Patent ID: 6310056
Filing Date: 2001-10-30
Classification: A61P,C07D

Abstract:
A compound represented by the formula (I), or a pharmaceutically acceptable salt thereof: ##STR28##whereinR.sup.1 represents a hydrogen or methyl,R.sup.2, R.sup.3, R.sup.4, and R.sup.5, either one of which represents the bond to the 2-position on the carbapenem ring, and the other three of which-may be the same or different, respectively representhydrogen,halogen,nitro,cyano,lower alkyl, in which one or more hydrogen atoms on the alkyl group may be substituted by groups selected from the group consisting of halogen, nitro, cyano, lower cycloalkyl, lower alkylthlio, lower alkoxy, hydroxy, amino, N-lower alkylamino, formyl, lower alkylcarbonyl, aryl carbonyl, carboxyl, lower alkoxycarbonyl, formylamino, lower alkylcarbonylamino, carbamoyl, N-lower alkylcarbamoyl, N,N-di-lower alkylaminocarbonyl, aminosulfonyl, (N-lower alkylamino)sulfonyl, (N,N-di-lower alkylamino)sulfonyl, (N-lower alkylamino)sulfonylamino, aminosulfonylamino, (N,N-di-lower alkylamino)sulfonylamino, and aryl,lower cycloalkyl, in ewhich one or more hydrogen atoms on the cycloalkyl group may be substituted by groups selected from the group consisting of lower alkyl, halogen, nitro, cyano, lower alkylthio, lower alkoxy, hydroxy, amino, N-lower alkylamino, formyl, lower alkylcarbonyl, aryl carbonyl, carboxyl, lower alkoxycarbonyl, formylamino, lower alkylcarbonylamino, carbamoyl, N-lower alkylcarbamoyl, N,N-di-lower alkylaminocarbonyl, aminosulfonyl, (N-lower alkylamino)sulfonyl, (N,N-di-lower alkylanmino)sulfonyl, (N-lower alkylamino)sulfonylamino, aminosulfonylamino, (N,N-di-lower alkylamino)sulfonylamino, and aryl,lower alkylthio,C.sub.2-4 alkenyl, in which one or more hydrogen atoms on the alkenyl group may be substituted by groups selected from the group consisting of lower alkyl, halogen, nitro, cyano, lower cycloalkyl, lower alkylthio, lower alkoxy, hydroxy, amino, N-lower alkylamino, formyl, lower alkylcarbonlyl, aryl carbonyl, carboxyl, lower alkoxycarbonyl, formylamino, lower alkylcarbonylamino, carbamoyl, N-lower alkylcarbamoyl, N,N-di-lower alkylaminocarbonyl, aminosulfonyl, (N-lower alkylamino)sulfonyl, (N,N-di-lower alkylamino)sulfonyl, (N-lower alkylamino)sulfonylamino, aminosulfonylamino, (N,N-di-lower alkylamino)sulfonylamino, and aryl,formyl,lower alkylcarbonyl,lower alkoxycarbonyl,lower alkylsulfonyl,lower arylsulfonyl,aminosulfonyl,aryl carbonyl,aryl, in which one or more hydrogen atoms on the aryl group may be substituted by groups selected from the group consisting of lower alkyl, halogen, nitro, cyano, lower cycloalkyl, lower alkylthio, lower alkoxy, hydroxy, amino, N-lower alkylamino, formyl, lower alkylcarbonyl, aryl carbonyl, carboxyl, lower alkoxycarbonyl, formylamino, lower alkylcarbonylamino, carbamoyl, N-lower alkylcarbamoyl, N,N-di-lower alkylaminocarbonyl, aminosulfonyl, (N-lower alkylamino)sulfonyl, (N,N-di-lower alkylamino)sulfonyl, (N-lower alkylamino)sulfonylamino, aminosulfonylamino, and (N,N-di-lower alkylamino)sulfonylamino,carbamoyl,N-lower alkylcarbamoyl,N,N-di-lower alkylaminocarbonyl,lower alkoxyiminomethyl, orhydroxyiminomethyl,R.sup.6 is not present or representslower alkyl, in which one or more hydrogen atoms on the alkyl group may be substituted by groups selected from the group consisting of halogen, nitro, cyano, lower cycloalkyl, lower alkylthio, lower alkoxy, hydroxy, amino, N-lower alkylamino, formyl, lower alkylcarbonyl, aryl carbonyl, carboxyl, lower alkoxycarbonyl, formylamino, lower alkylcarbonylamino, carbamoyl, N-lower alkylcarbamoyl, N,N-di-lower alkylaminocarbonyl, aminosulfonyl, (N-lower alkylamino)sulfonyl, (N,N-di-lower alkylamino)sulfonyl, (N-lower alkylamino)sulfonylamino, aminosulfonylamino, (N,N-di-lower alkylamino)sulfonylamino, and aryl,lower cycloalkyl, in which one or more hydrogen atoms on the cycloalkyl group may be substituted by groups selected from the group consisting of lower alkyl, halogen, nitro, cyano, lower alkylthio, lower alkoxy, hydroxy, amino, N-lower alkylamino, formyl, lower alkylcarbonyl, aryl carbonyl, carboxyl, lower alkoxycarbonyl, formylamino, lower alkylcarbonylamino, carbamoyl, N-lower alkylcarbamoyl, N,N-di-lower alkcylaminocarbonyl, aminosulfonyl, (N-lower alkylamino)sulfonyl, (N,N-di-lower alkylamino)sulfonyl, (N-lower alkylamino)sulfonylamino, aminosulfonylamino, (N,N-di-lower alkylamino)sulfonylamino, and aryl, orC.sub.2-4 alkenyl, in which one or more hydrogen atoms on the alkenyl group may be substituted by groups selected from the group consisting of lower alkyl, halogen, nitro, cyano, lower cycloalkyl, lower alkylthio, lower alkoyy, hydroxy, amino, N-lower alkylamino, formyl, lower alkylcarbonyl, aryl carbonyl, carboxyl, lower alkoxycarbonyl, formylamino, lower alkylcarbonyl amino, carbamoyl, N-lower alkylcarbaioyl, N,N-di-lower alkylaminocarbonyl, aminosulfonyl, (N-lower alkylamino)sulfonyl, (N,N-di-lower alkylamino)sulfonyl, (N-lower alkylamino)sulfonylamino, aminosulfonylamino, (N,N-di-lower alkylamino)sulfonylamino, and aryl, andR is not present, or represents hydrogen or a group which may be metabolically hydrolyzed in the body,provided that when R.sup.6 is not present, R represents hydrogen or group may be metabolically hydrolyzed in the body, and when R.sup.6 is present, R is not present and the compound forms an inner salt.