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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

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.

3. 发明授权

US5011849A Compounds for treating and preventing cognitive diseases and depression and methods of making same 失效
标题翻译：用于治疗和预防认知疾病和抑郁症的化合物及其制备方法
公开(公告)号：US5011849A
公开(公告)日：1991-04-30
申请号：US383777
申请日：1989-07-21
申请人： Walter Gassner , Rene Imhof , Emilio Kyburz
发明人： Walter Gassner , Rene Imhof , Emilio Kyburz
IPC分类号： A61K31/42 , A61K31/421 , A61K31/425 , A61K31/426 , A61P25/02 , A61P25/24 , A61P25/26 , C07D231/14 , C07D261/18 , C07D263/34 , C07D263/48 , C07D277/20 , C07D277/56 , C07D413/04 , C07D417/04
CPC分类号： C07D413/04 , C07D231/14 , C07D261/18 , C07D263/34 , C07D277/56 , C07D417/04
摘要： Ethylenediamine monoamides of the formulaR--CO--NH--CH.sub.2 --CH.sub.2 --NH.sub.2 Iwherein R is one of groups ##STR1## in which R.sup.1 is phenyl monohalophenyl, monolower-alkylphenyl, monolower-alkoxypheynl, monotrifluoromethylphenyl, monocyanophenyl or monoaryl-lower-alkoxyphenyl, dihalophenyl, furyl, thienyl or monohalothienyl, R.sup.2 is hydrogen, halogen or amino, R.sup.3, R.sup.5 and R.sup.7 each are phenyl, monohalophenyl, dihalophenyl, thienyl, furyl or monohalofuryl, R.sup.4 and R.sup.6 each are hydrogen or amino and R.sup.8 is hydrogen or lower-alkyl, as well as their pharmaceutically usable acid addition salts are disclosed. The compounds have monoamine oxidase inhibiting properties with low toxicity and are useful for the treatment of depressive states and cognitive disorders.
摘要翻译：式R-CO-NH-CH 2 -CH 2 -NH 2 I的乙二胺单酰胺，其中R是基团之一，其中R 1是苯基单卤代苯基，单低级烷基苯基，单低级烷氧基炔，单三氟甲基苯基，单氰基苯基或单芳基 - 低级烷氧基苯基，二卤代苯基，呋喃基，噻吩基或单卤噻吩基，R2是氢，卤素或氨基，R3，R5和R7各自为苯基，单卤代苯基，二卤代苯基，噻吩基，呋喃基或单卤代呋喃基，R4和R6各自为氢或氨基，R8为氢或低级烷基，以及它们的药学上可用的酸加成盐。该化合物具有低毒性的单胺氧化酶抑制性质，可用于治疗抑郁状态和认知障碍。

4. 发明授权

US4684731A Phenyl-quinolizidines 失效
标题翻译：苯基喹喔啉
公开(公告)号：US4684731A
公开(公告)日：1987-08-04
申请号：US474233
申请日：1983-03-11
申请人： Rene Imhof , Emilio Kyburz
发明人： Rene Imhof , Emilio Kyburz
IPC分类号： C07D211/76 , C07D455/02
CPC分类号： C07D211/76 , C07D455/02
摘要： Phenyl-quinolizidines of the general formula ##STR1## wherein X is hydrogen, fluorine, chlorine, lower-alkoxy, lower-alkyl or trifluoromethyl; Y is hydrogen, fluorine, chlorine, lower-alkoxy or lower-alkyl; and R.sup.1 acyl, acylamino or a group A of the formula ##STR2## wherein R.sup.2 is oxygen or sulfur; R.sup.3 is hydrogen or lower-alkyl; and one of R.sup.4 and R.sup.5 is hydrogen and the other is bromine, iodine, cyano, lower-alkoxycarbonyl or sulfamoyl,as racemates or enatiomers, as well as acid addition salts thereof, utilizing various intermediates, are described. The foregoing compounds are useful as neuroleptic, antiemetic and analgesic agents.
摘要翻译：苯基 - 喹啉子，其通式为其中X为氢，氟，氯，低级烷氧基，低级烷基或三氟甲基; Y是氢，氟，氯，低级烷氧基或低级烷基; 和R 1酰基，酰基氨基或式“IMAGE”的基团A，其中R 2是氧或硫; R3是氢或低级烷基; 描述了R 4和R 5中的一个是氢，另一个是溴，碘，氰基，低级烷氧基羰基或氨磺酰基，作为外消旋体或对映异构体，以及其酸加成盐，利用各种中间体。上述化合物可用作神经安定药，止吐剂和止痛剂。

5. 发明授权

US4236010A Phenyl-quinolizidines 失效
标题翻译：苯基喹喔啉
公开(公告)号：US4236010A
公开(公告)日：1980-11-25
申请号：US85096
申请日：1979-10-15
申请人： Rene Imhof , Emilio Kyburz
发明人： Rene Imhof , Emilio Kyburz
IPC分类号： A61K20060101 , A61K31/435 , C07D20060101 , C07D211/76 , C07D221/00 , C07D235/00 , C07D455/02 , C07D471/04
CPC分类号： C07D211/76 , C07D455/02 , Y10S514/872
摘要： Phenyl-quinolizidines of the formula ##STR1## wherein X, Y, R.sup.1 and R.sup.2 are as hereinafter set forth, are described. The compounds of formula I are useful as antipsychotics, antiemetics and analgesics.
摘要翻译：描述了其中X，Y，R 1和R 2如下文所述的式“IMAGE”I的苯基 - 喹嗪子。式I化合物可用作抗精神病药，止吐药和镇痛药。

6. 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。

7. 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。

8. 发明授权

US4329467A Phenyl-quinolizidines 失效
标题翻译：苯基喹喔啉
公开(公告)号：US4329467A
公开(公告)日：1982-05-11
申请号：US217887
申请日：1980-12-18
申请人： Rene Imhof , Emilio Kyburz
发明人： Rene Imhof , Emilio Kyburz
IPC分类号： A61K20060101 , A61K31/435 , C07D20060101 , C07D211/76 , C07D221/00 , C07D235/00 , C07D455/02 , C07D471/04
CPC分类号： C07D211/76 , C07D455/02 , Y10S514/872
摘要： Phenyl-quinolizidines of the formula ##STR1## wherein X, Y, R.sup.1 and R.sup.2 are as hereinafter set forth, are described. The compounds of formula I are useful as antipsychotics, antiemetics and analgesics.
摘要翻译：描述了其中X，Y，R 1和R 2如下文所述的式“IMAGE”I的苯基 - 喹嗪子。式I化合物可用作抗精神病药，止吐药和镇痛药。

9. 发明授权

US4272627A Phenyl-quinolizinones 失效
标题翻译：苯基喹诺酮类
公开(公告)号：US4272627A
公开(公告)日：1981-06-09
申请号：US148646
申请日：1980-05-12
申请人： Rene Imhof , Emilio Kyburz
发明人： Rene Imhof , Emilio Kyburz
IPC分类号： A61K20060101 , A61K31/435 , C07D20060101 , C07D211/76 , C07D221/00 , C07D235/00 , C07D455/02 , C07D471/04
CPC分类号： C07D211/76 , C07D455/02 , Y10S514/872
摘要： Phenyl-quinolizidines of the formula ##STR1## wherein X,Y,R.sup.1 and R.sup.2 are as hereinafter set forth, are described. The compounds of formula I are useful as antipsychotics, antiemetics and analgesics.
摘要翻译：描述了其中X，Y，R 1和R 2如下文所述的式“IMAGE”I的苯基 - 喹嗪子。式I化合物可用作抗精神病药，止吐药和镇痛药。

10. 发明授权

US4957911A 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：US4957911A
公开(公告)日：1990-09-18
申请号：US395380
申请日：1989-08-17
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## 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.

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