公开(公告)号：US09399651B2

公开(公告)日：2016-07-26

申请号：US14671452

申请日：2015-03-27

Applicant: Merck Sharp & Dohme Corp.

Inventor： Scott Wolkenberg ,  James C. Barrow ,  Michael S. Poslusney ,  Scott T. Harrison ,  Wesley B. Trotter ,  James Mulhearn ,  Kausik K. Nanda ,  Peter J. Manley ,  Zhijian Zhao ,  Jeffrey W. Schubert ,  Nathan R. Kett ,  Amy Zartman

IPC: C07D213/84 ,  A61K31/44 ,  C07F5/02 ,  A61K31/4412 ,  A61K31/4418 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/69 ,  A61K45/06 ,  C07D213/69 ,  C07D213/73 ,  C07D213/74 ,  C07D401/10 ,  C07D401/14 ,  C07D413/10 ,  C07D413/12 ,  C07D417/10 ,  C07D471/04 ,  C07D401/04 ,  C07D401/06

CPC classification number: C07F5/025 ,  A61K31/4412 ,  A61K31/4418 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/69 ,  A61K45/06 ,  C07D213/69 ,  C07D213/73 ,  C07D213/74 ,  C07D401/04 ,  C07D401/06 ,  C07D401/10 ,  C07D401/14 ,  C07D413/10 ,  C07D413/12 ,  C07D417/10 ,  C07D471/04

Abstract: The present invention relates to 4-pyridinone compounds which are inhibitors of catechol O-methyltransferase (COMT), and are useful in the treatment and prevention of neurological and psychiatric disorders and diseases in which COMT enzyme is involved. The present invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which COMT is involved.

公开(公告)号：US09266881B2

公开(公告)日：2016-02-23

申请号：US14357690

申请日：2012-11-09

Applicant: Merck Sharp & Dohme Corp.

Inventor： James C. Barrow ,  Christopher D. Cox ,  Mark B. Nolt ,  William D. Shipe

IPC: C07D471/04 ,  C07D401/14 ,  C07D413/14 ,  C07D401/06 ,  C07D403/06 ,  C07D417/14

CPC classification number: C07D471/04 ,  C07D401/06 ,  C07D401/14 ,  C07D403/06 ,  C07D413/14 ,  C07D417/14

Abstract: The present invention is directed to triazolopyridinone compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.

Abstract translation: 本发明涉及三唑并吡咯酮化合物，其可用作治疗与磷酸二酯酶10（PDE10）相关的中枢神经系统疾病的治疗剂。 本发明还涉及这些化合物用于治疗神经和精神疾病如精神分裂症，精神病或亨廷顿病以及与纹状体功能减退或基底神经节功能障碍相关的疾病的用途。

公开(公告)号：US20150024071A1

公开(公告)日：2015-01-22

申请号：US14502582

申请日：2014-09-30

Applicant: Merck Sharp & Dohme Corp.

Inventor： Scott Wolkenberg ,  Scott T. Harrison ,  James C. Barrow ,  Zhijan Zhao ,  Jeffrey Melamed ,  Nathan R. Kett ,  Amy Zartman

IPC: C07D401/14 ,  A61K45/06 ,  C07D239/553 ,  C07D401/10 ,  C07D239/54 ,  A61K31/513

CPC classification number: C07D401/14 ,  A61K45/06 ,  C07D239/54 ,  C07D239/553 ,  C07D401/10

Abstract: The present invention relates to 4-pyridinone compounds which are inhibitors of catechol O-methyltransferase (COMT), and are useful in the treatment and prevention of neurological and psychiatric disorders and diseases in which COMT enzyme is involved. The present invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which COMT is involved.

Abstract translation: 本发明涉及作为儿茶酚O-甲基转移酶（COMT）的抑制剂的4-吡啶酮化合物，可用于治疗和预防涉及COMT酶的神经和精神疾病和疾病。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及COMT的疾病中的用途。

公开(公告)号：US09260413B2

公开(公告)日：2016-02-16

申请号：US14502582

申请日：2014-09-30

Applicant: Merck Sharp & Dohme Corp.

Inventor： Scott Wolkenberg ,  Scott T. Harrison ,  James C. Barrow ,  Zhijan Zhao ,  Jeffrey Melamed ,  Nathan R. Kett ,  Amy Zartman

IPC: A61K45/06 ,  C07D401/14 ,  C07D239/54 ,  C07D239/553 ,  C07D401/10

CPC classification number: C07D401/14 ,  A61K45/06 ,  C07D239/54 ,  C07D239/553 ,  C07D401/10

Abstract: The present invention relates to 4-pyridinone compounds which are inhibitors of catechol O-methyltransferase (COMT), and are useful in the treatment and prevention of neurological and psychiatric disorders and diseases in which COMT enzyme is involved. The present invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which COMT is involved.

公开(公告)号：US20150299227A1

公开(公告)日：2015-10-22

申请号：US14671452

申请日：2015-03-27

Applicant: MERCK SHARP & DOHME CORP.

Inventor： Scott Wolkenberg ,  James C. Barrow ,  Michael S. Poslusney ,  Scott T. Harrison ,  Wesley B. Trotter ,  James Mulhearn ,  Kausik K. Nanda ,  Peter J. Manley ,  Zhijian Zhao ,  Jeffrey W. Schubert ,  Nathan R. Kett ,  Amy Zartman

IPC: C07F5/02 ,  A61K31/4418 ,  C07D401/04 ,  A61K31/4439 ,  C07D213/73 ,  C07D213/74 ,  A61K31/69 ,  A61K31/444 ,  C07D401/14 ,  C07D471/04 ,  C07D401/06 ,  A61K31/4725 ,  A61K31/4709 ,  A61K45/06 ,  C07D213/69

CPC classification number: C07F5/025 ,  A61K31/4412 ,  A61K31/4418 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/69 ,  A61K45/06 ,  C07D213/69 ,  C07D213/73 ,  C07D213/74 ,  C07D401/04 ,  C07D401/06 ,  C07D401/10 ,  C07D401/14 ,  C07D413/10 ,  C07D413/12 ,  C07D417/10 ,  C07D471/04

Abstract: The present invention relates to 4-pyridinone compounds which are inhibitors of catechol O-methyltransferase (COMT), and are useful in the treatment and prevention of neurological and psychiatric disorders and diseases in which COMT enzyme is involved. The present invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which COMT is involved.

公开(公告)号：US20140343053A1

公开(公告)日：2014-11-20

申请号：US14357690

申请日：2012-11-09

Applicant: Merck Sharp & Dohme Corp.

Inventor： James C. Barrow ,  Christopher D. Cox ,  Mark B. Nolt ,  William D. Shipe

IPC: C07D471/04

CPC classification number: C07D471/04 ,  C07D401/06 ,  C07D401/14 ,  C07D403/06 ,  C07D413/14 ,  C07D417/14

Abstract: The present invention is directed to triazolopyridinone compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.

Abstract translation: 本发明涉及三唑并吡咯酮化合物，其可用作治疗与磷酸二酯酶10（PDE10）相关的中枢神经系统疾病的治疗剂。 本发明还涉及这些化合物用于治疗神经和精神疾病如精神分裂症，精神病或亨廷顿病以及与纹状体功能减退或基底神经节功能障碍相关的疾病的用途。