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1. 发明授权

US4188396A New phenylazacycloalkanes 失效
标题翻译：新的苯基氮杂环烷烃
公开(公告)号：US4188396A
公开(公告)日：1980-02-12
申请号：US867644
申请日：1978-01-06
申请人： Georges Haas , Alberto Rossi , Pier G. Ferrini , Oswald Schier
发明人： Georges Haas , Alberto Rossi , Pier G. Ferrini , Oswald Schier
IPC分类号： A61K20060101 , A61K31/445 , A61K31/4465 , A61K31/451 , A61P25/24 , A61P25/26 , A61P43/00 , C07D20060101 , C07D211/08 , C07D211/12 , C07D211/14 , C07D211/16 , C07D211/18 , C07D211/22 , C07D211/30 , C07D211/32 , C07D211/52 , C07D211/62 , C07D211/70 , C07D211/74 , C07D211/76 , C07D211/78 , C07F3/02
CPC分类号： C07C255/00 , C07D211/12 , C07D211/14 , C07D211/16 , C07D211/18 , C07D211/22 , C07D211/32 , C07D211/52 , C07D211/70 , C07D211/74 , C07D211/78 , C07F3/02
摘要： New 4-(phenyl)-piperidine compounds of the general formula I ##STR1## in which R.sub.1 represents hydrogen or lower alkyl, Ph represents a p-phenylene group optionally substituted by lower alkyl, lower alkoxy, nitro and/or halogen, and R.sub.2 represents lower alkyl, and pharmaceutically acceptable acid addition salts thereof are useful as antidepressant agents.
摘要翻译：新的式（I）的4-（苯基） - 哌啶化合物，其中R 1表示氢或低级烷基，Ph表示任选被低级烷基，低级烷氧基，硝基和/或卤素取代的对亚苯基，R2表示低级烷基，其药学上可接受的酸加成盐可用作抗抑郁剂。

2. 发明授权

US4327091A N,N-Di and N,N,N-tri(hydroxy-lower alkyl) ammonium salts of substituted 3,4-dihydro-2H-1,2-benzothiazine 1,1 dioxide and pharmaceutical compositions thereof 失效
标题翻译：取代的3,4-二氢-2H-1,2-苯并噻嗪一氧化碳的N，N-Di和N，N，N-三（羟基 - 低级烷基）铵盐及其药物组合物
公开(公告)号：US4327091A
公开(公告)日：1982-04-27
申请号：US116200
申请日：1980-01-28
申请人： Alex Sele , Pier G. Ferrini , Georges Haas , Knut A. Jaeggi , Alberto Rossi
发明人： Alex Sele , Pier G. Ferrini , Georges Haas , Knut A. Jaeggi , Alberto Rossi
IPC分类号： A61K31/54 , A61P29/00 , C07D417/12
CPC分类号： C07D417/12
摘要： 3,4-Dihydro-2H-1,2-benzothiazine 1,1-dioxides of the formula ##STR1## wherein Ph represents a substituted or unsubstituted 1,2-phenylene radical, R represents a substituted or unsubstituted benzopyrone radical, and R.sub.1 represents hydrogen or a substituted or unsubstituted hydrocarbon radical of aliphatic character, and their salts, possess antiinflammatory properties and are useful as medicaments.
摘要翻译：式（Ⅰ）的3,4-二氢-2H-1,2-苯并噻嗪1,1-二氧化物，其中Ph表示取代或未取代的1,2-亚苯基，R表示取代或未取代的苯并吡喃酮基， R 1表示氢或取代或未取代的脂肪族烃基，它们的盐具有抗炎性质，可用作药物。

3. 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。

4. 发明授权

US4213980A Azathianaphthalenes 失效
标题翻译：氮杂萘
公开(公告)号：US4213980A
公开(公告)日：1980-07-22
申请号：US4113
申请日：1979-01-17
申请人： Alex Sele , Pier G. Ferrini , Georges Haas , Knut A. Jaeggi , Alberto Rossi
发明人： Alex Sele , Pier G. Ferrini , Georges Haas , Knut A. Jaeggi , Alberto Rossi
IPC分类号： A61K31/54 , A61P29/00 , C07D417/12 , C07D279/02
CPC分类号： C07D417/12
摘要： 3,4-Dihydro-2H-1,2-benzothiazine 1,1-dioxides of the formula ##STR1## wherein Ph represents a substituted or unsubstituted 1,2-phenylene radical, R represents a substituted or unsubstituted benzopyrone radical, and R.sub.1 represents hydrogen or a substituted or unsubstituted hydrocarbon radical of aliphatic character, and their salts, possess antiinflammatory properties and are useful as medicaments.
摘要翻译：式（Ⅰ）的3,4-二氢-2H-1,2-苯并噻嗪1,1-二氧化物，其中Ph表示取代或未取代的1,2-亚苯基，R表示取代或未取代的苯并吡喃酮基， R 1表示氢或取代或未取代的脂肪族烃基，它们的盐具有抗炎性质，可用作药物。

5. 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。

6. 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。

7. 发明授权

US3933835A New aliphatically substituted aryl-chalcogeno-hydrocarbon derivatives 失效
标题翻译：新的脂肪族取代芳基 - 硫属烃衍生物
公开(公告)号：US3933835A
公开(公告)日：1976-01-20
申请号：US409192
申请日：1973-10-24
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： C07C69/708 , C07C59/72 , C07C67/00 , C07C69/66 , C07C231/00 , C07C231/02 , C07C231/12 , C07C235/06 , C07C253/00 , C07C255/13 , C07C301/00 , C07C303/02 , C07C303/22 , C07C303/36 , C07C303/40 , C07C309/11 , C07C311/00 , C07C313/00 , C07C317/18 , C07C319/14 , C07C323/52 , C07D213/55
CPC分类号： C07C59/72
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 amino, 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, esterfied or amidised carboxyl, sulpho or sulphonamido and therapeutically acceptable salts thereof are useful as anti-allergic and hypolipidaemic agents.
摘要翻译：硝基，低级烷基，低级烷氧基，卤素或三氟甲基，X是氧基或硫基，其中R 1是金刚烷基，Ph是任选被氨基，硝基，低级烷基，低级烷氧基，卤素或三氟甲基取代的亚苯基，烷基是具有1至20个碳原子的亚烷基或具有2至20个碳原子的亚烯基，R2是游离的，酯化的或酰胺化的羧基，磺基或磺酰胺基，其治疗上可接受的盐可用作抗过敏和降血脂药。

8. 发明授权

US4297358A Novel 4,7-phenanthroline derivatives and pharmaceutical compositions containing them and their use 失效
标题翻译：新颖的4,7-菲咯啉衍生物和含有它们的药物组合物及其用途
公开(公告)号：US4297358A
公开(公告)日：1981-10-27
申请号：US109715
申请日：1980-01-04
申请人： Georges Haas , Knut A. Jaeggi , Alberto Rossi , Alex Sele
发明人： Georges Haas , Knut A. Jaeggi , Alberto Rossi , Alex Sele
IPC分类号： A61K31/47 , A61P37/08 , C07D215/26 , C07D215/38 , C07D471/04 , C07D487/04 , A61K31/435
CPC分类号： C07D215/38 , C07D215/26 , C07D471/04
摘要： New 4,7-phenanthroline derivatives of the formula (I) ##STR1## in which Ch represents an optionally substituted 5,6-quinolinylene radical of which the 6-position is joined to the --N(R.sub.E)-- group, andR represents an optionally esterified or amidated carboxy group,and in which eitherR.sub.A and R.sub.B together represent oxo,R.sub.C and R.sub.D together represent an additional link, andR.sub.E represents a radical R.sub.1 which is hydrogen, or an aliphatic, cycloaliphatic, araliphatic or heterocyclic-aliphatic radical, orR.sub.A represents an optionally etherified hydroxy group andR.sub.B together with R.sub.C and R.sub.D together with R.sub.E in each case represents an additional link,and salts of salt-forming compounds of the formula (I), compounds of the formula (I) or the salts thereof have anti-allergic properties. They can be prepared in accordance with processes known per se and may be used as active substances in pharmaceutical preparations.
摘要翻译：式（I）的新的4,7-菲咯啉衍生物其中Ch表示6位与-N（RE） - 基团连接的任意取代的5,6-喹啉基，并且R表示任选酯化或酰胺化的羧基，并且其中RA和RB一起表示氧代，RC和RD一起表示另外的连接，并且RE表示基团R 1，其为氢或脂族，脂环族，芳脂族或杂环脂族基团，或RA表示任选醚化的羟基，RB与RC和RD一起连同RE一起代表另外的连接，式（I）的成盐化合物的盐，式（I）的化合物）或其盐具有抗过敏性质。它们可以根据本身已知的方法制备，并且可以用作药物制剂中的活性物质。

9. 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.

10. 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。

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