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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。
    • 7. 发明授权
    • Substituted O-(2-hydroxypropyl)-aldoximes
    • 取代的O-(2-羟丙基) - 肟
    • US4235899A
    • 1980-11-25
    • US849936
    • 1977-11-09
    • Ulrich GebertWolfgang Raether
    • Ulrich GebertWolfgang Raether
    • A61K31/341A61K31/345A61K31/395A61K31/415A61K31/4427A61K31/443A61K31/445A61K31/495A61P33/02C07D233/95C07D307/73C07D401/12C07D403/12C07D405/12C07D407/12C07D413/12
    • C07D307/73C07D233/95
    • Compounds of general formula ##STR1## wherein X represents a methine group and Y is an oxygen atom, or X represents a nitrogen atom and Y the group NR.sup.3 in which R.sup.3 represents a radical selected from the group consisting of a hydrogen atom, a methyl, ethyl and hydroxyethyl group; and R.sup.1 and R.sup.2 each represent a radical of the group hydrogen atom, an alkyl and hydroxyalkyl group each containing up to 6 carbon atoms, or an aryl group containing up to 10 carbon atoms; and R.sup.1 and R.sup.2, together with the nitrogen atom to which they are attached, form a 5- to 7-membered saturated ring which contains not more than one further, heterocyclic atom selected from the group consisting of oxygen, sulphur and nitrogen and being unsubstituted or substituted by one of the groups an alkyl and hydroxyalkyl group each containing up to 6 carbon atoms and an aryl group containing up to 10 carbon atoms and physiologically acceptable acid addition salts thereof and a pharmaceutical composition containing them.
    • 通式(I)的化合物,其中X表示次甲基,Y是氧原子,或X表示氮原子,Y表示NR3基团,其中R3表示选自氢原子, 甲基,乙基和羟乙基; 并且R 1和R 2各自表示基团氢原子的基团,各自含有至多6个碳原子的烷基和羟烷基,或含有至多10个碳原子的芳基; 并且R 1和R 2与它们所连接的氮原子一起形成5-至7-元饱和环,其含有不多于一个另外的选自氧,硫和氮的杂环原子,并且是未被取代的 或者由一个基团取代各自含有至多6个碳原子的烷基和羟基烷基和含有至多10个碳原子的芳基及其生理上可接受的酸加成盐和含有它们的药物组合物。