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。

公开(公告)号：US09643970B2

公开(公告)日：2017-05-09

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: A61K31/4985 ,  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).

公开(公告)号：US09592230B2

公开(公告)日：2017-03-14

申请号：US14663706

申请日：2015-03-20

Applicant: H. Lundbeck A/S

Inventor： Andreas Ritzen ,  Morten Langgard ,  Jan Kehler ,  Jacob Nielsen ,  John Paul Kilburn ,  Mohamed M. Farah

IPC: C07D487/04 ,  A61K31/4985 ,  C07D403/12 ,  C07D471/04 ,  A61K31/437 ,  A61K45/06

CPC classification number: A61K31/4985 ,  A61K31/437 ,  A61K45/06 ,  C07D403/12 ,  C07D471/04 ,  C07D487/04

Abstract: This invention is directed to phenylimidazole derivatives having the formula I: wherein HET is an optionally substituted heteroaromatic group; -L- is selected from the group consisting of —CH2—CH2—, —S—CH2—, —CH2—S— and —CH═CH—, R1 is selected from the group consisting of H, C1-C6 alkyl; C1-C6 alkyl(C3-C8)cycloalkyl; C1-C6 hydroxyalkyl, CH2CN, CH2C(O)NH2, C1-C6 arylalkyl, and C1-C6 alkyl-heterocycloalkyl, and R2, R3, R4, R5 and R6 are selected individually from the group consisting of H, C1-C6 alkoxy and halogen, or pharmaceutically acceptable acid addition salts thereof, which are PDE10A enzyme inhibitors useful in the treatment of psychiatric disorders and drug addiction.

Abstract translation: 本发明涉及苯基咪唑化合物，它们是可用于治疗神经和精神疾病的PDE10A酶抑制剂。

公开(公告)号：US20150025081A1

公开(公告)日：2015-01-22

申请号：US14488554

申请日：2014-09-17

Applicant: H. Lundbeck A/S

Inventor： Andreas Ritzen ,  Morten Langgard ,  Jan Kehler ,  Jacob Nielsen ,  John Paul Kilburn ,  Mohamed M. Farah

IPC: C07D487/04 ,  A61K45/06 ,  A61K31/4985 ,  C07D471/04 ,  A61K31/437

CPC classification number: A61K31/4985 ,  A61K31/437 ,  A61K45/06 ,  C07D403/12 ,  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。

公开(公告)号：US20180179200A1

公开(公告)日：2018-06-28

申请号：US15849798

申请日：2017-12-21

Applicant: H. Lundbeck A/S

Inventor： Jan Kehler ,  Lars Kyhn Rasmussen ,  Morten Langgard ,  Mikkel Jessing ,  Paulo Jorge Vieira Vital ,  Karsten Juhl ,  Mauro Marigo

IPC: C07D471/04 ,  A61P25/28 ,  A61P25/18 ,  A61P25/16 ,  A61P25/00

CPC classification number: C07D471/04 ,  A61P25/00 ,  A61P25/16 ,  A61P25/18 ,  A61P25/28 ,  C07D487/04 ,  C07D519/00

Abstract: The present invention provides compounds of formula (I) that are PDE1 enzyme inhibitors and their use as a medicament, in particular for the treatment of neurodegenerative disorders and psychiatric disorders. The present invention also provides pharmaceutical compositions comprising compounds of the invention and methods of treating disorders using the compounds of the invention.

公开(公告)号：US20150175584A1

公开(公告)日：2015-06-25

申请号：US14574425

申请日：2014-12-18

Applicant: H. LUNDBECK A/S

Inventor： Jan Kehler ,  Lars Kyhn Rasmussen ,  Morten Langgard

IPC: C07D405/12

CPC classification number: C07D405/12

Abstract: The present invention provides Quinazolin-THF-amines as PDE1 inhibitors and their use as a medicament, in particular for the treatment of neurodegenerative disorders and psychiatric disorders.

Abstract translation: 本发明提供Quinazolin-THF-胺作为PDE1抑制剂及其作为药物的用途，特别是用于治疗神经变性疾病和精神障碍。

公开(公告)号：US10351561B2

公开(公告)日：2019-07-16

申请号：US15849798

申请日：2017-12-21

Applicant: H. Lundbeck A/S

Inventor： Jan Kehler ,  Lars Kyhn Rasmussen ,  Morten Langgard ,  Mikkel Jessing ,  Paulo Jorge Vieira Vital ,  Karsten Juhl ,  Mauro Marigo

IPC: A61K31/4162 ,  A61K31/4188 ,  A61K31/437 ,  A61K31/5025 ,  C07D471/04 ,  C07D487/04 ,  A61P25/28 ,  A61P25/18 ,  A61P25/00 ,  A61P25/16 ,  C07D519/00

Abstract: The present invention provides compounds of formula (I) that are PDE1 enzyme inhibitors and their use as a medicament, in particular for the treatment of neurodegenerative disorders and psychiatric disorders. The present invention also provides pharmaceutical compositions comprising compounds of the invention and methods of treating disorders using the compounds of the invention.

公开(公告)号：US20150190395A1

公开(公告)日：2015-07-09

申请号：US14663706

申请日：2015-03-20

Applicant: H. Lundbeck A/S

Inventor： Andreas Ritzen ,  Morten Langgard ,  Jan Kehler ,  Jacob Nielsen ,  John Paul Kilburn ,  Mohamed M. Farah

IPC: A61K31/4985 ,  A61K45/06

CPC classification number: A61K31/4985 ,  A61K31/437 ,  A61K45/06 ,  C07D403/12 ,  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。

公开(公告)号：US09018217B2

公开(公告)日：2015-04-28

申请号：US14488554

申请日：2014-09-17

Applicant: H. Lundbeck A/S

Inventor： Andreas Ritzen ,  Morten Langgard ,  Jan Kehler ,  Jacob Nielsen ,  John Paul Kilburn ,  Mohamed M. Farah

IPC: C07D239/42 ,  C07D231/10 ,  C07D487/04 ,  C07D471/04 ,  A61K31/437 ,  A61K31/4985 ,  A61K45/06

CPC classification number: A61K31/4985 ,  A61K31/437 ,  A61K45/06 ,  C07D403/12 ,  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。