发明名称 Catecholamine surrogates useful as beta 3 agonists
摘要 Compounds of the formula <IMAGE> I or pharmaceutically acceptable salts thereof wherein: A is a bond, -(CH2)n- or -CH(B)-, where n is an integer of 1 to 3 and B is -CN, -CON(R9)R9' or -CO2R7; R1 is lower alkyl, aryl or arylalkyl; R2 is hydrogen, hydroxy, alkoxy, -CH2OH, cyano, -C(O)OR7, -CO2H, -CONH2, tetrazole, -CH2NH2 or halogen; <IMAGE> R3 is hydrogen, alkyl, heterocycle or R4 is hydrogen, alkyl or B; R5, R5', R8, R8' or R8'' are independently hydrogen, alkoxy, lower alkyl, halogen, -OH, -CN, -(CH2)nNR6COR7, -CON(R6)R6', -CON(R6)OR6', -CO2R6, -SR7, -SOR7, -SO2R7, -N(R6)SO2R1, -N(R6)R6', -NR6COR7, -OCH2CON(R6)R6', -OCH2CO2R7 or aryl; or R5 and R5' or R8 and R8' may together with the carbon atoms to which they are attached form an aryl or heterocycle; R6 and R6' are independently hydrogen or lower alkyl; and R7 is lower alkyl; R9 is hydrogen, lower alkyl, alkyl, cycloalkyl, arylalkyl, aryl, heteroaryl; or R9 and R9' may together with the nitrogen atom to which they are attached form a heterocycle; with the proviso that when A is a bond or -(CH2)n and R3 is hydrogen or unsubstituted alkyl, then R4 is B or substituted alkyl. These compounds are beta3 adrenergic receptor agonists and are useful, therefore for example, in the treatment of diabetes, obesity and gastrointestinal diseases.
申请公布号 US5776983(A) 申请公布日期 1998.07.07
申请号 US19940346543 申请日期 1994.12.02
申请人 BRISTOL-MYERS SQUIBB COMPANY 发明人 WASHBURN, WILLIAM N.;GIROTRA, RAVINDAR N.;SHER, PHILIP M.;MIKKILINENI, AMARENDRA B.;POSS, KATHLEEN M.;MATHUR, ARVIND;BISACCHI, GREGORY S.;GAVAI, ASHVINIKUMAR V.
分类号 C07D295/12;A61K31/18;A61K31/215;A61K31/275;A61K31/336;A61K31/357;A61K31/36;A61K31/38;A61K31/381;A61K31/44;A61K31/4402;A61K31/4406;A61K31/4409;A61P1/00;A61P3/04;A61P3/08;A61P3/10;C07C311/08;C07C311/13;C07C311/21;C07D213/38;C07D213/64;C07D213/69;C07D213/71;C07D257/00;C07D303/36;C07D317/58;C07D317/66;C07D333/20;C07D333/58;(IPC1-7):A61K31/18;A61K31/22 主分类号 C07D295/12
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