申请人:——
公开号:US20030114438A1
公开(公告)日:2003-06-19
Lactam derivatives of the formula
1
where
X is -C(=O)NR
3′
-, -NR
3′
C(=O)-, -C(=NCN)NR
3′
-, -NR
3
′C(=NCN)-, -CH
2
NR
3′
-, -CH(alkyl)NR
3′
-, -CH(COOalkyl)NR
3′
-, -CH(CH
2
OH)NR3 -,-C(CH
2
Oalkyl)-;
R′ is halo, alkyl, cycloalkyl, alkyl(cycloalkyl), aryl, (aryl)alkyl, (aryl)alkenyl, (aryl)alkynyl, O-alkyl, O-alkenyl, O-aryl, O-alky(aryl), O-alkyl(heterocyclo), COO-alkyl, C)-alkyl, CO-amino, CO-substituted amino, alkyl-CO-amino, alkyl-CO-substituted amino, NHCO-alkyl, NHCO-aryl, NHCO-alkyl(aryl), NHCO-alkyl(heterocyclo), N(alkyl)CO-alkyl, N(alkyl)CO-aryl, N(alkyl)CO-heterocyclo, N(alkyl)CO-alkyl(aryl), N(alkyl)CO-alkyl(heterocyclo);
R
2
is hydrogen, alkyl, halo, aryl, (aryl)alkyl, O-alkyl, amino, substituted amino;
R
3
and R
3′
are the same or different and are independently selected from hydrogen, alkyl or alkyl(aryl);
R
4
which can be bonded to a ring carbon or nitrogen, is selected from hydrogen, alkyl, alkenyl, alky(aryl), alkyl(heterocyclo), cycloalkyl, alkyl(cycloalkyl), alkyl-(amino), alkyl-(substituted amino), alkyl-NHCO(alkyl), alkyl-NHCO(aryl), alkyl-NHCO(heterocyclo), alkyl-NHCO(alkylaryl), alkyl-NHCO(alkylheterocyclo); and n is an integer of 0 to 2. These compounds have been found to be useful in the treatment of arrhythmia.
这是一种公式为1的内酰胺衍生物,其中:
X为-C(=O)NR3′-, -NR3′C(=O)-, -C(=NCN)NR3′-, -NR3′C(=NCN)-, -CH2NR3′-, -CH(烷基)NR3′-, -CH(COO烷基)NR3′-, -CH(CH2OH)NR3-, -C(CH2O烷基)-;
R′为卤素,烷基,环烷基,烷基(环烷基),芳基,(芳基)烷基,(芳基)烯基,(芳基)炔基,O-烷基,O-烯基,O-芳基,O-烷基(芳基),O-烷基(杂环烷基),COO-烷基,C)-烷基,CO-氨基,CO-取代氨基,烷基-CO-氨基,烷基-CO-取代氨基,NHCO-烷基,NHCO-芳基,NHCO-烷基(芳基),NHCO-烷基(杂环烷基),N(烷基)CO-烷基,N(烷基)CO-芳基,N(烷基)CO-杂环烷基,N(烷基)CO-烷基(芳基),N(烷基)CO-烷基(杂环烷基);
R2为氢,烷基,卤素,芳基,(芳基)烷基,O-烷基,氨基,取代氨基;
R3和R3′相同或不同,独立选择自氢,烷基或烷基(芳基);
R4可以与环上的碳或氮相结合,选择自氢,烷基,烯基,烷(芳基),烷基(杂环烷基),环烷基,烷基(环烷基),烷基-(氨基),烷基-(取代氨基),烷基-NHCO(烷基),烷基-NHCO(芳基),烷基-NHCO(杂环烷基),烷基-NHCO(烷基芳基),烷基-NHCO(烷基杂环烷基);
n为0到2的整数。
这些化合物已被发现在心律失常的治疗中有用。