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1. 发明授权

US5498726A Preparation of physostigmine carbamate derivatives from physostigmine 失效
标题翻译：从毒扁豆碱制备毒扁豆碱氨基甲酸酯衍生物
公开(公告)号：US5498726A
公开(公告)日：1996-03-12
申请号：US216238
申请日：1994-03-22
申请人： George E. Lee , Thomas B. K. Lee , Donna M. Borek
发明人： George E. Lee , Thomas B. K. Lee , Donna M. Borek
IPC分类号： A61K31/40 , A61P25/04 , A61P25/28 , C07D20060101 , C07D487/04 , C07D487/00
CPC分类号： C07D487/04
摘要： This application relates to a new process for the preparation of a product of the formula ##STR1## wherein R, R.sup.1, R.sup.2, X and m are as defined within, which process comprises preparing treating a compound such as physostigmine to form eseroline which is then treated with an appropriate compound or its equivalent. Acetic acid is added to the reaction mixture after the formation of eseroline.
摘要翻译：本申请涉及制备式（I）的产物的新方法，其中R，R 1，R 2，X和m如上所定义，该方法包括制备治疗化合物如毒扁豆素以形成eseroline 然后用合适的化合物或其等同物处理。在形成eseroline后，将乙酸加入到反应混合物中。

2. 发明授权

US5053513A Method of reducing a carbonyl containing acridine 失效
标题翻译：减少含有亚油酸的方法
公开(公告)号：US5053513A
公开(公告)日：1991-10-01
申请号：US500967
申请日：1990-03-29
申请人： Thomas B. K. Lee , George E. Lee , George S. K. Wong , Donna M. Borek , Keith E. Goehring
发明人： Thomas B. K. Lee , George E. Lee , George S. K. Wong , Donna M. Borek , Keith E. Goehring
IPC分类号： B01J23/40 , C07B61/00 , C07D219/08 , C07D219/10 , C07D221/16
CPC分类号： C07D219/10
摘要： A method of reducing a carbonyl containing acridine of the formula ##STR1## where n is 1, 2 or 3; X is hydrogen, loweralkyl, loweralkoxy, halogen, hydroxy, trifluoromethyl, or NR.sub.3 R.sub.4 where R.sub.3 and R.sub.4 are independently hydrogen or loweralkyl; R is hydrogen or loweralkyl and R.sub.1 is hydrogen, loweralkyl, diloweralkylaminoloweralkyl, arylloweralkyl, diarylloweralkyl, furylloweralkyl, thienylloweralkyl, oxygen-bridged arylloweralkyl, oxygen-bridged diarylloweralkyl, oxygen-bridged furylloweralkyl or oxygen-bridged thienylloweralkyl, is disclosed.

3. 发明授权

US5489681A Method for the preparation of 4-phenyl-1,3-benzodiazepins 失效
标题翻译： 4-苯基-1,3-苯并二氮杂及其前体
公开(公告)号：US5489681A
公开(公告)日：1996-02-06
申请号：US304662
申请日：1994-09-09
申请人： Thomas B. K. Lee , George E. Lee
发明人： Thomas B. K. Lee , George E. Lee
IPC分类号： C07D243/04 , A61K31/55
CPC分类号： C07D243/04
摘要： A compound of the formula ##STR1## is prepared by reacting an N-acylated-o-toluidine of the formula ##STR2## with n-alkyllithium to form a dilithio intermediate of the formula ##STR3## which can then be quenched with N-benzylidenemethylamine to fore compound II. Hydrolysis of compound(II) yields the free base ##STR4## or its salt, which can be cyclized to form 4,5-dihydro-2,3-dimethyl-4-phenyl-3H-1,3-benzodiazepine or its physiologically acceptable salts, which are useful as pharmacological agents.
摘要翻译：通过使式（III）的N-酰化的邻甲苯胺与正烷基锂反应以形成式（IV）的二元中间体制备式（II）化合物：然后将其用N-亚苄基甲基胺淬灭至前体化合物II。化合物（II）的水解产生游离碱（V）或其盐，其可以环化形成4,5-二氢-2,3-二甲基-4-苯基-3H-1,3-苯并二氮杂或其生理上可接受的盐，其可用作药理学试剂。

4. 发明授权

US5349086A Method for the preparation of 4-phenyl-1,3-benzodiazepins and precursors thereof 失效
标题翻译： 4-苯基-1,3-苯并二氮杂的制备方法及其前体
公开(公告)号：US5349086A
公开(公告)日：1994-09-20
申请号：US980449
申请日：1992-11-23
申请人： Thomas B. K. Lee , George E. Lee
发明人： Thomas B. K. Lee , George E. Lee
IPC分类号： C07D243/04 , C07C231/08
CPC分类号： C07D243/04
摘要： A compound of the formula ##STR1## is prepared by reacting an N-acylated-o-toluidine of the formula ##STR2## with n-alkyllithium to form a dilithio intermediate of the formula ##STR3## which can then be quenched with N-benzylidenemethylamine to form compound II. Hydrolysis of compound(II) yields the free base ##STR4## or its salt, which can be cyclized to form 4,5-dihydro-2,3-dimethyl-4-phenyl-3H-1,3-benzodiazepine or its physiologically acceptable salts, which are useful as pharmacological agents.
摘要翻译：通过使式（III）的N-酰化的邻甲苯胺与正烷基锂反应以形成式（IV）的二元中间体制备式（II）化合物：然后用N-亚苄基甲基胺淬灭以形成化合物II。化合物（II）的水解产生游离碱（V）或其盐，其可以环化形成4,5-二氢-2,3-二甲基-4-苯基-3H-1,3-苯并二氮杂或其生理上可接受的盐，其可用作药理学试剂。

5. 发明授权

US4496732A Stereoselective reduction of 2- or 3-substituted 4-piperidones with sodium borohydride 失效
标题翻译：用硼氢化钠对2-或3-取代的4-哌啶酮进行立体选择性还原
公开(公告)号：US4496732A
公开(公告)日：1985-01-29
申请号：US474856
申请日：1983-03-14
申请人： George E. Lee , Thomas B. K. Lee
发明人： George E. Lee , Thomas B. K. Lee
IPC分类号： C07D211/44 , C07D211/46
CPC分类号： C07D211/46 , C07D211/44
摘要： A stereoselective reduction of 2- or 3-substituted 4-piperidones of the formula ##STR1## where R.sub.1 is hydrogen, loweralkyl or benzyl and R.sub.2 is methyl or ethyl, to the di-equatorial isomer of the corresponding 4-piperidinol is described. Said reduction is conducted by use of sodium borohydride in a protic solvent medium at a temperature substantially lower than ambient temperature in the presence of an effective amount of an inorganic acid. Under favorable reaction conditions, the stereoselectivity of the reduction is so high that simple crystallization of the reaction product affords the pure isomer in a commercially acceptable and advantageous process.
摘要翻译：描述了相应的4-哌啶醇的二 - 赤藓醇异构体的2-或3-取代的4-取代的4-取代的4-取代的哌嗪酮，其中R1是氢，低级烷基或苄基，R2是甲基或乙基。所述还原通过在有效量的无机酸存在下，在质子溶剂介质中使用硼氢化钠在基本上低于环境温度的温度下进行。在有利的反应条件下，还原的立体选择性非常高，使得在商业上可接受和有利的方法中，反应产物的简单结晶提供纯异构体。

6. 发明授权

US4374067A Intermediates for the preparation of 4-phenyl-1,3-benzodiazepins and methods for preparing the intermediates 失效
标题翻译：用于制备4-苯基-1,3-苯并二氮杂的中间体及其制备方法
公开(公告)号：US4374067A
公开(公告)日：1983-02-15
申请号：US333965
申请日：1981-12-23
申请人： Thomas B. K. Lee , George E. Lee
发明人： Thomas B. K. Lee , George E. Lee
IPC分类号： C07C67/00 , C07C209/00 , C07C209/62 , C07C211/49 , C07C231/00 , C07C231/10 , C07C231/12 , C07C233/07 , C07C233/25 , C07C233/43 , C07C239/08 , C07C271/28 , C07C301/00 , C07C303/28 , C07C309/63 , C07D243/04 , C07C143/68 , C07C103/127 , C07C125/06
CPC分类号： C07D243/04 , C07C233/07
摘要： The invention relates to compounds of the formula ##STR1## where Y is --OH; halogen; ##STR2## R.sub.1 SO.sub.3 --, where R.sub.1 is a straight chain or branched chain alkyl group having 1 to 5 carbon atoms, or aryl; and R.sub.2 is --C(CH.sub.3).sub.3 or --O--C(CH.sub.3).sub.3. Processes for preparing the compounds are provided. The compounds are useful as intermediates in the preparation of 4-phenyl-1,3-benzodiazepins, which exhibit activity as antidepressants, analgetics and anticonvulsants.
摘要翻译：本发明涉及式（I）的化合物，其中Y是-OH; 卤素; R1S3-，其中R1是具有1-5个碳原子的直链或支链烷基或芳基; 并且R 2是-C（CH 3）3或-O-C（CH 3）3。提供了制备化合物的方法。该化合物可用作制备4-苯基-1,3-苯并二氮杂的中间体，其表现出抗抑郁药，止痛药和抗惊厥药的作用。

7. 发明授权

US4709093A Method for the preparation of 4-phenyl-1,3-benzodiazepines and precursors thereof 失效
标题翻译： 4-苯基-1,3-苯并二氮杂的制备方法及其前体
公开(公告)号：US4709093A
公开(公告)日：1987-11-24
申请号：US757765
申请日：1985-07-23
申请人： Thomas B. K. Lee , George E. Lee
发明人： Thomas B. K. Lee , George E. Lee
IPC分类号： C07D243/04 , C07C103/44
CPC分类号： C07D243/04
摘要： A compound of the formula ##STR1## is prepared by reacting an N-acylated-o-toluidine of the formula ##STR2## with n-alkyllithium to form a dilithio intermediate of the formula ##STR3## which can then be quenched with N-benzylidenemethylamine to form compound II. Hydrolysis of compound(II)yields the free base ##STR4## or its salt, which can be cyclized to form 4,5-dihydro-2,3-dimethyl-4-phenyl-3H-1,3-benzodiazepine or its physiologically acceptable salts, which are useful as pharmacological agents.
摘要翻译：通过使式（III）的N-酰化的邻甲苯胺与正烷基锂反应以形成式（IV）的二元中间体制备式（II）化合物：然后用N-亚苄基甲基胺淬灭以形成化合物II。化合物（II）的水解产生游离碱（V）或其盐，其可以环化形成4,5-二氢-2,3-二甲基-4-苯基-3H-1,3-苯并二氮杂或其生理上可接受的盐，其可用作药理学试剂。

8. 发明授权

US4461728A Preparation of 4-phenyl-1,3-benzodiazepins 失效
标题翻译：制备4-苯基-1,3-苯并二氮杂
公开(公告)号：US4461728A
公开(公告)日：1984-07-24
申请号：US441128
申请日：1982-11-12
申请人： Thomas B. K. Lee , George E. Lee
发明人： Thomas B. K. Lee , George E. Lee
IPC分类号： C07C233/07 , C07D243/04 , C07C103/375
CPC分类号： C07C233/07 , C07D243/04
摘要： The invention relates to compounds of the formula ##STR1## where Y is --OH; halogen; ##STR2## where R.sub.1 is a straight chain or branched chain alkyl group having 1 to 5 carbon atoms, or aryl; and R.sub.2 is --C(CH.sub.3).sub.3 or --O--C(CH.sub.3).sub.3. Processes for preparing the compounds are provided. The compounds are useful as intermediates in the preparation of 4-phenyl-1,3-benzodiazepins, which exhibit activity as antidepressants, analgetics and anticonvulsants.
摘要翻译：本发明涉及式（I）的化合物，其中Y是-OH; 卤素; 其中R 1是具有1至5个碳原子的直链或支链烷基或芳基; 并且R 2是-C（CH 3）3或-O-C（CH 3）3。提供了制备化合物的方法。该化合物可用作制备4-苯基-1,3-苯并二氮杂的中间体，其表现出抗抑郁药，止痛药和抗惊厥药的作用。

9. 发明授权

US4417063A Process for preparation of 6,11-dihydro-11-oxodibenz[b,e]oxepinacetic acids 失效
标题翻译：制备6,11-二氢-11-氧代二苯并[b，e]氧杂乙酸的方法
公开(公告)号：US4417063A
公开(公告)日：1983-11-22
申请号：US264482
申请日：1981-05-18
申请人： Thomas B. K. Lee , George E. Lee , Gregory M. Jobin
发明人： Thomas B. K. Lee , George E. Lee , Gregory M. Jobin
IPC分类号： C07C59/68 , C07D313/12
CPC分类号： C07C59/68 , C07D313/12
摘要： A method for the preparation of 6,11-dihydro-11-oxodibenz[b,e]oxepin-acetic acids having pharmaceutical activity is disclosed. Compounds represented by the formula: ##STR1## wherein R is OH or Cl are provided as intermediates. An aldehyde of the formula: ##STR2## wherein R.sub.1 is a lower alkyl, e.g., 1 to 4 carbon atoms, is reacted with chloroform and aqueous base to form an .alpha.-hydroxy dicarboxylic acid. Alternatively, the aldehyde can be converted to the corresponding cyanohydrin, which is then converted to the corresponding .alpha.-hydroxy dicarboxylic acid. The .alpha.-hydroxy dicarboxylic acid can also be prepared from reaction of a halogenated toluate of the formula: ##STR3## wherein X is Cl or Br with mandelic acid or a derivative thereof of the formula: ##STR4## wherein R.sub.3 and R.sub.4 are independently selected from hydrogen and alkyl of 1 to 4 carbon atoms. The .alpha.-hydroxy dicarboxylic acid is cyclized and then converted to the oxepin acetic acid by reduction. Alternatively, the .alpha.-hydroxy dicarboxylic acid is cyclized and converted to an .alpha.-chloro-substituted oxepin acetic acid, which is then converted to the unsubstituted oxepin acetic acid by reductive removal of chlorine.
摘要翻译：公开了制备具有药物活性的6,11-二氢-11-氧代二苯并[b，e]氧杂七环素 - 乙酸的方法。由下式表示的化合物：其中R是OH或Cl，作为中间体。其中R 1是低级烷基，例如1至4个碳原子的下式的醛与氯仿和碱水溶液反应形成α-羟基二羧酸。或者，醛可以转化成相应的氰醇，然后将其转化为相应的α-羟基二羧酸。 α-羟基二羧酸也可以通过下式的卤代甲酸甲酯：其中X是Cl或Br与下式的扁桃酸或其衍生物反应来制备：其中R 3和R 4独立地选自从氢和1至4个碳原子的烷基。将α-羟基二羧酸环化，然后通过还原转化成氧杂环丁烷乙酸。或者，将α-羟基二羧酸环化并转化成α-氯取代的氧杂环丁酸乙酸，然后通过还原性除去氯而将其转化为未取代的氧杂环庚烯乙酸。

10. 发明授权

US07091199B1 Thienoisoxazole phenoxy unsubstituted ethyl and propyl derivatives useful as d4 antagonists 失效
标题翻译：可用作d4拮抗剂的噻吩异恶唑苯氧基未取代的乙基和丙基衍生物
公开(公告)号：US07091199B1
公开(公告)日：2006-08-15
申请号：US10088369
申请日：2000-09-13
申请人： George E. Lee , John G. Jurcak , Timothy A. Ayers
发明人： George E. Lee , John G. Jurcak , Timothy A. Ayers
IPC分类号： A61K31/55 , C07D403/00 , C07D413/04 , C07D401/41 , C07D261/20
CPC分类号： C07D498/04
摘要： The compounds are of the class of thienoisoxazole phenoxy unsubstituted ethyl and propyl derivatives, useful as D4 antagonists. Said compounds are useful for the treatment of medical conditions mediated by inhibition of D4 receptor. These conditions comprise, for example, Attention Deficit Hyperactivity Disorder, Obsessive-Compulsive Disorder, Psychoses, Substance Abuse, Substance Dependence, Parkinson's Disease, Parkinsonism, Tardive Diskinesia, Gilles de la Tourette Syndrome, Conduct Disorder, and Oppositional Defiant Disorder. A further aspect of the invention is to provide a pharmaceutical composition, intermediates, and a method of making said class of compounds.
摘要翻译：这些化合物是类似的噻吩异恶唑苯氧基未取代的乙基和丙基衍生物，可用作D 4 N 4拮抗剂。所述化合物可用于治疗通过抑制D 4受体介导的医学病症。这些病症包括例如注意力缺陷多动障碍，强迫症，精神病，药物滥用，物质依赖性，帕金森病，帕金森综合征，迟发性麻痹症，杜氏综合征，行为障碍和反对性反抗障碍。本发明的另一方面是提供药物组合物，中间体和制备所述类化合物的方法。

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