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US 5,770,615 AGranted
Catecholamine surrogates useful as .beta..sub.3 agonists
AssigneeBristol-Myers Squibb Company
InventorsPeter T. W. Cheng, Gregory S. Bisacchi, Ashvinikumar V. Gavai, Kathleen M. Poss, Denis E. Ryono, Philip M. Sher, Chong-qing Sun, William N. Washburn
Life of this patent
Estimating the term…
Abstract
Compounds of the formula ##STR1## and pharmaceutically acceptable salts thereof. These compounds are beta three adrenergic receptor agonists and are useful, therefore for example, in the treatment of diabetes, obesity and gastrointestinal diseases.
Claims23
A compound of the formula ##STR40## or pharmaceutically acceptable salts thereof wherein:
- R.sup.1 is lower alkyl, aryl or arylalkyl;
- R.sup.2 is hydrogen, hydroxyl, hydroxymethyl or halogen;
- R.sup.3 is hydrogen or alkyl;
- R.sup.4 and R.sup.4' are independently hydrogen, alkoxy, alkoxymethyl, hydroxyl, --CN, --CON(R.sup.6)R.sup.6', --CO.sub.2 R.sup.6, --N(R.sup.6)R.sup.6', --NR.sup.6 COR.sup.8, --NR.sup.6 SO.sub.2 R.sup.1 ;
- or R.sup.4 and R.sup.4' may together with the carbon atoms to which they are bonded form a heterocycle;
- R.sup.5, R.sup.5' and R.sup.5" are independently A or B, wherein A is hydrogen, alkyl, cycloalkyl, halogen, hydroxyl, aryl, alkoxy, cyano, --SR.sup.7, --SOR.sup.7, --SO.sub.2 R.sup.7, --N(R.sup.6)R.sup.6', --NR.sup.6 COR.sup.8, --OCH.sub.2 CON(R.sup.6)R.sup.6', --OCH.sub.2 CO.sub.2 R.sup.6, CON(R.sup.6)R.sup.6', --CO.sub.2 R.sup.6 ;
- and B is --(CH.sub.2).sub.m PO(OR.sup.6)OR.sup.6', --O-aryl, --OCH.sub.2 CH.sub.2 N(R.sup.6)R.sup.6', --COR.sup.7, --SO.sub.2 N(R.sup.6)R.sup.6', --NR.sup.6 CO.sub.2 R.sup.7, --NR.sup.6 CO(N(R.sup.6)R.sup.6'), heterocycle or --R.sup.5 and R.sup.5' may together with the carbon atoms to which they are bonded form a heterocycle;
- provided that at least one of R.sup.5, R.sup.5' and R.sup.5" is B;
- R.sup.6 and R.sup.6' are independently hydrogen or lower alkyl;
- R.sup.7 is lower alkyl;
- R.sup.8 is hydrogen, lower alkyl, aryl or arylalkyl;
- m is an integer of 0 to 6.
9 more elements
A compound of the formula ##STR41## where Pro is a protecting group;
- R.sup.1 is lower alkyl, aryl or arylalkyl;
- R.sup.2' is hydrogen, hydroxyl, halogen, --CO.sub.2 R.sup.7, --CH.sub.2 OPro', or --O-Pro', where Pro' is a protecting group;
- R.sup.3 is hydrogen or alkyl;
- R.sup.4 and R.sup.4' are independently hydrogen, alkoxy, hydroxyl, alkoxymethyl, --CN, --CON(R.sup.6)R.sup.6', --CO.sub.2 R.sup.7,--N(R.sup.6)R.sup.6', --NR.sup.6 COR.sup.8, --NR.sup.6 SO.sub.2 R.sup.1 ;
- or R.sup.4 and R.sup.4' may together with the carbon atoms to which they are bonded form a heterocycle;
- R.sup.6 and R.sup.6' are independently hydrogen or lower alkyl;
- R.sup.7 is lower alkyl;
- and
- R.sup.8 is hydrogen, lower alkyl, aryl or arylalkyl.
6 more elements
Dependencies are inferred from the claim text.