公开(公告)号：US3968214A

公开(公告)日：1976-07-06

申请号：US406129

申请日：1973-10-12

申请人： Jean-Marie Claverie ,  Gerard Loiseau ,  Georges Mattioda ,  Rene Millischer ,  Francois Percheron

发明人： Jean-Marie Claverie ,  Gerard Loiseau ,  Georges Mattioda ,  Rene Millischer ,  Francois Percheron

IPC分类号： C07D239/46 ,  C07D239/48 ,  C07D239/56 ,  A61K31/505

CPC分类号： C07D239/47 ,  C07D239/48 ,  C07D239/56

摘要： The compounds of the formula: ##SPC1##In which Y represents a chlorine atom or an alkoxy, dialkylaminoalkoxy, pyridylalkoxy group, R.sub.1 and R.sub.2 are identical or different substituents and represent alkyl or alkoxycarbonylalkyl groups, substituted or unsubstituted phenyl groups or form together with the nitrogen atom to which they are attached, a heterocyclic ring which may contain another hetero-atom, R.sub.3 and R.sub.4 are identical or different substituents and represent alkyl groups or form, together with the nitrogen atom to which they are attached, a heterocyclic ring which may contain another hetero-atom; process for their preparation; medicaments comprising such compounds or salts thereof, and their use in the treatment of human beings.The present invention relates to new pyrimidines, to their use as medicaments on account of their spasmolytic, coronary dilator and hypoglycemiant properties and to their preparation.These compounds, derived from 5-methylthio-pyrimidine, may be represented by the general formula: ##SPC2##In which Y represents a chlorine atom or an alkoxy, dialkylaminoalkoxy or pyridylalkoxy group, the alkoxy and alkyl groups preferably containing 1 to 4 carbon atoms, R.sub.1 and R.sub.2 are identical or different substituents and represent alkyl, alkoxycarbonylalkyl, substituted or unsubstituted phenyl or benzyl groups or form, together with the nitrogen atom to which they are attached, a heterocyclic ring which may contain another hetero-atom, the alkyl and alkoxy groups preferably containing 1 to 4 carbon atoms, R.sub.3 and R.sub.4 are identical or different substituents and represent alkyl groups preferably containing 1 to 4 carbon atoms or form, together with the nitrogen atom to which they are attached, a heterocyclic ring which may possibly contain another hetero-atom.Substituents of the phenyl group may be for example halogen atoms or alkyl, alkoxy or trihalomethyl groups.The compounds of formula (I) may be prepared for example by reacting a compound of the formula: ##SPC3##In which R.sub.1 and R.sub.2 have the same significance as above, with an ethylenediamine of the formula: ##EQU1## in which R.sub.3 and R.sub.4 have the same significance as above, and possibly replacing the remaining chlorine atom by an alkoxy, dialkylamino-alkoxy or pyridylalkoxy group.The reaction with the compound of formula (III) is preferably effected in a solvent, in the presence of an acid-absorbing agent, at a temperature between 20.degree.C. and 100.degree.C.The substitution of the remaining chlorine atom may be effected for example by the action of an alcoholate of an alkali metal or by the action of an excess of the corresponding alcohol and caustic potash at the refluxing temperature.

摘要翻译： 下式的化合物：