SUBSTITUTED AMIDE DERIVATIVES OF PIPERIZINYLCAMPHORSULFONYL OXYTOCIN ANTAGONISTS

摘要

Compound formula:Compounds, corresponding to this structural formula, when R<1> is:hydrogen, alkoxycarbonyl or unchanged or changed alkyl, when the mentioned substitute is hydroxyl, alkoxyl, carboxyl, carboxyalkyl, alkylsulfonyl or alkoxycarbonyl;and R<2> ishydrogen, alkoxyl, arylalkoxyl, alkoxycarbonyl, alkoxycarbonylamin, unchanged or changed cycloalkyl, when the mentioned substitute is carboxyl, (7) unchanged or changed phenyl, when the mentioned substitute or several substitutes belong to the group which includes carboxyl, carboxyalkyl or SO3H, unchanged or changed amine, when the mentioned substitute is unchanged or changed alkyl, comprising one or several substitutes, as well as carboxyl, alkylsulfonyl or unchanged pentanomial heterocycle ring with 1 or 2 heteroatoms, when the heteroatom is N,unchanged or changed rings that are expressed in the formulaswhen the mentioned substitutes is one or several radicals, including alkyl, carboxyl, carboxyalkyl, carboxyarylalkyl, arylalkylcarbonyl, arylalkoxycarbonyl, alkoxycarbonyl, alkoxycarbonylalkyl, alkoxycarbonylaminoalkylcarbonyl, oxygroup or changed amine, when the mentioned substitute is made of one or several radicals including alkyl, carboxyalkyl, alkoxycarbonyl or alkoxycarbonyl or alkoxycarbonylalkyl, or (10) unchanged or changed alkyl, when the mentioned substitute is made of one or several radicals including hydrocyl, carboxyl, carboxyalkyl phenyl, alkylsulfonyl, amine carbonyl, alkylaminocarbonyl, aryl alkyl, arylalkoxycarbonyl, halogen, alkoxycarbonyl, alkoxycarbonylalkyl, Het or unchanged/changed amine, when the mentioned substitute is one or several radicals, including alkyl, alkyl carbonyl, alkylsulfonyl, carboxyalkyl. Cyc, alkoxycarbonyl, alkoxycarbonylalkyl, arylalkoxycarbonyl, aminocarbonylalkyl, alkylaminocarbonyl, phenyl alkyl or unchanged/changed alkyl carbonyl, when the mentioned substitute is pentanomial heterocycle ring with 1 or 2 heteroatoms and when the heteroatoms herein are N, when Het values provided above for heterocycle rings and when Cyc is changed/unchanged cycloalkyl, when the mentioned substitute is selected from the group including alkoxycarbonyl, carboxyl, hydroxyl, oxygroup or spirodioxolinyl. These compounds are oxytocin antagonist and are useful for treating abortive birth, dysmenorrhea and for trying to stop the preparation for Caesarean sections.