Claims
- 1. A compound of the general formula (I)
- 2. A compound according to claim 1, wherein
R23, R24, R25, R26, and R27 independently of each other are selected from the group consisting of halogen, —C(O)OR2, —CN, —CF3, —OCF3, —NO2, —OR2, —NR2R3, C1-6-alkyl-Z-, cycloalkyl-Z-, heterocyclyl-Z-, aryl-Z-, or heteroaryl-Z-, N(R4R5)—C1-6-alkylene-Z-, R6—W1-Z-, R6—W1—N(R4)-Z-, R6—N(R4)-Z, and R6—W1—C1-6-alkylene-Z-.
- 3. A compound according to claim 1, wherein
R4, R5, and R6 independently of each other are selected from the group consisting of hydrogen, aryl, C1-6-alkyl, heteroaryl-C1-6-alkylene-, and aryl-C1-6-alkylene-.
- 4. A compound according to claim 1, wherein
Q is a direct bond, —CH2—, —O—, —S—, —S(O2)—, —C(O)—, —C(O)NH—, —NHC(O)—, —NHC(O)NH—, —NHSO2—, —SO2NH—, —C(O)—O—, —O—C(O)—, —NHSO2NH—, 558
- 5. A compound according to claim 1, wherein
W1 is a direct bond, —O—, —C(O)—, —NH—, —S—, —SO2—, —C(O)NH—, —NHC(O)—, —N(H)CON(H)—, —N(H)SO2—, —SO2N(H)—, —C(O)—O—, —N(H)SO2N(H)—, or —O—C(O)—.
- 6. A compound according to claim 1 wherein
R2 and R3 independently of each other are hydrogen, C1-6-alkyl, aryl-C1-6-alkylene-, heteroaryl-C1-6-alkylene-, C1-6-alkyl-arylene-, C1-6-alkyl-heteroarylene-, heteroaryl, or aryl.
- 7. A compound according to claim 1, wherein
R2 and R3, when attached to the same nitrogen atom, together with said nitrogen atom may form a 3 to 8 membered heterocyclic ring optionally containing one or two further heteroatoms selected from nitrogen, oxygen and sulfur, and optionally containing one or two double bonds.
- 8. A compound according to claim 1, wherein
Z is a direct bond, —O—, —NH—, —NHCH2—, —S—, —SO2—, —C(O)NH—, —NHC(O)—, —N(H)CON(H)—, —N(CH3)CONH—, —N(H)SO2—, —SO2N(H)—, —C(O)—O—, —N(H)SO2N(H)—, or —O—C(O)—.
- 9. A compound according to claim 1, wherein
A1 is 559
- 10. A compound according to claim 1, wherein
L1 is a bond, -D-alkylene-E-, —O—, —S—, —S(O)—, —S(O)2—, —C(O)—, —N(R11)—, or —C(═N—OR12).
- 11. A compound according to claim 1, wherein
D is a direct bond or —O—; E is a direct bond or —O—.
- 12. A compound according to claim 1, wherein
R11 is selected from hydrogen, C1-6-alkyl, aryl, carbamoyl, aryl-C1-6-alkylene-, C1-6-alkyl-NH—C(O)—, aryl-C1-6-alkylene-NH—C(O)—, C1-6-alkyl-SO2—, aryl-C1-6-alkylene-SO2—, aryl-SO2—, SO2—, C1-6-alkyl-C(O)—, aryl-C1-6-alkylene-C(O)—, N(R13)(R14)-C1-6-alkylene-Y—, and R15—W2—C1-6-alkylene-Y—, wherein
Y and W2 independently of each other are a direct bond, —CH2—, —SO2—, —N(H)CO—, —N(H)SO2—, or —O—C(O)—; R13 and R14 independently of each other are selected from hydrogen, aryl, C1-6-alkyl, or aryl-C1-6-alkylene-; or R13 and R14 may be taken together to form a ring having the formula —(CH2)o—X—(CH2)p— bonded to the nitrogen atom to which R13 and R14 are attached, wherein
o and p are independently of each other are 1, 2, 3, or 4; and X is a direct bond, —CH2—, —O—, —S—, —S(O2)—, —C(O)—, —CON(H)—, —NHC(O)—, —NHCON(H)—, —NHSO2—, —SO2N(H)—, —C(O)—O—, —O—C(O)—, —NHSO2NH—, 560wherein
R16 and R17 are selected from hydrogen, aryl, heteroaryl, C1-6-alkyl, C1-6-alkoxy, aryl-C1-6-alkylene-, heteroaryl-C1-6-alkylene-, C1-6-alkyl-arylene-, C1-6-alkyl-heteroarylene-, C1-6-alkoxy-arylene-, C1-6-alkoxy-heteroarylene-, heteroarylaryl-C1-6-alkoxy-, or aryl-C1-6-alkoxy-; and R15 is selected from the group consisting of aryl, heteroaryl, cycloalkyl, heterocyclyl, C1-6-alkyl, or aryl-C1-6alkylene-.
- 13. A compound according to claim 1, wherein
G1 is C1-6-alkyl, C2-6-alkenyl, C2-6-alkynyl, cycloalkyl or heterocyclyl, optionally substituted with one or more substituents selected from the group consisting of —CN, —CF3, —OCF3, —OR18, —NR18R19, C3-10-cycloalkyl and C1-6-alkyl.
- 14. A compound according to claim 1, wherein
G1 is alkyl or cycloalkyl, optionally substituted with one or more substituents selected from the group consisting of —CN, —CF3, —OCF3, —OR18, —NR18R19 and C1-6alkyl, or G1 is aryl optionally substituted with one or more substituents R40, R41, and R42.
- 15. A compound according to claim 1, wherein
G1 is aryl or heteroaryl, optionally substituted with one or more substituents R40, R41, and R42.
- 16. A compound according to claim 1, wherein
G1 is 561wherein R56, R57, R58, R59, and R60, independently of each other, are hydrogen or halogen, —CN, —NO2, C1-6-alkyl, —CHF2, —CF3, —OCF3, —OCHF2, —OCH2CF3, —OCF2CHF2, —S(O)2CF3, —SCF3, —OR61, —NR61R62, —SR61, —NR61S(O)2R62, —S(O)2NR61R62, —S(O)NR61R62, —S(O)R61, —S(O)2R61, —C(O)NR61R62, —OC(O)NR61R62, —NR61C(O)R62, —CH2C(O)NR61R62, —CH2C(O)OR61, —OCH2C(O)NR61R62, —CH2OR61, —CH2NR61R62, —OC(O)R61, —C(O)R61 and —C(O)OR61; or C2-6-alkenyl and C2-6-alkynyl, which may optionally be substituted with one or more substituents selected from —CN, —CF3, —OCF3, —OR6, —NR61R62 and C1-6-alkyl; C3-10-cycloalkyl, C4-8-cycloalkenyl, heterocyclyl, C3-10-cycloalkyl-C1-6-alkylene-, C3-10-cyclo-alkyl-C1-6-alkoxy-, C3-10-cycloalkyloxy, C3-10-cycloalkyl-C1-6-alkylthio-, C3-10-cycloalkylthio, C3-10-cycloalkyl-C2-6-alkenylene-, C3-10-cycloalkyl-C2-6-alkynylene-, C4-8-cycloalke-nyl-C1-6-alkylene-, C4-8-cycloalkenyl-C2-6-alkenylene-, C4-8-cycloalkenyl-C2-6-alkynylene-, heterocyclyl-C1-6-alkylene-, heterocyclyl-C2-6-alkenylene-, heterocyclyl-C2-6-alkynylene-; or aryl, aryloxy, aryloxycarbonyl, aroyl, aryl-C1-6-alkoxy-, aryl-C1-6alkylene-, aryl-C2-6-alkenylene-, aryl-C2-6-alkynylene-, heteroaryl, heteroaryl-C1-6-alkylene-, heteroaryl-C2-4-alkenylene- and heteroaryl-C2-6-alkynylene-, of which the aryl and heteroaryl moieties optionally may be substituted with one or more substituents selected from halogen, —C(O)OR61, —CN, —CF3, —OCF3, —NO2, —OR61, —NR61R62 or C1-6-alkyl, wherein
R61 and R62 independently of each other are hydrogen, C1-6-alkyl, C1-6-alkyl-arylene-, C1-6-alkyl-heteroarylene-, aryl-C1-6-alkylene-, heteroaryl-C1-6-alkylene-, heteroaryl, or aryl; or R61 and R62, when attached to the same nitrogen atom, together with the said nitrogen atom may form a 3 to 8 membered heterocyclic ring optionally containing one or two further heteroatoms selected from nitrogen, oxygen and sulfur, and optionally containing one or two double bonds.
- 17. A compound according to claim 1, wherein
L2 is a direct bond, C1-6-alkylene, C2-4-alkenylene, C2-6-alkynylene, —N—R20—, —C1-6-alkylene-N(R20)—, —C2-6-alkenylene-N(R20)—, or —C2-6-alkynylene-N(R20)—.
- 18. A compound according to claim 1, wherein
R52 and R53 independently of each other are hydrogen, C1-6alkyl, aryl-C1-6-alkylene-heteroaryl-C16-alkylene-heteroaryl, or aryl.
- 19. A compound according to claim 1, wherein
L3 is —C(O)—, —C(O)—C(O)— or —C(O)CH2C(O)—.
- 20. A compound according to claim 1, wherein
R1 is hydrogen, or R1 is C1-6-alkyl, C2-6-alkenyl, C2-6-alkynyl, C3-10-cycloalkyl-W4—, C3-10-heterocyclyl-W4—, C3-10-aryl-W4—, or C4-10-heteroaryl-W4—, optionally substituted with one or more substituents R33, R34, and R35.
- 21. A compound according to claim 1, wherein
R1 is hydrogen, C1-6-alkyl, C2-6-alkenyl, or C2-6-alkynyl, optionally substituted with one or more substituents R33, R34, and R35.
- 22. A compound according to claim 1, wherein
R33, R34, and R35 independently of each other are selected from —CHF2, —CF3, —OCF3, —OCHF2, —OCH2CF3, —OCF2CHF2, —S(O)2CF3, —SCF3, —OR52, —NR52R53, —SR52, —NR52S(O)2R53, —S(O)2NR52R53, —S(O)NR52R53, —S(O)R52, —S(O)2R52, —C(O)NR52R53, —OC(O)NR52R53, —NR52C(O)R53, —CH2C(O)NR52R53, —OCH2C(O)NR52R53, —CH2OR52, —CH2NR52R53, —OC(O)R52, —C(O)R52 and —C(O)OR52.
- 23. A compound according to claim 1, wherein
G2 is heteroaryl, fused heterocyclylheteroaryl, or fused cycloalkylheteroaryl, optionally substituted with one or more substituents R43, R44, and R45, wherein said heteroaryl group posesses a nitrogen atom adjacent to the atom joining G2 with —N(R1)—.
- 24. A compound according to clam 1, wherein
G2 is furanyl, thienyl, thiophenyl, pyrrolyl, imidazolyl, pyrazolyl, triazolyl, tetrazolyl, thiazolyl, oxazolyl, isoxazolyl, oxadiazolyl, thiadiazolyl, isothiazolyl, pyridinyl, pyridazinyl, pyrazinyl, pyrimidinyl, quinolinyl, isoquinolinyl, benzofuranyl, benzothiophenyl, indolyl, or indazolyl, optionally substituted with one or more substituents R43, R44, and R4.
- 25. A compound according to claim 1, wherein
R43, R44, and R45 independently of each other are selected from —CN, —NO2, —SCF3, —OR54, —NR54R55, —SR54, —S(O)2NR54R55, —S(O)NR54R55, —S(O)R54, —S(O)2R54, —C(O)NR54R55, —OC(O)NR54R55, —NR54C(O)R55, halogen, —S-C1-6-alkylene-OR54, —S(O)2—C1-6-alkylene-OR4, —C1-6-alkylene-S—R54, —C1-6-alkylene-S(O)R54, —C1-6-alkylene-S(O)2R54, —C1-6-alkylene-N(R54)S(O)2R55, —N(R54)S(O)2R55, —C1-6alkylene-C(O)NR54R55, —C1-6-alkylene-N(R54)C(O)R55, —N(R54)C(O)R55, —C1-6-alkylene-N(R54)C(O)NR55R56, C1-6-alkylene-NHC(═NR54)NR55R56, —C1-6-alkylene-N(R54)C(O)OR55, —N(R54)C(O)OR55, —C1-6-alkylene-C(O)OR54, —OCH2C(O)NR54RR55, —O(CH2)1-3OR54, —C1-6-alkylene-O—R54, —C1-6-alkylene-C(O)R54, —C1-6-alkylene-NR54R55, —C1-6-alkylene=N—O—R54, —C1-6-alkylene-N(R54)S(O)2NR55R56, —N(R54)S(O)2NR55R56, —N(R54)S(O)2NR55R56, —OC(O)R54, —C(O)N(R54)S(O)2R55, —C1-6-alkylene-C(R54)═N—OR55, —NHC(═NR54)NR55R56, —C1-6-alkylene-N═C(N(R54R55))2, —N═C(N(R54R55))2, —C(O)R54 and —C(O)OR54; or C1-6-alkyl or C2-6-alkenyl, each of which may optionally be substituted with one or more substituents independently selected from halogen, R54, —CN, —CF3, —OCF3, —OR54, —C(O)OR54, —NR54R55 and C1-6-alkyl; or C3-10-cycloalkyl, heterocyclyl, C3-10-cycloalkyl-C1-6-alkylene-, C3-10-cycloalkyl-C1-6-alkoxy-, C3-10-cycloalkyloxy, heterocyclyl-C1-6-alkylene-, of which the heterocyclyl moieties optionally may be substituted with one or more substituents independently selected from R70; or aryl, aryloxy, aryl-C1-6-alkoxy-, aryl-C1-6-alkylene-, heteroaryl, heteroaryl-C1-6-alkylene-, of which the aryl and heteroaryl moieties optionally may be substituted with one or more substituents selected from halogen, —C(O)OR54, —CN, —CF3, —OCF3, —NO2, —OR54, —NR54R55 or C1-6-alkyl.
- 26. A compound according to claim 1, wherein
R54, R55 and R56 independently of each other are hydrogen, C1-6-alkyl, aryl-C1-6-alkylene-, heteroaryl-C1-6-alkylene-, heterocyclyl, heterocyclyl-C1-6-alkylene-, heteroaryl, or aryl, each of which is optionally substituted with one or more substituents independently selected from R71; or
R54 and R55 independently of each other are hydrogen or —(CHR72)u—(CHR73)v—W6, or R54 and R55, when attached to the same nitrogen atom, together with the said nitrogen atom may form a 3 to 8 membered heterocyclic ring optionally containing one or two further heteroatoms selected from nitrogen, oxygen and sulfur, and optionally containing one or two double bonds, and optionally substituted with one or more C1-6-alkyl groups.
- 27. A compound according to claim 1, wherein
R54, R55 and R56 independently of each other are hydrogen, methyl, ethyl, propyl, butyl, isopropyl, isobutyl, sec-butyl, tert-butyl, 3-pentyl, 2-pentyl, or 3-methyl-butyl.
- 28. A compound according to claim 1, wherein
R54, R55 and R56 independently of each other are oxetanyl, tetrahydrofuranyl, tetrahydropyranyl, oxepanyl, azetidyl, pyrrolidyl, piperidyl, hexahydroazepinyl, thietanyl, thiolanyl, tetrahydrothiopyranyl, thiepanyl, 1,4-oxathianyl, 1,3-dioxolanyl, 1,2-dithiolanyl, 1,3-dithiolanyl, hexahydro-pyridazinyl, imidazolidyl, 1,3-dioxanyl, morpholinyl, 1,3-dithianyl, 1,4-dioxanyl, 1,4-dithianyl, or thiomorpholinyl, each of which is optionally substituted with one or more substituents independently selected from R71.
- 29. A compound according to claim 1, wherein
R4, R15 and R56 independently of each other are furanyl, thienyl, thiophenyl, pyrrolyl, imidazolyl, pyrazolyl, triazolyl, tetrazolyl, thiazolyl, oxazolyl, isoxazolyl, oxadiazolyl, thiadiazolyl, isothiazolyl, pyridinyl, pyridazinyl, pyrazinyl, pyrimidinyl, quinolinyl, isoquinolinyl, benzofuranyl, benzothiophenyl, indolyl, purinyl, or indazolyl, each of which is optionally substituted with one or more substituents independently selected from R71.
- 30. A compound according to claim 1, wherein R71 is methyl or ═O.
- 31. A compound according to claim 1, wherein R71 is —C(O)OH.
- 32. A compound according to claim 1, wherein R71 is —(CH2)1-3C(O)OH.
- 33. A compound according to claim 1, wherein R70 is —(CH2)1-3NR75R76.
- 34. A compound according to claim 1, wherein u is 0 or 1.
- 35. A compound according to claim 1, wherein
W6 is —O—R75, —C(O)O—R75, —C(O)—R75, —NR75R76, —NHCH2C(O)R75, —NHC(O)R75, —S(O)2R75, —NHS(O)2R75, or W6 is heterocyclyl.
- 36. A compound according to claim 1 selected from the following:
N-(2-Phenoxyphenyl)-N′-(thiazol-2-yl)urea, N-[2-(2,3-Dimethoxyphenoxy)-5-Fluorophenyl]-N′-(thizol-2-yl)sulfamide, 1-(2-phenoxyphenyl)-5-(thiazol-2-yl)biuret, 2-[([[(2-Phenoxyanilino)sulfonyl]amino]carbonyl)amino]thiazole, N-(2-Phenylsulfanylphenyl)-N′-(thiazol-2-yl)urea, N-(2-Phenylsulfonylphenyl)-N′-(thiazol-2-yl)urea, N-(2-Benzylphenyl)-N′-(thiazol-2-yl)urea, N-(2-Benzoylphenyl)-N′-(thiazol-2-yl)urea, N-[2-(Phenylamino)phenyl]-N′-(thiazol-2-yl)urea N-[2-Fluoro-6-(4-methoxyphenoxy)benzyl]-N′-(thiazol-2-yl)urea, N-(2-Benzyloxyphenyl)-N′-(thiazol-2-yl)urea, N-[2-(2,3,4-Trimethoxybenzyloxy)phenyl]-N′-(thiazol-2-yl)urea, N-(2-Ethoxyphenyl)-N′-(thiazol-2-yl)urea, N-(2-Phenoxyphenyl)-N′-(pyridin-2-yl)urea, N-(2-Phenoxyphenyl)-N′-[(4-methoxycarbonylmethyl)thiazol-2-yl]urea, N-Methyl-N-(2-phenoxyphenyl)-N′-(thiazol-2-yl)urea, N-isopropyl-N-(2-phenoxyphenyl)-N′-(thiazol-2-yl)urea, N-[2-(4-Methoxyphenoxy)phenyl)-N′-(thiazol-2-yl)urea, N-[2-(4-Fluorophenoxy)phenyl]-N′-(thiazol-2-yl)urea, N-[2-(4-Chlorophenoxy)phenyl]-N′-(thiazol-2-yl)urea, N-[2-(4-Cyanophenoxy)phenyl]-N′-thiazolylurea, N-[2-(4-Methoxycarbonylphenoxy)phenyl]-N′-(thiazol-2-yl)urea, N-[2-(4-Isopropylphenoxy)phenyl]-N′-(thiazol-2-yl)urea, N-[2-(3,4-Difluorophenoxy)phenyl]-N′-(thiazol-2-yl)urea, N-[2-(3,4-Dichlorophenoxy)phenyl]-N′-(thiazol-2-yl)urea, N-[2-(4-Chloro-3-methylphenoxy)phenyl]-N′-(thiazol-2-yl)urea, N-[2-(3,4-Dimethoxyphenoxy)phenyl]-N′-(thiazol-2-yl)urea, N-[2-(3,4-Methylenedioxyphenoxy)phenyl]-N′-(thiazol-2-yl)urea, N-[2-(2,4-Dichlorophenoxy)phenyl]-N′-(thiazol-2-yl)urea, N-[2-(2,4-Difluorophenoxy)phenyl]-N′-(thiazol-2-yl)urea, N-[2-(4-Fluoro-2-methoxyphenoxy)phenyl]-N′-(thiazol-2-yl)urea, N-[2-(4-Methoxy-2-methoxycarbonylphenoxy)phenyl]-N′-(thiazol-2-yl)urea, N-[2-(3-Methoxyphenoxy)phenyl]-N′-(thiazol-2-yl)urea, N-[2-(3-Fluorophenoxy)phenyl]-N′-(thiazol-2-yl)urea, N-[2-(3-Trifluoromethylphenoxy)phenyl]-N′-(thiazol-2-yl)urea, N-[2-(2-Methylphenoxy)phenyl]-N′-(thiazol-2-yl)urea, N-[2-(2-Methoxyphenoxy)phenyl]-N′-(thiazol-2-yl)urea, N-[2-(2-Isopropoxyphenoxy)phenyl]-N′-(thiazol-2-yl)urea, N-[2-(2-Fluorophenoxy)phenyl]-N′-(thiazol-2-yl)urea, N-[2-(2-Methylsulfanylphenoxy)phenyl]-N′-(thiazol-2-yl)urea, N-[2-(2-Methylsulfonylphenoxy)phenyl]-N′-thiazolylurea, N-[2-(2-Trifluoromethylphenoxy)phenyl]-N′-(thiazol-2-yl)urea, N-[2-(2,6-Dimethoxyphenoxy)phenyl]-N′-(thiazol-2-yl)urea, N-[2-(2,6-difluorophenoxy)phenyl]-N′-(thiazol-2-yl)urea, N-[2-(2-Fluoro-6-methoxyphenoxy)phenyl]-N′-(thiazol-2-yl)urea, N-[2-(2-Methoxy-6-methoxycarbonylphenoxy)phenyl]-N′-(thiazol-2-yl)urea, N-[(3-methoxy-2-methoxycarbonylphenoxy)phenyl]-N′-(thiazol-2-yl)urea, and N-[2-(2,3-Dimethoxyphenoxy)phenyl]-N′-(thiazol-2-yl)urea.
- 37. A compound according to claim 1 selected from the following:
N-[2-(2,3,4-Trichlorophenoxy)phenyl]-N′-(thiazol-2-yl)urea, N-[2-(2,4,6-Trifluorophenoxy)phenyl]-N′-(thiazol-2-yl)urea, N-[2-(2,4-dichloronaphth-1-oxy)phenyl]-N′-(thiazol-2-yl)urea, N-[2-(2-Methoxyphenoxy)-5-(methylsulfonyl)phenyl]-N′-(thiazol-2-yl)urea, N-[5-Cyano-2-(2-methoxyphenoxy)phenyl]-N′-(thiazol-2-yl)urea, N-[5-Fluoro-2-(2-methylsulfanylphenoxy)phenyl]-N′-thiazolylurea, N-[5-Fluoro-2-(2-fluoro-6-methoxyphenoxy)phenyl]-N′-(thiazol-2-yl)urea, N-[2-(2,3-Dimethoxyphenoxy)-5-fluorophenyl]-N′-(thiazol-2-yl)urea, N-[2-(3,4-Difluorophenoxy)-5-fluorophenyl]-N′-(thiazol-2-yl)urea, N-[5-Fluoro-2-(4-fluorophenoxy)phenyl]-N′-(thiazol-2-yl)urea, N-[2-(2,4-Dichlorophenoxy)-5-fluorophenyl]-N′-(thiazol-2-yl)urea, N-[5-Fluoro-2-(4-methoxyphenoxy)phenyl]-N′-(thiazol-2-yl)urea, N-[5-Fluoro-2-(2-methoxyphenoxy)phenyl]-N′-(thiazol-2-yl)urea, N-[5-Fluoro-2-(2-trifluoromethylphenoxy)phenyl]-N′-(thiazol-2-yl)urea, N-[5-Fluoro-2-(naphth-2-oxy)phenyl]-N′-(thiazol-2-yl)urea, N-[2-(2,3-Dimethoxyphenoxy)-6-fluorophenyl]-N′-(thiazol-2-yl)urea, N-[2-(4-Fluoro-2-methoxyphenoxy)phenyl]-N′-(thiazol-2-yl)urea, N-[2-(2,3-Dimethoxyphenoxy)-4-fluorophenyl]-N′-(thiazol-2-yl)urea, N-[4-Fluoro-2-(2-fluoro-6-methoxyphenoxy)phenyl]-N′-(thiazol-2-yl)urea, N-[2-(2-Fluoro-6-methoxyphenoxy)-4-methoxyphenyl]-N′-(thiazol-2-yl)urea, N-[3-Fluoro-2-(2-fluoro-6-methoxyphenoxy)phenyl]-N′-(thiazol-2-yl)urea, N-[2-(2,3-Dimethoxyphenoxy)-5-methoxyphenyl]-N′-thiazol-2-ylurea, N-[2-(2,3-Dimethoxyphenoxy)-4-methylphenyl]-N′-(thiazol-2-yl)urea, N-[2-(2,3-Dimethoxyphenoxy)-3-methylphenyl]-N′-(thiazol-2-yl)urea, N-[2-(2-Chlorophenoxy)-5-chlorophenyl]-N′-(thiazol-2-yl)urea, N-[5-Chloro-2-(4-chloro-3-methylphenoxy)phenyl]-N′-(thiazol-2-yl)urea, N-[2-(4-Chlorophenoxy)-5-(trifluoromethyl)phenyl]-N′-(thiazol-2-yl)urea, N-[4,5-difluoro-2-(2,3-dimethoxyphenoxy)phenyl]-N′-(thiazol-2-yl)urea, N-[4,5-Dichloro-2-(2,3-dimethoxyphenoxy)phenyl]-N′-(thiazol-2-yl)urea, N-[5-Chloro-2-(2,3-dimethoxyphenoxy)-4-dimethylaminophenyl]-N′-(thiazol-2-yl)urea, N-[5-Chloro-2-(2,3-dimethoxyphenoxy)-4-(4-morpholino)phenyl]-N′-(thiazol-2-yl)urea, N-[2-(2,4-Difluorophenoxy)pyridin-3-yl]-N′-(thiazol-2-yl)urea, N-[2-(2-Fluorophenoxy)pyridin-3-yl]-N′-[thiazol-2-yl]urea, N-[2-(2-Methoxyphenoxy)pyridin-3-yl]-N′-(thiazol-2-yl)urea, N-[2-(2,3-Dimethoxyphenoxy)pyridin-3-yl]-N-(thiazol-2-yl)urea, N-[4-Chloro-2-(2-chlorobenzoyl)phenyl]-N′-(thiazol-2-yl)urea, N-[4-Chloro-2-(2-fluorobenzoyl)phenyl]-N′-(thiazol-2-yl)urea, N-[2-(2,4-Difluorophenylsulfanyl)phenyl]-N′-(thiazol-2-yl)urea, 1-[2-(2-Fluorophenylsulfanyl)phenyl]-3-(thiazol-2-yl)urea, N-[2-(2-Chloro-4-fluorophenylsulfanyl)phenyl]-N′-(thiazol-2-yl)urea, N-[2-(2,3-Dichlorophenylsulfanyl)phenyl]-N′-(thiazol-2-yl)urea, N-[2-(3,5-Dimethylphenylsulfanyl)phenyl]-N′-(thiazol-2-yl)urea, N-[2-(2-Methoxycarbonylphenylsulfanyl)phenyl]-N′-(thiazol-2-yl)urea, N-[2-(2-Methoxyphenylsulfanyl)phenyl]-N′-(thiazol-2-yl)urea, N-[2-(2-Pyridinylsulfanyl)phenyl]-N′-(thiazol-2-yl)urea, N-(2-Propyloxyphenyl)-N′-(thiazol-2-yl)urea, N-(2-Butyloxyphenyl)-N′-(thiazol-2-yl)urea, and N-(2-(Cyclopentyloxyphenyl)-N′-(thiazol-2-yl)urea.
- 38. A compound according to claim 1 selected from the following:
N-(2-Isopropoxyphenyl)-N′-(thiazol-2-yl)urea, N-[2-(2-Methylpropoxy)phenyl]-N′-(thiazol-2-yl)urea, N-[2-(Cyclopentylmethoxy)phenyl]-N′-(thiazol-2-yl)urea, N-[2-(3-pentoxy)phenyl]-N′-(thiazol-2-yl)urea, N-[2-(2-pentoxy)phenyl]-N′-(thiazol-2-yl)urea, N-[2-(2-Methoxyethoxy)phenyl]-N′-(thiazol-2-yl)urea, (2-[3-(2-Benzylphenyl)ureido]thiazol-4-yl)acetic acid, (2-[3-(2-Benzoyl-4-chlorophenyl)ureido]thiazol-4-yl)acetic acid, (2-[3-(2-(2-Methylphenoxy)phenyl)ureido]thiazol-4-yl)acetic acid, (2-[3-(2-(4-Methoxyphenoxy)-5-(trifluoromethyl)phenyl)ureido}thiazol-4-yl)acetic acid, {2-[3-(2-phenoxyphenyl)ureido]thiazol-4-yl}acetic acid, 2-3-[5-Fluoro-2-(2-fluoro-6-methoxyphenoxy)phenyl]ureido}thiazole-4-carboxylic acid, 2-{3-[2-(2,3-Dimethoxyphenoxy)-5-fluorophenyl]ureido}thiazole-4-carboxylic acid ethyl ester, (2-{3-[2-(2,3-Dimethoxyphenoxy)-5-fluorophenyl]ureido}thiazol-4-yl)acetic acid ethyl ester, (2-{3-[5-Fluoro-2-(2-fluoro-6-methoxyphenoxy)phenyl]ureido}thiazol-4-yl)acetic acid, 2-{3-[2-(2,3-Dimethoxyphenoxy)-5-fluorophenyl]ureido}thiazole-4-carboxylic acid, (2-{3-[2-(2,3-Dimethoxyphenoxy)-5-fluorophenyl]ureido}thiazol-4-yl)acetic acid, 2-{3-[5-Fluoro-2-(2-fluoro-6-methoxyphenoxy)phenyl]ureido}-4-methylthiazole-5-carboxylic acid ethyl ester, 2-{3-[5-Fluoro-2-(2-fluoro-6-methoxyphenoxy)phenyl]ureido}-4-methylthiazole-5-carboxylic acid, N-Ethyl-2-(2-{3-[5-fluoro-2-(2-fluoro-6-methoxyphenoxy)phenyl]ureido}thiazol-4-yl)acetamide, 2-(2-{3-[5-Fluoro-2-(2-fluoro-6-methoxyphenoxy)phenyl]ureido}thiazol-4-yl)-N-(2-methoxy-ethyl)acetamide, 2-(2-{3-[5-Fluoro-2-(2-fluoro-6-methoxyphenoxy)phenyl]ureido}thiazol-4-yl)-N-(2-morpholin-4-ylethyl)acetamide, [2-(2-{3-[5-Fluoro-2-(2-fluoro-6-methoxyphenoxy)phenyl]ureido}thiazol-4-yl)acetylamino]acetic acid methyl ester, 2-{3-[2-(2,3-Dimethoxyphenoxy)-5-fluorophenyl]ureido}thiazole-4-carboxylic acid (2-methoxyethyl)amide, [2-(2-{3-[5-Fluoro-2-(2-fluoro-6-methoxyphenoxy)phenyl]ureido}thiazol-4-yl)acetylamino]acetic acid, 2-{3-[2-(2,3-Dimethoxyphenoxy)-5-fluorophenyl]ureido}thiazole-4-carboxylic acid ethylamide, [(2-{3-[2-(2,3-Dimethoxyphenoxy)-5-fluorophenyl]ureido}thiazole-4-carbonyl)amino]acetic acid methyl ester, (5-(3-[5-Fluoro-2-(2-fluoro-6-methoxyphenoxy)phenyl]ureido}-[1,3,4]thiadiazol-2-yl)acetic acid ethyl ester, [(2-{3-[2-(2,3-Dimethoxyphenoxy)-5-fluorophenyl]ureido)thiazole-4-carbonyl)amino]acetic acid, (5-{3-[5-Fluoro-2-(2-fluoro-6-methoxyphenoxy)phenyl]ureido}-[1,3,4]thiadiazol-2-yl)acetic acid, 5-{3-[2-(2,3-Dimethoxyphenoxy)-5-fluorophenyl]ureido}-[1,3,4]thiadiazole-2-carboxylic acid ethyl ester, (5-{3-[2-(2,3-Dimethoxyphenoxy)-5-fluorophenyl]ureido)-[1,3,4]thiadiazol-2-yl) acetic acid ethyl ester, 3-[2-(2-{3-[2-(2,3-Dimethoxyphenoxy)-5-fluorophenyl]ureido}thiazol-4-yl)acetylamino]propionic acid methyl ester, 2-(2-{3-[2-(2,3-Dimethoxyphenoxy)-5-fluorophenyl]ureido}thiazol-4-yl)-N-(2-morpholin-4-ylethyl)acetamide, [(2-{3-[5-Fluoro-2-(2-fluoro-6-methoxyphenoxy)phenyl]ureido}thiazole-4-carbonyl)amino]acetic acid methyl ester, 3-[2-(2-{3-[2-(2,3-Dimethoxyphenoxy)-5-fluorophenyl]ureido}thiazol-4-yl)acetylamino]propionic acid, [(2-{3-[5-Fluoro-2-(2-fluoro-6-methoxyphenoxy)phenyl]ureido}thiazole-4-carbonyl)amino]acetic acid, (R) 3-[(2-{3-[5-Fluoro-2-(2-fluoro-6-methoxyphenoxy)phenyl]ureido}thiazole-4-carbonyl)amino]-2-hydroxy-propionic acid, 2-[(2-{3-[5-Fluoro-2-(2-fluoro-6-methoxyphenoxy)phenyl]ureido}thiazole-4-carbonyl)amino]-3-hydroxy-propionic acid, 1-(2-Cyclopentanecarbonyl-4-methylphenyl)-3-thiazol-2-yl-urea, 1-(2-Isobutyryl-4-methylphenyl)-3-thiazol-2-yl-urea, 1-[5-Fluoro-2-(3-methylbutyryl)phenyl]-3-thiazol-2-yl-urea, 1-[5-Methyl-2-(3-methylbutyryl)phenyl]-3-thiazol-2-yl-urea, [3-Cyclopentanecarbonyl-4-(3-thiazol-2-yl-ureido)phenyl]acetic acid ethyl ester, [3-Cyclopentanecarbonyl-4-(3-thiazol-2-yl-ureido)phenyl]acetic acid, 2-[3-Cyclopentanecarbonyl-4-(3-thiazol-2-yl-ureido)phenyl]-N-methylacetamide, {2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-4-yl}-acetic acid ethyl ester, and {2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-4-yl}acetic acid.
- 39. A compound according to claim 1 selected from the following:
{3-Cyclopentanecarbonyl-4-{3-(4-ethoxycarbonylmethylthiazol-2-yl)-ureido}phenyl)acetic acid ethyl ester, 1-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-3-(5-methanesufonyl-thiazol-2-yl)-urea, 2-[3-(2-Cyclopentanecarbonyl-4-methylphenyl)-ureido]-thiazole-4-carboxylic acid ethyl ester, 2-[3-(2-Cyclopentanecarbonyl-4-methylphenyl)-ureido]-thiazole-4-carboxylic acid, 2-[3-(2-Cyclopentanecarbonyl-4-methylphenyl)-ureido]-thiazole-4-carboxamide, 2-{2-[3-(2-Cyclopentanecarbonyl-4-methylphenyl)-ureido]-thiazole-4-yl}-acetamide, 2-{2-[3-(2-Cyclopentanecarbonyl-4-methylphenyl)-ureido]-thiazol-4-yl}-N-methyl-acetamide, 4-(2-(2-[3-(2-Cyclopentanecarbonyl-4-methylphenyl)-ureido-thiazol-4-yl}-acetyl}-1-methyl-piperazinium chloride, 1-[4-Methyl-2-(2-methylpropoxy)phenyl]-3-thiazol-2-yl-urea, {2-[3-(4-Methyl-2-[2-methylpropoxy]phenyl)-ureido]-thiazol-4-yl}-acetic acid {2-[3-(4-Methyl-2-[2-methylpropoxy]phenyl)-ureido]-thiazol-4-yl}-N-methyl-acetamide, 1-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-3-(4-methyl-thiazol-2-yl)-urea, 1-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-3-(4-methoxymethyl-thiazol-2-yl)-urea, 1-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-3-(4-formyl-thiazol-2-yl)-urea, 1-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-3-(4-hydroxymethyl-thiazol-2-yl)-urea, 1-(4-Chloromethyl-thiazol-2-yl)-3-(2-cyclopentanecarbonyl-4-methyl-phenyl)-urea, 1-(4-Aminomethyl-thiazol-2-yl)-3-(2-cyclopentanecarbonyl-4-methyl-phenyl)-urea, 1-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-3-(4-dimethylaminomethyl-thiazol-2-yl)-urea, N-{2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-4-ylmethyl}-acetamide, 1-4-[2-(tert-Butyl-dimethyl-silanyloxy)-ethyl]-thiazol-2-yl}-3-(2-cyclopentanecarbonyl-4-methyl-phenyl)-urea, Acetic acid 2-[3-(2-cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-4-ylmethyl ester, 1-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-1-methyl-3-thiazol-2-yl-urea, 1-(5-Chloro-thiazol-2-yl)-3-(2-cyclopentanecarbonyl-4-methyl-phenyl)-urea, 1-(5-Bromo-thiazol-2-yl)-3-(2-cyclopentanecarbonyl-4-methyl-phenyl)-urea, 1-(5-Bromo-thiazol-2-yl)-3-(2-cyclopentanecarbonyl-5-fluoro-phenyl)-urea, 2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-4-methyl-thiazole-5-carboxylic acid ethyl ester, 2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-4-methyl-thiazole-5-carboxylic acid, 1-(2′-Amino-[4,4′]bithiazolyl-2-yl)-3-(2-cyclopentanecarbonyl-4-methylphenyl)-urea, 2-{2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-4-yl}-N-methoxy-N-methyl-acetamide, 1-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-3-[4-(2-morpholin-4-yl-2-oxo-ethyl)-thiazol-2-yl]-urea, 2-{2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-4-yl}-N-(4-methyl-piperazin-1-yl)-acetamide, 2-{2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-4-yl}-N-(2-morpholin-4-yl-ethyl)-acetamide, 2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazole-4-carboxylic acid methylamide, 1-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-3-[4-(morpholine-4-carbonyl)-thiazol-2-yl]-urea, N-(2-{2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-4-yl}-acetyl)-methanesulfonamide, N-{2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazole-4-carbonyl)-methanesulfonamide, 1-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-3-4-[3-(2-dimethylamino-ethyl)-ureidomethyl]-thiazol-2-yl}-urea, (3-{2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-4-ylmethyl}-ureido)-acetic acid, {2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-4-ylmethyl)-carbamic acid 2-dimethylamino-ethyl ester hydrochloride salt, N-{2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-4-ylmethyl}-N′,N′-dimethylsulfamide, 3-[{2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-4-ylmethyl)-(2-methoxycarbonyl-ethyl)-amino]-propionic acid methyl ester, ({2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-4-ylmethyl}-methoxycarbonylmethyl-amino)-acetic acid methyl ester, (Carboxymethyl-{2-[3-(2-cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-4-ylmethyl}-amino)-acetic acid, N-{2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-4-ylmethyl)-2-dimethylamino-acetamide, 1-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-3-(4-guanidinomethyl-thiazol-2-yl)-urea, 1-(2-Cyclopentanecarbonyl-4-methy-phenyl)-3-[4-(4-S-methyl-2,5-dioxo-imidazolidin-1-ylmethyl)-thiazol-2-yl]-urea, and 1-(4-[Bis-(3H-imidazol-4-ylmethyl)-amino]-methyl}-thiazol-2-yl)-3-(2-cyclopentanecarbonyl-4-methyl-phenyl)-urea.
- 40. A compound according to claim 1 selected from the following:
1-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-3-[4-(N′,N′,N″,N″-tetramethyl-guanidinomethyl)-thiazol-2-yl]-urea, 2-Amino-ethanesulfonic acid {2-[3-(2-cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-4-ylmethyl)-amide, N-{2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-4-ylmethyl}-2-methanesulfonylamino-acetamide, ([({2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-4-ylmethyl}-carbamoyl)-methyl]-amino)-acetic acid, {[({2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-4-ylmethyl}-carbamoyl)-methyl]-amino}-acetic acid methyl ester, 3-({2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-4-ylmethyl}-sulfamoyl)-propionic acid, N-{2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-4-ylmethyl}-2-methanesulfonyl-acetamide, 1-{2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-4-ylmethyl}-piperidine-S-3-carboxylic acid ethyl ester, 1-2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-4-ylmethyl}-piperidine-S-3-carboxylic acid, ({2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-4-ylmethyl}-amino)-(tetrahydro-pyran-4-yl)-acetic acid methyl ester, ({2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-4-ylmethyl}-amino)-(tetrahydro-pyran-4-yl)-acetic acid, 1-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-3-4-[(2-morpholin-4-yl-ethylamino)-methyl]-thiazol-2-yl}-urea, 1-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-3-(4-morpholin-4-ylmethyl-thiazol-2-yl)-urea, 1-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-3-[4-(3-oxo-piperazin-1-ylmethyl)-thiazol-2-yl]-urea, (4-{2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-4-ylmethyl}-piperazin-1-yl)-acetic acid ethyl ester, (4-(2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-4-ylmethyl}-piperazin-1-yl)-acetic acid, 3-(4-{2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-4-ylmethyl}-piperazin-1-yl)-propionic acid ethyl ester, 3-(4-{2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-4-ylmethyl)-piperazin-1-yl)-propionic acid, (3-{2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-4-ylmethyl}-ureido)-acetic acid, 1-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-3-[4-(2,5-dioxo-imidazolidin-1-ylmethyl)-thiazol-2-yl]-urea, 4-({2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-4-ylmethyl)-sulfamoyl)-benzoic acid, 3-({2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-4-ylmethyl}-sulfamoyl)-propionic acid methyl ester, (2-[3-(2-Cyclopentanecarbonyl-5-methyl-phenyl)-ureido]-thiazol-4-yl}-acetic acid ethyl ester, (2-[3-(2-Cyclopentanecarbonyl-5-methyl-phenyl)-ureido]-thiazol-4-yl)-acetic acid, 2-[3-(2-Cyclopentanecarbonyl-5-fluoro-phenyl)-ureido]-thiazol-4-yl}-acetic acid ethyl ester, {2-[3-(2-Cyclopentanecarbonyl-5-fluoro-phenyl)-ureido]-thiazol-4-yl}-acetic acid, {2-[3-(4-Bromo-2-cyclopentanecarbonyl-phenyl)-ureido]-thiazol-4-yl}-acetic acid ethyl ester, {2-[3-(4-Bromo-2-cyclopentanecarbonyl-phenyl)-ureido]-thiazol-4-yl}-acetic acid, {4-[3-(5-Chloro-thiazol-2-yl)-ureido]-3-cyclopentanecarbonyl-phenyl}-acetic acid ethyl ester, {4-[3-(5-Chloro-thiazol-2-yl)-ureido]-3-cyclopentanecarbonyl-phenyl}-acetic acid, 2-{4-[3-(5-Chloro-thiazol-2-yl)-ureido]-3-cyclopentanecarbonyl-phenyl}-N-(2-methanesulfonyl-ethyl)-acetamide, [2-(3-{2-Cyclopentanecarbonyl-4-[(2-methanesulfonyl-ethylcarbamoyl)-methyl]-phenyl}-ureido]-thiazol-4-yl]-acetic acid ethyl ester, 2-(3-{2-Cyclopentanecarbonyl-4-[2-methanesulfonyl-ethyl carbamoyl)-methyl]-phenyl}-ureido)-thiazol-4-yl-acetic acid, [3-Cyclopentanecarbonyl-4-(3-[1,3,4]thiadiazol-2-yl-ureido)-phenyl]-acetic acid ethyl ester, 1-[2-Cyclopentanecarbonyl-4-(2-morpholin-4-yl-2-oxo-ethyl)-phenyl]-3-thiazol-2-yl-urea, 1-{2-Cyclopentanecarbonyl-4-[2-(4-methyl-piperazin-1-yl)-2-oxo-ethyl]-phenyl)-3-thiazol-2-yl-urea, (2-[3-Cyclopentanecarbonyl-4-(3-thiazol-2-yl-ureido)-phenyl]-acetylamino}-acetic acid, {2-[3-(2-Cyclopentanecarbonyl-4-methylcarbamoylmethyl-phenyl)-ureido]-thiazol-4-yl}-acetic acid, {3-Cyclopentanecarbonyl-4-[3-(4-methylcarbamoylmethyl-thiazol-2-yl)-ureido]-phenyl)-acetic acid ethyl ester, 2-{3-Cyclopentanecarbonyl-4-[3-(4-methylcarbamoylmethyl-thiazol-2-yl)-ureido]-phenyl}-N-methyl-acetamide, 1-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-3-{4-[2-(pyridin-2-yloxy)-ethyl]-thiazol-2-yl}-urea, 1-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-3-4-[2-(pyridin-4-yloxy)-ethyl]-thiazol-2-yl}-urea, 5-(2-(2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-4-yl)ethoxy) nicotinic acid methyl ester, 5-(2-{2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-4-yl)ethoxy) nicotinic acid, 4-(2-{2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-4-yl}ethoxy) benzoic acid methyl ester, 4-(2-{2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-4-yl]ethoxy) benzoic acid, [4-(2-{2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-4-yl}ethoxy)-phenyl]acetic acid methyl ester, and [4-(2-(2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-4-yl}ethoxy)-phenyl]acetic acid.
- 41. A compound according to claim 1 selected from the following:
1-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-3-[4-(2-morpholin-4-yl-ethyl)-thiazol-2-yl]-urea, 1-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-3-{4-[2-(2-morpholin-4-yl-ethylamino)-ethyl]-thiazol-2-yl}-urea, 1-(2-2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-4-yl)-ethyl)-piperidin-3-carboxylic acid ethyl ester, 1-(2-2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-4-yl}-ethyl)-piperidin-3-carboxylic acid, 1-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-3-[4-(2-piperazin-1-yl-ethyl)-thiazol-2-yl]-urea, 1-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-3-{4-[2-(4-methanesufonyl-piperazin-1-yl-ethyl]-thiazol-2-yl}-urea, 1-[4-(2-Amino-ethyl)-thiazol-2-yl]-3-(2-cyclopentanecarbonyl-4-methyl-phenyl)-urea, 3-(2-{-2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-4-yl}-ethyl amino)-propionic acid, (2-{2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-4-yl}-ethyl amino)-acetic acid methyl ester, (2-{-2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-4-yl)-ethyl amino)-acetic acid, N-(2-f-2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-4-yl}-ethyl)-acetamide, N-(2-{-2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-4-yl}-ethyl)-methanesulfonamide, N-(2-{-2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-4-yl}-ethyl)-2-dimethylamino acetamide, N-(2-{2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-4-yl}-ethyl)-succinamic acid, 3-{2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-4-yl}-acrylic acid ethyl ester, 3-{2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-4-yl}-propionic acid ethyl ester, 3-{2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-4-yl}-propionic acid, 4-{2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-4-yl}-but-2-enoic acid ethyl ester, 1-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-3-[4-(1H-imidazol-2-ylsulfanylmethyl)-thiazol-2-yl]-urea, 1-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-3-[4-(1-methyl-1H-tetrazol-5-ylsulfanylmethyl)-thiazol-2-yl]-urea, 1-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-3-[4-(9H-purin-6-ylsufanylmethyl)-thiazol-2-yl]-urea, 1-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-3-[4-(9H-purine-6-sulfonylmethyl)-thiazol-2-yl]-urea, 1-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-3-[4-(pyridin-4-ylsufanylmethyl)-thiazol-2-yl]-urea, 1-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-3-4-(pyridine-4-sulfonylmethyl)-thiazol-2-yl]-urea, (5-{2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-4-ylmethylsulfanyl}-tetrazol-1-yl)-acetic acid, (5-{2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-4-ylmethylsulfanyl}-4-cyclopropyl-4H-[1,2,4]triazol-3-ylmethyl)-carbamic acid tert-butyl ester, 1-[4-(5-Aminomethyl-4-cyclopropyl-4H-[1,2,4]triazol-3-ylsulfanylmethyl)-thiazol-2-yl]-3-(2-cyclopentanecarbonyl-4-methyl-phenyl)-urea hydrochloride salt, 2-{2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-4-ylmethylsulfanyl}-1H-imidazole-4-carboxylic acid ethyl ester, 2-{2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-4-ylmethylsulfanyl}-1H-imidazole-4-carboxylic acid, 2-{2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-4-ylmethanesulfonyl}-1H-imidazole-4-carboxylic acid ethyl ester, 2-{2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-4-ylmethanesulfonyl}-1H-imidazole-4-carboxylic acid, 4-Amino-2-{2-[3-(2-cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-4-ylmethylsulfanyl}-pyrimidine-5-carboxylic acid ethyl ester, 4-Amino-2-{2-[3-(2-cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-4-ylmethylsulfanyl}-pyrimidine-5-carboxylic acid, 2-{2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-4-ylmethylsulfanyl}-4-hydroxy-pyrimidine-5-carboxylic acid, 1-[4-(5-Amino-thiazol-2-ylsufanylmethyl)-thiazol-2-yl]-3-(2-cyclopentanecarbonyl-4-methyl-phenyl)-urea, {2-[3-(2-Cyclopentanecarbonyl-5-methanesulfonylamino-4-methyl-phenyl)-ureido]-thiazol-4-yl}-acetic acid ethyl ester, {2-[3-(2-Cyclopentanecarbonyl-5-methanesulfonylamino-4-methyl-phenyl)-ureido]-thiazol-4-yl}-acetic acid, 1-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-3-{4-[2-(1H-imidazol-2-ylsulfanyl)-ethyl]-thiazol-2-yl}-urea, 1-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-3-{4-[2-(1-methyl-1H-imidazol-2-ylsulfanyl)-ethyl]-thiazol-2-yl}-urea, 1-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-3-{4-[2-(pyridin-2-ylsulfanyl)-ethyl]-thiazol-2-yl}-urea, 1-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-3-14-[2-(pyridin-4-ylsulfanyl)-ethyl]-thiazol-2-yl)-urea, 3-{2-[3-(2-Acetyl-4-methyl-phenyl)-ureido]-thiazol-4-ylmethylsulfanyl}-propionic acid, 1-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-3-(5-methylsulfanyl-thiazol-2-yl)-urea, {2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-5-ylsulfanyl)-acetic acid methyl ester, (2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-5-ylsulfanyl)-acetic acid, 12-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazole-5-sulfonyl}-acetic acid methyl ester, {2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazole-5-sulfonyl)-acetic acid, and 3-{2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-5-ylsulfanyl}-propionic acid methyl ester.
- 42. A compound according to claim 1 selected from the following:
3-(2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-5-ylsulfanyl}-propionic acid, 3-{2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazole-5-sulfonyl)-propionic acid methyl ester, 3-(2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazole-5-sulfonyl)-propionic acid, N-(2-{2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-5-yl-sulfanyl)-ethyl)-acetamide, N-(2-{2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-5-yl-sulfonyll}-ethyl)-acetamide, 2-Acetylamino-3-{2-[3-(2-cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-5-ylsulfanyl)-propionic acid methyl ester, 2-Acetylamino-3-12-[3-(2-cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-5-ylsulfanyl)-propionic acid, 2-tert-Butoxycarbonylamino-3-{2-[3-(2-cyclopentanecarbonyl-4-methyl-phenyl)-ureido]thiazol-5-ylsulfanyl}-propionic acid methyl ester, (2-{2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-5-ylsulfanyl}-ethyl)-carbamic acid tert-butyl ester, 2-(2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-5-ylsulfanyl}-ethyl-ammonium; chloride, (2-{2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazole-5-sulfonyl}-ethyl) carbamic acid tert-butyl ester, 2-{2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazole-5-sulfonyl}-ethyl ammonium; chloride, 1-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-3-[5-(2-dimethylamino-ethylsufanyl)-thiazol-2-yl]-urea, 1-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-3-[5-(2-hydroxy-ethylsufanyl)-thiazol-2-yl]-urea, 1-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-3-[5-(2-hydroxy-ethylsulfonyl)-thiazol-2-yl]-urea, 1-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-3-[5-(pyridin-2-ylsulfanyl)-thiazol-2-yl]-urea, 1-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-3-[5-(pyridine-2-sulfonyl)-thiazol-2-yl]-urea, 1-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-3-[5-(pyrimidin-2-ylsulfanyl)-thiazol-2-yl]-urea, 1-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-3-[5-(pyrimidin-2-ylsulfonyl)-thiazol-2-yl]-urea, 1-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-3-[5-(pyridin-4-ylsulfanyl)-thiazol-2-yl]-urea, 1-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-3-[5-(1-methyl-1H-imidazol-2-ylsulfanyl)-thiazol-2-yl]-urea, 1-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-3-[5-(1H-imidazol-2-ylsulfanyl)-thiazol-2-yl]-urea, 1-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-3-[5-(7H-purin-6-ylsulfanyl)-thiazol-2-yl]-urea, 2-{2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-5-ylsulfanyl}-nicotinic acid methyl ester, 2-{2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-5-ylsulfanyl}-nicotinic acid, 2-{2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-5-ylsulfonyl}-nicotinic acid methyl ester, 2-{2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-5-ylsulfonyll}-nicotinic acid, 6-{2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-5-ylsulfanyl}-nicotinic acid methyl ester, 6-{2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-5-ylsulfanyl}-nicotinic acid, 6-{2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-5-ylsulfonyl}-nicotinic acid methyl ester, 3-{2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-5-ylsulfanyl}-pyridine-2-carboxylic acid methyl ester, 3-{2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-5-ylsulfanyl}-pyridine-2-carboxylic acid, 2-{2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-5-ylsulfanyl}-1H-imidazole-4-carboxylic acid ethyl ester, 2-{2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-5-ylsulfanyl}-1H-imidazole-4-carboxylic acid, 2-{2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-5-ylsulfonyl}-1H-imidazole-4-carboxylic acid ethyl ester, 2-{2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-5-ylsulfonyl}-1H-imidazole-4-carboxylic acid, (3-Cyclopentanecarbonyl-4-{3-[5-(pyridin-2-ylsulfanyl)-thiazol-2-yl]-ureido}-phenyl)-acetic acid ethyl ester, (3-Cyclopentanecarbonyl-4-{3-[5-(pyridin-2-ylsulfanyl)-thiazol-2-yl]-ureido}-phenyl)-acetic acid, (3-Cyclopentanecarbonyl-4-{3-[5-(1H-imidazol-2-ylsulfanyl)-thiazol-2-yl]-ureido}-phenyl)acetic acid ethyl ester, (3-Cyclopentanecarbonyl-4-{3-[5-(1H-imidazol-2-ylsulfanyl)-thiazol-2-yl]-ureido}-phenyl)-acetic acid, 1-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-3-[5-(1-methyl-1H-tetrazol-5-ylsulfanyl)-thiazol-2-yl]-urea, (5-{2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-5-ylsulfanyl}-tetrazol-1-yl)-acetic acid, 1-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-3-{5-[1-(2-dimethylamino-ethyl)-1H-tetrazol-5-ylsulfanyl]-thiazol-2-yl}-urea, 1-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-3-[5-(4H-[1,2,4]triazol-3-ylsulfanyl)-thiazol-2-yl]-urea, 1-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-3-[5-(4-methyl-4H-[1,2,4]triazol-3-ylsulfanyl)-thiazol-2-yl]-urea, 1-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-3-[5-(4-methyl-4H-[1,2,4]triazole-3-sulfonyl)-thiazol-2-yl]-urea, (4-{2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-5-yl sulfanyl}-phenyl)-acetic acid, and 1-(5-Acetyl-4-methyl-thiazol-2-yl)-3-(2-cyclopentanecarbonyl-4-methyl-phenyl)-urea.
- 43. A compound according to claim 1 selected from the following:
1-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-3-(5-nitro-thiazol-2-yl)-urea, 1-(4-tert-Butyl-thiazol-2-yl)-3-(2-cyclopentanecarbonyl-4-methyl-phenyl)-urea, 1-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-3-pyridin-2-yl-urea, 1-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-3-(5-formyl-thiazol-2-yl)-urea, 1-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-3-[5-(hydroxyimino-methyl)-thiazol-2-yl]-urea, {2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-5-ylmethyleneaminooxy}-acetic acid, ({2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-5-ylmethyl}-amino)-acetic acid methyl ester, 3-{2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-5-yl}-acrylic acid ethyl ester, 3-{2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-5-yl}-propionic acid ethyl ester, 1-[2-(2-Methoxy-benzoyl)-5-methyl-phenyl]-3-thiazol-2-yl-urea, 1-[2-(2-Methoxy-benzoyl)-4-methyl-phenyl]-3-thiazol-2-yl-urea, 1-[5-Fluoro-2-(2-methoxy-benzoyl)-phenyl]-3-thiazol-2-yl-urea, 1-[5-Fluoro-2-(thiophene-2-carbonyl)-phenyl]-3-thiazol-2-yl-urea, N-[2-(2-Methoxy-benzoyl)-5-methoxy-phenyl]-N′-(thiazol-2-yl)urea, (2-{3-[2-(2-Methoxy-benzoyl)-5-methyl—phenyl]-ureido}-thiazol-4-yl)-acetic acid ethyl ester, (2-{3-[2-(2-Methoxy-benzoyl)-5-methyl-phenyl]-ureido}-thiazol-4-yl)-acetic acid, 2-(2-{3-[2-(2-Methoxy-benzoyl)-5-methyl-phenyl]-ureido}-thiazol-4-yl)-N-methyl-acetamide, 2-(2-{3-[2-(2-Methoxy-benzoyl)-5-methyl-phenyl]-ureido}-thiazol-4-yl)-N-(methoxy-ethyl)-acetamide, N-(2-Methanesulfonyl-ethyl)-2-(2-{3-[2-(2-methoxy-benzoyl)-5-methyl-phenyl]-ureido}-thiazol-4-yl)-acetamide, (2-{3-[5-Fluoro-2-(2-Methoxy-benzoyl)-phenyl]-ureido-thiazol-4-yl)-acetic acid ethyl ester, (2-{3-[5-Fluoro-2-(2-methoxy-benzoyl)-phenyl]-ureido}-thiazol-4-yl)-acetic acid, 2-(2-(3-[5-Fluoro-2-(2-methoxy-benzoyl)-phenyl]-ureido}-thiazol-4-yl)-N-methyl-acetamide, 2-(2-{3-[5-Fluoro-2-(2-methoxy-benzoyl)-phenyl]-ureido}-thiazol-4-yl)-N-(2-methoxy-ethyl)-acetamide, 1-[2-(Hydroxyimino-phenyl-methyl)-phenyl]-3-thiazol-2-yl-urea, 1-[5-Chloro-2-(hydroxyimino-phenyl-methyl)-phenyl]-3-thiazol-2-yl-urea, 1-(2-Benzoyl-5-methyl-phenyl)-3-thiazol-2-yl-urea, 1-[4-Bromo-2-(2-fluoro-benzoyl)-phenyl]-3-thiazol-2-yl-urea, 1-[5-Chloro-2-(2-fluoro-benzoyl)-phenyl]-3-thiazol-2-yl-urea, 1-[4-Fluoro-2-(2-methylsulfanyl-phenoxy)-phenyl]-3-thiazol-2-yl-urea, 2-[4-Fluoro-2-(3-thiazol-2-yl-ureido)-phenoxy]-6-methoxy-benzoic acid methyl ester, 2-[4-Fluoro-2-(3-thiazol-2-yl-ureido)-phenoxy]-6-methoxy-N-methyl-benzamide, 1-[5-Fluoro-2-(2-methanesulfonyl-phenoxy)-phenyl]-3-thiazol-2-yl-urea, 1-[2-(4,5-Dimethoxy-2-methyl-phenoxy)-phenyl]-3-thiazol-2-yl-urea, 3-[4-Fluoro-2-(3-thiazol-2-yl-ureido)-phenoxy]-benzoic acid methyl ester, 3-[4-Fluoro-2-(3-thiazol-2-yl-ureido)-phenoxy]-benzoic acid, 2-[4-Fluoro-2-(3-thiazol-2-yl-ureido)-phenoxy]-benzoic acid methyl ester, 2-[4-Fluoro-2-(3-thiazol-2-yl-ureido)-phenoxy]-N-methyl-benzamide, N-{3-[4-Fluoro-2-(3-thiazol-2-yl-ureido)-phenoxy]-2-methoxy-phenyl}-methanesulfonamide, N-[4-(2-Fluoro-6-methoxy-phenoxy)-3-(3-thiazol-2-yl-ureido)-phenyl]-acetamide, N-[4-(2-Fluoro-6-methoxy-phenoxy)-3-(3-thiazol-2-yl-ureido)-phenyl]-methanesulfonamide, (2-{3-[2-(2-Fluoro-6-methoxy-phenoxy)-5-methanesulfonylamino-phenyl]-ureido}-thiazol-4 yl)-acetic acid ethyl ester, (2-{3-[2-(2-Fluoro-6-methoxy-phenoxy)-5-methanesulfonylamino-phenyl]-ureido}-thiazol-4-yl)-acetic acid, N,N-[4-(2-Fluoro-6-methoxy-phenoxy)-3-(3-thiazol-2-yl-ureido)-phenyl]dimethanesulfonamide, N-[4-Isobutoxy-3-(3-thiazol-2-yl-ureido)-phenyl]-methanesulfonamide, 1-[5-Amino-2-(2-fluoro-6-methoxy-phenoxy)-phenyl]-3-thiazol-2-yl-urea, Pyridine-2-carboxylic acid [4-(2-fluoro-6-methoxy-phenoxy)-3-(3-thiazol-2-yl-ureido)-phenyl]-amide, N-[4-(2-Fluoro-6-methoxy-phenoxy)-3-(3-thiazol-2-yl-ureido)-phenyl]-isonicotinamide, and 5-Methyl-pyrazine-2-carboxylic acid [4-(2-fluoro-6-methoxy-phenoxy)-3-(3-thiazol-2-yl-ureido)-phenyl]-amide.
- 44. A compound according to claim 1 selected from the following:
2,2,2-Trifluoro-ethanesulfonic acid [4-(2-fluoro-6-methoxy-phenoxy)-3-(3-thiazol-2-yl-ureido)-phenyl]-amide, N-[4-(2-Fluoro-6-methoxy-phenoxy)-3-(3-thiazol-2-yl-ureido)-phenyl]-C-methanesulfonyl-methanesulfonamide, 1-Methyl-1H-imidazole-4-sulfonic acid [4-(2-fluoro-6-methoxy-phenoxy)-3-(3-thiazol-2-yl-ureido)-phenyl]-amide, 1,2-Dimethyl-1H-imidazole-4-sulfonic acid [4-(2-fluoro-6-methoxy-phenoxy)-3-(3-thiazol-2-yl-ureido)-phenyl]-amide, 1-[2-(2-Fluoro-6-methoxy-phenoxy)-5-methylamino-phenyl]-3-thiazol-2-yl-urea, 1-[2-(2-Fluoro-6-methoxy-phenoxy)-5-(1-methyl-3-thiazol-2-yl-ureido)-phenyl]-3-thiazol-2-yl-urea, 1-[5-Dimethylamino-2-(2-fluoro-6-methoxy-phenoxy)-phenyl]-3-thiazol-2-yl-urea, 1-2-(2-Fluoro-6-methoxy-phenoxy)-5-[(pyridin-3-ylmethyl)-amino]-phenyl}-3-thiazol-2-yl-urea, 1-[5-(Di-pyridin-2-yl-amino)-2-(2-fluoro-6-methoxy-phenoxy)-phenyl]-3-thiazol-2-yl-urea, Propane-1-sulfonic acid [4-(2-fluoro-6-methoxy-phenoxy)-3-(3-thiazol-2-yl-ureido)-phenyl]-amide, N-[4-(2-Fluoro-6-methoxy-phenoxy)-3-(3-thiazol-2-yl-ureido)-phenyl]-C-phenyl methanesulfonamide, N-{4-[4-(2-Fluoro-6-methoxy-phenoxy)-3-(3-thiazol-2-yl-ureido)-phenylsulfamoyl]-phenyl}-acetamide, 1-{2-(2-Fluoro-6-methoxy-phenoxy)-5-[(5-methyl-3H-imidazol-4-ylmethyl)-amino]-phenyl}-3-thiazol-2-yl-urea, 4-Acetyl-N-[4-(2-fluoro-6-methoxy-phenoxy)-3-(3-thiazol-2-yl-ureido)-phenyl]-benzenesulfonamide, 4-Cyano-N-[4-(2-fluoro-6-methoxy-phenoxy)-3-(3-thiazol-2-yl-ureido)-phenyl]benzenesulfonamide, N-[4-(2-Fluoro-6-methoxy-phenoxy)-3-(3-thiazol-2-yl-ureido)-phenyl]-4-isopropyl-benzenesulfonamide, N-(5-[4-(2-Fluoro-6-methoxy-phenoxy)-3-(3-thiazol-2-yl-ureido)-phenylsulfamoyl]-4-methyl-thiazol-2-yl)-acetamide, 5-Bromo-6-chloro-pyridine-3-sulfonic acid [4-(2-fluoro-6-methoxy-phenoxy)-3-(3-thiazol-2-yl-ureido)-phenyl]-amide, 3,5-Dimethyl-isoxazole-4-sulfonic acid [4-(2-fluoro-6-methoxy-phenoxy)-3-(3-thiazol-2-yl-ureido)-phenyl]-amide, 5-Chloro-1,3-dimethyl-1H-pyrazole-4-sulfonic acid [4-(2-fluoro-6-methoxy-phenoxy)-3-(3-thiazol-2-yl-ureido)-phenyl]-amide, 6-Morpholin-4-yl-pyridine-3-sulfonic acid [4-(2-fluoro-6-methoxy-phenoxy)-3-(3-thiazol-2-yl-ureido)-phenyl]-amide, 6-Oxazol-5-yl-pyridine-3-sulfonic acid [4-(2-fluoro-6-methoxy-phenoxy)-3-(3-thiazol-2-yl-ureido)-phenyl]-amide, 2-(2-(3-[2-(2-Fluoro-6-methoxy-phenoxy)-5-methanesulfonylamino-phenyl]-ureido}-thiazol-4-yl)-N-methyl-acetamide, [4-(2-Fluoro-6-methoxy-phenoxy)-3-(3-thiazol-2-yl-ureido)-phenyl]-carbamic acid tert-butyl ester, 1-(4-Methyl-2-propoxy-phenyl)-3-thiazol-2-yl-urea, 1-(2-Butoxy-4-methyl-phenyl)-3-thiazol-2-yl-urea, 1-[4-Methyl-2-(3-methyl-butoxy)-phenyl]-3-thiazol-2-yl-urea, 1-(2-Allyloxy-4-methyl-phenyl)-3-thiazol-2-yl-urea, 1-[4-Methyl-2-(2-methyl-allyloxy)-phenyl]-3-thiazol-2-yl-urea, 1-[4-Methyl-2-(3-methyl-but-2-enyloxy)-phenyl]-3-thiazol-2-yl-urea, 1-(2-Isopropoxy-4-methyl-phenyl)-3-thiazol-2-yl-urea, 1-(2-Cyclopentyloxy-4-methyl-phenyl)-3-thiazol-2-yl-urea, 1-(2-Cyclopropylmethoxy-4-methyl-phenyl)-3-thiazol-2-yl-urea, 1-[4-Methyl-2-(tetrahydro-pyran-2-ylmethoxy)-phenyl]-3-thiazol-2-yl-urea, 1-[4-Methyl-2-(tetrahydro-furan-2-ylmethoxy)-phenyl]-3-thiazol-2-yl-urea, 1-(2-Cyclopentylmethoxy-4-methyl-phenyl)-3-thiazol-2-yl-urea, {2-[3-(2-Cyclopropylmethoxy-4-methyl-phenyl)-ureido]-thiazol-4-yl}-acetic acid, {2-[3-(2-Cyclopentyloxy-4-methyl-phenyl)-ureido]-thiazol-4-yl}-acetic acid, 1-(2-Isobutoxy-4-methanesulfonylmethyl-phenyl)-3-thiazol-2-yl-urea, (2-{2-[3-(2-Isobutoxy-4-methyl-phenyl)-ureido]-thiazol-4-yl}-acetylamino)-acetic acid, 1-(5-Formyl-2-isobutoxy-phenyl)-3-thiazol-2-yl-urea, 2-{2-[3-(2-Isobutoxy-4-methyl-phenyl)-ureido]-thiazol-4-yl}-N-(2-methoxy-ethyl)-acetamide, 1-(5-Fluoro-2-isobutoxy-4-methyl-phenyl)-3-thiazol-2-yl-urea, 1-(5-Fluoro-2-isobutoxy-phenyl)-3-thiazol-2-yl-urea, 1-(2-Isobutylsulfanyl-4-methyl-phenyl)-3-thiazol-2-yl-urea, {2-[3-(2-Isobutylsulfanyl-4-methyl-phenyl)-ureido]-thiazol-4-yl}-acetic acid ethyl ester, 1-(2-Cyclopentanesulfinyl-4-methyl-phenyl)-3-thiazol-2-yl-urea, and 1-(2-Cyclopentanesulfonyl-4-methyl-phenyl)-3-thiazol-2-yl-urea.
- 45. A compound according to claim 1 selected from the following:
{2-[3-(2-Cyclopentanesulfonyl-4-methyl-phenyl)-ureido]-thiazol-4-yl}-acetic acid ethyl ester, {2-[3-(2-Cyclopentanesulfonyl-4-methyl-phenyl)-ureido]-thiazol-4-yl}-acetic acid, 2-{2-[3-(2-Cyclopentanesulfonyl-4-methyl-phenyl)-ureido]-thiazol-4-yl}-N-methyl-acetamide, 2-{2-[3-(2-Cyclopentanesulfonyl-4-methyl-phenyl)-ureido]-thiazol-4-yl}-N-(2-methoxy-ethyl)-acetamide, 1-(2-Cyclopentylamino-4-methyl-phenyl)-3-thiazol-2-yl-urea, 1-(2-Isobutylamino-4-methyl-phenyl)-3-thiazol-2-yl-urea, 1-[4-Methyl-2-(methyl-propyl-amino)-phenyl]-3-thiazol-2-yl-urea, 1-[2-(Butyl-methyl-amino)-4-methyl-phenyl]-3-thiazol-2-yl-urea, 1-(2-Diethylamino-4-methyl-phenyl)-3-thiazol-2-yl-urea, 1-[2-(Cyclopropylmethyl-propyl-amino)-4-methyl-phenyl]-3-thiazol-2-yl-urea, 1-[2-(Isobutyl-methyl-amino)-4-methyl-phenyl]-3-thiazol-2-yl-urea, (2-{3-[2-(Isobutyl-methyl-amino)-4-methyl-phenyl]-ureido}-thiazol-4-yl)-acetic acid ethyl ester, 2-(2-{3-[2-(Isobutyl-methyl-amino)-4-methyl-phenyl]-ureido}-thiazol-4-yl)-N-methyl-acetamide, 2-(2-{3-[2-(Isobutyl-methyl-amino)-4-methyl-phenyl]-ureido}-thiazol-4-yl)-N-(2-methoxy-ethyl)-acetamide, 1-(4-Methyl-2-pyrrolidin-1-yl-phenyl)-3-thiazol-2-yl-urea, 1-[2-(2,3-Dihydro-indol-1-yl)-5-fluoro-phenyl]-3-thiazol-2-yl-urea, 1-(4-Methyl-2-piperidin-1-yl-phenyl)-3-thiazol-2-yl-urea, {2-[3-(4-Methyl-2-piperidin-1-yl-phenyl)-ureido]-thiazol-4-yl)-acetic acid, 1-[2-(2-Fluoro-6-methoxy-phenoxy)-4-methyl-phenyl]-3-thiazol-2-yl-urea, 1-[2-(2-Fluoro-6-methoxy-phenoxy)-4-(4-methyl-piperazin-1-ylmethyl)-phenyl]-3-thiazol-2-yl-urea, (2-(3-[2-(2-Fluoro-6-methoxy-phenoxy)-4-methyl-phenyl]-ureido)-thiazol-4-yl)-acetic acid, 1-[2-(2-Fluoro-6-methoxy-phenoxy)-5-formyl-phenyl]-3-thiazol-2-yl-urea, 1-[2-(2-Fluoro-6-methoxy-phenoxy)-5-morpholin-4-ylmethyl-phenyl]-3-thiazol-2-yl-urea, 1-[2-(2-Fluoro-6-methoxy-phenoxy)-5-methanesulfonylmethyl-phenyl]-3-thiazol-2-yl-urea, (5-Chloro-2-[3-(2-cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-4-yl)-acetic acid ethyl ester, {5-Bromo-2-[3-(2-cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-4-yl}-acetic acid ethyl ester, {5-Chloro-2-[3-(2-cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-4-yl}-acetic acid, {5-Bromo-2-[3-(2-cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-4-yl}-acetic acid, Bromo-{2-[3-(2-cyclopentanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-4-yl}-acetic acid ethyl ester, {2-[3-(2-Cyclopentanecarbonyl-phenyl)-ureido]-thiazol-4-yl)-acetic acid ethyl ester, (2-[3-(2-Cyclopentanecarbonyl-phenyl)-ureido]-thiazol-4-yl)-acetic acid, (2-[3-(2-Cyclopentanecarbonyl-4-methoxy-phenyl)-ureido]-thiazol-4-yl}-acetic acid ethyl ester, (2-[3-(2-Cyclopentanecarbonyl-4-methoxy-phenyl)-ureido]-thiazol-4-yl}-acetic acid, {2-[3-(2-Cyclopropanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-4-yl}-acetic acid ethyl ester, {2-[3-(2-Cyclopropanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-4-yl-acetic acid, (2-[3-(2-Cyclobutanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-4-yl}-acetic acid ethyl ester, {2-[3-(2-Cyclobutanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-4-yl}-acetic acid, {2-[3-(2-Cyclohexanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-4-yl}-acetic acid ethyl ester, {2-[3-(2-Cyclohexanecarbonyl-4-methyl-phenyl)-ureido]-thiazol-4-yl}-acetic acid, {2-[(2-Cyclopentanecarbonyl-4-methyl-phenylaminooxalyl)-amino]-thiazol-4-yl}-acetic acid ethyl ester, {2-[(2-Cyclopentanecarbonyl-4-methyl-phenylaminooxalyl)-amino]-thiazol-4-yl}-acetic acid, {2-[3-(2-Cyclopentanecarbonyl-4-methyl-phenyl)-ureido}-5-(pyridin-2-ylsulfanyl)-thiazol-4-yl]-acetic acid ethyl ester, {2-[3-(2-Cyclopentanecarbonyl-4-trifluoromethyl-phenyl)-ureido]-thiazol-4-yl}-acetic acid ethyl ester, {2-[3-(2-Cyclopentanecarbonyl-4-trifluoromethyl-phenyl)-ureido]-thiazol-4-yl}-acetic acid, {2-[3-(4-Chloro-2-cyclopentanecarbonyl-phenyl)-ureido]-thiazol-4-yl}-acetic acid ethyl ester, {2-[3-(4-Chloro-2-cyclopentanecarbonyl-phenyl)-ureido]-thiazol-4-yl}-acetic acid, {2-[3-(2-Cyclopentanecarbonyl-4-fluoro-phenyl)-ureido]-thiazol-4-yl}-acetic acid ethyl ester, and {2-[3-(2-Cyclopentanecarbonyl-4-fluoro-phenyl)-ureido]-thiazol-4-yl}-acetic acid.
- 46. A compound according to claim 1, which compound is an activator of glucokinase, when tested in the Glucokinase Activation Assay (I) disclosed herein at a glucose concentration of 2 mM.
- 47. A method for the treatment of: hyperglycemia, IGT, Syndrome X, type 2 diabetes, type 1 diabetes, dyslipidemia, hyperlipidemia, hypertension, obesity, or lowering of food intake, appetite regulation, regulating feeding behaviour, or for enhancing the secretion of enteroincretins comprising administering to one in need of such treatment a therapeutically effective amount of a compound according to claim 1.
- 48. A pharmaceutical composition comprising, as an active ingredient, at least one compound according to claim 1 together with one or more pharmaceutically acceptable carriers or excipients.
- 49. A pharmaceutical composition according to claim 48 in unit dosage form, comprising from about 0.05 mg to about 1000 mg of the compound.
- 50. A pharmaceutical composition according to claim 48 in unit dosage form, comprising from about 0.05 mg to about 200 mg of the compound.
Priority Claims (2)
| Number |
Date |
Country |
Kind |
| PA 2002 00999 |
Jun 2002 |
DK |
|
| PA 2003 00286 |
Feb 2003 |
DK |
|
CROSS-REFERENCE TO RELATED APPLICATIONS
[0001] This application is a continuation of international application no. PCT/DK03/00449 filed Jun. 27, 2003 and claims priority under 35 U.S.C. 119 of Danish application no. PA 2002 00999 filed Jun. 27, 2002 and Danish application no. PA 2003 00286 filed Feb. 25, 2003 and U.S. application No. 60/394,144 filed Jul. 3, 2002 and U.S. application No. 60/452,228 filed Mar. 5, 2003, and claims priority under 35 U.S.C. 120 of international application no. PCT/DK03/00449 filed Jun. 27, 2003, the contents of each of which are fully incorporated herein by reference.
Provisional Applications (2)
|
Number |
Date |
Country |
|
60394144 |
Jul 2002 |
US |
|
60452228 |
Mar 2003 |
US |
Continuations (1)
|
Number |
Date |
Country |
| Parent |
PCT/DK03/00449 |
Jun 2003 |
US |
| Child |
10679887 |
Oct 2003 |
US |
Patent Application
20040122235
