Author: claimsbot

1. An overvoltage protection device comprising:
a doped substrate of a first conductivity type having a first doping level, coated with a doped epitaxial layer of the second conductivity type having a second doping level;
a first doped buried region of the second conductivity type having a third doping level greater than the second level, located at the interface between the substrate and the epitaxial layer in a first portion of the device, wherein the junction between the substrate and the first buried region forms a first diode having its conduction area of the second conductivity type coupled to a first terminal of the device via the epitaxial layer; and
a second doped buried region of the first conductivity type having a fourth doping level greater than the first level, located at the interface between the substrate and the epitaxial layer in a second portion of the device, the junction between the second buried region and the epitaxial layer forms a second diode having its conduction area of the second conductivity type coupled to a second terminal of the device via the epitaxial layer.
2. The device of claim 1, wherein the first and second diodes have their conduction areas of the first conductivity type connected via the substrate.
3. The device of claim 1, wherein the first diode is a diode having a controlled avalanche voltage.
4. The device of claim 1, wherein the second diode is a diode having a controlled avalanche voltage.
5. The device of claim 1, wherein the second diode is a standard diode which is not intended to operate in avalanche.
6. The device of claim 1, wherein the first and second diodes have their conduction areas of the second conductivity type separated by a vertical insulating region crossing the epitaxial layer.
7. The device of claim 1, wherein the second doping level is lower than the first doping level.
8. The device of claim 1, wherein the first doping level is greater than 1018 atomscm3, the second doping level is lower than 1017 atomscm3, the third doping level is greater than 1018 atomscm3, and the fourth doping level is from 2 to 10 times the first doping level.
9. The device of claim 1, wherein the first doping level is in the range from 1019 to 1021 atomscm3, the second doping level is in the range from 1013 to 1016 atomscm3, the third doping level is in the range from 1019 to 1021 atomscm3, and the fourth doping level is from 2 to 10 times the first doping level.
10. An overvoltage protection device comprising:
a doped substrate of a first conductivity type having a first doping level, coated with a doped epitaxial layer of the second conductivity type having a second doping level;
a first doped buried region of the second conductivity type having a third doping level greater than the second level, located at the interface between the substrate and the epitaxial layer in a first portion of the device, wherein the junction between the substrate and the first buried region forms a first diode; and
a second doped buried region of the first conductivity type having a fourth doping level greater than the first level, located at the interface between the substrate and the epitaxial layer in a second portion of the device, the junction between the second buried region and the epitaxial layer forms a second diode;
wherein the first diode is a diode having a controlled avalanche voltage.
11. The device of claim 10, wherein the first diode has its conduction area of the second conductivity type coupled to a first terminal of the device via the epitaxial layer, and wherein the second diode has its conduction area of the second conductivity type coupled to a second terminal of the device via the epitaxial layer.
12. The device of claim 10, wherein the second doping level is lower than the first doping level.
13. The device of claim 10, wherein the first doping level is greater than 1018 atomscm3, the second doping level is lower than 1017 atomscm3, the third doping level is greater than 1018 atomscm3, and the fourth doping level is from 2 to 10 times the first doping level.
14. The device of claim 10, wherein the first doping level is in the range from 1019 to 1021 atomscm3, the second doping level is in the range from 1013 to 1016 atomscm3, the third doping level is in the range from 1019 to 1021 atomscm3, and the fourth doping level is from 2 to 10 times the first doping level.
15. An overvoltage protection device comprising:
a doped substrate of a first conductivity type having a first doping level, coated with a doped epitaxial layer of the second conductivity type having a second doping level;
a first doped buried region of the second conductivity type having a third doping level greater than the second level, located at the interface between the substrate and the epitaxial layer in a first portion of the device, wherein the junction between the substrate and the first buried region forms a first diode; and
a second doped buried region of the first conductivity type having a fourth doping level greater than the first level, located at the interface between the substrate and the epitaxial layer in a second portion of the device, the junction between the second buried region and the epitaxial layer forms a second diode;
wherein the second diode is a diode having a controlled avalanche voltage.
16. The device of claim 15, wherein the first diode has its conduction area of the second conductivity type coupled to a first terminal of the device via the epitaxial layer, and wherein the second diode has its conduction area of the second conductivity type coupled to a second terminal of the device via the epitaxial layer.
17. The device of claim 15, wherein the second doping level is lower than the first doping level.
18. The device of claim 15, wherein the first doping level is greater than 1018 atomscm3, the second doping level is lower than 1017 atomscm3, the third doping level is greater than 1018 atomscm3, and the fourth doping level is from 2 to 10 times the first doping level.
19. The device of claim 15, wherein the first doping level is in the range from 1019 to 1021 atomscm3, the second doping level is in the range from 1013 to 1016 atomscm3, the third doping level is in the range from 1019 to 1021 atomscm3, and the fourth doping level is from 2 to 10 times the first doping level.
20. An overvoltage protection device comprising:
a doped substrate of a first conductivity type having a first doping level, coated with a doped epitaxial layer of the second conductivity type having a second doping level;
a first doped buried region of the second conductivity type having a third doping level greater than the second level, located at the interface between the substrate and the epitaxial layer in a first portion of the device, wherein the junction between the substrate and the first buried region forms a first diode; and
a second doped buried region of the first conductivity type having a fourth doping level greater than the first level, located at the interface between the substrate and the epitaxial layer in a second portion of the device, the junction between the second buried region and the epitaxial layer forms a second diode;
wherein the first and second diodes have their conduction areas of the second conductivity type separated by a vertical insulating region crossing the epitaxial layer.
21. The device of claim 20, wherein the first diode has its conduction area of the second conductivity type coupled to a first terminal of the device via the epitaxial layer, and wherein the second diode has its conduction area of the second conductivity type coupled to a second terminal of the device via the epitaxial layer.
22. The device of claim 20, wherein the second doping level is lower than the first doping level.
23. The device of claim 20, wherein the first doping level is greater than 1018 atomscm3, the second doping level is lower than 1017 atomscm3, the third doping level is greater than 1018 atomscm3, and the fourth doping level is from 2 to 10 times the first doping level.
24. The device of claim 20, wherein the first doping level is in the range from 1019 to 1021 atomscm3, the second doping level is in the range from 1013 to 1016 atomscm3, the third doping level is in the range from 1019 to 1021 atomscm3, and the fourth doping level is from 2 to 10 times the first doping level.

The claims below are in addition to those above.
All refrences to claim(s) which appear below refer to the numbering after this setence.

1. An image pick-up lens system comprising, from an object side to an image side:
an aperture stop;
a biconvex first lens;
a second lens having a concave surface facing the object side; and
a third lens having a concave surface facing the image side;
wherein the aperture stop and the first, second and third lenses are aligned in that order, the first, second and third lenses are made from essentially the same material, at least one of the first, second and third lenses has a diffraction grating formed thereon, and the following condition is satisfied:
\u22129<f3f<\u22121.7,
wherein f3 is a focal length of the third lens, and f is a focal length of the lens system.
2. The image pick-up lens system in accordance with claim 1, wherein the second lens is a meniscus-shaped lens.
3. The image pick-up lens system in accordance with claim 1, wherein the third lens is a meniscus-shaped lens.
4. The image pick-up lens system in accordance with claim 1, wherein the first lens and the second lens have positive focal power, and the third lens has negative focal power.
5. The image pick-up lens system in accordance with claim 1, wherein the first lens has a diffraction grating formed on a convex surface thereof that faces the image side.
6. The image pick-up lens system in accordance with claim 5, wherein the following condition is also satisfied:
\u2212470<C2\xd7(f1Rn2)<\u2212280,

wherein, C2 is a power phase coefficient of a phase function of the diffraction grating surface of the first lens, and Rn is a normalization radius of the diffraction grating.
7. The image pick-up lens system in accordance with claim 1, wherein the following condition is also satisfied:
1.4<Tf<1.8,

wherein T is a length from the aperture stop to an image pick-up surface.
8. The image pick-up lens system in accordance with claim 1, wherein the following condition is also satisfied:
0.7<f1f<1.2,

wherein, f1 is a focal length of the first lens.
9. The image pick-up lens system in accordance with claim 1, wherein the following condition is also satisfied:
\u22120.6<R4f\xd7(n\u22121)<\u22120.3,

wherein, R4 is a radius of curvature of a surface of the second lens that faces the object side, n is a refractive index of the second lens, and R4f\xd7(n\u22121) is a ratio of a focal length of a surface of the second lens that faces the object side to a total focal length of the lens system.
10. The image pick-up lens system in accordance with claim 1, wherein at least one of the first, second and third lenses has an aspheric surface.
11. The image pick-up lens system in accordance with claim 10, wherein each of the first, second and third lenses has at least one aspheric surface.
12. The image pick-up lens system in accordance with claim 10, wherein opposite surfaces of each of the second and third lenses are aspheric.
13. The image pick-up lens system in accordance with claim 1, wherein the first, second and third lenses are made from essentially the same plastic.
14. The image pick-up lens system in accordance with claim 13, wherein the first and second lenses are made from one of a polyolefin resin and a cyclo-olefin polymer material.
15. An image pick-up system comprising:
an aperture stop for receiving light from an outside of said system;
an image pick-up surface used to accept said light from said aperture stop for image generation of said system; and
at least three lenses disposed between said aperture stop and said image pick-up surface for transmitting said light therebetween, and made of same material, at least one surface of a selective lens of said at least three lenses forming a diffraction grating;
wherein said at least three lenses are made to satisfy at least one of the following conditions:
1.4<Tf<1.8,\u2003\u2003(1)
0.7<f1f<1.2,\u2003\u2003(2)
\u22129<f3f<\u22121.7,\u2003\u2003(3)
\u22120.6<R4f\xd7(n\u22121)<\u22120.3, and\u2003\u2003(4)
\u2212470<C2\xd7(f1Rn2)<\u2212280\u2003\u2003(5)
wherein f is a focal length of said system, T is a length from said aperture stop to said image pick-up surface, f1 is a focal length of a first lens of said at least three lenses closer to said aperture stop, f3 is a focal length of a third lens of said at least three lenses closer to said image pick-up surface, R4 is a radius of curvature of a surface of a second lens of said at least three lenses facing said aperture stop, n is a refractive index of said second lens, R4f\xd7(n\u22121) is a ratio of a focal length of said surface of said second lens facing said aperture stop to said focal length of said system, C2 is a power phase coefficient of a phase function of said diffraction grating, and Rn is a normalization radius of said diffraction grating.
16. The image pick-up system in accordance with claim 15, wherein said at least three lenses are made of same plastic material.
17. An image pick-up system comprising, from an object side to an image side:
an aperture stop;
a biconvex first lens;
a second lens having a concave surface facing the object side; and
a third lens having a concave surface facing the image side;
wherein the aperture stop and the first, second and third lenses are aligned in that order, the first, second and third lenses are made from essentially the same material, the first lens has a diffraction grating formed on a convex surface thereof that faces the image side, and the following condition is satisfied:
\u2212470<C2\xd7(f1Rn2)<\u2212280,
wherein, f1 is a focal length of the first lens, C2 is a power phase coefficient of a phase function of the diffraction grating, and Rn is a normalization radius of the diffraction grating.
18. The image pick-up system in accordance with claim 17, wherein the following condition is also satisfied:
\u22129<f3f<\u22121.7,

wherein f2 is a focal length of the third lens, and f is a focal length of the lens system.

1. A method for enhancing detail detectability in x-ray images, the method comprising:
providing, via an x-ray inspection device, a positive x-ray image of a suitcase or other container under examination for one or more items of interest therein, the positive x-ray image having a brightness that is inversely related to x-ray beam attenuation;
subdividing the x-ray image into an object region and an empty region, the object region including the suitcase or other container under examination and the items of interest therein, and the empty region excluding the suitcase or other container under examination and the items of interest therein; and
darkening the empty region of the x-ray image relative to the object region.
2. The method according to claim 1, wherein the darkening of the empty region is turned on by a viewer of the x-ray image.
3. The method according to claim 1, wherein the darkening of the empty region occurs automatically.
4. The method according to claim 1, wherein the degree of darkening is variable.
5. The method according to claim 1, wherein at least one of the object region or the empty region of the x-ray image is determined via image processing.
6. The method according to claim 1, wherein at least one of the object region or the empty region of the x-ray image is determined by sensors, photoelectric sensors or distance sensors.
7. The method according to claim 1, wherein the object region and the empty region are approximated by rectangles.
8. The method according to claim 1, wherein a contour of the suitcase or other container is detected precisely and reproduced.
9. The method according to claim 8, wherein a clearance distance is provided between the determined contour of the suitcase or other container and a separation between the object region and empty region in the x ray image.
10. An x-ray inspection system comprising:
an x-ray inspection device;
a display device for displaying a positive x-ray image of a suitcase or other container under examination for one or more items of interest therein, the positive x-ray image having a brightness that is inversely related to x-ray beam attenuation, wherein the x-ray image is subdivided into an object region and an empty region, the object region including the suitcase or other container under examination and the items of interest therein, and the empty region excluding the suitcase or other container under examination and the items of interest therein; and
a device for determining and darkening the empty region of the x-ray image relative to the object region.
11. The inspection system according to claim 10, further comprising an actuating element for darkening of the empty region.
12. The x-ray inspection system according to claim 10, further comprising an actuating element for influencing a degree of darkening of the empty region.
13. The method according to claim 1, wherein the darkening of the empty region is adjustable via image processing software.
14. A non-transitory computer-readable medium comprising code, which, when executed by a machine, causes the machine to perform operations for enhancing detail detectability in x-ray images, the computer-readable medium comprising:
code for analyzing a positive x-ray image of a suitcase or other container under examination from an x-ray inspection device for one or more items of interest therein, the positive x-ray image having a brightness that is inversely related to x-ray beam attenuation;
code for subdividing the x-ray image into an object region and an empty region, the object region including the suitcase or other container under examination and the items of interest therein, and the empty region excluding the suitcase or other container under examination and the items of interest therein; and
code for darkening the empty region of the x-ray image relative to the object region.
15. The method according to claim 1, wherein the other container includes one or more pieces of luggage.
16. The method according to claim 1, wherein the one or more items of interest correspond to dangerous contraband contained in the suitcase or other container.
17. The method according to claim 1, wherein darkening the empty region of the x-ray image relative to the object region comprises darkening the empty region while maintaining a brightness of the object region.
18. The method according to claim 1, wherein the empty region of the x-ray image is darkened according to a darkening factor.
19. The method according to claim 1, wherein the empty region of the x-ray image is darkened by replacing image information in the empty region with a uniform color.

The claims below are in addition to those above.
All refrences to claim(s) which appear below refer to the numbering after this setence.

1. A compound of the formula:
wherein
R1 is an optionally substituted aryl or optionally substituted heteroaryl;
R2 is hydrogen, C1\u201310 alkyl, C 3\u20137 cycloalkyl, C 3\u20137 cycloalkylalkyl, aryl, arylC1\u201310 alkyl, heteroaryl, heteroarylC1\u201310 alkyl, heterocyclic, or heterocyclylC1\u201310 alkyl moiety; and wherein each of these moieties, excluding hydrogen, are optionally substituted; provided that X is not hydrogen;
R3 is C1\u201310 alkyl, C 3\u20137 cycloalkyl, C 3\u20137 cycloalkyl C1\u201310 alkyl, arylC1\u201310 alkyl, heteroarylC1\u201310 alkyl, heterocyclylC1\u201310 alkyl moiety; and wherein each of these moieties are optionally substituted;
X is R2, OR2, S(O)mR2 or (CH2)n NR4R14, or (CH2)nNR2R4;
n is 0 or an integer having a value of 1 to 10;
m is 0 or an integer having a value of 1 or 2;
R4 and R14 are each independently selected from hydrogen, optionally substituted C1\u20134 alkyl, optionally substituted aryl or an optionally substituted aryl-C1\u20134 alkyl, or R4 and R14 together with the nitrogen which they are attached form a heterocyclic ring of 5 to 7 members which ring optionally contains an additional heteroatom selected from oxygen, sulfur or NR9, which ring may be optionally substituted;
R6 is hydrogen, C1\u201310 alkyl, C3\u20137 cycloalkyl, heterocyclyl, heterocyclyl C1\u201310alkyl, aryl, arylC1\u201310 alkyl, heteroaryl or heteroarylC1\u201310 alkyl; and wherein each of these moieties, excluding hydrogen, may be optionally substituted;
R9 is hydrogen, C(Z)R6, optionally substituted C1\u201310 alkyl, optionally substituted aryl or optionally substituted aryl-C1\u20134 alkyl;
Z is oxygen or sulfur;
or pharmaceutically acceptable salt thereof.
2. The compound according to claim 1 wherein the structure is of Formula (I), or a pharmaceutically acceptable salt thereof.
3. The compound according to claim 1 wherein R1 is an optionally substituted aryl.
4. The compound according to claim 3 wherein the aryl is substituted one or more times, independently, by halogen, alkyl, hydroxy, alkoxy, amino, or halosubstituted alkyl.
5. The compound according to claim 1 wherein X is R2, OR2, or S(O)mR2.
6. The compound according to claim 1 wherein X is (CH2)nNR4R14, or (CH2)nNR2R4.
7. The compound according to claim 1, which is:
7-Methylsulfanyl-5-phenyl-1-(1-phenylethyl)-3,4-dihydro-1H-pyrimido4,5-d-pyrimidin-2-one; or a pharmaceutically acceptable salt thereof.
8. A compound according to claim 1 wherein R1 is optionally substituted one to 4 times, independently, by halogen, C1\u20134 alkyl, halo-substituted C1\u20134 alkyl, cyano, nitro, (CR10R20)v NR4R14, (CR10R20)v C(Z)NR4R14, (CR10R20)v C(Z)OR8, (CR10R20)v CORa, (CR10R20)v C(O)H, S(O)mR5, (CR10R20)v OR8, ZC(Z)R11, NR10C(Z)R11, or NR10S(O)2R7, and wherein
Ra is C1\u20134 alkyl, halo-substituted C1\u20134 alkyl, C2\u20134 alkenyl, C2\u20134 alkynyl, C3\u20137 cycloalkyl, C5\u20137 cycloalkenyl, aryl, aryl C1\u20134 alkyl, heteroaryl, heteroaryl C1\u20134 alkyl, heterocyclyl, heterocyclyl C1\u20134 alkyl, (CR10R20)vOR7, (CR10R20)vS(O)mR7, (CR10R20)vNHS(O)2R7, or (CR10R20)v NR4R14, and wherein the alkyl, cycloalkyl, cycloalkenyl, aryl, arylalkyl, heterocyclyl, heterocyclylalkyl, heteroaryl, and heteroarylalkyl moieties are optionally substituted;
R5 is hydrogen, C1\u20134 alkyl, C2\u20134 alkenyl, C2\u20134 alkynyl or NR4R14, excluding the moieties SR5 (wherein m is 0) being SNR4R14, S(O)2R5 being SO2H (wherein m is 2) and S(O)R5 being SOH, (wherein m is 1);
R7 is C1\u20136alkyl, aryl, arylC1\u20136alkyl, heterocyclic, heterocyclylC1\u20136 alkyl, heteroaryl, or a heteroarylC1\u20136alkyl moiety; and wherein each of these moieties may be optionally substituted;
R8 is hydrogen, C1\u20134 alkyl, halo-substituted C1\u20134 alkyl, C2\u20134alkenyl, C2\u20134 alkynyl, C3\u20137 cycloalkyl, C5\u20137 cycloalkenyl, aryl, arylC1\u20134 alkyl, heteroaryl, heteroarylC1\u20134 alkyl, heterocyclyl, heterocyclylC1\u20134 alkyl, (CR10R20)tOR7, (CR10R20)tS(O)mR7, (CR10R20)tNHS(O)2R7, or (CR10R20)tNR4R14; and wherein the alkyl, cycloalkyl, cycloalkenyl, aryl, arylalkyl, heterocyclyl, heterocyclyl alkyl, heteroaryl, and heteroaryl alkyl moieties, may be optionally substituted;
R\u2003and R20 are each independently selected from hydrogen or C1\u20134 alkyl;
R\u2002is C1\u20134 alkyl, halo-substituted C1\u20134 alkyl, C2\u20134 alkenyl, C2\u20134alkynyl, C3\u20137 cycloalkyl, C5\u20137 cycloalkenyl, aryl, arylC1\u20134 alkyl, heteroaryl, heteroarylC1\u20134 alkyl, heterocyclyl, heterocyclylC1\u20134 alkyl, (CR10R20)tOR7, (CR10R20)tS(O)mR7, (CR10R20)tNHS(O)2R7, or (CR10R20)vNR4R14; and wherein the alkyl, cycloalkyl, cycloalkenyl, aryl, arylalkyl, heterocyclyl, heterocyclylalkyl, heteroaryl, and heteroaryl alkyl moieties may be optionally substituted;
t is an integer having a value of 1 to 3; and
v is 0 or an integer having a value of 1or 2.
9. A compound according to claim 8 wherein R1 is a phenyl ring optionally substituted, independently one or more times, by halogen or C1\u20134 alkyl.
10. The compound according to claim 1 wherein the structure is of Formula (Ia), or a pharmaceutically acceptable salt thereof.
11. The compound according to claim 9 wherein R1 is a phenyl substituted independently one or more times by chloro, fluoro or methyl.
12. The compound according to claim 1 wherein R3 is optionally substituted one or more times independently with C1\u201310 alkyl, halo-substituted C1\u201310 alkyl, C2\u201310 alkenyl, C2\u201310 alkynyl, C3\u20137 cycloalkyl, C3\u20137cycloalkylC1\u201310 alkyl, C5\u20137 cycloalkenyl, C5\u20137 cycloalkenyl C1\u201310 alkyl, halogen, (CR10R20)nOR6, (CR10R20)nSH, (CR10R20)nS(O)mR7, (CR10R20)nNHS(O)2R7, (CR10R20)nNR4R14, (CR10R20)nCN, (CR10R20)n S(O)2NR4R14, (CR10R20)nC(Z)R6, (CR10R20)nOC(Z)R6, (CR10R20)nC(Z)OR6, (CR10R20)nC(Z)NR4R14, (CR10R20)nNR10C(Z)R6, (CR10R20)nNR10C(=NR10) NR4R14, (CR10R20)nOC(Z)NR4R14, (CR10R20)nNR10C(Z) NR4R14, or (CR10R20)nNR10C(Z)OR7, wherein
R7 is C1\u20136alkyl, aryl, arylC1\u20136alkyl, heterocyclic, heterocyclylC1\u20136 alkyl, heteroaryl, or a heteroarylC1\u20136alkyl moiety; and wherein each of these moieties may be optionally substituted; and R\u2003and R20 are each independently selected from hydrogen or C1\u20134 alkyl.
13. The compound according to claim 12 wherein R3 is an optionally substituted arylC1\u201310alkyl, or a C3\u20137 cycloalkyl moiety.
14. The compound according to claim 13 which is:
5-(4-Fluoro-2-methylphenyl)-7-methylsulfanyl-1-((R)-1-phenylethyl)-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-2-one;
1-((S)-1-Phenylethyl -5-(2-methyl-4-fluoro)phenyl-7-methylsulfanyl-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-2-one;
1-Cyclohexyl -5-(2-methyl-4-fluoro)phenyl-7-methylsulfanyl-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-2-one;
1-Cyclohexyl-5-(4-fluoro-2-methylphenyl)-7-(1-methylpiperidin-4-ylamino)-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-one;
1-Cyclohexyl-5-(4-fluoro-2-methylphenyl)-7-(1-ethylpiperidin-4-ylamino)-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-one;
1-Cyclohexyl-5-(4-fluoro-2-methylphenyl)-7-(2-pyrrolidin-1-yl-ethylamino)-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-one;
1-Cyclohexyl-5-(4-fluoro-2-methylphenyl)-7-(2-piperidin-1-yl ethylamino)-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-one;
1-Cyclohexyl-5-(4-fluoro-2-methylphenyl)-7-(1H-tetrazol-5-ylamino)-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-one; SB-692441
1-Cyclohexyl-5-(4-fluoro-2-methylphenyl)-7-(2-hydroxy-1-hydroxymethyl-1-methylethylamino)-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-one;
1-Cyclohexyl-5-(4-fluoro-2-methylphenyl)-7-((R)-2-hydroxy-1-methyl-ethylamino)-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-one;
1-Cyclohexyl-5-(4-fluoro-2-methylphenyl)-7-((S)-2-hydroxy-1-methylethylamino)-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-one;
1-Cyclohexyl-5-(4-fluoro-2-methylphenyl)-7-(2-hydroxy-1,1-bis-hydroxymethyl-ethylamino)-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-one;
1-Cyclohexyl-5-(4-fluoro-2-methylphenyl)-7-(2-hydroxy-1,1-dimethyl-ethylamino)-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-one;
1-Cyclohexyl-5-(4-fluoro-2-methylphenyl)-7-(1,3dioxolan-2-ylmethyl)amino-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-one;
1-Cyclohexyl-5-(4-fluoro-2-methylphenyl)-7-3-(2-oxo-pyrrolidin-1-yl)-propylamino-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-one;
1-Cyclohexyl-5-(4-fluoro-2-methylphenyl)-7-(2-hydroxyethylamino)-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-one;
1-Cyclohexyl-5-(4-fluoro-2-methylphenyl)-7-(3-pyrrolidin-1-ylpropylamino)-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-one;
1-((S)-1-Phenylethyl)-5-(4-fluoro-2-methylphenyl)-7-(2-pyrrolidin-1-yl-ethylamino)-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-one;
1-((S)-1-Phenylethyl)-5-(4-fluoro-2-methylphenyl)-7-(2-piperidin-1-yl ethylamino)-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-one;
1-((S)-1-Phenylethyl)-5-(4-fluoro-2-methylphenyl)-7-(1H-tetrazol-5-ylamino)-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-one;
1-((S)-1-Phenylethyl)-5-(4-fluoro-2-methylphenyl)-7-((R)-2-hydroxy-1-methyl-ethylamino)-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-one;
1-((S)-1-Phenylethyl)-5-(4-fluoro-2-methylphenyl)-7-(2-hydroxyethyl)-methylamino-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-one;
1-((S)-1-Phenylethyl)-5-(4-fluoro-2-methylphenyl)-7-(1,3dioxolan-2-ylmethyl)amino-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-one;
1-((S)-1-Phenylethyl)-5-(4-fluoro-2-methylphenyl)-7-(1-methylpiperidin-4-ylamino)-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-one;
1-((S)-1-Phenylethyl)-5-(4-fluoro-2-methylphenyl)-7-(1-carboxyeth-2-ylamino)-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-one;
1-((S)-1-Phenylethyl)-5-(4-fluoro-2-methylphenyl)-7-(1-carboxyeth-2-ylamino)-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-one;
1-((S)-1-Phenylethyl)-5-(4-fluoro-2-methylphenyl)-7-(2-hydroxyethylamino)-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-one;
1-((S)-1-Phenylethyl)-5-(4-fluoro-2-methylphenyl)-7-(3-pyrrolidin-1-ylpropylamino)-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-one; or a pharmaceutically acceptable salt thereof.
15. The compound according to claim 8 wherein R1 is an optionally substituted phenyl.
16. The compound according to claim 15 wherein the phenyl ring is mono-substituted in the 4-position, or di-substituted in the 2,4- position.
17. The compound according to claim 16 wherein R1 is phenyl, 2-methylphenyl, 2-methyl-4-fluorophenyl, or 4-fluorophenyl.
18. The compound according to claim 12 wherein R3 is optionally substituted 1 to 4 times.
19. The compound according to claim 6 wherein X is (CH2)nNR2R4.
20. The compound according to claim 19 wherein R2 is hydrogen, substituted or unsubstituted C1\u201310 alkyl, substituted or unsubstituted heterocyclic, substituted or unsubstituted heterocyclic C1\u201310 alkyl, substituted or unsubstituted heteroaryl, or substituted or unsubstituted heteroaryl C1\u201310 alkyl.
21. The compound according to claim 20 wherein R2 is an optionally substituted imidazole, tetrazole, pyrrolidine, piperidine, piperazine, morpholine, 2-,3- or 4-pyridyl, pyrrolidinyl C1\u201310 alkyl, piperidinyl C1\u201310 alkyl, piperazinyl C1\u201310 alkyl, or morpholinyl C1\u201310 alkyl.
22. The compound according to claim 1 wherein the R2 moiety is substituted one to four times, independently by C1\u201310 alkyl, halo-substituted C1\u201310 alkyl, C2\u201310 alkenyl, C2\u201310 alkynyl, C3\u20137 cycloalkyl, C3\u20137cycloalkylC1\u201310alkyl, C5\u20137 cycloalkenyl, C5\u20137 cycloalkenyl C1\u201310 alkyl, halogen, (CR10R20)nOR6, (CR10R20)nSH, (CR10R20)nS(O)mR7, (CR10R20)nNHS(O)2R7, (CR10R20)nNR4R14, (CR10R20)nCN, (CR10R20)nS(O)2NR4R14, (CR10R20)nC(Z)R6, (CR10R20)nOC(Z)R6, (CR10R20)nC(Z)OR6, (CR10R20)nC(Z)NR4R14, (CR10R20)nNR10C(Z)R6, (CR10R20)nNR10C(=NR10)NR4R14, (CR10R20)nOC(Z)NR4R14, (CR10R20)nNR10C(Z)NR4R14, (CR10R20)nNR10C(Z)OR7, or a dioxyalkylene group of the formula -O-(CH2)s-O-, wherein s is 1 to 3;
R7 is C1\u20136alkyl, aryl, arylC1\u20136alkyl, heterocyclic, heterocyclylC1\u20136 alkyl, heteroaryl, or a heteroarylC1\u20136alkyl moiety; and wherein each of these moieties may be optionally substituted; and
R10 and R20 are each independently selected from hydrogen or C1\u20134 alkyl.
23. The compound according to claim 5 wherein X is S(O)mR2 and R2 is a substituted or unsubstituted C1\u201310alkyl, aryl or aryl alkyl.
24. The compound according to claim 23 wherein R2 is methyl.
25. The compound according to claim 6 wherein X is (CH2)nNR4R14.
26. The compound according to claim 25 wherein R4 and R14 are independently selected from hydrogen, optionally substituted C1\u20136alkyl which is substituted one or more times, independently by halogen, hydroxyl, hydroxy substituted C1\u201310alkyl, C1\u201310 alkoxy, halosubstituted C1\u201310 alkoxy, S(O)m C1\u20134alkyl, wherein m is 0, 1 or 2,; amino, mono or di-substituted C1\u20136alkyl amino, C3\u20137cycloalkyl, C3\u20137cycloalkyl C1\u201310 alkyl, halosubstituted C1\u201310 alkyl, optionally substituted aryl, or an optionally substituted arylalkyl; and wherein the these aryl or arylalkyl moieties may also themselves be substituted one to two times by halogen; hydroxy, hydroxy substituted alkyl; C1\u201310 alkoxy, S(O)m C1\u20134 alkyl, amino, mono or di-substituted C1\u20136 alkyl amino, C1\u20134 alkyl, or CF3.
27. The compound according to claim 26 wherein C1\u20136alkyl chain is substituted one or more times, independently by halogen, hydroxy, amino, or mono or di C1\u20134 alkyl substituted amino.
28. The compound according to claim 25 wherein R4 and R14 together with the nitrogen to which they are attached form a heterocyclic ring of 5 to 7 members which ring optionally contains an additional heteroatom selected from oxygen, sulfur or NR9, and which ring may be optionally substituted.
29. The compound according to claim 5 wherein X is the group OR2.
30. The compound according to claim 29 wherein R2 is an optionally substituted C1\u201310 alkyl, aryl, aryl C1\u201310alkyl, heteroaryl, heteroaryl C1\u201310 alkyl, heterocyclic or heterocyclic C1\u201310alkyl moiety.
31. A pharmaceutical composition comprising an effective amount of a compound according to claim 1 and a pharmaceutically acceptable carrier or diluent.
32. A pharmaceutical composition comprising an effective amount of a compound according to claim 14 and a pharmaceutically acceptable carrier or diluent.
33. A compound of the formula:
wherein
R1 is an optionally substituted aryl, or an optionally substituted heteroaryl;
R2 is an optionally substituted heterocyclic or optionally substituted heterocyclicC1\u201310 alkyl;
R2\u2032 is an optionally substituted heterocyclic, optionally substituted heterocyclicC1\u201310 alkyl, optionally substituted aryl, or optionally substituted heteroaryl;
R3 is an optionally substituted aryl or optionally substituted heteroaryl;
X is R2\u2032, OR2, S(O)mR2 or (CH2)n NR4R14, or (CH2)nNR2R4; provided that when X is (CH2)n NR4R14, then R4R14 must form the optionally substituted cyclized ring optionally comprising an oxygen, sulfur or nitrogen moiety;
n is 0 or an integer having a value of 1 to 10;
m is 0 or an integer having a value of 1 or 2;
R4 and R14 are independently selected from hydrogen, optionally substituted C1\u20134 alkyl, optionally substituted aryl, or optionally substituted arylC1\u20134 alkyl; or R4 and R14 together with the nitrogen which they are attached form a heterocyclic ring of 5 to 7 members which ring optionally contains an additional heteroatom selected from oxygen, sulfur or NR9, and which ring is optionally substituted;
R6 is hydrogen, C1\u201310 alkyl, C3\u20137 cycloalkyl, heterocyclyl, heterocyclyl C1\u201310alkyl, aryl, arylC1\u201310 alkyl, heteroaryl or a heteroarylC1\u201310 alkyl moiety; and wherein each of these moieties, excluding hydrogen, is optionally substituted;
R9 is hydrogen, C(Z)R6, optionally substituted C1\u201310 alkyl, optionally substituted aryl, or optionally substituted arylC1\u20134 alkyl;
Z is oxygen or sulfur;
or a pharmaceutically acceptable salt thereof.
34. The compound according to claim 33 wherein the structure is of Formula (III), or a pharmaceutically acceptable salt thereof.
35. The compound according to claim 33 wherein R1 is an optionally substituted aryl.
36. The compound according to claim 35 wherein the aryl is substituted one or more times, independently by halogen, alkyl, hydroxy, alkoxy, amino, or halosubstituted alkyl.
37. The compound according to claim 34 wherein X is OR2, or S(O)mR2.
38. The compound according to claim 34 wherein X is (CH2)n NR4R14, or (CH2)nNR2R4.
39. The compound according to claim 34 wherein X is R2\u2032.
40. The compound according to claim 39 wherein R2\u2032 is an optionally substituted heteroaryl ring or optionally substituted heterocyclic ring.
41. The compound according to claim 40 wherein the ring is an optionally substituted imidazole, pyrrolidine, piperidine, piperazine, or a morpholine ring.
42. The compound according to claim 41 wherein the ring is substituted one or more times, independently, by halogen, C1-10alkyl, halosubstituted C1-10alkyl, (CR10R20)nNR4R14, (CR10R20)nOR6, and (CR10R20)nC(Z)OR6.
43. A compound according to claim 33 wherein R1 is optionally substituted one to 4 times, independently, by halogen, C1\u20134 alkyl, halo-substituted C1\u20134 alkyl, cyano, nitro, (CR10R20)v NR4R14, (CR10R20)v C(Z)NR4R14, (CR10R20)v C(Z)OR8, (CR10R20)v CORa, (CR10R20)v C(O)H, S(O)mR5, (CR10R20)v OR8, ZC(Z)R11, NR10C(Z)R11, or NR10S(O)2R7, and wherein
Ra is C1\u20134 alkyl, halo-substituted C1\u20134 alkyl, C2\u20134 alkenyl, C2\u20134 alkynyl, C3\u20137 cycloalkyl, C5\u20137 cycloalkenyl, aryl, aryl C1-4 alkyl, heteroaryl, heteroaryl C1\u20134 alkyl, heterocyclyl, heterocyclyl C1\u20134 alkyl, (CR10R20)vOR7, (CR10R20)vS(O)mR7, (CR10R20)vNHS(O)2R7, or (CR10R20)v NR4R14, and wherein the alkyl, cycloalkyl, cycloalkenyl, aryl, arylalkyl, heterocyclyl, heterocyclylalkyl, heteroaryl, and heteroarylalkyl moieties are optionally substituted;
R5 is hydrogen, C1\u20134 alkyl, C2\u20134 alkenyl, C2\u20134 alkynyl or NR4R14, excluding the moieties SR5 (wherein m is 0) being SNR4R14, S(O)2R5 being SO2H (wherein m is 2) and S(O)R5 being SOH, (wherein m is 1);
R7 is C1\u20136alkyl, aryl, arylC1\u20136alkyl, heterocyclic, heterocyclylC1\u20136 alkyl, heteroaryl, or a heteroarylC1\u20136alkyl moiety; and wherein each of these moieties may be optionally substituted;
R8 is hydrogen, C1\u20134 alkyl, halo-substituted C1\u20134 alkyl, C2\u20134alkenyl, C2\u20134 alkynyl, C3\u20137 cycloalkyl, C5\u20137 cycloalkenyl, aryl, arylC1\u20134 alkyl, heteroaryl, heteroarylC1\u20134 alkyl, heterocyclyl, heterocyclylC1\u20134 alkyl, (CR10R20)tOR7, (CR10R20)tS(O)mR7, (CR10R20)tNHS(O)2R7, or (CR10R20)tNR4R14; and wherein the alkyl, cycloalkyl, cycloalkenyl, aryl, arylalkyl, heterocyclyl, heterocyclyl alkyl, heteroaryl, and heteroaryl alkyl moieties, may be optionally substituted;
R10 and R20 are each independently selected from hydrogen or C1\u20134 alkyl;
R11 is C1\u20134 alkyl, halo-substituted C1\u20134 alkyl, C2\u20134 alkenyl, C2\u20134alkynyl, C3\u20137 cycloalkyl, C5\u20137 cycloalkenyl, aryl, arylC1\u20134 alkyl, heteroaryl, heteroarylC1\u20134 alkyl, heterocyclyl, heterocyclylC1\u20134 alkyl, (CR10R20)tOR7, (CR10R20)tS(O)mR7, (CR10R20)tNHS(O)2R7, or (CR10R20)vNR4R14; and wherein the alkyl, cycloalkyl, cycloalkenyl, aryl, arylalkyl, heterocyclyl, heterocyclylalkyl, heteroaryl, and heteroaryl alkyl moieties may be optionally substituted;
t is an integer having a value of 1 to 3; and
v is 0 or an integer having a value of 1 or 2.
44. A compound according to claim 43 wherein R1 is a phenyl ring optionally substituted, independently one or more times, by halogen or C1\u20134 alkyl.
45. The compound according to claim 44 wherein R1 is a phenyl substituted independently one or more times by chloro, fluoro or methyl.
46. The compound according to claim 33 wherein R3 is optionally substituted one or more times independently with C1\u201310 alkyl, halo-substituted C1\u201310 alkyl, C2\u201310 alkenyl, C2\u201310 alkynyl, C3\u20137 cycloalkyl, C3\u20137cycloalkylC1\u201310 alkyl, C5\u20137 cycloalkenyl, C5\u20137 cycloalkenyl C1\u201310 alkyl, halogen, (CR10R20)nOR6, (CR10R20)nSH, (CR10R20)nS(O)mR7, (CR10R20)nNHS(O)2R7, (CR10R20)nNR4R14, (CR10R20)nCN, (CR10R20)nS(O)2NR4R14, (CR10R20)nC(Z)R6, (CR10R20)nOC(Z)R6, (CR10R20)nC(Z)OR6, (CR10R20)nC(Z)NR4R14, (CR10R20)nNR10C(Z)R6, (CR10R20)nNR10C(=NR10) NR4R14, (CR10R20)nOC(Z)NR4R14, (CR10R20)nNR10C(Z) NR4R14, or (CR10R20)nNR10C(Z)OR7, wherein
R7 is C1\u20136alkyl, aryl, arylC1\u20136alkyl, heterocyclic, heterocyclylC1\u20136 alkyl, heteroaryl, or a heteroaryiC1\u20136alkyl moiety; and wherein each of these moieties may be optionally substituted; and
R10 and R20 are each independently selected from hydrogen or C1\u20134 alkyl.
47. The compound according to claim 46 wherein R3 is an aryl optionally substituted independently, one or more times by halogen or alkyl.
48. The compound according to claim 47 wherein the aryl is a phenyl ring, substituted in the 2-position or di-substituted in the 2,6-position.
49. The compound according to claim 48 wherein R3 is 2,6-difluorophenyl.
50. The compound according to claim 33 wherein the structure is of Formula (IIIa), or a pharmaceutically acceptable salt thereof.
51. The compound according to claim 33 wherein R3 is phenyl, 2-chlorophenyl, 2,6-dimethylphenyl, 2-fluorophenyl, 2-methylphenyl, or 2,6-difluorophenyl.
52. The compound according to claim 8 wherein R3 is an optionally substituted phenyl, and X is (CH2)n NR4R14, or (CH2)nNR2R4.
53. The compound according to claim 33 which is:
1-(2,6-Difluorophenyl)-5-(4-fluoro-2-methylphenyl)-7-(2-piperidin-4-ylamino)-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-2-one trifluoroacetate;
1-(2,6-Difluorophenyl)-5-(4-fluoro-2-methylphenyl)-7-(1-methylpiperazin-4-yl)-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-2-one;
1-(2,6-Difluorophenyl)-5-(4-fluoro-2-methylphenyl)-7-(1-methyl-1H-imidazol-2-yl-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-2-one;
1-(2,6-Difluorophenyl)-5-(4-fluoro-2-methylphenyl)-7-(imidazol-1yl-)3,4-dihydro-1H-pyrimido4,5-dpyrimidin-2-one;
1-(2,6-Difluorophenyl)-5-(4-fluoro-2-methylphenyl)-7-(1-piperazin-4-yl)-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-2-one;
1-(2,6-Difluorophenyl)-5-(4-fluoro-2-methylphenyl)-7-(4-hydroxypiperdin-1-yl)-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-2-one;
1-(2,6-Difluorophenyl)-5-(4-fluoro-2-methylphenyl)-7-(4-carboxypiperidin-1-yl)-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-2-one;
1-(2,6-Difluorophenyl)-5-(4-fluoro-2-methylphenyl)-7-(4-carboethoxypiperidin-1-yl)-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-2-one;
1-(2,6-Difluorophenyl)-5-(4-fluoro-2-methylphenyl)-7-(4-hydroxymethylpiperdin-1-yl)-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-2-one;
1-(2,6-Difluorophenyl)-5-(4-fluoro-2-methylphenyl)-7-(1-methylpiperidin-4-yl-amino)-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-2-one;
1-(2,6-Difluorophenyl)-5-(4-fluoro-2-methylphenyl)-7-(1-morpholin-4-yl)-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-2-one;
1-(2,6-Difluorophenyl)-5-(4-fluoro-2-methylphenyl)-7-(2-morpholin-4-ylethylamino)-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-2-one;
1-(2,6-Difluorophenyl)-5-(4-fluoro-2-methylphenyl)-7-(2-pyrrolidin-1-yl ethylamino)-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-2-one;
1-(2,6-Difluorophenyl)-5-(4-fluoro-2-methylphenyl)-7-(2-piperidin-1-yl ethylamino)-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-2-one;
1-(2,6-Difluorophenyl)-5-(2-methylphenyl)-7-(1-piperazin-4-yl)-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-2-one;
1-(2,6-Difluorophenyl)-5-(4-fluoro-2-methylphenyl-7-(1-methylpiperidin-4-yloxy)-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-2-one;
a pharmaceutically acceptable salt thereof.
54. The compound according to claim 45 wherein the phenyl ring is mono-substituted in the 4-position, or di-substituted in the 2,4- position.
55. The compound according to claim 33 wherein R1 is phenyl, 2-methylphenyl, 2-methyl-4-fluorophenyl, or 4-fluorophenyl.
56. The compound according to claim 43 wherein R1 is an optionally substituted phenyl.
57. The compound according to claim 33 wherein R3 is phenyl, 2-chlorophenyl, 2,6-dimethylphenyl, 2-fluorophenyl, 2-methylphenyl, or 2,6-difluorophenyl.
58. The compound according to claim 46 wherein R3 is an optionally substituted phenyl.
59. The compound according to claim 46 wherein R3 is optionally substituted 1 to 4 times.
60. The compound according to claim 33 wherein R2\u2032 is optionally substituted one to four times, independently by C1\u201310 alkyl, halo-substituted C1\u201310 alkyl, C2\u201310 alkenyl, C2\u201310 alkynyl, C3\u20137 cycloalkyl, C3\u20137cycloalkylC1\u201310alkyl, C5\u20137 cycloalkenyl, C5\u20137 cycloalkenyl C1\u201310 alkyl, halogen, (CR10R20)nOR6, (C10R20)nSH, (CR10R20)nS(O)mR7, (CR10R20)nNHS(O)2R7, (CR10R20)nNR4R14, (CR10R20)nCN, (CR10R20)nS(O)2NR4R14, (CR10R20)nC(Z)R6, (CR10R20)nOC(Z)R6, (CR10R20)nC(Z)OR6, (CR10R20)nC(Z)NR4R14, (CR10R20)nNR10C(Z)R6, (CR10R20)nNR10C(=NR10) NR4R14, (CR10R20)nOC(Z)NR4R14, (CR10R20)nNR10C(Z) NR4R14, (CR10R20)nNR10C(Z)OR7, or a dioxyalkylene group of the formula -O-(CH2)s-O-, wherein s is 1 to 3;
R7 is C1\u20136alkyl, aryl, arylC1\u20136alkyl, heterocyclic, heterocyclylC1\u20136 alkyl, heteroaryl, or a heteroarylC1\u20136alkyl moiety; and wherein each of these moieties may be optionally substituted; and
R10 and R20 are each independently selected from hydrogen or C1\u20134 alkyl.
61. The compound according to claim 60 wherein R2\u2032 is an optionally substituted pyrrolidine, piperidine, piperazine, morpholine, pyrrolidinyl C1\u201310 alkyl, piperidinyl C1\u201310 alkyl, piperazinyl C1\u201310 alkyl, or morpholinyl C1\u201310 alkyl, phenyl, imidazole or tetrazole ring.
62. The compound according to claim 33 wherein R2 is optionally substituted one or more times, independently by C1\u201310 alkyl, halo-substituted C1\u201310 alkyl, C2\u201310 alkenyl, C2\u201310 alkynyl, C3\u20137 cycloalkyl, C3\u20137cycloalkylC1\u201310alkyl, C5\u20137 cycloalkenyl, C5\u20137 cycloalkenyl C1\u201310 alkyl, halogen, (CR10R20)nOR6, (CR10R20)nSH, (CR10R20)nS(O)mR7, (CR10R20)nNHS(O)2R7, (CR10R20)nNR4R14, (CR10R20)nCN, (CR10R20)nS(O)2NR4R14, (CR10R20)nC(Z)R6, (CR10R20)nOC(Z)R6, (CR10R20)nC(Z)OR6, (CR10R20)nC(Z)NR4R14, (CR10R20)nNR10C(Z)R6, (CR10R20)nNR10C(=NR10) NR4R14, (CR10R20)nOC(Z)NR4R14, (CR10R20)nNR10C(Z) NR4R14, (CR10R20)nNR10C(Z)OR7, or a dioxyalkylene group of the formula -O-(CH2)s-O-, wherein s is 1 to 3;
R7 is C1\u20136alkyl, aryl, arylC1\u20136alkyl, heterocyclic, heterocyclylC1\u20136 alkyl, heteroaryl, or a heteroarylC1\u20136alkyl moiety; and wherein each of these moieties may be optionally substituted; and
R10 and R20 are each independently selected from hydrogen or C1\u20134 alkyl.
63. The compound according to claim 62 wherein R2 is an optionally substituted pyrrolidine, piperidine, piperazine, morpholine, pyrrolidinyl C1\u201310 alkyl, piperidinyl C1\u201310 alkyl, piperazinyl C1\u201310 alkyl, or morpholinyl C1\u201310 alkyl.
64. A pharmaceutical composition comprising an effective amount of a compound according to claim 33 and a pharmaceutically acceptable carrier or diluent.
65. A pharmaceutical composition comprising an effective amount of a compound according to claim 53 and a pharmaceutically acceptable carrier or diluent.
66. The compound which is:
1-(2,6-Difluorophenyl)-5-phenyl-7-(4-methylpiperazin-1-yl)-3,4-dihydro-1H-pyrimido-4,5-dpyrimidin-2-one
1-(2,6-Difluorophenyl)-5-phenyl-7-piperazin-1-yl-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-2-one
1-(2,6-diflurorophenyl)-5-phenyl-7-(2-hydroxyethyl)methylamino-3,4-dihydro-1H-pyrimido-4,5-dpyrimidin-2-one
1-(2,6-diflurorophenyl)-5-phenyl-7-(4-carboethoxypiperidin-1-yl)-3,4-dihydro-1H-pyrimido-4,5-dpyrimidin-2-one
1-(2,6-diflurorophenyl)-5-phenyl-7-(4-hydroxypiperidin-1-yl)-3,4-dihydro-1H-pyrimido-4,5-dpyrimidin-2-one
1-(2,6-diflurorophenyl)-5-phenyl-7-(imidazol-1-yl)-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-2-one
1-(2,6-diflurorophenyl)-5-phenyl-7-(morpholin-1-yl)-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-2-one
1-(2,6-Difluorophenyl)-5-(4-fluorophenyl-7-(4-methylpiperazin-1-yl)-3,4-dihydro-1H-pyrimido-4,5-dpyrimidin-2-one
1-(2,6-diflurorophenyl)-5-(4-fluorophenyl)-7-(2-hydroxyethyl)methylamino-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-2-one
1-(2,6-difluorophenyl)-5-(4-fluorophenyl)-7-(piperazin-1-yl)-3,4-dihydro-1H-pyrimido-4,5-dpyrimidin-2-one
1-(2,6-difluorophenyl)-5-(4-fluorophenyl)-7-(4-carboethoxypiperidin-1-yl)-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-2-one
1-(2,6-difluorophenyl)-5-(4-fluorophenyl)-7-(4-hydroxypiperidin-1-yl)-3,4-dihydro-1H-pyrimido-4,5-dpyrimidin-2-one
1-(2,6-diflurorophenyl)-5-(4-fluorophenyl)-7-(imidazol-1-yl)-3,4-dihydro-1H-pyrimido-4,5-dpyrimidin-2-one
1-(2,6-diflurorophenyl)-5-(4-fluorophenyl)-7-(morpholin-1-yl)-3,4-dihydro-1H-pyrimido-4,5-dpyrimidin-2-one
1-(2,6-diflurorophenyl)-5-(4-fluorophenyl)-7-(4-hydroxymethylpiperidin-1-yl)-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-2-one
1-(2,6-difluorophenyl)-5-phenyl-7-(1-methyl-1H-imidazol-2-yl-3,4-dihydro-1H-pyrimido-4,5-dpyrimidin-2-one
1-(2,6-difluorophenyl)-5-(4-fluorophenyl)-7-(1-methyl-1H-imidazol-2-y)l-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-2-one
1-(2,6-difluorophenyl)-5-phenyl-7-(4-carboxypiperidin-1-yl)-3,4-dihydro-1H-pyrimido-4,5-dpyrimidin-2-one trifluoroacetate
1-(2,6-difluorophenyl)-5-(4-fluorophenyl)-7-(4-carboxypiperidin-1-yl)-3,4-dihydro-1H-pyrimido-4,5-dpyrimidin-2-one trifluoroacetate
1-(2-Chlorophenyl)-5-(4-fluoro-2-methylphenyl)-7-(2-pyrrolidin-1-yl-ethylamino)-3,4-dihydro-1H-pyrimidido4,5-dpyrimidin-2-one
1-(2-Chlorophenyl)-5-(4-fluoro-2-methylphenyl)-7-(1H-tetrazol-5-ylamino)-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-one
1-(2-Chlorophenyl)-5-(4-fluoro-2-methylphenyl)-7-(2-piperidin-1-ylethylamino)-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-one
1-(2-Chlorophenyl)-5-(4-fluoro-2-methylphenyl)-7-(2-hydroxy-1-hydroxymethyl-1-methylethylamino-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-one
1-(2-Chlorophenyl)-5-(4-fluoro-2-methylphenyl)-7-((R)-2-hydroxy-1-methylethylamino)-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-one
1-(2-Chlorophenyl)-5-(4-fluoro-2-methylphenyl)-7-((S)-2-hydroxy-1-methylethylamino)-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-one
1-(2-Chlorophenyl)-5-(4-fluoro-2-methylphenyl)-7-(2-hydroxy-1,1-bis-hydroxymethyl-ethylamino)-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-one
1-(2-Chlorophenyl)-5-(4-fluoro-2-methylphenyl)-7-(2-hydroxy-1,1-dimethyl-ethylamino)-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-one
1-(2-Chlorophenyl)-5-(4-fluoro-2-methylphenyl)-7-(2-hydroxyethy)-methylamino-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-one
1-(2-Chlorophenyl)-5-(4-fluoro-2-methylphenyl)-7-(racemic)-3-exo-(bicyclo 2.2.1hept-ene-2-carboxylic acid amide)amino)-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-one
1-(2-Chlorophenyl)-5-(4-fluoro-2-methylphenyl)-7-(racemic)-3-endo-(bicyclo 2.2.1hept-ene-2-carboxylic acid amide)amino-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-one;
or a pharmaceutically acceptable salt thereof.
67. A pharmaceutical composition comprising an effective amount of a compound according to claim 66 and a pharmaceutically acceptable carrier or diluent.
68. A compound of the formula:
wherein
X is R2, OR2, S(O)mR2 or (CH2)nNR4R14, or (CH2)nNR2R4;
n is 0 or an integer having a value of 1 to 10;
m is 0 or an integer having a value of 1 or 2;
R1 is an optionally substituted aryl ring;
R2 is hydrogen, C1\u201310 alkyl, C3\u20137 cycloalkyl, C3\u20137 cycloalkylalkyl, aryl, arylC1\u201310 alkyl, heteroaryl, heteroarylC1\u201310 alkyl, heterocyclic, or heterocyclylC1\u201310 alkyl moiety; and
wherein each of these moieties, excluding hydrogen are optionally substituted; provided that X is not hydrogen;

R3 is an optionally substituted aryl ring;
R4 and R14 are each independently selected from hydrogen, optionally substituted C1\u20134 alkyl, optionally substituted aryl or optionally substituted aryl-C1\u20134 alkyl, or R4 and R14 together with the nitrogen which they are attached form a heterocyclic ring of 5 to 7 members which ring optionally contains an additional heteroatom selected from oxygen, sulfur or NR9, and which ring is optionally substituted;
R6 is hydrogen, C1\u201310 alkyl, C3\u20137 cycloalkyl, heterocyclyl, heterocyclyl C1\u201310alkyl, aryl, arylC1\u201310 alkyl, heteroaryl or heteroarylC1\u201310 alkyl; and wherein each of these moieties, excluding hydrogen, may be optionally substituted;
R9 is hydrogen, C(Z)R6, optionally substituted C1\u201310 alkyl, optionally substituted aryl or optionally substituted aryl-C1\u20134 alkyl;
Z is oxygen or sulfur;
or a pharmaceutically acceptable salt thereof.
69. The compound according to claim 68 wherein R1 is an optionally substituted phenyl ring.
70. The compound according to claim 69 wherein the phenyl is substituted one or more times, independently, by halogen, alkyl, hydroxy, alkoxy, amino, or halosubstituted alkyl.
71. The compound according to claim 68 wherein R3 is a phenyl ring optionally substituted one or more times, independently with halogen.
72. The compound according to claim 69, wherein R1 is unsubstituted or substituted one or more times, independently with halogen or alkyl.
73. The compound according to claim 68 wherein X is OR2.
74. The compound according to claim 68 wherein X is S(O)mR2.
75. The compound according to claim 68 wherein X is (CH2)nNR4R14.
76. The compound according to claim 68 wherein X is (CH2)nNR2R4.
77. The compound according to claim 68 wherein X is R2.
78. The compound according to claim 54 wherein R2 is an optionally substituted C1\u201310 alkyl, optionally substituted heteroaryl, or optionally substituted heterocyclic moiety.
79. The compound according to claim 78 wherein R2 is an optionally substituted imidazole, pyrrolidine, piperidine, piperazine, or a morpholine ring.
80. The compound according to claim 79 wherein R2 is substituted one or more times, independently, by halogen, C1\u201310alkyl, halosubstituted C1\u201310alkyl, (CR10R20)nNR4R14, (CR10R20)nOR6, and (CR10R20)nC(Z)OR6.
81. The compound according to claim 68 wherein the structure is of Formula (V), or a pharmaceutically acceptable salt thereof.
82. The compound according to claim 68 wherein the structure is of Formula (Va), or a pharmaceutically acceptable salt thereof.
83. The compound according to claim 68 wherein R1 is optionally substituted one to 4 times, independently, by halogen, C1\u20134 alkyl, halo-substituted C1\u20134 alkyl, cyano, nitro, (CR10R20)v NR4R14, (CR10R20)v C(Z)NR4R14, (CR10R20)v C(Z)OR8, (CR10R20)v CORa, (CR10R20)v C(O)H, S(O)mR5, (CR10R20)v OR8, ZC(Z)R11, NR10C(Z)R11, or NR10S(O)2R7, and wherein
Ra is C1\u20134 alkyl, halo-substituted C1\u20134 alkyl, C2\u20134 alkenyl, C2\u20134 alkynyl, C3\u20137 cycloalkyl, C5\u20137 cycloalkenyl, aryl, aryl C1\u20134 alkyl, heteroaryl, heteroaryl C1\u20134 alkyl, heterocyclyl, heterocyclyl C1\u20134 alkyl, (CR10R20)vOR7, (CR10R20)vS(O)mR7, (CR10R20)vNHS(O)2R7, or (CR10R20)v NR4R14, and wherein the alkyl, cycloalkyl, cycloalkenyl, aryl, arylalkyl, heterocyclyl, heterocyclylalkyl, heteroaryl, and heteroarylalkyl moieties are optionally substituted;
R5 is hydrogen, C1\u20134 alkyl, C2\u20134 alkenyl, C2\u20134 alkynyl or NR4R14, excluding the moieties SR5 (wherein m is 0) being SNR4R14, S(O)2R5 being SO2H (wherein m is 2) and S(O)R5 being SOH, (wherein m is 1);
R7 is C1\u20136alkyl, aryl, arylC1\u20136alkyl, heterocyclic, heterocyclylC1\u20136 alkyl, heteroaryl, or a heteroarylC1\u20136alkyl moiety; and wherein each of these moieties may be optionally substituted;
R8 is hydrogen, C1\u20134 alkyl, halo-substituted C1\u20134 alkyl, C2\u20134alkenyl, C2\u20134 alkynyl, C3\u20137 cycloalkyl, C5\u20137 cycloalkenyl, aryl, arylC1\u20134 alkyl, heteroaryl, heteroarylC1\u20134 alkyl, heterocyclyl, heterocyclylC1\u20134 alkyl, (CR10R20)tOR7, (CR10R20)tS(O)mR7, (CR10R20)tNHS(O)2R7, or (CR10R20)tNR4R14; and wherein the alkyl, cycloalkyl, cycloalkenyl, aryl, arylalkyl, heterocyclyl, heterocyclyl alkyl, heteroaryl, and heteroaryl alkyl moieties, may be optionally substituted;
R10 and R20 are each independently selected from hydrogen or C1\u20134 alkyl;
R11 is C1\u20134 alkyl, halo-substituted C1\u20134 alkyl, C2\u20134 alkenyl, C2\u20134alkynyl, C3\u20137 cycloalkyl, C5\u20137 cycloalkenyl, aryl, arylC1\u20134 alkyl, heteroaryl, heteroarylC1\u20134 alkyl, heterocyclyl, heterocyclylC1\u20134 alkyl, (CR10R20)tOR7, (CR10R20)tS(O)mR7, (CR10R20)tNHS(O)2R7, or (CR10R20)vNR4R14; and wherein the alkyl, cycloalkyl, cycloalkenyl, aryl, arylalkyl, heterocyclyl, heterocyclylalkyl, heteroaryl, and heteroaryl alkyl moieties may be optionally substituted;
t is an integer having a value of 1 to 3; and
v is 0 or an integer having a value of 1 or 2.
84. The compound according to claim 83 wherein R1 is an optionally substituted phenyl.
85. The compound according to claim 68 wherein R3 is optionally substituted one or more times independently with C1\u201310 alkyl, halo-substituted C1\u201310 alkyl, C2\u201310 alkenyl, C2\u201310 alkynyl, C3\u20137 cycloalkyl, C3\u20137cycloalkylC1\u201310 alkyl, C5\u20137 cycloalkenyl, C5\u20137 cycloalkenyl C1\u201310 alkyl, halogen, (CR10R20)nOR6, (CR10R20)nSH, (CR10R20)nS(O)mR7, (CR10R20)nNHS(O)2R7, (CR10R20)nNR4R14, (CR10R20)nCN, (CR10R20)nS(O)2NR4R14, (CR10R20)nC(Z)R6, (CR10R20)nOC(Z)R6, (CR10R20)nC(Z)OR6, (CR10R20)nC(Z)NR4R14, (CR10R20)nNR10C(Z)R6, (CR10R20)nNR10C(\xd7NR10)NR4R14, (CR10R20)nOC(Z)NR4R14, (CR10R20)nNR10C(Z)NR4R14, or (CR10R20)nNR10C(Z)OR7, wherein
R7 is C1\u20136alkyl, aryl, arylC1\u20136alkyl, heterocyclic, heterocyclylC1\u20136 alkyl, heteroaryl, or a heteroarylC1\u20136alkyl moiety; and wherein each of these moieties may be optionally substituted; and
R10 and R20 are each independently selected from hydrogen or C1\u20134 alkyl.
86. The compound according to claim 85 wherein R3 is a phenyl substituted in the 2-position or di-substituted in the 2,6-position.
87. The compound according to claim 86 wherein R3 is 2,6-difluorophenyl.
88. The compound according to claim 68 wherein R3 is phenyl, 2-chlorophenyl, 2,6-dimethyiphenyl, 2-fluorophenyl, 2-methyiphenyl, or 2,6-difluorophenyl.
89. The compound according to claim 85 wherein R3 is optionally substituted 1 to 4 times.
90. The compound according to claim 68 wherein R1 is phenyl, 2-methylphenyl, 2-methyl-4-fluorophenyl, or 4-fluorophenyl.
91. The compound according to claim 74 wherein X is S(O)mR2 and R2 is a substituted or unsubstituted C1\u201310alkyl, aryl or aryl C1\u201310alkyl.
92. The compound according to claim 91 wherein R2 is methyl.
93. The compound according to claim 75 wherein X is (CH2)nNR4R14 and n is 0.
94. The compound according to claim 63 wherein R4 and R14 are independently selected from hydrogen, optionally substituted C1\u20136alkyl which is substituted one or more times, independently by halogen, hydroxyl, hydroxy substituted C1\u201310alkyl, C1\u201310 alkoxy, halosubstituted C1\u201310 alkoxy, S(O)m C1\u20134alkyl, wherein m is 0, 1 or 2,; amino, mono or di-substituted C1\u20136 alkyl amino, C3\u20137cycloalkyl, C3\u20137cycloalkyl C1\u201310 alkyl, halosubstituted C1\u201310 alkyl, optionally substituted aryl, or an optionally substituted arylalkyl; and wherein the these aryl or arylalkyl moieties may also themselves be substituted one to two times by halogen; hydroxy, hydroxy substituted alkyl; C1\u201310 alkoxy, S(O)m C1\u20134 alkyl, amino, mono or di-substituted C1\u20136 alkyl amino, C1\u20134 alkyl, or CF3.
95. The compound according to claim 94 wherein C1\u20136alkyl chain is substituted one or more times, independently by halogen, hydroxy, amino, or mono or di C1\u20134 alkyl substituted amino.
96. The compound according to claim 93 wherein R4 and R1\u20134 together with the nitrogen to which they are attached form a heterocyclic ring of 5 to 7 members which ring optionally contains an additional heteroatom selected from oxygen, sulfur or NR9, and which ring may be optionally substituted.
97. The compound according to claim 93 wherein R1 is an optionally substituted phenyl and R3 is an optionally substituted phenyl.
98. The compound according to claim 73 wherein X is OR2 and R2 is an optionally substituted C1\u201310 alkyl, aryl, aryl C1\u201310alkyl, heteroaryl, heteroaryl C1\u201310 alkyl, heterocyclic or heterocyclic C1\u201310alkyl moiety.
99. The compound according to claim 76 wherein X is (CH2)nNR2R4 and R2 is hydrogen, substituted or unsubstituted C1\u201310 alkyl, substituted or unsubstituted heterocyclic, substituted or unsubstituted heterocyclic C1\u201310 alkyl, substituted or unsubstituted heteroaryl, or substituted or unsubstituted heteroaryl C1\u201310 alkyl.
100. The compound according to claim 68 wherein R2 is an optionally substituted imidazole, tetrazole, pyrrolidine, piperidine, piperazine, morpholine, pyrrolidinyl C1\u201310 alkyl, piperidinyl C1\u201310 alkyl, piperazinyl C1\u201310 alkyl, or morpholinyl C1\u201310 alkyl.
101. The compound according to claim 99 wherein R3 is an optionally substituted phenyl; and R1 is an optionally substituted phenyl.
102. The compound according to claim 68 which is:
1,5-Diphenyl-7-methoxy-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-2-one;
1-(2,6-Difluorophenyl)-5-(4-fluoro-2-methylphenyl)-7-(2-1,3-dihydroxyprop-2-yl-amino)-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-2-one;
1-(2,6-Difluorophenyl)-5-(4-fluoro-2-methylphenyl-7-(2-hydroxyethoxy)-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-2-one;
1-(2,6-Difluorophenyl)-5-(4-fluoro-2-methylphenyl)-7-bis-(2-hydroxyethyl)-aminoethoxy-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-2-one;
1-(2,6-Difluorophenyl)-5-(4-fluoro-2-methylphenyl)-7-(2,3-dihydroxypropylamino)-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-2-one; or
1-(2-Chlorophenyl)-7-methylsulfanyl-5-(2-methyl-4-fluoro)phenyl-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-2-one;
1-(2,6-Difluorophenyl)-5-(4-fluoro-2-methylphenyl)-7-(2-methyl-1,3-dihydroxyprop-2-ylamino)-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-2-one;
1-(2,6-Difluorophenyl)-5-(4-fluoro-2-methylphenyl-7-ethoxy-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-2-one;
1-(2,6-Difluorophenyl)-5-(4-fluoro-2-methylphenyl)-7-((R)-2-hydroxy-1-methyl-ethylamino)-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-2-one;
1-(2,6-Difluorophenyl)-5-(4-fluoro-2-methylphenyl)-7-((S)-2-hydroxy-1-methyl-ethylamino)-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-2-one;
1-(2,6-Difluorophenyl)-5-(4-fluoro-2-methylphenyl)-7-(2-hydroxy-1,1-dimethyl-ethylamino)-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-2-one;
1-(2,6-Difluorophenyl)-5-(4-fluoro-2-methylphenyl)-7-(2-hydroxy-1,1-bis-hydroxy-methyl-ethylamino)-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-2-one;
1-(2,6-Difluorophenyl)-5-(4-fluoro-2-methylphenyl)-7-(2-hydroxyethylamino)-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-2-one;
1-(2,6-Difluorophenyl)-5-(4-fluoro-2-methylphenyl)-7-(2-dimethylamino)-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-2-one;
1-(2,6-Difluorophenyl)-5-(4-fluoro-2-methylphenyl)-7-(2-methylamino)-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-2-one;
1-(2,6-Difluorophenyl)-5-(2-methylphenyl)-7-methylsulfanyl-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-2-one;
1-(2,6-Difluorophenyl)-5-(2-methylphenyl)-7-(1-piperazin-4-yl)-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-2-one;
1-(2,6-Difluorophenyl)-5-(2-methylphenyl)-7-(2-diethylamino ethylamino)-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-2-one;
1-(2,6-Difluorophenyl)-5-phenyl-7-methoxy-3,4-dihydro-1H-pyrimido4,5-d-pyrimidin-2-one;
1-(2-Fluorophenyl)-7-methylsulfanyl-5-(2-methyl-4-fluoro)phenyl-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-2-one;
1-(2,6-Dimethylphenyl)-7-methylsulfanyl-5-(2-methyl-4-fluoro)phenyl-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-2-one;
1-(2-Methylphenyl)-7-methylsulfanyl-5-(2-methyl-4-fluoro)phenyl-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-2-one;
1-(2,6-Difluorophenyl)-5-(4-fluoro-2-methylphenyl)-7-(2-diethylamino ethylamino)-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-2-one;
1-(2,6-Difluorophenyl)-5-(4-fluoro-2-methylphenyl)-7-di(ethan-2-ol-)amino-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-2-one;
1-(2,6-Difluorophenyl)-7-methylsulfanyl-5-phenyl-3,4-dihydro-1H-pyrimido4,5-d-pyrimidin-2-one;
1-(2,6-Difluorophenyl)-7-methylsulfanyl-5-(4-fluorophenyl)-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-2-one;
1-(2,6-Difluorophenyl)-5-(4-fluoro-2-methylphenyl)-7-(2-hydroxyethyl)-methylamino-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-2-one;
5-(4-Fluoro-2-methylphenyl)-7-methylsulfanyl-1-((R)-1-phenylethyl)-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-2-one;
5-(4-Fluoro-2-methylphenyl)-7-methylsulfanyl-1-((S)-1-phenylethyl)-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-2-one;
7-Methylsulfanyl-1,5-diphenyl-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-2-one;
1-(2,6-Difluorophenyl)-5-(4-fluoro-2-methylphenyl)-7-methylsulfanyl-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-2-one;
1-(2,6-Difluorophenyl)-5-(4-fluoro-2-methylphenyl)-7-methylsulfonyl-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-2-one;
1-(2,6-Difluorophenyl)-5-(4-fluoro-2-methylphenyl)-7-(2-pyridin-3-yl ethylamino)-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-2-one;
1-(2,6-Difluorophenyl)-5-(4-fluoro-2-methylphenyl)-7-(2-pyridin-3-yl ethylamino)-3,4-dihydro-1H-pyrimido4,5-dpyrimidin-2-one;
or a pharmaceutically acceptable salt thereof.
103. A pharmaceutical composition comprising an effective amount of a compound according to claim 68 and a pharmaceutically acceptable carrier or diluent thereof.
104. A pharmaceutical composition comprising an effective amount of a compound according to claim 102 and a pharmaceutically acceptable carrier or diluent.