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公开(公告)号：US20190284266A1
公开(公告)日：2019-09-19
申请号：US16371902
申请日：2019-04-01
Applicant: H. Lundbeck A/S
Inventor： Jan Torleif Pedersen , Kristian Kjaergaard , Lars Østergaard Pedersen , Abdur-Rasheed Asuni , Nina Helen Rosenqvist , Justus Claus Daechsel , Karsten Juhl , Lena Tagmose , Mauro Marigo , Thomas Jensen , Søren Christensen , Laurent David , Christiane Volbracht , Lone Helboe
IPC: C07K16/18 , A61K39/395 , A61K49/00 , G01N33/68
Abstract: The present invention relates to a class of monoclonal antibody that specifically binds the phosphorylated serine 396 residue on pathological hyperphosphorylated (PHF) tau (pS396) with improved affinity, as well as to methods of using these molecules and their tau binding fragments in the treatment of Alzheimer's disease and other tauopathies.
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公开(公告)号：US20190282571A1
公开(公告)日：2019-09-19
申请号：US16345136
申请日：2017-10-26
Applicant: H. Lundbeck A/S
Inventor： Jan Kehler , Lars Kyhn Rasumssen , Morten Langgård , Mikkel Jessing , Paulo Jorge Vieira Vital , Karsten Juhl
IPC: A61K31/4985 , A61K31/553 , A61K31/5377 , A61K45/06 , A61P25/22 , A61P25/24 , A61P25/18 , A61P25/28
Abstract: The present invention provides combination treatments comprising administration of compounds that are PDE1 enzyme inhibitors and other compounds useful in the treatment of psychiatric and/or cognitive disorders such as for example Attention Deficit Hyperactivity Disorder (ADHD), depression, anxiety, narcolepsy, schizophrenia, cognitive impairment or cognitive impairment associated with schizophrenia (CIAS). Separate aspects of the invention are directed to the combined use of said compounds for the treatment of psychiatric and/or cognitive disorders. The present invention also provides phannaceutical compositions comprising said PDE1 enzyme inhibitors together with other compounds useful in the treatment of psychiatric and/or cognitive disorders.
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![1H-pyrazolo[4,3-b]pyridines as PDE1 inhibitors](/abs-image/US/2018/07/31/US10034861B2/abs.jpg.150x150.jpg)
公开(公告)号：US10034861B2
公开(公告)日：2018-07-31
申请号：US15637920
申请日：2017-06-29
Applicant: H. Lundbeck A/S
Inventor： Jan Kehler , Karsten Juhl , Mauro Marigo , Paulo Jorge Vieira Vital , Mikkel Jessing , Morten Langgård , Lars Kyhn Rasmussen , Carl Martin Sebastian Clementson
IPC: C07D401/14 , A61K31/437 , A61K31/4162 , A61K31/4745 , C07D413/04 , C07D471/04 , C07D305/06 , C07D401/04
Abstract: The present invention provides 1H-pyrazolo[4,3-b]pyridin-7-amines of formula (I) as PDE1 inhibitors and their use as a medicament, in particular for the treatment of neurodegenerative disorders and psychiatric disorders.
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34.发明申请2-Amino-3,5,5-Trifluoro-3,4,5,6-Tetrahydropyridines as BACE1 Inhibitors for Treatment of Alzheimer's Disease 审中-公开2-氨基-3,5,5-三氟-3,4,5,6-四氢吡啶作为治疗阿尔茨海默病的BACE1抑制剂公开(公告)号：US20170066741A1
公开(公告)日：2017-03-09
申请号：US15119639
申请日：2015-02-17
Applicant: H. Lundbeck A/S
Inventor： Karsten Juhl , Mauro Marigo , Lena Tagmose , Thomas Jensen
IPC: C07D401/12 , C07D211/72 , C07D405/12 , C07D413/12 , C07D417/12
CPC classification number: C07D401/12 , C07D211/72 , C07D227/10 , C07D405/12 , C07D413/12 , C07D413/14 , C07D417/12
Abstract: The present invention is directed to novel inhibitors of the BACE1 enzyme. Separate aspects of the invention are directed to pharmaceutical compositions comprising said compounds and uses of the compounds to treat disorders for which the reduction of Aβ deposits is beneficial such as Alzheimer's disease.
Abstract translation: 本发明涉及BACE1酶的新型抑制剂。 本发明的单独方面涉及包含所述化合物的药物组合物和该化合物用于治疗Aβ沉积物减少的疾病如阿尔茨海默病的用途。
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35.发明申请2-Amino-3-Fluoro-3-(Fluoromethyl)-6-Methyl-6-Phenyl-3,4,5,6-Tetrahydropyridines as BACE1 Inhibitors 有权2-氨基-3-氟-3-（氟甲基）-6-甲基-6-苯基-3,4,5,6-四氢吡啶作为BACE1抑制剂公开(公告)号：US20170044151A1
公开(公告)日：2017-02-16
申请号：US15233463
申请日：2016-08-10
Applicant: H. Lundbeck A/S
Inventor： Karsten Juhl , Lena Tagmose , Mauro Marigo
IPC: C07D417/12 , C07D413/12 , C07B59/00 , C07D211/72 , C07D401/12
CPC classification number: C07D401/12 , C07B59/002 , C07B2200/05 , C07D211/72 , C07D211/76 , C07D413/12 , C07D417/12
Abstract: The present invention provides compounds of Formula I for the treatment of neurodegenerative or cognitive diseases. The method further provides for piperidine-2-one and piperidine-2-thione intermediates to compounds of formula I.
Abstract translation: 用于治疗神经变性或认知疾病。 该方法还提供式I化合物的哌啶-2-酮和哌啶-2-硫酮中间体。
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Patent Agency Ranking
公开(公告)号：US09434733B2
公开(公告)日：2016-09-06
申请号：US14374278
申请日：2013-01-25
Applicant: H. Lundbeck A/S
Inventor： Niels Svenstrup , Klaus Bæk Simonsen , Lars Kyhn Rasmussen , Karsten Juhl , Morten Langgård , Kate Wen , Yazhou Wang
IPC: C07D487/04
CPC classification number: C07D487/04 , A61K31/53
Abstract: This invention is directed to compounds, which are PDE9 enzyme inhibitors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The present invention also provides processes for the preparation of the compounds of formula (I). The present invention further provides a method of treating a subject suffering from a neurodegenerative disorder comprising administering to the subject a therapeutically effective amount of a compound of formula (I). The present invention further provides a method of treating a subject suffering from a psychiatric disorder comprising administering to the subject a therapeutically effective amount of a compound of formula (I).
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37.发明授权2-amino 3,5,5-trifluoro-3,4,5,6-tetrahydropyridines as BACE1 inhibitors for treatment of Alzheimer's disease 有权2-氨基3,5,5-三氟-3,4,5,6-四氢吡啶作为治疗阿尔茨海默病的BACE1抑制剂公开(公告)号：US09353084B2
公开(公告)日：2016-05-31
申请号：US14625658
申请日：2015-02-19
Applicant: H. Lundbeck A/S
Inventor： Karsten Juhl , Mauro Marigo , Lena Tagmose , Thomas Jensen
IPC: C07D417/12 , C07D211/72 , C07D401/12 , C07D413/12
CPC classification number: C07D401/12 , C07D211/72 , C07D227/10 , C07D405/12 , C07D413/12 , C07D413/14 , C07D417/12
Abstract: The present invention is directed to novel inhibitors of the BACE1 enzyme. Separate aspects of the invention are directed to pharmaceutical compositions comprising said compounds and uses of the compounds to treat disorders for which the reduction of Aβ deposits is beneficial such as Alzheimer's disease.
Abstract translation: 本发明涉及BACE1酶的新型抑制剂。 本发明的单独方面涉及包含所述化合物的药物组合物和该化合物用于治疗A和Bgr的减少的病症的用途; 沉积物是有益的，例如阿尔茨海默氏病。
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38.发明申请2-Amino-6-(difluoromethyl)-5,5-difluoro-6-phenyl-3,4,5,6-tetrahydropyridines as BACE1 Inhibitors 有权2-氨基-6-（二氟甲基）-5,5-二氟-6-苯基-3,4,5,6-四氢吡啶作为BACE1抑制剂公开(公告)号：US20160130267A1
公开(公告)日：2016-05-12
申请号：US14933301
申请日：2015-11-05
Applicant: H. Lundbeck A/S
Inventor： Karsten Juhl , Lena Tagmose , Mauro Marigo
IPC: C07D417/12 , C07D413/12 , C07D401/12
CPC classification number: A61K31/4439 , C07D401/12 , C07D413/12 , C07D417/12
Abstract: The present invention is directed to novel inhibitors of the BACE1 enzyme. Separate aspects of the invention are directed to pharmaceutical compositions comprising said compounds and uses of the compounds to treat disorders for which the reduction of Aβ deposits is beneficial such as Alzheimer's disease.
Abstract translation: 本发明涉及BACE1酶的新型抑制剂。 本发明的单独方面涉及包含所述化合物的药物组合物和该化合物用于治疗A和Bgr的减少的病症的用途; 沉积物是有益的，例如阿尔茨海默氏病。
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公开(公告)号：US20150274736A1
公开(公告)日：2015-10-01
申请号：US14434308
申请日：2012-10-09
Applicant: H. LUNDBECK A/S
Inventor： Niels Svenstrup , Klaus Baek Simonsen , Lars Kyhn Rasmussen , Karsten Juhl , Morten Langgard , Kate Wen , Yazhou Wang
IPC: C07D487/04
CPC classification number: A61K31/506 , C07D487/04
Abstract: This invention is directed to compounds, which are PDE9 enzyme inhibitors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The present invention also provides processes for the preparation of the compounds of formula (I). The present invention further provides a method of treating a subject suffering from a neurodegenerative disorder comprising administering to the subject a therapeutically effective amount of a compound of formula (I). The present invention further provides a method of treating a subject suffering from a psychiatric disorder comprising administering to the subject a therapeutically effective amount of a compound of formula (I).
Abstract translation: 本发明涉及PDE9酶抑制剂的化合物。 本发明提供了包含治疗有效量的本发明化合物和药学上可接受的载体的药物组合物。 本发明还提供制备式（I）化合物的方法。 本发明还提供了治疗患有神经变性疾病的受试者的方法，其包括给予受试者治疗有效量的式（I）化合物。 本发明还提供了治疗患有精神障碍的受试者的方法，其包括向受试者施用治疗有效量的式（I）化合物。
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40.发明申请2-Amino-3,5,5-trifluoro-3,4,5,6-tetrahydropyridines as BACE1 inhibitors for treatment of Alzheimer's disease 有权2-氨基-3,5,5-三氟-3,4,5,6-四氢吡啶作为治疗阿尔茨海默病的BACE1抑制剂公开(公告)号：US20150232449A1
公开(公告)日：2015-08-20
申请号：US14625658
申请日：2015-02-19
Applicant: H. LUNDBECK A/S
Inventor： Karsten Juhl , Mauro Marigo , Lena Tagmose , Thomas Jensen
IPC: C07D401/12 , C07D417/12 , C07D211/72 , C07D413/12
CPC classification number: C07D401/12 , C07D211/72 , C07D227/10 , C07D405/12 , C07D413/12 , C07D413/14 , C07D417/12
Abstract: The present invention is directed to novel inhibitors of the BACE1 enzyme. Separate aspects of the invention are directed to pharmaceutical compositions comprising said compounds and uses of the compounds to treat disorders for which the reduction of Aβ deposits is beneficial such as Alzheimer's disease.
Abstract translation: 本发明涉及BACE1酶的新型抑制剂。 本发明的单独方面涉及包含所述化合物的药物组合物和该化合物用于治疗A和Bgr的减少的病症的用途; 沉积物是有益的，例如阿尔茨海默氏病。
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