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21. 发明授权

US4801604A Cis-N-(2-aminocycloaliphatic)benzamide anti-convulsants 失效
标题翻译：顺式-N-（2-氨基环脂肪族）苯甲酰胺抗惊厥药
公开(公告)号：US4801604A
公开(公告)日：1989-01-31
申请号：US76411
申请日：1987-07-21
申请人： Philip F. Vonvoigtlander , Jacob Szmuszkovicz
发明人： Philip F. Vonvoigtlander , Jacob Szmuszkovicz
IPC分类号： A61K31/165 , A61K31/40 , C07D295/135 , C07D295/06
CPC分类号： C07D295/135 , A61K31/165 , A61K31/40
摘要： Certain cis-N-(2-amino-cycloalophatic)benzamides of the formula ##STR1## where m is 0, n is 2, r is alkyl, R.sub.1 and R.sub.2 are taken together with the nitrogen denote a pyrrolidine ring, X and Y are hydrogen or a halogen having an atomic number of from 9 to 35, e.g., cis-3,4-dichloro-N-methyl-n[2-(1-pyrrolidinyl)cyclohexyl]benzamide, and salts thereof, have been found to have CNS seizure blocking or preventing drug action, e.g., anti-convulsant drug properties with little or no analgesic properties.
摘要翻译：某些式（I）的顺式-N-（2-氨基 - 环状）苯甲酰胺，其中m为0，n为2，r为烷基，R 1和R 2与氮一起表示吡咯烷环，X 和Y是氢或原子序数为9至35的卤素，例如顺式-3,4-二氯-N-甲基-N [2-（1-吡咯烷基）环己基]苯甲酰胺及其盐已经被发现CNS阻塞或阻止药物作用，例如具有很少或没有止痛特性的抗惊厥药物性质。

22. 发明授权

US4540690A 2-(Phenylmethylene)cycloalkylamines and -azetidines 失效
标题翻译： 2-（苯基亚甲基）环烷基胺和 - 氮杂环丁烷
公开(公告)号：US4540690A
公开(公告)日：1985-09-10
申请号：US408333
申请日：1982-08-16
申请人： Jacob Szmuszkovicz
发明人： Jacob Szmuszkovicz
IPC分类号： C07C45/56 , C07C45/66 , C07C45/72 , C07C45/74 , C07C49/683 , C07D205/04 , C07D307/52 , A61K31/36 , A61K31/395 , C07D405/08
CPC分类号： C07D307/52 , C07C45/56 , C07C45/66 , C07C45/72 , C07C45/74 , C07C49/683 , C07D205/04
摘要： 2-(Phenylmethylene)cycloalkylamines and -azetidines of the formula ##STR1## and acid addition salts thereof, e.g., 1-[2-(phenylmethylene)cyclohexyl]azetidine, and related compounds, which have analgesic, antidepressant and mixed analgesic/antidepressant central nervous system (CNS) activities, and which are useful in treating pain and/or depression in mammals including humans. The invention provides processes for preparing the compounds as well as compositions containing the compounds and methods for using the compounds as analgesic and/or antidepressant drugs for humans and valuable mammalian animals.
摘要翻译：具有式（I）的2-（苯基亚甲基）环烷基胺和 - 氮杂环丁烷及其酸加成盐，例如1- [2-（苯基亚甲基）环己基]氮杂环丁烷和相关化合物，其具有止痛，抗抑郁和混合止痛 /抗抑郁中枢神经系统（CNS）活性，其可用于治疗包括人在内的哺乳动物的疼痛和/或抑郁。本发明提供了制备化合物的方法以及含有这些化合物的组合物和使用该化合物作为人类和有价值哺乳动物的镇痛药和/或抗抑郁药物的方法。

23. 发明授权

US4360531A Substituted cycloalkanes 失效
标题翻译：取代的环烷烃
公开(公告)号：US4360531A
公开(公告)日：1982-11-23
申请号：US252535
申请日：1981-04-09
申请人： Moses W. McMillan , Jacob Szmuszkovicz
发明人： Moses W. McMillan , Jacob Szmuszkovicz
IPC分类号： C07D295/12 , A61K31/16 , A61K31/165 , A61K31/22 , A61K31/335 , A61K31/357 , A61K31/39 , A61P25/04 , C07C67/00 , C07C231/00 , C07C233/41 , C07C233/79 , C07C241/00 , C07C247/18 , C07C251/44 , C07C253/00 , C07C255/60 , C07C313/00 , C07C317/44 , C07C317/46 , C07C317/50 , C07C325/00 , C07C327/44 , C07C327/50 , C07D295/135 , C07D317/72 , C07D327/04 , C07D327/06 , C07D491/10 , C07D493/10 , C07F7/18 , C07D487/00 , A61K31/40
CPC分类号： C07D295/135 , C07D317/72 , C07D327/06 , C07D491/10 , C07D493/10 , C07F7/1804
摘要： [2-Amino(substituted cycloaliphatic)]benzeneacetamide and benzamide compounds, e.g., trans-3,4-dichloro-N-methyl-N-[7-(1-pyrrolidinyl)-1,4-dioxaspiro[4.5]dec-8-yl]benzeneacetamide, have useful analgesic activity and low abuse or physical dependence liability, or are useful as chemical intermediates for producing such analgesic compounds. Processes for their preparation are disclosed. Pharmaceutical compositions and methods of use are also disclosed.
摘要翻译： [2-氨基（取代的脂环族基）]苯乙酰胺和苯甲酰胺化合物，例如反式-3,4-二氯-N-甲基-N- [7-（1-吡咯烷基）-1,4-二氧杂螺[4.5] 8-yl]苯乙酰胺具有有用的止痛活性和低的滥用或物理依赖的责任，或作为生产这种止痛化合物的化学中间体是有用的。公开了其制备方法。还公开了药物组合物和使用方法。

24. 再颁专利

USRE30837E N-(2-Aminocycloheptyl)alkanoylanilides 失效
标题翻译： N-（2-氨基环庚基）烷酰苯胺
公开(公告)号：USRE30837E
公开(公告)日：1981-12-29
申请号：US190181
申请日：1980-09-24
申请人： Jacob Szmuszkovicz
发明人： Jacob Szmuszkovicz
IPC分类号： C07C55/07 , C07C57/145 , C07C57/15 , C07C233/02 , C07C271/06 , C07D295/135
CPC分类号： C07D295/135 , C07C233/02 , C07C271/06 , C07C55/07 , C07C57/145 , C07C57/15
摘要： N-(2-aminocycloheptyl)N-alkanoylanilides and their 2-N-oxides of the formula ##STR1## e.g., trans-3,4-dichloro-N-[2-(allylamino)cycloheptyl]propionanilide, and their pharmacologically acceptable salts, have been found to possess potent Central Nervous System antidepressant properties. Many of them are new.These compounds are promising antidepressant drugs which are characterized by lower toxicity than imipramine, and long acting activity which may allow longer durations between administrations, e.g., once a day. Pharmaceutical compositions containing these compounds and a process for treating conditions of depression with these compositions are disclosed.

25. 发明授权

US4192885A Analgesic N-{2-[N'-(2-furylmethyl and 2-thienyl-methyl)-N'-alkylamino]cycloaliphatic}cyanobenzamides 失效
标题翻译：镇痛N- {2- [N' - （2-呋喃基甲基和2-噻吩基 - 甲基）-N'-烷基氨基]环脂族}氰基苯甲酰胺
公开(公告)号：US4192885A
公开(公告)日：1980-03-11
申请号：US18550
申请日：1979-03-08
申请人： Jacob Szmuszkovicz
发明人： Jacob Szmuszkovicz
IPC分类号： C07D295/135 , A61K31/34 , A61K31/38 , C07D307/54 , C07D333/24
CPC分类号： C07D295/135
摘要： Cis- and trans-N-(2-aminocycloaliphatic)benzamide compounds of the formula ##STR1## e.g., N-methyl-N-[2-(N-pyrrolidinyl)cyclohexyl]-3,4-dichlorobenzamide, and their pharmaceutically acceptable salts, have been found to have potent analgesic activity, and compositions containing these compounds useful in pharmaceutical dosage unit form for alleviating pain in warm blooded animals, as well as methods for alleviating pain in animals with these compositions. Processes for preparing the compounds are also disclosed.
摘要翻译：例如N-甲基-N- [2-（N-吡咯烷基）环己基] -3,4-二氯苯甲酰胺及其药学上可接受的盐的顺式 - 和反式-N-（2-氨基环脂族）苯甲酰胺化合物已经发现具有有效的止痛活性，并且含有这些化合物的组合物可用于药物剂量单位形式以减轻温血动物的疼痛，以及用这些组合物减轻动物疼痛的方法。还公开了制备化合物的方法。

26. 发明授权

US4186208A Anti-depressant N-(3,4-dichlorophenyl)-N-dimethylaminoalkylene amides 失效
标题翻译：抗抑郁剂N-（3,4-二氯苯基）-N-二甲基氨基亚烷基酰胺
公开(公告)号：US4186208A
公开(公告)日：1980-01-29
申请号：US7127
申请日：1979-01-29
申请人： Michael P. Kane , Jacob Szmuszkovicz
发明人： Michael P. Kane , Jacob Szmuszkovicz
IPC分类号： A61K31/165 , C07C103/19 , A61K31/16 , C07C103/44
CPC分类号： A61K31/165 , A61K9/0019 , A61K9/0095 , A61K9/02 , A61K9/2018 , A61K9/4858
摘要： A pharmaceutical formulation containing, as active ingredient, a compound of the Formula III: ##STR1## wherein A is a group selected from --(CH.sub.2).sub.2 --; --(CH.sub.2).sub.3 --; --(CH.sub.2).sub.4 --; --(CH.sub.2).sub.5 --; ##STR2## wherein R is ethyl, vinyl, or cyclopropyl; and wherein X is bromo or chloro, or the pharmacologically acceptable acid addition salts for the treatment of depression in warm-blooded animals, including man.
摘要翻译：一种药物制剂，其含有作为活性成分的式III化合物：其中A是选自 - （CH 2）2 - 的基团; - （CH 2）3 - ; - （CH 2）4 - - （CH 2）5 - 其中R是乙基，乙烯基或环丙基; 和其中X是溴或氯，或用于治疗包括人在内的温血动物的抑郁症的药理学上可接受的酸加成盐。

27. 发明授权

US4128663A Anilide derivatives as antidepressants 失效
标题翻译：苯胺衍生物作为抗抑郁药
公开(公告)号：US4128663A
公开(公告)日：1978-12-05
申请号：US796989
申请日：1977-05-16
申请人： Jacob Szmuszkovicz
发明人： Jacob Szmuszkovicz
IPC分类号： C07C233/02 , C07C233/16 , C07C271/00 , A61K31/165 , A61K31/195 , A61K31/655 , C07C103/10
CPC分类号： C07C233/16 , C07C233/02 , C07C271/00
摘要： Anilide derivative compounds of the formula ##STR1## e.g., trans-N-(2-hydroxycyclopentyl)-3',4'-dichloropropionanilide, have been found to possess potent Central Nervous System (CNS) antidepressant properties.These compounds are promising antidepressant drugs which are characterized by less toxicity than imipramine, and long-acting activity which may allow longer durations between administrations, e.g., once a day. Pharmaceutical compositions containing these compounds and a process for treating conditions of depression with these compositions are also disclosed.
摘要翻译：已经发现式（IMAGE）的苯胺衍生化合物，例如反式-N-（2-羟基环戊基）-3'，4'-二氯丙酰苯胺具有有效的中枢神经系统（CNS）抗抑郁药性质。

28. 发明授权

US4978753A 7-phenylpyrimido[1,2-alpha][1,4]benzodiazepin-3(5H)-ones 失效
标题翻译： 7-苯基嘧啶并[1,2-a] [1,4]苯并二氮杂-3（5H） - 酮
公开(公告)号：US4978753A
公开(公告)日：1990-12-18
申请号：US430751
申请日：1989-11-02
申请人： Jacob Szmuszkovicz
发明人： Jacob Szmuszkovicz
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： A 7-phenylpyrimido[1,2-a][1,4]benzodiazepin-3(5H)-ones of the formula II: ##STR1## wherein R.sub.o is selected from the group consisting of hydrogen, alkyl of 1 to 3 carbon atoms, inclusive, --COOR in which R is alkyl defined as above, ##STR2## in which n is a number of 1 to 4, R.sub.6 and R.sub.7 are hydrogen or alkyl defined as above or together ##STR3## is selected from the group consisting of pyrrolidino, piperidino, morpholino, and 4-methylpiperazino, and --CH.sub.2 OH; wherein R.sub.1 is selected from the group consisting of hydrogen, hydroxy, acetoxy, propionoxy, succinyloxy, and alkyl esters thereof; wherein R.sub.2, R.sub.3, R.sub.4, and R.sub.5 are selected from the group consisting of hydrogen, halogen, nitro, cyano, trifluoromethyl, lower-alkyl, -alkoxy, -alkylthio, -alkylsulfinyl, -alkylsulfonyl, -alkanoylamino and -dialkylamino, are synthesized by condensing a 2-amino-5-phenyl-3H-1,4-benzodiazepine of the formula I ##STR4## with a compound selected from the group consisting of acetylenic compounds of the formulae HC.tbd.C--COOR, ROOC.tbd.C--COOR in which R is alkyl defined above, inclusive, and ##STR5## in which R' is alkyl defined as above or ##STR6## defined as above, to give a compound of formula IIa ##STR7## wherein R.sub.2, R.sub.3, R.sub.4, and R.sub.5 is defined as above, and Ro' is selected from the group consisting of hydrogen, alkyl as defined above, --COOR as defined above, and ##STR8## as defined above. Compounds of formula II wherein R.sub.o is --CH.sub.2 OH are obtained by reducing a compound IIa wherein R.sub.o is --CH.sub.2 OH are obtained by reducing a compound IIa wherein R.sub.o ' is --COOR.The compounds of formula II and their pharmacologically acceptable acid addition salts and N-oxides are useful tranquilizers and sedatives for birds and mammals.
摘要翻译：式II的7-苯基嘧啶并[1,2-a] [1,4]苯并二氮杂-3（5H）酮：其中R a选自氢，1至3个碳的烷基原子，包括其中R是如上定义的烷基的-COOR，其中n是1至4的数，R 6和R 7是氢或如上定义的烷基或一起选自的吡咯烷子基，哌啶子基，吗啉代和4-甲基哌嗪基，和-CH 2 OH; 其中R1选自氢，羟基，乙酰氧基，丙酰氧基，琥珀酰氧基及其烷基酯; 其中R2，R3，R4和R5选自氢，卤素，硝基，氰基，三氟甲基，低级烷基， - 烷氧基， - 烷硫基， - 烷基亚磺酰基， - 烷基磺酰基， - 烷酰基氨基和 - 二烷基氨基通过将式I的2-氨基-5-苯基-3H-1,4-苯并二氮杂与选自由下列化合物组成的组中的化合物缩合：式IIICO-COOR，ROOC 3BOND C- COOR，其中R是上述定义的烷基，包括端点的R 1和如上定义的R'或如上定义的，得到式IIa化合物其中R 2，R 3，R 4，并且R 5如上所定义，并且Ro'选自氢，上述定义的烷基，如上定义的-COOR和如上定义的“IMAGE”。其中Ro为-CH 2 OH的式II化合物通过还原其中Ro为-CH 2 OH的化合物IIa通过还原其中Ro'为-COOR的化合物IIa获得。式II化合物及其药理学上可接受的酸加成盐和N-氧化物是用于鸟类和哺乳动物的镇静剂和镇静剂。

29. 发明授权

US4652559A 2-(Phenylmethylene)cycloalkyl-azetidines 失效
标题翻译： 2-（苯基亚甲基）环烷基 - 氮杂环丁烷
公开(公告)号：US4652559A
公开(公告)日：1987-03-24
申请号：US757819
申请日：1985-07-22
申请人： Jacob Szmuszkovicz
发明人： Jacob Szmuszkovicz
IPC分类号： C07C45/56 , C07C45/66 , C07C45/72 , C07C45/74 , C07D205/04 , C07D307/52 , C07D405/08 , A61K31/395
CPC分类号： C07D307/52 , C07C45/56 , C07C45/66 , C07C45/72 , C07C45/74 , C07D205/04
摘要： 2-(Phenylmethylene)cycloalkylamines and -azetidines of the formula ##STR1## and acid addition salts thereof, e.g., 1-[2-(phenylmethylene)cyclohexyl]azetidine, and related compounds, which have analgesic, antidepressant and mixed analgesic/antidepressant central nervous system (CNS) activities, and which are useful in treating pain and/or depression in mammals including humans. The invention provides processes for preparing the compounds as well as compositions containing the compounds and methods for using the compounds as analgesic and/or antidepressant drugs for humans and valuable mammalian animals.
摘要翻译：具有式（I）的2-（苯基亚甲基）环烷基胺和 - 氮杂环丁烷及其酸加成盐，例如1- [2-（苯基亚甲基）环己基]氮杂环丁烷和相关化合物，其具有止痛，抗抑郁和混合止痛 /抗抑郁中枢神经系统（CNS）活性，其可用于治疗包括人在内的哺乳动物的疼痛和/或抑郁。本发明提供了制备化合物的方法以及含有这些化合物的组合物和使用该化合物作为人类和有价值哺乳动物的镇痛药和/或抗抑郁药物的方法。

30. 发明授权

US4598088A 2-pyrrolyl-cycloalkyl-amide analgesics 失效
标题翻译： 2-吡咯基 - 环烷基 - 酰胺镇痛药
公开(公告)号：US4598088A
公开(公告)日：1986-07-01
申请号：US738637
申请日：1985-05-29
申请人： Jacob Szmuszkovicz , John M. McCall , Lester J. Kaplan , Moses W. McMillan
发明人： Jacob Szmuszkovicz , John M. McCall , Lester J. Kaplan , Moses W. McMillan
IPC分类号： C07D207/20 , C07D405/04 , C07D409/04 , A61K31/40
CPC分类号： C07D405/04 , C07D207/20 , C07D409/04
摘要： N-[2-(2,5-dihydro-1H-pyrrol-1-yl)cycloaliphatic)]benzeneacetamide and -benzamide compounds, e.g., (1.alpha.,2.beta.)-(.+-.)-3,4-dichloro-N-[2-(2,5-dihydro-1H-pyrrol-1-yl)cyclohexyl]-N-methylbenzeneacetamide, and salts thereof, have useful analgesic activity, low abuse or physical dependence liability properties. Processes for their preparation are disclosed. Pharmaceutical compositions containing such compounds and methods for their use are also disclosed.
摘要翻译： N-（2-（2,5-二氢-1H-吡咯-1-基）环脂族基）]苯乙酰胺和苯甲酰胺化合物，例如（1α，2β） - （+/-） - 3,4-二氯 -N- [2-（2,5-二氢-1H-吡咯-1-基）环己基] -N-甲基苯乙酰胺及其盐具有有用的止痛活性，低滥用或物理依赖性责任性质。公开了其制备方法。还公开了含有这些化合物的药物组合物及其使用方法。

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