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1. 发明公开

EP1961738A1 New compounds with antiglutamatergic properties and uses thereof 审中-公开
标题翻译： Neue Verbindungen mit glutamatantagonistischen Eigenschaften und deren Verwendung
公开(公告)号：EP1961738A1
公开(公告)日：2008-08-27
申请号：EP07290196.0
申请日：2007-02-15
申请人： Faust Pharmaceuticals
发明人： Schann, Stephan , Mayer, Stanislas
IPC分类号： C07C281/12 , C07D241/04 , C07D295/135 , C07D295/15 , A61K31/175 , A61K31/4453 , A61K31/5375 , A61P25/28
CPC分类号： C07C281/12 , C07C2602/10 , C07D295/088 , C07D295/116 , C07D295/135 , C07D295/15
摘要： The present invention provides new compounds displaying antiglutamatergic properties. It also provides the use of such compounds for the treatment and/or prophylaxis of conditions and diseases linked to abnormalities in glutamatergic transmission. It further provides a pharmaceutical composition for the treatment and/or prophylaxis of acute and chronic neurodegenerative conditions and disorders.
摘要翻译：本发明提供了具有防反光特性的新化合物。它还提供了这样的化合物用于治疗和/或预防与谷氨酸能传递异常有关的病症和疾病。它进一步提供用于治疗和/或预防急性和慢性神经变性疾病和病症的药物组合物。

2. 发明公开

EP1798233A1 Pyrrolo[1,2-a]quinoxaline derivatives as Adenosine A3 receptor modulators and uses thereof 审中-公开
标题翻译：吡咯并[1,2-a] chinoxalinderivate als腺苷A-3-Receptorenmodulatore und deren Verwendung
公开(公告)号：EP1798233A1
公开(公告)日：2007-06-20
申请号：EP05292739.9
申请日：2005-12-19
申请人： Faust Pharmaceuticals
发明人： Schann, Stephan , Mayer, Stanislas , Gardan, Sophie
IPC分类号： C07D487/04 , A61K31/498 , A61P9/00
CPC分类号： C07D487/04
摘要： The present invention provides new compounds of formula (I) displaying high affinity for adenosine A 3 receptors. It also provides modulators of adenosine A 3 receptors. It further provides compounds for the treatment and/or prophylaxis of conditions and diseases where adenosine A 3 receptor plays a role. Pharmaceutical compositions for the treatment and/or prophylaxis of conditions and diseases where adenosine A 3 receptors play a role are also described.
摘要翻译：本发明提供了对腺苷A 3受体显示高亲和力的新的式（I）化合物。它还提供腺苷A 3受体的调节剂。它还提供用于治疗和/或预防腺苷A 3受体起作用的病症和疾病的化合物。还描述了用于治疗和/或预防腺苷A 3受体起作用的病症和疾病的药物组合物。

3. 发明公开

EP1777219A1 1,2-Substituted naphthalene derivatives with antiglutamatergic properties and uses thereof 审中-公开
标题翻译： 1,2-取代的具有antiglutamatergen性质萘衍生物及其用途
公开(公告)号：EP1777219A1
公开(公告)日：2007-04-25
申请号：EP05292212.7
申请日：2005-10-20
申请人： Faust Pharmaceuticals
发明人： Schann, Stephan , Mayer, Stanislas , Foucher, Laurence
IPC分类号： C07D295/08 , C07D295/12 , C07C211/57 , A61K31/4453 , A61K31/495 , A61K31/5375
CPC分类号： C07D295/088 , C07C237/06 , C07D295/13 , C07D295/135
摘要： The present invention provides new compounds displaying antiglutamatergic properties. It also provides the use of such compounds for the treatment and/or prophylaxis of conditions and diseases linked to abnormalities in glutamatergic transmission. It further provides a pharmaceutical composition for the treatment and/or prophylaxis of acute and chronic neurodegenerative conditions and disorders.

4. 发明公开

EP1604977A1 CIS pyrrolidinyl derivatives and their uses 审中-公开
标题翻译： CIS吡咯烷和及其用途
公开(公告)号：EP1604977A1
公开(公告)日：2005-12-14
申请号：EP04291373.1
申请日：2004-06-02
申请人： Faust Pharmaceuticals
发明人： Schann, Stephan , Acher, Francine
IPC分类号： C07D207/16 , C07D207/48 , A61K31/401 , A61P25/00
CPC分类号： C07D207/48 , C07D207/16 , Y02P20/55
摘要： The present invention provides new cis pyrrolidinyl of the formula (I) or (II)
in which:
R 1 , R 2 or R 3 are hydrogen or a carboxy or amino protecting group; R 4 to R 8 represent hydrogen or an alkyl radical; R 9 represents a (R 10 ) n (-R 11 ) m group wherein R 10 is -CO-, -CS-, -O-,-S-, -SO-, -SO 2 -, -COO-, -CON(C n' H 2n'+1 )-, -N(C n' H 2n'+1 )CO-, -CSN(C n' H 2n'+1 )- ,-N(C n' H 2n'+1 )CS-, -N(C n' H 2n'+1 )-, -(C n' H 2n'+1 )-, aryl, and R 11 is a polar group,
and to their use for the treatment and/or prophylaxis of a condition associated with altered glutamatergic signalling and/or functions, and/or conditions which can be affected by alteration of glutamate level or signalling

5. 发明公开

EP1992637A1 1-Aminocyclopentane-1,3,4- tricarboxylic acids derivatives 审中-公开
标题翻译：衍生冯1-氨基环戊烷-1,3,4-三羧酸
公开(公告)号：EP1992637A1
公开(公告)日：2008-11-19
申请号：EP07290629.0
申请日：2007-05-16
申请人： Faust Pharmaceuticals
发明人： Schann, Stephan , Mayer, Stanislas
IPC分类号： C07K5/06 , C07K1/02 , A61K38/05
CPC分类号： C07K5/06008 , A61K38/00 , C07K1/02 , C07K5/06026 , C07K5/06034 , C07K5/0606 , C07K5/06078
摘要： The invention provides derivatives of 1-aminocyclopentane-1,3,4-tricarboxylic acids which provide a sufficient bioavailability upon oral administration to be conveniently used as medicaments modulating the effect of glutamate.
摘要翻译：本发明提供了在口服给药时提供足够的生物利用度的1-氨基环戊烷-1,3,4-三羧酸的衍生物，以方便地用作调节谷氨酸的作用的药物。

6. 发明公开

EP1604978A1 Trans pyrrolidinyl derivatives and their pharmaceutical uses 审中-公开
标题翻译：跨Pyrrolidinylderivate和它们的药物使用
公开(公告)号：EP1604978A1
公开(公告)日：2005-12-14
申请号：EP04291374.9
申请日：2004-06-02
申请人： Faust Pharmaceuticals
发明人： Schann, Stephan , Acher, Francine
IPC分类号： C07D207/16 , C07D207/48 , A61K31/40
CPC分类号： C07D207/16 , C07D207/48 , Y02P20/55
摘要： The present invention relates to the use of trans pyrrolidinyl of the formula (I) or (II)
in which:
R 1 , R 2 or R 3 are hydrogen or a carboxy or amino protecting group; R 4 to R 8 represent hydrogen or an alkyl radical; R 9 represents a (R 10 ) n (-R 11 ) m group wherein R 10 is -CO-, -CS-, -O-, -S-, -SO-, -SO 2 -, -COO-, -CON(C n' H 2n'+1 )-,-N(C n' H 2n'+1 )CO-, -CSN(C n' H 2n'+1 )-, -N(C n' H 2n'+1 )CS-, -N(C n' H 2n'+1 )-, -(C n' H 2n'+1 )-, aryl, and R 11 is a polar group,
for the treatment and/or prophylaxis of conditions associated with altered glutamatergic signalling and/or functions, and/or conditions which can be affected by alteration of glutamate level or signalling in mammals.

7. 发明公开

EP1462103A1 NO donors, combination products and uses as modulators of neurotransmitter release 审中-公开
标题翻译： NO-Donoren，Kombinationspräparateund Verwendung als Modulatoren der Freisetzung von Neurotransmittern
公开(公告)号：EP1462103A1
公开(公告)日：2004-09-29
申请号：EP04290804.6
申请日：2004-03-25
申请人： Faust Pharmaceuticals
发明人： Schann, Stephan , Neuville, Pascal
IPC分类号： A61K31/403 , A61K31/437 , C07D209/86 , C07D401/04 , A61P25/00
CPC分类号： C07D401/04 , C07D209/86
摘要： The present invention relates to compounds of the general formula (I) or (II):
wherein:

R 1 , R 2 , R 3 , R 4 , R 5 and R 10 are, independently from one another, H or a moiety of the following general formula : -(R 6 ) n -R 7 , with R 6 is an alkyl chain and R 7 is, a moiety selected in the group consisting of -C n' H 2n'+1 , a cycloalkyl moiety, -N(C n' H 2n'+1 )(C n' H 2n'+1 ), -NH-cycloalkyl, -O(C n' H 2n'+1 ), -O-cycloalkyl, =O, =S, -NO 2 , , -I, -Br, -Cl, -F, -CF 3 , -OCF 3 , -COOH, -SO 3 H, -PO 3 H 2 , -CN, A 3 , A 4 , A 8 and A 9 are C, N, O and S, m is 0 to 2, n is 0 to 6, and to their use for the treatment and/or prevention of diseases and conditions mediated by the imbalance of acetylcholine, and for treating and/or preventing glutamate excitotoxicity.
摘要翻译：本发明涉及通式（I）或（II）的化合物：其中：R 1，R 2，R 3，R 4，R 5和R 5， 10>彼此独立地是H或下列通式的部分： - （R 6）n R 7，其中R 6是烷基链，R 7是选择的部分在由-Cn'H2n'+ 1，环烷基部分-N（Cn'H2n'+ 1）（Cn'H2n'+ 1）， - - - - - - - - 环烷基，-O（Cn'H2n'+ 1）组成的组中），-O-环烷基，= O，= S，-NO 2，-I，-Br，-Cl，-F，-CF 3，-OCF 3，-COOH，-SO 3 H，-PO 3 H 2，-CN， A8和A9为C，N，O和S，m为0至2，n为0至6，并且用于治疗和/或预防由乙酰胆碱不平衡介导的疾病和病症，以及用于治疗和/或预防谷氨酸兴奋性毒性。

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