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1. 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.

2. 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。

3. 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。

4. 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.

5. 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。

6. 发明授权

US4748180A .beta.-carboline-3-carboxylic acid derivatives, and their use as psychotropic and anti-epileptic agents 失效
标题翻译： β-咔啉-3-羧酸衍生物，以及它们作为精神药物和抗癫痫剂的用途
公开(公告)号：US4748180A
公开(公告)日：1988-05-31
申请号：US917333
申请日：1986-10-09
申请人： Erling N. Petersen , Leif H. Jensen , Frank Watjen , Dieter Seidelmann
发明人： Erling N. Petersen , Leif H. Jensen , Frank Watjen , Dieter Seidelmann
IPC分类号： A61K31/435 , A61P25/00 , A61P25/20 , A61P39/02 , C07D209/08 , C07D209/18 , C07D471/04 , A61K31/395 , A61K31/40
CPC分类号： C07D471/04 , C07D209/08 , C07D209/18
摘要： New .beta.-carboline-3-carboxylic acid esters have the general formula I: ##STR1## wherein R.sup.4, R.sup.5 and R.sup.6 have specified meanings. The new compounds exhibit surprising psychotropic properties.

7. 发明授权

US4670433A Oxadiazolyl imidazobenzodiazepine derivatives pharmaceutical compositions thereof, and method of treating therewith 失效
标题翻译：恶二唑基咪唑并二氮杂衍生物药物组合物及其处理方法
公开(公告)号：US4670433A
公开(公告)日：1987-06-02
申请号：US837100
申请日：1986-03-06
申请人： Frank Watjen , Mogens Engelstoft , John B. Hansen , Leif H. Jensen
发明人： Frank Watjen , Mogens Engelstoft , John B. Hansen , Leif H. Jensen
IPC分类号： C07D20060101 , C07D271/06 , C07D487/04 , C07D487/14 , A61K31/555
CPC分类号： C07D271/06 , C07D487/04 , C07D487/14
摘要： New oxadiazolyl imidazobenzodiazepine derivatives having the formula ##STR1## wherein R.sup.3 has the formula ##STR2## wherein R" is hydrogen, C.sub.1-6 alkyl C.sub.1-6 alkoxymethyl or C.sub.3-6 - cycloalkyl;R.sup.4 is hydrogen;R.sup.5 is C.sub.1-6 alkyl or R.sup.4 and R.sup.5 together form a 2-4 membered alkylene bridge; and R.sup.A is C.sub.1-6 alkyl, C.sub.1-6 alkoxy, or C.sub.1-3 trifluoroalkyl, pharmaceutical compositions thereof, and method of treating therewith, are disclosed.The compounds and pharmaceutical compositions are useful in the amelioration, mitigation, or elimination of central nervous system disorders related to benzodiazepine receptors and especially as anticonvulsants, anxiolytics, hypnotics, and nootropics.
摘要翻译：具有式“IMAGE”的新的恶二唑基咪唑并二氮杂衍生物，其中R 3具有式“IMAGE”，其中R“是氢，C 1-6烷基C 1-6烷氧基甲基或C 3-6 - 环烷基; R4是氢; R5是C1-6烷基或R4和R5一起形成2-4元亚烷基桥; RA是C 1-6烷基，C 1-6烷氧基或C 1-3三氟烷基，其药物组合物及其处理方法。化合物和药物组合物可用于改善，缓解或消除与苯二氮卓类受体相关的中枢神经系统疾病，特别是抗惊厥药，抗焦虑药，催眠药和嗜酸剂。

8. 发明授权

US4631285A .beta.-Carboline-3-carboxylic acid derivatives, and their use as psychotropic agents 失效
标题翻译： β-咔啉-3-羧酸衍生物及其作为精神药物的用途
公开(公告)号：US4631285A
公开(公告)日：1986-12-23
申请号：US734222
申请日：1985-05-15
申请人： Erling N. Petersen , Leif H. Jensen , Frank Watjen , Dieter Seidelmann
发明人： Erling N. Petersen , Leif H. Jensen , Frank Watjen , Dieter Seidelmann
IPC分类号： A61K31/435 , A61P25/00 , A61P25/20 , A61P39/02 , C07D209/08 , C07D209/18 , C07D471/04 , A61K31/395
CPC分类号： C07D471/04 , C07D209/08 , C07D209/18
摘要： New .beta.-carboline-3-carboxylic acid esters have the general formula I: ##STR1## wherein R.sup.4, R.sup.5 and R.sup.6 have specified meanings. The new compounds exhibit surprising psychotropic properties.
摘要翻译：新的β-咔啉-3-羧酸酯具有通式I：其中R 4，R 5和R 6具有特定的含义。新化合物表现出惊人的精神病学特性。

9. 发明授权

US5478859A Indole-derivatives, method of treatment therewith, and pharmaceutical compositions comprising such compounds 失效
标题翻译：吲哚衍生物，其治疗方法和包含这些化合物的药物组合物
公开(公告)号：US5478859A
公开(公告)日：1995-12-26
申请号：US259016
申请日：1994-06-13
申请人： Frank Watjen , Jorgen Drejer , Leif H. Jensen
发明人： Frank Watjen , Jorgen Drejer , Leif H. Jensen
IPC分类号： C07D209/40 , A61K31/40 , C07D403/12
CPC分类号： C07D209/40
摘要： The present patent application discloses compounds having the formula ##STR1## or a pharmaceutically acceptable salt thereof wherein R.sup.21 and R.sup.22 each independently are alkyl; andR.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.11, R.sup.12, R.sup.13, and R.sup.14 each independently are hydrogen, halogen, CF.sub.3, CN, or NO.sub.2.The compounds are useful as in vivo active glutamate antagonists.
摘要翻译：本专利申请公开了具有式“IMAGE”的化合物或其药学上可接受的盐，其中R 21和R 22各自独立地为烷基; 并且R 1，R 2，R 3，R 4，R 11，R 12，R 13和R 14各自独立地为氢，卤素，CF 3，CN或NO 2。这些化合物可用作体内活性谷氨酸拮抗剂。

10. 发明授权

US5223527A Isatineoxime derivatives and their use 失效
标题翻译：伊马替尼肟衍生物及其用途
公开(公告)号：US5223527A
公开(公告)日：1993-06-29
申请号：US899620
申请日：1992-06-16
申请人： Frank Watjen , Jorgen Drejer , Leif H. Jensen
发明人： Frank Watjen , Jorgen Drejer , Leif H. Jensen
IPC分类号： C07D209/60
CPC分类号： C07D209/60
摘要： A compound having the formula ##STR1## wherein R.sup.1 is C.sub.1-6 -alkyl which may be branched or cyclic;R.sup.2 is 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 --, wherein n is 3, 4, 5.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 1是可以是支链或环状的C 1-6 - 烷基; R2是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）n - ，其中n为3,4,5。以及治疗对谷氨酸和天冬氨酸受体的封闭反应的哺乳动物（包括人）的病症的方法，其中相同。

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