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    • 6. 发明授权
    • Antimalarial compositions
    • 抗疟组成
    • US4284627A
    • 1981-08-18
    • US166295
    • 1980-07-07
    • Wolfgang RaetherWalter DurckheimerHans Seidenath
    • Wolfgang RaetherWalter DurckheimerHans Seidenath
    • C07D219/06A61K31/44A61K31/445A61K31/47A61K31/49A61K31/505A61K31/53A61K31/635A61P33/02A61K31/625A61K31/435
    • A61K31/635A61K31/44A61K31/47A61K31/49A61K31/505A61K31/53Y10S514/895
    • Antimalarial compositions are disclosed containing as the active ingredient a mixture of a tetrahydroacridone of the general formula I ##STR1## in which R.sup.1 represents methyl, phenyl, p-chlorophenyl, m-chlorophenyl, p-fluorophenyl, p-trifluoromethylphenyl, o-trifluoromethylphenyl or o-chloro-p-trifluoromethylphenyl,R.sup.2 represents hydrogen or methyl, andR.sup.3 represents fluorine or chlorine,or a salt of such a compound with a physiologically compatible acid or base, with(a) 6-methoxy-.alpha.-(5-vinyl-2-quinuclidinyl)-4-quinoline-methanol (Quinine),(b) 7-chloro-4-(diethylamino-1-methyl-butylamino)-quinoline (Chloroquine),(c) .alpha.-(2-piperidyl)-2,8-bis(trifluoromethyl)-4-quinolinemethanol (Mefloquine),(d) 8-(4-amino-1-methylbutylamino)-6-methoxy-quinoline (Primaquine),(e) 2,4-diamino-5-p-chlorophenyl-6-ethylpyrimidine (Pyrimethamine),(f) 4,6-diamino-1-(p-chlorophenyl)-1,2-dihydro-2,2-dimethyl-s-triazine (Cycloguanil),(g) 2,4-diamino-5-(3,4,5-trimethoxybenzyl)-pyrimidine (Trimethoprim),(h) N'-(5,6-dimethoxy-4-pyrimidyl)-sulfanilamide (Sulfadoxine), or(i) 4,4'-diaminodiphenylsulfone (Dapsone),or with a salt of a compound sub (a) to (i), with a physiologically compatible acid or base, the mixtures being in a proportion by weight of between 25:1 and 1:300 (tetrahydroacridone to compound sub (a) to (i)) in admixture with a pharmaceutically acceptable carrier and/or adjuvant.This is a division of application Ser. No. 954,900, filed October 26, 1978.
    • 公开了抗疟组合物,其包含作为活性成分的通式I的四氢吖啶酮的混合物,其中R 1表示甲基,苯基,对氯苯基,间氯苯基,对氟苯基,对三氟甲基苯基,邻三氟甲基苯基或对 - 邻 - 氯 - 对三氟甲基苯基,R 2代表氢或甲基,R 3代表氟或氯,或这种化合物与生理相容的酸或碱的盐与(a)6-甲氧基-α-(5-乙烯基 -2-喹喔啉基)-4-喹啉 - 甲醇(奎宁),(b)7-氯-4-(二乙基氨基-1-甲基 - 丁基氨基) - 喹啉(氯喹),(c)α-(2-哌啶基) 2,8-双(三氟甲基)-4-喹啉甲醇(Mefloquine),(d)8-(4-氨基-1-甲基丁基氨基)-6-甲氧基 - 喹啉(Primaquine),(e)2,4-二氨基-5 对 - 氯苯基-6-乙基嘧啶(Pyrimethamine),(f)4,6-二氨基-1-(对氯苯基)-1,2-二氢-2,2-二甲基-s-三嗪(Cycloduanil),(g )2,4-二氨基-5-(3,4,5-三甲氧基苄基) - 嘧啶(Trimethopri m),(h)N' - (5,6-二甲氧基-4-嘧啶基) - 磺胺(磺胺多辛),或(i)4,4'-二氨基二苯砜(氨苯砜),或与化合物 )至(i)与生理上相容的酸或碱,所述混合物的重量比为25:1至1:300(四氢吖啶酮与化合物(a)至(i))的混合物与药学上可接受的 载体和/或佐剂。