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1. 发明申请

WO2012006760A1 TRICYCLIC COMPOUNDS AS ALLOSTERIC MODULATORS OF METABOTROPIC GLUTAMATE RECEPTORS 审中-公开
标题翻译：作为代谢谷氨酸盐受体的独立调节剂的三聚体化合物
公开(公告)号：WO2012006760A1
公开(公告)日：2012-01-19
申请号：PCT/CN2010/001062
申请日：2010-07-14
申请人： MERCK SHARP & DOHME CORP. , ADDEX PHARMA SA , LIVERTON, Nigel, J. , BOLÉA, Christelle , CELANIRE, Sylvain , LUO, Yunfu
发明人： LIVERTON, Nigel, J. , BOLÉA, Christelle , CELANIRE, Sylvain , LUO, Yunfu
IPC分类号： C07D513/04 , C07D513/14 , C07D515/14 , A61K31/506 , A61K31/554 , A61P25/00
CPC分类号： A61K31/506 , A61K31/133 , A61K31/135 , A61K31/192 , A61K31/554 , A61K45/06 , C07D513/04 , C07D513/10 , C07D513/14 , A61K2300/00
摘要： The present invention describes and claims compounds of the Structural Formula (I), Structural Formula (II), or Structural Formula (III). In Formula (I), R 1 , R 2 , R 3 and R 3' are -H or methyl, or R 3 and R 3' taken together form a double bond, or R 3' is -H and R 2 and R 3 taken together form a spiro-cyclopropyl substituent, R 4 is -H or -F, and R 5 is -H, methyl, -Cl or -Br. In Formula (II), R 1 is -H, ethyl-, isopropyl-, cyclopropyl-, methyl- or methoxy-, R 4 is -H or -F, and "Y" is: (a) -CH 2 -; (b) -CR 6 H-O-CR 7 R 8 -, wherein R 6 , R 7 , and R 8 are independently -H or methyl; (c) -CR 6 H-N(R 9 )-CR 7 R 8 -, wherein R 6 , R 7 , and R 8 are independently -H or methyl; (d) -CH 2 -C(R 9 )(R 10 )-C(R 7 )(R 8 )-, wherein R 7 , R 8 , R 9 and R 10 are independently -H or -methyl, or both R 7 and R 8 are -F, R 9 and R 10 are independently -H or -methyl, or both R 9 and R 10 are -F, or R 9 and R 10 taken together are (O=), which together with the carbon to which they are attached forms a carbonyl group.
摘要翻译：本发明描述并要求结构式（I），结构式（II）或结构式（III）的化合物。在式（I）中，R 1，R 2，R 3和R 3'是-H或甲基，或者R 3和R 3'一起形成双键，或者R 3'是-H，并且R 2和R 3一起形成螺环丙基取代基，R4是-H或-F，R5是-H，甲基，-Cl或-Br。在式（II）中，R 1是-H，乙基 - ，异丙基 - ，环丙基 - ，甲基 - 或甲氧基 - ，R 4是-H或-F，“Y”是：（a）-CH 2 - （b）-CR 6 H-O-CR 7 R 8 - ，其中R 6，R 7和R 8独立地为-H或甲基; （c）-CR 6 H-N（R 9）-CR 7 R 8 - ，其中R 6，R 7和R 8独立地为-H或甲基; （d）-CH 2 -C（R 9）（R 10）-C（R 7）（R 8） - ，其中R 7，R 8，R 9和R 10独立地为-H或 - 甲基，或者R 7和R 8均为-F，R 9和 R 10独立地是-H或 - 甲基，或者R 9和R 10都是-F，或者R 9和R 10一起是（O =），它们与它们所连接的碳一起形成羰基。

2. 发明申请

WO2012009000A2 NOVEL FUSED PYRAZOLE DERIVATIVES AND THEIR USE AS ALLOSTERIC MODULATORS OF METABOTROPIC GLUTAMATE RECEPTORS 审中-公开
标题翻译：新型掺杂的吡唑衍生物及其作为代谢谷氨酸受体的独立调节剂
公开(公告)号：WO2012009000A2
公开(公告)日：2012-01-19
申请号：PCT/US2011/001206
申请日：2011-07-11
申请人： ADDEX PHARMA S.A. , MERCK SHARP & DOHME CORP. , 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
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.
摘要翻译：本发明涉及新的式（I）化合物，其中M，A和Y如式（I）所定义; 本发明化合物是代谢型谷氨酸受体的调节剂 - 亚型4（“mGluR4”），其可用于治疗或预防中枢神经系统疾病以及由mGluR4受体调节的其它病症。本发明还涉及药物组合物和这些化合物在制备药物中的用途，以及这些化合物用于预防和治疗涉及mGluR4的疾病的用途。

3. 发明申请

WO2012009001A2 NOVEL TETRAHYDROPYRAZOLO[3,4-B]AZEPINE DERIVATIVES AND THEIR USE AS ALLOSTERIC MODULATORS OF METABOTROPIC GLUTAMATE RECEPTORS 审中-公开
标题翻译：新型四氢吡唑并[3,4-B]氮杂卓衍生物及其作为代谢型谷氨酸受体的调节剂的用途
公开(公告)号：WO2012009001A2
公开(公告)日：2012-01-19
申请号：PCT/US2011/001207
申请日：2011-07-11
申请人： ADDEX PHARMA S.A. , JONES, Philip , MERCK SHARP & DOHME CORP. , TANG, Lam , BOLEA, Christelle , CELANIRE, Sylvain , LIVERTON, Nigel, J.
发明人： JONES, Philip , TANG, Lam , BOLEA, Christelle , CELANIRE, Sylvain , LIVERTON, Nigel, J.
IPC分类号： C07D513/02
CPC分类号： C07D513/12 , A23L5/00 , A61B5/00 , 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
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.
摘要翻译：本发明涉及式（I）的新化合物，其中M，A和Y如式（I）中所定义; 本发明化合物是代谢型谷氨酸受体 - 亚型4（“mGluR 4”）的调节剂，其可用于治疗或预防中枢神经系统病症以及由mGluR调节的其它病症， 4受体。本发明还涉及药物组合物和这些化合物在制备药物中的用途，以及涉及这些化合物用于预防和治疗其中涉及mGluR4的疾病的用途

4. 发明申请

WO2012008999A2 TRICYCLIC COMPOUNDS AS ALLOSTERIC MODULATORS OF METABOTROPIC GLUTAMATE RECEPTORS 审中-公开
标题翻译：作为代谢谷氨酸盐受体的独立调节剂的三聚体化合物
公开(公告)号：WO2012008999A2
公开(公告)日：2012-01-19
申请号：PCT/US2011/001201
申请日：2011-07-09
申请人： MERCK SHARP & DOHME CORP. , ADDEX PHARMA S.A. , LIVERTON, Nigel, J. , BOLEA, Christelle , CELANIRE, Sylvain , YUNFU, Luo
发明人： LIVERTON, Nigel, J. , BOLEA, Christelle , CELANIRE, Sylvain , YUNFU, Luo
IPC分类号： C07D513/02
CPC分类号： C07D513/04 , A61K31/433 , A61K31/506 , A61K31/55 , A61K45/06 , C07D513/14
摘要： The present invention describes and claims compounds of the Structural Formula I, Structural Formula II, or Structural Formula III: wherein R 1 , R 2 , R 3 and R 3' are -H or methyl, or R 3 and R 3 taken together form a double bond, or R 3' is -H and R 2 and R 3 taken together form a spiro-cyclopropyl substituent, R 4 is -H or -F, and R5 is -H, methyl, -CI or -Br, Formula II wherein R 1 is -H, ethyl-, isopropyl-, cyclopropyl-, methyl- or methoxy-, R 4 is -H or -F, and "Y" is: (a) -CH 2 -; (b) -CR 6 H-0-CR 7 R 8 -, wherein R 6 , R 7 , and R 8 are independently - H or methyl; (c) -CR 6 H-N(R 9 )-CR 7 R 8 -, wherein R 6 , R 7 , and R 8 are independently -H or methyl; (d) -CH 2 -C(R 9 )(R 10 )-C(R 7 )(R 8 )-, wherein R 7 , R 8 , R 9 and R 10 are independently - H or -methyl, or both R 7 and R 8 are -F, R 9 and R 10 are independently -H or -methyl, or both R 9 and R 10 are -F, or R 9 and R 10 taken together are (0=), which together with the carbon to which they are attached forms a carbonyl group.
摘要翻译：本发明描述并要求结构式I，结构式II或结构式III的化合物：其中R1，R2，R3和R3'是-H或甲基，或R3和R3一起形成双键，或R3 '是-H并且R 2和R 3一起形成螺环丙基取代基，R 4是-H或-F，R 5是-H，甲基，-C 1或-Br，其中R 1是-H，乙基 - ， - 异丙基 - ，环丙基 - ，甲基或甲氧基 - ，R 4为-H或-F，“Y”为：（a）-CH 2 - ; （b）-CR6H-0-CR7R8-，其中R6，R7和R8独立地是-H或甲基; （c）-CR 6 H-N（R 9）-CR 7 R 8 - ，其中R 6，R 7和R 8独立地为-H或甲基; （d）-CH 2 -C（R 9）（R 10）-C（R 7）（R 8） - ，其中R 7，R 8，R 9和R 10独立地是-H或 - 甲基，或者R 7和R 8都是-F，R 9和 R 10独立地是-H或 - 甲基，或者R 9和R 10都是-F，或者R 9和R 10一起是（0 =），它们与它们所连接的碳一起形成羰基。

5. 发明申请

WO2013060029A1 ALLOSTERIC MODULATORS OF METABOTROPIC GLUTAMATE RECEPTORS 审中-公开
标题翻译：代谢型谷氨酸受体的独立调节剂
公开(公告)号：WO2013060029A1
公开(公告)日：2013-05-02
申请号：PCT/CN2011/081529
申请日：2011-10-28
申请人： MERCK SHARP & DOHME CORP , ADDEX PHARMA S.A. , LIVERTON, Nigel , JONES, Philip , BOLEA, Christelle , CELANIRE, Sylvain , TANG, Lam , BOUDOU, Cedric , LEI, Zhiyu , LIU, Fuqing , LUO, Yunfu , DONG, Jingchao , SOLL, Richard
发明人： LIVERTON, Nigel , JONES, Philip , BOLEA, Christelle , CELANIRE, Sylvain , TANG, Lam , BOUDOU, Cedric , LEI, Zhiyu , LIU, Fuqing , LUO, Yunfu , DONG, Jingchao , SOLL, Richard
IPC分类号： C07D471/04 , C07D487/04 , A61K31/4162 , A61P25/16
CPC分类号： C07D487/04 , C07D471/04
摘要： Formula (I), and salts thereof, wherein R 1 , R A2 , R A3 and R A4 , are defined herein, which have properties for positive allosteric modulation of mGluR-4 receptor sites. Also described are pharmaceutical formulations comprising the compounds of Formula (I) or their salts, and methods of treating Parkinson's disease and related disorders using the same.
摘要翻译：式（I）及其盐，其中R1，RA2，RA3和RA4在本文中定义，其具有对mGluR-4受体位点的正性变构调节的性质。还描述了包含式（I）化合物或其盐的药物制剂，以及使用其制备帕金森病和相关疾病的方法。

6. 发明申请

WO2012009009A3 NOVEL 2-AMINO-4-PYRAZOLYL-THIAZOLE DERIVATIVES AND THEIR USE AS ALLOSTERIC MODULATORS OF METABOTROPIC GLUTAMATE RECEPTORS 审中-公开
公开(公告)号：WO2012009009A3
公开(公告)日：2012-01-19
申请号：PCT/US2011/001222
申请日：2011-07-12
申请人： ADDEX PHARMA S.A. , BOLEA, Christelle , CELANIRE, Sylvain , BOUDOU, Cedric , TANG, Lam , ROCHER, Jean-Philippe , LIVERTON, Nigel, J.
发明人： BOLEA, Christelle , CELANIRE, Sylvain , BOUDOU, Cedric , TANG, Lam , ROCHER, Jean-Philippe , LIVERTON, Nigel, J.
IPC分类号： A61K31/415 , A01N43/78
摘要： The present invention relates to novel compounds of Formula (1), wherein M, A and B are defined as in Formula (I); invention compounds are modulators of metabotropic glutamate receptors - subtype 4 ("mGluR4") which are useful for the treatment or prevention of central nervous system disorders as well as other disorders modulated by mGluR4 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 mGluR4 is involved.

7. 发明公开

EP2592932A2 NOVEL TETRAHYDROPYRAZOLO[3,4-B]AZEPINE DERIVATIVES AND THEIR USE AS ALLOSTERIC MODULATORS OF METABOTROPIC GLUTAMATE RECEPTORS 有权转让
标题翻译：新型四氢[3,4-B] AZEPINDERIVATIVE及其使用代谢型谷氨酸受体的作为变构调节剂
公开(公告)号：EP2592932A2
公开(公告)日：2013-05-22
申请号：EP11807175.2
申请日：2011-07-11
申请人： Addex Pharma SA , Merck Sharp & Dohme Corp.
发明人： JONES, Philip , TANG, Lam , BOLEA, Christelle , CELANIRE, Sylvain , LIVERTON, Nigel, J.
IPC分类号： A01N43/00 , C07D498/00 , C07D513/00 , C07D515/00
CPC分类号： C07D513/12 , A23L5/00 , A61B5/00 , 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
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.

8. 发明授权

EP2592932B1 NOVEL TETRAHYDROPYRAZOLO[3,4-B]AZEPINE DERIVATIVES AND THEIR USE AS ALLOSTERIC MODULATORS OF METABOTROPIC GLUTAMATE RECEPTORS 有权转让
标题翻译： NEUARTIGE TETRAHYDROPYRAZOL [3,4-B] AZEPINDERIVATIVE UND IHRE VERWENDUNG ALS ALLOSTERISCHE MODULATOREN VON METABOTROPEN GLUTAMATREZEPTOREN
公开(公告)号：EP2592932B1
公开(公告)日：2016-01-20
申请号：EP11807175.2
申请日：2011-07-11
申请人： Addex Pharma SA , Merck Sharp & Dohme Corp.
发明人： JONES, Philip , TANG, Lam , BOLEA, Christelle , CELANIRE, Sylvain , LIVERTON, Nigel, J.
IPC分类号： C07D513/14 , A61K31/55 , A61P25/24 , A61P25/22 , A61P25/18 , A61P25/28
CPC分类号： C07D513/12 , A23L5/00 , A61B5/00 , 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

9. 发明申请

WO2009092764A1 COMPOUNDS COMPRISING A CYCLOBUTOXY GROUP 审中-公开
标题翻译：包含环磷酰氧基的化合物
公开(公告)号：WO2009092764A1
公开(公告)日：2009-07-30
申请号：PCT/EP2009/050719
申请日：2009-01-22
申请人： UCB PHARMA, S.A. , DENONNE, Frédéric , CELANIRE, Sylvain , VALADE, Anne , DEFAYS, Sabine , DURIEUX, Véronique
发明人： DENONNE, Frédéric , CELANIRE, Sylvain , VALADE, Anne , DEFAYS, Sabine , DURIEUX, Véronique
IPC分类号： C07D513/04 , C07D498/04 , C07F9/40 , A61K31/437 , A61P37/08
CPC分类号： C07D498/04 , C07D513/04 , C07F9/6561
摘要： The present invention relates to compounds of formula (I) comprising a cyclobutoxy group, processes for preparing them, pharmaceutical compositions comprising said compounds and their use as pharmaceuticals.
摘要翻译：本发明涉及包含环丁氧基的式（I）化合物，其制备方法，包含所述化合物的药物组合物及其作为药物的用途。

10. 发明公开

EP2595996A2 TRICYCLIC COMPOUNDS AS ALLOSTERIC MODULATORS OF METABOTROPIC GLUTAMATE RECEPTORS 审中-公开
标题翻译：三环化合物AS变构调节代谢型谷氨酸受体
公开(公告)号：EP2595996A2
公开(公告)日：2013-05-29
申请号：EP11807173.7
申请日：2011-07-09
申请人： Merck Sharp & Dohme Corp. , ADDEX Pharma S.A.
发明人： LIVERTON, Nigel, J. , BOLEA, Christelle , CELANIRE, Sylvain , YUNFU, Luo
IPC分类号： C07D513/02
CPC分类号： C07D513/04 , A61K31/433 , A61K31/506 , A61K31/55 , A61K45/06 , C07D513/14
摘要： The present invention describes and claims compounds of the Structural Formula I, Structural Formula II, or Structural Formula III: wherein R
1 , R
2 , R
3 and R
3' are -H or methyl, or R
3 and R
3 taken together form a double bond, or R
3' is -H and R
2 and R
3 taken together form a spiro-cyclopropyl substituent, R
4 is -H or -F, and R5 is -H, methyl, -CI or -Br, Formula II wherein R
1 is -H, ethyl-, isopropyl-, cyclopropyl-, methyl- or methoxy-, R
4 is -H or -F, and "Y" is: (a) -CH
2 -; (b) -CR
6 H-0-CR
7 R
8 -, wherein R
6 , R
7 , and R
8 are independently - H or methyl; (c) -CR
6 H-N(R
9 )-CR
7 R
8 -, wherein R
6 , R
7 , and R
8 are independently -H or methyl; (d) -CH
2 -C(R
9 )(R
10 )-C(R
7 )(R
8 )-, wherein R
7 , R
8 , R
9 and R
10 are independently - H or -methyl, or both R
7 and R
8 are -F, R
9 and R
10 are independently -H or -methyl, or both R
9 and R
10 are -F, or R
9 and R
10 taken together are (0=), which together with the carbon to which they are attached forms a carbonyl group.

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