公开(公告)号：WO2012078817A1

公开(公告)日：2012-06-14

申请号：PCT/US2011/063842

申请日：2011-12-07

Applicant: VANDERBILT UNIVERSITY ,  CONN, P., Jeffrey ,  LINDSLEY, Craig, W. ,  STAUFFER, Shaun, R. ,  JONES, Carrie, K. ,  CONDE-CEIDE, Susana ,  TONG, Han Min ,  BARTOLOME-NEBREDA, Jose, Manuel ,  MACDONALD, Gregor, James

Inventor： CONN, P., Jeffrey ,  LINDSLEY, Craig, W. ,  STAUFFER, Shaun, R. ,  JONES, Carrie, K. ,  CONDE-CEIDE, Susana ,  TONG, Han Min ,  BARTOLOME-NEBREDA, Jose, Manuel ,  MACDONALD, Gregor, James

IPC: A61K31/4162 ,  C07D231/54

CPC classification number: C07D487/04

Abstract: In one aspect, the invention relates to bicyclic pyrazole compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

Abstract translation: 一方面，本发明涉及可用作代谢型谷氨酸受体亚型5（mGluR5）的正变构调节剂的双环吡唑化合物，其衍生物和相关化合物。 制备化合物的合成方法; 包含该化合物的药物组合物; 以及使用所述化合物和组合物治疗与谷氨酸官能障碍相关的神经和精神障碍的方法。 该摘要旨在作为用于在特定技术中进行搜索的扫描工具，而不意在限制本发明。

公开(公告)号：WO2011154374A1

公开(公告)日：2011-12-15

申请号：PCT/EP2011/059330

申请日：2011-06-07

Applicant: JANSSEN PHARMACEUTICA NV ,  TRABANCO-SUÁREZ, Andrés, Avelino ,  TRESADERN, Gary, John ,  MACDONALD, Gregor, James ,  VEGA RAMIRO, Juan, Antonio

Inventor： TRABANCO-SUÁREZ, Andrés, Avelino ,  TRESADERN, Gary, John ,  MACDONALD, Gregor, James ,  VEGA RAMIRO, Juan, Antonio

IPC: C07D401/10 ,  C07D401/12 ,  C07D403/10 ,  A61K31/496 ,  A61P25/28 ,  A61P25/16

CPC classification number: C07D403/12 ,  C07D401/10 ,  C07D401/12 ,  C07D403/10

Abstract: The present invention relates to novel 5-amino-3,6-dihydro-1H-pyrazin-2-one derivatives as inhibitors of beta-secretase, also known as beta-site amyloid cleaving enzyme, BACE, BACE1, Asp2, or memapsin2. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which beta-secretaseis involved, such as Alzheimer's disease (AD), mild cognitive impairment, senility, dementia, dementia with Lewy bodies, Down's syndrome, dementia associated with stroke, dementia associated with Parkinson's disease or dementia associated with beta-amyloid.

Abstract translation: 本发明涉及作为β-分泌酶抑制剂的新型5-氨基-3,6-二氢-1H-吡嗪-2-酮衍生物，也称为β位点淀粉样蛋白切割酶BACE，BACE1，Asp2或memapsin2。 本发明还涉及包含这些化合物的药物组合物，制备这些化合物和组合物的方法，以及这些化合物和组合物用于预防和治疗所涉及的β-分泌酶如阿尔茨海默病（AD）的疾病的用途 ），轻度认知障碍，衰老，痴呆，路易体痴呆，唐氏综合征，与中风相关的痴呆，与帕金森病或与β-淀粉样蛋白相关的痴呆相关的痴呆。

公开(公告)号：WO2010094647A1

公开(公告)日：2010-08-26

申请号：PCT/EP2010/051843

申请日：2010-02-15

Applicant: ORTHO-MCNEIL-JANSSEN PHARMACEUTICALS, INC ,  GIJSEN, Henricus, Jacobus, Maria ,  BISCHOFF, François Paul ,  ZHUANG, Wei ,  VAN BRANDT, Sven, Franciscus, Anna ,  SURKYN, Michel ,  ZAJA, Mirko ,  BERTHELOT, Didier, Jean-Claude ,  DE CLEYN, Michel, Anna, Jozef ,  MACDONALD, Gregor, James ,  OEHLRICH, Daniel

Inventor： GIJSEN, Henricus, Jacobus, Maria ,  BISCHOFF, François Paul ,  ZHUANG, Wei ,  VAN BRANDT, Sven, Franciscus, Anna ,  SURKYN, Michel ,  ZAJA, Mirko ,  BERTHELOT, Didier, Jean-Claude ,  DE CLEYN, Michel, Anna, Jozef ,  MACDONALD, Gregor, James ,  OEHLRICH, Daniel

IPC: C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D413/12 ,  C07D413/14 ,  C07D471/04 ,  A61K31/506 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/454 ,  A61K31/4184 ,  A61K31/4439 ,  A61K31/423 ,  A61P25/00

CPC classification number: C07D413/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14 ,  C07D471/04

Abstract: The present invention is concerned with novel substituted benzoxazole, benzimidazole, oxazolopyridine and imidazopyridine derivatives of Formula (I) wherein R 1 , R 2 , R 3 , R 4 , X, A 1 , A 2 , A 3 , A 4 , Y 1 , Y 2 , Y 3 and Z have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.

Abstract translation: 本发明涉及式（I）的新的取代苯并恶唑，苯并咪唑，恶唑并吡啶和咪唑并吡啶衍生物，其中R1，R2，R3，R4，X，A1，A2，A3，A4，Y1，Y2，Y3和Z具有含义 在权利要求中限定。 根据本发明的化合物可用作γ-分泌酶调节剂。 本发明还涉及制备这种新化合物的方法，包含所述化合物作为活性成分的药物组合物以及所述化合物作为药物的用途。

公开(公告)号：WO2010060589A1

公开(公告)日：2010-06-03

申请号：PCT/EP2009/008346

申请日：2009-11-24

Applicant: ORTHO-MCNEIL-JANSSEN PHARMACEUTICALS, INC. ,  ADDEX PHARMA S.A. ,  CID-NUNEZ, José, Maria ,  TRABANCO-SUAREZ, Andrès, Avelino ,  MACDONALD, Gregor, James

Inventor： CID-NUNEZ, José, Maria ,  TRABANCO-SUAREZ, Andrès, Avelino ,  MACDONALD, Gregor, James

IPC: C07D471/04 ,  A61K31/437 ,  A61P25/00

CPC classification number: C07D265/36

Abstract: The present invention relates to novel indole and benzoxazine derivatives which are positive allosteric modulators of the metabotropic glutamate receptor subtype 2 ("mGluR2") and 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. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, and to the use of such compounds for the prevention or treatment of neurological and psychiatric disorders and diseases in which mGluR2 is involved.

Abstract translation: 本发明涉及新的吲哚和苯并恶嗪衍生物，其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能力障碍相关的神经和精神障碍及其中 涉及代谢型受体的mGluR2亚型。 本发明还涉及包含这种化合物的药物组合物，制备这些化合物和组合物的方法，以及这些化合物用于预防或治疗其中涉及mGluR2的神经和精神疾病和疾病的用途。

公开(公告)号：WO2010012758A1

公开(公告)日：2010-02-04

申请号：PCT/EP2009/059788

申请日：2009-07-29

Applicant: JANSSEN PHARMACEUTICA NV ,  BARTOLOMÉ-NEBREDA, José Manuel ,  MACDONALD, Gregor, James ,  VAN GOOL, Michiel, Luc, Maria

Inventor： BARTOLOMÉ-NEBREDA, José Manuel ,  MACDONALD, Gregor, James ,  VAN GOOL, Michiel, Luc, Maria

IPC: C07D213/74 ,  C07D213/84 ,  A61K31/496 ,  A61P25/00

CPC classification number: C07D213/74 ,  C07D213/84

Abstract: The present invention relates to piperazin-1-yl-trifluoromethyl-substituted-pyridines that are fast dissociating dopamine 2 receptor antagonists, processes for preparing these compounds, pharmaceutical compositions comprising these compounds as an active ingredient. The compounds find utility as medicines for treating or preventing central nervous system disorders, for example schizophrenia, by exerting an antipsychotic effect without motor side effects. Formula (I).

Abstract translation: 本发明涉及快速解离多巴胺2受体拮抗剂的哌嗪-1-基 - 三氟甲基取代的吡啶，制备这些化合物的方法，包含这些化合物作为活性成分的药物组合物。 该化合物可用作治疗或预防中枢神经系统疾病（例如精神分裂症）的药物，通过发挥抗精神病作用而没有运动副作用。 式（I）。

公开(公告)号：WO2009033704A1

公开(公告)日：2009-03-19

申请号：PCT/EP2008/007551

申请日：2008-09-12

Applicant: ORTHO-MCNEIL-JANSSEN PHARMACEUTICALS, INC. ,  ADDEX PHARMA S.A. ,  CID-NUNEZ, José Maria ,  TRABANCO-SUAREZ, Andrés, Avelino ,  MacDONALD, Gregor, James ,  DUVEY, Guillaume, Albert, Jacques ,  LÜTJENS, Robert, Johannes ,  FINN, Terry, Patrick

Inventor： CID-NUNEZ, José Maria ,  TRABANCO-SUAREZ, Andrés, Avelino ,  MacDONALD, Gregor, James ,  DUVEY, Guillaume, Albert, Jacques ,  LÜTJENS, Robert, Johannes ,  FINN, Terry, Patrick

IPC: C07D401/04 ,  C07D493/10 ,  A61K31/4545 ,  A61P25/00

CPC classification number: A61K31/4545 ,  A61K9/0014 ,  A61K9/0019 ,  A61K9/08 ,  A61K9/10 ,  A61K9/2009 ,  A61K9/2013 ,  A61K9/2018 ,  A61K9/2059 ,  A61K31/444 ,  A61K31/5377 ,  A61K45/06 ,  A61K47/10 ,  A61K47/44 ,  C07D211/86 ,  C07D401/04 ,  C07D491/107 ,  C07D493/10 ,  A61K2300/00

Abstract: 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.

Abstract translation: 本发明涉及新化合物，特别是根据式（I）的新型吡啶酮衍生物，其中所有基团如申请和权利要求中所定义。 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其中涉及代谢型受体的mGluR2亚型的疾病 。 特别地，这些疾病是选自焦虑，精神分裂症，偏头痛，抑郁症和癫痫组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。

公开(公告)号：WO2008107480A8

公开(公告)日：2008-09-12

申请号：PCT/EP2008/052767

申请日：2008-03-07

Applicant: JANSSEN PHARMACEUTICA NV ,  ADDEX Pharma S.A. ,  CID-NÚÑEZ, José, Maria ,  TRABANCO-SUÁREZ, Andrés, Avelino ,  MACDONALD, Gregor, James ,  DUVEY, Guillaume, Albert, Jacques ,  LÜTJENS, Robert, Johannes

Inventor： CID-NÚÑEZ, José, Maria ,  TRABANCO-SUÁREZ, Andrés, Avelino ,  MACDONALD, Gregor, James ,  DUVEY, Guillaume, Albert, Jacques ,  LÜTJENS, Robert, Johannes

IPC: 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

Abstract: 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.

公开(公告)号：WO2004080986A1

公开(公告)日：2004-09-23

申请号：PCT/EP2004/002554

申请日：2004-03-09

Applicant: GLAXO GROUP LIMITED ,  MACDONALD, Gregor, James ,  THOMPSON, Mervyn

Inventor： MACDONALD, Gregor, James ,  THOMPSON, Mervyn

IPC: C07D295/096

CPC classification number: C07D295/096

Abstract: This invention relates to novel phenyl sulfone compounds of formula (I), having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of CNS and other disorders.

Abstract translation: 本发明涉及具有药理学活性的式（I）的新型苯基砜化合物，其制备方法，含有它们的组合物及其在治疗CNS和其它疾病中的用途。

公开(公告)号：WO2003080608A2

公开(公告)日：2003-10-02

申请号：PCT/EP2003/003195

申请日：2003-03-25

Applicant: GLAXO GROUP LIMITED ,  JOHNSON, Christopher, Norbert ,  MACDONALD, Gregor, James ,  MITCHELL, Darren, Jason ,  MOSS, Stephen, Frederick ,  THOMPSON, Mervyn ,  WITTY, David

Inventor： JOHNSON, Christopher, Norbert ,  MACDONALD, Gregor, James ,  MITCHELL, Darren, Jason ,  MOSS, Stephen, Frederick ,  THOMPSON, Mervyn ,  WITTY, David

IPC: C07D471/04

CPC classification number: C07D471/04 ,  C07D215/40 ,  C07D215/46

Abstract: The present invention relates to novel quinoline and aza indole compounds having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of CNS and other disorders.

Abstract translation: 本发明涉及具有药理活性的新型喹啉和氮杂吲哚化合物，其制备方法，含有它们的组合物及其在治疗CNS和其它疾病中的用途。

公开(公告)号：WO2003080580A3

公开(公告)日：2003-10-02

申请号：PCT/EP2003/003197

申请日：2003-03-25

Applicant: GLAXO GROUP LIMITED ,  AHMED, Mahmood ,  JOHNSON, Christopher, Norbert ,  JONES, Martin, C ,  MACDONALD, Gregor, James ,  MOSS, Stephen, Frederick ,  THOMPSON, Mervyn ,  WADE, Charles, Edward ,  WITTY, David

Inventor： AHMED, Mahmood ,  JOHNSON, Christopher, Norbert ,  JONES, Martin, C ,  MACDONALD, Gregor, James ,  MOSS, Stephen, Frederick ,  THOMPSON, Mervyn ,  WADE, Charles, Edward ,  WITTY, David

IPC: C07D215/40

Abstract: The present invention relates to quinoline compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein R 1 and R 2 independently represent hydrogen or C 1-6 alkyl or R 1 is linked to R 2 to form a group (CH 2 ) 2 , (CH 2 ) 3 or (CH 2 ) 4 ; R 3 , R 4 and R 5 independently represent hydrogen, halogen, cyano, -CF 3 , -CF 3 O, C 1-6 alkyl, C 1-6 alkoxy, C 1-6 alkanoyl or a group -CONR 6 R 7 ; m represents an integer from 1 to 4, such that when m is an integer greater than 1, two R 2 groups may instead be linked to form a group CH 2 , (CH 2 ) 2 or (CH 2 ) 3 ; n represents an integer from 1 to 3; p represents 1 or 2; A represents a group -Ar 1 or -Ar 2 Ar 3 ; Ar 1 , Ar 2 and Ar 3 independently represent and aryl group or a heteroaryl group, both of which may be optionally substituted by one or more substituents having pharmacological activity, to processes for their preparation, to compositions containing them and to their use in the treatment of CNS and other disorders.