Patent ID: 6369110
Filing Date: 2002-04-09
Classification: C07C,C07D

Abstract:
A compound represented by the formula (1): wherein R1 is a hydrogen atom, an alkyl group, a substituted alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, a cycloalkenyl group, a saturated heterocyclic group, an aromatic group, an acyl group, a halogen atom, â€”OR6, â€”S(O)nR7, â€”Qâ€”Ra or wherein A is an oxygen atom or â€”S(O)nâ€”, R10 is a hydrogen atom, an alkyl group, a substituted alkyl group, an acyl group, â€”S(O)nR7 or â€”Qâ€”Ra, and the ring is a 3- to 8-membered saturated heterocyclic group composed of a nitrogen atom and carbon atoms; R2, R3, R4 and R5 are independently a hydrogen atom, an alkyl group, a substituted alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, a cycloalkenyl group, a saturated heterocyclic group, an aromatic group, an acyl group, a carboxyl group, an alkoxycarbonyl group, a halogen atom, a nitro group, â€”OR6, â€”N(R8)R9, â€”CON(R8)R9, â€”SO2N(R8)R9, â€”S(O)nR7, â€”Qâ€”Ra or wherein Aâ€²is an oxygen atom, â€”S(O)nâ€” or â€”N(R51)â€”, and R10 and the ring are as defined above; Y1, Y2, Y3 and Y4, which may be the same or different, are independently a single bond, â€”CH2â€”, â€”COâ€”, or â€”C(&boxH;C(R12)R13)â€” provided that at least two of Y1 through Y4 are independently a group other than a single bond; Z may be absent, or one or more Zs may be present and are, the same or different, independently the following substituent for a hydrogen atom bonded to any of the carbon atoms constituting the ring formed by Y1 through Y4, an alkyl group, a substituted alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, a cycloalkenyl group, a saturated heterocyclic group, a halogen atom, a carboxyl group, an alkoxy-carbonyl group, an aromatic group, an acyl group, â€”OR6, â€”N(R8)R9, â€”S(O)nR7, â€”C(O)N(R8)R9, â€”SO2N(R8)R9, or â€”Qâ€”Ra; Q is a substituted or unsubstituted lower alkylene group; Ra is a substituted or unsubstituted vinyl group, or a substituted or unsubstituted ethynyl group; R6 is a hydrogen atom, an alkyl group, a substituted alkyl group, a cycloalkyl group, a cycloalkenyl group, a saturated heterocyclic group or an aromatic group; R7 is an alkyl group, a substituted alkyl group or an aromatic group; n is an integer of 0, 1 or 2; R8 and R9 are independently a hydrogen atom, an alkyl group, a substituted alkyl group, a cycloalkyl group, a cycloalkenyl group, a saturated heterocyclic group, an aromatic group, an acyl group, â€”S(O)2R7 or â€”Qâ€”Ra, or R8 and R9, when taken together with the nitrogen atom to which they are bonded, form a 5- to 7-membered saturated cyclic amino group which may contain other heteroatom(s) in the ring and may be substituted by one or more alkyl groups, substituted alkyl groups, hydroxyl groups or â€”OR6 groups; R11 is a hydrogen atom, an alkyl group, a substituted alkyl group, a cycloalkyl group, a saturated heterocyclic group, an aromatic group, an acyl group, â€”S(O)2R7 or â€”Qâ€”Ra; R51 is a hydrogen atom, an alkyl group, a substituted alkyl group, a cycloalkyl group, a saturated heterocyclic group, an aromatic group, an acyl group, â€”S(O)2R7 or â€”Qâ€”Ra; and R12 and R13 are independently a hydrogen atom, an alkyl group, a substituted alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, a cycloalkenyl group, a saturated heterocyclic group, a halogen atom, a carboxyl group, an alkoxycarbonyl group, an aromatic group, an acyl group, â€”OR6, â€”CON(R8)R9, â€”S(O)nR7 or â€”Qâ€”Ra, a prodrug of said compound, or a pharmaceutically acceptable salt of said compound or prodrug; wherein the alkyl group is a linear or a branched alkyl group of 8 or less carbon atoms; the cycloalkyl group is either an unsubstituted one or a substituted one having as the substituent(s); 1 to 4 alkyl group(s), substituted alkyl group(s), hydroxyl group(s) or â€”OR6 group(s), and is a 3- to 8-membered cycloalkyl group; the cycloalkenyl group is either an unsubstituted one or a substituted one having as the substituent(s); 1 to 4 alkyl group(s), substituted alkyl group(s), hydroxyl group(s) or â€”OR6 group(s), and is a 3- to 8-membered cyoloalkenyl group having a double bond; the saturated heterocyclic group is either an unsubstituted one or a substituted one having as the substituent(s); 1 to 4 alkyl group(s), substituted alkyl group(s), hydroxyl group(s), or â€”OR6 group(s), and is a 3- to 8-membered saturated heterocyclic group having an oxygen atom or a sulfur atom; the alkoxycarbonyl group is a linear or branched alkoxycarbonyl group of 6 or less carbon atoms; the aromatic group is a substituted or unsubstituted aryl group, or a substituted or unsubstituted heteroaryl group, wherein the aryl group is 10 or less carbon atoms, and the heteroaryl group is a 5- or 6-membered heteroaryl group containing 1 to 4 nitrogen atoms or a 5- to 6-membered heteroaryl group containing 0 to 2 nitrogen atoms and an oxygen atom or a sulfur atom; the substituent of each of the substituted aryl group and the substituted heteroaryl group is an alkyl group, a substituted alkyl group, a halogen atom, a nitro group, an alkoxycarbonyl group , a carboxyl group, and a group represented by the formula â€”OR6, â€”N(R8)R9, â€”CON(R8)R9, â€”SO2N(R8)R9 or â€”S(O)nR7; the 5- to 7-membered cyclic amino group is a 5- to 7-membered ring group containing 1 to 3 nitrogen atoms or a 5- to 7-membered ring group containing a nitrogen atom and an oxygen atom; the substituent of the substituted alkyl group is a halogen atom, a hydroxyl group, an alkoxy group, a cycloalkyl group, a cyano group, a carboxy group, an alkoxycarbonyl group, an acyl group, an aromatic group, and a group represented by the formula â€”CONRpRq wherein Rp and Rq is independently a hydrogen atom or an alkyl group, or Rp and Rq, when taken together, represent a 5- to 7-membered saturated cyclic amino group which may contain another heteroatom; â€”N(R8)R9; or â€ƒwherein Râ€³ is a hydrogen atom, an alkyl group or a substituted alkyl group, and the ring is a 3- to 8-membered saturated heterocyclic group composed of a nitrogen atom and carbon atoms, the substituent of each of the lower alkylene group and the vinyl or ethynyl group is an alkyl group, a substituted alkyl group, a cycloalkyl group, a cycloalkenyl group, a saturated heterocyclic group, a carboxyl group, an alkoxycarbonyl group, an aromatic group, and a group represented by the formula â€”CON(R8)R9; the lower alkylene group is an alkylene group of 6 or less carbon atoms; the acyl group is a formyl group, an alkanoyl group of 2 to 6 carbon atoms, a cycloalkanecarbonyl group of 4 to 7 carbon atoms, a cycloalkenecarbonyl group of 3 to 6 carbon atoms, an aroyl group of 6 to 10 carbon atoms, a saturated heterocyclic ring-carbonyl group having a 5- or 6-membered saturated heterocyclic ring containing one or two heteroatoms selected from nitrogen atom, oxygen atom, and sulfur atom; or a heteroaromatic acyl group having a 5- or 6-membered heteroaromatic ring containing one or two heteroatoms selected from nitrogen atom, oxygen atom and sulfur atom; the alkenyl group is an alkenyl group of 6 or less carbon atoms; and the alkynyl group is an alkynyl group of 6 or less carbon atoms.