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1.发明申请IMIDAZO[1,2-b]PYRIDAZINE DERIVATIVES AND THEIR USE AS PDE10 INHIBITORS 审中-公开咪唑并[1,2-b]哒嗪衍生物及其作为PDE10抑制剂的用途
公开(公告)号：WO2011051342A8
公开(公告)日：2011-07-07
申请号：PCT/EP2010066264
申请日：2010-10-27
Applicant: JANSSEN PHARMACEUTICA NV , PASTOR-FERNANDEZ JOAQUIN , BARTOLOME-NEBREDA JOSE MANUEL , MACDONALD GREGOR JAMES , CONDE-CEIDE SUSANA , DELGADO-GONZALEZ OSCAR , VANHOOF GRETA CONSTANTIA PETER , VAN GOOL MICHIEL LUC MARIA , MARTIN-MARTIN MARIA LUZ , ALONSO-DE DIEGO SERGIO-ALVAR , SWINNEY KELLY ANN , LEYS CARINA , WEERTS JOHAN ERWIN EDMOND
Inventor： PASTOR-FERNANDEZ JOAQUIN , BARTOLOME-NEBREDA JOSE MANUEL , MACDONALD GREGOR JAMES , CONDE-CEIDE SUSANA , DELGADO-GONZALEZ OSCAR , VANHOOF GRETA CONSTANTIA PETER , VAN GOOL MICHIEL LUC MARIA , MARTIN-MARTIN MARIA LUZ , ALONSO-DE DIEGO SERGIO-ALVAR , SWINNEY KELLY ANN , LEYS CARINA , WEERTS JOHAN ERWIN EDMOND
IPC: C07D487/04 , A61K31/5025 , A61P3/00 , A61P25/00
CPC classification number: C07D487/04
Abstract: The present invention relates to novel imidazo[1,2-b]pyridazine derivatives which are inhibitors of the phosphodiesterase 10 enzyme (PDE10) and which are useful for the treatment or prevention of neurological, psychiatric and metabolic disorders in which the PDE10 enzyme is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, to the use of such compounds or pharmaceutical compositions for the prevention or treatment of neurological, psychiatric and metabolic disorders and diseases.
Abstract translation: 本发明涉及作为磷酸二酯酶10酶（PDE10）抑制剂的新型咪唑并[1,2-b]哒嗪衍生物，其可用于治疗或预防其中涉及PDE10酶的神经病学，精神病学和代谢病症 。 本发明还涉及包含此类化合物的药物组合物，涉及制备此类化合物和组合物的方法，涉及此类化合物或药物组合物用于预防或治疗神经病学，精神病学和代谢病症和疾病的用途。
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公开(公告)号：MY192029A
公开(公告)日：2022-07-23
申请号：MYPI2015002868
申请日：2014-06-03
Applicant: JANSSEN PHARMACEUTICA NV
Inventor： MEGENS ANTONIUS ADRIANUS HENDRIKUS PETRUS , MACDONALD GREGOR JAMES , DELGADO-GONZALEZ OSCAR , VAN GOOL MICHIEL LUC MARIA , ALONSO-DE DIEGO SERGIO-ALVAR , TRABANCO-SUAREZ ANDRES AVELINO , DECORTE ANNELIES MARIE ANTONIUS , CID-NU?EZ JOSE MARIA , GARCIA-MOLINA ARANZAZU , ANDRES-GIL JOSE IGNACIO
IPC: C07D487/04 , A61K31/4985 , A61P25/00
Abstract: The present invention relates to novel 6,7-dihydropyrazolo[l ,5-a]pyrazin-4(5H)-one derivatives of Formula (I) as negative allosteric modulators (NAMs) of the metabotropic glutamate receptor subtype 2 ("mGluR2"). 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 or treatment of disorders in which the mGluR2 subtype of metabotropic receptors is involved, especially CNS disorders. (No suitable figure)
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公开(公告)号：AU2015295299B2
公开(公告)日：2019-05-02
申请号：AU2015295299
申请日：2015-07-30
Applicant: JANSSEN PHARMACEUTICA NV
Inventor： ANDRES-GIL JOSE IGNACIO , VAN GOOL MICHIEL LUC MARIA , TRABANCO-SUAREZ ANDRES AVELINO , DE LUCAS OLIVARES ANA ISABEL , ALONSO-DE DIEGO SERGIO-ALVAR , DELGADO-GONZALEZ OSCAR
IPC: C07D487/04 , A61K31/4985 , A61P25/00
Abstract: The present invention relates to novel 6,7-dihydropyrazolo[1,5-a]pyrazin-4(5H)-one derivatives as negative allosteric modulators (NAMs) of the metabotropic glutamate receptor subtype 2 ("mGluR2"). 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 or treatment of disorders in which the mGluR2 subtype of metabotropic receptors is involved.
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公开(公告)号：ES2702192T3
公开(公告)日：2019-02-27
申请号：ES15742317
申请日：2015-07-30
Applicant: JANSSEN PHARMACEUTICA NV
Inventor： ANDRES-GIL JOSÉ IGNACIO , VAN GOOL MICHIEL LUC MARIA , TRABANCO-SUAREZ ANDRÉS AVELINO , DE LUCAS OLIVARES ANA ISABEL , ALONSO-DE DIEGO SERGIO-ALVAR , DELGADO-GONZALEZ OSCAR
IPC: C07D487/04 , A61K31/4985 , A61P25/00
Abstract: Un compuesto de la fórmula (I)**Fórmula** o una forma estereoisomérica del mismo, en la que R1 es fenilo o 2-piridinilo, cada uno de los cuales se sustituye opcionalmente con uno o más sustituyentes, cada uno independientemente seleccionado del grupo que consiste en halógeno, alquilo C1-4, monohalo-alquilo C1-4, polihalo-alquilo C1-4, -alquil C1-4-OH, -CN, -alquil C1-4-O-alquilo C1-4, cicloalquilo C3-7, -O-alquilo C1-4, monohaloalquiloxi C1-4, polihalo-alquiloxi C1-4, SF5, alquiltio C1-4, monohalo-alquiltio C1-4 y polihalo-alquiltio C1-4; R2 es fenilo o piridinilo, cada uno de los cuales se sustituye opcionalmente con uno o más sustituyentes, cada uno independientemente seleccionado del grupo que consiste en halógeno, alquilo C1-4, monohalo-alquilo C1-4, polihalo-alquilo C1-4, -OH, -O-alquilo C1-4, -alquil C1-4-O-alquilo C1-4, monohalo-alquiloxi C1-4, polihalo-alquiloxi C1-4, -alquil C1-4-OH y NR5aR5b; en la que R5a y R5b son cada uno independientemente hidrógeno o alquilo C1-4; R3 es hidrógeno o alquilo C1-4; R4 se selecciona del grupo que consiste en hidrógeno, alquilo C1-4, monohalo-alquilo C1-4, polihalo-alquilo C1-4, - alquil C1-4-O-alquilo C1-4 y -alquil C1-4-OH; o un N-óxido, o una sal farmacéuticamente aceptable o un solvato del mismo.
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公开(公告)号：AU2014276963C1
公开(公告)日：2018-11-08
申请号：AU2014276963
申请日：2014-06-03
Applicant: JANSSEN PHARMACEUTICA NV
Inventor： VAN GOOL MICHIEL LUC MARIA , ALONSO-DE DIEGO SERGIO-ALVAR , CID-NUNEZ JOSE MARIA , DELGADO-GONZALEZ OSCAR , DECORTE ANNELIES MARIE ANTONIUS , MACDONALD GREGOR JAMES , MEGENS ANTONIUS ADRIANUS HENDRIKUS PETRUS , TRABANCO-SUAREZ ANDRES AVELINO , GARCIA-MOLINA ARANZAZU , ANDRES-GIL JOSE IGNACIO
IPC: C07D487/04 , A61K31/4985 , A61P25/00
Abstract: The present invention relates to novel 6,7-dihydropyrazolo[1,5-a]pyrazin-4(5H)-one derivatives of Formula (I) as negative allosteric modulators (NAMs) of the metabotropic glutamate receptor subtype 2 ("mGluR2"). 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 or treatment of disorders in which the mGluR2 subtype of metabotropic receptors is involved, especially CNS disorders.
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Patent Agency Ranking
公开(公告)号：ES2651296T3
公开(公告)日：2018-01-25
申请号：ES10768978
申请日：2010-10-27
Applicant: JANSSEN PHARMACEUTICA NV
Inventor： PASTOR-FERNANDEZ JOAQUIN , BARTOLOME-NEBREDA JOSÉ , MACDONALD GREGOR , CONDE-CEIDE SUSANA , DELGADO-GONZALEZ OSCAR , VANHOOF GRETA , VAN GOOL MICHIEL , MARTIN-MARTIN MARÍA , ALONSO-DE DIEGO SERGIO-ALVAR , SWINNEY KELLY , LEYS CARINA , WEERTS JOHAN
IPC: C07D487/04 , A61K31/5025 , A61P3/00 , A61P25/00
Abstract: Un compuesto de Fórmula (I) **Fórmula** o una forma estereoisómera del mismos, en donde R1 se selecciona de piridinilo, morfolinilo y pirrolidinilo; R2 se selecciona de hidrógeno, metilo, etilo, ciclopropilo, isopropilo, metoxi y trifluorometilo; R3 se selecciona de hidrógeno, cloro, metilo, trifluorometilo y ciclopropilo; Het se selecciona de piridinilo y pirazolilo; R4 se selecciona de hidrógeno; metilo; etilo; isopropilo; isobutilo; trifluorometilo; 2,2,2-trifluoroetilo; 2-hidroxi-2- metilpropilo; (2,2-difluorociclopropil)metilo; 2,2-difluoro-2-ciclopropiletilo; ciclopropilo; 2-metoxietilo; 2-metoxipropilo; (2S)-2-metoxipropilo; 2-isopropoxietilo; 2-etoxietilo; etoximetilo; 1-metoxi-1-metiletilo; 1-metoxi-1-metiletilo; 2-metoxi- 1,1-dimetiletilo; 3-metoxi-3-metilbutilo; 3-metoxipropilo; 2-metoxi-2-metil-propilo; isopropoxi; 2,2,2-trifluoroetoxi; ciclopropilmetoxi; 2-metoxietoxi; 2-metoxi-2-metilpropoxi; tetrahidro-2H-piran-4-ilo; (piridin-3-il)metilo; 2-(pirrolidin-1- il)etilo; isopropilamino; morfolin-4-ilo; pirrolidin-1-ilo; piperacin-1-ilo; (3R)-3-metoxipirrolidin-1-ilo; y (3S)-3- metoxipirrolidin-1-ilo; y R5 es hidrógeno o metilo o una sal farmacéuticamente aceptable o un solvato del mismo.
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公开(公告)号：SI3004107T1
公开(公告)日：2017-09-29
申请号：SI201430322
申请日：2014-06-03
Applicant: JANSSEN PHARMACEUTICA NV
Inventor： VAN GOOL MICHIEL LUC MARIA , ALONSO-DE DIEGO SERGIO-ALVAR , CID-NUNEZ JOSE MARIA , DELGADO-GONZALEZ OSCAR , DECORTE ANNELIES MARIE ANTONIUS , MACDONALD GREGOR JAMES , MEGENS ANTONIUS ADRIANUS HENDRIKUS PETRUS , TRABANCO-SUAREZ ANDRES AVELINO , GARCIA-MOLINA ARANZAZU , ANDRES-GIL JOSE IGNACIO
IPC: C07D487/00 , A61K31/00 , A61P25/00
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公开(公告)号：PH12017500170A1
公开(公告)日：2017-07-10
申请号：PH12017500170
申请日：2017-01-27
Applicant: JANSSEN PHARMACEUTICA NV
Inventor： ALONSO-DE DIEGO SERGIO-ALVAR , VAN GOOL MICHIEL LUC MARIA , MARTIN-MARTIN MARIA LUZ , CONDE-CEIDE SUSANA , ANDRES-GIL JOSE IGNACIO , DELGADO-GONZALEZ OSCAR , TRESADERN GARY JOHN , TRABANCO-SUAREZ ANDRES
IPC: A61K31/4985 , A61P25/00 , C07D487/04
Abstract: The present invention relates to novel 6,7-dihydropyrazolo[1,5-a]pyrazin-4(5H)-one derivatives as negative allosteric modulators (NAMs) of the metabotropic glutamate receptor subtype 2 ("mGluR2"). 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 or treatment of disorders in which the mGluR2 subtype of metabotropic receptors is involved.
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公开(公告)号：CA2967164A1
公开(公告)日：2016-06-23
申请号：CA2967164
申请日：2015-12-16
Applicant: JANSSEN PHARMACEUTICA NV
Inventor： TRABANCO-SUAREZ ANDRES AVELINO , DELGADO-GONZALEZ OSCAR , GIJSEN HENRICUS JACOBUS MARIA , VAN GOOL MICHIEL LUC MARIA , VAN BRANDT SVEN FRANCISCUS ANNA , DE CLEYN MICHEL ANNA JOZEF , FUSTERO LARDIES SANTOS , MATEU SANCHIS NATALIA
IPC: C07D403/12 , A61K31/506 , A61P25/28 , C07D401/10 , C07D401/12 , C07D403/10 , C07D413/12
Abstract: The present invention relates to 2,3,4,5-tetrahydropyridin-6-amine and 3,4- dihydro-2H-pyrrol-5-amine compound inhibitors of beta-secretase having the structure shown in Formula (I), wherein the radicals are as defined in the specification. 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, dementia associated with beta- amyloid, age-related macular degeneration, type 2 diabetes or metabolic disorders.
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公开(公告)号：CA2954218A1
公开(公告)日：2016-02-04
申请号：CA2954218
申请日：2015-07-30
Applicant: JANSSEN PHARMACEUTICA NV
Inventor： ANDRES-GIL JOSE IGNACIO , VAN GOOL MICHIEL LUC MARIA , TRABANCO-SUAREZ ANDRES AVELINO , DE LUCAS OLIVARES ANA ISABEL , ALONSO-DE DIEGO SERGIO-ALVAR , DELGADO-GONZALEZ OSCAR
IPC: C07D487/04 , A61K31/4985 , A61P25/00
Abstract: The present invention relates to novel 6,7-dihydropyrazolo[1,5-a]pyrazin-4(5H)-one derivatives as negative allosteric modulators (NAMs) of the metabotropic glutamate receptor subtype 2 ("mGluR2"). 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 or treatment of disorders in which the mGluR2 subtype of metabotropic receptors is involved.
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