CATECHOLAMINE SURROGATES PROCESSES FOR THE PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME

阅读量:

5

申请(专利)号:

IL112060

申请日期:

1994-12-19

公开/公告号:

IL112060A

公开/公告日期:

1995-03-15

申请(专利权)人:

BRISTOL-MYERS SQUIBB COMPANY

摘要:

Compounds of the formula ##STR1## or pharmaceutically acceptable salts thereof wherein: A is a bond, --(CH.sub.2).sub.n -- or -- CH(B)--, where n is an integer of 1 to 3 and B is --CN, --CON(R.sup.9)R. sup.9' or --CO.sub. 2 R.sup.7 ;R.sup.1 is lower alkyl, aryl or arylalkyl; R.sup.2 is hydrogen, hydroxy, alkoxy, --CH.sub.2 OH, cyano, --C(O)OR. sup.7, --CO.sub.2 H, --CONH.sub.2, tetrazole, --CH.sub.2 NH.sub.2 or halogen; ##STR2## R.sup.3 is hydrogen, alkyl, heterocycle or R.sup.4 is hydrogen, alkyl or B;R. sup.5, R.sup.5', R. sup.8, R.sup.8' or R.sup. 8" are independently hydrogen, alkoxy, lower alkyl, halogen, --OH, --CN, --(CH.sub.2).sub.n NR. sup.6 COR.sup.7, -- CON(R.sup.6)R.sup.6', --CON(R. sup.6)OR.sup.6', --CO. sub.2 R.sup.6, --SR. sup.7, --SOR.sup.7, --SO.sub.2 R.sup.7, --N(R.sup.6) SO.sub.2 R.sup.1, -- N(R.sup.6)R.sup.6', --NR.sup.6 COR.sup.7, --OCH.sub. 2 CON(R.sup.6)R.sup. 6', --OCH.sub.2 CO.sub.2 R.sup. 7 or aryl; or< P>R.sup.5 and R.sup.5' or R.sup.8 and R.sup.8' may together with the carbon atoms to which they are attached form an aryl or heterocycle; R.sup.6 and R.sup.6' are independently hydrogen or lower alkyl; and< P>R.sup.7 is lower alkyl;< P>R.sup.9 is hydrogen, lower alkyl, alkyl, cycloalkyl, arylalkyl, aryl, heteroaryl; or R.sup.9 and R.sup.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.sub.2).sub.n and R.sup.3 is hydrogen or unsubstituted alkyl, then R. sup.4 is B or substituted alkyl. These compounds are beta.sub.3 adrenergic receptor agonists and are useful, therefore for example, in the treatment of diabetes, obesity and gastrointestinal diseases.

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