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US 6,660,739 B1Granted
Heterocyclic amides as inhibitors of factor Xa
AssigneeEli Lilly and Company
InventorsValentine Joseph Klimkowski, Jeffrey Alan Kyle, John Joseph Masters, Michael Robert Wiley
Life of this patent
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Abstract
This application relates to a compound of formula I (or a pharmaceutically acceptable salt thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.
Claims10
A compound of formula I
- (or a pharmaceutically acceptable salt thereof) wherein:
- Q1 is phenyl or 2-naphthalenyl either of which may bear one or more halo, trifluoromethyl, methoxy or methyl substituents;
- L1 is a direct bond, methylene, ethylene or ethen-1,2-diyl;
- and
- Q2 is Q2A, Q2B, or Q2C in which
- Q2A (showing the CO to which it is attached) is
- in which each of m and n independently is 0 or 1;
- Q2B is 1-piperazinyl which bears at the 4-position the group R;
- and
- Q2C is 3,4-didehydropiperidin-4-yl which bears at the 1-position the group R;
- and
- R is t-butyl, —CHRyRz, or —CHRwRx wherein
- each of Rw and Rx independently is hydrogen or (1-3C)normal alkyl;
- or —CHRwRx is 2-indanyl or (showing the nitrogen to which it is attached) is
- in which T is a single bond or methylene and U is methylene, ethylene, oxy, —S(O)q— (wherein q is 0, 1 or 2) or imino (which may bear a methyl substituent), or T is ethan-1,1-diyl and U is a single bond or methylene;
- Ry is hydrogen or methyl;
- and
- Rz is isopropyl, t-butyl, (3-6C)cycloalkyl, phenyl (which is unsubstituted or bears one or more substituents independently selected from halo, methyl, methoxy and hydroxy), 4-quinolinyl or heteroaryl (which heteroaryl is a 5-membered aromatic ring which has one to four heteroatoms selected from sulfur, oxygen and nitrogen or is a 6-membered aromatic ring which has one to three nitrogen atoms, wherein the heteroaryl is attached at carbon and may bear one or more methyl substituents on carbon or nitrogen);
- and
- wherein halo is fluoro, chloro, bromo or iodo;
- (1-3C)normal alkyl is methyl, ethyl or propyl;
- and (3-6C)cycloalkyl is cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl.
19 more elements
Dependencies are inferred from the claim text.