| 摘要 |
Compounds of the formula: <CHEM> Compounds according to the structural formula, wherein R<1> is (1) hydrogen, (2) alkoxycarbonyl or (3) unsubstituted or substituted alkyl wherein said substituent is hydroxyl, alkoxyl, carboxyl, carboxyalkyl., alkylsulfonyl or alkoxycarbonyl; and R<2> is (1) hydrogen, (2) alkoxyl, (3) aralkoxyl, (4) alkoxycarbonyl, (5) alkoxycarbonylamino, (6) unsubstituted or substituted cycloalkyl, wherein said substituent is carboxyl, (7) unsubstituted or substituted phenyl wherein said substituent is one or more of carboxyl, carboxyalkyl or SO3H, (8) unsubstituted or substituted amino, wherein said substituent is unsubstituted or substituted alkyl where said substituent is one or more of carboxyl, alkylsulfonyl or unsubstituted 5-membered heterocyclic rings having 1 or 2 heteroatoms, where said heteroatom is N, (9) unsubstituted or substituted rings of the formulae <CHEM> where said substituents are one or more of alkyl, carboxyl, carboxyalkyl, carboxyaralkyl, aralkylcarbonyl, aralkoxycarbonyl, alkoxycarbonyl, alkoxycarbonylalkyl, alkoxycarbonylaminoalkylcarbonyl, oxo or unsubstituted or substituted amino wherein said substituent is one or more of alkyl, carboxylalkyl, alkoxycarbonyl or alkoxycarbonylalkyl or (10) unsubstituted or substituted alkyl, wherein said substituent is one or more of hydroxyl, carboxyl, carboxyalkylphenyl, alkylsulfonyl, aminocarbonyl, alkylaminocarbonyl, aralkyl, aralkoxycarbonyl, halogen, alkoxycarbonyl, alkoxycarbonylalkyl, Het or unsubstituted or substituted amino, wherein said substituent is one or more of alkyl, alkylcarbonyl, alkylsulfonyl, carboxyalkyl, Cyc, alkoxycarbonyl, alkoxycarbonylalkyl, aralkoxycarbonyl, aminocarbonylalkyl, alkylaminocarbonyl, phenalkyl or unsubstituted or substituted alkylcarbonyl, where said substituent is a 5-membered heterocyclic ring having 1 or 2 heteroatoms and where said hetero atom is N, where Het is defined as for the above heterocyclic rings and where Cyc is defined as substituted or unsubstituted cycloalkyl wherein said substituent is selected from the group consisting of alkoxycarbonyl, carboxyl, hydroxyl, oxo or spiro-dioxolinyl . Such compounds are oxytocin antagonists useful in the treatment of preterm labor, dysmenorrhea and for the stoppage of labor preparatory to cesarean delivery. r |
