CATECHOLAMINE SURROGATES USEFUL AS BETA-3 ANTAGONISTS

• Main Authors: GAVAI,ASHVINIKUMAR, BISACCHI,GREGORY S, SHER,PHILIP M, MIKKILINENI,AMARENDRA B, GIROTRA,RAVINDAR N, POSS,KATHLEEN M, MATHUR,ARVIND, WASHBURN,WILLIAM N
• Format: Patent
• Language: English
• Published: 29.04.1996
• Edition: 6
• Subjects: ACYCLIC OR CARBOCYCLIC COMPOUNDS; CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

Compounds of the formula 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(R )R<9'> or -CO2R ; R is lower alkyl, aryl or arylalkyl; R is hydrogen, hydroxy, alkoxy, -CH2OH, cyano, -C(O)OR , -CO2H, -CONH2, tetrazole, -CH2NH2 or halogen; R is hydrogen, alkyl, heterocycle or R is hydrogen, alkyl or B; R , R<5'>, R , R<8'> or R<8''> are independently hydrogen, alkoxy, lower alkyl, halogen, -OH, -CN, -(CH2)nNR COR , -CON(R )R<6'>, -CON(R )OR<6'>, -CO2R , -SR , -SOR , -SO2R , -N(R )SO2R , -N(R )R<6'>, -NR COR , -OCH2CON(R )R<6'> , -OCH2CO2R or aryl; or R and R<5'> or R and R<8'> may together with the carbon atoms to which they are attached form an aryl or heterocycle; R and R<6'> are independently hydrogen or lower alkyl; and R is lower alkyl; R is hydrogen, lower alkyl, alkyl, cycloalkyl, arylalkyl, aryl, heteroaryl; or R and R<9'> may together with the nitrogen atom to which they are attached form a hetocycle; with the proviso that when A is a bond or -(CH2)n and R is hydrogen or unsubstituted alkyl, then R 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.