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21. 发明授权

US4731374A Tetrahydro-benzthiazoles, the preparation thereof and their use as intermediate products or as pharmaceuticals 失效
标题翻译：四氢 - 苯并噻唑，其制备方法及其作为中间产物或药物的用途
公开(公告)号：US4731374A
公开(公告)日：1988-03-15
申请号：US810947
申请日：1985-12-19
申请人： Gerhart Griss, deceased , Rudolf Hurnaus , Walter Kobinger , Ludwig Pichler , Rudolf Bauer , Joachim Mierau , Dieter Hinzen , Gunter Schingnitz
发明人： Gerhart Griss, deceased , Rudolf Hurnaus , Walter Kobinger , Ludwig Pichler , Rudolf Bauer , Joachim Mierau , Dieter Hinzen , Gunter Schingnitz
IPC分类号： A61K31/425 , C07D277/82
CPC分类号： C07D277/82
摘要： This invention relates to new tetrahydrobenzthiazoles of general formula ##STR1## wherein R.sub.1 represents a hydrogen atom, an alkyl group, an alkenyl or alkynylk group, an alkanoyl group, a phenyl alkyl or phenyl alkanoyl group, while the above mentioned phenyl nuclei may each be substituted by 1 or 2 halogen atoms,R.sub.2 represents a hydrogen atom or an alkyl group,R.sub.3 represents a hydrogen atom, an alkyl group a cycloalkyl group, an alkenyl or alkynyl group, an alkanoyl group, a phenyl alkyl or phenyl alkanoyl group, while the phenyl nucleus may be substituted by flurorine, chlorine or bromine atoms,R.sub.4 represents a hydrogen atom, an alkyl group, an alkyl or alkenyl group, orR.sub.3 and R.sub.4 together with the nitrogen atom between them represent a pyrrolidino, piperidino, hexamethyleneimino or morpholino group, the enantiomers and the acid addition salts thereof.The compounds of general formula I above in which one of the groups R.sub.1 or R.sub.3 or both groups R.sub.1 and R.sub.3 represent an acyl group are valuable intermediate products for preparing the other compounds of general formula I which have valuable pharmacological properties. The new compounds may be prepared using methods known per se.
摘要翻译：本发明涉及通式为（I）的新的四氢苯并噻唑，其中R 1表示氢原子，烷基，烯基或炔基，烷酰基，苯基烷基或苯基烷酰基，而上述苯基核可各自被1或2个卤素原子取代，R2表示氢原子或烷基，R3表示氢原子，烷基，环烷基，烯基或炔基，烷酰基，苯基烷基或苯基烷酰基基团可以被氟里酰，氯或溴原子取代，R4表示氢原子，烷基，烷基或烯基，或者R3和R4与它们之间的氮原子一起代表吡咯烷子基，哌啶子基，六亚甲基亚氨基或吗啉代基，其对映异构体及其酸加成盐。上述通式I的化合物，其中R1或R3基团或R1和R3两个基团之一表示酰基，是制备其它具有有价值的药理学性质的通式I化合物的有价值的中间产物。新化合物可以使用本身已知的方法制备。

22. 发明申请

US20060223869A1 COMPOUNDS FOR THE REDUCTION OF EXCESSIVE FOOD INTAKE 审中-公开
标题翻译：减少过量食物摄入的化合物
公开(公告)号：US20060223869A1
公开(公告)日：2006-10-05
申请号：US11423159
申请日：2006-06-26
申请人： Michael PIEPER , Joachim Mierau
发明人： Michael PIEPER , Joachim Mierau
IPC分类号： A61K31/428
CPC分类号： A61K31/426 , A61K31/00 , A61K31/428
摘要： The invention relates to the use of dopamine receptor agonists for preparing a pharmaceutical composition for the reduction of excessive food intake.
摘要翻译：本发明涉及多巴胺受体激动剂用于制备用于减少过量食物摄取的药物组合物的用途。

23. 发明申请

US20060030607A1 Compounds for the reduction of excessive food intake 审中-公开
公开(公告)号：US20060030607A1
公开(公告)日：2006-02-09
申请号：US11244806
申请日：2005-10-06
申请人： Michael Pieper , Joachim Mierau
发明人： Michael Pieper , Joachim Mierau
IPC分类号： A61K31/428
CPC分类号： A61K31/426 , A61K31/00 , A61K31/428
摘要： The invention relates to the use of dopamine receptor agonists for preparing a pharmaceutical composition for the reduction of excessive food intake.

24. 发明申请

US20050277664A1 Monoamine neurotransmitter re-uptake inhibitor for the inhibition of beta-amyloid generation 审中-公开
标题翻译：单胺神经递质再摄取抑制剂用于抑制β-淀粉样蛋白的产生
公开(公告)号：US20050277664A1
公开(公告)日：2005-12-15
申请号：US11144481
申请日：2005-06-03
申请人： Klaus Bornemann , Joachim Mierau , Dagmar Kugler
发明人： Klaus Bornemann , Joachim Mierau , Dagmar Kugler
IPC分类号： A61K31/46
CPC分类号： A61K31/46
摘要： The invention relates to the use of a monoamine neurotransmitter re-uptake inhibitor comprising a 2,3-disubstituted tropane moiety for the preparation of a medicament for inhibiting β-amyloid generation.
摘要翻译：本发明涉及包含2,3-二取代托烷部分的单胺神经递质再摄取抑制剂用于制备抑制β-淀粉样蛋白产生的药物的用途。

25. 发明申请

US20050154009A1 Pharmaceutical composition comprising a monoamine neurotransmitter re-uptake inhibitor and an acetylcholinesterase inhibitor 审中-公开
标题翻译：包含单胺神经递质再摄取抑制剂和乙酰胆碱酯酶抑制剂的药物组合物
公开(公告)号：US20050154009A1
公开(公告)日：2005-07-14
申请号：US10965994
申请日：2004-10-15
申请人： Thomas Friedl , Joachim Mierau , Andreas Raschig , Juergen Reess , Joergen Scheel-Krueger
发明人： Thomas Friedl , Joachim Mierau , Andreas Raschig , Juergen Reess , Joergen Scheel-Krueger
IPC分类号： A61K9/16 , A61K9/24 , A61K9/28 , A61K31/27 , A61K31/407 , A61K31/445 , A61K31/46 , A61K31/4706 , A61K31/55
CPC分类号： A61K31/46 , A61K9/1652 , A61K9/209 , A61K9/2866 , A61K31/27 , A61K31/407 , A61K31/445 , A61K31/4706 , A61K31/55 , A61K2300/00
摘要： The invention relates to a pharmaceutical composition comprising a monoamine neurotransmitter re-uptake inhibitor comprising a 2,3-disubstituted tropane moiety, or a tautomer, a pharmaceutically acceptable salt, solvate, or physiologically functional derivative thereof, and at least one acetylcholinesterase inhibitor or a pharmaceutically acceptable salt, solvate, or physiologically functional derivative thereof, and a pharmaceutically acceptable carrier or excipient, and optionally one or more other therapeutic ingredients.
摘要翻译：本发明涉及包含单胺神经递质再摄取抑制剂的药物组合物，其包含2,3-二取代的托烷部分或互变异构体，其药学上可接受的盐，溶剂合物或生理功能衍生物，以及至少一种乙酰胆碱酯酶抑制剂或其药学上可接受的盐，溶剂化物或生理功能衍生物，以及药学上可接受的载体或赋形剂，以及任选的一种或多种其它治疗成分。

26. 发明授权

US4981862A Tetrahydrobenzothiazoles, and the preparation and use thereof 失效
标题翻译：四氢苯并噻唑及其制备和应用
公开(公告)号：US4981862A
公开(公告)日：1991-01-01
申请号：US287829
申请日：1988-12-20
申请人： Claus Schneider , Herbert Merz , Rainer Sobotta , Rudolf Bauer , Joachim Mierau , Gunter Schingnitz
发明人： Claus Schneider , Herbert Merz , Rainer Sobotta , Rudolf Bauer , Joachim Mierau , Gunter Schingnitz
IPC分类号： C07D277/60 , A61K31/425 , A61K31/428 , A61P5/00 , A61P25/00 , A61P25/16 , A61P25/18 , C07D277/82
CPC分类号： C07D277/82
摘要： Tetrahydrobenzothiazole derivatives of the formula ##STR1## wherein n is 1, 2 or 3 and R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are defined substituents, said derivatives (I) being suitable as active compounds for treating parkinsonism or Parkinson's Disease.
摘要翻译：式（Ⅰ）的四氢苯并噻唑衍生物其中n为1,2或3，R 1，R 2，R 3，R 4，R 5和R 6为定义的取代基，所述衍生物（I）适用作治疗帕金森综合征或帕金森病疾病。

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