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    • 31. 发明授权
    • Acetal derivatives of
6-phenyl-4H-s-triazolo[4,3-a][1,4]benzodiazepine-1-carboxaldehyde
    • 6-苯基-4H-s-三唑并[8,3,3-a {9 {8 1,4 {9苯并二氮杂-1-甲醛
    • US3946032A
    • 1976-03-23
    • US406060
    • 1973-10-12
    • Hans AllgeierAndre Gagneux
    • Hans AllgeierAndre Gagneux
    • C07D487/04
    • C07D487/04
    • Compounds of the class of acetals of 6-phenyl-4H-s-triazolo[4,3-a][1,4]benzodiazepine-1-carboxaldehyde and the 5-oxides and pharmaceutically acceptable acid addition salts thereof have valuable pharmacological properties, in particular anticonvulsant effectiveness. Further, they show central depressant and muscle-relaxing activity and are active ingredients for therapeutic preparations. Specific embodiments are 6-phenyl-8-chloro-4H-s-triazolo[4,3-a][1,4]benzodiazepine-1-carboxaldehyde-diethylacetal, 6-(o-chlorophenyl)-8-chloro-4H-s-triazolo[4,3-a][1,4]benzodiazepine-1-carboxaldehyde-diethylacetal and 6-(o-fluorophenyl-8-chloro-4H-s-triazolo[4,3-a][1,4]benzodiazepine-1-carboxaldehyde-diethylacetal.
    • 6-苯基-4H-3-三唑并[4,3-a] [1,4]苯并二氮杂-1-甲醛的缩醛类化合物及其5-氧化物和药学上可接受的酸加成盐具有有价值的药理学性质, 特别是抗惊厥效果。 此外,它们显示中枢抑制剂和肌肉松弛活性,并且是治疗制剂的活性成分。 具体实施方案是6-苯基-8-氯-4H-三唑并[4,3-a] [1,4]苯并二氮杂1-甲醛二乙基缩醛,6-(邻氯苯基)-8-氯-4H - 三唑并[4,3-a] [1,4]苯并二氮杂-1-甲醛 - 二乙基缩醛和6-(邻 - 氟苯基-8-氯-4H-三唑并[4,3-a] 4]苯并二氮杂-1-c芳樟醛 - 二乙基缩醛。
    • 35. 发明授权
    • Etherified triazolobenzodiazepine derivatives
    • 醚化三唑并苯并二氮杂衍生物
    • US4178378A
    • 1979-12-11
    • US833421
    • 1977-09-15
    • Hans AllgeierAndre Gagneux
    • Hans AllgeierAndre Gagneux
    • A61K31/53A61K31/55A61P25/08A61P25/20C07D317/22C07D487/04A61K31/62
    • C07D487/04C07C243/00C07D317/22
    • Etherified diazepine derivatives of the formula ##STR1## in which R.sub.1 represents hydrogen or alkyl having up to 3 carbon atoms, R.sub.2 and R.sub.3 independently of one another each represent hydrogen or alkyl having up to 7 carbon atoms, or represent the partial formula R.sub.4 --(OCH.sub.2 --CH.sub.2).sub.m, in which R.sub.4 represents hydrogen or alkyl having up to 7 carbon atoms and m represents the number 1 to 3, A.sub.1 represents alkylidene or alkylene having up to 3 carbon atoms, A.sub.2, depending on the meaning of n, represents alkylene or alkanetriyl having up to 5 carbon atoms, no carbon atom in the radical A.sub.2 being bonded to more than one oxygen atom, n represents the number 0 or 1, Ph represents substituted or unsubstituted 1,2-phenylene and Ar represents an aromatic radical, and their addition salts are manufactured according to methods known per se. They are useful in the treatment of states of epilepsy, stress and agitation.
    • 其中R 1表示氢或具有至多3个碳原子的烷基的式(I)的醚化二氮杂衍生物,R 2和R 3彼此独立地表示氢或具有至多7个碳原子的烷基,或表示部分式 R 4 - (OCH 2 -CH 2)m,其中R 4表示氢或具有至多7个碳原子的烷基,m表示数1至3,A 1表示亚烷基或具有至多3个碳原子的亚烷基,取决于 n表示具有至多5个碳原子的亚烷基或烷三三基,基团A2中的碳原子不连接至多于一个氧原子,n表示数字0或1,Ph表示取代或未取代的1,2-亚苯基,Ar表示 芳族基团,并且它们的加成盐按照本身已知的方法制备。 它们可用于治疗癫痫,压力和激动的状态。
    • 40. 发明授权
    • 3-heteroaliphatyl- and 3-hetero(aryl)aliphatyl-2(1H)-quinolone
derivatives
    • 3-杂芳基和3-杂芳基芳基-2(1H) - 喹诺酮衍生物
    • US5633379A
    • 1997-05-27
    • US456358
    • 1995-06-01
    • Hans Allgeier
    • Hans Allgeier
    • A61K31/47A61P9/00A61P9/10A61P25/00A61P25/04A61P25/20A61P25/28C07D215/22C07D215/36C07D401/12C07D405/12C07D409/12C07D215/20C07D215/227
    • C07D215/22C07D215/36C07D401/12C07D405/12C07D409/12
    • 3-Heteroaliphatyl- and 3-hetero(aryl)aliphatyl-2(1H)quinolone derivatives of formula I ##STR1## wherein the radicals R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are each independently of the others hydrogen, an aliphatic hydrocarbon radical, free or etherified hydroxy, mercapto or etherified and/or oxidised mercapto, unsubstituted or aliphaticaliy substituted amino, nitro, free or esterified or amidated carboxy, cyano, free or amidated sulfamoyl, halogen or trifluoromethyl, X is oxy or optionally oxidised thio, A is a divalent aliphatic radical and R.sub.5 is an optionally partially hydrogenated aryl or heteroaryl radical that is unsubstituted or substituted by aliphatic or araliphatic hydrocarbon radicals, by free or etherified hydroxy, by mercapto or etherified and/or oxidised mercapto, by unsubstituted or aliphatically substituted amino, by aliphatic acyl, by free or esterified or amidated carboxy, by cyano, by free or amidated sulfamoyl, by halogen and/or by trifluoromethyl; free or etherified hydroxymethyl; cyano; or free or esterified or amidated carboxy, and tautomers and/or salts thereof, have antagonistic properties with respect to excitatory amino acids and can be used for the treatment of pathological conditions that are responsive to glycine-antagonistic blocking of NMDA-sensitive receptors.
    • 其中基团R 1,R 2,R 3和R 4各自独立地为氢,脂族烃基(C 1 -C 6)烷基, 游离或醚化的羟基,巯基或醚化的和/或氧化的巯基,未取代的或脂族取代的氨基,硝基,游离或酯化或酰胺化的羧基,氰基,游离或酰胺化的氨磺酰基,卤素或三氟甲基,X是氧或任选被氧化的硫代, R5是任选部分氢化的芳基或杂芳基,其未被取代或被脂肪族或芳脂族烃基取代,被游离的或醚化的羟基,被巯基或醚化和/或氧化的巯基取代,被未取代的或脂族取代的氨基 由脂族酰基,游离或酯化或酰胺化的羧基,氰基,游离或酰胺基氨磺酰基,卤素和/或三氟甲基取代; 游离的或醚化的羟甲基; 氰基; 或游离的或酯化的或酰胺化的羧基及其互变异构体和/或其盐对兴奋性氨基酸具有拮抗作用,并且可用于治疗对甘氨酸拮抗性阻断NMDA敏感性受体有反应的病理状况。