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11. 发明授权

US4263455A Novel 2-sulphonyl- (or -sulphinyl)-2'-aminoacetophenones 失效
标题翻译：新的2-磺酰基 - （或 - 亚磺酰基）-2'-氨基苯乙酮
公开(公告)号：US4263455A
公开(公告)日：1981-04-21
申请号：US79605
申请日：1979-09-27
申请人： Pier G. Ferrini , Richard Goschke , Alfred Sallmann , Alberto Rossi
发明人： Pier G. Ferrini , Richard Goschke , Alfred Sallmann , Alberto Rossi
IPC分类号： A61K31/135 , A61K31/18 , A61K31/255 , A61K31/44 , A61P7/02 , A61P29/00 , C07C67/00 , C07C313/00 , C07C315/04 , C07C317/28 , C07D213/70 , C07D213/71 , C07C87/60 , C07C97/10
CPC分类号： A61K31/255
摘要： 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.
摘要翻译：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。

12. 发明授权

US4013708A Arylchalcogeno-substituted aliphatic acids and esters 失效
标题翻译： ARYLCHALCOGENO取代的脂肪酸和酯
公开(公告)号：US4013708A
公开(公告)日：1977-03-22
申请号：US505111
申请日：1974-09-11
申请人： Georges Haas , Pier Giorgio Ferrini , Alberto Rossi
发明人： Georges Haas , Pier Giorgio Ferrini , Alberto Rossi
IPC分类号： C07C69/736 , A61K31/00 , A61K31/085 , A61K31/18 , A61K31/185 , C07C20060101 , C07C43/20 , C07C51/00 , C07C59/125 , C07C59/60 , C07C59/68 , C07C59/70 , C07C65/00 , C07C67/00 , C07C69/22 , C07C69/66 , C07C69/67 , C07C69/712 , C07C69/76 , C07C301/00 , C07C303/02 , C07C303/22 , C07C303/32 , C07C303/36 , C07C309/09 , C07C313/00 , C07C319/14 , C07C321/26 , C07C323/52 , C07C323/66 , C07C65/14
CPC分类号： C07C323/66 , C07C309/11 , C07C51/09 , C07C69/712 , C07C2101/14 , C07C2101/16 , C07C2101/18
摘要： New compounds of the general formula Ir.sub.1 -- ph -- X -- CR.sub.2 R.sub.4 -- alk -- R.sub.3 (I)wherein R.sub.1 denotes a cycloalkenyl radical or a monocyclic cycloalkyl radical, Ph denotes an optionally substituted phenylene radical, X denotes the oxy or thio group, R.sub.2 denotes hydrogen or alkyl, R.sub.3 denotes an optionally functionally modified carboxyl group, a sulpho group or a sulphamido group, alk denotes an alkylene or alkenylene radical which separates the groups R.sub.1 --Ph--X--CR.sub.2 R.sub.4 and R.sub.3 by at least 2 carbon atoms and R.sub.4 is hydrogen or, if alk separates the groups R.sub.1 --Ph--X--CR.sub.2 R.sub.4 and R.sub.3 by at least 3 carbon atoms or R.sub.1 denotes a cycloalkenyl radical, R.sub.4 can also denote alkyl, in the free form or in the form of salts are useful as antiallergics.

13. 发明授权

US3940434A Dicarboxylic acids and derivatives 失效
标题翻译：二羧酸及其衍生物
公开(公告)号：US3940434A
公开(公告)日：1976-02-24
申请号：US389105
申请日：1973-08-16
申请人： Georges Haas , Erwin F. Jenny , Alberto Rossi
发明人： Georges Haas , Erwin F. Jenny , Alberto Rossi
IPC分类号： C07C69/608 , C07C17/12 , C07C29/147 , C07C45/60 , C07C45/62 , C07C51/00 , C07C57/50 , C07C57/62 , C07C59/00 , C07C62/30 , C07C67/00 , C07C69/73 , C07C69/74 , C07C227/00 , C07C227/02 , C07C227/16 , C07C227/18 , C07C229/50 , C07C231/00 , C07C231/12 , C07C233/07 , C07C233/11 , C07C233/13 , C07C233/15 , C07C233/43 , C07C233/58 , C07C235/34 , C07C235/40 , C07C235/78 , C07C235/82 , C07C237/20 , C07C237/22 , C07C237/24 , C07D213/30 , C07D317/20 , C07C63/595 , C07C69/76
CPC分类号： C07D213/30 , C07C17/12 , C07C201/08 , C07C205/45 , C07C221/00 , C07C225/22 , C07C231/02 , C07C61/39 , C07C69/753 , C07D317/20 , C07C2101/14 , C07C2101/18 , Y10S514/87
摘要： Benzocycloalkenderivatives substituted in 1-position by carboxyl and carboxyalkyl or two carboxyl groups, and further substituted in the benzene ring by cycloalkyl and optionally other substituents, their esters, amides and pharmaceutically acceptable salts have antiinflammatory and analgesic activity and can be used for the treatment of inflammatory conditions and pain in mammals; a representative embodiment is 1-methoxycarbonyl-5-cyclohexyl-6-chloro-1-indanecarboxylic acid.
摘要翻译：通过羧基和羧基烷基或两个羧基在1-位取代的苯并环烷基化物，并且在苯环中被环烷基和任选的其它取代基进一步取代，它们的酯，酰胺和药学上可接受的盐具有抗炎和止痛活性，并且可用于治疗炎症状况和哺乳动物疼痛; 代表性的实施方案是1-甲氧基羰基-5-环己基-6-氯-1-茚满羧酸。

14. 发明授权

US4272547A Benzoyl indane carboxamides as antiphlogistics 失效
标题翻译：苯甲酰基吲哚甲酰胺作为消炎药
公开(公告)号：US4272547A
公开(公告)日：1981-06-09
申请号：US825637
申请日：1977-08-18
申请人： Georges Haas , Alberto Rossi
发明人： Georges Haas , Alberto Rossi
IPC分类号： C07D295/18 , A61K31/165 , A61K31/19 , A61K31/215 , A61K31/34 , A61K31/341 , A61K31/38 , A61K31/381 , A61P25/04 , A61P29/00 , C07C51/00 , C07C59/54 , C07C59/76 , C07C59/90 , C07C61/28 , C07C62/38 , C07C67/00 , C07C69/017 , C07C69/738 , C07C69/757 , C07C231/00 , C07C231/02 , C07C231/06 , C07C231/12 , C07C233/34 , C07C235/40 , C07C235/78 , C07C235/82 , C07D307/54 , C07D333/24 , C07C103/26 , A61K31/22 , C07C69/02
CPC分类号： C07C59/54
摘要： Compounds of the general formula I ##STR1## wherein one of the two radicals R.sub.1 and R.sub.2 denotes the acyl radical of a carboxylic acid of aromatic character and the other denotes hydrogen or optionally esterified or etherified hydroxyl, R.sub.3 denotes hydrogen, alkyl or hydroxyalkyl, R.sub.4 denotes optionally esterified or amidized carboxyl, m denotes 1 or 2 and n denotes 0 or 1, in the free form or in the form of their salts are useful as antiphlogistics, mild analgesics, antipyretics and as anti-rheumatic agents.
摘要翻译：通式I（I）的化合物，其中两个基团R 1和R 2中的一个表示芳族特征的羧酸的酰基，另一个表示氢或任选酯化或醚化的羟基，R 3表示氢，烷基或羟烷基，R 4表示任选酯化或酰胺化的羧基，m表示1或2，n表示0或1，以游离形式或其盐的形式可用作消炎剂，温和止痛剂，解热剂和抗风湿剂。

15. 发明授权

US4192873A Anti-inflammatory 2-sulphonyl- (or -sulphinyl)-2'-aminoacetophenones 失效
标题翻译：抗炎2-磺酰基 - （或 - 亚磺酰基）-2'-氨基苯乙酮
公开(公告)号：US4192873A
公开(公告)日：1980-03-11
申请号：US846305
申请日：1977-10-28
申请人： Pier G. Ferrini , Richard Goschke , Alfred Sallmann , Alberto Rossi
发明人： Pier G. Ferrini , Richard Goschke , Alfred Sallmann , Alberto Rossi
IPC分类号： A61K31/135 , A61K31/18 , A61K31/255 , A61K31/44 , A61P7/02 , A61P29/00 , C07C67/00 , C07C313/00 , C07C315/04 , C07C317/28 , C07D213/70 , C07D213/71 , C07C87/50 , C07C87/60
CPC分类号： A61K31/255
摘要： 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.
摘要翻译：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。

16. 发明授权

US4115416A Process for the manufacture of new carboxylic acids 失效
标题翻译：新型羧酸制备方法
公开(公告)号：US4115416A
公开(公告)日：1978-09-19
申请号：US721737
申请日：1976-09-09
申请人： Alberto Rossi , Christian Egli
发明人： Alberto Rossi , Christian Egli
IPC分类号： C07C59/68 , C07C59/70 , C07C69/712 , C07C69/76 , C11C1/00
CPC分类号： C07C59/70 , C07C59/68 , C07C69/712
摘要： .alpha.-Phenoxyacetic acids, in which the .alpha.-position is substituted by an alkyl residue with 5 to 12 carbon atoms and the phenyl residue is substituted by a cycloaliphatic hydrocarbon residue which is unsaturated in the 1-position and is only singly unsaturated, and their esters and amides are useful as hypolipidaemic agents.

17. 发明授权

US3944589A .alpha.-Cycloalkenylphenyl-fatty acid nitriles 失效
标题翻译： α-环烯基苯基 - 脂肪酸腈
公开(公告)号：US3944589A
公开(公告)日：1976-03-16
申请号：US457521
申请日：1974-04-03
申请人： Alberto Rossi
发明人： Alberto Rossi
IPC分类号： C07C17/16 , C07C29/14 , C07C29/147 , C07C33/38 , C07C33/50 , C07C41/26 , C07C43/192 , C07C43/196 , C07C45/59 , C07C49/798 , C07C51/08 , C07C121/66 , C07C121/75 , C07C121/78
CPC分类号： C07C45/59 , C07C17/16 , C07C29/14 , C07C29/147 , C07C33/38 , C07C33/50 , C07C41/26 , C07C43/192 , C07C43/196 , C07C51/08 , C07C2101/16
摘要： Compounds of the formula ##EQU1## in which X represents a free carboxyl group or in the second place an esterified or amidated carboxyl group; R represents a 1-cycloalkenyl residue; Ph represents an ortho-phenylene residue or especially a para-phenylene residue; and R.sub.1 and R.sub.2 each represents a hydrogen atom or a monovalent or together a divalent aliphatic or araliphatic hydrocarbon residue, e.g. the .alpha.-[p-(1-cyclohexenyl)-phenyl]-propionic acid, are useful as analgetic and antiinflammatoric agents.
摘要翻译：其中X表示游离羧基的式R 1 | R-Ph-C-X | R 2化合物或第二种酯化或酰胺化羧基的化合物; R表示1-环烯基残基; Ph表示邻 - 亚苯基残基或特别是对 - 亚苯基残基; 并且R 1和R 2各自表示氢原子或二价脂族或芳脂族烃残基的一价或一体。 α-对 - （对 - （1-环己烯基） - 苯基] - 丙酸可用作止痛和抗炎剂。

18. 发明授权

US4505913A Substituted anthranilamides and pharmaceutical preparations containing these compounds 失效
标题翻译：取代的邻氨基苯甲酰胺和含有这些化合物的药物制剂
公开(公告)号：US4505913A
公开(公告)日：1985-03-19
申请号：US431456
申请日：1982-09-30
申请人： Pier G. Ferrini , Alberto Rossi , Georges Haas
发明人： Pier G. Ferrini , Alberto Rossi , Georges Haas
IPC分类号： C07D295/18 , A61K31/635 , A61P25/04 , A61P29/00 , A61P37/08 , C07D295/192 , A61K31/495 , C07D241/04 , C07D401/04
CPC分类号： C07D295/192
摘要： Substituted anthranilamides of the formula ##STR1## in which R.sub.1 is hydrogen or an aliphatic, cycloaliphatic or cycloaliphatic-aliphatic hydrocarbon radical, R.sub.2 is hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl, R.sub.3 is hydrogen or an aliphatic or substituted or unsubstituted araliphatic or heteroaryl-aliphatic hydrocarbon radical and alk and alk' are identical or different lower alkylene radicals which separate the nitrogen atoms by 2 or 3 carbon atoms, and salts thereof, possess analgesic, anti-inflammatory and anti-allergic properties and may be used as active ingredients of analgesic, anti-inflammatory and anti-allergic pharmaceuticals. They are prepared, for example, by reacting an acid of the formula ##STR2## or a reactive functional derivative thereof, with an amine of the formula ##STR3## or a reactive derivative or salt thereof.
摘要翻译：取代的式（I）的邻氨基苯甲酰胺其中R1是氢或脂族，脂环族或脂环族脂族烃基，R2是氢，低级烷基，低级烷氧基，卤素或三氟甲基，R3是氢或脂族或取代的或未取代的芳脂族或杂芳基 - 脂族烃基和alk和alk'是将氮原子分开2或3个碳原子的相同或不同的低级亚烷基及其盐具有止痛，抗炎和抗过敏性质，用作镇痛，抗炎和抗过敏药物的有效成分。它们例如通过使式（III）的酸或其反应性官能衍生物与式（IV）的胺或其反应性衍生物或盐反应来制备。

19. 发明授权

US4013719A Adamantyl phenoxy alkylamides 失效
标题翻译： ADAMANTYL PHENOXY ALKYLAMIDES
公开(公告)号：US4013719A
公开(公告)日：1977-03-22
申请号：US605574
申请日：1975-08-18
申请人： Georges Haas , Roland Jaques , Alberto Rossi , Martin Ruegg
发明人： Georges Haas , Roland Jaques , Alberto Rossi , Martin Ruegg
IPC分类号： C07C59/68 , C07C59/70 , C07C303/00 , C07C309/09 , C07C103/26 , A61K31/165 , C07C83/10
CPC分类号： C07C59/68 , C07C309/09 , C07C59/70
摘要： Compounds of the formula Ir.sub.1 -- ph -- X -- alk -- R.sub.2 (I)wherein R.sub.1 is adamantyl, Ph is phenylene which is optionally substituted by, nitro, lower alkyl, lower alkoxy, halogen or trifluoromethyl, X is oxy or thio, alk is alkylene with 1 to 20 C atoms or alkenylene with 2 to 20 C atoms and R.sub.2 is free, esterified or amidised carboxyl, sulpho or sulphonamido and therapeutically acceptable salts thereof are useful as anti-allergic and hypolipidaemic agents.

20. 发明授权

US4004026A Dicarboxylic acids and derivatives in the treatment of pain and inflammation 失效
标题翻译：二羧酸及其衍生物治疗疼痛及炎症
公开(公告)号：US4004026A
公开(公告)日：1977-01-18
申请号：US632926
申请日：1975-11-18
申请人： Georges Haas , Erwin F. Jenny , Alberto Rossi
发明人： Georges Haas , Erwin F. Jenny , Alberto Rossi
IPC分类号： A61K31/19 , A61K31/22
摘要： Benzocycloalkenderivatives substituted in 1-position by carboxyl and carboxyalkyl or two carboxyl groups, and further substituted in the benzene ring by cycloalkyl and optionally other substituents, their esters, amides and pharmaceutically acceptable salts have antiinflammatory and analgesic activity and can be used for the treatment of inflammatory conditions and pain in mammals; a representative embodiment is 1-methoxycarbonyl-5-cyclohexyl-6-chloro-1-indanecarboxylic acid.
摘要翻译：通过羧基和羧基烷基或两个羧基在1-位取代的苯并环烷基化物，并且在苯环中被环烷基和任选的其它取代基进一步取代，它们的酯，酰胺和药学上可接受的盐具有抗炎和止痛活性，并且可用于治疗炎症状况和哺乳动物疼痛; 代表性的实施方案是1-甲氧基羰基-5-环己基-6-氯-1-茚满羧酸。

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