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    • 5. 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。
    • 6. 发明授权
    • Alkanecarboxylic acid compounds which have benzofuranyl or benzothienyl
substituents
    • 具有苯并呋喃基或苯并噻吩基取代基的烷烃羧酸化合物
    • US4187234A
    • 1980-02-05
    • US931055
    • 1978-08-04
    • Raymond BernasconiPier G. Ferrini
    • Raymond BernasconiPier G. Ferrini
    • C07D307/80C07D333/56
    • C07C323/00C07C45/71C07D307/80C07D333/56
    • Compounds of the formula ##STR1## in which Ar represents optionally substituted 1,2-phenylene, X.sub.1 represents oxygen or sulphur, R.sub.1 represents the radical of the formula ##STR2## in which Ph represents optionally substituted phenylene, X.sub.2 represents oxygen or sulphur, R.sub.3 and R.sub.4 independently of one another denote hydrogen or alkyl and R.sub.5 represents optionally etherified hydroxyl or optionally substituted amino and in which R.sub.2 denotes hydrogen, lower alkyl or the radical of the formula Ia and one of the groups R.sub.1 and R.sub.2 takes up the 2-position and the other takes up the 3-position, and salts of such compounds having salt-forming groups, e.g. ethyl 2-[4-(2-benzofuranyl)-phenoxy]-heptanoate. These compounds may be used as fibrinolytic and thrombolytic agents.
    • 式(Ⅰ)化合物其中Ar表示任意取代的1,2-亚苯基,X1表示氧或硫,R1表示式(Ia)中的基团,其中Ph表示任意取代的亚苯基,X2 R 3和R 4彼此独立地表示氢或烷基,R 5表示任选醚化的羟基或任选取代的氨基,其中R 2表示氢,低级烷基或式Ia基团和基团R 1和R 2之一 占据2-位,另一个占据3位,并且这些具有成盐基团的化合物的盐例如 2- [4-(2-苯并呋喃基) - 苯氧基] - 庚酸乙酯。 这些化合物可以用作纤维蛋白溶解和溶栓剂。
    • 9. 发明授权
    • Certain 2,4,5-tri-substituted thiazoles, pharmaceutical compositions
containing same and methods of using same
    • US4451471A
    • 1984-05-29
    • US355989
    • 1982-03-08
    • Pier G. FerriniRichard Goschke
    • Pier G. FerriniRichard Goschke
    • C07D277/20A61K31/425A61K31/426A61K31/44A61P29/00C07D213/50C07D277/24C07D277/30C07D277/32C07D277/36C07D417/04C07D417/12C07D513/04
    • C07D277/32C07D213/50C07D277/24C07D277/30C07D277/36C07D513/04
    • 2,4,5-Trisubstituted thiazoles of the formula ##STR1## in which each of R.sub.1 and R.sub.2, independently of the other, represents an aryl or optionally N-oxidized heteroaryl radical each of which is unsubstituted or substituted by aliphatic hydrocarbon radicals, free, etherified or esterified hydroxy, etherified optionally S-oxidized mercapto, aliphatically substituted amino and/or trifluoromethyl,X represents thio,n represents 0, 1, or 2, andR.sub.3 represents an aliphatic hydrocarbon radical that is unsubstituted or substituted by etherified or esterified hydroxy, etherified optionally S-oxidized mercapto and/or, in a position higher than the .alpha.-position, by oxo and/or hydroxy and optionally contains, in addition to terminally bonded hydroxy, sulpho that is present in salt form, or represents an araliphatic hydrocarbon radical that is unsubstituted or substituted in the aryl moiety as indicated for R.sub.1 and R.sub.2, or represents a cycloaliphatic or cycloaliphatic-aliphatic hydrocarbon radical that is unsubstituted or substituted in a position higher than the .alpha.-position by free, etherified or esterified hydroxy, or represents a group of the formula ##STR2## in which m represents, 0, 1 or 2, R.sub.4 represents an aliphatic hydrocarbon radical that is unsubstituted or substituted by etherified or esterified hydroxy, optionally S-oxidized etherified mercapto or, in a position higher than the .alpha.-position and lower than the .omega.-position, by oxo and/or hydroxy and that is optionally interrupted by oxa or thia, which may also be S-oxidized, or, if n and m represent O, represents a direct bond, and R.sub.1 ' and R.sub.2 ' have one of the meanings given for R.sub.1 and R.sub.2,and pharmaceutically acceptable salts thereof are suitable for combating rheumatic disorders, preferably as active ingredients in anti-rheumatic medicaments. The invention relates to medicaments of this type and to non-chemical processes for their manufacture, and also to novel compounds of the formula I and to processes for their manufacture.
    • 10. 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。