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1.发明授权公开(公告)号：US09096589B2
公开(公告)日：2015-08-04
申请号：US13513867
申请日：2010-12-15
Applicant: Ask Püschl , Jacob Nielsen , Jan Kehler , John Paul Kilburn , Mauro Marigo , Morten Langgård
Inventor： Ask Püschl , Jacob Nielsen , Jan Kehler , John Paul Kilburn , Mauro Marigo , Morten Langgård
IPC: C07D487/04 , C07D471/04 , A61P25/28 , A61P25/16 , A61P25/18 , A61P25/36 , A61P25/32 , A61P25/22 , A61P25/30 , A61P25/00
CPC classification number: A61K31/4985 , A61K45/06 , C07D471/04 , C07D487/04
Abstract: This invention is directed to compounds, which are PDE10A 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 also provides a method of treating a subject suffering from a drug addiction 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PDE10A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。 本发明还提供了制备式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，其包括向受试者施用治疗有效量的式I化合物。本发明 本发明还提供了治疗患有药物成瘾症的受试者的方法，其包括向受试者施用治疗有效量的式I化合物。本发明还提供了治疗患有精神病障碍患者的方法，包括给予 治疗有效量的式I化合物。
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2.发明申请公开(公告)号：US20120309764A1
公开(公告)日：2012-12-06
申请号：US13515351
申请日：2010-12-15
Applicant: Ask Püschl , Jacob Nielsen , Jan Kehler , John Paul Kilburn , Mauro Marigo , Morten Langgård
Inventor： Ask Püschl , Jacob Nielsen , Jan Kehler , John Paul Kilburn , Mauro Marigo , Morten Langgård
IPC: A61K31/4985 , C07D487/04 , C07D471/04 , A61P25/16 , A61P25/18 , A61P25/28 , A61P25/32 , A61P25/30 , A61K31/437 , A61P25/00
CPC classification number: C07D487/04 , C07D471/04
Abstract: This invention is directed to compounds, which are PDE10A 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 also provides a method of treating a subject suffering from a drug addiction 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PDE10A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。 本发明还提供了制备式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，其包括向受试者施用治疗有效量的式I化合物。本发明 本发明还提供了治疗患有药物成瘾症的受试者的方法，其包括向受试者施用治疗有效量的式I化合物。本发明还提供了治疗患有精神病障碍患者的方法，包括给予 治疗有效量的式I化合物。
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3.发明申请2-ARYLIMIDAZOLE DERIVATIVES AS PDE10A ENZYME INHIBITORS 有权2-ARYLIMIDAZOLE DERIVATIVES PDE10A ENZYME INHIBITORS公开(公告)号：US20120302548A1
公开(公告)日：2012-11-29
申请号：US13515325
申请日：2010-12-15
Applicant: Ask Püschl , Jacob Nielsen , Jan Kehler , John Paul Kilburn , Mauro Marigo , Morten Langgård
Inventor： Ask Püschl , Jacob Nielsen , Jan Kehler , John Paul Kilburn , Mauro Marigo , Morten Langgård
IPC: A61K31/4985 , C07D471/04 , A61K31/437 , A61K31/551 , A61P25/30 , A61P25/28 , A61P25/18 , A61P25/32 , A61P25/36 , C07D487/04 , A61K31/554
CPC classification number: C07D487/04 , C07D471/04
Abstract: This invention is directed to compounds, which are PDE10A 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 also provides a method of treating a subject suffering from a drug addiction 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PDE10A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。 本发明还提供了制备式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，其包括向受试者施用治疗有效量的式I化合物。本发明 本发明还提供了治疗患有药物成瘾症的受试者的方法，其包括向受试者施用治疗有效量的式I化合物。本发明还提供了治疗患有精神病障碍患者的方法，包括给予 治疗有效量的式I化合物。
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公开(公告)号：US08552045B2
公开(公告)日：2013-10-08
申请号：US13299368
申请日：2011-11-18
Applicant: Jan Kehler , Jacob Nielsen , Mauro Marigo , John Paul Kilburn , Morten Langgård
Inventor： Jan Kehler , Jacob Nielsen , Mauro Marigo , John Paul Kilburn , Morten Langgård
IPC: A61K31/415
CPC classification number: C07D487/04 , A61K31/437 , A61K31/4985 , A61K45/06 , C07D471/04 , C07D519/00
Abstract: This invention is directed to compounds with the structure which are PDE10A 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 1. 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 1. The present invention also provides a method of treating a subject suffering from a drug addiction comprising administering to the subject a therapeutically effective amount of a compound of formula 1. 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 1.
Abstract translation: 本发明涉及具有PDE10A酶抑制剂结构的化合物。 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。 本发明还提供了制备式1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，其包括向受试者施用治疗有效量的式1的化合物。本发明 本发明还提供了治疗患有药物成瘾的受试者的方法，包括向受试者施用治疗有效量的式1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，包括给予 服用治疗有效量的式1化合物。
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Patent Agency Ranking
公开(公告)号：US08501797B2
公开(公告)日：2013-08-06
申请号：US13515325
申请日：2010-12-15
Applicant: Ask Püschl , Jacob Nielsen , Jan Kehler , John Paul Kilburn , Mauro Marigo , Morten Langgård
Inventor： Ask Püschl , Jacob Nielsen , Jan Kehler , John Paul Kilburn , Mauro Marigo , Morten Langgård
IPC: A61K31/415
CPC classification number: C07D487/04 , C07D471/04
Abstract: This invention is directed to compounds of formula I having the structure which are PDE10A 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 also provides a method of treating a subject suffering from a drug addiction 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: 本发明涉及具有PDE10A酶抑制剂结构的式I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。 本发明还提供了制备式I化合物的方法。本发明还提供了治疗患有神经退行性疾病的受试者的方法，包括给予受试者治疗有效量的式I化合物本发明 还提供了治疗患有药物成瘾的受试者的方法，包括向受试者施用治疗有效量的式I化合物。本发明还提供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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公开(公告)号：US20120129836A1
公开(公告)日：2012-05-24
申请号：US13299368
申请日：2011-11-18
Applicant: Jan Kehler , Jacob Nielsen , Mauro Marigo , John Paul Kilburn , Morten Langgård
Inventor： Jan Kehler , Jacob Nielsen , Mauro Marigo , John Paul Kilburn , Morten Langgård
IPC: A61K31/4985 , C07D471/04 , A61K31/437 , A61P25/14 , A61P25/18 , A61K31/5513 , A61K31/519 , A61K31/554 , C07D487/04 , A61P25/28
CPC classification number: C07D487/04 , A61K31/437 , A61K31/4985 , A61K45/06 , C07D471/04 , C07D519/00
Abstract: This invention is directed to compounds, which are PDE10A 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 also provides a method of treating a subject suffering from a drug addiction 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PDE10A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。 本发明还提供了制备式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，其包括向受试者施用治疗有效量的式I化合物。本发明 本发明还提供了治疗患有药物成瘾症的受试者的方法，其包括向受试者施用治疗有效量的式I化合物。本发明还提供了治疗患有精神病障碍患者的方法，包括给予 治疗有效量的式I化合物。
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7.发明申请Catalytic Asymmetric Synthesis of Optically Active Alpha-Halo-Carbonyl Compounds 审中-公开光活性α-卤代羰基化合物的催化不对称合成公开(公告)号：US20070276142A1
公开(公告)日：2007-11-29
申请号：US10589256
申请日：2005-02-11
Applicant: Nis Halland , Karl Jorgensen , Mauro Marigo , Alan Braunton , Stephan Bachmann , Doris Schluter
Inventor： Nis Halland , Karl Jorgensen , Mauro Marigo , Alan Braunton , Stephan Bachmann , Doris Schluter
IPC: C07D207/04 , C07C45/00 , C07D211/00 , C07D211/70 , C07D317/72
CPC classification number: C07D207/08 , C07B53/00 , C07C45/63 , C07F7/1804 , C07F7/188 , C07C47/14 , C07C47/24 , C07C49/16 , C07C49/463 , C07C47/353 , C07C47/277 , C07C47/17
Abstract: A process for the catalytic asymmetric synthesis of an optically active compound of the formula (1a) or (1b) wherein R is an organic group; X is halogen; R1 and R2 which may the same or different represents H, or an organic group or R1 and R2 may be bridged together forming part of a ring system; R and R2 may be bridged together forming part of a ring system; with the provisio that R and R1 are different and R2, when different from H, is attached though a carbon-carbon bond, comprising the step of reacting a compound of the formula (2) with a halogenation agent in the presence of a catalytic amount of a chiral nitrogen containing organic compound.
Abstract translation: 一种用于催化不对称合成式（1a）或（1b）的光学活性化合物的方法，其中R是有机基团; X是卤素; R 1和R 2可以相同或不同，表示H或有机基团或R 1和R 2， SUB>可以桥接在一起形成环系统的一部分; R和R 2可以桥连在一起形成环系的一部分; 条件是R和R 1不同，R 2与H不同时，通过碳 - 碳键连接，包括使下列化合物与 式（2）与卤化剂在催化量的手性含氮有机化合物存在下反应。
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8.发明授权公开(公告)号：US08501795B2
公开(公告)日：2013-08-06
申请号：US13515351
申请日：2010-12-15
Applicant: Ask Püschl , Jacob Nielsen , Jan Kehler , John Paul Kilburn , Mauro Marigo , Morten Langgård
Inventor： Ask Püschl , Jacob Nielsen , Jan Kehler , John Paul Kilburn , Mauro Marigo , Morten Langgård
IPC: A61K31/41
CPC classification number: C07D487/04 , C07D471/04
Abstract: This invention is directed to compounds of formula I having the structure which are PDE10A 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 also provides a method of treating a subject suffering from a drug addiction 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: 本发明涉及具有PDE10A酶抑制剂结构的式I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。 本发明还提供了制备式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，其包括向受试者施用治疗有效量的式I化合物。本发明 本发明还提供了治疗患有药物成瘾症的受试者的方法，其包括向受试者施用治疗有效量的式I化合物。本发明还提供了治疗患有精神病障碍患者的方法，包括给予 治疗有效量的式I化合物。
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9.发明申请公开(公告)号：US20120309714A1
公开(公告)日：2012-12-06
申请号：US13513867
申请日：2010-12-15
Applicant: Ask Püschl , Jacob Nielsen , Jan Kehler , John Paul Kilburn , Mauro Marigo , Morten Langgård
Inventor： Ask Püschl , Jacob Nielsen , Jan Kehler , John Paul Kilburn , Mauro Marigo , Morten Langgård
IPC: A61K31/519 , C07D471/04 , A61K31/437 , A61K31/4985 , C07F7/10 , A61K31/496 , A61P25/28 , A61P25/18 , A61P25/00 , A61P25/22 , A61K31/551 , A61K31/554 , C07D487/04 , A61K31/695
CPC classification number: A61K31/4985 , A61K45/06 , C07D471/04 , C07D487/04
Abstract: This invention is directed to compounds, which are PDE10A 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 also provides a method of treating a subject suffering from a drug addiction 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PDE10A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。 本发明还提供了制备式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，其包括向受试者施用治疗有效量的式I化合物。本发明 本发明还提供了治疗患有药物成瘾症的受试者的方法，其包括向受试者施用治疗有效量的式I化合物。本发明还提供了治疗患有精神病障碍患者的方法，包括给予 治疗有效量的式I化合物。
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