摘要 |
Compounds of formula: (I) are found to antagonise N-type calcium channels wherein: - A is a 5- to 10-membered heteroaryl or heterocyclyl moiety, said moiety being optionally fused to a phenyl, 5- to 6-membered heteroaryl, C<SUB>3</SUB>-C<SUB>6</SUB> carbocyclyl or 5- to 6- membered heterocyclyl group; - B is a bond or a C<SUB>1</SUB>-C<SUB>6</SUB> alkyl or C<SUB>2</SUB>-C<SUB>6</SUB> alkenyl moiety; - either (a) R<SUP>1</SUP> is hydrogen or C<SUB>1</SUB>-C<SUB>6</SUB> alkyl and R<SUP>2</SUP> is hydrogen, C<SUB>1</SUB>-C<SUB>6</SUB> alkyl, C<SUB>2</SUB>-C<SUB>6</SUB> alkenyl, halogen, hydroxy, thio, amino, -Het-L or -L-Het-L', wherein L and L' are the same or different and represent C<SUB>1</SUB>-C<SUB>6</SUB> alkyl or C<SUB>2</SUB>-C<SUB>6</SUB>alkenyl and Het is O, S or NR, wherein R is hydrogen or C<SUB>1</SUB>-C<SUB>6</SUB> alkyl or (b) R<SUP>1</SUP> and R<SUP>2</SUP> form, together with the carbon to which they are attached, a 5- to 10-membered heterocyclyl or a C<SUB>3</SUB>-C<SUB>8</SUB> carbocyclyl moiety; R<SUP>3</SUP> is hydrogen, C<SUB>1</SUB>-C<SUB>6</SUB> alkyl, C<SUB>2</SUB>-C<SUB>6</SUB> alkenyl or -L-Het-L', wherein L, L' and Het are as defined above; and - R<SUP>4</SUP>, R<SUP>5</SUP> and R<SUP>6</SUP> are the same or different and represent hydrogen, halogen, hydroxy, amino, thio, C<SUB>1</SUB>-C<SUB>6 </SUB>alkyl, C<SUB>2</SUB>-C<SUB>6</SUB> alkenyl, C<SUB>1</SUB>-C<SUB>6</SUB> alkoxy, C<SUB>1</SUB>-C<SUB>6 </SUB>alkylthio, mono(C<SUB>1</SUB>-C<SUB>6</SUB> alkyl)amino or di(C<SUB>1</SUB>-C<SUB>6</SUB> alkyl)amino. |
申请人 |
VERNALIS (R & D) LIMITED;HOBBS, CHRISTOPHER, JOHN;LYNCH, ROSEMARY;MELLOR, SARAH, LOUISE;RADFORD, FLEUR;GILBERT, JENNY, CHRISTINE;STOKES, STEPHEN;GLEN, ANGELA;FUIMANA, ANDREA;EARNSHAW, CHRISTOPHER, GEOFFREY;KNUTSEN, LARS, JACOB, STRAY;DEAN, KATHRYN, ELIZABETH, SORREL |
发明人 |
HOBBS, CHRISTOPHER, JOHN;LYNCH, ROSEMARY;MELLOR, SARAH, LOUISE;RADFORD, FLEUR;GILBERT, JENNY, CHRISTINE;STOKES, STEPHEN;GLEN, ANGELA;FUIMANA, ANDREA;EARNSHAW, CHRISTOPHER, GEOFFREY;KNUTSEN, LARS, JACOB, STRAY;DEAN, KATHRYN, ELIZABETH, SORREL |