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New derivatives of octahydro-6, 10-dioxo-6H-pyridazino 1,2-A1,2diazepine-1-carboxylic acid, their preparation process and their use in the preparation of therapeutically active compounds
New derivatives of octahydro-6, 10-dioxo-6H-pyridazino 1,2-A1,2diazepine-1-carboxylic acid, their preparation process and their use in the preparation of therapeutically active compounds
The invention relates to compounds of general formula (I) ##STR1## wherein R is selected from ethyl, n-propyl, iso-propyl, n-butyl, iso- butyl, sec.-butyl and allyl; R.sub.4 is selected from hydrogen and pharmaceutically acceptable inorganic and organic cations; R.sub.5 is selected from methyl, ethyl, n-propyl, iso-propyl, methoxy, ethoxy, chloro, bromo, CF.sub.3, and OCH.sub.x F.sub.y ; wherein x=0-2, y=1-3 with the proviso that x+y=3; R.sub.6 is hydrogen; or R.sub.5 and R.sub.6 taken together are methylenedioxy; and any tautomer hereof. The invention also relates to pharmaceutical compositions containing a compound of the general formula (I) together with a pharmaceutically acceptable carrier. Included are also processes for the preparation of the compounds of formula (I), as well as methods of treating mammals suffering from diseases resulting from autoimmunity and pathological inflammation by administering a compound having the formula (I) to said mammal.
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机译:本发明涉及通式(I)的化合物,其中R选自乙基,正丙基,异丙基,正丁基,异丁基,仲丁基和烯丙基; R.sub.4选自氢以及药学上可接受的无机和有机阳离子; R 5选自甲基,乙基,正丙基,异丙基,甲氧基,乙氧基,氯,溴,CF 3和OCH xF。其中x = 0-2,y = 1-3,条件是x + y = 3; R 6是氢;或R 5和R 6一起是亚甲基二氧基;或及其任何互变异构体。本发明还涉及含有通式(I)的化合物和药学上可接受的载体的药物组合物。还包括制备式(I)化合物的方法,以及通过向所述哺乳动物施用具有式(I)的化合物来治疗患有由于自身免疫和病理性炎症导致的疾病的哺乳动物的方法。
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