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US 2003/0144287 A1Published application
Novel N-[4- (1H-imidazol-1-yl) -2-fluorophenyl ] -3- (trifluoromethyl) -1H-pyrazole-5-carboxamides as factor Xa inhibitors
AssigneeBristol-Myers Squibb Company
InventorMimi L. Quan
Life of this patent
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Abstract
The present application describes N-[4-(1H-imidazol-1-yl)-2-fluorophenyl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamides and derivatives thereof of, which are useful as inhibitors of factor Xa.
Claims15
A compound of formula I:
- 17
- or a pharmaceutically acceptable salt thereof, wherein:
- R is H or C1-6 alkyl;
- R1 is selected from the group:
- H;
- C1-6 alkenylene-C(O)—C1-6 alkyl;
- C(O)—C1-6 alkyl;
- C(O)—C1-6 alkyl-NRaRa, wherein Ra is independently H or C1-6 alkyl;
- C(O)CH2CH2CH(NRaRa)C(O)ORa, wherein Ra is independently H or C1-6 alkyl;
- C(O)-phenyl substituted with 0-2 R2;
- C(O)OCH2OPO3H;
- C(O)OCH2O—C1-6 alkyl;
- CH2OC(O)-phenyl substituted with 0-2 R2;
- CH2OC(O)CH2-5-6 membered heterocycle consisting of carbon atoms and 1-2 heteroatoms selected from O and N, and substituted with 0-2 R2;
- and,
- 18
- wherein the asterisk defines the point of attachment;
- R2 is selected from Cl, F, Br, I, OH, C1-6 alkyl, C1-6 alkyl-OH, C1-6 alkoxy, and C1-4 alkylene-OC(O)—C1-6 alkyl;
- and,
- R3 is selected from C1-6 alkyl and phenyl substituted with 0-2 R2.
17 more elements
A compound of formula II:
- 20
- or a pharmaceutically acceptable salt thereof, wherein:
- R1 is selected from the group:
- H;
- C(O)—C1-6 alkyl;
- C(O)—C1-6 alkyl-OH;
- C(O)O—C1-6 alkyl;
- C(O)OCH2OPO3H;
- and,
- C(O)-phenyl substituted with 0-2 R4;
- and,
- R4 is selected from:
- CH2NRaRa, wherein Ra is independently H or C1-6 alkyl;
- CH2NRaRa(CH2)2NRaRa, wherein Ra is independently H or C1-6 alkyl;
- CH2-5-6 membered heterocycle consisting of carbon atoms and 1-2 heteroatoms selected from O and N, and substituted with 0-2 R2.
12 more elements
A compound of formula III:
- 22
- or a pharmaceutically acceptable salt thereof.
A compound of formula IV:
- 23
- or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.