公开(公告)号：US10239849B2

公开(公告)日：2019-03-26

申请号：US15774157

申请日：2016-11-07

Applicant: Merck Sharp & Dohme Corp. ,  Michael T. Rudd ,  Edward J. Brnardic ,  Yuntae Kim ,  Robert S. Meissner ,  Vanessa L. Rada ,  Shawn J. Stachel ,  Celina V. Zerbinatti

Inventor： Michael T. Rudd ,  Edward J. Brnardic ,  Yuntae Kim ,  Robert S. Meissner ,  Vanessa L. Rada ,  Shawn J. Stachel ,  Celina V. Zerbinatti

IPC: C07D243/08 ,  C07D295/16 ,  C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/08 ,  C07D487/08 ,  C07D513/04 ,  A61P25/18 ,  A61P25/16 ,  A61P25/28 ,  A61P3/10

Abstract: In its many embodiments, the present invention provides substituted cyanopyridine containing compounds of the Formula (I): and acceptable salts thereof, wherein R1, R2, R3, R4, R5, X, Y, Q, and the moiety are as defined herein. The novel compounds of the invention, and pharmaceutically acceptable compositions comprising a compound thereof, are useful as Liver X-β receptor (LXRβ) agonists, and may be useful for treating or preventing pathologies related thereto. Such pathologies include, but are not limited to, inflammatory diseases and diseases characterized by defects in cholesterol and lipid metabolism, such as Alzheimer's disease.

公开(公告)号：US09278960B2

公开(公告)日：2016-03-08

申请号：US14356080

申请日：2012-10-26

Applicant: Merck Sharp & Dohme Corp.

Inventor： Christopher James Bungard ,  Antonella Converso ,  Barbara Hanney ,  Timothy John Hartingh ,  Peter J. Manley ,  Robert S. Meissner ,  James J. Perkins ,  Michael T. Rudd

IPC: C07D413/14 ,  C07D401/06 ,  C07D401/14 ,  C07D215/48 ,  C07D401/04 ,  C07D409/04 ,  C07D413/06 ,  C07D417/06 ,  C07D417/14 ,  C07D471/04 ,  C07D491/10

CPC classification number: C07D413/14 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/4985 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/541 ,  C07D215/48 ,  C07D401/04 ,  C07D401/06 ,  C07D401/14 ,  C07D409/04 ,  C07D413/06 ,  C07D417/06 ,  C07D417/14 ,  C07D471/04 ,  C07D491/10

Abstract: The present invention provides quinoline carboxamide and quinoline carbonitrile compounds of formula (I) wherein ring A, RQ, -L-, R1, n, R2, and R3 are as defined herein. The compounds of the invention are useful as non-competitive mGluR2 antagonists, or mGluR2 negative allosteric modulators (NAMs), and in methods of treating a patient (preferably a human) for diseases or disorders in which the mGluR2-NAM receptor is involved, such as Alzheimer's disease, cognitive impairment, schizophrenia and other mood disorders, pain disorders and sleep disorders, by administering to the patient a therapeutically effective amount of a compound of the invention, or a pharmaceutically acceptable salt thereof. The invention is also directed to pharmaceutical compositions comprising a compound of the invention, or a pharmaceutically acceptable salt thereof, (optionally in combination with one or more additional active ingredients), and a pharmaceutically acceptable carrier, and the use of the compounds and pharmaceutical compositions of the invention in the treatment of such diseases.

Abstract translation: 本发明提供式（I）的喹啉羧酰胺和喹啉腈化合物，其中环A，RQ，-L-，R1，n，R2和R3如本文所定义。 本发明的化合物可用作非竞争性mGluR2拮抗剂或mGluR2负变构调节剂（NAM），以及用于治疗患有（其中涉及mGluR2-NAM受体的疾病或病症）的患者（优选人）的方法，例如 作为阿尔茨海默病，认知障碍，精神分裂症和其他情绪障碍，疼痛障碍和睡眠障碍，通过向患者施用治疗有效量的本发明化合物或其药学上可接受的盐。 本发明还涉及包含本发明化合物或其药学上可接受的盐（任选与一种或多种另外的活性成分组合）和药学上可接受的载体的药物组合物，以及该化合物和药物组合物的用途 的本发明治疗这些疾病。