申请人:Pfizer Inc.
公开号:US05340831A1
公开(公告)日:1994-08-23
Muscarinic receptor antagonists of formula (I), and their pharmaceutically acceptable salts, wherein Y is --CH.sub.2 --, --(CH.sub.2).sub.2 --, --CH.sub.2 O--, --(CH.sub.2).sub.2 O-- or --CH.sub.2 S--; R is --CH or --CONH.sub.2 ; and R.sup.1 is a group of formula (a), where R.sup.2 and R.sup.3 are each independently H, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, --(CH.sub.2).sub.n OH, halo, trifluoromethyl, cyano, --(CH.sub.2).sub.n NR.sup.4 R.sup.5, --CO(C.sub.1 -C.sub.4 alkyl), --OCO(C.sub.1 -C.sub.4 alkyl), --CH(OH)(C.sub.1 -C.sub.4 alkyl), --C(OH)(C.sub.1 -C.sub.4 alkyl.sub.2, --SO.sub.2 NH.sub.2, --(CH.sub.2).sub.n CONR.sup.6 R.sup.7 or --(CH.sub.2).sub.n COO(C.sub.1 -C.sub.4 alkyl); R.sup.4 is H or C.sub.1 -C.sub.4 alkyl; R.sup.5 is H, C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkysulphonyl; R.sup.6 and R.sup.7 are each independently H or C.sub.1 -C.sub.4 alkyl; and n is 0, 1 or 2. The compounds are particularly useful in treating irritable bowel syndrome.
化学式(I)的肌制胆碱受体拮抗剂及其药用盐,其中Y为--CH.sub.2 --,--(CH.sub.2).sub.2 --,--CH.sub.2 O--,--(CH.sub.2).sub.2 O--或--CH.sub.2 S--; R为--CH或--CONH.sub.2; R.sup.1为化学式(a)的基团,其中R.sup.2和R.sup.3分别独立地为H,C.sub.1 -C.sub.4烷基,C.sub.1 -C.sub.4烷氧基,--(CH.sub.2).sub.n OH,卤素,三氟甲基,氰基,--(CH.sub.2).sub.n NR.sup.4 R.sup.5,--CO(C.sub.1 -C.sub.4烷基),--OCO(C.sub.1 -C.sub.4烷基),--CH(OH)(C.sub.1 -C.sub.4烷基),--C(OH)(C.sub.1 -C.sub.4烷基.sub.2,--SO.sub.2 NH.sub.2,--(CH.sub.2).sub.n CONR.sup.6 R.sup.7或--(CH.sub.2).sub.n COO(C.sub.1 -C.sub.4烷基); R.sup.4为H或C.sub.1 -C.sub.4烷基; R.sup.5为H,C.sub.1 -C.sub.4烷基或C.sub.1 -C.sub.4烷基磺酰基; R.sup.6和R.sup.7分别独立地为H或C.sub.1 -C.sub.4烷基; n为0,1或2。这些化合物在治疗肠易激综合征方面特别有用。