Novel thiourea derivatives and the pharmaceutical compositions containing the same

A compound of the following formula (I):

• 322
• or a pharmaceutically acceptable salt thereof,
• wherein:
• X represents S, O or —NCN;
• Y represents single bond, NR3, O or S;
• R1 represents
• 323
• pyridinylmethyl, pyrrolylmethyl, oxazolyhuethyl, pyrazolylnethyl, imidazolylnethyl, anthracenylnethyl, naphthylmethyl, quinolinylmethyl, alkoxycarbonyl or alkylcarbonyloxy (wherein, m is 0, 1, 2, 3 or 4;
• R4 and R5 are independentyl hydrogen, lower alkyl having 1 to 5 carbon atoms, hydroxy, methanesulfanylamino, lower alkoxy having 1 to 5 carbon atoms, methoxyalkoxy, methoxyalkoxyalkyl, alkoxycarbonyloxy, benzyloxy, acetoxymethyl, propinoyloxymethyl, butoxyalkyl, trimethylacetoxy, trimethylacetoxymethyl or halogen;
• and R6 and R7 are independently hydrogen, lower alkyl having 1 to 5 carbon atoms);
• R2 represents R8—(CH2)n—
• {wherein, n is 0, 1, 2, 3 or 4;
• R8 is benzoyl, imidazolyl, indolyl, indazolyl, thiazolyl, pyrazolyl, oxazolyl, isoxazolyl, benzimidazolyl, chromonyl or benzothiazolyl substituted or unsubstituted with lower alkyl having 1 to 5 carbon atoms, nitro, amino, cyano, methanesulfonylamino, formyl or halogen, or
• 324
• (wherein, R9 is hydrogen, halogen, lower alkyl having 1 to 5 carbon atoms, lower alkoxy having 1 to 5 carbon atoms, hydroxy, nitro, cyano, —NHSO2R2, —S(O)pR12, —NR13R14, carboxyl;
• R10 is hydrogen, nitro, NHSO2R12, S(O)pR12 or NR13R14;
• R11 is hydrogen or cyano;
• R12 is lower alkyl having 1 to 5 carbon atoms, methylphenyl, NR13R14, trifluoromethyl or alkenyl;
• R13 and R14 are independently hydrogen or lower alkyl having 1 to 5 carbon atoms;
• and p is 0 or 2.);
• or
• 325
• (wherein, Z is O, S, NH or —NCH3;
• R15 is hydrogen, halogen, lower alkyl having 1 to 5 carbon atoms, nitro, cyano, —NHSO2R12, —S(O)pR12, N,N-dimethylaminomethyl or alkoxycarbonylamino;
• and p and R12 have the same meanings as defined in R9);
• 326
• (wherein, W is O, S, NH, NR16, —N(SO2CH3)— or —CH2—;
• and R16 is pyridinyl or pyrimidinyl substituted or unsubstituted with lower alkyl having 1 to 5 carbon atoms, nitro, methanesulfonylamino or halogen;
• or benzyl or phenethyl substituted or unsubstitued with lower alkyl having 1 to 5 carbon atoms, alkoxy, hydroxy, nitro, methanesulfonylamino or halogen);
• or
• 327
• (wherein, R17, R18, R19, R20 and R21 are independently hydrogen, halogen, lower alkyl having 1 to 5 carbon atoms, alkoxy, methylenedioxy, methanesulfonylaminomethyl, alkoxycarbonyl, hydroxy, sulfamoyl, aminoalkoxy, alkoxycarbonylamno, —NHCH2CO2H, alkoxyalkylcarbonylamino, alkoxycarbonylalkylamino, nitro, formyl, acetyl, formnylarnino, acetoxyamino, cyano, —OSO2CH3, —NHSO2R12, —N(SO2R12)CH3, —N(SO2R12)2, —S(O)pR12, —NR13R14, thiocarbamnoyl, —C(═O)NHNH2, —C(═O)NHOH, —C(═O)NHOCH3, —PO(═O)(OCH3)2, carboxyl, NHBoc, —NHC(═O)SCH3 or guanidine;
• R22 and R23 are independently hydrogen, halogen, alkoxy or hydroxy;
• and p, R12, R13 and R14 have the same meanings as defined in R9);
• or hydroxyphenylalkyl or (methanesulfonylaminophenyl)alkyl};
• and
• R3 represents hydrogen, alkyl or cycloalkyl having 1 to 8 carbon atoms, lower alkylphenyl having 1 to 5 carbon atoms, pyridinylethyl, bisphenylmethyl;
• or phenylalkyl substituted with lower alkyl having 1 to 5 carbon atoms, halogen or methanesulfonylamino.