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3-AMINO-5-SUBSTITUTED-6-HALO-N-(3,4-DIHYDRO- OR 4,4-DISUBSTITUTED-6-SUBSTITUTED-1,3,5-TRIAZIN-2-YL)-2-PYRAZINECARBOXAMIDES, PROCESS FOR PREPARING AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME
3-AMINO-5-SUBSTITUTED-6-HALO-N-(3,4-DIHYDRO- OR 4,4-DISUBSTITUTED-6-SUBSTITUTED-1,3,5-TRIAZIN-2-YL)-2-PYRAZINECARBOXAMIDES, PROCESS FOR PREPARING AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME
This invention relates to 3-amino-5-substituted-6- halo-N-(3,4-dihydro- or 4,4-disubstituted-6-substituted- 1,3,5-triazin-2-yl)-2-pyrazinecarboxamides. The invention also relates to processes for preparing those compounds of the formula of the tautomeric form thereof CHEM wherein R is hydrogen,, C1-5 alkyl, C2-5 alkenyl or C3-6 cycloalkyl; R1 is hydrogen, C1-5 alkyl, C2-5 alkenyl or C3-6 cycloalkyl; R2 is hydrogen, or C1-5 alkyl; R3 is hydrogen, or C1-5 alkyl; R2 and R3 can be joined with the carbon atom to which they are attached to form a 3-7 membered carbon ring; X is halo Y is OH, SH, C1-5 alkoxy, C1-5 alkylthio and NR4R5 wherein R4 is hydrogen or C1-5 alkyl and R5 is hydrogen, C1-5 alkyl, CN, CONH2, CNH2, NO2 or NH2 NH and the pharmaceutical acid addition salts thereof. The compounds are eukalemic/saluretic agents useful in the treatment of edema and hypertension.
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机译:本发明涉及3-氨基-5-取代-6-卤代N-(3,4-二氢-或4,4-二取代-6-取代的1,3,5-三嗪-2-基)-2 -吡嗪羧酰胺。本发明还涉及制备其互变异构形式的那些式的那些化合物的方法,其中R是氢,C 1-5烷基,C 2-5烯基或C 3-6环烷基; R 1为氢,C 1-5烷基,C 2-5烯基或C 3-6环烷基; R 2为氢或C 1-5烷基; R 3为氢或C 1-5烷基; R 2和R 3可以与它们所连接的碳原子连接而形成3-7元碳环。 X是卤素Y是OH,SH,C 1-5烷氧基,C 1-5烷硫基和NR 4 R 5,其中R 4是氢或C 1-5烷基,R 5是氢,C 1-5烷基,CN,CONH 2,CNH 2,NO 2或NH 2 NH及其药物酸加成盐。所述化合物是可用于治疗水肿和高血压的真核生物/利尿剂。
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