公开(公告)号：WO2007135131A9

公开(公告)日：2008-04-03

申请号：PCT/EP2007054891

申请日：2007-05-21

Applicant: JANSSEN PHARMACEUTICA NV ,  ANDRES-GIL JOSE IGNACIO ,  ALCAZAR-VACA MANUEL JESUS ,  LINARES DE LA MORENA MARIA LOU ,  MARTINEZ GONZALEZ SONIA ,  OYARZABAL SANTAMARINA JULEN ,  PASTOR-FERNANDEZ JOAQUIN ,  VEGA RAMIRO JUAN ANTONIO ,  DELGADO-JIMENEZ FRANCISCA ,  DRINKENBURG WILHELMUS HELENA I

Inventor： ANDRES-GIL JOSE IGNACIO ,  ALCAZAR-VACA MANUEL JESUS ,  LINARES DE LA MORENA MARIA LOU ,  MARTINEZ GONZALEZ SONIA ,  OYARZABAL SANTAMARINA JULEN ,  PASTOR-FERNANDEZ JOAQUIN ,  VEGA RAMIRO JUAN ANTONIO ,  DELGADO-JIMENEZ FRANCISCA ,  DRINKENBURG WILHELMUS HELENA I

IPC: C07D241/18 ,  A61K31/497 ,  A61P25/28 ,  C07D401/12 ,  C07D401/14 ,  C07D403/06 ,  C07D405/14

CPC classification number: C07D403/06 ,  C07D241/18 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14

Abstract: The present invention concerns substituted pyrazinone derivatives according to the general Formula (I) a pharmaceutically acceptable acid or base addition salt thereof, a stereochemically isomeric form thereof, an N-oxide form thereof or a quaternary ammonium salt thereof, wherein the variables are defined in Claim 1, having selective a 2C -adrenoceptor antagonist activity. It further relates to their preparation, compositions comprising them and their use as a medicine. The compounds according to the invention are usefull for the prevention and/or treatment of central nervous system disorders, mood disorders, anxiety disorders, stress-related disorders associated with depression and/or anxiety, cognitive disorders, personality disorders, schizoaffective disorders, Parkinson's disease, dementia of the Alzheimer's type, chronic pain conditions, neurodegenerative diseases, addiction disorders, mood disorders and sexual dysfunction.

Abstract translation: 本发明涉及根据通式（I）的取代的吡嗪酮衍生物，其药学上可接受的酸或碱加成盐，其立体化学异构形式，其N-氧化物形式或其季铵盐，其中变量定义于 权利要求1，具有选择性的2C受体拮抗剂活性。 它还涉及它们的制备，包含它们的组合物及其作为药物的用途。 根据本发明的化合物可用于预防和/或治疗中枢神经系统疾病，情绪障碍，焦虑障碍，与抑郁和/或焦虑相关的压力相关疾病，认知障碍，人格障碍，分裂情感障碍，帕金森病 ，阿尔茨海默病的痴呆，慢性疼痛病症，神经变性疾病，成瘾症，情绪障碍和性功能障碍。

公开(公告)号：WO2007135131A8

公开(公告)日：2008-01-24

申请号：PCT/EP2007054891

申请日：2007-05-21

Applicant: JANSSEN PHARMACEUTICA NV ,  ANDRES-GIL JOSE IGNACIO ,  ALCAZAR-VACA MANUEL JESUS ,  LINARES DE LA MORENA MARIA LOU ,  MARTINEZ GONZALEZ SONIA ,  OYARZABAL SANTAMARINA JULEN ,  PASTOR-FERNANDEZ JOAQUIN ,  VEGA RAMIRO JUAN ANTONIO ,  DELGADO-JIMENEZ FRANCISCA ,  DRINKENBURG WILHELMUS HELENA I

Inventor： ANDRES-GIL JOSE IGNACIO ,  ALCAZAR-VACA MANUEL JESUS ,  LINARES DE LA MORENA MARIA LOU ,  MARTINEZ GONZALEZ SONIA ,  OYARZABAL SANTAMARINA JULEN ,  PASTOR-FERNANDEZ JOAQUIN ,  VEGA RAMIRO JUAN ANTONIO ,  DELGADO-JIMENEZ FRANCISCA ,  DRINKENBURG WILHELMUS HELENA I

IPC: C07D241/18 ,  A61K31/497 ,  A61P25/28 ,  C07D401/12 ,  C07D401/14 ,  C07D403/06 ,  C07D405/14

CPC classification number: C07D403/06 ,  C07D241/18 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14

Abstract: The present invention concerns substituted pyrazinone derivatives according to the general Formula (I) a pharmaceutically acceptable acid or base addition salt thereof, a stereochemically isomeric form thereof, an N-oxide form thereof or a quaternary ammonium salt thereof, wherein the variables are defined in Claim 1, having selective a 2C -adrenoceptor antagonist activity. It further relates to their preparation, compositions comprising them and their use as a medicine. The compounds according to the invention are usefull for the prevention and/or treatment of central nervous system disorders, mood disorders, anxiety disorders, stress-related disorders associated with depression and/or anxiety, cognitive disorders, personality disorders, schizoaffective disorders, Parkinson's disease, dementia of the Alzheimer's type, chronic pain conditions, neurodegenerative diseases, addiction disorders, mood disorders and sexual dysfunction.

Abstract translation: 本发明涉及根据通式（I）的取代的吡嗪酮衍生物，其药学上可接受的酸或碱加成盐，其立体化学异构形式，其N-氧化物形式或其季铵盐，其中变量如 权利要求1，具有选择性α2肾上腺素受体拮抗剂活性。 它进一步涉及它们的制备，包含它们的组合物以及它们作为药物的用途。 本发明化合物用于预防和/或治疗中枢神经系统病症，情绪障碍，焦虑症，与抑郁症和/或焦虑症相关的压力相关病症，认知障碍，人格障碍，情感分裂性精神障碍，帕金森病 ，阿尔茨海默型痴呆，慢性疼痛症状，神经退行性疾病，成瘾症，情绪障碍和性功能障碍。

公开(公告)号：AU2019289971A1

公开(公告)日：2020-12-17

申请号：AU2019289971

申请日：2019-06-20

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： BARTOLOMÉ-NEBREDA JOSÉ MANUEL ,  TRABANCO-SUÁREZ ANDRÉS AVELINO ,  DE LUCAS OLIVARES ANA ISABEL ,  DELGADO-JIMÉNEZ FRANCISCA ,  CONDE-CEIDE SUSANA ,  VEGA RAMIRO JUAN ANTONIO

IPC: C07D491/056 ,  A61K31/445 ,  A61P25/28 ,  C07D417/14 ,  C07D513/04

Abstract: The present invention relates to O-GIcNAc hydrolase (OGA) inhibitors having the structure shown in formula (I). 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 inhibition of OGA is beneficial, such as tauopathies, in particular Alzheimer's disease or progressive supranuclear palsy; and neurodegenerative diseases accompanied by a tau pathology, in particular amyotrophic lateral sclerosis or frontotemporal lobe dementia caused by C90RF72 mutations. wherein R

公开(公告)号：HRP20160030T1

公开(公告)日：2016-02-12

申请号：HRP20160030

申请日：2016-01-12

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： TRABANCO-SUÁREZ ANDRÉS AVELINO ,  GIJSEN HENRICUS JACOBUS MARIA ,  VAN GOOL MICHIEL LUC MARIA ,  VEGA RAMIRO JUAN ANTONIO ,  DELGADO-JIMÉNEZ FRANCISCA

IPC: C07D487/04 ,  A61K31/4985 ,  A61P25/28

公开(公告)号：ZA201306545B

公开(公告)日：2015-03-25

申请号：ZA201306545

申请日：2013-08-30

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： TRABANCO-SUAREZ ANDRES AVELINO ,  VAN GOOL MICHEL LUC MARIA ,  DELGADO-JIMENEZ FRANCISCA ,  GIJSEN HENRICUS JACOBUS MARIA ,  VEGA RAMIRO JUAN ANTONIO

IPC: A61K20060101 ,  A61P20060101 ,  C07D20060101

Abstract: The present invention relates to novel 6,7-dihydro-pyrazolo[1,5-a]pyrazin-4-yl-amine 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-secretase is 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.

公开(公告)号：NZ614551A

公开(公告)日：2014-06-27

申请号：NZ61455112

申请日：2012-02-29

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： TRABANCO-SUÁREZ ANDRÉS AVELINO ,  DELGADO-JIMÉNEZ FRANCISCA ,  VAN GOOL MICHIEL LUC MARIA ,  VEGA RAMIRO JUAN ANTONIO ,  GIJSEN HENRICUS JACOBUS MARIA

IPC: C07D487/04 ,  A61K31/4985 ,  A61P25/28

Abstract: Disclosed herein are 6,7-dihydro-pyrazolo[1,5-a]pyrazin-4-yl-amine derivatives as inhibitors of beta-secretase, also known as beta-site amyloid cleaving enzyme, BACE, BACEl, Asp2, or memapsin2. Also disclosed are pharmaceutical compositions comprising such compounds, processes for preparing such compounds and compositions, and the use of such compounds and compositions for the prevention and treatment of disorders in which beta-secretase is 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. In one embodiment the compound is (R)-5-methoxy-pyrazine-2-carboxylic acid [3-(4-amino-3-fluoro-2, 6-dimethyl-6,7-dihydro-pyrazolo[1, 5-a]pyrazin-6-yl)-4-fluoro-phenyl]amide.

公开(公告)号：CL2013002486A1

公开(公告)日：2014-02-21

申请号：CL2013002486

申请日：2013-08-28

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： GIJSEN HENRICUS JACOBUS MARIA ,  VAN GOOL MICHIEL LUC MARIA ,  VEGA RAMIRO JUAN ANTONIO ,  DELGADO-JIMÉNEZ FRANCISCA ,  TRABANCO-SUÁREZ ANDRÉS AVELINO

IPC: C07D487/04 ,  A61K31/4985 ,  A61P25/28

Abstract: LA PRESENTE INVENCIÓN SE REFIERE A DERIVADOS DE 6,7-DIHIDROPIRAZOLO[1,5-A]PIRAZIN-4-IL-AMINA COMO INHIBIDORES DE BETA-SECRETASA, CONOCIDA TAMBIÉN COMO LA ENZIMA QUE ESCINDE LA PROTEÍNA PRECURSORA DE AMILOIDE POR EL SITIO BETA, BACE, BACE1, ASP2 O MEMAPSINA 2. LA INVENCIÓN TAMBIÉN SE REFIERE A COMPOSICIONES FARMACÉUTICAS QUE COMPRENDEN TALES COMPUESTOS, Y AL USO DE TALES COMPUESTOS PARA PREVENIR Y TRATAR TRASTORNOS EN LOS QUE PARTICIPA LA BETA-SECRETASA, TALES COMO LA ENFERMEDAD DE ALZHEIMER (EA), EL DETERIORO COGNITIVO LEVE, SENILIDAD, DEMENCIA, DEMENCIA CON CUERPOS DE LEWY, SÍNDROME DE DOWN, DEMENCIA ASOCIADA CON EL ACCIDENTE CEREBROVASCULAR, DEMENCIA ASOCIADA CON LA ENFERMEDAD DE PARKINSON O DEMENCIA ASOCIADA CON BETA-AMILOIDES. LA FÓRMULA GENERAL 1 DE LOS COMPUESTOS DE LA INVENCIÓN CORRESPONDEN A: DONDE R1 , R 2 , R 3 , X 1 , X2 , X3 , X4 , L Y AR SON COMO SE DEFINEN EN LA MEMORIA DESCRIPTIVA.

公开(公告)号：SG191097A1

公开(公告)日：2013-08-30

申请号：SG2013044730

申请日：2011-12-21

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： TRABANCO-SUAREZ ANDRES AVELINO ,  DELGADO-JIMENEZ FRANCISCA ,  VEGA RAMIRO JUAN ANTONIO ,  TRESADERN GARY JOHN ,  GIJSEN HENRICUS JACOBUS MARIA ,  OEHLRICH DANIEL

Abstract: The present invention relates to novel 5,6-dihydro-imidazo[1,2-a]pyrazin-8- ylamine 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-secretase is involved, such as Alzheimer's disease (AD), mild cognitive impairment, senility, dementia, dementia with Lewy bodies, cerebrovascular amyloid angiopathy, multi- infarct dementia, Down's syndrome, dementia associated with stroke, dementia associated with Parkinson's disease or dementia associated with beta-amyloid.

公开(公告)号：CA2819175A1

公开(公告)日：2012-06-28

申请号：CA2819175

申请日：2011-12-21

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： TRABANCO-SUAREZ ANDRES AVELINO ,  DELGADO-JIMENEZ FRANCISCA ,  VEGA RAMIRO JUAN ANTONIO ,  TRESADERN GARY JOHN ,  GIJSEN HENRICUS JACOBUS MARIA ,  OEHLRICH DANIEL

IPC: C07D487/04 ,  A61K31/5025 ,  A61P25/00

Abstract: The present invention relates to novel 5,6-dihydro-imidazo[1,2-a]pyrazin-8- ylamine 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-secretase is involved, such as Alzheimer's disease (AD), mild cognitive impairment, senility, dementia, dementia with Lewy bodies, cerebrovascular amyloid angiopathy, multi- infarct dementia, Down's syndrome, dementia associated with stroke, dementia associated with Parkinson's disease or dementia associated with beta-amyloid.

公开(公告)号：AU2019291097A1

公开(公告)日：2020-12-17

申请号：AU2019291097

申请日：2019-06-20

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： BARTOLOMÉ-NEBREDA JOSÉ MANUEL ,  TRABANCO-SUÁREZ ANDRÉS AVELINO ,  DELGADO-JIMÉNEZ FRANCISCA ,  DE LUCAS OLIVARES ANA ISABEL ,  VEGA RAMIRO JUAN ANTONIO

IPC: C07D401/14 ,  A61K31/4427 ,  A61K31/4436 ,  A61K31/4439 ,  A61K31/444 ,  A61P25/28 ,  C07D409/14 ,  C07D413/14

Abstract: The present invention relates to O-GIcNAc hydrolase (OGA) inhibitors of formula (I). 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 inhibition of OGA is beneficial, such as tauopathies in particular Alzheimer's disease or progressive supranuclear palsy; and neurodegenerative diseases accompanied by a tau pathology, in particular amyotrophic lateral sclerosis or frontotemporal lobe dementia caused by C90RF72 mutations. R