1. A liquid crystal display, comprising:
a light guide plate having a light-emitting plane on one end surface;
a light source arranged on a side surface of the light guide plate; and
a liquid crystal panel arranged opposite the light-emitting plane;
wherein deflection patterns are formed on a surface opposite the light-emitting plane,
the defection patterns are arranged so that two independent components on the surface opposite the light-emitting plane become random,
in a certain region on the surface opposite the light-emitting plane, when an average number of the deflection patterns included in each region opposite each pixel of the liquid crystal panel is designated by \u03bcn and a standard deviation is designated by \u03c3n, their ratio satisfies the following relationship:
0<\u03c3n\u03bcn\u22660.154,
light from the light source introduced into the light guide plate is deflected towards the light-emitting plane by the deflection patterns so as to be emitted from the light-emitting plane,
the liquid crystal panel is illuminated by the light emitted from the light-emitting plane.
2. A liquid crystal display, comprising:
a light guide plate having a light-emitting plane on one end surface;
a light source arranged on a side surface of the light guide plate; and
a liquid crystal panel arranged opposite the light-emitting plane,
wherein deflection patterns are formed on a surface opposite the light-emitting plane,
the deflection patterns are arranged so that two independent components on the surface opposite the light-emitting plane are random,
in a certain square region having a side with length of K on the surface opposite the light-emitting plane, when the number of the deflection patterns included in the corresponding square region is designated by M, a ratio of a pixel pitch p of the liquid crystal panel to an average pattern gap defined by:
Samp_A=K(\u221aM)
satisfies the following relationship:
Samp_Ap\u22660.28,
light from the light source introduced into the light guide plate is deflected towards the light-emitting plane by the deflection patterns so as to be emitted from the light-emitting plane,
the liquid crystal panel is illuminated by the light emitted from the light-emitting plane.
3. A liquid crystal display, comprising:
a light guide plate having a light-emitting plane on one end surface;
a point light source arranged on a side surface of the light guide plate; and
a liquid crystal panel arranged opposite the light-emitting plane,
wherein deflection patterns are formed on a surface opposite the light-emitting plane,
the deflection patterns are arranged so that two independent components on the surface opposite the light-emitting plane are random,
in the case where a projection area of the deflection patterns to the light-emitting plane is designated by S, a distance between the light source and the deflection pattern is designated by Rp and a thickness of the light guide plate in positions of the deflection patterns is designate by d, in a certain region on the surface opposite the light-emitting plane, when an average value obtained by adding S(Rp\xd7d) of all the deflection patterns included in all the regions opposite the pixels of the liquid crystal panel is designated by \u03bc\u03b1 and a standard deviation is designated by \u03c3\u03b1, their ratio satisfies the following relationship:
0<\u03c3\u03b1\u03bc\u03b1\u22660.154,
light from the light source introduced into the light guide plate is deflected towards the light-emitting plane by the deflection patterns so as to be emitted from the light-emitting plane,
the liquid crystal panel is illuminated by the light emitted from the light-emitting plane.
4. The liquid crystal display according to claim 1, wherein a minimum gap between the deflection patterns is larger in a direction parallel with a direction of the light source than that in a direction perpendicular to the direction of the light source.
5. The liquid crystal display according to claim 2, wherein a minimum gap between the deflection patterns is larger in a direction parallel with a direction of the light source than that in a direction perpendicular to the direction of the light source.
6. The liquid crystal display according to claim 3, wherein a minimum gap between the deflection patterns is larger in a direction parallel with a direction of the light source than that in a direction perpendicular to the direction of the light source.
7. A surface light source device, comprising:
a light guide plate having a light-emitting plane on one end surface; and
a light source arranged on a side surface of the light guide plate;
wherein deflection patterns are formed on a surface opposite the light-emitting plane,
the defection patterns are arranged so that two independent components on the surface opposite the light-emitting plane become random,
in a certain region on the surface opposite the light-emitting plane, when an average number of the deflection patterns included in each pixel corresponding region is designated by \u03bcn and a standard deviation is designated by \u03c3n, their ratio satisfies the following relationship:
0<\u03c3n\u03bcn\u22660.154,
light from the light source introduced into the light guide plate is deflected towards the light-emitting plane by the deflection patterns so as to be emitted from the light-emitting plane.
8. A surface light source device, comprising:
a light guide plate having a light-emitting plane on one end surface; and
a light source arranged on a side surface of the light guide plate;
wherein deflection patterns are formed on a surface opposite the light-emitting plane,
the deflection patterns are arranged so that two independent components on the surface opposite the light-emitting plane are random,
in a certain square region having a side with length of K on the surface opposite the light-emitting plane, when the number of the deflection patterns included in the corresponding square region is designated by M, a ratio of a pixel pitch p of a pixel corresponding region to an average pattern gap defined by:
Samp_A=K(\u221aM)
satisfies the following relationship:
Samp_Ap\u22660.28,
light from the light source introduced into the light guide plate is deflected towards the light-emitting plane by the deflection patterns so as to be emitted from the light-emitting plane.
9. A surface light source device, comprising:
a light guide plate having a light-emitting plane on one end surface; and
a point light source arranged on a side surface of the light guide plate;
wherein deflection patterns are formed on a surface opposite the light-emitting plane,
the deflection patterns are arranged so that two independent components on the surface opposite the light-emitting plane are random,
in the case where a projection area of the deflection patterns to the light-emitting plane is designated by S, a distance between the light source and the deflection pattern is designated by Rp and a thickness of the light guide plate in positions of the deflection patterns is designate by d, in a certain region on the surface opposite the light-emitting plane, when an average value obtained by adding S(Rp\xd7d) of all the deflection patterns included in all the pixel corresponding regions of the liquid crystal panel is designated by \u03bc\u03b1 and a standard deviation is designated by \u03c3\u03b1, their ratio satisfies the following relationship:
0<\u03c3\u03b1\u03bc\u03b1\u22660.154,
light from the light source introduced into the light guide plate is deflected towards the light-emitting plane by the deflection patterns so as to be emitted from the light-emitting plane.
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 method of treating diabetes, which method involves treating a patient in need thereof with a therapeutically effective amount of a compound of formula (I):
in which:
Ra is hydrogen, halogen, C(1-3)alkyl, C(1-3)alkoxy, hydroxyC(1-3)alkyl, C(1-3)alkylthio, C(1-3)alkylsulphinyl, aminoC(1-3)alkyl, mono- or di-C(1-3)alkylaminoC(1-3)alkyl, C(1-3)alkylcarbonylaminoC(1-3)alkyl, C(1-3)alkoxyC(1-3)alkylcarbonylaminoC(1-3)alkyl, C(1-3)alkylsulphonylaminoC(1-3)alkyl, C(1-3)alkylcarboxy, or C(1-3)alkylcarboxyC(1-3)alkyl;
Rb is hydrogen, halogen, C(1-3)alkyl, or hydroxyC(1-3)alkyl, with the proviso that Ra and Rb are not simultaneously each hydrogen; or
Ra and Rb together are (CH2)n where n is 3 or 4, to form, with the pyrimidine ring carbon atoms to which they are attached a fused 5- or 6-membered carbocyclic ring; or
Ra and Rb together with the pyrimidine ring carbon atoms to which they are attached form a fused benzo or heteroaryl ring unsubstituted or substituted by 1, 2, 3 or 4 substituents which may be the same or different selected from the group consisting of halogen, C(1-4)alkyl, cyano, C(1-4)alkoxy or C(1-4)alkylthio, and mono to perfluoro-C(1-4)alkyl);
Rc is hydrogen or C(1-3)alkyl;
R2 is an aryl or heteroaryl group, unsubstituted or substituted by 1, 2, 3 or 4 substituents which may be the same or different selected from the group consisting of C(1-18)alkyl, C(1-18)alkoxy)C(1-18)alkylthio, arylC(1-18)alkoxy, hydroxy, halogen, CN, COR6, carboxy, COOR6, NR6COR7, CONR8R9, SO2NR8R9, NR6SO2R7, NR8R9, mono to perfluoro-C(1-4)alkyl, mono to perfluoro-C(1-4)alkoxyaryl, and arylC(1-4)alkyl;
R3 is hydrogen, C(1-6)alkyl which may be unsubstituted or substituted by 1, 2 or 3 substituents selected from the group consisting of hydroxy, halogen, OR6, COR6, carboxy, COOR6, CONR8R9, NR8R9, NR8COR9, mono- or di-(hydroxyC(1-6)alkyl)amino and N-hydroxyC(1-6)alkyl-N\u2014C(1-6)alkylamino; or
R3 is Het-C(0-4)alkyl in which Het is a 5- to 7-membered heterocyclyl ring comprising N and optionally O or S, bonded through a carbon ring atom and in which N is unsubstituted or substituted by COR6, COOR6, CONR8R9, or C(1-6)alkyl unsubstituted or substituted by 1, 2 or 3 substituents selected from the group consisting of hydroxy, halogen, OR6, COR6, carboxy, COOR6, CONR8R9 and NR8R9;
R4 is an aryl or a heteroaryl ring unsubstituted or substituted by 1, 2, 3 or 4 substituents which may be the same or different selected from the group consisting of C(1-18)alkyl, C(1-18)alkoxy, C(1-18)alkylthio, arylC(1-18)alkoxy, hydroxy, halogen, CN, COR6, carboxy, COOR6, NR6COR7, CONR8R9, SO2NR8R9, NR6SO2R7, NR8R9, mono to perfluoro-C(1-4)alkyl and mono to perfluoro-C(1-4)alkoxy;
R5 is an aryl or heteroaryl ring which is unsubstituted or substituted by 1, 2, 3 or 4 substituents which may be the same or different selected from the group consisting of C(1-18)alkyl, C(1-18)alkoxy, C(1-18)alkylthio, arylC(1-18)alkoxy, hydroxy, halogen, CN, COR6, carboxy, COOR6, CONR8R9, NR6COR7, SO2NR8R9, NR6SO2R7, NR8R9, mono to perfluoro-C(1-4)alkyl and mono to perfluoro-C(1-4)alkoxy;
R6 and R7 are independently hydrogen or C(1-20)alkyl;
R8 and R9 may be the same or different and are selected from the group consisting of hydrogen and C(1-12)alkyl; or
R8 and R9 together with the nitrogen to which they are attached form a 5- to 7 membered ring optionally containing one or more further heteroatoms which are oxygen, nitrogen or sulphur, and is unsubstituted or substituted by one or two substituents selected from the group consisting of hydroxy, oxo, C(1-4)alkyl, C(1-4)alkylCO, aryl, and aralkyl; or
R8 and R9 may be the same or different and are selected from the group consisting of CH2R10 and CHR11CO2H, or a salt thereof;
R10 is COOH or a salt thereof, COOR12, CONR6R7, CN, CH2OH or CH2OR6;
R11 is an amino acid side chain;
R12 is C(1-4)alkyl or a pharmaceutically acceptable in vivo hydrolysable ester group;
n is 1 to 4;
X is O or S;
Y is (CH2)p(O)q in which p is 1, 2 or 3 and q is 0 or p is 2 or 3 and q is 1; and
Z is O or a bond;
or a pharmaceutically acceptable salt thereof.
2. A method as claimed in claim 1 in which Ra is chloro, bromo, methyl, ethyl, n-propyl, methoxy, hydroxymethyl, hydroxyethyl, methylthio, methylsulphinyl, aminoethyl, dimethylaminomethyl, acetylaminoethyl, 2-(methoxyacetamido)ethyl, mesylaminoethyl, ethylcarboxy, methanesulfonamidoethyl, (methoxyacetamido)ethyl or iso-propylcarboxymethyl.
3. A method as claimed in claim 1 in which Rb is hydrogen or methyl.
4. A method as claimed in claim 1 in which Ra and Rb together with the pyrimidine ring carbon atoms to which they are attached form a fused 5-membered carbocyclic ring or a fused benzo or heteroaryl ring selected from the group consisting of benzo, pyrido and thieno.
5. A method as claimed in claim 1 in which Rc is hydrogen or methyl.
6. A method as claimed in claim 1 in which X is S.
7. A method as claimed in claim 1 in which Y is CH2.
8. A method as claimed in claim 1 in which Z is a direct bond.
9. A method as claimed in claim 1 in which R2 is an aryl group, unsubstituted or substituted by 1, 2, 3 or 4 substituents which are the same or different and are selected from the group consisting of C(1-6)alkyl, C(1-6)alkoxy, C(1-6)alkylthio, hydroxy, halogen, CN, mono to perfluoro-C(1-4)alkyl, mono to perfluoro-C(1-4)alkoxyaryl, and arylC(1-4)alkyl.
10. A method as claimed in claim 1 in which R2 is phenyl, unsubstituted or substituted by halogen.
11. A method as claimed in claim 1 in which R2 is phenyl optionally substituted by one to three fluorine atoms.
12. A method as claimed in claim 1 in which R3 is C(1-3)alkyl substituted by a substituent which is NR8R9; or R3 is Het-C(0-2)alkyl in which Het is a 5- to 7-membered heterocyclyl ring comprising N and in which N is unsubstituted or substituted by C(1-6)alkyl.
13. A method as claimed in claim 1 in which R3 is 2-(diethylamino)ethyl.
14. A method as claimed in claim 1 in which R4 is phenyl.
15. A method as claimed in claim 1 in which R5 is phenyl substituted by trifluoromethyl.
16. A method as claimed in claim 1 in which R4 and R5 together form a 4-(4-trifluoromethylphenyl)phenyl moiety.
17. A method as claimed in claim 1, wherein the compound of formula (I) is a compound of the formula (IA):
in which:
Ra is hydrogen, halogen, C(1-3)alkyl, C(1-3)alkoxy, hydroxyC(1-3)alkyl, C(1-3)alkylthio, C(1-3)alkylsulphinyl, aminoC(1-3)alkyl, mono- or di-C(1 -3)alkylaminoC(1-3)alkyl, C(1-3)alkylcarbonylaminoC(1-3)alkyl, C(1-3)alkoxyC(1-3)alkylcarbonylaminoC(1-3)alkyl, C(1-3)alkylsulphonylaminoC(1-3)alkyl, C(1-3)alkylcarboxy, or C(1-3)alkylcarboxyC(1-3)alkyl;
Rb is hydrogen, halogen, C(1-3)alkyl, or hydroxyC(1-3)alkyl, with the proviso that Ra and Rb are not simultaneously each hydrogen; or
Ra and Rb together are (CH2)n where n is 3 or 4, to form, with the pyrimidine ring carbon atoms to which they are attached a fused 5- or 6-membered carbocyclic ring; or
Ra and Rb together with the pyrimidine ring carbon atoms to which they are attached form a fused benzo or heteroaryl ring unsubstituted or substituted by 1, 2, 3 or 4 substituents which may be the same or different selected from the group consisting of halogen, C(1-4)alkyl, cyano, C(1-4)alkoxy or C(1-4)alkylthio, and mono to perfluoro-C(1-4)alkyl);
Rc is hydrogen or C(1-3)alkyl;
R2 is an aryl or heteroaryl group, unsubstituted or substituted by 1, 2, 3 or 4 substituents which may be the same or different selected from the group consisting C(1-18)alkyl, C(1-18)alkoxy)C(1-18)alkylthio, arylC(1-18)alkoxy, hydroxy, halogen, CN, COR6, carboxy, COOR6, NR6COR7, CONR8R9, SO2NR8R9, NR6SO2R7, NR8R9, mono to perfluoro-C(1-4)alkyl, mono to perfluoro-C(1-4)alkoxyaryl, and arylC(1-4)alkyl;
R3 is hydrogen, C(1-6)alkyl which may be unsubstituted or substituted by 1, 2 or 3 substituents selected from the group consisting of hydroxy, halogen, OR6, COR6, carboxy, COOR6, CONR8R9, NR8R9, NR8COR9, mono- or di-(hydroxyC(1-6)alkyl)amino and N-hydroxyC(1-6)alkyl-N\u2014C(1-6)alkylamino; or
R3 is Het-C(0-4)alkyl in which Het is a 5- to 7-membered heterocyclyl ring comprising N and optionally O or S, bonded through a carbon ring atom and in which N is unsubstituted or substituted by COR6, COOR6, CONR8R9; or C(1-6)alkyl unsubstituted or substituted by 1, 2 or 3 substituents selected from the group consisting of hydroxy, halogen, OR6, COR6, carboxy, COOR6, CONR8R9 and NR8R9;
R4 is an aryl or a heteroaryl ring optionally substituted by 1, 2, 3 or 4 substituents which may be the same or different selected from the group consisting of C(1-18)alkyl, C(1-18)alkoxy, C(1-18)alkylthio, arylC(1-18)alkoxy, hydroxy, halogen, CN, COR6, carboxy, COOR6, NR6COR7, CONR8R9, SO2NR8R9, NR6SO2R7, NR8R9, mono to perfluoro-C(1-4)alkyl and mono to perfluoro-C(1-4)alkoxy;
R5 is an aryl or heteroaryl ring which is unsubstituted or substituted by 1, 2, 3 or 4 substituents which may be the same or different selected from the group consisting of C(1-18)alkyl, C(1-18)alkoxy, C(1-18)alkylthio, arylC(1-18)alkoxy, hydroxy, halogen, CN, COR6, carboxy, COOR6, CONR8R9, NR6COR7, SO2NR8R9, NR6SO2R7, NR8R9, mono to perfluoro-C(1-4)alkyl and mono to perfluoro-C(1-4)alkoxy;
R6 and R7 are independently hydrogen or C(1-20)alkyl;
R8 and R9 may be the same or different and are selected from the group consisting of hydrogen and C(1-12)alkyl; or
R8 and R9 together with the nitrogen to which they are attached form a 5- to 7 membered ring optionally containing one or more further heteroatoms which are oxygen, nitrogen or sulphur, and is unsubstituted or substituted by one or two substituents selected from the group consisting of hydroxy, oxo, C(1-4)alkyl, C(1-4)alkylCO, aryl, and aralkyl; or
R8 and R9 may be the same or different and are selected from the group consisting of CH2R10 and CHR11CO2H, or a salt thereof;
R10 is COOH or a salt thereof, COOR12, CONR6R7, CN, CH2OH or CH2OR6;
R11 is an amino acid side chain;
R12 is C(1-4)alkyl or a pharmaceutically acceptable in vivo hydrolysable ester group;
n is 1 to 4; and
X is O or S.
18. A method as claimed in claim 1, wherein the compound of formula (I) is a compound of formula (IB):
in which:
Ra and Rb together with the pyrimidine ring carbon atoms to which they are attached form a fused 5-membered carbocyclic ring;
R2CH2X is 4-fluorobenzylthio;
R3 is C(1-3)alkyl substituted by NR8R9; or
R3 is Het-C(0-2)alkyl in which Het is a 5- to 7-membered heterocyclyl ring comprising N and in which N is unsubstituted or substituted by C(1-6)alkyl;
R4 and R5 form a 4-(4-trifluoromethylphenyl)phenyl moiety;
R8 and R9 which may be the same or different are selected from the group consisting of hydrogen, or C(1-6)alkyl); and
X is S.
19. A method of treating diabetes, which method involves treating a patient in need thereof with a therapeutically effective amount of a compound which is:
1-(N-(2-(diethylamino)ethyl)-N-(4-(4-trifluoromethylphenyl)benzyl)aminocarbonylmethyl)-2-(4-fluorobenzyl)thio-5-ethylpyrimidin-4-one;
1-(N-(2-(diethylamino)ethyl)-N-(2-(4-trifluoromethylphenyl)pyrid-5-yl-methyl)aminocarbonylmethyl)-2-(4-fluorobenzyl)thio-5-ethylpyrimidin-4-one;
1-(N-(2-(diethylamino)ethyl)-N-(4-(4-trifluoromethylphenyl)benzyl)aminocarbonylmethyl)-2-(4-fluorobenzyl)thio-5,6-trimethylenepyrimidin-4-one;
1-(N-(2-(diethylamino)ethyl)-N-(2-(4-trifluoromethylphenyl)pyrid-5-ylmethyl)aminocarbonylmethyl)-2-(4-fluorobenzyl)thio-5,6-trimethylenepyrimidin-4-one;
1-(N-(2-(diethylamino)ethyl)-N-(2-(4-trifluoromethylphenyl)pyrimid-5-ylmethyl)aminocarbonylmethyl)-2-(4-fluorobenzyl)thio-5,6-trimethylenepyrimidin-4-one;
1-(N-methyl-N-(2-(4-chlorophenyl)benzyl)aminocarbonylmethyl)-2-(4-fluorobenzyl)thio-5-(2-aminoethyl)pyrimidin-4-one;
1-(N-methyl-N-(2-(4-chlorophenyl)benzyl)aminocarbonylmethyl)-2-(4-fluorobenzyl)thio-5-(2-acetamidoethyl)pyrimidin-4-one;
1-(N-(2-(diethylamino)ethyl)-N-(2-(4-chlorophenyl)benzyl)aminocarbonylmethyl)-2-(4-fluorobenzyl)thio-5-(dimethylaminomethyl)pyrimidin-4-one;
1-(N-(2-(diethylamino)ethyl)-N-(4-(4-chlorophenyl)benzyl)aminocarbonylmethyl)-2-(4-fluorobenzyl)thio-5-methylpyrimidin-4-one;
1-(N-methyl-N-(2-(4-trifluoromethylphenyl)pyrid-5-ylmethyl)aminocarbonylmethyl)-2-(4-fluorobenzyl)thio-5-methylpyrimidin-4-one;
1-(N-(2-(diethylamino)ethyl)-N-(4-(4-trifluoromethylphenyl)benzyl)aminocarbonylmethyl)-2-(4-fluorobenzyl)thio-5-methylpyrimidin-4-one;
1-(N-(2-(diethylamino)ethyl)-N-(2-(4-trifluoromethylphenyl)pyrid-5-yl-methyl)aminocarbonylmethyl)-2-(4-fluorobenzyl)thio-5-methylpyrimidin-4-one
1-(N-(2-(diethylamino)ethyl)-N-(2-(4-chlorophenyl)pyrimid-5-yl-methyl)aminocarbonylmethyl)-2-(4-fluorobenzyl)thio-5-methylpyrimidin-4-one;
1-(N-(2-(diethylamino)ethyl)-N-(2-(4-trifluoromethylphenyl)pyrimid-5-ylmethyl)aminocarbonylmethyl)-2-(4-fluorobenzyl)thio-5-methylpyrimidin-4-one;
(\xb1)-1-(N-(2-(diethylamino)ethyl)-N-(1-(4-(4-chlorophenyl)phenyl)ethyl)-aminocarbonylmethyl)-2-(4-fluorobenzyl)thio-5-methylpyrimidin-4-one;
1-(N-(2-(1-piperidino)ethyl)-N-(4-(4-trifluoromethylphenyl)benzyl)aminocarbonylmethyl)-2-(4-fluorobenzyl)thio-5-methylpyrimidin-4-one;
1-(N-methyl-N-(4-(4-trifluoromethylphenyl)benzyl)aminocarbonylmethyl)-2-(4-fluorobenzyl)thio-5-ethylpyrimidin-4-one;
1-(N-(2-(diethylamino)ethyl)-N-(4-(4-chlorophenyl)benzyl)aminocarbonyl-methyl)-2-(4-fluorobenzyl)thio-5-ethylpyrimidin-4-one;
1-(N-methyl-N-(2-(4-trifluoromethylphenyl)pyrid-5-yl-methyl)-aminocarbonylmethyl)-2-(4-fluorobenzyl)thio-5-ethylpyrimidin-4-one;
1-(N-(2-(diethylamino)ethyl)-N-(2-(4-chlorophenyl)pyrimid-5-ylmethyl)-aminocarbonylmethyl)-2-(4-fluorobenzyl)thio-5-ethylpyrimidin-4-one;
1-(N-(2-(diethylamino)ethyl)-N-(2-(4-trifluoromethylphenyl)pyrimid-5-ylmethyl)aminocarbonylmethyl)-2-(4-fluorobenzyl)thio-5-ethylpyrimidin-4-one;
1-(N-(2-(diethylamino)ethyl)-N-(4-(4-chlorophenyl)benzyl)aminocarbonyl-methyl)-2-(4-fluorobenzyl)thio-5-propylpyrimidin-4-one;
1-(N-(2-(diethylamino)ethyl)-N-(4-(4-trifluoromethylphenyl)benzyl)aminocarbonylmethyl)-2-(4-fluorobenzyl)thio-5-propylpyrimidin-4-one;
1-(N-(2-(diethylamino)ethyl)-N-(4-(4-trifluoromethylphenyl)benzyl)aminocarbonylmethyl)-2-(4-fluorobenzyl)thio-5-ethoxycarbonylmethylpyrimidin-4-one;
1-(N-(2-(diethylamino)ethyl)-N-(4-(4-trifluoromethylphenyl)benzyl)aminocarbonylmethyl)-2-(4-fluorobenzyl)thio-5-isopropoxycarbonylmethylpyrimidin-4-one;
1-(N-(2-(diethylamino)ethyl)-N-(4-(4-chlorophenyl)benzyl)aminocarbonyl-methyl)-2-(4-fluorobenzyl)thio-5-hydroxymethylpyrimidin-4-one;
1-(N-(2-(diethylamino)ethyl)-N-(4-(4-trifluoromethylphenyl)benzyl)aminocarbonylmethyl)-2-(4-fluorobenzyl)thio-5-hydroxymethylpyrimidin-4-one;
1-(N-methyl-N-(4-(4-chlorophenyl)benzyl)aminocarbonylmethyl)-2-(4-fluorobenzyl)thio-5-(2-hydroxyethyl)pyrimidin-4-one;
1-(N-(2-(diethylamino)ethyl)-N-(4-(4-chlorophenyl)benzyl)aminocarbonyl-methyl)-2-(4-fluorobenzyl)thio-5-(2-hydroxyethyl)pyrimidin-4-one;
1-(N-(2-(diethylamino)ethyl)-N-(2-(4-trifluoromethylphenyl)pyrid-5-ylmethyl)aminocarbonylmethyl)-2-(4-fluorobenzyl)thio-5-(2-hydroxyethyl)pyrimidin-4-one;
1-(N-(2-(diethylamino)ethyl)-N-(4-(4-trifluoromethylphenyl)benzyl)aminocarbonylmethyl)-2-(4-fluorobenzyl)thio-5-(2-hydroxyethyl)pyrimidin-4-one;
1-(N-(2-(diethylamino)ethyl)-N-(4-(4-trifluoromethylphenyl)benzyl)aminocarbonylmethyl)-2-(4-fluorobenzyl)thio-5,6-dimethylpyrimidin-4-one;
1-(N-(2-(diethylamino)ethyl)-N-(4-(4-chlorophenyl)benzyl)aminocarbonyl-methyl)-2-(4-fluorobenzyl)thio-5,6-trimethylenepyrimidin-4-one;
1-(N-(2-(diethylamino)ethyl)-N-(4-(4-chlorophenyl)benzyl)aminocarbonyl-methyl)-2-(4-fluorobenzyl)thio-5,6-tetramethylenepyrimidin-4-one;
1-(N-(2-(diethylamino)ethyl)-N-(4-(4-trifluoromethylphenyl)benzyl)aminocarbonylmethyl)-2-(4-fluorobenzyl)thio-5,6-tetramethylenepyrimidin-4-one;
1-(N-(2-(diethylamino)ethyl)-N-(2-(4-trifluoromethylphenyl)pyrid-5-ylmethyl)aminocarbonylmethyl)-2-(4-fluorobenzyl)thio-5,6-tetramethylenepyrimidin-4-one;
1-(N-(2-(diethylamino)ethyl)-N-(4-(4-trifluoromethylphenyl)benzyl)aminocarbonylmethyl)-2-(4-fluorobenzyl)thio-5-chloropyrimidin-4-one;
1-(N-(2-(diethylamino)ethyl)-N-(4-(4-chlorophenyl)benzyl)aminocarbonyl-methyl)-2-(4-fluorobenzyl)thio-5-chloropyrimidin-4-one;
1-(N-(2-(diethylamino)ethyl)-N-(2-(4-trifluoromethylphenyl)pyrid-5-ylmethyl)aminocarbonylmethyl)-2-(4-fluorobenzyl)thio-5-chloropyrimidin-4-one;
1-(N-(2-(diethylamino)ethyl)-N-(4-(4-trifluoromethylphenyl)benzyl)aminocarbonylmethyl)-2-(4-fluorobenzyl)thio-5-bromopyrimidin-4-one;
1-(N-(2-(diethylamino)ethyl)-N-(4-(4-chlorophenyl)benzyl)aminocarbonylmethyl)-2-(4-fluorobenzyl)thio-5-bromopyrimidin-4-one;
1-(N-(2-(diethylamino)ethyl)-N-(4-(4-trifluoromethylphenyl)benzyl)aminocarbonylmethyl)-2-(4-fluorobenzyl)thio-5-methoxypyrimidin-4-one;
1-(N-(2-(diethylamino)ethyl)-N-(2-(4-trifluoromethylphenyl)pyrid-5-ylmethyl)aminocarbonylmethyl)-2-(4-fluorobenzyl)thio-5-methoxypyrimidin-4-one;
1-(N-(2-(diethylamino)ethyl)-N-(4-(4-trifluoromethylphenyl)benzyl)aminocarbonylmethyl)-2-(4-fluorobenzyl)thio-5-ethoxypyrimidin-4-one;
1-(N-(2-(diethylamino)ethyl)-N-(2-(4-trifluoromethylphenyl)pyrid-5-ylmethyl)aminocarbonylmethyl)-2-(4-fluorobenzyl)thio-5-ethoxypyrimidin-4-one;
1-(N-(2-(diethylamino)ethyl)-N-(2-(4-trifluoromethylphenyl)pyrid-5-ylmethyl)aminocarbonylmethyl)-2-(4-fluorobenzyl)thio-5-methylthiopyrimidin-4-one;
1-(N-(2-(diethylamino)ethyl)-N-(4-(4-trifluoromethylphenyl)benzyl)aminocarbonylmethyl)-2-(4-fluorobenzyl)thio-5-methylthiopyrimidin-4-one;
1-(N-(2-(diethylamino)ethyl)-N-(4-(4-trifluoromethylphenyl)benzyl)aminocarbonylmethyl)-2-(4-fluorobenzyl)thio-5-methylsulfinylpyrimidin-4-one;
1-(N-(2-(diethylamino)ethyl)-N-(2-(4-trifluoromethylphenyl)pyrid-5-ylmethyl)aminocarbonylmethyl)-2-(4-fluorobenzyl)thio-5-methylsulfinylpyrimidin-4-one;
1-(N-(2-(diethylamino)ethyl)-N-(4-(4-trifluoromethylphenyl)benzyl)aminocarbonylmethyl)-2-(2,3-difluorobenzyl)thio-5,6-trimethylenepyrimidin-4-one;
1-(N-(2-(diethylamino)ethyl)-N-(4-(4-trifluoromethylphenyl)benzyl)aminocarbonylmethyl)-2-(3,4-difluorobenzyl)thio-5,6-trimethylenepyrimidin-4-one;
1-(N-(2-(diethylamino)ethyl)-N-(4-(4-trifluoromethylphenyl)benzyl)aminocarbonylmethyl)-2-(2,3,4-trifluorobenzyl)thio-5,6-trimethylenepyrimidin-4-one;
1-(N-(2-(diethylamino)ethyl)-N-(4-(4-trifluoromethylphenyl)benzyl)aminocarbonylmethyl)-2-(2-fluorobenzyl)thio-5,6-trimethylenepyrimidin-4-one;
1-(N-methyl-N-(4-(4-trifluoromethylphenyl)benzyl)aminocarbonylmethyl)-2-(4-fluorobenzyl)thio-5,6-trimethylenepyrimidin-4-one;
1-(N-(2-(1-piperidino)ethyl)-N-(4-(4-trifluoromethylphenyl)benzyl)aminocarbonylmethyl)-2-(4-fluorobenzyl)thio-5,6-trimethylenepyrimidin-4-one;
1-(N-(2-(diethylamino)ethyl)-N-(3-(4-trifluoromethylphenoxy)benzyl)aminocarbonylmethyl)-2-(4-fluorobenzyl)thio-5,6-trimethylenepyrimidin-4-one;
1-(N-(2-(diethylamino)ethyl)-N-(4-(4-trifluoromethylphenoxy)benzyl)aminocarbonylmethyl)-2-(4-fluorobenzyl)thio-5,6-trimethylenepyrimidin-4-one;
1-(N-(2-(diethylamino)ethyl)-N-(4-(4-trifluoromethylbiphenyl-4-yl)propyl)aminocarbonylmethyl)-2-(4-fluorobenzyl)thio-5,6-trimethylenepyrimidin-4-one;
1-(N-(2-(diethylamino)ethyl)-N-(4-(4-trifluoromethylbiphenyl-4-yl)propyl)aminocarbonylmethyl)-2-(4-fluorobenzyl)thio-5-ethylpyrimidin-4-one;
1-(N-(2-(diethylamino)ethyl)-N-(4-(4-trifluoromethylbiphenyl-4-yloxy)ethyl)aminocarbonylmethyl)-2-(4-fluorobenzyl)thio-5-ethylpyrimidin-4-one;
1-(N-(1-ethylpiperidin-4-yl)-N-(4-(4-trifluoromethylphenyl)benzyl)aminocarbonylmethyl)-2-(4-fluorobenzyl)thio-5,6-trimethylenepyrimidin-4-one;
1-(N-(2-ethylamino-2-methylpropyl)-N-(4-(4-trifluoromethylphenyl)benzyl)aminocarbonylmethyl)-2-(4-fluorobenzyl)thio-5,6-trimethylenepyrimidin-4-one;
N-(2-tert-butylaminoethyl)-N-(4-(4-trifluoromethylphenyl)benzyl)aminocarbonylmethyl)-2-(4-fluorobenzyl)thio-5,6-trimethylenepyrimidin-4-one;
N-(2-diethylaminoethyl)-2-2-(4-fluorobenzylthio)-4-oxo-4H-thieno3,2-dpyrimidin-1-yl-N-(4\u2032-trifluoromethylbiphenyl-4-ylmethyl)acetamide;
N-(2-diethylaminoethyl)-2-2-(4-fluorobenzylthio)-4-oxo-4 H-quinazolin-1-yl-N-(4\u2032-trifluoromethylbiphenyl-4-ylmethyl)acetamide;
ethyl-{2-{2-(4-fluorobenzylthio)-4-oxo-4,5,6,7-tetrahydrocyclopentapyrimidin-1-ylethanoyl}-4\u2032-trifluoromethylbiphenyl-4-ylmethyl)aminoethyl}carbamic acid tert-butyl ester;
1-(N-(1-methylpiperidin-4-yl)-N-(4-(4-trifluoromethylphenyl)benzyl)aminocarbonylmethyl)-2-(4-fluorobenzyl)thio-5,6-trimethylenepyrimidin-4-one;
1-(N-(1-isopropylpiperidin-4-yl)-N-(4-(4-trifluoromethylphenyl)benzyl)aminocarbonylmethyl)-2-(4-fluorobenzyl)thio-5,6-trimethylenepyrimidin-4-one;
1-(N-(1-(2-methoxyethyl)piperidin-4-yl)-N-(4-(4-trifluoromethylphenyl)benzyl)aminocarbonylmethyl)-2-(4-fluorobenzyl)thio-5,6-trimethylenepyrimidin-4-one;
1-(N-(2-(diethylamino)ethyl)-N-(4-(4-trifluoromethylphenyl)benzyl)aminocarbonylmethyl)-2-(4-fluorobenzyl)thio-5-(2-aminoethyl)pyrimidin-4-one;
1-(N-(2-(diethylamino)ethyl)-N-(4-(4-trifluoromethylphenyl)benzyl)aminocarbonylmethyl)-2-(4-fluorobenzyl)thio-5-(2-acetamidoethyl)pyrimidin-4-one;
1-(N-(2-(diethylamino)ethyl)-N-(4-(4-trifluoromethylphenyl)benzyl)aminocarbonylmethyl)-2-(4-fluorobenzyl)thio-5-(2-methanesulfonamidoethyl)pyrimidin-4-one;
1-(N-(2-(diethylamino)ethyl)-N-(4-(4-trifluoromethylphenyl)benzyl)aminocarbonylmethyl)-2-(4-fluorobenzyl)thio-5-(2-(methoxyacetamido)ethyl)pyrimidin-4-one; or
1-(N-(2-(ethylamino)ethyl)-N-(4-(4-trifluoromethylphenyl)benzyl)aminocarbonylmethyl)-2-(4-fluorobenzyl)thio-5,6-trimethylenepyrimidin-4-one; or
a pharmaceutically acceptable salt thereof.
20. A method as claimed in claim 19, wherein the method involves treating a patient in need thereof with a therapeutically effective amount of a compound which is:
1-(N-(2-(diethylamino)ethyl)-N-(4-(4-trifluoromethylphenyl)benzyl)aminocarbonylmethyl)-2-(4-fluorobenzyl)thio-5-ethylpyrimidin-4-one;
1-(N-(2-(diethylamino)ethyl)-N-(2-(4-trifluoromethylphenyl)pyrid-5-ylmethyl)aminocarbonylmethyl)-2-(4-fluorobenzyl)thio-5-ethylpyrimidin-4-one;
1-(N-(2-(diethylamino)ethyl)-N-(4-(4-trifluoromethylphenyl)benzyl)aminocarbonylmethyl)-2-(4-fluorobenzyl)thio-5,6-trimethylenepyrimidin-4-one;
1-(N-(2-(diethylamino)ethyl)-N-(2-(4-trifluoromethylphenyl)pyrid-5-ylmethyl)aminocarbonylmethyl)-2-(4-fluorobenzyl)thio-5,6-trimethylenepyrimidin-4-one; or
1-(N-(2-(diethylamino)ethyl)-N-(2-(4-trifluoromethylphenyl)pyrimid-5-ylmethyl)aminocarbonylmethyl)-2-(4-fluorobenzyl)thio-5,6-trimethylenepyrimidin-4-one; or
a pharmaceutically acceptable salt thereof.
21. A method of treating diabetes, which method involves treating a patient in need thereof with a therapeutically effective amount of 1-(N-(2-(diethylamino)ethyl)-N-(4-(4-trifluoromethylphenyl)benzyl)aminocarbonylmethyl)-2-(4-fluorobenzyl)thio-5,6-trimethylenepyrimidin-4-one, or a pharmaceutically acceptable salt thereof.
22. A method as claimed in claim 21, wherein the method involves treating a patient in need thereof with a therapeutically effective amount of 1-(N-(2-(diethylamino)ethyl)-N-(4-(4-trifluoromethylphenyl)benzyl)aminocarbonylmethyl)-2-(4-fluorobenzyl)thio-5,6-trimethylenepyrimidin-4-one.