Patent ID: 6825187
Filing Date: 2004-11-30
Classification: A61P,C07D

Abstract:
A compound represented by formula (I) or a pharmaceutically acceptable salt thereof: whereinR1 represents a hydrogen atom or methyl; R2 and R3, which may be the same or different, each independently represent a hydrogen atom, a halogen atom, lower alkyl on which one or more hydrogen atoms are optionally substituted by hydroxyl or amino, lower alkylcarbonyl, carbamoyl, aryl, or lower alkylthio; R4 represents lower alkylthio on which one or more hydrogen atoms are optionally substituted by a group selected from the group consisting of: a halogen atom; nitro; azido; cyano; lower cycloalkyl; lower alkylthio; hydroxyl; lower alkoxy; formyl; lower alkylcarbonyl; arylcarbonyl; carboxy; lower alkoxycarbonyl; carbamoyl; N-lower alkylcarbamoyl; N,N-di-lower alkylcarbamoyl; amino; N-lower alkylamino; N,N-di-lower alkylamino; formylamino; lower alkylcarbonylamino; aminosulfonylamino; (N-lower alkylamino)sulfonylamino; (N,N-di-lower alkylamino)-sulfonylamino; formimidoylamino; acetimidoylamino; guanidino; aminosulfonyl; (N-lower alkylamino)sulfonyl; (N,N-di-lower alkylamino)sulfonyl; aryl; a monocyclic heterocyclic ring selected from the group consisting of pyrrolidine, piperidine, pyridine, imidazole, thiazole, and thiophene, lower cycloalkylthio wherein one or more hydrogen atoms of the cycloalkyl portion are optionally substituted by a group selected from the group consisting of a halogen atom, nitro, cyano, hydroxyl, carbamoyl, and amino, C2-4 alkenylthio, C2-4 alkynylthio, arylthio, thio substituted by a heterocyclic ring selected from the group consisting of pyrrolidine, piperidine, pyridine, imidazole, thiazole, and thiophene, lower alkylsulfinyl wherein one or more hydrogen atoms of the alkyl portion are optionally substituted by a group selected from the group consisting of a halogen atom, hydroxyl, carbamoyl, and amino, lower alkylsulfonyl wherein one or more hydrogen atoms of the alkyl portion are optionally substituted by a group selected from the group consisting of a halogen atom, hydroxyl, carbamoyl, and amino, or arylcarbonyl or R4 and R5 together form â€”R4â€”R5â€” which represents â€”Sâ€”(CH2)nâ€” wherein n is an integer of 2 to 4; R5 represents lower alkyl on which one or more hydrogen atoms are optionally substituted by a group selected from the group consisting of: a halogen atom; nitro; azido; cyano; lower cycloalkyl; lower alkylthio; hydroxyl; lower alkoxy; formyl; lower alkylcarbonyl; arylcarbonyl wherein one or more hydrogen atoms of the aryl portion are optionally substituted by a group selected from the group consisting of a halogen atom, nitro, cyano, lower alkyl on which one or more hydrogen atoms are optionally substituted by a halogen atom, hydroxyl, carbamoyl, or amino, hydroxyl, lower alkoxy, benzyloxy, carboxy, lower alkoxycarbonyl, carbamoyl, amino, and hydroxyamino; carboxy; lower alkoxycarbonyl; carbamoyl; N-lower alkylcarbamoyl wherein one or more hydrogen atoms of the alkyl portion are optionally substituted by amino, formimidoylamino, acetimidoylamino, or hydroxyl; N,N-di-lower alkylcarbamoyl wherein one or more hydrogen atoms of the alkyl portion are optionally substituted by amino, formimidoylamino, acetimidoylamino, or hydroxyl; heterocyclic carbonyl selected from the group consisting of morpholinylcarbonyl and piperazinylcarbonyl; N-arylcarbamoyl; N-hydroxycarbamoyl; N-benzyloxy-carbamoyl; N-lower alkyl-N-lower alkoxycarbamoyl; amino; N-lower alkylamino wherein one or more hydrogen atoms of the alkyl portion are optionally substituted by amino, formimidoylamino, acetimidoylamino, or hydroxyl; N,N-di-lower alkylamino wherein one or more hydrogen atoms of the alkyl portion are optionally substituted by amino, formimidoylamino, acetimidoylamino, or hydroxyl; formylamino; lower alkylcarbonylamino; aminosulfonylamino; (N-lower alkylamino)sulfonylamino; (N,N-di-lower alkylamino)sulfonylamino; piperazinyl-carbonylamino; N-lower alkylpiperazinylcarbonylamino; N-arylpiperazinylcarbonylamino; formimidoylamino; acet-imidoylamino; guanidino; aminosulfonyl; (N-lower alkylamino)sulfonyl; (N,N-di-lower alkylamino)sulfonyl; aryl on which one or more hydrogen atoms are optionally substituted by a group selected from the group consisting of a halogen atom, nitro, cyano, lower alkyl on which one or more hydrogen atoms are optionally substituted by a halogen atom, hydroxyl, carbamoyl, amino, hydroxyl, lower alkoxy, benzyloxy, carboxy, lower alkoxycarbonyl, carbamoyl, amino, and hydroxyamino; and a heterocyclic ring selected from the group consisting of pyrrolidine, imidazole, thiazole, piperidine, pyridine, and thiophene, wherein one or more hydrogen atoms of the ring are optionally substituted by a halogen atom, hydroxyl, carbamoyl, or amino and, when the ring contains a nitrogen atom, lower alkyl optionally substituted by carbamoyl may be attached to the nitrogen atom, lower cycloalkyl, C2-4 alkenyl, C2-4 alkynyl, a heterocyclic ring selected from the group consisting of pyrrolidine, piperidine, and morpholine, wherein one or more hydrogen atoms on the carbon atoms in the heterocyclic ring are optionally substituted by a group selected from the group consisting of: lower alkyl on which one or more hydrogen atoms are optionally substituted by hydroxyl or amino; carboxy; lower alkoxycarbonyl; carbamoyl; N-lower alkylcarbamoyl; and N,N-di-lower alkylcarbamoyl, and wherein a hydrogen atom on the nitrogen atom in the heterocyclic ring is optionally substituted by lower alkyl, C2-4 alkenyl, formimidoyl, acetimidoyl, or amidino.