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US 7,115,609 B2Granted
Alanyl-piperidine heterocyclic derivatives useful against cardiovascular diseases
AssigneeEli Lilly and Company
InventorsStuart Donald Jones, Daniel Jon Sall, Michael Robert Wiley
Life of this patent
Estimating the term…
Abstract
Compounds of formula (I) in which R1, R2, n and X1 have the meanings given in the specification are Factor Xa inhibitors useful in the treatment of thrombotic disorders.
Claims14
A compound of formula (I)
- in which
- X1 represents N;
- n is 1 or 2;
- R1 represents trifluoromethyl, COOH, CONH2, SO2NH2, phenyl, pyridyl, C-linked imidazolyl (which may bear an N-(1–4C)alkyl substituent) or a (3–6C)cycloalkyl, oxa (4–6C)cycloalkyl, thia(4–6C)cycloalkyl or C-linked aza (4–6C)cycloalkyl group, which C-linked aza(4–6C)cycloalkyl group may bear an N-(1–4C)alkyl substituent;
- and
- R2 is selected from
- in which
- X2 represents a hydrogen atom, a halogen atom or an amino group;
- X3 represents a hydrogen atom, a methyl group, a fluorine atom, a chlorine atom or a bromine atom;
- X4 represents a hydrogen atom, a methyl, group or a halogen atom;
- X5 represents a chlorine atom, a methoxy group or a methyl group;
- and
- X6 represents a hydrogen atom, a halogen atom or a methyl group;
- or a pharmaceutically acceptable metabolically labile ester thereof, or a pharmaceutically acceptable salt thereof.
11 more elements
A compound of formula (IV)
- or a salt thereof, in which
- X1 represents N;
- n is 1 or 2;
- and
- R1 represents trifluoromethyl, COOH, CONH2, SO2NH2, pyridyl, C-linked imidazolyl (which may bear an N-(1–4C)alkyl substituent) or a (3–6C)cycloalkyl, oxa(4–6C)cycloalkyl, thia(4–6C)cycloalkyl or C-linked aza(4–6C)cycloalkyl group, which C-linked aza(4–6C)cycloalkyl group may bear an N-(1–4C)alkyl substituent.
2 more elements
Dependencies are inferred from the claim text.