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1. 发明申请

WO2012008999A3 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：WO2012008999A3
公开(公告)日：2014-03-27
申请号：PCT/US2011001201
申请日：2011-07-09
申请人： MERCK SHARP & DOHME , ADDEX PHARMACEUTICALS SA , 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： A01N43/32 , A61K31/385
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 R1, R2, R3 and R3' are -H or methyl, or R3 and R3 taken together form a double bond, or R3' is -H and R2 and R3 taken together form a spiro-cyclopropyl substituent, R4 is -H or -F, and R5 is -H, methyl, -CI or -Br, Formula II wherein R1 is -H, ethyl-, isopropyl-, cyclopropyl-, methyl- or methoxy-, R4 is -H or -F, and "Y" is: (a) -CH2-; (b) -CR6H-0-CR7R8-, wherein R6, R7, and R8 are independently - H or methyl; (c) -CR6H-N(R9)-CR7R8-, wherein R6, R7, and R8 are independently -H or methyl; (d) -CH2-C(R9)(R10)-C(R7)(R8)-, wherein R7, R8, R9 and R10 are independently - H or -methyl, or both R7 and R8 are -F, R9 and R10 are independently -H or -methyl, or both R9 and R10 are -F, or R9 and R10 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。

2. 发明申请

WO2012009000A3 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：WO2012009000A3
公开(公告)日：2013-04-18
申请号：PCT/US2011001206
申请日：2011-07-11
申请人： ADDEX PHARMACEUTICALS SA , MERCK SHARP & DOHME , 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： A01N43/42
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 ("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.
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

WO2012009001A3 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：新型四氢呋喃并[3,4-B]亚胺衍生物及其作为代谢型谷氨酸受体的独立调节剂
公开(公告)号：WO2012009001A3
公开(公告)日：2012-03-15
申请号：PCT/US2011001207
申请日：2011-07-11
申请人： ADDEX PHARMACEUTICALS SA , JONES PHILIP , MERCK SHARP & DOHME , 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： 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 ("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.
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。

5. 发明专利

AU2011279722A1 Novel tetrahydropyrazolo[3,4-B]azepine derivatives and their use as allosteric modulators of metabotropic glutamate receptors 未知
公开(公告)号：AU2011279722A1
公开(公告)日：2013-02-21
申请号：AU2011279722
申请日：2011-07-11
申请人： ADDEX PHARMACEUTICALS SA , MERCK SHARP & DOHME
发明人： JONES PHILIP , TANG LAM , BOLEA CHRISTELLE , CELANIRE SYLVAIN , LIVERTON NIGEL J
IPC分类号： A01N43/00 , C07D498/00 , C07D513/00 , C07D513/02 , C07D515/00
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

6. 发明专利

CA2807318A1 NOVEL TETRAHYDROPYRAZOLO[3,4-B]AZEPINE DERIVATIVES AND THEIR USE AS ALLOSTERIC MODULATORS OF METABOTROPIC GLUTAMATE RECEPTORS 未知
公开(公告)号：CA2807318A1
公开(公告)日：2012-01-19
申请号：CA2807318
申请日：2011-07-11
申请人： ADDEX PHARMACEUTICALS SA , MERCK SHARP & DOHME
发明人： JONES PHILIP , TANG LAM , BOLEA CHRISTELLE , CELANIRE SYLVAIN , LIVERTON NIGEL J
IPC分类号： C07D513/14 , A61K31/433 , A61K31/4439 , A61K31/506 , A61K31/55 , A61P25/00 , C07D513/04
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 ("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. 发明专利

JP2011079828A Hcv ns3 protease inhibitor 有权
标题翻译： HCV NS3蛋白酶抑制剂
公开(公告)号：JP2011079828A
公开(公告)日：2011-04-21
申请号：JP2010227222
申请日：2010-10-07
申请人： Merck Sharp & Dohme Corp , メルク・シャープ・エンド・ドーム・コーポレイション
发明人： HOLLOWAY M KATHARINE , LIVERTON NIGEL J , LUDMERER STEVEN W , MCCAULEY JOHN A , OLSEN DAVID B , RUDD MICHAEL T , VACCA JOSEPH P , MCINTYRE CHARLES J
IPC分类号： C07K5/08 , A61K31/407 , A61K38/00 , A61P1/16 , A61P31/14 , A61P43/00 , C07D498/16 , C12N9/99
CPC分类号： C07K5/0808 , A61K38/00 , C07K5/0812 , C07K5/0827
摘要： PROBLEM TO BE SOLVED: To provide a compound for treating or preventing HCV infection. SOLUTION: There are provided macrocyclic compounds of formula (I) which are useful as inhibitors of hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections. COPYRIGHT: (C)2011,JPO&INPIT
摘要翻译：待解决的问题：提供用于治疗或预防HCV感染的化合物。提供式（I）的大环化合物，其可用作丙型肝炎病毒（HCV）NS3蛋白酶的抑制剂，其合成及其用于治疗或预防HCV感染的用途。版权所有（C）2011，JPO＆INPIT

8. 发明申请

WO2011106992A8 INHIBITORS OF HEPATITIS C VIRUS NS5B POLYMERASE 审中-公开
标题翻译： HEPATITIS C VIRUS NS5B聚合酶抑制剂
公开(公告)号：WO2011106992A8
公开(公告)日：2012-02-09
申请号：PCT/CN2011000332
申请日：2011-03-02
申请人： MERCK SHARP & DOHME , MCCOMAS CASEY CAMERON , LIVERTON NIGEL J , SOLL RICHARD , LI PENG , PENG XUANJIA , WU HAO , NARJES FRANK , HABERMANN JOERG , KOCH UWE , LIU SHILAN , ANGELETTI P IST RICHERCHE BIO
发明人： MCCOMAS CASEY CAMERON , LIVERTON NIGEL J , SOLL RICHARD , LI PENG , PENG XUANJIA , WU HAO , NARJES FRANK , HABERMANN JOERG , KOCH UWE , LIU SHILAN
IPC分类号： C07D307/84 , A61K31/343 , A61P31/14 , C07D405/04 , C07D405/10
CPC分类号： C07D307/84 , A61K31/343 , A61K45/06 , C07D405/04 , C07D405/10 , C07D405/12 , C07D405/14 , C07D407/12 , C07D409/10 , C07D413/04 , C07D413/10 , C07D413/14 , C07D417/10 , C07D471/04 , C07D473/00 , C07D487/04 , C07D491/04 , C07D495/04 , C07D498/04 , C07D513/04 , A61K2300/00
摘要： Disclosed are compounds of formula (I) that are used as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and /or viral production in a cell-based system.
摘要翻译：公开了用作丙型肝炎病毒（HCV）NS5B聚合酶抑制剂的式（I）化合物，这些化合物的合成，以及这些化合物用于抑制HCV NS5B聚合酶活性的用途，用于治疗或预防HCV感染和抑制在基于细胞的系统中HCV病毒复制和/或病毒生产。

9. 发明申请

WO2012009009A2 NOVEL 2-AMINO-4-PYRAZOLYL-THIAZOLE DERIVATIVES AND THEIR USE AS ALLOSTERIC MODULATORS OF METABOTROPIC GLUTAMATE RECEPTORS 审中-公开
标题翻译：新型2-氨基-4-吡唑并噻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：WO2012009009A2
公开(公告)日：2012-01-19
申请号：PCT/US2011001222
申请日：2011-07-12
申请人： ADDEX PHARMACEUTICALS SA , 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： C07D417/14
CPC分类号： C07D417/14 , A61K31/433 , A61K31/4439 , A61K31/506 , A61K31/53 , A61K31/5377 , A61K31/541 , A61K45/06 , C07D487/04
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.
摘要翻译：本发明涉及式（1）的新化合物，其中M，A和B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。

10. 发明专利

CY1113752T1 ΜΑΚΡΟΚΥΚΛΙΚΕΣ ΕΝΩΣΕΙΣ ΚΙΝΟΞΑΛΙΝΗΣ ΩΣ ΑΝΑΣΤΟΛΕΙΣ ΠΡΩΤΕΑΣΕΙΣ NS3 ΤΟΥ HCV 未知
公开(公告)号：CY1113752T1
公开(公告)日：2016-07-27
申请号：CY121101150
申请日：2012-11-28
申请人： MERCK SHARP & DOHME
发明人： HARPER STEVEN , SUMMA VINCENZO , LIVERTON NIGEL J , MCCAULEY JOHN A
IPC分类号： A61P31/14 , A61K38/06 , A61K38/07 , A61K38/08 , C07K5/08 , C07K5/10 , C07K5/12
摘要： Ηπαρούσαεφεύρεσηαφοράμακροκυκλικήένωσητύπου (Ι) καιτηχρήσητηςωςαναστολέατηςπρωτεάσης NS3 τουιούηπατίτιδας C (HCV), καιτηθεραπευτικήαγωγήή πρόληψημολύνσεωναπό HCV. Τύπος (Ι).

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