
Life of this patent
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Abstract
The present invention relates to azacycloalkylalkanoyl peptides and pseudopeptides which inhibit platelet aggregation and thrombus formation thereby being useful in the prevention and treatment of thrombosis associated with disease states such as myocardial infarction, stroke, peripheral arterial disease, and disseminated intravascular coagulation, to methods for the prevention or treatment of thrombosis in a mammal in need of such therapy comprising the administration of a therapeutically effective amount of such compounds, and to pharmaceutical compositions comprising such compounds.
Claims19
A compound of the formula
- 40
- wherein
- A is —H, amidino, or substituted amidino;
- B is alkyl, cycloalkyl, cycloalkylalkyl, alkylcycloalkyl, alkylcycloalkylalkyl, aryl, aralkyl, alkylaryl, or alkylaralkyl;
- Z is
- 41
- where
- E is —H or, in combination with F, forms a 4-, 5-, 6-, or 7-membered azacycloalkane ring,
- F is the a-carbon side chain of a naturally occuring a-amino acid, —H, alkyl, cycloalkyl, cycloalkylalkyl, alkylcycloalkyl, alkylcycloalkylalkyl, aryl, substituted aryl, aralkyl, substitued aralkyl, heterocyclyl, substituted heterocyclyl, heterocyclylalkyl, substituted heterocyclylalkyl, or, in combination with E, forms a 4-, 5-, 6-, or 7-membered azacycloalkane ring,
- G is alkyl, cycloalkyl, cycloalkylalkyl, alkylcycloalkyl, alkylcycloalkylalkyl, aryl, substituted aryl, aralkyl, substituted aralkyl, heterocyclyl, substituted heterocyclyl, heterocyclylalkyl, substituted heterocyclylalkyl, OR1, orNR1R2, where R1 and R2 are independently —H, alkyl, cycloalkyl, cycloalkylalkyl, alkylcycloalkyl, alkylcycloalkylalkyl, aryl, aralkyl, alkylaryl, or alkylaralkyl, and
- r is 0 or 1;
- R is H—, alkyl, aryl, or aralkyl;
- m is
- 1 to 5;
- n is 0 to 6;
- and
- p is 1 to 4;
- or a pharmaceutically acceptable salt thereof.
A compound of the formula
- 42
- wherein:
- A is —H or amidino,
- B is alkyl, cycloalkyl, cycloalkylalkyl, alkylcycloalkyl, alkylcycloalkylalkyl, aryl, aralkyl, alkylaryl, or alkylaralkyl,
- J is —H, alkyl, cycloalkyl, cycloalkylalkyl, alkylcycloalkyl, alkylcycloalkylalkyl, aryl, substituted aryl, aralkyl, substitued aralkyl,
- L is OR1, or NR1R2, where R1 and R2 are independently —H, alkyl, cycloalkyl, cycloalkylalkyl, alkylcycloalkyl, alkylcycloalkylalkyl, aryl, aralkyl, alkylaryl, or alkylaralkyl,
- m is 1 to 5,
- n is 2 to 6, and
- p is 1 or 2;
- or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.