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1. 发明授权

US08030331B2 Allosteric modulators of metabotropic glutamate receptors 失效
标题翻译：代谢型谷氨酸受体的变构调节剂
公开(公告)号：US08030331B2
公开(公告)日：2011-10-04
申请号：US12899542
申请日：2010-10-06
申请人： Anne-Sophie Bessis , Beatrice Bonnet , Emmanuel Le Poul , Jean-Philippe Rocher , Mark Epping-Jordan
发明人： Anne-Sophie Bessis , Beatrice Bonnet , Emmanuel Le Poul , Jean-Philippe Rocher , Mark Epping-Jordan
IPC分类号： A61K31/4523 , C07D401/04
CPC分类号： C07D413/14 , C07D211/18 , C07D211/60 , C07D401/04 , C07D413/04 , C07D417/14
摘要： The present invention relates to new compounds of formula (I) wherein A, B, P, Q, W, R1 and R2 are defined in the description; invention compounds are useful in the prevention or treatment of central nervous system disorders as well as other disorders modulated by mGluR5 receptors.
摘要翻译：本发明涉及式（I）的新化合物，其中A，B，P，Q，W，R 1和R 2在说明书中定义; 本发明化合物可用于预防或治疗中枢神经系统疾病以及由mGluR5受体调节的其它病症。

2. 发明申请

US20090215822A1 Substituted Oxadiazole Derivatives as Positive Allosteric Modulators of Metabotropic Glutamate Receptors 审中-公开
标题翻译：取代的恶二唑衍生物作为代谢型谷氨酸受体的正变构调节剂
公开(公告)号：US20090215822A1
公开(公告)日：2009-08-27
申请号：US11920603
申请日：2006-05-17
申请人： Marco Farina , Stefania Gagliardi , Emmanuel Le Poul , Vincent Mutel , Giovanni Palombi , Sonia-Maria Poli , Jean-Philippe Rocher
发明人： Marco Farina , Stefania Gagliardi , Emmanuel Le Poul , Vincent Mutel , Giovanni Palombi , Sonia-Maria Poli , Jean-Philippe Rocher
IPC分类号： A61K31/4545 , C07D413/04 , A61K31/454 , C07D413/14 , A61P25/18
CPC分类号： C07D413/04 , C07D413/14 , C07D417/14
摘要： The present invention relates to new compounds which are Oxadiazole derivatives of formula (I) wherein B, P, Q, W, R1 and R2 are defined in the description. Invention compounds are useful in the prevention or treatment of central or peripheral nervous system disorders as well as other disorders modulated by mGluR5 receptors.(I).
摘要翻译：本发明涉及新的化合物，其是式（I）的恶二唑衍生物，其中B，P，Q，W，R 1和R 2在说明书中定义。本发明化合物可用于预防或治疗中枢或周围神经系统疾病以及由mGluR5受体调节的其它障碍。（I）。

3. 发明申请

US20090082399A1 Carbamate derivatives as positive allosteric modulators of metabotropic glutamate receptors 审中-公开
标题翻译：氨基甲酸酯衍生物作为代谢型谷氨酸受体的正变构调节剂
公开(公告)号：US20090082399A1
公开(公告)日：2009-03-26
申请号：US11920616
申请日：2006-05-17
申请人： Piergiuliano Bugada , Stefania Gagliardi , Giovanni Palombi , Jean-Philippe Rocher
发明人： Piergiuliano Bugada , Stefania Gagliardi , Giovanni Palombi , Jean-Philippe Rocher
IPC分类号： A61K31/4545 , C07D211/42 , C07D401/12 , A61K31/40 , C07D207/12 , A61K31/445
CPC分类号： C07D295/192 , C07D207/12 , C07D211/42 , C07D211/56 , C07D401/12
摘要： The present invention relates to new compounds which are Carbamate derivatives of formula I wherein X, B, P, Q5W, R1 and R2 are defined in the description. Invention compounds are useful for treating CNS or PNS disorders which are affected by the neuromodulatory effect of mGluR5 positive allosteric modulators such as cognitive decline and also to treat both positive and negative symptoms in schizophrenia
摘要翻译：本发明涉及新的化合物，它们是式I的氨基甲酸酯衍生物，其中X，B，P，Q5W，R 1和R 2在说明书中定义。本发明化合物可用于治疗受到认知衰退的mGluR5阳性变构调节剂的神经调节作用影响的CNS或PNS病症，并且也用于治疗精神分裂症中的阳性和阴性症状

4. 发明申请

US20080287466A1 4-AMINO-2,3-DISUBSTITUTED THIENO [2,3,D]PYRIMIDINES AND PHARMACEUTICAL COMPOSITIONS THEREOF 审中-公开
标题翻译： 4-氨基-2,3-取代的噻吩并[2,3，D]嘧啶和其药物组合物
公开(公告)号：US20080287466A1
公开(公告)日：2008-11-20
申请号：US12169800
申请日：2008-07-09
申请人： Jerry Leroy Adams , Deborah Lynne Bryan , Yanhong Feng , Shinichiro Matsunaga , Yutaka Maeda , Yasushi Miyazaki , Masato Nakano , Jean-Philippe Rocher , Hideyuki Sato , Marcus Semones , Domingos J. Silva , Jun Tang
发明人： Jerry Leroy Adams , Deborah Lynne Bryan , Yanhong Feng , Shinichiro Matsunaga , Yutaka Maeda , Yasushi Miyazaki , Masato Nakano , Jean-Philippe Rocher , Hideyuki Sato , Marcus Semones , Domingos J. Silva , Jun Tang
IPC分类号： A61K31/519 , C07D491/04 , A61P43/00
CPC分类号： C07D491/04 , C07D495/04
摘要： Furo- and thienopyrimidine derivatives, which are useful as TIE-2 and/or VEGFR-2 inhibitors are described herein. The described invention also includes methods of making such furo- and thienopyrimidine derivatives as well as methods of using the same in the treatment of hyperproliferative diseases.
摘要翻译：本文描述了可用作TIE-2和/或VEGFR-2抑制剂的呋喃和噻吩并嘧啶衍生物。所述的发明还包括制备这些呋喃并噻吩并嘧啶衍生物的方法以及使用它们在治疗过度增殖性疾病中的方法。

5. 发明申请

US20050004142A1 Chemical compounds 失效
标题翻译：化合物
公开(公告)号：US20050004142A1
公开(公告)日：2005-01-06
申请号：US10489052
申请日：2002-09-10
申请人： Jerry Adams , Deborah Bryan , Yanhong Feng , Shinichiro Matsunaga , Yutaka Maeda , Yasushi Miyazaki , Masato Nakano , Jean-Philippe Rocher , Hideyuki Sato , Marcus Semones , Domingos Silva , Jun Tang
发明人： Jerry Adams , Deborah Bryan , Yanhong Feng , Shinichiro Matsunaga , Yutaka Maeda , Yasushi Miyazaki , Masato Nakano , Jean-Philippe Rocher , Hideyuki Sato , Marcus Semones , Domingos Silva , Jun Tang
IPC分类号： C07D491/048 , A61K31/519 , A61K31/5377 , A61K45/00 , A61P1/16 , A61P3/10 , A61P7/02 , A61P9/00 , A61P9/10 , A61P13/12 , A61P17/02 , A61P17/06 , A61P19/02 , A61P25/28 , A61P29/00 , A61P35/00 , A61P37/06 , A61P43/00 , C07D491/04 , C07D495/04 , C07D519/00 , C07D491/02
CPC分类号： C07D491/04 , C07D495/04
摘要： Furo- and thienopyrimidine derivatives, which are useful as TIE-2 and/or VEGFR-2 inhibitors are described herein. The described invention also includes methods of making such furo- and thienopyrimidine derivatives as well as methods of using the same in the treatment of hyperproliferative diseases.
摘要翻译：本文描述了可用作TIE-2和/或VEGFR-2抑制剂的呋喃和噻吩并嘧啶衍生物。所述的发明还包括制备这些呋喃并噻吩并嘧啶衍生物的方法以及使用它们在治疗过度增殖性疾病中的方法。

6. 发明授权

US5446059A Benzimidazole-derived compounds, method for preparing the same, and therapeutical and cosmetic uses thereof 失效
标题翻译：衍生自苯并咪唑的化合物，其制备方法及其治疗和美容用途
公开(公告)号：US5446059A
公开(公告)日：1995-08-29
申请号：US142464
申请日：1994-01-10
申请人： Jean-Philippe Rocher , Daniel Cavey
发明人： Jean-Philippe Rocher , Daniel Cavey
IPC分类号： A61K8/49 , A61K8/00 , A61K8/11 , A61K31/415 , A61K31/4184 , A61P29/00 , A61P37/08 , A61Q17/00 , A61Q19/00 , A61Q19/10 , C07D235/12 , C07D235/18 , C07F9/6506
CPC分类号： C07F9/65068 , A61K8/4946 , A61Q19/00 , C07D235/18
摘要： Benzimidazole derivatives having general formula (I), wherein R.sub.1 and R.sub.2 are a hydrogen atom, a lower alkyl radical, an OR.sub.4 radical, a lower fluoroalkyl radical or a halogen atom; R.sub.3 is a hydrogen atom, a lower alkyl radical, a halogen, a hydroxyl or a lower alkoxy radical having 1-6 carbon atoms; R.sub.4 is a hydrogen atom, a lower alkyl radical, a benzyl radical or a (II) radical, PO.sub.3 H, SO.sub.3 H or an aminoacid residue; R.sub.7 is a lower alkyl radical, a lower alkoxy radical having 1-6 carbon atoms, a --(CH.sub.2).sub.n --COOH radical where n=1-6, or the radical (III), where r' and r" are a hydrogen atom or a lower alkyl radical, or form, together with the nitrogen atom, a 5 or 6-membered heterocyclic ring optionally interrupted by a heteroatom; R.sub.5 and R.sub.6 are different and represent the OR.sub.8 radical or a mono or polycyclic cycloalkyl radical having 5-12 carbon atoms bound to the phenyl core by a tertiary carbon; R.sub.8 is a hydrogen atom, a lower alkyl radical, an acyl radical having 2-7 carbon atoms, a benzyl radical optionally substituted by one or more halogen atoms, or a benzoyl radical; and salts of said compounds obtained by adding a pharmaceutically acceptable acid or base. Said compounds may be used therapeutically, in particular in relation to inflammatory and/or immunoallergic conditions, and cosmetically to provide body and hair care.
摘要翻译： PCT No.PCT / FR92 / 00482 Sec。 371日期1994年1月10日 102（e）日期1994年1月10日PCT提交1992年5月29日PCT公布。 WO92 / 21663 PCT出版物 1992年12月10日授权。具有通式（I）的苯并咪唑衍生物，其中R1和R2为氢原子，低级烷基，OR4基，低级氟代烷基或卤素原子。 R3是氢原子，低级烷基，卤素，羟基或具有1-6个碳原子的低级烷氧基; R4是氢原子，低级烷基，苄基或（Ⅱ）基，PO3H，SO3H或氨基酸残基; R7是低级烷基，具有1-6个碳原子的低级烷氧基，其中n = 1-6的 - （CH2）n-COOH基团或基团（III），其中r'和r“是氢原子或低级烷基，或与氮原子一起形成任选被杂原子间隔的5或6元杂环; R5和R6不同，代表OR8基团或具有5-12个碳原子的单或多环环烷基，其通过叔碳与苯基键合; R8是氢原子，低级烷基，具有2-7个碳原子的酰基，任选被一个或多个卤素原子取代的苄基或苯甲酰基; 和通过加入药学上可接受的酸或碱获得的所述化合物的盐。所述化合物可以在治疗上，特别是关于炎性和/或免疫过敏性病症，以及美容方面用于提供身体和头发护理。

7. 发明授权

US08101637B2 Alkynyl derivatives as modulators of metatropic glutamate receptors 有权
标题翻译：炔基衍生物作为适应性谷氨酸受体的调节剂
公开(公告)号：US08101637B2
公开(公告)日：2012-01-24
申请号：US11630013
申请日：2005-06-17
申请人： Anne-Sophie Bessis , Christelle Bolea , Béatrice Bonnet , Mark Epping-Jordan , Nicholas Poirier , Sonia-Maria Poli , Jean-Philippe Rocher , Yves Thollon
发明人： Anne-Sophie Bessis , Christelle Bolea , Béatrice Bonnet , Mark Epping-Jordan , Nicholas Poirier , Sonia-Maria Poli , Jean-Philippe Rocher , Yves Thollon
IPC分类号： A61K31/4439 , A61K31/4188 , C07D401/06 , C07D235/02
CPC分类号： C07D471/04 , C07D213/56 , C07D215/06 , C07D233/56 , C07D239/26 , C07D263/56 , C07D277/22 , C07D401/06 , C07D403/06 , C07D413/06 , C07D417/06
摘要： The present invention relates to novel compounds of formula (I) wherein W, n, X and W′ are defined in the description; invention compounds are modulators of metabotropic glutamate receptors-subtype 5 (“mGluR5”) which are useful for the treatment of central nervous system disorders as well as other disorders modulated by mGluR5 receptors.
摘要翻译：本发明涉及式（I）的新化合物，其中W，n，X和W'在说明书中定义; 发明化合物是代谢型谷氨酸受体的调节剂 - 亚型5（“mGluR5”），其可用于治疗中枢神经系统疾病以及由mGluR5受体调节的其它病症。

8. 发明申请

US20110112143A1 ALLOSTERIC MODULATORS OF METABOTROPIC GLUTAMATE RECEPTORS 失效
标题翻译：代谢型谷氨酸受体的独立调节剂
公开(公告)号：US20110112143A1
公开(公告)日：2011-05-12
申请号：US12899542
申请日：2010-10-06
申请人： Anne-Sophie Bessis , Beatrice Bonnet , Emmanuel Le Poul , Jean-Philippe Rocher , Mark Epping-Jordan
发明人： Anne-Sophie Bessis , Beatrice Bonnet , Emmanuel Le Poul , Jean-Philippe Rocher , Mark Epping-Jordan
IPC分类号： A61K31/4545 , C07D413/14 , A61P25/18
CPC分类号： C07D413/14 , C07D211/18 , C07D211/60 , C07D401/04 , C07D413/04 , C07D417/14
摘要： The present invention relates to new compounds of formula (I) wherein A, B, P, Q, W, R1 and R2 are defined in the description; invention compounds are useful in the prevention or treatment of central nervous system disorders as well as other disorders modulated by mGluR5 receptors.
摘要翻译：本发明涉及式（I）的新化合物，其中A，B，P，Q，W，R 1和R 2在说明书中定义; 本发明化合物可用于预防或治疗中枢神经系统疾病以及由mGluR5受体调节的其它病症。

9. 发明授权

US07834035B2 Allosteric modulators of metabotropic glutamate receptors 失效
标题翻译：代谢型谷氨酸受体的变构调节剂
公开(公告)号：US07834035B2
公开(公告)日：2010-11-16
申请号：US10578589
申请日：2004-11-04
申请人： Anne-Sophie Bessis , Beatrice Bonnet , Emmanuel Le Poul , Jean-Philippe Rocher , Mark Epping-Jordan
发明人： Anne-Sophie Bessis , Beatrice Bonnet , Emmanuel Le Poul , Jean-Philippe Rocher , Mark Epping-Jordan
IPC分类号： A61K31/4523 , C07D401/04
CPC分类号： C07D413/14 , C07D211/18 , C07D211/60 , C07D401/04 , C07D413/04 , C07D417/14
摘要： The present invention relates to new compounds of formula (I) wherein A, B, P, Q, W, R1 and R2 are defined in the description; invention compounds are useful in the prevention or treatment of central nervous system disorders as well as other disorders modulated by mGluR5 receptors.
摘要翻译：本发明涉及式（I）的新化合物，其中A，B，P，Q，W，R 1和R 2在说明书中定义; 本发明化合物可用于预防或治疗中枢神经系统疾病以及由mGluR5受体调节的其它病症。

10. 发明申请

US20100081690A1 OXAZOLE DERIVATIVES AS POSITIVE ALLOSTERIC MODULATORS OF METABOTROPIC GLUTAMATE RECEPTORS 审中-公开
标题翻译：奥沙唑衍生物作为代谢性谷氨酸受体的阳性调节因子
公开(公告)号：US20100081690A1
公开(公告)日：2010-04-01
申请号：US12513907
申请日：2007-11-07
申请人： Emmanuel Le Poul , Giovanni Palombi , Jean-Philippe Rocher
发明人： Emmanuel Le Poul , Giovanni Palombi , Jean-Philippe Rocher
IPC分类号： A61K31/4545 , C07D413/14 , C07D413/04 , A61K31/454 , A61P25/00
CPC分类号： C07D413/14 , C07D413/04
摘要： The present invention provides new compounds of formula I, wherein P, A, W, B, Q, R1 and R2 are defined as in formula I; invention compounds are positive allosteric modulators of metabotropic receptors—subtype 5 (“mGluR5”) which are useful for the treatment or prevention of central nervous system disorders such as for example: cognitive decline, both positive and negative symptoms in schizophrenia as well as other disorders in which the mGluR5 subtype of glutamate metabotropic receptor is involved.
摘要翻译：本发明提供了新的式I化合物，其中P，A，W，B，Q，R 1和R 2如式I中所定义; 本发明化合物是代谢型受体 - 亚型5（“mGluR5”）的正性变构调节剂，其可用于治疗或预防中枢神经系统疾病，例如：认知衰退，精神分裂症中的阳性和阴性症状以及其他疾病其中涉及mGluR5亚型的谷氨酸代谢代谢受体。

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