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    • 6. 发明授权
    • Acylquinolinone derivatives, and antiallergic preparations and methods
of inhibiting allergic reactions using them
    • 酰基喹啉酮衍生物和抗过敏制剂以及使用它们抑制过敏反应的方法
    • US4476132A
    • 1984-10-09
    • US360016
    • 1982-03-19
    • Richard GoschkePier G. FerriniAlfred Sallmann
    • Richard GoschkePier G. FerriniAlfred Sallmann
    • A61K31/47A61P37/08C07D209/34C07D209/38C07D215/48C07D215/56C07D265/26C07D215/22
    • C07D265/26C07D209/34C07D209/38C07D215/48C07D215/56
    • Quinolinone derivatives of the formula (I) ##STR1## in which X represents oxy or a direct bond, R.sub.1 represents an aliphatic, cycloaliphatic, aromatic, araliphatic, heterocyclic or heterocyclic-aliphatic radical or hydrogen, Ph represents an optionally additionally substituted 1,2-phenylene radical containing the group R.sub.1 --X--C(O)--, and one of the radicals R.sub.2 and R.sub.3 represents an optionally esterified or amidated carboxy group R.sub.4 and the other represents hydrogen or an aliphatic radical or, in the case of a radical R.sub.3, hydroxy, and in which either R.sub.A and R.sub.B together represent oxo, R.sub.C and R.sub.D together represent an additional bond, or, when R.sub.2 represents a radical R.sub.4, R.sub.C is hydrogen and R.sub.3 and R.sub.D together represent oxo, and R.sub.E represents a radical R.sub.5 which represents hydrogen or an aliphatic, cycloaliphatic, araliphatic heterocyclic-aliphatic radical, or R.sub.A represents an optionally etherified hydroxy group and R.sub.B together with R.sub.C and also R.sub.D together with R.sub.E represent an additional bond in each case, or, when R.sub.2 represents a radical R.sub.4, R.sub.B and R.sub.C together represent an additional bond and R.sub.3 and R.sub.D together represent oxo and R.sub.E represents a radical R.sub.5, and their salts, have antiallergic properties. They are manufactured, for example, by subjecting a compound of the formula (IV) ##STR2## in which Z represents a removable radical, or a tautomer and/or salt thereof, to intramolecular cyclisation.
    • 式(I)的喹啉酮衍生物其中X表示氧基或直接键,R1表示脂族,脂环族,芳族,芳脂族,杂环或杂环 - 脂族基团或氢,Ph表示任选另外取代的 含有R1-XC(O) - 基团的1,2-亚苯基,其中一个基团R 2和R 3表示任选酯化或酰胺化的羧基R 4,另一个表示氢或脂族基,或者在 基团R3,羟基,其中RA和RB一起代表氧代,RC和RD一起表示另外的键,或者当R 2表示基团R 4时,RC是氢,R 3和R 4一起代表氧代,并且RE表示基团 代表氢或脂族,脂环族,脂环族杂环脂族基团的R 5或RA表示任选醚化的羟基,RB与RC一起,并且RD与RE一起代表另外的键 或者当R 2代表基团R 4时,R b和R c一起代表另外的键,并且R 3和R 4一起代表氧代,RE代表基团R 5,并且它们的盐具有抗过敏性质。 它们例如通过使其中Z表示可除去的基团或其互变异构体和/或其盐的式(IV)的化合物(IV)进行分子内环化来制备。
    • 7. 发明授权
    • Anti-inflammatory 2-sulphonyl- (or -sulphinyl)-2'-aminoacetophenones
    • 抗炎2-磺酰基 - (或 - 亚磺酰基)-2'-氨基苯乙酮
    • US4192873A
    • 1980-03-11
    • US846305
    • 1977-10-28
    • Pier G. FerriniRichard GoschkeAlfred SallmannAlberto Rossi
    • Pier G. FerriniRichard GoschkeAlfred SallmannAlberto Rossi
    • A61K31/135A61K31/18A61K31/255A61K31/44A61P7/02A61P29/00C07C67/00C07C313/00C07C315/04C07C317/28C07D213/70C07D213/71C07C87/50C07C87/60
    • A61K31/255
    • The invention relates to novel ortho-aminoacetophenones of the formula I ##STR1## and their tautomers, in which Z is hydrogen, halogen, lower alkyl, cycloalkyl, lower alkoxy, trifluoromethyl, nitro or substituted or unsubstituted sulphamoyl, m is 1 or 2, R is hydrogen, aryl or lower alkyl, R.sub.1 is hydrogen or lower alkyl, R.sub.2 is lower alkyl, cycloalkyl, aryl, cycloalkyl-lower alkyl, aryl-lower alkyl or substituted or unsubstituted pyridyl, R.sub.3 is hydrogen or lower alkyl and n is 1 or 2, with the exception of 2'-[N-(p-methoxyphenyl)-amino]-2-(methyl-sulphinyl)-acetophenone, 2'-amino-2-(methylsulphinyl)-acetophenone, 2'-amino-5'-chloro-2-(methylsulphinyl)-acetophenone, 2'-methylamino-2-(methylsulphinyl)-acetophenone, 2'-amino-5'-methyl-2-(methylsulphinyl)-acetophenone, 2'-amino-4'-chloro-2-(methylsulphinyl)-acetophenone, 2'-amino-6'-chloro-2-(methylsulphinyl)-acetophenone, 2'-amino-5',6'-dimethoxy-2-(methylsulphinyl)-acetophenone and 2'-amino-4',5'-dimethoxy-2-(methylsulphinyl)-acetophenone, and also to their salts.These compounds have a fibrinolytic and an antiinflammatory action.
    • 本发明涉及式I(I)的新型邻氨基苯乙酮及其互变异构体,其中Z为氢,卤素,低级烷基,环烷基,低级烷氧基,三氟甲基,硝基或取代或未取代的氨磺酰基,m为1 或2,R是氢,芳基或低级烷基,R1是氢或低级烷基,R2是低级烷基,环烷基,芳基,环烷基 - 低级烷基,芳基 - 低级烷基或取代或未取代的吡啶基,R3是氢或低级烷基, n为1或2,2' - [N-(对甲氧基苯基) - 氨基] -2-(甲基 - 亚磺酰基) - 苯乙酮,2'-氨基-2-(甲基亚磺酰基) - 苯乙酮,2' - 氨基-5'-氯-2-(甲基亚磺酰基) - 苯乙酮,2'-甲基氨基-2-(甲基亚磺酰基) - 苯乙酮,2'-氨基-5'-甲基-2-(甲基亚磺酰基) - 苯乙酮, 氨基-4'-氯-2-(甲基亚磺酰基) - 苯乙酮,2'-氨基-6'-氯-2-(甲基亚磺酰基) - 苯乙酮,2'-氨基-5',6'-二甲氧基-2-(甲基亚磺酰基 ) - 苯乙酮和2'-氨基-4',5'-二甲氧基-2-(甲基亚磺酰基) - 苯乙酮 ne,以及它们的盐。 这些化合物具有纤维蛋白溶解和抗炎作用。
    • 8. 发明授权
    • Novel 2-sulphonyl- (or -sulphinyl)-2'-aminoacetophenones
    • 新的2-磺酰基 - (或 - 亚磺酰基)-2'-氨基苯乙酮
    • US4263455A
    • 1981-04-21
    • US79605
    • 1979-09-27
    • Pier G. FerriniRichard GoschkeAlfred SallmannAlberto Rossi
    • Pier G. FerriniRichard GoschkeAlfred SallmannAlberto Rossi
    • A61K31/135A61K31/18A61K31/255A61K31/44A61P7/02A61P29/00C07C67/00C07C313/00C07C315/04C07C317/28C07D213/70C07D213/71C07C87/60C07C97/10
    • A61K31/255
    • The invention relates to novel ortho-aminoacetophenones of the formula I ##STR1## and their tautomers, in which Z is hydrogen, halogen, lower alkyl, cycloalkyl, lower alkoxy, trifluoromethyl, nitro or substituted or unsubstituted sulphamoyl, m is 1 or 2, R is hydrogen, aryl or lower alkyl, R.sub.1 is hydrogen or lower alkyl, R.sub.2 is lower alkyl, cycloalkyl, aryl, cycloalkyl-lower alkyl, aryl-lower alkyl or substituted or unsubstituted pyridyl, R.sub.3 is hydrogen or lower alkyl and n is 1 or 2, with the exception of 2'-[N-(p-methoxyphenyl)-amino]-2-(methyl-sulphinyl)-acetophenone, 2'-amino-2-(methylsulphinyl)-acetophenone, 2'-amino-5'-chloro-2-(methylsulphinyl)-acetophenone, 2'-methylamino-2-(methylsulphinyl)-acetophenone, 2'-amino-5'-methyl-2-(methylsulphinyl)-acetophenone, 2'-amino-4'-chloro-2-(methylsulphinyl)-acetophenone, 2'-amino-6'-chloro-2-(methylsulphinyl)-acetophenone, 2'-amino-5',6'-dimethoxy-2-(methylsulphinyl)-acetophenone and 2'-amino-4',5'-dimethoxy-2-(methylsulphinyl)-acetophenone, and also to their salts.These compounds have a fibrinolytic and an antiinflammatory action.
    • 本发明涉及式I(I)的新型邻氨基苯乙酮及其互变异构体,其中Z为氢,卤素,低级烷基,环烷基,低级烷氧基,三氟甲基,硝基或取代或未取代的氨磺酰基,m为1 或2,R是氢,芳基或低级烷基,R1是氢或低级烷基,R2是低级烷基,环烷基,芳基,环烷基 - 低级烷基,芳基 - 低级烷基或取代或未取代的吡啶基,R3是氢或低级烷基, n为1或2,2' - [N-(对甲氧基苯基) - 氨基] -2-(甲基 - 亚磺酰基) - 苯乙酮,2'-氨基-2-(甲基亚磺酰基) - 苯乙酮,2' - 氨基-5'-氯-2-(甲基亚磺酰基) - 苯乙酮,2'-甲基氨基-2-(甲基亚磺酰基) - 苯乙酮,2'-氨基-5'-甲基-2-(甲基亚磺酰基) - 苯乙酮, 氨基-4'-氯-2-(甲基亚磺酰基) - 苯乙酮,2'-氨基-6'-氯-2-(甲基亚磺酰基) - 苯乙酮,2'-氨基-5',6'-二甲氧基-2-(甲基亚磺酰基 ) - 苯乙酮和2'-氨基-4',5'-二甲氧基-2-(甲基亚磺酰基) - 苯乙酮 ne,以及它们的盐。 这些化合物具有纤维蛋白溶解和抗炎作用。