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1. 发明公开

EP3693370A1 CRYTALLINE MONO-PHOSPHATE SALT OF 6-FLUORO-2-[4-(PYRIDIN-2-YL)BUT-3-YN-1-YL] IMIDAZO[1,2A]PYRIDINE AS NEGATIVE ALLOSTERIC MODULATOR OF MGLU5 RECEPTOR 审中-公开
公开(公告)号：EP3693370A1
公开(公告)日：2020-08-12
申请号：EP20166777.1
申请日：2014-09-25
申请人： Addex Pharma S.A
发明人： BONNET, Béatrice , POLI, Sonia Maria
IPC分类号： C07D471/04 , A61P25/28 , A61K31/4184
摘要： The present invention relates to crystalline and amorphous forms of 6-fluoro-2-[4-(pyridin-2-yl)but-3-yn-1-yl]imidazo[1,2-a]pyridine mono-phosphate salt and methods of making these solid forms thereof. The invention compounds are modulators of mGlu 5 which are useful for the treatment or prevention of central nervous system disorders as well as other disorders modulated by mGlu 5 receptors. The invention is also directed to pharmaceutical compositions and the use of such compounds in the manufacture of medicaments, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGlu 5 is involved.

2. 发明公开

EP2134690A1 1,4-DISUBSTITUTED 3-CYANO-PYRIDONE DERIVATIVES AND THEIR USE AS POSITIVE MGLUR2 -RECEPTOR MODULATORS 有权
标题翻译： 1,4-二取代的3- CYANOPYRIDONDERIVATE及其作为正调节受体的mGluR2
公开(公告)号：EP2134690A1
公开(公告)日：2009-12-23
申请号：EP08717514.7
申请日：2008-03-07
申请人： Ortho-McNeil-Janssen Pharmaceuticals, Inc. , ADDEX Pharma S.A.
发明人： CID-NÚÑEZ, José, Maria , TRABANCO-SUÁREZ, Andrés, Avelino , MACDONALD, Gregor, James , DUVEY, Guillaume, Albert, Jacques , LÜTJENS, Robert, Johannes
IPC分类号： C07D213/85 , C07D401/04 , A61K31/4412 , A61K31/4418 , C07D409/04 , A61K31/443 , A61K31/4436 , A61K31/4439 , A61K31/444 , A61P25/22 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D405/06
CPC分类号： C07D213/85 , A61K31/198 , A61K31/444
摘要： The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I) including any stereochemically isomeric form thereof, or a pharmaceutically acceptable salt thereof or a solvate thereof, wherein all radicals are defined in the application and claims. The compounds according to the invention are positive allosteric modulators of metabotropic glutamate receptors subtype 2 ('mGluR2' ) which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety,schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions and processes to prepare such compounds and such compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved.

3. 发明公开

EP2089386A2 OXAZOLE DERIVATIVES AS POSITIVE ALLOSTERIC MODULATORS OF METABOTROPIC GLUTAMATE RECEPTORS 有权
标题翻译：恶唑，正变构调节代谢型谷氨酸受体
公开(公告)号：EP2089386A2
公开(公告)日：2009-08-19
申请号：EP07859227.6
申请日：2007-11-07
申请人： ADDEX Pharma S.A.
发明人： LE POUL, Emmanuel , PALOMBI, Giovanni , ROCHER, Jean-Philippe
IPC分类号： C07D413/14 , A61K31/422 , A61P25/00
CPC分类号： C07D413/14 , C07D413/04
摘要： The present invention provides new compounds of formula (I), wherein P3A, W, B, Q, Rl 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.

4. 发明公开

EP2593277A2 NOVEL FUSED PYRAZOLE DERIVATIVES AND THEIR USE AS ALLOSTERIC MODULATORS OF METABOTROPIC GLUTAMATE RECEPTORS 审中-公开
标题翻译：新的稠吡唑衍生物及其作为变构调节代谢型谷氨酸受体
公开(公告)号：EP2593277A2
公开(公告)日：2013-05-22
申请号：EP11807174.5
申请日：2011-07-11
申请人： ADDEX Pharma S.A. , Merck Sharp & Dohme Corp.
发明人： BOLEA,Christelle , CELANIRE, Sylvain , TANG, Lam , JONES, Philip , LIVERTON, Nigel J. , SOLL, Richard , DONG, Jinchao , LEI, Zhiyu , LIU, Fuquing , KONG, Yanling , JU, Yi , ZHANG, Haoyong , WEI, Jieping , WEI, Qaioxin , ZHANG, Mingxiang , LUO, Yunfu
IPC分类号： B26B5/00
CPC分类号： C07D513/12 , A23L27/2056 , A23L33/10 , A23V2002/00 , A61K9/0019 , A61K9/0095 , A61K9/06 , A61K9/10 , A61K9/2059 , A61K31/429 , A61K31/433 , A61K31/4439 , A61K31/506 , A61K31/55 , A61K45/06 , C07D513/04 , C07D513/14 , A61K2300/00 , A23V2200/16 , A23V2200/322 , A23V2200/328
摘要： The present invention relates to novel compounds of Formula (I), wherein M, A and Y are defined as in Formula (I); invention compounds are modulators of metabotropic glutamate receptors - subtype 4 ("mGluR
4 ") which are useful for the treatment or prevention of central nervous system disorders as well as other disorders modulated by mGluR
4 receptors. The invention is also directed to pharmaceutical compositions and the use of such compounds in the manufacture of medicaments, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR
4 is involved.

5. 发明授权

EP2205565B1 1,3-DISUBSTITUTED-4-PHENYL-1 H-PYRIDIN-2-ONES 有权
标题翻译： 1,3-DISUBSTITUIERTE 4-（苯基）-1H-吡啶-2-酮
公开(公告)号：EP2205565B1
公开(公告)日：2013-04-17
申请号：EP08802104.3
申请日：2008-09-12
申请人： Janssen Pharmaceuticals, Inc. , ADDEX Pharma S.A.
发明人： CID-NUNEZ, José Maria , TRABANCO-SUAREZ, Andrés, Avelino , MACDONALD, Gregor, James , DUVEY, Guillaume, Albert, Jacques , LÜTJENS, Robert, Johannes , FINN, Terry, Patrick
IPC分类号： C07D213/64 , C07D405/12 , C07D405/14 , A61K31/47
CPC分类号： C07D405/12 , C07D213/64 , C07D405/14

6. 发明公开

EP2220083A2 IMIDAZO[1,2-A]PYRIDINE DERIVATIVES AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS 有权
标题翻译： IMIDAZO [1,2-A] - 吡啶衍生物在IHRE VERWENDUNG ALS POSITIVE ALLOSTERISCHE MODULATOREN VON MGLUR2-REZEPTOREN
公开(公告)号：EP2220083A2
公开(公告)日：2010-08-25
申请号：EP08850488.1
申请日：2008-11-12
申请人： Ortho-McNeil-Janssen Pharmaceuticals, Inc. , ADDEX Pharma S.A.
发明人： TRABANCO-SUAREZ, Andrés, Avelino , TRESADERN, Gary, John , VEGA RAMIRO, Juan, Antonio , CID-NUNEZ, Jose, Maria
IPC分类号： C07D471/04 , C07D519/00 , A61K31/437 , A61P25/00
CPC分类号： C07D471/04 , C07D519/00
摘要： The present invention relates to novel compounds, in particular novel imidazo[1,2- a]piridine derivatives according to Formula (I). The compounds according to the invention are positive allosteric modulators of metabotropic receptors- subtype 2 ('mGluR2') which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions and processes to prepare such compounds and compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved.
摘要翻译：本发明涉及新的化合物，特别是根据式（I）的新型咪唑并[1,2-a]吡啶衍生物。根据本发明的化合物是代谢型受体 - 亚型2（'mGluR2'）的正性变构调节剂，其可用于治疗或预防与谷氨酸功能障碍相关的神经和精神障碍以及代谢代谢受体的mGluR2亚型的疾病参与。特别地，这些疾病是选自焦虑，精神分裂症，偏头痛，抑郁症和癫痫的中枢神经系统疾病。本发明还涉及制备这些化合物和组合物的药物组合物和方法，以及这些化合物用于预防和治疗其中涉及mGluR2的疾病的用途。

7. 发明公开

EP2205565A1 1,3-DISUBSTITUTED-4-PHENYL-1 H-PYRIDIN-2-ONES 有权
标题翻译： 1,3-二取代的4-（苯基）-1H-吡啶-2-酮
公开(公告)号：EP2205565A1
公开(公告)日：2010-07-14
申请号：EP08802104.3
申请日：2008-09-12
申请人： Ortho-McNeil-Janssen Pharmaceuticals, Inc. , ADDEX Pharma S.A.
发明人： CID-NUNEZ, José Maria , TRABANCO-SUAREZ, Andrés, Avelino , MacDONALD, Gregor, James , DUVEY, Guillaume, Albert, Jacques , LÜTJENS, Robert, Johannes , FINN, Terry, Patrick
IPC分类号： C07D213/64 , C07D405/12 , C07D405/14 , A61K31/47
CPC分类号： C07D405/12 , C07D213/64 , C07D405/14
摘要： The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I) wherein all radicals are as defined in the application and claims. The compounds according to the invention are positive allosteric modulators of metabotropic receptors - subtype 2 ('mGluR2') which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions and processes to prepare such compounds and compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved.

8. 发明公开

EP2134708A1 3-CYANO-4-(4-TETRAHYDROPYRAN-PHENYL)-PYRIDIN-2-ONE DERIVATIVES 有权
标题翻译： 3-氰基-4-（4-四氢吡喃 - 苯基） - 吡啶-2-酮衍生物
公开(公告)号：EP2134708A1
公开(公告)日：2009-12-23
申请号：EP08717515.4
申请日：2008-03-07
申请人： Ortho-McNeil-Janssen Pharmaceuticals, Inc. , ADDEX Pharma S.A.
发明人： CID-NÚÑEZ, José, Maria , TRABANCO-SUÁREZ, Andrés, Avelino , MACDONALD, Gregor, James , DUVEY, Guillaume, Albert, Jacques
IPC分类号： C07D405/12 , A61K31/4545 , A61P25/28
CPC分类号： C07D405/12
摘要： The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I) including any stereochemically isomeric form thereof, or a pharmaceutically acceptable salt thereof or a solvate thereof, wherein all radicals are defined in the application and claims. The compounds according to the invention are positive allosteric modulators of metabotropic glutamate receptors subtype 2 ( mGluR2 ) which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are centralnervous system disorders selected from the group of anxiety,schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions and processes to prepare such compounds and such compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved.
摘要翻译：本发明涉及新化合物，特别是式（I）的新型吡啶酮衍生物，包括其立体化学异构形式，或其药学上可接受的盐或其溶剂化物，其中所有基团在本申请和权利要求书中定义。本发明的化合物是代谢型谷氨酸受体亚型2（mGluR2）的正性变构调节剂，其可用于治疗或预防与谷氨酸功能障碍相关的神经和精神疾病以及涉及代谢型受体的mGluR2亚型的疾病。特别是，这些疾病是选自焦虑症，精神分裂症，偏头痛，抑郁症和癫痫症的中枢神经系统疾病。本发明还涉及制备这些化合物和这种组合物的药物组合物和方法，以及涉及这些化合物用于预防和治疗其中涉及mGluR2的疾病的用途。

9. 发明公开

EP2104670A2 NOVEL TRIAZINEDIONE DERIVATIVES AS GABA-B RECEPTOR MODULATORS 有权转让
标题翻译： NEW三嗪二酮衍生物作为GABA-B受体调节剂
公开(公告)号：EP2104670A2
公开(公告)日：2009-09-30
申请号：EP07825747.4
申请日：2007-11-09
申请人： Addex Pharma SA
发明人： RIGUET, Eric , CAMPO, Brice , GIBELIN, Antoine , MHALLA, Karim
IPC分类号： C07D401/06 , C07D403/06 , C07D403/10 , C07D405/06 , C07D405/10 , C07D409/06 , C07D413/06 , C07D413/10 , C07D417/06 , C07D417/12 , C07D491/04 , C07D253/075 , A61K31/53 , A61P35/00
CPC分类号： C07D253/075 , C07D401/06 , C07D403/06 , C07D403/10 , C07D405/06 , C07D405/10 , C07D409/06 , C07D413/06 , C07D413/10 , C07D417/06 , C07D417/12 , C07D491/04
摘要： The present invention provides novel compounds of formula (I) wherein W1, W2, W3, W4, W5, B, X1, X2, X3, X4, X5, E and L are as defined herein; invention compounds are gamma amino butyrique acid receptor-subtype B ('GABAB') positive allosteric modulators (enhancers), which are useful to provide methods of treating or preventing diseases or disorders, including treatment of anxiety, depression, epilepsy, schizophrenia, cognitive disorders, spasticity and skeletal muscle rigidity, spinal cord injury, multiple sclerosis, amyotrophic lateral sclerosis, cerebral palsy, neuropathic pain and craving associated with cocaine and nicotine, panic disorder, posttraumatic stress disorders, urge urinary incontinence, gastroesophageal reflux disease, transient lower oesophageal sphincter relaxations, functional gastrointestinal disorders and irritable bowel syndrome.

10. 发明公开

EP2030970A1 Allosteric modulators of metabotropic glutamate receptors 有权
标题翻译： Allosterische Modulatoren von metabotropen Glutamatrezeptoren
公开(公告)号：EP2030970A1
公开(公告)日：2009-03-04
申请号：EP08017193.7
申请日：2004-11-04
申请人： ADDEX Pharma S.A.
发明人： Bessis, Anne-Sophie , Bonnet, Beatrice , Le Poul, Emmanuel , Rocher, Jean-Philippe , Epping-Jordan, Mark
IPC分类号： C07D211/18 , C07D211/60 , C07D401/04 , C07D413/04 , C07D413/14 , C07D417/14 , A61K31/443 , A61K31/4436 , A61K31/4439 , A61P25/28 , 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, R 1 and R 2 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。

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