Catecholamine surrogates useful as β 3 agonists
申请(专利)号:
08/346543
申请日期:
12/02/1994
公开/公告号:
US5776983
公开/公告日期:
07/07/1998
被引量:
摘要:
Compounds of the formula ##STR1## or pharmaceutically acceptable salts thereof wherein: A is a bond, --(CH 2 ) n -- or --CH(B)--, where n is an integer of 1 to 3 and B is --CN, --CON(R 9 )R 9 ' or --CO 2 R 7 ; R 1 is lower alkyl, aryl or arylalkyl; R 2 is hydrogen, hydroxy, alkoxy, --CH 2 OH, cyano, --C(O)OR 7 , --CO 2 H, --CONH 2 , tetrazole, --CH 2 NH 2 or halogen; ##STR2## R 3 is hydrogen, alkyl, heterocycle or R 4 is hydrogen, alkyl or B; R 5 , R 5 ', R 8 , R 8 ' or R 8 " are independently hydrogen, alkoxy, lower alkyl, halogen, --OH, --CN, --(CH 2 ) n NR 6 COR 7 , --CON(R 6 )R 6 ', --CON(R 6 )OR 6 ', --CO 2 R 6 , --SR 7 , --SOR 7 , --SO 2 R 7 , --N(R 6 )SO 2 R 1 , --N(R 6 )R 6 ', --NR 6 COR 7 , --OCH 2 CON(R 6 )R 6 ', --OCH 2 CO 2 R 7 or aryl; or R 5 and R 5 ' or R 8 and R 8 ' may together with the carbon atoms to which they are attached form an aryl or heterocycle; R 6 and R 6 ' are independently hydrogen or lower alkyl; and R 7 is lower alkyl; R 9 is hydrogen, lower alkyl, alkyl, cycloalkyl, arylalkyl, aryl, heteroaryl; or R 9 and R 9 ' may together with the nitrogen atom to which they are attached form a heterocycle; with the proviso that when A is a bond or --(CH 2 ) n and R 3 is hydrogen or unsubstituted alkyl, then R 4 is B or substituted alkyl. These compounds are beta 3 adrenergic receptor agonists and are useful, therefore for example, in the treatment of diabetes, obesity and gastrointestinal diseases.
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