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1. 发明授权

US4876340A Benzazecine derivatives for cognitive and memory functions 失效
标题翻译：苯并嗪衍生物用于认知和记忆功能
公开(公告)号：US4876340A
公开(公告)日：1989-10-24
申请号：US154760
申请日：1988-02-11
申请人： Werner Aschwanden , Rene Imhof , Roland Jakob , Emilio Kyburz
发明人： Werner Aschwanden , Rene Imhof , Roland Jakob , Emilio Kyburz
IPC分类号： A61K31/395 , A61P25/28 , C07D221/10 , C07D225/06
CPC分类号： C07D221/10 , C07D225/06
摘要： Benzazecinediones of the formula ##STR1## where R.sup.1 and R.sup.2 are independently hydrogen or chlorine, R.sup.3 is hydrogen, fluorine, chlorine, bromine or methoxy, R.sup.4 is hydrogen, chlorine or methoxy and R.sup.5 is hydrogen, acetyl, propionyl, benzoyl, chlorobenzoyl, methoxybenzoyl or phenylacetyl, with the proviso that 2 or 3 of the groups R.sup.1 to R.sup.4 are hydrogen, as well as many of the corresponding benzo[f]quinolines from which these benzazecinediones can be prepared by oxidation are suitable for the control or prevention of cerebral insufficiency or for the improvement of cognitive functions in mammals. They can be produced according to various processes and can be prepared into pharmaceutical compositions.
摘要翻译：苯甲酸甲酯，其中R1和R2独立地是氢或氯，R3是氢，氟，氯，溴或甲氧基，R4是氢，氯或甲氧基，R5是氢，乙酰基，丙酰基，苯甲酰基，氯代苯甲酰基，甲氧基苯甲酰基或苯乙酰基，条件是R 1至R 4基团中的2或3个为氢，以及许多相应的苯并[f]喹啉可以通过氧化制备这些苯并吖嗪酮，适于控制或预防脑部不足或用于改善哺乳动物的认知功能。它们可以根据各种方法制备并且可以制备成药物组合物。

2. 发明授权

US4749791A Benzo[f]quinoline intermediates 失效
标题翻译：苯并[f]喹啉中间体
公开(公告)号：US4749791A
公开(公告)日：1988-06-07
申请号：US121987
申请日：1987-11-18
申请人： Werner Aschwanden , Rene Imhof , Roland Jakob , Emilio Kyburz
发明人： Werner Aschwanden , Rene Imhof , Roland Jakob , Emilio Kyburz
IPC分类号： A61K31/395 , A61P25/28 , C07D221/10 , C07D225/06 , C07D221/06
CPC分类号： C07D221/10 , C07D225/06
摘要： Benzazecinediones of the formula ##STR1## wherein R.sup.1 and R.sup.2 are independently hydrogen or chlorine, R.sup.3 is hydrogen, fluorine, chlorine, bromine or methoxy, R.sup.4 is hydrogen, chlorine or methoxy and R.sup.5 is hydrogen, acetyl, propionyl, benzoyl, chlorobenzoyl, methoxybenzoyl or phenylacetyl, with the proviso that 2 or 3 of the groups R.sup.1 to R.sup.4 are hydrogen,as well as many of the corresponding benzo[f]quinolines from which these benzazecinediones can be prepared by oxidation are suitable for the control or prevention of cerebral insufficiency or for the improvement of cognitive functions in mammals. They can be produced according to various processes and can be prepared into pharmaceutical compositions.
摘要翻译：苯甲酸甲酯，其中R1和R2独立地是氢或氯，R3是氢，氟，氯，溴或甲氧基，R4是氢，氯或甲氧基，R5是氢，乙酰基，丙酰基，苯甲酰基，氯代苯甲酰基，甲氧基苯甲酰基或苯乙酰基，条件是R 1至R 4基团中的2或3个为氢，以及许多相应的苯并[f]喹啉可以通过氧化制备这些苯并吖嗪酮，适于控制或预防脑部不足或用于改善哺乳动物的认知功能。它们可以根据各种方法制备并且可以制备成药物组合物。

3. 发明授权

US4732979A Benzazecine derivatives for cognitive and memory functions 失效
标题翻译：苯并嗪衍生物用于认知和记忆功能
公开(公告)号：US4732979A
公开(公告)日：1988-03-22
申请号：US5712
申请日：1987-01-21
申请人： Werner Aschwanden , Rene Imhof , Roland Jakob , Emilio Kyburz
发明人： Werner Aschwanden , Rene Imhof , Roland Jakob , Emilio Kyburz
IPC分类号： A61K31/395 , A61P25/28 , C07D221/10 , C07D225/06 , C07D227/08 , C07D221/06
CPC分类号： C07D221/10 , C07D225/06
摘要： Benzazecinediones of the formula ##STR1## wherein R.sup.1 and R.sup.2 are independently hydrogen or chlorine, R.sup.3 is hydrogen, fluorine, chlorine, bromine or methoxy, R.sup.4 is hydrogen, chlorine or methoxy and R.sup.5 is hydrogen, acetyl, propionyl, benzoyl, chlorobenzoyl, methoxybenzoyl or phenylacetyl, with the proviso that 2 or 3 of the groups R.sup.1 to R.sup.4 are hydrogen.as well as many of the corresponding benzo[f]quinolines from which these benzazecinediones can be prepared by oxidation are suitable for the control or prevention of cerebral insufficiency or for the improvement of cognitive functions in mammals. They can be produced according to various processes and can be prepared into pharmaceutical compositions.
摘要翻译：苯甲酸甲酯，其中R1和R2独立地是氢或氯，R3是氢，氟，氯，溴或甲氧基，R4是氢，氯或甲氧基，R5是氢，乙酰基，丙酰基，苯甲酰基，氯代苯甲酰基，甲氧基苯甲酰基或苯乙酰基，条件是R 1至R 4基团中的2或3个为氢。以及可以通过氧化制备这些苯并吖嗪酮的许多相应的苯并[f]喹啉适用于控制或预防脑功能不全或改善哺乳动物的认知功能。它们可以根据各种方法制备并且可以制备成药物组合物。

4. 发明授权

US4461906A Pyrrolidine 2-one derivatives 失效
标题翻译：吡咯烷-2-酮衍生物
公开(公告)号：US4461906A
公开(公告)日：1984-07-24
申请号：US172607
申请日：1980-07-28
申请人： Werner Aschwanden , Emilio Kyburz
发明人： Werner Aschwanden , Emilio Kyburz
IPC分类号： C07D207/27 , A61K31/40 , C07D207/26 , C07D207/263 , C07D207/273 , C07F7/10 , C07F7/18 , C07D407/12
CPC分类号： C07D207/27 , C07D207/273 , C07F7/10 , C07F7/1856 , Y10S514/878
摘要： 1-Substituted-2-pyrrolidinones of the formula ##STR1## wherein one of R.sup.1, R.sup.2 and R.sup.3 represents hydroxy and the remaining substituents represent hydrogen,are capable of counteracting cerebral insufficiency produced experimentally in animal tests. They can be used therapeutically in the control or prevention of cerebral insufficiency or in the improvement of intellectual capacity. They can be manufactured from novel intermediates and can be processed to provide medicaments.
摘要翻译： 1-取代的2-吡咯烷酮，其中R 1，R 2和R 3中的一个代表羟基，其余的取代基代表氢，能够抵抗动物实验中实验产生的脑功能不全。它们可用于治疗或预防脑功能不全或提高智力能力。它们可以由新型中间体制成，可以加工成药物。

5. 发明授权

US5034402A Methods and pharmaceutical compositions using pyrrolidine derivatives 失效
标题翻译：使用吡咯烷衍生物的方法和药物组合物
公开(公告)号：US5034402A
公开(公告)日：1991-07-23
申请号：US508675
申请日：1990-04-12
申请人： Werner Aschwanden , Emilio Kyburz
发明人： Werner Aschwanden , Emilio Kyburz
IPC分类号： C07D207/27 , A61K31/40 , A61K31/4015 , A61P25/28 , C07D207/26 , C07D207/273 , C07D403/12 , C07D405/12 , C07D413/12 , C07F7/18
CPC分类号： C07D207/273 , C07F7/1856 , Y10S514/96
摘要： Pyrrolidine derivatives of the formula ##STR1## wherein R.sup.1 is hydrogen or lower alkanoyl, R.sup.2 is hydrogen or lower alkyl and R.sup.3 is hydrogen, lower alkyl or a group of the formula --(CH.sub.2).sub.n --NR.sup.4 R.sup.5, wherein n is a whole number of 2 to 4 and R.sup.4 and R.sup.5 each, independently, are hydrogen or lower alkyl, or R.sup.4 and R.sup.5 taken together with the nitrogen atom are a pyrrolidinyl, piperidinyl, piperazinyl or morpholinyl group which is optionally substituted by one or two lower alkyl groups,enantiomers thereof, and acid addition salts of compounds of formula I and their enantiomers which are basic, are useful in the control or prevention of cerebral insufficiency or in the improvement of intellectual capacity. The compounds of formula I of the invention can be prepared starting from starting materials hereinafter described, and are useful as medicaments, for example, in the form of pharmaceutical preparations.

6. 发明授权

US5017608A Hydrocinnamic acid derivatives 失效
标题翻译：氢化肉桂酸衍生物
公开(公告)号：US5017608A
公开(公告)日：1991-05-21
申请号：US403532
申请日：1989-09-06
申请人： Werner Aschwanden , Rene Imhof , Roland Jakob-Roetne , Emilio Kyburz
发明人： Werner Aschwanden , Rene Imhof , Roland Jakob-Roetne , Emilio Kyburz
IPC分类号： C07D221/10 , A61K31/165 , A61K31/325 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61K31/445 , A61K31/47 , A61K31/473 , A61P25/28 , C07C67/00 , C07C231/00 , C07C231/02 , C07C231/12 , C07C233/47 , C07C235/52 , C07C237/12 , C07C237/20 , C07C237/22 , C07C237/36 , C07C239/00 , C07C275/24 , C07D213/30 , C07D213/75 , C07D213/81 , C07D225/06 , C07D295/13 , C07D295/185
CPC分类号： C07D213/75 , C07D213/81 , C07D295/13 , C07D295/185
摘要： Hydrocinnamic acid derivatives of the formula ##STR1## wherein one or two of the symbols R.sup.1 to R.sup.4 are halogen or methoxy and the others are hydrogen;R.sup.5 is hydrogen or phenyl;R.sup.6 is a residue of the formula ##STR2## R.sup.7 is (C.sub.1 -C.sub.4)-alkyl, (C.sub.2 -C.sub.5)-alkanoylamino-(C.sub.2 -C.sub.5)-alkyl, amino or (C.sub.1 -C.sub.4)-alkoxyphenyl;R.sup.8 and R.sup.9 each, independently, are hydrogen or (C.sub.1 -C.sub.4)-alkyl;R.sup.10 is hydrogen and R.sup.11 is hydroxy or R.sup.10 and R.sup.11 taken together are oxo;R.sup.12 is hydrogen, (C.sub.1 -C.sub.10)-alkyl, pyridylmethyl or carbamoylmethyl;R.sup.13 is hydrogen, (C.sub.1 -C.sub.4)-alkyl and R.sup.14 is hydrogen, (C.sub.1 -C.sub.4)-alkyl, pyridyl, phenyl-(C.sub.1 -C.sub.4)-alkyl, carboxy-(C.sub.1 -C.sub.4)-alkyl, carbamoyl-(C.sub.1 -C.sub.4)-alkyl, (C.sub.1 -C.sub.4)-alkoxycarbonyl-(C.sub.1 -C.sub.4)-alkyl, di-(C.sub.1 -C.sub.4)-alkoxycarbonyl-(C.sub.2 -C.sub.5)-alkyl, piperidino-(C.sub.2 -C.sub.4)-alkyl or halopyridinecarboxamido-(C.sub.2 -C.sub.4)-alkyl or R.sup.13 and R.sup.14 taken together with the nitrogen atom are 4-(C.sub.1 -C.sub.4)-alkyl-piperazin-1-yl,as well as pharmaceutically accpetable salts or basic compounds of formula I with acids or of acidic compounds of formula I with bases are described. The compounds of formula I and their pharmaceutically acceptable salts are suitable for the control or prevention of cerebral insufficiency or for the improvement of cognitive functions.

7. 发明授权

US4513002A Cycloheptene derivatives 失效
标题翻译：环庚烯衍生物
公开(公告)号：US4513002A
公开(公告)日：1985-04-23
申请号：US330733
申请日：1981-12-14
申请人： Werner Aschwanden , Quirico Branca , Emilio Kyburz , Rudolf Pfister
发明人： Werner Aschwanden , Quirico Branca , Emilio Kyburz , Rudolf Pfister
IPC分类号： C07D295/02 , A61K31/00 , A61P37/08 , C07C1/00 , C07C13/547 , C07C17/00 , C07C17/16 , C07C17/26 , C07C22/04 , C07C27/00 , C07C33/34 , C07C35/37 , C07C67/00 , C07C301/00 , C07C303/22 , C07C303/32 , C07C309/63 , C07D207/04 , C07D295/03 , A61K31/40
CPC分类号： C07D295/03 , C07C2103/32
摘要： 1-[2-(4,5,10,11-Tetrahydro-1H-dibenzo[a,d]cyclohepten-5-yl)ethyl]pyrrolidine of the formula ##STR1## and its pharmaceutically acceptable acid addition salts, prepared through various intermediates, are described. The compounds have valuable histamine-H.sub.1 antagonistic properties and are suitable for the control or prevention of allergic reactions, such as, urticaria, hay fever, anaphylaxis and over-sensitivity to medicaments.
摘要翻译：具有式I的1- [2-（4,5,10,11-四氢-1H-二苯并[a，d]环庚烯-5-基）乙基]吡咯并且其药学上可接受的酸加成盐，制备通过各种中间体进行描述。这些化合物具有有价值的组胺H1拮抗性质，适用于控制或预防过敏反应，如荨麻疹，花粉热，过敏反应和过度敏感的药物。

8. 发明授权

US4476308A 1-Pyrrolidine acetamides 失效
标题翻译： 1-吡咯烷乙酰胺
公开(公告)号：US4476308A
公开(公告)日：1984-10-09
申请号：US506147
申请日：1983-06-20
申请人： Werner Aschwanden , Emilio Kyburz
发明人： Werner Aschwanden , Emilio Kyburz
IPC分类号： C07D207/27 , A61K31/40 , A61K31/4015 , A61P25/28 , C07D207/26 , C07D207/273 , C07D403/12 , C07D405/12 , C07D413/12 , C07F7/18 , C07D401/12
CPC分类号： C07D207/273 , C07F7/1856 , Y10S514/96
摘要： Pyrrolidine derivatives of the formula ##STR1## wherein R.sup.1 is hydrogen or lower alkanoyl, R.sup.2 is hydrogen or lower alkyl and R.sup.3 is hydrogen, lower alkyl or a group of the formula --(CH.sub.2).sub.n --NR.sup.4 R.sup.5, wherein n is a whole number of 2 to 4 and R.sup.4 and R.sup.5 each, independently, are hydrogen or lower alkyl, or R.sup.4 and R.sup.5 taken together with the nitrogen atom are a pyrrolidinyl, piperidinyl, piperazinyl or morpholinyl group which is optionally substituted by one or two lower alkyl groups, enantiomers thereof, and acid addition salts of compounds of formula I and their enantiomers which are basic, are useful in the control or prevention of cerebral insufficiency or in the improvement of intellectual capacity. The compounds of formula I of the invention can be prepared starting from starting materials hereinafter described, and are useful as medicaments, for example, in the form of pharmaceutical preparations.
摘要翻译：其中R1是氢或低级烷酰基，R2是氢或低级烷基，R3是氢，低级烷基或式 - （CH2）n-NR4R5基团的吡咯烷衍生物，其中n是整数个 2至4，R 4和R 5各自独立地为氢或低级烷基，或者R 4和R 5与氮原子一起为吡咯烷基，哌啶基，哌嗪基或吗啉基，其任选被一个或两个低级烷基取代，对映异构体和式I化合物的酸加成盐及其对映体是碱性的，可用于控制或预防脑功能不全或提高智力能力。本发明式I化合物可以从下文描述的起始原料制备，并且可用作药物，例如以药物制剂的形式。

9. 发明授权

US4452807A (R,S)-1-(3-Hydroxy-4-methoxybenzoyl)-3-hydroxy-2-pyrrolidinone intermediates therefor and use for treating cerebral insufficiency 失效
标题翻译：（R，S）-1-（3-羟基-4-甲氧基苯甲酰基）-3-羟基-2-吡咯烷酮中间体，用于治疗脑功能不全
公开(公告)号：US4452807A
公开(公告)日：1984-06-05
申请号：US340920
申请日：1982-01-20
申请人： Werner Aschwanden , Emilio Kyburz
发明人： Werner Aschwanden , Emilio Kyburz
IPC分类号： C07D207/26 , A61K31/40 , A61K31/4015 , A61P25/28 , C07D207/273 , C07F7/10 , C07D207/12
CPC分类号： C07D207/273 , C07F7/10 , Y02P20/55
摘要： 1-(3-Hydroxy-4-methoxybenzoyl)-3-hydroxy-2-pyrrolidinone of the formula ##STR1## suitable for the control or prevention of cerebral insufficiency is described. The compound contains an asymmetric carbon atom. Therefore, the two optically active enantiomeric forms as well as the racemate are described. The compound of formula I can be prepared by cleaving the protecting group(s) from a corresponding compound in which at least one of the two hydroxy groups is protected.
摘要翻译：描述了适用于控制或预防脑功能不全的式（I）的1-（3-羟基-4-甲氧基苯甲酰基）-3-羟基-2-吡咯烷酮。该化合物含有不对称碳原子。因此，描述了两种光学活性对映体形式以及外消旋体。式I的化合物可以通过将保护基从保护两个羟基中的至少一个的相应化合物切割来制备。

10. 发明授权

US4239770A Substituted 2-pyrrolidinones for counteracting cerebral insufficiency 失效
标题翻译：用于抵抗脑功能不全的取代的2-吡咯烷酮
公开(公告)号：US4239770A
公开(公告)日：1980-12-16
申请号：US8674
申请日：1979-02-02
申请人： Emilio Kyburz , Werner Aschwanden
发明人： Emilio Kyburz , Werner Aschwanden
IPC分类号： C07D207/267 , A61K31/40 , A61K31/4015 , A61K38/35 , A61P25/28 , C07D207/26 , C07D207/263 , C07D207/27
CPC分类号： C07D207/27 , Y10S514/811 , Y10S514/879
摘要： 1-Substituted 2-pyrrolidinones and pharmaceutical compositions containing same are described. The pharmaceutical compositions are useful in counteracting cerebral insufficiency or improving intellectual capacity.
摘要翻译：描述1-取代的2-吡咯烷酮和含有它们的药物组合物。药物组合物可用于抵抗脑功能不全或提高智力能力。

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