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1. 发明授权

US5356912A 3-(5-isoxazolyl)-1-methyl-1,2,3,6-tetrahydropyridine useful for treating Alzheimer's disease 失效
标题翻译：可用于治疗阿尔茨海默氏病的3-（5-异恶唑基）-1-甲基-1,2,3,6-四氢吡啶
公开(公告)号：US5356912A
公开(公告)日：1994-10-18
申请号：US151402
申请日：1993-11-12
申请人： Lone Nielsen , Frank Watjen , Jens W. Kindtler , Preben H. Olesen , Per Sauerberg
发明人： Lone Nielsen , Frank Watjen , Jens W. Kindtler , Preben H. Olesen , Per Sauerberg
IPC分类号： A61K31/42 , A61K31/435 , A61K31/445 , A61K31/46 , A61P25/28 , C07D211/70 , C07D211/72 , C07D413/04 , C07D451/02 , C07D451/04 , C07D453/02 , A61K31/44
CPC分类号： C07D451/02 , C07D211/70 , C07D211/72 , C07D413/04 , C07D451/04 , C07D453/02
摘要： Novel azacyclic compounds selected from the group consisting of ##STR1## wherein R.sup.1 is H or C.sub.1-6 -alkylR.sup.3 is ##STR2## R" is H or C.sub.1-8 -alkyl or C.sub.1-6 -alkoxy or C.sub.1-4 -alkoxy-C.sub.1-4 -alkyl or aryl, andR.sup.4 is H, C.sub.1-8 -alkyl or Cl;and a salt thereof with a pharmaceutically-acceptable acid.The new compounds are useful in improving the cognitive functions of the forebrain and hippocampus of mammals, and are useful in the treatment of Alzheimer's disease.
摘要翻译：选自由下列组成的组的新型氮杂环烷化合物：其中R 1为H或C 1-6 - 烷基R 3为H或C 1-8 - 烷基或C 1-6 - 烷氧基或C 1-8 - 4-烷氧基-C 1-4 - 烷基或芳基，并且R 4是H，C 1-8 - 烷基或Cl; 及其与药学上可接受的酸的盐。新化合物可用于改善哺乳动物前脑和海马的认知功能，可用于治疗阿尔茨海默病。

2. 发明授权

US5262427A 3-substituted and optionally 1-substituted azacyclic or azabicyclic compounds, pharmaceutical compositions, thereof and their use as stimulants of cognitive functions 失效
标题翻译： 3-取代的和任选的1-取代的氮杂环或氮杂双环化合物，其药物组合物及其作为认知功能的兴奋剂的用途
公开(公告)号：US5262427A
公开(公告)日：1993-11-16
申请号：US268940
申请日：1988-11-08
申请人： Lone Nielson , Frank Watjen , Jens W. Kindtler , Preben H. Olesen , Per Sauerberg
发明人： Lone Nielson , Frank Watjen , Jens W. Kindtler , Preben H. Olesen , Per Sauerberg
IPC分类号： A61K31/42 , A61K31/435 , A61K31/445 , A61K31/46 , A61P25/28 , C07D211/70 , C07D211/72 , C07D413/04 , C07D451/02 , C07D451/04 , C07D453/02 , A61K31/41
CPC分类号： C07D451/02 , C07D211/70 , C07D211/72 , C07D413/04 , C07D451/04 , C07D453/02
摘要： Azacyclic compounds selected from the group consisting of ##STR1## wherein R.sup.1 is H or C.sub.1-6 -alkylR.sup.3 is ##STR2## wherein R' is C.sub.3-8 -alkyl, cyclopropyl, C.sub.4-8 -cycloalkyl, benzyl which may be substituted, or C.sub.1-4 -alkoxy-C.sub.1-4 -alkyl, andR" is H or C.sub.1-8 -alkyl or C.sub.1-6 -alkoxy or C.sub.1-4 -alkoxy-C.sub.1-4 -alkyl or aryl, andR'" is H or C.sub.1-6 -alkyl or C.sub.4-8 -cycloalkyl; andR.sup.4 is H, C.sub.1-8 -alkyl or Cl; and ##STR3## provided that R.sup.3 is not ##STR4## wherein R' is C.sub.3-8 -alkyl, cyclopropyl or C.sub.1-3 -alkoxymethyl, and provided that R.sup.3 is not --CH.dbd.N--OR'", wherein R'" is H or C.sub.1-6 -alkyl, when the compounds of formula I is ##STR5## and a salt thereof with a pharmaceutically-acceptable acid. The new compounds are useful in improving the cognitive functions of the forebrain and hippocampus of mammals, and are useful in the treatment of Alzheimer's disease.

3. 发明授权

US4933353A Lipophilically-substituted piperidine oxadiazolyl compounds and their use in stimulating cognitive functions (II) 失效
标题翻译：亲脂取代的哌啶恶二唑基化合物及其在刺激认知功能中的应用（二）
公开(公告)号：US4933353A
公开(公告)日：1990-06-12
申请号：US236550
申请日：1988-08-25
申请人： Leif H. Jensen , Per Sauerberg , Frank Watjen , Jens W. Kindtler
发明人： Leif H. Jensen , Per Sauerberg , Frank Watjen , Jens W. Kindtler
IPC分类号： A61K31/445 , A61K31/44 , A61P25/02 , A61P25/28 , C07D413/04 , C07D413/14 , G01N21/90
CPC分类号： C07D413/04 , C07D413/14
摘要： New piperidine compounds having the formula ##STR1## wherein at least one of R.sup.3, R.sup.4, and R.sup.5 are ##STR2## and the other independently are H, C.sub.1-6 -alkyl, wherein R' is H, C.sub.1-8 -alkyl, phenyl, thienyl, cyclopropyl, or C.sub.1-3 -alkoxymethyl; andR.sup.1 and R.sup.6 independently are H or C.sub.1-6 -alkyl, and wherein ##STR3## and salts thereof with pharmaceutically-acceptable acids. The new compounds are useful in improving the cognitive functions of the forebrain and hippocampus of mammals, and are therefore useful in the treatment of Alzheimer's disease.

4. 发明授权

US4837241A Lipophillically-substituted piperidine oxadiazolyl compounds and their use in stimulating cognitive functions 失效
标题翻译：亲油取代的哌啶恶二唑基化合物及其在刺激认知功能中的用途
公开(公告)号：US4837241A
公开(公告)日：1989-06-06
申请号：US89747
申请日：1987-08-26
申请人： Leif H. Jensen , Per Sauerberg , Frank Watjen , Jens W. Kindtler
发明人： Leif H. Jensen , Per Sauerberg , Frank Watjen , Jens W. Kindtler
IPC分类号： A61K31/445 , A61K31/44 , A61P25/02 , A61P25/28 , C07D413/04 , C07D413/14 , G01N21/90
CPC分类号： C07D413/04 , C07D413/14
摘要： New piperidine compounds having the formula ##STR1## wherein at least one of R.sup.3, R.sup.4, and R.sup.5 are ##STR2## and the other independently are H, C.sub.1-6 -alkyl, wherein R' is H, C.sub.1-8 -alkyl, phenyl, thienyl, cyclopropyl, or C.sub.1-3 -alkoxymethyl; and R.sup.1 and R.sup.6 independently are H or C.sub.1-6 -alkyl, and wherein ##STR3## and salts thereof with pharmaceutically-acceptable acids. The new compounds are useful in improving the cognitive functions of the forebrain and hippocampus of mammals, and are therefore useful in the treatment of Alzheimer's disease.
摘要翻译：具有式“IMAGE”的新的哌啶化合物，其中R 3，R 4和R 5中的至少一个是H，并且另外独立地是H，C 1-6 - 烷基，其中R'是H，C 1-8 - 烷基，苯基，噻吩基，环丙基或C 1-3 - 烷氧基甲基; 并且R 1和R 6独立地为H或C 1-6 - 烷基，并且其中其与药学上可接受的酸形成。新化合物可用于改善哺乳动物前脑和海马的认知功能，因此可用于治疗阿尔茨海默氏病。

5. 发明授权

US06649609B2 Benzimidazole derivatives and pharmaceutical compositions comprising these compounds 失效
标题翻译：苯并咪唑衍生物和包含这些化合物的药物组合物
公开(公告)号：US06649609B2
公开(公告)日：2003-11-18
申请号：US10012490
申请日：2001-12-12
申请人： Lene Teuber , Frank Watjen
发明人： Lene Teuber , Frank Watjen
IPC分类号： C07D23506
CPC分类号： C07D235/06 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/10 , C07D401/12 , C07D403/10 , C07D403/12 , C07D405/04 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D413/14
摘要： The present invention relates to novel 1-phenylbenzimidazole derivatives having particular alkoxycarbonyl substituents in the 5-position of the benz ring and having particular cyclic substituents in the meta-position of the phenyl ring, as well as to pharmaceutical compositions containing these compounds and to methods of treatment therewith. The compounds of the invention are useful in the treatment of central nervous system diseases and disorders, which are responsive to modulation of GABAA receptor complex, and in particular for inducing and maintaining anaesthesia, sedation, and muscle relaxation, as well as for combating febrile convulsions in children. The compounds of the invention may also be used by veterinarians.
摘要翻译：本发明涉及在苯环的5-位上具有特定的烷氧基羰基取代基并且在苯环的间位具有特定的环状取代基的新的1-苯基苯并咪唑衍生物以及含有这些化合物的药物组合物和方法的治疗。本发明的化合物可用于治疗中枢神经系统疾病和病症，其对GABAα受体复合物的调节有反应，特别是诱导和维持麻醉，镇静和肌肉松弛以及对于打击儿童发热性惊厥。本发明的化合物也可以由兽医使用。

6. 发明授权

US5843945A AMPA antagonists and a method of treatment 失效
标题翻译： AMPA拮抗剂和治疗方法
公开(公告)号：US5843945A
公开(公告)日：1998-12-01
申请号：US951059
申请日：1997-10-15
申请人： Frank Watjen , Jorgen Drejer
发明人： Frank Watjen , Jorgen Drejer
IPC分类号： C07D471/04 , C07D487/04 , A61K31/55 , A61K31/495 , C07D487/00
CPC分类号： C07D471/04 , C07D487/04
摘要： The present patent application discloses compounds having formula (I) or a pharmaceutically acceptable salt thereof wherein R.sup.1 is hydrogen, alkyl or benzyl; X is O or NOR.sup.2, wherein R.sup.2 is hydrogen, alkyl or benzyl; Y is N--R.sup.4 wherein R.sup.4 is hydrogen, OH or alkyl; n is 0 or 1; R.sup.6 is phenyl, naphthyl, thienyl, pyridyl, all of which may be substituted one or more times with substituents selected from the group consisting of halogen, CF.sub.3, NO.sub.2, amino, alkyl, alkoxy and phenyl; A is a ring of five to seven atoms fused with the benzo ring at the positions marked a and b. The compounds are useful in the treatment of cerebrovascular disorders. ##STR1##
摘要翻译：本专利申请公开了具有式（I）的化合物或其药学上可接受的盐，其中R 1是氢，烷基或苄基; X是O或NOR2，其中R2是氢，烷基或苄基; Y是N-R4，其中R4是氢，OH或烷基; n为0或1; R6是苯基，萘基，噻吩基，吡啶基，它们都可以被选自卤素，CF 3，NO 2，氨基，烷基，烷氧基和苯基的取代基取代一次或多次; A是在标记a和b的位置与苯环稠合的5至7个原子的环。该化合物可用于治疗脑血管障碍。

7. 发明授权

US5780493A AMPA antagonists and method of treatment therewith 失效
标题翻译： AMPA拮抗剂及其治疗方法
公开(公告)号：US5780493A
公开(公告)日：1998-07-14
申请号：US951821
申请日：1997-10-16
申请人： Frank Watjen , Jorgen Drejer
发明人： Frank Watjen , Jorgen Drejer
IPC分类号： C07D471/04 , C07D487/04 , A61K31/40 , A61K31/44 , C07D401/00 , C07D487/02
CPC分类号： C07D471/04 , C07D487/04
摘要： The present patent application discloses compounds having formula (I) or a pharmaceutically acceptable salt thereof wherein R.sup.1 is hydrogen, alkyl or benzyl; X is O or NOR.sup.2, wherein R.sup.2 is hydrogen, alkyl or benzyl; Y is N--R.sup.4 wherein R.sup.4 is hydrogen, OH or alkyl; n is 0 or 1; R.sup.6 is phenyl, naphthyl, thienyl, pyridyl, all of which may be substituted one or more times with substituents selected from the group consisting of halogen; CF.sub.3, NO.sub.2, amino, alkyl, alkoxy and phenyl; A is a ring of five to seven atoms fused with the benzo ring at the positions marked a and b. The compounds are useful in the treatment of cerebrovascular disorders for example. ##STR1##
摘要翻译：本专利申请公开了具有式（I）的化合物或其药学上可接受的盐，其中R 1是氢，烷基或苄基; X是O或NOR2，其中R2是氢，烷基或苄基; Y是N-R4，其中R4是氢，OH或烷基; n为0或1; R6是苯基，萘基，噻吩基，吡啶基，它们都可以被选自卤素的取代基取代一次或多次; CF 3，NO 2，氨基，烷基，烷氧基和苯基; A是在标记a和b的位置与苯环稠合的5至7个原子的环。该化合物可用于治疗例如脑血管障碍。（一）

8. 发明授权

US5736556A Tropane-2-aldoxime derivatives as nevro transmitter reuptake inhibitors 失效
标题翻译：托烷-2-醛肟衍生物作为神经发生器再摄取抑制剂
公开(公告)号：US5736556A
公开(公告)日：1998-04-07
申请号：US722010
申请日：1996-10-11
申请人： Peter Moldt , Frank Watjen , J.o slashed.rgen Scheel-Kruger
发明人： Peter Moldt , Frank Watjen , J.o slashed.rgen Scheel-Kruger
IPC分类号： A61K31/46 , A61P3/04 , A61P25/00 , A61P25/20 , A61P25/24 , A61P25/26 , A61P25/30 , A61P43/00 , C07D451/02 , A61K31/44 , C07D451/10
CPC分类号： C07D451/02
摘要： The present invention discloses compounds of the formula, ##STR1## any mixture thereof, or a pharmaceutically acceptable salt thereof; wherein R, R.sup.3, and R.sup.4 each have the meanings set forth in the specification. The compounds possess valuable pharmaceutical properties as monoamine neurotransmitter, i.e dopamine, serotonin, noradrenalin, reuptake inhibitors.
摘要翻译： PCT No.PCT / EP95 / 01358 Sec。 371日期：1996年10月11日 102（e）日期1996年10月11日PCT提交1995年4月12日PCT公布。 WO95 / 28401 PCT出版物日期：1995年10月26日本发明公开了下式的化合物：其任意混合物或其药学上可接受的盐; 其中R，R 3和R 4各自具有说明书中阐述的含义。该化合物具有作为单胺神经递质（即多巴胺，5-羟色胺，去甲肾上腺素，再摄取抑制剂）的有价值的药物性质。

9. 发明授权

US5242918A Isatinoxime derivatives, their preparation and use 失效
标题翻译：伊马替尼衍生物，其制备和用途
公开(公告)号：US5242918A
公开(公告)日：1993-09-07
申请号：US936579
申请日：1992-08-27
申请人： Frank Watjen , Bjarne H. Dahl , Jorgen Drejer , Leif H. Jensen
发明人： Frank Watjen , Bjarne H. Dahl , Jorgen Drejer , Leif H. Jensen
IPC分类号： C07C205/45 , C07D471/04 , C07D487/04 , C07D491/04 , C07D491/048 , C07D495/04
CPC分类号： C07D471/04 , C07C205/45 , C07D487/04 , C07D491/04 , C07D495/04
摘要： A compound having the formula ##STR1## wherein R.sup.4 and R.sup.5 independently are hydrogen, halogen, CF.sub.3, CN, NO.sub.2 or SO.sub.2 NR.sup.1 R.sup.2 whereinR.sup.1 is hydrogen or straight, C.sub.1-6 -alkyl which may be branched or cyclic,R.sup.2 is hydrogen or straight, C.sub.1-6 -alkyl which may be branched or cyclic,or wherein R.sup.1 and R.sup.2 together represent --(CH.sub.2).sub.n --A--(CH.sub.2).sub.m --, wherein A is O, S, CH.sub.2 or NR.sup.I, wherein R.sup.I is H, C.sub.1-6 -alkyl which may be straight, branched or cyclic, n is 0, 1, 2, 3, 4, 5 and m is 0, 1, 2, 3, 4, 5;Q is NOH or O;Z=O, S, N--R.sup.II, ##STR2## wherein R.sup.II, R.sup.III, R.sup.IV and R.sup.V independently are hydrogen, benzyl, C.sub.1-6 carboxylic acid-acyl, C.sub.1-6 -alkoxy which may be branched or cyclic, or C.sub.1-6 -alkyl which may be branched or cyclic;X is --(CH.sub.2).sub.o -- wherein o is 0, 1, 2, or 3;Y is --(CH.sub.2).sub.p -- wherein p is 0, 1, 2 or 3;.alpha. and .beta. indicate attachment points,and a method of treating disorders of a mammal, including a human, responsive to the blockade of glutamic and aspartic acid receptors, with the same.
摘要翻译：具有式“IMAGE”的化合物，其中R 4和R 5独立地是氢，卤素，CF 3，CN，NO 2或SO 2 NR 1 R 2，其中R 1是氢或直链，可以是支链或环状的C 1-6 - 烷基，R 2是氢或直链，可以是支链或环状的C 1-6 - 烷基，或其中R 1和R 2一起表示 - （CH 2）nA-（CH 2）m - ，其中A是O，S，CH 2或NRI，其中R 1是H，C 1-6 - 烷基，其可以是直链，支链或环状的，n为0,1,2,3,4,5，m为0,1,2,3,4,5; Q是NOH或O; Z = O，S，N-RII，其中RII，RIII，RIV和RV独立地是氢，苄基，C1-6羧酸 - 酰基，可以是支链或环状的C1-6 - 烷氧基或C1-6 可以是支链或环状的 - 烷基; X是 - （CH 2）o - ，其中o是0,1,2或3; Y是 - （CH 2）p - ，其中p是0,1,2或3; α和β表示连接点，以及一种治疗对谷氨酸和天冬氨酸受体的封闭有反应的哺乳动物（包括人）的病症的方法。

10. 发明授权

US5075304A Imidazoquinoxaline compounds and their preparation and use 失效
标题翻译：咪唑啉酮化合物及其制备和使用
公开(公告)号：US5075304A
公开(公告)日：1991-12-24
申请号：US353793
申请日：1989-05-18
申请人： Holger C. Hansen , Frank Watjen
发明人： Holger C. Hansen , Frank Watjen
IPC分类号： A61K31/495 , A61P25/00 , C07D487/04
CPC分类号： C07D487/04
摘要： New imidazoquinoxaline compounds having the general formula ##STR1## wherein R.sup.3 is ##STR2## or CO.sub.2 R' wherein R' isC.sub.3-7 -cycloalkyl;R.sup.5 is methyl, which is substituted with hydrogen, alkoxycarbonyl, heteroaryl, morpholino, C.sub.3-7 -cycloalkyl, C.sub.1-6 -alkenyl, arylacyl, alkylacyl, alkoxyalkyl, alkoxy, phthalimidophenyl, aralkyl or aryl, all of which are substituted with hydrogen, halogen, C.sub.1-6 -alkyl, amino, azido, or C.sub.1-6 -alkoxy;and R.sup.6 is H, C.sub.1-6 -alkyl, halogen, or CF.sub.3.The compounds are useful in psychopharmaceutical preparations as anticonvulsants, anxiolytics, hypnotics, and in improving the cognitive function of the brain of mammals.

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