1. A lubrication system for a wind turbine gearbox, the lubrication system comprising:
a supply subsystem for providing oil via an oil tank or a hydraulic accumulator to a gearbox of the wind turbine for lubrication during at least one of idling or loss of electric grid; and
a control subsystem for controlling the flow of oil in the lubrication system.
2. The lubrication system according to claim 1, wherein the system provides lubrication by converting a dry sump gearbox to a wet sump gearbox for splash lubrication.
3. The lubrication system according to claim 1, wherein the supply subsystem provides oil to the gearbox by gravity.
4. The lubrication system according to claim 1, wherein the supply subsystem provides oil to the gearbox at an optimum pressure for lubrication of a plurality of components of the gearbox.
5. The lubrication system according to claim 1, wherein the lubrication system comprises a drain tank for collecting the oil flowing out of the gearbox.
6. The lubrication system according to claim 5, wherein the lubrication system comprises a pump for pumping the oil from the drain tank to the supply subsystem.
7. The lubrication system according to claim 1, wherein the lubrication system comprises a manifold with a plurality of nozzles in the gearbox for providing a flow of pressurized oil to the plurality of components of the gearbox.
8. The lubrication system according to claim 1, wherein the supply subsystem comprises the oil tank at a predefined elevation above the gearbox for providing oil to the gearbox.
9. The lubrication system according to claim 1, wherein the hydraulic accumulator is provided at any convenient location.
10. The lubrication system according to claim 9, wherein the hydraulic accumulator comprises a pressure storage reservoir filled with oil and a compressed gas and provides oil by gravity or at a pressure to lubricate various components of the gearbox.
11. The lubrication system according to claim 1, wherein the system comprises a plurality of direction control valves and a plurality of drain ports for controlling the flow of oil in the lubrication system
12. The lubrication system according to claim 1, wherein the control subsystem comprises a control logic for controlling the plurality of direction control valves and the plurality of drain ports.
13. The lubrication system according to claim 1, wherein the control subsystem further controls opening or closing of the plurality of drain ports in a drain manifold of the gearbox to permit storage of the oil at an optimal level in the gearbox for splash lubrication.
14. The lubrication system according to claim 1, wherein the control subsystem is provided with auxiliary power supply for operation of the valves under loss of electric grid and idling condition.
15. The lubrication system according to claim 1, wherein the direction control valves comprises a plurality of solenoid valves and a plurality of check valves.
16. A lubrication system for a wind turbine, the lubrication system comprising:
a hydraulic accumulator for providing oil to a gearbox of the wind turbine for splash lubrication during idling or loss of electric grid;
a control subsystem for controlling a plurality of direction control valves and a plurality of drain ports configured to control the flow of oil in the lubrication system;
a drain tank for collecting the oil flowing out of the gearbox; and
an auxiliary pump for pumping the oil from the drain tank to the accumulator.
17. The lubrication system according to claim 16, wherein the accumulator is charged using the auxiliary pump or a scavenge pump or a main electrical pump with a directional control valve.
18. The lubrication system according to claim 16, wherein the accumulator is charged with a gas charging cylinder if a bladder pressure is reduced below a level.
19. The lubrication system according to claim 16, wherein the accumulator provides oil by gravity to the gearbox for splash lubrication.
20. The lubrication system according to claim 16, wherein the accumulator provides oil at a pressure to lubricate a plurality of components of the gearbox
21. A lubrication system for a wind turbine, the lubrication system comprising:
an oil tank for providing oil to a gearbox of the wind turbine for splash lubrication during idling or loss of electric grid;
a control subsystem for controlling a plurality of direction control valves and a plurality of drain ports configured to control the flow of oil in the lubrication system;
a drain tank for collecting the oil flowing out of the gearbox; and
a pump for pumping the oil from the drain tank to the oil tank.
22. The lubrication system according to claim 21, wherein the oil tank is compensated with oil provided by the pump or a scavenge pump or a main electrical pump with a directional control valve for charging.
23. A method for lubricating a wind turbine gearbox, the method steps comprising:
providing a supply subsystem for supplying oil to the gearbox for splash lubrication during loss of electric grid or idling;
controlling a plurality of direction control valves and a plurality of drain ports using a control subsystem for allowing controlled flow of oil;
collecting the oil flowing out of the gearbox in a drain tank; and
recycling the oil collected in the drain tank by pumping the oil to the supply subsystem.
24. The method of claim 23, wherein the supply subsystem provides oil to the gearbox from an oil tank at a predefined elevation.
25. The method of claim 23, wherein the supply subsystem provides oil to the gearbox from an accumulator.
26. The method of claim 23, wherein the method comprises charging of the supply subsystem during on-grid conditions and discharging the supply subsystem during gridloss and idling.
27. The method of claim 26, wherein the charging of the supply subsystem comprises flowing the oil from the gearbox to the drain tank through a plurality of normally closed direction control valves connected to the gearbox.
28. The method of claim 26, wherein the charging of the supply subsystem comprises operating an auxiliary pump and closing a normally open direction control valve connected to the auxiliary pump for pumping the oil from the drain tank to the supply subsystem and filling the supply subsystem to an optimal level or pressure.
29. The method of claim 26, wherein the charging of the supply subsystem comprises preventing flow of oil from the supply subsystem to the gearbox through a plurality of normally open direction control valves connected to the supply subsystem.
30. The method of claim 26, wherein the discharging of the supply subsystem comprises closing the plurality of normally closed direction control valves connected to the gearbox for preventing the flow of oil from the gearbox to the drain tank.
31. The method of claim 26, wherein the discharging of the supply subsystem comprises preventing any addition of oil in the supply subsystem by the auxiliary pump and the normally open direction control valve connected to the auxiliary pump for.
32. The method of claim 26, wherein the discharging of the supply subsystem comprises opening the plurality of normally open direction control valves connected to the supply subsystem for flowing the oil from the supply subsystem to the gearbox.
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 of Formula I:
102
or a stereoisomer or pharmaceutically acceptable salt thereof, wherein;
ring M, including M1, M2, and M3, is a 5, 6, or 7 membered non-aromatic carbocycle or 5, 6, or 7 membered non-aromatic heterocycle, consisting of: carbon atoms, 0-3 N, and 0-1 heteroatoms selected from 0 and S(O)p, provided that ring M consists of a total of 0-3 O, S(O)p and N;
alternatively, ring M is an aromatic heterocycle selected from 2-pyridinone, 3-pyridazinone, 4-pyrimidinone, 2-pyrazinone, pyrimidine-2,4-dione, pyridazine-3,6-dione, 1H-quinolin-2-one, 1,4-dihydro-pyrrolo3,2-bpyridin-5-one and 1,4-dihydro-imidazo4,5-bpyridin-5-one;
ring M is substituted with 0-2 R1a, 0-1 Z, and 0-2 carbonyl groups, and, comprises: 0-2 double bonds;
provided that ring M is other than an isoxazoline, isothiazoline, pyrazoline, triazoline, tetrazoline, 3-phenyl-substituted pyrrolidine, 3-phenyl-substituted pyrroline, 3-phenyl-substituted isoxazolidine, or 4-phenyl-substituted isoxazolidine;
G is a group of formula IIa or IIb:
103
G1 is selected from (CR3aR3b) 1-5, (CR3aR3b)0-2CR3aCR3a(CR3aR3b) 0-2, (CR3aR3b)0-2CC(CR3aR3b)0-2, (CR3aR3b)uC(O)(CR3aR3b)w, (CR3aR3b)uC(O)O(CR3aR3b)w, (CR3aR3b)uOC(O)(CR3aR3b)w, (CR3aR3b)uO(CR3aR3b)w, (CR3aR3b)uNR3e(CR3aR3b)w, (CR3aR3b)uC(O)NR3(CR3aR3b)w, (CR3aR3b)uNR3C(O)(CR3aR3b)w, (CR3aR3b)uOC(O)uNR3(CR3aR3b)w, (CR3aR3b)uNR3C(O)O(CR3aR3b)w, (CR3aR3b)uNR3C(O)NR3(CR3aR3b)w, (CR3aR3b)uNR3C(S)NR3(CR3aR3b)w, (CR3aR3b)uS(CR3aR3b)w, (CR3aR3b)uS(O)(CR3aR3b)w, (CR3aR3b)uS(O)2(CR3aR3b)w, (CR3aR3b)uS(O)NR3(CR3aR3b)w, (CR3aR3b)uNR3S(O)2 (CR3aR3b)w, (CR3aR3b)uS(O)2NR3(CR3aR3b)w, (CR3aR3b)uNR3S(O)2NR3(CR3aR3b)w, and (CR3aR3b)uS(O)2NR3C(O)NR3(CR3aR3b)w, wherein uw total 0, 1, 2, 3, or 4, provided that G1 does not form a NN or NO bond with either group to which it is attached;
ring D, including the two atoms of Ring E to which it is attached, is a 5-6 membered non-aromatic ring consisting of carbon atoms, 0-1 double bonds, and 0-2 N, and D is substituted with 0-2 R;
alternatively, ring D, including the two atoms of Ring E to which it is attached, is a 5-6 membered aromatic system consisting of carbon atoms and 0-2 heteroatoms selected from the group consisting of N, O, and S(O)p, and D is substituted with 0-2 R;
E is selected from phenyl, pyridyl, pyrimidyl, pyrazinyl, and pyridazinyl, and is substituted with 0-2 R;
R is selected from C1-4 alkyl, F, Cl, Br, I, OH, OCH3, OCH2CH3, OCH(CH3)2, OCH2CH2CH3, CN, C(NR8)NR7R9, NHC(NR8)NR7R9, NR8CH(NR7), NH2, NH(C1-3 alkyl), N(C1-3 alkyl)2, C(NH)NH2, CH2NH2, CH2NH(C1-3 alkyl), CH2N(C1-3 alkyl)2, CH2CH2NH2, CH2CH2NH(C1-3 alkyl), CH2CH2N(C1-3 alkyl)2, (CR8R9)tC(O) H, (CR8R9)tC(O)R2c, (CR8R9) tNR7R8, (CR8R9) tC(O)NR7R8, (CR8R9) tOR3a, (CR8R9)tNR7C(O)R7, (CR8R9)tS(O)pNR7R8, (CR8R9)tNR7S(O)pR3f, (CR8R9)tS(O)R3c, (CR8R9)tS(O)2R3c, and OCF3;
alternatively, the bridging portion of ring D is absent, and ring E is selected from phenyl, thienyl, pyridyl, pyrimidyl, pyrazinyl, and pyridazinyl, and ring E is substituted with Ra and Rb;
alternatively, ring E is substituted with a 5-6 membered aromatic heterocycle consisting of: carbon atoms and 1-4 heteroatoms selected from the group consisting of N, O, and S(O)p, and said aromatic heterocycle is substituted with Ra and Rb;
alternatively, ring E is substituted with a 5-6 membered non-aromatic hetercocyle consisting of: carbon atoms and 1-4 heteroatoms selected from the group consisting of N, O, and S(O)p, and said non-aromatic hetercocyle is substituted with Ra and Rb, 0-2 carbonyl groups and containing 0-2 double bonds;
Ra and Rb, at each occurrence, are independently selected from H, C1-4 alkyl, F, Cl, Br, I, OH, OCH3, OCH2CH3, OCH(CH3)2, OCH2CH2CH3, CN, C(NR8)NR7R9, NHC(NR8)NR7R9, NR8CH(NR7), NH2, NH(Cl1-3 alkyl), N(C1-3 alkyl)2, C(NH)NH2, CH2NH2, CH2NH(C1-3 alkyl), CH2N(C1-3 alkyl) 2, CH2CH2NH2, CH2CH2NH(C1-3 alkyl), CH2CH2N(C1-3 alkyl)2, (CR8R9)tC(O)H, (CR8R9)tC(O)R2c, (CR8R9) tNR7R8, (CR8R9) tC(O)NR7R8, (CR8R9) tOR3a, (CR8R9)tNR7C(O)R3f, (CR8R9)tS(O)pNR7R8, (CR8R9)tNR7S(O)pR3f, (CR8R9)tS(O)R3c, (CR8R9)tS(O)2R3c, and OCF3;
alternatively, Ra and Rb combine to form methylenedioxy or ethylenedioxy;
alternatively, the bridging portion of ring D is absent, and ring E is selected from pyrrolyl, pyrazolyl, imidazolyl, isoxazolyl, oxazolyl, triazolyl, thienyl, and thiazolyl, and ring E is substituted with 0-2 Rc;
Rc is selected from C1-4 alkyl, F, Cl, Br, I, OH, OCH3, OCH2CH3, OCH(CH3)2, OCH2CH2CH3, CN, C(NR8)NR7R9, NHC(NR8)NR7R9, NR8CH(NR7), NH2, NH(C1-3 alkyl), N(C1-3 alkyl)2, C(NH)NH2, CH2NH2, CH2NH(C1-3 alkyl), CH2N(C1-3 alkyl)2, CH2CH2NH2, CH2CH2NH(C1-3 alkyl), CH2CH2N(C1-3 alkyl)2, (CR8R9)tNR7R8, (CR8R9)tC(O)NR7R8, (CR8R9)tC(O)H, (CR8R9)tC(O)R2c, (CR8R9)tNR7C(O)R7, (CR8R9)tS(O)pNR7R8, (CR8R9)tNR7S(O)pR3f, (CR8R9)tS(O)R3f, (CR8R9)tS(O)2R3f, and OCF3;
A is selected from:
C3-10 carbocyclic residue substituted with 0-2 R4, and 5-12 membered heterocyclic system containing from 1-4 heteroatoms selected from the group consisting of N, O, and S substituted with 0-2 R4;
provided that B and ring M are attached to different atoms on A;
B is selected from: Y and XY;
X is selected from (CR2R2a)1-4, CR2(CR2R2b) (CH2)t, C(O), C(NR1c), CR2(NR1cR2), CR2(OR2), CR2 (SR2), C(O)CR2R2a, CR2R2aC(O), S, S(O), S(O)2, SCR2R2a, S(O)CR2R2a, S(O)2CR2R2a, CR2R2aS, CR2R2aS(O), CR2R2aS(O)2, S(O)2NR2, NR2S(O)2, NR2S(O)2CR2R2a, CR2R2aS( )2NR2, NR2S(O)2NR2, C(O)NR2, NR2C(O), C(O)NR2CR2R2a, NR2C(O)CR2R2a, CR2R2aC(O)NR2, CR2R2aNR2C(O), NR2C(O)O, OC(O)NR2, NR2C(O)NR2, NR2, NR2CR2R2a, CR2R2aNR2, O, CR2R2aO, and OCR2R2a;
Y is selected from:
(CH2)rNR2R2a, provided that XY do not form a NN, ON, or SN bond,
C3-10 carbocyclic residue substituted with 0-2 R4a, and
5-10 membered heterocyclic system containing from 1-4 heteroatoms selected from the group consisting of N, O, and S substituted with 0-2 R4a;
provided that B and Y are other than tetrazolyl;
Z is selected from H, S(O)2NHR3, C(O)R3, C(O)NHR3, C(O)OR3f, S(O)R3f, S(O)2R3f,
C1-6 alkyl substituted with 0-2 R1a;
C2-6 alkenyl substituted with 0-2 R1a;
C2-6 alkynyl substituted with 0-2 R1a;
cycloalkyl(C0-4 alkyl)-substituted with 0-3 R1a;
heterocyclyl(C0-4 alkyl)-substituted with 0-3 R1a;
aryl(C0-4 alkyl)-substituted with 0-3 R1a;
heteroaryl(C0-4 alkyl)-substituted with 0-3 R1a;
R1a, is selected from H, (CH2)rR1b, CHCHR1b, NCH2R1c, OCH2R1c, S(O)pCH2R1c, NH(CH2)2(CH2)tR1b, O(CH2)2(CH2)tR1b, and S(CH2)2(CH2)tR1b, provided that R1a forms other than an N-halo, NN, NS, NO, or NCN bond with the group to which it is attached;
alternatively, when two R1as are attached to adjacent atoms, together with the atoms to which they are attached they form a 5-7 membered ring consisting of: carbon atoms and 0-2 heteroatoms selected from the group consisting of N, O, and S(O)p, this ring being substituted with 0-2 R4b and 0-1 Z, comprising: 0-3 double bonds;
R1b is selected from H, C1-3 alkyl, F, Cl, Br, I, CN, CHO, (CF2)rCF3, (CH2)rOR2, NR2R2a, C(O)R2c, C(O)OR2, OC(O) R2, (CF2)rCO2R2a, S (O)pR2b, NR2 (CH2)rOR2, C(NR2c)NR2R2a, NR2C(O)R2b, NR2C(O)NHR2b, NR2C(O)2R2a, OC(O)NR2aR2b, C(O)NR2R2a, C(O)NR2(CH2)rOR2, SO2NR2R2a, NR2SO2R2b, C3-10 carbocycle substituted with 0-2 R4a, and 5-10 membered heterocycle consisting of carbon atoms and from 1-4 heteroatoms selected from the group consisting of N, O, and S(O)p substituted with 0-2 R4a, provided that R1b forms other than an N-halo, NN, NS, NO, or NCN bond with the group to which it is attached;
R1c is selected from H, CH(CH2OR2)2, C(O)R2c, C(O)NR2R2a, S(O)R2b, S(O)2R2b, and SO2NR2R2a;
R2, at each occurrence, is selected from H, CF3, C1-6 alkyl optionally substituted with 0-2 R2b, benzyl, a C3-10 carbocyclic-(CH2)r residue substituted with 0-2 R4b, and (5-6 membered heterocyclic system)-(CH2)r containing from 1-4 heteroatoms selected from the group consisting of N, O, and S substituted with 0-2 R4b;
R2a, at each occurrence, is selected from H, CF3, C1-6 alkyl optionally substituted with 0-2 R4b, benzyl, a C3-10 carbocyclic-(CH2)r residue substituted with 0-2 R4b, and (5-6 membered heterocyclic system)-(CH2)r containing from 1-4 heteroatoms selected from the group consisting of N, O, and S substituted with 0-2 R4b;
alternatively, R2 and R2a, together with the atom to which they are attached, combine to form a 5 or 6 membered saturated, partially saturated or unsaturated ring substituted with 0-2 R4b and containing from 0-1 additional heteroatoms selected from the group consisting of N, O, and S;
R2b, at each occurrence, is selected from CF3, C1-4 alkoxy, C1-6 alkyl, benzyl, C3-10 carbocyclic-(CH2)r residue substituted with 0-2 R4b, and (5-6 membered heterocyclic system)-(CH2)r containing from 1-4 heteroatoms selected from the group consisting of N, O, and S substituted with 0-2 R4b;
R2c, at each occurrence, is selected from CF3, OH, C1-4 alkoxy, C1-6 alkyl, benzyl, C3-10 carbocyclic-(CH2)r residue substituted with 0-2 R4b, and (5-6 membered heterocyclic system)-(CH2)r containing from 1-4 heteroatoms selected from the group consisting of N, O, and S substituted with 0-2 R4b;
R3, at each occurrence, is selected from H,
C1-6 alkyl substituted with 0-2 R1a;
C2-6 alkenyl substituted with 0-2 R1a;
C2-6 alkynyl substituted with 0-2 R1a;
cycloalkyl(C0-4 alkyl)-substituted with 0-3 R1a;
heterocyclyl(C0-4 alkyl)-substituted with 0-3 R1a;
aryl(C0-4 alkyl)-substituted with 0-3 R1a;
heteroaryl(C0-4 alkyl)-substituted with 0-3 R1a;
R3a and R3b, at each occurrence, are independently selected from H, C1-4 alkyl, phenyl, and benzyl;
R3c, at each occurrence, is selected from C1-4 alkyl, phenyl, and benzyl;
R3d, at each occurrence, is selected from H and C1-4 alkyl;
R3e, is selected from H, S(O)2NHR3, C(O)R3, C(O)NHR3, C(O)OR3f, S(O)R3f, S(O)2R3f,
C1-6 alkyl substituted with 0-2 R1a;
C2-6 alkenyl substituted with 0-2 R1a;
C2-6 alkynyl substituted with 0-2 R1a;
cycloalkyl(C0-4 alkyl)-substituted with 0-3 R1a;
heterocyclyl(C0-4 alkyl)-substituted with 0-3 R1a;
aryl (C0-4 alkyl)-substituted with 0-3 R1a;
heteroaryl(C0-4 alkyl)-substituted with 0-3 R1a;
R3f, at each occurrence, is selected from:
C1-6 alkyl substituted with 0-2 R1a;
C2-6 alkenyl substituted with 0-2 R1a;
C2-6 alkynyl substituted with 0-2 R1a;
cycloalkyl(C0-4 alkyl)-substituted with 0-3 R1a;
heterocyclyl(C0-4 alkyl)-substituted with 0-3 R1a;
aryl(C0-4 alkyl)-substituted with 0-3 R1a;
heteroaryl(C0-4 alkyl)-substituted with 0-3 R1a;
R4, at each occurrence, is selected from H, O, (CH2)rOR2, F, Cl, Br, I, C1-4 alkyl, CN, NO2, (CH2)rNR2R2a, (CH2)rC(O)R2C, NR2C(O)R2b, C(O)NR2R2a, NR2C(O)NR2R2a, C(NR2)NR2R2a, C(NS(O)2R3f)NR2R2a, NHC(NR2)NR2R2a, C(O)NHC(NR2)NR2R2a, SO2NR2R2a, NR2SO2NR2R2a, NR2SO2C1-4 alkyl, NR2SO2R3f, S(O)pR3f, (CF2)rCF3, NCH2R1c, OCH2R1c, SCH2R1c, N(CH2)2(CH2)tR1b, O(CH2)2(CH2)tR1b, S(CH2)2(CH2)tR1b, and 5-6 membered carbocycle substituted with 0-1 R5, and a 5-6 membered heterocycle consisting of: carbon atoms and 1-4 heteroatoms selected from the group consisting of N, O, and S(O)p substituted with 0-1 R5;
R4a, at each occurrence, is selected from H, O, (CH2)rOR2, (CH2)rF, (CH2)rBr, (CH2)rCl, C1-4 alkyl, CN, NO2, (CH2)rNR2R2a, (CH2)rC(O)R2C, NR2C(O)R2b, C(O)NR2R2a, (CH2)rNCHOR3, C(O)NH(CH2)2NR2R2a, NR2C(O)NR2R2a, C(NR2)NR2R2a, NHC(NR2)NR2R2a, SO2NR2R2a, NR2SO2NR2R2a, NR2SO2C1-4 alkyl, C(O)NHSO2C1-4 alkyl, NR2SO2R3f, S(O)pR3f, (CF2)rCF3, and 5-6 membered carbocycle substituted with 0-1 R5, and a 5-6 membered heterocycle consisting of: carbon atoms and 1-4 heteroatoms selected from the group consisting of N, O, and S(O)p substituted with 0-1 R5;
R2b, at each occurrence, is selected from H, O, (CH2)rOR3, (CH2)rF, (CH2)rCl, (CH2)rBr, (CH2)rI, C1-4 alkyl, (CH2)rCN, (CH2)rNO2, (CH2)rNR3R3a, (CH2)rC(O)R3, (CH2)rC(O)OR3c, (CH2)rNR3C(O)R3a, (CH2)rC(O)NR3R3a, (CH2)rNR3C(O)NR3R3a, (CH2)rC(NR3)NR3R3a, (CH2)rNR3C(NR3)NR3R3a, (CH2)rSO2NR3R3a, (CH2)rNR3SO2NR3R3a, (CH2)rNR3SO2-C1-4 alkyl, (CH2)rNR3SO2CF3, (CH2)rNR3SO2-phenyl, (CH2)rS(O)pCF3, (CH2)rS(O)pC1-4 alkyl, (CH2)rS(O)p-phenyl, and (CF2)rCF3;
R5, at each occurrence, is selected from H, C1-6 alkyl, O, (CH2)rOR3, F, Cl, Br, I, CN, NO2, (CH2)rNR3R3a, (CH2)rC(O)R3, (CH2)rC(O)OR3c, NR3C(O)R3a, C(O)NR3R3a, NR3C(O)NR3R3a, CH(NOR3d), C(NR3)NR3R3a, NR3C(NR3)NR3R3a, SO2NR3R3a, NR3SO2NR3R3a, NR3SO2C1-4 alkyl, NR3SO2CF3, NR3SO2-phenyl, S(O)pCF3, S(O)pC1-4 alkyl, S(O)p-phenyl, (CF2)rCF3, phenyl substituted with 0-2 R6, naphthyl substituted with 0-2 R6, and benzyl substituted with 0-2 R6;
R6, at each occurrence, is selected from H, OH, (CH2)rOR2, halo, C1-4 alkyl, CN, NO2, (CH2)rNR2R2a, (CH2)rC(O)R2b, NR2C(O)R2b, NR2C(O)NR2R2a, C(NH)NH2, NHC(NH)NH2, SO2NR2R2a, NR2SO2NR2R2a, and NR2SO2C1-4 alkyl;
R7, at each occurrence, is selected from H, OH, C1-6 alkyl, C1-6 alkylcarbonyl, C1-6 alkoxy, C1-4 alkoxycarbonyl, (CH2)n-phenyl, C6-10 aryloxy, C6-10 aryloxycarbonyl, C6-10 arylmethylcarbonyl, C1-4 alkylcarbonyloxy C1-4 alkoxycarbonyl, C6-10 arylcarbonyloxy C1-4 alkoxycarbonyl, C1-6 alkylaminocarbonyl, phenylaminocarbonyl, and phenyl C1-4 alkoxycarbonyl;
R8, at each occurrence, is selected from H, C1-6 alkyl and (CH2)n-phenyl;
alternatively, R7 and R8 combine to form a 5-10 membered saturated, partially saturated or unsaturated ring which contains 0-2 additional heteroatoms selected from the group consisting of N, O, and S;
R9, at each occurrence, is selected from H, C1-6 alkyl and (CH2)n-phenyl;
n, at each occurrence, is selected from 0, 1, 2, and 3;
p, at each occurrence, is selected from 0, 1, and 2;
r, at each occurrence, is selected from 0, 1, 2, and 3; and
t, at each occurrence, is selected from 0, 1, 2, and 3;
provided that when ring M is piperidin-2,6-dione and A is phenyl, then:
(i) one of Ra and Rb is other than halo, alkyl, alkoxy, and CF3;
(ii) B is phenyl and R4a is other than alkyl;
(iii) B is pyridyl or imidazolyl; or
(iv) X is present and is C(O);
provided that when ring M is oxazolidinone and G1 is CONHCH2, then G is other than thienyl or benzothienyl.
2. A compound according to claim 1, wherein the compound is selected from the group:
104
wherein the above formulas are substituted with 0-2 R1a and a is a single or double bond;
A is selected from one of the following carbocyclic and heterocyclic systems which are substituted with 0-2 R4;
phenyl, piperidinyl, piperazinyl, pyridyl, pyrimidyl, furanyl, morpholinyl, thienyl, pyrrolyl, pyrrolidinyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, pyrazolyl, imidazolyl, oxadiazolyl, thiadiazolyl, triazolyl, 1,2,3-oxadiazolyl, 1,2,4-oxadiazolyl, 1,2,5-oxadiazolyl, 1,3,4-oxadiazolyl, 1,2,3-thiadiazolyl, 1,2,4-thiadiazolyl, 1,2,5-thiadiazolyl, 1,3,4-thiadiazolyl, 1,2,3-triazolyl, 1,2,4-triazolyl, 1,2,5-triazolyl, 1,3,4-triazolyl, benzofuranyl, benzothiofuranyl, indolyl, benzimidazolyl, benzoxazolyl, benzthiazolyl, indazolyl, benzisoxazolyl, benzisothiazolyl, and isoindazolyl;
B is selected from: Y and XY;
X is selected from (CR2R2a)1-4, C(O), C(NR1c), CR2(NR1cR2), C(O)CR2R2a, CR2R2aC(O), C(O)NR2, NR2C(O), C(O)NR2CR2R2a, NR2C(O)CR2R2a, CR2R2aC(O)NR2, CR2R2aNR2C(O), NR2C(O)NR2, NR2, NR2CR2R2a, CR2R2aNR2, O, CR2R2aO, and OCR2R2a;
Y is (CH2)rNR2R2a, provided that XY do not form a NN or ON bond;
alternatively, Y is selected from one of the following carbocyclic and heterocyclic systems which are substituted with 0-2 R4a;
cyclopropyl, cyclopentyl, cyclohexyl, phenyl, piperidinyl, piperazinyl, pyridyl, pyrimidyl, furanyl, morpholinyl, thienyl, pyrrolyl, pyrrolidinyl, oxazolyl, isoxazolyl, isoxazolinyl, thiazolyl, isothiazolyl, pyrazolyl, imidazolyl, oxadiazolyl, thiadiazolyl, triazolyl, 1,2,3-oxadiazolyl, 1,2,4-oxadiazolyl, 1,2,5-oxadiazolyl, 1,3,4-oxadiazolyl, 1,2,3-thiadiazolyl, 1,2,4-thiadiazolyl, 1,2,5-thiadiazolyl, 1,3,4-thiadiazolyl, 1,2,3-triazolyl, 1,2,4-triazolyl, 1,2,5-triazolyl, 1,3,4-triazolyl, benzofuranyl, benzothiofuranyl, indolyl, benzimidazolyl, benzoxazolyl, benzthiazolyl, indazolyl, benzisoxazolyl, benzisothiazolyl, and isoindazolyl; and
alternatively, Y is selected from the following bicyclic heteroaryl ring systems:
105
K is selected from O, S, NH, and N.
3. A compound according to claim 2, wherein the compound is selected from the group:
106
wherein compounds of the above formulas are substituted with 0-2 R1a; and
G is selected from the group:
107
4. A compound according to claim 3, wherein the compound is selected from the group:
108
wherein compounds of the above formulas are substituted with 0-2 R1a;
G is selected from:
109
G1 is selected from (CR3aR3b)1-2, CR3CR3, CC, (CHR3a)uC(O)(CHR3a), (CHR3a)uC(O)O(CHR3a)w, (CHR3a)uO(CHR3a)w, (CHR3a)uNR3e(CHR3a)w, (CHR3a)uC(O)NR3(CHR3a)w, (CHR3a) NR3C(O)(CHR3a)w, (CHR3a)uS(O)2(CHR3a)w, (CHR3a)uNR3S(O)2(CHR3a)w, and (CHR3a)uS(O)2NR3(CHR3a)w, wherein uw total 0, 1, or 2, provided that G1 does not form a NN or NO bond with either group to which it is attached;
R3, at each occurrence, is selected from H, C1-4 alkyl substituted with 0-2 R1a;
C2-4 alkenyl substituted with 0-2 R1a;
C2-4 alkynyl substituted with 0-2 R1a;
C3-7 cycloalkyl(C0-2 alkyl)-substituted with 0-3 R1a;
heterocyclyl(C0-2 alkyl)-substituted with 0-3 R1a;
aryl(C0-2 alkyl)-substituted with 0-3 R1a;
heteroaryl(C0-2 alkyl)-substituted with 0-3 R1a;
R3a, at each occurrence, is selected from H, C1-4 alkyl, and benzyl; and
R3b, at each occurrence, is selected from H, C1-4 alkyl, and benzyl.
5. A compound according to claim 4, wherein:
G is selected from:
110
A is selected from phenyl, piperidinyl, pyridyl, and pyrimidyl, and is substituted with 0-2 R4; and,
B is selected from phenyl, pyrrolidino, N-pyrrolidino-carbonyl, morpholino, N-morpholino-carbonyl, 1,2,3-triazolyl, imidazolyl, and benzimidazolyl, and is substituted with 0-1 R4a;
R2, at each occurrence, is selected from H, CH3, CH2CH3, cyclopropylmethyl, cyclobutyl, and cyclopentyl;
R2a, at each occurrence, is H or CH3, and CH2CH3;
alternatively, R2 and R2a, together with the atom to which they are attached, combine to form pyrrolidine substituted with 0-2 R4b or piperidine substituted with 0-2 R4b;
R4, at each occurrence, is selected from H, OH, OR2, (CH2)OR2, (CH2)2OR2, F, Br, Cl, I, C1-4 alkyl, NR2R2a, (CH2)NR2R2a, (CH2)2NR2R2a, CF3, and (CF2)CF3;
R4a is selected from H, C1-4 alkyl, CF3, OR2, (CH2)OR2, (CH2)2OR2, NR2R2a, (CH2)NR2R2a, (CH2)2NR2R2a, SR5, S(O)R5, S(O)2R5, SO2NR2R2a, and 1-CF3-tetrazol-2-yl;
R2b, at each occurrence, is selected from H, CH3, and OH;
R5, at each occurrence, is selected from CF3, C1-6 alkyl, phenyl, and benzyl; and,
r, at each occurrence, is selected from 0, 1, and 2.
6. A compound according to claim 5, wherein:
A is selected from the group: phenyl, piperidinyl, 2-pyridyl, 3-pyridyl, 2-pyrimidyl, 2-Cl-phenyl, 3-Cl-phenyl, 2-F-phenyl, 3-F-phenyl, 2-methylphenyl, 2-aminophenyl, and 2-methoxyphenyl; and,
B is selected from the group: 2-(aminosulfonyl)phenyl, 2-(methylaminosulfonyl)phenyl, 1-pyrrolidinocarbonyl, 2-(methylsulfonyl)phenyl, 2-(N,N-dimethylaminomethyl)phenyl, 2-(N,N-diethylaminomethyl)phenyl, 2-(N-methylaminomethyl)phenyl, 2-(N-ethyl-N-methylaminomethyl)phenyl, 2-(N-pyrrolidinylmethyl)phenyl, 1-methyl-2-imidazolyl, 2-methyl-1-imidazolyl, 2-(dimethylaminomethyl)-1-imidazolyl, 2-(methylaminomethyl)-1-imidazolyl, 2-(N-(cyclopropylmethyl)aminomethyl)phenyl, 2-(N-(cyclobutyl)aminomethyl)phenyl, 2-(N-(cyclopentyl)aminomethyl)phenyl, 2-(N-(4-hydroxypiperidinyl)methyl)phenyl, 2-(N-(3-hydroxypyrrolidinyl)methyl)phenyl, and 2-(N-(2-hydroxyethyl)methylamino)-methyl)phenyl.
7. A compound according to claim 1, wherein the compound is selected from the group:
3-(1-3-fluoro-2-(methylsulfonyl)-1,1-biphenyl-4-yl-2-oxo-3-piperidinyloxy)benzonitrile;
3-(1-3-fluoro-2-(methylsulfonyl)-1,1-biphenyl-4-yl-2-oxo-3-piperidinyloxy)benzene-carboximidamide;
4-(1-3-fluoro-2-(methylsulfonyl)-1,1-biphenyl-4-yl-2-oxo-3-piperidinyloxy)benzene-carboximidamide;
3-(1-2-(dimethylamino)methyl-3-fluoro-1,1-biphenyl-4-yl-2-oxo-3-piperidinyloxy)benzonitrile;
3-(1-2-(dimethylamino)methyl-3-fluoro-1,1-biphenyl-4-yl-2-oxo-3-piperidinyloxy)benzene-carboximidamide;
3-(1-2-(dimethylamino)methyl-1,1-biphenyl-4-yl-2-oxo-3-piperidinyloxy)benzene-carboximidamide;
3-(1-2-(dimethylamino)methyl-3-fluoro-1,1-biphenyl-4-yl-2-oxo-3-piperidinylamino)benzene-carboximidamide;
2,4-dichloro-N-1-3-fluoro-2-(methylsulfonyl)-1,1-biphenyl-4-yl-2-oxo-3-piperidinylbenzamide;
3-chloro-N-1-3-fluoro-2-(methylsulfonyl)-1,1-biphenyl-4-yl-2-oxo-3-piperidinyl-N-methyl-benzamide;
3,4-dichloro-N-1-3-fluoro-2-(methylsulfonyl)-1,1-biphenyl-4-yl-2-oxo-3-piperidinyl-benzamide;
4-fluoro-N-1-3-fluoro-2-(methylsulfonyl)-1,1-biphenyl-4-yl-2-oxo-3-piperidinyl-benzamide;
4-chloro-N-1-3-fluoro-2-(methylsulfonyl)-1,1-biphenyl-4-yl-2-oxo-3-piperidinyl-benzamide;
2-chloro-N-1-3-fluoro-2-(methylsulfonyl)-1,1-biphenyl-4-yl-2-oxo-3-piperidinyl-isonicotinamide;
6-chloro-N-1-3-fluoro-2-(methylsulfonyl)-1,1-biphenyl-4-yl-2-oxo-3-piperidinyl-nicotinamide;
N-1-3-fluoro-2-(methylsulfonyl)-1,1-biphenyl-4-yl-2-oxo-3-piperidinyl-6-(1H-pyrazol-1-yl)nicotinamide;
1-3-fluoro-2-(methylsulfonyl)-1,1-biphenyl-4-yl-2-oxo-3-piperidinyl-2-chloronicotinate;
1-3-fluoro-2-(methylsulfonyl)-1,1-biphenyl-4-yl-2-oxo-3-piperidinyl4-methoxybenzoate;
2-(1-3-fluoro-2-(methylsulfonyl)-1,1-biphenyl-4-yl-2-oxo-3-piperidinyloxy)-5-methoxybenzaldehyde;
3-5-chloro-2-pyridynyl)amino-1-3-fluoro-2-(methylsulfonyl)-1,1-biphenyl-4-yl-2-piperidinone;
1-3-fluoro-2-(methylsulfonyl)-1,1-biphenyl-4-yl-3(4-methoxyphenoxy)-2-piperidinone;
2-(1-3-fluoro-2-(methylsulfonyl)-1,1-biphenyl-4-yl-2-oxo-3-piperidinyloxy)-5-methoxybenzoate;
3-3-(aminomethyl)phenoxy-1-3-fluoro-2-(methylsulfonyl)-1,1-biphenyl-4-yl-2-piperidinone;
3-2-(anilinomethyl)-4-methoxyphenyloxo-1-3-fluoro-2-(methylsulfonyl)-1,1-biphenyl-4-yl-2-piperidinone;
3-chloro-N-1-3-fluoro-2-(methylsulfonyl)-1,1-biphenyl-4-yl-2-oxo-3-piperidinyl-benzamide;
N-benzyl-4-chloro-N-1-3-fluoro-2-(methylsulfonyl)-1,1-biphenyl-4-yl-2-oxo-3-piperidinyl-benzamide;
N-1-3-fluoro-2-(methylthio)-1,1-biphenyl-4-yl-2-oxo-3-piperidinyl-1H-indole-5-carboxamide;
N-1-3-fluoro-2-(methylthio)-1,1-biphenyl-4-yl-2-oxo-3-piperidinyl-1H-pyrazole-4-carboxamide;
N-1-3-fluoro-2-(methylthio)-1,1-biphenyl-4-yl-2-oxo-3-piperidinyl-isonicotinamide;
N-1-3-fluoro-2-(methylthio)-1,1-biphenyl-4-yl-2-oxo-3-piperidinyl-nicotinamide;
6-amino-N-1-3-fluoro-2-(methylthio)-1,1-biphenyl-4-yl-2-oxo-3-piperidinyl-nicotinamide;
6-amino-N-1-3-fluoro-2-(methylthio)-1,1-biphenyl-4-yl-2-oxo-3-piperidinyl-nicotinamide;
3-1-2-aminosulfonyl-1,1-biphenyl-4-yl-2-oxo-3-piperidinyl(benzyl)aminosulfonyl-benzenecarboximidamide;
3-1-(3-fluoro-2-aminosulfonyl)-1,1-biphenyl-4-yl-2-oxo-3-piperidinyl(benzyl)aminosulfonylbenzenecarboximidamide;
3-N-benzyl-N-2-oxo-1-(2-sulfamoyl-biphenyl-4-yl)-piperidin-3-yl-sulfamoyl-benzamidine;
4-chloro-N-1-3-fluoro-1-(2-methylsulfonyl-biphenyl-4-yl)-2-oxo-piperidin-3-yl-benzenesulfonamide;
6-chloro-N-1-(3-fluoro-2-methylsulfonyl-biphenyl-4-yl)-2-oxo-piperidin-3-yl-naphthalene-2-sulfonamide;
7-chloro-N-1-(3-fluoro-2-methylsulfonyl-biphenyl-4-yl)-2-oxo-piperidin-3-yl-naphthalene-2-sulfonamide;
5-chloro-N-1-(3-fluoro-2-methylsulfonyl-biphenyl-4-yl)-2-oxo-piperidin-3-yl-thiophene-2-sulfonamide;
5-(3-isoxazolyl)-1-3-fluoro-(2-methylsulfonyl-biphenyl-4-yl)-2-oxo-piperidin-3-yl-thiophene-2-sulfonamide;
4-fluoro-N-1-(3-fluoro-1-2-methylsulfonyl-biphenyl-4-yl)-2-oxo-piperidin-3-yl-benzenesulfonamide;
N-1-(3-fluoro-1-2-methylsulfonyl-biphenyl-4-yl)-2-oxo-piperidin-3-yl-4-methoxyl-benzenesulfonamide;
4-ethyl-N-1-(3-fluoro-1-2-methylsulfonyl-biphenyl-4-yl)-2-oxo-piperidin-3-yl-benzenesulfonamide;
N-3-fluoro-1-(2-methylsulfonyl-biphenyl-4-yl)-2-oxo-piperidin-3-yl-3-methoxyl-benzenesulfonamide;
5-bromo-6-chloro-3-fluoro-1-(2-methanesulfonyl-biphenyl-4-yl)-2-oxo-piperidin-3-yl-pyridine-3-sulfonamide;
5-(2-pyridyl)-3-fluoro-1-(2-methanesulfonyl-biphenyl-4-yl)-2-oxo-piperidin-3-yl-thiophene-2-sulfonamide;
3,4-difluoro-N-3-fluoro-1-(2-methylsulfonyl-biphenyl-4-yl)-2-oxo-piperidin-3-yl-benzenesulfonamide;
3-chloro-N-3-fluoro-1-(2-methylsulfonyl-biphenyl-4-yl)-2-oxo-piperidin-3-yl-benzenesulfonamide;
3,5-dichloro-3-fluoro-1-(2-methanesulfonyl-biphenyl-4-yl)-2-oxo-piperidin-3-yl-thiophene-2-sulfonamide;
3-cyano-N-3-fluoro-1-(2-methanesulfonyl-biphenyl-4-yl)-2-oxo-piperidin-3-yl-benzenesulfonamide;
3-chloro-4-fluoro-N-3-fluoro-1-(2-methanesulfonyl-biphenyl-4-yl)-2-oxo-piperidin-3-yl-benzenesulfonamide
1-methyl-3-fluoro-1-(2-methanesulfonyl-biphenyl-4-yl)-2-oxo-piperidin-3-yl-imidazole-4-sulfonamide;
2,5-dichloro-N-3-fluoro-1-(2 -methylsulfonyl-biphenyl-4-yl)-2-oxo-piperidin-3-yl-benzenesulfonamide;
3,5-dichloro-N-3-fluoro-1-(2-methylsulfonyl-biphenyl-4-yl)-2-oxo-piperidin-3-yl-benzenesulfonamide;
5-chloro-N-1-(2-diethylaminomethyl-3-fluoro-biphenyl-4-yl)-2-oxo-piperidin-3-yl-thiophene-2-sulfonamide;
5-chloro-N-1-(3-fluoro-1-2-pyrrolidin-1-ylmethyl-biphenyl-4-yl)-2-oxo-piperidin-3-yl-thiophene-2-sulfonamide;
5-chloro-N-1-(3-fluoro-1-2-(3-hydroxypyrrolidin-1-ylmethyl)-biphenyl -4-yl-2-oxo-piperidin-3-yl-thiophene-2-sulfonamide;
5-chloro-N-1-3-fluoro-1-2-(4-hydroxypiperidin-1-ylmethyl)-biphenyl-4-yl-2-oxo-piperidin-3-yl-thiophene-2-sulfonamide;
N-benzyl-5-chloro-N-1-(2-diethylaminomethyl-3-fluoro-biphenyl-4-yl)-2-oxo-piperidin-3-yl-thiophene-2-sulfonamide;
N-benzyl-5-chloro-N-1-(3-fluoro-1-2-pyrrolidin-1-ylmethyl-biphenyl-4-yl)-2-oxo-piperidin-3-yl-thiophene-2-sulfonamide;
N-benzyl-5-chloro-N-1-3-fluoro-1-2-(3-hydroxypyrrolidin-1-ylmethyl)-biphenyl-4-yl-2-oxo-piperidin-3-yl-thiophene-2-sulfonamide;
N-benzyl-5-chloro-N-1-3-fluoro-1-2-(4-hydroxypiperidin-1-ylmethyl)-biphenyl-4-yl-2-oxo-piperidin-3-yl-thiophene-2-sulfonamide;
5-chloro-3-fluoro-1-(2-(2-hydroxy-ethyl)-methyl-amino-methyl-biphenyl-4-yl)-2-oxo-piperidin-3-yl-thiophene-2-sulfonamide;
3-amino-N-1-(3-fluoro-2-methanesulfonyl-biphenyl-4-yl)-2-oxo-piperidin-3-yl-benzodisoxazole-5-sulfonamide;
3-(3-amino-benzodisoxazol-5-ylamino)-1-(3-fluoro-2-methanesulfonyl-biphenyl-4-yl)-piperidin-2-one;
2-fluoro-5-1-(3-fluoro-2-methanesulfonyl-biphenyl-4-yl)-2-oxo-piperidin-3-ylamino-N-hydroxy-benzamidine;
1-(3-fluoro-2-methanesulfonyl-biphenyl-4-yl)-3-3-(5-oxo-4,5-dihydro-1H-1,2,4triazol-3-yl)-phenylamino-piperidin-2-one;
N-benzyl-4-chloro-N-1-(2-methanesulfonyl-biphenyl-4-yl)-2-oxo-piperidin-3-yl-benzenesulfonamide;
4-chloro-N-methyl-N-1-(2-methanesulfonyl-biphenyl-4-yl)-2-oxo-piperidin-3-yl-benzenesulfonamide;
4-chloro-N-ethyl-N-1-(2-methanesulfonyl-biphenyl-4-yl)-2-oxo-piperidin-3-yl-benzenesulfonamide;
4-chloro-N-1-(3-fluoro-2-methanesulfonyl-biphenyl-4-yl)-2-oxo-piperidin-3-yl-N-(3-pyridylmethyl)-benzenesulfonamide;
4-chloro-N-1-(3-fluoro-2-methanesulfonyl-biphenyl-4-yl)-2-oxo-piperidin-3-yl-N-(2-pyridylmethyl)-benzenesulfonamide;
3-1,2-dihydro-1-2-(methylsulfonyl)1,1-biphenyl-4-yl-2-oxo-3-pyridinylamino-benzenecarboximidamide;
3-(4-methoxyphenyl)amino-1-2-(methylsulfonyl)1,1-biphenyl-4-yl-2(1H)-pyridinone;
N-1,2-dihydro-1-2-(methylsulfonyl)1,1-biphenyl-4-yl-2-oxo-3-pyridinyl-4-methoxy-benzamide;
6-chloro-N-1,2-dihydro-1-2-(methylsulfonyl)1,1-biphenyl-4-yl-2-oxo-3-pyridinyl-3-pyridinecarboxamide;
3-1,2-dihydro-1-2-(3-hydroxy-1-pyrrolidinyl)methyl1,1-biphenyl-4-yl-2-oxo-4-(1-pyrrolidinyl)-3-pyridinylamino-benzenecarboximidamide;
3-1,2-dihydro-1-2-(3-hydroxy-1-pyrrolidinyl)methyl1,1-biphenyl-4-yl-2-oxo-4-(1-pyrrolidinyl)-3-pyridinylamino-benzamide;
3-3-(2-methanesulfonyl-biphenyl-4-yl)-2-oxo-tetrahydro-pyrimidin-1-ylmethyl-benzamidine;
4-benzyloxycarbonyl-3-(4-chlorobenzenesulfonylamino)-1-(2-methanesulfonyl-biphenyl-4-yl)-2-oxo-piperazine;
4-benzyloxycarbonyl-3-(4-methoxybenzenesulfonylamino)-1-(2-methanesulfonyl-biphenyl-4-yl)-2-oxo-piperazine;
5-chloro-2-(3-fluoro-2-methanesulfonyl-biphenyl-4-yl)-3-oxo-1,2,3,4-tetrahydroisoquinolin-4-yl-thiophene-2-sulfonamide;
3-1-(2-dimethylaminomethyl-biphenyl-4-yl)-2-oxo-azepan-3-ylamino-benzamidine;
N-3-benzyl-1-(2-methanesulfonyl-biphenyl-4-yl)-2-oxo-piperidin-3-yl-4-chlorobenzamide;
3-(6-chloro-naphthalene-2-sulfonylamino)-1(2-methanesulfonyl-biphenyl-4-yl)-2-oxo-piperidin-3-yl-acetic acid methyl ester;
N-1-(3-fluoro-2-methanesulfonyl-biphenyl-4-yl)-2-oxo-piperidin-3-yl-3-(5-oxo-4,5-dihydro-1H-1,2,4triazol-3-yl)-benzenesulfonamide;
1-(3-fluoro-2-methanesulfonyl-biphenyl-4-yl)-3-3-(5-oxo-4,5-dihydro-1H-1,2,4triazol-3-yl)-phenoxy-piperidin-2-one;
1-(3-fluoro-2-methanesulfonyl-biphenyl-4-yl)-2-oxo-piperidin-3-yl-benzenesulfonamide;
1-(3-fluoro-2-methanesulfonyl-biphenyl-4-yl)-2-oxo-piperidin-3-yl-pyridin-3-yl-sulfonamide;
5-chloro-3-methyl-N-1-3-fluoro-1-2-(4-hydroxypiperidin-1-ylmethyl)-biphenyl-4-yl-2-oxo-piperidin-3-yl-thiophene-2-sulfonamide;
1-(3-fluoro-2-methanesulfonyl-biphenyl-4-yl)-2-oxo-piperidin-3-yl-quinolin-3-yl-sulfonamide;
1-(3-fluoro-2-methanesulfonyl-biphenyl-4-yl)-2-oxo-piperidin-3-yl-quinolin-6-yl-sulfonamide;
1-(3-fluoro-2-methanesulfonyl-biphenyl-4-yl)-2-oxo-piperidin-3-yl-quinoxalin-6-yl-sulfonamide;
1-(3-fluoro-2-methanesulfonyl-biphenyl-4-yl)-2-oxo-piperidin-3-yl-(6-amino-pyridin-3-yl)-sulfonamide;
1-(3-fluoro-2-methanesulfonyl-biphenyl-4-yl)-2-oxo-piperidin-3-yl-indazol-6-yl-sulfonamide;
6-chloronaphthalene-2-sulfonic acid 1-benzyl-4-(2-dimethylaminomethylbiphenyl-4-yl)-5-oxo-1,4-diazepan-6-ylamide;
5-chloro-N-1-2-(methylsulfonyl)-1,1-biphenyl-4-yl-2-oxo-2,3,4,5-tetrahydro-1H-1-benzazepin-3-yl-2-thiophenesulfonamide;
(6-chloro-naphthalene-2-sulfonyl)-1-(3-fluoro-2-methanesulfonyl-biphenyl-4-yl)-2-oxo-piperidin-3-yl-amino-acetic acid methyl ester;
(6-chloro-naphthalene-2-sulfonyl)-1-(3-fluoro-2-methanesulfonyl-biphenyl-4-yl)-2-oxo-piperidin-3-yl-amino-acetic acid ethyl ester;
(6-chloro-naphthalene-2-sulfonyl)-1-(3-fluoro-2-methanesulfonyl-biphenyl-4-yl)-2-oxo-piperidin-3-yl-amino-acetic acid t-butyl ester;
6-chloro-naphthalene-2-sulfonic acid benzoyl-1-(3-fluoro-2-methanesulfonyl-biphenyl-4-yl)-2-oxo-piperidin-3-yl-amide;
(6-chloro-naphthalene-2-sulfonyl)-1-(3-fluoro-2-methanesulfonylbiphenyl-4-yl)-2-oxo-piperidin-3-ylaminoacetic acid;
2-(6-chloronaphthalene-2-sulfonyl)-1-(3-fluoro-2-methanesulfonylbiphenyl-4-yl)-2-oxo-piperidin-3-yl-amino-N-(2-dimethylaminoethyl)-N-methylacetamide;
2-(6-Chloro-naphthalene-2-sulfonyl)-1-(3-fluoro-2-methanesulfonyl-biphenyl-4-yl)-2-oxo-piperidin-3-yl-amino-N-(2-hydroxy-ethyl)-acetamide; and
2-(6-Chloro-naphthalene-2-sulfonyl)-1-(3-fluoro-2-methanesulfonyl-biphenyl-4-yl)-2-oxo-piperidin-3-yl-amino-N-(2-dimethylamino-ethyl)-acetamide;
or a pharmaceutically acceptable salt form thereof.
8. A pharmaceutical composition, comprising: a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound of claim 1 or a pharmaceutically acceptable salt form thereof.
9. A method for treating a thromboembolic disorder, comprising: administering to a patient in need thereof a therapeutically effective amount of a compound of claim 1 or a pharmaceutically acceptable salt form thereof.
10. A method of treating a patient in need of thromboembolic disorder treatment, comprising: administering a compound of claim 1 or a pharmaceutically acceptable salt form thereof in an amount effective to treat a thromboembolic disorder
11. A method, comprising: administering a compound of claim 1 or a pharmaceutically acceptable salt form thereof in an amount effective to treat a thromboembolic disorder.
12. A compound of claim 1 for use in therapy.
13. Use of a compound of claim 1 for the manufacture of a medicament for the treatment of a thromboembolic disorder.