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1. 发明授权

US4843086A 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：US4843086A
公开(公告)日：1989-06-27
申请号：US124197
申请日：1987-11-23
申请人： Gerhart Griss, deceased , Claus Schneider , Rudolf Hurnaus , Walter Kobinger , Ludwig Pichler , Rudolf Bauer , Joachim Mierau , Dieter Hinzen , Gunter Schingnitz
发明人： Gerhart Griss, deceased , Claus Schneider , 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 alkynyl 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 fluorine, 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，而苯基核可以被氟取代，氯或溴原子，R4表示氢原子，烷基，烷基或烯基或R3和R4以及它们之间的氮原子表示吡咯烷子基，哌啶子基，六亚甲基亚氨基或吗啉代基，对映体和酸加成的盐。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。

2. 发明授权

US4886812A 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：US4886812A
公开(公告)日：1989-12-12
申请号：US256671
申请日：1988-10-12
申请人： Gerhart Griss, deceased , Claus Schneider , Rudolf Hurnaus , Walter Kobinger , Ludwig Pichler , Rudolf Bauer , Joachim Mierau , Dieter Hinzen , Gunter Schingnitz
发明人： Gerhart Griss, deceased , Claus Schneider , 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 alkynyl group, an alkanoyl group, a phenyl alkyl or phenyl alkanoyl group, while the above mentioned phenyl nucleic 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 fluorine, 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，而上述苯基核酸可各自被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，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。

3. 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。

4. 发明授权

US5068325A 4,5,7,8-tetrahydro-6H-thiazolo[5,4-d]azepines, their preparation and their use as pharmaceutical compositions 失效
标题翻译： 4,5,7,8-四氢-6H-噻唑（5,4-D）亚胺，其制备及其作为药物组合物的用途
公开(公告)号：US5068325A
公开(公告)日：1991-11-26
申请号：US368753
申请日：1989-06-20
申请人： Wolfgang Grell , Rudolf Hurnaus , Manfred Reiffen , Robert Sauter , Ludwig Pichler , Walter Kobinger , Michael Entzeroth , Joachim Mierau , Gunter Schingnitz
发明人： Wolfgang Grell , Rudolf Hurnaus , Manfred Reiffen , Robert Sauter , Ludwig Pichler , Walter Kobinger , Michael Entzeroth , Joachim Mierau , Gunter Schingnitz
IPC分类号： A61K31/55 , A61P9/00 , A61P25/00 , C07D513/04
CPC分类号： C07D513/04
摘要： The present invention relates to new 4,5,7,8-tetrahydro-6H-thiazolo[5,4-d]azepines of general formula II ##STR1## wherein the substituents are defined herein below, which compounds have valuable pharmacological properties, namely selective effects on the dopaminergic system which are achieved by stimulating (predominantly D2) dopamine receptors.
摘要翻译：本发明涉及通式II（II）的新的4,5,7,8-四氢-6H-噻唑并[5,4-d]吖庚因，其中取代基如下文所定义，该化合物具有有价值的药理学性质，即通过刺激（主要是D2）多巴胺受体而实现的对多巴胺能系统的选择性作用。

5. 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。

6. 发明授权

US5053430A Use of 2,7-diamino-1,2,3,4-tetrahydronaphthalenes as medicaments, new 2,7-diamino-1,2,3,4-tetrahydronaphthalenes and processes for their preparation 失效
标题翻译： 2,7-二氨基-1,2,3,4-四氢萘酮作为药物的用途，新的2,7-二氨基-1,2,3,4-四氢萘并对其制备方法
公开(公告)号：US5053430A
公开(公告)日：1991-10-01
申请号：US411146
申请日：1989-09-22
申请人： Matthias Grauert , Herbert Merz , Joachim Mierau , Gunter Schingnitz , Claus Schneider
发明人： Matthias Grauert , Herbert Merz , Joachim Mierau , Gunter Schingnitz , Claus Schneider
IPC分类号： A61K31/135 , A61K31/17 , A61K31/18 , A61K31/33 , A61K31/38 , A61K31/381 , A61K31/425 , A61K31/426 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61P25/00 , A61P25/18 , A61P25/20 , C07C211/60 , C07C233/43 , C07C271/24 , C07C271/30 , C07C275/26 , C07C275/40 , C07C311/08 , C07C311/13 , C07C323/25 , C07D213/38 , C07D277/28 , C07D307/52 , C07D307/56 , C07D333/20 , C07D333/26 , C07D521/00
CPC分类号： C07C271/30 , C07C211/60 , C07C233/43 , C07C271/24 , C07C275/40 , C07C311/08 , C07C323/25 , C07D333/20 , C07C2101/02 , C07C2102/10
摘要： Novel compounds having the general formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as defined herein. These compounds are useful in the treatment of schizophrenia.
摘要翻译：具有通式的新型化合物，其中R 1，R 2，R 3和R 4如本文所定义。这些化合物可用于治疗精神分裂症。

7. 发明授权

US5196454A Method of treating disorders of the dopaminergic systems using 2,5-diaminotetralines 失效
标题翻译：使用2,5-DIAMINOTETRALIN治疗多巴胺系统疾病的方法
公开(公告)号：US5196454A
公开(公告)日：1993-03-23
申请号：US539093
申请日：1990-06-15
申请人： Matthias Grauert , Herbert Merz , Joachim Mierau , Gunter Schingnitz , Claus Schneider
发明人： Matthias Grauert , Herbert Merz , Joachim Mierau , Gunter Schingnitz , Claus Schneider
IPC分类号： C07D209/14 , A61K31/135 , A61K31/165 , A61K31/17 , A61K31/34 , A61K31/341 , A61K31/38 , A61K31/381 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/535 , A61K31/5375 , A61P9/12 , A61P25/00 , A61P25/18 , C07C209/08 , C07C211/57 , C07C211/60 , C07C217/60 , C07C233/43 , C07C233/80 , C07C271/30 , C07C275/28 , C07D209/16 , C07D227/04 , C07D295/20 , C07D307/52 , C07D333/20
CPC分类号： C07C271/30 , C07C211/60 , C07C217/60 , C07C233/43 , C07C233/80 , C07D209/16 , C07D307/52 , C07D333/20 , C07C2101/02 , C07C2102/10
摘要： The invention relates to novel 2,5-diaminotetralines of the formula: ##STR1## wherein R1, R2, R3 and R4 are defined herein, processes for preparing them and their use in pharmaceutical compositions. The novel 2,5-diaminotetralines are useful in treating diseases caused by disorders of the dopaminergic systems.
摘要翻译：本发明涉及下式的新的2,5-二氨基四氢萘酮：其中R1，R2，R3和R4如本文所定义，其制备方法及其在药物组合物中的应用。该新型2,5-二氨基四氢萘可用于治疗由多巴胺能系统疾病引起的疾病。

8. 发明授权

US5006533A Certain 3-bromo-2,6-dimethoxybenzamides and pharmaceutical use thereof 失效
标题翻译：某些3-溴-2,6-二甲氧基苯甲酰胺及其药物用途
公开(公告)号：US5006533A
公开(公告)日：1991-04-09
申请号：US440917
申请日：1989-11-22
申请人： Rainer Sobotta , Adolf Langbein , Herbert Merz , Rudolf Bauer , Joachim Mierau
发明人： Rainer Sobotta , Adolf Langbein , Herbert Merz , Rudolf Bauer , Joachim Mierau
IPC分类号： C07D221/22 , A61K31/435 , A61P25/00 , A61P25/02 , A61P25/20 , C07D451/04 , C07D471/02
CPC分类号： C07D451/04
摘要： 3-Bromo-2,6-dimethoxybenzamides useful as neuroleptic agents are described.
摘要翻译：描述了用作神经安定药的3-溴-2,6-二甲氧基苯甲酰胺。

9. 发明授权

US4393069A 8-Arylalkyl-3-phenyl-3-nortropanols and salts thereof 失效
标题翻译： 8-芳基烷基-3-苯基-3-正丙醇和其盐
公开(公告)号：US4393069A
公开(公告)日：1983-07-12
申请号：US324680
申请日：1981-11-25
申请人： Adolf Langbein , Herbert Merz , Rainer Sobotta , Rudolf Bauer , Hans M. Jennewein , Joachim Mierau
发明人： Adolf Langbein , Herbert Merz , Rainer Sobotta , Rudolf Bauer , Hans M. Jennewein , Joachim Mierau
IPC分类号： A61K31/46 , A61K31/49 , A61P5/00 , C07D451/06 , C07D401/02
CPC分类号： C07D451/06
摘要： Compounds of the formula ##STR1## wherein Ar is ##STR2## R.sub.1 is hydrogen, fluorine, bromine, methyl or methoxy; X is .dbd.CO, .dbd.CH--CN, .dbd.CH--OH, --O--, --S--, --NH--, ##STR3## and R is hydrogen, 4-fluoro, 4-chloro, 4-trifluoromethyl, 3-trifluoromethyl, 3-trifluoromethyl-4-chloro, 4-methyl or 4-methoxy;and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as neuroleptics.
摘要翻译：其中Ar为R 1的式“IMAGE”的化合物是氢，氟，溴，甲基或甲氧基; X为= CO，= CH-CN，= CH-OH，-O - ， - S - ， - NH-，+ IMA，其中R为氢，4-氟，4-氯，三氟甲基，3-三氟甲基，3-三氟甲基-4-氯，4-甲基或4-甲氧基; 和无毒的，药学上可接受的酸加成盐。化合物及其盐可用作神经安定药。

10. 发明申请

US20080051443A1 Compounds for the reduction of excessive food intake 审中-公开
公开(公告)号：US20080051443A1
公开(公告)日：2008-02-28
申请号：US11857016
申请日：2007-09-18
申请人： Michael Pieper , Joachim Mierau
发明人： Michael Pieper , Joachim Mierau
IPC分类号： A61K31/426 , A61P3/04
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.

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