1. An ink tank comprising:
an ink-containing part having an inside configured to contain ink; and
an optical detector configured to optically detect a presence or an absence of ink in the ink-containing part,
wherein the optical detector comprises:
a luminescent material;
a light-reflecting part configured to reflect irradiation light irradiated from an outside of the ink-containing part onto the luminescent material, so that the luminescent material is excited by the light that has been reflected by the light-reflecting part and emits light of a wavelength that is different from a wavelength of the irradiation light; and
a light-shielding part configured to shield the luminescent material from refracted light when ink is present in the ink-containing part, wherein the luminescent material receives the reflected light from the light-reflecting part and emits the light of the different wavelength when ink is absent from the ink-containing part.
2. An ink tank comprising:
an ink-containing part having an inside configured to contain ink; and
an optical detector configured to optically detect a presence or an absence of ink in the ink-containing part,
wherein the optical detector comprises:
a luminescent material; and
a light-reflecting part formed at an interface between the ink-containing part and a prism, and configured to reflect irradiation light irradiated from the outside of the ink-containing part onto the luminescent material, so that the luminescent material is excited by the light that has been reflected by the light reflecting part and emits light of a wavelength that is different from a wavelength of the irradiation light when ink is not present in the ink-containing part, and further configured to refract the irradiation light so as not to reflect the irradiation light to the luminescent material when ink is present in the ink-containing part.
3. The ink tank according to claim 2, wherein the luminescent material is provided in the interior of the prism.
4. The ink tank according to claim 2, wherein the luminescent material is provided outside the prism.
5. A method of detecting the presence or absence of ink in an ink tank, comprising:
irradiating light with a first wavelength from a light source;
directing the irradiated light into a prism in the ink tank, the prism having a refractive index chosen so that if the prism has an interface with ink, the irradiated light is refracted through that interface, and if the prism has an interface with air, the irradiated light is totally internally reflected from that interface, the prism containing a luminescent material that emits light with a second wavelength when the irradiated light with the first wavelength is absorbed by the luminescent material;
detecting light emerging from the prism; and
determining, from the emerging light, whether the light has been refracted and ink is present in the ink tank, or the light has been totally internally reflected onto the luminescent material and ink is absent from the ink tank.
6. A method according to claim 5, further comprising:
displaying a notification indicating whether ink is present or absent in the ink tank based on the result of the determining step.
7. An ink tank comprising:
a case;
an ink-containing part that is capable of containing an ink; and
a light-reflecting part used for optically detecting a presence or an absence of ink in the ink-containing part,
wherein the light-reflecting part reflects irradiation light irradiated from the outside of the ink-containing part and irradiates reflected reflection light to luminescent material fixed on the case, and
wherein the luminescent material is excited by the reflection light that has been irradiated and emits light of a wavelength that is different from a wavelength of the irradiation light.
8. An ink tank according to claim 7, wherein the light-reflecting part totally reflects the irradiation light to the luminescent material when the ink is absent from the ink-containing part and refracts the irradiation light when the ink is present in the ink-containing part.
The claims below are in addition to those above.
All refrences to claim(s) which appear below refer to the numbering after this setence.
What is claimed is:
1. A compound having Formula I:
93
and pharmaceutically acceptable salts thereof, where:
X1 and X2 are hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl, aralkyl, cycloalkylalkyl, (CH2)m-halogen, (CH2)m-heteroaryl, (CH2)mSOR3, (CH2)mOCOR3, (CH2)mOSO2R3, (CH2)mOSO2NR4R5, (CH2)m-NR6COR3, (CH2)mNR6SO2R3, (CH2)mNR3SO2NR4R5, (CH2)mNR4R5, (CH2)mOR3, CN, NO2, CF(3-n)Hn, (CH2)mO(CH2)mR3 , (CH2)mO(CH2)mOR3 , (CH2)mO(CH2)mNR4R5, (CH2)mR3, (CH2)mCO2R3, (CH2)mCOR3, (CH2)mCONR4R5, (CH2)mNR6COR3, (CH2)mNR6CONR4R5, (CH2)mSO2R3, (CH2)mSO2NR4R5,
94
or are joined together to form a substituted or unsubstituted three to eight member ring wherein 0 to 3 atoms of the ring are heteroatoms;
A is aryl, arylcycloalkyl, heteroaryl, heteroarylcycloalkyl, cycloalkyl, or cycloalkenyl;
M is arylene, heteroarylene, cycloalkylene, heterocycloalkylene, cycloalkenylene or heterocycloalkenylene;
Q is CONR4R5, aryl, heteroaryl, cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl;
R1 is hydrogen, alkyl, aryl, heteroaryl or alkenyl;
R2 is hydrogen, alkyl, aryl, heteroaryl, alkenyl, cycloalkyl, cycloalkylalkyl, aralkyl, heteroaralkyl, heterocycloalkylalkyl, carboxy, (CH2)mNR4R5, (CH2)mOR3, (CH2)mSR3, (CH2)mCONR4R5, or (CH2)mNR6COR3;
R3 is hydrogen, alkyl, aryl, heteroaryl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aralkyl, or heteroarylalkyl;
R6 is hydrogen, alkyl, aryl, heteroaryl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aralkyl, or heteroarylalkyl;
R4 and R5 are each independently hydrogen, alkyl, aryl, heteroaryl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aralkyl, heteroarylalkyl,
95
or joined together to form a 3 to 8 member ring;
m is 0 to 8;
n is 0 to 2; and
p is 1 to 3;
with the proviso that when R1 and R2 are H, neither X1 nor X2 is H.
2. The compound of claim 1, wherein A is aryl or heteroaryl.
3. The compound of claim 2, wherein A is
96
wherein Y is CH or N; and R8 is hydrogen, halo, or C1-C6 alkyl.
4. The compound of claim 3, wherein A is
97
wherein Y is CH or N; and R8 is hydrogen, Cl, Br, or F.
5. The compound of claim 4, wherein A is 4-chlorophenyl or 5-chloro-2-pyridyl.
6. The compound of claim 1, wherein M is arylene or heteroarylene.
7. The compound of claim 6, wherein M is
98
wherein R9 is hydrogen, halo, or C1-C6 alkyl.
8. The compound of claim 7, wherein M is
99
wherein R9 is hydrogen, methyl, trifluoromethyl, Cl, Br, or F.
9. The compound of claim 8, wherein M is phenylene-1,4-diyl, 2-fluoro-phenylene-1,4-diyl, 2-methyl-phenylene-1,4-diyl, 2-trifluoromethyl-phenylene-1,4-diyl, or pyridine-2,5-diyl.
10. The compound of claim 1, wherein Q is aryl, heteroaryl or heterocycloalkyl.
11. The compound of claim 10, wherein Q is
100
wherein G is O, S, NH, N(C1-C6alkyl),
101
R14 is hydrogen, halo, C1-C6 alkyl, SO2NR12R13, SO2alkyl or oxo; R16 and R17 are independently hydrogen, C1-C6 alkyl, or are joined together to form a saturated or unsaturated 3 to 8 membered ring; and R10 is hydrogen, halo, C1-C6 alkyl, SO2NR12R13, or SO2alkyl, C1-C6 alkyl, wherein R12 and R13 are independently hydrogen, C1-C6 alkyl, or are joined together to form a saturated 5 to 7 membered ring.
12. The compound of claim 11, wherein Q is
102
wherein G is NH, N(C1-C6alkyl) or
103
R14 is hydrogen, SO2NR12R13, SO2alkyl or oxo; and R10 is hydrogen, Cl, Br, F, SO2NR12R13, or SO2alkyl, wherein R12 and R13 are independently hydrogen, or C1-C6 alkyl.
13. The compound of claim 11, wherein Q is 2-methanesulfonylphenyl, 2-sulfamoylphenyl, 2-oxo-2H-pyridin-1-yl, or 2-oxo-piperidin-1-yl.
14. The compound of claim 1, wherein X1 and X2 are hydrogen, alkyl, (CH2)mOR3, or alkenyl.
15. The compound of claim 1, wherein X1 and X2 are alkyl, (CH2)mOR3, alkenyl or CH2NR7R7 where R7 and R7 are independently hydrogen, C1-C6 alkyl
104
16. The compound of claim 1, wherein X1 and X2 are hydrogen, methyl, CH2OH, CH2NH2, CH2N(CH3)2, or CH2N(CH2CH3)2.
17. The compound of claim 1, wherein X1 and X2 together form a cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cyclopentenyl ring.
18. The compound of claim 1, wherein X1 and X2together are
105
wherein R15 and R15 are independently hydrogen, (CH2)1-6OH, (CH2)1-6OC1-C6 alkyl, (CH2)1-6NH2, COOH, or OH; and E is O, S, or NR16 wherein R16 is hydrogen, C1-C6 alkyl,
106
19. The compound of claim 1, wherein R2 is alkyl, aryl, heteroaryl, cycloalkyl, cycloalkylalkyl, aralkyl, heteroaralkyl, heterocycloalkylalkyl, carboxy, (CH2)mNR4R5, (CH2)mOR3, (CH2)mSR3, (CH2)mCONR4R5, or (CH2)mNR6COR3; wherein R3, R4, R5 and R6 as as described in claim 1.
20. The compound of claim 19, wherein R2 is C1-C6 alkyl, phenyl, pyridyl, cyclopropyl, cyclopropylmethyl, cyclobutylmethyl, cyclopentylmethyl, cyclohexylmethyl, 2-cyclopropylethyl, 2-cyclopentylethyl, benzyl, 2-pyridinylmethyl, 3-pyridinylmethyl, 4-pyridinylmethyl, 3-(2-pyridinyl)-propyl, thienylmethyl, 2-morpholin-4-yl-ethyl, 2-thiomorpholin-4-yl-ethyl, (CH2)1-3NH2, (CH2)1-3N(C1-C6alkyl)2, (CH2)1-3NHC1-C6alkyl, (CH2)1-3OC1-C6alkyl, (CH2)1-3SC1-C6alkyl, (CH2)1-3CONH2, (CH2)1-3CON(C1-C6alkyl)2, (CH2)1-3CONHC1-C6alkyl, or (CH2)1-3NHCOC1-C6alkyl.
21. The compound of claim 1, wherein where A is
107
wherein Y is CH or N; and R8 is hydrogen, Cl, Br, or F;
M is
108
wherein R9 is hydrogen, Cl, Br, or F;
Q is
109
wherein G is NH, N(C1-C6alkyl) or
110
R14 is hydrogen, SO2NR12R13, SO2alkyl or oxo; and R10 is hydrogen, Cl, Br, F, SO2NR12R13, or SO2alkyl, where R12 and R13 are independently hydrogen, or C1-C6 alkyl;
X1 and X2 are hydrogen, methyl, CH2OH, CH2NR7R7 where R7 and R7 are independently hydrogen or C1-C6 alkyl, or X1 and X2 together form a cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cyclopentenyl ring or together are
111
wherein R15 and R15 are independently hydrogen, (CH2)1-6OH, (CH2)1-6OC1-C6 alkyl, (CH2)1-6NH2, COOH, or OH; and E is O, S, or NR16 where R16 is R16 is hydrogen, C1-C6 alkyl,
112
R1 and R3 are each independently hydrogen, or C1-C6alkyl; and
R2 is hydrogen, C1-C6 alkyl, phenyl, pyridyl, cyclopropyl, cyclopropylmethyl, cyclobutylmethyl, cyclopentylmethyl, cyclohexylmethyl, 2-cyclopropylethyl, 2-cyclopentylethyl, benzyl, 2-pyridinylmethyl, 3-pyridinylmethyl, 4-pyridinylmethyl, 3-(2-pyridinyl)-propyl, thienylmethyl, 2-morpholin-4-yl-ethyl, 2-thiomorpholin-4-yl-ethyl, (CH2)1-3NH2, (CH2)1-3N(C1-C6alkyl)2, (CH2)1-3NHC1-C6alkyl, (CH2)1-3OC1-C6alkyl, (CH2)1-3SC1-C6alkyl, (CH2)1-3CONH2, (CH2)1-3CON(C1-C6alkyl)2, (CH2)1-3CONHC1-C6alkyl, or (CH2)1-3NHCOC1-C6alkyl.
22. The compound of claim 1, wherein the compounds is
1-3-(4-Chloro-phenyl)-ureido)-cyclopropanecarboxylic acid (3-fluoro-2-methanesulfonyl-biphenyl-4-yl)-amide;
1-3-(5-Chloro-pyridin-2-yl)-ureido-cyclopropanecarboxylic acid (3-fluoro-2-sulfamoyl-biphenyl-4-yl)-amide;
2-3-(5-Chloro-pyridin-2-yl)-ureido-N-(3-fluoro-2-methanesulfonyl-biphenyl-4-yl)-2-methyl-propionamide;
2-3-(4-Chloro-phenyl)-ureido-N-(3-fluoro-2-sulfamoyl-biphenyl-4-yl)-2-methyl-propionamide;
4-3-(4-Chloro-phenyl)-ureido-tetrahydro-thiopyran-4-carboxylic acid (3-fluoro-2-sulfamoyl-biphenyl-4-yl)-amide;
1-3-(4-Chloro-phenyl)-ureido-cyclopropanecarboxylic acid (3-fluoro-2-sulfamoyl-biphenyl-4-yl)-amide;
1-3-(5-Chloro-pyridin-2-yl)-ureido-cyclopropanecarboxylic acid (3-fluoro-2-methanesulfonyl-biphenyl-4-yl)-amide;
4-3-(4-Chloro-phenyl)-ureido-tetrahydro-pyran-4-carboxylic acid (3-fluoro-2-sulfamoyl-biphenyl-4-yl)-amide;
1-3-(4-Chloro-phenyl)-ureido-cyclopentanecarboxylic acid (2-methanesulfonyl-biphenyl-4-yl)-amide;
1-3-(4-Chloro-phenyl)-ureido-cyclohexanecarboxylic acid (2-methanesulfonyl-biphenyl-4-yl)-amide;
2-3-(4-Chloro-phenyl)-1-methyl-ureido-N-(3-fluoro-2-methanesulfonyl-biphenyl-4-yl)-acetamide;
2-3-(4-Chloro-phenyl)-1,3-dimethyl-ureido-N-(3-fluoro-2-methanesulfonyl-biphenyl-4-yl)-acetamide;
2-3-(4-Chloro-phenyl)-ureido-3-hydroxy-2-hydroxymethyl-N-(2-sulfamoyl-biphenyl-4-yl)-propionamide;
1-3-(4-Chloro-phenyl)-ureido-cyclopropanecarboxylic acid (2-methanesulfonyl-biphenyl-4-yl)-amide;
2-3-(4-Chloro-phenyl)-ureido-N-(3-fluoro-2-methanesulfonyl-biphenyl-4-yl)-2-methyl-propionamide;
2-3-(4-Chloro-phenyl)-ureido-N-(3-fluoro-2-methanesulfonyl-biphenyl-4-yl)-acetamide;
1-3-(4-Chloro-phenyl)-ureido-cyclopent-3-enecarboxylic acid (3-fluoro-2-sulfamoyl-biphenyl-4-yl)-amide; and
2-3-(4-Chloro-phenyl)-3-methyl-ureido-N-(3-fluoro-2-methanesulfonyl-biphenyl-4-yl)-acetamide;
(1S,2S)-1-3-(4-Chloro-phenyl)-ureido-2-hydroxymethyl-cyclopropanecarboxylic acid (3-fluoro-2-methanesulfonyl-biphenyl-4-yl)-amide;
(1R,2S)-1-3-(4-Chloro-phenyl)-ureido-2-hydroxymethyl-cyclopropanecarboxylic acid (3-fluoro-2-methanesulfonyl-biphenyl-4-yl)-amide;
(1R,2S)-1-3-(4-Chloro-phenyl)-ureido-2-hydroxymethyl-cyclopropanecarboxylic acid 2-fluoro-4-(2-oxo-piperidin-1-yl)-phenyl-amide;
(1S,2S)-1-3-(4-Chloro-phenyl)-ureido-2-hydroxymethyl-cyclopropanecarboxylic acid 2-fluoro-4-(2-oxo-piperidin-1-yl)-phenyl-amide;
2-3-(4-Chloro-phenyl)-ureido-N-2-fluoro-4-(2-oxo-piperidin-1-yl)-phenyl-2-methyl-propionamide;
2-3-(5-Chloro-pyridin-2-yl)-ureido-2-methyl-N-4-(2-oxo-piperidin-1-yl)-phenyl-propionamide;
2-3-(4-Chloro-phenyl)-ureido-2-methyl-N-4-(2-oxo-piperidin-1-yl)-phenyl-propionamide;
2-3-(5-Chloro-pyridin-2-yl)-ureido-N-2-fluoro-4-(2-oxo-piperidin-1-yl)-phenyl-2-methyl-propion amide;
N-2-Fluoro-4-(2-oxo-piperidin-1-yl)-phenyl-2-3-(4-fluoro-phenyl)-ureido-2-methyl-propionamide;
1-3-(4-Chloro-phenyl)-ureido-cyclopropanecarboxylic acid 2-fluoro-4-(2-oxo-piperidin-1-yl)-phenyl-amide;
1-3-(5-Chloro-pyridin-2-yl)-ureido-cyclopropanecarboxylic acid 4-(2-oxo-piperidin-1-yl)-phenyl-amide;
1-3-(4-Chloro-phenyl)-ureido-cyclopropanecarboxylic acid 4-(2-oxo-piperidin-1-yl)-phenyl-amide;
1-3-(5-Chloro-pyridin-2-yl)-ureido-cyclopropanecarboxylic acid 2-fluoro-4-(2-oxo-piperidin-1-yl)-phenyl-amide;
1-3-(4-Fluoro-phenyl)-ureido-cyclopropanecarboxylic acid 2-fluoro-4-(2-oxo-piperidin-1-yl)-phenyl-amide;
1-3-(4-Chloro-phenyl)-ureido-cyclohexanecarboxylic acid 2-fluoro-4-(2-oxo-piperidin-1-yl)-phenyl-amide;
1-3-(5-Chloro-pyridin-2-yl)-ureido-cyclohexanecarboxylic acid 4-(2-oxo-piperidin-1-yl)-phenyl-amide;
1-3-(4-Chloro-phenyl)-ureido-cyclohexanecarboxylic acid 4-(2-oxo-piperidin-1-yl)-phenyl-amide;
1-3-(5-Chloro-pyridin-2-yl)-ureido-cyclohexanecarboxylic acid 2-fluoro-4-(2-oxo-piperidin-1-yl)-phenyl-amide;
1-3-(4-Fluoro-phenyl)-ureido-cyclohexanecarboxylic acid 2-fluoro-4-(2-oxo-piperidin-1-yl)-phenyl-amide;
2-3-(4-Chloro-phenyl)-ureido-N-2-fluoro-4-(2-oxo-piperidin-1-yl)-phenyl-3-hydroxy-2-hydroxymethyl-propionamide;
2-3-(5-Chloro-pyridin-2-yl)-ureido-3-hydroxy-2-hydroxymethyl-N-4-(2-oxo-piperidin-1-yl)-phenyl-propionamide;
2-3-(4-Chloro-phenyl)-ureido-3-hydroxy-2-hydroxymethyl-N-4-(2-oxo-piperidin-1-yl)-phenyl-propionamide;
2-3-(5-Chloro-pyridin-2-yl)-ureido-N-2-fluoro-4-(2-oxo-piperidin-1-yl)-phenyl-3-hydroxy-2-hydroxymethyl-propionamide;
N-2-Fluoro-4-(2-oxo-piperidin-1-yl)-phenyl-2-3-(4-fluoro-phenyl)-ureido-3-hydroxy-2-hydroxymethyl-propionamide;
2-3-(4-Chloro-phenyl)-ureido-N-2-fluoro-4-(2-oxo-piperidin-1-yl)-phenyl-acetamide;
2-3-(5-Chloro-pyridin-2-yl)-ureido-N-2-fluoro-4-(2-oxo-piperidin-1-yl)-phenyl-acetamide;
2-3-(5-Chloro-pyridin-2-yl)-ureido-N-4-(2-oxo-piperidin-1-yl)-phenyl-acetamide;
2-3-(4-Chloro-phenyl)-ureido-N-4-(2-oxo-piperidin-1-yl)-phenyl-acetamide;
1-3-(4-Chloro-phenyl)-ureido-cyclopropanecarboxylic acid 5-(2-methanesulfonyl-phenyl)-pyridin-2-yl-amide;
1-3-(4-Chloro-phenyl)-ureido-cyclopropanecarboxylic acid 5-(2-sulfamoyl-phenyl)-pyridin-2-yl-amide;
1-3-(5-Chloro-pyridin-2-yl)-ureido-cyclopropanecarboxylic acid 5-(2-methanesulfonyl-phenyl)-pyridin-2-yl-amide;
1-3-(5-Chloro-pyridin-2-yl)-ureido-cyclopropanecarboxylic acid 5-(2-sulfamoyl-phenyl)-pyridin-2-yl-amide;
1-3-(4-Chloro-phenyl)-ureido-cyclopropanecarboxylic acid (2-methanesulfonyl-3-trifluoromethyl-biphenyl-4-yl)-amide;
1-3-(4-Chloro-phenyl)-ureido-cyclopropanecarboxylic acid (2-sulfamoyl-3-trifluoromethyl-biphenyl-4-yl)-amide;
1-3-(5-Chloro-pyridin-2-yl)-ureido-cyclopropanecarboxylic acid (2-methanesulfonyl-3-trifluoromethyl-biphenyl-4-yl)-amide;
1-3-(5-Chloro-pyridin-2-yl)-ureido)-cyclopropanecarboxylic acid (2-sulfamoyl-3-trifluoromethyl-biphenyl-4-yl)-amide;
1-3-(4-Chloro-phenyl)-ureido-cyclopropanecarboxylic acid (2-methanesulfonyl-3-methyl-biphenyl-4-yl)-amide;
1-3-(4-Chloro-phenyl)-ureido-cyclopropanecarboxylic acid (3-methyl-2-sulfamoyl-biphenyl-4-yl)-amide;
1-3-(5-Chloro-pyridin-2-yl)-ureido-cyclopropanecarboxylic acid (2-methanesulfonyl-3-methyl-biphenyl-4-yl)-amide;
1-3-(5-Chloro-pyridin-2-yl)-ureido-cyclopropanecarboxylic acid (3-methyl-2-sulfamoyl-biphenyl-4-yl)-amide;
2-3-(5-Chloro-pyridin-2-yl)-1-methyl-ureido-N-(2-methanesulfonyl-biphenyl-4-yl)-acetamide;
2-3-(4-Chloro-phenyl)-1-methyl-ureido-N-(2-sulfamoyl-biphenyl-4-yl)-acetamide;
2-3-(5-Chloro-pyridin-2-yl)-1-methyl-ureido-N-(3-fluoro-2-sulfamoyl-biphenyl-4-yl)-acetamide;
2-3-(4-Chloro-phenyl)-1-methyl-ureido-N-(3-fluoro-2-sulfamoyl-biphenyl-4-yl)-acetamide;
2-3-(5-Chloro-pyridin-2-yl)-1-methyl-ureido-N-(3-fluoro-2-methanesulfonyl-biphenyl-4-yl)-acetamide;
2-3-(4-Chloro-phenyl)-1-methyl-ureido-N-(2-methanesulfonyl-biphenyl-4-yl)-acetamide;
1-3-(4-Chloro-phenyl)-ureido-2-hydroxymethyl-cyclopropanecarboxylic acid (2-methanesulfonyl-biphenyl-4-yl)-amide;
1-3-(4-Chloro-phenyl)-ureido-2-hydroxymethyl-cyclopropanecarboxylic acid (2-sulfamoyl-biphenyl-4-yl)-amide;
1-3-(4-Chloro-phenyl)-ureido-2-hydroxymethyl-cyclopropanecarboxylic acid (3-fluoro-2-methanesulfonyl-biphenyl-4-yl)-amide;
1-3-(4-Chloro-phenyl)-ureido-2-hydroxymethyl-cyclopropanecarboxylic acid (3-fluoro-2-sulfamoyl-biphenyl-4-yl)-amide;
3-3-(4-Chloro-phenyl)-ureido-pyrrolidine-3-carboxylic acid (3-fluoro-2-methanesulfonyl-biphenyl-4-yl)-amide;
3-3-(4-Chloro-phenyl)-ureido-pyrrolidine-3-carboxylic acid (3-fluoro-2-sulfamoyl-biphenyl-4-yl)-amide;
1-3-(4-Chloro-phenyl)-ureido-3-hydroxymethyl-cyclobutanecarboxylic acid (3-fluoro-2-methanesulfonyl-biphenyl-4-yl)-amide;
1-3-(4-Chloro-phenyl)-ureido-3-hydroxymethyl-cyclobutanecarboxylic acid (3-fluoro-2-sulfamoyl-biphenyl-4-yl)-amide;
1-3-(4-Chloro-phenyl)-ureido-2-methoxymethyl-cyclopropanecarboxylic acid (3-fluoro-2-methanesulfonyl-biphenyl-4-yl)-amide;
1-3-(4-Chloro-phenyl)-ureido-2-methoxymethyl-cyclopropanecarboxylic acid (3-fluoro-2-sulfamoyl-biphenyl-4-yl)-amide;
2-Aminomethyl-1-3-(4-chloro-phenyl)-ureido-cyclopropanecarboxylic acid (3-fluoro-2-methanesulfonyl-biphenyl-4-yl)-amide;
2-Aminomethyl-1-3-(4-chloro-phenyl)-ureido-cyclopropanecarboxylic acid (3-fluoro-2-sulfamoyl-biphenyl-4-yl)-amide;
2-3-(4-Chloro-phenyl)-ureido-2-(3-fluoro-2-methanesulfonyl-biphenyl-4-ylcarbamoyl)-cyclopropanecarboxylic acid;
2-3-(4-Chloro-phenyl)-ureido-2-(3-fluoro-2-sulfamoyl-biphenyl-4-ylcarbamoyl)-cyclopropanecarboxylic acid;
3-3-(4-Chloro-phenyl)-ureido-1-methyl-pyrrolidine-3-carboxylic acid (3-fluoro-2-methanesulfonyl-biphenyl-4-yl)-amide;
3-3-(4-Chloro-phenyl)-ureido-1-methyl-pyrrolidine-3-carboxylic acid (3-fluoro-2-sulfamoyl-biphenyl-4-yl)-amide;
1-Acetyl-3-3-(4-chloro-phenyl)-ureido-pyrrolidine-3-carboxylic acid (3-fluoro-2-methanesulfonyl-biphenyl-4-yl)-amide;
1-Acetyl-3-3-(4-chloro-phenyl)-ureido-pyrrolidine-3-carboxylic acid (3-fluoro-2-sulfamoyl-biphenyl-4-yl)-amide;
1-3-(4-Chloro-phenyl)-ureido-3-methoxymethyl-cyclobutanecarboxylic acid (3-fluoro-2-methanesulfonyl-biphenyl-4-yl)-amide;
1-3-(4-Chloro-phenyl)-ureido-3-methoxymethyl-cyclobutanecarboxylic acid (3-fluoro-2-sulfamoyl-biphenyl-4-yl)-amide;
3-Aminomethyl-1-3-(4-chloro-phenyl)-ureido-cyclobutanecarboxylic acid (3-fluoro-2-methanesulfonyl-biphenyl-4-yl)-amide;
3-Aminomethyl-1-3-(4-chloro-phenyl)-ureido-cyclobutanecarboxylic acid (3-fluoro-2-sulfamoyl-biphenyl-4-yl)-amide;
3-3-(4-Chloro-phenyl)-ureido-3-(3-fluoro-2-methanesulfonyl-biphenyl-4-ylcarbamoyl)-cyclobutanecarboxylic acid;
3-3-(4-Chloro-phenyl)-ureido-3-(3-fluoro-2-sulfamoyl-biphenyl-4-ylcarbamoyl)-cyclobutanecarboxylic acid;
4-3-(4-Chloro-phenyl)-ureido-piperidine-4-carboxylic acid (3-fluoro-2-methanesulfonyl-biphenyl-4-yl)-amide;
4-3-(4-Chloro-phenyl)-ureido-piperidine-4-carboxylic acid (3-fluoro-2-sulfamoyl-biphenyl-4-yl)-amide;
4-3-(4-Chloro-phenyl)-ureido-1-methyl-piperidine-4-carboxylic acid (3-fluoro-2-methanesulfonyl-biphenyl-4-yl)-amide;
4-3-(4-Chloro-phenyl)-ureido-1-methyl-piperidine4-carboxylic acid (3-fluoro-2-sulfamoyl-biphenyl-4-yl)-amide;
1-Acetyl-4-3-(4-chloro-phenyl)-ureido-piperidine-4-carboxylic acid (3-fluoro-2-methanesulfonyl-biphenyl-4-yl)-amide;
1-Acetyl-4-3-(4-chloro-phenyl)-ureido-piperidine-4-carboxylic acid (3-fluoro-2-sulfamoyl-biphenyl-4-yl)-amide;
1-3-(4-Chloro-phenyl)-ureido-3,4-dihydroxy-cyclopentanecarboxylic acid (3-fluoro-2-methanesulfonyl-biphenyl-4-yl)-amide;
1-3-(4-Chloro-phenyl)-ureido-3,4-dihydroxy-cyclopentanecarboxylic acid (3-fluoro-2-sulfamoyl-biphenyl-4-yl)-amide;
3-3-(4-Chloro-phenyl)-ureido)-tetrahydro-furan-3-carboxylic acid (3-fluoro-2-methanesulfonyl-biphenyl-4-yl)-amide;
3-3-(4-Chloro-phenyl)-ureido-tetrahydro-furan-3-carboxylic acid (3-fluoro-2-sulfamoyl-biphenyl-4-yl)-amide;
3-3-(4-Chloro-phenyl)-ureido-tetrahydro-thiophene-3-carboxylic acid (3-fluoro-2-methanesulfonyl-biphenyl-4-yl)-amide;
3-3-(4-Chloro-phenyl)-ureido-1-methyl-pyrrolidine-3-carboxylic acid 2-fluoro-4-(2-oxo-piperidin-1-yl)-phenyl-amide;
1-Acetyl-3-3-(4-chloro-phenyl)-ureido-pyrrolidine-3-carboxylic acid 2-fluoro-4-(2-oxo-piperidin-1-yl)-phenyl -amide;
1-Acetyl-3-3-(4-chloro-phenyl)-ureido-azetidine-3-carboxylic acid (3-fluoro-2-methanesulfonyl-biphenyl-4-yl)-amide;
1-Acetyl-3-3-(4-chloro-phenyl)-ureido-azetidine-3-carboxylic acid (3-fluoro-2-sulfamoyl-biphenyl-4-yl)-amide;
1-3-(4-Chloro-phenyl)-1-methyl-ureido-2-hydroxymethyl-cyclopropanecarboxylic acid 2-fluoro-4-(2-oxo-piperidin-1-yl)-phenyl-amide;
1-3-(4-Chloro-phenyl)-1-methyl-ureido-2-hydroxymethyl-cyclopropanecarboxylic acid (3-fluoro-2-sulfamoyl-biphenyl-4-yl)-amide;
1-3-(4-Chloro-phenyl)-1-methyl-ureido-2-hydroxymethyl-cyclopropanecarboxylic acid (3-fluoro-2-methanesulfonyl-biphenyl-4-yl)-amide;
3-3-(4-Chloro-phenyl)-ureido-tetrahydro-thiophene-3-carboxylic acid (3-fluoro-2-sulfamoyl-biphenyl-4-yl)-amide;
3-3-(4-Chloro-phenyl)-ureido-1-methyl-azetidine-3-carboxylic acid (3-fluoro-2-methanesulfonyl-biphenyl-4-yl)-amide;
3-3-(4-Chloro-phenyl)-ureido-1-methyl-azetidine-3-carboxylic acid (3-fluoro-2-sulfamoyl-biphenyl-4-yl)-amide;
1-3-(4-Chloro-phenyl)-ureido-2-hydroxymethyl-cyclopropanecarboxylic acid 2-fluoro-4-(2-oxo-piperidin-1-yl)-phenyl-amide;
1-3-(4-Chloro-phenyl)-ureido-2-methoxymethyl-cyclopropanecarboxylic acid 2-fluoro-4-(2-oxo-piperidin-1-yl)-phenyl-amide;
3-Amino-2-aminomethyl-2-3-(4-chloro-phenyl)-ureido-N-(3-fluoro-2-sulfamoyl-biphenyl-4-yl)-propionamide;
3-Amino-2-aminomethyl-2-3-(4-chloro-phenyl)-ureido-N-(3-fluoro-2-methanesulfonyl-biphenyl-4-yl)-propionamide;
2-3-(4-Chloro-phenyl)-ureido-3-ethylamino-2-ethylaminomethyl-N-(3-fluoro-2-methanesulfonyl-biphenyl-4-yl)-propionamide;
2-3-(4-Chloro-phenyl)-1-cyclopropylmethyl-ureido-N-(3-fluoro-2-sulfamoyl-biphenyl-4-yl)-acetamide;
2-3-(4-Chloro-phenyl)-1-cyclopropylmethyl-ureido-N-2-fluoro-4-(2-oxo-piperidin-1-yl)-phenyl-acetaminde;
2-3-(4-Chloro-phenyl)-1-cyclopropylmethyl-ureido-N-2-fluoro-4-(2-oxo-2H-pyridin-1-yl)-phenyl-acetamide;
2-3-(5-Chloro-pyridin-2-yl)-1-cyclopropylmethyl-ureido-N-(3-fluoro-2-methanesulfonyl-biphenyl-4-yl)-acetamide;
2-3-(4-Chloro-phenyl)-1-cyclopropyl-ureido-N-(3-fluoro-2-methanesulfonyl-biphenyl-4-yl)-acetamide;
2-3-(5-Chloro-pyridin-2-yl)-1-cyclopropylmethyl-ureido-N-(3-fluoro-2-sulfamoyl-biphenyl-4-yl)-acetamide;
2-3-(5-Chloro-pyridin-2-yl)-1-cyclopropylmethyl-ureido-N-2-fluoro-4-(2-oxo-piperidin-1-yl)-phenyl-acetamide;
2-3-(5-Chloro-pyridin-2-yl)-1-cyclopropylmethyl-ureido-N-2-fluoro-4-(2-oxo-2H-pyridin-1-yl)-phenyl-acetamide;
2-3-(4-Chloro-phenyl)-1-isopropyl-ureido-N-(3-fluoro-2-methanesulfonyl-biphenyl-4-yl)-acetamide;
2-3-(4-Chloro-phenyl)-1-cyclopentyl-ureido-N-(3-fluoro-2-methanesulfonyl-biphenyl-4-yl)-acetamide;
2-3-(4-Chloro-phenyl)-1-cyclopentylmethyl-ureido-N-(3-fluoro-2-methanesulfonyl-biphenyl-4-yl)-acetamide;
2-3-(4-Chloro-phenyl)-1-(2-cyclopropyl-ethyl)-ureido-N-(3-fluoro-2-methanesulfonyl-biphenyl-4-yl)-acetamide;
2-3-(4-Chloro-phenyl)-1-phenyl-ureido-N-(3-fluoro-2-methanesulfonyl-biphenyl-4-yl)-acetamide;
2-3-(4-Chloro-phenyl)-1-thiophen-3-ylmethyl-ureido-N-(3-fluoro-2-methanesulfonyl-biphenyl-4-yl)-acetamide;
2-3-(4-Chloro-phenyl)-1-pyridin-3-ylmethyl-ureido-N-(3-fluoro-2-methanesulfonyl-biphenyl-4-yl)-acetamide;
2-3-(4-Chloro-phenyl)-1-cyclohexylmethyl-ureido-N-(3-fluoro-2-methanesulfonyl-biphenyl-4-yl)-acetamide;
2-3-(4-Chloro-phenyl)-1-(2-cyclopentyl-ethyl)-ureido-N-(3-fluoro-2-methanesulfonyl-biphenyl-4-yl)-acetamide;
2-3-(4-Chloro-phenyl)-1-thiophen-2-ylmethyl-ureido) -N-(3-fluoro-2-methanesulfonyl-biphenyl-4-yl)-acetamide;
2-3-(4-Chloro-phenyl)-1-pyridin-2-ylmethyl-ureido)-N-(3-fluoro-2-methanesulfonyl-biphenyl-4-yl)-acetamide;
2-3-(4-Chloro-phenyl)-1-pyridin-4-ylmethyl-ureido-N-(3-fluoro-2-methanesulfonyl-biphenyl-4-yl)-acetamide;
2-3-(4-Chloro-phenyl)-1-(2-ethoxy-ethyl)-ureido-N-(3-fluoro-2-methanesulfonyl-biphenyl-4-yl)-acetamide;
2-3-(4-Chloro-phenyl)-1-(2-methylsulfanyl-ethyl)-ureido-N-(3-fluoro-2-methanesulfonyl-biphenyl-4-yl)-acetamide;
3-(4-Chloro-phenyl)-1-(3-fluoro-2-methanesulfonyl-biphenyl-4-ylcarbamoyl)-methyl-ureido-acetic acid;
2-3-(4-Chloro-phenyl)-1-(2-morpholin-4-yl-ethyl)-ureido-N-(3-fluoro-2-methanesulfonyl-biphenyl-4-yl)-acetamide;
2-3-(4-Chloro-phenyl)-1-(2-thiomorpholin-4-yl-ethyl)-ureido-N-(3-fluoro-2-methanesulfonyl-biphenyl-4-yl)-acetamide;
2-3-(4-Chloro-phenyl)-l1-phenethyl-ureido-N-(3-fluoro-2-methanesulfonyl-biphenyl-4-yl)-acetamide;
2-3-(4-Chloro-phenyl)-1-(2-methylsulfanyl-ethyl)-ureido-N-(3-fluoro-2-methanesulfonyl-biphenyl-4-yl)-acetamide;
2-3-(4-Chloro-phenyl)-1-methylcarbamoylmethyl-ureido-N-(3-fluoro-2-methanesulfonyl-biphenyl-4-yl)-acetamide;
2-3-(4-Chloro-phenyl)-1-2-(4-methyl-piperazin-1-yl)-ethyl-ureido-N-(3-fluoro-2-methanesulfonyl-biphenyl-4-yl)-acetamide;
2-1-(2-Acetylamino-ethyl)-3-(4-chloro-phenyl)-ureido-N-(3-fluoro-2-methanesulfonyl-biphenyl-4-yl)-acetamide;
2-3-(4-Chloro-phenyl)-1-(2,2-dimethyl-propyl)-ureido-N-(3-fluoro-2-methanesulfonyl-biphenyl-4-yl)-acetamide;
3-3-(4-Chloro-phenyl)-ureido-3-(3-fluoro-2-methanesulfonyl-biphenyl-4-ylcarbamoyl)-pyrrolidine-1-carboxylic acid benzyl ester;
2-3-(4-Chloro-phenyl)-1-(2,2-dimethyl-propyl)-ureido-N-2-fluoro-4-(2-oxo-piperidin-1-yl)-phenyl-acetamide;
2-3-(4-Chloro-phenyl)-1-cyclobutylmethyl-ureido-N-(3-fluoro-2-methanesulfonyl-biphenyl-4-yl)-acetamide;
2-3-(4-Chloro-phenyl)-1-cyclopropylmethyl-ureido-N-(3-fluoro-2-methanesulfonyl-biphenyl-4-yl)-acetamide;
2-3-(4-Chloro-phenyl)-1-(2-methoxy-ethyl)-ureido-N-(3-fluoro-2-methanesulfonyl-biphenyl-4-yl)-acetamide;
2-3-(4-Chloro-phenyl)-1-isobutyl-ureido-N-(3-fluoro-2-methanesulfonyl-biphenyl-4-yl)-acetamide;
2-3-(4-Chloro-phenyl)-1-(2-dimethylamino-ethyl)-ureido-N-(3-fluoro-2-methanesulfonyl-biphenyl-4-yl)-acetamide;
2-1-Benzyl-3-(4-chloro-phenyl)-ureido-N-(3-fluoro-2methanesulfonyl-biphenyl-4-yl)-acetamide;
2-3-(4-Chloro-phenyl)-1-(4-methoxy-benzyl) ureido)-N-(3-fluoro-2-methanesulfonyl-biphenyl-4-yl)-acetamide;
(1R,2S)-(1-3-(4-Chloro-phenyl)-ureido-2-hydroxymethyl-cyclopropanecarboxylic acid 2-fluoro4-(2-oxo-2H-pyridin-1-yl)-phenyl-amide;
(1S,2S)-1-3-(4-Chloro-phenyl)-ureido-2-hydroxymethyl-cyclopropanecarboxylic acid 2-fluoro-4-(2-oxo-2H-pyridin-1-yl)-phenyl-amide;
1-3-(4-Chloro-phenyl)-ureido-cyclopropanecarboxylic acid 2-fluoro-4-(2-oxo-2H-pyridin-1-yl)-phenyl-amide;
1-3-(4-Chloro-phenyl)-ureido-cyclopropanecarboxylic acid 2-fluoro-4-(5-methyl-pyrazol-1-yl)-phenyl-amide;
(1R,2S)-1-3-(4-Chloro-phenyl)-ureido-2-hydroxymethyl-cyclopropanecarboxylic acid 2-fluoro-4-(5-methyl-pyrazol-1-yl)-phenyl)-amide;
(1S,2S)-1-3-(4-Chloro-phenyl)-ureido-2-hydroxymethyl-cyclopropanecarboxylic acid 2-fluoro-4-(5-methyl-pyrazol-1-yl)-phenyl)-amide;
2-3-(4-Chloro-phenyl)-1-cyclopropylmethyl-ureido-N-2-fluoro-4-(5-methyl-pyrazol-1-yl)-phenyl-acetamide;
1-3-(4-Chloro-phenyl)-ureido-cyclopropanecarboxylic acid 4-(3,5-dimethyl-pyrazol-1-yl)-2-fluoro-phenyl-amide;
2-3-(4-Chloro-phenyl)-1-cyclopropylmethyl-ureido-N-4-(3,5-dimethyl-pyrazol-1-yl)-2-fluoro-phenyl-acetamide;
(1R,2S)-1-3-(4-Chloro-phenyl)-ureido)-2-hydroxymethyl-cyclopropanecarboxylic acid (2-fluoro-4-pyrazol-1-yl-phenyl)-amide;
(1S,2S)-1-3-(4-Chloro-phenyl)-ureido-2-hydroxymethyl-cyclopropanecarboxylic acid (2-fluoro-4-pyrazol-1-yl-phenyl)-amide;
(1R,2S)-1-3-(4-Chloro-phenyl)-ureido-2-hydroxymethyl-cyclopropanecarboxylic acid 2-fluoro-4-(3-methyl-pyrazol-1-yl)-phenyl-amide;
(1S,2S)-1-3-(4-Chloro-phenyl)-ureido-2-hydroxymethyl-cyclopropanecarboxylic acid 2-fluoro-4-(3-methyl-pyrazol-1-yl)-phenyl-amide;
(1R,2S)-1-3-(4-Chloro-phenyl)-ureido-2-hydroxymethyl-cyclopropanecarboxylic acid 2-fluoro-4-(2-methyl-imidazol-1-yl)-phenyl-amide;
(1S,2S)-1-3-(4-Chloro-phenyl)-ureido-2-hydroxymethyl-cyclopropanecarboxylic acid 2-fluoro-4-(2-methyl-imidazol-1-yl)-phenyl-amide;
(1R,2S)-1-3-(4-Chloro-phenyl)-ureido-2-hydroxymethyl-cyclopropanecarboxylic acid 4-(2,5-dihydro-pyrrole-1-carbonyl)-2-fluoro-phenyl-amide;
(1S,2S)-1-3-(4-Chloro-phenyl)-ureido-2-hydroxymethyl-cyclopropanecarboxylic acid 4-(2,5-dihydro-pyrrole-1-carbonyl)-2-fluoro-phenyl-amide;
(1R,2S)-1-3-(4-Chloro-phenyl)-ureido-2-hydroxymethyl-cyclopropanecarboxylic acid 2-fluoro-4-(pyrrolidine-1-carbonyl)-phenyl-amide;
(1S,2S)-1-3-(4-Chloro-phenyl)-ureido-2-hydroxymethyl-cyclopropanecarboxylic acid 2-fluoro-4-(pyrrolidine-1-carbonyl)-phenyl-amide;
(1R,2S)-2-(Acetylamino-methyl)-1-3-(4-chloro-phenyl)-ureido-cyclopropanecarboxylic acid (3-fluoro-2-methanesulfonyl-biphenyl-4-yl)-amide;
(1S,2S)-2-(Acetylamino-methyl)-1-3-(4-chloro-phenyl)-ureido-cyclopropanecarboxylic acid (3-fluoro-2-methanesulfonyl-biphenyl-4-yl)-amide;
or a pharmaceutically acceptable salt thereof.
23. A process for the preparation of compounds of Formula I, wherein P1 is a protecting group, Y1 is a halogen and X1, X2, A, M, and Q are as defined above, comprising
(a) contacting an amino acid having Formula III with a reagent capable of forming a protecting group on the amino group of the amino acid to form a compound with Formula IV
113
(b) activating of the carboxylic acid of Formula IV and contacting it with an amino compound of the formula H2N-M-Y1 to form a compound of Formula V
114
(c) coupling the compound of Formula V with a compound having Q to form a compound of Formula VI
115
(d) removing the amino protecting group of the compound of Formula VI and contacting the resulting free amine with an isocyanate having A to form a compound of Formula I
116
24. A process for the preparation of compounds of Formula I, wherein P1 is a protecting group, and X1, X2, A, M, and Q are as defined above, comprising
(a) contacting an amino acid having Formula X with a reagent capable of forming a protecting group on the amino group of the amino acid to form a compound with Formula XI
117
(b) activating of the carboxylic acid of Formula XI and contacting it with an amino compound of the formula H2N-M-Q to form a compound of Formula XII
and
118
(c) removing the amino protecting group of the compound of Formula XII and contacting the resulting free amine with an isocyanate having A to form a compound of Formula I
119
25. A process for the preparation of compounds of Formula I, wherein A, M, Q and R2 are as defined above, comprising
(a) contacting a compound of Formula XVII with a bromoacetyl chloride of the Formula XX to form a compound of Formula XXI
120
(b) contacting a compound of Formula XXI with an amine of Formula XXII to form a compound of Formula XXIII
121
and
(c) contacting a compound of Formula XXIII with an isocyanate having A to form a compound of Formula I
122
26. A process for the preparation of compounds of Formula I, wherein P1 and P2 are independent protecting groups and A, M, and Q are as defined above, comprising
(a) base catalyzed ring opening of a compound of Formula XXVIII to form a compound of Formula XXIX
123
(b) contacting a compound of Formula XXIX with a reagent capable of forming a protecting group on the hydroxyl groups followed by contacting the resulting intermediate with a reagent capable of selective deprotection of the carboxylic acid hydroxyl group to form a compound with Formula XXX
124
(c) activating the carboxylic acid of Formula XXX and contacting it with an amino compound of the formula XXXI to form a compound of Formula XXXII
125
and
(d) removing the amino protecting group of the compound of Formula XXXII and contacting the resulting free amine with an isocyanate having A to from a compound of Formula I
126
27. A process for the preparation of compounds of Formula I, wherein P1 and P2 are independent protecting groups and A, M, and Q are as defined above, comprising
(a) contacting a compound of Formula XXXIII with a reagent capable of selectively forming a protecting group on the alcohol hydroxyl group to form a compound with Formula XXXIV
127
(b) activating the carboxylic acid of Formula XXXIV and contacting it with an amino compound of the formula XXXV to form a compound of Formula XXXVI
128
(c) removing the amino protecting group of the compound of Formula XXXVI and contacting the resulting free amine with an isocyanate having A to from a compound of Formula XXXVII
129
and
(d) removing the alcohol hydroxy protecting group of the compound of Formula XXXVII to from a compound of Formula I
130
28. A process for the preparation of compounds of Formula I, wherein P1 and P2 are independently protecting groups and A, M, and Q are as defined above, comprising
(a) contacting a compound of Formula XXXVIII with acid to form a compound of Formula XXXIX
131
(b) contacting a compound of Formula XXXIX with a reagent capable of forming a protecting group on the amino moiety to form a compound of Formula XL
132
(c) contacting a compound of Formula XL with a reagent capable of forming a protecting group on the heterocycle nitrogen to form a compound of Formula XLI
133
(d) contacting a compound of Formula XLI with a reagent capable of removing the protecting group of the carboxylic acid to form a compound of Formula XLII
134
(e) activating the carboxylic acid of Formula XLII and contacting it with an amino compound of the formula XLIII to form a compound of Formula XLIV
135
and
(f) removing the amino protecting group of the compound of Formula XLIV and contacting the resulting free amine with an isocyanate having A to from a compound of Formula I
136
29. A method of treating or preventing thrombotic disorders in a mammal comprising administering to said mammal a therapeutically effective amount of a compound according to claims 1 or 22.
30. The method of claim 29, wherein said disorder is venous thrombosis.
31. The method of claim 29, wherein said disorder is arterial thrombosis.
32. The method of claim 29, wherein said disorder is pulmonary embolism.
33. The method of claim 29, wherein said disorder is myocardial infarction.
34. The method of claim 29, wherein said disorder is cerebral infarction.
35. The method of claim 29, wherein said disorder is restenosis.
36. The method of claim 29, wherein said disorder is cancer.
37. The method of claim 29, wherein said disorder is angina.
38. The method of claim 29, wherein said disorder is diabetes.
39. The method of claim 29, wherein said disorder is atrial fibrillation.
40. The method of claim 29, wherein said disorder is heart failure.
41. A method of inhibiting Factor Xa in a mammal comprising administering to said mammal a compound according to claims 1 or 22.l
42. A pharmaceutical formulation comprising a compound of claim 1 or 22 admixed with a carrier, diluent, or excipient.